INJECTABLE FORMULATIONS CONTAINING SUCCINATE

• US 20070249522A1
• Filed: 07/03/2007
• Published: 10/25/2007
• Est. Priority Date: 04/03/1998
• Status: Abandoned Application

• Current Assignee: Novartis Vaccines And Diagnostics Incorporated (Novartis Ag)
• Original Assignee: Novartis Vaccines And Diagnostics Incorporated (Novartis Ag)
• Inventors: Hora, Maninder, Shirley, Bret
• Application Number:
  US11/773,184
• Publication Number:
  US 20070249522A1
• Time in Patent Office: Days
• US Class Current: 514/8.600
• CPC Class Codes: A61K 38/30 Insulin-like growth factors, i.e. somatomedins, e.g. IGF-1, IGF-2 insulin-like growth factor binding protein A61K38/1754
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• 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

Abstract

The invention is directed to formulations of a pharmaceutically active agent for in vivo use. The formulations to which the invention is directed are designed to minimize the pain associated with components in injectable formulations, other than the pharmaceutically active agent. The invention is particularly directed to buffers that provide for minimum pain upon injection. Insulin-like growth factor I (IGF-I) is a preferred pharmaceutically active agent.

Claims

1. A pharmaceutical composition comprising human insulin-like growth factor 1 (IGF-I) and a buffer, wherein said buffer consists substantially of succinate at a concentration of about 10 mM to about 40 mM and a counterion.

2. The composition of claim 1, wherein said counterion is selected from the group consisting of sodium, potassium, ammonium, and said IGF-I.

3. The composition of claim 1, wherein the concentration of succinate is about 10 mM to about 30 mM.

4. The composition of claim 3, wherein the concentration of succinate is about 10 mM to about 20 mM.

5. The composition of claim 4, wherein the concentration of succinate is about 10 mM.

6. The composition of claim 1, wherein said composition has a pH of about 4.0to about 7.0.

7. The composition of claim 6, wherein said pH is about 4.6 to about 6.6.

8. The composition of claim 7, wherein said pH is about 6.0.

9. The composition of claim 1, further comprising a sufficient concentration of a tonicifying agent such that the composition is isotonic.

10. The composition of claim 9, wherein said tonicifying agent is sodium chloride.

11. The composition of claim 1, wherein said human IGF-I is recombinant human IGF-I.

12. The composition of claim 11, wherein said composition has a pH of about 6.0, the concentration of said succinate is about 10 mM, and the composition further comprises about 140 mM sodium chloride.

13. The pharmaceutical composition of claim 1, wherein said composition is a liquid.

14. The pharmaceutical composition of claim 1, wherein said composition is lyophilized.

17. A method for the treatment, prevention or diagnosis of a disease or condition, comprising administering by injection, a pharmaceutically effective amount of the pharmaceutical composition of claim 1 to a subject in need of treatment with said pharmaceutically active agent.

18. A method for the treatment, prevention or diagnosis of a disease or condition, comprising administering by injection, a pharmaceutically effective amount of the pharmaceutical composition of claim 12 to a subject in need of treatment with said pharmaceutically active agent.

15. A sterile injectable pharmaceutical composition comprising human insulin-like growth factor I (IGF-I) or a biologically active variant thereof and a buffer, wherein said buffer consists substantially of succinate at a concentration of 7 mM to 45 mM and a counterion, wherein said variant is a polypeptide having IGF-I activity and at least 70% sequence identity to human IGF-I.

16. The composition of claim 15, wherein said composition has a pH of about 6.0, the concentration of said succinate is about 10 mM, and the composition further comprises about 140 mM sodium chloride.

19. A method for the treatment, prevention or diagnosis of a disease or condition, comprising administering by injection, a pharmaceutically effective amount of the pharmaceutical composition of claim 15 to a subject in need of treatment with said pharmaceutically active agent.

20. A method for reducing pain upon injection of a pharmaceutical composition comprising human insulin-like growth factor I (IGF-I) or a biologically active variant thereof, said method comprising administering to a subject in need thereof the pharmaceutical composition of claim 15.