Document Detail


Identification of mebeverine acid as the main circulating metabolite of mebeverine in man.
MedLine Citation:
PMID:  12062694     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Arnel Stockis; P J M Guelen; D de Vos
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Publication Detail:
Type:  Clinical Trial; Journal Article    
Journal Detail:
Title:  Journal of pharmaceutical and biomedical analysis     Volume:  29     ISSN:  0731-7085     ISO Abbreviation:  J Pharm Biomed Anal     Publication Date:  2002 Jun 
Date Detail:
Created Date:  2002-06-13     Completed Date:  2002-07-23     Revised Date:  2004-11-17    
Medline Journal Info:
Nlm Unique ID:  8309336     Medline TA:  J Pharm Biomed Anal     Country:  England    
Other Details:
Languages:  eng     Pagination:  335-40     Citation Subset:  IM    
Affiliation:
SGS Biopharma S.A., 1301 Bierges, Belgium. arnel.stockis@ucb-group.com
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MeSH Terms
Descriptor/Qualifier:
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:
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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