复方痛痹舒自微乳释药系统基质组成的研究

Study on composition of substrate from Compound Tongbishu self-microemulsifying drug delivery system

目的筛选复方痛痹舒自微乳释药系统(SMEDDS)的基质组成并确定配方比例。方法采用溶解度方法测定复方痛痹舒中主要有效成分在不同油相、乳化剂和助乳化剂中的溶解度,结合不同油相与乳化剂的配伍结果,筛选油相、乳化剂与助乳化剂,采用水滴定法绘制伪三元相图,以澄清度、粒径和自乳化时间为考察指标,筛定油相、乳化剂和助乳化剂的类型及其组成范围。结果复方痛痹舒SMEDDS基质组成:油相为肉豆蔻酸异丙酯(IPM),乳化剂为RH40/聚山梨酯-80(1∶1),助乳化剂为甘油;各相系占SMEDDS基质组成的比例范围按质量分数计:油相9.96%~40.49%,乳化剂23.31%~59.97%,助乳化剂19.83%~60.02%。结论筛定的复方痛痹舒SMEDDS基质,其分散相粒径可以达到10~100 nm,为进一步研究奠定基础。

Objective To initially screen the composition of the substrate from Compound Tongbishu self-microemulsion system（SMEDDS） and define the proportional range. Methods The solubility of main active ingredients in different oil phases, surfactants, and cosurfactants was determined by the solubility method. Combined with the result of different oil phases and emulsifier compatibility experiment, several relatively good oil phases, emulsifiers, and co-emulsifiers were selected. The pseudo-ternary phase diagram was drawn by water titration. The transparency, particle size, and self-emulsification time were used as the indexes to preferably select the optimum oil phase, emulsifier and co-emulsifier and to determine the compositional range of each composition. Results The optimal composition of substrate from Compound Tongbishu SMEDDS was as follows： Oil phase was isopropyl myristate（IPM）, emulsifier was RH40/Tween-80（1∶1）, and co-emulsifier was glycerol. The proportion of self-microemulsion matrix was calculated from the mass percentage： oil phase of 9.96%—40.49%, emulsifier of 23.31%—59.97%, and co-emulsifier of 19.83%—60.02%. Conclusion The dispersed particle size can reach 10—100 nm using the substrate from Compound Tongbishu SMEDDS that is screened and determined, which establishes the foundation for further research.