Summary
The pharmacokinetics of fenbufen (3.4-biphenylylcarbonyl propionic acid) a new antiinflammatory agent, and its metabolites, γ-hydroxy-4-biphenylbutyric acid and 4-biphenylacetic acid have been studied after oral administration to seven patients with rheumatoid arthritis. Fenbufen was administered as a single oral dose of 600 mg in hard gelatine capsules. A specific, sensitive gas chromatographic method was used to measure the concentration of the three compounds. A linear two-compartment open model appeared suitable to describe the course of the plasma level of fenbufen with time. This compound appeared in the blood after a lag time of 0.45 h and the peak plasma concentration of 5.97 µg/ml was observed after 1.19 h. The half-life of plasma disappearance was 10.26 h for fenbufen and 10.07 h and at 9.95 h for metabolites II and III, respectively.
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References
Child, R. G., Osterberg, A. C., Sloboda, A. E., Tomoufcik, A. S.: Fenbufen, a new antiinflammatory analgesic: synthesis and structure-activity relationships of analogs. J. Pharm. Sci.66, 466–476 (1977)
Coutinho, A., Bonelli, J., Carvalho, P. C. N.: A double-blind comparative study of analgesic effects of Fenbufen, Codeine, Aspirin, Propoxyphene and placebo. Curr. Ther. Res.19, 58–65 (1976)
Cuisinaud, G., Legheand, J., Belkahia, C., Sassard, J.: Gas chromatographic determination of 3-(4-biphenylylcarbonyl) propionic acid (Fenbufen) and two metabolites in human plasma. J. Chromatogr.148, 509–513 (1978)
De Salcedo, I., Arias, L. F., Greenberg, B. P.: Fenbufen — a new non-steroidal antiinflammatory agent: comparison with Phenylbutazone in rheumatoid arthritis. Curr. Ther. Res.18, 295–302 (1975)
Franklin, R. A.: Some studies on the metabolism of BDH 7538 in animals and man, with particular reference to its antiinflammatory properties. Br. J. Clin. Pharmacol.3, 513–514 (1976)
Mathias-Filho, A. P., Bianchi, W.: A double-blind crossover study of Fenbufen and Indomethacin in patients with rheumatoid arthritis. A Folha Medica71, 459–462 (1975)
Sloboda, A. E., Ostergerg, A. C.: The pharmacology of Fenbufen, 3-(4-biphenylylcarbonyl) propionic acid, and 4-biphenylacetic acid, interesting antiinflammatory-analgesic agents. Inflammation1, 415–438 (1976)
Sunshine, A.: Analgesic value of Fenbufen in post-operative patients. A comparative oral analgesic study of Fenbufen, Aspirin, and placebo. J. clin. Pharmacol.15, 591–597 (1975)
Wagner, J. G.: Biopharmaceutics and Relevant Pharmacokinetics. Hamilton, Il: Drug Intelligence Publications, Hamilton Press 1971
Yamazaki, F.: Evaluation of a study of the analgesic, antiinflammatory and antipyretic effects of Fenbufen on upper respiratory infections, nasal and external auditory canal furuncles. Basic Pharmacol. Ther.3, 183–193 (1975)
Yoshizawa, H., Tada, Y., Naruke, T., Mizumura, M.: Concentration of Fenbufen and its metabolites in human serum. Basic Pharmacol. Ther.2, 31–40 (1974)
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Cuisinaud, G., Legheand, J., Llorca, G. et al. Pharmacokinetics of fenbufen in man. Eur J Clin Pharmacol 16, 59–61 (1979). https://doi.org/10.1007/BF00644968
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DOI: https://doi.org/10.1007/BF00644968