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1. 发明申请

US20050003003A1 Modulation of release from dry powder formulations 审中-公开
标题翻译：干粉配方的释放调制
公开(公告)号：US20050003003A1
公开(公告)日：2005-01-06
申请号：US10425194
申请日：2003-04-28
申请人： Sujit Basu , Giovanni Caponetti , Daniel Deaver , Katharina Elbert , Jeffrey Hrkach , Michael Lipp
发明人： Sujit Basu , Giovanni Caponetti , Daniel Deaver , Katharina Elbert , Jeffrey Hrkach , Michael Lipp
IPC分类号： A61K9/16 , A61K9/00 , A61K9/26 , A61K9/72 , A61K31/135 , A61K31/137 , A61K31/566 , A61K38/00 , A61K45/00 , A61K47/12 , A61K47/14 , A61K47/18 , A61K47/24 , A61K47/26 , A61K47/28 , A61K47/30 , A61K47/36 , A61K47/42 , A61P11/06 , A61K9/14
CPC分类号： A61K9/0078 , A61K9/0075 , A61K9/1617 , A61K31/135 , A61K31/137 , A61K2300/00
摘要： Particles which include a bioactive agent are prepared to have a desired matrix transition temperature. Delivery of the particles via the pulmonary system results in modulation of drug release from the particles. Sustained release and/or sustained pharmacologic action of the drug can be obtained by forming particles which include a combination of phospholipids that are miscible in one another and have a high matrix transition temperature.
摘要翻译：制备包含生物活性剂的颗粒具有所需的基质转变温度。通过肺系统递送颗粒导致药物从颗粒释放的调节。药物的持续释放和/或持续的药物作用可以通过形成包含相互混溶并具有高基质转变温度的磷脂组合的颗粒来获得。

2. 发明申请

US20050158249A1 Aerodynamically light particles for pulmonary drug delivery 审中-公开
公开(公告)号：US20050158249A1
公开(公告)日：2005-07-21
申请号：US11064065
申请日：2005-02-23
申请人： David Edwards , Giovanni Caponetti , Jeffrey Hrkach , Noah Lotan , Justin Hanes , Abdellaziz Ben-Jebria , Robert Langer
发明人： David Edwards , Giovanni Caponetti , Jeffrey Hrkach , Noah Lotan , Justin Hanes , Abdellaziz Ben-Jebria , Robert Langer
IPC分类号： A61K9/12 , A61K9/00 , A61K9/14 , A61K9/16 , A61K9/72 , A61K31/137 , A61K47/32 , A61K48/00 , A61K31/353 , A61K31/4439 , A61K31/56 , A61K31/573 , A61K38/09
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.

3. 发明授权

US07947742B2 Inhalable epinephrine 有权
标题翻译：可吸入的肾上腺素
公开(公告)号：US07947742B2
公开(公告)日：2011-05-24
申请号：US10607571
申请日：2003-06-26
申请人： Richard P. Batycky , Giovanni Caponetti , Mariko Childs , Elliot Ehrich , Karen Fu , Jeffrey S. Hrkach , Wen-I Li , Michael M. Lipp , Mei-Ling Pan , Jason Summa
发明人： Richard P. Batycky , Giovanni Caponetti , Mariko Childs , Elliot Ehrich , Karen Fu , Jeffrey S. Hrkach , Wen-I Li , Michael M. Lipp , Mei-Ling Pan , Jason Summa
IPC分类号： A61K31/137 , A61K9/14 , A61K9/00
CPC分类号： A61K31/137 , A61K9/0073 , A61K9/0075 , A61K9/1617 , A61K31/135 , A61M15/0091 , A61M2202/06
摘要： The present invention is directed toward particles for delivery of epinephrine to the respiratory system and methods for treating a patient in need of epinephrine. The particles and respirable compositions comprising the particles of the present invention described herein comprise the bioactive agent epinephrine, or a salt thereof, as a therapeutic agent. The particles are preferably formed by spray drying. Preferably, the particles and the respirable compositions are substantially dry and are substantially free of propellents. In a preferred embodiment, the particles have aerodynamic characteristics that permit targeted delivery of epinephrine to the site(s) of action.
摘要翻译：本发明涉及将肾上腺素递送至呼吸系统的颗粒和用于治疗需要肾上腺素的患者的方法。包含本文所述的本发明的颗粒的颗粒和可呼吸组合物包含作为治疗剂的生物活性剂肾上腺素或其盐。颗粒优选通过喷雾干燥形成。优选地，颗粒和可呼吸组合物基本上是干燥的并且基本上不含推进剂。在优选的实施方案中，颗粒具有允许将肾上腺素靶向递送至作用部位的空气动力特性。

4. 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.

5. 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.

