Document Detail

Directly-coupled HPLC-NMR spectroscopic studies of metabolism and futile deacetylation of phenacetin in the rat.
MedLine Citation:
PMID:  10746955     Owner:  NLM     Status:  MEDLINE    
The metabolism and futile deacetylation of phenacetin has been investigated in the rat via 1H NMR spectroscopic analysis of urine. Animals were dosed with either phenacetin or phenacetin-C2H3 and urine samples were collected for -24-0 (pre-dosing), 0-8. 8-24, and 24-48 h post-dosing. Drug metabolites of the two compounds were concentrated from the urine using solid-phase extraction prior to the use of directly-coupled HPLC-1H NMR spectroscopy for separation and identification. Following dosing of phenacetin, the metabolites identified were paracetamol glucuronide, paracetamol and N-hydroxyparacetamol, whilst paracetamol and N-hydroxyparacetamol sulphate were identified following dosing of phenacetin-C2H3. Quantitatively the percentage futile deacetylation of phenacetin-C2H3 metabolites was found to be 32% in both paracetamol and N-hydroxyparacetamol sulphate. This study further indicated the importance of futile deacetylation in simple analgesics and the value of directly-coupled HPLC-NMR spectroscopy for the study of this process.
A W Nicholls; J C Lindon; R D Farrant; J P Shockcor; I D Wilson; J K Nicholson
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of pharmaceutical and biomedical analysis     Volume:  20     ISSN:  0731-7085     ISO Abbreviation:  J Pharm Biomed Anal     Publication Date:  1999 Sep 
Date Detail:
Created Date:  2000-05-16     Completed Date:  2000-05-16     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  8309336     Medline TA:  J Pharm Biomed Anal     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  865-73     Citation Subset:  IM    
Section of Biological Chemistry, Imperial College of Science, Technology and Medicine, London, UK.
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MeSH Terms
Acetaminophen / urine
Analgesics, Non-Narcotic / metabolism*,  urine
Chromatography, High Pressure Liquid
Injections, Intraperitoneal
Magnetic Resonance Spectroscopy
Phenacetin / metabolism*
Reg. No./Substance:
0/Analgesics, Non-Narcotic; 103-90-2/Acetaminophen; 62-44-2/Phenacetin

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