Induction of Cytochrome P450 2B6 Activity by the Herbal Medicine Baicalin As Measured by Bupropion Hydroxylation

Overview

Journal Eur J Clin Pharmacol

Specialty Pharmacology

Date 2008 Dec 11

PMID 19066872

Citations 20

Authors

Lan Fan

Jin-Chao Wang

Feng Jiang

Zhi-Rong Tan

Yao Chen

Qing Li

Wei Zhang

Guo Wang

He-Ping Lei

Dong-Li Hu

Dan Wang

Hong-Hao Zhou

Affiliations

Soon will be listed here.

Abstract

Purpose: 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.

Method: 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.

Result: 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).

Conclusion: Baicalin significantly induced CYP2B6-catalyzed bupropion hydroxylation, and the effects of baicalin on other CYP2B6 substrate drugs deserve further investigation.

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