JP6960434B2 - Oral composition - Google Patents

Description

The present invention relates to oral compositions.

By supplying fluorine ions in the oral cavity, the hydroxyl groups of hydroxyapatite are replaced with fluorine and changed to fluoroxyapatite, so that remineralization is promoted. The supply of calcium ions is also effective in promoting remineralization. Therefore, sodium fluoride capable of supplying fluorine ions and calcium glycerophosphate capable of supplying calcium ions have both been conventionally used in various oral compositions.

For example, Patent Document 1 discloses a liquid oral composition using condensed phosphoric acid or a salt thereof and a cationic bactericide while using sodium fluoride and calcium glycerophosphate in combination, and is excellent in remineralization. We are trying to achieve both a promoting effect and a continuous bactericidal effect against caries-causing bacteria. Further, in Patent Document 2, a composition using xylitol in addition to a fluorine ion supply compound such as sodium fluoride and calcium glycerophosphate is used to effectively increase the amount of fluorine ions taken up on the tooth surface. ing.

JP-A-2017-66036 JP-A-2017-105755

However, in order to further increase the amount of fluorine ions taken up on the tooth surface, in the case of the composition as described in Patent Document 1, calcium fluoride, calcium phosphate and the like are unnecessarily precipitated in the oral composition. Therefore, the amount of fluorine ions taken up on the tooth surface may be reduced. On the other hand, in the composition of Patent Document 2, xylitol greatly contributes to an increase in the amount of fluorine ions taken up on the tooth surface. However, by using an easily available component without relying on such xylitol, the tooth can be used. It is desired to realize a composition capable of effectively and effectively increasing the amount of fluorine ions taken up on the surface.

Therefore, the present invention relates to an oral composition capable of effectively and effectively increasing the amount of fluorine ions taken up on the tooth surface.

Therefore, as a result of various studies, the present inventors have conducted various studies and found that, under predetermined conditions, the oral composition contains sodium fluoride and calcium glycerophosphate, and further contains glycerin and propylene glycol in a specific amount to contain xylitol. It has been found that an oral composition capable of effectively increasing the amount of fluorine ions taken up on the tooth surface can be obtained even if the above is restricted.

Therefore, in the present invention, the following components (A) to (D):
(A) Sodium fluoride 0.04% by mass or more and 1.05% by mass or less (B) Calcium glycerophosphate (C) One or two selected from glycerin and propylene glycol 0.1% by mass or more and 40% by mass or less (D) ) Water is contained, the content of condensed phosphoric acid or a salt thereof is less than 0.05% by mass, the content of xylitol is 13% by mass or less, and the content of a fluorine compound other than the component (A) is It provides an oral composition which is less than 0.1% by mass.

According to the oral composition of the present invention, the amount of fluorine taken up into the tooth surface is effective and efficient by effectively presenting fluorine ions and calcium ions to form fine crystals of calcium fluoride on the tooth surface. Can be increased to.

Hereinafter, the present invention will be described in detail.
The oral composition of the present invention contains 0.04% by mass or more and 1.05% by mass or less of sodium fluoride as the component (A). Such a component (A) can rapidly supply fluorine ions in the oral cavity, and can effectively form calcium fluoride on the tooth surface together with the calcium ions supplied by the calcium glycerophosphate of the component (B). Therefore, it is possible to efficiently and remarkably increase the amount of fluorine taken up on the tooth surface.

The content of the component (A) is 0.04% by mass or more, preferably 0.1% by mass, in the oral composition of the present invention from the viewpoint of efficiently forming calcium fluoride on the tooth surface. % Or more, more preferably 0.15% by mass or more. The content of the component (A) is 1.05% by mass or less, preferably 0.8 in the oral composition of the present invention, from the viewpoint of effectively increasing the amount of fluorine taken up on the tooth surface. It is 0% by mass or less, and more preferably 0.5% by mass or less. The content of the component (A) in the oral composition of the present invention is 0.04% by mass or more and 1.05% by mass or less, preferably 0.1 to 0.8% by mass. , More preferably 0.15 to 0.5% by mass.

The oral composition of the present invention contains calcium glycerophosphate as a component (B). By containing such a component (B), along with the fluorine ions supplied by the component (A), microcrystalline calcium fluoride is satisfactorily formed on the tooth surface, and the amount of fluorine uptake into the tooth surface is effectively increased. Can be done.

