Claims
- 1. A crystalline bicalutamide of form II.
- 2. The bicalutamide according to claim 1, having an IR absorbance peak at 847 cm−1+/−5 cm−1.
- 3. The bicalutamide according to claim 1, having an IR absorbance spectra substantially as shown in FIG. 4.
- 4. The bicalutamide according to claim 1, having an x-ray diffraction peak at an angle of about 25.9°.
- 5. The bicalutamide according to claim 4, having an x-ray diffraction peak at an angle of 25.85°+/−0.05°.
- 6. The bicalutamide according to claim 1, having x-ray diffraction peaks at angles of about 11.6°, 13.0°, 18.1°, 24.4°, 25.3-25.9°, 26.7°, 29.9° and 33.6°.
- 7. The bicalutamide according to claim 1, having x-ray diffraction peaks at angles of about 11.6°, 13.0°, 16.2°, 18.1°, 24.4°, 25.3-25.9°, 26.7°, 29.9° and 33.6°.
- 8. The bicalutamide according to claim 1, wherein said bicalutamide has an x-ray diffractogram substantially as shown in FIG. 2.
- 9. The bicalutamide according to claim 1, wherein said bicalutamide is racemic bicalutamide.
- 10. The bicalutamide according to claim 1, wherein said bicalutamide is at least 90% pure form II bicalutamide.
- 11. Crystalline bicalutamide having an x-ray diffraction peak at an angle of about 25.9°.
- 12. A bicalutamide in amorphous form.
- 13. A composition comprising crystalline bicalutamide of form II and at least one of crystalline bicalutamide of form I and amorphous bicalutamide.
- 14. A pharmaceutical composition comprising the bicalutamide of form II according to claim 1, and a pharmaceutically acceptable excipient.
- 15. The pharmaceutical composition according to claim 14, wherein said composition is a unit dose and said bicalutamide of form II is contained in an antiandrogenic effective amount.
- 16. The pharmaceutical composition according to claim 15, wherein said composition is substantially free of form I bicalutamide.
- 17. The pharmaceutical composition according to claim 14, wherein said pharmaceutically acceptable excipient is a carrier or diluent.
- 18. The pharmaceutical composition according to claim 17, wherein said excipient is selected from the group consisting of calcium phosphates, microcrystalline cellulose, hydroxypropyl methylcellulose, lactose, and starches.
- 19. The pharmaceutical composition according to claim 14, wherein said composition is a solid oral dosage form.
- 20. The pharmaceutical composition according to claim 14, wherein said composition is a solution or suspension.
- 21. The pharmaceutical composition according to claim 14, which further comprises bicalutamide form I.
- 22. The pharmaceutical composition according to claim 21, wherein the relative amount of bicalutamide form II is within the range of 0.1-99.9% based on the total weight of all forms of bicalutamide.
- 23. A method for producing an antiandrogenic effect, which comprises administering an antiandrogenic effective amount of the bicalutamide according to claim 1 to a mammal in need thereof.
- 24. A process, which comprises precipitating bicalutamide form II from a solution containing bicalutamide.
- 25. The process according to claim 24, wherein said precipitation is carried out in the presence of seed crystals of bicalutamide form II.
- 26. The process according to claim 24, wherein said precipitation is carried out by lowering the temperature of the bicalutamide solution and/or contacting said bicalutamide solution with a contrasolvent.
- 27. The process according to claim 24, wherein said precipitation occurs at a temperature of 35° C. or higher.
- 28. A process which comprises heating an amorphous bicalutamide to form one or more crystals of bicalutamide form II.
- 29. A process which comprises heating a solid form of bicalutamide to form a melt and cooling said melt to form amorphous bicalutamide.
Parent Case Info
[0001] This application claims the benefit of priority under 35 U.S.C. § 119(e) of U.S. Provisional Application No. 60/413,765, filed Sep. 27, 2002, and U.S. Provisional Application No. 60/470,223, filed May 14, 2003, the entire contents of each Application being incorporated herein by reference.
Provisional Applications (2)
|
Number |
Date |
Country |
|
60413765 |
Sep 2002 |
US |
|
60470223 |
May 2003 |
US |