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1.发明申请Methods for fabrication, uses and compositions of small spherical particles of AAT prepared by controlled phase separation 审中-公开通过控制相分离制备的AAT小球形颗粒的制备，使用和组成的方法公开(公告)号：US20050147687A1
公开(公告)日：2005-07-07
申请号：US10894429
申请日：2004-07-19
CPC分类号： B01J13/06 , A61K9/5026 , A61K9/5031 , A61K38/28
摘要： The present invention is related to a method for preparing small spherical particles of an active agent by providing a solution in a single liquid phase. The single liquid phase comprises an active agent, a phase separation enhancing agent, and a first solvent. A phase change is induced at a controlled rate in the solution to cause a liquid-solid phase separation of the active agent and to form a solid phase and a liquid phase. The solid phase comprises solid small spherical particles of the active agent. The liquid phase comprises the phase separation enhancing agent and the solvent. The small spherical particles are substantially spherical and having a size from about 0.01 μm to about 200 μm.
摘要翻译： 本发明涉及通过在单一液相中提供溶液来制备活性剂的小球形颗粒的方法。 单液相包含活性剂，相分离增强剂和第一溶剂。 在溶液中以受控的速率诱导相变，引起活性剂的液固相分离并形成固相和液相。 固相包含活性剂的固体小球形颗粒。 液相包含相分离增效剂和溶剂。 小球形颗粒基本上是球形的并且具有约0.01μm至约200μm的尺寸。
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公开(公告)号：US20060024379A1
公开(公告)日：2006-02-02
申请号：US11127704
申请日：2005-05-12
申请人： Larry Brown , Vered Bisker-Leib , Debra LaFreniere , John McGeehan , Julia Rashba-Step , Terrence Scott
发明人： Larry Brown , Vered Bisker-Leib , Debra LaFreniere , John McGeehan , Julia Rashba-Step , Terrence Scott
IPC分类号： A61K39/395 , A61K9/50 , A61K9/16
CPC分类号： C07K16/2896 , A61K9/0019 , A61K9/10 , A61K9/1688 , C07K16/2866 , C07K16/36 , C07K2317/24
摘要： The present invention relates to compositions of methods of making and compositions small compositions of particles of an active agent. In accordance with the method of production, the active agent is dissolved in an aqueous or aqueous-miscible solvent containing a dissolved phase-separation enhancing agent (PSEA) to form a solution in a single liquid phase. The solution is subjected to a liquid-solid phase separation to cause the active agent to form small spherical that are substantially amorphous or non-crystalline and are injectable through fine gauge needles at high concentrations. The invention has special application for higher molecular weight proteins.
摘要翻译： 本发明涉及制备方法的组合物和组合物活性剂颗粒的小组合物。 根据生产方法，将活性剂溶解在含有溶解的相分离增强剂（PSEA）的水溶性或水溶性溶剂中以形成单一液相中的溶液。 使溶液进行液固相分离，使活性剂形成基本上无定形或非结晶的小球形，并且可以通过高浓度的细针针进行注射。 本发明对高分子量蛋白质具有特殊应用。
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3.发明申请公开(公告)号：US20060260777A1
公开(公告)日：2006-11-23
申请号：US11380556
申请日：2006-04-27
申请人： Julia Rashba-Step , Terrence Scott , Ramin Darvi , Yuri Lvov , Tatsiana Shutava
发明人： Julia Rashba-Step , Terrence Scott , Ramin Darvi , Yuri Lvov , Tatsiana Shutava
IPC分类号： D21H23/00
CPC分类号： A61K31/7105 , A61K9/0019 , A61K9/0024 , A61K9/1272 , A61K9/16 , A61K9/1635 , A61K9/1658 , A61K9/1688 , A61K9/5026 , A61K9/5036 , A61K9/5047 , A61K9/5052 , A61K9/5057 , A61K9/5073 , A61K9/5089 , C07K17/08
摘要： Surface-modified microparticles and methods of making and using such particles are disclosed. The surface modified microparticles include a preformed or core microparticle that contains at least one active agent. The outer surface of the preformed or core microparticle carries a net surface charge. A monolayer is associated with the outer surface of the preformed or core microparticle. The monolayer includes at least one charged compound that has a charge that is different from the net surface charge of the preformed or core microparticle,
摘要翻译： 公开了表面改性微粒及其制造和使用方法。 表面改性微粒包括含有至少一种活性剂的预制或核心微粒。 预制的或芯的微粒的外表面带有净表面电荷。 单层与预制或核心微粒的外表面相关联。 单层包括至少一种带电荷的化合物，其具有不同于预形成或核微粒的净表面电荷的电荷，
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公开(公告)号：US08333995B2
公开(公告)日：2012-12-18
申请号：US11127704
申请日：2005-05-12
申请人： Larry Brown , Vered Bisker-Leib , Debra LaFreniere , John McGeehan , Julia Rashba-Step , Terrence Scott
发明人： Larry Brown , Vered Bisker-Leib , Debra LaFreniere , John McGeehan , Julia Rashba-Step , Terrence Scott
IPC分类号： A61K39/395
CPC分类号： C07K16/2896 , A61K9/0019 , A61K9/10 , A61K9/1688 , C07K16/2866 , C07K16/36 , C07K2317/24
摘要： The present invention relates to compositions of methods of making and compositions small compositions of particles of an active agent. In accordance with the method of production, the active agent is dissolved in an aqueous or aqueous-miscible solvent containing a dissolved phase-separation enhancing agent (PSEA) to form a solution in a single liquid phase. The solution is subjected to a liquid-solid phase separation to cause the active agent to form small spherical that are substantially amorphous or non-crystalline and are injectable through fine gauge needles at high concentrations. The invention has special application for higher molecular weight proteins.
