公开(公告)号：US11844865B2

公开(公告)日：2023-12-19

申请号：US17010106

申请日：2020-09-02

申请人： GRÜNENTHAL GMBH

发明人： Johannes Bartholomäus ,  Heinrich Kugelmann ,  Elisabeth Arkenau-Maric

IPC分类号： A61K9/20 ,  A61K9/28 ,  A61K31/485 ,  A61K9/00

CPC分类号： A61K9/2031 ,  A61K9/0002 ,  A61K9/0053 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2068 ,  A61K9/2095 ,  A61K9/28 ,  A61K9/2893 ,  A61K31/485

摘要： The present invention relates to an abuse-proofed, oral dosage form with controlled opioid-release for once daily administration, characterised in that it comprises at least one opioid with potential for abuse (A), at least one synthetic or natural polymer (C), optionally delayed-release matrix auxiliary substances, physiologically acceptable auxiliary substances (B), optionally a wax (D) and optionally at least one delayed-release coating, component (C) or (D) in each case exhibiting a breaking strength of at least 500 N, preferably of at least 1000 N.

公开(公告)号：US09629807B2

公开(公告)日：2017-04-25

申请号：US15132325

申请日：2016-04-19

申请人： GRÜNENTHAL GMBH

发明人： Elisabeth Arkenau-Maric ,  Johannes Bartholomaeus ,  Heinrich Kugelmann

IPC分类号： A61K49/00 ,  A61K9/20 ,  A61K31/485 ,  A61J3/07 ,  A61K9/00 ,  A61K31/135

CPC分类号： A61K9/2031 ,  A61J3/07 ,  A61K9/0092 ,  A61K9/2004 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2068 ,  A61K9/2072 ,  A61K9/2086 ,  A61K9/2095 ,  A61K31/135 ,  A61K31/485

摘要： The invention relates to a dosage form that is thermoformed without discoloration and is safeguarded from abuse, comprising at least one synthetic or natural polymer having a breaking strength of at least 500 N in addition to one or more active substances that could be subject to abuse. The invention also relates to a corresponding method for producing said dosage form.

公开(公告)号：US20160220517A1

公开(公告)日：2016-08-04

申请号：US15095336

申请日：2016-04-11

申请人： GRÜNENTHAL GMBH

发明人： Johannes BARTHOLOMÄUS ,  Heinrich Kugelmann ,  Elisabeth Arkenau-Maric

IPC分类号： A61K31/137 ,  A61K9/48 ,  A61K9/00 ,  A61K9/20

CPC分类号： A61K31/137 ,  A61K9/0053 ,  A61K9/20 ,  A61K9/2013 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/2077 ,  A61K9/2095 ,  A61K9/2893 ,  A61K9/4808 ,  A61K31/135 ,  A61K47/10 ,  A61K47/38

摘要： The present invention relates to an abuse-proofed oral dosage form with controlled release of (1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol for once daily administration, which comprises the active ingredient and/or one or more of the pharmaceutically acceptable salts thereof (A), at least one synthetic or natural polymer (C), delayed-release auxiliary substances, optionally physiologically acceptable auxiliary substances (B) and optionally a wax (D), component (C) or (D) in each case exhibiting a breaking strength of at least 500 N, preferably of at least 1000 N.

摘要翻译： 本发明涉及具有受控释放的（1R，2R）-3-（3-二甲基氨基-1-乙基-2-甲基 - 丙基）苯酚的滥用防治口服剂型，每天一次给药，其包含活性成分 至少一种合成或天然聚合物（C），延迟释放辅助物质，任选的生理上可接受的辅助物质（B）和任选的蜡（D），组分（A）和/或其一种或多种药学上可接受的盐 （C）或（D）在每种情况下表现出至少500N的断裂强度，优选至少为1000N。

公开(公告)号：US20180243237A1

公开(公告)日：2018-08-30

申请号：US15964635

申请日：2018-04-27

申请人： Grünenthal Gmbh

发明人： Elisabeth Arkenau-Maric ,  Johannes Bartholomaus ,  Heinrich Kugelmann

IPC分类号： A61K31/135 ,  A61K45/06 ,  A61K9/20 ,  B29C47/40 ,  B29C47/06 ,  B29C47/00 ,  A61K47/10 ,  A61K36/81 ,  A61K36/67 ,  A61K31/5513 ,  A61K31/515 ,  A61K31/485 ,  A61K31/4725 ,  B29K71/00 ,  B29K105/00 ,  B29L31/00

