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1. 发明授权

US07052678B2 Particles for inhalation having sustained release properties 有权
公开(公告)号：US07052678B2
公开(公告)日：2006-05-30
申请号：US10094955
申请日：2002-03-07
申请人： Rita Vanbever , Robert S. Langer , David A. Edwards , Jeffrey Mintzes , Jue Wang , Donghao Chen
发明人： Rita Vanbever , Robert S. Langer , David A. Edwards , Jeffrey Mintzes , Jue Wang , Donghao Chen
IPC分类号： A61K9/12 , A61K9/14
CPC分类号： A61K9/0075 , A61K9/1617 , A61K9/1623 , A61K9/1641 , A61K9/1647 , A61K9/1658 , A61K31/135 , A61K31/137 , A61K38/28 , A61K38/38 , A61K47/6921
摘要： The invention generally relates to a method for pulmonary delivery of therapeutic, prophylactic and diagnostic agents to a patient wherein the agent is released in a sustained fashion, and to particles suitable for use in the method. In particular, the invention relates to a method for the pulmonary delivery of a therapeutic, prophylactic or diagnostic agent comprising administering to the respiratory tract of a patient in need of treatment, prophylaxis or diagnosis an effective amount of particles comprising a polycationic complexing agent which is complexed with a therapeutic, prophylactic or diagnostic agent or any combination thereof having a charge capable of complexing with the polycationic complexing agent upon association with the bioactive agent. The particles can further comprise a pharmaceutically acceptable carrier. The amount of polycationic complexing agent present in the particles is an amount sufficient to sustain the release of diagnostic, therapeutic or prophylactic agent from the particles. For example, the amount of complexing agent present can be at about 5% weight/weight (w/w) or more of the total weight of the complexing agent and therapeutic, diagnostic or prophylactic agent. Release of the agent from the administered particles occurs in a sustained fashion.

2. 发明授权

US06652837B1 Preparation of novel particles for inhalation 有权
标题翻译：用于吸入的新型颗粒的制备
公开(公告)号：US06652837B1
公开(公告)日：2003-11-25
申请号：US09394233
申请日：1999-09-13
申请人： David A. Edwards , Robert S. Langer , Rita Vanbever , Jeffrey Mintzes , Jue Wang , Donghao Chen
发明人： David A. Edwards , Robert S. Langer , Rita Vanbever , Jeffrey Mintzes , Jue Wang , Donghao Chen
IPC分类号： A61K912
CPC分类号： A61K9/0075 , A61K9/1617 , A61K9/1623 , A61K9/1641 , A61K9/1647 , A61K9/1658 , A61K31/135 , A61K31/137 , A61K38/28 , A61K38/38 , A61K47/6927 , Y10S514/958
摘要： Particles incorporating a surfactant and/or a hydrophilic or hydrophobic complex of a positively or negatively charged therapeutic agent and a charged molecule of opposite charge for drug delivery to the pulmonary system, and methods for their synthesis and administration are provided. In a preferred embodiment, the particles are made of a biodegradable material and have a tap density less than 0.4 g/cm3 and a mass mean diameter between 5 &mgr;m and 30 &mgr;m, which together yield an aerodynamic diameter of the particles of between approximately one and three microns. The particles may be formed of biodegradable materials such as biodegradable polymers. For example, the particles may be formed of poly(lactic acid) or poly(glycolic acid) or copolymers thereof. Alternatively, the particles may be formed solely of a therapeutic or diagnostic agent and a surfactant. Surfactants can be incorporated on the particle surface for example by coating the particle after particle formation, or by incorporating the surfactant in the material forming the particle prior to formation of the particle. Exemplary surfactants include phosphoglycerides such as dipalmitoyl phosphatidylcholine (DPPC). The particles can be effectively aerosolized for administration to the respiratory tract to permit systemic or local delivery of wide a variety of therapeutic agents. Formation of complexes of positively or negatively charged therapeutic agents with molecules of opposite charge can allow control of the release rate of the agents into the blood stream following administration.
摘要翻译：提供了将具有正或负电荷的治疗剂的表面活性剂和/或亲水或疏水配合物和用于药物递送至肺系统的带电分子的相反电荷的颗粒，以及用于其合成和给药的方法。在一个优选的实施方案中，颗粒由可生物降解的材料制成，并且具有小于0.4g / cm 3的振实密度和5μm和30μm之间的质量平均直径，这两个颗粒之间的颗粒的空气动力学直径在大约一到三微米。颗粒可以由可生物降解的材料如可生物降解的聚合物形成。例如，颗粒可以由聚（乳酸）或聚（乙醇酸）或其共聚物形成。或者，颗粒可以仅由治疗剂或诊断剂和表面活性剂形成。表面活性剂可以结合在颗粒表面上，例如通过在颗粒形成之后涂覆颗粒，或者通过在形成颗粒之前将表面活性剂并入形成颗粒的材料中。示例性表面活性剂包括磷酸甘油酯，例如二棕榈酰磷脂酰胆碱（DPPC）。这些颗粒可以有效地雾化，用于给呼吸道施用以允许全身或局部递送各种各样的治疗剂。正电荷或带负电荷的治疗剂与相反电荷分子的复合物的形成可以允许在给药后将药剂释放到血流中的释放速率。

