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100% found this document useful (1 vote)

689 views

AICTE Sponsored SCOPE Conference Proceedings PDF

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Pustaka Helvetia

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ALL INDIA COUNCIL FOR TECHNICAL EDUCATION (AICTE) NEW DELHI

SMRITI COLLEGE OF PHARMACEUTICAL EDUCATION, INDORE, CONFERENCE PROCEEDINGS I PAGE- I

ALL INDIA COUNCIL FOR TECHNICAL EDUCATION (AICTE) NEW DELHI
Sponsored National Conference
“Global Perspective towards green Pharmacy and Modern era of Phyto-Pharmaceuticals”
18th January, 2020
Organized by Smriti College of Pharmaceutical Education, Indore

About Institute
Smriti College of Pharmaceutical Education, Indore
(SCOPE) is a premier institute of central India, imparting
pharmaceutical education in a quality manner to stir out
technically competent pharmacist and job-ready post
graduates. Nestled on MR 11 near flourishing bypass, SCOPE was founded in 1999 under the aegis of
B. R. Nahata Smriti Sansthan with an objective “Quality Education for All”. Carving a niche in
pharmaceutical education, we are the forefront of research ever since BRNSS group launched the
first private organization that has started UG and PG courses in the Madhya Pradesh.

SCOPE academics have been benchmarked against the best prevailing standards with regular up
gradation. It is our belief that value based learning, leading to total personality development and
expertise of student and the faculties will be long lasting contribution to the overall growth &
development of our Nation and society. Our contribution has been phenomenal in innovations,
publications, presentations by faculty members and research from budding pharmacists and
scholars. We advocate skill based education rather than rote learning for syllabus driven and exam
oriented approach.

We are the only institute running exclusively pharmacy course both UG and PG level in Madhya
Pradesh. Our courses are approved by AICTE and PCI and Affiliated to RGPV. We are the only
institute accredited by NBA in the year 2013 and also secured platinum rank in AICTE CII Survey in
Indore region.

SMRITI COLLEGE OF PHARMACEUTICAL EDUCATION, INDORE, CONFERENCE PROCEEDINGS I PAGE- II

About Conference
Smriti College of Pharmaceutical Education, Indore is organizing one day national Conference at
college premises on 18th January, 2020. The theme of the AICTE Sponsored National Conference is
“Global Perspective towards green Pharmacy and Modern era of Phyto-Pharmaceuticals”
The most knowledgeable Pharmaceutical Researchers, intellectuals, academicians and scientists
spearheading the pharmacy education throughout the country, are participating in the conference
to explore this influential theme.

The conference, besides technical, scientific sessions and poster presentations, will also published
the presented research papers in International Journal of Pharmaceutical Sciences and Research.

The convention will facilitate intellectuals to come with their expertise, novel ideas, innovations,
technical modules on one platform which will definitely help to improve the pharmacy profession as
a whole in India.

The conference will discuss various aspects of drug discovery from the traditional medicine. The
knowledge and expert advices gained in the conference will bring a deeper understanding of
phytochemistry, pharmacognosy and ethnopharmacology to support the production of new and safe
pharmacologically active compounds with minimal undesired toxic effects.

IMPORTANCE OF THE EVENT

Traditional herbal medicines are naturally occurring plant-derived substances with minimal or no
industrial processing that have been used to treat illness within local or regional healing practices.
Traditional herbal medicines are getting significant attention in global health debates. Medicinal
plants have become the focus of intense study recently in terms of discovering new drugs and as to
whether their traditional uses are supported by pharmacological effects. The R&D thrust in the
pharmaceutical sector is focused on development of new drugs, innovative/indigenous processes for
known drugs and development of plant-based drugs through investigation of leads from the
traditional systems of medicine. Nowadays there is a renewed interest in investigating plants for
medically useful compounds, with some of the leading pharmaceutical and research institutions
involved in this search. More than 50% of the 25 best-selling drugs worldwide were related directly
to natural products.

The search for a new drug from nature is based on a biological and ecological rationale. Herbal
medicines have provided many effective drugs. These include older drugs such as quinine and
morphine and newer drugs such as paclitaxel, camptothecin, etoposide, mevastatin, and artemisinin.

SMRITI COLLEGE OF PHARMACEUTICAL EDUCATION, INDORE, CONFERENCE PROCEEDINGS I PAGE- III

Herbal medicines have thus played an important role in drug discovery in the past and promise to
provide still more drugs in the future. The discovery of novel drugs from nature is also important
because many isolated molecules are quite complex, and would not be obtained by a simple
synthetic approach. Most bioactive compounds of natural origin are secondary metabolites, i.e.
species-specific chemical agents that can be grouped into various categories.
In view of the wide range of medicinal plant and their traditional claim it is imperative that more
preclinical and clinical studies should be conducted to investigate unexploited potential of this
traditional knowledge. Hence this conference is an effort to make people more aware about the
importance of herbal medicines and potential of medicinal plants.

TOPICS TO BE DISCUSSED
This conference will deal with various aspects of Herbal Medicines as a Foundation for Drug
Discovery such as:
 Present status of Drug discovery from Medicinal Plants
 Herbal medicine research and global health: an ethical analysis
 Challenges and Future Directions of Herbal Medicine Research
 Herbal Medicine Today: Clinical and Research Issues
 Research Methodological Issues in Evaluating Herbal Interventions

EXPECTED OUTCOME
Plant base drugs provide outstanding contribution to modern therapeutics. The knowledge and
expert advices gained in the conference will bring an deeper understanding of phytochemistry,
pharmacognosy and ethnopharmacology to support the production of new and safe
pharmacologically active compounds with minimal undesired toxic effects.

SMRITI COLLEGE OF PHARMACEUTICAL EDUCATION, INDORE, CONFERENCE PROCEEDINGS I PAGE- IV

Chairman Message
Welcome to Smriti College of Pharmaceutical Education in AICTE sponsored National
Conference on “Global Perspective towards green Pharmacy and Modern era of Phyto-
Pharmaceuticals” on 18th January 2020.

A majority of the world's population in developing countries still relies on herbal

medicines to meet its health needs. Herbal medicines are often used to provide first-line
and basic health service, both to people living in remote areas where it is the only
available health service, and to people living in poor areas where it offers the only
affordable remedy. Even in areas where modern medicine is available, the interest on
herbal medicines and their utilization have been increasing rapidly in recent years. Hence
it is the need of the day to share knowledge and experiences in the field of herbal research.
This conference emphasizes the importance of herbal medicine as a foundation for drug
discovery. I expect this conference will definitely provide a good platform for drug
discovery and development from natural sources.

I am sure this conference will provide an excellent opportunity to share the experiences
and perspectives among the participants. I would like to extend my heartiest welcome to
all delegates and wish them a very beneficial participation and make this conference a
successful event.

I also extend my best wishes to the organizers for the success of the conference.

Shri Narendra Nahata

Chairman, B.R. Nahata Smriti Sansthan
Mandsaur

SMRITI COLLEGE OF PHARMACEUTICAL EDUCATION, INDORE, CONFERENCE PROCEEDINGS I PAGE- V

Executive Chairman Message

I am glad to discern that Smriti College of Pharmaceutical Education is organizing a
National Conference on “Global Perspective towards green Pharmacy and Modern era of
Phyto-Pharmaceuticals” on 18th January 2020.

The WHO has indicated that as many as 80% of all people living in the world make use of
herbal medicine as their main source of healthcare. Many of the pharmaceuticals which
are currently used can be traced back to herbal remedies which were developed many
centuries ago.

Both pharmacognosists and natural practitioners are looking in different parts of the
globe to find natural chemicals that can be used in the treatment of numerous diseases.
This event will be an excellent opportunity for the scientists to encourage the profound
administration of herbs as medicament and explore the best case reports where ultimate
results to justify curing and healing by various herbals. Various ailments have also been
noted with evidence proving herbals to be the righteous option for treating chronic
ailments.

I am sure that this conference will provide a unique opportunity to the budding pharmacy
professionals to update their knowledge and understand the importance of herbal
medicine in the field of drug discovery.

I extend my corroboration to the organizers for the immeasurable success of the event.

Shri Rahul Nahata

Executive Chairman, B.R. Nahata Smriti Sansthan
Mandsaur

SMRITI COLLEGE OF PHARMACEUTICAL EDUCATION, INDORE, CONFERENCE PROCEEDINGS I PAGE- VI

Convener Message
I am humbled and privileged to be Convener of National Conference on “Global Perspective
towards green Pharmacy and Modern era of Phyto-Pharmaceuticals” on 18th January
2020.

It’s a great honour and pleasure for me to invite you all to participate in the national
conference. The usage of herbs to treat variety of ailments is universal, and exists in every
human culture on Earth. Despite this, the largest use of medical herbs occurs in societies which
are not fully industrialized. Because of the high costs involved with manufacturing modern
medicines, many people living in developing nations simply do not have the financial resources
to pay for them, and as a result, they are forced to use natural herbs as an affordable
alternative. In recent years, many people living in industrialized countries have a second look
at herbal medicines due to the rising cost of medicine and healthcare in their own nations.
There are a number of herbal systems that dominate the world today, and these systems are
Chinese herbs, Ayurvedic medicine, Roman and Greek herbs, and Shamanic herbs.

The conference anticipates two hundred aspirant delegates including keynote speakers and
poster presentations by students which will craft a platform for herbal medicines role in the
field of drug discovery. The current conference will be helpful to explore the potential of
Herbal medicines in present scenario as well as for the future perspectives of herbal medicines.

I am sure that this conference will provide an opportunity to share the experiences and
perspectives among the participants. I would also like to extend my heartiest welcome to all
delegates and wish them a very beneficial participation and make this conference a successful
event.

Dr. Neelesh Malviya

Principal, Smriti College of Pharmaceutical Education
Indore

SMRITI COLLEGE OF PHARMACEUTICAL EDUCATION, INDORE, CONFERENCE PROCEEDINGS I PAGE- VII

ORGANIZING COMMITTEE
CONVENER

Dr. Neelesh Malviya

REGISTRATION COMMITTEE SCIENTIFIC COMMITTEE SPONSORSHIP COMMITTEE

Mr. Tahir Nizami Mrs. Kushagra Dubey Mr. Rajiv Saxena

Mr.Ankit Mangal Mrs.Ruchi Gupta Ms. Namrata Mrs. Darshana Mrs. Neelima Ms. Yashu
Rathore Patidar Salvi Chourasiya

TECHNICAL COMMITTEE HOSPITALITY COMMITTEE MEDIA COMMITTEE

Mrs. Arti J Majumdar Mr. Anindya Goswami Mrs. Himani Singh

Ms. Priya Mourya

Mrs. Archana Patidar Ms. Vishakha Chauhan

SMRITI COLLEGE OF PHARMACEUTICAL EDUCATION, INDORE, CONFERENCE PROCEEDINGS I PAGE- VIII

Conference Report
Smriti College of Pharmaceutical Education organized AICTE Sponsored one
day National Conference on “Global perspective Towards Green Pharmacy
and Modern Era of Phyto-Pharmaceuticals” on 18th January 2020.

Introduction
The theme of national conference was befitting the present scenario of Global Perspective
towards green Pharmacy and Modern era of Phyto-pharmaceuticals. The objective of the
seminar was to provide a very good platform in which researchers, herbalists, experts from
industries and renowned academicians engaged in drug discovery and development from
across the nation share experience and perspective of phyto-pharmaceuticals research
among the participants.

About 300 delegates from all over India have attended the conference and got benefited by
getting the new ideas on modern era of green pharmacy and phyto-pharmaceuticals shared
by renowned academicians and experts from industries.

SMRITI COLLEGE OF PHARMACEUTICAL EDUCATION, INDORE, CONFERENCE PROCEEDINGS I PAGE- IX

Prof. Shailendra Saraf, Vice President, Pharmacy Council of India, New Delhi, Prof.
Swarnalata Saraf, Prof. University of Pharmacy, Pt. Ravishankar Shukla University, Raipur,
Dr. D.K. Jain, Director, College of Pharmacy, IPS Academy, Indore, Prof. P.K. Dubey, Principal,
Swami Vivekanand, College of Pharmacy, Indore, Prof. Vimal Kumar, Dean and Principal,
School of Pharmacy, ITM, Barodra University, Varoda, Dr. Deependra Singh, Asst. Prof.
University, Institute of Pharmacy, Pt. Ravishankar Shukla University, Raipur and Dr. Tanveer
Naved, Joint Head, Amity Institute of Pharmacy, Amity University, Noida had shared their
experience and thoughts on current researches on phyto-pharmaceuticals, use and
importance of green pharmacy in the modern era, and many more.

SMRITI COLLEGE OF PHARMACEUTICAL EDUCATION, INDORE, CONFERENCE PROCEEDINGS I PAGE- X

Inauguration Ceremony
The conference was inaugurated by chief guest Prof. Shailendra Saraf, and started with
lightening the lamp and saraswati vandana. Dr. Neelesh Malviya, Principal, Smriti College of
Pharmaceutical Education, Indore welcomed chief guest, chief speaker, guest of honour and
resource persons by presenting them bouquet.

The conference was started by the enlightening words of the Principal of Smriti College of
Pharmaceutical Education, Indore, Dr. Neelesh Malviya about the importance of green
pharmacy and phyto-pharmaceuticals in the modern era.

SMRITI COLLEGE OF PHARMACEUTICAL EDUCATION, INDORE, CONFERENCE PROCEEDINGS I PAGE- XI

Prof. Shailendra Saraf informed that green pharmacy is the modern translation of ayurveda.
He also discussed about uniqueness and quality of herbal products, shared new ideas for
research in herbal trade.

Prof. Swarnalata Saraf shared her experience as a woman leader and also highlighted
woman leadership. As ayurveda is native to India, India is known all over the world for its
spices that are not only used in food but also as home remedy to cure and prevent various
diseases. She said everyone of us must use green treatment as it is free from toxic effects.
She also discussed scale up techniques that can be adopted by academicians in new
researches.

SMRITI COLLEGE OF PHARMACEUTICAL EDUCATION, INDORE, CONFERENCE PROCEEDINGS I PAGE- XII

Dr. D.K. Jain shared his experience in research and also the ideas to promote green
pharmacy. Also discussed about water conservation techniques.

Prof. P.K. Dubey shared basic concepts behind green pharmacy, education for appropriate
use and disposal of unused or expired drugs. He explained rationale and significance of
herbal products. Use of biosensors and importance in modern era.

SMRITI COLLEGE OF PHARMACEUTICAL EDUCATION, INDORE, CONFERENCE PROCEEDINGS I PAGE- XIII

Abstract Book Release

More than 200 abstracts had been received by the scientific committee, out of which 135
abstracts were approved after the proper validation for the poster presentation. These
abstracts were published in the abstract book which was released during the ceremony.

Felicitation of Guests
Smriti College of Pharmaceutical Education, Indore feel privileged to welcome our
distinguished guests who graced the occasion with their auspicious presence. We extend
our gratitude of thanks and as a token of remembrance presented mementoes to the
guests.

SMRITI COLLEGE OF PHARMACEUTICAL EDUCATION, INDORE, CONFERENCE PROCEEDINGS I PAGE- XIV

Technical Sessions
Prof. Vimal Kumar Jain highlighted modern lifestyle and eating habits. Changes in diet and
daily habits that may not only prevent but also may cure diseases. He discussed some of the
remedies, herbal researches that are already dictated in charaksayantam, also discussed
some vegetables which are beneficial in many health conditions.

Dr. Deependra Singh highlighted current scenario and future aspects of herbal drugs, scope
in herbal industries, opportunities, limitations of herbal products and conservation in
biodiversity.

SMRITI COLLEGE OF PHARMACEUTICAL EDUCATION, INDORE, CONFERENCE PROCEEDINGS I PAGE- XV

Dr. Tanveer Naved enlightened all with the benefits of nutraceuticals and herbal products.
Consuming nutraceuticals may improve health, delay aging, prevent chronic diseases,
support functions of body and also may increase life expectancy.

Mr. Amit Palande, Application Chemist, Anchrom Enterprises (I), Pvt, Ltd, Mumbai discussed
uses of High Performance Thin Layer Chromatography and its applications in herbal drug
formulation.

Poster Presentation Session

The poster presentation session was followed by the conference which was inaugurated by
Prof. Shailendra Saraf and Prof. Swarnlata Saraf. In the poster presentation session, nearly
135 posters accepted by the scientific committee had been displayed. The abstracts for
poster presentation had been called with relation to distinctive themes of Pharmaceutical
Sciences: Pharmaceutical Technology, Medicinal Chemistry, Pharmaceutical Analysis, Quality

SMRITI COLLEGE OF PHARMACEUTICAL EDUCATION, INDORE, CONFERENCE PROCEEDINGS I PAGE- XVI

Assurance, Pharmacognosy, Phytochemistry, Pharmacology and Toxicology and Regulatory

Affairs. The posters were evaluated by the judges.

Valedictory Function
Participants who scored first, second and third position in poster presentation in different
trades (Pharmaceutics, pharmacognosy, pharmacology and pharmaceutical chemistry) were
honored with certificate and memento.

The conference was successfully concluded with high tea. The organizing committee had put
all their efforts to make this event a successful one.

SMRITI COLLEGE OF PHARMACEUTICAL EDUCATION, INDORE, CONFERENCE PROCEEDINGS I PAGE- XVII

International Journal of
Pharmaceutical Sciences and Research
ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

SELECTED RESEARCH PAPERS

S. PRESENTING
TITLE OF PAPER COLLEGE NAME PAGE NO.
NO. AUTHOR
1. FORMULATION AND GAURAV JAIN A.P. J. ABDUL KALAM UNIVERSITY, 8-10
EVALUATION OF MATRIX INDORE, M.P. (INDIA)
TYPE TRANSDERMAL
PATCHES OF LULICONAZOLE

2. FORMULATION DESIGN AND KULDEEP SCHOOL OF PHARMACY-DEVI 11-13

EVALUATION OF WATER VINCHURKAR AHILYAVISHWAVIDYALAYA,
DISPERSIBLE TABLET OF INDORE, M.P. (INDIA
GUAIFENESIN FOR
PAEDIATRIC USE

3. FORMULATION DESIGN AND SHEETAL MANE SCHOOL OF PHARMACY-DEVI 14-16

EVALUATION OF FAST AHILYAVISHWAVIDYALAYA,
DISSOLVING TASTE MASKED INDORE, M.P. (INDIA)
TABLET OF LAFUTIDINE

4. SYNTHESIS AND EKTA YADAV SWAMI VIVEKANAND COLLEGE 17-18

CHARACTERIZATION OF OF PHARMACY, INDORE, M.P.
SILVER NANO PARTICLES (INDIA)
USING PLANT
POMEGRANATE (PUNICA
GRANATUM)

5. EVALUATION OF BHAWANA SHRI DEVBHOOMI INSTITUTE OF 19-21

TRANSDERMAL PATCHES OF KAPOOR SCIENCES AND TECHNOLOGY,
LORNOXICAM PAUNDHA, DEHRADUN, (INDIA)

6. DEVELOPMENT AND ADITYA SHARMA SMRITI COLLEGE OF 22-23

CHARACTERIZATION OF PHARMACEUTICAL EDUCATION,
HERBAL FACIAL TONIC INDORE, M.P. (INDIA)

7. FORMULATION AND JANHVI YADAV SMRITI COLLEGE OF 24-25

EVALUATION OF HERBAL PHARMACEUTICAL EDUCATION,
HAIR SERUM INDORE, M.P. (INDIA)

8. DEVELOPMENT AND VISHAKHA SMRITI COLLEGE OF 26-27

CHARACTERIZATION OF CHAUHAN PHARMACEUTICAL EDUCATION,
HERBAL FACE SERUM INDORE, M.P. (INDIA)

9. DEVELOPMENT AND HIMANI SINGH SMRITI COLLEGE OF 28-29

EVALUATION OF FLAX SEED PHARMACEUTICAL EDUCATION,
AND GREEN TEA HAIR INDORE, M.P. (INDIA)
GEL: A NATURAL HAIR
STYLER

10. FORMULATION AND HARSHAL SMRITI COLLEGE OF 30-31

EVALUATION OF DESHMUKH PHARMACEUTICAL EDUCATION,
CUCURBITA PEPO HERBAL INDORE, M.P. (INDIA)
FACIAL SCRUB

International Journal of Pharmaceutical Sciences and Research: Conference Proceedings: Special ssue; March, 2020 Page | 1
International Journal of
Pharmaceutical Sciences and Research
ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

S. PRESENTING
TITLE OF PAPER COLLEGE NAME PAGE NO.
NO. AUTHOR
11. APPLICATION OF MADHAVI MANDSAUR UNIVERSITY, REWAS 32-34
LIQUISOLID TECHNIQUE TO KASTURI DEWDA ROAD, MANDSAUR, M.P.
ENHANCE SOLUBILITY AND (INDIA)
DISSOLUTION PROFILE OF
FLURBIPROFEN

12. FORMULATION AND NAMRATA SMRITI COLLEGE OF 35-38

EVALUATION OF HERBAL RATHORE PHARMACEUTICAL EDUCATION,
ANTIBACTERIAL SOAP FOR INDORE, M.P. (INDIA)
TREATMENT OF ACNE

13. PREPARATION AND ARTI SMRITI COLLEGE OF 39-41

CHARACTERIZATION OF MAJUMDAR PHARMACEUTICAL EDUCATION,
DOCETAXEL LOADED NANO INDORE, M.P. (INDIA)
LIPID CARRIERS

14. IN-VITRO FORMULATION ASHIMA AHUJA INSTITUTE OF PHARMACEUTICAL 42-44

AND EVALUATION OF RESEARCH, GLA UNIVERSITY,
LAMIVUDINE MATHURA-281406, U.P. (INDIA)
TRANSDERMAL PATCHES

15. FORMULATION, JITENDRA INSTITUTE OF PHARMACEUTICAL 45-47

CHARACTERIZATION AND GUPTA RESEARCH, GLA UNIVERSITY,
ANTIMICROBIAL ACTIVITY MATHURA-281406, U.P. (INDIA)
OF POLYHERBAL HAND
WASH

16. DEVELOPMENT AND NEELIMA SALVI SMRITI COLLEGE OF 48-49

CHARACTERIZATION OF PHARMACEUTICAL EDUCATION,
SOLID LIPID INDORE, M.P. (INDIA)
NANOPARTICLES
CONTAINING RUTIN FOR
THE MANAGEMENT OF
DIABETES MELLITUS

17. PREPARATION AND ABRAR HUSSAIN SMRITI COLLEGE OF 50-51

EVALUATION OF NOVEL IN- PHARMACEUTICAL EDUCATION,
SITU GEL CONTAINING INDORE, M.P. (INDIA)
ACYCLOVIR FOR THE
TREATMENT OF HERPES
SIMPLEX KERATITIS

18. FORMULATION AND DIPALI TRIVEDI SMRITI COLLEGE OF 52-53

EVALUATION OF FLOATING PHARMACEUTICAL EDUCATION,
TABLET OF RILPIVIRINE INDORE, M.P. (INDIA)
HYDROCHLORIDE FOR THE
TREATMENT OF HIV-1

19. FORMULATION AND FARHEEN NAAZ SMRITI COLLEGE OF 54-55

EVALUATION OF PHARMACEUTICAL EDUCATION,
TRANSDERMAL PATCH OF INDORE, M.P. (INDIA)
FEBUXOSTAT FOR
MANAGEMENT OF GOUT

International Journal of Pharmaceutical Sciences and Research: Conference Proceedings: Special ssue; March, 2020 Page | 2
International Journal of
Pharmaceutical Sciences and Research
ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

S. PRESENTING
TITLE OF PAPER COLLEGE NAME PAGE NO.
NO. AUTHOR
20. FORMULATION AND NARGIS KHAN SMRITI COLLEGE OF 56-57
EVALUATION OF PHARMACEUTICAL EDUCATION,
FEBUXOSTAT AND INDORE, M.P. (INDIA)
DICLOFENEC SODIUM
EMULGEL FOR
MANAGEMENT OF GOUT

21. FORMULATION AND PRIYANSHI SMRITI COLLEGE OF 58-59

EVALUATION OF ENTRIC SAHU PHARMACEUTICAL EDUCATION,
COATED TABLET OF INDORE, M.P. (INDIA)
TENOFOVIER ALAFENAMIDE
FUMARATE

22. FORMULATION AND RAHUL SMRITI COLLEGE OF 60-61

EVALUATION OF ORLISTAT VISHVAKARMA PHARMACEUTICAL EDUCATION,
LOADED MICROSPONGES INDORE, M.P. (INDIA)
FOR THE TREATMENT OF
OBESITY

23. FORMULATION AND URVASHI JAIN SMRITI COLLEGE OF 62-63

EVALUATION OF PHARMACEUTICAL EDUCATION,
SUBLINGUAL TABLET OF INDORE, M.P. (INDIA)
TENOFOVIR ALAFENAMIDE
FUMARATE USING SOLID
DISPERSION TECHNIQUE

24. FORMULATION PRIYA MOURYA SMRITI COLLEGE OF 64-66

DEVELOPMENT AND PHARMACEUTICAL EDUCATION,
EVALUATION OF NANO INDORE, M.P. (INDIA)
LIPPOIDAL CARRIER FOR
THE TOPICAL DELIVERY OF
CISPLATIN

25. DEVELOPMENT & URVASHI ORIENTAL UNIVERSITY, GATE 67-72

EVALUATION OF ANTI ACNE SHARMA NO.1, SANWER ROAD, JAKHYA,
CREAM USING EXTRACTS OF OPPOSITE REVATI RANGE,
VITEX NEGUNDO AND INDORE, M.P. (INDIA)
HIBISCUS ROSA-SINENSIS

26. FORMULATION AND SANJAY K. CHAMELI DEVI INSTITUTE OF 73-76

EVALUATION OF MISHRA PHARMACY, INDORE, M.P.(INDIA)
CONTROLLED RELEASE
FLOATING TABLETS OF
NIZATIDINE USING
HYDROPHILIC POLYMERS
27. FORMULATION, SHIKHA JAISWAL DEPARTMENT OF 77-78
DEVELOPMENT AND PHARMACEUTICS, DR. APJ ABDUL
EVALUATION OF KALAM UNIVERSITY, M.P.(INDIA)
NANOMIEMGEL FOR THE
TREATMENT OF SKIN
DISEASE

International Journal of Pharmaceutical Sciences and Research: Conference Proceedings: Special ssue; March, 2020 Page | 3
International Journal of
Pharmaceutical Sciences and Research
ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

S. PRESENTING
TITLE OF PAPER COLLEGE NAME PAGE NO.
NO. AUTHOR
28. FORMULATION AND ASHISH GUPTA ACROPOLIS INSTITUTE OF 79-81
EVALUATION OF PHARMACEUTICAL
MEDICATED NAIL LACQUER EDUCATION AND RESEARCH
OF TERBINAFINE INDORE M.P.(INDIA)
HYDROCHLORIDE FOR THE
TREATMENT OF
ONYCHOMYCOSIS

29. FORMULATION AND DARSHANA SMRITI COLLEGE OF 82-83

EVALUTION OF HERBAL SHAMA PHARMACEUTICAL EDUCATION,
SHAMPOO CONTAINING INDORE, M.P. (INDIA)
EXTRACTS OF ALLIUM CEPA
AND ANNONA SQUAMOSA.

30. MORPHOLOGICAL STUDIES DEEPIKA PATEL A.P.J. ABDUL KALAM UNIVERSITY, 84-85
OF FEW HERBS USED IN THE INDORE, M.P. (INDIA)
TREATMENT OF LIVER
DISORDERS

31. ANTI-CANDIDAL ACTIVITY SHWETA A.P. J. ABDUL KALAM UNIVERSITY, 86-87

OF HERBAL FORMULATIONS SHRIWAS INDORE, M.P. (INDIA)
CONTAINING HYDRO-
ALCOHOLIC EXTRACT OF
IPOMEA CAIRICA LINN.
(LEAVES) USED FOR THE
TREATMENT OF VAGINAL
INFECTION

32. STUDY OF ANTIOXIDANT PRAGYA SOFTVISION COLLEGE AND 88-90

PROPERTIES OF RATHORE RESEARCH CENTER, INDORE, M.P.
HYLOCEREUS UNDULATES (INDIA)
(DRAGON FRUIT)

33. Α-AMYLASE INHIBITORY RAJIV SAXENA SMRITI COLLEGE OF 91-93

ACTIVITY OF JASMINUM PHARMACEUTICAL EDUCATION,
SAMBAC FOR THE INDORE, M.P. (INDIA)
MANAGEMENT OF
DIABETES AND ITS
COMPLICATIONS

34. FORMULATION AND RUCHI GUPTA SMRITI COLLEGE OF 94-95

EVALUATION OF HERBAL PHARMACEUTICAL EDUCATION,
ANTITUSSIVE ASH SYRUP OF INDORE, M.P. (INDIA)
COCOS NUSIFERA IN MICE

35. PRELIMINARY REENA GUPTA INSTITUTE OF PHARMACEUTICAL 96-98

PHYTOCHEMICAL ANALYSIS RESEARCH, GLA UNIVERSITY,
AND ANTIMICROBIAL MATHURA-281406, U.P. (INDIA)
ACTIVITY OF HERBAL HAND
SANITIZER GEL

International Journal of Pharmaceutical Sciences and Research: Conference Proceedings: Special ssue; March, 2020 Page | 4
International Journal of
Pharmaceutical Sciences and Research
ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

S. PRESENTING
TITLE OF PAPER COLLEGE NAME PAGE NO.
NO. AUTHOR
36. EFFECT OF EXTRACT OF ASHISH ORIENTAL UNIVERSITY, GATE 99-101
CENTELLA ASIATICA ON PAGARIYA NO.1, SANWER ROAD, JAKHYA,
INFLAMAMATION: AN IN OPPOSITE REVATI RANGE,
VIVO STUDY INDORE, M.P. (INDIA)

37. PHYTOCHEMICAL KANCHAN INSTITUTE OF PHARMACEUTICAL 102-103

SCREENING AND MATHUR RESEARCH, GLA UNIVERSITY,
HEPATOPROTECTIVE EFFECT CHAUMUHAN, MATHURA-
OF HYDROALCOHOLIC 281406, U.P. (INDIA)
EXTRACT OF OXALIS
CORNICULATA LINN IN MICE
38. HERBAL ANTIDANDRUFF PRERNA MM SCHOOL OF PHARMACY, MM 104-105
POWDER SHAMPOO SHARMA UNIVERSITY, SADOPUR
(AMBALA), HARYANA, (INDIA)

39. REPELLENT EFFICACY OF DEEPAK KUMAR A.P.J. ABDUL KALAM UNIVERSITY, 106-108
SOME ESSENTIAL OILS GUPTA INDORE, M.P. (INDIA)
AGAINST THE MOSQUITO

40. PHYTOCHEMICAL ISHAN DUBEY SURESH GYAN VIHAAR 109-111

EVALUATION AND UNIVERITY, JAIPUR, RJ, (INDIA)
ANTIOXIDANT ACTIVITY OF
LEAVES OF CINNAMOMUM
TAMALA

41. COMPARATIVE ANTI NITU SINGH ORIENTAL COLLEGE OF 112-113

DIARRHOEAL ACTIVITY OF PHARMACY AND RESEARCH
DADIMASHTAKA CHURNA INDORE, M.P. (INDIA)
AND MARKETED
FORMULATIONS

42. INSULIN MIMICS ACTIONS VIKAS B D. Y. PATIL INSTITUTE OF 114-116

OF POLY-HERBAL GAWALI PHARMACEUTICAL SCIENCES AND
FORMULATION (HF) AND ITS RESEARCH,PIMPRI, PUNE (INDIA)
ANTI-HYPERGLYCEMIC
EFFECTS ON ALBINO RATS

43. COMPARATIVE STUDY ON YAMINI BM COLLEGE OF 117-122

EFFECT OF NATURAL CHAURASIA PHARMACEUTICAL EDUCATION
SUPERDISINTEGRANTS IN AND RESEARCH, INDORE, M.P.
THE FORMULATION OF (INDIA)
AMLAKYADI CHURNA
TABLET

44. EFFECT OF ETHANOLIC RUPESH SONI B. R. NAHATA COLLEGE OF 123-125

EXTRACT OF TERMINALIA PHARMACY - CRC, MANDSAUR
CHEBULA FRUITS ON UNIVERSITY, MANDSAUR, M.P.
ADVANCE GLYCATION END (INDIA)
PRODUCTS IN
EXPERIMENTAL STZ
DIABETIC RATS

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International Journal of
Pharmaceutical Sciences and Research
ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

S. PRESENTING
TITLE OF PAPER COLLEGE NAME PAGE NO.
NO. AUTHOR
45. ANTI-ALZHEIMER ACTIVITY ANKUR JOSHI MANDSAUR UNIVERSITY, 126-127
OF TERMINALIA MANDSAUR, M.P. (INDIA)
CATAPPAFRUIT EXTRACTIN
STREPTOZOTOCIN INDUCED
ALZHEIMER IN
EXPERIMENTAL RATS

46. “EVALUATION OF JYOTI YADAV OXFORD INTERNATIONAL 128-129

ANTIBACTERIAL ACTIVITY OF COLLEGE, INDORE, M.P. (INDIA)
ANNONA SQUAMOSA
LEAVES EXTRACT”

47. EFFECT OF FLAVONOID AKANCHA ORIENTAL UNIVERSITY, GATE 130-133

FRACTION OF BUTEA GODRE NO.1, SANWER ROAD, JAKHYA,
MONOSPERMA ON OPPOSITE REVATI RANGE,
RHEUMATOID ARTHRITIS: INDORE, M.P. (INDIA)
AN IN VIVO STUDY

48. WOUND HEALING ACTIVITY MAYURI ORIENTAL UNIVERSITY, GATE 134-136

OF FLAVONOID FRACTION CHOUDHARY NO.1, SANWER ROAD, JAKHYA,
OF JUGLANS REGIA LINN. IN OPPOSITE REVATI RANGE,
DIABETIC RATS BY INDORE, M.P. (INDIA)
DIFFERENT WOUND
MODELS

49. EFFECT OF METHANOLIC URMILA ORIENTAL UNIVERSITY, GATE 137-140

EXTRACT OF ALSTONIA SONATA NO.1, SANWER ROAD, JAKHYA,
SCHOLARIS IN DIFFERENT OPPOSITE REVATI RANGE,
MODELS OF DIABETIC INDORE, M.P. (INDIA)
NEPHROPATHY IN RATS

50. STUDY OF THE ACHLA VYAS LAKSHMI NARAINCOLLEGE OF 141-143

ANTINOCICEPTIVE EFFECT PHARMACY (RCP), REVATI,
OF ANNONASQUAMOSA SANWER ROAD, INDORE, M.P.
LEAF EXTRACT IN MICE (INDIA)

51. ASSESSMENT OF YASHRAJ YADAV ORIENTAL COLLEGE OF 144-147

ANTI‐DIABETIC AND PHARMACY & RESEARCH,
ANALGESIC PROPERTIES OF ORIENTAL UNIVERSITY,INDORE,
HYDROALCOHOLIC EXTRACT M.P. (INDIA)
OF SARCOSTEMMA ACIDUM
IN RAT

52. ANALYTICAL METHOD TAHIR NIZAMI SMRITI COLLEGE OF 148-149

DEVELOPMENT AND PHARMACEUTICAL EDUCATION,
VALIDATION FOR INDORE, M.P. (INDIA)
SIMULTANEOUS
ESTIMATION OF
ERTUGLIFLOZIN AND
SITAGLIPTIN IN TABLET
FORMULATIONS BY RP-HPLC
METHOD

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S. PRESENTING
TITLE OF PAPER COLLEGE NAME PAGE NO.
NO. AUTHOR
53. REVERSE MOLECULAR KUSHAGRA SMRITI COLLEGE OF 150-152
DOCKING STUDIES AND IN DUBEY PHARMACEUTICAL EDUCATION,
VITRO EVALUATION OF INDORE, M.P. (INDIA)
BAICALIN FOR ANTIDIABITIC
ACTIVITY

54. DESIGNING AND KHUSHBU JAIN ORIENTAL UNIVERSITY, GATE 153-155

MOLECULAR MODELING NO.1, SANWER ROAD, JAKHYA,
STUDIES ON CHALCONE OPPOSITE REVATI RANGE,
DERIVATIVES AGAINST INDORE, M.P. (INDIA)
PLASMODIUM FALCIPARUM

55. ANTI-MICROBIAL ACTIVITY PRERNA DEPARTMENT OF 156-157

OF [4-(6-(2- CHATURVEDI PHARMACEUTICAL SCIENCES,
CHLOROPHENYL)- JAIPUR NATIONAL UNIVERSITY,
[1,2,4]TRIAZOLO[3,4- JAIPUR, (R.J.) - (INDIA)
B][1,3,4] THIADIAZOL-3-
YL)PHENOL] TRIAZOLO-
THIADIAZOLE DERIVATIVE

56. MOLECULAR MODELLING JASDEV S. SCHOOL OF PHARMACY, DEVI 158-159

STUDIES OF BENZOXAZOLES TUTEJA AHILYA VISHWAVIDYALAYA,
AS POTENTIAL ANTI- INDORE, M.P. – 452020
CONVULSANT AGENTS

57. MOLECULAR DOCKING AND PRITI PATIDAR SCHOOL OF PHARMACY, DEVI 160-162
ADMET STUDIES OF AHILYA VISHWAVIDYALAYA
PYRAZOLE ACRYLIC ACID INDORE, MADHYA PRADESH-
BASED OXAZOLE AND 452020
AMIDE DERIVATIVES AS
ANTIMALARIAL AND
ANTICANCER AGENTS

58. EMPLOYMENT OF AYUSHI SHRI G.S. INSTITUTE OF 163-167

HYDROTROPIC AND MIXED MOHADIKAR TECHNOLOGY AND SCIENCE, 23,
HYDROTROPIC SOLUTIONS PARK ROAD, INDORE, M.P. –
AS MOBILE PHASE TO 452020
CARRY OUT TLC
PRECLUDING THE USE OF
ORGANIC SOLVENTS

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FORMULATION AND EVALUATION OF MATRIX TYPE TRANSDERMAL PATCHES OF

LULICONAZOLE
Gaurav Jain* and Rakesh Patel
Faculty of Pharmacy, Dr. A.P. J. Abdul Kalam University, Indore (M.P.)

ABSTRACT
The skin is the most readily accessible organ of the body and acts as a barrier against the micro and
macromolecules of the environment because of its low permeability to such substances. The goal of drug
administration through skin is for topical treatment of skin diseases or for transdermal absorption of drugs in
the systemic circulation. In the present investigation matrix patches were casted on a glass mould by solvent
casting methods. Seven types of polymer patches were prepared and evaluated using the drug luiconazole
which is used to treat fungal infections.
Keywords: Transdermal patches, Luliconazole, Formulation

Introduction Span 80 was selected on the basis of compatibility

Patches have various disadvantages, most study. Prefοrmulatiοn studies are needed tο
commonly skin irritation, because of their ensure the develοpment οf a stable,
occlusive properties causing obstruction of sweat therapeutically effective and safe dοsage fοrm.
ducts, which in turn prevents loss of water vapor Through visual inspection, the physical appearance
from skin surface, difficulty in applying on the and melting point of pure drug was carried out as
curved surfaces, pain while peeling off and poor per Indian Pharmacopoeia. The UV spectrum of
1-2
aesthetic appeal. Therefore there is a need for drugs was recorded using UV-visible
development of a dosage form which permits less spectrοphοtοmeter (Mοdel-1700, Shimadzu,
frequent dosing by maintaining a close contact Japan). The FTIR studies will be done using using
with the skin for prolonged time period thereby FTIR spectrοphοtοmeter (Mοdel-8400 S,
improving the patient compliance. Luliconazole is Shimadzu, Japan). Standard cure for the drugs was
an antifungal drug and have imidazole. plotted as per standard procedure. Matrix patches
were casted on a glass mould by solvent casting
Material and Methods methods. All formulated batches were evaluated
3-4
Drug luliconazole was selected for present as per standard procedure.
investigation. The excipients viz., HPMC E5, Ethyl
cellulose, Propylene glycol and

Table 1: Formulation of matrix transdermal patches of Luliconazole

Ingredients TPL1 TPL2 TPL3 TPL4 TPL5 TPL6 TPL7
(1:2) (1:3) (1:4) (1:4) (1:(2:8) (1:(1:9) (1:(2:8)
Drug (EN) 70 70 70 70 70 70 70
HPMC E5 140 210 280 280 140 70 140
EC - - - 560 630 560
Span 80 (%) - - - 1 - - 1
Propylene glycol (%) 3 3 3 3 3 3 3
Note: All the reading is in mg

Results and Discussion uptakes were increases. The results indicated that
The prepared transdermal patches were evaluated the hydrοphilicity οf the pοlymers is directly
fοr their physiοchemical characteristics. The prοpοrtiοnal tο the percent οf mοisture cοntents
fοrmulated patches were fοund tο be clear, and mοisture uptake. The lοw percentage οf
smοοth, unifοrm, flexible in their physical mοisture cοntent in fοrmulatiοns cοuld help them
appearance and free frοm entrapment οf air tο remain stable and prevents them frοm being
bubble. The mοisture cοntent and mοisture completely dried. Alsο, lοw mοisture uptake
uptake οf variοus fοrmulatiοns shοwed that with prοtects the material frοm micrοbial
increasing in cοncentratiοn οf pοlymer bοth cοntaminatiοn and bulkiness οf the patch.
percentages οf mοisture cοntent and mοisture

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Table 2: Evaluatiοn οf transdermal patches of Luliconazole

FC Thicknes Weight Flatnes Folding Tensile pH % %Moistur % Drug
s Variatio s Endurance Strength Moistur e uptake content
(mm) n (mg) (kg/mm2) e
content
TPL 0.17 ±0.0 ± 2.38 100 242.1±0.9 10.22 ± 0. 5. 2.14 4.94 ±0.18 98.29
1 9 11 7 ±0.22 ±0.13
TPL 0.18 ± 1.79 100 250.4±0.0 11.87 ± 6. 2.16 4.92±0.22 98.32±0.1
2 ±0.02 1 0.02 2 ±0.07 8

TPL 0.18 ± 2.29 100 252.2±0. 11.92 ± 5. 2.06 5.14 ±0. 98.89±0.7
3 ±0.02 17 0.01 8 ±0.02 18 7

TPL 0.21 ± 2.92 100 251.9±0.1 12.29 ± 6. 2.88 3.16 ±0.11 98.91
4 ±0.07 8 0.02 2 ±0.07 ±0.16

TPL 0.16 ±1.16 100 255.8±0.2 12.96±0.0 6. 1.96 3.12 ±0. 98.96 ±0.
5 ±0.08 2 2 3 ±0.29 19 12

TPL 0.19 ± 2.62 100 250.9±0.8 11.98 ± 5. 1.99 3.83 ±0.17 98.32 ±0.
6 ±0.09 8 0.02 8 ±0.02 19

TPL 0.19 ± 2. 18 100 247.7±0.1 12.03 ± 0. 5. 2.27 3.10 ±0.20 97.98 ±0.
7 ±0.03 9 13 8 ±0.02 17

Table 3: In vitrο dissοlutiοn prοfile οf transdermal patches of luliconazole

Cummulative % οf drug release
TPL1 TPL 2 TPL 3 TPL 4 TPL 5 TPL 6 TPL 7
0 0 0 0 0 0 0 0
1 2.91 2.29 3.19 4.02 4.98 4.02 3.01
4 6.98 7.19 8.21 9.12 11.91 11.01 10.01
8 8.37 9.21 12.11 14.19 17.02 17.09 15.11
12 9.29 11.87 21.10 22.28 37.10 36.01 30.02
16 13.10 12.02 22.10 32.02 50.11 44.12 37.10
20 19.29 22.12 32.21 36.01 52.29 50.09 40.08
24 32.32 39.18 42.88 47.12 57.08 56.11 49.19
28 42.18 48.10 52.11 56.13 62.11 59.12 57.11
32 62.08 66.11 69.02 72.11 79.19 75.11 73.01
36 73.91 74.31 75.29 77.06 84.90 81.28 79.11

100
% cumulative
drug relese

0
1 2 3 4 5 6 7 8 9 10 11

Time (h)

Graph 3: Cumulative % drug release of transdermal patches containing luliconazole

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Conclusion transdermal patches of luliconazole may prove to

The results of luliconazole transdermal matrix be a better alternative to conventional dosage
patch showed that the most promising forms in fungal infection as revealed by the
formulation was TPL5 (formulation containing results.
Drug: HPMC:EC:Span:PG; (1:(2:8)). Thus optimized
transdermal matrix patch of luliconazole using References
polymers such as HPMC and EC with Span & PG as 1. Michaels A.S., Chandrasekaran S.K. and Shaw
permeation enhancers demonstrated their ability J.E. Drug permeation through human skin:
to give sustained release, because of excellent theory and in vitro experimental measurement
release and permeation of drug and its influence AIChE J, 1975: 21(5); 985-996
on efficacy on skin infection. The developed 2. Prausnitz M.R. and Langer R. Transdermal drug
formulation of luliconazole is expected to improve delivery Nat Biotechnol, 2008; 26 (11);
the patient compliance, form better dosage pp. 1261-1268.
regimen and provide maintenance therapy to 3. Ganju E. and Ganju K. Formulation & evaluation
patients. These promising results showed the of transdermal patch of acetohexamide.
feasibility of delivering luliconazole through European Journal of Pharmaceutical and
transdermal matrix patch. The developed Medical research, 2017; 3(7):233-235.

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FORMULATION DESIGN AND EVALUATION OF WATER DISPERSIBLE TABLET OF

GUAIFENESIN FOR PAEDIATRIC USE
KuldeepVinchurkar*, Sheetal Mane, Jitendra Sainy, Masheer Ahmed Khan
School of Pharmacy, Devi Ahilya Vishwavidyalaya, Indore
Indore Institute of Pharmacy, Indore
[email protected]

ABSTRACT
Generally more often or so young children suffer from spells of cold and cough. Cough isone of the most
common symptoms of childhood illness. The coughing has been classified into various types however, barking,
whooping types of cough are quite severe. Most widely used dosage form for children include cough syrups or
suspension. However, dispersible tablets offer advantage of both liquid and solid dosage forms. Dispersible
tablets are unique class of tablets that disintegrate rapidly in water to form a stabilized suspension or when
placed on toung, disperse instantaneously in the mouth. This property makes them more convenient for oral
administration than conventional tablets. Guaifenesin is expectorants for treatment of cough. It has a bitter
taste which deters its use in the pediatric patients.Because of this, the compliance of these patients with its
dose regimen poses a great challenge. This results in insufficient therapeutic benefits of the expectorant
therapy. Hence, present studies are undertaken to mask the bitter taste of Guaifenesin by complexation
technique and to design dispersible tablet formulation, a suitable dosage form for pediatric patients. Weak
cation exchange resin Kyron - T114 and Indion 214 were used in formulation of complexes with drug. PEG 4000
and PEG 6000 were used for solid dispersion technique by solvent evaporation technique to mask the bitter
taste of drug. The complexes were evaluated for bulk density, angle of repose, taste masking and in vitro drug
release. In vitro drug release studies showed more than 95% drug release from the optimized formulation
within 30 min. Kyron T114 (1:1) was found to be better complexing agent for masking the bitter taste of
guaifenesin.
Keywords: Cough, whooping cough, Guaifenesin

Introduction Cross carmellose sodium was procured from Vama

Cough is one of the most common symptoms of pharma, Nagpur. All the chemicals and reagents
childhood illness. Most widely used dosage form were of analytical grade.
for children include cough syrups or suspension.
However, dispersible tablets offer advantage of Experimental Work
both liquid and solid dosage forms.They are Characterizationof drug and excipients by
unique class of tablets that disintegrate rapidly in physiochemical properties and spectrometric
water to form a stabilized suspension or when analysis, after that, tastemask of drug using solid
placed on tongue, disperse instantaneously in the dispersion by solvent evaporationtechnique with
mouth which makes them more convenient for PEG 4000 and PEG 6000 in ratio of 1:1, 1:3 and 1:5
oral administration than conventional tablets. and complexation with ion exchange resinwith
Guaifenesin is an expectorantfor treatment of Kyron T-114 and Indion -214 in the ratio of 1:1,
cough having bitter taste which deters its use in 1:2, and 1:3. Then, evaluation of taste modified
the pediatric patients. Because of this, the drug samples by organoleptic and functional
compliance of these patients with its dose regimen properties. Finally, formulation and evaluation of
poses a great challenge. This results in insufficient water dispersible tablet formulation of taste
therapeutic benefits of the expectorant therapy. masked Guaifenesin and Stability testing of water
Hence, present studies aims to mask the bitter dispersible tablet was done.
taste of Guaifenesin by complexation technique
and to design dispersible tablet formulation, a Results and discussion
suitable dosage form for pediatric patients. The study of drug resin complex with Indion 214
and Kyron T114 showed that guaifenesin resinate
Materials and Methods with Kyron T114 (1:1) gave best drug loading as
Guaifenesin was generously gifted by Vama 92.80% and the drug content of resinate was 96.91
pharma, Kyron T114 was procured from Corel and Indion 214 gave drug loading 86.80% and drug
pharma, Ahmedabad, Aspartame, Indion 214, content 88.60%. Hence, drug resiante complex

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with Kyron T114 was selected for further studies. croscarmallose sodium as superdisintegrants 4%
The taste modified forms of Guaifenesin viz. w/w (G6)ensured the release within 30
physical mixtures with sweeteners, resinates and respectively. The stability data of these dispersible
solid dispersions possessed following flow tablets indicate no adverse effect of temperature
characteristics viz. Angle of repose (22-29) and humidity on the characteristics viz.
excellent. Compressibility index (13-16). The appearance, disintegration time (in-vitro),
spectroscopic analysis (IR) of all the modified hardness, friability, assay, uniformity of dispersion
forms of Guaifenesin indicated absence of any and drug release (in-vitro). The stability data of
probable interaction of Guaifenesin with these dispersible tablets indicate no adverse effect
excipients or vice versaas demonstrated by the of temperature and humidity on the
presence of intact peaks for major functional characteristics viz. appearance, disintegration time
groups in the drug as well as excipients. The (in-vitro), hardness, friability, assay, uniformity of
results indicate that, drug resinate complex with dispersion and drug release (in-vitro).
kyronT 114 (1:1, bitterness score rating 0) and

Table 1:Formulation of dispersible tablet of guaifenesin

Name of the ingredients (mg) G1 G2 G3 G4 G5 G6
Drug kyronT 114 resinate 200 200 200 200 200 200
Microcrystalline cellulose 140 134 128 140 134 128
Sodium starch glycolate 14 20 26
Cross carmallose sodium 14 20 26
Talc 6 6 6 6 6 6
Magnesiumstearate 6 6 6 6 6 6
Sucrose 16 16 16 16 16 16
Aspartame 8 8 8 8 8 8
Flavor 10 10 10 10 10 10

Table 2: Taste score on the scale of bitterness by solid dispersion and complexation technique
Guaifenesin: Guaifenesin: Guaifenesin: Indion Guaifensin: Kyron
PEG 4000 PEG 6000 214 T114
Ratio 1:1 1:2 1:3 1:1 1:2 1:3 1:1 1:2 1:3 1:1 1:2 1:3
Batch
GP1 GP2 GP3 GP4 GP5 GP6 GI1 GI2 GI3 GK4 GK5 GK6
code
Score on
scale of 1 1 1 1 1 1 0 0 0 0 0 0
bitterness

Table 3: Post compression parameters of guaifenesin water dispersible tablet

Batch Wetting Water absorption In-vitro dispersion time In-vitro disintegration time
code time (Sec) ratio (Sec) (Sec)
G1 21.19 ± 1.6 79.09± 0.11 27.99 ± 0.04 24.44 ± 1.3
G2 26.18 ± 1.9 96.59± 0.05 29.01 ± 0.13 31.32 ± 1.4
G3 21.58 ± 1.2 87.19± 0.03 26.98 ± 0.11 28.31 ± 1.1
G4 24.51 ± 0.6 88.34± 0.06 31.00 ± 0.15 26.39 ± 1.5
G5 21.55 ± 1.1 91.51± 0.06 21.97 ± 0.16 22.18 ± 1.4
G6 20.45± 1.2 99.25± 0.13 20.01 ± 0.04 20.36 ± 1.8
Average of four determination (SD), n=4.

References science and nanotechnology 2010;

1. Vijay kumar B: Development and 3:1122- 1127.
evaluation of Guaifenesin bilayer tablet. 2. Wagh MP, YewaleCP, ZateSU:
International Journal ofpharmaceutical Formulation and evaluation of fast
dispersible tablets of Aceclofenac using

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ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

different superdisintegrant. International 4. Lakshmi CS,Nitesh JP. Formulation and

Journal of pharmacy and pharmaceutical evaluation of oral dispersible tablets of
science. 2010; 2:154 - 156. Cinnarizine using sublimation technique.
3. Shimul H, Islam A: Development and International Journal of Pharmaceutical
evaluation of water dispersible tablet of Science and Research 2011; 2:178 - 182.
acyclovir. International journal of 5. Subrahmanyam CVS:Text book of physical
advanced research in biological sciences. pharmaceutics. Vallabh Prakashan,
2014;2:439 - 451. second edition, 2004: 210-228.

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FORMULATION DESIGN AND EVALUATION OF FAST DISSOLVING TASTE MASKED TABLET

OF LAFUTIDINE
Sheetal Mane*, KuldeepVinchurkar, Jitendra Sainy, Masheer Ahmed Khan
School of Pharmacy, Devi Ahilya Vishwavidyalaya, Indore
[email protected]

ABSTRACT
Lafutidine is a cytoprotective H2 receptor blocker with greater potency and practically insoluble in water with
bitter taste. In the present study, an attempt has been made to improve the solubility of drug by solid
dispersion technique and masked the bitter taste by complexation technique. PEG 4000, PEG 6000 and PEG
8000 were used as a carrier with drug in solid dispersion technique to enhance the solubility of drug. Beta
cyclodextrin and Hydroxypropyl betacyclodextrin were used as a complexing agent in formulation of
complexes with the drug by physical and kneading method. The drug complexes were evaluated for bulk
density, angle of repose, taste masking and in vitro drug release. In vitro drug release studies showed more
than 90% drug release from the optimized formulation within 30 min. Hydroxypropyl betacyclodextrin was
found to be better complexing agent by kneading method for masking the bitter taste of drug while PEG 6000
out of PEG 8000 and PEG 4000 give better dissolution profile.

Introduction Drug was gifted byPure Chem PVT LTD. Gujarat.

A fast dissolving tablet system can be defined as a Cross carmellose sodium was obtained from Vama
dosage form for oral administration, which when pharma, Nagpur. Camphor and ammonium
placed in mouth, rapidly dispersed or dissolved bicarbonate was procured from Shanti chemicals,
and can be swallowed in form of liquid.The Chennai. All the chemicals and reagents were of
benefits, in terms of patient compliance, rapid analytical grade.
onset of action, increased bioavailability and good
stability make these tablets popular as a dosage Method
form of choice in the current market. Lafutidine is Characterization of the drug Lafutidine and
a superior and novel second generation H 2 formulation additives, followed by spectrometric
receptor antagonist, proton pump inhibitor with and thermal characterization. Solubility
gastro protective activity.It is 8-20 times more enhancement and taste masking of drug achieved
potent. The main objective of this study is to by physical mixing and kneading method with beta
improve palatability by increasing solubility and cyclodextrin (βCD) and Hydroxypropyl beta
masking the bitter taste of drug. cyclodextrin (HPβCD). Afterthat, formulation of
taste modified tablet of Lafutidine by sublimation
Materials method and Evaluation of optimised formulation
and stability studies was conducted.

Table 1: Formulation of fast melting / dissolving tablet of Lafutidine prepared by sublimation method.

Ingredients (mg) FS1 FS2 FS3 FS4 FS5 FS6 FS7

Lafutidine (Complex) 42 42 42 42 42 42 42
Camphor 2.0 3.0 4.0 - - - -
Ammonium bicarbonate - - - 2.0 3.0 4.0 -
Cross carmellose sodium 5% 5% 5% 5% 5% 5% 5%

Mannitol 49.5 48.5 47.5 49.5 48.5 47.5 51.5

Aspartame 1% 1% 1% 1% 1% 1% 1%

Magnesium stearate 0.5% 0.5% 0.5% 0.5% 0.5% 0.5% 0.5%

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Table 2: The comparative dissolution data of Lafutidine from inclusion complexes with cyclodextrin
prepared by physical mixture and kneading method.

