WO1999044574A1

WO1999044574A1 - Toothpaste and mouth rinse compositions

Info

Publication number: WO1999044574A1
Application number: PCT/US1999/004971
Authority: WO
Inventors: James J. Marshall
Original assignee: Life Plus International
Priority date: 1998-03-06
Filing date: 1999-03-05
Publication date: 1999-09-10
Also published as: AU2987999A

Abstract

A composition for oral administration as a toothpaste or mouth rinse has an effective amount of one or more plant extracted polyphenols and/or an effective amount of oligomeric proanthocyanidin. The composition provides anticaries and antigingivitis benefits without necessitating the use of fluoride, and with increased stability.

Description

TOOTHPASTE AND MOUTH RINSE COMPOSITIONS

TECHNICAL FIELD

The present invention relates to toothpaste and mouth rinse compositions,

which exhibit therapeutic effects by having various components for optimum

anticaries and antigingivitis benefits.

BACKGROUND OF THE INVENTION

Recently, multiple benefit dentifrice formulations have been prepared that are

capable of addressing more than an anticaries need. These include antitartar

benefits, control of dentinal hypersensitivity and antigingivitis efficacy. The present

invention aims at a novel combination of components which provide a toothpaste

that exhibits tooth whitening as well as plaque control both with and without the use

of a fluoride compound. An oral rinse is also provided that is alcohol free, using a

combination of natural ingredients to promote oral hygiene.

SUMMARY AND OBJECTS OF THE INVENTION

It is an object of the present invention to provide a toothpaste and/or mouth

rinse composition which utilizes a combination of polyphenols, among other

ingredients, which exhibits plaque control properties.

It is a further object of the present invention to provide compositions optionally

which contain a fluoride compound, which is useful in retarding the development of

plaque/gingivitis. 2

It is a further object to provide a mouth rinse and/or toothpaste composition

which additionally includes an oligomeric proanthocyanadin (OPC).

These and other objects of the present invention are achieved by a

toothpaste composition comprising:

(a) a safe and effective amount of one or more polyphenols, and/or

(b) a safe and effective amount of oligomeric proanthocyanadin (OPC), and

(c) various optional ingredients customarily used for formulating a toothpaste or

mouth rinse such as water, humectants, sweeteners, thickeners, flavor agents,

stabilizers, abrasives, foaming agents, etc. Preferably, both OPC and the

polyphenols are used. Certain other active ingredients are preferably optionally

included in the toothpaste and/or mouth rinse; namely, aloe vera gel, colloidal silver,

and a chlorophyllin complex which have therapeutic as well as esthetic effects.

Fluoride is an optional ingredient as the toothpaste does not rely on fluoride for

effectiveness.

A mouth rinse according to the present invention comprises:

(a) A safe and effective amount of one or more polyphenols; and/or

(b) A safe and effective amount of oligomeric proanthocyanadins (OPC)

and

(c) Various ingredients customarily used for formulating a mouth rinse

such as water, sweeteners, flavor agents, preservatives, and optionally aloe vera

gel, chlorophyllin complex and colorants.

Utilizing the present invention, a toothpaste and/or mouth rinse provides

optimum anticaries and antigingivitis benefits, utilizing compounds that commonly 3 occur in plants and plant extracts, as opposed to a reactive chemical such as

fluoride. Additionally, stability is enhanced as fluoride compounds are known to loose their effectiveness with time.

DETAILED DESCRIPTION OF THE INVENTION

The compositions of the present invention include oligomeric

proanthocyanadin (OPC), as described for example in U.S. Patent No. 4,698,360

and/or a group of plant extracted polyphenols. Other optional ingredients such as

emulsifying agents, favorants, food dyes, and sweeteners can be added to the

composition. In accordance with the invention, either or both of the two key

ingredients can be used.

The oligomeric proanthocyanadins were first described by Dr. J. Masquelier,

et al., International Journal for Vitamin and Nutrition Research, Vol. 49, No. 3, pp.

307-311 (1979). This group includes the catechins and their derivatives which have

the flavan-3-ol structure. The oligomers (preferably dimers and trimers) extracted

from grape seed and/or maritime pine bark are fairly well known and commercially

available, with the oligomeric proanthocyanadins commonly referred to as OPC.

As to the OPC, this material is present in the compositions at a level of from

about 0.001 to about 0.15 weight percent, more preferably at about 0.05 weight

percent. All percentages and ratios used herein are by weight of the total

composition unless otherwise specified. OPC provides beneficial antioxidant

properties, as well as contributes to vascular health in the gum tissue.

