U.S. patent application number 16/178788 was filed with the patent office on 2019-05-09 for oral compositions containing zinc, stannous and fluoride ion sources.
This patent application is currently assigned to Colgate-Palmolive Company. The applicant listed for this patent is Colgate-Palmolive Company. Invention is credited to Linh FRUGE, Michael PRENCIPE, Kavita VEMISHETTI.
Application Number | 20190133903 16/178788 |
Document ID | / |
Family ID | 51168464 |
Filed Date | 2019-05-09 |
United States Patent
Application |
20190133903 |
Kind Code |
A1 |
VEMISHETTI; Kavita ; et
al. |
May 9, 2019 |
Oral Compositions Containing Zinc, Stannous and Fluoride Ion
Sources
Abstract
An oral care composition containing a source of stannous ions, a
source of fluoride ions and an insoluble source of zinc ions, such
as zinc oxide. The composition contains an amount of citric acid
sufficient to increase the level of soluble zinc ions.
Inventors: |
VEMISHETTI; Kavita;
(Brooklyn, NY) ; FRUGE; Linh; (Hillsborough,
NJ) ; PRENCIPE; Michael; (West Windsor, NJ) |
|
Applicant: |
Name |
City |
State |
Country |
Type |
Colgate-Palmolive Company |
New York |
NY |
US |
|
|
Assignee: |
Colgate-Palmolive Company
New York
NY
|
Family ID: |
51168464 |
Appl. No.: |
16/178788 |
Filed: |
November 2, 2018 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
|
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15319636 |
Dec 16, 2016 |
10154948 |
|
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PCT/US2014/043427 |
Jun 20, 2014 |
|
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16178788 |
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Current U.S.
Class: |
1/1 |
Current CPC
Class: |
A61Q 11/00 20130101;
A61K 8/19 20130101; A61K 8/24 20130101; A61K 8/365 20130101; A61K
8/21 20130101; A61K 8/27 20130101 |
International
Class: |
A61K 8/27 20060101
A61K008/27; A61K 8/24 20060101 A61K008/24; A61K 8/21 20060101
A61K008/21; A61K 8/365 20060101 A61K008/365; A61Q 11/00 20060101
A61Q011/00; A61K 8/19 20060101 A61K008/19 |
Claims
1. An oral care composition comprising in a single phase: (a) an
orally acceptable vehicle; (b) a source of fluoride ions; (c) a
source of stannous ions; (d) an insoluble source of zinc ions; (e)
a buffering system comprising citric acid wherein the amount of
citric acid is 0.5-4% by weight of the composition, and wherein the
composition has a total water content of less than 15% by weight,
based on the weight of the composition.
2-5. (canceled)
6. The composition of claim 1 wherein the insoluble source of zinc
ions comprises a zinc salt of an organic acid.
7. The composition of claim 3, wherein the insoluble source of zinc
ions comprises zinc oxide, zinc phosphate, zinc pyrophosphate or a
mixture thereof.
8. The composition of claim 1 wherein the source of fluoride ions
and the source of stannous ions comprises stannous fluoride.
9. The composition of claim 1 comprising at least one polyphosphate
salt selected from the group consisting of inorganic polyphosphate
salts which have equal to or less than three phosphorous atoms.
10. The composition of claim 6, wherein the at least one
polyphosphate is selected from the group consisting of tetrasodium
pyrophosphate, sodium tripolyphosphate, and mixtures thereof;
wherein the total polyphosphate comprises from 1 to 10 wt % of the
composition
11. The composition of claim 1 wherein the buffering system
comprises a mixture of citric acid and trisodium citrate.
12. The composition of claim 1 comprising polyvinylpyrrolidone, a
gum, or a mixture thereof.
13. The composition of claim 1 comprising a modified cellulose such
as carboxymethyl cellulose.
14. The composition of claim 1 further comprising at least one
humectant selected from the group consisting of glycerin,
polyethylene glycol, propylene glycol, and mixtures thereof.
15. The composition of claim 1 wherein the composition is a
dentifrice comprising one or more of an abrasive, a surfactant, a
foaming agent, a vitamin, a polymer, a whitening agent, an enzyme,
a humectant, a thickener, an antimicrobial agent, a preservative,
L-arginine, a flavoring, or a coloring agent.
16. The composition of claim 1 in a single phase.
17. An oral care composition comprising: (a) 0.5-3 wt. % citric
acid; (b) 0.5-10 wt % Trisodium citrate; (c) 0.1-5 wt % Zinc oxide;
(d) 0.1-5 wt % Stannous fluoride; (e) 10-50 wt % Glycerin; (f) 1-25
wt. % Propylene glycol; optionally comprising one or more of: (g)
0.1-12 wt % xanthan gum; (h) 0.25-10 wt % polyvinylpyrrolidone
(PVP); (i) 0.2-1.5% wt. % carboxymethylcellulose (CMC); (j) 5-60 wt
% Silica (total); (k) 0.1-10 wt % Tetrasodium Pyrophosphate (TSPP);
(l) 0- 5 wt % Sodium acid pyrophosphate (SAPP); (m) 0.1-10 wt %
Sodium Tripolyphosphate (STPP); (n) 0.1-10 wt % Sodium lauryl
sulfate (SLS); (o) 0.1-10 wt % Cocamidopropyl betaine.
18-19. (canceled)
20. A method of treating or preventing a disease or condition of
the oral cavity comprising contacting an oral cavity surface of a
patient in need thereof with the composition of claim 1 any one of
the foregoing claims.
21. The method of claim 20, wherein the disease or condition of the
oral cavity is biofilm formation, plaque formation, oral
inflammation or a combination thereof
Description
CROSS-REFERENCE TO RELATED PATENT APPLICATIONS
[0001] The present application is continuation of U.S. application
Ser. No. 15/319,636, filed Dec. 16, 2016, which is a U.S. national
stage application under 35 U.S.C. .sctn. 371 of PCT Application No.
PCT/US2014/043427 filed Jun. 20, 2014, the entirety of which is
incorporated herein by reference.
BACKGROUND
[0002] There is a need for agents in oral care products that
provide enhanced benefits including antibacterial, anticavity,
enamel erosion prevention, breath freshening, and the like. The
antibacterial effects of zinc ions, stannous ions and/or fluoride
ions in the oral cavity are described in the art and numerous
attempts have been made to prepare dentifrice compositions
incorporating zinc ions, stannous ions and/or fluoride ions to take
advantage of therapeutic benefits such as reduced plaque, gum
inflammation, gingivitis, and the like. In particular, soluble zinc
salts, such as zinc citrate, have been used in dentifrice
compositions.
[0003] Insoluble zinc ion sources, such as zinc oxide, have also
been disclosed for use in dentifrices, see for example US Patent
Application Publication 2012/0207686 ("the '686 publication").
However, use of insoluble zinc salts often is limited by the low
levels of zinc ions available for delivery to tooth surfaces, and
undesirable consumer astringency when higher levels of zinc are
used.
[0004] It would be desirable to provide an oral care composition
which exhibits even greater efficacy than previously-known
compositions in its prevention and/or reduction of biofilm, plaque,
oral inflammation, and the like.
