Orally-disintegrating solid preparation

Abstract

The present invention provides an orally-disintegrating solid preparation such as a tablet produced by tabletting fine granules showing controlled release of a pharmaceutically active ingredient and an additive, and the like, and the orally-disintegrating solid preparation containing fine granules coated with a coating layer containing a polymer affording a casting film having an elongation at break of about 100-about 700%. With the preparation, breakage of fine granules during tabletting can be suppressed in the production of an orally-disintegrating solid preparation containing fine granules showing controlled release of a pharmaceutically active ingredient.

1 - 39 . (canceled) 
     
     
         40 . An orally-disintegrating solid preparation comprising enteric fine granules, the enteric fine granules comprising core granules comprising lansoprazole or an optically active form thereof or a salt thereof as a pharmaceutically active ingredient, a controlled release film, and an intermediate coating layer formed between the controlled release film and the core granules, the controlled release film comprises a polymer comprising a methacrylic acid-methyl acrylate-methyl methacrylate copolymer affording a casting film having an elongation at break of 100%-700%,
 wherein the intermediate coating layer comprises one or more kinds selected from the group consisting of low-substituted hydroxypropyl cellulose, hydroxypropyl cellulose, hypromellose, polyvinylpyrrolidone, polyvinyl alcohol, methylcellulose and hydroxyethylmethylcellulose, wherein the amount of the intermediate coating layer to be applied is 0.02 part by weight to 1.5 part by weight per 1 part by weight of the granules core comprising the pharmaceutically active ingredient,   wherein the amount of the pharmaceutically active ingredient dissolved from the enteric fine granules showing controlled release of the pharmaceutically active ingredient is not more than 10% in 2 hours as expressed by the dissolution rate in a pH 1.2 solution, and not more than 5% in 1 hour as expressed by the dissolution rate in a pH 6.8 solution,   wherein the enteric fine granules have an average particle size of 500 μm or below, and   wherein the pharmaceutically active ingredient is unstable in acid.   
     
     
         41 . The preparation of  claim 40 , further comprising a plasticizer. 
     
     
         42 . The preparation of  claim 40 , wherein the granules have an enteric layer comprises one or more kinds selected from the group consisting of hypromellose phthalate, cellulose acetate phthalate, carboxymethyl ethyl cellulose, methyl methacrylate-methacrylic acid copolymer, methacrylic acid-ethyl acrylate copolymer, methacrylic acid-methyl acrylate-methyl methacrylate copolymer, ethyl acrylate-methyl methacrylate-trimethylammonioethyl methacrylate chloride copolymer, butyl methacrylate-2-dimethylaminoethyl methacrylate-methyl methacrylate copolymer, ethyl acrylate-methyl methacrylate copolymer, hydroxypropyl methylcellulose acetate succinate, polyvinyl acetate phthalate and shellac. 
     
     
         43 . The preparation of  claim 40 , wherein the controlled release film is coated in an amount of 5-80 wt % of the core granules comprising the pharmaceutically active ingredient. 
     
     
         44 . The preparation of  claim 40 , further comprising a coating layer comprising a water-soluble sugar alcohol as the outermost layer of the enteric fine granules. 
     
     
         45 . The preparation of  claim 41 , wherein the content of the plasticizer is 1-20 wt % of the weight of the solid content of the polymer. 
     
     
         46 . The preparation of  claim 41 , wherein the plasticizer is triethyl citrate. 
     
     
         47 . The preparation of  claim 40 , wherein the enteric fine granules comprising the pharmaceutically active ingredient are pH-dependent controlled release fine granules. 
     
     
         48 . The preparation of  claim 40 , wherein the controlled release film comprises a polymer substance that is soluble at pH less than 7.5, but not at pH less than 6.0. 
     
     
         49 . The preparation of  claim 40 , wherein the core granules further comprise a basic inorganic salt. 
     
     
         50 . The preparation of  claim 40 , wherein the controlled release film has a polymer substance content of 30-100 wt % of the enteric fine granules. 
     
     
         51 . The preparation of  claim 40 , wherein the controlled release film has a polymer substance content of 50-100 wt % of the enteric fine granules.