中药方剂配伍理论是指导中药成方和临床合理用药的基本理论，体现了中药的药性理论和用药法度，是中药的特色与优势。合理的方剂配伍能影响其所含化学成分的吸收、分布、代谢和排泄的体内药物代谢动力学行为，能够在增强疗效的同时消除或减弱药物的不良反应。转运体和代谢酶是药物完成生物转化的重要组成部分，中药配伍引起转运体和代谢酶功能改变是方剂中药效成分体内过程发生变化的重要机制。研究基于转运体及代谢酶的中药相互作用是阐明方剂配伍规律的重要方向之一，有助于阐明中药方剂配伍规律和中药毒性的科学内涵，为临床组方用药提供科学依据。从转运体介导和代谢酶介导的中药相互作用两方面展开综述，旨在阐述方剂配伍与药物代谢的规律，总结中药配伍规律的内在联系，探讨中药方剂配伍的科学性，为阐明中药方剂作用机制的科学内涵及其现代配伍研究提供启示。

The compatibility of traditional Chinese medicine (TCM) prescription is the basic theory that guides the formulation of TCM and clinical rational drug use, which embodies the medicinal theory and medication method of TCM, representing the characteristics and advantages of TCM. Reasonable prescription compatibility can affect the absorption, distribution, metabolism and excretion of the chemical components in the pharmacokinetic behavior and enhance the efficacy while eliminating or weakening the toxic side effects. Transporters and metabolic enzymes are important components of drug biotransformation. The function changes of transporters and metabolic enzymes caused by the compatibility of TCM are important mechanisms for the changes in the in vivo process of the effective components in the prescriptions. Research on the interaction of TCM based on transporters and metabolic enzymes is one of the important directions to clarify the rules of prescriptions, which helps to show the rules of TCM prescription compatibility and the scientific connotation of TCM toxicity and to provide a scientific basis for the clinical prescription. This article reviews the interaction of TCM mediated by transporters and metabolic enzymes, aiming to elaborate the rules of prescription compatibility and drug metabolism, and summarize the internal relationship in the regulations of TCM prescription compatibility. This article discusses the scientificity of TCM prescription compatibility, so as to provide enlightenment for elucidating the scientific connotation of the mechanism of prescription action and the modern prescription compatibility of TCM.

R914;R285

天津市科技计划项目（24ZXZSSS00480）;药物成药性评价与系统转化全国重点实验室资助项目（712023001，712023002，712024001）