HERBAL FORMULATIONS

Dr. Manisha
Assistant professor
Department of Pharmacognosy

K.K.WaghCollege
Krupanidhi College of
of Pharmacy,
 Learning Objective

🠶 After completion of this learner will be able to-

1. Know preparation herbal formulations in detail.
2. Understand evaluation parameters of herbal Syrup,
mixtures and tablet
powder
3. Introduce NDDS for hernals

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 Content
🠶 Definition of herbal formulation
🠶 Challenges in herbal formulation
🠶 Steps in herbal drug formulations
🠶 Conventional herbal formulations:
🠶Syrups
🠶Mixtures
🠶Tablets
🠶Novel dosage forms:
🠶Liposomes
🠶Phytosomes
🠶Nanoparticals
🠶Microsphere

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 Herbal formulations

🠶 According to WHO, herbal dosage forms are physical form like liquid, solid,
semi-solid products produced from herb, with or without excipients, in a
particular formulation.
🠶 The herbal materials such as dried roots or fresh juices or herbal preparations
such as extracts are used to produce herbal dosage forms.
🠶 Herbal formulations means a dosage form consisting of one or more herbs or
processed herbs in specified quantities to provide specific nutritional, cosmetic
benefits meant for use to diagnose, treat, mitigate diseases of human beings or
animals, alter the structure or physiology of human beings or animals.

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 Challenges in herbal formulation:

🠶The toxicological, epidemiological, and other data available regarding

herbal
formulations is confusing.
🠶Authentication of herbal materials is difficult.
🠶Pharmacological, toxicological and clinical documentation is tedious task.
🠶It is difficult to follow pharmacovigilance guidelines in case of herbal formulations.
🠶Standardization, safety and efficacy measurement of herbal formulations are a big
challenge.
🠶There are various hurdles in conduction of clinical trial of herbal formulations.

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 Steps in herbal drug formulations

🠶Selection, drying and grinding of herbal drugs.

🠶Extraction of plant material.
🠶Filtration and concentration of extract.
🠶Powdered extract.
🠶Preparation of dosage forms.

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🠶Conventional herbal formulations
🠶Syrups
🠶Mixtures
🠶Tablets
🠶Novel dosage forms
🠶Liposomes
🠶Phytosomes
🠶Nanoparticals
🠶Microsphere

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 Syrup

🠶 Syrup are viscous liquids containing high amount of sugars or other sweetening
agents.
🠶 They are prepared by various methods such as dissolving, mixing, suspending or
emulsifying herbal extracts or decoctions in a solution of honey, sucrose or
other sweetening agents.
🠶 Syrups can also be prepared by using infusions.
🠶 Syrups may or may not contain medicines or flavouring agent.
🠶 Non-medicated syrups are containing flavouring agents.
🠶 Medicated syrups are containing medication.

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 Syrup
Advantages
🠶Unpleasant taste of medications can be masked.
🠶It is easy to swallow medication in syrup form.
🠶It is easy to administer drug in paediatric patients as they are sweet in taste
and easy to swallow.
🠶It have a soothing effect on irritated tissues.
🠶Tasty and easier for children and picky family members to take
🠶Long shelf life
🠶Can be made with almost any herb
🠶Helpful for a variety of health issues
🠶Raw honey is nutritious and soothing for the throat
Depending on which herbs you use, you can have an herbal syrup on hand to boost
immunity, ease a cough, calm digestion, soothe a sore throat, and much more.
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 Preparation of Herbal Syrup
1. Preparation of decoction of plant material:
🠶Weighed quantity of plant material is extracted
with sufficient quantity of boiling water.
🠶The boiling is continued till the volume of solution reduces to one fourth of
its orginal volume.
🠶Then the liquid is cooled and filtered.
2.To prepare simple syrup
🠶66.67 gm of sucroseis dissolved in sufficient
water to get 100mL of concentrated simple syrup.
OR
🠶Other Sweetening agent used in place of simple syrup like honey, Sachharin
solution

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3. Preparation of Syrup
Finally plant decoction is mixed with simple syrup in 1:4 ratio respectively
to get 100 mL of herbal syrup. Or proportion as given in formulae
Preservatives, colourants and flavouring agents may be added.