The content of the component (B) is preferably 0.1% by mass or more, more preferably 0.15 in the oral composition of the present invention from the viewpoint of effectively forming microcrystalline calcium fluoride. It is 0% by mass or more, more preferably 0.2% by mass or more, still more preferably 0.25% by mass or more, still more preferably 0.3% by mass or more, and even more preferably 0. It is 35% by mass or more. The content of the component (B) is preferably 5% by mass or less, more preferably 4% by mass, in the oral composition of the present invention from the viewpoint of effectively increasing the amount of fluorine taken up into the tooth surface. It is less than or equal to, more preferably 3% by mass or less, further preferably 2.5% by mass or less, still more preferably 1.8% by mass or less, still more preferably 1.2% by mass or less. It is more preferably 0.6% by mass or less. The content of the component (B) is preferably 0.1% by mass or more and 5% by mass or less, more preferably 0.15 to 4% by mass, and further, in the oral composition of the present invention. It is preferably 0.2 to 3% by mass, even more preferably 0.25 to 2.5% by mass, even more preferably 0.3 to 1.8% by mass, and even more preferably 0. It is 35 to 1.2% by mass, and even more preferably 0.35 to 0.6% by mass.

The mass ratio ((B) / (A)) of the content of the component (B) to the fluorine atom equivalent amount of the component (A) is preferably 3 from the viewpoint of effectively increasing the amount of fluorine uptake on the tooth surface. The above is more preferably 3.5 or more, and further preferably 4 or more. The mass ratio ((B) / (A)) of the content of the component (B) to the fluorine atom equivalent of the component (A) is preferably 6 or less, more preferably 5.8 or less. , More preferably 5.5 or less, and even more preferably 5 or less. The mass ratio ((B) / (A)) of the content of the component (B) to the fluorine atom equivalent amount of the component (A) is preferably 3 to 6, and more preferably 3.5 to 5. It is 8.8, more preferably 4 to 5.5, and even more preferably 4 to 5.

The oral composition of the present invention contains, as the component (C), one or two selected from glycerin and propylene glycol in an amount of 0.1% by mass or more and 40% by mass or less. By containing such a component (C), storage stability can be promoted.

As the component (C), either one of glycerin and propylene glycol may be contained alone or both may be contained, but propylene glycol is preferably used from the viewpoint of the amount of fluorine adsorbed.

The content of the component (C) is the present invention from the viewpoint of sufficiently allowing the component (C) to act sufficiently to enhance the storage stability and sufficiently exert the effect of promoting the increase in the amount of fluorine uptake into the tooth surface. In the oral composition of the above, 0.1% by mass or more, preferably 0.2% by mass or more, more preferably 0.3% by mass or more, and preferably 40% by mass or less. Is 30% by mass or less, more preferably 20% by mass or less. The content of the component (C) in the oral composition of the present invention is 0.1% by mass or more and 40% by mass or less, preferably 0.2 to 30% by mass, and more preferably. It is 0.3 to 20% by mass.

The mass ratio ((C) / (A)) of the content of the component (C) to the fluorine atom equivalent amount of the component (A) is determined from the viewpoint of effectively and effectively increasing the amount of fluorine uptake on the tooth surface. It is preferably 0.2 or more, more preferably 0.5 or more, still more preferably 1 or more, preferably 600 or less, more preferably 300 or less, still more preferably 200 or less.

The oral composition of the present invention contains water as the component (D). By adjusting the water content, it is possible to effectively and effectively increase the amount of fluorine taken up on the tooth surface. 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 determined by the viewpoint of increasing the contribution of the presence of the component (C) to the increase in the amount of fluorine taken up into the tooth surface, and by the fluorine ion of the component (A) and the calcium ion of the component (B). From the viewpoint of effectively refining the crystals of calcium chemicals, the composition for oral use of the present invention preferably contains 15% by mass or more, more preferably 25% by mass or more, and further preferably 30% by mass or more. It is more preferably 40% by mass or more, preferably 99% by mass or less, more preferably 95% by mass or less, still more preferably 90% by mass or less, and even more preferably 85% by mass. It is as follows. The content of the component (D) is preferably 15% by mass or more and 99% by mass or less, more preferably 25 to 95% by mass, and further preferably 30 to 30% by mass in the oral composition of the present invention. It is 90% by mass, more preferably 40 to 85% by mass.

