Nateglinide-containing preparation

Abstract

The present invention discloses, as a immediate-release preparation useful as an antidiabetic, a nateglinide-containing preparation comprising nateglinide as an active ingredient wherein the nateglinide is amorphous.

1 . An amorphous nateglinide-containing preparation comprising:
 (a) amorphous nateglinide, and   (b) at least one hydrophilic material selected from the group consisting of a water-soluble polymer, a water-swelling polymer, a sugar alcohol, a salt, and mixtures thereof, wherein said water-soluble polymer or said water-swelling polymer is at least one member selected from the group consisting of a polyvinyl pyrrolidone compound, a polysaccharide, a polyacrylic acid compound, a polylactic acid compound, a polyoxyethylene compound, a polyvinyl alcohol compound, a surfactant, and mixtures thereof,   wherein said amorphous nateglinide is produced by a process comprising
 dissolving nateglinide and said at least one hydrophilic material in a solvent, and 
 removing said solvent to provide said amorphous nateglinide-containing preparation. 
   
   
   
       2 . The amorphous nateglinide-containing preparation according to  claim 1 , wherein said solvent is an organic type solvent comprising an organic solvent or a mixed type of solvent comprising water and an organic solvent wherein said organic solvent is selected from the group consisting of an alcohol, a ketone, a cyclic ether, acetonitrile. 
   
   
       3 . The amorphous nateglinide-containing preparation according to  claim 2 , wherein said solvent is a mixed type of solvent comprising ethanol and water. 
   
   
       4 . The amorphous nateglinide-containing preparation according to  claim 1 , wherein said hydrophilic material is a water-soluble polymer, a water-swelling polymer, a sugar alcohol, and mixtures thereof. 
   
   
       5 . The amorphous nateglinide-containing preparation according to  claim 1 , wherein said polysaccharide is at least one member selected from the group consisting of methylcellulose SM-4, hydroxypropylcellulose SL, hydroxypropylcellulose SSL, and mixtures thereof. 
   
   
       6 . The amorphous nateglinide-containing preparation according to  claim 1 , wherein said polyoxyethylene compound is polyethyleneglycol. 
   
   
       7 . The amorphous nateglinide-containing preparation according to  claim 1 , wherein said sugar alcohol is at least one member selected from the group consisting of sorbitol, xylitol, mannitol, and mixtures thereof. 
   
   
       8 . The amorphous nateglinide-containing preparation according to  claim 1 , wherein said water-swelling polymer is crospovidone (KOLLIDON CL-M). 
   
   
       9 . A tablet comprising said amorphous nateglinide-containing preparation according to  claim 1 . 
   
   
       10 . A capsule comprising said amorphous nateglinide-containing preparation according to  claim 1 , wherein said capsule is filled with a liquid in which said amorphous nateglinide-containing preparation is dissolved. 
   
   
       11 . The capsule according to  claim 10 , wherein said liquid is at least one member selected from the group consisting of a water-soluble polymer, a surfactant, and mixtures thereof. 
   
   
       12 . The capsule according to  claim 11 , wherein said water-soluble polymer or said surfactant is a polyoxyethylene compound. 
   
   
       13 . The amorphous nateglinide-containing preparation according to  claim 1 , wherein said solvent is ethanol. 
   
   
       14 . The amorphous nateglinide-containing preparation according to  claim 1 , wherein said removing comprises evaporation and drying under vacuum. 
   
   
       15 . The amorphous nateglinide-containing preparation according to  claim 1 , wherein the nateglinide in said dissolving is B-type crystals of nateglinide.