U.S. patent application number 14/594234 was filed with the patent office on 2015-05-07 for methods for improving taste and oral care compositions with improved taste.
The applicant listed for this patent is The Procter & Gamble Company. Invention is credited to John Christian Haught, Yakang Lin, Lowell Alan Sanker, Koti Tatachar Sreekrishna.
Application Number | 20150125405 14/594234 |
Document ID | / |
Family ID | 43030558 |
Filed Date | 2015-05-07 |
United States Patent
Application |
20150125405 |
Kind Code |
A1 |
Haught; John Christian ; et
al. |
May 7, 2015 |
Methods For Improving Taste And Oral Care Compositions With
Improved Taste
Abstract
Provided herein are compositions and methods relating to oral
care compositions with improved taste. One such method includes
providing an oral care composition comprising a metal salt, a
peroxide, an antimicrobial agent, a bad breath reduction agent, a
surfactant, or a combination thereof and adding to the oral care
composition a TRPV1 activator and/or vanitrope.
Inventors: |
Haught; John Christian;
(West Chester, OH) ; Sreekrishna; Koti Tatachar;
(Mason, OH) ; Lin; Yakang; (Liberty Township,
OH) ; Sanker; Lowell Alan; (Mason, OH) |
|
Applicant: |
Name |
City |
State |
Country |
Type |
The Procter & Gamble Company |
Cincinnati |
OH |
US |
|
|
Family ID: |
43030558 |
Appl. No.: |
14/594234 |
Filed: |
January 12, 2015 |
Related U.S. Patent Documents
|
|
|
|
|
|
Application
Number |
Filing Date |
Patent Number |
|
|
12763933 |
Apr 20, 2010 |
8962057 |
|
|
14594234 |
|
|
|
|
61177457 |
May 12, 2009 |
|
|
|
61173711 |
Apr 29, 2009 |
|
|
|
Current U.S.
Class: |
424/52 ; 424/49;
424/53 |
Current CPC
Class: |
A61K 8/4926 20130101;
A61K 8/19 20130101; A61K 8/49 20130101; A61Q 11/00 20130101; A61K
8/42 20130101; A61K 8/347 20130101; A61K 8/4973 20130101; A61K
8/9794 20170801; A61K 8/27 20130101; A61K 2800/592 20130101; A61K
8/9717 20170801; A61K 8/35 20130101; A61K 8/22 20130101; A61K 8/21
20130101; A61K 8/365 20130101 |
Class at
Publication: |
424/52 ; 424/49;
424/53 |
International
Class: |
A61K 8/34 20060101
A61K008/34; A61K 8/21 20060101 A61K008/21; A61K 8/365 20060101
A61K008/365; A61K 8/22 20060101 A61K008/22; A61K 8/42 20060101
A61K008/42; A61K 8/35 20060101 A61K008/35; A61Q 11/00 20060101
A61Q011/00; A61K 8/49 20060101 A61K008/49 |
Claims
1. An oral care composition with improved taste comprising: a. at
least about 0.003%, by weight of the composition, vanillyl butyl
ether; and b. a metal salt selected from the group consisting of
zinc salt, stannous salt, potassium salt, copper salt, and mixtures
thereof.
2. The composition of claim 1 wherein the metal salt comprises a
zinc salt comprising zinc citrate and wherein the metal salt is
present in an amount from about 0.05% to about 5.0%, by weight of
the oral care composition.
3. The composition of claim 1 wherein the at least about 0.006%, by
weight of the composition, of vanillyl butyl ether is added.
4. The composition of claim 1 wherein the vanillyl butyl ether is
present in an amount from about 0.002% to about 0.02% by weight of
the oral care composition.
5. The composition of claim 1 wherein the metal salt comprises
stannous salt comprising stannous fluoride.
6. The composition of claim 1 wherein the composition further
comprises from about 5% to about 80% by weight of the oral care
composition of water.
7. The composition of claim 3 further comprising cetyl pyridinium
chloride.
8. The method of claim 1 further comprising a peroxide selected
from the group consisting hydrogen peroxide, carbamide peroxide,
calcium peroxide, sodium peroxide, and combinations thereof.
9. The composition of claim 1 further comprising a TRPV1 activator
selected from the group consisting of capsaicin, capsiate, shoagol,
gingerol, piperine, or a combination thereof.
10. The composition of claim 1, further comprising adding to the
oral care composition a TRPV1 enhancer selected from the group
consisting of damascone, geranyl butyrate, 2-octanone, furfural,
ionone, 2,6-dimethyl-5-heptenal, tetrasodium pyrophosphate, alpha
dimethyl phenethyl acetate, phenylacetaldehyde dimethyl acetal,
kephalis, linalool oxide, carvyl acetate, farnesene,
trans-2-hexenyl acetate, heptyl alcohol, or a combination
thereof.
11. An oral care composition with improved taste comprising: a. at
least about 0.003%, by weight of the composition, vanillyl butyl
ether; b. from about 0.01% to about 0.15%, by weight of the
composition, zingerone; and c. a metal salt selected from the group
consisting of zinc salt, stannous salt, potassium salt, copper
salt, and mixtures thereof.
12. The composition of claim 11 wherein the vanillyl butyl ether is
present in an amount from about 0.003% to about 0.025% by weight of
the oral care composition.
13. The composition of claim 11 wherein the composition comprises
from about 0.02% to about 0.04%, by weight of the composition, of
zingerone.
14. The composition of claim 11 wherein the metal salt comprises a
zinc salt comprising zinc citrate and wherein the metal salt is
present in an amount from about 0.05% to about 5.0%, by weight of
the oral care composition.
15. The composition of claim 11 wherein the composition further
comprises from about 5% to about 80%, by weight of the oral care
composition, water.
16. An oral care composition with improved taste comprising: a. at
least about 0.003%, by weight of the composition, vanillyl butyl
ether; b. vanitrope; and c. a metal salt selected from the group
consisting of zinc salt, stannous salt, potassium salt, copper
salt, and mixtures thereof.
17. The composition of claim 16 wherein the composition comprises
from about 0.01% to about 0.15%, by weight of the composition,
vanitrope.
18. The method of claim 16 wherein the composition comprises from
about 0.02% to about 0.04%, by weight of the composition, of
vanitrope.
19. The composition of claim 16 wherein the metal salt comprises a
zinc salt comprising zinc citrate and wherein the metal salt is
present in an amount from about 0.05% to about 5.0%, by weight of
the oral care composition.
20. The composition of claim 16 wherein the composition further
comprises from about 5% to about 80%, by weight of the oral care
composition, water.
Description
FIELD OF THE INVENTION
[0001] The present invention is directed to oral care compositions
with improved taste and methods of improving the taste of oral care
compositions.
BACKGROUND OF THE INVENTION
[0002] People are always looking for ways to improve their smile
and the health of their teeth and oral cavity. The first step on
this journey for many is the use of oral care compositions like
toothpaste and rinse. The benefits achieved from the use of those
types of products cover a broad range from cosmetic benefits, like
whitening and fresh breath, to health benefits, like reduced
tartar. Unfortunately, many components used in oral care
compositions, including the agents giving the desired benefits,
often have a negative impact on the overall taste of the product.
As such, there is a need for methods which provide improved flavor
in oral care compositions and oral care compositions with improved
flavor.
SUMMARY OF THE INVENTION
[0003] In one embodiment, the present invention is directed to a
method for improving taste of an oral care composition. The method
includes mixing a TRPV1 activator and a bad taste agent selected
from the group consisting of: a metal salt, a peroxide, an
antimicrobial agent, a bad breath reduction agent, a surfactant,
and combinations thereof, to form an oral care composition.
[0004] In another embodiment, the present invention is directed to
a method for improving taste of an oral care composition where the
method includes mixing vanillyl butyl ether and a bad taste agent
comprising a zinc salt, stannous salt, a potassium salt, copper
salt, or a combination thereof, to form an oral care composition,
wherein the vanillyl butyl ether is present in an amount of about
0.001% to about 0.025% by weight of the oral care composition.
[0005] In another embodiment, the present invention is directed to
a method for improving taste of an oral care composition where the
method includes mixing vanitrope and a bad taste agent comprising a
metal salt, a peroxide, or a combination thereof, to form an oral
care composition, wherein the vanitrope is present in an amount of
about 0.01% to about 0.4% by weight of the oral care
composition.
[0006] It is believed that these as well as other embodiments of
the present invention will be better understood from the following
description.
DETAILED DESCRIPTION OF THE INVENTION
Definitions
[0007] All percentages and ratios used hereinafter are by weight of
total composition, unless otherwise indicated. All percentages,
ratios, and levels of ingredients referred to herein are based on
the actual amount of the ingredient, and do not include solvents,
fillers, or other materials with which the ingredient may be
combined as a commercially available product, unless otherwise
indicated.
