WO1995009603A1

WO1995009603A1 - Calciumperoxide-bicarbonate oral composition

Info

Publication number: WO1995009603A1
Application number: PCT/US1994/011204
Authority: WO
Inventors: Thomas Edward Huetter; Cheryl Therese Ruffin
Original assignee: The Procter & Gamble Company
Priority date: 1993-10-04
Filing date: 1994-10-03
Publication date: 1995-04-13
Also published as: CA2173110A1; CN1136772A; PL313796A1; JPH09503508A; HUT74081A; AU7964494A; PE30695A1; BR9407743A; HU9600867D0; CZ98796A3; EP0722311A1

Abstract

Oral compositions comprising a first calcium peroxide containing component and a second bicarbonate containing component.

Description

Calciumperoxide-bicarbonate oral composition

BACKGROUND OF THE INVENTION Oral compositions utilizing a peroxide component and a bicarbonate component have been disclosed. The most widely used peroxide has been hydrogen peroxide and the peroxide and the bicarbonate have been physically separated prior to use. Patents disclosing executions of this type include U.S. Patents 4,849,213 and 4,528,180 to Schaeffer. These compositions deliver benefits in the antipiaque and antigingivitis areas. Other benefits may also be provided.

While peroxide executions have been developed, there is still the need for additional products which provide for additional benefits or ease of manufacture. The present inventors have found that products based on calcium peroxide can provide excellent performance when used with a bicarbonate salt.

It is an object therefore of the present invention to provide a calcium peroxide-bicarbonate dual-component composition.

A further object of the present invention is to provide compositions which deliver a variety of benefits to the mouth such as those described above. These and other objects of the present invention will become more readily apparent from the more detailed description and examples which follow.

All percentages and ratios used herein are by weight unless otherwise specified. Also, all measurements referred to herein are made at 25°C in the compositions unless otherwise specified. SUMMARY OF THE INVENTION

The present invention, in one of its aspects, relates to an oral composition comprising:

(A) a first component comprising:

(1) calcium peroxide present in an amount of from about .05% to about 10.0% of the first component; and

(2) a suitable carrier; and

(B) a second component comprising:

(1) a bicarbonate salt present in an amount of from about 1.0% to about 60.0% of the second component; and (2) a suitable carrier wherein components A and B are held in separate areas of a container containing the components prior to use . Examples of containers suitable for use in the present invention are described in US Patents 4 , 849 , 213 and 4 , 528 , 180 to Schaeffer . By "oral compositions" as used herein means a product which in the ordinary course of usage is not intentionally swallowed for purposes of systemic administration of particular therapeutic agents, but is rather retained in the oral cavity for a time sufficient to contact substantially all of the dental surfaces and/or oral tissues for purposes of oral activity.

By "safe and effective amount" as used herein means sufficient amount of material to provide the desired benefit while being safe to the hard and soft tissues of the oral cavity.

By the term "comprising", as used herein, is meant that various additional components can be conjointly employed in the compositions of this invention as long as the listed materials perform their intended functions.

By the term "carrier" as used herein- is meant a vehicle which is suitable for use to apply the present compositions in the oral cavity.

DETAILED DESCRIPTION OF THE INVENTION The present invention in a certain aspect involves a composition containing a bicarbonate salt component and a second composition containing a calcium peroxide component. The essential and optional components of the compositions are set forth in detail below. Bicarbonate Sah An essential component of the present invention is a bicarbonate salt.

Preferred salts are alkali metal salts such as sodium and potassium. The most preferred bicarbonate salt is sodium bicarbonate which is a staple item of commerce. The bicarbonate is used at a level of from about 1.0% to about 60%, preferably from about 10% to about 30%. Calcium Peroxide

A second essential component of the present invention is calcium peroxide. This material is used at a level of from about 0.05% to about 10%, preferably from about 1.0% to about 5.0%. Additional Components Water may also be present in the two compositions of this invention.

Water employed in the preparation of commercially suitable compositions should preferably be deionized and free of organic impurities. Water generally comprises from about 10% to 50%, preferably from about 20% to 40%, by weight of the toothpaste compositions herein. These amounts of water include the free water which is added plus that which is introduced with other materials as with sorbitol. The compositions of the present invention may contain in addition to the above-listed components many others which will be somewhat dependent on the type of composition (toothpastes, topical gels, prophylaxis pastes and the like). Toothpastes are the preferred systems with toothpastes being the most preferred.

