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采用非封闭多剂量方案评估七种专利皮质类固醇乳膏的血管收缩活性和生物利用度;临床意义。

Vasoconstrictor activities and bio-availabilities of seven proprietary corticosteroid creams assessed using a non-occluded multiple dosage regimen; clinical implications.

作者信息

Barry B W, Woodford R

出版信息

Br J Dermatol. 1977 Nov;97(5):555-60. doi: 10.1111/j.1365-2133.1977.tb14135.x.

Abstract

The bio-availabilities and activities of commercial creams (Metosyn, Synalar, Betnovate, Locoid, Alphaderm, Dioderm and Efcortelan 1%) were assessed using a multiple dosage regimen vasoconstrictor assay in ten volunteers. The blanching response first increased but then diminished with continued application over a 5-day period: following a 2-day 'resting period', when no steroid was applied, the application sites recovered considerably but tachyphylaxis again resulted from subsequent repeated applications. Acute tolerance occurred with the hydrocortisone formulations (Alphaderm, Dioderm and Efcortelan 1%) in a manner similar to that observed with the potent preparations. Metosyn was significantly more active (P less than 0.05), and Efcortelan 1% was significantly less active (P less than 0.05), than the other formulations. Apart from the reversal of Dioderm and Alphaderm the rank order of preparations was similar to that previously noted in the 6 h occluded single-application vasoconstrictor test. The results may have significance in dosage from design and application for topical corticosteroid formulations.

摘要

采用多剂量方案血管收缩试验,在10名志愿者中评估了市售乳膏(美卓乐、仙乃乐、倍他米松新霉素乳膏、乐肤液、α-皮康、特美肤和1%氯倍他索丙酸酯乳膏)的生物利用度和活性。在5天的持续用药过程中,皮肤变白反应起初增强,但随后减弱:在2天“停药期”(未使用类固醇)后,用药部位有相当程度的恢复,但随后再次重复用药又导致快速耐受性产生。氢化可的松制剂(α-皮康、特美肤和1%氯倍他索丙酸酯乳膏)出现急性耐受性的方式与强效制剂类似。美卓乐的活性显著更高(P<0.05),1%氯倍他索丙酸酯乳膏的活性显著更低(P<0.05),与其他制剂相比。除特美肤和α-皮康的顺序颠倒外,制剂的排名顺序与先前在6小时封包单次用药血管收缩试验中记录的相似。这些结果可能对局部用皮质类固醇制剂的剂量设计和应用具有重要意义。

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