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Claims for Patent: 6,129,930

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Claims for Patent: 6,129,930

Title: Methods and sustained release nicotinic acid compositions for treating hyperlipidemia at night
Abstract:An orally administered antihyperlipidemia composition according to the present invention includes from about 250 to about 3000 parts by weight of nicotinic acid, and from about 5 to about 50 parts by weight of hydroxypropyl methylcellulose. Also, a method of treating hyperlipidemia in a hyperlipidemic having a substantially periodic physiological loss of consciousness, includes the steps of forming a composition having an effective antihyperlipidemic amount of nicotinic acid and a time release sustaining amount of a swelling agent. The method also includes the step of orally administering the composition to the hyperlipidemic once per day "nocturnally," that is in the evening or at night.
Inventor(s): Bova; David J. (Boca Raton, FL)
Assignee:
Application Number:08/814,974
Patent Claims: 1. A daily method of treating hyperlipidemia in a patient comprising orally administering to the patient a sustained release composition of nicotinic acid once per day during the evening for providing an effective antihyperidemic amount of nicotinic acid to the patient to induce at least some lowering of total cholesterol, LDL cholesterol, triglycerides and Lp(a) and at least some increase in HDL cholesterol in the patient's blood stream, without causing abnormalities in uric acid levels or glucose levels or both to an extent which would require said daily treatment to be discontinued by the patient, the sustained release composition comprising an effective antihyperlipidemic amount of nicotinic acid and an excipient to provide sustained release of the nicotinic acid.

2. A method of claim 1, wherein the effective antihyperlipidemic amount of nicotinic acid is from about 250 mg to about 3000 mg of nicotinic acid.

3. A method of claim 1, wherein the excipient is selected from the group consisting of a swelling agent, a binder, a processing aid and mixtures thereof.

4. A method of claim 3, wherein the swelling agent is selected from group consisting of a polymer, a wax, a natural material and mixtures thereof.

5. A method of claim 4, wherein the polymer is selected from the group consisting of hydroxypropyl methylcellulose, sodium carboxymethylcellulose and ethylcellulose.

6. A method of claim 4, wherein the wax is bees wax.

7. A method of claim 4, wherein the natural material is selected from the group consisting of gums and gelatins.

8. A method of claim 3, wherein the binder is povidone.

9. A method of claim 3, wherein the processing aid is a lubricant.

10. A method of claim 9, wherein the lubricant is stearic acid.

11. A method of claim 5, wherein the hydroxypropyl methylcellulose is in an amount ranging from about 5% to about 50% parts by weight per 100 parts by weight of the sustained release composition.

12. A method of claim 3, wherein the binder is in an amount ranging from about 1% to about 5% parts by weight per 100 parts by weight of the sustained release composition.

13. A method of claim 3, wherein the processing aid is in an amount ranging from about 0.5% to about 2% parts by weight per 100 parts by weight of the sustained release composition.

14. A method of claim 1, wherein the sustained release composition consists essentially of nicotinic acid, hydroxypropyl methylcellulose, povidone and stearic acid.

15. A method of claim 1, wherein the sustained release composition consists essentially of

nicotinic acid 375.0 mg,

hydroxypropyl methylcellulose 188.75 mg,

povidone 12.9 mg., and

stearic acid 5.8 mg.

16. A method of claim 1, wherein the sustained release composition consists essentially of

nicotinic acid 500.0 mg,

hydroxypropyl methylcellulose 203.0 mg,

povidone 17.2 and

stearic acid 7.3.

17. A method of claim 1, wherein the sustained release composition consists essentially of

nicotinic acid 750.0

hydroxypropyl methylcellulose 204.7

povidone 25.9 and

stearic acid 9.9.

18. A sustained release composition of nicotinic acid for oral administration to a patient once per day during the evening or at night for providing and effective antihyperlipidemic amount of nicotinic acid to the patient to induce at least some lowering of total cholesterol, LDL cholesterol, triglycerides and Lp(a) and at least some increase in HDL cholesterol in the patient's blood stream, without causing abnormalities in uric acid levels or glucose levels or both to an extent which would require the use of said release composition by the patient to be discontinued, said sustained release composition comprising (a) an effective antihyperlipidemic amount of nicotinic acid, and (b) an excipient to provide sustained release of the nicotinic acid.

