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    Preparation of novel particles for inhalation
    12.
    发明授权
    Preparation of novel particles for inhalation 有权
    用于吸入的新型颗粒的制备

    公开(公告)号：US06652837B1

    公开(公告)日：2003-11-25

    申请号：US09394233

    申请日：1999-09-13

    Applicant: David A. Edwards ,  Robert S. Langer ,  Rita Vanbever ,  Jeffrey Mintzes ,  Jue Wang ,  Donghao Chen

    Inventor： David A. Edwards ,  Robert S. Langer ,  Rita Vanbever ,  Jeffrey Mintzes ,  Jue Wang ,  Donghao Chen

    IPC: A61K912

    CPC classification number: A61K9/0075 ,  A61K9/1617 ,  A61K9/1623 ,  A61K9/1641 ,  A61K9/1647 ,  A61K9/1658 ,  A61K31/135 ,  A61K31/137 ,  A61K38/28 ,  A61K38/38 ,  A61K47/6927 ,  Y10S514/958

    Abstract: Particles incorporating a surfactant and/or a hydrophilic or hydrophobic complex of a positively or negatively charged therapeutic agent and a charged molecule of opposite charge for drug delivery to the pulmonary system, and methods for their synthesis and administration are provided. In a preferred embodiment, the particles are made of a biodegradable material and have a tap density less than 0.4 g/cm3 and a mass mean diameter between 5 &mgr;m and 30 &mgr;m, which together yield an aerodynamic diameter of the particles of between approximately one and three microns. The particles may be formed of biodegradable materials such as biodegradable polymers. For example, the particles may be formed of poly(lactic acid) or poly(glycolic acid) or copolymers thereof. Alternatively, the particles may be formed solely of a therapeutic or diagnostic agent and a surfactant. Surfactants can be incorporated on the particle surface for example by coating the particle after particle formation, or by incorporating the surfactant in the material forming the particle prior to formation of the particle. Exemplary surfactants include phosphoglycerides such as dipalmitoyl phosphatidylcholine (DPPC). The particles can be effectively aerosolized for administration to the respiratory tract to permit systemic or local delivery of wide a variety of therapeutic agents. Formation of complexes of positively or negatively charged therapeutic agents with molecules of opposite charge can allow control of the release rate of the agents into the blood stream following administration.

    Abstract translation: 提供了将具有正或负电荷的治疗剂的表面活性剂和/或亲水或疏水配合物和用于药物递送至肺系统的带电分子的相反电荷的颗粒，以及用于其合成和给药的方法。 在一个优选的实施方案中，颗粒由可生物降解的材料制成，并且具有小于0.4g / cm 3的振实密度和5μm和30μm之间的质量平均直径，这两个颗粒之间的颗粒的空气动力学直径在 大约一到三微米。 颗粒可以由可生物降解的材料如可生物降解的聚合物形成。 例如，颗粒可以由聚（乳酸）或聚（乙醇酸）或其共聚物形成。 或者，颗粒可以仅由治疗剂或诊断剂和表面活性剂形成。 表面活性剂可以结合在颗粒表面上，例如通过在颗粒形成之后涂覆颗粒，或者通过在形成颗粒之前将表面活性剂并入形成颗粒的材料中。 示例性表面活性剂包括磷酸甘油酯，例如二棕榈酰磷脂酰胆碱（DPPC）。 这些颗粒可以有效地雾化，用于给呼吸道施用以允许全身或局部递送各种各样的治疗剂。 正电荷或带负电荷的治疗剂与相反电荷分子的复合物的形成可以允许在给药后将药剂释放到血流中的释放速率。

    Manufacture of particles for pulmonary drug delivery by carbon dioxide assisted nebulization
    16.
    发明申请
    Manufacture of particles for pulmonary drug delivery by carbon dioxide assisted nebulization 审中-公开
    通过二氧化碳辅助雾化制造用于肺部药物递送的颗粒

    公开(公告)号：US20060105051A1

    公开(公告)日：2006-05-18

    申请号：US11260884

    申请日：2005-10-27

    Applicant: Blair Jackson ,  David Bennett ,  Donghao Chen ,  Michael Lipp ,  Purav Dave

    Inventor： Blair Jackson ,  David Bennett ,  Donghao Chen ,  Michael Lipp ,  Purav Dave

    IPC: A61K9/14 ,  B29B9/00

    CPC classification number: A61K9/007 ,  A61K9/0075

    Abstract: Methods of making porous particles by using carbon dioxide assisted nebulization (CAN) technology in combination with spray drying technologies are disclosed. As the mixture of carbon dioxide (CO2) and the solvent with drug matrix is expanded through the nebulizer to atmospheric conditions, the resulting aerosol contains fine micro-bubbles and/or micro-droplets that contains dissolved CO2 which is co-currently fed into a spray drying chamber.

