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Similar to Sublingual drug delivery
Sublingual drug delivery
- 1. Makwana Saroj V, B.k.ModyGovernment Pharmacy College, Rajkot. Sublingual drug delivery
- 2. Sublingual drug deliverysystem: 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 B.K.Mody Gov. Pharmacy college,Rajkot. 2
- 3. Factors affecting thesublingual absorption: • Lipophilicity of drug: Drug must have slightly higher lipid solubility than tha t required for GI absorption is necessary for passive permeation. • Solubility in salivary secretion: Drug soluble in aqueous buccal fluid • pH and pKa of the saliva: pH of the saliva is 6.0, this pH favors the absorption of drugs which remain unionized. • The absorption of the drugs through the oral mucosa occurs if the pKa is g reater than 2 for an acid and less than 10 for a base. B.K.Mody Gov. Pharmacy college,Rajkot. 3
- 4. B.K.Mody Gov. Pharmacycollege,Rajkot. 4 • Binding to oral mucosa: Systemic availability of drugs that bind to oral mucosa is poor. • Thickness of oral epithelium: thickness of sublingual epithelium-100-200 μm which is less compared to buccal thickness. • Absorption of drugs is faster due to thin epithelium. • Oil to water partition coefficient:40-2000 optimal for drug absorption.
- 5. Rapid absorption Dose reduction Increase Bioavaibility Reductionin side effects Suitable in disease like nausea, vomiting Not required water Advantages: B.K.Mody Gov. Pharmacy college,Rajkot. 5
- 6. Disadvantage B.K.Mody Gov. Pharmacycollege,Rajkot. 6 High dose can not be administered Less area is available for absorption Not suitable for bitter and irritating drugs Less patient compliance No eating, Drinking and smoking is allowed Highly ionic drugs can not be administered
- 7. 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. B.K.Mody Gov. Pharmacy college,Rajkot. 7
- 8. Fast-disintegrating sublingual tablets B.K.ModyGov. Pharmacy college,Rajkot. 8 • 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. • Only the small volume of saliva is usually sufficient to result in tablet disintegration in the oral cavity. • Medication can then be absorbed partially or entirely into the systemic circulation from blood vessels in the sublingual mucosa.
- 9. Thin film drugdelivery • Delivering drugs to the systemic circulation via a thin film that dissolves when in contact with liquid, referred to as a dissolving film or strip. • Advantage: • Potential to improve the onset of action, • Lower the dosing, • Enhance the efficacy • Safety profile of the medicament. B.K.Mody Gov. Pharmacy college,Rajkot. 9
- 10. Lipid matrix sublingualtablet • 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 neutraceuticals that are often taken orally. B.K.Mody Gov. Pharmacy college,Rajkot. 10
- 11. B.K.Mody Gov. Pharmacycollege,Rajkot. 11 • Examples: 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
- 12. Sublingual immunotherapy: • 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. • Swallowing the extract seems to work better. • Immunotherapy by the oral route (swallowed and not kept under the tongue for any period of time), causes too many gastrointestinal side effects (nausea, vomiting, diarrhea), and therefore is not used. B.K.Mody Gov. Pharmacy college,Rajkot. 12
- 13. Sublingual immunotherapy: B.K.Mody Gov.Pharmacy college,Rajkot. 13 • Administered : • Daily • Multiple times per week, • Over a period of year. • Uses: • Pediatric patients with allergic rhinitis and/or asthma due to grass pollen.
- 14. Sublingual vitamin tablet: •The only Sublingual vitamin that all doctors recommend is vitamin B12 (Cyanocobalamin). • Recommended to be taken once a day. B.K.Mody Gov. Pharmacy college,Rajkot. 14
- 15. Evaluation • In vitroevaluation : • Uniformity of weight • Content uniformity • Hardness • Thickness • Diameter • Disintegration time • Friability B.K.Mody Gov. Pharmacy college,Rajkot. 15
- 16. Wetting Time (WT): B.K.ModyGov. Pharmacy college,Rajkot. 16 • The tablet was placed at the centre 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.
