ABUSE RESISTANT LYSINE AMPHETAMINE COMPOUNDS
    76.
    发明申请
    ABUSE RESISTANT LYSINE AMPHETAMINE COMPOUNDS 有权
    抗生素赖氨酸AMPHETAMINE化合物

    公开(公告)号:US20080086016A1

    公开(公告)日:2008-04-10

    申请号:US11745019

    申请日:2007-05-07

    IPC分类号: C07C233/00

    摘要: The present invention describes compounds, compositions and methods of using the same comprising lysine covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

    摘要翻译: 本发明描述了使用其包含与苯丙胺共价连接的赖氨酸的化合物,组合物和方法。 这些化合物和组合物可用于减少或预防滥用和过量安非他明。 这些化合物和组合物特别用于提供某些障碍(例如注意力缺陷多动障碍(ADHD),ADD,发作性睡病和肥胖)的耐药性替代治疗。 苯丙胺的口服生物利用度维持在治疗有用的剂量。 在较高剂量下,生物利用度显着降低,从而提供减少口服滥用责任的方法。 此外,本发明的化合物和组合物通过肠胃外途径(例如静脉内或鼻内给药)降低苯丙胺的生物利用度,进一步限制其滥用责任。

    Abuse-resistant hydrocodone compounds
    77.
    发明授权
    Abuse-resistant hydrocodone compounds 有权
    滥用抗氢可可酮化合物

    公开(公告)号:US07338939B2

    公开(公告)日:2008-03-04

    申请号:US10953110

    申请日:2004-09-30

    IPC分类号: A61K38/00

    CPC分类号: A61K38/08 A61K47/64

    摘要: The present invention decreases the potential for abuse of opioids, particularly hydrocodone, by covalent modification. The invention provides methods of delivering hydrocodone as conjugates that release the hydrocodone following oral administration while being resistant to abuse by circuitous routes such as intravenous (“shooting”) injection and intranasal administration (“snorting”). Further, hydrocodone compositions of the invention are resistant to oral abuse as well, since release of the hydrocodone at suprapharmacological doses reaches saturation.

    摘要翻译: 本发明通过共价修饰降低了阿片样物质,特别是氢可酮的滥用的可能性。 本发明提供了递送氢可酮作为缀合物的方法,其在口服给药之后释放氢可酮,同时抵抗诸如静脉内(“射击”)注射和鼻内给药(“嗅觉”)等迂回途径的滥用。 此外,本发明的氢可酮组合物也耐口服滥用,因为以超药物剂量的氢可酮的释放达到饱和。