JPWO2010143589A1 - Oral composition - Google Patents

Abstract

(A) Ascorbic acid phosphate ester or salt thereof, (B) Vitamin E or derivative thereof, (C) POE hydrogenated castor oil having 10 to 60 average EO addition moles, EO average addition moles with alkyl groups of C14 to 18 A surfactant comprising 5 to 8 POE alkyl ethers and alkyl glucosides having an alkyl group of C10 to 14 and (D) a nonionic fungicide, and a total of (A), (B) and (D) The amount is 0.2-1.5% by mass, (C) / ((B) + (D)) is 8-20 by mass ratio, (A)-(C) component, and (E) cationic sterilization The total amount of components (A), (B) and (E) is 0.2 to 1.3% by mass, and (C) / ((B) + (E)) is 8 to 8 by mass ratio. The composition for oral cavity which is 18, and according to the present invention, ascorbic acid phosphate ester or salt thereof, Vita Emissions E or derivatives thereof, and fungicides are stable and effective formulation, exert prophylactic or improvement effect of excellent periodontal disease, and excellent storage stability over time.

Description

  The present invention relates to an oral composition containing an ascorbic acid phosphate ester or a salt thereof, exhibiting a high periodontal disease prevention or improvement effect and excellent in storage stability over time. Among the symptoms associated with the disease, the effect of improving bad breath and gingival crevicular fluid volume increase is particularly high, and the storage stability of ascorbic acid phosphate or its salt over time is excellent, and separation and discoloration are prevented and the appearance The present invention relates to a composition for oral cavity that is also excellent in stability.

  Periodontal disease is counted as one of the major causes of tooth loss, and its prevention is expected to lead to an improvement in QOL (Quality of Life). Many periodontal diseases are thought to be infections caused by bacteria, mainly obligate anaerobic gram-negative bacilli, resulting in destruction of connective tissue and alveolar bone. Redness, swelling, bleeding, drainage, bad breath, etc. are observed as clinical findings in this process. There is also a bacterial-host reaction between cause and effect.

  In chronic periodontal diseases, it is known that tissue destruction is caused by a host-derived enzyme such as collagenase while the cycle of inflammation circulates. In addition, in the tissue, accumulation of neutrophils in the periodontal pocket, infiltration of lymphocytes into the gingival tissue, etc. are observed, and plasmin, a fibrinolytic enzyme, is involved in gingiva affected by periodontal disease. It has been reported that

  In the living body, neutrophils have a function of killing bacteria and protecting the living body. However, particularly in chronic inflammation, leakage of cellular components and production of excessive active oxygen adversely affect living tissues. Therefore, it is useful to prevent tissue destruction by active oxygen by using an antioxidant such as ascorbic acid phosphate or a salt thereof. It is described in, for example, Patent Document 1 that blending an ascorbic acid phosphate ester or a derivative thereof into an oral composition is effective in preventing periodontal disease. However, ascorbic acid phosphate ester is easily decomposed in the preparation, and there is a problem that the storage stability is not sufficient when water or an anionic surfactant is present.

  In addition, promoting gingival blood circulation and activating metabolism is also effective in preventing periodontal disease. Vitamin E (also known as tocopherol) derivatives are effective in preventing periodontal diseases because they have an antioxidant effect in addition to blood circulation promoting effects. For example, Patent Document 2 discloses that blending a vitamin E derivative into an oral composition is effective in preventing periodontal disease. However, there is a problem that vitamin E derivatives are easily decomposed in the preparation and it is difficult to ensure storage stability.

  Moreover, in order to solubilize and stably mix an oil-soluble vitamin E derivative in an oral composition, it is common to use a surfactant in combination. However, in this case, depending on the amount of the surfactant, the micelle formed by the surfactant becomes too rigid, and the vitamin E derivative incorporated in the micelle is not released at the target site, and the effect is exhibited. There was a problem that it became difficult.

  It is described in, for example, Patent Document 3 and the like that a bactericidal agent that exhibits an effect by directly reducing the number of oral bacteria that cause inflammation of gums is effective in preventing and improving periodontal diseases. . However, it is common to use a surfactant to solubilize a bactericidal agent in an oral composition and stably mix it, but depending on the amount of surfactant, micelles formed by the surfactant may be rigid. Therefore, there was a problem that the bactericide incorporated in the micelle was not released at the target site, making it difficult to exert its effect.

  As described above, ascorbic acid ester or a salt thereof, vitamin E or a derivative thereof, and a bactericidal agent still have room for improvement in terms of stably blending them into the oral composition and sufficiently exerting these effects. It has been difficult to stably blend the ingredients at the same time to achieve high effects and to improve storage stability over time.

