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Non-steroid anti-inflammatory agent-chitosan synthesizing method and product thereof

A non-steroidal anti-inflammatory drug and a synthesis method technology, applied in the directions of anti-inflammatory agents, drug combinations, pharmaceutical formulations, etc., can solve the problems of complicated methods, high cost, inconvenience to expand production, etc., and achieve cost reduction, simplification of synthesis process, Beneficial to industrial production

Inactive Publication Date: 2017-09-22
FOSHAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Comparative documents 1-4 mainly discuss that chitosan can be linked or synthesized with other drugs, and these synthetic products have certain pharmacological effects, and some solve the main side effects of some non-steroidal anti-inflammatory drugs, but comparative documents 1-4 The method adopted is too complicated and the cost is too high to be convenient for large-scale production
Moreover, the existing synthetic method is limited to a non-steroidal anti-inflammatory drug, which is inconvenient to expand production and cannot meet the medical needs of different occasions

Method used

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  • Non-steroid anti-inflammatory agent-chitosan synthesizing method and product thereof
  • Non-steroid anti-inflammatory agent-chitosan synthesizing method and product thereof
  • Non-steroid anti-inflammatory agent-chitosan synthesizing method and product thereof

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preparation example Construction

[0038] see figure 1 , the invention provides a kind of synthetic method of NSAID-chitosan, comprising:

[0039] 1. Add 5~50ml of dichloromethane and 0.5~5.0g of chitosan into the reaction vessel and shake well;

[0040] Wherein, the dichloromethane is anhydrous dichloromethane, and the present invention selects dichloromethane, because chitosan and most non-steroidal anti-inflammatory drugs are easier to dissolve therein, and are volatile and easy to remove.

[0041] The chitosan is dried at 55-90°C for 1-5 hours. Preferably, the chitosan is dried at 60-80°C for 1-3 hours. More preferably, the chitosan is dried at 65-75°C for 1-2 hours. The chitosan is specially dried to remove moisture to the greatest extent without destroying its structure, which is beneficial for chemical reactions to occur under anhydrous conditions.

[0042] 2. Add 0.6~6.0g non-steroidal anti-inflammatory drugs and 1.0~10.0g activated 3A molecular sieve, mix well and stir to dissolve;

[0043] Wherei...

Embodiment 1

[0072] 1. Add 5ml of anhydrous dichloromethane and 0.5g of chitosan to the reaction vessel, shake well, wherein the chitosan is dried at 55°C for 1 hour;

[0073] 2. Add 0.6g of non-steroidal anti-inflammatory drugs and 1.0g of activated 3A molecular sieves, mix well and stir to dissolve. Among them, the non-steroidal anti-inflammatory drugs are dried at 55°C for 1 hour; the activated 3A molecular sieves are dried at 90°C for 5 hours;

[0074] 3. Put the reaction vessel under an ice-water bath, add 0.3 g of N,N1-dicyclohexylcarbodiimide and 0.01 g of 4-dimethylaminopyridine, continue to stir, slowly warm up to room temperature, and react for 12 hours;

[0075] 4. Filter the reaction solution to remove molecular sieves and insoluble matter, wash the filter residue with 1ml of dichloromethane, freeze the filtrate overnight, then filter and wash, repeat several times until no precipitation occurs;

[0076] 5. Repeatedly washing and extracting the dichloromethane solution with di...

Embodiment 2

[0078] 1. Add 10ml of anhydrous dichloromethane and 1.0g of chitosan to the reaction vessel, shake well, wherein the chitosan is dried at 60°C for 2 hours;

[0079] 2. Add 1.0 g of non-steroidal anti-inflammatory drugs and 2.0 g of activated 3A molecular sieves, mix well and stir to dissolve. Among them, the non-steroidal anti-inflammatory drugs are dried at 65°C for 2 hours; the activated 3A molecular sieves are dried at 100°C for 10 hours;

[0080] 3. Put the reaction vessel under an ice-water bath, add 0.5 g of N,N1-dicyclohexylcarbodiimide and 0.05 g of 4-dimethylaminopyridine, continue to stir, slowly warm up to room temperature, and react for 20 hours;

[0081] 4. Filter the reaction solution to remove molecular sieves and insoluble matter, wash the filter residue with 2ml of dichloromethane, freeze the filtrate overnight, then filter and wash, repeat several times until no precipitation occurs;

[0082] 5. Repeatedly washing and extracting the dichloromethane solution ...

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Abstract

The invention discloses a synthesis method of chitosan, a non-steroidal anti-inflammatory drug, which comprises: adding 5-50ml of dichloromethane and 0.5-5.0g of chitosan into a reaction vessel, shaking well; adding 0.6-6.0g Mix non-steroidal anti-inflammatory drugs and 1.0~10.0g of activated 3A molecular sieves evenly and stir to dissolve; put the reaction vessel under an ice-water bath, add 0.01~1g of catalyst, continue to stir, slowly warm up to room temperature, and react for 12-72h ; filter the reaction solution to remove molecular sieves and insoluble matter, wash the filter residue with dichloromethane solution, freeze the filtrate overnight, then filter and wash, repeat several times until no precipitation is precipitated; repeatedly wash and extract the dichloromethane solution with distilled water, and then After drying, the product was obtained. By adopting the invention, the synthesis process can be simplified, the cost can be reduced, the industrial production is beneficial, and the common side effects of most non-steroidal anti-inflammatory drugs can be reduced.

Description

technical field [0001] The invention relates to the technical field of medicine synthesis, in particular to a synthesis method of non-steroidal anti-inflammatory drug-chitosan, and non-steroidal anti-inflammatory drug-chitosan amide derivatives prepared by the synthesis method. Background technique [0002] Non-steroidal anti-inflammatory drugs (Non-steroidal Anti-inflammatory Drugs, NSAIDs) have antipyretic, pain-relieving, anti-inflammatory, cooling, and anti-rheumatic effects, and their chemical structure is similar to that of adrenal cortex hormones. In the case of enoic acid metabolism, the reduction of prostaglandin synthesis is a compound that is different from other pharmacological mechanisms. Commonly used clinically include aspirin, ibuprofen, indomethacin, diclofenac, naproxen, acetaminophen, rofecoxib, etc. Long-term high-dose administration can lead to gastrointestinal reactions, liver, kidney and blood system damage etc. [0003] Chitosan is a natural glucosa...

Claims

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Application Information

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IPC IPC(8): A61K47/61A61K45/00A61P29/00C08B37/08
CPCY02P20/582A61K45/00C08B37/003
Inventor 聂鑫刘泳珊谢婉仪林荣喜陈小祝梁伟光杜卓
Owner FOSHAN UNIVERSITY
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