JP6960433B2 - Oral composition - Google Patents

Description

The present invention relates to oral compositions.

It is known that the combined use of sodium fluoride, which can supply fluorine ions, and calcium glycerophosphate, which can supply calcium ions, has an excellent effect of promoting remineralization, and has been further improved in recent years. It is also done.

For example, in Patent Document 1, in a liquid oral composition in which sodium fluoride and calcium glycerophosphate are used in combination, by using condensed phosphoric acid or a salt thereof and a cationic bactericide, a remineralization promoting effect and persistence against caries-causing bacteria are obtained. It is designed to be compatible with the bactericidal effect.

JP-A-2017-66036

However, in the first place, Patent Document 1 only shows a technique for improving the remineralization rate for artificially decalcified superficial decalcified lesions. On the other hand, the present invention is a technique for effectively suppressing elution of calcium ions from tooth enamel and cementum due to acid produced by bacteria in the oral cavity, and preventing tooth weakening. These two techniques are completely different.

Therefore, the present invention relates to an oral composition capable of effectively suppressing the elution amount of calcium while maintaining good storage stability.

Therefore, as a result of various studies, the present inventor used tripolyphosphoric acid and its salt in a specific content and mass ratio while using sodium fluoride and calcium glycerophosphate in combination, and contained pyrophosphoric acid and its salt and propylene glycol. It has been found that by limiting the composition, an oral composition capable of effectively and effectively suppressing the elution of calcium can be obtained.

That is, in the present invention, the following components (A) to (C):
(A) Sodium fluoride 0.02% by mass or more and 5% by mass or less (B) Calcium glycerophosphate (C) One or more kinds selected from tripolyphosphate and salts thereof 0.01% by mass or more and 2% by mass or less death,
The mass ratio ((B) / (C)) of the content of the component (B) to the content of the component (C) is 0.01 or more and 7 or less.
It provides an oral composition having a content of one or more selected from pyrophosphate and a salt thereof of less than 0.01% by mass and a content of propylene glycol of less than 3% by mass. ..

According to the oral composition of the present invention, the amount of calcium eluted can be effectively suppressed, so that the tooth substance can be sufficiently strengthened and diseases such as dental caries can be effectively prevented. .. Further, since it also has excellent storage stability, a highly useful oral composition can be realized.

6 is a photograph showing the evaluation results of storage stability of the oral compositions obtained in Example 7 and Comparative Example 7. FIG. 1 (a) is a photograph of each oral composition stored in a styrene rod bottle at the start of evaluation, and FIG. 2 (b) is a styrene rod bottle after storage at 50 ° C. for 24 hours. It is a photograph of each oral composition stored in.

Hereinafter, the present invention will be described in detail.
The oral composition of the present invention contains 0.02% by mass or more and 5% by mass or less of sodium fluoride as the component (A). Such a component (A) rapidly supplies fluorine ions in the oral cavity, and together with the calcium ions supplied by the calcium glycerophosphate of the component (B), suppresses the elution of calcium on the tooth surface.

The content of the component (A) is 0.02% by mass or more, preferably 0.1% by mass or more, more preferably, in the oral composition of the present invention from the viewpoint of suppressing the elution of calcium. It is preferably 0.2% by mass or more. Further, the content of the component (A) is 5% by mass or less, preferably 3% by mass or less, in the oral composition of the present invention, from the viewpoint of ensuring good storage stability. It is preferably 1% by mass or less. The content of the component (A) in the oral composition of the present invention is 0.02% by mass or more and 5% by mass or less, preferably 0.1 to 3% by mass, and more preferably. It is 0.2 to 1% by mass.

The oral composition of the present invention contains calcium glycerophosphate as a component (B). By containing such a component (B), the elution of calcium can be effectively suppressed in combination with the component (C) described later.

