U.S. patent application number 15/548468 was filed with the patent office on 2018-01-18 for oral care compositions and methods of use.
This patent application is currently assigned to Colgate-Palmolive Company. The applicant listed for this patent is Colgate-Palmolive Company. Invention is credited to Xiaoyi HUANG, Andre MORGAN, Vyoma PATEL, Michael PRENCIPE, Amy RUSSO, Hansruedi STETTLER, Betty WON, Peng YAN.
Application Number | 20180015016 15/548468 |
Document ID | / |
Family ID | 56297163 |
Filed Date | 2018-01-18 |
United States Patent
Application |
20180015016 |
Kind Code |
A1 |
HUANG; Xiaoyi ; et
al. |
January 18, 2018 |
Oral Care Compositions and Methods of Use
Abstract
An oral care composition comprises arginine or lysine, zinc
citrate and zinc oxide, a fluoride source, and glycerin, as well as
to methods of using and of making the composition.
Inventors: |
HUANG; Xiaoyi; (Guangzhou,
CN) ; PRENCIPE; Michael; (West Windsor, NJ) ;
RUSSO; Amy; (Belle Mead, NJ) ; STETTLER;
Hansruedi; (Basel, CH) ; PATEL; Vyoma;
(Hillsborough, NJ) ; WON; Betty; (Princeton
Junction, NJ) ; YAN; Peng; (Guangzhou,Guangdong,
CN) ; MORGAN; Andre; (Robbinsville, NJ) |
|
Applicant: |
Name |
City |
State |
Country |
Type |
Colgate-Palmolive Company |
New York |
NY |
US |
|
|
Assignee: |
Colgate-Palmolive Company
New York
NY
|
Family ID: |
56297163 |
Appl. No.: |
15/548468 |
Filed: |
June 24, 2016 |
PCT Filed: |
June 24, 2016 |
PCT NO: |
PCT/CN2016/086995 |
371 Date: |
August 3, 2017 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
|
|
62187801 |
Jul 1, 2015 |
|
|
|
Current U.S.
Class: |
1/1 |
Current CPC
Class: |
A61K 8/362 20130101;
A61P 31/04 20180101; A61K 8/44 20130101; A61K 2800/92 20130101;
A61P 31/02 20180101; A61K 8/345 20130101; A61K 8/21 20130101; A61K
8/27 20130101; A61P 1/02 20180101; A61K 8/365 20130101; A61K
2800/28 20130101; A61Q 11/00 20130101; A61K 8/25 20130101 |
International
Class: |
A61K 8/44 20060101
A61K008/44; A61K 8/34 20060101 A61K008/34; A61K 8/21 20060101
A61K008/21; A61K 8/27 20060101 A61K008/27; A61Q 11/00 20060101
A61Q011/00; A61K 8/362 20060101 A61K008/362 |
Claims
1. An oral care composition comprising: a. a basic amino acid in
free or salt wherein the amino acid is selected from arginine,
lysine, and combinations thereof; b. zinc oxide and zinc citrate c.
a fluoride source d. glycerin
2. The oral care composition of claim 1, wherein the basic amino
acid is arginine and wherein the arginine has the
L-configuration.
3. The oral care composition of claim 1, wherein the amino acid is
arginine and wherein the arginine is present in an amount
corresponding to 1% to 15%, the weight of the basic amino acid
being calculated as free form.
4. The oral care composition of claim 1 wherein the amino acid is
arginine from about 1.5 wt. %.
5. The oral care composition of claim 1 wherein the amino acid is
arginine in free form.
6. The oral care composition of claim 1 wherein the amino acid is
arginine or lysine in partially or wholly salt form.
7. The oral care composition of claim 1, wherein the ratio of the
amount of zinc oxide (by wt %) to zinc citrate (by wt %) is 2:1,
2.5:1, 3:1, 3.5:1 or 4:1, wherein the ratio is by wt. of the
overall composition.
8. The oral care composition of claim 7, wherein the ratio of the
amount of zinc oxide (by wt %) to zinc citrate (by wt %) is
2:1.
9. The oral care composition of claim 1, wherein the zinc citrate
is in an amount of from 0.25 to 1.0 wt % and zinc oxide may be
present in an amount of from 0.75 to 1.25 wt % based on the weight
of the oral care composition.
10. The oral care composition of claim 1, wherein the zinc citrate
is in an amount of about 0.5 wt % and zinc is present in an amount
of about 1.0% based on the weight of the oral care composition.
11. The oral care composition of claim 1, wherein the fluoride
source is sodium fluoride.
12. The oral care composition of claim 1, wherein the glycerin is
in an amount from 25%-40% based on the weight of the oral care
composition.
13. The oral care composition of claim 12, wherein the glycerin is
in an amount of about 35% by wt.
14. The oral care composition of claim 12, wherein the glycerin is
in an amount of about 26% by wt.
15. The oral care composition of claim 1, wherein the composition
further comprises sorbitol.
16. The composition of claim 15, wherein the sorbitol is in an
amount of about 13% by wt. and the glycerin is in an amount of
about 26% by wt.
17. The oral care composition of claim 1 comprising: a. about 1.0%
zinc oxide b. about 0.5% zinc citrate c. about 1.5% L-arginine d.
about 0.32% sodium fluoride; and e. about 35% glycerin.
18. The oral care composition of claim 1 comprising: a. about 1.0%
zinc oxide b. about 0.5% zinc citrate c. about 5% L-arginine d.
about 0.32% sodium fluoride; e. about 26% glycerin; and f. about
13% sorbitol.
19. The oral care composition of claim 1, wherein the oral
composition may be any of the following oral compositions selected
from the group consisting of: a toothpaste or a dentifrice, a
mouthwash or a mouth rinse, a topical oral gel, and a denture
cleanser.
20. The oral care composition of claim 1, wherein the composition
is obtained or obtainable by combining the ingredients as set forth
in any of the preceding compositions.
21. A method to improve oral health comprising applying an
effective amount of the oral composition of claim 1 set forth above
to the oral cavity of a subject in need thereof, wherein the method
is effective to: i. reduce or inhibit formation of dental caries,
ii. reduce, repair or inhibit early enamel lesions, e.g., as
detected by quantitative light-induced fluorescence (QLF) or
electrical caries measurement (ECM), iii. reduce or inhibit
demineralization and promote remineralization of the teeth, iv.
reduce hypersensitivity of the teeth, v. reduce or inhibit
gingivitis, vi. promote healing of sores or cuts in the mouth, vii.
reduce levels of acid producing bacteria, viii. to increase
relative levels of arginolytic bacteria, inhibit microbial bio film
formation in the oral cavity, x. raise and/or maintain plaque pH at
levels of at least pH 5.5 following sugar challenge, xi. reduce
plaque accumulation, xii. treat dry mouth, xiii. enhance systemic
health, including cardiovascular health, xiv. Whiten teeth, xv.
reduce erosion of the teeth, xvi. immunize (or protect) the teeth
against cariogenic bacteria and their effects, and/or xvii. clean
the teeth and oral cavity.