The composition contains from about 0.001 to about 2.0%, more preferably

about 0.005-1.5% of a mixture of plant extracted polyphenols, with about 1 % most 4 preferred in a toothpaste and about 0.5% preferred in a mouth rinse. In particular, a

mixture of plant extracted polyphenols from the tannin family is used because they

provide a complementary combination of properties such as antimicrobial action,

inhibition of plaque adhesion, among other beneficial properties. From 2 to 10 such

extracts are typically combined, with about 7 preferred to optimize this

complementality. Preferably, the pH is between from about 5 to about 8.0, more

preferably from about 3.5 to about 7.2 in the toothpaste, about 4 to 5.5 in the mouth

rinse.

The composition is incorporated in a carrier, which is a paste or gel

(hereinafter simply referred to as "paste" for convenience) for the toothpaste and an

aqueous mouth rinse base for the mouth rinse. A humectant is present in the

toothpaste at a level of from about 50 to about 90%. The preferred humectant is

anhydrous glycerin, though sorbitol, as a 70 percent solution, may be substituted for

part of the glycerin. Other suitable humectants include any of the edible polyhydric

alcohols, such as polyethylene glycol.

An abrasive polishing material may be used in the toothpaste. This can be

any material which does not excessively abrade dentin. Acceptable abrasives

include, for example, silicas, including gels and precipitates thereof, insoluble

sodium polymetaphosphate, beta-phase calcium pyrophosphate, and hydrated

alumina.

Silica dental abrasives can provide exceptional dental cleaning and polishing

performance without unduly abrading tooth enamel or dentin. Silica abrasives are 5 generally compatible with sources of soluble fluoride and are preferred for use

herein, with those formulations optionally including such soluble fluoride.

The abrasive polishing materials useful herein generally have an average

particle size ranging from about 0.1 to about 30 microns, preferably about 5 to 15

microns. The abrasive is optionally present at from about 5% to about 25%,

preferably from about 7 to about 15% of the toothpaste composition.

In preparing a toothpaste, it is usually necessary to add a thickener,

sometimes referred to as a binder, to provide a desirable consistency. Many

conventional thickeners such as carboxymethyl cellulose may be used.

Furthermore, cellulose gums, hydroxyethyl cellulose and carboxyvinyl polymers may

be used in the inventive compositions. Those particularly useful in the toothpastes

described herein are carboxyvinyl polymers made by B.F. Goodrich and designated

by the trade names "Carbopol 934", "Carbopol 940", "Carbopol 941", "Carbopol 974"

and "Carbopol 980". The thickener is present in the proposed composition at a level

of from about 0.05% to about 3.0%, preferably from about 0.4 % to 1.5%.

For optimal rheological properties and dispersibility, at least one secondary

thickener/binder should be used in addition to the thickener. Among the preferred

secondary thickening agents are xanthan gum, carrageenan, colloidal magnesium

aluminum silicate and finely divided silica. Silica thickeners are particularly useful

and are preferred in the present composition. These secondary thickeners, if used,

should be present as part of the total thickener added, and comprise about 0.5 to

about 2.0% more preferably about 0.6 to about 1.4% of the composition. 6

An aqueous mouth rinse base that is primarily water and preferably alcohol

free is used to form the inventive mouth rinse. To this may be added not only the

compositions of the invention but other conventional mouth rinse ingredients.

Flavoring agents can be added to both the toothpaste and mouth rinse.

Suitable flavoring agents include, but are not limited to, oil of wintergreen, oil of

peppermint, oil of spearmint, oil of sassafras, and oil of clove. Sweetening agents

can also be used, including aspartame, acesulfame, saccharin, dextrose, levulose

and sodium cyclamate. Flavoring and sweetening agents are generally used in

toothpastes at levels of from about 0.005% to about 2% by weight. Colorants and

opacifiers, such as titanium dioxide, of course, can be included in the inventive

composition.

The toothpaste composition can also contain emulsifying surfactant agents,

preferably those which are reasonably stable and foam throughout a wide pH range,

including non-soap anionic, nonionic, cationic, zwitterionic and amphoteric organic

synthetic emulsifiers, sodium lauryl sulfate and sodium lauryl sarcosinate are

exemplary emulsifying agents.

