摘要
药物在体内产生药效作用有两个前提条件,其一是给药后药物分子能被机体有效利用(即:能够通过体内的生物屏障到达作用靶位,达到并维持起效浓度);其二是药物分子到达作用靶位的化学形式(原型化合物或代谢物)具有与药效关联的生物活性。中药药代动力学是中药药理学的重要分支,它从中药活性成分能否被机体有效利用的角度,研究与中药药效和安全性相关的物质问题。中药化学组成复杂,通常含众多活性成分,许多中药的发展经过"临床→研究→临床"的过程;与此相对应,化药通常为单一成分,其发展一般经过"研究→临床"的过程;这些带来了中药药代动力学研究有别于化药相关研究的特点。中药药代动力学研究常围绕临床有效中药,为揭示中药药效物质基础迈出关键的一步,并通过"选对成分"和"用好成分"为中药疗效的提高创造条件。作者主要基于其研究团队近年来开展的中药多成分药代动力学研究工作,重点介绍开展这类研究的思路和方法。
There are two prerequisites for the therapeutic action of a drug,i. e.,having sufficient bioavailability to and biopersistence at the locus of action after dosing and having intrinsic ability to produce desired pharmacodynamic effects in their major exposure forms,unchanged and metabolized. As a special branch of pharmacology of Chinese herbal medicines,pharmacokinetics is to investigate issues related to the medicines＇ efficacy and safety by assessing the herbal ingredients＇ bioavailability to and biopersistence at the locus of action in the body. Chinese herbal medicines are often herb combinations of complex mixture and contain multiple bioactive ingredients working in concert. Unlike most investigational synthetic drugs developed from bench to bedside,Chinese herbal medicines are often developed from bedside to bench to bedside. Accordingly,pharmacokinetic research on Chinese herbal medicines could serve as a crucial step in identifying the chemical basis of the medicines＇ therapeutic actions and could facilitate development of new herbal medicines with enhanced efficacy and safety by using the right herbal ingredients in the right way. Mainly based on studies by the author＇s research group,this article illustrates approach to and methodology of multi-compound pharmacokinetic research on Chinese herbal medicines.
作者
李川
LI Chuan(State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China)
出处
《中国中药杂志》
CAS
CSCD
北大核心
2017年第4期607-617,共11页
China Journal of Chinese Materia Medica
基金
国家重点基础研究发展计划项目(2005CB523403
2012CB518403)
国家科技重大专项(2009ZX09304-002)
国家杰出青年科学基金项目(30925044)
上海市科技成果转化和产业化项目(13DZ1970200)
关键词
多成分药代动力学研究
中药
中药药代标识物
multi-compound pharmacokinetic research
Chinese herbal medicines
pharmacokinetic markers for Chinese herbal medicines
