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1. 发明申请

WO2007032993A2 SURFACTANT SYSTEMS FOR DELIVERY OF ORGANIC COMPOUNDS 审中-公开
标题翻译：用于交付有机化合物的表面活性剂体系
公开(公告)号：WO2007032993A2
公开(公告)日：2007-03-22
申请号：PCT/US2006/034891
申请日：2006-09-07
申请人： BAXTER INTERNATIONAL INC. , BAXTER HEALTHCARE S.A. , CHAUBAL, Mahesh , DOTY, Mark, J. , KONKEL, Jamie, T. , RABINOW, Barrett, E.
发明人： CHAUBAL, Mahesh , DOTY, Mark, J. , KONKEL, Jamie, T. , RABINOW, Barrett, E.
IPC分类号： A61K9/10 , A61K9/14 , A61K47/34 , A61K9/127 , A61K9/16
CPC分类号： B01J13/04 , A61K9/10 , A61K9/1271 , A61K9/145 , A61K9/146 , A61K31/436
摘要： Submicron particles of an organic compound, such as therapeutic and diagnostic agent are disclosed. The organic compound particles are associated with a least two surfactants including a block copolymer and phospholipids conjugated with a hydrophilic polymer.
摘要翻译：公开了有机化合物的亚微米颗粒，例如治疗和诊断剂。有机化合物颗粒与至少两种表面活性剂缔合，包括嵌段共聚物和与亲水性聚合物共轭的磷脂。

2. 发明申请

WO2005072706A2 NANOSUSPENSIONS OF ANTI-RETROVIRAL AGENTS FOR INCREASED CENTRAL NERVOUS SYSTEM DELIVERY 审中-公开
标题翻译：用于增加中央神经系统递送的抗逆转录病毒剂的纳米抗体
公开(公告)号：WO2005072706A2
公开(公告)日：2005-08-11
申请号：PCT/US2005/001861
申请日：2005-01-21
申请人： BAXTER INTERNATIONAL INC. , BAXTER HEALTHCARE S.A. , WERLING, Jane , CHAUBAL, Mahesh, V. , KIPP, James, E. , RABINOW, Barrett, E.
发明人： WERLING, Jane , CHAUBAL, Mahesh, V. , KIPP, James, E. , RABINOW, Barrett, E.
IPC分类号： A61K9/10
CPC分类号： A61K9/10 , A61K9/5123 , A61K31/00 , A61K31/551 , A61K31/7072 , A61K31/7076
摘要： The present invention provides compositions comprising dispersions of anti-retroviral agents and methods of manufacture. The nanosuspensions are made by the process of microprecipitation and energy addition. Preferably, the nanosuspensions are made by the tandem process of microprecipitation-homogenization.
摘要翻译：本发明提供了包含抗逆转录病毒剂分散体和制造方法的组合物。纳米悬浮液是通过微量沉淀和能量添加的过程制成的。优选地，通过微沉淀均质化的串联方法制备纳米悬浮液。

3. 发明申请

WO2005046671A1 METHOD FOR PREPARING SUBMICRON PARTICLES OF PACLITAXEL 审中-公开
标题翻译：制备PACLITAXEL的亚微米颗粒的方法
公开(公告)号：WO2005046671A1
公开(公告)日：2005-05-26
申请号：PCT/US2004/036604
申请日：2004-11-03
申请人： BAXTER INTERNATIONAL INC. , CHAUBAL, Mahesh , WERLING, Jane , RABINOW, Barrett, E.
发明人： CHAUBAL, Mahesh , WERLING, Jane , RABINOW, Barrett, E.
IPC分类号： A61K31/337
CPC分类号： A61K9/1271 , A61K9/10 , A61K9/14 , A61K9/145 , A61K9/146 , A61K9/1688 , A61K31/12 , A61K31/337 , A61K31/495 , A61K31/496 , A61K31/55 , A61K31/573
摘要： The present invention is concerned with the formation of submicron particles of an antineoplastic agent, particularly paclitaxel, by precipitating the antineoplastic agent in an aqueous medium to form a pre-suspension followed by homogenization. Surfacants with phospholipids conjugated with a water soluble or hydrophilic polymer such as PEGare used as coating for the particles. The particles produced generally have an average particle size of less than about 1000 nm and are not rapidly soluble.
摘要翻译：本发明涉及通过在水性介质中沉淀抗肿瘤剂以形成预悬浮液，随后进行均质化而形成抗肿瘤药物，特别是紫杉醇的亚微米颗粒。具有与水溶性或亲水性聚合物（例如PEG）缀合的磷脂的表面活性剂用作颗粒的涂层。生产的颗粒通常具有小于约1000nm的平均粒度，并且不易迅速溶解。