Sr. Method of Saturation solubility Time

Complexes
No. preparation (μg/ml) t (Min) t (Min)
50 90

1. Lafutidine (Plain) - 25.28 - -

2. Lafutidine : βCD Physical mixture 84.07 12.98 44.93
3. Lafutidine : βCD Kneading method 91 8.57 27.10
4. Lafutidine : HPβCD Physical mixture 150.57 13.58 36.32
5. Lafutidine : HPβCD Kneading method 157.14 2.95 8.95

Table 3: Gradation of bitter taste of Lafutidine inclusion complexes with cyclodextrins (physical mixture (PM)
and kneading method (KM)).
Mean scoreofLafutidine Complexes(β-cyclodextrin) Complexes(Hp-β-cyclodextrin)

PM KN PM KN
1:1 1:1 1:1 1:1
1 1 0 1 0
0- No bitter taste, 1- Slightly bitter taste, 2- Moderately bitter taste, 3- Strong bitter taste,
The inclusion complexes with hydroxypropylbetacyclodextrin prepared by kneading method demonstrated
highest solubility (157.14 μg/ ml) and fastest in vitro dissolution profile of Lafutidine (100% drug release in 10
min.) and effective masking of slightly bitter taste. Hence, was selected for formulation of fast melting/
dissolving tablets of Lafutidine.
Table 4: Characteristic of fast dissolving tablets of Lafutidine.
Batch Diameter Thickness Wt. Content D.T. Wetting Water
code (mm) (mm) Variation Uniformity (sec.) time (sec) absorption
(mg) (%) ratio
FS1 8.048 2.04 100.21 98.26 14 11 89.78

FS2 8.019 2.12 100.45 98.34 12 10 90.54

FS3 8.038 2.37 99.98 99.95 13 9 93.87

FS4 8.028 2.09 101.02 99.97 12 10 95.68

FS5 8.076 1.98 100.09 97.38 09 11 92.49

FS6 8.055 2.25 100.45 97.42 07 9 90.9

FS7 8.034 1.99 98.99 97.75 15 12 97.04

All the formulations indicated disintegration time in between 7 to 14 sec. The control formulation (FS7)
indicated disintegration time of 15 sec.
fast dissolving tablet of Lafutidine containing
Conclusion ammonium bicarbonate(4%) and cross carmellose
The results obtained suggest that, Hp- β- sodium (5%) i.e. Optimized formulation (FS7) gave
cyclodextrinand β-cyclodextrincomplex with drug the best disintegration time and also complete
mask the bitter taste of lafutifdine but drug drug release within 10 min.It was concluded that
complex with Hp- β-cyclodextrinby kneading Hp- β-cyclodextrincan successfully mask the bitter
method proceed for further process. Taste masked taste of drug by kneading method and addition

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International Journal of
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technique of superdisintegrant is useful technique Camphor as Sublimating Agent.

for preparing fast dissolving tablet by sublimation American-Eurasian Journal of Scientific
method. Rapid absorption, improved Research. 2010; 5: 264-269.
bioavailability, effective therapy and better patient 3. Shaikh S, Khirsagar RV, Quazi A: Fast
compliance may be predicted from such Lafutidine disintegrating tablets: An overview of
fast dissolving tablet formulation. formulation and technology. IntJ
Pharmacy Pharm Sci. 2010; 2:9-14.
References: 4. Narmada GY, Mohini K, Prakash Rao B,
1. Apparao. B, Shivalingam MR, Reddy YVK, Gowrinath DP, Kumar KS: Formulation
Rao S, Rajesh. K, N. Sunitha: Formulation evaluation and optimization of fast
and evaluation of Aceclofenac solid dissolving tablets containing Amlodipine
dispersions for dissolution rate besylateby sublimation method.
enhancement. International Journal of ARSPharmceutica. 2009;50:129-144.
Pharmaceutical Sciences and Drug 5. Subrahmanyam CVS: Text book of
Research. 2010; 2: 146-150. physical pharmaceutics. Vallabh
2. Bhardwaj V, Bansal M, Sharma PK: Prakashan, second edition, 2004: 210-
Formulation and Evaluation of Fast 228.
Dissolving Tablets of Amlodipine besylate
using different Superdisintegrants and

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SYNTHESIS AND CHARACTERIZATION OF SILVER NANO PARTICLES USING PLANT

POMEGRANATE
(PUNICA GRANATUM)
Yadav Ekta*1, Dr. Dubey P.K.2
1Department of Pharmaceutics, Swami Vivekanand College Of Pharmacy, Indore (M.P) India
2Department of Pharmaceutics, Swami Vivekanand College Of Pharmacy, Indore (M.P) India
[email protected]
[email protected]

ABSTRACT
ABSTRACT: Nanoparticles (NP) have been shown to have various useful applications. They are generally
synthesized using chemical processes involving hazardous chemicals. Therefore, green synthesis of NPs using
natural products can be an environmentally friendly alternative. The green synthesis of silver nanoparticles
from the extract of different plant parts has gained a wide range of engrossment among the researchers due
to its unique optical and structural property. The aim of this study is green synthesis of silver nanoparticles
from the ethanolic leaf extract of pomegranate (Punica granatum). The formation of synthesized AgNPs were
studied using different analytical methods, including ultraviolet-visible(UV-VIS) spectroscopy, X-ray diffraction
(XRD) analysis.
Keywords: silver nanoparticles, Ethanolic leaf extract pomegranate, Green Synthesis and Charcterization

Introduction: Nanotechnology is emerging as a Pharmacy, Indore. The leaves were drie in a hot air
o
rapidly growing field with its application in Science oven at 25 C and Powdered.
and Technology for the purpose of manufacturing
1
new materials at the nanoscale level .The word 2.2 Preparation of Plant Exract:
“nano” is used to indicate one billionth a meter or The Punica grantum extract was prepared using
9.
10- The term Nanotechnology was coined by Soxhlet extractor using Ethanol as a solvent. About
Professor Noria Taniguchi of Tokyo Science 100 gm of powder material was uniformly packed
University in the year 1974 to describe precision in to a thimble and run in Soxhlet extractor.
manufacturing of materials at the nanometer
level. “Nano” is a Greek word synonymous to 2.3 Biosyntesis of Nano- Silver Particles:
-3
dwarf meaning extremely small. Nanoparticles are 100-ml aqueous solution of 1.0 x 10 m silver
beginning viewed as fundamental building blocks Nitrate was mixed with plant extract solution of
2
of nanotechnology . Green synthesis of different concentrationIn Silver Nitrate Solutions
nanoparticle is an important methodology that has in Silvber Nitrate Solution plant extract was added
been used in the synthesis of metallic followed by intermittent strring at room
nanoparticles, being an eco-friendly method (less temperature. By mixing both solutions, Ag ions
toxic to human and environment), using different were reduced and clustered together to form
parts of any selected plants (having medicinal monodispersed nanoparticles as a transparent sol
3
effect) .The pomegranate plant (Punica granatum) in aqueous medium. The Ag solution was yellow
is considered an important traditional source to because of the absorption at 390 nm.The solution
treat perilous ailments dueto its high content of was stirred repeatedly whenever some dark color
various important appeared for approximately an hour until it
4
phytochemicals .Theseimportantphytochemicals became stabilized. At this point this solution of Ag
make pomegranate as a rich source of antioxidant. nanoparticles was so stable that it did not change
The phytochemical analysis of pomegranate leaves color for as long as several months without any
has interpreted the presence of flavones, stabilizing agent.
luteoloin, glycosides, alkaloids, organic acids and
5
tannins. 3. Characterization and Results Discussion
3.1 UV –Visible Spectral Analysis of Nanosilver
2.1 Materials Particles:
Pomegranate leaves were collected from Nanosilver particles were confirmed by taking UV-
Medicinal Plant of Swami Vivekanand College of vis spectrum. The bioreduction of Ag+ in aqueous

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solution was monitored by periodic sampling of For Punica grantum extract:

aliquots (0.2ml) of the susoension. There was a Different concentration PG1, PG2, PG3 & PG4 i.e.
gradual increase in color development in the 40, 60, 80 and 100microgram/ml respectively) of
reaction mixture (silver nitrate solution + plant leaf ethanolic extract of Punica grantum, was added to
-3
extract). 1x 10 M silver nitrate solution. There was a
gradual increase in color development in the
partical size, dielectic medium and chemical
surroundings.Sample

Table.1 UVspectrophotometric Data of nanosilver from Punica grantum Extract:

S.NO. Concentration (μg/ml) 0 hrs 0.15 hrs 0.30 hrs 1hrs

PG1 40 284 284 286 286

PG2 60 286 292 292 292
PG3 80 300 300 300 296
PG4 100 324 322 324 322

3.2 X-Ray Diffraction Studies: A thin film of the Ag

nanoparticles was made by placing solution and References
carried out the X-ray studies. The difraction 1. Albrecht MA, Evan, CW, Raston CL, 2006.
pattern was recorded by Co-Kal radiation. The Green chemistry and the health
scanning was done in the region of 20 0 to 80 0 implications of nanoparticles. Green
and the time constant was 2 s. The crystalline Chem 2008; 8: 417-432.
nature of Ag nanoparticles was confirmed from 2. Taniguchi N, On the Basic Concept of
the X-ray diffraction analysis [35, 36, 136, and 137] Nano-Technology. Proc. Intl. Conf.Prod.
X-ray diffraction of pure silver nitrate. Eng. Tokyo, Part II. Japan society of
Precision Engineering, 1974.
For Punica grantum: XRD studies of nanosilver 3. Zarfeshany A, Asgary S and Javanmard S H
particles from sample PG3 ie. 80ug/ml shows the 2014 Potent health effects of
XRD pattern with the diffraction peaks around 32, pomogranate Adv. Biomed. Res. 3 100
35, 45 and 54 corresponding to the (101), 4. Chauhan S, Upadhyay M K, Rishi N and
(111).(111), (200) and (200) facets. In Sample PG4 Rishi S 2011 Phytofabrication of silver
i.e. 100ug/ml, there were diffraction peaks around nanoparticles using pomegranate fruit
32, 45 and 54 corresponding to the (101), (111) seeds Int. J. Nanomater. Biostruct. 1 17
and (200) facets 5. Nisha H M, Tamileswari R, Jesurani S,
Kanagesan S, Hashim M, Catherine S and
Conclusion Alexander P 2015 Green synthesis of
Silver nanoparticles are successfully synthesized silver nanoparticles from pomogranate
from a silver nitrate solution through a simple (Punica)
green medicated leaf plant of Punica grantum
which act as a reducing as well as capping agent.
The size of the silver nanoparticles was estimated
at 320 nm. The bioreduced silver nanoparticles
were characterized using UV-Vis, XRD. From a
technological point of view, these obtained silver
nanoparticles have potential applications in the
biomedical field and this simple procedure has
several advantages such as cost-effectiveness,
compatibility for medical and pharmaceutical
applications as well as large scale commercial
production. By using green chemistry, the silver
nanoparticles have prepared using Punica grantum
leaf extract which is a non toxic. We can be used
effectively these particles more than one month

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EVALUATION OF TRANSDERMAL PATCHES OF LORNOXICAM

Bhawana Kapoor*1, Hemant Rangarh2, Dr Sonu Sharma3
1. Shri Dev Bhoomi Institute of Sciences And Technology, Paundha, Dehradun (UK)
2. Executive QA, Windlas Healthcare Pvt. Ltd, Mohebewala, Dehradun (UK)
3. School Of Pharmaceutical Sciences, Jaipur National University, Jagatpura, Jaipur
(Rajasthan)

ABSTRACT
The purpose of this research was to develop a matrix-type transdermal therapeutic system containing drug
Lornoxicam with different ratios of hydrophilic (hydroxyl propyl methyl cellulose) and hydrophobic (cellulose
acetate) polymeric systems by the solvent evaporation technique by using 30 % w/w of propylene glycol to the
polymer weight, incorporated as plasticizer. The anti-inflammatory and analgesic effects of the selected
patches were determined using paw edema method and writhing test respectively and the results were found
to be statistically significant at P <0.01. The results of the study show that Lornoxicam could be administered
transdermally over a period of 24 h. through the matrix type TDDS for effective control of pain and
inflammation.
Keywords: Transdermal patches, Lornoxicam, In-vitro release, HPMC, Cellulose acetat

INTRODUCTION inflammation induction. The animals of group II

Lornoxicam, also known as chlortenoxicam, is a served as the test group and treated with
2
member of the oxicam group of non steroidal anti- transdermal patches of lornoxicam (2.0×2.0 cm ).
inflammatory drugs (NSAIDs) with extremely Patches were applied and fixed to the abdominal
potent anti-inflammatory and analgesic activities. area of rat of group II, 6 hrs prior to the
It is widely used for the symptomatic treatment of carrageenan injection.
pain and inflammation in patients with Degree of paw swelling in both the groups was
rheumatoid arthritis, osteoarthritis and in calculated as:
management of pre/post operative pain 𝑉𝑡 − 𝑉
% 𝑆𝑤𝑒𝑙𝑙𝑖𝑛𝑔 = × 100
associated with different surgeries. Currently it is 𝑉
available in oral and parenteral formulations in the Where, Vt is the mean volume of carrageenan
market. However lornoxicam has a relatively injected paw and V is the mean volume of saline
superior gastrointestinal (GI) tolerability when injected paw
compared with other NSAIDs, its repetitive daily The edema formation was calculated using
administration may cause various gastrointestinal following formula:
side effects range from mild dyspepsia, heartburn 𝑆𝑡
% 𝐸𝑑𝑒𝑚𝑎 𝑖𝑛ℎ𝑖𝑏𝑖𝑡𝑖𝑜𝑛 = 1 − × 100
to ulceration and hemorrhage while renal side 𝑆𝑐
effects can range from acute and chronic renal Where, St is the percent swelling of drug treated
failure to edema and electrolyte imbalance. Added group and Sc is the percent swelling of control
to that, lornoxicam shows a distinct pH-dependent group
solubility characterized by poor solubility in low pH Analgesic activity: To assess the analgesic activity
conditions present in the stomach which of lornoxicam transdermal patch, a writhing test
1-
consequently leads to delay in its analgesic effect was performed. The mice were divided into two
2
. groups (each group having 6 mice). On the
previous day of the experiment, the hair of the
MATERIALS AND METHODS abdominal area of the mice was removed
Anti-inflammatory activity physically with the help of hair removal cream and
The anti-inflammatory effect of selected the skin was cleared with rectified spirit. The
transdermal formulation was measured by animals of the group I served as the control, and
3,4
carrageenan – induced paw edema in male rat received no treatment prior to the induction of
.The anti-inflammatory activity in rat was writhing response. The animals of group II served
measured using plethysmometer. The rats were as the test group and treated with transdermal
2
divided into two groups (each group having 6 rats). patches of lornoxicam (2.0×2.0 cm ). Patches were
The animals of the group I served as the control, applied and fixed to the abdominal area of mice of
and received no treatment prior to the group II, 12 hrs prior to the acetic acid injection.

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The mean writhing number was obtained for each Anti-inflammatory activity: Anti-inflammatory
group and percent analgesic activity was study was carried out in rats by carrageenan-
calculated by the following formula: induced paw edema method. As shown in table 1,
there was a significant difference in percentage of
𝑁𝑡 swelling at 1, 2 and 3hrs. The inhibition in edema
% 𝐴𝑛𝑎𝑙𝑔𝑒𝑠𝑖𝑐 𝑎𝑐𝑡𝑖𝑣𝑖𝑡𝑦 = 1 − × 100
𝑁𝑐 was found to be statistically significant at P < 0.01
with 50.39% inhibition within 3hrs of carrageenan
Where, Nt is mean number of writhes of test group injection which revealed that the tested
and Nc is mean number of writhes of the control formulation (A1S) showed significantly improved
group anti-inflammatory activity as compared to control
formulation.
RESULTS AND DISCUSSION
Table 1: Anti-inflammatory activity of selected transdermal patch (A1S) by carrageenan induced paw edema
in rats (n=6)
Increase in paw
Time (hrs.) Group a % Swelling % Inhibition
volume (mL)
Control 1.2±0.026 25.53
1 ** 33.33
Test 0.82±0.017 17.02
Control 2.42±0.031 50.00
2 ** 40.44
Test 1.37±0.021 29.78
Control
3.53±0.042 72.91
3 ** 50.39
Test 1.67±0.021 36.17
n: number of animals per group a: values are the mean ± S.E.M. of 6 observations
** P <0.01, ANOVA followed by Dunnet’s t-test

Analgesic activity: Analgesic activity was writhing response was found to be statistically
measured in mice by acetic acid induced writhing significant at P < 0.01 with 76.18 % inhibition
method. As shown in table 2, there was a which revealed that the tested formulation (A1S)
significant difference in number of writhes showed significantly improved analgesic activity as
between control and test group. The inhibition in compared to control formulation.

Table 2: Analgesic activity of selected transdermal patch (A1S) by Acetic acid induced writhing in mice (n=6)
a
Group No. of writhes % Inhibition in writhing response

Control 77.66±3.073
** 76.18
Test 18.5±1.875
n: number of animals per group a: values are the mean ± S.E.M. of 6 observation
** P <0.01, ANOVA followed by Dunnet’s t-test

CONCLUSION obtained, further studies can be carried out using

In conclusion, monolithic transdermal patches of the formulation A1S to correlate in vitro and in
lornoxicam can be formulated by solvent casting vivo permeation for the development of suitable
technique, using hydrophilic polymers, transdermal system of lornoxicam.
hydroxypropyl methylcellulose (K4M, K15M, and
K100M) and hydrophobic polymer (cellulose REFERENCES
acetate). Skin irritation test and biological 1. Hamza YS, Aburahama MS. Design and in
activities of the best formulation A1S, it was vitro evaluation of novel sustained-
revealed that the prepared transdermal patches release matrix tablets for lornoxicam
are capable for the treatment of pain and based on the combination of hydrophilic
inflammation with more effectiveness and better matrix formers and basic pH-modifiers.
patient compliance. In view of the results Pharm Devlop Tech. 2010; 15(2): 139-153.

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International Journal of
Pharmaceutical Sciences and Research
ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

2. Hamza YS, Aburahama. Novel sustained- hydrochloride. Int J Res Pharm Sci. 2010;
release fast-disintegrating multi-unit 1(3): 259-266.
compressed tablets of lornoxicam 4. Bharkatiya M, Nema RK, Bhatnagar M.
containing Eudragit RS coated chitosan- Development and characterization of
alginate beads. Pharm Devlop Tech. 2010; transdermal patches of metoprolol
15(3):1-15. tartrate. Asian J Pharm Clinical Res. 2010;
3. Prabhakara P, Koland M, Ahmed MG, 3(2):130-134.
Narayana CR, Satyanarayana D.
Preparation and evaluation of
transdermal patches of papaverine

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DEVELOPMENT AND CHARACTERIZATION OF HERBAL FACIAL TONIC

ADITYA SHARMA*, VISHAKHA CHAUHAN, RAJIV SAXENA, NEELESH MALVIYA
Department of Pharmacy, Smriti College of Pharmaceutical Education,
4/1 Pipliya Kumar, MR-11, Dewas Naka, Indore-452010 (M.P), INDIA
[email protected]

ABSTRACT
The purpose of this study was to produce a herbal facial tonic product containing coffee as an active
ingredient. The herbal facial tonic easily pampers your dull and tired skin on the go. The effective ingredients
like coffee and honey provide total nourishment to your skin thus enhancing the skin texture. This face
treatment formula also facilitates long-lasting hydration to your dry skin and adds a healthy appeal to it.
Coffee fights free radicals and tightens skin pores. it also reduces cellulite. Soothes skin benefit obtained by
rose water. Glycerine helps to retain the moisture to the skin.Soxhlet extraction process used for obtaining the
key ingredients. Sesame oil has the ability to fight the damage caused by free radicals that harm the cellular
structure of the skin. Almond oil restores the firmness.The facial tonic was formulated and evaluated for all
the required parameters. Thus, it can be concluded that herbal facial tonic helps in diminishing the appearance
of wrinkles, fine linesand gain the elasticity of skin.
Keywords: Herbal face tonic, Coffee, sesame oil, almond oil

Introduction
The herbal facial tonic easily pampers your dull Soothes skin benefit obtained by rose water.
and tired skin on the go. The effective ingredients Glycerin helps to retain the moisture to the skin.
like coffee and honey provide total nourishment to The herbal facial tonic results in diminishing the
your skin thus enhancing the skin texture. Skin appearance of wrinkles, fine lines, and gain the
tonics moisturize the layers of the skin to a few elasticity of skin. Cucumis sativa has an excellent
extents and also refresh the skin feel. Tonics leaves potential for cooling, healing and soothing to an
your skin revitalize when you are on the irritated skin. Cucumis sativa extract is often used
go.This face treatment formula also facilitates for skin problems, wrinkles, sunburn and as an
long-lasting hydration to your dry skin and adds a antioxidant. Honey improves skin texture and also
healthy appeal to it. Coffee Fights Free Radicals have antioxidant properties.
and Tightens Skin pores. it also reduces Cellulite.

Table No.1 Formula of herbal face tonic

Ingredients Quantity (%)
Coffee extract 30
Cucumis sativus extract 20
Honey 10
Almond oil 5
Sesame oil 5
Glycerine 10
Methyl paraben, propyl paraben 5
Rose water q.s. to 100

Methods Skin tonics are prepared by mixing the oil part and
Firstly, coffee bean was grounded to fine powder. the aqueous part separately. Then coffee extract
The powder was mixed with 80% propylene glycol was added to the above mixture. After proper
and placed in a shaker for 24 hours at 180rpm. mixing all the phases together gaining a single
Cucumis sativus extracted by Soxhlet extraction phase out of the two. Lastly rose water used to
technique using ethanol as solvent. obtained the final consistency.
The prepared herbal skin tonic was evaluated for following parameters whose values are tabulated in table

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Fig.1 Herbal Formulation of Face Tonic Evaluation

Table No.2 Evaluation of herbal face tonic

S. No. Parameters Inference
1. Color and Appearance Coffee brown and liquid consistency
2. Homogeneity Smoothly blended homogenized liquid formulation
3. pH 6.0
4. Immediate skin feel Moisturizing, Nogreasiness
5. Sensitivity test No irritation
6. After feel (4 hours) Light on skin

Result and discussion

The physical appearance was visually evident tighten the pores.It diminishes fine lines and
showing coffee brown color with light liquid wrinkles. Also provide lost lasting hydration to
consistency. The ingredients in the tonic was facial skin.
suitably homogenized at good speed. pH of the
toner adjusted to 6.0. Immediate skin test References
revealed that it has no greasiness and evenly  Rajvanshi A., Sharma S.,Khokhra S.L., “
absorbs to the layers of the skin. After feel was Formulation and evaluation of
checked after four hours of application of the tonic cyperusrotendus and cucumis sativus
to the skin which showed no grittiness and supple based herbal face cream”,
texture of skin. Pharmacologyonline 2: 1238-1244 (2011)
 Choudhuri, RK. Emblica cascading
CONCLUSION antioxidants: Novel natural skin care
The extracts of the ingredients were obtained ingredients. Skin Pharmacol. Applied Skin
successfully by solvent extraction and Soxhlet Physiol 2002; 15: 374-380.
method. Herbal tonic was formulated by  Rasheed A, Reddy GAK, Mohanalakshmi S,
mechanical homogenization method. The Kumar CKA. Formulation and comparative
prepared tonic was then evaluated for several evaluation of poly herbal anti-acne face
parameters to evidence the controlled wash gels. Pharmaceutical Biology 2011;
formulation. From the above experiment it can be 49(8): 771–774.
concluded that the tonic formulated using herbal
constituents turned out to be a good solution for
facial ailments. It fights the free radicals and

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FORMULATION AND EVALUATION OF HERBAL HAIR SERUM

Janhvi Yadav*, Harshal Deshmukh, Vishakha Chauhan, Neelesh Malviya
Smriti College of Pharmaceutical Education, Indore
*Corresponding author – Janhvi Yadav
[email protected]

ABSTRACT
Herbal formulations have uncontrollable demand in the world wide market because of their minimal side
effects and enhanced activity. They are precious and valuable gift of nature. Herbs are used as fundamental
part of health care system. Along with medicines herbs are also used in the preparation of several cosmetics
like cream, shampoo and oils etc. The present study is intended to formulate herbal hair serum for general
purpose using numerous herbs. These herbs are used to treat a lot of good hair obstacles like hair loss,
dandruff, thinning and flakiness of hair and dry scalp. In the present work, the herbal serum is prepared by
homogenizing. The key ingredients involved in this study are Fenugreek seeds and curry leaves. Aloe gel is
extracted from its leaves (Aloe barbadensis), Tulsi leaves (Ocimum sanctum), Neem leaves (Azadiracta indica),
Fenugreek seeds (Trigonella foenum-graecum), curry leaves, castor oil and sugar which are blended in coconut
oil by homogenizing method. The formulated hair serum is compared with marketed serum and found to give
the better results. Thus, it is concluded that the formulated hair serum provide better hair quality than
marketed products.
Keywords: Herbal Hair Serum, Formulations, Hair Loss, Dandruff, Boiling

Introduction moisturizing the scalp and provide the smooth and

Herbal is the data about plants with reference to soft texture to hair.
their therapeutic activity. Cosmeceuticals derived
from the terms cosmetics and pharmaceuticals. Materials and methods
They are the cosmetic formulations with bioactive Materials
constituents indicate to have medical benefits. All the plants like aloe vera, neem, curry leaves
Hair plays an important role in human being and and tulsi leaves used in the formulation of herbal
1
effectively increases the outlook of a person. serum was collected from the medicinal garden of
Serum is the product which coats the surface of Smriti College of Pharmaceutical Education, Indore
the hair and keep them smooth, silky and and oils was collected from local market of Indore.
untangled. The key element fenugreek have the
high proteins and nicotinic acid content which are Methods
beneficial in hair fall and dandruff and also treat Extraction of herbs: The extract was geared up by
3
baldness and hair thinning. Aloe gel, neem, curry the cold maceration. The fenugreek seeds, neem
leaves and tulsi keep the scalp conditioned, leaves, curry leaves and aloe gel were ground and
provide healthy hair growth and also help to kept in water for 72hrs. They were then dried and
improve blood circulation which keeps the scalp stored under desiccators for their further use.
cool. Castor oil and coconut oils both are used for

Table 1: Formulation of herbal serum

S.No Ingredients name Quantity (%)
1. Fenugreek seeds 100
2. Aloe gel 5
3. Tulsi leaves 5
4. Neem leaves 5
5. Curry leaves 5
6. Sugar 10
7. Castor oil 5
8. Coconut oil 5

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Preparation of serum: Suitable quantity of the oil The preservatives like methyl parabens and propyl
extracts was taken and size was reduced by the parabens was also added into the formulation
mechanical homogenization. Then all the aqueous which were in the proportion 1:1.
extracts were uniformly distributed in sufficient
quantity. Later, it was added into the prepared oil RESULT
extracts in the homogenizer and was blended The prepared formulated serum was evaluated
uniformly until a thick, clear liquid was formed. and the result was shown in the table number 02.

Fig. No.1 Herbal Hair Serum

Table 2: Evaluation of herbal serum

S. no Parameters Observation
1 Colour Light green
2 Odour Characteristic
3 Consistency Semi-solid
4 Viscosity
5 Spread-ability Good spreadability
6 pH 8
7 Wash-ability Easily washable
8 Irritability Non-irritant

CONCLUSION 2. Venkataramana A.P, Jayaganesh S and

The present study was done to prepare and Jainendra M; Evaluation of leave-on hair
evaluate a herbal serum using fenugreek seeds, serum containing higher amount of
aloe gel, tulsi leaves, curry leaves and neem leaves silicones; 2016; 2516-2517.
as the active ingredient. The prepared herbal 3. Adhirajan N, Ravi Kumar T,
serum was also evaluated for various parameters Shanmugasundaram N, Mary Babu J;
and was found to fulfill the required nourishment, Ethnopharmacology; National Center for
growth and texture of the hair. Biotechnology Information; 2003; 235-
239.
REFERENCES 4. Aruna V, Amruthavalli GV and Gayathri R;
Hair Root Activation by Anagen Grow- A
1. Akshay Negi, Dr. Luv Kush; Trichophoric Herbal Hair Growth Serum; JOJ
Ayurvedicophore; International Journal of Dermatology and Cosmetics; 2019; 0056-
Innovative Research and Development; 0058.
2013; 128-131.

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DEVELOPMENT AND CHARACTERIZATION OF HERBAL FACE SERUM

VISHAKHA CHAUHAN*, HIMANI SINGH, ARTI MAJUMDAR, NEELESH MALVIYA
Department of Pharmacy, Smriti College of Pharmaceutical Education,
4/1 Pipliya Kumar, MR-11, Dewas Naka, Indore-452010 (M.P), INDIA
[email protected]

ABSTRACT
The purpose of this study was to produce a serum product containing Glycyrrhiza glabra and
Nyctanthesarbortristis as an active ingredient. The serum is a care product that you can apply to your skin after
cleansing, but hydration with the intention of transmitting powerful ingredients directly to the skin. The serum
is particularly suitable for this function because it is composed of small molecules which can penetrate deep
into the skin and provide a very high concentration of active ingredients. Maceration process used for the
extraction of key ingredients. The herbal face serum was prepared and then evaluated for distinguish
physiochemical parameters such as appearance,globule size, consistency of the serum, spreadability and pH.
The serum was slightly viscous and sunset yellow in color. The pH of formulation was found to be 6.1. The size
of globule was found to be in range of 0.3 to 0.8μm which enhances the penetration power of serum into skin
layers. The herbal face serum stimulates cell growth and restoring of damaged skin.Thus, it can be concluded
that herbal faceserum restores firmness and suitable for various skin ailments.
Keywords: Face serum, Nyctanthesarbortristis, Glycyrrhiza glabra, Anti-oxidant

Introduction superficial layer of the skin, while the serum

Serum is a product that has a gel-like texture, acts at a deeper level, thus completing the
a concentrate that provides more hydration beauty routine.As Ayurveda promotes hydration
to the skin, while providing a variety of as an important part of the skin care regimen
substances that can help fight aging or containing the double advantage of essential oils
scarring. Thanks to its light texture, it is very and glycosides, the attractive. N. arbortristis
quickly absorbed by the cosmetic skin, and flower offers antifungal properties and treats skin
acts in the deeper layers of the dermis to problems such as blackheads, pimples.
Yashtimadhu or Liquorice rootprovides even tone
promote its well-being. The serum is filled
to the skin and lighten the complexion.
with moisturizing ingredients to help the skin
retain moisture. Face lotions and creams are Benefits of herbal face serum
more enriched and create a barrier on the Increases collagen production,Gives a satiny
skin thatkeeps all the good things texture to the skin, Restores strength, Signs of
inside.Neither moisturizers for the face or aging decrease, Lightens pigmentation, Eliminate
anti-aging creams nor eye contour creams, fine lines.
because these products act in the most

Table No.1 Formula of herbal face serum

Ingredients Quantity (ml)
Glycyrrhiza glabra 30
N. arbortristis 25
Glycerine 15
Almond oil 10
Propyl paraben 2
Methyl paraben 2
Rose water q.s. to 100

Cold maceration process: grounded to coarse powder using grinder

The flowers of Nyctanthes arbor tristis and roots of separately. A conical flask with 100gms of the
Glycyrrhiza glabrawere collected and dried in the powdered substance taken and five hundred
shade for 5 days. Dried petals and roots were milliliters ethanol poured into it. The mixture was

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stirred thoroughly with a glass rod. The conical ethanolic extract of Glycyrrhiza glabra and
flask was kept with intermittent shaking for 72 h. Nyctanthes arbor tristis added to it, again mixed to
The mixture was filtered, and the resultant residue get a proper blend of all the ingredients. Methyl
was kept in a refrigerator till further use. paraben and propyl paraben added as
preservatives. The thick paste was obtained. At
Formulation of herbal serum: Herbal face serum last rose water used to attain the final serum
was prepared by using mechanical homogenization solution of suitable consistency.
method. the excipients placed together in a
homogenizer to obtain size reduction. Then the

Fig.1 Herbal Formulation of Face Serum

Table No.2 Evaluation of herbal face serum

S. No. Parameters Inference
1. Color and Appearance Sunset yellow and liquid consistency
2. Texture Smooth
3. Viscosity 0.91poise
4. Homogeneity Smoothly blended homogenized liquid formulation
5. pH 6.1
6. Sensitivity test No irritation
7. Immediate skin feel No greasiness
8. After feel (4 hours) Light on skin

Results and discussion necessary parameters which was found in limit.

Approximately 9g extract was obtained from 100 g Thus, it can be concluded that herbal face serum
of powder through cold maceration. The pH of restores firmness and suitable for various skin
formulation was found to be 6.1. The texture of ailments.
serum was smooth, no greasiness at the time of
application and felt light even after 4hours of References
application on skin. The size of globule was found 1. P Divya Paikara1, Sheetal Singh and
to be in range of 0.3 to 0.8μm which enhances the Bhawana Pandey Pytochemical Analysis of
penetration power of serum into skin layers. The Leave Extract of Nyctanthesarbortristis IOSR
herbal face serum stimulates cell growth and Journal of Environmental Science,
restoring of damaged skin. Toxicology and Food Technology (IOSR-
JESTFT) e-ISSN: 2319-2402,p-ISSN: 2319-
Conclusion 2399. 1(3): 39-42.
The aim of the study was to formulate and 2. Shan Sasidharan, PyarryJoseph ,Junise, “
evaluate herbal face serum. The extraction of N. Formulation and evaluation of fairness
arbortristis and Glycyrrhiza glabra was successfully serum using polyherbal extracts”.
done by cold maceration process. The herbal International Journal of Pharmacy. 2014;
serum was formulated by mechanical 4(3): 105-112
homogenization method and evaluated for all the

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DEVELOPMENT AND EVALUATION OF FLAX SEED AND GREEN TEA HAIR GEL: A
NATURAL HAIR STYLER
HIMANI SINGH*, VISHAKHA CHAUHAN, ARTI MAJUMDAR, NEELESH MALIYA
Smriti College of Pharmacy Education, Indore
[email protected]

ABSTRACT
Nowadays herbal preparations are gaining popularity in the world market, due to side effect of synthetic
preparations. The present study deals with the development and characterization of herbal hair styling
preparation. The focus of the current research was to prepare and evaluate the herbal gel of flaxseed and
green tea extract for the purpose of nourishing the hair. Flaxseed (also known as linseed) is full of fatty-acids
and anti-oxidants which help to remove toxins and dead cells from the scalp and green tea have good solar
protection activity as well as antioxidant activity. We prepared and evaluated different concentration of gel
formulations which containing carbopol 934 ranging from 0.5, 1, 1.5 and 2%.The pharmacopeial evaluations
were done to all the formulation batches (F1 to F4). Various Pharmaceutical parameters like physical
appearance, viscosity, grittiness, spreadibilty and pH of gel evaluated. Gel which contains 0.5% carbopol 934
has liquid consistency and run easily within 4 to 5 hours of preparation. When we made gel from 1.5%
carbopol 934 the formulation was satisfactory to some extent but the problem of liquefaction was found after
24 hours. It was found that 2% carbopol 934 containing formulation was satisfactory and got a uniform and
smooth gel that was not runny even after 24 hrs. F4 having 2% carbopol among all the four formulations,
showed better evaluation result and was stable for long period of time.
Keywords: herbal gel, Carbopol 934, Antioxidant, Flax seed, Green tea

Introduction 200, methyl-paraben and glycerine were

Flaxseed and green tea are natural ingredients purchased from OM enterprises Indore.
which are used for various benefits. Now a day
synthetic preparations are harmful in some extent Methodology
due to chemical ingredients in it. So the industry Formulation of Herbal Hair Gel
moved on herbal preparation because of less or Polyethylene glycol, glycerine and methyl paraben
1
none side effects and no use of chemicals. Hair gel was weighed in a measure quantity and added the
is a hair styling products that used for a particular entire measured ingredients into 35 ml water in a
hairstyle and have so many side effect like hair beaker. This mixture was mixed by a mechanical
loss, dandruff, discoloration and damage so for stirrer at a high speed. After that carbopol 934 and
that reason we made herbal hair gel using herbal PVP were added slowly into above mixture with
ingredients like green tea and flex seed. As u all continuous stirring. Then slowly gelling agent
know flex seed also known as linseed has (triethnolamine) was added into above liquid and
important functional ingredient having chemical it was stirred continuously until gel was obtained.
constituents like α-linolenic acid, lignans, and fiber. Carbopol used in various concentrations like 0.5g,
Flaxseed oil has ability to impart some health 1g, 1.5g, 2g and 2.5g as a gel base. After that we
benefits such as in cardiovascular disease found that 0.5 and 1g carbopol gel base was
reduction, use in atherosclerosis, in cancer liquefied after 4 to 5hr. For 1.5 g carbopol gel base
treatment, and diabetes etc. Besides this, it was also liquefied after 24 hr. Gel formed with
flaxseeds contain fatty acid with anti-oxidants 2g was smooth and uniform in nature and not
which help in removing dead cells from the scalp liquefied. 2.5 g carbopol gel base was too thick so
2
and toxin too. Green tea also rich in catechins, we was choose 2 g carbopol gel base for
and it help in hair loss reduction because reducing formulation batches preparation.
(Dihydrotestosetrone) and it also help in fight
3
dryness of scalp and dandruff. Preparation of herbal hair gel
Flaxseed aqueous extract was prepared by adding
Materials and methods seeds into boiling water with continuous stirring
Materials used until thick mucilage were formed. Obtained
Flaxseeds and green tea were purchased by from mucilage was constrained using sieve and stored
the local market. Carbopol934, Polyethylene glycol at room temperature for further use. Green tea

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extraction obtained by decoction process. After method with 2 % carbopol gel base. The prepared
that five different formulation batches (HF1 to herbal gel formulations were stored at room
HF5) were prepared by simple gel preparation temperature until further evaluation.

Table.1 Formulation of herbal hair gel

Formulation code HF1 HF2 HF3 HF4 HF5
Aqueous extract of flaxseed % 5 10 15 20 25
Green tea extract g 0.5 0.5 1 1.5 2
Carbopol 934(g) 2 2 2 2 2
PVP (mg) 4 4 4 4 4
Methyl paraben (mg) 70 70 70 70 70
Glycerine (ml) 3 3 3 3 3
PEG (ml) 6.15 6.15 6.15 6.15 6.15
Triethanolamine(ml) 0.5 0.5 0.5 0.5 0.5
Water (ml) 35 35 35 35 35

Results and discussion or aggregates were checked visually. For all the
Physical appearance formulations homogeneity was found good.
The colour of all the herbal gel formulations HF1,
HF2, HF3, HF4 and HF5 were found to be pale Viscosity determination
brown with opalescent and smooth on application. The viscosity of all the formulations were found in
the range of 1,5321 to 1,52, 765 cps. From the
Homogeneity results it is clear that as the concentration of
All the formulated batches were tested for flaxseed extract increased from 5% to 20% the
homogeneity. Presences of any lumps, flocculates viscosity of the formulations also increased.

Table 2: Evaluation of herbal hair gel

Formulation Code Physical appearance Homogeneity *pH Viscosity cps.
H1F4 Opalescent , pale brown, smooth Good 6.5 1,50,321
H2F4 Opalescent , pale brown, smooth Good 6.6 1,50,745
H3F4 Opalescent , pale brown, smooth Good 6.7 1,51,342
H4F4 Opalescent , pale brown, smooth Good 6.9 1,51,790
H5F4 Opalescent , pale brown, smooth Good 7.1 1,52,765
*Each reading is an average of three readings

Conclusions 3. Han A and Mirmirani P. Clinical approach

The formulation of hair gel provides a good base to the patient with alopecia. Semin Cutan
for treating the scalp and strengthens the hair Med Surg. 2006; 25(1):11-23.
thereby preventing the hair fall. There is a further
scope for pharmacological studies in lower
animals.

References
1. Singh KK, Mridula D, Jagbir Rehal and
Barnwal P. Flaxseed. A Potential Source of
Food, Feed and Fiber, Critical Reviews in
Food Science and Nutrition. 2011;
51(3):210-222.
2. Ankit Goyal, Vivek Sharma, Neelam
Upadhyay and Sandeep Gill. Flax and
flaxseed oil an ancient medicine and
modern functional food. J Food Sci
Technol. 2014; 59(9):1633-1653.

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FORMULATION AND EVALUATION OF CUCURBITA PEPO HERBAL FACIAL SCRUB

Harshal Deshmukh*, Janhvi Yadav, Vishakha Chauhan, Neelesh Malviya
Smriti College of Pharmaceutical Education, Indore
[email protected]

ABSTRACT

“Cosmetics” is derived from the combination of two Greek words viz: “kosmtikos”, meaning of which relates to
adornment. In general, cosmetics can be referred as the products that are meant for cleansing, beautifying and
promoting attractiveness. Herbs are widely used as remedial agents because herbs are less expensive, easily
available and non toxic. Thus, Herbal cosmetics, prepared by the association of bioactive ingredients and
pharmaceutical products have become more popular. The existence of number of photochemical and botanicals
in the herbal products have twofold impact: one that they are used as cosmetics for body care and another that
photochemical improves the biological functions of human body naturally results in healthy skin. The main aim
of the present study is to formulate and evaluate the cucurbita pepo facial scrub using natural ingredients. The
natural ingredients are used to fight against the wrinkles, acne problem and various other skin problems. The
natural ingredients used are employed with antibacterial, antioxidant and anti ageing properties. In this
preparation cucurbita pepo, turmeric, honey and cinnamon are used as active ingredients which are then
incorporated into the scrub formulation. Other ingredients include glycerine, rosewater, triethanolamine and
sodium lauryl sulphate. Then, various parameters such as appearance, pH, viscosity, spreadability, washability,
irritability are evaluated for the prepared gel. Also, it is checked to be satisfying with all the required
characterizations. Thus, the developed formulation can be used for the healthy and glowing skin benefits.
Keywords: Cosmetic, Cucurbita pepo, Anti-ageing, anti-oxidant, Acne, Anti-bacterial, Scrub

Introduction: Preparation of the extract (Phase I): The extract

Cosmetics are available in various different forms was geared up by the cold maceration. The
with each one having the significant effect on skin. Cucurbita pepo, turmeric and cinnamon were grind
The various skin problems such as non-glowing and separately and kept in water for 72hrs. They were
dullness over the skin can be swept away by the use then dried and stored under desiccators for their
of the prepared scrub formulation. Skin can be further use.
classified into following three types which are: dry Preparation of the Phase II: Honey and glycerine
2
skin, oily skin and sensitive skin. On frequent was added in the container and with their addition
application of the scrub, the skin turns out be triethanolamine was also added to neutralize the
glowing and smoother as the dead cells from the pH.Later on, the volume was made up by the
skin are removed and persistently exposing the new addition of rosewater if required. The active
cells. Scrubs can be applied directly or through the ingredient mixture was then mixedand stirred in the
4
use with a cosmetic pad. Gentle massage is usually phase II. Finally, the prepared scrub formulation
recommended as it tends to enhance the blood was obtained as desired.
circulation and also increase the oxygen supply to
3
the skin. Therefore, the present study is focussed Result
on the Formulation and Evaluation of the Cucurbita The prepared formulated scrub was evaluated and
pepo herbal facial scrub. The key ingredients the result was shown in the table number 02.
employed are Cucurbita pepo, turmeric, cinnamon
and honey which possess specific properties: Conclusion
Antibacterial, Antioxidant, Anti-ageing and Anti- The present study was attempted to prepare a
inflammatory. Cucurbita pepo herbal scrub using Cucurbita pepo,
turmeric and cinnamon as the active ingredient.
Materials and methods The prepared scrub formulation was also evaluated
Materials: Plant was collected from the medicinal for various parameters and was found to be
garden of Smriti college of Pharmaceutical satisfied with the application on the skin to make
Education, Indore and local market of Indore. the skin healthy and glowing without any side
effects.

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Table 1:Formulation of Cucurbita pepo herbal scrub

S.No Ingredients name Quantity (%)
1. Cucurbita pepo 10
2. Turmeric 1
3. Cinnamon 8
4. Glycerine 4
6. Honey 4
7. Triethanolamine 2
9. Rose water q.s 50

Fig.01: Prepared fprmulation

Table 2: Evaluation of Cucurbita pepo herbal scrub

S.No Parameters Observation
1. Colour Pale yellow
2. Odour Characteristic
3. Consistency Good
4. pH 6.1
5. Viscosity 1.452 poise
6. Wash-ability Easily washable
7. Foam-ability Foam volume 100ml at 5 minutes
8. Irritability Non-irritant

REFERENCE 3. Harish N.M., Prabhakara Prabhu, and

1. Shoba Rani R; Herimanth, Textbook of Subrahmanyam E.V.S. Formulation and
Industrial Pharamcy, Drug Delivery systems Evaluation of in situ gels containing
and Cosmetics and Herbal Drug Clotrimazole for oral candidiasis. Indian J.
Technology: Universities press (India) Ltd; Pharm.Sci. 2009; 71(4): 421-427.
nd
2 edition. 4. Bharadwaj S., G.D. Gupta and U.K. Sharma,
2. Garg A., Agrawal, D. And Garg; s. Spreading Topical Gel: A Novel Approach for drug
of semi-solid formulation. Pharm Tech. delivery. J. Chem. Bio. Phy. Sci 2012; 2(2):
2002; 9:89-105. 856-857.

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APPLICATION OF LIQUISOLID TECHNIQUE TO ENHANCE SOLUBILITY AND DISSOLUTION

PROFILE OF FLURBIPROFEN
Madhavi Kasturi*1 and Neelesh Malviya2
1
Research Scholar, Mandsaur University, Rewas Dewda Road, Mandsaur, M.P- 458001
2
Department of Pharmaceutics, Smriti College of Pharmaceutical Education, Indore – 452010
[email protected]

ABSTRACT
The purpose of the current research work was to enhance solubility and dissolution profile of poorly water
soluble drug, Flurbiprofen using liquidsolid technique. Flurbiprofen is a potent NSAID indicated for acute and
chronic treatment of rheumatoid arthritis, osteoarthritis, and ankylosing spondylytis. Reason to select
Flurbiprofen as model drug is that because it belongs to BCS Class II having poor aqueous solubility (0.013
mg/mL) and shows dissolution limited absorption. Initially, saturated solubility studies were performed to select
suitable solvent using various non volatile solvents. Later, Flurbiprofen liquisolid compacts were prepared using
PEG 600 as non volatile hydrophilic vehicle, Avicel PH 102 as carrier and Aerosil 200 as coating material. Several
formulations of Flurbiprofen liquisolid compacts were prepared ranging from F1 to F9 and are subjected to pre-
compression rheological studies; and post-compression evaluations such as weight variation, disintegration and
in vitro drug release. Among all, F3 formulation was selected as it showed highest drug release in 60 minutes and
also showed better release profile compared to conventional formulation. Drug-excipient interaction was not
observed which was confirmed using FTIR studies. Finally, it can be concluded that liquisolid technique proved
successful in enhancing both solubility and dissolution profile of poorly water soluble drugs like Flurbiprofen.
Keywords: Flurbiprofen, Liquisolid technique, carrier material, coating material, solubility

Introduction Materials and methods

Liquisolid also known as Powder solution Materials and Methods
technology introduced by Spireas (Spireas S; 2000) Flurbiprofen, Avicel PH 102 and Aerosil 200, sodium
is the most promising and innovative technique for starch glycolate, propylene glycol, PEG 200, PEG
promoting dissolution and in vivo bioavailability of 400, PEG 600, Tween 80, Tween 20. All reagents
poorly soluble drugs. This technique involves used were of analytical grade
admixture of poorly water soluble drug with non
volatile solvent capable of solubilising drug to form Solubility studies
liquid medication. Further this is admixed with Saturated solutions were prepared by adding an
suitable carrier material and coating material to excess drug to vehicles and shaking with a shaker
form free flowing readily compressible powder. The for 48h at 25±0.5 °C and analyzed by
Liquisolid techniques are considered as pleasantly spectrophotometer at λmax 247 nm.
flowing and compressible powdered forms of liquid
medications (Shashidher B, 2011). Flurbiprofen is Formulation of Flurbiprofen liquisolid compact
non-steroidal anti-inflammatory drug that belongs Nine liquisolid compacts from F1 to F9 containing
to BCS class II (Bhaskar D, 2017) and hence selected 50 mg of Flurbiprofen were prepared
to formulate as liquisolid compacts.
Table 1. Formulation of Flurbiprofen liquisolid compacts
F Drug R Drug Lf PEG Q q SSG Mg Talc Final
code concentration(%) stearate wt
TF1 33.33 5 50 0.382 100 392.67 78.5 15 5 2 643.2
TF2 33.33 7.5 50 0.333 100 450.45 60.0 15 5 2 682.5
TF3 33.33 10 50 0.309 100 485.43 48.5 15 5 2 705.9
TF4 40 5 50 0.382 75 327.22 65.4 15 5 2 539.6
TF5 40 7.5 50 0.333 75 375.37 50.0 15 5 2 572.4
TF6 40 10 50 0.309 75 404.53 40.4 15 5 2 591.9
TF7 50 5 50 0.382 50 261.78 52.3 15 5 2 436.1
TF8 50 7.5 50 0.333 50 300.3 40.0 15 5 2 462.3
TF9 50 10 50 0.309 50 323.62 32.3 15 5 2 477.9

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Results and discussion studies were conducted for all formulations. Finally
Based on solubility studies PEG 600 is selected as F3 formulation is selected as best.
vehicle to prepare liquid medication for
Flurbiprofen. Conclusion
Finally, it can be concluded that liquisolid technique
Pre-compression studies and post compression proved successful and a better alternative
studies technique in enhancing both solubility and
Pre-compression studies and post compression dissolution profile of poorly water soluble drug
studies pre-compression rheological studies and Flurbiprofen.
post-compression evaluation such as weight
variation, disintegration and in vitro drug release

500
400
300
200
Series1
100
0 Series2

Fig 1. Solubility studies for Flurbiprofen

Table 2. Pre and post compression studies

Parameter F1 F2 F3 F4 F5 F6 F7 F8 F9
Pre-compression
Bulk 0.427± 0.442±0. 0.446±0. 0.411±0. 0.421±0. 0.436±0. 0.379±0. 0.586±0. 0.392±0.
density 0.03 07 02 04 01 02 03 02 01
Tapped 0.507± 0.532±0. 0.543±0. 0.486±0. 0.507±0. 0.527±0. 0.465±0. 0.472±0. 0.487±0.
density 0.05 02 11 03 02 03 02 04 02
Carr’s 15.779 16.917 17.863 15.432 16.962 17.267 18.494 18.220 19.507
Index
Hausner’s 1.1873 1.20361 1.21748 1.18248 1.20427 1.20871 1.22691 1.22279 1.24234
Ratio
Angle of 30.14± 29.14±1. 28.02±1. 32.10±1. 31.66±1. 31.94±1. 33.77±1. 32.85±1. 30.49±1.
repose 1.44 13 28 30 25 33 21 31 43
Post compression
Weight 643.20 682.510 705.980 539.670 572.425 591.983 436.136 462.340 477.987
variation
Hardness 3.3±0. 3.4±0.05 3.7±0.13 3.1±0.17 3.1±0.12 3.2±0.07 2.8±0.09 2.8±0.12 2.9±0.09
05
Friability 0.53±0 0.54±0.0 0.51±0.0 0.49±0.1 0.61±0.0 0.58±0.0 0.57±0.1 0.58±0.1 0.56±0.1
.06 5 9 2 7 8 1 4 8
Disintegrat 3.09±0 3.12±0.4 2.96±0.3 2.73±0.3 2.87±0.2 3.03±0.3 2.14±0.3 2.31±0.2 2.56±0.3
ion (min) .22 1 4 2 1 1 7 9 4

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Flurbiprofen liquisolid compacts

TF1
Cumulative percent drug 120 TF2
100 TF3
80
TF4
60
TF5
release

40
20 TF6
0 TF7
0 20 40 60 80 TF8
TF9
Time (min) DCT

Fig 2. In vitro drug release studies of Flurbiprofen liquisolid compacts

References Pharmaceutical Sciences 2011; 47(3):475-

1. Spireas S and Bolton SM. Liquisolid 482.
systems and methods for preparing same, 3. Bhaskar D, Naveen C, Sateesh Kumar V and
United States patent 6,096,337, 2000. Rama Rao T: Solubility and dissolution
2. Shashidher B, Madhusudhanrao Y and enhancement of flurbiprofen by solid
Venkateswarlu V: The Liquisolid technique: dispersion using hydrophilic carriers.
an overview. Brazilian Journal Brazilian Journal Pharmaceutical Sciences
2017; 53(4) 1-10

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FORMULATION AND EVALUATION OF HERBAL ANTIBACTERIAL SOAP FOR TREATMENT OF

ACNE
Namrata Rathore, Tahir Nizami, Darshana Sharma, Neelesh Malviya
Smriti College of Pharmaceutical Education, 4/1 Pipliya Kumar, MR-11, Dewas Naka,
Indore-452010 (M.P), INDIA
[email protected]

ABSTRACT
The herbal plants are known to have various potentials like antibacterial and antiacne properties. Skin infections
are most common amongst people, requiring significant attention for treatment and also to maintain healthy
skin. Some herbal plant extracts have antibacterial activity and anti aging activity. The Herbal plants (leaves and
flower pallets and steam barks) extract preparations are used to enlarge the physical appearance and need to
protect and maintain a healthy skin. The motive of the present research work was to formulate herbal soap for
purify the skin, prevent clogging pores, blemish free skin and control acne breakouts. It keeps skin hydrated and
treatment of multiple diseases of the skin. Different herbal and crude components like Aloe Vera leaves, Neem
leaves and steam bark and Tea leave and hibiscus flower pallets were used in new formulation. The
compositions of formulation were evaluated for different physicochemical parameters for which fine
characteristics was observed. This formulation exhibited a good antibacterial effect. The easy availability of herbs
and plants around us with cost-effective benefits and less or no side effects.
Keywords: Antibacterial Activity, Aloe Barbadensis, Hibiscus Rosa-Sinensis, Azadirachta Indica

Introduction wounds to moisturizing. There's a small amount of

Bacteria are the plural of bacterium, which are scientific evidence suggesting that applying aloe
microscopic one-celled organisms. They are found Vera to your skin may help reduce the appearance
everywhere and can be harmful, as in infections; or of hyper pigmented areas, though it won't
they can be beneficial, as in fermentation or completely get rid of these darker spots.
decomposition. Different antibiotics (Coccus,
Bacillus, Spirillum, Rickettsia, and Mycoplasma) and Materials and methods
their chemical composition are used to diseases Collection and Authentification of the Plant:
caused by human pathogens. The use of antibiotics The Leaves of hibiscus, neem and aloe-vera were
has been under constant challenge due to collected from Botanical garden of SCOPE, Indore.
emergence of resistant microorganisms. An herbal Preparation of extracts of hibiscus flower and tea
remedy for skin care with antibacterial activities is leave, neem steam bark and leave:
prepared from a variety of plant parts such as The accurately weighed powdered plant materials
leaves, stem, root, bark, flower or fruit. These were extracted using petroleum ether, chloroform,
medicines are administered topically and may be ethyl acetate, ethanol and distilled water in Soxhlet
applied in the form of cream, lotion, gel, soap, apparatus. After about forty siphons of each solvent
scrub, solvent extract or ointment, and have been extraction step, the materials were concentrated by
established to possess antimicrobial properties. evaporation.
Hibiscus rosa-sinensis extracts are used in Preliminary antibacterial screening of the extracts:
various skin care products as they contain high All the extracts of leaf and flower were subjected to
levels of Vitamin C in the natural form. Since preliminary antimicrobial screening by agar well
the flower also has anti-inflammatory properties, it diffusion method against the organisms E coli
is used in anti-acne creams and soap. (MTCC-1698), S aureus (MTCC-1143). The extracts
Azadirachta Indica leaves moisturise your skin and which exhibited maximum activity were selected for
make it soft and supple. It's anti-fungal and the formulation.
antibacterial properties also helps lighten scars and Preparation of formulations:
pigmentation that are caused by acne. Neem leaves Three extracts that exhibited maximum
are also known to cure pimples on your face. Make antibacterial activity were prepared in
a decoction of Neem leaves and apply it on your combinations in two different concentrations i.e.
pimples for a smooth skin. 250 mg each (750 mg) and 500 mg each (1500 mg)
Aloe barbadensis has been found to have many and these combinations of extracts were
health benefits for the skin, from helping to heal incorporated in the prepared formulations.

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Herbal antibacterial soap for anti-acne: ml with distilled water in 100 ml measuring
Solidified basic glycerine soap was broken down to cylinder. Measured the foam height, above the
smaller pieces and melted on water bath. 1.5grams aqueous volume by given 25 strokes.
of the extract (Aloe Barbadensis, Hibiscus Rosa- Foam Retention:
Sinensis, Azadirachta Indica) combinations were Prepared the 25 ml of the 1% soap solution and
added to the melted soap along with 5ml of transferred into the 100 ml of measuring cylinder.
ethanol. 0.033 g of stearic acid, 1ml each of coconut Then the cylinder was shaken 10 times. The volume
oil and tea oil was added to the melted soap. The of foam was recorded at one minute for 2.5 to 2.6
melted soap was gently mixed for about 30 minutes minutes.
and moulded in circular moulds. The soap was Wash ability:
allowed to solidify at room temperature until set Herbal formulations were applying on the skin then
and kept under physical observation for any simply remove by washing with water was checked
characteristic changes. manually.
Antibacterial testing of the prepared soap
Evaluation parameters formulations:
All the soap base formulations prepared were The prepared soap was subjected to antibacterial
tested for their physicochemical properties. screening by agar well diffusion method.
Organoleptic evaluation: Organisms used were E coli (MTCC-1698), S aureus
Organoleptic evaluation (color, and clarity) was
(MTCC- 1143). One gram of soap was mixed with 5
done by sensory and visual inspection.
Determination of pH: ml of sterile water and used for evaluating the
The pH of prepared herbal formulation (soap) was antibacterial activities. The plates were incubated
0
determined by using a digital pH meter. at 37 C for 24 hours and the zones of inhibition
Foam Height:Dissolved 0.5 gm of prepared soap in were recorded.
distilled water then make up the volume up to 50

Table: 1 Evaluation Parameter of Herbal Antibacterial Soap Formulation anti-acne:

Form Color Od Appea p % Foam Foam Alcohol High
ulatio our rance H free heig retention insoluble temperatur
n alkali ht (min) matter e stability
e
Soap Gree Frag Good 7. 0.32 25cm 2.5 9.2 Soap melts
0
n rant 3 above 60 C

Results
Preliminary antibacterial screening of the extracts: Antimicrobial screening of the prepared
The initial susceptibility testing of the different formulations:
extracts of leaves, flowers and stem bark of Aloe The extracts that exhibited maximum antimicrobial
Barbadensis, Hibiscus Rosa-Sinensis, Azadirachta activity were ethyl acetate bark extracts of
Indica was done by using agar diffusion method. Azadirachta Indica and ethanolic bark extracts of
The stem bark extracts of Azadirachta Indica Azadirachta Indica and Hibiscus Rosa-Sinensis with
showed considerable antbacteriall activity in terms zones of inhibition ranging from 11 to20 mm. Hence
of zones of inhibition. The extracts of leaves these three extracts were prepared in combinations
showed inhibition zones. The leaves and of Aloe and incorporated in formulations in two different
Barbadensis, Hibiscus Rosa-Sinensis, Camellia concentrations i.e. 250 mg each (750 mg) and 500
sinensis also showed significant zones of inhibition. mg each (1500 mg). Both the formulations
The observations are recorded in Table 2. exhibited good zones of inhibition ranging from
18to26 mm. The results are tabulated in Table 3.
Discussion and conclusion good antibacterial effect among which the ethyl
The plants Azadirachta Indica and Aloe Barbadensis, acetate bark extracts of Azadirachta Indica a and
Hibiscus Rosa-Sinensis were extracted using four ethanolic bark extracts of and Azadirachta Indica
different solvents of increasing polarity and the and and Hibiscus Rosa-Sinensis exhibited maximum
extracts were subjected to antibacterial screening. activity with zones of inhibition ranging from 11 to
Results revealed that most of the extracts exhibited 18 mm. This is in accordance with the antibacterial

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International Journal of
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ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

activities. Furthermore those extracts exhibiting synergistic effect or total sum of effects produced
maximum activity were selected and their by the combinations of extracts. Further, the
combinations were included in our prepared herbal prepared soap formulations were standardized by
soap formulations. The prepared formulations evaluating various physicochemical properties such
when tested for antibacterial activity exhibited as pH, colour, appearance, foam height, foam
zones of inhibition ranging from 18 to 26 mm which retention, wash ability and etc. However, these
was far better than the zones of inhibition of formulations need to be further standardized as
individual extracts. This enhancement of good antibacterial activity.
antibacterial properties may be attributed to the

Table 2: Zones of inhibition (mm) of leaf and bark extracts of Azadirachta Indica, Hibiscus Rosa-Sinensis Zones of
inhibition (mm) of leaf and Aloe Barbadensis.
S.No. Sample code Microorganism
E.coli S.aureus
1. AIB PET 8 6
2. AIB CHL 14 -
3. AIB ETH 18 18
4. AIB EOH 20 18
5. AIL PET 16 -
6. AIL CHL 16 10
7. AIL ETH 16 7
8. AIL EOH 18 10
9. HRSB PET - -
10. HRSB CHL - -
11. HRSB ETH 8 -
12. HRSB EOH 11 8
13. HRSL PET - -
14. HRSL CHL 12 7
15. HRSL ETH 14 6
16. HRSL EOH 18 11
17. ABL PET - -
18. ABL CHL 10 -
19. ABL ETH 18 10
20. ABL EOH 15 -
AIB =AILAzadirachta Indica Bark, AIL=Azadirachta Indica Leave, ABL=Aloe Barbadensis Leave, HRSL=Hibiscus
Rosa-Sinensis Leave , HRSB=Hibiscus Rosa-Sinensis Bark PET= Petroleum ether, CHL= Chloroform, ETH=
Ethyl acetate, EOH= Ethanol.

Table: 3 Antibacterial screening of the prepared formulation:

S. No. Formulation Zones of inhibition in mm
E. coli S aureus
1 HS-1 20.0 18.0
2 HS-2 22.0 24.0
HS-1=Herbal Soap with 750 mg concentration, HS-2=Herbal Soap with 1500 mg concentration.

Reference
1. Oyedele AO, Akinkunmi EO, Fabiyi DD, 2. Nagat M, Barka E, Lawrence R, Saani M.
Orafidiya LO. Physicochemical properties Phytochemical screening, antioxidant and
and antimicrobial activities of soap antibacterial activity of active compounds
formulations containing Senna alata and from Hemidesmus indicus. Int J Curr Pharm
Eugenia uniflora leaf preparations. J Med Res 2016;8:24-7.
Plant Res 2017;11:778-87. 3. Maru AD, Lahoti SR. Formulation and
evaluation of moisturizing cream

International Journal of Pharmaceutical Sciences and Research: Conference Proceedings: Special ssue; March, 2020 Page | 37
International Journal of
Pharmaceutical Sciences and Research
ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

containing sunflower wax. Int J Pharm Adina cordifolia (karamkigaach). Indian J.

Pharm Sci 2018;11:54-9. Physiol. Pharmacol.,14: 209-210.
4. Sharma K, Joshi N, Goyal C. Critical review 7. KR. Khandelwal, Practical Pharmacognosy
of ayurvedic var?ya herbs and their technique and
tyrosinase inhibition effect. Anc Sci Life experiments,NiraliPrakashan, Pune, 2001,
2015;35:18-25. 2nd edition, 149-56.
5. Hussain A, Virmani OP, Popil SP, Mishra LN 8. Trease GE, Evans WC. Text book of
and Gupta AK. Dictionary of Indian Pharmacognosy. 13th (eds).Alden Press;
Medicinal Plants. CIMAP Lucknow, 1980. Oxford; 2003, 512-513.
6. Sabir, M. and Razdan, M.K. (1970).
Antifertility study with leaf extracts of

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International Journal of
Pharmaceutical Sciences and Research
ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

PREPARATION AND CHARACTERIZATION OF DOCETAXEL LOADED NANO LIPID CARRIERS

Arti Majumdar1,2, Nidhi Dubey1, Neelesh Malviya2
1
Devi Ahilya Vishwavidyalaya, Indore, M.P., 2Smriti College of Pharmaceutical Education,
Indore (M.P.)
[email protected]

ABSTRACT
Nano lipid carriers loaded with docetaxel were prepared by Solvent emulsification evaporation method. Stearic
acid and soya phosphotidylcholine was used as solid lipid and oleic acid was used as liquid lipid in the ratio 8:1:1
respectively. The developed NLCs were evaluated for various parameters like average particle size, polydispersity
index (PDI) Zeta potential, entrapment efficiency and in vitro drug release study. The prepared formulations
were also studied for in vitro cell line and cell uptake study. It was revealed that the average size of NLCs was
found 269.5±4.12, PDI was 0.126±2.26, percent entrapment efficiency and drug loading was found 69.8±3.24
and 6.52±1.28 respectively and Zeta potential was found -21.3±3.5. In vitro drug release study 72.5±3.2% drug
was released after 24 hr. Therefore it can be inferred that NLCs can be used as an effective drug delivery system
and is able to release drug for longer period of time.
Keywords: Docetaxel, NanoLipidCarriers, Cytotoxicity, Solvent emulsification evaporation, Cell uptake

Introduction a clear lipid phase. In a separate beaker, 100 ml of

Docetaxel used to treat a number of breast cancer, double-distilled water containing 1 % tween 80 was
head and neck cancer, stomach cancer, prostate heated up to 70°C. Under the high-speed
cancer, and non-small-cell lung cancer. It is the homogenizer (IKA T 25 digital ULTRA-TURRAX®,
taxane family of medications [1]. Unwanted drug Germany) at 10000 rpm the lipid phase containing
distributions or chemotherapeutic failure of drug is drug was added dropwise with the help of a
the major reason behind various side effects and it micropipette to the aqueous phase to make
is needed to design an appropriate safe and stable microemulsion. The aqueous phase was maintained
drug delivery system which overcomes the side at 70ᵒC. After 30 min heating was stopped and the
effect. Nano Liquid Crystals (NLCs) are novel drug stirring was continued on magnetic stirrer at
delivery systems having properties and advantages 1500rpm for two hours at room temperature. After
like polymeric nanoparticles and solid lipid separation with the help of cooling centrifuge, the
nanoparticles with better drug loading and stability prepared formulation was lyophilized using
by eliminating drug expulsion as observed in case of Labconco freeze dryer (Labconco, Cascade Freezone
SLN [2,3]. NLCs are non-toxic and can be prepared Plus 4.5 L Benchtop Freeze dryer, USA) and stored
by using biocompatible lipids. at 8 °C until further used for characterization.

Materials and methods Characterizations of docetaxel-loaded NLCS

Materials Docetaxel was obtained as a gift sample Determination of particle size, PDI and surface
from Sun Pharma Pvt Ltd. Ahmadabad, India. charge: After dilution of formulations 10 times v/v
Stearic acid was purchased from Himedia, Mumbai, with deionized water, mean particle size
India. Oleic acid was purchased from Loba distribution of Docetaxel loaded NLCs and
Chemical, Mumbai, India. and soya PC were polydispersity index (PDI) of the NLCs were
purchased from Sigma Aldrich, USA. Other determined by Particle and Zeta Analyzer with
chemicals and solvents were used of analytical autotitrator, Lite Sizer 500 (Anton Paar, Austria)
reagent grade. Fig.1).For the determination of zeta potential
Preparation of docetaxel loaded NLC: The samples were diluted with 0.9 % NaCl to adjust the
docetaxel-loaded NLCs were prepared Solvent conductivity of 50 μS/cm. Zeta potential was
emulsification evaporation method reported earlier determined by Lite Sizer 500 (Anton Paar, Austria)
with slight modification. The lipids, stearic acid, Particle size, size distribution, and zeta potential the
oleic acid and soya PC were taken in ratio 8:1:1 prepared formulation was performed at the
dissolved in 12 ml of ethanol: acetone(1:1)solvent Department of Pharmacy, IGNTU, Amarkantak, MP,
system in a 25 ml of beaker. 30mg of Drug India. (Table 1)
(docetaxel 10%w/w of lipid content) was added to Shape and surface morphology: The shape and
above mixture. The mixture was melted 70 °C to get surface morphology were examined by scanning

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ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

electron microscopy (SEM). The photomicrographs Results and discussion

of prepared NLCs were taken with SEM (FESEM, Determination of particle size and PDI
GeminiO, Giess, Netherlands) fig. 2. Analysis of Simadzu 1800 UV- visible spectrophotometer at
sample on SEM was carried out at IISER, Bhopal, 232nm
India. In Vitro release study
Lyophilized NLC formulation equivalent to 10 mg of
Determination of entrapment efficiency (EE) and drug were dispersed in 50 ml 0.5 wt % sodium
Drug loading: lauryl sulfate PBS 7.4 solution in 50 ml glass test-
The lyophilized NLC formulation equivalent to 10 tube. The resulting sample was stirred at 300 rpm,
mg of drug was taken in a 50 ml of beaker and one milliliter of the dispersion was withdrawn
containing 10 ml of ethanol and dissolved. The from the system at definite time interval and
solution was then centrifuged at 10000 rpm for 15 filtered with 0.22µm filter. The filtrate was analysed
min. The 1.0 ml of the supernatant solution was by UV-VIS spectrophotometer (UV-1800 Shimadzu
withdrawn with the help of micropipette and Spectrophotometer) at 232nm as described above
transfered in to a 10 ml volumetric flask. The (fig. 3).
volume was made up to 10 ml with PBS 7.4 and In Vitro release study: 72.5±3.2% drug was released
analyzed spectroscopically for drug content using after 24 hrs (fig 3)

Fig 1: Determination of particle size and PDI

Table 1: Characterization of Docetaxel loaded NLCs

Average vesicle size (nm) PDI Zeta % Entrapment efficiency Drug
potential loading
(mV)
269.5±4.12 0.126 ±2.26 -21.3±3.5 69.8±3.24 6.52±1.28

100
80
% Drug release

60
40
20
0
0 1 2 3 4 5 6 12 24
Time(hrs)

Fig 3: In Vitro % Drug release

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Fig 2: SEM image of Docetaxel loaded NLC

Conclusion 2. Majumdar A, Dubey N, Malviya N.