BRIEF SUMMARY
[0005] The present invention relates to an oral care composition,
for example a dentifrice composition, that can effectively combine
a stannous ion source, a fluoride ion source, and an insoluble zinc
ion source in a low water, preferably single phase, system that has
efficacious delivery the ions to the oral cavity. Stannous and zinc
ions have been found to help in the reduction/prevention of oral
inflammation such as gingivitis and periodontitis, plaque
formation, oral biofilm formation, tooth sensitivity, and improved
breath benefits.
[0006] The present invention concerns an oral care composition
comprising: [0007] (a) an orally acceptable carrier; [0008] (b) a
source of fluoride ions; [0009] (c) a source of stannous ions;
[0010] (d) an insoluble source of zinc ions; [0011] (e) a buffering
system comprising citric acid wherein the amount of citric acid is
at least 1% by weight of the composition, and wherein the
composition has a total water content of less than 15% by
weight.
[0012] In another aspect, the embodiments described herein provide
a method for the treatment and prevention of bacterial plaque
accumulation comprising administering to the oral cavity the
dentifrice composition described above.
[0013] It should be understood that the detailed description and
specific examples, while indicating the preferred embodiment of the
invention, are intended for purposes of illustration only and are
not intended to limit the scope of the invention.
DETAILED DESCRIPTION
[0014] As used throughout, ranges are used as shorthand for
describing each and every value that is within the range. Any value
within the range can be selected as the terminus of the range. In
addition, all references cited herein are hereby incorporated by
referenced in their entireties. In the event of a conflict in a
definition in the present disclosure and that of a cited reference,
the present disclosure controls.
[0015] Unless otherwise specified, all percentages and amounts
expressed herein and elsewhere in the specification should be
understood to refer to percentages by weight. The amounts given are
based on the active weight of the material.
[0016] In this description, unless otherwise stated, the use of the
singular also includes the plural. For example, "a stannous ion
source" also comprehends the case where more than one stannous ion
source is used.
[0017] As used herein, the words "preferred" and "preferably" refer
to embodiments of the invention that afford certain benefits, under
certain circumstances. However, other embodiments also may be
preferred, under the same or other circumstances. Furthermore, the
recitation of one or more preferred embodiments does not imply that
other embodiments are not useful, and is not intended to exclude
other embodiments from the scope of the invention.
Insoluble Zinc Ion Source
[0018] The insoluble zinc ion source in one embodiment is an
insoluble zinc ion salt. As used herein the term "insoluble" means
the material or compound has a solubility of less than 0.1 wt. %
(based on the weight of the composition) in a 25.degree. C. water
solution at pH 7. It also will be understood that at lower or
higher pH, the insoluble zinc ion sources may become significantly
more soluble. Examples of suitable insoluble zinc ion sources
include zinc oxide, zinc phosphate, zinc pyrophosphate, and other
zinc compounds. The insoluble zinc ion source preferably is zinc
oxide.
[0019] In general, the higher the level of solubilized zinc ions
available for delivery to oral surfaces, the higher the level of
efficacy. The present invention provides for high levels of zinc
ions to be present in the composition from the insoluble zinc ion
source. Typically, a composition of the invention has greater than
50% soluble zinc ions (e.g. for a composition with 1% by weight
(1.0) of an insoluble zinc ion source, the amount of zinc would be
greater than 0.5% (0.5) after aging for 13 weeks at 40.degree. C.),
in other embodiments greater that 60%, greater than 70%, or greater
than 80%, after aging for 13 weeks at 40.degree. C.
[0020] The amount of zinc ion source typically will be present in
an amount of from 0.1% to 2 wt. %, by weight of the final
composition. In one embodiment, the zinc ion source is present in
an amount of from 0.5 to 1.5%, or from 0.9% to 1.1%.
Stannous Ion Source
[0021] The compositions of the present invention comprise a
stannous ion source. The stannous ion source can be a soluble or an
insoluble compound of stannous with inorganic or organic counter
ions. Examples include the fluoride, chloride, chlorofluoride,
acetate, hexafluorozirconate, sulfate, tartrate, gluconate,
citrate, malate, glycinate, pyrophosphate, metaphosphate, oxalate,
phosphate, carbonate salts and oxides of stannous.
[0022] Oral compositions containing stannous salts, particularly
stannous fluoride and stannous chloride, are described in U.S. Pat.
No. 5,004,597. Other descriptions of stannous salt dentifrices are
found in U.S. Pat. No. 5,578,293. The preferred stannous salts are
stannous fluoride and stannous chloride dihydrate. Other examples
of stannous salts include stannous acetate, stannous tartrate and
sodium stannous citrate.
[0023] In general, the higher the level of solubilized stannous
ions available for delivery to oral surfaces, the higher the level
of efficacy. The present invention provides for high levels of
stannous ions to be present in the composition from the insoluble
zinc ion source. Typically, a composition of the invention has
greater than 50% soluble stannous ions, in other embodiments
greater that 60%, greater than 70%, greater than 80%, or greater
than 90% after ageing for 13 weeks at 40.degree. C.
[0024] The stannous ion source typically will be present in an
amount of from 0.05% to 5%, by weight of the final composition. In
one embodiment, the stannous ion source is present in an amount of
from 0.1 to 1%, or from 0.35% to 0.55%.
[0025] Stannous and zinc ions are derived from the ion source(s)
found in the oral care composition in an effective amount. An
effective amount is defined as from at least 1000 ppm metal (zinc
plus stannous) ion, preferably 2,000 ppm to 15,000 ppm. More
preferably, metal ions are present in an amount from 3,000 ppm to
13,000 ppm and even more preferably from 4,000 ppm to 10,000 ppm.
This is the total amount of metal ions (stannous and zinc) that is
present in the compositions for delivery to the tooth surface.
[0026] The combined metal ion sources (stannous and zinc) typically
will be present in an amount of from 0.15% to 7%, by weight of the
final composition. Preferably, the metal ion sources are present in
an amount of from 0.6 to 2.5%, more preferably from 1.25% to
1.65%.
Fluoride Ion Source
[0027] The fluoride ion source herein is a fluoride source capable
of providing free fluoride ions. Soluble fluoride ion sources
include sodium fluoride, stannous fluoride, indium fluoride, zinc
fluoride, and sodium monofluorophosphate. Sodium fluoride and
stannous fluoride are the preferred soluble fluoride ion sources.
U.S. Pat. No. 2,946,725 and U.S. Pat. No. 3,678,154, disclose such
fluoride ion sources as well as others.
[0028] The fluoride ion source in the present compositions
preferably is present as a solid dispersion in the composition
during storage, prior to actual brushing usage of the composition
by a consumer. The level of water in the present compositions is
too low to permit the fluoride source to dissolve in the
composition during storage. Thus, interaction between the fluoride
ion and other ingredients such the polyphosphate, or silica if
present, is minimized during storage, providing a stable
composition during storage. When the composition is contacted by
saliva and/or water at the time of brushing, the fluoride source
preferably will be dispersed and the active ion will be delivered
to the oral cavity.