Description
CROSS REFERENCE TO RELATED APPLICATIONS
[0001] This application claims the benefit of U.S. Provisional
Application 62/187,801, filed on Jul. 1, 2015, the contents of
which are incorporated herein by reference in their entirety.
FIELD
[0002] This invention relates to oral care compositions comprising
arginine or lysine or salt thereof, zinc oxide and zinc citrate,
and a fluoride source, as well as to methods of using and of making
these compositions.
BACKGROUND
[0003] Oral care compositions present particular challenges in
preventing microbial contamination. Arginine and other basic amino
acids have been proposed for use in oral care and are believed to
have significant benefits in combating cavity formation and tooth
sensitivity.
[0004] Commercially available arginine-based toothpaste contains
arginine bicarbonate and precipitated calcium carbonate. The
carbonate ion is believed to have cariostatic properties, and the
calcium is believed to form in complex with arginine to provide a
protective effect.
[0005] The formulation of certain oral care compositions presents
special challenges. For example, not all preservatives are active
at higher pH. Some preservatives negatively affect the taste or
aesthetics of the product. While certain preservatives, such as
ethanol or parabens, are known to be effective at a range of pHs,
these preservatives are not suitable for all products or all
markets.
[0006] Zinc formulations also present challenges. Zinc is a known
antimicrobial agent used in toothpaste compositions. Zinc is also a
known essential mineral for human health, and has been reported to
help strengthen dental enamel and to promote cell repair.
Unfortunately, conventional toothpaste formulations often require a
high concentrations of zinc, e.g., 2% by weight or more, to achieve
efficacy. At this concentration, the zinc imparts a notably
astringent taste to the composition.
[0007] Foaming perception is also an important aspect of a user's
experience and can be critical to the aesthetic and qualitative
qualities of the oral care composition.
[0008] Accordingly, there is a need for improved foaming agents for
use in oral compositions comprising basic amino acids and zinc
salts.
BRIEF SUMMARY
[0009] It has been surprisingly found that particular
concentrations and ratios of glycerin--used as a humectant--can
play a positive role in foam perception in oral care compositions
with a zinc citrate, zinc oxide, and amino acid base. Without being
bound by theory, glycerin can form weak hydrogen-bonds with water
on the surface of the surfactant micelle, reducing water
evaporation and minimizing bubble coalescence. In some aspects, the
glycerin can be used as the sole humectant or in a particular ratio
with sorbitol. This unique humectant blend (whether it is glycerin
alone in a particular amount, a ratio of glycerin and sorbitol) has
an unexpected positive impact on foam generation and foam density
perception in oral care compositions.
[0010] In one aspect the invention is an oral care composition
(Composition 1.0) comprising: [0011] a. Basic amino acid in free or
salt wherein the amino acid is selected from arginine, lysine, and
combinations thereof (e.g., free form arginine) [0012] b. zinc
oxide and zinc citrate [0013] c. a fluoride source (e.g., sodium
fluoride); and [0014] d. glycerin (e.g., from 26-35 wt %)
[0015] For example, the invention contemplates any of the following
compositions (unless otherwise indicated, values are given as
percentage of the overall weight of the composition) [0016] 1.1
Composition 1.0 wherein the basic amino acid has the
L-configuration (e.g., L-arginine). [0017] 1.2 Any of the preceding
compositions wherein the basic amino acid is arginine in free form.
[0018] 1.3 Any of the preceding compositions wherein the basic
amino acid is provided in the form of a di- or tri-peptide
comprising arginine, or salts thereof. [0019] 1.4 Any of the
preceding compositions wherein the basic amino acid is arginine,
and wherein the arginine is present in an amount corresponding to
1% to 15%, e.g., 3 wt. % to 10 wt. % of the total composition
weight, about e.g., 1.5%, 4%, 5%, or 8%, wherein the weight of the
basic amino acid is calculated as free form. [0020] 1.5 Any of the
preceding compositions wherein the amino acid is arginine from 0.1
wt. %-6.0 wt. % (e.g., about 1.5 wt %). [0021] 1.6 Any of the
preceding compositions wherein the amino acid is arginine from
about 1.5 wt. %. [0022] 1.7 Any of the preceding compositions
wherein the amino acid is arginine from 4.5 wt. %-8.5 wt. % (e.g.,
5.0%). [0023] 1.8 Any of the preceding compositions wherein the
amino acid is arginine from about 5.0 wt. %. [0024] 1.9 Any of the
preceding compositions wherein the amino acid is arginine from 3.5
wt. %-9 wt. %. [0025] 1.10 Any of the preceding compositions
wherein the amino acid is arginine from about 8.0 wt. %. [0026]
1.11 Any of the preceding compositions wherein the amino acid is
L-arginine. [0027] 1.12 Any of the preceding compositions wherein
the amino acid is free form arginine. [0028] 1.13 Any of the
preceding compositions wherein the amino acid is arginine. [0029]
1.14 Composition 1.19 wherein the amino acid is arginine phosphate.
[0030] 1.15 Composition 1.19 wherein the amino acid is arginine
hydrochloride. [0031] 1.16 Composition 1.19 wherein the amino acid
is arginine bicarbonate. [0032] 1.17 Any of the preceding
compositions wherein the amino acid is arginine ionized by
neutralization with an acid or a salt of an acid. [0033] 1.18 Any
of preceding compositions wherein the composition is ethanol-free.
[0034] 1.19 Any of the preceding compositions further comprising a
fluoride source 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. [0035] 1.20 Any of the preceding compositions
wherein the fluoride source is sodium fluoride. [0036] 1.21 Any of
the preceding compositions wherein the fluoride source is a
fluoride salt present in an amount of 0.1 wt. % to 2 wt. % (0.1 wt
%-0.6 wt. %) of the total composition weight (e.g., sodium fluoride
(e.g., about 0.32 wt. %0). [0037] 1.22 Any of the preceding
compositions wherein the fluoride source is a soluble fluoride salt
which provides fluoride ion in an amount of from 50 to 25,000 ppm
(e.g., 750-2000 ppm, e.g., 1000-1500 ppm, e.g., about 1000 ppm,
e.g., about 1450 ppm). [0038] 1.23 Any of the preceding
compositions wherein the fluoride source is sodium fluoride which
provides fluoride in an amount from 750-2000 ppm (e.g., about 1450
ppm). [0039] 1.24 Any of the preceding compositions wherein the
fluoride source is sodium fluoride and which provides fluoride in
an amount from 1000 ppm-1500 ppm. [0040] 1.25 Any of the preceding
compositions wherein the fluoride source is sodium fluoride and
which provides fluoride in an amount of about 1450 ppm. [0041] 1.26
Any of the preceding compositions wherein the pH is between 7.5 and
10.5, e.g., 8-9.5, e.g., 7.2-9.0, about 8.0, about 9.0. [0042] 1.27
Any of the preceding compositions further comprising calcium
carbonate. [0043] 1.28 The composition of 1.38, wherein the calcium
carbonate is a precipitated calcium carbonate high absorption
(e.g., 20% to 30% by weight of the composition) (e.g., 25%
precipitated calcium carbonate high absorption). [0044] 1.29 The
composition of 1.35, further comprising a precipitated calcium
carbonate light (e.g., about 10% precipitated calcium
carbonate-light) (e.g., about 10% natural calcium carbonate).
