聚乙二醇修饰小分子药物的研究进展  

Research progress of polyethylene glycol modified small molecule drugs

作　　者：刘霞[1] 丁志山[1] 蒋福升[1] 

机构地区：[1]浙江中医药大学生命科学学院分子与遗传教研室,浙江杭州310053

出　　处：《中国药理学与毒理学杂志》2010年第5期380-386,共7页Chinese Journal of Pharmacology and Toxicology

基　　金：浙江省自然科学基金(M303722);浙江省自然科学基金(Y206776);浙江省中医药重点项目研究计划(2005Z001);浙江省中医药青年课题研究计划(2009YB001);浙江省教育厅科研项目(Y200805067)~~

摘　　要：聚乙二醇修饰技术是目前药物化学修饰的研究热点,它能够显著提高药物分子水溶性,同时改善药物的药动学和药效学特性,增加了药物临床应用的范围和疗效,具有较好的开发应用前景;但同时也存在诸多问题,有待改进,目前在国内研究相对较少,值得进一步研究开发。本文从聚乙二醇修饰技术被修饰的小分子药物种类、连接臂类型、聚乙二醇载体以及修饰后药物药动学性质和药效学性质改变等方面进行系统综述。The polyethylene glycol ( PEG) modification technique of chemical drugs has recently become a research focus. It can dramatically enhance the water solubility and pharmacokinetic and pharmacodynamic properties of the small-molecule drugs,extend their clinical application range,improve their therapeutic effects and has showed great prospect. However,many problems remain unsettled. Only a few studies on it have been reported in China. An overview of small-molecule drug PEGylation is presented in the current review,which focuses on small-molecule drugs,linkers,PEG carriers and the change in pharmacokinetic and pharmacodynamic properties of small-molecule drugs with PEGylation in recent years.

关 键 词：聚乙二醇类 药物载体 药物前体 

分 类 号：R962[医药卫生—药理学]