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1. 发明申请

WO2017042696A1 TARGETED DELIVERY OF SPRAY-DRIED FORMULATIONS TO THE LUNGS 审中-公开
标题翻译：有针对性地提供喷雾干燥配方
公开(公告)号：WO2017042696A1
公开(公告)日：2017-03-16
申请号：PCT/IB2016/055331
申请日：2016-09-07
申请人： NOVARTIS AG , UNG, Keith Try , WEERS, Jeffry , HUANG, Daniel , RAO, Nagaraja , SON, Yoen-Ju
发明人： UNG, Keith Try , WEERS, Jeffry , HUANG, Daniel , RAO, Nagaraja , SON, Yoen-Ju
IPC分类号： A61K9/00 , A61K9/16 , A61K38/00 , A61K39/00
CPC分类号： A61K9/0075 , A61K9/1688 , A61K38/2221 , A61K39/0011 , A61K2039/5158 , A61K2039/55522
摘要： Disclosed are inhalation formulations of dry powders comprising particles and processes which yield particles to effectively bypass unwanted deposition in the mouth and throat. Embodiments of the invention are characterized by an inertial parameter which provide an in vitro total lung dose of greater than 80% of a nominal dose. Embodiments of formulations include neat formulations containing active agent only; formulations of active agent and buffer; and formulations comprising active agent, a glass-forming, and/or a shell-forming excipient. Also provided are methods for making the dry powder formulations. The powder formulations are useful for the treatment of diseases and conditions especially respiratory diseases and conditions.
摘要翻译：公开了包含颗粒的干燥粉末的吸入制剂，其产生颗粒以有效地绕过口腔和喉部中的不希望的沉积。本发明的实施方案的特征在于惯性参数，其提供大于标称剂量的80％的体外总肺剂量。制剂的实施方案包括仅含活性成分的纯制剂; 活性剂和缓冲剂的配方; 和包含活性剂，成形玻璃和/或成壳赋形剂的制剂。还提供了制备干粉配方的方法。粉末制剂可用于治疗疾病和病症，特别是呼吸道疾病和病症。

2. 发明申请

WO2015145353A1 SPRAY-DRIED SOLID-IN-OIL-IN-WATER DISPERSIONS FOR INHALATION OF ACTIVE PHARMACEUTICAL INGREDIENTS 审中-公开
标题翻译：用于吸入活性药物成分的喷雾干燥的水中固体分散体
公开(公告)号：WO2015145353A1
公开(公告)日：2015-10-01
申请号：PCT/IB2015/052151
申请日：2015-03-24
申请人： NOVARTIS AG , HUANG, Daniel , RAO, Nagaraja , TAN, Trixie , MILLER, Danforth , WEERS, Jeffry
发明人： HUANG, Daniel , RAO, Nagaraja , TAN, Trixie , MILLER, Danforth , WEERS, Jeffry
IPC分类号： A61K9/00
CPC分类号： A61K9/5089 , A61K9/0075 , A61K9/5015 , A61K31/365 , A61K31/436 , A61K31/4704 , A61K38/13 , A61K45/06 , B01J2/04
摘要： Embodiments of the invention relate to particulate agents and compositions comprising particulate agents for inhalation, and methods for preparing such particulate agents and compositions for inhalation, as well as therapeutic methods. Embodiments of the method comprise preparing an emulsion by combining an oil phase dispersion of hydrophobic seed particles and an aqueous dispersion comprising an emulsifier and an emulsion stabilizer and preparing a feedstock comprising encapsulated particles by homogenizing the emulsion, and forming a plurality of coated particles by spray drying the feedstock, wherein resulting particles comprises a porous shell disposed on or over a core and the core comprises at least one hydrophobic seed particle.
摘要翻译：本发明的实施方案涉及包含用于吸入的颗粒剂的颗粒剂和组合物，以及用于制备这种颗粒剂和用于吸入的组合物的方法以及治疗方法。该方法的实施方案包括通过将疏水种子颗粒的油相分散体和包含乳化剂和乳液稳定剂的水性分散体组合制备乳液，并通过均化乳液制备包含包封颗粒的原料，并通过喷雾形成多个涂覆颗粒干燥原料，其中所得颗粒包括设置在芯上或其上的多孔壳，并且芯包含至少一个疏水种子颗粒。

