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1. 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。

2. 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.

3. 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。

4. 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。

5. 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。

6. 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。

7. 发明申请

WO2007059515A2 COMPOSITIONS OF LIPOXYGENASE INHIBITORS 审中-公开
标题翻译： LIPOXYGENASE抑制剂的组合物
公开(公告)号：WO2007059515A2
公开(公告)日：2007-05-24
申请号：PCT/US2006/060939
申请日：2006-11-15
申请人： BAXTER INTERNATIONAL, INC. , BAXTER HEALTHCARE S.A. , KIPP, James, E. , WERLING, Jane , GUPTA, Pramod , BURESH, Rita
发明人： KIPP, James, E. , WERLING, Jane , GUPTA, Pramod , BURESH, Rita
IPC分类号： A61K9/24 , A61K9/19 , A61K31/381 , A61P1/00 , A61P9/10 , A61P11/06
CPC分类号： A61K9/10 , A61K9/0043 , A61K9/0048 , A61K9/19 , A61K9/5146 , A61K31/38 , A61K31/381
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。药物组合物为水性悬浮液的形式，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。

8. 发明申请

WO2007059507A3 COMPOSITIONS COMPRISING LIPOXYGENASE INHIBITORS AND CYCLODEXTRIN 审中-公开
公开(公告)号：WO2007059507A3
公开(公告)日：2007-05-24
申请号：PCT/US2006/060914
申请日：2006-11-15
申请人： BAXTER INTERNATIONAL, INC. , BAXTER HEALTHCARE S.A. , KIPP, James, E. , GUPTA, Pramod
发明人： KIPP, James, E. , GUPTA, Pramod
IPC分类号： A61K47/48 , A61K31/38 , A61P11/06 , A61P29/00 , A61P37/08
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.

9. 发明申请

WO2008080047A2 MAGNETIC SEPARATION OF FINE PARTICLES FROM COMPOSITIONS 审中-公开
标题翻译：从组合物中磁性分离细颗粒
公开(公告)号：WO2008080047A2
公开(公告)日：2008-07-03
申请号：PCT/US2007/088527
申请日：2007-12-21
申请人： BAXTER INTERNATIONAL INC. , BAXTER HEALTHCARE S.A. , KIPP, James, E. , WONG, Joseph, Chung Tak , WERLING, Jane, O.
发明人： KIPP, James, E. , WONG, Joseph, Chung Tak , WERLING, Jane, O.
IPC分类号： B03C1/28
CPC分类号： B03C1/288
摘要： The disclosure describes apparatuses and methods of use thai may be used to remove material with magnetic properties from compositions, particularly pharmaceutical compositions. The apparatuses provide a conduit or column in which a magnetic field exists and through which a composition flows. Magnetic material in the composition is substantially reduced after flowing through the conduit or column.
摘要翻译：本公开描述了可用于从组合物，特别是药物组合物中去除具有磁性的材料的装置和使用方法。该设备提供了其中存在磁场并且组合物流经其中的导管或柱。流经管道或塔后，组合物中的磁性材料大大减少。

10. 发明申请

WO2004082659A1 METHOD FOR PREPARING SMALL PARTICLES 审中-公开
标题翻译：制备小颗粒的方法
公开(公告)号：WO2004082659A1
公开(公告)日：2004-09-30
申请号：PCT/US2004/005696
申请日：2004-02-25
申请人： BAXTER INTERNATIONAL INC. , KIPP, James, E. , WONG, Joseph, Chung, Tak , WERLING, Jane , REBBECK, Christine, L. , BRYNJELSEN, Sean
发明人： KIPP, James, E. , WONG, Joseph, Chung, Tak , WERLING, Jane , REBBECK, Christine, L. , BRYNJELSEN, Sean
IPC分类号： A61K9/10
CPC分类号： A61K31/495 , A61K9/10 , A61K9/14 , A61K9/145 , A61K9/146 , A61K9/1682 , A61K9/1688 , A61K31/12 , A61K31/337 , A61K31/496 , A61K31/55 , A61K31/573
摘要： The present invention is concerned with the formation of small particles or organic compounds by precipitating the organic compounds in an aqueous medium to form a pre-suspension followed by adding energy to stabilize a coating of the particle or to alter the lattice structure of the particle. The process includes the steps of: (i) dissolving the organic compound in the water-miscible first solvent to form a solution; (ii) mixing the solution with the second solvent to define a presuspension of particles; and (iii) adding energy to the presuspension to form a suspension of particles having an average effective particle size of less than about 100 μm. The process is preferably used to prepare a suspension of small particles of a poorly water-soluble, pharmaceutically active compound suitable for in vivo delivery by an administrate route such as parenteral, oral, pulmonary, nasal, buccal, topical ophthalmic, rectal, vaginal, transdermal or the like.
摘要翻译：本发明涉及通过在水性介质中沉淀有机化合物以形成预悬浮液，然后加入能量以稳定颗粒的涂层或改变颗粒的晶格结构来形成小颗粒或有机化合物。该方法包括以下步骤：（i）将有机化合物溶解在水混溶的第一溶剂中以形成溶液; （ii）将溶液与第二溶剂混合以限定颗粒的预悬浮液; 和（iii）向预悬浮液中加入能量以形成平均有效粒径小于约100μm的颗粒的悬浮液。该方法优选用于制备适用于通过给药途径（例如肠胃外，口服，肺，鼻，口腔，局部眼科，直肠，阴道，阴道内）的体内递送的难溶于水的药学活性化合物的小颗粒的悬浮液，透皮等。

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