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Pharmacokinetics of fluoride in man after single and multiple oral doses
Authors:J. Ekstrand  G. Alván  L. O. Boréus  A. Norlin
Affiliation:(1) Department of Pharmacology and Cariology, Karolinska Institute, Stockholm, Sweden;(2) Department of Clinical Pharmacology, Karolinska Hospital, Stockholm, Sweden;(3) Department of Clinical Pharmacology, Huddinge Hospital, Stockholm, Sweden
Abstract:
Summary The doses of fluoride (F) recommended in the literature for caries prevention and for the treatment of osteoporosis vary. This partly reflects inadequate knowledge of F pharmacokinetics. In the present study various single and multiple oral doses of F were given to eight volunteers, who had a strictly controlled F intake in the diet. The resulting plasma and parotid saliva concentrations as well as urinary output of F were measured. The plasma data fitted a two-compartment open model with a beta-slope half-life ranging between 2 and 9 h. Plasma clearance was 0.15±0.02 (SD) liter/kg/h. Data from the highest dose (10 mg) were fitted to both two- and three-compartment models, and there was no significant difference between them. Multiple doses of F 3.0 or 4.5 mg yielded steady state concentrations ranging from 54 to 145 ng/ml. About 50 per cent of the given dose was recovered in the urine, which is indicative of considerable accumulation in the body. The saliva F/plasma F concentration ratio was 0.64 with a coefficient of variation of 5%.
Keywords:Fluoride  single- and multiple dose kinetics  plasma concentration  urinary excretion  saliva/plasma concentration ratio
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