Formulation comprising antibacterial substance and antiulcer substance

Abstract

The present invention includes a formulation which comprises an antibacterial substance and an antiulcer substance, wherein at least either of them is formulated into a gastrointestinal mucosa-adherent solid preparation. The formulation of the present invention shows long retention time in the gastrointestinal tract because of adhesion to the gastrointestinal tract mucosa, synergetically enhances the pharmaceutical effects of an antibacterial substance, specially antibiotic against Helicobacter pylori (HP) and an antiulcer substance, with very low doses of active ingredients, particularly the anti-HP antibiotic with low prevalence of side effects. The present agent is useful as an antiulcer agent, showing potent anti-HP activity.

What we claim is:  
     
         1 . A formulation which comprises an antibacterial substance and an antiulcer substance, wherein at least one of them is formulated into a gastrointestinal mucosa-adherent solid preparation.  
     
     
         2 . The formulation according to    claim 1   , wherein the antibacterial substance is an antibacterial substance against  Helicobacter pylori.    
     
     
         3 . The formulation according to    claim 1   , wherein the gastrointestinal mucosa-adherent solid preparation further comprises a matrix containing a polyglycerin fatty acid ester.  
     
     
         4 . The formulation according to    claim 1   , wherein the gastrointestinal mucosa-adherent solid preparation contains the antibacterial substance.  
     
     
         5 . The formulation according to    claim 1   , wherein the antibacterial substance is a penicillin.  
     
     
         6 . The formulation according to    claim 1   , wherein the antibacterial substance is a macrolide antibiotic.  
     
     
         7 . The formulation according to    claim 5   , wherein the penicillin is amoxicillin.  
     
     
         8 . The formulation according to    claim 1   , wherein the antiulcer substance is a proton pump inhibitor.  
     
     
         9 . The formulation according to    claim 8   , wherein the proton pump inhibitor is a compound represented by the formula: 
                   
       wherein ring A may optionally be substituted, R 1 , R 3  and R 4  are, the same or different, hydrogen, or an alkyl or alkoxy group, R 2  is a hydrocarbon group which may optionally be substituted, and n is 0 or 1, or a salt thereof.  
     
     
         10 . The formulation according to    claim 3   , wherein the gastrointestinal mucosa-adherent solid preparation comprises a viscogenic agent capable of developing viscosity on contact with water.  
     
     
         11 . The formulation according to    claim 10   , wherein the viscogenic agent is dispersed in the gastrointestinal mucosa-adherent solid preparation.  
     
     
         12 . The formulation according to    claim 10   , wherein the viscogenic agent coats the gastrointestinal mucosa-adherent solid preparation.  
     
     
         13 . The formulation according to    claim 10   , wherein the viscogenic agent is an acrylic acid polymer or its salt.  
     
     
         14 . A set for the use in treating a gastrointestinal ulcer in mammals which comprises (1) an antibacterial substance and a pharmaceutically acceptable carrier thereof, and (2) an antiulcer substance and a pharmaceutically acceptable carrier thereof, wherein at least one of the substances is formulated into a gastrointestinal mucosa-adherent solid preparation.  
     
     
         15 . A method of treating a gastrointestinal ulcer in mammals which comprises administering to the mammals a therapeutically effective amount of an antibacterial substance and a therapeutically effective amount of an antiulcer substance.  
     
     
         16 . The method according to    claim 15   , wherein the antibacterial substance and the antiulcer substance are administered simutaneously.  
     
     
         17 . The method according to    claim 15   , wherein the antibacterial substance and the antiulcer substance are administered sequentially.