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Variability in the stereoselective disposition of ibuprofen in patients with rheumatoid arthritis.
Author(s) -
Geisslinger G,
Stock KP,
Loew D,
Bach GL,
Brune K
Publication year - 1993
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1993.tb04189.x
Subject(s) - ibuprofen , pharmacokinetics , cmax , medicine , rheumatoid arthritis , confidence interval , urine , pharmacology , gastroenterology
1. Patients suffering from rheumatoid arthritis received oral doses of 600 mg racemic ibuprofen (n = 25; RAC) or 400 mg (S)‐ibuprofen (n = 25; S‐IBU) in a double‐blind, randomized parallel‐group study. 2. The pharmacokinetic parameters of (S)‐ibuprofen were not statistically different between treatments (P > 0.05). Comparing (S)‐ and (R)‐ ibuprofen within the group receiving the racemate significantly higher Cmax (20.3 +/‐ 5.3 vs 17.7 +/‐ 4.4 micrograms ml‐1; P < 0.02; 95% confidence interval for differences (CI): 0.5‐4.6), AUC (86.2 +/‐ 23.5 vs 67.6 +/‐ 26.6 micrograms ml‐1 h; P < 0.001; CI: 9.5‐27.6), mean residence time (4.5 +/‐ 1.1 vs 4.1 +/‐ 1.2 h; P < 0.01; CI: 0.1‐0.6) and renal clearance (0.8 +/‐ 0.6 vs 0.0 +/‐ 0.0 ml min‐1; P < 0.001; CI: 0.5‐1.0) values were observed for the (S)‐enantiomer. 3. No difference was found (P > 0.05) between treatments in the percentage of the dose recovered in the urine as (R)‐ or (S)‐ibuprofen plus metabolites (S‐IBU: 80.2 +/‐ 8.47 vs RAC: 74.1 +/‐ 14.0%). 4. Interindividual variation in the pharmacokinetics of (S)‐ibuprofen following administration of the racemate was similar to that following the administration of the single isomer suggesting that chiral inversion is not a major factor contributing to variability in the disposition of this drug.