伊曲康唑自乳化释药系统的处方研究

Study on Itraconazole Self-Emulsifying Drug Delivery System

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。

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 panicle size as parameters. And the physic-chemical characters and dissolution in vitro of ITZ-SEDDS were also determined. RESULTS The optimum selfemulsifying drug delivery system was composed of Maisine 35-1 （25%） , Cremophor EL （30%） and Transcutol P（45% ）. The panicle 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.