19. A sustained release composition of claim 18, wherein said excipient is selected from the group consisting of a swelling agent, a binder, a processing aid and mixtures thereof.

20. A sustained release composition of claim 19, wherein the swelling agent is selected from group consisting of a polymer, a wax, a natural material and mixtures thereof.

21. A sustained release composition of claim 20, wherein the polymer is selected from the group consisting of hydroxypropyl methylcellulose, sodium carboxymethylcellulose and ethylcellulose.

22. A sustained release composition of claim 20, wherein the wax is bees wax.

23. A sustained release composition of claim 20, wherein the natural material is selected from the group consisting of gums and gelatins.

24. A sustained release composition of claim 19, wherein the binder is povidone.

25. A sustained release composition of claim 19, wherein the processing aid is a lubricant.

26. A sustained release composition of claim 25, wherein the lubricant is stearic acid.

27. A sustained release composition of claim 21, wherein the hydroxypropyl methylcellulose is in an amount ranging from about 5% to about 50% parts by weight per 100 parts by weight of the sustained release composition.

28. A sustained release composition of claim 19, wherein the binder is in an amount ranging from about 1% to about 5% parts by weight per 100 parts by weight of the sustained release composition.

29. A sustained release composition of claim 19, wherein the processing aid is in an amount ranging from about 0.5% to bout 2% parts by weight per 100 parts by weight of the sustained release composition.

30. A sustained release composition of claim 18, wherein the sustained release composition consists essentially of nicotinic acid, hydroxypropyl methylcellulose, povidone and stearic acid.

31. A sustained release composition of claim 18, wherein the sustained release composition consists essentially of

nicotinic acid 375.0 mg,

hydroxypropyl methylcellulose 188.7 mg,

povidone 12.9 mg., and

stearic acid 5.8 mg.

32. A sustained release composition of claim 18, wherein the sustained release composition consists essentially of

nicotinic acid 500.0 mg,

hydroxypropyl methylcellulose 203.0 mg,

povidone 17.2 mg., and

stearic acid 7.3 mg.

33. A sustained composition of claim 18, wherein the sustained release composition consists essentially of

nicotinic acid 750.0 mg,

hydroxypropyl methylcellulose 204.7 mg,

povidone 25.9 mg., and

stearic acid 9.9 mg.

34. A daily method of treating hyperlipidemia in a patient without inducing treatment-limiting elevations in uric acid levels or glucose levels or both in the patient, said daily method comprising orally dosing the patient with an effective antihyperlipidemic amount of nicotinic acid once per day during the evening or at night as a dose, wherein the nicotinic acid is combined with at least one pharmaceutically acceptable carrier to form an oral sustained release solid dosage form.

35. A method, as set forth in claim 34, wherein the patient is dosed with from about 250 mg to about 3000 mg of nicotinic acid.

36. A method, as set forth in claim 35, wherein the release rate of the nicotinic acid is from about 2.0% per hour to about 25% per hour.

37. A method, as set forth in claim 34, wherein the oral sustained release solid dosage form is prepared by formulating the nicotinic acid with from about 5 parts to about 50 parts by weight of hydroxypropyl methylcellulose per 100 parts by weight of the oral sustained release solid dosage form.

38. A method, as set forth in claim 34, wherein the oral sustained release solid dosage form contains from about 1 part to about 4 parts by weight of binder per 100 parts by weight of the oral sustained release solid dosage form.

39. A method, as set forth in claim 36, wherein the binder is a polymer having the repeating polymerization unit 1-ethenyl-2-pyrrolidone.

40. A method, as set forth in claim 34, wherein the oral sustained release solid dosage form contains from abut 0.5 parts to abut 2.5 parts by weight of a lubricant per 100 parts by weight of the oral sustained release solid dosage form.

41. A method, as set forth in claim 40, wherein the lubricant is selected from the group consisting of lubricants consisting of stearic acid and magnesium stearate.

