Human glucagon-like peptide-1 compound and its preparing method

A technology of glucagon and compound, which is applied in the field of peptide or protein modification compound and its preparation, which can solve the problems of poor biological stability, subcutaneous injection 3-4 times a day, and patients’ reluctance to accept it, and achieve production cost Low, improve bioavailability, improve the effect of biological stability

Inactive Publication Date: 2005-10-05
EAST CHINA NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, human glucagon-like peptide-1 is a biologically active small peptide, which is easily degraded by a specific dipeptidyl peptidase IV (DPP IV) in vivo, resulting in poor biological stability, and its half-life in vivo is only 2- 3 minutes
The peak blood concentration produced by subcutaneous injection of human glucagon-like peptide-1 can only be maintained for a short time. If it is used for diabetes treatment, it needs to be injected subcutaneously 3-4 times a day, which will bring pain to the patient or make the patient uncomfortable. willing to accept

Method used

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  • Human glucagon-like peptide-1 compound and its preparing method
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  • Human glucagon-like peptide-1 compound and its preparing method

Examples

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Embodiment 1

[0026] Example 1 Preparation of complexes of human glucagon-like peptide-1. In this embodiment, the active group of monomethoxypolyethylene glycol activated by succinimide is monomethoxypolyethylene glycol-succinimide propionate, ie mPEG-SPA, with a molecular weight of 5KD.

[0027] In the first step, 1.0mg of human glucagon-like peptide-1 (7-37) was dissolved in 0.5ml of 100mM, pH7.4 phosphate buffer, and then mixed with 0.5ml of 200mM phosphoric acid of pH6.0-9.0 Salt buffer or boric acid-borax buffer mixed;

[0028] In the second step, 1.5 mg of monomethoxypolyethylene glycol-propionic acid succinimide with a molecular weight of 5KD, i.e. mPEG-SPA, was added to the solution of the first step, and mixed uniformly;

[0029] In the third step, the solution obtained in the second step is placed at 4°C to 40°C for mPEG modification reaction for 0.5 to 24 hours;

[0030] In the fourth step, the solution treated in the third step is placed at -20°C to terminate the reaction, so fa...

Embodiment 2

[0037] Example 2 Preparation of complexes of human glucagon-like peptide-1. In this embodiment, the monomethoxypolyethylene glycol of the active group activated by succinimide is a branched monomethoxypolyethylene glycol-succinimide ester, namely mPEG-NHS, which The molecular weight is 10KD.

[0038] In the first step, 1.0 mg of human glucagon-like peptide-1 (7-37) was dissolved in 0.5 ml of 100 mM, pH 7.4 phosphate buffer, and then mixed with 0.5 ml of 200 mM phosphoric acid of pH 6.0 to 9.0 Salt buffer or boric acid-borax buffer mixed;

[0039] In the second step, 3.0 mg of branched monomethoxypolyethylene glycol-succinimide ester with a molecular weight of 10KD, i.e. mPEG-NHS, was added to the solution of the first step, and mixed uniformly;

[0040] The third step to the fifth step are carried out according to the corresponding operation steps in the first embodiment.

[0041] In the sixth step, the elution solution collected in the fifth step was concentrated with a Mi...

Embodiment 3

[0044] Example 3 Preparation of complexes of human glucagon-like peptide-1. In this embodiment, the monomethoxypolyethylene glycol of the active group activated by succinimide is monomethoxypolyethylene glycol-succinimide propionate, i.e. mPEG-SPA, and its molecular weight is 20KD.

[0045] In the first step, 1.0 mg of human glucagon-like peptide-1 (7-37) was dissolved in 0.5 ml of 100 mM pH7.4 phosphate buffer, and then mixed with 0.5 ml of 200 mM pH8.4 phosphate buffer solution or boric acid-borax buffer mixed;

[0046] In the second step, 6.0 mg of monomethoxypolyethylene glycol-propionic acid succinimide, i.e. mPEG-SPA, with a molecular weight of 20KD was added to the solution of the first step, and mixed uniformly;

[0047] The third step to the fifth step are carried out according to the corresponding operation steps in the first embodiment.

[0048] In the sixth step, the elution solution collected in the fifth step was concentrated with a MilliporeAmicon Ultra-15 ul...

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Abstract

The present invention relates to a human pancreatic glucagons sample peptide-1 compound and its preparation method. The human pancreatic glucagons sample peptide-1 in said compound is human pancreatic glucagons sample peptide-1(7-37) or human pancreatic glucagons sample peptide-1(7-36)Nh2. Said compound is formed from human pancreatic glucagons sample peptide-1 and monomethoxy polyglycol containing active group activated by succinimide, namely said compound is mPEG-GLP-1.

Description

technical field [0001] The present invention relates to a complex of human glucagon-like peptide-1 and a preparation method thereof, specifically, to a monomethoxypolyethylene glycol-human glucagon-like peptide-1, i.e. mPEG- The compound of GLP-1 and its preparation method belong to the technical field of modification compound of peptide or protein and its preparation. Background technique [0002] Diabetes is a worldwide disease with a high incidence rate and poses a serious threat to human health. According to the latest report of the International Diabetes Institute (IDI) in 2003, there are 194 million people with diabetes worldwide. According to the current growth rate, by 2025, the number of patients will reach 333 million. There are more than 40 million diabetic patients in my country. In the early 1980s, the incidence rate of diabetes in my country was only 0.67%. Now the incidence rate in Beijing, Shanghai and other places has exceeded 10%, and this number is still ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/17A61P3/10
Inventor 黄静吴自荣左翼徐进楼旻徐伟东
Owner EAST CHINA NORMAL UNIV
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