WO1998017236A1

WO1998017236A1 - Oral preparations containing biologically active crystallized glass

Info

Publication number: WO1998017236A1
Application number: PCT/JP1997/003843
Authority: WO
Inventors: Tamae Inoue; Akiyoshi Osaka
Original assignee: Sunstar Inc.
Priority date: 1996-10-23
Filing date: 1997-10-23
Publication date: 1998-04-30
Also published as: AU4723297A

Abstract

An oral preparation characterized by containing a biologically active crystallized glass comprising 25 to 60 wt.% of SiO2, 15 to 60 wt.% of CaO and 0 to 30 wt.% of P2O5, with each percentage being based on the crystallized glass; an oral paint prepared by further adding a film-forming substance and an organic solvent to the preparation; and another oral preparation prepared by further adding a polymer capable of adhering to the surface of a tooth to the above preparation.

Description

Description Bioactive crystallized glass-containing oral composition Technical field

The present invention relates to a bioactive crystallized glass-containing oral composition, and more particularly to an oral composition that forms a hydroxyapatite film on a tooth surface. Background art

It is known that when an artificial material is implanted in a bone defect, a defense reaction occurs in the living body.However, some glass and ceramics naturally bind to living tissue. Called the active material. Bioactive glass, which has bioactivity, is one of them, and is already used as artificial bone or artificial root.

These bioactive glasses can be broadly classified into bioactive crystallized glass containing crystals such as apatite-wollastonite in the glass and ordinary bioactive glass containing no such crystals. For example, Japanese Patent Publication No. Sho 62-10939 discloses a crystallized glass containing avatitate and wollastonite crystals, and the apatite crystals are chemically bonded to bone. It is stated that wollastonite crystals can increase the mechanical strength of glass.

Further, Japanese Patent Publication No. 1-550204 discloses a glass containing apatite or a crystal of avatitate and aluminum orthophosphate, and these crystal phases have a bone growth. It is described as stimulating. Further, Japanese Patent Application Laid-Open Nos. Hei 3-149570 and Hei 5-31166 disclose artificial bones and artificial joints obtained by coating bioactive crystallized glass on a metal such as titanium. Imprint materials such as are disclosed.

Further, Japanese Patent Publication No. 54-423384 discloses a bone cement made of a methacrylate resin and crystallized glass having an abatite crystal.

Japanese Unexamined Patent Publication No. 2-255555 / 15 discloses that using bioactive glass, regardless of inorganic material, metal material, and organic material, bone repair material, implantable medical device, medical device A method is disclosed in which a bioactive abatite film similar to bone in a living body is formed on the surface of all materials used in the living body, such as products and artificial organs.

On the other hand, in the field of oral preparations, a film-forming agent is known, and a technique for forming a film using a silicone derivative to suppress stains and dental caries (Japanese Patent Application Laid-Open No. 2-1990985) Japanese Patent Application Laid-Open No. HEI 3-38517), a technique of coating tooth surfaces using fluoroalkyl phosphates to suppress plaque dust, A technique of forming a thin film on the tooth surface using tines to inhibit plaque formation (Japanese Patent Application Laid-Open No. HEI 4-134025) and the like are disclosed. In addition, antibacterial agents are blended with a varnish base composed of natural resin and ethanol, and a technology for antibacterial preparations having long-term activity (Japanese Patent Application Laid-Open No. 5-5088383) has been developed. Technology relating to polymer preparations comprising a release acryl polymer, a drug, and a release controlling agent to give sustained release of the drug (Japanese Patent Application Laid-Open No. 3-128316), chelating capping agents And Japanese Patent Application Laid-Open No. S50-110892 disclose a technique in which a dental primer varnish in which is dissolved in a volatile solvent gives good adhesion to the tooth surface. However, there is no disclosure of a technique for retaining bioactive crystallized glass on the tooth surface to form hydroxyapatite on the tooth surface.

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 , KC l, M g C l was added chlorides such as _2, a technique for Koti packaging the tooth surface by increasing the water solubility (JP 5 6 7 3 0 1 5 JP) and the like are known Have been. Also, a technique for converting carbonated abatite to hydroxyapatite under neutral or weakly alkaline conditions (Japanese Patent Application Laid-Open No. Sho 64-70408), a dentifrice composition containing a calcium salt, and the like. There is disclosed a technique for converting nitrocellulose into hydroxyapatite in the presence of water (saliva) in the oral cavity (Japanese Patent Application Laid-Open No. Hei 7-22930).

