Storage stable thyroxine active drug formulations and methods for their production

• US 7,195,779 B2
• Filed: 06/03/2005
• Issued: 03/27/2007
• Est. Priority Date: 11/13/2001
• Status: Expired due to Term

• Current Assignee: Mylan Pharmaceuticals Incorporated (Pfizer Inc.)
• Original Assignee: Mylan Pharmaceuticals Incorporated (Pfizer Inc.)
• Inventors: Wargo, David John, Hanshew, Dwight D. Jr.
• Primary Examiner(s): Hartley; Michael G.
• Assistant Examiner(s): Oh; Simon J.
• Application Number:
  US11/143,645
• Publication Number:
  US 20050232991A1
• Time in Patent Office: 662 Days
• Field of Search: 424/400, 424/464, 424/465, 424/468, 424/489, 424/499, 424/502, 514/567
• US Class Current: 424/465
• 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 9/1623 Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
• CPC Class Codes: A61K 9/2018 Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
• CPC Class Codes: A61K 9/205 Polysaccharides, e.g. alginate, gums; Cyclodextrin
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2077 Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets

Abstract

This invention provides a storage-stable dosage form of a thyroxine active drug composition which exhibits an improved stability. The formulation contains a thyroxine active drug substance, an alditol, and a saccharide, and, optionally, additional pharmaceutically accepted excipients. Levothyroxine sodium is the preferred active drug substance, mannitol is the preferred alditol, and sucrose is the9 preferred saccharide. Additional preferred excipients include, for example, microcrystalline cellulose, crospovidone, magnesium stearate, colloidal silicon dioxide, and sodium lauryl sulfate.

Claims

1. A storage stable pharmaceutical composition in unit dosage form which comprises levothyroxine sodium in a therapeutically effective amount, mannitol in the amount of about 58% of the total weight of said composition, and sucrose in an amount of about 14% of the total weight of said composition.

2. A composition of claim 1 which comprises at least one further pharmaceutical excipient.

4. A method for the treatment of thyroid disorders comprising orally administering the composition of claims 1 or 3 to a human.

5. A composition of claims 1 or 3 which is a solid oral dosage form.

6. A composition of claims 1 or 3 which is a tablet.

3. A storage stable oral pharmaceutical composition in unit dosage form which comprises a therapeutically effective amount of levothyroxine sodium, a stabilizing amount of mannitol, a stabilizing amount of sucrose, and optionally further comprises other pharmaceutically acceptable excipients wherein said stabilizing amount of mannitol is from about 25% to about 70% of the total weight of said composition and wherein said stabilizing amount of sucrose is from about 20% to about 40% of the total weight of said composition.