HFSH AQUEOUS FORMULATION

• US 20110201554A1
• Filed: 09/25/2006
• Published: 08/18/2011
• Est. Priority Date: 09/27/2005
• Status: Abandoned Application

• Current Assignee: LG Life Sciences Limited (LG Corporation)
• Original Assignee: LG Life Sciences Limited (LG Corporation)
• Inventors: Choi, Suk Young, Jeh, Hoon Sung
• Application Number:
  US12/066,190
• Publication Number:
  US 20110201554A1
• Time in Patent Office: Days
• US Class Current: 514/9.9
• CPC Class Codes: A61K 38/24 Follicle-stimulating hormone [FSH]; Chorionic gonadotropins, e.g. HCG; Luteinising hormone [LH]; Thyroid-stimulating hormone [TSH]
• CPC Class Codes: A61K 47/02 Inorganic compounds
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/16 containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
• CPC Class Codes: A61K 47/20 containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
• CPC Class Codes: A61K 47/24 containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• 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: A61K 9/08 Solutions composition of solutions A61K47/00
• CPC Class Codes: A61P 15/08 for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
• CPC Class Codes: A61P 5/00 Drugs for disorders of the endocrine system
• CPC Class Codes: A61P 5/06 of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
• CPC Class Codes: A61P 5/24 of the sex hormones

Abstract

Provided is an aqueous formulation of a human follicle stimulating hormone (hFSH) which is stabilized to maintain the activity of hFSH for a prolonged period of time. The formulation of the present invention is an aqueous formulation comprising a therapeutically effective amount of hFSH stabilized in a phosphate buffer containing glycine, methionine and a non-ionic surfactant, preferably polysorbate 20, which is capable of maintaining the activity of hFSH for an extended period of time.

Claims

1. An aqueous formulation of a human follicle stimulating hormone (hFSH), comprising a therapeutically effective amount of hFSH, and glycine, methionine, a non-ionic surfactant and a phosphate buffer as stabilizers.

2. The formulation according to claim 1, wherein the hFSH is a naturally-occurring hFSH or a recombinant FSH (rFSH).

3. The formulation according to claim 1, wherein the non-ionic surfactant is selected from the group consisting of a polysorbate-based non-ionic surfactant, a poloxamer-based non-ionic surfactant and any combination thereof.

4. The formulation according to claim 3, wherein the non-ionic surfactant is polysorbate 20.

5. The formulation according to claim 1, wherein glycine is included in an amount of 0.1 to 10% (w/v).

6. The formulation according to claim 1, wherein methionine is included in an amount of 0.01 to 2.0% (w/v).

7. The formulation according to claim 1, wherein the non-ionic surfactant is included in an amount of 0.001 to 0.02% (w/v).

8. The formulation according to claim 1, wherein the phosphate buffer has a salt concentration of 1 mM to 50 mM and a pH of 6.5 to 7.5.

9. The formulation according to claim 1, wherein the formulation further includes a preservative and/or an isotonic agent.

10. The formulation according to claim 9, wherein the preservative is benzyl alcohol, cresol, alkyl paraben or a mixture thereof, and the isotonic agent is a water-soluble inorganic salt and/or a sugar alcohol.