Forms of rifaximin and uses thereof
View Patent ↗The present invention relates to new rifaximin forms kappa, theta, rifaximin:piperazine cocrystal 1 and rifaximin:piperazine cocrystal 2, methods of making same and to their use in medicinal preparations and therapeutic methods.
1. A rifaximin polymorph Form kappa, wherein the polymorph Form kappa exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ at
5.41-5.65, 6.45-6.67, 6.83-6.94, 7.03-7.06, and 7.52-7.56;
6.45-6.67, 6.83-6.94, 7.03-7.06, 7.68-7.78, and 18.46-18.61;
5.41-5.65, 6.45-6.67, 6.83-6.94, 7.03-7.06, 7.52-7.56, and 18.46-18.61; or
6.45-6.67, 6.45-6.67, 6.83-6.94, 7.03-7.06, 7.68-7.78, and 18.46-18.61.
2. The rifaximin polymorph Form kappa according to claim 1 , containing less than 5% by weight total impurities.
3. The rifaximin polymorph Form kappa according to claim 1 , wherein the compound 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.
4. A pharmaceutical composition comprising the rifaximin polymorph Form kappa according to claim 1 ; and a pharmaceutically acceptable carrier.
5. The composition according to claim 4 , wherein the rifaximin Form kappa is formulated as coated or uncoated tablets, hard or soft gelatin capsules, sugar-coated pills, lozenges, wafer sheets, pellets or powders in sealed packets.
6. A rifaximin:piperazine cocrystal 1, wherein the rifaximin:piperazine cocrystal 1 exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ at 6.58, 7.49, 18.15, and 20.21; or
5.74, 6.58, 7.49, 18.15, and 20.21.
7. The rifaximin:piperazine cocrystal 1 according to claim 6 , containing less than 5% by weight total impurities.
8. The rifaximin:piperazine cocrystal 1 according to claim 6 , wherein the compound 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.
9. A pharmaceutical composition comprising the rifaximin:piperazine cocrystal 1 according to claim 6 ; and a pharmaceutically acceptable carrier.
10. The composition according to claim 9 , wherein the rifaximin:piperazine cocrystal 1 is formulated as coated or uncoated tablets, hard or soft gelatin capsules, sugar-coated pills, lozenges, wafer sheets, pellets or powders in sealed packets.
11. A rifaximin:piperazine cocrystal 2, wherein the rifaximin:piperazine cocrystal 1 exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ at 5.58, 6.45, 7.19, and 7.29; or
5.58, 6.45, 7.19, 7.29, and 8.27.
12. The rifaximin:piperazine cocrystal 2 according to claim 11 , containing less than 5% by weight total impurities.
13. The rifaximin:piperazine cocrystal 2 according to claim 11 , wherein the compound 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.
14. A pharmaceutical composition comprising the rifaximin:piperazine cocrystal 2 according to claim 11 ; and a pharmaceutically acceptable carrier.
15. The composition according to claim 14 , wherein the rifaximin:piperazine cocrystal 2 is formulated as coated or uncoated tablets, hard or soft gelatin capsules, sugar-coated pills, lozenges, wafer sheets, pellets or powders in sealed packets.
16. A rifaximin polymorph Form kappa, wherein the polymorph Form kappa exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ at 6.83-6.94 (+/−0.20), 7.52-7.56 (+/−0.20), 7.68-7.78 (+/−0.20) and 8.30-8.34 (+/−0.20).
17. The rifaximin polymorph Form kappa according to claim 16 , containing less than 5% by weight total impurities.
18. The rifaximin polymorph Form kappa according to claim 16 , wherein the compound 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.
19. A pharmaceutical composition comprising the rifaximin polymorph Form kappa according to claim 16 ; and a pharmaceutically acceptable carrier.
20. The composition according to claim 19 , wherein the rifaximin Form kappa is formulated as coated or uncoated tablets, hard or soft gelatin capsules, sugar-coated pills, lozenges, wafer sheets, pellets or powders in sealed packets.