The content of the component (B) is preferably 0.01% by mass or more, more preferably 0.05% by mass or more in the oral composition of the present invention from the viewpoint of suppressing the elution of calcium. , More preferably 0.08% by mass or more. The content of the component (B) is preferably 5% by mass or less in the oral composition of the present invention from the viewpoint of effectively suppressing the elution of calcium while maintaining good storage stability. , More preferably 1% by mass or less, still more preferably 0.5% by mass or less. The content of the component (B) in the oral composition of the present invention is preferably 0.01% by mass or more and 5% by mass or less, more preferably 0.05 to 1% by mass, and further. It is preferably 0.08 to 0.5% by mass.

The mass ratio ((B) / (A)) of the content of the component (B) to the content of the component (A) is preferably 0.04 or more from the viewpoint of effectively suppressing the elution of calcium. It is more preferably 0.1 or more, still more preferably 0.4 or more, and even more preferably 1 or more. Further, the mass ratio ((B) / (A)) of the content of the component (B) to the content of the component (A) effectively suppresses the elution of calcium while ensuring good storage stability. From the viewpoint, it is preferably 3 or less, more preferably 2.5 or less, and further preferably 2 or less. The mass ratio ((B) / (A)) of the content of the component (B) to the content of the component (A) is preferably 0.04 or more and 3 or less, more preferably 0.1 to 1. It is 2.5, more preferably 0.4 to 2.5, and even more preferably 1-2.

The oral composition of the present invention contains, as the component (C), one or more selected from tripolyphosphoric acid and salts thereof, in an amount of 0.01% by mass or more and 1% by mass or less. As a result, the elution of calcium on the tooth surface can be effectively suppressed.
Examples of the salt of the component (C) include sodium salt, potassium salt and the like.

The content of the component (C) is 0.01% by mass or more in the oral composition of the present invention from the viewpoint of effectively suppressing the elution of calcium and ensuring good storage stability. , It is preferably 0.03% by mass or more, and more preferably 0.08% by mass or more. The content of the component (C) in the oral composition of the present invention is 2% by mass or less, preferably 1% by mass or less, and more preferably 0.7% by mass or less. More preferably, it is 0.5% by mass or less. The content of the component (C) in the oral composition of the present invention is 0.01% by mass or more and 2% by mass or less, preferably 0.01 to 1% by mass, and more preferably. It is 0.03 to 0.7% by mass, more preferably 0.08 to 0.5% by mass.

In the oral composition of the present invention, the mass ratio ((B) / (C)) of the content of the component (B) to the content of the component (C) is 0.01 or more and 7 or less. As a result, good storage stability can be maintained while ensuring an excellent calcium elution suppressing effect.
The mass ratio ((B) / (C)) of the content of the component (B) to the content of the component (C) is preferably 0.01 or more from the viewpoint of sufficiently suppressing the amount of calcium elution. Is 0.06 or more, more preferably 0.15 or more, still more preferably 1.5 or more. Further, the mass ratio ((B) / (C)) of the content of the component (B) to the content of the component (C) ensures good storage stability while sufficiently suppressing the elution of calcium. From the viewpoint, it is 7 or less, preferably 6.5 or less, and more preferably 6 or less. The mass ratio ((B) / (C)) of the content of the component (B) to the content of the component (C) is 0.01 or more and 7 or less, preferably 0.06 to 6. It is 5, more preferably 0.15 to 6, and even more preferably 1.5 to 6.

The oral composition of the present invention contains water (D). By adjusting the content of such water, each component can be satisfactorily dispersed or dissolved and diffused well in the oral cavity, and the component (A) and the component (B) provide excellent calcium on the tooth surface. It can exert the effect of suppressing elution. The water of the component (D) is not only purified water or the like blended in the oral composition, but also water contained in each blended component such as a 70% sorbitol solution (aqueous solution) used when prescribing. Means the total water content contained in the oral composition, which also includes.

The content of the component (D) is preferably 20% by mass or more, more preferably 25% by mass or more in the oral composition of the present invention from the viewpoint of satisfactorily exerting the calcium elution suppressing effect on the tooth surface. It is more preferably 28% by mass or more, preferably 55% by mass or less, more preferably 45% by mass or less, and further preferably 35% by mass or less.

