Patent ID: 8197850
Filing Date: 2012-06-12
Classification: A61K,A61P

Abstract:
1. A medicament based on at least one biguanide anti-hyperglycemic agent which is administered by the oral route, wherein the medicament comprises a plurality of microcapsules for oral administration; wherein the microcapsules have a particle size between 50 and 750 microns; wherein the microcapsules have a core comprising at least one biguanide antihyperglycemic agent; wherein the mean fraction by mass of the biguanide in the microcapsules is greater than 50%; wherein the microcapsules are coated with a coating film adapted to prolong the release in vivo of the biguanide antihyperglycemic agent and to extend over at least 8 hours the dissolution of the biguanide antihyperglycemic agent in an in vitro dissolution test; wherein the coating film comprises at least one film-forming macromolecule and at least one plasticizer; wherein the film forming macromolecules are selected from the group consisting of: cellulose ethers, cellulose ethers/esters, cellulose esters, cellulose diesters, cellulose triesters, cellulose acylate, cellulose diacylate, cellulose triacylate, cellulose diacetate and triacetate, cellulose acetate/propionate, cellulose acetate/butyrate, polymethacrylates, waxes, vinyl acetate copolymers, and mixtures thereof; wherein the plasticizers are selected from the group consisting of: tributyl acetylcitrate, triethyl acetylcitrate, acetylated glycerides, castor oil, dibutyl phthalate, diethyl phthalate, diethyl sebacate, dibutyl sebacate, dimethyl phthalate, glycerol, glycerol monostearate, glyceryl triacetate, polyethylene glycol, polyoxyethylene/polyoxypropylene copolymers, propylene glycol, tributyl citrate, triethyl citrate, adipate, azelate, enzoate, citrate, citric acid esters, vegetable oils, glycerin sorbitol, diethyl oxalate, diethyl malate, diethyl fumarate, dibutyl succinate, diethyl malonate, dioctyl phthalate, glycerol tributyrate, and mixtures thereof; wherein the coating film is not an enteric composition; and wherein the coating film does not have a nitrogenous polymer, present in a proportion of 2 to 25%, by weight on a dry basis with respect to the total mass of the coating composition and composed of at least one polyacrylamide, and/or one poly-N-vinylamide and/or one poly-N-vinyllactam.