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Claims for Patent: 6,746,691

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Claims for Patent: 6,746,691

Title: Intermediate release nicotinic acid compositions for treating hyperlipidemia having unique biopharmaceutical characteristics
Abstract:Intermediate release nicotinic acid formulations having unique biopharmaceutical characteristics, which are suitable for oral administration once per day as a single dose preferably administered 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. The 375 mg, 500 mg and 750 mg nicotinic acid tablets of the present invention have a dissolution curve similarity fit factor F.sub.2 of at least about 79, and the 1000 mg nicotinic acid tablets of the present invention have a dissolution curve similarity fit factor F.sub.2 of at least 44.
Inventor(s): Cefali; Eugenio A. (Lauderhill, FL)
Assignee: Kos Pharmaceuticals, Inc. (Miami, FL)
Application Number:08/962,424
Patent Claims: 1. An intermediate release nicotinic acid formulation suitable for oral administration once-a-day as a single dose for treating hyperlipidemia without causing drug-induced (i) hepatotoxicity and (ii) elevations in uric acid or glucose or both, to levels which would require use of said intermediate release nicotinic acid formulation to be discontinued, said intermediate release nicotinic acid formulation comprising a dissolution curve similarity fit factor F.sub.2 of at least about 79; and an in vitro dissolution profile, when measured in a type I dissolution apparatus (basket), according to U.S. Pharmacopeia XXII, at about 37.degree. C. in deionized water at about 100 rpm, as follows: (a) less than about 15% of the nicotinic acid is released after about 1 hour in the 1510 apparatus, (b) between about 15% and about 30% of the nicotinic acid is released after about 3 hours in the 1510 apparatus, (c) between about 30% and about 45% of the nicotinic acid is released after about 6 hours in the 1510 apparatus, (d) between about 40% and about 60% of the nicotinic acid is released after about 9 hours in the 1510 apparatus, (e) between about 50% and about 75% of the nicotinic acid is released after about 12 hours in the 1510 apparatus, and (f) at least about 75% is released after about 20 hours in the 1510 apparatus.

2. An intermediate release nicotinic acid formulation of claim 1, wherein approximately 100% of the nicotinic acid is released after about 20 hours in the apparatus.

3. An intermediate release nicotinic acid formulation of claim 1, wherein said nicotinic acid formulation is a tablet.

4. An intermediate release nicotinic acid formulation of claim 3, wherein said tablet contains nicotinic acid in an amount selected from the group consisting of about 375 mg, about 500 mg and about 750 mg.

5. An intermediate release nicotinic acid formulation of claim 1, wherein said in vitro dissolution profile is as follows: (a) between about 9.6% and about 13.8% of the nicotinic acid is released after about 1 hour in the apparatus; (b) between about 21.2% and about 27.8% of the nicotinic acid is released after about 3 hours in the apparatus; (c) between about 35.1% and about 44.2% of the nicotinic acid is released after about 6 hours in the apparatus; (d) between about 45.6% and about 58.5% of the nicotinic acid is released after about 9 hours in the apparatus; (e) between about 56.2% and about 72% of the nicotinic acid is released after about 12 hours in the apparatus; and (f) at least about 75% is released after about 20 hours in the apparatus.

6. An intermediate release nicotinic acid formulation of claim 5, wherein approximately 100% of the nicotinic acid is released after about 20 hours in the apparatus.

7. An intermediate release nicotinic acid formulation of claim 5, wherein said nicotinic acid formulation is a tablet.

8. An intermediate release nicotinic acid formulation of claim 7, wherein said tablet contains nicotinic acid in an amount selected from the group consisting of about 375 mg, about 500 mg and about 750 mg.

9. An intermediate release nicotinic acid formulation of claim 1, wherein said in vitro dissolution profile is as follows: (a) between about 9.6% and about 13.8% of the nicotinic acid is released after about 1 hour in the apparatus; (b) between about 21.2% and about 27.8% of the nicotinic acid is released after about 3 hours in the apparatus; (c) between about 35.1% and about 44.2% of the nicotinic acid is released after about 6 hours in the apparatus; (d) between about 45.6% and about 58.5% of the nicotinic acid is released after about 9 hours in the apparatus; (e) between about 56.2% and about 72% of the nicotinic acid is released after about 12 hours in the apparatus; and (f) at least about 75% is released after about 20 hours in the apparatus.

