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Bestatin glycol chitosan and preparation method thereof

A technology of ethylene glycol chitosan and plain ethylene glycol, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the difficulty and easy precipitation of bestatin and other issues to achieve a good effect of inhibiting activity

Inactive Publication Date: 2016-09-07
JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, bestatin is insoluble in water and prone to precipitation under physiological environment pH conditions (such as intestinal tract), so it is difficult to fully exert its effect
[0004] The present invention prepares bestatin ethylene glycol chitosan through chemical modification, uses drugs such as thymopentin, thymotetrapeptide and thymotripeptide as aminopeptidase substrate models, and bestatin ethylene glycol chitosan The enzyme inhibitory activity of sugar was studied, and the concentration-time curve of the model drug was drawn. The effect was good, but there were no reports

Method used

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  • Bestatin glycol chitosan and preparation method thereof
  • Bestatin glycol chitosan and preparation method thereof
  • Bestatin glycol chitosan and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Weigh 1g of ethylene glycol chitosan into a beaker, add 90ml of deionized water, adjust the pH to 6.0 with 5M hydrochloric acid, add 0.08g of bestatin, mix well, add an appropriate amount of deionized water to make the total liquid volume reach 100ml . Weigh 1.917g of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and 0.058g of N-hydroxysuccinimide, add them to the aforementioned solution together, and keep away from light at room temperature Stir for 12 hours. After the reaction, the reaction solution was transferred to a dialysis bag with a molecular weight cut-off of 10,000 Daltons for dialysis. At 4°C, 0.05M HCl was used as the dialysis medium for dialysis in 5 L of dialysis fluid, and the dialysis fluid was changed every 4 hours. Dialyze for 48 hours, use deionized water as the dialysis medium to dialyze in 5L of dialysate, change the dialysate every 4 hours, and continue to dialysis for 48 hours. The dialysate was transferred to a beaker, pre-frozen...

Embodiment 2

[0033] Weigh 1g of ethylene glycol chitosan into a beaker, add 45ml of deionized water, adjust the pH to 6.0 with 5M hydrochloric acid, add 0.3g of bestatin, and mix well. Weigh 1.917g of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and 0.058g of N-hydroxysuccinimide into a beaker, add 45ml of deionized water, and use 5M Hydrochloric acid is used to adjust the pH value to 6.0, then the solution is combined into the aforementioned solution containing ethylene glycol chitosan and bestatin, an appropriate amount of deionized water is added to make the total liquid volume reach 100ml, and the solution is stirred at room temperature in the dark for 12 hours. After the reaction, the reaction solution was transferred to a dialysis bag with a molecular weight cut-off of 10,000 Daltons for dialysis. At 4°C, 0.05M HCl was used as the dialysis medium for dialysis in 5 L of dialysis fluid, and the dialysis fluid was changed every 4 hours. Dialyze for 48 hours, use deionized...

Embodiment 3

[0037]Weigh 1g of ethylene glycol chitosan into a beaker, add 45ml of deionized water, adjust the pH to 6.0 with 5M hydrochloric acid, add 1g of bestatin, and mix well. Weigh 7.668g of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and 0.232g of N-hydroxysuccinimide into a beaker, add 45ml of deionized water, and use 5M Hydrochloric acid is used to adjust the pH value to 6.0, then the solution is combined into the aforementioned solution containing ethylene glycol chitosan and bestatin, an appropriate amount of deionized water is added to make the total liquid volume reach 100ml, and the solution is stirred at room temperature in the dark for 12 hours. After the reaction, the reaction solution was transferred to a dialysis bag with a molecular weight cut-off of 10,000 Daltons for dialysis. At 4°C, 0.05M HCl was used as the dialysis medium for dialysis in 5 L of dialysis fluid, and the dialysis fluid was changed every 4 hours. Dialyze for 48 hours, use deionized wa...

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Abstract

The invention belongs to the technical field of a pharmaceutical adjuvant, and discloses glycol chitosan having an aminopeptidase inhibitory activity and a preparation method thereof. The bestatin glycol chitosan is generated through a reaction of bestatin and glycol chitosan under a catalysis condition. In structural formula of the bestatin glycol chitosan, R represents either CH3CO- or H, n is equal to or greater than 20 and equal to or less than 320, and m / (m+n)=0.2-0.8. Physical and chemical indicators of the compound are as follows: the compound is represented as light yellow to white powdery solid which is dissolvable in water, and molecular weight is 80-250KD. By introducing the bestatin to a molecular carbohydrate chain of the glycol chitosan, the compound has a significant inhibitory activity to aminopeptidase. The bestatin glycol chitosan can inhibit aminopeptidase's degradation on small peptide protein, and can serve as a multifunctional adjuvant component in a pharmaceutical process.

Description

technical field [0001] The invention relates to an ethylene glycol chitosan derivative grafted with bestatin, which belongs to the technical field of pharmaceutical auxiliary materials. Background technique [0002] In recent years, more and more biologically active protein and polypeptide drugs have been discovered, which are widely used in the treatment of various diseases because of their high efficiency and specificity in physiological functions. However, its application is limited because it is easily degraded in the body and its biological half-life is short. Therefore, the development of protein and polypeptide drug delivery systems is a research hotspot. At present, this research mainly focuses on two aspects: one is to improve, modify, and embed peptide drugs themselves to change their physical and chemical properties; the other is to change the drug absorption environment, such as using enzyme inhibitors and absorption enhancers. [0003] Ethylene glycol chitosan ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/36C08B37/08A61K38/06A61K38/07A61K38/08
Inventor 张勇陈妍孔维
Owner JILIN UNIV