The absolute bioavailability investigation of LS177 in rats using ultra-performance liquid chromatography-tandem mass spectrometry

Drug Testing and Analysis
Lunhui ZhangXiaohui Chen

Abstract

LS177 is a novel inhibitor of mesenchymal epithelial transition (MET) that was used as an anticancer agent. The present study was to evaluate the absolute bioavailability of LS177 in rats. A rapid and sensitive ultra-high performance liquid chromatography-mass spectrometry (UHPLC-MS/MS) method has been developed and validated for the determination of LS177 in rat plasma. LS177 and internal standard (IS, LS410) were extracted from rat plasma samples by protein precipitation (PPT) for intravenous group and liquid-liquid extraction (LLE) procedure for oral group, then separated on a Phenomenex Kinetex XB-C18 (2.1 mm I.D. × 50 mm, 2.6 µm) using a mobile phase consisting of 0.1% formic acid in acetonitrile-0.1% formic acid water with a gradient elution program. The standard curves were linear over the ranges of 5.0-2000.0 ng · mL(-1) for PPT and 1.0-200.0 ng · mL(-1) for LLE. The mean recovery of LS177 was greater than 83.4% for PPT and not less than 88.5% for LLE, respectively. The intra- and inter-day accuracy and precision were within the acceptable limits of less than 15.0% at all concentrations. The validated method was successfully applied to the bioavailability study in rat plasma of LS177 and its absolute bioavailability was...Continue Reading

References

Apr 1, 1980·Journal of Pharmaceutical Sciences·P V Pedersen, R Miller
Dec 20, 2003·Nature Reviews. Molecular Cell Biology·Carmen BirchmeierGeorge F Vande Woude
Feb 7, 2007·Antimicrobial Agents and Chemotherapy·Olanrewaju OkusanyaUNKNOWN ACTG 5043 Protocol Team
May 31, 2008·Nature Reviews. Drug Discovery·Paolo M ComoglioLivio Trusolino
Jun 14, 2008·Expert Opinion on Investigational Drugs·Xiangdong LiuPeggy A Scherle
Mar 26, 2009·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Joseph Paul EderPatricia M LoRusso
Jul 25, 2009·Hepatology Research : the Official Journal of the Japan Society of Hepatology·Akio Ido, Hirohito Tsubouchi
Dec 18, 2009·Anti-cancer Agents in Medicinal Chemistry·Ted L UnderinerSheila J Miknyoczki
Jan 27, 2010·Expert Opinion on Therapeutic Patents·John Porter
May 9, 2012·Nature Reviews. Clinical Oncology·Solange Peters, Alex A Adjei
Dec 6, 2012·Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology·Toni K ChoueiriRamaprasad Srinivasan

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