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公开(公告)号：US09044381B2
公开(公告)日：2015-06-02
申请号：US10868680
申请日：2004-06-15
申请人： Barrett Rabinow , James E. Kipp , Howard Gendelman
发明人： Barrett Rabinow , James E. Kipp , Howard Gendelman
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 phagocytized 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。 药物组合物作为颗粒的分散体例如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。
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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
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。
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公开(公告)号：US20090274765A1
公开(公告)日：2009-11-05
申请号：US12398894
申请日：2009-03-05
CPC分类号： A61K9/5115 , A61K9/146 , A61K9/5161 , A61K9/5169 , A61K31/337 , A61K47/48561 , A61K47/48853 , A61K47/48861 , A61K47/6849 , A61K47/6921 , A61K47/6923 , C07K16/283 , Y10T428/2991
摘要： The present disclosure is directed to surface-modified particles and to methods of making and using the same. The surface-modified particles comprise a particle core and a coating associated with the particle core, wherein the particle core comprises an active agent, the coating comprises an opsonin, and the surface-modified particle has an average size from about 1 nm to about 2,000 nm.
摘要翻译： 本公开涉及表面改性的颗粒及其制备和使用方法。 表面改性的颗粒包括颗粒芯和与颗粒芯相关联的涂层，其中颗粒芯包含活性剂，所述涂层包含调理素，并且表面改性颗粒的平均尺寸为约1nm至约2,000 nm。
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公开(公告)号：US09364443B2
公开(公告)日：2016-06-14
申请号：US12398894
申请日：2009-03-05
IPC分类号： A61K31/337 , A61K9/51 , A61K9/14 , A61K47/48 , C07K16/28
CPC分类号： A61K9/5115 , A61K9/146 , A61K9/5161 , A61K9/5169 , A61K31/337 , A61K47/48561 , A61K47/48853 , A61K47/48861 , A61K47/6849 , A61K47/6921 , A61K47/6923 , C07K16/283 , Y10T428/2991
摘要： The present disclosure is directed to surface-modified particles and to methods of making and using the same. The surface-modified particles comprise a particle core and a coating associated with the particle core, wherein the particle core comprises an active agent, the coating comprises an opsonin, and the surface-modified particle has an average size from about 1 nm to about 2,000 nm.
摘要翻译： 本公开涉及表面改性的颗粒及其制备和使用方法。 表面改性的颗粒包括颗粒芯和与颗粒芯相关联的涂层，其中颗粒芯包含活性剂，所述涂层包含调理素，并且表面改性颗粒的平均尺寸为约1nm至约2,000 nm。
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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。
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6.发明授权Method for treating infectious organisms normally considered to be resistant to an antimicrobial drug 有权通常认为对抗微生物药物具有抗性的感染性生物体的治疗方法公开(公告)号：US08263131B2
公开(公告)日：2012-09-11
申请号：US12414484
申请日：2009-03-30
申请人： Barrett Rabinow , Randy White , Chong-Son Sun , Joseph Chung Take Wong , James E. Kipp , Mark Doty , Christine L. Rebbeck , Pavlos Papadopoulos
发明人： Barrett Rabinow , Randy White , Chong-Son Sun , Joseph Chung Take Wong , James E. Kipp , Mark Doty , Christine L. Rebbeck , Pavlos Papadopoulos
IPC分类号： A61K9/14
CPC分类号： A61K9/10 , A61K9/14 , A61K9/145 , A61K9/146 , A61K9/1688 , A61K9/5015 , A61K9/5031 , A61K9/5036 , A61K9/5042 , A61K9/5123 , A61K9/5138 , A61K9/5146 , A61K9/5192 , A61K31/495 , 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- to micron-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 diffractometry.
摘要翻译： 本发明涉及抗微生物剂亚微米级微粒的组合物。 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级至微米级颗粒的含水悬浮液，其含有涂覆有选自以下的至少一种表面活性剂：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。
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7.发明申请Method for Treating Infectious Organisms Normally Considered to be Resistant to an Antimicrobial Drug 有权治疗通常被认为对抗微生物药物有抵抗力的传染性生物的方法公开(公告)号：US20100086611A1
公开(公告)日：2010-04-08
申请号：US12414484
申请日：2009-03-30
申请人： Barrett Rabinow , Randy White , Chong-Son Sun , Joseph Chung Tak Wong , James E. Kipp , Mark J. Doty , Christine Rebbeck , Pavlos George Papadopoulos
发明人： Barrett Rabinow , Randy White , Chong-Son Sun , Joseph Chung Tak Wong , James E. Kipp , Mark J. Doty , Christine Rebbeck , Pavlos George Papadopoulos
IPC分类号： A61K9/14 , A61K31/4196 , A61K31/496 , A61K31/4164 , A61K31/505 , A61P31/10
CPC分类号： A61K9/10 , A61K9/14 , A61K9/145 , A61K9/146 , A61K9/1688 , A61K9/5015 , A61K9/5031 , A61K9/5036 , A61K9/5042 , A61K9/5123 , A61K9/5138 , A61K9/5146 , A61K9/5192 , A61K31/495 , 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- to micron-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 diffractometry.
