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 0h及 10h小粒径 (小于 0 .15 μm)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 80∶(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 .4mg/ml,采用乙醇滴加 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 18.9nm。结论
AIM:To optimize the preparation and formulation of nimodipine containing nanoliposome. METHOD:Orthogonal design was adopted to screen the preparation and formulation of nimodipine containing nanoliposome on the basis of the comprehensive score of the entrapment efficiency of reconstitution, utilization ratio of nimodipine, percentages of nimodipine entrapped in the liposomes (below 0.15 μm) 0 h and 10 h after reconstitution, leaking percentage and particle size of the reconstituted nanoliposomes. RESULT:The ideal combination of preparation and formulation is nimodipine∶(egg lecithin+cholesterol)=1∶40; sodium deoxycholate∶(egg lecithin+cholesterol)=1∶4; Tween 80∶(egg lecithin+cholesterol)=1∶4; weight percentage of mannitol within the formulation is 65%, using specified volume of distilled water as hydrating medium, and preparing by ethanol dripping ultrasonic technique. The average 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 nimodipine containing nanoliposome are satisfactory.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2003年第1期25-28,共4页
Journal of China Pharmaceutical University
