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1. 发明申请

US20070122353A1 Drug condensation aerosols and kits 审中-公开
标题翻译：药物冷凝气溶胶和试剂盒
公开(公告)号：US20070122353A1
公开(公告)日：2007-05-31
申请号：US11504419
申请日：2006-08-15
申请人： Ron Hale , Craig Hodges , Peter Lloyd , Amy Lu , Daniel Myers , Joshua Rabinowitz , Martin Wensley , Jeffrey McKinney , Alejandro Zaffaroni
发明人： Ron Hale , Craig Hodges , Peter Lloyd , Amy Lu , Daniel Myers , Joshua Rabinowitz , Martin Wensley , Jeffrey McKinney , Alejandro Zaffaroni
IPC分类号： A61K9/14
CPC分类号： A61K9/0004 , A61K9/007 , A61K9/0078 , A61K9/12 , A61K31/4468 , A61K31/519 , A61K31/5415 , A61K31/5517 , A61K31/553 , A61M11/002 , A61M11/005 , A61M11/04 , A61M11/041 , A61M11/042 , A61M11/047 , A61M15/00 , A61M2207/00
摘要： The present invention provides novel condensation aerosols for the treatment of disease and/or intermittent or acute conditions. These condensation aerosols have little or no pyrolysis degradation products and are characterized by having an MMAD of between 1-3 microns. These aerosols are made by rapidly heating a substrate coated with a thin film of drug having a thickness of between 0.05 and 20 μm, while passing a gas over the film, to form particles of a desirable particle size for inhalation. Kits comprising a drug and a device for producing a condensation aerosol are also provided The device contained in the kit typically, has an element for heating the drug which is coated as a film on the substrate and contains a therapeutically effective dose of a drug when the drug is administered in aerosol form, and an element allowing the vapor to cool to form an aerosol. Also disclosed, are methods for using these aerosols and kits.
摘要翻译：本发明提供用于治疗疾病和/或间歇或急性病症的新型凝结气溶胶。这些凝结气溶胶几乎没有或没有热解降解产物，其特征在于MMAD为1-3微米。这些气溶胶是通过在使薄膜上的气体通过膜的同时，快速加热涂覆有厚度为0.05至20μm的药物的薄膜的基材，以形成用于吸入的理想颗粒尺寸的颗粒。还提供了包含药物和用于产生冷凝气雾剂的装置的试剂盒。典型地，试剂盒中所含的装置具有用于加热药物的元件，其在基底上以薄膜形式包被，并含有治疗有效剂量的药物药物以气溶胶形式施用，并且允许蒸气冷却以形成气溶胶的元素。还公开了使用这些气溶胶和试剂盒的方法。

2. 发明申请

US20070031340A1 Thin-film drug delivery article and method of use 有权
标题翻译：薄膜给药制品及使用方法
公开(公告)号：US20070031340A1
公开(公告)日：2007-02-08
申请号：US10633877
申请日：2003-08-04
申请人： Ron Hale , Amy Lu , Daniel Myers , Joshua Rabinowitz , Martin Wensley
发明人： Ron Hale , Amy Lu , Daniel Myers , Joshua Rabinowitz , Martin Wensley
IPC分类号： A61L9/04 , A61K9/14
CPC分类号： A61K9/7007 , A61K9/007 , Y10S514/958
摘要： An article for use in an aerosol device, for producing an aerosol of a drug composition is disclosed. The article includes a heat-conductive substrate having a surface with a selected surface area, and a drug composition film on the substrate surface having a selected film thickness of between 0.05 and 20 μm. The film thickness is such that an aerosol formed by vaporizing the drug composition by heating the substrate and condensing the vaporized compound contains 10% or less drug-degradation product and at least 50% of the total amount of drug composition contained in the film. The selected substrate surface area is such as to yield an effective human therapeutic dose of the drug aerosol. Also disclosed are methods of making and using the article.
摘要翻译：公开了一种用于产生药物组合物气溶胶的气溶胶装置的制品。所述制品包括具有选择的表面积的表面的导热基材和在所述基材表面上的具有0.05至20μm的选定膜厚度的药物组合物膜。膜厚度使得通过加热基底并冷凝汽化的化合物使药物组合物蒸发而形成的气溶胶含有10％以下的药物降解产物和膜中所含的药物组合物总量的至少50％。所选择的底物表面积是产生有效的人类治疗剂量的药物气溶胶。还公开了制造和使用制品的方法。

