U.S. patent application number 15/749541 was filed with the patent office on 2018-08-09 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 Amit AHUJA, Claude BLANVALET, Xiao Yi HUANG, Lisa MANUS, Andre MORGAN, Vyoma PATEL, Andrei POTANIN, Tilo POTH, Michael PRENCIPE, Amy RUSSO, Hansruedi STETTLER, Michael STRANICK, Chengkang TAN, Betty WON, Peng YAN.
Application Number | 20180221259 15/749541 |
Document ID | / |
Family ID | 59276905 |
Filed Date | 2018-08-09 |
United States Patent
Application |
20180221259 |
Kind Code |
A1 |
POTANIN; Andrei ; et
al. |
August 9, 2018 |
Oral Care Compositions and Methods of Use
Abstract
Described herein are oral care compositions comprising a basic
amino acid; a combination of zinc ion sources; and a thickening
system comprising a nonionic cellulose ether having a viscosity,
measured at 2% in water at 25.degree. C., of 4500 to 7500 cps; and
a polysaccharide gum; along with methods of making and using
same.
Inventors: |
POTANIN; Andrei;
(Hillsborough, NJ) ; POTH; Tilo; (Weinheim,
DE) ; AHUJA; Amit; (Highland Park, NJ) ;
BLANVALET; Claude; (Angleur, BE) ; WON; Betty;
(Princeton Junction, NJ) ; MANUS; Lisa;
(Lawrenceville, NJ) ; STRANICK; Michael;
(Bridgewater, NJ) ; HUANG; Xiao Yi; (Guangzhou,
CN) ; PRENCIPE; Michael; (West Windsor, NJ) ;
RUSSO; Amy; (Belle Mead, NJ) ; STETTLER;
Hansruedi; (Basel, CH) ; YAN; Peng;
(Guangzhou, CN) ; TAN; Chengkang; (Guangzhou,
CN) ; PATEL; Vyoma; (Hillsborough, NJ) ;
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: |
59276905 |
Appl. No.: |
15/749541 |
Filed: |
June 23, 2017 |
PCT Filed: |
June 23, 2017 |
PCT NO: |
PCT/US17/39074 |
371 Date: |
February 1, 2018 |
Current U.S.
Class: |
1/1 |
Current CPC
Class: |
A61K 8/44 20130101; A61K
8/25 20130101; A61K 2800/48 20130101; A61Q 11/00 20130101; A61K
8/731 20130101; A61K 8/042 20130101; A61K 2800/52 20130101; A61K
2800/28 20130101; A61K 8/27 20130101; A61K 8/365 20130101; A61P
1/02 20180101; A61K 8/24 20130101; A61K 8/34 20130101; A61K 8/21
20130101; A61K 8/37 20130101; A61K 8/442 20130101; A61K 8/73
20130101 |
International
Class: |
A61K 8/44 20060101
A61K008/44; A61K 8/27 20060101 A61K008/27; A61K 8/37 20060101
A61K008/37; A61K 8/73 20060101 A61K008/73; A61K 8/21 20060101
A61K008/21; A61K 8/04 20060101 A61K008/04; A61Q 11/00 20060101
A61Q011/00 |
Foreign Application Data
Date |
Code |
Application Number |
Jun 24, 2016 |
CN |
PCT/CN2016/086994 |
Claims
1. An oral care composition comprising: a. a basic amino acid in
free or salt form wherein the basic amino acid is selected from
arginine, lysine, and a combination thereof, b. a combination of
zinc ion sources: and c. a thickening system comprising: i. from
about 0.1 wt. % to about 1 wt. % of a nonionic cellulose ether: and
ii. from about 0.25 wt. % to about 1 wt. % of a polysaccharide
gum.
2. The oral care composition according to claim 1, wherein the
nonionic cellulose ether has a viscosity, measured at 2% in water
at 25.degree. C., of from about 4500 to about 7500 cps.
3. The oral care composition according to claim 1, wherein the
nonionic cellulose ether has a viscosity, measured at 2% in water
at 25.degree. C., of from about 4500 to about 6500 cps.
4. The oral care composition according to claim 1, wherein the
nonionic cellulose ether has a viscosity, measured at 2% in water
at 25.degree. C., of from about 6000 to about 7500 cps.
5. The oral care composition according to claim 1, comprising from
about 0.1 wt. % to about 0.8 wt. % of a nonionic cellulose
ether.
6. The oral care composition according to claim 1, comprising from
about 0.1 wt. % to about 0.5 wt. % of a nonionic cellulose
ether.
7. The oral care composition according to claim 1, comprising from
about 0.1 wt. % to about 0.3 wt. % of a nonionic cellulose
ether.
8. The oral care composition according to claim 1, comprising 0.1
wt. %, 0.15 wt. %, 0.2 wt. %, 0.25 wt. % or 0.3 wt. % of a nonionic
cellulose ether.
9. The oral care composition according to claim 1, wherein the
nonionic cellulose ether comprises hydroxyethylcellulose.
10. The oral care composition according to claim 1, comprising from
about 0.3 wt. % to about 1 wt. % of a polysaccharide gum.
11. The oral care composition according to claim 1, comprising from
about 0.4 wt. % to about 1 wt. % of a polysaccharide gum.
12. The oral care composition according to claim 1, comprising from
about 0.5 wt. % to about 1 wt. % of a polysaccharide gum.
13. The oral care composition according to claim 1, comprising from
about 0.6 wt. % to about 0.9 wt. % of a polysaccharide gum.
14. The oral care composition according to claim 1, comprising
about 0.3 wt. %, 0.4 wt. %, 0.5 wt. %, 0.6 wt. %, 0.7 wt. %, 0.8
wt. %, 0.9 wt. % or 1 wt. % of a polysaccharide gum.
15. The oral care composition according to claim 1, wherein the
polysaccharide gum is xanthan gum.
16. The oral care composition according to claim 1, wherein the
thickening system further comprises from about 5 wt. % to to about
10 wt. %
17. The oral care composition according to claim 1, wherein the
thickening system comprises from about 0.5 wt. % to about 15 wt. %
of the oral care composition.
18. The oral care composition according to claim 1, wherein the
nonionic cellulose ether and the polysaccharide gum are present in
a weight ratio of from about 1:1 to about 1:10.
19. The oral care composition according to claim 1, wherein the
nonionic cellulose ether and the polysaccharide gum are present in
a weight ratio of from about 1:2 to about 1:10.
20. The oral care composition according to claim 1, wherein the
nonionic cellulose ether and the polysaccharide gum are present in
a weight ratio of from about 1:3 to about 1:10.
21. The oral care composition according to claim 1, wherein the
nonionic cellulose ether and the polysaccharide gum are present in
a weight ratio of 1:3, 1:4, 1:5, 1:6, 1:7, 1:8, or 1:9.
22. The oral care composition according to claim 1, wherein the
combination of zinc ion sources comprises zinc oxide and zinc
citrate.
23. The oral care composition according to claim 1, wherein the
amino acid is arginine, and is present at about 1.5 wt. %, 5 wt. %,
or about 8 wt. %, of the oral care composition.
24. The oral care composition according to claim 22, wherein the
weight ratio of zinc oxide to zinc citrate is about 2:1.
25. The oral care composition according to claim 22, wherein the
zinc citrate is in an amount of about 0.5 wt. % and zinc oxide is
present in an amount of about 1.0 wt. % based on the total weight
of the oral care composition.
26. The oral care composition according to claim 1, further
comprising a fluoride ion source selected from sodium fluoride,
sodium monofluorophosphate, and stannous fluoride.
27. The oral care composition according to claim 26, wherein the
fluoride ion source provides soluble fluoride in an amount of about
1450 ppm.
28. The oral care composition according to claim 26, wherein the
fluoride ion source comprises stannous fluoride.