42. A method, as set forth in claim 34, wherein the oral sustained release solid dosage form contains from about 250 mg to about 3000 mg of nicotinic acid.

43. A method, as set forth in claim 34, wherein the oral sustained release solid dosage form is an oral sustained release tablet.

44. A method, as set forth in claim 43, wherein the oral sustained release tablet contains nicotinic acid in an amount selected from the group consisting of about 375 mg, about 500 mg and about 750 mg.

45. A method, as set forth in claim 43, wherein the oral sustained release tablet contains

(a) about 375 mg nicotinic acid,

(b) about 189 mg hydroxypropyl methylcellulose as a swelling agent

(c) about 13 mg a polymer having the repeating polymerization unit 1-ethenyl-2-pyrrolidone as a binder, and

(d) about 6 mg of stearic as a lubricant.

46. A method, as set forth in claim 43, wherein the oral sustained release tablet contains

(a) about 500 mg nicotinic acid,

(b) about 203 mg hydroxypropyl methylcellulose as a swelling agent

(c) about 17.2 mg polyvinyl pyrrolidone as a binder, and

(d) about 7.3 mg of stearic as a lubricant.

47. A method, as set forth in claim 43, wherein the oral sustained release tablet contains

(a) about 750 mg nicotinic acid,

(b) about 205 mg hydroxypropyl methylcellulose as a swelling agent

(c) about 26 mg polyvinyl pyrrolidone as a binder, and

(d) about 10 mg of stearic as a lubricant.

48. A method, as set forth in claim 43, wherein the oral sustained release tablet contains

(a) about 30% to about 90% by weight nicotinic acid,

(b) about 5% to about 50% by weight hydroxypropyl methylcellulose as a swelling agent,

(c) about 1% to about 5% by weight a polymer having repeating polymerization unit 1-ethenyl-2-pyrrolidone as a binder, and

(d) about 0.5% to about 2% by weight stearic acid as a lubricant.

49. A method, as set forth in claim 43, wherein the oral sustained release tablet contains

(a) about 30% to about 90% by weight nicotinic acid,

(b) about 5% to about 50% by weight hydroxypropyl methylcellulose as a swelling agent.

50. A method, as set forth in claim 34, wherein said single dose treatment during the evening or at night elevates HDL cholesterol in the patient.

51. A daily method of treating hyperlipidemia in a patient without inducing treatment-limiting abnormalities in uric acid levels or glucose levels or both in the patient, said daily method comprising orally dosing the patient with an effective antihyperlipidemic amount of nicotinic acid once per day during the evening or at night as a single dose for providing an effective antihyperlipidemic amount of nicotinic acid to the patient to induce at least some decrease in levels of total cholesterol, LDL cholesterol, triglycerides and Lp(a) in the patient and to induce at least some increase in levels of HDL cholesterol in the patient, without causing

abnormalities in either uric acid or glucose levels or both to an extent which would require said daily treatment to be discontinued by the patient, wherein the nicotinic acid is combined with at least one pharmaceutically acceptable component to form an oral sustained release solid dosage form.

52. A method, as set forth in claim 51, wherein said single dose treatment induces at least some decrease in levels of total cholesterol, LDL cholesterol, triglycerides and Lp(a) in the patient.

53. A method, as set forth in claim 51, wherein said single dose treatment elevates HDL cholesterol in the patient.

54. A method of treating hyperlipidemia in a human without causing treatment-limiting elevations in uric acid levels or glucose levels or both in the human, said daily treatment comprising ingesting an oral sustained release nicotinic acid tablet once per day as a single dose for providing an effective antihyperlipidemic amount of nicotinic acid to the human without causing treatment-limiting elevations in uric acid or glucose levels or both in the human, wherein the nicotinic acid is combined with at least one pharmaceutically acceptable component to form the oral sustained release tablet.

55. A method, as set forth in claim 54, wherein said single dose treatment induces at least some decrease in levels of total cholesterol, LDL cholesterol, triglycerides and Lp(a) in the human.