The oral composition of the present invention contains less than 0.05% by mass of condensed phosphoric acid or a salt thereof. Since it was found that condensed phosphoric acid or a salt thereof may inhibit the formed microcrystals of calcium fluoride from being adsorbed on the tooth surface in the oral composition of the present invention, the oral composition of the present invention is used. In the composition, the content thereof is limited.

Specific examples of such condensed phosphoric acid include linear polyphosphoric acid such as pyrophosphoric acid, tripolyphosphoric acid and tetrapolyphosphoric acid, and cyclic polyphosphoric acid such as trimetaphosphoric acid and tetrapolyphosphoric acid, and examples thereof include salts thereof. Examples include sodium salt and potassium salt.

The content of condensed phosphoric acid or a salt thereof is less than 0.05% by mass in the oral composition of the present invention, preferably 0. It is preferably 03% by mass or less, more preferably 0.01% by mass or less, or the oral composition of the present invention substantially does not contain condensed phosphoric acid or a salt thereof.

The oral composition of the present invention has a xylitol content of 13% by mass or less. As described above, even in the formulation in which the content of xylitol is limited, the oral composition of the present invention promotes the atomization of calcium fluoride and sufficiently increases the amount of fluorine uptake on the tooth surface. Can be done.

The content of xylitol is 13% by mass or less, preferably 10% by mass or less, and more preferably 5% by mass or less in the oral composition of the present invention from the viewpoint of flavor, flavor, and cost. Or, the oral composition of the present invention does not have to contain xylitol.

The oral composition of the present invention contains less than 0.1% by mass of a fluorine compound other than the component (A). If an excessive amount of a fluorine compound other than the component (A) is present, the formation of microcrystalline calcium fluoride by the component (A) and the component (B) may be inhibited in the presence of the component (C). Since the amount of fluorine taken up on the tooth surface can be reduced, the oral composition of the present invention limits the content of fluorine compounds 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. The content of the fluorine compound other than the component (A) in the oral composition of the present invention is less than 0.1% by mass, preferably less than 0.08% by mass, and more preferably 0. It is preferably 05% by mass or less, or the oral composition of the present invention does not contain a fluorine compound other than the component (A).

The oral composition of the present invention is from the viewpoint of avoiding inhibition of the formation of microcrystalline calcium fluoride by the component (A) and the component (B) and ensuring a sufficient amount of fluorine uptake on the tooth surface. , It is preferable to limit the content of the organic acid or a salt thereof. Examples of such an organic acid or a salt thereof include one or more selected from salts such as citric acid, tartaric acid, malic acid, carbonic acid, and potassium salts and sodium salts thereof.
The content of such an organic acid or a salt thereof in the oral composition of the present invention is preferably 1.0% by mass or less, more preferably less than 0.8% by mass, still more preferably 0.5% by mass. It is preferably less than mass%, or the oral composition of the present invention does not contain an organic acid or a salt thereof.

The oral composition of the present invention preferably has a polyvalent metal salt content of less than 0.1% by mass. If the polyvalent metal salt is excessively present, the formation of microcrystalline calcium fluoride by the component (A) and the component (B) may be inhibited in the presence of the component (C), and fluorine on the tooth surface may be inhibited. Since the amount of uptake can be reduced, it is preferable to limit the content of the polyvalent metal salt in the oral composition of the present invention, as in the case of the fluorine compound other than the component (A).
Specific examples of such polyvalent metal salts include one or more salts selected from copper, iron, calcium, magnesium, aluminum, zinc, and tin. The content of the polyvalent metal salt in the oral composition of the present invention is preferably less than 0.05% by mass, more preferably 0.03% by mass or less, still more preferably 0.01% by mass. % Or less, or the oral composition of the present invention preferably does not contain a polyvalent metal salt.

The oral composition of the present invention effectively and efficiently forms microcrystalline calcium fluoride by the component (A) and the component (B) in the presence of the component (C), and the amount of fluorine uptake on the tooth surface. It is preferable to limit the content of the anionic surfactant from the viewpoint of further increasing the increase in calcium fluoride. Examples of such anionic surfactants include sodium lauryl sulfate, sodium lauroylmethyl taurine and the like. The content of the anionic surfactant in the oral composition of the present invention is preferably less than 1% by mass, more preferably less than 0.6% by mass, still more preferably 0.4% by mass for the same reason. Less than mass%, more preferably less than 0.2% by weight, even more preferably less than 0.08% by weight, or the oral compositions of the present invention substantially contain anionic surfactants. It is preferable not to contain it.

