药用辅料对药物转运体影响研究现状  

Review of pharmaceutical excipients effects on drug transports

作　　者：刘鑫[1,2] 陈露露 方青 巨舸航 欧阳冬生 LIU Xin;CHEN Lu-lu;FANG Qing;JU Ge-hang;OUYANG Dong-sheng(Department of Clinical Pharmacology,Xiangya Hospital,Central South University,Changsha 410000,Hunan Province,China;Hunan Key Laboratory for Bioanalysis of Complex Matrix Samples,Changsha 410000,Hunan Province,China;Changsha Duxact Biotech Co Ltd,Changsha 410000,Hunan Province,China)

机构地区：[1]中南大学湘雅医院临床药理研究所,湖南长沙410000 [2]复杂基质样本生物分析湖南省重点实验室,湖南长沙410000 [3]长沙都正生物科技股份有限公司,湖南长沙410000

出　　处：《中国临床药理学杂志》2022年第10期1128-1132,共5页The Chinese Journal of Clinical Pharmacology

基　　金：湖南省创新型省份建设专项基金资助项目(2019CB1014);湖南省创新型省份建设专项基金资助项目(2019SK2241);湖南省创新型省份建设专项基金资助项目(2019GK5020);长沙市科技计划基金资助项目(kh1902002)。

摘　　要：药用辅料是药物制剂中不可缺少的组成成分,其通常作为惰性物质影响药物制剂的崩解、溶出等过程。近年来,随着研究的深入,许多常见药用辅料如表面活性剂,稳定剂,润滑剂等均在体内外表现出一定的生理和药理活性。研究表明药用辅料可通过影响药物转运体和肝药酶,进而影响药物的体内处置过程,导致药动学和药效学行为发生改变,甚至引起临床药物不良反应的发生。药用辅料对常见ATP结合盒转运体,如P-糖蛋白转运体、乳腺癌耐药蛋白和多药耐药相关蛋白,以及溶质载体转运体,如有机阴离子转运肽,有机阴离子转运体,有机阳离子转运体和寡肽转运蛋白等多具有一定的抑制作用,也有少量报道辅料对转运体具有诱导作用,但其抑制和诱导机制尚未完全阐明。本文就目前药用辅料对药物转运体影响的研究及其可能存在的机制展开综述,以期为仿制药及创新药物制剂方面研发提供新思路。Pharmaceutical excipients are usually considered as inert substances but essential components of drug formulation,which could affect the disintegration and dissolution of pharmaceutical preparations.Recently,many sudies showed that various types of pharmaceutical excipients,such as surfactants,stabilizers and lubricants et al.could affect the activity and expression of drug transporters and cytochrome P450 enzymes in several studies,which may have an effect on the drug process in vivo,such as the changing of pharmacokinetics and pharmacodynamics process.There are many literatures have reported that pharmaceutical excipients have potential inhibition effects on drug transporters,such as Adenosine-triphosphate binding cassette transporters and solute carrier transporters;however,the mechanism of these effects still remain unknown.The purpose of this review is to summarize the effect and the possible mechanism of pharmaceutical excipients on drug transporters.

关 键 词：药用辅料 药物转运体 药物处置 药物相互作用 

分 类 号：R97[医药卫生—药品]