聚合胆汁酸螯合剂研究进展  

Research progress in polymeric bile acid sequestrant

作　　者：李香玉 台仲佳 张应辉[3] 杨美燕 高春生 LI Xiang-yu;TAI Zhong-jia;ZHANG Ying-hui;YANG Mei-yan;GAO Chun-sheng(Institute of Pharmacology and Toxicology,Academy of Military Medical Sciences,Beijing 100850,China;Pharmaceutical College,Henan University,Kaifeng 475004,China;Guangzhou Special Service Recuperation Center of PLA Rocket Force,Guangzhou 510515,China)

机构地区：[1]军事科学院军事医学研究院毒物药物研究所,北京100850 [2]河南大学药学院,开封475004 [3]中国人民解放军火箭军广州特勤中心,广州510515

出　　处：《中国新药杂志》2020年第18期2075-2082,共8页Chinese Journal of New Drugs

基　　金：国家“重大新药创制”科技重大专项资助项目:应急药物特种制剂创新及产业化关键技术平台(2018ZX09711003-008-001)。

摘　　要：近年来,聚合胆汁酸螯合剂(polymeric bile acid sequestrant,PBAS)用于治疗高胆固醇血症受到越来越多的关注。这些聚合物通常是带正电荷的非吸收性树脂,能选择性地结合并从胃肠道除去胆汁酸,降低血浆胆固醇水平。不同类型的聚合物的胆汁酸螯合机制不同,本文综述并讨论了含有季铵基团的两亲性聚合物、环糊精及聚β-环糊精和分子印迹聚合物3类不同PBAS的合成路径、体外胆汁酸结合活性以及体内降脂活性及其影响因素,旨在为PBAS的后续研究提供帮助。In recent years,the application of polymeric bile acid sequestrant(PBAS)for the treatment of hypercholesterolemia has received increasing attention.These polymers are positively charged non-absorbent resins that selectively bind and remove bile acids from the gastrointestinal tract,thus decreasing plasma cholesterol levels.The bind mechanisms of different types of polymers are different.The synthetic pathways,in vitro bile acid binding activity and in vivo lipid-lowering activity and its influencing factors of amphiphilic polymers containing quaternary ammonium groups,cyclodextrin and poly-β-cyclodextrin and molecularly imprinted polymers are reviewed and discussed in this paper,aiming to assist in the follow-up study of PBAS.

关 键 词：聚合胆汁酸螯合剂 胆汁酸 含季铵基团两亲性聚合物 环糊精 分子印迹聚合物 

分 类 号：R944[医药卫生—药剂学]