去甲斑蝥素白蛋白微球的制备

Preparation and characteristics of norcantharidin albumin microspheres

目的:对去甲斑蝥素白蛋白微球的制备工艺及质量进行研究。方法:以白蛋白为载体,采用乳化交联法制备去甲斑蝥素白蛋白微球。在单因素考察的基础上,利用正交设计优化去甲斑蝥素白蛋白微球制备工艺,并对微球的粒径、形态、体外释放特性及稳定性进行研究。结果:制得的微球形态圆整,平均粒径为(0.54±0.13)μm,平均载药量为(51.36±2.45)%,平均包封率为(62.28±3.27)%,体外释放符合Higuchi方程,Q=10.1854t1/2-1.0858(r=0.998 1)。结论:本实验获得了较理想的去甲斑蝥素白蛋白微球,其体外释放特性符合长效制剂特征。

OBJECTIVE To prepare norcantharidin albumin microspheres, and evaluate its characteristics. METHODS The microspheres were prepared by emulsion chemical cross-linking method using albumin as carrier. Based on the result of single-factor selecting experiment, the methods of preparation were evaluated by ortbogonal experiment method. The mean diameter and the size distribution of microspheres, the drug loading, the envelop efficiency, the reproducibility of pharmaceutical technology and the stability of optimized micropheres were examined. RESULTS The microspheres were round and the surface was smooth. The average particle size was（0. 54 ± 0. 13）um , drug loading rate was （51.36 ±2.45）% and entrapment was （62.28 ±3.27） %. The drug release in vitro profile could be described by Higuchi equation Q= 10. 1854 t^1/2 -1. 0858（r= 0. 998 1）. CONCLUSION This paper describes the optimized preparation conditions of sustained-release norcantharidin albumin microsphere.