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    Method for delivering drugs to the brain
    1.
    发明申请
    Method for delivering drugs to the brain 有权
    向大脑输送药物的方法

    公开(公告)号：US20050048002A1

    公开(公告)日：2005-03-03

    申请号：US10868680

    申请日：2004-06-15

    申请人： Barrett Rabinow ,  James Kipp ,  Howard Gendelman

    发明人： Barrett Rabinow ,  James Kipp ,  Howard Gendelman

    IPC分类号： A61K9/00 ,  A61K9/51 ,  A61K47/48 ,  A61L9/04 ,  A61K9/14

    CPC分类号： A61K9/00 ,  A61K9/0085 ,  A61K9/5123 ,  A61K9/5146 ,  A61K47/6901

    摘要： The present invention is concerned with delivering a pharmaceutical composition to the brain of a mammalian subject for treating brain diseases or disorders. The process includes the steps of: (i) providing a dispersion of the pharmaceutical composition as particles having an average particle size of from about 150 nm to about 100 microns, and (ii) administering the dispersion to the mammalian subject for delivery to the brain of a portion of the pharmaceutical composition by cells capable of reaching the brain. The dispersion of the pharmaceutical composition as particles, for example, can be phagocytised or adsorbed by the cells prior or subsequent to administration into the mammalian subject. The dispersion of the pharmaceutical composition can be administered to the central nervous system or the vascular system. After administration, the loaded cells transport the pharmaceutical composition as particles into the brain.

    摘要翻译： 本发明涉及向哺乳动物受试者的脑中递送药物组合物以治疗脑部疾病或病症。 该方法包括以下步骤：（i）提供药物组合物的分散体作为平均粒度为约150nm至约100微米的颗粒，和（ii）向哺乳动物受试者施用分散体以递送至脑 的药物组合物的一部分能够到达脑的细胞。 例如，作为颗粒的药物组合物的分散体可以在给予哺乳动物受试者之前或之后被细胞吞噬或吸附。 药物组合物的分散体可以施用于中枢神经系统或血管系统。 给药后，负载的细胞将药物组合物作为颗粒输送到脑中。

    Method for delivering particulate drugs to tissues
    2.
    发明申请
    Method for delivering particulate drugs to tissues 有权
    将颗粒药物递送至组织的方法

    公开(公告)号：US20060280430A1

    公开(公告)日：2006-12-14

    申请号：US11406986

    申请日：2006-04-19

    申请人： Barrett Rabinow ,  Howard Gendelman ,  James Kipp

    发明人： Barrett Rabinow ,  Howard Gendelman ,  James Kipp

    IPC分类号： G11B27/00

    CPC分类号： A61K9/0085 ,  A61K9/10 ,  A61K9/5123 ,  A61K9/5146 ,  A61K47/6901

    摘要： The present invention is concerned with delivering a pharmaceutical composition to a tissue target of a mammalian subject for treating brain diseases or disorders. The process includes the steps of: (i) providing a dispersion of the pharmaceutical composition as particles having an average particle size of from about 150 nm to about 100 microns, and (ii) administering the dispersion to the mammalian subject for delivery to the tissue target of a portion of the pharmaceutical composition by cells capable of reaching the tissue target. The dispersion of the pharmaceutical composition as particles, for example, can be phagocytised or adsorbed by the cells prior or subsequent to administration into the mammalian subject. The dispersion of the pharmaceutical composition can be administered to the central nervous system or the vascular system. After administration, the loaded cells transport the pharmaceutical composition as particles into the tissue target.

    摘要翻译： 本发明涉及将药物组合物递送至哺乳动物受试者的组织靶以治疗脑部疾病或病症。 该方法包括以下步骤：（i）提供药物组合物的分散体作为平均粒度为约150nm至约100微米的颗粒，和（ii）向哺乳动物受试者施用分散体以递送至组织 通过能够到达组织靶的细胞的一部分药物组合物的靶标。 例如，作为颗粒的药物组合物的分散体可以在给予哺乳动物受试者之前或之后被细胞吞噬或吸附。 药物组合物的分散体可以施用于中枢神经系统或血管系统。 给药后，负载的细胞将药物组合物作为颗粒输送到组织靶中。

    Ex-vivo application of solid microparticulate therapeutic agents
    4.
    发明申请
    Ex-vivo application of solid microparticulate therapeutic agents 有权
    离体应用固体微粒治疗剂

