Abstract: (EN) The invention relates to the use of a partially neutralized, anionic (meth)acrylate copolymer comprising radically polymerized units of 25 to 95 percent by weight of C1 to C4 alkyl esters of acrylic or methacrylic acid and 5 to 75 percent by weight of (meth)acrylate monomers with an anionic group, at least 4 percent of which are neutralized by means of a base, for producing a medicament that is provided with an active substance-containing core and is coated with the partially neutralized, anionic (meth)acrylate copolymer. Said medicament releases at least 30 percent of the active substance contained therein in 30 minutes at a pH at which the active substance is sufficiently soluble and stable and at which the corresponding medicament that is coated with the non-neutralized anionic (meth)acrylate polymer releases less than 10 percent of the active substance contained therein.

Abstract: The invention relates to the use of mixture of 2 to 60 wt. % of one or more polymers (I) with 40 to 98 wt. % of one or more polymers (II), whereby the polymer (I) is a (meth)acrylate copolymer, containing 90 to 100 wt. % radically polymerised of 40 to 95 wt. % of C1 to C4 alkyl esters of acrylic or methacrylic acid and 5 to 60 wt. % of units of (meth)acrylate monomers with an anionic group with 0 to 10 wt. % of further vinylic polymerisable monomers and polymer(ll) is a vinyl polymer different from polymer (I) or a polysaccharide or a derivative of a polysaccharide, containing 88 to 100 % neutral monomer units and up to 12 wt. % polymerisable monomer units with ionic groups, for production of a coated pharmaceutical formulation, containing an active agent core and a polymeric coating made from the mixture of polymers (I) and (II), characterised in that the glass temperature of polymer (I) is not more than 70° C.

Abstract: The invention relates to an oral multiparticle pharmaceutical dosage form in the form of a receptacle reducing the pH values of stomach, containing a plurality of pellets, particles, granules or agglomerates whose mean diameter ranges from 50 to 2500 ?n substentially consisting of a) an internal matrix layer containing an active agent which is neither peptide or protein, nor the derivatives or conjugates thereof, a lipophilic matrix whose melting point is greater than 37° C. and a polymer with mucoadhesive effect, b) an external film coating substentially consisting of a polymer or an anionic copolymer which is optionally formulated with conventional pharmaceutical additives, wherein the active agent has a water solubility according to DAB 10, of at least 30 volume parts of water for one part by weight of the active agent and is coated with the lipophilic matrix and said active agent-containing lipophilic matrix is coated with a matrix made of a polymer with mucoadhesive effect.

Abstract: The invention relates to a multiparticulate pharmaceutical form, comprising pellets with a multilayer structure for controlled active ingredient release, comprising a) optionally a neutral core (nonpareilles), b) an inner controlling layer comprising a substance having a modulating effect, which is embedded in a matrix which influences the delivery of the modulatory substance and which comprises pharmaceutically usable polymers, waxes, resins and/or proteins, and where appropriate an active ingredient, c) an active ingredient layer comprising an active pharmaceutical ingredient and, where appropriate, a substance having a modulating effect, d) an outer controlling layer comprising at least 60% by weight of one or a mixture of a plurality of (meth) acrylate copolymers where the outer controlling layer has a thickness from 20 to less than 55 ?m and contains 0,1 to 10% by weight of glycerol monostearate, where the multiparticulate pharmaceutical form contains 20 to 60% by weight of the pellets, which are compres

Abstract: The invention relates to a macroporous plastics bead material with an average particle diameter from 10 to 1000 ?m, containing a copolymer of a) 5-60 wt. % vinylically polymerizable monomers with a water solubility of at least 1% at 20° C., b) 1-40 wt. % vinylically polymerizable monomers with an additional functional group, which can enter into covalent bonds with the nucleophilic groups of the ligands in a polymer-like reaction, c) 10-40 wt. % hydrophilic, crosslinking radical-polymerizable monomers with two or more ethylenically unsaturated polymerizable groups and d) 10-60 wt. % vinylically polymerizable monomers with a water solubility of at most 1% at 20° C. are contained, as a rule with the monomers a) to d) adding up to 100%.

Abstract: A pharmaceutical preparation comprising: a) a core with an active ingredient and with an organic acid and/or the salt of an organic acid; and b) a coating which envelops the core and which comprises a polymer content of (meth)acrylate copolymers which have not more than 15% by weight of cationic or anionic groups, and which comprises at least 60% by weight of a (meth)acrylate copolymer which is composed of free-radically polymerized units of 93 to 98% by weight C1- to C4-alkyl esters of acrylic or of methacrylic acid and 7 to 2% by weight (meth)acrylate monomers having a quaternary ammonium group in the alkyl radical, wherein the active ingredient has a solubility in water of at least 10 g/l at 20° C. and the coating comprises silicon dioxide particles having an average particle size in the range from 1 to 50 ?m.

Abstract: A pharmaceutical form, contains an active compound-containing core, which is covered with a coating layer of a gastric juice-resistant, intestinal juice-soluble (meth)acrylate copolymer, a separating layer situated between said core and said coating layer, the separating layer containing a film-forming water-soluble polymer, wherein the separating layer contains at least two layers: an inner layer containing a water-repellent substance, and thereon a layer comprising the film-forming water-soluble polymer.

Abstract: The invention relates to methods for producing drugs having a stable profile for the release of active ingredients, said drugs exhibiting a controlled release characteristic as a result of the coating of vinyl (co)polymers. The inventive methods are characterised in that the coated drugs are conditioned in a fluidised bed coating appliance or a drum coating appliance for at least 10 minutes until a stable profile for the release of active ingredients is reached at a temperature of between 30 and 70° C. A humidity of between 5 and 30% is regulated during the conditioning process.

