CZ98796A3 - Mouth lotion containing calcium peroxide - bicarbonate - Google Patents

Abstract

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

Description

Technical Field I

BACKGROUND OF THE INVENTION The present invention relates to an oral composition comprising calcium peroxide containing _the first component and a polycarbonate containing bi carbonate.

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Background Art

Oral compositions employing peroxide components and bicarbonate components are known. The most commonly used peroxide is hydrogen peroxide, where the peroxide and bicarbonate are physically separated before use. Patents include U.S. Pat. No. 4,849,213, and the compositions provide advantages in the field of Schaeffer's implementation of the present invention. These caries suppression and suppression of gum formation - gingivitis. They also provide other benefits.

Peroxide compositions have already been developed, but other products are still needed to provide additional benefits or ease of manufacture. The present inventors have found that calcium peroxide based products achieve excellent efficacy when used with bi carbonate salt.

SUMMARY OF THE INVENTION

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

It is a further object of the present invention to provide compositions providing a variety of beneficial effects on the mouth, such as those described above.

These objects of the present invention will become apparent from the following detailed description and examples.

All percentages and dosages used in this invention are by weight unless otherwise indicated. Also, all measurements reported in the invention are carried out at a composition temperature of 25 ° C unless otherwise indicated.

In one aspect, the present invention relates to an oral composition consisting of = (A) a first component comprising (1) calcium peroxide in an amount of from 0.05X to 10.0% by weight. the first component and (2) a suitable carrier; and (B) second components comprising:

(1) a Bi carbonate salt (acidic carbonate) in an amount of from 1.0% to 60% by weight; the second component: and (2) a suitable support wherein components A and B are in separate portions of the container containing both components prior to use. Examples of packaging suitable for use in the present invention are described by Schaeffer in USP 4,849,213 and USP 4,528,180.

As used in the invention, the oral composition refers to a product which, in its normal use, is not intended to be swallowed for systemic administration of a particular therapeutic agent, but is intended to be held in the oral cavity for a period of time sufficient to thoroughly contact all the surfaces of the teeth and / or oral tissues. to activate the oral cavity.

In the invention, the term " safe " and " effective ", as used herein, means an amount of material that is sufficient to achieve the desired effect and which is simultaneously safe against the hard and soft tissues of the oral cavity.

As used herein, the term "consisting of" means that various other components may be used together in the composition of the present invention as long as the listed materials fulfill their intended functions.

As used herein, the term "carrier" means a carrier that is suitable for use in the oral composition of the invention.

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AND

DETAILED DESCRIPTION OF THE INVENTION.

In one aspect, the invention relates to a composition comprising a bicarbonate salt component and a second composition comprising a calcium peroxide component. Substantial and most advantageous components of the composition are detailed below.

B i k arbon átov1

An essential component of the invention is a bicarbonate salt (bicarbonate). Alkali metal salts are preferred. The most preferred bicarbonate salt is sodium bicarbonate, which is commercially available. The bicarbonate is used in an amount of from 1.0% to 60% by weight, preferably from 10% to 30% by weight.

Calcium peroxide

The second essential component of the invention is calcium peroxide. This material is used in an amount of from 0.05% to 10% by weight, preferably from 1.0 K to 5.0% by weight.

Other components

Water may also be present in both compositions of the present invention. It is preferred that the water used to prepare the commercially suitable compositions be de ionized and freed of high impurities. The water content is usually from 10 to 50% by weight, preferably from 20 to 40% by weight. from the weight of the toothpaste of the invention. These amounts of water include both free water added and water introduced with other materials such as sorbitol.

In addition to the above-mentioned components, the compositions of the present invention also contain numerous other components which are somewhat dependent on the type of composition (toothpaste, topical gels, prophylactic pastes and the like). Preferred systems are toothpastes, which are also the most advantageous uses.