摘要翻译： 本发明涉及抗微生物剂亚微米级微粒的组合物。 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级至微米级颗粒的含水悬浮液，其含有涂覆有选自以下的至少一种表面活性剂：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。
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8.发明授权Methods of controlling venous irritation associated with the treatment of a cardiac disorder 有权控制与心脏病症治疗相关的静脉刺激的方法公开(公告)号：US08829047B2
公开(公告)日：2014-09-09
申请号：US13358949
申请日：2012-01-26
申请人： Jerome H. Gass , Jeff McKee , Barrett Rabinow
发明人： Jerome H. Gass , Jeff McKee , Barrett Rabinow
IPC分类号： A61K31/24
CPC分类号： A61K31/24
摘要： A pharmaceutical composition comprising (S)-methyl-3-[4-(2-hydroxy-3-isopropylamino)propoxy]phenylpropionate in a concentration between about 75 mM and about 150 mM, which is substantially free of the R-isomer or pharmaceutically acceptable salt thereof, is provided. A method of treating a cardiac disorder is also provided and includes administering to a subject in need thereof a therapeutically effective amount of a pharmaceutical composition comprising (S)-methyl-3-[4-(2-hydroxy-3-isopropylamino)propoxy]phenylpropionate hydrochloride, wherein the (S)-methyl-3-[4-(2-hydroxy-3-isopropylamino)propoxy]phenylpropionate hydrochloride is present at a concentration between about 75 mM and about 150 mM and wherein the pharmaceutical composition is substantially free of (R)-methyl-3-[4-(2-hydroxy-3-isopropylamino)propoxy]phenylpropionate or pharmaceutically acceptable salt thereof.
摘要翻译： 一种药物组合物，其包含浓度为约75mM至约150mM的（S） - 甲基-3- [4-（2-羟基-3-异丙基氨基）丙氧基]苯基丙酸酯，其基本上不含R-异构体或药学上 提供其可接受的盐。 还提供了治疗心脏疾病的方法，包括向有需要的受试者施用治疗有效量的药物组合物，其包含（S） - 甲基-3- [4-（2-羟基-3-异丙基氨基）丙氧基] 苯基丙酸盐酸盐，其中（S） - 甲基-3- [4-（2-羟基-3-异丙基氨基）丙氧基]苯基丙酸盐酸盐盐酸盐以约75mM至约150mM的浓度存在，其中药物组合物基本上不含 的（R） - 甲基-3- [4-（2-羟基-3-异丙基氨基）丙氧基]苯基丙酸酯或其药学上可接受的盐。
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公开(公告)号：US08067032B2
公开(公告)日：2011-11-29
申请号：US10703395
申请日：2003-11-07
申请人： Mahesh Chaubal , Jane Werling , Barrett Rabinow
发明人： Mahesh Chaubal , Jane Werling , Barrett Rabinow
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. Surfactants with phospholipids conjugated with a water soluble or hydrophilic polymer such as PEG are 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如PEG共轭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。
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10.发明申请公开(公告)号：US20120277309A1
公开(公告)日：2012-11-01
申请号：US13358949
申请日：2012-01-26
申请人： Jerome H. Gass , Jeff McKee , Barrett Rabinow
发明人： Jerome H. Gass , Jeff McKee , Barrett Rabinow
IPC分类号： A61K31/216 , A61P9/06 , A61P9/12 , C07C229/34 , A61P9/00
CPC分类号： A61K31/24
摘要： A pharmaceutical composition comprising (S)-methyl-3-[4-(2-hydroxy-3-isopropylamino)propoxy]phenylpropionate in a concentration between about 75 mM and about 150 mM, which is substantially free of the R-isomer or pharmaceutically acceptable salt thereof, is provided. A method of treating a cardiac disorder is also provided and includes administering to a subject in need thereof a therapeutically effective amount of a pharmaceutical composition comprising (S)-methyl-3-[4-(2-hydroxy-3-isopropylamino)propoxy]phenylpropionate hydrochloride, wherein the (S)-methyl-3-[4-(2-hydroxy-3-isopropylamino)propoxy]phenylpropionate hydrochloride is present at a concentration between about 75 mM and about 150 mM and wherein the pharmaceutical composition is substantially free of (R)-methyl-3-[4-(2-hydroxy-3-isopropylamino)propoxy]phenylpropionate or pharmaceutically acceptable salt thereof.
摘要翻译： 一种药物组合物，其包含浓度为约75mM至约150mM的（S） - 甲基-3- [4-（2-羟基-3-异丙基氨基）丙氧基]苯基丙酸酯，其基本上不含R-异构体或药学上 提供其可接受的盐。 还提供了治疗心脏疾病的方法，包括向有需要的受试者施用治疗有效量的药物组合物，其包含（S） - 甲基-3- [4-（2-羟基-3-异丙基氨基）丙氧基] 苯基丙酸盐酸盐，其中（S） - 甲基-3- [4-（2-羟基-3-异丙基氨基）丙氧基]苯基丙酸盐酸盐盐酸盐以约75mM至约150mM的浓度存在，其中药物组合物基本上不含 的（R） - 甲基-3- [4-（2-羟基-3-异丙基氨基）丙氧基]苯基丙酸酯或其药学上可接受的盐。
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