Patent ID: 7927623
Filing Date: 2011-04-19
Classification: A61K,A61P,C07D

Abstract:
1. An intraorally rapidly disintegrating tablet having hardness of 20 N or more and porosity within the range of 25% to 50%, comprising the following ingredients: i) a medicinal substance selected from the group consisting of: (S)-2-(2-hydroxymethyl-1-pyrrolidinyl)-4-(3-chloro-4-methoxybenzylamino)-5[N-(2-pyrimidinylmethyl)-carbamoyl]pyrimidine; 2-(5,6,7,8-tetrahydroimidazo[1,2-a]pyrazin-7-yl)-4-(3-chloro-4-methoxybenzylamino)-5-[N-(2-pyrimidinylmethyl)-carbamoyl]pyrimidine; 2-(5,6,7,8-tetrahydro-1,7-naphthyridin-7-yl)-4-(3-chloro-4-methoxybenzylamino)-5-[N-(2-morpholinoethyl)carbamoyl]-pyrimidine; and (S)-2-(2-hydroxymethyl-1-pyrrolidinyl)-4-(3-chloro-4-methoxybenzylamino)-5-[N-(5-pyrimidinylmethyl)carbamoyl]-pyrimidine; ii) a water-soluble acidic substance selected from the group consisting of fumaric acid, tartaric acid, succinic acid, malic acid, ascorbic acid and aspartic acid; iii) a water-soluble binding agent being soluble in alcoholic solvent selected from the group consisting of polyvinylpyrrolidone and hydroxypropylcellulose; and iv) a water-soluble saccharide selected from the group consisting of mannitol, xylitol, erythritol, maltitol, sorbitol and lactose, wherein at least one of the ingredients (i) and (ii) is coated with a water-soluble coating agent being insoluble in an alcoholic solvent selected from the group consisting of hydroxypropylmethyl cellulose, methyl cellulose, hydroxyethyl cellulose, dextran, pullulan, agar, sodium arginate, polyvinyl alcohol and gelatine, and which tablet is obtainable by subjecting a mixture containing the ingredients (i), (ii), (iii) and (iv) and optionally one or more pharmaceutically acceptable additives for pharmaceutical preparations to compression, treating the compressed products with an alcohol, and removing the alcohol.