U.S. patent application number 11/742061 was filed with the patent office on 2007-11-01 for oral compositions comprising siloxane polymers.
Invention is credited to THOMAS J. BOYD.
Application Number | 20070253919 11/742061 |
Document ID | / |
Family ID | 38606500 |
Filed Date | 2007-11-01 |
United States Patent
Application |
20070253919 |
Kind Code |
A1 |
BOYD; THOMAS J. |
November 1, 2007 |
ORAL COMPOSITIONS COMPRISING SILOXANE POLYMERS
Abstract
Oral compositions are provided that comprise an active
ingredient comprising a siloxane polymer having at least one
hydrophilic region. The oral care composition comprises a siloxane
polymer having a phosphorus-containing moiety. A source of fluoride
ions and/or other oral care actives can be included in the oral
care composition. Methods of making and using the oral compositions
are also provided.
Inventors: |
BOYD; THOMAS J.; (Metuchen,
NJ) |
Correspondence
Address: |
COLGATE-PALMOLIVE COMPANY
909 RIVER ROAD
PISCATAWAY
NJ
08855
US
|
Family ID: |
38606500 |
Appl. No.: |
11/742061 |
Filed: |
April 30, 2007 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
|
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60796384 |
May 1, 2006 |
|
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Current U.S.
Class: |
424/54 |
Current CPC
Class: |
A61Q 11/00 20130101;
B65D 83/205 20130101; A61K 8/896 20130101; A61P 31/02 20180101;
A61P 31/04 20180101 |
Class at
Publication: |
424/54 |
International
Class: |
A61K 8/00 20060101
A61K008/00 |
Claims
1. An oral care composition comprising a siloxane polymer having a
phosphorus-containing moiety.
2. A composition according to claim 1, wherein at least one of the
moieties comprising phosphorus is selected from the group
consisting of: phosphate, phosphonate, phospholipids, a
phosphate-containing group, and combinations thereof.
3. A composition according to claim 1, wherein the siloxane polymer
comprises a compound having the formula: ##STR00007## wherein
R.sub.1 is selected from the group consisting of: alkyl, aryl,
amide, ester, pyrrolidone, vinyl, acrylate, siloxane, urethane,
carbonate, vinyl alcohol, alkylene oxide, and combinations thereof;
and R.sub.2 comprises a moiety selected from the group consisting
of: phosphate, phosphonate, phospholipids, a phosphate-containing
group, and combinations thereof, "x" is 0 to 100 and "y" is 1 to
100.
4. A composition according to claim 3, wherein R.sub.1 has the
formula: --(CH.sub.2).sub.v-(Q).sub.z, where Q is at least one
group selected from: C.sub.2H.sub.2O, C.sub.3H.sub.6O;
CH.sub.2CH(OH); CONH,CO.sub.2, NH, CONH, ##STR00008## wherein "v"
and "z" are 1 to 16.
5. An oral care composition according to claim 1 comprising about
0.001 to about 3% by weight of the siloxane polymer.
6. A composition according to claim 1, wherein the composition
comprises an ingredient selected from the group consisting of:
surface active agents, viscosity modifiers, thickeners, humectants,
diluents, fillers, pH modifying agents, plasticizers, fillers,
waxes, texture modifiers, flavoring agents, sweetening agents,
coloring agents, preservatives, solvents, and mixtures thereof.
7. A composition according to claim 1, further comprising an active
ingredient selected from the group consisting of an antimicrobial
agent, an antitartar agent, an anti-plaque, an anticaries agent, a
biofilm disruption agent, an antioxidant, an anti-inflammatory
agent, a tooth whitening agent, an anti-adhesion agent, a
desensitizing agent, a malodor control agent, a flavoring agent, a
coloring agent, an anti-aging agent, a salivary stimulant, a
periodontal active, a conditioning agent, a natural extract, an
essential oil, a nutrient, an enzyme, a protein, an amino acid, a
vitamin, an analgesic, and mixtures thereof.
8. An oral care composition comprising a siloxane polymer having a
phosphorus-containing moiety, wherein the siloxane polymer is an
anti-attachment agent that substantially inhibits bacteria from
forming a biofilm on a tooth surface.
9. An oral care composition according to claim 8, wherein the
moiety containing phosphorus is selected from the group consisting
of: phosphate, phosphonate, phospholipids, a phosphate-containing
group, and combinations thereof.
10. An oral care composition according to claim 9, wherein the
siloxane polymer comprises an alkyl phosphate siloxane.
11. An oral care composition according to claim 9, wherein the
siloxane polymer comprises a polydimethylsiloxane phosphate.
12. An oral care composition according to claim 8, wherein the
siloxane polymer comprises a compound having the formula:
##STR00009## wherein R.sub.1 is selected from the group consisting
of: alkyl, aryl, amide, ester, pyrrolidone, vinyl, acrylate,
siloxane, urethane, carbonate, vinyl alcohol, alkylene oxide, and
combinations thereof; and R.sub.2 comprises a moiety selected from
the group consisting of: phosphate, phosphonate, phospholipids, a
phosphate-containing group, and combinations thereof, "x" is 0 to
100 and "y" is 1 to 100.
13. An oral care composition according to claim 12, wherein R.sub.1
has the formula: --(CH.sub.2).sub.v-(Q).sub.z, where Q is at least
one group selected from: C.sub.2H.sub.2O, C.sub.3H.sub.6O;
CH.sub.2CH(OH); ##STR00010## CONH,CO.sub.2, NH, CONH, wherein "v"
and "z" are 1 to 16.
14. An oral care composition according to claim 8, wherein the
siloxane polymer comprises a compound having the formula:
##STR00011## wherein R.sub.2 is --PO.sub.3H.sub.2 or
--(CH.sub.3CH.sub.2H.sub.3O).sub.nPO.sub.3H.sub.2, "x" is 0 to 100,
"y" is 1 to 100, and "m" is 0 to 15.
15. An oral care composition according to claim 8, wherein the
siloxane polymer comprises a compound having the formula:
##STR00012## wherein R.sub.3 is an alkyl group, "x" is 0 to 100,
and "y" is 1 to 100.
16. An oral care composition according to claim 15, wherein R.sub.3
is a C.sub.1-8 alkyl group.
17. An oral care composition according to claim 8 comprising about
0.001 to about 3% by weight of the siloxane polymer.
18. An oral care composition according to claim 8, further
comprising an active ingredient selected from the group consisting
of an antimicrobial agent, an antitartar agent, an anti-plaque, an
anticaries agent, a biofilm disruption agent, an antioxidant, an
anti-inflammatory agent, a tooth whitening agent, an anti-adhesion
agent, a desensitizing agent, a malodor control agent, a flavoring
agent, a coloring agent, an anti-aging agent, a salivary stimulant,
a periodontal active, a conditioning agent, a natural extract, an
essential oil, a nutrient, an enzyme, a protein, an amino acid, a
vitamin, an analgesic, and mixtures thereof.
