Crystalline forms of bosentan salts and processes for their preparation

Abstract

The present invention relates to crystalline forms of bosentan salts and processes for their preparation.

We claim: 
     
         1 . Crystalline Form C of bosentan sodium having an XRPD pattern comprising interplanar spacing (d) values substantially at 2.64, 2.82, 2.88, 2.97, 3.02, 3.16, 3.22, 3.36, 3.43, 3.48, 3.68, 3.79, 3.84, 3.90, 3.95, 4.01, 4.10, 4.11, 4.22, 4.34, 4.48, 4.58, 4.66, 4.74, 4.80, 4.87, 4.97, 5.24, 5.68, 5.79, 6.29, 6.72, 6.85, 7.36, 8.90, 9.73, 10.47, 10.86, 13.70, and 14.29 (Å). 
     
     
         2 . Crystalline Form C of bosentan sodium according to  claim 1 , wherein the crystalline Form C of bosentan sodium is made by a process comprising:
 a) treating bosentan sodium with an organic solvent or treating bosentan with a sodium ion source in the presence of an organic solvent or a mixture of organic solvents; and   b) isolating crystalline Form C of bosentan sodium from the mixture thereof.   
     
     
         3 . Crystalline Form C of bosentan sodium according to  claim 2 , having a purity of about 98% or above. 
     
     
         4 . Crystalline Form C of bosentan sodium according to  claim 2 , having a purity of about 99% or above. 
     
     
         5 . Crystalline Form C of bosentan sodium according to  claim 2 , comprising
 a) treating bosentan sodium with an organic solvent; and   b) isolating crystalline Form C of bosentan sodium from the mixture thereof.   
     
     
         6 . Crystalline Form C of bosentan sodium according to  claim 2 , comprising
 a) treating bosentan with a sodium ion source in the presence of an organic solvent or a mixture of organic solvents; and   b) isolating crystalline Form C of bosentan sodium from the mixture thereof.   
     
     
         7 . A pharmaceutical composition comprising crystalline Form C of bosentan sodium according to  claim 1  and one or more carriers. 
     
     
         8 . Crystalline Form C of bosentan sodium having an XRPD pattern substantially as depicted in  FIG. 7  or a DSC pattern substantially as depicted in  FIG. 9 .