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SEMINAR ON
Sublingual Drug Delivery
System
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. It’s 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 tablet’s
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
patient’s 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.drugdeliverytechonline.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.Duchêne, 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) 1–10; DOI: 10.1002/jps.2600810102.
9.www.pharmainfo.net
10.www.pubmed.com
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7.Mahrag Tur, K., Ch’ng, H.-S., 1998. Evaluation of possible mechanim(s) of bioadhesion. Int. J.
Pharm., 160,61-74.
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