Claims for Patent: 6,717,015

Summary for Patent: 6,717,015

Title:	Venlafaxine besylate
Abstract:	Venlafaxine besylate compounds provide certain advantages over venlafaxine hydrochloride and are useful in forming pharmaceutical compositions and n treating venlafaxine-treatable diseases and conditions. Venlafaxine besylate can be easily formulated into an extended release dosage form including a hydrogel tablet as well as other matrix-based tablet compositions. A preferred tablet making process involves hot melt granulation.
Inventor(s):	Keltjens; Rolf (Nijmegen, NL), Platteeuw; Johannes Jan (s'Hertogenbosch, NL), Cucala Escoi; Juan (Barcelona, ES), Margallo Lana; Inocencia (Barcelona, ES), Picha; Frantisek (Brno, CZ), Gallego Luengo; Montserrat (Barcelona, ES)
Assignee:	Synthon BV (Nijmegen, NL)
Application Number:	10/397,373
Patent Claims:	1. A venlafaxine besylate compound. 2. The venlafaxine besylate compound according to claim 1, which is crystalline venlafaxine besylate. 3. The venlafaxine besylate compound according to claim 1, wherein said venlafaxine is (+/-)-venlafaxine. 4. The venlafaxine besylate compound according to claim 2, which is crystalline venlafaxine besylate monohydrate. 5. The venlafaxine besylate compound according to claim 4, which is crystalline (+/-)-venlafaxine besylate monohydrate. 6. The venlafaxine besylate compound according to claim 2, which is crystalline venlafaxine besylate anhydrate. 7. The venlafaxine besylate compound according to claim 1, wherein said venlafaxine is pure or substantially pure (+) or (-) venlafaxine enantiomer. 8. A pharmaceutical composition comprising a venlafaxine besylate compound and at least one pharmaceutically acceptable excipient. 9. The composition according to claim 8, wherein said at least one excipient is selected from the group consisting of polymers, waxes, calcium phosphates, and sugars. 10. The composition according to claim 9, wherein said at least one excipient is selected from the group consisting of HPMC, microcrystalline cellulose, and calcium phosphates. 11. The composition according to claim 10, which further comprises a lubricant. 12. The composition according to claim 9, wherein said at least one excipient is selected from the group consisting of hydrogenated castor oil, glyceryl behenate, glycerylpalmito stearate, and saturated polyglycolyzed glycerate. 13. The composition according to claim 8, wherein said composition is in the form of granules, pellets, or a powder blend. 14. The composition according to claim 8, wherein said composition is in the form of a tablet. 15. The composition according to claim 8, wherein said composition is a unit dosage form and said venlafaxine besylate is contained in an amount between 30 mg and 300 mg. 16. The composition according to claim 8, wherein said composition is an extended release composition. 17. The composition according to claim 16, wherein said composition has a dissolution profile such that less than 30% of said venlafaxine besylate is released from said composition in 2 hours using either purified water or SGF at 37.degree. C. with stirring at 100 r.p.m. in a basket apparatus. 18. The composition according to claim 17, wherein said composition has a release profile that satisfies the following: using USP Apparatus 1 (basket) at 100 rpm in purified water at 37.degree. C. 19. The composition according to claim 16, wherein said composition is a once daily dose tablet. 20. The composition according to claim 16, wherein said composition is a tablet and said at least one excipient is a matrix material. 21. The composition according to claim 20, wherein said matrix material is a hydrophilic, lipophilic or biodegradable matrix material. 22. The composition according to claim 21, wherein said tablet is a hydrogel tablet. 23. The composition according to claim 21, wherein said tablet comprises hydroxypropylmethyl cellulose and venlafaxine besylate. 24. The composition according to claim 23, which further comprises a calcium phosphate, microcrystalline cellulose, or a lubricant. 25. The composition according to claim 23, wherein said tablet is a once daily dose tablet. 26. The composition according to claim 21, wherein said matrix material is a lipophilic matrix material. 27. The composition according to claim 26, wherein said matrix material is selected from the group consisting of glyceryl palmitostearate, glyceryl behenate, and hydrogenated castor oil. 28. The composition according to claim 27, wherein said tablet further comprises a calcium phosphate or a lubricant. 29. The composition according to claim 26, wherein said tablet is a once daily dose tablet. 30. The composition according to claim 16, wherein said composition is in the form of pellets. 31. The composition according to claim 30, wherein said pellets have a dissolution profile that satisfies the following criteria: using USP Apparatus 1 (basket) at 100 rpm in purified water at 37.degree. C. 32. The composition according to any one of claims 8-31, wherein said venlafaxine besylate is (+/-)-venlafaxine besylate monohydrate. 33. A method for treating a venlafaxine-treatable disease or condition, which comprises administering to a patient in need thereof an effective amount of a venlafaxine besylate compound. 34. The method according to claim 33, wherein said venlafaxine besylate compound is administered in the form of a tablet. 35. The method according to claim 34, wherein said patient suffers from depression and said effective amount of venlafaxine besylate is an antidepressant amount. 36. The method according to claim 33, wherein said venlafaxine besylate compound is administered once daily. 37. The method according to claim 36, wherein said venlafaxine besylate compound is administered orally in the form of one or two tablets once daily. 38. A process, which comprises: mixing venlafaxine besylate and a molten fusible carrier to form a partially melted mass; and cooling said partially melted mass to form a solidified product. 39. The process according to claim 38, wherein said solidified product is in the form of granules or pellets. 40. The process according to claim 39, which further comprises milling said solidified product to form granules. 41. The process according to claim 38, which further comprises combining, prior to said mixing step, said fusible carrier in a non-molten state with said venlafaxine besylate and heating to render said fusible carrier molten. 42. The process according to claim 38, wherein said fusible carrier is a lipophilic matrix material. 43. The process according to claim 42, wherein said fusible carrier is a wax. 44. The process according to claim 38, wherein said mixing step further includes mixing at least excipient selected from the group consisting of calcium phosphates, microcrystalline cellulose, and lactose. 45. The process according to claim 44, which further comprises mixing said solidified product, optionally after milling, with a lubricant to form a tabletting mixture and forming a tablet from said tabletting mixture. 46. The process according to claim 38, which further comprises mixing said solidified product, optionally after milling, with a lubricant and at least one excipient selected from the group consisting of calcium phosphates, microcrystalline cellulose, and lactose. 47. The process according to claim 38, which further comprises converting said solidified product into a tablet. 48. The process according to claim 47, wherein said tablet is an extended release tablet. 49. The process according to claim 48, wherein said tablet has a release profile that satisfies the following: using USP Apparatus 1 (basket) at 100 rpm in purified water at 37.degree. C.