Other optional active ingredients include those with therapeutic benefit. These

include, but are not limited to, antitartar agents, dentin desensitizers such as

potassium nitrite, and antimicrobials, such as quaternary ammonium salts, bis-

bisquanide salts, nonionic antimicrobial salts and essential oils. In particular,

colloidal silver, aloe vera gel, preferably in concentrated form (1 :10), and

chlorophyllin complex may be used in the inventive toothpaste and mouth rinse

compositions. 7

The toothpaste and mouth rinse compositions of the present invention can be

made using methods which are reasonably common to the oral products industry.

Toothpaste compositions of the present invention are used in a conventional

manner. The toothpaste compositions or slurries thereof are brushed onto dental

surfaces in amounts from about 0.2 gram to about 2 grams, and subsequently rinsed

away. During use of the toothpaste herein, pastes or slurries generally contact

dental surfaces for from about 15 seconds to about 60 seconds. It is an advantage

of the present invention that the composition is effective with or without the presence

of fluoride, and fluoride is an optional ingredient.

Similarly, the mouth rinse composition is used in the conventional manner,

rinsing once or twice a day. However, since the composition is alcohol free and

contains natural ingredients, it may be swallowed after rinsing.

The following examples further describe and demonstrate preferred

embodiments within the scope of the present invention. The examples are given

solely for illustration and are not to be construed as limitations of this invention as

many variations are possible without departing from the scope of the invention.

Examples I, II and III are toothpastes, Example IV and V are mouth rinse.

8

TABLE in

EXAMPLES I - V

Weight %

Components I II III IV V

Water, 14.84 14.84 14.24 94.37 93.87 Purified

Sorbitol 42.0 42.0 42.0 - -

(70% solution)

Glycerin 5.27 5.00 5.27 5.0 5.0

Polyethy2.00 2.00 2.00 - - lene Glycol

Titanium 1.00 1.00 1.00 - - Dioxide

Silica 28.5 28.5 28.5 0 0 Abrasive

Poly 1.0 1.0 1.5 0 0.5 Phenols

Methyl 0.01 0.01 0.01 0 0 Paraben

Xanthan 0.7 0.7 0.7 0 0 Gum

Surfactant/ 1.53 1.53 1.53 0.172 0.172 emulsifier

Sodium — 0.27 — 0 0 Fluoride

Sodium 0.50 0.50 0.50 0.15 0.15 Saccharin

Flavor 1.95 1.95 1.95 0.25 0.25 Agents

Colloidal 0.05 0.05 0.05 0.002 0.002 I Silver Aloe Vera 0.05 0.05 0.05 0.002 0.002 Gel (1 OX cone) pH Adjust/ 0.58 0.58 0.58 0 0 Buffer

Chloro- 0.02 0.02 0.02 0.002 0.002 hyllin

Complex

OPC 0 0 0.10 0.05 0.05

COLOR0 0 0 0.002 0.002

ANT

The inventive compositions preferably include the Oligomeric

Proanthocyanidins (OPC's), produced by the patented method developed by Dr.

Jack Masquelier - along with a special blend of polyphenols, known as PPE-7. The

OPC and PPE-7 have properties which relate in great part to their ability to cling to,

bind to, or otherwise interact with protein. In the mouth, these polyphenolic

materials can interact with proteins of special interest to those concerned with oral

health care.

Saliva, for example, contains glycoproteins which are building blocks for the

initial film which may form on the enamel of the teeth, eventually leading to plaque.

Bacteria, such as Streptococcus mutant, are involved in the process leading to

plaque build-up. Other materials in the mouth such as left-over food particles, dead

skin cells and sugars, can be used by these bacteria for energy and growth sources,

also playing a part in plaque build-up. Plaque itself is a hardened mucus-rich films

that can form on the teeth. Plaque can harbor bacteria on the teeth, and in so

doing, can lead to the acidification that these bacteria can cause. This acid

environment, in turn, leads to "dental caries" or cavities. 10 The polyphenols as a class are used for their tendency to be substantive to

protein, and to interfere at all the right stages of plaque formation. They can bind

with the glycoproteins in saliva, proteinaceous food particles, dead skin cells and

with bacteria. They can also bind with the protein-rich plaque, itself. Additionally,

the poly phenols can be substantive and protective to the walls of the small blood

vessels in and around the gums. The OPC's are of prime importance in supporting

the collagen tissue of the gums.