29. The oral care composition according to claim 1, comprising: a.
about 1.0 wt. % zinc oxide b. about 0.5 wt. % zinc citrate c. about
1.5 wt. % L-arginine d. from about 0.3 wt. % to about 0.9 wt. % of
xanthan gum; and e. from about 0.1 wt. % to about 0.5 wt. % of
hydroxyethylcellulose.
30. The oral care composition according to claim 29, comprising
from about 0.6 wt. % to about 0.8 wt. % of xanthan gum.
31. The oral care composition according to claim 29, comprising
from about 0.1 wt. % to about 0.3 wt. % of
hydroxyethylcellulose.
32. The oral care composition according to claim 1, wherein the
oral care composition is in a form selected from: a toothpaste, a
mouthwash, and a gel.
33. The oral care composition according to claim 1, having a static
yield stress greater than about 20 Pa, 25 Pa, 30 Pa, 35 Pa, or 40
Pa.
34. The oral care composition according to claim 1, having a
drainage time of less than about 10 minutes, about 9 minutes, about
8 minutes, about 7 minutes, about 6 minutes, about 5 minutes, about
4 minutes, about 3 minutes or about 2 minutes.
35. The oral care composition according to claim 1, demonstrating
less than about 225 grams of left-overs.
36. The oral care composition according to claim 1, wherein the
oral care composition loses no more than about 25% of its initial
viscosity after one year.
37. A method to improve oral health comprising applying an
effective amount of the oral care composition according to claim 1
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, ix. inhibit microbial bio
film formation in the oral cavity, x. raise and/or maintain plaque
pH at levels of at least 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 APPLICATION
[0001] This application claims the benefit of priority from PCT/CN
2016/086994, filed Jun. 24, 2016, the contents of which are hereby
incorporated by reference in their entirety.
BACKGROUND
[0002] Arginine-based oral care compositions generally include some
combination of polymers, abrasive(s); and in some instances,
additional active ingredients. In those instances where additional
active ingredients are included and comprise cationic metal ions,
e.g. zinc, maintaining the physical stability of the composition is
a challenge because of the interaction between these cationic metal
ions and certain polymeric components and abrasive systems.
[0003] The use of certain abrasives or specific concentrations of
particular polymers are two ways in which the stability issues have
been addressed. However, these methods have generally focused
individually on stand-up (i.e., appearance on the brush) and
squeezability from packaging (toothpaste tubes). As such, there
remains a need to reconcile these physical stability and
rheological concerns. Certain embodiments of the present invention
are designed to address this need.
BRIEF SUMMARY
[0004] Some embodiments of the present invention provide oral care
compositions comprising a basic amino acid in free or salt wherein
the amino acid is selected from arginine, lysine, and a combination
thereof; a combination of zinc ion sources; and a thickening system
comprising from about 0.1 wt. % to about 0.5 wt. % of a nonionic
cellulose ether; and from about 0.25 wt. % to about 1 wt. % of a
polysaccharide gum. In some embodiments, the nonionic cellulose
ether is hydroxyethylcellulose and the polysaccharide gum is
xanthan gum.
[0005] Other embodiments provide compositions further comprising a
silica abrasive which exhibits an approximately neutral pH when
measured in an aqueous medium. Still further embodiments provide
oral care compositions comprising a basic amino acid in free or
salt wherein the amino acid is selected from arginine, lysine, and
a combination thereof; a combination of zinc ion sources; a
thickening system comprising from about 0.1 wt. % to about 0.5 wt.
% of a nonionic cellulose ether; and from about 0.5 wt. % to about
1 wt. % of a polysaccharide gum; and a silica abrasive which
exhibits an approximately neutral pH when measured in an aqueous
medium.
[0006] In some embodiments, the oral care compositions of the
present invention demonstrate the ability to avoid viscosity loss
and maintain static yield stress over an extended period of time,
e.g. after one year.
[0007] In one aspect the invention is an oral care composition
(Composition 1.0) comprising: [0008] a. A basic amino acid in free
or salt from, wherein the amino acid is selected from arginine,
lysine, and combinations thereof; (e.g., free form arginine);
[0009] b. zinc oxide and zinc citrate; [0010] c. a fluoride source
(e.g., sodium fluoride); and [0011] d. a silica abrasive which
exhibits an acid pH when measured as an aqueous slurry (e.g.,
prophy silica).
[0012] 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): [0013] 1.01
Composition 1.0 wherein the silica abrasive which exhibits an acid
pH when measured as an aqueous slurry is prophy [0014] 1.02 Any of
the preceding compositions wherein the silica abrasive which
exhibits an acid pH when measured as an aqueous slurry is Sylodent
783. [0015] 1.03 Any of the preceding compositions wherein the
silica abrasive exhibits a pH of 3.5-4.5 in an aqueous slurry of
the abrasive. [0016] 1.04 Any of the preceding compositions wherein
the silica abrasive which exhibits an acid pH when measured as an
aqueous slurry is present in an amount from 2 to 35 weight percent.
[0017] 1.05 Any of the preceding compositions wherein the silica
abrasive which exhibits an acid pH when measured as an aqueous
slurry is present in an amount from 3 to 15 weight percent. [0018]
1.06 Any of the preceding compositions wherein the silica abrasive
which exhibits an acid pH when measured as an aqueous slurry is
present in an amount selected from 2 wt. %, 3 wt. %, 4 wt. %, 5 wt.
%, 6 wt. %, 7 wt. %, 8 wt. %, 9 wt. %, 10 wt. %, 11 wt. %, 12 wt.
%, 13 wt. %, 14 wt. %, 15 wt. %, 16 wt. %, 17 wt. %, 18 wt. %, 19
wt. %, 20 wt. %. [0019] 1.07 Any of the preceding compositions
wherein the basic amino acid has the L-configuration (e.g.,
L-arginine). [0020] 1.08 Any of the preceding compositions wherein
the basic amino acid is arginine or lysine is in free form. [0021]
1.09 Any of the preceding compositions wherein the basic amino acid
is provided in the form of a di- or tri-peptide comprising arginine
or lysine, or salts thereof. [0022] 1.10 Any of the preceding
compositions wherein the basic amino acid is arginine or lysine,
and wherein the arginine or lysine 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. [0023]
1.11 Any of the preceding compositions wherein the amino acid is
arginine from 0.1 wt. %-6.0 wt. %. (e.g., about 1.5 wt. %). [0024]
1.12 Any of the preceding compositions wherein the amino acid is
arginine from about 1.5 wt. %. [0025] 1.13 Any of the preceding
compositions wherein the amino acid is arginine from 4.5 wt. %-8.5
wt, % (e.g., 5.0%). [0026] 1.14 Any of the preceding compositions
wherein the amino acid is arginine from about 5.0 wt. %. [0027]
1.15 Any of the preceding compositions wherein the amino acid is
arginine from 3.5%-9 wt. %. [0028] 1.16 Any of the preceding
compositions wherein the amino acid is arginine from about 8.0 wt.
%. [0029] 1.17 Any of the preceding compositions wherein the amino
acid is L-arginine. [0030] 1.18 Any of the preceding compositions
wherein the amino acid is a free form arginine. [0031] 1.19 Any of
the preceding compositions wherein the basic amino acid is lysine
2% wt., 3% wt., 4% wt., 5% wt., 6% wt.), (e.g., 4% wt.). [0032]
1.20 Any of the preceding compositions wherein the amino acid is
lysine from 1.0 wt.-6.0 wt. %. [0033] 1.21 Any of the preceding
compositions wherein the amino acid is lysine from about 1.5 wt. %.
