JP2017066108A - Composition for application on tooth - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a composition for application on a tooth that can be applied on a tooth by a method such as application, has the effect of promoting tooth remineralization, and reduces a blending amount of a fluorine compound.SOLUTION: A composition for application on a tooth comprises (a) lactobionic acid or salt thereof, (b) hydrogen phosphate, (c) film formation polymer, (d) alcohol, and (e) water, and is used by application on a tooth.SELECTED DRAWING: None

Description

  The present invention relates to a composition for applying a tooth that can promote remineralization of the tooth by applying it to the tooth.

  A dental application composition is applied to a tooth by a method such as application to a tooth and is held on the tooth for a certain period of time to prevent dental caries or to promote the effect of remineralization of the tooth. For the composition.

  As a tooth coating composition, a tooth coating composition containing no casein phosphopeptide-amorphous calcium phosphate complex (CPP-ACP), a film-forming polymer, an alcohol, a fluorine compound, and a thickener is used. It is disclosed (for example, Patent Document 1). Among these, a fluorine compound is sodium fluoride, for example, and it is widely known that it has effects such as promotion of remineralization of teeth, improvement of acid resistance, prevention of caries and the like.

  As described above, it has been recognized that the fluorine compound is highly effective for dentistry. It is widely recognized that it has a proven track record and high safety. However, since it is not always preferable to blend the fluorine compound at a high concentration, a composition in which the blending amount of the fluorine compound is suppressed has been demanded.

JP 2011-73983 A

  Therefore, the present invention provides a composition for applying a tooth that can be applied by a method such as application to a tooth, brings about an effect of promoting remineralization of the tooth, and suppresses the blending amount of a fluorine compound. And

  As a result of intensive studies, the inventors of the present invention include lactobionic acid and / or a salt thereof as a main component of the remineralization effect, and further, a tooth application containing hydrogen phosphate, a film-forming polymer, alcohol, and water. The present invention was completed by finding that the composition could solve the above problems.

  That is, the present invention includes (a) lactobionic acid and / or a salt thereof, (b) hydrogen phosphate, (c) a film-forming polymer, (d) alcohol, (e) water, and is used by applying to teeth. This is a composition for applying a tooth.

  The composition for applying a tooth according to the present invention can be applied by a method such as application to a tooth, is held on the tooth for a certain period of time, has the effect of promoting remineralization of the tooth, and the blending amount of the fluorine compound It is the composition for tooth application which suppressed the above.

  Hereinafter, the composition for tooth bleaching which concerns on this invention is demonstrated in detail.

  The composition for tooth bleaching according to the present invention comprises (a) lactobionic acid and / or a salt thereof, (b) hydrogen phosphate, (c) a film-forming polymer, (d) alcohol, (e) water, A composition for applying a tooth, which is used by applying to a tooth.

(A) Lactobionic acid and / or a salt thereof provide the tooth coating composition of the present invention with an effect of promoting remineralization. As lactobionic acid and / or its salt, lactobionic acid and its salt, calcium lactobionic acid, sodium lactobionic acid, potassium lactobionic acid, zinc lactobionic acid, copper lactobionic acid, strontium lactobionic acid, lithium lactobionic acid, barium lactobionic acid Examples thereof include lithium lactobionate and magnesium lactobionate. These may be used alone or in combination of two or more. Among these, calcium lactobionate which is a calcium supply source as well as the ability to promote remineralization is particularly preferable.
(A) It is preferable that the compounding quantity of lactobionic acid and / or its salt is 0.5-20 weight% in a composition. If it is 0.5% by weight or more, the effect of promoting remineralization becomes sufficient, and if it is 20% by weight or less, storage stability tends to be maintained. More preferably, it is 1 to 10% by weight.

(B) Hydrogen phosphate plays a role as a phosphate source, and has the effect of promoting remineralization. Examples of hydrogen phosphate include sodium hydrogen phosphate, potassium hydrogen phosphate, calcium hydrogen phosphate, lithium hydrogen phosphate, magnesium hydrogen phosphate, strontium hydrogen phosphate, barium hydrogen phosphate, magnesium hydrogen phosphate, hydrogen phosphate Examples include zinc and copper hydrogen phosphate. These may be used alone or in combination of two or more. Of these, sodium hydrogen phosphate is particularly preferred.
(B) It is preferable that the compounding quantity of hydrogen phosphate is 0.5 to 20 weight% in a composition. If it is 0.5% by weight or more, the effect of promoting remineralization becomes sufficient, and if it is 20% by weight or less, storage stability tends to be maintained. More preferably, it is 1 to 10% by weight.

