文档介绍：效应面法优化甲巯咪唑聚乳酸
【关键词】重叠等高线图
摘要:目的优化甲巯咪唑聚乳酸羟基乙酸共聚物微球的处方工艺。方法采用O/O型乳化溶剂挥发法制备微球,通过Draper/lin小中心复合因子设计试验考察药物和PLGA的重量比、PLGA在内相的浓度、司盘-80在外相的浓度3个影响因子对微球的包封率、载药量和粒径的影响。根据最佳数学模型绘制效应面,通过重叠等高线图确定最优处方工艺。结果 3个影响因素和3个考察指标之间存在定量关系,∶1,PLGA的浓度为40%,司盘的浓度为5%。优化处方各指标的预测值和目标值非常接近。结论采用因子设计-效应面法完成了甲巯咪唑微球的多目标同步优化。
关键词:甲巯咪唑;微球;O/O型乳化溶剂挥发法;效应面法;重叠等高线图
Abstract: Objective To optimize the formulation of methimazoleloaded oglycolic acid (PLGA) microspheres. Methods Methimazoleloaded PLGA microspheres were prepared by the oilinoil emulsion solvent evaporation technique. Three factors,including the weight ratio of drug to PLGA,PLGA concentration in internal phase and the emulsifier (Span 80) concentration in external phase,were known to be associated with the quality of the microspheres. A posite design (Draper/Lin method) was used to investigate the effects of the three factors on encapsulation efficiency,drug loading and size distribution. Response surface and overlay contour plot were delineated according to the bestfit mathematic models. Optimum formulation was selected by overlay contour plot. Results The quantitative relationships between the three factors and three responses were obtained. The variables were optimized and the following processing conditions resulted in the highest drug loading and best yields of the microspheres: the weight ratio of drug to PLGA was :1