19. An oral care composition according to claim 8, further
comprising a carrier ingredient selected from the group consisting
of surface active agents, viscosity modifiers, thickeners,
humectants, diluents, pH modifying agents, emollients,
moisturizers, mouth feel agents, sweetening agents, flavoring
agents, solvent, water, colorants, preservatives, and mixtures
thereof.
20. An oral composition comprising an anti-plaque and/or antitartar
active ingredient comprising a siloxane polymer having at least one
hydrophilic region, wherein the siloxane polymer is an
anti-attachment agent that substantially inhibits bacteria from
forming a biofilm on a tooth surface, and wherein the composition
is substantially free of lipophilic active ingredients.
21. An oral composition according to claim 20, wherein the
hydrophilic region comprises a moiety selected from the group
consisting of: alkylene oxides, phosphates, phosphonates,
phospholipids, amines, and combinations thereof.
22. An oral composition according to claim 20, wherein the siloxane
polymer comprises a compound having the formula: ##STR00013##
wherein R.sub.4 is selected from H or --PO.sub.3H.sub.2, "x" is 0
to 100, "y" is 1 to 100, "m" is 0 to 15, and "n" is 0 to 15.
23. An oral composition according to claim 20, wherein the siloxane
polymer comprises a compound having the formula: ##STR00014##
wherein "x" is 0 to 100, "y" is 1 to 100, and "m" is 0 to 15.
24. An oral composition according to claim 20, wherein the siloxane
polymer comprises a compound having the formula: ##STR00015##
wherein R.sub.1 is selected from the group consisting of: alkyl,
aryl, amide, ester, pyrrolidone, vinyl, acrylate, siloxane,
urethane, carbonate, vinyl alcohol, alkylene oxide, and
combinations thereof; and R.sub.2 comprises a moiety selected from
the group consisting of: phosphate, phosphonate, phospholipids, a
phosphate-containing group, and combinations thereof, "x" is 0 to
100 and "y" is 1 to 100.
25. An oral composition according to claim 20, wherein the siloxane
polymer comprises a compound having the formula: ##STR00016##
wherein R.sub.2 is --PO.sub.3H.sub.2 or
--(CH.sub.3CH.sub.2H.sub.3O).sub.NPO.sub.3H.sub.2, "x" is 0 to 100,
"y" is 1 to 100, and "m" is 0 to 15.
26. An oral composition according to claim 20, wherein the siloxane
polymer comprises a compound having the formula: ##STR00017##
wherein R.sub.3 is a C.sub.18 alkyl group, "x" is 0 to 100, and "y"
is 1 to 100.
27. An oral composition according to claim 20 comprising about
0.001 to about 3% by weight of the siloxane polymer.
28. An oral composition according to claim 20, further comprising a
non-lipophilic active ingredient selected from the group consisting
of an anticaries agent, a biofilm disruption agent, an antioxidant,
an anti-inflammatory agent, a tooth whitening agent, an
anti-adhesion agent, a desensitizing agent, a malodor control
agent, a flavoring agent, a coloring agent, an anti-aging agent, a
salivary stimulant, a periodontal active, a conditioning agent, a
natural extract, an essential oil, a nutrient, an enzyme, a
protein, an amino acid, a vitamin, an analgesic, and mixtures
thereof.
Description
CROSS REFERENCE TO RELATED APPLICATION
[0001] This application claims the benefit of U.S. Provisional
Patent Application No. 60/796,384 filed May 1, 2006, the contents
of which is incorporated herein by reference.
BACKGROUND OF THE INVENTION
[0002] Dental plaque or plaque biofilm is a soft deposit that forms
on teeth and is implicated in the occurrence of gingivitis,
periodontitis, caries and other forms of periodontal disease. A
plaque biofilm provides a locus for calculus or tartar formation,
which is a hard mineralized solid formed on the teeth when crystals
of calcium phosphate are deposited in the pellicle and
extracellular matrix of the dental plaque biofilm and become
crystalline hydroxyapatite. While regular brushing helps to prevent
rapid build-up of these deposits, even regular brushing is not
sufficient to remove all of the calculus deposits which adhere to
the teeth.
[0003] Various antibacterial agents have found to have the clinical
ability to retard the growth of bacterial and hence have the
ability to minimize plaque formation, oral infections and diseases
associated therewith. However, many antibacterial agents are
incompatible or unstable with other oral care active ingredients,
difficult to deliver in vivo, or may inactivate other desirable
additional oral care ingredients. Some antibacterial agents are
difficult to formulate in oral compositions or are expensive.
[0004] It would be desirable to develop highly efficacious oral
compositions that prevent or combat plaque formation, as well as
other detrimental oral health implications, by using a stable
antiplaque and/or antitartar active agent. Thus, there is a need
for an oral care composition that effectively reduces the
development or progression of oral disease, preferably by having an
active ingredient that functions to diminish the effects of oral
disease by preventing or reducing multiple etiological factors that
contribute to and/or exacerbate oral disease. Further, there is a
need to use stable oral care actives in an oral composition, so
that their functionality and bioavailability as delivered to a
subject in vivo is preserved and stabilized.
DETAILED DESCRIPTION OF THE INVENTION
[0005] The following description is merely exemplary in nature and
is not intended to limit the present disclosure, application, or
uses.
[0006] In various embodiments, oral care compositions are provided
with an active ingredient that comprises a siloxane polymer that
provides various oral care benefits, such as antiplaque effects and
tartar control, among others. A "siloxane polymer" refers to a
polymer that has a basic backbone of silicon and oxygen with side
constituent groups that may be the same or different, generally
described by the structural repeating unit (--O--SiRR'--).sub.n,
where R and R' may be the same or different side constituent
groups, and n may be any value above 2 designating the repetition
of the SRU in the polymer backbone. Siloxane polymers are also
known in the art as "silicone" polymers. Siloxane polymers may
include polyheterosiloxanes, where side groups and/or structural
repeating units may be different entities (having different side
constituent groups), such as, for example, the siloxane co-polymer
described by the nominal SRU formula,
(--O--SiRR').sub.n--(--O--Si--R''R''').sub.m, wherein R and R' are
distinct side groups from R'' and R''' and m is an integer. Further
R and R' may be different from one another; likewise the same may
be true for R'' and R'''. Such siloxane polymers may terminate in
any variety of terminal groups, such as for example, trimethyl
silyl ((CH.sub.3).sub.3Si) terminated siloxane, or ethyl vinyl
terminated siloxane. Often, the siloxane polymer is crosslinked,
for example, in a hydrosilylation reaction where ethylenically
unsaturated groups react with hydride groups.
