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    Pharmaceutical formulation comprising a water-insoluble active agent
    2.
    发明授权
    Pharmaceutical formulation comprising a water-insoluble active agent 有权
    包含水不溶性活性剂的药物制剂

    公开(公告)号：US08668934B2

    公开(公告)日：2014-03-11

    申请号：US12953259

    申请日：2010-11-23

    申请人： Reinhard Vehring ,  Danforth P Miller ,  David Lechuga-Ballesteros

    发明人： Reinhard Vehring ,  Danforth P Miller ,  David Lechuga-Ballesteros

    IPC分类号： A61K9/00 ,  A61K9/12 ,  A61P31/00 ,  A61P29/00 ,  A61P11/00

    CPC分类号： A61K9/0075 ,  A61K9/1617 ,  A61K9/167 ,  A61K9/1694 ,  A61K9/5015 ,  A61K9/5089 ,  A61K31/00

    摘要： A method of preparing a pharmaceutical formulation comprises providing a solution comprising a first solvent, a second solvent, an active agent, and an excipient. The second solvent is less polar than the first solvent and the excipient is more soluble in water than the active agent. The first and second solvents are removed from the solution to produce particles comprising the active agent and the excipient. In one version, the excipient comprises an amino acid and/or a phospholipid. A pharmaceutical formulation made by a version of the invention comprises particles comprising an active agent and an excipient which at least partially encapsulates the active agent, wherein the excipient is more soluble in water than the active agent.

    摘要翻译： 制备药物制剂的方法包括提供包含第一溶剂，第二溶剂，活性剂和赋形剂的溶液。 第二溶剂的极性比第一溶剂少，赋形剂比活性剂更易溶于水。 从溶液中除去第一和第二溶剂以产生包含活性剂和赋形剂的颗粒。 在一个版本中，赋形剂包含氨基酸和/或磷脂。 由本发明版本制成的药物制剂包含包含至少部分包封活性剂的活性剂和赋形剂的颗粒，其中赋形剂比活性剂更易溶于水。

    PHARMACEUTICAL FORMULATION COMPRISING A WATER-INSOLUBLE ACTIVE AGENT
    4.
    发明申请
    PHARMACEUTICAL FORMULATION COMPRISING A WATER-INSOLUBLE ACTIVE AGENT 有权
    包含水不溶性活性剂的药物制剂

    公开(公告)号：US20110070309A1

    公开(公告)日：2011-03-24

    申请号：US12953259

    申请日：2010-11-23

    申请人： Reinhard Vehring ,  Danforth P. Miller ,  David Lechuga-Ballesteros

    发明人： Reinhard Vehring ,  Danforth P. Miller ,  David Lechuga-Ballesteros

    IPC分类号： A61K9/14 ,  A61K47/44 ,  A61K9/00 ,  A61K9/12 ,  A61P31/00 ,  A61P29/00 ,  A61P11/00 ,  A61P9/00 ,  A61P25/00 ,  B29B9/16

    CPC分类号： A61K9/0075 ,  A61K9/1617 ,  A61K9/167 ,  A61K9/1694 ,  A61K9/5015 ,  A61K9/5089 ,  A61K31/00

    摘要： A method of preparing a pharmaceutical formulation comprises providing a solution comprising a first solvent, a second solvent, an active agent, and an excipient. The second solvent is less polar than the first solvent and the excipient is more soluble in water than the active agent. The first and second solvents are removed from the solution to produce particles comprising the active agent and the excipient. In one version, the excipient comprises an amino acid and/or a phospholipid. A pharmaceutical formulation made by a version of the invention comprises particles comprising an active agent and an excipient which at least partially encapsulates the active agent, wherein the excipient is more soluble in water than the active agent.

    摘要翻译： 制备药物制剂的方法包括提供包含第一溶剂，第二溶剂，活性剂和赋形剂的溶液。 第二溶剂的极性比第一溶剂少，赋形剂比活性剂更易溶于水。 从溶液中除去第一和第二溶剂以产生包含活性剂和赋形剂的颗粒。 在一个版本中，赋形剂包含氨基酸和/或磷脂。 由本发明版本制成的药物制剂包含包含至少部分包封活性剂的活性剂和赋形剂的颗粒，其中赋形剂比活性剂更易溶于水。

    Chemically Modified Small Molecules
    10.
    发明申请
    Chemically Modified Small Molecules 有权
    化学改性的小分子

    公开(公告)号：US20100210676A1

    公开(公告)日：2010-08-19

    申请号：US12710167

    申请日：2010-02-22

    申请人： C. Simone Fishburn ,  David Lechuga-Ballesteros ,  Tacey Viegas ,  Mei-Chang Kuo ,  Yuan Song ,  Hema Gursahani ,  Chester Leach

    发明人： C. Simone Fishburn ,  David Lechuga-Ballesteros ,  Tacey Viegas ,  Mei-Chang Kuo ,  Yuan Song ,  Hema Gursahani ,  Chester Leach

    IPC分类号： A61K31/485 ,  A61P25/36

    CPC分类号： A61K9/007 ,  A61K31/167 ,  A61K31/485 ,  A61K47/60 ,  C07C41/24

    摘要： Methods of modifying the rate of systemic absorption of a drug administered to a subject by a pulmonary route, the method comprising covalently conjugating a hydrophilic polymer to a drug, wherein the drug has a half-life of elimination from the lung of less than about 180 minutes, to form a drug-polymer conjugate, wherein the drug-polymer conjugate has a net hydrophilic character and a weight average molecular weight of from about 50 to about 20,000 Daltons, and wherein the half-life of elimination from the lung of the drug-polymer conjugate is at least about 1.5-fold greater than the half-life of elimination from the lung of the drug, wherein the half-life of elimination from the lung is measured by bronchoalveolar lavage followed by assaying residual lung material.

    摘要翻译： 通过肺途径改变施用于受试者的药物的全身吸收速率的方法，所述方法包括将亲水性聚合物与药物共价共轭，其中所述药物具有从肺中消除的半衰期小于约180 分钟，以形成药物 - 聚合物缀合物，其中药物 - 聚合物缀合物具有净亲水特性和约50至约20,000道尔顿的重均分子量，并且其中从药物的肺中消除的半衰期 - 聚合物缀合物比从药物肺消除的半衰期大至少约1.5倍，其中通过支气管肺泡灌洗测量肺部消除的半衰期，然后测定残留的肺部材料。