JPH10167941A - Composition for oral cavity containing biologically active glass - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain the subject composition, capable of forming, in a short time, a uniform film of hydroxyapatite over a tooth surface, which is not stained with time, by incorporating biologically active glass and a compound selected from the group consisting of anethole, carvone and the like. SOLUTION: This composition for oral carvity is obtained by incorporating (A) 0.001 to 50wt.% of biologically active glass preferably comprising 30 to 60wt.% of SiO2 , 10 to 50wt.% of CaO, 0 to 30wt.% of Na2 O, and, as required, at least one inorganic compound elected from the group consisting of P2 O5 , K2 O, Li2 O, TiO2 , Al2 O3 , MgO, B2 O3 , ZrO2 and F, (B) 0.001 to 5wt.% of at least one compound selected from the group consisting of anethole, carvone, menthol eugenol, cineol, menthone and methyl salicylate, and, as required a pH a adjustor to keep the composition at pH 3-10. The composition can be provided in various forms, e.g. dentifrifice (e.g. toothpaste, tooth wash), mouthwash and gel.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to an oral composition for forming a hydroxyapatite film on a tooth surface.

[0002]

2. Description of the Related Art It is known that when an artificial material is implanted into a bone defect, a protective reaction occurs in a living body. However, some glasses and ceramics naturally bind to living tissue. It is called a bioactive material. Bioactive glass having bioactivity is one of them, and is already used as an artificial bone or an artificial tooth root.

[0003] These bioactive glasses can be broadly classified into bioactive crystallized glass containing crystals such as apatite and wollastonite in the glass, and ordinary bioactive glass containing no such crystals. For example,
No. 10939 discloses a crystallized glass for artificial bone containing apatite and wollastonite crystals and a method for producing the same. The crystallized glass has excellent biocompatibility,
It describes that it forms a chemical bond directly with bone and has excellent mechanical strength.

[0004] Japanese Patent Application Laid-Open No. 6-30984 discloses that
In artificial bone made of glass or crystallized glass containing CaO and SiO ₂ as main components, by adjusting the amount of Ca ²⁺ ions eluted by binding a hydrophobic group to the glass surface,
There is disclosed a technique for preventing deterioration of glass strength. JP-A-5-31166 discloses a technique in which a metal such as titanium is coated with a bioactive glass and used as a bone replacement material.

[0005] Further, Japanese Patent Application Laid-Open No. 2-255515 discloses that bone-repair materials, implantable medical instruments and equipment, medical supplies, artificial organs using bioactive glass regardless of inorganic materials, metallic materials, and organic materials. For example, a method of forming a bioactive apatite film similar to bone in a living body on the surface of all materials used in the living body is disclosed.

[0006] On the other hand, in the field of oral preparations, it is known to form a hydroxyapatite film on the tooth surface using a calcium phosphate compound. For example, NaCl, KCl, Mg
A technique of adding a chloride such as Cl ₂ to increase the solubility in water to coat the tooth surface (Japanese Patent Application Laid-Open No. 56-73015) is known. Further, a technique for converting carbonate apatite into hydroxyapatite under neutral or weakly alkaline conditions (Japanese Patent Laid-Open No. 70408/1988), or a method for converting a dentifrice composition containing a calcium salt into water (saliva) in the oral cavity. Underneath, it is converted to hydroxyapatite (JP-A-7-22930)
Publication) technology is disclosed. However, such a current oral composition cannot uniformly coat the tooth surface in a short period of time, and thus cannot exhibit an effective caries prevention effect.

[0007]

Since bioactive glass is converted into apatite in saliva in a short time, it can be uniformly coated on a tooth surface in a short time when used in an oral preparation. However, the oral composition containing bioactive glass has problems such as coloring over time.

[0008]

Means for Solving the Problems The present inventors have conducted intensive studies to solve the above-mentioned problems, and as a result, have found that coloring can be prevented by adding a specific compound to a bioactive glass-containing oral composition. The present invention has been completed.

That is, the present invention provides one of the bioactive glasses.
An object of the present invention is to provide an oral composition containing one or more species selected from the group consisting of one or more anethole, carvone, menthol, eugenol, cineol, menthone, and methyl salicylate.

