Roehm Gmbh & Co Kg

Evonik Roehm Gmbh

Evonik Rohm Gmbh

Evonik Operations Gmbh

Universitéde Montreal

Christian Meier

Hans-Ulrich Petereit

Erna Roth

Klaus Schultes

Andreas Gryczke

Thomas Suefke

Rosario Lizio

Michael Damm

Jan Hendrik Schattka

Thomas Boller

Jean-Christophe Leroux

Florian Hermes

Johannes Vorholz

Andreas Weber

Michael Korell

Kathrin Nollenberger

Roger Recktenwald

Ruediger Alexowsky

Marcus Denger

Norbert Hoffmann

Michael Schnabel

Stefan Menzler

Norbert Windhab

Sven Balk

Thomas Riermeier

Stephan Wieber

Thomas Hasskerl

Stefan Bernhardt

Dirk Poppe

Manfred Assmus

Günter Schmitt

Michael Gottschalk

Benedikt Hartwig

Melanie Liefke

Herbert Jung

Markus Pridöhl

Jennifer Dressman

Nikolaos Papadopoulos

Pamela Boehmann

Andreas Klosendorf

Alpertunga Kueksal

Stefan Grimm

Marie-Andree Yessine

Fang Liu

Abdul W Basit

Thomas Dassinger

Juan Tome Alcalde

Christine Körner

Johanna Eisele

Senada Schaack

Malin Kummer

Ingrid Blesing

Thomas Eurich

Michael Flittner

Rene Leubert

Hedi Krachtus

Jessica Del Rosario Ferrand

Jörn Klaus Erich Wolf

Angela Olf

Christine Miess

Marie-Andrée Yessine

Alpertunga Küksal

Pamela Böhmann

René Leubert

Karin Knuppen

Rüdiger Alexowsky

Markus PRIDÖHL

Thomas Endres

Marie Andree Yessine

The present invention relates to a process for oxidizing secondary amino groups to the corresponding radical nitroxyl groups within a polymer comprising, for example, 2,2,6,6-tetramethylpiperidinyl units. The process assures a particularly high degree of oxidation.

Method for the improved oxidation of secondary amine groups

The present invention relates to a process for polymerization, wherein the monomers are used in the form of solid particles in an aqueous phase. The polymers obtained thereby can be oxidized further to polymers which can be used as electrical charge storage means, especially secondary batteries.

Method for producing an electrode material

The present invention relates to the technical field of 3D printing, especially in the form of the binder jetting method, in which particulate material in a powder bed is bonded by means of a printed adhesive to form a three-dimensional object. The particulate materials may be inorganic materials, for example sand or a metal powder, or particulate polymeric materials, for example polymethacrylates or polyamides. For this purpose, polymethacrylates may take the form, for example, of suspension polymers, called bead polymers. The present invention relates to the use of porous particles in the binder jetting process, in particular of porous suspension polymers. These powders for 3-D printing differ from the prior art in that the porosity results in a faster and better absorption of the printed binder by the powder particles. A great advantage of this procedure is additionally that a product with less warpage is formed and that the end product has a better surface appearance.

Production and use of porous bead polymers in 3D printing using the binder jetting method

The invention provides a gastric resistant, enteric-coated solid dosage form including a core containing a pharmaceutically active ingredient, an inner coating for the core, and an outer enteric coating. The inner coating comprises an anionic polymeric material or a water-soluble neutral polymeric material, and further comprises a water soluble inorganic salt which is not a carbonate or bicarbonates. The outer enteric coating comprises an anionic polymeric material which is less neutralized than the polymeric material comprising the inner coating and disintegrates rapidly at a pH of 5.5 to 7.0 upon entering the small intestine.

Solid dosage forms comprising an enteric coating with accelerated drug release

A powdery or granulated composition, containing: (a) a copolymer containing, in polymerized form, a C- to C-alkyl ester of acrylic or methacrylic acid and an alkyl(meth)acrylate monomer containing a tertiary amino group in an alkyl radical; (b) 0.5 to 10% by weight based on (a) of a dicarboxylic acid having 3 to 10 carbon atoms; and (c) 5 to 20% by weight based on (a) of a fatty monocarboxylic acid having 8 to 18 carbon atoms, where the composition contains at least by 30% by weight of (a), (b), and (c).

