화학공학소재연구정보센터
학회 한국고분자학회
학술대회 2005년 가을 (10/13 ~ 10/14, 제주 ICC)
권호 30권 2호
발표분야 의료용 고분자 부문위원회
제목 Improvement of insolubility by using self-emulsifying drug delivery system
초록 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. Absolute bioavailability of atorvastatin is about 14% and the whole body availability of control on HMG-CoA reductase is 30%. Characterization of atorvastatin calcium was determinated by XRD, DSC. Solubility of atorvastatin was determined in various vehicles. Pseudo-ternary phase diagrams were constructed to identify 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 90 (50%), Cremophor EL (38.4%), and Carbitol (9.6%). The release rate of atorvastatin from SMEDDS was significantly higher than the conventional tablet(Lipitor®). The absorption of simvastatin acid from SMEDDS form resulted in about 1.5-fold increase in bioavailability compared with the conventional tablet. Our studies illustrated the potential use of SMEDDS for the delivery of hydrophobic compounds, such as atorvastatin by the oral route.


Acknowledgment : This work was supported by KMOHW (0405-BO01-0204-0006).
저자 김순희1, 서성미2, 이창래1, 이규배1, 김문석2, 이종문1, 이해방2, 강길선1
소속 1전북대, 2한국화학(연)
키워드 SMEDDS; Atorvastatin; capryol90; cremophorEL; tetraglycol
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