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体外经皮吸收研究方法V:透过受损皮肤的渗透

Methods for in vitro percutaneous absorption studies V: Permeation through damaged skin.

作者信息

Bronaugh R L, Stewart R F

出版信息

J Pharm Sci. 1985 Oct;74(10):1062-6. doi: 10.1002/jps.2600741008.

Abstract

The permeation of compounds through skin damaged by different methods was compared because agents that are absorbed through skin are sometimes applied to a damaged barrier. The removal of the stratum corneum by stripping the skin with cellophane tape was the most effective method for enhancing absorption. A minimal increase in water permeation was obtained when one abrasion line was made with a hypodermic needle, but the absorption increased substantially when three to six lines were made across the site of application. Similar values were obtained with in vivo and in vitro techniques for penetration of cortisone and nicotinic acid through normal and abraded rat skin. Sever damage by UV irradiation to rats in vivo resulted in nicotinic acid absorption similar to that obtained in vitro through abraded or tape-stripped skin. Damage from mild irradiation could not be accurately duplicated by in vitro methods. The magnitude of the increase in absorption of seven chemicals through abraded human and rat skin was related to the extent to which the molecules were absorbed by the skin. The greatest increases in penetration were obtained with the compounds that were most poorly absorbed.

摘要

由于有时会将通过皮肤吸收的药剂应用于受损屏障,因此比较了化合物通过不同方法损伤的皮肤的渗透情况。用玻璃纸胶带剥离皮肤去除角质层是增强吸收的最有效方法。用皮下针划一条磨损线时,水渗透率仅有微小增加,但在施用部位划三到六条线时,吸收则大幅增加。对于可的松和烟酸通过正常和磨损大鼠皮肤的渗透,体内和体外技术得到了相似的值。体内紫外线对大鼠的严重损伤导致烟酸吸收与体外通过磨损或胶带剥离皮肤获得的吸收相似。轻度照射造成的损伤无法通过体外方法准确复制。七种化学物质通过磨损的人和大鼠皮肤吸收增加的幅度与分子被皮肤吸收的程度有关。渗透率增加最大的是那些吸收最差的化合物。

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