Identification of non-reported bupropion metabolites in human plasma

Jamie N. Connarn, Ruijuan Luo, Jim Windak, Xinyuan Zhang, Andrew Babiskin, Marisa Kelly, Gloria Harrington, Vicki L. Ellingrod, Masoud Kamali, Melvin McInnis, Duxin Sun

    Research output: Contribution to journalArticlepeer-review

    Abstract

    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.

    Original languageEnglish (US)
    Pages (from-to)550-560
    Number of pages11
    JournalBiopharmaceutics and Drug Disposition
    Volume37
    Issue number9
    DOIs
    StatePublished - Dec 1 2016

    Keywords

    • LC–MS/MS
    • bupropion
    • metabolite identification

    ASJC Scopus subject areas

    • Pharmacology
    • Pharmaceutical Science
    • Pharmacology (medical)

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