Claims
- 1. A crystalline solid famciclovir form I, characterized by a XRD pattern with peaks at 15.5 and 15.9±0.2 deg. 2θ.
- 2. The crystalline solid famciclovir of claim 1, further characterized by a XRD pattern with peaks at 8.2, 10.4, 14.5, 17.0, 17.7, 19.5, 20.6, 21.1, 22.3, 23.0, 23.9, 24.4, 25.6, 26.5, 28.6, 29.0 and 32.6±0.2 deg. 2θ.
- 3. The crystalline solid famciclovir of claim 2, further characterized by a XRD pattern as substantially depicted in FIG. 1.
- 4. The crystalline solid famciclovir of any of claims 1-3, wherein the crystalline solid famciclovir contains less than about 5% wt of other famciclovir crystalline forms.
- 5. The crystalline solid famciclovir of any of claims 1-3, wherein the crystalline solid famciclovir contains less than about 5% wt of form II.
- 6. The crystalline solid famciclovir of claim 4, wherein the crystalline solid famciclovir contains less than about 1% wt of other famciclovir crystalline forms.
- 7. The crystalline solid famciclovir of claim 6, wherein the crystalline solid famciclovir contains less than about 1% wt of form II.
- 8. A crystalline solid famciclovir form II, characterized by a XRD pattern with peaks at 16.2 and 16.4±0.2 deg. 2θ.
- 9. The crystalline solid famciclovir of claim 8, further characterized by a XRD pattern with peaks at 8.3, 14.6, 17.8, 19.7, 20.7, 21.2, 24.5 and 25.6±0.2 deg. 2θ.
- 10. The crystalline solid famciclovir of claim 9, further characterized by an XRD pattern as substantially depicted in FIG. 2.
- 11. A crystalline solid famciclovir form III, characterized by an XRD pattern with peaks at 6.6 and 13.0±0.2 deg. 2θ.
- 12. The crystalline solid famciclovir of claim 11, further characterized by an XRD pattern with peaks at 15.9, 16.7, 18.4, 19.6, 24.5, 25.0 and 26.2±0.2 deg. 2θ.
- 13. The crystalline solid famciclovir of claim 12, further characterized by an XRD pattern as substantially depicted in FIG. 3.
- 14. The crystalline solid famciclovir of claim 11, wherein the crystalline solid of famciclovir is a methanol solvate.
- 15. The crystalline solid famciclovir of claim 11, wherein the crystalline solid of famciclovir is an ethanol solvate.
- 16. Crystalline solid famciclovir methanol solvate.
- 17. Crystalline solid famciclovir ethanol solvate.
- 18. A process for preparing the crystalline solid famciclovir of claim 1, comprising the steps of:
a) triturating an anhydrous famciclovir form in an organic solvent selected from the group consisting of isopropyl alcohol, acetonitrile, and diethylether; and b) isolating the crystalline solid famciclovir of claim 1.
- 19. A crystalline solid famciclovir form I prepared by triturating an anhydrous famciclovir form in an organic solvent selected from the group consisting of isopropyl alcohol, acetonitrile, and diethylether.
- 20. A process for preparing the crystalline solid famciclovir of claim 1, comprising the steps of:
a) heating crystalline solid famciclovir of claim 11 to about 40° C. to about 90° C.; and b) isolating the crystalline solid famciclovir of claim 1.
- 21. The process of claim 20, wherein the heating of crystalline solid famciclovir of claim 11 is performed at a temperature of about 60° C. to about 70° C.
- 22. A process for preparing the crystalline solid famciclovir of claim 1, comprising the steps of:
a) heating famciclovir monohydrate to about 40° C. to about 80° C.; and b) isolating the crystalline solid famciclovir of claim 1.
- 23. The process of claim 22, wherein the famciclovir monohydrate includes the crystalline solid famciclovir of claim 1.
- 24. The process of claim 22, wherein the heating of famciclovir monohydrate is performed at a temperature of about 60° C. to about 70° C.
- 25. A process for preparing the crystalline solid famciclovir of claim 1, comprising the steps of:
a) heating the crystalline solid famciclovir of claim 8 to about 40° C. to about 90° C.; and b) isolating the crystalline solid famciclovir of claim 1.
- 26. The processes of any of claims 18, 20, 22 and 25, wherein the isolated crystalline solid famciclovir of claim 1 contains less than about 5% wt of other famciclovir crystalline forms.
- 27. The processes of any of claims 18, 20, 22, 25 and 26, wherein the isolated crystalline solid famciclovir of claim 1 contains less than about 5% wt of the form of claim 8.
- 28. The process of claim 26, wherein the isolated crystalline solid famciclovir of claim 1 contains less than about 1% wt of other famciclovir crystalline forms.
- 29. The process of claim 28, wherein the isolated crystalline solid famciclovir of claim 1 contains less than about 1% wt of the form of claim 8.