3. 发明申请

US20120107241A1 Particles for Inhalation Having Sustained Release Properties 审中-公开
标题翻译：具有持续释放性质的吸入颗粒
公开(公告)号：US20120107241A1
公开(公告)日：2012-05-03
申请号：US13220334
申请日：2011-08-29
申请人： David A. Edwards , Robert S. Langer , Rita Vanbever , Jeffrey Mintzes , Jue Wang , Donghao Chen
发明人： David A. Edwards , Robert S. Langer , Rita Vanbever , Jeffrey Mintzes , Jue Wang , Donghao Chen
IPC分类号： A61K49/00 , A61K9/00
CPC分类号： A61K9/0073 , A61K9/0075 , A61K9/16 , A61K9/1617 , A61K9/1623 , A61K9/1641 , A61K9/1647 , A61K9/1658 , A61K9/1694 , A61K31/135 , A61K31/137 , A61K31/566 , A61K38/28 , A61K38/38 , A61K47/12 , A61K47/183 , A61K47/24 , A61K47/6927
摘要： The invention generally relates to a method for pulmonary delivery of therapeutic, prophylactic and diagnostic agents to a patient wherein the agent is released in a sustained fashion, and to particles suitable for use in the method. In particular, the invention relates to a method for the pulmonary delivery of a therapeutic, prophylactic or diagnostic agent comprising administering to the respiratory tract of a patient in need of treatment, prophylaxis or diagnosis an effective amount of particles comprising a therapeutic, prophylactic or diagnostic agent or any combination thereof in association with a charged lipid, wherein the charged lipid has an overall net charge which is opposite to that of the agent upon association with the agent. Release of the agent from the administered particles occurs in a sustained fashion.
摘要翻译：本发明一般涉及将治疗性预防和诊断试剂肺部递送给患者，其中药剂以持续方式释放，以及适用于该方法的颗粒。特别地，本发明涉及用于肺部递送治疗性，预防性或诊断性药物的方法，其包括对需要治疗，预防或诊断的患者的呼吸道施用有效量的包含治疗性，预防性或诊断性的颗粒药剂或其任何组合与带电脂质相结合，其中带电脂质具有与药剂相关的与药剂相反的总净电荷。药剂从给药颗粒中的释放以持续的方式发生。

