DS125-2019

Products for clinical remineralization:

Over the counter fluoride products
- effectiveness and composition

Peter Rechmann
Peter.Rechmann@ucsf.edu
University of California San Francisco

Course Objectives
1. to know the various forms of fluoride
delivery for home use and office use,
including the ADA recommendations for
office topical applications
2. to understand the limitations of
formulating fluoride products to make
them effective
 Protective Factors

Numerous clinical trials showed ~30% reduction

with fluoride toothpaste 1000-2800 ppm F.
Curnow, Pine, et al, 2002 reported 56% reduction
with supervised brushing 2 x daily with a 1000 ppm
F toothpaste compared with unsupervised

Brushing twice daily with

a fluoride-containing
toothpaste is one of the
most effective ways to
control dental decay.

But - High bacterial

challenge overcomes the
therapeutic effects of
fluoride.

Sodium Fluoride

Stannous Fluoride

Sodium Fluoride
plus multiple

Sodium Fluoride +
Baking Soda

Sodium Fluoride +
Whitening
Over the counter fluoride rinses (0.05% NaF) are
effective in moderate caries risk patients: twice daily for
one minute, plus a fluoride-containing dentifrice.
O’Reilly and Featherstone, 1987
 Q: How often should we recommend
brushing with a fluoride toothpaste?

u Once a week
u Every two days
u At least once a day
u At least twice a day
u Four times a day

Products for clinical

remineralization:
Over the counter fluoride product
effectiveness and composition

Brushing at least
twice daily with a
fluoride-containing
toothpaste is one of
the most effective
ways to control
dental decay.
High bacterial
challenge overcomes
the therapeutic
effects of fluoride.
Over the counter fluoride rinses (0.05% NaF, ~220 ppm F)
are very effective when used once or twice daily for one
minute, plus a fluoride-containing toothpaste.

Whole Saliva F Conc. (µmol/L)

Gel, 5000 ppm

Rinse, 225 ppm

Toothpaste,
1100 ppm

Toothpaste,
<1 ppm

1 µmol/L = 0.02 ppm F Time

Zero et al, J Dent Res 1992

Fluoride from Dentifrice or

Mouth Rinse
u Initial high concentration in whole
saliva and plaque which takes 1-6 hours
to fall to baseline
u Baseline concentrations in whole saliva
are elevated and maintained at 0.04 - 0.1
ppm, depending on the subject
u These levels are sufficient to enhance
remineralization
 Protective Factors

Orthodontic brackets attract cariogenic bacteria,

leading to “white spot lesions” - early decay

Caries Preventive Regimen

for Orthodontic Patients
u O ’ Reilly
and Featherstone, 1987
u Daily home use of combination of
fluoride products
u Fluoride-containing toothpaste -
twice daily
u 0.05% NaF mouthrinse twice daily
(morning and night)

Toothpaste Components - 1
u Abrasive 40-50% to clean the teeth
§ Insoluble sodium metaphosphate (NaPO3 )x
§ Dicalcium phosphate dihydrate CaHPO4 .2H2 O
§ Calcium carbonate CaCO3
§ Hydrated silica SiO2
§ Baking Soda NaHCO3
u Usually contains 1000, 1100 or 1450 ppm
fluoride as sodium fluoride or sodium
monofluorophosphate
u Other possibilities: stannous fluoride, amine
fluoride
 Toothpaste Components - 2
u Humectant (glycerol) 20-40% - retains
moisture
u Water 20-30%
u Detergent 1-2% e.g. sodium lauryl sulfate
u Binder 0.5-2 % e.g. carboxy methyl cellulose
u Flavor, color, filler e.g. titanium dioxide
u Other “therapeutic” agents - see below, e.g.
tartar control agents, antibacterial for
gingivitis, peroxide, baking soda, whiteners

Toothpaste Active Components

Sodium Fluoride
u Sodiumfluoride, NaF
u Dentifrice
usually contains 1000, 1100 or
1450 ppm F- (free fluoride ion)
u Must have a compatible abrasive that does
not bind the fluoride e.g. hydrated silica
u All other components must not interfere with
fluoride topical actions
u Must be stable with time and temperature
 Toothpaste Active Components
Sodium Monofluorophosphate
Colgate patent 1950
u SMFP. Na2FPO 3
u Dentifrice usually contains the equivalent of
1000 ppm total F , mostly as FPO 32- ion.
u Abrasive not so critical
u MFP does not enhance remineralization
u Hydrolyzes rapidly in dental plaque to form
free F- ion which then acts
u Must be stable with time and temperature

Toothpaste Active Components

Stannous Fluoride
u Stannous (Tin) fluoride, SnF2. Stannous ion
antibacterial. Anti-gingivitis activity
u Dentifrice contains 1000 - 1500 ppm F as total
F, mostly F- (free fluoride ion)
u Must be with a compatible abrasive
u All other components must not interfere with
fluoride topical actions
u Must be stable with time and temperature.
Older formulations deteriorated with age
 Stannous Fluoride Stabilized Formula 2007

Orthodontic brackets attract cariogenic bacteria, leading to

“white patch” decay

Toothpaste Active Components

Amine Fluoride
u Amine fluoride, AmineF. Amine ion basic.
Strong complex with F enhances diffusion
u Dentifrice
contains 1000 - 1500 ppm F as total
F, mostly F- (free fluoride ion)
u Must be with a compatible abrasive
u All other components must not interfere with
fluoride topical actions
u Must be stable with time and temperature.
Older formulations deteriorated with age
 Toothpaste Components
Other Additives
u Must not interfere with fluoride action, either
in the tube or in the mouth
u Compatible abrasive

u Must be stable with time and temperature

u Long term non-interaction with fluoride or
other components
must not interfere with additive’s
u Fluoride
proposed mode of action

Toothpaste Components
Anti-calculus Products
u Pyrophosphate, P2O 74- , with a compatible
abrasive system
u Inhibits
mineral growth at tooth surface and in
plaque
u Strongly adsorbed to apatite. Does not diffuse
into lesion subsurface
u P 2O 74- does not interfere with subsurface
remineralization action of fluoride
 Toothpaste Components
Whitening products
u By altering abrasive. Must be compatible
with F
u By oxidizing agent: e.g. Carbamate peroxide

u Mustnot interfere with F or vice versa

u Canalso contain pyrophosphate for anti-
calculus
u Can also contain a compatible antibacterial

Toothpaste Components
Bicarbonate

u Bicarbonate,HCO 3-
u Baking soda – abrasive itself

u Compatible with fluoride

u Buffers acids
u Has antibacterial properties
 Toothpaste Components
Multi-component Toothpaste
u Difficult
to formulate correctly
u Requires very careful study of cross-reactions
of components
u Careful choice of fluoride source
u Compatible abrasive

u Laboratory and In situ remineralization studies

u Maintain effectiveness of fluoride action
 Mouthrinse Components
Fluoride Mouthrinses
u Contain 0.05 % NaF, 225 ppm F in solution as F-.
u Used in conjunction with F dentifrice adds to
caries protective efficacy
u Fluoride retained in saliva and plaque longer
and at higher levels than from F dentifrice use
u Use for moderate caries risk individuals

Over the counter

fluoride products
are very effective at
controlling caries if
used two or more
times daily.

Course objectives:

1. to understand the limitations of formulating

fluoride products to make them effective

2. to know the various forms of fluoride delivery

for home use and office use, including the ADA
recommendations for office topical applications