文章基本信息

标题：Absorption Characteristics of Azasetron from Rectal and Oral Routes in Rabbits
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作者：Yuhsuke MORIYAMA ; Kazuhiko ARIMORI ; Masahiro NAKANO 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：1997
卷号：20
期号：6
页码：701-703
DOI：10.1248/bpb.20.701
出版社：The Pharmaceutical Society of Japan
摘要：The absorption characteristics of azasetron, a serotonin type 3 (5-HT₃) receptor antagonist which is used for the treatment of chemotherapy-induced emesis and nausea, were investigated in rabbits. The serum concentrations of azasetron following rectal administration as a suppository increased rapidly and showed the mean t_max value of 0.18 h. The concentrations were greater after rectal administration than those after oral administration. The absolute bioavailability was significantly different between the rectal, 52.9% and oral doses, 21.6%. The mean C_max and t_max values after the rectal dose were 904.8 ng/ml and 0.18 h, respectively, whereas those after the oral dose averaged 124.7 ng/ml and 0.85 h, respectively.These results indicate that azasetron in absorbed to a greater extent and more rapidly into the systemic circulation via the rectum than via the intestine in rabbits. Consequently, the suppository form azasetron hydrochloride may be feasible for the treatment of chemotherapy-induced acute emesis and nausea.
关键词：azasetron;suppository;serotonin type 3 inhibitor;bioavailability