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 Evaluation of herbal syrup
1. Description: Colour, Odour, Taste,
Apperance
2. Physical Parameter
Specific gravity/
Weight/ml Refractive
index
Viscosity
Optical rotation
3. Physiochemical parameter
pH value
Total Solid Content

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4. Chemical Parameter
a) Total acidity by Acid value
b) Non reducing sugars
c) Test for methanol
d) Reducing sugars
e) GLC/TLC/HPTLC/HPLC/GC-MS (any one of all)
f) Test for heavy/toxic metals like Lead, Cadmium, Mercury, Arsenic (Limits as per
ASU Pharmacopoeia)
g) Pesticide residue: Organo chlorine pesticides, organophosphorus pesticides,
pyrethroids
(Limits as per ASU Pharmacopoeia)
5. Biological Evaluation:
a) Efficacy and Toxicty Study
b) Microbial contamination Total viable aerobic count Enterobacteriaceae Total fungal
count
(Limits as per ASU Pharmacopoeia
c) est for specific pathogen Escherichia coli, Salmonella spp., Staphyloccocus aureus,
Pseudomonas aeruginosa (Limits as per ASU Pharmacopoeia)
d) Aflatoxins ( Bi,B2,Gi G2 ) (Limits as per ASU Pharmacopoeia)
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🠶 Stability testing:
🠶 In this syrup is stored at room temperature and accelerated temperature
conditions.
🠶 Then at the interval of 24hrs, 48hrs, 72hrs syrup is evaluated for
physicochemical parameters, turbidity, thermal stability, degradation and
homogenesity.

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 Example

🠶 Raspberry Syrup:
🠶It is prepared from fresh juice of ripened raspberries and
possesses a very pleasant taste that is enjoyed by children.
🠶It is particularly useful for masking the taste of bromides, citrates
and other saline drugs, as well as for antipyrine and substances
having an acid taste.

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 Tablet
s
🠶 Tablets are solid dosage forms made up of the herbal extract powder, plant
powder or granules is blended with excipients such as binders, glidants,
disintegrating agents, diluents, etc. and are compressed to form defined
shape and size.
🠶 Tablets are coated or uncoated.

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 Preparation of Tablets
🠶 Tablets can be prepared by following methods:
🠶Direct compression method
🠶Wet granulation method
🠶Granulation by preliminary compression
🠶Coating of tablets

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1) Direct compression method:
🠶 In this method, herbal ingredients are accurately weighed and mixed with
appropriate excipients.
🠶 Then by using tablet compression machine mixture
(Herbals and Exceipents) are directly compressed to form
tablet.
2) Wet granulation method
🠶 In this method, accurately weighed herbal
extracts are triturated with excipients and binder solution.
🠶 The wet mass thus obtained is passed through sieve to obtain granules.
🠶 Then the granules are dried, sieved and mixed with lubricants.
🠶 These granules are punched by tablet compression machine into desired
size and shape.
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3) Granulation by preliminary compression
🠶 This method is used for moisture sensitive drugs.
🠶 First dry extract powder is compressed to form large slugs or tablets.
🠶 Then these slugs are break into small pieces and sieved through
specific sieve to obtain granules.
🠶 These granules are mixed with lubricating and disintegrating agents
and
compressed to form tablets.
4) Coating of tablets:
🠶 Coating is done to mask undesirable colour, odour and taste, to
protect
from moisture or to make sustained release product.
🠶 It is carried out using pan coating or press coating method.
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 Evaluation of Tablets
🠶 General Appearance-Colour, Odour
🠶 Loss on drying at 105OC/ Moisture content
🠶 Alcohol- soluble extractive
🠶 Water -soluble extractive
🠶 Size & shape
🠶 Unique identification marking
🠶 Hardness
🠶 Friability
🠶 Weight variation test
🠶 Content uniformity test
🠶 Disintegration test
🠶 Dissolution test
🠶 Stability testing

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2 Mixture/ Churna
1
🠶 They are solid dosage forms.
🠶 They are based on number & nature of drug and size
of particles.
Based on number & nature of drug:
1) Simple churna
2) Compound churna
3) Churna with metallic powders
Based on size of particles:
4) Sthoola churna
5) Sookshma churna
6) Atyanta sookshma chruna
24-Jun-23

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2 Preparation
2
🠶 Drugs are cleaned and dried properly.
🠶 They are finely powdered & sieved (80 mesh )
🠶 If more than one drug is their than they are separately
powdered and sieved and than they are mixed.
🠶 Powder should not adhere together or become moist.
🠶 Finer powder has better therapeutic value.
🠶 It should be preserved/stored in air tight containers.

 Marketed preparations:
 Triphala churna
 Sudharshan churna
24-Jun-23

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2
3
Preservation

🠶 It should be stored in the air tight containers.

 Precautions :
🠶 Cleaned and dried drugs should be used for
preparation of churans.
🠶 They should be finely sifted.
🠶 Each substance should be powdered separately and then mixed.
🠶 Mortar & pestle should be clean & dry.
🠶 Must be stored in a dry container.
🠶 Should not be prepared in rainy season.

