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1. 发明申请

US20070104658A1 Use of simple amino acids to form porous particles 审中-公开
公开(公告)号：US20070104658A1
公开(公告)日：2007-05-10
申请号：US11637353
申请日：2006-12-12
申请人： Richard Batycky , Michael Lipp , Ralph Niven
发明人： Richard Batycky , Michael Lipp , Ralph Niven
IPC分类号： A61K9/14
CPC分类号： A61K9/1617 , A61K9/0075 , A61K9/0082 , A61K9/145 , A61K31/137 , A61K31/685 , A61K47/183
摘要： Particles having a tap density of less than 0.4 g/cm3 include a hydrophobic amino acid or salt thereof and a therapeutic, prophylactic or diagnostic agent or any combination thereof. Preferred particles include a phospholipid, have a median geometric diameter between about 5 and about 30 microns and an aerodynamic diameter between about 1 and about 5 microns. The particles can be formed by spray-drying and are useful for delivery to the pulmonary system.

2. 发明申请

US20070104657A1 Particulate compositions for pulmonary delivery 有权
公开(公告)号：US20070104657A1
公开(公告)日：2007-05-10
申请号：US11633750
申请日：2006-12-05
申请人： Richard Batycky , David Edwards , Michael Lipp
发明人： Richard Batycky , David Edwards , Michael Lipp
IPC分类号： A61K9/14
CPC分类号： A61K9/0075 , A61K9/1694
摘要： This invention concerns an improved particulate composition for delivering a drug to the pulmonary system. Applicants disclose a method of identifying an optimal form of aerodynamically light particles which are highly dispersible. The particles of the instant invention are made by creating hollow, spherical drug particles (i.e., progenitor particles) that collapse in the process of particle formation, leading to wrinkled, thin-walled drug particles of very low envelope density. Additionally, Applicants have found that such particles are especially optimal for inhaled aerosols when the surface area parameter (σ) is greater than 2, optimally greater than 3.

3. 发明申请

US20050191360A1 Particles for inhalation having rapid release properties 审中-公开
标题翻译：具有快速释放性能的吸入颗粒
公开(公告)号：US20050191360A1
公开(公告)日：2005-09-01
申请号：US11051497
申请日：2005-02-04
申请人： Richard Batycky , Michael Lipp
发明人： Richard Batycky , Michael Lipp
IPC分类号： A61K9/00 , A61K9/14 , A61K38/29 , A61K47/24
CPC分类号： A61K9/0075 , A61K47/24
摘要： The invention generally relates to formulations having particles comprising phospholipids, bioactive agent and excipients and the pulmonary delivery thereof. Dry powder inhaled PTH formulations are disclosed. Improved formulations comprising DPPC, PTH and sodium citrate which are useful in the treatment of lowered PTH conditions 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 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. Kits containing receptacles of the formulations are also disclosed.
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PTH制剂。公开了可用于治疗降低的PTH病症的包含DPPC，PTH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，其包括向需要治疗的患者的呼吸道施用有效量的包含生物活性剂或其任何组合的颗粒，其中释放来自施用颗粒的试剂以快速方式发生。还公开了含有制剂的容器的试剂盒。

4. 发明申请

US20070123449A1 High load particles for inhalation having rapid release properties 审中-公开
标题翻译：用于吸入的高负载颗粒具有快速释放性能
公开(公告)号：US20070123449A1
公开(公告)日：2007-05-31
申请号：US11590562
申请日：2006-10-31
申请人： Henry Brush , Fen-Ni Fu , Michael Lipp , Jennifer Schmitke
发明人： Henry Brush , Fen-Ni Fu , Michael Lipp , Jennifer Schmitke
IPC分类号： A61K38/28 , A61K31/19
CPC分类号： A61K38/28 , A61K9/0075 , A61K9/10 , A61K9/1272 , A61K9/1611 , A61K9/1617 , A61K31/19
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。

5. 发明申请

US20070041912A1 Trospium containing compositions 审中-公开
标题翻译：含有Trospium的组合物
公开(公告)号：US20070041912A1
公开(公告)日：2007-02-22
申请号：US10550471
申请日：2003-09-04
申请人： Elliot Ehrich , Daniel Deaver , Robert Clarke , Michael Lipp
发明人： Elliot Ehrich , Daniel Deaver , Robert Clarke , Michael Lipp
IPC分类号： A61K31/4747 , A61L9/04
CPC分类号： A61K9/0078 , A61K9/0075 , A61K9/1617 , A61K31/40 , A61K31/438 , A61K31/46 , A61K45/06
摘要： The invention relates to a method for treating a disease characterized by a constrictive airway comprising administering to a patient in need thereof via inhalation a pharmaceutical composition comprising trospium, wherein said patient achieves an effective therapy for at least 10 hours. The trospium composition is preferably a particulate formulation useful for administration via a dry powder inhaler. In a preferred embodiment, the composition further comprises a second active agent, such as a beta-2 agonist. A particularly preferred second active agent is formoterol, wherein the trospium, formoterol composition is manufactured by spray drying a mixture comprising trospium and formoterol.
摘要翻译：本发明涉及用于治疗特征在于缩窄性气道的疾病的方法，其包括通过吸入给予有需要的患者包含trospium的药物组合物，其中所述患者达到有效治疗至少10小时。 ium组合物优选是可用于通过干粉吸入器施用的颗粒制剂。在优选的实施方案中，组合物还包含第二活性剂，例如β-2激动剂。特别优选的第二活性剂是福莫特罗，其中通过将包含trospium和福莫特罗的混合物喷雾干燥来制备tro石福莫特罗组合物。

