目的研究长春西汀自微乳化给药系统(VIN-SMEDDS)的处方工艺。方法通过溶解度实验、处方配伍实验和伪三相图的绘制,以乳化时间、色泽和粒径的大小为指标,筛选油相、表面活性剂、助表面活性剂的最佳搭配和处方配比。并对VIN-SMEDDS的理化性质和体外溶出度进行了测定。结果长春西汀的自微乳化处方中油相为GTCC(55%)、油酸(5%),乳化剂为Cremophor EL(30%),助乳化剂为Transcutol P(10%)。VIN-SMEDDS的粒径为(40.16±5.58)nm,自微乳化时间<1min,人工肠液中2h累积溶出百分率为90.01%,是原料药(11.07%)的8.1倍。结论所制备的VIN-SMEDDS达到了设计要求,为VIN的新制剂开发提供了依据。

OBJECTIVE To develop the formulation of self-microemulsifying drug delivery system for vinpocetine(VIN-SMEDDS). METHODS The optimum formulations of VIN-SMEDDS were screened by solubility experiments, compatibility tests and pseudo-ternary phase diagrams,with the time of formulating microemulsion, the consequence of visual examination and particle size as parameters. And the physic-chemical characters and dissolution in vitro of VIN-SMEDDS were also determined.RESULTS The optimum self-microemulsifying drug delivery system was composed of GTCC(55%), oil acid(5%),Cremophor EL(30%), Transcutol P(10%).The particle diameter was (40.16±5.58) nm, the time of self-microemulsifying was less than 1 min. The percent of accumulated dissolution of vinpocetine in SMEDDS in simulated intenstinal fluid was at 2 h up to 90.01%,which was 8.1 times as much as that of VIN raw powder(11.07%).CONCLUSION The formulation of VIN-SMEDDS preparation achieves the request of design. It can provide reference for the new dosage form.