去甲斑蝥素肝动脉栓塞缓释微球的制备及其体外释放性评价  

Preparation and in Vitro Drug Release of Norcantharidin Sustained-release Microsphere for Hepatic Arterial Embolism

作　　者：周欣颖[1] 王浩[1] 贝永燕[1] 许静玉[1] 王文娟[1] 张学农[1] 

机构地区：[1]苏州大学药学院,苏州市215123

出　　处：《中国药房》2011年第13期1185-1189,共5页China Pharmacy

基　　金：国家科技支撑计划课题资助(2006BAI09B00);江苏省"六大人才高峰"资助项目;2009年国家大学生创新性实验计划立项项目(57315924)

摘　　要：目的:制备去甲斑蝥素肝动脉栓塞缓释微球(NCTD-MS),并考察其体外释放特性。方法:以NCTD为主药,海藻酸钠ALG)/壳聚糖(CS)为复合载体,采用内部凝胶化法制备NCTD-MS;选取ALG浓度、凝胶化反应剂冰醋酸的用量、药物-载体重量比(简称药载比)为因素,以粒径偏差、载药量及包封率为指标进行正交设计优化最佳处方并进行验证;动态透析法考察微球在不同介质(磷酸盐缓冲液和生理盐水)中的体外释放特性,并与NCTD原料药的释放性进行比较。结果:最佳处方为ALG浓度2.0%、冰醋酸1.0mL、药-载重量比0.8∶1,以该处方制备的微球平均粒径为(309.75±2.19)μm、载药量为(12.65±0.87)%、包封率为(68.66±0.38)%;NCTD-MS在2种介质中24h释放可达80%,释放行为均遵循Weibull方程,而NCTD原料药在3h内即释放完毕。结论:NCTD-MS制备工艺简单,缓释效果明显。OBJECTIVE： To prepare Norcantharidin sustained-release microsphere （NCTD-MS） for hepatic arterial embolism, and to investigate in vitro release characteristics of it. METHODS： NCTD-MS were prepared by inner gel technique with alginate -chitosan （ALG-CS） as carrier and NCTD as the main component. The formulation of NCTD-MS was optimized by orthogonal test using ALG concentration, emulsifier amount, ratio of drug to carrier （called drug-loading rate in short） as factors and with di- ameter deviation, drug loading content and encapsulation efficiency as indices. Dynamic dialysis method was adopted to study the release characteristics of NCTD-MS in different mediums （phosphate buffer solution and normal saline） in vitro, which was compared with release characteristics of NCTD raw material. RESULTS： The optimized formulation was as follows： ALG concentration 2.0 %, glacial acetic acid 1.0 mL, drug-loading rate 0.8 ： 1. The MS was of average diameter （309.75±2.19） μm, drug-loading content （12.65±0.87）%, encapsulation efficiency （68.66± 0.38）%. Drug release rate of NCTD-MS in 2 kinds of mediums was 80% in 24 h. The drug release of NCTD-MS was in line with Weibull equation. NCTD raw material released completely in 3 h. CONCLUSION： The preparation technology of NCTD-MS is simple and it is characterized with sustained-release effect.

关 键 词：去甲斑蝥素 壳聚糖 海藻酸钠 缓释微球 制备 释放性 

分 类 号：R927.11[医药卫生—药学] R943