Phenylephrine pharmaceutical formulations and compositions for colonic absorption
    1.
    发明授权
    Phenylephrine pharmaceutical formulations and compositions for colonic absorption 有权
    去氧肾上腺素药物制剂和用于结肠吸收的组合物

    公开(公告)号:US08956662B2

    公开(公告)日:2015-02-17

    申请号:US11756881

    申请日:2007-06-01

    摘要: The invention discloses a pharmaceutical composition comprising phenylephrine or a pharmaceutically acceptable salt thereof and an erodible layer which is for oral administration wherein the composition delivers phenylephrine or a pharmaceutically acceptable salt thereof via absorption in the colon. The pharmaceutical composition comprises a core comprising phenylephrine or a pharmaceutically acceptable salt thereof and an erodible layer which is in a time-dependent, pH-dependent, or colon-specific enzyme-dependent erodible layer that degrades to expose the core to release phenylephrine in the colon. In one preferred embodiment, the erodible layer encases the core. The composition optionally further comprises phenylephrine in the erodible layer or other additional layer(s). The pharmaceutical composition can further comprise one or more additional therapeutically active agents selected from one or more of the group consisting of antihistamines, analgesics, anti-pyretics, and non-steroidal anti-inflammatory agents. The invention also discloses methods of administering phenylephrine via the colon, thereby increasing the bioavailable amount of therapeutically active unconjugated phenylephrine relative to the total phenylephrine in the plasma.

    摘要翻译: 本发明公开了一种药物组合物,其包含去氧肾上腺素或其药学上可接受的盐和用于口服给药的可溶性层,其中所述组合物通过在结肠中的吸收递送苯肾上腺素或其药学上可接受的盐。 药物组合物包含包含去氧肾上腺素或其药学上可接受的盐的核心和可溶性层,其处于时间依赖性,依赖于pH或结肠特异性的酶依赖性可溶解层,其降解以暴露核心以释放出去氧肾上腺素 结肠。 在一个优选实施例中,可侵蚀层包裹芯。 所述组合物任选地还包含可腐蚀层或其它附加层中的去氧肾上腺素。 药物组合物还可以包含一种或多种另外的治疗活性剂,其选自抗组胺剂,止痛剂,抗热解剂和非甾体抗炎剂中的一种或多种。 本发明还公开了通过结肠施用苯肾上腺素的方法,从而相对于血浆中的总去氧肾上腺素增加了治疗活性的非共轭去氧肾上腺素的生物可利用量。