[0029] The present compositions may contain a soluble fluoride ion
source capable of providing from 50 ppm to 3500 ppm, and preferably
from 500 ppm to 3000 ppm of free fluoride ions. To deliver the
desired amount of fluoride ions, fluoride ion source may be present
in the total oral care composition at an amount of from 0.1% to 5%,
in one embodiment from 0.2% to 1%, and even from 0.3 to 0.6%, by
weight of the total composition.
Buffering System
[0030] The compositions described herein also contain a buffering
system comprising citric acid. It has been surprisingly found that
an amount of citric acid greater than 0.6%, by weight of the oral
care composition will result in substantially more zinc ions and or
stannous ions being present in the composition, from the respective
zinc and/or stannous ion sources in the composition, when aged at
40.degree. C. for 8 or 13 weeks. In some embodiments the amount of
citric acid is 0.5-4 wt. % or 1-3 wt. %, or 1.1-1.5 wt. % or
1.8-2.2 wt. % or 1.3% or 2% by weight of the oral care composition.
In one embodiment the buffering system comprises citric acid and
sodium citrate, in particular trisodium citrate. Buffering agents,
as used herein, refer to agents that can be used to adjust the pH
of the compositions to a range of pH 3.0 to pH 10, more typically 6
to 8.
[0031] In addition to citric acid, other buffering agents which may
optionally be present include alkali metal hydroxides, ammonium
hydroxide, organic ammonium compounds, carbonates,
sesquicarbonates, borates, silicates, phosphates, imidazole, and
mixtures thereof. Specific buffering agents include monosodium
phosphate, trisodium phosphate, sodium benzoate, benzoic acid,
sodium hydroxide, potassium hydroxide, alkali metal carbonate
salts, sodium carbonate, imidazole, and pyrophosphate salts. Total
amounts of buffering agents typically are from 0.1% to 30%, or from
0.1% to 10%, or from 0.3% to 3%, by weight of the present
composition.
Total Water Content
[0032] Water employed in the preparation of commercially suitable
oral compositions should preferably be of low ion content and free
of organic impurities. In the dentifrice composition, water will
generally comprise less than 20 wt. %, or less than 15 wt. %, or
from less than 15% to greater than 10 wt. %, by weight of the
composition herein. The amounts of water include the free water
that is added plus that which is introduced with other materials,
such as with silica, surfactant solutions, and/or color
solutions.
Orally Acceptable Carrier
[0033] In certain embodiments, the present invention provides
compositions comprising an orally acceptable carrier or vehicle. As
used herein, an "orally acceptable carrier" and "orally acceptable
vehicle" are used interchangeably, and refer to a material or
combination of materials that is safe for use in the present
compositions, commensurate with a reasonable benefit/risk ratio,
with which the other ingredients may be associated while retaining
significant clinical efficacy. Such carrier materials should be
selected for compatibility with the other ingredients of the
compositions, and preferably do not substantially reduce the
efficacy of the other ingredients. Selection of specific carrier
components is dependent on the desired product form, including
dentifrices, rinses, gels, and paints.
[0034] Materials useful in carriers include but are not limited to:
adhesion agents, thickening agents, viscosity modifiers, diluents,
surfactants, anticalculus agents, abrasives, foam modulators,
whitening agents such as peroxides, peroxide activators, peroxide
stability agents, pH modifying agents, humectants, mouth feel
agents, sweeteners, flavorants, colorants, and combinations
thereof
Adhesion Agents
[0035] As used herein, an "adhesion agent" is a material or
combination of materials that enhances the retention of an
ingredient to an oral cavity surface onto which it is applied. Such
adhesion agents include without limitation: adhesives, film forming
materials and viscosity enhancers; for example, hydrophilic organic
polymers, hydrophobic organic polymers, silicone gums, silicone
adhesives, silicas, and combinations thereof. In one embodiment
adhesive agent is a methyl vinyl ether/maleic anhydride copolymer
having an average molecular weight (M.W.) of 30,000 to 1,000,000,
e.g. 300,000 to 800,000. Preparation of the polymethyl vinyl
ether-maleic anhydride copolymer is specifically set forth in U.S.
Pat. Nos. 5,047,490 and 4,627,977. The polymethyl vinyl ether
maleic anhydride copolymer is also commercially available under the
trade name Gantrez.RTM. AN from ISP (Ashland), Wayne, N.J.
Thickening Agents
[0036] The dentifrice compositions of the present invention may
incorporate one or more thickening agents which may act as a binder
system. The total amount of thickening agent is typically from 0%
to 3 wt. %, or from 0.1% to 1.5 wt. %, or from 0.2% -0.5 wt. % by
weight of the oral care composition
[0037] One such thickening agent is polyvinylpyrrolidone (PVP), in
particular crosslinked PVP, optionally in combination with a gum
such as xanthan gum. Other thickening agents include
polysaccharides, carbomers, poloxamers, modified celluloses, e.g.,
carboxymethyl cellulose (CMC), and mixtures thereof. In some
embodiments these thickening agents provide desirable consistency
and gellation to the low water oral care composition. It has
previously been known that gelling materials that provide desirable
rheology with water and humectant provide generally less
satisfactory rheology when the water is not present to activate
their gellation binding properties. This is believed to be
especially true of glycerin humectant. The thickening agent may
also comprise additional inorganic thickening agents.
[0038] Polysaccharides, including gums, that are suitable for use
herein as thickening agents include carageenans, gellan gum, locust
bean gum, xanthan gum, and mixtures thereof. Carageenan is a
polysaccharide derived from seaweed and has been known for use as a
binder or thickener in toothpastes, see, e.g., U.S. Pat. Nos.
6,187,293 B1 and 6,162,418. There are several types of carageenan
that may be distinguished by their seaweed source and/or by their
degree of and position of sulfation. Suitable for use in the
present invention are kappa carageenans, modified kappa
carageenans, iota carageenans, modified iota carageenans, and
mixtures thereof. Carageenans suitable for use herein include those
commercially available from the FMC Company under the series
designation "Viscarin," including but not limited to Viscarin TP
329, Viscarin TP 388, and Viscarin TP 389.
[0039] Gellan gum is another polysaccharide that is suitable for
use herein. It is a polysaccharide aerobically fermented by
pseudomonas elodea. It can also form an acceptable low water matrix
when it is present at a level of from 0.1% to 3%, preferably from
0.4% to 1.8% (w/w).
[0040] Locust bean gum and xanthan gum are also suitable
polysaccharides for use herein. Locust bean gum or xanthan gum as
thickening agents can form a stable and acceptable dentifrice
matrix when water level is lower than 10% in the composition.
[0041] Poloxamers are also suitable as thickening agents in the low
water matrix herein. Poloxamer is a synthetic block copolymer of
ethylene oxide and propylene oxide. It is available in several
types. Herein, poloxamer 407 is preferable. It can be partly
dissolved in water. When temperature is higher than 65.degree. C.,
it can dissolve in glycerin. POLOXAMER 407.RTM. is available, for
example, from the BASF CORPORATION, New Jersey, USA.
[0042] Carbomers are also suitable as thickening agents in a low
water matrix, especially in non-water matrix.
[0043] Modified celluloses such as hydroxyethyl cellulose and CMC
are also good thickening agents in low water matrix. Since the
water level is limited in the present compositions, modified
hydroxyethyl cellulose with a hydrophobic chain (C.sub.12-C.sub.20)
are preferred to increase the solubility and hydration of this
thickening agent in other low polar solvents, such as glycerin,
propylene glycol and polyethylene glycol (PEG).