  Patent Document 4 discloses a dentifrice composition containing an ascorbic acid phosphate salt, a vitamin E derivative, and a cationic fungicide, a vitamin E derivative, a cationic fungicide, and polyoxyethylene hydrogenated castor oil (hereinafter, polyoxyethylene is POE). In Japanese Patent Application Laid-Open No. 2003-318, a composition containing a vitamin E derivative, a cationic bactericidal agent and POE hydrogenated castor oil in combination with a non-aqueous oral cavity composition is described. ing. However, the periodontal disease preventive effect of these compositions is not sufficient, and there is no description of an appropriate average number of moles of ethylene oxide added to POE hydrogenated castor oil (hereinafter referred to as EO average number of moles added). In addition, Patent Document 6 describes a composition using an ascorbic acid phosphate ester salt, a vitamin E derivative and a nonionic fungicide in combination as a caries prevention coating composition containing no abrasive. However, solubilization and blending stability of vitamin E derivatives and nonionic fungicides are not sufficient.

  As dentifrice composition containing vitamin E or its derivative, ascorbic acid phosphate, vitamin E derivative, POE stearyl ether (EO average addition mole number 5), POE hydrogenated castor oil (EO average addition mole number 40) and cation Patent Document 7 describes a composition using a combination of anaerobic fungicide. However, in this composition, it is difficult to say that the mixing ratio of each component is appropriate. For this reason, the micelle formed by the surfactant becomes too rigid, and the vitamin E derivative and the bactericide incorporated in the micelle are in the target site. It was not released sufficiently and there was room for improvement in the manifestation of the effect.

  Patent Document 8 describes a composition in which an ascorbic acid phosphate ester salt, a vitamin E derivative, a POE alkyl ether, and a nonionic fungicide are blended as an oral composition containing vitamin E or a derivative thereof. However, in this composition, it is difficult to say that the blending ratio of each component, in particular, the blending ratio of the POE alkyl ether to the vitamin E derivative and the nonionic fungicide is appropriate. For this reason, the stability of the vitamin E derivative and the nonionic fungicide That is not enough. Furthermore, Patent Document 8 does not define the alkyl group part of the POE alkyl ether, and there is a description that the ascorbic acid derivative stabilizes vitamin E. However, simultaneous stabilization of vitamin E and ascorbic acid derivative is described. Is not shown.

  The applicant formulated an oral composition containing an ascorbic acid phosphate ester salt and a POE hydrogenated castor oil having an EO average addition mole number of 5 to 10, and adjusted the pH to 6.5 to 9.0. A product was proposed in Japanese Patent Application No. 2007-326959 (Japanese Patent Laid-Open No. 2009-149537). This application includes ascorbic acid phosphate salt, vitamin E derivative, PEO hydrogenated castor oil with 5 and 20 EO average addition moles, POE cetyl ether with 7 EO average addition moles and isopropylmethylphenol in Example 30. The composition to contain is described. However, this technology improves the oral retention and mucosal permeability of ascorbic acid phosphate ester salt by blending specific POE hydrogenated castor oil and adjusting the pH, and is derived from ascorbic acid phosphate ester salt. The effect can be effectively exhibited, and the technical idea is different from the present invention.

  In addition, none of the techniques listed here includes a description regarding techniques for suppressing bad breath derived from periodontal diseases, and the technical idea and operational effects of the configuration of the present invention cannot be derived from these techniques.

  Therefore, the composition for oral cavity which has solved the above-mentioned problems, has a higher preventive or ameliorating effect on periodontal diseases, and has excellent storage stability over time, and appearance stability typified by prevention of separation and discoloration. Development of things is desired.

JP 2007-169201 A JP 2005-350483 A JP 2006-312588 A JP 2005-239654 A JP 2002-114656 A JP 2005-187333 A JP 2005-247786 A JP 2004-323488 A

"Thinking about periodontal disease and general health-a bridge to new health sciences", Lion Dental Institute, Ed. 221 "Thinking about periodontal disease and general health-a bridge to new health sciences", Lion Dental Institute, Ed. 116

  The present invention has been made in view of the above circumstances, and ascorbic acid phosphate or a salt thereof, vitamin E or a derivative thereof, and a bactericidal agent are stably and effectively blended, and has an excellent periodontal disease prevention or improvement effect. An object of the present invention is to provide an oral composition that is effective and has excellent storage stability over time.

As a result of intensive studies to achieve the above object, the present inventors have (A) ascorbic acid phosphate ester or salt thereof, (B) vitamin E or derivative thereof, and (C) EO average added mole number. POE hydrogenated castor oil having 10 to 60 moles, POE alkyl ether having 14 to 18 carbon atoms in the alkyl group and 5 to 8 moles of EO average addition mole, and alkyl glucoside having 10 to 14 carbon atoms in the alkyl group One or more selected surfactants are blended, and (D) a nonionic germicide or (E) a cationic germicide is blended as a germicide, and the blending amounts and blending ratios of these components are shown below. It was found that the composition for oral cavity in such a suitable range is excellent in preventing or ameliorating periodontal disease and excellent in storage stability over time.
According to the present invention, ascorbic acid phosphate or a salt thereof, vitamin E or a derivative thereof, and a bactericidal agent are stably blended at the same time, the effects derived from these components are effectively expressed, and bad breath and gums derived from periodontal diseases. A high effect of improving the increase in the amount of cough exudate (hereinafter referred to as GCF) and a high bactericidal effect on periodontal disease-causing bacteria are exhibited at the same time. Acid ester or a salt thereof and vitamin E or a derivative thereof are blended stably over a long period of time, and separation and discoloration do not occur over time, and the storage stability over time is excellent.

