长春西汀自微乳化给药系统的制备与体外评价  

Preparation of self-microemulsifying drug delivery system (SMEDDS) of vinpocetine and in vitro evaluation

作　　者：崔淑霞[1] 聂淑芳[1] 张世忠[1] 徐昕[1] 周晓堂[1] 潘卫三[1] 

机构地区：[1]沈阳药科大学药学院,沈阳110016

出　　处：《中国新药杂志》2009年第19期1897-1901,共5页Chinese Journal of New Drugs

基　　金：国家重点基础研究发展计划(973计划)(2009CB930300)

摘　　要：目的:制备长春西汀自微乳化给药系统,并对其体外释药及初步稳定性进行了评价。方法:通过溶解度实验、相分离实验以及三元相图的研究筛选了长春西汀自微乳化处方;并对制剂进行了粒径分布、溶出度及初步稳定性的考察。结果:长春西汀自微乳处方组成:Solutol HS 15(A)为表面活性剂;Transcutol P(B)为辅助表面活性剂;Ethyl Oleate(C)为油相。所得处方的自微乳化时间<1 min,粒径<100 nm。体外释放实验表明自微乳化制剂受溶出介质pH值影响小,在不同pH值非依赖型介质中均能快速完全释放药物。结论:所制备的长春西汀自微乳化制剂能够显著提高难溶性药物的溶解度,为体内研究提供实验依据。Objective：To develop a SMEDDS for vinpocetine and to assess the drug release behavior in vitro and primary stability. Methods ：The formula of vinpocetine SMEDDS was optimized on the basis of the solubility in various vehicles, compatibility of various oils with surfactants,and the self-microemulsification regions were identified with ternary phase diagrams. The particle size and dissolution of optimal formulation were determined. The dosage form was a suitable delivery system for vinpocetine. Results：In the optimal vinpocetine SMEDDS, Solutol HS 15,Transcutol P and Ethyl Oleate were selected as surfactant, co-surfactant and oil, respectively. And the dissolution release of vinpocetine was rapid, complete, not influenced by the pH of dissolution medium. Conclusion：The solubility of vinpocetine was highly enhanced by the formulation of SMEDDS, and further investigations were warranted.

关 键 词：长春西汀 自徽乳化药物传递系统(SMEDDS) 三元相图 体外评价 初步稳定性 

分 类 号：R943.4[医药卫生—药剂学] R971.7[医药卫生—药学]