Anti-inflammatory drug (polysaccharide conjugate) as well as preparation and application of drug composition thereof

A technology of anti-inflammatory drugs and conjugates, applied in the field of pharmaceutical preparations, can solve the problems of harsh synthesis conditions, low grafting rate, and low yield, and achieve the effects of good redispersibility, high drug loading, and smooth surface

Inactive Publication Date: 2010-06-16
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Some polysaccharide-drug conjugates are currently in the research stage, but these conjugates are only administered in the form of drug-polysaccharide conjugates, and it is still impossible to achieve the purpose of combined therapy through one formulation, and the drug release behavior is single, which is difficult to achieve. Meeting the Treatment Requirements for Rheumatoid Arthritis
In addition, there are also the following defects: the inherent difficulties in the c

Method used

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  • Anti-inflammatory drug (polysaccharide conjugate) as well as preparation and application of drug composition thereof
  • Anti-inflammatory drug (polysaccharide conjugate) as well as preparation and application of drug composition thereof
  • Anti-inflammatory drug (polysaccharide conjugate) as well as preparation and application of drug composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Embodiment 1: the synthesis of ketoprofen-chondroitin sulfate conjugate

[0053] Take 10mmol of ketoprofen, 12mmol of dicyclohexylcarbodiimide (DCC), and 15mmol of hydroxysuccinimide (NHS), dissolve them in 30ml of N,N-dimethylformamide, keep away from light, under the protection of nitrogen, and place in an ice bath Reacted for 30min, then rose to room temperature for 24h. After the reaction, the precipitate was filtered off, and a large amount of ethyl acetate was added to wash the precipitate. The filtrate was extracted, the ethyl acetate layers were combined, and the solvent was removed by rotary evaporation to obtain the activated intermediate ester of ketoprofen. 3mmol ketoprofen activated intermediate ester is dissolved in 15ml dichloromethane, under ice-bath condition, slowly drips in the dichloromethane solution of 9mmol / ml ethylenediamine, thin-layer chromatography (TLC method) monitoring reaction is to complete Afterwards, the reaction solution is extracted...

Embodiment 2

[0054] Embodiment 2: the synthesis of ibuprofen-heparin conjugate

[0055] Take 10mmol ibuprofen, 16mmol dicyclohexylcarbodiimide (DCC), and 16mmol hydroxysuccinimide (NHS), dissolve them in 20ml N, N-dimethylformamide, keep away from light, under the protection of nitrogen, and place in an ice bath Reacted for 45min, then rose to room temperature for 24h. After the reaction, the precipitate was filtered off, and a large amount of ethyl acetate was added to wash the precipitate. The filtrate was extracted, the ethyl acetate layers were combined, and the solvent was removed by rotary evaporation to obtain the activated intermediate ester of ibuprofen. Dissolve 2mmol of ciprofloxacin activated intermediate ester in 10ml of dichloromethane, slowly drop into the dichloromethane solution of 5mmol / ml ethylenediamine under ice-bath conditions, and monitor the reaction by thin layer chromatography (TLC method) to After completion, the reaction solution is extracted, the organic laye...

Embodiment 3

[0056] Example 3: Synthesis of diclofenac-hyaluronic acid conjugates

[0057] Take 10mmol of diclofenac, 15mmol of dicyclohexylcarbodiimide (DCC), and 15mmol of hydroxysuccinimide (NHS), dissolve them in 25ml of dimethyl sulfoxide, keep away from light, and react in an ice bath for 40min under the protection of nitrogen, then rise to Reaction at room temperature for 24h. After the reaction, the precipitate was filtered off, and a large amount of ethyl acetate was added to wash the precipitate. The filtrate was extracted, the ethyl acetate layers were combined, and the solvent was removed by rotary evaporation to obtain the activated intermediate ester of diclofenac. Dissolve 3mmol of diclofenac activated intermediate ester in 25ml of dichloromethane, slowly drop into the dichloromethane solution of 5mmol / ml ethylenediamine under ice-bath conditions, and monitor the reaction by thin layer chromatography (TLC method) until complete, The reaction liquid is extracted, the organi...

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Abstract

The invention discloses an anti-inflammatory drug (polysaccharide conjugate) as well as preparation and application of a drug composition thereof. The anti-inflammatory drug composition comprises an anti-inflammatory drug (polysaccharide conjugate) and slow-acting antirheumatic drugs. The anti-inflammatory drug (polysaccharide conjugate) has amphipathic characteristics by using alkylene diamines as a connecting arm and introducing hydrophobic non-steroidal anti-inflammatory drugs containing carbonyl on a polysaccharide framework, and is self-assembled to form a nano micelle in water, thereby physically coating the antirheumatic drugs, combining the chemically coupled non-steroidal anti-inflammatory drugs, and achieving the effect of combination treatment on the rheumatoid arthritis. The conjugate and the drug composition have high safety and good treatment effect, and can be used for injection, oral administration or external drug administration.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an anti-inflammatory drug-polysaccharide conjugate with good anti-inflammatory activity and biodegradability as a drug carrier for combined therapy. The invention also relates to a preparation method of the conjugate and a drug combination thereof application of things. Background technique [0002] Rheumatoid arthritis is an autoimmune disease of unknown etiology. Treatment methods include drug therapy, surgical treatment, and psychotherapy, etc., and drug therapy is generally the main method. Antirheumatic drugs can be divided into four major categories: NSAIDs, disease-modifying antirheumatic drugs, corticosteroids, and botanicals. [0003] Studies have shown that no single drug can both relieve symptoms and improve the condition, nor can it be used alone for a long time. For example, non-steroidal anti-inflammatory drugs such as ibuprofen and indomethacin have good...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K45/00A61K45/06A61P29/00A61P19/02A61P19/04A61K47/61
Inventor 周建平姚静侯琳
Owner CHINA PHARM UNIV
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