[0044] The thickening agent may comprise inorganic thickening
agents such as colloidal magnesium aluminum silicate or finely
divided silica to further improve texture. Additional inorganic
thickening agents if present can be used in an amount from 0.1% to
15%, more preferably from 0.1% to 5%, by weight of the oral care
composition.
Humectant
[0045] The humectant serves to keep toothpaste compositions from
hardening upon exposure to air and certain humectants can also
impart desirable sweetness of flavor to toothpaste compositions.
Suitable humectants for use in the invention include glycerin,
sorbitol, polyethylene glycol, propylene glycol, xylitol, and other
edible polyhydric alcohols. Preferred are glycerin, polyethylene
glycol, polypropylene glycol, and mixtures thereof, especially
mixtures thereof. The humectant generally comprises from 0.1% to
70%, preferably from 1% to 60%, and more preferably from 15% to
55%, by weight of the composition.
[0046] The humectant is believed to have a significant impact on
the viscosity of the low water matrix. For example, when using
polysaccharide as the thickening agent in the composition, the
viscosity of the matrix will increase when the level of glycerin or
polyethylene glycol increases. On the contrary, the viscosity of
matrix will decrease when the level of propylene glycol increases
in the composition.
Anticalculus Agents
[0047] In various embodiments of the present invention, the oral
care composition may comprise an anticalculus (tartar control)
agent. Generally, tartar control agents are categorized as being
incompatible with some whitening agents, but embodiments of the
present invention incorporate tartar control agents and whitening
agents in a single phase whitening composition. Suitable
anticalculus agents include without limitation phosphates and
polyphosphates (for example pyrophosphates and tripolyphosphates),
polyaminopropanesulfonic acid (AMPS), hexametaphosphate salts, zinc
citrate trihydrate, polypeptides (such as polyaspartic and
polyglutamic acids), polyolefin sulfonates, polyolefin phosphates,
and diphosphonates (e.g., EHDP; AHP). The oral composition may
include a mixture of different anticalculus agents. In one
preferred embodiment, tetrasodium pyrophosphate (TSPP), sodium
tripolyphosphate (STPP), tetrapotassium pyrophosphate (TKPP), or
mixtures thereof are used. The anticalculus agent may comprise 0.1%
to 30%. or 0.1% to 15%, or 1% to 10%, or 2% to 6%, by weight.
Abrasives
[0048] An abrasive polishing material may also be included in the
toothpaste compositions. The abrasive polishing material
contemplated for use in the compositions of the present invention
can be any material that does not excessively abrade dentin.
Typical abrasive polishing materials include silicas including gels
and precipitates; aluminas; phosphates including orthophosphates,
polymetaphosphates, and pyrophosphates; and mixtures thereof.
Specific examples include dicalcium orthophosphate dihydrate,
calcium pyrophosphate, tricalcium phosphate, calcium
polymetaphosphate, insoluble sodium polymetaphosphate, hydrated
alumina, beta calcium pyrophosphate, calcium carbonate, and
resinous abrasive materials such as particulate condensation
products of urea and formaldehyde, and others such as disclosed in
U.S. Pat. No. 3,070,510. Mixtures of abrasives may also be, used.
If the dentifrice composition or particular phase comprises a
polyphosphate having an average chain length of 4 or more, calcium
containing abrasives and alumina are not preferred abrasives. The
most preferred abrasive is silica.
[0049] Silica dental abrasives of various types are preferred
because of their unique benefits of exceptional dental cleaning and
polishing performance without unduly abrading tooth enamel or
dentine. The silica abrasive polishing materials herein, as well as
other abrasives, generally have an average particle size ranging
between 0.1 to 30 microns, and preferably from 5 to 15 microns. The
abrasive can be precipitated silica or silica gels such as the
silica xerogels described in U.S. Pat. No. 3,538,230, and U.S. Pat.
No. 3,862,307. Preferred are the silica xerogels marketed under the
trade name "SYLOID.RTM." by the W. R. Grace & Company, Davison
Chemical Division. Also preferred are the precipitated silica
materials such as those marketed by the J. M. Huber Corporation
under the trade name, "ZEODENT.RTM.", particularly the silica
carrying the designation "Zeodent 119." The types of silica dental
abrasives useful in the toothpastes of the present invention are
described in more detail in U.S. Pat. No. 4,340,583. Silica
abrasives are also described in U.S. Pat. Nos. 5,589,160;
5,603,920; 5,651,958; 5,658,553; and 5,716,601. The abrasive in the
oral care compositions described herein is generally present at a
level of from 6% to 70% by weight of the composition. Preferably,
toothpastes contain from 10% to 50% of abrasive, by weight of the
composition.
Peroxide Source
[0050] The present invention may include a peroxide source in the
composition. The peroxide source is selected from the group
consisting of hydrogen peroxide, calcium peroxide, urea peroxide,
and mixtures thereof. The preferred peroxide source is calcium
peroxide. The following amounts represent the amount of peroxide
raw material, although the peroxide source may contain ingredients
other than the peroxide raw material. The present composition may
contain from 0.01% to 10%, preferably from 0.1% to 5%, more
preferably from 0.2% to 3%, and most preferably from 0.3% to 0.8%
of a peroxide source, by weight of the dentifrice composition.
Alkali Metal Bicarbonate Salt
[0051] The compositions also may include an alkali metal
bicarbonate salt. Alkali metal bicarbonate salts are soluble in
water and unless stabilized, tend to release carbon dioxide in an
aqueous system. Sodium bicarbonate, also known as baking soda, is
the preferred alkali metal bicarbonate salt. The alkali metal
bicarbonate salt also functions as a buffering agent. The present
composition may contain from 0.5% to 50%, preferably from 0.5% to
30%, more preferably from 2% to 20%, and most preferably from 5% to
18% of an alkali metal bicarbonate salt, by weight of the
dentifrice composition.
Surfactants
[0052] The compositions also may comprise surfactants, also
commonly referred to as sudsing agents. Suitable surfactants are
those that are reasonably stable and foam throughout a wide pH
range. The surfactant may be anionic, nonionic, amphoteric,
zwitterionic, cationic, or mixtures thereof. Anionic surfactants
useful herein include 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 and sodium coconut monoglyceride sulfonates
are examples of anionic surfactants of this type. Other suitable
anionic surfactants are sarcosinates, such as sodium lauroyl
sarcosinate, taurates, sodium lauryl sulfoacetate, sodium lauroyl
isethionate, sodium laureth carboxylate, and sodium dodecyl
benzenesulfonate. Mixtures of anionic surfactants can also be
employed. Many suitable anionic surfactants are disclosed in U.S.
Pat. No. 3,959,458.
[0053] Nonionic surfactants that can be used in the compositions
can broadly be defined as compounds produced by the condensation of
alkylene oxide groups (hydrophilic in nature) with an organic
hydrophobic compound which may be aliphatic or alkyl-aromatic in
nature. Examples of suitable nonionic surfactants include
poloxamers (sold under trade name PLURONIC.RTM.), polyoxyethylene,
polyoxyethylene sorbitan esters (sold under trade name
TWEENS.RTM.), Polyoxyl 40 hydrogenated castor oil, fatty alcohol
ethoxylates, 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 mixtures of such materials. The amphoteric
surfactants useful in the present invention can be broadly
described as derivatives of aliphatic secondary and tertiary amines
in which the aliphatic radical can be a straight chain or branched
and wherein one of the aliphatic substituents contains from 8 to 18
carbon atoms and one contains an anionic water-solubilizing group,
e.g., carboxylate, sulfonate, sulfate, phosphate, or phosphonate.
Other suitable amphoteric surfactants are betaines, specifically
cocamidopropyl betaine. Mixtures of amphoteric surfactants can also
be employed. Many of these suitable nonionic and amphoteric
surfactants are disclosed in U.S. Pat. No. 4,051,234. The present
composition typically comprises one or more surfactants each at a
level of from 0.25% to 12%, preferably from 0.5% to 8%, and most
preferably from 1% to 6%, by weight of the composition.
[0054] In an embodiment, the oral care composition includes a
surfactant system comprising sodium laurel sulfate (SLS),
cocamidopropyl betaine, or a mixture thereof.
Antimicrobial Agents
[0055] The present compositions may also include antimicrobial
agents. Included among such agents are water insoluble 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,
bisphenolic compounds and halogenated salicylanilides, benzoic
esters, and halogenated carbanilides, polyphenols, and herbals. The
water soluble antimicrobials include quaternary ammonium salts and
bis-biquanide salts, among others. Triclosan monophosphate is a
preferred additional water soluble antimicrobial agent. The
quaternary ammonium agents include those in which one or two of the
substitutes on the quaternary nitrogen has a carbon chain length
(typically alkyl group) from 8 to 20, typically from 10 to 18
carbon atoms while the remaining substitutes (typically alkyl or
benzyl group) have a lower number of carbon atoms, such as from 1
to 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 dimethylstearyl ammonium
chloride, cetyl pyridinium chloride, quaternized
5-amino-1,3-bis(2-ethyl-hexyl)-5-methyl hexa hydropyrimidine,
benzalkonium chloride, benzethonium chloride and methyl
benzethonium chloride are exemplary of typical quaternary ammonium
antibacterial agents. Other compounds are
bis[4-(R-amino)-1-pyridinium]alkanes as disclosed in U.S. Pat. No.
4,206,215, issued Jun. 3, 1980, to Bailey.
[0056] Other antimicrobials such as copper bisglycinate, copper
glycinate, zinc citrate, and zinc lactate may also be included.
Also useful are enzymes, including endoglycosidase, papain,
dextranase, mutanase, and mixtures thereof. Such agents are
disclosed in U.S. Pat. No. 2,946,725 and in U.S. Pat. No.
4,051,234. Specific antimicrobial agents include chlorhexidine,
triclosan, triclosan monophosphate, and flavor oils such as thymol.
Triclosan is a preferred antimicrobial agent for inclusion in the
present compositions. Triclosan and other agents of this type are
disclosed in U.S. Pat. No. 5,015,466 and U.S. Pat. No. 4,894,220.
These agents may be present at levels of from 0.01% to 1.5%, by
weight of the composition.
[0057] Titanium dioxide may also be added to the present
composition. Titanium dioxide is a white powder which adds opacity
to the compositions. Titanium dioxide generally comprises from
0.25% to 5%, by weight of the composition.
[0058] Coloring agents may also be added to the present
composition. The coloring agent may be in the form of an aqueous
solution, preferably 1% coloring agent in a solution of water.
Color solutions generally comprise from 0.01% to 5%, by weight of
the composition.
[0059] A flavor system can also be added to the compositions.
Suitable flavoring components include oil of wintergreen, oil of
peppermint, oil of spearmint, clove bud oil, menthol, anethole,
methyl salicylate, eucalyptol, cassia, 1-menthyl acetate, sage,
eugenol, parsley oil, oxanone, alpha-irisone, marjoram, lemon,
orange, propenyl guaethol, cinnamon, vanillin, ethyl vanillin,
heliotropine, 4-cis-heptenal, diacetyl, methyl-para-tert-butyl
phenyl acetate, and mixtures thereof. Coolants may also be part of
the flavor system. Preferred coolants in the present compositions
are the paramenthan carboxyamide agents such as
N-ethyl-p-menthan-3-carboxamide (known commercially as "WS-3") and
mixtures thereof. A flavor system is generally used in the
compositions at levels of from 0.001% to 5%, by weight of the
composition.
[0060] Sweetening agents can be added to the compositions. These
include saccharin, dextrose, sucrose, lactose, xylitol, maltose,
levulose, aspartame, sodium cyclamate, D-tryptophan,
dihydrochalcones, acesulfame, and mixtures thereof. Various
coloring agents may also be incorporated in the present invention.
Sweetening agents and coloring agents are generally used in
toothpastes at levels of from 0.005% to 5%, by weight of the
composition.
[0061] A herbal agent, including but not limited to, golden thread
extract, honeysuckle extract, and mixtures thereof, may also be
present in the compositions herein at levels of from 0.01% to
0.05%. Such herbal agents are believed to provide anti-bacterial
efficacy. Polyphenols may further be included at levels from 0.01%
to 2%. A preferred polyphenol is tea polyphenol.
[0062] An effective amount of a desensitizing agent may also be
incorporated into the present compositions. The desensitizing
agents include those selected from alkaline metal salts with a
chloride, nitrate sulfate, or acetate of a group II metal or
aluminum or polymerizable monomer to occlude the tubules, alkaline
metal or ammonium nitrate, ammonium oxylate, citric acid and sodium
citrate. Preferred salts are potassium nitrate, potassium citrate,
and mixtures thereof. Such desensitizing agents are disclosed in
e.g., U.S. Pat. No. 5,718,885.
[0063] A stain reducing agent such as Plasdone S-630 or aluminum
hydrate may further be added to the composition. Plasdone is
polyvinyl pyrrolidone (PVP) that can be synthesized by polymerizing
vinylpyrrolidone. Commercially, it has been produced as a series of
products having mean molecular weights ranging from 10,000 to
700,000. Herein, the low molecular weights and middle molecular
weights (from 10,000 to 100,000) are preferred. In order to remove
stain effectively, the level of PVP is preferably from 0.5% to 10%,
more preferably from 1.0% to 7.0%, and even more preferably from
1.5% to 5.0%.
[0064] The compositions of the present invention optionally
comprise a nutrient. Suitable nutrients include vitamins, minerals,
amino acids such as L-arginine, and mixtures thereof. Vitamins
include Vitamins C and D, thiamine, riboflavin, calcium
pantothenate, niacin, folic acid, nicotinamide, pyridoxine,
cyanocobalamin, para-aminobenzoic acid, bioflavonoids, and mixtures
thereof. Nutritional supplements include amino acids (such as
L-tryptophane, L-lysine, methionine, threonine, levocarnitine and
L-carnitine), lipotropics (such as choline, inositol, betaine, and
linoleic acid), and mixtures thereof.
[0065] It is understood that while general attributes of each of
the above categories of materials may differ, there may be some
common attributes and any given material may serve multiple
purposes within two or more of such categories of materials. All of
the ingredients in the compositions may have functions in addition
to their primary function, and may contribute to the overall
properties of the composition, including its stability, efficacy,
consistency, mouthfeel, taste, odor and so forth. Preferably, the
carrier ingredients are selected for compatibility with other
ingredients of the composition.
[0066] A type of product form of the present invention is a
dentifrice. The term "dentifrice" generally denotes formulations
which are used to clean the surfaces of the oral cavity. The
dentifrice is an oral composition that is not intentionally
swallowed for purposes of systemic administration of therapeutic
agents, but is applied to the oral cavity, used to treat the oral
cavity and then expectorated. Typically the dentifrice is used in
conjunction with a cleaning implement such as a toothbrush, usually
by applying it to the bristles of the toothbrush and then brushing
the accessible surfaces of the oral cavity. Preferably the
dentifrice is in the form of a paste or a gel (or a combination
thereof)
[0067] The oral care compositions of the invention are typically in
a single phase. However, in some embodiments, components are
physically separated, for example by using a dual compartmented
package. The dentifrice compositions may be a paste, gel, or any
configuration or combination thereof. A further embodiment of the
present invention includes dual-phase or multi-phase compositions
comprising the present low-water compositions as one phase and at
least one other separate phase comprising additional dentifrice
components to further enhance stability, performance and/or
aesthetics of the dentifrice product. For example, a dual phase
composition may comprise a first phase comprising the present
low-water composition with polyphosphate and ionic active(s) and a
separate second phase comprising additional active agents such as
bleaching agents, preferably a peroxide source, or a tooth surface
conditioning agent to provide improved cleaning, whitening,
anti-staining and mouth feel benefits. Examples of tooth
conditioning agents are polysiloxanes and modified polysiloxanes,
including diorganopolysiloxanes such as polydimethylsiloxane
(PDMS); alkyl- and alkoxy-dimethicone copolyols such as C.sub.12 to
C.sub.20 alkyl dimethicone copolyols; and aminoalkylsilicones.
These siloxane polymers are described for example in U.S. Pat. Nos.
5,759,523; 6,024,891; 6,123,950; 6,019,962; and 6,139,823.
[0068] The dispenser for the dentifrice compositions may be a tube,
pump, or any other container suitable for dispensing toothpaste. In
a dual phase oral composition, each oral composition will be
contained in a physically separated compartment of a dispenser and
dispensed side-by-side.
Methods of Use
[0069] In practicing the embodiments, the user need only apply the
oral care composition herein, to the tooth surfaces of a human or
animal, in the areas desired, in order to obtain a desired effect,
e.g., plaque reduction or prevention, whitening, breath freshening,
caries prevention, pain relief, gum health, tartar control, erosion
control, etc. Use of dentifrices to control erosion of the tooth
surface, or to prevent demineralization, are known and described
in, for example, U.S. Pat. No. 6,685,920. The compositions also may
be applied to other oral cavity surfaces, such as the gingival or
mucosal tissues, although it is believed that the benefits are best
achieved when the dentifrice compositions are applied to the teeth.
The dentifrice composition may contact the tooth and/or oral cavity
surface either directly, or indirectly, however, it is preferred
that the dentifrice composition be directly applied. The dentifrice
composition may be applied by any means, but is preferably applied
with a brush or by rinsing with a dentifrice slurry. The
application may be at least once a day, although up to five times
per day may be preferred, and may be carried out over a duration of
time, e.g., one week, up to one year, up to three years or for a
lifetime
[0070] The manufacture of the oral composition of the present
invention may be accomplished by any of the various standard
techniques for producing such compositions. For example,
preparation methods for dentifrices are well known, for example, as
described in U.S. Pat. No. 3,966,863; U.S. Pat. No. 3,980,767; U.S.
Pat. No. 4,328,205; and U.S. Pat. No. 4,358,437. To make a
dentifrice, a vehicle may be prepared containing humectant, for
example, one or more of glycerin, glycerol, sorbitol, and propylene
glycol, thickener agents and antibacterial agent such as triclosan,
and the vehicle and a mixture of anionic and amphoteric surfactants
are added, followed by blending in of a polishing agent, as well as
fluoride salts, with the pre-mix. Finally, flavoring agent, is
admixed and the pH is adjusted to between 6.8 to 7.0.
[0071] Some embodiments of the present invention provide an oral
care composition (Composition 1) comprising: [0072] (a) an orally
acceptable carrier; [0073] (b) a source of fluoride ions; [0074]
(c) a source of stannous ions; [0075] (d) an insoluble source of
zinc ions; [0076] (e) a buffering system comprising citric acid
wherein the amount of citric acid is at least 1% by weight of the
composition, and wherein the composition has a total water content
of less than 15% by weight, for example: [0077] 1.1. Composition 1
wherein the amount of citric acid is 0.5-4 wt. % or 1-3 wt. %, or
1.1-1.5 wt. % or 1.8-2.2 wt. % or 1.3% or 2% by weight. [0078] 1.2.
Any of the foregoing compositions wherein the insoluble source of
zinc ions comprises a zinc salt of an organic acid; [0079] 1.3. Any
of the foregoing compositions wherein the insoluble source of zinc
ions comprises zinc oxide, zinc phosphate, zinc pyrophosphate or a
mixture thereof; [0080] 1.4. Any of the foregoing compositions
wherein the fluoride ion source is a salt selected from stannous
fluoride, sodium fluoride, potassium fluoride, sodium
monofluorophosphate, sodium fluorosilicate, ammonium
fluorosilicate, amine fluoride (e.g.,
N'-octadecyltrimethylendiamine-N,N,N'-tris(2-ethanol)-dihydrofluoride),
ammonium fluoride, titanium fluoride, hexafluorosulfate, and
combinations thereof; [0081] 1.5. Any of the foregoing compositions
wherein the stannous ion source is selected from stannous fluoride,
stannous chloride dehydrate, stannous acetate, stannous tartrate,
sodium stannous citrate, or a mixture thereof; [0082] 1.6. Any of
the foregoing compositions wherein the source of fluoride ions and
the source of stannous ions comprises stannous fluoride; [0083]
1.7. Any of the foregoing compositions comprising at least one
polyphosphate salt selected from the group consisting of inorganic
polyphosphate salts which have equal to or less than three
phosphorous atoms [0084] 1.8. Composition 1.5 wherein the at least
one polyphosphate is selected from the group consisting of
tetrasodium pyrophosphate, sodium tripolyphosphate, and mixtures
thereof; wherein the total polyphosphate comprises from 1 to 10 wt
% of the composition; [0085] 1.9. Any of the foregoing compositions
wherein the buffering system comprises a mixture of citric acid and
trisodium citrate; [0086] 1.10. Any of the foregoing compositions
comprising a thickening agent which comprises, in combination,
cross-linked polyvinylpyrrolidone and a gum; [0087] 1.11. Any of
the foregoing compositions comprising a thickening agent which
comprises a cellulose, a synthetic block copolymer of ethylene
oxide and propylene oxide, or a mixture thereof; [0088] 1.12. Any
of the foregoing compositions wherein the zinc ion source is
present in an amount of from 0.1 to 2 wt. %, or from 0.5% to 1.5
wt. % or from 0.9% to 1.1 wt. %; 1.13. Any of the foregoing
compositions wherein the stannous ion source is present in an
amount of from 0.05% to 5% wt., or from 0.1% to 1% wt.; or from
0.35-0.55 wt. % [0089] 1.14. Any of the foregoing compositions
wherein the amount fluoride ion source is from 0.1% to 5%, or from
0.2% to 1%, or from 0.3 to 0.6%, by weight of the total
composition; [0090] 1.15. Any of the foregoing compositions wherein
the composition has a total water content of less than 20%, or less
than 15%, or from less than 15% to greater than 10 wt. %, based on
the weight of the composition; [0091] 1.16. Any of the foregoing
compositions wherein combined metal ion source is present in an
amount of from 0.15% to 7%, by weight, or from 0.6 to 2.5%, or from
1.25% to 1.65%, by weight of the composition; [0092] 1.17. Any of
the foregoing compositions comprising a methyl vinyl ether/maleic
anhydride copolymer having an average molecular weight (M.W.) of
30,000 to 1,000,000, e.g. 300,000 to 800,000; [0093] 1.18. Any of
the foregoing compositions comprising L-arginine in free or orally
acceptable salt form; [0094] 1.19. Any of the foregoing
compositions comprising additional buffering agents, e.g., sodium
phosphate buffer (e.g., sodium phosphate monobasic and disodium
phosphate); [0095] 1.20. Any of the foregoing compositions
comprising a humectant, e.g., selected from, sorbitol, propylene
glycol, polyethylene glycol, xylitol, and mixtures thereof; [0096]
1.21. Any of the foregoing compositions further comprising an
abrasive or particulate; [0097] 1.22. The foregoing composition
wherein the abrasive or particulate is selected from sodium
bicarbonate, calcium phosphate (e.g., dicalcium phosphate
dihydrate), calcium sulfate, precipitated calcium carbonate, silica
(e.g., hydrated silica), iron oxide, aluminum oxide, perlite,
plastic particles, e.g., polyethylene, and combinations thereof;
[0098] 1.23. Any of the foregoing compositions comprising an
abrasive in an amount of 15 wt. % to 70 wt. % of the total
composition weight; [0099] 1.24. Any of the foregoing compositions
comprising one or more surfactants, e.g., selected from anionic,
cationic, zwitterionic, and nonionic surfactants, and mixtures
thereof, e.g., comprising an anionic surfactant, e.g., a surfactant
selected from sodium lauryl sulfate, sodium ether lauryl sulfate,
and mixtures thereof, e.g. in an amount of from 0.3% to 4.5% by
weight; [0100] 1.25. Any of the foregoing compositions further
comprising one or more polymers selected from polyethylene glycols,
polysaccharides (e.g., cellulose derivatives, for example
carboxymethyl cellulose, polysaccharide gums, for example xanthan
gum or carrageenan gum), and combinations thereof; [0101] 1.26. Any
of the foregoing compositions comprising one or more antibacterial
agents, for example comprising an antibacterial agent selected from
halogenated diphenyl ether (e.g. triclosan), herbal extracts and
essential oils (e.g., rosemary extract, tea extract, magnolia
extract, thymol, menthol, eucalyptol, geraniol, carvacrol, citral,
hinokitol, catechol, methyl salicylate, epigallocatechin gallate,
epigallocatechin, gallic acid, miswak extract, sea-buckthorn
extract), bisguanide antiseptics (e.g., chlorhexidine, alexidine or
octenidine), quaternary ammonium compounds (e.g., cetylpyridinium
chloride (CPC), benzalkonium chloride, tetradecylpyridinium
chloride (TPC), N-tetradecyl-4-ethylpyridinium chloride (TDEPC)),
phenolic antiseptics, hexetidine, octenidine, sanguinarine,
povidone iodine, delmopinol, salifluor, metal ions (e.g., zinc
salts, for example, zinc citrate, stannous salts, copper salts,
iron salts), sanguinarine, propolis and oxygenating agents (e.g.,
hydrogen peroxide, buffered sodium peroxyborate or
peroxycarbonate), phthalic acid and its salts, monoperthalic acid
and its salts and esters, ascorbyl stearate, oleoyl sarcosine,
alkyl sulfate, dioctyl sulfosuccinate, salicylanilide, domiphen
bromide, delmopinol, octapinol and other piperidino derivatives,
nicin preparations, chlorite salts; and mixtures of any of the
foregoing; e.g., comprising triclosan or cetylpyridinium chloride;
[0102] 1.27. Any of the foregoing compositions comprising a
whitening agent, e.g., a selected from the group consisting of
peroxides, metal chlorites, perborates, percarbonates, peroxyacids,
hypochlorites, and combinations thereof; [0103] 1.28. Any of the
foregoing compositions further comprising hydrogen peroxide or a
hydrogen peroxide source, e.g., urea peroxide or a peroxide salt or
complex (e.g., such as peroxyphosphate, peroxycarbonate, perborate,
peroxysilicate, or persulphate salts; for example calcium
peroxyphosphate, sodium perborate, sodium carbonate peroxide,
sodium peroxyphosphate, and potassium persulfate); [0104] 1.29. Any
of the foregoing compositions further comprising a source of
calcium and phosphate selected from (i) calcium-glass complexes,
e.g., calcium sodium phosphosilicates, and (ii) calcium-protein
complexes, e.g., casein phosphopeptide-amorphous calcium phosphate;
[0105] 1.30. Any of the foregoing compositions further comprising a
soluble calcium salt, e.g., selected from calcium sulfate, calcium
chloride, calcium nitrate, calcium acetate, calcium lactate, and
combinations thereof; [0106] 1.31. Any of the foregoing
compositions further comprising a physiologically or orally
acceptable potassium salt, e.g., potassium nitrate or potassium
chloride, in an amount effective to reduce dentinal sensitivity;
[0107] 1.32. Any of the foregoing compositions in the form of a
dentifrice, for example a toothpaste, e.g., a clear gel or opaque
toothpaste; [0108] 1.33. Any of the foregoing compositions in the
form of a single phase; [0109] 1.34. Any of the foregoing
compositions comprising one or more of the following in the recited
amounts:
TABLE-US-00001 [0109] Citric acid 0.5-3 or 1.1-1.5 or 1.8-2.2 wt. %
Trisodium citrate 0.5-10 or 1-6 or 2-4 or 2.9-3.1 wt % Zinc oxide
0.1-5 or 0.5-2 or 0.9-1.1 wt % Stannous fluoride 0.1-5, or 0.1-2,
or 0.4-0.6% wt % Glycerin 10-50 wt % Propylene glycol 1-25, or
2-10, or 6-8 wt % Xantham gum 0.1-12 or 0.1-1, or 0.1-.0.5 or
0.275-0.325 wt % polyvinylpyrrolidone 0.25-10 wt % CMC 0.2-1.5 or
0.3-0.9 or 0.65-0.75% Silica (total) 5-60 or 10-50, or 10-40 or
22-26 wt % Tetrasodium 0.1-10 or 0.5-5 or 1-4 or 1.75-2.25 wt %
Pyrophosphate (TSPP) Sodium acid 0-5 or 0-3 or 0.5-1.5 or 0.9-1.1
wt % pyrophosphate (SAPP) Sodium 0.1-10, or 0.5-5 or 1-4, or
2.75-3.25 wt % Tripolyphosphate (STPP) Sodium lauryl 0.1-10, or
0.2-5, or 1.2-2.5 or 1.5-1.75 wt % sulfate (SLS) Cocamidopropyl
0.1-10, or 0.5-5 or 0.5-2 or 0.75 to 1.25 wt % betaine
[0110] 1.35. Any of the foregoing compositions which does not
contain methylvinyl ether-maleic anhydride copolymer; [0111] 1.36.
