Concentrations of metronidazole in human plasma and saliva after tablet or gel administration. (6th November 2013)

• Record Type: Journal Article
• Authors: de C Bergamaschi, Cristiane; Berto, Luciana A; Venâncio, Paulo C; Cogo, Karina; Franz-Montan, Michelle; Motta, Rogério H L; Santamaria, Mauro P; Groppo, Francisco C
• Is Part Of: Journal of pharmacy and pharmacology. Volume 66:Number 1(2014:Jan.)
• Page Start: 40
• Page End: 47
• Publication Date: 2013-11-06
• Subjects: gel -- metronidazole -- plasma -- saliva -- tablet; Pharmacy -- Periodicals; Pharmacology -- Periodicals; 615.1
• DOI: 10.1111/jphp.12161
• Languages: English
• ISSNs: 0022-3573

Abstract

Abstract: Objectives: 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. Methods: 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. Key findings: 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. Conclusions: 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.