The effects of sodium ferulate on the pharmacokinetics of bupropion and its active metabolite in healthy men

摘要

AIMS: Sodium ferulate (SF) is widely prescribed in clinic for the treatments of cardiovascular and cerebrovascular diseases. In our study, we investigated the effect of SF on the pharmacokinetics of bupropion and its active metabolite 4-Hydroxybupropion in healthy Chinese men. METHODS: In a two-Phase, randomized, crossover study with a 2-Week wash-Out period between phases, nineteen healthy male volunteers were given with or without pretreatment with SF 150 mg three times daily for fourteen days, and a single dose of bupropion 150 mg was administered. Pharmacokinetics profiles for bupropion and 4-Hydroxybupropion were determined. RESULTS: After SF treatment relative to bupropion alone, the geometric mean ratios and 90% confidence interval of 4-Hydroxybupropion were 1.25 (1.17, 1.34) for AUC0-??, 1.10 (1.05, 1.15) for Cmax, and 1.14 (1.09, 1.20) for t1/2 respectively. The corresponding values for bupropion were 0.907 (0.811, 1.014), 0.974 (0.910, 1.045) and 1.13 (1.06, 1.21) respectively. The corresponding values for AUC0-?? ratio of 4-Hydroxybupropion over bupropion were 1.28 (0.811, 1.014). CONCLUSIONS, Bupropion hydroxylation was slightly induced by the 14 days of SF pre-Treatment. Whether co-Administration with SF require a dosage adjustment of bupropion needs further exploration.