单纯形网格法优化外用中药不同油水分配系数多成分微乳制剂处方  

Optimization of multicomponent microemulsion of Chinese materia medica with different oil-water partition coefficients by simplex lattice method

作　　者：徐铃燕 谢远平 康倩[1] 刘葭[1] 孙铭忆 吴清[1] 

机构地区：[1]北京中医药大学中药学院,北京100102

出　　处：《中草药》2017年第19期3961-3969,共9页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金资助项目(81473365);北京中医药大学在读研究生自主选题项目(2017-JYB-XS-078)

摘　　要：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 prepare multicomponent microemulsion of Chinese materia medica（CMM） with different oil-water partition coefficients（log P values） by simplex lattice method and evaluate its quality. Methods The surfactants, cosurfactants and oil phases were screened by saturated solubility method. Ochratins, ligustrazine, ferulic acid, puerarin and geniposide were model drugs to represent the complex components of CMM. Based on the pseudo-ternary diagram, simplex lattice method was adopted to optimize the multicomponent microemulsion of CMM with different log P values by appearance, particle size and polydispersity index as evaluation indexes. The experimental design and model building were constructed by Design Expert 8.06 software to optimize the response surface data analysis and validate the optimal prescription composition. The quality of microemulsion was evaluated by observing appearance and stability as well as measuring particle size and potential. Results The optimum formulation was oleic acid-Labrasol-propylene glycol-water（5.303∶29.336∶7.334∶58.027）. The prepared microemulsion was clear in appearance with good yellowish color and stable property. The average particle size was（118.77 ± 0.37） nm, PDI was 0.282 ± 0.02 and Zeta potential was（0.346 ± 0.05） m V. Conclusion The results indicated that the multicomponent microemulsion of CMM with different log P values is optimized and the drug loading was high. The multicomponents microemulsion of CMM with different log P values（-1.01—3.85） is established and optimized, providing a feasible microemulsion carrier for the multicomponent CMM to simplify its prescription screening work.

关 键 词：单纯形网格法 油水分配系数 多成分微乳 处方优化 质量评价 蛇床子素 川芎嗪 阿魏酸 葛根素 京尼平苷 饱和溶解度法 伪三元相图 

分 类 号：R283.6[医药卫生—中药学]