Determination of 2-(3-Benzoyl)-4-Hydroxy-1,1-Dioxo-2H-1,2-Benzothiazine-2-yl-1-Phenylethanone by Liquid Chromatography-Tandem Mass Spectrometry
- Authors
- Zheng, Zhi; Song, Jin Sook; Lee, Byung Hoi; Ahn, Sung-Hoon; Ahn, Jin-Hee; Woo, JaeChun; Park, Ji-Young; Yoo, Dae Seok; Bae, Myung Ae
- Issue Date
- 5월-2014
- Publisher
- OXFORD UNIV PRESS INC
- Citation
- JOURNAL OF CHROMATOGRAPHIC SCIENCE, v.52, no.5, pp.406 - 412
- Indexed
- SCIE
SCOPUS
- Journal Title
- JOURNAL OF CHROMATOGRAPHIC SCIENCE
- Volume
- 52
- Number
- 5
- Start Page
- 406
- End Page
- 412
- URI
- https://scholar.korea.ac.kr/handle/2021.sw.korea/98671
- DOI
- 10.1093/chromsci/bmt050
- ISSN
- 0021-9665
- Abstract
- 2-(3-Benzoyl)-4-hydroxy-1,1-dioxo-2H-1,2-benzothiazine-2-yl-1-phenylethanone (KR-66344), a 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) inhibitor, is newly developed for the control of type 2 diabetes mellitus (T2DM) and metabolic syndrome. A method for the determination of KR-66344 in rat plasma was developed by liquid chromatography-electrospray ionization tandem mass spectrometry (LC-ESI-MS-MS) to evaluate the pharmacokinetics of KR-66344. Plasma samples were processed by a liquid-liquid extraction method with ethyl acetate and introduced onto the LC-MS-MS system. The analyte and imipramine (internal standard) were analyzed by multiple reaction monitoring based on transitions at m/z 420.1 -> 105.0 and 282.2 -> 86.0, respectively. The calibration curve was linear (r = 0.9993) over the concentration range of 1.0-1,000 ng/mL. The mean recovery values for KR-66344 and imipramine were 83.8 and 86.2%, respectively. The mean inter-day and intra-day assay precision values were 3.9 and 2.4%, respectively. KR-66344 was stable under various handling and storage conditions. This developed method was applied to a pharmacokinetic study after the oral administration of KR-66344 in rats. The concentration of KR-66344 was readily measurable in rat plasma up to 24 h post-dose after an oral administration, suggesting that current assay is applicable to pharmacokinetic studies for KR-66344.
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