[0045] 1.30 Any of the preceding compositions further comprising an
effective amount of one or more alkali phosphate salts, e.g.,
sodium, potassium or calcium salts, e.g., selected from alkali
dibasic phosphate and alkali pyrophosphate salts, e.g., alkali
phosphate salts selected from sodium phosphate dibasic, potassium
phosphate dibasic, dicalcium phosphate dihydrate, calcium
pyrophosphate, tetrasodium pyrophosphate, tetrapotassium
pyrophosphate, sodium tripolyphosphate, disodium
hydrogenorthophoshpate, monosodium phosphate, pentapotassium
triphosphate and mixtures of any of two or more of these, e.g., in
an amount of 0.1-20%, e.g., 0.1-8%, e.g., e.g., 0.2 to 5%, e.g.,
0.3 to 2%, e.g., 0.3 to 1%, e.g about 0.5%, about 1%, about 2%,
about 5%, about 6%, by weight of the composition. [0046] 1.31 Any
of the preceding compositions comprising tetrapotassium
pyrophosphate, disodium hydrogenorthophoshpate, monosodium
phosphate, and pentapotassium triphosphate. [0047] 1.32 Any of the
preceding compositions comprising a polyphosphate. [0048] 1.33 The
composition of 1.43, wherein the polyphosphate is tetrasodium
pyrophosphate. [0049] 1.34 The composition of 1.44, wherein the
tetrasodium pyrophosphate is from 0.1-1.0 wt % (e.g., about 0.5 wt
%). [0050] 1.35 Any of the preceding compositions further
comprising an abrasive or particulate (e.g., silica). [0051] 1.36
Any of the preceding compositions wherein the silica is synthetic
amorphous silica. (e.g., 1%-28% by wt.) (e.g., 8%-25% by wt.).
[0052] 1.37 Any of the preceding composition wherein the silica
abrasives are silica gels or precipitated amorphous silicas, e.g.
silicas having an average particle size ranging from 2.5 microns to
12 microns. [0053] 1.38 Any of the preceding compositions further
comprising a small particle silica having a median particle size
(d50) of 1-5 microns (e.g., 3-4 microns) (e.g., about 5 wt. %
Sorbosil AC43 from PQ Corporation, Warrington, United Kingdom).
[0054] 1.39 Any of the preceding compositions wherein 20-30 wt % of
the total silica in the composition is small particle silica (e.g.,
having a median particle size (d50) of 3-4 microns) and wherein the
small particle silica is about 5 wt. % of the oral care
composition. [0055] 1.40 Any of the preceding compositions
comprising silica wherein the silica is used as a thickening agent,
e.g., particle silica. [0056] 1.41 Any of the preceding
compositions further comprising a nonionic surfactant, wherein the
nonionic surfactant is in an amount of from 0.5-5%, e.g, 1-2%,
selected from poloxamers (e.g., poloxamer 407), polysorbates (e.g.,
polysorbate 20), polyoxyl hydrogenated castor oil (e.g., polyoxyl
40 hydrogenated castor oil), and mixtures thereof. [0057] 1.42 Any
of the preceding compositions, wherein the poloxamer nonionic
surfactant has a polyoxypropylene molecular mass of from 3000 to
5000 g/mol and a polyoxyethylene content of from 60 to 80 mol %,
e.g., the poloxamer nonionic surfactant comprises poloxamer 407.
[0058] 1.43 Any of the preceding compositions, wherein the ratio of
the amount of zinc oxide (e.g., wt. %) to zinc citrate (e.g., wt %)
is from 1.5:1 to 4.5:1 (e.g., 2:1, 2.5:1, 3:1, 3.5:1, or 4:1).
[0059] 1.44 Any of the preceding compositions, wherein the zinc
citrate is in an amount of from 0.25 to 1.0 wt % (e.g., 0.5 wt. %)
and zinc oxide may be present in an amount of from 0.75 to 1.25 wt
% (e.g., 1.0 wt. %) based on the weight of the oral care
composition. [0060] 1.45 Any of the preceding compositions wherein
the zinc citrate is about 0.5 wt %. [0061] 1.46 Any of the
preceding compositions wherein the zinc oxide is about 1.0 wt %.
[0062] 1.47 Any of the preceding compositions where the zinc
citrate is about 0.5 wt % and the zinc oxide is about 1.0 wt %.
[0063] 1.48 Any of the preceding compositions further comprising an
additional ingredient selected from: benzyl alcohol,
Methylisothizolinone ("MIT"), Sodium bicarbonate, sodium methyl
cocoyl taurate (tauranol), lauryl alcohol, and polyphosphate.
[0064] 1.49 Any of the preceding compositions wherein the benzyl
alcohol is present from 0.1-0.6 wt %., (e.g., 0.1-0.4 wt %) e.g.
about 0.1 wt. %, about 0.2 wt. %, or about 0.3 wt. %. [0065] 1.50
Any of the preceding compositions wherein the benzyl alcohol is
about 0.1 wt %. [0066] 1.51 Any of the preceding composition
wherein benzyl alcohol is present at is considered a preservative.
[0067] 1.52 Any of the preceding compositions comprising polymer
films. [0068] 1.53 Any of the preceding compositions comprising
flavoring, fragrance and/or coloring. [0069] 1.54 The composition
of 1.42, wherein the flavoring agent is sodium saccharin,
sucralose, or a mixture thereof. [0070] 1.55 Any of the preceding
compositions, wherein the composition comprises a thickening agents
selected from the group consisting of carboxyvinyl polymers,
carrageenan, xanthan, hydroxyethyl cellulose and water soluble
salts of cellulose ethers (e.g., sodium carboxymethyl cellulose and
sodium carboxymethyl hydroxyethyl cellulose). [0071] 1.56 Any of
the preceding compositions, wherein the compositions comprises
sodium carboxymethyl cellulose (e.g., from 0.5 wt. %-1.5 wt. %)
[0072] 1.57 Any of the preceding compositions comprising from
5%-40%, e.g., 10%-35%, e.g., about 15%, 25%, 30%, and 35% water.
[0073] 1.58 Any of the preceding compositions comprising an
additional 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 Chloride, Zinc Lactate, Zinc Sulfate, 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. [0074] 1.59 Any of the preceding compositions comprising
an antioxidant, e.g., selected from the group consisting of
Co-enzyme Q10, PQQ, Vitamin C, Vitamin E, Vitamin A, BHT,
anethole-dithiothione, and mixtures thereof. [0075] 1.60 Any of the
preceding compositions comprising a whitening agent. [0076] 1.61
Any of the preceding compositions comprising a whitening agent
selected from a whitening active selected from the group consisting
of peroxides, metal chlorites, perborates, percarbonates,
peroxyacids, hypochlorites, and combinations thereof. [0077] 1.62
Any of the preceding 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), or hydrogen peroxide polymer complexes such as
hydrogen peroxide-polyvinyl pyrrolidone polymer complexes. [0078]
1.63 Any of the preceding compositions, wherein the glycerin is in
an amount from 20%-40% by wt. of the composition. [0079] 1.64 The
composition of 1.62, wherein the glycerin is in an amount from
25%-40% by wt. of the composition. [0080] 1.65 The composition of
1.63, wherein the glycerin is about 26% by wt. of the composition.
