吲哚布芬缓释微丸的制备及其体外释放  

Preparation and in vitro release study of indobufen sustained-release pellets

作　　者：孙帅[1] 郭海燕[1] 张宁[1] 何海冰[1] 唐星[1] 王艳娇[1] SUN Shuai GUO Hai-yan ZHANG Ning HE Hai-bing TANG Xing WANG Yan-jiao(School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 11 O016, China)

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2017年第3期193-200,共8页Journal of Shenyang Pharmaceutical University

摘　　要：目的制备一种工艺简便、易于放大生产的吲哚布芬缓释微丸。方法结合流化床的底喷技术与液相层积法进行空白丸芯上药制备载药微丸,以新型水分散体Kollicoat~SR30D为包衣材料制备缓释微丸,考察包衣处方因素、热处理条件和释放介质等因素对释放度的影响。采用BET比表面积分析仪测定衣膜孔隙度和比表面积,探讨致孔剂对衣膜孔隙度的影响机制。初步考察微丸在不同条件下的稳定性并推测其体外的释放机制。结果吲哚布芬缓释微丸圆整度良好,包衣膜光滑完整,载药质量分数约为50%,在加速试验和长期试验中均能保持稳定的释药特性。致孔剂的添加能够增加衣膜内部的孔容及孔隙数量,从而显著增加膜层的比表面积。微丸体外释药机制符合一级动力学。结论所制得的吲哚布芬缓释微丸释药平稳、性质稳定、制备工艺简便、易于操作。Objective To prepare indobufen sustained-release pellets.Methods Fluid-bed spraying technique and drug solution layered technique were applied to prepare indobufen pellets.Kollicoat^（R） SR30 D,a novel aqueous dispersion,was used as the coating materials.The effects of different coating thickness,amount of pore-forming agents,heat-treatment conditions and dissolution media were investigated.The total pore volume and BET surface area were determined using surface area and pore size analyzer.Results The prepared indobufen sustained-release pellets had good roundness and the coating film was smooth and complete.Drug loading was 50%.The release profiles of pellets has no changed after long-term storage.The in vitro release data was well fitted to first-order drug release model.The pore-forming agent could increase the specific surface area by increasing the pore volume and pore number.Conclusions The preparation process is simple and reliable and the obtained sustain-release pellets have a good sustained-release behavior.

关 键 词：吲哚布芬 缓释微丸 流化床 体外释放 

分 类 号：R94[医药卫生—药剂学]