However, the material for forming hydroxyapatite mixed with such an oral composition has short contact with the teeth and cannot uniformly coat the tooth surface in a short time. It is not possible to produce an effective formation of cartilage and thus an effective caries prevention effect. Accordingly, an object of the present invention is to provide a bioactive crystallized glass-containing oral composition that can form an excellent hydroxyapatite film on a tooth surface and effectively prevent dental caries.

Next, an object of the present invention is to allow the bioactive crystallized glass to stay on the tooth surface to form hydroxyapatite on the tooth surface.

In addition, bioactive crystallized glass is a material capable of forming a hydroxyapatite film on the tooth surface, but when incorporated into an oral composition, the bioactive crystallized glass itself remains on the tooth surface. However, there is a problem in that it is difficult to expect effective hydroxyapatite film formation. In order to solve such a problem, an object of the present invention is to allow bioactive crystallized glass to stay on the tooth surface to effectively form hydroxyapatite on the tooth surface.

Disclosure of the invention

The present inventors have conducted intensive studies to solve the above-mentioned problems, and as a result, by blending a bioactive crystallized glass having a specific composition into an oral composition, a high-density coating can be uniformly applied to the tooth surface in a short time. The inventors have found that a droxypatite film can be formed, and have completed the present invention.

In addition, the present inventor has found that by blending bioactive crystallized glass, a film-forming substance, and an organic solvent, the bioactive crystallized glass can be retained on the tooth surface for a long period of time to form a uniform hydroxyapatite film. This led to the completion of the present invention. Furthermore, the present inventors improved the retention of the bioactive crystallized glass on the tooth surface by blending the bioactive crystallized glass and the tooth-surface-adhering polymer into the oral tissue, and uniformly coated the bioactive crystallized glass on the tooth surface. They have found that a hydroxyapatite film can be formed, and have completed the present invention.

That is, the above object of the present invention has been achieved by the following inventions.

1. 25 to 60% by weight of SiO ₂ , 15 to 60% by weight of CaO and 0 to 30% by weight, preferably 10 to 2 0 wt%, the oral composition characterized by formulating a bioactive glass-ceramics consisting of P ₂ 0 ₅ in. In 2. Is et al, bioactive crystallized _{_{glass, N a 2 0, K 2}} 0, L i 2 0, T i 0, A 1 0, B a 0, Z r 0, F, N b 2 0 5 the 1 containing _{_{L a 2 0 3, T a}} 3 0, Y 0, S r O, B a O, Z n 0 and one Ru is selected from the group consisting of Mg 0 or two or more inorganic compounds 2. The composition for oral cavity according to item 1. 3. The bioactive crystallized glass forms one or more crystals selected from the group consisting of apatite, wollastonite, magnesium titanate, aluminum orthophosphate, diopside, and mica. 3. The oral composition according to the above 1 or 2, which contains the composition.

4. The composition for oral cavity according to any one of the above items 1 to 3, wherein the size of the bioactive crystallized glass is less than 32 mesh paths.

5. The oral composition according to any one of the above items 1 to 4, which contains 0.0001 to 50% by weight of a bioactive crystallized glass.

6. The oral composition according to any one of the above 1 to 5, which is a dentifrice or a mouthwash.

7. The oral coating preparation according to the above 1, 2, and 4, further comprising a film-forming substance and an organic solvent.

8. The oral coating agent according to the above item 7, wherein the film-forming substance is dissolved or dispersed in an organic solvent, and the compounding amount is 0.01 to 15% by weight based on the total amount of the coating agent. .

9. The oral composition according to the above 1, 2, and 4, further comprising a tooth surface-adhering polymer.

10. The tooth-adhering polymer is soluble in water, alcohol, or a wetting agent, and the compounding amount is 0.01 to 5% by weight based on the total amount of the composition. Oral composition.

ADVANTAGE OF THE INVENTION According to this invention, the composition for oral cavity which can solve the above-mentioned problem and form a hydroxyapatite film | membrane on a tooth surface in a short time and uniformly, and can prevent caries effectively can be provided.