Toothpastes contain an abrasive as a major component. The abrasive polishing material intended for use in the present invention may be any material that does not excessively dent dentin. These include, for example, silica including gels and precipitates, calcium carbonate (calcium carbonate), calcium dihydrate, tricalcium phosphate, polymetaphosphate calcium, hydrated alumina, such as certain dicalciumorthophosphate products, pyrophosphate (calcium phosphate), insoluble sodium polymetaphosphate, and resinous abrasive materials, condensation of urea and formaldehyde, and others reported by Cooley et al. U.S. Patent 3,070,510, issued December 25, 1962, incorporated herein by reference. It is also possible to use a mixture of abrasive materials.

Silica dental abrasives of various types offer the advantage of exceptionally good cleaning and polishing of teeth without unduly abrading dental enamel or dentin. Silica abrasive materials are also exceptionally compatible with soluble fluoride sources or other ion sources. For these reasons, they are preferably used according to the invention.

The silica abrasive and polishing materials used in the present invention, as well as other abrasives, have an average particle size of 0.1 to 30 microns, preferably 5 to 15 microns. The silica abrasive may be a precipitated silica or silica gel as the silica xerogels described by Pader et al. In US 3,538,230 of March 2, 1970, and Digiulio in USP 3,862,307 of June 21, 1975, both incorporated herein by reference. Preferred are the xxerogels marketed under the trade name Syloid by R.R., Grace & Company, Davison Chemical Division. Materials sold by J.M. Huber Corporation under the trade name Zeodent 110 are preferably used from the precipitated siliceous materials. These siliceous abrasives are described in USP 4,340,583 of July 29, 1982, incorporated herein by reference.

The abrasives in the dentifrice compositions of the present invention are present in an amount of from 6% to 70% by weight, preferably from 15% to 30% by weight, of the dentifrice.

Flavoring agents are also added to the dental and other compositions of the present invention. Suitable flavoring and flavoring agents are peppermint oil, oil of mint, essential oil of sassafras and cloves. Sweeteners may also be used. which are aspartame (aspartic acid derivative), acesulfame, saccharin, dextrose, levulose and sodium cyclamate.

gum arabic, tragacanth, xanthan gum. To concentrate 1 and use (cyclamen oil). The aromatizing agents and sweeteners are usually used in the compositions of the invention in an amount of from 0.005% to 2% by weight.

In preparing toothpastes, a thickening material must be added to achieve the desired consistency. Preferred thickeners are carboxyvinylpolymers, carrageenan, hydroxyethylcellulose and water-soluble salts of cellulose ethers such as Na-carboxymethylcellulose and Na-carboxymethyl-hydroxyethylcellulose. Natural gum-resins, such as karaya gum, and saccharide resins such as improving the structure as part of colloidal magnesium aluminum silicate or finely divided silica (silica gel) can also be used. Thickeners are used in a combined amount of from 0.5% to 5% by weight of the composition.

It is also preferred to use various types of surfactants in the compositions of the present invention. Suitable surfactants are those which are sufficiently stable and which are effective in a wide pH range. These include unsaponified anionic, nonionic, cationic, zwitterionic and amphoteric organic synthetic surfactants. Many of them are reported by Gieaeke et al., U.S. Patent 4,051,234, 2, September 27, 1988, which is incorporated herein by reference.

It is also desirable to add a humectant (moisture stabilizer) to the dental paste. Suitable humectants are glycerin, sorbitol, and other edible polyhydric alcohols in an amount of from 10% to 90% by weight.

One of the component phases of the present invention is a non-abrasive gel. The thickener is the dominant component of this phase, and the thickening is achieved by a material such as carboxyvinyl.

Another preferred component of the composition of the present invention is an anionic polycarboxylate that has anticalculus activity. The anionic polymeric polycarboxylates optionally, preferably used according to the invention, are well known and are used in the form of free acids or partially or preferably fully neutralized water-soluble alkali metal salts (e.g., preferably sodium) or ammonium salts. Preferred are copolymers of 1: 4 to 4U maleic anhydride or other polymerizable ethylenically unsaturated monomer, preferably methyl vinyl ether (methoxyethylene) having a molecular weight (MW) of 30,000 to 1,000,000. These copolymers are available, for example, under the name Gantrez AN 139 (MW 500,000), AN 119 (MW 250,000), and preferably S-97 Pharmaceutical Quality (MW 70,000) from GAF Corporation.