56. A method, as set forth in claim 54, wherein said single dose treatment elevates HDL cholesterol in the human.

57. A daily method of treating hyperlipidemia in a patient without inducing treatment-limiting liver damage, said daily method comprising orally dosing the patient with an effective antihyperlipidemic amount of nicotinic acid once per day during the evening or at night as a single dose, wherein the nicotinic acid is combined with at least one pharmaceutically acceptable carrier to form an oral sustained release solid dosage form, said single daily dose treatment causing little or no serious damage to the liver of the patient.

58. A method, as set forth in claim 57, wherein the patient is dosed with from about 250 mg to about 3000 mg of nicotinic acid.

59. A method, as set forth in claim 58, wherein the release rate of the nicotinic acid is from about 2.0% per hour to about 25% per hour.

60. A method, as set forth in claim 58, wherein the oral sustained release solid dosage form is prepared by formulating the nicotinic acid with from about 5 parts to about 50 parts by weight of hydroxypropyl methylcellulose per 100 parts by weight of the oral sustained release solid dosage form.

61. A method, as set forth in claim 57, wherein the oral sustained release solid dosage form contains from about 1 part to about 4 parts by weight of binder per 100 parts by weight of the oral sustained release solid dosage form.

62. A method, as set forth in claim 59, wherein the binder is a polymer having the repeating polymerization unit 1-ethenyl-2-pyrrolidone.

63. A method, as set forth in claim 59, wherein the oral sustained release solid dosage form contains from about 0.5 parts to about 2.5 parts by weight of a lubricant per 100 parts by weight of the oral sustained release solid dosage form.

64. A method, as set forth in claim 63, wherein the lubricant is selected from the group consisting of lubricants consisting of stearic acid and magnesium stearate.

65. A method, as set forth in claim 57, wherein the oral sustained release solid dosage form contains from about 250 mg to about 3000 mg of nicotinic acid.

66. A method, as set forth in claim 57, wherein the oral sustained release solid dosage form is an oral sustained release tablet.

67. A method, as set forth in claim 66, wherein the oral sustained release tablet contains nicotinic acid in an amount selected from the group consisting of about 375 mg, about 500 mg and about 750 mg.

68. A method, as set forth in claim 66, wherein the oral sustained release tablet contains

(a) about 375 mg nicotinic acid,

(b) about 189 mg hydroxypropyl methylcellulose as a swelling agent

(c) about 13 mg a polymer having the repeating polymerization unit 1-ethenyl-2-pyrrolidone as a binder, and

(d) about 6 mg of stearic as a lubricant.

69. A method, as set forth in claim 66, wherein the oral sustained release tablet contains

(a) about 500 mg nicotinic acid,

(b) about 203 mg hydroxypropyl methylcellulose as a swelling agent

(c) about 17.2 mg polyvinyl pyrrolidone as a binder, and

(d) about 7.3 mg of stearic acid as a lubricant.

70. A method, as set forth in claim 66, wherein the oral sustained release tablet contains

(a) about 750 mg nicotinic acid,

(b) about 205 mg hydroxypropyl methylcellulose as a swelling agent

(c) about 26 mg polyvinyl pyrrolidone as a binder, and

(d) about 10 mg of stearic acid as a lubricant.

71. A method, as set forth in claim 66, wherein the oral sustained release tablet contains

(a) about 30% to about 90% by weight nicotinic acid,

(b) about 5% to about 50% by weight hydroxypropyl methylcellulose as a swelling agent,

(c) about 1% to about 5% by weight a polymer having repeating polymerization unit 1-ethenyl-2-pyrrolidone as a binder, and

(d) about 0.5% to about 2% by weight stearic acid as a lubricant.

72. A method, as set forth in claim 66, wherein the oral sustained release tablet contains

(a) about 30% to about 90% by weight nicotinic acid,

(b) about 5% to about 50% parts by weight hydroxypropyl methylcellulose as a swelling agent.

73. A method, as set forth in claim 57, wherein said single dose treatment during the evening or at night elevates HDL cholesterol in the patient.

74. A method, as set forth in claim 57, wherein said single dose treatment during the evening or at night results in little or no serious increase in a liver function test in the patient, wherein the liver function test is selected from the group consisting of an AST, ALT and alkaline phosphatase liver function test.