CPC分类号： A61K31/135 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2031 ,  A61K9/205 ,  A61K9/2054 ,  A61K9/2068 ,  A61K9/2072 ,  A61K9/2077 ,  A61K9/2095 ,  A61K31/4725 ,  A61K31/485 ,  A61K31/515 ,  A61K31/5513 ,  A61K36/67 ,  A61K36/81 ,  A61K45/06 ,  A61K47/10 ,  B29C48/0011 ,  B29C48/0022 ,  B29C48/022 ,  B29C48/03 ,  B29C48/18 ,  B29C48/40 ,  B29K2071/02 ,  B29K2105/0035 ,  B29K2105/0088 ,  B29K2105/25 ,  B29K2995/007 ,  B29K2995/0089 ,  B29L2031/753 ,  A61K2300/00

摘要： The invention relates to a dosage form that is thermoshaped without being extruded and that is safeguarded from abuse, comprising at least one synthetic or natural polymer having a breaking strength of at least 500 N in addition to one or more active substances that could be subject to abuse and optionally physiologically acceptable adjuvants. The invention also relates to a corresponding method for producing said dosage form.

公开(公告)号：US20160120810A1

公开(公告)日：2016-05-05

申请号：US14994691

申请日：2016-01-13

申请人： Grünenthal GmbH

发明人： Judy Ashworth ,  Elisabeth Arkenau-Maric ,  Johannes Bartholomäus ,  Heinrich Kugelmann

IPC分类号： A61K9/20 ,  A61K9/28 ,  A61K31/277 ,  A61K31/55 ,  B29B9/02 ,  A61K31/135 ,  A61K31/485 ,  B29C43/02 ,  B29B9/12 ,  B29B7/00 ,  A61K31/554 ,  A61K31/4422

摘要： The invention relates to a dosage form comprising a physiologically effective amount of a physiologically active substance (A), a synthetic, semi-synthetic or natural polymer (C), optionally one or more physiologically acceptable auxiliary substances (B) and optionally a synthetic, semi-synthetic or natural wax (D), wherein the dosage form exhibits a resistance to crushing of at least 400 N and wherein under physiological conditions the release of the physiologically active substance (A) from the dosage form is at least partially delayed.

公开(公告)号：US20180235908A1

公开(公告)日：2018-08-23

申请号：US15956867

申请日：2018-04-19

申请人： GRÜNENTHAL GMBH

发明人： Johannes BARTHOLOMÄUS ,  Heinrich Kugelmann ,  Elisabeth Arkenau-Maric

IPC分类号： A61K31/137 ,  A61K47/38 ,  A61K47/10 ,  A61K31/135 ,  A61K9/48 ,  A61K9/28 ,  A61K9/00 ,  A61K9/20

CPC分类号： A61K31/137 ,  A61K9/0053 ,  A61K9/20 ,  A61K9/2013 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/2077 ,  A61K9/2095 ,  A61K9/2893 ,  A61K9/4808 ,  A61K31/135 ,  A61K47/10 ,  A61K47/38

摘要： The present invention relates to an abuse-proofed oral dosage form with controlled release of (1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol for once daily administration, which comprises the active ingredient and/or one or more of the pharmaceutically acceptable salts thereof (A), at least one synthetic or natural polymer (C), delayed-release auxiliary substances, optionally physiologically acceptable auxiliary substances (B) and optionally a wax (D), component (C) or (D) in each case exhibiting a breaking strength of at least 500 N, preferably of at least 1000 N.

