20(S)-原人参二醇自微乳释药系统的处方优化和有效期预测  

Prescription Optimization and Expiration Term Prediction of 20(S)-Protopanaxadiol Self-microemulsion Drug Delivery System

作　　者：王冰[1] 浦益琼[1] 徐本亮[1] 张彤[1] 陶建生[1] 

机构地区：[1]上海中医药大学,上海201203

出　　处：《中国实验方剂学杂志》2016年第22期1-6,共6页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：国家自然科学基金项目(81303233)

摘　　要：目的:优化20(S)-原人参二醇自微乳释药系统处方并预测其有效期。方法:以油相中油酸质量分数、油相比例、乳化剂与助乳化剂比值为自变量,载药量,粒径,Zeta电位和优选10 min时药物溶出度为因变量,采用星点设计-效应面法优选20(S)-原人参二醇自微乳的处方组成;利用单因素试验优选制备工艺;通过Q10法在较高温度下进行加速试验,预测该制剂的有效期。结果:自微乳的最佳处方为油相中油酸质量分数84.09%,油相比例30%,乳化剂-助乳化剂(2.58∶1);载药量102.22mg·g-1,粒径39.67 nm,Zeta电位-13.1 m V,10 min时药物溶出度75.01%。制备工艺参数为混合方式为磁力搅拌,混合速度400 r·min-1,混合时间30 min,混合温度45℃。Q10法预测自微乳的室温贮存有效期约1.51年。结论:优选的制剂处方合理、工艺可行、样品稳定性良好,可为20(S)-原人参二醇的新型制剂探索提供研究数据。Objective： To optimize prescription of 20（S）-protopanaxadiol self-microemulsifying drug delivery system（PPD-SMEDDS） and predict its expiration term. Method： Ratio of oleic acid in oil phase,ratio of oil phase and ratio of emulsifier to co-emulsifier were selected as independent variables. Drug loading,particle size,Zeta-potential and dissolution of PPD in 10 min were set as dependent variables. Central composite designresponse surface methodology was applied to optimize prescription of PPD-SMEDDS, and then its preparation technology was investigated by single factor tests. Q10 method was adopted to predict the expiration term by the accelerated test at high temperature. Result： Optimal prescription was as following,ratio of oleic acid in oil phase was 84. 09%,ratio of oil phase was 30%,ratio of emulsifier to co-emulsifier was 2. 58∶1. Under these conditions,drug loading was 102. 22 mg·g- 1,the particle size was 39. 67 nm,the Zeta potential was- 13. 1 m V,dissolution of PPD in 10 min was 75. 01%. The process parameters were determined as： magnetic stirring,the mixing speed of 400 r·min- 1,the mixing time of 30 min,the mixing temperature of 45 ℃. The expiration term at room temperature of PPD-SMEDDS was about 1. 51 years by Q10 method. Conclusion： These optimized processes are stable and feasible with good stability of samples,which can provide some research data for the new preparations exploration of PPD.

关 键 词：20(S)-原人参二醇 自微乳释药系统 有效期 载药量 粒径 油酸 

分 类 号：R283.6[医药卫生—中药学] R284.1[医药卫生—中医学]