[0081] 1.66 The composition of 1.63, wherein the glycerin is about
35% by wt. of the composition. [0082] 1.67 Any of the preceding
compositions, wherein the composition further comprises sorbitol.
[0083] 1.68 The composition of 1.66, wherein the sorbitol is from
10%-20% by wt. of the composition. [0084] 1.69 The composition of
1.67, wherein the sorbitol is about 13% by wt. of the composition.
[0085] 1.70 The composition of 1.68, wherein the composition
comprises about 13% by wt. sorbitol and about 26% by wt. glycerin.
[0086] 1.71 Any of the preceding compositions further comprising an
agent that interferes with or prevents bacterial attachment, e.g.,
ethyl lauroyl arginiate (ELA) or chitosan. [0087] 1.72 Any of the
preceding compositions comprising: [0088] a. about 1.0% zinc oxide
[0089] b. about 0.5% zinc citrate [0090] c. about 1.5% L-arginine
[0091] d. about 0.32% sodium fluoride; and [0092] e. about 35%
glycerin. [0093] 1.73 Any of compositions 1.0-1.81 comprising:
[0094] a. about 1.0% zinc oxide [0095] b. about 0.5% zinc citrate
[0096] c. about 5% L-arginine [0097] d. about 0.32% sodium
fluoride; [0098] e. about 26% glycerin; and [0099] f. about 13%
sorbitol. [0100] 1.74 Any of the preceding compositions effective
upon application to the oral cavity, e.g., by rinsing, optionally
in conjunction with brushing, to (i) reduce or inhibit formation of
dental caries, (ii) reduce, repair or inhibit pre-carious lesions
of the enamel, e.g., as detected by quantitative light-induced
fluorescence (QLF) or electrical caries measurement (ECM), (iii)
reduce or inhibit demineralization and promote remineralization of
the teeth, (iv) reduce hypersensitivity of the teeth, (v) reduce or
inhibit gingivitis, (vi) promote healing of sores or cuts in the
mouth, (vii) reduce levels of acid producing bacteria, (viii) to
increase relative levels of arginolytic bacteria, (ix) inhibit
microbial biofilm formation in the oral cavity, (x) raise and/or
maintain plaque pH at levels of at least pH 5.5 following sugar
challenge, (xi) reduce plaque accumulation, (xii) treat, relieve or
reduce dry mouth, (xiii) clean the teeth and oral cavity (xiv)
reduce erosion, (xv) prevents stains and/or whiten teeth, (xvi)
immunize the teeth against cariogenic bacteria; and/or (xvii)
promote systemic health, including cardiovascular health, e.g., by
reducing potential for systemic infection via the oral tissues.
[0101] 1.75 Any of the preceding oral compositions, wherein the
oral composition may be any of the following oral compositions
selected from the group consisting of: a toothpaste or a
dentifrice, a mouthwash or a mouth rinse, a topical oral gel, and a
denture cleanser.
[0102] 1.76 A composition obtained or obtainable by combining the
ingredients as set forth in any of the preceding compositions.
[0103] A composition obtained or obtainable by combining the
ingredients as set forth in any of the preceding compositions.
[0104] A composition for use as set for in any of the preceding
compositions.
[0105] In another embodiment, the invention encompasses a method to
improve oral health comprising applying an effective amount of the
oral composition of any of the embodiments set forth above to the
oral cavity of a subject in need thereof, e.g., a method to [0106]
i. reduce or inhibit formation of dental caries, [0107] ii. reduce,
repair or inhibit early enamel lesions, e.g., as detected by
quantitative light-induced fluorescence (QLF) or electrical caries
measurement(ECM), [0108] iii. reduce or inhibit demineralization
and promote remineralization of the teeth, [0109] iv. reduce
hypersensitivity of the teeth, [0110] v. reduce or inhibit
gingivitis, [0111] vi. promote healing of sores or cuts in the
mouth, [0112] vii. reduce levels of acid producing bacteria, [0113]
viii. to increase relative levels of arginolytic bacteria, [0114]
ix. inhibit microbial bio film formation in the oral cavity, [0115]
x. raise and/or maintain plaque pH at levels of at least pH 5.5
following sugar challenge, [0116] xi. reduce plaque accumulation,
[0117] xii. treat dry mouth, [0118] xiii. enhance systemic health,
including cardiovascular health,e.g., by reducing potential for
systemic infection via the oral tissues, [0119] xiv. Whiten teeth,
[0120] xv. reduce erosion of the teeth, [0121] xvi. immunize (or
protect) the teeth against cariogenic bacteria and their effects,
and/or [0122] xvii. clean the teeth and oral cavity.
[0123] The invention further comprises the use of sodium
bicarbonate, sodium methyl cocoyl taurate (tauranol), MIT, and
benzyl alcohol and combinations thereof in the manufacture of a
Composition of the Invention, e.g., for use in any of the
indications set forth in the above method of Composition 1.0, et
seq.
DETAILED DESCRIPTION
[0124] As used herein, the term "oral composition" means the total
composition that is delivered to the oral surfaces. The composition
is further defined as a product which, during the normal course of
usage, is not, the purposes of systemic administration of
particular therapeutic agents, intentionally swallowed but is
rather retained in the oral cavity for a time sufficient to contact
substantially all of the dental surfaces and/or oral tissues for
the purposes of oral activity. Examples of such compositions
include, but are not limited to, toothpaste or a dentifrice, a
mouthwash or a mouth rinse, a topical oral gel, a denture cleanser,
and the like.
[0125] As used herein, the term "dentifrice" means paste, gel, or
liquid formulations unless otherwise specified. The dentifrice
composition can be in any desired form such as deep striped,
surface striped, multi-layered, having the gel surrounding the
paste, or any combination thereof. Alternatively the oral
composition may be dual phase dispensed from a separated
compartment dispenser.
Basic Amino Acids
[0126] The basic amino acids which can be used in the compositions
and methods of the invention include not only naturally occurring
basic amino acids, such as arginine, lysine, and histidine, but
also any basic amino acids having a carboxyl group and an amino
group in the molecule, which are water-soluble and provide an
aqueous solution with a pH of 7 or greater.
[0127] Accordingly, basic amino acids include, but are not limited
to, arginine, lysine, serine, citrullene, ornithine, creatine,
histidine, diaminobutanoic acid, diaminoproprionic acid, salts
thereof or combinations thereof. In a particular embodiment, the
basic amino acids are selected from arginine, citrullene, and
ornithine.
[0128] In certain embodiments, the basic amino acid is arginine,
for example, L-arginine, or a salt thereof.
[0129] The compositions of the invention (e.g., Composition 1.0 et
seq) are intended for topical use in the mouth and so salts for use
in the present invention should be safe for such use, in the
amounts and concentrations provided. Suitable salts include salts
known in the art to be pharmaceutically acceptable salts are
generally considered to be physiologically acceptable in the
amounts and concentrations provided. Physiologically acceptable
salts include those derived from pharmaceutically acceptable
inorganic or organic acids or bases, for example acid addition
salts formed by acids which form a physiological acceptable anion,
e.g., hydrochloride or bromide salt, and base addition salts formed
by bases which form a physiologically acceptable cation, for
example those derived from alkali metals such as potassium and
sodium or alkaline earth metals such as calcium and magnesium.