[0034] 1.22 Any of the preceding compositions wherein the amino
acid is lysine from about 4.0 wt. %. [0035] 1.23 Any of the
preceding compositions wherein the amino acid is L-lysine. [0036]
1.24 Any of the preceding compositions wherein the amino acid is
free form lysine. [0037] 1.25 Any of the preceding compositions
wherein the amino acid is arginine or lysine in partially or wholly
in salt form. [0038] 1.26 Composition 1.25 wherein the amino acid
is arginine phosphate. [0039] 1.27 Composition 1.25 wherein the
amino acid is arginine hydrochloride. [0040] 1.28 Composition 1.25
wherein the amino acid is arginine bicarbonate. [0041] 1.29
Composition 1.25 wherein the amino acid is lysine phosphate. [0042]
1.30 Composition 1.25 wherein the amino acid is lysine
hydrochloride. [0043] 1.31 Composition 1.25 wherein the amino acid
is lysine bicarbonate. [0044] 1.32 Any of the preceding
compositions wherein the amino acid is arginine or lysine ionized
by neutralization with an acid or a salt of an acid. [0045] 1.33
Any of preceding compositions wherein the composition is
ethanol-free. [0046] 1.34 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. [0047] 1.35 The composition of 1.34, wherein
the fluoride source is stannous fluoride. [0048] 1.36 Any of the
preceding compositions wherein the fluoride source is a
fluorophosphate. [0049] 1.37 Any of the preceding compositions
wherein the fluoride source is sodium monofluorophosphate. [0050]
1.38 The composition of 1.34, wherein the fluoride source is sodium
fluoride. [0051] 1.39 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. %) or sodium
monofluorophosphate) [0052] 1.40 Any of the preceding compositions
wherein the fluoride source is sodium fluoride in an amount about
0.32 wt. % based on the weight of the composition. [0053] 1.41 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., 750-2000ppm, e.g., 1000-1500 ppm,
e.g., about 1000 ppm, e.g., about 1450 ppm) [0054] 1.42 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). [0055] 1.43 Any of the preceding
compositions wherein the fluoride source is selected from sodium
fluoride and sodium monofluorophosphate and which provides fluoride
in an amount from 1000 ppm-1500 ppm. [0056] 1.44 Any of the
preceding compositions wherein the fluoride source is sodium
fluoride or sodium monofluorophosphate and which provides fluoride
in an amount of about 1450 ppm. [0057] 1.45 Any of the preceding
compositions wherein the pH is between 6.0 and 10.5, e.g., 7.0 to
9.0, e,g., about 8.0. [0058] 1.46 Any of the preceding compositions
further comprising calcium carbonate. [0059] 1.47 The composition
of 1.46, 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). [0060] 1.48 The composition of 1.47, further
comprising a precipitated calcium carbonate-light (e.g., about 10%
precipitated calcium carbonate-light) (e.g., about 10% natural
calcium carbonate). [0061] 1.49 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, 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. [0062] 1.50 Any of the
preceding compositions comprising tetrapotassium pyrophosphate,
disodium hydrogenorthophosphate, monosodium phosphate, and
pentapotassium triphosphate. [0063] 1.51 Any of the preceding
compositions, wherein the composition further comprises stannous
pyrophosphate, wherein the stannous pyrophosphate is from 0.1%-3%
by wt. of the composition. (e.g., about 1% by wt. of the
composition). [0064] 1.52 Any of the preceding compositions
comprising a polyphosphate. [0065] 1.53 The composition of 1.49,
wherein the polyphosphate is tetrasodium pyrophosphate. [0066] 1.54
The composition of 1.53, wherein the tetrasodium pyrophosphate is
from 0.1-1.0 wt. % (e.g., about 0.5 wt. %). [0067] 1.55 Any of the
preceding compositions further comprising a second abrasive or
particulate (e.g., silica). [0068] 1.56 Any of the preceding
compositions wherein the second abrasive silica is synthetic
amorphous silica. (e.g., 1%-28% by wt.) (e.g., 8%-25% by wt.)
[0069] 1.57 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. [0070] 1.58 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 Chemicals, Warrington, United Kingdom).
[0071] 1.59 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 3-4microns) and
wherein the small particle silica is about 5 wt. % of the oral care
composition. [0072] 1.60 Any of the preceding compositions
comprising silica wherein the silica is used as a thickening agent,
e.g., particle silica. [0073] 1.61 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
polysorbate 20), polyoxyl hydrogenated castor oil (e.g., polyoxyl
40 hydrogenated castor oil), and mixtures thereof. [0074] 1.62 Any
of the preceding compositions, wherein the poloxamer nonionic
surfactant has an average polyoxypropylene molecular mass (Mw) 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. [0075] 1.63 Any of the preceding compositions
further comprising glycerin, wherein the glycerin is in a total
amount of 25-40% (e.g., about 35%). [0076] 1.64 The composition of
1.63, wherein the glycerin is in an amount of about 35% by wt. of
the composition. [0077] 1.65 The composition of 1.63, wherein the
glycerin is in an amount of about 26% by wt. of the composition.
[0078] 1.66 Any of the preceding compositions further comprising
sorbitol, wherein the sorbitol is in a total amount of 10-40%
(e.g., about 23%). [0079] 1.67 The composition of 1.66, wherein the
sorbitol is in an amount of about 13% by wt. of the composition.
[0080] 1.68 The composition of any of 1.63-1.67, wherein the
glycerin is an amount of about 26% by wt., and the sorbitol is in
an amount of about 13% by wt. [0081] 1.69 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). [0082] 1.70 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. [0083] 1.71 Any of the
preceding compositions wherein the zinc citrate is about 0.5 wt. %.
[0084] 1.72. Any of the preceding compositions wherein the zinc
oxide is about 1.0 wt. %. [0085] 1.73 Any of the preceding
compositions where the zinc citrate is about 0.5 wt. % and the zinc
oxide is about 1.0 wt. %. [0086] 1.74 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. [0087] 1.75 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. %. [0088] 1.76 Any of the preceding compositions
wherein the benzyl alcohol is about 0.1 wt. %. [0089] 1.77 Any of
the preceding compositions wherein the benzyl alcohol is considered
a preservative. [0090] 1.78 Any of the preceding compositions
comprising polymer films. [0091] 1.79 Any of the preceding
compositions comprising flavoring, fragrance and/or coloring.
[0092] 1.80 The composition of 1.65, wherein the flavoring agent is
sodium saccharin, sucralose, or a mixture thereof. [0093] 1.81 Any
of the preceding compositions, wherein the composition comprises a
thickening agents selected from the group consisting of
carboxyvinyl polymers, xanthan gum, carrageenan, hydroxyethyl
cellulose and water soluble salts of cellulose ethers (e.g., sodium
carboxymethyl cellulose and sodium carboxymethyl hydroxyethyl
cellulose). [0094] 1.82 Any of the preceding compositions, wherein
the compositions comprises sodium carboxymethyl cellulose (e.g.,
from 0.5 wt. %-1.5 wt. %) [0095] 1.83 Any of the preceding
compositions comprising from 5%-40%, e.g., 10%-35%, e.g., about
15%, 25%, 30%, and 35% water. [0096] 1.84 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,
honokiol, catechol, methyl salicylate, epigallocatechin gallate,
epigailocatechin, 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 and zinc compounds, for example, Zinc Chloride, Zinc Lactate,
Zinc Sulfate, Zinc Oxide, 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 piperidine derivatives,
nicin preparations, chlorite salts; and mixtures of any of the
foregoing. [0097] 1.85 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,
anethole-dithiothione, and mixtures thereof. [0098] 1.86 Any of the
preceding compositions comprising a whitening agent.
[0099] 1.87 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. [0100] 1.88 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.
