3,5,3'-TRIIODOTHYRONINE SULFATE AS THYROMIMETIC AGENT AND PHARMACEUTICAL FORMULATIONS THEREOF

• US 20170007563A1
• Filed: 09/21/2016
• Published: 01/12/2017
• Est. Priority Date: 11/13/2002
• Status: Active Grant

• Current Assignee: Bracco SPA
• Original Assignee: Bracco SPA
• Inventors: Cavalieri, Livio, Rivolta, Giovanni, Vella, Fulvia
• Granted Patent: US 10,238,615 B2
• Time in Patent Office: Days
• US Class Current: 1/1
• CPC Class Codes: A61K 31/197 the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid carnitine A61K31/205
• 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 31/28 Compounds containing heavy metals
• CPC Class Codes: A61K 9/0053 Mouth and digestive tract, i.e. intraoral and peroral administration rectal administration A61K9/0031
• CPC Class Codes: A61K 9/20 Pills, tablets, discs, rods A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095
• CPC Class Codes: A61K 9/2009 Inorganic compounds
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2059 Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
• CPC Class Codes: A61P 3/00 Drugs for disorders of the metabolism of the blood or the extracellular fluid A61P7/00
• CPC Class Codes: A61P 37/02 Immunomodulators
• CPC Class Codes: A61P 5/14 of the thyroid hormones, e.g. T3, T4
• CPC Class Codes: G01N 21/76 Chemiluminescence; Bioluminescence
• CPC Class Codes: G01N 33/561 Immunoelectrophoresis
• CPC Class Codes: G01N 33/78 Thyroid gland hormones , e.g. T3, T4, TBH, TBG or their receptors

Abstract

The invention regards the use of triiodothyronine sulfate, commonly named T₃S, as a medicament having thyromimetic activity for the treatment of pathologies due to organic deficiency of triiodothyronine (T₃), as such or in association with thyroxine (T₄), and pharmaceutical formulations for oral administration thereof.

Claims

1. A daily dosage thyroid hormone composition comprising T₃S as the active principle, in a quantity ranging from 1 to 1000 μ

g;

at least one diluent selected from the group consisting of;

microcrystalline cellulose, calcium carbonate, magnesium carbonate, and mixtures thereof;

at least one glidant selected from the group consisting of;

glycerol dibenhate and talc;

at least one lubricant selected from the group consisting of;

magnesium stearate, zinc stearate, and colloidal silica; and

at least one disintegrant selected from the group consisting of;

croscarmellose or salts thereof and crosovidone or salts thereof.

2. The daily dosage of claim 1 wherein T₃S is in a quantity from 2.5 to 500 μ

g.

3. The daily dosage of claim 2 comprising T₃S in a range from 5-250 μ

g.

4. The daily dosage of claim 2 further comprising from 5-800 μ

g T4 (thyroxine).

9. The daily dosage of claim 1 wherein the disintegrant is croscarmellose or salts thereof.

12. The daily dosage of claim 1 wherein the glidant is glycerol dibehenate.

13. The daily dosage of claim 1 in the form of a tablet.

15. The daily dosage of claim 13 wherein the tablet is a 80-150 mg tablet.

23. A therapeutic or prophylactic treatment method for a hypothyroid condition due to total thyroid hormone depletion before ¹³¹I radiotherapy comprising administering the daily dosage according to claim 1 to a thyroidectomised patient up to 5 days before radioactive isotope administration.

24. The therapeutic treatment method of claim 23 wherein said hypothyroid condition is selected from the group consisting of:

asthenia, fatigue, skin dryness, somnolence, speech fluency impairment, cold intolerance, weight gain and memory deficit.

25. A therapeutic treatment method for a hypothyroid condition comprising administering the daily dosage according to claim 1.

26. The therapeutic treatment method of claim 25 wherein said hypothyroid condition is selected form the group consisting of:

asthenia, fatigue, skin dryness, somnolence, speech fluency impairment, cold intolerance, weight gain and memory deficit.

28. The daily dosage according to claim 9 wherein the disintegrant is present in a quantity of from 1-10 mg/tablet.

29. The daily dosage according to claim 28, wherein the disintegrant is present in a quantity of from 2-6 mg/tablet.

5-8. -8. (canceled)

10. (canceled)

11. (canceled)

14. (canceled)

16-21. -21. (canceled)

22. (canceled)

27. (canceled)