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    SUSTAINED-RELEASE COMPOSITION AND METHOD OF USE THEREOF
    1.
    发明申请
    SUSTAINED-RELEASE COMPOSITION AND METHOD OF USE THEREOF 审中-公开
    持续释放组合物及其使用方法

    公开(公告)号：US20080139655A1

    公开(公告)日：2008-06-12

    申请号：US11850063

    申请日：2007-09-05

    申请人： Jonathan Bortz ,  Michael Grimshaw ,  David F. Erkoboni ,  Michael F. Dickus

    发明人： Jonathan Bortz ,  Michael Grimshaw ,  David F. Erkoboni ,  Michael F. Dickus

    IPC分类号： A61K31/195 ,  A61P25/28

    CPC分类号： A61K31/198 ,  A61K9/0065 ,  A61K9/205 ,  A61K9/2054

    摘要： A pharmaceutical composition comprising levodopa is provided that, when administered in a unit dosage amount of levodopa of about 100 to about 500 mg at a dosage interval of about 6 to about 24 hours, exhibits a sufficiently long release period and a sufficiently long residence time in the upper gastrointestinal tract to provide a trough concentration of levodopa in plasma of the subject that is not lower than a minimum threshold concentration below which adverse motor effects are observed in the subject. A method for treating Parkinson's disease in a subject is also provided, comprising orally administering such a composition to the subject in a unit dosage amount of levodopa of about 50 to about 1000 mg at a dosage interval of about 3 to about 24 hours.

    摘要翻译： 提供包含左旋多巴的药物组合物，其以约6至约24小时的剂量间隔以约100至约500mg的单位剂量的左旋多巴施用时，显示足够长的释放期和足够长的停留时间 上消化道提供受试者血浆中左旋多巴的谷浓度，其不低于在受试者中观察到不良运动效应的最低阈值浓度。 还提供了治疗受试者中帕金森病的方法，其包括以约3至约24小时的剂量间隔以约50至约1000mg的单位剂量的左旋多巴口服施用该组合物。

    Method of making granular pharmaceutical vehicle
    6.
    发明授权
    Method of making granular pharmaceutical vehicle 失效
    制造颗粒药物载体的方法

    公开(公告)号：US06379707B2

    公开(公告)日：2002-04-30

    申请号：US09886100

    申请日：2001-06-21

    申请人： Ronald S. Vladyka, Jr. ,  David F. Erkoboni ,  Pamela R. Stergios

    发明人： Ronald S. Vladyka, Jr. ,  David F. Erkoboni ,  Pamela R. Stergios

    IPC分类号： A61K916

    CPC分类号： A61K9/145 ,  A61K9/1617 ,  A61K9/1652 ,  A61K31/496 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： A formulation of a sparingly water-soluble, crystalline pharmaceutically active agent wherein the active agent is converted to and stabilized in its amorphous form as a solid solution of a normally hydrophobic vehicle is described. The amorphous state is stabilized by the composition of the formulation, providing long shelf life of the improved composition. This stabilized formulation also provides increased solubility and bioavailability of the active agent. Solutions of the active agent are stabilized by the composition, preventing recrystallization and precipitation of the less soluble, crystalline form of the active agent from aqueous solutions thereof.

    摘要翻译： 描述了一种微溶于水的结晶药物活性剂的制剂，其中活性剂以正常疏水性载体的固体溶液转化为其非晶形式并稳定化。 无定形状态通过制剂的组成稳定，提供改进的组合物的长的保质期。 这种稳定化的制剂还提供活性剂的增加的溶解度和生物利用度。 活性剂的溶液通过组合物稳定，防止活性剂从其水溶液中的较不溶解的结晶形式的再结晶和沉淀。

    Hydrolyzed cellulose granulations of salts of drugs
    7.
    发明授权
    Hydrolyzed cellulose granulations of salts of drugs 失效
    药物盐水解纤维素颗粒

    公开(公告)号：US06596312B1

    公开(公告)日：2003-07-22

    申请号：US09669533

    申请日：2000-09-26

    申请人： David F. Erkoboni ,  Ronald S. Vladyka, Jr. ,  Christopher A. Sweriduk ,  Andrew J. Favara

    发明人： David F. Erkoboni ,  Ronald S. Vladyka, Jr. ,  Christopher A. Sweriduk ,  Andrew J. Favara

    IPC分类号： A61K920

    CPC分类号： A61K9/1652 ,  A61K9/2054

    摘要： The present invention provides a method for preparing a spray-dried, compressible granular formulation for preparing pharmaceutical tablets in which essentially water-insoluble, acidic, amphoteric, and basic pharmaceutically active agents are converted to more water-soluble salts which are granulated with hydrolyzed cellulose, drug-containing slurries, the resulting granulations, capsules containing granulations, and pharmaceutical tablets compressed from such granules. In these formulations there is employed from 1% to 85% by weight of the pharmaceutically active agent and its salt form, from 5% to 99% of hydrolyzed cellulose, based on the dry weight of the granulation, and optionally, conventional granulation and/or tableting additives such as surfactants, disintegrants, and antiadherents/flow aids. Said tablets have significantly increased dissolution of the pharmaceutically active agent at the pH of the gastrointestinal tract in comparison with the unconverted free pharmaceutically active agent.

    摘要翻译： 本发明提供了一种制备用于制备药物片剂的喷雾干燥的可压缩颗粒制剂的方法，其中基本上不溶于水的，酸性的，两性的和碱性的药物活性剂转化为更多的水溶性盐，其被水解的纤维素 ，含药浆液，所得颗粒，含有颗粒的胶囊和从该颗粒压制的药物片剂。 在这些制剂中，基于造粒物的干重，使用1％至85％重量的药学活性剂及其盐形式，5％至99％的水解纤维素，以及任选的常规制粒和/ 或压片添加剂如表面活性剂，崩解剂和抗粘附剂/流动助剂。 与未转化的游离药物活性剂相比，所述片剂在胃肠道的pH下显着增加药物活性剂的溶出度。