Pharmaceutical formulations for thyroid hormones

• US 7,723,390 B2
• Filed: 07/02/2002
• Issued: 05/25/2010
• Est. Priority Date: 07/02/2001
• Status: Expired due to Term

• Current Assignee: Altergon SA
• Original Assignee: Altergon SA
• Inventors: Di Martino, Alessandro, Mateo Echanagorria, Angel, Garavani, Alberto, Marchiorri, Maurizio
• Primary Examiner(s): Wax; Robert A
• Assistant Examiner(s): Sasan; Aradhana
• Application Number:
  US10/188,467
• Publication Number:
  US 20030050344A1
• Time in Patent Office: 2,884 Days
• Field of Search: 424/451, 424/464, 424/456, 424/463, 424/452, 514/567
• US Class Current: 514/567
• 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 38/24 Follicle-stimulating hormone [FSH]; Chorionic gonadotropins, e.g. HCG; Luteinising hormone [LH]; Thyroid-stimulating hormone [TSH]
• CPC Class Codes: A61K 9/1611 Inorganic compounds
• CPC Class Codes: A61K 9/1623 Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
• CPC Class Codes: A61K 9/1652 Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin homeopathic globules A61K9/1623
• CPC Class Codes: A61K 9/485 Inorganic compounds
• CPC Class Codes: A61K 9/4858 Organic compounds
• CPC Class Codes: A61K 9/4866 Organic macromolecular compounds
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 25/22 Anxiolytics
• 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 3/04 Anorexiants; Antiobesity agents
• CPC Class Codes: A61P 5/14 of the thyroid hormones, e.g. T3, T4

Abstract

The present invention provides for pharmaceutical formulations based on thyroid hormones enabling a safe and stable oral administration in the framework of the strict therapeutic index prescribed in case of thyroid disorders.

Claims

1. A pharmaceutical composition comprising thyroid hormones or their sodium salts in the form of either:

a) a soft elastic capsule consisting of a shell of gelatin material containing a liquid or half-liquid inner phase comprising said thyroid hormones or their salts in a range between 0.001 and 1% by weight of said inner phase, dissolved in gelatin and/or glycerol, and optionally ethanol, said liquid or half-liquid inner phase being in direct contact with said shell without any interposed layers, or

b) a swallowable uniform soft-gel matrix comprising glycerol and said thyroid hormones or their salts in a range between 0.001 and 1% by weight of said matrix.

2. The composition according to claim 1, wherein said thyroid hormones are selected from the group consisting of T3, T4 and their sodium salts.

3. The composition according to claim 1, wherein said swallowable uniform soft-gel matrix further comprises gelatin of A type or B type.

4. The composition according to claim 1, wherein said liquid or half-liquid inner phase of said soft elastic capsules comprises a vehicle consisting of ethanol, glycerol or mixtures thereof.

5. The composition according to claim 1, wherein said swallowable uniform soft gel matrix comprises a glycerol/ethanol mixture.

6. The pharmaceutical composition according to claim 1, having an enteric coating enabling the release of thyroid hormones in the small intestine.

7. The pharmaceutical composition according to claim 1, having an outer coating which simplifies ingestion.

8. The pharmaceutical composition according to claim 1, wherein the material of the capsule contents or the swallowable uniform soft-gel matrix includes a plasticizer to control its hardness.

9. The pharmaceutical composition according to claim 8, wherein said plasticizer is selected from the group consisting of glycerol, 1,2-propylene glycol, a solution of sorbitol/sorbitanes and combinations thereof.

10. A pharmaceutical composition according to claim 1, wherein said liquid or half-liquid inner phase comprises gelatin, glycerol and ethanol.