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    Controlled absorption diltiazem formulations
    2.
    发明授权
    Controlled absorption diltiazem formulations 失效
    受控吸收地尔硫卓制剂

    公开(公告)号：US5002776A

    公开(公告)日：1991-03-26

    申请号：US273192

    申请日：1988-11-18

    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： A61K31/554 ,  A61K31/55 ,  A61K9/5078 ,  A61K9/5084

    摘要： A controlled absorption 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 optionally 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, when said water soluble polymer is present, being effective to permit release of diltiazem from the pellet at a rate allowing controlled absorption thereof over not less than 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 60% of the total diltiazem is released after four hours of measurement and 100% of the diltiazem is released no earlier than after 8 hours of measurement in said apparatus.

    摘要翻译： 用于口服给药的受控吸收性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，并且含有主要比例的药学上可接受的成膜水不溶性 合成聚合物和任选的少量可药用成膜的水溶性合成聚合物。 当所述水溶性聚合物存在时，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沉淀物中释放硫氮，其速率允许其控制吸收不小于十二分之一 口服后小时。 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溶液装置（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4小时后，不超过60％的总硫酸化合物被释放，并且100％的地尔硫卓在所述装置中测定8小时后不会释放。

    Controlled absorption diltiazem formulation
    3.
    发明授权
    Controlled absorption diltiazem formulation 失效
    受控吸收地尔硫卓制剂

    公开(公告)号：US4917899A

    公开(公告)日：1990-04-17

    申请号：US121224

    申请日：1987-11-16

    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

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

    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 lubricant, and a membrane surrounding the core comprising a multiplicity of sequentially applied and dried layers, each layer containing a major proportion of a pharmaceutically acceptable film-forming, water insoluble, naturally occurring polymer and a minor proportion of a pharmaceutically acceptable film-forming, water soluble 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 twelve 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和润滑剂相关的地尔硫卓核心或其药学上可接受的盐，以及围绕芯的膜，包含多个顺序施加和干燥的层，每层包含主要比例 的药学上可接受的成膜的水不溶性天然存在的聚合物和较小比例的药学上可接受的成膜的水溶性聚合物。 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以口服给药后12小时内允许其受控吸收的速率从沉淀中释放地尔硫卓。

    Controlled absorption pharmaceutical formulation
    4.
    发明授权
    Controlled absorption pharmaceutical formulation 失效
    受控吸收药物制剂

    公开(公告)号：US4826688A

    公开(公告)日：1989-05-02

    申请号：US930138

    申请日：1986-11-12

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

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

    IPC分类号： A61K9/30 ,  A61K9/22 ,  A61K9/50 ,  A61K31/49 ,  A61K9/52

    CPC分类号： A61K31/49 ,  A61K9/5078

    摘要： A controlled absorption quinidine formulation for oral administration comprises a pellet having a core of quinidine or a pharmaceutically acceptable salt thereof in association with an organic acid and optionally other excipients, and an outer membrane which permits release of quinidine in an aqueous medium at a controlled rate which is substantially pH independent. The pellet has a dissolution rate in vitro, which when measured in a Basket Assembly according to U.S. Pharmacopoeia XXI at 37.degree. C. and 75 r.p.m. is not more than 15% after one hour of measurement. Not more than 50% of the total quinidine is release after a total of 4 hours of measurement, not more than 80% is released after a total of 8 hours of measurement and not less than 90% release is achieved after a total of 24 hours.

    摘要翻译： 用于口服给药的对照吸收奎尼丁制剂包括与有机酸和任选的其它赋形剂结合的具有奎尼丁核心或其药学上可接受的盐的丸剂和允许以受控速率在水性介质中释放奎尼丁的外膜 其基本上不依赖于pH。 丸在体外具有溶解速率，当根据美国药典XXI在37℃和75r.p.m。 在测量1小时后不超过15％。 总计4小时不超过总奎尼丁的50％，总共8小时后不超过80％，总共24小时后不得少于90％释放 。

    Controlled absorption diltiazem formulation for once-daily administration
    7.
    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：US4894240A

    公开(公告)日：1990-01-16

    申请号：US121225

    申请日：1987-11-16

    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

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

    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。

    Controlled absorption diltiazen pharmaceutical formulation
    10.
    发明授权
    Controlled absorption diltiazen pharmaceutical formulation 失效
    受控吸收剂diltiazen药物制剂

    公开(公告)号：US4721619A

    公开(公告)日：1988-01-26

    申请号：US684661

    申请日：1984-12-20

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

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

    IPC分类号： C07D281/10 ,  A61K9/00 ,  A61K9/16 ,  A61K9/22 ,  A61K9/48 ,  A61K9/50 ,  A61K9/52 ,  A61K9/62 ,  A61K31/55 ,  A61K31/554 ,  A61P3/00 ,  A61P9/08 ,  A61P9/10 ,  A61K9/58

    CPC分类号： A61K9/5078 ,  A61K31/55 ,  A61K31/554 ,  Y10S514/965

    摘要： A controlled absorption diltiazem formulation for oral administration comprises a pellet having a core of diltiazem or a pharmaceutically acceptable salt thereof in association with an organic acid and a lubricant, and an outer membrane which permits release of diltiazem in an aqueous medium at a controlled rate which is substantially pH independent. The pellet has a dissolution rate in vitro, which when measured according to the Paddle Method of U.S. Pharmacopoeia XX, is not more than 10% of the total diltiazem after 2 hours of measurement in a buffered medium. Not more than 30% of the total diltiazem is released after a total of 4 hours measurement and not more than 40% of the total diltiazem is released after a total of 6 hours. 100% release is achieved after 12 hours, with a maximum of 80% of the total diltiazem being released after 8 hours.

    摘要翻译： 用于口服给药的受控吸收性地尔硫卓制剂包含与有机酸和润滑剂结合的具有地尔硫卓核心或其药学上可接受的盐的颗粒，以及外部膜，其允许以水平的控制速率在水性介质中释放地尔硫卓 基本上与pH无关。 颗粒在体外具有溶解速率，当根据美国药典XX的桨法测量时，其在缓冲介质中测量2小时后不超过总的地尔硫卓的10％。 在总共4小时测量后，不超过总量的地尔硫卓的30％被释放，总共6小时后，不超过40％的总硫酸盐地被释放。 12小时后达到100％的释放，8小时后最多可以释放总硫丹毒素的80％。