Evonik Roehm Gmbh

Evonik Rohm Gmbh

Roehm Gmbh & Co Kg

Andreas Gryczke

Christian Meier

Hans-Ulrich Petereit

Norbert Windhab

Rosario Lizio

Erna Roth

Michael Damm

Michael Gottschalk

Benedikt Hartwig

Melanie Liefke

Kathrin Nollenberger

Pravin Nalawade

Smitha Shetty

Juan Tome Alcalde

Jennifer Dressman

Angela Olf

Shripad Gadhinglajkar

Hema Ravishankar

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 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

A pellet or pellets having an average particle size in the range from 300 to 1,100 &#x3bc;m, comprising a pharmaceutically active substance embedded in a polymer matrix of one or more water-insoluble polymers, wherein the polymer matrix additionally contains 10 to 90% by weight of an anionic polymer and with the proviso that the pellets release no more than 10% of the active compound contained in the release test according to USP in artificial gastric juice at pH 1.2 after 120 min and release at least 50% of the active compound contained after altogether a further 300 min at pH 6.8 and/or pH 7.5.

Pellets having a gastric juice-resistant active compound matrix

The invention relates to a process for the production of granules or powders, suitable as coating agents and binders for oral or dermal pharmaceutical forms, for cosmetics or food supplements, consisting essentially of (a) a copolymer, consisting of free radical-polymerized C1- to C4-esters of acrylic or methacrylic acid and further (meth)acrylate monomers which contain functional tertiary amino groups, (b) 3 to 25% by weight, based on (a), of an emulsifier having an HLB of at least 14, (c) 5 to 50% by weight, based on (a), of a C- to C-monocarboxylic acid or of a C- to C-hydroxyl compound, where the components (a), (b) and (c) are simultaneously or successively blended or mixed with one another, optionally with addition of a pharmaceutical active compound and/or further customary additives, fused in a heatable mixer, mixed, the melt is cooled and comminuted to give granules or powders.

Granulate or powder for producing coating or binding agents for medicaments

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Griesheim, Germany

Andreas Gryczke