Oral composition

Abstract

To provide an oral composition that is high in intraoral biofilm removal effect with an increased amount of fluorine ions adsorbed onto a tooth surface.SOLUTION: An oral composition contains following components (A)-(D): (A) a fluorine ion supply compound, (B) calcium glycerophosphate, (C) a fatty acid having a C10-22 hydrocarbon group or a salt thereof, and (D) a cationic germicide, wherein the ratio between the molar amount of the component (D) and the molar amount of the component (C) ((D) / (C)) is 0.4 or more and 7.0 or less.SELECTED DRAWING: None

Description

[Technical field]

[0001] The present invention relates to an oral composition. [Background technology]

[0002] Fluoride ion-supplying compounds such as sodium fluoride are known to have the effect of releasing fluoride ions in the oral cavity and promoting remineralization, and various oral compositions have been developed to increase the amount of fluoride ions absorbed into the tooth surface.

[0003] For example, Patent Document 1 discloses a mouthwash containing sodium fluoride, water-soluble calcium salts such as calcium chloride and calcium glycerophosphate, and water-soluble magnesium salts under specific quantitative conditions, which promotes the progress of remineralization of early caries. Patent Document 2 discloses a toothpaste composition containing xylitol, a fluoride ion donating compound, and calcium glycerophosphate under specific quantitative conditions, which increases the amount of fluoride ions taken up by the tooth surface while ensuring the stabilization of the composition.

[0004] On the other hand, the inventors have found that fatty acid salts such as sodium oleate can be effective in removing oral biofilms. Therefore, the combined use of the above technology and the inventors' findings may be an effective strategy for increasing the amount of fluoride ions taken up by the tooth surface while exerting an excellent oral biofilm removal effect. [Prior art documents] [Patent documents]

[0005] [Patent Document 1] JP 2008-156251 A [Patent Document 2] JP 2017-105755 A Summary of the Invention [Problem to be solved by the invention]

[0006] However, the present inventors have found that in a composition in which calcium glycerophosphate and a fatty acid or a salt thereof coexist, the fatty acid calcium salt immediately precipitates, and the expected effect is not fully exerted.

[0007] That is, the present invention relates to an oral composition that can increase the amount of fluoride ions adsorbed onto tooth surfaces while exerting an excellent oral biofilm removing effect. [Means for solving the problem]

[0008] Therefore, the present inventors conducted extensive research to solve the above problems, and as a result, they discovered an oral composition which contains a fluoride ion supplying compound, calcium glycerophosphate, and a specific fatty acid or a salt thereof, and further contains a cationic bactericide in a specific molar ratio, thereby effectively suppressing the reaction between calcium glycerophosphate and the fatty acid or a salt thereof, effectively increasing the amount of fluoride ion adsorption onto the tooth surface, and which also has an excellent effect of removing oral biofilms.

[0009] Therefore, the present invention provides the following components (A) to (D): (A) Fluoride ion donor compound (B) Calcium glycerophosphate (C) A fatty acid or a salt thereof having a hydrocarbon group having 10 to 22 carbon atoms (D) Cationic disinfectants and wherein the ratio of the molar amount of component (D) to the molar amount of component (C) ((D) / (C)) is 0.4 or more and 7.0 or less. Effect of the Invention

[0010] According to the oral composition of the present invention, it is possible to realize an oral composition that effectively promotes remineralization by increasing the amount of fluoride ions adsorbed onto the tooth surface, while also exhibiting excellent oral biofilm removal effects. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0011] The present invention will be described in detail below. The oral composition of the present invention contains a fluoride ion supplying compound as component (A). In the oral composition of the present invention, even in the presence of component (C) fatty acid or a salt thereof, component (A) which effectively supplies fluoride ions in the oral cavity and component (B) calcium glycerophosphate, which will be described later, work together effectively to increase the amount of fluoride ions adsorbed onto the tooth surface.

[0012] Component (A) may be one or more selected from sodium fluoride, potassium fluoride, ammonium fluoride, sodium monofluorophosphate, tin fluoride, hexylamine hydrofluoride, decanolamine hydrofluoride, and octadecenylamine hydrofluoride. Among these, sodium fluoride is preferred from the viewpoint of exhibiting an excellent oral biofilm removing effect while rapidly supplying fluoride ions to efficiently form calcium fluoride and effectively increasing the amount of fluoride ions adsorbed on the tooth surface.

