Oral treatment and manufacture of an oral composition

ORAL COMPOSITIONS "M-OMM ·. . j - II · f - -

TECHNICAL FIELD * The present invention relates to oral compositions, toothpaste, toothpaste and oral washing liquids which have a good effect on the tooth stone (both inorganic and organic).

BACKGROUND OF THE INVENTION * Tooth stone, or otherwise tartar as it is sometimes called, is a deposit or formed on the surface of the tooth at the margin of the gum. * The stone above the gum mainly appears in the areas around the salivary glands * e.g., on the surface of the tongue on the lower front and on the upper side. surfaces of the posterior molars (bank).

* The mature stone of the columns consists of an inorganic part of which is predominantly calcium phosphate arranged in a crystalline structure of a hydrogeapatite, similar to that of the structure.

There is also an organic part consisting of exfoliated epithelial cells, white cells, saliva sediment, food residues and various types of microorganisms.

As it grows, the mature stone becomes visible in white or yellowish color except if it forms spots or if discolored by any external medium. * While they are both bad and undesirable for aesthetic appeal, mature stone deposits are potential sources of gum irritation.

* A variety of chemical and biological agents have been prioritized by the art for delaying stone formation or for removing stone after its formation. * Mechanical removal of this material periodically from dentists, of course, is a standard procedure in the dental office.

The chemical process for blocking the stone generally comprises the formation of a chemical compound with calcium ion and / or the inhibition of the growth of the crystal or crystalline compound.

-3 stone is formed and / or crushed in rubble by removal of calcium.

The prior art describes a variety of chelating agents for this purpose. U.S. Patent 490,584, February 15, 1957 "describes (discloses) oral compositions containing ethylenediaminetetraacetic acid, yttrilotriacetic acid and related compounds as lithium. U.S. Patent 5,678,154, July 18, 1982 to WIDDER ET AL discloses oral compositions containing certain polyphosphates and fluoro compounds. U.S. Patent 5,737, 555, 5, June 1975 to FRANCIS provides oral compositions containing certain carbonyl bisphosphonates.

* In addition to the above references, the prior art discloses both liquid toothpastes and mouthwashes having soluble pyrophosphates which have been indicated for a variety of purposes. A. 2,941,926, June 21, I960 to Salzman et al., Which announces dental powders containing chlorophyll and pyrophosphates. U.S. Patent 5,376,632, June 16, 1964 to SCHIRALDI discloses toothpaste containing pyrophosphates. The U.S. Patent Nos. 209 and 202_L.December 6, 1975;

BAINES ET AL and HARVEY ET AL, toothpastes which use soluble pyrophosphates as detergents. Shipwreck [Inventory_HEAD_L.A_4_₁244_₁93I_L.January 2, 1981 and 4,247,526, January 27, 1981 to JARVIS et al for pyrophosphates in calcium pyrophosphate systems. * Japanese Patent Application.

‘

4945-1974 announces soluble pyrophosphates; a v / i- i) dt 'variety of toothpaste systems. U.S. Patent 4,555,55, April 6, 1982 to PARRAN discloses tetraalkali metal salts in liquid mouthwash compositions. Finally DRAUS, LESNIEWSKI and MIKLOS, PYROPHOSPHATE and HEXAMETAPHOSPHATE EFFECTS IN VITRO CALEULUS FORMATION * ARCH. ORAL BIOL, Volume 15, p. 895-896 (I970) An in vitro (IN VITRO) ineffective soluble pyrophosphate against stone.

however, they report that pyrophosphates can be inhibited by pyrophosphatase in vivo. J

Despite the many announcements in the anti-stone sector and in the pyrophosphate sector, or inadequate, an ineffective anti-stone product still exists. Unexpectedly mixtures of certain pyrophosphates can give a safe and effective product without also presenting difficult formulation problems.

It is an object of the present invention to provide compositions which have an effective beneficial effect on the stone of the road.

It is a further object of the present invention to provide an ineffective anti-inflammatory stone product using a mixture of soluble pyrophosphates.

It is still a further object of the invention to provide an effective method for treating stone gum.

This and other objects will become more apparent from the detailed description which follows.

All percentages and ratios used are given by weight unless otherwise specified.