24-Jun-23

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 Mixture

Churna is defined as a fine powder of drug or drugs in Ayurvedic system of

medicine. Drugs mentioned in patha, are cleaned properly, dried thoroughly pulverized and
then sieved. Churna is solid ayurvedic preparation of powder of drugs with often taken with
some anupan like milk, ghee, honey. fine the powder the better its therapeutic effect
These are two types:
1. Simple churana:
It contains only one medicament.

2. Compound churana:
It contains two or more than two medicaments.

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Preparation of
Mixture
Drug mentioned in yoga are cleaned and dried properly They are finely
powdered and sieved. If more than one drug are present then each one is
separately powdered, sieved, accurately weighed and then all mixed together.
The powder is fine to the extent of at least 80 mesh sieves. It should not
adhere together or become moist. The finer powder has better therapeutic value.

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Evaluation of Mixture
1. Description: Colour, Odour, Taste
2. Physical
Parameter Foreign
matters Powder
microscopy
Particle size (80-
100 mesh for
Cuma)
Bulk density and
Tap density,
Hausner ratio
Angle of repose
3. Physiochemical parameter
• pH (1% aqueous extract)
• Loss on drying at 105
C /Moisture content
• Total ash
K.K.Wagh
• Acid -insolubleCollege
KrupanidhiashCollege ofofPharmacy,
Pharmacy, Nashik
4. Chemical Parameter
a) Assay for major ingredients/Major constituents of main
ingredients
b) TLC/HPTLC/HPLC/LC-MS (with marker)
c) Test for heavy/toxic metals Lead, Cadmium, Mercury, Arsenic
(Limits as per ASU Pharmacopoeia)
d) Pesticide residue Organo chlorine pesticides, organophosphorus
pesticides, pyrethroids (Limits as per ASU Pharmacopoeia)
5. Biological Evaluation:
a)Microbial
contamination Total viable
aerobic count,
Enterobacteriaceae,
Total fungal count (Limits
as per ASU
Pharmacopoeia)
b) Test for specific
Pathogen Escherichia
coli, Salmonella spp.,
K.K.Wagh
Krupanidhi
Staphyloccocus College
aureus,College ofofPharmacy,
Pharmacy, Nashik
 Novel dosage forms
🠶 Novel Drug Delivery System means the approaches, formulations, technologies
and systems to transport of Pharmaceutical compound in the body so that it can
safely achieve its desired therapeutic activity.
🠶 Novel Drug Delivery System is nothing but the combination of advanced
techniques new dosage forms in which drug is delivered by the system other
than conventional Drug Delivery System.
Drawbacks of conventional dosage forms
🠶 Poor patient compliance, increased chances of missing the dose of drug.
🠶 The unavailable fluctuation of drug concentration may lead to under medication
or over medication.
🠶 A typical peak valley plasma concentration time profile id obtained which make
attainment of steady state condition difficult.
🠶 The fluctuation in drug levels may lead to
precipitation of adverse effects especially of a
drug with small therapeutic index whenever over
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medication
Advantages of using Novel drug delivery system herbal drugs
🠶 Enhancement of solubility
🠶 Enhancement of Bioavailability,
🠶 Protection from toxicity,
🠶 Enhancement of pharmacological activity,
🠶 Enhancement of stability,
🠶 Improving tissue macrophages distribution,
🠶 Sustained delivery,
🠶 Protection from physical and chemical degradation etc.

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Types of novel drug delivery system
 Liposome
 Nanoparticles
 Phytosome
 Emulsion (Nanoemulsion and Microemulsion)

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 Liposomes
🠶 Liposomes are biodegradable,colloidal and spherical vesicles (0.05-5.0 µm in
diameter) composed of a bilayer membrane entrapping an aqueous core.
🠶 Aqueous core enclosed in one or more phospholipids layer enclosing an
aqueous core and used to convey vaccine, drug, enzyme or other subs to
target cell or organ
🠶 Liposome consists of polar liquid and have hydrophilic and lipophilic Groups.

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Liposome
s

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Preparation:
All the methods of preparing the liposomes involve four basic stages:
🠶 1. Drying down lipids from organic solvent.
🠶 2. Dispersing the lipid in aqueous media. Drug loading is carried out by active and
passive loading techniques.
🠶 3. Purifying the resultant liposome.
🠶 4. Analyzing the final product.
Advantages
🠶 They are highly biocompatible.
🠶 They are biodegradable, biologically inactive, non immunogenic in nature.
🠶 Easy to prepare.
🠶 Acts as carrier for hydrophilic, amphiphilic and lipophilic compounds.
🠶 It can be used to produce control release and sustained release formulation.

