Bioavailability of fluoride administered as sodium fluoride or monofluorophosphate to humans

Abstract

A double-bind cross-over study was conducted on four healthy subjects, aged 19–29 years, in order to determine the relative bioavailability and other pharmacokinetics features of fluoride (F) after single oral administration in fasting conditions of 2 mg F as sodium F (NaF) or sodium monofluorophosphate (MFP). The bioavailability was evaluated on the basis of the plasma levels and of the urinary excretion of F. Blood was sampled before and during the 8 h after the administration of the test solutions. For F excretion urine was sampled 12 h before the study and over the 8 h after the administration. Data were tested for statistically significant differences by ANOVA and Tukey's post hoc tests, and also by Student's t-test ( p < 0.05). For the two formulations, the pharmacokinetics of F in plasma was characterized by a rapid absorption and by a peak ( C max = 0.1 μg/mL) which was reached 20 min after administration, followed by a biphasic elimination. In the 8 h following the administration the urinary excretion of F accounted for 35–41% of the administered dose, without significant differences between the two formulations. The AUCs (±S.D.) for NaF and MFP were 21.15 (±0.58) and 19.04 (±1.75) min μg mL −1, respectively, and were not significantly different ( p = 0.079). Based on the AUC and C max of F in plasma and on the urinary excretion of F during the 8 h following administration, the relative bioavailabilities of the two F formulations were equivalent.