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1. 发明申请

WO2009092601A1 PHARMACEUTICAL DOSAGE FORM 审中-公开
标题翻译：药物剂型
公开(公告)号：WO2009092601A1
公开(公告)日：2009-07-30
申请号：PCT/EP2009/000438
申请日：2009-01-23
申请人： GRÜNENTHAL GMBH , JANS, Eugeen, Marie, Jozef , KIEKENS, Filip, René, Irena , VOORSPOELS, Jody, Firmin, Marceline , FAURE, Anne , ARKENAU-MARIC, Elisabeth , BARNSCHEID, Lutz , BARTHOLOMÄUS, Johannes , FREVEL, Marc , GALIA, Eric , ZIEGLER, Iris
发明人： JANS, Eugeen, Marie, Jozef , KIEKENS, Filip, René, Irena , VOORSPOELS, Jody, Firmin, Marceline , FAURE, Anne , ARKENAU-MARIC, Elisabeth , BARNSCHEID, Lutz , BARTHOLOMÄUS, Johannes , FREVEL, Marc , GALIA, Eric , ZIEGLER, Iris
IPC分类号： A61K9/20 , A61K31/485 , A61K47/30 , A61K47/34
CPC分类号： A61K9/2072 , A61K9/2018 , A61K9/2031 , A61K9/2054 , A61K9/2059 , A61K31/135 , A61K31/137 , Y10T428/24479
摘要： The invention relates to a pharmaceutical dosage form, preferably with controlled release of a pharmacoiogicaiiy active compound (A) contained therein, the pharmaceutical dosage form very preferably being tamper-resistant and most preferably having a breaking strength B 1 of at least 500 N in direction of extension E 1 and having a breaking strength B 2 of less than 500 N in direction of extension E 2 .
摘要翻译：本发明涉及一种药物剂型，优选具有其中所含的药物代谢活性化合物（A）的受控释放，所述药物剂型非常优选是抗篡改的，最优选地具有至少500N的断裂强度B1 并且在延伸方向E2具有小于500N的断裂强度B2。

2. 发明申请

WO2011009604A1 OXIDATION-STABILIZED TAMPER-RESISTANT DOSAGE FORM 审中-公开
标题翻译：氧化稳定的耐篡改剂型
公开(公告)号：WO2011009604A1
公开(公告)日：2011-01-27
申请号：PCT/EP2010/004461
申请日：2010-07-21
申请人： GRÜNENTHAL GMBH , BARNSCHEID, Lutz , GALIA, Eric , SCHWIER, Sebastian , BERTRAM, Ulrike , GEISSLER, Anja , GRIESSMANN, Kornelia , BARTHOLOMÄUS, Johannes
发明人： BARNSCHEID, Lutz , GALIA, Eric , SCHWIER, Sebastian , BERTRAM, Ulrike , GEISSLER, Anja , GRIESSMANN, Kornelia , BARTHOLOMÄUS, Johannes
IPC分类号： A61K9/20 , A61K9/28 , A61K31/485
CPC分类号： A61K9/2013 , A61K9/20 , A61K9/2031 , A61K9/2054 , A61K9/2095 , A61K9/284 , A61K31/485
摘要： The invention relates to a thermoformed pharmaceutical dosage form having a breaking strength of at least 300 N, said dosage form comprising - a pharmacologically active ingredient (A), - a free physiologically acceptable acid (B) in an amount of from 0.001 wt.-% to 5.0 wt.-%, based on the total weight of the pharmaceutical dosage form, and - a polyalkylene oxide (C) having a weight average molecular weight M w of at least 200,000 g/mol.
摘要翻译：本发明涉及具有至少300N的断裂强度的热成型药物剂型，所述剂型包含药理活性成分（A）， - 游离生理上可接受的酸（B），其量为0.001重量％％至5.0重量％，基于药物剂型的总重量，和 - 重均分子量Mw至少为200,000g / mol的聚环氧烷（C）。

3. 发明申请

WO2012028318A1 TAMPER RESISTANT DOSAGE FORM COMPRISING AN ANIONIC POLYMER 审中-公开
标题翻译：阻燃剂剂型包含阴离子聚合物
公开(公告)号：WO2012028318A1
公开(公告)日：2012-03-08
申请号：PCT/EP2011/004405
申请日：2011-09-01
申请人： GRÜNENTHAL GMBH , BARNSCHEID, Lutz, Dr. , SCHWIER, Sebastian, Dr. , BARTHOLOMÄUS, Johannes, Dr.
发明人： BARNSCHEID, Lutz, Dr. , SCHWIER, Sebastian, Dr. , BARTHOLOMÄUS, Johannes, Dr.
IPC分类号： A61K9/16 , A61K9/20
CPC分类号： A61K9/2031 , A61K9/2013 , A61K9/2027 , A61K9/2054 , A61K9/2095 , A61K31/137
摘要： The invention relates to a pharmaceutical dosage form exhibiting a breaking strength of at least 500 N, said dosage form containing - a pharmacologically active ingredient (A); - a physiologically acceptable polymer (B) obtainable by polymerization of a monomer composition comprising an ethylenically unsaturated monomer bearing an anionic functional group, in protonated form or a physiologically acceptable salt thereof; - a polyalkylene oxide (C) having a weight average molecular weight of at least 200,000 g/mol, wherein the content of the polyalkylene oxide (C) is at least 20 wt.-%, based on the total weight of the dosage form; wherein the pharmacologically active ingredient (A) is present in a controlled-release matrix comprising the polymer (B) and the polyalkylene oxide (C).
摘要翻译：本发明涉及显示至少500N的断裂强度的药物剂型，所述剂型含有药理活性成分（A）; - 通过聚合具有质子化形式的含有阴离子官能团的烯属不饱和单体或其生理学上可接受的盐的单体组合物可获得的生理上可接受的聚合物（B） - 重均分子量为至少200,000g / mol的聚环氧烷（C），其中聚环氧烷（C）的含量为至少20重量％，基于剂型的总重量; 其中药理活性成分（A）存在于包含聚合物（B）和聚环氧烷（C）的控释基质中。

