Levothyroxine formulation with acacia

• US 9,271,951 B2
• Filed: 12/21/2012
• Issued: 03/01/2016
• Est. Priority Date: 12/21/2012
• Status: Active Grant

• Current Assignee: Mylan Incorporated (Pfizer Inc.)
• Original Assignee: Mylan Incorporated (Pfizer Inc.)
• Inventors: Kirsch, John, Nallamothu, Ramakrishna, Polat, Baris E.
• Primary Examiner(s): HOFFMAN, SUSAN COE
• Application Number:
  US13/723,485
• Publication Number:
  US 20140178511A1
• Time in Patent Office: 1,166 Days
• Field of Search: None
• US Class Current: 1/1
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/198 Alpha-amino acids, e.g. alanine or edetic acid [EDTA] betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00
• CPC Class Codes: A61K 31/235 having an aromatic ring attached to a carboxyl group
• CPC Class Codes: A61K 36/48 Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/205 Polysaccharides, e.g. alginate, gums; Cyclodextrin

Abstract

A pharmaceutical composition comprising thyroxine, acacia, and an antioxidant selected from propyl gallate, butylated hydroxyanisol, and butylated hydroxytoluene is disclosed. The pharmaceutical composition has an improved shelf life. In one embodiment, the composition additionally comprises sucrose, microcrystalline cellulose, and mannitol. The pharmaceutical composition may be used for treating thyroid disorders by orally administering the composition to a patient in need thereof.

Claims

1. A pharmaceutical composition comprising thyroxine, acacia, and about 0.001% wt % to about 0.5% wt % of an antioxidant selected from propyl gallate, butylated hydroxyanisol, and butylated hydroxytoluene, and

wherein the composition comprises from about 0.1% wt % to about 10% wt % acacia.

2. The composition of claim 1, wherein the composition comprises from about 0.25% wt % to about 2.5% wt % acacia.

3. The composition of claim 1, wherein the composition comprises from about 0.4% wt % to about 2.0% wt % acacia.

4. The composition of claim 1, wherein the composition comprises from about 0.005% wt % to about 0.5% wt % propyl gallate.

5. The composition of claim 4, wherein the composition comprises about 1% wt % to about 2% wt % acacia.

6. The composition of claim 1, wherein the composition comprises from about 0.005% wt % to about 0.5% wt % butylated hydroxyanisol.

7. The composition of claim 1, wherein the composition comprises from about 0.005% wt % to about 0.5% wt % butylated hydroxytoluene.

8. The composition of claim 1, wherein the thyroxine comprises levothyroxine sodium.

9. The composition of claim 8, wherein the composition comprises from about 0.4% wt % to about 2.0% wt % acacia and from about 0.005% wt % to about 0.5% wt % of the antioxidant.

10. The composition of claim 1, wherein the composition is a unit dosage form which comprises about 0.1 μ

g to about 5000 μ

g thyroxine.

11. The composition of claim 1, wherein the composition additionally comprises sucrose, microcrystalline cellulose, and mannitol.

12. The composition of claim 11, wherein the composition comprises from about 5% wt % to about 70% wt % sucrose, from about 5% wt % to about 90% wt % microcrystalline cellulose, and from about 5% wt % to about 90% wt % mannitol.

13. The composition of claim 12, wherein the composition is a solid oral dosage form.

14. The composition of claim 1, wherein the decrease in potency, after 6 months at the accelerated conditions of 40°

C. and 75% relative humidity, is less than 5%.

15. The composition of claim 14, wherein the decrease in potency, after 6 months at the accelerated conditions of 40°

C. and 75% relative humidity, is less than 2.5%.

16. The composition of claim 1, wherein the composition is a solid oral dosage form.

17. The composition of claim 16, wherein the composition is a tablet.

18. The composition of claim 1, wherein the composition comprises about 1.5% wt % acacia.

19. A method for treating thyroid disorders comprising orally administering the composition of claim 1 to a patient in need thereof.

20. The method of claim 19, wherein 25 to 300 μ

g of thyroxine is administered once daily.