Marshall R C, Du Vivier A
Br J Dermatol. 1978 Mar;98(3):355-9. doi: 10.1111/j.1365-2133.1978.tb06164.x.
An animal model for evaluating the effects of drugs on epidermal DNA synthesis has been used to determine the time of onset, period of maximum activity and duration of effect of two topically applied proprietary glucocorticosteroids, clobetasone butyrate and clobetasol propionate. Both drugs produced maximum inhibition of epidermal DNA synthesis by 24 h after application. Clobetasol propionate exhibited a significantly earlier onset (4 1/2 h) and longer duration (36 h) of activity than clobetasone butyrate (6 and 24 h respectively). A systemic effect was not observed at any time after the application of clobetasone butyrate but was observed for up to 24 h after the application of clobetasol propionate. Clobetasol butyrate was also assayed in this system and was found to be as potent as clobetasol propionate. It is concluded that the alcoholic, as opposed to the ketonic, grouping in the 11 positions of the steroid ring profoundly alters the potentials of this molecule for systemic activity.
一种用于评估药物对表皮DNA合成影响的动物模型已被用于确定两种局部应用的专利糖皮质激素丁酸氯倍他松和丙酸氯倍他索的起效时间、最大活性期和作用持续时间。两种药物在应用后24小时均产生了对表皮DNA合成的最大抑制作用。与丁酸氯倍他松（分别为6小时和24小时）相比，丙酸氯倍他索表现出显著更早的起效时间（4.5小时）和更长的活性持续时间（36小时）。在应用丁酸氯倍他松后的任何时间均未观察到全身效应，但在应用丙酸氯倍他索后长达24小时观察到了全身效应。丁酸氯倍他松也在该系统中进行了测定，发现其效力与丙酸氯倍他索相同。得出的结论是，甾体环11位上的醇基而非酮基，深刻改变了该分子产生全身活性的潜力。