[0101] 1.89 Any of the preceding compositions further comprising an
agent that interferes with or prevents bacterial attachment, e.g.,
ethyl lauryl arginate (ELA) or chitosan. [0102] 1.90 Any of the
preceding compositions comprising: [0103] a. about 1.0% zinc oxide
[0104] b. about 0.5% zinc citrate [0105] c. about 1.5% L-arginine
[0106] d. about 0.32% sodium fluoride; [0107] e. about 3 wt. % to
15 wt. % silica abrasive which exhibits an acid pH when measured as
an aqueous slurry (e.g., prophy silica) (e.g., Sylodent 783) [0108]
1.91 Any of the preceding compositions comprising: [0109] a. about
1.0% zinc oxide [0110] b. about 0.5% zinc citrate [0111] c. about
5% L-arginine [0112] d. about 0.32% sodium fluoride [0113] e. about
10 wt. % to 15 wt. % silica abrasive which exhibits an acid pH when
measured as an aqueous slurry (e.g., prophy silica) (e.g., Sylodent
783), and [0114] 1.92 Any of the preceding compositions comprising:
[0115] a. about 1.0% zinc oxide [0116] b. about 0.5% zinc citrate
[0117] c. about 5% L-arginine [0118] d. about 0.32% sodium
fluoride; [0119] e. about 3 wt. % to 15 wt. % silica abrasive which
exhibits an acid pH when measured as an aqueous slurry. (e.g.,
prophy silica) (e.g., Sylodent 783) [0120] 1.93 Any of the
preceding compositions comprising a silica, wherein the silica is
Zeodent 114. [0121] 1.94 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. [0122] 1.95 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. [0123] 1.96 A
composition obtained or obtainable by combining the ingredients as
set forth in any of the preceding compositions. [0124] 1.97 A
composition obtained or obtainable by combining the ingredients as
set forth in any of the preceding compositions. [0125] 1.98 A
composition for use as set for in any of the preceding
compositions.
[0126] 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 (e.g.,
any of Composition 1.0 et seq) to the oral cavity of a subject in
need thereof, e.g., [0127] i. a method to reduce or inhibit
formation of dental caries, reduce, repair or inhibit early enamel
lesions, e.g., as detected by quantitative light-induced
fluorescence (QLF) or electrical caries measurement (ECM), [0128]
ii. reduce or inhibit demineralization and promote remineralization
of the teeth, [0129] iii. reduce hypersensitivity of the teeth,
[0130] iv. reduce or inhibit gingivitis, [0131] v. promote healing
of sores or cuts in the mouth, [0132] vi. reduce levels of acid
producing bacteria, [0133] vii. to increase relative levels of
arginolytic bacteria, [0134] viii. inhibit microbial bio film
formation in the oral cavity, [0135] ix. raise and/or maintain
plaque pH at levels of at leas 5.5 following sugar challenge,
[0136] x. reduce plaque accumulation, [0137] xi. treat dry mouth,
[0138] xii. enhance systemic health, including cardiovascular
health, e.g., by reducing potential for systemic infection via the
oral tissues, [0139] xiii. Whiten teeth, [0140] xiv. reduce erosion
of the teeth, [0141] xv. immunize (or protect) the teeth against
cariogenic bacteria and their effects, and/or [0142] xvi. clean the
teeth and oral cavity.
[0143] The invention further comprises the use of sodium
bicarbonate, sodium methyl cocoyl taurate (tauranol),
methylisothiazolinone, 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
[0144] As used herein, the terms "oral composition" and "oral care
composition" refer to 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 intended for
systemic administration of particular therapeutic agents or
intentionally swallowed; but rather, is 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.
[0145] 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 is provided as a dual phase composition, wherein
individual compositions are combined when dispensed from a
separated compartment dispenser.
Basic Amino Acids
[0146] 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.
[0147] 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.
[0148] In certain embodiments, the basic amino acid is arginine,
for example, L-arginine, or a salt thereof.
[0149] The compositions of the invention 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 which 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
[0150] The oral care compositions 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
[0151] 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 coca-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(CH2).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-.sub.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%.
[0152] 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.
[0153] 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 polaxamers (e.g., polaxamer 407),
polysorbates (e.g., polysorbate 20), polyoxyl hydrogenated castor
oils (e.g., polyoxyl 40 hydrogenated castor oil), and mixtures
thereof.
[0154] 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.
[0155] Illustrative zwitterionic surfactants of Composition 1.0, et
seq., that can be used in the compositions of the invention include
derivatives of aliphatic quaternary ammonium, phosphonium and
sulfonium compounds 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 carboxy, sulfonate,
sulfate, phosphate or phosphonate). The surfactant or mixtures of
compatible surfactants can be present in the compositions of the
present invention 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
[0156] 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.
[0157] The flavoring agent is incorporated in the oral composition
at a concentration of 0.01 to 1% by weight.
Chelating and Anti-Calculus Agents
[0158] The oral care compositions of the invention (e.g.,
Composition 1.0 et seq) 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.
[0159] 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 the effect of water activity.
Polymers
[0160] The oral care compositions of the invention (e.g.,
Composition 1.0, et seq.) 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.
[0161] 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.
[0162] 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-chlorosorbic, 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.
[0163] 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 acrylamnidoalykane 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.
[0164] Another useful class of polymeric agents includes polyamine
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.
[0165] 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
[0166] Generally, the inclusion of abrasives in dentifrice
formulations is necessary for effective cleaning of teeth by
brushing. It has been determined that by including an abrasive
silica having an acid pH in the composition, compositions of
enhanced viscosity stability are obtained. Prophy silica available
from Grace, offered as Sylodent.TM., can be used with various
embodiments of the present invention (e.g., Composition 1.0 et
seq).
[0167] The acidic silica abrasive is included in the dentifrice
components at a concentration of about 2 to about 35% by weight;
about 3 to about 20% by weight, about 3 to about 15% by weight,
about 10 to about 15% by weight. For example, the acidic silica
abrasive may be present in an amount selected from 2 wt. %, 3 wt.
%, 4% wt. %, 5 wt. %, 6 wt. %, 7 wt. %, 8 wt. %, 9 wt. %, 10 wt. %,
11 wt. %, 12 wt. %, 13 wt. %, 14 wt. %, 15 wt. %, 16 wt. %, 17 wt.
%, 18 wt. %, 19 wt. %, 20 wt. %.
[0168] A commercially available acidic silica abrasive is Sylodent
783 available from W. R. Grace & Company, Baltimore, Md.
Sylodent 783 has a pH of 3.4-4.2 when measured as a 5% by weight
slurry in water. For use in the present invention, the silica
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.
[0169] The composition may also include any silica suitable for
oral care compositions, 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.
[0170] The invention may also comprise a commercially available
cleaning silica in certain embodiments of the invention (e.g., any
of Composition 1.0, et seq). Zeodent 114 offered by J.M. Huber
Finland Oy Telakkatie 5 FIN-49460 Hamina, is one such commercially
available silica.
Water
[0171] 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
[0172] Within certain embodiments of the oral compositions (e.g.,
Composition 1.0 et seq), it is also desirable to incorporate a
humectant 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.
[0173] 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 glycerin and
sorbitol may be used in certain embodiments as the humectant
component of the compositions herein.
[0174] The present invention in its method aspect involves applying
to the oral cavity a safe and effective amount of the compositions
described herein.
[0175] 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.
[0176] In some embodiments, the present invention provides an oral
care composition comprising: a basic amino acid in free or salt
wherein the amino acid is selected from arginine, lysine, and a
combination thereof; a combination of zinc ion sources; and a
thickening system comprising: from about 0.1 wt. % to about 2 wt. %
of a nonionic cellulose ether; and from about 0.25 wt. % to about 1
wt. % of a polysaccharide gum. In other embodiments, the present
invention provides an oral care composition comprising: a basic
amino acid in free or salt wherein the amino acid is selected from
arginine, lysine, and a combination thereof; a combination of zinc
ion sources; and a thickening system comprising: from about 0.1 wt.
% to about 1 wt. % of a nonionic cellulose ether; and from about
0.25 wt. % to about 1 wt. % of a polysaccharide gum.
[0177] Some embodiments provide compositions comprising a nonionic
cellulose ether having a molecular weight of from about 650,000 to
about 750,000. Other embodiments provide compositions comprising a
nonionic cellulose ether having a molecular weight of about
700,000. While other embodiments provide compositions comprising a
nonionic cellulose ether having a molecular weight of about
720,000.
