U.S. patent application number 12/042870 was filed with the patent office on 2008-06-26 for dual component dental composition containing enzyme.
This patent application is currently assigned to COLGATE-PALMOLIVE COMPANY. Invention is credited to James G. Masters, Michael Prencipe, Malcolm Williams.
Application Number | 20080152601 12/042870 |
Document ID | / |
Family ID | 31976251 |
Filed Date | 2008-06-26 |
United States Patent
Application |
20080152601 |
Kind Code |
A1 |
Williams; Malcolm ; et
al. |
June 26, 2008 |
Dual Component Dental Composition Containing Enzyme
Abstract
A two component desensitizing dentifrice composition is
disclosed which comprises a first dentifrice component containing
an enzyme such as papain and a second dentifrice component
containing an ionic surfactant such as sodium lauryl sulfate, the
first and second dentifrice components being maintained separate
from the other until dispensed for application to teeth whereby
enzyme activity is maintained with improved dentifrice foaming
characteristics.
Inventors: |
Williams; Malcolm;
(Piscataway, NJ) ; Prencipe; Michael; (West
Windsor, NJ) ; Masters; James G.; (Ringoes,
NJ) |
Correspondence
Address: |
COLGATE-PALMOLIVE COMPANY
909 RIVER ROAD
PISCATAWAY
NJ
08855
US
|
Assignee: |
COLGATE-PALMOLIVE COMPANY
New York
NY
|
Family ID: |
31976251 |
Appl. No.: |
12/042870 |
Filed: |
March 5, 2008 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
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11191501 |
Jul 28, 2005 |
|
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12042870 |
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Current U.S.
Class: |
424/50 |
Current CPC
Class: |
A61K 8/66 20130101; A61K
2800/88 20130101; A61Q 11/00 20130101 |
Class at
Publication: |
424/50 |
International
Class: |
A61K 8/66 20060101
A61K008/66 |
Claims
1. A two component enzyme dentifrice composition comprising: a
first dentifrice component substantially free of an ionic
surfactant comprising an enzyme and a source of fluoride ions in an
orally acceptable vehicle; and a second dentifrice component
substantially free of the enzyme comprising an ionic surfactant in
an orally acceptable vehicle.
2. The composition of claim 1 wherein the enzyme is selected from
the group consisting of papain, glucoamylase, bromelain,
chymotripsin, ficin, alacalase, alpha-amylase, beta-amylase,
dextranase, mutanase, gastric lipase, pancreatic lipase, or
combinations thereof.
3. (canceled)
4. The composition of claim 1 wherein the ionic surfactant is an
anionic surfactant.
5. The composition of claim 4 wherein the anionic surfactant is
sodium lauryl sulfate.
6. The composition of claim 1 wherein the enzyme is present in the
first dentifrice component at a concentration of about 0.01 to
about 10% by weight.
7. The composition of claim 1 wherein the ionic surfactant is
present in the second component at a concentration of about 1 to
about 5% by weight.
8. A method for improving the foam characteristics of an oral care
composition containing an enzyme without substantial denaturation
of the enzyme which comprises: a. preparing a first dentifrice
component substantially free of an ionic surfactant comprising the
enzyme and a source of fluoride ions in an orally acceptable
vehicle b. preparing a second dentifrice component substantially
free of the enzyme comprising an ionic surfactant in an orally
acceptable vehicle, c. separately housing the first and second
components, d. dispensing the first and second components
simultaneously, e. combining the dispensed components; and f.
applying the combined components to the teeth whereby the enzyme
activity is substantially retained during application to the
teeth.
9. The method of claim 8 wherein the ionic surfactant is an anionic
surfactant.
10. The method of claim 9 wherein the anionic surfactant is sodium
lauryl sulfate.
11. The method of claim 8 wherein the enzyme is selected from the
group consisting of papain, glucoamylase bromelain, chymotripsin,
ficin, alacalase, alpha-amylase, beta-amylase, dextranase,
mutanase, gastric lipase, pancreatic lipase, or combinations
thereof.
12. (canceled)
13. The method of claim 8 wherein the enzyme is present in the
dentifrice component at a concentration of about 0.01 to about 10%
by weight.
