PMID: 7082777Jan 1, 1982Paper

The pharmacokinetics and metabolism of 14C-carprofen in man

Biopharmaceutics & Drug Disposition
J E Ray, D N Wade


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


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