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i

This invention includes an oral composition in the form of a mouthwash, a wet toothpaste or a toothpaste comprising:

(a) from about 0 ° /_The up to about 7 ° /₀ a toothbrush excavator selected from the group consisting of silica, alumina, calcium pyrophosphate, insoluble metaphosphates and thermosetting polymeric resins *

(b) an amount from a fluorine source is sufficient to provide about 50 parts per million to 3500 parts per million fluoride ions;

C) an amount of a soluble pyrophosphate of a salt selected from the group consisting of dialkali metal pyrophosphates and mixtures of dialkali metal and tetraalkali metal sufficient to give at least about 1.5 ° /._The PgO? "^ And

D) about 2 ° /_Q up to about 95 ° /_The water wherein the pH of said composition is from about 6.0 to about 10.0 and the composition does not contain more than about 4.0 * The present invention also comprises a method for delaying the growth of the stone.

• 6 DETAILED DESCRIPTION OF SURFACE3

The essential as well as potential components of the compositions of the present invention are described in the following paragraphs:

* Toothbrush

The abrasives useful in the form of a toothpaste composition of the present invention include many different materials. Calcium pyrophosphate may be used, including the β-phase calcium pyrophosphate prepared in accordance with the teaching of SCHWEIZER, U.S. Pat. 5,112,247, November 26, 1965. The β-phase calcium pyrophosphate is prepared by heating the γ-phase calcium pyrophosphate at 7 ° C to 9 ° C to vary at least 5 ° C._The of the γ-phase in the β-phase and then by direct diffusion, Another class of excipients for use herein are the detailed polymeric thermosetting resins as described by COOLEN et al. December 5, 1962. Suitable resins include, e.g. melanin, phenolic resins, urea, melamine urea, melaminoformaldehyde, urea-formaldehyde, melamine-urea-formaldehyde, cross-linked epoxides, and polyesters with cross-linked.

Dental toothpaste silicas are also useful in the present compositions. The non-abrasive silica-like silicone materials have a mean particle size varying

<img file="GR79211B_D0002.tif" />

-7 to about 0.1 to 3 microns, preferably 5 to 15 microns. The disintegrants may be precipitated silica or silica gels such as the silica gels which are described in PADER et al. Silicone drywallers are preferred to those offered under the brand name STLOID under WR GRACE and COMPANY, DAVISON CHEMICAL DIVISION. Also preferred are precipitated silica materials such as those pre-branded under J.M. HUBER CORPORATION under the trademark '' ZEODENT ''.¹. The types of non-abrasive silicas for teeth which are useful in the toothpastes of the present invention are described in greater detail in DIGIULIO, U.S. Patent No. 3,862,307 *. upside down.

Other suitable disinfectants include alumina and insoluble metaphosphates such as insoluble sodium metaphosphate (IMP). It is also possible to use mixtures also of unsodium. In any event, the total amount of disinfectants in the toothpaste embodiments of this invention may range from 0 ° / s._Q up to 7 ° /₀ on the weight of the toothpaste. Preferably the toothpaste contains from 10 ° to 5 ° /₀ by weight abrasive.

Preferred abrasives are β-phase pyrophosphate calcium of U.S. patent 3,112,247; fluorinated insoluble metaphosphates; U.S. patent resinous abrasives. 3, Fig. 510; and the non-abrasive silica as long as these are more compatible with other media. Most preferred are non-abrasive silica.

V source of fluoride ions

The second basic component of the present compositions is a source of fluoride ions. * The number herein is large and includes those disclosed in U.S. Patent 5,555, 421, October 20, 1977 to BKINEB et al., Incorporated herein by air. ^ substandard materials include:

Stannous fluoride, potassium fluoride, lithium fluoride, cesium fluoride, ammonium fluoride, aluminum fluoride, fluoride didyyamon copper, fluoride iydiou, fthoriozirkouikou tin fluoride, lead fluoride, ferric fluoride, nickel fluoride poilladion, silver fluoride, zinc fluoride, fluoride zirkdnion, acylamide hydrofluorate, daphylamine hydrofluorate, myristylamine hydrofluorate, decanolamine hydrofluorate, octadecylamine hydrofluoride, myristoxyamiyi hydrofluoride, hydrofluoride diaithylamiyoaithylooktoulamidi, hydrofluoric diaithanolaminoaithyloeleflamidi, diydrofthoriki d 'chithanslaminopropyl-N-oktadekenylamini, diydrofthoriki I-ethane-2-exadekylimidazolini, hydrofluoric oktoulaithanolamini fluoride oktylotrimethylammoyion fluoride dodekyoaithylodimethylamimoniou, tetraethylammonium fluoride, tetraethylammonium fluoride, fluorinated didafnylodimethylammonion fluoride IV -oktadekenylovenzylodimethylammoyion , Fluorinated diokrylodiaithylammoniou fluoride kykloezyloketylodimethylammouiou fluoride fourfourylodafnylodimethylammonion fluoride fainoxyaithyloketylodimethylammonion, bifluoride N: N * tetramethyl-N: N; -didafyyloaithylenodiammdnion fluoride, N-cetylpyridinium fluoride, N: N-didafyyl-morpholinium fluoride, N-myrystyl-N-ethylmorpholinium, N- (octylaminocarbonylethyl) -N-bezyl-dimethylammonium fluoride, N (β-hydroxydodecyl)-trimethylammonium fluoride, N-phenyl-N-hexadecyl diethyl fluoride,

N-cyclohexyl-N-octadecyl dimethylammonium-9-fluoride, N- (2-carbomethoxyethyl) -N-bezyl-dimethylammonium fluoride, N- (2-carboxy | 2-carboxy | -dodek.ylodimethylammoyion, fluoride N- / ~ 2- (N, N * -dimethylaminokarvouyl)) - aithyl_7-N-dodekylodiaithylammoniou, fluoride, N-carboxymethyl-N-eikosylodimethylammoyion, hydrofluoride betaine, sarkosiyokassiteron fluoride, fluoride alaninokassiterou, fluoride glykinokaliou, glycosine hydrocarbon fluoride, lysine hydrofluorate, alanine hydrofluoride, beta-azodicar fluoride, sodium monofluorophosphate, and mixtures thereof. Sodium fluoride is the preferred source of fluoride.

The amount of the fluoride ion source should be sufficient to provide approximately 50 parts per million to 3500 parts ti&gt;

million and preferably from about 500 parts per million to 5,000 parts per million fluoride.

Intercalate and tetraalkali metal salts

<img file="GR79211B_D0003.tif" />

The pyrophosphates useful in the compositions herein include dialkali metal pyrophosphates and mixtures of dialkali metal and tetraalkali metal pyrophosphates. Ta, yeah?^KHydrogen peroxide as such and in its present form are the preferred species. The percentages of each species of this kind which are preferably used in the compositions are as follows (but are in anhydrous form).

Ha₂THE₂P₂0₇ - 0.5 °/₀ - I3.8 ° /_THE

To₄P₂0_? 0 - ⁶· Θ ° /₀

K₄P₂0_? 0 - 4.0°/_The

<img file="GR79211B_D0004.tif" />

-10 * Minimum amount required in the compositions herein, 1.5 ° /₀ Can it therefore be given only from No ^ H ^ PgO? or APD mixtures of Na ^^ PgO; with one or both of the tetraalkali metal salts. Bilateral mixtures of sodium salts and tripartite mixtures thereof with tetra salt are preferred. The highest levels of sodium species are determined on the basis of solubility whereas the percentage of sodium is determined on the basis of taste criteria.

The pyrophosphates are described in greater detail in KIRK and OTHMER, EKCYCLOPEBIA OF CHEMICAL TECHNOLOGY; GY, SECOND EDITION, Volume 15, INTERSCIENCE PUBLISHERS (1968), where applicable.

Water is another essential ingredient of the compositions of this invention. Water is used for the preparation of commercially suitable oral and / or oral compositions, - it should preferably be of low ion content and free of organic impurities. The water is about 2 ° C to about 95 ° C_THE , preferably aps of about 20 ° /_q up to about 95 ° /₀ of the compositions of this invention. When these are in the form of a toothpaste, the amount of water preferably ranges from about 2 ° / s._The up to about 45 ° /₀ , while the mouthwash fluids preferably contain about 45 ° /_Qup to about 95 ° /₀ · * Possible ingredients * In addition to the essential ingredients described above, the oral compositions of this invention are possible

<img file="GR79211B_D0005.tif" />

-It contains a variety of potentially common ingredients for oral compositions. Such potential ingredients include foaming agents, flavoring agents, sweeteners, anti-tartar, coloring agents and pigments.

