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1. 发明申请

US20070212405A1 DISPERSION FOR PULMONARY DELIVERY OF A BIOACTIVE AGENT 失效
标题翻译：用于脉冲递送生物剂的分散体
公开(公告)号：US20070212405A1
公开(公告)日：2007-09-13
申请号：US11675073
申请日：2007-02-14
申请人： Luis Dellamary , Thomas Tarara , Alexey Kabalnov , Jeffry Weers , Ernest Schutt
发明人： Luis Dellamary , Thomas Tarara , Alexey Kabalnov , Jeffry Weers , Ernest Schutt
IPC分类号： A61K9/16 , A61K9/127
CPC分类号： A61K9/008 , A61K9/0073 , A61K9/0075 , A61K9/0078 , A61K9/1611 , A61K9/1617 , A61K9/1635 , A61K9/1641 , A61K9/1652 , A61K9/1694 , A61K31/685 , Y10S514/937 , Y10S977/904 , Y10S977/906 , Y10S977/926
摘要： Stabilized dispersions are provided for the delivery of a bioactive agent. The dispersions preferably comprise a plurality of perforated microstructures dispersed in a suspension medium that typically comprises a liquid fluorochemical. As density variations between the suspended particles and suspension medium are minimized and attractive forces between microstructures are attenuated, the disclosed dispersions are particularly resistant to degradation, such as by settling or flocculation. In particularly preferred embodiments the stabilized dispersions may be directly administered to the lung of a patient using an endotracheal tube or bronchoscope.
摘要翻译：提供稳定的分散体用于递送生物活性剂。分散体优选包括分散在通常包含液体含氟化合物的悬浮介质中的多个穿孔微结构。随着悬浮颗粒和悬浮介质之间的密度变化被最小化，微结构之间的吸引力减弱，所公开的分散体特别地耐降解，例如通过沉降或絮凝。在特别优选的实施方案中，稳定的分散体可以使用气管内导管或支气管镜直接施用于患者的肺。

2. 发明申请

US20060159629A1 Pulmonary delivery particles with phospholipid structural matrix 审中-公开
标题翻译：肺输送颗粒与磷脂结构基质
公开(公告)号：US20060159629A1
公开(公告)日：2006-07-20
申请号：US11317523
申请日：2005-12-22
申请人： Thomas Tarara , Jeffry Weers , Alexey Kabalnov , Ernest Schutt , Luis Dellamary
发明人： Thomas Tarara , Jeffry Weers , Alexey Kabalnov , Ernest Schutt , Luis Dellamary
IPC分类号： A61K9/14 , A61K31/685 , A61L9/04
CPC分类号： A61K9/008 , A61K9/0073 , A61K9/0075 , A61K9/0078 , A61K9/1611 , A61K9/1617 , A61K9/1635 , A61K9/1641 , A61K9/1652 , A61K9/1694 , A61K31/685 , Y02A50/41 , Y02A50/466 , Y10S514/937 , Y10S977/904 , Y10S977/906 , Y10S977/926
摘要： A pulmonary delivery medicament comprises a plurality of particulates, each particulate having a perforated microstructure comprising a phospholipid structural matrix and active agent, the phospholipid structural matrix comprising greater than about 50% w/w phospholipid, and the particulates having a geometric diameter of from 0.5 to 50 μm. The medicament can be made from a liquid feedstock having greater than about 20% w/w phospholipid with an added active agent, which is spray dried to produce the particulates.
摘要翻译：肺递送药物包括多个颗粒，每个颗粒具有包含磷脂结构基质和活性剂的穿孔微结构，所述磷脂结构基质包含大于约50％w / w磷脂，并且所述颗粒的几何直径为0.5 到50个妈妈药物可以由具有大于约20％w / w磷脂的液体原料与添加的活性剂制成，其被喷雾干燥以产生颗粒。

