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人身上关于戊酸二氟可龙、倍他米松-17-戊酸酯、二丙酸倍氯米松和醋酸氟轻松经皮吸收的比较研究

[Comparative studies in man on the percutaneous absorption of diflucortolone valerate, betamethasone-17-valerate, beclomethasone dipropionate and fluocinolone acetonide].

作者信息

Täuber V U, Amin M, Fuchs P, Speck U

出版信息

Arzneimittelforschung. 1976;26(7b):1492-5.

PMID:1036945
Abstract

Percutaneous absorption of 6alpha,9-difluor-11beta-hydroxy-16alpha-methyl-21-valeryloxy-1,4-pregnadience-3,20-dione (diflucortolone valerate, DFV, Nerisona), betamethasone 17-valerate (BV), beclomethasone dipropionate (BDP) and fluocinolone acetonide (FA) by damaged skin was examined on the backs of 4 healthy males from whom the stratum corneum had been removed by "stripping". The determination of percutaneous absorption was performed on the one hand by a method employing radioactive labelled compounds (DFV, BV) and measuring the elimination with the urine and faeces and on the other hand by photometric determination (DFV, BV, BD, fa) of the corticoid remaining on the skin immediately following application and at the end of a 24-h period of exposure. Direct measurement of the radioactivity in the urine and faeces revealed that percutaneous absorption from a new W/O emulsion takes place up to 2.2+/-0.8% in the case of DFV (0.1%) and to at least 12.2+/-3.3% in the case of BV (0.12%) within 24 h. The determination of percutaneous absorption via recovery from the skin produced the following results for the 4 corticoid preparations examined: DFV (14.8+/-4.2%) and BDP (14.0+/-4.3%) approximately equal, BV (23.5+/-4.1%) a marked increase and FA (39.2+/-2.4%) the highest level of absorption. This order for percutaneous absorption appears to correlate to the frequency of systemic side effects.

摘要

在4名健康男性的背部进行了研究,这些男性的角质层已通过“剥脱”去除,以检测受损皮肤对6α,9 - 二氟 - 11β - 羟基 - 16α - 甲基 - 21 - 戊酰氧基 - 1,4 - 孕二烯 - 3,20 - 二酮(戊酸倍他米松,DFV,Nerisona)、倍他米松17 - 戊酸酯(BV)、二丙酸倍氯米松(BDP)和醋酸氟轻松(FA)的经皮吸收情况。经皮吸收的测定一方面采用放射性标记化合物(DFV、BV)的方法,通过测量尿液和粪便中的排泄量来进行;另一方面通过光度法测定(DFV、BV、BDP、FA)涂抹后立即以及暴露24小时结束时皮肤表面残留的皮质类固醇。直接测量尿液和粪便中的放射性发现,对于新的水包油乳液,24小时内DFV(0.1%)的经皮吸收可达2.2±0.8%,BV(0.12%)的经皮吸收至少为12.2±3.3%。通过从皮肤回收来测定经皮吸收,对于所检测的4种皮质类固醇制剂得出以下结果:DFV(14.8±4.2%)和BDP(14.0±4.3%)大致相等,BV(23.5±4.1%)显著增加,FA(39.2±2.4%)吸收水平最高。这种经皮吸收的顺序似乎与全身副作用的发生率相关。

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