6. 发明授权

US07048908B2 Particles for inhalation having sustained release properties 有权
公开(公告)号：US07048908B2
公开(公告)日：2006-05-23
申请号：US10202616
申请日：2002-07-23
申请人： Sujit K. Basu , Jeffrey Hrkach , Michael Lipp , Katharina Elbert , David A. Edwards
发明人： Sujit K. Basu , Jeffrey Hrkach , Michael Lipp , Katharina Elbert , David A. Edwards
IPC分类号： A61K9/12 , A61K9/127
CPC分类号： A61K9/0075 , A61K9/1617 , A61K38/28 , A61K47/544 , Y10S514/958
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.

7. 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。

8. 发明申请

US20060134009A1 Low dose corticosteroid powders for inhalation 审中-公开
标题翻译：用于吸入的低剂量皮质类固醇粉末
公开(公告)号：US20060134009A1
公开(公告)日：2006-06-22
申请号：US11302535
申请日：2005-12-13
申请人： Daniel Deaver , Michael Lipp
发明人： Daniel Deaver , Michael Lipp
IPC分类号： A61K31/573 , A61K9/14 , A61L9/04
CPC分类号： A61K9/0075 , A61K31/573
摘要： The invention relates to a method of treating a corticosteroid-responsive condition of the air passage ways and lungs by delivering a corticosteroid to the pulmonary system of a patient, comprising administering a particle mass comprising a corticosteroid from an inhaler characterized in that the corticosteroid is not substantially deposited in the mouth and throat and is not substantially systemically absorbed. The invention also relates to receptacles containing the particle mass and the inhaler for use therein.
摘要翻译：本发明涉及通过将皮质类固醇递送到患者的肺部系统来治疗空气通道和肺的皮质类固醇反应状态的方法，包括从吸入器施用包含皮质类固醇的颗粒物质，其特征在于皮质类固醇不是基本上沉积在嘴和喉部并且基本上不被全身吸收。本发明还涉及包含用于其中的颗粒物质和吸入器的容器。

9. 发明申请

US20060105051A1 Manufacture of particles for pulmonary drug delivery by carbon dioxide assisted nebulization 审中-公开
标题翻译：通过二氧化碳辅助雾化制造用于肺部药物递送的颗粒
公开(公告)号：US20060105051A1
公开(公告)日：2006-05-18
申请号：US11260884
申请日：2005-10-27
申请人： Blair Jackson , David Bennett , Donghao Chen , Michael Lipp , Purav Dave
发明人： Blair Jackson , David Bennett , Donghao Chen , Michael Lipp , Purav Dave
IPC分类号： A61K9/14 , B29B9/00
CPC分类号： A61K9/007 , A61K9/0075
摘要： Methods of making porous particles by using carbon dioxide assisted nebulization (CAN) technology in combination with spray drying technologies are disclosed. As the mixture of carbon dioxide (CO2) and the solvent with drug matrix is expanded through the nebulizer to atmospheric conditions, the resulting aerosol contains fine micro-bubbles and/or micro-droplets that contains dissolved CO2 which is co-currently fed into a spray drying chamber.
摘要翻译：公开了通过使用二氧化碳辅助雾化（CAN）技术与喷雾干燥技术组合制备多孔颗粒的方法。由于二氧化碳（CO 2 CO 2）和溶剂与药物基质的混合物通过喷雾器膨胀至大气条件，所得气溶胶含有细小的微气泡和/或微滴，其含有溶解的CO 其共同进料到喷雾干燥室中。

10. 发明申请

US20080039366A1 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：US20080039366A1
公开(公告)日：2008-02-14
申请号：US11436404
申请日：2006-05-18
申请人： Sujit K. Basu , Jeffrey Hrkach , Michael Lipp , Katharina Elbert , David A. Edwards
发明人： Sujit K. Basu , Jeffrey Hrkach , Michael Lipp , Katharina Elbert , David A. Edwards
IPC分类号： A61K38/28 , A61P3/00
CPC分类号： A61K9/0075 , A61K9/1617 , A61K38/28 , A61K47/544 , Y10S514/958
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。

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