Kecskés A, Jahn P, Wendt H, Lange L, Kuhlmann R K
Human Pharmacology, Schering AG, Berlin, FRG.
Eur J Clin Pharmacol. 1992;43(2):157-9. doi: 10.1007/BF01740663.
Topical glucocorticosteroids are useful in the treatment of various skin diseases. Although many corticosteroids are available today, there is still a need for highly potent compounds with minimal adverse effects. Methylprednisolone aceponate (MPA) has recently been synthesized. Its activity has been evaluated using the vasoconstrictor assay and the poison ivy test (rhus dermatitis) in 19/20 healthy volunteers of either sex. Comparable blanching was found with MPA in a cream vehicle, in an ointment and a fatty ointment. Vasoconstriction and suppression of experimentally-induced poison ivy contact dermatitis were dose-dependent in the concentration range 0.01% to 0.5% MPA. Concentrations of MPA of at least 0.05% were significantly active. Following the highest dose, blanching was close to the maximum which can be obtained. This finding, and the improvement of rhus dermatitis, suggest that MPA belongs to the highly potent local glucocorticosteroids.
外用糖皮质激素在多种皮肤病的治疗中很有用。尽管如今有许多皮质类固醇药物可供使用,但仍需要具有最小副作用的高效化合物。醋丙甲泼尼龙(MPA)最近已被合成。在19/20名健康的男女志愿者中,使用血管收缩试验和毒漆藤试验(漆树皮炎)对其活性进行了评估。在乳膏载体、软膏和脂肪性软膏中发现MPA具有相当的皮肤变白作用。在0.01%至0.5%的MPA浓度范围内,血管收缩和对实验性诱导的毒漆藤接触性皮炎的抑制呈剂量依赖性。至少0.05%的MPA浓度具有显著活性。在最高剂量后,皮肤变白接近所能达到的最大值。这一发现以及对漆树皮炎的改善表明,MPA属于高效局部糖皮质激素。