蜘蛛香总缬草三酯自微乳的制备及质量评价  

Preparation and Quality Evaluation of Self-microemulsion of Total Valepotriates in Valerianae Jatamansi Rhizoma et Radix

作　　者：刘开萍 程盛勇 郁林娜 罗喜荣 杨军[2] 刘兴赋 尹航 Kai-ping;CHENG Sheng-yong;YU Lin-na;LUO Xi-rong;YANG Jun;LIU Xing-fu;YIN Hang(School of Pharmaceutical Sciences, Guizhou Medical University, Guiyang 550025, China;Institute of Geochemistry, Chinese Academy of Sciences, Guiyang 550081 , China)

机构地区：[1]贵州医科大学药学院,贵阳550025 [2]中国科学院地球化学研究所,贵阳550081

出　　处：《中国实验方剂学杂志》2018年第11期16-21,共6页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：贵州省社发攻关项目(黔科合SY字[2015]3032号);贵州省中药现代化专项项目(黔科合ZY字[2012]3010号);贵州省联合基金项目(黔科合LH字[2014]7091号)

摘　　要：目的：制备蜘蛛香总缬草三酯自微乳并对其质量进行评价,为该有效部位的后续研究与开发提供参考。方法：通过溶解度考察、配伍试验和三元相图法优选处方;以油相、乳化剂及助乳化剂比例为考察因素,粒径、自乳化时间及载药量为评价指标,采用单纯形质心混料设计优化蜘蛛香总缬草三酯自微乳处方并对其药剂学性质进行评价。结果：蜘蛛香总缬草三酯自微乳最佳处方为油酸乙酯-（15-羟基硬脂酸聚乙二醇酯）-二乙二醇单乙基醚（10∶61∶29）;平均粒径38.8 nm,自乳化时间0.57 min,载药量131.23 mg·g^-1,5 min累积溶出度达94.99%;高温及光照会影响该制剂的稳定性,应低温避光保存。结论：蜘蛛香总缬草三酯自微乳制备工艺简单,可显著改善蜘蛛香总缬草三酯的水溶性和溶出度,有望提高其口服生物利用度。Objective： To prepare self-microemulsion of total valepotriates in Valerianae Jatamansi Rhizoma et Radix and evaluate its quality. Method： The prescription was selected by solubility experiment,compatibility test and ternary phase diagram method. Taking rates of oil phase,emulsifier and co-emulsifier as factors,the particle size,self-emulsifying time and drug loading as indexes,simplex centroid mixture design was applied to optimize the prescription of self-microemulsion of total valepotriates in Valerianae Jatamansi Rhizoma et Radix,and the pharmaceutical properties of the self-microemulsion were evaluated. Result： Optimum formulation of the self-microemulsion was 10% of ethyl oleate,61% of polyoxyl 15 hydroxystearate,29% of diethylene glycol monoethyl ether; its average particle size was 38. 8 nm,self-emulsifying time was 0. 57 min,and drug loading was 131. 23 mg·g^-1 in the optimal prescription,cumulative dissolution at 5 min was 94. 99%. Self-microemulsion of total valepotriates in Valerianae Jatamansi Rhizoma et Radix was affected by high temperature and illumination,indicating it should be stored at low temperature and avoid light. Conclusion： The preparation technology of this self-microemulsion is simple, it can significantly improve the solubility, bioavailability and dissolution of total valepotriates in Valerianae Jatamansi Rhizoma et Radix.

关 键 词：蜘蛛香 总缬草三酯 抗抑郁 镇静催眠 自微乳 三元相图 单纯形质心混料设计 

分 类 号：R22[医药卫生—中医基础理论] R289[医药卫生—中医学]