Immediately disintegrable medicinal composition

Abstract

The present invention relates to a pharmaceutical composition useful for rapid disintegration, which comprises a sparingly soluble medicament held on a gel-forming water-soluble polymer as a solid dispersion, wherein it contains a salt substance that comprises an alkali and a weak or strong acid and has an endothermic standard enthalpy of solution or heat of solution. Since rapid disintegration of the pharmaceutical composition of the present invention and rapid dissolution of the medicament contained in the preparation can be made in the digestive tracts pH-independently, good bioavailability can be attained.

1 . A rapidly disintegrable pharmaceutical composition which comprises a sparingly soluble medicament held on a gel-forming water-soluble polymer as a solid dispersion, wherein it contains a salt substance that comprises an alkali and a weak or strong acid and has an endothermic standard enthalpy of solution (KJ/mol) or heat of solution (Kcal/mol).  
     
     
         2 . A rapidly disintegrable pharmaceutical composition according to  claim 1 , which further comprises a surfactant, wherein it contains a salt substance that comprises an alkali and a weak or strong acid and has an endothermic standard enthalpy of solution or heat of solution.  
     
     
         3 . A rapidly disintegrable pharmaceutical composition according to  claim 1  or  2 , wherein the salt substance that comprises an alkali and a weak or strong acid and has an endothermic standard enthalpy of solution or heat of solution is at least one substance selected from the group consisting of sodium bicarbonate, potassium bicarbonate, potassium sulfate, potassium chloride, sodium chloride and potassium dihydrogenphosphate.  
     
     
         4 . A rapidly disintegrable pharmaceutical composition according to  claim 3 , wherein the salt substance that comprises an alkali and a weak or strong acid and has an endothermic standard enthalpy of solution or heat of solution is sodium bicarbonate and/or potassium bicarbonate.  
     
     
         5 . A rapidly disintegrable pharmaceutical composition according to any one of  claims 1  to  4 , wherein the salt substance that comprises an alkali and a weak or strong acid and has an endothermic standard enthalpy of solution or heat of solution is contained in an amount of 0.1 part by weight or more based on 1 part by weight of the gel-forming water-soluble polymer.  
     
     
         6 . A rapidly disintegrable pharmaceutical composition according to  claim 5 , wherein the salt substance that comprises an alkali and a weak or strong acid and has an endothermic standard enthalpy of solution or heat of solution is contained in an amount of from 0.1 to 6 parts by weight based on 1 part by weight of the gel-forming water-soluble polymer.  
     
     
         7 . A rapidly disintegrable pharmaceutical composition according to any one of  claims 1  to  6 , which is in the form of tablets, granules or capsules.  
     
     
         8 . A rapidly disintegrable pharmaceutical composition according to any one of  claims 1  to  7 , wherein the sparingly soluble medicament is 4′-[(2-methyl-1,4,5,6-tetrahydroimidazo[4,5-d][1] benzoazepin-6-yl)carbonyl]-2-phenylbenzanilide or a salt thereof.  
     
     
         9 . A pharmaceutical preparation which comprises 4′-[(2-methyl-1,4,5,6-tetrahydroimidazo[4,5-d][1] benzoazepin-6-yl)carbonyl]-2-phenylbenzanilide or a salt thereof and a pharmaceutical carrier that exhibits the dissolution of 75% of said medicament within 15 minutes when a test is performed using 500 ml of the first fluid (pH 1.2) at 100 r.p.m. in accordance with the second method (paddle method) for dissolution specified in  Japanese Pharmacopoeia,  13th Edition.  
     
     
         10 . A pharmaceutical preparation according to  claim 9 , wherein the pharmaceutical carrier as claimed in  claim 9  comprises a gel-forming water-soluble polymer, a surfactant and a salt substance that comprises an alkali and a weak or strong acid and has an endothermic standard enthalpy of solution or heat of solution.