75. A method, as set forth in claim 57, wherein said single dose treatment during the evening or at night results in little or no serious increase in uric acid in the patient.

76. A method, as set forth in claim 57, wherein said single dose treatment during the evening or at night results in little or no serious increase in free fasting glucose in the patient.

77. A daily method of treating hyperlipidemia in a patient without inducing treatment-limiting hepatotoxicity, said daily method comprising orally dosing the patient with an effective amount of nicotinic acid once per day during the evening or at night as a single dose for reducing hyperlipidemia in the patient, wherein the nicotinic acid is combined with at least one pharmaceutically acceptable component to form an oral sustained release solid dosage form, and wherein said single daily nicotinic acid dose treatment administered during the evening or at night is at least as effective in lowering at least one serum lipid in a patient wherein the serum lipid is selected from the group consisting of total cholesterol, LDL cholesterol, triglycerides and Lp(a), as treatment with an oral sustained release nicotinic acid preparation when it is dosed daily in two divided doses at a total daily nicotinic acid dosage which is at least equivalent to said single daily nicotinic acid dose treatment administered only during the evening or at night, and wherein said single daily nicotinic acid dose treatment administered during the evening or at night is essentially free of treatment-limiting hepatotoxic side effects which are generally associated with the oral sustained release nicotinic acid preparation when it is dosed daily in two divided doses at a total daily nicotinic acid dosage which is at least equivalent to said single daily nicotinic acid dose treatment administered during the evening or at night.

78. A method, as set forth in claim 77, wherein the patient is dosed with from 250 mg to about 3000 mg of nicotinic acid.

79. A method, as set forth in claim 77, wherein the release rate of said nicotinic acid is from about 2.0% per hour to about 25% per hour.

80. A method, as set forth in claim 77, wherein the oral solid dosage form is prepared by formulating the nicotinic acid with from about 5 to about 50 parts by weight of hydroxypropyl methylcellulose per 100 parts by weight of the oral solid dosage form.

81. A method, as set forth in claim 77, wherein the oral solid dosage form further contains from about 1 to about 4 parts by weight of a binder per 100 parts by weight of the oral solid dosage form.

82. A method, as set forth in claim 81, wherein the binder is polyvinyl pyrrolidone.

83. A method, as set forth in claim 77, wherein the oral solid dosage form further contains from about 0.5 to about 2.5 parts by weight of a lubricant per 100 parts by eight of the solid dosage form.

84. A method, as set forth in claim 83, wherein the lubricant is selected from the group consisting of stearic acid and magnesium stearate.

85. A method, as set forth in claim 77, wherein the oral sustained release solid dosage form contains from about 250 mg to about 3000 mg of nicotinic acid.

86. A method, as set forth in claim 77, wherein the oral sustained release solid dosage form is an oral sustained release tablet.

87. A method, as set forth in claim 86, wherein the oral sustained released tablet contains nicotinic acid in an amount selected from the group consisting of about 375 mg, about 500 mg and about 750 mg.

88. A method, as set forth in claim 86, wherein the oral sustained release tablet contains

(a) about 375 mg nicotinic acid,

(b) about 189 mg hydroxypropyl methylcellulose as a swelling agent,

(c) about 13 mg polyvinyl pyrrolidone as a binder, and

(d) about 6 mg of stearic acid as a lubricant.

89. A method, as set forth in claim 86, wherein the oral sustained release tablet contains

(a) about 500 mg nicotinic acid,

(b) about 203 mg hydroxypropyl methylcellulose as a swelling agent,

(c) about 17 mg polyvinyl pyrrolidone as a binder, and

(d) about 7 mg of stearic acid as a lubricant.

90. A method, as set forth in claim 86, wherein the oral sustained release tablet contains

(a) about 750 mg nicotinic acid,

(b) about 205 mg hydroxypropyl methylcellulose as a swelling agent,

(c) about 26 mg polyvinyl pyrrolidone as a binder, and

(d) about 10 mg stearic acid as a lubricant.