(C) The film-forming polymer has an effect of forming a stable film containing lactobionic acid and / or a salt thereof and a hydrogen phosphate salt on the tooth when the tooth coating composition is applied to the tooth, Thereby, the composition for tooth application | coating is hold | maintained on a tooth for a fixed time on a tooth. As film-forming polymers, natural products such as shellac, rosin, pullulan, zein, acacia gum, gum arabic, carnauba wax, hemirose, gelatin, agar, chitin, chitosan, chitosamine, polyethylene glycol, polyvinyl acetate, polyethyl acetate, Polypropylene glycol, polyethylene oxide, polyvinyl alcohol, alkyl acrylate polymer, alkyl methacrylate polymer, methoxymethylene, maleic anhydride copolymer, polyethylene glycol-methylene diisocyanate cyclohexane copolymer, polypropylene glycol-methylene diisocyanate A cyclohexane copolymer etc. are illustrated. These may be used alone or in combination of two or more.
(C) It is preferable that the compounding quantity of a film formation polymer | macromolecule is 5 to 60 weight% in a composition. When the amount is 5% by weight or more, the coating tends to be maintained for a sufficient period, and when the amount is 60% by weight or less, the storage stability tends to be maintained. More preferably, it is 10 to 50% by weight.

(D) Alcohol is mix | blended as a volatile component. By blending alcohol, the operability during application by application to teeth, etc. is improved, and it volatilizes by drying, so that a film is easily formed. Examples of the alcohol include ethanol, methanol, propanol, isopropanol, butanol, isobutanol, pentanol, isopentanol, oleyl alcohol, methyl cellosolve, ethyl cellosolve, and butyl cellosolve. These may be used alone or in combination of two or more.
(D) It is preferable that the compounding quantity of alcohol is 5 to 50 weight% in a composition. If the amount is 5% by weight or more, precipitation of lactobionic acid and / or a salt thereof in the composition is unlikely to occur and storage stability tends to be maintained. When applied to the film, it tends to be dried and the film formation tends to be facilitated. More preferably, it is 1 to 40% by weight.

(E) Water is blended in order to increase the solubility of lactobionic acid and / or its salt, and hydrogen phosphate, and to provide a stable tooth coating composition.
(E) It is preferable that the compounding quantity of water is 0.5 to 30 weight% in a composition. When the amount is 0.5% by weight or more, precipitation of lactobionic acid and / or a salt thereof in the composition is unlikely to occur and storage stability tends to be maintained. When it is applied to the teeth, it tends to be dried and the film formation tends to be facilitated. More preferably, it is 5 to 20% by weight.

  In addition to the above components (a) to (e), the composition for tooth application according to the present invention can further contain (f) a calcium phosphate compound.

(F) A calcium phosphate compound is a compound containing phosphate ions and calcium ions, and has the effect of further enhancing the remineralization of teeth by serving as a source of phosphate ions and calcium ions. Examples of the calcium phosphate compound include casein phosphopeptide-amorphous calcium phosphate (CPP-ACP), β-TCP, α-TCP, fTCP, HAP (hydroxyapatite), carbonate apatite, and the like. These may be used alone or in combination of two or more.
(F) It is preferable that the compounding quantity in the case of mix | blending a calcium phosphate compound is 0.5-20 weight% in a composition. When the amount is 0.5% by weight or more, a sufficient effect tends to be obtained, and when the amount is 20% by weight or less, storage stability tends to be maintained. Particularly preferably, it is 1 to 10% by weight.

  In addition to the above components (a) to (e), the composition for tooth application according to the present invention may further contain (g) an antibacterial agent.

