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公开(公告)号：US5733526A
公开(公告)日：1998-03-31
申请号：US572859
申请日：1995-12-14
CPC分类号： A61K9/0026 , A61K9/113 , Y10S514/937 , Y10S977/786 , Y10S977/795 , Y10S977/902 , Y10S977/904 , Y10S977/905 , Y10S977/915 , Y10S977/926 , Y10S977/927 , Y10S977/962
摘要： Novel hydrocarbon oil/fluorochemical preparations and methods for their use are provided. The preparations, which preferably comprise a fluorophilic dispersing agent, may be in the form of hydrocarbon oil-in-fluorochemical dispersions or in the form of a multiple emulsion comprising a polar liquid continuous phase and are particularly useful for administering bioactive agents. In particular the preparations of the present invention may be used to control the bioavailability and improve the efficacy of lipophilic bioactive agents having limited solubility in an aqueous physiological environment.
摘要翻译： 提供新型烃油/含氟化合物制剂及其使用方法。 优选包含嗜氟分散剂的制剂可以是烃油中的含氟化合物分散体的形式或者包含极性液体连续相的多重乳液的形式，并且特别可用于施用生物活性剂。 特别地，本发明的制剂可用于控制生物利用度并改善在水性生理环境中溶解度有限的亲脂性生物活性剂的功效。
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2.发明授权
公开(公告)号：US5874481A
公开(公告)日：1999-02-23
申请号：US483468
申请日：1995-06-07
IPC分类号： A61K9/00 , A61K31/02 , A61K31/045
CPC分类号： A61K9/0026
摘要： A thermodynamically stable molecular solution providing enhanced bioavailability for lipophilic pharmaceutical agents, comprising a liquid carrier comprising one or more physiologically acceptable lipophilic fluorochemicals, and a pharmaceutically effective amount of at least one lipophilic pharmaceutical agent in said liquid carrier to form a thermodynamically stable molecular solution, optionally also including a co-solvent for facilitating solubilization of the pharmaceutical agent. Methods of making and using the molecular solution are also disclosed.
摘要翻译： 一种热力学稳定的分子溶液，其为亲脂性药剂提供增强的生物利用度，其包含一种液体载体，其包含一种或多种生理学上可接受的亲油性含氟化合物，以及在所述液体载体中的药学有效量的至少一种亲脂性药剂以形成热力学稳定的分子溶液， 任选地还包括用于促进药剂溶解的共溶剂。 还公开了制备和使用分子溶液的方法。
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3.发明授权
公开(公告)号：US5667809A
公开(公告)日：1997-09-16
申请号：US482176
申请日：1995-06-07
CPC分类号： A61K9/0026 , Y10S514/937
摘要： A method for preparing a pharmaceutical microdispersion exhibiting enhanced bioavailability, including the steps of providing a thermodynamically stable pharmaceutical composition comprising at least one lipophilic pharmaceutical agent incorporated in a physiologically acceptable liquid carrier, the liquid carrier comprising one or more lipophilic solvents such as fluorochemicals and preferably at least one nonfluorinated co-solvent, and combining the stable pharmaceutical composition with an amount of at least one miscible diluent sufficient to initiate phase separation of the lipophilic pharmaceutical agent from the pharmaceutical composition wherein a microdispersion of the pharmaceutical composition is formed. Also disclosed are microdisperse pharmaceutical compositions and kits for forming such compositions.
摘要翻译： 一种制备显示增强的生物利用度的药物微分散体的方法，包括以下步骤：提供包含至少一种引入生理学上可接受的液体载体的亲脂性药剂的热力学稳定的药物组合物，所述液体载体包含一种或多种亲脂性溶剂如含氟化合物， 至少一种非氟化共溶剂，并将稳定的药物组合物与一定量的至少一种可混溶的稀释剂组合，所述至少一种可混溶的稀释剂足以引发亲脂性药剂与药物组合物的相分离，其中形成药物组合物的微分散体。 还公开了用于形成这种组合物的微分散药物组合物和试剂盒。
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公开(公告)号：US07442388B2
公开(公告)日：2008-10-28
申请号：US09851226
申请日：2001-05-08
CPC分类号： A61K9/0075 , A61K9/008 , A61K9/0082 , A61K9/10 , A61K9/1611 , A61K9/1617 , A61K9/1694 , A61K38/29 , A61K47/02 , A61M15/0065 , A61M2205/3306
摘要： Phospholipid based powders for drug delivery applications are disclosed. The powders comprise a polyvalent cation in an amount effective to increase the gel-to-liquid crystal transition temperature of the particle compared to particles without the polyvalent cation. The powders are hollow and porous and are preferably administered via inhalation.
