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1. 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.

2. 发明授权

US06436443B2 Porous particles comprising excipients for deep lung delivery 有权
标题翻译：包含用于深肺输送的赋形剂的多孔颗粒
公开(公告)号：US06436443B2
公开(公告)日：2002-08-20
申请号：US09888688
申请日：2001-06-25
申请人： David A. Edwards , Giovanni Caponetti , Jeffrey S. Hrkach , Noah Lotan , Justin Hanes , Robert S. Langer , Abdellaziz Ben-Jebria
发明人： David A. Edwards , Giovanni Caponetti , Jeffrey S. Hrkach , Noah Lotan , Justin Hanes , Robert S. Langer , Abdellaziz Ben-Jebria
IPC分类号： A61K914
CPC分类号： A61K9/0075 , A61K9/1647 , A61K31/137 , Y10S514/826 , Y10S514/851
摘要： Improved porous particles for drug delivery to the pulmonary system, and methods for their synthesis and administration are provided. In a preferred embodiment, the porous particles are made of a biodegradable material and have a mass density less than 0.4 g/cm3/. 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, porous particles having a relatively 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 porous 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.
摘要翻译：提供用于向肺系统递送药物的改进的多孔颗粒，以及用于其合成和给药的方法。在优选的实施方案中，多孔颗粒由可生物降解的材料制成，其质量密度小于0.4g / cm 3 /。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，所述聚酯接枝共聚物由具有至少一个氨基酸基团的直链α-羟基酸聚酯主链和至少一个从氨基酸延伸的聚（氨基酸）侧链组成集团在聚酯骨干。在一个实施方案中，具有相对大的平均直径，例如大于5um的多孔颗粒可用于增强治疗剂递送至肺的肺泡区域。掺入治疗剂的多孔颗粒可以有效地雾化，用于给予呼吸道以允许全身或局部递送多种治疗剂。

3. 发明授权

US06447752B2 Amorphous porous particles for deep lung delivery 有权
标题翻译：用于深肺输送的无定形多孔颗粒
公开(公告)号：US06447752B2
公开(公告)日：2002-09-10
申请号：US09888781
申请日：2001-06-25
申请人： David A. Edwards , Giovanni Caponetti , Jeffrey S. Hrkach , Noah Lotan , Justin Hanes , Robert S. Langer , Abdellaziz Ben-Jebria
发明人： David A. Edwards , Giovanni Caponetti , Jeffrey S. Hrkach , Noah Lotan , Justin Hanes , Robert S. Langer , Abdellaziz Ben-Jebria
IPC分类号： A61K912
CPC分类号： A61K9/0075 , A61K9/1647 , A61K31/137 , Y10S514/826 , Y10S514/851
摘要： Improved porous particles for drug delivery to the pulmonary system, and methods for their synthesis and administration are provided. In a preferred embodiment, the porous particles are made of a biodegradable material and have a mass density less than 0.4 g/cm3/. 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, porous particles having a relatively 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 porous 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.
摘要翻译：提供用于向肺系统递送药物的改进的多孔颗粒，以及用于其合成和给药的方法。在优选的实施方案中，多孔颗粒由可生物降解的材料制成，其质量密度小于0.4g / cm 3 /。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，颗粒可以由官能化聚酯接枝共聚物形成，该聚酯接枝共聚物由具有至少一个氨基酸基团的直链α-羟基酸聚酯主链和至少一个从氨基酸延伸的聚（氨基酸）侧链组成集团在聚酯骨干。在一个实施方案中，具有相对大的平均直径，例如大于5um的多孔颗粒可用于增强治疗剂递送至肺的肺泡区域。掺入治疗剂的多孔颗粒可以有效地雾化，用于给予呼吸道以允许全身或局部递送多种治疗剂。

