US 6,274,553 B1 · Method for stabilizing peptides and freeze-dried medicinal compositions containing peptides obtained by using the method

Abstract

A method is provided for elevating the stability of peptides containing the sequence -Asp-Gly- or -Asn-Gly- by preventing these sequences from changing into succinimide compounds or β-transition compounds. The method comprises adding an organic acid to a solution of peptides containing these sequences to bring the pH value of the solution to a pH of between 5 and 6.5 followed by freeze-drying. In one embodiment, sucrose or mannitol is added together with the organic acid. Freeze-dried medicinal compositions obtained by using the method have excellent stability. In one embodiment of the invention, compositions produced by the method are provided and comprise hirudin or hirudin variants.

Claims27

Dependent claims

A method for stabilizing a peptide which comprises a sequence -Asp-Gly- or -Asn-Gly- by reducing the conversion of said peptide into a succinimide compound or a β-transition compound, the method comprising:

adding an amount of an organic-acid to a solution of said peptide comprising said -Asp-Gly- or -Asn-Gly- sequence, wherein said amount of organic acid is sufficient to reduce conversion of said peptide to a succinimide or β-transition compound;
adjusting the pH of the solution to a pH of between 5 and 6.5, and then lyophilizing the pH-adjusted solution.

Dependencies are inferred from the claim text.

Facts

Application

09/341,926Filed 21 Dec 1999

Priority

JP 9-02095720 Jan 1997

Granted

14 Aug 2001

Term ends

Not estimatedThe source records don’t support an estimate.

Classification9 codes

A61K 9/19
Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles: lyophilised , i.e.…
A61K 38/58
From animals; from humans: from leeches, e.g. hirudin, eglin
A61K 47/12
Containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides: carboxylic acids; Salts or anhydrides thereof
A61K 47/26
Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite: carbohydrates, e.g. sugar alcohols,…

Method for stabilizing peptides and freeze-dried medicinal compositions containing peptides obtained by using the method

Life of this patent

Method for stabilizing peptides and freeze-dried medicinal compositions containing peptides obtained by using the method

Life of this patent

Abstract

Claims27