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A kind of modification method of insulin

A modification, insulin technology, applied in pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., can solve the problems of low quality of life of patients, low patient compliance, etc. Absorption, good drug dispersion, strong targeting effect

Active Publication Date: 2021-03-26
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Long-term injections have a great impact on the patient's body and mind, resulting in low patient compliance and many complications, making the patient's quality of life low

Method used

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  • A kind of modification method of insulin
  • A kind of modification method of insulin
  • A kind of modification method of insulin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Dissolve 1 g of porcine insulin in 10 ml of DMSO, and add 1.0 ml of triethylamine. Add 84 mg of di-tert-butyl dicarbonate and stir at room temperature for 30 min. Then, a mixed solvent of 14 ml of acetic acid and 100 ml of water was added to stop the reaction. Freeze-drying, dissolving in a mixed solution of water and acetonitrile with a molar ratio of 2:3, and separating through a C4 chromatographic column to obtain product A.

[0031] Weigh 1.0250g of HPMA monomer, 0.234g of RAFT reagent 2-cyano-2-propylbenzodisulfide, 0.0769g of AIBN solvent with a mass concentration of 1%, dissolve in 2.5513g of DMAc, shake well and transfer into poplar In the test tube, put it in a 70°C oil bath for 24 hours after refrigerating and pumping for 4 times, and then pass air to cool down to stop the reaction and mark it as B.

[0032] Weigh 0.62 g of product B and 50 mg of product A, add 2 ml of triethylamine, and then add 10 ml of DMSO at 25°C for 10 h, then dialyze to remove small m...

Embodiment 2

[0035] Dissolve 1 g of porcine insulin in 10 ml of DMF, and add 1.0 ml of triethylamine. Add 60 mg of di-tert-butyl dicarbonate and stir at room temperature for 60 min. Then, a mixed solvent of 15 ml of acetic acid and 100 ml of water was added to stop the reaction. Freeze-drying, dissolving in a mixed solution of water and acetonitrile with a molar ratio of 2:3, and separating through a C4 chromatographic column to obtain product A.

[0036] Weigh 1.52g of methyl acrylate, 0.356g of RAFT-NHS, and 0.06g of ammonium persulfate, dissolve in 3.5g of acetonitrile, shake well and transfer to a Young’s test tube, freeze and drain 3 times, then place in a 50°C oil bath After 18 hours of reaction, the reaction was stopped by air cooling and marked as B.

[0037] Weigh 0.75g of product B and 50mg of product A respectively, add 1ml of triethylamine, and then add 10ml of DMSO at room temperature 25°C for 10h, then dialyze to remove small molecules and freeze-dry to obtain 0.8gC, a coup...

Embodiment 3

[0040]Dissolve 1 g of porcine insulin in 10 ml of water, and add 1.0 ml of triethylamine. Add 65 mg of di-tert-butyl dicarbonate and stir at room temperature for 50 min. Then, a mixed solvent of 25 ml of acetic acid and 100 ml of water was added to stop the reaction. Freeze-drying, dissolving in a mixed solution of water and acetonitrile with a molar ratio of 2:3, and separating through a C4 chromatographic column to obtain product A.

[0041] Weigh - 1.25g of methyl methacrylate monomer, 0.234g of RAFT reagent S-ethyl-S'-(2-methyl-2-propionyl) trithiocarbonate, 0.085g mass fraction is 1 % of azobisisopropylimidazoline solvent, dissolved in 3.5g of ethanol, shake well and transfer to Young's test tube, freeze and drain for 5 times, put it in a 65°C oil bath for 10 hours, and then cool down with air to stop the reaction Marked as B.

[0042] Weighed 0.9g of product B and 50mg of product A, added 3ml of triethylamine, and then added 10ml of DMSO at room temperature 25°C for 1...

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Abstract

The invention discloses an insulin modification method. Chemical coupling is adopted to combine a water-soluble polymer and the insulin through covalent bonding, wherein firstly the insulin is dissolved in a solvent, triethylamine and di-tert-butyl dicarbonate are added and stirred for a reaction, and a product A is obtained through freeze-drying and separation; then, a water-soluble polymer monomer is dissolved in a solvent, an RAFT reagent and an initiator are added for a reaction to obtain a product B; the product A and the product B are weighed, a solvent triethylamine is added, a productC is obtained through dialysis and freeze-drying, the product C is dissolved in water, trifluoroacetic acid is added for a reaction, and a coupled product D of the polymer and the insulin is obtainedthrough dialysis and freeze-drying. The chemically modified insulin is protected from degradation and inactivation by enzymes and the acid environment in the gastrointestinal environment through the water-soluble polymer, so that the degradation of the digestive enzymes of the gastrointestinal tract is effectively inhibited, and the product property is stable.

Description

technical field [0001] The invention relates to a method for modifying insulin, which uses a water-soluble polymer to protect the insulin from being degraded and inactivated by enzymes and acidic environments in the environment of the gastrointestinal tract. Solve the side effects, complications and other problems caused by insulin injection. The product prepared by the method is suitable for diabetic patients. Background technique [0002] In recent years, although people's quality of life is constantly improving, diabetic patients are also increasing year by year. Insulin is the only important protein hormone in the human body that can reduce the sugar content in the blood, secreted by pancreatic β cells. Diabetes is a disease in which the patient cannot metabolize carbohydrates due to the abnormal secretion of insulin. There are mainly two types of diabetes, type 1 diabetes and type 2 diabetes. Patients with type 1 diabetes cannot secrete insulin normally and have long-...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/28A61K47/58A61K47/60A61P3/10C08F8/00C08F120/20C08F120/14C08F120/28
CPCA61K38/28A61K47/58A61K47/60A61P3/10C08F8/00C08F120/14C08F120/20C08F120/28
Inventor 冯岸超潘翔宇沈家锋汤华燊张立群
Owner BEIJING UNIV OF CHEM TECH
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