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公开(公告)号：US06447753B2
公开(公告)日：2002-09-10
申请号：US09891131
申请日：2001-06-25
申请人： David A. Edwards , Giovanni Caponetti , Jeffrey S. Hrkach , Noah Lotan , Justin Hanes , Robert S. Langer , Abdellaziz Ben-Jebria
发明人： David A. Edwards , Giovanni Caponetti , Jeffrey S. Hrkach , Noah Lotan , Justin Hanes , Robert S. Langer , Abdellaziz Ben-Jebria
IPC分类号： A61K912
CPC分类号： A61K9/0075 , A61K9/1647 , A61K31/137 , Y10S514/826 , Y10S514/851
摘要： Improved porous particles for drug delivery to the pulmonary system, and methods for their synthesis and administration are provided. In a preferred embodiment, the porous particles are made of a biodegradable material and have a mass density less than 0.4 g/cm3/. 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, porous particles having a relatively 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 porous 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.
摘要翻译： 提供用于向肺系统递送药物的改进的多孔颗粒，以及用于其合成和给药的方法。 在优选的实施方案中，多孔颗粒由可生物降解的材料制成，其质量密度小于0.4g / cm 3 /。 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，具有相对大的平均直径，例如大于5um的多孔颗粒可用于增强治疗剂递送至肺的肺泡区域。 掺入治疗剂的多孔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多种治疗剂。
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12.发明授权公开(公告)号：US09138407B2
公开(公告)日：2015-09-22
申请号：US12090899
申请日：2006-10-20
CPC分类号： A61K9/0078 , A61K9/0075 , A61K45/06
摘要： Provided is an inhalatory pharmaceutical composition that comprises a drug, a soluble excipient and a surfactant, wherein the soluble excipient is present in an amount between 10% and less than 100% by weight; and the solid excipient forms a solid matrix in which the drug is dispersed; the weight ratio between the surfactant and drug is between 0.01 and 10; the particle size of at least 50% of the particles of the powder is below 5 μm; the bulk density db of the powder is between 0.1 and 0.3 g/cc; the tapped density dt of the powder is between 0.15 and 0.7 g/cc and the ratio db/dt is between 0.2 and 0.65. Also provided is the method for fabricating the composition.
摘要翻译： 本发明提供一种吸入性药物组合物，其包含药物，可溶性赋形剂和表面活性剂，其中所述可溶性赋形剂的存在量为10重量％至小于100重量％ 固体赋形剂形成药物分散的固体基质; 表面活性剂与药物的重量比为0.01〜10; 粉末颗粒的至少50％的粒径小于5μm; 粉末的体积密度db在0.1至0.3g / cc之间; 粉末的抽头密度dt在0.15和0.7g / cc之间，比率db / dt在0.2和0.65之间。 还提供了用于制造组合物的方法。
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13.发明申请Dry Powder Pharmaceutical Compositions, Its Preparation Process and Stable Aqueous Suspension Obtained from such Composition 审中-公开干粉药物组合物，其制备方法和从该组合物获得的稳定的水悬浮液公开(公告)号：US20130052233A1
公开(公告)日：2013-02-28
申请号：US13558566
申请日：2012-07-26
CPC分类号： A61K9/145 , A61K9/0075 , A61K9/0078 , A61K9/14 , A61K9/143 , A61K31/192 , A61K31/573 , A61K31/58
摘要： Pharmaceutical composition in a dry powder form comprising at least one hydrophobic active principle, at least one water-soluble excipient and at least one surfactant, wherein the particles in said dry powder state have a Volume Mean Diameter VMDd greater than the Volume Mean Diameter VMDw of particles in a suspension obtained from said pharmaceutical composition at standard conditions of dispersion in a water-medium. It is also disclosed a process to prepare such dry composition and an extemporaneous suspension for inhalation therapy obtainable from said dry composition.