3. 发明申请

US20070028916A1 Rapid-heating drug delivery article and method of use 有权
标题翻译：快速加热药物输送物品及其使用方法
公开(公告)号：US20070028916A1
公开(公告)日：2007-02-08
申请号：US10633876
申请日：2003-08-04
申请人： Ron Hale , Peter Lloyd , Amy Lu , Daniel Myers , Reynaldo Quintana , Joshua Rabinowitz , Dennis Solas , Soonho Song , Curtis Tom , Martin Wensley
发明人： Ron Hale , Peter Lloyd , Amy Lu , Daniel Myers , Reynaldo Quintana , Joshua Rabinowitz , Dennis Solas , Soonho Song , Curtis Tom , Martin Wensley
IPC分类号： A61M11/00
CPC分类号： A61M11/041 , A61K9/007 , A61K9/0073 , A61M11/042 , A61M11/047 , A61M15/002 , A61M15/0028 , A61M2016/0039 , A61M2205/3606 , A61M2205/3653 , A61M2205/368 , A61M2205/50 , B05B7/1686 , B05B17/04 , Y10S514/958
摘要： A device, method, and system for producing a condensation aerosol are disclosed. The device includes a chamber having an upstream opening and a downstream opening which allow gas to flow through the chamber, and a heat-conductive substrate located at a position between the upstream and downstream openings. Formed on the substrate is a drug composition film containing a therapeutically effective dose of a drug when the drug is administered in aerosol form. A heat source in the device is operable to supply heat to the substrate to produce a substrate temperature greater than 300° C., and to substantially volatilize the drug composition film from the substrate in a period of 2 seconds or less. The device produces an aerosol containing less than about 10% by weight drug composition degradation products and at least 50% of the drug composition of said film.
摘要翻译：公开了一种用于生产冷凝气雾剂的装置，方法和系统。该装置包括具有允许气体流过腔室的上游开口和下游开口的腔室，以及位于上游和下游开口之间位置的导热基底。在基质上形成药物组合物膜，当药物以气溶胶形式施用时，其含有治疗有效剂量的药物。装置中的热源可操作以向衬底供应热量以产生大于300℃的衬底温度，并且在2秒或更短的时间内使药物组合物膜从衬底基本挥发。该装置产生含有小于约10重量％的药物组合物降解产物和所述膜的药物组合物的至少50％的气溶胶。

4. 发明申请

US20070286816A1 Drug and excipient aerosol compositions 审中-公开
标题翻译：药物和赋形剂气溶胶组合物
公开(公告)号：US20070286816A1
公开(公告)日：2007-12-13
申请号：US11744799
申请日：2007-05-04
申请人： Ron Hale , Joshua Rabinowitz , Daniel Myers , Amy Lu , Alejandro Zaffaroni
发明人： Ron Hale , Joshua Rabinowitz , Daniel Myers , Amy Lu , Alejandro Zaffaroni
IPC分类号： A61K9/12
CPC分类号： A61K9/0004 , A61K9/007 , A61K9/0078 , A61K9/12 , A61K31/4468 , A61K31/519 , A61K31/5415 , A61K31/5517 , A61K31/553 , A61M11/002 , A61M11/005 , A61M11/04 , A61M11/041 , A61M11/042 , A61M11/047 , A61M15/00 , A61M2207/00
摘要： The present invention provides novel condensation aerosols for the treatment of disease and/or intermittent or acute conditions. These condensation aerosols have little or no pyrolysis degradation products and are characterized by having an MMAD of between 1-3 microns. These aerosols are made by rapidly heating a substrate coated with a thin film of drug having a thickness of between 0.05 and 20 μm, while passing a gas over the film, to form particles of a desirable particle size for inhalation. Kits comprising a drug and a device for producing a condensation aerosol are also provided. The device contained in the kit typically, has an element for heating the drug which is coated as a film on the substrate and contains a therapeutically effective dose of a drug when the drug is administered in aerosol form, and an element allowing the vapor to cool to form an aerosol. Also disclosed, are methods for using these aerosols and kits.
摘要翻译：本发明提供用于治疗疾病和/或间歇或急性病症的新型凝结气溶胶。这些凝结气溶胶几乎没有或没有热解降解产物，其特征在于MMAD为1-3微米。这些气溶胶是通过在使薄膜上的气体通过膜的同时，快速加热涂覆有厚度为0.05至20μm的药物的薄膜的基材，以形成用于吸入的理想颗粒尺寸的颗粒。还提供了包含药物和用于产生冷凝气溶胶的装置的试剂盒。包含在试剂盒中的装置通常具有用于加热药物的元件，其作为膜被涂覆在基底上并且当药物以气溶胶形式施用时含有治疗有效剂量的药物，以及允许蒸气冷却的元件以形成气溶胶。还公开了使用这些气溶胶和试剂盒的方法。

