Compositions and methods employing aminopterin
    14.
    发明申请
    Compositions and methods employing aminopterin 有权
    使用氨蝶呤的组合物和方法

    公开(公告)号:US20050209239A1

    公开(公告)日:2005-09-22

    申请号:US11078614

    申请日:2005-03-09

    IPC分类号: A61K31/519

    CPC分类号: A61K31/519

    摘要: The present invention relates to pharmaceutical compositions containing the antifolate aminopterin, processes for making the compositions, and methods of using them to treat disorders in adult and pediatric patients. Pharmaceutical compositions substantially free of impurities are provided comprising a therapeutically effective amount of aminopterin, or a pharmaceutically acceptable salt thereof. Relative to the teachings of the prior art, the disclosed methods and compositions provide unexpected improvements that include a greater interpatient oral bioavailability in pediatric patients, a smaller interpatient coefficient of variation of oral bioavailability, a smaller mean intrapatient coefficient of variation of oral bioavailability, a greater therapeutic index, a smaller coefficient of variation of toxicity, efficacy in combination therapy, and efficacy of certain polyglutamated metabolites.

    摘要翻译: 本发明涉及含有抗叶酸氨蝶呤的药物组合物,用于制备组合物的方法,以及使用它们治疗成人和儿科患者的疾病的方法。 提供了基本上不含杂质的药物组合物,其包含治疗有效量的氨基喋呤或其药学上可接受的盐。 相对于现有技术的教导,所公开的方法和组合物提供意想不到的改进,其包括在儿科患者中具有更大的患者口服生物利用度,口服生物利用度的较小的间质变异系数,口服生物利用度的较小的平均脑室内变异系数 更大的治疗指数,较小的毒性变异系数,联合治疗的疗效以及某些聚谷氨酸代谢物的功效。