14. The method of claim 7 wherein the ionic surfactant is present
in the dentifrice component at a concentration of about 1 to about
5% by weight.
15. The method of claim 8 wherein the first and second components
are housed in a common container and are separated from one another
by a wall integrally formed with the container which prevents
mixing of the components prior to being dispensed.
16. The composition of claim 1 wherein the first and second
components are maintained separate from each other until dispensed
and combined for application to teeth, wherein enzyme activity is
substantially retained during application of the combined
components to teeth during brushing.
17. The composition of claim 1 wherein the source of fluoride ions
is present in an amount sufficient to supply about 25 ppm to 5,000
ppm fluoride ions.
18. The composition of claim 1 wherein the source of fluoride ions
is an inorganic fluoride salt, soluble alkali metal salt, or
combinations thereof.
19. The composition of claim 1 wherein the source of fluoride ions
is selected from the group consisting of sodium fluoride, potassium
fluoride, sodium fluorosilicate, sodium monfluorophosphate,
ammonium fluorosilicate, stannous fluoride, and combinations
thereof.
20. The composition of claim 1 wherein the first dentifrice
component comprises an antibacterial agent.
21. The composition of claim 20 wherein the antibacterial agent is
a halogenated diphenyl ether.
22. The composition of claim 1 wherein the first dentifrice
component comprises an antitartar agent.
23. The composition of claim 22 wherein the antitartar agent is a
pyrophosphate salt.
24. The composition of claim 22 wherein the antitartar agent is an
dialkali metal pyrophosphate salt, a tetraalkali metal
pyrophosphate salt, or combinations thereof.
25. The composition of claim 1 wherein the second dentifrice
component comprises a source of fluoride ions.
26. The composition of claim 1 wherein the second dentifrice
component comprises an antibacterial agent.
27. The composition of claim 26 wherein the antibacterial agent is
a halogenated diphenyl ether.
28. The composition of claim 1 wherein the second dentifrice
component comprises an antitartar agent.
29. The method of claim 8 wherein the source of fluoride ions is
present in an amount sufficient to supply about 25 ppm to 5,000 ppm
fluoride ions.
30. The method of claim 8 wherein the source of fluoride ions is an
inorganic fluoride salt, soluble alkali metal salt, or combinations
thereof.
31. The method of claim 8 wherein the first dentifrice component
comprises an antibacterial agent.
32. The method of claim 31 wherein the antibacterial agent is a
halogenated diphenyl ether.
33. The method of claim 8 wherein the second dentifrice component
comprises a source of fluoride ions.
34. The method of claim 8 wherein the second dentifrice component
comprises an antibacterial agent.
35. The method of claim 34 wherein the antibacterial agent is a
halogenated diphenyl ether.
Description
CROSS REFERENCE TO RELATED APPLICATIONS
[0001] This application is a continuation of U.S. Ser. No.
11/191,501, filed Jul. 28, 2005 which claims priority to U.S. Ser.
No. 10/229,551, filed Aug. 28, 2002.
BACKGROUND OF THE INVENTION
[0002] Oral compositions such as toothpastes, gels and mouth washes
are designed to loosen and remove plaque in conjunction with a
regular toothbrushing regimen. Dental plaque is present to some
degree, in the form of a film, on virtually all dental surfaces. It
is a by product of microbial growth, and comprises a dense
microbial layer consisting of a mass of microorganisms embedded in
a polysaccharide matrix. Plaque itself adheres firmly to dental
surfaces and is removed only with difficulty even through a
rigorous brushing regimen. Moreover, plaque rapidly reforms on the
tooth surface after it is removed. Plaque may form on any part of
the tooth surface, and is found particularly at the gingival
margin, in cracks in the enamel, and on the surface of dental
calculus. The problem associated with the formation of plaque on
the teeth lies in the tendency of plaque to build up and eventually
produce gingivitis, periodontitis and other types of periodontal
disease, as well as dental caries and dental calculus.
[0003] It is known to the art to incorporate antimicrobial agents
in oral compositions wherein these agents destroy or inhibit oral
bacteria. Other agents are also incorporated in the oral
composition to enhance the efficacy of the antimicrobial agents.
For example, it is known to incorporate enzymes in oral
compositions which disrupt or interfere with plaque formation and
bacterial adhesion to tooth surfaces as disclosed in U.S. Pat. Nos.