A particular blend of polyphenols can be extracted from plants from the

following group, though the invention is not limited to these: Camellia sinensis,

Docks, Golden Rod, Rhatany, Witch hazel, Birch, Prickly ash, Black walnut, Uva

Ursi, Prickly elder, Areca nut, Wood Betony, Wattle, Oak, Valones, Sumach,

Gambier, Chinese nut gall, Quebracho. By extracting a tannin fraction, one

produces the blend of polyphenols unique to the source, which can of course be

blended with other extracts to form the polyphenol ingredient used in the present

invention. These tannin based polyphenols are believed to interfere with the

enzymes to produce dental plaque.

A more preferred group would be the Wattle (Acacia sp.), Oak (Quercus sp.),

Valones (Quercus aegilops), sumach (Rhus sp.), Gambier (Uncaria gambier),

Chinese nut gall (Rhus semialata) and Quebracho (Shinopsis sp.).

The inventive compositions optionally contain Aloe Vera and Chlorophyll.

Aloe has been associated in published studies with beneficial effects relating to

reduction in localized levels of thromboxane (an arachidonic acid metabolite) which, 11 in turn, may have a positive effect on maintenance of normal healthy gum tissue.

Chlorophyll is a plant material with a history of use for control of oral odors.

It should be understood that other active ingredients such as vitamins,

minerals, pharmaceuticals or prophylactics that do not interfere with the activity of

the primary ingredients may additionally be included to enhance or add additional

beneficial effects without varying from the scope of the invention.

While preferred embodiments of the present invention have been described, it

will be understood by one skilled in the art that the invention is not so limited and

that various changes and modification may be made without varying from the scope

of the invention.

What is claimed is:

Claims

12 CLAIMS

Claim 1. A composition for use in the mouth comprising:

(a) an effective amount of one or more polyphenols; and/or

(b) a safe and effective amount of oligomeric proanthocyanadin; and

(c) a carrier.

Claim 2. The composition of claim 1 wherein the carrier is a paste which

contains water, a humectant, and a thickener.

Claim 3. The composition of claim 2 wherein the paste carrier further

contains an ingredient selected from the group consisting of sweeteners, flavor

agents, a secondary thickener, foam agents, abrasives, colorants, opacifiers,

surfactants and combination thereof.

Claim 4. The composition of claim 1 further comprising an ingredient

selected from the group consisting of aloe Vera gel, colloidal silver, antitartar agents,

dentin desensitizers, antimicrobials, Chlorophyllin complex and combinations

thereof.

Claim 5. The composition of claim 1 wherein from 0.001 to 0.15 weight

percent OPC is used.

13 Claim 6. The composition of claim 1 wherein from 0.001 to about 2.0 wt.

percent plant extracted polyphenols is used.

Claim 7. The composition of claim 1 further comprising soluble fluoride and a stabilizer.

Claim 8. The composition of claim 1 wherein the carrier is an aqueous mouth

rinse base.

Claim 9. The composition of claim 8 wherein the aqueous mouth rinse base

contains an ingredient selected from the group consisting of sweeteners, flavor

agents, colorants, surfactants and combinations thereof.

Claim 10. The composition of claim 8 wherein the aqueous mouth rinse base

has an active ingredient selected from the group consisting of colloidal silver,

antittartar agents, dentin desensitizers, antimicrobials, Chlorophyllin complex and

combinations thereof.

Claim 11. A method for reducing gingivitis and caries comprising contacting

tooth surfaces and mouth tissue surfaces with a composition having a safe and

effective amount of one or more polyphenols, and/or a safe and effective amount of

oligomeric proanthocyanidins in a carrier.

14 Claim 12. The method of claim 11 wherein the carrier is a paste carrier and

further comprising applying the composition to a brush, and contacting the tooth

surfaces and mouth tissue surfaces using the brush.

Claim 13. The method of claim 11 wherein the carrier is an aqueous mouth

rinse base and further comprising orally administering the composition and rinsing

the mouth with the composition.

Claim 14. The method of claim 11 wherein the composition has from 0.001 to

0.15 wt. percent OPC.

Claim 15. The method of claim 11 wherein the composition has from 0.001 to

2.0 wt. percent plant extracted polyphenols.

Claim 16. The method of claim 11 wherein the composition further comprises

an active ingredient selected from the group consisting of colloidal silver, antittartar

agents, dentin desensitizers, antimicrobials, Chlorophyllin complex and

combinations thereof.