Synthesis, Characterization and Comparison of Local Analgesic, Anti-Inflammatory, Anti-Ulcerogenic Activity of Copper and Zinc Complexes of Indomethacin
2017
Background: Non-steroidal anti-inflammatory drugs (NSAID) exert gastrointestinal
upset by inhibiting mucosal cyclooxygenase (COX) activity and complexation technique
with metals has been adopted to overcome this drawback.
Objective: The study aimed to overcome the gastrointestinal side effects associated with indomethacin
treatment by synthesizing copper (Cu) and zinc (Zn) complexes of indomethacin
along with assessing potential pharmacological effects of these complexes.
Method: The characterization of synthesized complexes was done by FT-IR, XRD, UV-Vis,
Atomic Absorption Spectroscopy (AAS) and Differential Scanning Calorimetry (DSC).
Biological properties as local analgesic activity, anti-inflammatory activity and antiulcerogenic
activity were evaluated following radiant heat tail flick, inhibition of rat hind
paw edema and inhibition of NSAID induced gastroenteropathy method respectively.
Results: 0.3 ml of indomethacin-copper complex demonstrated prominent analgesia at 25
µg/ml dose and 0.3 ml of indomethacin-zinc complex, after 30, 60 and 90 minutes of oral
administration, shown significant local analgesia at 25, 50 and 100 µg/ml dose. In antiinflammatory
activity assay, indomethacin-copper exhibited significant inhibition at 20
mg/kg dose after 2nd, 3rd and 4th hour of administration whereas indomethacin-zinc illustrated
significant inhibition at 10 mg/kg dose after 2nd, 3rd and 4th hour of administration.
Anti-ulcerogenic activity study of the complexes exhibited no macroscopic damage to the
stomach and intestine, except minor microscopic damage.
Conclusion: In view of the results, the copper and zinc complexes of indomethacin may be
used as better substitutes of the parent indomethacin owing to their minimal side effects
with additional pharmacological effects.
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