2,527,686; 3,991,177; 3,194,738; 4,082,841; 4,115,546; 4,140,759;
4,152,418; 4,986,981; 5,000,939; 5,370,831; 5,431,903; 5,537,856;
5,849,271.
[0004] A problem encountered with the use of enzymes in oral care
compositions is that often the enzyme of choice is not compatible
with surfactants, namely ionic surfactants such as anionic
surfactants which are preferred for use in oral compositions such
as dentifrices and mouthwashes to achieve increased prophylactic
action, provide superior foaming properties and render the
compositions more cosmetically acceptable. Anionic surfactants such
as the higher alkyl sulfates are not compatible with enzymes as the
surfactant facilitates denaturing of the enzyme and loss in
activity. As a result, the use of this desirable class of
surfactants has been avoided by the art in the preparation of
enzyme containing dentifrices.
SUMMARY OF THE INVENTION
[0005] The present invention is based upon the discovery that when
a dual component dentifrice comprised of separately housed
dentifrice components in which a first component contains an ionic
or other surfactant normally incompatible with an enzyme and the
second component contains the enzyme, when the components are mixed
and combined during use, the enzyme is not found to denature but
retains its activity in the presence of the normally incompatible
ionic surfactant for at least the period of time involved in
toothbrushing.
[0006] In accordance with the present invention there is provided a
method for combining the plaque dispersion properties of active
enzymes and the superior foaming action of ionic surfactants using
a multicomponent dentifrice which dentifrice is comprised of
separately housed, semi-solid aqueous components; the first
component containing the enzyme in an orally acceptable vehicle and
a second component containing an ionic surfactant in an orally
acceptable vehicle whereupon combination of the components provides
a dentifrice having superior foaming properties without antiplaque
enzyme activity being significantly affected.
DESCRIPTION OF THE PREFERRED EMBODIMENTS
[0007] In use, the components of the two component dentifrice of
the present invention comprise a first enzyme containing dentifrice
component, and a second ionic surfactant containing dentifrice
component. The two components are preferably combined for use in
approximately equal weight proportions, so that about one-half of
the concentration of any particular ingredient within either
component will be present when the components are combined and
applied to the teeth, as by brushing. Both components are
preferably formulated to have similar physical characteristics, so
that the two components may be simultaneously delivered in the
desired predetermined amounts by extrusion when separately housed
in a multicompartmented tube or pump device.
First Dentifrice Component
Enzymes
[0008] The enzymes useful in the practice of the present invention
include enzymes extracted from natural fruit products such as
well-known protein substances within the class of proteases, which
breakdown or hydrolyze proteins. The proteolytic enzymes are
obtained from natural sources or by the action of microorganisms
having a nitrogen source and a carbon source. Examples of
proteolytic enzymes useful in the practice of the present invention
include the naturally occurring enzymes papain (from papaya),
bromelain (from pineapple), as well as serine proteases such as
chymotrypsin. Additional enzymes include ficin and alcalase.
[0009] Enzymes such as proteolytic enzymes are included in the
first dentifrice component of the present invention at a
concentration of about 0.010 to about 10.0% by weight and
preferably about 0.2 to about 5% by weight.
[0010] Papain obtained from the milky latex of the Papaya tree is
the proteolytic enzyme preferred for use in the practice of the
present invention and is preferably incorporated in the oral care
composition of the present invention in an amount of about 0.2 to
about 5% by weight, such papain having an activity of 150 to 900
units per milligram as determined by the Milk Clot Assay Test of
the Biddle Sawyer Group (see J. Biol. Chem., vol. 121, pages
737-745).
[0011] Enzymes which may beneficially be used in combination with
the proteolytic enzymes include carbohydrases such as glucoamylase,
alpha-amylase, beta-amylase, dextranase and mutanase, tannase and
lipases such as plant lipase, gastric lipase and pancreatic
lipase.