Therefore from the above study it can be concluded Nanostructure lipid carriers: a promising tool
that NLCs can be used as an effective drug delivery for the drug delivery in the treatment of skin
system and are able to release drug for longer cancer. Asian J Pharm Clin Res. 2019; 5: 15-26
period of time 3. Majumdar A, Dubey N. Formulation of
Paclitaxel loaded nanostructured lipid carriers
References: to study the effect of concentration of liquid
1. Majumdar A, Dubey N, Dubey N, Dermal lipids on drug release. Journal of Drug Delivey
delivery of docetaxel loaded nano liquid and Therapeutics. 2017; 7(7): 26-28.
crystals for the treatment of skin cancer, Int J
App Pharm, Vol 11, 2019; 5: 188-193

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ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

IN-VITRO FORMULATION AND EVALUATION OF LAMIVUDINE TRANSDERMAL PATCHES

*1 1 1
Ashima Ahuja, Jitendra Gupta, Reena Gupta
*1
Institute of Pharmaceutical Research, GLA University, Mathura-281406, U.P, India
[email protected]

ABSTRACT
Lamivudine an antiretroviral(ARV) drug effective against HIV through reverse transcriptase resulting in
termination of DNA chain were casted as transdermal patches act as a non-invasive delivery of medication across
skin membrane in order to improve patient compliance &minimise the side effects of oral medication. The oral
bioavailability (80%, plasma half life 6hrs) of lamivudine is poor due to high pass first effect this lead to
formulation of polymeric based matrix trans-dermal patches of LAMto provide better rational to control the drug
release across the membrane. This study focuses on usage of polymers HPMCK 4M,Eudragit RS 100 &evaluated
for Drug polymer interaction using FTIR, other parameters like physical appearance, thickness, drug content
uniformity,(%) moisture absorption, folding endurance, tensile strength, in-vitro drug release study performed
usingphosphate buffer (pH 7.4). In-vitro drug release showing LAM2 (1:1) showedhighest percentage
(98.55±0.03%) of drug release following zero kinetics.
Keywords:Transdermal patches, Lamivudine, patient compliance, ARV.

Introduction Patches were visually inspected for clarity and

Transdermal drug delivery promotesdelivery of appearance.
drug into circulatory system to obtain immediate, Drug Content Uniformity
effective, potent release of active drug at controlled Patches were cut, dissolved in Phosphatebuffer (pH
rate across skin membrane for decreasing incidence 7.4), stirred overnight; drug content was assessed
5
&intensity of adverse effects of oral medication by UV-VIS spectroscopy .
1
achieving optimum plasma concentration .Over a Thickness
past decade there has constant surge &attempts Thickness of patches was measured using calliper.
made to eradicate HIV from society by controlling Folding endurance andTensile strength (T.S.)
multiplication of virus inside human Patches were cut, repeatedly folded at same place
2,3
body .Lamivudine improves health andexpandlife until they broke to determine folding endurance.
span of HIV infected patients. Patches were sandwiched between plates, one end
was fixed, other end was attached to pulley,
Materials and methods gradually weights were added, breakage time was
Materials noted down, and tensile strength was calculated
4
Lamivudine, HPMCK4M, ERS 100, as a gift sample using formula .
obtained from Nishka scientific &research lab, T.S. = F/cd(1+L/1), where, F-Force needed for
Hyderabad. All the other reagents were of breaking, c-patches width, d-thickness, L-elongation
analytical grade. at break
DrugPolymer Interactions Percentage moisture absorption
Pure drug of LAM was analysed by FTIR Patches were weighed, stored in desiccators
3
(Shimadzu1700) . contain potassium chloridefor determination of
6
Fabrication of Matrix Lamivudine Transdermal percentage moisture absorption .
Patches (%) moisture absorption=[final weight-initial
Matrix type LAM transdermal patches were weight] X 100
formulated with HPMCK4M, ERS100 (solvent In-vitro Drug release study
casting method). After 24 hrs of drying, patches In-vitro drug release studyusing phosphatebuffer
were suitably cut for characterization study(Table (pH 7.4)was performed fordetermination of amount
4 6
1) . of cumulative drug permeated across skin .

Evaluation parameters of transdermal patches Results and discussion

Surface morphology SEM showed formation of pores ensuring drug
Surface morphologywas performed using SEM (EM release from the patches(Fig.1),FTIR(drug&LAM 2)
5 -1
5800 LV instrument, Japan) . (Fig.2)have prominent peaks at 1850cm (cystedine
-1 -1
Physical Appearance nucleus), 1384cm , 1063cm (oxathilane ring),
physical appearance was found to be clear, good,

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showing thickness ranging from 0.37±0.041 to ranging from 2.68±0.12 to 2.97±0.03, in-vitro drug
0.47±0.021mm, folding endurance showed good, release for formulation LAM1-LAM4 showed
satisfactory results ranging from 75±4 to 78±4mm, release of 97.43±%, 98.55% , 94.98±%, and 91.11±%
found to be increasing with increased conc. of respectively and showing decreased drug release
ERS100, tensile strength was uniform ranging from with increased ERS100 as compare to HPMC K 4M,
1.78±0.5 to 2.45±0.5mm, %age moisture (Table 1, Fig.3).
absorptiondecreased with increasing ERS100 conc.

Table 1: Evaluation parameters of lam patches

Patch Drug Polymers mg Thickness Tensile Folding %Moisture %Drug %Cumulative
code (mg) (mm) ±SD strength Endurance absorption Content drug release
a a a a
ERS HPMC (mm) ±SD ±SD ±SD (24hrs)
100 K 4M ±SD
LAM 1 50 250 500 0.40±0.023 1.78±0.5 75±4 2.97±0.03 98.5±0.9 97.43
LAM 2 50 500 500 0.37±0.041 1.96±0.8 76±2 2.84±0.01 99.1±0.1 98.55
LAM 3 50 750 500 0.47±0.021 2.12±0.3 78±1 2.71±0.03 98.9±0.4 94.98
LAM 4 50 1000 500 0.38±0.040 2.45±0.5 78±4 2.68±0.12 97.8±0.6 91.11
a
( N=3±S.D.)

Fig1: sem of LAM 2 patch

100
90
Cumulative % Drug Release at

80
70
60
50
40 Cumulative
24 hrs

30 percentage
20
10 release
0
LAM 1 LAM 2 LAM 3 LAM 4
Patch

Fig 3: % Drug release of LAM patches

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(a)

(b)
Fig2: FTIR of LAM2 patch (a), pure LAM (b)

Conclusion Future Journal of Pharmaceutical

The present study focuses on formulation Sciences Dec 2018; 4(2):166-174.
&evaluation of LAM transdermal patches with ERS 4. Posina A, Sundarapandiyan R, Mohamed
100 and HPMC K4M. The results indicated that the S, KommireddyUmasankari, Boddu PR and
LAM patches can be successfully used in C Chetty M: Preparation of in-vitro, in-vivo
management of HIV patients and control of ARV characterization of transdermal patch
disease. containing glibenclamide and atenolol: A
combinational approach. Pakistan Journal
References of Pharmaceutical Sciences April
1. Ham A and Buckheit R: Current and 2011;24(2):155-163.
emerging formulation strategies for the 5. Suksaeree J, Siripornpinyo P and Chaiprasit
effective transdermal delivery of HIV S: Formulation, Characterization and In-
inhibitors. Therapeutic delivery future vitro Evaluation of Transdermal Patches for
Science 2015;6(2): 217–229. Inhibiting Crystallization of Mefenamic
2. Jain S, Tiwary A, Sapra B and Jain Acid. Journal of Drug Delivery 2017:1-7.
N:Formulation and Evaluation of 6. Mamatha T, Venkateswara R, Mukkanti K
Ethosomes for transdermal delivery of and Ramesh G: Development of matrix
Lamivudine. AAPS PharmSciTech 2007; 8 type transdermal patches of lercanidipine
(4):1-9. hydrochloride: physicochemical and in-
3. Ramadan E, Borg T, Abdelghani GM and vitro characterization. DARU Journal of
Saleh NM: Design and in vivo Pharmaceutical Sciences 2010; 18(1): 9-11
pharmacokinetic study of a newly
developed lamivudine transdermal patch.

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FORMULATION, CHARACTERIZATION AND ANTIMICROBIAL ACTIVITY OF POLYHERBAL HAND

WASH
Jitendra Gupta, Reena Gupta,1 Ashima Ahuja1
‡1
†1
Institute of Pharmaceutical Research, GLA University, Mathura-281406, Uttar Pradesh, India
[email protected]

ABSTRACT
Hand hygiene is the primary &foremost important for preventing nosocomial infections because hand is
responsible for transmission of pathogenic bacteria. The research work was carried out to investigate
phytochemical screening of Tulsi (Ocimum sanctum), Cinnamon (Cinnamon zeylanicum), Neem
(Azadirachtaindica) extracts, andLemon grass oilwith antimicrobial activity of their polyherbal hand wash
formulations F1, F2 and F3 by using disc diffusion method against S. aureus,Pseudomonas aureogenosa, and E.
coli pathogen. It was concluded that all formulation (800>400>200µg/mL) showed significant antimicrobial
activity against all pathogens but F3 formulation (800µg/mL) showed potent effect against E. coli in comparison
to other due to the presence of medicinally active phytoconstituents.This research becomes fruitful for the herbal
industry to commercially developed plant extract not only for polyherbal hand wash but also for antiseptic soaps
or lotions or gels to overcome the undesirable side effects of synthetic hand sanitizers and effectively maintained
hygiene.
Keywords: Tulsi, Cinnamon, Sensitivity test, Nosocomial infections, Herbal hand wash.

Introduction room tempwith addition of perfume andmade up to

3
Nosocomial infectionisthe common problem of 100 with water .
mankind responsible for enhanced morbidity
&mortality. The contaminated hand causes the Evaluation of herbal extracts and polyherbal hand
transmission of pathogens responsible for wash
1
nosocomial infection .Hand wash containing Preliminary Phytochemical Tests
alcohol controls the nosocomial infection but have The presence of various phytoconstituents were
side effects like itching, contact dermatitis, identified in methanolic extracts responsible for
4
sensitivity reaction etc. So such problem can be antimicrobial activity .
managed by using polyherbal hand wash (PHW) Physical properties
which contain potent phytoconstituents like Organoleptic properties such as color, odour,
tannins, terpenoids, glycosides, flavonoids, phenolic homogeneity & appearance of polyherbal hand
compounds, alkaloids &volatile oil having proven wash formulations werevisually inspected
2
potential for in-vitro antimicrobial activity . pH
pH ofPHW formulations (F1 to F3) calculated with
Materials and methods digital pH meter.
Plant materials & Authentication Viscosity
Cinnamon bark, Tulsi & Neem Leaves procured from Brookfield viscometer (LV model) was used for
herbal garden and authenticated fromDept. of study ofviscosity of all PHW.
Pharmacognosy, GLA University Mathura. Foam height
Pathogenic microbesas E. coli (ATCC-10531), Ps. 20 mL PHW formulation was taken in graduated
aeruginosa (ATCC-25619), S. aureus (ATCC-65388) measuring cylinder separately andshaken 10 times.
were chosen for antibacterial activity. The volume of foam was recorded for 4 min at 1
Preparation of extracts min. interval.
10gdried powder of Cinnamon bark, Tulsi, Neem In-vitro Antimicrobial sensitivity of polyherbal
leaves wereextracted in Soxhlet extractor hand wash
0
separately at 60 C using methanol & water (9:1) Agar plate disc diffusion method
2
ratio, 60 min . The antimicrobial sensitivity test using ciprofloxacin
Preparation of Polyherbal hand wash as a standard against pathogens of different
The methanolic extracts of Cinnamon,Tulsi, Neem concentration of PHW (F1 to F3) were investigated
5
(Table 1) were dissolved with sodium lauryl .
sulphate (surfactant), glycerin (humectant)present Stability
in aqueous medium containing preservative. As per ICH guidelines 8th, 2003, stability study ofF1
6
Thesolution was homogenized by homogenizer at to F3 were investigated .
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Result and discussions wall and causes cell lysis. All PHW were found to be
Physicochemical properties like colour, odour, stable with no sign of colour change and phase
homogeneity, appearance of PHW(F1 to F3)were separation.
depicted in Table 2. Phytochemical
screeningshowed the existence of active Conclusion
phytoconstituents(Table 3)in methanolic extracts Polyherbal hand wash were developed for proper
that are responsible for antimicrobial activity.From health andhygiene. From the resultsit was
Table 4, the results of antimicrobial activity concluded that methanolic extract of herbs andtheir
depicted thatPHW(F1 to F3)(800>400>200µg/mL) combination with lemon grass oil have significant
showed significant antibacterial action against all ZOIfor pathogens against skin infection serving as
pathogens but F3 (800µg/mL) showed more potent rational for using hand wash as antiseptic soaps,
action against S. aureus because of interaction lotions or gels in maintaining hand hygiene.
&partition of phytoconstituents in to bacterial cell

Table 1: Composition of various PWH formulations.

Ingredients F1(100mL) F2 (100mL) F3 (100mL)
Methanolic Extract of Cinnamon, Neem 20 mL - -
Methanolic Extract of Tulsi, Neem - 20 mL -
Methanolic Extract of Cinnamon, Neem, Tulsi - - 20 mL
Lemmon grass oil 0.1 mL 0.1 mL 0.1 mL
Perfume q.s. q.s. q.s.
Glycerine 40 mL 40 mL 40 mL
Sodium lauryl sulphate 6g 6g 6g
Preservative 0.25 g 0.25 g 0.25 g
Distilled water q.s. q.s. q.s.

Table 2: Physicochemical characteristics of PHW.

b b
FC Color Homog Appearance Odour pH Viscosity F.R. (sec)
b
eneity (Cps)
F1 Brown-greenish HG TLT Fragrant 6.5±0.3 52±1.2 173±7
F2 Greenish yellow HG TLT Characteristics 6.4±0.2 58±0.9 117±4
F3 Brown-greenish HG TLT Fragrant 6.8±0.5 61±1.7 238±9
b
N=3±SD, FC: Formulation code, TLT: Translucent, HG: Homogenous; F.R.: Foam retention

TABLE 3: Phytochemical analysis of various methanolic extracts.

EXT Terpenoids Saponins Alkaloids Tannins Flavonoids Phenols Steroids
TE + + + - + + +
CE + + + + + - -
NE - + + + + + +
+: Presence, -: Absence,EXT:Extracts; CE:CinnamonExt., TE:TulsiExt., NE:NeemExt.

Table 4: In-vitro antimicrobial activity of various phw.

Micro- Zone of Inhibition (mm)
organism F1 (µg/mL) F2 (µg/mL) F3 (µg/mL) Standard
200 400 800 200 400 800 200 400 800 100
E. coli 17±0.5 21±0.3 25±0.4 14±0.3 18±0.5 21±0.4 20±0.4 24±0.5 27±0.5 33±0.5
Ps. aeruginosa 10±0.3 14±0.4 15±0.5 9±0.3 11±0.4 13±0.2 13±0.3 16±0.2 18±0.4 24±0.4
S. aureus 15±0.5 18±0.4 22±0.3 11±0.2 16±0.3 19±0.6 17±0.2 21±0.5 24±0.3 29±0.6
b
N=3±S.D., Standard- Ciprofloxacin

References
1. Black J: Microbiology: Principles and 2. Gupta R, Gupta MK, Bhandari A, Gupta J and
Applications, New Jersey, 1996; (3):436-443. Pathan I: Preparation and standardization of
polyherbomineral formulation. International
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Pharmaceutical Sciences and Research
ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

Journal of Drug Development and Research 1999;(2) 181,213,216, 224, 279, 315, 322, 390,
2014; 6(2):211-19. 425-427, 593-597.
3. Sandeep DS, Rompicherla NC, Nayak P, 5. Gupta R and Gupta J: Investigation of
Maharjan A and Ghalan I: Formulations of antimicrobial activity of Euphorbia hirta leaves.
antimicrobial polyherbal hand wash. Research International Journal of Life Science and
Journal of Pharmacy and Technology Pharma Research 2019;9(3):32-37.
2016;9(7):1-3. 6. ICH guidelines, Stability testing of new drug
4. Kokate CK, Purohit AP and Gokhale substances and products, 27th October, 1993.
SB:Pharmacognosy, NiraliPrakashan, Pune,

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DEVELOPMENT AND CHARACTERIZATION OF SOLID LIPID NANOPARTICLES CONTAINING

RUTIN FOR THE MANAGEMENT OF DIABETES MELLITUS
Neelima Salvi*1, Gajendra P. Choudhary1
*Smriti College of Pharmaceutical Education, Indore, M.P.-452010
1
School of Pharmacy, Devi Ahilya Vishwavidyalaya, Indore, M.P.-452001
[email protected]

ABSTRACT
Current work aimed at the modified release of content from carrier system at predetermined rate and secondly,
to decrease the use of synthetic drug on biological system. Successive solvent extraction of crude drug of Aegle
Marmelos plant was done. Active constituent of leaves that is rutin was isolated and identified through HPTLC
and FTIR. SLN was selected as carrier system and fabricated by solvent diffusion method. Characterization and
performance evaluation of particulate system loaded with herbal plant extract of the Aegle Marmelos leaves was
done. TEM, In-vitro drug release profile, entrapment efficiency and particle size was determined. Solid lipid
nanoparticles have enormous effect in loading high amount or loading dose concentration in body and also
maintain the same over prolonged interlude of time. was formulated and characterized for the particle size,
shape and its distribution, percentage drug entrapment and In-vitro drug release profile along with the stability
studies. Conclusion: Solid lipid nanoparticles also show good stability as compared to other novel carrier systems.
Prolonged release of natural drug from carrier system, decrease the dosing frequency and also decrease the dose
size. Better results than marketed synthetic anti-diabetic drugs.
Keywords: Particulate system, plant extract, Aegle Marmelos, diabetes mellitus, controlled release.

Introduction college, Indore. Identification and authentication

Diabetes mellitus (DM) is a metabolic disorders, was confirmed by Department of Botany, Holkar
which is characterized hypergycemia (high blood Science College, Indore.
[1]
glucose). Nanoparticles are the submicron Preparation of extracts: The coarsely powdered,
measured particles, going 10–1000 mm. dried plant parts (50 g) were extricated with 300 mL
- 500 mL oil ether by hot extraction procedure
Material and methods (soxhlet) for 4 hours. Then extracts were used for
Collection and authentication of plant leaves: phytochemical screening.
Aegle marmelos was collected from Agriculture

Figure 1: HPLC spectra of isolated rutin

Spectrophotometric analysis: and no. of particles formed. Optimized formula used

UV double beam spectrophotometer- Shimadzu for further work. Solvent diffusion method has been
model no.1800 used in which Glyceryl monostearate was dissolved
HPLC- The isolated moiety was distinguished by in acetone and ethanol (1:1 v/v) in water bath at
HPLC strategy and contrasted and standard of the 60ºC and this was added to aqueous phase (distilled
equivalent, by utilizing section and a blend of water) under mechanical agitation for 45 minutes.
methanol: water (1:1 proportion). This was subjected to centrifugation at 4000 rpm for
10 minutes. Resuspended in water which results in
Preparation of Nanoparticulate system: formation of solid particles. Finally the
Solid lipid nanoparticles were optimized on the nanoparticles were collected by filtration and are
basis of % entrapment, drug content, stirring time washed with demineralized water.
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Table 1: Optimization of GMS: Drug ratio

3
Formulation GMS:rutin ratio Average particle size (nm) % Entrapment No. of particles per mm X1000
NPL-1 9:1 2.23±0.35 64.4±1.2 27±2.5
NPL-2 8:2 2.34±0.89 68.8±0.98 28±2.2
NPL-3* 7:3 2.69±0.65 70.5±1.10 36±1.9
NPL-4 6:4 2.75±0.18 65.4±1.43 28±1.6
NPL-5 5:5 2.77±0.18 64.6±1.43 25±1.4
*Data SD (n= 3)are shown as mean

Characterization of Nanoparticulate system:

Particle size and distribution: The size and size Entrapment Efficiency: The amount of drug
distribution of particles was determined using laser entrapped in the particles was then determined by
diffraction particle size analyzer (Cilas, 1064 L, disrupting the particles followed by filtration and
France). The particulate suspension was dispersed subsequent determination of the drug content using
in distilled water and then it was put into the spectrophotometric method (Table No. 1).
sample chamber of particle size analyzer and
measurement of particle size was carried out (Table
No. 1).
Particle Size and Shape

60
NPL-3
%Drug Release

0
0 10 20 30
Time (hrs)
Figure 2: In-vitro drug release of rutin nanoparticles
Results and discussion profile because of carrier system which results in
Nanoparticles was prepared by optimizing the zero order drug delivery in body. We used drug of
formula and process, formulation NPL-3 (7:3) shows herbal origin which is again a benefit to get rid of
average size 2.69µm with % entrapment of continuous use of synthetic drugs daily, which
70.5±1.10 % was selected for further experiment. ultimately gives side effects on body.
Drug release pattern performed and after different
time interval drug release pattern continuously References
increased in sustained manner. Release also altered 1. Tan Q, Liu W, Guo C, Zhai G. Preparation
with the solid lipid nanoparticles prepared by and evaluation of quercetin-loaded
solvent diffusion method; shows improved drug lecithin-chitosan nanoparticles for topical
release profile. In-vitro drug release studies shows delivery. International journal of
that drug release controlled over prolong period of nanomedicine. 2011;6:1621.
time i.e. after 24hrs. 45.7% drug was released; this 2. Rao KJ, Paria S. Green synthesis of silver
will also decrease the dosing frequency of active nanoparticles from aqueous Aegle
constituent. marmelos leaf extract. Materials Research
Bulletin. 2013 Feb 1;48(2):628-34.
Conclusions
After development of solid lipid nanoparticles
containing rutin shows controlled drug release
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PREPARATION AND EVALUATION OF NOVEL IN-SITU GEL CONTAINING ACYCLOVIR FOR THE
TREATMENT OF HERPES SIMPLEX KERATITIS
Abrar Hussain*, Arti Majumdar, Neelesh Malviya
Smriti College of Pharmaceutical Education, Indore (M.P.)
[email protected]

ABSTRACT
Herpes simplex Keratitis (HSK), which is a major cause of corneal infection. The virus (Herpes simplex virus) enters
into a latent phase. It presents primary infection as conjunctiva and eyelids swelling and mild inflammation.
According to global research of herpes Keratitis is around 1.5 million, including 40,000 new cases of severe
monocular visual impairment or blindness every year. Several topical and oral antiviral drugs for HSK are
commercially available. However, low patient compliance and toxicity hamper use in HSK. Thus, a safe and
effective delivery for HSK is required. The conventional ocular drug delivery systems such as suspension,
ointments and solutions show drawbacks such as increased low efficiency, blurred vision and precorneal
elimination respectively, leading to poor bioavailability. Ophthalmic In-situ gels, which are viscous polymer-based
liquids that are instilled into eyes as drops that further undergoes sol-to-gel transition which improved ocular
bioavailability by increasing duration of corneal contact and thereby reducing frequency of administration. Merits
of Ophthalmic in-situ gels over conventional dosage forms are possibility of releasing drugs at constant and slow
rate with accurate dosing, increased ocular residence time and increased shelf life. This research includes ion
induced in-situ-forming polymeric systems using combination of gelling agents to prolong corneal contact time,
eradicate drug elimination and increase the bioavailability.
Keywords: Ion activated Phase transition system, in-situ gel, Sodium Alginate, Bioavailability.

Introduction temperature. After cooling to room temperature,

A new approach is to try to combine advantages of drug and preservative were added and stirred until
both solutions and gels, such as accuracy and facility drug dissolved. Remaining amount of sodium
of administration of the former and prolonged chloride solution was added into it. The resulting
residence time of the later. Thus in situ gels can be solution was stored in a refrigerator for further use.
instilled as eye drops and undergo an immediate Crystallization of the drug was observed after 48
gelation when in contact with the eye. In situ- hour. To avoid crystallization of drug in freeze thaw
forming hydrogels are liquid upon instillation and conditions, 0.05% of disodium edetate was
under ocular cul-de-sac to form viscoelastic gel and incorporated in the formulation. It is also reported
this provides a response to environmental changes. in literature, that disodium edetate prevents
In-situ forming hydrogels are liquids that can crystallization in freeze thaw conditions.
undergo a phase transition from a liquid to gel (or Formulation was terminally sterilized by autoclaving
◦
solid phase), upon instillation into the lower cul-de- at 121 C temperature and 15 psi pressure for 15
sac of the eye. It transforms from an easy to instill min.
liquid to a transparent or translucent gel that is
retained longer in the eye by reduced lacrimal Result and Discussion
drainage, which results into prolonged release of
the drug, and increased bioavailability, thus Rheological studies
reducing the need of frequent administration. Viscosity of sol and gel was found to be 55 cps and
1325 cps respectively at 50 rpm.
Materials and method
Materials: Acyclovir was provided by Sunpharma Conclusion
Pharmaceutical Pvt. Ltd., Indore and further To overcome bioavailability problems, as observed
reagents and chemicals used during formulation in drops present in market which shows rapid
were analytical grade. precorneal loss and only small amount of applied
drug penetrates cornea.
Method As a consequence of precorneal loss, typical corneal
Formulation of Acyclovir In-situ Gel contact time is limited to 1-2 minutes with less than
Sodium chloride was dissolved in 100 ml of distilled 10% bioavailability. Aqueous solution dropped in
water. Sodium alginate was dispersed in a part of eye undergoes transition into gel state which
◦
above solution and stirred for 20 min at 90 C improves
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bioavailability and patient compliance. It combines accuracy and facility of administration and prolongs
advantage of both solutions and gels such as residence time.

Table 1: Gelling Property of Sodium alginate Solution with Simulated Lacrimal Fluid (SLF)
Concentration of Sodium alginate Solution Gelling Property in SLF
0.5% -
1% +
1.5% ++
2% ++
2.5% +
3% +
- = no gelation + = immediate gelation ++ = immediate gelation which persisted for extended period of time.

Table 2: Evaluation parameter of In-situ Gel formulations

Parameters Observations
AN/ACYISG/1 AN/ACYISG/2 AN/ACYISG/3
Clarity Clear Clear Clear
pH 7.4 7.4 7.4
Drug Content(%) 98.75% 98.53% 97.46%

Table 3: Stability Data for Optimized In-Situ Gel of Acyclovir

Time Storage Condition Colour Clarity pH Drug Content
Initial NA Slight yellow Clear 6.3 98.75%
One week 2-8˚C Slight yellow Clear 6.3 98.53%
Room temp. Slight yellow Clear 6.3 97.46%
40˚C Slight yellow Clear 6.28 97.15%

References in ocular drug delivery. Adv Drug Delivery Rev

1. Sreeraj M. and Mitra A. K.: Overview of ocular 2005; 57:1595-639.
drug delivery. Ophthalmic drug Delivery 4. Smart J. D.: The basics and underlying
systems, Second edition. Ed. Marcel Deckker, mechanisms of mucoadhesion. Adv Drug
Inc.: Kanas city Missouri U.S.A. 2003; 1-5. Delivery Rev. 2005; 57:1556- 1568.
2. Kristiina, J.; Tomi, J. and Urtii, A.: Ocular 5. Nanjawade B. K.; Manvi F. V. and Manjappa A.
absorption following drug delivery. Adv Drug S.: In situ-forming hydrogels for sustained
Delivery Rev. 1995; 16:3-19. ophthalmic drug delivery. Journal of Control
3. Ludwig, A.: The use of mucoadhesive polymers Release 2007; 122 (2): 119-34.

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FORMULATION AND EVALUATION OF FLOATING TABLET OF RILPIVIRINE HYDROCHLORIDE

FOR THE TREATMENT OF HIV-1
Dipali Trivedi*, Arti Majumdar, Neelesh Malviya
Smriti College of Pharmaceutical Education, Indore (M.P.)
[email protected]

ABSTRACT
Besides enormous improvements in drug delivery, oral route has been highly and effectively utilized route of
administration. Floating drug delivery that is also known to be Low Density System is an advancement in the class
of Gastro-retentive drug delivery system. In the present research work, floating drug delivery of Rilpivirine
hydrochloride was developed by overcoming various limitations and troubles associated with the drug including
poor absorption in intestinal pH and degradation when comes in contact with higher pH environment. Prepared
formulations were evaluated for various parameters like friability, hardness, thickness, drug content analysis,
floating properties and in-vitro drug release study. Based on the evaluation, concluded that floating drug delivery
system is a non-toxic as well as cost-effective technique for the rationale of enhancing bioavailability and
absorption of poorly water soluble drugs. Floating delivery system are those having sufficient buoyancy over
[5]
gastric fluid due to the lower density of drug as compared to gastric fluid. The FDDS can float in the gastric
environment for several hours to prolong the residence time of drug in gastric region and thus improves the
absorption of drug that are unsuitable for intestinal pH. It can be able to use in the future for more acidic soluble
drugs to enhance solubility and absorption.
Keywords: Floating, Rilpivirine, gastric residence time, effervescent.

Introduction Materials and Methods

A virus that devastate the immune system of the Materials
body and causes Acquired Immuno Deficiency Rilpivirine hydrochloride was received as a gift
Syndrome (AIDS) is Human Immuno Deficiency Virus sample from Cipla Research and Development,
(HIV). Number of drugs are investigated to be anti- Mumbai. HPMC, Sodium bicarbonate and micro
[1]
HIV. The drugs like Rilpivirine appears to be most crystalline cellulose were received from Smriti
appropriate non- nucleoside reverse transcriptase College of Pharmaceutical Education, Indore.
inhibitor for the treatment of HIV-1 in adults Further chemicals used during formulation were
because it has better tolerability which leads to less analytical grade.
drug discontinuation and fewer side effects as
compared to other NNRTIs. Methods
The main objective of the research work was to Preparation of Tablets
develop a gastric floating drug delivery system The active ingredient and excipients were weighed
consisting Rilpivirine. The solubility and systemic accurately and powder blend was directly
absorption of Rilpivirine is pH dependent. It is compressed into tablet with the help of tablet
demonstrated by an increased bioavailability in an punching machine consisting of 25 mg of Rilpivirine
[2]
acidic environment. To improve the absorption of hydrochloride.
Rilpivirine by preventing the drug from alkaline
environment, floating tablet was prepared.

Table 1: Composition of Rilpivirine hydrochloride floating tablets

Composition F1(mg) F2(mg) F3(mg)
Rilpivirine hydrochloride 25 25 25
HPMC 70 90 80
Cross povidone 60 40 50
Microcrystalline cellulose 50 60 40
Magnesium stearate 10 12 15
Sodium bicarbonate 28 19 25
Citric acid 50 70 55
Lactose 7 9 10
Total weight 300 300 300
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Result and Discussion sodium bicarbonate and citric acid as gas forming
The prepared tablet of Rilpivirine hydrochloride agents. From the dissolution studies, it was
were evaluated. observed that the formulation can float on the
surface of dissolution medium (0.1 N HCl gastric
Conclusion fluid) and sustain drug release for ˃24 hrs. The
In the present research work, effervescent floating tablets prepared showed better results with respect
tablet of rilpivirine hydrochloride were successfully to floating lag time, total floating time and drug
prepared using mixture of hydroxyl-methyl cellulose release profiles.
and microcrystalline cellulose as polymer matrix and

Table 2: Pre compression studies of designed formulation

Formulation Bulk density Tapped Carr’s Index Angle of repose
Code (gm/mL) Density (gm/mL) (%) (Ɵ)
F1 0.412±0.009 0.612±0.014 12.7±0.08 25.30±0.91
F2 0.516±0.007 0.741±0.022 13.24±0.13 26.33±0.88
F3 0.374±0.006 0.542±0.018 11.81±0.18 24.55±0.86

Table 3: Post compression studies of designed formulation

Formulation Thickness Hardness (Kg/cm2) Friability Weight Drug content
Code (mm) (%) Variation (mg) (%)

F1 3.12 ± 0.05 5.30 ± 0.25 0.84 ± 0.018 289 ± 0.10 96.25 ± 1.65
F2 3.89 ± 0.09 5.60 ± 0.30 0.78 ± 0.014 291 ± 0.15 93.15 ± 1.27
F3 4.10 ± 0.08 5.85 ± 0.40 0.90 ± 0.016 295 ± 0.18 95.22 ± 1.55

Table 4: Floating lag time and total floating time of designed formulation
Formulation Floating lag time Total floating time
Code (min:sec) (hrs.)
F1 5:55 ˃24
F2 7:95 ˃24
F3 8:10 ˃24

References 3. Vyas S.P. and Khar R.: Controlled Drug

1. Reeves J. and Doms R.: Human Immuno- Delivery concepts and advances. Vallabh
nd
deficiency Virus. Journal of General Prakashan, 2 edition 2012; 196-200.
Virology 2002; 83:2-6. 4. Rahim S.A. and Carter P.: Design and
2. Sharma M. and Louis D.: Rilpivirine: a new evaluation of effervescent floating tablet
non-nucleoside reverse transcriptase based on hydroxyethyl cellulose and
inhibitor. Journal of Antimicrobial sodium alginate using pentoxifylline.
Chemotherapy 2012; 68:1-2. Dovepress drug design, development and
therapy 2015; 1-6.

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FORMULATION AND EVALUATION OF TRANSDERMAL PATCH OF FEBUXOSTAT FOR

MANAGEMENT OF GOUT
Farheen Naaz*, Arti Majumdar, Neelesh Malviya
Smriti College of Pharmaceutical Education, Indore, M.P. (India)
[email protected]

ABSTRACT
The present research was aimed to formulate a soft and easy to handle transdermal patch consisting simple and
cost effective monolithic polymeric film as an attempt to deliver Febuxostat transdermally and overcoming
problems associated with its poor bioavailability and hepatic first pass metabolism. Transdermal patches of
Febuxostat were prepared by solvent casting method. Prepared formulations were evaluated for various
parameters tensile strength, thickness, folding endurance, % moisture content, % moisture uptake, % drug
content, % elongation, In vitro release and drug excipient compatibility. Based on the evaluation of transdermal
patches, concluded that the concept of transdermal drug delivery is a novel, nontoxic as well cost-effective
technique for enhancing the aqueous solubility and bioavailability of the drug. It can be concluded that
transdermal drug delivery works very simple in which drug is applied inside the patch and it is worn on skin for
long period of time. By this constant concentration of drug remain in blood for long time. Thus, overcome the
adverse effects caused by oral route.
Keywords: Febuxostat, Transdermal patch, Gout.

Introduction Material and method

Arthritis Material
Arthritis is the swelling and tenderness of one or Febuxostat was obtained as a gift sample from
more of your joints. The main symptoms of arthritis Alembic Pharmaceutical Pvt.Ltd. vadodra Gujarat,
are joint pain and stiffness, which typically worsen India. Ethyl cellulose (EC) was gift from Colorcon
with age. The most common types of arthritis are Asia Pvt. Ltd (Mumbai, India) and Maan
osteoarthritis and rheumatoid arthritis. Pharmaceuticals Ltd. (Ahmedabad, India),
Osteoarthritis causes cartilage — the hard, slippery respectively. Oleic acid (OA) and di-n-butyl-
tissue that covers the ends of bones where they phthalate (DBP) were procured from Sigma
form a joint — to break down. Rheumatoid arthritis Chemicals Ltd. (Ahmedabad, India). Other materials
is a disease in which the immune system attacks the used in the study (chloroform, methanol,
joints, beginning with the lining of joints. [1] dichloromethane, glycerol, potassium dihydrogen
phosphate, etc.) were of analytical grade. Double-
Gout distilled water was used throughout the study.
Gout is a form of inflammatory arthritis that
develops in some people who have high level of uric Method
acid in blood. The acid can form needle like crystals Transdermal patches containing Febuxostat were
in a joint and cause sudden, severe episode of pain prepared by the solvent evaporation technique in
tenderness, redness, warmth and swelling. [2] petridish. The backing membrane was cast by
pouring a 2.5 % (m/v) polyvinyl alcohol (PVA)
Transderamal patch solution followed by drying at 60 °C for 6 h, forming
A transdermal patch is a medicated adhesive patch a smooth, uniform,and transparent backing
that is placed on the skin to deliver a specific dose of membrane . The drug reservoir was prepared by
medication through the skin and into dissolving sodium alginate in Ethanol: Water (1:2)
the bloodstream. Often, this promotes healing to an mixture. Dibutyl phthalate 15 % (w/w of dry
injured area of the body. polymer composition) was used as a plasticizer. The
In almost all transdermal patch designs, the drug is drug 40 mg (in 5 mL solvent mixture Ethanol: water)
stored in a reservoir that is enclosed on one side was added into the homogeneous dispersion under
with an impermeable backing and has an adhesive slow stirring with a magnetic stirrer. The uniform
that contacts the skin on the other side. dispersion was cast on a PVA backing membrane
and dried at room temperature.

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Table 1: Composition of Transdermal Patch

S.No INGREDIENTS TD1 TD2 TD3 TD4
1 Febuxostat 40 40 40 40
2 Sodium alginate 150 150 - -
3 Ethyl cellulose - - 150 150
4 PEG400 22.5 - 22.5 -
5 Dibutyl phthalate - 22.5 - 22.5
6 Oleic acid 22.5 22.5 22.5 22.5

Result and discussion

Table 2: Evaluation of transdermal patch
Parameter TD1 TD2 TD3 TD4
Thickness(mm) 0.55 0.59 0.60 0.56
Drug content (%) 60 66 62 65
Folding endurance 5 4 5 5
-2)
Tensile strength(kg cm 3 3 4 5
Moisture content (%) 33 32 35 33

Conclusion References
The method of preparation of transdermal patches 1. Roddy, E., Doherty M., 2010. Epidemiology of
of Febuxostat presented in this research work is gout. Arthritis research and therapy.51-59.
simple. All formulation also showed good 2. Ragab, G., Elshahaly M., Bardian Thomas., 2017.
physicochemical properties like thickness, weight Gout: An old disease in new perspective.
variation, drug content, flatness, folding endurance, Journal of advanced research. 1057-1059.
moisture content. The data showed that the patch 3. Patel, R.P., et al., 2009. Formulation and
formulation have been affected by types of polymer evaluation of transdermal patch of Acelofenac.
and concentration of polymer. Effect of penetration International journal of drug delivery .41-51.
enhancer like oleic acid and Dibutyl pthalate have 4. Cherukuri, S., Batchu, R., 2018. Formulation and
been checked on in-vitro permeation of drug. These evaluation of transdermal patch of topirate
studies indicated that as the concentration of .International journal of pharmaceutical
penetration enhancer increased drug permeation investigation. 10-17.
was increased. The finding of this result revealed 5. Ramadan,E., Borg, G.M., Saleh, N.M., 2018.
that the problems of febuxostat on oral Design and in vivo pharmacokinetic study of a
administration like dissolution rate limited newly developed lamivudine transdermal patch.
absorption and gastric side effects can be overcome Future journal of pharmaceutical sciences.166-
by applying febuxostat topically in the form of 174.
transdermal patch, and concluded that sodium
alginate with Dibutyl phthalate shows good result.

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FORMULATION AND EVALUATION OF FEBUXOSTAT AND DICLOFENAC SODIUM EMULGEL

FOR THE MANAGEMENT OF GOUT
Nargis Khan*, Arti Majumdar, Neelesh Malviya
Smriti College of Pharmaceutical Education, Indore - 452010, Madhya Pradesh, India
[email protected]

ABSTRACT
Emulgels have been emerged as a promising drug delivery system for the delivery of hydrophobic drugs. Emulgels
provide potential opportunity to deliver poorly water soluble drugs through gellified system.When gels and and
emulsions are used in combine form, it results in the formation of emulgel. Emulgels are emulsions, either of the
oil-in-water or water-in-oil type,which are gelled by mixing with a gelling agent. Also, emulgels provides benefits
and possess the advantages of both gel and emulsion. Therefore, emulgels have been recently used as vehicles
for the delivery of drugs through skin.The aim of the present work was to develop an emulgel formulation,
containing Febuxostat ,anti-gout drug and Diclofenac Sodium ,a NSAID with the aim to enhance the penetration
and improve systemic availability of the selected drugs.The study also aims to minimize the severe gastric distress
of the drugs by oral route.Emulgel was prepared by using carbopol 934 as a gelling agent.Mentha oil and clove oil
were used as penetration enhancers.The emulsion was prepared and incorporated into the gel base.The
prepared formulation was evaluated for physical appearance,rheological studies,spreadability studies and
swelling index.Skin irritancy study,in vitro drug release,drug content and stability studies were also examined.
Keywords: Emulgel, gout, Febuxostat, Diclofenac sodium

Introduction Materials and methods

Emulgels are emulsions, either of the oil-in-water or Materials
water –in-oil type, which are gelled by mixing with Febuxostat was gifted by Alembic Pharmaceutical
with a gelling agent.Emulsified gel is stable one and Pvt. Ltd. Vadodara Gujarat, India. And diclofenac
better vehicle for for the hydrophobic or poorly sodium gifted by sun pharmaceuticals Pvt. Ltd
water soluble drugs [1]. Dewas M.P. India. Carbopol 934 was obtained by
Loba chemicals Pvt. Ltd. Mumbai India. Span 20,
Arthritis Tween 20 obtained by Loba chemicals Pvt. Ltd.
Arthritis is the swelling and tenderness of one or Mumbai ,India. All other solvent and chemicals use
more of your joints. The main symptoms of arthritis during preparation of formulation was of analytical
are joint pain and stiffness, which typically worsen grade.
with age. The most common types of arthritis are
osteoarthritis and rheumatoid arthritis. Method
Different formulations were prepared by using
Types of arthritis: varying amount of gelling agent.The gel phase was
Ankylosing spondylitis, Gout, Joint infections, Juvenile prepared by dispersing carbopol 934 in water with
idiopathic arthritis, Osteoarthritis constant stirring ,ph was adjusted using tri ethanol
Psoriatic arthritis, Reactive arthritis, Rheumatoid arthritis,
amine(TEA).Oil phase of emulsion was prepared by
Septic arthritis, Thumb arthritis.[2] dissolving Span 20 in light liquid paraffin and
aqueous phase prepared by dissolving tween 20 in
Gout purified water.Methyl paraben dissolved in
Gout is a form of inflammatory arthritis that propylene glycol whereas drugs(febuxostat and
develop in some people who have high level of uric diclofenac sodium)were dissolved in ethanol,then
acid in blood .the acid can form needle like crystals both solutions were mixed with aqueous phase
in a joint and cause sudden ,severe episode of pain .Both the oily and aqueous phase were heated
tenderness, redness, warmth and swelling. Gout is cseparately upto 70-80:C and oily phase was added
the most prevalent form of inflammatory to aqueous phase with stirring.Obtained emulsion
arthritis.[3] was then incorporated into gel by gentle stirring to
form emulgel.

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Table 1: Composition of emulgel batche

S.No. Ingredients E1 E2 E3
1 Febuxostat 80mg 80mg 80mg
2 Diclofenac sodium 100mg 100mg 100mg
3 Carbopol 934 1 2 3
4 Light Liquid paraffin 5.5 5.5 5.5
5 Tween 20 0.5 0.5 0.5
6 Span 20 1 1 1
7 Propylene glycol 5 5 5
8 Ethanol 2 2 2
9 Methyl paraben 0.03 0.03 0.03
10 Water q.s. q.s. q.s

Results and discussion

Table 2: Evaluation of emulgel
Formulation code pH Viscosity Drug content(%) Spreadability Swelling index(%)
(cps) (g.cm/s)
E1 6.8 785 68.6 23.5 -
E2 6.6 1022 60.4 27.2 -
E3 7.0 1236 85.4 28.5 3.3

Conclusion References
Emulgel formulations were developed and 1. Kumar,L,Verma,R.,2014.In vitro evaluation
evaluated successfully and concluded that carbopol of topical gel prepared by natural
934 with 2% concentration showed good gelling polymer.International journal of drug
property.It is also concluded from results that delivery,58-63.
formulation batches showed acceptable physical 2. Roddy,E.,Doherty,M.,2010.Epidemiology of
property.Hence, emulgels are suitable drug delivery gout –A review arthritis research and
system for poorly water drugs for transdermal drug therapy,50-55.
delivery. 3. Ragab, G., Elshahalay, M., Thomas,B., 2017.
A Review. Journal of Advanced research,
1057-1059

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FORMULATION AND EVALUATION OF ENTERIC COATED TABLET OF TENOFOVIR

ALAFENAMIDE FUMARATE FOR THE TREATMENT OF HIV-1
Priyanshi sahu*, Arti Majumdar, Neelesh Malviya
Smriti College of Pharmaceutical Education, Indore (M.P.)
[email protected]

ABSTRACT
In the present research, Enteric coated tablet are solid dosage form which are designed to bypass the stomach
and release the drug in small intestine. Enteric coated work by presenting a coated surface that is stable at the
highly acidic pH found in stomach . Tenofovir alafenamide is a nucleotide reverse transcriptage inhibitor and used
in the treatment of HIV infection and chronic hepatitis B.coated tablet of tenofovir alafenamide fumarate were
prepared by direct compression method using mannitol as diluents, crosscarmellose sodium as disintegrating
agents, magnesium stearate and talc was used as glidant and lubricants respectively . Material used for enteric
coating include enteric coating polymer CAP and the present research describes enteric coating,their ideal
property ,benefits and limitation various polymer used , their chemical structure, machenism , method of
manufacturing. Prepared formulation were evaluated by the solubility studies, Fourier transforms infrared
spectroscopy, melting point , dissolution , DSC, And drug content .This research work shows prevention of drug
from acidic environment which improves bioavailability of drug and hide bitter taste of drug.
Keyword: Tenofovir alafenamide fumarate, Enteric coating, direct compression , cellulose acetate phthalate.

Introduction biconvex round shape die and punches . One batch

A tablet dosage form comprising a mixture of active of fourty tablets wereprepared 6, 7. Detailed
substances and excipients, usually in powder form, composition of azythromycin core tablets is given in
pressed or compacted from a powder into a solid Table 1
dose.[1] The excipients can include is a
pharmaceutical glidants (flow aids), diluents, Preparation of tablets
binders or granulating agents and lubricants to An ideal mixture of granules was directly punched
ensure efficient tableting; disintegrants to promote into tablets weighing about 150 mg containing 25
tablet break-up in the digestive tract;[2] sweeteners mg of tenofovir alafenamide fumarate, using tablet
or flavours to enhance taste; and pigments to make compression machine.
the tablets visually attractive.The main objectives of
the present study was To formulate and evaluate Preparation of enteric coating solution
enteric coated tablets tenofovir alafenamide The enteric coating solution was prepared by simple
fumarate by direct compression method,To solution method. It was prepared cellulose acetate
overcome the drug degradation by the gastric phthalate as an enteric polymer, PEG as plasticizer
enzymes as well as the acidic environment of the and acetone was used as solvent.
stomach[2]
Results and discussion
Material and method The prepared Tenofovir alafenamide fumarate
Materials: Tenofovir alafenamide fumarate was powder for tabletting was prepared by direct
provided by cipla research and development compression method and evaluated
Mumbai. Lactose (Smriti college of pharmaceutical
education )Magnesium stearate (Smriti college of Conclusion
pharmaceutical education), Talc, Cellulose acetate An attempt was made in this research work to
phthalate formulate an oral enteric coating tablet of tenofovir
alafenamide fumarate and evaluate it. In this
Preparation of core tablets present research work, both the polymer has been
The core tablets were prepared by direct used as an enteric coating polymer, with the best
compression method. All the ingredients were formulation. Cellulose acetate phthalate have been
mixed and passed through sieve no. 60(250 used with the best formulation. From the
microns) to get uniformally distributed and uniform dissolution studies it was observed that, the enteric
sized particles.Then after sieving process the coated both polymer was intact for 2 hours in pH
mixture is put for the compression on 8 station 1.2 buffer.
tablet punching machine using 10 mm diameter
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ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

Therefore the study proved that the tenofovir pantoprazole as an enteric coated tablet may solve
alafenamide fumarate enteric coated tablets can be the stability problem of drug in the stomach and
used for treatment of HIV-1. Hence, formulation of release the drug in the intestine.

Table.1.Composition of tenofovir alafenamide enteric coated tablets

Composition F1(mg) F2(mg)
tenofovir alafenamide fumarate, 25 25
Lactose 50 60
Cross povidone 5 4
Mannitol 50 50
Magnesium stearate 10 4
Talc 10 7
Total weight 150 150

Table.2.Composition of coating solution

Ingredients Quantity (%)
Cellulose acetate phthalate 6.0
PEG 1.5
Acetone 59.4

Table.3.Pre compression parameters of Tenofovir alafnamide fumarate

Formulation Bulk density Tapped Carr’s Index Angle of repose
Code (gm/mL) Density (gm/mL) (%) (Ɵ )
F1 0.357±0.03 0.384±0.05 7.03±0.09 28.31±0.26

F2 0.312±0.04 0.335±0.02 6.86±0.15 27.20±0.14

Table.4.Post compression parameters of Tenofovir alafenamide fumarate core tablets

Formulation Hardness (Kg/cm2) Friability Weight Drug content Disintegration
Code (%) Variation (mg) (%) Time (min)
F1 5.80 ± 0.12 0.69 ± 0.015 199 ± 0.12 96.28 ± 0.15 10.6± 0.62
F2 5.56 ± 0.24 0.51 ± 0.017 206 ± 0.24 97.62 ± 0.27 8.26± 0.56

References 5. Chanchal M, Anil G, Mukesh S, Asha R,

1. Anroop N, Rachna G, Rachna K, Shery J, Pantoprazole and its enteric coating
Mahesh A, Formulation and Evaluation of polymer concentration for stable coating in
Enteric Coated Tablets of Proton Pump acid media in stomach, International
Inhibitor, Journal of Basic and Clinical Journal of Pharmaceutical and Clinical
Pharmacy, 1(4), 2010, 45-49 Research, 3(2), 2011, 45-47.
4. 2.Bozdag S, Çalis S, Sumnu M, Formulation 6. Liberman H, Lachman L, The Theory and
and stability evaluation of enteric-coated Practice of Industrial Pharmacy. 3rd Ed.
omeprazole formulations. S.T.P. Pharma Bombay: Verghese Publication House,
Sciences, 9 (4), 1999, 321-327. 1991, 171-193.

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FORMULATION AND EVALUATION OF ORLISTAT LOADED MICROSPONGES FOR THE

TREATMENT OF OBESITY
Rahul Vishvakarma*, Arti Majumdar, Neelesh Malviya
Smriti College of Pharmaceutical Education, Indore - 452010, Madhya Pradesh, India
[email protected]

ABSTRACT
The purpose of this study was to design novel drug delivery system containing orlistat micro sponges.
Microsponges containing orlistatand EudragitRS 100 prepared by quasi emulsion solvent diffusion method. The
compatibility of the drug with formulation component was established by (FTIR) Fourier Transform infra-Red
Spectroscopy. The formulations were prepared by gradually increases Drug: polymer ratio. The particle size
(microscopy), Surface Morphology and structure examination (SEM) Production yield, Loading Efficiency and in
vitro drug release studied of micro sponges were examined. The drug orlistat disperse in GIT for better
therapeutic effect as micro sponges disperse freely in GIT. To improve absorption of orlistat so as to enhance
bioavailability, micro sponges is used as delivery systems which show better absorption and bioavailability then
other dosage form of orlistat.Microsponges’ drug delivery technology landscape has become highly and rapidly
evolving. Microsponges are safe biologically and unique advantage programmable release. . Microsponges are
profitable drug delivery system. They are allowing for novel product form.
Keywords: Microsponges, Enhance bioavailability, orlistat, Eudragit RS-100

Introduction was dissolved in 5 ml of ethyl alcohol. Orlistat was

Microsponges added and mixed well until it gets dissolved
Microsponges are polymeric delivery systems completely and to which tri-ethyl citrate 2 ml was
composed of porous microspheres. They are tiny added to facilitate plasticity (used as Plasticizer).
sponge-like spherical particles with a large porous External phase: Accurately weighed PVA is added to
surface. Microsponges are porous, polymeric distilled water to form clear solution. Than internal
microspheres that are used mostly for topical use phase was added in external phase. The mixture
and have recently been used for oral was stirred 500 RPM for 2 hours, at Room Temp.
1,2,3
administration. The formed Microsponge were filtered and washed
Obesity with distilled water than dried at room temperature
According to WHO - Overweight and obesity are for 24 hour. All formulation of orlistat loaded
defined as abnormal or excessive fat accumulation microsponges of different drug: polymer ratios were
that presents a risk to health. A crude population prepared.
measure of obesity is the body mass index (BMI), a
person's weight (in kilograms) divided by the square Results and discussion
of his or her height (in meters).it is a pathological Evaluation of prepared orlistat loaded
condition in which excess body fat accumulated, microsponges
leading adverse effects on health and life Physical appearance
4
expectancy. The orlistat loaded Microsponge particles are fairly
pure white were obtained by quasi-emulsion
Materials and methods solvent diffusion method with good flow properties
Materials than as compared with pure drug.
Orlistat was gifted by Sun Pharmaceutical Pvt. Ltd. Particle Size Analysis
Dewas Madhya Pradesh India. Eudragit RS-100 was Particle size of microsponge was determined using
purchased by Evonic Degussa Pvt. Ltd. Mumbai optical microscope. A few quantity microsponges
India. Triethyl were determined of some batch. The values were
Citrate purchased by Himedia laboratories Pvt. Ltd, given in table. The all formulation of mean
India. And all solvent and chemical use during particlesize show in (Table-2)
formulationwas of analytical grade.
Determination of Percentage Yield
Method Percentage yield of the prepared orlistat loaded
Orlistat Microsponges were prepared by quasi microsponges was in the range of 67.33. The
emulsion solvent diffusion method. In this method, formulation-2 prepared with drug polymer ratio
internal phase: Polymer Eudragit RS 100 (100 mg) 3:1 Show very good production yield (Table 2)
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International Journal of
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ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

Determination of loading efficiency microsponges was found in the range of71.28.The

The Drug content of different microsponge best loading efficiency was found in the
formulationestimate by Ultraviolet spectroscopic formulation-2. The reduction of drug loading
method. Drug entrapment depended on the right efficiency show in (Table 2)
molecular association of the drug polymer ratio. The
drug loading efficiency of orlistat loaded

Fig 1: Prepared Microsponge

Table: 2 Production yield, particle size and drug entrapment of prepared microsponges
Formulation code Production Yield(%) Particle size(μm) Drug Entrapment (%)
F-1 65.20 43.50 67.55
F-2 67.33 36.00 71.28
F-3 78.65 49.70 75.69

Conclusions Pharmaceutical drug delivery Technology,16(4)

Orlistat is a poorly soluble drug with short half -life, 367-376
To improve absorption of orlistat so as to enhance 2. Osmani, R.A., Aloorkar, N.H., Kulkarni, A.S.,
bioavailability, microsponges is used as delivery Kulkarni, P.K., Hani, U., Thirumaleshwar, S.
system which show better absorption and Bhosale, R.R., 2015. Novel cream containing
bioavailability then other dosage form of microsponges of anti-acne agent: formulation
orlistat.Orlistat is formulated as Microsponges by development and evaluation, Current Drug
Quasi emulsion solvent diffusion method using Delivery, 12(5), 504-516.
polymers Eudragit RS 100 and PVA. This method 3. Jelvehgari, M., Siahi-Shadbad, MR., Azarmi, S.,
found to be easy and rapid method. Martin, G.P., Nokhodchi, A., 2006. The
microsponge delivery system of benzoyl
References peroxide: preparation, characterization and
1. Sharma, R., Pathak, K., 2011. Polymeric Nano- release studies. International Journal of
sponges as an alternative carrier for improved Pharmaceutics, 124–132.
retention of econazole nitrate onto the skin 4. Rang, H.P., Dale, M.M., Ritter, J.M., Moore P.K.,
through topical hydrogel formulation. 2005. A text book of pharmacology, fifth
edition, published by Elsevier. 394-404

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FORMULATION AND EVALUATION OF SUBLINGUAL TABLET OF TENOFOVIR ALAFENAMIDE

FUMERATE USING SOLID DISPERSION TECHNIQUE FOR THE TREATMENT OF HIV I
Urvashi Jain*, Arti Majumdar, Neelesh Malviya
Smriti College of Pharmaceutical Education, Indore - 452010, Madhya Pradesh, India
[email protected]

ABSTRACT
The objective of this research is to prepare sublingual tablets of Tenofovir alafenamide fumerate with the aim to
increase its solubility and thus improving its oral bioavailability. Materials and Methods: Pure drug, polymer, and
other excipients were characterized by infrared spectroscopy and differential scanning calorimetry. The solid
dispersion of Tenofovir alafenamide fumerate was prepared using betacyclodextrin and PEG. The solubility of
Tenofovir alafenamide fumerate was increased by formulating as solid dispersion by kneading techniques. The
prepared solid dispersion was further used in the formulation of sublingual tablets. Sublingual tablets were
formulated using superdisintegrants such as crospovidone and sodium starch glycolate. Results: In a total no. of 3
batches of formulations from F1 to F3 were prepared by varying superdisintegrants concentration. Results of
evaluation parameters revealed that formulation F3 containing-4% sodium starch glycolate found to be most
optimized formulation in terms of flow properties, hardness, quick wetting, and disintegration time. Conclusion:
All the three formulations were successfully prepared and evaluated. However, results of parameters evaluated
conclude that among all prepared formulations, F3 was observed as most optimized formulation.
Keywords: Tenofovir alafenamide fumerate ,sublingual, Crospovidone, sodium starch glycolate.

Introduction from Loba chemicals. Microcrystalline from loba

Oral drug delivery system achieved great success chemicals. Talc, sucrose, mannitol, magnesium
and very common route of drug administration. The stearate (Loba chemicals).
reason behind this popularity may be by its "ease of
administration" but one factor may affect its Methods
popularity and use of administration[1], i.e., Preparation of solid dispersion by kneading
extensive first-pass metabolism. The drug degrades method
by first-pass metabolism results in short duration of In this method, drug and polymer were taken to
therapeutic action and low systemic bioavailability. reduce the size of the mixture. Distilled water was
In Sublingual route, a drug is administered by the added in the physical mixture, and slurry mass was
mouth in such way that the drug is rapidly absorbed formed which dried in hot air oven at 45°C[2]. The
by the blood vessels rather than absorbing through dried product was passed through sieve no. 36.
gastrointestinal tract. This category of drugs
releases their drug content directly into mucosal Preparation of sublingual tablets of Tenofovir
lining of the mouth beneath the tongue. alafenamide fumerate
Tenofovir alafenamide is a nucleotide reverse Formulation, all the three batches of sublingual
transcriptase inhibitor and used in the treatment of tablets, was prepared by changing the
HIV infection. Tenofovir alafenamide is poorly concentration of sodium starch glycolate and
water-soluble drug. Its having aqueous solubility <I crospovidone. All the ingredients except talc was
mg/ml. Tenofovir alafenamide comes under BCS weighed and sieved individually through #44 mesh
Class-II drug. Tenofovir alafenamide undergoes size[3]. After sieving all the ingredients were mixed
extensive hepatic first-pass metabolism. It is having in geometrical order. Talc was weighed and passed
a dose ranging from 10mg and 25mg. The present through the same sieve and was added to the
research focused on the preparation and evaluation formulation and mixed for 2 min to get free-flowing
of sublingual tablets of TAF using powder and at last, the blend was compressed into
superdisintegrants. the tablet and evaluated. [Table 1]

Materials Results and discussion

Tenofovir alafenamide fumarate was obtained as a The prepared Tenofovir alafenamide fumarate
gift sample from Cipla R&D, Mumbai. Sodium starch sublingual tablet was prepared by direct
glycolate and lactose were obtained from HiMedia compression method and evaluated.
Laboratories, Mumbai. Crospovidone was obtained

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Table.1: Composition of tenofovir alafenamide fumerate sublingual tablets.

Ingredients Fl F2 F3
tenofovir 25 mg 25 mg 25 mg
Sodium starch - 5mg 10mg
glycolate
Crospovidone 5 mg 10 mg -
Lactose 50 mg 50mg 50mg
Sucrose 15 mg 15 mg 15 mg
MCC 50 mg 50 mg 50 mg
Talc 10 mg 5 mg 5 mg

Conclusion and super disintegrates increased solubility and in

Sublingual tablets of Tenofovir alafenamide vitro drug release of Tenofovir alafenamide
fumerate were prepared, and solubility of fumerate within 2min. Preparing sublingual
Tenofovir alafenamide fumerate was found to be formulation (tablets) will increase the
increased using solid dispersion prepared by bioavailability of Tenofovir alafenamide fumerate
kneading techniques. From the present study, it and prevent them from extensive first- pass effect.
can be concluded that the use of solid dispersion

Table.2: Pre compression parameters of Tenofovir alafnamide fumerate

Pre-compression parameters Fl F2 F3

Bulk density(g/ml) 0.612 0.601 0.608

Tapped density(g/m1) 0.716 0.699 0.724
Angle of repose(degree) 25.8 22.3 24.7
Compressibility index (%) 17.18 16.06 13.01
Hausner's ratio 1.2 1.19 1.14

Table.3: Post compression parameters of Tenofovir alafenamide fumerate sublingual tablets:

Post-compression parameters Fl F2 F3

Diameter (mm) 10.3 10.3 10.7

Hardness (kg/cm2)) 3 3.4 3.6
Thickness (mm) 1.93 1.95 1.9
Friability(%) 0.69 0.54 0.23
Weight variation (mg) 148±0.8 148±0.3 I 150±0.99
Wetting time(sec.) 90 39 30
Disintegration time(min.) 1 1.5 2
Content uniformity(%) 99.12 99.87 99.54

References 3. Richman MD, Fox D. Shangraw RE'.