- 17. In-vivo evaluation: B.K.Mody Gov.Pharmacy college,Rajkot. 17 o Pharmacokinetic data analysis oMaximal plasma concentration (Cmax) oTime to reach maximum plasma concentration (Tmax) oPlasma concentration‐ curve (AUC) o Bioavailability evaluation
- 18. Drugs used inthe formulation of sublingual dosage forms: • Physostigmine salicylate -Anti‐Alzheimer’s • Scopolamine - Opioid analgesic Spray • Furosemide - Diuretic Tablet • Nifedipine, Nitro-glycerine - Anti‐anginal Tablet • Vinpocetine - Neutropic Agent Tablet • Terbutaline sulphate -Bronchodilator Tablet • Amlodipine besylate , Captopril - Anti hypertensive Tablet • Ondansetron Hydrochloride - Anti emetic Film • Salbutamol sulphate - Anti‐asthmatic agent B.K.Mody Gov. Pharmacy college,Rajkot. 18
- 19. Market preparation: • Tenorminsublingual tablet (isoproterenol) • Microtab sublingual tablet (nicotine) • Nascobal sublingual tablet (vitamin B12) • Subuter sublingual tablet (buprenorphine) • Nitroquick sublingual tablet (nitroglycerin) B.K.Mody Gov. Pharmacy college,Rajkot. 19
- 20. References : • AnOverview On Buccal Drug Delivery System, by Surender Verma, Mahima Kaul, Aruna Rawat and Sapna Saini, IJPSR (2011), Vol. 2, Issue 6,page no.:1-19. • A Review on Buccal Mucoadhesive Drug Delivery Systems, by Santanu Roychowdhury, Rajesh Gupta, Sourav Saha ,Indo-Global Journal of Pharmaceutical Sciences, 2011, Vol 1., Issue 3: Page No. 223-233. • A Review on Buccal Drug Delivery System Nishan N. Bobade , Sandeep C. Atram, Vikrant P. Wankhade, Dr. S.D. Pande, Dr. K.K. Tapa, International Journal of Pharmacy and Pharmaceutical Science Research, 2013; 3(1) page no-35-41, B.K.Mody Gov. Pharmacy college,Rajkot. 20
- 21. References : B.K.Mody Gov.Pharmacy college,Rajkot. 21 • An Overview on: Sublingual Route for Systemic Drug Delivery by,K. Patel Nibha1 and SS. Panchol, International Journal of Research in Pharmaceutical and Biomedical Sciences ,Vol. 3 (2) Apr – Jun2012,page no-913-923 • Formulation And Evaluation Of Bioadhesive Buccal Tablets Of Simvastatin B. Agaiah Goud, Kumara Swamy. S And Praveen Kumar. V, JAPS/Vol.1/Issue 1/2011,page no-29-38. • Buccal Drug Delivery: Past, Present and Future – A Review, by A. Puratchikody, Prasanth V.V, Sam T. Mathew, Ashok Kumar B, International Journal of Drug Delivery 3 (2011) page no-171-184.
- 22. References : • AReview on study of Buccal Drug Delivery System,by Rajesh Mujoriya, Innovative Systems Design and Engineering ,Vol 2, No 3,page no-1-14. • Sublingual Mucosa As A Route For Systemic Drug Delivery,by Neha Narang1, Jyoti Sharma, International Journal of Pharmacy and Pharmaceutical Sciences,Vol 3, Suppl 2, 2011,page no-1-5. • Buccal Mucosa As A Route For Systemic Drug Delivery: A Review, by Amir H. Shojaei, J Pharm Pharmaceut Sci (www.ualberta.ca/~csps) 1 (1):15-30, 1998,page no-15-31. B.K.Mody Gov. Pharmacy college,Rajkot. 22
- 23. References : • RecentAdvances In Mucoadhesive Buccal Drug Delivery Systems And Its Marketed Scope And Opportunities ,by K.P.Sampath Kumar ,DebjitBhowmik,AmitsankarDutta ,ShravanPaswan, Issue 1 : 2012,page no:79-93. • A review on bioadhesive buccal drug delivery systems: current status of formulation and evaluation methods by Chinna Reddy P,Chaitanya K.S.C.,Madhusudan Rao Y, DARU Journal of Pharmaceutical Sciences Vol. 19, No. 6 2011,page no385-405. • Sublingual Route For Systemic Drug Delivery Amit Kumar Bind,G. Gnanarajan and Preeti Kothiyal, Int. J. Drug Res. Tech. 2013, Vol. 3 (2), page no-31-36. B.K.Mody Gov. Pharmacy college,Rajkot. 23
- 24. B.K.Mody Gov. Pharmacycollege,Rajkot. 24
Editor's Notes
- #9 The sublingual route usually produces a faster onset of action than orally ingested tablets and the portion absorbed through the sublingual blood vessels bypasses the hepatic first-pass metabolic processes.
- #10 Thin film strips are typically designed for oral administration, with the user placing the strip on or under the tongue or along the inside of the cheek.