Abstract: 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.
Type:
Application
Filed:
April 19, 2018
Publication date:
August 23, 2018
Applicant:
GRÜNENTHAL GMBH
Inventors:
Johannes BARTHOLOMÄUS, Heinrich Kugelmann, Elisabeth Arkenau-Maric
Abstract: The invention relates to a monolithic pharmaceutical dosage form comprising a hot melt-extruded first segment (S1) and a second segment (S2); wherein the first segment (S1) contains at least a first pharmacologically active ingredient (A1) and/or the second segment (S2) contains at least a second pharmacologically active ingredient (A2); and the segment (S1) and/or the segment (S2) is tamper-resistant and/or exhibits a breaking strength of at least 300 N.
Type:
Application
Filed:
January 30, 2018
Publication date:
August 9, 2018
Applicant:
GRÜNENTHAL GMBH
Inventors:
ANJA GEIßLER-FICHTNER, Klaus Wening, Lutz Barnscheid, Jana Pätz
Abstract: The invention relates to Cebranopadol or a physiologically acceptable salt thereof for use in the treatment or the prevention of pain and/or opioid drug dependence in a subject with impaired hepatic and/or renal function.
Type:
Grant
Filed:
January 22, 2016
Date of Patent:
July 17, 2018
Assignee:
GRÜNENTHAL GMBH
Inventors:
Elke Kleideiter, Annette Christoph, Rene Fussen, Joachim Ossig, Ramesh Boinpally
Abstract: 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.
Type:
Application
Filed:
February 21, 2018
Publication date:
June 28, 2018
Applicant:
GRÜNENTHAL GMBH
Inventors:
Lutz BARNSCHEID, Eric GALIA, Sebastian SCHWIER, Ulrike BERTRAM, Anja GEISSLER, Kornelia GRIESSMANN, Johannes BARTHOLOMÄUS
Abstract: 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.
Type:
Application
Filed:
January 24, 2018
Publication date:
May 31, 2018
Applicant:
GRÜNENTHAL GMBH
Inventors:
Johannes Bartholomäus, Heinrich Kugelmann, Elisabeth Arkenau-Maric
Abstract: 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.
Type:
Grant
Filed:
September 1, 2015
Date of Patent:
March 27, 2018
Assignee:
GRÜNENTHAL GMBH
Inventors:
Lutz Barnscheid, Eric Galia, Sebastian Schwier, Ulrike Bertram, Anja Geissler, Kornelia Griessmann, Johannes Bartholomäus
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:
January 12, 2017
Date of Patent:
March 27, 2018
Assignee:
GRÜNENTHAL GMBH
Inventors:
Stefan Schunk, Melanie Reich, Florian Jakob, Nils Damann, Michael Haurand, Achim Kless, Marc Rogers, Kathy Mackenzie
Abstract: The present invention relates to a compound according to general formula (I) which acts as a modulator of FPR2 and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by FPR2.
Type:
Application
Filed:
September 20, 2017
Publication date:
March 22, 2018
Applicant:
GRÜNENTHAL GMBH
Inventors:
FLORIAN JAKOB, SONJA NORDHOFF, DAVID RIDER, MARKUS WAGENER, GREGOR BAHRENBERG, TORSTEN DUNKERN
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: 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: 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: 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: 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: 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: 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: 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 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