3. 发明申请

WO2014141069A1 DEAMORPHIZATION OF SPRAY-DRIED FORMULATIONS VIA SPRAY-BLENDING 审中-公开
标题翻译：通过喷雾混合去除喷雾干燥配方
公开(公告)号：WO2014141069A1
公开(公告)日：2014-09-18
申请号：PCT/IB2014/059632
申请日：2014-03-11
申请人： NOVARTIS AG , WEERS, Jeffry , HUANG, Daniel , TARARA, Thomas , MILLER, Danforth
发明人： WEERS, Jeffry , HUANG, Daniel , TARARA, Thomas , MILLER, Danforth
IPC分类号： A61K9/00 , A61K9/16 , A61K31/00
CPC分类号： A61K9/0075 , A61K9/1617 , A61K9/1694 , A61K31/40 , A61K31/4704 , A61K31/573 , A61K31/58 , A61M15/0045 , A61M2202/064 , A61K2300/00
摘要： Dry powder formulations for inhalation and their use in the treatment diseases and conditions. The formulation contains a uniform blend of a first spray-dried powder and a second spray-dried powder. The first spray-dried powder contains spray-dried particles of a therapeutically active ingredient dispersed in a pharmaceutically acceptable hydrophobic excipient. The second spray-dried powder contains spray-dried particles formed from a pharmaceutically acceptable hydrophobic excipient but are substantially free of any therapeutically active ingredient. The active ingredient in the first spray-dried powder is loaded sufficiently high to compensate for the second spray-dried powder being substantially free of any active ingredient. A process for preparing such formulations is also described.
摘要翻译：用于吸入的干粉配方及其用于治疗疾病和病症。该制剂含有第一喷雾干燥粉末和第二喷雾干燥粉末的均匀混合物。第一喷雾干燥的粉末包含分散在药学上可接受的疏水性赋形剂中的治疗活性成分的喷雾干燥颗粒。第二喷雾干燥粉末含有由药学上可接受的疏水性赋形剂形成的喷雾干燥颗粒，但基本上不含任何治疗活性成分。第一喷雾干燥粉末中的活性成分被充分地加载以补偿基本上没有任何活性成分的第二喷雾干燥粉末。还描述了制备这种制剂的方法。

4. 发明申请

WO2012106575A1 DRY POWDER FORMULATIONS OF PARTICLES THAT CONTAIN TWO OR MORE ACTIVE INGREDIENTS FOR TREATING OBSTRUCTIVE OR INFLAMMATORY AIRWAYS DISEASES 审中-公开
标题翻译：含有两种或更多活性成分的颗粒的干粉配方用于治疗阻塞性或炎症性气道疾病
公开(公告)号：WO2012106575A1
公开(公告)日：2012-08-09
申请号：PCT/US2012/023727
申请日：2012-02-03
申请人： NOVARTIS AG , WEERS, Jeffry
发明人： WEERS, Jeffry
IPC分类号： A61K9/14 , A61K9/00 , A61P11/00
CPC分类号： A61K9/50 , A61K9/0075 , A61K9/1611 , A61K9/1617 , A61K9/1623 , A61K9/501 , A61K9/5015 , A61K31/40 , A61K31/4704 , A61K31/56 , A61K31/58 , A61K45/06 , A61M15/00
摘要： Dry powder formulations for inhalation comprising spray-dried particles and their use in the treatment of an obstructive or inflammatory airways disease. Each particle has a core of a first active ingredient in substantially crystalline form that is coated with a layer of a second active ingredient in substantially amorphous form that is dispersed in a pharmaceutically acceptable hydrophobic excipient. A process for preparing such formulations is also described.
摘要翻译：用于吸入的干粉制剂包括喷雾干燥颗粒及其用于治疗阻塞性或炎性气道疾病的用途。每个颗粒具有基本上结晶形式的第一活性成分的核心，其以基本上无定形形式的第二活性成分层涂覆，所述第二活性成分分散在药学上可接受的疏水性赋形剂中。还描述了制备这种制剂的方法。

