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目的采用单纯形网格法优化中药不同油水分配系数(log P值)多成分微乳给药系统,并对其质量进行评价。方法通过饱和溶解度法筛选了表面活性剂、助表面活性剂及油相,并以蛇床子素、川芎嗪、阿魏酸、葛根素及京尼平苷为模型药代表中药复杂成分,在伪三元相图的基础上,应用单纯形网格法优化中药不同油水分配系数多成分微乳,以外观、粒径及多分散指数(PDI)为评价指标,通过Design Expert 8.06软件进行试验设计和模型构建,响应面数据分析优化和验证最佳处方组成。通过对微乳外观、稳定性及其粒径、Zeta电位等的测定对其进行质量评价。结果优化得到的最佳处方为油酸-Labrasol-丙二醇-水(5.303∶29.336∶7.334∶58.027),所形成的微乳外观澄清透明,流动性好,呈淡黄色,平均粒径为(118.77±3.37)nm,PDI为0.282±0.020,Zeta电位为(0.346±0.050)m V,稳定性良好。结论优化之后的中药不同油水分配系数多成分微乳性质稳定,载药量高;制备并优化了适宜于不同logP值(-1.01~3.85)成分的微乳载体,为此范围内的多成分中药提供可行的微乳载体,简化其前期微乳处方筛选工作。
OBJECTIVE To optimize the multi-component microemulsion drug delivery system with different log-value of oil and water by using simplex grid method and evaluate its quality. Methods The surfactant, cosurfactant and oil phase were screened by saturation solubility method. The complex components of traditional Chinese medicine were represented by Osthol, ligustrazine, ferulic acid, puerarin and geniposide, Based on the phase diagram, the simplex grid method was used to optimize the multi-component microemulsion with different oil-water partition coefficients. The appearance, particle size and polydispersity index (PDI) were used as the evaluation indexes. The experimental design and model Build, Respond Surface Data Analysis Optimize and validate the best prescriptions. The quality of microemulsion was evaluated by its appearance, stability, particle size and Zeta potential. Results The optimal formulation was oleic acid-Labrasol-Propylene Glycol-Water (5.303:29.336:7.334:58.027). The formed microemulsion had a clear and transparent appearance, good fluidity and light yellow color with an average diameter of (118.77 ± 3.37) nm, the PDI was 0.282 ± 0.020, the Zeta potential was (0.346 ± 0.050) m V, and the stability was good. Conclusion After optimization, the multi-component microemulsion with different oil-water partition coefficients is stable and the drug loading is high. The microemulsion carrier suitable for different logP values (-1.01 ~ 3.85) is prepared and optimized, and the multi-component traditional Chinese medicine Provide viable microemulsion carriers and simplify pre-microemulsion prescription screening.