Physiologically acceptable salts may be obtained using standard
procedures known in the art, for example, by reacting a
sufficiently basic compound such as an amine with a suitable acid
affording a physiologically acceptable anion.
Fluoride Ion Source
[0130] The oral care compositions (e.g., Composition 1.0 et seq)
may further include one or more fluoride ion sources, e.g., soluble
fluoride salts. A wide variety of fluoride ion-yielding materials
can be employed as sources of soluble fluoride in the present
compositions. Examples of suitable fluoride ion-yielding materials
are found in U.S. Pat. No. 3,535,421, to Briner et al.; U.S. Pat.
No. 4,885,155, to Parran, Jr. et al. and U.S. Pat. No. 3,678,154,
to Widder et al., each of which are incorporated herein by
reference. Representative fluoride ion sources used with the
present invention (e.g., Composition 1.0 et seq.) include, but are
not limited to, stannous fluoride, sodium fluoride, potassium
fluoride, sodium monofluorophosphate, sodium fluorosilicate,
ammonium fluorosilicate, amine fluoride, ammonium fluoride, and
combinations thereof. In certain embodiments the fluoride ion
source includes stannous fluoride, sodium fluoride, sodium
monofluorophosphate as well as mixtures thereof. Where the
formulation comprises calcium salts, the fluoride salts are
preferably salts wherein the fluoride is covalently bound to
another atom, e.g., as in sodium monofluorophosphate, rather than
merely ionically bound, e.g., as in sodium fluoride.
Surfactants
[0131] The invention may in some embodiments contain anionic
surfactants, e.g., the Compositions of Composition 1.0, et seq.,
for example, water-soluble salts of higher fatty acid monoglyceride
monosulfates, such as the sodium salt of the monosulfated
monoglyceride of hydrogenated coconut oil fatty acids such as
sodium N-methyl N-cocoyl taurate, sodium cocomo-glyceride sulfate;
higher alkyl sulfates, such as sodium lauryl sulfate; higher
alkyl-ether sulfates, e.g., of formula
CH.sub.3(CH.sub.2).sub.mCH.sub.2(OCH.sub.2CH.sub.2).sub.nOS0.sub.3X,
wherein m is 6-16, e.g., 10, n is 1-6, e.g., 2, 3 or 4, and X is Na
or, for example sodium laureth-2 sulfate
(CH.sub.3(CH.sub.2).sub.10CH.sub.2(OCH.sub.2CH.sub.2).sub.2OS0.sub.3Na);
higher alkyl aryl sulfonates such as sodium dodecyl benzene
sulfonate (sodium lauryl benzene sulfonate); higher alkyl
sulfoacetates, such as sodium lauryl sulfoacetate (dodecyl sodium
sulfoacetate), higher fatty acid esters of 1,2 dihydroxy propane
sulfonate, sulfocolaurate (N-2-ethyl laurate potassium
sulfoacetamide) and sodium lauryl sarcosinate. By "higher alkyl" is
meant, e.g., C.sub.6-3o alkyl. In particular embodiments, the
anionic surfactant (where present) is selected from sodium lauryl
sulfate and sodium ether lauryl sulfate. When present, the anionic
surfactant is present in an amount which is effective, e.g.,
>0.001% by weight of the formulation, but not at a concentration
which would be irritating to the oral tissue, e.g., 1%, and optimal
concentrations depend on the particular formulation and the
particular surfactant. In one embodiment, the anionic surfactant is
present at from 0.03% to 5% by weight, e.g., 1.5%.
[0132] In another embodiment, cationic surfactants useful in the
present invention can be broadly defined as derivatives of
aliphatic quaternary ammonium compounds having one long alkyl chain
containing 8 to 18 carbon atoms such as lauryl trimethylammonium
chloride, cetyl pyridinium chloride, cetyl trimethylammonium
bromide, di-isobutylphenoxyethyldimethylbenzylammonium chloride,
coconut alkyltrimethylammonium nitrite, cetyl pyridinium fluoride,
and mixtures thereof. Illustrative cationic surfactants are the
quaternary ammonium fluorides described in U.S. Pat. No. 3,535,421,
to Briner et al., herein incorporated by reference. Certain
cationic surfactants can also act as germicides in the
compositions.
[0133] Illustrative nonionic surfactants of Composition 1.0, et
seq., that can be used in the compositions of the invention can be
broadly defined as 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, but are
not limited to, the Pluronics, 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. In a
particular embodiment, the composition of the invention comprises a
nonionic surfactant selected from poloxamers (e.g., poloxamer 407),
polysorbates (e.g., polysorbate 20), polyoxyl hydrogenated castor
oils (e.g., polyoxyl 40 hydrogenated castor oil), and mixtures
thereof.
[0134] Illustrative amphoteric surfactants of Composition 1.0, et
seq., that can be used in the compositions of the invention include
betaines (such as cocamidopropylbetaine), derivatives of aliphatic
secondary and tertiary amines in which the aliphatic radical can be
a straight or branched chain and wherein one of the aliphatic
substituents contains about 8-18 carbon atoms and one contains an
anionic water-solubilizing group (such as carboxylate, sulfonate,
sulfate, phosphate or phosphonate), and mixtures of such
materials.
[0135] The surfactant or mixtures of compatible surfactants can be
present in the compositions of the present invention (e.g.,
Composition 1.0 et seq) in 0.1% to 5%, in another embodiment 0.3%
to 3% and in another embodiment 0.5% to 2% by weight of the total
composition.
Flavoring Agents
[0136] The oral care compositions of the invention may also include
a flavoring agent. Flavoring agents which are used in the practice
of the present invention include, but are not limited to, essential
oils and various flavoring aldehydes, esters, alcohols, and similar
materials, as well as sweeteners such as sodium saccharin. Examples
of the essential oils include oils of spearmint, peppermint,
wintergreen, sassafras, clove, sage, eucalyptus, marjoram,
cinnamon, lemon, lime, grapefruit, and orange. Also useful are such
chemicals as menthol, carvone, and anethole. Certain embodiments
employ the oils of peppermint and spearmint.
[0137] The flavoring agent is incorporated in the oral composition
(e.g., Composition 1.0 et seq) at a concentration of 0.01 to 2% by
weight.
Chelating and Anti-Calculus Agents
[0138] The oral care compositions of the invention also may include
one or more chelating agents able to complex calcium found in the
cell walls of the bacteria. Binding of this calcium weakens the
bacterial cell wall and augments bacterial lysis.
