地红霉素肠溶微丸的处方与制备工艺研究  

Formulation and preparation of dirithromycin enteric-coated pellets

作　　者：崔文奇[1] 王东凯[1] 贺小玲[1] 肖玉婷[1] 高飞[1] 贾军[2] 殷栋二 

机构地区：[1]沈阳药科大学药学院,沈阳110016 [2]沈阳沃森药物研究所,沈阳110016 [3]海南碧凯药业,海口570216

出　　处：《中国新药杂志》2009年第12期1164-1167,1174,共5页Chinese Journal of New Drugs

摘　　要：目的:优化地红霉素肠溶微丸的处方与制备工艺。方法:以挤出滚圆法制备载药素丸,采用正交设计法优化处方和制备工艺参数;用流化床对载药素丸进行包衣,并以体外溶出释放度和杂质限量为控制指标,对包衣液处方进行优化。结果:优化的处方和挤出滚圆法工艺为:辅料与主药的比例为1∶1,挤出速度300 r.min-1,滚圆转速200 r.min-1,滚圆时间4 min。当隔离衣层增重为8%、肠溶衣层增重达到30%时,制剂长期试验12个月后各项指标均符合药典标准。结论:优化后的工艺简单且重现性好,适于地红霉素的工业化生产。Objective： To optimize the formulation and process of dirithromycin enteric-coated pellets. Methods：The uncoated dirithromycin pellets were prepared by extrusion-spheronization method and the processing parameters were optimized by orthogonal design. The pellets were coated by fluid-bed method. The coating formulation was optimized according to the in vitro release test and impurity level. Results：The optimized formulation and procedure parameters of dirithromyein enteric-coated pellets were as follows ： the ratio of excipients to drug was 1 ： 1 , the extrusive speed was 300 r·min^-1 ,the frequency of spheronization was 200 r·min^-1 and rotation time was 4 minutes. The pellets containing 8% weight gain of subcoating and 30% weight gain of enteric coating met the USP enteric claim for the long term stability of 12 months. Conclusion ：The procedure was simple,feasible and replieable. It is worth further development for the industrial production of the dirithromycin enteric-coated pellets.

关 键 词：地红霉素 肠溶微丸 正交设计 挤出滚圆 流化床 

分 类 号：R943.42[医药卫生—药剂学] R978.15[医药卫生—药学]