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.

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

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

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 alcools, 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

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.

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.

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.

TABLE in EXAMPLES I-V Weight % Components I II lil 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 Polyethy-2.00 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 Silver

Aloe Vera 0.05 0.05 0.05 0.002 0.002 Gel (10X conc) 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 1 COLOR-0 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.

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 celis 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,

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: