Back to results
US 4,737,357 AGranted
Aqueous coating dispersions
AssigneeRohm Co., Ltd.
InventorsKlaus Lehmann, Dieter Dreher, Wolfgang Weisbrod
Life of this patent
Estimating the term…
Abstract
Aqueous dispersions of a water-swellable but water-insoluble polymer formed between a quaternary ammonium monomer and a nonionic monomer; methods for making such dispersions by dispersing said copolymers, in the form of a powder, in water; methods for coating pharmaceutical cores, powders, or granules with such dispersions; and coated pharmaceutical products made by such methods.
Claims3
The method of making a pharmaceutical dosage form which comprises the steps of
- (A) preparing a polymer dispersion by dispersing particles of a preformed dry powdered copolymer in an aqueous phase by stirring at an elevated temperature until no sediment forms when said dispersion is allowed to stand, whereby self-emulsifying dispersed particles smaller than said powder particles are formed, said aqueous medium consisting essentially of water or of water and a pharmaceutically acceptable plasticizer for said copolymer, said copolymer being a water swellable but water insoluble copolymer consisting essentially of
- (1) a monoethylenically unsaturated quaternary ammonium compound selected from the group consisting of N-vinyl pyridinium salts and quaternary aminoalkyl esters and quaternary aminoalkyl amides of acrylic acid of methacrylic acid of the formula ##STR2## wherein R is hydrogen or methyl;
- A is oxygen or --NH--;
- B is linear or branched alkyl or an alicyclic hydrocarbon;
- R.sub.1, R.sub.2, and R.sub.3, taken alone, are the same or different alkyl or aralkyl, or R.sub.1 and R.sub.2, taken together with the quaternary nitrogen atom, are piperidinium or morpholinium;
- and
- (2) at least one nonionic monomer, and
- (B) applying said polymer dispersion to a core comprising a pharmaceutically active substance and drying said dispersion.
5 more elements
A method for making a granulation of a pharmaceutically active powder which comprises the steps of
- (A) preparing a polymer dispersion by dispersing particles of a preformed dry powdered copolymer in an aqueous phase by stirring at an elevated temperature until no sediment forms when said dispersion is allowed to stand, whereby self-emulsifying dispersed particles smaller than said powder particles are formed, said aqueous medium consisting essentially of water or of water and a pharmaceutically acceptable plasticizer for said copolymer, said copolymer being a water swellable but water insoluble copolymer consisting essentially of
- (1) a monoethylenically unsaturated quaternary ammonium compound selected from the group consisting of n-vinyl pyridinium salts and quaternary aminoalkyl esters and quaternary aminoalkyl amides of acrylic acid or of methacrylic acid of the formula ##STR3## wherein R is hydrogen or methyl;
- A is oxygen or --NH--;
- B is linear or branched alkyl or an alicyclic hydrocarbon;
- R.sub.1, R.sub.2, and R.sub.3, taken alone, are the same or different alkyl or aralkyl, or R.sub.1 and R.sub.2, taken together with the quaternary nitrogen atom, are piperidinum or morpholinium;
- and
- (2) at least one nonionic monomer, and
- (B) coating said powder with said polymer dispersion and drying said dispersion.
5 more elements
The method for making a film layer having a therapeutically active substance embedded therein which comprises the steps of
- (A) preparing a polymer dispersion by dispersing particles of a preformed dry powdered copolymer in an aqueous phase by stirring at an elevated temperature until no sediment forms when said dispersion is allowed to stand, whereby self-emulsifying dispersed particles smaller than said powder particles are formed, said aqueous medium consisting essentially of water or of water and a pharmaceutically acceptable plasticizer for said copolymer, said copolymer being a water swellable but water insoluble copolymer consisting essentially of
- (1) a monoethylenically unsaturated quaternary ammonium compound selected from the group consisting of N-vinyl pyridinium salts and quaternary aminoalkyl esters and quaternary aminoalkyl amides of acrylic acid or of methacrylic acid of the formula ##STR4## wherein R is hydrogen or methyl;
- A is oxygen or --NH--;
- B is linear or branched alkyl or an alicyclic hydrocarbon;
- R.sub.1, R.sub.2, and R.sub.3, taken alone, are the same or different alkyl or aralkyl, or R.sub.1 and R.sub.2, taken together with the quaternary nitrogen atom, are piperidinum or morpholinium;
- and
- (2) at least one nonionic monomer, and
- (B) mixing said polymer dispersion with said active substance and drying said dispersion in the form of a layer.
5 more elements
Dependencies are inferred from the claim text.