In the oral composition of the present invention, the content of one or more selected from pyrophosphate and salts thereof is less than 0.01% by mass. That is, in the oral composition of the present invention, if one or more selected from pyrophosphate and a salt thereof is excessively present, the effect of suppressing calcium elution by the component (C) may be hindered. However, since it was found by the present inventor, its content is limited.
Examples of the pyrophosphoric acid salt include sodium salt, potassium salt and the like.

The content of one or more selected from such pyrophosphate and salts thereof is less than 0.01% by mass, preferably 0.005% by mass or less in the oral composition of the present invention. , More preferably 0.001% by mass or less, or the oral composition of the present invention preferably does not substantially contain one or more selected from pyrophosphate and salts thereof.

In the oral composition of the present invention, the content of propylene glycol is less than 3% by mass. That is, in the oral composition of the present invention, as in the case of one or more selected from the above pyrophosphate and salts thereof, the presence of propylene glycol also exerts the effect of suppressing calcium elution by the component (C). Since it has been found by the present inventor that there is a risk of being inhibited, the content thereof is limited.

The content of such propylene glycol in the oral composition of the present invention is less than 3% by mass, preferably 1% by mass or less, more preferably 0.1% by mass or less, or the present invention. The oral composition of No. 1 preferably contains substantially no propylene glycol.

In the oral composition of the present invention, it is preferable to limit the content of the anionic surfactant from the viewpoint of ensuring the excellent effect of suppressing calcium elution and maintaining good storage stability. Examples of such anionic surfactants include alkyl sulfate ester salts such as sodium lauryl sulfate and sodium myristyl sulfate; N-acylsarcosine salts such as N-lauroyl sarcosin salt and N-myristyl sarcosin salt; and N-lauroyl methyl taurine salt. N-methylacyl taurine salts such as N-myristoyl methyl taurine salt; N-acyl taurine salts such as N-lauryl taurine salt, N-myristoyl taurine salt; N-lauroyl glutamate, N-myristoyl glutamate, N-palmitoyl glutamate Examples thereof include salts, N-acylglutamates such as N-cocoyl glutamate; alkyl phosphates such as lauryl phosphate; and α-olefin (C14-16) sulfonates having 14 to 16 carbon atoms in the olefin. ..

The content of the anionic surfactant in the oral composition of the present invention is preferably less than 1.5% by mass, more preferably 1% by mass or less, still more preferably 0.1% by mass or less. Yes, or the oral composition of the present invention preferably contains substantially no anionic surfactant.

In the oral composition of the present invention, the total content of the fluorine compound other than the component (A) and the polyvalent metal salt is preferably less than 1% by mass. If an excessive amount of a fluorine compound or a polyvalent metal salt other than the component (A) is present, the calcium elution inhibitory effect brought about by the oral composition of the present invention may be inhibited, and the oral composition of the present invention may be used. It is preferable to limit the content of fluorine compounds and polyvalent metal salts other than the component (A).

Specific examples of the fluorine compound other than the component (A) include a fluorine ion supply compound such as potassium fluoride, calcium fluoride, and ammonium fluoride, and a fluorine compound which is a fluorine-containing compound such as sodium monofluorophosphate. Can be mentioned. Specific examples of the polyvalent metal salt include one or more salts selected from copper, iron, calcium, magnesium, aluminum, zinc, and tin. The total content of the fluorine compound and the polyvalent metal salt other than these components (A) is preferably less than 1% by mass, more preferably 0.1% by mass or less in the oral composition of the present invention. More preferably, it is 0.01% by mass or less, or the oral composition of the present invention preferably does not substantially contain a fluorine compound and a polyvalent metal salt other than the component (A).

The oral composition of the present invention preferably contains polyethylene glycol. As a result, an excellent calcium elution suppressing effect can be sufficiently exhibited, and further good storage stability can be ensured. The mass average molecular weight of such polyethylene glycol is preferably 1000 or less, more preferably 850 or less, and preferably 200 or more from the viewpoint of good foam quality, from the viewpoint of satisfactorily exerting the effect of suppressing calcium elution. , More preferably 400 or more.
The average molecular weight of the polyethylene glycol means the mass average molecular weight measured by GPC (gel permeation chromatography).