(G) By adding an antibacterial agent, an antibacterial and bactericidal effect can be provided on the tooth. Antibacterial agents include sodium azulene sulfonate, ε-aminocaproic acid, allantoin, allantoinchlorohydroxyaluminum, allantoindihydroxyaluminum, epidihydrocholesterine, dihydrocholesterol, glycyrrhizic acid, diammonium glycyrrhizinate, disodium glycyrrhizinate, glycyrrhizic acid tri Sodium, dipotassium glycyrrhizinate, monoammonium glycyrrhizinate, chlorhexidine gluconate, β-glycyrrhetinic acid, isopropylmethylphenol, cetylpyridinium chloride, decalinium chloride, benzalkonium chloride, benzalkonium chloride, benzethonium chloride, benzethonium chloride, hydrochloric acid Alkyldiaminoethylglycine solution, chlorhexidine hydrochloride, chlorogluconate Xidine, triclosan, pyridoxine hydrochloride, dl-α-tocopherol acetate, dl-α-tocopherol nicotinate, zeolite, methyl paraoxybenzoate, ethyl paraoxybenzoate, propyl paraoxybenzoate, butyl paraoxybenzoate, benzyl paraoxybenzoate, pyrroline Disodium dihydrogen acid, sodium pyrophosphate, anhydrous sodium pyrophosphate, sodium monohydrogen phosphate, trisodium phosphate, sodium polyphosphate, stearyldimethylbenzylammonium chloride, lauryldimethylbenzylammonium chloride, distearyldimethylammonium chloride, stearyl chloride Trimethylammonium, cetyltrimethylammonium chloride, lauryltrimethylammonium chloride, stearyltrimethylammonium bromide, cetyltrimethyl bromide Ruammonium, benzalkonium chloride, benzethonium chloride, decalinium chloride, chlorhexidine chloride, chlorhexidine gluconate, chlorhexidine acetate, other chlorhexidine salts, hexetidine, alkyldiaminoethylglycine hydrochloride, domifene bromide, lauroylcoraminoformylmethylpyridinium chloride, cetyl Trimethylammonium saccharin, triclosan, 2,2'-dihydroxy-5,5'-dibromo-diphenyl ether, other halogenated diphenyl ethers, 4 ', 5-dibromosalicylanilide, 3,4', 5-trichlorosalicylamide, etc. Halogenated salicylanilide, 3,4 ', 4-trichlorocarbanilide, 3-trifluoromethyl-4,4-dichlorocarboanilide, other halogenated carboanilide, 2-isopropyl-5-methyl-phenol (thymol), 2-me Xyl-4- (2-propenyl) -phenol (eugenol), other phenol derivatives, methyl-p-chlorophenol, ethyl-p-chlorophenol, other mono- and poly-alkyls, and alkyl-halophenols, resorcinol, hexyl resorcinol, methyl Examples include luresorcinol, methyl-resorcinol, other resorcinol and derivatives thereof, dodecyldiaminoethylglucin, benzoate, lauroyl sarcosine salt, lauryl sulfate and the like. These may be used alone or in combination of two or more.
(G) It is preferable that the compounding quantity of an antibacterial agent is 0.001 to 3 weight% in a composition. Sufficient antibacterial effect is easily obtained when it is 0.001% by weight or more, and sufficient antibacterial effect is obtained at 3% by weight or less. Most preferably, it is 0.01 to 0.5 weight%.

  In addition to the components (a) to (e), the composition for tooth application according to the present invention can further contain (h) a thickener.

  (H) The thickener has an effect of increasing the viscosity of the composition and making it easy to apply such as gel or paste. Thickeners include aerosil, methylcellulose, carboxymethylcellulose, sodium carboxymethylcellulose, carboxymethylcellulose calcium, carboxymethylcellulose potassium, polyvinylpyrrolidone, guar gum, kajib bean gum, tara gum, tamarind seed gum, tragacanth gum, caraya gum, carrageenan, xanthan gum, gellan gum, curdlan Glycerin, sodium alginate, propylene glycol alginate, sodium starch glycolate, sodium starch phosphate, sodium polyacrylate, and the like. These may be used alone or in combination of two or more.

  In addition to the components (a) to (e) above, (i) an organic solvent other than alcohol can be blended in the tooth coating composition according to the present invention.

(I) Organic solvents other than alcohol have the effect of improving the feeling of use and stability. Examples of organic solvents other than alcohol include acetone, methyl ethyl ketone, methyl isobutyl ketone, styrene, n-pentane, isopentane, tetramethylmethane, n-hexane, cyclohexane, n-heptane, 2-methylhexane, 3-methylhexane, and dimethylpentane. , Trimethylbutane, butyl glycol, methyl diglycol, ethyl diglycol, butyl diglycol, dimethyl diglycol, 1-methoxy-2-propanol, methyldipropylene glycol, 3-methoxybutanol, tetrahydrofuran, ethyl acetate, propyl acetate, acetic acid Examples include isopropyl, butyl acetate, isobutyl acetate, butyl cellosolve acetate, ethyl carbitol acetate and the like. These may be used alone or in combination of two or more.
(I) It is preferable that the compounding quantity of organic solvents other than alcohol is 0.5 to 30 weight% in a composition. If it is 0.5% by weight or more, the effect of improving the feeling of use and stability is sufficient, and if it is 30% by weight or less, the coating tends to be easily formed. Particularly preferred is 5 to 20% by weight.

