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%.