公开(公告)号：US10369109B2

公开(公告)日：2019-08-06

申请号：US16032533

申请日：2018-07-11

申请人： GRÜNENTHAL GMBH

发明人： Johannes Bartholomaeus ,  Heinrich Kugelmann

IPC分类号： A61K31/485 ,  A61K9/20 ,  A61K9/48 ,  A61K31/137 ,  A61K31/5513 ,  A61K45/06 ,  A61K47/38 ,  A61K9/00

摘要： A solid administration form, protected from parenteral abuse and containing at least one viscosity-increasing agent in addition to one or more active substances that have parenteral abuse potential. The agent forms, when a necessary minimum amount of an aqueous liquid is added, on the basis of an extract obtained from the administration form, a preferably injectable gel that remains visually distinct when introduced into another quantity of an aqueous liquid.

公开(公告)号：US10335373B2

公开(公告)日：2019-07-02

申请号：US13864450

申请日：2013-04-17

申请人： GRÜNENTHAL GMBH

发明人： Klaus Wening ,  Lutz Barnscheid ,  Sebastian Schwier

IPC分类号： A61K9/20 ,  A61K31/135 ,  A61K9/00

摘要： A tamper-resistant pharmaceutical dosage form comprising a pharmacologically active ingredient embedded in a prolonged release matrix, which comprises a prolonged release matrix material selected from the group consisting of nonionic acrylic polymers and waxy materials and which provides prolonged release of the pharmacologically active ingredient, resistance against solvent extraction, resistance against grinding, and resistance against dose-dumping in aqueous ethanol.

公开(公告)号：US10300141B2

公开(公告)日：2019-05-28

申请号：US14979888

申请日：2015-12-28

申请人： GRÜNENTHAL GMBH

发明人： Lutz Barnscheid

IPC分类号： A61K9/20 ,  A61K47/02 ,  A61K47/10 ,  A61K31/135 ,  A61K31/485

摘要： A pharmaceutical dosage form exhibiting a breaking strength of at least 500 N, wherein the dosage form contains 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 the matrix comprises at least a time interval during which the release follows zero order kinetics.

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：US20180078544A1

公开(公告)日：2018-03-22

申请号：US15823918

申请日：2017-11-28

申请人： GRÜNENTHAL GMBH

发明人： KLAUS WENING ,  ANJA GEIßLER ,  JANA DENKER ,  LUTZ BARNSCHEID

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

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：US20180028670A1

公开(公告)日：2018-02-01

申请号：US15665549

申请日：2017-08-01

申请人： Grünenthal GMBH

发明人： Klaus WENING ,  Carmen Stomberg

IPC分类号： A61K47/38 ,  A61K31/485 ,  A61K31/137 ,  A61K47/10

CPC分类号： A61K47/38 ,  A61K9/2031 ,  A61K9/205 ,  A61K9/2054 ,  A61K9/2059 ,  A61K31/137 ,  A61K31/485 ,  A61K45/06 ,  A61K47/10

摘要： A pharmaceutical dosage form having a breaking strength of at least 300 N, said dosage form comprising: an opioid (A) selected from Oxymorphone, Oxycodone, Tapentadol, Hydromorphone, Hydrocodone, Morphine, and physiologically acceptable salts thereof; wherein the weight content of the opioid (A) is from 5.0 to 35 wt.-%; an anionic polysaccharide (B) selected from croscarmellose, carmellose, crosslinked carboxymethyl starch, carboxymethyl starch, and physiologically acceptable salts thereof; wherein the weight content of the anionic polysaccharide (B) is within from 5.0 to 35 wt.-%; and a polyalkylene oxide (C) having a weight average molecular weight of at least 200,000 g/mol; wherein the weight content of the polyalkylene oxide (C) is from 20 to 80 wt.-%; wherein all wt.-%'s are based on a total weight of the dosage form, and the opioid (A) is present in a controlled-release matrix comprising the anionic polysaccharide (B) and the polyalkylene oxide (C).

公开(公告)号：US09872835B2

公开(公告)日：2018-01-23

申请号：US14719351

申请日：2015-05-22

申请人： GRÜNENTHAL GMBH

发明人： Lutz Barnscheid ,  Klaus Wening ,  Jana Pätz ,  Anja Geissler

IPC分类号： A61K31/135 ,  A61K9/16 ,  A61K9/48 ,  A61K31/485

CPC分类号： A61K9/1652 ,  A61K9/1623 ,  A61K9/1682 ,  A61K9/4866 ,  A61K31/135 ,  A61K31/485

摘要： The invention relates to an oral pharmaceutical dosage form providing resistance against dose dumping in aqueous ethanol and comprising a pharmacologically active ingredient embedded in a matrix material, wherein the matrix material comprises an alkyl cellulose and a heteropolysaccharide; and wherein the relative weight ratio of heteropolysaccharide to alkyl cellulose is within the range of from 1:20 to 20:1; and wherein the total content of alkyl cellulose and heteropolysaccharide is at least 35 wt.-%, relative to the total weight of the dosage form. A process of producing the dosage form and methods of using the dosage form, for example to treat pain, are also disclosed.

公开(公告)号：US20170209379A1

公开(公告)日：2017-07-27

申请号：US15459180

申请日：2017-03-15

申请人： GRÜNENTHAL GMBH

发明人： Elisabeth ARKENAU-MARIC ,  Johannes BARTHOLOMAEUS ,  Heinrich KUGELMANN

IPC分类号： A61K9/20 ,  A61K31/485 ,  B29C47/06 ,  B29C47/00 ,  A61J3/10 ,  A61K31/135 ,  A61J3/06

CPC分类号： A61K31/485 ,  A61J3/005 ,  A61J3/06 ,  A61J3/10 ,  A61K9/0053 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2031 ,  A61K9/205 ,  A61K9/2054 ,  A61K9/2068 ,  A61K9/2072 ,  A61K9/2086 ,  A61K9/2095 ,  A61K9/2893 ,  A61K9/4808 ,  A61K31/135 ,  A61K31/277 ,  A61K31/4418 ,  A61K31/4422 ,  A61K31/55 ,  A61K31/554 ,  B29B7/002 ,  B29B9/02 ,  B29B9/12 ,  B29C35/0261 ,  B29C43/02 ,  B29C45/0001 ,  B29C47/0004 ,  B29C47/004 ,  B29C47/0066 ,  B29C47/0085 ,  B29C47/065 ,  B29C2793/009 ,  B29K2105/0035 ,  B29K2105/0044 ,  B29K2105/251 ,  B29K2995/0056 ,  B29L2031/753 ,  B29L2031/772

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：US09688683B2

公开(公告)日：2017-06-27

申请号：US15018968

申请日：2016-02-09

申请人： GRÜNENTHAL GMBH

发明人： Florian Jakob ,  Ingo Konetzki ,  Tobias Craan ,  Antonio Nardi ,  Christian Hesslinger

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： Novel substituted condensed pyrimidine compounds of general formula (I) in which the chemical groupings, substituents and indices are as defined in the description, and to their use as medicaments, in particular as medicaments for the treatment of conditions and diseases that can be treated by inhibition of the PDE4 enzyme.

公开(公告)号：US09655853B2

公开(公告)日：2017-05-23

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： A61K47/32 ,  A61K31/74 ,  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.