JPH0314512A - Oral cavity composition for suppressing deposition of dental plaque - Google Patents

Abstract

PURPOSE:To provide an oral cavity composition containing a specific polymer, effective in suppressing the deposition of dental plaque and useful for the prevention of dental caries and periodontosis. CONSTITUTION:A composition for oral cavity application containing 0.001-10wt.% of a polymer having a recurring unit expressed by formula (R1 and R2 are 1-10C lower alkyl; n is a number corresponding to an average molecular weight of 50,000-500,000) is properly compounded with conventional abrasive, wetting agent, foaming agent, preservative, flavor, drug-active component, etc., and formed by conventional process to obtain the objective composition. It can be prepared in the form of tooth paste, tooth powder, liquid dentifrice, wet dentifrice, mouth wash, etc. An example of the polymer of formula is poly(methylvinyl ether/maleic acid) monoethyl ester, which is commercially available as Gantrez ES-225 (product of GAF Chemicals Inc.).

Description

DETAILED DESCRIPTION OF THE INVENTION Field of the Invention The present invention relates to an oral implant such as a toothpaste that suppresses the adhesion of dental plaque and prevents caries and periodontal disease.

Conventional techniques and problems It has been clarified that caries and periodontal disease are caused by dental plaque caused by the proliferation of oral bacteria.

That is, caries is caused by the acid produced when certain bacteria such as Streptoconoccus mutans in dental plaque metabolize sugar and demineralize tooth enamel. Also, certain bacteria in plaque secrete enzymes and endotoxins that irritate the gums, causing inflammation of the gums, which causes them to bleed easily, lose elasticity, and pull away from the teeth. This causes periodontal blur. This periodontal pocket becomes a home for anaerobic bacteria, and their metabolites destroy the periodontal tissue, causing periodontal disease.

Therefore, various methods and substances have been proposed to suppress the adhesion of dental plaque in order to prevent dental caries and periodontal disease. However, nothing that is fully satisfactory has yet been found.

In view of this current situation, the present inventors conducted various studies on suppressing the adhesion of dental plaque, and surprisingly found that certain polymers have an excellent effect of suppressing the adhesion of dental plaque, and that they can be used in oral compositions such as toothpaste. It has been found that it is useful as an agent for inhibiting plaque adhesion on objects.

It has been known for some time to formulate certain polymers into oral compositions, e.g., U.S. Pat. No. 4,303,7.
No. 66 is a film substitute with a molecular weight of 2000 to 4,000,000 that prevents the elution of a drug applied to the teeth from the teeth.
Discloses a toothpaste composition formulated with polyacrylic acid fuborimer. Furthermore, JP-A-61-165317 discloses the formulation of polyacrylic acid polymers or copolymers having an average molecular weight of 3,500 to 7,500 in oral cavity compositions as anti-calculus agents. Furthermore, JP-A-63-3
No. 3321 discloses that oral compositions formulated with acrylic acid cobolimers promote the absorption of fusodide into tooth enamel.

However, these polymers do not inhibit plaque adhesion.

Means for Solving the Problems The present invention provides the formula: [1] E, in which R1 and R are the same or different, and each
Lower alkyl having 1 to 10 carbon atoms, n is an average molecular weight of 50
,000 to 500,000] A plaque adhesion inhibiting oral cavity composition characterized by containing a polymer having a repeating unit represented by the following as a plaque adhesion inhibitor. This is what we provide.

The formula of cobolimer used as a plaque adhesion inhibitor in the present invention [
In the repeating unit represented by 1], R and the alkyl of R include methyl, ethyl, proyl, butyl,
Bentyl, hexyl, etc. are mentioned, and R1 is particularly preferably methyl.

The average molecular weight is preferably about 50,000 to 500,000. Typical examples of polymers having repeating units of formula [1] include R, methyl, R2, ethyl, isobrobyl, or butyl, that is, poly(
monoethyl of methyl vinyl ether/maleic acid),
monoisopropyl or monobutyl esters, which are Gantorenotsu ES-225, ES
-335, ES-425 and ES-435 are polymers manufactured by Gaff Chemicals (GAFCH).
MICALS) is more commercially available. These poamers are generally formulated in an amount of 0.001 to 10% by weight based on the oral cavity composition from the viewpoint of inhibiting plaque adhesion.

The oral composition of the present invention can be made into a dosage form such as a toothpaste, powdered toothpaste, overnight toothpaste, moisturized toothpaste, mouthwash, etc. according to known instructions, and other ingredients are not particularly limited. However, known abrasives, wetting agents, foaming agents, preservatives, fragrances, medicinal agents, etc. can be appropriately formulated.

EXAMPLES Next, the present invention will be explained in more detail with reference to experimental examples and examples.

