Benzamide formulation with histone deacetylase inhibitor activity
    62.
    发明授权
    Benzamide formulation with histone deacetylase inhibitor activity 失效
    具有组蛋白脱乙酰酶抑制剂活性的苯甲酰胺制剂

    公开(公告)号:US06638530B1

    公开(公告)日:2003-10-28

    申请号:US10069582

    申请日:2002-02-27

    IPC分类号: A61K966

    摘要: There are provided pharmaceutical formulations with improved oral absorptivity and injections that contain, as active ingredients, high concentrations of benzamide derivatives and their pharmaceutically acceptable salts, which are useful as histone deacetylase inhibitors. A pharmaceutical solution is prepared by dissolving a benzamide derivative or a pharmaceutically acceptable salt thereof in an organic solvent and/or acidic liquid, and a pharmaceutical formulation is prepared by adding a surfactant, an acidic substance and/or a polyethylene glycol. The present invention has enabled dissolution of benzamide derivatives or their pharmaceutically acceptable salts at high concentrations, to prepare practical injections and oral liquid formulations and improve absorptivity with oral administration.

    摘要翻译: 提供具有改进的口服吸收性和注射剂的药物制剂,其含有作为活性成分的高浓度苯甲酰胺衍生物及其药学上可接受的盐,其可用作组蛋白脱乙酰酶抑制剂。药物溶液通过将苯甲酰胺衍生物或药物 在有机溶剂和/或酸性液体中可接受的盐,并且通过加入表面活性剂,酸性物质和/或聚乙二醇制备药物制剂。本发明使苯甲酰胺衍生物或其药学上可接受的盐在高温下溶解 浓度,以制备实用的注射剂和口服液体制剂,并通过口服给药改善吸收性。