摘要翻译： 本发明涉及制备方法的组合物和组合物活性剂颗粒的小组合物。 根据生产方法，将活性剂溶解在含有溶解的相分离增强剂（PSEA）的水溶性或水溶性溶剂中以形成单一液相中的溶液。 使溶液进行液固相分离，使活性剂形成基本上无定形或非结晶的小球形，并且可以通过高浓度的细针针进行注射。 本发明对高分子量蛋白质具有特殊应用。
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公开(公告)号：US20080026068A1
公开(公告)日：2008-01-31
申请号：US11736372
申请日：2007-04-17
申请人： Larry Brown , John McGeehan , Qin Yuanxi , Julia Rashba-Step , Terrence Scott
发明人： Larry Brown , John McGeehan , Qin Yuanxi , Julia Rashba-Step , Terrence Scott
CPC分类号： A61K9/0075 , A61K38/28
摘要： Compositions of spherical insulin particles having improved pulmonary application potentials and methods of forming and using these compositions are disclosed in the present application. In one clinical trial with 30 healthy male human subjects, no coughing was observed upon a single pulmonary administration of the spherical insulin particles at an insulin dose of 6.5 mg, nor during the 10-hour post dosing period.
摘要翻译： 在本申请中公开了具有改善的肺部施用电位的球形胰岛素颗粒的组合物以及形成和使用这些组合物的方法。 在30名健康雄性人类受试者的一项临床试验中，在胰岛素剂量为6.5mg的单次肺部施用球素胰岛素颗粒时，也不在给药后10小时期间观察不到咳嗽。
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6.发明申请METHODS FOR FABRICATION, USES, COMPOSITIONS OF INHALABLE SPHERICAL PARTICLES 审中-公开制造方法，使用，可吸入的球形颗粒的组合物公开(公告)号：US20070092452A1
公开(公告)日：2007-04-26
申请号：US11379727
申请日：2006-04-21
CPC分类号： B01J13/06
摘要： Inhalable spherical particles that contain an active agent having unexpectedly good bioavailability when compared to the expected bioavailability are disclosed. Inhalable spherical particles, particles of the agent that contain an amount of a cation such as zinc provide for further improvement in bioavailability.
摘要翻译： 公开了与预期的生物利用度相比，含有具有出乎意料的良好生物利用度的活性剂的可吸入球形颗粒。 可吸入的球形颗粒，含有一定量的阳离子如锌的试剂颗粒提供生物利用度的进一步改善。
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7.发明申请Methods for encapsulating small spherical particles prepared by controlled phase separation 审中-公开包封通过控制相分离制备的小球形颗粒的方法公开(公告)号：US20050170005A1
公开(公告)日：2005-08-04
申请号：US11033780
申请日：2005-01-12
申请人： Julia Rashba-Step , Ramin Darvari , Terrence Scott
发明人： Julia Rashba-Step , Ramin Darvari , Terrence Scott
CPC分类号： A61K9/0019 , A61K9/10 , A61K9/1647 , A61K9/1688 , A61K9/1694
摘要： The present invention relates to methods of making and compositions of microencapsulated small particles of an active agent. In accordance with the method of production, the active agent is dissolved in an aqueous or aqueous-miscible solvent containing a dissolved phase-separation enhancing agent (PSEA) to form a solution in a single liquid phase. The solution is then subjected to a liquid-solid phase separation to cause the active agent to form solid spherical small particles in the solid phase while the PSEA and solvent comprising the liquid phase. The spherical small particles formed are then microencapsulated within a polymeric matrix using an emulsion/evaporation process.