Experimental Example 1 Effect on adsorption of Strebutochonoccus mutans 6715 onto salivary limb-coated hydroquinoapatite (}{AP) beads (1) 20xt HAP beads were mixed with human saliva (blood type ○
)O. Incubated with Elj for 1 hour at room temperature. The beads were mixed with 0.05M KCQ, 1mM PO.
．． , 1 mM CaCIL and 1 mM MgCQ, pH 6.0 buffer, and washed twice with 1 ffl2.

(This buffer mimics the inorganic components of saliva).

The beads were then added to a pH 70 sample solution o.
Incubate for 1 hour with szc, buffer 1 above.
I washed it twice in the village.

Next, [3H]thymidine-labeled bacteria (Streptoconoccus mutans) was added to the buffer 0.5xI2 for 5 minutes. A suspension containing 10' OX was added to the beads and incubated for 1 hour at room temperature. 3 in 1 village of the buffer solution
After washing twice, the beads were transferred to a vial and radioactivity was counted using a liquid scintillation counter. On the other hand, the known c'H]t=percentage of sensitive cells was counted using the same method, and a calibration curve for the number of bacteria was created.

The sample solutions used are shown in the column of salivary HAP treatment in Table 1.

It was confirmed that the 1% copolymer aqueous solution (Gantresotsu ES225) significantly suppressed the adsorption of bacteria to saliva-coated HAP.

Experimental Example 2 Plaque and gingivitis inhibiting effects of the polymer on beagle dogs Completely removed plaque and tartar from 20 beagle dogs.
They were fed soft food and drink for 4 weeks. 10 of these are the first
group and treated with distilled water not containing the polymer,
The remaining l○ rats were treated as the nth group and treated with an aqueous solution containing a polymer (Gantret ES-225). This treatment was carried out once a day, 5 days a week, by applying 5 to 6 cc of sample solution to all teeth, and a double-blind method was adopted. Plaque and gingivitis are treated with the help of low and sillness.
Scandinavica, Q 1551-55
5 (1963)).

The results are shown in Table 2.

giant fin Shizuku lol N -3- Kubo 1 Example 1 A toothpaste was manufactured by a conventional method according to the following recipe.

Weight % Calcium carbonate 50 hydroxyethyl cellulose l゛'/l/e・t
l 5 Glycerin 10 Sodium lauryl sulfate 0.5 Pluroninoc
1 Sodium benzoate
0 2 saccharin sodium
0.1 GANTRENOTS ES-225 1 Sodium hydroxide 02 Fragrance
1 Purified water Remainder Example 2 A toothpaste was manufactured by a conventional method according to the following recipe.

Ingredients Weight % Dicalcium phosphate dihydrate 50 silicic anhydride
3 sorbitol
20 carboxymethyl cellulose
1 Sodium lauroyl sarcosine 05 Polyoxyethylene hydrogenated human oil 2 Methyl benzoate 0.2 Stevia extract
0.2 Gun Torenotsu ES-335
Tophferol triacetate 0.
5 allantoin 0.5 fragrance l purified water
Remaining Example 3 A liquid toothpaste was manufactured by a conventional method according to the following recipe.

Ingredients Weight% Glycerin 35 Brobylene Glycol 5 Sodium polyacrylate
3 Sodium lauryl sulfate 1
Borioki 7 Ethylene Hydrogenated Castor Oil 2 Sa/Karin Sodium 0.2 Gantreno ES-4
25 0.5 Sodium hydroxide
0.2 fragrance 1 purified water remainder Example 4 According to the following formulation, a Junsei toothpaste was produced by a conventional method.

Bokubun Juumei% Carunium carbonate 70 Hydroxyethyl cellulose 1 Sorbit
10 glycerin 1
5 Sodium lauryl sulfate l Tocopherol acetate 0.5 Sodium lauryl sulfate
0.2 Methyl paraoxybenzoate
0.1 sanocalin sodium
0.1 GANTRENO ES-435 0
．． 1 fragrance 1 purified water remainder Example 5 A mouthwash was manufactured by a conventional method according to the following formulation.

Bokubun Weight% Glycerin 10 Polyoxyethylene hydrogenated castor oil 1 Etasul
15 Saccharin sodium
0.2 Sodium benzoate 0.2 Gantrenot ES-225 1 Sodium hydroxide O, 4 Fragrance
0.3 Purified Water Residual Effects of the Invention According to the present invention, an oral cavity composition that can effectively suppress the adhesion of dental plaque and is useful for caries and periodontal disease is obtained.

Claims (1)

[Claims] (1) Formula: ▲There are mathematical formulas, chemical formulas, tables, etc.▼ [In the formula, R_1 and R_2 are the same or different, each is a lower alkyl having 1 to 10 carbon atoms, n has an average molecular weight of 50,000 to 500, 000] A dental plaque adhesion-inhibiting oral composition characterized by containing a polymer having a repeating unit represented by the following as a dental plaque adhesion inhibitor.