| Studies on interactions between functional foods or dietary supplements and medicines. I. Effects of Ginkgo biloba leaf extract on the pharmacokinetics of diltiazem in rats. | |
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MedLine Citation:
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PMID: 12951478 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The effects of Ginkgo biloba leaf extract (GBE), one of the most widely used herbal dietary supplements in Japan, on the pharmacokinetics of diltiazem (DTZ), a typical probe of cytochrome P450 (CYP) 3A, were examined in rats. The simultaneous addition of GBE to small intestine and liver microsomes inhibited the formation of N-demethyl DTZ (MA), an active metabolite of DTZ produced by CYP3A, in a concentration-dependent manner, with an IC(50) of about 50 and 182 microg/ml, respectively. This inhibition appeared to be caused, at least in part, by a mechanism-based inhibition. Both the rate of formation of MA and total amount of CYP in intestinal or hepatic microsomes after a single oral pretreatment with GBE (20 mg/kg) decreased transiently. The pretreatment significantly decreased the terminal elimination rate constant and increased the mean residence time, after intravenous administration of DTZ (3 mg/kg). Furthermore, it significantly increased the area under the concentration-time curve and absolute bioavailability after oral administration of DTZ (30 mg/kg). These results indicated that the concomitant use of GBE in rats increased the bioavailability of DTZ by inhibiting both intestinal and hepatic metabolism, at least in part, via a mechanism-based inhibition for CYP3A. |
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Authors:
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Noriaki Ohnishi; Mayako Kusuhara; Mutsunobu Yoshioka; Kazuo Kuroda; Akihiro Soga; Fumi Nishikawa; Tomokazu Koishi; Masato Nakagawa; Satoshi Hori; Tsuyoshi Matsumoto; Masayuki Yamashita; Shunsaku Ohta; Koji Takara; Teruyoshi Yokoyama |
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Publication Detail:
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Type: In Vitro; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Biological & pharmaceutical bulletin Volume: 26 ISSN: 0918-6158 ISO Abbreviation: Biol. Pharm. Bull. Publication Date: 2003 Sep |
Date Detail:
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Created Date: 2003-09-02 Completed Date: 2004-04-09 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 9311984 Medline TA: Biol Pharm Bull Country: Japan |
Other Details:
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Languages: eng Pagination: 1315-20 Citation Subset: IM |
Affiliation:
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Faculty of Pharmaceutical Sciences, Kyoto Pharmaceutical University, Kyoto, Japan. ohnishi@mb.kyoto-phu.ac.jp |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Administration, Oral Animals Area Under Curve Aryl Hydrocarbon Hydroxylases / antagonists & inhibitors Calcium Channel Blockers / administration & dosage, pharmacokinetics* Cytochrome P-450 CYP3A Cytochromes b5 / metabolism Diltiazem / administration & dosage, pharmacokinetics* Drug Interactions Enzyme Inhibitors / pharmacology Ginkgo biloba / chemistry* Half-Life Injections, Intravenous Intestine, Small / drug effects, enzymology, metabolism Male Methylation Microsomes / drug effects, enzymology, metabolism Microsomes, Liver / drug effects, enzymology, metabolism Oxidoreductases, N-Demethylating / antagonists & inhibitors Plant Extracts / pharmacology Rats Rats, Wistar |
| Chemical | |
Reg. No./Substance:
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0/Calcium Channel Blockers; 0/Enzyme Inhibitors; 0/Plant Extracts; 42399-41-7/Diltiazem; 9035-39-6/Cytochromes b5; EC 1.14.14.1/Aryl Hydrocarbon Hydroxylases; EC 1.14.14.1/Cytochrome P-450 CYP3A; EC 1.5.-/Oxidoreductases, N-Demethylating |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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