止痛微乳制剂制备与处方优化

Preparation and optimization of Zhitong micro-emulsion formula

该实验以临床经验方止痛方为模型药,以方中挥发油部分作为油相,水煎液作为水相制备了止痛微乳。实验考察了表面活性剂和助表面活性剂的种类,利用微乳电导率变化与其构型改变相关的特点,绘制了微乳体系水的百分量与电导率变化的曲线和微乳精细伪三元相图,确定了表面活性剂和助表面活性剂质量比K m。之后利用设计中的D-混料设计,以微乳粒径和表面还张力为考察指标优化了止痛微乳处方,最后测定了止痛微乳的部分理化参数,并初步考察了微乳的稳定性。结果显示止痛微乳的表面活性剂以EL-35与聚氧乙烯失水山梨醇单月桂酸酯按4∶1复配的效果最好,而助表面活性剂选择无水乙醇效果,表面活性剂与助表面活性剂比例即K m为1.5,最终确定的微乳处方是12%表面活性剂,8%助表面活性剂,70%的1 g·mL-1水煎液和8%油,之后初步稳定性实验显示止痛微乳稳定性较好。

To prepare Zhitong micro-emulsion in this study, with the empirical formula of Zhitong preparation as the model medicine, the essential oil in the formula as the oil phase, and the water decoction as the water phase. The types of surfactant and co- surfactant were investigated. The changes in micro-emulsion conductivity and construction, the water percentage in the micro-emulsion system, the changing curve of conductivity and the fine pseudo-ternary phase diagram of micro-emulsion were drawn to determine the surfactant-co-surfactant mass ratio（Km ）. Subsequently, the D-mixture design was used to optimize Zhitong Micro-emulsion formula, with particle size and surface tension of micro-emulsion as the indexes. Finally, efforts were made to determine part of physical parame- ters of Zhitong micro-emulsion and preliminarily detect its stability. The results showed that the micro-emulsion was optimal with the EL-35-tween 20 ratio of 4：1 in surfactant, whereas the absolute ethyl alcohol was recommended as the co-surfactant. The ratio between surfactant and co-surfactant （Km ） was 1.5. The finalized micro-emulsion formula contains 12% surfaetant, 8% co-surfactant, 70% 1 g · mL^-1 water decoction and 8% oil. The results of the preliminary stability experiment showed a better stability of Zhitong micro- emulsion.