SUSTAINED-RELEASE LIPID PRE-CONCENTRATE OF GNRH ANALOGUES AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
    2.
    发明申请
    SUSTAINED-RELEASE LIPID PRE-CONCENTRATE OF GNRH ANALOGUES AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME 审中-公开
    GNRH类似物的持续释放脂肪预浓缩物和包含其的药物组合物

    公开(公告)号:WO2014104791A1

    公开(公告)日:2014-07-03

    申请号:PCT/KR2013/012269

    申请日:2013-12-27

    Abstract: Disclosed is a pharmaceutical composition, comprising: a) at least one sorbitan unsaturated fatty acid ester having a polar head with at least two or more -OH (hydroxyl) groups; b) at least one phospholipid; c) at least one liquid crystal hardener which is free of an ionizable group and has a triacyl group with 15 to 40 carbon atoms or a carbon ring structure in a hydrophobic moiety; and d) at least one GnRH (gonadotropin-releasing hormone) analogue as a pharmacologically active substance, wherein said lipid pre-concentrate exists as a liquid phase in absence of aqueous fluid and forms into a liquid crystal in presence of aqueous fluid. The pharmaceutical composition is configured to enhance the sustained release of the pharmacologically active substance GnRH analogue.

    Abstract translation: 公开了一种药物组合物,其包含:a)至少一种具有至少两个或更多个-OH(羟基)基团的极性头的脱水山梨糖醇不饱和脂肪酸酯; b)至少一种磷脂; c)至少一种不含可离子化基团且具有15至40个碳原子的三酰基或疏水部分中的碳环结构的液晶硬化剂; 和d)至少一种GnRH(促性腺激素释放激素)类似物作为药理学活性物质,其中所述脂质预浓缩物以不含水流体的形式存在,并在含水流体存在下形成液晶。 药物组合物被配置为增强药理活性物质GnRH类似物的持续释放。

    SUSTAINED-RELEASE LIPID PRE-CONCENTRATE OF ANIONIC PHARMACOLOGICALLY ACTIVE SUBSTANCES AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
    4.
    发明申请
    SUSTAINED-RELEASE LIPID PRE-CONCENTRATE OF ANIONIC PHARMACOLOGICALLY ACTIVE SUBSTANCES AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME 审中-公开
    持久释放脂质预先浓缩的化学药物活性物质和包含其的药物组合物

    公开(公告)号:WO2014104788A1

    公开(公告)日:2014-07-03

    申请号:PCT/KR2013/012265

    申请日:2013-12-27

    CPC classification number: A61K47/24 A61K9/0019 A61K9/107 A61K31/439 A61K31/69

    Abstract: Disclosed is a sustained-release lipid pre-concentrate, comprising: a) at least one liquid crystal former; b) at least one phospholipid; c) at least one liquid crystal hardener; and d) at least one bi- or multivalent metal salt, wherein the sustained-release pre-concentrate exists as a lipid liquid phase in the absence of aqueous fluid and forms into a liquid crystal upon exposure to aqueous fluid. The sustained-release lipid pre-concentrate is configured to enhance the sustained release of anionic pharmacologically active substances through ionic interaction between the bi- or multivalent metal salt and the anionic pharmacologically active substances.

    Abstract translation: 公开了一种持续释放的脂质预浓缩物,其包含:a)至少一种液晶成形剂; b)至少一种磷脂; c)至少一种液晶硬化剂; 和d)至少一种二价或多价金属盐,其中所述持续释放预浓缩物在不存在水性流体时作为脂质液相存在,并且在暴露于含水流体时形成液晶。 缓释脂质预浓缩物被配置为通过二价金属盐和阴离子药理活性物质之间的离子相互作用来增强阴离子药理学活性物质的持续释放。

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