Toothpastes contain as a major component an abrasive. The abrasive polishing material contemplated for use in the present invention can be any material which does not excessively abrade dentin. These include, for example, silicas including gels and precipitates, calcium carbonate, dicalcium orthophosphate dihydrate, calcium pyrophosphate, tricalcium phosphate, calcium polymetaphosphate, insoluble sodium polymetaphosphate, hydrated alumina, and resinous abrasive materials such as paniculate condensation products of urea and formaldehyde, and others such as disclosed by Cooley et al. in U.S. Patent 3.070.510. December 25, 1962, incorporated herein by reference. Mixtures of abrasives may also be used.

Silica dental abrasives, of various types, can provide the unique benefits of exceptional dental cleaning and polishing performance without unduly abrading tooth enamel or dentin. Silica abrasive materials are also exceptionally compatible with sources of soluble fluoride and other ion sources. For these reasons they are preferred for use herein.

The silica abrasive polishing materials useful herein, as well as the other abrasives, generally have an average particle size ranging between about 0.1 and 30 microns, preferably S and IS microns. The silica abrasive can be precipitated silica or silica gels such as the silica xerogels described in Pader et al., U.S. Patent 3.538.230. issued March 2, 1970 and Digiulio, U.S. Patent 3.862.307- June 21, 197S, both incorporated herein by reference. Preferred are the silica xerogels marketed under the tradename "Syloid" by the W. R. Grace & Company, Davison Chemical Division. Preferred precipitated silica materials include those marketed by the J. M. Huber Corporation under the tradename "Zeodent", particularly the silica carrying the designation "Zeodent 110". These silica abrasives are described in U.S. Patent 4.340.583. July 29, 1982, incorporated herein by reference.

The abrasive in the dentifrice compositions described herein is present at a level of from about 6% to about 70%, preferably from about 15% to about 30% when the dentifrice is a toothpaste.

Flavoring agents can also be added to the dentifrice and other compositions of the present invention. Suitable flavoring agents include oil of wintergreen, oil of peppermint, oil of spearmint, oil of sassafras, and oil of clove. Sweetening agents are also useful and include aspartame, acesulfame, saccharin, dextrose, levulose and sodium cyclamate. Flavoring and sweetening agents are generally used in the compositions herein at levels of from about 0.005% to about 2% by weight. In preparing toothpastes, it is necessary to add some thickening material to provide a desirable consistency. Preferred thickening agents are carboxyvinyl polymers, carrageenan, hydroxy-ethyl cellulose and water soluble salts of cellulose ethers such as sodium carboxymethyl cellulose and sodium carboxymethyl hydroxyethyl cellulose. Natural gums such as gum karaya, gum arabic, and gum tragacanth and polysaccharide gums such as xanthan gum can also be used. Colloidal magnesium aluminum silicate or finely divided silica can be used as part of the thickening agent to further improve texture. Thickening agents in a combined amount from 0.5% to 5.0% by weight of the total composition may be used.

Surfactants are also useful in the compositions of this invention and include many different types of materials. Suitable surfactants include any which are reasonably stable and function over a wide pH range. Included are non-soap anionic, nonionic, cationic, zwitterionic and amphoteric organic synthetic surfactants. Many of these are disclosed by Gieseke et al. in U.S. Patent 4,051,234, September 27, 1988 incorporated herein in total by reference.

It is also desirable to include a humectant in a toothpaste to keep h from hardening. Suitable humectants include glycerin, sorbitol, and other edible polyhydric alcohols at a level of from about 10% to about 90%. One of the component phases of the present invention may be a gel without abrasive. The humectant is the dominant component of such component phase and the thickening is provided by a material such as a carboxyvinyl polymer.

Another optional component of the compositions of this invention is an anionic polycarboxytate which may provide an anticalculus effect. The anionic polymeric polycarboxylates optionally but preferably employed herein are well known, being employed in the form of their free acids or partially or preferably fully neutralized water soluble alkali metal (e.g., preferably sodium) or ammonium salts. Preferred 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 1,000,000. These copolymers are available for example as Gantrez AN 139 (M.W. 500,000), AN 119 (M.W. 250,000) and preferably S-97 Pharmaceutical Grade (M.W. 70,000), of GAF Corporation.

