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Claims for Patent: 6,916,941

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Claims for Patent: 6,916,941

Title: Crystalline composition containing escitalopram
Abstract:Crystalline particles of escitalopram oxalate with a particle size of at least 40 .mu.m is disclosed. Method for the manufacture of said crystalline particles and pharmaceutical compositions comprising said crystalline particles are also disclosed.
Inventor(s): Christensen; Troels Volsgaard (Holb.ae butted.k, DK), Liljegren; Ken (V.ae butted.rl.o slashed.se, DK), Elema; Michiel Onne (K.o slashed.bnhavn .O slashed., DK), Andresen; Lene (R.o slashed.dovre, DK), Mahashabde; Shashank (Kendall Park, NJ), Assenza; Sebastian P. (Fort Salonga, NY)
Assignee: H. Lundbeck A/S (Valby-Copenhagen, DK)
Application Number:10/403,453
Patent Claims: 1. Crystalline particles of escitalopram oxalate having a median particle size of at least 40 .mu.m.

2. The crystalline particles of claim 1 wherein the median particle size is from 50-200 .mu.m.

3. A method for the manufacture of crystalline particles of escitalopram oxalate, which comprises (a) dissolving escitalopram oxalate in a solvent at a first temperature between about 50.degree. C. and the refluxing temperature of the solvent to form a solution of escitalopram oxalate; (b) gradually cooling the solution of escitalopram oxalate to a second temperature between about 0.degree. C. and 20.degree. C. while maintaining a controlled cooling rate; (c) adding crystals of escitalopram oxalate during the cooling of step (b); (d) holding the solution at the second temperature; and (e) isolating crystalline particles of escitalopram oxalate from the solution.

4. The method of claim 3 wherein the median particle size of the crystalline particles is at least 40 .mu.m.

5. The method of claim 3 wherein the median particle size of the crystalline particles is from 50-200 .mu.m.

6. The method of claim 3 wherein the solvent contains at least one alcohol and optionally water.

7. The method of claim 6 wherein the solvent system contains ethanol.

8. The method of claim 3 wherein the solute:solvent weight ratio is between about 0.05:1 and 0.6:1.

9. The method of claim 3 wherein the solute:solvent weight ratio is between about 0.1:1 and 0.5:1.

10. The method of claim 3 wherein the solute:solvent weight ratio is between about 0.2:1 and 0.4:1.

11. The method of claim 3 wherein the first temperature is between about 60.degree. C. and the refluxing temperature of the solvent.

12. The method of claim 3 wherein the first temperature is between about 70.degree. C. and the refluxing temperature of the solvent.

13. The method of claim 3 wherein the second temperature is between about 0.degree. C. and 1520 C.

14. The method of claim 3 wherein the second temperature is between about 7.degree. C. and 15.degree. C.

15. The method of claim 3 wherein the controlled cooling rate comprises an initial cooling period during which the cooling rate does not exceed 0.6.degree. C. per minute.

16. The method of claim 15 wherein the initial cooling period comprises the time between the start of the cooling period and the time at which the temperature is below 60.degree. C.

17. The method of claim 15 wherein the initial cooling period comprises the time between the start of the cooling period and the time at which the temperature is below 50.degree. C.

18. The method of claim 15 wherein the initial cooling period comprises the time between the start of the cooling period and the time at which the temperature is below 40.degree. C.

19. The method of claim 15 wherein the cooling rate of the solution comprises from 0.2 to 0.4.degree. C. per minute.

20. The method of claim 3 which comprises adding crystals of escitalopram oxalate at least two times during the cooling of step (b).

21. The method of claim 3 which comprises holding the solution at the second temperature for at least one hour.

22. The method of claim 3 which comprises holding the solution at the second temperature for 4 to 24 hours.

23. The method of claim 3, which comprises holding the solution at the second temperature for 6 to 12 hours.

24. The method of claim 3, wherein step (e) comprises isolating the crystalline particles of escitalopram oxalate by solid/liquid separation techniques.

25. The method of claim 24, wherein the solid/liquid separation techniques comprise filtration.

26. A solid unit dosage form comprising the crystalline particles of escitalopram oxalate of claim 1.

27. A solid unit dosage form comprising the crystalline particles of escitalopram oxalate of claim 2.

28. The solid unit dosage form of claim 26, which comprises a tablet prepared by direct compression of a mixture of escitalopram oxalate and pharmaceutically acceptable excipients.

29. The solid unit dosage form of claim 28, wherein the tablet is coated.

30. The solid unit dosage form of claim 26, which is prepared by filling a hard gelatin capsule with a mixture of escitalopram oxalate and pharmaceutically acceptable excipients.

31. The solid unit dosage form of claim 26, which does not contain a binder.

32. The solid unit dosage form of claim 26, which comprises 1-30% w/w active ingredient calculated as escitalopram base.

33. The solid unit dosage form of claim 26, which comprises 4-20% w/w active ingredient calculated as escitalopram base.

34. The solid unit dosage form of claim 26, which comprises 6-10% w/w active ingredient calculated as escitalopram base.

35. The solid unit dosage form of claim 26, which further comprises a filler selected from e group consisting of lactose, sugars, calcium phosphates, starch, modified starches, micro crystalline cellulose, calcium sulfate and calcium carbonate.

36. The solid unit dosage form of claim 35, wherein the filler comprises a sugar selected from the group consisting of sorbitol, mannitol, dextrose and sucrose.

37. The solid unit dosage form of claim 35, wherein the filler comprises a calcium phosphate selected from the group consisting of dibasic, tribasic, hydrous and anhydrous calcium phosphate.

38. The solid unit dosage form of claim 35, wherein the filler comprises microcrystalline cellulose.

39. The solid unit dosage form of claim 38, wherein the microcrystalline cellulose is selected from the group consisting of ProSolv SMCC90 and Avicel PH 200.

40. The solid unit dosage form of claim 26, further comprising a lubricant.

41. The solid unit dosage form of claim 40, wherein the lubricant comprises a member selected from the group consisting of metallic stearates, stearic acid, wax, hydrogenated vegetable oil, talc and colloidal silica.

42. The solid unit dosage form of claim 41, wherein the lubricant comprises a metallic stearate selected from the group consisting of magnesium, calcium and sodium stearate.

43. The solid unit dosage form of claim 41, wherein the lubricant comprises a member selected from the group consisting of talc, magnesium stearate and calcium stearate.

44. The solid unit dosage form of claim 41, wherein the lubricant comprises talc and magnesium stearate.

45. The solid unit dosage form of claim 44, wherein the magnesium stearate is present in a weight percent of 0.4% to 2%, calculated on the weight of the solid dosage form.

46. The solid unit dosage form of claim 44, wherein the magnesium stearate is present in a weight percent of 0.7% to 1.4%, calculated on the weight of the solid dosage form.

47. The solid unit dosage form of claim 26, which is substantially free of lactose.
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