Kecskés A, Jahn P, Wendt H, Kleine-Kuhlmann R, Lange L
Department of Human Pharmacology, Schering Aktiengesellschaft, Berlin.
Arzneimittelforschung. 1993 Feb;43(2):144-7.
Topical glucocorticosteroids are useful in the treatment of various skin diseases. Although there are already many corticosteroids available, there is still need for highly potent and well tolerated ones. The anti-inflammatory activity of methylprednisolone aceponate (MPA, CAS 86401-95-8) has been investigated in 165 healthy volunteers of either sex. UV-B irradiation or cellophane tape stripping has served to produce erythema. First, the dose response relationship of MPA ointment (0.01%, 0.05%, 0.1% and 0.5%) has been evaluated. MPA effects have been related to those of the vehicle and difluocortolone 21-valerate 0.1% (DFV) ointment. Then the activity of 0.1% MPA (cream, ointment and fatty ointment) has been related to those of the respective vehicles as well as commercially available preparations of five corticosteroids: betamethasone 17,21-dipropionate 0.64% (BDP), betamethasone 17-valerate 0.1% (BV), clobetasol 17-propionate 0.05% (CP), hydrocortisone 17-butyrate 0.1% (HCB), prednicarbate 0.25% (P). In each experiment, MPA activity significantly exceeded that of the respective vehicle (p < or = 0.05). MPA 0.01-0.5% ointment exhibited strong anti-inflammatory activity, at least corresponding to that of 0.1% DFV ointment. A dose-dependent activity could only be observed in the UV-B-erythema test using 3 fold MED (minimal erythema doses) for irradiation, a test model differentiating strong corticosteroids. The comparison of 0.1% MPA formulations with respective reference preparations showed the following results: On stripped skin no significant differences could be detected which is demonstrated in the example of cream formulations.(ABSTRACT TRUNCATED AT 250 WORDS)
外用糖皮质激素在多种皮肤病的治疗中很有用。尽管已有许多皮质类固醇可用，但仍需要高效且耐受性良好的药物。已在165名男女健康志愿者中研究了醋丙甲泼尼龙（MPA，CAS 86401-95-8）的抗炎活性。采用紫外线B照射或透明胶带剥离法诱发红斑。首先，评估了MPA软膏（0.01%、0.05%、0.1%和0.5%）的剂量反应关系。将MPA的效果与赋形剂以及0.1%戊酸倍他米松（DFV）软膏的效果进行了比较。然后，将0.1%MPA（乳膏、软膏和脂肪性软膏）的活性与相应的赋形剂以及五种皮质类固醇的市售制剂进行了比较：0.64%倍他米松17,21-二丙酸酯（BDP）、0.1%倍他米松17-戊酸酯（BV）、0.05%丙酸氯倍他索（CP）、0.1%氢化可的松17-丁酸酯（HCB）、0.25%泼尼卡酯（P）。在每个实验中，MPA的活性均显著超过相应赋形剂（p≤0.05）。0.01%-0.5%的MPA软膏表现出较强的抗炎活性，至少与0.1%的DFV软膏相当。仅在使用3倍最小红斑量（MED）进行照射的紫外线B红斑试验中观察到剂量依赖性活性，该试验模型可区分强效皮质类固醇。0.1%MPA制剂与相应参比制剂的比较结果如下：在剥离皮肤上未检测到显著差异，乳膏制剂的例子证明了这一点。（摘要截断于250字）