[0007] Conventional polyorganosiloxane polymers are hydrophobic.
However, in accordance with various aspects of the disclosure, the
active ingredient comprises a siloxane polymer that has at least
one hydrophilic region. In various embodiments, the hydrophilic
region comprises one or more hydrophilic moieties, such as alkylene
oxides, amines or phosphorus-containing groups. In certain
embodiments, the hydrophilic region includes a moiety comprising
phosphorus. Exemplary phosphorus containing moieties include, by
way of example, phosphates, phosphonates, phospholipids, and the
like, as will be described in more detail below.
[0008] In certain embodiments, the siloxane polymer comprises has
pendent alkyl groups. The siloxane polymer further comprises a
phosphorus-containing moiety, for example, a phosphate. In this
regard, a suitable siloxane polymer for use as an oral care active
ingredient comprises a phosphate and one or more alkyl groups, and
is broadly referred to as an alkyl phosphate siloxane polymer. In
certain embodiments, the alkyl groups are selected to be methyl
groups and the siloxane polymer comprises a polydimethylsiloxane
having a phosphate group.
[0009] In certain embodiments, the siloxane polymer comprises a
compound according to the nominal general formula (I):
##STR00001##
where R.sub.1 is selected from the group consisting of: alkyl,
aryl, amide, ester, pyrrolidone, vinyl, acrylate, siloxane,
urethane, carbonate, vinyl alcohol, alkylene oxide, and
combinations thereof; and R.sub.2 comprises a moiety selected from
the group consisting of: phosphate, phosphonate, phospholipids, a
phosphate-containing group, and combinations thereof. In certain
embodiments, R.sub.1 alkyl and/or aryl groups range from
(C.sub.1-C.sub.50), and in some embodiments have lower alkyl/aryl
groups, for example having from C.sub.2-C.sub.10, optionally from
C.sub.2-C.sub.6. In certain embodiments, alkylene oxides can range
from C.sub.2-C.sub.4, thus including ethylene oxide, propylene
oxide, and butylene oxide, of which multiple groups may be
provided. "x" ranges from 0 to 100 and "y" from 1 to 100.
[0010] In certain embodiments, R.sub.1 comprises
--(CH.sub.2).sub.v-(Q).sub.z, where Q is at least one group
selected from: an alkylene oxide having C.sub.2-C.sub.3, such as
C.sub.2H.sub.2O or C.sub.3H.sub.6O; CH.sub.2CH(OH); CONH,CO.sub.2,
NH, CONH,
##STR00002##
wherein v and z are respectively 1 to 16. For example, R.sub.2 can
be selected from PO.sub.3H.sub.2, PO.sub.3K.sub.2,
PO.sub.3Na.sub.2, PO.sub.3Liz and PO.sub.3(NH.sub.4).sub.2, from
phospholipids, such as phosphatidyl choline, phosphatidic acid,
phosphatidyl inositol, phosphatidyl ethanolamine, and the like.
[0011] Suitable siloxane polymers are disclosed in U.S. Pat. No.
5,530,084 to Ihara et al.; U.S. Pat. No. 5,070,171 and 6,175,028
both to O'Lenick; U.S. Pat. No. 6,124,490 to Gormley et al.; U.S.
Pat. Nos. 6,225,489, 5,849,313, and 5,688,496 all to Fost et al.;
and 5,859,161 to Imperante et al. All references cited in the
detailed description, including those listed above, are expressly
incorporated by reference in their entireties.
[0012] In some embodiments, the siloxane polymer having a
phosphate-containing moiety comprises a dimethicone copolyol
phosphate of the type disclosed in U.S. Pat. No. 5,070,171. Such
siloxane polymers have a pendant phosphate functional group and are
prepared by reacting a hydroxyl-containing silicone with a
phosphating reagent.
[0013] In certain embodiments, the siloxane polymer comprising a
phosphate moiety is a compound having the formula (II):
##STR00003##
where R.sub.2 is a pendant phosphate group, such as
--PO.sub.3H.sub.2 or
--(CH.sub.3CH.sub.2H.sub.3O).sub.nPO.sub.3H.sub.2, "x" is 0 to 100,
"y" is 1 to 100, "m" is 0 to 15. In other embodiments, the siloxane
polymer comprises at least one phosphate and at least one amine
group. An example of a suitable compound of such a siloxane polymer
comprising a phospholipid as the phosphorus-containing moiety has
the formula (III):
##STR00004##
where R.sub.3 is an alkyl group ranging from C.sub.1 to C.sub.50,
"x" is 0 to 100, "y" is 1 to 100. In some embodiments, R.sub.1 is a
C.sub.1-8 alkyl group.
[0014] Non-limiting examples of siloxane polymers comprising a
moiety comprising phosphorus suitable for use in oral care and/or
personal care compositions include phosphated silicone polymers
that are available commercially from Phoenix Chemical of
Somerville, N.J., United States of America under the trade
designations PECOSIL.RTM. PS-100 (a dimethicone polyethylene glycol
(PEG-7) phosphate), PS-200 (a dimethicone polyethylene glycol
(PEG-10) phosphate), WDS-100 (a dimethicone polyethylene
glycol/polypropylene glycol (PEG/PPG-7/4) phosphate), WDS-200
dimethicone polyethylene glycol/polypropylene glycol (PEG/PPG-12/4)
phosphate), and PECOSIL.RTM. PSQ-418 (Steardimonium hydroxypropyl
PEG-7 dimethicone).
[0015] These commercially available phosphated siloxane polymers
generally have the following structural formulas (IV):
##STR00005##
where R.sub.5 is (C.sub.2H.sub.4O).sub.a where "a" varies based on
the desired ethylene glycol (PEG) chain length/desired molecular
weight; and PECOSIL.RTM. WDS-100 and WDS-200 are
(CH.sub.3C.sub.2H.sub.3O).sub.b(C.sub.2H.sub.4O).sub.c where "b"
and "c" vary based on the selected chain length of the propylene
glycol (PPG) and ethylene glycol (PEG) respectively. Polymers of
this general class have "x" of 0 to 100 and "y" of 1 to 100.
[0016] Another siloxane polymer having a hydrophilic region
including a phosphorus-containing moiety useful as active
ingredients for oral compositions is linoleamidopropyl PG-diimonium
chloride phosphate dimethicone available commercially under the
trade name MONASIL.TM. PLN (also available as ARLASILKT.TM.