5. 发明申请

US20050037506A1 Methods of determining film thicknesses for an aerosol delivery article 审中-公开
标题翻译：确定气溶胶输送制品的膜厚度的方法
公开(公告)号：US20050037506A1
公开(公告)日：2005-02-17
申请号：US10912462
申请日：2004-08-04
申请人： Ron Hale , Amy Lu , Daniel Myers , Joshua Rabinowitz
发明人： Ron Hale , Amy Lu , Daniel Myers , Joshua Rabinowitz
IPC分类号： A61K9/00 , A61K31/00 , A61M15/00 , G01N1/18
CPC分类号： A61K9/007 , A61K9/0073 , A61K31/00 , A61M11/001 , A61M15/0028 , A61M2205/3653 , A61M2209/02
摘要： Methods for determining the film thickness of a compound composition needed to provide a selected purity and yield of a condensation aerosol via vaporization of the compound composition have applications in aerosol delivery technology, in pulmonary drug delivery, and in other therapeutic treatment regimes. The methods for determining such film thickness, for use in a device having a film of drug composition to be aerosolized, include generating purities and yields of a drug composition by vaporizing films of the drug composition from substrates at two or more temperatures in the range of 150° C. to 500° C. and two or more film thickness in the range of 0.05 to 50 microns, determining from these yields and purities if a thickness and temperature exist where the aerosol has at least 90% purity and at least 50% yield, and repeated such measurements until the selected purity and yield requirement are met.
摘要翻译：用于确定通过化合物组合物蒸发提供选择的纯度和产生缩合气溶胶所需的化合物组合物的膜厚度的方法可用于气雾剂递送技术，肺部药物递送和其它治疗方案中。用于确定具有待雾化的药物组合物的膜的装置中的这种膜厚度的方法包括通过在两个或多个温度范围内从基材中蒸发药物组合物的膜而产生药物组合物的纯度和产率 150℃至500℃，以及0.05至50微米范围内的两个或多个膜厚度，如果存在厚度和温度，则气溶胶具有至少90％的纯度和至少50％的纯度，产量和重复这样的测量，直到满足所选择的纯度和产量要求。

