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1.发明授权Stable pharmaceutical solution formulations for pressurized metered dose inhalers 失效用于加压计量剂量吸入器的稳定的药物溶液制剂公开(公告)号：US07381402B2
公开(公告)日：2008-06-03
申请号：US11065569
申请日：2005-02-25
IPC分类号： A61K9/12 , A61K9/08 , A61K31/47 , A61K31/4704 , A61M11/00 , A61M11/04 , A61M15/00 , A61M15/06
CPC分类号： A61K9/008 , A61K31/137 , A61K31/47 , A61K31/4704 , A61K47/02 , A61M15/009 , A61M2205/0222 , A61K2300/00
摘要： Aerosol solution formulations for use in an aerosol inhaler which comprise 8-hydroxy-5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino]-ethyl]-2(1H)-quinolinone or a salt thereof, in particular the hydrochloride salt (TA 2005), as an active ingredient, a propellant containing a hydrofluoroalkane, and a cosolvent, stabilized by addition of a specific small amount of a high concentrated phosphoric acid exhibit improved shelf life. The formulation may be optionally contained in a can having part or all of its internal metallic surfaces lined with an inert organic coating.
摘要翻译： 用于气溶胶吸入器的气溶胶溶液制剂，其包含8-羟基-5 - [（1R）-1-羟基-2 - [[（1R）-2-（4-甲氧基苯基）-1-甲基乙基]氨基] - 乙基 ] -2（1H） - 喹啉酮或其盐，特别是盐酸盐（TA 2005）作为活性成分，含有氢氟烷烃和助溶剂的推进剂，通过加入特定量的高浓度 磷酸表现出改善的保质期。 制剂可以任选地包含在其内部具有惰性有机涂层的部分或全部内部金属表面的罐中。
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2.发明申请Stable Pharmaceutical Solution Formulations for Pressurized Metered Dose Inhalers 审中-公开用于加压计量吸入器的稳定的药物溶液制剂公开(公告)号：US20070025920A1
公开(公告)日：2007-02-01
申请号：US11467515
申请日：2006-08-25
IPC分类号： A61L9/04 , A61K31/4704
CPC分类号： A61K31/4704 , A61K9/008 , A61K47/02 , A61M15/009
摘要： Aerosol solution formulations for use in an aerosol inhaler include 8-hydroxy-5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1-methyl ethyl]amino]ethyl]-2(1H)-quinolinone or a salt thereof, preferably the hydrochloride thereof, as an active ingredient, a propellant containing a hydrofluoroalkane, and a cosolvent, stabilized by addition of a specific small amount of a high concentrated phosphoric acid and optionally by the use of a suitable can having part or all of its internal metallic surfaces lined with an inert organic coating.
摘要翻译： 用于气溶胶吸入器的气溶胶溶液制剂包括8-羟基-5 - [（1R）-1-羟基-2 - [[（1R）-2-（4-甲氧基苯基）-1-甲基乙基]氨基]乙基] -2（1H） - 喹啉酮或其盐，优选其盐酸盐作为活性成分，含有氢氟烷烃和助溶剂的推进剂，通过加入特定量的高浓度磷酸和任选地通过 使用合适的罐，其具有内部具有惰性有机涂层的部分或全部内部金属表面。
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3.发明申请Stable pharmaceutical solution formulations for pressurized metered dose inhalers 失效用于加压计量剂量吸入器的稳定的药物溶液制剂公开(公告)号：US20050220718A1
公开(公告)日：2005-10-06
申请号：US11065569
申请日：2005-02-25
CPC分类号： A61K9/008 , A61K31/137 , A61K31/47 , A61K31/4704 , A61K47/02 , A61M15/009 , A61M2205/0222 , A61K2300/00
摘要： Aerosol solution formulations for use in an aerosol inhaler which comprise 8-hydroxy-5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino]-ethyl]-2(1H)-quinolinone or a salt thereof, in particular the hydrochloride salt (TA 2005), as an active ingredient, a propellant containing a hydrofluoroalkane, and a cosolvent, stabilized by addition of a specific small amount of a high concentrated phosphoric acid exhibit improved shelf life. The formulation may be optionally contained in a can having part or all of its internal metallic surfaces lined with an inert organic coating.