摘要翻译： 包含至少一种疏水活性成分，至少一种水溶性赋形剂和至少一种表面活性剂的干粉形式的药物组合物，其中所述干粉状态的颗粒的体积平均直径VMDd大于体积平均直径VMDd， 在由水介质中分散的标准条件下由所述药物组合物获得的悬浮液中的颗粒。 还公开了制备这种干组合物和可从所述干组合物获得的用于吸入治疗的临时悬浮液的方法。
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公开(公告)号：US07754242B2
公开(公告)日：2010-07-13
申请号：US10392333
申请日：2003-03-19
CPC分类号： A61K9/0078 , A61K9/0075 , A61K9/1617 , A61K31/40 , A61K31/438 , A61K31/46 , A61K45/06
摘要： The present invention is based, in part, on the unexpected discovery that particles for pulmonary delivery of a therapeutic, prophylactic or diagnostic agent that comprise a phospholipid and a sufficient amount of leucine can produce sustained effect of the agent. Specifically, particles for pulmonary delivery of a therapeutic, prophylactic or diagnostic agent that contain a phospholipid or combination of phospholipids, wherein the phospholipid or combination of phospholipids is present in the particles in an amount of about 1 to 46 weight percent; and leucine, wherein leucine is present in the particles in an amount of at least 46 weight percent, can contribute to sustained effect of the agent. Particles that comprise at least 46 weight percent leucine but that do not contain phospholipids do not exhibit these same sustained effect properties.
摘要翻译： 本发明部分地基于意想不到的发现，即用于肺部递送包含磷脂和足够量的亮氨酸的治疗性，预防性或诊断剂的颗粒可以产生药剂的持久作用。 具体地，用于肺部递送含有磷脂或磷脂组合的治疗性预防或诊断剂的颗粒，其中磷脂或磷脂组合以约1至46重量％的量存在于颗粒中; 和亮氨酸，其中亮氨酸以至少46重量％的量存在于颗粒中，可有助于药剂的持续作用。 包含至少46重量百分比的亮氨酸但不含磷脂的颗粒不具有这些相同的持续作用特性。
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公开(公告)号：US07399528B2
公开(公告)日：2008-07-15
申请号：US10806240
申请日：2004-03-23
CPC分类号： A61K9/0075 , A61K9/145 , A61K9/1623 , Y10T428/2991 , Y10T428/2998
摘要： Carrier particles, for use in the preparation of powdery mixtures for administration by inhalation, and having a median diameter of greater than 90 microns and a surface rugosity expressed as the fractal dimension of less than or equal to 1.1, may be prepared by subjecting particles having a median diameter of greater than 90 microns to repeated stages of wetting with a solvent and drying.
摘要翻译： 用于制备用于通过吸入给药的粉末混合物并且具有大于90微米的中值粒径和表示为小于或等于1.1的分形维数的表面粗糙度的载体颗粒可以通过使具有 中等直径大于90微米，重复使用溶剂润湿阶段并进行干燥。
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公开(公告)号：US20050118113A1
公开(公告)日：2005-06-02
申请号：US10806240
申请日：2004-03-23
CPC分类号： A61K9/0075 , A61K9/145 , A61K9/1623 , Y10T428/2991 , Y10T428/2998
摘要： Carrier particles, for use in the preparation of powdery mixtures for administration by inhalation, and having a median diameter of greater than 90 microns and a surface rugosity expressed as the fractal dimension of less than or equal to 1.1, may be prepared by subjecting particles having a median diameter of greater than 90 microns to repeated stages of wetting with a solvent and drying.
摘要翻译： 用于制备用于通过吸入给药的粉末混合物并且具有大于90微米的中值粒径和表示为小于或等于1.1的分形维数的表面粗糙度的载体颗粒可以通过使具有 中等直径大于90微米，重复使用溶剂润湿阶段并干燥。
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公开(公告)号：US06436443B2
公开(公告)日：2002-08-20
申请号：US09888688
申请日：2001-06-25
申请人： David A. Edwards , Giovanni Caponetti , Jeffrey S. Hrkach , Noah Lotan , Justin Hanes , Robert S. Langer , Abdellaziz Ben-Jebria
发明人： David A. Edwards , Giovanni Caponetti , Jeffrey S. Hrkach , Noah Lotan , Justin Hanes , Robert S. Langer , Abdellaziz Ben-Jebria
IPC分类号： A61K914
CPC分类号： A61K9/0075 , A61K9/1647 , A61K31/137 , Y10S514/826 , Y10S514/851
摘要： Improved porous particles for drug delivery to the pulmonary system, and methods for their synthesis and administration are provided. In a preferred embodiment, the porous particles are made of a biodegradable material and have a mass density less than 0.4 g/cm3/. 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, porous particles having a relatively 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 porous 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.
