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公开(公告)号：WO2008130803A2
公开(公告)日：2008-10-30
申请号：PCT/US2008059094
申请日：2008-04-02
Applicant: BAXTER INT , BAXTER HEALTHCARE SA , BROWN LARRY R , MCGEEHAN JOHN K , YUANXI QIN , RASHBA-STEP JULIA , SCOTT TERRENCE L
Inventor： BROWN LARRY R , MCGEEHAN JOHN K , YUANXI QIN , RASHBA-STEP JULIA , SCOTT TERRENCE L
CPC classification number: A61K9/0075 , A61K38/28
Abstract: 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.
Abstract translation: 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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公开(公告)号：WO2010022293A3
公开(公告)日：2010-08-19
申请号：PCT/US2009054550
申请日：2009-08-20
Applicant: BAXTER INT , BAXTER HEALTHCARE SA , DARVARI RAMIN , LAMBERT ADAM , RASHBA-STEP JULIA E , YANG MARK X , ZHANG JUNHONG , O'CONNELL ED
Inventor： DARVARI RAMIN , LAMBERT ADAM , RASHBA-STEP JULIA E , YANG MARK X , ZHANG JUNHONG , O'CONNELL ED
CPC classification number: A61K9/1611 , A61K9/1641 , A61K9/1694 , A61K31/70 , A61K31/7088 , C07K16/36
Abstract: A method for processing compositions containing microparticles is provided. The method comprises providing a composition comprising a plurality of solid microparticles and at least one non-volatile material, providing one or more non- solvents comprising an aqueous solution containing at least one free multivalent cation, exposing the composition to the non-solvent to form a mixture containing one or more liquid phases and the solid microparticles, and removing at least a portion of the resulting one or more liquid phases while retaining at least the micropartieles, thereby removing at least a portion of the non- volatile material from the composition.
Abstract translation: 提供了一种处理含有微粒的组合物的方法。 该方法包括提供包含多个固体微粒和至少一种非挥发性物质的组合物，提供包含至少一种游离多价阳离子的水溶液的一种或多种非溶剂，将组合物暴露于非溶剂形成 含有一个或多个液相和固体微粒的混合物，并且至少一部分所得到的一个或多个液相同时至少保留微粒，从而从组合物中除去至少一部分非挥发性材料。
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3.发明申请
公开(公告)号：WO2010006194A2
公开(公告)日：2010-01-14
申请号：PCT/US2009/050145
申请日：2009-07-09
Applicant: BAXTER INTERNATIONAL INC. , BAXTER HEALTHCARE S.A. , DARVARI, Ramin , RASHBA-STEP, Julia, E. , SCOTT, Terrence, L.
Inventor： DARVARI, Ramin , RASHBA-STEP, Julia, E. , SCOTT, Terrence, L.
CPC classification number: A61K9/5052 , A61K9/5073
Abstract: The present disclosure is directed to surface-modified microparticles, pharmaceutical compositions thereof, and methods of making and using such particles. The surface-modified microparticles include a microparticle core, and at least one monolayer associated with the microparticle core. The monolayer comprises an amphiphilic polymer or non-ionic polymer grafted to an ionic polymer.
Abstract translation: 本公开涉及表面改性的微粒，其药物组合物，以及制备和使用这些微粒的方法。 表面改性的微粒包括微粒核和至少一个与微粒核相关的单层。 单层包含接枝到离子聚合物上的两亲聚合物或非离子聚合物。
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4.发明申请MICROSPHERES COMPRISING PROTEIN AND SHOWING INJECTABILITY AT HIGH CONCENTRATIONS OF SAID AGENT 审中-公开包含蛋白质的微胶囊和显示在该药物高浓度下的可注射性
公开(公告)号：WO2005112893A1
公开(公告)日：2005-12-01
申请号：PCT/US2005/016651
申请日：2005-05-12
Applicant: BAXTER INTERNATIONAL INC. , BROWN, Larry , BISKER-LEIB, Vered , LAFRENIERE, Debra , McGEEHAN, John , RASHBA-STEP, Julia , SCOTT, Terrence
Inventor： BROWN, Larry , BISKER-LEIB, Vered , LAFRENIERE, Debra , McGEEHAN, John , RASHBA-STEP, Julia , SCOTT, Terrence
IPC: A61K9/16
CPC classification number: C07K16/2896 , A61K9/0019 , A61K9/10 , A61K9/1688 , C07K16/2866 , C07K16/36 , C07K2317/24
Abstract: The present invention relates to composition of microparticles comprising a suspension of substantially amorphous protein microparticles, the composition providing a concentration of at least about 50 mg of said protein per ml of said composition, and the protein has a molecular weight of at least about 25,000 Daltons. 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.
