Intermediate release nicotinic acid compositions for treating hyperlipidemia
DCFirst Claim
1. An intermediate release nicotinic acid formulation suitable for oral administration once-a-day for treating hyperlipidemia without causing drug-induced hepatotoixicity to a level which woud require use of said intermediate release nicotinic acid formulation to be discontinued, said intermediate release nicotinic acid formulation containing at least about 375 mg of nicotinic acid and having:
- a nicotinic acid Cmax of about 3 μ
g/ml;
a nicotinic acid Tmax in the range of between about 5.6 hours and about 6 bours; and
an AUC for nictoinic acid of about 6 μ
ghr/ml.
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Abstract
Intermediate release nicotinic acid formulations having unique biopharmaceutical characteristics, such as Cmax, Tmax and AUC, which are suitable for oral administration once per day during the evening or at night for treating hyperlipidemia without causing drug-induced hepatotoxicity to such a level that requires the therapy to be discontinued, are disclosed. The intermediate nicotinic acid formulations can be administered as tablets in dosage strengths of, for example, 375 mg, 500 mg, 750 mg and 1000 mg.
298 Citations
28 Claims
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1. An intermediate release nicotinic acid formulation suitable for oral administration once-a-day for treating hyperlipidemia without causing drug-induced hepatotoixicity to a level which woud require use of said intermediate release nicotinic acid formulation to be discontinued, said intermediate release nicotinic acid formulation containing at least about 375 mg of nicotinic acid and having:
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a nicotinic acid Cmax of about 3 μ
g/ml;
a nicotinic acid Tmax in the range of between about 5.6 hours and about 6 bours; and
an AUC for nictoinic acid of about 6 μ
ghr/ml.- View Dependent Claims (2)
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3. An intermediate release nicotinic acid formulation suitable for oral administration once-a-day for treating hyperlipidemia without causing drug-induced hepatotoxicity to a level which would require use of said intermediate realse nicotinic acid formulation to be discontinued, said intermediate release nicotinic acid formulation containing at least about 375 mg of nicotinic acid and having:
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a nicotinuric acid Cmax of about 2 μ
g/ml;
a nicotinuric acid Tmax in the range of between about 5.6 hours and about 6 hours; and
an AUC for nictoinuric acid of about 10 μ
ghr/ml.
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4. An intermediate release nicotinic acid formulation of clain 3, wherein said nicotinic acid formulation is a tablet.
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5. An intermediate release nicotinic acid formulation suitable for oral administration once-a-day for treating hyperlipidemia without causing drug-induced hepatotoxicity to a level which would require use of said intermediate release nicotinc acid fomlation to be discontinued, said intermediate release nicotinic acid formulation containing at least about 500 mg of nicotinic acid and having:
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a nicotinic acid Cmax in the range of from between about 1 μ
g/ml and 10 μ
g/ml;
a nicotinic acid Tmax in the range of between about 5.6 hours and about 6 hours; and
an AUC for nictoinic acid in the range of from between about 2 μ
ghr/ml and about 34 μ
ghr/ml.- View Dependent Claims (6, 7, 8)
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9. An intermediate release nicotinic acid formulation suitable for oral admministration once-a-day for treating hyperlipidemia without causing drug-induced hepatotoxicity to a level which would require use of said intermediate release nicotinic acid formulation to be discontinued, said intermediate release nicotinic acid formulation containig at least about 500 mg of nicotinic acid and having:
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a nicotinuric acid Cmax in the range of from between about 2 μ
g/ml and 3 μ
g/ml;
a nicotinuric acid Tmax in the range of beween about 5.6 hours and about 6 hours; and
an AUC for nicotinuric acid in the range of from between about 6 μ
ghr/ml and about 16 μ
ghr/ml.- View Dependent Claims (10, 11, 12)
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13. An intermediate release nicotinic acid formulation suitable for oral asministration once-a-day for treating hyperlipidemia without causing drug-induced hepatotoxcity to a level which would require use of said intermediate release nicotinic acid formlation to be discontinued, said intermediate release nicotinic acid formulation containing at least about 750 mg of nicotinic acid and having:
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a nicotinic acid Cmax in the range of from between about 8 μ
g/ml and 9 μ
g/ml;
a nicotinic acid Tmax in the range of between about 5.6 hours and about 6 hours; and
an AUC for nictoinic acid in the range of from between about 21 μ
ghr/ml and about 22 μ
ghr/ml.- View Dependent Claims (14, 15, 16)
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17. An intermediate release nicotinic acid formulation suitable for oral administration once-a-day for treating hyperlipidemia without causing drug-induced hepatotoxicity to a level which would require use of said intermediate release nicotinic acid formulation to be discontinued, said intermediate release nicotinic acid formulation containing at least about 750 mg of nicotinic acid and having:
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a nicotinuric acid Cmax in the range of from between about 3 μ
g/ml and 3.2 μ
g/ml;
a nicotinuric acid Tmax in the range of between about 5.6 hours and about 6 hours; and
an AUC for nicotinuric acid in the range of from between about 11 μ
ghr/ml and about 13 μ
ghr/ml.- View Dependent Claims (18, 19, 20)
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21. An intermediate release nicotrinic acid formulation suitable for oral administration once-a-day for treating hyperlipidemia without causing drug-induced hepatotoxicity to a level which would require use of said intermediate release nicotinic acid formulation to be discontinued, said intermediate release nicotinic acid formulation containg at least about 100 mg of nicoinic acid and having:
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a nicotinic acid Cmax in the range of from between about 9 μ
g/ml and 17 μ
g/ml;
a nicotinic acid Tmax in the range of between about 5.6 hours and bout 6 hours; and
an AUC for nictoinic acid in the range of from between about 24 μ
ghr/ml and about 43 μ
ghr/ml.- View Dependent Claims (22, 23, 24)
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25. An intermediate release nicotinic acid formulation suitable for oral administration once-a-day for treating hyperlipidemia without causing drug-induced hepatotoxicity to a level which would require use of said intermediate release nicotinic acid formulation to be discontinued, said intermediate release nicotinic acid formulation containing at least about 1000 mg of nicotinic acid and having:
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a nicotinuric acid Cmax in the range of from between about 3 μ
g/ml and 5 μ
g/ml;
a nicotinuric acid Tmax in the range of between about 5.6 hours and about 6 hours; and
an AUC for niotinuric acid in the range of from between about 12 μ
ghr/ml and about 19 μ
ghr/ml.- View Dependent Claims (26, 27, 28)
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Specification