POLYMORPH OF 4-[2-[4-[1-(2-ETHOXYETHYL)-1H-BENZIMIDAZOLE-2-YL]-1-PIPERIDINYL]ETHYL]-alpha alpha-DIMETHYL-BENZENEACETIC ACID

Abstract

Crystalline form 1 4-[2-[4-[1 -(2-ethoxyethyl)-1H-benzimidazole-2-yl]-1-piperidinyl]-ethyl]-αα-dimethyl-benzeneacetic acid of formula (I) is described, procedures for its preparation, pharmaceutical formulae containing crystalline form 1 and the use of crystalline form 1 to treat allergic reactions and pathological processes mediated by histamine in mammals such as man.

1 . A liquid antihistaminic pharmaceutical composition comprising the crystalline form 1 of bilastine as the active ingredient together with at least one excipient, said crystalline form 1 of bilastine having, upon X-ray crystallography analysis, crystal parameters of substantially the following: 
       
         
           
                 
                 
                 
                 
               
                     
                     
                 
                     
                   Crystallographic system 
                   Monoclinic 
                     
                 
                     
                   Spatial group 
                   P2 (1)/c 
                 
                     
                   Crystal size 
                   0.56 × 0.45 × 0.24 mm 
                 
                     
                   Cell dimension 
                   a = 23.38 (5) A angstrom 
                   α = 90° 
                 
                     
                     
                   b = 8.829 (17) A 
                   β = 90° 
                 
                     
                     
                   c = 12.59 (2) A 
                   γ = 90° 
                 
                     
                   Volume 
                   2600 A 3   
                 
                     
                   Z, calculated density 
                   4, 1.184 mg/m 3 , 
                 
                     
                     
                 
             
                
               
               
                
                
                
                
                
                
                
                
                
               
            
           
         
       
       an infrared spectrum in potassium bromide with the following bands:
 Wavenumber (cm −1 ) 
 3057 
 2929 
 2883 
 2857 
 2797 
 1666 
 1481 
 1431 
 1346 
 1326 
 1288 
 1020 
 973 
 945 
 829 
 
       and an infrared spectrum in potassium bromide which is substantially identical to that shown in  FIG. 1 . 
     
     
         2 . A liquid antihistaminic pharmaceutical composition according to  claim 1 , wherein said composition is a suspension. 
     
     
         3 . A liquid antihistaminic pharmaceutical composition according to  claim 1 , wherein said composition is an emulsion. 
     
     
         4 . A liquid antihistaminic pharmaceutical composition according to  claim 1 , wherein said composition is a lotion. 
     
     
         5 . A liquid antihistaminic pharmaceutical composition according to  claim 1 , wherein said composition is a cream. 
     
     
         6 . A liquid antihistaminic pharmaceutical composition according to  claim 1 , wherein said composition is an ointment. 
     
     
         7 . A process for treating allergic diseases in a patient in need thereof, wherein the process comprises administering to said patient a liquid pharmaceutical composition according to  claim 1 . 
     
     
         8 . A process for treating allergic diseases in a patient in need thereof, wherein the process comprises administering to said patient an effective amount of crystalline form 1 of bilastine in a liquid pharmaceutical composition according to  claim 1 .