[0013] The content of component (A) in the oral cavity composition of the present invention is preferably 0.02% by mass or more, more preferably 0.1% by mass or more, and even more preferably 0.16% by mass or more, from the viewpoint of ensuring a rapid supply of fluoride ions in the oral cavity. Also, the content of component (A) in the oral cavity composition of the present invention is preferably 5% by mass or less, more preferably 2% by mass or less, and even more preferably 0.5% by mass or less, from the viewpoint of efficiently forming calcium fluoride on the tooth surface. And, the content of component (A) in the oral cavity composition of the present invention is preferably 0.02 to 5% by mass, more preferably 0.1 to 2% by mass, and even more preferably 0.16 to 0.5% by mass.

[0014] The oral composition of the present invention contains calcium glycerophosphate as component (B). Component (B) acts as a calcium source to efficiently form calcium fluoride together with component (A). As a result, microcrystalline calcium fluoride is well formed on the tooth surface, and fluoride adsorption to the tooth surface can be enhanced.

[0015] The content of component (B) in the oral composition of the present invention is preferably 0.08% by mass or more, more preferably 0.12% by mass or more, and even more preferably 0.25% by mass or more, from the viewpoint of efficiently forming calcium fluoride on the tooth surface in combination with component (A). The content of component (B) in the oral composition of the present invention is preferably 1% by mass or less, more preferably 0.8% by mass or less, and even more preferably 0.5% by mass or less, from the viewpoint of enhancing the oral biofilm removal effect. The content of component (B) in the oral composition of the present invention is preferably 0.08 to 1% by mass, more preferably 0.12 to 0.8% by mass, and even more preferably 0.25 to 0.5% by mass.

[0016] The oral composition of the present invention contains, as component (C), a fatty acid or a salt thereof having a hydrocarbon group having from 10 to 22 carbon atoms. By containing component (D) described below, the oral composition of the present invention can exhibit an excellent oral biofilm removal effect due to component (C) despite the presence of component (B) in the system. In addition, the fatty acid or salt thereof of component (C) may be in the form of a fatty acid or an ionized salt, either partially or completely separated, in the oral composition of the present invention, or in the form of a fatty acid salt.

[0017] From the viewpoint of exerting an excellent oral biofilm removal effect, the number of carbon atoms in the hydrocarbon group of the fatty acid or salt thereof in component (C) is 10 or more, preferably 12 or more, more preferably 14 or more, even more preferably 16 or more, even more preferably 18 or more, and 22 or less, preferably 20 or less. Examples of such hydrocarbon groups include saturated hydrocarbon groups, unsaturated hydrocarbon groups, straight-chain hydrocarbon groups, and branched-chain hydrocarbon groups, and specific examples include one or more types selected from capric acid, lauric acid, myristic acid, pentadecylic acid, palmitic acid, palmitoleic acid, stearic acid, oleic acid, linoleic acid, linolenic acid, arachidonic acid, and behenic acid. Examples of the salt of the fatty acid or salt thereof of component (C) include sodium and potassium.

[0018] Furthermore, component (C) preferably contains a fatty acid or a salt thereof having at least a partial unsaturated hydrocarbon group, i.e., an unsaturated fatty acid or a salt thereof. Examples of such unsaturated hydrocarbon groups include one or more selected from palmitoleic acid, oleic acid, linoleic acid, linolenic acid, etc. Among them, from the viewpoint of achieving a good balance between the effect of increasing the amount of fluoride ion adsorbed onto the tooth surface and the effect of removing oral biofilm, one or more selected from palmitoleic acid, oleic acid, and linoleic acid are preferred, and oleic acid is more preferred.

[0019] From the viewpoint of achieving a good balance between the effect of increasing the amount of fluoride ion adsorption onto the tooth surface and the effect of removing oral biofilm, the content of unsaturated fatty acid or its salt in component (C) is preferably 15% by mass or more, more preferably 20% by mass or more, even more preferably 25% by mass or more, more preferably 30% by mass or more, even more preferably 35% by mass or more, even more preferably 50% by mass or more, even more preferably 55% by mass or more, even more preferably 75% by mass or more, even more preferably 80% by mass or more, even more preferably 90% by mass or more, and even more preferably 95% by mass or more.

