Pharmaceutical formulation for treating the upper digestive tract

Abstract

The invention relates to an effervescent tablet for preparing a mouth rinsing solution, wherein the effervescent tablet exhibits a high release rate of budesonide. A high availability of the active ingredient during use as a mouth rinsing solution on the inflamed mucosa of the upper digestive tract is thereby achieved. The advantage of the formulation according to the invention lies in the bioavailability comparable to oral forms of administration, which allows the formulation to be used safely over an extended period of time.

What is claimed: 
     
         1 . A solid pharmaceutical composition comprising a therapeutically effective amount of budesonide in combination with an effervescent mixture of a pharmaceutically acceptable acid in solid form and a compound containing carbonate and/or hydrogen carbonate, wherein said composition is formulated to rapidly dissolve in a specific volume of liquid so as to generate an orally-administrable mouth rinsing solution comprising a therapeutically effective amount of dissolved budesonide suitable for the treatment of inflammatory changes in the upper digestive tract. 
     
     
         2 . The solid pharmaceutical composition according to  claim 1 , wherein said tablet contains from 0.1 to 10 mg of budesonide per composition. 
     
     
         3 . The solid pharmaceutical composition according to  claim 1 , wherein said tablet further comprises polyvinylpyrrolidone in a concentration of from 0.5 to 10% by weight, based on the weight of the composition. 
     
     
         4 . The solid pharmaceutical composition according to  claim 1 , wherein said tablet further comprises ducosate sodium in a concentration of from 0.1‰ to 5.0‰ by weight, based on the composition. 
     
     
         5 . The solid pharmaceutical composition according to  claim 1 , wherein said tablet contains an agent that produces a cooling effect in the mouth in a concentration of from 0.1 to 1.0% by weight, based on the composition. 
     
     
         6 . An effervescent tablet containing budesonide, wherein said tablet is formulated to rapidly dissolve in a specific volume of liquid so as to generate an orally-administrable mouth rinsing solution comprising a therapeutically effective amount of dissolved budesonide suitable for the treatment of inflammatory changes in the upper digestive tract. 
     
     
         7 . The effervescent tablet according to  claim 6 , wherein said tablet contains from 0.1 to 10 mg of budesonide per prepared effervescent tablet. 
     
     
         8 . The effervescent tablet according to  claim 6 , wherein said tablet further comprises polyvinylpyrrolidone in a concentration of from 0.5 to 10% by weight, based on the weight of the prepared effervescent tablet. 
     
     
         9 . The effervescent tablet according to  claim 6 , wherein said tablet further comprises ducosate sodium in a concentration of from 0.1‰ to 5.0‰ by weight, based on the prepared effervescent tablet. 
     
     
         10 . The effervescent tablet according to  claim 6 , wherein said tablet comprises an effervescent mixture of a pharmaceutically acceptable acid in solid form and a compound containing carbonate and/or hydrogen carbonate. 
     
     
         11 . The effervescent tablet according to  claim 6 , wherein said tablet contains an agent that produces a cooling effect in the mouth in a concentration of from 0.1 to 1.0% by weight, based on the prepared effervescent tablet. 
     
     
         12 . An orally-administrable mouth rinsing solution comprising a therapeutically effective amount of dissolved budesonide suitable for the treatment of inflammatory changes in the upper digestive tract prepared by dissolving the effervescent tablet of  claim 1  in a specific volume of liquid. 
     
     
         13 . The orally-administrable mouth rinsing solution according to  claim 12 , wherein said tablet contains from 0.1 to 10 mg of budesonide per effervescent tablet. 
     
     
         14 . The orally-administrable mouth rinsing solution according to  claim 12 , wherein said tablet further comprises polyvinylpyrrolidone in a concentration of from 0.5 to 10% by weight, based on the weight of the effervescent tablet. 
     
     
         15 . The orally-administrable mouth rinsing solution according to  claim 12 , wherein said tablet further comprises ducosate sodium in a concentration of from 0.1‰ to 5.0‰ by weight, based on the effervescent tablet. 
     
     
         16 . The orally-administrable mouth rinsing solution according to  claim 12 , wherein said tablet comprises an effervescent mixture of a pharmaceutically acceptable acid in solid form and a compound containing carbonate and/or hydrogen carbonate. 
     
     
         17 . The orally-administrable mouth rinsing solution according to  claim 12 , wherein said tablet contains an agent that produces a cooling effect in the mouth in a concentration of from 0.1 to 1.0% by weight, based on the prepared effervescent tablet. 
     
     
         18 . A method for the treatment of inflammatory changes in the upper digestive tract, said method comprising (1) dissolving the solid pharmaceutical composition of  claim 1  in a specific volume of liquid to generate a mouth rinsing solution comprising a therapeutically effective amount of dissolved budesonide and (2) orally administering said mouth rinse solution to a patient in need thereof. 
     
     
         19 . The method according to  claim 18 , characterized in that the inflammatory changes of the upper digestive tract are localized in the region of the oral cavity and/or pharynx. 
     
     
         20 . The method according to  claim 18 , characterized in that the inflammatory changes of the upper digestive tract are non-infectious inflammations. 
     
     
         21 . The method according to  claim 18 , characterized in that the inflammatory changes of the upper digestive tract are the result of chemotherapy. 
     
     
         22 . The method according to  claim 18 , characterized in that the inflammatory changes of the upper digestive tract are the result of mucositis, an autoimmune disorder of the oral cavity, Crohn's disease in the upper digestive tract or eosinophilic oesophagitis. 
     
     
         23 . The method according to  claim 18 , wherein said liquid is water. 
     
     
         24 . The method accordingly to  claim 18 , wherein said specific volume of liquid added is 5 to 20 ml. 
     
     
         25 . The method according to  claim 18 , further comprising (3) gargling the mouth rinsing solution for a predetermined time between 2 and 15 minutes and (4) expelling said mouth rinsing solution from the mouth. 
     
     
         26 . A method for the treatment of inflammatory changes in the upper digestive tract, said method comprising (1) dissolving the effervescent tablet of  claim 6  in a specific volume of liquid to generate a mouth rinsing solution comprising a therapeutically effective amount of dissolved budesonide and (2) orally administering said mouth rinse solution to a patient in need thereof. 
     
     
         27 . The method according to  claim 26 , characterized in that the inflammatory changes of the upper digestive tract are localized in the region of the oral cavity and/or pharynx. 
     
     
         28 . The method according to  claim 26 , characterized in that the inflammatory changes of the upper digestive tract are non-infectious inflammations. 
     
     
         29 . The method according to  claim 26 , characterized in that the inflammatory changes of the upper digestive tract are the result of chemotherapy. 
     
     
         30 . The method according to  claim 26 , characterized in that the inflammatory changes of the upper digestive tract are the result of mucositis, an autoimmune disorder of the oral cavity, Crohn's disease in the upper digestive tract or eosinophilic oesophagitis. 
     
     
         31 . The method according to  claim 26 , wherein said liquid is water. 
     
     
         32 . The method accordingly to  claim 26 , wherein said specific volume of liquid added is 5 to 20 ml. 
     
     
         33 . The method according to  claim 26 , further comprising (3) gargling the mouth rinsing solution for a predetermined time between 2 and 15 minutes and (4) expelling said mouth rinsing solution from the mouth.