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Formulations Active Applications of liposome Biological activity Method of % Route of
ingredients formulations preparation Entrapment administr
efficiency ation
Quercetin Quercetin Reduced dose, enhance Antioxidant Reverse 60% Intranasal
penetration in blood brain Anticancer evaporation
liposomes barrier technique
Liposomes Silymarin Improve bioavailability Hepatoprotective Reverse 69.22 ± Buccal
encapsulated evaporation 0.6%
silymarin technique
Liposoma Artemisia Targeting of essential oils to Antiviral Film method 60–74% In vitro
artemisia arborescens cells, enhance penetration and
arborescens essential into, cytoplasmatic barrier sonication
oil

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 Phytosomes
🠶 The term phyto means plant and some means cell like. Phytosomes
are novel dosage forms of standardized plant extract of water
soluble phytoconstituents which are entrapped into phospholipids to
produce lipid compatible molecular complexs.
Preparation:
🠶 Phospholipids are dissolved in organic solvent. Then extract of
phytoconstituents in above solution in ratio1:1.
🠶 The isolation of phytosomal complex can be carried out by
precipitation with solvents containing aliphatic hydrocarbons or
bi lyophilization or by spray drying.
🠶 Phospholipid like phosphatidylcholine isolated from soyabin is
commonly used in preparation of phytosomes.
🠶 Phytoconstituents attach phospholipid by forming a chemical
bond.

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🠶 Advantages:
🠶 Phytosomes can give protection against distruction of herb by digestive
secretions and gut bacteria.
🠶 Proper drug delivery at site of action.
🠶 Nutrient safety of herbal drug is retained.
🠶 Reduction in dose, enhanced absorption and bioaviability of active principle.
🠶 Entrapment Efficiency is high and predetermined.
🠶 Has greater clinical benefit.
🠶 Superior to liposomes in skin care products.
🠶 Better stability due to formation of chemical bonds.

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Formulations Active Applications of phytosomal Biological activity Method of Dose
ingredients formulations preparation
Ginkgo biloba Flavonoids Flavonoids of GBP Cardio-protective, Phospholipids 100 mg and
phytosomes stabilize the ROS antioxidant 200 mg/ kg
activity complexation
Ginkgoselect Flavonoids Inhibits lipid peroxidation Hepatoprotective, Phospholipids 25 and
phytosome (LPO), stabilize the ROS antioxidant 50 mg/ kg
complexation
Silybin Flavonoids Absorption of silybin Hepatoprotective, Silybin- phospholipid 120 mg
phytosome phytosome from silybin is antioxidant for complexation
approximately 7 times liver and skin
greater
Ginseng Ginsenosides Increase absorption Nutraceutical, Phospholipids 150 mg
phytosome mmunomodulator
complexation
Green tea Epigallocatechin Increase absorption Nutraceutical, Phospholipids 50–
100 mg
phytosome Krupanidhi College ofsystemic Pharmacy,
antioxidant,
 Nanoparticles

🠶 Nanoparticles are nanosized particles, ranging from 10-1000nm, containing synthetic or semi
synthetic or herbal drugs.
🠶 These are used as carrier for hydrophilic and hydrophobic drugs.
🠶 Nanospheres have a matrix type structure in which the active ingredient is dispersed throughout
(the particles),
🠶 Nanocapsules have a polymeric membrane and an active ingredient core.
🠶 Nanoparticles are prepared with the objective to control particle size, surface properties of drug
and to achieve the site specific action of the drug.

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Preparation:
🠶Nanoparticles are prepared from dispersion of polymers by Different
techniques like nanoprecipitation, emulsification, salting out,
dialysis and supercritical fluid Technology.

Advantages:
🠶It can enhance compound solubility, reduce doses, can dilever drug to
site of action and improve absorbance.

