Validated LC-MS/MS methods for the determination of dapagliflozin, a sodium-glucose co-transporter 2 inhibitor in normal and ZDF rat plasma

被引：27

作者：

Aubry, Anne-Francoise ^{[1
]}

Gu, Huidong ^{[1
]}

Magnier, Reynald ^{[2
]}

Morgan, Ling ^{[3
]}

Xu, Xiaohui ^{[1
]}

Tirmenstein, Mark ^{[4
,5
]}

Wang, Bonnie ^{[4
,5
]}

Deng, Yuzhong ^{[1
]}

Cai, Jinnan ^{[1
]}

Couerbe, Philippe ^{[2
]}

Arnold, Mark ^{[1
]}

机构：

[1] Bristol Myers Squibb Co, Bioanalyt Sci, Princeton, NJ 08540 USA

[2] AtlanBio, St Nazaire, France

[3] Tandem Labs, Woburn, MA USA

[4] Bristol Myers Squibb Co, Drug Safety Evaluat, New Brunswick, NJ USA

[5] Bristol Myers Squibb Co, Drug Safety Evaluat, Princeton, NJ USA

来源：

BIOANALYSIS | 2010年 / 2卷 / 12期

关键词：

SGLT2; INHIBITOR; MASS-SPECTROMETRY; POTENT;

D O I：

10.4155/BIO.10.139

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Background: Dapagliflozin is an inhibitor of sodium-glucose co-transporter 2 (SGLT-2) in development for the treatment of Type 2 diabetes. To support toxicology studies, LC-MS/MS methods were developed and validated for the quantitation of dapagliflozin in rat plasma. Results: The assay uses solid phase extraction and LC-MS/MS analysis in negative ion electrospray ionization mode. Because dapagliflozin readily forms adducts in the presence of formic acid, the mobile phases were simple mixtures of water and acetonitrile. The assay was validated in the concentration range of 5-2000 ng/ml with good intra- and inter-day precisions and acceptable sample stability. Conclusion: The validated assay was successfully applied to the quantitation of dapagliflozin in plasma in support of preclinical studies in both normal and diabetic rats.

引用

页码：2001 / 2009

页数：9

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