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Claims for Patent: 6,555,581

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Claims for Patent: 6,555,581

Title: Levothyroxine compositions and methods
Abstract:The present invention generally relates to stable pharmaceutical compositions, and methods of making and administering such compositions. In one aspect, the invention features stabilized pharmaceutical compositions that include pharmaceutically active ingredients such as levothyroxine (T4) sodium and liothyronine (T3) sodium (thyroid hormone drugs), preferably in an immediate release solid dosage form. Also provided are methods for making and using such immediate release and stabilized compositions.
Inventor(s): Franz; G. Andrew (St. Louis, MO), Strauss; Elaine A. (Seminole, FL), DiMenna; Philip A. (St. Petersburg, FL), Gemma; Rocco L. (Dover, OH)
Assignee: Jones Pharma, Inc. (St. Petersburg, FL)
Application Number:10/077,677
Patent Claims: 1. A stable, solid, immediate release pharmaceutical composition for oral administration to treat a thyroid disorder, said composition comprising: (a) about 0.00005 wt % to about 5 wt % of a levothyroxine salt; (b) at least about 50 wt % of a .beta.-form microcrystalline cellulose particles, said .beta.-form microcrystalline cellulose particles having generally flat needle-shapes, a bulk density in a range of from about 0.10 g/cm.sup.3 to about 0.23 g/cm.sup.3, and a conductivity of less than about 200 .mu.S/cm; and (c) about 0.5 wt % to about 30 wt % disintegrating agent;

wherein (1) at least about 90 wt % of the levothyroxine salt in the composition dissolves in an aqueous solution in less than about 5 minutes, (2) potency loss for said levothyroxine salt is no more than about 0.3% per month for a period of at least about 18 months, and (3) said composition is essentially sugar-free.

2. A stable, solid, immediate release pharmaceutical composition of claim 1, wherein at least about 90 wt % of the levothyroxine salt in the composition dissolves in an aqueous solution in less than about 2.5 minutes.

3. A stable, solid, immediate release pharmaceutical composition of claim 1, wherein said pharmaceutical composition exhibits a levothyroxine (T4) plasma Cmax of from between about 10 .mu.g/dL to about 20 .mu.g/dL.

4. A stable, solid, immediate release pharmaceutical composition of claim 1, wherein said pharmaceutical composition exhibits a levothyroxine (T4) plasma Cmax of from between about 12 .mu.g/dL to about 16 .mu.g/dL.

5. A stable, solid, immediate release pharmaceutical composition of claim 1, wherein said pharmaceutical composition exhibits a triiodothyronine (T3) plasma Cmax of from between about 0.1 ng/mL to about 10 ng/mL.

6. A stable, solid, immediate release pharmaceutical composition of claim 1, wherein said pharmaceutical composition exhibits a triiodothyronine (T3) plasma Cmax of from between about 0.5 ng/mL to about 2 ng/mL.

7. A stable, solid, immediate release pharmaceutical composition of claim 1, wherein said pharmaceutical composition exhibits a levothyroxine (T4) plasma Tmax of from between about 1 hours to about 3 hours.

8. A stable, solid, immediate release pharmaceutical composition of claim 1, wherein said pharmaceutical composition exhibits a triiodothyronine (T3) plasma Tmax of from between about 12 hours to about 16 hours.

9. A stable, solid, immediate release pharmaceutical composition of claim 1, wherein said pharmaceutical composition exhibits a levothyroxine (T4) AUC(0-t) of between from about 500 .mu.g-hour/dL to about 550 .mu.g-hour/dL.

10. A stable, solid, immediate release pharmaceutical composition of claim 1, wherein said pharmaceutical composition exhibits a triiodothyronine (T3) AUC(0-t) of between from about 20 ng-hour/mL to about 60 ng-hour/mL.

11. A stable, solid, immediate release pharmaceutical composition of claim 1, wherein said pharmaceutical composition is a non-granular composition.

12. A stable, solid, immediate release pharmaceutical composition of claim 1, wherein said .beta.-form microcrystalline cellulose particles have a bulk density in a range of from about 0.17 g/cm.sup.3 to about 0.23 g/cm.sup.3.

13. A stable, solid, immediate release pharmaceutical composition of claim 1, wherein said pharmaceutical composition is formulated as a tablet.

14. A stable, solid, immediate release pharmaceutical composition of claim 13, wherein said tablet has a total hardness of from between about 5 KP to about 15 KP.

15. A stable, solid, immediate release pharmaceutical composition of claim 13, wherein said tablet has a surface area of from between about 0.9 in..sup.2 to about 15 in..sup.2.

16. A stable, solid, immediate release pharmaceutical composition of claim 13, wherein said tablet is beveled.

17. A stable, solid, immediate release pharmaceutical composition of claim 13, wherein said tablet is scored.

18. A stable, solid, immediate release pharmaceutical composition of claim 13, wherein said tablet has a raised violin configuration.

19. A stable, solid, immediate release pharmaceutical composition of claim 1, wherein said pharmaceutical composition includes less than about 10% total impurities.

20. A stable, solid, immediate release pharmaceutical composition of claim 1, wherein said pharmaceutical composition includes less than about 5% total impurities.

21. A stable, solid, immediate release pharmaceutical composition of claim 1, wherein said disintegrant is a croscarmellose salt.

22. A stable, solid, immediate release pharmaceutical composition of claim 1, wherein said pharmaceutical composition further includes at least one pharmaceutically acceptable coloring agent.

23. A stable, solid, immediate release pharmaceutical tablet for oral consumption comprising: (a) between from about 0.01 mg to about 0.8 mg levothyroxine sodium; (b) between from about 100 mg to about 110 mg of .beta.-microcrystalline cellulose particles, said .beta.-form microcrystalline cellulose particles having generally flat needle-shapes, a bulk density in a range of from about 0.10 g/cm.sup.3 to about 0.23 g/cm.sup.3, and a conductivity of less than about 200 .mu.S/cm; (c) between from about 25 mg to about 50 mg of croscarmellose sodium; and (d) between from about 0.5 mg to about 5 mg of magnesium stearate,

wherein (1) at least about 90 wt % of the levothyroxine salt in the composition dissolves in an aqueous solution in less than about 5 minutes, (2) potency loss for said levothyroxine salt is no more than about 0.3% per month for a period of at least about 18 months, and (3) said composition is essentially sugar-free.

24. A stable, solid, immediate release pharmaceutical tablet of claim 23, wherein said tablet further includes at least one pharmaceutically acceptable coloring agent.

25. A stable, solid, immediate release pharmaceutical composition for oral administration to treat a thyroid disorder, said composition comprising: (a) about 0.00005 wt % to about 5 wt % of a levothyroxine salt; (b) at least about 50 wt % of a .beta.-form microcrystalline cellulose particles, said .beta.-form microcrystalline cellulose particles having generally flat needle-shapes, a bulk density in a range of from about 0.10 g/cm.sup.3 to about 0.23 g/cm.sup.3, and a conductivity of less than about 200 .mu.S/cm; and (c) about 0.5 wt % to about 30 wt % disintegrating agent;

wherein (1) at least about 90 wt % of the levothyroxine salt in the composition dissolves in an aqueous solution in less than about 5 minutes, (2) potency loss on average for said levothyroxine salt is no more than about 0.2% per month for a period of at least about 18 months, and (3) said composition is essentially sugar-free.
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