Orodispersible tablets containing fexofenadine

Abstract

The present invention concerns orodispersible tablets, which are able to disintegrate in the buccal cavity upon contact with saliva by formation of an easy-to-swallow suspension, in less than 60 seconds, preferably in less than 40 seconds, containing fexofenadine in the form of coated granules, and a mixture of excipients comprising at least one disintegrating agent, a soluble diluent agent, a lubricant and optionally a swelling agent, a permeabilising agent, sweeteners, flavoring agents and colors; the process for obtaining such orodispersible tablets and the coated granules incorporated therein and the use of said orodispersible tablets in the treatment of seasonal allergic rhinitis.

1 - 13 . (canceled)  
     
     
         14 . Granules of fexofenadine, or one of its pharmaceutically acceptable salts, wherein the granules are coated and contain: 
 microcrystals of fexofenadine, or one of its pharmaceutically acceptable salts,    at least one binder selected from the group consisting of cellulosic polymers, such as ethylcellulose, hydroxypropylcellulose and hydroxypropylmethylcellulose, acrylic polymers such as insoluble acrylate ammoniomethacrylate copolymer, polyacrylate or polymethacrylic copolymer, povidones, copovidones, polyvinylalcohols, alginic acid, sodium alginate, starch, pregelatinized starch, sucrose and its derivatives, guar gum, polyethylene glycol and mixtures thereof.    
     
     
         15 . Granules according to  claim 14  which further contain a diluent agent selected from the group consisting of microcrystalline cellulose, sucrose, dicalcium phosphate starches, lactose, polyols of less than 13 carbon atoms such as mannitol, xylitol, sorbitol, maltitol, pharmaceutically acceptable amino acids such as glycin, and their mixtures, an antistatic agent selected from the group consisting of micronised or non micronised talc, fumed silica, precipitated and colloidal silica, a sweetening agent or a coloring agent.  
     
     
         16 . Granules according to  claim 14 , which further comprise a disintegrating agent selected from the group consisting of croscarmellose, crospovidone and mixtures thereof or a surfactant which can be an anionic, nonionic, cationic or amphoteric surfactant.  
     
     
         17 . Granules according to  claim 15 , comprising: 
 from 10% to 95% of fexofenadine, or one of the pharmaceutically acceptable salts thereof,    at most 20% by weight of the binder, relative to the weight of fexofenadine, or one of the pharmaceutically acceptable salts thereof,    at most 5% of the antistatic agent, relative to the weight of said granules.    
     
     
         18 . Granules according to  claim 17 , comprising: 
 from 50% to 70% of fexofenadine, or one of the pharmaceutically acceptable salts thereof,    at most 10% by weight of the binder, relative to the weight of fexofenadine, or one of the pharmaceutically acceptable salts thereof,    at most 2% by weight of the antistatic agent, relative to the weight of said granules.    
     
     
         19 . Granules according to  claim 17 , further comprising a diluent agent for the balance to 100%.  
     
     
         20 . Granules according to  claim 18 , further comprising a diluent agent for the balance to 100%.  
     
     
         21 . Granules according to  claim 14 , wherein they are coated with a coating composition containing at least one coating polymer selected rom the group consisting of cellulosic polymers such as ethylcellulose, hydroxypropylcellulose and hydroxypropylmethylcellulose, acrylic polymers such as insoluble acrylate amoniomethacrylate copolymer, polyacrylate or methacrylic copolymers, and mixtures thereof.  
     
     
         22 . Granules according to  claim 21 , wherein the coating composition further contains permeabilizing agents, plasticizers, soluble agents, disintegrating agents or surfactants.  
     
     
         23 . Granules according to  claim 14  comprising: 
 from 10% to 95% of granules of fexofenadine, or one of its pharmaceutically acceptable salts.    from 5 to 90% of a coating polymer, the percentages being expressed by weight relative to the weight of the granules of the fexofenadine, or one of its pharmaceutically acceptable salts.    from 0 to 10% of a permeabilising agent, the percentages being expressed by weight relative to the weight of the coating polymer.    
     