Furthermore, according to the present invention, the bioactive crystallized glass can be retained on the tooth surface, and effective formation of hydroxyapatite on the tooth surface can be achieved, which is excellent in preventing caries. . Further, according to the present invention, the bioactive crystallized glass stays on the tooth surface by the action of the tooth surface-adhering polymer, and effective formation of hydroxyapatite on the tooth surface can be achieved. BEST MODE FOR CARRYING OUT THE INVENTION

The crystals contained in the bioactive crystallized glass used in the present invention are apatites such as wollastonite, hydroxyapatite or oxyfluorapatite, magnesium titanate, aluminum orthophosphate, diopside. And at least one selected from the group consisting of mica such as phlogopite and iron mica, and those containing 1 to 80% by weight with respect to the whole glass are preferred, and 50 to 8% by weight. 0% by weight is most preferred. If the amount of crystals in the glass is less than 1% by weight, the effective effect of each crystal will not be exhibited, while if it exceeds 80% by weight, the apatite-forming ability will decrease, which is not preferable. Of these crystals, wollastonite, magnesium titanate and mica increase the mechanical strength of the glass, and apatite, aluminum orthophosphate and diopside increase the affinity for the tooth surface. Works. Further, if the Sio in the bioactive crystallized glass is less than 25% by weight, the affinity with the tooth surface is reduced. On the other hand, if it exceeds 60% by weight, melting becomes difficult, which is not preferable. Further, if the content of CaO in the glass is less than 15% by weight, the affinity with the tooth surface is reduced. On the other hand, if the content exceeds 60% by weight, vitrification becomes difficult, which is not preferable. Although P ₂₀ in the glass stabilizes the glass, if it exceeds 30% by weight, no appropriate reactivity can be obtained.

In the oral composition of the present invention, one or more of these bioactive crystallized glasses may be combined in an amount of 0.001 to 50% by weight based on the total amount of the oral composition. it can. If the amount is less than 0.001% by weight, no apatite is formed on the tooth surface, while if it exceeds 50% by weight, the tooth surface is damaged, which is not preferable.

Et al is, the bioactive crystallized glass used in the present _{_{invention, N a 2 0, K 2}} 0, L i 0, T i 0 2, A l 2 0 3, Mg O, B 2 0 3, Z r 0 _{_2,} F, n b ₂ 〇 _{_{5, L a 2 0, T}} a 2 0 5, Y 2 0 3, S r O, B a O and Z n 1 kind or 2 O is the group or al selection consisting of More than one inorganic compound can be included. this Of al the inorganic _{_{compound, N a 2 0, K 2}} 0, L i 0 and B ₂ 0 ₃ is a TeiTorusei the _{glass, T i 0 2, A 1} 0, M g O, Z r 0 2 and F act to regulate apatite _{reactivity, n b 2 0, L a} 0, T a 2 0 5, Y 2 0 3, S r O, B a 0 and Z n 0 is the performance of the glass Acts to regulate. These inorganic compounds can be contained in an amount of 0 to 30% by weight based on the whole bioactive crystallized glass.

The bioactive crystallized glass used in the present invention has a shape such as a spherical shape, a bead shape, a granular shape, and a granular shape. For example, Japanese Patent Publication No. 62-10939, Japanese Patent Publication No. It can be produced by the method disclosed in JP-A-2004-204. Further, as the bioactive crystallized glass, those having less than 32 mesh paths are preferably used, and 65 mesh paths are particularly preferred. If the size is more than 32 mesh passes, it is not preferable because the feeling of use of the oral composition is impaired.

The composition for oral cavity of the present invention can be prepared by a conventional method using toothpaste, toothpaste, jewel, ointment, mouthwash, chewing gum, dental floss, patch, sealant, glass ionomer, vanish, It can be in the form of a troche, gargle tablet, oral pasta, foam, film-forming agent or liniment, but is preferably used as a dentifrice or mouthwash because of its usability. Used.

For example, in the case of a dentifrice, the abrasive may be calcium diphosphate / dihydrate and anhydride, calcium phosphate, calcium tertiary phosphate, calcium carbonate, calcium pyrophosphate , Aluminum hydroxide, alumina, maleic anhydride, silica gel, aluminum gayate, insoluble sodium metaphosphate, magnesium tertiary phosphate, magnesium carbonate, calcium sulfate, polymethacrylate Methyl acrylate, bentonites, zirconium gaylate, synthetic resins, 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% for toothpaste. % By weight.