A preferred optional ingredient is a foaming agent; Suitable foaming agents are those which are readily stable and are foamy in a large range of pH, i.e., non-soap anionic, nonionic, cationic, amphoteric ionic and amphoteric surfactants. The means of foaming these types are more fully described in AGRICOLA et al. U.S. Patent 3,959,458 granted May 25, 1976; and HAEEELE * U.S. Patent 3,937,807; these patents are incorporated by reference.

Anionic foaming agents which are useful herein include water-soluble alkyl sulfate salts which have from 10 to 18 carbon atoms in the alkyl radical and the water-soluble salts of sulfonated monoglycerides of 10 fatty acids. The lauryl sulfate and the sodium salts of the coconut oil monoglyceride sulfonic acid compounds are examples of anionic surfactants of this type. It is also possible to use surfactant mixtures of anionic surfactants.

Non-ionic foaming agents which may be used in the compositions of the present invention may generally be defined as compounds which are produced by condensation of alkylene oxide (hydrophilic) groups having an organic or hydrophilic nature.

-12 mph. Examples of suitable nonionic foaming agents include PLURONIC, polyethylene oxide condensation products of alkyl phenols, products derived from the condensation of ethylene oxide with the product reaction propylenooxeid'iou and ethylene diamine, ethylene sympvknoseos products j oxide aliphatic alcohols, makrds chain tritotagdn aminooxdon- specific, makrds tertiary phosphine chain, long chain of dialkylsulfoxides and mixtures of such materials.

Amphoteric ionic foam synthetic agents useful in the compositions of the present invention may generally describe as derivatives of ammonium, phosphonium and sulfonated aliphatic quaternary compounds in which they are aliphatic or the aliphatic substituents contain about 8 to 18 carbon atoms and one contains an anionic water solubilized group, e.g. carboxy, sulphonate sulfate, phosphate, orthophosphate.

The cationic foaming agents useful in the compositions of the present invention can be generally defined as quaternary ammonium compounds having a long alkyl chain containing about 8 to about 18 carbon atoms such as carbon atoms. cetyltrimethylammonium bromide * diisobutylphenoxyethyloxy dimethylbenzylammonium fluorocarbon cetylpyridinium nitrite, etc.

The amphoteric foaming agents useful in providing the invention may in general be described as derivatives of aliphatic secondary and tertiary amines which

<img file="GR79211B_D0006.tif" />

-15 in the aliphatic radical may be a straight chain or branched chain and wherein one of the alloy state substituents contains about 8 to about 18 carbon atoms and one contains an anionic water-soluble carbohydrate, e.g. or phonophonic.

The foaming agent may be contained in the compositions of this invention in an amount from about 0 ° C to about 10 ° C._Q on the total weight of the composition.

It may also be added to flavorings in the present compositions, and Suitable flavorings include winter green oil, peppermint oil, mint oil, SASSAFRAS oil and carnation oil. Sweeteners that may be used include saccharin, dextrose, lebulose, aspartame, D-tryptophan, dihydroalkyldones, acesulfame and cyclamate sodium. Aromatics are generally used in compositions at rates of about 0, 4⁰/_Q up to about 2 ° / w and sweeteners at rates of about 0 ° / o_Q up to about 5 ° /_The by weight.

It is also possible to use binders with the toothpicks of the present invention. Such binders include, for example, xanthine gum, Irish lichen (carrageenanf (IRISH MOWW, VISCARIN ®), and carboxyvinylpolymers. These binders are generally present at a rate of about 0.1 ° C).₀ to I.^The/ i ·

It may be possible to add also means against the bis-diguavide moiety in the compositions of this invention. Such agents include chlorohexidine (I, 6-bis- (N-) -trifluoromethyl (I, 2-bis- (N-) -trifluoromethyl N -diguanido) of ethane are described

<img file="GR79211B_D0007.tif" />

-14- US HAEEELE, U.S. Patent 3,923 002, granted January 20, 1976; December, 1976 and Procter &amp; Gamble, Belgian patent 844,764, published January 31, 1977; these patents are incorporated herein by reference.

* If contained, any anti-harvested media are generally present in the range of from about 0 ° to about 5 ° /_Q depending on the weight of the compositions herein.

