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Simultaneous quantitative analysis of retagliptin and its main active metabolite in human multi-matrices by liquid chromatography tadem mass spectrometry

Abstract

Retagliptin is a dipeptidyl peptidase 4 (DPP-4) inhibitor which has proven efficacy and safety on type 2 diabetes mellitus (T2DM). In order to investigate the pharmacokinetics of retagliptin and its main active metabolite, retagliptin acid, we developed the liquid chromatography tandem mass spectrometry (LC-MS/MS) methods for simultaneous determination of retagliptin and retagliptin acid in human plasma, urine and feces. The lower limit of quantification (LLOQ) for retagliptin and retagliptin acid are 0.1 ng/mL and 0.3 ng/mL in plasma, 5 ng/mL and 10 ng/mL in urine, 1 ng/mL and 3 ng/mL in feces. The methods were fully validated and successfully applied in the pharmacokinetic study in human after an oral administration of 100 mg retagliptin.

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Publication details

The article was received on 08 Jan 2018, accepted on 30 Mar 2018 and first published on 03 Apr 2018


Article type: Paper
DOI: 10.1039/C8AY00040A
Citation: Anal. Methods, 2018, Accepted Manuscript
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    Simultaneous quantitative analysis of retagliptin and its main active metabolite in human multi-matrices by liquid chromatography tadem mass spectrometry

    X. Meng, L. Cai, T. Ren, D. Sun and J. Gu, Anal. Methods, 2018, Accepted Manuscript , DOI: 10.1039/C8AY00040A

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