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Diclofenac-glycine-resveratrol conjugate, preparation method and application

A technology of diclofenac and resveratrol, which is applied in the direction of drug combinations, pharmaceutical formulas, active ingredients of hydroxyl compounds, etc., can solve the problems of complex reaction steps, unfavorable industrial production, long reaction time, etc., achieve fewer steps and quickly exert drug effects , The effect of fast hydrolysis speed

Active Publication Date: 2019-06-07
药大制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But its reaction step is complicated, and reaction time is long, is unfavorable for industrialized production

Method used

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  • Diclofenac-glycine-resveratrol conjugate, preparation method and application
  • Diclofenac-glycine-resveratrol conjugate, preparation method and application
  • Diclofenac-glycine-resveratrol conjugate, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1: the preparation of diclofenac

[0030] Add 20 g of diclofenac sodium into 400 ml of distilled water, heat and stir to dissolve it completely, slowly add 3 mol / L HCl solution dropwise, and a white solid precipitates out. Cool to room temperature, filter with suction, wash the precipitate with water, and dry to obtain diclofenac.

Embodiment 2

[0031] Embodiment 2: the preparation of diclofenac-glycine

[0032] Dissolve diclofenac (5g) in N,N-dimethylformamide, after complete dissolution, add 115mg N-hydroxysuccinimide (NHS), 100mg N,N dicyclohexylcarboimide (DCC), and react at room temperature for 2h . Dissolve 1.27g of glycine in 10mL of saturated sodium bicarbonate solution, then drop it into the reaction solution, and continue the reaction for 6h. After the reaction was completed, the solvent was removed by rotary evaporation, 50 mL of ether was added to the residue, cooled until the precipitate was completely precipitated, and the precipitate was obtained by filtration, which was the diclofenac-glycine product.

Embodiment 3

[0033] Embodiment 3: Preparation of diclofenac-glycine-resveratrol

[0034] Diclofenac-glycine (3.0 g), dissolved in 20 mL of dichloromethane. To the above solution was added 84 mg of 4-dimethylaminopyridine (DMAP) and 310 mg of N,N-dicyclohexylcarbodiimide (DCC). After stirring for 0.5h, 1.94g of resveratrol was added and reacted for 6h. After the reaction is completed, the solvent is removed by rotary evaporation, and the aqueous solution is lyophilized to obtain a diclofenac-glycine-resveratrol product.

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PUM

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Abstract

The invention discloses a diclofenac-glycine-resveratrol conjugate, a preparation method and an application. The conjugate is formed by coupling glycine serving as a linking arm with diclofenac and resveratrol respectively; diclofenac and glycine are linked by an amido bond; a diclofenac-glycine conjugate is linked with resveratrol by multiple sites of ester bonds. Due to introduction of glycine,the solubility of the conjugate is increased, due to introduction of diclofenac and resveratrol, the anti-arthritis effect of the conjugate is significantly enhanced, adverse reactions are reduced, and safety is higher. The synthesis method of the conjugate is simple and suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a conjugate synthesized from diclofenac and resveratrol with stronger drug properties and higher solubility, and also relates to a synthesis method and application of the conjugate. Background technique [0002] Diclofenac sodium (Diclofenac sodium) is a non-steroidal anti-inflammatory drug derived from phenylacetic acid, mainly used for the treatment of osteoarthritis, rheumatoid arthritis, polymyositis, dermatomyositis, spondyloarthropathies, Spondylitis, gout, and conditions requiring acute pain relief such as migraine, toothache, gallstones, and kidney stones. Medicinal diclofenac often uses sodium salt or potassium salt. In China, the sodium salt is the main one, that is, diclofenac sodium. However, diclofenac sodium is more irritating, and the main adverse reaction is gastrointestinal reaction, manifested as gastrointestinal irritation symptoms, such as nausea, vomiting, diarrhea, ab...

Claims

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Application Information

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IPC IPC(8): A61K47/54A61K47/55A61K31/05A61K31/196A61P19/02A61P29/00
Inventor 郝静梅霍美蓉陶琳琳
Owner 药大制药有限公司
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