[0010]

DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS The bioactive glass used in the present invention is not limited as long as it is a glass material that naturally bonds to the tooth surface, and bioactive crystallized glass containing crystals in the glass, or Any of the usual bioactive glasses that do not contain such crystals may be used. The composition of the bioactive glass preferably contains 20 to 70% by weight of SiO ₂ and 10 to 60% by weight of CaO based on the whole glass, and particularly, 30 to 60% by weight of SiO ₂ and C
preferably contains 0-30 wt% 10 to 50 wt% and Na ₂ O to aO-. If the content of SiO ₂ in the glass is less than 20% by weight, the affinity with the tooth surface decreases, while
If it exceeds 70% by weight, vitrification becomes difficult, which is not preferable. If the content of CaO in the glass is less than 10% by weight, the affinity for the tooth surface is reduced, while if it exceeds 60% by weight, vitrification becomes difficult, which is not preferable. Na
₂ O is a TeiTorusei the glass, but not preferred to lower the affinity exceeds the tooth surface 30 wt%.

In the present invention, one or more of these bioactive glasses can be used, and the compounding amount thereof is 0.001 to 50% by weight based on the whole composition. If the amount is less than 0.001% by weight, apatite is not formed on the tooth surface, while if it exceeds 50% by weight, the tooth surface is damaged, which is not preferable.

Further, in the bioactive glass used in the present invention, P ₂ O ₅ , K ₂ O, Li ₂ O, TiO ₂ , Al ₂ O ₃ , M
One or more inorganic compounds selected from the group consisting of gO, B ₂ O ₃ , ZrO ₂ , and F can be contained. Among these inorganic compounds, P ₂ O ₅ stabilizes the glass, K ₂ O, Li ₂ O and B ₂ O _{3 make} the glass low-melting, TiO ₂ , Al ₂ O ₃ , MgO, ZrO ₂ and F acts to adjust the coating rate of apatite. These inorganic compounds can be contained in the bioactive glass composition in an amount of 0 to 30% by weight.

The bioactive glass used in the present invention is spherical,
It has a bead shape, a granular shape, a granular shape, and the like, and can be produced based on a method disclosed in, for example, Japanese Patent Application Laid-Open No. 60-239341. Also, bioactive glass is
Those with less than 32 mesh passes are suitably used, with 65 mesh passes being particularly preferred. When the size is 32 mesh or more, the feeling of use of the oral composition is impaired, which is not preferable.

The oral composition of the present invention contains at least one selected from anethole, carvone, menthol, eugenol, cineol, menthone, and methyl salicylate. The blending amount thereof is not limited, but it is particularly preferably 0.001 to 5% by weight in total.
0.005 to 2% by weight is most preferred. Further, the oral composition of the present invention has a pH of 3 to 10 and is particularly excellent in forming hydroxyapatite. If necessary, citric acid, phosphoric acid, malic acid, pyrophosphoric acid, lactic acid, tartaric acid, glycerophosphoric acid, acetic acid, A pH adjuster such as nitric acid or a salt thereof, sodium hydroxide, and triethanolamine may be used.

The oral composition of the present invention can be provided in the form of toothpaste such as toothpaste, powdered toothpaste, liquid toothpaste, mouthwash, gel and the like. In the composition of the present invention, an abrasive, a foaming agent, a flavoring agent, a sweetening agent, a binder, a medicinal ingredient, and the like can be appropriately blended in a range that does not impair the effects of the present invention.

Examples of abrasives include dibasic calcium phosphate dihydrate and anhydride, calcium phosphate, tribasic calcium phosphate, calcium carbonate, calcium pyrophosphate, aluminum hydroxide, alumina, silicic anhydride, silica gel, aluminum silicate, and insoluble methaline. Sodium acid, magnesium triphosphate, magnesium carbonate, calcium sulfate, polymethyl methacrylate, bentonite, zirconium silicate, synthetic resin, and the like can be used. These abrasives may be used alone or in combination of two or more. The compounding amount is usually 5 to 90% by weight based on the whole composition, and 5 to 60% by weight in the case of toothpaste. It is.

