Tablet quickly disintegrating in the oral cavity and method for producing the same

Abstract

The invention relates to a tablet which is rapidly disintegrated in an oral cavity containing an active ingredient at a high content and a production method thereof. That is, the present invention provides a tablet which is rapidly disintegrated in an oral cavity containing an active ingredient in not less than 25% of the total weight, having a disintegration time of within 40 seconds and an absolute hardness of 1.8 N/mm 2 or more, which is obtained by granulating a powder containing an active ingredient with a binding solution containing mannitol and corn-derived pregelatinized starch, mixing the resulting granules with at least one kind of a disintegrant selected from cornstarch, hydroxypropylstarch, carmellose and crospovidone, and compression molding the mixture.

1 . A tablet, which is rapidly disintegrated in an oral cavity, comprising an active ingredient in not less than 25% of the total weight, which is obtained by compression molding of a mixture comprising a granule comprising the active ingredient, mannitol and corn-derived pregelatinized starch, and at least one kind of disintegrant selected from the group consisting of cornstarch, hydroxypropylstarch, carmellose and crospovidone. 
     
     
         2 . The tablet, which is rapidly disintegrated in an oral cavity, according to  claim 1 , further having a disintegration time of within 40 seconds and an absolute hardness of 1.8 N/mm 2  or more, which is obtained by compression molding of a mixture of a granule produced by granulating a powder containing the active ingredient with a binding solution containing mannitol and corn-derived pregelatinized starch, and at least one kind of disintegrant selected from the group consisting of cornstarch, hydroxypropylstarch, carmellose and crospovidone. 
     
     
         3 . The tablet, which is rapidly disintegrated in an oral cavity, according to  claim 1 , wherein the absolute hardness is 2.0 N/mm 2  or more. 
     
     
         4 . The tablet, which is rapidly disintegrated in an oral cavity, according to  claim 1 , wherein the disintegrant is cornstarch or hydroxypropylstarch. 
     
     
         5 . The tablet, which is rapidly disintegrated in an oral cavity, according to  claim 1 , wherein the powder comprises the active ingredient and mannitol. 
     
     
         6 . The tablet, which is rapidly disintegrated in an oral cavity, according to  claim 1 , comprising the active ingredient in not less than 40% of the total weight. 
     
     
         7 . The tablet, which is rapidly disintegrated in an oral cavity, according to  claim 6 , comprising the active ingredient in 40%-70% of the total weight. 
     
     
         8 . The tablet, which is rapidly disintegrated in an oral cavity, according to  claim 1 , wherein the active ingredient is droxidopa or levodopa. 
     
     
         9 . A method of producing a tablet, which is rapidly disintegrated in an oral cavity, comprising an active ingredient in not less than 25% of the total weight, which method comprises the following steps:
 (1) a step of granulating a powder comprising the active ingredient with a binding solution comprising containing mannitol and corn-derived pregelatinized starch to produce a granule containing the active ingredient;   (2) a step of mixing the granule comprising the active ingredient obtained in (1) with at least one kind of disintegrant selected from the group consisting of cornstarch, hydroxypropylstarch, carmellose and crospovidone; and   (3) a step of compression molding a pre-tableting composition comprising the mixture obtained in (2).   
     
     
         10 . The production method of the tablet, which is rapidly disintegrated in an oral cavity, according to  claim 9 , comprising the following steps:
 (1) a step of granulating a powder comprising the active ingredient with a binding solution comprising mannitol and corn-derived pregelatinized starch to produce a granule containing the active ingredient;   (2) a step of mixing the granule comprising the active ingredient obtained in (1) with at least one kind of disintegrant selected from the group consisting of cornstarch, hydroxypropylstarch, carmellose and crospovidone; and   (3) a step of compression molding of the mixture obtained in (2).   
     
     
         11 . The method according to  claim 9 , wherein a disintegration time of the tablet, which is rapidly disintegrated in an oral cavity, is 40 seconds or less, and an absolute hardness thereof is 1.8 N/mm 2  or more. 
     
     
         12 . The method according to  claim 9 , comprising a step of compression molding by an external lubrication method. 
     
     
         13 . The method according to  claim 9 , wherein the absolute hardness of the tablet, which is rapidly disintegrated in an oral cavity, is 2.0 N/mm 2  or more. 
     
     
         14 . The method according to  claim 9 , wherein the active ingredient is droxidopa or levodopa.