[0008] All measurements referred to herein are made at 25.degree.
C. (i.e. room temperature) unless otherwise specified.
[0009] As used herein, the word "about" means+/-10 percent.
[0010] As used herein, the word "include," and its variants, are
intended to be non-limiting, such that recitation of items in a
list is not to the exclusion of other like items that may also be
useful in the materials, compositions, devices, and methods of this
invention.
[0011] By "oral care composition" is meant a product, which in the
ordinary course of usage, is not intentionally swallowed for
purposes of systemic administration of particular therapeutic
agents, but is rather retained in the oral cavity for a time
sufficient to contact dental surfaces and/or oral tissues. The oral
care composition may be in various forms including toothpaste,
dentifrice, tooth gel, subgingival gel, mouth rinse, mousse, foam,
mouth spray, lozenge, chewable tablet, chewing gum or denture care
product. The oral care composition may also be incorporated onto
strips or films for direct application or attachment to oral
surfaces.
[0012] The term "dentifrice", as used herein, includes paste, gel,
or liquid formulations unless otherwise specified. The dentifrice
can be in a dual phase form, like a striped paste for example, and
can also be used as a regimen.
[0013] The term "bad taste agent" as used herein, refers to a
component in an oral care composition which gives an adverse taste
to a user, for example, a metallic taste or an astringent taste, or
an adverse sensation, for example, a feeling of dry mouth.
[0014] The term "teeth", as used herein, refers to natural teeth as
well as artificial teeth or dental prosthesis.
[0015] The term "TRPV1" as used herein refers to the transient
receptor potential vanilloid receptor 1 which is a ligand-gated,
non-selective cation channel preferentially expressed on
small-diameter sensory neurons and detects noxious as well as other
substances.
[0016] The term "TRPV1 activator" as used herein refers to any
component which at a concentration of 1 mM gives a calcium flux
count of at least 1000 counts above the background level of calcium
present in the cell according to the FLIPR method as discussed
herein. The term "count" is defined as the change in fluorescence
of the transfected cell lines due to the influx of calcium across
the cell membrane, which reacts with the calcium sensitive dye
present within the cells.
[0017] The term "TRPV1 enhancer" as used herein refers to any
component that boosts the calcium flux activity of a compound that
directly activates TRPV1, but does not directly activate TRPV1.
[0018] Active and other ingredients useful herein may be
categorized or described herein by their cosmetic and/or
therapeutic benefit or their postulated mode of action or function.
However, it is to be understood that the active and other
ingredients useful herein can, in some instances, provide more than
one cosmetic and/or therapeutic benefit or function or operate via
more than one mode of action. Therefore, classifications herein are
made for the sake of convenience and are not intended to limit an
ingredient to the particularly stated function(s) or activities
listed.
Oral Care Compositions and Methods
[0019] It is highly desirable that consumer products for use in
cleaning and care of the oral cavity impart a fresh and clean
feeling as this provides consumers with a signal of continuing
freshness and cleanliness. In addition to the feeling of
cleanliness, consumers also want to experience the benefits of oral
care actives like anti-tartar agents, for example, through their
oral care regimen. The ability to formulate a consumer acceptable
oral care composition, however, raises challenges as many of the
components used to impart a flavor, deliver a benefit, or that are
part of the base for the oral care composition add unwanted tastes
and/or sensations along with the targeted benefit for which they
are added. Thus, formulating oral care compositions can be a
balancing act between acceptable flavor and acceptable
benefits.
[0020] As will be seen below, many of the components which can be
used to formulate an oral care composition provide an off taste and
thus make formulating a consumer acceptable product a challenge. It
has now been discovered that the addition of certain components to
an oral care composition can reduce many of the off tastes
associated with many of the components discussed below and thus
improve the taste. These taste improving components include, for
example, TRPV1 activators and vanitrope.
[0021] The first group of components which will help to improve
taste in an oral care composition are Transient Receptor Potential
Vanilloid 1 (TRPV1) activators. TRPV1 is a ligand-gated,
non-selective cation channel preferentially expressed on small
diameter sensory neurons. In looking at this receptor, it was
discovered that activation of this receptor caused a surprising
effect. By adding a TRPV1 activator to an oral care composition
with an off tasting component, the user of the composition
experienced an improved taste over an oral care composition without
the TRPV1 activator. Thus, the TRPV1 activator is working to
off-set the bad taste associated with many components used in oral
care compositions.
[0022] In order to determine whether TRPV1 is activated, the
intracellular calcium ion (Ca.sup.+2) levels in TRPV1 receptors is
measured. HEK-23 (human embryonic kidney) cells stably transfected
with human TRPV1 are grown in 15 ml growth medium [high glucose
DMEM (Dulbecco's Modification of Eagle's Medium) supplemented with
10% FBS (fetal bovine serum), 100 .mu.g/ml Penicillin/streptomycin,
100 .mu.g/ml G418] in a 75 Cm.sup.2 flask for 3 days at 33.degree.
C. in a mammalian cell culture incubator set at 5% CO.sub.2. Cells
are detached with addition of 10 ml of PBS (phosphate buffered
saline) by hand shaking gently. Cells are transferred to a 50 ml
tube and centrifuged at 850 rpm for 3 minutes to remove PBS. After
centrifugation, a pellet of cells is formed in the bottom of the
tube separating them from the supernatant solution. The supernatant
is discarded and the cell pellet is suspended in 1 ml of fresh
growth medium to which 5 .mu.l (12.5 .mu.g) of Fluo-4 AM (Molecular
Probes, Inc.) calcium indicator is added and incubated for 30 min
with gentle shaking. Fluo-4 is a fluorescent dye used for
quantifying cellular Ca.sup.2+ concentrations in the 100 nM to 1
microM range. At the end of the 30 minutes, 45 ml of assay buffer
[1.times.HBSS (Hank's Balanced Salt Solution), 20 mM HEPES
(4-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid)] is added to
wash cells and the resulting combination is then centrifuged at 850
rpm for 3 minutes to remove excess buffer and Fluo-4 AM calcium
indicator.
[0023] The pellet cells are re-suspended in 10 ml assay buffer and
90 .mu.l aliquots (.about.50,000 cells) per well delivered to a
96-well assay plate containing 10 .mu.l of test compounds (1 mM in
assay buffer, final concentration 100 .mu.M) or buffer control and
incubated at room temperature for 30 minutes. After 30 minutes, the
plate is placed into a fluorometric imaging plate reader
(FLIPR.sup.384 from Molecular Devices) and basal fluorescence
recorded (excitation wave length 488 nm and emission wave length
510 nm). The FLIPR assay is an accepted method for detecting
changes in intracellular calcium concentration. Then 20 .mu.l of
the molecule being tested as a TRPV1 activator is added and
fluorescence recorded. For determining the direct effect of test
compounds on TRPV1, fluorescence is measured immediately after
addition of each compound. Additional discussion of the FLIPR
method can be found in Smart et al., Characterization using FLIPR
of human vanilloid VR1 receptor pharmacology, European Journal of
Pharmacology 417, 51-58 (2001) and Liu et al., Development and
validation of a platelet calcium flux assay using a fluorescent
imaging plate reader, Analytical Biochemistry 357, 216-224
(2006).
[0024] TRPV1 responds to, for example, both noxious and painful
stimuli. A noxious stimulus would include those which give a
burning (i.e. hot) sensation. A chart below lists some TRPV1
activators which fall into this class and give a burning sensation
as measured on the standard Scoville hotness scale.
TABLE-US-00001 `Hotness` Compound (as log Scoville Units)
Dihydrocapsaicin 7.2 Capsaicin 7.2 NorhydroCapsaicin 7.0
HomodihydroCapsaicin 6.9 HomoCapsaicin 6.9 Vanillyl Butyl Ether 5.7
Piperine 5.3 6-Shoagol 5.1 6-Gingerol 4.9 Allicin 4.0 Zingerone
<4.0
Since many of these compounds are derived from natural sources,
they often retain the inherent pungency of the source material when
used at levels to exert a warming effect. For example, piperine is
peppery, capsaicin is like red peppers, and zingerone retains the
pungency of ginger. This also holds true for synthetic compounds,
like vanillyl butyl ether, as described in US6570010B2.
Interestingly, the use of TRPV1 activators, like those above, at an
amount below that which triggers a burning effect gives a reduction
in off-taste and a product in which the consumer can detect the
improved taste. The use of a level which triggers a burning effect
results in the consumer noticing the burning sensation and not,
necessarily, an improved flavor. In one embodiment, a TRPV1
activator will be added in an amount of about 0.0001% to about 0.1%
by weight of the oral care composition. However, the level of
activation of TRPV1 is related to the level of hotness of the
activator. Thus, the level of TRPV1 activator used will depend on
the strength of its hotness. For example, vanillyl butyl ether
(which has an activation level of approximately 14942.84 calcium
ions at a concentration of 1 mM) will generally be used at an
amount of about 0.025% or below while capsaicin (which has an
activation level of about 14127.16 calcium ions at a much lower
concentration level of 300 nM) will be used at an amount of about
0.009% or below. Thus a much smaller concentration of capsaicin
(300 nM) gives nearly the same level of activation as a much higher
concentration of VBE (1 mM) and thus can be used in smaller
quantities.
