中药药代动力学是在中医理论指导下，采用药代动力学研究方法与技术，阐明中药活性成分、活性部位、单味中药及复方在体内吸收、分布、代谢和排泄的动态变化规律的学科。中药来源与组分复杂，绝大多数中药的药效物质和作用机制尚不十分明确，故中药药代动力学研究晚于化学药，也远比化学药复杂，其发展也面临更多挑战。我国中药药代动力学研究起源于20世纪50年代，从最初的单一活性成分体内过程研究，到活性成分药代动力学与药效学相关研究，再到中药复方和多组分药代动力学研究，已经历70余年的发展。近年来，借助先进的提取分离与分析技术、基因编辑动物与细胞模型、多组学技术、蛋白纯化与结构解析技术以及人工智能等，中药药代动力学在揭示与阐明中药药效物质与作用机制、中药新药研发、中成药大品种科技提升及指导临床合理用药中亦得到实质应用。中药药代动力学研究在理论、方法、技术及应用等多方面取得了显著突破和长足发展。该文综述了中药药代动力学的发展史和前沿研究进展，以期为中药药代动力学及相关研究提供思路与参考。

Pharmacokinetics of traditional Chinese medicine（TCM）is a discipline that adopts pharmacokinetic research methods and techniques under the guidance of TCM theories to elucidate the dynamic changes in the absorption，distribution，metabolism and excretion of active ingredients，active sites，single-flavour Chinese medicinal and compounded formulas of TCM in vivo. However，the sources and components of TCM are complex，and the pharmacodynamic substances and mechanisms of action of the majority of TCM are not yet clear，so the pharmacokinetic study of TCM is later than that of chemical medicines，and is far more complex than that of chemical medicines，and its development also confronts with challenges. The pharmacokinetic study of TCM originated in the 1950s and has experienced more than 70 years of development from the initial in vivo study of a single active ingredient，to the pharmacokinetic and pharmacodynamic study of active ingredients，to the pharmacokinetic study of compound and multi-component of Chinese medicine. In recent years，with the help of advanced extraction，separation and analysis technologies，gene-editing animals and cell models，multi-omics technologies， protein purification and structure analysis technologies， and artificial intelligence， etc.，the pharmacokinetics of TCM has been substantially applied in revealing and elucidating the pharmacodynamic substances and mechanisms of action of Chinese medicines，research and development of new drugs of TCM，scientific and technological upgrading of large varieties of Chinese patent medicines，as well as guiding the rational use of medicines in clinics. Pharmacokinetic studies of TCM have made remarkable breakthroughs and significant development in theory，methodology，technology and application. In this paper，the history of the development of pharmacokinetics of TCM and the progress of cutting-edge research was reviewed，with the aim of providing ideas and references for the pharmacokinetics of TCM and related research.

R969.1

国家自然科学基金国际 （地区）合作研究项目 （编号：81961128028）；国家自然科学基金区域联合重点项目 （编号：U22A20368）；国家自然科学基金重点项目 （编号：81930114）；广东省自然科学基金杰出青年项目 （编号：2022B1515020079）；“广东特支计划”杰出人才 （编号：2021JC050230）；广东省“岭南中医药现代化”重点专项项目 （编号：2020B1111100004）