Other operative polymeric polycarboxylates include those such as the 1:1 copolymers of maleic anhydride with ethyl acrylate, hydroxyethyl methacrylate, N- vinyl-2-pyroUidone, or ethylene, the latter being available for example as Monsanto EMA No. 1103, M.W. 10,000 and EMA Grade 61, and 1:1 copolymers of acrylic acid with methyl or hydroxyethyl methacrylate, methyl or ethyl acrylate, isobutyl vinyl ether or N-vinyl-2-pyττolidone.

Additional operative polymeric polycarboxylates disclosed in above referred to U.S. Patent Nos. 4.138.477 and 4.183.914. incorporated herein by reference, include copolymers of maleic anhydride with styrene, isobutylene or ethyl vinyl ether, polyacrylic, polyitaconic and polymaleic acids, and sulfoacrylic oligomers of M.W. as low as 1,000 available as Uniroyal ND-2.

Suitable generally are polymerized olefinically or ethylenically unsaturated carboxylic acids containing an activated carbon-to-carbon olefinic double bond and at least one carboxyl group, that is, an acid containing an olefinic double bond which readily function sin polymerization because of its presence in the monomer molecule either in the alpha-beta position with respect to a carboxyl group or as part of a terminal methylene grouping. Illustrative of such acids are acrylic, methacryiic, ethacrylic, alpha-chloroacrylic, crotonic, beta-acryioxy propionic, sorbic, alpha-chlorsorbic, cinnamic, beta-styrylacrylic, muconic, haconic, c raconic, mesaconic, glutaconic, aconitic, alpha-phenyl-acrylic, 2-benzyl acrylic, 2-cyclohexylacrylic, angelic, umbellic, fumaric, maleic acids and anhydrides. Other different olefinic monomers copolymerizable with such carboxylic monomers include vinylacetate, vinyl chloride, dimethyl maleate and the like. Copolymers contain sufficient carboxylic salt groups for water-solubility.

The synthetic anionic polymeric polycarboxylate component is mainly a hydrocarbon with optional halogen and 0-containing substituents and linkages as present in for example ester, ether and OH groups, and when present is generally employed in the instant compositions in approximate weight amounts of 0.05 to 3%, preferably 0.05 to 2%, more preferably 0.1 to 2%.

Another optional component is a fluoride ion source. The sources of fluoride ions, or fluoride-providing compounds, useful according to this invention are well known in the art as anti-caries agents and pyrophosphatase inhibitors and also act as such agents in the practice of this invention. These compounds may be slightly soluble in water or may be fully water-soluble. They are characterized by their ability to release fluoride ions in water and by freedom from undesired reaction with other compounds of the oral preparation. Among these materials are inorganic fluoride salts, such as soluble alkali metal, alkaline earth metal salts, for example, sodium fluoride, barium fluoride, sodium fluor-silicate, ammonium fluorosilicate, sodium fluorozirconate, sodium onofluorophosphate, aluminum mono- and di-fluorophosphate, and fluorinated sodium calcium pyrophosphate. Alkali metal and tin fluorides, such as sodium and stannous fluorides, sodium ono-fluorophosphate (MFP) and mixtures thereof! are preferred. The amount of fluoride-providing compound is dependent to some extent upon the type of compound, its solubility, and the type of oral preparation, but it must be a nontoxic amount, generally about 0.005 to about 3.0% in the preparation. In a dentifrice preparation, e.g. dental gel, toothpaste (including cream), an amount of such compound which releases up to about 5,000 ppm of F- ion by weight of the preparation is considered satisfactory. Any suitable minimum amount of such compound may be used, but it is preferable to employ sufficient compound to release about 300 to 2,000 ppm, more preferably about 800 to about 1,500 ppm of fluoride ion. Typically, in the cases of alkali metal fluorides and stannous fluoride, this component is present in an amount up to about 2% by weight, based on the weight of the preparation, and preferably in the range of about 0.05% to 1%. In the case of sodium monofluorophosphate, the compound may be present in an amount of about 0.1-3%, more typically about 0.76%.

