目的 研究川芎嗪微乳递药系统的制备工艺，对其物理药剂学性质进行评价；以不同油相制备不同粒径大小的微乳，考察粒径因素对制剂释药行为的影响。方法 以川芎嗪溶解度为指标，筛选油相、乳化剂、助乳化剂；采用伪三元相图法对微乳处方进行优化；采用超滤离心法对载药量、包封率进行研究；采用马尔文粒径仪对粒径、电位进行检测；采用透析袋法对不同粒径微乳的释药行为进行对比研究。结果 成功制备了川芎嗪微乳，外观澄清透明，pH均值约为5.46；成功建立了微乳包封率的检测方法；川芎嗪载药量为1.2 mg/mL时，包封率为（87.43±0.20）%。通过改变油相（油酸乙酯、油酸、IPM）制备不同粒径的微乳，当载药量为1.2 mg/mL时3者的粒径分别为（16.80±0.91）、（129.50±1.21）、（18.51±0.24）nm。释放实验显示，在4 h内3者释放率均能达到90%以上，无显著性差异。结论 成功制备了均一、稳定的川芎嗪微乳；不同粒径川芎嗪微乳的释药行为不受粒径因素的影响。

Objective To study the preparation process of ligustrazine microemulsion delivery system and evaluate its physical pharmacy properties; Microemulsions of different particle sizes were prepared in different oil phases, and the effect of particle size factors on the release behavior of the preparation was investigated. Methods Taking the solubility of ligustrazine as index, the oil phase, emulsifier, and co-emulsifier were screened. The microemulsion formulation was optimized by pseudo-ternary phase diagram method. The encapsulation efficiency and drug loading was studied by ultrafiltration centrifugation. The particle size and potential were detected by the particle size analyzer. The release behavior of microemulsions with different particle sizes was compared by dialysis bag method. Results The tetramethylpyrazine microemulsion was successfully prepared, and the appearance was clear and transparent. The average pH value was about 5.46. The detection method of microemulsion encapsulation rate was successfully established. When the drug loading of ligustrazine was 1.2 mg/mL, the encapsulation efficiency was (87.43 ±0.20)%. The microemulsions of different particle sizes were prepared by changing the oil phase (ethyl oleate, oleic acid, and IPM). When the drug loading was 1.2 mg/mL, the three particle sizes were (16.80 ±0.91), (129.50 ±1.21), and (18.51 ±0.24) nm, respectively. The release test showed that the release rate of all three could reach more than 90% within 4 h, and there was no significant difference. Conclusion The uniform and stable tetramethylpyrazine microemulsion is successfully prepared; The release behavior of different tetramethylpyrazine microemulsions is not affected by the particle size factor.

国家自然科学基金项目（81803738）；中央高校基本科研业务费专项资金资助（2018-JYBZZ-JS019）；北京中医药大学自主课题项目（2019-JYB-XS-068）