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Issue 18, 2018
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Simultaneous quantitative analysis of retagliptin and its main active metabolite in human multiple matrices by liquid chromatography tandem mass spectrometry

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Abstract

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

Graphical abstract: Simultaneous quantitative analysis of retagliptin and its main active metabolite in human multiple matrices by liquid chromatography tandem mass spectrometry

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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, 2018,10, 2108-2114
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    Simultaneous quantitative analysis of retagliptin and its main active metabolite in human multiple matrices by liquid chromatography tandem mass spectrometry

    X. Meng, L. Cai, T. Ren, D. Sun and J. Gu, Anal. Methods, 2018, 10, 2108
    DOI: 10.1039/C8AY00040A

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