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1. 发明申请

WO2018186866A1 SUSTAINED RELEASE COMPOSITIONS OF 4-AMINOPYRIDINE 审中-公开
公开(公告)号：WO2018186866A1
公开(公告)日：2018-10-11
申请号：PCT/US2017/026360
申请日：2017-04-06
申请人： COBB, Joseph, E., Jr. , GOLD, Thomas, B. , D'SOUZA, Rohini , WAY, Susan, L.
发明人： COBB, Joseph, E., Jr. , GOLD, Thomas, B. , D'SOUZA, Rohini , WAY, Susan, L.
IPC分类号： A61K9/28 , A61K31/44
摘要： The present invention generally relates to sustained release 4-aminopyridine tablets, which include a core and a coating. The sustained release tablets of the invention are generally suitable for once daily oral administration for the treatment of neurological disorders.

2. 发明申请

WO2007014061A2 COATED TABLES WITH ZERO-ORDER OR NEAR ZERO-ORDER RELEASE KINETICS 审中-公开
标题翻译：带有零订单或零零排放动态的涂层表
公开(公告)号：WO2007014061A2
公开(公告)日：2007-02-01
申请号：PCT/US2006/028447
申请日：2006-07-21
申请人： METRICS, INC. , GOLD, Thomas, B. , WOODAL, Patrick, Brian
发明人： GOLD, Thomas, B. , WOODAL, Patrick, Brian
IPC分类号： A61K9/20
CPC分类号： A61K9/2031 , A61K9/2866
摘要： Tablets for the controlled release of an active ingredient in a zero-order or near zero-order fashion are provided. The tablet includes a core and a coating. The core includes at least one active pharmaceutical agent and a polyethylene oxide with a molecular weight of between about 1,000,000 and 10,000,000, preferably between about 4,000,000 and 8,000,000. The core material is optionally, but preferably, coated with a cellulosic material. The active pharmaceutical agent can be hydrophilic, hydrophobic, or amphiphilic. When the active pharmaceutical agent is a hydrophilic agent, it is preferred that the coating is a relatively hydrophobic cellulose, such as ethylcellulose or propylcellulose. However, if the tablet is uncoated, it can provide a near-zero-order release rate rather than a zero-order release rate. When the active pharmaceutical agent is a hydrophobic or amphiphilic agent, the hydrophilic polymeric carrier is the same as in the first embodiment, the coating is a relatively more hydrophilic cellulose. The release rate for the active pharmaceutical agent can be controlled by adjusting the thickness of the coating, and, optionally, by adjusting the concentration of the polymeric excipients, as well as certain non-polymeric excipients which may optionally be present. An advantage of using relatively high molecular weight polyethylene oxide is that the release is pH independent, unlike where ionic polymers such as polyacrylic acids are used. Further, active pharmaceutical agents including functional groups that might react with such polymers can be used without an adverse reaction between the active agent and the polymer.
摘要翻译：提供以零级或接近零级方式控制释放活性成分的片剂。片剂包括芯和涂层。核心包括至少一种活性药剂和分子量为约1,000,000至10,000,000，优选约4,000,000至8,000,000的聚环氧乙烷。核心材料是任选的，但优选地涂覆有纤维素材料。活性药剂可以是亲水的，疏水的或两亲的。当活性药剂是亲水剂时，优选涂层是相对疏水的纤维素，例如乙基纤维素或丙基纤维素。然而，如果平板电脑是未涂覆的，则它可以提供接近零级的释放速率而不是零级释放速率。当活性药剂是疏水性或两亲性剂时，亲水性聚合物载体与第一实施方案相同，涂层是相对较亲水的纤维素。活性药剂的释放速率可以通过调节涂层的厚度和任选地通过调节聚合物赋形剂的浓度以及可任选存在的某些非聚合物赋形剂来控制。使用相对高分子量的聚环氧乙烷的优点在于，与使用离子聚合物如聚丙烯酸不同，其释放是不依赖于pH的。此外，可以使用包括可能与这种聚合物反应的官能团的活性药剂，而不会在活性剂和聚合物之间产生不良反应。

3. 发明申请

WO2007014061A3 COATED TABLES WITH ZERO-ORDER OR NEAR ZERO-ORDER RELEASE KINETICS 审中-公开
标题翻译：带零级或零零排放动态的涂层表
公开(公告)号：WO2007014061A3
公开(公告)日：2009-04-16
申请号：PCT/US2006028447
申请日：2006-07-21
申请人： METRICS INC , GOLD THOMAS B , WOODAL PATRICK BRIAN
发明人： GOLD THOMAS B , WOODAL PATRICK BRIAN
IPC分类号： A61K9/20
CPC分类号： A61K9/2031 , A61K9/2866
摘要： Tablets for the controlled release of an active ingredient in a zero-order or near zero-order fashion are provided. The tablet includes a core and a coating. The core includes at least one active pharmaceutical agent and a polyethylene oxide with a molecular weight of between about 1,000,000 and 10,000,000, preferably between about 4,000,000 and 8,000,000. The core material is optionally, but preferably, coated with a cellulosic material. The active pharmaceutical agent can be hydrophilic, hydrophobic, or amphiphilic. When the active pharmaceutical agent is a hydrophilic agent, it is preferred that the coating is a relatively hydrophobic cellulose, such as ethylcellulose or propylcellulose. However, if the tablet is uncoated, it can provide a near-zero-order release rate rather than a zero-order release rate. When the active pharmaceutical agent is a hydrophobic or amphiphilic agent, the hydrophilic polymeric carrier is the same as in the first embodiment, the coating is a relatively more hydrophilic cellulose. The release rate for the active pharmaceutical agent can be controlled by adjusting the thickness of the coating, and, optionally, by adjusting the concentration of the polymeric excipients, as well as certain non-polymeric excipients which may optionally be present. An advantage of using relatively high molecular weight polyethylene oxide is that the release is pH independent, unlike where ionic polymers such as polyacrylic acids are used. Further, active pharmaceutical agents including functional groups that might react with such polymers can be used without an adverse reaction between the active agent and the polymer.
摘要翻译：提供了以零级或接近零级方式控制释放活性成分的片剂。片剂包括芯和涂层。核心包括至少一种活性药剂和分子量为约1,000,000至10,000,000，优选约4,000,000至8,000,000的聚环氧乙烷。核心材料是任选的，但优选地涂覆有纤维素材料。活性药剂可以是亲水的，疏水的或两亲的。当活性药剂是亲水剂时，优选涂层是相对疏水的纤维素，例如乙基纤维素或丙基纤维素。然而，如果平板电脑是未涂覆的，则它可以提供接近零级的释放速率而不是零级释放速率。当活性药剂是疏水性或两亲性剂时，亲水性聚合物载体与第一实施方案相同，涂层是相对较亲水的纤维素。活性药剂的释放速率可以通过调节涂层的厚度和任选地通过调节聚合物赋形剂的浓度以及可任选存在的某些非聚合物赋形剂来控制。使用相对高分子量的聚环氧乙烷的优点在于，与使用离子聚合物如聚丙烯酸不同，其释放是不依赖于pH的。此外，可以使用包括可能与这种聚合物反应的官能团的活性药剂，而不会在活性剂和聚合物之间产生不良反应。

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