4. 发明申请

WO2012028317A1 TAMPER RESISTANT DOSAGE FORM COMPRISING AN ANIONIC POLYMER 审中-公开
标题翻译：阻燃剂剂型包含阴离子聚合物
公开(公告)号：WO2012028317A1
公开(公告)日：2012-03-08
申请号：PCT/EP2011/004404
申请日：2011-09-01
申请人： GRÜNENTHAL GMBH , BARNSCHEID, Lutz , SCHWIER, Sebastian , BARTHOLOMÄUS, Johannes
发明人： BARNSCHEID, Lutz , SCHWIER, Sebastian , BARTHOLOMÄUS, Johannes
IPC分类号： A61K9/20 , A61K9/48
CPC分类号： A61K31/137 , A61K9/2031 , A61K9/205 , A61K9/2054 , A61K9/2059 , A61K9/2095
摘要： The invention relates to a pharmaceutical dosage form exhibiting a breaking strength of at least 500 N, said dosage form containing - a pharmacologically active ingredient (A); - an anionic polysaccharide (B) obtainable by introducing anionic functional groups, in protonated form or a physiologically acceptable salt thereof, into a polysaccharide; and - a polyalkylene oxide (C); wherein the pharmacologically active ingredient (A) is present in a controlled-release matrix comprising the anionic polysaccharide (B) and the polyalkylene oxide (C).
摘要翻译：本发明涉及显示至少500N的断裂强度的药物剂型，所述剂型含有药理活性成分（A）; - 通过将质子化形式的阴离子官能团或其生理学上可接受的盐引入多糖中获得的阴离子多糖（B）; 和 - 聚环氧烷（C）; 其中药理活性成分（A）存在于包含阴离子多糖（B）和聚环氧烷（C）的控释基质中。

5. 发明申请

WO2013017242A1 TAMPER-RESISTANT TABLET PROVIDING IMMEDIATE DRUG RELEASE 审中-公开
标题翻译：耐药片提供立即药物释放
公开(公告)号：WO2013017242A1
公开(公告)日：2013-02-07
申请号：PCT/EP2012/003196
申请日：2012-07-27
申请人： GRÜNENTHAL GMBH , SCHWIER, Sebastian , HAUPTS, Marcel , RÜTTGERS, Udo , BARNSCHEID, Lutz , PÄTZ, Jana
发明人： SCHWIER, Sebastian , HAUPTS, Marcel , RÜTTGERS, Udo , BARNSCHEID, Lutz , PÄTZ, Jana
IPC分类号： A61K9/20 , A61K31/00
CPC分类号： A61K9/2077 , A61K9/2031 , A61K9/2081 , A61K9/28 , A61K31/135 , A61K31/137 , A61K31/138 , A61K31/485
摘要： The invention relates to a tamper-resistant tablet comprising a matrix material in an amount of more than one third of the total weight of the tablet; and a plurality of particulates in an amount of less than two thirds of the total weight of the tablet; wherein said particulates comprise a pharmacologically active compound and a polyalkylene oxide; and form a discontinuous phase within the matrix material.
摘要翻译：本发明涉及一种防篡改片剂，其包含多于片剂总重量的三分之一的量的基质材料; 以及少于所述片剂总重量的三分之二的多个颗粒; 其中所述颗粒包含药理活性化合物和聚环氧烷; 并在基体材料内形成不连续相。

