Forms of rifaximin and uses thereof
View Patent ↗The present invention relates to Rifaximin polymorphic forms, to their use in medicinal preparations and to therapeutic methods using them.
1. A polymorphic Form ζ of rifaximin, wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ (+/−0.20 degree θ) comprising 4.69, 7.63, 12.52, 13.87.
2. The polymorph Form ζ of rifaximin of claim 1 , comprising an XRPD pattern as substantially depicted in FIG. 4 or FIG. 15 wherein peaks in the XRPD patterns have a variation of +/−0.2 theta.
3. A polymorphic Form η of rifaximin, wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ (+/−0.20 degree θ) comprising
6.1, 7.3, and 7.5 degrees 2-θ; or
6.1, 7.3, and 7.9 degrees 2-θ; or
5.3, 6.1, 7.3, 7.5, 8.8, and 12.7 degrees 2-θ.
4. A polymorphic Form ι of rifaximin, wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ (+/−0.20 degree θ) comprising
5.49, 5.88, 7.86, 9.03, 12.66, and 13.89; or
5.5, 5.9, 7.9, and 9.0; or
12.7, 13.9, and 14.9; or
5.5, 5.9, 7.9, and 12.7; or
5.5, 5.9, 9.0, and 12.7; or
5.9, 13.9, and 14.9; or
5.5, 5.9, 7.9, and 14.9; or
5.5, 9.0, 12.7, and 14.9; or
5.5, 5.9, 7.9, 9.0, and 14.9; or
5.5, 5.9, 7.9, 9.0, and 12.7; or
5.9, 7.9, 9.0, 12.7, 13.9, and 14.9.
5. The polymorph Form ι of rifaximin of claim 4 , comprising an XRPD pattern as substantially depicted in FIG. 3 or FIG. 9 wherein peaks in the XRPD patterns have a variation of +/−0.2 theta.
6. The polymorph Form ι of rifaximin of claim 4 , comprising thermal data as substantially depicted in FIG. 10 or proton NMR spectrum as substantially depicted in FIG. 12 or vapor data as substantially depicted in FIG. 11 or FT-IR spectrum as substantially depicted in FIG. 13 .
7. A polymorphic Form ι-dry of rifaximin, wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ(+/−0.10 degree θ) comprising 6.04, 7.90, 8.92, 9.49, 12.76, and 14.14.
8. The polymorph Form ι-dry of rifaximin of claim 7 , comprising an XRPD pattern as substantially depicted in FIG. 1 or FIG. 6 or thermal data as substantially depicted in FIG. 7 .
9. A polymorphic Form ι-dry' of rifaximin, wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ(+/−0.15 degree θ) comprising 6.16, 7.92, 8.89, 9.55, 12.80, and 14.25.
10. The polymorph Form ι-dry' of rifaximin of claim 9 , comprising an XRPD pattern as substantially depicted in FIG. 2 or FIG. 8 wherein peaks in the XRPD patterns have a variation of +/−0.15 theta.
11. The polymorph Form ι of claim 1 , wherein the polymorph comprises from between about 50 to about 100% pure polymorphous form before or after formulation, or from between about 75 to about 100% pure polymorphous form before or after formulation.
12. A pharmaceutical dosage form comprising the polymorphic Form ι of claim 1 .
13. The polymorph Form η of claim 3 , wherein the polymorph comprises from between about 50 to about 100% pure polymorphous form before or after formulation, or from between about 75 to about 100% pure polymorphous form before or after formulation.
14. A pharmaceutical dosage form comprising the polymorphic Form η of claim 3 .
15. The polymorph Form ι of claim 4 , wherein the polymorph comprises from between about 50 to about 100% pure polymorphous form before or after formulation, or from between about 75 to about 100% pure polymorphous form before or after formulation.
16. A pharmaceutical dosage form comprising the polymorphic Form ι of claim 4 .
17. The polymorph Form ι-dry of claim 7 , wherein the polymorph comprises from between about 50 to about 100% pure polymorphous form before or after formulation, or from between about 75 to about 100% pure polymorphous form before or after formulation.
18. A pharmaceutical dosage form comprising the polymorphic Form ι-dry of claim 7 .
19. The polymorph Form ι-dry' of claim 9 , wherein the polymorph comprises from between about 50 to about 100% pure polymorphous form before or after formulation, or from between about 75 to about 100% pure polymorphous form before or after formulation.
20. A pharmaceutical dosage form comprising the polymorphic Form ι-dry' of claim 9 .