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    • 1. 发明申请
    • Specific time-delayed burst profile delivery system
    • 具体的延时突发配置文件传送系统
    • US20060280795A1
    • 2006-12-14
    • US11147388
    • 2005-06-08
    • Adel PenhasiMila GombergMaxim Gomberg
    • Adel PenhasiMila GombergMaxim Gomberg
    • A61K9/24
    • A61K9/2886A61K9/4891
    • The invention provides a delivery device for the delayed release of an active agent in the gastrointestinal tract comprising a core, comprising an active agent; a first outer coating, comprising a relatively hydrophobic substantially water insoluble polymer having substantially water insoluble hydrophilic particles embedded therein; and a first inner coating layer, comprising an agent that can cause the dissolution of at least one of the water insoluble components of the outer coating, and optionally a water soluble polymer, such that the insoluble particles in the outer coating, upon absorption of liquid, form channels leading to the inner coating layer, thus enabling the dissolution thereof, whereby the agents contained therein are released to cause the dissolution and/or degradation (destruction) of the outer coating, and the release of the pharmaceutically acceptable active agent from the core of the device.
    • 本发明提供了用于在胃肠道中延迟释放活性剂的递送装置,其包含核心,其包含活性剂; 第一外涂层,其包含相对疏水的基本上不溶于水的聚合物,其中嵌有基本上不溶于水的亲水性颗粒; 以及第一内涂层,其包含可引起外涂层的至少一种水不溶性组分和任选的水溶性聚合物的溶解的试剂,使得外涂层中的不溶性颗粒在吸收液体时 形成通向内涂层的通道,从而使其溶解,由此其中所含的试剂被释放以引起外涂层的溶解和/或降解(破坏),并且药学上可接受的活性剂从 设备的核心
    • 7. 发明申请
    • Localized controlled absorption of statins in the gastrointestinal tract for achieving high blood levels of statins
    • 他汀类药物在胃肠道局部控制吸收,达到高血糖的他汀类药物
    • US20060251720A1
    • 2006-11-09
    • US11305544
    • 2005-12-15
    • Adel PenhasiMaxim Gomberg
    • Adel PenhasiMaxim Gomberg
    • A61K31/401A61K31/366A61K31/22A61K9/22
    • A61K31/366A61K9/2027A61K9/2054A61K9/2077A61K9/2846A61K9/2866A61K9/2886A61K31/22A61K31/401
    • The present invention relates to a localized controlled absorption formulation of a statin in which rapid release of the active ingredient preferentially occurs in the lower gastrointestinal tract including the colon. The formulation provides significantly higher blood level concentration and bioavailability of the active ingredient in the body of a subject as compared to the bioavailability achieved from the currently available conventional formulations The blood levels are maintained for a significantly longer period of time as compared with currently available conventional formulations. The formulation preferably includes a core, over which an outer coating is layered. The core preferably includes a burst controlling agent and optionally a disintegrant. The outer coating includes a water insoluble polymer and at least one water permeable agent allowing entry of water into said core, the water permeable agent comprising hydrophilic particulate matter. The core is preferably in the form of a tablet.
    • 本发明涉及他汀类的局部受控吸收制剂,其中活性成分的快速释放优先发生在包括结肠的下胃肠道中。 与目前可获得的常规制剂相比,该制剂提供了与受试者体内活性成分相比显着更高的血液浓度和生物利用度。与目前可获得的常规制剂相比,血液水平维持较长的时间 配方。 该制剂优选包括芯,在其上分层外涂层。 核心优选包括爆发控制剂和任选的崩解剂。 外涂层包括水不溶性聚合物和允许水进入所述核心的至少一种水可渗透剂,所述水可渗透剂包含亲水性颗粒物质。 核心优选为片剂的形式。