Abstract translation: 本发明涉及包含基本无定形蛋白质微粒悬浮液的微粒组合物，该组合物提供至少约50mg所述蛋白质/ ml所述组合物的浓度，并且该蛋白质具有至少约25,000道尔顿的分子量 。 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）的水溶性或含水混溶性溶剂中以形成单一液相中的溶液。 将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。 本发明特别适用于较高分子量蛋白质。
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公开(公告)号：WO2003015750A1
公开(公告)日：2003-02-27
申请号：PCT/US2002/026243
申请日：2002-08-16
Applicant: EPIC THERAPEUTICS, INC. , BROWN, Larry, R. , SCOTT, Terrence, L. , RASHBA-STEP, Julia , MCGEEHAN, John, K.
Inventor： BROWN, Larry, R. , SCOTT, Terrence, L. , RASHBA-STEP, Julia , MCGEEHAN, John, K.
IPC: A61K9/00
CPC classification number: A61K9/0075 , A61K9/008 , A61K9/1635 , A61K9/1641 , A61K9/1694 , A61K38/28
Abstract: Pulmonary formulations containing microparticles and a propellant are provided. The microparticles, preferably microspheres, contain protein and exhibit a fine particle fraction in the range of 25 to 100%.
Abstract translation: 提供含有微粒和推进剂的肺制剂。 微粒，优选微球，含有蛋白质，并表现出25〜100％范围内的微细粒子分数。
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Patent Agency Ranking
公开(公告)号：WO2010022293A2
公开(公告)日：2010-02-25
申请号：PCT/US2009/054550
申请日：2009-08-20
Applicant: BAXTER INTERNATIONAL INC. , BAXTER HEALTHCARE S.A. , DARVARI, Ramin , LAMBERT, Adam , RASHBA-STEP, Julia, E. , YANG, Mark, X. , ZHANG, Junhong , O'CONNELL, Ed
Inventor： DARVARI, Ramin , LAMBERT, Adam , RASHBA-STEP, Julia, E. , YANG, Mark, X. , ZHANG, Junhong , O'CONNELL, Ed
CPC classification number: A61K9/1611 , A61K9/1641 , A61K9/1694 , A61K31/70 , A61K31/7088 , C07K16/36
Abstract: A method for processing compositions containing microparticles is provided. The method comprises providing a composition comprising a plurality of solid microparticles and at least one non-volatile material, providing one or more non- solvents comprising an aqueous solution containing at least one free multivalent cation, exposing the composition to the non-solvent to form a mixture containing one or more liquid phases and the solid microparticles, and removing at least a portion of the resulting one or more liquid phases while retaining at least the micropartieles, thereby removing at least a portion of the non- volatile material from the composition.
Abstract translation: 提供了用于处理含有微粒的组合物的方法。 该方法包括提供包含多个固体微粒和至少一种非挥发性材料的组合物，提供包含含有至少一种游离多价阳离子的水溶液的一种或多种非溶剂，将组合物暴露于非溶剂以形成 含有一个或多个液相和固体微粒的混合物，并除去至少一部分所得到的一个或多个液相，同时至少保留微粒，从而从组合物中除去至少一部分非挥发性物质。
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公开(公告)号：WO2008130803A3
公开(公告)日：2008-10-30
申请号：PCT/US2008/059094
申请日：2008-04-02
Applicant: BAXTER INTERNATIONAL INC. , BAXTER HEALTHCARE S.A. , BROWN, Larry R. , MCGEEHAN, John K. , YUANXI, Qin , RASHBA-STEP, Julia , SCOTT, Terrence L.