摘要翻译： 用于气溶胶吸入器的气溶胶溶液制剂，其包含8-羟基-5 - [（1R）-1-羟基-2 - [[（1R）-2-（4-甲氧基苯基）-1-甲基乙基]氨基] - 乙基 ] -2（1H） - 喹啉酮或其盐，特别是盐酸盐（TA 2005）作为活性成分，含有氢氟烷烃和助溶剂的推进剂，通过加入特定量的高浓度 磷酸表现出改善的保质期。 制剂可以任选地包含在其内部具有惰性有机涂层的部分或全部内部金属表面的罐中。
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4.发明申请Pharmaceutical aerosol formulations for pressurized metered dose inhalers comprising a sequestering agent 有权用于加压计量剂量吸入器的药物气溶胶制剂，其包含螯合剂公开(公告)号：US20060193785A1
公开(公告)日：2006-08-31
申请号：US11361562
申请日：2006-02-24
申请人： David Lewis , Brian Meakin , Maurizio Delcanale , Fausto Pivetti
发明人： David Lewis , Brian Meakin , Maurizio Delcanale , Fausto Pivetti
IPC分类号： A61K31/573 , A61K31/4704 , A61L9/04
CPC分类号： A61K9/008 , A61K31/4704 , A61K31/573 , A61K31/58 , A61K47/02
摘要： Aerosol solution formulation for use in an aerosol inhaler which includes at least one active ingredient selected from 20-ketosteroids and quinolinone derivatives, a propellant containing a hydrofluoroalkane, a cosolvent, and a specific amount of a sequestering agent that stabilizes the formulation. By way of example, the stabilizing agent may be phosphoric acid or sulphuric acid.
摘要翻译： 用于气溶胶吸入器的气溶胶溶液制剂，其包含至少一种选自20-酮类和喹啉酮衍生物的活性成分，含有氢氟烷烃的助推剂，助溶剂和稳定该制剂的特定量的螯合剂。 举例来说，稳定剂可以是磷酸或硫酸。
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5.发明授权公开(公告)号：US06713047B1
公开(公告)日：2004-03-30
申请号：US09831886
申请日：2001-07-18
申请人： David Lewis , David Ganderton , Brian Meakin , Paolo Ventura , Gaetano Brambilla , Raffaella Garzia
发明人： David Lewis , David Ganderton , Brian Meakin , Paolo Ventura , Gaetano Brambilla , Raffaella Garzia
IPC分类号： A61K912
CPC分类号： A61K9/008
摘要： In a solution composition for use in an aerosol inhaler which comprises an active material, a propellant containing a hydrofluoroalkane, a cosolvent and optionally a low volatility compound the use of a mixture of HFA 134a and HFA 227 allows to modulate the mass median aerodynamic diameter (MMAD) of the aerosol particles on actuation of the inhaler to target specific regions of the respiratory tract. Moreover the fine particle dose (FPD) of the active ingredient in the composition increases by reducing the metering chamber volume.
摘要翻译： 在用于气溶胶吸入器的溶液组合物中，其包含活性物质，含有氢氟烷烃，助溶剂和任选的低挥发性化合物的推进剂，使用HFA134a和HFA227的混合物允许调节质量中值空气动力学直径（ MMAD）气雾剂颗粒在致动吸入器以靶向呼吸道的特定区域时。 此外，组合物中活性成分的细颗粒剂量（FPD）通过减少计量室体积而增加。
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公开(公告)号：US20060083693A1
公开(公告)日：2006-04-20
申请号：US11289479
申请日：2005-11-30
IPC分类号： A61L9/04 , A61K31/573 , A61K31/4745 , A61M11/00
摘要： An aerosol solution composition for use in an aerosol inhaler comprises an active material, a propellant containing a hydrofluoroalkane, a cosolvent and optionally a low volatility component to increase the mass median aerodynamic diameter (MMAD) of the aerosol particles on actuation of the inhaler. The composition is stabilized by using a small amount of mineral acid and a suitable can having part or all of its internal metallic surfaces made of stainless steel, anodized aluminium or lined with an inert organic coating.
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7.发明授权Stable pharmaceutical solution formulations for pressurized metered dose inhalers 有权用于加压计量剂量吸入器的稳定的药物溶液制剂公开(公告)号：US07018618B2
公开(公告)日：2006-03-28
申请号：US10640005
申请日：2003-08-14
CPC分类号： A61K9/008 , A61K9/124 , A61K31/167 , A61K31/439 , A61K31/4745 , A61K31/5386 , A61K31/573 , A61K45/06 , A61K2300/00
摘要： An aerosol solution composition for use in an aerosol inhaler comprises an active material, a propellant containing a hydrofluoroalkane, a cosolvent and optionally a low volatility component to increase the mass median aerodynamic diameter (MMAD) of the aerosol particles on actuation of the inhaler.The composition is stabilized by using a small amount of mineral acid and a suitable can having part or all of its internal metallic surfaces made of stainless steel, anodized aluminium or lined with an inert organic coating.