1. Liberman H, Lachman L, The Theory and Preparation and stability of
Practice of Industrial Pharmacy. 3rd Ed. glyceryltrinitrate sublingual tablets
Bombay: Verghese Publication House, prepared by direct compression. J Pharm
1991, 171-193. Sci 1965;54:447-51.
2. Lolisson T. Duchene, cyclodextrins and
their pharmaceutical application. Int J
Pharm 2007; 329:1-11

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FORMULATION DEVELOPMENT AND EVALUATION OF NANO LIPPOIDAL CARRIER FOR THE

TOPICAL DELIVERY OF CISPLATIN
Priya Mourya, Arti J Majumdar, Neeleshmalviya
Smriti College of Pharmaceutical Education, Indore, M.P. (India)
[email protected]

ABSTRACT
Nano structured lipid carriers are drug delivery system composed of solid as well as liquid lipids. In the present
research work, NLCs were prepared by solvent diffusion method using different proportions of solid lipid
(stearic acid) and liquid lipid (oleic acid). Prepared NLCs were evaluated for different parameters like particle
size, surface morphology, entrapment efficiency, % drug loading and % cumulative drug release. Mean particle
size and entrapment efficiency was found to be 343 nm and 68% respectively.

Introduction Mumbai. Ethanol, acetone and other chemicals

Nanotechnology has a great potential for the were analytical reagent grade.
drug delivery system. Lipid-based Nano
particulate drug delivery systems have been Method of Preparation
proved as emerging carriers for cytotoxic drugs Cisplatin loaded NLCs were prepared by solvent
because of their potential to increase the diffusion method in an aqueous system as
bioavailability and solubility of poorly water- reported earlier with slight modification.
soluble drugs. The lipids which are used for the Formulation were optimized by using Box-Behnken
preparation of lipid NPs are usually design expertBriefly, selected lipid (SA and OA)
biodegradable lipids having low toxicity. The with varying content and drug were dissolved
major advantage of nanostructured lipid carrier completely in a mixture of acetone and ethanol
as drug delivery system is its ability to (1:1, v/v) in water bath at 70°C. This lipid solution
accommodate large quantities of drugs as a was poured into 100 ml of an aqueous phase
result of formation of a less ordered lipid matrix containing 1% SLS under continuous mechanical
with many defaults. agitation (Remi Instruments, Mumbai, India) with
5000 rpm at room temperature (25–28 ◦C) for 3
Materials and Methods min. The pH value of the acidic aqueous phase was
Materials adjusted to 1.20 by addition of 0.1 M hydrochloric
Stearic acid (Loba Chemie, Mumbai, India) was acid to form aggregation of nanoparticles. The
used as solid lipid, Oleic acid (Loba Chemie, nanoparticles were then centrifuged at 20000 rpm
Mumbai, India) was used as liquid lipid. Cisplatin for 30 min, to get the precipitate of
was kindly donated by Intas Pharmaceutical Ltd., nanostructuered carriers. The precipitate was
Ahmedabad, (India). The surfactant, sodium lauryl collected.
sulfate, was provided byMerck Specialties Pvt. Ltd.,

Table 1: Concentration of independent variables from batch NLC-01 to NLC-08

Independent Formulation code
variable NLC-01 NLC-02 NLC-03 NLC-04 NLC-05 NLC-06 NLC-07 NLC-08
X1 (%) 75 100 75 50 100 75 50 75
X2 (%) 25 25 0 25 50 25 0 0
X3 (mg) 7.5 5 5 10 7.5 7.5 7.5 10

Table 2: Concentration of independent variables from batch NLC-09 to NLC-15

Independent Formulation code
Variable NLC-09 NLC-10 NLC-11 NLC-12 NLC-13 NLC-14 NLC-15
X1 (%) 75 100 50 75 100 75 50
X2 (%) 50 0 50 50 25 25 25
X3 (mg) 5 7.5 7.5 10 10 7.5 5

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Table 3: Composition of predicted optimized formulation and responses obtained

Independent variable Response obtained
Stearic Oleic Cisplatin Particle Drug % cumulative drug release(Y3-Y9)
acid acid size(nm) entrapment
1 hr 2 hr 4hr 8hr 12hr 24 hr
Y1 (%)Y2
72.34 % 29.36 8.2 mg 343 68% 4.94 12.26 18.46 25.93 42.88 57.37
%

80
% Drug release

60
Predicted drug
40 release
Observed drug
20
release
0
0 5 10 Time 15
(hours) 20 25 30

Fig 1: % Cumulative drug release profile of predicted and observed formulation

Result and Discussion The percentage entrapment efficiency was

Particle size and poly dispersibility index:Mean calculated by following formula: EE = (Wα– Ws) /
particle size and PDI were determined using Wα X 100 and found to be 68.72%
nanotrac wave and found to be 343 nm.
(Microtrac; USA) using water as a dispersion Surface morphology
medium. Surface morphology was determined by using
optical microscope.
Entrapment efficiency

Data Value
MI(nm) 343.0
MN(nm) 263.9
MA(nm) 315.0
CS 19.06
SD 93.09
PDI 0.598
Mz 337.8
Si 96.64
Fig.2: Particle size distribution of optimized batch of Cisplatin NLCs Ski 156.3
Kg 1076

Fig.3: Microscopic image of optimized batch of Cisplatin NLCs

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Conclusion concentration of liquid lipids on drug

In the summation, it can be concluded that the release, Journal of Drug Delivery and
NLC of cisplatin developed in the present studies Therapeutics 2017; 7(7): 26-28
showed consistent drug release for a period of 24 2. Jenning V, Thünemann AF, Gohla SH.
hrs and was superior to the simple SLN in terms of (2000) Characterisation of a novel solid
% drug release. NLC of cisplatin could thus be lipid nanoparticle carrier system based on
developed using oleic acid as liquid lipid and can binary mixtures of liquid and solid lipids.
be used in the treatment of cancer effectively. Int J Pharm: 199: 167-77
3. HuFQ,JiangSP,DuYZ,etal.(2005).Preparat
References ionandcharacterizationofstearicacidnan
1. Majumdar A, Dubey N, Formulation of ostructuredlipidcarriersbysolventdiffusi
paclitaxel loaded nanostructured lipid onmethodinanaqueoussystem.ColloidsS
carriers to study the effect of urfBBiointerfaces 45:167–73.

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DEVELOPMENT & EVALUATION OF ANTI ACNE CREAM USING EXTRACTS OF VITEX

NEGUNDO AND HIBISCUS ROSA-SINENSIS
Urvashi Sharma1, Ayushi Sharma1, Sapna Malviya2, Neetesh K Jain1
1. Oriental University, Gate No.1, Sanwer Road, Jakhya, Opposite Revati Range, Indore, M.P.
(India)
2. Modern Institute of Pharmaceutical Sciences, Indore, M.P. (India)
[email protected]

ABSTRACT
Acne vulgaris is the most common chronic skin disease of the world. The bacteria responsible for acne are
Staphylococcus aureus. So many synthetic products are available in the market for acne treatment including
antibiotics, but serious side effects arises due to the long-term use of synthetically prepared anti-acne
preparations. Bacterial resistance is the major problem that occurs due to the irrational use of antibiotics, in
addition to this skin problem, such as erythema, allergy, sunburn and melanin pigmentation. As from ancient
times, natural plant substances have been shown to be promising candidates for acne treatment without side
effects. Therefore in the present study, the anti acne cream formulation has been prepared using Vitex
negundo (leaves), Hibiscus rosa-sinensis (flower) and Tea Tree Oil (Melaleuca alternifoli). The prepared
formulation was evaluated on the basis of greasiness, spreadability, homogeneity, skin irritancy, viscosity, pH,
emolliency and stability. The antibacterial study was also performed using a well diffusion technique and
results showed that formulation possess sufficient anti bacterial activity. This showed that the optimized
formulation has anti-acne properties.
Keywords: Anti-acne, Staphylococcus aureus, Vitex negundo, Hibiscus rosa-sinensis, Melaleuca alternifolia.

Introduction Development of acne occurs due to blockage of

Acne vulgaris is the formation of comedones, follicles, hyper keratinization and the formation of
papules, pustules, nodules and cysts due to the keratin and sebum (microcomedo). Increase in
obstruction and inflammation of the pilosebaceous production of androgen, increases the size of
units (hair follicles and their sebaceous glands). sebaceous glands and hence shows increase in the
Acne can also happen due to non-inflammatory production of sebum. The microcomedo can be
lesions, inflammatory lesions or a mixture of both, expanded to form an open blackhead or a closed
which mainly affect the face but can also seep into comedo. Comedones occur due to the obstruction
the back and chest. The most common responsible of the sebaceous glands with sebum, natural oil
bacteria for acne are Staphylococcus aureus, but and dead skin cells. The natural commensal
some studies reported that Propionibacterium bacterium Propionibacterium acnes can cause
acne has also been isolated from the acne patient inflammation and inflammatory lesions such as
and hence found to be responsible. pustules or nodules and papules infected in the
dermis around the microcomedo or comedone,
Etiology which cause redness, scarring or
[1]
hyperpigmentation .
[1]
Table 1: Factors Responsible for Acne Development
Medications Drugs that causes acne are Phenytoin, Isoniazid, Phenobarbital, Lithium, Ethionamide, Steroids,
Azathioprine, Quinine and Rifampin
Hormonal Menstrual cycles and puberty may causes acne because of increase in androgens level and increased
sebum production
Psychological Studies shows that increased stress levels are associated with increased acne severity
Genetic There is a tendency for acne to run in families, and specific genetic mutations may increase your risk of
developing acne
Infectious P. acnes are anaerobic bacterium species that mainly causes acne. However Staphylococcus aureus has
also been discovered to play an important role
Diet Certain dietary factors, including skim milk and carbohydrate-rich foods such as bread, bagels and chips
may worsen acne. Chocolate has long been suspected of making acne worse

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Various available treatments include drugs like Phytochemical screening

benzoyl peroxide, clindamycin, salicylic acid, Detection of Saponin
adapalene etc. But because of their serious side Foam Test: Small quantity of extract was shaken
effects such as increased resistance towards vigorously with 2ml of water for 15min in a
bacteria, dryness, skin irritation, burning etc. graduated cylinder. If foam production persists for
[2] [6]
herbal remedies is replacing them . 10 min, it indicated the presence of saponins .
Among the alternate system of medicine, the Detection of Carbohydrate
herbal topical therapeutic agents are gaining more Benedict’s test: Extract was boiled with small
attention because of its convenience and lesser amount of benedict solution (alkaline solution of
side effects. Vitex negundo, commonly known as cupric-citrate complex), if color changes from blue
Nirgundi and also known as Chinese chaste tree to yellow and finally to red, it indicated the
[6]
and horseshoe vitex, is native to tropical Eastern presence of carbohydrate .
and Southern Africa and Asia. Studies have Detection of Tannin
reported that fruits, flowers and leaves posses Galactic Test: 1% gelatin solution containing
antibacterial activity found against E. coli, P. sodium chloride was added to the extract, white
[7]
aeruginosa and S. aureus. precipitation indicated the presence of tannins .
Hibiscus rosa-sinensis known colloquially as china Detection of Flavonoids
rose is a bushy, evergreen shrub or small tree Aluminum Chloride Test: A small quantity of
bearing flower. Reports have confirmed the extract was taken and heated with ethyl acetate
presence of flavonoids, tannins and triterpenoids (10ml) on water bath for 3minutes. The mixture
responsible for its antibacterial effects. Tea Tree was filtered and used for test. The filtrates were
oil has also been added for its additional shaken with 1 ml of 1% aluminum chloride
antimicrobial properties. Thus, in the present solution. The light yellow color indicated the
study anti acne cream is formulated using extracts presence of flavonoid. On addition of dilute NaOH
[3]
of Vitex negundo and Hibiscus rosa-sinensis . and HCl, the yellow solution turned to colorless
[8]
confirming the presence of flavonoids .
Materials and method Detection of Alkaloids
Collection and authentication Mayer’s Test: To 2-3 ml of extract, 2 ml of
The leaves of Vitex negundo, flowers of Hibiscus concentrated HCl was added followed by adding
Rosa sinesis and tea tree oil were purchased from few drops of Mayer’s reagent by side of the test
local market and authenticated by Dr. Narendra tube. Formation of white yellowish precipitate
[6]
Vyas, Department of Pharmacognosy, Modern indicates the existence of alkaloids .
Institute of Pharmaceutical Sciences, Indore
[9]
(HERB/MIPS/2018/0031). All the other ingredients Formulation of herbal anti acne cream
were of analytical grades. The formulation was prepared as water in oil
emulsion using extracts of Vitex Negundo leaves &
Prepration of extracts Hibiscus Rosa Sinensis flower. The oil soluble
The leaves of Vitex negundo and flowers of Rosa components stearic acid, tea tree oil and others
sinensis were air dried and powder was used for such as cetyl alcohol, lanolin wax liquid paraffin
extraction. and vitamin E were mixed to form oil phase (Part
For Vitex negundo leaves extract A). The phase was prepared by dissolving the
50 gm of dried powder of leaves was taken and components in the beaker on water bath at a
used for extraction using soxhlet apparatus with temperature of 80°C. The water soluble
o
500 ml of ethanol at 40-50 C. The ethanolic extract components glycerin, triethanolamine and extracts
was collected and evaporated to get dried extract in different proportions were dissolved in the
[4]
. purified water to form Part B by heating on water
For Rosa sinensis extract bath at same temperature up to 80ºC. Water
50gm of dried powder was taken and macerated phase (Part B) was then mixed in oil phase with
with 250 ml of cold water in a conical flask for 24 h constant stirring until cream was formed.
and then filtered off using sterile Whatman No. 1 Preservative (methyl paraben) was then added
filter paper. Then the filtrate was collected and with continuous trituration. The composition of
[5]
evaporated to get dried powder . anti-acne cream is shown in Table 2.
.

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Table 2: Composition of Anti Acne Cream (100 gm)

SNO. INGERDIENTS F1 (%) F2 (%)
1 Vitex negundo 1% 2%
2 Hibiscus Rosa sinesis 2% 1%
3 Tea Tree oil 2% 2%
4 Stearic acid 10% 10%
5 Cetyl alcohol 4% 4%
6 Lanolin wax 4% 4%
7 Liquid paraffin 5% 5%
8 Glycerin 5% 5%
9 Methyl paraben 0.05% 0.05%
10 Thiethanolamine 0.05% 0.05%
11 Vitamin E 0.5% 0.5%
12 Purified water Up to 100% Up to 100%
[10,11]
Evaluation of formulations was added to the pan and the top plate was
The following parameters were assessed to subjected to pull with the help of string attached
evaluate the prepared anti acne cream: to the hook. The time in which the upper glass
Physical appearance slide moves over the lower plate to cover a
The physical appearance of the formulation was distance of 10 cm is noted.
checked visually and included following: The spreadability (S) can be calculated using the
Color - The color of the formulations was checked formula
against white background. S=M×L/T
Odor- The odor of the cream was checked by Where, S= Spreadability, M = Weight in the pan
mixing the formulation in water and taking the (tied to the upper slide), L = Length glass slide, T =
smell. Time (in sec.) taken to separate the slides.
Greasiness- The greasiness of the formulation was The determinations were carried out in triplicate
assessed by the application on to the skin. and the average of three readings was recorded.
Pearlescence - The pearlescent texture of Type of smear
formulation was checked visually. The type of film or smear formed on the skin after
Greasiness - The greasiness was assessed by application of cream was checked.
applying the formulation onto the skin. Emolliency
pH measurement Emolliency, slipperiness and amount of residue left
The pH of various formulations was determined by after the application of fixed amount of cream was
Digital pH meter. One gram of each formulation observed.
(cream) was dissolved in 100 ml of distilled water Skin Irritancy test
(i.e. 1% aqueous solution) and pH was measured. Area of 1sq.cm was marked on the left hand dorsal
The measurement of pH of each formulation was surface. The cream was applied to the specified
done three time and average values were area and time for occurrence of any sensitivity or
mentioned. reaction was noted. Development of irritancy,
Homogeneity erythema, and edema was checked if any for
Homogeneity and texture were tested by pressing regular intervals up to 24 hrs and reported.
a small amount of formulation between thumb Anti-bacterial Testing
and finger. Microorganism: The gram positive bacterial strain
Grittiness of Staphylococcus aureus was selected for study
The preparations were subjected to immediate and obtained from the Department of
skin feel by applying it on skin so as to test the Microbiology,Modern Laboratory Pvt Ltd. The test
presence of any gritty particles. organisms were further subculture at 37ºC for 24
Spreadability hours. The culture of bacteria were maintained in
The spreadability was determined by taking about their appropriated ager slant at 4ºC throughout
3gm sample and applying it between two glass the study and used as stock cultures.
slides. The slides were pressed together to obtain Well - diffusion Method
a film of uniform thickness by placing 1000 gm The nutrient media selected for study was Nutrient
weight for 5 minutes. Thereafter a weight (10gm) Agar (Hi media). The formulations were subjected

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to antibacterial activity using agar well diffusion of equidistance in each of the plates. The samples
method. Fucidin cream was used as standard. prepared with different concentration of
Plates were sterilized in hot air oven at 160ºC for 2 formulated creams (10 and 100mg/ml) were
hrs and were used for preparation of plates. The introduced into wells and plates were incubated at
bacterial suspension was spread uniformly on the 37ºCfor 24 hours. The antibacterial activity was
solid agar using cotton swabs and plates were evaluated by measuring the zone of inhibition (in
o
incubated at 37 C for 24 hrs for bacterial growth. A mm) and was expressed as Mean ± Standard Error
sterile borer of 8mm was then used to make wells Mean.

F1 F2
Figure No. 1 Antibacterial Activity of Anti-acne Formulations

Stability Study accelerated stability test showed that there were

The stability study was carried out by storing the no changes in the color of the cream.
anti acne cream in air tight container at three
different temperatures which are 8ºC, 27ºC and Discussion
40ºC for 2 month. The preparations were The present study was undertaken to develop
evaluated after prescribed duration for color, herbal formulation in the management of acne
homogeneity and pH. caused by bacterial infection. The extract of Vitex
negundo and Rosa sinesis leaves had earlier
Result scientifically proven for its antibacterial activity.
Phytochemical screening Preliminary phytochemical screening of ethanolic
The results of phytochemical screening of extracts extract of Vitex nigundo and hydroalcoholic extract
confirmed the presence of active constituents of Rosa sinesis showed the presence of
responsible for anti bacterial activity. constitutent’s flavonoids and tannins that are
presponsible gives anti bacterial activity. Herbal
Evaluation of preapred formulations cream has been developed containing extract of
The herbal anti-acne cream was prepared and Vitex nigundo and Rosa sinesis leaves. The
evaluated on various physicochemical parameters developed cream was evaluated using various
and the results are shown in table 4. Both the physicochemical parameters. The pH
preparations gave satisfactory results on all the measurement of the formulation ranges from 6.4
defined parameters. to 6.9, which lies in the normal pH range of the
human skin. Spreadability values showed that both
Stability Study the creams spread with an ease and the type of
Results concluded that Formulation 1 showed smear is non greasy. From the stability studies,
much greater anti bacterial effect, hence was formulations showed no changes in color,
chosen for stability study. After two months of appearance and homogeneity.
stability study, the tested physicochemical The results of antibacterial activity revealed that
parameters were maintained and results of study between the two prepared formulations
showed no change in appearance of cream during containing extract of Vitex nigundo and Rosa
the accelerated stability studies at temperatures sinesis leaves, F1 exhibited more significant
8°C, 27°C and 40°C for 8 weeks. The results of antibacterial activity when compared with
standard (Fucidin cream).

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Table 3: Phytochemical Screening of Vitex negundo, Hibiscus rosa-sinensis and Tea Tree Oil
Chemical Test Vitex negundo Hibiscus rosa-sinensis Tea Tree Oil
Saponins + - +
Carbohydrate + + -
Tannins + + +
Flavonoids + + +
Alkaloids - + +

Table 4: Physicochemical Evaluation of Formulated Anti-acne Cream

Parameters Results
Formulation 1 Formulation 2
Color Light brown Light brown
Odor Pleasant Pleasant
Pearlescence Present Present
pH 6.0+0.03 6.6+0.05
Homogeneity Smooth and consistent Smooth and consistent
Grittiness Non gritty Non gritty
Spreadability 4.03 3.28
(g-cm/sec)
Type of smear Non greasy Non greasy
Emolliency No residue left No residue left
Skin irritation Non irritating Non irritating

Table 5: Anti Bacterial Activity of Anti-acne Formulation

Concentration (mg/ml) Zone of Inhibition (mm)
F1 F2
10 4.83+0.75 3.15+1.54
100 15.12+1.02 14.95+0.23
Positive Control 16.08+0.17 15.78+0.61

Table 6: Stability Study of Formulation F1

Parameters Before Stability Study After Stability Study
8ºC 27ºC 40ºC
Color Light brown Light brown Light brown Light brown
Homogeneity Smooth and consistent Smooth and Smooth and Smooth and
consistent consistent consistent
pH 6.0+0.03 6.1+0.54 6.2+0.23 6.4+0.12

Conclusion So the study concluded that the prepared anti

Anti acne formulation that are being widely used acne cream is effective in treating acne vulgaris
are synthetic and are associated with many side and is safe for long term use.
effects such as microbial resistance etc. Moreover
allopathic drugs are also frequently used to treat Reference
acne vulgaris and results in adverse side effects. 1. Suva Manoj A, Patel Ankita M, Sharma Neeraj,
For this reason herbal remedies are considered as Bhattacharya Chandrayee, Mangi Ravi K: A
safe and their demand is increasing in global Brief Review on Acne Vulgaris:- Pathogenesis,
market. In the present study, the formulations are Diagnosis and Treatment. Research &
prepared with extracts of herbal plants i.e. Vitex Reviews: Journal of Pharmacology 2014;
negundo and Rosa sinesis and evaluated at various 4(3):1-12.
parameters. The prepared formulations showed
significant effects against acne causing organism.

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2. Rathi Sanjay K: Acne Vulgaris Treatment- The 7. Tiwari Prashant, Kumar Bimlesh, Kaur
Current Scenario. Indian Journal of Mandeep, Kaur Gurpreet, Kaur Harleen:
Dermatology 2011; 56(1):7–13. Phytochemical screening and Extraction: A
3. Arora Vimal, Lohar Vikram, Singhal Sandeep, Review. Internationale Pharmaceutica Sciencia
Bhandari Anil: Vitex negundo - A Chinese 2011; 1(1):98-106.
Chaste Tree. International Journal of Review 8. Nguyen Le BaoDuy, Dao Thi Diem Trang,
Article Pharmaceutical Innovations 2011; Nguyen Pham Minh Trang: Preliminary
1(5):9-20. Phytochemical Analysis of Leaf Extracts of
4. Deogade Meena Shamrao, Pandya Tarulata, Thuja Orientalis (L.) Endl. International Journal
Shivarama Kethamakka Prasad, Kale Kunal, of Research Science & Management 2015;
Tankhiwal Nilima: Antimicrobial Activity of 2(1):21-25.
Vitex Negundo Linn (Nirgundi) Leaves Extract. 9. Sekar Mahendran, Hanim Fouzia, Halim Abdul.
Journal of Res. Tradit. Medicine 2016; 2(4):99- Formulation and Evaluation of Natural Anti-
102. Acne Cream containing Syzygium
5.
P Ruban, K Gajalakshmi: In vitro antibacterial samarangense Fruits Extract. Annual Research
activity of Hibiscus rosa-sinensis flower extract & Review in Biology 2017; 17(3):1-7.
against human pathogens. Asian Pacific 10. Vats Aditi, Sharma Pranav: Formulation and
Journal of Tropical Biomedicies 2012; Evaluation of Topical Anti Acne Formulation of
2(5):399–403. Coriander Extract. International Journal of
6. Saima Ali, Khan Muhammad Rashid , Pharmaceutical Sciences Review and Research
Irfanullah, Moniba Sajid, Zartash Zahra: 2012; 16(2):97-103.
Phytochemical investigation and antimicrobial
appraisal of Parrotiopsis jacquemontiana
(Decne) Rehder. BMC Complementary and
Alternative Medicine 2018; 18(43):1-15.

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FORMULATION AND EVALUATION OF CONTROLLED RELEASE

FLOATING TABLETS OF NIZATIDINE USING HYDROPHILIC POLYMERS
Sanjay K. Mishra1*, Satish Namdeo2
1*
Chameli Devi Institute of Pharmacy, Indore, Madhya Pradesh.
2
ADINA Institute of Pharmaceutical Sciences, Sagar, Madhya Pradesh.
[email protected]

ABSTRACT
To prepare and evaluate controlled release tablet of Nizatidine using Hydrophilic polymers to increase the
buoyancy time and release the drug in longer periods of time in the stomach. Nine batches formulation (F1-F9)
was prepared from active drug Nizatidine with different concentration of excipients like hydrophilic polymer
polyvinyl alcohol, gas releasing agent sodium bicarbonate and citric acid along with other ingredients. All
batches formulation was evaluated for in vitro buoyancy study, drug content uniformity, in vitro dissolution
and disintegration study etc. among them selected F4 batch formulation conducted for stability study. In vitro
buoyancy studied result show that, the floating lag time of all batches formulation were found to be in the
range of 66 s to 84 s and the total floating time were found to be 7 h to 12 h and disintegration studied result
was found to be 400±1 min to 574.6±2.39 min. The in vitro dissolution studied result of F4 batch formulation
was found to be maximum compare to other that was 97.46±0.96% at 12 h in 0.1 N hydrochloric acid medium.
The stability studied results of selected F4 Batch’s formulation indicated that the post compression parameters
result were not much more different before and after the stability study (40±2°C at 75 % RH). So from the
above studied results it concluded that to enhance the bioavailability and gastric residence time of Nizatidine
drug, F4 batches controlled release floating tablets of Nizatidine is best choice.
Keywords: Nizatidine , floating tablets, controlled release, hydrophilic polymers

Introduction The hardness of all batches 06 tablets were

Peptic ulcer is the most common gastrointestinary measured by the Pfizer hardness tester. The
disorder in clinical practice. Peptic ulcer occurs due reading was noted down in Kg/cm2.
to an imbalance between the aggressive and the Diameter and thickness
defensive factors. The half-life of Nizatidine about Diameter and Thickness of all batches 6 tablets
3.5 h and it has poor bioavailability, to overcome were measured by Vernier caliper.
these problem we prepared controlled release
floating tablets of Nizatidine with hydrophilic Friability test
polymer, viscosity enhancer such as polyvinyl All batches 20 tablets were placed in the friabilator
alcohol, gas releasing excipients sodium bi and rotating vertically at 25 rpm for 4 min. After
carbonate and citric acid. dusting the total remaining weight of the tablet
was measured and calculated the % friability by
Materials and methods the following formula.
Materials used in the development of controlled % Friability= [(Weight Final - Weight
release floating tablets, Nizatidine was a gift Original) / Weight Original] × 100
sample from Dr. Reddy’s Pharmaceutical Ltd.
Hyderabad , polyvinyl alcohol, ethyl cellulose, In vitro buoyancy study
carbopol-934, beeswax, sodium bicarbonate, citric In vitro buoyancy study was performed to
acid, talc, magnesium stearate, all were of determine the floating lag time and total floating
analytical grade. A direct compression technique time. In the study one tablet was placed in USP
was used for the preparation of controlled release type II paddle apparatus. Dissolution basket was
floating tablets of Nizatidine. Nine batches (F1 to filled with 900 ml of 0.1N hydrochloric acid and
F9) tablets were prepared from active drug maintained the temperature at 37 ± 0.50C.
Nizatidine along with different concentration of
excipients by trial and error methods. Uniformity of weight
For the study, from each batch 20 individual
Evaluation parameters of prepared tablets tablets without dusting randomly selected and
Hardness test weight by electronic weigh balance.

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Drug content uniformity controlled release floating tablets. The

Each batch 20 tablets were powdered and the temperature of dissolution flask was maintained at
blend equivalent to 200mg Nizatidine was weighed 37± 0.5°C and filled 900ml 0.1N hydrochloric acid
and dissolved in 1000ml of 0.1N hydrochloric acid. in the flask. The apparatus was allowed to run for
The prepared solution was sonicated, filtered, and 12h at 50rpm. 5ml sample solution was withdrawn
suitably diluted. After this, the drug content was after every 1 hour using a pipette and filtered the
determined with the help of Double Beam UV solution by 0.45µm syringe filter.. All samples were
Spectrophotometer (UV-1800 Shimadzu) at 287.8 suitably diluted and analyzed by double beam UV
nm. Spectrophotometer (UV-1800 Shimadzu) at
287.8nm to determine the amount of drug
Disintegration study content.
The disintegration test apparatus (Electro lab
disintegration test apparatus) was used to conduct Stability study
the disintegration study. There was thermostat, Stability study was conducted for F4 batch’s
which is provided to regulate the temperature of formulation, as F4 batches formulation was best
the fluid medium to the desired temperature. The among the nine batches formulation (F1-F9) based on
test was carried out on 6 tablets in each batch the buoyancy time, disintegration time, in vitro drug
formulation using disintegration media, 900ml released study. Stability studies were performed over
0.1N hydrochloric acid at temperature 37.5ºC± a period of 90 days at a temperature of 40±2°C at 75%
2ºC. RH.

In vitro drug release study Results and discussion

USP- type II dissolution apparatus (paddle type)
was used for the dissolution study of prepared

Table 1: Composition of controlled released floating tablets of Nizatidine

Ingredients F1 F2 F3 F4 F5 F6 F7 F8 F9
Nizatidine 200 200 200 200 200 200 200 20 200
Hydrochloride(mg) 0
Polyvinyl 85 76 68 59 68 63 65 71 76
alcohol(mg)
Sodium bi 32 35 40 44 39 44 43 39 38
carbonate (mg)
Citric acid (mg) 13 16 20 24 21 22 21 18 16
Ethylcellulose(mg) 70 70 70 70 70 70 70 70 70
Bees wax(mg) 80 80 80 80 80 80 80 80 80
Carbopol-934(mg) 52 52 52 52 52 52 52 52 52
Mag. stearate(mg) 15 15 15 15 15 15 15 15 15
Talc(mg) 13 13 13 13 13 13 13 13 13

Table 2: In vitro buoyancy studied results, floating lag time and total floating time
Formulation Floating lag time Total floating
Sr. No batch code (s) time(h)
1. F1 82 >10
2. F2 81 >8
3. F3 76 >9
4. F4 68 >10
5. F5 75 >9
6. F6 78 >8
7. F7 77 >9
8. F8 79 >9
9. F9 80 >9

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Table 3: Evaluation parameters of controlled release floating tablets of Nizatidine

Formulatio Mean Diameter and Friability Uniformi Mean drug Disintegration
n batch hardness thickness % w/w ty content time (min)
code Kg/cm 2 (mm) weight %±SD,
(mg) n=3
F1 11.05 12.1,4.1 0.53 560 99.6±0.81 400± 1.00
F2 10.23 12.1,4.2 0.52 559.9 98.8±1.05 436.6 ± 0.57
F3 9.72 12.3,4.1 0.56 560.2 100.6±0.7 494.6 ± 1.52
F4 9.58 12.2,4.1 0.51 560.1 100.3±0.8 577.6± 2.59
F5 9.89 12.1,4.2 0.58 560.4 101.2±1.0 457.0 ± 2.00
F6 9.62 12.1,4.2 0.4 560 101.1±1.0 519.3 ± 2.08
F7 10.20 12.1,4.2 0.54 560 101.5±0.8 452.3 ±1.52
F8 10.05 12.1,4.1 0.55 560 99.6±1.82 445.6 ±2.51
F9 9.95 12.1,4.2 0.57 560 99.0±1.00 439.6 ±2.08

Table 4: Cumulative % drug released of tablets in 900ml 0.1N hydrochloric acid medium
Tim Cumulative % drug released of tablets in 900ml 0.1N
e hydrochloric acid medium
(h) F1 F2 F3 F4 F5 F6 F7 F8 F9
1 8.11±0.8 9.21±0.9 9.59±0.9 11.49±0. 8.86±0.9 10.71±1. 9.31±1.0 9.09±1.1 8.78±
9 1 7 95 5 10 2 0 1.34
2 12.23±0. 13.67±0. 16.51±1. 22.63±0. 16.56±1. 16.65±1. 16.78±0. 15.35±1. 14.42±0.
80 84 11 97 05 00 69 05 92
3 20.86±1. 20.63±1. 24.46±1. 31.52±1. 23.63±1. 27.70±0. 23.26±1. 22.44±0. 21.58±1.
24 11 06 06 00 90 00 95 15
4 27.52±0. 30.31±1. 35.49±0. 40.45±0. 34.56±1. 34.53±0. 34.45±1. 32.64±1. 31.37±1.
94 33 79 98 20 95 01 06 01
5 39.01±1. 40.44±0. 47.53±1. 49.56±0. 46.60±1. 48.68±0. 46.70±0. 44.65±1. 42.34±1.
20 98 01 91 05 82 90 01 22
6 46.78±1. 46.60±1. 53.33±0. 58.59±0. 52.36±1. 55.64±2. 53.30±1. 50.45±0. 48.50±0.
16 00 99 90 11 05 07 90 76
7 53.04±1. 55.42±1. 59.59±1. 66.60±1. 58.55±1. 65.67±1. 57.71±1. 57.20±1. 56.33±0.
72 27 00 23 12 06 11 11 92
8 56.73±0. 57.50±1. 64.64±1. 71.40±1. 64.40±0. 71.38±1. 64.90±1. 61.30±1. 59.30±1.
98 14 32 07 86 06 73 15 21
9 60.49±1. 61.37±0. 69.49±0. 77.72±0. 68.57±0. 77.55±1. 67.41±1. 64.33±1. 62.46±1.
06 99 92 76 92 25 48 05 49
10 61.60±1. 67.49±1. 73.61±0. 82.57±1. 73.19±0. 81.67±1. 72.35±1. 70.27±1. 68.28±1.
11 05 99 11 82 07 17 00 04
11 66.66±0. 71.69±1. 78.56±1. 90.51±1. 77.50±1. 87.91±1. 77.37±0. 74.49±0. 72.55±1.
87 12 05 15 10 44 99 83 27
12 71.26±1. 73.61±0. 84.46±1. 98.48±0. 83.68±1. 93.48±1. 81.56±1. 77.35±1. 75.09±1.
01 85 26 98 15 22 05 11 56

Table 5: Stability studied results of F4 batch’s controlled release floating tablets of Nizatidine
Formulation 1st day 30th day 60th day 90th day
99.948±0.0518 99.913±0.0563 99.620±0.0896 99.693±0.072
F4
% % % 3%

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Figure 1: Cumulative % drug released with time in 900ml 0.1N hydrochloric acid medium

Conclusion Aliu A, Daka A, Basha N. Clinical role of

The aim of the study was to formulate and Nizatidinein community-acquired
evaluate controlled release floating tablet of infections. Prilozi 2011;32(2):143-55
Nizatidine with hydrophilic polymers as well as 3. Ige OM, Okesola AO. Comparative
viscosity enhancers such as polyvinyl alcohol and efficacy and safety of Nizatidineand
gas releasing excipients sodium bicarbonate and ciprofloxacin in the management of
citric acid along with other excipients. Nine adults with community-acquired
batches (F1 to F9) tablets were prepared and their pneumonia in Ibadan, Nigeria. Annals of
quality control tests were performed like hardness, Ibadan Postgraduate Medicine
friability, in vitro buoyancy study, floating time, 2015;13(2):72-78.
disintegration study, dissolution study, stability 4. Healy DP, Sahai J V, Sterling LP, Racht
study etc. On the above studied results revealed EM. Influence of an antacid containing
that F4 formulation was the best formulation aluminium and magnesium on the
among F1 to F9 batches formulation. So from the pharmacokinetics of cefixime.
above studied results concluded that prepared F4 Antimicrobial agents and
batch’s Nizatidine controlled release floating chemotherapy1989;33(11):1994-1997.
tablets can be best choice to enhance the gastric 5. K.K. Formulation and evaluation of
residence time and bioavailability. Prepared F4 effervescent floating tablets of tizanidine
batch’s Nizatidine controlled release floating hydrochloride. Acta Pharm. 61 (2011)
tablets can be best choice to enhance the gastric 217–226. doi:10.2478/v10007-011-0015-
residence time and bioavailability. 5.
6. Arza RAK, Gonugunta CSR, Veerareddy
References PR. Formulation and evaluation of
1. Sirisolla J, Ramanamurthy K V. swellable and floating gastroretentive
Formulation and evaluation of ciprofloxacin hydrochloride tablets.
Nizatidinetrihydrate matrix tablets using AAPS PharmSciTech 2009;10(1):220-226.
hpmc,Sodium cmc, ethyl cellulose. doi:10.1208/s12249-009-9200-y.
Indian Journal of Pharmaceutical 7. Ghosal K, Chakrabarty S, Nanda A.
Sciences2015;77(3): 321-327. Hydroxypropyl methylcellulose in drug
2. Dreshaj Sh, Doda-Ejupi T, Tolaj IQ, delivery. Pelagia Research Library
Mustafa A, Kabashi S, Shala N, Geca Nj, 2011;2(2):152-168.

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FORMULATION, DEVELOPMENT AND EVALUATION OF NANOMIEMGEL FOR THE

TREATMENT OF SKIN DISEASE
Shikha Jaiswal*1 and Revathi A. Gupta2
1. Department of pharmaceutics, Dr. APJ Abdul Kalam University, Indore (M.P.)
2. Department of pharmaceutical chemistry, Dr. APJ Abdul Kalam University, Indore (M.P.)
[email protected]

ABSTRACT
The objective of this study was to formulate and evaluate a unique matrix mixture (nanomiemgel) of
nanomicelle and nanoemulsion containing Fluconazole and Ketoconazole and to compare it to a marketed
formulatin. Nanomicelles were prepared using Vitamin E TPGS by solvent evaporation method and
nanoemulsion was prepared by high-pressure homogenization method. Using a new combination of two
different drug delivery systems (NEM+NMI), the absorption of the combined system (NMG) was found to be
better than either of the individual drug delivery systems due to the utilization of the maximum possible paths
of absorption available for that particular drug. The formulation was evaluated for pH, solubility, spreadibility,
drug content etc.
Keywords: Nanomiemgel, Nanoemulsion, Nanomicelle, Combination therapy.

Introduction Transcutol’’ mixture (1:1). The oil and surfactant

One of the most promising drug delivery systems mixture-containing drug were sonicated for about
for enhancing skin permeation of drugs is the 15 minutes to get clear oil & surfactant mixture. To
microemulsion or nanoemulsion system. the mixture, 11 mL of deionized water was added
Nanoemulsions are thermodynamically stable while homogenizing to get a primary emulsion.
transparent (translucent) dispersions of oil in The obtained o/w emulsion was homogenized
water stabilized by an interfacial film of surfactant further for 5 minutes at 3000 rpm to obtain a
and co-surfactant molecules with droplet size less microemulsion.
than 1000 nm. In this study, we have developed a Preparation of Nanomicelle (NMI)
drug delivery system called nanomiemgel through The FLZ and KTZ nanomicelle was prepared with
a novel formulation strategy, which utilizes the Vitamin E TPGS using the solvent evaporation
‘‘Multi Absorption Mechanism’’ (MAM) concept method where the organic solvent was removed
and has a broad applicability. Nanomiemgel through evaporation. The Vitamin E TPGS (7.55
consists of two types of matrices; A & B. Matrix A gm), fluconazole (200mg) and ketoconazole
comprises the nanoemulsion whilst matrix B (200mg) were added to 2 mL of acetone. When a
comprises the nanomicelles. The hypothesis of the clear solution was obtained, 25 mL of distilled
present study is that every nano drug delivery water was added. Then the organic solvent was
system is unique and its rate, extent and removed gradually through evaporation.
mechanism of absorption depend on the size,
charge and composition of the nano drug delivery Preparation of Nanomiemgel (NMG)
system. So, when a combination of completely 50 mL of purified distilled water and propylene
different drug delivery systems is utilized for the glycol (1:1) were put into a beaker and heated up
0
delivery of a drug, the absorption of the combined to 70 C. EDTA (0.5%) and pluronic F-127 (0.5%)
system would be better than either of the were added into the warmed purified water with
individual drug delivery systems due to the continuous stirring after which the mixture was
0
utilization of the maximum possible paths of cooled down to 50 C. The mixture was then added
1-3
absorption available for that particular drug. to carbopol (1 g) under continuous low rpm
stirring to form a uniform gel that was free from
Material and Methods lumps and bubbles. The pH of gel was then
Preparation of Nanoemulsion (NEM) neutralized with triethanolamine (TEA). After
0
The fluconazole (FLZ) and ketoconazole (KTZ) cooling the gel phase to 40 C, the NEM and NMI
nanoemulsion (NEM) was prepared by first formulations were incorporated into the carbopol
dissolving 200 mg of FLZ and 200 mg of KTZ in 8 mL gel and mixed uniformly to obtain the NMG. The
of olive oil and miglyol (1:1), followed by the NEM and NMI were dispersed into the carbopol
addition of 6 mL of ‘‘Polysorbate 80 and gel to achieve the final concentration of FLZ and

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KTZ at 1.5% & 0.01% respectively, whereas the The studies demonstrate that the NMG comprising
final concentration of carbopol was maintained at NEM and NMI enhanced the skin permeation of
2%. The NMG was evaluated for pH, SEM, TEM, Fluconazole and Ketoconazole by translocating the
drug content, viscosity study, spreadibility, skin nanoparticle across the deeper skin layers by
irritation, extrudability study, homogeneity and improving the skin contact time, hydrating the skin
4-5
grittiness. and by forming a thin layer on the skin surface
(occlusive effect). Thus, the increase in skin
Results and conclusion permeation of Fluconazole and Ketoconazole was
The formulated NMG was evaluated and the further responsible for the improved therapeutic
results are given in table 1. From the data obtained response. NMG suggesting the potential of the
it was concluded that the NMG have better results combination therapy to treat skin diseases
as compared to individual formulations and other.

Table 1: Evaluation parameters of NMG

Formulations pH Drug content Viscosity Spreadibility Skin Extrudability Homogeneity Grittiness
UV HPLC (cps) (cm) irritation (%)
NEM 6.7 99.29 99.10 45100 5.05 - 97.99 H NG
NMI 6.8 99.28 99.25 57300 4.32 - 98.71 H NG
NMG 6.9 100.03 100.01 51600 5.58 - 99.10 H NG
ALZ (FD-1) 6.8 98.97 99.91 47800 4.98 - 98.27 H NG
KTZ (FD-2) 6.8 99.02 99.01 45200 4.95 - 98.19 H NG
MKT 7.1 99.98 99.87 68500 4.10 - 99.98 H NG

References xenograft mouse epidermoid carcinoma

1. Sahoo S, Pani NR and Sahoo SK. Effect of model compared to dacarbazine
microemulsion in topical sertaconazole suspension. Nanomedicine, 2011: 7: 277–
hydrogel: in vitro and in vivo study. Drug 283.
Deliv, 2014: 20: 1–8. 4. Raza K, Kumar M, Kumar P, Malik R and
2. Yu M, Ma H, Lei M, Li N and Tan F. In Sharma G. Topical Delivery of
vitro/in vivo characterization of Aceclofenac: Challenges and Promises of
nanoemulsion formulation of Novel Drug Delivery Systems. Biomed Res
metronidazole with improved skin Int 2014: 406731.
targeting and anti-rosacea properties. Eur 5. Marto J, Baltazar D, Duarte A, Fernandes
J Pharm Biopharm 2014: 2: 00115–00115. A and Gouveia L. Topical gels of
3. Kakumanu S, Tagne JB, Wilson TA and etofenamate: in vitro and in vivo
Nicolosi RJ. A nanoemulsion formulation evaluation. Pharm Dev Technol: 2014: 1–
of dacarbazine reduces tumor size in a 6.

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FORMULATION AND EVALUATION OF MEDICATED NAIL LACQUER OF TERBINAFINE

HYDROCHLORIDE FOR THE TREATMENT OF ONYCHOMYCOSIS
Gupta Ashish, Pandya Janhvi, Sharma Ravi, Sharma Pravin K, Darwhekar GN
Acropolis Institute of Pharmaceutical Education and Research Indore (MP) 453771
[email protected]

ABSTRACT
Onychomycosis (also known as dermatophytic onychomycosis or Tinea unguium) is a fungal infection of the
nail. The causative pathogens of onychomycosis include dermatophytes, Candida, and non dermatophytic
molds. In the present work, a medicated antifungal nail lacquer of terbinafine hydrochloride has been
developed. The objective of the study was to deliver a sustained release of drug over extended period of time
and hence reduce the frequency of administration. This was expected to improve clinical efficacy and also
improve the patient compliance. The nail lacquer formulation were prepared by simple mixing and analyzed
for non -volatile content, gloss, drying time, smoothness to flow, drug diffusion studies, drug content
estimation, anti -microbial studies. Among all formulation, nail lacquer prepared with 1% terbinafine
hydrochloride, 6% nitrocellulose, 4% ethyl cellulose, 1.5 % Di-n-butyl phthalate and other additives exhibited
good nonvolatile content, drug release, drug content estimation and zone of inhibition. The drug release
could be extended up to 48 hour and a complete release of 98.38±1.909% was observed. Formulation and
usage of these systems are considered to be safe, without any complication. So we can conclude that the
antifungal nail lacquer may be one of the novel dosage forms that can revolutionize the pharmaceutical and
health care sector.
Keyword: Onychomycosis, Nail Lacquer, Terbinafine Hydrochloride, Transungual Delivery, Permeation
Enhancer.

Introduction cellulose, di-butyl phthalate, thioglycolic acid and

Human nails do not have only protective and 2-mercaptoethnol were purchased from Loba
decorative role, but can also be considered as an chemicals pvt Ltd. All the chemical used were
alternative pathway for drug delivery, especially in analytical grade.
nail diseases such as Onychomycosis or Psoriasis. Nail lacquer was prepared by using simple stirring
These nail diseases are widely spread in the method in which all the ingredients were added on
population, particularly in elderly and immune- continuous stirring. Nail lacquer was prepared by
compromised patients. But as we know that the adding film formers in appropriate solvents in
structure and composition of nail plate severely which after obtaining a clear solution, the drug and
limits penetration of drugs and because of that plasticizer was added along with the selected
only a fraction of topical drugs penetrates across permeation enhancer. The volume was made up
the nail, as well as the oral therapies accompanied with the solvent.
by systemic side effects and drug interaction. The film base for nail lacquer was selected by
Hence for the successful treatment of nail evaluating the film with desired characteristic. The
diseases, the applied active drug must penetrate film was prepared by adding nitrocellulose in small
through the dense keratinized nail plate and reach amount of ethyl acetate and ethyl cellulose in
deeper layers, the nail bed and the nail matrix. isopropyl alcohol in a separate beaker under
continuous stirring. Both the solutions were mixed
Objective together and di-n-butyl phthalate was added to it
The aim of the present work was to formulate and as a plasticizer under stirring. The stirring was
evaluate the medicated nail lacquer of terbinafine continued till a clear solution was obtained. Then,
for the treatment of onychomycosis and to the volume was made up to with ethyl acetate and
provide the better patient compliance and for stored in air tight container.
target delivery of drug.
Evaluation
Material and Method The prepared film base was characterized and
Terbinafine hydrochloride was obtained as a gift optimized on the basis of film thickness, folding
sample from Yarrow chem. lab which was chosen endurance and water resistance.
as the model antifungal agent. Nitrocellulose, ethyl

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The formulation of the nail lacquer was Stability studies

characterized on the basis of non-volatile content, The stability studies was performed for period of
drying time, drug content determination, diffusion one month and evaluated on various parameters.
studies across dialysis membrane and further
optimized batch was characterized as- Result and Discussion
All formulations showed desired film formation,
Ex-vivo transungual permeation studies good smoothness of flow, drying time was found
The in-vitro permeation study of the optimum to be satisfactory. Desired amount of nonvolatile
batch was performed on the animal hooves. matter was seen with complete evaporation of
Hooves, obtained from the freshly slaughtered volatile matter leaving a thin film, it range from 19-
cattle, which was free of adhering connective 44%.Drying time of the lacquers was found in
tissues, were soaked in distilled water for 24 hrs. range of 30-48sec, except F7. Smoothness of flow
After that, from the distal part of the hooves, the and Gloss were found to be satisfactory.
membranes of about 1 mm thickness were cut. Percentage drug content for all the lacquers was in
The studies were carried out by using Franz between 89-98% .Drug content more than 90% in
diffusion cell. The receptor compartment of cell the formulation shows the high amount of drug
was filled with solvent containing phosphate present in the formulation, without causing any
buffer pH 7.4 and methanol (4:1). The hoof change in the ideal property of ideal lacquers. The
membrane was placed carefully on the cell without in vitro diffusion studies showed very good release
any air bubbles. The sample equivalent to 50 mg of 98.38% in the 24th hrs in F3. The film
was applied evenly on the surface of the hoof characteristics, smoothness to flow and drying
membrane. The whole assembly was placed under time were also better for this formulation. The
constant stirring and was maintained at 37º C for evaluation of formulations after stability charging
48 hrs. The 5 ml aliquot of sample was withdrawn showed there was no significant change in physical
at 1, 2, 3, 4, 6, 8, 24, and 48 hours and was appearance and colour. Non volatile content,
replaced by 5 ml of fresh solvent. After required drying time, smoothness of flow, gloss along with
dilutions the sample was analyzed using double- changes in % drug content and drug release study
beam UV spectrophotometer at wavelength of showed results obtained before stability charging.
280.50 nm and drug release was determined and Thus the results of stability study showed that
compared with the results obtained from dialysis there are no stability problems. The formulations
membrane. The procedure was carried out in were found to be stable for a period of one month
0
triplicate. at 40 C.

Zone of inhibition Conclusion

The zone of inhibition was determined by using From the above work done, it was concluded that
cup plate method. Candida albicans were the nail lacquer containing 10% of thioglycolic acid
employed for testing antifungal activity. The (F3) shows the highest percentage drug release
culture was maintained on sabouraud’s agar (98.38 %) at 48 hours with desired drying time
slants. 20 ml of sabouraud’s agar medium in (31.6 seconds), having drug content up to 98.42 %.
melted form was inoculated with 48 hours old 0.2 Hence, F3 formulation was selected as the
ml suspension of Candida albicans in three optimized batch. From all the datas, it can be
petridish and was kept undisturbed for 15 minutes concluded that medicated nail lacquers can be
to solidify. The cups (1 cm diameter) were used as a tool for the ungual drug delivery system
punched in all three petridish and was filled with in the treatment of onychomycosis. Apart from
0.05 ml of a solution containing sample (equivalent treating the nail infections, the medicated nail
to 0.5 mg drug) dissolved in DMSO in first lacquers can be also used for beautification of nails
petridish, 0.05 ml of solution containing pure drug with ease of application. This improves patient
(0.5 mg) dissolved in DMSO in second petridish compliance and acceptability. This whole research
and 0.05 ml of pure DMSO in third petridish. These work still requires a process of clinical trials before
plates were kept for diffusion at 40º C for 1 hour, marketing the formula for treatment.
and then incubated at 30º C for 48 hrs. After the
completion of incubation period, the zone of Reference
inhibition was measured. 1. Elewski, B.E. (1998) Onychomycosis:
Pathogenesis, Diagnosis, and

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International Journal of
Pharmaceutical Sciences and Research
ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

Management. Clinical Microbiology 4. Gupta, A.K. and Ryder, J.E. (2003) The Use
Reviews 11, 41429. of Oral Antifungal Agents to Treat
2. Gaddime, S.B., Nagoba, S.N., Pattewar, Onychomycosis. Dermatologic Clinics 21,
S.G. and Wadulkar, R.D. (2018) 469-479.
Formulation and Evaluation of Medicated 5. Havu, V., Brandt, H., Heikkila, A., Hollmen,
Nail Patches for the Treatment of A., Oksman, R., Rantanen, T.andSaari, S.
Onychomycosis. International Journal of (1997) A Double-blind, Randomized Study
Pharmaceutical Science Invention 7(4), Comparing Itraconazole Pulse Therapy
52-58. With Continuous Dosing for The
3. Goodfield, M.J.D. (1992) Short-duration Treatment of Toe-nail Onychomycosis.
Therapy with Terbinafine for British Journal of Dermatology 136, 230-
Dermatophyte Onychomycosis: a 234.
multicenter trial. British Journal of
Dermatology 126(39), 33-35.

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FORMULATION AND EVALUTION OF HERBAL SHAMPOO CONTAINING

EXTRACT OF ALLIUM CEPA AND ANNONA SQUAMOSA.
Darshana Sharma*,Tahir Nizami, Namrata Rathore, Neelesh Malviya
Smriti College of Pharmaceutical Education, Indore, M.P. (India)
[email protected]

ABSTRACT
Shampoo is a hair care product used for the removal of oils, dirt, dandruff and environmental pollutants. We
prepared onion and annonasaquamosa herbal anti-lice shampoo for dry and damage hair. Hair fall is common
problem in India. Our formulation was clear good foam formation. Anti- lice herbalshampoo was prepared
with annonasaquamos seed extract and allium cepa were used as cleansing agent. Evaluation of organoleptic
properties, physicochemical and performance test were performed and compared with synthetic marketed
anti -lice product. The advantage of this shampoo is better nutrient and nourishment to hair follicles and
promote hair growth possess antibacterial antimicrobial, anti-lice properties
Keywords:-Annona Squamosa, Anti-lice, Allium cepa, Organoleptic, Follicles

Introduction alcohol, methyl paraben, lemon juice, coconut oil,

Allium cepa, family liliaceae has been reported castor oiled and extract of annona squamosa is
to possess antimicrobial, antibacterial, better used for formulation of shampoo. First 100 grams
nourishment, nutrients and also used as hair of bulbs of Allium cepa and 100gm of Annona
scalper hair loss.[1, 2] Annona squamosa Linn. squamosa was weighed and it was extracted
(Annonaceae) is available in India. It contain anti – using ethanol (100%) within four days. After
lice activity and used as hair cleanser. the most Filtered with cloth and filtrate was allowed to
prevalent alkaloid is annonainclude oxophoebine, heating mantel at 40 degree temp. The
retiailine andisocorydine. Also used as anti-lice supernatant was collected and incorporated in the
agent.[3, 4] Shampooing is the most common shampoo base formula
form of hair treatment and primary function of
shampoo is cleansing of the hair.[5] we formulated Formulation of Shampoo
onion and Annona herbal shampoo for specially For the preparation of the shampoo Coconut oil
dry hair. Dry hair is common problem in India. and castor oil were saponified with potassium
Formulating cosmetics using completely natural hydroxide using reflux condenser. After
raw materials is a difficult task. complete saponification, glycerin was added with
stirring followed by mixing of onion and
Material and methods annona squamosa . In this preparation Ethyl
Bulbs of Allium cepa (onion) and seeds of alcohol, methyl paraben used as preservative and
Annona squamosa were collected and used for lemon juice used for masking the pungent
the preparation of extract. Plant extraction was smell of extract. For the formulations of
performed by hot continuous extraction (Soxhlet) shampoocomposition as mentioned in table 1.
process. Potassium hydroxide, glycerin, ethyl

Table 1: Formulation of herbal Shampoo

S.No. Ingredients Quantity taken
1 Coconut oil 10
2 Allium cepa 2
3 annona squamosa 2
4 methyl paraben 0.5
5 potassium hydroxide 1
6 Glycerin 5
7 lemon juice 2
8 castor oil 5
9 Campher 2

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Evaluation parameters water. After thorough mixing of shampoo and

PH: 1% shampoo solution was used to determine water the surface tension was measured by
the pH by using the pH meter using stalagmometer (Borosil Pvt. Ltd.)
Foam Formation (Shake Test): Took 50 ml of the Skin irritation test: Applied the solution of
1% shampoo solution in a 250 ml graduated prepared shampoo on skin and kept for 5 min
cylinder and recorded the volume. Then covered and observed for redness of skin and irritation
the cylinder with hand and shaken 10 times. The there, were no any red coloration and the
total volume of the contents was recorded after irritation to the skin.
shaking. Calculated the volume of the foam and 5) Viscosity: Viscosity was determined by using
recorded the size of the bubbles. the Ostwald viscometer (Borosil Pvt. Ltd).
Surface Tension: Prepared 1% v/v solution of
shampoo by mixing 2 milliliters of shampoo with Result
200 ml of distilled water. The shampoo was taken The prepared formulated shampoo was evaluated
in the beaker and then slowly added distilled and the result was shown in the table 02.

Table 2: Evaluation of herbal shampoo

S.No. Parameters Observation
1 pH 6.3
2 Surface Tension 38.45
3 Foam Formation (Shake Test) Good
4 Skin Irritation Test No Irritation
5 Viscosity 6.5
8 castor oil 5
9 Campher 2

Conclusion Reference
From the above study it can be concluded that the 1. Allium cepa l-the plant list “the plantlist
formulation of herbal shampoo using annona org.” publication details; sp.pl, 2013; 300:
squamosa and Allium Cepa provide nutritious and 1753.
as a result they are effective as a cleansing agent 2. ABC “All about onion” national onion
with antimicrobial, antibacterial properties. association retrieved 2013-03-24. 1-2
Flavonoids are important for increasing blood cells 3. Mainkar A.an jolly, formulation of natural
and they also help the blood to circulate to all shampoo. International journal cosmetics. sci,
parts of the body including scalp. Allium Cepa juice 2001; 23(1): 59-62.
helps the blood cells and it increases the blood 4. Kokatec.k., Purohit AP, Gokhale SB”
flow in the hair follicle. pharmacognosy”twenty fourth edition
published by NiraliPrakashan, 2003; 343.

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MORPHOLOGICAL STUDIES OF FEW HERBS USED IN THE TREATMENT OF LIVER DISORDERS

Deepika Patel1, Raju Choukse1 and Sumeet Dwivedi2
1, Research Scholar, Faculty of Pharmacy, Dr. A.P.J. Abdul Kalam University, Indore, (M.P.) –
India 2, Department of Pharmacognosy, Oriental College of Pharmacy & Research, Oriental
University, Indore, (M.P.) – India
[email protected]

ABSTRACT
Liver disorders are very common now-a-days due to social and status life style of human beings. A number of
modern medicines are available in the market but have various adverse effects. Traditional system of medicine
is so ingrained in our culture that, about 80% of the Indian population depends on this system for relief. With
such a huge section of an ever increasing population relying on herbal remedies, it is imperative that the plant
products which have been in use for such a long time be scientifically supported for their efficacy. The present
paper deals with the investigation of morphological studies of AI: Abutilon indicum(Leaves), PN: Phyllanthus
niruri (Fruits), EA: Eclipta alba (Leaves) and AS: Allium sativa (Bulb).
Keywords: Herbs, Liver disorders, Morphological studies

Introduction The plant parts viz., AI: Abutilon indicum(Leaves),

In the last few years there has been an exponential PN: Phyllanthus niruri (Fruits), EA: Eclipta alba
growth in the field of herbal medicine and these (Leaves) and AS: Allium sativa (Bulb) were
drugs are gaining popularity both in developing collected in the months of October-December
and developed countries because of their natural 2018 from the various local sites of Malwa region
origin and less side effects. Many traditional of Madhya Pradesh and identified & authenticated
medicines in use are derived from medicinal by Dr. S. N. Dwivedi, Prof. and Head, Department
plants, minerals and organic matter. A number of of Botany, Janata PG College, A.P.S. University,
medicinal plants, traditionally used for over 1000 Rewa, (M.P.) and was deposited in our Laboratory.
years named rasayana are present in herbal The macroscopy of different parts of the plant
preparations of Indian traditional health care such as color, odor, size, shape, taste, surface
4-7
systems. In Indian systems of medicine most characters and fractures were carried out.
practitioners formulate and dispense their own
recipes. The World Health Organization (WHO) has Results and Discussion
listed 21,000 plants, which are used for medicinal The plant parts viz., AI: Abutilon indicum(Leaves),
purposes around the world. Among these 2500 PN: Phyllanthus niruri (Fruits), EA: Eclipta alba
species are in India, out of which 150 species are (Leaves) and AS: Allium sativa (Bulb) were
used commercially on a fairly large scale. India is collected from local sites of Malwa region of
the largest producer of medicinal herbs and is Madhya Pradesh, India and identified
1-3
called as botanical garden of the world. The morphologically and compared with standard
present work was aimed on study of pharmacopoeial monograph.The macroscopy of
morphological parameters of few herbs used in different parts of the plant such as color, odor,
the treatment of liver disorders. size, shape, taste, surface characters and fractures
were carried out. The results were presented in
Material and Methods table 1

Table 1: Morphological characters of selected plant material

Parameters AIL PNF EAL ASB
Color Light green Light green Light green Cream
Odor Characteristics Sweet Characteristics Peculiar
Taste Bitter Sweet Acrid Astringent
Shape Ovate Oval Oblong oblong
Size L=4-5 cm B:1-2 cm L=1-2.5 cm B: 0.8-1.5 cm L= 3-7 cm B= 1-2.5 cm L=2-5 cm B=0.5-1.5 cm
Surface Rough Smooth Smooth Smooth
character
Fractures Absent Absent Absent Absent

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Conclusion some side effects if used for the longer duration.

The prevalence of liver disorders are very common The present work was undertaken to revel the
and alarming. In traditional system of medicine morphological studies of few herbs viz., AI:
herbal healers treat these diseases using the plants Abutilon indicum (Leaves), PN: Phyllanthus niruri
which have immense medicinal potentiality. (Fruits), EA: Eclipta alba (Leaves) and AS: Allium
Despite various available allopathic formulations, sativa (Bulb)
the relief from the disease is temporarily and has

Fig. 1: AI: Abutilon indicum (Leaves) Fig. 2: PN: Phyllanthus niruri (Fruits)

Fig. 3: EA: Eclipta alba (Leaves) Fig. 4: AS: Allium sativa (Bulb)

References 5. Khandelwal K.R., Practical Pharmacognosy,

1. Lipinski B. Pathophysiology of oxidative Thirteenth edition 2005, Nirali Prakashan,
stress in diabetes mellitus. J. Diabet. Pune, 149-156.
Complications. 2001; 15:203–210. 6. The Ayurvedic Pharmacopoeia of India.
st
2. Grover J.K., Yadav S., Vats V. Medicinal Part-I. Vol.-III. 1 ed. New Delhi: published
plants of India with antidiabetic potential. J. by Gov. of India ministry of health and
Ethnopharmacol. 2002; 81:81–100. family welfare department of
3. Seth S.D., Sharma B. Medicinal plants of Homoeopathy. 1999; 225
India. Indian J. Med. Res. 2004; 120:9–11. 7. Quality control method for medicinal plant
th st
4. Kokate CK. “Practical Pharmacognosy.; 4 material, 1 edition, published by World
ed. Vallabh Prakashan : 2005;18, 112-121. Health Organisation Geneva, Delhi; 2002.