91. A method, as set forth in claim 86, wherein the oral sustained release tablet contains

(a) about 30% to about 90% by weight nicotinic acid,

(b) about 5% to about 50% by weight hydroxypropyl methylcellulose as a swelling agent,

(c) about 1% to about 5% by weight polyvinyl pyrrolidone as a binder, and

(d) about 0.5% to about 2% by weight stearic acid as a lubricant.

92. A method, as set forth in claim 87, wherein the oral sustained release tablet contains

(a) about 30% to about 90% parts by weight nicotinic acid, and

(b) about 5% to about 50% parts by weight hydroxypropyl methylcellulose as a swelling agent.

93. A method, as set forth in claim 77, wherein said single dose treatment during the evening or at night elevates HDL cholesterol in the patient.

94. A method, as set forth in claim 77, wherein said single dose treatment during the evening or at night results in little or no serious increase in a liver function test in the patient, wherein the liver function test is selected from the group consisting of an AST, ALT and alkaline phosphatase liver function test.

95. A method, as set forth in claim 77, wherein said single dose treatment during the evening or at night results in little or no serious increase in uric acid in the patient.

96. A method, as set forth in claim 77, wherein said single dose treatment during the evening or at night results in little or no serious increase in free fasting glucose in the patient.

97. A method of treating hyperlipidemia in a patient comprising orally dosing the patient with an effective amount of nicotinic acid once per day during the evening or at night as a single dose for lowering serum lipids, wherein said single nicotinic acid dosing is accomplished by ingestion of an oral sustained release tablet comprising nicotinic acid, a swelling agent, a binder and a lubricant, wherein said single nicotinic acid dosing during the evening or at night is at least as effective in lowering at least one serum lipid in a patient, wherein the serum lipid is selected

from the group consisting of total cholesterol, LDL cholesterol, triglycerides and Lp(a), as treatment with an oral sustained release nicotinic acid preparation when it is dosed in two daily divided doses at a total daily nicotinic acid dosage which is at least equivalent to said single nicotinic acid dose treatment administered during the evening or at night, and wherein said single nicotinic acid dosing administered during the evening or at night causes less elevations in liver function tests than treatment with the oral sustained release nicotinic acid preparation when it is dosed in two daily divided doses at a total daily nicotinic acid dosage which is at least equivalent to said single nicotinic acid dosing administered during the evening or at night.

98. A method, as set forth in claim 97, wherein the patient is dosed with from 250 mg to about 3000 mg of nicotinic acid.

99. A method, as set forth in claim 97, wherein the release rate of said nicotinic acid is from about 2.0% per hour to about 25% per hour.

100. A method, as set forth in claim 97, wherein said single dose treatment during the evening or at night elevates HDL cholesterol in the patient.

101. A method, as set forth in claim 97, wherein said single dose treatment during the evening or at night results in little or no serious increase in a liver function test in a patient wherein the liver function test is selected from the group consisting of an AST, ALT and alkaline phosphatase liver function test.

102. A method, as set forth in claim 97, wherein said single dose treatment during the evening or at night results in little or no serious increase in uric acid in the patient.

103. A method, as set forth in claim 97, wherein said single dose treatment during the evening or at night results in little or no serious increase in free fasting glucose in the patient.

104. A method, as set forth in claim 97, wherein the oral sustained release tablet contains about 5 to about 50 parts by weight of hydroxypropyl methylcellulose per 100 parts by weight of the oral sustained release tablet as the swelling agent.

105. A method, as set forth in claim 97, wherein the oral sustained release tablet further contains about 1 to about 4 parts by weight of a binder per 100 parts by weight of the oral sustained release tablet.

106. A method, as set forth in claim 105, wherein the binder is polyvinyl pyrrolidone.

107. A method, as set forth in claim 97, wherein the oral sustained release tablet further contains about 0.5 to about 2.5 parts by weight of a lubricant per 100 parts by weight of the oral sustained release tablet.

108. A method, as set forth in claim 107, wherein the lubricant is selected from the group consisting of stearic acid and magnesium stearate.

109. A method, as set forth in claim 97, wherein the oral sustained release tablet contains from about 250 mg to about 3000 mg of nicotinic acid.