4. 发明授权

US07628977B2 Particles for inhalation having sustained release properties 失效
公开(公告)号：US07628977B2
公开(公告)日：2009-12-08
申请号：US10420071
申请日：2003-04-18
申请人： David A. Edwards , Robert S. Langer , Rita Vanbever , Jeffrey Mintzes , Jue Wang , Donghao Chen
发明人： David A. Edwards , Robert S. Langer , Rita Vanbever , Jeffrey Mintzes , Jue Wang , Donghao Chen
IPC分类号： A61K9/14 , A61K31/66 , A61K31/661 , A61K31/6615
CPC分类号： A61K9/0073 , A61K9/0075 , A61K9/16 , A61K9/1617 , A61K9/1623 , A61K9/1641 , A61K9/1647 , A61K9/1658 , A61K9/1694 , A61K31/135 , A61K31/137 , A61K31/566 , A61K38/28 , A61K38/38 , A61K47/12 , A61K47/183 , A61K47/24 , A61K47/6927
摘要： The invention generally relates to a method for pulmonary delivery of therapeutic, prophylactic and diagnostic agents to a patient wherein the agent is released in a sustained fashion, and to particles suitable for use in the method. In particular, the invention relates to a method for the pulmonary delivery of a therapeutic, prophylactic or diagnostic agent comprising administering to the respiratory tract of a patient in need of treatment, prophylaxis or diagnosis an effective amount of particles comprising a therapeutic, prophylactic or diagnostic agent or any combination thereof in association with a charged lipid, wherein the charged lipid has an overall net charge which is opposite to that of the agent upon association with the agent. Release of the agent from the administered particles occurs in a sustained fashion.

5. 发明授权

US5985309A Preparation of particles for inhalation 失效
标题翻译：吸入颗粒的制备
公开(公告)号：US5985309A
公开(公告)日：1999-11-16
申请号：US971791
申请日：1997-11-17
申请人： David A. Edwards , Robert S. Langer , Rita Vanbever , Jeffrey Mintzes , Jue Wang , Donghao Chen
发明人： David A. Edwards , Robert S. Langer , Rita Vanbever , Jeffrey Mintzes , Jue Wang , Donghao Chen
IPC分类号： A61K9/16 , A61K31/135 , A61K31/137 , A61K38/28 , A61K38/38 , A61K13/00
CPC分类号： A61K9/1647 , A61K31/135 , A61K31/137 , A61K38/28 , A61K38/38
摘要： Particles incorporating a surfactant and/or a hydrophilic or hydrophobic complex of a positively or negatively charged therapeutic agent and a charged molecule of opposite charge for drug delivery to the pulmonary system, and methods for their synthesis and administration are provided. In a preferred embodiment, the particles are made of a biodegradable material and have a tap density less than 0.4 g/cm.sup.3 and a mass mean diameter between 5 .mu.m and 30 .mu.m, which together yield an aerodynamic diameter of the particles of between approximately one and three microns. The particles may be formed of biodegradable materials such as biodegradable polymers. For example, the particles may be formed of poly(lactic acid) or poly(glycolic acid) or copolymers thereof. Alternatively, the particles may be formed solely of a therapeutic or diagnostic agent and a surfactant. Surfactants can be incorporated on the particle surface for example by coating the particle after particle formation, or by incorporating the surfactant in the material forming the particle prior to formation of the particle. Exemplary surfactants include phosphoglycerides such as dipalmitoyl phosphatidylcholine (DPPC). The particles can be effectively aerosolized for administration to the respiratory tract to permit systemic or local delivery of wide a variety of therapeutic agents. Formation of complexes of positively or negatively charged therapeutic agents with molecules of opposite charge can allow control of the release rate of the agents into the blood stream following administration.
摘要翻译：提供了将具有正或负电荷的治疗剂的表面活性剂和/或亲水或疏水配合物和用于药物递送至肺系统的带电分子的相反电荷的颗粒，以及用于其合成和给药的方法。在优选的实施方案中，颗粒由可生物降解的材料制成，并且具有小于0.4g / cm 3的振实密度和5μm至30μm之间的质量平均直径，其一起产生颗粒的空气动力学直径在约一和三微米。颗粒可以由可生物降解的材料如可生物降解的聚合物形成。例如，颗粒可以由聚（乳酸）或聚（乙醇酸）或其共聚物形成。或者，颗粒可以仅由治疗剂或诊断剂和表面活性剂形成。表面活性剂可以结合在颗粒表面上，例如通过在颗粒形成之后涂覆颗粒，或者通过在形成颗粒之前将表面活性剂并入形成颗粒的材料中。示例性表面活性剂包括磷酸甘油酯，例如二棕榈酰磷脂酰胆碱（DPPC）。这些颗粒可以有效地雾化，用于给呼吸道施用以允许全身或局部递送各种各样的治疗剂。正电荷或带负电荷的治疗剂与相反电荷分子的复合物的形成可以允许在给药后将药剂释放到血流中的释放速率。