6. 发明申请

US20050034723A1 Substrates for drug delivery device and methods of preparing and use 审中-公开
标题翻译：用于药物输送装置的基材及其制备和使用方法
公开(公告)号：US20050034723A1
公开(公告)日：2005-02-17
申请号：US10912417
申请日：2004-08-04
申请人： Bryson Bennett , Ron Hale , Amy Lu , Daniel Myers , Krishnamohan Sharma , Joshua Rabinowitz
发明人： Bryson Bennett , Ron Hale , Amy Lu , Daniel Myers , Krishnamohan Sharma , Joshua Rabinowitz
IPC分类号： A61K9/00 , A61M11/04 , A61M11/00 , A61M15/00
CPC分类号： A61K31/553 , A61K9/00 , A61K9/007 , A61K9/0073 , A61M11/001 , A61M11/041 , A61M11/042 , A61M11/047
摘要： An assembly and method for producing a condensation aerosol are disclosed. The assembly includes a heat-conductive metal substrate with an oxidation resistant exterior surface and a drug composition film on the exterior surface and is for use in an aerosol device. The thickness of the film and the surface of the substrate is such that the aerosol formed by vaporizing and condensing the drug composition the aerosol contain 10% by weight or less drug-degradation products and at least 50% of the total amount of the drug composition in the film. The methods for treating the exterior surface include heat and chemical treatment and formation of a protective overcoat.
摘要翻译：公开了一种用于生产冷凝气雾剂的组件和方法。组件包括具有耐氧化外表面的导热金属基底和外表面上的药物组合物膜，并用于气溶胶装置。膜的厚度和基材的表面使得通过气溶剂和冷凝药物组合物形成的气溶胶含有10重量％以下的药物降解产物和药物组合物总量的至少50％在电影里。用于处理外表面的方法包括加热和化学处理以及形成保护性外涂层。

7. 发明申请

US20060193788A1 Acute treatment of headache with phenothiazine antipsychotics 审中-公开
标题翻译：用吩噻嗪抗精神病药物急性治疗头痛
公开(公告)号：US20060193788A1
公开(公告)日：2006-08-31
申请号：US11346548
申请日：2006-02-02
申请人： Ron Hale , Peter Lloyd , Amy Lu , Patrik Munzar , Joshua Rabinowitz , Roman Skowronski
发明人： Ron Hale , Peter Lloyd , Amy Lu , Patrik Munzar , Joshua Rabinowitz , Roman Skowronski
IPC分类号： A61K9/14 , A61L9/04
CPC分类号： A61K31/553 , A61K9/007 , A61K9/0073 , A61K31/382 , A61K31/4439 , A61K31/445 , A61K31/4515 , A61K31/454 , A61K31/496 , A61K31/519 , A61K31/5377 , A61K31/5415 , A61K31/55 , A61K31/551 , A61K31/554 , A61M15/00 , A61M15/0028 , A61M15/0033 , A61M2202/064 , A61M2205/075
摘要： Methods of treating headache with antipsychotics are provided. A kit for treating headache is also provided, comprising an antipsychotic and a device for rapid delivery of the antipsychotic.
摘要翻译：提供了使用抗精神病药治疗头痛的方法。还提供了用于治疗头痛的试剂盒，其包含抗精神病药和用于快速递送抗精神病药的装置。

8. 发明申请

US20070140982A1 Diuretic Aerosols and Methods of Making and Using Them 有权
标题翻译：利尿剂及其使用方法
公开(公告)号：US20070140982A1
公开(公告)日：2007-06-21
申请号：US11670892
申请日：2007-02-02
申请人： Nathan Every , Ron Hale , Amy Lu , Joshua Rabinowitz
发明人： Nathan Every , Ron Hale , Amy Lu , Joshua Rabinowitz
IPC分类号： A61K9/14
CPC分类号： A61K9/0073 , A61K9/007 , A61K31/58
摘要： Described herein are diuretic condensation aerosols and methods of making and using them. Kits for delivering a condensation aerosol are also described. The diuretic aerosols typically comprise diuretic condensation aerosol particles that comprise a diuretic compound. In some variations the diuretic compound is selected from the group consisting of bumetanide, ethacrynic acid, furosemide, muzolimine, spironolactone, torsemide, triamterene, tripamide, BG 9928, and BG 9719. Methods of treating edema using the described aerosols are also provided. In general, the methods typically comprise the step of administering a therapeutically effective amount of diuretic condensation aerosol to a person with edema. The diuretic condensation aerosol may be administered in a single inhalation, or may be administered in more than one inhalation. Methods of forming a diuretic condensation aerosol are also described. The methods typically comprise the steps of providing a diuretic composition, vaporizing the composition to form a vapor, and then condensing the diuretic composition vapor.
摘要翻译：本文描述的是利尿凝结气溶胶及其制备和使用方法。还描述了用于递送冷凝气雾剂的组件。利尿剂气溶胶通常包含利尿剂缩合气溶胶颗粒，其包含利尿剂。在一些变体中，利尿剂化合物选自布美他尼，依西醋酸，呋塞米，多佐立胺，螺内酯，托塞米明，扑热息痛，三酰胺，BG 9928和BG 9719.还提供了使用所述气溶胶治疗水肿的方法。通常，所述方法通常包括向具有水肿的人施用治疗有效量的利尿冷凝气雾剂的步骤。利尿冷凝气雾剂可以在单次吸入中施用，或者可以在多于一次的吸入中施用。还描述了形成利尿冷凝气雾剂的方法。所述方法通常包括提供利尿组合物，蒸发组合物以形成蒸气，然后冷凝利尿组合物蒸气的步骤。

