Melarange R, Gentry C, Blower P R, Toseland C D, Spangler R
SmithKline Beecham Pharmaceuticals, Research and Development Technologies Harlow, Essex, UK.
Eur J Rheumatol Inflamm. 1994;14(2):15-22.
To determine the effects of nabumetone, compared with tiaprofenic acid and etodolac, on anti-inflammatory efficacy and gastrointestinal irritancy in the rat when dosed orally for one month at a high anti-inflammatory dose.
Carrageenan paw edema was used as a model of inflammation. Gastrointestinal mucosal integrity was assessed by concurrently measuring ulcer formation. mucosal and tissue prostanoid production and plasma haptoglobin. Haemoglobin, present in the cecal contents, was used as a measure of blood loss.
Nabumetone, tiaprofenic acid and etodolac inhibited inflammation. Etodolac induced marked gastrointestinal damage and blood loss whereas tiaprofenic acid caused only gastric damage. Nabumetone was found not to alter mucosal integrity.
Nabumetone proved to be an effective anti-inflammatory agent that was devoid of gastrointestinal irritancy.
将萘丁美酮与噻洛芬酸和依托度酸进行比较,以确定在大鼠以高抗炎剂量口服给药一个月时,萘丁美酮对其抗炎疗效和胃肠道刺激性的影响。
角叉菜胶足爪水肿用作炎症模型。通过同时测量溃疡形成、粘膜和组织前列腺素生成以及血浆触珠蛋白来评估胃肠道粘膜完整性。盲肠内容物中的血红蛋白用作失血的指标。
萘丁美酮、噻洛芬酸和依托度酸均能抑制炎症。依托度酸可引起明显的胃肠道损伤和失血,而噻洛芬酸仅导致胃部损伤。未发现萘丁美酮会改变粘膜完整性。
事实证明,萘丁美酮是一种有效的抗炎药,且无胃肠道刺激性。