  That is, in the present invention, the composition as described above can provide an oral composition having a high periodontal disease improving effect and excellent storage stability with time, which cannot be achieved by the conventional techniques. Ascorbic acid phosphate or a salt thereof, vitamin E or a derivative thereof, and a bactericidal agent are known to be effective in preventing or ameliorating periodontal diseases. However, in the present invention, as will be understood from the examples described later. In addition, by combining the above ingredients and blending them at an appropriate blending amount and ratio, these ingredients act synergistically, and in particular, among the symptoms associated with periodontal diseases, a high effect of improving the bad breath and the increase in the amount of GCF is exhibited. In addition, a high bactericidal effect on periodontal disease-causing bacteria is also exhibited. Furthermore, in the present invention, ascorbic acid phosphate ester or a salt thereof and vitamin E or a derivative thereof are stably retained even after long-term storage, and the effects derived from these components can be stably expressed over time. In addition, separation and discoloration do not occur during long-term storage, and good appearance stability is achieved. Such operational effects of the present invention are exceptional that cannot be achieved if any of the essential components according to the present invention is missing or the blending amount and ratio of each component is inappropriate.

  Although bad breath due to periodontal disease is produced by gram-negative bacteria in the oral cavity, the sulfur-containing amino acid serving as the substrate is supplied from GCF or blood. When suffering from a periodontal disease, the amount of GCF increases, that is, a bad breath is generated because the substrate of bad breath production increases (Non-patent Document 1). In the present invention, a high periodontal disease improving effect is exhibited, and the amount of sulfur-containing amino acid that is a substrate of halitosis production is reduced by reducing the amount of GCF, and that the bactericidal agent sterilizes halitosis producing bacteria synergistically. However, it is estimated that this is one factor that suppresses bad breath derived from periodontal diseases. This GCF is present in the gingiva and gingival crevice, and actively blocks foreign substances such as bacteria and toxins by antibody components, etc., and contributes to biological defense. On the other hand, interleukin (hereinafter referred to as IL) Abbreviations) -1, cytokines such as IL-6, IL-8, and the like have been suggested to be associated with periodontal diseases (Non-patent Document 2). In the present invention, the periodontal disease is remarkably improved, the amount of GCF once increased is decreased, the substrate of bad breath production is reduced, and the bactericidal agent sterilizes the bad breath producing bacteria. It is speculated that this can be suppressed. In addition, since the amount of GCF increases when suffering from a periodontal disease and decreases when it improves, it is used as an index for measuring the degree of severity and improvement of the periodontal disease.

  The composition of the present invention further contains (F) glycyrrhetinic acid, ε-aminocaproic acid, glycyrrhizinate, tranexamic acid, buckwheat extract, and allantoin to prevent periodontal disease. Alternatively, the improvement effect is further improved, and the amount of GCF that has increased with the onset of periodontal disease can be more effectively reduced.

Accordingly, the present invention provides the following oral composition.
Claim 1;
(A) Ascorbic acid phosphate or a salt thereof,
(B) Vitamin E or a derivative thereof,
(C) Polyoxyethylene hydrogenated castor oil having an average addition mole number of ethylene oxide of 10 to 60 moles, polyoxyethylene alkyl having an alkyl group of 14 to 18 carbon atoms and an average addition mole number of ethylene oxide of 5 to 8 moles One or more surfactants selected from ethers and alkyl glucosides having 10 to 14 carbon atoms in the alkyl group,
(D) contains a nonionic fungicide, the total content of components (A), (B) and (D) is 0.2 to 1.5% by mass, and (C) / ((B) + (D)) is 8-20 by mass ratio, The composition for oral cavity characterized by the above-mentioned.
Claim 2;
(D) The composition for oral cavity according to claim 1, wherein the nonionic fungicide is isopropylmethylphenol or triclosan.
Claim 3;
(A) Ascorbic acid phosphate or a salt thereof,
(B) Vitamin E or a derivative thereof,
(C) Polyoxyethylene hydrogenated castor oil having an average addition mole number of ethylene oxide of 10 to 60 moles, polyoxyethylene alkyl having an alkyl group of 14 to 18 carbon atoms and an average addition mole number of ethylene oxide of 5 to 8 moles One or more surfactants selected from ethers and alkyl glucosides having 10 to 14 carbon atoms in the alkyl group,
(E) contains a cationic fungicide, the total content of components (A), (B) and (E) is 0.2 to 1.3% by mass, and (C) / ((B) + (E)) is 8-18 by mass ratio, The composition for oral cavity characterized by the above-mentioned.
Claim 4;
(E) The composition for oral cavity according to claim 3, wherein the cationic fungicide is at least one selected from cetylpyridinium chloride, benzethonium chloride, benzalkonium chloride, chlorhexidine gluconate, and chlorhexidine hydrochloride.
Claim 5;
The total content of the component (A), the component (B), and the component (D) or (E) is 0.2 to 1.0% by mass, and (C) / [(B) + (( The composition for oral cavity according to any one of claims 1 to 4, wherein D) or (E))] is 8 to 15 in terms of mass ratio.
Claim 6;
Furthermore, (F) 1 or more types chosen from glycyrrhetinic acid, (epsilon) -aminocaproic acid, a glycyrrhizinate, tranexamic acid, a buckwheat extract, and allantoins are contained, The any one of Claims 1 thru | or 5 characterized by the above-mentioned. Oral composition.

