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In vitro kinetic study of donepezil N- oxide metabolites | ||
| Iraqi Journal of Pharmacy | ||
| Article 1, Volume 11, Issue 2, 2011, Pages 93-101 PDF (0 K) | ||
| DOI: 10.33899/iphr.2011.49912 | ||
| Authors | ||
| Faris T. Abachi; Ammar B. Behnan; Riyath A. Atto | ||
| Abstract | ||
| Objective: The aim of this study was to examine the metabolism of donepezil via N – oxidation of donepezil HCl in vitro, and the kinetic studies at a temperature similar to that of the human body. Methods: Direct reaction of donepezil with hydrogen peroxide and formic acid at room temperature, the N – oxide undergoes a series of rearrangements, the reaction was followed by ultraviolet at λmax= 268 nm at 37 °C. The donepezil N- oxide was also tested as potential cholinesterase inhibitor using electrometric for cholinesterase determination. Results: According to the present work , the structure of donepzil N- oxide was elucidated using spectroscopic analysis , also , in vitro kinetic study at 37 °C using ultraviolet spectrophotometer at λmax = 268 nm showed that the reaction proceeded at a first order reaction . Biologically, the compound was found to inhibit both plasma and erythrocyte cholinesterase activities in vitro .. Conclusion: We concluded that the N- oxide of denepezil undergoes a series of rearrangements, the reaction followed first order at 37 °C. It has a potential anticholinesterase activity | ||
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