Another potential component of the present compositions is a hygroscopic substance. * Hygroscopic substance serves to keep the toothpaste's 4th connections from hardening when exposed to air and mouthwashes gives a mouthful of moisture. Certain hygroscopic substances may also impart a desired sweetness or aroma to the mouthwash and toothpaste compositions. * Hygroscopic substance, on a pure hydrocarbon basis, generally contains about ca.₀ to 7 ° /_Q, preferably APP of about 0 ° /_Q 'up to 55 ° /₀ , by weight of the composition herein.

<img file="GR79211B_D0008.tif" />

glycerol, sorbitol, zyltidl and propylene glycol. * Sorbitol

<img file="GR79211B_D0009.tif" />

<img file="GR79211B_D0010.tif" />

<img file="GR79211B_D0011.tif" />

-15Ts of pH of the compositions herein is in the range of 6.0 to 10.0 and preferably from 7.3 to 9.0; pH of pH is preferably achieved by appropriate equilibration of pyrophosphates or by addition of aliphatic salts.

Method of preparation

The compositions herein are prepared using conventional mixing methods. A contaminant method is described in Example I.

^WN&gt;9^!-T-T^T.] 9 T.^a-P ^^TheT^&lt;In the art, the compositions of the present invention are normally used.

The following examples further describe and illustrate preferred embodiments within the scope of the present invention. The examples are given for illustrative purposes only and should not be construed as limiting the invention. Many variations of this are possible without departing from the spirit and scope of the invention.

-16—

EXAMPLE I

Below we have a toothpaste which is opposed to the present invention.

<td>Ingredient</td><td> %</td>

<td>* Distilled water</td><td> 16.484</td>

<td>Sorbitol (7 ° aqueous solution /_The )</td><td> 49.565</td>

<td>Saccharinic sodium</td><td> 0.500</td>

<td>Color solution</td><td> 0.550</td>

<td>Submerged silica</td><td> 20.00</td>

<td>Sodium fluoride</td><td> 0.245</td>

<td>*Perfume</td><td> 1.350</td>

<td>* Sodium alkyl sulfate (27.9 ° aqueous solution /₀ )</td><td>5.oc</td>

<td>jsL- CAKBOPOL 94OS⁷</td><td> 0.180</td>

<td>Xavier gum</td><td> 0.600</td>

<td></td><td> 2.400</td>

<td>Na2H2 ^ 2O7</td><td>I.90</td>

<td>K 2?₁-_;(aqueous solution 65.5 ° /_The )</td><td> 2.560</td>

<td></td><td> 100.000 °/</td>

* A carboxyvinylpolymer polymer offered by BF Goodrich. COMPANY.

* The above compositions are prepared by combining water and a good portion of sorbitol in an untreated mixture and by

<img file="GR79211B_D0012.tif" />

-17 Heat the mixture to I40 ° F. * Next, Na2H2O-p Na2 PgO2 is added, the saccharin, sodium fluoride and or precipitated silica in series, and the total mixture is mixed for 5 to 10 minutes. Then add the aroma, color and / or superficially active substance. In a separate container, the remainder of the sorbitol, CAKBOPOL, and xanthine xanthine are slurried, and the main mixing container is then added. * The completed batch is stirred for about half an hour and then milled and blown out of the air (discarded).

EXAMPLE II

Below is provided another representative toothpaste of the present invention.

Component ° /

<td>Sorbitol (7 ° aqueous solution /_The )</td><td>_____The___ 50.745</td>

<td>* Distilled water</td><td> 16.484</td>

<td>Sodium sucrose</td><td> 0.500</td>

<td>Color solution</td><td> 0.550</td>

<td>I precipitated silica</td><td> 20.000</td>

<td>Sodium fluoride</td><td> 0.245</td>

<td>* Chariot</td><td> 1.550</td>

<td>Sodium alkylthioacetate 2,9 .9 ° /₀ )</td><td> 5.000</td>

<td>CAKBOPOL 940 S</td><td> 0.180</td>

<td>Xanthi gum</td><td> 0.600</td>

<td> ^^a4 ^ 2θ7 Na2H2^P2°7</td><td>⁵·⁴⁰⁰ 1.570 100.000 0/</td>

<img file="GR79211B_D0013.tif" />

-18 Both the composition of Example I and the composition of Example II are effective in reducing the presence of toothpaste and have acceptable cosmetic properties, in addition to the possible percentages and combinations of the examples which are presented using and others which are compatible with the invention or which are described and deserved herein.