[0012] Glucoamylase is a saccharifying glucoamylase of Aspergillus
niger origin. This enzyme can hydrolyze both the alpha-D-1,6
glucosidic branch points and the alpha-1,4 glucosidic bonds of
glucosyl oligosaccharides. The product of this invention comprises
about 0.01 to 10% of the carbohydrases. The lipase enzyme is
derived from a select strain of Aspergillus niger. The enzyme has
maximum lipolytic activity at pH 5.0 to 7.0 when assayed with olive
oil. The enzyme has 120,000 lipase units per gram. Among the
carbohydrases useful in accordance with this invention are
glucoamylase, alpha and beta-amylase, dextranase and mutanase.
[0013] Other enzymes which may be denatured in the presence of
anionic surfactants and used in the practice of the present
invention include other carbohydrases such as alpha-amylase,
beta-amylase, dextranase and mutanase and lipases such as plant
lipase, gastric lipase, pancreatic lipase, pectinase, tannase
lysozyme and serine proteases.
[0014] The lipase enzyme is derived from a select strain of
Aspergillus niger, exhibiting random cleaving of the 1,3 positions
of fats and oils. The enzyme has maximum lipolytic activity at pH
5.0 to 7.0 when assayed with olive oil. The enzyme has a measured
activity of 120,000 lipase units per gram. The lipase may be
included in the dentifrice composition at a concentration of about
0.010 to about 5.0% by weight and preferably about 0.02 to about
0.10% by weight.
[0015] The presence of tannase enzyme can be further beneficial in
facilitating the breakdown of extrinsic stain. Tannase enzymes have
been purified from Aspergillus niger and Aspergillus allianceus and
are useful in the hydrolysis of tannins, known to discolor the
tooth surface.
[0016] Other suitable enzymes which can comprise the present
invention include lysozyme, derived from egg white, which contains
a single polypeptide chain crosslinked by four disulfide bonds
having a molecular weight of 14,600 daltons. The enzyme can exhibit
antibacterial properties by facilitating the hydrolysis of
bacterial cell walls cleaving the glycosidic bond between carbon
number 1 of N-acetylmuramic acid and carbon number 4 of
N-acetyl-D-glucosamine, which in vivo, these two carbohydrates are
polymerized to form the cell wall polysaccharide. Additionally,
pectinase, an enzyme that is present in most plants facilitates the
hydrolysis of the polysaccharide pectin into sugars and
galacturonic acid. Finally, glucanase, which may be utilized to
catalyze the breakdown of complex carbohydrates to glucans and the
hydrolysis of beta glucan to glucose.
Enzyme Stabilizing Agents
[0017] The enzyme containing component of the present invention may
also contain ingredients which stabilize enzymes in a dentifrice
environment. These stabilizers protect the enzyme from inactivation
by chelating metal impurities present in the oral composition which
have the propensity to denature the active site of the enzyme by
protecting the enzyme from oxidation. Agents stabilizing the enzyme
against oxidation include sodium bisulfite, metal gallates, sodium
stannate, 3,5-di-tert-butyl-4-hydroxytoluene (BHT), Vitamin E
(.alpha., .beta., .gamma., forms)/Vitamin E acetate and ascorbic
acid at concentrations between about 0.03 to about 1.5%, preferably
between about 0.3 and about 0.75%.
[0018] Additional chelating agents of mono and di charged cationic
species include sodium tripolyphosphate and tetrasodium
pyrophosphate, ethylene diamine tetraacetic acid and sodium
gluconate which may be incorporated in the dentifrice component at
a concentration of about 0.01 to about 1% by weight and preferably
between about 0.1 to about 0.5% by weight.
Dentifrice Vehicle
[0019] Orally-acceptable vehicles used to prepare the dentifrice
components of the present invention include a water-phase,
containing a humectant therein. The humectant is preferably
glycerin, sorbitol, xylitol, and/or propylene glycol of molecular
weight in the range of 200 to 1,000; but, other humectants and
mixtures thereof may also be employed. The humectant concentration
typically totals about 5 to about 70% by weight of the oral
composition.
[0020] Reference hereto to sorbitol refers to the material
typically commercially available as a 70% aqueous solution. Water
is present typically in amount of at least about 10% by weight, and
generally about 25 to 70% by weight of the dentifrice component.
Water employed in the preparation of commercially suitable oral
compositions should preferably be deionized and free of organic
impurities. These amounts of water include the free water which is
added plus that which is introduced with other materials such as
with sorbitol.
