JPH0627062B2 - Oral composition - Google Patents

Description

TECHNICAL FIELD The present invention relates to an oral composition, and more particularly to an oral composition in which adsorption of cetylpyridinium chloride, which is a bactericide, to tooth surfaces is promoted.

[Prior Art] Plaque (plaque) is formed by the adsorption and growth of oral bacteria such as Streptococcus mutans on the tooth surface, and is well known to cause dental caries. Furthermore, it has been revealed that it is also a cause of gingivitis and alveolar pyorrhea. Therefore, plaque removal and adhesion prevention (plaque control) are important for oral hygiene.

The most common method of plaque control is brushing or mechanical brushing to remove plaque. However, a thorough brushing technique is required to completely remove plaque by brushing. Most people don't brush well enough that they don't have enough plaque removal and they are brushing
Currently, the prevalence of caries, gingivitis, and alveolar pyorrhea has not decreased.

Therefore, a method of chemical plaque control has been studied to supplement brushing or as an alternative to brushing, and a pyridinium compound having a C _{8 to} C ₁₈ linear or branched alkyl group is prominent. Among them, cetylpyridinium chloride is a compound which is clinically recognized to be effective and safe.

Cetylpyridinium chloride has the formula: It is known that it has a bactericidal action and is relatively easily adsorbed on the oral mucosa and the tooth surface, which prevents the adsorption of bacteria in the oral cavity on the tooth surface and, by extension, plaque. Is believed to prevent the formation of But,
At present, no studies have been found to promote the adsorption of this cetylpyridinium chloride on the tooth surface and further improve its effect.

[Problems to be Solved by the Invention] The present inventors have earnestly studied for the purpose of further enhancing the effect of preventing the formation of plaque by promoting the retention of cetylpyridinium chloride in the oral cavity, particularly on the tooth surface. As a result, they have found that the combination of cetylpyridinium chloride with phytic acid or its derivative significantly promotes the adsorption of cetylpyridinium chloride to the teeth, and completed the present invention.

[Means for Solving the Problems] The present invention provides an oral composition characterized by containing cetylpyridinium chloride and phytic acid or a derivative thereof.

Cetylpyridinium chloride is added to the composition in an amount of 0.0002% by weight or more, preferably 0.01% by weight or more.
From the viewpoint of bactericidal effect, the upper limit of the amount of cetylpyridinium chloride is not particularly limited.However, cetylpyridinium chloride has a bitter taste, and a large amount may cause coloration of teeth, or an effect on the oral mucosa, etc. Considering
Usually, 1% by weight or less is preferable.

The phytic acid used has the formula: A compound widely found in cereal seeds, represented by
It is a highly safe compound that is industrially extracted from rice bran and used as a food improving agent. Since phytic acid exhibits a fairly strong acidity, it is preferable to use a base-neutralized or esterified one when used as a component of an oral composition. Thus, the phytic acid derivative of the present invention includes such neutralized products and esterified products. Examples of these include sodium phytate, potassium phytate, lithium phytate, magnesium phytate, calcium phytate, ammonium phytate, ethanolamine neutralized products of phytic acid, esters of phytic acid and alcohol, and the like. To be

In the present invention, phytic acid or a derivative thereof promotes the adsorption of cetylpyridinium chloride to the tooth surface, and its blending amount is at least 1/10 or more, usually 1/10, the weight of the base cetylpyridinium. ~ 20
Double is preferred. If the amount is too small, the effect of promoting adsorption of cetylpyridinium chloride to the teeth becomes insufficient.

The oral composition of the present invention can be used as a powder toothpaste, a toothpaste, a mouthwash, a troche, etc. by mixing the desired components by a conventional method, and can also be sprayed into the oral cavity as an aerosol. it can. Further, it can be used as a tooth coating agent, or can be used by impregnating it with dental floss or toothpick. The other compounding ingredients may be any of those usually used in this type of composition as long as they do not inhibit the adsorption of cetylpyridinium chloride on the tooth surface or its bactericidal action, but a foaming agent or a solubilizing agent may be used. When used, anionic ones are not preferred, nonionic or cationic ones,
In particular, it was found that the effects of cetylpyridinium chloride are further improved by using polyoxyethylene polyoxypropylene glycol, ethylenediamine tetrapolyoxyethylene polyoxypropylene glycol, or the like.

[Examples] Hereinafter, the present invention will be described in more detail by experiments and examples, but the present invention is not limited to these examples. In the examples, "%" is "% by weight".

Experiment 1 Experiment of adsorption of cetylpyridinium chloride on the tooth surface The composition of enamel on the tooth surface was 97% inorganic and 1 organic.
%, Water content 2%, and the main inorganic component is calcium phosphate, which is called hydroxyapatite (Ca ₁₀ (PO ₄ ) ₆ (OH) ₂ ).

