Pharmaceutical composition as solid dosage form and method for manufacturing thereof

Abstract

The present invention relates to a novel pharmaceutical composition as a solid dosage form comprising desmopressin as a therapeutically active ingredient, and to a method for manufacturing thereof. The invention relates to a pharmaceutical composition as a solid dosage form comprising desmopressin, or a pharmaceutically acceptable salt thereof, as a therapeutically active ingredient together with a pharmaceutically acceptable excipient, diluent or carrier, or mixture thereof, wherein at least one of said excipient, diluent and carrier is a substance selected from a monosaccharide, disaccharide, oligosaccharide and a polysaccharide, wherein the said substance has an average particle size in the range of from 60 to 1,000 μm. A method according to the present invention provides an improved production of solid dosage forms of desmopressin.

1 . A pharmaceutical composition as a solid dosage form comprising desmopressin, or a pharmaceutically acceptable salt thereof, as a therapeutically active ingredient together with a pharmaceutically acceptable excipient, diluent or carrier, or mixture thereof, wherein at least one of said excipient, diluent and carrier is a disaccharide, wherein the said disaccharide has an average particle size in the range of from 70 to 500 μm, and wherein said solid dosage form is a tablet.  
   
   
       2 . The pharmaceutical composition according to  claim 1 , wherein said average particle size is in the range of from 75 to 350 μm.  
   
   
       3 . The pharmaceutical composition according to  claim 3 , wherein said average particle size is in the range of from 100 to 200 μm.  
   
   
       4 . The pharmaceutical composition according to  claim 4 , wherein said average particle size is in the range of from 120 to 180 μm.  
   
   
       5 . The pharmaceutical composition according to  claim 1 , wherein said disaccharide is lactose.  
   
   
       6 . The pharmaceutical composition according to  claim 1 , wherein the total combined amount of said excipient, diluent and carrier is from 5 to 99 percent by weight of the pharmaceutical composition.  
   
   
       7 . The pharmaceutical composition according to  claim 1 , which comprises desmopressin acetate in an amount of from 20 to 600 μg per unit of solid dosage form.  
   
   
       8 . The pharmaceutical composition according to  claim 5 , wherein said lactose is lactose-α-monohydrate.  
   
   
       9 . The pharmaceutical composition according to  claim 6 , wherein the total combined amount of said excipient, diluent and carrier is from 50 to 99 percent by weight of the pharmaceutical composition.  
   
   
       10 . The pharmaceutical composition according to  claim 1 , wherein said tablet is adapted for administration by a route selected from the group consisting of oromucosal, buccal and sublingual administration.