星点设计-效应面法优化蒿甲醚自微乳释药系统

目的：研究蒿甲醚自微乳释药系统（SMEDDS）的制备优化及体外评价。方法通过溶解度实验、伪三元相图的绘制及星点设计-效应面法，以粒径、Zeta电位和平衡溶解度为指标，筛选最优处方，并对蒿甲醚自微乳的理化性质和体外释药进行评价。结果蒿甲醚自微乳最优处方为：Cremophor RH40为39.29%、Transcutol HP为35.71%、MCT为25%；其平均粒径为24.52 nm，Zeta电位为-10.10 mV，平衡溶解度＞88 mg/g。结论应用星点设计-效应面优化法得到蒿甲醚SMEDDS的最优处方，显著提高蒿甲醚的溶解度和体外溶出度。

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

Objective To optimize and assess the formulation of self-microemulsifying drug delivery systems(SMEDDS)for artemether(ARM). Methods The optimized formulation of ARM-SMEDDS was screened by solubility,ternary phase diagram and cen?tral composite design-response surface methodology,with the particle size,Zeta potential and solubility as parameters. The physico-chemical property and dissolution characters of ARM-SMEDDS were also determined. Results The optimized SMEDDS was composed of Cremophor RH40(39.29%),Transcutol HP(35.71%)and MCT(25%). The average particle size after the emulsification was 24.52 nm,the Zeta potential was-10.10 mV,and the drug loading of self-microemulsifying exceeded 88 mg/g. Conclusion The opti?mized formulation of ARM-SMEDDS using the star point design-response surface methodology has significantly enhanced the solubility and in vitro dissolution of ARM.