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Identification of nonāreported bupropion metabolites in human plasma
Bupropion and its three active metabolites exhibit clinical efficacy in the treatment of major depression, seasonal depression and smoking cessation. The pharmacokinetics of bupropion in humans is highly variable. It is not known if there are any nonāreported metabolites formed in humans in addition to the three known active metabolites. This paper reports newly identified and nonāreported metabolites of bupropion in human plasma samples. Human subjects were dosed with a single oral dose of 75Ā mg of an immediate release bupropion HCl tablet. Plasma samples were collected and analysed by LCāMS/MS at 0, 6 and 24Ā h. Two nonāreported metabolites (M1 and M3) were identified with massātoācharge (m/z) ratios of 276 (M1, hydration of bupropion) and 258 (M3, hydroxylation of threo/erythrohydrobupropion) from human plasma in addition to the known hydroxybupropion, threo/erythrohydrobupropion and the glucuronidation products of the major metabolites (M2 and M4āM7). These new metabolites may provide new insight and broaden the understanding of bupropionās variability in clinical pharmacokinetics. Ā© 2016 The Authors Biopharmaceutics & Drug Disposition Published by John Wiley & Sons Ltd.Peer Reviewedhttp://deepblue.lib.umich.edu/bitstream/2027.42/134787/1/bdd2046_am.pdfhttp://deepblue.lib.umich.edu/bitstream/2027.42/134787/2/bdd2046.pd