Passage of nonsteroidal anti-inflammatory agents across the synovial membrane
Netter, P.; Bannwarth, B.; Monot, C.; Royer, R.J.; Gaucher, A.
Presse Medicale 12(33): 2049-2052
1983
ISSN/ISBN: 0755-4982 PMID: 6226020 Document Number: 214386
The therapeutic effectiveness of non-steroid anti-inflammatory (NSAI) drugs is partly determined by their passage across the synovial membrane. The synovium can be compared to a double barrier the permeability of which to NSAI drugs depends on the degree of inflammation of the joint and on the pharmacokinetic properties of the drugs (lipophilia, pka, protein-binding). A few hours after one single systemic dose, concentrations in the synovial fluid are higher than in serum. During chronic administration, concentrations of NSAI drugs with a short half-life vary less in synovial fluid than in serum. During steady state, free fractions of NSAI drugs with prolonged half-life may be similar in both compartments.