Powdery or granulated composition comprising a copolymer, a dicarboxylic acid and a fatty monocarboxylic acid

The invention relates to a coating composition suitable for the coating of a pharmaceutical or nutraceutical dosage form, comprising a core comprising one or more pharmaceutical or nutraceutical active ingredients, wherein the coating composition is comprising at least 20% by weight of an enteric core/shell polymer composition derived from an emulsion polymerization process, wherein either the core of the core/shell polymer composition is formed by a water-insoluble, not cross-linked polymer or copolymer and the shell of the core/shell polymer composition is formed by an anionic polymer or copolymer or vice versa.

Coating composition suitable for pharmaceutical or nutraceutical dosage forms

The invention discloses a gastric resistant pharmaceutical or nutraceutical composition, comprising a core, comprising a pharmaceutical or nutraceutical active ingredient and a gastric resistant coating layer onto the core, wherein the gastric resistant coating layer comprises at least 30% by weight of a (meth)acrylate copolymer comprising polymerized units of 10 to 40% by weight of acrylic or methacrylic acid, 10 to 80% by weight of a C- to C-alkyl ester of acrylic or methacrylic acid and optionally 0 to 60% by weight of another vinylic monomer, whereby the release of the pharmaceutical or nutraceutical active ingredient is not more than 10% under in-vitro conditions at pH 1.2 after 2 hours in medium according to USP with and without the addition of 20% (v/v) ethanol.

Gastric resistant pharmaceutical or nutraceutical composition with resistance against the influence of ethanol

The invention relates to a coating composition suitable for the coating of pharmaceutical or nutraceutical dosage form, comprising a core comprising one or more pharmaceutical or nutraceutical active ingredients, wherein the coating composition is comprising at least 20% by weight of an enteric core/shell polymer composition derived from an emulsion polymerization process, wherein the core of the core/shell polymer composition is formed by a water-insoluble, cross-linked polymer or copolymer and the shell of the core/shell polymer composition is formed by an anionic polymer or copolymer.

The present invention provides a solid dosage form including an inner coating located between a core containing a pharmaceutically active ingredient and an outer enteric coating; wherein the inner coating includes a partially neutralized anionic polymeric material, and at least a carboxylic acid having 2 to 16 carbon atoms the salts thereof or mixtures of the acid and its salt; wherein the outer coating includes an anionic polymeric material which is less or not at all neutralized than the material of the inner coating.

The present invention provides a process for converting a solid (meth)acrylate copolymer into a dispersed form by preparing an aqueous dispersion comprising the components (a) a (meth)acrylate copolymer which is composed of free-radical polymerized methyl methacrylate, ethylacrylate and a salt of 2-trimethylammoniumethyl methacrylate, present in solid form as a powder or as a granulate, (b) up to 50% by weight calculated on the (meth)acrylate copolymer (a) of a dispersing agent selected from the groups of (b) i) plasticizers in combination with emulsifiers and/or (b) ii) pharmaceutically acceptable carbohydrates having 6 to 18 carbon atoms with a functional group and (c) water by mixing the components (a), (b) and (c) to give a suspension which becomes an aqueous dispersion during the conversion of the solid (meth)acrylate copolymer into the dispersed form, characterized in that, the (meth)acrylate copolymer is converted into the dispersed form by means of the presence of the dispersing agent at a temperature of less than 50&#xb0; C.

Process for converting a solid (meth)acrylate copolymer into a dispersed form by means of a dispersing agent

The invention relates to an oral dosage form, comprising at least one biologically active agent, formulation auxiliary substances and magnetizable particles, wherein the dosage form has an at least two phase composition, wherein the phases can dissolve in the body after oral administration due to their formulation and the magnetizable particles are bound in formulation auxiliary substances and are present in a magnetized state, wherein the magnetized particles are present in at least two phases of the dosage form and generate magnetic fields, wherein these phases dissolve at different times in the body after oral administration, and wherein the magnetic field strength with respect to time, position and movement in the body is acquired using a detection system and can be evaluated using a computer-based evaluation system.

