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Evidence-Based Complementary and Alternative Medicine
Volume 2013 (2013), Article ID 730734, 8 pages
http://dx.doi.org/10.1155/2013/730734
Research Article

Opposite Effects of Single-Dose and Multidose Administration of the Ethanol Extract of Danshen on CYP3A in Healthy Volunteers

1Lab of Clinical Pharmacokinetics, Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China
2Lab of Pharmacokinetics, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China
3Key Lab of Drug Metabolism & Pharmacokinetics, China Pharmaceutics University, Nanjing 210038, China

Received 10 April 2013; Revised 13 July 2013; Accepted 27 August 2013

Academic Editor: Moses S. S. Chow

Copyright © 2013 Furong Qiu et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

The aim of this study was to investigate the effect of single- and multidose administration of the ethanol extract of danshen on in vivo CYP3A activity in healthy volunteers. A sequential, open-label, and three-period pharmacokinetic interaction study design was used based on 12 healthy male individuals. The plasma concentrations of midazolam and its metabolite 1-hydroxymidazolam were measured. Treatment with single dose of the extract caused the mean of midazolam to increase by 87% compared with control. After 10 days of the danshen extract intake, the mean AUC , , and of midazolam were decreased by 79.9%, 66.6%, and 43.8%, respectively. The mean clearance of midazolam was increased by 501.6% compared with control. The in vitro study showed that dihydrotanshinone I in the extract could inhibit CYP3A, while tanshinone IIA and cryptotanshinone could induce CYP3A. In conclusion, a single-dose administration of the danshen extract can inhibit intestinal CYP3A, but multidose administration can induce intestinal and hepatic CYP3A.