Therefore, as a model of tooth enamel, hydroxya
Patite disc (Bio-Gel HTP, US Bio-Ra
De Laboratories, 13mmφ, 250mg, 150kg
/cm²Tableted and sintered at 600 ° C for 6 hours), human saliva
What was immersed in this at 37 ° C. for 18 hours was used. In saliva
On the surface of hydroxyapatite by immersing in
Actual tooth wetted with saliva by adsorbing liquid mucoprotein etc.
The state of enamel was approximated. This saliva processing hydroxy
Put the sheapatite disk in a test tube and 0.05% chloride
Add 1 ml of cetylpyridinium (Merck) aqueous solution, and add 37
Soak at 30 ° C. for 30 minutes. Then, wash with 6 ml of water and extract
Solvent (50 mM sodium lauryl sulfate, 40 mM citric acid
Extraction with buffer pH 3.0 / acetonitrile = 30/70)
Then, it was used as a sample for high-speed liquid chromatography. High speed liquid
Romanography is Licrosolve RP kept at 40 ℃
Select B (Lichrosorb RP SelectB, 4.0mmφ × 25
0 mm) as the separation column and the extraction solvent as the eluent.
I used it. The flow rate was 1 ml / min and cetylpyridinium chloride
Is detected by measuring the absorbance at 258 nm, and
Quantification using a calibration curve prepared with lupyridinium standard
went.

Similarly, after the saliva-treated apatite disc was immersed in a mixed solution in which each additive shown in Table 1 was added to 0.05% cetylpyridinium chloride in an amount of 0.1%, the amount of cetylpyridinium chloride was determined. It was Among the additives showing the effect of increasing the adsorption amount of cetylpyridinium chloride on the apatite disk, sodium phytate was added in an amount of 0.005, 0.01, 0.05.
%, And the effect of the concentration on the adsorption amount of cetylpyridinium chloride was examined. The results are shown in Table 1.

As shown in Table 1, when phytic acid or its derivative is blended, cetylpyridinium chloride is specifically adsorbed on the hydroxyapatite disk, and its concentration needs to be 1/10 or more in weight ratio with cetylpyridinium chloride.

Experiment 2 Since cetylpyridinium chloride may be inactivated by forming a salt with an acidic substance, the following experiment was carried out to maintain bactericidal activity.

For samples in which phytic acid or its derivative was added and the adsorption of cetylpyridinium chloride to hydroxyapatite discs was increased, the discs were suspended in 5% sucrose BHI medium, and Streptococcus mutans ATCC25175 strain was cultivated in a platinum-plated manner. 18 at 37 ° C
Incubated for hours. As a result, no plaque was observed on the hydroxyapatite disc, and it was confirmed that the cetylpyridinium chloride adsorbed on the hydroxyapatite disc retained the antibacterial activity.

Example 1 A toothpaste was produced by degassing, kneading and stirring the following components by a conventional method.

Ingredients Calcium hydrogen phosphate 20.0% Polyoxyethylene Polycocypropylene glycol 30.0% Glycerin 10.0% Cetylpyridinium chloride 0.1% Sodium phytate 0.05% Sodium saccharin 0.2% Fragrance 1.0% Remaining purified water Example 2 A toothpaste was manufactured by deaeration, kneading and stirring by a conventional method.

Ingredients Calcium carbonate 35.0% Hydroxyethyl cellulose 1.5% Ethylediamine tetrapolyoxy ethylene polyoxypropylene glycol 5.0% Sorbitol 30.0% Cetylpyridinium chloride 0.01% Potassium phytate 0.01% Sodium saccharin 0.1% Fragrance 1.0% Refined water balance Example 3 The following components were mixed and stirred by a conventional method to produce a liquid gargle.

Ingredients Ethanol 10.0% Glycerin 10.0% Polyoxyethylene polyoxy propylene glycol 1.5% Sodium saccharin 0.02% Cetylpyridinium chloride 0.05% Sodium phytate 0.1% Fragrance 0.3% Refined water balance Example 4 A 630 denier yarn obtained by twisting a plurality of denier filaments was dipped in the following mixed solution, passed through a drying tube at 50 ° C., and wound on a spool while evaporating ethanol to produce a dental cloth.

Composition: Cetylpyridinium chloride 5.0% Sodium phytate 10.0% Ethanol 85.0% [Effect of the invention] According to the present invention, adsorption of cetylpyridinium chloride on the tooth surface is promoted, which is excellent in preventing plaque formation and preventing dental caries. A composition for oral cavity exhibiting the above effect can be obtained.

Claims (1)

[Claims] 1. Cetylpyridinium chloride and 1/10 times to 20 times the weight of the cetylpyridinium chloride.
A composition for oral cavity not containing stannous fluoride, which is obtained by blending a double amount of phytic acid or a derivative thereof.