Other operative polymeric polycarboxylates are copolymers of 1L of maleic anhydride with ethyl acrylate, hydroxyethyl methacrylate, N-vinyl-2-pyrrolidone or ethylene, the latter being available, for example, as Monsanto EMA No.1103, m.h. 10,000, and EMA Grade 61, as well as 1: 1 acrylic acid copolymers with methyl or hydroxyethyl methacrylate, methyl or ethyl acrylate, isobutyl vine ether or N-vinyl-2-pyrrolidone.

Other operative polymeric polycarboxylates named in the aforementioned U.S. Pat. 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 oligomers of m.h. at least 1,000, which are available under the name Uníroyal ND.2.

In general, polymerized, olefinically or ethylenically unsaturated carboxylic acids containing an activated double bond (carbon to carbon) and at least one carboxyl group, ie, an olefinic double bond-containing acid that is easily sintered due to its presence in the monomeric molecule at the alpha-beta position, are suitable. in terms of carboxyl groups or as part of terminal (terminal) methylenes such acids are acrylic acid, alpha-chloroacrylic, crotonic, alpha-chlorosorbic, cinnamic, itaconic, citraconic, groups. Examples of methacrylic, ethacrylic, beta-acryloxy-propionic, sorbic, beta-styrylacrylic, muconic, mesaconic, glutaconic, aconltic, alpha-phenylacrylic,

2-benzyl-acrylic, 2-cyclohexylacrylic, anglic. umbelic, fumaric, maleic and the corresponding anhydrides. Other different olefinic monomers copolymerizable with these carboxylic monomers are vinyl acetate, vinyl chloride, dimethyl maleate and the like. The copolymers contain enough carboxylic acid salt groups so that they are water soluble.

The synthetic anionic polymer component is mostly a hydrocarbon with preferred halogen and oxygen-containing substituents and bonds such as in esters, ethers and hydroxyl (OH) groups, and when used in the instant compositions, in an amount of about from 0.05 to 3% by weight, preferably from 0.05 to 2% by weight, and most preferably from 0.1 to 2% by weight;

Another optional component is the source of fluoride ion sources, or fluoride ion, the fluorine-releasing compounds useful in the present invention are well known in the art as caries and pyrophosphatase inhibitors, and as such also act in practice of the present invention. . These compounds are slightly or completely soluble in water. They are characterized by their ability to release fluoride ions in the water and by not entering into the adverse reaction with other compounds in oral preparations. These materials are inorganic fluorine salts such as soluble alkali metal and caustic earth salts such as sodium fluoride, barium fluoride, sodium and ammonium fluorosilicate, sodium fluorozirconate, sodium monofluorophosphate, aluminum mono- and di-fluorophosphate, and fluorinated sodium calcium phosphate. . Preferably, alkali metal fluorides and reagents are used. such as sodium fluoride and stannous, sophisticated monofluorophosphate (MFP), and mixtures thereof.

The amount of fluoride-releasing compound is to some extent dependent on the type of compound, its solubility, and the type of oral composition, but it must be a non-toxic amount, usually from 0.005 to 3.0% by weight. in the device. In a dental composition, e.g., a dental gel, in a toothpaste (including cream), the amount of compound that releases up to 5,000 ppm of fluorine ion per weight of the composition is considered sufficient. An appropriate minimum amount of such a compound is used, but it is preferred to use as much of the compound to release 300-2,000 ppm, and even more preferably 800-1,500 ppm fluoride ion. Typically, in the case of alkali metal fluorides and cadmium fluoride, the component is present in an amount of up to 2% by weight, based on the weight of the composition and preferably in the range of 0.05 to 1% by weight. In the case of sodium monofluorophosphate, the compound should be present in an amount of 0.1 to 3%, typically 0.76% by weight.

Other anticalculus agents are ions such as zinc, as reported by Vinson in U.S. Pat.

May 10, 1977, which is incorporated herein by reference. Still others are the polymers reported by Benedict in US 4,661,341 of 28 April 1987, and Shedlovsky in US 3,429,963 of Feb. 25, 1969, both incorporated herein by reference. These metals are used in an amount of from 0.01 to 5% by weight.