3. 发明申请

US20050074498A1 Engineered particles and methods of use 审中-公开
标题翻译：工程粒子和使用方法
公开(公告)号：US20050074498A1
公开(公告)日：2005-04-07
申请号：US10612393
申请日：2003-07-03
申请人： Thomas Tarara , Jeffry Weers , Alexey Kabalnov , Ernest Schutt , Luis Dellamary
发明人： Thomas Tarara , Jeffry Weers , Alexey Kabalnov , Ernest Schutt , Luis Dellamary
IPC分类号： A61K9/00 , A61K9/12 , A61K9/16 , A61K9/22 , A61K9/51 , A61K9/72 , A61K45/00 , A61K47/24 , A61K49/04 , A61P11/00 , A61P39/00 , A61K9/14 , A61K9/50
CPC分类号： A61K9/008 , A61K9/0073 , A61K9/0075 , A61K9/0078 , A61K9/1611 , A61K9/1617 , A61K9/1635 , A61K9/1641 , A61K9/1652 , A61K9/1694 , A61K31/685 , Y02A50/41 , Y02A50/466 , Y10S514/937 , Y10S977/904 , Y10S977/906 , Y10S977/926
摘要： Engineered particles are provided may be used for the delivery of a bioactive agent to the respiratory tract of a patient. The particles may be used in the form of dry powders or in the form of stabilized dispersions comprising a nonaqueous continuous phase. In particularly preferred embodiments the particles may be used in conjunction with an inhalation device such as a dry powder inhaler, metered dose inhaler or a nebulizer.
摘要翻译：提供的工程颗粒可用于将生物活性剂递送到患者的呼吸道。颗粒可以以干粉形式或以包含非水连续相的稳定分散体的形式使用。在特别优选的实施方案中，颗粒可以与吸入装置如干粉吸入器，计量剂量吸入器或喷雾器结合使用。

4. 发明申请

US20050207986A1 Stabilized preparations for use in nebulizers 审中-公开
标题翻译：用于雾化器的稳定制剂
公开(公告)号：US20050207986A1
公开(公告)日：2005-09-22
申请号：US11076430
申请日：2005-03-09
申请人： Ernest Schutt , Thomas Tarara , Luis Dellamary , Alexey Kabalnov , Jeffry Weers
发明人： Ernest Schutt , Thomas Tarara , Luis Dellamary , Alexey Kabalnov , Jeffry Weers
IPC分类号： A61F2/00 , A61F13/00 , A61K9/00 , A61K9/14 , A61K9/16 , A61L9/04 , A61M11/00
CPC分类号： A61K9/0078 , A61K9/0075 , A61K9/008 , Y02A50/41 , Y02A50/466
摘要： Stabilized dispersions are provided for the delivery of a bioactive agent to the respiratory tract of a patient. The dispersions preferably comprise a stabilized colloidal system which may comprise a fluorochemical component. In particularly preferred embodiments, the stabilized dispersions comprise perforated microstructures dispersed in a fluorochemical suspension medium. As density variations between the suspended particles and suspension medium are minimized and attractive forces between microstructures are attenuated, the disclosed dispersions are particularly resistant to degradation, such as by settling or flocculation. In particularly preferred embodiments, the stabilized dispersions may be administered to the lung of a patient using a nebulizer.
摘要翻译：提供稳定的分散体用于将生物活性剂递送到患者的呼吸道。分散体优选包含稳定的胶体体系，其可以包含含氟化合物组分。在特别优选的实施方案中，稳定的分散体包含分散在含氟化合物悬浮介质中的穿孔微结构。随着悬浮颗粒和悬浮介质之间的密度变化被最小化，微结构之间的吸引力减弱，所公开的分散体特别地耐降解，例如通过沉降或絮凝。在特别优选的实施方案中，稳定的分散体可以使用喷雾器施用于患者的肺。

5. 发明授权

US07205343B2 Stabilized bioactive preparations and method of use 失效
标题翻译：稳定的生物活性制剂和使用方法
公开(公告)号：US07205343B2
公开(公告)日：2007-04-17
申请号：US09999071
申请日：2001-12-03
申请人： Luis A. Dellamary , Thomas Tarara , Alexey Kabalnov , Jeffry Weers , Ernest Schutt
发明人： Luis A. Dellamary , Thomas Tarara , Alexey Kabalnov , Jeffry Weers , Ernest Schutt
IPC分类号： C08K7/22
CPC分类号： A61K9/008 , A61K9/0073 , A61K9/0075 , A61K9/0078 , A61K9/1611 , A61K9/1617 , A61K9/1635 , A61K9/1641 , A61K9/1652 , A61K9/1694 , A61K31/685 , Y10S514/937 , Y10S977/904 , Y10S977/906 , Y10S977/926
摘要： Stabilized dispersions are provided for the delivery of a bioactive agent. The dispersions preferably comprise a plurality of perforated microstructures dispersed in a suspension medium that typically comprises a liquid fluorochemical. As density variations between the suspended particles and suspension medium are minimized and attractive forces between microstructures are attenuated, the disclosed dispersions are particularly resistant to degradation, such as by settling or flocculation. In particularly preferred embodiments the stabilized dispersions may be directly administered to the lung of a patient using an endotracheal tube or bronchoscope.
摘要翻译：提供稳定的分散体用于递送生物活性剂。分散体优选包括分散在通常包含液体含氟化合物的悬浮介质中的多个穿孔微结构。随着悬浮颗粒和悬浮介质之间的密度变化被最小化，微结构之间的吸引力减弱，所公开的分散体特别地耐降解，例如通过沉降或絮凝。在特别优选的实施方案中，稳定的分散体可以使用气管内导管或支气管镜直接施用于患者的肺。