摘要翻译： 提供用于向肺系统递送药物的改进的多孔颗粒，以及用于其合成和给药的方法。 在优选的实施方案中，多孔颗粒由可生物降解的材料制成，其质量密度小于0.4g / cm 3 /。 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，具有相对大的平均直径，例如大于5um的多孔颗粒可用于增强治疗剂递送至肺的肺泡区域。 掺入治疗剂的多孔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多种治疗剂。
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公开(公告)号：US20080241253A1
公开(公告)日：2008-10-02
申请号：US11867254
申请日：2007-10-04
IPC分类号： A61K9/14
CPC分类号： A61K9/0073 , A61K9/1611 , A61K9/1617
摘要： Particles having a tap density less than about 0.4 g/cm3 are formed by spray drying from a colloidal solution including a carboxylic acid or salt thereof, a phospholipid, a divalent salt and a solvent such as an aqueous-organic solvent. The colloidal solution can also include a therapeutic, prophylactic or diagnostic agent. Preferred carboxylic acids include at least two carboxyl groups. Preferred phospholipids include phosphatidylcholines, phosphatidylethanolamines, phosphatidylglycerols, phophstidylserines, phosphatidylinositols and combinations thereof. The particles are suitable for pulmonary delivery.
摘要翻译： 通过从包含羧酸或其盐，磷脂，二价盐和溶剂如水 - 有机溶剂的胶体溶液喷雾干燥，形成振实密度小于约0.4g / cm 3的颗粒。 胶体溶液还可以包括治疗剂，预防剂或诊断剂。 优选的羧酸包括至少两个羧基。 优选的磷脂包括磷脂酰胆碱，磷脂酰乙醇胺，磷脂酰甘油，磷脂酰丝氨酸，磷脂酰肌醇及其组合。 这些颗粒适用于肺部输送。
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公开(公告)号：US07279182B2
公开(公告)日：2007-10-09
申请号：US10833613
申请日：2004-04-28
CPC分类号： A61K9/0073 , A61K9/1611 , A61K9/1617
摘要： Particles having a tap density less than about 0.4 g/cm3 are formed by spray drying from a colloidal solution including a carboxylic acid or salt thereof, a phospholipid, a divalent salt and a solvent such as an aqueous-organic solvent. The colloidal solution can also include a therapeutic, prophylactic or diagnostic agent. Preferred carboxylic acids include at least two carboxyl groups. Preferred phospholipids include phosphatidylcholines, phosphatidylethanolamines, phosphatidylglycerols, phophstidylserines, phosphatidylinositols and combinations thereof. The particles are suitable for pulmonary delivery.
摘要翻译： 通过从包含羧酸或其盐，磷脂，二价盐和溶剂如水 - 有机溶剂的胶体溶液喷雾干燥，形成振实密度小于约0.4g / cm 3的颗粒。 胶体溶液还可以包括治疗剂，预防剂或诊断剂。 优选的羧酸包括至少两个羧基。 优选的磷脂包括磷脂酰胆碱，磷脂酰乙醇胺，磷脂酰甘油，磷脂酰丝氨酸，磷脂酰肌醇及其组合。 这些颗粒适用于肺部输送。
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20.发明申请Dry Powder Pharmaceutical Composition, Its Preparation Process and Stable Aqueous Suspension Obtained from Such Composition 有权干粉药物组合物，其制备方法和由这种组合物获得的稳定的水悬浮液公开(公告)号：US20070224276A1
公开(公告)日：2007-09-27
申请号：US11578661
申请日：2005-04-21
IPC分类号： A61K9/16
CPC分类号： A61K9/145 , A61K9/0075 , A61K9/0078 , A61K9/14 , A61K9/143 , A61K31/192 , A61K31/573 , A61K31/58
摘要： Pharmaceutical composition in a dry powder form comprising at least one hydrophobic active principle, at least one water-soluble excipient and at least one surfactant, wherein the particles in said dry powder state have a Volume Mean Diameter VMDd greater than the Volume Mean Diameter VMDw of particles in a suspension obtained from said pharmaceutical composition at standard conditions of dispersion in a water-medium. It is also disclosed a process to prepare such dry composition and an extemporaneous suspension for inhalation therapy obtainable from said dry composition.
摘要翻译： 包含至少一种疏水活性成分，至少一种水溶性赋形剂和至少一种表面活性剂的干粉形式的药物组合物，其中所述干燥粉末状态的颗粒具有体积平均直径VMD < 大于在水介质中在标准条件下从所述药物组合物获得的悬浮液中的颗粒的体积平均直径VMD 。 还公开了制备这种干组合物和可从所述干组合物获得的用于吸入治疗的临时悬浮液的方法。
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