SUSTAINED RELEASE

• US 20100136109A1
• Filed: 04/22/2008
• Published: 06/03/2010
• Est. Priority Date: 04/23/2007
• Status: Abandoned Application

• Current Assignee: Hiep Huatan, Richard Ross
• Original Assignee: Hiep Huatan, Richard Ross
• Inventors: Huatan, Hiep, Ross, Richard
• Application Number:
  US12/597,153
• Publication Number:
  US 20100136109A1
• Time in Patent Office: Days
• US Class Current: 424/457
• 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 9/143 with inorganic compounds
• CPC Class Codes: A61K 9/145 with organic compounds
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61P 5/14 of the thyroid hormones, e.g. T3, T4

Abstract

We describe a medicament for the treatment of thyroid disorders that typically result from a hypoactive thyroid gland that releases thyroxine and triiodothyronine in a sustained pattern when administered to a subject.

Claims

1. A medicament comprising a pharmaceutically effective amount of thyroxine and triiodothyronine and a means to release both thyroxine and triiodothyronine in a sustained release pattern when administered to a subject.

2. The medicament according to claim 1, wherein the medicament comprises at least 100 μ

g of thyroxine.

3. The medicament according to claim 1, wherein the medicament comprises at least 6 μ

g triiodothyronine.

4. The medicament according to claim 1, wherein the medicament comprises thyroxine at about 25 to 200 μ

g per unit dose.

5. The medicament according to claim 1, wherein the medicament comprises triiodothyronine at about 1 to 20 μ

g per unit dose.

6. The medicament according to claim 1, wherein the medicament comprises thyroxine at about 100 μ

g and triiodothyronine at about 6 μ

g per unit dose.

7. The medicament according to claim 1, wherein said medicament comprises polymers that facilitate the release of thyroxine and triiodothyronine in a sustained pattern.

8. The medicament according to claim 7, wherein said polymers are hydrophilic polymers.

9. The medicament according to claim 8, wherein said hydrophilic polymers are cellulose based.

10. The medicament according to claim 9, wherein said hydrophilic polymers are selected from the group consisting of:

hydroxypropylmethylcellulose, hydroxypropyl cellulose, methyl cellulose, sodium carboxymethylcellulose poly(ethylene)oxide, polymethyacrylates, and polyvinyl alcohol.

11. The medicament according to claim 10, wherein said hydrophilic polymer is hydroxypropylmethylcellulose.

12. The medicament according to claim 10, wherein said hydrophilic polymer is polymethyl methacrylate.

13. The medicament according to claim 7, wherein said polymer is non-hydrophilic.

14. The medicament according to claim 13, wherein said non hydrophilic polymer is selected from the group consisting of a water insoluble ethyl derivative, microcrystalline cellulose, and dicalcium phosphate.

15. The medicament according to claim 7, wherein said medicament is a multiparticulate formulation.

16. The medicament according to claim 15, wherein said multiparticulate formulation comprises polyvinylpyrrolidone.

17. The medicament according to claim 16, wherein said multiparticulate formulation comprises polyvinylpyrrolidone and microcrystalline cellulose.

18. The medicament according to claim 16, wherein said multiparticulate formulation comprises polyvinylpyrrolidone and dicalcium phosphate.

19. The medicament according to claim 16, wherein said multiparticulate formulation comprises polyvinylpyrrolidone and lactose.

20. The medicament according to claim 16, wherein said multiparticulate formulation comprises polyvinylpyrrolidone and at least one or all of the following:

microcrystalline cellulose, dicalcium phosphate, or lactose.

21. The medicament according to claim 15, wherein said multiparticulate formulation comprises thyroxine and triiodothyronine combined in individual multiparticulate units within a capsule dosage form.

22. The medicament according to claim 15, wherein said multiparticulate formulation comprises thyroxine and triiodothyronine in separate multiparticulate units combined together within a capsule dosage form.

23. The medicament according to claim 16, wherein the medicament comprises polyvinylpyrrolidone at between 0.5% w/w and 5% w/w.

24. The medicament according to claim 23, wherein polyvinylpyrrolidone is provided between 1-3% w/w.

25. The medicament according to claim 24, wherein polyvinylpyrrolidone is provided at about 1% w/w.

26-45. -45. (canceled)

46. A method for the treatment of hypothyroidism comprising administering to a subject a medicament comprising an effective amount of a combined preparation of thyroxine and triiodothyronine wherein both thyroxine and triiodothyronine are released in a sustained pattern when administered to the subject.

47. The method according to claim 46, wherein said medicament is administered to the subject between 18:

00 h and 00;

00 h.

48. The method according to claim 46, wherein administering the medicament comprises the use of an administration pattern that reproduces a circadian rhythm of Ft3 in said subject.

49. The method according to claim 46, wherein administering the medicament comprises the use of an administration pattern that reproduces a constant concentration of Ft4 in said subject.