Higgins A J, Lees P, Sedgwick A D, Buick A R, Churchus R
Royal Veterinary College, North Mymms, Hatfield, Hertfordshire.
Equine Vet J. 1987 Jan;19(1):60-6. doi: 10.1111/j.2042-3306.1987.tb02584.x.
In a two-part cross-over experiment in six ponies, an acute inflammatory reaction was generated by injecting carrageenin solution into subcutaneously-implanted tissue-cages lined with fibrovascular granulation tissue. In each part of the cross-over, half of the ponies received a novel phenylpyrazoline anti-inflammatory agent (BW540C) orally and half received a placebo treatment. BW540C inhibited platelet cyclo-oxygenase for 24 h but the reductions in exudate eicosanoid concentrations were less pronounced. A significant suppression in the rise of surface skin temperature in BW540C-treated ponies paralleled drug-induced inhibition of thromboxane B2 bicyclic prostaglandin (PG) E2 concentrations at the inflamed site. The drug had no significant effect on 6-keto-PGF1 alpha, migrating leucocytes, lactate dehydrogenase or total protein in exudates. Maximum plasma concentrations of both compounds occurred 2 to 4 h after dosing and maximum exudate levels of drug and metabolite occurred at 12 h. Both compounds penetrated approximately three times less readily into exudate than into plasma.
在一项针对6匹小马的两部分交叉实验中,通过将角叉菜胶溶液注入内衬纤维血管肉芽组织的皮下植入组织笼中引发急性炎症反应。在交叉实验的每个部分,一半的小马口服一种新型苯基吡唑啉抗炎药(BW540C),另一半接受安慰剂治疗。BW540C可抑制血小板环氧化酶24小时,但渗出液中类花生酸浓度的降低不太明显。在BW540C治疗的小马中,体表皮肤温度升高受到显著抑制,这与药物诱导的炎症部位血栓素B2和双环前列腺素(PG)E2浓度抑制平行。该药物对6-酮-PGF1α、迁移的白细胞、乳酸脱氢酶或渗出液中的总蛋白没有显著影响。给药后2至4小时出现两种化合物的最大血浆浓度,药物和代谢物的最大渗出液水平出现在12小时。两种化合物渗入渗出液的难易程度比渗入血浆大约低三倍。