星点设计-效应面优化法优化普罗布考自微乳化给药系统  

Optimization of the self micro-emulsifying drug delivery system of probucol by the central composite design-response surface methodology

作　　者：吴娟[1] 沙先谊[1] 方晓玲[1] 

机构地区：[1]复旦大学药学院药剂教研室,上海201203

出　　处：《复旦学报（医学版）》2010年第1期63-67,共5页Fudan University Journal of Medical Sciences

摘　　要：目的确定普罗布考自微乳化给药系统(self micro-emulsifying drug delivery system,SMEDDS)的较优处方。方法以微乳粒径、zeta-电位、药物在空白自微乳给药系统的平衡溶解度及5 min时药物的溶出度为指标,采用星点设计-效应面优化法,确定较优处方。结果处方中橄榄油占油相比例、油相占处方比例及表面活性剂与助表面活性剂的比值分别为0.33、0.5和2.0时,为较优处方。此时微乳粒径为92.7 nm,zeta-电位为-17.38 mV,药物在空白自微乳给药系统中的平衡溶解度为65.17 mg/mL,5 min时药物的溶出度为63.46%。结论应用星点设计-效应面优化法能够快速方便的得到普罗布考自微乳化给药系统的较优处方,所建立的模型预测性良好。Objective To determine the optimized self micro-emulsifying drug delivery system（SMEDDS） formulation of probucol. Methods According to the indexes of mean particle size,zeta-potential,solubility of probucol in blank SMEDDS and the dissolution percentage in 5 minutes of the preparations,the optimized formulation was determined by the central composite design-response surface methodology. Results When the correspondent percentage of olive oil in oil phase（W/W） was 0.33,the percentage of oil phase in formulation（W/W） was 0.5,and the ratio of surfactant to co-surfactant（W/W） was 2.0,respectively.The mean particle size,zeta-potential,solubility of probucol and dissolution percentage in 5 minutes of micro-emulsion was 92.7 nm,-17.38 mV,65.17 mg/mL and 63.46%,respectively. Conclusions The optimized formulation of the probucol SMEDDS was obtained quickly and conveniently by the central composite design-response surface methodology.The method had a reliable predictability.

关 键 词：普罗布考 自微乳化给药系统 星点设计-效应面优化 

分 类 号：R944.9[医药卫生—药剂学]