Stereoselective disposition of flurbiprofen in healthy subjects following administration of the single enantiomers.

Plasma concentrations of the enantiomers of flurbiprofen were measured following oral administration of (S)‐flurbiprofen 50 mg and (R)‐ flurbiprofen 50 mg and 100 mg to sixteen healthy subjects. Chiral inversion did not occur to a measurable extent. Significantly higher values of AUC (55.2 +/‐ 17.0 vs 44.6 +/‐ 11.2 micrograms ml‐1h) elimination half‐life (5.6 +/‐ 1.4 vs 4.0 +/‐ 1.0 h) and mean residence time (7.5 +/‐ 1.6 vs 5.7 +/‐ 1.2 h) were observed after 50 mg (S)‐ flurbiprofen as compared with 50 mg (R)‐flurbiprofen. With the exception of Cmax and AUC values pharmacokinetic data for the 50 mg and the 100 mg dose of (R)‐flurbiprofen did not differ significantly. The data are of clinical relevance if (R)‐flurbiprofen also has analgesic activity in humans and is to be developed as an analgesic.

DOI: 10.1111/j.1365-2125.1994.tb04295.x

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