  The oral composition of the present invention exhibits a high effect of improving an increase in halitosis and the amount of GCF, among other symptoms associated with periodontal diseases, and a high bactericidal effect on periodontal disease-causing bacteria, and preservation over time Excellent stability and excellent appearance stability represented by separation and discoloration. Furthermore, the inhibitory effect of the higher increase in the amount of GCF is exhibited by mix | blending the said (F) component. Therefore, the composition for oral cavity of the present invention is useful for prevention or improvement of periodontal diseases.

  Hereinafter, the present invention will be described in more detail. The composition for oral cavity of the present invention comprises (A) ascorbic acid phosphate or a salt thereof, (B) vitamin E or a derivative thereof, (C) a specific surfactant, And (D) a nonionic fungicide or (E) a cationic fungicide as a fungicide.

  (A) Ascorbic acid phosphoric acid ester and its salt, one or two or more hydroxyl groups at any of the 2, 3, 5, and 6 positions of ascorbic acid became esters of compounds such as phosphoric acid and polyphosphoric acid. For example, ascorbic acid-2-phosphate, ascorbic acid-3-phosphate, ascorbic acid-6-phosphate, ascorbic acid-2-polyphosphate, etc. , Alkali metal salts such as sodium salt, potassium salt, calcium salt and magnesium salt, and alkaline earth metal salts. In particular, magnesium salts and sodium salts of ascorbic acid phosphate ester, that is, L-ascorbyl magnesium phosphate and sodium L-ascorbyl phosphate are preferably used from the viewpoint of use for oral cavity and the effect of preventing gingivitis.

  Ascorbic acid phosphate ester and salts thereof are commercially available products. Specifically, L-ascorbyl magnesium phosphate is Showa Denko KK (trade name: ascorbic acid PM), Wako Pure Chemical Industries, Ltd. (trade name: phosphorus L-ascorbyl sodium phosphate, such as L-ascorbyl acid phosphate, is available from DSM Nutrition Japan (trade name: Stay-C50), BASF Japan Ltd. (trade name: L-ascorbyl sodium phosphate), etc. it can.

  The compounding amount of ascorbic acid phosphate or a salt thereof is 0.05 to 0.8% (mass%, the same applies hereinafter) of the entire composition from the viewpoint of periodontal disease prevention effect and storage stability over time, and particularly 0. .1 to 0.5% is preferable. If the compounding amount is less than 0.05%, the effect of preventing or improving periodontal disease cannot be obtained sufficiently, and if it exceeds 0.8%, discoloration may occur over time, and irritation will be adversely affected. There is a case.

(B) As vitamin E or a derivative thereof (hereinafter, vitamin E is abbreviated as VE), d-α-tocopherol, dl-α-tocopherol, β-tocopherol, γ-tocopherol, δ-tocopherol and acetic acid thereof Further, esters or salts with organic acids such as nicotinic acid, succinic acid and linolenic acid can be used. Examples of the VE derivative include d-α-tocopherol acetate, dl-α-tocopherol acetate, d-α-tocopherol nicotinate, dl-α-tocopherol nicotinate, d-α-tocopherol succinate, dl-α-succinate. Tocopherol, linolenic acid d-α-tocopherol, linolenic acid dl-α-tocopherol, tocopherol calcium succinate and the like can be mentioned.
Vitamin E or a derivative thereof is particularly dl-α-tocopherol, dl-α-tocopherol acetate, nicotinic acid dl because it has high physiological activity and is colorless to pale yellow and hardly affects the color tone or appearance of the preparation. -Α-tocopherol is preferred. In addition, VE or its derivative (s) can be mix | blended individually by 1 type or in combination of 2 or more types.

  As VE or a derivative thereof, those conforming to the former cosmetic raw material standard (Making basic group) or quasi-drug raw material standard 2006 can be used, and those generally used in cosmetics and oral compositions can be used. . As VE or a derivative thereof, a commercial product sold by DSM Nutrition Japan, Eisai Food Chemical, BASF Japan, or the like can be used.

  The blending amount of VE or a derivative thereof is preferably 0.05 to 0.5%, particularly 0.05 to 0.3% of the whole composition from the viewpoint of periodontal disease prevention effect and storage stability over time. If the blending amount is less than 0.05%, the periodontal disease prevention / amelioration effect cannot be sufficiently obtained, and if it exceeds 0.5%, it is difficult to solubilize in the preparation, and separation or discoloration occurs over time, It may become oily and have a poor taste.

  Component (C) is a POE alkyl ether having an EO average addition mole number of 5 to 8 mol and an alkyl group having 14 to 18 carbon atoms, a POE hydrogenated castor oil having an EO average addition mole number of 10 to 60 mol, and an alkyl group. Are one or more nonionic surfactants selected from alkyl glucosides having 10 to 14 carbon atoms.