As foaming agents, sucrose fatty acid esters,
Maltose fatty acid ester, maltitol fatty acid ester, maltotriitol fatty acid ester, maltotetriitol fatty acid ester, maltopentitol fatty acid ester, maltohexaitol fatty acid ester, maltoheptitol fatty acid ester, sorbitan fatty acid ester, lactose fatty acid ester , Lactinose fatty acid ester, polyoxyethylene polyoxypropylene copolymer, polyoxyethylene alkyl ethers, polyoxyethylene fatty acid esters, fatty acid alkanolamides, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene hydrogenated castor oil, poly Nonionic surfactants such as glycerin fatty acid fatty acid esters,

Water-soluble salts of higher alkyl sulfates having 8 to 18 carbon atoms in the alkyl group, such as sodium lauryl sulfate and sodium myristyl sulfate, polyoxyethylene alkyl sulfates, alkyl sulfoacetates, α-olefin sulfonates , Sulfosuccinic acid derivatives, higher fatty acid sodium monoglyceride monosulfate, N-
Examples include anionic surfactants such as methyl-N-palmitoyl tauride salt, N-long-chain acyl basic amino acid salt, and taurate derivative.

Further, there may be mentioned betaine type amphoteric surfactants, imidazolium type amphoteric surfactants, imidazolium betaine type amphoteric surfactants, carboxylic acid type amphoteric surfactants and the like. These blowing agents may be used alone or in combination of two or more, and the compounding amount is usually 0.1 to 10% by weight based on the whole composition.

Examples of the binder include cellulose derivatives such as carboxymethylcellulose, alkali metal alginate such as sodium alginate, propylene glycol alginate, gelatin, xanthan gum, tragacanth gum, karaya gum, gum arabic, gum such as carrageenan, polyvinyl alcohol, polyalcohol and the like. Examples include synthetic binders such as sodium acrylate, carboxyvinyl polymer, and polyvinylpyrrolidone, and inorganic binders such as silica gel, aluminum silica gel, veegum, and laponite. These binders may be used alone or in combination of two or more. May be used in combination, and the amount thereof is usually 0.3 to 5% by weight based on the whole composition.

Also, wetting agents such as sorbit, glycerin, ethylene glycol, propylene glycol, 1,3-butylene glycol, polyethylene glycol, polypropylene glycol, maltite, lactit can be blended.

Cinamic aldehyde, limonene, ocimene, n-decyl alcohol, citronellol, α-terpineol, methyl acetate, citronellyl acetate, methyl eugenol, linalool, ethyl linalool, crocodile, thymol, spearmint oil, peppermint oil, lemon oil, Orange oil, sage oil, rosemary oil, cinnamon oil, pimento oil, diatom oil, perilla oil, winter green oil,
Flavoring agents such as clove oil and eucalyptus oil or saccharin sodium, acetyl farm potassium, stevioside, neohesporidyl dihydrochalcone, glycyrrhizin, xylit, perillartin, thaumatin, aspartyl phenylalanine methyl ester, p-methoxycinnamic aldehyde, maltitol, lactit, etc. Sweetener can also be added.

Bactericides such as chlorhexidine gluconate, cetylpyridinium chloride, and triclosan; enzymes such as dextranase, amylase, protease, mutanase, lysozyme, and lytic enzyme (Litech enzyme); sodium monofluorophosphate; Alkali metal monofluorophosphates such as potassium acid, fluorides such as sodium fluoride and stannous fluoride, vitamin derivatives, tranexamic acid and epsilon aminocaproic acid, aluminum chlorhydroxyallantoin, dihydrocholesterol, glycyrrhizin salts, glycyrrhetinic acid, glycerophosphate , Chlorophyll, sodium chloride, caropeptide, water-soluble inorganic phosphate compound, etc.
More than one species may be used in combination.

[0024]

Next, the present invention will be described more specifically with reference to examples and comparative examples, but the present invention is not limited to these examples. Unless otherwise stated, [%]
Indicates% by weight. The following dentifrice compositions containing the components shown in Table 1 were prepared by a conventional method, and the stability over time was evaluated.