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ANTI-CANDIDAL ACTIVITY OF HERBAL FORMULATIONS CONTAINING HYDRO-ALCOHOLIC EXTRACT

OF IPOMEA CAIRICA LINN. (LEAVES) USED FOR THE TREATMENT OF VAGINAL INFECTION
Shweta Shriwas1* and Sumeet Dwivedi1
1, Faculty of Pharmacy, Dr. A.P. J. Abdul Kalam University, Indore (M.P.)
2, Department of Pharmacognosy,
Oriental College of Pharmacy & Research, Oriental University, Indore, (M.P.) - India
[email protected]

ABSTRACT
Vaginal infections are prone and are very frequent and common among Indian women due to various un-
hygienic issues. The major fungus causing vaginal infection is Candida species. The present work aims to
investigate the anti-candida activity of herbal formulations (tablet & Cream) containing hydroalcoholic extract
of Ipomea cairica Linn. (Leaves). The results obtained were compared with standard anti-fungal drugs
amphotericin B. Further studies need to be establish to deepen knowledge on this area, namely, focused on
clinical trials to provide safer and more effective anti-fungal than the current ones.
Keywords: Herbal formulation, Ipomea cairica, Vaginal infection

o
Introduction distilled water and sterilized by autoclave at 121 C
In India approximately every women suffers from for 1 hour. The media were cooled and poured in
vaginal infection or any other associated disease. sterilized petri plate to solidified at room
The percentage is more in rural women than urban temperature. The fungal strains (Candida albicans)
women and the reason behind this is the life style, were used as obtained from Index Medical College,
food habit and un-hygienic conditions in rural Malwanchal University, Indore. The innoculum of
1-2
areas . strains were transferred to the recultured before
During past few years plant derived extracts and staring the lab work. The re-cultured fungal strains
their isolated phytochemicals are gaining were used for antifungal evaluation. The strains
importance and are also a new emerging area of were streak on the Mueller Hinton media and the
research. In last two decades anti-candida effects drug entrapped patches were placed. For negative
in the category of anti-microbial is of great control disc of distilled water and for positive
interest. Candida, a fungus is very often associated control amphotericin B disc (10 μg) were used. The
3-5
with the vaginal infections. The present study petri plates were kept in incubator for 24 hrs.
was designed to evaluate the anti-candidal activity After 24 hrs the petri-plates were checked for zone
of hydro-alcoholic extract of Ipomea cairica Linn. of inhibition. The zone of inhibition diameter was
(Leaves). recorded with the help of zone reader scale. The
zone of inhibition was calculated by subtracting
Material and Methods diameter of sample or standard or control by
Formulated anti-fungal tablet and cream of hydro- diameter of disc. The more the zone of inhibition
alcoholic extract of Ipomea cairica Linn. (Leaves) the more will be antifungal activity. All the reading
7
were taken and Anti-Candida activity were obtained were analyzed using one way analysis of
screened out. Fungal strain i.e., Candida albicans variance i.e., ANOVA. Student t-test was used. The
(ATTC) was obtained from Index Medical College, values are found to be statistically significant
Malwanchal University, Indore, (M.P.). was used (*P<0.00, **P<0.01). All the values obtained are
for the present investigation. Disc of whatsmann expressed as mean± standard error means (SEM).
filter paper of one quarter inch in diameter was
prepared and the same was sterilized using Results and Discussion
autoclave. The accurately weighed extracts were The investigation of the efficiency of plant extract
dissolved in methanol of different stock solutions and their formulations in induced systemic and
(10, 20, 30, 40, 50 μg/ml) solutions were prepared. local infection model is of quite interesting. Plants
All the dilution prepared was applied to have various phytochemicals such as flavonoids,
whatsmann filter paper disc using a micropipette. alkaloids, saponins, terpenoids which are
The disc were then dried and sterilized. The responsible for anti-microbial properties. Anti-
sabouraund’s agar and mueller Hinton agar media candida activity of herbal formulations (tablet &
were prepared by dissolving media in 1000ml of cream) containing hyd-roalcoholic extract of

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Ipomea cairica Linn. (Leaves) were evaluated. The Conclusion

zone of inhibition of formulations on Candida From the results (table 1, graph 1) obtained it was
albicans were presented in table 1. Results concluded that the PHC (HC5) have optimum anti-
indicate (Graph 1) that all the selected extracts candida activity when compared with standard
have significant anti-candida activity when and may be used for the treatment of vaginal
compared with standard drug amphotericin B. infections. Moreover detailed clinical approaches
need to establish for the formulation of safe and
effective drugs.

Table 1: Anti-Candida activity of PHF-F7 & PHC-HC-5

S/No. Test Zone of Inhibition (mm)
1. Negative Control 4.90±0.21
2. Positive Control 20.47±0.32**
3. PHF-F7 19.51±0.09*
4. PHC-HC-5 19.44±0.21**

Note: All values are expressed as Mean (X) ±SEM, (n=3). One way ANOVA followed by student test, values are
statistically significance *P<0.01, **P<0.001 when compared with control and standard.

50
ZOI (mm)

0 Zone of Inhibition (mm)

Test
Graph 1: Anti-Candida activity of PHF-F7 & PHC-HC-5

References 4. Sher A. Antimicrobial activity of natural products

1. Lakshmi V. and Gupta RK. Ayurvedic preparations from medicinal plants, Gomal Journal of Medical
and gynaecological disorders. International Journal Sciences, 2009, 7(1): 72–78, 2009.
of Ayurveda & Alternative Medicine, 2014, 5(2):10- 5. Rubió L., Motilva MJ and Romero MP. Recent
14. advances in biologically active compounds in herbs
2. Dwivedi S., Tripathi R. and Dwivedi SN. Ethno- and spices: a review of the most effective
medicinal plants used to treat gynecological antioxidant and anti-inflammatory active
disorders by tribal people of Madhya Pradesh, principles,” Critical Reviews in Food Science and
India. International Journal of Pharmacy and Life Nutrition, 2013, 53(9): 943–953.
Sciences, 2010, 1(3): 160-169. 6. Harborne JB. Phytochemical methods, Chapman
st
3. Palombo EA. Traditional medicinal plant extracts and Hall, 1984, I Edition, London.
and natural products with activity against oral 7. Lopes G., Pinto E., Andrade PB and Valentão P.
bacteria: potential application in the prevention Antifungal activity of phlorotannins against
and treatment of oral diseases, ”Evidence-Based dermatophytes and yeasts: approaches to the
Complementary and Alternative Medicine, 2011, mechanism of action and influence on Candida
Vol. 2011, Article ID 680354, 15. albicans virulence factor. PLoS One, 2013, 8(8):
Article ID e72203.

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STUDY OF ANTIOXIDANT PROPERTIES OF HYLOCEREUS UNDULATES (DRAGON FRUIT)

Pragya Rathore*Sarvesh Seth* Lubaina Kaba*
Softvision College and Research Centre, Indore
[email protected]

ABSTRACT
Hylocereus undulates is an exotic species of Cactaceae family with all goodness of natural components. The
peel, pulp and seeds of the fruit were studied extensively. The attractive red peels were found to be excellent
source of bioactive compound betacyanin, the pulp was rich in flavonoids and the seed oil rich in tocopherol.
All these bioactive compounds possess rich antioxidative properties and health promoting functions.
The total betacyanin content in the peel extract was found to be 2.2 mg/100 gm of peel extract.The total
flavonoid content using AlCl3 method using quercetin as standard was used. The methanolic extract of
Hylocereus pulp was found to be 158.6µg/ mg quercetin equivalent. Total polyphenol content was measured
using Folin Ciocalteau method and it was found to be 40mg/100g gallic acid equivalent. The stability of
betacyanin in the Hylocereus peel was evaluated by exposing the extracts of betacyanin at various pH
conditions and exposure times at a temperature of 100ºC. The extracts were prepared from dehydrated
samples (1g) diluted in buffer solution of Na 2HPO4 (0.2M) and citric acid (0.1M). The extract was exposed to a
temperature of 100 ºC. The absorbance was read at 538nm. The total flavonoid content of peel was
determined with the use of aluminium chloride (AlCl3) and the absorbance was read at 510nm using UV- Vis
spectrophotometer. The total flavonoids were then calculated from quercetin standard curve. All the tests
were performed in triplicates. The chemical and nutritive composition of the fruit makes it a desirable
nutraceutical.

Introduction W/V extract was prepared. The extracts were

Hylocereus Undatus or pitahaya Blanca or white- prepared in triplicates (n=3). Then the extract was
fleshed pitahaya belongs to the genus Hylocereus kept in refrigerator for maceration process for 24
in the family Cactaceae commonly known as hours. From extract, the solid material was
dragon fruit. Dragon fruit was selected for this separated by the use of funnel through Whatman
study to explore the anti-oxidants present in No. 42 filter paper in order to obtain a coloured
different parts of the fruit. For this purpose the solution. The solid residue was re-extracted twice
fruit was separated into peel, pulp and seeds and to increase the yielding efficiency. The filtrate was
these were studied individually for the presence of then centrifuged for 15 minutes at 8000 rpm and
these natural bioactive components. Betacyanin supernatant was collected. The obtained filtrate
has good tendency to lose electrons and get was used for the determination of total betacyanin
oxidized and the Betalamic acid, the core structure content, total phenolic content and total flavonoid
+3 +2
of betacyanin, can reduce Fe ions to Fe ions. content. The filtrate was then concentrated by
Flavonoids are a class of good anti-oxidant evaporation and dried in order to obtain powder.
compounds as they have high free radical
scavenging property. Determination of Betacyanin concentration
Betacyanin was quantified by measuring its
Materials and Methods absorbance at 538nm with UV-Vis
Sample Preparation spectrophotometer. The quantification of
Dragon Fruit (H. Undatus) was bought from the betacyanin was done using the formula described
[1]
market. The fruit was washed with tap water to by Lim et al. The concentration of betacyanin
remove impurities such as dirt, grit and dust. Then (mg/100gm of fresh weight) will be estimated by
fresh peel was separated. 50 g was weighed and the following formula: -
cut into small pieces in order to increase the Concentration of betacyanin (mg/100gm of fresh
surface area which will increase the extraction weight) = A538×M.W×V×D.F×100
efficiency. €×l×w
Where A538 = absorbance at 538 nm (λ max), l
Betacyanin Extraction (path length) =1.0 cm, DF dilution factor, V
For the extraction 50 g of peel was taken, 200mL volume of extract= 250ml, w fresh weight of
of 80% methanol was added to the sample and 1:4 extracting material=50g. For betacyanin, € (mean

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molar absorptivity or molar extinction co-efficient) Determination of Total Phenolic Content

4
=6.5 x 10 l/mol cm and MW (molecular weight) = Total phenolic content of methanolic extract of
550 g/mol. Dragon fruit was estimated by Folin-Ciocalteau
Five dilutions along with pure methanol extract of reagent using gallic acid as standard as described
[2]
betacyanin were prepared and their absorbance by Singleton and Rossi . The absorbance was
was taken at 538nm using colorimeter and their measured at 765 nm.
concentration was estimated using above formula.
All tests were performed in triplicates (n=3) Determination of Total Flavonoid Content
The total flavonoid content of peel was
Method to check stability determined with the use of aluminum chloride
The stability of betalains present in the pitahaya (AlCl3) method using quercetin as a standard
[3]
peel was evaluated by exposing the extracts of described by D. Marinova et al. The absorbance
betalains at various pH conditions (2.4, 3.2, 3.7, was read at 510 nm.
4.2, 4.5, 5, 5.5, 6, 6.5, 7, 7.5, and 8) and exposure
0
times (20,40,60,70,80 and 90 min) at 100 Celsius Results and Discussion
and exposure of 1 week, 2 week,3 week and 1 Betacyanin stability was found to be only affected
0
month at 4 C. The samples were taken at by light intensity, the temperature does not have
prescribed time intervals for the analysis by UV-Vis major effect on its stability. It is also stable in a
spectrophotometer, scanning absorbance at wide range of pH 3-7. The concentration of
538nm. betacyanin was found to be as follows:
The mean concentration was found to be 2.1789 ±
0.116 milligram/100gram as shown in Table1.

Table 1: Determination of Betacyanin concentration

DILUTIONS CONCENTRATION
(mg/100g)

PURE 2.172 ± 0.0199

1:1 2.144 ± 0.0399
1:2 2.073 ± 0.0598
1:3 2.313 ± 0.0798
1:4 2.256 ± 0.0998
1:5 2.115 ± 0.1196

Fig 1: Concentration (µg/mg quercetin equivalent)

Total flavonoid content obtained by the graph: f(x) and absorbance. The obtained regression equation
= mx+c equation , f(x) = 0. 4244x + 0.01538 for quercetin as the standard flavonoid solution
2
R value = 0.9931 Linear line obtained when the was y = 0.4244x + 0.01538.The determination
2
regression line is plotted between concentration coefficient (R ) obtained for standard flavonoid

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solution was 0.9931. Good correlation coefficient health promoting functions making Hylocereus a
shows the correlation between concentration and high value neutraceutical.
absorbance.The concentration of flavonoid
content of methanolic extract of dragon fruit from References
the above equation was found to be 158.6 µg/mg 1. Lim, S. D., Yusof, Y.A., Chin, N.L., Talib,
quercetin equivalents. T.A., Endan, J. and Aziz, M.G.:Effect of
extraction parameters on the yield of
Conclusion betacyanins from pitaya fruit pulps. J
The presence of rich antioxidants in different part Food Agr Environ 2011; 9:158-162.
of fruit makes it desirable, fruit peels to be used as 2. V.L. Singleton, J.A. Rossi: Colorimetry of
food additives, pulp to be consumed directly and total phenolics with phosphomolybdic-
the seeds for edible oil rich in tocopherols, all with phosphotungstic acid reagents Am J Enol
Vitic.1965;16:144-158.

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α-AMYLASE INHIBITORY ACTIVITY OF JASMINUM SAMBAC FOR THE MANAGEMENT OF

DIABETES AND ITS COMPLICATIONS
Rajiv Saxena1, Kushagra Dubey1, Ruchi Gupta1, Neelesh Malviya1
1
Smriti College of Pharmaceutical Education, Indore
[email protected]

ABSTRACT
The objective of this study is to evaluate the α-amylase inhibitory activity of different leaves extracts of
Jasminum sambac, for the treatment and management of diabetes. The leaves extract was prepared
sequentially with methanol, chloroform and distilled water by soxhlation technique. Different concentrations
(50, 75,100,125 and 150µg/ml) of each extract were subjected to α-amylase inhibitory assay by 3,5 dinitro
salicylic acid method. The absorbance was measured at 540nm. Percentage of inhibition and IC50 value of each
extract was calculated. The methanolic and aqueous extract of leaves of J. sambac shows highest α-amylase
inhibitory potential with IC50 value of 63.78±0.04 µg/ml and 74.61±0.05 µg/ml, respectively, when compared
with standard drug: acarbose (IC50 value 86.33±0.05 µg/ml).Whereas Chloroform extract fail to inhibit alpha-
amylase enzyme. The results of the present study indicates that, the methanolic and aqueous extracts of
leaves of J. sambac are potent α-amylase inhibitors and it was concluded that they can be used for the
management of postprandial hyperglycemia.
Keywords: Extracts, α-amylase inhibition, in-vitro, 3,5 dinitro salicylic acid

Introduction Forestry and Medicinal Plants, J.N.K.V.V, Jabalpur.

Diabetes mellitus is a chronic metabolic disorder. It The leaves were washed under running tap water
triggers the failing of insulin production or insulin and dried under shade. The leaves were ground
[1]
action or both. Medicinal plants have always into a fine powder using a domestic electric
been an essential part of the traditional healthcare grinder.
system around the globe to cure particular
[2]
ailments. The medicinal plants involved in Preparation of Plant Extracts
delaying the absorption of glucose by inhibiting The dried powder of leaves of J. Sambac was
the carbohydrate hydrolyzing enzymes and soxhlet extracted with methanol, chloroform, and
subsequently dulling the increase in postprandial distilled water. All the extracts were evaporated
plasma glucose. Several indigenous medicinal using rotary evaporator, under reduced pressure.
[3]
plants potential inhibit the α-amylase enzyme. The percentage yield of methanolic, chloroform
Jasminum sambac is frequently referred to as and aqueous extracts were 8.23%, 6.45%, and
mogra. It belongs to the oleaceae family and is 3.89%, respectively. All the three extracts were
distributed to the tropical and subtropical dissolved in DMSO to make different
[4]
regions. This study was carried out to evaluate concentrations and then α-amylase assay was
the in vitro inhibitory effect of various extracts performed.
(methanol, chloroform, and aqueous) of J. sambac
on porcine pancreatic amylase activity. α-amylase Inhibition Assay
α-amylase inhibitory activity of aqueous,
Materials and Methods methanolic and chloroform extract was studied by
α- amylase, methanol, chloroform, starch, 3,4- 3,5 dinitro salicylic acid method of Sangeetha with
[5]
dinitrosalicylic acid (DNS), sodium potassium slight modifications . Acarbose (50,
tartarate, sodium di-hydrogen phosphate, 75,100,125,150 µg/mL) was used as a positive
disodium hydrogen phosphate, sodium hydroxide, control. Each experiment was performed in
and acarbose were purchased from Loba Chemie, triplicates. The results were expressed as
India and Sigma -Aldrich, India. percentage inhibition and the α-amylase inhibitory
Plant Materials activity of ME, AE, CE, and acarbose were
The leaves of J. sambac were collected from the calculated and IC50 values were determined and
medicinal garden of Smriti College of statistical analysis was done and results are
Pharmaceutical Education, Indore. The expressed in terms of mean ± standard deviation.
authentication of the plant was done by Dr. S.D.
Upadhyaya, Professor & Head, Department of

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Results inhibitory activity with an IC50 values 63.78±0.04

Acarbose (at a concentration 150 μg/mL) showed μg/mL, and74.61±0.05/mL respectively.
81.28±0.1% α-amylase inhibitory activity with an Chloroform extract fails to produce α- amylase
IC50 value 86.33 ± 0.05 μg/mL *Table 1]. The inhibition. Both methanolic and aqueous extracts
methanol extract and aqueous extract of J. of J. sambac showed significant α-amylase
sambac (at a concentration 150 μg/mL) exhibited inhibitory activity when compared with acarbose
97.76±0.1 % , and 95.38±0.05 % of the α-amylase [Figure 1].

Table-1: Percentage of Alpha-amylase inhibitory activity of different extracts of J. sambac and standard
drug:acarbose
Percentage Inhibition
Extracts/Drug 50 75 100 µg/mL 125 µg/mL 150 µg/mL IC50
µg/mL µg/mL
ME 42.62± 0.1 56.25± 0.1 69.88±0.1 82.90±0.10 97.76±0.1 63.78±0.04
AE 34.48±0.1 51.30±0.05 65.16±0.05 80.53±0.12 95.38±0.05 74.61±0.05
Acarbose 32.75±0.01 44.04±0.10 56.76±0.01 68.59±0.15 81.28±0.1 86.33±0.05
ME-Methanolic Extract AE-Aqueous Extract

120
Percentage of Inhibition

100

60 ME
AE
40
Acarbose
20

0
50 75 100 125 150
Concentration (µg/mL)
ME-Methanolic Extract AE-Aqueous Extract
Figure-1: Percentage of Alpha-amylase inhibitory activity of methanolic extract, aqueous extract and standard
drug
Discussion aqueous, a methanolic extract shows the best α-
We compared IC50 values of α-amylase inhibitory amylase inhibitory activity.
effects of methanol, chloroform and
aqueous extracts of J. sambac. From the result, it Reference
was found that both methanolic and aqueous 1. Telagari M, Hullatti K: In-vitro α-amylase
extracts are potent inhibitor when compared to and α-glucosidase inhibitory activity of
acarbose and there was a dose-dependent Adiantum caudatum Linn. and Celosia
increase in percentage inhibitory activity against α- argentea Linn. extracts and fractions.
amylase. It may be due to the presence of Indian journal of pharmacology
flavonoids in ethanolic and aqueous extract of 2015;47(4):425.
leaves. 2. Tamil IG, Dineshkumar B, Nandhakumar
M, Senthilkumar M, Mitra A: In vitro study
Conclusion on α-amylase inhibitory activity of an
The present study indicated that J. sambac could Indian medicinal plant, Phyllanthus
be useful in the management of postprandial amarus. Indian journal of pharmacology
hyperglycemia. It can be concluded that out of 2010; 42(5):280.
three extracts i.e methanolic, chloroform and 3. Dubey K, Dubey R, Gupta R, Gupta A:
Anti-Diabetic Potential of Aqueous,

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Methanolic and Saponin Extract of Leaves extract of Jasminum sambac. Journal of

of Ziziphus nummlaria Linn. Journal of ethnopharmacology 2015;160:140-8.
Drug Delivery and Therapeutics 5. Sangeetha R, Vedasree N: In vitro α-
2017;7(7):173-4. amylase inhibitory activity of the leaves of
4. Sengar N, Joshi A, Prasad SK, Hemalatha Thespesia populnea. ISRN pharmacology
S: Anti-inflammatory, analgesic and anti- 2012;2012:1-4.
pyretic activities of standardized root

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FORMULATION AND EVALUATION OF HERBAL ANTITUSSIVE ASH SYRUP OF COCOS

NUSIFERA IN MICE
Ruchi Gupta1*, Rajiv Saxena 1, Kushagra Dubey1, Neelesh Malviya1
Smriti College of Pharmaceutical Education, Indore, M.P. (India)
[email protected]

ABSTRACT

Plant derived medicine plays an important role in the management of various disorders. These drugs are highly
effective and have none or very less side effect. Many newer formulation are developed with the use of herbal
drugs. The herbs ash is highly valued in Ayurvedic system of medication for Antitussive activity. The present
work has been carried out on the ash of endosperm of crocos nusifera syrup for their antitussive effect of
ammonium hydroxide induced cough model in mice. Crocos nucifera belongs to Arecaceae family. Tradition
data revealed the certain pharmacological action like antihelminthic activity, anti inflammatory activity,
antinociceptive ,antioxidant, antimicrobial, antibacterial and anti tumour activities were carried out . But not
much work carried on Antitussive activity. The main object of this research was to develop formulation of the
ash of endosperm of crocos nusifera syrup and subjected to evaluate its physicochemical and pharmacological
parameters. The result of antitussive ash syrup excihibited significant antitussive activity in dose dependent
manner against the standared drug diphenylhydramine HCL. It has been observed that the extract has
produced 55%, 75%, 80% reduction in cough bouts at the dose level of 1,2,3 respectively after 1 hour of drug
administration. The dose of 3ml was found to be very effective and it was found that antitussive activity
produced by the herbal formulation in the minimum dose was comparable as compare to the standard drug.
Keywords: Antitussive agent, Crocos nusifera, Citric acid, Diphenyl hydramine HCL, ammonium hydroxide

Introduction with the help of grinder. After weighing Cocos

Cough is a reflex action of respiratory diseases. nucifera ignite in muffle furnace at temperature
This is most important defensive and protective 250℃ in crucible disk. After igniation they
mechanism of respiratory tract system . Asthma converted into ash.
,bronchitis etc are all the respiratory tract disease Preparation of simple ash syrup
those action inhibits the entry of noxious As per B.P.(British Pharmacopoeia) prepared
substance, mucus and infection. Some demulcent 66.67% w/v of simple ash syrup. 200mg of ash of
and hydration of respiratory tract by steam Cocos nucifera. Honey were dissolve in simple
inhalation are prominent effective in reducing syrup I.P. and the volume was made up to 100ml
system in majority of case. Among cough and finally preservative was added.
suppressant opioids, codein, noscapine, Pharmacological Screening
diphenyhydramine HCL etc are effective but they Animals
have significant side effect like constipation, Mice (200-250 gm.) of either sex were used in
sedation, respiratory depression, drowsiness, experiments. The experimental animal was kept in
addiction. Literature of ash of Crocos Nusifera quarantine area for their acclimatization and then
showed promising cough suppressant activity but transferred to animal house. The animal house
no scientific evidence was available about it . was maintained with standard conditions of light
Hence the present research work is focused on as 12 hour day light and 12 hour dark along with
evaluation of antitussive activity of ash Crocos humidity conditions of 35-60% humidity was
Nusifera. maintained. The polyvinyl cages that do not have
more than 6 animals in each cage, was housed.
Experimental Materials Standard mice pellet diet and water ad libitum was
Ash of Cocos nucifera, ammonium hydroxide , given as animal feed. Institutional Animal Ethical
honey, diphenylhydralamine HCL. Committee approved the experimental protocol.
Collection and preparation of Ash of Crocos Every experimental procedure followed animal
nusifera ethical norms.
Ripe endosperm part of Cocos nucifera fruit For Antitussive activity of ash syrup of Crocos
purchase from the local market of the Indore. The Nusifera describe by D. Marina (Marina GD ) was
ripe endosperm part of Cocos nucifera fruit grind adopted to evaluate its

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International Journal of
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The mice were divided into 5 groups. frequency of cough bouts was monitor for 5
Group- I control group. minute this procedure was repeated for all treated
Group -II received Diphenhydramine hydrochloride group mice
(250mg/kg).
Group -III received 1ml formulated ash cough Statistical ANALYSIS
syrup of Cocos nucifera. Mean ±SD was used to express the result of
Group -IV received 2 ml formulated ash cough pharmacological studies. graph pad prism 5 project
syrup of Cocos nucifera. software one way ANOVA (Analysis of variance)
Group -V received 3 ml formulated ash cough which was followed by student t-test was used to
syrup of Cocos nucifera. evaluated the total variance present in the data p-
Pharmacological antitussive activity value less then 0.05 as compared to control
Ammonium hydroxide induced cough showed a statistically significant result.
Evaluation of the in-vivo antitussive activity against
ammonium hydroxide liquor induced cough was Result and Discussion
done. Mice were first selected then they were A prototype cough suppressant i.e. the
divided in five group among them Group one was diphenylhydralamine HCL was administered to
formed as a control. Standard drug (20mg/kg) was animals which is produced 55%, 75%, 80%
used to form group second .mice treated with ash inhibition of frequency of cough bouts which is
cough syrup of Cocos nucifera formed third group. induced by ammonium hydroxide after 60 minute.
all mice of each group where individual placed on As shown in below table dose dependent cough
wire gauze platform in dessicator after one hour of suppressant activity was shown by the ash syrup of
oral administration of test drug. Then they are Crocos Nusifera in multiple dose .a significant
exposed to 0.3ml ammonium hydroxide (25%) activity 3ml (82.45%)was shown by Crocos
which is generated by nebulizer for 45 second . Nusifera.
then immediately the mice were placed in
observation chamber where by a stopwatch

Table 1: Effect of ash syrup of Crocos Nusifera formulation on cough frequency in Ammonium liquor induced
cough mice
Experimental Treatment No. of Frequency of Percentage
Group animals cough bouts inhibition of cough
bouts
Group I Control 6 78.23±0.81 -
Group II Diphenhydramine hydrochloride 6 51.45±0.12* 58.23
Group III Ash cough syrup of Cocos nucifera. 6 24.24±0.32*** 60.12
Group IV Ash cough syrup of Cocos nucifera. 6 42.10±0.32* 52.36
Group V Ash cough syrup of Cocos nucifera. 6 28.30±0.08** 82.45
Values are Mean ± SEM, n=6, No. of animals in each group.
*p < 0.05, **p < 0.01, ***p<0.001 for comparison of treated groups vs control

Conclusion Reference
To conclude, our study indicate that the 1.Jeba Sunilson A, Anandarajagopal J, Khan
antitussive ash syrup of Crocos Nusifera Abdullah K, Khaja P, Bin HQ and Puspa V,
formulation exerted significant (p < 0.05) Kuna R, Antihistaminic evaluation of formulated
antitussive effect in experimentally induced cough polyherbal cough syrup, Journal of
reflex in mice comparable to the Diphenyl Medicinal Plants Research, 2010, 4(14), 18 (7),
hydramine HCL as a standard drug and provides 1482-1485.
pharmacological evidence for the traditional use of 2. Aragão WM. Côco: pós-colheita. Série frutas do
ash syrup of Crocos Nusifera as antitussive agents. Brasil. Brasília: Embrapa Informação Tecnológica;
Hence, additional research work relating to 2002. http://livraria.sct.embrapa.br/liv_resumos/p
evaluation of their mechanism of action for df/00070000.pdf [Google Scholar
antitussive effect should be carried out.

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PRELIMINARY PHYTOCHEMICAL ANALYSIS AND ANTIMICROBIAL ACTIVITY OF HERBAL

HAND SANITIZER GEL
Reena Guptaa,b, Jitendra Guptab, AshimaAhujab
a,b
Institute of Pharmaceutical Research, GLA University, Mathura-281406, U.P., India
[email protected]

ABSTRACT
Poly Herbal Hand Sanitizers (HHS)are prepared with an objective of maintaining proper “hand hygiene”. It
helps in the prevention, control & reduction of any acquired andNosocomialinfection that stops the
transmission of microorganisms from hands to other parts of body. With the emergency andusage of HHZ, side
effects like itching, irritation, contact dermatitis of synthetic hand sanitizer’s can be overcome. The present
research was aimed to study preliminary phytochemical analysis &formulate HHS gel of Tulsi,
Eucalyptus,Neem, Clove oiland evaluate their anti-microbial efficacy by agar plate diffusion method against E.
coli, Ps. aureogenosaandS. aureus. This work suggests the utilization &incorporation of traditional plant
materials in the gel formulation that support significant anti-microbial effects of HHS gel(800>400>200µg/mL)
in maintaining proper hygiene providing primitive tool in treatment, reduction of infections.
Keywords: Antimicrobial activity, Nosocomial infections, Herbal hand sanitizer.

Introduction: Skin being the highly exposed part of added to denatured alcohol, glycerin, polysorbate
human body requires protection against various 20 and dissolved in aqueous phase. Methyl and
pathogens due to increased no. of Nosocomial propyl parabenwere added along withperfume
4
infections resulting in extended hospitalization for and stored HHS (F1, F2) in air tight container .
better patient care with increased morbidity
1
&mortality . The hands of Health Care Workers Evaluation of herbal extracts and hhs gel
working in hospitals are the primary mode of Preliminary Phytochemical screening
transmission of pathogens promoting usage of The presence of phytoconstituents were identified
antiseptics for washing hands.Pathogenic in methanolic extracts of Neem,Tulsi &Eucalyptus
4,5
resistance is an emerging problem in public places having antimicrobial activity .
where an unhygienic condition promotes spreading Organoleptic properties
of diseases that can be minimized by using Organoleptic properties like color, odour,
HHSmade with traditionally available homogeneity &appearance were visualized by
2
antimicrobials . naked eyes.
pH
Materials and methods pH of HHSgel F1 and F2 were investigated using
Collection & Authentication of plants digital pH meter.
Neem, Eucalyptus, Tulsi leaves were authenticated Viscosity
in Dept. of Pharmacognosy, GLA University The viscosity of HHSweredoneusing Brookfield
Mathura after collection from herbal garden. viscometer, LV model, USA).
Pathogens such as Staphylococcus aureus (gram Spreadability
+ve), Pseudomonas aeruginosa (gram–ve) HHS (0.1g)was placed between two glass plates
&Escherichia coli (gram–ve) were selected for and measured the diameter after 1 minute using
testing of antimicrobial action. following formula.
Preparation of extracts S= (l x w)/t Where, S = Spreadability, w =
100g powdereddry leaves of Neem, Tulsi Weight, t- Time (in sec.) and l = Length
&Eucalyptus were extracted with 900 and 100 parts In-vitro Antimicrobial sensitivity test by agar plate
ᵒ
of methanol &water at 60 C for 1husing Soxhlet disc diffusion method
3
apparatus . The antimicrobial sensitivity test for screening of
Formulations of HHS Gel extracts &HHS using ciprofloxacin as standard
Carbopol in deionized water was were performed (agar plate disc diffusion) against
stirredcontinuously with slow addition of different microorganisms. The different
triethanolamine to avoid bubble formation, kept concentration of methanolic extracts of herbs,HHS
aside for 24 hrs. The methanolic extracts of Neem, (F1, F2) and standard were added into agar
Tulsi &Eucalyptus (Table 1) with clove oil were petriplate after inoculation of microorganism

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International Journal of
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andkept in an incubator. After two days, diameter antimicrobial activity against all the
of zone of inhibition (ZOI) was determined and microorganisms(800>400>200µg/mL) but
compared results against standard. formulation F2showed more potent, effective
Stability against S. aureus in comparison to F1 due to
Stability study HHS as per ICH guidelines were presence medicinally active phytoconstituentsthat
investigated after exposing to 25±C, 37±C interact and partition in to bacterial cell wall
&40±C for 12 weeks and observed for colour causescell death. Further, stability study depicts
6
change &phase separation . that formulations (F1,F2) were stable andhaving no
sign of colour changeandphase separation.
Result and discussions
Phytochemical screening of various methanolic Conclusion
extracts confirms the presence of HHS gel were prepared with an objective to
phytoconstituents(Table2)which is responsible for maintain proper health and hygiene. It provides
antimicrobial activity.Organoleptic properties of future for the commercial development of plant
HHS gel were examined(Table 3),that aredesired extract as HHS that are useful for herbal industry
for formulation of gelappearance, spreadingon to overcome the undesirable side effects of
hands.Results of in-vitro sensitivity test(Table synthetic hand sanitizers.
4),formulation (F1, F2) showed significant

Table 1: Composition of herbal hand sanitizer gels

Ingredients F1(%w/v) F2(%w/v)
Neem leaves extract 1 1
Tulsi leaves extract 1.5 -
Clove oil 0.5 0.5
Eucalyptus extract - 1.5
Carbopol 940 0.5 0.5
Alcohol denatured 62.2 62.2
Triethanolamine 0.7 0.7
Polysorbate 20 0.5 0.5
Glycerine 2.3 2.3
Preservative 0.5 0.5
Deionised water 30 30
Perfume 0.5 0.5
Table 2: Phytochemical analysis of various methanolic extracts
Phytoconstituents NE TE EE
Alkaloids + + +
Saponins + + +
Tannins + - -
Glycosides + + -
Flavonoids + + +
Reducing sugars + - +
Phenols + + +
Terpenoids - + +
Steroids + + +
Absent- (-), Present- (+), EE-Eucalyptus extract, TE-Tulsi extract, NE-Neem extra

Table 3: Physicochemical parameters of hhs gels

Viscosity Spreadability
a a a
Formulation Color Homogeneity Appearance Odour pH (Cps) (g.cm/sec.)
F1 CB Homogenous Translucent Characteristics 6.57±0.06 97±0.38 14±0.2
F2 CG Homogenous Translucent Characteristics 6.72±0.09 98±0.61 15±0.7
a
N=3±S.D., CB-Creamy brown, CG-Creamy green

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Table 4: Antimicrobial activity of extracts of herbs &hhs gel

†
Zone of Inhibition (mm)
St
Micro- EE (µg/mL) TE(µg/mL) CO(µg/mL) NE(µg/mL) F1(µg/mL) F2(µg/mL)
d.
organism
20 40 80 20 40 80 20 40 80 20 40 80 20 40 80 20 40 80 10
0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0
13 17 20 14 18 21 20 23 15 19 22 18 21 25 17 20 24 28
16
E. ± ± ± ± ± ± ± ± ± ± ± ± ± ± ± ± ± ±
±
Coli 0. 0. 0. 0. 0. 0. 0. 0. 0. 0. 0. 0. 0. 0. 0. 0. 0. 0.
0.3
2 4 3 5 2 4 5 4 2 3 6 5 4 3 2 5 3 4
10 14 11 15 11 16 12 16 12 17 19 10 15 18 25
Ps. 0.9
N ± ± N ± ± ± ± N ± ± ± ± ± ± ± ± ±
aerugi- ±
A 0. 0. A 0. 0. 0. 0. A 0. 0. 0. 0. 0. 0. 0. 0. 0.
nosa 0.1
5 3 3 2 6 2 4 2 3 4 5 3 2 4 5
16 20 22 17 21 23 21 25 18 22 24 23 25 28 19 22 26 32
18
S. ± ± ± ± ± ± ± ± ± ± ± ± ± ± ± ± ± ±
±
Aureus 0. 0. 0. 0. 0. 0. 0. 0. 0. 0. 0. 0. 0. 0. 0. 0. 0. 0.
0.4
7 2 5 6 7 3 2 4 3 5 4 5 3 4 7 4 5 4
†
N=3±S.D., NA-No activity, EE-Eucalyptus extract, TE-Tulsi extract, CO-Clove oil, NE Neem extract

References physicochemical analysis: A poly

1. Black J: Microbiology: Principles & herbomineral Formulation. Inter. J. Drug
Applications, New Jersey, 1996; (3): 436- Develop. Research 2014, 6(3):85-92.
443. 4. Kokate CK, Purohit AP and Gokhale SB:
2. Nandkishor SW and Bhalerao: Pharmacognosy, NiraliPrakashan, Pune,
Formulation & Evaluation of Herbal 1999, (2) 181,213, 216, 224, 279, 315,
Sanitizer. Inter. J. Pharm. Tech. 2013; 322, 390, 425-427, 593-597.
5(1):40-43. 5. ICH guidelines, Stability testing of new
3. Gupta R, Gupta MK, Bhandari A and drug substances and products, 27th
Gupta J: Preliminary pharmacognostical& October,

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EFFECT OF EXTRACT OF CENTELLA ASIATICA ON INFLAMAMATION: AN IN VIVO STUDY

Ashish Pagariya*, Neetesh K Jain, Mahavir Chhajed
Oriental University, Gate No.1, Sanwer Road, Jakhya, Opposite Revati Range, Indore, M.P.
(India)
[email protected]

ABSTRACT
The methanolic extract of Centella asiatica (MECA) (200 mg/kg) significantly (p<0.01) inhibited carrageenan
induced rat paw edema as compared to control group. Maximum inhibition of rat paw edema was observed
with MECA (400 mg/kg) at the end of 4 h when compared to control group. For the acute inflammatory
condition, MECA was evaluated by carrageenan induced rat paw edema model. MECA showed moderate to
potent significant activity in dose dependant manner compared to standard indomethacin. Methanolic extract
was further selected for the fractionization and isolation of active constituents. No toxic effects were observed
at a higher dose of 2000 mg/kg body weight of Wistar rats.
Keywords: Centella asiatica, extract, anti-inflammatory

Introduction scheme of medicine and other system of

Inflammation is an important physiological medicines, which have been widely useful as in the
response which arises in rejoinder to a ample treatment of inflammation. In the absence of any
assortment of injurious mediators (e.g. bacterial scientific evidence for their anti-inflammatory
infection, physical trauma, chemicals or any other activity in acute and chronic inflammatory
1
phenomenon). Inflammatory processes are conditions, there is a need in scientifically
required for immune surveillance, optimal repair, establishing the anti-inflammatory activity so that
2
and regeneration after injury. The inflammatory we are able to come up with a more effective and
process protects our body from diseases by potent bioactive phytoconstituents with less side
releasing cells and mediators that combat foreign effects in comparison with existing synthetic
3-4
substances and avoid infection. However, drugs. C. asiatica has potent antioxidant and anti-
sustained, excessive or inappropriate dermatitic effect. However, its anti-inflammatory
inflammation is the cause of abundant diseases properties have not been reported so far. In this
including rheumatoid arthritis, psoriasis and study, we investigated the anti-inflammatory
5
inflammatory bowel disease. Inflammation is a effects methanolic extract of C. asiatica (MECA) in
major component of the damage caused by a caragennan induced rat paw edema animal
autoimmune diseases, and is a fundamental model.
provider of various infectious and non-infectious
diseases such as cancer, diabetes, cardiovascular Materials and methods
disease, rheumatoid arthritis, Alzheimer’s and The leaves of C. asiatica were collected in the
arteriosclerosis. month of March from Medicinal Garden (Nursery),
Corticosteroids reduce inflammation or swelling by Mandsaur. All the plant materials were
binding to corticoid receptors. NSAIDs typically taxonomically authenticated and by Dr. S. N.
alleviate inflammation and associated pain by Dwivwdi, Botanist, Janta PG college, APS
inhibiting COX involved in the production of University, Rewa. The specimen herbarium sheets
prostaglandins. Long-term corticosteroids use has were submitted and preserve in Department.
several severe side effects eg. Hyperglycemia,
insulin resistance, diabetes mellitus, osteoporosis, Preparation of Methanolic Extract
6
anxiety effects etc.. NSAID use is associated with a All the plant materials were dried under shade and
high risk of upper gastrointestinal symptoms and subjected to coarse powder for extraction process.
lesions such as oesophagitis, gastritis, peptic Accurately weighed quantity of leaf powder of C.
ulcers, and their severe complications including asiatica was extracted using 95 % methanol by
bleeding and perforation. soxhlet apparatus for 72 h. The extract was dried
India is a rich foundation of medicinal plants and a under the reduced pressure to get crude extract.
number of plant derived extracts are used against After drying, weighed and percentage yield was
8
diseases in a variety of systems of medicine. There determined.
are various reported medicinal plants in traditional

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International Journal of
Pharmaceutical Sciences and Research
ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

th
Preliminary Phytochemical Tests plethysmograph at 0, 1, 2, 3, 4 and 5 h after
11
Qualitative chemical tests of Methanolic extract injection.
was subjected to various chemical tests to detect
9-10
various phytoconstituents. Measurements of paw volume
The severity of adjuvant arthritis was quantified by
Preliminary In-Vivo Anti-inflammatoryActivity measuring the volume of the hind paw by means
of Plethysmograph. Paw volume (mL) was
Selection of animals measured at 0 days and thereafter 4, 8, 12, 16 and
6-7
Wistar albino rats of either sex between 2 and 3 21 days of FCA post-inoculation. .
months of age weighing 150-200 gm were Percentage inhibition=Vc-Vt/Vt×100
selected. All animals were housed under normal Where, Vc-Paw volume of control animals; Vt-Paw
0
condition of 25±1 C, 12 hr light and dark cycle. volume of treated animals

Acute toxicity studies Statistical Analysis

The acute oral toxicity study was approved as per The results were analyzed by ANOVA followed by
the OECD guidelines, revised draft 423. All extracts Dunnet’s "t” test to decide the statistical
were prepared as a suspension by triturating dried significance. p<0.05 was selected as the level of
extracts with 1% Tween 80 in distilled water. Prior significance.
to dosing, animals were fasted for 12 h and water
given ad libitum. Animals were weighed and test Results and Discussion
substance was administered at dose of 2000
mg/kg p.o. In first step, each dose was tested on Acute Toxicity Studies of Extract & Fractions
single rat and then administered to other rats. No toxic effects were observed at a higher dose of
Observation was made during the first four hours 2000 mg/kg body weight. Hence, 1/ 10th dose was
after the drug administration to notice change in selected as therapeutic dose. The cut off value of
skin, fur, eye, mucus membrane, hyperactivity, 200 and 1/5 dose double of 400 mg/kg were
grooming, convulsions, sedation, hypothermia, selected for anti-inflammatory activity to assess
tremor, salivation, coma, lethargy, body weight the dose dependent action for the evaluation of
and mortality up to 14 days. antiarthritic activity.

Evaluation of anti-inflammatory activity Anti-inflammatory Activity of Extract

Animals were divided into 7 groups and each The methanolic extract of Centella asiatica (200
group contains 6 animals. The animal groups and mg/kg) significantly (p<0.01) inhibited carrageenan
treatment schedule are reported in table 1. induced rat paw edema as compared to control
Inflammation was induced by 0.1 mL of 1% group. Maximum inhibition of rat paw edema was
suspension of carrageenan into hind paw of rat by observed with methanolic extract of plant (400
sub planter route. Treatments of all fractions were mg/kg) at the end of 4 hr when compared to
given 1 h prior to administration of carrageenan. control group. Indomethacin (10 mg/kg) highly
Paw volume was measured with digital significantly inhibited the paw edema in
inflammatory rats.

Table No 1: Effect of monoterpenes on carrageenan induced rat paw edema

#
S. Groups Treatment Paw Volume in mL
No. 0h 1h 2h 3h 4h
1 NC NS 5 ml/kg 0.34±0.12 0.33±0.11 0.32±0.11 0.34±0.11 0.36±0.12
2 DC -- 0.33±0.11 0.47±0.14* 0.82±0.24** 0.94±0.18*** 0.87±0.20***
3 MECA 200 mg/kg 0.35±0.18 0.41±0.18 0.46±0.11** 0.53±0.23** 0.59±0.19**
4 MECA 400 mg/kg 0.32±0.13 0.39±0.12* 0.44±0.17*** 0.51±0.11*** 0.54±0.07***
5 Std. 10 mg/kg 0.32±0.12 0.37±0.05* 0.41±0.07*** 0.47±0.04*** 0.49±0.02***
# all dose administered p.o., Standard used was Indomethacin. NC: Normal Control. DC: Disease control. NS:
Normal saline, Values are expressed as mean±SEM, n=6 in each group; * p <0.05, ** p<0.01, *** p <0.001,
compared to disease control

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Figure No1. Effect of methanolic extract on paw volume in carrageenan induced paw edema

Conclusion (2010). Synthesis and anti-inflammatory

In the preliminary study, dried powders of plant activity of novel (substituted) benzylidene
was extracted by using methanol. The extract was acetone oxime ether derivatives:
dried and screened for the presence of various molecular modeling study. Eur J Med
active constituents. The extract showed the Chem. 45: 1403-1414.
presence of alkaloids, terpenoids, flavonoids, 5. Franklin PX, Pillai AD, Rathod PD, Yerande
glycosides, phenolic compounds, tannins, steroids S, Nivsarkar M, Padh H, Vasu KK,
and fatty acids. Acute oral toxicity studies of MECA Sudarsanam V (2008). 2-Amino-5-thiazolyl
was carried out and no toxic effects i.e. motif: a novel scaffold for designing anti-
hypersensitivity reactions, diarrhoea, itching, inflammatory agents of diverse
behavioral changes and mortality at the dose of structures. Eur J Med Chem. 43: 129-134.
2000 mg/kg body weight was seen. Hence, 1/10th 6. Donihi AC, Raval D, Saul M, Korytkowski
(200 mg/kg) and 1/5 (400 mg/kg) of the lethal MT, DeVita MA (2006). Prevalence and
dose were selected as effective dose for further predictors of corticosteroid-related
acute inflammatory activities. For the acute hyperglycemia in hospitalized patients.
inflammatory condition, MECA was evaluated by Endocrine Practice 12: 358-362.
carrageenan induced rat paw edema model. MECA 7. Cryer B, Kimmey MB (1998).
showed moderate to potent significant activity in Gastrointestinal side effects of
dose dependant manner compared to standard nonsteroidal anti-inflammatory drugs.
indomethacin. Methanolic extract was further The American J Med. 105: 20S-30S.
selected for the fractionization and isolation of 8. Mukherjee, P.K., 2002. Quality Control of
active constituents. Herbal Drugs-an Approach to Evaluation
of Botanicals. New Delhi, Business
References Horizons Pharmaceutical Publishers
1. Nathan C (2002). Points of control in 9. Kokate, C.K., 1996, Practical
inflammation. Nature 420: 846-852. Pharmacognosy. Delhi, Vallabh
2. Vodovotz Y, Csete M, Bartels J, Chang S, Prakashan.
An G (2008). Translational systems 10. Khandelwal, K.R., 2006. Practical
biology of inflammation. PLoS Pharmacognosy. Pune, Nirali Prakashan.
Computational Biol. 4: 1-6. 11. Arulmozhi, S., Mazumdar, P.M.,
3. Frank MM, Fries LF (1991). The role of Sathiyanarayanan, L., Thakurdesai, P.A.,
complement in inflammation and 2011. Anti-arthritic and antioxidant
phagocytosis. Immunology Today 12: 322- activity of leaves of Alstonia scholaris
326. Linn. R.Br. Eur J Integ Med, Vol. 3, pp.
4. El-Gamal MI, Bayomi SM, El-Ashry SM, e83–e90.
Said SA, Abdel-Aziz AA, Abdel-Aziz NI

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PHYTOCHEMICAL SCREENING AND HEPATOPROTECTIVE EFFECT OF HYDROALCOHOLIC

EXTRACT OF OXALIS CORNICULATA LINN IN MICE
Kanchan Mathur1,2,Reena Gupta*1, Jitendra Gupta1
*1Institute of Pharmaceutical Research, GLA University, Mathura-281406, U.P., India
2
Monad College of Pharmacy, Monad University, District Hapur- - 245304, U.P., India
[email protected]

ABSTRACT
There are number of herbal formulations that found its acceptance in Indian herbal medicine having
hepatoprotective effect. Oxalis corniculata Linn (oxalidaceae) is a native herbal plant product of Himalayan
region, that promotes the usage of safe, effective and potent drug in management of liver disorders. The
present research work is aimed to evaluate the effect of whole plant of Oxalis corniculata as hepatoprotective
and to prove the efficacy of herbal hydroalcoholic extract of O. corniculata (HEOC) using paracetamol induced
hepatotoxicity in animal model. Results of preliminary phytochemical screening demonstrates that intake of
Paracetamol causes increase in the level of serum bilirubin, SGPT, SGOT and reduction in triglycerides levels
indicating considerable liver toxicity. Administration of herbal HEOC at dose 400mg/kg body weight in animal
model found to have significant hepatoprotective effect due to presence of flavonoids, beta catotene,
glycoside and tannins.
Keywords: Hepatotoxicity, Herbal hydroalcoholic extract, Paracetamol

Introduction group 3 (100mg/kg), and Group 4, 5 animals were

Herbal formulations have become a potent store given HEOC extract (200 mg/kg and 400 mg/kg) 14
th
house of remedies against majority of ailments days respectively. On 14 day all the groups were
found in human body that contributes the treated with Paracetamol (PCM) suspension
importance of herbal extract as botanical, (100mg/kg) except control group, animals were
1
chemical & pharmacological origin . It is widely sacrificed after 36 hours of the experiment and
distributed in temperate and warmer regions blood samples were withdrawn for biochemical
5
throughout India. Liver disorders is one of major estimation of serum .
health hazard that are prominently found in
developing countries due to poor eating habits, Evaluation hydroalcoholic extract of Oxalis
over consumption of alcohol, smoking and corniculata
unhygienic surrounding impacting human health Preliminary Phytochemical Screening: The
2,3,4
and reduces life expectancy . presence of flavonoids, tannins, carbohydrates as
phytoconstituents subjected to antioxidant and
6
Materials and methods hepatoprotective effect of HEOC extract.
Collection and Authentication of plants Biochemical Estimation: Animals were
Drugs Silymarin and Paracetamol as a gift sample anaesthetized after 36 hours using chloroform,
was received from Advik laboratories, Gurgaon; blood samples were collected and coagulated at
Haryana. Whole plants of Oxalis corniculatawas room temperature for separation of serum and
collected from the herbal garden of Kurukshetra centrifuged at 2500rpm for biochemical analysis of
University, and authentifiedby NISCAIR (New Serum glutamate oxaloacetic transaminase
Delhi), India(NISCAIR/RHMD/Consult/-2009- (SGOT), Serum glutamate pyruvic transaminase
10/1345/147). Albino mice weighing 25-30g were (SGPT), Bilirubin and total protein. Liver of mices
selected for study as per CPSCSEA guidelines [Reg. were taken subsequently washed with normal
No. 235/CPCSEA]. HEOC extract of Oxalis saline for further study.
corniculatawas extracted for 48hrs by soxhlet Statistical analysis:The results were investigated
extraction by one-way analysis of variance followed by
Experimental Study Design Student’s t-test with Graph Pad Prism (5 project
Five groups were selected for the experimental software). The results were considered statistically
7
analysis containing six animals each. Group 1 and 2 significant when p< 0.01, p< 0.05 versus control.
animals treated as control and were administered Results and discussions
with 2% tween-80(1ml/kg, body weight, p.o.). Preliminary phytochemical screening confirms the
Salimyrin as a standard drug was administered to presence of glycoside, tanninsand

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carbohydrates(Table 1). Result of biochemical O.curiculata was successfully used for targeting
estimation showed dose dependent liver disorders (Table 2).
hepatoprotective effect in animal model. Further
the administration of paracetamol at 400mg/kg Conclusion
showed maximum and significant It was concluded that HEOH extract of Oxalis
hepatoprotective effects as compared to curiculata serves as potential herbericous plant
200mg/kg showing increased levels of total having significant hepatoprotective effects in
proteins, SGPT, SGOT, bilirubin where HEOH of combating liver disorders.

Table 1. Physicochemical screening of heoh extract

Phytoconstituents HEOH Extract
Alkaloids -
Glycoside +
Tannins +
Carbohydrates +
Flavonoids +
Absent: (-), present :(+), HEOH: hydroalcoholic extract of O. corniculata

Table 2. Biochemical estimation of heoh extract.

a a a a
Groups Dose SGPT SGOT Total protein Bilirubin
** **
Control 1ml/kg 79.140 ±4.39** 87.178±4.40 10.798±0.5806 1.186±0.074
PCM 100mg/kg 244.95±18.4** 289.7±30.2** 8.763±0.99 1.688± 0.1804
Salimyrin 100mg/kg 96.612 ±1.77** 82.478±3.3** 22.088±5.344 0.8180±0.04200
HEOH 200mg/kg 180.26 ±6.78** 141.7±24.9** 14.024±2.497 0.9500±0.04382
extract 400mg/kg 106.13 ±8.16** 116.±5.68** 17.845±7.348 0.9040±0.02676
a
N=3±SEM.,**p< 0.01, *p<0.05, SGOT: Serum glutamateoxaloacetic transaminase, SGPT: Serum glutamate
pyruvic transaminase, PCM: Paracetamol

References Digestive Diseases,2018; 4(3): 1-4.

1. SinghV and Pandey RP: Ethnobotany of 5. Das K, Kathiriya AK,Kumar EP, Benson MK and
Rajasthan, Scientific Publishers India, 2008: John WE: Evaluation of hepatoprotective
164-165. activity of aqueous and ethanolic extract
2. Trease GE and Evans WC: Pharmacognosy, of Oxalis corniculata against intoxication of
Elsevier Toronto: Edinburgh London New York thioacetamide induced rats. Brazilian Journal
Philadelphia St Louis Sydney, 2007;21: 477. of Pharmacognosy 2012; 22(2):412-417.
3. Rastogi RP and Mehrotra BN: Compendium of 6. Kokate CK, Purohit AP and Gokhale SB:
Indian medicinal plant. NISCAIR Press, New Pharmacognosy, NiraliPrakashan, Pune,
Delhi. 1979; (2):502-503. 1999;(2) 181,213,216, 224, 279, 315, 322, 390,
4. Srivastava R and SrivastavaP: Hepatotoxicity 425-427, 593-597.
and the role of some herbal hepatoprotective
plants in present scenario. Global Journal of

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FORMULATION AND EVALUATION OF HERBAL ANTIDANDRUFF POWDER SHAMPOO

Prerna Sharma, Nidhi Rani, Vikas Sharma, Vivek Dhiman
MM School Of Pharmacy, MM University, Sadopur (Ambala), Haryana, India 133001

ABSTRACT
In today’s scenario, synthetic formulations have occupied a huge part in our life. Day by day, people are
becoming dependent on these formulations. But these synthetic formulations are associated with a wide
range of side effects. To overcome these side effects, Ayurvedic formulations came into existence. In case of
hair disorders like dandruff problem, herbal powder shampoo has been formulated to fight against dandruff
.This herbal shampoo was formulated using natural ingredients with proven hair care properties. The
formulation at laboratory scale was done and evaluated for number of parameters to ensure its safety and
efficacy.
Keywords: Herbal Shampoo, Dandruff, Evaluation.

Introduction synthetic additives, skin friendly and no petroleum

Shampoo is a hair cleansing product used for based ingredients [4]. To overcome these vast side
dandruff treatment, hair coloring, management of effects, we have prepared a multipurpose powder
gluten or wheat allergies [1]. Herbal shampoos are shampoo for hair problem treatment.
the cosmetic preparations containing ayurvedic
herbs. They are used for removal of oils, dandruff, Materials and methods
dirt, pollution etc. Powder shampoos have the Procurement of Material
advantage over liquid shampoo of being spill-proof The different parts of the plants selected for the
and easy to apply [2,3]. Herbal shampoos have study were procured from Herbal garden of MM
number of advantages over synthetic shampoo. University, Sadopur-Ambala. Various ingredients,
They contain pure and organic ingredients, free their concentration and properties have been
from side effects, no harmful surfactants, no reported in Table 1.

Table 1: Formula of the herbal shampoo along with the biological source and Properties of the ingredients.
Concentration Ingredient [3] Biological name [2] Properties of
[1] ingredient
0.3% Mustard Dried seeds, Brassica nigra Anti- dandruff
(Brassicaceae) property.
0.3% Ashwagandha Dried stems, Withania somnifera Hair shining
(Solanaceae) property.
0.3% Henna Dried leaves Lawsonia inemis Works as pH
(Lythraceae) balancer.
0.5% Chandan Dried heartwood, Santalum album Provides fragrance
(Santalaceae) to the formulation.
1% Aloe vera Dried leaf extract Aloe barbadensis Prevents Hair fall.
(Lilliaceae)
1% Amla Dried fruits, Emblica officinalis Hair Growth
(Euphorbiaceae) Property.
42% Reetha Dried fruits, Sapindustri foliates Acts as surfactant.
(Sapindaceae)

Procedure
Evaluation of Herbal Powder Shampoo [6-11].
Preparation of Powder Shampoo. All the The prepared powder shampoo was subjected to
ingredients of herbal shampoo were air dried, various evaluation parameters such as
reduced to very fine ingredient, weighed according organoleptic evaluation, general powder
to the formula and mixed. The powder mixture characteristics, physic-chemical evaluation and
was then passed through sieve number 80 in order extractive values.
to get sufficiently fine powder [4,5].