Examples of the foaming agent include mainly nonionic surfactants and anionic surfactants. Examples of the nonionic surfactant include sugar or fatty acid ester of sugar alcohol. The fatty acid residues each have 12 to 18 carbon atoms, Those having a degree of tellurization of 1.1 to 2.5, preferably 1.2 to 1.9 can be used. Examples of the fatty acid ester of the sugar or sugar alcohol include sucrose fatty acid ester, maltose fatty acid ester, maltitol fatty acid ester, maltotriethyl fatty acid ester, maltote tritol Examples include fatty acid esters, maltopentitol fatty acid esters, maltohexitol fatty acid esters, maltohexyl fatty acid esters, sorbitan fatty acid esters, lactose fatty acid esters, and lactinose fatty acid esters.

Other nonionic surfactants include polyoxyethylene, polyoxyethylene sorbitan monolaurate, polyoxyethylene sorbitan monostearate, and the like. Ethylene sorbitan fatty acid ester, polyoxyethylene hydrogenated castor oil, polyoxyethylene fatty acid ester, fatty acid monoglyceride, polyoxyethylene higher alcohol ether, polyoxyethylene polyoxypropylene fatty acid ester, etc. It is.

These nonionic surfactants may be used alone or in combination of two or more. The amount of the nonionic surfactants is usually from 0.01 to 40% by weight based on the whole composition. And preferably 0.01 to 30% by weight.

Examples of the anionic surfactant include higher alkyl sulfates having an alkyl group of 8 to 18 carbon atoms, such as sodium lauryl sulfate and sodium myristyl sulfate. Water-soluble salts, alpha-sulfur refinsulfonate salts, higher fatty acid sodium monoglyceride monosulfate, Ν-methylamine-palmitoyl tauride salt, Ν-long chain acetyl basic amino acid salts and the like. These anionic surfactants may be used alone or in combination of two or more. The compounding amount is usually 0.0001 to 10% by weight based on the whole composition, It is preferably 0.01 to 5% by weight.

Examples of the binder include cellulose derivatives such as carboxymethylcellulose, alkaline metal alginates such as sodium alginate, propylene glycol alginate, xanthan gum, tragacanth gum, karaya gum, and arabia gum. , Gums such as carrageenan, polyvinyl alcohol, and sodium polyacrylate Synthetic binders such as rubber, carboxyvinyl polymer, and polyvinylpyrrolidone; and inorganic binders such as silica gel, aluminum silica gel, bi-gum, and labonite. These compounds may be used alone or in combination of two or more. The compounding amount is usually 0.001 to 5% by weight based on the whole composition.

In addition, menthol, carvone, phenol, eugenol, methyl salicylate, limonene, osimene, n-decyl alcohol, citronellol, α-tervineol, methyl acetate, citronellyl acetate, methyl Eugenol, Sionaire, linalool, ethyl linalool, penilin, thymol, spare mint oil, peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, cinnamon oil, pimentum oil, Flavoring agents such as diatom oil, perilla oil, winter green oil, clove oil, and eucalyptus oil may be used alone or in combination of two or more.The amount of the flavoring agent is usually based on the total amount of the composition. 0.1 to 10% by weight, preferably 0.05 to 5% by weight.

In addition, saccharin sodium, acetylfirm calcium, stepioside, neohesporidildihydrochalcone, glycyrrhizin, perillaltin, thaumatin, aspartyl phenylalanalanine methyl ester, ρ-methoxy cinnamamic aldehyde, etc. The sweetener may be used alone or in combination of two or more. The amount of the sweetener is usually 0.01 to 5% by weight based on the whole composition.

In addition, dosage forms such as dentifrices or mouthwashes include sorbitol, glycerin, ethylene glycol, propylene glycol, 1,3-butylene glycol, polyethylene glycol, polypropylene glycol, and xylitol. A wetting agent such as tut, mulch or lacquet may be used alone or in combination of two or more kinds. The compounding amount is usually 1 to 70% by weight based on the whole composition. is there.

