Particulate pharmaceutical composition
    1.
    发明授权
    Particulate pharmaceutical composition 有权
    颗粒状药物组成

    公开(公告)号:US09198860B2

    公开(公告)日:2015-12-01

    申请号:US13122546

    申请日:2011-02-14

    摘要: The present invention provides a particulate pharmaceutical composition which has improved drug encapsulation stability and is suitable for a drug delivery system. The particulate pharmaceutical composition 1 contains: a plurality of block copolymer unit 2 arranged radially, each of which has a hydrophobic polymer-chain segment 2b, which is arranged radially inside, and a hydrophilic polymer-chain segment 2a, which is arranged radially outside; a drug 4, which includes a biomacromolecule; and a charged lipid 3, which has an electrical charge opposite to that of the drug 4; wherein the charged lipid 3 is being attracted to the hydrophobic polymer-chain segment 2b, and the drug 3 is positioned radially inside the hydrophobic polymer-chain segment 2b. The pharmaceutical composition 1 can effectively prevent the drug 4 from disengaging from the particle.

    摘要翻译: 本发明提供了具有改善的药物包封稳定性并且适合于药物递送系统的颗粒药物组合物。 颗粒状药物组合物1包含:径向配置的多个嵌段共聚物单元2,其各自具有径向配置的疏水性聚合物链段2b和位于径向外侧的亲水性聚合物链段2a; 包括生物大分子的药物4; 和带电荷的脂质3,其具有与药物4的电荷相反的电荷; 其中带电脂质3被吸引到疏水聚合物链段2b,并且药物3位于疏水性聚合物链段2b的径向内侧。 药物组合物1可以有效地防止药物4与粒子分离。

    Method of Producing Coated Fine Particles
    4.
    发明申请
    Method of Producing Coated Fine Particles 审中-公开
    生产涂层微粒的方法

    公开(公告)号:US20080226704A1

    公开(公告)日:2008-09-18

    申请号:US10593723

    申请日:2005-03-23

    CPC分类号: B01J13/02 Y10T428/2989

    摘要: The present invention provides a method of producing coated fine particles in which core fine particles is coated with a coating layer, which comprises the steps of preparing a liquid (liquid A) containing a polar organic solvent in which core fine particles are dispersed and a component constituting a coating layer is dissolved; preparing a liquid (liquid B) which is miscible with the liquid A and does not contain a polar organic solvent or contains a polar organic solvent in a ratio lower than that in the liquid A; and letting the liquid A flow from at least one inlet of a device for producing coated fine particles equipped with an in-line mixing means having two or more inlets and one or more outlet(s) and letting the liquid B flow from at least one remaining inlet to mix the liquids thereby coating the core fine particles with the coating layer.

    摘要翻译: 本发明提供一种制备其中芯细颗粒涂覆有涂层的涂覆微粒的方法,该方法包括以下步骤:制备包含其中分散芯细颗粒的极性有机溶剂的液体(液体A)和组分 构成涂层溶解; 制备与液体A混溶并且不含极性有机溶剂或含有比液体A中的比例低的极性有机溶剂的液体(液体B); 并且使液体A从用于生产包含具有两个或更多个入口和一个或多个出口的直列混合装置的涂覆微粒的装置的至少一个入口流出并使液体B从至少一个流出 剩余的入口混合液体,从而涂覆核心微粒与涂层。

    Method Of Producing Coated Fine Particles
    5.
    发明申请
    Method Of Producing Coated Fine Particles 审中-公开
    生产涂层微粒的方法

    公开(公告)号:US20080171090A1

    公开(公告)日:2008-07-17

    申请号:US11883165

    申请日:2006-01-27

    摘要: An object of the present invention is to provide a method for easily producing coated fine particles in which core fine particles are coated with a coating layer component, etc. There are provided a method of producing coated fine particles comprising core fine particles coated with a coating layer component, comprising the steps of dispersing the core fine particles and the coating layer component(s) in a liquid and the process of coating the core fine particles with the coating layer component, wherein the liquid contains a polar organic solvent in which the coating layer component(s) is soluble, and the concentration of the polar organic solvent is such that the core fine particles is not dissolved and the coating layer component(s) can be in the dispersed state in the liquid, and the like.

