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1-十二烷基六氢-2H-氮杂䓬-2-酮(氮酮)对盐酸维拉帕米体外透过大鼠、无毛小鼠和人类尸体皮肤的影响。

Influence of 1-dodecylhexahydro-2H-azepin-2-one (Azone) on the in vitro permeation of verapamil hydrochloride across rat, hairless mouse, and human cadaver skin.

作者信息

Agrawala P, Ritschel W A

机构信息

Division of Pharmaceutics and Drug Delivery Systems, College of Pharmacy, University of Cincinnati Medical Center, OH 45267-0004.

出版信息

J Pharm Sci. 1988 Sep;77(9):776-8. doi: 10.1002/jps.2600770912.

DOI:10.1002/jps.2600770912
PMID:3225773
Abstract

The effect of 1-dodecylhexahydro-2H-azepine-2-one (Azone; laurocapran; 1) on the permeation of verapamil hydrochloride (2) through rat skin was studied. Compound 1 was used in various concentrations in the donor phase. The permeation of the drug increased significantly in the presence of 1 and the enhancement in permeation was dependent on the concentration of 1. A comparison of the enhancing effect of 3% 1 on permeation of 2 through rat, hairless mouse, and human cadaver skin was made. Compound 1 altered the permeability of hairless mouse skin significantly, whereas the effect on rat and human skin was comparable and not very drastic.

摘要

研究了1-十二烷基六氢-2H-氮杂卓-2-酮(氮酮;月桂氮卓酮;1)对盐酸维拉帕米(2)透过大鼠皮肤的影响。化合物1在供体相中以不同浓度使用。在存在1的情况下,药物的渗透显著增加,且渗透增强取决于1的浓度。比较了3%的1对2透过大鼠、无毛小鼠和人体尸体皮肤的增强作用。化合物1显著改变了无毛小鼠皮肤的渗透性,而对大鼠和人体皮肤的影响相当且不太显著。

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Disposition and metabolic profiling of the penetration enhancer Azone. I. In vitro studies: urinary profiles of hamster, rat, monkey, and man.渗透促进剂氮酮的处置与代谢谱分析。I. 体外研究:仓鼠、大鼠、猴及人类的尿液谱分析。
Pharm Res. 1990 May;7(5):496-9. doi: 10.1023/a:1015864632474.
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Use of shed snake skin as a model membrane for in vitro percutaneous penetration studies: comparison with human skin.
将蛇蜕作为体外经皮渗透研究的模型膜的应用:与人体皮肤的比较。
Pharm Res. 1990 Oct;7(10):1042-7. doi: 10.1023/a:1015943200982.