β-内酰胺酶抑制剂后效应研究进展  

Research progress of postβ-lactamase inhibitor effect

作　　者：谭舒文 何晓静[1] 菅凌燕[1] TAN Shuwen;HE Xiaojing;JIAN Lingyan(Department of Pharmacy,Shengjing Hospital of China Medical University,Liaoning Shenyang 110004,China)

机构地区：[1]中国医科大学附属盛京医院药学部,辽宁沈阳110004

出　　处：《中国医院药学杂志》2023年第20期2344-2349,共6页Chinese Journal of Hospital Pharmacy

摘　　要：β-内酰胺酶抑制剂后效应这一概念于1992年由Thorburn CE等学者首次提出,是指产酶细菌与β-内酰胺类抗菌药物/β-内酰胺酶抑制剂复方制剂接触一定的时间,只去除β-内酰胺酶抑制剂后,产酶细菌生长受到持续抑制的效应。这一效应为半衰期相差较大的β-内酰胺类抗菌药物与β-内酰胺酶抑制剂组成复方制剂的合理性提供了依据,为新药的开发提供了思路。该文综合了国内外相关研究文献,通过测定实验组和对照组细菌增长1个log10单位所需时间差值来确定β-内酰胺酶抑制剂后效应测定方法,对β-内酰胺酶抑制剂后效应可能的产生机制加以阐述,并讨论了细菌类型及产酶特点、β-内酰胺类抗菌药物及β-内酰胺酶抑制剂种类、抗菌药物浓度等影响因素以及已上市复方制剂的β-内酰胺酶抑制剂后效应研究结果,为后续研究提供参考。The concept of postβ-lactamase inhibitor effect was first proposed by Thorburn CE and other scholars in 1992,which refers to the effect of sustained inhibition of the growth of enzyme-producing bacteria after a certain period of exposure toβ-lactams/β-lactamase inhibitors with the removal ofβ-lactamase inhibitors only.This effect provides a basis for the rationality of the combination ofβ-lactam antibiotics andβ-lactamase inhibitors with large half-life differences,and provides an idea for the development of new drugs.In this paper,we have synthesized relevant domestic and foreign research literature,and explained the method of determining postβ-lactamase inhibitor effect by measuring the difference in the time required for the growth of bacteria in the experimental and control groups by one log10 and the possible mechanism of postβ-lactamase inhibitor effect.We focus on the influencing factors including bacterial types and enzyme-producing characteristics,types ofβ-lactam antibiotics andβ-lactamase inhibitors,antibacterial drug concentrations,and the results of postβ-lactamase inhibitor effect studies of marketed compound formulations to provide a reference for further research.

关 键 词：Β-内酰胺类抗菌药物 Β-内酰胺酶抑制剂 β-内酰胺酶抑制剂后效应 

分 类 号：R978.1[医药卫生—药品]