| Identification of mebeverine acid as the main circulating metabolite of mebeverine in man. | |
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MedLine Citation:
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PMID: 12062694 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The intestinal spasmolytic drug mebeverine is known to undergo fast in vivo enzymatic hydrolysis into mebeverine alcohol and veratric acid. A reversed-phase HPLC method with coulometric detection was developed in order to assay the hitherto unidentified secondary metabolite mebeverine acid. After intake of a single oral dose of 405 mg mebeverine hydrochloride in four healthy human volunteers, peak plasma concentrations of mebeverine acid were found to be 1000-fold higher than those of mebeverine alcohol, i.e. approximately 3 microg/ml versus 3 ng/ml. The appearance of mebeverine acid in plasma (median T(max)=1.25 h) as well as its disappearance (median apparent t(1/2)=1.1 h) were rapid. The urinary excretion of mebeverine acid within the first 4 h after dosing amounted to 67% of the mebeverine dose (median range: 23-107%). Mebeverine acid appears to be a valuable marker of oral exposure to mebeverine. |
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Authors:
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Arnel Stockis; P J M Guelen; D de Vos |
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Publication Detail:
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Type: Clinical Trial; Journal Article |
Journal Detail:
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Title: Journal of pharmaceutical and biomedical analysis Volume: 29 ISSN: 0731-7085 ISO Abbreviation: J Pharm Biomed Anal Publication Date: 2002 Jun |
Date Detail:
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Created Date: 2002-06-13 Completed Date: 2002-07-23 Revised Date: 2004-11-17 |
Medline Journal Info:
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Nlm Unique ID: 8309336 Medline TA: J Pharm Biomed Anal Country: England |
Other Details:
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Languages: eng Pagination: 335-40 Citation Subset: IM |
Affiliation:
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SGS Biopharma S.A., 1301 Bierges, Belgium. arnel.stockis@ucb-group.com |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Administration, Oral Adult Anticonvulsants / administration & dosage, metabolism*, pharmacokinetics Area Under Curve Chromatography, High Pressure Liquid Half-Life Humans Male Phenethylamines / administration & dosage, blood*, metabolism*, pharmacokinetics, urine |
| Chemical | |
Reg. No./Substance:
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0/Anticonvulsants; 0/Phenethylamines; 14367-47-6/mebeverine alcohol; 3625-06-7/mebeverine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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