The content of polyethylene glycol is preferably 1% by mass or more, more preferably 3 in the oral composition of the present invention, from the viewpoint of ensuring good storage stability as well as an excellent calcium elution suppressing effect. It is 5% by mass or more, preferably 10% by mass or less, and more preferably 7% by mass or less.

The oral composition of the present invention can contain an abrasive within the limit of the total content of the fluorine compound and the polyvalent metal salt other than the component (A). Such abrasives include abrasive silica (oil absorption 50-150 mL / 100 g, depending on the amount of oil absorbed in boiling aluminum by JIS K5101-13-2 (established in 2004)), calcium dibasic phosphate dihydration. One or more selected from materials and anhydrides, calcium pyrophosphate, calcium carbonate, alumina, aluminum hydroxide, magnesium acetate, magnesium dibasic phosphate, magnesium acetate, magnesium tribasic phosphate, abrasives such as zeolite, etc. Can be mentioned.

In addition to the above components, the oral composition of the present invention contains a cationic surfactant, an amphoteric surfactant such as coconut oil fatty acid amide propyl betaine, polyoxyethylene hydrogenated castor oil, and sorbitol, as long as the effects of the present invention are not impaired. Surfactants such as nonionic surfactants such as sugar fatty acid ester and sorbitan fatty acid ester; sugar alcohols such as sorbitol, lactol and erythritol; sodium alginate, sodium carboxymethyl cellulose, carrageenan, xanthan gum, sodium polyacrylate, hydroxyethyl cellulose, hydroxy Binders such as propyl cellulose, pectin, tragant gum, Arabic gum, and guar gum; thickening silica; sweeteners such as sodium saccharin; wetting agents such as glycerin; fragrances; pigments; medicinal ingredients can be appropriately contained.

The pH of the oral composition of the present invention at 25 ° C. is preferably 5.5 or more, more preferably 5.8 or more, from the viewpoint of effectively and effectively suppressing the elution of calcium on the tooth surface. More preferably, it is 6 or more. The pH of the oral composition of the present invention at 25 ° C. is preferably 10.5 or less, more preferably 10 or less, still more preferably 9.5 or less, from the viewpoint of avoiding discoloration of the composition. It is more preferably 9 or less.
The pH of the oral composition of the present invention is a value measured at 25 ° C. using a pH electrode, and when the oral composition of the present invention is a liquid oral composition, the composition is diluted. When the oral composition of the present invention is a toothpaste composition, it is measured after adjusting to an aqueous solution having a concentration of 10% by mass with purified water consisting of ion-exchanged water or distilled water. Means the value of

Examples of the form of the oral composition of the present invention include dentifrice compositions such as dentifrices and powdered dentifrices, and liquid oral compositions such as mouthwashes and liquid dentifrices. Among them, the toothpaste composition is preferable from the viewpoint of fully enjoying the effect of suppressing the elution amount of calcium brought about by the present invention. The method of application to the oral cavity may be brushing with a toothbrush, application, or gargle.
The method for producing the oral composition of the present invention is not particularly limited, and the components (A) to (C) may be blended in the above content and mass ratio, and other components may be blended if necessary. Well, then these may be appropriately mixed by a conventional method.

Hereinafter, the present invention will be specifically described based on examples. Unless otherwise specified in the table, the content of each component indicates mass%.

[Examples 1 to 6, Comparative Examples 1 to 6]
Each oral composition having a pH of 8.5 at 25 ° C. was prepared according to the formulation shown in Table 1. Using the obtained oral composition, the amount of calcium eluted was measured according to the following method.
The results are shown in Table 1.

