Alpermann H G, Sandow J, Vogel H G
Arzneimittelforschung. 1982;32(6):633-8.
Prednisolone-17-ethylcarbonate-21-propionate (PrEP, Hoe 777) was tested for antiinflammatory activity in various animal models by topical and systemic administration. In those models being indicative of topical efficacy, the potency of PrEP was the same as that of desoximetasone. However, systemic effects after topical administration of PrEP in shaved skin of the dorsum of rats were relatively weak compared with the reference compound. Moreover, there were less systemic glucocorticoid effects after s.c. administration of PrEP than after desoximetasone. Thus, PrEP is obviously a compound with a considerable split of topical and systemic activity, suggesting its testing in man for systemic effects after topical administration.
泼尼松龙 -17 - 乙基碳酸酯 -21 - 丙酸酯(PrEP,Hoe 777)通过局部和全身给药在各种动物模型中进行抗炎活性测试。在那些表明局部疗效的模型中,PrEP的效力与去氧米松相同。然而,与参比化合物相比,在大鼠背部剃毛皮肤上局部施用PrEP后的全身作用相对较弱。此外,皮下注射PrEP后的全身糖皮质激素作用比注射去氧米松后少。因此,PrEP显然是一种局部和全身活性有显著差异的化合物,这表明有必要在人体中测试其局部给药后的全身作用。