前药的药代动力学研究进展  

Research on the pharmacokinetics of prodrugs

作　　者：朱胤慈[1] 孙建国[1] 彭英[1] 王广基[1] 

机构地区：[1]中国药科大学药物代谢动力学重点实验室

出　　处：《中国临床药理学与治疗学》2012年第12期1433-1440,共8页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金："十一五"重大新药创制科技重大专项资助(2009ZX09304-001);中央高校基本科研业务费专项资助(JKP2009007)

摘　　要：前药是自身无活性,在体内经生物转化后释放出有药效活性的代谢物或原药的化合物。前药设计已成为改善药物的一些不良性质如水溶性低、生物利用度差、半衰期太短及缺乏理想的靶向性等的一种重要手段。然而如何从药物代谢动力学角度评价前药尚缺乏统一的标准。本文对近年来前药的药代动力学研究状况进行了概括总结,并提出如何从吸收、分布、代谢和排泄角度对前药的药代动力学性质进行全面评价。Prodrugs are chemicals with little or no pharmacological activity,which can be changed to therapeutically active metabolite after undergoing biotransformation in vivo.The design of prodrugs has become an important way to overcome the shortcomings of drugs such as poor solubility,low bioavailability,short elimination half-life,devoid of ideal targets and so on.However,there still lacks criteria to evaluate pharmacokinetic properties of prodrugs.This paper reviews the pharmacokinetic profiles of various types of prodrugs in recent years,and proposes full evaluation from absorption,distribution,metabolism and excretion perspectives.

关 键 词：前药 药物代谢动力学 转化 

分 类 号：R969.1[医药卫生—药理学]