文章基本信息

标题：Effect of Ethanol on the Binding of Warfarin Enantiomers to Human Serum Albumin
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作者：Akitoshi Tatsumi ; Muneo Kadobayashi ; Seigo Iwakawa 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2007
卷号：30
期号：4
页码：826-829
DOI：10.1248/bpb.30.826
出版社：The Pharmaceutical Society of Japan
摘要：Ethanol is widely used as a pharmaceutical excipient for the solubilization of many hydrophobic drugs for injections. However, there are only few studies about drug interaction with pharmaceutical excipients in the body after injection. In this study, the effect of ethanol (500 m M ) or several alcohols (500 m M ) on the stereoselective binding of warfarin enantiomers to fatty acid-free human serum albumin (HSA) or proteins of commercial albumin preparations was investigated. An ultrafiltration method was used for the separation of unbound warfarin enantiomers. By the addition of ethanol or 1-propanol, the unbound fraction of the S -enantiomer was decreased. On the other hand, the unbound fraction of the R -enantiomer was increased by the addition of ethanol or 1-propanol. Unbound fractions of both the S - and R -enantiomer were decreased by 2-propanol. In various commercial albumin preparations, unbound fractions of both the S - and R -enantiomer were increased by ethanol. The different effects of ethanol among fatty acid-free HSA and commercial albumin preparations were observed.
关键词：warfarin;ethanol;protein binding;stereoselectivity;human serum albumin;commercial albumin preparation