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Peptide complex, pharmaceutical composition thereof, and preparation and application thereof

A composition and drug technology, applied in the direction of drug combination, pharmaceutical formula, specific peptide, etc., can solve the problems of increasing the pain of patients and short half-life, and achieve the effect of prolonging the half-life and facilitating clinical promotion and application.

Inactive Publication Date: 2013-03-06
天津拓飞科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the Exendin-4 drugs currently on the market still have the problem of short half-life. The medicinal Exenatide (Exenatide) is injected twice a day, which greatly increases the suffering of patients.
Therefore, there is currently a need for methods to address the short in vivo half-life of Exendin-4 drugs

Method used

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  • Peptide complex, pharmaceutical composition thereof, and preparation and application thereof
  • Peptide complex, pharmaceutical composition thereof, and preparation and application thereof
  • Peptide complex, pharmaceutical composition thereof, and preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Solid Phase Synthesis of Peptides

[0053] Using the solid-phase peptide synthesis method of the Fmoc strategy, the CS 336X instrument produced by CSBio Company was used to synthesize the peptide in the patent. The method of synthesis was carried out according to the manufacturer's instruction manual.

[0054] The prepared polypeptide was purified using HPLC C18 semi-preparative column, and the mobile phase was acetonitrile. The polypeptide freeze-dried powder is obtained by desalting and freeze-drying. The polypeptides included in this patent all contain disulfide bonds, and ammonium bicarbonate or other reducing agents are used to form disulfide bonds in the polypeptides.

Embodiment 2

[0056] Hypoglycemic function related to GLP-1 analog (SEQ ID NO 4)

[0057] In this example, the polypeptides we use are as follows (401-427 corresponds to the sequence list 1-27):

[0058] SEQ ID NO 401: 7 HAEGT FTS C V SSYLE GQAAK EFIAW LVKGR G 37 GGGGG C GGG

[0059] SEQ ID NO 402: 7 HAEGT FTS C V SSYLE GQAAK EFIAW LVKGR G 37 GGGGG GGGGG C GGG

[0060] SEQ ID NO 403: 7 HAEGT FTS C V SSYLE GQAAK EFIAW LVKGR G 37 GGGGG GGGGG GGGGG C GGG

[0061] SEQ ID NO 404: 7 HAEGT FTS C V SSYLE GQAAK EFIAW LVKGR G 37 GGGGG C GGGGG G

[0062] SEQ ID NO 405: 7 HAEGT FTS C V SSYLE GQAAK EFIAW LVKGR G 37 GGGGG C GGGGG GGGG

[0063] SEQ ID NO 406: 7 HAEGT FTS C V SSYLE GQAAK EFIAW LVKGR G 37 GGGGG GGGGG C GGGGG G

[0064] SEQ ID NO 407: 7 HAEGT FTS C V SSYLE GQAAK EFIAW LVKGR G 37 GGGGG GGGGG C GGGGG GGGG

[0065] SEQ ID NO 408: 7 HAEGT FTS C V SSYLE GQAAK EFIAW LVKGR G 37 GGGGG GGGGG GGGGG C GGGGG G

[0066] SEQ ID NO 409: 7 HAEGT FTS C V SSYLE GQAAK ...

Embodiment 3

[0087] Hypoglycemic function associated with GLP-1 analog (SEQ ID NO 5). (Sequence Listing 28-55)

[0088] SEQ ID NO 501: 7 HAEGT FTSDV SSYLE GQAAK EFI C W LVKGR G 37 G C GGGGG GGGGG

[0089] SEQ ID NO 502: 7 HAEGT FTSDV SSYLE GQAAK EFI C W LVKGR G 37 G C GGGGG GGGGG GGGGG

[0090] SEQ ID NO 503: 7 HAEGT FTSDV SSYLE GQAAK EFI C W LVKGR G 37 G C GGGGG GGGGG GGGGG GGGGG GGGGG

[0091] SEQ ID NO 504: 7 HAEGT FTSDV SSYLE GQAAK EFI C W LVKGR G 37 GG C GGGGG GGGGG

[0092] SEQ ID NO 505: 7 HAEGT FTSDV SSYLE GQAAK EFI C W LVKGR G 37 GG C GGGGG GGGGG GGGGG

[0093] SEQ ID NO 506: 7 HAEGT FTSDV SSYLE GQAAK EFI C W LVKGR G 37 GG C GGGGG GGGGG GGGGG GGGGG

[0094] SEQ ID NO 507: 7 HAEGT FTSDV SSYLE GQAAK EFI C W LVKGR G 37 GGGGG C GGGGG GGGGG

[0095] SEQ ID NO 508: 7 HAEGT FTSDV SSYLE GQAAK EFI C W LVKGR G 37 GGGGG C GGGGG GGGGG GGGGG

[0096] SEQ ID NO 509: 7 HAEGT FTSDV SSYLE GQAAK EFI C W LVKGR G 37 GGGGG C GGGGG GGGGG GGGGG GGGGG

[0097]...

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Abstract

The invention relates to a peptide complex, a pharmaceutical composition thereof, and a preparation and an application thereof. The invention relates to a GLP-1 analog. Aiming at defects of short in-vivo retention time and the need of daily injection administration of GLP-1 analog, the invention provides a GLP-1 analog with a longer half-life period. The invention also discloses a composition composed of the GLP-1 analog as an effective component and pharmaceutically acceptable auxiliary materials. The invention also relates to the application of the GLP-1 analog in preparing medicines used for treating and / or preventing obesity.

Description

technical field [0001] The present invention relates to the technical field of medicines related to diabetes treatment, in particular, the present invention relates to a polypeptide complex, which has prolonged exendin-4 half-life in vivo. The invention also relates to the preparation method and application of the polypeptide complex. Background technique [0002] Diabetes mellitus is a metabolic disorder syndrome characterized by chronic hyperglycemia associated with genetic factors and multiple environmental factors. Because diabetes is also accompanied by many complications, it has become the third largest health killer after malignant tumors and cardiovascular diseases. In 1984, the glucagon peptide-1 (GLP-1) class of drugs was discovered, which is an incretin with 30 amino acids. The main reason why GLP-1 is limited as a hypoglycemic drug is that the half-life of GLP-1 in vivo is only 3-5 minutes. [0003] Exendin-4 is a straight-chain polypeptide composed of 39 amin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/575A61K38/22A61P3/10A61P3/04
Inventor 许辉
Owner 天津拓飞科技有限公司
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