Nonionic Surfactants
[0021] Nonionic surfactants compatible with enzymes present in the
first dentifrice component include nonanionic polyoxyethylene
surfactants such as Polyoxamer 407, Steareth 30, Polysorbate 20,
and PEG-40 castor oil and amphoteric surfactants such as
cocamiopropyl betaine (tegobaine) and cocamidopropyl betaine lauryl
glucoside condensation products of ethylene oxide with various
hydrogen containing compounds that are reactive therewith and have
long hydrorphobic chains (e.g., aliphatic chains of about 12 to 20
carbon atoms), which condensation products ("ethoxamers") contain
hydrophilic polyoxyethylene moieties, such as condensation products
of poly(ethylene oxide) with fatty acids, fatty alcohols, fatty
amides and other fatty moieties, and with propylene oxide and
polypropylene oxides (e.g., Pluronic.RTM. materials). The nonionic
surfactants are included in the oral composition at a concentration
of between about 2 to abut 10% by weight and preferably between
about 3.5 to 6.5% by weight.
Abrasives
[0022] In the preparation of dentifrice components of the present
invention abrasives which may be used to prepare the components of
the present invention include silica abrasives such as precipitated
silicas having a mean particle size of up to about 20 microns, such
as Zeodent 115, marketed by J.M. Huber Chemicals Division, Havre de
Grace, Md. 21078, or Sylodent 783 marketed by Davison Chemical
Division of W.R. Grace & Company. Other useful dentifrice
abrasives include sodium metaphosphate, potassium metaphosphate,
tricalcium phosphate, dihydrated dicalcium phosphate, aluminum
silicate, calcined alumina, bentonite or other siliceous materials,
or combinations thereof.
[0023] Preferred abrasive materials useful in the practice of the
preparation of the dentifrice components in accordance with the
present invention include silica gels and precipitated amorphous
silica having an oil absorption value of less than 100 cc/100 g
silica and preferably in the range of from about 45 cc/100 g to
less than about 70 cc/100 g silica. These silicas are colloidal
particles having an average particle size ranging from about 3
microns to about 12 microns, and more preferably between about 5 to
about 10 microns and a pH range from 4 to 10 preferably 6 to 9 when
measured as a 5% by weight slurry.
[0024] Oil absorption values are measured using the ASTM Rub-Out
Method D281. The low oil absorption silica abrasive is present in
the oral are compositions of the present invention at a
concentration of about 5 to about 40% by weight and preferably
about 10 to about 30% by weight.
[0025] Low oil absorption silica abrasives particularly useful in
the practice of the present invention are marketed under the trade
designation Sylodent XWA by Davison Chemical Division of W.R. Grace
& Co., Baltimore, Md. 21203. Sylodent 650 XWA, a silica
hydrogel composed of particles of colloidal silica having a water
content of 29% by weight averaging from about 7 to about 10 microns
in diameter, and an oil absorption of less than 70 cc/100 g of
silica is a preferred example of a low oil absorption silica
abrasive useful in the practice of the present invention.
[0026] The dentifrice components of the present invention can
contain a variety of optional ingredients. As described below, such
optional ingredients can include, but are not limited to,
thickening agents, a source of fluoride ions, a flavoring agent,
antibacterial agents, antitartar and coloring agents.
Thickening Agents
[0027] Thickeners used in the preparation of the dentifrice
components of the present invention include natural and synthetic
gums and colloids. Not all naturally occurring polymer thickeners
(such as cellulose or carrageenans) are compatible with enzymes.
Thickeners compatible with enzymes such as proteolytic enzymes,
include xanthan gum, polyglycols of varying molecular weights sold
under the tradename Polyox and polyethylene glycol. Compatible
inorganic thickeners include amorphous silica compounds which
function as thickening agents and include colloidal silicas
compounds available under the trade designation Cab-o-sil
manufactured by Cabot Corporation and distributed by Lenape
Chemical, Bound Brook, N.J.; Zeodent 165 from J.M. Huber Chemicals
Division, Havre de Grace, Md. 21078; and Sylodent 15, available
from Davison Chemical Division of W.R. Grace Corporation,
Baltimore, Md. 21203. Other inorganic thickeners include natural
and synthetic clays, lithium magnesium silicate (Laponite) and
magnesium aluminum silicate (Veegum).
