文章基本信息

标题：Evaluation of a Pharmaceutical Preparation of 2-[4-(p-Fluorobenzoyl)-piperidin-1-yl]-2'-acetonaphthone Hydrochloride with Enhanced Dissolution Rate
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作者：Tadakazu TOKUMURA ; Tomohide TANAKA
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1994
卷号：17
期号：8
页码：1138-1140
DOI：10.1248/bpb.17.1138
出版社：The Pharmaceutical Society of Japan
摘要：A granule of 2-[4-(p-fluorobenzoyl)-piperidin-1-yl]-2'-acetonaphthone hydrochloride (E2001) with an enhanced dissolution rate (preparation A) prepared by a method previously reported (T. Tokumura, T. Tanaka, Yakuzaigaku, accepted) was evaluated by the dissolution test and its bioavailability in beagle dogs was determined. The dissolution rate of E2001 from preparation A at pH 6.0-6.8 was increased significantly in comparison with that from preparation B (a physical mixture of the same formula). There was no significant difference in C_max, area under the concentration-time curve (AUC_0-6h), or T_max between preparations A and B when a dose equivalent to 20 mg of E2001 was administered to the beagle dogs. However, a significant difference was observed between the AUC_0-6h values after oral administration of the two preparations with NaHCO₃. These findings suggest that the bioavailability of E2001 from the oral administration preparation A will be higher than that of preparation B.
关键词：anti-ischemic agent;dissolution rate;bioavailability;beagle dog;pH