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Claims for Patent: 7,589,079

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Claims for Patent: 7,589,079

Title:Crystalline and amorphous forms of beta-L-2'-deoxythymidine
Abstract:Physical forms of beta-L-2'-deoxythymidine are disclosed that can be characterized by physical appearance, purity levels, Infra-Red and Raman spectroscopy, X-ray powder diffraction patterns, thermal properties, and methods of manufacture. These forms of beta-L-2'-deoxythymidine can be used in the manufacture of other forms of beta-L-2'-deoxythymidine, or in pharmaceutical compositions. Particularly preferred uses are in the treatment of hepatitis B.
Inventor(s): Jonaitis; David (Lafayette, IN), Storer; Richard (Kent, GB)
Assignee: Novartis AG (Basel, CH)
Application Number:11/807,232
Patent Claims: 1. A non-solvated crystalline form of beta-L-2'-deoxythymidine devoid of waters of association, having an endotherm of about 190.degree. C. and 0.1% or less of volatiles measured at 175.degree. C.

2. A non-solvated crystalline form of beta-L-2'-deoxythymidine having an endotherm of about 190.degree. C., and having less than 0.1 percent volatiles measured at 175.degree. C., in the absence of amorphous beta-L-2'-deoxythymidine.

3. The beta-L-2'-deoxythymidine of claim 1 prepared by crystallizing beta-L-2'-deoxythymidine from solution, optionally filtering said crystallized beta-L-2'-deoxythymidine, and drying said beta-L-2'-deoxythymidine in an environment comprising less than about 40% relative humidity.

4. A process of manufacturing pharmaceutical formulations of crystalline beta-L-2'-deoxythymidine having an endotherm of about 190.degree. C., and having less than 0.1 percent volatiles measured at 175.degree. C. comprising: (a) crystallizing two or more batches of beta-L-2'-deoxythymidine from solution; (b) measuring IR spectrometry of the batches; (c) selecting for further processing the batches that do not display significant breadth of peaks between 2200-2600, 1600-1800, 1000-1500, or 500-1000 cm.sup.-1 from a known IR spectra for crystalline beta-L-2'-deoxythymidine, said crystalline beta-L-2'-deoxythymidine having an endotherm of about 190.degree. C., and having less than 0.1 percent volatiles measured at 175.degree. C.; and (d) formulating said selected batches into pharmaceutical formulations of beta-L-2'-deoxythymidine.

5. A process of manufacturing pharmaceutical formulations of crystalline beta-L-2'-deoxythymidine having an endotherm of about 190.degree. C., and having less than 0.1 percent volatiles measured at 175.degree. C., comprising: (a) crystallizing two or more batches of beta-L-2'-deoxythymidine from the solution; (b) measuring Raman spectrometry of the batches; (c) selecting for further processing the batches that do not display significant breadth of peaks between 2800-3200, 1600-1675, 1300-1500, or 700-900 cm.sup.-1 from a known Raman spectra for crystalline beta-L-2'-deoxythymidine, said crystalline beta-L-2'-deoxythymidine having an endotherm of about 190.degree. C., and having less than 0.1 percent volatiles measured at 175.degree. C.; and (d) formulating said selected batches into pharmaceutical formulations of beta-L-2'-deoxythymidine.

6. A pharmaceutical formulation of crystalline beta-L-2'-deoxythymidine having an endotherm of about 190.degree. C., and having less than 0.1 percent volatiles measured at 175.degree. C., prepared by the process of claim 4 or 5.

7. A process of making a non-solvated crystalline form of beta-L-2'-deoxythymidine that is devoid of waters of association, said non-solvated crystalline from having an endotherm of about 190.degree. C., and having less than 0.1 percent volatiles measured at 175.degree. C., comprising: a) crystallizing beta-L-2'-deoxythymidine from solution; b) optionally filtering said crystallized beta-L-2-deoxythymidine; and c) drying said filtered beta-L-2-deoxythymidine in an environment comprising less than about 40% humidity.

8. A pharmaceutical formulation comprising the non-solvated crystalline form of beta-L-2'-deoxythymidine according to claim 1.

9. A pharmaceutical formulation comprising the non-solvated crystalline form of beta-L-2'-deoxythymidine according to claim 2.

10. The pharmaceutical formulation according to claim 8 or 9 in an oral solid form.

11. The oral solid formulation of claim 10 further comprising at least one of an inert diluent, an edible carrier, excipient, a compatible binding agent, glidant, lubricant or adjuvant material.

12. The oral solid formulation of claim 11 wherein the binding agent is microcrystalline cellulose, the excipient is starch, the glidant is colloidal silicon dioxide, and the lubricant is magnesium stearate.

13. The oral solid formulation of claim 11 in the form of a tablet, troche or capsule.

14. The oral solid formulation of claim 13 having a dosage unit of 50-1000 mg.

15. The oral solid formulation of claim 13 in the form of a tablet having a dosage unit of 50-1000 mg.

16. The tablet of claim 15 comprising a coating of sugar, shellac or other enteric agent.

17. A method of treating hepatitis B in a human subject comprising administering the oral solid formulation of claim 14.

18. A method of treating hepatitis B in a human subject comprising administering the oral solid formulation of claim 15.

19. A method of treating hepatitis B virus comprising administering to a human afflicted with Hepatitis B virus the oral solid formulation of claim 14.

20. A method of treating hepatitis B virus comprising administering to a human afflicted with Hepatitis B virus the oral solid formulation of claim 15.

21. A non-solvated crystalline form of beta-L-2'-deoxythymidine devoid of waters of association, having less than 0.1% weight loss at 5% relative humidity, 1.1% weight gain at 95% relative humidity and 1.1% weight loss from 95%-5% relative humidity.

22. A non-solvated crystalline form of beta-L-2'-deoxythymidine devoid of waters of association and having the X-ray powder diffraction pattern shown in FIG. 1.

23. The beta-L-2'-deoxythymidine of claim 21 or 22 prepared by crystallizing beta-L-2'-deoxythymidine from solution, optionally filtering said crystallized beta-L-2'-deoxythymidine, and drying said beta-L-2'-deoxythymidine in an environment comprising less than about 40% relative humidity.

24. A pharmaceutical formulation comprising the non-solvated crystalline form of beta-L-2'-deoxythymidine according to claim 21 or 22.

25. The pharmaceutical formulation according to claim 24 in an oral solid form.

26. The oral solid formulation of claim 25 further comprising at least one of an inert diluent, an edible carrier, excipient, a compatible binding agent, glidant, lubricant or adjuvant material.

27. The oral solid formulation of claim 26 wherein the binding agent is microcrystalline cellulose, the excipient is starch, the glidant is colloidal silicon dioxide, and the lubricant is magnesium stearate.

28. The oral solid formulation of claim 26 in the form of a tablet, troche or capsule.

29. The oral solid formulation of claim 28 having a dosage unit of 50-1000 mg.

30. The oral solid formulation of claim 28 in the form of a tablet having a dosage unit of 50-1000 mg.

31. The tablet of claim 30 comprising a coating of sugar, shellac or other enteric agent.

32. A method of treating hepatitis B in a human subject comprising administering the oral solid formulation of claim 29.

33. A method of treating hepatitis B in a human subject comprising administering the oral solid formulation of claim 30.

34. A method of treating hepatitis B virus comprising administering to a human afflicted with Hepatitis B virus the oral solid formulation of claim 29.

35. A method of treating hepatitis B virus comprising administering to a human afflicted with Hepatitis B virus the oral solid formulation of claim 30.
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