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Identification of non‐reported bupropion metabolites in human plasma
Author(s) -
Connarn Jamie N.,
Luo Ruijuan,
Windak Jim,
Zhang Xinyuan,
Babiskin Andrew,
Kelly Marisa,
Harrington Gloria,
Ellingrod Vicki L.,
Kamali Masoud,
McInnis Melvin,
Sun Duxin
Publication year - 2016
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.2046
Subject(s) - bupropion , pharmacokinetics , pharmacology , glucuronidation , active metabolite , metabolite , chemistry , biopharmaceutics , hydroxylation , drug , medicine , smoking cessation , microsome , biological activity , biochemistry , pharmacognosy , enzyme , pathology , in vitro
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 non‐reported metabolites formed in humans in addition to the three known active metabolites. This paper reports newly identified and non‐reported metabolites of bupropion in human plasma samples. Human subjects were dosed with a single oral dose of 75 mg of an immediate release bupropion HCl tablet. Plasma samples were collected and analysed by LC–MS/MS at 0, 6 and 24 h. Two non‐reported metabolites (M1 and M3) were identified with mass‐to‐charge ( 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 M4–M7). These new metabolites may provide new insight and broaden the understanding of bupropion's variability in clinical pharmacokinetics. © 2016 The Authors Biopharmaceutics & Drug Disposition Published by John Wiley & Sons Ltd.