Stabilized pharmaceutical and thyroid hormone compositions and method of preparation

• US 20030119911A1
• Filed: 02/15/2002
• Published: 06/26/2003
• Est. Priority Date: 02/15/2001
• Status: Active Grant

• Current Assignee: Elaine A. Strauss, Franz G. Andrew, Philip A. Dimenna, Rocco L. Gemma
• Original Assignee: Elaine A. Strauss, Franz G. Andrew, Philip A. Dimenna, Rocco L. Gemma
• Inventors: Gemma, Rocco L., Franz, G. Andrew, Strauss, Elaine A., DiMenna, Philip A.
• Granted Patent: US 7,067,148 B2
• Time in Patent Office: Days
• US Class Current: 514/567
• CPC Class Codes: A61K 31/195 having an amino group
• 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 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2072 characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms A61K9/0004, A61K9/0056, A61K9/0065 take precedence
• CPC Class Codes: A61P 5/14 of the thyroid hormones, e.g. T3, T4
• CPC Class Codes: B01F 25/433 Mixing tubes wherein the shape of the tube influences the mixing, e.g. mixing tubes with varying cross-section or provided with inwardly extending profiles
• CPC Class Codes: B01F 25/4334 Mixers with a converging cross-section
• CPC Class Codes: B01F 25/82 uniting flows of material taken from different parts of a receptacle or from a set of different receptacles

Abstract

A pharmaceutical composition with β-sheet microcrystalline cellulose with improved potency life and methods of preparation therefor. Improved thyroid hormone pharmaceutical compositions comprising 50 weight % or more of β-sheet microcrystalline cellulose.

Claims

1. A pharmaceutical composition in solid form comprising a pharmaceutically active ingredient and a β

-sheet form of microcrystalline cellulose.

2. The pharmaceutical composition of claim 1 wherein at least about 50 weight % of the composition weight is β

-sheet form of microcrystalline cellulose.

3. The pharmaceutical composition of claim 1 wherein the active ingredient is levothyroxine sodium.

4. The pharmaceutical composition of claim 2 wherein the active ingredient is levothyroxine sodium.

5. The pharmaceutical composition of claim 1 wherein the active ingredient is liothyronine sodium.

6. The pharmaceutical composition of claim 2 wherein the active ingredient is liothyronine sodium.

7. A method of preparing a solid dosage form of a pharmaceutically active ingredient comprising forming a blend by blending the pharmaceutically active ingredient and β

-sheet form of microcrystalline cellulose, and forming therefrom a solid dosage.

8. The method of claim 7 wherein the solid dosage is formed by compressing the blend in a tableting machine.

9. The method of claim 8 wherein the blend is compressed in a ratio of initial volume to final volume from 3.3:

1 to 4.0;

1.

10. The method of claim 7 wherein the pharmaceutically active ingredient comprises levothyroxine sodium.

11. The method of claim 7 wherein the pharmaceutically active ingredient comprises liothyronine sodium.

12. The method of claim 8 wherein the tableting machine further comprises extra deep tablet dies that maintain a free clearance of at least 3.0 mm during filling.

13. The method of claim 12 wherein the tableting machine forms tablets in a shape selected from the group consisting of cylindrical shape and raised violin shape.