10. An intermediate release nicotinic acid formulation of claim 9, wherein approximately 100% of the nicotinic acid is released after about 20 hours in the apparatus.

11. An intermediate release nicotinic acid formulation of claim 9, wherein said nicotinic acid formulation is a tablet.

12. An intermediate release nicotinic acid formulation of claim 11, wherein said tablet contains nicotinic acid in an amount selected from the group consisting of about 375 mg, about 500 mg and about 750 mg.

13. An intermediate release nicotinic acid formulation suitable for oral administration once-a-day as a single dose for treating hyperlipidemia without causing drug-induced (i) hepatotoxicity and (ii) elevations in uric acid or glucose or both, to levels which would require use of said intermediate release nicotinic acid formulation to be discontinued, said intermediate release nicotinic acid formulation comprising a dissolution curve similarity fit factor F.sub.2 of at least about 44; and an in vitro dissolution profile, when measured in a type I dissolution apparatus (basket), according to U.S. Pharmacopeia XXII, at about 37.degree. C. in deionized water at about 100 rpm, as follows: (a) less than about 15% of the nicotinic acid is released after about 1 hour in the 1510 apparatus, (b) between about 15% and about 30% of the nicotinic acid is released after about 3 hours in the 1510 apparatus, (c) between about 30% and about 45% of the nicotinic acid is released after about 6 hours in the 1510 apparatus, (d) between about 40% and about 60% of the nicotinic acid is released after about 9 hours in the 1510 apparatus, (e) between about 50% and about 75% of the nicotinic acid is released after about 12 hours in the 1510 apparatus, and (f) at least about 75% is released after about 20 hours in the 1510 apparatus.

14. An intermediate release nicotinic acid formulation of claim 13, wherein approximately 100% of the nicotinic acid is released after about 20 hours in the apparatus.

15. An intermediate release nicotinic acid formulation of claim 13, wherein said nicotinic acid formulation is a tablet.

16. An intermediate release nicotinic acid formulation of claim 13, wherein said in vitro dissolution profile is as follows: (a) between about 9.6% and about 13.8% of the nicotinic acid is released after about 1 hour in the apparatus; (b) between about 21.2% and about 27.8% of the nicotinic acid is released after about 3 hours in the apparatus; (c) between about 35.1% and about 44.2% of the nicotinic acid is released after about 6 hours in the apparatus; (d) between about 45.6% and about 58.5% of the nicotinic acid is released after about 9 hours in the apparatus; (e) between about 56.2% and about 72% of the nicotinic acid is released after about 12 hours in the apparatus; and (f) at least about 75% is released after about 20 hours in the apparatus.

17. An intermediate release nicotinic acid formulation of claim 16, wherein approximately 100% of the nicotinic acid is released after about 20 hours in the apparatus.

18. An intermediate release nicotinic acid formulation of claim 16, wherein said nicotinic acid formulation is a tablet.

19. An intermediate release nicotinic acid formulation of claim 1, wherein said in vitro dissolution profile is as follows: (a) between about 9.6% and about 13.8% of the nicotinic acid is released after about 1 hour in the apparatus; (b) between about 21.2% and about 27.8% of the nicotinic acid is released after about 3 hours in the apparatus; (c) between about 35.1% and about 44.2% of the nicotinic acid is released after about 6 hours in the apparatus; (d) between about 45.6% and about 58.5% of the nicotinic acid is released after about 9 hours in the apparatus; (e) between about 56.2% and about 72% of the nicotinic acid is released after about 12 hours in the apparatus; and (f) at least about 75% is released after about 20 hours in the apparatus.

20. An intermediate release nicotinic acid formulation of claim 19, wherein approximately 100% of the nicotinic acid is released after about 20 hours in the apparatus.

21. An intermediate release nicotinic acid formulation of claim 19, wherein said nicotinic acid formulation is a tablet.
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