Also, ρρ regulators such as sodium hydrogen phosphate, cunic acid, sodium citrate, fungicides such as chlorhexidine gluconate, cetylpyridinium chloride, triclosan, dextranase, Enzymes such as amylase, protease, mutanase, lysozyme, and lytic enzyme (Litechenzyme), and alkaloids such as monofluorophosphate sodium phosphate and monofluorophosphate phosphate. Metal fluorides such as monofluorophosphate, sodium fluoride, stannous fluoride, vitamin タ derivatives, tranexamic acid and epsilon aminocaproic acid, aluminum chlorohydroxide Active ingredients such as silalanine toin, dihydrocholesterol, glycyrrhizin salts, glycyrrhetinic acid, glycerol phosphate, chlorophyll, sodium chloride, liposide peptides, and water-soluble inorganic phosphoric acid compounds May be used alone or in combination of two or more.

The tooth surface-adhering polymer used in the oral composition of the present invention may be any polymer as long as it is a polymer that imparts retention of the bioactive crystallized glass on the tooth surface. Examples of the polymer include water, alcohol, and a wetting agent. A natural polymer or a synthetic polymer soluble in at least one kind is exemplified. Examples of natural polymers include cellulose derivatives such as carboxymethylcellulose, methylcellulose, ethylcellulose, hydroxypropylcellulose, hydroxyethylcellulose, cellulose acetate phthalate, and sodium alginate. Examples include alkali metal alginate, propylene glycol alginate, gums such as xanthan gum, tragacanth gum, karaya gum, arabic gum and carrageenan, and gelatin. Examples of synthetic polymers include non-ionic polymers such as polyvinylpyrrolidone and polyvinyl alcohol, epoxy vinyl polymer, methyl vinyl ether maleate copolymer, sodium polyacrylate and the like. And anionic copolymers such as methyl acrylate, methyl methacrylate copolymer, and aminoalkyl methacrylate copolymer.

The molecular weight of these polymers is preferably in the range of 50,000 to 50,000 in terms of number average molecular weight.

These tooth-surface-adhering polymers may be used alone or in combination of two or more, and the compounding amount is 0.01 to 5% by weight based on the total amount of the composition. If the amount is less than 0.01% by weight, the effect of attaching the bioactive crystallized glass to the tooth surface is not obtained, which is not preferable. Further, when the amount is more than 5% by weight, the viscosity becomes too high, which is not preferable.

Examples of the alcohol that dissolves the tooth-surface-adhering polymer include methyl alcohol, ethyl alcohol, propyl alcohol, aryl alcohol, and benzyl alcohol. Is appropriately used. Further, the oral coating composition of the present invention can be prepared by an aerosol, mist, It can be in the form of a brush, a brush or the like, and is applied to the tooth surface by a method of directly spraying on the tooth surface, a method using a tray, or a method of applying with a brush. In addition to the bioactive crystallized glass described above, the oral composition and the coating composition of the present invention may further include an abrasive, a foaming agent, a flavoring agent, a sweetening agent, a binder, and a pH adjusting agent according to each dosage form. A base such as an agent and a wetting agent, as well as a medicinal ingredient and the like can be appropriately compounded within a range that does not impair the effects of the present invention.

As the film-forming substance used in the coating agent of the present invention, those known for film formation can be used.

For example, natural resins such as silicone resin, rosin, sandalack, alkyd resin, copalite, Sumatran benzoate, polyvinyl alcohol, polyvinylpyrrolidone, polyurethane, and polystyrene Len, polymethylmethacrylate, vinyl acetate, polyvinyl chloride, polyacrylonitrile, vinyl lipidone z vinyl acetate polymer, vinylpyrrolidone Z dimethylethyla Nonionic polymers such as methinoethyl methacrylate copolymer, carboxyvinyl polymer, methylvinyl ether / maleic acid ester copolymer, and acrylic acid ester / methyl ester Anionic polymers such as acrylic acid ester copolymers, vinyl acetate copolymers, etc., dimethyl aryl ammonium chloride polymers Polymers, hydroxymethyl cellulose / dimethylphenylammonium chloride copolymers, vinylpyrrolidone quaternized dialkylaminoalkylacrylate polymers, etc., cationic polymers, higher alkyl resins, etc. Monoalkyl acetic acid amphoteric polymer of dialkylaminoethyl methacrylate polymer, amphoteric polymer such as octyl acrylamide / butyl amino methacrylate / acrylic acid ester copolymer, and fluoroalkyl lin It is a fluororesin such as acid ester, a silicon derivative such as dimethylsiloxane, etc., which is dissolved or dispersed in an organic solvent.

