Sustained release oral preparations

Abstract

An object of the present invention is to provide a pharmaceutical preparation containing the drug as an active ingredient, which is capable of improving the QOL and the compliance of the patient who doses the drug while avoiding any excessive increase in the plasma level of the drug by means of controlling the in vivo release rate of the drug and also by means of reducing the frequency of taking the drug.

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       16 . A method for producing a medium dispersion preparation, characterized by using a fully intermeshing twin-screw compounding extruder having a kneading element in its screw shaft.  
   
   
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       32 . A method for producing a controlled release oral preparation comprising a composition of which 2-amino-3-cyano-5-(2-fluorophenyl)-4-methylpyrrole as an active ingredient is dispersed and enclosed in a pharmaceutically acceptable medium consisting essentially of a hydrogenated oil and a hydroxyalkyl cellulose, comprising the steps of: 
 a. processing a mixture including the active ingredient and the medium with applying heat in a fully intermeshing twin-screw compounding extruder to obtain a composition of which the active ingredient is dispersed and enclosed in the medium;    b. granulating the composition; and    c. producing the preparation from the granules, whereby the preparation exhibits a release ratio of the active ingredient of 0 to 70% by weight after 1 hour, 0 to 80% by weight after 2 hours, 5 to 95% by weight after 4 hours, 10 to 100% by weight after 8 hours, 20 to 100% by weight after 12 hours and 50 to 100% by weight after 24 hours in the dissolution test as directed in Method 2 under the 13 th  Japanese Pharamacopoeia.    
   
   
       33 . The method according to  claim 32 , wherein the medium further contains a higher fatty acid.  
   
   
       34 . The method according to  claim 32 , wherein the hydrogenated oil is hydrogenated castor oil or hydrogenated rapeseed oil.  
   
   
       35 . The method according to  claim 32 , wherein the hydroxyalkyl cellulose is hydroxypropyl cellulose or hydroxypropylmethy cellulose.  
   
   
       36 . The method according to  claim 33 , wherein the higher fatty acid is stearic acid.