Synthesis of a novel pharmaceutical excipient: An anion exchange resin  

一种新型药用辅料阴离子交换树脂的合成

作　　者：Zhannuan Yin Xianghuan Meng Yingshu Feng Ke Li Xinyi Tang Hongfei Liu Haibing He Wei Mi 殷站暖;孟祥欢;冯颖淑;李可;唐欣怡;刘宏飞;何海冰;米伟(安徽中医药大学,安徽合肥230000;江苏大学药学院,江苏镇江212013;镇江学院医药化工研究所镇江功能化学重点实验室,江苏镇江212028;江苏海之宏生物医药有限公司,江苏南通226100;沈阳药科大学药学系,辽宁沈阳110016;江西阿尔法高科药业有限公司,江西萍乡337000)

机构地区：[1]Anhui University of Chinese Medicine,Hefei 230000,Anhui,China [2]College of Pharmacy,Jiangsu University,Zhenjiang 212013,Jiangsu,China [3]Zhenjiang Key Laboratory of Functional Chemistry,Institute of Medicine&Chemical Engineering,Zhenjiang College,Zhenjiang 212028,Jiangsu,China [4]Jiangsu Haizhihong Biopharmaceutical Co.,Ltd.,Nantong 226100,Jiangsu,China [5]Department of Pharmaceutics,Shen yang Pharmaceutical University,Shenyang 110016,Liaoning,China [6]Jiangxi Alpha Hi-tech Pharmaceutical Co.,Ltd.,Pingxiang,337000,Jiangxi,China

出　　处：《Journal of Chinese Pharmaceutical Sciences》2025年第2期109-125,共17页中国药学(英文版)

基　　金：2023 Nantong Jianghai Talents Project,the Nantong Social Livelihood Science and Technology Plan for 2023;the 2022 New Drugs and Platform Enhancement Project of the Yangtze Delta Drug Advanced Research Institute.Additionally,support was p rovided by the Zhenjiang Science and Technology Project(Grant No.SH2020048);the China Postdoctoral Science Foundation(Grant No.2020M681532);the Jiangsu Planned Projects for Postdoctoral Research Funds(Grant No.2020Z209);the Natural Science Research Projects of Universities in Jiangsu Province(Grant No.20KJD350001).

摘　　要：The aim of this study was to develop a novel pharmaceutical excipient:an anion exchange resin.Initially,polystyrenedivinylbenzene(PS-DVB)microspheres were synthesized via suspension polymerization.Subsequently,these microspheres served as a substrate for chloromethylation using methanol,formaldehyde,and chlorosulfonic acid.By optimizing the reaction conditions,the chloromethylated microspheres were characterized using infrared spectroscopy,scanning electron microscopy,and the Mohr method.Under optimal reaction conditions,the resulting products exhibited uniformity and spherical morphology,with an average particle size of approximately 190μm.The PS-DVB microspheres effectively incorporated chloromethyl groups,as evidenced by a chlorine content of 14.67%.Scanning electron microscopy analysis indicated that the appearance of the microspheres remained largely unchanged post-reaction.Overall,the research findings demonstrated the successful preparation of the anion exchange resin.Characterization and quality assessment confirmed that the ion exchange resin met the required standards.本研究旨在制备一种新型的药用辅料——阴离子交换树脂。首先,采用悬浮聚合法合成了聚苯乙烯-二乙烯基苯微球。接下来,以聚苯乙烯二乙烯基苯微球为基质,用甲醇、甲醛和氯磺酸对其进行氯甲基化。通过优化反应条件,用红外光谱、扫描电子显微镜和莫尔法对氯甲基化微球进行了表征。在合适的反应条件下,产物呈均匀球形,平均粒径约190μm,聚苯乙烯-二乙烯基苯微球可以成功引入氯含量为14.67%的氯甲基,扫描电子显微镜显示反应后微球的外观没有显著变化。研究结果表明,阴离子交换树脂已成功制备,经过表征和质量研究,离子交换树脂符合标准。

关 键 词：Suspension polymerization reaction POLYSTYRENE-DIVINYLBENZENE Quaternarization reaction Anion exchange resin Fluidized bed coating method Pharmacokinetic research 

分 类 号：R944[医药卫生—药剂学]