ANTIINFLAMMATORY, ANALGESIC AND ULCEROGENIC PROPERTIES OF S-(-IBUPROXAM, RACEMIC IBUPROXAM-BETA-CYCLODEXTRIN AND S-(+)-IBUPROXAM-BETA-CYCLODEXTRIN())

The anti-inflammatory, analgesic and gastric mucosal damage-inducing a ctivities of S-(+)-ibuproxam, and S-(+)-ibuproxam-beta-cyclodextrin, n ew propionic acid derivatives, and racemic ibuproxam-beta-cyclodextrin were investigated in three animal models and compared with those of r acemic ibuproxam, racemic ibuprofen and its optical enantiomer S-(+)-i buprofen. The anti-inflammatory activities of racemic ibuprofen, S-(+) -ibuprofen and racemic ibuproxam in carrageenan-induced paw oedema in rats were almost equipotent and slightly greater than those of S-(+)-i buproxam and S-(+)-ibuproxam-beta-cyclodextrin, and significantly grea ter than that of racemic ibuproxam-beta-cyclodextrin. In abdominal con striction tests in mice, the analgesic effects of racemic ibuproxam, S -(+)-ibuproxam, racemic ibuproxam-beta-cyclodextrin and S-(+)-ibuproxa m-beta-cyclodextrin were significantly less pronounced than those of r acemic ibuprofen and S-(+)-ibuprofen. Ulcerogenic activity of S-(+)-ib uproxam-beta-cyclodextrin in rats was found to be significantly weaker than that of racemic ibuproxam-beta-cyclodextrin, racemic ibuproxam a nd S-(+)ibuproxam and, most notably, weaker than those of racemic ibup rofen ans S-(+)ibuprofen. These results indicate that S-(+)-ibuproxam- beta-cyclodextrin could be a novel potent anti-inflammatory and analge sic agent with a therapeutic index more favourable than that of the cl assical non-steroid antiinflammatory drugs ibuprofen and ibuproxam.