[0178] In some embodiments, the nonionic cellulose ether comprises
hydroxyethylcellulose. In further embodiments, the oral care
composition comprises from about 0.1 wt. % to about 0.75 wt. % of
hydroxyethylcellulose. Still further embodiments provide oral care
compositions comprising from about 0.1 wt. % to about 0.5 wt. % of
hydroxyethylcellulose. Yet other embodiments provide oral care
compositions comprising about 0.1 wt. %, about 0.15 wt. %, about
0.2 wt. %, about 0.25 wt. %, about 0.3 wt. %, about 0.35 wt. %,
about 0.4 wt. %, about 0.45 wt. % or about 0.5 wt. % of
hydroxyethylcellulose. Certain embodiments provide oral care
compositions comprising 0.1 wt. %, 0.15 wt. %, 0.2 wt. %, 0.25 wt.
%, 0.3 wt. %, 0.35 wt. %, 0.4 wt. %, 0.45 wt. % or 0.5 wt. % of
hydroxyethylcellulose.
[0179] In some embodiments, the hydroxyethylcellulose has a
viscosity, measured at 2% in water at 25.degree. C., of about 4500
to about 7500 cps. In some embodiments, the hydroxyethylcellulose
has a viscosity, measured at 2% in water at 25.degree. C., of about
4500 to about 6500 cps. In some embodiments, the
hydroxyethylcellulose has a viscosity, measured at 2% in water at
25.degree. C., of about 6000 to about 7500 cps.
[0180] In some embodiments, the hydroxyethylcellulose having a
viscosity, measured at 2% in water at 25.degree. C., of about 4500
to about 6500, is present in an amount of from about 0.1 wt. % to
about 1 wt. %, of the oral care composition. In some embodiments,
the hydroxyethylcellulose having a viscosity, measured at 2% in
water at 25.degree. C., of from about 4500 to about 6500 cps, is
present in an amount of from about 0.1 wt. % to about 0.5 wt. %, of
the total composition. In some embodiments, the
hydroxyethylcellulose having a viscosity, measured at 2% in water
at 25.degree. C., of about 4500 to about 6500 cps, is present in an
amount of about 0.1 wt. %, about 0.15 wt. %, about 0.2 wt. %, about
0.25 wt. %, about 0.3 wt. %, about 0.35 wt. %, about 0.4 wt. %,
about 0.45 wt. % or about 0.5 wt. % of the oral care
composition.
[0181] Some embodiments provide oral care compositions comprising
hydroxyethylcellulose having a molecular weight of about 700,000,
e.g. 720,000, in the amount of from about 0.1 wt. % to about 0.5
wt. %, of the oral care composition. Other embodiments provide oral
care compositions comprising 0.05 wt. %, 0.1 wt. %, 0.15 wt. %, 0.2
wt. %, 0.25 wt. %, 0.3 wt. %, 0.35 wt. %, 0.4 wt. %, 0.45 wt. % or
0.5 wt. % of a hydroxyethylcellulose having a molecular weight of
about 700,000, e.g. 720,000.
[0182] Some embodiments provide oral care compositions comprising
hydroxyethylcellulose having a molecular weight of about 350,000,
in the amount of from about 0.1 wt. % to about 0.5 wt. %, of the
oral care composition. Other embodiments provide oral care
compositions comprising 0.05 wt. %, 0.1 wt. %, 0.15 wt. %, 0.2 wt.
%, 0.25 wt. %, 0.3 wt. %, 0.35 wt. %, 0.4 wt. %, 0.45 wt. % or 0.5
wt. % of a hydroxyethylcellulose having a molecular weight of about
350,000.
[0183] In some embodiments, the polysaccharide gum is xanthan gum.
In further embodiments, the oral care composition comprises from
about 0.3 wt. % to about 1 wt. % of xanthan gum. In other
embodiments, the oral care composition comprises from about 0.4 wt.
% to about 1 wt. % of xanthan gum. In some embodiments, the oral
care composition comprises from about 0.5 wt. % to about 1 wt. % of
xanthan gum. Yet other embodiments provide oral care compositions
comprising from about 0.6 wt. % to about 0.9 wt. % of xanthan gum.
In further embodiments, the oral care composition comprises from
about 0.7 wt. % to about 0.8 wt. % of xanthan gum. Still further
embodiments provide oral care compositions comprising about 0.1 wt.
%, 0.2 wt. %, 0.3 wt. %, 0.4 wt. % 0.5 wt. %, 0.6 wt. %, 0.7 wt. %,
0.8 wt. %, 0.9 wt. % or 1 wt. %, of a polysaccharide gum, e.g.
xanthan gum.
[0184] In some embodiments, the present invention provides an oral
care composition comprising: a basic amino acid in free or salt
wherein the amino acid is selected from arginine, lysine, and a
combination thereof; a combination of zinc ion sources; and a
thickening system comprising: from about 0.1 wt. % to about 0.5 wt.
% of a nonionic cellulose ether; and from about 0.5 wt. % to about
0.9 wt. % of a polysaccharide gum. In some embodiments, the present
invention provides an oral care composition comprising: a basic
amino acid in free or salt wherein the amino acid is selected from
arginine, lysine, and a combination thereof; a combination of zinc
ion sources; and a thickening system comprising: from about 0.1 wt.
% to about 0.3 wt. % of a nonionic cellulose ether; and from about
0.7 wt. % to about 0.8 wt. % of a polysaccharide gum.
[0185] In some embodiments, the thickening system further comprises
from about 5 wt. % to about 10 wt. % silica. In some embodiments,
the thickening system comprises from about 0.5 wt. % to about 15
wt. % of the oral care composition.
[0186] In certain embodiments, the hydroxyethylcellulose and the
polysaccharide gum are present in a weight ratio of from about 1:1
to about 1:10, in other embodiments, the hydroxyethylcellulose and
the polysaccharide gum are present in a weight ratio of from about
1:2 to about 1:9. Yet other embodiments provide compositions
wherein the hydroxyethylcellulose and the polysaccharide gum are
present in a weight ratio of from about 1:3 to about 1:7.
[0187] In some embodiments, the oral care composition further
comprises a fluoride ion source selected from sodium fluoride,
sodium monofluorophosphate, and stannous fluoride.
[0188] In some embodiments, the oral care composition comprises
about 1.0 wt. % zinc oxide; about 0.5 wt. % zinc citrate; about 1.5
wt. % L-arginine; from about 0.3 wt. % to about 1 wt. % of xanthan
gum; and from about 0.1 wt. % to about 1 wt. % of
hydroxyethylcellulose. Some embodiments comprise from about 0.6 wt.
% to about 0.9 wt. % of xanthan gum. Some embodiments comprise from
about 0.7 wt. % to about 0.8 wt. % of xanthan gum.
[0189] In further embodiments, the oral care composition loses no
more than about 45% of its initial viscosity after one year. In
some embodiments, the oral care composition loses no more than
about 40% of its initial viscosity after one year. In other
embodiments, the oral care composition loses no more than about 35%
of its initial viscosity after one year, In yet other embodiments,
the oral care composition loses no more than about 30% of its
initial viscosity after one year. In some embodiments, the oral
care composition loses no more than about 25%, 24%, 23%, 22%, 21%
or 20% of its initial viscosity after one year.
[0190] In some embodiments, the oral care composition has a G'/G''
ratio of greater than 0.5. In some embodiments, the oral care
composition has a G'/G'' ratio of greater than 0.75. In some
embodiments, the oral care composition has a G'/G'' ratio of
greater than 1. In some embodiments, the oral care composition has
a G'/G'' ratio of greater than 1.5. In some embodiments, the oral
care composition has a G'/G'' ratio of less than 2. In some
embodiments, the oral care composition has a G'/G'' ratio of less
than 1.5. In some embodiments, the oral care composition has a
G'/G'' ratio of less than 1. Methods of quantifying the elastic
modulus (G'), the loss modulus (G'') and G'/G'' ratios are
described, for example, in WO 2013/089734 A1, the contents of which
are hereby incorporated herein by reference in their entirety.
