目的研究山楂叶总黄酮自微乳化释药系统的处方工艺。方法通过溶解度、处方配伍试验和伪三元相图的绘制,以色泽、乳化时间和乳化后粒径大小为指标,筛选油相、表面活性剂、助表面活性剂的最佳配伍和处方配比。并以益心酮片为参比,测定山楂叶总黄酮自微乳化释药系统的溶出度。结果山楂叶的自微乳化处方中油相为乳化剂为Labrasol(35%),助乳化剂为Transcutol P(10%)。自微乳化后的粒径为(39.5±5.4)nm,自微乳化时间小于1min。蒸馏水中10min累积溶出度达70%以上,而益心酮片60min的溶出度不足50%。结论所制备的山楂叶总黄酮自微乳化释药系统达到了设计要求,为山楂叶总黄酮新制剂开发提供了依据。

Objective To develop the formulation of self-microemulsifying drug delivery system forhawthorn leaves flavonoids(HAW-SMEDDS).Methods The optimum formulations of oil phase,surfac-rant,and assistant surfactant for HAW-SMEDDS were screened by solubility test,compatibility test,andpseudo-ternary phase diagrams,with the time of formulating microemulsion,the consequence of visual ex-amination,and particle size as indexes.The dissolution of HAW-SMEDDS was measured.taking the tom-mercial tablet Yixintong Tablet as reference.Results The optimum self-microemulsifying drug deliverysystem was composed of Labrasol(35％),Transcutol P(10％).The particle diameter was(39.5±5.4)nm.the time of self-microemulsifying was less than 1 min.The percent of accumulated dissolution of hawthorn leaves flavonoids in SMEDDS in distilled water was up to 70％at 10 min,while that in theYixintong Tablet was less than 50％at 60 min.Conclusion The formulation of HAW-SMEDDS prepara-tion could meet the request of the design.It could provide the reference for the new dosage form.

广东省科技计划项目(2007B060401058)