One or more of these film-forming substances may be used in combination, and the compounding amount is 0.01 to 15% by weight based on the total amount of the coating agent. If the amount is less than 0.01% by weight, the film-forming ability is poor, and if the amount exceeds 15% by weight, the activity of the bioactive crystallized glass is unfavorably impaired.

Examples of the organic solvent used in the present invention include ethyl acetate, dichloromethane, chloroform, alcohol, dioxane, siloxane, hexane, cyclohexane, and hexane. It is a volatile organic solvent such as sun, acetate, ether, petroleum ether, propylene carbonate and the like, and these may be used alone or in combination of two or more, and the compounding amount is 10 to 9 with respect to the total amount of the coating agent. 0% by weight, preferably 20 to 70% by weight. Next, the present invention will be described in more detail with reference to Examples and Experimental Examples, but the present invention is not limited thereto. Unless otherwise specified, [%] indicates% by weight.

Examples and comparative examples (formulations in which hydroxyapatite was replaced with bioactive crystallized glass, and formulations in which both components were not blended) were prepared by a conventional method and used for evaluation.

Example 1

Toothpaste

Ingredients Content (%) Calcium carbonate 400 Carboxymethylcellulose sodium 20 Sodium benzoate 04 Saccharin sodium 0 1 Sodium sodium lauryl sulfate 1 2 Polyethylene dextrin 50 50 Fragrance 10 Water suitable weight Bioactive crystallized glass 5.0 (glass phase (Si02 / Ca0 / P20545 / 30'25%) 95%, diopside crystal 5 %)

Total 1 0 0.0 0.0 Comparative Example 1

Toothpaste

Ingredient Content () Calcium carbonate 40.0 Carboxymethylcellulose sodium 2.0 Sodium sodium benzoate 4 Saccharinium sodium 1 Sodium sodium lauryl sulfate 2 Polyethylene glycol 0 Fragrance 0 Water-suitable water-weight hydroxyapatite 5.0 α10.

Approximately 1 X 3 mm sections were made from adult permanent tooth enamel. This section was embedded in acrylic resin, brushed with the toothpaste of Example 1 and a commercially available toothbrush for 5 minutes, and then left in whole saliva at 37 ° C for 6 hours. did. A microradiograph of the adult permanent tooth showed that a hydroxyapatite film of about 5 m was formed uniformly on the enamel surface. However, when the same operation was performed with the toothpaste of Comparative Example 1, it took 24 hours to form about 5 hydroxyapatite films, and the bioactive crystallized glass was obtained from the formulation of Example 1. When the same operation was performed with the toothpaste in the same manner as above, no hydroxyapatite film was formed on the enamel surface.

Example 2

Mouthwash

Ingredient Content (%) Glycerin 15.0 Ethanol 100 Polyoxyethylene hydrogenated castor oil (60 E〇) 0 5 pH adjuster 0 5 Stevia 0 2 Water weight Bioactive crystallized glass 5. 0 (glass phase _{(S i 0 2 / C a} 0 / P 2 0 5: 5 0/0 '3 0%) (80%, mica crystal 20%)

Total 1 0 0.0 Evaluation

The mouthwash of Example 2 was added so as to be 1% in the whole saliva, and left at 37 ° C for 12 hours. As a result, crystals precipitated in the solution, and were analyzed by infrared spectroscopy and X-ray diffraction, and were confirmed to be hydroxyapatite. However, when the same operation was performed using a mouthwash having the above formulation except for the bioactive crystallized glass, no crystals were precipitated in the liquid.

Example 3

Toothpaste

Ingredient Content (%) Gay anhydride 15.0 Carboxymethylcellulose sodium 20 Metzkins 02 Saccharin sodium 0 1 Sodium sodium lauryl sulfate 12 Fragrance 1 0 Water weight bioactive crystallized glass 5 0.0 (glass phase _{(S i 0 2 / C a} OZP 2 0 5 B 2 0

5 0/2 0/2 5/5%)) 5 0%,

(Wollastonite crystal 50%)

Mouth 110 00.0 Even with the toothpaste of Example 3, it was confirmed that a uniform hydroxyabatite film was formed on the tooth surface in a short time as in Example 1.