[0028] The thickening agent is present in the dentifrice
composition in amounts of about 0.1 to about 10% by weight,
preferably about 0.5 to about 4.0% by weight.
Fluoride and Other Active Agents
[0029] The oral composition of the present invention may also
contain a source of fluoride ions or fluorine-providing component,
as anticaries agent in amount sufficient to supply about 25 ppm to
5,000 ppm of fluoride ions and include inorganic fluoride salts,
such as soluble alkali metal salts. For example, preferred fluoride
sources which are compatible with enzymes present in the
composition are sodium fluoride, potassium fluoride, sodium
fluorosilicate, sodium monfluorophosphate (MFP), ammonium
fluorosilicate, as well as tin fluorides, such as stannous fluoride
and stannous chloride. Sodium fluoride or MFP is preferred.
[0030] In addition to fluoride compounds, there may also be
included in the oral compositions of the present inventions
antitartar agents such as pyrophosphate salts including dialkali or
tetraalkali metal pyrophosphate salts such as
Na.sub.4P.sub.2O.sub.7, K.sub.4P.sub.2O.sub.7,
Na.sub.2K.sub.2P.sub.2O.sub.7, Na.sub.2H.sub.2P.sub.2O.sub.7 and
K.sub.2H.sub.2P.sub.2O.sub.7, polyphosphates such as sodium
tripolyphosphate, sodium hexametaphosphate and cyclic phosphates
such as sodium tripolyphosphate sodium trimetaphosphate. These
antitartar agents are included in the dentifrice composition at a
concentration of about 1 to about 5% by weight.
[0031] Another active agent useful in dentifrice compositions of
the present invention are antibacterial agents, which can be from
0.2 to 1.0% by weight of the dentifrice composition. Such useful
antibacterial agents include non-cationic antibacterial agents
which are based on phenolic or bisphenolic compounds, such as
halogenated diphenyl ethers such as Triclosan
(2,4,4'-trichloro-2'-hydroxydiphenyl ether).
Flavor
[0032] The dentifrice components of the present invention may also
contain a flavoring agent. Flavoring agents which are used in the
practice of the present invention include essential oils as well as
various flavoring aldehydes, esters, alcohols, and similar
materials. 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. Of these, the most commonly employed are the oils of
peppermint and spearmint.
[0033] The flavoring agent is incorporated in the oral composition
at a concentration of about 0.1 to about 5% by weight and
preferably about 0.5 to about 1.5% by weight.
Other Ingredients
[0034] Various other materials may be incorporated in the
dentifrice components of the present invention, including
desensitizers, such as potassium nitrate; whitening agents, such as
hydrogen peroxide, calcium peroxide and urea peroxide;
preservatives; silicones; and chlorophyll compounds. These
additives, when present, are incorporated in the dentifrice
components of the present invention in amounts which do not
substantially adversely affect the properties and characteristics
desired.
Second Dentifrice Component
[0035] The vehicle of the second dentifrice component is formulated
to have a composition similar to the vehicle of the first
dentifrice component, so that two components will be of
substantially equivalent rheologies, which will permit them to be
synchronously coextrudable from a container in which the components
are separately housed. In order to maintain that the physical
characteristics of the second component have rheological properties
substantially equivalent to the first component, the vehicle
composition of the second component, specifically the humectant and
abrasive content, is adjusted.
[0036] The water and humectant comprise the liquid portion of the
second dentifrice component. The humectant is preferably sorbitol,
but other humectants such as glycerin and polyethylene glycol may
also be employed. The humectant content is generally in the range
of about 30% to about 70% by weight and preferably about 40 to
about 65% by weight, the water content is in the range of about 5
to about 40% by weight and preferably 10 to about 30% by
weight.
[0037] Preferred abrasives are siliceous materials, such as silica,
and preferably a precipitated amorphous hydrated silica, and
preferably a precipitated amorphous hydrated silica, such as
Zeodent 115, available from Huber Corporation. The abrasive is
generally present in the second dentifrice component at a
concentration of about 10 to about 40% by weight and preferably
about 15 to about 30% by weight.
