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Sci. Pharm. 2010, 78(3), 465-472; doi:10.3797/scipharm.1003-10

Effect of Itraconazole on the Pharmacokinetics of Diclofenac in Beagle Dogs

Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia
Received: 13 March 2010 / Accepted: 19 May 2010 / Published: 19 May 2010
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Abstract

The objective of this study was to investigate the potential effect of itraconazole on the pharmacokinetics of diclofenac potassium in beagle dogs after oral coadministration. Five male beagle dogs received a single oral 50 mg dose of diclofenac potassium alone in phase I, and along with a single oral 100 mg dose of itraconazole in phase II. Blood samples obtained for 8.0 hours post dose were analysed for diclofenac concentration using a validated high performance liquid chromatography (HPLC) assay method. The area under plasma concentration-time curve (AUC0–∞), maximum plasma concentration (Cmax), time to reach Cmax (Tmax) and elimination half-life (t1/2), were calculated for diclofenac before and after itraconazole administration. The coadministration of itraconazole with diclofenac potassium has resulted in a significant reduction in AUC0–∞ and Cmax of diclofenac, which was about 31 and 42%; respectively. No statistically significant differences were observed for Tmax and t1/2 of diclofenac between the two phases. Therefore, it could be concluded that oral coadministration of itraconazole may have the potential to affect the absorption of diclofenac as indicated by the significant reduction in its AUC and Cmax in beagle dogs.
Keywords: Interaction; Pharmacokinetic parameters; Plasma concentration; Absorption; HPLC Interaction; Pharmacokinetic parameters; Plasma concentration; Absorption; HPLC
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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AL-JENOOBI, F.I. Effect of Itraconazole on the Pharmacokinetics of Diclofenac in Beagle Dogs. Sci. Pharm. 2010, 78, 465-472.

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