(Polyalkoxy)sulfonate surface modifiers
    1.
    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

    IPC分类号: A61K9/14

    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
    2.
    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

    IPC分类号: A61K31/205 A61B5/055

    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。

    Method for delivering drugs to the brain
    4.
    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

    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
    5.
    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

    IPC分类号: G11B27/00

    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。

    Submicron suspensions with polymorph control
    6.
    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

    IPC分类号: A61K9/00

    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。

    COMPOSITIONS OF LIPOXYGENASE INHIBITORS
    9.
    发明申请
    COMPOSITIONS OF LIPOXYGENASE INHIBITORS 审中-公开
    LIPOXYGENASE抑制剂的组合物

    公开(公告)号:US20070134341A1

    公开(公告)日:2007-06-14

    申请号:US11560324

    申请日:2006-11-15

    IPC分类号: A61K31/381 A61K9/14

    摘要: Pharmaceutical compositions comprising particles of lipoxygenase inhibitor compounds having an effective average size of from about 10 nm to about 50 microns are provided. More particularly, pharmaceutical compositions of particle of a 5-lipoxygenase inhibitor compound having an effective average size of from about 50 nm to about 5 microns are provided. The pharmaceutical compositions are in the form of aqueous suspensions with the particle of the 5-lipoxygenase inhibitor compound present in concentrations of from about 5 to about 200 mg/ml. In addition, methods for making such pharmaceutical compositions are provided. In particular, microprecipitation and direct homogenization in the presence of at least one surfactant are disclosed for making the pharmaceutical compositions.

    摘要翻译: 提供了包含具有约10nm至约50微米的有效平均尺寸的脂氧合酶抑制剂化合物颗粒的药物组合物。 更具体地,提供了具有约50nm至约5微米的有效平均尺寸的5-脂氧合酶抑制剂化合物的颗粒的药物组合物。 药物组合物呈水性悬浮液的形式,其中5-脂氧合酶抑制剂化合物的颗粒以约5至约200mg / ml的浓度存在。 此外,提供了制备这种药物组合物的方法。 特别地,公开了在至少一种表面活性剂存在下的微沉淀和直接均化,用于制备药物组合物。

    COMPOSITIONS COMPRISING LIPOXYGENASE INHIBITORS AND CYCLODEXTRIN
    10.
    发明申请
    COMPOSITIONS COMPRISING LIPOXYGENASE INHIBITORS AND CYCLODEXTRIN 审中-公开
    包含LIPOXYGENASE抑制剂和环糊精的组合物

    公开(公告)号:US20070111965A1

    公开(公告)日:2007-05-17

    申请号:US11560242

    申请日:2006-11-15

    摘要: The present invention is directed to formulations of inclusion complexes of lipoxygenase inhibitors and cyclodextrins having a therapeutically effective concentration of the lipoxygenase inhibitor, methods of making the same and methods of treating disease states using the same. Forming cyclodextrin complexes permits the enhancement of the aqueous solubility of lipoxygenase inhibitors which allows higher concentrations of the lipoxygenase in solution. Aqueous formulations of lipoxygenase inhibitors-cyclodextrin complexes are suitable for parenteral or oral administration for treating and/or preventing inflammatory disease states. The aqueous formulations can be lyophilized to prolong storage stability, assist in oral administration and/or provide for convenient and economical packaging.

    摘要翻译: 本发明涉及脂氧合酶抑制剂和具有治疗有效浓度的脂氧合酶抑制剂的环糊精的包合物的制剂,其制备方法以及使用其的治疗疾病状态的方法。 形成环糊精复合物允许提高脂氧合酶抑制剂的水溶性,其允许溶液中更高浓度的脂氧合酶。 脂氧合酶抑制剂 - 环糊精复合物的水性制剂适用于肠胃外或口服给药以治疗和/或预防炎性疾病状态。 水性制剂可以冻干以延长储存稳定性,有助于口服给药和/或提供方便和经济的包装。