4. 发明授权

US07435408B2 Porous particles comprising excipients for deep lung delivery 有权
标题翻译：包含用于深肺输送的赋形剂的多孔颗粒
公开(公告)号：US07435408B2
公开(公告)日：2008-10-14
申请号：US10818902
申请日：2004-04-06
申请人： David A. Edwards , Giovanni Caponetti , Jeffrey S. Hrkach , Noah Lotan , Justin Hanes , Robert S. Langer , Abdellaziz Ben-Jebria
发明人： David A. Edwards , Giovanni Caponetti , Jeffrey S. Hrkach , Noah Lotan , Justin Hanes , Robert S. Langer , Abdellaziz Ben-Jebria
IPC分类号： A61K9/00 , A61K9/12 , A61K9/14 , A61K38/00 , A61K33/00 , A61K31/00 , A61K31/70 , A61K31/7052
CPC分类号： A61K9/0075 , A61K9/1647 , A61K31/137 , Y10S514/826 , Y10S514/851
摘要： Improved porous particles for drug delivery to the pulmonary system, and methods for their synthesis and administration are provided. In a preferred embodiment, the porous particles are made of a biodegradable material and have a mass density less than 0.4 g/cm3/. 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 a-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, porous particles having a relatively large mean diameter, for example greater than 5 μm, can be used for enhanced delivery of a therapeutic agent to the alveolar region of the lung. The porous 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.
摘要翻译：提供用于向肺系统递送药物的改进的多孔颗粒，以及用于其合成和给药的方法。在优选的实施方案中，多孔颗粒由可生物降解的材料制成，并具有小于0.4g / cm 3的质量密度。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，该聚酯接枝共聚物由具有至少一个氨基酸基团的直链α-羟基酸聚酯主链和至少一个从氨基酸延伸的至少一个（氨基酸）侧链集团在聚酯骨干。在一个实施方案中，具有相对大的平均直径，例如大于5um的多孔颗粒可用于增强治疗剂递送至肺的肺泡区域。掺入治疗剂的多孔颗粒可以有效地雾化，用于给予呼吸道以允许全身或局部递送多种治疗剂。

5. 发明授权

US06635283B2 Aerodynamically light particles for pulmonary drug delivery 有权
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：US06635283B2
公开(公告)日：2003-10-21
申请号：US10027212
申请日：2001-12-20
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.
摘要翻译：提供用于向肺系统输送药物的空气动力学轻微颗粒，以及用于其合成和给药的方法。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，颗粒可以由官能化聚酯接枝共聚物形成，该聚酯接枝共聚物由具有至少一个氨基酸基团的直链α-羟基酸聚酯主链和至少一个从氨基酸延伸的聚（氨基酸）侧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）的空气动力学轻微颗粒可用于增强治疗剂递送至肺的肺泡区域。掺入治疗剂的空气动力学轻微颗粒可以被有效地雾化，用于给予呼吸道以允许全身或局部递送多种治疗剂。

6. 发明授权

US06447753B2 Porous particles for deep lung delivery 有权
标题翻译：用于深肺输送的多孔颗粒
公开(公告)号：US06447753B2
公开(公告)日：2002-09-10
申请号：US09891131
申请日：2001-06-25
申请人： David A. Edwards , Giovanni Caponetti , Jeffrey S. Hrkach , Noah Lotan , Justin Hanes , Robert S. Langer , Abdellaziz Ben-Jebria
发明人： David A. Edwards , Giovanni Caponetti , Jeffrey S. Hrkach , Noah Lotan , Justin Hanes , Robert S. Langer , Abdellaziz Ben-Jebria
IPC分类号： A61K912
CPC分类号： A61K9/0075 , A61K9/1647 , A61K31/137 , Y10S514/826 , Y10S514/851
摘要： Improved porous particles for drug delivery to the pulmonary system, and methods for their synthesis and administration are provided. In a preferred embodiment, the porous particles are made of a biodegradable material and have a mass density less than 0.4 g/cm3/. 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, porous particles having a relatively 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 porous 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.
摘要翻译：提供用于向肺系统递送药物的改进的多孔颗粒，以及用于其合成和给药的方法。在优选的实施方案中，多孔颗粒由可生物降解的材料制成，其质量密度小于0.4g / cm 3 /。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，颗粒可以由官能化聚酯接枝共聚物形成，该聚酯接枝共聚物由具有至少一个氨基酸基团的直链α-羟基酸聚酯主链和至少一个从氨基酸延伸的聚（氨基酸）侧链组成集团在聚酯骨干。在一个实施方案中，具有相对大的平均直径，例如大于5um的多孔颗粒可用于增强治疗剂递送至肺的肺泡区域。掺入治疗剂的多孔颗粒可以有效地雾化，用于给予呼吸道以允许全身或局部递送多种治疗剂。

