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Claims for Patent: 6,406,715

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Claims for Patent: 6,406,715

Title: Intermediate release nicotinic acid compositions for treating hyperlipidemia having unique urinary metabolite profiles
Abstract:Intermediate release nicotinic acid formulations having unique urinary metabolite profiles, which are suitable for oral administration once-a-day as a single dose during a 24 hour period for treating hyperlipidemia without causing drug-induced hepatotoxicity or drug-induced elevations in uric acid or glucose or both to levels that require the therapy to be discontinued, are disclosed.
Inventor(s): Cefali; Eugenio A. (Lauderhill, FL)
Assignee: Kos Pharmaceuticals, Inc. (Miami, FL)
Application Number:08/962,423
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 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

nicotinic acid and a swelling agent, said intermediate release nicotinic acid formulation having an in vitro urinary metabolite profile resulting from the absorption of the nicotinic acid released from the intermediate release formulation following the oral administration of the nicotinic acid formulation to an individual when the nicotinic acid formulation is dosed at about 1000 mg

(a) nicotinic acid and nicotinic acid present in the urine in an amount of from about 4.0% to about 26%, and

(b) Pathway 2 metabolites present in the urine in an amount of from about 74% to about 95%.

2. An intermediate release nicotinic acid formulation of claim 1, wherein the in vivo urinary metabolite profile is based upon a mean which is as follows:

(a) nicotinic acid and nicotinic acid present in the urine in an amount of about 12%;

(b) Pathway 2 metabolites present in the urine in an amount of about 88%.

3. An intermediate release nicotinic acid formulation of claim 1, wherein said nicotinic acid formulation is administered as two tablets wherein each tablet contains about 500 mg of nicotinic acid.

4. An intermediate release nicotinic acid formulation of claim 2, wherein said nicotinic acid formulation is administered as two tablets wherein each tablet contains about 500 mg of nicotinic acid.

5. An immediate release nicotinic acid formulation suitable for oral administration once-a-day as a single dose 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 comprising

nicotinic acid and a swelling agent, said intermediate release nicotinic acid formulation having an in vivo urinary metabolite profile resulting from the absorption of the nicotinic acid released from the intermediate release formulation following the oral administration of the nicotinic acid formulation to an individual when the nicotinic acid formulation is dosed at about 1500 mg

(a) nicotinic acid and nicotinic acid present in the urine in an amount of from about 11.0% to about 45%, and

(b) Pathway 2 metabolites present in the urine in an amount of from about 55% to about 89%.

6. An intermediate release nicotinic acid formulation of claim 5, wherein the in vivo urinary metabolite profile is based upon a mean which is as follows:

(a) nicotinic acid and nicotinic acid present in the urine in an amount of about 21%;

(b) Pathway 2 metabolites present in the urine in an amount of about 79%.

7. An intermediate release nicotinic acid formulation of claim 5, wherein said nicotinic acid formulation is administered as two tablets wherein each tablet contains about 750 mg of nicotinic acid.

8. An intermediate release nicotinic acid formulation of claim 6, wherein said nicotinic acid formulation is administered as two tablets wherein each tablet contains about 750 mg of nicotinic acid.

9. 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

nicotinic acid and a swelling agent, said intermediate release nicotinic acid formulation having an in vitro urinary metabolite profile resulting from the absorption of the nicotinic acid released from the intermediate release formulation following the oral administration of the nicotinic acid formulation to an individual when the nicotinic acid formulation is dosed at about 2000 mg

(a) nicotinic acid and nicotinic acid present in the urine in an amount of from about 22% to about 48%, and

(b) Pathway 2 metabolites present in the urine in an amount of from about 52% to about 78%.

10. An intermediate release nicotinic acid formulation of claim 9, wherein the in vivo urinary metabolite profile is based upon a mean which is as follows:

(a) nicotinic acid and nicotinic acid present in the urine in an amount of about 32%;

(b) Pathway 2 metabolites present in the urine in an amount of about 68%.

11. An intermediate release nicotinic acid formulation of claim 9, wherein said nicotinic acid formulation is administered as two tablets wherein each tablet contains about 1000 mg of nicotinic acid.

12. An intermediate release nicotinic acid formulation of claim 10, wherein said nicotinic acid formulation is administered as two tablets wherein each tablet contains about 1000 mg of nicotinic acid.

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

nicotinic acid and a swelling agent, said intermediate release nicotinic acid formulation having an in vitro urinary metabolite profile resulting from the absorption of the nicotinic acid released from the intermediate release formulation following the oral administration of the nicotinic acid formulation to an individual when the nicotinic acid formulation is dosed at about 2500 mg

(a) nicotinic acid and nicotinic acid present in the urine in an amount of from about 25% to about 66%, and

(b) Pathway 2 metabolites present in the urine in an amount of from about 34% to about 75%.

14. An intermediate release nicotinic acid formulation of claim 13, wherein the in vivo urinary metabolite profile is based upon a mean which is as follows:

(a) nicotinic acid and nicotinic acid present in the urine in an amount of about 42%;

(b) Pathway 2 metabolites present in the urine in an amount of about 58%.

15. An intermediate release nicotinic acid formulation of claim 13, wherein said nicotinic acid formulation is administered as three tablets wherein each tablet contains about 1000 mg of nicotinic acid.

16. An intermediate release nicotinic acid formulation of claim 14, wherein said nicotinic acid formulation is administered as three tablets wherein each tablet contains about 1000 mg of nicotinic acid.
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