Phospholipid PLN) from Uniqema Inc., of Wilmington, Del., United
States of America. This polymer has the structure previously shown
in Formula III above, and polymers of this general class include in
certain embodiments, R.sub.3 representing C.sub.18, "x" from 0 to
100, and "y" from 1 to 100.
[0017] In some embodiments, the hydrophilic region of the siloxane
polymer comprises one or more hydrophilic groups, such as alkylene
oxides and/or amines, where the siloxane polymer comprises a
compound having the formula (V):
##STR00006##
where R.sub.4 is selected from H or --PO.sub.3H.sub.2, "x" is 0 to
100, "y" is 1 to 100, and "m" is 0 to 15, and "n" is 0 to 15. For
example, a siloxane polymer having R.sub.4 selected to be H is
commercially available as DC-190 and is available from the
Dow-Corning Company, Midland, Mich., United States of America.
Other suitable siloxane polymers having hydrophilic regions are
commercially available under the trade names DC-193 (polyethylene
methylpolysiloxane copolymer or PEG-12 dimethicone) and DC-5103
(siloxylated polyether surfactants with ethylene oxide and/or
propylene oxide from Dow-Corning Company, Midland, Mich., United
States of America.
[0018] In various embodiments, the siloxane polymers comprising at
least one hydrophilic region are believed to function as an
antiattachment or antiadhesion agent. While not limiting as to the
present invention, antiattachment oral care active ingredients are
generally believed to operate by either (or both) of two
predominant anti-attachment mechanisms. Biofilms (also referred to
as pellicle) are a matrix formed on an oral surface, typically on a
hard tissue surface, comprising bacteria (generally about 60-70% of
the biomatrix), bacterial extracellular byproducts, proteins,
lipids, and glycolipids. The term "oral surface" encompasses hard
and soft tissues within the oral cavity. Hard tissues include the
teeth, periodontal support, and the like. Soft tissues comprise
gums, the tongue, surfaces of the buccal cavity, and the like. The
oral compositions of the various embodiments can be used in a
mammalian subject, which includes humans and other warm blooded
higher level vertebrate animals, such as felines and canines.
[0019] Without being bound by theory, it is believed that early
stages of biofilm formation include an initial bacteria layer that
attaches to an oral surface, generally believed to be attached by
ligands or adhesins on the bacterial cell wall that interact with
receptors on an oral surface. It is believed that the bacterial
cells attach to the salivary glycoproteins on the oral surface,
e.g., enamel. The bacteria appear to form a stronger attachment by
generating extracellular glucan polymers to adhere to the oral
surface. The bacteria then grow and divide to form a dense layer on
the oral surface. After a specific density is reached, it is
believed that the bacteria reorganize and begin to form pillars and
irregular surface structures. Further, the biofilm matrix is
believed to have a complex association of multi-layered and diverse
species that form cell clusters attached to the anchoring bacteria
of the first layer.
[0020] Without being bound by any particular theory, it is believed
that one mechanism by which anti-attachment oral care agents are
believed to operate is where the anti-attachment agent interacts
with the bacteria itself to disable it from attaching to the oral
surface, likely by interacting with the adhesins, ligands, or other
moieties on the surface of the bacteria that would ordinarily
facilitate a linkage with a receptor or other moiety on the oral
surface.
[0021] Another anti-attachment mechanism is one where agents
interact with an oral surface to form a protective layer, such that
the bacteria and biofilm components cannot adhere to the oral or
tooth surface, thereby preventing an initial anchoring layer from
forming on the oral surface. Such an anti-attachment agent may
substantially cover an oral surface, and prevent attachment of the
bacteria and other components of the biofilm matrix. While not
limiting as to any particular mechanism by which the invention
operates, it is believed that the siloxane polymer active agents of
the various embodiments of the disclosure operate via such a
mechanism, coating a tooth surface, altering its surface energy,
and inhibiting bacterial attachment.
[0022] Thus, while not wishing to be limited to any particular
mechanism it is believed that oral care compositions comprising a
siloxane having a hydrophilic region as an active ingredient, e.g.,
a phosphorus-containing moiety, function via an anti-attachment
mechanism that substantially inhibits bacterial attachment to a
tooth surface. By "substantially inhibit" it is meant that the
biofilm generation or proliferation is impeded; however the extent
to which the inhibition occurs depends upon concentration and
distribution of the active ingredient as delivered in vivo to the
oral surface, as well as the amount of biofilm present prior to
treatment with the active ingredient. It appears that certain
siloxane polymers having hydrophilic regions alter the surface
energy of hard tissues, such as enamel (by reducing the surface
energy), and in turn, prevent or reduce adherence and attachment of
microorganisms that may form a plaque biofilm on the tooth surface.
Preferred siloxane polymers have substantivity on the tooth
surface, such that they remain attached for a sufficient period of
time to effectively prevent or reduce microorganisms' growth and or
adherence to the tooth surface, thereby preventing or reducing
biofilm formation.
[0023] In some embodiments, an oral composition comprises an
anti-plaque and/or antitartar active ingredient that is a siloxane
polymer comprising at least one hydrophilic region that is believed
to be an anti-attachment agent that substantially inhibits bacteria
from forming a biofilm on a tooth surface. The hydrophilic region
comprises a moiety selected from the group consisting of: alkylene
oxides, phosphates, phosphonates, phospholipids, amines, and
combinations thereof. Such siloxane polymers include those
described above, inter alia. The efficacy of the siloxane polymer
as delivered in an oral composition is sufficient such that there
is no need for an additional antibacterial agent. For example, in
certain embodiments, the oral composition is substantially free of
lipophilic active ingredients, such as halogenated diphenyl ethers,
eucalyptol, thymol, menthol and the like. In this regard, the
compositions have high antiplaque efficacy, while requiring fewer
active ingredients, which can be costly and complex to formulate.
By "substantially free" it is meant that the component or compound
is absent to the extent that it cannot be detected or it is still
suitable to use the item for its intended purpose (where the
absence of the desired characteristic or property is required). In
certain embodiments, substantially free means that there is less
than about 3% by weight of the non-ionic or lipophilic active
ingredients, optionally less than about 2%; optionally less than
about 1%, and preferably entirely free of the active ingredient. In
certain embodiments, the oral composition consists essentially of
an anti-plaque and/or antitartar active ingredient that is a
siloxane polymer comprising at least one hydrophilic region.
[0024] Such oral compositions can optionally comprise other active
ingredients that are less complex to formulate in an oral
composition or provide particular desirable oral care benefits, for
example, polyphosphate anticalculus compounds or anticaries agents,
as will be discussed in more detail below. In certain embodiments,
the oral composition comprises an antiplaque or antitartar agent
that consists essentially of a siloxane polymer having at least one
hydrophilic region.
