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    • 2. 发明申请
    • Aerodynamically light particles for pulmonary drug delivery
    • 用于肺部药物递送的空气动力学轻微颗粒
    • US20050244341A1
    • 2005-11-03
    • US11177719
    • 2005-07-08
    • David EdwardsGiovannia CaponettiJeffrey HrkachNoah LotanJustin HanesAbdell Ben-JebriaRobert Langer
    • David EdwardsGiovannia CaponettiJeffrey HrkachNoah LotanJustin HanesAbdell Ben-JebriaRobert Langer
    • A61K9/00A61K9/14A61K9/16A61K31/57A61K38/28A61K47/34A61L9/04G06F7/00G06F17/30
    • A61K31/57A61K9/0075A61K9/1647A61K9/1682A61K38/28A61K47/34G06F16/284
    • Improved aerodynamically light particles for delivery to the pulmonary system, and methods for their preparation and administration are provided. In a preferred embodiment, the aerodynamically light 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 μm and 30 μm. The particles may be formed of biodegradable materials such as biodegradable polymers. For example, the particles may be formed of a functionalized polyester graft copolymer consisting of a linear a-hydroxy-acid polyester backbone having at least one amino acid group incorporated herein and at least on poly(amino acid) side chain extending from an amino acid group in the polyester backbone. In one embodiment, aerodynamically light particles having a large mean diameter, for example greater than 5 μm, can be used for enhanced delivery of a therapeutic or diagnostic agent to the alveolar region of the lung. The aerodynamically light particles optionally can incorporate a therapeutic or diagnostic agent, and may be effectively aerosolized for administration to the respiratory tract to permit systemic or local delivery of a wide variety of incorporated agents.
    • 提供用于递送至肺系统的改善的空气动力学轻微颗粒,以及其制备和给药方法。 在优选的实施方案中,空气动力学轻微颗粒由可生物降解的材料制成,并且振实密度小于0.4g / cm 3,质量平均直径在5μm和30μm之间。 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,颗粒可以由官能化的聚酯接枝共聚物形成,所述官能化聚酯接枝共聚物由具有至少一个引入本文的氨基酸基团和至少在从氨基酸延伸的聚(氨基酸)侧链上的直链α-羟基酸聚酯主链组成 集团在聚酯骨干。 在一个实施方案中,具有大平均直径(例如大于5μm)的空气动力学轻的颗粒可用于增强治疗或诊断剂递送至肺的肺泡区域。 空气动力学轻微颗粒任选地可以掺入治疗剂或诊断剂,并且可以有效地雾化用于给予呼吸道以允许各种并入药剂的全身或局部递送。
    • 3. 发明授权
    • Particles incorporating surfactants for pulmonary drug delivery
    • 含有肺部药物递送表面活性剂的颗粒
    • US5855913A
    • 1999-01-05
    • US784421
    • 1997-01-16
    • Justin HanesDavid A. EdwardsCarmen EvoraRobert Langer
    • Justin HanesDavid A. EdwardsCarmen EvoraRobert Langer
    • A61K9/00A61K9/12A61K9/14A61K9/16A61K31/135A61K31/137A61K38/28A61K38/38A61K47/48
    • A61K9/0075A61K31/135A61K31/137A61K38/28A61K38/38A61K9/1617A61K9/1623A61K9/1641A61K9/1647A61K9/1658
    • Aerodynamically light particles incorporating a surfactant on the surface thereof for drug delivery to the pulmonary system, and methods for their synthesis and administration are provided. In a preferred embodiment, the aerodynamically light 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. 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 the drug 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 L-.alpha.-phosphatidylcholine dipalmitoyl. The aerodynamically light particles incorporating a therapeutic or diagnostic agent and a surfactant may be effectively aerosolized for administration to the respiratory tract to permit systemic or local delivery of wide a variety of therapeutic agents.
    • 提供了在其表面上并入表面活性剂用于向肺系统输送药物的空气动力学轻微颗粒,以及用于其合成和给药的方法。 在优选的实施方案中,空气动力学轻微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-30μm之间的质量平均直径。 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,颗粒可以仅由药物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。 示例性的表面活性剂包括磷酸甘油酯如L-α-磷脂酰胆碱二棕榈酰基。 包含治疗剂或诊断剂和表面活性剂的空气动力学轻微颗粒可以有效地雾化,用于给予呼吸道以允许全身或局部递送各种各样的治疗剂。
    • 4. 再颁专利
    • Particles incorporating surfactants for pulmonary drug delivery
    • 含有肺部药物递送表面活性剂的颗粒
    • USRE37053E1
    • 2001-02-13
    • US09351341
    • 1999-07-12
    • Justin HanesDavid A. EdwardsCarmen EvoraRobert Langer
    • Justin HanesDavid A. EdwardsCarmen EvoraRobert Langer
    • A61K914
    • A61K31/135A61K9/0073A61K9/1617A61K9/1623A61K9/1641A61K9/1647A61K9/1658A61K31/137A61K38/28A61K38/38
    • Improved aerodynamically light particles for drug delivery to the pulmonary system, and methods for their synthesis and administration are provided. In a preferred embodiment, the aerodynamically light 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. The particles may be formed of biodegradable materials such as biodegradable polymers. For example, the particles may be formed of a functionalized polyester graft copolymer consisting of a linear &agr;-hydroxy-acid polyester backbone having at least one amino acid group incorporated therein and at least one poly(amino acid) side chain extending from an amino acid group in the polyester backbone. In one embodiment, aerodynamically light particles having a large mean diameter, for example greater than 5 &mgr;m, can be used for enhanced delivery of a therapeutic agent to the alveolar region of the lung. The aerodynamically light particles incorporating a therapeutic agent may be effectively aerosolized for administration to the respiratory tract to permit systemic or local delivery of wide variety of therapeutic agents.
    • 提供用于向肺系统输送药物的空气动力学轻微颗粒,以及用于其合成和给药的方法。 在优选的实施方案中,空气动力学轻微颗粒由可生物降解的材料制成,并且振实密度小于0.4g / cm 3,质量平均直径在5μm和30μm之间。 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,颗粒可以由官能化聚酯接枝共聚物形成,该聚酯接枝共聚物由具有至少一个氨基酸基团的直链α-羟基酸聚酯主链和至少一个从氨基酸延伸的聚(氨基酸)侧链组成 集团在聚酯骨干。 在一个实施方案中,具有大平均直径(例如大于5μm)的空气动力学轻微颗粒可用于增强治疗剂递送至肺的肺泡区域。 掺入治疗剂的空气动力学轻微颗粒可以被有效地雾化,用于给予呼吸道以允许全身或局部递送多种治疗剂。