伊曲康唑自乳化释药系统的处方研究

 目的研究伊曲康唑自乳化给药系统(ITZ-SEDDS)的处方工艺。方法通过溶解度实验?处方配伍和伪三相图的绘制,以自乳化时间?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ITZ-SEDDS的理化性质和体外溶出度进行了测定。结果伊曲康唑自乳化最终优化处方为:Maisine 35-1-Cremophor EL-Transcutol P=25∶30∶45。ITZ-SEDDS的粒径为162.5 nm,自乳化时间<1 min,ITZ-SEDDS在人工肠液中2 h累积溶出百分率为90.9%,是原药(0.52%)的174.8倍,市售胶囊(10.1%)的9.0倍。结论所制备的ITZ-SEDDS达到了设计要求,为ITZ的新制剂开发提供了实验依据。

Study on Itraconazole Self-Emulsifying Drug Delivery System

OBJECTIVE To develop the formulation of self-emulsifying drug delivery system for itraconazole(ITZ-SEDDS).METHODS The optimum formulations of ITZ-SEDDS were screened by solubility experiments,compatibility tests and pseudo-ternary phase diagrams,with the time of formulating emulsion,the consequence of visual examination and particle size as parameters.And the physic-chemical characters and dissolution in vitro of ITZ-SEDDS were also determined.RESULTS The optimum self-emulsifying drug delivery system was composed of Maisine 35-1(25%),Cremophor EL(30%) and Transcutol P(45%).The particle diameter was 162.5 nm,the time of self-microemulsifying was less than 1 min.The percent of accumulated dissolution of itraconazole in SEDDS in simulated intenstinal fluid was up to 90.9% at 2 h,which was 174.8 times as much as that of ITZ crude powder,and 9.0 times as much as that of ITZ capsules.CONCLUSION The formulation of ITZ-SEDDS prepared achieved the requirement of design.It could provide reference for the new dosage form of itraconazole.