公开(公告)号：US09750701B2

公开(公告)日：2017-09-05

申请号：US14965935

申请日：2015-12-11

申请人： GRÜNENTHAL GMBH

发明人： Eugeen Marie Jozef Jans ,  Filip René Irena Kiekens ,  Jody Firmin Marceline Voorspoels ,  Anne Faure ,  Iris Ziegler ,  Elisabeth Arkenau-Maric ,  Lutz Barnscheid ,  Johannes Bartholomäus ,  Marc Frevel ,  Eric Galia ,  Andrea Schüessele

IPC分类号： A61K9/20 ,  A61K31/135 ,  A61K31/137

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 pharmacologically active compound (A) contained therein, the pharmaceutical dosage form very preferably being tamper-resistant and most preferably having a breaking strength B1 of at least 500 N in direction of extension E1 and having a breaking strength B2 of less than 500 N in direction of extension E2.

公开(公告)号：US20150150978A1

公开(公告)日：2015-06-04

申请号：US14618030

申请日：2015-02-10

申请人： GRÜNENTHAL GMBH

发明人： Elisabeth Arkenau-Maric ,  Johannes Bartholomäus ,  Heinrich Kugelmann

IPC分类号： A61K47/10 ,  A61K9/20 ,  A61K31/135

CPC分类号： A61K31/135 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2031 ,  A61K9/205 ,  A61K9/2054 ,  A61K9/2068 ,  A61K9/2072 ,  A61K9/2077 ,  A61K9/2095 ,  A61K31/4725 ,  A61K31/485 ,  A61K31/515 ,  A61K31/5513 ,  A61K36/67 ,  A61K36/81 ,  A61K45/06 ,  A61K47/10 ,  B29C48/0011 ,  B29C48/0022 ,  B29C48/022 ,  B29C48/03 ,  B29C48/18 ,  B29C48/40 ,  B29K2071/02 ,  B29K2105/0035 ,  B29K2105/0088 ,  B29K2105/25 ,  B29K2995/007 ,  B29K2995/0089 ,  B29L2031/753 ,  A61K2300/00

摘要： The invention relates to a dosage form that is thermoshaped without being extruded and that is safeguarded from abuse, comprising at least one synthetic or natural polymer having a breaking strength of at least 500 N in addition to one or more active substances that could be subject to abuse and optionally physiologically acceptable adjuvants. The invention also relates to a corresponding method for producing said dosage form.

摘要翻译： 本发明涉及一种剂型，其不经挤出而被热成型并且被防止滥用，其包含至少一种具有至少500N的断裂强度的合成或天然聚合物，除了一种或多种可能经受 滥用和任选的生理上可接受的佐剂。 本发明还涉及用于生产所述剂型的相应方法。

公开(公告)号：US20180147149A1

公开(公告)日：2018-05-31

申请号：US15878524

申请日：2018-01-24

申请人： GRÜNENTHAL GMBH

发明人： Johannes Bartholomäus ,  Heinrich Kugelmann ,  Elisabeth Arkenau-Maric

IPC分类号： A61K9/20 ,  A61K31/485 ,  A61K9/28 ,  A61K9/00

CPC分类号： A61K9/2031 ,  A61K9/0002 ,  A61K9/0053 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2068 ,  A61K9/2095 ,  A61K9/28 ,  A61K9/2893 ,  A61K31/485

摘要： The present invention relates to an abuse-proofed, oral dosage form with controlled opioid-release for once daily administration, characterised in that it comprises at least one opioid with potential for abuse (A), at least one synthetic or natural polymer (C), optionally delayed-release matrix auxiliary substances, physiologically acceptable auxiliary substances (B), optionally a wax (D) and optionally at least one delayed-release coating, component (C) or (D) in each case exhibiting a breaking strength of at least 500 N, preferably of at least 1000 N.

公开(公告)号：US20130320592A1

公开(公告)日：2013-12-05

申请号：US13962098

申请日：2013-08-08

申请人： Grünenthal GmbH

发明人： Elisabeth Arkenau-Maric ,  Johannes Bartholomaus

IPC分类号： A61K9/20

CPC分类号： A61K9/2095 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/2072 ,  A61K31/135 ,  A61K31/485 ,  A61K31/515 ,  A61K31/5513 ,  B30B11/16 ,  B30B11/34

摘要： The present invention relates to a process for the production of abuse-proofed, thermoformed dosage forms containing, apart from one or more active ingredients with potential for abuse and optionally physiologically acceptable auxiliary substances, at least one synthetic or natural polymer with a breaking strength of at least 500 N.