[0191] In some embodiments, the compositions of the present
invention provide a consistency, K, less than 30 Pa*s.sup.n. In
some embodiments, the compositions of the present invention provide
a flow index, n, of greater than 0.3. In some embodiments, the
compositions of the present invention provide a consistency, K,
less than 30 Pa*s.sup.n and a flow index, n, of greater than 0.3.
In some embodiments, the compositions of the present invention
provide a consistency, K, less than 30 Pa*s.sup.n; a flow index, n,
of greater than 0.3; and a G'/G'' ratio of less than 2. In some
embodiments, the compositions of the present invention provide a
flow index, n, of greater than 0.3; and a G'/G'' ratio of less than
2. In some embodiments, the compositions of the present invention
provide a consistency, K, less than 30 Pa*s.sup.n; and a G'/G''
ratio of less than 2.
[0192] In some embodiments, the oral care compositions of the
present invention provide a yield stress greater than 20 Pa. In
some embodiments, the oral care compositions of the present
invention provide a yield stress greater than 25 Pa. In other
embodiments, the oral care compositions of the present invention
provide a yield stress greater than 30 Pa. Yet further embodiments,
provide oral care compositions that demonstrate a yield stress
greater than 35 Pa. In some embodiments, the oral care compositions
of the present invention provide a yield stress greater than 40
Pa.
[0193] Some embodiments provide compositions having a drainage time
of less than about 10 minutes when draining 3 kg of an intermediate
product (gel pre-mix) from a tank of 21 cm in diameter through a 1
mm wide bottom opening at negative pressure of -0.95 bar. Other
embodiments provide compositions having a drainage time of less
than about 9 minutes. Further embodiments provide compositions
having a drainage time of less than about 8 minutes. Yet other
embodiments provide compositions having a drainage time of less
than about 7 minutes, 6 minutes, 5 minutes, 4 minutes, 3 minutes, 2
minutes or 1 minute.
[0194] Some embodiments provide compositions demonstrating less
than 300 grams of left-overs. Other embodiments provide
compositions demonstrating less than 275 grams of left-overs.
Further embodiments provide compositions demonstrating less than
250 grams of left-overs. Yet other embodiments provide compositions
demonstrating less than 225 grams of left-overs. Still further
embodiments provide compositions demonstrating less than 200 grams
of left-overs. While other embodiments provide compositions
demonstrating less than 175 grams, 150 grams, 125 grams, 100 grams
or 50 grams of left-overs. Certain embodiments provide compositions
demonstrating a drainage time of less than 10 minutes and less than
225 grams of left-overs.
[0195] 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.
[0196] 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.
EXAMPLES
Example 1
[0197] The examples herein detail how the viscosity over time for a
composition which exhibits a problem of rapid reduction in
viscosity (Run A), is compared to five compositions which show the
stabilized viscosity provided by the invention (Compositions 1-5 in
Table 1).
[0198] Viscosity is measured on a Brookfield HADV2 viscometer using
a V74 vane spindle. This viscometer applies a user-controlled
angular velocity to the spindle, typically measured in rotations
per second (RPM), and reports torque on the shaft of the spindle.
Viscosity is then calculated from RPM and torque as explained in
the Brookfield Manual (Operating Instructions) using too conversion
parameters SRC (shear rate constant) and SMC (spindle multiplier
constant). The conversion parameters are defined as follows:
SMC=290, SRC=0.2723. The test is performed at room temperature, and
varies between 22 and 25.degree. C. During the test, RPM of the
spindle is swept from 200 to 0.5 in 12 steps, 10 seconds per step.
The viscosity reading reported is taken at RPM=1.
[0199] Compositions containing zinc oxide, zinc citrate, arginine
and a fluoride source are prepared as described in Table 1, below.
All compositions are formulated to provide a 10% pH of 8-8.5 using
0-0.35% phosphoric acid. The composition identified as Run A does
not contain a silica abrasive which exhibits an acid pH when
measured as an aqueous slurry. The compositions identified as
Compositions 1-5 in Table 1 (below) contain a silica abrasive which
exhibits an acid pH (Prophy Silica-Sylodent 783) when measured as
an aqueous slurry in varying amounts, as detailed below.
TABLE-US-00001 TABLE 1 Dentifrice Formulations Experiment ID
INGREDIENTS Run A Composition 1 Composition 2 Composition 3
Composition 4 Composition 5 99.0%-101.0% 35 35 35 35 35 35 GLYCERIN
- USP, EP VEG DEMINERALIZED Q.S. Q.S. Q.S. Q.S. Q.S. Q.S. WATER
PROPHY SILICA 0 15 10 5 5 3 (SYLODENT 783) ABRASIVES (e.g., 20 5 10
15 15 17 includes Abrasive silcas, High Cleaning Silicas) SILICA-
6.5 7 7 7 7 7 THICKENER ANIONIC 2 2 2 2 2 2 SURFACTANT L-ARGININE
1.5 1.5 1.5 1.5 1.5 1.5 AMPHOTERIC 1.25 1.25 1.25 1.25 1.25 1.25
SURFACTANT NON-IONIC 0.75 0.75 0.75 0.75 0.75 0.75 SURFACTANT ZINC
OXIDE 1 1 1 1 1 1 POLYMER 1 1.3 1.3 1.3 1.3 1.3 COLORANT 0.75 0.75
0.75 0.75 0.75 0.75 ALKALI 0.5 0.5 0.5 0.5 0.5 0.5 PHOSPHATE SALT
ZINC CITRATE 0.5 0.5 0.5 0.5 0.5 0.5 TRIHYDRATE PRESERVATIVE 0.4
0.4 0.4 0.4 0.4 0.4 SODIUM 0.32 0.32 0.32 0.32 0.32 0.32 FLUORIDE -
USP, EP 85% SYRUPY 0.35 0 0 0 0 0 PHOSPHORIC ACID - FOOD GRADE
FLAVORING AGENT 2 2 2 2 1.82 1.52 TOTAL COMPONENTS 100 100 100 100
100 100
[0200] The composition identified as Run A displays an initial
viscosity which is initially 500,000 cps to 600,00 cps high, but
decreases to under 400,000 cps in 2 weeks, and under 200,000 cps at
6 weeks. Surprisingly, the compositions containing a silica
abrasive which exhibits an acid pH (Prophy Silica Sylodent 783)
when measured as an aqueous slurry, Compositions 1 to 5 in Table 1
(above), eliminate this undesirable characteristic and instead
produce viscosities that are stable or increase over time (See,
Table 2 below).
TABLE-US-00002 TABLE 2 Viscosity data Experiment ID Compo- Compo-
Compo- Compo- Compo- Run A sition 1 sition 2 sition 3 sition 4
sition 5 Time Viscosity (cps) 0 491040 363489 1 d.sup. 539119
211912 300155 272475 5 d.sup. 601597 309816 1 wk 627362 288561
383245 371651 2 wk 433485 340733 328495 403212 364565 3 wk 343310
314325 334292 4 wk 224794 395483 304019 430909 423823 5 wk 375515
338801 322698 6 wk 193233 376804 344598 334292 406432 442503 7 wk
334292 9 wk 387753 10 wk 351039 364565 11 wk 158451 373583 381956
12 wk 405788 357480 13 wk 405788 398059 393550
[0201] Upon further investigation, it was found that the silica
abrasive which exhibits an acid pH when measured as an aqueous
slurry silica is acidic (pH 3.4-4.2) does not require phosphoric
acid to adjust the product pH. Other abrasive silicas and high
cleaning silicas are about neutral in pH (pH 7-8) and thus, require
phosphoric acid for pH adjustment.
