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    Once-daily administration of central nervous system drugs
    1.
    发明申请
    Once-daily administration of central nervous system drugs 审中-公开
    每日一次中枢神经系统药物

    公开(公告)号：US20070104788A1

    公开(公告)日：2007-05-10

    申请号：US11594876

    申请日：2006-11-09

    申请人： Seamus Mulligan

    发明人： Seamus Mulligan

    IPC分类号： A61K9/22

    CPC分类号： A61K9/5026 ,  A61K9/5073 ,  A61K31/135

    摘要： Delayed onset chronotherapeutic formulations of central nervous system (CNS) drugs are disclosed. The formulations comprise at least one CNS drug or pharmaceutically acceptable salt thereof that exhibits an in vivo elimination half-life of less than about 8 hours, wherein the formulation exhibits at least one in vivo parameter, at steady state following administration to a subject, chosen from: an initial lag in absorption from about 2 hours to about 6 hours; a peak-to-trough ratio greater than or equal to about 4:1; a percent fluctuation of greater than or equal to about 100%; and a minimum time cover of greater than or equal to 50% of Cmax of at least 8 hours.

    摘要翻译： 公布了中枢神经系统（CNS）药物延迟发作的时间治疗剂型。 所述制剂包含至少一种CNS药物或其药学上可接受的盐，其表现出体内消除半衰期小于约8小时，其中所述制剂在施用于受试者后在稳定状态下显示至少一种体内参数，所述体内参数选择 从：从约2小时到约6小时的吸收的初始滞后; 峰谷比大于或等于约4：1; 百分比波动大于或等于约100％; 并且至少8小时的C max的大于或等于50％的最小时间覆盖。

    Controlled absorption diltiazem formulation for once daily administration
    3.
    发明授权
    Controlled absorption diltiazem formulation for once daily administration 失效
    受控吸收地尔硫卓制剂每日一次给药

    公开(公告)号：US5364620A

    公开(公告)日：1994-11-15

    申请号：US921459

    申请日：1992-07-28

    申请人： Edward J. Geoghegan ,  Seamus Mulligan ,  Donald E. Panoz

    发明人： Edward J. Geoghegan ,  Seamus Mulligan ,  Donald E. Panoz

    IPC分类号： A61K9/50 ,  A61K31/55 ,  A61K31/554 ,  A61K9/16

    CPC分类号： A61K31/55 ,  A61K31/554 ,  A61K9/5078 ,  A61K9/5084

    摘要： A diltiazem pellet formulation for oral administration comprises a core of diltiazem or a pharmaceutically acceptable salt thereof in association with an organic acid, and a multi-layer membrane surrounding the core and containing a major proportion of a pharmaceutically acceptable film-forming, water insoluble synthetic polymer and a minor proportion of a pharmaceutically acceptable film-forming, water soluble synthetic polymer. The number of layers in the membrane and the ratio of the water soluble to water insoluble polymer being effective to permit release of the diltiazem from the pellet at a rate allowing controlled absorption thereof over a twenty four hour period following oral administration.

    摘要翻译： 用于口服给药的地尔硫卓丸剂制剂包含与有机酸结合的地尔硫卓核心或其药学上可接受的盐，以及包围核心的多层膜，并含有主要比例的药学上可接受的成膜水不溶性合成 聚合物和较小比例的药学上可接受的成膜水溶性合成聚合物。 膜中的层数和水溶性与水不溶性聚合物的比例有效地允许从口服释放二氧化硫以粒子的速度允许其控制吸收二十四小时。

    Diltiazem formulations and methods of treatment
    4.
    发明授权
    Diltiazem formulations and methods of treatment 失效
    地尔硫配方及治疗方法

    公开(公告)号：US5336504A

    公开(公告)日：1994-08-09

    申请号：US64401

    申请日：1993-05-19

    申请人： Edward J. Geoghegan ,  Seamus Mulligan ,  Donald E. Panoz

    发明人： Edward J. Geoghegan ,  Seamus Mulligan ,  Donald E. Panoz

    IPC分类号： A61K9/50 ,  A61K9/58 ,  A61K31/55 ,  A61K9/16

    CPC分类号： A61K31/55 ,  A61K9/5078 ,  Y10S514/821

    摘要： A diltiazem pellet formulation for oral administration comprises a core of diltiazem or a pharmaceutically acceptable salt thereof in association with an organic acid, and a multi-layer membrane surrounding the core and containing a major proportion of a pharmaceutically acceptable film-forming, water insoluble synthetic polymer and a minor proportion of a pharmaceutically acceptable film-forming, water soluble synthetic polymer. The number of layers in the membrane and the ratio of the water soluble to water insoluble polymer being effective to permit release of diltiazem from the pellet at a rate allowing controlled absorption thereof over a twelve hour period following oral administration. The pellet has a dissolution rate in vitro which when measured in a dissolution apparatus (Paddle) according to U.S. Pharmacopoeia XXI in 0.05 M KC1 at pH 7.0 results in not more than 35% of the total diltiazem being released after 2 hours of measurement. Not more than 80% of the total diltiazem is released after six hours of measurement and not less than 85% of the total diltiazem is released after 13 hours of measurement.