(Toothpaste) Ingredients Compounding amount (%) Silicic anhydride 15.0 Sodium carboxymethylcellulose 2.0 Sorbit 60.0 Methyl parahydroxybenzoate 0.2 Saccharin sodium 0.1 Sodium lauryl sulfate 1.2 Table 1 components shown (and amount) of water balance bioactive glass _{5.0 (SiO 2 / CaO; 50} /50%) total 100.0

The evaluation was performed by the following method. (Evaluation method) After the toothpaste was prepared, it was filled into tubes at 0 ° C, room temperature, and 40 ° C, respectively, and allowed to stand. Three months later, the tube was squeezed out of the tube, and the coloring was evaluated according to the following criteria. Table 1 shows the results. (Evaluation criteria) ：: Same as immediately after preparation, no coloring. Δ: Slightly colored after preparation. ×: considerably colored than immediately after preparation.

[0027]

[Table 1]

As is clear from the results shown in Table 1, it was confirmed that the Example was a dentifrice composition that did not stain with time as compared with the Comparative Example.

Example 6 Toothpaste Ingredients Content (%) Calcium carbonate 40.0 Sodium carboxymethylcellulose 2.0 Sodium benzoate 0.4 Sodium saccharin 0.1 Sodium lauryl sulfate 1.2 Sorbit 25.0 Polyethylene glycol 5. 0 carboxylic 0.2 menthone 0.1 menthol 0.7 perfume 0.3 water qs bioactive glass _{5.0 (SiO 2 / CaO / Na2O} ; 45/30/25%) total 100.0 (purified water 4 PH of Example 6 diluted 1: fold: 6.5)

The toothpaste of Example 6 was found to be a composition that did not discolor even after long-term storage. Also, a section of about 1 × 3 mm 2 from adult permanent tooth enamel was embedded in acrylic resin, brushed with this toothpaste and a commercially available toothbrush for 5 minutes, and then left in whole saliva at 37 ° C. for 12 hours. did. Observation of the adult permanent teeth with a microradiograph revealed that a hydroxyapatite film was uniformly formed on the surface of the enamel at about 5 μm.

Example 7 Mouthwash Component Ingredient Content (%) Glycerin 15.0 Alcohol 10.0 Polyoxyethylene (60) hydrogenated castor oil 1.0 Sodium citrate (pH adjuster) 0.05 Stevia 0.0 02 anethole 0.01 menthol 0.09 perfume 0.02 water qs bioactive glass _{5.0 (SiO 2 / CaO / Na} 2 0 / F; 50/20/20/10%) total 100.0 (pH 7. 0)

In Example 7, no coloration occurred over time, and crystals were precipitated in artificial saliva. The crystals were analyzed by infrared spectroscopy and X-ray diffraction, and were confirmed to be hydroxyapatite.

[0032]

According to the present invention, it is possible to provide a stable oral composition which forms a hydroxyapatite film on the enamel surface of a tooth in a short time and uniformly and does not discolor over time. .

Claims (6)

[Claims] 1. One or more bioactive glasses,
1 selected from anethole, carvone, menthol, eugenol, cineole, menthone, methyl salicylate
A composition for the oral cavity, characterized by blending two or more species. 2. The composition for oral cavity according to claim 1, wherein the composition of the bioactive glass contains a bioactive glass containing 20 to 70% by weight of SiO ₂ and 10 to 60% by weight of CaO. 3. The composition of the bioactive glass comprises 30-60% by weight of SiO ₂ , 10-50% by weight of CaO, and 0% by weight.
Claim 1 to incorporate bioactive glass containing 30 wt% of Na ₂ O, and oral composition according to any one of two terms. 4. The bioactive glass further comprises P_TwoO_Five, K
_TwoO, Li_TwoO, TiO_Two, Al_TwoO_Three, MgO, B_TwoO_Three,
ZrO_Two, And one selected from the group consisting of F
Contains two or more inorganic compounds.
Item 4. The oral composition according to any one of Items 3 to 3. 5. The blending amount of the bioactive glass is 0.001 to 0.001.
The oral composition according to any one of claims 1, 2, 3, and 4, which is 50% by weight. 6. The method according to claim 1, wherein the pH is 3 to 10.
6. The oral composition according to any one of items 3, 4, and 5.