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水杨酸铜和苯基丁氮酮作为大鼠和马的局部抗炎剂

Copper salicylate and copper phenylbutazone as topically applied anti-inflammatory agents in the rat and horse.

作者信息

Auer D E, Ng J C, Seawright A A

机构信息

Department of Veterinary Pathology and Public Health, University of Queensland, St Lucia, Australia.

出版信息

J Vet Pharmacol Ther. 1990 Mar;13(1):67-75. doi: 10.1111/j.1365-2885.1990.tb00749.x.

Abstract

Topically applied copper phenylbutazone, phenylbutazone, copper salicylate, salicylate and dimethylsulfoxide glycerol (80:20) were investigated as anti-inflammatory agents in rats and horses. Dimethylsulfoxide and glycerol (80:20) or dimethylsulfoxide, ethanol and glycerol (60:20:20) were used as the drug solvents. Subcutaneously administered carrageenin was used to induce inflammatory oedema, either in the paws of rats or the alar fold of the horse. The severity of the oedema and the anti-inflammatory effect of the drugs were assessed by measuring changes in the paw or alar-fold diameters. Copper salicylate and copper phenylbutazone were effective inhibitors of the inflammatory oedema in both species, but dimethylsulfoxide:glycerol (80:20) was not. In the rat, copper salicylate and copper phenylbutazone were superior anti-inflammatory agents compared to either salicylate or phenylbutazone, respectively. Following the topical application of four times the recommended daily dose of copper phenylbutazone to the horse for 5 days, minor skin irritation occurred and trace concentrations of phenylbutazone (maximum 0.6 microgram/ml) and negligible concentrations of oxyphenbutazone and gamma-hydroxyphenylbutazone were detected in the plasma.

摘要

研究了局部应用的苯基布他酮铜、苯基布他酮、水杨酸铜、水杨酸以及二甲基亚砜甘油(80:20)对大鼠和马的抗炎作用。二甲基亚砜和甘油(80:20)或二甲基亚砜、乙醇和甘油(60:20:20)用作药物溶剂。皮下注射角叉菜胶以在大鼠爪部或马的鼻翼皱襞处诱导炎性水肿。通过测量爪部或鼻翼皱襞直径的变化来评估水肿的严重程度和药物的抗炎效果。水杨酸铜和苯基布他酮铜对两种动物的炎性水肿均有有效抑制作用,但二甲基亚砜:甘油(80:20)则无此作用。在大鼠中,与水杨酸或苯基布他酮相比,水杨酸铜和苯基布他酮铜分别是更有效的抗炎剂。对马局部应用四倍于苯基布他酮推荐日剂量的药物,持续5天,出现了轻微的皮肤刺激,并且在血浆中检测到痕量浓度的苯基布他酮(最高0.6微克/毫升)以及可忽略不计浓度的羟布宗和γ-羟基苯基布他酮。

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