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J Pharm Pharmacol ; 66(1): 40-7, 2014 Jan.
Article in English | MEDLINE | ID: mdl-24341948

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 (C(max)), the time to C(max), 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 AUC0-48 h 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.


Subject(s)
Gels/administration & dosage , Metronidazole/administration & dosage , Metronidazole/blood , Saliva/metabolism , Tablets/administration & dosage , Administration, Oral , Adult , Area Under Curve , Cross-Over Studies , Gels/pharmacokinetics , Humans , Male , Metronidazole/pharmacokinetics , Tablets/pharmacokinetics
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