Zeng Mei, Yang Lan, He Dan, Li Yao, Shi Mingxin, Zhang Jingqing
a Chongqing Research Center for Pharmaceutical Engineering , Chongqing Medical University , Chongqing , China.
Drug Metab Rev. 2017 Nov;49(4):464-476. doi: 10.1080/03602532.2017.1377222. Epub 2017 Sep 14.
Drug metabolism plays an important role in the drug disposal process. Differences in pharmacokinetics among individuals are the basis for personalized medicine. Natural medicines, formed by long-term evolution of nature, prioritize the action of a target protein with a drug. Natural medicines are valued for structural diversity, low toxicity, low cost, and definite biological activities. Metabolic pathway and pharmacokinetic research of natural medicines is highly beneficial for clinical dose adjustment and the development of personalized medicine. This review was performed using a systematic search of all available literature. It provides an overview and discussion of metabolic pathways and the pharmacokinetics of natural medicines with low permeability. The related enzymes and factors affecting them are analyzed. The series of metabolic reactions, including phase I reactions(oxidation hydrolysis, and reduction reactions) and phase II reactions (binding reactions), catalyzed by intracellular metabolic enzymes (such as CYP450, esterase, SULT, and UGT enzymes) in tissues (such as liver and gastro-intestinal tract) or in the body fluid environment were examined. The administration route, drug dose, and delivery system had a large influence on absorption, metabolism, and pharmacokinetics. Natural medicines with low permeability had distinctive metabolisms and pharmacokinetics. The metabolic and in vivo kinetic properties were favorably modified by choosing suitable drug delivery systems, administration routes and drug doses, among other variables. This study provides valuable information for clinicians and pharmacists to guide patients safe, effective, and rational drug use. The research of metabolism and pharmacokinetics is significant in guiding personalized clinical medicine.
药物代谢在药物处置过程中起着重要作用。个体间药代动力学的差异是个性化医疗的基础。天然药物是自然长期演化形成的，其优先与药物作用于靶蛋白。天然药物因其结构多样性、低毒性、低成本和明确的生物活性而受到重视。天然药物的代谢途径和药代动力学研究对临床剂量调整和个性化医疗的发展非常有益。本综述通过系统检索所有可用文献进行。它概述并讨论了低渗透性天然药物的代谢途径和药代动力学。分析了相关酶及其影响因素。研究了由组织（如肝脏和胃肠道）或体液环境中的细胞内代谢酶（如CYP450、酯酶、SULT和UGT酶）催化的一系列代谢反应，包括I相反应（氧化、水解和还原反应）和II相反应（结合反应）。给药途径、药物剂量和给药系统对吸收、代谢和药代动力学有很大影响。低渗透性天然药物具有独特的代谢和药代动力学。通过选择合适的药物递送系统、给药途径和药物剂量等变量，可以有利地改变其代谢和体内动力学性质。本研究为临床医生和药剂师指导患者安全、有效和合理用药提供了有价值的信息。代谢和药代动力学研究在指导个性化临床医学方面具有重要意义。
