Claims
- 1. A substantially crystalline clindamycin free base.
- 2. The substantially crystalline clindamycin free base of claim 1, characterized by bright birefringence using polarized microscopic inspection or by sharp peaks using powder x-ray diffraction.
- 3. The substantially crystalline clindamycin free base of claim 1 which is substantially all Form I.
- 4. The substantially crystalline clindamycin free base of claim 3 which is characterized by an X-ray powder diffraction pattern substantially as shown in FIG. 1.
- 5. The substantially crystalline clindamycin of claim 3 which is characterized by a differential scanning calorimetry exhibiting an endotherm having an extrapolated onset temperature of about 67° C., a peak temperature of about 69° C. and an associated heat of about 51 J/g.
- 6. The substantially crystalline clindamycin free base of claim 1 which is substantially all Form II.
- 7. The substantially crystalline clindamycin free base of claim 6 which is characterized by an X-ray powder diffraction pattern substantially as shown in FIG. 5.
- 8. The substantially crystalline clindamycin free base of claim 6 which is characterized by a differential scanning calorimetry exhibiting an endotherm having an extrapolated onset temperature of about 62.7° C., a peak temperature of about 75.1° C. and an associated heat of about 65.0 J/g.
- 9. The substantially crystalline clindamycin free base of claim 1 which is substantially all Form III.
- 10. The substantially crystalline clindamycin free base of claim 9 which is characterized by an X-ray powder diffraction pattern substantially as shown in FIG. 9.
- 11. The substantially crystalline clindamycin free base of claim 9 which is characterized by a differential scanning calorimetry exhibiting an endotherm having an extrapolated onset temperature of about 64.4° C., a peak temperature of about 69.4° C. and an associated heat of about 69.4 J/g.
- 12. A clindamycin free base drug substance, comprising about 10% (w/w) to about 100% (w/w) crystalline clindamycin free base.
- 14. The drug substance of claim 13, comprising about 60% (w/w) to about 100% (w/w) crystalline clindamycin free base.
- 15. The drug substance of claim 14, wherein the crystalline free base is substantially all Form I.
- 16. The drug substance of claim 15, wherein the crystalline free base is characterized by an X-ray powder diffraction pattern substantially as shown in FIG. 1.
- 17. The drug substance of claim 15, wherein the crystalline free base is characterized by a differential scanning calorimetry exhibiting an endotherm having an extrapolated onset temperature of about 66.9° C., a peak temperature of about 69.1° C. and an associated heat of about 50.7 J/g.
- 18. The drug substance of claim 13 wherein the crystalline free base is substantially all Form II.
- 19. The drug substance of claim 18, wherein the crystalline free base is characterized by an X-ray powder diffraction pattern substantially as shown in FIG. 5.
- 20. The drug substance of claim 19, wherein the crystalline free base is characterized by a differential scanning calorimetry exhibiting an endotherm having an extrapolated onset temperature of about 62.7° C., a peak temperature of about 75.1° C. and an associated heat of about 65.0 J/g.
- 21. The drug substance of claim 13, wherein at least about 10% (w/w) of the crystalline clindamycin free base is Form III.
- 22. The drug substance of claim 21, wherein the clindamycin crystalline free base is characterized by an X-ray powder diffraction pattern having peaks at substantially the same two-theta angles as shown in FIG. 9.
- 23. The drug substance of claim 21, wherein the clindamycin crystalline free base is characterized by a differential scanning calorimetry exhibiting an endotherm having an extrapolated onset temperature of about 64.4° C., a peak temperature of about 69.4° C. and an associated heat of about 69.4 J/g.
- 24. A pharmaceutical composition comprising at least about 1% (w/w) crystalline clindamycin free base in a pharmaceutically acceptable formulation.
- 25. The pharmaceutical composition of claim 24 wherein the crystalline clindamycin free base is substantially all Form I.
- 26. The pharmaceutical composition of claim 25 wherein the crystalline clindamycin free base is characterized by an X-ray powder diffraction pattern substantially as shown in FIG. 1.
- 27. The pharmaceutical composition of claim 26 which is characterized by a differential scanning calorimetry exhibiting an endotherm having an extrapolated onset temperature of about 66.9° C., a peak temperature of about 69.1° C. and an associated heat of about 50.7 J/g.
- 28. The pharmaceutical composition of claim 24 wherein the crystalline clindamycin free base is substantially all Form II.
- 29. The pharmaceutical composition of claim 29 which is characterized by an X-ray powder diffraction pattern substantially as shown in FIG. 5.
- 30. The pharmaceutical composition of claim 28 which is characterized by a differential scanning calorimetry exhibiting an endotherm having an extrapolated onset temperature of about 62.7° C., a peak temperature of about 75.1° C. and an associated heat of about 65.0 J/g.
- 31. The pharmaceutical composition of claim 24 wherein at least about 10% (w/w) of the crystalline clindamycin free base is Form III.
- 32. The pharmaceutical composition of claim 31 which is characterized by an X-ray powder diffraction pattern substantially shown in FIG. 9.
- 33. The pharmaceutical composition of claim 31 which is characterized by a differential scanning calorimetry exhibiting an endotherm having an extrapolated onset temperature of about 64.4° C., a peak temperature of about 69.4° C. and an associated heat of about 69.4 J/g.
- 34. The pharmaceutical composition of claim 24, in an extended release dosage form.
- 35. A method of using the pharmaceutical composition of claim 24 to treat a bacterial infection in a subject, comprising administering to the subject a therapeutically effective amount of the pharmaceutical composition.
Parent Case Info
[0001] This application claims the benefit of U.S. provisional application serial No. 60/315,375, filed Aug. 28, 2001, and U.S. provisional application serial No. 60/377,892, filed May 1, 2002.
Provisional Applications (2)
|
Number |
Date |
Country |
|
60315375 |
Aug 2001 |
US |
|
60377892 |
May 2002 |
US |