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KMID : 0369820080380020111
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Jorunal of Korean Pharmaceutical Sciences
2008 Volume.38 No. 2 p.111 ~ p.117
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Improved Dissolution and Characterization of Solid Dispersed Atorvastatin Calcium
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Lee Jun-Hee
Ku Jeong
Park Jung-Soo
Park Jong-Hak
Ahn Sik-Il
Mo Jong-Hyun
Kim Yun-Tae
Rhee John-M
Lee Hae-Bang
Khang Gil-Son
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Abstract
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To overcome the solubility of poorly water-soluble drug, the formation of solid dispersion using a spray-dryer with polymeric material, that can potentially enhance the dissolution rate extend of drug absorption was considered in this study. E100 as carrier for solid dispersion is acrylate copolymer that soluble in acidic buffer solutions (below pH 5.0). It was used to increase dissolution of atorvastatin calcium as a water-insoluble drug in acidic environments. In this study, a spray-dryer was used to prepare solid dispersion of atorvastatin calcium and E100 for purpose of improving the solubility of drug. Atorvastatin calcium and E100 were dissolved in ethanol and spray-dryed. DSC and XRD were used to analyze the crystallinity of the sample. It was found that atorvastatin calcium is amorphous in the E100 solid dispersion. FT-IR was used to analyze the salt formation by interaction between atorvastatin calcium and E100. Comparative dissolution study exhibited better dissolution characteristics than the commercial drug () as control. The dissolution rate of atorvastatin calcium was markedly increased in solid dispersion system in simulated gastric juice (pH 1.2). This study proposed that this solid dispersion system improved the bioavailability of poorly water-soluble atorvastatin calcium.
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KEYWORD
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Solid dispersion, Spray dryer, Atorvastatin calcium, E100, Dissolution rate
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