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多烯磷脂酰胆碱(易善复100)对非甾体抗炎药胃耐受性的改善作用

Improvement of the gastric tolerance of non-steroidal anti-inflammatory drugs by polyene phosphatidylcholine (Phospholipon 100).

作者信息

Leyck S, Dereu N, Etschenberg E, Ghyczy M, Graf E, Winkelmann J, Parnham M J

出版信息

Eur J Pharmacol. 1985 Oct 29;117(1):35-42. doi: 10.1016/0014-2999(85)90469-8.

Abstract

The effect of co-administration with polyene phosphatidylcholine (Phospholipon 100) on the oral gastrotoxicity of various non-steroidal anti-inflammatory drugs (NSAIDs) was studied in the rat. The highly unsaturated phospholipid reduced gastric mucosal lesions measured 3.5 h after oral administration of aspirin, indomethacin, phenylbutazone, diclofenac, piroxicam and sudoxicam to rats which had received a 3 day bread diet followed by 24 h fasting. The extent of reduction of gastrotoxicity varied amongst the individual NSAIDs. Phospholipon 100 also reduced gastric lesions induced by 3 day oral piroxicam and diclofenac administration. A trend towards reduction of oral diclofenac gastrotoxicity was observed following intravenous Phospholipon 100 administration. Phospholipon 100 H (100% saturated phosphatidylcholine) was less effective than Phospholipon 100 in improving acute gastric tolerance to oral phenylbutazone, diclofenac and piroxicam. Administration of the NSAID-Phospholipon 100 combination produced little change in the anti-inflammatory activities of diclofenac on carrageenan paw oedema and diclofenac and piroxicam on adjuvant arthritis in the rat. Combination with Phospholipon 100 offers a novel means for reducing the gastric side-effects of NSAID therapy.

摘要

在大鼠中研究了与多烯磷脂酰胆碱(易善复100)联合给药对各种非甾体抗炎药(NSAIDs)口服胃毒性的影响。在给接受3天面包饮食后禁食24小时的大鼠口服阿司匹林、吲哚美辛、保泰松、双氯芬酸、吡罗昔康和舒多昔康3.5小时后,这种高度不饱和磷脂减少了胃黏膜损伤。胃毒性的降低程度在各个NSAIDs之间有所不同。易善复100还减少了3天口服吡罗昔康和双氯芬酸引起的胃损伤。静脉注射易善复100后,观察到口服双氯芬酸胃毒性有降低趋势。易善复100 H(100%饱和磷脂酰胆碱)在提高对口服保泰松、双氯芬酸和吡罗昔康的急性胃耐受性方面比易善复100效果差。NSAIDs与易善复100联合给药对双氯芬酸对角叉菜胶足爪水肿的抗炎活性以及双氯芬酸和吡罗昔康对大鼠佐剂性关节炎的抗炎活性几乎没有影响。与易善复100联合使用为减少NSAID治疗的胃部副作用提供了一种新方法。

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