Topical Oral Cavity Pharmacokinetic Modeling of a Stannous Fluoride Dentifrice: An Unusual Two Compartment Model

Scott, Douglas C.; Coggan, John; Cruze, Charles A.; He, Tao; Johnson, Robert D.

doi:10.1002/jps.21691

Cited by 10 publications

(11 citation statements)

References 19 publications

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“…It also begs the question as to the nature of Sn 2+ bound to dental biofilm. Its retention profile in dental biofilms [Scott et al, 2009], especially in comparison to that of fluoride [Newby et al, 2013], suggests that once delivered to a biofilm it is firmly retained and therefore unlikely to be in an ionic state. In conclusion, no synergy between Sn 2+ and fluoride was observed, yet there were interactions as Sn 2+ modulated the effect of fluoride.…”

Section: Discussionmentioning

confidence: 99%

“…The chosen fluoride concentration is representative of that found in plaque fluid several hours after the application of a 48-m M fluoride rinse (as NaF) [Ekstrand, 1997]. The studied Sn 2+ concentrations were based on the range observed in whole plaque after the application of a toothpaste containing stannous fluoride [Scott et al, 2009]. A mechanistic approach (constant composition, acidic gels to mimic biofilm fluid) was chosen to allow for more concrete conclusions about Sn 2+ effects on de-and remineralization to be drawn that would not be possible using pH cycling models where both de-and remineralization challenges occur.…”

Section: Discussionmentioning

confidence: 99%

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Mechanistic Observations on the Role of the Stannous Ion in Caries Lesion De- and Remineralization

Lippert

2016

Caries Res

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Two mechanistic, laboratory, factorial design studies were conducted to investigate the effect of the stannous ion (Sn²⁺) in the absence or presence of fluoride on caries lesion de- and remineralization. Study I was concerned with determining changes in mineral distribution of subsurface lesions, whereas study II investigated changes in surface hardness of surface-softened lesions as a function of pH. Study I showed that Sn²⁺ modulates the effects of fluoride by preventing lamination. Study II revealed that the effect of Sn²⁺ on rehardening is pH dependent. Neither study demonstrated synergy between Sn²⁺ and fluoride, yet interactions were observed. Sn²⁺ does interfere with remineralization to some extent although it provided acid resistance. The role of Sn²⁺ in the caries process is complex.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Mechanistic Observations on the Role of the Stannous Ion in Caries Lesion De- and Remineralization

Lippert

2016

Caries Res

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“…For example, the half-lives of the initial rapid clearance phase for each of the 0.026 mol/l NaF rinses, t 1/2 (1) = ln2/α, are 3.2, 3.7 and 4.2 min for the additive-free rinse, the rinse with added NaCl and the rinse with added sucrose, respectively. Corresponding half-lives for other substances where a two-compartment salivary clearance model has been applied are 4.6 min, tin [Scott et al, 2009]; 4.3-4.8 min, triclosan [Creeth et al, 1993]; and 5.3 min, zinc [Creeth et al, 1993]. All these data are close to, but less than, values obtained by Sreebny et al [1985] for the 'unstimulated saliva' clearance phase for the non-binding molecules glucose and sucrose of 6.9 and 7.7 min, respectively, reflecting what is a common salivary 'wash-out' phase.…”

Section: Discussionmentioning

confidence: 99%

On the Relationship between the Rate of Salivary Flow and Salivary Fluoride Clearance

Duckworth

Jones²

2015

Caries Res

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The amount of fluoride retained in the mouth following the application of dentifrices, mouthwashes, etc. may be important in determining their anticaries efficacy. In this study we investigated the relationship between the salivary flow rate and salivary fluoride clearance. Ten adults tested six mouthrinses, consisting of aqueous sodium fluoride solutions (0.013, 0.026 mol/l) with and without added sodium chloride (1.28 mol/l) or sucrose (0.44 mol/l), in a randomised order. Prior to each test, subjects swallowed, rinsed for 2 min with 2 ml water and then expectorated into a preweighed container to obtain a measure of initial saliva flow rate. Next, the procedure was repeated using one of the test rinses. Finally, samples of unstimulated whole saliva were collected for up to 3 h after each mouthrinse application and analysed for fluoride. Salivary fluoride concentrations were significantly lower after application of mouthrinses that contained either sucrose or NaCl, both of which compounds markedly enhanced salivary flow, than after the use of corresponding mouthrinses without any additive. Area under the salivary fluoride clearance curve (AUC) values were inversely correlated with salivary flow rate on an individual basis (p < 0.01). The observed behaviour could not be completely attributed to treatment dilution by saliva at the time of application.

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“…Also worth noting are corresponding values for the half-life of the initial rapid phase of salivary clearance, where a two-compartment model has been applied: 4.6 min, tin [70]; 4.3-4.8 min, triclosan [69]; 5.3 min, zinc [69]. Corresponding values for fluoride are not dissimilar: 6.5-9.1 min for Na 2 FPO 3 toothpaste [14] and 2.9-4.1 min for NaF solution [58].…”

Section: Other Active Ingredientsmentioning

confidence: 99%

“…The clearance kinetics of substantive agents has been modelled by both single phase [65][66][67] and dual phase approaches [68][69][70]. Data for various active ingredients are listed in table 2.…”

Section: Other Active Ingredientsmentioning

confidence: 99%

Pharmacokinetics in the Oral Cavity: Fluoride and Other Active Ingredients

Duckworth¹

2013

Monographs in Oral Science

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Modern commercial toothpastes contain therapeutic ingredients to combat various oral conditions, for example, caries, gingivitis, calculus and tooth stain. The efficient delivery and retention of such ingredients in the mouth is essential for good performance. The aim of this chapter is to review the literature on the oral pharmacokinetics of, primarily, fluoride but also other active ingredients, mainly anti-plaque agents. Elevated levels of fluoride have been found in saliva, plaque and the oral soft tissues after use of fluoridated toothpaste, which persist at potentially active concentrations for hours. Both experiment and mathematical modelling suggest that the soft tissues are the main oral reservoir for fluoride. Qualitatively similar observations have been made for anti-plaque agents such as triclosan and metal cations, though their oral substantivity is generally greater. Scope for improved retention and subsequent efficacy exists.

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Topical Oral Cavity Pharmacokinetic Modeling of a Stannous Fluoride Dentifrice: An Unusual Two Compartment Model

Cited by 10 publications

References 19 publications

Mechanistic Observations on the Role of the Stannous Ion in Caries Lesion De- and Remineralization

Mechanistic Observations on the Role of the Stannous Ion in Caries Lesion De- and Remineralization

On the Relationship between the Rate of Salivary Flow and Salivary Fluoride Clearance

Pharmacokinetics in the Oral Cavity: Fluoride and Other Active Ingredients

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