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倍他米松 17-戊酸酯的皮肤药代动力学:制剂粘度和皮肤表面清洁程序的影响。

Dermatopharmacokinetics of betamethasone 17-valerate: influence of formulation viscosity and skin surface cleaning procedure.

作者信息

Wiedersberg Sandra, Leopold Claudia S, Guy Richard H

机构信息

Department of Pharmacy & Pharmacology, University of Bath, Bath, UK.

出版信息

Eur J Pharm Biopharm. 2009 Feb;71(2):362-6. doi: 10.1016/j.ejpb.2008.10.001. Epub 2008 Oct 10.

Abstract

The objective was to compare the in vivo distribution profiles of betamethasone 17-valerate (BMV) across the stratum corneum (SC) following (a) delivery from gelled and un-gelled formulations, and (b) two different skin cleaning procedures at the end of the application period. BMV was dissolved in gelled and un-gelled vehicles comprising either medium chain triglycerides (MCT) or a brand microemulsion (ME). The BMV concentration was adjusted to 80% of saturation and applied to the forearms of healthy volunteers. After 2 h, the treated skin site was cleaned either with a dry paper towel or with an isopropyl alcohol swab, and the SC was then progressively removed by repeated adhesive tape-stripping. BMV distribution profiles across the SC showed reasonable reproducibility, and that delivery from the ME was significantly superior to that from MCT. Gelled vehicles were less efficiently removed from the skin surface by dry wiping than un-gelled formulations. Removing excess formulation more aggressively with isopropyl alcohol resulted in a lower apparent uptake of drug into the SC. Excess gelled formulation may be trapped in the skin 'furrows', and requires an efficient skin cleaning procedure to ensure its complete removal.

摘要

目的是比较戊酸倍他米松(BMV)在角质层(SC)中的体内分布情况,具体如下:(a)从凝胶化和未凝胶化制剂中释放后;(b)在应用期结束时采用两种不同的皮肤清洁程序。BMV溶解于包含中链甘油三酯(MCT)或一种品牌微乳剂(ME)的凝胶化和未凝胶化载体中。将BMV浓度调整至饱和度的80%,并应用于健康志愿者的前臂。2小时后,用干纸巾或异丙醇棉签清洁处理过的皮肤部位,然后通过反复粘贴胶带逐步去除SC。BMV在SC中的分布情况显示出合理的重现性,并且从ME中的释放明显优于从MCT中的释放。与未凝胶化制剂相比,凝胶化载体通过干擦从皮肤表面去除的效率较低。用异丙醇更积极地去除多余制剂会导致药物在SC中的表观摄取量较低。多余的凝胶化制剂可能被困在皮肤“沟纹”中,需要有效的皮肤清洁程序以确保其完全去除。

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