摘要翻译： 本发明涉及制备活性剂微胶囊化小颗粒的方法和组合物。 根据生产方法，将活性剂溶解在含有溶解的相分离增强剂（PSEA）的水溶性或水溶性溶剂中以形成单一液相中的溶液。 然后将溶液进行液固相分离，使活性剂在固相中形成固体球形小颗粒，而PSEA和溶剂包含液相。 然后使用乳液/蒸发方法将形成的球形小颗粒微胶囊化在聚合物基体内。
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8.发明申请Methods for fabrication, uses and compositions of small spherical particles of hGH prepared by controlled phase separation 审中-公开通过控制相分离制备的hGH的小球形颗粒的制备，使用和组成的方法公开(公告)号：US20050142201A1
公开(公告)日：2005-06-30
申请号：US10894408
申请日：2004-07-19
CPC分类号： B01J13/06 , A61K9/5026 , A61K9/5031 , A61K38/28
摘要： The present invention is related to a method for preparing small spherical particles of an active agent by providing a solution in a single liquid phase. The single liquid phase comprises an active agent, a phase separation enhancing agent, and a first solvent. A phase change is induced at a controlled rate in the solution to cause a liquid-solid phase separation of the active agent and to form a solid phase and a liquid phase. The solid phase comprises solid small spherical particles of the active agent. The liquid phase comprises the phase separation enhancing agent and the solvent. The small spherical particles are substantially spherical and having a size from about 0.01 μm to about 200 μm.
摘要翻译： 本发明涉及通过在单一液相中提供溶液来制备活性剂的小球形颗粒的方法。 单液相包含活性剂，相分离增强剂和第一溶剂。 在溶液中以受控的速率诱导相变，引起活性剂的液固相分离并形成固相和液相。 固相包含活性剂的固体小球形颗粒。 液相包含相分离增效剂和溶剂。 小球形颗粒基本上是球形的并且具有约0.01μm至约200μm的尺寸。
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9.发明申请Methods for fabrication, uses and compositions of small spherical particles of insulin prepared by controlled phase separation 审中-公开通过控制相分离制备的胰岛素小球形颗粒的制备方法，用途和组成公开(公告)号：US20050233945A1
公开(公告)日：2005-10-20
申请号：US10894432
申请日：2004-07-19
申请人： Larry Brown , John McGeehan , Yuanxi Qin , Julia Rashba-Step , Terrence Scott
发明人： Larry Brown , John McGeehan , Yuanxi Qin , Julia Rashba-Step , Terrence Scott
CPC分类号： B01J13/06 , A61K9/5026 , A61K9/5031 , A61K38/28
摘要： The present invention is related to a method for preparing small spherical particles of an active agent by providing a solution in a single liquid phase. The single liquid phase comprises an active agent, a phase separation enhancing agent, and a first solvent. A phase change is induced at a controlled rate in the solution to cause a liquid-solid phase separation of the active agent and to form a solid phase and a liquid phase. The solid phase comprises solid small spherical particles of the active agent. The liquid phase comprises the phase separation enhancing agent and the solvent. The small spherical particles are substantially spherical and having a size from about 0.01 μm to about 200 μm.
摘要翻译： 本发明涉及通过在单一液相中提供溶液来制备活性剂的小球形颗粒的方法。 单液相包含活性剂，相分离增强剂和第一溶剂。 在溶液中以受控的速率诱导相变，引起活性剂的液固相分离并形成固相和液相。 固相包含活性剂的固体小球形颗粒。 液相包含相分离增效剂和溶剂。 小球形颗粒基本上是球形的并且具有约0.01μm至约200μm的尺寸。
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10.发明申请Methods for fabrication, uses and compositions of small spherical particles prepared by controlled phase separation 有权通过控制相分离制备的小球形颗粒的制备方法，用途和组成公开(公告)号：US20050142206A1
公开(公告)日：2005-06-30
申请号：US10894430
申请日：2004-07-19
申请人： Larry Brown , John McGeehan , Julia Rashba-Step , Terrence Scott
发明人： Larry Brown , John McGeehan , Julia Rashba-Step , Terrence Scott
CPC分类号： B01J13/06 , A61K9/5026 , A61K9/5031 , A61K38/28
摘要： The present invention is related to a method for preparing small spherical particles of an active agent by providing a solution in a single liquid phase. The single liquid phase comprises an active agent, a phase separation enhancing agent, and a first solvent. A phase change is induced at a controlled rate in the solution to cause a liquid-solid phase separation of the active agent and to form a solid phase and a liquid phase. The solid phase comprises solid small spherical particles of the active agent. The liquid phase comprises the phase separation enhancing agent and the solvent. The small spherical particles are substantially spherical and having a size from about 0.01 μm to about 200 μm.
摘要翻译： 本发明涉及通过在单一液相中提供溶液来制备活性剂的小球形颗粒的方法。 单液相包含活性剂，相分离增强剂和第一溶剂。 在溶液中以受控的速率诱导相变，引起活性剂的液固相分离并形成固相和液相。 固相包含活性剂的固体小球形颗粒。 液相包含相分离增效剂和溶剂。 小球形颗粒基本上是球形的并且具有约0.01μm至约200μm的尺寸。
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