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目的优选丹参酮ⅡA自微乳化给药系统(丹参酮ⅡA-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ⅡA-SMEDDS的处方组成:油酸乙酯-Labrasol-PEG400=10%∶45%∶45%,载药量2.25mg/g。丹参酮ⅡA-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ⅡA—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ⅡA自微乳化制剂。
Objective To optimize the formulation of tanshinone ⅡA self-microemulsifying drug delivery system (tanshinone ⅡA-SMEDDS) and to evaluate its quality. Methods The pseudo-ternary phase diagram was used as a guide to investigate the ability and area of drugs and different emulsifying agents and emulsions to form oil emulsion. The phase diagrams of different prescriptions were drawn. On the basis of this, the prescription composition was optimized and the self-emulsifying time , Droplet morphology, particle size distribution, ζ-potential, stability and other aspects of quality evaluation. Results The formulation of tanshinone ⅡA-SMEDDS was determined as follows: ethyl oleate-Labrasol-PEG400 = 10%: 45%: 45%, drug loading 2.25 mg / g. Tanshinone Ⅱ A-SMEDDS was self-microemulsified in 0.1mol / L dilute hydrochloric acid solution for less than 1min, and its particle size was smaller than normal (mean diameter was (84.9 ± 2.1) nm, n = 3) , The stability was good, and the average ζ-potential of the three batches was (-24.0 ± 1.15) mV (n = 3). Conclusion Tanshinone ⅡA-SMEDDS has good self-emulsifying properties and is expected to be used in further preparation of tanshinone ⅡA self-microemulsifying preparation with stable quality.