caa a22 4500 47705739X CHVBK 20180405111350.0 cr unu---uuuuu 170330e19960601xx s 000 0 eng 10.1007/s002280050109 doi (NATIONALLICENCE)springer-10.1007/s002280050109 Stereoselective distribution of tiaprofenic acid in synovium and cartilage in osteoarthritic patients [Elektronische Daten] [F. Lapicque, D. Mainard, P. Gillet, E. Payan, B. Bannwarth, P. Netter] Objective: In order to document the stereoselective distribution in joints of a chiral nonsteroidal anti-inflammatory drug, the relative affinities of the enantiomers of tiaprofenic acid in synovium and for cartilage were compared. Methods: The distribution of tiaprofenic acid in synovium and in cartilage was studied 25 h after administering the racemic drug for 2 days (600 mg of a sustained-release preparation, once daily), in 12 inpatients with osteoarthritis of the hip requiring arthroplasty. Enantiomers were quantified in plasma and freeze-ground tissues by a chiral HPLC assay. Results: Plasma concentrations of the dextrorotatory (R) enantiomer (0.40 μg/ml) were higher than those of its antipode. The concentration of racemate in synovium (in dried and fresh tissues, 150% and 40%, respectively, of the concentration in plasma) was much higher than that in cartilage (in dried tissues 32% of the plasma concentration). The ratio of the active, dextrorotatory (R) enantiomer to its antipode was higher in synovial tissue than in plasma. Conclusion: Tiaprofenic acid is distributed stereoselectively in plasma and synovium, which contain a higher concentration of the active, dextrorotatory (R) enantiomer. In cartilage, it reaches only a very low concentration. Springer-Verlag Berlin Heidelberg, 1996 Key words Tiaprofenic acid nationallicence articular distribution nationallicence synovium nationallicence cartilage nationallicence chiral NSAID nationallicence Lapicque F. Laboratoire de Pharmacologie and URA CNRS 1288, Faculté de Médecine, BP 184, F-54505 Vandoeuvre les Nancy, France, FR aut Mainard D. Laboratoire de Pharmacologie and URA CNRS 1288, Faculté de Médecine, BP 184, F-54505 Vandoeuvre les Nancy, France, FR aut Gillet P. Laboratoire de Pharmacologie and URA CNRS 1288, Faculté de Médecine, BP 184, F-54505 Vandoeuvre les Nancy, France, FR aut Payan E. Laboratoire de Pharmacologie and URA CNRS 1288, Faculté de Médecine, BP 184, F-54505 Vandoeuvre les Nancy, France, FR aut Bannwarth B. Laboratoire de Pharmacologie and URA CNRS 1288, Faculté de Médecine, BP 184, F-54505 Vandoeuvre les Nancy, France, FR aut Netter P. Laboratoire de Pharmacologie and URA CNRS 1288, Faculté de Médecine, BP 184, F-54505 Vandoeuvre les Nancy, France, FR aut https://doi.org/10.1007/s002280050109 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/s002280050109 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Lapicque F. Laboratoire de Pharmacologie and URA CNRS 1288, Faculté de Médecine, BP 184, F-54505 Vandoeuvre les Nancy, France, FR aut NATIONALLICENCE 700 1- Mainard D. Laboratoire de Pharmacologie and URA CNRS 1288, Faculté de Médecine, BP 184, F-54505 Vandoeuvre les Nancy, France, FR aut NATIONALLICENCE 700 1- Gillet P. Laboratoire de Pharmacologie and URA CNRS 1288, Faculté de Médecine, BP 184, F-54505 Vandoeuvre les Nancy, France, FR aut NATIONALLICENCE 700 1- Payan E. Laboratoire de Pharmacologie and URA CNRS 1288, Faculté de Médecine, BP 184, F-54505 Vandoeuvre les Nancy, France, FR aut NATIONALLICENCE 700 1- Bannwarth B. Laboratoire de Pharmacologie and URA CNRS 1288, Faculté de Médecine, BP 184, F-54505 Vandoeuvre les Nancy, France, FR aut NATIONALLICENCE 700 1- Netter P. Laboratoire de Pharmacologie and URA CNRS 1288, Faculté de Médecine, BP 184, F-54505 Vandoeuvre les Nancy, France, FR aut Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer