Hiroi J, Fujii T, Satoh S, Ochi T, Kobayashi K, Ohyanagi Y, Senoh H, Mori J, Kikuchi H
Nihon Yakurigaku Zasshi. 1985 Sep;86(3):219-31. doi: 10.1254/fpj.86.219.
The systemic and topical antiinflammatory activities of budesonide (B) were studied in rats and mice and compared with those of commercially available steroids. Betamethasone 17-valerate (BV) was used as the main reference compound, and fluosinolone acetonide (FA), hydrocortisone 17-butyrate (HB) and hydrocortisone 21-acetate (HA) were also used. B given systemically had stronger antiinflammatory effect than BV on carrageenin edema, cotton pellet granuloma, adjuvant arthritis, croton oil edema, PCA reaction, Arthus reaction, contact hypersensitivity and histamine or serotonin skin reaction. The potency of antiinflammatory activity of the 5 compounds in carrageenin edema, croton oil edema and contact hypersensitivity tests was in the order of FA, B, BV, HB and HA. B given locally also produced stronger antiinflammatory effects than BV on carrageenin edema, cotton pellet granuloma, croton oil edema and contact hypersensitivity. The order of potency of the 5 compounds in carrageenin edema, croton oil edema and contact hypersensitivity tests was the same as by systemic application. In general, the ratio of the dose required to cause atrophy of the thymus and adrenals to the dose required to produce the antiinflammatory effect was the greatest with B by both systemic and local application. The results suggest that B has a stronger antiinflammatory activity with fewer systemic side effects than conventional steroid compounds.
在大鼠和小鼠中研究了布地奈德(B)的全身和局部抗炎活性,并与市售类固醇的活性进行了比较。以倍他米松17 - 戊酸酯(BV)作为主要参照化合物,同时还使用了醋酸氟轻松(FA)、氢化可的松17 - 丁酸酯(HB)和氢化可的松21 - 醋酸酯(HA)。全身给予B时,在角叉菜胶性水肿、棉球肉芽肿、佐剂性关节炎、巴豆油水肿、被动皮肤过敏反应(PCA反应)、阿瑟斯反应、接触性超敏反应以及组胺或血清素皮肤反应方面,其抗炎作用比BV更强。在角叉菜胶性水肿、巴豆油水肿和接触性超敏反应试验中,这5种化合物的抗炎活性效力顺序为FA、B、BV、HB和HA。局部给予B时,在角叉菜胶性水肿、棉球肉芽肿、巴豆油水肿和接触性超敏反应方面,其抗炎作用也比BV更强。在角叉菜胶性水肿、巴豆油水肿和接触性超敏反应试验中,这5种化合物的效力顺序与全身给药时相同。总体而言,无论是全身给药还是局部给药,导致胸腺和肾上腺萎缩所需剂量与产生抗炎作用所需剂量之比,B是最大的。结果表明,与传统类固醇化合物相比,B具有更强的抗炎活性且全身副作用更少。