[0025] In various embodiments, such an antiattachment effect is
obtained at relatively low concentrations. For example, the oral
composition comprises an active ingredient having a siloxane
polymer having one or more hydrophilic regions that is present in
the oral composition at about 0.001 to about 3% by weight, more
preferably between about 0.5 to about 2.5% by weight. In certain
embodiments, the oral composition comprises a siloxane polymer
having one or more hydrophilic regions at about 1% by weight.
[0026] In accordance with various embodiments, the application of
oral compositions having an active ingredient comprising a siloxane
polymer with a hydrophilic region, as provided in the various
embodiments of the present disclosure, promotes longer and more
effective anti-plaque benefits at lower concentrations in
comparison with many other antimicrobial ingredients which are
washed away in the aqueous oral cavity. Such a reduction in plaque,
in turn, provides calculus or tartar control, as well.
[0027] In various embodiments, a highly efficacious antiplaque and
anticalculus oral care composition contains the siloxane polymers
having a hydrophilic region as the sole antiplaque/antibacterial
ingredient. However, in certain embodiments, one or more additional
active ingredients may be included in the oral care compositions.
Any additional active agents for use with the siloxane polymer
should be carefully selected. If added, the additional active
ingredients should not react with or detract from the efficacy and
bioavailability of the siloxane polymer agents.
[0028] Non-limiting examples of oral care active ingredients for
oral compositions, include for example, tooth whitening agents,
antimicrobial agents, anti-caries agents, antitartar agents,
anti-plaque agents, anti-adhesion agents, desensitizing agents,
anti-inflammatory agents, malodor control agents, flavoring agents,
coloring agents, anti-aging agents, salivary stimulants,
periodontal actives, conditioning agents, moisturizing agents,
including emollients, occlusive reagents and humectants, natural
extracts and essential oils, nutrients, enzymes, proteins, amino
acids, vitamins, analgesics, antibiotics, and mixtures thereof.
Exemplary oral care actives among those useful herein are disclosed
in U.S. Pat. No. 4,894,220 to Nabi et al., U.S. Pat. No. 5,288,480
and 5,776,435, both to Gaffar et al., U.S. Pat. No. 5,681,548 to
Esposito et al., U.S. Pat. No. 5,912,274 and 5,723,500 both to
Stringer et al., U.S. Pat. No. 6,290,933 to Durga et al., and U.S.
Pat. No. 6,685,921 to Lawlor, as well as in United States Patent
Application Publication No. 2003/0206874 to Doyle et al. Further, a
wide variety of suitable active ingredients for both oral and
personal care compositions are listed in Gottschalk et al. eds.,
International Cosmetic Ingredient Dictionary and Handbook, Tenth
Edition, Volume 3 (2004). Such active ingredients are well known to
one of skill in the art.
[0029] Mixtures of additional oral care active ingredients, even
within the same classification, are contemplated by the present
disclosure. In various embodiments, the additional active
ingredients comprise from about 0.0001% to about 10%, preferably
from about 0.001% to about 5%, more preferably from about 0.01% to
about 3% by weight of the oral composition, depending on the
concentration of the active compounds and form of the oral
composition.
[0030] In various embodiments, it is preferred that the additional
active ingredients are non-lipophilic or non-ionic. However, for
certain embodiments, a non-ionic antibacterial agents is optionally
included in oral compositions, and may include phenolic and/or
bisphenolic compounds, such as, halogenated diphenyl ethers,
including triclosan (2,4,4'-trichloro-2'-hydroxy-diphenylether,
triclocarban (3,4,4-trichlorocarbanilide), 2-phenoxyethanol,
benzoate esters, carbanilides, phenols, thymol, eugenol, hexyl
resorcinol and 2,2'-methylene bis(4-chloro-6-bromophenol).
[0031] The active ingredient may also optionally comprise a
cationic active ingredient. In certain embodiments, the siloxane
polymer comprises an anionic group or moiety and it is desirable to
avoid strongly cationic active ingredients, because such anionic
compounds can bind to the cationic active ingredient potentially
reducing its bioavailability. In such embodiments, the oral
composition containing an anionic siloxane polymer, such as an
anionic siloxane polymer having a pendant phosphorus-containing
moiety, is substantially free of cationic active ingredients.
[0032] However, in other embodiments, cationic active ingredients
can be suitable for use in oral compositions, particularly when the
siloxane polymer is only mildly anionic or the cationic active is
only slightly cationic. In various embodiments, suitable cationic
actives include, for example, quaternary ammonium compounds, such
as, benzalkonium chloride and benzethonium chloride; pyridinium and
isoquinolinium compounds, including hexadecylpyridinium chloride;
pyrimidine derivatives such as hexetidine; amidine derivatives such
as hexamidine isethionate; bispyridine derivatives such as
octenidine. Other cationic actives include guanides, such as
bis-biguanides include chlorhexidine and alexidine. Other optional
active ingredients that are cationic compounds include N.sup.a-acyl
amino acid alkyl esters and salts, including ethyl lauroyl arginine
ester hydrochloride (ELAH).
[0033] In some embodiments, the additional active ingredient
comprises an oral care active that is a biofilm disruption agent. A
biofilm disruption agent is generally a compound that prevents
formation of and/or attacks a biofilm (or pellicle) already formed
on an oral surface and includes enzymes that can hydrolyze
proteins, starch and lipids, which form a part of a biofilm matrix.
In certain embodiments, such active ingredients are enzymes,
including by way of example, protease enzymes, such as cysteine
proteases or serine proteases. Examples are most desirably selected
from the group: papain (for example, isolated from the latex of the
green fruit and leaves of Carica papaya), ficin (for example,
isolated from the latex of tropical fig trees Ficus glabrata),
krillase (for example, isolated from Antarctic krill), other
cysteine and serine proteases, glucoamylase, dextranase, mutanase,
lysozyme, plant lipase, gastric lipase, pancreatic lipase, tannase,
bromelain, chymotrypsin, alcalase, amalysecs, lactoferrin,
gingipains, glucose oxidase, elastases and/or cellusases pectinase,
and mixtures thereof. Other exemplary biofilm disruption agents for
the oral cavity include synthetic histatin, furanone, derivatives
of furanone, and mixtures of any of the above.
[0034] Other useful oral active ingredients include fluoride ion
sources, preferably present in an amount sufficient to supply about
25 ppm to about 5,000 ppm of fluoride ions, such as sodium
fluoride, potassium fluoride, sodium fluorosilicate, ammonium
fluorosilicate, sodium monfluorophosphate (MFP), and amine
fluorides, including olaflur
(N'-octadecyltrimethylendiamine-N,N,N'-tris(2-ethanol)-dihydrofluoride).