A method of treating or preventing a disease or condition of the
oral cavity comprising contacting an oral cavity surface of a
patient in need thereof with the composition of any one of the
foregoing compositions; [0112] 1.37. Any of the foregoing methods
which is a method for the treatment and prevention of bacterial
plaque accumulation or prevention of tooth erosion.
[0113] The following examples are further illustrative of the
preferred embodiments, but it is understood that the invention is
not limited thereto.
EXAMPLES
Example 1
Procedure
[0114] Four formulations are prepared with the ingredients
indicated for Formula A, with the amounts of CMC and citric acid,
TKPP, SAPP and STPP varied as indicated in Tables 1 and 2.
[0115] The technique to determine water soluble tin and water
soluble zinc in the formulations is by flame atomic absorption
spectroscopy (FAAS). A suitable double beam atomic absorption
spectrophotometer fitted with an air-acetylene burner and deuterium
background correction, e.g. Varian SpectrAA 220FS, can be used.
Also, a suitable zinc hollow cathode lamp and AA grade acetylene
can be used. Water soluble zinc or tin can be measured in the
compositions by FAAS after dilution of a sample in water and
comparing to zinc or tin standards. A portion of the formulation is
dispersed with water, solutions are transferred to a volumetric
flask, diluted to volume with water and centrifuged. Tin or zinc is
detected in the supernatant by atomic absorption spectroscopy and
quantitated by comparing the absorbance of the sample solution to
absorbances of external calibration standards of known tin or zinc
concentration. To determine total tin or zinc, rather than
dispersing the samples in water, the samples are digested with a
suitable acid mixture, e.g., hydrochloric, nitric, and or
hydrofluoric, over a steam bath.
[0116] The formulas are aged at 40.degree. C. for up to 13 weeks.
The total tin, total zinc, soluble tin and soluble zinc levels are
determined at various time points.
TABLE-US-00002 TABLE 1 Product Test Initial 4 wk 8 wk 13 wk 0% CMC
+ 1.3% Soluble Tin 0.25 0.12 0.09 0.17 Citric Acid Soluble Zinc
0.69 0.68 0.57 0.55 Total Tin 0.35 -- -- -- Total Zinc 0.96 -- --
-- pH (as is) 5.73 6.53 6.56 6.61 10% pH 7.96 8.05 7.88 7.89 0.4%
CMC + 1.3% Soluble Tin 0.25 0.12 0.1 0.11 Citric Acid Soluble Zinc
0.68 0.66 0.59 0.625 Total Tin 0.35 -- -- -- Total Zinc 0.92 -- --
-- pH (as is) 6.1 6.89 6.78 6.93 10% pH 8.02 7.77 7.77 7.65 0% CMC
+ 2% Soluble Tin 0.33 0.28 0.29 0.34 Citric Acid Soluble Zinc 0.64
0.7 0.62 0.6 Total Tin 0.34 -- -- -- Total Zinc 0.72 -- -- -- pH
(as is) 5.32 5.9 5.96 5.98 10% pH 6.77 6.83 6.81 6.84 0.4% CMC + 2%
Soluble Tin 0.35 0.33 0.35 0.32 Citric Acid Soluble Zinc 0.62 0.63
0.54 0.63 Total Tin 0.37 -- -- -- Total Zinc 0.76 -- -- -- pH (as
is) 5.9 6.07 6.11 6.13 10% pH 6.67 6.75 6.74 6.67
TABLE-US-00003 TABLE 2 Percent Zinc Soluble Initial 4 wk 8 wk 13 wk
Sn + ZnO + 1.3% Citric 71.88% 70.83% 59.38% 57.29% Acid + 0% CMC Sn
+ ZnO + 1.3% Citric 73.91% 71.74% 64.13% 67.93% Acid + 0.4% CMC Sn
+ ZnO + 2.0% Citric 88.89% 97.22% 86.11% 83.33% Acid + 0% CMC Sn +
ZnO + 2.0% Citric 81.58% 82.89% 71.05% 82.89% Acid + 0.4% CMC
[0117] Solubility of Stannous Fluoride: 31 g/100mL (0.degree. C.),
35 g/100 mL (20.degree. C.)
TABLE-US-00004 [0117] Formula A Ingredient Weight % Demineralized
Water 10 Sodium Saccharin 0.6 Trisodium Citrate Dihydrate 3 Citric
Acid-Anydrous 1.3-2 Stannous Fluoride 0.45 Zinc Oxide 1 Tetrasodium
Pyrophosphate 0-2 Sodium Tripolyphosphate 0-3 99.0%-101.0% Glycerin
balance Polyethylene Glycol 600 3 Propylene Glycol 4 PVP 1 Dye
<0.01 Titanium Dioxide Coated Mica 0.15 Xanthan Gum 0.3
Carboxymethyl Cellulose (CMC 7) 0-0.4 Syn. Amorph. PPT.
Silica-Abrasive 12 High Cleaning Silica 12 Sodium Lauryl Sulfate
Powder 1.75 Cocamidopropyl Betaine 1 Flavor 1.4 Total 100
Results
Comparative Example
[0118] Earlier work with a formula comprising a soluble zinc source
(2 wt. % zinc citrate) and 0.454 wt. % stannous fluoride with 0.6
wt. % citric acid/3.0 wt. % trisodium citrate. This formula had an
initial amount of soluble zinc of only 0.39 wt. % which decreased
slightly to 0.34 wt. % after 12 weeks of aging. The amount of
stannous remained steady from its initial solubility to the end of
the 12 week aging period (ranging from 0.31 wt. %-0.36 wt. %).
[0119] Surprisingly, formulas with or without CMC with the same
amount (0.454 wt. %) stannous fluoride and a lesser amount (1 wt.
%) of less soluble zinc source (ZnO) showed greater initial
solubility when greater than 1 wt. % citric acid was used (ranging
from 0.62 wt. % to 0.69 wt. %) and this higher level of solubility
was maintained despite 13 weeks of aging (0.55 wt. % to 0.63 wt.
%).
[0120] Furthermore, when the amount of citric acid was increased to
2%, the initial amount of soluble stannous and amount after 13
weeks of aging (0.32 wt. % to 0.35 wt. %) was comparable to the
ranges measured in the Comparative Example.
[0121] As those skilled in the art will appreciate, numerous
changes and modifications may be made to the embodiments described
herein without departing from the spirit of the invention. It is
intended that all such variations fall within the scope of the
appended claims.
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