Ionic Surfactants
[0038] Ionic surfactants incorporated in the second dentifrice
component are preferably anionic surfactants, examples of which
include higher alkyl sulfates such as potassium or sodium lauryl
sulfate which is preferred, higher fatty acid monoglyceride
monosulfates, such as the salt of the monosulfatedmonoglyceride of
hydrogenated coconut oil fatty acids, alkyl aryl sulfonates such as
sodium dodecyl benzene sulfonate, higher fatty sulfoacetates,
higher fatty acid esters of dihydroxy propane sulfonate, and the
substantially saturated higher aliphatic acyl amides of lower
aliphatic amino carboxylic acid compounds such as those having 12
to 16 carbons in the fatty acid, alkyl or acyl radicals, and the
like. Examples of the last mentioned amides are N-lauroyl sarcosine
and the salts of N-lauroyl, N-myristoyl, or N-palmitoyl sarcosine.
The surfactant is generally present in the potassium salt
dentifrice compositions of the present invention at a concentration
of about 0.5 to about 5.0% by weight.
[0039] A thickener may be incorporated in the second dentifrice
component at a concentration of about 0.5 to abut 10%, by weight
and preferably about 1 to about 5% by weight. Organic thickeners of
natural and synthetic gums of the same type used to prepare the
dentifrice component may also be incorporated at a concentration of
about 0.1 to abut 3% by weight and preferably about 0.2 to about 2%
by weight.
[0040] Additional ingredients such as fluoride and other active
agents such as antitartar agents, flavors and sweeteners similar to
that used for the preparation of the first component may be
included in the preparation of the second dentifrice component at
similar concentrations.
Preparation of Dentifrice Components
[0041] To prepare the enzyme containing dentifrice component of the
present invention, generally the humectants such as glycerin,
sorbitol are dispersed in the water in a conventional mixer under
agitation. Into the dispersion are added salts, such as sodium
fluoride anticaries agents, chelating agents such as bisulfite
salts, antitartar agents such as tetrasodium pyrophosphate and
sodium tripolyphosphate and any sweeteners; the resultant mixture
is agitated until a homogeneous gel phase is formed. Into the gel
phase are added a pigment such as TiO.sub.2, and any buffering salt
such as NaH2PO4 Na2HPO4 to buffer the pH at 6.3 to 7.5. These
ingredients are mixed until a homogenous phase is obtained.
Thereafter a dispersion in water and humectant of enzyme compounds
such as papain, glycoamylase is added and admixed with the
homogeneous phase This mixture is then transferred to a high
speed/vacuum mixer; wherein, thickeners such as xanthan gum,
Zeodent 165, laponite ingredients are added to the mixture.
Thereafter the abrasive is added together with the flavor oils to
be included in the composition and the solution is added along with
the nonionic surfactants to the mixture, which is then mixed at
high speed for from 5 to 30 minutes, under vacuum of from about 20
to 50 mm of Hg, preferably about 30 mm Hg. The resultant product is
in each case is a homogeneous, semi-solid, extrudable paste or gel
product. The final pH of the dentifrice measured neat was
determined to range between 6.7 and 7.25.
[0042] To prepare the second dentifrice components of the present
invention, generally the humectants, for example, sorbitol are
dispersed with any organic thickeners and sweetener. Water is then
added into this dispersion and the ingredients mixed until a
homogenous phase is obtained for the component. Thereafter silica
abrasive, flavor and ionic surfactant ingredients are added and the
ingredients mixed at high speed under vacuum of from about 20 to
100 mm of Hg. The resultant product, in the case of each component,
is a homogeneous, semi-solid, extrudible paste product.
[0043] The multicomponent dentifrice composition of the present
invention is packaged in a suitable dispensing container in which
the components are maintained physically separated and from which
the separated components may be dispensed synchronously as a
combined ribbon for application to a toothbrush. Such containers
are known in the art. An example of such a container is a two
compartment dispensing container, such as a pump or a tube, having
collapsible sidewalls, as disclosed in U.S. Pat. Nos. 4,487,757 and
4,687,663; wherein, the tube body is formed from a collapsible
plastic web such as polyethylene or polypropylene and is provided
with a partition within the container body defining separate
compartments in which the physically separated components are
stored and from which they are dispensed through a suitable
dispensing outlet.
