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KMID : 0369820070370060339
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Jorunal of Korean Pharmaceutical Sciences
2007 Volume.37 No. 6 p.339 ~ p.347
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Improvement of Solubility of Atorvastatin Calcium Using Self-Microemulsion Drug Delivery System(SMEDDS)
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Lee Jun-Hee
Mo Jong-Hyun
Kim Moon-Suk
Khang Gil-Son
Lee Hae-Bang
Choi Myoung-Kyu
Kim Yun-Tae
Kim Myoung-Jin
Oh Jae-Min
Park Jung-Soo
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Abstract
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SMEDDS is mixture of oils, surfactants, and cosurfactants, which are emulsified in aqueous media under conditions of gentle agitation and digestive motility that would be encountered in the gastro-intestinal(GI) tract. The main purpose of this work is to prepare self-microemulsifying drug delivery system(SMEDDS) for oral bioavailability enhancement of a poorly water soluble drug, atorvastatin calcium. Solubility of atorvastatin calcium was determined in various vehicles. Pseudo-ternary phase diagrams were constructed to identity the efficient self-emulsification region and particle size distributions of the resultant micro emulsions were determined using a laser diffraction sizer. Optimized formulations for in vitro dissolution and bioavailability assessment were 90(50%), Tetraglycol(16%), and EL(32%). The release rate of atorvastatin from SMEDDS was significantly higher than the conventional tablet (), 2-fold. Our studies illustrated the potential use of SMEDDS for the delivery of hydrophobic compounds, such as atorvastatin calcium by the oral route.
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KEYWORD
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Atorvastatin calcium, SMEDDS, Phase diagram, Cosurfactant, Surfactant, Oil
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