Abstract: The invention relates to a process for the preparation of cephalexin with the aid of a penicillin amidase immobilized on a crosslinked hydrophilic copolymer which has binding activity for ligands having nucleophilic groups and is in bead form.

Abstract: The invention relates to a multilayer pharmaceutical form for controlled active ingredient release, essentially comprising a) optionally a neutral core (nonpareilles), b) an inner controlling layer comprising a substance having a modulating effect, which is embedded in a matrix which influences the delivery of the modulatory substance and which comprises pharmaceutically usable polymers, waxes, resins and/or proteins, and where appropriate an active ingredient, c) an active ingredient layer comprising an active pharmaceutical ingredient and, where appropriate, a substance having a modulating effect, d) an outer controlling layer comprising at least 60% by weight of one or a mixture of a plurality of (meth)acrylate copolymers composed of 98 to 85 C1 to C4 alkyl esters of (meth)acrylic acid and 2 to 15% by weight of methacrylate monomers with a quaternary ammonium group in the alkyl radical, and, where appropriate, further water-insoluble pharmaceutically usable polymers, where the layers may additionally and

Abstract: 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 C12- to C18-monocarboxylic acid or of a C12- to C18-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.

Abstract: The invention relates to an oral, multiparticle pharmaceutical dosage form containing pellets, the size of which ranges from 50 to 2500 ?m and which essentially consist of: a) an inner matrix layer containing an active substance which is a peptide or a protein, including the derivatives or conjugates thereof, and which is embedded in a matrix consisting of a polymer with mucoadhesive effect, and b) an outer film coating essentially consisting of an anionic polymer or copolymer, which can be optionally formulated with pharmaceutically conventional adjuvants, more particularly softening agents.

Abstract: The invention relates to a process for the preparation of a coating and binding agent for oral or dermal pharmaceutical forms, essentially consisting 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 ammonium groups, the coplymer being present in powdered form having an average particle size of 1–40 ?m, (b) 3 to 15% by weight, based on (a), of an emulsifier having an HLB of at least 14 and (c) 5 to 50% by weight, based on (a), of a C12—to C18-monocarboxylic acid or a C12—to C18-hydroxyl compound, the components (a), (b) and (c) being blended or mixed with one another with or without addition of water and if appropriate with addition of a pharmaceutical active compound and further customary additives and the coating and binding agent being produced from the mixture by melting, casting, spreading or spraying. The invention further relates to the coating and binding agent itself.

Abstract: A pH-sensitive polymer which has cytotoxic or membranolytic properties at pH values below pH 6.5. Carriers for natural or synthetic biomolecules or active pharmaceutical ingredients using such a pH-sensitive polymer.

Abstract: The invention relates to a multilayer pharmaceutical dosage form for the controlled release of active substances, containing: a) a core layer containing a substance that acts in a modulatory manner with regard to the release of active substances, optionally a neutral core and/or an active substance; b) an inner control layer that influences the release of the substance that acts in a modulatory manner and of the optionally contained active substance from the core layer, containing pharmaceutically useable polymers, waxes, resins and/or proteins; c) an active substance layer containing a pharmaceutical active substance and, optionally, a substance that acts in a modulatory manner; d) an outer control layer containing a (meth)acrylate copolymer or a mixture consisting of a number of (meth)acrylate copolymers comprised of 98 to 85 C1-C4 alkyl esters of (meth)acrylic acid and 2 to 15% by weight of methacrylate monomers with a quaternary ammonium group in the alkyl radical and optionally containing pharmaceuticall

Abstract: The invention relates to a multilayer dosage form comprised of: a) a neutral core; b) an inner coating consisting of a methacrylate copolymer; c) an outer coating consisting of a copolymer of which 40 to 95% by weight is composed of radically polymerized C1 to C4 alkyl esters of acrylic acid or of methacrylic acid and of which 5 to 60% by weight is composed of (meth)acrylate monomers having an anionic group in the alkyl radical. The invention is characterized in that the inner coating is essentially comprised of a methacrylate copolymer, of which at least up to 90% by weight consists of (meth)acrylate monomers with neutral radicals, which, in accordance with DIN 53 787, has a minimum film formation temperature of no higher than 30° C., and which contains the pharmaceutical active substance in bound form.

Abstract: The invention relates to a method for producing pharmaceuticals or parts thereof or food supplements or parts thereof, by coating substrates with a film-forming coating agent containing a pigment which is incompatible with the coating agent. The invention also relates to appliances for carrying out said method, especially a drum coater, a mushroom mixer, a fluidised bed appliance or a spray sifter comprising multiple spray devices.

Abstract: The invention relates to a process for synthesis, by inverse bead polymerization of a monomer phase, of a bead-like, cross-linked, hydrophilic copolymer which has binding activity toward ligands containing nucleophilic groups. The invention relates to support polymer materials with high binding capacity for penicillin acylase and low swelling factor, as well as to use of the same.

Abstract: 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 C1-C4 esters 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 C12-C22 carboxylic 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 ?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.

Abstract: The invention relates to a dispersion suitable for use as coating agent and binder for pharmaceutical forms, having a solids content of 10–70% by weight consisting of a) from 90 to 99% by weight of a methacrylate copolymer consisting of at least 90% by weight of (meth)acrylate monomers containing neutral radicals and having a glass transition temperature Tg of from ?20° C. to +20° C. as determined by the DSC method, and b) 1–10% by weight of a nonionic emulsifier having an HLB of from 15.2 to 17.3.