Document Detail


Determination of dicumarol metabolites in bile of rats.
MedLine Citation:
PMID:  50434     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
After intravenous administration of dicumarol-14C to rats, the bile excreted over the next 24 hr contained from 32 to 46% of the administered radioactivity. At least three primary metabolites and a small amount of unchanged dicumarol were present in the bile. Over 91% of the primary metabolites was converted to dicumarol and 7-hydroxydicumarol by hydrolysis with beta-glucuronidase. Some primary metabolites were hydrolyzed simply by acidification to pH 3 or by treatment under the acidic conditions utilized in the enzymatic hydrolysis. The three primary metabolites contain carboxylic acid groups, as indicated by their electrophoretic mobility-pH profiles, and some are simple glucuronides of dicumarol and 7-hydroxydicumarol. The possibility that others are derivatives of these compounds in which a coumarin lactone ring is opened cannot be ruled out. When the metabolites released by either acidification or enzymatic hydrolysis were chromatographed in n-butanol-3 M ammonia, artifacts were produced, presumably as a result of decomposition of 7-hydroxydicumarol. The question is raised whether a previously reported metabolite (B055) is an artifact.
Authors:
W D Conway; F H Lee; L Neufeld
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Publication Detail:
Type:  Journal Article; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Journal of pharmaceutical sciences     Volume:  64     ISSN:  0022-3549     ISO Abbreviation:  J Pharm Sci     Publication Date:  1975 Jul 
Date Detail:
Created Date:  1975-11-07     Completed Date:  1975-11-07     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  2985195R     Medline TA:  J Pharm Sci     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  1158-62     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Animals
Bile / analysis*,  metabolism
Chromatography, Paper
Dicumarol / analogs & derivatives,  analysis*,  metabolism
Electrophoresis, Paper
Feces / analysis
Glucuronidase
Hydrolysis
Male
Radioisotope Dilution Technique
Rats
Chemical
Reg. No./Substance:
66-76-2/Dicumarol; EC 3.2.1.31/Glucuronidase

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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