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Synthesis and application of exenatide joined with polyethylene glycol

A technology of exenatide and polyethylene glycol, which is applied in the synthesis and application field of exenatide, can solve the problems of short half-life, etc., and achieve the effect of long half-life, simple and effective preparation method, and long action time

Inactive Publication Date: 2012-07-04
CHEMFUTURE PHARMATECH JIANGSU
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the blood sugar control effect is obvious, the half-life of exenatide in the human body is relatively short, so it needs to be injected twice a day to maintain the drug effect. The long-acting exenatide will obviously bring convenience to patients’ lives and meet the The needs of a large number of people with type 2 diabetes

Method used

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  • Synthesis and application of exenatide joined with polyethylene glycol
  • Synthesis and application of exenatide joined with polyethylene glycol
  • Synthesis and application of exenatide joined with polyethylene glycol

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] The preparation method of the polyethylene glycol-conjugated exenatide proposed by the present invention comprises the following reactions:

[0068]

[0069] Specifically, the reaction process comprises the following steps:

[0070] (1) Dissolve exenatide (Ⅲ) in Tris-HCl buffer and adjust its pH to 7.0;

[0071] (2) Add activated compound (II), wherein the molar ratio of exenatide (III) to compound (II) is 1:8, the reaction time is 30 minutes, and the reaction temperature is 25°C;

[0072] Among them, compound (II) is methoxypolyethylene glycol succinimide propionate 5000 (mPEG-SPA-5000);

[0073] (3) After the reaction is completed, add glycine 110 times more than the molar amount of the reactants to terminate the reaction, and obtain polyethylene glycol-conjugated exenatide (I).

[0074] The separation and purification of polyethylene glycol-conjugated exenatide proposed by the present invention comprises the following steps:

[0075] The reaction solution was f...

Embodiment 2

[0096] The difference from Example 1 is that the pH is 6.5; the molar ratio of exenatide (Ⅲ) to compound (II) is 1:10, the reaction time is 60 minutes, and the reaction temperature is 30°C; among them, the compound ( In II), the value of n is 1, and the value of a in mPEG is 120.

Embodiment 3

[0098] The difference from Example 1 is that the pH is 7.5; the molar ratio of exenatide (Ⅲ) to compound (II) is 1:0.1, the reaction time is 240 minutes, and the reaction temperature is 37°C; among them, the compound ( II) is methoxypolyethylene glycol succinimidyl propionate 1000.

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PUM

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Abstract

The invention relates to exenatide joined with polyethylene glycol. The structural general formula of exenatide is (I), mPEG represents residue of methoxy polyethylene glycol, the selected value of n is 0-3, R represents an exenatide molecule from which an amino is removed, the amino is of lysine residue or of N-end histidine residue in the exenatide molecule, and the molecular weight of the exenatide joined with polyethylene glycol is 9,800-110,000. The invention further relates to a preparation method of the compound and application of the compound in preparing medicines for curing type 2 diabetes mellitus. The exenatide joined with polyethylene glycol has the advantages of being long in half-life period and good in stability and hypoglycemic effect.

Description

technical field [0001] The invention relates to a medicine, in particular to the synthesis and application of polyethylene glycol-conjugated exenatide. Background technique [0002] With the improvement of people's living standards in our country, the population of diabetes is growing rapidly. According to statistics in 2010, the incidence of diabetes in my country has reached 9.7%, and the absolute number is close to 100 million. Considering that the detection rate of diabetes in my country is still less than 40%, my country The actual number of patients with diabetes is very large, and among the diabetes patients in my country, type 2 diabetes patients account for more than 90%, and the number has surpassed that of India to become the world's number one, and the number is still growing. [0003] At present, several commonly used drugs for the treatment of type 2 diabetes may cause adverse reactions in the body, especially metformin, which has the risk of causing lactic acid...

Claims

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Application Information

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IPC IPC(8): C07K14/575C07K1/20C07K1/107A61K38/22A61K47/48A61P3/10
Inventor 赖文陆明王宝利
Owner CHEMFUTURE PHARMATECH JIANGSU
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