Pharmaceutical preparation comprising phenylalanine derivative

Abstract

The disclosed pharmaceutical preparation comprises a compound represented by the chemical formula (A) or a pharmaceutically acceptable salt thereof, which is dispersed in a matrix consisting of a water-soluble high molecular weight substance; and Crospovidone: The pharmaceutical preparation is excellent in the solubility and the storage stability even if the amount of the compound or the salt included in each individual dosage unit is increased.

What is claimed is: 
     
         1 . A pharmaceutical preparation comprising the compound represented by the chemical formula (A) or a pharmaceutically acceptable salt thereof, which is dispersed in a matrix consisting of a water-soluble high molecular weight substance, and Crospovidone: 
       
         
           
           
               
               
           
         
       
     
     
         2 . The pharmaceutical preparation as set forth in  claim 1 , wherein the water-soluble high molecular weight substance is at least one member selected from the group consisting of celluloses or derivatives thereof selected from methyl cellulose, hypromellose, hydroxypropyl cellulose, hydroxypropyl-methyl cellulose phthalate, hydroxypropyl-methyl cellulose acetate succinate, carboxymethyl-ethyl cellulose, sodium carboxymethyl cellulose, hydroxyethyl cellulose, and cellulose acetate phthalate; synthetic polymer selected from polyethylene glycol, polyvinyl alcohol, polyvinyl pyrrolidone, polyvinyl-acetal diethylamino acetate, aminoalkyl methacrylate copolymer E, aminoalkyl methacryl copolymer RS, methacrylic acid copolymer L, methacrylic acid copolymer LD, methacrylic acid copolymer S, and carboxy vinyl polymer; and naturally occurring polymers or saccharides selected from gum Arabic, sodium alginate, alginic acid propylene glycol ester, agar, gelatin, tragacanth gum, and xanthane gum. 
     
     
         3 . The pharmaceutical preparation as set forth in  claim 1 , wherein the water-soluble high molecular weight substance is at least one member selected from the group consisting of methyl cellulose, hypromellose, hydroxypropyl cellulose, polyethylene glycol, polyvinyl alcohol and polyvinyl pyrrolidone. 
     
     
         4 . The pharmaceutical preparation as set forth in  claim 1 , wherein it comprises a granulated product formed from a dispersion obtained by dispersing the compound represented by the foregoing chemical formula (A) or a pharmaceutically acceptable salt thereof in the matrix of the water-soluble high molecular weight substance, and Crospovidone. 
     
     
         5 . The pharmaceutical preparation as set forth in  claim 1 , wherein it comprises 14 to 40% by mass of the compound represented by the foregoing chemical formula (A) or a pharmaceutically acceptable salt thereof, the water-soluble high molecular weight substance in an amount ranging from 0.1 to 10 parts by mass per one part by mass of the compound or the pharmaceutically acceptable salt thereof; and 0.1 to 20% by mass of Crospovidone. 
     
     
         6 . The pharmaceutical preparation as set forth in  claim 1 , wherein it further comprises sodium Cros-carmellose. 
     
     
         7 . The pharmaceutical preparation as set forth in  claim 1 , wherein it further comprises an excipient. 
     
     
         8 . The pharmaceutical preparation as set forth in  claim 7 , wherein the excipient is at least one member selected from the group consisting of mannitol, pre gelatinized starch and crystalline cellulose. 
     
     
         9 . The pharmaceutical preparation as set forth in  claim 1 , wherein it is in the form of a tablet. 
     
     
         10 . The pharmaceutical preparation as set forth in  claim 9 , wherein it is in the form of a coating tablet whose surface is covered with a coating agent. 
     
     
         11 . The pharmaceutical preparation as set forth in  claim 10 , wherein the coating agent is at least one member selected from the group consisting of aminoalkyl methacrylate copolymer E, hypromellose, methyl cellulose, methyl-hydroxyethyl cellulose, Opadry, calcium carmellose, sodium carmellose, polyvinyl pyrrolidone, polyvinyl alcohol, dextrin, pullulan, gelatin, agar and gum Arabic.