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Result and Discussion

Preparation of the Herbal Shampoo Evaluation
The ingredients for the shampoo were air dried, Various properties such as organoleptic, general
reduced to fine powder, weighed, mixed and powder characteristics, physicochemical and
sieved through sieve number 80 in order to find extractive properties have been reported in tables
sufficiently fine and uniform powder. 2.
Table 2: Properties of shampoo
1. Organoleptic Properties 2. General powder characteristics
Color Light Brown Particle Size 150-180um
Odor Characteristic Angle of repose 19.7
3
Taste Bitter Bulk density 0.52g/cm
3
Texture Fine & amorphopus Tapped Density 0.56g/cm
3. Physiochemical Properties 4. Extractive Properties
Washability Easily Washable Alcohol soluble 13.9%w/w
Solubility Slightly soluble Water soluble 12.01%w/w
Loss on drying 86% Ash Value 7%w/w
Skin irritation No harmful effect on skin Wetting Time 5.37s
Stability Stable
Foaming Index 142.8%

Conclusion safety of Anti Dandruff Shampoo in the

The above research study represents a number of treatment of dandruff. The Antiseptic
plant drugs that can be used to treat several hair 2005;102:1-5.
related problems. Based upon the traditional 5. Manikar, Jolly. International Journals of
knowledge of herbal drugs, herbal powder Cosmetic Sciences. 2000;22(5):385- 91.
shampoo was formulated. The study has widened 6. Parry M E, Sharpe G R. Seborrheic Dermatitis
the scope for developing herbal powder shampoos is not caused by an altered immune
for treating various scalp diseases. response to Malssezia yeast. Br J Dermatol
1998;139:254-63.
Reference 7. McGrath J, Murphy G M. The control of
1. Kokate C K, Purohit A P, Gokhale S B. A text seborrhoeic dermatitis and dandruff by
book of Pharmacognosy. published by Nirali antipityrosporal drugs. Drugs 1991;41:178-
Prakashan,2017,9.71-9.73, 10.4-10.5, 9.9- 84.
9.16, 15.77-15.79, 9.103-9.104. 8. Sharma P P. Cosmetics- Formulation,
2. Ali Mohammad. A text book of Manufacturing and Quality control,703.
pharmacognosy, Published by CBS 9. Kokate C K. Practical Pharmacognosy,
Publishers & distributors, 2008, 143-149. Vallabh Prakashan, New Delhi, 1994,123,
3. Rangari Vinod. A text book of 10. Evans W C. Pharmacognosy, 16th Ed.,
pharmacognosy & phytochemistry, Harcourt Brace and Company,1997,128.
Published by Career publications, 2012, 11. Khandelwal KR. Practical Pharmacognosy
103-109, 489-491. Techniques & Experiment. Nirali Prakashan
4. Ravichandran G, Bharadwaj S V, Kolhapure S 2008, 102,106.
A. Evaluation of the clinical efficacy and

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REPELLENT EFFICACY OF SOME ESSENTIAL OILS AGAINST THE MOSQUITO

Deepak Kumar Gupta*, Revathi A. Gupta
Dr. A.P.J. Abdul Kalam University, Indore
Bypass Road, Arandia Village, Post Jhalaria, Indore
Madhya Pradesh - 452016
[email protected]

ABSTRACT
The present study was carried out to establish the mosquito repellent efficacy of certain selected plant
materials in order to obtain safe and effective herbal mosquito repellent formulations by combining selected
plant materials. I have used essential oils of all selected plant. Essential oils of Origanum
Majorana(Marua/Marwa), Tanacetum Cinerarifolium(Pyrethrum), Juniperus Communis (Aiteal), Scented
Geranium(Pelargonium), Thuja Occidentalis L. ( Arbor Vitae,White Cedor/Yellow Cedor), Tecoma Stans (L.) Juss.
Ex Kunth (Piliya/ Pila Kaner/ Yellow Bells, Artenmisia Arborescent(Worm Wood/ Mugworts, And Calamintha
Acinos(Thyme Basil) were Purchased from a reliable source. essential oil containing ethanol solutions was
prepared by 10 percent (V / V percent) of each plant essential oil and mosquito repellent activity testing was
carried out using arm-in-cage method. Volunteer's forearm, rubbed with 1 ml of the test solution, was exposed
to the cage where 25 blood-seeking mosquitoes were placed and the number of mosquitoes aligning or biting
the arm was recorded for five minutes in each minute. For each essential oil containing ethanol solutions,
three replicates were performed. A mosquito repellent formulation 16 percent (V / V percent) after analyzing
the mosquito repellent activity of individual essential oils. Outdoor and indoor field trials were performed
between 5 p.m. and 10 p.m. in two days by applying the mosquito repellent formulation on the legs of
volunteers. This formulation showed 100% mosquito repellence for outdoor and indoor field studies that were
conducted for two days for 5 hours each day.
Keywords: Mosquito repellent activity, Essential oil

Introduction Since most of the mosquito repellent products and

The WHO (world health organisation) reports the devices on the market have reported harmful
mosquito-borne malaria, a parasitic disease. effects on humans, the aim of this study is to
Mosquitoes are parasites and pathogens that are develop effective mosquito repellent products
transmitted. They spread disease such as malaria, based on plants.
chikungunya, and dengue. Mosquito can transmit
malaria to more than 700 million people Materials and methods
worldwide each year, 3 million of whom cost a The plant selection was based on survey of the
lifetime for malaria, including 2 children per different literature and its availability of essential
minute. Infants and young children experience oils, scientific evidence, and folkloric use as
nearly 90% of the mortality attributed to it. repellents for mosquitoes.
Mosquito control and personal protection from Essential oils of Origanum
mosquito bites are currently the most important Majorana(Marua/Marwa), Tanacetum
measure to control this disease. It is necessary to Cinerarifolium(Pyrethrum), Juniperus Communis
use the correct mosquito repellent to prevent (Aiteal), Scented Geranium(Pelargonium),
disease. Throughout the world, scientists are Thuja Occidentalis L. ( Arbor Vitae,White
trying to create a safe and effective malaria Cedor/Yellow Cedor), Tecoma Stans (L.) Juss. Ex
vaccine. But there is still no authorized vaccine for Kunth (Piliya/ Pila Kaner/ Yellow Bells, Artenmisia
human use for malaria. Considering the severity of Arborescent(Worm Wood/ Mugworts, And
malaria, the current research will highlight the Calamintha Acinos(Thyme Basil) were Purchased
preventive approach to malaria. In various from a reliable source.
traditional resources, such as Ayurveda, various
herbal sources with mosquito repellent activities Preparation of the test solutions
[1-2]
have been claimed. Using each plant essential oil, 10% (v / v percent)
of plant essential oil containing ethanol solutions
The objective of the study were prepared. Three drops of Tween 80 were
mixed with 0.3 ml of each plant extract or essential

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oil. Ethanol was then added up to 3 ml of volume. host-seeking and the experiment on repellency
Ethanol was applied to 3 drops of Tween 80 to continued.The forearm of Volunteer rubbed with 1
prepare the test solution until the amount was 3 ml of the test solution was exposed to the cage
ml. and the number of mosquitoes aligning or biting
the arm was recorded for 5 minutes in each
Testing the mosquito repellent activity of plant minute. Mosquitoes were given an interval of
essential oils using arm-in-cage method more than one hour and for each of the other
The mosquitoes used in this experiment were plant extracts and essential oils the above protocol
caught between 7 p.m. and 10 p.m. using a net was followed.
while biting people. Mosquitoes have been hungry
for 24 hours and 20 mosquitoes have been placed Results and discussion
in the cage (45×15×30 cm). Research schedule was Percentage the mosquito repellency for plant
between 7 p.m. and 10 p.m. as typically the extract/essential oil shown in Table was calculated
mosquitoes strike at night. Before the experiment, as below,
the mosquitoes ' host-seeking behaviour was Percentage mosquito repellency =C-N/C×100,
tested. This was done by placing a pre-cleaned Where, C= Number of mosquitoes aligned/left and
hand in the cage and counting within 10 seconds aligned/bit when the solvent was used= Number
the number of mosquitoes that aligned. If at least of mosquitoes aligned/left and aligned/bit when
5 mosquitoes were aligned on the hand, the the extract or the essential oil was used
mosquitoes inside the cage were considered to be

Table 1: Mean values of the mosquitoes aligned/left and aligned/bit for plant essential oils and mosquito
repellency (percentages) of plant essential oils
Essential Oils Replicate 1 Replicate 2 Replicate 3 Calculated Percentage
Total Number Total Number Total Number Mean Value Mosquito
of of of of Repellency
Mosquitoes Mosquitoes Mosquitoes Mosquitoes (%)
Aligned/Left Aligned/Left Aligned/Left Aligned/Left
and and and and
Aligned/Bit Aligned/Bit Aligned/Bit Aligned/Bit
Origanum Majorana 0 1 0 0.33 97.94
10 %( V/V %)
Pyrethrum 4 2 3 3.00 81.25
10 %( V/V %)
Juniperus Communis 2 3 0 1.67 89.56
10 %( V/V %)
Scented Geranium 3 1 3 2.33 85.44
10 %( V/V %)
Thuja Occidentalis L 0 0 0 0.00 100
10 %( V/V %)
Tecoma Stans 1 2 0 1.00 93.75
10 %( V/V %)
Artenmisia Arborescent 0 0 0 0.00 100
10 %( V/V %)
Calamintha Acinos 1 0 1 0.67 95.81
10 %( V/V %)
Solvent (Ethanol and 18 14 16 16.00 0.00
Tween 80)

Analysis was carried out as a triplicate and Acinos(95.81%) > Juniperus Communis(89.56) >
mosquito repellent activities were found to be in Scented Geranium(85.44%) > Pyrethrum(81.25%).
the order: Thuja Occidentalis L.and Artenmisia Many researchers have shown that essential plant
Arborescent(100%) > Origanum Majorana(97.94%) oils are more efficient in repelling than extracts
> Tecoma Stans(93.75%) > Calamintha from plants. All the essential oils are highly

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volatile, however, and this contributes as Ecological Considerations for the Armed
mosquito repellents to their poor longevity. No Force.MAFI 2007;63:112-114.
skin irritations or rashes with herbs, essential oils . 3. Adeniran O. I.and F.E.A cream formulation
of an effective mosquito repellent: a
Conclusion topical product from lemongrass oil
Compared to plant extracts, plant essential oils (Cymbopogon citratus) Stapf”Journal of
had higher mosquito repellent activity according Natural Product and Plant Resourse.2012;
to the survey and research we are using 8 type of 2(2):322-327.
essential oil for the study of mosquito repellent 4. Sharma S., Jadon U.A Review on low cost
activity then Analysis was carried out as a triplicate herbal Mosquito repellent from Begunia
and mosquito repellent activities were found to be Leaf, IJARPB.2011; 1(1):17-21.
in the order: Thuja Occidentalis L.and Artenmisia 5. Solomon B, Sahle F.F, Gebre-Mariam T,
Arborescent(100%)> Origanum Asres K, Neubett R.H.Microencapsulation
Majorana(97.94%)> of citronella oil for mosquito-repellent
Tecoma Stans(93.75%)> Calamintha application: Formulation and in vitro
Acinos(95.81%)> Juniperus Communis(89.56)> permeation studies, European Journal of
Scented Geranium(85.44%)> Pyrethrum(81.25%). Pharmaceutics and
Biopharmaceutics.2012;80(1):61-66.
References 6. Adia M.M., Anywar G., Byamukama R.,
1. Karande M.K., Chavare D. S. Malaria a Life Mugisha M. K., Sekegya Y., Kakudidi E.K.,
Threatening Disease, Research Front.2014; Kiremire B.T. Medicinal Plants used in
2:79-84. malaria treatment by prometra herbalists
2. Jaiswal P, Srinivasan S, Mehta V K,Banerjee in Uganda, Journal of Ethno pharmacology,
A, Acharya I.Malaria on the move: 2014;155: 580-588.

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PHYTOCHEMICAL EVALUATION AND ANTIOXIDANT ACTIVITY OF LEAVES OF

CINNAMOMUM TAMALA
Ishan Dubey , Manmeet Singh Saluja2, Mahavir Chhajed3, R.K.Singh2
1*
1
department Of Pharmacy, Suresh Gyan Vihaar Univerity, Jaipur, Rajasthan, India, 2central
Drug Research Institute, Lucknow, Up, India, 3university Institute of Pharmacy, Oriental
University, Opp. Rewati Range, Jakhya, Indore, MP, India
[email protected]

ABSTRACT
The constituents which inhibit oxidation are known as Antioxidants, they act by removing the potentially
damaging oxidizing agents in a living organism. It is highly critical to know about the phytoconstituents
responsible for antioxidant activity. In the present study, the DPPH radicalscavenging, Nitric oxide radical
scavenging by different extracts ofCinnamomumtamala, Madhucalongifolia andAdina cordifolia is performed
and compared with the standards. The extractsCTPE, MLHA and ACET have more significantly potent activity
than other extracts and showed 30.97, 46.60 and 49.72 % inhibition respectively compared to standard
ascorbic acid against DPPH free radical. The potent % inhibition value of extracts was found to be 47.67, 33.79,
45.17 exhibited by CTET MLHA, ACPE compared to standard curcumin w against nitrous oxide free radical.
Keywords: Cinnamomumtamala, Madhucalongifolia, Adina cordifolia

Introduction Materials and methods

Herbal medicines are being used by about 80% of Collection and Authentification of the Plant
the world population primarily in the developing The Leaves ofCinnamomumtamala,
countries for primary health care. They have stood Madhucalongifolia andAdina cordifoliawere
the test of time for their safety, efficacy, cultural collected from botanical garden of
acceptability and lesser side effects. The chemical AshtangAyurvedic College, Indore and
constituents present in them are a part of the authenticated by Dr. Shakun Mishra, Head of the
physiological functions of living flora and hence Department (Botany), Shree S.N Govt. P.G.
they are believed to have better compatibility with College, Khandwa. A Voucher specimen of all the
1
the human body. Phytochemicals are the natural plants has been preserved for further references.
bioactive compounds found in plants and they Preparation of extracts of Cinnamomumtamala,
work with nutrients and fibers to form an integral Madhucalongifolia andAdina cordifolia leaves.
part of defense system against various disease and The accurately weighed powdered plant materials
stress conditions. They are basically divided into were extracted using petroleum ether, chloroform,
two groups i.e. primary and secondary acetone, ethanol and distilled water in Soxhlet
constituents, according to their functions in plant apparatus. After about forty siphons of each
metabolism. Primary constituents comprise solvent extraction step, the materials were
9,10
common sugars, amino acids, protein and concentrated by evaporation.
chlorophyll while secondary metabolite consist of Preliminary phytochemical screening
alkaloids, terpenoids, flavonoids, so Extracts of Cinnamomumtamala,
2
on. Cinnamomumtamalaalso known as tejpat, Madhucalongifolia andAdina cordifolia were
belonging to the family Lauraceae.It is widely used subjected to qualitative tests for the identification
in pharmaceutical preparation because of its of various active constituents viz. carbohydrate,
hypoglycemic, stimulant and carminative, glycoside, alkaloid, amino acids, flavanoids, fixed
antidiabetic, antibacterial, antioxidant, anti-ulcer oil, tannins, gum and mucilage, phytosterols etc.
3
and antimicrobial properties. Madhuca, The phytoconstituents were identified by chemical
Madhucalongifolia belonging to the tests, which showed the presence of various
familySapotaceae. It is widely used as tonic, constituents in the different extracts.
analgesic, diuretic, rheumatism, chronic bronchitis
4
and diabetes mellitus , chronic bronchitis, Free Radical Scavenging
Cushing’s disease,gastropathy, dermatopathy, In the present study, the antiradical activity of the
5-6
rheumatism, cephalgia and hemorrhoids. Adina plants extracts in two in vitro models, including
7-8
cordifoliais belonging to the family Rubiaceae. DPPH radicalscavenging, Nitric oxide radical
scavenging, were investigated.

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DPPH radical scavenging activity extracts in different concentrations (10, 20, 30, 40,
o
Leaf extracts of different plants were evaluated for 50 and 100 µg)were incubated at 25 C for 150 min.
their in vitro free radical scavenging activities by At every 30 min interval, 0.5 mL of the incubated
2,2-diphenyl-1-picrylhydrazyl (DPPH) assay extracts was removed and 0.5 mL of Griess reagent
method. To determine the free radical scavenging (1% sulphanilamide, 0.1% naphthylethylene
activity, a method based on the reduction of a diamine dihydrochloride in 2% H3PO4) was added.
methanolic solution of the coloured DPPH radical The absorbance of the chromophore formed was
was used. To a set of test tubes containing 3 mL of measured at 546 nm. All the analyses were
methanol, 50 μL of DPPH reagent (2 mg/mL) was performed in triplicate and the results were
added. The initial absorbance was measured. To averaged. The percentage inhibition of nitric oxide
these test tubes, methanolic solution of different generated was measured by comparing the
extract (1 mg/mL) were added (10-50 μL). Ascorbic absorbance values of control and test. Curcumin
acid (0.5 mg/mL) was also added in the was used as a reference compound.
concentration of 10, 20, 30, 40,50 and 100 μL.
After 20 minutes, absorbance was recorded at 516 Results and Discussion
nm. The experiment was performed in triplicate. DPPH free radical Scavenging assay
The percentage reduction in absorbance was The antioxidant reacts with stable free radical,
calculated from the initial and final absorbance of DPPH and converts it to 1,1-diphenyl-2-picryl
each solution.Percentage scavenging of DPPH hydrazine. The ability to scavenge the free radical,
radical was calculated using the formula DPPH was measured at an absorbance of 516 nm.
% Scavenging of DPPH = [(Control-Test)/Control] × So the DPPH and its % inhibition of petroleum
100 ether, ethanol, hydro-alcoholic and distilled water
Nitric oxide radical scavenging effect: extract reported in Table 1.
Nitric oxide generated from sodium nitroprusside Nitrous oxide radical scavenging activity
in aqueous solution at physiological pH interacts In the present study, the tested extracts competes
with oxygen to produce nitrite ions which were with oxygen to react with nitric oxide and thus
measured by the Griess reaction. Scavenger of restrains formation of the anions. Table 1
nitric oxide compete with oxygen leading to demonstrates the percentage inhibition of nitric
reduced production of nitric oxide. The reaction oxide production by varying concentrations of
mixture (3mL) containing sodium nitroprusside (10 tested compounds.
mM) in phosphate buffered saline (PBS) and the

Table 1: DPPH and Nitrous oxide free radical scavenging activity of different extracts
DPPH Method* Nitrous oxide Method*
S. No. Treatment
Absorbance at 516nm % Inhibition Absorbance at 546nm % Inhibition
1 Control 1.877± 0.056 0 0.856 ± 0.0056 0
1
2 Standard 1.002 ± 0.006 67.45 ± 3.467 NA NA
2
3 Standard NA NA 0.487 ± 0.0011 52.09 ±0.1386
4 CTPE 1.266 ± 0.024 30.97 ± 2.182 0.626 ± 0.0045 33.37 ± 0.0743
5 CTET 1.433 ± 0.046 20.49 ± 1.010 0.529 ± 0.0043 47.67 ± 0.0461
6 CTHA 1.381 ± 0.026 24.98 ± 1.016 0.632 ± 0.0051 30.09 ± 0.2372
7 CTDW 1.475 ± 0.039 18.02 ± 1.156 0.800 ± 0.0005 11.59 ± 0.0692
8 MLPE 1.434 ± 0.062 20.32 ± 1.024 0.621 ± 0.0017 30.51 ± 2.071
9 MLET 1.237 ± 0.024 28.07 ± 1.092 0.727 ± 0.0106 19.44 ± 2.1651
10 MLHA 1.205 ± 0.002 46.60 ± 3.502 0.631 ± 0.0186 33.79 ± 0.106
11 MLDW 1.364 ± 0.026 25.42 ± 1.027 0.627 ± 0.0051 29. 97 ± 0.2193
12 ACPE 1.468 ± 0.032 18.02 ± 1.146 0.522 ± 0.0186 45.17 ± 0.1062
13 ACET 1.217 ± 0.002 49.72 ± 3.502 0.719 ± 0.0203 21.57 ± 0.1223
14 ACHA 1.316 ± 0.024 29.83 ± 2.193 0.657 ± 0.0015 26.21 ± 0.2078
15 ACDW 1.487 ± 0.062 20.49 ± 1.024 0.727 ± 0.0021 19.87 ± 2.0710
1 2
n=3, * All the value are represented as Mean ± SEM, Standard used is ascorbic acid, standard used is
curcumin.

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Conclusion evaluation of mahua flowers. J. Oil

Screening of three medicinal plants was analysis to Technol. Assoc., 30, 1998, 170-72.
maximum classes of phytoconstituents is present. 5. Chandra D. (2001). Analgesic effect of
The medicinal plants have highest therapeutic aqueous and alcoholic extracts of
efficiency by pharmaceutical field. Amongst all the Madhucalongifolia. Indian J.
extract the hydroalcoholic extract indicate the Pharmacology, 33, 108-111.
more positive results. This research reveals that 6. Prajapati V, Tripathi AK, Khanuja SPS,
above plants gives a basis of its use in medicine Kumar S. (2003). Anti-insect screening of
and develop to further drugs in the treatment of medicinal plants from Kukrail Forest,
cancer since these have good antioxidant activity Lucknow, India. Pharmaceutical Biology,
and also in further drugs in pharmaceutical area 4, 166-170.
and also contains the different biologically active 7. Iqbal, P.F.; Bhat, A. R. and Azam, A.
constituents, and secondary products are valuable (2009). Antiamoebiccoumarins from the
of further analysis. root bark of Adina cordifolia and their
new thiosemicarbazone derivatives.
References European Journal of Medicinal Chemistry,
1. WHO, in Progress Report by the Director 44: 2252-2259.
General, Document No. A44/20, 22 March 8. Sabir, M. and Razdan, M.K. (1970).
1991, World Health Organization, Antifertility study with leaf extracts of
Geneva, 1991. Adina cordifolia (karamkigaach). Indian J.
2. Amrit Pal Singh Promising phytochemicals Physiol. Pharmacol.,14: 209-210.
from Indian Medicinal Plants. 9. KR. Khandelwal, Practical Pharmacognosy
Ethnobotanicals Leaflets,vol:2005 Issue, technique and
Article 18. experiments,NiraliPrakashan, Pune, 2001,
3. Hussain A, Virmani OP, Popil SP, Mishra 2nd edition, 149-56.
LN and Gupta AK. Dictionary of Indian 10. Trease GE, Evans WC. Text book of
Medicinal Plants. CIMAP Lucknow, 1980. Pharmacognosy. 13th (eds).Alden Press;
4. Jayasree B., Harishankar N., and Rukmini Oxford; 2003, 512-513.
C., Chemical composition and biological

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COMPARATIVE ANTI DIARRHOEAL ACTIVITY OF DADIMASHTAKA CHURNA AND MARKETED

FORMULATIONS
Nitu Singh* Sumeet Dwivedi
Oriental college of Pharmacy and Research, Oriental University, Indore (MP) – India
[email protected]

ABSTRACT
Diarrhoea is a leading cause of illness and death among children in developing countries, where an estimated
1.3 thousand million episodes and 3.2 million deaths occur each year in those under five years of age .The
present study is to compare the antidiarrhoeal activity of a polyherbal formulations available in the market
named as Dadimashtaka Churna of different companies. It is used to treat gastro intestinal complaints like
diarrhoea. The key ingredient of Dadimashtaka churna is Pomegranate (Dadima). Castor oil induced diarrhea
and Gastro-intestinal motility test model are used for antidiarrhoeal screening of formulations .The results of
the present study clearly indicate that there is differences in the results of antidiarrhoeal activity of
formulations.
Keywords: Diarrhoea, Dadimashtaka, Churna, Dadima, Polyherbal

Introduction hydroalcohol (70ml alcohol + 30ml distilled water)

3
Diarrhoea is a leading cause of illness and death Wistar albino rats of either sex, weighing 150 –
among children in developing countries, where an 200 g were used for the study. Pharmacological
estimated 1.3 thousand million episodes and 3.2 study was approved by Institutional Animal Ethics
million deaths occur each year in those under five Committee (IAEC) of NIMS University, with CPCSEA
1
years of age. There are various Ayurvedic Registration No. 302/ac/CPCSEA. The acute
formulations which are used for the treatment of toxicity study was carried by using OECD Guideline
4
diarrhoea Most of the medicines are effective but No.420.
only one major drawback is lack of
5
standardization. Therefore, there is a need to Castor oil induced diarrhea : The results are
develop a standardization technique to mingle this expressed as a percentage of inhibition of
system of medicine in the main stream of health diarrhea. Table 2
2
science. The present study is to compare the
6
antidiarrhoeal activity of polyherbal formulations Gastro-intestinal motility test model :The results
available in the market called as Dadimashtaka are expressed as a percentage of inhibition of the
Churna of different companies. distance traveled by charcoal . Table 3

Materials and Methods Statistical analysis

Three antidiarrhoeal polyherbal formulation All the values are expressed as mean ± standard
(Dadimashtaka churna) of three different deviation and analyzed for ANOVA followed by
companies namely (MFI), (MFII) and (MFIII) were Dunnet’s t-test. Differences between groups were
procured from a registered Ayurvedic Pharmacy of considered significant at P < 0.05 levels. The
Jaipur and Nashik respectively. statistical analysis was carried out using Graph Pad
All the three formulations were extracted with Prism 5 software.

Table 1. Group of animals for Castor oil induced Diarrhoea and Gastro-intestinal motility test model
S.no Groups Dose
1 I (Control) Vehicle 0.5 % Tween 80 in distilled water (1 ml);
2 II (Standard) Loperamide ( 3 mg/kg ) Atropine sulphate (5 mg/kg body weight)
3 III 200mg/kg of Marketed formulation I(MFI)
4 IV 200mg/kg of Marketed Formulation (MFII),
5 V 200mg/kg of Marketed formulation III (MFIII)
6 VI 200mg/kg of Inhouse formulation (IHF)

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Results and Discussion

Table 2.Results of castor oil induced Diaarhoea.
Group Total no. of Total no. of % Inhibition Total weight of % Inhibition
faeces Diarrhoeal faeces faeces
I [Control] 22.80 ± 0.86 18.6 ± 0.74 - 6.40±1.043 -
II [Standard] 9.80 ±1.65 5.20 ± 1.15* 72.04 1.55±0.067 74.50*
III (MFI) 17.24± 1.53 7.13±0.77* 61.66 2.56±0.211 60*
IV (MFII) 16.21±1.14 6.65 ±0.78* 64.24 2.20±0.261 65.62*
V(MFIII) 15.60± 1.80 6.20 ± 0.58* 67.00 2.04±0.251 68.12*
Values are expressed as mean ± S.E.M ( n=5 ) in each group. Statistical analysis ANOVA followed by Dunnett t-
test.* P<0.05 as compared with Group I (control group).
Table 3 Result of Gastro-intestinal motility test model
Group Mean length of small intestine Percentage of distance travelled by charcoal meal % Inhibition
I 103.35±0.68 81.15±1.21 -
II 106.58±1.26 22.72±1.12* 72.00
III (MFI) 105.22±1.35 32.44±1.11* 60.02
IV(MFII) 107.12±1.55 29.14±1.78* 64.09
V(MFIII) 104.44±1.50 26.22±0.62* 67.68
Values are expressed as mean ± S.E.M (n =5 ) in each group. Statistical analysis ANOVA followed by Dunnett t-
test. * P<0.05 as compared with Group I (control group).

Antidiarrhoeal properties of medicinal plants formulation. To establish the future of Ayurvedic

might be ascribed to tannins, alkaloids, saponins, medicine, research needs to be proceed on
flavonoids, sterols and reducing sugars[9]. Tannins different areas of Ayurveda to meet the
present in antidiarrhoeal plants denature proteins requirement of the society. This can be achieved
in the intestinal mucosa by forming protein by standardization of raw materials, methods, and
tannates which make the intestinal mucosa more procedures for preparation, preservation,
resistant to chemical alteration and reduce presentation, and administration of Ayurvedic
secretion.[10].The main chemical constituents in drugs. Thus, the basis and judicious use of modern
Punica granatum peel extract responsible for scientific methods should be used for the
antidiarrhoeal activity are tannins, phenols, development of Ayurveda.
alkaloids, flavonoids and terpenoid by increasing
colonic water and electrolyte reabsorption and References
inhibiting intestinal motility.[11 ] 1. Syder J D and Mersom M H,The magnitude of the
global problem of the acute diarrhea disease :A
Conclusion review of active surveillance data ,Bull World
health organ,1982 :60:605-61
It is evident from the results that Dadimashtaka
2. Pallavi D. Rai and Sadhana J. Rajput Biological
churna possess significant antidiarrhoeal property.
Evaluation of Polyherbal Ayurvedic Cardiotonic
But, the differences in the results of Preparation “Mahamrutyunjaya rasa” Evidence-
pharmacological studies prove that the contents Based Complementary and Alternative Medicine
of tannins are significantly varied in the ,2011,1-11.
Dadimashtaka formulations. In Herbal 3. Harborne JB. Phytochemical Methods: A guide to
Formulations, major variations are in the active modern technique of plant Analysis. 3, London:
constituents is due to many reasons like change in Chapman & Hall; 1998;3:90
weather, change in geographical sources, change 4. OECD , Acute oral Toxicity – Acute oral toxic class
method, Guideline 423, adopted 23.03.1996
in species, different collection time, adulteration
5. Mujumdar A M .Antidiarrhoeal activity of
at the time of collection and harvesting. Due to
Azadirachta indica leaf extract , Indian Drugs ,
these reasons, the effectiveness of herbal 1998, 35 .7: 417- 420.
formulation is not same all the time. To decrease 6. Galvez J, Zarzuelo A, Crespo M E
these effects, exact determination of active et.al.,Antidiarrhoeic activity of Euphorbia hirta
constituents is necessary. Therefore there is a extract and isolation of an active flavonoid
need of strict regulatory control over the constituent. Planta Medica,1993;333- 336.
manufacture and quality control of this

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INSULIN MIMICS ACTIONS OF POLY-HERBAL FORMULATION (HF) AND ITS ANTI-

HYPERGLYCEMIC EFFECTS ON ALBINO RATS.
Vikas B Gawali1* , Niraj S Vyawahare2
1 Ph D Research Student,Dr. D. Y. Patil institute of Pharmaceutical Sciences and
Research,Pimpri, Pune-411018, [email protected]
2 Proffesor, Dr D Y Patil College of Pharmacy, Akurdi, Pune- 411035,
[email protected]

ABSTRACT
The extract of six herbs such as Syzgium Cumini, Annona Squamosa, Momordica Charantia, Tinospora
Cordifolia, Gymnema Sylvestre and Curcuma Longa was procured and prepares polyherbal formulation in three
different doses (225 mg/kg p.o., 450 mg/kg p.o. and 850 mg/kg p.o.) against standard drug Metformin
(500mg/kg p.o.). The daily dose of HF and Metformin for the period of 7 days and studied the effect of insulin
mimics actions on epinephrine (0.8 mg/kg i.p.) induced hyperglycemia. The acute toxicity of HF was studied as
per OECD guideline 425. The HF-V2 (119.503.55), HF-V3 (103.003.90) and metformin (80.053.63) shown
significant (p<0.01), against the positive control (154.504.42) in epinephrine model, HF-V2 (80.832.07), The
epinephrine is known to enhance glucagon secretion by α-cells of pancreas and activation of β receptors
resulting in an increased glycogenolysis and gluconeogenesis, which causes increase blood sugar level. The
active phyto-constituents present in HF are flavonoids such as 9-octadecenamide, 7-methoxypigenin-6-C-B-
glucoside; triterpenesaponins known as gymnemic acids, gymnemasaponins promote the release of insulin and
delay the absorption of glucose; Curcumin suppress the diabetes, Momordicin, isoquinoline alkaloids have
reported for insulin mimicking and releasing effects which reflect into the decrease the blood glucose level.
The Herbal formulation reduced blood glucose level and shown insulin mimic effects.
Keywords: Polyherbal formulation, insulin mimics, epinephrine, Momordicin, Gymnemic acids

Introduction and curcuma longa had proved for its anti-diabetic

The tremendous research on the diabetes and its effects with nerve tonic, anti-allergic reaction, lipid
7
complication but no single theory is available for lowering effects . The freshly preparedpolyherbal
complete treatment for DM, and its formulation were studied for preclinical evaluation
complication.Traditional herb plays an important for anti-hyperglycemic effects on albino rats and
8
role in treatment of diabetes. It was proved that 5- also examine for acute oral toxicity study .
6 herbal formulation having significantly reduced
1
the dose of insulin and hypoglycemic drugs . The Materials and Methods
herbal medicine is often used with allopathic drug Extract of Herbs; were procure and authenticated
2
for therapeutic remedies . The herbs used for from S G phyopharmaceutical Kolhapur.
various remedies in India is common phenomena, Chemicals; The glucose strip were purchase from
Ayurveda elucidated the practice of use of herbal local market, Epinephrin HCl, glucose, diethyl
1, 2
drugs, their combination and line of treatment . ether, etc puchased from New Neeta Chemicals.
In diabetic patient had observed that they take the
herbal formulation with the hypoglycemic agents Preparation of Poly herbalformulation
for their batter control of sugar and its The freshly prepared three different polyherbal
complications. The some herbs having wide formulation contains syzygium cumini, Annona
therapeutic value and lower cost is beneficial for Squamosa, Momordica Charantia, Tinospora
the patient, also sensitize pancreas for release of cordifolia, curcuma longa, Gymnema Sylvestre
insulin, and enhance the utilization of sugar by (See Table.1). The all extract was weighed in
peripheral mechanism. The Momordica Cherantia, motor, added water and mix it well to form a
Sygium cumini and Gymnema sylvestre has widely homogeneous liquid mixture; adjust volume up to
3, 4
studied for anti-hyperglycemic effects , the 20 ml purified water.
active constituents of plant extracts responsible Animals
for glucose lowering effect in alloxan and STZ Adult albino rats were procure from Padro
5, 6
induced diabetic rats . Some research article Laboratories Pvt. Ltd., Pune of either six weight
stated that annonasquamosa¸ tinosporacordifolia range 200 gm to 220 gm and female albino mice

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(20-25 gm) were maintained at (25  1) room IPCSEA Approval no DYPCOP/IAEC/2019-01-01.

temperature and relative humidity of 45 -50%.

Table 1.The composition of herbal formulations

Sr. No. Herbal Extract Composition of herbal extract mg/kg
HF-V1 HF-V2 HF-V3
1 Aq. Extract of Tinospora Cordifolia 52.5 87.5 175
2 Aq. Extract of Syzgium Cumini 30 50 100
3 Aq. Extract of Gymnema Sylvestre 45 75 150
4 Aq. Alcoholic Extract of Annona Retculata 52.5 87.5 175
5 Aq. Alcoholic Extract of Momordica Charantia 45 75.5 150
6 Alcoholic Extract of 30 50 100
Curcuma Longa
Total dose (mg/kg p. o.) 225 425 850

Experimental designing: Epinephrine induced 850mg/kg) decrease blood glucose leve

hyperglycemic rats significantly at 1, 2 and 4 hr.
The albino rats were divided into five groups (n=6)
as follows, Epinephrine hydrochloride (0.8 mg/kg) Discussion
was given to all groups Group 1 Induced Control, Most of herbal formulation was prepared base on
Group 2 HF-V1 (225 mg/kg p.o.), Group 3 Treated Ayurveda and preparation of drug theory is
with HF-V2 (450 mg/kg p.o.), Group 4 HF-V3 (850 available in Charaka Samhita and Sushruta Samhita
mg/kg p.o.), Group 5 Metformin (500 mg/kg). is base on two main principle i) use of single herbs
Daily dose of epinephrine hydrochloride induced ii) use of multi herbs. The use of more than two
hyperglycemic animal were treated for 7 days and herbal drugs for preparation of formulation is
at the end of study animal were overnight fasted known as polyherbal formulation, multi-herbs
and give a dose of epinephrine HCL, different gives more beneficial and additional
2,
concentration of HF and Metformin, after dosing complementary effects than the single drug used
4
0.5, 1, 2, and 4 hr, blood sugar level was measured . The hypoglycemic activity of HF was also
4
by glucometer . observed in epinephrine induced hyperglycemic
rats. The observed hypoglycemic effect of HF may
Statistical Analysis be explained in the following way (a) restoration of
The data were expressed as Mean  SEM. The delayed insulin response or (b) decreased
statistical significance between means was intestinal glucose absorption. Alternatively
analyzed by one-way analysis of variance (ANOVA) hypoglycemic effect of HFmay be attributed to
followed by Dunnetsmultiple ‘t’ test was used. A increased secretion of insulin from intact β-islets
9
“P” Value of less than 0.05 was of Langarhan or its release from bound insulin .
consideringspastically significant. The herbal formulation contains flavonoids such as
9-octadecenamide ethyl isoallocholate, 7-
Results: Acute Toxicity study methoxyapigeninn 6- c –b glucoside, lead to
Not showing any mortality on dose range 2000 regenaration of pancreatoc B-cells and prevent the
10, 11
mg/kg upto 5000 mg/kg in acute toxicity studies necrosis and degeneration . Phenolic
carried out respectively single oral dose and compounds and flavonoids having excellent free
animal were observed for 14 days. radical scavenging agents, prevents free radical
chain reaction in the body. Triterpene saponins
Epinephrine induced hyperglycemic rats such as gymnemic acid, gynema saponins having
Thepoly herbal formulation elicited their anti- sweet inactivation properties, gymnemic acid –IV
hyperglycemic effect of HF-V2 (119.503.55), HF- increases plasma insulin levels in diabetic mice, it
V3 (103.003.90) and metformin (80.053.63) at is reported for reduced obecity and to delay the
12
time interval upto 4 hr after dosing shown glucose absorption in the blood .
significant (p<0.01), against the positive control
(154.504.42) in epinephrine HCL (0.8 mg/kg, ip.) Conclusion
hyperglycemia in rats. The HF (225, 450, &

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The polyherbal formulation significantly reducess 6. Achyuth K, Karthiek R, Meena S, Asha G:

the blood glucose level, further study need to be Anti-diabetic activity of Gymnema
carried out on diabetic rats. Sylvestre leaf extract on alloxan induced
diabetic rats. International Journal of
Reference: Trends in Pharmacy and Life Science
1. Kumar D, Mitra A, Manjunatha M: In vitro 2016; 2: 813 - 20.
and in vivo studies of antidiabetic indian 7. Saha S, Ghosh S: Tinospora cordifolia One
medicinal plants: a review. Journal of plant, many roles. Ancient Science of Life
Herbal Medicine and Toxicology 2009; 3: 2012; 31: 151 - 60.
10 – 17. 8. Carson JF: Chemistry and biological
2. Kolhe SS, Punit R, Rachh PR: Review on properties of onion and garlic. Food Rev.
potent anti-diabetic plants or herbs from International 1987; 3: 71– 03.
traditional medicine. Journal of Drug 9. Arumugam G, Manjula P, Paari N: A
Delivery and Therapeutics 2018; 8: 92-98. review: Anti diabetic medicinal plants
3. Singh j, Cumming E, Gunasekar M, Huba used for diabetes mellitus. Journal of
K, Adeghate E: Medicinal Chemistry of the Acute Diseases 2013; 2: 196- 00.
Anti-diabetic effects of Momordica 10. Raut SP, Kar DM, Maharana L: Anti-
Charantia: active constituents and modes hyperglycemic effect of different fractions
of actions. Open Medicinal Chemistry of Annona Reticulata leaf. Asian Journal
Journal 2011; 5: 70-77. Pharmacy and clinical Research 2016; 9:
4. Naik SR, Mandalik RV, Desai SK: 256 - 62.
Antidiabetic activity of a polyherbal 11. Zhang Z, Radziuk J: Inverse relationship
formulation (DRF/AY/5001). Indian between peripheral insulinremoval and
Journal of Experimental Biology 2008; 46: action: studies with metformin. American
599 - 06. Journal Physiology Endocrinology
5. Olatunde A, Joel EB, Tijjani H, Obidola SM, Metabolism. 2001; 281: 1240 - 48.
Luka CD: Anti-diabetic Activity of Aqueous 12. Eidi A, Eidi M, Esmaeili E: Antidiabetic
Extract of Curcuma longa (Linn) Rhizome effect of garlic (Allium sativum L.) in
in Normal and Alloxan-Induced Diabetic normal and streptozotocin-induced
Rats. Researcher 2014; 6: 58-65. diabetic rats. Phytomedicine 2006. 13:
624 - 29.

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COMPARATIVE STUDY ON EFFECT OF NATURAL SUPERDISINTEGRANTS IN THE

FORMULATION OF AMLAKYADI CHURNA TABLET
Yamini Chaurasia*, S.C Mahajan, Sunita Pandey, Nisha Mandloi
BM College of Pharmaceutical Education and Research, Indore, M.P. (India)
[email protected]

ABSRACT
In the present study, Amlakyadi churna prepared and convert Amlakyadi churna into solid dosage form (tablet)
(ACT) using natural disintegrants (Plantago ovata and Carica papaya pulp) by wet granulation method, in
varying concentration, to get minimum possible disintegration time by varying the concentration of the both
the natural superdisintegrants. Those tablets were evaluated for weight variation , hardness, disintegration
time, drug content, friability and dissolution. Hence, present study revealed that this natural superdisintegrant
(Plantago ovata mucilage) showed better disintegrating property than the natural superdisintegrant (Carica
papaya pulp) in the formulation of ACT.
Keywords: Amlakyadi churna, Plantago ovata mucilage, Carica papaya pulp, disintegration

Introduction in the formulation of Amlakyadi churna tablet

Ayurvedic formulations cover wide range of (ACT) by wet granulation method.
product from solid to semisolid to liquid dosage
forms. In Ayurveda there are several different Materials and methods
types of formulation like - Solid dosage forms The plants part used in Amlakyadi churna were
(vatika, gutika, guggulu), semisolid dosage forms purchased from local market of Ujjain (M.P), and
(kalka, avleha), liquid dosage forms (asava, identified at Department of Botany, Vikram
arista, swarasa, taila), and powder dosage form University Ujjain (M.P). All above drugs were
(churna) (Ayurvedic Pharmacopoeia of India). shade dried, reduced to coarse powder, weighted
Among all these formulations churna are most separately and sieved through sieve No. 20 (for
prescribed Ayurvedic dosage form. The selected coarse powder).
formulation has been taken for present research Isolation of mucilage
work by discursive attempts of studying various Seeds of Plantago ovata were soaked in distilled
classical literatures. Thus, formulation was water for 48 hours and then boiled for 1 hour for
enlisted as essential drug list by Central Council completed release of mucilage into water. The
of Ayurveda. Amlakyadi churna is a well known materials were filtered by squeezing in muslin
ayurvedic formulation described in ayurvedic cloth to remove marc, equal volume of acetone
text Ayurvedic formulary of India. It is a potent was added up filtrate to precipitate the mucilage.
ayurvedic medicine used in the treatment of The mucilage was separated and dried in oven at a
constipation, dyspepsia and fever. The main 0
temperature less than 60 C, powdered, weighed
components are Embilica officinalis, Terminalia and stored in desiccators. (Shirsand et al., 2009)
chebula, Plumbago zeylanica, Piper longum and Preparation of Formulation
Saindhava and prescribed dose of Amlakyadi Amlakyadi churna is an important herbal
churna is 3-5gm. Amlakyadi churna was selected formulation, official in Ayurvedic Pharmacopoeia
as: used mostly for constipation, having all the of India, were prepared in laboratory (AC-L) as-
effective ingredients which are easily cure the Take all the ingredients of Amlakyadi churna of
particular diseases, also having other therapeutic pharmacopoeial quality. Roast saindhava lavan in a
values (Ayurvedic Formulary of India). Mucilage stainless steel pan at low temperature till it
of natural origin is preferred as they are becomes free from moisture, prepare fine powder
comparatively cheaper, abundantly available, and pass through sieve number 85. Wash and dry
non-irritating and non-toxic in nature. Mucilage all the ingredients of Amlakyadi churna, powder
of Plantago ovata has various characteristics like individually in pulverizer and pass through sieve
binding, disintegrating, and sustaining properties number 85. Weigh separately each ingredient, mix
(Baveja, 1968). Hence, in the present study, together and pass through sieve number 44 to
mucilage of Plantago ovata compared with obtain a homogeneous blend. Amlakyadi churna
Carica papaya pulp used as super disintegrants used for the treatment of anorexia, dyspepsia,
fever, and in indigestion.

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Table no.1 Ingredients of Amlakyadi churna

S.No. Drugs Biological Source Part Used Quantity Taken
1. Amla Embilica officinalis Fruit pulp 1 part
2. Harad Terminalia chebula Fruit pulp 1 part
3. Chitraka Plumbago zeylanica Roots 1 part
4. Pippali Piper longum Fruit 1 part
5. Saindhava Rock salt Salt 1 part

Preparation of Amlakyadi churna tablet tablets of Amlakyadi churna tablet were prepared
Ayurvedic powders dosage uniformity and patient by wet granulation technique with different
compliance can be increased by formulating into concentration of natural disintegrants Plantago
tablet dosage form. So, that in the present study ovata and Carica papaya.

Table no. 2. Composition for Amlakyadi churna Tablet

S.No. Ingredient per Tablet F-1 F-2 F-3 F-4 F-5 F-6
1. Amlakyadi churna (mg) 482 482 482 482 482 482
2. Plantago ovata (mg) 10 15 20 ---- --- ----
3. Carica papaya (mg) ---- --- --- 10 15 20
4. Gum acacia (%) 2 2 2 2 2 2
5. Lactose (mg) 2 2 2 2 2 2
6. Talc (mg) 2 2 2 2 2 2
7. Magnesium stearate (mg) 2 2 2 2 2 2

Amlakyadi churna were passed through 80 mesh, granules were prepared by passing the damp mass
and weighed individually. All the crude drugs through sieve (16). The granules were then dried
mixed with different concentration of Plantago at 50°C in hot air oven. Dried granules were
ovata and Carica papaya (10%, 15%, 20% blended with other ingredients (talc, magnesium
w/w),where lactose, gum acacia and talc, stearate) thoroughly by tumbling in a polythene
magnesium stearate used as diluent, binder and bag. Tablets were compressed by using tablet
lubricant respectively. 2% of aqueous solution of compression machine. Granules were analyzed for
gum acacia used as binder was added drop wise till following pre-compression parameter: Bulk
suitable mass for granulation was obtained. The density, Tapped density, Carr’s index, Angle of
wet mass granulated through sieve no. 16. The repose. (Alton et al., 2002)

Table no. 3. Parameters of Granules Properties

S.No. Formulation Angle of Loose bulk True bulk Compressibility
repose density density index
1. F-1 24.32±0.11 0.553±0.35 0.625±0.02 14.31±0.36
2. F-2 25.34±0.03 0.546±0.03 0.623±0.14 13.10±0.05
3. F-3 24.22±0.06 0.539±0.13 0.612±0.03 13.01±0.14
4. F-4 23.16±0.01 0.532±0.02 0.624±0.13 14.24±0.01
5. F-5 25.03±0.12 0.521±0.14 0.597±0.06 13.13±0.12
6. F-6 26.23±0.04 0.513±0.18 0.583±0.02 14.06±0.02
All the values are in mean ±SD (Standard deviation) (where n=3)

Evaluation of tablets weight. Monsanto hardness tester was used for

All the formulated tablets were evaluated for the determination of hardness of the tablet. The
weight variation, hardness, thickness, friability, friability of tablets was determined using a Roche
wetting time, disintegration time and stability friabilator. Two tablets from each batch takened
study. In the weight variation test, 20 tablets were and placed in the friabilator then operated for 100
selected at random and the average weight was revolutions. Then the tablets were dedusted and
calculated. Then, individual tablets were weighed reweighed. Percentage friability was calculated
and the weight was compared with an average using the formula,

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F = (1‐W0 / W) × 100 Drug Release

In the disintegration time study, the tablets were For drug release of ACT first prepared standard
taken and introduced in each tube of curve of piperine at 343 nm and standard curve of
disintegration apparatus and the tablet rack of the gallic acid at 270 nm after that drug release was
disintegration apparatus was positioned in to a 1 carried out using USP dissolution testing apparatus
liter beaker containing 900ml of distilled water and II (paddle method) at 37 ± 0.5ºC and100 rpm using
time of disintegration was recorded at 37±20C. In 900 ml of 0.1 N HCl containing 10% alcohol as a
the wetting time study, a piece of tissue paper dissolution medium. 10 ml of the sample solution
folded twice was placed in a petridish (with was withdrawn from the dissolution apparatus at
internal diameter 6.5cm) containing 5ml of each 10 min intervals, and the samples replaced
distilled water. A tablet was placed on the paper with fresh dissolution medium. The samples were
and time for complete wetting of the tablets was filtered through a 0.45m membrane filter and
measured in seconds. The stability study of the diluted to a suitable concentration with 0.1N HCl
tablets was carried out according to ICH containing 10% alcohol. Absorbance of these
guidelines, by storing the tablets in stability solutions was measured at 343 nm for piperine
0
chamber at 40 ± 2 C /75 ± 5%RH for three and 270 nm gallic acid, using a Shimadzu UV-1700.
months. At the end of each month tablets were Cumulative percentage of drug release was
tested for disintegration time. (Lachman, 2008) calculated using the equation obtained from a
standard curve.

Standard curve of piperine

y = 0.0352x - 0.0009
R2 = 0.9978
0.4
0.35
0.3
Absorbance

0.25
abs
0.2
Linear (abs)
0.15
0.1
0.05
0
0 2 4 6 8 10 12
Cocentration (ug/mi)

Fig.1. Standard curve for Piperine Fig.2. Standard curve for Gallic acid

Table no. 4 Evaluating parameters after compreesing

Formulations Hardness Friability Weight Disintegration % Drug release
2
(kg/cm ) (%) Variation(%) time (in mins) Piperine Gallic acid
F-1 3.26±0.03 0.51±0.14 500.61 ± 0.02 4.86±0.46 71.38±0.44 71.01±0.93
F-2 3.14±0.13 0.54±0.01 499.89±0.14 4.29±0.70 73.29±0.50 71.28±0.10
F-3 3.19±0.02 0.58±0.07 500.23±0.12 3.83±0.11 79.62±0.50 78.93±1.15
F-4 3.29±0.14 0.63±0.12 500.71±0.01 5.44±0.40 70.23±2.62 78.61±0.62
F-5 3.32±0.07 0.53±0.04 501.16±0.13 4.63±0.30 71.19±1.80 73.53±0.50
F-6 3.37±0.06 0.57±0.18 500.77±0.04 5.22±0.16 72.98±1.81 74.95±2.50
All the values are in mean ±SD (Standard deviation) (where n=3)

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Fig.3. In vitro drug release of Plantago ovata Fig.4. In vitro drug release of Plantago ovata
disintegrant for piperine disintegrant for gallic acid

Fig.5. In vitro drug release of Carica papaya Fig.6. In vitro drug release of Carica papaya
disintegrant for Piperine disintegrant for gallic acid

From the above studies it was concluded that The selected formulations were packed in yellow-
0
among all the six tablet formulations, results of F3 colored ALU, stored at 40 C / 75 % RH for 3
observed best and within the standard limits. In F3 months and evaluated for their physical
with increase in the concentration of natural appearance and drug content at specified intervals
disintegrants (plantago ovata, carica papaya), of time. Amlakyadi churna tablets were prepared
there was decrease in the disintegration time and and evaluated for all the physical parameters and
hardness increases which results good friability of in vitro studies. (ICH Guideline Q1B 2003) shown
the tablets and shows better drug release when in table 5.
compared to other formulations and so selected as
optimized formulation and evaluated for further
analysis parameters.
Table no. 5. Stability study of F-3
S. No. Parameter After 1 Month After 2 Month After 3 Month
1. Weight Variation 485.10±1.49 476.03±1.51 471.09±1.24
2. Hardness 3.37±0.13 3.32±0.11 3.28±0.09
3.. Friability 0.38±0.15 0.37±0.12 0.34±0.07
4. Disintegration (in mins) 4.13±0.30 4.09±0.34 4.07±0.42
5. Piperine 79.14±0.47 79.11±0.74 79.08±0.96
6. Gallic acid 78.21±0.08 78.15±0.61 78.06±1.60
All the values are in mean ±SD (Standard deviation) (where n=3)

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Fig.7. In vitro release for piperine Fig.8. In vitro release for gallic acid
after stability study F-3 after stability study F-3

Results and discussion Conclusion

Amlakyadi churna is a well known ayurvedic The results indicate that, the dosage uniformity
formulation, official in Ayurvedic Formulary of and patient compliance of ayurvedic churnas can
India. It is one of the most widely used formulation be increased by formulating them into tablets.
for the treatment of constipation, dyspepsia and Present study envisaged was to convert Amlakyadi
fever. Amlakyadi churna prepared in the churna into solid dosage form (tablet) by using
laboratory as per given in Ayurvedic Formulary of natural disintegrants (Plantago ovata and Carica
India. Tablet formulation were prepared by wet papaya pulp) in varying concentration. The
granulation method employing Plantago ovata Amlakyadi churna was prepared in laboratory as
mucilage and Carica papaya pulp powder as per procedure given in Ayurvedic formulary and
natural disintegrant used in different ratios. A total tablet of Amlakyadi churna were prepared by wet
six tablet formulations were designed using granulation method, according to standard
various excipients. Granules were compressed into procedure. Six batches of Amlakyadi churna
tablets and the evaluation parameters of the tablets was prepared using natural disintegrants
tablets for all the six formulations (F1, F2, F3, F4, (Plantago ovata and Carica papaya) with three
F5, F6) respectively - weight variation , hardness, different concentration (10%, 15%, 20% w/w).
friability, disintegration time and drug release Results indicated that at 15% w/w (F3)
study were performed and results are within the concentration of disintegrant (Plantago ovata)
acceptable limit. From the above studies it was show minimum disintegration time and higher
concluded that among all the six formulations, drug release as compare to other formulation.
results of F3 observed best and within the Results of research suggest that Plantago ovata
standard limits. In F3 with increase in the mucilage can be used as a disintegrant in the
concentration of natural disintegrants (plantago formulation of uncoated tablets.
ovata, carica papaya), there was decrease in the
disintegration time and hardness increases which References
results good friability of the tablets and shows 1. Stability studies information: International
better drug release when compared to other Conference on Harmonization (ICH)
formulations and so selected as optimized Stability testing for new dosage forms Q1C,
formulation. The physical parameter of granules of Photostability Testing of New drug
F3 formulation angle of repose, bulk density, substances and products Q1B 2003; Feb 6.
tapped density, carr’s index, was found to be 2. Shirshand SB, Sarasija S, Para MS, Swamy
24.22±0.06, 0.539±0.31, 0.612±0.03, 13.01±0.14 PV, Kumar DN. Plantago ovata in the
respectively. Tablet F3 formulation evaluated for- design of fast disintegrating tablets. Indian
weight variation, hardness, friability, disintegration J. Pharm. Sci. 2009;71(1):41-45.
time was found to be 500.23±0.12, 3.19±0.12 3. International Conference on
2
kg/cm , 0.58±0.07 %, 3.83±0.11, respectively. The Harmonization (ICH), Harmonized
result shows all the parameter with in the Tripartite guideline for stability testing of
acceptant range. The in-vitro drug release new drugs substances and products
(piperine, gallic acid) was found to be 79.62±0.50, Q1A(R2) 2003; Feb 6.
78.93±1.15 respectively which shows the better 4. Ayurvedic Formulary of India: Ministry of
drug release as compared to other formulation. Health and Family Welfare. Govt. of India,

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International Journal of
Pharmaceutical Sciences and Research
ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

New Delhi: Controller of Publications; Indian Journal of Pharmaceutical Sciences,

1999. 30(11),1968,247-251.
5. Ayurvedic Pharmacopoeia of India, part II, 7. Lachman L, Liberman HA, Kanig JL, The
st
vol.1, 1 edition , Govt. of India, Ministry of theory and practice of industries
rd
Health and Family Welfare ,Dept. of pharmacy, 3 edition. Varghese publishing
health; 14:100. house 2008.
6. Baveja SK, Gupta BM, Rheology of Aqueous
dispersion of Plantago ovata seed husk-II,

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EFFECT OF ETHANOLIC EXTRACT OF TERMINALIA CHEBULA FRUITS ON ADVANCE

GLYCATION END PRODUCTS IN EXPERIMENTAL STZ DIABETIC RATS
Soni Rupesh 1, 2*, Mehta N. M. 2, Srivastava D. N. 1
1. Department of Pharmacology & Toxicology, B. R. Nahata College of
Pharmacy - CRC, Mandsaur (Madhya Pradesh)
2. Department of Pharmacy, Jodhpur National University, Jodhpur (Rajasthan)
[email protected]

ABSTRACT
Haritaki (Chebulic Myrobalan) has been reported as folklore medicine for treatment of various types of disease
and disorders in alone as well as in combination with other herbal medicines. Many investigators have been
reported activity of Chebulic Myrobalan in hyperglycemia, wound healing, ulcers, diarrhea, immunity and
digestive disorders of GIT. In present study we investigated effect of ethanolic extract of Terminalia chebula
fruits on advance glycation end products in streptozotocin induced diabetic rats. The diabetic rats were treated
with ethanolic extract of Terminalia chebula fruits at a dose of 100 mg/kg orally for 14 days and found significant
decrease in blood glucose, glycated hemoglobin, glycated albumin and serum glycated fructosamine level in
treated diabetic rats as compared to non treated diabetic rats
Keywords: Diabetes, HbA1c, Glycated Hemoglobin, Advance Glycation end products, Glycated Fructosamine
Glycated Albumin

Introduction mg/kg, i.p.) and checked by Glucometer. Animals

Diabetes is a group of disorders characterized by blood glucose level more than 250 mg/dl were
hyperglycemia resulting abnormalities in glucose selected for further cutaneous wound healing
1 4
metabolism. Diabetes i s a s s o c i a t e d w i th activity.
g l y c a t io n o f essential proteins and hormones, due Treatment Procedure: In this study rats were
to presence of high blood sugar level. The advance divided in to four groups on the basis of their
glycation leads to formation of glycated proteins, treatment receiving procedure. One T. chebula
which are abnormal functionless proteins and group of streptozotocin-induced diabetic rats was
2
reduces the normal efficacy of body. The AGEs treated with ethanolic extract of T. chebula
produces defects in cellular protein components (100mg/kg, n=6) and another positive control group
and interfere with normal working of these was treated with Glyburide (4 mg/kg, n=6)
proteins, hormones, enzymes etc, these involved in respectively for 30 days, at the end of which plasma
5
growth, development, repair and maintenance of glucose, glycosylated hemoglobin, serum
normal physiology of cells and organs are fails to 6
fructosamine and Serum albumin level were
work and this disturbed working generates measured in all animals and the results compared
disorder or complication in body physiology
with those of the untreated diabetic control and
especially wound healing or repair and regeneration
3 normal control rats.
of tissues. It is well known fact that traditional
medicines are more effective in treatment of Results
diabetes and its complications. The current research
As per results showed in Table 1, there was
is aimed to investigate effect of ethanolic extract
decrease in blood glucose level (upto 73.67
of Terminalia chebula leaves on advance mg/dl) of rats in ethanolic extract treated group
glycation in streptozotocin induced diabetic rats.
and (upto 72.46 mg/dl) in rats of positive control
group. While the control group of diabetic
Materials and methods
animals showed higher blood glucose level
Plant material extraction and induction of Diabetes (303.8 mg/dl) as compared to normal control
Mellitus
group. In case of serum glycated proteins; the
The dried fruits of Terminalia chebula were
ethanolic extract of T. chebula treated rats
extracted by ethanol. Wistar rats were made exhibited lower level of hemoglobin (%HbA1c)
diabetic by a single injection of streptozotocin (60 4.533 % fructosamine 0.560 % compared to high

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amount of these in diabetic control group 11.78 Glyburide showed similar improvements and as
% and 3.11 % respectively. The level of serum compared with T. chebula treated rats. The
albumin was observed higher (5.792 gm/dl) in treatment of ethanolic extract of T. chebula
ethanolic extract treated rats which was less possesses significant comparable beneficial effects
(3.140 gm/dl) in non treated diabetic rats. The in diabetic rats.
diabetic rats of positive control group treated with

Table 1: Effect of Terminalia chebula fruits Extracts on Hematological Parameters in Blood

Parameters Normal Control Diabetic Control T. chebula Group Positive Control
Group Group Group
Blood Glucose 80.00±4.139 303.8±10.82 73.67±3.211 72.46±2.018
(mg/dl) *** *** ***
% HbA1c (Glycated 4.633±0.033 11.78±0.030 4.533±0.071 4.616±0.064
*** *** ***
Serum Fructosamine 1.223±0.040 3.118±0.023 0.560±0.011 0.818±1.351
*** *** ***
Serum Albumin 4.390±0.059 3.140±0.032 5.792±0.039 5.948±0.072
** *** *** ***
Data are expressed as Mean ± SEM and analyzed statistically by One way ANOVA followed by Dunnett's
Multiple Comparison Test.

Discussion and conclusion 2000, 71(1) 343–347,

Advance glycation reaction involves addition of 2. Goodson W. H. and Hunt T. K.: Wound
carbohydrate metabolites with proteins and can healing and the diabetic patient. Surgical
reduce the cellular functioning and promotes them Gynecology and Obstetrics, 1 9 7 9 , 149(4)
7
for damage. During diabetes level of glycated 600-608.
proteins was increased with high blood glucose 3. Ahmed N.: Advanced glycation end products
8 - role in pathology of diabetic complications.
level. The AGEs reacts with hemoglobin and
Diabetes Research and Clinical Practice,
formed glycated HbA1C can leads to anemia,
defect in growth and repair and skin 2005, 67(3) 21-22.
4. Gajdosik A., Gajdosikova A., Stefek M.: STZ
inflammations. In diabetes the increased level
9
induced experimental diabetes in male
of glycted albumin and serum fructosamine wistar rates. General Physiology Biophysics,
resembles the gestational and metabolic 1999, 18(1), 54-62.
10
complications of diabetes. The chronic diabetes 5. Balamurugan R., Selvaraj N., Sathiyapriya V.:
produces defect in metabolism, growth, repair and Increased glycated hemoglobin level in non-
regeneration, cellular damage. High amount of diabetic nephrotic children with
phenolics and tannin compounds in ethanolic o x i d a t i v e s t r e s s . Indian Journal of
11,12
extract of Terminalia chebula fruits reported Physiology and Pharmacology, 2007, 51(2)
that ethanolic extract of Terminalia chebula fruits 153-159.
exhibits antihyperglycemic activity. In this study 6. Sahu A. and Sarkar P. D.: Comparative
the treatment of ethanolic extract of Terminalia study of NBT reduction method for
chebula fruits, improves the glycemic control in estimation of glycated protein serum
diabetes rats. All these treatment effects of fructoseamine. Indian Journal Physiology
ethanolic extract of Terminalia chebula fruits and Pharmacology, 2008, 52(4) 408-412.
comparable with glyburide. These effects can play 7. Farris P K.: Innovative cosmeceuticals; Sirtuin
a major role in treatment of diabetes and can activators and antiglycation compound. J
overcome the chronic complications of diabetes. Cutan Med Surg, 2011, 30(3) 163-166.
8. Anjuman Gul, and M Ataur Rahman :
References Changes in glycosylated proteins in diabetic
1. Teixeira C. C., Rava C. A., Anselmi F. : and non-diabetic patients with and without
Absence of antihyperglycemic effect of cardiovascular complications. Asia Pac. J.
jambolan in experimental and clinical Clin. Nutr., 2003, 12(3) 277-281.
models, Journal of Ethnopharmacology, 9. Sidorenkow G, Zeeuw de D. and Denig P.A.:

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International Journal of
Pharmaceutical Sciences and Research
ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

longitudinal study examining adherence dry fruits of Terminalia chebula in

to guideline in diabetes care according to experimental diabetes mellitus. Indian
different definitions of adequacy and Journal of Clinical Biochemistry 2004, 19(2)
timeliness. Pubic Library Science, 2011, 6(9) 202-204.
24278. 12. Murali Y.K.: Long term effects of Terminalia
10. Furusyo N. and Hayashi J.: Glyacted albumin chebula Retz. On hyperglycemia and tissue
and diabetes mellitus. Biochemica et glycogen content & release of insulin in stz
Biophysicaal Acta, 2013, 1830(12) 5509- induced diabetic rats. Exprimental Clinical
5514. Endocrinology and Diabetes 2007, 115 (10)
11. Murli Y. K., Chandra R. and Murthy P.S.: 641-646.
Antihyperglycemic effect of water extract of

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ANTI-ALZHEIMER ACTIVITY OF TERMINALIA CATAPPAFRUIT EXTRACTIN STREPTOZOTOCIN INDUCED

ALZHEIMER IN EXPERIMENTAL RATS
1 2
Joshi Ankur , MalviyaNeelesh
1. Research Scholar, Mandsaur University, Mandsaur
2. Smriti College of Pharmaceutical Education, Indore, M.P., India
[email protected]

ABSTRACT
The present researchdeals with the assessment of Anti-Alzheimer affect Terminalia catappafruit extracts(TCFE)
in Alzheimer diseased (AD) rat and also propose its probable mechanism of action. Alzheimer disease was
induced by administering streptozotocin i.e. STZ (3 mg/kg) by Intracerebroventricular injection (i.c.v. injection)
st rd
day 1 and3 day, after surgery. Stereotaxic apparatus was used for surgery.Anesthetized rats were used for
surgery. Streptozotocin induced Alzheimer diseased rats were treated with hydroalcoholic extract of TCFE (100
and 200 mg/kg, p.o.) for 14 days. Effects of TCFE in Alzheimer diseased rats were assessed for biochemical
parameter in the brain tissue oxidative stress parameters (SOD, CAT, GSH and TBARS), amyloid β peptide (Aβ)
and acetylcholinesterase (AchE). TCFE significantly (p<0.01) decreases the Aβ1-40, Aβ1-42
peptides.Acetylcholinesterase level in the rats brain tissue reduced compared to Alzheimer diseased rats. TCFE
significantly decreases the oxidative stress level in Alzheimer diseased rats. The present study revealsthat the
TCFEproduces Anti-Alzheimer’s effect in Alzheimer diseased rats by decreasing oxidative stresslevel , Aβ
protein level and Acetylcholinesterase level in the brain tissue.
Keyword:Terminalia catappa, Alzheimers, amyloid β peptide (Aβ) and acetylcholinesterase (AchE), Oxidative
stress.