From these results, it was confirmed that the oral composition of the present invention forms a hydroxyapatite film on the tooth surface in a shorter time and more uniformly than the conventional oral composition.

Example 4 Component Content (%)

Ethanol 30.0

Glycerin 1 0

Polyoxyethylene hydrogenated castor oil (60E0) 1

Acrylic acid copolymer 1

Bioactive crystallized glass 1 0

(Glass phase _{(S i O 2 ZC a O} : 5 0 5 0) 5 0%, apatite crystals 50%) water 54 8.0

Total 1 0 0. 0

These components were mixed by a conventional method to produce an oral coating composition.

Comparative Example 2

Component Content (%)

Ethanol 30.0

Glycerin 1 0.0

Polyoxyethylene hydrogenated castor oil (60E0) 1.0

Bioactive crystallized glass 1 0.0

(Glass phase (Sio / Ca0: 50/50) 50%, apatite crystal 50%) Water 49.0

Total 1 0 0. 0

Example 4 and Comparative Example 2 were applied to an acrylic plate in an amount of 0.1 g each and immersed in artificial saliva for 24 hours. Twenty-four hours later, it was confirmed by induction crystal plasma emission spectrometry that a hydroxyaperite was formed on the coating of Example 4.

Example 5

Component Content (%)

Ethanol 50.0

Thunderrack 2.0

Bioactive crystallized glass 1 0.0

(Glass phase _{(S i 0 2 / C a} 0 / P 0: 5 0 2 5/2 5) 7 0%, (Diopsite crystal 30%)

Water 38.0

Total 1 0 0. 0

Comparative Example 3

Component Content (%)

Ethanol 50.0

Bioactive crystallized glass 1 0.0

(Glass phase (S i 0 / C a 0 / P 0 5: 5 0 2 5/2 5) 7 0% - Jiopusai Bok crystal 3 0%)

Water 4 0.0

Total 1 0 0. 0

Example 6

Component Content (%)

Ethyl acetate 85.0

Polyurethane 5.0

Bioactive crystallized glass 1 0.0

(Glass phase _{(S i 0 2 / C a} 0 / N a 2 0 / P 2 0 5: 4 5/2 5/5/2 5) 2 0%, apatite crystals 50%, Wallace Tokyo preparative crystal 3 0%)

Total 1 0 0. 0

The application agents of Example 5 and Example 6 were applied to the extracted adult permanent tooth enamel with a brush. The adult permanent teeth were immersed in whole saliva for one week. In Examples 5 and 6, a film was formed on adult permanent teeth even after one week, and hydroxyapatite was detected from compounds extracted from the film. On the other hand, when Comparative Example 3 was similarly applied to adult permanent teeth and immersed in whole saliva, no film remained after one week.

From these results, it was confirmed that the oral composition of the present invention forms a film on the tooth surface and uniformly forms a hydroxyapatite film on the tooth surface. Examples 7 to 9 and Comparative Examples 4 to 6

According to the prescription shown in Table 1, a gel containing the tooth surface-adhering polymer was prepared by a conventional method (Examples? To 9 and Comparative Examples 4 to 6), and the bioactive crystallized glass was used as artificial saliva. The solution was applied to an acrylic plate so as to have a concentration of 0.1%, and was allowed to stand at 37 ° C for 12 hours. The retention on the acrylic plate after 12 hours and the apatite conversion were evaluated based on the following criteria.

(1) Retentivity: retention area of acrylic plate after 12 hours

〇: 70% or more of the applied area stays

△: 40 to 70% of the applied area stays

X: 40% or less of coating area stays

(2) Apatite conversion: When gel is immersed in artificial saliva for 12 hours, the rate at which glass in the formulation is converted to apatite

〇: More than 80% of glass is converted to aperitite

Δ: 40 to 80% of glass is converted to aperitite

X: 40% or less of glass is converted to aperture

Inductively coupled plasma emission spectrometry was used for quantification of the apatite.

table 1

1 6

Replacement form (Rule 26) Example 10

Toothpaste

Ingredients Content (%) Gay anhydride 15 0 Carrageenan 20 Sodium benzoate 04 Saccharin sodium 0 1 Sodium sodium lauryl sulfate 10 Sorbit 60 0 Fragrance 10 Water appropriate amount Bioactive crystallized glass 5.0 (Glass phase (Si0 / Ca0 / P060 / 200%) 20%, wollastonite crystal 80% )