[0020] The content of component (C) in the oral cavity composition of the present invention is preferably 0.05% by mass or more, more preferably 0.1% by mass or more, even more preferably 0.2% by mass or more, even more preferably 0.25% by mass or more, and even more preferably 0.35% by mass or more, from the viewpoint of exerting an excellent cleaning effect in the oral cavity and effectively removing oral biofilms adhered to the tooth surface. The content of component (C) in the oral cavity composition of the present invention is preferably 5% by mass or less, more preferably 3% by mass or less, more preferably 1.5% by mass or less, and even more preferably 1% by mass or less, from the viewpoint of suppressing the reaction between component (B) and component (C) while satisfactorily securing the effect of increasing the amount of fluoride ions adsorbed to the tooth surface. The content of component (C) in the oral cavity composition of the present invention is preferably 0.05 to 5% by mass, more preferably 0.1 to 3% by mass, even more preferably 0.2 to 1.5% by mass, even more preferably 0.25 to 1% by mass, and even more preferably 0.35 to 1% by mass. The content of component (C) is expressed as the amount converted into fatty acid.

[0021] Furthermore, the content of component (C) in the oral composition of the present invention is, in terms of mass molar concentration, preferably 0.0018 to 0.18 mass molar concentration, more preferably 0.0036 to 0.11 mass molar concentration, even more preferably 0.0071 to 0.053 mass molar concentration, even more preferably 0.0089 to 0.036 mass molar concentration, and even more preferably 0.012 to 0.036 mass molar concentration.

[0022] The oral composition of the present invention contains a cationic bactericide as component (D). By containing such component (D), it is possible to effectively prevent a reduction in the oral biofilm removing effect of component (C) caused by a prior reaction between component (B) and component (C), and therefore it is possible to simultaneously achieve the effect of increasing the amount of fluoride ions adsorbed onto the tooth surface.

[0023] As component (D), a cationic disinfectant having a quaternary ammonium is preferable, and specifically, one or more selected from alkylpyridinium salts, benzyl long-chain alkyl short-chain dialkylammonium salts and their derivatives, and long-chain alkyl short-chain trialkylammonium salts, etc. More specifically, one or more selected from benzalkonium chloride, cetylpyridinium chloride, lauryltrimethylammonium chloride, benzethonium chloride, stearyldimethylbenzylammonium chloride, myristyltrimethylammonium chloride, cetyltrimethylammonium chloride, and stearyltrimethylammonium chloride, etc. are included. Among these, from the viewpoint of effectively suppressing the reaction between components (B) and (C) and achieving both the effect of increasing the amount of fluoride ion adsorbed onto the tooth surface and the effect of removing oral biofilm, one or more selected from benzalkonium chloride, cetylpyridinium chloride, and lauryltrimethylammonium chloride are preferred, and one or two selected from cetylpyridinium chloride and benzalkonium chloride are more preferred.

[0024] The content of component (D) in the oral cavity composition of the present invention is preferably 0.12% by mass or more, more preferably 0.2% by mass or more, even more preferably 0.3% by mass or more, even more preferably 0.5% by mass or more, and even more preferably 1% by mass or more, from the viewpoint of effectively suppressing the reaction between component (B) and component (C). The content of component (D) in the oral cavity composition of the present invention is preferably 5% by mass or less, more preferably 4% by mass or less, and even more preferably 2.5% by mass or less, from the viewpoint of ensuring good solubility or dispersibility of each component in the composition. The content of component (D) in the oral cavity composition of the present invention is preferably 0.12 to 5% by mass, more preferably 0.2 to 4% by mass, even more preferably 0.3 to 2.5% by mass, even more preferably 0.5 to 2.5% by mass, and even more preferably 1 to 2.5% by mass.

[0025] Furthermore, the content of component (D) in the oral composition of the present invention is, in terms of mass molar concentration, preferably 0.0034 to 0.15 mass molar concentration, more preferably 0.0056 to 0.11 mass molar concentration, and even more preferably 0.0085 to 0.074 mass molar concentration.

[0026] The ratio of the molar amount of component (D) to the molar amount of component (C) ((D) / (C)) is 0.4 or more, preferably 0.7 or more, more preferably 1.2 or more, and even more preferably 2.2 or more, from the viewpoint of effectively suppressing the reaction between component (B) and component (C) and ensuring the exertion of an excellent oral biofilm removal effect. In addition, the ratio of the molar amount of component (D) to the molar amount of component (C) ((D) / (C)) is 7.0 or less, preferably 6.5 or less, more preferably 6.0 or less, and even more preferably 4.5 or less, from the viewpoint of exerting an excellent oral biofilm removal effect and obtaining a good appearance. In addition, the ratio of the molar amount of component (D) to the molar amount of component (C) ((D) / (C)) is 0.4 or more and 7.0 or less, preferably 0.7 to 6.5, more preferably 1.2 to 6.0, and even more preferably 2.2 to 4.5.

