Abstract: 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.
Type:
Application
Filed:
November 28, 2017
Publication date:
March 22, 2018
Applicant:
GRÜNENTHAL GMBH
Inventors:
KLAUS WENING, ANJA GEIßLER, JANA DENKER, LUTZ BARNSCHEID
Abstract: The invention is directed to an immediate release capsule which mitigates the abuse of Tapentadol or physiologically acceptable salt thereof by direct intravenous injection. The capsule comprises a tamper resistant formulation which when mixed with water and heated, results in a turbid, bubbling mixture that is not injectable with a standard insulin syringe.
Type:
Grant
Filed:
September 7, 2016
Date of Patent:
March 13, 2018
Assignee:
GRÜNENTHAL GMBH
Inventors:
Ingo Friedrich, Richard Fuhrherr, Silke Möschter, Simone Wengner
Abstract: The invention relates to aryl substituted heterocyclyl sulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
Type:
Grant
Filed:
April 14, 2015
Date of Patent:
February 20, 2018
Assignee:
GRÜNENTHAL GMBH
Inventors:
Stefan Schunk, Melanie Reich, Florian Jakob, René Michael Koenigs, Nils Damann, Michael Haurand, Marc Rogers, Kathy MacKenzie, Richard Hamlyn
Abstract: Crystalline salts of 4,5 ?-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.
Type:
Application
Filed:
October 24, 2017
Publication date:
February 15, 2018
Applicant:
GRÜNENTHAL GMBH
Inventors:
Klaus WENING, Lutz BARNSCHEID, Anja GEISSLER, Jana DENKER, Dagmar LISCHKE
Abstract: 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.
Type:
Application
Filed:
October 24, 2017
Publication date:
February 15, 2018
Applicant:
Grünenthal Gmbh
Inventors:
Klaus WENING, Lutz BARNSCHEID, Anja GEISSLER, Jana DENKER, Dagmar LISCHKE
Abstract: A pharmaceutical dosage form having a breaking strength of at least 300 N and comprising an ephedrine component selected from the group consisting of ephedrine, pseudoephedrine and the physiologically acceptable salts thereof, wherein the weight content of the ephedrine component is within the range of from 0.1 to 60 wt.-%, relative to the total weight of the pharmaceutical dosage form.
Type:
Application
Filed:
August 11, 2017
Publication date:
February 15, 2018
Applicant:
GRÜNENTHAL GMBH
Inventors:
Carmen STOMBERG, Klaus WENING, Sebastian SCHWIER
Abstract: A tamper-resistant, oral pharmaceutical dosage form comprising a pharmacologically active ingredient having psychotropic action and a polyethylene glycol graft copolymer, wherein the content of the polyethylene glycol graft copolymer is at least 25 wt.-%, relative to the total weight of the pharmaceutical dosage form. Also disclosed is the manufacture of the dosage form and its use.
Abstract: 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).
Abstract: The invention relates to aryl substituted heterocyclyl sulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
Type:
Grant
Filed:
April 14, 2015
Date of Patent:
January 30, 2018
Assignee:
GRÜNENTHAL GMBH
Inventors:
Stefan Schunk, Melanie Reich, Florian Jakob, Nils Damann, Michael Haurand, Achim Kless, Marc Rogers, Kathy MacKenzie
Abstract: 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.
Type:
Grant
Filed:
May 22, 2015
Date of Patent:
January 23, 2018
Assignee:
GRÜNENTHAL GMBH
Inventors:
Lutz Barnscheid, Klaus Wening, Jana Pätz, Anja Geissler
Abstract: Spirocyclic cyclohexane compounds corresponding to formula I a method for producing them, pharmaceutical compositions containing them, and methods of using them.
Type:
Grant
Filed:
July 21, 2015
Date of Patent:
January 9, 2018
Assignee:
Gruenenthal GmbH
Inventors:
Claudia Hinze, Otto Aulenbacher, Bernd Sundermann, Stefan Oberboersch, Elmar Friderichs, Werner Englberger, Babette-Yvonne Koegel, Klaus Linz, Hans Schick, Helmut Sonnenschein, Birgitta Henkel, Valerie Sarah Rose, Michael Jonathan Lipkin
Abstract: 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.