Still other anticalculus agents are the pyrophosphate salts, such as the di- and tetra-substituted alkali metal pyrophosphates reported by Parran et al.

April 12, 1991, which is incorporated herein by reference.

Another optional component of the composition herein is nonionic, water-insoluble agents such as triclosan.

These materials are described in Vinson et al., U.S. Patent 4,022,899, which is incorporated herein by reference.

Method of production

The composition of the invention may be prepared by the method described in the following Examples.

Use of the composition

The present invention contemplates the application of a safe and effective amount of the composition to the oral cavity. Generally speaking, an effective amount of at least 1 gram of the composition is effective.

The following are examples of the present invention. The examples describe and represent preferred embodiments within the scope of the present invention.

EXAMPLES OF THE INVENTION

The examples are given for purposes of illustration only and are not intended to limit the invention. Numerous options are possible without departing from the spirit and content of the invention.

Example I

The following are means of characterizing the present invention:

Bicarbonate composition

Component

Sorbit

Bi sodium carbonate

Silicon dioxide (silica)

Water

Glycerine

Sassafras essential oil

Sodium carbonate

Flavoring and flavoring agent

CMC

Sachar1n

T102

Fluoride

Blue dye

Total

Paste (¾ wt

40,040 20,000 15,000 10,000

7,000 4,000 1,000 1,000 0, 850 0,517 0, 350,043,000

100,000

Calcium peroxide formulations

The following are four calcium peroxide formulations useful with the above bicarbonate composition.

Example 1 % by weight Sodium fluoride 0.243 Saccharin 0.33 Citric acid 0.2 Sodium citrate 5.59 Calcium peroxide 1.5 Triethanolamine 3 Carbopol 956 3 Flavoring agent 0.963 Glycerine 85.174 TOTAL 100. 000

Example 2 % by weight Sodium fluoride 0.243 Saccharin 0.33 Citric acid 0.2 Sodium citrate 5.59 Calcium peroxide 1.5 Triethanolamine 3 Carbopo1 956 3 Flavoring agent 963 PEG-6 85,174 TOTAL 100,000

Example 3 % weight i Sodium fluoride 0.243 Saccharin 0.33 Calcium peroxide 1.5 Poloxamer 407 20 (Pi uronic 127) Flavoring agent 0.963

76.964

100,000

Glycerine

TOTAL

Example 4

Sodium Fluoride Saccharin Calcium Peroxide Poloxamer 407 (Pluronie 127)

TOTAL% weight

243

0.33

1.5

0, 963, 76, 964, 100,000

Prior to use, the bicarbonate composition and the calcium peroxide composition must be in separate portions of the container containing both components. Examples of packaging suitable for use herein are Schaeffer in USP 4,849,213 and USP 4,528,180.

Frůmyslové use also

The industrial application of the present invention resides in the industrial manufacture of a toothpaste formulation.

Claims (7)

PATENT CLAIMS An oral composition comprising (a) a first dental composition comprising: (i) an effective amount of calcium peroxide: and (i i) a suitable carrier; (b) a second dental device comprising: ii) an effective amount of bicarbonate salts; and (i) a suitable carrier, wherein components (a) and (b) are stored in separate portions of the container containing the components before use. Oral composition according to claim 1, characterized in that one or both of compositions A and B comprise an abrasive. Oral composition according to claim 1 or 2, characterized in that one or both of the means A and B comprise a source of soluble fluoride ion. 4. Oral means according to of any claim 1 to 4, marked teaching s e t 1 m, that bicarbonate sol i in composition B the sodium bicarbonate. The leaf composition of any one of claims 1 to 4, wherein one or both of compositions A and B comprises an effective amount of a tartar preventing agent. Oral composition according to any one of Claims 1 to 5, characterized in that the tartar control agent is a pyrophosphate or polyphosphate salt. Oral composition according to any one of claims 1 to 5, characterized in that one or both of compositions A and B comprise an antiseptic. The oral composition of any one of claims 1 to 7, wherein the antiseptic is triclosan.