Concentrations of metronidazole in human plasma and saliva after tablet or gel administration
Article first published online: 6 NOV 2013
© 2013 Royal Pharmaceutical Society
Journal of Pharmacy and Pharmacology
Volume 66, Issue 1, pages 40–47, January 2014
How to Cite
de C. Bergamaschi, C., Berto, L. A., Venâncio, P. C., Cogo, K., Franz-Montan, M., Motta, R. H.L., Santamaria, M. P. and Groppo, F. C. (2014), Concentrations of metronidazole in human plasma and saliva after tablet or gel administration. Journal of Pharmacy and Pharmacology, 66: 40–47. doi: 10.1111/jphp.12161
- Issue published online: 17 DEC 2013
- Article first published online: 6 NOV 2013
- Manuscript Accepted: 16 SEP 2013
- Manuscript Received: 7 MAY 2013
- São Paulo Research Foundation (FAPESP). Grant Numbers: #2006/01492-0, #2006/0898-9
The aim of this study was to determine the pharmacokinetic profile of metronidazole (Mtz) tablet and to compare Mtz gel and tablet concentrations in both blood plasma and saliva.
In this randomized cross-over study with a 1-week washout period, 13 volunteers randomly received one (a single oral dose of 750 mg Mtz (Flagyl® – tablet) and 2) 3 g of 15% Mtz benzoate gel (applied by using a dental tray). The HPLC with ultraviolet detection was used to quantify plasma and saliva concentrations of Mtz. The pharmacokinetic parameters (PPs) areas under the curves from 0 to 48 h (AUC0–48) and from 0 to infinity (AUC0–∞), the maximum plasma concentration (Cmax), the time to Cmax, volume of distribution and renal clearance were determined for Mtz tablet.
Considering the Mtz tablet, plasma showed higher Mtz concentration from 6 to 24 h after drug administration and the highest values concerning AUC0–48h and AUC0–∞ than those obtained in saliva (P < 0.05). No significant differences were observed between plasma and saliva concentrations for Mtz gel.
The study showed that some PPs were higher in plasma (P < 0.05) than in saliva concerning Mtz tablet. Gel formulation had similar Mtz bioavailability in plasma and saliva resulting in systemic absorption.