埃索美拉唑药物树脂复合物包衣微囊的制备及评价  

Preparation and evaluation of esomeprazole drug resin complex coated microcapsules

作　　者：茅关兴 辛渊蓉 窦玉甜 王佳鹏 刘宏飞[2,3] MAO Guan-xing;XIN Yuan-rong;DOU Yu-tian;WANG Jia-peng;LIU Hong-fei(Shanghai Pharmaceutical Industry Co.,Ltd.,Shanghai 200002;Jiangsu University,Zhenjiang Jiangsu 212000;Jiangsu Sunan Pharmaceutical Industrial Co.,Ltd.,Zhenjiang Jiangsu 212000)

机构地区：[1]上海医药工业有限公司,上海200002 [2]江苏大学,江苏镇江212000 [3]江苏苏南药业实业有限公司,江苏镇江212000

出　　处：《中南药学》2024年第7期1718-1724,共7页Central South Pharmacy

基　　金：2021句容市社会发展科技计划项目(No.ZA42109)。

摘　　要：目的采用离子交换技术和流化床包衣技术制备具有肠溶效果的埃索美拉唑药物树脂复合物包衣微囊(ESO-CM)。方法以多孔阴离子交换树脂为载体,静态载药法制备ESO树脂复合物(ESO-DRC),对其进行结合机制表征和体外释放考察。采用流化床包衣技术对ESO-DRC进行包衣,制得ESO-CM,观察其形态并考察体外释放过程。结果制备的ESO-DRC的载药量为0.93 mg ESO/1 mg树脂,药物利用率为92.30%。树脂与ESO通过离子键结合。在介质为900 mL 0.15 mo1·L^(-1)NaCl溶液,介质温度(37±0.5)℃,转速50 r·min^(-1)的体外释放条件下,ESO-DRC可在60 min内释放90%左右。ESO-CM粒径均匀,表面光滑,含量均一,肠溶效果明显。结论本研究成功开发了一种稳定、肠溶效果良好的埃索美拉唑药物树脂复合物包衣微囊。Objective To prepare esomeprazole drug resin complex coated microcapsules(ESOCM)with enteric-coating effect through ion exchange and fluidized bed coating.Methods ESO drug resin complex(ESO-DRC)was prepared with static drug loading using porous anion exchange resin as the carrier.The binding mechanism and in vitro release were determined.ESO-DRC was coated with fluidized bed coating to prepare ESO-CM,whose morphology and in vitro release was observed.Results The drug loading of ESO-DRC was 0.93 mg ESO/1 mg resin,with drug utilization rate at 92.30%.The combination of resin and ESO was achieved through ionic bonds.Under the in vitro release conditions of 900 mL 0.15 mo1·L^(-1)NaCl solution,medium temperature of(37±0.5)℃,and rotation speed of 50 r·min^(-1),about 90%of ESO-DRC was released within 60 min.ESOCM had uniform particle size and content,smooth surface,and significant enteric dissolution effect.Conclusion This study successfully develops a stable ESO-CM with enteric-coating effect.

关 键 词：埃索美拉唑 离子交换树脂 流化床包衣技术 肠溶包衣微囊 

分 类 号：R944[医药卫生—药剂学]