公开(公告)号：US20180044348A1

公开(公告)日：2018-02-15

申请号：US15791563

申请日：2017-10-24

申请人： Grünenthal Gmbh

发明人： Klaus WENING ,  Lutz BARNSCHEID ,  Anja GEISSLER ,  Jana DENKER ,  Dagmar LISCHKE

IPC分类号： C07D489/04

CPC分类号： C07D489/04 ,  C07B2200/13

摘要： Crystalline salts of 7,8-Didehydro-4,5 alpha-epoxy-17-methylmorphinan-3,6 alpha-diol sulfate(2:1), i.e. of morphine sulphate, are disclosed and four polymorphic forms of these salts are reported. The invention further relates to a pharmaceutical composition comprising an amount of such a salt and such a salt as a medicament and for the treatment and/or prevention of pain.

公开(公告)号：US20160310486A1

公开(公告)日：2016-10-27

申请号：US15135588

申请日：2016-04-22

申请人： GRÜNENTHAL GMBH

发明人： Klaus WENING ,  Lutz BARNSCHEID ,  Anja GEIßLER ,  Jana DENKER ,  Jessica REDMER

IPC分类号： A61K31/485 ,  A61K9/20 ,  A61K31/167 ,  A61K9/16 ,  A61K9/48 ,  A61K45/06

CPC分类号： A61K31/485 ,  A61K9/1635 ,  A61K9/1641 ,  A61K9/1652 ,  A61K9/1694 ,  A61K9/2031 ,  A61K9/4866 ,  A61K31/135 ,  A61K31/137 ,  A61K31/167 ,  A61K31/192 ,  A61K31/407 ,  A61K45/06 ,  A61K2300/00

摘要： A tamper-resistant pharmaceutical dosage form comprising two pharmacologically active ingredients, wherein the dosage form provides under in vitro conditions fast release, preferably immediate release according to Ph. Eur., of both pharmacologically active ingredients. The dosage form is useful for pharmaceutical combination therapy that is achieved by administering dosage forms containing more than one pharmacologically active ingredient as fixed-dose combinations.

摘要翻译： 包含两种药理学活性成分的抗篡改药物剂型，其中所述剂型在体外条件下提供快速释放，优选根据Ph.Eur。立即释放两种药理活性成分。 剂型可用于药物联合治疗，其通过施用含有多于一种药理学活性成分的剂型作为固定剂量组合来实现。

公开(公告)号：US20160271066A1

公开(公告)日：2016-09-22

申请号：US15166573

申请日：2016-05-27

申请人： GRÜNENTHAL GMBH

发明人： Lutz BARNSCHEID ,  Jessica REDMER ,  Sebastian SCHWIER

IPC分类号： A61K9/20 ,  A61K31/135

CPC分类号： A61K9/2027 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/2077 ,  A61K9/2095 ,  A61K31/135 ,  A61K47/32

摘要： The invention relates to a pharmaceutical dosage form having a breaking strength of at least 300 N and comprising a pharmacologically active compound, an anionic polymer bearing carboxylic groups, wherein the content of the anionic polymer is ≧20 wt.-%, based on the total weight of the pharmaceutical dosage form, and a nonionic surfactant.

公开(公告)号：US20130129826A1

公开(公告)日：2013-05-23

申请号：US13677446

申请日：2012-11-15

申请人： GRÜNENTHAL GMBH

发明人： Anja GEIßLER ,  Lutz BARNSCHEID ,  Sebastian SCHWIER ,  Johannes BARTHOLOMÄUS

IPC分类号： A61K47/10 ,  A61K47/32

CPC分类号： A61K47/10 ,  A61K9/2027 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/2095 ,  A61K31/485 ,  A61K47/32 ,  A61K2300/00

摘要： The invention relates to a pharmaceutical dosage form for oral administration having a breaking strength of at least 300 N and comprising (i) a pharmacologically active ingredient; (ii) an opioid antagonist and/or an aversive agent; (iii) a polyalkylene oxide having an average molecular weight of at least 200,000 g/mol; and (a) further comprising (iv) an anionic polymer; and/or (b) having a storage stability at 40° C. of at least 3 months.

摘要翻译： 本发明涉及一种口服给药的药物剂型，其具有至少300N的断裂强度，并包含（i）药理学活性成分; （ii）阿片拮抗剂和/或厌食剂; （iii）平均分子量至少为200,000g / mol的聚环氧烷; 和（a）还包含（iv）阴离子聚合物; 和/或（b）在40℃下具有至少3个月的储存稳定性。

公开(公告)号：US20180044347A1

公开(公告)日：2018-02-15

申请号：US15791508

申请日：2017-10-24

申请人： GRÜNENTHAL GMBH

发明人： Klaus WENING ,  Lutz BARNSCHEID ,  Anja GEISSLER ,  Jana DENKER ,  Dagmar LISCHKE

IPC分类号： C07D489/04

CPC分类号： C07D489/04 ,  A61P25/04 ,  A61P29/00 ,  C07B2200/13 ,  C07D489/02

摘要： Crystalline salts of 4,5 α-epoxy-3-methoxy-17-methylmorphinan-6-one tartrate (1:1) (hydrocodone bitartrate) are disclosed and three polymorphic forms of these salts are reported. The invention further relates to a pharmaceutical composition comprising such a salt and such a salt as a medicament and for the treatment and/or prevention of pain.

