XENON AS NMDA ANTAGONIST for neuroprotection
    4.
    发明授权
    XENON AS NMDA ANTAGONIST for neuroprotection 无效
    氙作为NMDA拮抗剂用于神经保护

    公开(公告)号:EP1200103B1

    公开(公告)日:2008-08-13

    申请号:EP00948171.4

    申请日:2000-07-28

    申请人: Protexeon Limited

    IPC分类号: A61K33/00 A61P25/28 A61P25/36

    摘要: The present invention relates to the use of xenon as a neuroprotectant and/or as an inhibitor of synaptic plasticity. In a preferred aspect, the xenon acts as an NMDA antagonist. The present invention also provides a method of reducing the level of activation of the NMDA receptors in a mammal, the method comprising modulating the activity of the NMDA receptor by administering to the mammal a therapeutically effective amount of xenon, wherein said reduction achieves neuroprotection and/or an inhibition of synaptic plasticity. A further embodiment of the invention provides a pharmaceutical composition for providing neuroprotection and/or inhibition of synaptic plasticity, together with a process for the process for the preparation thereof.

    摘要翻译: 本发明涉及氙作为神经保护剂和/或作为突触可塑性抑制剂的用途。 在优选的方面,氙充当NMDA拮抗剂。 本发明还提供了降低哺乳动物NMDA受体活化水平的方法,所述方法包括通过向哺乳动物施用治疗有效量的氙来调节NMDA受体的活性,其中所述减少实现神经保护和/ 或抑制突触可塑性。 本发明的另一个实施方案提供用于提供神经保护和/或抑制突触可塑性的药物组合物,以及其制备方法。

    A MICROEMULSION PREPARATION OF HIGH CONCENTRATION PROPOFOL FOR ANESTHETIC USES
    6.
    发明公开
    A MICROEMULSION PREPARATION OF HIGH CONCENTRATION PROPOFOL FOR ANESTHETIC USES 审中-公开
    高度集中的异丙酚用于麻醉应用微乳液法制备

    公开(公告)号:EP1713444A1

    公开(公告)日:2006-10-25

    申请号:EP05713453.8

    申请日:2005-02-14

    IPC分类号: A61K9/113 A61K31/05

    摘要: The invention provides a method and a composition for enhancing the dissolution and bioavailable properties of propofol (2, 6 diisopropyl phenol) for use as an intravenously administered anesthetic in mammals. The method produces a self-microemulsifyable emulsion base composition that is utilized in the production of a water-based microemulsiori preparation. In a preferred two (2) component base composition, the base composition consists of: a surfactant, containing polyethylene glycol; and liquid propofol. The microemulsion is prepared by mixing the base composition with a carrier liquid, which results in the formation of a microemulsion containing concentrations of propofol of up to about 4% by weight of propofol to the volume of the microemulsion. In a four (4) component base composition, the base composition consists of: a surfactant, containing polyethylene glycol; liquid propofol; a water-immiscible solvent; and ethanol. The microemulsion is prepared by mixing the base composition with a carrier liquid, which results in the formation of a microemulsion containing concentrations of propofol of up to about 10% by weight of propofol to the volume of the microemulsion.