星点设计-效应面法优化依托泊苷自微乳化释药系统

目的 研制稳定的依托泊苷自微乳制剂并评价其质量.方法 通过溶解度试验、处方配比、三元相图的绘制及星点设计-效应面法的优化,以粒径、溶解度和zeta电位为指标,筛选各组分的最佳组合和处方配比,并对依托泊苷自微乳的理化性质和体外溶出进行测定.结果 依托泊苷自微乳最佳处方为:依托泊苷(2.0％)、Capryol 90(15.1％)、Cremophor RH40(30.4％)、Transcutol HP(52.5％),平均粒径为18.31 nm,自乳化时间＜1min,乳化后载药量＞ 25 mg· mL-1.结论 制备的依托泊苷自微乳稳定性好,载药量高.

Optimization of etoposide self-microemulsifying drug delivery system by central composite design-response surface methodology

Objective To develop the stable formulation of etoposide self-microemulsifying system and evaluate its quality.Methods The optimum formulations of etoposide SMEDDS were screened by solubility,compatibility tests,tertiary phase diagrams and central composite design-response surface methodology,with the particle size,solubility and zeta electric potential as parameters.The physic-chemical property and dissolution characters of etoposide SMEDDS were also determined.Results The optimum self-microemulsifying drug delivery system was composed of etoposide(2.0%),Capryol 90(15.1%),Cremophor RH40(30.4%),and Transcutol HP(52.5%).The mean particle diameter after the emulsification was 18.31 nm,the self-microemulsifying time was less than 1 min,and the drug loading of emulsifying exceeded 25 mg · mL-1.Conclusion The prepared etoposide SMEDDS is stable with good drug loading.