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 Formulations Active Applications of Biological activity Method of preparation % Route of
ingredients nanostructured formulations Entrapment administrat
efficiency ion
Triptolide nanoparticle Triptolide Enhance the penetration of drugs Anti-inflammatory Emulsification-ultrasound – Topical
through the stratum corneum by (skin)
increased hydration
Nanoparticles of Flavonoids Improve water solubility, Hepatoprotective and Nanosuspension method 90% Oral
Cuscuta chinensis and antioxidant effects
lignans
Triptolide-loaded Triptolide Decreasing the toxicity Anti-inflammatory Emulsification-ultrasound – Oral
solid lipid nanoparticle
Artemisinin nanocapsules Artemisinin Sustained drug release Anticancer Self-assembly procedure 90–93% In vitro
Taxel-loaded nanoparticles Taxel Enhance the bioavailability Anticancer Emulsion solvent 99.44% –
and sustained drug release evaporation
method
Berberine-loaded Berberine Sustained drug release Anticancer Ionic gelation method 65.40 ± In vitro
nanoparticles 0.70%
Silibini-loaded nanoparticles Silibini High entrapment efficiency Hepatoprotective High pressure 95.64% –
and stability homogenizatio
n
Tetrandrine- Tetrandrine Sustained drug release Lung Self-emulsification and 84% In vitro
loaded solvent
nanoparticles evaporating
Glycyrrhizic acid- Glycyrrhizi Improve the bioavailability Anti- Rotary-evaporated 91.76% –
loaded nanoparticles c acid inflammatory, filmultrasonication method
antihypertensive
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 Micro-emulsion or
Nanoemulsion

Emulsion refers to a non-homogeneous dispersion system that is composed

of two kinds of liquids unable to dissolve each other, and one of which
disperse in the other one in a form of droplets. Generally, emulsion is
composed of oil phase, water phase, surfactant and sub-surfactant. Its
appearance is translucent to transparent liquid.
Emulsion can be classified into
• Ordinary emulsion (0.1–100 μm),
• Micro-emulsion (10– 100 nm) the Micro-emulsion is also
called Nanoemulsions
• Sub-micro-emulsion (100–600 nm), Sub-micro-emulsion is also called
lipid emulsion.
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Preparation
🠶 High pressure homogenization
🠶 Micro fluidization
🠶 Ultra sonication
🠶 Phase inversion Emulsification
🠶 Self Nanoemulsification
Advantages
🠶 Apart from its targeted sustained release, producing the herbal drug into
emulsion will also strengthen the
🠶 Stability of the hydrolyzed materials,
🠶 Improve the penetrability of drugs to the skin and mucous,

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 Formulations Active Applications of Biological Method of Droplet Drug Route of
ingredients Emulsion formulations activity preparation size loading administration
Self- Zedoary Improved aqueous Hepatoprotection Drawing 68.3± 30% Oral
nanoemulsifying Turmeric oil Dispersibility, stability and oral anticancer and ternary phase 1.6 nm
Zedoary essential bioavailability. anti-bacterial Diagram
oil
Triptolide micro- Triptolide Enhance the penetration of Anti- High b100 nm – Topical
emulsion drugs through the stratum inflammatory pressure
corneum by increased Homogenization
hydration method
Docetaxel Docetaxel Improve residence time Anticancer High 166.00 90% Intravenous
pressure nm
submicron Homogenization
emulsion method
Berberine Berberine Improve residence time and Anticancer Drawing 56.80 nm 0.50% Oral
nanoemulsion absorption ternary
phase diagram
Silybin Silybin Sustained release formulation Hepatoprotective Emulsification 21.20 nm – Intramuscular
nanoemulsion method
Quercetin micro- Quercetin Enhance penetration Antioxidant High 10– 0.3% Topical
emulsion into stratum corneum and pressure 100 nm solution
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epidermis Homogenization
THANK OU

4
4
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 Unit test 3

1. Annatto contain Bixin and Norbixin as colouring agent. Which colour gives
Norbixin?
A. Orange
B. Yellow
C. Red
D. Green
2. Coloring agent obtained from animal Source-
A. Cochineal
B. Spirulina
C. Indigo
D. Annatto
3. Which Sweetening agent not rise in blood sugar level?
A. Sucrose
B. Sorbitol
C. Thaumatin
D. Glucose

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 Unit test 3

4. The substance that holds or draws other materials together mechanically, chemically or as an
adhesive, to form a cohesive whole is known as _
A. Binding agent
B. Disintegrating agent
C. Viscosity Builders
D. Lubricant
5. Identify Flavouring agents except-
A. Cardamom oil
B. Ginger oil
C. Peppermint oil
D. Sandal wood oil
6. Simple Syrup contain %w/v of Sucrose
A. 60.67
B. 54.67
C. 66.67
D. 16.67

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 Unit test 3
7. Coating is carried out
A. To mask undesirable colour, odour and taste,
B. To protect from moisture or
C. To make sustained release product
D. All of the above
8. Loss on drying is carried out at O C temperate to determine LOD

A. 100
B. 90
C. 70
D. 105
9. Phospholipids layer enclosing an aqueous core is present in-
A. Nonoparticles
B. Matrix
C. Liposomes
D. Microemulsion
10. Size of Nanoparticles
A. 10-1000nm
B. 200-400 nm
C. 1-10 nm
D. 10-200 micrometer
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