Sustained release composition and method utilizing xanthan gum and an active ingredient

• US 5,292,534 A
• Filed: 03/25/1992
• Issued: 03/08/1994
• Est. Priority Date: 03/25/1992
• Status: Expired due to Term

• Current Assignee: Advanced Technology Pharmaceuticals Corp.
• Original Assignee: Valentine Enterprises, Inc.
• Inventors: Valentine, William, Valentine, William K.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): BENSTON JR, WILLIAM E
• Application Number:
  US07/857,516
• Time in Patent Office: 713 Days
• Field of Search: 424/451, 424/457, 424/469, 424/470, 424/489
• US Class Current: 424/451
• CPC Class Codes: A61K 31/455 Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
• CPC Class Codes: A61K 9/205 Polysaccharides, e.g. alginate, gums; Cyclodextrin
• CPC Class Codes: A61K 9/2077 Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets

Abstract

A compacted sustained release composition for delivering a drug as an active ingredient to the gastro-intestinal tract comprises an effective amount of the active ingredient in mixture with xanthan gum, the active ingredient comprising in excess of 40 percent by weight of the total of the active ingredient and the xanthan gum, the mixture being in the form of a unit dose in capsule or tablet form. In addition to niacin, the active ingredient may be an analgesic, antipyretic, anti-inflammatory agent, vitamin, electrolyte replenisher, decongestant, antihistamine, and useful bacteriological organisms for the gastro-intestinal tract.

Claims

1. A sustained release composition for slow delivery of a drug as an active ingredient to the gastro-intestinal tract consisting of an effective amount of said active ingredient in mixture with xanthan gum and a lubricant, the mixture being in the form of a compacted unit dose, said active ingredient being present in an amount of 40-80 weight percent of said unit dose, said xanthan gum being present in an amount of 20-50 weight percent of said unit dose.

32. The composition of claim 1 wherein said active ingredient is an analgesic.

33. The composition of claim 1 wherein said active ingredient is an antipyretic.

34. The composition of claim 1 wherein said active ingredient is an anti-inflammatory agent.

35. The composition of claim 1 wherein said active ingredient is a vitamin.

36. The composition of claim 1 wherein said active ingredient is an electrolyte replenisher.

37. The composition of claim 1 wherein said active ingredient is a decongestant.

38. The composition of claim 1 wherein said active ingredient is an antihistamine.

39. The composition of claim 1 wherein said active ingredient is a useful bacteriological organism for the gastro-intestinal tract.

2. A method of producing a sustained release composition for slow delivery of a drug as an active ingredient to the gastro-intestinal tract consisting of mixing an effective amount of said active ingredient with xanthan gum and a lubricant, said active ingredient being present in an amount of 40-80 weight percent of said unit dose, said xanthan gum being present in an amount of 20-50 weight percent of the mixture, compacting the mixture and forming the mixture into a unit dose.

40. The method of claim 2 wherein said active ingredient is an analgesic.

41. The method of claim 2 wherein said active ingredient is an antipyretic.

42. The method of claim 2 wherein said active ingredient is an anti-inflammatory agent.

43. The method of claim 2 wherein said active ingredient is a vitamin.

44. The method of claim 2 wherein said active ingredient is an electrolyte replenisher.

45. The method of claim 2 wherein said active ingredient is a decongestant.

46. The method of claim 2 wherein said active ingredient is an antihistamine.

47. The method of claim 2 wherein said active ingredient is a useful bacteriological organism for the gastro-intestinal tract.

3. A sustained release composition for slow delivery of niacin as an active ingredient to the gastro-intestinal tract consisting of an effective amount of niacin in mixture with xanthan gum and a lubricant, the mixture being in the form of a compacted unit dose, said niacin being present in an amount of 40-80 weight percent of said unit dose, said xanthan gum being present in an amount of 20-50 weight percent of said unit dose.

4. A method of producing a sustained release composition for slow delivery of niacin as an active ingredient to the gastro-intestinal tract consisting of mixing an effective amount of niacin with xanthan gum and a lubricant, said niacin being present in an amount of 40-80 weight percent of said unit dose, said xanthan gum being present in an amount of 20-50 weight percent of the mixture, compacting the mixture and forming the mixture into a unit dose.

56. The method of claim 4 wherein said active ingredient is an analgesic.

5. A sustained release composition for slow delivery of a drug as an active ingredient to the gastro-intestinal tract consisting of an effective amount of said active ingredient in mixture with xanthan gum, the mixture being in the form of a unit dose in capsule or tablet form, said active ingredient being present in an amount of 40-80 weight percent of said unit dose, said xanthan gum being present in an amount of 20-50 weight percent of said unit dose.

6. The composition of claim 5 wherein said active ingredient is niacin.

7. The composition of claim 5 wherein said active ingredient is selected from the group consisting of analgesics, antipyretics, anti-inflammatory agents, vitamins, electrolyte replenishers, decongestants, antihistamines, and useful bacteriological organisms for the gastro-intestinal tract.

8. The composition of claim 5 wherein said unit dose comprises a major amount by weight of said active ingredient and a minor amount by weight of xanthan gum.

9. The composition of claim 5 wherein said active ingredient is niacin and said unit dose comprises a major amount by weight of niacin and a minor amount by weight of xanthan gum.

10. The composition of claim 5 wherein said active ingredient is combined with a water soluble, carbohydrate-based agglomerate.

