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标题：In Vitro Metabolism Study of Edaravone in Wistar and Hairless Rat Skin
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作者：Toshiaki Sato ; Keizo Mizuno ; Fumiyoshi Ishii 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：2008
卷号：31
期号：6
页码：1150-1154
DOI：10.1248/bpb.31.1150
出版社：The Pharmaceutical Society of Japan
摘要：We investigated the skin metabolism of edaravone as a radical scavenger in Wistar and hairless rat skin. Approximately 1 g of abdominal skin was excised from 10-week-old Wistar and hairless rats, homogenized in 10 ml saline, and centrifuged at 10000 g for 20 min. The supernatant fluid was used for the examination of edaravone metabolism in the skin, and we also used supernatant fluid that was heated at 80 °C. Edaravone solution (0.05 ml, 2.4 μmol/ml) was added to 0.95 ml Wistar rat and hairless rat skin homogenate supernatant fluids. In Wistar rats, the residual amount of edaravone in skin homogenate supernatant fluid at 37 °C after 0, 5, 10, 20 and 30 min was 61.58±1.65, 41.84±8.52, 35.54±8.62, 19.73±5.99 and 13.89±4.40%, respectively. In hairless rats, the residual amount of edaravone in skin homogenate supernatant fluid at 37 °C after 0, 5 and 10 min was 50.19±14.17, 6.71±5.82 and 0.89±0.80%, respectively, and edaravone was not detected after 20 min. Although it was thought that metabolic enzyme activity in skin homogenate supernatant fluid was lost following heat treatment at 80 °C, the residual amount of edaravone in our skin homogenate supernatant fluid decreased with time. It is suggested that edaravone metabolism in the skin is necessary for non-enzymatic reactions.
关键词：edaravone;Wistar rat skin;hairless rat skin;HPLC;drug metabolism