[0139] Another group of agents suitable for use as chelating or
anti-calculus agents in the present invention are the soluble
pyrophosphates. The pyrophosphate salts used in the present
compositions can be any of the alkali metal pyrophosphate salts. In
certain embodiments, salts include tetra alkali metal
pyrophosphate, dialkali metal diacid pyrophosphate, trialkali metal
monoacid pyrophosphate and mixtures thereof, wherein the alkali
metals are sodium or potassium. The salts are useful in both their
hydrated and unhydrated forms. An effective amount of pyrophosphate
salt useful in the present composition is generally enough to
provide least 0.1 wt. % pyrophosphate ions, e.g., 0.1 to 3 wt 5,
e.g., 0.1 to 2 wt %, e.g., 0.1 to 1 wt %, e.g., 0.2 to 0.5 wt %.
The pyrophosphates also contribute to preservation of the
compositions by lowering water activity.
Polymers
[0140] The oral care compositions of the invention also optionally
include one or more polymers, such as polyethylene glycols,
polyvinyl methyl ether maleic acid copolymers, polysaccharides
(e.g., cellulose derivatives, for example carboxymethyl cellulose,
or polysaccharide gums, for example xanthan gum or carrageenan
gum). Acidic polymers, for example polyacrylate gels, may be
provided in the form of their free acids or partially or fully
neutralized water soluble alkali metal (e.g., potassium and sodium)
or ammonium salts. Certain embodiments include 1:4 to 4:1
copolymers of maleic anhydride or acid with another polymerizable
ethylenically unsaturated monomer, for example, methyl vinyl ether
(methoxyethylene) having a molecular weight (M.W.) of about 30,000
to about 1,000,000. These copolymers are available for example as
Gantrez AN 139(M.W. 500,000), AN 1 19 (M.W. 250,000) and S-97
Pharmaceutical Grade (M.W. 70,000), of GAF Chemicals
Corporation.
[0141] Other operative polymers include those such as the 1:1
copolymers of maleic anhydride with ethyl acrylate, hydroxyethyl
methacrylate, N-vinyl-2-pyrollidone, or ethylene, the latter being
available for example as Monsanto EMA No. 1 103, M.W. 10,000 and
EMA Grade 61, and 1:1 copolymers of acrylic acid with methyl or
hydroxyethyl methacrylate, methyl or ethyl acrylate, isobutyl vinyl
ether or N-vinyl-2-pyrrolidone.
[0142] Suitable generally, are polymerized olefinically or
ethylenically unsaturated carboxylic acids containing an activated
carbon-to-carbon olefinic double bond and at least one carboxyl
group, that is, an acid containing an olefinic double bond which
readily functions in polymerization because of its presence in the
monomer molecule either in the alpha-beta position with respect to
a carboxyl group or as part of a terminal methylene grouping.
Illustrative of such acids are acrylic, methacrylic, ethacrylic,
alpha-chloroacrylic, crotonic, beta-acryloxy propionic, sorbic,
alpha-chlorsorbic, cinnamic, beta-styrylacrylic, muconic, itaconic,
citraconic, mesaconic, glutaconic, aconitic, alpha-phenylacrylic,
2-benzyl acrylic, 2-cyclohexylacrylic, angelic, umbellic, fumaric,
maleic acids and anhydrides. Other different olefinic monomers
copolymerizable with such carboxylic monomers include vinylacetate,
vinyl chloride, dimethyl maleate and the like. Copolymers contain
sufficient carboxylic salt groups for water-solubility.
[0143] A further class of polymeric agents includes a composition
containing homopolymers of substituted acrylamides and/or
homopolymers of unsaturated sulfonic acids and salts thereof, in
particular where polymers are based on unsaturated sulfonic acids
selected from acrylamidoalkane sulfonic acids such as 2-acrylamide
2 methylpropane sulfonic acid having a molecular weight of about
1,000 to about 2,000,000, described in U.S. Pat. No. 4,842,847,
Jun. 27, 1989 to Zahid, incorporated herein by reference.
[0144] Another useful class of polymeric agents includes polyamino
acids, particularly those containing proportions of anionic
surface-active amino acids such as aspartic acid, glutamic acid and
phosphoserine, as disclosed in U.S. Pat. No. 4,866,161 Sikes et
al., incorporated herein by reference.
[0145] In preparing oral care compositions, it is sometimes
necessary to add some thickening material to provide a desirable
consistency or to stabilize or enhance the performance of the
formulation. In certain embodiments, the thickening agents are
carboxyvinyl polymers, carrageenan, xanthan gum, hydroxyethyl
cellulose and water soluble salts of cellulose ethers such as
sodium carboxymethyl cellulose and sodium carboxymethyl
hydroxyethyl cellulose. Natural gums such as karaya, gum arabic,
and gum tragacanth can also be incorporated. Colloidal magnesium
aluminum silicate or finely divided silica can be used as component
of the thickening composition to further improve the composition's
texture. In certain embodiments, thickening agents in an amount of
about 0.5% to about 5.0% by weight of the total composition are
used.
Abrasives
[0146] Natural calcium carbonate is found in rocks such as chalk,
limestone, marble and travertine. It is also the principle
component of egg shells and the shells of mollusks. The natural
calcium carbonate abrasive of the invention is typically a finely
ground limestone which may optionally be refined or partially
refined to remove impurities. For use in the present invention, the
material has an average particle size of less than 10 microns,
e.g., 3-7 microns, e.g. about 5.5 microns. For example a small
particle silica may have an average particle size (D50) of 2.5-4.5
microns. Because natural calcium carbonate may contain a high
proportion of relatively large particles of not carefully
controlled, which may unacceptably increase the abrasivity,
preferably no more than 0.01%, preferably no more than 0.004% by
weight of particles would not pass through a 325 mesh. The material
has strong crystal structure, and is thus much harder and more
abrasive than precipitated calcium carbonate. The tap density for
the natural calcium carbonate is for example between 1 and 1.5
g/cc, e.g., about 1.2 for example about 1.19 g/cc. There are
different polymorphs of natural calcium carbonate, e.g., calcite,
aragonite and vaterite, calcite being preferred for purposes of
this invention. An example of a commercially available product
suitable for use in the present invention includes Vicron.RTM.
25-11 FG from GMZ.
[0147] Precipitated calcium carbonate is generally made by
calcining limestone, to make calcium oxide (lime), which can then
be converted back to calcium carbonate by reaction with carbon
dioxide in water. Precipitated calcium carbonate has a different
crystal structure from natural calcium carbonate. It is generally
more friable and more porous, thus having lower abrasivity and
higher water absorption. For use in the present invention, the
particles are small, e.g., having an average particle size of 1-5
microns, and e.g., no more than 0.1%, preferably no more than 0.05%
by weight of particles which would not pass through a 325 mesh. The
particles may for example have a D50 of 3-6 microns, for example
3.8=4.9, e.g., about 4.3; a D50 of 1-4 microns, e.g. 2.2-2.6
microns, e.g., about 2.4 microns, and a D10 of 1-2 microns, e.g.,
1.2-1.4, e.g. about 1.3 microns. The particles have relatively high
water absorption, e.g., at least 25 g/100 g, e.g. 30-70 g/100 g.
Examples of commercially available products suitable for use in the
present invention include, for example, Carbolag.RTM. 15 Plus from
Lagos Industria Quimica.