TABLE-US-00003 TABLE 3 Compo- Compo- Compo- sition 6 sition 7
sition 8 Demineralized Water Q.S. Q.S. Q.S. Glycerin - 99.5% 35 35
35 Polymer 1.2 1.2 1.2 Zinc Oxide 1 1 1 Zinc Citrate 0.5 0.5 0.5
Alkali Phosphate Salt 0.5 0.5 0.5 Flavoring agent 1.82 1.82 1.82
Sodium Fluoride 0.32 0.32 0.32 Colorant 0.75 0.75 0.75 L-Arginine
1.5 1.5 1.5 Non-Ionic Surfactant 0.5 0.5 0.5 Abrasives (e.g., 8 10
12 includes Abrasive Silcas, High Cleaning Silicas) Prophy silica
(Sylodent 783) 7 5 3 Silica - thickener 7 7 8.5 Preservative 0.4
0.4 0.4 Anionic Surfactant 5.7 5.7 5.7 Amphoteric Surfactant 1.25
1.25 1.25 Total Components 100 100 100
[0202] Upon further investigation, when phosphoric acid is removed
from further formulations (Compositions 6-8 in Table 3, above),
they demonstrate improvement in viscosity stability, and this
viscosity trend remained relatively stable from day 1 to 4 weeks
when tested at: room temperature, 40.degree. C. and 49.degree. C.
The data is further detailed in Table 4 below.
TABLE-US-00004 TABLE 4 Composition 6 Composition 7 Composition 8
Viscosity, Viscosity, Viscosity, 10.sup.3 cps 10.sup.3 cps 10.sup.3
cps 40.degree. 49.degree. 40.degree. 49.degree. 40.degree.
49.degree. RT C. C. RT C. C. RT C. C. 0 471 324 336 0.14 370 197
268 1 363 418 390 200 227 258 230 256 263 2 360 430 440 201 243 269
220 250 258 3 325 205 246 245 228 277 274 4 314 412 385 224 253 253
227 268 272 6 327 218 233
Example 2
[0203] Table 5 (below) describes the formulas of three exemplary
compositions of the present invention (Compositions 9, 10 and 11)
and a comparative example (Comparative Example I).
TABLE-US-00005 TABLE 5 Compo- Compo- Compo- Comparative sition 9
sition 10 sition 11 Example I Ingredient Wt % GLYCERIN 35.00000
26.00000 26.00000 35.00000 SORBITOL -- 13.00000 13.00000 -- WATER
30.90474 27.82474 27.62474 30.84874 SILICA ABRASIVE 1 10.00000
10.00000 10.00000 10.00000 SILICA-THICKENER 7.00000 6.00000 6.00000
7.00000 SILICA ABRASIVE 2 5.00000 5.00000 5.00000 5.00000 Na-LAURYL
2.10526 2.10526 2.10526 2.10526 SULFATE GRANULES Flavor 1.50000
1.50000 1.50000 1.50000 L-ARGININE 1.50000 1.50000 1.50000 1.50000
COCAMIDOPROPYL 1.25000 1.25000 1.25000 1.25000 BETAINE ZINC OXIDE
1.00000 1.00000 1.00000 1.00000 TITANIUM DIOXIDE 0.75000 0.75000
0.75000 -- XANTHAN GUM 0.60000 0.30000 0.30000 0.40000 SODIUM CMC
-- -- -- 1.10000 HYDROXYETHYL- 0.50000 0.80000 1.00000 -- CELLULOSE
(HEC)* TETRASODIUM 0.50000 0.50000 0.50000 0.50000 PYROPHOSPHATE
ZINC CITRATE 0.50000 0.50000 0.50000 0.50000 TRIHYDRATE POLOXAMER
407 0.50000 0.50000 0.50000 0.50000 BENZYL ALCOHOL 0.40000 0.40000
0.40000 0.40000 85% PHOSPHORIC 0.35000 0.35000 0.35000 0.35000 ACID
SODIUM 0.32000 0.32000 0.32000 0.32000 FLUORIDE - USP, EP
Sweeteners 0.32000 0.40000 0.40000 0.42000 Additional Colorants --
-- -- 0.30600 *HEC having a viscosity, measured at 2% in water at
25.degree. C., of 6000 to 7500 cps
Example 3
[0204] Table 6 (below) describes the results of viscosity and
static yield stress evaluations preformed on an exemplary
composition of the present invention and a reference formula.
[0205] Viscosity and Yield Stress are measured on a Brookfield
HADV2 viscometer using V74 vane spindle 1.176 cm in length and
0.589 cm in diameter. This viscometer applies a user-controlled
angular velocity to the spindle, typically measured in rotations
per second (RPM), and reports torque, T %, measured in the
percentage of the maximum total torque on the shaft of the spindle.
The torque, T, measured in SI units, N*m, is related to T % as
reported by the above mentioned viscometer as T=1.437*10.sup.-5*T
%.
[0206] The tests are performed at room temperature (22 to
25.degree. C.). During the test 0.5 RPM of the spindle is first
rotated for 400 sec and then RPM is swept from 0.5 to 200 and back
to 0.5 in 12 logarithmical steps each way, 10 seconds per step. The
viscosity reading is taken at RPM=1 on the decreasing RPM sweep.
Viscosity is then calculated from RPM and T as explained in the
Brookfield Manual (Operating Instructions) using two conversion
parameters SRC (shear rate constant) and SMC (spindle multiplier
constant). In this case, the conversion parameters are defined as
follows: SMC=290, SRC=0.27.
[0207] Static Yield Stress (YS) is calculated as a fitting
parameter by fitting experimental T(RPM) dependence on increasing
RPM sweep with the theoretical one which was calculated assuming
the so-called Casson constitutive equation and is implicitly given
by the following equation:
RPM = 15 .pi. .intg. YS SW ( S n - YS n ) 1 / n HSV * S dS
##EQU00001##
where HSV (high-shear viscosity limit) is another fitting
parameter, n=0.3, and SW is the stress on the imaginary wall
encompassing the vane which is estimated as follows:
SW = 2 T .pi. LD 2 ( 1 + D 3 L ) ##EQU00002##
T(RPM) is calculated from these two equations numerically. Only
data points with RPM from 5 to 200 and T % between 3 and 100 are
fitted.
TABLE-US-00006 Days after Viscosity at Static Yield Manufacturing 1
RPM (cP) Stress (Pa) Comparative Example I 1 442984 152 21 277573
161 30 202798 133 37 203931 99 90 167110 94 365 226817 40
Composition 11 1 609528 161 14 527956 184 44 425990 187 75 431088
199 290 493401 250
[0208] The data described in Table 6 (above) demonstrates the
unexpected stabilizing effects provided by the inventive thickening
systems of the present invention. Importantly, these effects are
observed over an extended period of time, rather than being
transient in nature.
Example 4
[0209] Table 7 (below) describes the formulas of two additional
compositions of the present invention (Compositions 12 and 13) and
another comparative formula (Comparative Example II.
TABLE-US-00007 TABLE 7 Compo- Compo- Comparative sition 12 sition
13 Example II Ingredient Wt % GLYCERIN -- 26.000000 35.000000
SORBITOL 39.000000 13.000000 -- SUCRALOSE -- -- 0.020000 WATER
27.824737 28.244737 30.848737 SODIUM SACCHARIN 0.400000 0.400000
0.400000 ABRASIVE SILICA 10.000000 10.000000 10.000000
SILICA-THICKENER 6.000000 6.000000 7.000000 AMORPHOUS SILICA
5.000000 5.000000 5.000000 Na-LAURYL 2.105263 2.105263 2.105263
SULFATE GRANULES Flavor 1.500000 1.500000 1.500000 L-ARGININE
1.500000 1.500000 1.500000 COCAMIDOPROPYL 1.250000 1.250000
1.250000 BETAINE ZINC OXIDE 1.000000 1.000000 1.000000 TITANIUM
DIOXIDE 0.750000 -- 0.300000 XANTHAN GUM 0.300000 0.300000 0.400000
SODIUM CMC -- -- 1.100000 HYDROXYETHYL 0.800000 1.000000 --
CELLULOSE (HEC)* TETRASODIUM 0.500000 0.500000 0.500000
PYROPHOSPHATE ZINC CITRATE 0.500000 0.500000 0.500000 TRIHYDRATE
POLOXAMER 407 0.500000 0.500000 0.500000 BENZYL ALCOHOL 0.400000
0.400000 0.400000 85% PHOSPHORIC ACID 0.350000 0.350000 0.350000
SODIUM 0.320000 0.320000 0.320000 FLUORIDE - USP, EP Additional
Colorants -- 0.130000 0.006000 *HEC having a viscosity at 2% in
water, of 6000 to 7500 cps at 25.degree. C.
