PMID: 7082777Jan 1, 1982Paper

The pharmacokinetics and metabolism of 14C-carprofen in man

Biopharmaceutics & Drug Disposition
J E Ray, D N Wade

Abstract

Three healthy male subjects received single 100 mg oral doses of carprofen containing 20 microCi of 14C-carprofen. Venous blood samples were drawn during the first 48 h after the dose and urine and faeces were collected for 120 h. Concentrations of carprofen and its metabolites in body fluids were determined by TLC and mass spectral analysis. After a lag time of 0.3 +/- 0.1 h (mean +/- S.D.), carprofen was absorbed rapidly and peak concentrations in the plasma were reached in 2.7 +/- 1.3 h. The 14C plasma concentrations declined in a biphasic fashion. The mean half-lives of the initial (alpha) and terminal (beta) phases were 1.1 h and 20.6 +/- 6.1 h, respectively. Biotransformation to a glucuronide metabolite appeared to be the major mechanism of carprofen clearance. In 48 h 74.0 per cent of administered radioactivity was recovered in urine and 14.1 per cent was recovered in faeces. A glucuronide of carprofen comprised 85.0 per cent of the radiolabelled compounds in urine. The remaining radioactivity was comprised of parent drug (12.0 per cent) and un unidentified acid-labile conjugate of the parent drug (3.0 per cent). This pattern of metabolism and excretion is different from that in the dog and rat and may explain species di...Continue Reading

References

Oct 1, 1979·Journal of Clinical Pharmacology·J E RayR O Day
Jun 1, 1977·Clinical Pharmacology and Therapeutics·R C LudersC Li
Jan 1, 1974·Current Medical Research and Opinion·A RubinA S Ridolfo
Nov 1, 1980·Journal of Pharmaceutical Sciences·F RubioB Koechlin

Citations

Jun 9, 2001·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·K WaltonA G Renwick
Nov 7, 2001·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·J L DorneA G Renwick
Nov 7, 2001·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·K WaltonA G Renwick
Jul 17, 1998·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·R Maire-GauthierE Benoit
Sep 1, 1989·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·J A ScatinaM N Cayen
Mar 1, 1985·Journal of Clinical Pharmacology·A A HolazoR K Brazzell

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