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Sublingual Dds

This document provides an overview of sublingual drug delivery. It discusses the anatomy and physiology of the oral mucosa, followed by different types of sublingual drug delivery systems including sublingual tablets, fast-disintegrating sublingual tablets, bioadhesive sublingual tablets, thin films, and lipid matrix sublingual tablets. It also covers sublingual immunotherapy, evaluation methods, marketed products, relevant patents, and references. The goal is rapid drug absorption through the oral mucosa to produce quick systemic effects while avoiding first-pass metabolism.

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175 views

Sublingual Dds

This document provides an overview of sublingual drug delivery. It discusses the anatomy and physiology of the oral mucosa, followed by different types of sublingual drug delivery systems including sublingual tablets, fast-disintegrating sublingual tablets, bioadhesive sublingual tablets, thin films, and lipid matrix sublingual tablets. It also covers sublingual immunotherapy, evaluation methods, marketed products, relevant patents, and references. The goal is rapid drug absorption through the oral mucosa to produce quick systemic effects while avoiding first-pass metabolism.

Uploaded by

randatag
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as PPT, PDF, TXT or read online on Scribd
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System

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SEMINAR ON
ublingual Drug Delivery

1. Anatomy physiology of mucosa


2. Sublingual tablets
3. Fast-disintegrating sublingual tablets
4. Bioadhesive sublingual tablet
5. Thin film drug delivery
6. Lipid matrix sublingual tablet
7. Sublingual immunotherapy
8. Sublingual vitamin tablet
9. Market preparation
10.PATENTS
11.References

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List of contents

1:Anatomy and Physiology of mucosa


Thickness of mucosa: 100-200 micrometer
Epithelium: Non keratinized
Composition: Neutral but polar lipid eg. Cholesterol sulfate,
Glucosyl ceramide
Composition of saliva: 99.5 % water, Proteins, Glycoprotein,
High K (7X Plasma), Bicarbonate( 3X plasma), Calcium,
Phosphorous, Chloride, Low sodium(1/10X Plasma)

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Sublingular gland: 5% saliva


pH : 5.6-7.0

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Mechanism of transportation
Highly vascular mucosal lining
Sublingual capillaries and veins
Jugular veins
Superior Vena cava

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Arterial Circulation

Sublingual tablets
They are to be placed under the tongue and produce immediate
systemic effect by enabling the drug absorbed directly through
mucosal lining of the mouth beneath the tongue.

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The drug absorbed from stomach goes to mesenteric circulation


which connects to stomach via portal vein. Thus, absorption through
oral cavity avoids first-pass metabolism

The tablets are usually small and flat, compressed lightly


to keep them soft. The tablet must dissolve quickly
allowing the API to be absorbed quickly. Its designed to
dissolve in small quantity of saliva. After the tablet is
placed in the mouth below the tongue, the patient should
avoid eating, drinking, smoking and possibly talking in
order to keep the tablet in place.

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Swallowing of saliva should also be avoided since the


saliva may contain dissolved drug. Bland excipients are
used to avoid salivary stimulation.

Advantages
1) Rapid absorption

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2) Dose reduction
3) Fast on set of action
4) Increase B.A.
5) Reduction in side effects
6) Suitable in disease like nausea, vomitting
7) Not required water

Disadvantage

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1) High dose can not be administered


2) Less area is available for absorption
3) Not suitable for bitter and irritating drugs
4) Less patient compliance
5) No eating, Drinking and smoking is allowed
6) Highly ionic drugs can not be administered

Suitability of API for preparation of sublingual tablet


Many drug properties could potentially affect the performance of
sublingual tablets.
For example, the solubility,
crystal morphology,
particle size,
hygroscopicity,
compressibility and
bulk density of a drug can significantly affect the final tablets
characteristics, such as tablet strength and disintegration.

Drugs that are unstable in parenteral preparation are suitable for


sublingual dosage form.

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Some drugs undergoes extensive first pass metabolism which


results in poor bioavailability of its oral dosage forms that kind of
drugs are suitable for sublingual dosage form.

Surface pH of the tablet


Uniformity of weight
Content uniformity
Hardness
Thickness
Diameter
Disintegration time
Wetting time and
Friability
Wetting Time (WT): The tablet was placed at the center of 2
layers of absorbent paper fitted into a rectangular plastic dish (11
cm 7.5 cm). After the paper was thoroughly wetted with
distilled water, excess water was completely drained out of the
dish. The time required for the water to diffuse from the wetted
absorbent paper throughout the entire tablet was then recorded
using a stopwatch

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Evaluation

3. Fast-disintegrating sublingual tablets

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Tablets that disintegrate or dissolve rapidly in the


patients mouth are convenient for young children, the
elderly and patients with swallowing difficulties, and in
situations where potable liquids are not available.

