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Synthesis method and application of chitosan oligosaccharide/indometacin graft

A technology of indomethacin grafts and synthesis methods, which can be applied in the direction of drug combinations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., and can solve the problems of poor selectivity and insoluble in water, etc. It achieves the effects of strong inhibition rate, no organic solvent residue, and simple preparation

Inactive Publication Date: 2014-01-22
HANGZHOU NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In order to solve the problems of poor selectivity and insoluble water in many chemical antineoplastic drugs currently used clinically, the present invention provides a synthesis method of chitosan / indomethacin grafts. Sugar and indomethacin with different grafting rates can achieve controlled and sustained release of the drug

Method used

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  • Synthesis method and application of chitosan oligosaccharide/indometacin graft
  • Synthesis method and application of chitosan oligosaccharide/indometacin graft
  • Synthesis method and application of chitosan oligosaccharide/indometacin graft

Examples

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Effect test

Embodiment 1

[0052] (1) Weigh carbodiimide EDC (0.5953g, 3.105mmol) and indomethacin 0.2222g (0.6210mmol) into 8ml of acetone to form A liquid, and stir the A liquid at a constant temperature of 25°C The solution dissolves. Then weigh 0.2g (0.02222mmol) of chitosan oligosaccharide (Mw=9000) and put it in 10ml of distilled water to form B solution, which is also stirred and dissolved at a constant temperature of 25°C. At 25°C, slowly drop liquid A into liquid B while liquid B is stirring. After the dropwise addition, the solution was placed on a constant temperature heating magnetic stirrer, and reacted at a reaction temperature of 25° C. for 53 hours. After the reaction, the reaction solution was transferred to a dialysis bag (membrane molecular weight cut-off MWCO=7000), and deionized water was used as the dialysate for dialysis for 10 hours. The water was changed every half hour for the first three hours, and the water was changed every hour thereafter. After the dialysis is finished, ...

Embodiment 2~7

[0055] Different molecular weight chitosan oligosaccharides and different graft ratios of indomethacin as described in table 1, according to the synthetic method of the chitosan oligosaccharide / indomethacin graft of embodiment 1, synthetically obtains chitosan oligosaccharide / indomethacin Purified products of octyl grafts 2-7.

[0056] Table 1: Chitooligosaccharides with different molecular weights and different grafting ratios of indomethacin

[0057]

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Abstract

The invention relates to the technical field of pharmaceutical materials, provides a method for synthesizing a chitosan oligosaccharide / indometacin graft and aims to solve the problems that many chemical antitumor drugs for clinical use are low in selectivity and are difficultly dissolved in water at present. Chitosan oligosaccharide of different molecular weights and indometacin with different grafting rates are selected, so that controlled / slow release of drugs can be realized. Meanwhile, the invention also provides application of the chitosan oligosaccharide / indometacin graft on a slightly soluble drug targeting vector, namely an alkaline adriamycin-loaded chitosan oligosaccharide / indometacin microparticle drug delivery system is provided. The drug delivery system has the characteristics of high drug loading capacity and encapsulation rate.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical auxiliary materials, in particular to a chitosan / indomethacin synthesis method and application thereof. Background technique [0002] Cancer is one of the most common causes of human health and death today. According to a new report by the American Cancer Society, in 2007, there will be more than 12 million new cancer cases in the world, and 7.6 million people will die of cancer, that is, 20,000 people will die of cancer every day. Cancer is becoming one of the most important diseases facing the world. In the past 30 years in China, the incidence of cancer has been increasing at an average annual rate of 3%-5%. There are 2.8 million new cancer cases every year, and one out of every four to five deaths is from cancer. Cancer has become the number one killer threatening national health. Therefore, the treatment of cancer is a major challenge in front of our medical workers, and the develop...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08B37/08A61K47/36A61K31/704A61P35/00
Inventor 魏晓红
Owner HANGZHOU NORMAL UNIVERSITY
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