[0148] In certain embodiments the invention may comprise additional
calcium-containing abrasives, for example calcium phosphate
abrasive, e.g., tricalcium phosphate (Ca.sub.3(P0.sub.4).sub.2),
hydroxyapatite (Ca.sub.10(PO.sub.4).sub.6(OH).sub.2), or dicalcium
phosphate dihydrate (CaHP0.sub.4.2H.sub.20, also sometimes referred
to herein as DiCal) or calcium pyrophosphate, and/or silica
abrasives, sodium metaphosphate, potassium metaphosphate, aluminum
silicate, calcined alumina, bentonite or other siliceous materials,
or combinations thereof. Any silica suitable for oral care
compositions may be used, such as precipitated silicas or silica
gels. For example synthetic amorphous silica. Silica may also be
available as a thickening agent, e.g., particle silica. For
example, the silica can also be small particle silica (e.g.,
Sorbosil AC43 from PQ Corporation, Warrington, United Kingdom).
However the additional abrasives are preferably not present in a
type or amount so as to increase the RDA of the dentifrice to
levels which could damage sensitive teeth, e.g., greater than
130.
Water
[0149] Water is present in the oral compositions of the invention.
Water, employed in the preparation of commercial oral compositions
should be deionized and free of organic impurities. Water commonly
makes up the balance of the compositions and includes 5% to 45%,
e.g., 10% to 20%, e.g., 25-35%, by weight of the oral compositions.
This amount of water includes the free water which is added plus
that amount which is introduced with other materials such as with
sorbitol or silica or any components of the invention. The Karl
Fischer method is a one measure of calculating free water.
Humectants
[0150] Within certain embodiments of the oral compositions, it is
also desirable to incorporate a further humectant (e.g., in
addition to glycerin) to reduce evaporation and also contribute
towards preservation by lowering water activity. Certain humectants
can also impart desirable sweetness or flavor to the compositions.
The humectant, on a pure humectant basis, generally includes 15% to
70% in one embodiment or 30% to 65% in another embodiment by weight
of the composition.
[0151] Suitable humectants include edible polyhydric alcohols such
as glycerin, sorbitol, xylitol, propylene glycol as well as other
polyols and mixtures of these humectants. Mixtures of glycerine and
sorbitol may be used in certain embodiments as the humectant
component of the compositions herein (e.g., Composition 1.0 et
seq).
[0152] The present invention in its method aspect involves applying
to the oral cavity a safe and effective amount of the compositions
described herein.
[0153] The compositions and methods according to the invention
(e.g., Composition 1.0 et seq) can be incorporated into oral
compositions for the care of the mouth and teeth such as
toothpastes, transparent pastes, gels, mouth rinses, sprays and
chewing gum.
[0154] 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
reference 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. It is understood that when
formulations are described, they may be described in terms of their
ingredients, as is common in the art, notwithstanding that these
ingredients may react with one another in the actual formulation as
it is made, stored and used, and such products are intended to be
covered by the formulations described.
[0155] The following examples further describe and demonstrate
illustrative embodiments within the scope of the present invention.
The examples are given solely for illustration and are not to be
construed as limitations of this invention as many variations are
possible without departing from the spirit and scope thereof.
Various modifications of the invention in addition to those shown
and described herein should be apparent to those skilled in the art
and are intended to fall within the appended claims.
Example 1
[0156] Combinations of humectants (single and mixed, with net
humectant levels of about 35%) are evaluated for foam analysis
(Foam Volume) using the SITA Foam Tester R-2000 at 40 Seconds.
[0157] Samples are prepared as toothpaste slurries. While mixing
this slurry, minimum foam is generated. The slurry is poured into a
jacketed glass beaker each time. To ensure that the slurry does not
separate, the mixture is continuously stirred on a magnetic stir
plate. Once the program starts, 250 mL of the slurry is transferred
via a rubber hose. Once the desired amount is reached, needles
measure the baseline and then, the rotor speeds up to 800 rpm. The
volume of foam generated is measured every 10 s for 40 s by the
needles. The foam volume at 40 s is determined as the average over
all replicates.
[0158] Foam density is assessed visually while the SITA foam tester
is measuring foam decay at 10 s intervals After the Foam Generation
procedure, the Foam Tester will measure foam decay at 10 s second
intervals 6 times. At a set time interval the following values are
considered: foam volume given by the SITA instrument; actual liquid
volume. With these observations and knowing the original test
volume and the density of the test slurry, foam density is
calculated.
Results are demonstrated in Table 1.
TABLE-US-00001 TABLE 1 (Foam Volume) Description Net Avg. Foam (%
listed by Humectant Volume Std. Formulation wt. of composition) (%)
(ml) Dev. Formula A ZnO 1.0%, ZnCit 0.5%, 34.5 219 3 Arginine 1.5%,
Sorbitol 45%, Glycerin 3% Formula B ZnO 1.0%, ZnCit 0.5%, 34 198 10
Arginine 1.5%, Sorbitol 20%, Glycerin 20% Formula C ZnO 1.0%, ZnCit
0.5%, 35.1 306 8 Arginine 1.5% Sorbitol 13%, Glycerin 26% Formula D
ZnO 1.0%, ZnCit 0.5%, 35 294 25 Arginine 1.5% Glycerin 35%
[0159] Formulations A and B contain sorbitol (70% in solution) at
amounts from 20-45% by wt. of the total composition.
[0160] Formulations C and D contain sorbitol (70% in solution) at
amounts from 0-13% by wt. The glycerin ranges from 26%-35% in these
formulations. Foam volume of Formulations C and D is significantly
increased than either Formulation A or B.
Example 2
[0161] Combinations of humectants (single and mixed, with net
humectant levels of about 35%) are evaluated for foam analysis
(Foam Density) using the SITA Foam Tester R-2000 at 40 Seconds.
Results are demonstrated in Table 2.
TABLE-US-00002 TABLE 2 Net Avg. Foam Humectant Density Std.
Formulation Description (%) (g/ml) Dev. Formula E ZnO 1.0%, ZnCit
0.5%, 34.5 0.275 0.005 Arginine 1.5% Sorbitol 45%, Glycerin 3%
Formula F ZnO 1.0%, ZnCit 0.5%, 35 0.361 0.006 Arginine 1.5%
Glycerin 35%
[0162] Formula E comprises 45% by wt of the composition sorbitol
(70% in solution) and 3% glycerin, and Formula F comprises 35%
glycerin without the addition of any sorbitol. The foam density of
Formula F (glycerin 35%) shows a clear increase over the foam
density of Formula E wherein the sorbitol amount by wt. of the
composition, is used in far greater amounts than the glycerin.
[0163] Examples 1 and 2 demonstrate increased foam volume and foam
density in formulations which employ glycerin in an amount from
26%-35% by wt. (as compared to the representative sorbitol
formulations).
Example 3
[0164] In one representative formulation, a dentifrice comprises
the following: [0165] a. 1.0 wt. % zinc oxide [0166] b. 0.5 wt. %
zinc citrate [0167] c. 1.5 wt. % L-arginine [0168] d. 0.32 wt. %
sodium fluoride; and [0169] e. 35% wt. glycerin
[0170] Wherein the dentifrice is expected to have increased foam
volume and density compared to formulations which employ between
20%-45% sorbitol.