110. A method, as set forth in claim 97, wherein the sustained release tablet contains

(a) about 30% to about 90% parts by weight nicotinic acid,

(b) about 5% to about 50% parts by weight hydroxypropyl methylcellulose as the swelling agent.

111. A method, as set forth in claim 97, wherein the oral sustained release tablet contains

(a) about 30% to about 90% by weight nicotinic acid,

(b) about 5% to about 50% by weight hydroxypropyl methylcellulose as a swelling agent,

(c) about 1% to about 5% by weight a polymer having repeating polymerization unit 1-ethenyl-2-pyrrolidone as a binder, and

(d) about 0.5% to about 2% by weight stearic acid as a lubricant.

112. A method, as set forth in claim 97, wherein the sustained release tablet contains

(a) about 375 mg nicotinic acid,

(b) about 189 mg hydroxypropyl methylcellulose as a swelling agent,

(c) about 13 mg polyvinyl pyrrolidone as a binder, and

(d) about 6 mg of stearic acid as a lubricant.

113. A method, as set forth in claim 97, wherein the sustained release tablet contains

(a) about 500 mg nicotinic acid,

(b) about 203 mg hydroxypropyl methylcellulose as a swelling agent,

(c) about 17 mg polyvinyl pyrrolidone as a binder, and

(d) about 7 mg of stearic acid as a lubricant.

114. A method, as set forth in claim 98, wherein the sustained release tablet contains

(a) about 750 mg nicotinic acid,

(b) about 205 mg hydroxypropyl methylcellulose as a swelling agent,

(c) about 26 mg polyvinyl pyrrolidone as a binder, and

(d) about 10 mg stearic acid as a lubricant.

115. A method of treating hyperlipidemia in a patient without inducing treatment-limiting (i) hepatotoxicity and (ii) abnormalities in uric acid levels or glucose levels or both, said method comprising orally dosing the patient with an effective antihyperlipidemic amount of nicotinic acid once per day during the evening or at night as a single dose, wherein the nicotinic acid is combined with at least one pharmaceutically acceptable component to form an oral sustained release solid dosage form, wherein the oral sustained release solid dosage form is effective in reducing a serum lipid without causing treatment-limiting (i) hepatotoxicity and (ii) elevations in uric acid levels or glucose levels or both in the patient to a level which would require said treatment to be discontinued by the patient when it is ingested by the patient once per day during the evening or at night as the single dose in accordance with said single dose treatment.

116. A daily method of treating hyperlipidemia in a patient comprising orally administered to the patient a sustained release composition of nicotinic acid once per day during the evening or or night for providing an effective antihyperlipidemic amount of nicotinic acid to the patient to induce at least some lowering of total cholesterol, LDL cholesterol, triglycerides and Lp(a) and at least some increase in HDL cholesterol in the patient's blood stream, without causing abnormalities in liver function tests and uric acid levels or glucose levels to an extent which would require said daily treatment to be discontinued by the patient, the sustained release composition comprising an effective antihyperlipidemic amount of nicotinic acid and an excipient to provide sustained release of the nicotinic acid.

117. A method of claim 116, wherein the effective antihyperlipidemic amount of nicotinic acid is from about 250 mg to about 3000 mg of nicotinic acid.

118. A method of claim 116, wherein the excipient is selected from the group consisting of a swelling agent, a binder, a processing aid and mixtures thereof.

119. A method of claim 118, wherein the swelling agent is selected from group consisting of a polymer, a wax, a natural material and mixtures thereof.

120. A method of claim 119, wherein the polymer is selected from the group consisting of hydroxypropyl methylcellulose, sodium carboxymethylcellulose and ethylcellulose.

121. A method of claim 119, wherein the wax is bees wax.

122. A method of claim 119, wherein the natural material is selected from the group consisting of gums and gelatins.

123. A method of claim 118, wherein the binder is povidone.

124. A method of claim 118, wherein the processing aid is a lubricant.

125. A method of claim 124, wherein the lubricant is stearic acid.

126. A method of claim 120, wherein the hydroxypropyl methylcellulose is in an amount ranging from about 5% to about 50% parts by weight per 100 parts by weight of the sustained release composition.

