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1. WO2004100880 - FORMULATION A LIBERATION CONTROLEE DE DERIVES D'ERYTHROMYCINE

Note: Texte fondé sur des processus automatiques de reconnaissance optique de caractères. Seule la version PDF a une valeur juridique

[ EN ]

WHAT IS CLAIMED IS:

1. A controlled release formulation in tablet form comprising a pharmaceutically effective amount of an erythromycin derivative and a lubricating effective amount of a lubricant in the absence of a material selected from the group consisting of alginic acid or salts thereof and hydrophilic sustained release polymers when said alginic acid or salt thereof or hydrophilic sustained release polymer is present in
concentrations effective to retard the release of the erythromycin derivatives from the pharmaceutical composition.

2. The controlled release formulation of Claim 1 which additionally comprises an release promoter.

3. The controlled release formulation of Claim 1 which additionally comprises a binder.

4. The controlled release formulation of Claim 2 which additionally comprises a binder.

5. The controlled release formulation according to Claim 1 wherein the
erythromycin derivative is present in concentration ranging from about 40% by weight to about 99% by weight of the tablet.

6. The controlled release formulation according to Claim 5 wherein the
erythromycin derivative is present in a concentration from about 50% to about 90% by weight of the tablet.

7. The controlled release formulation of Claim 1 wherein the lubricant is present in amounts ranging from about 1 to about 10% by weight of the tablet.

8. The controlled release formulation according to Claim 7 wherein the lubricant is present in amounts ranging from about 2 to about 5% by weight of the tablet.

9. The controlled release formulation according to Claim 1 wherein the release promoter is present in amounts ranging from about 0.01 %> to about 60% by weight of the tablet.

10. The controlled release formulation according to Claim 9 wherein the release promoter is hydrophilic.

11. The controlled release formulation according to Claim 10 wherein the release promoter is microcrystalline cellulose, silicified microcrystalline cellulose, maltodextrin, lactose, starch, or sugar, or combination thereof.

12. The controlled release formulation according to Claim 10 wherein the release promoter is present in amounts ranging from 10% to about 60%) by weight of the tablet.

13. The controlled release formulation according to Claim 12 wherein the release promoter is present in amounts ranging from about 15% to about 45%> by weight of the tablet.

14. The controlled release formulation according to Claim 2 wherein the release promoter is a water soluble organic acid.

15. The controlled release formulation of Claim 14 wherein the water soluble organic acid is present in amounts ranging from about 0.1% to about 10% by weight of the tablet.

16. The controlled release formulation of Claim 15 wherein the water soluble organic acid is present in amounts ranging from about 0.5 to about 5% by weight of the tablet.

17. The controlled release formulation of Claim 15 wherein the water soluble organic acid is present in amounts ranging from about 1.0 to about 3% by weight of the tablet.

18. The controlled release formulation according to Claim 14 wherein the water soluble organic acid is citric acid, benzoic acid, tartaric acid or cinnamic acid.

19. The controlled release formulation according to Claim 2 wherein the release promoter is a hydrophilic surfactant.

20. The controlled release formulation according to Claim 19 wherein the hydrophilic surfactant is a non-ionic surfactant or ionic surfactant.

21. The controlled release formulation according to Claim 20 wherein the hydrophilic surfactant is sodium lauryl sulfate.

22. The controlled release fonnulation according to Claim 3 wherein the binder is a hydrophilic polymer.

23. The controlled release formulation according to Claim 22 wherein the hydrophilic binder is PVP, HPMC, polyethylene glycol or hydroxypropyl cellulose.

24. The controlled release formulation according to Claim 22, wherein the polymeric binder is present in amounts ranging from about 0.1 to about 10% by weight of the tablet.

25. The controlled release formulation according to Claim 24 wherein the polymeric binder is present in amounts ranging from about 2% to about 6% by weight of the tablet.

26. The controlled release formulation according to Claim 25 wherein the polymeric binder is present in amounts ranging from about 2% to about 5% by weight of the tablet.

27. The controlled release formulation according to Claim 1 wherein
microcrystalline.cellulose or silicified microcrystalline cellulose is additionally present.

28. The controlled release formulation according to Claim 1 wherein maltodextrin is additionally present.

29. The controlled release formulation according to Claim 1 wherein the tablet additionally comprises maltodextrin in combination with a cellulose derivative selected from the group consisting of microcrystalline cellulose and silicified microcrystalline cellulose.