    摘要翻译： 用于口服给药的地尔硫卓丸剂制剂包含与有机酸结合的地尔硫卓核心或其药学上可接受的盐，以及包围核心的多层膜，并含有主要比例的药学上可接受的成膜水不溶性合成 聚合物和较小比例的药学上可接受的成膜水溶性合成聚合物。 膜中的层数以及水溶性与水不溶性聚合物的比例有效地允许从口服释放硫酸盐，以允许其在口服给药后12小时内受控吸收的速率。 颗粒体外具有溶解速率，当根据美国药典XXI在pH 7.0的0.05M KCl中的溶出装置（桨）中测量时，在测量2小时后不超过35％的总硫酸盐地被释放。 在测量6小时后，不超过总量的地尔硫卓的80％被释放，并且在13小时的测量后不少于85％的总硫酸盐被释放。

    Methods of treatment with diltiazem formulations
    5.
    发明授权
    Methods of treatment with diltiazem formulations 失效
    用地尔硫卓制剂治疗的方法

    公开(公告)号：US5219621A

    公开(公告)日：1993-06-15

    申请号：US918925

    申请日：1992-07-22

    申请人： Edward J. Geoghegan ,  Seamus Mulligan ,  Donald E. Panoz

    发明人： Edward J. Geoghegan ,  Seamus Mulligan ,  Donald E. Panoz

    IPC分类号： A61K9/50 ,  A61K31/55

    CPC分类号： A61K9/5078 ,  A61K31/55 ,  Y10S514/821

    摘要： A diltiazem pellet formulation for oral administration comprises a core of diltiazem or a pharmaceutically acceptable salt thereof in association with an organic acid, and a multi-layer membrane surrounding the core and containing a major proportion of a pharmaceutically acceptable film-forming, water insoluble synthetic polymer and a minor proportion of a pharmaceutically acceptable film-forming, water soluble synthetic polymer. The number of layers in the membrane and the ratio of the water soluble to water insoluble polymer being effective to permit release of diltiazem from the pellet at a rate allowing controlled absorption thereof over a twelve hour period following oral administration. The pellet has a dissolution rate in vitro which when measured in a dissolution apparatus (Paddle) according to U.S. Pharmacopoeia XXI in 0.05 M KCl at pH 7.0 results in not more than 35% of the total diltiazem being released after 2 hours of measurement. Not more than 80% of the total diltiazem is released after six hours of measurement and not less than 85% of the total diltiazem is released after 13 hours of measurement.

    摘要翻译： 用于口服给药的地尔硫卓丸剂制剂包含与有机酸结合的地尔硫卓核心或其药学上可接受的盐，以及包围核心的多层膜，并含有主要比例的药学上可接受的成膜水不溶性合成 聚合物和较小比例的药学上可接受的成膜水溶性合成聚合物。 膜中的层数以及水溶性与水不溶性聚合物的比例有效地允许从口服释放硫酸盐，以允许其在口服给药后12小时内受控吸收的速率。 颗粒体外具有溶解速率，当根据美国药典XXI在0.05M KCl中在pH7.0下的溶解装置（桨）中测量时，在测量2小时后不超过35％的总硫酸盐地被释放。 在测量6小时后，不超过总量的地尔硫卓的80％被释放，并且在13小时的测量后不少于85％的总硫酸盐被释放。

    SUSTAINED RELEASE AMINOPYRIDINE COMPOSITION
    7.
    发明申请
    SUSTAINED RELEASE AMINOPYRIDINE COMPOSITION 审中-公开
    持续释放氨基吡啶组合物

    公开(公告)号：US20130045276A1

    公开(公告)日：2013-02-21

    申请号：US13585277

    申请日：2012-08-14

    申请人： Sean Cunningham ,  Seamus Mulligan ,  Michael Myers

    发明人： Sean Cunningham ,  Seamus Mulligan ,  Michael Myers

    IPC分类号： A61K9/22 ,  A61P25/00 ,  A61P25/28 ,  A61K31/4409

    CPC分类号： A61K31/4409 ,  A61K9/20 ,  A61K9/2054 ,  A61K9/2077 ,  A61K31/44 ,  A61K47/12 ,  A61K47/14 ,  A61K47/38 ,  A61K47/44

    摘要： A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hours or more and the use of the composition to treat various neurological diseases.

    摘要翻译： 一种药物组合物，其包含分散在释放基质中的治疗有效量的氨基吡啶，包括例如可以配制成稳定的持续释放口服剂量制剂的组合物，例如在给药至 患者，氨基吡啶的治疗有效血浆水平至少12小时，优选24小时或更长的时间，以及该组合物用于治疗各种神经疾病的用途。

    METHOD FOR TITRATING CLOZAPINE
    8.
    发明申请
    METHOD FOR TITRATING CLOZAPINE 审中-公开
    用于治疗CLOZAPINE的方法

    公开(公告)号：US20110172210A1

    公开(公告)日：2011-07-14

    申请号：US12987660

    申请日：2011-01-10

    申请人： Seamus MULLIGAN ,  Fintan KEEGAN

    发明人： Seamus MULLIGAN ,  Fintan KEEGAN

    IPC分类号： A61K31/551 ,  A61P25/18

    CPC分类号： A61K31/5513

    摘要： Method for titrating clozapine in treatment of psychotic disorders in a human patient in need of treatment with clozapine including administering once-a-day controlled release clozapine to the human patient titrating to a therapeutic dose of clozapine within a period of less than one week, or administering controlled release clozapine to the patient at an initial dose of at least 37.5 mg and titrating to a therapeutic dose within a period of less than ten days.

    摘要翻译： 在需要用氯氮平治疗的人类患者中滴定氯氮平治疗精神病的方法，包括每日一次氯地普控制氯沙平治疗剂量在不到一周的时间内滴定至治疗剂量的氯氮平，或 以至少37.5mg的初始剂量向患者施用控释氯氮平，并在少于10天的时间内滴定至治疗剂量。