摘要翻译： 用于气溶胶吸入器的气溶胶溶液组合物包含活性物质，含有氢氟烷烃的助推剂，助溶剂和任选的低挥发性成分，以增加气雾剂颗粒在吸入器致动时的质量中值空气动力学直径（MMAD）。 通过使用少量的无机酸和适当的罐来稳定组合物，该罐具有由不锈钢，阳极氧化铝或惰性有机涂层衬里制成的部分或全部内部金属表面。
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8.发明申请Aerosol formulations for pulmonary administration of medicaments to produce a systemic effect 审中-公开用于肺部给药的气溶胶制剂以产生全身效应公开(公告)号：US20050129621A1
公开(公告)日：2005-06-16
申请号：US10505679
申请日：2003-02-26
申请人： Rebecca Davies , David Ganderton , David Lewis , Brian Meakin , Gaetano Brambilla , Alessandra Ferraris
发明人： Rebecca Davies , David Ganderton , David Lewis , Brian Meakin , Gaetano Brambilla , Alessandra Ferraris
IPC分类号： A61K9/12 , A61K9/00 , A61K31/00 , A61K31/4704 , A61K31/485 , A61K45/06 , A61K47/10 , A61K47/14 , A61K47/34 , A61P25/04 , A61L9/04
CPC分类号： A61K9/008 , A61K31/00 , A61K31/4704 , A61K31/485 , A61K45/06 , A61K47/10 , A61K2300/00
摘要： The invention discloses an aerosol pharmaceutical composition comprising a medicament in solution in a mixture of a hydrfluoroalkane propellant and one or more co-solvents wherein the aerosol liquid droplets delivered on actuation of the inhaler have a particle size comprised between 0.5 μm and 2.5 μm, with a mass median aerodynamic diameter of about 1-2 μm and wherein the fine particle fraction is at least 30%.
摘要翻译： 本发明公开了一种气溶胶药物组合物，其包含在氢氟烷烃推进剂和一种或多种共溶剂的混合物中的溶液中的药物，其中在致动吸入器时输送的气溶胶液滴的粒径为0.5μm和2.5μm之间， 大约1-2μm的质量中值空气动力学直径，并且其中细颗粒分数为至少30％。
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公开(公告)号：US07740463B2
公开(公告)日：2010-06-22
申请号：US10612072
申请日：2003-07-03
申请人： David Lewis , David Ganderton , Brian Meakin , Paolo Ventura , Gaetano Brambilla , Raffaella Garzia
发明人： David Lewis , David Ganderton , Brian Meakin , Paolo Ventura , Gaetano Brambilla , Raffaella Garzia
CPC分类号： A61K9/008 , A61K9/12 , A61M15/009 , Y10S514/958
摘要： The invention relates to the use of pressurised metered dose inhalers (MDIs) having part or all of their internal surfaces consisting of stainless steel, anodised aluminium or lined with an inert organic coating; and to compositions to be delivered with said MDIs.
摘要翻译： 本发明涉及使用加压计量吸入器（MDI），其具有由不锈钢，阳极氧化铝或惰性有机涂层衬里组成的部分或全部内表面; 以及与所述MDI一起递送的组合物。
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公开(公告)号：US20080115782A1
公开(公告)日：2008-05-22
申请号：US12023315
申请日：2008-01-31
申请人： David LEWIS , David Ganderton , Brian Meakin , Paolo Ventura , Gaetano Brambilla , Raffaella Garzia
发明人： David LEWIS , David Ganderton , Brian Meakin , Paolo Ventura , Gaetano Brambilla , Raffaella Garzia
IPC分类号： A61M11/00
CPC分类号： A61K9/008 , A61K9/12 , A61M15/009 , Y10S514/958
摘要： The invention relates to pressurized metered dose inhalers (MDIs) in which all or part of the internal surface is stainless steel, anodized aluminum, or lined with an inert organic coating and which contain a formulation which comprises ipratropium bromide.
摘要翻译： 本发明涉及加压计量吸入器（MDI），其中内表面的全部或部分是不锈钢，阳极氧化铝或用惰性有机涂层衬里，并含有包含异丙托溴铵的制剂。
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