尼莫地平前体脂质体的制备及其质量评价  

Preparation of proliposome nimodipine and quality evaluation

作　　者：王志宣[1] 邓英杰[1] 张晓鹏[1] 杨静文[1] 王娜[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2006年第11期681-685,共5页Journal of Shenyang Pharmaceutical University

摘　　要：目的制备尼莫地平前体脂质体,并进行质量评价,以期得到高效、低毒和稳定的尼莫地平新剂型。方法采用叔丁醇-水共溶剂冻干法制备尼莫地平前体脂质体,考察了影响药物包封率的因素,并对重建脂质体的药物含量、包封率、粒径、Zeta电位、溶血性及稳定性进行考察。结果磷脂浓度、表面电荷是影响尼莫地平脂质体包封率的主要因素。尼莫地平脂质体包封率大于98%,平均粒径为57 nm,Zeta电位小于-20 mV,无溶血性,稳定性好。结论采用叔丁醇水共溶剂冻干法获得了高包封率、粒径均一、无溶血性、稳定的尼莫地平前体脂质体制剂,可用于静脉注射给药。Objective To obtain high efficiency, low toxic and stable nimodipine new dosage form and prepare proliposome nimodipine. Methods Proliposome nimodipine was prepared by lyophilization tertiary butyl alcohol-water co-solvent system. The influencing factors on entrapment efficiency were studied. The content, entrapment efficiency, particle size, hemolysis and stability of the proliposome were determined. Results The lipid concentration and surface charge were the main factors that influenced the entrapment efficiency of nimodipine. The entrapment efficiency of liposome nimodipine was over 98 % with an average particle size of 57 nm, the Zeta potential was lower than - 20 mV, and the prepared liposome was stable and safe. Conclusions Proliposome nimodipine with high entrapment efficiency and homogeneous particle size distribution is obtained by lyophilization tertiary butyl alcohol-water co-solvent method, the prepared liposome is safe, stable and suitable for intravenous injection.

关 键 词：尼莫地平 前体脂质体 质量评价 

分 类 号：R944.9[医药卫生—药剂学]