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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-emulsification technology was used to make Mitoxillone self-microemulsion delivery system. The two-factor and five-level star design was used. The effects of the main factors influencing the delivery system (such as oil phase ratio, Surfactant mass ratio) to the microemulsion particle size, zeta potential and drug solubility balance as the evaluation index, the establishment of the corresponding mathematical model. The optimized formulation was: oil phase ratio 11%, surfactant ratio Cremophor EL: Labrasol 1.95 (w / w). The oral bioavailability of mitosilol self-microemulsions was 436.3% relative to its suspension.