The pharmacokinetics of the enantiomers of flurbiprofen in patients with rheumatoid arthritis.
Open Access
- 1 January 1991
- journal article
- Published by Wiley in British Journal of Clinical Pharmacology
- Vol. 31 (1) , 102-104
- https://doi.org/10.1111/j.1365-2125.1991.tb03865.x
Abstract
Plasma and synovial fluid concentrations of the enantiomers of flurbiprofen were measured in 15 rheumatoid patients receiving 100 mg racemic flurbiprofen twice daily. Pharmacokinetic parameters showed considerable variability within the group of patients, although differences in S(+)/R(-) plasma concentration ratios were small. The average values (+/− s.d.) of oral plasma clearance, volume of distribution and elimination half-life for R(-)-flurbiprofen were 0.075 (+/− 0.066) l min-1, 12.47 (+/− 5.79) l and 138 (+/− 61) min, respectively. The average values (+/− s.d.) of oral plasma clearance, volume of distribution and elimination half-life for S(+)-flurbiprofen were 0.057 (+/− 0.035) l min-1, 12.81 (+/− 4.43) l and 155 (+/− 49) min, respectively. S(+)/R(-) ratios (+/− s.d.) rose from 1.06 (+/− 0.12) to 1.75 (+/− 0.61) at the end of the 12 h interval in plasma and from 1.18 (+/− 0.13) to 1.47 (+/− 0.24) over the measured time course in synovial fluid. Increases in S(+)/R(-) ratios may be clinically important as they demonstrate accumulation of the pharmacologically active species.Keywords
This publication has 16 references indexed in Scilit:
- The metabolic chiral inversion and dispositional enantioselectivity of the 2-arylpropionic acids and their biological consequencesBiochemical Pharmacology, 1988
- Plasma and synovial fluid kinetics of flurbiprofen in rheumatoid arthritis.British Journal of Clinical Pharmacology, 1986
- Stereochemistry, a basis for sophisticated nonsense in pharmacokinetics and clinical pharmacologyEuropean Journal of Clinical Pharmacology, 1984
- High-performance liquid chromatographic separation of the enantiomers of anti-inflammatory 2-arylpropionates: suitability of the method for in vitro metabolic studiesJournal of Chromatography A, 1984
- The metabolic chiral inversion of 2-arylpropionic acids—a novel route with pharmacological consequencesJournal of Pharmacy and Pharmacology, 1983
- Dose‐response study with ibuprofen in rheumatoid arthritis: clinical and pharmacokinetic findings.British Journal of Clinical Pharmacology, 1983
- Inhibition of prostaglandin synthesis and leucocyte migration by flurbiprofenCurrent Medical Research and Opinion, 1977
- Pharmacological differences between the optical isomers of ibuprofen: evidence for metabolic inversion of the (—)-isomerJournal of Pharmacy and Pharmacology, 1976
- GLC Determination of Ibuprofen [(±)-2-(p-Isobutylphenyl)propionic Acid] in PlasmaJournal of Pharmaceutical Sciences, 1974
- Diagnostic Criteria for Rheumatoid ArthritisAnnals of the Rheumatic Diseases, 1959