丹参酮ⅡA自微乳化给药系统的研究

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-PEG 400=10%:45%:45%,载药量2.25 mg/g.丹参酮Ⅱ_A-SMEDDS在0.1 mol/L的稀盐酸溶液中自微乳化时间<1 min,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.

Preparation and evaluation of self-microemulsifying drug delivery systems containing tanshinone II_A

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 diagrams 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-emulsifying 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; ethyl oleate-Labrasol-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-emulsifying performance. It is expected to further stabilize the preparation of tanshinone II A self-microemulsifying agents.