Type:
Grant
Filed:
June 1, 2016
Date of Patent:
January 2, 2018
Assignee:
GRÜNENTHAL GMBH
Inventors:
Klaus Wening, Anja Geiβler, Jana Denker, Lutz Barnscheid
Abstract: The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient selected from (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, and a second pharmacologically active ingredient which is a salicylic acid component selected from the group consisting of acetylsalicylic acid, salicylic acid, salicylamide, ethenzamide, salsalate, dipyrocetyl, benorilate, diflunisal, guacetisal, and the physiologically acceptable salts thereof.
Type:
Grant
Filed:
May 13, 2013
Date of Patent:
January 2, 2018
Assignee:
Gruenenthal GmbH
Inventors:
Stefanie Frosch, Klaus Linz, Klaus Schiene
Abstract: A process for the preparation of substituted 3-(1-amino-2-methylpentane-3-yl)phenyl compounds which has advantages over conventional processes with respect to higher conversions and yields, flexibility, a shorter overall route, environmentally acceptable conditions, influence of stereoselectivity such as diastereoselectivity in a targeted manner and at least partial suppression of the formation of undesired side-products and/or undesired stereoisomers, in particular undesired diastereomers.
Type:
Grant
Filed:
May 17, 2016
Date of Patent:
December 26, 2017
Assignee:
GRUENENTHAL GMBH
Inventors:
Helmut Heinrich Buschmann, Joerg Holenz
Abstract: 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.
Type:
Application
Filed:
July 14, 2017
Publication date:
November 2, 2017
Applicant:
Grünenthal GmbH
Inventors:
Judy ASHWORTH, Elisabeth ARKENAU-MARIC, Johannes BARTHOLOMÄUS, Heinrich KUGELMANN
Abstract: The invention relates to pyrrole carboxamides bearing a fluoromethyl-moiety as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
Type:
Grant
Filed:
June 14, 2016
Date of Patent:
October 31, 2017
Assignee:
GRUENENTHAL GMBH
Inventors:
Melanie Reich, Stefan Schunk, Florian Jakob, Henning Steinhagen, Nils Damann, Michael Haurand, Richard Hamlyn, Marc Rogers, Kathy MacKenzie
Abstract: The invention relates to amidic oxotetrahydro-2H-furo[3.2-b]pyrrol-4(5H)-yl) derivatives as dual CatS/K inhibitors exhibiting a pronounced CatK-inhibition, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
Type:
Grant
Filed:
April 23, 2015
Date of Patent:
October 31, 2017
Assignee:
GRÜNENTHAL GMBH
Inventors:
Antonio Nardi, Paul Ratcliffe, Tobias Craan, Torsten Hertrampf, Bernhard Lesch, Henning Steinhagen
Abstract: 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.
Type:
Application
Filed:
June 29, 2017
Publication date:
October 19, 2017
Applicant:
GRÜNENTHAL GMBH
Inventors:
Lutz BARNSCHEID, Anja Geissler, Klaus Wening, Stefanie Strauch, Jana Pätz, Sebastian Schwier
Abstract: The invention relates to a pharmaceutical dosage form for oral administration comprising a pharmacologically active compound; wherein a portion of said pharmacologically active compound is contained in a multitude of immediate release particles providing immediate release of the pharmacologically active compound; wherein another portion of said pharmacologically active compound is contained in at least one controlled release particle providing controlled release of the pharmacologically active compound; and wherein the breaking strength of each of the immediate release particles and/or of the at least one controlled release particle is at least 300 N.
Type:
Application
Filed:
April 17, 2017
Publication date:
October 19, 2017
Applicant:
GRÜNENTHAL GMBH
Inventors:
KLAUS WENING, HARALD PAUL, SEBASTIAN SCHWIER, CARMEN STOMBERG
Abstract: The invention relates to certain compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders that are, at least partially, mediated by TSPO activity.
Type:
Grant
Filed:
October 11, 2013
Date of Patent:
October 3, 2017
Assignee:
GRÜNENTHAL GMBH
Inventors:
Petra Bloms-Funke, Gregor Bahrenberg, Wolfgang Schröder, Sven Kühnert, Simon Lucas