Total 1 0 0.0 0.0 Comparative Example 7

Toothpaste

Ingredient Content (%) Gay anhydride 15.0 Sodium benzoate 0 4 Saccharin sodium 0 1 Sodium sodium lauryl sulfate 10 Sorbit 6 0 0 Fragrance 1 0 Suitable for water The amount bioactive crystallized glass 5.0 (glass phase _{(S i 0 2 / C a} 0 / P 0 6 0/2 0 2 0%) 2 0%, Wallace Tokyo Bok crystal 80%)

Total 1 0 0. 0 Evaluation

Approximately 1 × 3 mm ² sections were prepared from adult permanent tooth enamel. This section was embedded in acrylic resin, brushed for 5 minutes using the toothpaste of Example 10 and a commercially available toothbrush, and then left in whole saliva for 12 hours at 37 ° C. Was placed. Observation of the adult permanent teeth with a micro-mouth radiograph revealed that about 5 m of hydroxyapatite film was uniformly formed on the surface of the enamel. However, when the same operation was performed with the toothpaste of Comparative Example 7, only a hydroxytite film of about 2 μm was formed in 12 hours. In addition, when the same operation was performed using toothpaste having a formulation in which the bioactive glass had been removed from the formulation of Example 10, no formation of a hydroxyapatite film was observed on the surface of the enamel.

From these results, it was confirmed that the oral composition of the present invention stayed on the tooth surface and uniformly formed a hydroxyapatite film on the tooth surface. Industrial applicability

According to the present invention, it is possible to provide an oral composition effective for preventing dental caries, which forms a hydroxyapatite film on the enamel surface of a tooth in a short time and uniformly.

Further, according to the present invention, a uniform hydroxyapatite film can be formed on the tooth surface, prevention of secondary caries and root caries, repair of defects such as wedge-shaped defects, relaxation of hyperesthesia, It is possible to provide an oral coating agent effective for aesthetic coating of the tooth surface. Furthermore, according to the present invention, it is possible to provide an oral composition effective for preventing dental caries, which forms a hydroxyapatite film on the enamel surface of a tooth in a short time and uniformly. The oral composition is also effective in preventing secondary caries and root caries, repairing defects such as wedge-shaped defects, alleviating hyperesthesia, and aesthetically coating tooth surfaces. .

Claims

The scope of the claims

1. for the entire bioactive crystallized glass, 2 5-6 0% by weight of S i 0 _2, 1 5 ~ 6 0 wt% of Flip a 0 and 0-3 0 weight ^ Bruno! ³ ₂ 0 ₅ incorporating the more becomes bioactive glass-ceramics oral composition characterized.

2. In addition, bioactive crystallized _{_{glass, N a 2 0, K 2}} 0, L i 2 0, T i 〇 _{_{2, A 1 0 3, B}} 0 3, Z r 0 2, F, N b 2 0 _{_{_{5, L a 2 0 3,}}} T a 3 0, Y 0, S r O, B a O, wherein containing Z n O and Mg 1 or O from the group consisting of Ru is selected or two or more inorganic compounds Item 6. The oral composition according to Item 1.

3. The bioactive crystallized glass is one or more selected from the group consisting of apatite, wollastonite, magnesium titanate, aluminum orthophosphate, diopside, and mica The oral composition according to any one of claims 1 to 2, comprising a crystal of (1).

4. The composition for oral cavity according to any one of claims 1 to 3, wherein the size of the bioactive crystallized glass is less than 32 mesh paths.

5. The oral composition according to any one of claims 1 to 4, further comprising 0.0001 to 50% by weight of a bioactive crystallized glass.

6. The oral composition according to any one of claims 1 to 5, which is a dentifrice or a mouthwash (

7. The oral coating preparation according to claim 1, 2, or 4, further comprising a film-forming substance and an organic solvent.

8. The oral coating composition according to claim 7, wherein the film-forming substance is dissolved or dispersed in an organic solvent, and the compounding amount thereof is 0.01 to 15% by weight based on the total weight of the coating composition. .

9. The oral composition according to claim 1, further comprising a tooth surface-adhering polymer.

10. The tooth surface-adhering polymer is soluble in water, alcohol, or a humectant, and the compounding amount is 0.01 to 5% by weight based on the total amount of the composition. Oral composition.