公开(公告)号：US20160310487A1

公开(公告)日：2016-10-27

申请号：US15169778

申请日：2016-06-01

申请人： GRÜNENTHAL GMBH

发明人： Klaus WENING ,  Anja GEIßLER ,  Jana DENKER ,  Lutz BARNSCHEID

IPC分类号： A61K31/485 ,  A61K9/48 ,  A61K31/137 ,  A61K9/20 ,  A61K9/16 ,  A61K9/50

CPC分类号： A61K31/485 ,  A61K9/1611 ,  A61K9/1617 ,  A61K9/1635 ,  A61K9/1641 ,  A61K9/1652 ,  A61K9/1658 ,  A61K9/1694 ,  A61K9/2077 ,  A61K9/4808 ,  A61K9/50 ,  A61K31/137

摘要： A tamper-resistant pharmaceutical dosage form comprising a multitude of particles which comprise a pharmacologically active compound, a polyalkylene oxide, and a disintegrant; wherein the pharmacologically active compound is dispersed in a matrix comprising the polyalkylene oxide and the disintegrant; wherein the content of the disintegrant is more than 5.0 wt.-%, based on the total weight of the pharmaceutical dosage form and/or based on the total weight of the particles; wherein the content of the polyalkylene oxide is at least 25 wt.-%, based on the total weight of the pharmaceutical dosage form and/or based on the total weight of the particles; and wherein the dosage form provides under in vitro conditions immediate release of the pharmacologically active compound in accordance with Ph. Eur.

公开(公告)号：US20150366809A1

公开(公告)日：2015-12-24

申请号：US14841829

申请日：2015-09-01

申请人： GRÜNENTHAL GMBH

发明人： Lutz BARNSCHEID ,  Eric GALIA ,  Sebastian SCHWIER ,  Ulrike BERTRAM ,  Anja GEISSLER ,  Kornelia GRIESSMANN ,  Johannes BARTHOLOMÄUS

IPC分类号： A61K9/20 ,  A61K31/485

CPC分类号： A61K9/2013 ,  A61K9/20 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/2095 ,  A61K9/284 ,  A61K31/485

摘要： 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 Mw of at least 200,000 g/mol.

摘要翻译： 一种具有至少300N断裂强度的热成型药物剂型，所述剂型包含药理学活性成分（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，以及重均分子量Mw至少为200,000g / mol的聚环氧烷（C）。

公开(公告)号：US20190125680A1

公开(公告)日：2019-05-02

申请号：US16225418

申请日：2018-12-19

申请人： Grünenthal GmbH

发明人： Sebastian SCHWIER ,  Marcel HAUPTS ,  Lutz BARNSCHEID ,  Jana PÄTZ

IPC分类号： A61K9/20 ,  A61K31/135 ,  A61K31/137 ,  A61K31/138

摘要： The invention relates to a tamper-resistant tablet comprising (i) a matrix material in an amount of more than one third of the total weight of the tablet; and (ii) 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.; and method of using said tablet to treat pain and other conditions.

公开(公告)号：US20180177732A1

公开(公告)日：2018-06-28

申请号：US15901063

申请日：2018-02-21

申请人： GRÜNENTHAL GMBH

发明人： Lutz BARNSCHEID ,  Eric GALIA ,  Sebastian SCHWIER ,  Ulrike BERTRAM ,  Anja GEISSLER ,  Kornelia GRIESSMANN ,  Johannes BARTHOLOMÄUS

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

CPC分类号： A61K9/2013 ,  A61K9/20 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/2095 ,  A61K9/284 ,  A61K31/485

摘要： 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 Mw of at least 200,000 g/mol.

公开(公告)号：US20170296472A1

公开(公告)日：2017-10-19

申请号：US15636957

申请日：2017-06-29

申请人： GRÜNENTHAL GMBH

发明人： Lutz BARNSCHEID ,  Anja Geissler ,  Klaus Wening ,  Stefanie Strauch ,  Jana Pätz ,  Sebastian Schwier

IPC分类号： A61K9/20 ,  A61K31/485 ,  A61K31/167 ,  A61K9/24 ,  A61K45/06

CPC分类号： A61K9/2086 ,  A61K9/2031 ,  A61K9/209 ,  A61K9/2095 ,  A61K31/167 ,  A61K31/485 ,  A61K45/06 ,  A61K2300/00

摘要： The invention relates to a pharmaceutical dosage form comprising (i) at least one formed segment (S1), which contains a first pharmacologically active ingredient (A1) and provides prolonged release thereof, and (ii) at least one further segment (S2), which contains a second pharmacologically active ingredient (A2) and provides immediate release thereof, wherein the at least one formed segment (S1) exhibits a higher breaking strength than the at least one further segment (S2) and the at least one formed segment (S1) exhibits a breaking strength of more than 500 N.