尼莫地平自微乳化释药系统处方优化  

Development of the formulation of self-microemulsifying drug delivery system of nimodipine

作　　者：杨茜[1] 张邦乐[1] 滕增辉[1] 宦梦蕾[1] 刘仁旺[1] 周四元[1] 

机构地区：[1]第四军医大学药学系药理学教研室,陕西西安710032

出　　处：《现代生物医学进展》2008年第5期920-923,共4页Progress in Modern Biomedicine

摘　　要：目的:制备尼莫地平的自微乳化释药系统。方法:通过溶解度实验筛选各种辅料,按照处方设计制得系列自微乳化液,并通过体外评价以确定最优处方。结果:最优处方为尼莫地平、聚氧乙烯氢化蓖麻油-35、油酸乙酯和单辛酸甘油酯的质量百分数分别为3.5%、40%、40%和16.5%。在0.1 mol oL^(-1)稀盐酸中轻微搅拌,该优化处方能够在1min内迅速乳化,得到粒径均值58.6nm的乳滴,1min时的溶出率为84.3%。结论:按优化处方制得的尼莫地平自微乳化释药系统显著提高了尼莫地平的溶出。Objective： To prepare a self-microemulsifying drug delivery system （SMEDDS） of nimodipine, Methods： The adjuvants were screened out by the solubility of nimodipine in them. The SEDDS was prepared according to the experiment design and evaluated in vitro to optimize its formulation. Results： The ratios （%） of nimodipine, Cremophor EL, ethyl oleate and GMC in the optimized formulation were 3.5 %, 40 %, 40 % and 16.5 % respectively, The optimized formulation was emulsified rapidly within 1 min after stirred in the 0.1 mol oL^-1 HCl. The average size of emulsion drops was 58nm. The dissolution rate of the optimized formulation was 84.3% at 1 min. Conclusions： The present study revealed that the optimized formulation of self-microemulsifying drug delivery systems of nimodipine can greatly enhance the dissolution rate of nimodipine in the medium.

关 键 词：尼莫地平 自微乳化释药系统 体外评价 

分 类 号：R944[医药卫生—药剂学] R944.9[医药卫生—药学]