6. 发明申请

US20080226730A1 PARTICLES FOR INHALATION HAVING RAPID RELEASE PROPERTIES 审中-公开
标题翻译：具有快速释放特性的吸入颗粒
公开(公告)号：US20080226730A1
公开(公告)日：2008-09-18
申请号：US11860302
申请日：2007-09-24
申请人： Jennifer L. Schmitke , Donghao Chen , Richard P. Batycky , David A. Edwards , Jeffrey S. Hrkach
发明人： Jennifer L. Schmitke , Donghao Chen , Richard P. Batycky , David A. Edwards , Jeffrey S. Hrkach
IPC分类号： A61K9/14 , A61K38/28
CPC分类号： A61K9/1617 , A61K9/0075 , A61K38/28 , A61K47/544
摘要： The invention generally relates to formulations having particles comprising phospholipids, bioactive agent and excipients and the pulmonary delivery thereof. Dry powder inhaled insulin formulations are disclosed. Improved formulations comprising DPPC, insulin and sodium citrate which are useful in the treatment of diabetes are disclosed. Also, the invention relates to a method of for the pulmonary delivery of a bioactive agent comprising administering to the respiratory tract of a patient in need of treatment, or diagnosis an effective amount of particles comprising a bioactive agent or any combination thereof in association, wherein release of the agent from the administered particles occurs in a rapid fashion.
摘要翻译：本发明一般涉及具有包含磷脂，生物活性剂和赋形剂以及其肺部递送的颗粒的制剂。公开了干粉吸入胰岛素制剂。公开了包含可用于治疗糖尿病的DPPC，胰岛素和柠檬酸钠的改进制剂。此外，本发明涉及一种用于肺部递送生物活性剂的方法，包括向需要治疗的患者的呼吸道施用或相关地诊断包含生物活性剂或其任何组合的有效量的颗粒，其中药剂从施用的颗粒的释放以快速方式发生。

7. 再颁专利

USRE41996E1 Composition and methods for enhancing receptor-mediated cellular internalization 有权
标题翻译：用于增强受体介导的细胞内化的组合物和方法
公开(公告)号：USRE41996E1
公开(公告)日：2010-12-14
申请号：US11821513
申请日：2007-06-21
申请人： Daniel R. Deaver , David A. Edwards , Robert S. Langer
发明人： Daniel R. Deaver , David A. Edwards , Robert S. Langer
IPC分类号： A61F2/02 , A61F13/02 , A61K9/48 , A61K9/20 , A61K9/14
CPC分类号： A61K9/0046 , A61K9/0031 , A61K9/0034 , A61K9/0043 , A61K9/006 , A61K9/0073 , A61K9/06 , A61K31/56 , A61K31/573 , A61K31/715 , A61K47/38 , A61K48/00 , A61K48/0008 , A61K48/0083 , Y10S977/906
摘要： Compositions and methods for improving cellular internalization of one or more compounds are disclosed. The compositions include a compound to be delivered and a biocompatible viscous material, such as a hydrogel, lipogel, or highly viscous sol. The composition also include, or are administered in conjunction with, an enhancer in an amount effective to maximize expression of or binding to receptors and enhance RME of the compound into the cells. This leads to high transport rates of compounds to be delivered across cell membranes, facilitating more efficient delivery of drugs and diagnostic agents. Compositions are applied topically orally, nasally, vaginally, rectally, and ocularly. The enhancer is administered with the composition or separately, either systemically or preferably locally. The compound to be delivered can also be the enhancer.
摘要翻译：公开了用于改善一种或多种化合物的细胞内化的组合物和方法。组合物包括待递送的化合物和生物相容的粘性材料，例如水凝胶，脂凝胶或高粘度溶胶。该组合物还包括或者与增效剂一起施用，其量可以有效地最大程度地使受体的表达或结合，并增强化合物进入细胞的RME。这导致要跨细胞膜递送的化合物的高传输速率，有助于更有效地递送药物和诊断剂。组合物经口，鼻，阴道，直肠和眼部局部应用。增强剂与组合物一起施用或分开施用，全部或优选局部施用。待递送的化合物也可以是增强剂。