The oral composition of the present invention does not contain an abrasive, or 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 alcohol, as long as the effects of the present invention are not impaired. Surfactants such as nonionic surfactants such as sugar fatty acid esters and sorbitan fatty acid esters; polyhydric alcohols other than glycerin and propylene glycol such as polyethylene glycol; sugar alcohols such as sorbitol, lactol and erythritol; sodium alginate, carboxy Caking agents such as sodium methylcellulose, carrageenan, xanthan gum, sodium polyacrylate, hydroxyethyl cellulose, hydroxypropyl cellulose, pectin, tragant gum, arabic gum, and guar gum; thickening silica; sweeteners such as sodium saccharin; fragrances; pigments; medicinal ingredients Can be appropriately contained.

The pH of the oral composition of the present invention at 25 ° C. is such that the component (A) and the component (B) effectively and efficiently form microcrystalline calcium fluoride in the presence of the component (D) to form a tooth. From the viewpoint of further increasing the increase in the amount of fluorine uptake on the surface, it is preferably 5.0 or more, more preferably 6.0 or more, and further preferably 6.5 or more. Further, the pH of the oral composition of the present invention at 25 ° C. is preferably 10.0 or less, more preferably 9.6 or less, still more preferably 9. It is 3 or less, more preferably 9.0 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, a liquid oral composition is preferable from the viewpoint of sufficiently spreading the effect of the present invention to the gums or the oral mucosa. The method of application to the oral cavity may be application, brushing with a toothbrush, or gargle.
The method for producing the oral composition of the present invention is not particularly limited, and the components (A) to (D) may be blended in the same amount as the above-mentioned content, and if necessary, other components may be blended. 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 10, Comparative Examples 1 to 3]
Each oral composition was prepared according to the formulations shown in Tables 1-2. Using the obtained oral composition, measurement and evaluation were carried out according to the following method.
The results are shown in Tables 1-2.

<< Measurement of pH >>
The pH was measured using pH / ION METER F53 (manufactured by HORIBA) without diluting 20 ml of each oral composition.

<< Measurement of fluorine adsorption amount >>
After allowing 1 ml of each oral composition to act on 10 mg of hydroxyapatite powder (Bio-Gel HTP hydroxyapatite manufactured by BIO-RAD) for 2 minutes, the supernatant solution was drained by centrifugation. Further, the hydroxyapatite powder was rinsed with water three times and air-dried. Next, the naturally dried hydroxyapatite powder was treated with 1 ml of 1N hydrochloric acid for 1 minute to dissolve it, and after further neutralizing treatment, the amount of fluorine adsorbed on the hydroxyapatite powder was measured by an ionplus-fluoride (manufactured by ORION). )), And quantified (mg / g HAP) by an ion analyzer (Expandable ionAnalyzer EA940 (manufactured by ORION)).

[Prescription Examples 1 to 3]
The oral composition of the present invention was produced according to the formulation shown in Table 3.

Claims (4)

The following components (A) to (D):
(A) Sodium Fluoride 0.04% by mass or more and 1.05% by mass or less (B) Calcium glycerophosphate (C) One or two selected from glycerin and propylene glycol 0.1% by mass or more and 40% by mass or less (D) ) Water is contained, the content of condensed phosphoric acid or a salt thereof is less than 0.05% by mass, the content of xylitol is 13% by mass or less, and the content of a fluorine compound other than the component (A) is less than 0.1% by mass is,
Content and mass ratio of the fluorine atoms in terms of the component (A) ((C) / (A)) is an oral composition Ru der 0.2 or 55.3 following components (C). The oral composition according to claim 1, wherein the mass ratio ((B) / (A)) of the content of the component (B) to the fluorine atom equivalent amount of the component (A) is 3 or more and 6 or less. The oral composition according to claim 1 or 2 , wherein the content of the component (D) is 15% by mass or more and 99% by mass or less. The oral composition according to any one of claims 1 to 3 , wherein the pH at 25 ° C. is 5.0 or more and 10.0 or less.