Actives can also include stannous and/or zinc ion sources. Suitable
stannous ion sources include without limitation stannous fluoride,
other stannous halides such as stannous chloride dihydrate,
stannous pyrophosphate, organic stannous carboxylate salts such as
stannous formate, acetate, gluconate, lactate, tartrate, oxalate,
malonate and citrate, stannous ethylene glyoxide and the like. Zinc
ion sources, such as zinc acetate, zinc chlorite, zinc citrate,
zinc gluconate, zinc glycinate, zinc oxide, zinc sulfate, sodium
zinc citrate and the like are also suitable for use in oral
compositions.
[0035] Certain types of useful anticalculus active ingredients are
linear molecularly dehydrated polyphosphate salts. Polyphosphate
salts are generally employed in the form of their wholly or
partially neutralized water soluble alkali metal (e.g., potassium,
sodium or ammonium salts, and any mixtures thereof). Thus, linear
molecularly dehydrated polyphosphate compounds useful as antitartar
agents include those such as sodium tripolyphosphate, sodium
hexametaphosphate pyrophosphate, 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, and
cyclic phosphates such as sodium tripolyphosphate sodium
trimetaphosphate, or mixtures thereof. In various embodiments, such
active ingredients are present at concentrations from about 0.001
to about 10%, more preferably between about 1 to about 5% of the
composition. Polyphosphates may also be used, for example, as
active ingredients in home care and cleansing compositions, as will
be discussed in more detail below.
[0036] Synthetic anionic linear polycarboxylates are also well
known as efficacy enhancing agents for certain active ingredients,
in particular for enhancing efficacy of oral care ingredients,
including antibacterial, antitartar or other active agents within
the composition. Further, such compounds may also be used to form
films, as described below. Such anionic polycarboxylates are
generally employed in the form of their free acids, or preferably
partially neutralized or more preferably fully neutralized water
soluble alkali metal (e.g., potassium and preferably sodium) or
ammonium salts. Preferred copolymers are 1:4 to 4:1 copolymers of
maleic anhydride or acid with another polymerizable ethylenically
unsaturated monomer, preferably methyl vinyl ether
(methoxyethylene) having a molecular weight (M.W.) of about 30,000
to about 5,000,000. One preferable copolymer is
methylvinylether/maleic anhydride. Examples of these copolymers are
available from ISP Corporation, Wayne, N.J., United States of
America, under the trade name GANTREZ.RTM., e.g., AN 139 (M.W.
1,100,000), AN 119 (M.W. 200,000); S-97 Pharmaceutical Grade (M.W.
1,500,000), AN 169 (M.W. 2,000,000), and AN 179 (M.W. 2,400,000);
wherein the preferred copolymer is S-97 Pharmaceutical Grade (M.W.
1,500,000). In various embodiments where a synthetic anionic
polycarboxylate is included in the composition, it is preferably
present from about 0.001% to about 5% weight
[0037] Saliva stimulating agents are other conventional active
ingredients and include food acids such as citric, lactic, maleic,
succinic, ascorbic, adipic, fumaric and tartaric acids, and
mixtures thereof. H.sub.2 histamine receptor antagonists are other
useful active ingredients. H.sub.2 antagonists useful herein
include cimetidine, etintidine, ranitidine, ICIA-5165, tiotidine,
ORF-17578, lupititidine, donetidine, famotidine, roxatidine,
pifatidine, lamtidine, BL-6548, BMY-25271, zaltidine, nizatidine,
mifentidine, BMY-52368, SKF-94482, BL-6341A, ICI-162846,
ramixotidine, Wy-45727, SR-58042, BMY-25405, loxtidine, DA-4634,
bisfentidine, sufotidine, ebrotidine, HE-30-256, D-16637, FRG-8813,
FRG-8701, impromidine, L-643728, HB-408.4, and mixtures thereof.
Desensitizing agents useful herein include potassium citrate,
potassium chloride, potassium tartrate, potassium bicarbonate,
potassium oxalate, potassium nitrate, strontium salts, and mixtures
thereof.
[0038] The oral compositions of the present invention can
optionally comprise other anti-plaque/plaque disrupting agents in
addition to those set forth above, including without limitation:
copper, magnesium, and strontium ion sources, typically provided in
salt form; dimethicone copolyols such as cetyl dimethicone
copolyol; urea; calcium lactate; calcium glycerophosphate;
strontium polyacrylates; and mixtures thereof.
[0039] In certain embodiments, the active ingredient is an
anti-inflammatory agent. Certain useful anti-inflammatory compounds
include flavonoids, flavans, parthenolides, such as sesquiterpene
lactone parthenolides, androstenediol (AED) and
dehydroepiandrosterone (DHEA). Other useful anti-inflaimnatory
agents are non-steroidal anti-inflammatory drugs (NSAIDs). Examples
of useful NSAIDs include indomethicin, flurbiprofen, ketoprofen,
ibuprofen, naproxen, meclofenamic acid, and mixtures thereof. Other
suitable anti-inflammatory agents useful for oral care active
agents include oregano extract (for example, extracts from Origanum
vulgare (commonly known as "oregano", "wild oregano", or "wild
marjoram")) as disclosed in U.S. patent application Ser. No.
11/256,788 to Worrell et al., filed Oct. 24, 2005, or magnolia
extract, derived from plants in the Magnoliacene family, such as
Magnolin Officinalis as described in U.S. patent application Ser.
No. 11/285,809 to Gaffar et al., filed Nov. 23, 2005. Alternatively
or in addition, a local or systemic analgesic such as aspirin,
codeine, acetaminophen, sodium salicylate or triethanolamine
salicylate can be used.
[0040] Further, a suitable anti-inflammatory active ingredient safe
for oral care compositions comprises a combination of at least one
flavonoid and at least one flavan, such an example is
UNIVESTIN.RTM., which is manufactured and sold by Unigen
Pharmaceuticals, Inc., Superior, Colo., United States of America. A
full description of UNIVESTIN.RTM. can be found in United States
Patent Application Publication No. 2003/0216481 to Jia.
[0041] Exemplary antioxidants useful as active ingredients include
butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT),
vitamin A, carotenoids, tocopherols (vitamin E), flavonoids,
polyphenols, ascorbic acid (vitamin C), herbal antioxidants,
chlorophyll, melatonin, chloride, calcium, calcium oxide, calcium
chloride, disodium ubiquinone (coenzyme Q.sub.10), ethylhexyl
gallate, hydrogen peroxide (also useful as a whitening agent),
iodine, lycopene, magnesium ascorbate, potassium sulfite, sodium
bisulfite, thiolactic acid, and mixtures thereof. These active
ingredients are also used in personal care and cleansing
compositions.