48. The composition of claim 5 wherein said active ingredient is an analgesic.

49. The composition of claim 5 wherein said active ingredient is an antipyretic.

50. The composition of claim 5 wherein said active ingredient is an anti-inflammatory agent.

51. The composition of claim 5 wherein said active ingredient is a vitamin.

52. The composition of claim 5 wherein said active ingredient is an electrolyte replenisher.

53. The composition of claim 5 wherein said active ingredient is a decongestant.

54. The composition of claim 5 wherein said active ingredient is an antihistamine.

55. The composition of claim 5 wherein said active ingredient is a useful bacteriological organism for the gastro-intestinal tract.

11. A method of producing a sustained release composition for slow delivery of a drug as an active ingredient to the gastro-intestinal tract consisting of mixing an effective amount of said active ingredient with xanthan gum, said active ingredient being present in an amount of 40-80 weight percent of said mixture, said xanthan gum being present in an amount of 20-50 weight percent of said mixture, compacting the mixture and forming the mixture into a unit dose in capsule or tablet form.

12. The method of claim 11 wherein said active ingredient is niacin.

13. The method of claim 11 wherein said active ingredient is selected from the group consisting of analgesics, antipyretics, anti-inflammatory agents, vitamins, electrolyte replenishers, decongestants, antihistamines, and useful bacteriological organisms for the gastro-intestinal tract.

14. The method of claim 11 wherein said mixture comprises a major amount by weight of said active ingredient and a minor amount by weight of xanthan gum.

15. The method of claim 11 wherein said mixture comprises a major amount by weight of niacin and a minor amount by weight of xanthan gum.

16. The method of claim 11 further including combining said active ingredient with a water soluble, carbohydrate-based agglomerate prior to mixing with said xanthan gum.

57. The method of claim 11 wherein said active ingredient is an antipyretic.

58. The method of claim 11 wherein said active ingredient is an anti-inflammatory agent.

59. The method of claim 11 wherein said active ingredient is a vitamin.

60. The method of claim 11 wherein said active ingredient is an electrolyte replenisher.

61. The method of claim 11 wherein said active ingredient is a decongestant.

62. The method of claim 11 wherein said active ingredient is an antihistamine.

63. The method of claim 11 wherein said active ingredient is a useful bacteriological organism for the gastro-intestinal tract.

17. A sustained release composition for slow delivery of a drug as an active ingredient to the gastro-intestinal tract consisting of an effective amount of said active ingredient, xanthan gum and a lubricant, the mixture being in the form of a unit dose in capsule or tablet form, said active ingredient being present in an amount of 40-80 weight percent of said unit dose and said xanthan gum being present in an amount of 20-50 weight percent of said unit dose.

18. The composition of claim 17 wherein said active ingredient is niacin.

19. The composition of claim 17 wherein said active ingredient is selected from the group consisting of analgesics, antipyretics, anti-inflammatory agents, vitamins, electrolyte replenishers, decongestants, antihistamines, and useful bacteriological organisms for the gastro-intestinal tract.

20. The composition of claim 17 wherein said active ingredient comprises between 50 and 80 weight percent of said unit dose.

21. The composition of claim 20 wherein said active ingredient is niacin.

22. The composition of claim 20 wherein said active ingredient is selected from the group consisting of analgesics, antipyretics, anti-inflammatory agents, vitamins, electrolyte replenishers, decongestants, antihistamines, and useful bacteriological organisms or the gastro-intestinal tract.

23. A method for producing a sustained release composition for slow delivery of a drug as an active ingredient to the gastro-intestinal tract consisting of mixing an effective amount of said active ingredient, xanthan gum and a lubricant, said active ingredient being present in an amount of 40-80 weight percent of said mixture and said xanthan gum being present in an amount of 20-50 weight percent of said mixture, compacting the mixture and forming the mixture into a unit dose in capsule or tablet form.

24. The method of claim 23 wherein said active ingredient is niacin.

25. The method of claim 23 wherein said active ingredient is selected from the group consisting of analgesics, antipyretics, anti-inflammatory agents, vitamins, electrolyte replenishers, decongestants, antihistamines, and useful bacteriological organisms for the gastro-intestinal tract.

26. The method of claim 23 wherein said active ingredient comprises between 50 and 80 weight percent of said mixture.

27. The method of claim 26 wherein said active ingredient is niacin.

28. The method of claim 26 wherein said active ingredient is selected from the group consisting of analgesics, antipyretics, anti-inflammatory agents, vitamins, electrolyte replenishers, decongestants, antihistamines, and useful bacteriological organisms for the gastro-intestinal tract.

29. A sustained release composition for slow delivery of a drug as an active ingredient to the gastro-intestinal tract consisting of an effective amount of said active ingredient, a water soluble carbohydrate-based agglomerate, xanthan gum, and a lubricant, the mixture being in the form of a unit dose in capsule or tablet form, said active ingredient being present in an amount of 40-80 weight percent of said unit dose and said xanthan gum being present in an amount of 20-50 weight percent of said unit dose.

30. The composition of claim 29 wherein said active ingredient is niacin.

31. The composition of claim 29 wherein said active ingredient is selected from the group consisting of analgesics, antipyretics, anti-inflammatory agents, vitamins, electrolyte replenishers, decongestants, antihistamines, and useful bacteriological organisms for the gastro-intestinal tract.

64. The composition of claim 29 wherein said active ingredient is an analgesic.

65. The composition of claim 29 wherein said active ingredient is an antipyretic.

66. The composition of claim 29 wherein said active ingredient is an anti-inflammatory agent.

67. The composition of claim 29 wherein said active ingredient is a vitamin.

68. The composition of claim 29 wherein said active ingredient is an electrolyte replenisher.

69. The composition of claim 29 wherein said active ingredient is a decongestant.

70. The composition of claim 29 wherein said active ingredient is an antihistamine.

71. The composition of claim 29 wherein said active ingredient is a useful bacteriological organism for the gastro-intestinal tract.