Other anti calculus agents are metal ions such as zinc disclosed in U.S. Patent 4.022.880. May 10, 1977 to Nmson incorporated herein by reference. Still others are polymers such as those described in U.S. Patent 4.661.341. April 28, 1987 to Benedict and U.S. Patent 3.429.963. February 25, 1969 to Shedlovsky, both of which are incorporated herein by reference. Such metals are used in an amount of from about 0.01% to about 5%, preferably about 0.1% to about 2%, while such polymers are used in amounts of from about 0.1% to about 10%, preferably from about 0.5% to about 5%.

Still other anti calculus agents are pyrophosphate salts such as di- and tetra-alkali metal pyrophosphates and others disclosed in U.S. Patent 4,999,184, March 12, 1991, to Parran et al., incorporated herein by reference. Other optional components for use in the present compositions are non- cationic water insoluble agents such as triclosan. Such materials are disclosed in U.S. 4,022,899 to Vlnson et al., incorporated herein by reference. METHOD OF MANUFACTURE The compositions of the present invention can be prepared using the method described following the Examples.

COMPOSITION USE The present invention in its method aspect involves applying to the oral cavity safe and effective amounts of the compositions. Generally, amounts of at least about 1 gram of the composition is effective.

Given below are examples representative of the present invention. They describe and demonstrate preferred embodiments within the invention's scope. The examples are given solely for the purpose of illustration and are not to be construed as limitations of this invention. Many variations thereof are possible without departing from the invention's spirit and scope.

EXAMPLE I Given below are compositions representative of the present invention:

Bicarbonate Composition

Component Paste fWt.%1

Sorbitol 40.040

Sodium Bicarbonate 20.000 Silica 15.000

Water 10.000

Glycerin 7.000

SASS 4.000

Sodium Carbonate 1.000 Flavor 1.000

CMC 0.850

Saccharin 0.517

Ti02 0.350

Fluoride 0.243 Blue Dye 0000

TOTAL 100.000

Calcium Peroxide Compositions Given below are four calcium peroxide compositions which are useful for use with the above bicarbonate composition.

OPTION #1 wτ_τ % OPTION #2 wτ, %

Sodium Fluoride 0.243 Sodium Fluoride 0.243

Saccharin 0.33 Saccharin 0.33

Citric Acid 0.2 Citric Acid 0.2

Sodium Citrate 5.59 Sodium Citrate 5.59

Calcium Peroxide 1.5 Calcium Peroxide 1.5

Triethanolamine 3 Triethanolamine 3

Carbopol 956 3 Carbopol 956 3

Flavor 0.963 Flavor 0.963

Glycerin 85.174 PEG-6 85.174

TOTAL 100.000 100.000 OPTION #3 WT % OPTION S WT. %

Sodium Fluoride 0.243 Sodium Fluoride 0.243

Saccharin 0.33 Saccharin 0.33

Calcium Peroxide 1.5 Calcium Peroxide 1.5

Poloxamer 407 20 Poloxamer 407 20

(Pluronic 127) (Pluronic 127)

Flavor 0.963 Flavor 0.963

Glycerin 76,964 PEG-6 76,964

TOTAL 100.000 TOTAL 100.000

Prior to use, the bicarbonate composition and the calcium peroxide composition must be held in separate areas of a container containing the components. Examples, of containers suitable for use in the present invention are described in US Patents 4,849,213 and 4,528,180 to Schaeffer.

Claims

What is Claimed is:

1. An oral composition comprising:

(a) a first dentifrice composition comprising:

(i) an effective amount of calcium peroxide; and (ii) a suitable carrier;

(b) a second dentifrice composition comprising:

(i) an effective amount of a bicarbonate salt; and

(ii) a suitable carrier, wherein components (a) and (b) are held in separate areas of a container containing the components prior to use.

2. An oral formulation according to Claim 1 wherein one or both compositions A and B contain an abrasive.

3. An oral formulation according to either of Claims 1 or 2 wherein one or both of compositions A and B contain a soluble fluoride ion source.

4. An oral formulation according to any of Claims 1-3 wherein the bicarbonate salt in composition B is sodium bicarbonate.

5. An oral formulation according to any of Claims 1-4 wherein one or both of compositions A and B contain an effective amount of anticalculus agent.

6. An oral formulation according to Claim 5 wherein the anticalculus agent is a pyrophosphate salt or a polyphosphate salt.

7. An oral formulation according to any of Claims 1-5 wherein one or both of compositions A and B contain an antimicrobial agent.

8. An oral formulation according to any of Claims 1-7 wherein the antimicrobial agent is triclosan.