    Abstract translation: 公开了通过使用二氧化碳辅助雾化（CAN）技术与喷雾干燥技术组合制备多孔颗粒的方法。 由于二氧化碳（CO 2 CO 2）和溶剂与药物基质的混合物通过喷雾器膨胀至大气条件，所得气溶胶含有细小的微气泡和/或微滴，其含有溶解的CO 其共同进料到喷雾干燥室中。

    Preparation of particles for inhalation
    17.
    发明授权
    Preparation of particles for inhalation 失效
    吸入颗粒的制备

    公开(公告)号：US5985309A

    公开(公告)日：1999-11-16

    申请号：US971791

    申请日：1997-11-17

    Applicant: David A. Edwards ,  Robert S. Langer ,  Rita Vanbever ,  Jeffrey Mintzes ,  Jue Wang ,  Donghao Chen

    Inventor： David A. Edwards ,  Robert S. Langer ,  Rita Vanbever ,  Jeffrey Mintzes ,  Jue Wang ,  Donghao Chen

    IPC: A61K9/16 ,  A61K31/135 ,  A61K31/137 ,  A61K38/28 ,  A61K38/38 ,  A61K13/00

    CPC classification number: A61K9/1647 ,  A61K31/135 ,  A61K31/137 ,  A61K38/28 ,  A61K38/38

    Abstract: Particles incorporating a surfactant and/or a hydrophilic or hydrophobic complex of a positively or negatively charged therapeutic agent and a charged molecule of opposite charge for drug delivery to the pulmonary system, and methods for their synthesis and administration are provided. In a preferred embodiment, the particles are made of a biodegradable material and have a tap density less than 0.4 g/cm.sup.3 and a mass mean diameter between 5 .mu.m and 30 .mu.m, which together yield an aerodynamic diameter of the particles of between approximately one and three microns. The particles may be formed of biodegradable materials such as biodegradable polymers. For example, the particles may be formed of poly(lactic acid) or poly(glycolic acid) or copolymers thereof. Alternatively, the particles may be formed solely of a therapeutic or diagnostic agent and a surfactant. Surfactants can be incorporated on the particle surface for example by coating the particle after particle formation, or by incorporating the surfactant in the material forming the particle prior to formation of the particle. Exemplary surfactants include phosphoglycerides such as dipalmitoyl phosphatidylcholine (DPPC). The particles can be effectively aerosolized for administration to the respiratory tract to permit systemic or local delivery of wide a variety of therapeutic agents. Formation of complexes of positively or negatively charged therapeutic agents with molecules of opposite charge can allow control of the release rate of the agents into the blood stream following administration.

    Abstract translation: 提供了将具有正或负电荷的治疗剂的表面活性剂和/或亲水或疏水配合物和用于药物递送至肺系统的带电分子的相反电荷的颗粒，以及用于其合成和给药的方法。 在优选的实施方案中，颗粒由可生物降解的材料制成，并且具有小于0.4g / cm 3的振实密度和5μm至30μm之间的质量平均直径，其一起产生颗粒的空气动力学直径在约 一和三微米。 颗粒可以由可生物降解的材料如可生物降解的聚合物形成。 例如，颗粒可以由聚（乳酸）或聚（乙醇酸）或其共聚物形成。 或者，颗粒可以仅由治疗剂或诊断剂和表面活性剂形成。 表面活性剂可以结合在颗粒表面上，例如通过在颗粒形成之后涂覆颗粒，或者通过在形成颗粒之前将表面活性剂并入形成颗粒的材料中。 示例性表面活性剂包括磷酸甘油酯，例如二棕榈酰磷脂酰胆碱（DPPC）。 这些颗粒可以有效地雾化，用于给呼吸道施用以允许全身或局部递送各种各样的治疗剂。 正电荷或带负电荷的治疗剂与相反电荷分子的复合物的形成可以允许在给药后将药剂释放到血流中的释放速率。

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