Mucoadhesive pharmaceutical composition and preparation method therefor

Abstract

Disclosed is a mucoadhesive pharmaceutical composition comprising a poly-ionic complex of chitosan and a polyacrylic acid polymer. As an oral formulation, the composition has the extended retention time in the gastrointestinal tract by its mucoadhesive and swelling properties, which is useful as sustained release formulations, retentive formulations of active ingredients with limited absorption regions, and active ingredients with pH dependent solubility.

1 . A mucoadhesive pharmaceutical composition, comprising a micronized poly-ionic complex of chitosan and polyacrylic acid. 
     
     
         2 . The mucoadhesive pharmaceutical composition according to  claim 1 , further comprising a water soluble polymer. 
     
     
         3 . The mucoadhesive pharmaceutical composition according to  claim 1 , further comprising an active ingredient. 
     
     
         4 . The mucoadhesive pharmaceutical composition according to  claim 1 , wherein the poly-ionic complex is one micronized to have an average diameter of 1 nm to 300 μm. 
     
     
         5 . The mucoadhesive pharmaceutical composition according to  claim 3 , wherein the active ingredient is in the form of micronized powder, crystalline solid, granule, particle or pellet. 
     
     
         6 . The mucoadhesive pharmaceutical composition according to  claim 3 , wherein the active ingredient is one coated with a mixture of chitosan and polyacrylic acid. 
     
     
         7 . The mucoadhesive pharmaceutical composition according to  claim 1 , wherein the chitosan has a viscosity of 5 to 50,000 cps. 
     
     
         8 . The mucoadhesive pharmaceutical composition according to  claim 1 , wherein the polyacrylic acid has a molecular weight of 50,000 to 6,000,000. 
     
     
         9 . The mucoadhesive pharmaceutical composition according to  claim 1 , wherein the weight ratio of the chitosan to the polyacrylic acid is 1:0.1 to 1:10. 
     
     
         10 . The mucoadhesive pharmaceutical composition according to  claim 2 , wherein the water soluble polymer is selected from the group consisting of water soluble cellulose ether, polyethylene glycol, gelatin, alginate, dextrin, water soluble polyvinyl alcohol derivative and combinations thereof. 
     
     
         11 . An oral formulation, comprising the mucoadhesive pharmaceutical composition according to  claim 1 . 
     
     
         12 . A method for preparing a mucoadhesive pharmaceutical composition, comprising:
 (a) adjusting pH of an acidic aqueous solution of chitosan and an aqueous solution of polyacrylic acid, respectively, and mixing them, or adjusting pH of a mixture of an acidic aqueous solution of chitosan and an aqueous solution of polyacrylic acid, to obtain a poly-ionic complex; and   (b) drying and milling the obtained poly-ionic complex of chitosan and polyacrylic acid to obtain micronized poly-ionic complex.   
     
     
         13 . The method for preparing a mucoadhesive pharmaceutical composition according to  claim 12 , wherein the pH is adjusted to 5.0 to 6.0. 
     
     
         14 . The method for preparing a mucoadhesive pharmaceutical composition according to  claim 12 , wherein the poly-ionic complex is micronized to have an average diameter of 1 nm to 300 μm. 
     
     
         15 . The method for preparing a mucoadhesive pharmaceutical composition according to  claim 12 , further comprising (c) mixing the micronized poly-ionic complex with an active ingredient. 
     
     
         16 . The method for preparing a mucoadhesive pharmaceutical composition according to  claim 15 , wherein the active ingredient is one coated with a mixture of chitosan and polyacrylic acid. 
     
     
         17 . The method for preparing a mucoadhesive pharmaceutical composition according to  claim 12 , further comprising mixing the micronized poly-ionic complex with a water soluble polymer.