8. 发明授权

US06977087B2 Aerodynamically light particles for pulmonary drug delivery 失效
标题翻译：用于肺部药物递送的空气动力学轻微颗粒
公开(公告)号：US06977087B2
公开(公告)日：2005-12-20
申请号：US10090418
申请日：2002-03-01
申请人： David A. Edwards , Giovannia Caponetti , Jeffrey S. Hrkach , Noah Lotan , Justin Hanes , Abdell Aziz Ben-Jebria , Robert S. Langer
发明人： David A. Edwards , Giovannia Caponetti , Jeffrey S. Hrkach , Noah Lotan , Justin Hanes , Abdell Aziz Ben-Jebria , Robert S. Langer
IPC分类号： A61K9/00 , A61K9/14 , A61K9/16 , A61K31/56 , A61K31/568 , A61K38/28
CPC分类号： A61K9/0075 , A61K9/1647 , A61K31/56 , A61K31/568 , A61K38/28
摘要： Improved aerodynamically light particles for delivery to the pulmonary system, and methods for their preparation and administration are provided. In a preferred embodiment, the aerodynamically light particles are made of a biodegradable material and have a tap density less than 0.4 g/cm3 and a mass mean diameter between 5 μm and 30 μm. The particles may be formed of biodegradable materials such as biodegradable polymers. For example, the particles may be formed of a functionalized polyester graft copolymer consisting of a linear α-hydroxy-acid polyester backbone having at least one amino acid group incorporated herein and at least on poly(amino acid) side chain extending from an amino acid group in the polyester backbone. In one embodiment, aerodynamically light particles having a large mean diameter, for example greater than 5 μm, can be used for enhanced delivery of a therapeutic or diagnostic agent to the alveolar region of the lung. The aerodynamically light particles optionally can incorporate a therapeutic or diagnostic agent, and may be effectively aerosolized for administration to the respiratory tract to permit systemic or local delivery of a wide variety of incorporated agents.
摘要翻译：提供用于递送至肺系统的改善的空气动力学轻微颗粒，以及其制备和给药方法。在优选的实施方案中，空气动力学轻微颗粒由可生物降解的材料制成，并且振实密度小于0.4g / cm 3，质量平均直径在5μm和30μm之间。颗粒可以由可生物降解的材料如可生物降解的聚合物形成。例如，颗粒可以由官能化的聚酯接枝共聚物形成，所述官能化聚酯接枝共聚物由具有至少一个引入本文的氨基酸基团和至少在从氨基酸延伸的聚（氨基酸）侧链上的直链α-羟基酸聚酯主链组成集团在聚酯骨干。在一个实施方案中，具有大平均直径（例如大于5μm）的空气动力学轻的颗粒可用于增强治疗或诊断剂递送至肺的肺泡区域。空气动力学轻微颗粒任选地可以掺入治疗剂或诊断剂，并且可以有效地雾化用于给予呼吸道以允许各种并入药剂的全身或局部递送。

