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氯喹那多( Sterosan)的经皮吸收

Percutaneous absorption of chlorquinaldol (Sterosan).

作者信息

Degen P H, Moppert J, Schmid K, Weirich E G

出版信息

Dermatologica. 1979;159(3):239-44. doi: 10.1159/000250600.

Abstract

The percutaneous absorption of chlorquinaldol from three different preparations for skin treatment (Sterosan-hydrocortison ointment and cream, Sterosan ointment) was evaluated by measuring the cumulative urinary excretion of chlorquinaldol and was compared to that found after an equivalent oral dose. In the blood the concentrations were below the detection limit of the analytical procedure, i.e., smaller than 0.02 microgram/ml. The study was carried out in 3 healthy volunteers using a four-period change-over design. The topical preparations were applied under occlusive dressings. Following epicutaneous application of the three topicals in quantities containing 30 mg chlorquinaldol each, the mean urinary excretion of the drug amounted to 11.1 +/- 6.6, 19.5 +/- 3.5 and 13.0 +/- 2.5% of the applied dose. When the same dose of chlorquinaldol was administered orally, 67.6 +/- 9.5% of the dose was excreted in the urine. Taking the urinary elimination as the minimal amount of drug absorbed, the extent of percutaneous absorption from the three dermatological preparations varied between 4.2 and 23.5% of the applied dose. There was no difference in the pattern of urinary excretion products among the three topicals and the oral formulation. The bulk of chlorquinaldol (mean 98.0 +/- 0.1%) was excreted as sulfate (mean 1.3 +/- 0.3%) or unchanged drug (mean 0.8 +/- 0.1%).

摘要

通过测量氯喹那多的累积尿排泄量,评估了三种不同皮肤治疗制剂(Sterosan - 氢化可的松软膏和乳膏、Sterosan软膏)中氯喹那多的经皮吸收情况,并与等量口服剂量后的情况进行了比较。血液中的浓度低于分析方法的检测限,即小于0.02微克/毫升。该研究在3名健康志愿者中采用四周期交叉设计进行。局部制剂在封闭敷料下应用。在分别应用含30毫克氯喹那多的三种局部制剂后,药物的平均尿排泄量分别为给药剂量的11.1±6.6%、19.5±3.5%和13.0±2.5%。当口服相同剂量的氯喹那多时,67.6±9.5%的剂量经尿液排泄。以尿排泄作为吸收的最小药物量,三种皮肤科制剂的经皮吸收程度在给药剂量的4.2%至23.5%之间变化。三种局部制剂和口服制剂的尿排泄产物模式没有差异。大部分氯喹那多(平均98.0±0.1%)以硫酸盐(平均1.3±0.3%)或未变化的药物(平均0.8±0.1%)形式排泄。

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