Preparation and in Vitro Drug Release Evaluation of Once-Daily Metformin Hydrochloride Sustained-Release Tablets

Abstract

The objective of this study was to develop once-daily metformin hydrochloride sustained-release tablets (MHSRT) and evaluate their in vitro release behavior. MHSRT were prepared by the film coating method. The in vitro drug release rate of MHSRT and the commercial tablets Fortamet? made in the United States of America in water was fitted with zero order kinetic equation, and Ritger-Peppas kinetic equation in 0.1 M HCl and pH 6.8-phosphate buffer, respectively. The similarity factor f2 values of MHSRT in three different dissolution medium were 82, 80 and 74, respectively in comparison with imported Fortamet?, which were all greater than 50. The results of storage-stability showed that MHSRT were stable for at least 6 months under stress condition (40℃ ± 2℃, RH 75% ± 5%). Therefore, in this study, MHSRT were successfully prepared using optimized formulation technologies that meet mass produce. The in vitro release behavior of MHSRT was almost similar to that of imported Fortamet?.

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L. Zhao, Y. Wei, Y. Mei, L. Yang, Y. You, X. Yang and Y. Jiang, "Preparation and in Vitro Drug Release Evaluation of Once-Daily Metformin Hydrochloride Sustained-Release Tablets," Pharmacology & Pharmacy, Vol. 3 No. 4, 2012, pp. 468-473. doi: 10.4236/pp.2012.34064.

Conflicts of Interest

The authors declare no conflicts of interest.

References

[1] X. X. Yin, Y. D. Zhang, H. T. Zhuo, J. P. Shen, L. M. Li, Q. J, “Pharmacokinetics and relative bioavailability of metformin hydrochloride sustained release tablets in healthy Chinese volunteers,”Asian J. Drug Metab. Pharmacok, Vol.4, No.2, 2004, pp.137-142.
[2] G. Corti, M. Cirri, F. Maestrelli, N. Mennini, P. Mura, “Sustained-release matrix tablets of metformin hydrochloride in combination with triacetyl–beta-cyclodextrin,” Eur. J. Pharm. Biopharm, Vol.68, No.2, 2008, pp. 303-309.
[3] L. D. Hu , Y. Liu, X. Tang, Q. Zhang, “Preparation and in vitro/in vivo evaluation of sustained-release met-formin hydrochloride pellets,” Eur. J. Pharma. Biopharma, Vol.64, No.2, 2006, pp.185-192.
[4] P. J. Pentikainen, P. J. Neuvonen, A. Penttila, “Pharmacokinetics of metformin after intravenous and oral administration to man,” Eur. J. Clin. Pharmacol, Vol. 16, No. 3, 1979, pp.195-202.
[5] G. T. Tucker, C. Casey, P. J. Phillips, H. Connor, J. D. Ward, H. F. Woods, “Metformin kinetics in healthy subjects and in patients with diabetes mellitus,” Br. J. Clin. Pharmacol, Vol. 12, No. 2, 1981, pp.235-246.
[6] P. K. Bhoyar, D. M. Biyani, “Formulation and In vitro Evaluation of Sustained Release Dosage Form with Taste Masking of Metformin Hydrochloride,” Indian J. Pharm. Sci, Vol. 72, No. 2, 2010, pp.184-190.
[7] O. Defang, N. Shufang, L. Wei, G. Hong, L. Hui, P. Weisan, “In vitro and in vivo evaluation of two extended release preparations of combination metformin and glipizide,” Drug Dev. Ind. Pharm, Vol. 31, No. 7, 2005, pp.677-685.
[8] A. Ghosh, A. Bose, U. Bhaumik, “Application of Response Surface Methodology in the Formulation of Sustained Release Matrix Tablets of Metformin Hydrochloride,” Asian J. Chem, Vol. 20, No. 7, 2008, pp. 5541-5556.
[9] J. Piao, J. E. Lee, K.Y. Weon, D. W. Kim, J. S. Lee, J. D. Park, Y. Nishiyama, I. Fukui, J. S. Kim, “Development of novel mucoadhesive pellets of metformin hydrochloride,” Arch. Pharm. Res, Vol. 32, No. 3, 2009, pp. 391-397.
[10] P. Subhedar, J. B. Naik, D. N. Muley, “Effect of Polymer Concentration on Sustained Release Microparticles of Metformin Hydrochloride Prepared by Using Spray Dryer,” Polymer-Plast. Technol, Vol. 49, No. 1-3, 2010, pp. 267-271.
[11] H. F. Liu, X. Y. Su, X. Li, X. Zhao, L. Zang, W. S. Pan, “Development of Prolonged Release Microspheres of Metformin Hydrochloride Using Ion Exchange Resins,” J. Chinese Pharmaceu. Sci, Vol. 15, No. 3, 2006, pp. 155-161.
[12] S. P. Boldhane, B. S. Kuchekar, “Gastroretentive drug delivery of metformin hydrochloride: formulation and in vitro evaluation using 3(2) full factorial design,” Current drug deliver, Vol. 6, No. 5, 2009, pp. 477-485.
[13] G. Di Colo, S. Falchi, Y. Zambito, “In vitro evaluation of a system for pH-controlled peroral delivery of metformin,” J. Contro. Rel, Vol. 80, No. 1-3, 2002, pp. 119-128.
[14] P. C. Wu, M. J. Tsai, Y. B. Huang, J. S. Chang, Y. H. Tsai, “In vitro and in vivo evaluation of potassium chloride sustained release formulation prepared with saturated polyglycolyed glycerides matrices,” Int. J. Pharm, Vol. 243, No. 1-2, 2002, pp. 119-124.
[15] J. E. Polli, G. S. Rekhi, L L. Augsburger, V. P. Shah, “Methods to compare dissolution profiles and a rationale for wide dissolution specifications for metoprolol tartrate tablets,”J. Pharm. Sci. Vol. 86, No. 6, 1997, pp. 690-700.
[16] S.G. Wang, L. Wang, Z. Z. Shao, X. P. Lu, X. Q. Hang, “Study on the release rate of niacin in different media for the compound niacin extended-release and simvastatin tablets,”Chinese J. Pharmaco, Vol. 8, No. 10, 2011, pp. 581-584.
[17] N. A. Peppas, “Analysis of Fickian and non-Fickian drug release from polymers,” Vol. 60, No. 4, 1985, pp. 110-111.

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