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SONG Lin, WANG Mao, WEN Aidong, YANG Lin, JIA Yuntao, XIE Huiru, JIANG Xuehua, WANG Ling. Determination of agomelatine in human plasma by LC-MS/MS:application to a pharmacokinetic study in Chinese volunteers[J]. Journal of China Pharmaceutical University, 2014, 45(6): 698-702. DOI: 10.11665/j.issn.1000-5048.20140615
Citation: SONG Lin, WANG Mao, WEN Aidong, YANG Lin, JIA Yuntao, XIE Huiru, JIANG Xuehua, WANG Ling. Determination of agomelatine in human plasma by LC-MS/MS:application to a pharmacokinetic study in Chinese volunteers[J]. Journal of China Pharmaceutical University, 2014, 45(6): 698-702. DOI: 10.11665/j.issn.1000-5048.20140615

Determination of agomelatine in human plasma by LC-MS/MS:application to a pharmacokinetic study in Chinese volunteers

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  • To establish an LC-MS/MS method for the determination of agomelatine in human plasma and to study the pharmacokinetics in Chinese healthy volunteers following oral administration of agomelatine tablets. 72 volunteers were administered with single oral dose of 25 mg of agomelatine. The plasma concentration of agomelatine was determined by LC-MS/MS. The pharmacokinetic parameters were calculated by Phoenix WinNonlin 6. 3. 0. The calibration curve of agomelatine was linear over the range of 0. 051 3-10. 38 ng/mL(r=0. 999 4). The lower limit of quantification of agomelatine was 0. 051 3 ng/mL. Both intra- and inter-day RSD were less than 15%. The main pharmacokinetic parameters were as follows: cmax was(13. 25±15. 78)ng/mL; tmax was(0. 68±0. 41)h; AUClast was(14. 00±19. 26)ng/mL ·h; AUCinf was(14. 14±19. 35)ng/mL ·h and t1/2 was(0. 78±0. 44)h. The LC/MS/MS method was convenient, precise and reproducible. It can be used for the determination of agomelatine in human plasma and its clinical pharmacokinetic studies.
  • [1]
    Wang X, Ma HM, Zhou YS. The graphical synthetic routes of agomelatine[J].Chin J Med Chem(中国药物化学杂志),2012,99(4):334-336.
    [2]
    Landolt HP,Wehrle R.Antagonism of serotonergic 5-HT2A/2C receptors:mutual improvement of sleep,cognition and mood[J].Eur J Neurosci,2009,29(9):1 795-1 809.
    [3]
    Howland RH.Critical appraisal and update on the clinical utility of agomelatine,a melatonergic agonist,for the treatment of major depressive disease in adults[J].Neuropsychiatr Dis Treat,2009,5:563-576.
    [4]
    Millan M,Gobert A,Lejeune F,et al.The novel melatonin agonist agomelatine(S20098)is an antagonist at 5-hydroxytryptamine 2C receptors,blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways[J].J Pharmacol Exp Ther,2003,306(3):954-964.
    [5]
    Banasr M,Soumier A,Hery M,et al.Agomelatine,a new antidepressant,induces regional changes in hippocampal neurogenesis[J].Biol Psychiatry,2006,59(11):1 087-1 096.
    [6]
    Wei MJ,Zhang ZF,Zhang ZF.Discussion on accuracy in the analysis of biological samples and improvement measures[EB/OL].(2012-04-11)[2012-09-30] .http://www.cde.org.cn/dzkw.do?method=largePage&id=312642.
    [7]
    European Medicines Agency. CHMP ASSESSMENT REPORT FOR Valdoxan[EB/OL].(2008-11-20)[2011-12-12] .http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/000915/WC500046226.pdf.
    [8]
    European Medicines Agency.Guideline on the investigation of bioequivalence[EB/OL].(2010-01-20)[2011-12-12] .http://www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2010/01/WC500070039.pdf.
    [9]
    Chow SC,Liu J.Design and Analysis of Bioavailability and Bioequivalence Studies[M].CRC Press,2000.
    [10]
    Patil SR,Nerurkar KK,Kalamkar AM,et al.Validated LC-MS/MS method for quantification of agomelatine in human plasma and its application in a pharmacokinetic study[J].J Mass Spectrom,2012,47(1):23-28.

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