Inhibitory Effects of Baicalin on the Expression and Activity of CYP3A Induce the Pharmacokinetic Changes of Midazolam in Rats
Joint Authors
Tian, Xin
Qiao, Hai-Ling
Jin, Han
Gao, Jie
Cheng, Zhen-Yu
Source
Evidence-Based Complementary and Alternative Medicine
Issue
Vol. 2013, Issue 2013 (31 Dec. 2013), pp.1-10, 10 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2013-04-24
Country of Publication
Egypt
No. of Pages
10
Main Subjects
Abstract EN
Baicalin, a flavonoid compound isolated from Scutellaria baicalensis, has been shown to possess antiinflammatory, antiviral, antitumour, and immune regulatory properties.
The present study evaluated the potential herb-drug interaction between baicalin and midazolam in rats.
Coadministration of a single dose of baicalin (0.225, 0.45, and 0.90 g/kg, i.v.) with midazolam (10 mg/kg, i.v.) in rats resulted in a dose-dependent decrease in clearance (CL) from 25% (P<0.05) to 34% (P<0.001) with an increase in AUC0−∞ from 47% (P<0.05) to 53% (P<0.01).
Pretreatment of baicalin (0.90 g/kg, i.v., once daily for 7 days) also reduced midazolam CL by 43% (P<0.001), with an increase in AUC0−∞ by 87% (P<0.01).
Multiple doses of baicalin decreased the expression of hepatic CYP3A2 by approximately 58% (P<0.01) and reduced midazolam 1′-hydroxylation by 23% (P<0.001) and 4′-hydroxylation by 21% (P<0.01) in the liver.
In addition, baicalin competitively inhibited midazolam metabolism in rat liver microsomes in a concentration-dependent manner.
Our data demonstrated that baicalin induced changes in the pharmacokinetics of midazolam in rats, which might be due to its inhibition of the hydroxylation activity and expression of CYP3A in the liver.
American Psychological Association (APA)
Tian, Xin& Cheng, Zhen-Yu& Jin, Han& Gao, Jie& Qiao, Hai-Ling. 2013. Inhibitory Effects of Baicalin on the Expression and Activity of CYP3A Induce the Pharmacokinetic Changes of Midazolam in Rats. Evidence-Based Complementary and Alternative Medicine،Vol. 2013, no. 2013, pp.1-10.
https://search.emarefa.net/detail/BIM-452256
Modern Language Association (MLA)
Tian, Xin…[et al.]. Inhibitory Effects of Baicalin on the Expression and Activity of CYP3A Induce the Pharmacokinetic Changes of Midazolam in Rats. Evidence-Based Complementary and Alternative Medicine No. 2013 (2013), pp.1-10.
https://search.emarefa.net/detail/BIM-452256
American Medical Association (AMA)
Tian, Xin& Cheng, Zhen-Yu& Jin, Han& Gao, Jie& Qiao, Hai-Ling. Inhibitory Effects of Baicalin on the Expression and Activity of CYP3A Induce the Pharmacokinetic Changes of Midazolam in Rats. Evidence-Based Complementary and Alternative Medicine. 2013. Vol. 2013, no. 2013, pp.1-10.
https://search.emarefa.net/detail/BIM-452256
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-452256