乙醇注入法制备水飞蓟宾脂质体及其质量评价  

The preparation of silybin liposome by ethanol injection method and its quality evaluation

作　　者：高飞[1] 王东凯[1] 张春叶[1] 崔文奇[1] 苏娟娟[2] 贾军[2] 

机构地区：[1]沈阳药科大学药学院 [2]沈阳沃森药物研究所

出　　处：《中国药剂学杂志（网络版）》2008年第6期301-308,共8页Chinese Journal of Pharmaceutics：Online Edition

摘　　要：目的制备水飞蓟宾脂质体,优化其处方和工艺,并对其相关性能进行评价。方法采用乙醇注入法制备水飞蓟宾脂质体;采用HPLC法和超滤法测定脂质体的药物含量和包封率,单因素考察处方及工艺对包封率的影响,并采用正交设计法进行处方工艺优化。结果确定最佳处方工艺为:磷脂质量浓度为0.006mg·mL-1,磷脂与胆固醇的质量比为10∶1,药脂比为1∶60,缓冲液pH值为7.30,类脂溶液的溶解顺序是将磷脂、胆固醇、水飞蓟宾一起溶解在乙醇中,溶解温度设定为35℃,类脂溶液的溶解时间为25min。制得的水飞蓟宾脂质体包封率为(92.44±0.98)%,平均粒径为(151±21)nm,Zeta电位为(-34.6±1.2)mV,此制剂无溶血性。结论乙醇注入法制备水飞蓟宾脂质体工艺简单可行,所制备的水飞蓟宾脂质体包封率高、粒径较小、无溶血性。Objective To prepare silybin liposome, optimize the formulation and preparation technology, and evaluate its properties. Method Silybin liposome was prepared by ethanol injection method. HPLC and ultrafiltration methods were used to determine silybin entrapment efficiency in the liposome. Factors influencing the encapsulation efficiency of silybin in the liposome was investigated, and formulation and process parameters were optimized with orthogonal design. Result The optimized condition was as follows: the total phospholipid concentration 0.006 mg·mL-1, the ratio of phospholipid to cholesterol 10:1(m:m), the ratio of drug to total lipid 1:60 (m:m), pH=7.30, the lipid solution was prepared by dissolving phospholipid, cholesterol and drug together in ethanol of 35 ℃ for 25 min. Encapsulation efficiency of silybin in liposome reached (92.44±0.98) % after optimization, with the mean size of (151±21) nm and the Zeta potential of (-34.6±1.2) mV. The prepared liposome caused no hemolysis. Conclusion It is feasible to prepare silybin liposome by ethanol injection method. The obtained silybin liposome has high encapsulation efficiency, low particle size without hemolysis.

关 键 词：药剂学 脂质体 乙醇注入法 水飞蓟宾 包封率 

分 类 号：TQ461[化学工程—制药化工]