川芎挥发油自微乳化软胶囊的制备及处方工艺筛选

Preparation of Chuanxiong volatile oil self-microemulsifying drug delivery soft capsules and investigation on drug formulation and process

目的:筛选川芎挥发油自微乳化给药系统的处方工艺并制备自微乳化软胶囊。方法:通过伪三元相图确定O/W自微乳区并筛选出最佳自微乳处方。以乳化时间、色泽和粒径的大小为指标,筛选油相(GTCC)、表面活性剂(聚山梨酯-80)、助表面活性剂(丙二醇)的最佳处方配比,以处方量明胶、甘油、PEG400制备胶囊,考察崩解时间和乳化效果。结果:川芎挥发油自微乳化处方中,载药量5%时川芎挥发油-GTCC-聚山梨酯-80-丙二醇(1∶5∶12∶2)为最佳配比,载药量10%时川芎挥发油-GTCC-聚山梨酯-80-丙二醇(1∶2∶6∶1)为最佳配比,自微乳化时间<1min,澄清且微泛蓝色乳光。结论:不同载药量的川芎挥发油-GTCC-聚山梨酯-80-丙二醇的给药系统存在最佳处方配比,可制备川芎挥发油自微乳化软胶囊。

OBJECTIVE To study the setf-microemulsifying drug delivery system of Chinese traditional medicine Chuanxiong volatile oil, the formulation and the preparation of SMEDDS soft capsules. METHODS Screen out the O/W self-microemulsifying drug delivery domains and choose the best self-microemulsifying drug recipe by ternary phase diagrams. Find the best ratio of oil phase（GTCC）, surfactants（Tween 80） and co-surfactants（1,2-propanediol） based on indexes such as the self emulsifying time, color and luster, particle size. Use glutin, glycerin, PEG 400 as the formulation constituents to prepare soft capsules and evaluate the disintegrating time and emulsifying effect. RFNULTS In the Chuanxiong volatile oil formulation, the best ratios were naphtha： GTCC： Tween 80 ： 1,2-propanediol （ 1 ： 5 ： 12 ： 2） or （ 1 ： 4 ： 12 ： 2）. The self-emulsifying time was less than 1 minute. Its appearance was clear emulsified liquid with blue fluorescence. CONCLUSION There are best self-microemulsifying drug recipe ratios of Chuanxiong volatile oil ：GTCC： Tween 80： 1,2-propanediol, Chuanxiong volatiIe oil SMEDDS soft capsules is prepared.