SEMINAR ON

Sublingual Drug Delivery

System

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List of contents
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

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11.References
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)

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

Arterial Circulation

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 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.

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

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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.

Swallowing of saliva should also be avoided since the

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

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 Advantages
1) Rapid absorption
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

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 Disadvantage
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

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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.

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.

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Drugs that are unstable in parenteral preparation are suitable for
sublingual dosage form.
Evaluation
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

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using a stopwatch
3. Fast-disintegrating sublingual tablets

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.

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4. Bioadhesive sublingual tablet

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.

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5. Thin film drug delivery

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.

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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.

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

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

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

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Convenient & Consistent Dosing Application
Single or Combination Drug Delivery
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

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.

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9. Market preparation

Tenormin sublingual tablet (isoproterenol)

Microtab sublingual tablet (nicotine)

Nascobal sublingual tablet (vitamin B12)

Subuter sublingual tablet (buprenorphine)

Nitroquick sublingual tablet (nitroglycerin)

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10.PATENTS
US PATENT SUBJECT YEAR
NO.
Sublingually absorbable nontoxic aspirin 1985
4539315
composition
Formulae and methods for sublingual ingestion of 1990
4927816
natural progesterone
New pharmaceutical compositions for the buccal 1991
4988683
tract and process for their preparation
5320848 Chewable drug-delivery composition 1994
Method for galenically preparing a therapeutic 1997
5629022
composition based on aspirin
Galenic preparation of therapeutic composition 1997
5683721
comprising aspirin
6183775 Buccal delivery system 2001

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6447754 Oral rinse methods and compositions 2002
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". Monosolrx.com.
http://www.monosolrx.com/news_08/news_41508.html. Retrieved 2009-09-21
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.
7.Mahrag Tur, K., Chng, H.-S., 1998. Evaluation of possible mechanim(s) of bioadhesion. Int. J.
Pharm., 160,61-74.
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.

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9.www.pharmainfo.net
10.www.pubmed.com
THANK YOU

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