4. Bioadhesive sublingual tablet

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The new sublingual tablet concept presented is based on


interactive mixtures consisting of a water-soluble carrier
covered with fine drug particles and a bioadhesive component.
With this approach, it is possible to obtain rapid dissolution in
combination with bioadhesive retention of the drug in the oral
cavity.

5. Thin film drug delivery

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Thin film drug delivery is a process of delivering drugs to the


systemic circulation via a thin film that dissolves when in
contact with liquid, often referred to as a dissolving film or
strip. thin film strips are typically designed for oral
administran, with the user placing the strip on or under the
tongue or along the inside of the cheek. As the strip dissolves,
the drug can enter the blood stream enterically buccally or
sublingually.The sublingual delivery of a drug via thin film has
the potential to improve the onset of action, lower the dosing,
and enhance the efficacy and safety profile of the medicament.

6. Lipid matrix sublingual tablet


Lipid Matrix Sublingual Tablet is formulated using advances in
sublingual and liposomal technology to create a dosage form that offers a
faster and more complete absorption than traditional oral routes of
administration.

Examples Include: Glutathione MB12 (Methylcobalamin) Melatonin


A True Sublingual Tablet + Lipid Matrix Technology:
Not a Lozenge, Troche, or Tablet Triturate: A True Sublingual Tablet!
Rapid Dissolve Formula
Liposomal Drug Delivery
Bioavailable & Avoids First Pass Effect
Convenient & Consistent Dosing Application
Single or Combination Drug Delivery

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The Lipid Matrix Sublingual Tablet is a bioavailable, quick, convenient,


and consistent dosage form for many specialty nutraceuticals that are
often taken orally.

7. Sublingual immunotherapy
Sublingual immunotherapy, or SLIT, is a form of immunotherapy
that involves putting drops of allergen extracts under the tongue.
SLIT is usually delivered one of two ways: drops (or tablets) of
allergen extract are placed under the tongue, then either swallowed
or spat out.

8. Sublingual vitamin tablet

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The only Sublingual vitamin that all doctors recommend is vitamin


B12 (Cyanocobalamin). you must have enough of it for your
bodies metabolism.
Recommended to be taken once a day.

9. Market preparation
Tenormin sublingual tablet (isoproterenol)
Microtab sublingual tablet (nicotine)
Nascobal sublingual tablet (vitamin B12)
Subuter sublingual tablet (buprenorphine)

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Nitroquick sublingual tablet (nitroglycerin)

10.PATENTS
4539315
4927816
4988683
5320848
5629022
5683721
6183775
6447754

SUBJECT

Sublingually absorbable nontoxic aspirin


composition
Formulae and methods for sublingual ingestion of
natural progesterone
New pharmaceutical compositions for the buccal
tract and process for their preparation
Chewable drug-delivery composition
Method for galenically preparing a therapeutic
composition based on aspirin
Galenic preparation of therapeutic composition
comprising aspirin
Buccal delivery system
Oral rinse methods and compositions

YEAR
1985
1990
1991
1994
1997
1997
2001
2002

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US PATENT
NO.

REFERENCE
1.Hariharan,
Madhu;
Bogue,
B.
Arlie
(February
2009).
"Orally Dissolving Film Strips (ODFS): The Final Evolution of Orally Dissolving Dosage Forms".
Drug Delivery Technology (Montville, New Jersey) 9 (2): 24-29. ISSN 1537-2898. OCLC 48060225.
http://www.drugdeliverytech-online.com/drugdelivery/200902/?pg=24.
2."Oral Thin Films," in Orally Disintegrating Tablet and Film Technologies, 5th ed. (Technology
Catalysts International, Falls Church, VA, 2008)
3."S. S. Biradar, S. T. Bhagavati, I. J. Kuppasad: Fast Dissolving Drug Delivery Systems: A Brief
Overview. The Internet Journal of Pharmacology. 2006. Volume 4 Number 2".
4.
"Thin
Film
Manufacturing
Process
Patent".
http://www.monosolrx.com/news_08/news_41508.html. Retrieved 2009-09-21

Monosolrx.com.

5.Mathiowitz,E., Chickering, D.E., Lehr, C.M. (eds.), Bioadhesive drug delivery systems:
Fundamentals, novel approaches and development. Marcel Dekker Inc, New York, USA, pp. 1-10.
6.Duchne, D., Touchard, F., Peppas, N.A., 1988. Pharmaceutical and medical aspects of bioadhesive
systems for drug administration. Drug Dev. Ind. Pharm., 14, 283-318.

8.D. Harris and J. R. Robinson, Drug delivery via the mucous membranes of the oral cavity, J.
Pharm.Sci. 81 (1992) 110; DOI: 10.1002/jps.2600810102.
9.www.pharmainfo.net
10.www.pubmed.com

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7.Mahrag Tur, K., Chng, H.-S., 1998. Evaluation of possible mechanim(s) of bioadhesion. Int. J.
Pharm., 160,61-74.

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THANK YOU

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