European Journal of Clinical Pharmacology

, Volume 38, Issue 5, pp 493–497 | Cite as

Pharmacokinetics of S(+)- and R(−)-ibuprofen in volunteers and first clinical experience of S(+)-ibuprofen in rheumatoid arthritis

  • G. Geisslinger
  • O. Schuster
  • K. -P. Stock
  • D. Loew
  • G. L. Bach
  • K. Brune


S(+)-, R(−)- or racemic ibuprofen was administered orally to volunteers in doses of 150 mg, 300 mg and 500 mg pure S(+)-, 300 mg pure R(−)- and 600 mg racemic ibuprofen.

The pharmacokinetic parameters in humans showed that S(+)-ibuprofen was not inverted to R(−)-ibuprofen, whereas R(−)-ibuprofen was inverted to S(+)-ibuprofen to a variable degree. S(+)-ibuprofen and R(−)-ibuprofen given alone more rapidly reached significantly higher maximal plasma concentrations than after the same doses of the racemic compound. The elimination half-lives and clearance values for all three forms of ibuprofen were comparable. The mean residence time of S(+)-ibuprofen after R(−)- and racemic ibuprofen was significantly longer than after administration of the pure S(+)-enantiomer.

Judged by the AUC, the bioavailability of S(+)-ibuprofen was independent of the dose within the range tested.

Administration of S(+)-ibuprofen to 6 rheumatic patients showed that the pharmacokinetic behaviour of S(+)-ibuprofen in patients was similar to that found in volunteers. S(+)-ibuprofen proved to be an effective analgesic antirheumatic drug in the dose range 1 to 1.5 g/day.

Key words

ibuprofen rheumatoid arthritis enantiomer stereoselectivity pharmacokinetics 


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Copyright information

© Springer-Verlag 1990

Authors and Affiliations

  • G. Geisslinger
    • 1
  • O. Schuster
    • 2
  • K. -P. Stock
    • 3
  • D. Loew
    • 4
  • G. L. Bach
    • 3
  • K. Brune
    • 1
  1. 1.Department of Pharmacology and ToxicologyUniversity of ErlangenErlangenGermany
  2. 2.PAZ Arzneimittelentwicklungsgesellschaft mbHFrankfurt/MainGermany
  3. 3.Klinik HerzoghoeheBayreuthGermany
  4. 4.KaternbergerstraßeWuppertalGermany

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