Forms of rifaximin and uses thereof

Abstract

The present invention relates to Rifaximin polymorphic, salt, hydrate, and amorphous forms, to their use in medicinal preparations and to therapeutic methods using them.

1 . Polymorphic Form ζ, Form η, or Form ι, of rifaximin. 
     
     
         2 . The polymorph Form ζ of  claim 1 , wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ (+/−0.20 degree θ) at 4.7 (doublet), 7.6 (doublet), and 9.5 degrees 2-θ. 
     
     
         3 .- 9 . (canceled) 
     
     
         10 . The polymorph Form ζ of  claim 1 , wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ (+/−0.20 degree θ) at 4.7 (doublet), 6.3, 6.4, 7.3, 7.6 (doublet), 8.2, 8.6, 9.5, 10.2 (triplet), 10.5, 11.2 (doublet), 11.9 (doublet), 12.2 (weak), 12.6 (quintet), 12.9 (doublet), 13.2 (doublet) degrees 2-θ. 
     
     
         11 . The polymorph Form η of  claim 1 , wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ (+/−0.20 degree θ) at 6.1, 7.3, and 7.5 degrees 2-θ. 
     
     
         12 .- 25 . (canceled) 
     
     
         26 . The polymorph Form η of  claim 1 , wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ (+/−0.20 degree θ) at 5.3, 6.1, 7.3, 7.5, 7.9, 8.8, and 12.7 degrees 2-θ. 
     
     
         27 . The polymorph Form ι of  claim 1 , wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ (+/−0.20 degree θ) at 5.9±0.1; 7.9±0.1; 9.0±0.1; or 12.7±0.1; 13.9±0.1; 14.9±0.1; or 5.9±0.1; 7.9±0.1; 12.7±0.1; or 5.9±0.1; 9.0±0.1; 12.7±0.1; or 5.9±0.1; 13.9±0.1; 14.9±0.1; or 5.9±0.1; 7.9±0.1; 14.9±0.1; or 9.0±0.1; 12.7±0.1; 14.9±0.1; or 5.9±0.1; 7.9±0.1; 9.0±0.1; 14.9±0.1; or 5.9±0.1; 7.9±0.1; 9.0±0.1; 12.7±0.1; or 5.9±0.1; 7.9±0.1; 9.0±0.1; 12.7±0.1; 13.9±0.1; 14.9±0.1. 
     
     
         28 .- 45 . (canceled) 
     
     
         46 . The polymorph Form ι of  claim 1 , wherein the polymorph Form ι exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ (+/−0.20 degree θ) at 5.9±0.1; 7.9±0.1; 9.0±0.1; 12.7±0.1. 
     
     
         47 .- 74 . (canceled) 
     
     
         75 . The Form ζ, Form η, or Form ι of rifaximin of  claim 1 , wherein the polymorph contains less than 5% by weight total impurities. 
     
     
         76 . The Form ζ, Form η, or Form ι, of rifaximin of  claim 1 , wherein the form is at least 50% pure, or at least 75% pure, or at least 80% pure, or at least 90% pure, or at least 95% pure, or at least 98% pure. 
     
     
         77 . A pharmaceutical composition comprising one or more of a Form ζ, Form η, or Form ι, of rifaximin and a pharmaceutically acceptable carrier. 
     
     
         78 .- 113 . (canceled) 
     
     
         114 . The Form ζ of rifaximin of  claim 1 , characterized by an XRPD pattern substantially similar to  FIG. 2  or  FIG. 8 . 
     
     
         115 . The Form η of rifaximin of  claim 1 , characterized by an XRPD pattern substantially similar to  FIG. 3  or  FIG. 9 . 
     
     
         116 - 120 . (canceled) 
     
     
         121 . The Form ι of rifaximin of  claim 1 , characterized by one or more of an XRPD pattern substantially similar to  FIG. 11 ; comprising thermal data substantially similar to  FIG. 31 ; or proton NMR spectrum substantially similar to  FIG. 34 . 
     
     
         122 .- 139 . (canceled)