A 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: 2022-06-07
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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  • A diclofenac-glycine-resveratrol conjugate, preparation method and application
  • A diclofenac-glycine-resveratrol conjugate, preparation method and application
  • A diclofenac-glycine-resveratrol conjugate, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1: Preparation of Diclofenac

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

Embodiment 2

[0031] Example 2: Preparation of Diclofenac-Glycine

[0032] Dissolve diclofenac (5g) in N,N-dimethylformamide, after complete dissolution, add 115mg N-hydroxysuccinimide (NHS), 100mg N,N dicyclohexylcarbimide (DCC), and react at room temperature for 2h . 1.27 g of glycine was dissolved in 10 mL of saturated sodium bicarbonate solution, and then added dropwise to the reaction solution, and the reaction was continued for 6 h. 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] Example 3: Preparation of Diclofenac-Glycine-Resveratrol

[0034] Diclofenac-glycine (3.0 g) was dissolved in 20 mL of dichloromethane. To the above solution were 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 to react for 6h. After the reaction is completed, the solvent is removed by rotary evaporation, and the aqueous solution is subjected to freeze-drying treatment 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 uses glycine as a connecting arm, and is respectively coupled with diclofenac and resveratrol; the diclofenac and glycine are connected through an amide bond; and the diclofenac-glycine conjugate is connected with resveratrol at multiple sites through an ester bond. Due to the introduction of glycine, the solubility of the conjugate increases, and the introduction of diclofenac and resveratrol significantly enhances the anti-arthritis effect of the conjugate, reduces adverse reactions, and has higher safety; the synthesis method of the conjugate is simple and suitable for industrialization Production.

Description

technical field [0001] The invention belongs to the field of pharmacy, relates to a synthetic conjugate of diclofenac and resveratrol with stronger medicinal properties and higher solubility, and also relates to a synthetic method and application of the conjugate. Background technique [0002] Diclofenac sodium is a non-steroidal anti-inflammatory drug derived from phenylacetic acid, mainly used for the treatment of osteoarthritis, rheumatoid arthritis, polymyositis, dermatomyositis, spondyloarthropathy, ankylosing Spondylitis, gout, and conditions such as migraines, toothaches, gallstones, and kidney stones that require acute pain relief. Medicinal diclofenac often uses sodium salt or potassium salt, mainly sodium salt in China, namely diclofenac sodium. However, diclofenac sodium is more irritating, and the main adverse reactions are gastrointestinal reactions, manifested as gastrointestinal irritation symptoms, such as nausea, vomiting, diarrhea, abdominal cramps, indige...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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