    公开(公告)号：US20050276861A1

    公开(公告)日：2005-12-15

    申请号：US11148453

    申请日：2005-06-09

    申请人： James Kipp ,  Barrett Rabinow

    发明人： James Kipp ,  Barrett Rabinow

    IPC分类号： A61K9/14 ,  A61K35/12 ,  A61K45/00 ,  A61K47/48 ,  A61K49/00 ,  C12N5/06

    CPC分类号： A61K49/0002 ,  A61K9/14 ,  A61K35/12 ,  A61K47/6901 ,  A61K2035/124

    摘要： The present invention is concerned with a method of preparing and delivering small particles of a pharmaceutically active material to a mammalian subject for treating diseases or disorders. A preferred embodiment entails: (i) the collection of tissue cells from an animal donor, (ii) selective or non-selective growth of these cells in a cell culture medium to which is added solid particles of a therapeutically active compound, mostly free of a drug carrier (about 10% or less, by weight), and having an average particle size of less than about 100 microns, (iii) contacting the cells in the cell culture medium with the solid particles of therapeutically active compound causing the particles to be taken up by the cells into either the intracellular compartment of the cultured cells, attachment of the active compound as particles to the periphery of such cells, or a combination of intracellular uptake and attachment to the cell surface, (iv) optionally, isolation and/or resuspension of the cells prepared in steps i through iii, (v) administering the cells to the mammalian subject. The pharmaceutically active material can be administered intravenously, intramuscularly, subcutaneously, intradermally, intra-articularly, intrathecally, epidurally, intracerebrally, via buccal route, rectally, topically, transdermally, orally, intranasally, via pulmonary route, intraperitoneally, or combinations thereof. After administration, the loaded cells transport the pharmaceutical composition as particles.

    摘要翻译： 本发明涉及制备和递送药物活性物质的小颗粒到哺乳动物受试者中用于治疗疾病或病症的方法。 优选的实施方案包括：（i）从动物供体收集组织细胞，（ii）这些细胞在细胞培养基中的选择性或非选择性生长，其中加入主要不含 药物载体（约10重量％或更少，重量百分比），平均粒径小于约100微米，（iii）使细胞培养基中的细胞与治疗活性化合物的固体颗粒接触， 被细胞吸收到培养细胞的细胞内区室中，将活性化合物作为颗粒附着到这种细胞的周边，或细胞内摄取和附着到细胞表面的组合，（iv）任选的分离和 /或在步骤i至iii中制备的细胞的再悬浮，（v）向哺乳动物受试者施用细胞。 药物活性物质可以通过静脉内，肌内，皮下，皮内，关节内，鞘内，硬膜外，脑内，经口颊途径，直肠，局部，经皮，口服，鼻内，经由肺途径，腹膜内或其组合施用。 给药后，加载的细胞将药物组合物作为颗粒运输。

    (Polyalkoxy)sulfonate surface modifiers
    6.
    发明申请
    (Polyalkoxy)sulfonate surface modifiers 有权
    （聚烷氧基）磺酸盐表面改性剂

    公开(公告)号：US20060141048A1

    公开(公告)日：2006-06-29

    申请号：US11304421

    申请日：2005-12-15

    申请人： James Kipp ,  Ton Hai ,  Bennett Melnick

    发明人： James Kipp ,  Ton Hai ,  Bennett Melnick

    IPC分类号： A61K9/14

    CPC分类号： C08G65/334 ,  A61K8/90 ,  A61K9/146 ,  A61K47/34 ,  A61Q19/00 ,  C08G65/326 ,  C08L71/02

    摘要： The present invention is directed to novel compounds, methods of manufacture and methods of use. The present invention is also directed to solid drug/active agent particles having one or more of the compounds of the present invention associated with the surface thereof. The compounds of the present invention are comprised of a non-polar polyether covalently linked to an anionic sulfonate group. The compounds have an amphipathic quality and preferably, are surface active. Such compounds are preferably useful as surface-active agents to coat and stabilize dispersions of particles in a continuous liquid medium. These surface-active agents may be applied in the stabilization of suspensions, emulsions, or liposome formulations intended for pharmaceutical, medical, cosmetic, or agricultural use. The particles that can be prepared by a variety of methods and will preferably comprise a pharmaceutical agent. Pharmaceutical compositions of the present invention can be used to treat a myriad of conditions and can be administered by many routes, including intravenous, intramuscular, subcutaneous, intrathecal, subdural, intracameral, intracerebral, intralesional, topical, oral, buccal, rectal, transcutaneous, pulmonary, and nasal.

