Pharmaceutical composition of topiramate

Abstract

The invention is directed to a pharmaceutical composition of topiramate, an anticonvulsant which is useful for treating epilepsy. More specifically, the present invention provides a solid dosage formulation of topiramate intended primarily for use by pediatric patients, or for patients who have difficulty swallowing tablets. Processes for preparing the pharmaceutical composition are also described.

1 . A method of treating convulsions comprising administering to a mammal in need thereof a therapeutically effective amount of a pharmaceutical composition comprising
 (a) core particles containing an active agent of topiramate, a binder and a diluent wherein the core particles have an initial particle size between about 0.100 mm and 2.5 mm; and   (b) a taste mask coating, wherein the taste mask coating comprises between about 7% by weight and about 15% by weight of the pharmaceutical composition and wherein the coated particles of the pharmaceutical composition have a final particle size of between about 0.100 mm to about 2.5 mm; and   wherein the coated particles are sprinkled onto soft food and swallowed.   
     
     
         2 . The method of  claim 1 , wherein the diluent in the core particles is sugar spheres. 
     
     
         3 . The method of  claim 2 , wherein the taste masking mixture comprises about 9 to about 13% by weight of the pharmaceutical composition. 
     
     
         4 . The method of  claim 3 , wherein the taste mask coating comprises about 11% by weight of the pharmaceutical composition. 
     
     
         5 . The method of  claim 1 , wherein the core particles have an initial particle size between about 0.5 mm and 1.5 mm and the coated particles of the pharmaceutical composition have a final particle size between about 0.5 mm and 1.5 mm. 
     
     
         6 . The method of  claim 5 , wherein the core particles have an initial particle size between about 0.710 mm and 1.18 mm and the coated particles of the pharmaceutical composition have a final particle size between about 0.850 mm and 1.18 mm. 
     
     
         7 . The method of  claim 1 , wherein the binder is selected from povidone, HPMC, sodium alginate, panwar gum, acacia gum, gelatin, sugar, molasses, starch, pregelatinized starch, methycellulose, ethylcellulose or caroboxymethylcellulose; and the taste mask coating comprises a taste masking agent and a disintegrant, wherein the taste masking agent is selected from cellulose acetate, methylcellulose, ethylcellulose, a Eudragit or cellulose acetate butyrate; and the disintegrant is selected from povidone, cellulose, carboxymethylcellulose, croscarmellose sodium, magnesium aluminate silicate, starch, sodium starch glycolate, pregelatinized starch, alginic acid or guar gum. 
     
     
         8 . The method of  claim 7 , wherein the binder is povidone, the taste masking agent is cellulose acetate and the disintegrant is povidone. 
     
     
         9 . The method of  claim 8 , wherein the coated particles of the pharmaceutical composition are encapsulated. 
     
     
         10 . A method of treating epilepsy comprising administering to a mammal in need thereof a therapeutically effective amount of a pharmaceutical composition comprising
 (a) core particles containing an active agent of topiramate, a binder and a diluent wherein the core particles have an initial particle size between about 0.100 mm and 2.5 mm; and   (b) a taste mask coating, wherein the taste mask coating comprises between about 7% by weight and about 15% by weight of the pharmaceutical composition and wherein the coated particles of the pharmaceutical composition have a final particle size of between about 0.100 mm to about 2.5 mm; and   wherein the coated particles are sprinkled onto soft food and swallowed.   
     
     
         11 . The method of  claim 10 , wherein the diluent in the core particles is sugar spheres. 
     
     
         12 . The method of  claim 11 , wherein the taste masking mixture comprises about 9 to about 13% by weight of the pharmaceutical composition. 
     
     
         13 . The method of  claim 3 , wherein the taste mask coating comprises about 11% by weight of the pharmaceutical composition. 
     
     
         14 . The method of  claim 10 , wherein the core particles have an initial particle size between about 0.5 mm and 1.5 mm and the coated particles of the pharmaceutical composition have a final particle size between about 0.5 mm and 1.5 mm. 
     
     
         15 . The method of  claim 14 , wherein the core particles have an initial particle size between about 0.710 mm and 1.18 mm and the coated particles of the pharmaceutical composition have a final particle size between about 0.850 mm and 1.18 mm. 
     
     
         16 . The method of  claim 10 , wherein the binder is selected from povidone, HPMC, sodium alginate, panwar gum, acacia gum, gelatin, sugar, molasses, starch, pregelatinized starch, methycellulose, ethylcellulose or caroboxymethylcellulose; and the taste mask coating comprises a taste masking agent and a disintegrant, wherein the taste masking agent is selected from cellulose acetate, methylcellulose, ethylcellulose, a Eudragit or cellulose acetate butyrate; and the disintegrant is selected from povidone, cellulose, carboxymethylcellulose, croscarmellose sodium, magnesium aluminate silicate, starch, sodium starch glycolate, pregelatinized starch, alginic acid or guar gum. 
     
     
         17 . The method of  claim 16 , wherein the binder is povidone, the taste masking agent is cellulose acetate and the disintegrant is povidone. 
     
     
         18 . The method of  claim 17 , wherein the coated particles of the pharmaceutical composition are encapsulated. 
     
     
         19 . A pharmaceutical composition, process for making a pharmaceutical composition, method of using a pharmaceutical composition or any other invention substantially as described herein.