opposite effects of single-dose and multidose administration of the ethanol extract of danshen on cyp3a in healthy volunteers

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ID: 216788
2013
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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 Cmax of midazolam to increase by 87% compared with control. After 10 days of the danshen extract intake, the mean AUC0–12, Cmax, and t1/2 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.
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qiu2013evidence-basedopposite Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Furong Qiu, Jian Jiang, Yueming Ma, Guangji Wang, Chenglu Gao, Xinfeng Zhang, Liang Zhang, Songcan Liu, Min He, Leilei Zhu, Yujie Ye, Qiuye Li, Ping Miao
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Journal ACS applied materials & interfaces
Year 2013
DOI
10.1155/2013/730734
URL
http://dx.doi.org/10.1155/2013/730734
Keywords
Other systems of medicine

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