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Claims for Patent: 7,906,542

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Claims for Patent: 7,906,542

Title:Pharmaceutical compositions comprising polymorphic forms .alpha., .beta., and .gamma. of rifaximin
Abstract:Crystalline polymorphous forms of rifaximin (INN), referred to as rifaximin .alpha. and rifaximin .beta., and a poorly crystalline form referred to as rifaximin .gamma., useful in the production of medicaments containing rifaximin for oral and topical use and obtained by means of a crystallization process carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a fixed temperature and for a fixed period of time, followed by a drying under controlled conditions until reaching a precise water content in the end product, are the object of the invention.
Inventor(s): Viscomi; Giuseppe Claudio (Bologna, IT), Campana; Manuela (Bologna, IT), Braga; Dario (Bologna, IT), Confortini; Donatella (Bologna, IT), Cannata; Vincenzo (Bologna, IT), Righi; Paolo (Bologna, IT), Rosini; Goffredo (Bologna, IT)
Assignee: Alfa Wassermann, S.p.A. (Bologna, IT)
Application Number:12/119,622
Patent Claims: 1. A pharmaceutical composition comprising rifaximin in polymorphic Form .alpha. and a pharmaceutically acceptable excipient or carrier, wherein the rifaximin Form .alpha. has x-ray powder diffraction pattern peaks at about 7.4.degree.; 19.7.degree.; 21.0.degree. and 22.1.degree. 2-.theta., and wherein after administration to a patient, the observed plasma concentration of rifaxmin is no more than about 2.6 ng/ml.

2. The pharmaceutical composition of claim 1, wherein the polymorph Form .alpha. has a water content of about 2% to about 3%.

3. The pharmaceutical composition of claim 1, wherein the excipient is selected from the group consisting of a diluting agent, a binding agent, a lubricating agent, a disintegrating agent, a coloring agent, a flavoring agent, and a sweetening agent.

4. The pharmaceutical composition of claim 1, wherein the composition is formulated for selected coated and uncoated tablets, hard and soft gelatin capsules, sugar-coated pills, lozenges, wafer sheets, pellets and powders in a sealed packet.

5. The pharmaceutical composition of claim 1, wherein after administration to a patient, the t.sub.max of the Form .alpha. is about 9.5 hours.

6. The pharmaceutical composition of claim 1, wherein after administration to a patient, the AUC.sub.0-24 h of the Form .alpha. is about 13 ngh/ml.

7. The pharmaceutical composition of claim 2, wherein after administration to a patient, the t.sub.max of the Form .alpha. is about 9.5 hours.

8. The pharmaceutical composition of claim 2, wherein after administration to a patient, the AUC.sub.0-24 h of the Form .alpha. is about 13 ngh/ml.

9. A pharmaceutical composition comprising rifaximin in polymorphic Form .beta. and a pharmaceutically acceptable excipient or carrier, wherein the rifaximin Form .beta. has x-ray powder diffraction pattern peaks at about 5.4.degree.; 9.0.degree.; and 20.9.degree. 2-.theta., and wherein after administration to a patient, the observed plasma concentration of rifaximin is no more than about 1.1 ng/ml.

10. The pharmaceutical composition of claim 9, wherein the polymorph Form .beta. has a water content of from between greater than about 4.5%.

11. The pharmaceutical composition of claim 9, wherein the excipient is selected from the group consisting of a diluting agent, a binding agent, a lubricating agent, a disintegrating agent, a coloring agent, a flavoring agent, and a sweetening agent.

12. The pharmaceutical composition of claim 9, wherein the composition is formulated for selected coated and uncoated tablets, hard and soft gelatin capsules, sugar-coated pills, lozenges, wafer sheets, pellets and powders in a sealed packet.

13. The pharmaceutical composition of claim 9, wherein after administration to a patient, the t.sub.max of the Form .beta. is about 4 hours.

14. The pharmaceutical composition of claim 9, wherein after administration to a patient, the AUC.sub.0-24 h of the Form .beta. is about 11 ngh/ml.

15. The pharmaceutical composition of claim 10, wherein after administration to a patient, the t.sub.max of the Form .beta. is about 4 hours.

16. The pharmaceutical composition of claim 10, wherein after administration to a patient, the AUC.sub.0-24 h of the Form .beta. is about 11 ngh/ml.

17. The pharmaceutical composition of claim 10, wherein the intrinsic dissolution rate of the Form .beta. is about 0.014 mg/min/cm.sup.2.

18. A pharmaceutical composition comprising rifaximin in polymorphic Form .gamma. and a pharmaceutically acceptable excipient or carrier, wherein the rifaximin Form .gamma. has x-ray powder diffraction pattern peaks at about 5.0.degree., 7.1.degree., and 8.4.degree. 2-.theta., and wherein after administration to a patient, the observed plasma concentration of rifaximin is no more than about 668 ng/ml.

19. The pharmaceutical composition of claim 18, wherein the intrinsic dissolution rate of the Form .gamma. is about 0.14 mg/min/cm.sup.2.

20. The pharmaceutical composition of claim 18, wherein the polymorph Form .gamma. has a water content of from between about 1% to about 2%.

21. The pharmaceutical composition of claim 18, wherein the excipient is selected from the group consisting of a diluting agent, a binding agent, a lubricating agent, a disintegrating agent, a coloring agent, a flavoring agent, and a sweetening agent.

22. The pharmaceutical composition of claim 18, wherein the composition is formulated for selected coated and uncoated tablets, hard and soft gelatin capsules, sugar-coated pills, lozenges, wafer sheets, pellets and powders in a sealed packet.

23. The pharmaceutical composition of claim 18, wherein after administration to a patient, the t.sub.max of the Form .gamma. is about 2.3 hours.

24. The pharmaceutical composition of claim 20, wherein after administration to a patient, the t.sub.max of the Form .gamma. is about 2.3 hours.

25. The pharmaceutical composition of claim 18, wherein after administration to a patient, the AUC.sub.0-24 h of the Form .gamma. is about 4000 ngh/ml.
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