克拉霉素缓释包衣微丸的制备及体外释放度研究  

Preparation and in Vitro Release Study of Sustained-release Coated Pellets Containing Clarithromycin

作　　者：柳晓蕊[1,2,3] 章正赞[1,2] 贺周扬[1,2] 潘昕[1,2] 吴传斌[1,2] 

机构地区：[1]中山大学药学院,广州510006 [2]广东省创新药物制剂工程技术研究中心,广州510006 [3]广州医学院附属肿瘤医院,广州510095

出　　处：《中国现代应用药学》2013年第2期143-147,共5页Chinese Journal of Modern Applied Pharmacy

基　　金：广东省创新药物制剂工程技术研究开发中心(2011B080100019)

摘　　要：目的制备克拉霉素缓释包衣微丸,并对其体外释放度进行考察。方法采用挤出滚圆技术制备克拉霉素含药微丸。以优化的丙烯酸树脂类Eudragit NE30D和Eudragit L30D-55混和水分散体为包衣材料,采用流化床包衣技术,制备缓释包衣微丸。考察自制缓释微丸的体外释药速率,并与市售的克拉霉素缓释胶囊进行比较。结果通过释药行为的评价,得到优化的包衣处方为5∶1的Eudragit NE30D和Eudragit L30D-55混和包衣材料,其体外释放行为在不同的pH溶出介质中与市售制剂产品没有明显差异,体外释药过程符合一级释放模型。结论采用挤出滚圆和流化床技术,以及优化的Eudragit NE30D和Eudragit L30D-55混和水分散体包衣材料,成功制备了克拉霉素缓释包衣微丸。OBJECTIVE To prepare sustained-release coated pellet containing clarithromycin, and to investigate its in vitro drug release behavior. METHODS Extrusion-spheronization technology was used to prepare clarithromycin-containing pellets. The drug contained pellets were coated with the optimized polymeric combination of Eudragit NE30D and Eudragit L30D-55 by using fluid-bed technology. In vitro drug release behavior of the coated pellets was studied and compared with the commercially available sustained-release capsules of clarithromycin. RESULTS There were no significant differences in different pH dissolution medium between the coated pellets and commercial products in drug release behavior, with optimized coating material as Eudragit NE30D and Eudragit L30D-55 at ratio of 5 ： 1. The drug release mechanism of coated pellets was in accordance with first-order release model. CONCLUSIONS With extrusionspheronization and fluid-bed technology, the sustained-release coated pellets containing clarithromycin are successfully prepared by using the mixture aqueous dispersion of Eudragit NE30D and Eudragit L30D-55 as coating material.

关 键 词：克拉霉素 挤出滚圆 流化床 丙烯酸树脂 缓释包衣微丸 

分 类 号：R943[医药卫生—药剂学]