Claims
- 1. A solid paroxetine composition comprising a paroxetine salt and an excipient wherein said composition has a pH of 6.5 or less.
- 2. The composition according to claim 1, wherein said pH is within the range of about 4.5 to 6.5.
- 3. The composition according to claim 1, wherein said paroxetine salt is a paroxetine sulfonate salt or a paroxetine hydrochloride salt.
- 4. The composition according to claim 3, wherein said pH is less than 6.0.
- 5. The composition according to claim 3, wherein said pH is within the range of about 4.5 to 6.5.
- 6. The composition according to claim 5, wherein said paroxetine salt is paroxetine methane sulfonate or paroxetine hydrochloride.
- 7. The composition according to claim 6, wherein said paroxetine salt is paroxetine methane sulfonate.
- 8. The composition according to claim 1, wherein the excipient is acidic calcium phosphate.
- 9. The composition according to claim 1, wherein said composition is a tablet and said paroxetine salt is contained in a pharmaceutically effective amount and is selected from paroxetine sulfonate salts and paroxetine hydrochloride salts.
- 10. The composition according to claim 9, wherein said excipient is selected from the group consisting of a diluent, a binder, a disintegrant, a lubricant, a colorant, or a combination of two or more thereof.
- 11. The composition according to claim 10, which does not contain a hydrosoluble or hydrophilic diluent.
- 12. The composition according to claim 11, which does not contain a taste masking coating.
- 13. The composition according to claim 11, which comprises calcium phosphate, a lubricant and a disintegrant.
- 14. The composition according to claim 13, wherein said paroxetine salt is paroxetine methane sulfonate salt.
- 15. A paroxetine solid dosage form comprising a paroxetine sulfonate salt and having been made with the aid of water.
- 16. The dosage form according to claim 15, wherein said dosage form is a tablet or a capsule.
- 17. The dosage form according to claim 16, wherein said paroxetine sulfonate salt is paroxetine methane sulfonate.
- 18. The dosage form according to claim 15, wherein said paroxetine sulfonate salt was combined as an aqueous solution with at least one excipient in preparing said dosage form.
- 19. The dosage form according to claim 18, wherein said dosage form has a pH of 6.5 or less.
- 20. A granulate formed by mixing water, paroxetine sulfonate, and at least one excipient and drying the resulting mixture.
- 21. The granulate according to claim 20, wherein said mixing was accomplished by adding together an aqueous solution of said paroxetine sulfonate salt with said at least one excipient.
- 22. The granulate according to claim 21, wherein said aqueous solution of paroxetine sulfonate salt is a concentrated solution having at least about a 10 wt % concentration of paroxetine sulfonate.
- 23. The granulate according to claim 22, wherein said aqueous solution has a paroxetine sulfonate salt concentration of at least about 30 wt %.
- 24. The granulate according to claim 20, wherein said mixing and said drying are carried out simultaneously.
- 25. The granulate according to claim 21, wherein said aqueous solution of paroxetine sulfonate was added to a powdered or granulated blend of said at least one excipient.
- 26. The granulate according to claim 20, wherein said granulate has an average remaining added water content of about 2.0 wt % or less.
- 27. The granulate according to claim 26, wherein said granulate has an average remaining added water content of about 1.0 wt % or less.
- 28. The granulate according to claim 27, wherein said granulate has an average remaining added water content of about 0.8 wt % or less.
- 29. The granulate according to claim 20, wherein said granulate composition exhibits a pH value of 6.5 or less.
- 30. The granulate according to claim 29, wherein said granulate has a pH of about 6.0 or less.
- 31. The granulate according to claim 29, wherein said granulate has a pH within the range of 4.5 to 6.5.
- 32. The granulate according to claim 20, wherein said paroxetine sulfonate salt is paroxetine methane sulfonate.
- 33. A process, which comprises:
mixing an aqueous solution containing at least 10 wt % of a paroxetine sulfonate with at least one solid excipient; and drying to form a granulate.
- 34. The process according to claim 33, wherein said drying step produces a granulate having a remaining added water content of about 2.0 wt % or less.
- 35. The process according to claim 34, wherein said drying step produces a granulate having a remaining added water content of about 1.3 wt % or less.
- 36. The process according to claim 35, wherein said drying step produces a granulate having a remaining added water content of about 1.0 wt % or less.
- 37. The process according to claim 36, wherein said drying step produces a granulate having a remaining added water content of about 0.8 wt % or less.
- 38. The process according to claim 33, wherein said aqueous solution concentration of said paroxetine sulfonate is at least 30 wt %.
- 39. The process according to claim 38, wherein said aqueous solution concentration of said paroxetine sulfonate is at least 40 wt %.
- 40. The process according to claim 33, wherein said mixing and drying steps are performed concurrently.
- 41. The process according to claim 33, wherein said solid excipient is a granulate.
- 42. The process according to claim 33, which further comprises optionally mixing additional excipients with said granulate and pressing said granulate composition into a tablet.
- 43. The process according to claim 42, which further comprises film coating said tablet.
- 44. The process according to claim 33, which further comprises filling said granulate into a capsule or sachet.
- 45. The process according to claim 33, which further comprises processing said granulate into effervescent tablets, sublingual tablets, controlled release tablets or delayed release tablets.
- 46. The process according to claim 33 wherein the excipients comprise at least one ingredient selected from the group consisting of binders, disintegrants, and fillers.
- 47. The process according to claim 46, wherein said granulate exhibits a pH value of 6.5 or less.
- 48. The process according to claim 47, wherein said granulate has a pH of about 6.0 or less.
- 49. The process according to claim 47, wherein said granulate has a pH of about 5.5 or less.
- 50. The process according to claim 33, wherein said paroxetine sulfonate is paroxetine methane sulfonate.
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application claims the benefit of priority under 35 U.S.C. §119(e) from prior U.S. provisional application serial No. 60/228,110 filed Aug. 28, 2000 and from prior U.S. provisional application serial No. 60/234,936 filed Sep. 26, 2000: the entire contents of each of the aforementioned provisional applications being incorporated herein by reference.
Provisional Applications (2)
|
Number |
Date |
Country |
|
60228110 |
Aug 2000 |
US |
|
60234936 |
Sep 2000 |
US |