尼莫地平纳米脂质体制备工艺及处方优化研究  

Study on Optimize the Preparation and Formulation of Mimodipine-Containing Nanoliposome

作　　者：赵若威[1] 王强[1] 刘立恒[1] 樊荣[1] 

机构地区：[1]哈尔滨医科大学第二临床医学院药学药物研究所,黑龙江哈尔滨150086

出　　处：《黑龙江医学》2006年第11期817-820,共4页Heilongjiang Medical Journal

摘　　要：目的优化制备尼莫地平纳米脂质体的工艺和处方。方法采用正交设计法,以尼莫地平脂质体冻干粉重建包封率、药物利用率、重建后0 h及10 h小粒径(<0.15μm)脂质体包封药物的百分率、粒径分布、泄漏率等多个指标综合评分,优化尼莫地平脂质体的处方和工艺。结果尼莫地平脂质体的最佳工艺处方为:药物:(磷脂+胆固醇)为1:40;胆固醇:磷脂为1:6;去氧胆酸钠:(磷脂+胆固醇)为1:4;吐温280:(磷脂+胆固醇)为1:4;冻干保护剂甘露醇的用量为处方总重的65%,水合介质为注射用蒸馏水,制备浓度为0.4 mg/mL,采用乙醇滴加2超声工艺制备,按该处方工艺组合制备3批脂质体,包封率平均为92.8%,平均粒径为18.9 nm。结论按优化处方制得的尼莫地平纳米脂质体的包封率和粒径均令人满意。Objective To optimize the preparation and formulation of nimodipine 2 containing nanoliposome. Methods Orthogonal design was adopted to screen the preparation and formulation of nimodipine 2 containing nanolipo 2 some on the basis of the comprehensive score of the entrapment efficiency of reconstitution, utilization ratio of nimodip2ine, percentages of nimodipine entrapped in the liposomes （below 0.15μm） 0 h and 10 h after reconstitution, leakingpercentage and particle size of the reconstituted nanoliposomes. Results The ideal combination of preparation and formulation is nimodipine： （ egg lecithin ＋ cholesterol） = 1 ： 40; sodium deoxycholate： （ egg lecithin ＋ cholesterol） = 1 ： 4; Tween280： （ egg lecithin ＋ cholesterol） = 1：4; weight percentage of mannitol within the formulation is 65%, usingspecified volume of distilled water as hydrating medium, and preparing by ethanol dripping2ultrasonic technique. Theaverage entrapment efficiency of the optimized nanoliposome is 92.8%, and the average particle size is 18.9 nm. Conclusion The entrapment efficiency and particle size of the optimized nimodipine2containing nanoliposome are satisfactory.

关 键 词：尼莫地平 纳米脂质体 正交设计 

分 类 号：R96[医药卫生—药理学]