[0044] The following example is further illustrative of the present
invention, but it is understood that the invention is not limited
thereto. All amounts and proportions referred to herein and in the
appended claims are by weight, unless otherwise stated.
Example
[0045] A two component (Component A and B) enzyme containing
dentifrice of the present invention was prepared, wherein Component
A was a paste prepared with the enzymes papain and glycoamylase and
the second Component B was prepared having incorporated therein the
anionic surfactant sodium lauryl sulfate. The ingredients of
Components A and B are listed in Table I below.
TABLE-US-00001 TABLE I Component A Component B Ingredient Wt. %
Ingredient Wt. % Water 16.0 Water 9.8 Pluronic F-127 1.50
Carboxymethyl cellulose 0.60 Laponite D 0.70 Tetrasodium
pyrophosphate 0.50 Glycerin 18.13 NaFluoride 0.243 Tetrasodium
pyrophosphate 2.0 Sorbitol 59.937 Sodium tripolyphosphate 3.0
NaSaccarin 0.30 Xanthan 0.35 Silica 25.50 NaFluoride 0.243 Flavor
0.72 NaSaccarin 0.4 Sodium lauryl sulfate (SLS) 2.40 NaH2PO4 0.03
Na2HPO4 0.2 NaHSO3 0.1 Sorbitol 20.0 Sylodent XWA 650 20.0 Zeodent
115 5.0 Zeodent 165 1.75 TiO2 0.4 PEG-600 4.0 Papain 1.0
Glucoamylase 0.1 Flavor 1.1 Polysorbate 2.0 Tegobetaine 2.0
[0046] To determine the stability of enzyme (papain) activity of
the dentifrice when the individual components (Components A and B)
are mixed and combined in tooth brushing, equal amounts (3 grams)
of Components A and B were mixed in 18 milliliters of water and
stirred for 3, 10 and 20 minute intervals. Time expended by
consumers involved in toothbrushing normally ranges from 0.5 to 2.0
minutes.
[0047] The protease enzyme activity for each solution was
determined using a standard enzyme assay procedure, namely a
procedure developed by Sigma Chem. Corp using a titrimetric
determination of the acid produced during the hydrolysis of
benzoyl-L-arganinine ethyl ester (BAEE), (Amon, R., Methods in
Enzymology, 1970).
[0048] A similar enzyme activity assay was conducted for Component
A alone. The results of the assays are recorded in Table II
below.
TABLE-US-00002 TABLE II Papain Activity % Enzyme Activity Remaining
Mixing Time: Component 3 minutes 10 minutes 20 minutes A 100% 100%
97% A + B 96% 82% 43%
[0049] The results recorded in Table II show that both dentifrice
systems had similar enzyme activities in the first few minutes of
mixing. However, the combined components (A+B) started to lose
enzyme activity after 10 minutes of mixing. The results in Table II
show that unexpectedly, the enzyme can coexist in the presence of
the anionic surfactant SLS for a period of time sufficient (3
minutes) to provide activity and plaque dispersion efficacy, before
a significant enzyme denaturation is encountered.
[0050] The foam characteristics of Component A and the mixture of
Components A and B were also evaluated. The foam volume
measurements were made by dispersing 10 grams of dentifrice in 90
milliliters (ml) of distilled water. Then 20 ml of the slurry was
transferred into a 50 ml graduated cylinder. The foam was generated
by alternately inverting the cylinder (shaking) 10 times. The foam
volume was monitored as a function of time using the graduation
mark.
[0051] The result of the foam tests are recorded in Table III
below. For purposes of comparison, a commercially available silica
based fluoride toothpaste which did not contain enzymes
(Colgate.RTM. Cavity Protection) but which contained sodium lauryl
sulfate as the surfactant was also evaluated for foam volume.
TABLE-US-00003 TABLE III FOAM PROPERTIES Dentifrice Component Foam
Volume, ml A 42 (A + B) 64 Colgate .RTM. Cavity Protection 67
[0052] The results recorded in Table III show that the dentifrice
composed of combined dentifrice Components A and B delivered foam
substantially greater than the enzyme containing Component A.
Further, the combined dentifrice components (A+B) delivered foam
substantially equivalent to silica based commercial toothpastes
which contained sodium lauryl sulfate.
* * * * *