6. 发明授权

US08415397B2 Inhalable epinephrine 有权
标题翻译：可吸入的肾上腺素
公开(公告)号：US08415397B2
公开(公告)日：2013-04-09
申请号：US13082626
申请日：2011-04-08
申请人： Richard P. Batycky , Giovanni Caponetti , Mariko Childs , Elliot Ehrich , Karen Fu , Jeffrey S. Hrkach , Wen-I Li , Michael M. Lipp , Mei-Ling Pan , Jason Summa
发明人： Richard P. Batycky , Giovanni Caponetti , Mariko Childs , Elliot Ehrich , Karen Fu , Jeffrey S. Hrkach , Wen-I Li , Michael M. Lipp , Mei-Ling Pan , Jason Summa
IPC分类号： A61K9/14 , A61K31/13 , A61K31/135 , A61K31/045
CPC分类号： A61K31/137 , A61K9/0073 , A61K9/0075 , A61K9/1617 , A61K31/135 , A61M15/0091 , A61M2202/06
摘要： The present invention is directed toward particles for delivery of epinephrine to the respiratory system and methods for treating a patient in need of epinephrine. The particles and respirable compositions comprising the particles of the present invention described herein comprise the bioactive agent epinephrine, or a salt thereof, as a therapeutic agent. The particles are preferably formed by spray drying. Preferably, the particles and the respirable compositions are substantially dry and are substantially free of propellents. In a preferred embodiment, the particles have aerodynamic characteristics that permit targeted delivery of epinephrine to the site(s) of action.
摘要翻译：本发明涉及将肾上腺素递送至呼吸系统的颗粒和用于治疗需要肾上腺素的患者的方法。包含本文所述的本发明的颗粒的颗粒和可呼吸组合物包含作为治疗剂的生物活性剂肾上腺素或其盐。颗粒优选通过喷雾干燥形成。优选地，颗粒和可呼吸组合物基本上是干燥的并且基本上不含推进剂。在优选的实施方案中，颗粒具有允许将肾上腺素靶向递送至作用部位的空气动力特性。

7. 发明授权

US08252334B2 Dry powder pharmaceutical compositions comprising surfactants, hydrophobic active principles, and water-soluble excipients, process of preparing, and stable aqueous suspensions thereof 有权
标题翻译：包含表面活性剂，疏水性活性成分和水溶性赋形剂的干粉药物组合物，制备方法及其稳定的水性悬浮液
公开(公告)号：US08252334B2
公开(公告)日：2012-08-28
申请号：US11578661
申请日：2005-04-21
申请人： Giovanni Caponetti , Mariella Artusi , Loretta Maggi , Paolo Corvi Mora
发明人： Giovanni Caponetti , Mariella Artusi , Loretta Maggi , Paolo Corvi Mora
IPC分类号： A61K9/00 , A61K9/10 , A61K9/14
CPC分类号： A61K9/145 , A61K9/0075 , A61K9/0078 , A61K9/14 , A61K9/143 , A61K31/192 , A61K31/573 , A61K31/58
摘要： Pharmaceutical composition in a dry powder form comprising at least one hydrophobic active principle, at least one water-soluble excipient and at least one surfactant, wherein the particles in said dry powder state have a Volume Mean Diameter VMDd greater than the Volume Mean Diameter VMDw of particles in a suspension obtained from said pharmaceutical composition at standard conditions of dispersion in a water-medium. It is also disclosed a process to prepare such dry composition and an extemporaneous suspension for inhalation therapy obtainable from said dry composition.
摘要翻译：包含至少一种疏水活性成分，至少一种水溶性赋形剂和至少一种表面活性剂的干粉形式的药物组合物，其中所述干粉状态的颗粒的体积平均直径VMDd大于体积平均直径VMDd，在由水介质中分散的标准条件下由所述药物组合物获得的悬浮液中的颗粒。还公开了制备这种干组合物和可从所述干组合物获得的用于吸入治疗的临时悬浮液的方法。

8. 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。

9. 发明授权

US06780508B1 Powder particles with smooth surface for use in inhalation therapy 有权
标题翻译：具有光滑表面的粉末颗粒用于吸入治疗
公开(公告)号：US06780508B1
公开(公告)日：2004-08-24
申请号：US10030686
申请日：2002-04-16
申请人： Giovanni Caponetti , Pier Luigi Catellani , Ruggero Bettini , Paolo Colombo , Paolo Ventura
发明人： Giovanni Caponetti , Pier Luigi Catellani , Ruggero Bettini , Paolo Colombo , Paolo Ventura
IPC分类号： B32B516
CPC分类号： A61K9/0075 , A61K9/145 , A61K9/1623 , Y10T428/2991 , Y10T428/2998
摘要： Carriers for use in the preparation of mixtures for inhalation powders intended for pulmonary administration of micronized drugs by means of a dry powder inhaler and the method for their preparation are described.
摘要翻译：描述了用于制备用于通过干粉吸入器肺部给予微粉化药物的吸入粉末的混合物的载体及其制备方法。

10. 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。

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