  As the POE alkyl ether, those having an alkyl group having 14 to 18 carbon atoms, preferably 16 to 18 carbon atoms are preferable. If the alkyl group has less than 14 carbon atoms, the lipophilicity is low, so that the oil-soluble component is not sufficiently solubilized, and sufficient foaming properties cannot be obtained. Due to its small size, the oil-soluble component is insufficiently solubilized, and a unique taste and oiliness are produced during use of the preparation. Specific examples of the POE alkyl ether include POE cetyl ether, POE myristyl ether, POE stearyl ether and the like, and POE stearyl ether is particularly preferable.

Moreover, the EO average addition mole number of POE alkyl ether is in the range of 5 to 8 moles. When the EO average added mole number is lower than 5 moles, the solubilizing ability is insufficient, so that the oil-soluble liquid component is separated in the preparation. Deterioration occurs and the feeling of use becomes inferior.
As such POE alkyl ether, commercially available products such as EMALEX 105, 107, 605, and 608 of Nippon Emulsion Co., Ltd. can be used.

As the POE hydrogenated castor oil, those having an EO average added mole number of 10 to 60 can be used. For example, when used for a toothpaste, those having an EO average addition mole number of 10 to 30 are particularly preferred, and when used for a mouthwash, those having an EO average addition mole number of 40 to 60 are particularly preferred. If the EO average added mole number is less than 10 moles, the solubilizing ability of the oil-soluble component is insufficient, and particularly when it is prepared as a toothpaste, rough skin at a low temperature may occur and the appearance may deteriorate. If it exceeds 60 mol, the solubilizing ability of oil-soluble components such as vitamin E or its derivatives and bactericides, as well as oil-soluble active ingredients and fragrance ingredients may be inferior and the oil-soluble ingredients may be separated.
As such POE hydrogenated castor oil, commercially available products such as NIKKOL HCO-10, HCO-20, HCO-30, HCO-40, HCO-50, and HCO-60 from Nikko Chemicals Co., Ltd. can be used. .

As the alkyl glucoside, those having 10 to 14 carbon atoms, preferably 10 to 12 carbon atoms, are used. If the number of carbon atoms is less than 10, sufficient foaming properties cannot be obtained, and if it exceeds 14, a unique taste or oiliness is produced during use.
As such an alkyl glucoside, commercially available products such as planter care 1200UP and planter care 2000UP manufactured by Cognis can be used.

  (C) As a component, you may mix | blend the above-mentioned POE alkyl ether, POE hydrogenated castor oil, or alkyl glucoside, or mix | blend combining 2 or more types chosen from POE alkyl ether, POE hydrogenated castor oil, and alkyl glucoside. May be. When using 2 or more types together, combined use of POE alkyl ether and POE hydrogenated castor oil is preferable. In the case of a dentifrice such as a toothpaste, a POE-cured castor having an alkyl group with 16 to 18 carbon atoms and an EO average addition mole number of 5 to 8 moles and an EO average addition mole number of 10 to 30 It is preferable to use oil in a mass ratio of 3: 7 to 7: 3. In particular, when a POE alkyl ether having an alkyl group with 16 to 18 carbon atoms and an EO addition mole number of 6 or less is used, a POE hydrogenated castor oil having an EO average addition mole number of 20 to 40 is used in combination. In the case of using POE hydrogenated castor oil having an addition mole number of less than 20, it is possible to use a POE alkyl ether having an alkyl group having 16 to 18 carbon atoms and an EO average addition mole number of 7 to 8 in order to stabilize the component (B). Most preferable from the standpoint of property and suppression of separation.

  The total blending amount of the nonionic surfactant (C) is 0.5 to 5% of the total composition, particularly from the viewpoint of solubilization ability of oil-soluble ingredients, expression of effects of oil-soluble ingredients, and usability. 0.5 to 3% is preferable. If the blending amount is less than 0.5%, sufficient oil-soluble component solubilizing ability cannot be obtained, and VE or its derivatives and nonionic fungicides are not sufficiently solubilized, resulting in insufficient storage stability. is there. If it exceeds 5%, the micelle due to component (C) becomes too rigid and the oil-soluble active ingredient taken into the micelle is not released into the oral cavity, so it is sufficient to prevent and improve periodontal disease and bad breath May not be obtained, or bitterness or irritation may occur and the preparation cannot be applied to the oral cavity for a long time. In particular, in the case of dentifrice, since many oil-soluble components such as fragrances are blended, the blending amount is most preferably 1 to 3%.

  Furthermore, (D) nonionic fungicide or (E) cationic fungicide is mix | blended with this invention composition as a fungicide.

  (D) Nonionic fungicides include isopropylmethylphenol, triclosan, hinokitiol, phenol, etc., and one or more of these can be used. In particular, in terms of bactericidal power and taste, isopropylmethylphenol Phenol and triclosan are preferred. Commercially available products can be used for nonionic fungicides, isopropylmethylphenol can be obtained from Osaka Kasei Co., Ltd. (trade name: isopropylmethylphenol), and triclosan can be obtained from Ciba Specialty Chemicals Co., Ltd. (trade name: Irgasan DP-300). Can do.

