目的 优选丹参酮Ⅱ_A自微乳化给药系统(丹参酮Ⅱ_A-SMEDDS)的处方,并对其进行初步的质量评价。方法 以伪三元相图为指导考察药物与不同乳化剂、油相形成乳剂的能力和区域,绘制不同处方组成的相图,在此基础上优化处方组成,并对优化处方进行了自乳化时间、乳滴形态、粒径分布、ζ-电位、稳定性等方面的质量评价。结果 确定丹参酮Ⅱ_A-SMEDDS的处方组成:油酸乙酯-Labrasol-PEG400=10%:45%:45%,载药量2.25mg/g。丹参酮Ⅱ_A-SMEDDS在0.1mol/L的稀盐酸溶液中自微乳化时间<1min,粒径较小呈正态分布[平均粒径为(84.9±2.1)nm,n=3],形态较圆整,稳定性良好,3批制剂的平均ζ-电位为(-24.0±1.15)mV(n=3)。结论 制备的丹参酮Ⅱ_A—SMEDDS具备良好的自乳化性能,有望进一步制备质量稳定的丹参酮Ⅱ_A自微乳化制剂。

Objective To optimize the formulation of self-microemulsifying drug delivery systems containing tanshinone Ⅱ_A (tanshinone Ⅱ_A SMEDDS) and assess the quality of tanshinone Ⅱ_A SMEDDS.Methods Pseudoternary phase diag rams were used to choose the oil,emulsifier,co-emulsifier,and their proportion in the formulation on the basis of the ability to form emulsions and regions.Then the self-emul-sifying time,droplet and morphology,size distribution,ζ-potential,stability,and other aspects of the quality were evaluated.Results The formulation of tanshinone Ⅱ_A-SMEDDS was as follows:ethyloleate-Labraso-PEG 400= 10%:45%:45%,drug loading ratio was 2.25 mg/g.The self microemulsifying time of tanshinone Ⅱ_A-SMEDDS in 0.1 mol/L hydrochloric acid solution was less than 1 min,the emulsion drops were spherical shape with average particle size of (84.9 ±2.1) nm and the average ζ-potential (-24.0 ± 1.15) mV (n= 3) So tanshinone Ⅱ_A-SMEDDS was stable.Conclusion In this paper,the tanshinone Ⅱ_A-SMEDDS has a good self-emulsify ing performance.It is expected to further stabilize the preparation of tanshinone Ⅱ_A self-microemulsifying agents.

浙江省教育厅青年教师资助计划;浙江中医药大学资助项目(17105012)