6. 发明申请

US20050281747A1 Mixed gas microbubble compositions 审中-公开
标题翻译：混合气体微泡组合物
公开(公告)号：US20050281747A1
公开(公告)日：2005-12-22
申请号：US11181661
申请日：2005-07-14
申请人： Ernest Schutt , David Evitts , Rene Kinner , Charles Anderson , Jeffry Weers
发明人： Ernest Schutt , David Evitts , Rene Kinner , Charles Anderson , Jeffry Weers
IPC分类号： A61K49/00 , A61B8/00 , A61K49/22 , B01J13/02 , F21V8/00
CPC分类号： A61K49/227 , A61K49/223 , G02B6/0006
摘要： A microbubble preparation formed of a plurality of microbubbles comprising a first gas and a second gas surrounded by a membrane such as a surfactant, wherein the first gas and the second gas are present in a molar ratio of from about 1:100 to about 1000:1, and wherein the first gas has a vapor pressure of at least about (760-x) mm Hg at 37 C., where x is the vapor pressure of the second gas at 37 C., and wherein the vapor pressure of each of the first and second gases is greater than about 75 mm Hg at 37 C.; also disclosed are methods for preparing microbubble compositions, including compositions that rapidly shrink from a first average diameter to a second average diameter less than about 75% of the first average diameter and are stabilized at the second average diameter; kits for preparing microbubbles; and methods for using such microbubbles as ultrasound contrast agents
摘要翻译：一种由多个微泡形成的微泡制品，包括第一气体和被诸如表面活性剂的膜包围的第二气体，其中第一气体和第二气体以约1:100至约1000:1的摩尔比存在。 1，并且其中第一气体在37℃下具有至少约（760-x）mm Hg的蒸汽压，其中x是第二气体在37℃的蒸汽压，并且其中每个第一和第二气体在37℃下大于约75mm Hg。还公开了制备微泡组合物的方法，包括从第一平均直径快速收缩至小于第一平均直径的约75％的第二平均直径的组合物，并且稳定在第二平均直径; 用于制备微泡的试剂盒以及使用这种微泡作为超声造影剂的方法

7. 发明申请

US20150374685A1 PULMONARY DELIVERY OF A FLUOROQUINOLONE 审中-公开
标题翻译：荧光素的脉冲递送
公开(公告)号：US20150374685A1
公开(公告)日：2015-12-31
申请号：US14844373
申请日：2015-09-03
申请人： Jeffry Weers , Thomas Tarara
发明人： Jeffry Weers , Thomas Tarara
IPC分类号： A61K31/496 , A61K9/00
CPC分类号： A61K31/496 , A61K9/0075 , A61K31/47 , A61M15/0041
摘要： A composition for pulmonary administration comprises a fluoroquinolone betaine, such as ciprofloxacin betaine, and an excipient. In one version, the particles have a mass median aerodynamic diameter from about 1 μm to about 5 μm, and the fluoroquinolone has a half life in the lungs of at least 1.5 hours. The composition is useful in treating an endobronchial infection, such as Pseudomonas aeruginosa, and is particularly useful in treating cystic fibrosis.
摘要翻译：用于肺部给药的组合物包含氟喹诺酮甜菜碱，如环丙沙星甜菜碱和赋形剂。在一个版本中，颗粒具有约1μm至约5μm的质量中值空气动力学直径，并且氟喹诺酮在肺中的半衰期至少为1.5小时。该组合物可用于治疗支气管炎感染，例如铜绿假单胞菌，并且特别可用于治疗囊性纤维化。