  The blending amount of the nonionic fungicide is preferably 0.01 to 0.3%, particularly preferably 0.02 to 0.1% of the whole composition from the viewpoint of periodontal disease prevention effect and usability. If the blending amount is less than 0.01%, the bactericidal effect is inferior, the periodontal disease and bad breath amelioration effect by sterilization is not sufficiently obtained, and even if the blending amount exceeds 0.3%, it is not solubilized and separated over time Or discoloration may occur, or bitterness may occur, resulting in poor usability.

  (E) Cationic fungicides include quaternary ammonium compounds such as cetylpyridinium chloride, benzethonium chloride, benzalkonium chloride and decalinium chloride, bisguanides such as chlorhexidine gluconate and chlorhexidine hydrochloride, and alkyldiaminoethylglycine hydrochloride. 1 type or 2 types or more are used, and quaternary ammonium type and bisguanide type are particularly preferable in terms of bactericidal power and taste. Among them, cetylpyridinium chloride, benzethonium chloride, benzalkonium chloride, gluconic acid Most preferred are chlorhexidine and chlorhexidine hydrochloride.

  Commercially available cationic fungicides can be used, cetylpyridinium chloride is Wako Pure Chemical Industries (trade name: cetylpyridinium chloride), benzethonium chloride is Lonza Japan (trade name: Hyamine 1622), and benzalkonium chloride is sweet potato chemistry. Sangyo Co., Ltd. (trade name: 10% benzalkonium chloride solution), Chlorhexidine Gluconate is Dainippon Sumitomo Pharma Co., Ltd. (trade name: Hibiten Gluconate Solution), Chlorhexidine Hydrochloride is Dainippon Sumitomo Pharma Co., Ltd. (trade name: 5% Hibiten) Liquid) or the like.

  The blending amount of the cationic bactericidal agent is preferably 0.001 to 0.1%, particularly preferably 0.01 to 0.05% of the whole composition from the viewpoint of periodontal disease prevention effect and usability. If the blending amount is less than 0.001%, the bactericidal effect is inferior, the periodontal disease and bad breath improving effect due to sterilization cannot be sufficiently obtained, and if it exceeds 0.1%, bitterness etc. occurs and the feeling of use becomes worse, May cause discoloration.

  In the present invention, the total amount of (A) ascorbic acid phosphate or a salt thereof, (B) vitamin E or a derivative thereof, and (D) a nonionic bactericidal agent is effective for preventing periodontal diseases and appearance stability. From the point, it is 0.2 to 1.5% of the whole composition, and 0.2 to 1.0% is particularly preferable. If the total blending amount is less than 0.2%, the periodontal disease prevention effect is not sufficiently exhibited, and if it exceeds 1.5%, the component (A), (B) or (D) is separated over time or discoloration occurs. Arise.

  Furthermore, the blending ratio of the components (C), (B) and (D) is (C) / ((B) + (D) from the viewpoint of the periodontal disease prevention effect, the stability of the component (B) and the suppression of separation. )) Is a mass ratio of 8 to 20, and a range of 8 to 15 is particularly preferred. If the blending ratio is less than 8, the component (B) or the component (D) is not solubilized, resulting in insufficient storage stability or separation in the preparation, and if it exceeds 20, the micelle by the component (C) Becomes too rigid, and the component (B) and component (D) incorporated in the micelle are not released into the oral cavity, and the periodontal disease prevention effect is not sufficiently exhibited.

  In the present invention, the total amount of (A) ascorbic acid phosphate or a salt thereof, (B) vitamin E or a derivative thereof, and (E) a cationic fungicide is a point of periodontal disease prevention effect and appearance stability. Therefore, it is 0.2 to 1.3% of the whole composition, and 0.2 to 1.0% is particularly preferable. If the total blending amount is less than 0.2%, the periodontal disease prevention effect is not sufficiently exhibited, and if it exceeds 1.3%, the component (A), (B) or (E) is separated over time or discoloration occurs. Arise.

  Further, the blending ratio of the components (C), (B) and (E) is (C) / ((B) + (E) in terms of periodontal disease prevention effect, stability of the component (B) and appearance stability. )) Is a mass ratio of 8-18, and a range of 8-15 is particularly preferred. When the blending ratio is less than 8, the component (B) is not solubilized, so the storage stability becomes insufficient and separation occurs in the preparation. When it exceeds 18, the micelle by the component (C) becomes too rigid. The components (B) and (E) incorporated in the micelles are not released into the oral cavity, and the effects derived from these components are not fully exhibited.

  In particular, in the present invention, the total content of the component (A), the component (B), and the component (D) or (E) is 0.2 to 1.0%, and (C) / ((B ) + ((D) or (E)) is most effective because the mass ratio is 8 to 15 because the effect of preventing or improving periodontal disease is further improved and the storage stability with time is excellent. .