9. 发明申请

US20110240014A1 SUBSTRATES FOR DRUG DELIVERY DEVICE AND METHODS OF PREPARING AND USE 审中-公开
标题翻译：用于药物递送装置的基质及其制备和使用方法
公开(公告)号：US20110240014A1
公开(公告)日：2011-10-06
申请号：US13078668
申请日：2011-04-01
申请人： Bryson Bennett , Ron L. Hale , Amy Lu , Daniel J. Myers , Krishnamohan Sharma , Joshua D. Rabinowitz
发明人： Bryson Bennett , Ron L. Hale , Amy Lu , Daniel J. Myers , Krishnamohan Sharma , Joshua D. Rabinowitz
IPC分类号： A61M11/00
CPC分类号： A61K31/553 , A61K9/00 , A61K9/007 , A61K9/0073 , A61M11/001 , A61M11/041 , A61M11/042 , A61M11/047
摘要： An assembly and method for producing a condensation aerosol are disclosed. The assembly includes a heat-conductive metal substrate with an oxidation resistant exterior surface and a drug composition film on the exterior surface and is for use in an aerosol device. The thickness of the film and the surface of the substrate is such that the aerosol formed by vaporizing and condensing the drug composition the aerosol contain 10% by weight or less drug-degradation products and at least 50% of the total amount of the drug composition in the film. The methods for treating the exterior surface include heat and chemical treatment and formation of a protective overcoat.
摘要翻译：公开了一种用于生产冷凝气雾剂的组件和方法。组件包括具有耐氧化外表面的导热金属基底和外表面上的药物组合物膜，并用于气溶胶装置。膜的厚度和基材的表面使得通过气溶剂和冷凝药物组合物形成的气溶胶含有10重量％以下的药物降解产物和药物组合物总量的至少50％在电影里。用于处理外表面的方法包括加热和化学处理以及形成保护性外涂层。

10. 发明授权

US5607691A Compositions and methods for enhanced drug delivery 失效
标题翻译：用于增强药物递送的组合物和方法
公开(公告)号：US5607691A
公开(公告)日：1997-03-04
申请号：US449188
申请日：1995-05-24
申请人： Ron L. Hale , Amy Lu , Dennis Solas , Harold E. Selick , Kevin R. Oldenburg , Alejandro C. Zaffaroni
发明人： Ron L. Hale , Amy Lu , Dennis Solas , Harold E. Selick , Kevin R. Oldenburg , Alejandro C. Zaffaroni
IPC分类号： A61K9/00 , A61K9/127 , A61K47/48 , A61K9/70 , A61K31/00
CPC分类号： A61K31/70 , A61K31/568 , A61K47/4803 , A61K47/48992 , A61K9/0009 , A61K9/1272
摘要： The present invention relates to methods of delivering pharmaceutical agents across membranes, including the skin layer or mucosal membranes of a patient. A pharmaceutical agent is covalently bonded to a chemical modifier, via a physiologically cleavable bond, such that the membrane transport and delivery of the agent is enhanced.
摘要翻译：本发明涉及通过膜（包括患者的皮肤层或粘膜）递送药剂的方法。药剂通过生理上可切割的键共价结合到化学改性剂上，使得药物的膜输送和递送得到增强。

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