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European Journal of Clinical Pharmacology

, Volume 31, Issue 3, pp 307–311 | Cite as

Transsynovial distribution and protein binding of pirazolac in patients with rheumatoid arthritis

  • M. Kurowski
  • A. Dunky
  • M. Geddawi
Originals

Summary

Following a washout period of 7 days, twenty-one patients suffering from rheumatoid arthritis and 3 from osteo-arthritis, who all required articular puncture were given a non-steroidal anti-inflammatory drug pirazolac 450 mg b.d. for 7 days. After discontinuation of the treatment the subjects were divided into 4 groups each of 6 patients.

The non protein bound fraction of pirazolac in synovial fluid (0.86%) was significantly higher than that in plasma (0.53%). The average pirazolac concentration in plasma within the dosing interval fluctuated between 30.9 µg/ml and 59 µg/ml, and in synovial fluid between 16.6 µg/ml and 29.9 µg/ml. The half-life of pirazolac calculated from the measured and interpolated data from all patients was 30.9 h in plasma and 66.2 h in synovial fluid. The absolute free concentrations in plasma and synovial fluid (approx. 250 ng/ml) were in the range of the IC50-values for inhibition of cyclooxygenase in mouse peritoneal macrophages.

Key words

pirazolac rheumatoid arthritis transsynovial distribution synovial fluid drug level pharmacokinetics protein binding 

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Copyright information

© Springer-Verlag 1986

Authors and Affiliations

  • M. Kurowski
    • 1
    • 4
  • A. Dunky
    • 2
  • M. Geddawi
    • 3
  1. 1.Institut für Pharmazie der Freien Universität BerlinBerlinGermany
  2. 2.Krankenhaus der Stadt WienLainzAustria
  3. 3.Schering AGBerlinGermany
  4. 4.Institut für Pharmakologie und Toxikologie der Friedrich-Alexander-Universität Erlangen-NürnbergErlangenFederal Republic of Germany

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