4. 发明申请

WO2004096180A1 FORMULATION TO RENDER AN ANTIMICROBIAL DRUG POTENT AGAINST ORGANISMS NORMALLY CONSIDERED TO BE RESISTANT TO THE DRUG 审中-公开
标题翻译：制定一种抗反刍药物的抗生素药物标准
公开(公告)号：WO2004096180A1
公开(公告)日：2004-11-11
申请号：PCT/US2004/013268
申请日：2004-04-29
申请人： BAXTER INTERNATIONAL INC. , RABINOW, Barrett, E. , WHITE, Randy , SUN, Chong-Son , WONG, Joseph, Chung, Tak , KIPP, James, E. , DOTY, Mark, J. , REBBECK, Christine, L. , PAPADOPOULOS, Pavlos
发明人： RABINOW, Barrett, E. , WHITE, Randy , SUN, Chong-Son , WONG, Joseph, Chung, Tak , KIPP, James, E. , DOTY, Mark, J. , REBBECK, Christine, L. , PAPADOPOULOS, Pavlos
IPC分类号： A61K9/14
CPC分类号： A61K9/5123 , A61K9/5015 , A61K9/5138 , A61K9/5146 , A61K9/5192 , A61K31/496
摘要： The present invention relates to compositions of submicron- to micron-size particles of antimicrobial agents. More particularly the invention relates to a composition of an antimicrobial agent that renders the agent potent against organisms normally considered to be resistant to the agent. The composition comprises an aqueous suspension of submicron-tomicron-size particles containing the agent coated with at least one surfactant selected from the group consisting of: ionic surfactants, non-ionic surfactants, biologically derived surfactants, and amino acids and their derivatives. The particles have a volume-weighted mean particle size of less than 5 µm as measured by laser diffractonetry.
摘要翻译：本发明涉及抗微生物剂亚微米级微粒子的组合物。更具体地，本发明涉及一种抗微生物剂的组合物，其使得该试剂对通常被认为对该试剂具有抗性的生物有效。该组合物包含亚微米 - 微粒尺寸颗粒的水悬浮液，其含有涂覆有至少一种表面活性剂的试剂，所述表面活性剂选自：离子表面活性剂，非离子表面活性剂，生物衍生的表面活性剂，以及氨基酸及其衍生物。通过激光衍射测量，颗粒具有小于5μm的体积加权平均粒度。

5. 发明申请

WO2007124224A2 METHOD FOR DELIVERING PARTICULATE DRUGS TO TISSUES 审中-公开
标题翻译：将颗粒药物递送给组织的方法
公开(公告)号：WO2007124224A2
公开(公告)日：2007-11-01
申请号：PCT/US2007/064679
申请日：2007-03-22
申请人： BAXTER INTERNATIONAL INC. , BAXTER HEALTHCARE S.A. , RABINOW, Barrett, E. , GENDELMAN, Howard, E. , KIPP, James, E.
发明人： RABINOW, Barrett, E. , GENDELMAN, Howard, E. , KIPP, James, E.
IPC分类号： A61K9/00 , A61K9/51 , A61K47/48
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。

6. 发明申请

WO2009140162A1 STABLE PHARMACEUTICAL FORMULATIONS 审中-公开
标题翻译：稳定的药物制剂
公开(公告)号：WO2009140162A1
公开(公告)日：2009-11-19
申请号：PCT/US2009/043295
申请日：2009-05-08
申请人： BAXTER INTERNATIONAL INC. , BAXTER HEALTHCARE S.A. , KIPP, James, E. , WONG, Joseph, C., T. , NAIR, Lakshmy , MILLER, Reagan , RABINOW, Barrett, E.
发明人： KIPP, James, E. , WONG, Joseph, C., T. , NAIR, Lakshmy , MILLER, Reagan , RABINOW, Barrett, E.
IPC分类号： A61K9/00 , A61K47/10 , A61K47/40
CPC分类号： A61K9/0019 , A61K47/36 , A61K47/40
摘要： Stable pharmaceutical formulations and methods of making same are provided. In a general embodiment, the present disclosure provides a method of making a stable pharmaceutical formulation comprising adding one or more vitrifying additives to an aqueous pharmaceutical solution to raise the glass transition temperature of the aqueous pharmaceutical solution. The aqueous pharmaceutical solution can be cooled to a temperature of about -50 C to about -10 C. The vitrifying additive enhances the formation of a glass or amorphous solid of the aqueous pharmaceutical solution at cryogenic temperatures (-50 to -10C), and the pharmaceutical formulation can be thawed to liquid form and administered to a mammalian subject.
摘要翻译：提供稳定的药物制剂及其制备方法。在一般实施方案中，本公开提供了制备稳定药物制剂的方法，其包括向药物水溶液中加入一种或多种玻璃化添加剂以提高药物水溶液的玻璃化转变温度。水性药物溶液可以冷却至约-50℃至约-10℃的温度。玻璃化添加剂在低温（-50至-10℃）下增强了药物水溶液的玻璃或无定形固体的形成，药物制剂可以解冻为液体形式并给予哺乳动物受试者。

