radafaxine and baicalin

This study investigated the effect of the herbal medicine baicalin on bupropion hydroxylation, a probe reaction for CYP2B6 activity related to different CYP2B6 genotype groups.. Seventeen 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.. Baicalin administration increased hydroxybupropion maximum plasma concentration (C(max)) by 73% [90% confidence interval (CI), 44-108%; P < 0.01] and the area under the concentration time curve extrapolated to infinity (AUC(0-infinity)) of hydroxybupropion by 87% (90% CI, 48-137%; P < 0.01), with no change in the elimination half-life of hydroxybupropion. Baicalin increased the AUC(0-infinity) ratio of hydroxybupropion to bupropion by 63% (90% CI, 38-92%; P < 0.01).. Baicalin significantly induced CYP2B6-catalyzed bupropion hydroxylation, and the effects of baicalin on other CYP2B6 substrate drugs deserve further investigation.

Topics: Adult; Area Under Curve; Aryl Hydrocarbon Hydroxylases; Bupropion; Cytochrome P-450 CYP2B6; Dopamine Uptake Inhibitors; Enzyme Induction; Flavonoids; Glucuronidase; Haplotypes; Herb-Drug Interactions; Humans; Hydroxylation; Male; Oxidoreductases, N-Demethylating; Plant Extracts; Polymorphism, Single Nucleotide; Time Factors