Rapidly disintegrating antihistamine formulation

Abstract

The invention relates to a rapidly disintegrating oral antihistamine dosage formulation and method of preparing the rapidly disintegrating formulation wherein the formulation is designed to dissolve in the buccal cavity of the patient.

We claim:  
     
         1 . A rapidly disintegrating oral antihistamine dosage formulation consisting essentially of: 
 a) 5-40 weight percent of antihistamine or pharmaceutically acceptable salt thereof;    b) 40-90 weight percent of a filler;    c) 0.5-10 weight percent of a binder;    d) 0.5 to 10 weight percent of a flavoring agent; and    e) 1-15 weight percent of a disintegrant.    
     
     
         2 . The dosage formulation of  claim 1  wherein the filler is a mixture of water soluble and water insoluble fillers.  
     
     
         3 . The dosage formulation of  claim 2  wherein the water soluble filler comprises at least 50% of the total amount of filler in the dosage formulation.  
     
     
         4 . The dosage formulation of  claim 2  wherein the water soluble filler comprises at least 60% of the total amount of filler in the dosage formulation.  
     
     
         5 . The dosage formulation of  claim 2  wherein the water soluble filler comprises at least 70% of the total amount of filler in the dosage formulation.  
     
     
         6 . The dosage formulation of  claim 1  wherein the antihistamine is selected from the group consisting of astemizole, azatadine, cetrizine, descarboethoxyloratadine, fexofenadine, loratadine or a pharmaceutically acceptable salt thereof.  
     
     
         7 . The dosage formulation of  claim 1  wherein the antihistamine is loratadine.  
     
     
         8 . The dosage formulation of  claim 1  wherein the filler is selected from the group consisting of lactose, starch, dextrose, sucrose, fructose, maltose, mannitol, sorbitol, kaolin, microcrystalline cellulose, powdered cellulose or combinations of the foregoing.  
     
     
         9 . The dosage formulation of  claim 1  wherein the binder is a water soluble polymer.  
     
     
         10 . The dosage formulation of  claim 8  wherein the water soluble polymer is selected from the group consisting of polyvinyl alcohol, polyvinylpyrrolidone, methylcellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, hydroxymethyl cellulose and combinations of the foregoing.  
     
     
         11 . The dosage formulation of  claim 1  wherein the disintegrant is selected from the group consisting of corn starch, croscarmelose sodium, crospovidone sodium starch glycolate or any combination of the foregoing.  
     
     
         12 . The dosage formulation of  claim 10  wherein the disintegrant is crospovidone or sodium starch glycolate.  
     
     
         13 . The dosage formulation of  claim 1  wherein the taste enhancing agent is an artificial sweetener or a flavorant.  
     
     
         14 . The dosage formulation of  claim 12  wherein the taste enhancing agent comprises a mixture of artificial sweeteners and flavorants.  
     
     
         15 . The dosage formulation of  claim 1  wherein the antihistamine is 5-20 weight percent of the formulation, the filler is 60-85 weight percent of the dosage formulation, the binder is 1-5 weight percent of the dosage formulation, the taste enhancing agent is 1-7 weight percent of the dosage formulation and the disintegrant is 2.5-10 weight percent if the dosage formulation.  
     
     
         16 . A rapidly disintegrating oral antihistamine dosage formulation consisting of: 
 a) 5-20 weight percent of loratadine or pharmaceutically acceptable salt thereof;    b) 60-86 weight percent of a filler wherein at least 50 percent of the filler is water soluble;    c) 1-5 weight percent of a binder;    d) 1-7 weight percent of a taste enhancing agent;    e) 2.5-10 weight percent of a disintegrant and    f) 0-5% of conventional tablet processing aids.    
     
     
         17 . A method for manufacturing a rapidly disintegrating oral antihistamine oral dosage formulation comprising: a) preparing a wet granulation consisting essentially of an antihistamine, a binder and 40-70 weight percent of a first allotment of filler based upon the total weight of the filler employed in the final dosage formulation; b) blending the antihistamine granules from step (a) with a disintegrant, a taste enhancing agent and 30-60 weight percent of a second allotment of filler based upon the total weight of the filler employed in the final dosage formulation; and c) compressing the blend of step (b) into a tablet.  
     
     
         18 . The method recited in  claim 17  wherein the first and second allotments of filler are mixtures of water soluble and water insoluble fillers.  
     
     
         19 . The method recited in  claim 18  wherein the first allotment of filler comprises 75-100 percent of the total amount of water insoluble filler used in formulation.  
     
     
         20 . A product prepared according to the method recited in  claim 17.