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.
CN104761576BInactive Publication Date: 2017-07-28SHANDONG UNIV OF TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHANDONG UNIV OF TECH
Publication Date
2017-07-28
Estimated Expiration
Not applicable · inactive patent

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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.
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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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