Topical oral cavity pharmacokinetic modeling of a stannous fluoride dentifrice: an unusual two compartment model

A pharmacokinetic model was developed describing the pharmacokinetics of stannous fluoride in human subjects after oral topical application of a stannous fluoride dentifrice. Twenty subjects participated in an investigation of an experimental dentifrice. Subjects rinsed their mouths with the experim...

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Veröffentlicht in:Journal of pharmaceutical sciences Jg. 98; H. 10; S. 3862
Hauptverfasser: Scott, Douglas C, Coggan, John W, Cruze, Charles A, He, Tao, Johnson, Robert D
Format: Journal Article
Sprache:Englisch
Veröffentlicht: United States 01.10.2009
Schlagworte:
Algorithms
Dental Caries - prevention & control
Dental Plaque - metabolism
Dentifrices - administration & dosage
Dentifrices - pharmacokinetics
Dentifrices - therapeutic use
Fluorides, Topical - administration & dosage
Fluorides, Topical - pharmacokinetics
Fluorides, Topical - therapeutic use
Half-Life
Humans
Models, Biological
Mouthwashes
Saliva - metabolism
Tin - pharmacokinetics
Tin Fluorides - administration & dosage
Tin Fluorides - pharmacokinetics
Tin Fluorides - therapeutic use
ISSN:1520-6017, 1520-6017
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Zusammenfassung:A pharmacokinetic model was developed describing the pharmacokinetics of stannous fluoride in human subjects after oral topical application of a stannous fluoride dentifrice. Twenty subjects participated in an investigation of an experimental dentifrice. Subjects rinsed their mouths with the experimental dentifrice slurry. Saliva and plaque samples were obtained from the subjects at various times up to 6 h after administration. Samples were analyzed for total tin content, used as an analytical marker for the active stannous fluoride ingredient, using a graphite furnace atomic absorption spectrometer. The modeling indicates that there is an obvious kinetic relationship between saliva and plaque compartments and that stannous fluoride is very well retained in and slowly released from plaque (and oral surfaces) into saliva. Additionally, both compartments are simultaneously loaded during administration unlike typical systemic drug behavior, and the elimination rate "constant" from the central compartment (saliva) changes due to changes in salivary flow. Stannous fluoride is cleared from saliva rapidly but very well retained in gingival plaque. The model with simultaneous loading of plaque and saliva describes these observations and may account for the prolonged antiplaque and antigingivitis benefits of stannous fluoride.
Bibliographie:ObjectType-Article-1
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ISSN:1520-6017
1520-6017
DOI:10.1002/jps.21691