Compositions of peptides and processes of preparation thereof

a technology of peptides and peptides, which is applied in the field of peptides, polypeptides, proteins, analogues or derivatives, can solve the problems that the stability of peptides has become a significant barrier, and achieve the effects of improving the stability of peptides, and polypeptides

Inactive Publication Date: 2009-11-12
NOVO NORDISK AS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0006]The present invention provides compositions comprising a therapeutically effective amount of at least one peptide, polypeptide, protein, an analog or derivative thereof and a sufficient amount of at least one stabilizing agent to improve the stability of the peptide, polypeptide, protein, analog or derivative thereof in a solution, wherein at least one stabilizing agent is a medium chain fatty acid salt, or an ester, an ether, or a derivative of a medium chain fatty acid and has a carbon chain length of from about 4 to about 20 carbon atoms or is a surface active agent. In some embodiments, at least one peptide, polypeptide, protein, an analog or derivative thereof is insulin, or an analog or derivative thereof. In one embodiment, at least one peptide, polypeptide, protein, analog or derivative thereof is Glucagon-Like Peptide (GLP), or an analog or derivatives thereof. In another embodiment, the stabilizing agent is selected from the group consisting of sodium caprylate, sodium caprate and sodium laurate.
[0007]According to another aspect of the present invention, methods for preparation of a composition of at least one peptide, polypeptide, protein, analog or derivative thereof are provided. In some embodiments, the methods comprises mixing the peptide, polypeptide, protein, analog or derivative thereof with a sufficient amount of at least one stabilizing agent to improve the stability of the peptide, polypeptide, protein, analog or derivative thereof, and the stabilizing agent is a medium chain fatty acid salt, or an ester, an ether, or a derivative of a medium chain fatty acid and has a carbon chain length of from about 4 to about 20 carbon atoms. In one embodiment, the stabilizing agent is a medium chain fatty acid salt has a carbon chain length of from about 8 to about 14 carbon atoms.

Problems solved by technology

The instability of the peptides has become a significant barrier for the preparation, process, storage and delivery of these peptides.

Method used

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  • Compositions of peptides and processes of preparation thereof
  • Compositions of peptides and processes of preparation thereof
  • Compositions of peptides and processes of preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0098]The study of gelation for different acyline batches in propylene glycol is carried out and the result is summarized in FIG. 2. The 9% and 16.7% of acyline sampls are prepared by using the acyline batches listed in FIG. 1. The 9% acyline sample of XF 173 / 315-125, XF 185 / 165-133 and XF 173 / 315-151A are prepared by using acyline prepared via use of a co-solvent during the lyophilization step. The acyline batches of XF 173 / 315-125, XF 185 / 165-133 and XF 173 / 315-151A appear clear and non-viscous after 2 hours. Other batches which are lyophilized by using water as a solvent did not appear as clear and non-viscous solutions due to the presence of gelled acyline.

example 2

[0099]The gelation of different acyline drug batches in water is investigated and the results are summarized in FIG. 3. The 0.5% and 1% acyline samples are prepared by using the acyline batches listed in FIG. 1. The 0.5% and 1% of acyline samples of XF 173 / 315-125, XF 185 / 165-133 and XF 173 / 315-151A which are prepared by using co-solvent during the lyophilization step appear clear and non viscous upon dissolving in water.

example 3

[0100]The tendency of gelation of different acyline batches in standardized microemulsion (SM) is investigated. The result is summarized in FIG. 4(a). The formulation of the standard micro emulsion is shown in FIG. 4(b). The 5 mg and 10 mg formulations of acyline in a microemulsion are prepared by using the acyline lots synthesized in FIG. 1. 5 mg and 10 mg dose of acyline batches of XF 173 / 315-151A which are prepared by using co-solvent during the lyophilization step appeared clear and transparent after 2 hours.

2. Application of Anti-Gelling Agents in the Formulation of Acyline Compositions General Procedures of Comparison Experiments

[0101]Different concentrations of acyline composition are prepared by adding acyline to pH 6.8 buffer solution either at room temperature or 37° C. All acyline solutions contain 0.6 mg / mL sodium caprate (sodium caprate is referred as C10 in the figures). All samples are centrifuged and filtered prior to analysis. Samples are analyzed by reverse phase H...

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Abstract

The present invention provides composition of comprising a therapeutically effective amount of at least one peptide, polypeptide, analog or derivative thereof and a sufficient amount of at least one stabilizing agent to improve the stability of the peptide, polypeptide, an analog or derivative thereof, wherein at least one stabilizing agent is a medium chain fatty acid salt, an ester, an ether, or a derivative of a medium chain fatty acid and has a carbon chain length of from about 4 to about 20 carbon atoms or is a surface active agent. The method for preparation of a composition of a peptide, polypeptide, protein, an analog and / or derivative thereof is also provided. The process comprises mixing the peptide, polypeptide, protein, an analog or derivative thereof with a sufficient amount of at least one stabilizing agents to improve the stability of the peptide, polypeptide, protein, an analog or derivative thereof, and the agent is a medium chain fatty acid salt, an ester, an ether, or a derivative of a medium chain fatty acid and has a carbon chain length of from about 4 to about 20 carbon atoms or is a surface active agent.

Description

RELATED APPLICATIONS[0001]This application claims the benefit under 35 U.S.C. §119(e) of U.S. Provisional Patent Application Ser. No. 61 / 051,038, filed May 7, 2008, the disclosures of which is incorporated herein by reference in its entirety.FIELD OF THE INVENTION[0002]The present invention generally relates to compositions of peptides, polypeptides, proteins, analogues or derivatives thereof, and the process of preparation thereof.BACKGROUND OF THE INVENTION[0003]A variety of biologically active peptides, polypeptides and proteins have been widely used for medical treatment. For a majority of medical treatments, there is a need to deliver a sustained level of biologically active peptides or proteins to animals or humans to provide a stable therapeutic effect. Additionally, the biologically active peptides or proteins also need to be stored for a prolonged period of time and still maintain their activity. However, many naturally occurring and synthetic peptides and proteins as well ...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/48A61K9/32A61K38/00
CPCA61K9/2846A61K9/4891A61K47/14A61K47/12A61K38/09A61K38/28A61P15/00A61P15/16A61P15/18A61P25/28A61P35/00A61P37/02A61P43/00A61P5/02A61P5/24A61P3/10A61K38/02A61K38/03A61K38/16C07K7/06
Inventor LEONARD, THOMAS W.
Owner NOVO NORDISK AS
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