     
         24 . Granules according to  claim 23  comprising: 
 from 40 to 75% of granules of fexofenadine, or one of its pharmaceutically acceptable salts,    from 10 to 70% of a coating polymer, the percentages being expressed by weight relative to the weight of the granules of the fexofenadine, or one of its pharmaceutically acceptable salts.    from 0 to 10% of colloidal silica as permeabilising agent, the percentages being expressed by weight relative to the weight of the coating polymer.    
     
     
         25 . Granules according to  claim 24 , comprising from 25 to 55% of a coating polymer.  
     
     
         26 . Granules according to  claim 23 , comprising fexofenadine hydrochloride.  
     
     
         27 . Coated granules of fexofenadine, or one of its pharmaceutically acceptable salts, according to  claim 14 , which are coated with a coating layer containing fexofenadine wherein the granules and the coating layer comprise each from 70% to 95% by weight of fexofenadine, or one of the pharmaceutically acceptable salts thereof, the balance to 100% being formed with at least one binder.  
     
     
         28 . Coated granules of fexofenadine, or one of its pharmaceutically acceptable salts, according to  claim 27 , which are coated with a coating layer containing fexofenadine wherein the granules and the coating layer comprise each from 80% to 95% by weight of fexofenadine, or one of the pharmaceutically acceptable salts thereof, the balance to 100% being formed with at least one binder.  
     
     
         29 . Process for the preparation of granules according to  claim 14  wherein it comprises the successive steps consisting in: 
 dry mixing the microcrystals of the fexofenadine or one of its pharmaceutically acceptable salts;    granulating the mixture obtained in the above step by spraying of a solution or suspension of at least one binder,    coating the thus obtained granules with a suspension of a coating composition,    drying the thus obtained coated granules.    
     
     
         30 . Process for the preparation of granules according to  claim 15 , wherein it comprises the successive steps consisting in: 
 dry mixing the microcrystals of the fexofenadine or one of its pharmaceutically acceptable salts with an antistatic agent or a diluent agent;    granulating the mixture obtained in the above step by spraying of a solution or suspension of at least one binder,    coating the thus obtained granules with a suspension of a coating composition,    drying the thus obtained coated granules.    
     
     
         31 . Process for the preparation of granules according to  claim 27  wherein it comprises the successive steps consisting in: 
 dry mixing the microcrystals of the fexofenadine or one of its pharmaceutically acceptable salts;    granulating the mixture obtained in the above step by spraying of a solution or suspension of at least one binder,    applying a layer over the thus obtained granules by spraying thereon a suspension, or a solution comprising fexofenadine, or one of its pharmaceutically acceptable salts with at lease one binder,    coating the thus obtained granules with a suspension of a coating composition,    drying the thus obtained coated granules.    
     
     
         32 . Process according to  claim 31  wherein it comprises the successive steps consisting in: 
 dry mixing the microcrystals of the fexofenadine or one of its pharmaceutically acceptable salts with an antistatic agent or a diluent agent;    granulating the mixture obtained in the above step by spraying of a solution or suspension of a least one binder,    applying a layer over the thus obtained granules by spraying thereon a suspension, or a solution comprising fexofenadine, or one of its pharmaceutically acceptable salts with at least one binder,    coating the thus obtained granules with suspension of a coating composition,    drying the thus obtained coated granules.    
     
     
         33 . Process for the preparation of tablets according to  claim 31 , comprising the successive steps consisting in: 
 preparing coated granules of fexofenadine, or one of its pharmaceutically acceptable salts,    dry mixing coated granules and a mixture of excipients consisting of at least one disintegrating agent and a soluble diluent agent,    compressing the mixture of coated granules and excipients into a tablet.    
     
     
         34 . Process for the preparation of tablets according to  claim 31 , wherein the mixture of excipients further comprises a lubricant, a permeabilising agent, a swelling agent, sweeteners, an antistatic agent, flavorings and colors.  
     
     
         35 - 36 . (canceled).