Example 5
[0210] Table 8 (below) describes the percentage change in viscosity
loss and loss of static yield stress for two exemplary compositions
of the present invention (Compositions 12 and 13) and a comparative
composition (Comparative Example II). Viscosity and Static Yield
Stress were calculated in accordance with the methods described in
Example 3 herein.
TABLE-US-00008 TABLE 8 Viscosity Loss Loss of Static Yield Stress
Composition (1 Year) (After 1 Year) Composition 12 19% Stable
Composition 13 21% Stable Comparative Example II 49% 73%
[0211] The data described in Table 8 (above) not only shows that
compositions of the present invention demonstrate less viscosity
loss and static yield stress loss than a comparative composition,
but it also demonstrates that the benefits are reproducible.
Example 6
[0212] Table 9 (below) describes another exemplary backbone for
oral care compositions of the present invention comprising--inter
alia--a basic amino acid in free or salt form (e.g. L-arginine);
and a combination of zinc ion sources.
TABLE-US-00009 TABLE 9 Ingredient Wt. % L-Arginine 1.50 Zinc
Citrate Trihydrate 0.50 Sodium Fluoride 0.32 Non-ionic surfactant
0.50 Alkali Phosphate salt 0.50 Zinc Oxide 1.00 Saccharin 0.40
Colorant 0.75 Silica Abrasives 15.00 Silica thickener 7.50 Anionic
surfactant 2.00 Flavoring agent 1.52 Preservative 0.40 Amphoteric
surfactant 1.25
[0213] Added to this backbone were the various combinations of
water, a nonionic cellulose ether (hydroxyethylcellulose [HEC]);
and a polysaccharide gum (xanthan gum), described in Table 10
(below).
TABLE-US-00010 TABLE 10 Water Glycerin Xanthan Gum HEC**
Composition Wt. % 14 32.78 32.78 0.3 1 15 33.03 33.03 0.3 0.5 16
32.83 32.83 0.2 1 17 32.86 32.86 0.35 0.8 18 32.91 32.91 0.45 0.6
19 32.71 32.71 0.25 1.2 20 33.08 33.08 0.55 0.15 21 32.93 32.93 0.5
0.5 22 32.88 32.88 0.5 0.6 23 32.91 32.91 0.55 0.5 **HEC having a
viscosity, measured at 2% in water at 25.degree. C., of 4500 to
6500 cps
[0214] Toothpastes were prepared from each of the combinations
described in Table 10 (above) by first creating a gel comprising
water, glycerin, xanthan gum and hydroxyethylcellulose (HEC); and
then combining each gel with the remaining components (see Table 9)
in a Ross double planetary mixer. The rheological profiles of both
the gel pre-mixes and the toothpaste end products are
evaluated.
[0215] Table 11 (below) describes exemplary gel pre-mixes of the
present invention. Although not shown in Table 11, the gel
pre-mixes also included water and glycerin in equal amounts.
TABLE-US-00011 TABLE 11 Xanthan Gum HEC** Composition Wt. % A 0.9
0.2 B 0.7 0.35 C 0.6 0.5 D 0.55 0.6 E 0.5 0.7 F 0.45 0.8 G 0.7 0.7
H 0.8 0.5 I 1 0.3 J 1.2 0.15 K 1.1 0 L 0.9 0 M 1.05 0.15 N 0.9 0.1
O 0.85 0.3 P 0.9 0.4 Q 0.7 0.5 R 0.45 0.35 S 0.3 0.4 T 0.25 1.2 U
0.4 0.6 V 0.55 0.15 W 0.68 0.25 X 0.6 0.45 **HEC having a
viscosity, measured at 2% in water at 25.degree. C., of 4500 to
6500 cps
Example 7
[0216] The processability of the gel pre-mixes described in Table
11 (above) evaluated by flowing a sample gel through a gel tank
exposed to negative pressure (at room temperature), and
characterizing each sample in terms of "drainage time" and
"left-overs". In these experiments 3 kg of the gel is being drained
from a tank of 21 cm in diameter through a 1 mm wide bottom opening
at negative pressure of (-)0.95 bar, "Drainage time" is defined as
the time elapsed between the start of the flow from the inlet and
the time at which air begins to enter the outlet (at the bottom) of
the gel tank. The material remaining in the gel tank is collected
and weighed to determine "left-overs". The results of these
evaluations are described in Table 12 (below)
TABLE-US-00012 TABLE 12 Composition Left-overs (g) Drainage Time
(min) A 473 24 B 494 13 C 335 38.5 D 341 45 E 846 65 F 765 85 G
1062.5 78 H 533 60 I 607 40 J 879 48 K 642 13 L 384 8.5 M 637 28 N
409.5 15.5 O 474 33 P 591 46 Q 370 33 R 128 13 S 92.6 4.5 T 1106
n/a U 347 28 V 101 2
Example 8
[0217] Static Yield Stress (YS) of toothpastes prepared by adding
the combinations described in Table 10 (above) to the backbone
described in Table 9 (above) was calculated as follows.
Measurements are performed on ARG2 rheometer by TA Instrument using
a cylindrical cup and vane upper geometry. The measurements were
performed in the same containers, in which the samples were aged.
Those were standard 50 cc centrifuge tubes, available from VWR,
into which the samples were placed at the time of preparation. Then
the samples were consolidated by centrifuging at low rotations in
the centrifuge so as to remove air pockets and aged directly in
these tubes at room temperature (RT) or at 49.degree. C. for up to
2 months. Before the measurements the heated tubes were allowed to
cool for 2 hours at RT and then inserted directly into the cup of
the rheometer. To avoid the tubes mobility in the cup, they were
wrapped with a thin layer of tape. The vane was inserted into the
tubes and samples measured directly inside them. The measurement
procedure closely mimicked the one described above for Brookfield
viscometer, i.e., a constant shear rate of 0.05 sec.sup.-1 was
applied for 400 sec and followed by shear rate sweeps up and down
from 0.1 to 30 sec.sup.-1. Here shear rate is calculated from
angular velocity of the vane, .OMEGA., following TA instruments
conventions as follows:
S = 1 + k 2 1 - k 2 .OMEGA. ##EQU00003##
where k is the ratio of the diameter of the vane to the diameter of
the tube. Torque, T, on the shaft of the vane was measured. Yield
stress was calculated by fitting T(.OMEGA.) with the theoretical
function calculated assuming Casson constitutive equation and
implicitly given by the following equation:
.OMEGA. = 1 2 .intg. SW 0 SW ( S n - YS n ) 1 / n HSV * S dS
##EQU00004##
where HSV (high-shear viscosity limit) is another fitting
parameter, n=0.2, and SW is the stress on the imaginary wall
encompassing the vane which is estimated as follows:
SW = 2 T .pi. LD 2 ( 1 + D 3 L ) ##EQU00005##
and SW0 is the largest of the two values: YS and k.sup.2SW. Note
that the exponent n used to process these data is different from
the one used to process Brookfield data above (0.2 instead of 0.3)
to accommodate a wide range of shear rates as measured by a
rheometer.
[0218] The results are described below in Table 13.
TABLE-US-00013 TABLE 13 Composition YS (Pa) 14 40.2 15 9.5 16 17.6
17 30.3 18 39.1 19 35.8 20 24.9 21 27.7 22 33.2 23 39.1
[0219] 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.
[0220] 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.
[0221] 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.
* * * * *