Peptide pharmaceutical formulations

• US 20020061838A1
• Filed: 05/17/2001
• Published: 05/23/2002
• Est. Priority Date: 05/17/2000
• Status: Abandoned Application

• Current Assignee: Jefferson Pharmaceuticals LLC
• Original Assignee: Jefferson Pharmaceuticals LLC
• Inventors: Holmquist, Barton, Dormady, Daniel C.
• Application Number:
  US09/858,880
• Publication Number:
  US 20020061838A1
• Time in Patent Office: Days
• US Class Current: 514/2
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 38/25 Growth hormone-releasing factor [GH-RF], i.e. somatoliberin
• CPC Class Codes: A61K 38/26 Glucagons
• CPC Class Codes: A61K 38/29 Parathyroid hormone, i.e. parathormone; Parathyroid hormone-related peptides
• 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

Abstract

A pharmaceutical composition for administration to a mammal is disclosed. The composition includes a therapeutically effective amount of a peptide, such as a GLP-1 molecule, a PTH molecule, or a GRF molecule. The composition further includes a buffer including a weak acid having an acid dissociation constant value of greater than about 1×10⁻⁵, such as acetic acid. The composition also includes an excipient for making the composition generally isotonic, such as D-mannitol.

Claims

1. A pharmaceutical composition comprising:

a molecule selected from the group consisting of a GLP1 molecule, and GRF molecule and a PTH molecule;

an acid having a dissociation constant value of greater than 1×

10<sup>−

5</sup>; and

an excipient;

wherein the pH of said composition is between about 3.0 and 5.0.

2. The composition according to claim 1, wherein said acid comprises acetic acid.

3. The composition according to claim 1, wherein said excipient is D-mannitol.

4. The composition according to claim 1 wherein said acid is acetic acid and said excipient is D-mannitol.

5. A composition according to claim 1, wherein said composition comprises GLP-1(7-36)amide.

6. The composition according to claim 1, wherein said composition comprises GRF(1-44)amide.

7. The composition according to claim 1, wherein said composition comprises PTH(1-34)OH.

8. The composition of claim 1, wherein said composition is in unit dosage form.

9. The composition of claim 1, wherein said composition is sterile.

10. A system for administering a pharmaceutical composition comprising:

an infusion pump for administering a unit dose of the composition according to claim 1.

11. A system of claim 10, wherein said composition is diluted up to about 40-fold with isotonic saline prior to administration.

12. A method for the treatment of a disease or condition in a mammal comprising administering to the mammal a pharmaceutically effective amount of a composition according to claim 1.

13. The method of claim 12, wherein the disease or condition is selected from the group consisting of diabetes, excess appetite, obesity, stroke, ischemia, reperfusion injury, disturbed glucose metabolism, surgery, coma, shock, gastrointestinal disease, digestive hormone disease, atherosclerosis, vascular disease, gestational diabetes, liver disease, liver cirrhosis, glucorticoid excess, Cushings disease, the presence of activated counterregulatory hormones that occur after trauma or a disease, hypertriglyceridemia, chronic pancreatitis, the need for parenteral feeding, osteoporosis, and a catabolic state following surgery or injury.

14. The method of claim 12, wherein said composition is administered to said mammal by a method selected from the group consisting of intravenous, subcutaneous, continuous, intermittent, parenteral, and combinations thereof.