[0025] In addition to its role as a noxious substance detector, it
is believed that the activation of TRPV1 also has some downstream
affects. Specifically, without being limited by theory, it is
believed that activation of TRPV1 causes changes in other taste
receptors, specifically PKD1L3, PKD2L1, and the TAS2R family of
receptors. It is believed the changes in the TAS2R16, TAS2R38,
PKD2L1, and PKD1L3 receptors also contribute to the improvement in
taste.
[0026] Interestingly, some of the compounds which give an off taste
also affect the activity of TRPV1, but at a very low level (i.e.
below that needed to be a TRPV1 activator). Without being limited
by theory, for those components which render an off taste in oral
care compositions and which affect the TRPV1 receptor activity but
do not rise to the level of an activator, it is believed the TRPV1
activators out compete these components for binding of the TRPV1
receptor. This prevents the off-taste components from spreading any
off-taste through TRPV1 or any downstream activities caused by the
binding of the off taste component to TRPV1.
[0027] In light of the above, according to one embodiment of the
invention, an oral care composition comprising a bad taste agent
and a TRPV1 activator(s) would have an improved taste.
Additionally, in one embodiment, a method of improving the taste of
an oral care composition comprises mixing a TRPV1 activator and a
bad taste agent selected from the group consisting of: a metal
salt, a peroxide, an antimicrobial agent, a bad breath reduction
agent, a surfactant, and combinations thereof, to form an oral care
composition.
[0028] In one embodiment, the TRPV1 activator comprises vanillyl
butyl ether, zingerone, capsaicin, capsiate, shoagol, gingerol,
piperine, or a combination thereof. In a further embodiment, the
TRPV1 activator comprises vanillyl butyl ether. In one embodiment,
the vanillyl butyl ether is added at an amount of about 0.001% to
about 0.25% by weight of the oral care composition. In another
embodiment, the vanillyl butyl ether is added in an amount of from
about 0.002% to about 0.02% by weigh of the oral care
composition.
[0029] In another embodiment, a method for improving taste of an
oral care composition comprises mixing vanillyl butyl ether and a
bad taste agent comprising a zinc salt, stannous salt, a potassium
salt, copper salt, or a combination thereof, to form an oral care
composition, wherein the vanillyl butyl ether is present in an
amount of about 0.001% to about 0.025% by weight of the oral care
composition. In a further embodiment, the oral care composition or
method further comprises adding vanitrope, zingerone, or a
combination thereof to the oral care composition. In one
embodiment, the zingerone is added at an amount from about 0.01% to
about 0.015%. In another embodiment, the vanitrope is added at an
amount from about 0.01% to about 0.015%.
[0030] Additionally, some compounds have been found to enhance the
effect of TRPV1 activators, even though these enhancers do not
activate TRPV1 on their own. For examples, see the chart below,
where the enhancer is added after a TRPV1 actovator (capsaicin) to
determine if additional activation occurs.
TABLE-US-00002 % Compound Name CAS # Enhancement delta-damascone
57378-68-4 28.53 Alpha-Damascone 43052-87-5 28.1 Geranyl Butyrate
106-29-6 23.46 2-Octanone 111-13-7 19.87 Furfural 98-01-1 19.29
Alpha-Ionone 127-41-3 18.84 2,6-Dimethyl-5-Heptenal 106-72-9 17.5
Tetrasodium Pyrophosphate 7722-88-5 15.62 Alpha, Alpha
Dimethylphenethyl Acetate 151-05-3 14.64 Phenylacetaldehyde
Dimethyl Acetal 101-48-4 14.07 Kephalis 36306-87-3 13.74 Linalool
Oxide 1365-19-1 13.67 carvyl acetate 97-42-7 12.83 Farnesene
502-61-4 12.33 Trans-2-Hexenyl Acetate 2497-18-9 10.62 Heptyl
Alcohol 111-70-6 10.16
In a separate test, the TRPV1 activator (VBE) and the enhancer are
added together. Here, without being limited by theory, it appears
there surprisingly is an additional affect on the activation of the
TRPV1 activator when the enhancer is added at the beginning. See
the chart below.
TABLE-US-00003 Percent Enhancement When combined VBE Enhancer with
3.5 Level Enhancer Level microMolar VBE 3.5 micro- Alpha, Alpha
1000 microMolar 420% Molar Dimethyl- 200 microMolar 410% phenethyl
100 microMolar 310% Acetate 50 microMolar 300% 3.5 micro-
Farnescene 1000 microMolar 400% Molar 200 microMolar 175% 100
microMolar 100% 50 microMolar 25%
The use of an enhancer will provide a further boost to improving
the taste of an oral care composition and can reduce the amount of
TRPV1 activator required. The level of enhancement can be used to
help determine the effect of the booster and any desired reduction
in TRPV1 activator. For example, in one embodiment vanillyl butyl
ether would be used at 0.012%, but with the enhancer delta
damascene at 0.003%, VBE could be used at 0.008% to achieve the
same effect as without the enhancer.
[0031] Thus, in one embodiment, an oral care composition or a
method of improving taste of an oral care composition further
comprises adding a TRPV1 enhancer to the oral care composition. In
a further embodiment, the TRPV1 enhancer is selected from the group
consisting of damascone, geranyl butyrate, 2-octanone, furfural,
ionone, 2,6-dimethyl-5-heptenal, tetrasodium pyrophosphate, alpha
dimethyl phenethyl acetate, phenylacetaldehyde dimethyl acetal,
kephalis, linalool oxide, carvyl acetate, farnesene,
trans-2-hexenyl acetate, heptyl alcohol, and combinations
thereof.
[0032] Although not considered to be a TRPV1 activator, vanitrope
also has the ability to reduce the off taste associated with at
least some of the components listed above. Vanitrope is a eugenol
derivative which has a vanilla note. Without being limited by
theory, it is believed that Vanitrope likely modulates the taste
receptors aforementioned directly, without the assistance of the
TRPV1 activation.
[0033] In light of the above, an oral care composition comprising
an oral care component which gives a bad taste and vanitrope would
have an improved taste. Additionally, in one embodiment, the
present invention is directed to a method for improving taste of an
oral care composition, comprising mixing vanitrope and a bad taste
agent comprising a metal salt, a peroxide, or a combination
thereof, to form an oral care composition, wherein the vanitrope is
present in an amount of about 0.01% to about 0.4% by weight of the
oral care composition.
[0034] In one embodiment, the metal salt comprises a zinc salt,
stannous salt, potassium salt, copper salt, or a combination
thereof. In another embodiment, the peroxide is selected from the
group consisting hydrogen peroxide, carbamide peroxide, calcium
peroxide, sodium peroxide, and combinations thereof. In another
embodiment, the vanitrope is added in an amount from about 0.05% to
about 0.15% by weight of the oral care composition. In an
additional embodiment, the potassium salt comprises potassium
nitrate and is present in an amount of from about 0.01% to about
5.0% by weight of the oral care composition. In another embodiment,
the zinc salt comprises zinc citrate and is present in an amount
from about 0.05% to about 5.0% by weight of the oral care
composition.
[0035] In an additional embodiment, the combination of vanitrope,
zingerone, and vanillyl butyl ether can be used to give an improved
taste in oral care compositions. Thus, in one embodiment, an oral
care composition with an improved taste comprises vanitrope,
zingerone, and vanillyl butyl.
[0036] The order of addition of the TRPV1 activators and/or
vanitrope is not critical. Thus, the TRPV1 activators and/or
vanitrope can be added in with the oral care components at the time
of making the oral care composition or at some point after the oral
care composition is complete.
Oral Care Composition
[0037] Oral care compositions are often made up of a combination of
components which can include carrier materials, surfactants,
flavors, colorants, sensates, actives, and other additives.
Carrier Material
[0038] Carrier materials generally represents anywhere from about
5% to about 80% of the oral care composition by weight. Examples of
materials which can act as a carrier material include water,
glycerin, sorbitol, polyethylene glycols having a molecular weight
of less than about 50,000, propylene glycol and other edible
polyhydric alcohols, ethanol, or combinations thereof. Of these
carrier materials, examples of some which provide an unwanted taste
within an oral care composition include, for example, propylene
glycol and/or ethanol. The unwanted tastes often associated with
these types of materials are bitterness, burning, astringency,
and/or earthy or dirty tastes.