  In addition to the above-mentioned components, additives such as commonly used colorants, flavoring agents, bleaching agents and the like can be appropriately added to the tooth coating composition according to the present invention. Specifically, as a coloring agent, titanium oxide, iron oxide, zinc oxide, mica, silica, alumina, natural pearl, mica titanium, synthetic pigment, etc., as a flavoring agent, sucrose, maltose, sorbitol, xylitol, lactose, Examples of bleaching agents such as sodium saccharin, sucralose, aspartame, acesulfame, various fragrances and flavoring oils include hydrogen peroxide, calcium peroxide, polyphosphate and urea peroxide. These may be used alone or in combination of two or more.

  Although it will not specifically limit if it is a form applicable to a tooth | gear as a form of the composition for tooth application | coating based on this invention, For example, liquid form, gel form, paste form, cream form etc. are mentioned.

  A method for applying the tooth coating composition according to the present invention to the tooth is not particularly limited, and examples thereof include a method of applying using a brush or a cotton swab, a method of spraying by a spray, a method of directly applying to a tooth, and the like.

  EXAMPLES Hereinafter, although an Example and a comparative example are shown and this invention is demonstrated further in detail, this invention is not limited to these Examples.

  Examples 1-7 and Comparative Examples 1-4 are summarized in Table 1. The unit of numerical values in Table 1 is% by weight.

<Evaluation of remineralization effect>
(1) The bovine teeth were cut to a thickness of 1 mm, and the bovine enamel side was polished with # 1500 water-resistant abrasive paper, and then nail polish was applied to leave about 3 mm on the enamel side to obtain a test specimen.
(2) The test specimen was immersed in decalcified gel (lactic acid: 0.1 M, calcium chloride: 1.5 mM, potassium dihydrogen phosphate: 0.9 mM, sodium carboxymethylcellulose: 1 wt%, pH 4.8) for 4 days. And artificial caries were developed.
(3) Manicure was applied to the end portion of the enamel portion of the test body where artificial caries was developed in order to prevent remineralization.
(4) A tooth coating composition having the composition shown in Table 1 was applied to the artificial caries portion of the test specimen, and then dried to form a coating.
(5) An artificial saliva (sodium chloride: 14.4 mM, potassium chloride: 16.1 mM, magnesium chloride: 0.3 mM, potassium hydrogen phosphate: 2.0 mM, calcium chloride: (1.0 mM, pH 7.0) for 2 weeks. The artificial saliva was changed every day.
(6) An X-ray image of the specimen after immersion in artificial saliva was taken with an X-ray CT apparatus (Inspexio SMX-100CT; manufactured by Shimadzu Corporation). With respect to the captured image, in a predetermined area, using the image analysis software “Image J”, the luminance of the enamel surface layer portion that is not decalcified is 255, and the luminance of the lowest luminance portion is 0, The brightness (256 levels from 0 to 255) of the part where nail polish was applied and remineralization was suppressed, and the part where the tooth coating composition was applied were obtained, and the obtained numerical values were used to The conversion rate (%) was determined.
Remineralization rate (%) =
[{255- (Brightness of portion where nail polish is applied and remineralization is suppressed)}-{255- (Brightness of portion where composition for tooth application is applied)}] / {255- (Nail polish is applied and relime is applied) The brightness of the part that suppresses the generation)} × 100
The larger the value, the greater the degree of remineralization. The results are summarized in Table 1.

  As is clear from Table 1, the composition for applying a tooth according to the present invention is applied to a tooth and dried to form a film, and lactobionic acid and / or salt thereof contained as a component, and hydrogen phosphate. It has been confirmed that it has the effect of promoting the remineralization of teeth at the same level or higher than that of a tooth coating composition containing a high concentration of fluorine compounds, despite the fact that it does not contain fluorine compounds, due to the action of salt. It was done.

Claims (1)

  (A) lactobionic acid or a salt thereof, (b) hydrogen phosphate, (c) a film-forming polymer, (d) alcohol, and (e) water, which are used by applying to teeth. A composition for applying a tooth.