Melarange R, Rashbrook L C
Beecham Pharmaceuticals, Medicinal Research Centre, Harlow, Essex, UK.
J Pharm Pharmacol. 1987 Sep;39(9):717-20. doi: 10.1111/j.2042-7158.1987.tb06975.x.
The effect of nabumetone on rat gastric mucosal cyclooxygenase activity ex-vivo and in-vitro has been compared with that of indomethacin. Nabumetone was less potent and less active in inhibiting the production of gastric mucosal 6-keto-PGF1 alpha compared with indomethacin either ex-vivo or in-vitro. Anti-inflammatory doses of nabumetone failed to enhance bile salt-induced gastric erosion or mucosal permeability to dextran whereas indomethacin significantly enhanced gastric erosion and increased dextran permeability. These results suggest that nabumetone fails to promote gastric damage or increase permeability because of minimal effects on gastric mucosal cyclooxygenase.
已将萘丁美酮对大鼠胃黏膜环氧化酶活性的体外和体内作用与吲哚美辛进行了比较。与吲哚美辛相比,无论是在体外还是体内,萘丁美酮抑制胃黏膜6-酮-前列腺素F1α生成的效力和活性都较低。抗炎剂量的萘丁美酮未能增强胆盐诱导的胃糜烂或胃黏膜对右旋糖酐的通透性,而吲哚美辛则显著加剧胃糜烂并增加右旋糖酐通透性。这些结果表明,萘丁美酮对胃黏膜环氧化酶的影响极小,故而不会促进胃损伤或增加通透性。