5. 发明申请

WO2013090841A2 AEROSOLIZATION APPARATUS FOR INHALATION PROFILE-INDEPENDENT DRUG DELIVERY 审中-公开
标题翻译：用于吸入型独立药物递送的放射化装置
公开(公告)号：WO2013090841A2
公开(公告)日：2013-06-20
申请号：PCT/US2012/069938
申请日：2012-12-14
申请人： NOVARTIS AG , CHAN, Leo , UNG, Try Keith , WEERS, Jeffry
发明人： CHAN, Leo , UNG, Try Keith , WEERS, Jeffry
IPC分类号： A61M15/00
CPC分类号： A61M15/0035 , A61K31/66 , A61M11/001 , A61M15/0021 , A61M15/0028 , A61M15/0041 , A61M15/0045 , A61M15/0093 , A61M2202/064
摘要： A powder aerosolization apparatus comprises a housing comprising an outlet adapted to be inserted into a user's mouth and one or more bypass air openings. A receptacle support within the housing supports a receptacle containing a powder pharmaceutical formulation. A puncturing mechanism within the housing creates in the receptacle one or more inlet openings and one or more powder outflow openings, wherein the powder outflow openings have a total area of from 0.2 mm 2 to 4.0 mm 2 . Upon a user's inhalation through the outlet, air flows through the one or more bypass air openings and through the receptacle to aerosolize the powder pharmaceutical formulation in the receptacle. In one version, the relative flow parameters between the flow through the one or more bypass openings and the one or more powder outflow openings are selected so that flow of aerosolized pharmaceutical formulation does not occur until a predetermined inhalation flow rate is achieved.
摘要翻译：粉末雾化装置包括壳体，其包括适于插入使用者嘴中的出口和一个或多个旁路空气开口。壳体内的容器支撑件支撑容纳粉末药物制剂的容器。壳体内的穿刺机构在容器中产生一个或多个入口开口和一个或多个粉末流出开口，其中粉末流出开口的总面积为0.2mm 2至4.0mm 2。当使用者通过出口吸入时，空气流过一个或多个旁通空气开口并通过容器使雾化药剂在容器中。在一个版本中，选择流过一个或多个旁路开口的流量与一个或多个粉末流出开口之间的相对流动参数，使得雾化药物制剂的流动不会发生，直到达到预定的吸入流量。

6. 发明申请

WO2014141135A1 RESPIRABLE AGGLOMERATES OF POROUS CARRIER PARTICLES AND MICRONIZED DRUG 审中-公开
标题翻译：多孔载体颗粒和微量化药物的有效组合
公开(公告)号：WO2014141135A1
公开(公告)日：2014-09-18
申请号：PCT/IB2014/059739
申请日：2014-03-13
申请人： NOVARTIS AG , HARTMAN, Michael , TARARA, Thomas , TEUNG, Patrick , WEERS, Jeffry
发明人： HARTMAN, Michael , TARARA, Thomas , TEUNG, Patrick , WEERS, Jeffry
IPC分类号： A61K47/02 , A61K45/06 , A61K9/00 , A61K47/24 , A61K9/14 , A61K31/40 , A61K31/4704 , A61K31/58
CPC分类号： A61K31/58 , A61K9/0075 , A61K9/145 , A61K9/1611 , A61K9/1617 , A61K9/1682 , A61K31/40 , A61K31/4704 , A61K45/06 , A61K47/02 , A61K47/24 , Y10S514/826 , A61K2300/00
摘要： A pharmaceutical composition for pulmonary delivery that is a dry powder that contains a porous carrier particles and active agent particles. The porous carrier particles and the active agent particles form an ordered mixture of respirable agglomerates that are useful to treat diseases of the lung. The active agent particles can comprise one, two, three or more active ingredients. A spray-drying process for preparing the respirable agglomerates is also described.
摘要翻译：一种用于肺部输送的药物组合物，其是含有多孔载体颗粒和活性剂颗粒的干粉。多孔载体颗粒和活性剂颗粒形成可用于治疗肺疾病的可呼吸团聚体的有序混合物。活性剂颗粒可以包含一种，两种，三种或更多种活性成分。还描述了用于制备可呼吸团聚体的喷雾干燥方法。

7. 发明申请

WO2019145897A1 HIGH DOSE DELIVERY OF INHALED THERAPEUTICS 审中-公开
公开(公告)号：WO2019145897A1
公开(公告)日：2019-08-01
申请号：PCT/IB2019/050607
申请日：2019-01-24
申请人： NOVARTIS AG
发明人： SON, Yoen-Ju , HUANG, Daniel , MILLER, Danforth , WEERS, Jeffry
IPC分类号： A61K9/00 , A61K47/18 , A61K9/16 , A61K9/50 , A61K31/137 , A61K31/5383 , A61K31/7036
CPC分类号： A61K9/0075 , A61K9/1617 , A61K9/1623 , A61K9/5015 , A61K31/137 , A61K31/5383 , A61K31/7036 , A61K39/39591 , A61K45/06 , A61K47/183 , C07K16/244 , C07K2317/21 , C07K2317/55 , C07K2317/76
摘要： The present invention comprises methods and formulations to increase drug payload, especially in regard to a receptacle-based, inhalation dosed, dry powder therapeutic, wherein the methods and formulations are characterized by a high product density, as well as a high TLD per receptacle, while maintaining highly efficient aerosol performance from the device. Embodiments of the present invention comprise a spray-dried pharmaceutical powder comprising particles deliverable from a dry powder inhaler, the composition comprising active agent, and a shell-forming excipient, wherein the powder is characterized by a product density greater than 50 mg/ml. 46

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