Bird J, Kim H P, Lee H J
Steroids. 1986 Jan;47(1):35-40. doi: 10.1016/0039-128x(86)90074-7.
Prednisolone derivatives, methyl 20 alpha- and 20 beta-dihydroprednisolonate and methyl 17,20 alpha- and 17,20 beta-acetonidodihydroprednisolonate have been evaluated for their topical anti-inflammatory activity in the croton oil induced ear edema test. The order of anti-inflammatory potency was prednisolone greater than methyl 17,20 alpha-acetonidodihydroprednisolonate greater than methyl 17,20 beta-acetonidodihydroprednisolonate greater than methyl 20 beta-dihydroprednisolonate greater than methyl 20 alpha-dihydroprednisolonate. This order was paralleled by the compounds' octanol-aqueous partition coefficients. Furthermore, after two consecutive days topical administration of an equipotent anti-inflammatory dose, only prednisolone significantly decreased plasma corticosterone levels and relative thymus weight, while the new steroid derivatives had no effect on these parameters, indicating their lack of systemic side effects.
已对泼尼松龙衍生物、20α-和20β-二氢泼尼松龙甲酯以及17,20α-和17,20β-亚丙酮基二氢泼尼松龙甲酯在巴豆油诱导的耳水肿试验中的局部抗炎活性进行了评估。抗炎效力顺序为泼尼松龙＞17,20α-亚丙酮基二氢泼尼松龙甲酯＞17,20β-亚丙酮基二氢泼尼松龙甲酯＞20β-二氢泼尼松龙甲酯＞20α-二氢泼尼松龙甲酯。该顺序与化合物的辛醇-水分配系数平行。此外，连续两天局部给予等效抗炎剂量后，只有泼尼松龙显著降低血浆皮质酮水平和相对胸腺重量，而新的类固醇衍生物对这些参数没有影响，表明它们没有全身副作用。
