穗花杉双黄酮自微乳化给药系统的制备及体外评价  

Preparation and in vitro Evaluation of Self-Microemulsifying Drug Delivery System Containing Amentoflavone

作　　者：任秋霞[1,2] 王亚男[1,2] 曲新艳[2] 郑冰清 洪婷[2] 周喆[2] 

机构地区：[1]天津中医药大学,天津300193 [2]军事医学科学院放射与辐射医学研究所,北京100850

出　　处：《中国实验方剂学杂志》2013年第24期5-9,共5页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：国家自然科学基金项目(81172981)

摘　　要：目的:制备穗花杉双黄酮自微乳化给药系统并对其进行质量评价。方法:通过溶解度试验、处方配伍试验及绘制伪三元相图筛选辅料种类及用量,通过比较不同处方自微乳外观、粒径及乳化时间优选处方工艺,确定穗花杉双黄酮自微乳载药量并评价其体外释放情况和稳定性。结果:穗花杉双黄酮自微乳最佳处方为m穗花杉双黄酮∶m聚氧乙烯蓖麻油∶m油酸乙酯∶m1,2-丙二醇=5.0∶47.5∶19.0∶28.5,乳滴呈圆球性,粒径(15.37±0.09)nm,Zeta电位(-17.1±0.24)mV,在不同pH介质中自微乳制剂均能快速完全释放药物。结论:穗花杉双黄酮自微乳可显著提高穗花杉双黄酮的体外溶出度,且制备工艺简单、性质稳定。Objective： To develop a self-microemulsifying drug delivery system （SMEDDS） for amentoflavone （AMF） and evaluate its quality. Method： The amount and type of excipients was screened by solubility test,compatibility of oil and surfactant and pseudo-ternary phase diagram,formulation technology of AMF-SMEDDS was optimized by comparing appearance,particle size,self-microemulsifying time and drug loading of different prescriptions,then physicochemical characteristics,in vitro release and stability of AMF-SMEDDS were determined. Result： The best prescription of AMF-SMEDDS was as following：mAMF：mcremophor EL-35：methyl oleate：m1,2-propanediol（5.0：47.5：19.0：28.5）;After being diluted with water,AMF-SMEDDS consisted of small spherical droplets with the mean particle size of （15.37±0.09） nm and Zeta potential of （-17.1±0.24） mV,microemulsion could quickly complete release of AMF at different pH medium. Conclusion： AMF-SMEDDS could significantly improve in vitro dissolution of AMF,and its preparation technology was stable and simple.

关 键 词：穗花杉双黄酮 自微乳化给药系统 伪三元相图 稳定性试验 体外释放曲线 载药量 

分 类 号：R283.6[医药卫生—中药学] R943[医药卫生—中医学]