摘要
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)。
Drug transporters play vital roles in absorption, distribution and excretion of drugs. Under- standing the transport activity can improve the effectiveness and safety of drugs and guide clinical rational use of drugs. Metformin is a first-line drug in the treatment of type 2 diabetes mellitus, of which the pharmaeokinetics involves several transporters. The changes in expression and function of these transporters affect directly the pharmacokinetics/pharmacodynamics of metformin. This paper reviews the research progress of pharmacokinetics of metformin based on transporters, and these transporters are organic cation transporters （OCTs）, multidrug and toxin extrusion proteins （MATE）, plasma membrane monoamine transporter protein （PMAT）, serotonin reuptake transporter （SERT）, thiamine transporter 2 （THTR-2）, and carnitine/organic cation 1 （OCTN1）.
出处
《药学学报》
CAS
CSCD
北大核心
2017年第6期865-870,共6页
Acta Pharmaceutica Sinica
基金
国家自然科学基金资助项目(81303296)
杏林学者(2013)
