药物-血浆蛋白结合率测定方法的研究进展  

Recent advances in determination methods of drug protein binding

作　　者：关瑾[1] 丁爽[1] 刘芷含[1] 董西鑫 阎峰[1] 石爽[1] 

机构地区：[1]沈阳化工大学应用化学学院,沈阳110142

出　　处：《中国新药杂志》2014年第10期1149-1153,共5页Chinese Journal of New Drugs

基　　金：辽宁省自然基金(20092055);辽宁省教育厅科学研究一般项目(L2012150)

摘　　要：药物与血浆蛋白的结合作用影响药物在体内的吸收、分布、代谢与排泄,从而影响药理效应强度和时间。药物进入人体,只有游离的药物分子能够跨膜运转并与受体结合发生药理效应,因此测定药物与血浆蛋白结合率在新药研发及临床研究中非常重要。本文主要评述了近年来相关研究的技术和方法,包括平衡透析法、微透析法、超滤法、超速离心法,以及以光谱学为基础的方法(如紫外-可见吸收光谱法,荧光光谱法和表面等离子体子共振技术法等)和以色谱法为基础的方法(如高效亲和色谱法、高效前沿分析法等)。此外,对各种方法的原理、优缺点进行了概括总结,并对其发展前景进行了展望。Binding of drugs to plasma protein is critically involved in drug pharmacokinetics（i. e.,absorption,distribution,metabolism,and elimination） and pharmacodynamics（pharmacological effects）. Generally the free drug fraction is available for diffusion and transport across cell membranes. It is therefore highly important to estimate drug-binding ability to these macromolecules in the early stages of drug discovery and in clinical practice. This review focuses on the most important approaches used to characterize drug-protein binding sciences including equilibrium dialysis,micro-dialysis,ultrafiltration,ultracentrifugation,spectroscopy methods（e. g.,ultraviolet-visible absorption spectrum,fluorescence spectrum and surface plasmon resonance,etc.） and chromatography methods（e. g.,high performance affinity chromatography,high performance frontal analysis,etc）. A description of the principle of each method with its inherent strengths and weaknesses is outlined. Finally,the future prospects in this field are also discussed.

关 键 词：药物 血浆蛋白结合率 测定方法 毛细管电泳法 应用 

分 类 号：R914.1[医药卫生—药物化学]