Identification of Non ‐Reported Bupropion Metabolites in Human Plasma

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 unknown if there are any non‐reported metabolites formed in humans in addition to the three known active metabolites. In this paper, we report 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 analyzed by LC‐MS/MS at 0, 6, and 24 hours. Two non‐reported metabolites (M1 and M3) were identified with mass‐to‐charge (m/z) ratio 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 & M4‐M7). These new metabolites may provide new insight and broaden the understanding of bupropion's variability in clinical pharmacokinetics.
Source: Biopharmaceutics and Drug Disposition - Category: Drugs & Pharmacology Authors: Tags: Original Paper Source Type: research