Introduction Animals
Alzheimer is associated with neuronal Male wistar rats (200-250 g) at about eight weeks
degeneration, characterized by memory loss and of age were used for the pharmacological
altered behaviour. Many pathological conditions screening.
like increased oxidative stress, amyloid β (Aβ)
plaque formation, neuroinflamation results in Induction Alzheimer’s
1
AD .Due to excess of reactive oxygen species (ROS) Rats were divided into five different groups:
oxidative stress develops which overexpress Aß in Control, Streptozotocin treated rat (STZ, 3 mg/kg,
the neuron which modifies the cellular function icv), STZ plus Donepezil (5 mg/kg), STZ plus TCFE
and thereby activates the neurodegeneration. 100 mg/kg, STZ plus TCFE 200 mg/kg. Alzheimer
Various reports suggested that drugs which are was induced by stereotaxic surgery.
having property to stabilize free radical activity
possess neuroprotective effect.Terminalia catappa Estimation of beta amyloid
is a well-recognized herb.Terminalia catappa has Aβ was measured in brain tissue extracts using a
been known for its therapeutically essential ELISA Kit.
phytoconstituents, such as flavonoid,phenol and
carotenoid. Various pharmacological researches Determination of AChE activity in brain
have confirmed thatTerminalia catappa Colorimetric method was used for the estimation
possesseshepatoprotective,antimicrobial, of acetycholinesterase (AchE)
antidiabetic,and anti-inflammatory.
Estimation of markers of oxidative stress
Materials and Methods Superoxide dismutase (SOD) was estimated in the
brain of AD rats by using method Arutla. TBARS
Collection and preparation of plant extract was estimated the method given by Ohkawaka.
Fresh Terminalia catappa fruits were collected. Activity of catalase (CAT) in the brain was
The fruits were sliced into small pieces and dried it measuredby ability of catalase to oxidize
under shade. Dried fruits were coarsely powdered H2O2.Reduced glutathione assay (GSH) was
13
and subjected to hydroalcoholic (70:30) estimated by the method of Jollow .
soxhletion. The extract was concentrated and
dried kept in a desiccators.

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Result and discussion

Table No. 1 Effect of Terminalia catappa fruits extract on biochemical parameters
Treatment CAT SOD GSH TBARS
(nmole/g) (nmole/g) (nmole/g) (nmole/g)
Vehicle control 11.0 ± 0.25 7.18 ± 2.8 174.5 ± 10.7 184.5 ± 8.7
Streptozotocin (STZ)(3mg/kg) 9.0±0.21 5.02±3.2 156.0±12.3 160.56±7.6
Donepezil (5mg/kg)+ STZ (3mg/kg) 16.0±0.39 20.23±1.8 230.0±17.23 218±5.9
Terminalia catappa fruits Extracts 15.5 ± 2.8** 13.5 ± 1.4** 203.3 ± 15.3** 200.3 ± 7.3**
(100mg/kg) STZ (3mg/kg)
Terminalia catappa fruits Extracts 14.0±1.12** 18.3 ± 1.7** 218.0 ± 13.5** 208.0 ± 11.0**
(200mg/kg) STZ (3mg/kg)
Values are means ± S.E.M. (n=5); @p < 0.01 (vs. Control group), **p < 0.01 (vs. Negative control group)

Table No. 2 Effect of Terminalia catappa fruits extract on β amyloid in brain tissue
Treatment Aβ1-40 Aβ1-42
Vehicle control 50 ±1.12 14 ±1.12
Streptozotocin (STZ)(3mg/kg) 78 ± 2.8 25 ±1.8
Donepezil (5mg/kg)+ STZ (3mg/kg) 52 ± 0.39 20 ±1.23
Terminalia catappa fruits Extracts (100mg/kg) STZ (3mg/kg) 58 ± 0.21 17 ± 1.3**
``Terminalia catappa fruits Extracts (200mg/kg) STZ (3mg/kg) 55± 0.25 15± 13.5**
Values are means ± S.E.M. (n=5); @p < 0.01 (vs. Control group), **p < 0.01 (vs. Negative control group)

Table No. 3 Effect of Terminalia catappa fruits extract on AchEInhibiton Activity

Treatment AChE concentrated (μMol/minute/g of
tissue)
Vehicle control 6.74±0.18
Streptozotocin (STZ)(3mg/kg) 10.39±0.35
Donepezil (5mg/kg)+ STZ (3mg/kg) 5.68±0.28
Terminalia catappa fruits Extracts (100mg/kg) STZ (3mg/kg) 4.90±0.31**
Terminalia catappa fruits Extracts (200mg/kg) STZ (3mg/kg) 4.96±0.31**
Values are means ± S.E.M. (n=5); @p < 0.01 (vs. Control group), **p < 0.01 (vs. Negative control group)

Discussion in the AD rat. Decreased concentration of βA

Effect of TCFE on superoxide dismutase, catalase, peptide in the AD rat decreases the AchE level
reduced glutathione and Thiobarbituaric acid which increases the level of acetylcholine in the
reactive species in the brain tissue of STZ treated brain and thereby it protects the
AD rats were shown in Table 1.TCFE significantly neurodegeneration in STZ induced AD rats.
increased level of antioxidants in brain tissues ((P<
0.01)). β amyloid level of Aβ1-40 and Aβ1-42 in the Reference
brain tissue decreased significantly (p<0.01) in 1. A Joshi (2019) Neuroprotective activity of
TCFE treated group compared to AD rats (Negative Heliantus annusseeds in experimental mice
control group)(Table 2)STZ administration Alzheimer's & Dementia: The Journal of the
produced significant elevation in brain AchE Alzheimer's Association, 15(7),966
activity compared to control group of rats. 2. Joshi, A., &Malviya, N. (2019). Anti-Alzheimer
However, TCFEsignificantly inhibited (P< 0.01) of Activity of Hydroalcoholic Extract of
AchE activity in brain tissue as compared with the Buteamonosperma leaves. Journal of Drug
negative control group of rats. Delivery and Therapeutics, 9(2-A), 62-67.
3. Arutla S, Arra GS, Prabhakar CM. (1998). Pro-
Conclusion and anti-oxidant effects of some antileprotic
The current study concludes that TCFE possesses drugs in vitro and their influence on
neuroprotective effect in STZ induced AD rats. superoxide dismutase activity. Arzneim-
Study also suggests the mechanism of its action as Forsch J Drug Res., 48:10-24.
treatment with TCFE reduces oxidative stress 4. Beers RF, Sizer IW. (1952) Estimation of
which decreases the concentration of βA peptide catalase. J BiolChem 195:133

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EVALUATION OF ANTIBACTERIAL ACTIVITY OF ANNONA SQUAMOSA LEAVES EXTRACT

Jyoti Yadav, Ragini Pawar, Deepak Birla
Oxford International College, Indore, MP
[email protected],

ABSTRACT
From the very beginning the plants have been recognized as the most imperative source of the medicine. The
different phytochemicals derived from the different parts of plant provide the potential bioactive agent for
various disease treatment strategies. Microbial infections are one of the major health problems globally.
Although awareness about the disease and the ways to prevent it has been increasing during the last decade,
these diseases are the major causes of illness and death. Annona squamosa is a small, semi-deciduous tree, 3-7
m in height, with a broad, open crown or irregularly spreading branches; bark light brown with visible leaf
scars and smoothish to slightly fissured into plates; inner bark light yellow and slightly bitter; twigs become
brown with light brown dots(lenticels). The active ingredients in Annona squamosa include glycosides,
alkaloids, saponins, flavonoids, tannins, carbohydrates, proteins, phenolic compounds, phytosterols and amino
acids.
Keywords: Antibacterial, Annona Squamosa, Phytochemical Screening.

Introduction of Indore district. The entire specimen was rinsed

According to World Health Organization (WHO) with distilled water for the removal of traces of
medicinal plants are the best source to obtain a dust and soil present in the plant part. The dried
variety of drugs. Therefore, medicinal plants leaves of Annona squamosa were grinded in mixer
should be investigated to better understand their grinder and about 400 gm. of the powdered
1
properties, safety and efficiency . Microbial material was treated with. 95% ethanol using
4
infections are one of the major health problems continuous hot percolation method .
globally. Although awareness about the disease
and the ways to prevent it has been increasing Antibacterial screening
during the last decade, these diseases are the Antibacterial Sensitivity test by Disk Diffusion
major causes of illness and death. Annona Susceptibility Testing (Kirby-Bauer Method)
squamosa is a small, semi-deciduous tree, 3-7 m in
height, with a broad, open crown or irregularly Microorganisms used
spreading branches; bark light brown with visible The test organisms (Pseudomonas aureogenosa,
leaf scars and smoothish to slightly fissured into Staphylococcus aureus, Staphylococcus epidermis,
plates; inner bark light yellow and slightly bitter; Shigella flexineri, Bacillus substilis & E.Coli )
twigs become brown with light brown
2
dots(lenticels) . The active ingredients in Annona Culture Media: The medium used for the
squamosa include glycosides, alkaloids, saponins, activation of the microorganisms was nutrient
flavonoids, tannins, carbohydrates, proteins, broth. The nutrient agar media was used for the
phenolic compounds, phytosterols and amino antibacterial test.
acids. The plant is found to be rich in various
minerals like K, Ca, Mg, P, Cl, Na, Zn, S, Mn, Se, Ni, Concentration: Four different concentrations of
3
Cu etc . Annona squamosa extract was prepared (100, 75,
50, and 25%). 100% = 1 g crude extract in 1 ml of
Materials and methods freshly prepared double distilled water. Afterward,
serial dilution was prepared: 75% =75 mg in 1 ml,
5,6
Collection and Extraction of plant material 50% = 50 mg in 1 ml, and 25% = 25 mg in 1 ml .
The fresh plant part of Annona squamosa was
collected from local botanical garden and market

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Result and discussion

TABLE 1: Effect of Annona squamosa extract on inhibition of different bacteria
S. Microorganism Concentration (Zone of inhibition in mm)
NO
25% Conc. 50% Conc. 75% Conc. 100% Conc.
1. Bacillus subtilis 15 17 19 22
2 Shigella flexineri 12 14 17 21
3. S. epidermis 10 13 15 19
4. S. aureus 8 10 13 15
5. E. coli 11 13 16 19
6. P. Aeruginosa 9 11 15 19
The above observations suggest that different concentration (25%, 50 %, 75 % & 100 %) were having good
antibacterial activity against Streptococcus aureus, Streptococcus epidermis, Psudomonas aeriginosa, Shigella
flexineri, Escherichia coli and Bacillus subtilis. Thus the extract is showing varying activity against the entire
microorganism.

Table 2: Antibacterial activity of standard antibiotic (gram positive) against different bacteria.
Name of Name Standard antibiotics [zone of inhibition(mm)]
microorganisms TE OF AZ PC
S.aureus 15 16 16 14
B.subtilis 14 16 18 14
S.epidermidis 14 18 17 17
TE- Tetracycline, OF- Ofloxacin, AZ- Azithromycin & PC- Piperacillin

Table 3: Antibacterial activity of standard antibiotic (gram negative) against different bacteria.
Name of Name Standard antibiotics [zone of inhibition(mm)]
microorganisms FU GM CX NF
E.coli 12 16 11 16
S.flexineri 18 18 12 21
P. Aeruginosa 14 13 18 20
FU- Nitrofurantoin, GM- Gentamicin, CX- Cefotaxime & NF- Norfloxacin

Conclusion 3. Asolkar LV, et al. Glossary of Indian Medicinal

Indian literatures like Ayurveda and various Plants with Active Principles. New
ancient literatures have already mentioned herbal Delhi:Publication and Information Directorate;
remediation for a number of human ailments. 1992. p. 72-73.
Medicinal plants were the potent source of human 4. Kokate C.K., Plant Constituents Chapter 6 In:
health due to their active phytochemical Practical Pharmacognosy, Vallabh Prakashan,
th
compounds. In the present study tested the Delhi. 1997, 4 Edition, pp 107 - 111.
antibacterial property of Annona Squamosa plant. 5. Patel JD, Kumar V. Annona squamosa L.:
Phytochemical analysis and antimicrobial
References screening. J Pharm Res 2008;1(1):34-8.
1. Gupta AK,Chitme HR."Herbal Medicine for 6. Jennifer Billing and Paul W. Sherman
Health,The Eastern Pharmacist 2000: 41. “Antimicrobial functions of spices: why some
2. Easu K., Plant Anatomy, john Willey and Sons, like it hot". Q Rev Biol. 73 (1), 3–49.
New York, 1964, pp 767.

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EFFECT OF FLAVONOID FRACTION OF BUTEA MONOSPERMA ON RHEUMATOID ARTHRITIS:

AN IN VIVO STUDY
Akancha Godre*, Neetesh K Jain, Mahavir Chhajed
Faculty of Pharmacy, Oriental University, Sanwer Road, Jakhya, Indore, MP 453555 INDIA
[email protected]

ABSTRACT
Methanolic extract of Butea monosperma flowers (MEBM), ethyl acetate fraction (EAFBM) and the butanol
fractions (BFBM) of flavonoids were studied for chronic anti-inflammatory activity against Freund’s Complete
Adjuvant FCA induced paw edema Wistar albino rats. MEBM, EAFBM and BFBM at oral doses of 200 mg/kg and
400 mg/kg, dose-dependently inhibited the paw edema significantly. The acute toxicity study of MEBM and
flavonoid fraction showed there was no mortality or toxic reaction at fixed dose of 2000mg/kg body weight.
Keywords: Butea monosperma, anti-inflammatory activity, flavonoid fraction

Introduction Qualitative chemical tests of MEBM were

4-5
Rheumatoid arthritis is a systemic autoimmune subjected to occurrence of flavonoid.
disease with chronic inflammation characterized
by hyperplasia of synovial cells and angiogenesis in Preliminary In-Vivo Anti-Arthritic Activity
exaggerated joints, causes destruction of cartilages
and bone which is accountable for deformity and Selection of animals
1
disability. Traditional plant-based medicines still Wistar albino rats of either sex between 2 and 3
exert great deal of importance to people and months of age weighing 150-200 gm were
also serve as foundation to discovery of new drug selected. All animals were housed under normal
0
candidates for a variety of diseases. Chemical condition of 25±1 C, 12 hr light and dark cycle.
substances derived from natural source
encompass second hand to treat various human Acute toxicity studies
2
diseases. B. monosperma flower, family fabaceae, The acute oral toxicity study was approved as per
widely used in the acute and chronic inflammatory the OECD guidelines 423. MEBM, EAFBM and
conditions, showed presence of the flavonoids in BFBM suspensions were prepared by triturating
various extract. Any scientific evidence of activity dried extracts with 1% Tween 80 in distilled water.
of flavonoid fraction in chronic inflammatory Prior dosing, animals were fasted for 12 h and
conditions is not reported so far. water given ad libitum. Animals were weighed and
test substances were administered at dose of 2000
Materials and Methods mg/kg p.o. Observation was made during the first
The flowers of B. monosperma were collected in four hours after the drug administration to notice
the month of March, were taxonomically change and mortality up to 14 days.
authenticated by Dr. S. N. Dwivedi, Botanist, Janta
PG college, Rewa. The specimen herbarium sheets Evaluation of anti-arthritic activity
were submitted and preserve in Department. The rats were divided into nine groups of six
animals in each. For the induction of chronic
Preparation of Methanolic Extract & Flavonoid inflammatory response, Freund’s Complete
Fraction Adjuvant (FCA) 0.1 ml was injected through intra
250 gm dried powdered flowers of Palash were articular injection in left ankle joint of rats on 0
extracted with methanol in a soxhlet for 20 h. The day. Pre induction baseline was taken prior to the
solvent removes under reduced pressure, to injection of FCA measured by left paw volume of
obtain an orange powder 70 gm (MEBM). 10 gm each animal at 0 day for the induction of arthritis
MEBM was partitioned between water and ethyl in rats. The treatments with extracts were given
st 6
acetate. The ethyl acetate fraction was removed; once daily from day of injection to 21 day. The
the water phase was treated with n-butanol. The animal groups and results are reported in table 1.
solvents were removed under reduced pressure to
3
yield 0.8 gm EAFBM and 3.8 gm BFBM. Measurements of paw volume
Paw volume (ml) was measured at 0 days and
Preliminary Phytochemical Tests thereafter 4, 8, 12, 16 and 21 days of FCA post-

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6-7
inoculation. . Percentage inhibition=Vc- No toxic effects were observed at a higher dose of
Vt/Vt×100 2000 mg/kg body weight. Hence, 1/ 10th dose was
Where, Vc-Paw volume of control animals; Vt-Paw selected as therapeutic dose. The cut off value of
volume of treated animals 200 and 1/5 dose double of 400 mg/kg were
selected for anti-inflammatory activity.
Measurements of body weight
Body weight was deliberate of all groups at zero Anti-Arthritic Activity of Extracts & Fractions
st st
days and at 21 day after treatments over by with The assessment made on the 21 day showed that
8
a single pan weighing balance. the MEBM and fractions treatments at both doses
have moderate to highly significant effect and
Arthritis assessment reduced the adjuvant induced lesions in the
The severity of the arthritis in every paw was respective treatment groups as compared with the
6
quantified daily by a clinical score measurement. arthritis control group. In arthritic group, decrease
in body weight was observed on the subsequent
Statistical Analysis days, whereas groups treated with standard,
The results were analyzed by ANOVA followed by extract and fractions showed improvements in
th
Dunnet’s "t” test to decide the statistical body weight. This effect was observed from 14
significance. p<0.05 was selected as the level of day to last day of the experiment as compared to
significance. arthritic rats. Extract and fractions had moderately
and highly significant increase in body weight as
Results and Discussion compared to arthritic rats.
Acute Toxicity Studies of Extract & Fractions

Table No 1: Effects of extract & fractions on paw volume in FCA induced arthritis in rat
S. Paw Volume in mL
No Group Treatmen Zero
th
4 Day
th
8 Day
th
12 Day
th
16 Day
st
21 Day
. s t
#
Day
1 NC 0.28±0.0 0.32±0.02 0.31±0.02 0.30±0.04 0.30±0.03 0.31±0.11
4
2 AC 1% 0.30±0.0 0.52±0.04* 0.87±0.01* 0.93±0.05* 1.32±0.06* 1.64±0.02*
Tween80 2 * ** ** ** **
3 Std. 10 mg/kg 0.32±0.0 0.32±0.06* 0.42±0.18* 0.44±0.03* 0.51±0.04* 0.53±0.08*
7 * ** ** **
4 MEB 200 0.31±0.1 0.41±0.02 0.51±0.01* 0.61±0.04* 0.66±0.01* 0.72±0.02*
M mg/kg 0 * **
5 MEB 400 0.31±0.0 0.39±0.04 0.45±0.03* 0.53±0.03* 0.61±0.02* 0.62±0.01*
M mg/kg 1 * ** **
6 EAFB 200 0.31±0.0 0.43±0.05 0.51±0.03* 0.62±0.04* 0.71±0.04* 0.75±0.12*
M mg/kg 6 * *
7 EAFB 400 0.33±0.0 0.40±0.11 0.49±0.02* 0.55±0.02* 0.60±0.03* 0.66±0.03*
M mg/kg 4 * * **
8 BFBM 200 0.31±0.0 0.45±0.13 0.66±0.04 0.70±0.03* 0.79±0.03* 0.83±0.06*
mg/kg 4 * *
9 BFBM 400 0.32±0.0 0.45±0.12 0.60±0.03 0.63±0.03* 0.69±0.04* 0.73±0.06*
mg/kg 1 * ** **
# all dose administered p.o., Standard used was Prednisolone. NC: Normal Control. AC: Arthritic control. Values
are expressed as mean±SEM, n=6 in each group; * p <0.05, ** p<0.01, *** p <0.001, compared to disease
control

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Table No 2: Effects of extract & fractions on body weight in FCA induced arthritis in rat
#
S. No. Groups Treatments Days
st
Zero 21
1 NC 190.20±0.78 191.28±0.10
2 AC 1% Tween 80 191.40±0.18 162.13±0.11***
3 Prednisolone 10 mg/kg 191.80±0.20 213.31±0.18***
4 MEBM 200 mg/kg 191.18±0.40 210.20±0.12**
5 MEBM 400 mg/kg 190.20±0.50 214.21±0.05***
6 EAFBM 200 mg/kg 190.18±0.12 209.22±0.11**
7 EAFBM 400 mg/kg 192.25±0.40 213.61±0.11***
8 BFBM 200 mg/kg 191.10±0.65 211.33±0.12**
9 BFBM 400 mg/kg 190.50±0.20 216.49±0.19**
# all dose administered p.o., Standard used was Prednisolone. NC: Normal Control. AC: Arthritic control. Values
are expressed as mean±SEM, n=6 in each group; * p <0.05, ** p<0.01, *** p <0.001, compared to disease
control

Conclusion 2011. Anti-arthritic and antioxidant

It is observed that the MEBM and flavonoid activity of leaves of Alstonia scholaris
fraction have valuable effects in long lasting Linn. R.Br. European Journal of Integrative
lessening in rat paw edema, arthritic index. The Medicine, Vol. 3, pp. e83–e90.
mechanism may be mediated via the inhibition of 7. Ignacimuthu, S., Babu, N.P., Pandikumar,
prostaglandin synthesis in acute inflammatory P., 2011. Lysosomal membrane
feedback as well as inhibition of various lysosomal stabilization and anti-inflammatory
enzymes in unceasing inflammatory responses. activity of Clerodendrum phlomidis L.f., a
The present conclusions are noteworthy for the traditional medicinal plant. Journal of
development of alternative, reasonably priced and Ethnopharmacology, Vol. 135, Issue 3, pp.
perhaps safer strategies for the treatment of 779–785.
diseases. 8. Jalalpure, S.S., Yuvaraj, D., Mandavkar,
P.R., Khalure, G.S., Shinde, P., Shelar, A.,
References Shah, A.S., 2011. Anti-arthritic activity of
1. Kandaswamy, M., Narendhirakannan, various extracts of Mesua ferrea Linn.
R.T., Subramanian, S., 2007. Anti- Seed. Journal of Ethnopharmacology, Vol.
inflammatory and lysosomal stability 138, Issue 3, pp. 700– 704.
actions of Cleome gynandra L. studied in 9. to Evaluation of Botanicals. New Delhi,
adjuvant induced arthritic rats. Food and Business Horizons Pharmaceutical
chemical Technology, Vol. 45, Issue 6, pp. Publishers.
1001-12.
10. Kokate, C.K., 1996, Practical
2. Koehn, F.E., and Carter, G.T., 2005. The Pharmacognosy. Delhi, Vallabh
evolving role of natural products in drug Prakashan.
discovery. Nature Reviews, Vol. 4, pp.
11. Khandelwal, K.R., 2006. Practical
206-220.
Pharmacognosy. Pune, Nirali Prakashan.
3. Mukherjee, P.K., 2002. Quality Control of 12. Arulmozhi, S., Mazumdar, P.M.,
Herbal Drugs-an Approach to Evaluation
Sathiyanarayanan, L., Thakurdesai, P.A.,
of Botanicals. New Delhi, Business
2011. Anti-arthritic and antioxidant
Horizons Pharmaceutical Publishers.
activity of leaves of Alstonia scholaris
4. Kokate, C.K., 1996, Practical Linn. R.Br. European Journal of Integrative
Pharmacognosy. Delhi, Vallabh Medicine, Vol. 3, pp. e83–e90.
Prakashan.
13. Ignacimuthu, S., Babu, N.P., Pandikumar,
5. Khandelwal, K.R., 2006. Practical P., 2011. Lysosomal membrane
Pharmacognosy. Pune, Nirali Prakashan. stabilization and anti-inflammatory
6. Arulmozhi, S., Mazumdar, P.M., activity of Clerodendrum phlomidis L.f., a
Sathiyanarayanan, L., Thakurdesai, P.A., traditional medicinal plant. Journal of

International Journal of Pharmaceutical Sciences and Research: Conference Proceedings: Special ssue; March, 2020 Page | 132
International Journal of
Pharmaceutical Sciences and Research
ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

Ethnopharmacology, Vol. 135, Issue 3, pp. various extracts of Mesua ferrea Linn.
779–785. Seed. Journal of Ethnopharmacology, Vol.
14. Jalalpure, S.S., Yuvaraj, D., Mandavkar, 138, Issue 3, pp. 700– 704.
P.R., Khalure, G.S., Shinde, P., Shelar, A.,
Shah, A.S., 2011. Anti-arthritic activity of

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WOUND HEALING ACTIVITY OF FLAVONOID FRACTION OF JUGLANS REGIA LINN. IN

DIABETIC RATS BY DIFFERENT WOUND MODELS
Mayuri Choudhary*, Neetesh K Jain, Mahavir Chhajed, Urvashi Sharma
Faculty of Pharmacy, Oriental University, Sanwer Road, Jakhya, Indore, MP- 453555 INDIA
[email protected]

ABSTRACT
The present work is deals with study of the wound healing activity of flavonoid fraction of Juglans regia (FFJR)
in Diabetic Rats. The diabetes was induced by Streptozotocin in citrate buffer. The wound healing activity was
determined by Dead space, Incision and Excision wound models. The fasting blood glucose level in diabetic
animals were higher than those of normal animals. Topical application of flavonoid fraction, ointment base and
Povidone iodine on dorsal inter scapular region causes significant and faster rate of wound closure and
reduced epithelialization period. In incision wound model, there is a significant increase in skin tensile strength
by 10% w/w and 20% w/w ointment of FFJR compared to control. The hydroxyproline content was increased
significantly in dose dependant manner by 20% FFJR. FFJR significantly decreased the epithelialization period,
hence effect on the proliferative phase of wound healing.
Keywords- Juglans regia, Wound, Diabetes

Introduction Animals
Wound healing is a multifaceted and dynamic Male Wistar albino rats of 2-3 months of age
procedure of restoring cellular structures and weighing 150-200 gm were selected. All animals
0
tissue layers. These wounds may eventually pass were housed under normal condition of 25±1 C,
through the repair procedure without restoring 12 hr light and dark cycle, were fed with palatable
1
sustained anatomical and useful results. Plants or rat feed and water ad libitum.
chemical entities consequent from plants need to
be identified and formulated for treatment and Determination of preliminary phytochemicals
supervision of wounds. In this direction, a number The chemical tests were performed for the
of herbal products have been used in managing presence of flavonoids.
2
and treatment of wounds over the years. The
main aim of research, to augment the rate of Acute Toxicity Studies
healing of diabetic wounds using flavonoid fraction The acute toxicity study was carried out in rats by
of J. regia (FFJR) in the shortest time possible, with OECD guideline no. 425. The animals were
minimal pain, discomfort and scarring to the administered orally at dose level of 2000 mg/kg.
patient. At the site of wound closure, a supple and Then the animals were observed continuously for
3
fine scar with high tensile strength is desired. 3 h for general behavioral, neurological,
autonomic profiles and then after every 30 min for
Materials and Methods next 3h and finally for mortality after 24 hour till
14 days.
Procurement of Material Induction of Diabetes
Fruits of J. regia were procured freshly from the Diabetes was induced by a single i.p. injection of
local market were taxonomically authenticated by streptozotocin (STZ) (50 mg/kg) dissolved in 0.1 M
Dr. S. N. Dwivedi, Botanist, APS University, Rewa. of cold citrate buffer (pH 4.5) 15 min after the i.p.
administration of Nicotinamide (110 mg/kg body.
4
Flavonoid fraction preparation wt) in overnight fasted rats. After two weeks, rats
Fruits were shade dried and subjected to coarse with blood glucose level greater than 250 mg/dl
powder, was macerated with 70% methanol in were deemed as diabetic and used for the
dark and filtered to harvest a viscous supernatant, experiment.
dried under vacuum below 40°C. Methanolic Surgical Wound Models
extract was dissolved in water and taken in a Preparation of ointment
separating funnel and ether, ethyl acetate and Simple ointment of FFJR (5%, 10%, 20% w/w) was
butanol were added as per their polarity. A prepared using white soft paraffin ointment base.
butanol fraction was unruffled and dried under Povidone iodine ointment (5%w/w) was used as
5
vacuum to acquire flavonoid fraction. the standard drug.

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Excision Wound Parameters for wound healing activity

All the test sample and standard drug were applied The parameters for wound healing activity was
6-9
topically just the once a day after cleansing with determined by the reported methods
surgical cotton wool.
Procedure for wound creation Results and Discussion
2
A predetermined area of 500mm full thickness Total phenolics content in the crude extract was
skin was excised in the dorsal inter scapular found to be 224 mg/gm in terms of Gallic acid
region. The areas of the wounds were measured equivalent. Butanolic fraction was non toxic in
(sq.mm). All the test samples were applied acute toxicity study. Fasting blood glucose level
formerly daily. The wound area of each animal was was significantly reduced in treatment groups
measured on days 0, 2, 4, 6, 8, 10, 12 and 14 after table 1. In incision wound model, there is a
6
inflicting the wound. significant increase in skin tensile strength by 10%
Incision Wound Model w/w and 20% w/w ointment of FFJR and standard
One full thickness paravertibral incision of 1.5cm as compared to control group animals. The
length was made including the cutaneous muscles hydroxyproline content was increased significantly
depilated back of each rat. The test sample was in dose dependant manner by 20% FFJR (Table 2).
applied in a similar manner as in excision wound
7
model.

Table 1: Changes in blood glucose level (mg/dl) during study period.

Treatment Days
S. No. Group
0 7 14 28
1. NC 0.9% NS 110.3±2.21 112.4±3.45 121.2±2.31 121.4±3.12
2. DC 321.1±3.22 352.3±3.44 345.5±3.29 344.2±2.21
3. FFJR 200 mg/kg 321.3±4.31 301.8±4.13** 280.8±3.14*** 210.2±4.22***
4. FFJR 400 mg/kg 319.5±3.22 270.2±4.22*** 220.2±5.41*** 160.5±3.38***
NC: Normal Control. DC: Disease control. NS: Normal Saline, Values are expressed as mean±SEM, n=6 in each
group; * p <0.05, ** p<0.01, *** p <0.001, compared to disease control

Table 2: Effect of FFJR on wound area of excised uninfected wound, on tensile strength and by
Hydroxyproline content of excised uninfected wound in rats
2
Gr Treat Wound area in mm Tensile Hydrox
th th th th th th th th
ou ment 0 2 4 6 8 10 12 14 strengt yprolin
p (% h e
2
w/w (g/cm (μg/mg
) ) tissue)
Co 389.1 387.3 386.3 385.3 384.55 385.16± 382.83± 383.56± 87.50± 0.73±0.
ntr 2±3.3 4±4.2 4±9.2 7±4.73 ±5.44 9.46 5.55 8.77 7.15 04
ol 3 2 2
Std 5 390.3 388.8 380.2 375.1 361.16 355.66± 312.16± 301.50± 220.20 0.89±0.
3±4.9 3±8.3 2±8.4 6±6.77 ±5.34 6.66* 5.13** 5.24* ±9.41* 02***
1 4 4 *
FFJ 5 390.3 380.3 375.1 370.5 360.66 351.16± 312.50± 305.83± 158.31 0.68±0.
R 3±3.1 3±9.2 6±4.3 0±6.22 ±7.29* 6.19** 3.19** 7.86** ±5.22* 05
5 2 4
FFJ 10 383.5 371.6 365.1 355.3 340.33 320.16± 310.33± 290.16± 190.83 0.72±0.
R 0±6.8 6±7.5 6±8.1 3±8.42 ±4.57* 6.51** 7.09** 8.50** ±9.44* 03*
0 4 4 * * *
FFJ 20 388.0 370.3 365.8 350.5 340.33 331.66± 307.16± 280.50± 215.16 0.80±0.
R 0±2.3 3±4.3 3±8.4 0±8.78 ±9.18* 5.61*** 7.96*** 8.46*** ±8.56* 06***
0 3 5 * * *
Std-Povidone Iodine Ointment 5%w/w, NC: Normal Control. DC: Disease control. NS: Normal Saline, Values are
expressed as mean±SEM, n=6 in each group; * p <0.05, ** p<0.01, *** p <0.001, compared to disease control

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Conclusion 5. Sunilson AJ, Venkatanarayan R. 2004.

There was significant wound contraction by Wound healing activity of Jasminum
flavonoid fraction. It increases the number of sambac leaf extract. Adv Pharmacol
fibroblasts, collagen tissue and causes complete Toxicol. 5,1-10.
Epithelialization. Diabetic rats show delayed 6. Morton JJ, Malone MH. 1972. Evaluation
Epithelialization period compared to non-diabetic of vulneray activity by an open wound
rats. In our study, flavonoid fraction significantly procedure in rats. Arch International de
decreased the epithelialization period. So, Pharmacodyn Ther. 196, 117-26.
flavonoid fraction may have significant effect on 7. Ehrlich HP, Hunt TK. 1969. Healing
the proliferative phase of wound healing in potential of some natural agents. Annals
diabetic rats. An increase in tensile strength and Surg .170, 203-5.
hydroxyproline content of treated wounds in the 8. Lee KH, Krei CH. 1968. Efficacy of some
present study may be due to increase in collagen natural agents on dermal wounds. J
concentration and stabilization of fibers. Pharm Sci. 57, 102-4.
9. Nayak BS, Sandiford S, Maxwell A. 2009.
References Evaluation of the wound-healing activity
1. Nancy Broderick RN. 2009. Understanding of ethanolic extract of Morinda citrifolia L.
chronic wound healing. Nurse Pract Leaf. Evidence Based Compl Alt Med. 6,
34:17-22. 351-356.
2. Sandhya S, Sai Kumar P, Vinod KR, David 10. Ehrlich HP, Hunt TK. 1969. Healing
Banji, Kumar K. 2011. Plants as potent potential of some natural agents. Annals
anti diabetic and wound healing agents- A of Surgery .170, 203-5.
review. Hygeia JD Med 3:11-19. 11. Lee KH, Krei CH. 1968. Efficacy of some
3. Douglas MacKay ND, Alan L. Miller ND. natural agents on dermal wounds. Journal
2003. Nutritional support for wound of Pharmaceutical Sciences. 57, 102-4.
healing. Altern Med Rev 8:359-377. 12. Nayak BS, Sandiford S, Maxwell A. 2009.
4. Masiello P, Broca C, Gross R, Roye M, Evaluation of the wound-healing activity
Manteghetti M, Hillaire-Buys D, Novelli of ethanolic extract of Morinda citrifolia L.
M, Ribes G. 1998. Experimental NIDDM: Leaf. Evidence Based complementary and
development of a new model in adult rats Alternative Medicine. 6, 351-356.
administered streptozotocin and
nicotinamide. Diabetes 47:224-229.

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EFFECT OF METHANOLIC EXTRACT OF ALSTONIA SCHOLARIS IN DIFFERENT MODELS OF

DIABETIC NEPHROPATHY IN RATS
Urmila Sonata*, Ashish Pagariya, Neetesh K Jain, Mahavir Chhajed
Oriental University, Gate No.1, Sanwer Road, Jakhya, Opposite Revati Range, Indore, M. P.
(India)
[email protected]

ABSTRACT
Methanolic Extract of Bark of Alstonia scholaris plant was prepared and evaluated by different diabetic
nephropathy model. After assessment of activity, various biochemical parameters were measured. There was
a significant high level of blood urea nitrogen in diabetic nephropathy animals as compared to the normal
animals; 28 days treatment regimen showed significant reduction in elevated urea level. Elevated serum
creatinine level was observed in diabetic animals which were significantly reduced by treatment groups;
highest reduction was observed in methanolic extract group treated. Elevated serum creatinine level was
observed in diabetic control, nephropathy control and diabetic nephropathy control groups; after the
treatment with the drugs the creatinine level were significantly reduced. Urine protein and albumin excretion
were highly increased in diseased group. After the treatment regimen; group showed a significant effect on
urinary excretion profile. The drugs controlling both metabolic and hemodynamic process can effectively
revert the progressive diabetic nephropathy in diabetes patients.
Key Words: Alstonia scholaris, Methanolic extract, Diabetes Mellitus, Nephropathy, Ischemia Model

Introduction selected on basis of literature; traditional, tribal

Diabetic nephropathy or nodular diabetic and rural folk lore use.
glomerulosclerosis is a progressive kidney
disease caused by angioplasty of capillaries in Materials & Methods
[1]
the kidney glomerular. Diabetic nephropathy is Collection of plant materials
one of the important micro vascular complications Dried stem bark of A. scholaris collected in the
of diabetes mellitus and the most common cause month of March from Medicinal Garden (Nursery),
of chronic kidney disease (CKD) and end stage Mandsaur. All the plant materials were
[2]
renal disease (ESRD) in many countries. Type I taxonomically authenticated and by Dr. S. N.
diabetes is associated with a higher prevalence of Dwivwdi, Botanist, Janta PG college, APS
[3]
renal disease than type II diabetes. Slowing down University, Rewa. The specimen herbarium sheets
the progression of diabetic nephropathy, by were submitted and preserve in Department.
modifying the life style is the best way to reduce Preparation of Extract
[4]
mortality and maintain a high quality of life. Stem bark of A. scholaris was dried under shade
Nephropathy develops in about 20% - 40% of all and subjected to coarse powder for extraction
diabetic patients, with approximately 40% of process. Accurately weighed quantity of
patients with type 1 diabetes and 5 - 15% of barkpowder was extracted using 95 % methanol by
patients with type 2 diabetes, although the soxhlet apparatus. The extract was dried under the
incidence is substantially higher in certain ethnic reduced pressure to get crude extract. After
[5]
groups. In forthcoming years India will see an drying, weighed and percentage yield was
[7]
increase in the number of patients with diabetes determined.
and its complication; with 25 -40% of these
subjects likely to develop CKD and burden of the Preliminary In-Vivo diabetic nephropathy Activity
[6]
ESRD will rise. In present study, attempts have Selection of animals
been made to rationalize the scientific validity of Wistar albino rats of either sex between 2 and 3
methanolic extract of Alstonia scholaris (MEAS) months of age weighing 150-200 gm were
on diabetic nephropathy models. Plants selected selected. All animals were housed under normal
0
have antidiabetic as well as nephroprotective condition of 25±1 C, 12 hr light and dark cycle.
activity along with antioxidant and Acute toxicity studies
antihypertensive potential based on previous The acute oral toxicity study was approved as per
research work in this field. Plants for study were the OECD guidelines 423. MEAS suspension was
prepared by triturating dried extracts with 1%

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Tween 80 in distilled water. Prior to dosing, Pyrogallole Red end point method. Urinary
animals were fasted for 12 h and water given ad albumin excretion was estimated using
libitum. Animals were weighed and test bromocresol green (BCG) colorimetry test.
substances were administered at dose of 2000 Statistical analysis
mg/kg p.o. In first step, each dose was tested on The results were analyzed by ANOVA followed by
single rat and then administered to other rats. Dunnet’s "t” test to decide the statistical
Observation was made during the first four hours significance. p<0.05 was selected as the level of
after the drug administration to notice change in significance.
skin, fur, eye, mucus membrane, hyperactivity,
grooming, convulsions, sedation, hypothermia, Results and Discussion
tremor, salivation, coma, lethargy, body weight Toxicity Profile
[8]
and mortality up to 14 days. Methanolic extract was non toxic when subjected
[9]
Model I: Neonatal diabetic model to acute toxicity study at a dose of 2000 mg/kg. No
Neonatal diabetic model serves as a chronic characteristic behavioral, autonomic and
diabetes complication model resembling human neurological effects were observed. Hence,
prolonged diabetic complication. In this model the 200mg/kg and 400mg/kg were selected as dose of
2 day’s old litters were isolated from their extracts for overall study.
mothers. Pups were weighed and streptozotocin Model I: Neonatal Diabetic Model
(50 mg/kg in 0.1M citrate buffer pH 4.5) was Animals showed a slow progression in growth
injected by i.p. route. The pups were again placed compared to the normal animals of same age.
with their respective mothers. Animals having Treatment groups showed a significant increase in
fasting blood glucose levels more than 150 mg/kg body weight. Diabetic animals showed an increase
were selected for future screening. Animals were in food and water demand which was significantly
treated for 28 days. reduced by the extracts (Table1). During the
Sample collection experimental period the fasting blood glucose
th th th
Blood and urine were collected on 0 , 7 , 14 and level in diabetic animals were higher than those of
th th
28 day and organs were collected on 28 day of normal animals. However the fasting blood
commencement of experiment. Urine was glucose level was significantly reduced in
collected with the help of metabolic cages in the treatment groups. There was a significant high
graduated tubes and volume was measured. level of blood urea nitrogen in diabetic
Collected urine was used to assess biochemical nephropathy animals as compared to the normal
parameters. animals; 28 days treatment regimen showed
Assessment of biochemical parameters significant reduction in elevated urea level.
Tails of rats were sterilized with spirit and a small Elevated serum creatinine level was observed in
cut was made on tail with fresh blade and blood diabetic animals which were significantly reduced
glucose level was checked by glucometer. (Easy by treatment groups; highest reduction was
Gluco, Morepen Laboratories Ltd.; New Delhi). observed in methanolic extract group treated.
Blood urea nitrogen (BUN) and urinary urea Urinary protein, albumin excretion were highly
nitrogen (UUN), was estimated using glutamate increased in diabetic nephropathy animals and
dehydrogenase (GLDH) - urease method. Plasma & glucose was also found in urine of diabetic
urine creatinine were estimated using Modified animals; GFR was also increased to many folds in
Jaffe’s Reaction. Urine protein was estimated using the diabetic animals (Table 2).

Table 1: Changes in physiological parameters during study period

#
Treatment Parameters
Group Body weight Food intake Water intake Urinary output
(gm) (gm) (ml) (ml)
NC NS 211.7±6.01 32.83±1.51 34.17±0.79 9.83±0.31
DC NA 147.3±4.77 46.83±0.95 105.80±2.04 41.17±1.19
MEAS 200 mg/kg 197.2±4.11*** 36.31±0.41** 75.65±1.23*** 22.54±2.59**
MEAS 400 mg/kg 206.0±3.28*** 31.82±0.72*** 51.22±1.44*** 21.21±2.37***
# all dose administered p.o., Standard used was Prednisolone. NC: Normal Control. DC: Disease control. NS:
Normal Saline, Values are expressed as mean±SEM, n=6 in each group; * p <0.05, ** p<0.01, *** p <0.001,
compared to disease control

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Table 2: Changes in blood glucose, blood urea nitrogen and serum creatinine level during study period
blood glucose level (mg/dl) blood urea nitrogen (mg/dl) serum creatinine level (mg/dl)
Gr Days Days
ou 0 7 14 28
# 0 7 14 28 0 7 14 28
p
101. 16.5 14.67 15.67± 18.67± 0.36
98.0±3 103.2± 97.0±3 0.35± 0.33± 0.35±0
NC 3±2. 0±3. ±1.19 1.08 1.68 ±0.0
.22 2.32 .11 0.011 0.008 .004
33 33 28
312. 33.6 34.67 32.67± 32.67± 1.07
355.3± 363.5± 346.2± 1.14± 1.13± 1.19±0
DC 1±3. 7±2. ±1.33 3.80 1.70 ±0.0
5.67 11.09 12.12 0.019 0.014 .021
22 11 19
ME 299. 224.8± 132.2± 35.8 30.00 26.50± 27.22± 1.06 0.95±
315.8± 1.06± 0.75±0
20 3±4. 2.44** 1.27** 3±3. ±2.52 2.43** 2.42** ±0.0 0.029
4.19** 0.018 .032**
0 31 * * 23 24 *
ME 343. 263.2± 211.2± 116.5± 33.1 27.17 20.83± 21.31± 1.07 0.90± 0.79± 0.35±0
40 5±5. 2.44** 5.22** 3.48** 7±2. ±2.33 1.48** 3.68** ±0.0 0.009 0.014 .015**
0 20 * * * 45 * * * 18 * ** *
# all dose administered p.o., Standard used was Prednisolone. NC: Normal Control. DC: Disease control. NS:
Normal Saline, Values are expressed as mean±SEM, n=6 in each group; * p <0.05, ** p<0.01, *** p <0.001,
compared to disease control

Table 3: Changes in biochemical profile of urine during study period.

Group Treatment Urinary protein (mg/24 hrs) Urine albumin excretion (mg/24
hrs)
NC NS 18.17±2.48 2.81±2.04
DC NA 133.74±2.72 11.31±2.52
MEAS 200 mg/kg 78.33±2.25*** 8.53±1.28*
MEAS 400 mg/kg 56.27±1.44*** 6.13±1.44***

After the treatment for 28 days all group showed

highly significant results on urinary protein References
excretion. Elevated serum creatinine level was 1. Diabetic nephropathy. http://en.
observed in diabetic control, nephropathy control wikipedia.org/ wiki/Diabetic_nephropathy.
and diabetic nephropathy control groups; after the Accessed on: 09 april 2010.
treatment with the drugs the creatinine level were 2. Ha H, Hwang IA, Park JH, Lee HB. Role of
significantly reduced. Urine protein and albumin reactive oxygen species in the pathogenesis
excretion were highly increased in diseased group. of diabetic nephropathy. Diabetes Res Clin
After the treatment regimen; group showed a Pr 2008; 82 Suppl 1:42-45.
significant effect on urinary excretion profile 3. Mauer SM. Structural-functional
(Table 3). correlations of diabetic nephropathy.
Kidney Int 1994; 45:612-622.
Conclusion 4. Shumway JT, Gambert SR. Diabetic
The onset of diabetic nephropathy is often silent nephropathy-pathophysiology and
and progression is very slow, so it is difficult to management – a review. Int Urol
diagnose directly or reach on the stage to confirm Nephrol 2002; 34:257–264.
the disease. Diabetic kidney disease is 5. DeFronzo R. Diabetic nephropathy: etiologic
characterized by structural and functional changes. and therapeutic considerations. Diabetes
Metabolic, hemodynamic and genetic processes Rev 1995; 3:510-564.
contribute to the development of diabetic 6. Modi GK, Jha V. The incidence of end-stage
nephropathy. The drugs controlling both metabolic renal disease in India: A population-based
and hemodynamic process can effectively revert study. Kidney Int 2006; 70:2131–2133.
the progressive diabetic nephropathy in diabetes 7. Eddouks M, Maghrani M, Zeggwagh NA,
patients. Michel JB. Study of the hypoglycaemic

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ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

activity of Lepidium sativum L. aqueous 9. Hamedan WAA. Protective effect of

extract in normal and diabetic rats. J Lepidium sativum L. seeds powder and
Ethnopharmacol 2005; 97:391–395. extract on hypercholesterolemic rats. Am J
8. Bafeel SO, Ali SS. The potential liver toxicity Sci 2010; 6(11):873-879.
of Lepidium sativum seeds in albino rats.
Res J Biol Sci 2009; 4(12):1250-1258.

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STUDY OF THE ANTINOCICEPTIVEEFFECT OF ANNONASQUAMOSA LEAF EXTRACT IN MICE

AchlaVyasa*, AyushiNigama, KapilVyasb and R. K. Nemaa
a
Lakshmi Narain College of Pharmacy (RCP), Revati, Sanwer Road, Indore, M.P., India.
453331
b
SymbiotecPharmalab Pvt. Limited, SEZ, Pithampur, M.P., India.
Mrs. AchlaVyas, Lakshmi Narain College of Pharmacy (RCP), Revati, Sanwer Road, Indore,
M.P., India. 453331,
[email protected]

ABSTRACT
Annonasquamosa, a plant famous for the sweetness of its fruits, earlier research shows, bark, leaves, seeds, of
this plant have many medicinal properties like analgesics, antioxidant, antibacterial, antifungal, antiulcer,
anticancer, antidiabetic. Sickness/Grievance is identified by pain and it’s very sore for the patient. Analgesics
synonym of antinociceptive/pain killers used to treat the soreness. Organic molecules/synthesized molecules
create a dependency for our body and after period cells create tolerance for the respective molecule/drug. As
currently, a number of antinociceptive molecules are available to heal pain; however, it's required to carry out
work on the outmoded medication system. In this study, we worked on Annonasquamosaleaves to determine
its antinociceptive properties. In this research, the ethanolic extract obtained from the leaves of
Annonasquamosa is obtained and after performing phytochemical screening, tail-flick method and the acid-
induced Writhing test is used for the examination of antinociceptive activity of methanolic extract of
Annonasquamosa leaves.
Keywords:-Antinociceptive activity, tail-flick method, acid-induced Writhing test, Annonasquamosa,
phytochemical screening.

Introduction The mature leaves of Annonasquamosa were

Antinociceptives are very common nowadays we collected from the medicinal garden of Lakshmi
use mostly to reduce pain but we innovate more Narain College of Pharmacy (RCP) Indore in the
potency of the drug in less amount of drug with month of September and authenticated by
avoid side effects. Pain is the most common sign of botonist. After collection leaves were washed with
any disease, injuries. This is the herbal effective water to remove the adhering soil, mud, and
molecule we used in this activity and the most debris and all insect damage or fungus infected
important thing there is no side effect of the leaves were removed. After drying the leaves in
herbal drug. We want to reuse that traditional shade at room temperature was coarsely
culture with modification of science. Sugar apple powdered using blender and finally the powder
plantcommonly known as sitafal having scientific was stored in an air tight container and protected
name AnnonaSquamosais species of the genus from light. 45 g powdered drug taken in filter
1
Annona and member of the family Annonaceae . paper bag and kept this bag on soxhlet, then after
Plant famous for the sweetness of its fruits, earlier we added solvent (methanol) in small quantity up
research shows, bark, leaves, seeds, of this plant to 450 ml. we extracted for 24 hrs at constant
have many medicinal properties like analgesics, temperature 40°C. Result of evaporation process
antioxidant, antibacterial, antifungal, antiulcer, result we get a dark green colour sticky product.
anticancer, antidiabetic. The whole plant of
Annonasquamosa possesses medicinal values Phytochemical screening
apart from its sweet taste. The seeds of the plant Phytochemical screening of plant leave extract
2 3
are found to antidiabetic anti thyroid , shows presence of Alkaloids, Glycosides,
4 5
antioxidant , and anti-lice activity . On the other Flavonoids, Phenolic & tannins, Sterol,
hand, the whole plant extract and the leaves are Carbohydrates.
6
found to possess anti lipidemic and vasorelaxant
7
acitivity . Experimental& Methods
Animals
Material and Methods Wistar Albino mice weighing select for the activity
Collection of plant material& Extraction had free access to food and water and they were

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housed under a natural (12 h each) light-dark cycle Note the onset of writes. Calculate the mean
with access to standard pellet chow and water and writhing response of control, standard, and test
acclimatized for 5 days to the laboratory group.
conditions before performing the experiments.
Result& Discussion
Tail Flick method Pain is a subjective experience, which is difficult to
In tail flick method we adjust the tail of mice over define exactly even though everyone experiences
the heat source and note the time of tail it. Screening of centrally and peripherally acting
withdrawal from the radiant heat source. Mice are analgesic activity to intraperitoneal injection of
divided into three groups, first group is control noxious chemicals is performed by the tail flick
group, to this group distil water orally given by method and the writhing response of the animals.
feeder needle, stander drug paracetamol Acetic acid causes algesia by liberating
(100mg/kg) given to the second group is, the third endogenous substances that excite the pain nerve
group is given Annonasquamosa leaves to extract endings.
a three different dose(100 , 200, 500mg/kg). From the results it is apparent that the ethanolic
extract of Annonasquamosa showed a significant
Acid induced Writhing test antinociceptive effect in the tail flick method and
In this study we are using three groups of animals writhing response which is comparable to the
first is a control that we administered acetic acid standard. There are reports on the role of tannins
1% (1ml/100g) according to the bodyweight of the and flavanoids in antinociceptive activities. The
animals. Place them to a glass jar and note the extract of Annonasquamosa leaves was found to
response of abdominal constriction, trunk twist possess significant analgesic activity which is quite
response and starching of legs response for 10 comparable to paracetamole. Furthermore a
min. the second group we used standard drug detailed investigation on the extract is underway
indomethacin (20 mg/kg) after 15 min of acetic to determine the phytoconstituents that are
acid administration. Note the onset of writes. The responsible for these activities as well as to define
third group we used Annonasquamosa leaves the exact mechanism of action of the herbal drug.
extract after 15 min of acetic acid administration.

Table:1 Results obtained from tail flick method

Basal Reaction Reaction Time after drug
Treatment Dose Time(sec.) administration (sec)
i ii iii 15 min 30 min 45 min 60 min
Control Distil. water 2 3 2 2 3 2 4
Standard drug(PCM) 100 mg/kg 1 3 3 3 5 7 9
Annonasquamosa leaves
100 mg/kg 2 3 3 3 6 7 8
extract
Annonasquamosa
200 mg/kg 2 2 3 4 6 9 12
leaves extract
Annonasquamosa
500 mg/kg 1 2 3 5 8 10 14
leaves extract

Results from Acid induced Writhing test

Table:3 Results obtained from acid induced Writhing test are tabulated below:
Duration of paw licking (seconds)
Group Dose (mg/kg) st nd
1 Phase Inhibition % 2 Phase Inhibition %
Control Distil. water 86.62 + 3.18 - 93.87 + 2.73 -
Standard drug(PCM) 100 mg/kg 85.87 + 2.88 - 91.25 + 3.07 -
Annonasquamosa leaves extract 100 mg/kg 66.12 + 2.13 23.67 65.62 + 1.72 30.09
Annonasquamosaleaves extract 200 mg/kg 47.62 + 2.13 45.02 46.67 + 1.68 50.20
Annonasquamosa leaves extract 500 mg/kg 16.21 + 0.14 81.24 19.37 + 0.94 79.36
Conclusion

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Phytochemical Screening shows the presence of 4. Kaleem M, Asif M, Ahmed QU and Bano B:
Alkaloids, Glycosides, Flavonoids, Phenolic & Antidiabetic and antioxidant activity of
Tannins, sterol and carbohydrates in ethanolic Annonasquamosa extract in streptozotocin-
extract of leaves of Annona squamosal. Results induced diabetic rats. Singapore Medical J.
obtained from Table-1 and Table 2 shows Annona 2006; 47(8): 670-675. Research J.
squamosa leaves have significant antinociceptive Pharmacognosy and Phytochemistry 2012;
effect and analgesic activities as compared to 4(3): 182-185
standard drugs, and it is confirmed by tail flick 5. Intaranongpai J, Chavasiri W andGritsanapan
method and writhing response. W: Anti-head lice effect of Annonasquamosa
seeds. The Southeast Asian J Tropical Med
References Public Health. 2005; 37(3): 532-535.
1. Rathore DS. Custard Apples In: Bose TK, Mitra 6. Gupta RK, Kesari AN, Diwakar S, Tyagi A,
SK, eds. Fruits: Tropical and sub-tropical, Tandon V, Chandra R andWatal G: In vivo
Calcutta: NayaProkash; 1990. p. 449-468. evaluation of anti-oxidant and anti-lipidimic
2. Gupta RK, Kesari AN, Murthy PS, Chandra R, potential of Annonasquamosa aqueous
Tandon V and Watal G: Hypoglycemic and extract in Type 2 diabetic models. J
antidiabetic effect of ethanolic extract of Ethnopharmacol. 2008; 1: 21-25.
leaves of AnnonasquamosaL. in experimental 7. Morita H, Iizuka T, Choo CY, Chan KL, Takeya K
animals. J Ethnopharmacol. 2005; 99(1): 75- and Kobayashi J:Vasorelaxant activity of cyclic
81. peptide, cyclosquamosin B, from
3. Panda S, Kar A:Annonasquamosa seed extract Annonasquamosa. Bioorg Med ChemLett.
in the regulation of hyperthyroidism and lipid- 2006a; 16(17): 4609-461
peroxidation in mice: possible involvement of
quercetin. Phytomedicine. 2007; 14(12): 799-
805.

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ASSESSMENT OF ANTI‐DIABETIC AND ANALGESIC PROPERTIES OF HYDROALCOHOLIC

EXTRACT OF SARCOSTEMMA ACIDUM IN RAT
Yashraj Yadav1*, Neeraj Sharma1, Karunakar Shukla2, Ankur Agrwal1
1
Oriental College of Pharmacy & Research, Oriental University, Indore [MP]
2
College of Pharmacy, APJ Abdul kalam University Indore [MP]
[email protected]

ABSTRACT
Objective: Present study was aim to evaluate a hypoglycaemic and analgesic activity of hydroalcoholic extract
of sarcostemma acidum in rat. Materials and Methods: all animal was divided in five group; the Experimental
diabetes was induced by a single injection of streptozotocin in rats. Acute pain was evaluated by using hot-
plate method by administration of Diclofenac sod. 10 mg/kg. Result: Our results show that hydroalcoholic
extract of sarcostemma acidum was significantly prevent (P < 0.001) analgesic and reduce glucose level on
blood Conclusion: It was observed that hydroalcoholic extract of sarcostemma acidum was to reduce glucose
level and analgesic activity
Keyword: Anti‐Diabetic, Analgesic, Sarcostemma Acidum

Introduction M.P. with Voucher specimen No. SG/KN/3210.

Sarcostemma acidum is an Indian traditional Extraction and Phytochemical identification
medicinal plant. It has been categorized as test:The dried ariel part of Sarcosteema acidum
candidate of Soma plants by various authors. It were powdered and defatted by petroleum ether
was said that Soma (Somlata) was used to prepare and hydroalcoholic (ethanol) solvent in equal ratio
‘Somras’ (Rejuvenating drink) by Aryans. Chemical (3:1) at room temperature with occasional shaking
constituents - Malic acid, Succinic acid, Reducing Finally, a highly concentrated ethanolic extract
5
sugar – sucrose, Traces of tannin, Alkaloids, were obtained. Phytochemical screening of the
Phytosterols, Alpha & beta amyrins, Lupeol & extracts was carried out according to the standard
6,7
lupeol acetate, Beta sitosterol. Diabetes Mellitus procedures All extracts were subjected to
(DM) is a systemic metabolic disease characterized preliminary phytochemical screening to identify
by hyperglycaemia, abnormal elevated levels of the various phyto-constituents present in them i.e.
1
lipid, and fat in blood and hyperinsulinemia. These alkaloids, terpenoids, glycosides, steroids,
drugs tend to cause side effects like nausea, triterpenoids, flavonoids, carbohydrates, saponins
vomiting, abdominal pain, diarrhoea, head ache, and tannins.Acute toxicity studies: Animals were
abnormal weight gain, allergic reaction, low blood selected at random from animal house of faculty
glucose, dark urine, fluid retention, or of Pharmaceutical Science & Technology (FPST),
2
swelling. Moreover, they are not safe for use AKS University, Satna AKS University Satna MP,
during pregnancy. Active research has been India. Animals were housed in relative humidity of
performed on traditionally available medicinal 30.7 % at 22 ± 2 °C and 12:12 light and dark cycle.
plants for the discovery of new antidiabetic drug All animal experiments were approved by IAECof,
as an alternative for synthetic drugs. Hence the faculty of Pharmaceutical Science & Technology
current study is focussed to evaluate the (FPST), AKS University, Satna (CPCSEA Reg No. -
antidiabetic potential of selected medicinal 2056/PO/RC/S/CPCSEA/19)The acute toxic class
3
plants. Pain has been officially defined as an method was done as OECD guideline 423
unpleasant sensory and emotional experience .Streptozotocin induced antidiabetics activities in
associated with actual or potential tissue damage. rat: All experimental animal divided in four group -
Therefore, search for new analgesic drugs with I is control (only DMSO)group -II is given only
promising pharmacological actions has become an streptozotocin group -III to IV(HASA-200 and 400)
4
urgent need. is treatment group. The Rats were fasted overnight
and experimental diabetes was induced by
Materials and methods intraperitonealinjection of 55 mg/kg body weight
Plant material collection the plant from Local of streptozotocin (STZ; Sigma) dissolved in freshly
Garden of Indore and was authenticated by prepared citrate buffer (0.1 mol/L, pH 4.5).group-I
Dr.Karunkar Shukla Principal and Professor College is revised only DMSO whereas remain all group
of Phamracy,Dr.APJabdul Kalam university Indore received streptozotocin as inducer and

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interventional agent and The hyperglycaemia was fore- and hind-paws and bounced out of the hot
induced experimentally by a single intraperitoneal plate before and 15, 30, 45 and 60 min following
9
dose administration and the blood glucose level administration of test agents.
was measured after 48 hr using a glucometer.
Analgesic activity by Hot Plate Method: All groups Results
of 4 rats each were utilized for this study after 15 a).Phytochemicalidentification of Hydroalcoholic
days wash up period. Group I (control) animals extract of sarcostemma acidum(HASA): after the
received the vehicle (normal saline, 5 mL/kg, performed phytochemical test alkaloids phenol
orally), whereas Group II and group III carbohydrate, tannin, flavonoid and saponin found
respectivelyHASA 200 and HASA400 mg /kgorally in HASAb). Oral administration of test extract of
respectively. Group IV animals received the Hydroalcoholic extract of sarcostemma acidum
standard (Diclofenac sod. -10 mg/kg) respectively (HASA) in rats did not produced any signs of
(S.C.). The animals were positioned on an toxicity and mortality up to 2000 mg/kg. These
aluminium hot plate maintained at a temperature findings indicated that extract is safe.
of 55 ± 0.5 °C for a maximum time of 30s. Reaction c). Streptozotocin induced antidiabetics activities
time was recorded when the animals licked their in rat

Table 01. Streptozotocin induced antidiabetics activities in rat

Treatment of Groups Blood Glucose level mg/dl Blood Glucose level mg/dl
Fasting -12 hr After meal
Group 1 (NS) 79.55±1.8 93.80±2.5
Group 2 (Streptozotocin only) 206.77±4.2 216.45±3.3
a a
Group 3(HASA 200 mg) 170.87±1.2 * 188.60±2.4 *
a a
Group 4(HASA 400 mg) 169.0±1.6 * 155.13±2.6 *
Group 5 (Standard) 74.05±4.0* 94.80±3.1*
Values are mean ± SD, n=4, One‑way ANOVA followed by Bonferroni multiple comparison tests. a is compared
to group 2 which is a diabetic control group, *p <0.001; there is a statistically significant difference (P =
<0.001).

STZ induced antidiabetics activities in rat

250
blood Glucose level mg/dl

200
150
100
50
0

mean(fasting) mean(after meal 120 min )

Figure 1. IC50 value of Rottlerin and standard drugs on aldose reductase , α-glucosidase and α-amylase
enzymes.

Table 02. Analgesic activity in Eddy's hot plate model

0 Min 30 min 60 min 90 min
Group 1(NS) 5.6±0.47 5.7±0.56 5.8±0.51 5.7±0.55
a
Group 2(HASA 200mg) 5.7±0.48 6±0.22 7.1±0.62 12±0.77 *
a a
Group 3(HASA 400mg) 5.8±0.38 6.1±0.18 10.1±0.28 * 14.5±0.81 *
Group 4 (std) Diclofenac sod 5.9±0.15 9.3±0.41* 17.2±0.61* 22.5±0.63*
Values are mean ± SD, n=4, One‑way ANOVA followed by Bonferroni multiple comparison tests. a is compared
to group 1 which is a control group, *p <0.001; a statistically significant difference (P = <0.001).

