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The pharmacokinetics of the enantiomers of ketoprofen after oral administration of 12.5 mg, 25 mg and 50 mg and i.v. administration of 50 mg racemic ketoprofen to 24 healthy subjects were investigated. The AUC values of R- (r2 = 0.929) and S-ketoprofen (r2 = 0.930) were proportional to dose. The absolute bioavailability of the 50 mg oral dose was 84.5 (s.d. 20.6) % and 81.4 (18.0) % for R-ketoprofen and S-ketoprofen, respectively. With the exception of AUC values no dose dependent differences in pharmacokinetic parameters were observed. However, the R-enantiomer had higher AUC, lower clearance data and higher Cmax values than the S-form after oral administration. The results suggest that stereochemical and pharmacokinetic considerations cannot explain the lack of dose response observed with ketoprofen doses below 50 mg.