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转运体在药物的吸收、分布以及排泄过程中发挥着重要作用。明确药物转运机制有利于提高药物安全性和有效性,从而指导临床合理用药。二甲双胍作为2型糖尿病的临床一线用药,多种转运体参与了其体内过程,转运体表达和功能的改变直接影响其药动学和药效学。本文综述了基于药物转运体机制的二甲双胍体内过程,这些转运体包括有机阳离子转运体(OCTs)、多药及毒性化合物外排转运蛋白(MATE)、质膜单胺蛋白转运体(PMAT)、五羟色胺转运体(SERT)、硫胺素转运体2(THTR-2)、肉碱/有机阳离子体1(OCTN1)。
Transporters play an important role in the absorption, distribution and excretion of drugs. Clear mechanism of drug transport is conducive to improving drug safety and effectiveness, so as to guide clinical rational drug use. As a clinical first-line drug for type 2 diabetes, metformin participates in many in vivo processes. The changes in the expression and function of transporters have a direct impact on their pharmacokinetics and pharmacodynamics. This article reviews the in vivo processes of metformin based on drug transporter mechanisms including organic cation transporters (OCTs), multi-drug and toxic compound efflux transporter (MATE), plasma membrane monoamine transporter (PMAT), serotonin Transporter (SERT), thiamine transporter 2 (THTR-2), carnitine / organic cation 1 (OCTN1).