7. 发明申请

WO2004112747A2 METHOD FOR DELIVERING DRUGS TO THE BRAIN 审中-公开
标题翻译：将药物递送至脑的方法
公开(公告)号：WO2004112747A2
公开(公告)日：2004-12-29
申请号：PCT/US2004/018850
申请日：2004-06-15
申请人： BAXTER INTERNATIONAL INC. , RABINOW, Barrett, E. , GENDELMAN, Howard, E. , KIPP, James, E.
发明人： RABINOW, Barrett, E. , GENDELMAN, Howard, E. , KIPP, James, E.
IPC分类号： A61K9/00
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。

8. 发明申请

WO2005123907A2 EX-VIVO APPLICATION OF SOLID MICROPARTICULATE THERAPEUTIC AGENTS 审中-公开
标题翻译：固体微粒治疗药物的实例应用
公开(公告)号：WO2005123907A2
公开(公告)日：2005-12-29
申请号：PCT/US2005/022992
申请日：2005-06-08
申请人： BAXTER INTERNATIONAL INC. , KIPP, James E. , RABINOW, Barrett, E.
发明人： KIPP, James E. , RABINOW, Barrett, E.
IPC分类号： 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 threof. 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以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），平均粒度小于约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。药物活性物质可以静脉内，肌肉内，皮下，皮内，关节内，鞘内，硬膜外，脑内，经口腔途径，直肠，局部，经皮，口服，鼻内，经由肺途径，腹膜内或组合Threof施用。给药后，加载的细胞将药物组合物作为颗粒转运。

9. 发明申请

WO2004112747A3 SPECIFIC DELIVERY OF DRUGS TO THE BRAIN 审中-公开
公开(公告)号：WO2004112747A3
公开(公告)日：2004-12-29
申请号：PCT/US2004/018850
申请日：2004-06-15
申请人： BAXTER INTERNATIONAL INC. , RABINOW, Barrett, E. , GENDELMAN, Howard, E. , KIPP, James, E.
发明人： RABINOW, Barrett, E. , GENDELMAN, Howard, E. , KIPP, James, E.
IPC分类号： A61K9/14
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.

10. 发明申请

WO2005030273A2 HIGH-PRESSURE STERILIZATION TO TERMINALLY STERILIZE PHARMACEUTICAL PREPARATIONS AND MEDICAL PRODUCTS 审中-公开
标题翻译：高压灭菌终止灭菌药物制剂和医药产品
公开(公告)号：WO2005030273A2
公开(公告)日：2005-04-07
申请号：PCT/US2004/031107
申请日：2004-09-22
申请人： BAXTER INTERNATIONAL INC. , RODRIGUEZ, Alfredo , RABINOW, Barrett, E. , DOTY, Mark , KONKEL, Jamie
发明人： RODRIGUEZ, Alfredo , RABINOW, Barrett, E. , DOTY, Mark , KONKEL, Jamie
IPC分类号： A61L2/00
CPC分类号： B65B55/02 , A61L2/0011 , A61L2/0023 , A61L2/02 , A61L2/04
摘要： The present invention provides a process for sterilizing a system, preferably a pharmaceutical preparation such as a dispersion of small particles or droplets of a pharmaceutically active compound using high pressure terminal sterilization techniques and products therefrom.
摘要翻译：本发明提供一种使用高压终端灭菌技术及其产品对系统，优选药物制剂如药物活性化合物的小颗粒或液滴的分散体进行灭菌的方法。

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