Surfactants
[0039] Another component of an oral care composition can include
surfactants. Surfactants are generally included in an oral care
composition in a range of about 1% to about 15%. The surfactant may
be anionic, nonionic, amphoteric, zwitterionic, cationic, or
combinations thereof. Anionic surfactants useful herein include,
for example, the water-soluble salts of alkyl sulfates having from
8 to 20 carbon atoms in the alkyl radical (e.g., sodium alkyl
sulfate) and the water-soluble salts of sulfonated monoglycerides
of fatty acids having from 8 to 20 carbon atoms. Sodium lauryl
sulfate (SLS) and sodium coconut monoglyceride sulfonates are
examples of anionic surfactants of this type. Other suitable
anionic surfactants include sarcosinates, such as sodium lauroyl
sarcosinate, taurates, sodium lauryl sulfoacetate, sodium lauroyl
isethionate, sodium laureth carboxylate, and sodium dodecyl
benzenesulfonate. Combinations of anionic surfactants can also be
employed. Many suitable anionic surfactants are disclosed by
Agricola et al., U.S. Pat. No. 3,959,458. In varying embodiments,
the present compositions comprise an anionic surfactant at a level
of from about 0.025% to about 9%, from about 0.05% to about 5%, or
from about 0.1% to about 1%.
[0040] Another class of anionic surfactants useful here are alkyl
phosphates. The surface active organophosphate agents have a strong
affinity for enamel surface and have sufficient surface binding
propensity to desorb pellicle proteins and remain affixed to enamel
surfaces. Suitable examples of organophosphate compounds include
mono-, di- or triesters represented by the general structure below
wherein Z1, Z2, or Z3 may be identical or different, at least one
being an organic moiety, in one embodiment selected from linear or
branched, alkyl or alkenyl group of from 1 to 22 carbon atoms,
optionally substituted by one or more phosphate groups; alkoxylated
alkyl or alkenyl, (poly)saccharide, polyol or polyether group.
##STR00001##
[0041] Some other agents include alkyl or alkenyl phosphate esters
represented by the following structure:
##STR00002##
wherein R.sub.1 represents a linear or branched, alkyl or alkenyl
group of from 6 to 22 carbon atoms, optionally substituted by one
or more phosphate groups; n and m, are individually and separately,
2 to 4, and a and b, individually and separately, are 0 to 20;
Z.sub.2 and Z.sub.3 may be identical or different, each represents
hydrogen, alkali metal, ammonium, protonated alkyl amine or
protonated functional alkyl amine such as an alkanolamine, or a
R.sub.1--(OC.sub.nH.sub.2n).sub.a(OC.sub.mH.sub.2m).sub.b-- group.
Examples of suitable agents include alkyl and alkyl (poly)alkoxy
phosphates such as lauryl phosphate; PPG5 ceteareth-10 phosphate;
Laureth-1 phosphate; Laureth-3 phosphate; Laureth-9 phosphate;
Trilaureth-4 phosphate; C12-18 PEG 9 phosphate; Sodium dilaureth-10
phosphate. In one embodiment, the alkyl phosphate is polymeric.
Examples of polymeric alkyl phosphates include those containing
repeating alkoxy groups as the polymeric portion, in particular 3
or more ethoxy, propoxy isopropoxy or butoxy groups.
[0042] Additional suitable polymeric organophosphate agents include
dextran phosphate, polyglucoside phosphate, alkyl polyglucoside
phosphate, polyglyceryl phosphate, alkyl polyglyceryl phosphate,
polyether phosphates and alkoxylated polyol phosphates. Some
specific examples are PEG phosphate, PPG phosphate, alkyl PPG
phosphate, PEG/PPG phosphate, alkyl PEG/PPG phosphate, PEG/PPG/PEG
phosphate, dipropylene glycol phosphate, PEG glyceryl phosphate,
PBG (polybutylene glycol) phosphate, PEG cyclodextrin phosphate,
PEG sorbitan phosphate, PEG alkyl sorbitan phosphate, and PEG
methyl glucoside phosphate. Suitable non-polymeric phosphates
include alkyl mono glyceride phosphate, alkyl sorbitan phosphate,
alkyl methyl glucoside phosphate, alkyl sucrose phosphates.
[0043] Another suitable surfactant is one selected from the group
consisting of sarcosinate surfactants, isethionate surfactants and
taurate surfactants. In one embodiment, an alkali metal or ammonium
salts of these surfactants are used. Examples of those sodium and
potassium salts include following: lauroyl sarcosinate, myristoyl
sarcosinate, palmitoyl sarcosinate, stearoyl sarcosinate and oleoyl
sarcosinate, or combinations thereof. Of these anionic surfactants,
examples of some which provide an unwanted taste within an oral
care composition include, for example, SLS, lauroyl sarcosinate,
and/or fatty alcohols or acids associated with natural based
surfactants. The unwanted tastes often associated with these
surfactants are soapy, chemical, and/or artificial.
[0044] Zwitterionic or amphoteric surfactants useful in oral care
compositions include derivatives of aliphatic quaternary ammonium,
phosphonium, and sulfonium compounds, in which the aliphatic
radicals can be straight chain or branched, and one of the
aliphatic substituents contains from about 8 to 18 carbon atoms and
one contains an anionic water-solubilizing group, e.g., carboxy,
sulfonate, sulfate, phosphate or phosphonate. Suitable betaine
surfactants are disclosed in U.S. Pat. No. 5,180,577 to Polefka et
al. Typical alkyl dimethyl betaines include decyl betaine or
2-(N-decyl-N,N-dimethylammonio) acetate, coco betaine or
2-(N-coco-N, N-dimethyl ammonio) acetate, myristyl betaine,
palmityl betaine, lauryl betaine, cetyl betaine, cetyl betaine,
stearyl betaine, etc. The amidobetaines are exemplified by
cocoamidoethyl betaine, cocoamidopropyl betaine (CADB), and
lauramidopropyl betaine. Of these surfactants, examples of some
which provide an unwanted taste within an oral care composition
include, for example, cocoamidopropyl betaine and lauryl betaine.
The unwanted tastes often associated with these types of
surfactants are soapy and chemical. These surfactants are generally
included in an oral care composition in a range of about 0.5% to
about 5%.
[0045] Cationic surfactants useful in the present invention
include, for example, derivatives of quaternary ammonium compounds
having one long alkyl chain containing from about 8 to 18 carbon
atoms such as lauryl trimethylammonium chloride; cetyl pyridinium
chloride; cetyl trimethylammonium bromide; coconut
alkyltrimethylammonium nitrite; cetyl pyridinium fluoride or
combinations thereof. Additional quaternary ammonium fluorides
having detergent properties are described in U.S. Pat. No.
3,535,421 to Briner et al. Of these surfactants, examples of some
which provide an unwanted taste within an oral care composition
include, for example, cetyl pyridinium chloride or chlorhexidine.
The unwanted tastes often associated with these surfactants are
chemical and/or antiseptic.
[0046] Nonionic surfactants that can be used in the compositions of
the present invention include, for example, compounds produced by
the condensation of alkylene oxide groups (hydrophilic in nature)
with an organic hydrophobic compound which may be aliphatic or
alkylaromatic in nature. Examples of suitable nonionic surfactants
include the Pluronics.RTM. which are poloxamers, polyethylene oxide
condensates of alkyl phenols, products derived from the
condensation of ethylene oxide with the reaction product of
propylene oxide and ethylene diamine, ethylene oxide condensates of
aliphatic alcohols, long chain tertiary amine oxides, long chain
tertiary phosphine oxides, long chain dialkyl sulfoxides and
combinations of such materials.
Flavors
[0047] Another component which can be part of an oral care
composition includes flavors. Flavors are generally present in an
amount of about 0.4% to about 3% by weight of the oral care
composition. Examples of some flavors and flavor components used in
oral care compositions are mint oils, wintergreen, clove bud oil,
cassia, sage, parsley oil, marjoram, lemon, orange, propenyl
guaethol, heliotropine, 4-cis-heptenal, diacetyl,
methyl-p-tert-butyl phenyl acetate, methyl salicylate, ethyl
salicylate, 1-menthyl acetate, oxanone, .alpha.-irisone, methyl
cinnamate, ethyl cinnamate, butyl cinnamate, ethyl butyrate, ethyl
acetate, methyl anthranilate, iso-amyl acetate, iso-amyl butyrate,
allyl caproate, eugenol, eucalyptol, thymol, cinnamic alcohol,
octanol, octanal, decanol, decanal, phenylethyl alcohol, benzyl
alcohol, .alpha.-terpineol, linalool, limonene, citral, neral,
geranial, geraniol nerol, maltol, ethyl maltol, anethole,
dihydroanethole, carvone, menthone, .beta.-damascenone, ionone,
.gamma.-decalactone, .gamma.-nonalactone, .gamma.-undecalactone, or
combinations thereof. Generally suitable flavoring ingredients are
chemicals with structural features and functional groups that are
less prone to redox reactions. These include derivatives of flavor
chemicals that are saturated or contain stable aromatic rings or
ester groups. Of these flavors, examples of some which provide an
unwanted taste include, for example, citral, geranial, eucalyptol,
and eugenol. The unwanted tastes often associated with these types
of flavors are sourness, chemical, bitter, pungent, and/or
astringent.
