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丙酸氯倍他索的生物利用度——采用胶带剥离法通过皮肤药代动力学对角质层中药物浓度进行定量分析。

Bioavailability of clobetasol propionate-quantification of drug concentrations in the stratum corneum by dermatopharmacokinetics using tape stripping.

作者信息

Weigmann H, Lademann J, v Pelchrzim R, Sterry W, Hagemeister T, Molzahn R, Schaefer M, Lindscheid M, Schaefer H, Shah V P

机构信息

Charité, Universitätsklinikum der Humboldt-Universität zu Berlin, Klinik für Dermatologie, Venerologie und Allergologie mit Asthmapoliklinik, Berlin, Germany.

出版信息

Skin Pharmacol Appl Skin Physiol. 1999 Jan-Apr;12(1-2):46-53. doi: 10.1159/000029845.

DOI:10.1159/000029845
PMID:10325583
Abstract

The concentration of clobetasol propionate in the stratum corneum after application of three different formulations was determined, quantifying the influence of the formulations on the bioavailability of the drug. The stratum corneum was sampled by tape stripping. The concentrations of clobetasol propionate were determined quantitatively by HPLC. After application of Clobetasol Propionate Cream USP, 0.05%, and Temovate Cream, 0.05%, identical amounts of the drug were found in the stratum corneum, whereas after application of Temovate epsilon Emollient, 0.05%, the quantity was clearly decreased. From results obtained measuring the drug concentration in the adjacent sites of the skin where the creams had not been applied, it became clear that clobetasol propionate in Temovate epsilon Emollient, migrated to a large extent in the lateral direction. This explains the lower concentration measured for this formulation in the skin areas where the cream had been applied. In general, a lateral distribution of the applied drug must be taken into account when positioning the application areas on the forearm.

摘要

测定了三种不同制剂应用后丙酸氯倍他索在角质层中的浓度,以量化制剂对药物生物利用度的影响。通过胶带剥离法采集角质层样本。采用高效液相色谱法定量测定丙酸氯倍他索的浓度。应用0.05%的丙酸氯倍他索乳膏(美国药典)和0.05%的特美肤乳膏后,角质层中发现的药物量相同,而应用0.05%的特美肤润肤乳膏后,药物量明显减少。通过测量未涂抹乳膏的皮肤相邻部位的药物浓度所获得的结果表明,特美肤润肤乳膏中的丙酸氯倍他索在很大程度上向侧向迁移。这就解释了在涂抹乳膏的皮肤区域中该制剂测得的浓度较低的原因。一般来说,在前臂上定位涂抹区域时,必须考虑所涂抹药物的侧向分布。

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