8. 发明申请

US20050214224A1 Lipid formulations for spontaneous drug encapsulation 审中-公开
标题翻译：用于自发药物包封的脂质制剂
公开(公告)号：US20050214224A1
公开(公告)日：2005-09-29
申请号：US10982191
申请日：2004-11-04
申请人： Jeffry Weers , Thomas Tarara , Stelios Tzannis
发明人： Jeffry Weers , Thomas Tarara , Stelios Tzannis
IPC分类号： A61K9/00 , A61K9/127 , A61K9/16 , A61L9/04 , A61M15/00
CPC分类号： A61K9/0075 , A61K9/127 , A61K9/1617 , A61M15/0028 , A61M15/0041 , A61M2202/064
摘要： A pharmaceutical formulation for pulmonary administration is disclosed. The pharmaceutical formulation comprises a lipid component and an active agent, wherein the pharmaceutical formulation has a liquid phase transition temperature of less than or equal to 37° C. when hydrated and a liquid phase transition temperature of greater than 57° C. when non-hydrated, whereby the lipid component spontaneously encapsulates and/or entraps the active agent when the pharmaceutical formulation is administered to the lungs. A targeting agent may also be provided. In one version, the pharmaceutical formulation is useful to treat an infection, such as an inhalation anthrax infection.
摘要翻译：公开了一种用于肺部给药的药物制剂。药物制剂包含脂质组分和活性剂，其中当水合时，药物制剂的液相转变温度小于或等于37℃，液相转变温度大于57℃时，当药物制剂施用于肺时，脂质组分自发地包封和/或捕获活性剂。还可以提供靶向剂。在一个版本中，药物制剂可用于治疗感染，例如吸入性炭疽感染。

9. 发明授权

US09155732B2 Pulmonary delivery of a fluoroquinolone 有权
标题翻译：氟喹诺酮的肺部输送
公开(公告)号：US09155732B2
公开(公告)日：2015-10-13
申请号：US14457162
申请日：2014-08-12
申请人： Jeffry Weers , Thomas Tarara
发明人： Jeffry Weers , Thomas Tarara
IPC分类号： A61K9/14 , A61K31/47 , A61K31/496 , A61P11/00 , A61P31/04 , A61K9/00 , A61M15/00
CPC分类号： A61K31/496 , A61K9/0075 , A61K31/47 , A61M15/0041
摘要： A composition for pulmonary administration comprises a fluoroquinolone betaine, such as ciprofloxacin betaine, and an excipient. In one version, the particles have a mass median aerodynamic diameter from about 1 μm to about 5 μm, and the fluoroquinolone has a half life in the lungs of at least 1.5 hours. The composition is useful in treating an endobronchial infection, such as Pseudomonas aeruginosa, and is particularly useful in treating cystic fibrosis.
摘要翻译：用于肺部给药的组合物包含氟喹诺酮甜菜碱，如环丙沙星甜菜碱和赋形剂。在一个版本中，颗粒具有约1μm至约5μm的质量中值空气动力学直径，并且氟喹诺酮在肺中的半衰期至少为1.5小时。该组合物可用于治疗支气管炎感染，例如铜绿假单胞菌，并且特别可用于治疗囊性纤维化。

10. 发明申请

US20110123626A1 PULMONARY DELIVERY OF A FLUOROQUINOLONE 有权
标题翻译：荧光素的脉冲递送
公开(公告)号：US20110123626A1
公开(公告)日：2011-05-26
申请号：US12992371
申请日：2009-05-15
申请人： Jeffry Weers , Thomas Tarara
发明人： Jeffry Weers , Thomas Tarara
IPC分类号： A61K9/14 , A61K31/497 , A61K31/702 , A61P11/00 , A61P31/04
CPC分类号： A61K31/496 , A61K9/0075 , A61K31/47 , A61M15/0041
摘要： A composition for pulmonary administration comprises a fluoroquinolone betaine, such as ciprofloxacin betaine, and an excipient. In one version, the particles have a mass median aerodynamic diameter from about 1 μm to about 5 μm, and the fluoroquinolone has a half life in the lungs of at least 1.5 hours. The composition is useful in treating an endobronchial infection, such as Pseudomonas aeruginosa, and is particularly useful in treating cystic fibrosis.
摘要翻译：用于肺部给药的组合物包含氟喹诺酮甜菜碱，如环丙沙星甜菜碱和赋形剂。在一个版本中，颗粒具有约1μm至约5μm的质量中值空气动力学直径，并且氟喹诺酮在肺中的半衰期至少为1.5小时。该组合物可用于治疗支气管炎感染，例如铜绿假单胞菌，并且特别可用于治疗囊性纤维化。

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