Colorants
[0048] Additionally, colorants can form part of an oral care
composition. Colorants are generally present in an amount of about
0.001% to about 0.5% by weight of the oral care composition.
Examples of some colorants used in oral care compositions include
D&C Yellow No. 10, FD&C Blue No. 1, FD&C Red No. 40,
D&C Red No. 33 and combinations thereof. Levels of the colorant
may range from about 0.0001% to about 0.1%. In one embodiment, the
colorant is in an amount from about 0.001% to about 0.01% by weight
of the oral care composition. Of these colorants, an example of a
colorant which provides an unwanted taste includes, for example,
D&C Red No. 33. The unwanted tastes often associated with this
colorant are metallic and/or chemical.
Sensates
[0049] Another component which can be part of an oral care
composition is a sensate. Sensate molecules such as cooling,
warming, and tingling agents are useful to deliver signals to the
consumer. Sensates are generally present in an amount of about
0.001% to about 0.8% by weight of the oral care composition. The
most well-known cooling sensate compound is menthol, particularly
l-menthol, which is found naturally in peppermint oil. Other
isomers of menthol (neomenthol, isomenthol and neoisomenthol) have
somewhat similar, but not identical odor and taste, i.e., having
disagreeable notes described as earthy, camphor, musty, etc. The
biggest difference among the isomers is in their cooling potency.
L-menthol provides the most potent cooling, i.e., having the lowest
cooling threshold of about 800 ppb, i.e., the concentration level
where the cooling effect could be clearly recognized. At this
level, there is no cooling effect for the other isomers.
[0050] Among synthetic coolants, many are derivatives of or are
structurally related to menthol, i.e., containing the cyclohexane
moiety, and derivatized with functional groups including
carboxamide, ketal, ester, ether and alcohol. Examples include the
.rho.-menthanecarboxamide compounds such as
N-ethyl-p-menthan-3-carboxamide. An example of a synthetic
carboxamide coolant that is structurally unrelated to menthol is
N,2,3-trimethyl-2-isopropylbutanamide. Additional examples of
synthetic coolants include alcohol derivatives such as
3-1-menthoxypropane-1,2-diol, isopulegol, and
.rho.-menthane-3,8-diol; menthone glycerol acetal; menthyl esters
such as menthyl acetate, menthyl acetoacetate, menthyl lactate, and
monomenthyl succinate. Carboxamide cooling agents are described for
example in U.S. Pat. Nos. 4,136,163; 4,150,052; 4,153,679;
4,157,384; 4,178,459 and 4,230,688.
[0051] Additional agents that are structurally unrelated to menthol
but have been reported to have a similar physiological cooling
effect include alpha-keto enamine derivatives described in U.S.
Pat. No. 6,592,884 including
3-methyl-2-(1-pyrrolidinyl)-2-cyclopenten-1-one (3-MPC),
5-methyl-2-(1-pyrrolidinyl)-2-cyclopenten-1-one (5-MPC), and
2,5-dimethyl-4-(1-pyrrolidinyl)-3(2H)-furanone (DMPF); icilin (also
known as AG-3-5, chemical name
1-[2-hydroxyphenyl]-4-[2-nitrophenyl]-1,2,3,6-tetrahydropyrimidine-2-one)
described in Wei et al., J. Pharm. Pharmacol. (1983), 35:110-112.
Of these cooling sensates, examples of some which provide an
unwanted taste include, for example, menthol and menthone. The
unwanted tastes often associated with these cooling sensates
include burning, chemical, and/or medicinal.
[0052] Some examples of warming sensates include ethanol; capsicum;
nicotinate esters, such as benzyl nicotinate; polyhydric alcohols;
capsicum powder; a capsicum tincture; capsicum extract; capsaicin;
homocapsaicin; homodihydrocapsaicin; nonanoyl vanillyl amide;
nonanoic acid vanillyl ether; vanillyl alcohol alkyl ether
derivatives such as vanillyl ethyl ether, vanillyl butyl ether,
vanillyl pentyl ether, and vanillyl hexyl ether; isovanillyl
alcohol alkyl ethers; ethylvanillyl alcohol alkyl ethers; veratryl
alcohol derivatives; substituted benzyl alcohol derivatives;
substituted benzyl alcohol alkyl ethers; vanillin propylene glycol
acetal; ethylvanillin propylene glycol acetal; ginger extract;
ginger oil; gingerol; zingerone; or combinations thereof. Warming
sensates are generally included in an oral care composition at a
level of about 0.05% to about 2%.
[0053] Examples of some tingling sensates include, jambu Oleoresin,
Zanthoxylum peperitum, saanshool-I, saanshool II, sanshoamide,
piperine, piperidine, eugenol, spilanthol,
4-(1-methoxymethyl)-2-phenyl-1,3-dioxolane, or combinations
thereof. Tingling sensates are generally included in an oral care
composition at a level of about 0.0005% to about 1%. Of these
tingling sensates, examples of some which provide an unwanted taste
within an oral care composition include, for example, jambu,
saanshool, and/or eugenol. The unwanted taste(s) often associated
with these tingling sensates include a peppery, bitter, and/or
metallic taste.
Sweeteners
[0054] Another component which can be included in an oral care
composition includes a sweetener. Sweeteners can be both natural
and artificial and are generally present at about 0.1% to about 1%,
by weight of the oral care composition. Some suitable water-soluble
sweeteners include monosaccharides, disaccharides and
polysaccharides such as xylose, ribose, glucose (dextrose),
mannose, galactose, fructose (levulose), sucrose (sugar), maltose,
invert sugar (a combination of fructose and glucose derived from
sucrose), partially hydrolyzed starch, corn syrup solids,
dihydrochalcones, monellin, steviosides, glycyrrhizin, or
combinations thereof. Suitable water-soluble artificial sweeteners
include soluble saccharin salts, i.e., sodium or calcium saccharin
salts, cyclamate salts, the sodium, ammonium or calcium salt of
3,4-dihydro-6-methyl-1,2,3-oxathiazine-4-one-2,2-dioxide, the
potassium salt of
3,4-dihydro-6-methyl-1,2,3-oxathiazine-4-one-2,2-dioxide
(acesulfame-K), the free acid form of saccharin, and the like.
Other suitable sweeteners include dipeptide based sweeteners, such
as L-aspartic acid derived sweeteners, such as
L-aspartyl-L-phenylalanine methyl ester (aspartame),
N-[N-(3,3-dimethylbutyl)-L-.alpha.-aspartyl]-L-phenylalanine
1-methyl ester (neotame), and materials described in U.S. Pat. No.
3,492,131,
L-alpha-aspartyl-N-(2,2,4,4-tetramethyl-3-thietanyl)-D-alaninamide
hydrate, methyl esters of L-aspartyl-L-phenylglycerin and
L-aspartyl-L-2,5,dihydrophenyl-glycine,
L-aspartyl-2,5-dihydro-L-phenylalanine,
L-aspartyl-L-(1-cyclohexylen)-alanine, and the like. Water-soluble
sweeteners derived from naturally occurring water-soluble
sweeteners, such as a chlorinated derivative of ordinary sugar
(sucrose), known, for example, under the product description of
sucralose as well as protein based sweeteners such as thaumatoccous
danielli (Thaumatin I and II) can be used. Of these sweeteners,
examples of some which provide an unwanted taste within an oral
care composition include, for example, aspartame, saccharin, or
neotame. The unwanted taste(s) often associated with these
sweeteners include bitterness and sourness.
Actives
[0055] An additional component which can be included in an oral
care composition includes oral care actives. Oral care actives are
generally present in an amount of about 0.0001% to about 8%. Some
examples of oral care actives include anticaries agents,
antimicrobial agents, antitartar agents, bad breath reduction
agents, and bleaching agents. Anticaries agents are generally used
in an amount of about 0.01% to about 3.0%. It is common to have a
fluoride compound present in dentifrices and other oral
compositions in an amount sufficient to give a fluoride ion
concentration in the composition of from about 0.0025% to about
5.0% by weight to provide anticaries effectiveness. In one
embodiment, the fluoride concentration is from about 0.005% to
about 2.0% by weight. A wide variety of fluoride ion-yielding
materials can be employed as sources of soluble fluoride in the
present compositions and methods. Examples of suitable fluoride
ion-yielding materials are found in U.S. Pat. No. 3,535,421 to
Briner et al. and U.S. Pat. No. 3,678,154 to Widder et al.
