FORMULATIONS OF LIQUID STABLE ANTITHROMBIN

• US 20110082083A1
• Filed: 05/03/2010
• Published: 04/07/2011
• Est. Priority Date: 04/10/2009
• Status: Abandoned Application

• Current Assignee: LFB USA, Inc. (Agence des Participations de l’Etat)
• Original Assignee: GTC Biotherapeutics, Inc.
• Inventors: Patel, Usha S., Masiello, Nicholas C., Fontana, Lauren K., Allard, Greg J., Magneson, Gerald R., Pearce, Joseph L., Grandoni, Jerry A.
• Application Number:
  US12/773,000
• Publication Number:
  US 20110082083A1
• Time in Patent Office: Days
• US Class Current: 514/14.9
• CPC Class Codes: A61K 38/4833 Thrombin (3.4.21.5)
• CPC Class Codes: A61K 38/57 from animals; from humans A61K38/553, A61K38/556 take precedence
• CPC Class Codes: A61K 47/02 Inorganic compounds
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• CPC Class Codes: A61K 9/0019 Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner non-active ingredients are additionally classified in A61K47/00
• CPC Class Codes: A61P 7/02 Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors

Abstract

In one aspect, the invention provides liquid stable formulations of antithrombin.

Claims

1. A formulation comprising:

antithrombin, a buffer, a carboxylic acid, a disaccharide sugar and a salt.

2. The formulation of claim 1, wherein the formulation does not include a surfactant.

3. The formulation of claim 1, wherein the antithrombin is recombinant human antithrombin (rhAT).

4. The formulation of claim 1, wherein the antithrombin has a concentration of 45 to 55 mg/ml.

5. The formulation of claim 1, wherein the carboxylic acid is sodium citrate.

6. The formulation of claim 1, wherein the carboxylic acid has a concentration of 50 to 600 mM.

7. The formulation of claim 1, wherein the buffer is a tris-phosphate buffer.

8. The formulation of claim 1, wherein the buffer is between 1 mM and 100 mM.

9. The formulation of claim 1, wherein the pH is between 7.5 and 8.5.

10. The formulation of claim 1, wherein the disaccharide sugar is sucrose.

11. The formulation of claim 1, wherein the disaccharide sugar is 0.5 to 5% of volume by weight.

12. The formulation of claim 1, wherein the salt is sodium chloride.

13. The formulation of claim 1, wherein the salt has a concentration of between 25 mM and 100 mM.

14. The formulation of claim 1, wherein the antithrombin has a concentration of 50 mg/ml, wherein the carboxylic acid is sodium citrate and has a concentration of 300 mM, wherein the disaccharide sugar is sucrose and is 1% of volume by weight, wherein the salt is sodium chloride and has a concentration of 50 mM.

15. The formulation of claim 14, wherein the antithrombin is antithrombin alfa.

16. The formulation of claim 14, wherein the buffer is 10 mM tris-phosphate and the pH is 8.