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在环糊精影响下氢化可的松对人离体皮肤的渗透作用。

Penetration of hydrocortisone into excised human skin under the influence of cyclodextrins.

作者信息

Preiss A, Mehnert W, Frömming K H

机构信息

Institut für Pharmazie, Pharmazeutische Technologie, Freie Universität Berlin.

出版信息

Pharmazie. 1995 Feb;50(2):121-6.

PMID:7700965
Abstract

Hydrocortisone (HC) penetration into excised human skin from 1% (w/w) HC containing formulations with white petrolatum, an o/w cream and an aqueous polyacrylate gel is described. The experiments were performed with pure HC and the inclusion compounds with beta-cyclodextrin and hydroxypropyl-beta-cyclodextrin. The smallest HC amounts in the skin were found with the petrolatum preparations. No differences between the incorporation of free HC and the inclusion compounds was found. The highest HC amounts in the skin are found with the o/w cream and hydrogel formulation containing nonincluded HC. Incorporation of both inclusion compounds into these vehicles diminishes the HC concentration in the upper skin layers but not in the dermis. It is assumed that the preferred penetration route for the easily soluble inclusion compounds is a transappendageal diffusion rather than a transdermal one. A comparison with release results by using an ointment liberation model gives a good correlation with the penetration results in the dermis but not in the other skin layers.

摘要

描述了氢化可的松(HC)从含1%(w/w)HC的白色凡士林制剂、水包油乳膏和聚丙烯酸水凝胶制剂渗入切除的人体皮肤的情况。实验使用了纯HC以及与β-环糊精和羟丙基-β-环糊精的包合物。凡士林制剂在皮肤中的HC含量最低。未发现游离HC和包合物的掺入有差异。在水包油乳膏和含未包合HC的水凝胶制剂中,皮肤中的HC含量最高。将两种包合物掺入这些载体中会降低上层皮肤中的HC浓度,但不会降低真皮中的浓度。据推测,易溶性包合物的首选渗透途径是经附属器扩散而非经皮扩散。使用软膏释放模型的释放结果与之比较,与真皮中的渗透结果有良好相关性,但与其他皮肤层的结果无关。

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