127. A method of claim 118, wherein the binder is in an amount ranging from about 1% to about 5% parts by weight per 100 parts by weight of the sustained release composition.

128. A method of claim 118, wherein the processing aid is in an amount ranging from about 0.5% to about 2% parts by weight per 100 parts by weight of the sustained release composition.

129. A method of claim 117, wherein the sustained release composition consists essentially of nicotinic acid, hydroxypropyl methylcellulose, povidone and stearic acid.

130. A method of claim 117, wherein the sustained release composition consists essentially of

nicotinic acid 375.0 mg,

hydroxypropyl methylcellulose 188.7 mg,

povidone 12.9 mg., and

stearic acid 5.8 mg.

131. A method of claim 116, wherein the sustained release composition consists essentially of

nicotinic acid 500.0 mg,

hydroxypropyl methylcellulose 203.0 mg,

povidone 17.2 mg, and

stearic acid 7.3 mg.

132. A method of claim 116, wherein the sustained release composition consists essentially of

nicotinic acid 750.0 mg.

hydroxypropyl methylcellulose 204.7 mg.

povidone 25.9 mg. and

stearic acid 9.9 mg.

133. A sustained release composition of nicotinic acid for oral administration to a patient once per day during the evening or night for providing an effective antihyperlipidemic amount of nicotinic acid to the patient to induce at least some lowering of total cholesterol, LDL cholesterol, triglycerides and Lp(a) and at least some increase in HDL cholesterol in the patient's blood stream, without causing abnormalities in liver function tests and uric acid levels or glucose levels or both to an extent which would require the use of said sustained release composition by the patient to be discontinued, the sustained release composition comprising (a) an effective antihyperlipidemic amount of nicotinic acid, and (b) an excipient to provide sustained release of the nicotinic acid.

134. A sustained release composition of claim 133, wherein said excipient is selected from the group consisting of a swelling agent, a binder, a processing aid and mixtures thereof.

135. A sustained release composition of claim 134, wherein the swelling agent is selected from group consisting of a polymer, a wax, a natural material and mixtures thereof.

136. A sustained release composition of claim 135, wherein the polymer is selected from the group consisting of hydroxypropyl methylcellulose, sodium carboxymethylcellulose and ethylcellulose.

137. A sustained release composition of claim 135, wherein the wax is bees wax.

138. A sustained release composition of claim 135, wherein the natural material is selected from the group consisting of gums and gelatins.

139. A sustained release composition of claim 134, wherein the binder is povidone.

140. A sustained release composition of claim 134, wherein the processing aid is a lubricant.

141. A sustained release composition of claim 140, wherein the lubricant is stearic acid.

142. A sustained release composition of claim 136, wherein the hydroxypropyl methylcellulose is in an amount ranging from about 5% to about 50% parts by weight per 100 parts by weight of the sustained release composition.

143. A sustained release composition of claim 134, wherein the binder is in an amount ranging from about 1% to about 5% parts by weight per 100 parts by weight of the sustained release composition.

144. A sustained release composition of claim 134, wherein the processing aid is in an amount ranging from about 0.5% to about 2% parts by weight per 100 parts by weight of the sustained release composition.

145. A sustained release composition of claim 133, wherein the sustained release composition consists essentially of nicotinic acid, hydroxypropyl methylcellulose, povidone and stearic acid.

146. A sustained release composition of claim 133, wherein the sustained release composition consists essentially of

nicotinic acid 375.0 mg.

hydroxypropyl methylcellulose 188.7 mg.

povidone 12.9 mg. and

stearic acid 5.8 mg.

147. A sustained release composition of claim 133, wherein the sustained release composition consists essentially of

nicotinic acid 500.0 mg.

hydroxypropyl methylcellulose 203.0 mg.

povidone 17.2 mg. and

stearic acid 7.3 mg.

148. A sustained release composition of claim 134, wherein the sustained release composition consists essentially of

nicotinic acid 750.0 mg.

hydroxypropyl methylcellulose 204.7 mg.

povidone 25.9 mg. and

stearic acid 9.9 mg.
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