30. The controlled release formulation according to Claim 1 which additionally comprises a water insoluble pharmaceutically acceptable non-polymeric material.

31. The controlled release formulation according to Claim 30 wherein the non-polymeric material is a wax.

32. The controlled release formulation according to Claim 1 wherein the pharmaceutical dosage form is coated with a water soluble polymer or water insoluble polymer or combination thereof.

33. The controlled release formulation according to Claim 32 wherein the coating is present in amounts ranging from about 0.5% to about 10%> of the tablet.

34. The controlled release formulation according to Claim 33 wherein the coating is present in amounts ranging from about 1% to about 6% by weight of the tablet.

35. The controlled release formulation according to Claim 34 wherein the coating is present in amounts ranging from about 2% to about 5%> by weight of the tablet.

36. The controlled release formulation according to Claim 32 wherein the polymer is HPMC.

37. The controlled release formulation according to Claim 1 wherein the tablet contains 100 mg to 1500 mg inclusive of erythromycin derivative.

38. The controlled release formulation according to Claim 37 wherein the tablet contains 500 mg to 1000 mg inclusive of erythromycin derivative.

39. The controlled release formulation according to any one of Claims 1-38 wherein the erythromycin derivative is clarithromycin.

40. A method for facilitating the release of an erythromycin derivative from a pharmaceutical composition comprising a therapeutically effective amount of the erythromycin derivative and a lubricating effective amount of a lubricant, said method comprising adding to said composition a release promoter in tablet disintegrating effective amounts to facilitate the release of the erythromycin derivative from the tablet.

41. The method according to Claim 40 wherein the tablet additionally comprises a binder.

42. The method according to Claim 40 wherein the erythromycin derivative is present in concentration ranging from about 40% by weight to about 99% by weight of the tablet.

43. The method according to Claim 42 wherein the erythromycin derivative is present in a concentration from about 50%> to about 90%> by weight of the tablet.

44. The method according to Claim 40 wherein the lubricant is present in amounts ranging from about 1 to about 10% by weight of the tablet.

45. The method according to Claim 44 wherein the lubricant is present in amounts ranging from about 2 to about 5% by weight of the tablet.

46. The method according to Claim 44 wherein the release promoter is present in amounts ranging from about 0.01% to about 60% by weight of the tablet.

47. The method according to Claim 40 wherein the release promoter is hydrophilic.

48. The method according to Claim 47 wherein the release promoter is
microcrystalline cellulose, silicified microcrystalline cellulose, maltodextrin, lactose, starch, sugar, or combination thereof.

49. The method according to Claim 46 wherein the release promoter is present in amounts ranging from 10% to about 60% by weight of the tablet.

50. The method according to Claim 49 wherein the release promoter is present in amounts ranging from about 15% to about 45%) by weight of the tablet.

51. The method according to Claim 40 wherein the release promoter is a water soluble organic acid.

52. The method according to Claim 51 wherein the water soluble organic acid is present in amounts ranging from about 0.1% to about 10%o by weight of the tablet.

53. The method according to Claim 52 wherein the water soluble organic acid is present in amounts ranging from about 0.5 to about 5% by weight of the tablet.

54. The method according to Claim 53 wherein the water soluble organic acid is present in amounts ranging from about 1.0 to about 3% by weight of the tablet.

55. The method according to Claim 54 wherein the water soluble organic acid is citric acid, benzoic acid, tartaric acid or cinnamic acid.

56. The method according to Claim 40 wherein the release promoter is a
hydrophilic surfactant.

57. The method according to Claim 56 wherein the hydrophilic surfactant is a non-ionic surfactant or ionic surfactant.

58. The method according to Claim 57 wherein the hydrophilic surfactant is sodium lauryl sulfate.

59. The method according to Claim 41 wherein the binder is a hydrophilic polymer.

60. The method according to Claim 59 wherein the hydrophilic binder is PVP, HPMC polyethylene glycol or hydroxypropyl cellulose.

61. The method according to Claim 59 wherein the polymeric binder is present in amounts ranging from about 0.1 to about 10%> by weight of the tablet.

62. The method according to Claim 61 wherein the polymeric binder is present in amounts ranging from about 2% to about 6% by weight of the tablet.

63. The method according to Claim 62 wherein the polymeric binder is present in amounts ranging from about 2%> to about 5% by weight of the tablet.

64. The method according to Claim 40 wherein the tablet is coated with a water soluble polymer or water insoluble polymer.

65. The method according to any one of Claims 40-64 wherein the erythromycin derivative is clarithromycin.