5-氨基水杨酸pH依赖型控释微丸的制备及质量评价  

Preparation and Quality Evaluation of Mesalazine pH Controlled-release Pellet

作　　者：程娟 田丽娟 周建平[2] 黄春玉 戴银娣[2] 谢俊 

机构地区：[1]南京金陵药业股份有限公司技术中心,南京210009 [2]中国药科大学药剂教研室,南京210009

出　　处：《药学与临床研究》2012年第1期27-30,共4页Pharmaceutical and Clinical Research

摘　　要：目的:制备5-氨基水杨酸(美沙拉嗪)pH依赖型控释微丸,考察影响载药丸芯制备和微丸控释的因素。方法:以圆整度、粒度分布和收率、脆碎度和流动性为指标,采用正交设计法筛选丸芯的处方和工艺以及包衣的增重和老化条件。结果:最佳处方工艺为载药量80%、粘合剂用量40mL/100 g、挤出速度30 Hz、滚圆速度30 r.min-1;包衣增重8%,老化条件为60℃、24 h。结论:制备了适合流化床包衣的美沙拉嗪载药丸芯,以尤特奇水分散体包衣得到了pH依赖型控释微丸。Objective： To prepare mesalazine pH controlled-release pellets and investigate the factors affecting the preparation and dissolution. Methods： Taking aspect ratio（AR）, circularity, yield, friability, fluidity as key indexes, an orthogonal design was carried out to optimize the formulation and technology of pellet as well as the gaining weight and ageing conditions of coating. Results： The best formulation and production parameters were： drug loading rate, 80%; binders, 40mL/100g; extrusion rate, 30r.min^-1; spheronization rate, 30 Hz; coating weight gaining, 8%; and ageing at 60℃ for 24 h. Conclusion： It is possible to prepare mesalazine pH-controlled-release pellet by extrusion-spheronization and Eudragit S 100 coating.

关 键 词：美沙拉嗪 微丸 质量评价 pH依赖型控释 

分 类 号：R944.9[医药卫生—药剂学] R927.11[医药卫生—药学]