Inventor： BROWN, Larry R. , MCGEEHAN, John K. , YUANXI, Qin , RASHBA-STEP, Julia , SCOTT, Terrence L.
Abstract: 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.
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8.发明申请
公开(公告)号：WO2006116546A1
公开(公告)日：2006-11-02
申请号：PCT/US2006/015918
申请日：2006-04-27
Applicant: BAXTER INTERNATIONAL INC. , BAXTER HEALTHCARE S. A. , LOUISIANA TECH UNIVERSITY , RASHBA-STEP, Julia , SCOTT, Terrence, L. , DARVI, Ramin , LVOV, Yuri , SHUTAVA, Tatsiana
Inventor： RASHBA-STEP, Julia , SCOTT, Terrence, L. , DARVI, Ramin , LVOV, Yuri , SHUTAVA, Tatsiana
IPC: A61K9/00 , A61K9/50 , A61K38/28 , A61K38/27 , A61K39/395 , A61K31/7105
CPC classification number: 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
Abstract: 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.
Abstract translation: 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心微粒的净表面电荷的电荷。
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9.发明申请
公开(公告)号：WO2010006194A3
公开(公告)日：2010-08-05
申请号：PCT/US2009050145
申请日：2009-07-09
Applicant: BAXTER INT , BAXTER HEALTHCARE SA , DARVARI RAMIN , RASHBA-STEP JULIA E , SCOTT TERRENCE L
Inventor： DARVARI RAMIN , RASHBA-STEP JULIA E , SCOTT TERRENCE L
CPC classification number: A61K9/5052 , A61K9/5073
Abstract: The present disclosure is directed to surface-modified microparticles, pharmaceutical compositions thereof, and methods of making and using such particles. The surface-modified microparticles include a microparticle core, and at least one monolayer associated with the microparticle core. The monolayer comprises an amphiphilic polymer or non-ionic polymer grafted to an ionic polymer.
Abstract translation: 本公开涉及表面改性的微粒，其药物组合物，以及制备和使用这些颗粒的方法。 表面改性微粒包括微粒核和与微粒核相关的至少一个单层。 单层包括接枝到离子聚合物上的两亲聚合物或非离子聚合物。
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10.发明申请MICROENCAPSULES CONTAINING SURFACE-MODIFIED MICROPARTICLES AND METHODS OF FORMING AND USING THE SAME 审中-公开含有表面改性微球的微囊藻类及其形成和使用方法
公开(公告)号：WO2008060786A3
公开(公告)日：2009-05-07
申请号：PCT/US2007080863
申请日：2007-10-09
Applicant: BAXTER INT , BAXTER HEALTHCARE SA , RASHBA-STEP JULIA E , SCOTT TERRENCE L , DARVARI RAMIN
Inventor： RASHBA-STEP JULIA E , SCOTT TERRENCE L , DARVARI RAMIN
CPC classification number: A61K9/1647 , A61K9/0019 , A61K9/5031 , A61K9/5084
Abstract: An encapsulated particle, comprising a plurality of preformed microparticles encapsulated in an amorphous matrix, wherein at least one of the preformed microparticles comprises a core microparticle and a monolayer associated with the outer surface of the core microparticle. The core microparticle comprises at least one active agent that is capable of being released from the encapsulated particle.
Abstract translation: 一种包封颗粒，其包含封装在无定形基体中的多个预成型微粒，其中至少一个所述预成型微粒包含核微粒和与所述芯微粒的外表面相关联的单层。 核心微粒包括至少一种能够从包封的颗粒释放的活性剂。
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