摘要翻译： 公开了用于药物递送应用的基于磷脂的粉末。 与没有多价阳离子的颗粒相比，粉末包含有效增加颗粒的凝胶 - 液晶的转变温度的多价阳离子。 粉末是中空的和多孔的，并且优选通过吸入给药。
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公开(公告)号：US08709484B2
公开(公告)日：2014-04-29
申请号：US12258163
申请日：2008-10-24
CPC分类号： A61K9/0075 , A61K9/008 , A61K9/0082 , A61K9/10 , A61K9/1611 , A61K9/1617 , A61K9/1694 , A61K38/29 , A61K47/02 , A61M15/0065 , A61M2205/3306
摘要： Phospholipid based powders for drug delivery applications are disclosed. The powders may include a polyvalent cation in an amount effective to increase the gel-to-liquid crystal transition temperature of the particle compared to particles without the polyvalent cation. The powders are hollow and porous and are preferably administered via inhalation.
摘要翻译： 公开了用于药物递送应用的基于磷脂的粉末。 与没有多价阳离子的颗粒相比，粉末可以包括有效增加颗粒的凝胶 - 液晶的转变温度的多价阳离子。 粉末是中空的和多孔的，并且优选通过吸入给药。
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公开(公告)号：US20090047358A1
公开(公告)日：2009-02-19
申请号：US12258163
申请日：2008-10-24
IPC分类号： A61K9/14 , A61K38/21 , A61K31/58 , A61K31/7036 , A61P43/00 , F26B3/06 , A61K31/137 , A61K38/28 , A61K31/351
CPC分类号： A61K9/0075 , A61K9/008 , A61K9/0082 , A61K9/10 , A61K9/1611 , A61K9/1617 , A61K9/1694 , A61K38/29 , A61K47/02 , A61M15/0065 , A61M2205/3306
摘要： Phospholipid based powders for drug delivery applications are disclosed. The powders comprise a polyvalent cation in an amount effective to increase the gel-to-liquid crystal transition temperature of the particle compared to particles without the polyvalent cation. The powders are hollow and porous and are preferably administered via inhalation.
摘要翻译： 公开了用于药物递送应用的基于磷脂的粉末。 与没有多价阳离子的颗粒相比，粉末包含有效增加颗粒的凝胶 - 液晶的转变温度的多价阳离子。 粉末是中空的和多孔的，并且优选通过吸入给药。
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7.发明申请PULMONARY DELIVERY PARTICLES COMPRISING WATER INSOLUBLE OR CRYSTALLINE ACTIVE AGENTS 审中-公开包含水不溶性或结晶活性剂的脉冲递送颗粒公开(公告)号：US20100272823A1
公开(公告)日：2010-10-28
申请号：US12774540
申请日：2010-05-05
IPC分类号： A61K9/14 , A61K38/43 , A61K31/56 , A61K31/7088 , A61K31/713 , A61K38/00 , A61P11/00 , A61P31/00 , A61P37/08 , A61P29/00 , A61P23/00 , A61P9/00 , B29B9/12
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： A pulmonary delivery medicament comprises a plurality of particulates, the particulates comprising a structural matrix and a water insoluble and/or crystalline active agent. The particulates have a geometric diameter of 0.5 to 50 μm. The water insoluble active agent can be a fungicide, antibiotic, budesonide. A method of making the medicament comprises forming a liquid feedstock, and forming a feedstock suspension by suspending in the liquid feedstock, the active agent and an excipient capable of forming a structural matrix, such as a phospholipid. The feedstock suspension is spray dried to produce the particulates.
摘要翻译： 肺递送药物包括多个颗粒，所述颗粒包含结构基质和水不溶性和/或结晶活性剂。 颗粒的几何直径为0.5至50μm。 水不溶性活性剂可以是杀真菌剂，抗生素，布地奈德。 制备药物的方法包括形成液体原料，并通过悬浮在液体原料，活性剂和能够形成结构基质如磷脂的赋形剂中形成原料悬浮液。 将原料悬浮液喷雾干燥以产生颗粒。
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公开(公告)号：US07393544B2
公开(公告)日：2008-07-01
申请号：US11675073
申请日：2007-02-14
IPC分类号： 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。
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公开(公告)号：US06946117B1
公开(公告)日：2005-09-20
申请号：US09218213
申请日：1998-12-22
CPC分类号： A61K9/0078 , A61K9/0075 , A61K9/008 , Y02A50/41 , Y02A50/466 , Y02A50/472
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.
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公开(公告)号：US06565885B1
公开(公告)日：2003-05-20
申请号：US09219736
申请日：1998-12-22
IPC分类号： A61K914
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 , Y02A50/472 , Y10S514/937 , Y10S977/904 , Y10S977/906 , Y10S977/926
摘要： Spray drying methods for forming powder compositions for pharmaceutical applications are disclosed. According to one aspect of the invention, the spray drying feed stock comprises a bioactive agent, surfactant, and a blowing agent. Another aspect of the invention is directed to spray drying a feed stock comprising a phospholipid and calcium chloride.
摘要翻译： 公开了用于形成药物应用的粉末组合物的喷雾干燥方法。 根据本发明的一个方面，喷雾干燥原料包含生物活性剂，表面活性剂和发泡剂。 本发明的另一方面涉及喷雾干燥包含磷脂和氯化钙的原料。
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