L. Fan, Jin-Chao Wang, F. Jiang
Apr 1, 2009
Citations
1
Influential Citations
49
Citations
Quality indicators
Journal
European Journal of Clinical Pharmacology
Abstract
PurposeThis study investigated the effect of the herbal medicine baicalin on bupropion hydroxylation, a probe reaction for CYP2B6 activity related to different CYP2B6 genotype groups.MethodSeventeen healthy male volunteers (6 CYP2B6*1/*1, 6 CYP2B6*1/*6, and 5 CYP2B6*6/*6) received orally administered bupropion alone and during daily treatment with baicalin. Blood samples were taken up to 72 h after each bupropion dose, and pharmacokinetics profiles were determined on days 1 and 25 for bupropion and hydroxybupropion.ResultBaicalin administration increased hydroxybupropion maximum plasma concentration (Cmax) by 73% [90% confidence interval (CI), 44–108%; P < 0.01] and the area under the concentration time curve extrapolated to infinity (AUC0–∞) of hydroxybupropion by 87% (90% CI, 48–137%; P < 0.01), with no change in the elimination half-life of hydroxybupropion. Baicalin increased the AUC0–∞ ratio of hydroxybupropion to bupropion by 63% (90% CI, 38–92%; P < 0.01).ConclusionBaicalin significantly induced CYP2B6-catalyzed bupropion hydroxylation, and the effects of baicalin on other CYP2B6 substrate drugs deserve further investigation.