  The oral composition of the present invention further contains (F) one or more active ingredients selected from (F) glycyrrhetinic acid, ε-aminocaproic acid, glycyrrhizinate, tranexamic acid, buckwheat extract and allantoins. It is preferable. By blending the component (F), the periodontal disease prevention / amelioration effect can be further improved, and as a result, the leaching of GCF associated with the periodontal disease can be further suppressed. Allantoins include allantoin, allantoinchlorohydroxyaluminum, and allantoindihydroxyaluminum (also known as aldioxa).

  Component (F) may be a natural product or a synthetic product, and a commercially available product can be used. Specifically, glycyrrhetinic acid is Maruzen Pharmaceutical Co., Ltd. (trade name: glycyrrhetinic acid), ε-aminocaproic acid is Daiichi Chemicals Co., Ltd. (trade name: epsilon-aminocaproic acid) and Ajinomoto Co. (trade name: epsilon-aminocaproic acid), Examples of glycyrrhizinate include dipotassium glycyrrhizinate Maruzen Pharmaceutical Co., Ltd. (trade name: glycyrrhizin K2) and Alps Yakuhin Kogyo Co., Ltd. (trade name: glycyrrhizic acid 2K). Awaku Extract is Oshiro Pharmaceutical Co., Ltd. (trade name: Awaku Extract) and Iwase Cosfa (trade name: Awaku Liquid E), Allantoin is DSM Nutrition Japan (trade name: Allantoin), Allantoin Chloroxyaluminum is Merck (trade name: RonaCare Allan Toin (registered trademark)) and allantoin dihydroxyaluminum include those available from Kawaken Fine Chemical Co., Ltd. (trade name: ALDA).

  (F) When mix | blending component, the compounding quantity is 0.01 to 0.5% of the whole composition, and especially 0.01 to 0.3% from the point of a periodontal disease prevention effect or a usability | use_condition. If the blending amount is less than 0.01%, the GCF amount increase inhibitory effect may not be satisfactorily exhibited and the periodontal disease prevention effect may not be sufficiently improved. It can happen.

  Dextranase can be further added to the oral composition of the present invention. By adding dextranase, it becomes easy to decompose and remove plaque, which is one of the causes of periodontal diseases, and the effect of preventing and improving periodontal diseases can be further enhanced.

  Dextranase is an enzyme produced by the genus Ketomium, the genus Penicillium, the genus Aspergillus, the genus Spicaria, the genus Lactobacillus, the genus Servibrio, and has a plaque-degrading action. Dextranase can be obtained from Daiichi Sankyo Propharma Co., Ltd. (trade name: dextranase).

  In the case where dextranase is blended, the blending amount is preferably 2 to 200 units / g, particularly 10 to 50 units / g, from the viewpoint of plaque degradation effect and formulation stability. One unit of dextranase is the amount of dextranase that produces a free reducing sugar corresponding to 1 μmol of glucose per minute when the reaction is carried out using dextran as a substrate. For example, when 13,000 units / g dextranase is used, the blending amount is preferably 0.016 to 1.5%, particularly 0.08 to 0.38% of the entire composition. If the blending amount is less than 2 units / g, the blending effect, for example, a sufficient plaque removing effect may not be obtained. If it exceeds 200 units / g, discoloration of the preparation may occur.

  The oral composition of the present invention can further contain a fluoride ion source. By compounding a fluoride ion supply source, it is possible to reinforce the tooth quality of the root part exposed as a result of gingival retraction due to periodontal disease, and to prevent or suppress the development or progression of root caries. The tooth root part is easily dissolved in acid, so it tends to be caries. However, in the case of healthy gingiva, the tooth root part is inside the gingiva, so it does not come into contact with acid and does not become caries. . However, if the gingiva retreats due to periodontal disease, the root of the tooth is exposed and dissolved by contact with acid, resulting in caries. This is called “root caries”. In the present invention, by incorporating a fluoride ion supply source, the tooth quality at the root portion is strengthened and hardly dissolved in the acid, and the development or progression of root caries can be prevented or suppressed.

  Fluorine ion supply sources include sodium fluoride, potassium fluoride, ammonium fluoride, tin fluoride, amine fluoride, sodium monofluorophosphate, potassium monofluorophosphate, sodium silicon fluoride, calcium calcium fluoride, etc. It is done. These can use 1 type (s) or 2 or more types, However, Sodium fluoride and sodium monofluorophosphate are preferable especially in terms of taste. In addition, a commercially available fluorine ion supply source can be used, for example, sodium fluoride can be obtained from Stella Chemifa Corporation, and sodium monofluorophosphate can be obtained from Albright & Wilson Corporation.

  When blending a fluorine ion source, the blending amount is preferably 0.02 to 10.0%, particularly 0.05 to 1.5% of the entire composition from the viewpoint of root caries prevention effect and solubility. . For example, in the case of sodium fluoride, 0.02 to 3.0%, particularly 0.05 to 1.5%, and in the case of sodium monofluorophosphate, 0.05 to 10.0%, particularly 0.1 to 5%. In the case of 0.0% and tin fluoride, 0.01 to 1.6%, particularly 0.03 to 0.8% is preferable. If the blending amount of the fluoride ion source is less than 0.02%, a satisfactory blending effect may not be obtained, and if it exceeds 10.0%, solubilization in the preparation may be difficult.