Representative fluoride ion sources include: stannous fluoride,
sodium fluoride, potassium fluoride, amine fluoride, sodium
monofluorophosphate, indium fluoride, amine fluorides such as
Olaflur, and many others. In one embodiment, the anticaries agent
comprises stannous fluoride in an amount of about 0.454%. In
another embodiment, the anticaries agent comprises sodium fluoride
in an amount of about 0.243%. Of these anticaries agents, examples
of some which provide an unwanted taste include, for example,
stannous fluoride and potassium fluoride. The unwanted tastes often
associated with these anticaries agents include earthy, dirty,
and/or metallic.
[0056] Another oral care active is an antimicrobial agent. One
example of an antimicrobial agent is a quaternary ammonium
compound. Those useful herein include, for example, those in which
one or two of the substitutes on the quaternary nitrogen has a
carbon chain length (typically alkyl group) from about 8 to about
20, typically from about 10 to about 18 carbon atoms while the
remaining substitutes (typically alkyl or benzyl group) have a
lower number of carbon atoms, such as from about 1 to about 7
carbon atoms, typically methyl or ethyl groups. Dodecyl trimethyl
ammonium bromide, tetradecylpyridinium chloride, domiphen bromide,
N-tetradecyl-4-ethyl pyridinium chloride, dodecyl dimethyl
(2-phenoxyethyl) ammonium bromide, benzyl dimethoylstearyl ammonium
chloride, cetylpyridinium chloride, quaternized
5-amino-1,3-bis(2-ethyl-hexyl)-5-methyl hexahydropyrimidine,
benzalkonium chloride, benzethonium chloride and methyl
benzethonium chloride are exemplary of typical quaternary ammonium
antibacterial agents. Other compounds include
bis[4-(R-amino)-1-pyridinium]alkanes as disclosed in U.S. No.
4,206,215, Jun. 3, 1980 to Bailey. Other quaternary ammonium
compounds include the pyridinium compounds. Examples of pyridinium
quaternary ammonium compounds include cetylpyridinium and
tetradecylpyridinium halide salts (i.e., chloride, bromide,
fluoride and iodide). The quaternary ammonium antimicrobial agents
can be included at levels of at least about 0.035%. In other
embodiments they are included from about 0.045% to about 1.0% or
from about 0.05% to about 0.10% by weight of the oral care
composition.
[0057] The present invention may also include other antimicrobial
agents including non-cationic antimicrobial agents such as
halogenated diphenyl ethers, phenolic compounds including phenol
and its homologs, mono and poly-alkyl and aromatic halophenols,
resorcinol and its derivatives, xylitol, bisphenolic compounds and
halogenated salicylanilides, benzoic esters, and halogenated
carbanilides. Also useful antimicrobials are enzymes, including
endoglycosidase, papain, dextranase, mutanase, and combinations
thereof. Such agents are disclosed in U.S. Pat. No. 2,946,725, Jul.
26, 1960, to Norris et al. and in U.S. Pat. No. 4,051,234 to Gieske
et al. Examples of other antimicrobial agents include
chlorhexidine, triclosan, triclosan monophosphate, and flavor oils
such as thymol. Triclosan and other agents of this type are
disclosed in Parran, Jr. et al., U.S. Pat. No. 5,015,466, and U.S.
Pat. No. 4,894,220 to Nabi et al. These agents may be present at
levels of from about 0.01% to about 1.5%, by weight of the
dentifrice composition. Of the above antimicrobial agents, examples
of some which provide an unwanted taste include, for example,
chlorhexidine, triclosan, and thymol. The unwanted tastes often
associated with these types of antimicrobial agents include bitter,
dirty, earthy, sour, and/or astringent.
[0058] Another oral care active agent includes antitartar agents.
One example of an antitartar agent is a pyrophosphate salt as a
source of pyrophosphate ion. The pyrophosphate salts useful in the
present compositions include, for example, the mono-, di- and
tetraalkali metal pyrophosphate salts and combinations thereof.
Disodium dihydrogen pyrophosphate (Na.sub.2H.sub.2P.sub.2O.sub.7),
sodium acid pyrophosphate, tetrasodium pyrophosphate
(Na.sub.4P.sub.2O.sub.7), and tetrapotassium pyrophosphate
(K.sub.4P.sub.2O.sub.7) in their unhydrated as well as hydrated
forms are further species. In compositions of the present
invention, the pyrophosphate salt may be present in one of three
ways: predominately dissolved, predominately undissolved, or a
combination of dissolved and undissolved pyrophosphate. The amount
of pyrophosphate salt useful in making these compositions is any
tartar control effective amount. In varying embodiments, the amount
of pyrophosphate salt is from about 1.5% to about 15%, from about
2% to about 10%, or about 3% to about 8%, by weight of the oral
care composition.
[0059] An additional example of an oral care active is a bleaching
agent. Bleaching agents are generally agents which whiten teeth.
Examples of bleaching agents include peroxides, perborates,
percarbonates, peroxyacids, persulfates, and combinations thereof.
Suitable peroxide compounds include hydrogen peroxide, urea
peroxide, calcium peroxide, sodium peroxide, zinc peroxide, or
combinations thereof. One example of a percarbonate is sodium
percarbonate. An example of a persulfate includes oxones. The
following amounts represent the amount of peroxide raw material,
although the peroxide source may contain ingredients other than the
peroxide raw material. For example, the peroxide source could be a
solution a peroxide raw material and a carrier material. Generally,
the present composition may contain from about 0.01% to about 30%
of peroxide raw material. In other embodiments, the peroxide raw
material is from about 0.1% to about 10% or from about 0.5% to
about 5%, by weight of the oral care composition. Of these
bleaching agents, examples of some which provide an unwanted taste
within an oral care composition include, for example, peroxide and
percarbonate. The unwanted tastes often associated with these
bleaching agents include dirty, chemical, and/or sour.
[0060] Another oral care active is a bad breath reduction agent.
These agents generally work to reduce breath malodor. Examples of
bad breath reduction agents include copper salts and carbonyl
compounds such as ascorbic acid [3-oxo-L-gulofuranolactone];
cis-jasmone[3-methyl-2-(2-pentenyl-2-cyclopentenone];
2,5-dimethyl-4-hydroxy-3(2H)-furanone;
5-ethyl-3-hydroxy-4-methyl-2(5H)-furanone; vanillin
[4-hydroxy-3-methoxybenzaldehyde]; ethyl vanillin; anisaldehyde
[4-methoxybenzaldehyde]; 3,4-methylenedioxybenzaldehyde;
3,4-dimethoxybenzaldehyde; 4-hydroxybenzaldehyde;
2-methoxybenzaldehyde; benzaldehyde;
cinnamaldehyde[3-phenyl-2-propenal]; hexyl cinnamaldehyde;
.alpha.-methyl cinnamaldehyde; ortho-methoxy cinnamaldehyde; or
combinations thereof. Without being limited by theory, it is
believed some bad breath reduction agents work as "traps" by
reacting with the thiol or sulfide and forming products with less
odor impact. Of these bad breath reduction agents, an example of
one which provide an unwanted taste within an oral care composition
include, for example, anisaldehyde. Generally, a flavor is not
considered a bad breath reduction agent. The unwanted tastes often
associated with these types of bad breath reduction agents include
chemical, plastic, bitter, and/or sour.
Metal Salts
[0061] Another potential component in an oral care composition is a
metal salt. Metal salts have a wide range of functions from
antimicrobial agents to sensitivity agents and/or buffers. In one
embodiment, the metal salt comprises a zinc salt, stannous salt,
potassium salt, copper salt, or a combination thereof. In a further
embodiment, the zinc salt is selected from the group consisting of
zinc fluoride, zinc chloride, zinc iodide, zinc chlorofluoride,
zinc actetate, zinc hexafluorozirconate, zinc sulfate, zinc
lactate, zinc tartrate, zinc gluconate, zinc citrate, zinc malate,
zinc glycinate, zinc pyrophosphate, zinc metaphosphate, zinc
oxalate, zinc phosphate, zinc carbonate, zinc oxide, and
combinations thereof. In another embodiment, the zinc salt
comprises zinc chloride, zinc citrate, zinc gluconate, zinc
lactate, zinc oxide, or combinations thereof.
[0062] In an additional embodiment, the potassium salt is selected
from the group consisting of potassium nitrate, potassium citrate,
potassium oxalate, potassium bicarbonate, potassium acetate,
potassium chloride, and combinations thereof. In a further
embodiment, the potassium salt comprises potassium nitrate,
potassium citrate, potassium chloride, or combinations thereof.
[0063] In an additional embodiment, the copper salt is selected
from the group consisting of copper fluoride, copper chloride,
copper iodide, copper chlorofluoride, copper actetate, copper
hexafluorozirconate, copper sulfate, copper lactate, copper
tartrate, copper gluconate, copper citrate, copper malate, copper
glycinate, copper pyrophosphate, copper metaphosphate, copper
oxalate, copper phosphate, copper carbonate, and combinations
thereof. In a further embodiment, the copper salt comprises copper
gluconate, copper acetate, copper glycinate, or a combination
thereof.
