Pharmaceutical compositions containing epinastine and pseudoephedrine

Abstract

The present invention relates to novel oral pharmaceutical compositions comprising as pharmaceutically active compounds a combination of an antihistaminic-effective amount of epinastine or a pharmaceutically acceptable salt thereof and of a decongestant-effective amount of pseudoephedrine or a pharmaceutically acceptable salt thereof and further comprising suitable pharmaceutically acceptable carriers or excipients. The invention further relates to methods for the preparation these compositions and methods of using them in the treatment of allergic diseases and/or disorders.

1 ) An oral pharmaceutical composition comprising a combination of an antihistaminic-effective amount of epinastine or a pharmaceutically acceptable salt thereof and a decongestant-effective amount of pseudoephedrine or a pharmaceutically acceptable salt thereof and further comprising pharmaceutically acceptable carriers or excipients, with the proviso that the composition does not contain a leukotriene antagonist.  
     
     
         2 ) An oral pharmaceutical composition according to  claim 1 , which contains as active ingredients only the antihistaminic-effective amount of epinastine or a pharmaceutically acceptable salt thereof and the decongestant-effective amount of pseudoephedrine or a pharmaceutically acceptable salt thereof.  
     
     
         3 ) An oral pharmaceutical composition according to  claim 1 , which provides for a sustained release of the decongestant effective amount of pseudoephedrine and an immediate release of the antihistaminic effective amount of epinastine.  
     
     
         4 ) An oral pharmaceutical composition according to  claim 2 , which provides for a sustained release of the decongestant effective amount of pseudoephedrine and an immediate release of the antihistaminic effective amount of epinastine.  
     
     
         5 ) An oral pharmaceutical composition according to  claim 1 ,  2 ,  3  or  4 , in the form of a bilayer tablet.  
     
     
         6 ) A bilayer tablet according to  claim 5 , wherein a first layer A, providing for the sustained release of pseudoephedrine, comprises a decongestant-effective amount of pseudoephedrine or a pharmaceutically acceptable salt thereof and wherein a second layer B, providing for the immediate release of epinastine, comprises an antihistaminic-effective amount of epinastine or a pharmaceutically acceptable salt thereof.  
     
     
         7 ) A bilayer tablet according to  claim 6 , which additionally contains a tablet coating C consisting of pharmaceutically acceptable excipients.  
     
     
         8 ) A bilayer tablet according to  claim 6 , wherein layer A comprises a decongestant-effective amount of pseudoephedrine, or a pharmaceutically acceptable salt thereof, in a matrix of a swellable hydrophilic polymer.  
     
     
         9 ) A bilayer tablet according to  claim 7 , wherein layer A comprises a decongestant-effective amount of pseudoephedrine, or a pharmaceutically acceptable salt thereof, in a matrix of a swellable hydrophilic polymer.  
     
     
         10 ) A bilayer tablet according to  claim 5 , wherein the concentration range of the pharmaceutically acceptable salt of pseudoephedrine is 5 to 240 mg/tablet and the concentration range of the pharmaceutically acceptable salt of epinastine salt is 2 to 20 mg/tablet.  
     
     
         11 ) A bilayer tablet according to  claim 6 , wherein the concentration range of the pharmaceutically acceptable salt of pseudoephedrine is 5 to 240 mg/tablet and the concentration range of the pharmaceutically acceptable salt of epinastine salt is 2 to 20 mg/tablet.  
     
     
         12 ) A bilayer tablet according to  claim 11 , wherein layer A comprises 120 mg pseudoephedrine sulfate and layer B comprises 10 mg epinastine-HCl.  
     
     
         13 ) A method of treating allergic rhinitis, allergic congestion of the Eustachian tubes and/or other diseases of allergic origin treatable by the administration of antihistamine and decongestant agents, comprising administering to a host in need of such treatment an oral pharmaceutical composition according to  claim 1 ,  2 ,  3  or  4 .  
     
     
         14 ) A method according to  claim 13 , wherein the condition treated is allergic rhinitis.  
     
     
         15 ) A method of treating the common cold and/or symptoms associated with the common cold, comprising administering to a host in need of such treatment an oral pharmaceutical composition according to  claim 1 ,  2 ,  3  or  4 .