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KMID : 0614020060210010066
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Journal of Pharmaceutical Sciences (C.N.U.)
2006 Volume.21 No. 1 p.66 ~ p.72
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Preparation and dissolution properties of oral controlled release formulations containing metformin hydrochloride
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Goo Bon-Cheol
Kim Jeong-Soo
Lee Gye-Won
Jee Ung-Kil
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Abstract
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Metformin is an antihyperglycemic agent of the biguanide class used in the treatment of non-in-sulin-dependent diabetes mellitus. Metformin hydrochloride has intrinsically poor permeability in the lower portion of the GI-tract leading to absorption almost exclusively in the upper part of the GI-tract. Its oral bioavailability is in the range of 50 to 60%. It also has a very high water solubility. In this study, we prepared sustained release matrix system containing metformin hydrochloride using various characteristics of polyethylene oxide (PEO). The metformin hydrochloride matrix tablets were prepared by direct compressed method and wet granulation compressed method with various molecular weight of PEO. Even though the molecular weights of PEOs used were 900K, 2,000K, and 5,000K. Moreover, three types of matrix tablets were formulated compositions were same, the hardness was different. The release kinetics were studied for 9 hours in pH 1.2 simulated gastric fluid and pH 6.8 simulated intestinal fluid, using a dissolution tester at 37.5℃, 50 rpm. As the molecular weight of PEO increased, the release rate decreased due to the slower swelling and dissolution of PEO. For the effect of hardness of matrix tablets, the rate of drug release was decreased with increasing hardness.
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KEYWORD
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Sustained release, Metformin hydrochloride, Polyethylene oxide(PEO)
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