Abstract: 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.
Abstract: Preparation and characterization of novel forms of (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl) phosphonic acid, suitable for pharmaceutical compositions in drug delivery systems for humans.
Type:
Application
Filed:
November 12, 2018
Publication date:
May 16, 2019
Applicant:
GRUNENTHAL GMBH
Inventors:
Mazen HANNA, Ning SHAN, David R. WEYNA, Miranda L. CHENEY
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:
January 9, 2019
Publication date:
May 16, 2019
Applicant:
GRUNENTHAL GMBH
Inventors:
Johannes BARTHOLOMÄUS, Heinrich KUGELMANN, Elisabeth ARKENAU-MARIC
Abstract: The invention relates to a tamper-resistant pharmaceutical dosage form comprising one or more particles, wherein each of said one or more particles comprises a pharmacologically active ingredient and a physiologically acceptable polymer; has a breaking strength of at least 300 N; has a weight of at least 2 mg; and optionally, comprises a film-coating; wherein the total weight of the pharmaceutical dosage form is greater than the total weight of said one or more particles.
Type:
Application
Filed:
November 9, 2018
Publication date:
May 16, 2019
Applicant:
GRÜNENTHAL GMBH
Inventors:
LUTZ BARNSCHEID, ANJA GEIßLER, KLAUS WENING, JANA PÄTZ
Abstract: The invention relates to a reinforced pharmaceutical dosage form comprising a pharmacologically active ingredient and fibers. The reinforced pharmaceutical dosage form is tamper-resistant and thus useful for the avoidance of drug abuse or misuse. The invention also relates to the preparation of such dosage forms and their use in therapy.
Type:
Application
Filed:
January 7, 2019
Publication date:
May 9, 2019
Applicant:
GRÜNENTHAL GMBH
Inventors:
Marcel HAUPTS, Klaus WENING, Carmen STOMBERG, Siegfried EBNER
Abstract: 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.
Type:
Application
Filed:
December 19, 2018
Publication date:
May 2, 2019
Applicant:
Grünenthal GmbH
Inventors:
Sebastian SCHWIER, Marcel HAUPTS, Lutz BARNSCHEID, Jana PÄTZ
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:
Grant
Filed:
September 20, 2017
Date of Patent:
April 23, 2019
Assignee:
GrÜNENTHAL GMBH
Inventors:
Florian Jakob, Sonja Nordhoff, David Rider, Markus Wagener, Gregor Bahrenberg, Torsten Dunkern
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:
October 12, 2018
Publication date:
April 18, 2019
Applicant:
Grünenthal GmbH
Inventors:
Carmen Stomberg, Harald Paul, Klaus Wening, Sebastian Schwier
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:
December 12, 2018
Publication date:
April 18, 2019
Applicant:
GRÜNENTHAL GMBH
Inventors:
KLAUS WENING, ANJA GEIßLER- FICHTNER, JANA DENKER, LUTZ BARNSCHEID
Abstract: The invention relates to 3-(carboxymethyl)-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.
Type:
Application
Filed:
December 7, 2018
Publication date:
April 11, 2019
Applicant:
GRÜNENTHAL GMBH
Inventors:
Sven KUEHNERT, Rene Michael KOENIGS, Florian JAKOB, Achim KLESS, Paul RATCLIFFE, Ruth JOSTOCK, Thomas KOCH, Klaus LINZ, Wolfgang SCHROEDER, Klaus SCHIENE, Anita WEGERT
Abstract: The invention relates to 3-(carboxyethyl)-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.
Type:
Application
Filed:
December 3, 2018
Publication date:
April 4, 2019
Applicant:
GRÜNENTHAL GMBH
Inventors:
Sven KUEHNERT, Rene Michael KOENIGS, Florian JAKOB, Achim KLESS, Anita WEGERT, Paul RATCLIFFE, Ruth JOSTOCK, Thomas KOCH, Klaus LINZ, Wolfgang SCHROEDER
Abstract: Preparation and in vitro and in vivo characterization of novel forms of active pharmaceutical ingredients, suitable for pharmaceutical compositions in drug delivery systems for humans.
Abstract: A hitherto unknown crystalline form of (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride, pharmaceutical compositions containing the new crystalline form, methods of producing the new crystalline form, and a related method of use including treatment of, e.g., pain and/or urinary incontinence.
Type:
Application
Filed:
October 26, 2018
Publication date:
February 28, 2019
Applicant:
Grünenthal GmbH
Inventors:
Andreas FISCHER, Helmut BUSCHMANN, Michael GRUSS, Dagmar LISCHKE
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:
October 22, 2018
Publication date:
February 21, 2019
Applicant:
GRÜNENTHAL GMBH
Inventors:
Klaus Wening, Anja Geissler-Fichtner, Jana Denker, Lutz Barnscheid
Abstract: Preparation, in-vitro and in vivo characterization of novel forms of (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl) phosphonic acid, suitable for pharmaceutical compositions in drug delivery systems for humans.
Abstract: The present invention relates to an abuse-proofed, thermoformed dosage form containing, in addition to one or more active ingredients with abuse potential optionally together with physiologically acceptable auxiliary substances, at least one synthetic or natural polymer with a breaking strength of at least 500 N and to a process for the production thereof.
Type:
Application
Filed:
September 28, 2018
Publication date:
January 31, 2019
Applicant:
GRÜNENTHAL GMBH
Inventors:
Johannes BARTHOLOMÄUS, Heinrich KUGELMANN, Elisabeth ARKENAU-MARIĆ
Abstract: The invention relates to a pharmaceutical dosage form having a density below the density of gastric fluid, wherein the dosage form comprises a pharmacologically active ingredient and a cavity. The invention also relates to a process for the preparation of said dosage form comprising a three-dimensional printing step.
Type:
Application
Filed:
September 18, 2018
Publication date:
January 17, 2019
Applicant:
GRÜNENTHAL GMBH
Inventors:
Klaus WENING, Carmen STOMBERG, Marcel HAUPTS
Abstract: The invention relates to a three-dimensionally printed pharmaceutical dosage form comprising a first pharmacologically active ingredient and a second pharmacologically active ingredient; wherein the relative weight ratio of the first pharmacologically active ingredient to the second pharmacologically active ingredient in the pharmaceutical dosage form is within the range of from 10,000:1 to 1:1. The invention also relates to a process for the preparation of such pharmaceutical dosage form by three-dimensional printing, preferably by fused deposition modeling.
Type:
Application
Filed:
September 18, 2018
Publication date:
January 17, 2019
Applicant:
GRÜNENTHAL GMBH
Inventors:
Carmen STOMBERG, Klaus WENING, Marcel HAUPTS
Abstract: The invention relates to 1,3-diaza-spiro-[3.4]-octane derivatives, their preparation and use in medicine, particularly in various neurological disorders, including but not limited to pain, neurodegenerative disorders, neuroinflammatory disorders, neuropsychiatric disorders, substance abuse/dependence.
Type:
Application
Filed:
July 12, 2018
Publication date:
January 17, 2019
Applicant:
GRÜNENTHAL GMBH
Inventors:
Paul RATCLIFFE, Ingo KONETZKI, Nikolay SITNIKOV, Thomas KOCH, Ruth JOSTOCK
Abstract: 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.
Type:
Application
Filed:
July 11, 2018
Publication date:
January 10, 2019
Applicant:
GRÜNENTHAL GMBH
Inventors:
Elisabeth ARKENAU MARIC, Johannes BARTHOLOMAEUS, Heinrich KUGELMANN