[0064] In another embodiment, the stannous salt is selected from
the group consisting of stannous fluoride, stannous chloride,
stannous iodide, stannous chlorofluoride, stannous actetate,
stannous hexafluorozirconate, stannous sulfate, stannous lactate,
stannous tartrate, stannous gluconate, stannous citrate, stannous
malate, stannous glycinate, stannous pyrophosphate, stannous
metaphosphate, stannous oxalate, stannous phosphate, stannous
carbonate, stannous gluconate, and combinations thereof. In a
further embodiment, the stannous salt comprises stannous fluoride,
stannous chloride, stannous chloride dihydrate, stannous fluoride,
stannous lactate, stannous gluconate, stannous sulfate, or a
combination thereof.
[0065] Dentifrices containing stannous salts, particularly stannous
fluoride and stannous chloride, are described in U.S. Pat. No.
5,004,597 to Majeti et al. Other descriptions of stannous salts are
found in U.S. Pat. No. 5,578,293 issued to Prencipe et al. and in
U.S. Pat. No. 5,281,410 issued to Lukacovic et al. In addition to
the stannous ion source, other ingredients needed to stabilize the
stannous may be included, such as the ingredients described in
Majeti et al. and Prencipe et al.
[0066] Some examples of metal salts which give an off taste include
zinc chloride, zinc citrate, copper gluconate, zinc gluconate, or
combinations thereof. The off taste associated with these types of
metal salts are dirty, dry, earthy, metallic, sour, bitter, and
astringent.
[0067] The metal salt will be present in an amount from about 0.05%
to about 11%, by weight of the oral care composition in one
embodiment. In other embodiments, the metal salts are present in an
amount of from about 0.5 to about 7% or from about 1% to about 5%.
In additional embodiments, the stannous salts are present in an
amount of from about 0.1 to about 7% or from about 1% to about 5%
or from about 1.5% to about 3% by weight of the oral care
composition. In certain embodiments, the amount of zinc or copper
salts used in the present invention can range from about 0.01 to
about 5%. In other embodiments the amount of zinc or copper salts
are from about 0.05 to about 4% or from about 0.1 to about
3.0%.
Miscellaneous
[0068] In addition to the above, other components may be included
in the oral care compositions to achieve the desired benefit. These
miscellaneous components include, for example, chelating agents,
abrasives, salivation agents, fillers, solvents, emollients,
refractive particles (ex. mica), thickeners, and extracts of
natural components.
[0069] The oral care composition and its components may contain any
combination of elements and properties as disclosed herein.
EXAMPLES
Consumer Test I
[0070] In order to show the effect of the addition of a TRPV1
activator and/or Vanitrope on the perception of taste in an oral
care composition, the following compositions are made and given to
consumers to sample.
TABLE-US-00004 +Vani- Control +VBE trope +Zingerone Zinc citrate
dihydrate 0.79 0.79 0.79 0.79 Sodium Citrate tribasic 0.27 0.27
0.27 0.27 dihydrate Sodium Fluoride 0.24 0.24 0.24 0.24 Stannous
Chloride 0.21 0.21 0.21 0.21 Dihydrate Sorbitol (70%) 45.00 45.00
45.00 45.00 Sodium Saccharin 0.25 0.25 0.25 0.25 Vanitrope 0.04
Zingerone 0.04 VBE 0.003 Hydroxyethyl cellulose 0.30 0.30 0.30 0.30
250M Sodium 1.30 1.30 1.30 1.30 Carboxymethylcellulose Carrageenan
Mixture 0.70 0.70 0.70 0.70 Titanium Dioxide, 0.53 0.53 0.53 0.53
Anatase Hydrated Silica 17.00 17.00 17.00 17.00 amorphous Z119
Sodium Alkyl Sulfate 5.00 5.00 5.00 5.00 (28%) Flavor 1.00 1.00
1.00 1.00 Water Purified, USP QS QS QS QS
[0071] The base of the control dentifrice (i.e. everything but the
flavor) is made via vacuum mixing. The flavor is added in a second
step my speed mixing to complete the control. The additional
compositions are then made by speed mixing into the control base
the TRPV1 activator and/or vanitrope plus flavor at the stated
levels. The samples are then placed in tubes and delivered to the
testing facility.
[0072] At the testing facility, panelists are provided with a
generic brush with 1.0 g of toothpaste. Each panelist has an
individual sink, mirror, disposable cup and paper towels. They are
asked to brush as they normally would at home. Before and after
brushing the panelist will answer a series of questions relating to
their experience with the toothpaste. The panelists are asked to
comment on their experience right after brushing and then at each
hour interval for three hours. The comments from the consumers are
translated into numerical values for comparison. The results for
the above compositions as it related to bothersome and bad
aftertaste are shown below.
TABLE-US-00005 Control +VBE +Zingerone +Vanitrope Bothersome (Hr 1)
2.5 0.8 1.1 1.5 Bothersome (Hr 2) 1.2 0.4 0.6 0.7 Bothersome (Hr 3)
0.7 0.3 0.4 0.4 Bad Aftertaste 2.4 1.0 1.8 1.5 (Hr 1) Bad
Aftertaste 1.0 0.4 0.5 0.9 (Hr 2) Bad Aftertaste 0.5 0.2 0.3 0.5
(Hr 3)
As can be seen from the above chart, each of the TRPV1 activators
(VBE and zingerone) showed an improved taste over the control for
both bothersome and bad aftertaste for each of hours 1-3 while
vanitrope showed a taste improvement for hours 1-3 for bothersome
and hours 1-2 for bad aftertaste.
[0073] Also included in the above testing are combinations of TRPV1
activators and/or vanitrope. The formulations for these tests are
below and the control is the same as that listed above.
TABLE-US-00006 +Vani- +VBE +VBE trope +Zinger- and and and one
Zingerone Vani- Zinger- and and trope one VBE Vanitrope Zinc
citrate dehydrate 0.79 0.79 0.79 0.79 Sodium Citrate tribasic 0.27
0.27 0.27 0.27 dihydrate Sodium Fluoride 0.24 0.24 0.24 0.24
Stannous Chloride Dihydrate 0.21 0.21 0.21 0.21 Sorbitol (70%)
45.00 45.00 45.00 45.00 Sodium Saccharin 0.25 0.25 0.25 0.25
Vanitrope 0.04 0.04 0.02 Zingerone 0.04 0.04 0.02 VBE 0.003 0.003
0.006 Hydroxyethyl cellulose 250M 0.30 0.30 0.30 0.30 Sodium
Carboxymethyl- 1.30 1.30 1.30 1.30 cellulose Carrageenan Mixture
0.70 0.70 0.70 0.70 Titanium Dioxide, Anatase 0.53 0.53 0.53 0.53
Hydrated Silica amorphous 17.00 17.00 17.00 17.00 Z119 Sodium Alkyl
Sulfate (28%) 5.00 5.00 5.00 5.00 Flavor 1.00 1.00 1.00 1.00 Water
Purified, USP QS QS QS QS
The results for the above compositions are shown below.
TABLE-US-00007 Vani- Vanitrope + Zinger- Con- trope + Vanitrope +
Zingerone + one + trol VBE Zingerone VBE VBE Bothersome 2.5 09. 2.0
1.6 1.2 (Hr 1) Bothersome 1.2 0.2 1.1 0.8 0.5 (Hr 2) Bothersome 0.7
0.1 0.6 0.7 0.1 (Hr 3) Bad Aftertaste 2.4 0.8 0.8 1.4 0.9 (Hr 1)
Bad Aftertaste 1.0 0.2 0.2 0.3 0.5 (Hr 2) Bad Aftertaste 0.5 0.1
0.1 0.3 0.2 (Hr 3)
As can be seen from the above results, the various combinations of
TRPV1 activators and/or vanitrope showed an improvement over the
control in both bothersome and bad taste at all of hours 1-3 except
the combination of all 3 which showed an equivalent taste at hour
3. Thus, when comparing to the results of the individual TRPV1
activators or vanitrope above, while VBE tends to give to best
result at hour 1, some of the combinations give better results at
hours 2 and 3, depending on the measurement used. Interestingly,
however, the combination of vanitrope, zingerone, and VBE, while
not getting the best results in the testing as to reduction of
bothersome or bad aftertaste, seems to have a preferred taste to
the consumer over the other combinations tried. Thus, while it is
not the best at reducing off taste, consumers seem to prefer
it.
[0074] Additional panel testing with rinses made with VBE and long
lasting coolants shows that the compositions containing VBE provide
longer lasting pleasant sensory experiences, which are described as
less sourness and cooling. Rinses made with CPC and lower levels of
ethanol could still provide an ethanol like clean signal due to the
VBE.
