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11.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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12.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：US20060120966A1
公开(公告)日：2006-06-08
申请号：US10531867
申请日：2003-06-18
申请人： Tanya Church , David Lewis , David Ganderton , Brian Meakin , Gaetano Brambilla
发明人： Tanya Church , David Lewis , David Ganderton , Brian Meakin , Gaetano Brambilla
IPC分类号： A61L9/04 , A61K31/573 , A61K31/4745 , A61K31/46 , A61M11/00
CPC分类号： A61K9/008 , A61K31/4704 , A61K31/485 , A61K45/06 , A61K2300/00
摘要： The present invention relates to a pharmaceutical formulation for use in the administration of a long-acting β2-agonist by inhalation. In particular this invention relates to a chemically stable, highly efficient salmeterol HFA solution formulation to be administered by pressurised metered dose inhalers (pMDIs) characterized by a deep lung penetration. The invention also relates to methods for the preparation of said formulation and to its use in respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD).
摘要翻译： 本发明涉及用于通过吸入施用长效β2激动剂的药物制剂。 特别地，本发明涉及一种化学稳定，高效的沙美特罗HFA溶液制剂，其由以深肺渗透为特征的加压计量剂量吸入器（pMDI）施用。 本发明还涉及制备所述制剂及其在呼吸系统疾病如哮喘和慢性阻塞性肺疾病（COPD）中的应用的方法。
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公开(公告)号：US20050152846A1
公开(公告)日：2005-07-14
申请号：US10504151
申请日：2003-02-26
申请人： Rebecca Davies , David Ganderton , David Lewis , Brian Meakin , Tanya Church , Gaetano Brambilla , Alessandra Ferraris
发明人： Rebecca Davies , David Ganderton , David Lewis , Brian Meakin , Tanya Church , Gaetano Brambilla , Alessandra Ferraris
IPC分类号： A61K9/12 , A61K9/00 , A61K9/72 , A61K31/00 , A61K31/167 , A61K31/4704 , A61K31/485 , A61K45/06 , A61K47/06 , A61K47/10 , A61P11/00 , A61P11/06 , A61P11/08 , A61P11/16 , A61P43/00 , C07D215/26 , A61L9/04 , A61K9/14 , A61K31/205
摘要： The present invention relates to a pharmaceutical formulation for use in the administration of a long-acting β2-agonist by inhalation. In particular this invention relates to a chemically stable highly efficient formoterol HFA solution formulation to be administered by pressurised metered dose inhalers (pMDIs) characterized by a deep lung penetration. The invention also relates to methods for the preparation of said formulation and to its use in respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD).
摘要翻译： 本发明涉及用于通过吸入施用长效β2激动剂的药物制剂。 特别地，本发明涉及一种化学稳定的高效福莫特罗HFA溶液制剂，其由以深层肺穿透为特征的加压计量剂量吸入器（pMDI）施用。 本发明还涉及制备所述制剂及其在呼吸系统疾病如哮喘和慢性阻塞性肺疾病（COPD）中的应用的方法。
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15.发明申请Aerosol formulations containing esters of 3,17-dihydroxy oestratriene derivatives for pulmonary delivery 审中-公开含有3,17-二羟基雌三烯衍生物的酯用于肺部输送的气溶胶制剂公开(公告)号：US20050209207A1
公开(公告)日：2005-09-22
申请号：US10504841
申请日：2003-02-24
申请人： Reecca Davies , David Ganderton , David Lewis , Brian Meakin , Gaetano Brambilla , Alessandra Ferraris
发明人： Reecca Davies , David Ganderton , David Lewis , Brian Meakin , Gaetano Brambilla , Alessandra Ferraris
IPC分类号： A61K9/00 , A61K9/12 , A61K9/72 , A61K31/565 , A61K31/566 , A61K31/567 , A61K47/10 , A61P5/30 , A61L9/04 , A61K31/56
CPC分类号： A61K9/008 , A61K31/565 , A61K47/10
摘要： The invention discloses formulations for administration with pressurized metered dose inhalers containing as active ingredient esters of 3,17-dihydroxy oestratriene derivatives, in solution in a hydrofluorocarbon propellant, optionally one or more co-solvents, and their use for the treatment of postmenopausal symptoms as well as of menstrual migraine headaches.