9. 发明授权

US06399102B1 Aerodynamically light particles for pulmonary drug delivery 有权
公开(公告)号：US06399102B1
公开(公告)日：2002-06-04
申请号：US09562988
申请日：2000-05-01
申请人： David A. Edwards , Giovanni Caponetti , Jeffrey S. Hrkach , Noah Lotan , Justin Hanes , Abdellaziz Ben-Jebria , Robert S. Langer
发明人： David A. Edwards , Giovanni Caponetti , Jeffrey S. Hrkach , Noah Lotan , Justin Hanes , Abdellaziz Ben-Jebria , Robert S. Langer
IPC分类号： A61K914
CPC分类号： A61K9/0075 , A61K9/1647 , A61K31/137
摘要： Improved aerodynamically light particles for drug delivery to the pulmonary system, and methods for their synthesis and administration are provided. In a preferred embodiment, the aerodynamically light particles are made of biodegradable material and have a tap density of less than 0.4 g/cm3 and a mass mean diameter between 5 &mgr;m and 30 &mgr;m. The particles may be formed of biodegradable materials such as biodegradable polymers. For example, the particles may be formed of a functionalized polyester graft copolymer consisting of a linear &agr;-hydroxy-acid polyester backbone having at least one amino acid group incorporated therein and at least one poly(amino acid) side chain extending from an amino acid group in the polyester backbone. In one embodiment, aerodynamically light particles having a large mean diameter, for example greater than 5 &mgr;m, can be used for enhanced delivery of a therapeutic agent to the alveolar region of the lung. The aerodynamically light particles incorporating a therapeutic agent may be effectively aerosolized for administration to the respiratory tract to permit systemic or local delivery of wide variety of therapeutic agents.

10. 发明授权

US5985320A Materials and methods for enhancing cellular internalization 失效
标题翻译：用于增强细胞内化的材料和方法
公开(公告)号：US5985320A
公开(公告)日：1999-11-16
申请号：US810275
申请日：1997-03-03
申请人： David A. Edwards , Daniel R. Deaver , Robert S. Langer
发明人： David A. Edwards , Daniel R. Deaver , Robert S. Langer
IPC分类号： A61K9/06 , A61K9/00 , A61K9/127 , A61K31/70 , A61K31/7088 , A61K38/00 , A61K38/22 , A61K38/43 , A61K38/55 , A61K39/395 , A61K47/10 , A61K47/26 , A61K47/32 , A61K47/36 , A61K47/38 , A61K48/00 , A61K49/00
CPC分类号： A61K9/0043 , A61K47/38 , A61K9/0034 , A61K47/10 , A61K47/26 , A61K47/36 , Y10S436/829
摘要： Compositions and methods for delivering agents across cell membranes are disclosed. The compositions include an agent to be delivered, a viscous material, such as a hydrogel, lipogel or viscous sol, and, optionally, a carrier that includes a ligand that binds to or interacts with cell surface receptors. The agent to be delivered binds to or otherwise interacts with cell surface receptors, is attached, either covalently or ionically to a molecule that binds to or interacts with a cell surface receptor, or is associated with the carrier. Agents to be delivered include bioactive compounds and diagnostic agents. The compositions have an apparent viscosity roughly equal to the viscosity of the cytosol in the cell to which the agent is to be delivered. The rate of cellular internalization is higher when the viscosity of the viscous material and that of the cytosol in the cell are approximately the same, relative to when they are not the same. The compositions enhance cellular entry of bioactive agents and diagnostic materials when administered vaginally, nasally, rectally ocularly, orally, or to the respiratory or pulmonary system.
摘要翻译：公开了用于递送细胞膜的药剂的组合物和方法。组合物包括待递送的试剂，粘性物质，例如水凝胶，脂凝胶或粘稠溶胶，以及任选的包含与细胞表面受体结合或与细胞表面受体相互作用的配体的载体。待递送的药剂与细胞表面受体结合或以其他方式相互作用，与结合细胞表面受体或与细胞表面受体相关的分子共价或离子地连接。待递送的试剂包括生物活性化合物和诊断剂。组合物的表观粘度大致等于试剂要递送的细胞中细胞溶胶的粘度。当粘性物质和细胞质中的细胞溶胶的粘度相差不大时，细胞内化速率较高。当阴道，鼻，直肠眼，口服或呼吸或肺部系统施用时，组合物增强生物活性剂和诊断材料的细胞进入。

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