新型缓释盐酸安非他酮包衣微囊的制备、表征与体外评价  

Preparation,characterization and in vitro evaluation of a novel sustained-release bupropion hydrochloride coated microcapsules

作　　者：杨泉竹 韩美苹 陈天祥 张新 金静维 刘宏飞 YANG Quan-zhu;HAN Mei-ping;CHEN Tian-xiang;ZHANG Xin;JIN Jing-wei;LIU Hong-fei(Wuyi University,Jiangmen Guangdong 529020;Jiangsu University,Zhenjiang Jiangsu 212013;Jiangmen Hongxiao Biomedical Co.,Ltd.,Jiangmen Guangdong 529000)

机构地区：[1]五邑大学,广东江门529020 [2]江苏大学,江苏镇江212013 [3]江门宏晓生物医药科技有限公司,广东江门529000

出　　处：《中南药学》2024年第6期1462-1469,共8页Central South Pharmacy

基　　金：五邑大学科研项目(No.2017RC28,No.2023AL001);2021句容市社会发展科技计划项目(No.ZA42109)。

摘　　要：目的 利用离子交换树脂技术和表面包衣法制备具有缓释效果的盐酸安非他酮包衣微囊(BH-CM)。方法 以强酸性阳离子交换树脂为载体,采用静态载药法制备盐酸安非他酮药物树脂复合物(BH-DRC),通过SEM、XRD、FTIR等对BH-DRC进行表征,并对BH-DRC的体外释放影响因素如溶出介质种类、介质浓度、温度、转速、体积等进行了考察。采用表面包衣法对BH-DRC进行包裹得到BH-CM,并通过单因素试验对BH-CM制备工艺进行了优化。结果 最终制备的BH-DRC的载药量(Q_(∞))为0.86 mg/1 mg Amberlite IRP69树脂,药物利用率(E)为86.90%。SEM、XRD、FTIR的结果表明BH与离子交换树脂不是简单的物理吸附,而是通过离子键结合。BH-DRC体外药物释放结果表明,BH释放过程受反离子种类、离子强度和转速的影响。采用表面包衣法优化后制备的3批BH-CM有明显的缓释效果。结论 本试验成功制备了一种新型的具有良好缓释效果的BH-CM,可为该药物缓释制剂的研发提供参考。Objective To prepare bupropion hydrochloride coated microcapsule(BH-CM)with sustained release by ion exchange resin technology and surface coating method.Methods Bupropion hydrochloride resin complex(BH-DRC)was prepared by bath method with highly acidic cation exchange resin as the carrier.The BH-DRC was characterized by SEM,XRD and FTIR,and the factors affecting the release of BH-DRC in vitro were also investigated,such as dissolution medium,medium concentration,temperature,rotation speed and volume.BH-DRC was coated by surface coating method to obtain BH-CM,and BH-CM was optimized by single factor experiment.Results The drug loading(Q_(∞))of BH-DRC was 0.86 mg/1 mg Amberlite IRP69 resin,and the drug utilization rate(E)was 86.90%.The results of SEM,XRD and FTIR showed that BH and ion exchange resin were not simply combined physically,but through ionic bonds.The drug release of BH-DRC in vitro showed that the release process of BH was affected by the kinds of countra-ion,ionic strength and rotating speed.Three batches of BH-CM with optimized surface coating had obvious sustained release effect.Conclusion A novel BH-CM with good sustained-release effect is successfully prepared in this experiment,which provides a new idea for the research and development of bupropion hydrochloride sustained-release preparation.

关 键 词：离子交换树脂 盐酸安非他酮 表面包衣法 体外释放 药物树脂复合物 包衣微囊 

分 类 号：R943[医药卫生—药剂学] R96[医药卫生—药学]