摘要翻译： 本发明公开了用于给予含有3,17-二羟基雌三烯衍生物的活性成分的加压计量吸入器的制剂，在氢氟烃推进剂的溶液中，任选的一种或多种共溶剂，以及它们用于治疗绝经后症状的用途 以及月经偏头痛。
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16.发明申请公开(公告)号：US20050154013A1
公开(公告)日：2005-07-14
申请号：US10505861
申请日：2003-02-27
申请人： Rebecca Davies , David Ganderton , David Lewis , Brian Meakin , Tanya Church , Gaetano Brambilla , Alessandra Ferraris
发明人： Rebecca Davies , David Ganderton , David Lewis , Brian Meakin , Tanya Church , Gaetano Brambilla , Alessandra Ferraris
IPC分类号： A61K9/12 , A61K9/00 , A61K9/72 , A61K31/00 , A61K31/167 , A61K31/4704 , A61K31/485 , A61K45/06 , A61K47/06 , A61K47/10 , A61P11/00 , A61P11/06 , A61P11/08 , A61P11/16 , A61P43/00 , C07D215/26 , A61K31/4706 , A61L9/04
摘要： The present invention relates to a pharmaceutical formulation for use in the administration of 2(1H)-quinolinone derivatives long-acting β2-agonists by inhalation. In particular this invention relates to a chemically stable highly efficient TA 2005 HFA solution formulation to be administered by pressurised metered dose inhalers (pMDIs) characterized by a deep lung penetration. The invention also relates to methods for the preparation of said formulation and to its use in respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD).
摘要翻译： 本发明涉及用于通过吸入给药2（1H） - 喹啉酮衍生物长效β2 - 激动剂的药物制剂。 特别地，本发明涉及一种化学稳定高效的TA 2005 HFA溶液制剂，其通过深层肺穿透特征的加压计量剂量吸入器（pMDI）来施用。 本发明还涉及制备所述制剂及其在呼吸系统疾病如哮喘和慢性阻塞性肺疾病（COPD）中的应用的方法。
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17.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：US06716414B2
公开(公告)日：2004-04-06
申请号：US09860689
申请日：2001-05-21
IPC分类号： A61K912
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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18.发明授权Formulations containing an anticholinergic drug for the treatment of chronic obstructive pulmonary disease 失效含有用于治疗慢性阻塞性肺疾病的抗胆碱能药物的制剂公开(公告)号：US06964759B2
公开(公告)日：2005-11-15
申请号：US10204307
申请日：2001-02-19
CPC分类号： A61K9/008 , A61K31/439 , Y10S514/826
摘要： Formulations for the administration through pressurized metered dose aerosol inhalers containing an anticholineric drug in solution in a hydrofluorocarbon propellant, a cosolvent and a low volatility component, and the use thereof in chronic obstructive pulmonary disease.
摘要翻译： 通过在氢氟烃推进剂，共溶剂和低挥发性组分的溶液中含有抗胆碱药物的加压计量剂量气溶胶吸入器及其在慢性阻塞性肺疾病中的用途来施用的制剂。
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19.发明申请公开(公告)号：US20060257324A1
公开(公告)日：2006-11-16
申请号：US11408026
申请日：2006-04-21
申请人： David Lewis , Brian Meakin , Gaetano Brambilla
发明人： David Lewis , Brian Meakin , Gaetano Brambilla
IPC分类号： A61L9/04 , A61K31/573 , A61K31/4745 , A61K31/138
CPC分类号： A61K9/008 , A61K9/124 , A61K31/138 , A61K31/167 , A61K31/4704 , A61K31/4745 , A61K31/57 , A61K31/573 , A61K31/58 , A61K45/06 , A61K47/10 , A61K2300/00
摘要： A method for delivering two or more active drug substances to the lungs by inhalation from a single pressurized metered dose inhaler product, said inhaler containing a HFA/cosolvent based solution formulation wherein all the active drug substances are fully dissolved in the formulation.
摘要翻译： 一种通过从单个加压计量吸入器产品吸入将两种或更多种活性药物物质递送至肺的方法，所述吸入器含有基于HFA /助溶剂的溶液制剂，其中所有活性药物物质完全溶解于制剂中。
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20.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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