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:
Application
Filed:
September 2, 2016
Publication date:
December 22, 2016
Applicant:
GRÜNENTHAL GMBH
Inventors:
Elisabeth ARKENAU-MARIC, Johannes BARTHOLOMÄUS
Abstract: The invention relates to a form of administration which is secured against misuse and which is thermoformed without extrusion, comprising at least one synthetic or natural polymer having a resistance to breaking of at least 500 N in addition to one or several active ingredients with a misuse potential and, optionally physiologically compatible auxiliary substances. The invention also relates to a method for the production thereof.
Type:
Application
Filed:
August 26, 2016
Publication date:
December 15, 2016
Applicant:
GRUENENTHAL GMBH
Inventors:
Johannes BARTHOLOMÄUS, Heinrich KUGELMANN, Elisabeth ARKENAU-MARIC
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:
August 24, 2016
Publication date:
December 15, 2016
Applicant:
GRÜNENTHAL GMBH
Inventors:
JOHANNES BARTHOLOMAEUS, HEINRICH KUGELMANN
Abstract: The invention relates to novel substituted condensed pyrimidine compounds of general formula (I) in which the chemical groupings, substituents 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:
August 4, 2015
Date of Patent:
November 29, 2016
Assignee:
GRÜNENTHAL GMBH
Inventors:
Ingo Konetzki, Florian Jakob, Tobias Craan, Christian Hesslinger
Abstract: Summary: 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:
August 5, 2016
Publication date:
November 24, 2016
Applicant:
GRÜNENTHAL GMBH
Inventors:
ANJA GEIßLER, KLAUS WENING, LUTZ BARNSCHEID, JANA PÄTZ
Abstract: A tamper-resistant pharmaceutical dosage form comprising two pharmacologically active ingredients, wherein the dosage form provides under in vitro conditions fast release, preferably immediate release according to Ph. Eur., of both pharmacologically active ingredients. The dosage form is useful for pharmaceutical combination therapy that is achieved by administering dosage forms containing more than one pharmacologically active ingredient as fixed-dose combinations.
Type:
Application
Filed:
April 22, 2016
Publication date:
October 27, 2016
Applicant:
GRÜNENTHAL GMBH
Inventors:
KLAUS WENING, LUTZ BARNSCHEID, ANJA GEISSLER, JANA DENKER, JESSICA REDMER
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:
April 22, 2016
Publication date:
October 27, 2016
Applicant:
GRÜNENTHAL GMBH
Inventors:
KLAUS WENING, ANJA GEIßLER, JANA DENKER, LUTZ BARNSCHEID
Abstract: A tamper-resistant pharmaceutical dosage form comprising two pharmacologically active ingredients, wherein the dosage form provides under in vitro conditions fast release, preferably immediate release according to Ph. Eur., of both pharmacologically active ingredients. The dosage form is useful for pharmaceutical combination therapy that is achieved by administering dosage forms containing more than one pharmacologically active ingredient as fixed-dose combinations.
Type:
Application
Filed:
April 22, 2016
Publication date:
October 27, 2016
Applicant:
GRÜNENTHAL GMBH
Inventors:
Klaus WENING, Lutz BARNSCHEID, Anja GEIßLER, Jana DENKER, Jessica REDMER
Abstract: A tamper-resistant pharmaceutical dosage form comprising two pharmacologically active ingredients, wherein the dosage form provides under in vitro conditions fast release, preferably immediate release according to Ph. Eur., of both pharmacologically active ingredients. The dosage form is useful for pharmaceutical combination therapy that is achieved by administering dosage forms containing more than one pharmacologically active ingredient as fixed-dose combinations.
Type:
Application
Filed:
April 22, 2016
Publication date:
October 27, 2016
Applicant:
GRÜNENTHAL GMBH
Inventors:
KLAUS WENING, LUTZ BARNSCHEID, ANJA GEISSLER, JANA DENKER, JESSICA REDMER
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:
Application
Filed:
June 17, 2016
Publication date:
October 6, 2016
Applicant:
GRÜNENTHAL GMBH
Inventors:
Melanie REICH, Stefan SCHUNK, Florian JAKOB, Henning STEINHAGEN, Nils DAMANN, Michael HAURAND, Marc ROGERS, Kathy MACKENZIE
Abstract: The invention relates to a pharmaceutical dosage form having a breaking strength of at least 300 N and comprising a pharmacologically active compound, an anionic polymer bearing carboxylic groups, wherein the content of the anionic polymer is ?20 wt.-%, based on the total weight of the pharmaceutical dosage form, and a nonionic surfactant.
Type:
Application
Filed:
May 27, 2016
Publication date:
September 22, 2016
Applicant:
GRÜNENTHAL GMBH
Inventors:
Lutz BARNSCHEID, Jessica REDMER, Sebastian SCHWIER
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:
April 19, 2016
Publication date:
September 15, 2016
Applicant:
GRÜNENTHAL GMBH
Inventors:
Elisabeth ARKENAU MARIC, Johannes BARTHOLOMAEUS, Heinrich KUGELMANN
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 11, 2016
Publication date:
August 4, 2016
Applicant:
GRÜNENTHAL GMBH
Inventors:
Johannes BARTHOLOMÄUS, Heinrich Kugelmann, Elisabeth Arkenau-Maric
Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.
Type:
Grant
Filed:
March 14, 2013
Date of Patent:
August 2, 2016
Assignee:
GRUENENTHAL GMBH
Inventors:
Bert Nolte, Wolfgang Schröder, Klaus Linz, Werner Englberger, Hans Schick, Heinz Graubaum, Birgit Braun, Sigrid Ozegowski, József Bálint, Helmut Sonnenschein
Abstract: The invention relates to a pharmaceutical dosage form, preferably with controlled release of a pharmacologically active compound (A) contained therein, the pharmaceutical dosage form very preferably being tamper-resistant and most preferably having a breaking strength B1 of at least 500 N in direction of extension E1 and having a breaking strength B2 of less than 500 N in direction of extension E2.
Type:
Application
Filed:
December 11, 2015
Publication date:
July 14, 2016
Applicant:
GRÜNENTHAL GMBH
Inventors:
EUGEEN MARIE JOZEF JANS, FILIP RENÉ IRENA KIEKENS, JODY FIRMIN MARCELINE VOORSPOELS, ANNE FAURE, IRIS ZIEGLER, ELISABETH ARKENAU-MARIC, LUTZ BARNSCHEID, JOHANNES BARTHOLOMÄUS, MARC FREVEL, ERIC GALIA, ANDREA SCHÜESSELE
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:
March 18, 2016
Publication date:
July 14, 2016
Applicant:
Grünenthal GmbH
Inventors:
Sebastian Schwier, Marcel Haupts, Udo Rüttgers, Lutz Barnscheid, Jana Pätz
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:
August 21, 2013
Date of Patent:
July 12, 2016
Assignee:
GRUENENTHAL GMBH
Inventors:
Helmut Heinrich Buschmann, Joerg Holenz
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:
March 3, 2016
Publication date:
June 30, 2016
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:
Application
Filed:
March 4, 2016
Publication date:
June 30, 2016
Applicant:
GRÜNENTHAL GMBH
Inventors:
Elisabeth ARKENAU-MARIC, Johannes Bartholomäus, Heinrich Kugelmann