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新型糠酸莫米松 0.1%轻润乳膏的生物利用度、抗银屑病疗效和耐受性

Bioavailability, antipsoriatic efficacy and tolerability of a new light cream with mometasone furoate 0.1%.

机构信息

Department of Dermatology and Allergology, Ludwig Maximilian University, Munich, Germany.

出版信息

Skin Pharmacol Physiol. 2012;25(3):133-41. doi: 10.1159/000335656. Epub 2012 Feb 17.

Abstract

Mometasone furoate, a potent glucocorticoid (class III) with a favorable benefit/risk ratio, has emerged as a standard medication for the treatment of inflammatory skin disorders. The purpose of the investigation presented here was to determine the noninferiority of a topical mometasone formulation, a light cream (O/W 60/40 emulsion) with mometasone furoate 0.1% (water content of 33%) versus marketed comparators. Using the vasoconstrictor assay, a strong blanching effect of the new cream (called Mometasone cream) comparable to that of a mometasone comparator, a fatty cream with mometasone furoate 0.1%, could be demonstrated. Thus, the topical bioavailability of the active ingredient mometasone furoate (0.1%) was regarded to be similar for Mometasone cream and the mometasone comparator. Using the psoriasis plaque test, a strong antipsoriatic effect comparable to that of the mometasone comparator was found for Mometasone cream after 12 days of occlusive treatment. A nearly identical reduction in the mean infiltrate thickness and similar mean AUC values were noted with both formulations confirmed by clinical assessment data. The noninferiority of Mometasone cream to its active comparator with respect to the AUC of change to baseline in infiltrate thickness was demonstrated. Both medications were well tolerated. Overall, Mometasone cream and the mometasone comparator showed similar efficacy and tolerability. Mometasone cream, in addition to its high potency and good tolerability, provides the properties of a light cream, which might make this new medication particularly suitable for application on acutely inflamed and sensitive skin.

摘要

莫米松糠酸酯是一种强效糖皮质激素(III 类),具有良好的收益/风险比,已成为治疗炎症性皮肤疾病的标准药物。本研究旨在确定一种局部莫米松制剂(一种含有 0.1%莫米松糠酸酯的轻奶油[O/W 60/40 乳剂],含水量为 33%)与市售对照药物的非劣效性。使用血管收缩剂测定法,可证明新型乳膏(称为莫米松乳膏)具有与莫米松对照药物相当的强烈发白作用。因此,活性成分莫米松糠酸酯(0.1%)的局部生物利用度被认为与莫米松乳膏和莫米松对照药物相似。使用银屑病斑块测试,在 12 天的封闭治疗后,发现莫米松乳膏具有与莫米松对照药物相当的强烈抗银屑病作用。临床评估数据证实,两种制剂的平均浸润厚度的几乎相同的减少和相似的平均 AUC 值。证明了莫米松乳膏在浸润厚度的基线变化的 AUC 方面相对于其活性对照药物的非劣效性。两种药物均具有良好的耐受性。总的来说,莫米松乳膏与莫米松对照药物在疗效和耐受性方面具有相似性。除了高疗效和良好的耐受性外,莫米松乳膏还具有轻奶油的特性,这可能使这种新药物特别适合应用于急性炎症和敏感皮肤。

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