Oral dosage form, comprising at least one biologically active agent, formulation auxiliary substances and magnetizable particles

The invention relates to a method for producing an oral form of administration which decomposes immediately and releases active ingredients in the mouth. According to said method, (a) an anionic pharmaceutical active ingredient is intensively mixed with (b) a copolymer consisting of radically polymerized C-Cesters of the acrylic acid or methacrylic acid and other (meth)acrylate monomers containing functional tertiary amino groups, and (c) between 5 and 50 wt. %, in relation to (b), of a C-Ccarboxylic acid in the melted mass; the mixture is solidified and ground to form a powder containing active ingredients having an average particle size of 200 &#x3bc;m or less; and the powder is encapsulated in a water-soluble matrix consisting of pharmaceutically standard adjuvants, on the condition that no more than 3 wt. %, in relation to the copolymer, of emulsifiers with an HLB value of at least 14 must be contained therein. The invention also relates to the powder containing active ingredients and the uses of the same.

Method for producing an immediately decomposing oral form of administration which releases active ingredients

The invention relates to a process for preparing a (meth)acrylate copolymer containing tertiary amino groups by free-radical polymerization in solution from a monomer mixture selected from a) 30 to 70% by weight of a C-C-alkyl ester of acrylic acid or methacrylic acid and b) 70 to 30% by weight of an alkyl ester of acrylic acid or methacrylic acid with a tertiary amino group in the alkyl radical and c) 0 to 10% of further copolymerizable vinyl monomers, whereby one or more polymerization initiators, optionally one or more molecular weight regulators and one or more solvents or of a solvent mixture are added to the monomer mixture to give a polymerization mixture, which is polymerized at temperatures from 30 to 120&#xb0; C. over a period of 2 to 24 hours, where the polymerization mixture is finally polymerized to give a polymerization syrup with a conversion of the monomers to the copolymer of at least 99% by weight, where the polymerization syrup is subsequently degassed by distillation or by extrusion and the degassed polymerization syrup is further comminuted to a copolymer preparation in the form of a granulate or powder, where the copolymer preparation is characterized by a molecular weight (M) of 25.000 to 75.000 g/mol a polydispersity index of 2.1 to 2.9 and a residual solvent concentration of less than 1.000 ppm by weight.

Process for preparing a (meth)acrylate copolymer containing tertiary amino groups by free-radical polymerization in solution

The invention relates to a process for preparing a (meth)acrylate copolymer containing quaternary ammonium groups from a monomer mixture selected from: (a) 80 to 99% by weight of a C1-C4-alkyl ester of acrylic acid or methacrylic acid; and (b) 20 to 1% by weight of an alkyl ester of acrylic acid or methacrylic acid with a quaternary ammonium group in the alkyl radical; and (c) 0 to 10% of further copolymerizable vinyl monomers whereby one or more polymerization initiators, optionally one or more molecular weight regulators and one or more solvents or of a solvent mixture are added to the monomer mixture to give a polymerization mixture, which is polymerized at temperatures from 30 to 120 C over a period of 2 to 24 hours, where the polymerization mixture is polymerized to a polymerization syrup with a conversion of the monomers to the copolymer of at least 99% by weight, where the polymerization syrup is subsequently degassed by distillation or by extrusion and the degassed polymerization syrup is further comminuted to a copolymer preparation in the form of a granulate or powder and where the copolymer preparation is characterized by a molecular weight (Mw) of 25.000 to 50.000, a polydispersity index of 2.0 to 3.0 and a residual solvent concentration of less than 10.000 ppm by weight.

Process for preparing a (meth)acrylate copolymer containing quaternary ammonium groups by free-radical polymerization in solution

The invention relates to a method for producing active ingredient-containing granules or powders involving the following steps: a) melting a mixture consisting of a pharmaceutical active ingredient and of a (meth)acrylate copolymer, which is comprised of 40 to 75 wt. % of radically polymerized C1 to C4 alkyl esters of acrylic acid or of methacrylic acid and can be comprised of 25 to 60 wt. % (meth)acrylate monomers having an anionic group in the alkyl radial; b) extruding the mixture, and; c) comminuting the extrudate to form a granule or powder. The inventive method is characterized in that the active ingredient is the salt of an alkaline substance, and in that the pH value, which can be measured on the obtained powder or granule, is equal to or less than pH 7.0. The invention also relates to pharmaceutical dosage forms or precursors thereof, which can be produced using the inventive method.

Melt extrusion of salts of active ingredients

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Darmstadt, Germany

Christian Meier