7. 发明授权

US06942868B2 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：US06942868B2
公开(公告)日：2005-09-13
申请号：US10441948
申请日：2003-05-20
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： A61K9/12 , A61K9/00 , A61K9/14 , A61K9/16 , A61K9/72 , A61K31/137 , A61K47/32 , A61K49/00 , A61L15/00
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 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 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 μm, 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.
摘要翻译：提供用于向肺系统输送药物的空气动力学轻微颗粒，以及用于其合成和给药的方法。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。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，所述聚酯接枝共聚物由具有至少一个氨基酸基团的直链α-羟基酸聚酯主链和至少一个从氨基酸延伸的聚（氨基酸）侧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）的空气动力学轻微颗粒可用于增强治疗剂递送至肺的肺泡区域。掺入治疗剂的空气动力学轻微颗粒可以被有效地雾化，用于给予呼吸道以允许全身或局部递送多种治疗剂。

8. 发明授权

US06740310B2 Porous particles comprising excipients for deep lung delivery 有权
公开(公告)号：US06740310B2
公开(公告)日：2004-05-25
申请号：US10209654
申请日：2002-07-30
申请人： David A. Edwards , Giovanni Caponetti , Jeffrey S. Hrkach , Noah Lotan , Justin Hanes , Robert S. Langer , Abdellaziz Ben-Jebria
发明人： David A. Edwards , Giovanni Caponetti , Jeffrey S. Hrkach , Noah Lotan , Justin Hanes , Robert S. Langer , Abdellaziz Ben-Jebria
IPC分类号： A61K912
CPC分类号： A61K9/0075 , A61K9/1647 , A61K31/137 , Y10S514/826 , Y10S514/851
摘要： Improved porous particles for drug delivery to the pulmonary system, and methods for their synthesis and administration are provided. In a preferred embodiment, the porous particles are made of a biodegradable material and have a mass density less than 0.4 g/cm3/. 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 a-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, porous particles having a relatively 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 porous 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.

9. 发明授权

US06254854B1 Porous particles for deep lung delivery 有权
公开(公告)号：US06254854B1
公开(公告)日：2001-07-03
申请号：US09569153
申请日：2000-05-11
申请人： David A. Edwards , Giovanni Caponetti , Jeffrey S. Hrkach , Noah Lotan , Justin Hanes , Robert S. Langer , Abdellaziz Ben-Jebria
发明人： David A. Edwards , Giovanni Caponetti , Jeffrey S. Hrkach , Noah Lotan , Justin Hanes , Robert S. Langer , Abdellaziz Ben-Jebria
IPC分类号： A61K912
CPC分类号： A61K9/0075 , A61K9/1647 , A61K31/137 , Y10S514/826 , Y10S514/851
摘要： Improved porous particles for drug delivery to the pulmonary system, and methods for their synthesis and administration are provided. In a preferred embodiment, the porous particles are made of a biodegradable material and have a mass density less than 0.4 g/cm3/. 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, porous particles having a relatively 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 porous 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

US5874064A Aerodynamically light particles for pulmonary drug delivery 失效
公开(公告)号：US5874064A
公开(公告)日：1999-02-23
申请号：US739308
申请日：1996-10-29
申请人： David A. Edwards , Giovanni Caponetti , Jeffrey S. Hrkach , Noah Lotan , Justin Hanes , Abdell Aziz Ben-Jebria , Robert S. Langer
发明人： David A. Edwards , Giovanni Caponetti , Jeffrey S. Hrkach , Noah Lotan , Justin Hanes , Abdell Aziz Ben-Jebria , Robert S. Langer
IPC分类号： A61K9/12 , A61K9/00 , A61K9/14 , A61K9/16 , A61K9/72 , A61K31/137 , A61K47/32
CPC分类号： A61K9/0075 , A61K31/137 , A61K9/1647
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 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. 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 .alpha.-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 .mu.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.

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