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Analgesic activity in Eddy's hot plate model

25
Reaction Time (Sec)

0
0 Min 30 min 60 min 90 min
Group 1(NS) Group 2(EAC 200mg ) Group 3(EAC 400mg ) Group 4 (standard) Diclofenac sod

Discussion the efficacy of the plant extract as a potential

the experimental results have indicated in Table. analgesic drug and to demonstrate a positive
1As expected in the diabetic control, there was result.
severe hyperglycemia as compared to the normal
animals. Compared to the diabetic control, all the Conclusion
two extracts (HASA 200 and HASA 400 mg) Streptozotocin has been shown to hydroalcoholic
lowered the elevated blood glucose levels only in extracts Extract in the dose of 400 mg/kg reduced
subacute treatment. It was observed that the the reduction in the blood glucose levels
standard drug glibenclamide lowered the blood compared to Extract in the dose of 200 mg/kg. The
glucose level significantly, bringing it nearly back literature reports reveal that phenol, polyphenol,
to normal, whereas HASA 200 and HASA 400 mg flavonoids and tannins present in the plant extract
significantly (P < 0.01) decreased fasting blood known to possess antihyperglycemic activity.
serum glucose in the diabetic rats on as Antihyperglycemic potential of test extract was
compared to fasting blood serum glucose levels. observed may be due to presence of active
HASA 400 mg extract as less lowering blood phytoconstituents like flavonoid and phenolic
glucose level after meal as compare to fasting content which was evident by preliminary
The analgesic activity of the HASA was examined phytochemical screening. In the present
using Hot plate method. Animals were divided into investigation demonstrated hydroalcoholic extract
four groups, each group containing for 4 animals of sarcostemma acidum has the significant anti-
each. Group I served as the control with no diabetic and analgesic
protection. Group 4 animals received the standard References
drug of Diclofenac sod. -10 mg/kg body weight, 1. Dave BK, Dhirawat R, Kumawat M.
whereas group 2 and 3 animals were orally Pharmacognostical study of a medicinal
administered the plant extracts viz., 200 and 400 plant of India–Sarcostemma acidum. Int J
mg/kg body weight respectively. There is no Pharm Phytochem Res. 2014;6:690-7.
significant response at 0 min in all groups due to 2. Vijayalakshmi K, Selvaraj IC, Sindhu S,
Initiation of dose. after 30 min reaction time is Arumugam P. In vitro investigation of
increase in extract group as compare to group 1 antidiabetic potential of selected
but no marked reaction time noted. After 60 min traditional medicinal plants. IJPPR.
interval the reaction time is significate increase in 2015;6(4):856-61.
standard and group 3 HASA 400 mg where 200 mg 3. Hasan SR, Hossain MM, Akter R, Jamila M,
HASA not show significant response in 60 mi. After Mazumder ME, Alam MA, Faruque A,
90 min interval group 2 to 4 show most significant Rana S, Rahman S. Analgesic activity of
(P<0.01) as compare to control group. The result of the different fractions of the aerial parts
hot plate test indicates that the extract has of Commelinabenghalensis Linn. Int J
marked analgesic effects with a reasonable safety Pharmacol. 2010 Jan 1;6(1):63-7.
profile and possesses the ability to reduce 4. Soulimani R, Fleurentin J, Mortier F,
centrally mediated pain. This attempt is to prove Misslin R, Derrieu G, Pelt JM. Neurotropic

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action of the hydroalcoholic extract of aqueous-ethanolic extracts of Ricinus

Melissa officinalis in the mouse. Planta communis leaves on streptozotocin-
Medica. 1991 Apr;57(02):105-9. induced diabetes in rats. PeerJ. 2019 Feb
5. Gokhale SB, Kokate CK, Purohit AP. A text 18;7:e6441.
book of Pharmacognosy. NiraliPrakshan, 8. Das M, Gohain K, Das S. Evaluation of
Pune, India. 1993:345-8. Central and Peripheral Analgesic Activities
6. Evans WC. Trease and evans' of Solanum Melongena Ethanolic Leaf
pharmacognosy E-book. Elsevier Health Extract In Experimental Animals. Group.
Sciences; 2009 May 27. 2017 Mar 1;5:0-9.
7. Gad-Elkareem MA, Abdelgadir EH,
Badawy OM, Kadri A. Potential
antidiabetic effect of ethanolic and

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ANALYTICAL METHOD DEVELOPMENT AND VALIDATION FOR SIMULTANEOUS

ESTIMATION OF ERTUGLIFLOZIN AND SITAGLIPTIN IN TABLET FORMULATIONS BY RP-HPLC
METHOD
Tahir Nizami*, Ankit Mangal, Namrata Rathore, Darshana Sharma, Neelesh Malviya
Smriti College of Pharmaceutical Education, 4/1 Pipliya Kumar, MR-11, Dewas Naka,
Indore-452010 (M.P), INDIA
[email protected]

ABSTRACT
An accurate, simple and economical RP-HPLC method using a PDA detector at 240 nm wavelength for
simultaneous estimation of Ertugliflozin and Sitagliptin in pharmaceutical dosage forms has been developed.
The method was validated as per ICH guidelines over a range of 3.75-22.5 μg/mL and 25-150 µg/ml for
Ertugliflozin and Sitagliptin respectively. Analytical column used was ACE Column C18, (150 mm x 4.6 mm i.d,
5μm) with flow rate of 1.0 mL / min at a temperature of 30°C ± 0.5°C. The separation was carried out using a
mobile phase consisting of buffer (Potassium dihydrogen Ortho Phosphate): Acetonitrile (70:30v/v). Retention
times of 2.91and 4.42 and min were obtained for Ertugliflozin and Sitagliptin respectively. The percentage
recoveries of Ertugliflozin and Sitagliptin are 100.12% and 99.42% respectively. The relative standard
deviations are always less than 2%.
Keywords: RP-HPLC, Ertugliflozin, Acetonitrile

Introdcution Sample Preparation of Standard Stock Solution

Ertugliflozin is (1S,2S,3S,4R,5S)-5-(4-chloro-3- Standard stock solution of ERTU was prepared by
(4ethoxybenzyl) phenyl)-1-(hydroxymethyl)-6,8- dissolving 2.5 mg of ERTU in 25 ml of diluent in a
dioxabicyclo[3.2.1]octane-2,3,4-triol, compound 25 ml clean dry volumetric flask separately and the
with (2S)-5oxopyrrolidine-2-carboxylic acid Fig 2.3 standard solutions was filtered through 0.45μm
is potent and selective inhibitors of the sodium- nylon membrane filter and degassed by sonicator
dependent glucose co transporters (SGLT). to get the concentration of 100μg/ml of ERTU. In
Sitagliptin chemically7-[(3R)-3-amino-1-oxo-4- separate volumetric flask same procedure was
(2,4,5-trifluorophenyl)butyl]-5,6,7,8tetrahydro-3- followed by taking 25 mg of METF to produce
(trifluoromethyl)- 1,2,4-triazolo[4,3-a] pyrazine standard stock solution of 1000μg/ml of METF.
phosphate (1:1) monohydrate. Sitagliptin is a The above standard stock solutions suitably
highly selective DPP-4 inhibitor. diluted with diluents to obtain various
concentrations of ERTU and METF.
Material and Methods
Preparation of Working Standard Solution 20
Materials Milli-Q Water, HPLC grade Acetonitrile, tablets were accurately weighed and powdered
Water, Methanol (Milli-Q Water, Mumbai) and powder equivalent to 15mg ERTU and 100mg
Monosodium Phosphate, Di sodium Phosphate, of SITA were taken into a 100ml clean and dry
Phosphoric acid, sodium Hydroxide, Acetonitrile volumetric flask, diluent mixture was then added
was obtained from SD Fine Chemicals Pvt. and solution was sonicated in order to dissolve
Ltd.,Ahmedabad, India . final volume was made up to the mark with the
diluent mixture. The above sample solution was
Instrumentation Chromatographic system then filtered and diluted suitably to achieve
consisted of a Waters Model Alliance 2998 concentration of 150µg/ml of ERTU and
separation module equipped with auto sampler 1000µg/ml of SITA respectively.
Photodiode array ultraviolet (UV) detector. The
data recorded using empowers software. The Validation parameter The method was validated
column used was ACE Column C18, (150 mm x 4.6 according to ICH guideline for linearity, precision,
mm i.d, 5μm) and samples were eluted using accuracy, selectivity. Selectivity was checked using
Acetonitrile and Water, 50:50v/v as the mobile ERTU and SITA and a mixture of standards in order
phase at a flow rate of 1ml/min. to optimize separation and detection. Linearity of
the method was performed by analyzing a

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standard solution of drugs by the method in the the extraction process. The mean amount and
concentration range 3-15 μg/ml for ERTU and 25- standard deviation (SD) value of each constitute
150 µg/ml μg/ml for SITA respectively. The were calculated.
accuracy of the proposed method was determined
by a recovery study carried out by addition Results and Conclusion
method. The samples were spiked with three The results showed that the method provided
different amounts of standard compounds. The adequate accuracy, precision, sensitivity,
spiked samples were extracted in triplicate and reproducibility with better resolution for the
analyzed under the previously established optimal simultaneous analysis of ERTU and SITA. The
conditions. The obtained average contents of the advantages of proposed method are its short
target compounds were used to calculate the analysis time and a simple procedure for sample
spike. Precision was determined by repeatability preparation. The RP-HPLC method developed for
and inter-day and inter-day reproducibility simultaneous analysis of ERTU and SITA can be
experiments. Standard solution containing ERTU used for routine quality control of their bulk drug
and SITA were injected six times. Drugs were also mixture and their combined dosage form.
extracted six times to evaluate the repeatability of

Fig 1: Chromatogram of standard

References University, Volume 55, Issue 2, 2017, 311-

1. Hanan A.etval, Merey, Nesrin K. Ramadan, 317.
Sherine S. Diab, Azza A. Moustafa 2. Harmonised Tripartite Guideline: Validation
Chromatographic methods for the of Analytical Procedures: Methodology (Q2B)
simultaneous determination of binary 2005. International Conference on
mixture of Saxagliptin HCl and Metformin Harmonisation (ICH), 2005.
HCl, Bulletin of Faculty of Pharmacy, Cairo

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REVERSE MOLECULAR DOCKING STUDIES AND IN VITRO EVALUATION OF ROTTLERIN FOR

ANTIDIABITIC ACTIVITY
Kushagra Dubey*1,Raghvendra Dubey2, Revathi A. Gupta2, Arun Kumargupta3
* 1Department of Pharmaceutical Chemistry, Smriti College of Pharmaceutical Education,
4/1 Pipliya Kumar, MR-11, Dewas Naka Indore, Madhya Pradesh 452010, 2Department of
Pharmaceutical Chemistry , Matoshri Institute of Pharmcy ,Dhanore, Maharashtra 423401
3Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Dr. A.P.J. Abdul Kalam.
University, Indore Bypass Road, Near Omaxe city 1, Indore District, Arandia, Madhya
Pradesh 452016, 4Department of Pharmaceutical Chemistry, Chameli Devi College of
Pharmacy, Khandwa Road, Village, Umrikheda, Near Toll booth, Indore, Madhya Pradesh
[email protected]

ABSTRACT
The present study demonstrates the potential plant isolate, Rottlerin against the enzymes aldose reductase, α-
glucosidase, and α-amylase involved in diabetes and its complications. The MolDock score, Rerank score, and
Hydrogen Bond Interactions were calculated by Insilico Reverse molecular docking approach for using Molegro
Virtual Docker (MVD) Software. The MolDock Score found to be -183.531 against aldose reductase, -159.613
against α-glucosidase and -169.276 against α-amylase respectively, which was much higher than standard
ranirestat -151.57 against aldose reductase and acarbose -125.08 & -157.32 against α-glucosidase and α-
amylase respectively. Results indicated that rottlerin potentially bind to the enzymes more as compared to
that of the standard drugs. In vitro evaluation of activity also supported the In silico prediction. The percentage
inhibitions calculated from a dose-response curve showed a rise in inhibition in aldose reductase, α-
glucosidase and α-amylase activity in the range 10 to 30% as compared to standard.
Keywords: Reverse Docking, Aldose reductase, α -glucosidase, α -amylase, Rottlerin

Introduction Molecular docking

Inverse docking, first suggested by Chen et al in Preparation of Ligand and Enzyme
2001, in which specific small molecule of interest is The 3D structure of Rottlerin and standard drugs
computationally docked into a library of receptor were identified from PubChem chemical database.
structures. By this technique may new potential Structures were drawn using Chem3D and energy
biological targets of known compounds or targets minimization using the MM2 force field and saved
for compounds among a family of related in .mol format. From Protein Data Bank the 3D
receptors were identified1. Structure of Aldose Reductase (PDB ID: 1PWM), α-
Rottlerin is a polyphenol natural product isolated Amylase (PDB ID: 4GQQ) and α-Glucosidase (PDB
from the Asian tree Mallotus philippensis. used in ID:5NN8) were retrieved. For docking studies the
the treatment of numerous disease. Rottlerin, also enzymes, phytoconstituent and standard drugs
called mallotoxin is the principal phloroglucinol were prepared by importing to the workspace and
constituent of kamala and can be extracted, assigning the missing bond orders, charges, bonds,
3
purified, and concentrated from the powder.2 and hybridization states in MVD Software .
The purpose of the present research is to explore
the effects of Rottlerin on some identified targets Biological Evaluation
such as α-amylase, α-glucosidase and aldose Aldose reductase (ARE) inhibitory activity
reductase enzymes involved in diabetes and its The lenses were quickly removed from goat
complications. eyeballs which were obtained from local abattoir
soon after slaughtering. Lenses (100 to 200 g)
Material and methods were homogenized in 3 volumes of cold distilled
Natural Compounds and Drugs water in a homogenizer and centrifuged at 10,400
Rottlerin and standard drugs were purchased from RPM at 0-4°C for 15 minutes to remove insoluble
commercial suppliers. The isolates were subjected material. Saturated ammonium sulphate was
to the experimental evaluation against the added to the supernatant fluid to 40%,50% and
enzymes purchased from Himedia. 75’% saturation. The precipitate obtained was
Methods used for the enzymatic assay4.

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A sample cuvette was taken containing mixture of α-amylase (AAE) Inhibition Assay
0.7 mL of phosphate buffer (0.067 M), 0.1 mL of A total of 500 µL Rottlerin of concentration 20, 40,
NADPH (25×10-5 M), 0.1 mL of lens supernatant, 60, 80 and 100µg/mL and 500 µL of 0.02 M sodium
0.1 ml of (Rottlerin at different concentrations) 0.1 phosphate buffer with 0.006 M sodium chloride,
mL of DL-glyceraldehyde (substrate) (5×10-4 M), containing 20 µL of amylase (0.5 mg/mL) were
absorbance of the final solution was taken against incubated (at 25 C for 10 min). Further, 1% starch
a reference blank cuvette containing all the solution (500 µL) in buffer (0.02 M sodium
compounds except the substrate. The enzymatic phosphate, pH 6.9 with 0.006 M sodium chloride)
reaction was started by the addition of the was added to all test tubes, incubated (for 15 min)
substrate and the absorbance was recorded at 340 and reaction was stopped by adding
nm. The reaction was initiated by the addition of dinitrosalicyclic acid (1 mL). After that all test
0.1 mL DL-glyceraldehyde. Ranirestat was used as tubes were incubated (for 5 min) in boiling water
standard drug. The assay was performed in bath, cooled, diluted with distilled water (10 mL)
triplicate. IC50 value and percentage inhibitions and absorbance was measured at 540 nm.
were calculated from a dose-response curve5. Acarbose is used as a positive control.
α-glucosidase (AGE) inhibition assay
A 20 mM phosphate buffer (pH 6.9) was used to Statistical Analysis
prepare the p-nitrophenyl glucopyranoside (pNPG) All the results were expressed as mean ± SEM for
substrate solution. Various concentrations (20- triplicate determinations.
100µg/mL) of Rottlerin (50µL) was preincubated
for10 min. With α-glucosidase (100 µL) and the Results and discussion
reaction started by adding up 3.0 mM pNPG (50 Molecular docking studies of Rottlerin with
µL) solution while stopped by adding 0.1 M aldose reductase, α-glucosidase and α-amylase
Na2CO3 (2mL) solution. The reaction mixtures The results reported in table 1 clearly indicated
were incubated (at 37oC for 20 min) and assessed that Rottlerin fits perfectly at the active site of
for p-nitrophenol release from pNPG at 405 nm. aldose reductase, α-glucosidase and α-amylase
Acarbose is used as a standard drug. The enzyme than their standard drugs.
inhibition rate expressed as a percentage of
inhibition was calculated6.

Table-1 Result of reverse molecular docking studies of Rottlerin and standard drugs with aldose reductase , α-
glucosidase and α-amylase enzymes.
Rottlerin Ranirestat Acarbose

MVD Result ARE AGE AAE ARE AGE AAE

Moldock score -183.531 -159.613 -169.276 -151.57 -125.08 -157.32

Rerank score -80.6892 -141.265 -127.888 -63.72 -122.78 -119.34
H bond -7.66601 -11.39 -11.2122 -8.61 -23.57 -24.28
ARE: Aldose Reductase Enzyme, AGE: Α Gulcosidase Enzyme, AAE: Α-amylase Enzyme.

Antidiabetic effect for enzymes. Ranirestat for aldose reductase (IC50:

In vitro inhibitory effect of Rottlerin on aldose 42.39±.07µg/ml ), Acarbose for α-glucosidase
reductase, α-glucosidase and α-amylase (IC50:44.97±.04µg/ml) and (IC50:47.38±.05µg/ml),
The inhibitory property of Rottlerin (20-100µg/ml) respectively.The result shows that Rottlerin
on aldose reductase, α-glucosidase and α-amylase efficiently inhibited all the three enzymes in vitro
was evaluated (Table 2, Fig. 2). It shows potent and there was a dose-dependent increase in
inhibitory effect against aldose reductase percentage inhibitory activity against the enzymes.
(IC50:33.88±0.04µg/ml),α- From the result, it was observed that Rottlerin
glucosidase(IC50:41.3±0.01µg/ml) and α- shows a high percentage of inhibition than the
amylase(IC50:37.36±0.04µg/ml) respectively. The standard drugs.
standard drugs shows moderate inhibitory activity

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Table 2. Percent inhibitory activity of Rottlerin on aldose reductase , α-glucosidase and α-amylase enzymes.
Concentration in µg/ml Percent Inhibitory Activity
Diosmin Ranirestat Acarbose
ARE AGE AAE ARE AGE AAE
20 40.14±0.05 35.18±0.06 37.47±0.08 33.46±.05 33.51±.06 31.59±.06
40 54.90±0.06 48.99±0.10 51.46±0.05 48.73±.05 47.54±0.11 44.77±.34
60 68.96±0.05 63.65±0.06 65.92±0.05 62.82±.12 62.57±.05 58.29±.10
80 84.83±0.05 77.77±0.06 80.44±0.08 76.60±.08 76.90±.09 73.49±.06
100 97.81±0.14 91.47±0.09 96.59±0.08 89.78±.11 92.2±.1 87.08±.10
IC50 33.88±0.04 41.3±0.01 37.36±0.04 42.39±.07 44.97±.04 47.38±.05
ARE: Aldose Reductase Enzyme, AGE: Α Gulcosidase Enzyme, AAE: Α-amylase Enzyme

Figure 1. IC50 value of Rottlerin and standard drugs on aldose reductase , α-glucosidase and α-amylase
enzymes.

Conclusion Phytoconstituents Identified in Crocus

From the study, it was concluded that Rottlerin sativus, Curcuma longa, Cassia
shows the good docking score and more stable occidentalis and Moringa oleifera on
bonding with α -amylase, aldose reductase and α- Thymidylate Synthase–An Enzyme Target
glucosidase as compared to standard drugs. It was for Anti-Cancer Activity. Journal of
observed by both in silico Reverse docking and in Applied Pharmaceutical Science 2016
vitro analysis that, it can control hyperglycemia by ;6(12):131-5.
inhibiting the carbohydrate metabolizing enzymes 4. Ajani EO, Sabiu S, Odufuwa KT, Ibrahim TB
and the polyol pathway due to which diabetes and Salau BA: Evaluation of Lens Aldose
complications like cataractogenesis occurs. Further Reductase Inhibitory and Free Radical
research can be performed to discover Scavenging Potential of Fractions of
pharmacokinetic properties of these Lonchocarpus cyanescens: Potential for
phytoconstituents and to identify the safety and Cataract Remediation. Pharmacognosy
efficacy parameters at both preclinical and clinical Journal 2017; 9(1).
stages and to prepare the effective formulation by 5. Patel DK, Kumar R, Sairam K and
using this phytoconstituent for the treatment of Hemalatha S: Aldose reductase inhibitory
diabetes and its complications. activity of alcoholic extract of Pedalium
murex Linn fruit. Asian Pacific Journal of
References Tropical Biomedicine 2012; 2(1): S265-9.
1. Grinter SZ, Liang Y, Huang SY, Hyder SM 6. Ahmed S, Al-Rehaily AJ, Alam P, Alqahtani
and Zou X: An inverse docking approach AS, Hidayatullah S, Rehman MT, Mothana
for identifying new potential anti-cancer RA, Abbas SS, Khan MU, Khalid JM and
targets. Journal of Molecular Graphics Siddiqui NA: Antidiabetic, antioxidant,
and Modelling 2011; 29(6): 795-9. molecular docking and HPTLC analysis of
2. Maioli E., Torricelli C., Valacchi G. miquelianin isolated from Euphorbia
Rottlerin and Cancer: Novel Evidence and schimperi C. Presl. Saudi Pharmaceutical
Mechanisms, The Scientific World Journal, Journal 2019; 27(5):655-63.
2012, 2012,1-11.
3. Heble NK, Mavillapalli RC, Selvaraj R and
Jeyabalan S: Molecular Docking Studies of

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DESIGNING AND MOLECULAR MODELING STUDIES ON CHALCONE DERIVATIVES AGAINST

PLASMODIUM FALCIPARUM
Khushbu Jain*, Neetesh Kumar Jain
Faculty of Pharmacy, Oriental University, Gate No.1, Sanwer Road, Jakhya, Opposite Revati
Range, Indore, Madhya Pradesh 453555 India
[email protected]

ABSTRACT
Plasmodium falciparum is unicellular protozoa which causes the Malaria in human being. Malaria is most
deathly and major health issue in worldwide. 31 chalcone derivatives were obtained from the literature. Free
Wilson QSAR studies were performed on the data set which is given in literature. On the basis of QSAR results
the compounds were designed. The designed compounds were investigated in molecular docking to check the
binding affinity on the protein. The result obtained by the present studies can be used to make more potent
antimalarial drugs.
Keywords: chalcone derivatives, QSAR, Docking, Plasmodium falciparum

Introduction derivatives (31 molecules) were taken from

Malaria, a disease caused by protozoan parasites literature. Free-wilson (Fujita ban) QSAR studies
of Plasmodium Genus, especially by most were performed on the given data set with the
[1 2]
prevalent parasite Plasmodium Falciparum. ’ Half help of VALSTAT program and the best QSAR
of the world population is under the risk of being model was choose for the further studies. For the
infected and more than 200 million new clinical docking new compounds were designed on the
cases with around half a million death occurs basis of QSAR results.
[3]
annually. Resistance of malarial parasites to Molecular Docking: In molecular docking the
current pharmacotherapy has emerged as an area ligand protein interactions was studied to predict
of concern in anti malarial drug discovery. Using biological properties of molecules. In this study 20
Plasmodium Falciparum genome sequences, the chalcone derivatives were designed on the basis of
investigation states that the genetic diversity of QSAR result. All the structure of molecules was
eleven gene-targets of promising anti-malarial design with the help of chemdraw ultra 8.0 and
compounds and assessed their potential efficiency energy minimization was done with the help of
[4]
across malaria endemic regions. The emergence chemdraw ultra 3D 8.0. After the designing all the
of P. falciparum strains resistant to almost all structures K1-K20 were subjected to molecular
antimalarials prompted medicinal chemists and docking studies using molegro 6.0. PDB used for
biologists to study their effective replacement with the docking studies was 4j4n.
an alternative mechanism of action and new
[5]
molecules. 31 chalcone derivatives were Result and discussion
obtained from the literature. Chalcone nucleus is QSAR Analysis: Free-Wilson analysis was
present in many natural sources isolated from performed on all analogues K1-K20 and best
plants with potent in vivo and in vitro antimalarial model developed by VALSTAT program was
[6]
activity against Plasmodium falciparum. choose. According to the QSAR results, the
electron donating groups such as o-allyl group are
Materials and methods most active substituent at R1, R2 and R3 positions.
QSAR studies: In QSAR studies the biological This study helped in the designing of more
properties are co-relate with different substituent effective biologically activity compounds.
present in a nucleus. A new series of chalcone

Table 1: QSAR Results

Parameter Value Parameter Value Biological activity = [5.65283(± 0.164212)] +1OCH3 [-
N 30 Std error 0.274 0.761833(± 0.592074)] +2OCH2CHCH2 [-0.3795(± 0.23223)]
+2OCH2CHC(CH3)3 ([0.643667(± 0.592074)] +2Cl [-0.470833(±
R 0.711 F 44.6
2 2 0.434463)] +34OCH2O [-0.626833(± 0.434463)]
r 0.505 Q 0.914
variance 0.075

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OCH3

Fig 1: Chalcone moiety

Table 2: All derivatives with substituents
Comp. R1 R2 R3 Comp. R1 R2 R3
K1 OH OH 3,4-OCH2O K11 NH2 O-Allyl 3-OH
K2 OCH3 OCH3 3,4-OCH2O K12 H H 4-OCH2C(CH3)3
K3 OCH3 Cl 4-OCH2CH3 K13 O-Allyl H 4-OCH2C(CH3)3
K4 OH OCH3 4-OCH3 K14 H Cl 3,4-OCH2O
K5 OH Cl 4-OCH2CH3 K15 OCOCH3 H 3-OCOCH3
K6 NH2 OCH3 4-OH K16 OCH3 OH 4-OCOCH3
K7 NH2 OCH3 4-OCH3 K17 OCH3 OCH3 3-OCH3
K8 O-Allyl NH2 4-O-Allyl K18 O-Allyl NH2 3-NH2
K9 OCOCH3 OH 4-OH K19 CH=CH2 O-Allyl 4-NH2
K10 CH=CH2 OH 4-NH2 K20 OCOCH3 OCH2C(CH3)3 4-OH

Molecular Docking 101 and Asp 56. It was found that the scores
The Protein used, PDB code 4j4n, it was reported obtained were higher than the co-crystallized
contains a co-crystallized ligand name D44 bind to ligand. The most active compound K9 having
active site with H bond interaction with Ile 110, Tyr binding with Tyr 101 and Asp 56 (fig 1.2).

Table3: Docking results

Compound MolDock Score Re rank score H-bond interaction
K9 -104.196 -82.54 -9.207
K20 -107.153 -51.95 -8.442
K19 -106.028 -82.98 -4.085
K18 -105.362 -86.63 -6.817
K2 -101.284 -67.85 -7.179

Fig 2: Interaction of the compound K9 with the protein

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Conclusion 3. Chu-Mei C, Cong W, Wen-ling W, Li-Li L,

5 potential compounds were identified with the Kun-Lai S: Triazole derivatives and their
help of QSAR and molecular docking studies which antiplasmodial and antimalarial activities,
can be used for further in vitro and in vivo studies European journal of Medicinal Chemistry
against the treatment of malaria. 2019; 166:206-223.
4. Gomes AR, Ravenhall M, Benavente ED,
References Campino S: Genetic Diversity of next
1. Tibon SN, Chew HN, Siew LC: Current generation antimalarial targets, A
progress in antimalarial pharmacotherapy baseline for drug resistance surveillance
and multi-target drug discovery, programmes, International Journal for
European Journal of Medicinal Chemistry Parasitology: Drugs and Drug Resistance
2019; 188. 2017; 7: 174-180.
2. Sahu S, Ghosh SK, Gahtori P: In Silico 5. Hu YQ, Gao C, Zhang S, Xu L, Xu Z, Feng
ADMET study, docking synthesis and LS, Wu X, Zhao F: Quinoline hybrids and
antimalarial evaluation of thiazole-1, 3, 5, their antispasmodial and antimalarial
Pf-DHFR inhibitor, Pharmacological Activities, European Journal of Medicinal
Reports 2019; 71:762-767. Chemistry 2017; 139:22-47.

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ANTI-MICROBIAL ACTIVITY OF [4-(6-(2-CHLOROPHENYL)-[1,2,4]TRIAZOLO[3,4-B][1,3,4]

THIADIAZOL-3-YL)PHENOL] TRIAZOLO-THIADIAZOLE DERIVATIVE
Prerna Chaturvedi1*, P.K. Dubey2 and Birendra Shrivastava1
1, Department of Pharmaceutical Sciences, Jaipur National University, Jaipur, (R.J.) - India
2, Swami Vivekanand College of Pharmacy, Indore, (M.P.) – India
[email protected]

ABSTRACT
An antimicrobial agent is any variety of chemical or physical compounds that can destroy or prevent the
growth of microorganisms. Current drug discovery includes the identification of screening hits, medicinal
chemistry and optimization of these hits to increase the affinity, selectivity (to reduce the potential of side
effects), efficacy/potency, metabolic stability (to increase the half-life), and oral bioavailability. In the present
paper antimicrobial activity triazolo-thiadiazole derivative i.e., 4-(6-(2-chlorophenyl)-[1,2,4]triazolo[3,4-
b][1,3,4] thiadiazol-3-yl)phenol was screened for antimicrobial activity against wo representatives of Gram-
positive bacteria viz. S. aureus, B. subtilis, two Gram-negative bacteria viz. E. coli, P. aerugenosa and two fungi
viz. C. albicans, A. niger by the broth microdilution MIC method. Results suggest that the compound possess
optimum activity when compared with standard drug.
Keywords: Anti-microbial, triazolo-thiadiazole derivative, Standard drug

1-6
Introduction drug. Primary inoculation of bacteria was done
4-(6-(2-chlorophenyl)-[1,2,4]triazolo[3,4-b][1,3,4] into Mueller- Hinton agar for overnight growth to
thiadiazol-3-yl)phenol was synthesized which is produce a number of colonies, which were then
triazolo-thiadiazole derivative. Yield: 62%; directly suspended in saline solution until the
o - turbidity matched the turbidity of the McFarland
m.p.:176-178 C; Rf : 0.57; FT-IR υ max (KBr , cm
standard (10 CFU ml), i.e., inoculum size for test
1 strain was adjusted to 108 colony forming unit
): 3389 (NH stretching), 3030 (Ar- CH
stretching), 2903 (aliphatic-CH stretching), 1546 (CFU)/ml per well by comparing the turbidity
(C=C stretching), 1330 (CH bending), 1278 (C=N-N (turbidimetric method). Similar procedure was
stretching), 1250 (C-N stretching), 760 (C-Cl adopted for fungi with Sabouraud dextrose broth.
stretching), 707 (substituted benzene), 677 (C-S Dimethyl sulfoxide (DMSO) was used as diluents to
1 get desired concentration of the compounds and
bending); H NMR δ (CDCl3, ppm): 6.45-7.55 (m, standard drugs. Compound and standard drugs
11H, aromatic), 3.95 (s,1H, NH), 2.75 (s, 2H, - were diluted to obtain 500 μg/ml concentrations,
CH2-). In the present paper anti-microbial activity as a stock solution. Stock solution was further
of 4-(6-(2-chlorophenyl)-[1,2,4]triazolo[3,4- progressively diluted with the test medium and
b][1,3,4] thiadiazol-3-yl)phenol was evaluated required concentrations were obtained for
against bacterial and fungal species. primary and secondary screening. In primary
screening 500, 250 and 125 μg/ml concentrations
Methodology of the compounds was tested. The active
The in vitro antimicrobial activity of all the compounds found in this primary screening were
compounds and standard drugs were assessed further diluted and tested against the
against two representatives of Gram-positive corresponding microorganism. Each test tube was
bacteria viz. S. aureus, B. subtilis, two Gram- then put for incubation at 37° for 24 h for bacteria
negative bacteria viz. E. coli, P. aerugenosa and and 48 h for fungi. Growth or a lack of growth in
two fungi viz. C. albicans, A. niger by the broth the tubes containing the antimicrobial agent was
microdilution MIC method. Mueller Hinton broth determined by comparison with the growth
and Sabouraud dextrose broth were used as a control, indicated by turbidity. The lowest
nutrient medium to grow and dilute the concentration that completely inhibited visible
compound suspension for the test bacteria and growth of the organism was recorded as the MIC
fungi, respectively. Ampicillin, Norfloxacin was (μg/ml).
used as standard antibacterial drugs, whereas
fluconazole was used as standard antifungal

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N N

N S
HO Cl
N

Fig. 1: Structure of 4-(6-(2-chlorophenyl)-[1,2,4]triazolo[3,4-b][1,3,4] thiadiazol-3-yl)phenol

Results and Conclusion was used as standard antifungal drug. The

The in-vitro antimicrobial activity of all the obtained results (Table 1) revealed that all of the
compounds and standard drugs were assessed synthesized compounds exhibit antibacterial
against two representatives of Gram-positive activities against both Gram-positive strains. The
bacteria viz. S. aureus, B. subtilis, two Gram- obtained results for antifungal activities as
negative bacteria viz. E. coli, P. aerugenosa and depicted in Table 1 revealed that compounds
two fungi viz. C. albicans, A. niger by the broth could inhibit the growth of the tested fungal
micro-dilution MIC method. Ampicillin was used as strains.
standard antibacterial drugs, whereas fluconazole

Table 1: Minimum inhibitory concentration (MIC, μg/ml) of synthesized compounds

Compound MIC, μg/ml
S. B. subtilis P. E. A. C.
aureus aeruginosa coli niger albicans
C1 30.2 32.6 28.8 18.0 28.2 32.4
Ampicillin 10.6 10.8 - - - -
Norfloxacin 11.8 14.2 10.4 7.8 - -
Fluconazole - - - - 9.6 10.4

References 4. El-Sayed W. A., Nassar I. F., and Abdel-

1. Colanceska-Ragenovic K., Dimova V., Rahman A. A.- H. C-Furyl glycosides, II:
Kakurinov V., Molnar D. G., and Synthesis and antimicrobial evaluation of
Buzarovska A. Synthesis, antibacterial and C-furyl glycosides bearing pyrazolines,
antifungal activity of 4-substituted5-aryl- isoxazolines, and 5,6-
1,2,4-triazoles. Molecules. 2001; 6, 815 – dihydropyrimidine2(1H)-thiones.
824. Monatsh. Chem. 2009; 140, 365 – 370.
2. Demirbas N., Alpay Karaoglu S., Demirbas 5. Greenwood D. (2000), Antimicrobial
A., and Sancak K. Synthesis and Chemotherapy, 4th ed., Oxford University
antimicrobial activities of some new 1-(5- Press, New York, p. 114.
phenylamino-[1,3,4]thiadiazol-2- 6. Jatav V, Jain SK, Kashaw SK, Mishra.
yl)methyl-5-oxo-[1,2,4]triazole and 1-(4- Synthesis and Antimicrobial activity of
phenyl-5- thioxo-[1,2,4]triazol-3- Novel 2-Methyl-3-(1,3,4- thiadiazolyl)-4-
yl)methyl-5-oxo-[1,2,4]triazole (3H)Quinazolinones. Ind J Pharma Sci
derivatives. Eur. J. Med. Chem. 2004; 39, 2006; May-June: 360-3.
793 – 804. 7. Liu F, Luo XQ, Song BA, Bhadury PS, Yang
3. El-Sayed W. A., Ramiz M. M. M., and S, Jin LH, et al. Synthesis and antifungal
Abdel-Rahman A. A.-H. C-Furyl glycosides, activity of novel sulfoxide derivatives
I: Synthesis and antimicrobial evaluation containing trimethoxyphenyl substituted
of C-furyl glycosides and chalcones 1,3,4- thiadiazole and 1,3,4-oxadiazole
derived therefrom. Monatsh. Chem. moiety. Bioorg Med Chem 2008; 16:
2008; 139, 1499 – 1505. 3632-40.

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MOLECULAR MODELLING STUDIES OF BENZOXAZOLES AS POTENTIAL

ANTI-CONVULSANT AGENTS
Jasdev S. Tuteja
School of Pharmacy, Devi Ahilya Vishwavidyalaya, Indore, M.P.
[email protected]

ABSTRACT
Epilepsy is a neuronal disorder which is characterized by the hyper-synchronous discharge of neurons leading to
abnormal electrical conductivity in brain causing convulsions. Even with the use of currently available anti-epileptic
drugs many patients fail to achieve seizure control, which makes the need for developing newer anticonvulsant
agents. In continuation, benzoxazole derivatives were identified as the potential lead structure and subjected to docking
studies and docking based QSAR studies. The docking and 3D-QSAR studies were performed using SYBYL X 2.1
software. The docking study conducted using PDB ID: 1Y6A revealed the best binding interaction of Compound
No.06 that matched to that of natural ligand having Cys917 with a highest total score of 7.14. Therefore, the QSAR
model and docking model developed in this study may be successfully utilized for the designing of new anticonvulsant
agents.
Keywords: Docking study, QSAR, Anti-Convulsants, Benzoxazoles.

Introduction with the help of drawing tools in the software. The

Epilepsy is a disease of the brain characterized by a sketched 2D structures are transformed into 3D
continued propensity to produce epileptic seizures and structures using module of the program followed by
which causes various deleterious effects on cognitive, energy minimization and saving them into .mol
psychological, and social domains. [2] Docking is a format.
method which tells regarding how the ligand is going CoMFA and CoMSIA were carried out using the
to bind to the active site of the receptors and also QSAR project while Docking study was
about the extent to which conformational changes can carried out as per the docking suite of SYBYL–X 2.1
be brought in the receptor structure when the ligand program [3] using the PDB: 1Y6A. [4]
binds to it. Docking comprises of two tasks. The first
is the prediction of favourable binding cavities for a
small molecule in the binding site of a target protein
and estimation of the binding energy of the complex
formed. The second is also known as scoring in which
according to how the binding is the ligand is given a
score.
Various Steps Carried Out- Splitting and Alignment
Objective
The aim of CoMFA is to derive a correlation between
the biological activity of a set of molecules and their
3D shape, electrostatic and hydrogen bonding
characteristics. COMSIA is basically done to find the
steric indices of the molecules and representing
contour maps.

Materials and methods

For the study data sets of 19 molecules of
benzoxazole derivatives possessing anti-convulsant
activity were taken from the earlier reported work CoMFA
Wei et al. [1] The biological activity data, TOTAL Steric Bulk Desirable– Green; Steric Bulk Undesirable-
SCORE were converted to negative logarithmic Yellow Positive Charge Desirable-Blue; Negative Charge
concentration in moles for QSAR studies. ChemDraw Desirable-Red
Ultra 8.0 was used for the sketching of the molecules

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Docking
CoMSIA
Interaction Matched with PDB (1Y6A): Cys 917
Magenta –acceptor bulk desirable; Red –acceptor bulk
undesirable.

Results and discussion

Table 01: Docking Scores
Molecule Total Score Crash Polar Similarity
06 7.1432 -1.6177 1.1037 0.507
05 5.4897 -2.5337 1.149 0.377
Zonisamide 3.8649 -1.0598 1.0644 0.105

Table 02: Interactions

Ligand Interaction
1Y6A(PDB) Cys917
Compound-06 Cys917

Table 03: QSAR Results

3-D r2 q2 Standard Error Charges Selected
Parameter
CoMFA 0.817 0.405 0.0312 Gasteiger
CoMSIA 0.806 0.395 0.0313 Gasteiger– donor and acceptor

Conclusion References
The compound number 06 i.e. 2-Nonyl-6-(4H-1,2,4- 1. Wei C.X. et al, 2009. Synthesis of 2-
triazol-4-yl)benzo[d]oxazole showed that it had the Substituted-6-(4H-1,2,4-triazol-4-
highest total score of 7.1432 and had Cys 917 as yl)benzo[d]oxazoles as Potential
interaction that matched with that of the PDB-1Y6A Anticonvulsant Agents, Arch Pharm Res, Vol
it can be further used for in-vitro and in-vivo studies. 32, No 1, pp. 23-31.
The best model of QSAR gave above tabulated values 2. Trevor, J.A., Katzung, B.G., Hall, M.K.,Katzung
for correlation coefficient (r2) and cross- validated And Trevors’s Pharmacology-Board and
Examination Review, Mc Graw Hill
correlation coefficient (q2) which can be used further
to design a better compound with enhanced activity. Education,11th ed, pp.201-207.
Blue Colour suggested that the substitution of 3. SYBYL-X 2.1, Tripos International, 1699
withdrawing groups like Chlorine in the compounds at South Hanley Rd., St. Louis, MO, 63144,
that positions will enhance activity whereas Red USA.
suggested the vice versa. 4. Harris, P.A., Cheung, M. et al, 2005.
Discovery and evaluation of 2-anilino-5-
aryloxazoles as a novel class of VEGFR2
kinase inhibitors, Journal of Medicinal
Chemistry, 48(5), pp.1610- 1619.

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MOLECULAR DOCKING AND ADMET STUDIES OF PYRAZOLE ACRYLIC ACID BASED OXAZOLE
AND AMIDE DERIVATIVES AS ANTIMALARIAL AND ANTICANCER AGENTS
Priti Patidar
School of Pharmacy, Devi Ahilya Vishwavidyalaya Indore, Madhya Pradesh-452020
[email protected]

ABSTRACT
The cyclization compounds (oxadiazole) favored antimalarial activity while non-cyclized compounds (amides)
emerged as better anticancer agents. Docking study was carried out on 32 derivatives using molegrow virtual
docker 6.0. ChemDraw 3D was used for structure energy minimization. PDB code: 3BPF or 3D4Q study showed
that the most active compound binds to the active site of the protein. Whereas most active compounds
showed high calculated binding free energy as compared to standard co-crystallized ligand (Antimalarial
agents) Falcipain-2 and (anticancer agents) B-Raf proto-oncogene serine/threonine-protein kinase.
Antimalarial agent targeting falcipain-2 and colon and breast cancer against as anticancer agents.
Keywords: Pyrazole based derivatives, oxadiazole, Amide, malaria and cancer

Introduction option by clinicians for treatment of cancer.

Malaria caused by Plasmodium parasites has Failure in cancer chemotherapy is generally
emerged as a serious issue imposing its fatal observed due to development of the multi-drug
effects on human health. Amongst different resistance, a condition where cancer cells become
potential targets for curbing malaria, cysteine resistant to structurally unrelated
protease falcipain-2 of P. falciparum is one of the chemotherapeutic agents. Another reason is poor
most extensively studied targets. During the life patient compliance which arises due to clinical
cycle of malaria parasite, erythrocytic phase is systemic toxicity, which is generally observed in
accountable for symptoms in humans. During bone marrow and GI tract.
intra-erythrocytic phase, the parasites utilize
different proteases bringing about hydrolysis of Materials and methods
hemoglobin in the acidic food vacuole leading to Molecular docking study
the generation of amino acids required for parasite Preparation of ligand
protein synthesis. Falcipain-2 is one of the key CS Chem Office 8.0 was use for the sketching of
enzymes involved in this digestion. Treatment with molecules with the help of drawing tools of Chem
falcipain-2 inhibitors leads to accumulation of Draw. The sketched 2D structures were
undigested hemoglobin in the swollen food transformed into 3D structures using Chem3D
vacuole, hence resulting in blockage of parasite Ultra 8.0. The 3D structures were then subjected
development. The cyclization compounds like to energy minimization using MM2 (Molecular
(oxadiazole) favored antimalarial activity while Mechanics) and MOPAC (Molecular Orbital
non-cyclized compounds (amides) emerged as Package).
better anticancer agents. It has not spread to
other parts of the body is called localized cancer. It Docking procedure
is known to encompass a broad spectrum of Preparation of protein
diseases in which host cells flee their normal cell Molecular docking study was carried out using
cycle regulation and show the hallmark of Protein (PDB code: 3BPF and 3D4Q) is downloaded
uncontrollable proliferation. This particular from the Protein Data Bank by PDB format then
phenomenon can be linked to a number of factors protein molecule is import in Molegrow Virtual
like gender, ethnicity, age of onset and lifestyle. Docker 6.0, remove all water molecules by the
However, this can also be associated with cellular create surface and identify
transformation linked to viral infection, chemical cavities of the protein. Import mole files for
or radiation exposure or the reason may be docking and then go docking wizard needed to
spontaneous in nature. Combination of surgery import molecules. The active site is predicted and
and radiotherapy is the most opted therapeutic later all ligands is uploaded. Arrange all the

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parameters such as number of poses to be Antimalarial and Anticancer agents. Whereas most
obtained score and start Docking. active compounds showed high calculated binding
The score is calculated and even the display free energy as compared to standard co-
analyzed your data and selects the most optimum crystallized ligand (Antimalarial agents) Falcipain-2
ligand and its pose. To the selection of the ligand and (anticancer agents) B-Raf proto-oncogene
from the docking wizard was done on the basis of serine. The docked pose of the most active
the scoring function (Moldock score and Rerank antimalarial compound 32 with Falcipain-2 PDB ID:
score). 3BPF and dock pose of most active anticancer
compound 28 with colon and breast cancer PDB
ADMET predictor ID: 3D4Q.
ADMET studies were evaluated by using ADMET The docking results showed that compound E64
Predictor 2.0, software structures were selected in was found to give best Moldock score with (3BPF)
which various pharmacokinetic parameters like PDB and the compound SM5 was found to give
LogP and LogD values, Plasma protein binding best Moldock score with (3D4Q) PDB.
(PPB), Pgp-inhibition Inhibitor, Pure-water- The common amino acid residue between the co-
solubility, Skin-Permeability, crystallized ligand and compound 32 with enzyme
Buffer solubility mg L, BBB etc. 3bpf is His 174 and Moldock score -196.525 and
common amino acid residue between the co-
Result and Discussion crystallized ligand and compound 28 with enzyme
Docking results 3d4q is Cys532, Glu501 and Moldock.
Molecular Docking: - In this study, compounds
shows that a good protein binding against their

i ii
Figure1: Docking image 3BPF (i) and 3D4Q: PDB (ii) showed hydrogen bond interactions

ADMET drugs in the clinical phases. In ADMET

The prediction of the ADMET properties plays an properties of the five most active compounds
important role in the drug design process because
these properties for the failure of about 60% of all

Compound BBB Buffer Plasma Protein Pure water solubility Skin

solubility mg L Binding mg L Permeability
1 3.21995 18.2408 100.000000 0.000486401 -2.68756
2 2.61975 9.70941 97.703396 0.00103263 -2.45172
3 0.0335315 3.35843 94.935902 0.00382504 -2.38328
4 1.28015 4.47033 100.000000 0.00243944 -2.17777
5 2.88914 5.3232 100.000000 0.000772365 -2.30586

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Conclusion 2. https://preadmet.bmdrc.kr/
In conclusion, a series of pyrazole based 3. Verma, G., Chashoo, G., Ali, A., Khan,
derivatives were taken for molecular docking M.F., Akhtar, W., Ali, I., Akhtar, M., Alam,
study. Molecular docking with the protein PDB M.M. and Shaquiquzzaman, M., 2018.
code: 3BPF and 3D4Q, shown Moldock score of Synthesis of pyrazole acrylic acid based
compounds as compared to co-crystallized ligand. oxadiazole and amide derivatives as
antimalarial and anticancer
Reference agents. Bioorganic chemistry, 77, pp.106-
1. https://www.rcsb.org/structure/3bpf. 124.

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EMPLOYMENT OF HYDROTROPIC AND MIXED HYDROTROPIC SOLUTIONS AS MOBILE

PHASE TO CARRY OUT TLC PRECLUDING THE USE OF ORGANIC SOLVENTS
R.K. Maheshwari, Anuj Jain, Ayushi Mohadikar*, Pawan Jat, Isha Kalaria, Harshal Wadhwani
Shri G.S. Institute of Technology and Science, 23, Park Road, Indore - 452003 (M.P.), India
[email protected]

ABSTRACT
A large number of organic solvents, viz. butanol, acetic acid, hexane, acetone, chloroform, ether, ethyl acetate,
ethanol, toluene, dichloromethane, xylene, heptane, and cyclohexane are employed to perform thin-layer
chromatography (TLC) of various drugs. Most of these organic solvents are costly and hazardous to health.
Some have been reported to be carcinogenic. To a certain extent, such solvents are responsible for
environmental pollution also. Also, their disposal requires stringent procedures which makes the process both
costly and typical. In the present investigation, hydrotropic and mixed hydrotropic solutions were employed as
mobile phase to perform TLC of poorly water-soluble drugs precluding the use of organic solvents. Norfloxacin,
diazepam, metronidazole, naproxen & nimesulide were selected as model poorly water-soluble drugs; and
sodium benzoate, urea, sodium citrate, sodium acetate, & niacinamide in various combinations as model
hydrotropic agents. In the case of the proposed methods, solutions of the above listed hydrotropic agents in
distilled water were employed as mobile phases to perform TLC of the selected drugs. The observed R f values
in the case of proposed methods ranged from 0.35 to 0.89. The proposed TLC methods are new, simple, cost-
effective, environment-friendly, and safe. In future, hydrotropic solutions shall prove a boon in TLC and high
performance thin layer chromatography (HPTLC) analysis of a vast number of drugs discouraging the use of
organic solvents to a great extent.
Keywords: TLC, Hydrotropic agents, Organic solvents

Introduction volumes of chloroform, 10 volumes of

Increasing the aqueous solubility of insoluble and diethylamine, 10 volumes of ethanol, and 1
slightly soluble drugs is of major importance. volume of water.
24
Hydrotropy refers to the ability of a concentrated In the case of TLC studies of naproxen , the
solution of a chemical compound to increase the mobile phase used as per the British
aqueous solubility of another compound (usually a Pharmacopoeia (BP) 2002 involves a mixture of 3
poorly water-soluble compound). Compounds that volumes of glacial acetic acid, 9 volumes of
have this property are called ‘hydrotropes.’ A large tetrahydrofuran, and 90 volumes of toluene.
1
number of hydrotropic and mixed hydrotropic Hydrotropic solubilization technique has nicely
agents have been reported to enhance the been employed in RP-HPLC analysis of cefixime
aqueous solubilities of a vast variety of poorly tablets using 6% w/v sodium acetate solution in
1-24
water-soluble drugs thus eliminating the use of water (after adjusting pH to 6.2 using acetic acid)
organic solvents. precluding the use of organic solvents. Hydrotropic
21
In case of TLC studies of norfloxacin , mobile and mixed hydrotropic solutions have been
phase used as per the Indian Pharmacopoeia (IP) employed for UV-spectrophotometric analysis and
2007 involves a mixture of 40 volumes of titrimetric analysis of a large number of poorly
dichloromethane, 40 volumes of methanol, 20 water-soluble drugs precluding the use of organic
2-8
volumes of toluene, 14 volumes of diethylamine, solvents .Hydrotropic solutions have been
and 8 volumes of water. employed for TLC studies making the use of
22 9-11
In the case of TLC studies of diazepam , the organic solvents .
mobile phase used as per the Indian
Pharmacopoeia (IP) 2007 involves a mixture of Materials
equal volumes of hexane and ethyl acetate. The bulk drug samples of norfloxacin,
23
In the case of TLC studies of metronidazole , metronidazole, and naproxen were generously
mobile phase used as per the Indian provided by M/S Alkem Laboratories Ltd.,
Pharmacopoeia (IP) 2007 involves a mixture of 80 Mumbai.Diazepam was a gift sample from Sun

International Journal of Pharmaceutical Sciences and Research: Conference Proceedings: Special ssue; March, 2020 Page | 163
International Journal of
Pharmaceutical Sciences and Research
ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

Pharmaceutical Industries Ltd., Dewas.Nimesulide coated plates were air-dried at 100-105°C for
waskindly supplied by Schon Pharmaceuticals Ltd., about one hour.
Indore.All chemicals and solvents used were of Thin layer chromatography of the drugs were
analytical grade. carried out on TLC glass plates, precoated with
silica gel G using different hydrotropic and mixed
Method hydrotropicsolutions. The spots of drugs were
Preparation of plates visualized by treating them with iodine vapours.
Suspension of silica gel G was prepared and it was The retention factor values of spots were
uniformly spread keeping thickness between 0.25 calculated by using the following formula:
to 0.30 mm on the glass slides7 cm long. The

Figure 1: Chamber development for TLC

Rf = distance travelled by solute front/distance travelled by the solvent front

Figure 2: Measurement of Rf after TLC plate development

TLC Studies  In the case of TLC studies of diazepam,

 In the case of TLC studies of norfloxacin, the proposed method employed the use
the proposed method employed the use of hydrotropic solution of30% sodium
of mixed hydrotropic blend containing benzoate,and mixed hydrotropic
15% sodium benzoate and 15% sodium blendcontaining 15% sodium benzoate
citrate (Blend A), 15% sodium benzoate and 15% sodium citrate (Blend A) as
and 15% urea (Blend B), and 7.5% sodium mobile phases. The detection of the spot
benzoate and 7.5% urea (Blend C), as was done using iodine chamber. The Rf
mobile phases. The detection of the spot values obtained by both the methods are
was done using iodine chamber. The presented in Table 1.
Rfvalues obtained by all three methods  In the case of TLC studies of
are presented in Table 1. metronidazole, the proposed method

International Journal of Pharmaceutical Sciences and Research: Conference Proceedings: Special ssue; March, 2020 Page | 164
International Journal of
Pharmaceutical Sciences and Research
ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

employed the use of hydrotropic solution detection of the spot was done using
of 30% sodium benzoate, and mixed iodine chamber. The Rf value obtained by
hydrotropic blend containing 15% sodium the method is presented in Table 1.
benzoate and 15% sodium citrate (Blend  In the case of TLC studies of nimesulide,
A), and 15% sodium benzoate and 15% the proposed method employed the use
sodium acetate (Blend D), as mobile of mixed hydrotropic blendcontaining
phases. The detection of the spot was 15% sodium benzoate and 15% sodium
done using iodine chamber. The Rf values citrate (Blend A), 15% sodium benzoate
obtained by all the three methods are and 15% sodium acetate (Blend D), and
presented in Table 1. 15% niacinamide and 15% sodium
 In the case of TLC studies of naproxen, benzoate (Blend E), as mobile phases. The
the proposed method employed the use detection of the spot was done using
of mixed hydrotropic blend containing iodine chamber. The Rf values obtained by
15% sodium benzoate and 15% sodium all three methods are presented in Table
acetate (Blend D), as mobile phase. The 1.

Table 1: Results of Thin Layer Chromatography Studies

Drug Solvent System Rf Value
Norfloxacin Mixed hydrotropic blend containing 15% sodium benzoate and 15% sodium 0.50
citrate
(Blend A)
Norfloxacin Mixed hydrotropic blend containing 15% sodium benzoate and 15% urea 0.64
(Blend B)
Norfloxacin Mixed hydrotropic blend containing 7.5% sodium benzoate and 7.5% urea 0.35
(Blend C)
Diazepam Hydrotropic solution of 30% sodium benzoate 0.63
Diazepam Mixed hydrotropic blend containing 15% sodium benzoate and 15% sodium 0.68
citrate
(Blend A)
Metronidazole Hydrotropic solution of 30% sodium benzoate 0.78
Metronidazole Mixed hydrotropic blend containing 15% sodium benzoate and 15% sodium 0.77
citrate
(Blend A)
Metronidazole Mixed hydrotropic blend containing 15% sodium benzoate and 15% sodium 0.85
acetate (Blend D)
Naproxen Mixed hydrotropic blend containing 15% sodium benzoate and 15% sodium 0.42
acetate (Blend D)
Nimesulide Mixed hydrotropic blend containing 15% sodium benzoate and 15% sodium 0.82
citrate
(Blend A)
Nimesulide Mixed hydrotropic blend containing 15% sodium benzoate and 15% sodium 0.75
acetate (Blend D)
Nimesulide Mixed hydrotropic blend containing 15% niacinamide and 15% sodium 0.89
benzoate
(Blend E)

Results and discussion urea (Blend B), and 7.5% sodium benzoate and
As evident from Table 1, the obtained Rf values for 7.5% urea (Blend C), were 0.5, 0.64 and 0.35,
norfloxacin using mixed hydrotropic blend respectively.
containing 15% sodium benzoateand 15% sodium The obtained Rf values for diazepam, using
citrate (Blend A), 15% sodium benzoate and 15% hydrotropic solution of 30% sodium benzoate, and

International Journal of Pharmaceutical Sciences and Research: Conference Proceedings: Special ssue; March, 2020 Page | 165
International Journal of
Pharmaceutical Sciences and Research
ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

mixed hydrotropic blend containing 15% sodium solutions do not require such stringent
benzoate and 15% sodium citrate (Blend A), were procedures.
0.63 and 0.68, respectively. It may, thus, be concluded that the proposed
The obtained Rf values for metronidazole, using method of analysis was new, simple, cost-
hydrotropic solution of 30% sodium benzoate, effective, environment-friendly and safe. The
andmixed hydrotropic blend containing 15% decided advantage was that the organic solvents
sodium benzoate and 15% sodium citrate (Blend were precluded. The proposed method can be
A), and 15% sodium benzoate and 15% sodium successfully employed in the TLC of other drugs, as
acetate (Blend D), were 0.78, 0.77 and 0.85, well. It is expected that the hydrotropic solution
respectively. systems can be employed in HPTLC analysis in
The obtained Rf values for naproxen, using mixed future and can be developed as a novel tool to
hydrotropic blend containing 15% sodium eliminate the use of expensive, pollutant, and toxic
benzoate and 15% sodium acetate (Blend D) was organic solvents.
found to be 0.42.
The obtained Rf values for nimesulide, using mixed References
hydrotropic blend containing 15% sodium 1. Remi, S.L.; Varkey J.; Maheshwari, R.K.
benzoate and 15% sodium citrate (Blend A), 15% Novel RP-HPLC method development and
sodium benzoate and 15% sodium acetate (Blend validation of cefixime in bulk and its
D), and 15% niacinamide and 15% sodium dosage form by using hydrotropic solution
benzoate (Blend E), were 0.82, 0.75 and 0.89, as mobile phase. Asian Journal of
respectively. Pharmaceutical Sciences, 2018; 2, 1907-
It is, thus, well-observed that the Rf values 1914.
obtained employing the proposed methods using 2. Maheshwari, R.K.; Mohadikar, A.; Mulani,
the hydrotropic solutions as mobile phases were P.; Mitali Jain. Spectrophotometric
nearly satisfactory. The proposed methods were analysis of tablets of piroxicam using
mostly devoid of the tailing effect. The hydrotropic melted niacinamide as solvent. Global
resolution also showed an advantage of the Journal for Research Analysis,2019; Vol 8,
absence of tailing effect. Time effectiveness was Issue 12, Print ISSN No. 2277 – 8160.
also observed. 3. Sharma, R.; Pathodiya, G.; Mishra, G. P.
Qualitative and quantitative estimation of
Conclusion water insoluble drugs from its
TLC and HPTLC studies are largely conducted in formulations simultaneously: A
various colleges (institutions), analytical hydrotropic approach. Academic Journals
laboratories, forensic science laboratories, Database,2010; 3, 37-40.
chemistry laboratories, pharmacy laboratories, 4. Maheshwari R.K.; Wanare G.; Chahar N.;
chemical industries, pharmaceutical industries, Joshi P.; Nayak N. Quantitative estimation
government analytical laboratories etc. All of naproxen in tablets using ibuprofen
TLC/HPTLC studies involve the use of organic sodium as hydrotropic agent. Indian J.
solvents like butanol, hexane, tetrahydrofuran, Pharm. Sci, 2009;(71): 335.
diethylamine, toluene, dichloromethane, ethyl 5. Maheshwari, R.K.; Rajput M.S.; Sharma, S.
acetate, xylene, chloroform, and heptane. Most of Simple titrimetric method to estimate
these organic solvents are costly and their ketoprofen in bulk using mixed
exposure to the human being is harmful. Some of hydrotropy. Journal of Pharmacy
them are carcinogenic as well. In the present Research, 2010; 3, 442-43
investigation, the use of organic solvents has nicely 6. Maliwal, D.; Maheshwari, R. K.; Jain, A.;
been replaced with economic and harmless Patidar, V. Simultaneous
hydrotropic agents. This concept is very new and spectrophotometric estimation of
has great potential for all above-mentioned metronidazole and norfloxacin in
organizations. combined tablet formulations using
Also, the disposal of used organic solvents is hydrotropy. Research Journal of
typical and costly but the disposal of hydrotropic

International Journal of Pharmaceutical Sciences and Research: Conference Proceedings: Special ssue; March, 2020 Page | 166
International Journal of
Pharmaceutical Sciences and Research
ISSN (Online): 0975-8232 I ISSN (Print): 2320-5148

Pharmacy and Technology, 2008; 1, 357- Pharmaceutical Technology

361. & Research, 2013; 3, 36-38.
7. Maheshwari, R.K.; Chaturvedi, S. C.; Jain, 15. Kumar S.T.; Gandhi N.N. A study on the
N.K. Novel application of hydrotropic properties of hydrotrope solutions for the
solubilization in the quantitative analysis enhancement of solubility of p-
of some NSAIDs and their solid dosage aminobenzoic acid through hydrotropy.
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Sciences, 2007; 69, 101-105. Sciences and Research,2012; 4 (4): 324-
8. Maheshwari, R. K.; Lakkadwala, S.; Vyas, 330.
R.; Ghode, P. Spectrophotometric 16. Kumar S.T.; Gandhi N.N. Association
determination of naproxen tablets using model of hydrotropy for the effect of
niacinamide as hydrotropic solubilizing hydrotropes on solubility and mass
additive. Journal of Current transfer coefficient of acetylsalicylic acid.
Pharmaceutical Research, 2010; 5, 99- International Journal of Pharmaceutical
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9. Jayronia Sonali, Yadav Kamaldeep, 605.
Sharma Bhumika, Jain Sanjay, 17. Maheshwari R.K; Jagwani Y. Hydrotropy: a
Maheshwari R.K. Hydrotropy: A novel promising tool for solubility
approach in estimation of poorly aqueous enhancement. Indian J. Pharm. Sci.,2011;
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Journal of Pharmacy and Pharmaceutical 18. Darwish, A.; Florence, A.T.; Saleh, A.M.
Sciences, 2013; Vol 5, Issue 2, 176-178. Effects of hydrotropic agents on the
10. R.K.Maheshwari, Garvita Joshi, SC solubility, precipitation, and protein
Mahajan. Novel application of hydrotropy binding of etoposide, J. Pharm. Sci.,1989;
in thin layer chromatography, Indian (78): 577.
Pharmacist, 2010; IX, 57-59. 19. Rasool A.A.; Hussain A.A.; Dittert L.W.
11. Mangal, A.; Bhadoryia, S. S.; Verma, A.; Solubility enhancement of some water-
Mishra K. K. Novel application of insoluble drugs in the presence of
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Messiry, H. M. Enhancement of solubility Release,2005; (101): 59- 68.
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International Journal of Pharmaceutical Sciences and Research: Conference Proceedings: Special ssue; March, 2020 Page | 167

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