Alpermann H G, Sandow J, Vogel H G
Z Hautkr. 1986;61 Suppl 1:7-17.
Prednisolone-17-ethyl carbonate-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 corticoid 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.
对泼尼松龙-17-碳酸乙酯-21-丙酸酯(PrEP,Hoe 777)进行了研究,通过局部和全身给药在各种动物模型中测试其抗炎活性。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给予PrEP后的全身效应相对较弱。此外,皮下给予PrEP后的全身皮质激素效应比给予去氧米松后的要少。因此,PrEP显然是一种局部和全身活性有显著差异的化合物,这表明应对其进行人体试验,以研究局部给药后的全身效应。