[0027] The oral composition of the present invention preferably contains water, which satisfactorily dissolves or disperses the above-mentioned components while enhancing the diffusibility of the oral composition after application to the oral cavity, thereby increasing the amount of fluoride ions adsorbed onto the tooth surface and providing an excellent oral biofilm removal effect.

[0028] The water content in the oral composition of the present invention is preferably 15% by mass or more, more preferably 25% by mass or more, even more preferably 35% by mass or more, and preferably 99.7% by mass or less, more preferably 99.5% by mass or less, even more preferably 99% by mass or less, even more preferably 95% by mass or less, and even more preferably 90% by mass or less. In addition, water in the present invention means the total moisture contained in the oral composition, including not only purified water etc. directly blended into the oral composition, but also the moisture contained in each of the blended components. The water content can be measured by calculation from the amount of water added and the amount of water in the added components, but can also be measured, for example, with a Karl Fischer moisture meter.

[0029] In order not to unduly inhibit the reaction suppression effect of components (B) and (C), it is preferable that the oral cavity composition of the present invention limit the content of divalent metal ion supplying compounds other than component (B). Such divalent metal ion supplying compounds are compounds capable of releasing divalent metal ions in the oral cavity, and specific examples of divalent metal ions include calcium ions, which can also be released by component (B), as well as magnesium ions, zinc ions, copper (II) ions, and manganese (II) ions.

[0030] Specific examples of divalent metal ion supplying compounds other than component (B) include chlorides such as calcium chloride containing these divalent metals, sulfates such as magnesium sulfate, and powders containing these divalent metals.

[0031] From the viewpoint of not unduly reducing the inhibitory effect of the reaction between components (B) and (C), the content of divalent metal ion supplying compounds other than component (B) in the oral composition of the present invention is preferably less than 0.05 mass%, more preferably less than 0.02 mass%, and even more preferably less than 0.01 mass%, or it is preferable that the oral composition of the present invention does not contain any divalent metal ion supplying compounds other than component (B).

[0032] The oral composition of the present invention may contain, in addition to the above-mentioned components, for example, a pH adjuster such as sodium hydroxide, a surfactant, a flavoring, a sweetener, a colorant, etc., within the scope of not impairing the effects of the present invention.

[0033] The pH of the oral composition of the present invention at 25°C is preferably 8.2 or higher, more preferably 8.6 or higher, even more preferably 9.0 or higher, and is preferably 11 or lower, more preferably 10.8 or lower, even more preferably 10.6 or lower, from the viewpoint of effectively achieving both the effect of increasing the amount of fluoride ion adsorption onto the tooth surface and the effect of removing oral biofilm.

[0034] The oral composition of the present invention may be in the form of a liquid oral composition such as a mouthwash, a mouth spray, or a liquid dentifrice, or may be a dentifrice composition such as a powder dentifrice or a toothpaste. Among these, a liquid oral composition is preferred from the viewpoint of effectively suppressing the reaction between component (B) and component (C) while effectively achieving both the effect of increasing the amount of fluoride ion adsorbed onto the tooth surface and the effect of removing oral biofilm. EXAMPLES

[0035] The present invention will now be described in detail with reference to the following examples. In the tables, the content of each component is expressed as mass % unless otherwise specified.

[0036] [Examples 1 to 11, Comparative Examples 1 to 3] Each oral composition was prepared according to the formulation shown in Tables 1 and 2. Then, using the obtained oral composition, measurements and evaluations were carried out according to the following methods. The pH of the obtained oral compositions was measured at 25° C. (measuring device: F-53 manufactured by Horiba, Ltd.), and all were found to be pH 10. The results are shown in Tables 1 and 2.

[0037] <Measurement of fluorine adsorption amount> After 10 mg of hydroxyapatite powder (Bio-Gel HTP hydroxyapatite, manufactured by BIO-RAD) was applied with 1 ml of each oral composition for 2 minutes, the supernatant solution was discarded by centrifugation. The hydroxyapatite powder was then rinsed three times with water and allowed to dry naturally. The hydroxyapatite powder was then dissolved in 1 ml of 1N hydrochloric acid for 1 minute, and neutralized. The amount of fluorine adsorbed to the hydroxyapatite powder (fluorine adsorption amount) was then quantified using a fluoride ion electrode (ionplus20Fluoride, manufactured by ORION) and an ion analyzer (Expandable ionAnalyzer EA 940, manufactured by ORION).

