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http://dx.doi.org/10.4333/KPS.2007.37.6.339

Improvement of Solubility of Atorvastatin Calcium Using Self-Microemulsion Drug Delivery System(SMEDDS)  

Lee, Jun-Hee (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University)
Choi, Myoung-Kyu (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University)
Kim, Yun-Tae (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University)
Kim, Myoung-Jin (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University)
Oh, Jae-Min (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University)
Park, Jung-Soo (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University)
Mo, Jong-Hyun (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University)
Kim, Moon-Suk (Nanobiomaterials Laboratory, Korea Research Institute of Chemical Technology)
Khang, Gil-Son (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University)
Lee, Hai-Bang (Nanobiomaterials Laboratory, Korea Research Institute of Chemical Technology)
Publication Information
Journal of Pharmaceutical Investigation / v.37, no.6, 2007 , pp. 339-347 More about this Journal
Abstract
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 $Capryol^{(R)}$ 90(50%), Tetraglycol(16%), and $Cremophor^{(R)}$ EL(32%). The release rate of atorvastatin from SMEDDS was significantly higher than the conventional tablet ($Lipitor^{(R)}$), 2-fold. Our studies illustrated the potential use of SMEDDS for the delivery of hydrophobic compounds, such as atorvastatin calcium by the oral route.
Keywords
Atorvastatin calcium; SMEDDS; Phase diagram; Cosurfactant; Surfactant; Oil;
Citations & Related Records
Times Cited By KSCI : 5  (Citation Analysis)
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