米托噻咯自微乳处方优化及体内外评价  

Optimization, in vitro and in vivo Evaluation of Mitothiorole Self-microemulsions

作　　者：吕祎凡 孙寅静[1] 李瑾[1] 陆伟跃[1] 潘俊[1] 

机构地区：[1]复旦大学药学院药剂学教研室,上海201203

出　　处：《中国医药工业杂志》2010年第11期836-840,共5页Chinese Journal of Pharmaceuticals

基　　金：国家重点基础研究发展计划(973计划)资助项目(2007CB935800)

摘　　要：采用自乳化技术将米托噻咯制成自微乳递释系统,并采用两因素五水平的星点设计,利用效应面法考察了影响递释系统的主要因素(如油相比例,两种表面活性剂的质量比),以微乳的粒径、ζ电位及药物平衡溶解度为评价指标,建立相应的数学模型。所得优化处方为:油相比例为11%,表面活性剂比例Cremophor EL∶Labrasol为1.95(w/w)。相对于其混悬剂,米托噻咯自微乳的口服生物利用度为436.3%。Self-microemulsions loaded with mitothiorole was prepared with self-emulsion technology.Independent formulation variables such as the mass ratio of Cremophor EL to Labrasol and the proportion of oil phase were optimized by a two-factor-five-level central composite experimental design combined with response surface methodology with particle size,ζ potential and solubility as response variables.The optimized formulation was as follows： the proportion of oil phase was 11%,and the mass ratio of Cremophor EL to Labrasol was 1.95.The relative bioavailability of mitothiorole self-microemulsions to its suspension was 436.3%.

关 键 词：米托噻咯 自微乳给药系统 星点设计 效应面法 药动学 

分 类 号：R944.9[医药卫生—药剂学]