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: A composition of matter comprising in combination as component (a) at least one 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol compound, and as component (b) at least one antiepileptic, a pharmaceutical formulation and a dosage form comprising said composition of matter, and a method of treating pain, e.g. neuropathic pain, in which components (a) and (b) are administered simultaneously or sequentially to a mammal, whereby component (a) may be administered before or after component (b) and whereby components (a) or (b) are administered to the mammal either via the same or a different pathway of administration.
Type:
Grant
Filed:
October 30, 2015
Date of Patent:
February 19, 2019
Assignee:
GRUENENTHAL GMBH
Inventors:
Klaus Schiene, Petra Bloms-Funke, Thomas Christoph
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:
Grant
Filed:
July 27, 2012
Date of Patent:
February 12, 2019
Assignee:
GRUENENTHAL GMBH
Inventors:
Sebastian Schwier, Marcel Haupts, Lutz Barnscheid, Jana Pätz
Abstract: The invention relates to substituted spirocyclic cyclohexane derivatives which have an affinity for the ? opioid receptor and the ORL1 receptor, processes for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.
Type:
Grant
Filed:
July 15, 2015
Date of Patent:
February 12, 2019
Assignee:
GRUENENTHAL GMBH
Inventors:
Anita Wegert, Bert Nolte, Klaus Linz, Stephanie Harlfinger, Babette-Yvonne Koegel, Paul Ratcliffe, Fritz Theil, Olga Groeger, Birgit Braun
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 novel substituted pyrimidine compounds of general formula (I) in which the chemical groupings, substituents, variables 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.
Type:
Grant
Filed:
November 17, 2016
Date of Patent:
January 29, 2019
Assignee:
GRUENENTHAL GMBH
Inventors:
Antonio Nardi, Florian Jakob, Ingo Konetzki, Tobias Craan, Christian Hesslinger, Robin Doodeman
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 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 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
Abstract: The invention relates to an oral pharmaceutical dosage form comprising a plurality of coated particles, wherein said coated particles comprise a core which comprises a Tapentadol component and which is coated with a controlled release coating material, wherein the controlled release coating material comprises a lubricant component and a polymer component, wherein the polymer component comprises one or more cellulose ethers and/or one or more acrylates, and wherein the pharmaceutical dosage form provides controlled release of the Tapentadol component.
Type:
Application
Filed:
May 29, 2018
Publication date:
December 27, 2018
Applicant:
GRÜNENTHAL GMBH
Inventors:
Marc SCHILLER, Ulrich REINHOLD, Ulrike BERTRAM, Wolfgang PRANGE, Anika-Anina PHILIPP, Stefanie STRAUB, Annette GRAVE, Norbert POELLINGER
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:
August 29, 2018
Publication date:
December 27, 2018
Applicant:
GRÜNENTHAL GMBH
Inventors:
Klaus WENING, ANJA GEIßLER, 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:
June 25, 2018
Publication date:
December 27, 2018
Applicant:
GRÜNENTHAL GMBH
Inventors:
Judy ASHWORTH, Elisabeth ARKENAU-MARIC, Johannes BARTHOLOMÄUS, Heinrich KUGELMANN
Abstract: The invention relates to Cebranopadol for use in the treatment of pain, wherein Cebranopadol is administered according to an administration regimen comprising (i) a first administration interval, which lasts for at least 2 consecutive days, wherein a first daily dose of Cebranopadol is administered on every day of the first administration interval; and (ii) a second administration interval, which lasts for at least 2 consecutive days and directly follows the first administration interval without interruption, wherein a second daily dose of Cebranopadol is administered on every day of the second administration interval; wherein the first daily dose of Cebranopadol is lower than the second daily dose of Cebranopadol.
Type:
Application
Filed:
August 29, 2018
Publication date:
December 27, 2018
Applicant:
GRÜNENTHAL GMBH
Inventors:
Shaonan WANG, Chiara PIANA, Roberta BURSI
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 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 polyalkylene oxide; and form a discontinuous phase within the matrix material; and method of using said tablet to treat pain and other conditions.
Type:
Application
Filed:
August 30, 2018
Publication date:
December 27, 2018
Applicant:
Grünenthal GmbH
Inventors:
Sebastian Schwier, Marcel Haupts, Udo Rüttgers, Lutz Barnscheid, Jana DENKER
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:
Grant
Filed:
May 27, 2014
Date of Patent:
December 18, 2018
Assignee:
GRÜNENTHAL GMBH
Inventors:
Lutz Barnscheid, Anja Geiβler, Klaus Wening, Jana Pätz
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:
Grant
Filed:
September 14, 2016
Date of Patent:
November 20, 2018
Assignee:
GRÜNENTHAL GMBH
Inventors:
Johannes Bartholomäus, Heinrich Kugelmann, Elisabeth Arkenau-Marić
Abstract: A thermoformed, tamper-resistant pharmaceutical dosage form comprises: a) a pharmacologically active ingredient; b) a polyalkylene oxide having a weight average molecular weight of more than 200,000 g/mol; and c) a zinc component, wherein the content of said zinc component is at least 1 ppm, relative to the total weight of the pharmaceutical dosage form. When the pharmacologically active ingredient is effective against pain, the pharmaceutical dosage form may be used in a method of treating pain. When the pharmacologically active ingredient has abuse potential, the pharmaceutical dosage form may be used in a method of reducing the incidence of the abuse of said pharmacologically active ingredient.
Type:
Application
Filed:
July 20, 2018
Publication date:
November 15, 2018
Applicant:
GRÜNENTHAL GMBH
Inventors:
LUTZ BARNSCHEID, ERIC GALIA, ANJA GEIßLER, JANA PÄTZ, SEBASTIAN SCHWIER, JULIA BARONSKY-PROBST
Abstract: The invention relates to 3-((hetero-)aryl)-alkyl-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:
May 21, 2018
Publication date:
November 15, 2018
Applicant:
GRÜNENTHAL GMBH
Inventors:
Sven KUEHNERT, Rene Michael KOENIGS, Achim KLESS, Anita WEGERT, Paul RATCLIFFE, Ruth JOSTOCK, Thomas KOCH, Klaus LINZ, Wolfgang SCHROEDER, Klaus SCHIENE, Ingo KONETZKI
Abstract: 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.
Type:
Application
Filed:
July 11, 2018
Publication date:
November 8, 2018
Applicant:
GRÜNENTHAL GMBH
Inventors:
JOHANNES BARTHOLOMAEUS, HEINRICH KUGELMANN