公开(公告)号：US20070014738A1

公开(公告)日：2007-01-18

申请号：US11523914

申请日：2006-09-20

申请人： David Edwards ,  Robert Langer ,  Rita Vanbever ,  Jeffrey Mintzes ,  Jue Wang ,  Donghao Chen

发明人： David Edwards ,  Robert Langer ,  Rita Vanbever ,  Jeffrey Mintzes ,  Jue Wang ,  Donghao Chen

IPC分类号： A61K38/17 ,  A61K9/14 ,  A61L9/04

CPC分类号： A61K9/0073 ,  A61K9/0075 ,  A61K9/16 ,  A61K9/1617 ,  A61K9/1623 ,  A61K9/1641 ,  A61K9/1647 ,  A61K9/1658 ,  A61K9/1694 ,  A61K31/135 ,  A61K31/137 ,  A61K31/566 ,  A61K38/28 ,  A61K38/38 ,  A61K47/12 ,  A61K47/183 ,  A61K47/24 ,  A61K47/6927

摘要： The invention generally relates to a method for pulmonary delivery of therapeutic, prophylactic and diagnostic agents to a patient wherein the agent is released in a sustained fashion, and to particles suitable for use in the method. In particular, the invention relates to a method for the pulmonary delivery of a therapeutic, prophylactic or diagnostic agent comprising administering to the respiratory tract of a patient in need of treatment, prophylaxis or diagnosis an effective amount of particles comprising a therapeutic, prophylactic or diagnostic agent or any combination thereof in association with a charged lipid, wherein the charged lipid has an overall net charge which is opposite to that of the agent upon association with the agent. Release of the agent from the administered particles occurs in a sustained fashion.

摘要翻译： 本发明一般涉及将治疗性预防和诊断试剂肺部递送给患者，其中药剂以持续方式释放，以及适用于该方法的颗粒。 特别地，本发明涉及用于肺部递送治疗性，预防性或诊断性药物的方法，其包括对需要治疗，预防或诊断的患者的呼吸道施用有效量的包含治疗性，预防性或诊断性的颗粒 药剂或其任何组合与带电脂质相结合，其中带电脂质具有与药剂相关的与药剂相反的总净电荷。 药剂从给药颗粒中的释放以持续的方式发生。

公开(公告)号：US5985309A

公开(公告)日：1999-11-16

申请号：US971791

申请日：1997-11-17

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

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

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

CPC分类号： A61K9/1647 ,  A61K31/135 ,  A61K31/137 ,  A61K38/28 ,  A61K38/38

摘要： 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.

摘要翻译： 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。