<< Measurement of calcium elution amount >>
Take 20 mg of hydroxyapatite (HAp) powder (HAP-200, manufactured by Taihei Kagaku Sangyo Co., Ltd.) in a microtube (capacity 1.5 mL, manufactured by Eppendorf), and further add each oral composition shown in Table 1 with purified water. After 4-fold dilution, 1000 μL of the slurry solution supernatant centrifuged at a rotation speed of 3000 rpm for 10 minutes was added, and the mixture was stirred at 37 ° C. for 5 minutes. After stirring, the supernatant was removed by centrifugation at a rotation speed of 10000 rpm for 5 minutes. Next, 900 μL of purified water was added, and the mixture was stirred for 10 seconds and then centrifuged in the same manner to remove the supernatant and washed, and this was repeated 3 times. Further, 1000 μL of 0.1 M lactic acid (adjusted to pH 4.0 with sodium hydroxide) was added to the remaining powder, and after stirring at 37 ° C. for 30 minutes, centrifugation was performed to remove the supernatant, which was 5 times. Diluted.
Next, the calcium ions eluted using Calcium E-Test Wako (manufactured by Wako Pure Chemical Industries, Ltd.) were measured at an absorbance of 610 nm and used as the amount of calcium eluted.
Based on the value of the obtained calcium elution amount, an exponential notation with Comparative Example 4 as the reference 100 was used as an index for evaluation.

[Example 7, Comparative Example 7]
Each oral composition was prepared according to the formulation shown in Table 2. Using the obtained oral composition, in the same manner as above, based on the measured value of the calcium elution amount, the exponential notation with Comparative Example 7 as the reference 100 is used as an evaluation index, and storage stability is performed according to the following method. Sexual evaluation was performed.
The results are shown in Table 2.

<< Evaluation of storage stability >>
After preparing each oral composition shown in Table 2, 15 g was collected and stored in a styrene rod bottle having a capacity of 25 ml. A photograph of each oral composition immediately after being stored in the bottle (at the start of evaluation) is shown in FIG. 1 (a).
Next, after storing each bottle in an incubator at 50 ° C. for 24 hours, the presence or absence of a precipitate (precipitate) and the presence or absence of turbidity are visually evaluated. When there was a problem, it was evaluated as "x". A photograph of each oral composition stored in the bottle at the time of completion of storage (at the time of evaluation) is shown in FIG. 1 (b).

From the results of Table 2 and FIG. 1, the oral composition obtained in Example 7 effectively suppresses the elution of calcium and maintains good transparency from the start to the end of the evaluation. It was confirmed that even at the time of completion, no precipitate was formed and the storage stability was excellent. On the other hand, in the oral composition obtained in Comparative Example 7, a precipitate was visually recognized at the completion, and it was confirmed that the storage stability was inferior.

Claims (7)

The following components (A) to (C):
(A) Sodium fluoride 0.02% by mass or more and 5% by mass or less (B) Calcium glycerophosphate (C) One or more kinds selected from tripolyphosphate and salts thereof 0.01% by mass or more and 2% by mass or less death,
The mass ratio ((B) / (C)) of the content of the component (B) to the content of the component (C) is 0.15 or more and 7 or less.
One or more content selected from pyrophosphoric acid and salts thereof is not more than 0.001 wt%, the content of propylene glycol Ri der 0.1 wt%, and
The weight average molecular weight of 1,000 or less of the content of the polyethylene glycol is 1% by weight to 10% by weight der Ru oral composition. The oral composition according to claim 1, wherein the mass ratio ((B) / (A)) of the content of the component (B) to the content of the component (A) is 0.04 or more and 3 or less. The oral composition according to claim 1 or 2, which contains 20% by mass or more and 55% by mass or less of water (D). The oral composition according to any one of claims 1 to 3, wherein the content of the anionic surfactant is less than 1.5% by mass. The oral composition according to any one of claims 1 to 4, wherein the content of the component (B) is 0.01% by mass or more and 5% by mass or less. The oral composition according to any one of claims 1 to 5, wherein the total content of the fluorine compound other than the component (A) and the polyvalent metal salt is less than 1% by mass. The oral composition according to any one of claims 1 to 6, wherein the pH at 25 ° C. is 5.5 or more and 10.5 or less.

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