6. 发明申请

WO2013017234A1 TAMPER-RESISTANT TABLET PROVIDING IMMEDIATE DRUG RELEASE 审中-公开
标题翻译：耐药片提供立即药物释放
公开(公告)号：WO2013017234A1
公开(公告)日：2013-02-07
申请号：PCT/EP2012/003188
申请日：2012-07-27
申请人： GRÜNENTHAL GMBH , SCHWIER, Sebastian , HAUPTS, Marcel , BARNSCHEID, Lutz , PÄTZ, Jana
发明人： SCHWIER, Sebastian , HAUPTS, Marcel , BARNSCHEID, Lutz , PÄTZ, Jana
IPC分类号： A61K9/20 , A61K31/00
CPC分类号： A61K9/2081 , A61K31/135 , A61K31/137 , A61K31/138 , A61K2300/00
摘要： The invention relates to a tamper-resistant tablet comprising a matrix material in an amount of more than one third of the total weight of the tablet; and a plurality of coated particulates in an amount of less than two thirds of the total weight of the tablet; wherein said particulates comprise a pharmacologically active compound and a physiologically acceptable polymer, preferably a polyalkylene oxide; and form a discontinuous phase within the matrix material; which preferably provides under in vitro conditions immediate release of the pharmacologically active compound in accordance with Ph. Eur.
摘要翻译：本发明涉及一种防篡改片剂，其包含多于片剂总重量的三分之一的量的基质材料; 以及多于所述片剂总重量的三分之二的涂覆微粒; 其中所述颗粒包含药理活性化合物和生理上可接受的聚合物，优选聚环氧烷; 并在基体材料内形成不连续相; 其优选在体外条件下提供根据Ph.Eur。的药理活性化合物的立即释放。

7. 发明申请

WO2012028319A1 TAMPER RESISTANT DOSAGE FORM COMPRISING INORGANIC SALT 审中-公开
标题翻译：含有无机盐的抗T药剂型
公开(公告)号：WO2012028319A1
公开(公告)日：2012-03-08
申请号：PCT/EP2011/004406
申请日：2011-09-01
申请人： GRÜNENTHAL GMBH , BARNSCHEID, Lutz
发明人： BARNSCHEID, Lutz
IPC分类号： A61K9/16 , A61K9/20 , A61K47/02
CPC分类号： A61K47/02 , A61K9/2009 , A61K9/2031 , A61K31/135 , A61K31/485 , A61K47/10
摘要： The invention relates to a pharmaceutical dosage form exhibiting a breaking strength of at least 500 N, said dosage form containing a pharmacologically active ingredient (A); an inorganic salt (B); and a polyalkylene oxide (C) having a weight average molecular weight of at least 200,000 g/mol, wherein the content of the polyalkylene oxide (C) is at least 20 wt.-%, based on the total weight of the dosage form; wherein the pharmacologically active ingredient (A) is present in a controlled-release matrix comprising the inorganic salt (B) and the polyalkylene oxide (C) and wherein, under in vitro conditions, the release profile of the pharmacologically active ingredient (A) from said matrix comprises at least a time interval during which the release follows zero order kinetics.
摘要翻译：本发明涉及显示至少500N的断裂强度的药物剂型，所述剂型含有药理活性成分（A）; 无机盐（B）; 和重均分子量为至少200,000g / mol的聚环氧烷（C），其中聚环氧烷（C）的含量为至少20重量％，基于剂型的总重量; 其中药理活性成分（A）存在于包含无机盐（B）和聚环氧烷（C）的控释基质中，并且其中在体外条件下，药理活性成分（A）的释放曲线来自所述矩阵包括至少一个时间间隔，在该时间间隔期间释放遵循零级动力学。

8. 发明申请

WO2011009602A1 HOT-MELT EXTRUDED CONTROLLED RELEASE DOSAGE FORM 审中-公开
标题翻译： HOT-MELT EXTREDED CONTROLLED RELEASE剂型
公开(公告)号：WO2011009602A1
公开(公告)日：2011-01-27
申请号：PCT/EP2010/004459
申请日：2010-07-21
申请人： GRÜNENTHAL GMBH , BARNSCHEID, Lutz , GALIA, Eric
发明人： BARNSCHEID, Lutz , GALIA, Eric
IPC分类号： A61K9/20 , A61K31/137
CPC分类号： A61K9/2072 , A61K9/2031 , A61K9/2054 , A61K9/2095 , A61K31/137
摘要： The invention relates to a hot-melt extruded pharmaceutical dosage form with controlled release of a pharmacologically active ingredient (A) embedded in a matrix comprising a polymer (C), the dosage form exhibiting a breaking strength of at least 300 N and having an oblong shape comprising a longitudinal direction of extension, a transversal direction of extension orthogonal to the longitudinal direction of extension, a front side, an opposite back side and a circumferential rim between said front and back side; wherein the core of the pharmaceutical dosage form has a morphological orientation caused by hot-melt extrusion that is substantially orthogonal to the longitudinal direction of extension of the dosage form; and/or - the release per area of the pharmacologically active ingredient (A) through the front side and the opposite back side is faster than the release through the circumferential rim.
摘要翻译：本发明涉及一种具有控制释放包含聚合物（C）的基质中的药理学活性成分（A）的热熔挤出药物剂型，所述剂型具有至少300N的断裂强度并且具有长方形形状，其包括纵向延伸方向，垂直于所述纵向延伸方向的横向方向，所述前侧和后侧之间的前侧，相对的后侧和周向边缘; 其中所述药物剂型的核心具有由与所述剂型的延伸长度方向基本正交的热熔融挤出引起的形态取向; 和/或 - 通过前侧和相对的后侧的药理学活性成分（A）的每个面积的释放比通过周缘的释放快。

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