Levothyroxine Formulations

US 20130053445A1
Filed: 08/29/2012
Published: 02/28/2013
Est. Priority Date: 08/30/2011
Status: Active Grant

First Claim

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1. A composition, comprising:

from 100 to 500 micrograms of levothyroxine sodium, andfrom 1 to 5 milligrams mannitol;

where the composition is a solid.

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Abstract

A levothyroxine composition includes levothyroxine sodium and mannitol. The composition is a solid. The composition may include from 100 to 500 micrograms levothyroxine sodium and from 1 to 5 milligrams mannitol. The composition may include from 100 to 200 micrograms levothyroxine sodium, and the mass ratio of mannitol to levothyroxine sodium in the composition may be at most 40:1. The composition may include about 500 micrograms levothyroxine sodium, and the mass ratio of mannitol to levothyroxine sodium in the composition may be at most 10:1.

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30 Claims

1. A composition, comprising:
- from 100 to 500 micrograms of levothyroxine sodium, andfrom 1 to 5 milligrams mannitol;
  
  where the composition is a solid.
- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10)
- - 2. The composition of claim 1, where the amount of mannitol is from 2 to 4 milligrams.
  - 3. The composition of claim 1, where the amount of mannitol is from 2.9 to 3.1 milligrams.
  - 4. The composition of claim 1, further comprising a phosphate buffer.
  - 5. The composition of claim 4, further comprising a base;
    - where, when the composition is reconstituted in 5 milliliters of 0.9% aqueous sodium chloride, the pH of the reconstituted liquid is from 9.5 to 11.5.
  - 6. The composition of claim 5, where the amount of mannitol is from 2.9 to 3.1 milligrams.
  - 7. The composition of claim 5, where the composition is formed byforming a liquid mixture by combiningthe levothyroxine sodium,the mannitol,dibasic sodium phosphate,a solvent comprising water, anda base;
    - andlyophilizing the liquid mixture.
  - 8. The composition of claim 7, where the amount of dibasic sodium phosphate in the liquid mixture is from 400 to 600 micrograms.
  - 9. The composition of claim 1, where when the composition is stored at 25°
    - C., at most 0.20% of the levothyroxine sodium is converted to liothyronine over a period of 12 months.
  - 10. The composition of claim 1, where when the composition is stored at 40°
    - C., at most 0.20% of the levothyroxine sodium is converted to liothyronine over a period of 3 months.

11. A composition, comprising:
- from 100 to 200 micrograms of levothyroxine sodium, andmannitol;
  
  where the mass ratio of mannitol to levothyroxine sodium is at most 40;
  
  1, andthe composition is a solid.
- View Dependent Claims (12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23)
- - 12. The composition of claim 11, where the amount of levothyroxine sodium is about 100 micrograms.
  - 13. The composition of claim 12, where the mass ratio of mannitol to levothyroxine sodium is at most 30:
    - 1.
  - 14. The composition of claim 13, further comprising a phosphate buffer.
  - 15. The composition of claim 14, where the composition is formed byforming a liquid mixture by combiningthe levothyroxine sodium,the mannitol,dibasic sodium phosphate, anda solvent comprising water;
    - andlyophilizing the liquid mixture.
  - 16. The composition of claim 15, where the amount of dibasic sodium phosphate in the liquid mixture is from 400 to 600 micrograms.
  - 17. The composition of claim 11, where the amount of levothyroxine sodium is about 200 micrograms.
  - 18. The composition of claim 17, where the mass ratio of mannitol to levothyroxine sodium is at most 15:
    - 1.
  - 19. The composition of claim 18, further comprising a phosphate buffer.
  - 20. The composition of claim 19, where the composition is formed byforming a liquid mixture by combiningthe levothyroxine sodium,the mannitol,dibasic sodium phosphate, anda solvent comprising water;
    - andlyophilizing the liquid mixture.
  - 21. The composition of claim 20, where the amount of dibasic sodium phosphate in the liquid mixture is from 400 to 600 micrograms.
  - 22. The composition of claim 11, where when the composition is stored at 25°
    - C., at most 0.20% of the levothyroxine sodium is converted to liothyronine over a period of 12 months.
  - 23. The composition of claim 11, where when the composition is stored at 40°
    - C., at most 0.20% of the levothyroxine sodium is converted to liothyronine over a period of 3 months.

24. A composition, comprising:
- about 500 micrograms of levothyroxine sodium, andmannitol;
  
  where the mass ratio of mannitol to levothyroxine sodium is at most 10;
  
  1, andthe composition is a solid.
- View Dependent Claims (25, 26, 27, 28, 29, 30)
- - 25. The composition of claim 24, where the mass ratio of mannitol to levothyroxine sodium is at most 6:
    - 1.
  - 26. The composition of claim 25, further comprising a phosphate buffer;
  - 27. The composition of claim 26, where the composition is formed byforming a liquid mixture by combiningthe levothyroxine sodium,the mannitol,dibasic sodium phosphate, anda solvent comprising water;
    - andlyophilizing the liquid mixture.
  - 28. The composition of claim 27, where the amount of dibasic sodium phosphate in the liquid mixture is from 400 to 600 micrograms dibasic sodium phosphate.
  - 29. The composition of claim 24, where when the composition is stored at 25°
    - C., at most 0.15% of the levothyroxine sodium is converted to liothyronine over a period of 12 months.
  - 30. The composition of claim 24, where when the composition is stored at 40°
    - C., at most 0.15% of the levothyroxine sodium is converted to liothyronine over a period of 3 months.

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Current Assignee
Fresenius KABI USA LLC (Fresenius SE & Co. KGaA)
Original Assignee
Fresenius KABI USA LLC (Fresenius SE & Co. KGaA)
Inventors
Usayapant, Arunya, Jiang, Zhi-Qiang, Monen, George

Granted Patent

US 9,006,289 B2
Time in Patent Office

Days
Field of Search
US Class Current

514/567
CPC Class Codes

A61K 31/197   the amino and the carboxyl ...

A61K 31/198   Alpha-amino acids, e.g. ala...

A61K 47/02   Inorganic compounds

A61K 47/10   Alcohols; Phenols; Salts th...

A61K 47/26   Carbohydrates, e.g. sugar a...

A61K 9/0019   Injectable compositions; In...

A61K 9/19   lyophilised , i.e. freeze-d...

Levothyroxine Formulations

First Claim

1 Assignment

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Abstract

8 Citations

30 Claims

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Levothyroxine Formulations

First Claim

1 Assignment

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0 Petitions

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Accused Products

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Abstract

8 Citations

30 Claims

Specification

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Solutions

Use Cases

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