[0038] <Measurement of biofilm removal rate> 1) Collection of sterile saliva Healthy male subjects in their 20s and 30s were asked to chew gum pellets included in Dent Buff Strips (OralCare Inc.) and spit saliva into a Falcon tube each time. The saliva was collected in the Falcon tube by filtering it through a 0.45μm filter to obtain sterile human saliva.

[0039] 2) Preparation of biofilm model One side of an HAp substrate (Cosmo Bio, 1 cm square) was mirror-polished using 40 μm, 12 μm, and 3 μm abrasive paper, and then immersed in 1N HCl for 1 minute for acid decalcification treatment. The treated HAp plate was washed with ion-exchanged water, dried, placed in a 24-well plate, and treated with the above-prepared human sterile saliva for 2 hours to be used as a carrier for the biofilm model. The culture medium used was TSB medium (Trypticase Soy Broth, BD) supplemented with 1% sucrose. Streptococcus mutans (JCM5705) was suspended in the culture medium, and the turbidity at 600 nm (OD ) was measured using a spectrophotometer. 600nmThe bacterial solution was appropriately diluted so that the pH was 0.03. 1 mL of the bacterial solution was added to each saliva-treated HAp substrate, which was then stored in a plastic case together with a CO2 pack under anaerobic conditions and cultured at 37°C for 24 hours.

[0040] 3) Evaluation of biofilm removal effect The bacterial solution in the plate was sucked up using a vacuum pump, 1 mL of ion-exchanged water was added, and the plate was shaken for 5 minutes. Next, the water was sucked up using a pump, and 1 mL of each of the oral compositions obtained was added, and the plate was shaken for 10 minutes. The shaking was performed using a shaker (BioShake iQ (Wakembie Tech Co., Ltd.)) at room temperature (25°C) and 500 rpm. Thereafter, each oral composition was sucked up, 1 mL of ion-exchanged water was added, and the mixture was shaken for 5 minutes, which was repeated twice. Next, the water was sucked up, and 750 μL of a 0.1% by mass crystal violet (CV) solution was added, and the mixture was shaken for 15 minutes. The CV solution was then sucked up using a pump, 1 mL of ion-exchanged water was added, and the mixture was shaken for 5 minutes. This process was repeated twice. Next, the water was sucked up using a pump, 500 μL of ethanol was added and pipetted, after which the extract was diluted 10-fold with ion-exchanged water and the absorbance (Abs) was measured using a microplate recorder (TECAN Wavelength Variable Absorption Microplate Reader Sunrise Rainbow Thermo). 595nm was measured. In addition, the absorbance Abs was measured by simply washing with ion-exchanged water without using the above-obtained composition. 595nm The biofilm removal rate (%) was calculated using the initial value as the standard according to the following formula. Biofilm removal rate (%) = 100 - {Abs when using the above-obtained composition} 595nm / Abs washed only with ion-exchanged water 595nm}×100 [Table 1] [Table 2]

Claims

1. The following components (A) to (D): (A) Fluorine ion donor compound: 0.1% by mass or more and 5% by mass or less (B) Calcium glycerophosphate: 0.08% by mass or more and 1% by mass or less (C) a fatty acid or a salt thereof having a hydrocarbon group having 10 to 22 carbon atoms: 0.05% by mass to 5% by mass (D) Cationic disinfectant wherein component (C) contains an oleate, the ratio of the molar amount of component (D) to the molar amount of component (C) ((D) / (C)) is 0.7 or more and 4.5 or less, and the pH at 25°C is 8.2 or more and 11 or less.

2. 2. The oral composition according to claim 1, wherein the component (D) is a cationic bactericide having a quaternary ammonium group.

3. 3. The oral composition according to claim 1, wherein the carbon number of the hydrocarbon group contained in component (C) is 18 or more and 22 or less.

4. 4. The oral composition according to claim 1, wherein the content of unsaturated fatty acids in component (C) is 15% by mass or more.

5. The oral composition according to any one of claims 1 to 4, wherein the water content is from 15% by mass to 99.7% by mass.

6. 6. The oral composition according to claim 1, wherein the content of divalent metal ion supplying compounds other than component (B) is less than 0.05 mass%.

Images