Concentrations of metronidazole in human plasma and saliva after tablet or gel administration

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Processo FAPESP: 06/01492-0

Processo FAPESP: 06/0898-9

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.MethodsIn this randomized cross-over study with a 1-week washout period, 13 volunteers randomly received one (a single oral dose of 750mg Mtz (Flagyl (R) - tablet) and 2) 3g 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 48h (AUC(0-48)) and from 0 to infinity (AUC(0-)), the maximum plasma concentration (C-max), the time to C-max, volume of distribution and renal clearance were determined for Mtz tablet.Key findingsConsidering the Mtz tablet, plasma showed higher Mtz concentration from 6 to 24h after drug administration and the highest values concerning AUC(0-48h) and AUC(0-) than those obtained in saliva (P<0.05). No significant differences were observed between plasma and saliva concentrations for Mtz gel.ConclusionsThe 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.