    摘要翻译： 本发明涉及新化合物，制备方法和使用方法。 本发明还涉及具有一种或多种与其表面相关的本发明化合物的固体药物/活性剂颗粒。 本发明的化合物由与阴离子磺酸盐基团共价连接的非极性聚醚组成。 该化合物具有两性质量，优选表面活性。 这些化合物优选用作表面活性剂以涂覆和稳定颗粒在连续液体介质中的分散体。 这些表面活性剂可以用于稳定用于制药，医疗，化妆品或农业用途的悬浮液，乳剂或脂质体制剂。 可以通过多种方法制备并且优选包含药剂的颗粒。 本发明的药物组合物可用于治疗无数的病症，并且可以通过许多途径施用，包括静脉内，肌肉内，皮下，鞘内，硬膜下，阴道内，脑内，肠内，局部，口腔，口腔，直肠，经皮， 肺和鼻。

    Preparation and Use of a Stable Formulation of Allosteric Effector Compounds
    7.
    发明申请
    Preparation and Use of a Stable Formulation of Allosteric Effector Compounds 审中-公开
    稳定配方的变构效应剂的制备和应用

    公开(公告)号：US20070212302A1

    公开(公告)日：2007-09-13

    申请号：US11749610

    申请日：2007-05-16

    申请人： Douglas Johnson ,  Mark Doty ,  James Kipp

    发明人： Douglas Johnson ,  Mark Doty ,  James Kipp

    IPC分类号： A61K31/205 ,  A61B5/055

    CPC分类号： A61K31/195 ,  A61K9/0019 ,  A61K47/12 ,  A61K47/18 ,  A61K47/183 ,  A61K49/10

    摘要： A pharmaceutical composition of 2-[4-[2-[(3,5-dimethylphenyl)amino]-2-oxoethyl]phenoxy]-2-methyl-propionic acid or its physiologically acceptable salts suitable for parenteral administration includes an aqueous formulation of 2-[4-[2-[(3,5-dimethylphenyl)amino]-2-oxoethyl]phenoxy]-2-methyl-propionic acid or its physiologically acceptable salt and a buffer to maintain the pH from about 6 to about 11. The composition in accordance with the invention reduces the amount of particulate matter that forms in solution after heat sterilization. The invention also includes a process for making a pharmaceutical composition of 2-[4-[2-[(3,5-dimethylphenyl)amino]-2-oxoethyl]phenoxy]-2-methyl-propionic acid or its physiologically acceptable salt that has a shelf life in excess of thirty days and is useful in parenteral administration.

    摘要翻译： 2- [4- [2 - [（3,5-二甲基苯基）氨基] -2-氧代乙基]苯氧基] -2-甲基 - 丙酸或其适用于胃肠外给药的生理学上可接受的盐的药物组合物包括 2- [4- [2 - [（3,5-二甲基苯基）氨基] -2-氧代乙基]苯氧基] -2-甲基 - 丙酸或其生理上可接受的盐和缓冲液，以将pH保持在约6至约11 根据本发明的组合物减少加热灭菌后在溶液中形成的颗粒物质的量。 本发明还包括制备2- [4- [2 - [（3,5-二甲基苯基）氨基] -2-氧代乙基]苯氧基] -2-甲基 - 丙酸或其生理上可接受的盐的药物组合物的方法， 保质期超过30天，可用于肠胃外给药。

    Submicron suspensions with polymorph control
    8.
    发明申请
    Submicron suspensions with polymorph control 审中-公开
    具有多态性控制的亚微米悬浮液

    公开(公告)号：US20060134150A1

    公开(公告)日：2006-06-22

    申请号：US11283397

    申请日：2006-02-27

    申请人： Jane Werling ,  James Kipp ,  Rajaram Sriram ,  Mark Doty

    发明人： Jane Werling ,  James Kipp ,  Rajaram Sriram ,  Mark Doty

    IPC分类号： A61K9/00

    CPC分类号： A61K9/10 ,  A61K9/14 ,  A61K9/145 ,  A61K9/146 ,  A61K9/1688 ,  A61K31/495 ,  A61K31/496

    摘要： The present invention provides a method for preparing a suspension of a pharmaceutically active compound, the solubility of which is greater in a water miscible first organic solvent than in a second solvent which is aqueous, The process includes the steps of: (i) dissolving a first quantity of the pharmaceutically active compound in the water miscible first organic solvent to form a first solution; (ii) mixing the first solution with the second solvent to precipitate the pharmaceutically active compound; and (iii) seeding the first solution or the second solvent or the presuspension.

    摘要翻译： 本发明提供了一种制备药物活性化合物的悬浮液的方法，所述药物活性化合物的溶解度在与水相混溶的第一有机溶剂中大于在水溶液中的溶解度。该方法包括以下步骤：（i）将 第一量的药物活性化合物在水混溶的第一有机溶剂中以形成第一溶液; （ii）将第一溶液与第二溶剂混合以沉淀药物活性化合物; 和（iii）接种第一溶液或第二溶剂或预悬浮液。