SEMINAR ON Sublingual Drug Delivery System

1/20

2

Sublingual

List of contents1. 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

3/20

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

4/20

5/20

Mechanism of transportation   Highly vascular mucosal lining

Sublingual capillaries and veins

Jugular veins

Superior Vena cava

Arterial Circulation

6/20

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

7/20

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.

Swallowing of saliva should also be avoided since the saliva may contain dissolved drug. Bland excipients are used to avoid salivary stimulation.

8/20

1) Rapid absorption2) Dose reduction3) Fast on set of action4) Increase B.A.5) Reduction in side effects6) Suitable in disease like nausea, vomitting7) Not required water

AdvantagesAdvantages

9/20

DisadvantageDisadvantage

1) High dose can not be administered2) Less area is available for absorption3) Not suitable for bitter and irritating drugs4) Less patient compliance5) No eating, Drinking and smoking is allowed6) Highly ionic drugs can not be administered

10/2

0

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.

•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.

•Drugs that are unstable in parenteral preparation are suitable for sublingual dosage form. 11

/20

Evaluation•Surface pH of the tablet•Uniformity of weight •Content uniformity•Hardness•Thickness•Diameter•Disintegration time •Wetting time and •FriabilityWetting 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

12/2

0

3. Fast-disintegrating sublingual tablets

•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.

13/2

0

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.

14/2

0

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.

15/2

0

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) MelatoninA 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 16

/20

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.

17/2

0

9. Market preparation

•Tenormin sublingual tablet (isoproterenol)

•Microtab sublingual tablet (nicotine)

•Nascobal sublingual tablet (vitamin B12)

•Subuter sublingual tablet (buprenorphine)

•Nitroquick sublingual tablet (nitroglycerin)

18/2

0

10.PATENTS US PATENT NO.

SUBJECT YEAR

4539315Sublingually absorbable nontoxic aspirin composition

1985

4927816Formulae and methods for sublingual ingestion of natural progesterone

1990

4988683New pharmaceutical compositions for the buccal tract and process for their preparation

1991

5320848 Chewable drug-delivery composition 1994

5629022Method for galenically preparing a therapeutic composition based on aspirin

1997

5683721Galenic preparation of therapeutic composition comprising aspirin

1997

6183775 Buccal delivery system 2001

6447754 Oral rinse methods and compositions 2002

19/2

0

REFERENCE1.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.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. 

7.Mahrag Tur, K., Ch’ng, 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) 1–10; DOI: 10.1002/jps.2600810102. 

9.www.pharmainfo.net 

10.www.pubmed.com  20/2

0

21/2

0

THANK YOU