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. 1988 Dec;26(6):765–770. doi: 10.1111/j.1365-2125.1988.tb05317.x

The disposition of ketoprofen enantiomers in man.

B C Sallustio 1, Y J Purdie 1, A G Whitehead 1, M J Ahern 1, P J Meffin 1
PMCID: PMC1386593  PMID: 3242582

Abstract

1. The disposition of ketoprofen enantiomers was studied in 21 patients taking racemic ketoprofen (Orudis SR). 2. In each patient the plasma concentrations of the R- and S-enantiomers were similar at all times over a 24 h dosing interval. The mean (+/- s.e. mean) time-averaged plasma ketoprofen concentrations over the dosage interval were 0.76 (+/- 0.06) mg l-1 for R-ketoprofen and 0.78 (+/- 0.06) mg l-1 for S-ketoprofen. 3. Creatinine clearances for the 21 patients ranged from 6-162 ml min-1. There was no correlation between creatinine clearance and time-averaged plasma concentration for either R- or S-ketoprofen. 4. Approximately 30% of the dose was recovered in urine (unconjugated + glucuronide conjugate) and this was made up of 43% R-ketoprofen and 57% S-ketoprofen. Because of incomplete urine recoveries of ketoprofen it was not possible to determine whether inversion from the R- to the S-enantiomer takes place in man. 5. The data suggest that in terms of total (bound + unbound) ketoprofen, half the concentration value derived by a non-enantiospecific analysis would give a reasonable approximation of the pharmacologically active S-enantiomer concentration in plasma.

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Selected References

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