Kyuki K, Shibuya T, Tsurumi K, Fujimura H
Nihon Yakurigaku Zasshi. 1981 Jan;77(1):73-85.
The anti-inflammatory activity of dexamethasone 17-valerate ointment (DV-17, 0.12%) was investigated by topical application in mice and rats, and the effects compared with those of dexamethasone (DX, 0.12%), betamethasone 17-valerate (BV-17, 0.12%), beclomethasone 17,21-dipropionate (BE, 0.025%) and hydrocortisone 17-butyrate (HC, 0.1%) which were prepared with the same ointment base. DV-17 inhibited markedly the superficial inflammation such as increased vascular permeability induced by intradermal injection of histamine or bradykinin in rats and edema induced by a drop of croton oil into the mouse ear. DV-17 also inhibited significantly rat paw edema induced by carrageenin, yeast, nystatin and mustard. The inhibitory activity of DV-17 on those acute inflammatory responses was similar to that of DX and BV-17. In the inhibitory activity on carrageenin induced paw edema, DV-17 was less potent than that of DX when given orally, however was similar to DX in topical application. DV-17 also inhibited granulation tissue proliferation by subcutaneous paper disk implantation and nontreated foot swelling in adjuvant arthritic rats, but the inhibitory activity of DV-17 on the inflammation of these distant areas was lower than that of DX. On the other hand, systemic effects such as decrease in weight of adrenal or thymus and body weight loss were most evident in the case of DX and lower with DV-17. DV-17 prolonged wound healing and inhibited the delayed-type hypersensitivity induced by picryl chloride. The activity was equivalent to that of DX and BV-17. From the above results, it may be considered that DV-17 possesses potent anti-inflammatory activity, whereas it has fewer side effects and is a useful glucocorticoid for external application.
通过在小鼠和大鼠身上局部应用,研究了戊酸地塞米松17酯软膏(DV - 17,0.12%)的抗炎活性,并将其效果与用相同软膏基质制备的地塞米松(DX,0.12%)、倍他米松17 - 戊酸酯(BV - 17,0.12%)、二丙酸倍氯米松(BE,0.025%)和丁酸氢化可的松(HC,0.1%)进行比较。DV - 17显著抑制大鼠皮内注射组胺或缓激肽诱导的血管通透性增加等浅表炎症以及小鼠耳部滴入巴豆油诱导的水肿。DV - 17还显著抑制角叉菜胶、酵母、制霉菌素和芥子油诱导的大鼠足爪水肿。DV - 17对这些急性炎症反应的抑制活性与DX和BV - 17相似。在对角叉菜胶诱导的足爪水肿的抑制活性方面,口服给药时DV - 17的效力低于DX,但局部应用时与DX相似。DV - 17还通过皮下纸片植入抑制肉芽组织增生,并抑制佐剂性关节炎大鼠未处理足爪肿胀,但DV - 17对这些远处炎症区域的抑制活性低于DX。另一方面,DX导致的肾上腺或胸腺重量减轻和体重下降等全身效应最为明显,而DV - 17的这些效应较弱。DV - 17延长伤口愈合并抑制苦基氯诱导的迟发型超敏反应。其活性与DX和BV - 17相当。从上述结果可以认为,DV - 17具有强大的抗炎活性,而副作用较少,是一种有用的外用糖皮质激素。