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Comparative study of anti-inflammatory and ulcerogenic activities of different cyclo-oxygenase inhibitors.

机译:不同环氧化酶抑制剂的抗炎和促溃疡活性的比较研究。

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摘要

The aim of the present work was to study the in vivo anti-inflammatory activity of six NSAIDs, ibuprofen, diclofenac, nimesulide, meloxicam, celecoxib and rofecoxib, using the rat air-pouch model of inflammation to characterize the ability of these drugs to induce gastric damage and PGE(2) inhibition. Selective compounds were observed to have no ulcerogenic properties at anti-inflammatory doses; however, these drugs were weaker inhibitors of several inflammatory aspects such as cell influx and exudate formation. In contrast, the non-selective and preferential compounds present anti-inflammatory properties at lower doses than presented by selective drugs. At anti-inflammatory doses, only meloxicam and ibuprofen produced gastric damage and inhibition of PGE(2) synthesis, suggesting that ulcerogenic properties of NSAIDs cannot be predicted by their selectivity index, since meloxicam demonstrates ulcerogenic properties despite its preferential profile.
机译:本研究的目的是使用大鼠气袋炎症模型来研究这6种非甾体抗炎药(ibuprofen,双氯芬酸,尼美舒利,美洛昔康,塞来昔布和罗非考昔)的体内抗炎活性,以表征这些药物诱导炎症的能力。胃损害和PGE(2)抑制。在抗炎剂量下观察到选择性化合物没有致溃疡的特性;但是,这些药物在某些炎症方面(如细胞大量涌入和渗出液形成)是较弱的抑制剂。相反,非选择性和优先化合物以比选择性药物更低的剂量呈现抗炎特​​性。在抗炎剂量下,只有美洛昔康和布洛芬产生胃部损伤和抑制PGE(2)的合成,这表明不能通过其选择性指数预测NSAIDs的致溃疡性,因为美洛昔康尽管具有优先性,但仍具有致溃疡性。

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