中药具有多成分、多靶点、代谢复杂、临床应用广泛的特点。中药药动学（pharmacokinetics，PK）是中药研究中的重大科学问题之一，在阐释中医中药的科学性、推进中药国际化、现代化中具有重要意义。基于生理学的药动学（physiologically based pharmacokinetics，PBPK）模型与基于生理学的生物药剂学（physiologically based biopharmaceutics，PBBM）模型针对中药及其复方，采用“自下而上”的方法预测药物的体外特性与体内血浆或不同组织中药物及其代谢物的药动学过程，为阐明中药药效物质基础、揭示中药有效性与安全性的科学内涵、中药新药研发与剂型改进等方面提供重要的参考信息。介绍PBPK/PBBM模型在中药药动学研究中的优势和应用，以期为中药现代化研究和临床合理用药等方面提供参考。

Traditional Chinese medicine (TCM) has been characterized by multi-component, multi-target, complex metabolism and wide clinical applications. Pharmacokinetics (PK) of TCM is one of the major scientific issues in the study of TCM, which plays a pivotal role in explaining the scientific nature of TCM and promoting the internationalization and modernization of TCM. The physiologically based pharmacokinetics (PBPK) and physiologically based biopharmaceutics (PBBM) models were found to not only simulate in vitro properties of TCM, but also predict pharmacokinetic processes of TCM and their metabolites in plasma or different tissues in vivo with a bottom-up approach. Furthermore, they provide important references for elucidating the material basis of the efficacy of TCM, revealing the scientific connotation of efficacy and safety of TCM, as well as improving dosage forms of new TCM. In this review, the advantages and applications of PBPK/PBBM model in pharmacokinetic study of TCM were summarized, with view to providing references for the modernization study and the rational clinical use of TCM.

国家自然科学基金资助项目（82141209）