Formulation and In-vitro evaluation of sustained release matrix tablet of Metformin hydrochloride
Abstract
The low bioavailability and short half-life of Metformin hydrochloride (MH) make the development of sustained-release forms desirable. Present work involves preparation and optimization of sustained release matrix tablet of MH by direct compression method using HPMC K 100 and ethyl cellulose as a matrix forming polymer. Avicel was added as a direct compaction vehicle to improve the compaction behavior of Metformin which otherwise exhibits poor compaction behavior which again is further increased by its relatively high dose. Hydrophilic matrix of HPMC alone resulted in initial burst of Metformin release, however when combined with ethyl cellulose drug release was slowed down and thereafter it became optimal at particular concentration of polymers.
Keywords: Metformin, HPMC, Ethyl cellulose, sustained release, matrix, tablet.
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References
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2. Vyas SP and Khar RK, Controlled Drug Delivery, Concepts and Advances, 2002; First edition, Vallabh Prakashan, Delhi: 1-2, 10-12, 156-160.
3. Chien YW, Concepts and system design for Rate controlled drug delivery. In: Novel Drug Delivery Systems 2nd ed. New York: Marcel Dekker; 1992. P. 1‑38.
4. Hu LD, Liu Y, Preparation and in vitro/in vivo evaluation of sustained-release metformin hydrochloride pellets, Eur. J. Pharm. Biopharm. 64 (2006) 185–192.
5. Stepensky D, Friedman M, Srour W, Raz I, Hoffman A, Preclinical evaluation of pharmacokinetic–pharmacodynamic rationale for oral CR metformin formulation, J. Control. Release 2001; 71:107-115.
6. Siepe S, Lueckel B, Kramer A, Strategies for the design of hydrophilic matrix tablets with controlled microenvironmental pH, Int. J Pharm 2006; 316:14-20.
7. Sung KC, Nixon PR, Skoug JW, Effect of formulation variables on drug and polymer release from HPMC based matrix tablets. Int. J Pharm 1996; 142:53-60.
8. Dunn C.J. and Peters D.H. Metformin: A review of its pharmacological properties and therapeutic use in non-insulin-dependent diabetes mellitus. Drugs., 1995; 49:721-749.
9. Defang O, Shufang N, and Wei L., In vitro and in vivo evaluation of two extended Release preparations of combination metformin and glipizide. Drug Dev. Ind. Pharm., 2005, 31, 677–685.
10. Stepensky D, Friedman M , Srour W , Raz I , and Hoffman A., Preclinical evaluation of pharmacokinetic–pharmacodynamic rationale for oral CR metformin formulation, J. Cont. Rel,2001; 71:107–115.
11. Shaikh N.A, Abidi S.E. and Block L.H., Evaluation of ethylcellulose matrix for prolonged release formulations: Water soluble drugs: acetaminophen and theophylline. Drug Dev. Ind. Pharm., 1987; 13:1345-1369.
12. Colombo R, Bettini P.S, Peppas N.A., Swellable matrixes for controlled drug delivery: gel-layer behavior, mechanisms and optimal performance, Pharm. Sci. Technol. Today., 2000; 3:198–204.
13. Siepmann J, Kranz H, Bodmeier R, and Peppas NA., HPMC-matrices for controlled drug delivery: a new model combining diffusion, swelling, and dissolution mechanisms and predicting the release kinetics. Pharm Res., 1999; 16:1748-1756.
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Gaware RU, Waykar GR, Yewale MK, Mhaske RB, Mhaske PS. Formulation and In-vitro evaluation of sustained release matrix tablet of Metformin hydrochloride. JDDT [Internet]. 15May2019 [cited 28Feb.2020];9(3):95-8. Available from: http://jddtonline.info/index.php/jddt/article/view/2606
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