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在线固相萃取-高效液相色谱法对血浆蛋白结合解离的表征

Characterization of plasma protein binding dissociation with online SPE-HPLC.

作者信息

Li Ping, Fan Yiran, Wang Yunlong, Lu Yaxin, Yin Zheng

机构信息

College of Pharmacy &State Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, P.R.China.

Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), Tianjin 300071, P.R.China.

出版信息

Sci Rep. 2015 Oct 13;5:14866. doi: 10.1038/srep14866.

Abstract

A novel parameter of relative recovery (R re) was defined and determined by online SPE-HPLC to characterize plasma protein binding (PPB) kinetics of highly plasma binding drugs. The proportional relationship of R re with k off of PPB has been established with a new SPE model. A rapid, easy to use method could potentially be used to categorize PK properties of the drug candidates in the decision process of drug discovery and development.

摘要

定义了一个新的相对回收率(R re)参数,并通过在线固相萃取-高效液相色谱法(online SPE-HPLC)进行测定,以表征高血浆结合药物的血浆蛋白结合(PPB)动力学。利用一种新的固相萃取模型建立了R re与PPB解离速率常数(k off)的比例关系。在药物发现和开发的决策过程中,一种快速、易于使用的方法可能会被用于对候选药物的药代动力学特性进行分类。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5dab/4602217/d15a29f914ce/srep14866-f1.jpg

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