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
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
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...
PUM
Property | Measurement | Unit |
---|---|---|
Particle size | aaaaa | aaaaa |
Abstract
Description
Claims
Application Information
- R&D Engineer
- R&D Manager
- IP Professional
- Industry Leading Data Capabilities
- Powerful AI technology
- Patent DNA Extraction
Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.
© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com