Methods for the preparation of controlled gastric residence time medicament formulations

Claim 1

A method of preparing a controlled gastric residence medicament formulation comprising: a. applying a first coating to a medicament core of a non-toxic, water hydratable and water permeable, polymeric film comprising a ratio of eight parts of a prepolymer of the formula: ##STR2## wherein R 1 and R 2 are independently, hydrogen, hydroxy, halo having an atomic weight of 19 to 36, alkyl having 1 to 16 carbon atoms, substituted aralkyl or SO 3 H; polymerized with alkylvinylether having 1 to 16 carbon atoms, alkene, aryl, aralkyl, or substituted aralkyl and represents an average polymer molecular weight of from 100,000 to 5,000,000; said prepolymer cross-linked with from about 0.15 to about 2 parts of a cross-linking agent selected from the group consisting of alkylene diol, polyalkylene glycols, polyoxyethylene sorbitan ethers, diamines, and triols, about 1 to about 10 parts of plasticizer selected from the group consisting of glycerol triacetate, ethylacetate, diethylphthalate, dibutyl phthalate, di(n-butyl)sebacate, propylene glycol, polyethylene glycol, glycerin, sorbitol and mixtures thereof; b. treating the polymeric film coated core with a volatile amine vapor for about 5 minutes to about 24 hours; c. coating the amine treated polymeric film core with a second coating of the polymeric film of step (a); and d. maintaining the coated medicament formulation at a relative humidity of from about 30 to about 95 percent at a temperature of from about 10° to about 90° C. for about 4 to 200 hours to crosslink said second coating.

Claim 2

A method of preparing a controlled gastric residence medicament formulation comprising: a. applying a first coating to a medicament core of a non-toxic, water hydratable and water permeable, polymeric film comprising a ratio of eight parts of a prepolymer of the formula: ##STR2## wherein R 1 and R 2 are independently, hydrogen, hydroxy, halo having an atomic weight of 19 to 36, alkyl having 1 to 16 carbon atoms, substituted aralkyl or SO 3 H; polymerized with alkylvinylether having 1 to 16 carbon atoms, alkene, aryl, aralkyl, or substituted aralkyl and represents an average polymer molecular weight of from 100,000 to 5,000,000; said prepolymer cross-linked with from about 0.15 to about 2 parts of a cross-linking agent selected from the group consisting of alkylene diol, polyalkylene glycols, polyoxyethylene sorbitan ethers, diamines, and triols, about 1 to about 10 parts of plasticizer selected from the group consisting of glycerol triacetate, ethylacetate, diethylphthalate, dibutyl phthalate, di(n-butyl)sebacate, propylene glycol, polyethylene glycol, glycerin, sorbitol and mixtures thereof; b. treating the polymeric film coated core with a volatile amine vapor for about 5 minutes to about 24 hours; c. coating the amine treated polymeric film core with a second coating of the polymeric film of step (a); and d. maintaining the coated medicament formulation at a relative humidity of from about 30 to about 95 percent at a temperature of from about 10° to about 90° C. for about 4 to 200 hours to crosslink said second coating.