尼莫地平微乳的制备及质量评价  

Preparation of nimodipine microemulsion and its quality evaluation

作　　者：周丽娟[1] 陈曦[1] 刘清飞[1] 王义明[1] 罗国安[1] 

机构地区：[1]清华大学生命科学与医学研究院

出　　处：《中国新药杂志》2008年第13期1145-1149,共5页Chinese Journal of New Drugs

基　　金：国家自然科学基金(30500666);清华大学裕元基金(20240000529,20240000548)

摘　　要：目的:研究尼莫地平微乳的制备和质量评价。方法:考察尼莫地平在不同油相、乳化剂和助乳化剂中的平衡溶解度,并通过滴定法绘制伪三元相图,确定最优的Km值和处方,分别考察载药微乳的外观、稳定性、形态和粒径大小。用高效液相色谱法测定微乳中尼莫地平的包封率和载药量。结果:尼莫地平微乳为澄清或略带乳光的淡黄色液体,稳定,透射电镜下呈圆球形,分布均匀。平均粒径18.2 nm,呈Gauss分布。微乳经0.9%氯化钠注射液和5%葡萄糖注射液稀释50倍后,外观、pH值、载药量、粒径均无明显变化,高效液相色谱法测定包封率为97.62%,载药量为0.402 g.L-1。结论:微乳能提高尼莫地平的溶解度,微乳制剂质量稳定,易于制备。Objective ：To study the preparation of nimodipine-loaded microemulsion and its quality evaluation. Methods：The equilibrium solubility of nimodipine in different compositions of oil,emulsifier and assistant emulsifier was investigated. The optimal Km was determined and nimodipine-loaded microemulsion was prepared by using the method of titration to prepare the pseudo-ternary phase diagram. The appearance, morphology, size distribution,stability of nimodipine microemulsion were determined. The concentration and encapsulated efficiency were determined by HPLC. Results：The nimodipine microemulsion,with good stability,was a translucent diluted-yellow solution with visible sky-blue opalescence. Nimodipine microemulsion in electron microscopy consisted of small spherical drops with a mean diameter of 18.2 nm. The appearance, pH, concentration and particle size of microemulsion were stable after the microemulsion was diluted by 50-folded with sodium chloride injection and glucose injection,respectively. The encapsulated efficiency and the concentration of nimodipine microemulsion were 97.62% and 0. 402 g·L^-1 , respectively. Conclusion ： The solubility of nimodipine was significantly increased in microemulsion and the stability of nimodipine microemulsion was satisfying.

关 键 词：尼莫地平 微乳 伪三元相图 制备 质量评价 

分 类 号：R972.4[医药卫生—药品] R944.9[医药卫生—药学]