- 30. A process for preparing the crystalline solid famciclovir of claim 1, comprising the steps of:
a) providing a solution of famciclovir in an organic solvent selected from the group consisting of dichloromethane, chloroform, acetonitrile, ethylacetate, acetone, THF, diethyl ether/dichloromethane mixture, dichloromethane/toluene mixture, ethylacetate/toluene mixture, acetonitrile/toluene mixture, dimethylacetamide and isopropylalcohol; b) cooling the solution; and c) isolating the crystalline solid famciclovir of claim 1.
- 31. A process for preparing the crystalline solid famciclovir of claim 8, comprising the steps of:
a) providing a solution of famciclovir in an organic solvent selected from the group consisting of ethanol and n-buthanol, b) cooling the solution whereby the crystalline solid famciclovir form II crystallizes, and c) isolating the crystalline solid famciclovir of claim 8.
- 32. A process for preparing a mixture of crystalline solid famciclovir of claim 8 and crystalline solid famciclovir of claim 1 comprising the steps of:
a) providing a solution of famciclovir in an organic solvent selected from the group consisting of chloroform, ethylacetate, diethyl ether/dichloromethane mixture, tetrahydrofuran, acetonitrile/toluene mixture, dimethylacetamide and isopropanol, b) cooling the solution, and c) isolating the mixture of the crystalline solid famciclovir of claim 8 and the crystalline solid famciclovir of claim 1.
- 33. A process for preparing the crystalline solid famciclovir of claim 11, comprising the steps of:
a) triturating an anhydrous famciclovir in methanol; and b) isolating the crystalline solid famciclovir of claim 11.
- 34. A process of preparing a mixture of the crystalline solid famciclovir of claim 11 and the crystalline solid famciclovir of claim 1, comprising the steps of:
a) triturating an anhydrous famciclovir in ethanol; and b) isolating the mixture of the crystalline solid famciclovir of claim 11 and the crystalline solid famciclovir of claim 1.
- 35. A process of preparing a crystalline solid famciclovir monhydrate, comprising the steps of:
a) providing a solution of famciclovir in an organic solvent selected from the group consisting of acetonitrile, ethyl acetate, acetone, isopropyl alcohol, tetrahydrofuran, ethanol/water mixture, acetone/water mixture, DMF/water mixture, DMA/water mixture, acetonitrile/water mixture, methanol/water mixture, tetrahydrofuran/water mixture, and isopropyl alcohol/water mixture; and b) cooling the solution; and c) isolating the crystalline solid famciclovir monohydrate.
- 36. A process for preparing a mixture of the crystalline solid famciclovir of claim 11 and crystalline solid famciclovir monohydrate, comprising the steps of:
a) triturating anhydrous famciclovir in an organic solvent selected from the group consisting of isopropyl alcohol and ethanol; and b) isolating the mixture of the crystalline solid famciclovir of claim 11 and crystalline solid famciclovir monohydrate.
- 37. A pharmaceutical composition comprising the crystalline solid famciclovir of claim 1 and a pharmaceutically-acceptable excipient, wherein the crystalline solid famciclovir of claim 1 contains less than about 5% wt of other famciclovir crystalline forms.
- 38. The pharmaceutical composition of claim 37, wherein the crystalline solid famciclovir of claim 1 contains less than about 1% wt of other famciclovir crystalline forms.
- 39. A pharmaceutical composition comprising the crystalline solid famciclovir of claim 8 and a pharmaceutically-acceptable excipient, wherein the crystalline solid famciclovir form II contains less than about 5% wt of other famciclovir crystalline forms.
- 40. The pharmaceutical composition of claim 39, wherein the crystalline solid famciclovir of claim 8 contains less than about 1% wt of other famciclovir crystalline forms.
- 41. A pharmaceutical composition comprising the crystalline solid famciclovir of claim 11 and a pharmaceutically-acceptable excipient, wherein the crystalline solid famciclovir form III contains less than about 5% wt of other famciclovir crystalline forms.
- 42. The pharmaceutical composition of claim 41, wherein the crystalline solid famciclovir of claim 11 contains less than about 1% wt of other famciclovir crystalline forms.
- 43. A method of treating a human in need of treatment with famciclovir comprising administering to the human the pharmaceutical composition of any of claims 37-42.
CROSS-REFERENCE TO RELATED APPLICATION
[0001] This application claims the benefit under 35 U.S.C. § 1.119(e) of Provisional Application Serial Nos. 60/406,173 filed Aug. 26, 2002 and 60/422,243 filed Oct. 29, 2002, the disclosure of which is incorporated by reference in its entirety herein.
Provisional Applications (2)
|
Number |
Date |
Country |
|
60406173 |
Aug 2002 |
US |
|
60422243 |
Oct 2002 |
US |