    摘要翻译: 本发明的目的是提供一种容易地生产其中芯细颗粒涂覆有涂层组分等的涂覆微粒的方法。提供了一种制备涂覆微粒的方法,其包括涂覆有涂层的芯细颗粒 包括以下步骤:将芯细颗粒和涂层组分分散在液体中,以及用芯层细颗粒涂覆涂层组分的方法,其中液体含有极性有机溶剂,其中涂层 层组分是可溶的,并且极性有机溶剂的浓度使得芯细颗粒不溶解,并且涂层组分可以在液体中处于分散状态等。

    Sustained-release polymer micelle disruptable by HDL
    7.
    发明授权
    Sustained-release polymer micelle disruptable by HDL 有权
    持续释放的聚合物胶束可被HDL破坏

    公开(公告)号:US08574601B2

    公开(公告)日:2013-11-05

    申请号:US13258797

    申请日:2011-02-07

    IPC分类号: A61K38/02 A61K9/00

    CPC分类号: A61K9/1075 A61K9/0019

    摘要: A pharmaceutical composition containing a drug encapsulated in a polymer micelle composition containing a first block copolymer having affinity with HDL and a second block copolymer having affinity with a lipoprotein excluding HDL, each block copolymer having a hydrophobic polymer chain segment and a hydrophilic polymer chain segment such that a plurality of block copolymers arrange radially with the hydrophobic segments directed inward and the hydrophilic segments directed outward. In the composition, a detachment of the first block copolymer is induced by HDL adhesion which forms a gap and promotes the release of a drug encapsulated, while the second block copolymer excluding an affinity with HDL controls a release speed of the drug encapsulated.

    摘要翻译: 一种药物组合物,其包含包含在与HDL亲和性的第一嵌段共聚物的聚合物胶束组合物中的药物和与除了HDL之外的脂蛋白具有亲和性的第二嵌段共聚物,每个嵌段共聚物具有疏水性聚合物链段和亲水性聚合物链段, 多个嵌段共聚物径向布置,其中疏水片段向内指向,亲水片段向外指向。 在组合物中,第一嵌段共聚物的脱离是由HDL粘附引起的,其形成间隙并促进包封的药物的释放,而不包括与HDL的亲和力的第二嵌段共聚物控制包封的药物的释放速度。

    COMPOUND MODIFIED WITH GLYCEROL DERIVATIVE
    8.
    发明申请
    COMPOUND MODIFIED WITH GLYCEROL DERIVATIVE 审中-公开
    用甘油衍生物修饰的化合物

    公开(公告)号:US20100172967A1

    公开(公告)日:2010-07-08

    申请号:US12708714

    申请日:2010-02-19

    摘要: Objects of the present invention are to provide a compound which is useful as a surface modifier for producing a drug carrier or the like, or a salt thereof; a fine particle comprising the same; and the like. The present invention provides a compound in which a substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance, is modified with a glycerol derivative represented by the following formula (1): wherein R represents a residue comprising a reactive group for the substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance or for a spacer capable of binding the substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance, to R—X, or a group capable of being transformed into the reactive group; n represents an integer of 3 or more; and X represents a residue capable of having the following structure by n in number: directly or via the spacer, or a salt thereof; a fine particle comprising the same; and the like.

    摘要翻译: 本发明的目的是提供一种可用作生产药物载体等的表面改性剂或其盐的化合物; 包含该颗粒的细颗粒; 等等。 本发明提供一种化合物,其中选自由两亲物质和疏水性物质组成的组中的被改性物质用下式(1)表示的甘油衍生物进行改性:其中R表示残基 包括选自两亲物质和疏水性物质的待修饰物质的反应性基团或能够与被修饰物质结合的间隔基,其选自两亲物质 和疏水性物质,R-X或能够转化为反应性基团的基团; n表示3以上的整数, X表示可以直接或经由间隔基或其盐具有n数的以下结构的残基: 包含该颗粒的细颗粒; 等等。

    Compound modified with glycerol derivative
    10.
    发明授权
    Compound modified with glycerol derivative 失效
    用甘油衍生物修饰的化合物

    公开(公告)号:US07696359B2

    公开(公告)日:2010-04-13

    申请号:US10570623

    申请日:2004-09-03

    IPC分类号: C07D207/46 C07F9/09

    摘要: Objects of the present invention are to provide a compound which is useful as a surface modifier for producing a drug carrier or the like, or a salt thereof; a fine particle comprising the same; and the like. The present invention provides a compound in which a substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance, is modified with a glycerol derivative represented by the following formula (1): wherein R represents a residue comprising a reactive group for the substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance or for a spacer capable of binding the substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance, to R-X, or a group capable of being transformed into the reactive group; n represents an integer of 3 or more; and X represents a residue capable of having the following structure by n in number: directly or via the spacer, or a salt thereof; a fine particle comprising the same; and the like.

    摘要翻译: 本发明的目的是提供一种可用作生产药物载体等的表面改性剂或其盐的化合物; 包含该颗粒的细颗粒; 等等。 本发明提供一种化合物,其中选自由两亲物质和疏水性物质组成的组中的被改性物质用下式(1)表示的甘油衍生物进行改性:其中R表示残基 包括选自两亲物质和疏水性物质的待修饰物质的反应性基团或能够与被修饰物质结合的间隔基,其选自两亲物质 和疏水性物质,至RX或能够转化为反应性基团的基团; n表示3以上的整数, X表示可以直接或经由间隔基或其盐具有n数的以下结构的残基: 包含该颗粒的细颗粒; 等等。