[0042] In certain embodiments, the compositions comprise active
ingredients that are antibiotics, such as augmentin, amoxicillin,
tetracycline, doxycycline, minocycline, metronidazole, neomycin,
kanamycin and clindamycin; and mixtures thereof.
[0043] Suitable nutrients include vitamins, minerals, amino acids,
and mixtures thereof. Vitamins include Vitamins C and D, thiamine,
riboflavin, calcium pantothenate, niacin, folic acid, nicotinamide,
pyridoxine, cyanocobalamin, para-aminobenzoic acid, bioflavonoids,
and mixtures thereof. Nutritional supplements include amino acids
(such as L-tryptophan, L-lysine, methionine, threonine,
levocarnitine and L-carnitine), lipotropics (such as choline,
inositol, betaine, and linoleic acid), fish oil (including
components thereof such as omega-3 (N-3) polyunsaturated fatty
acids, eicosapentaenoic acid and docosahexaenoic acid), and
mixtures thereof.
[0044] The oral compositions are preferably provided in an orally
acceptable carrier or vehicle. The carrier can be a liquid,
semi-solid, or solid phase, in the form of a mouth rinse,
dentifrice (including toothpastes, toothpowders, and prophylaxis
pastes), confectionaries (including lozenges, and gum), medicament,
film, or any other form known to one of skill in the art. Selection
of specific carrier components is dependant on the desired product
form.
[0045] By way of example, the compositions comprising the siloxane
active material can be provided in an oral care composition, which
can be in the form of a dentifrice, such as toothpastes,
toothpowders, and prophylaxis pastes, confectionaries, including
gums, beads and chews, films, paint-on products, professional
polishing formulations or any other form known to one of skill in
the art.
[0046] In various embodiments, an orally acceptable dentifrice
carrier used to prepare an oral composition comprises a
water-phase. Conventional ingredients that can be used to form the
carriers listed above are well known to the skilled artisan. As
recognized by one of skill in the art, the oral compositions
optionally include other materials in addition to those components
previously described, including for example, surface active agents,
such as surfactants, emulsifiers, and foam modulators, viscosity
modifiers and thickeners, humectants, diluents, pH modifying
agents, emollients, moisturizers, mouth feel agents, sweetening
agents, flavor agents, colorants, preservatives, solvents, such as
water and combinations thereof. It is understood that while general
attributes of each of the above categories of materials may differ;
there may be some common attributes and any given material may
serve multiple purposes within two or more of such categories of
materials. Preferably, such carrier materials are selected for
compatibility and stability with all of the constituents of the
active ingredient, including siloxane polymer and any additional
active compounds selected for the oral composition.
[0047] Typical useful surface active agents are disclosed in the
patent references referenced and discussed above, including in U.S.
Pat. No. 4,894,220 and U.S. patent application Ser. No. 11/256,788
to Worrell. Surface active agents generally are an important aspect
of the oral composition, as they can function as surfactants,
emulsifiers foam modulators, and/or active ingredient dispersion
agents. For example, in embodiments where the oral composition has
an active ingredient comprising an anionic active ingredient, it is
preferred that the carrier comprises surfactants that are not
strongly cationic, as such anionic compounds can bind to the
cationic active ingredient potentially reducing its
bioavailability. Depending on the chemical composition of the
siloxane polymer (for example, the identity of the R.sub.1 and
R.sub.2 groups identified in Formula I above), the siloxane polymer
may have anionic portions or characteristics. Thus, where the
siloxane polymer has an anionic character in certain embodiments,
it is preferred that the carrier is substantially free of
non-compatible surfactants, such as strongly cationic
surfactants.
[0048] Generally, suitable surface active agents for oral carriers
are those which are reasonably stable and foam throughout a wide pH
range. These compounds are well known in the art, and include
non-soap anionic (e.g., sodium lauryl sulfate (SLS), N-myristoyl,
and N-palmitoyl sarcosine), nonionic (e.g., Polysorbate 20
(polyoxyethylene 20 sorbitan monolaurate, TWEEN.RTM. 20) and
Polysorbate 80 (polyoxyethylene 20 sorbitan mono-oleate, TWEEN.RTM.
80), Poloxamer 407, available under the trade name PLURONIC.RTM.
F127 from BASF Corporation, Florham Park, N.J., United States of
America, cationic, zwitterionic (e.g., cocoamidopropyl betaine and
lauramido propyl betaine), and amphoteric organic synthetic
detergents. In embodiments where the active ingredient comprises an
anionic compound, the surface active agent is preferably selected
from the group consisting of: non-ionic surfactants, anionic
surfactants, amphoteric surfactants and mixtures thereof. In
certain embodiments, one or more surface active agents are present
in the oral composition in the range from about 0.001% to about 5%,
preferably from about 0.5% to about 2.5%.
[0049] Any suitable flavoring or sweetening material may also be
employed. Examples of suitable flavoring constituents are flavoring
oils, e.g. oil of spearmint, peppermint, wintergreen, sassafras,
clove, sage, eucalyptus, marjoram, cinnamon, lemon, lime, orange,
grapefruit, and methyl salicylate. Also useful are such chemicals
as menthol, carvone, and anethole. Suitable sweetening agents
include sucrose, lactose, maltose, sorbitol, xylitol, sodium
cyclamate, perillartine, AMP (aspartyl phenyl alanine, methyl
ester), saccharine and the like. As discussed above, in certain
embodiments, the oral compositions are substantially free of
lipophilic agents, such as lipophilic flavorants. However, in
certain embodiments, the flavor and sweetening agents may each or
together be incorporated into the oral composition at a
concentration of about 0.05 to about 5% and preferably about 0.5 to
about 1.5%.
[0050] In embodiments where the oral composition is in the form of
a mouthrinse an exemplary carrier is substantially liquid. The term
"mouth rinse" includes mouth washes, sprays, rinses, and the like.
In such a preparation, the orally acceptable carrier typically has
an aqueous phase comprising either water, or a water and alcohol
mixture. Further, in various embodiments, the oral carrier
typically has a humectant, surfactant, and a pH buffering
agent.
[0051] In embodiments where the oral composition is in the form of
a confectionary, an exemplary carrier is substantially solid or
semi-solid. Confectionary carriers are well known in the art. For a
lozenge, the carrier typically comprises a lozenge base material
(for example, comprising a non-cariogenic polyol and/or
starch/sugar derivative), an emulsifier, a lubricant, a flavoring
agent, a thickener, and optionally, a coating material. Chewing gum
carriers generally have a chewing gum base, one or more
plasticizing agents, a sweetening agent, and a flavoring agent.
[0052] In embodiments where the oral composition is in the form of
a film, an exemplary carrier is substantially solid or semi-solid.
