康普瑞丁脂质体的研制及评价

Preparation and evaluation of CA4 liposome

目的研究康普瑞丁(CA4)脂质体的处方,并评价其性质。方法采用乙醚注入法制备CA4脂质体,以正交设计优化最佳处方,测定脂质体的形态和粒径,用HPLC法测定脂质体中CA4的包封率,并考察脂质体的体外释放规律。结果制备的脂质体平均粒径为16.04nm,最佳工艺处方为磷脂与胆固醇比为6∶1,附加剂P、A、B的用量分别为2%、2%、20%。所制3批脂质体的平均包封率为92.78%,体外释药规律符合Higuchi方程。结论乙醚注入法制备CA4脂质体可行。

OBJECTIVE To study the formulation of CA4 liposome and evaluate its quality. METHODS Liposome was prepared with ether injection method by using the orthogonal design to screen the formulation. Its shape and particle sizes were determined by electronic microscopy and Zetamaster. The encapsulation efficiencies were determined by HPLC. The release behavior of the liposome were evaluated. RESULTS The average size was about 16.04 nm. The optimal preparation conditions of CA4 liposome were as follows ： soybean phosphatidylcholine ： cholesterol was 6 ： 1. The dosage of P, A, B were 2% , 2% and 20%. The average encapsulation efficiency of the liposome was 92.78%. Its in vitro release profile accorded with Higuchi model. CONCLUSION It is a practically acceptable formulation by ether injection method.