Abstract: The present invention relates to a process for the production of an abuse-proofed dosage form containing, apart from one or more active ingredients with potential for abuse and optionally physiologically acceptable auxiliary substances, at least one synthetic or natural polymer (C) with a breaking strength of at least 500 N, wherein the formulation mixture is combined with a solvent for the polymer (C) at least in quantities such that the formulation mixture is at least uniformly moistened, the at least moistened composition is optionally divided into sub-portions, dried and shaped to yield the dosage form.
Type:
Grant
Filed:
September 2, 2016
Date of Patent:
August 4, 2020
Assignee:
GRÜNENTHAL GMBH
Inventors:
Elisabeth Arkenau-Marić, Johannes Bartholomäus
Abstract: An aqueous pharmaceutical composition adapted for parenteral administration of tapentadol or a physiologically acceptable salt thereof having a pH value of at least 5.4.
Type:
Application
Filed:
March 13, 2020
Publication date:
July 9, 2020
Applicant:
GRÜNENTHAL GMBH
Inventors:
Thomas CHRISTOPH, Sabine Karine Katrien INGHELBRECHT, Roger Carolus Augusta EMBRECHTS, Ulrich REINHOLD, Marc SCHILLER, Eva WULSTEN, Petra BLOMS-FUNKE, Klaus SCHIENE, Ulrich FEIL
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:
February 21, 2020
Publication date:
July 9, 2020
Applicant:
GRÜNENTHAL GMBH
Inventors:
Elisabeth ARKENAU-MARIC, Johannes BARTHOLOMAEUS, Heinrich KUGELMANN
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:
Grant
Filed:
May 20, 2019
Date of Patent:
June 30, 2020
Assignee:
GRÜNENTHAL GMBH
Inventors:
Sebastian Schwier, Marcel Haupts, Udo Rüttgers, Lutz Barnscheid, Jana Denker
Abstract: The invention relates to a tamper-resistant, oral pharmaceutical dosage form comprising a pharmacologically active ingredient having psychotropic action and an ethylene-vinyl acetate (EVA) polymer which provides resistance against solvent extraction, resistance against grinding, and resistance against dose-dumping in aqueous ethanol.
Type:
Application
Filed:
March 5, 2020
Publication date:
June 25, 2020
Applicant:
GRÜNENTHAL GMBH
Inventors:
Klaus WENING, Lutz Barnscheid, Sebastian Schwier, Anja Geibler
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:
February 21, 2020
Publication date:
June 18, 2020
Applicant:
GRÜNENTHAL GMBH
Inventors:
Johannes BARTHOLOMÄUS, Heinrich KUGELMANN, Elisabeth ARKENAU-MARIC
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:
Grant
Filed:
March 4, 2016
Date of Patent:
June 9, 2020
Assignee:
GRÜNENTHAL GMBH
Inventors:
Elisabeth Arkenau-Marić, Johannes Bartholomäus, Heinrich Kugelmann
Abstract: Compositions are provided that contain a TRPV1 agonist, such as capsaicin, and a solvent system. Topical application of the composition results in rapid delivery of agonist to the dermis and epidermis. Method of using the compositions for reducing nociceptive nerve fiber function in subjects, and for treatment of capsaicin-responsive conditions are also provided.
Type:
Grant
Filed:
August 1, 2017
Date of Patent:
May 19, 2020
Assignees:
GRT US Holding, Inc., Grünenthal GmbH
Inventors:
Naweed Muhammad, Gene Curtis Jamieson, Keith R. Bley, Sanjay Chanda
Abstract: The invention relates to a tamper-resistant, oral pharmaceutical dosage form comprising a pharmacologically active ingredient having psychotropic action and an ethylene-vinyl acetate (EVA) polymer which provides resistance against solvent extraction, resistance against grinding, and resistance against dose-dumping in aqueous ethanol.
Type:
Grant
Filed:
July 10, 2014
Date of Patent:
April 21, 2020
Assignee:
GRÜNENTHAL GMBH
Inventors:
Klaus Wening, Lutz Barnscheid, Sebastian Schwier, Anja Geißler
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 14, 2019
Publication date:
April 2, 2020
Applicant:
Grünenthal GmbH
Inventors:
Andreas FISCHER, Helmut BUSCHMANN, Michael GRUSS, Dagmar LISCHKE
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:
December 3, 2019
Publication date:
April 2, 2020
Applicant:
GRÜNENTHAL GMBH
Inventors:
Lutz BARNSCHEID, Eric GALIA, Sebastian SCHWIER, Ulrike BERTRAM, Anja GEISSLER, Kornelia GRIESSMANN, Johannes BARTHOLOMÄUS
Abstract: Formulations and methods are provided for the treatment of pain, and neuropathic pain in particular. The formulations are eutectic mixtures of a capsaicinoid and a local anesthetic agent and/or an anti-pruritic agent.
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:
August 16, 2019
Publication date:
February 6, 2020
Applicant:
GRÜNENTHAL GMBH
Inventors:
Johannes BARTHOLOMÄUS, Heinrich KUGELMANN, Elisabeth ARKENAU-MARIC
Abstract: Thermoformed pharmaceutical dosage form having a breaking strength of at least 300 N, comprising an opioid (A), a free physiologically acceptable acid (B) in an amount of from 0.001 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.
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 dosage form provides under in vitro conditions immediate release of the pharmacologically active compound in accordance with Ph. Eur. The tamper-resistant pharmaceutical dosage form is useful in methods of treat diseases or disorders susceptible to the pharmacologically active compound; and in some embodiments discourages abuse in that when reduced to a powder the powdered dosage form exhibits a lower score for drug-liking than the pharmacologically active compound itself as assessed on a visual analog scale.
Type:
Application
Filed:
September 27, 2019
Publication date:
January 30, 2020
Applicant:
GRÜNENTHAL GMBH
Inventors:
KLAUS WENING, ANJA GEIßLER- FICHTNER, JANA DENKER, LUTZ BARNSCHEID
Abstract: The present invention relates to compounds according to general formula (I) which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.
Type:
Application
Filed:
July 19, 2019
Publication date:
January 23, 2020
Applicant:
Grünenthal GmbH
Inventors:
Florian JAKOB, Jo ALEN, Simon LUCAS, Tobias CRAAN, Ingo KONETZKI, Achim KLESS, Stefan SCHUNK, Paul RATCLIFFE, Sebastian WACHTEN, Simon CRUWYS
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:
July 19, 2019
Publication date:
January 9, 2020
Applicant:
GRÜNENTHAL GMBH
Inventors:
Johannes BARTHOLOMÄUS, Heinrich KUGELMANN, Elisabeth ARKENAU-MARIC
Abstract: The use of tapentadol in the treatment of pain and/or pain chronification in a subject suffering from pain chronification and/or in the treatment of pain and inhibition of pain chronification in a subject suffering from pain and at risk of pain chronification, as well as the use of tapentadol for the treatment or inhibition of migraine.
Type:
Application
Filed:
July 19, 2019
Publication date:
January 9, 2020
Applicant:
Grünenthal GmbH
Inventors:
Klaus SCHIENE, Ilona STEIGERWALD, Michel HAMON, Johannes SCHNEIDER, Silvia REINARTZ, Ulrich JAHNEL, Thomas TZSCHENTKE
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:
July 19, 2019
Publication date:
January 9, 2020
Applicant:
GRÜNENTHAL GMBH
Inventors:
KLAUS WENING, ANJA GEISSLER, JANA DENKER, LUTZ BARNSCHEID
Abstract: The invention relates to a pharmaceutical composition comprising Tapentadol or a physiologically acceptable salt thereof for use in local anesthesia.