交泰丸有效部位自微乳化释药系统的处方设计

Self-microemulsifying drug delivery system formulation optimization design of effective fraction of Jiaotai Pill

目的:研究交泰丸(黄连、肉桂)有效部位自微乳化释药系统的处方工艺。方法:通过溶解度实验、乳化剂的选择、伪三元相图的绘制、处方比例的优化,以所形成自乳剂外观、乳化后乳剂的外观、自乳化时间为指标筛选最佳处方;通过药物在不同温度的溶解情况确定载药量。结果:最优处方为辛酸/葵酸甘油三酯-CremophorRH40-丙二醇-黄连总碱-肉桂油(以桂皮醛含量计)(20∶50∶30∶3∶0.6)。结论:交泰丸有效部位自微乳对药物增溶作用明显,制备方法简单。

AIM： To explore the formulation design and quality evaluation of self-microemulsifying drug delivery system （SMEDDS） from the effective constituents of Jiaotai Pill（Rhizoma Coptidis,Cortex Cinnamomi）. METHODS： The self-microemulsion formulation of effective constituents of Jiaotai Pill was optimized based on its solubility in various kinds of oils,and the self-microemulsifying efficiency of various combinations of emulsifier and co-emulsifer was evaluated using the pseudo-ternary phase diagrams. The appearance,particle size in the selfemulsifying system,and the emulsifying speed were examined. RESULTS： The optimum formulations of Jiaotai Pill SMEDDS were composed of caprylic acid/capric triglyceride,Cremophor RH40,propanediol,Coptis total alkaloids,and cinnamon oil at the ratio of 20 ∶ 50 ∶ 30 ∶ 3 ∶ 0. 6,calculated as cinnamyl aldehyde. CONCLUSION： The solubility of effective fraction of Jiaotai Pill is significantly increased in self-emulsifying system and the formulation is stable and easy to prepare.