Diclofenac zinc complex and its preparation method and use

A technology of zinc diclofenac and sodium diclofenac, which is applied in the directions of zinc organic compounds, pharmaceutical formulations, and medical preparations containing active ingredients, can solve the problems of gastrointestinal side effects of diclofenac, and achieve the effects of good anti-inflammatory activity and low gastric side effects.

Inactive Publication Date: 2017-07-28
SHANDONG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But like other NSAIDs, diclofenac has very serious gastrointestinal side effects

Method used

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  • Diclofenac zinc complex and its preparation method and use
  • Diclofenac zinc complex and its preparation method and use
  • Diclofenac zinc complex and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1: Preparation of a zinc complex (complex 1) with diclofenac and tetramethylethylenediamine as ligands.

[0020] Preparation of diclofenac sodium solution (0.1mmol / mL ethanol): Accurately weigh 31.8g (10mmol) of diclofenac sodium and dissolve in 100mL ethanol. Preparation of zinc acetate solution (0.1mmol / mL ethanol): Accurately weigh 2.19g (10mmol) of zinc acetate and dissolve in 100mL ethanol. Preparation of tetramethylethylenediamine solution (1mmol / mL ethanol): Accurately weigh 1.1621g of tetramethylethylenediamine and dissolve in 10mL ethanol. Accurately measure 10 mL of diclofenac sodium solution (0.1 mmol / mL ethanol) and 5 mL of ZnAc solution (0.1 mmol / mL ethanol) in a beaker, add ethanol to 60 mL, stir at room temperature for 5 minutes, then dropwise add tetramethylethylenediamine solution ( 1mmol / mL ethanol) 0.5mL, sealed with a parafilm, pierced with a toothpick, placed at room temperature and slowly volatilized, after a few days, colorless transparen...

Embodiment 2

[0023] Example 2: Preparation of a zinc complex (complex 2) using diclofenac and 1,3-propanediamine as ligands.

[0024] Preparation of diclofenac sodium solution (0.1 mmol / mL methanol): Accurately weigh 3.18 g (10 mmol) of diclofenac sodium and dissolve in 100 mL methanol. Preparation of 0.1mmol / mL zinc acetate solution (0.1mmol / mL methanol): Accurately weigh 2.19g (10mmol) of zinc acetate and dissolve in 100mL methanol. Preparation of 1,3-propylenediamine solution (1mmol / mL methanol): Accurately weigh 0.74g (10mmol) of 1,3-propylenediamine and dissolve it in 10mL methanol. Accurately measure 1.5mL of diclofenac sodium solution (0.1mmol / mL methanol) and 0.75mL of ZnAc solution (0.1mmol / mL methanol) in a heating kettle, then dropwise add 75ul of 1,3-propanediamine solution (1mmol / mL methanol) , add methanol to a total volume of 10mL, keep warm in a 75°C drying oven for two days, filter the mixture with filter paper, put the filtrate into a small beaker, seal the beaker with p...

Embodiment 3

[0030] Example 3: Study on anti-inflammatory and gastric side effects of diclofenac zinc complex

[0031] 1 Experimental materials and methods

[0032] 1.1 Drugs and reagents

[0033] Sodium Chloride Diclofenac Sodium CMC-Na Carrageenan Formaldehyde

[0034] 1.2 Experimental animals

[0035] SD rat

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Abstract

The invention relates to two diclofenac zinc complexes with anti-inflammatory activity and a preparation method thereof, belonging to the technical fields of complex synthesis and medicinal chemistry. Of the two complexes provided by the present invention, complex 1 is a 6-coordinated mononuclear structure, and each complex molecule contains 2 molecules of deprotonated diclofenac, 1 molecule of tetramethylethylenediamine and a zinc ion. Complex 2 is a 6-coordinate mononuclear structure, and each complex molecule contains 2 molecules of deprotonated diclofenac, 1 molecule of 1,3‑propylenediamine and a zinc ion. After testing, it was found that the complexes 1 and 2 of the present invention achieved 52.24% ± 1.33% and 54.88% ± 5.5% respectively, and the gastric ulcer index was 4.75 ± 0.95 and 11.8 ± 2.179 respectively, and diclofenac sodium The inhibition rate to rat paw swelling is 36.08%, and the gastric ulcer index is 24.4. In contrast, the two complexes of the present invention have better anti-inflammatory activity and lower gastric side effects, and can be used to prepare anti-inflammatory drugs.

Description

technical field [0001] The invention relates to two diclofenac zinc complexes with anti-inflammatory activity and a preparation method thereof, belonging to the technical fields of complex synthesis and medicinal chemistry. Background technique [0002] Non-steroidal anti-inflammatory drugs (NSAIDs) are one of the most widely used drugs in the world. These drugs do not contain the steroidal structure of corticosteroid anti-inflammatory drugs, so they are called NSAIDs. Diclofenac is a widely used NSAIDs. It exerts its pharmacological effects by inhibiting the synthesis of the prostate. It has anti-rheumatic, anti-inflammatory, analgesic and antipyretic effects. It is clinically used in the treatment of rheumatism and rheumatoid arthritis. But like other NSAIDs, diclofenac has very serious gastrointestinal side effects. Literature data show that after some non-steroidal anti-inflammatory drugs form complexes with metal ions, the anti-inflammatory, analgesic and antipyretic ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F3/06A61K31/315A61P29/00
CPCC07F3/003
Inventor 盛桂华王存芳胡晓明闫凯陈相飞李珍李健朱海亮
Owner SHANDONG UNIV OF TECH
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