Example 4
[0171] Representative Dentifrice Formulations
The data from the following formulations is detailed in above
Example 1 and Example 2.
TABLE-US-00003 Formulation Formulation Formulation Ingredient A
(wt. %) Ingredient B (wt. %) Ingredient C (wt. %) 99.0%-101.0% 3
99.0%-101.0% 20 99.0%-101.0% 26 GLYCERIN - USP, GLYCERIN - USP,
GLYCERIN - USP, EP VEG EP VEG EP VEG POLYMERS 1.1 POLYMERS 1.1
POLYMERS 1.1 FLAVORING 2 DEMINERALIZED Q.S. DEMINERALIZED Q.S.
AGENTS WATER WATER SODIUM 0.32 FLAVORING 2 FLAVORING 2 FLUORIDE -
USP, AGENTS AGENTS EP ALKALI 0.5 SODIUM 0.32 SODIUM 0.32 PHOSPHATE
FLUORIDE - USP, FLUORIDE - USP, SALT EP EP SORBITOL - 45 ALKALI 0.5
ALKALI 0.5 NON-CRYSTAL - PHOSPHATE PHOSPHATE 70% SOLN USP, SALT
SALT DEMINERALIZED Q.S. SORBITOL 20 SORBITOL 13 WATER NON-CRYSTAL -
NON-CRYSTAL - 70% SOLN USP, 70% SOLN USP, EP EP ZINC CITRATE 0.5
ZINC CITRATE 0.5 ZINC CITRATE 0.5 TRIHYDRATE TRIHYDRATE TRIHYDRATE
L-ARGININE 1.5 L-ARGININE 1.5 L-ARGININE 1.5 85% SYRUPY 0.35 85%
SYRUPY 0.35 85% SYRUPY 0.35 PHOSPHORIC PHOSPHORIC PHOSPHORIC ACID -
FOOD ACID - FOOD ACID - FOOD GRADE GRADE GRADE ZINC OXIDE 1 ZINC
OXIDE 1 ZINC OXIDE 1 COLORANT 0.75 COLORANT 0.75 COLORANT 0.75
ABRASIVES 20 ABRASIVES 20 ABRASIVES 20 SILICA- 4.5 THICKENER 4.5
THICKENER 4.5 THICKENR SILICA SILICA AMPHOTERIC 1.25 AMPHOTERIC
1.25 AMPHOTERIC 1.25 SURFACTANT SURFACTANT SURFACTANT NON-IONIC 0.5
NON-IONIC 0.5 NON-IONIC 0.5 SURFACTANTS SURFACTANTS SURFACTANTS
ANIONIC 2 ANIONIC 2 ANIONIC 2 SURFACTANT SURFACTANT SURFACTANT
PRESERVATIVE 0.2 PRESERVATIVE 0.2 PRESERVATIVE 0.2 Total Components
100 Total Components 100 Total Components 100 Formulation
Formulation Formulation Ingredient D (wt. %) Ingredient E (wt. %)
Ingredient F (wt. %) 99.0%-101.0% 35 99.0%-101.0% 3 99.0%-101.0% 35
GLYCERIN - USP, GLYCERIN - USP, GLYCERIN - USP, EP VEG EP VEG EP
VEG POLYMERS 1.1 POLYMERS 0.7 POLYMERS 1.2 DEMINERALIZED Q.S.
FLAVORING 1.9 SODIUM 0.32 WATER AGENTS FLUORIDE - USP, EP FLAVORING
2 SODIUM 0.32 ALKALI 0.5 AGENT FLUORIDE - USP, PHOSPHATE EP SALT
SODIUM 0.32 ALKALI 0.5 DEMINERALIZED Q.S. FLUORIDE - USP, PHOSPHATE
WATER EP SALT ALKALI 0.5 SORBITOL 45 ABRASIVES 15 PHOSPHATE SALT
ZINC CITRATE 0.5 SILICA- 6 TRIHYDRATE THICKENER L-ARGININE 1.5
ABRASIVES 20 FLAVORING 1.9 INGREDIENT 85% SYRUPY 0.35 SILICA - 6.5
ANIONIC 5.7 PHOSPHORIC THICKENER SURFACTANT ACID - FOOD GRADE ZINC
OXIDE 1 ANIONIC 5.7 AMPHOTERIC 1.25 SURFACTANT SURFACTANT COLORANT
0.75 AMPHOTERIC 1.25 NON-IONIC 0.5 SURFACTANT SURFACTANTS ABRASIVES
20 NON-IONIC 0.5 ZINC CITRATE 0.5 SURFACTANTS TRIHYDRATE SILICA -
4.5 ZINC OXIDE 1 COLORANT 0.75 THICKENER AMPHOTERIC 1.25 ZINC
CITRATE 0.5 PRESERVATIVE 0.4 SURFACTANT TRIHYDRATE NON-IONIC 0.5
COLORANT 0.75 85% SYRUPY 0.35 SURFACTANTS PHOSPHORIC ACID - FOOD
GRADE ANIONIC 2 PRESERVATIVE 0.3 L-ARGININE 1.5 SURFACTANT
PRESERVATIVE 0.2 85% SYRUPY 0.35 ZINC OXIDE 1 PHOSPHORIC ACID -
FOOD GRADE Total Components 100 L-ARGININE 1.5 Total Components 100
DEMINERALIZED Q.S. WATER Total Components 100
Example 5
Representative Dentifrice Formulations
TABLE-US-00004 [0172] Description Formula 1 Formula 2 Formula 3
DEMINERALIZED WATER Q.S. Q.S. Q.S. ABRASIVES 10%-20% 15%-20%
15%-20% 99.0%-101.0% GLYCERIN - 35 35 35 USP, EP VEG L-Arginine 1.5
1.5 1.5 AMPHOTERIC SURFACTANT 1.0%-1.5% 1.0%-1.5% 1.0%-1.5%
NON-IONIC SURFACTANTS 0.25%-0.75% 0.25%-0.75% 0.25%-0.75% POLYMERS
1.0%-1.4% 0.75%-1.25% 1.1%-1.5% ALKALI PHOSPHATE SALT 0.25%-0.75%
0.25%-0.75% 0.25%-0.75% ZINC CITRATE TRIHYDRATE 0.5 0.5 0.5
COLORANT 0.25%-1.0% 0.25%-1.0% 0.25%-1.0% FLAVORING AGENTS
1.5%-1.9% 1.5%-1.9% 1.5%-1.9% 85% SYRUPY PHOSPHORIC 0.35 0.35 0
ACID - FOOD GRADE SODIUM FLUORIDE - 0.32 0.32 0.32 USP, EP SILICA -
THICKENER 5%-7% 5%-7% 6%-8% ANIONIC SURFACTANT 1%-3% 1%-3% 1%-3%
ZINC OXIDE 1 1 1 PRESERVATIVE 0.4 0.4 0.4 Total Components 100 100
100
[0173] 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.
[0174] 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.
[0175] While the present invention has been described with
reference to embodiments, it will be understood by those skilled in
the art that various modifications and variations may be made
therein without departing from the scope of the present invention
as defined by the appended claims.
* * * * *