Generally, such film carriers comprise a water soluble or
dispersible film forming agent, such as a hydrophilic polymer.
Optionally, the film carrier may also comprise hydrophobic film
forming polymers, either as a removable backing layer, or mixed
with a hydrophilic film forming polymer. Film carriers optionally
comprise plasticizers, surface active agents, fillers, bulking
agents, and viscosity modifying agents.
[0053] In embodiments where an oral composition is in the form of a
dentifrice, an exemplary carrier is substantially semi-solid or a
solid. Dentifrices typically contain surface active agents,
humectants, viscosity modifying agents and/or thickeners,
abrasives, solvents, such as water, flavoring agents, and
sweetening agents.
[0054] In various embodiments, an oral composition may be provided
within a single component or phase. In other embodiments, the oral
composition includes both a first and a second component that are
separately maintained. Maintaining the components separately
requires only that the components are maintained in such a way as
to substantially prevent the interaction of one component of the
oral composition with another component of the oral composition.
Typically, a dual component oral composition is employed where
there are one or more incompatible ingredients included in the oral
composition. For example, if the active ingredient comprises a
siloxane polymer ingredient that has an anionic nature, it is
advantageous to separately maintain cationic compounds from
strongly anionic components. The separation of components can be
accomplished through any means known or to be discovered in the art
and includes chemical, physical, and mechanical means of separation
of any combination of these. For example, the first and second
components may be combined but certain components are separately
maintained by wrapping or encapsulating one or both in a film,
coating, capsule, micelle, and the like.
[0055] Thus, any of the various embodiments of the oral care
composition described above are contacted with or applied regularly
to an oral surface, preferably at least one time a day, more
preferably on multiple days in a week, and most preferably on a
long-term daily basis.
[0056] The oral compositions may be prepared by suitably admixing
the various ingredients. For instance, in the preparation of a
mouthrinse, the siloxane polymer is dispersed in an aqueous solvent
and/or alcohol and then added to a mixture of humectants,
surfactants, and water. The resulting rinse product is then
packaged.
[0057] Dentifrices are typically prepared by adding various salts
(including fluoride salts, when included in the composition), and
sweeteners (e.g., saccharin), and any water-soluble oral care
active ingredient compounds to water, where it is mixed. Into
another container, all humectants, gums, and polymers, including
the siloxane polymer ingredient, are added together. The water
based mixture described above is added to the container with the
humectants, gums, and polymers. The combined ingredients are
optionally heated to a temperature of greater than about 40.degree.
C., for example from about 60.degree. C. to about 70.degree. C., to
disperse the gums and polymers. The heated mixture is then cooled
to less than approximately 38.degree. C. (about 100.degree. F.).
The mixture is then combined with abrasives, where it is mixed at
high speed under a vacuum for about 15 to about 20 minutes. Any
flavor oil and any lipophilic oral care active ingredients are
admixed. This mixture is admixed to the water based mixture above,
where it is mixed under high speed and vacuum until sufficiently
dispersed. The surfactant(s) are added and the mixture is again
mixed to disperse. The siloxane polymer may optionally be added
with the surfactants, rather than into the polymer phase.
[0058] The oral composition can be incorporated into confectionary
and tropes. Such methods of forming confectionary (e.g., gum) or
tropes (e.g., lozenges) are well known by one of skill in the art,
and can be prepared by stirring the other oral care active
compound(s) into a warm gum base or coating the outer surface of a
gum base (for example, jelutone, rubber latex, vinylite resins,
inter alia), desirably with conventional plasticizers or softeners,
sugar or other sweeteners or carbohydrates such as glucose,
sorbitol and the like. Preferably, the siloxane polymer is added to
the gum base.
[0059] Where the oral composition is in the form of a film, it can
be formed by any number of conventional film forming processes,
such as conventional extrusion or solvent casting processes. For
example, to prepare a film by solvent casting, a film forming
polymer is dissolved in a sufficient amount of a solvent which is
compatible with the polymer. After a solution has been formed, a
plasticizer can be added with stirring, and heat can be applied, if
necessary, to aid dissolution, until a clear and homogeneous
solution has been formed, followed by the addition of the active
ingredients, including the siloxane polymer, surface active agents,
bulking agents, and any other ingredients such as flavors and
sweeteners. For ease of use, the dry film can be cut into pieces of
suitable size and shape and packed into a suitable container.
[0060] The following examples further describe and demonstrate
various embodiments contemplated by the disclosure.
EXAMPLE I
[0061] Three oral compositions are prepared in accordance with
various embodiments of the disclosure, with each containing a
distinct siloxane polymer having a hydrophilic portion. Two
compositions designated "Composition A" and "Composition B" contain
siloxane polymer having phosphorus-containing moieties, namely the
PECOSIL.RTM.WDS-200 and PECOSIL.RTM. PS-100, respectively.
"Composition C" contains a siloxane polymer comprising a
hydrophilic portion having polyethylene and polypropylene oxide,
namely DC-190. Each of these polymers was fully described above.
Compositions A, B, and C are prepared using the ingredients listed
in Table I. Additional active ingredients included in the
composition are tetrasodium pyrophosphate (an anti-calculus active
ingredient) and sodium fluoride (an anticaries active
ingredient).
TABLE-US-00001 TABLE I Toothpaste formula with silicone (Weight %)
Composition A B C Polyethylene glycol 3.0 3.0 3.0 Sodium CMC 0.6
0.6 0.6 Tetrasodium pyrophosphate 0.5 0.5 0.5 Purified water q.s.
q.s. q.s. Sodium fluoride 0.243 0.243 0.243 Sorbitol 53.9 53.9 53.9
Sodium saccharin 0.3 0.3 0.3 ZEODENT .RTM. 115 25.5 25.5 25.5
Sodium lauryl sulfate 1.2 1.2 1.2 WDS-200 1.0 0 0 PS-100 0 1.00 0
DC-190 0 0 1.00 FD&C Blue #1 1% solution 0.16 0.16 0.16 Flavor
0.72 0.72 0.72 Total 100 100 100
[0062] Dentifrice compositions containing the siloxane polymers
having at least one hydrophilic region have good antiplaque
activity. The oral compositions are applied to one or more oral
surfaces in the oral cavity, and promote overall oral health,
including inhibition of plaque formation, gingivitis,
periodontitis, caries, and the like. For example, where an oral
care composition comprises a siloxane polymer having at least one
hydrophilic region, the oral composition effectively inhibits
plaque formation and growth of various oral bacteria on an oral
surface. In certain embodiments, the oral composition further
provides at least one of: antitartar, anti-caries, biofilm
disruption and/or anti-inflammatory activity. Thus, certain oral
compositions provide multiple oral care benefits
simultaneously.
* * * * *