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目的:为新药的开发、已上市药物的结构改造以及一线临床联合用药方案的制定提供依据。方法:检索CHKD及PubMed数据库,分别以细胞色素、相互作用、体外试验为关键词进行检索,对2003~2013年的相关文献进行总结。分析细胞色素氧化酶的生物学特性以及如何选择合适的酶系统对药物进行体外代谢的药动学研究,以便推导其体内相互作用的可能性。结果:[I]/Ki值与药物相互作用的潜在可能性密切相关,但[I]值的估算是难点,应针对具体情况进行灵活调整。结论:以体外试验预测药物代谢及相互作用的技术能最大程度地避免繁琐的体内研究,可缩短新药研发周期,降低经济成本,并为临床合理联合用药提供理论依据并及时反馈风险警示。
OBJECTIVE: To provide evidence for the development of new drugs, the structural transformation of listed drugs and the formulation of first-line clinical combination regimens. Methods: The databases of CHKD and PubMed were searched, and the key words of cytochrome, interaction and in vitro test were searched respectively. The related literatures from 2003 to 2013 were summarized. Analysis of the biological characteristics of cytochrome oxidase and how to choose the right enzyme system for drug metabolism in vitro pharmacokinetic studies in order to derive the possibility of their body interaction. RESULTS: The value of [I] / Ki was closely related to the potential of drug interactions, but the estimation of [I] values was a difficult task and should be flexibly adjusted to specific situations. CONCLUSIONS: In vitro experiments predict drug metabolism and interaction technology to avoid cumbersome in vivo studies to the greatest extent, shorten the development cycle of new drugs, reduce economic costs and provide a theoretical basis for clinical rational combination of drugs and timely feedback risk warning.