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Stereoselective Pharmacokinetics and Inversion of (R)‐ Ketoprofen in Healthy Volunteers
Author(s) -
Rudy Anita C.,
Liu Yingxian,
Brater D. Craig,
Hall Stephen D.
Publication year - 1998
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/j.1552-4604.1998.tb04411.x
Subject(s) - ketoprofen , pharmacokinetics , enantiomer , urine , cmax , pharmacology , chemistry , stereoselectivity , anesthesia , medicine , stereochemistry , biochemistry , catalysis
The pharmacokinetics of ketoprofen enantiomers were evaluated after 25‐, 50‐, and 100‐mg doses of (R)‐ ketoprofen and 100 mg of racemic ketoprofen in 25 healthy volunteers (12 male and 13 female). The fractional inversion (F inv ) of (R)‐ ketoprofen was 8.9 ± 3.3% using plasma data and 10.0 ± 2.2% using urine data. There were small (<5%) but significant differences between the enantiomers for areas under the plasma concentration‐time curve (AUC) after the racemic dose (P < 0.005). Half‐lives were 130–144 minutes for (R)‐ ketoprofen and 132–209 minutes for (S)‐ ketoprofen. Dose proportionality in AUC and maximum plasma concentration (C max ) values was noted for both enantiomers. A total of 69% of the dose was recovered in the urine as (R)‐ and (S)‐ ketoprofen and conjugates. The elimination rate constant of (R)‐ ketoprofen was significantly different (P < 0.05) between men and women. Exposure to cyclooxygenase inhibiting (S)‐ ketoprofen was approximately 10% of the dose after the administration of pure (R)‐ ketoprofen and was independent of gender. J Clin Pharmacol 1998;38:3S‐10S.