Example Product I
Metal Salt Containing Dentifrice
[0075] The dentifrices are made using conventional methods and are
shown below with amounts in weight %.
TABLE-US-00008 Ingredient IA IB IC ID IE Calcium Carbonate 40.00
Binders 1.00 1.8 1.00 1.00 0.20 Thickeners 2.00 1.00 1.25 0.4 0.8
Color Solution (1%) 0.05 0.05 0.175 Dibasic Calcium 35.00 Phosphate
Dihydrate Flavor.sup.1 1.00 1.00 1.00 1.00 1.00 Coolants 0.03 0.24
0.20 0.50 0.58 VBE 0.01 0.01 0.01 0.01 0.01 Glycerin USP 16.489
15.00 Poloxamer 407 NF 0.20 Monosodium Orthophosphate Potassium
Nitrate 5.00 Saccharin Sodium USP 0.47 0.25 0.30 0.300 0.58 Silica
Abrasive 24.00 12.50 17.00 Sodium Lauryl Sulfate 7.50 7.00 5.50
7.00 4.00 (27.9% soln) NaOH 50% Solution 1.00 Sodium 0.76 0.76 0.76
0.76 Monofluorophosphate Sodium Fluoride 0.32 Sodium Gluconate 1.00
Stannous Chloride 1.00 Dihydrate Zinc Citrate 0.50 Sodium
Phosphate, 3.20 Tribasic Humectant 10.50 33.00 12.00 14.00 57.00
Tetra Sodium 0.50 0.50 3.85 Pyrophosphate, Anhydrous Sodium Acid
1.00 Pyrophosphate Titanium Dioxide 0.50 0.50 0.25 Water, Purified,
USP QS QS QS QS QS Ingredient IF IG IH IJ IK Calcium Carbonate
40.00 Binders 1.00 1.8 1.00 1.00 0.20 Thickeners 0.5 1.00 1.25 0.4
0.8 Color Solution (1%) 0.05 0.05 0.175 Dibasic Calcium 35.00
Phosphate Dihydrate Flavor.sup.1 1.5 1.0 0.8 1.00 0.8 Coolants 0.5
0.2 0.08 VBE 0.01 Capsaicin 0.001 Piperine 0.002 Vanitrope 0.06
0.10 Zingerone 0.04 Glycerin USP 16.489 15.00 0.10 Potassium
Nitrate 5.00 Saccharin Sodium USP 0.47 0.25 0.30 0.300 0.58 Silica
Abrasive 24.00 12.50 17.00 Sodium Lauryl Sulfate 7.50 7.00 5.50
7.00 4.00 (27.9% soln) NaOH 50% Solution 1.00 Sodium 0.76 0.76 0.76
0.76 Monofluorophosphate Sodium Fluoride 0.32 Sodium Gluconate 1.00
Stannous Chloride 1.00 Dihydrate Zinc Citrate 0.50 Sodium
Phosphate, 3.20 Tribasic Humectant 12.00 33.00 12.00 14.00 57.00
Tetra Sodium 0.50 0.50 3.85 Pyrophosphate, Anhydrous Sodium Acid
1.00 Pyrophosphate Titanium Dioxide 0.50 0.50 0.25 Water, Purified,
USP QS QS QS QS QS .sup.1Flavor comprises about 31.3% menthol
supplying about 500 ppm menthol.
Example Product II
Mouth Rinse Compositions
[0076] Mouth rinse compositions are made using conventional methods
and are shown below with amounts of components in weight %.
TABLE-US-00009 Ingredient IIA IIB IIC Ethanol, USP 190 proof 15.000
15.000 15.000 Glycerin 7.500 7.500 7.500 Polysorbate 80, NF 0.120
0.120 0.120 Flavor 0.160 0.160 0.160 Saccharin Sodium 0.067 0.067
0.060 Color Solution 0.040 0.040 0.040 VBE 0.003 0.005 0.001
Zingerone 0.01 Vanitrope 0.008 0.005 Cetylpyridinium Chloride 0.045
0.045 0.045 Benzoic Acid 0.005 0.005 0.005 Sodium Benzoate 0.054
0.054 0.054 Water QS QS QS
Example Product III
Peroxide Mouth Rinse Compositions
[0077] Peroxide-containing mouth rinse compositions are shown below
with amounts of components in weight %. These compositions are made
using conventional methods. The mouth rinse compositions provide a
pleasant high-impact minty taste during use and noticeable
long-lasting fresh breath.
TABLE-US-00010 Ingredient IIIA IIIB IIIC IIID IIIE IIIF 35%
H.sub.2O.sub.2 solution 4.286 4.286 4.286 2.143 4.286 4.286 Coolant
0.075 0.02 0.04 0.04 0.03 0.04 VBE 0.003 0.005 0.01 0.005 Capsaicin
0.0003 0.00001 Piperine 0.0001 0.00001 Zingerone 0.005 0.002 0.004
Vanitrope 0.008 0.002 0.005 Flavor 0.145 0.135 0.135 0.15 0.135
0.135 Calcium Chloride 0.025 0.025 0.02 0.025 0.025 Poloxamer 407
0.75 0.75 0.750 0.10 0.10 0.10 Glycerin 11.00 11.00 11.00 20.00
20.00 20.00 Propylene Glycol 3.00 3.00 4.00 4.00 4.00 Sucralose
0.05 -- -- Sodium Saccharin 0.08 -- 0.068 0.06 0.08 0.06
Polyphosphate 1.00 Phytic Acid 2.00 Cetyl Pyridinium Chloride 0.074
0.10 0.10 Na Citrate 0.212 0.212 Citric Acid 0.052 0.052 0.052
Alcohol, USP 5.00 Water, Purified, USP QS QS QS QS QS QS
Example Product IV
Tartar Control Dentifrice compositions
[0078] The dentifrices are made using conventional methods and are
shown below with amounts in weight %.
TABLE-US-00011 Ingredient VA VB VC VD VE Calcium Peroxide FCC 0.10
Thickener 5.0 2.5 4.5 0.80 5.0 Binder 0.60 0.75 0.40 0.45 0.70
Polymer 0.20 Color Solution (1%) 0.05 0.05 0.50 0.75 0.175 Flavor
0.15 Coolant 0.02 0.05 0.02 VBE 0.01 0.05 0.005 0.001 Capsaicin
0.005 Piperine 0.005 Zingerone 0.02 0.01 0.02 Vanitrope 0.02 0.08
0.04 0.08 Glycerin USP 99.7% 9.00 11.85 33.164 9.00 Poloxamer 407
NF 1.00 0.20 Tetra Potassium 6.38 Pyrophosphate (60% Soln)
Propylene Glycol USP 10.00 Crest Saccharin Sodium USP 0.46 0.50
0.45 0.40 0.58 Granular Sodium Acid 2.10 4.00 1.00 Pyrophosphate
Silica Abrasive 22.00 31.00 20.00 21.00 17.00 Silica Thickening
2.00 Sodium Bicarbonate USP 1.50 9.00 Sodium Carbonate 0.50
Anhydrous NF Sodium Hydroxide 50% 1.74 2.20 Solution Sodium Lauryl
Sulfate 4.00 5.00 3.00 4.00 4.00 (27.9% soln) Sodium 0.76 0.76 0.76
0.76 0.76 Monofluorophosphate Sorbitol Solution USP 24.28 24.54
3.985 44.686 56.885 Tetra Sodium 2.05 5.045 3.85 3.85
Pyrophosphate, Anhydrous Titanium Dioxide 0.50 1.00 0.25 Titanium
Dioxide/ 0.60 0.30 Carnauba Wax Prills Water, Purified, USP QS QS
QS QS QS
[0079] The dimensions and values disclosed herein are not to be
understood as being strictly limited to the exact numerical values
recited. Instead, unless otherwise specified, each such dimension
is intended to mean both the recited value and a functionally
equivalent range surrounding that value. For example, a dimension
disclosed as "40 mm" is intended to mean "about 40 mm."
[0080] Every document cited herein, including any cross referenced
or related patent or application is hereby incorporated herein by
reference in its entirety unless expressly excluded or otherwise
limited. The citation of any document is not an admission that it
is prior art with respect to any invention disclosed or claimed
herein or that it alone, or in any combination with any other
reference or references, teaches, suggests or discloses any such
invention. Further, to the extent that any meaning or definition of
a term in this document conflicts with any meaning or definition of
the same term in a document incorporated by reference, the meaning
or definition assigned to that term in this document shall
govern.
[0081] While particular embodiments of the present invention have
been illustrated and described, it would be obvious to those
skilled in the art that various other changes and modifications can
be made without departing from the spirit and scope of the
invention. It is therefore intended to cover in the appended claims
all such changes and modifications that are within the scope of
this invention.
* * * * *