The composition for oral cavity of the present invention includes various kinds of toothpastes such as toothpaste, toothpaste, foam toothpaste, liquid toothpaste, liquid toothpaste, mouthwash, mouth freshener, oral pasta, gargle tablets, chewing gum and the like. And can be suitably prepared as a dentifrice or mouthwash.
In this case, the composition for oral cavity can be blended with other known components in addition to the above components according to various dosage forms within a range not impairing the effects of the present invention, and can be prepared by a usual method. it can. As optional components that can be blended, abrasives, wetting agents, binders, solvents, surfactants other than the above component (C), further sweeteners, preservatives, various active ingredients, pH adjusters, if necessary, A coloring agent, a fragrance | flavor, etc. can be mix | blended and these components can be mixed and manufactured.

Examples of the abrasive include silica-based abrasives such as silica gel, precipitated silica, aluminosilicate, zirconosilicate, and amorphous anhydrous silicic acid, dicalcium phosphate dihydrate, dibasic calcium phosphate anhydride, tricalcium phosphate, fourth Calcium phosphate, eighth calcium phosphate, calcium pyrophosphate, aluminum hydroxide, alumina, titanium dioxide, insoluble calcium metaphosphate, light calcium carbonate, heavy calcium carbonate, magnesium carbonate, tribasic magnesium phosphate, zeolite, polymethyl methacrylate, nylon powder, Examples thereof include silk powder, cellulose powder, and glucomannan.
The compounding quantity of an abrasive | polishing agent is 0-50% normally, and 2-40% is especially preferable in a dentifrice composition.

  Examples of the wetting agent include sorbitol, glycerin, propylene glycol, polyethylene glycol having an average molecular weight of 200 to 6000, 1,3-butylene glycol, xylitol, erythritol, lactitol, palatinose, palatinit, trehalose, and other sugar alcohols and polyhydric alcohols. (The amount is usually 0 to 50%, particularly 5 to 45%).

  Binders include xanthan gum, sodium polyacrylate, carrageenan, sodium alginate, propylene glycol alginate, carboxyvinyl polymer, tragacanth gum, guar gum, hydroxypropyl guar gum, tara gum, locust bean gum, karaya gum, quince seed gum, tamarind gum, carboxy Sodium methylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, methylcellulose, cellulose, gellan gum, gelatin, curdlan, gum arabic, agar, pectin, sodium caseinate, polyvinyl alcohol, polyvinylpyrrolidone, pullulan, thickening silica, beegum, smectite , Laponite, montmorillonite, bentonai Etc. The (amount is usually 0-5%. Especially 0.1% to 5%).

  As the solvent, water is generally used. In the case of containing water, the amount is usually 1 to 99%, and usually 1 to 50% in the dentifrice composition. A lower alcohol such as ethanol may be blended as a solvent, and the blending amount of the lower alcohol is preferably 0.1 to 30%. The total amount of the solvent is usually 0 to 99%.

As the surfactant, in addition to the surfactant of component (C), other nonionic surfactants, anionic surfactants, cationic surfactants, and amphoteric surfactants can be blended. Specifically, POE polyoxypropylene copolymer, sucrose fatty acid ester, sorbitan fatty acid ester, glycerin fatty acid ester, polyglycerin fatty acid ester, POE sorbitan fatty acid ester, POE sorbit fatty acid ester, POE glycerin fatty acid ester, POE glycol fatty acid ester POE alkyl ether phosphoric acid and its salt, POE alkyl ether sulfate, POE phytosterol and phytostanol, POE alkyl phenyl ether phosphoric acid and its salt, POE lanolin and lanolin alcohol, POE alkylamine and fatty acid amide, POE alkylphenyl formaldehyde condensation Products, POE polyoxypropylene alkyl ether, POE alkyl phenyl ether and fatty acid ethanolamide, Nonionic surfactants such as reethylene glycol fatty acid esters, octyl sulfate, decyl sulfate, lauryl sulfate, myristyl sulfate, palmityl sulfate, stearyl sulfate and alkali metal salts thereof (alkali metal salts such as sodium, potassium, lithium, etc.) Alkyl sulfate ester or salt thereof, acyl sarcosine sodium such as sodium N-lauroyl sarcosine, sodium N-myristoyl sarcosine, sodium dodecylbenzenesulfonate, hydrogenated coconut fatty acid sodium monoglyceride monosulfate, sodium lauryl sulfoacetate, sodium N-palmitoyl glutamate, etc. N-acyl glutamate, N-methyl-N-acyl taurine sodium, N-methyl-N-acylalanine sodium, α-olefin sulfonic acid Examples include anionic surfactants such as sodium and sodium dioctylsulfosuccinate, cationic surfactants such as alkylammonium and alkylbenzylammonium salts, and amphoteric surfactants such as betaine acetate, imidazolinium betaine, and fatty acid amidopropyl betaine. . The amount of these surfactants is usually 0 to 5%. In particular, nonionic surfactants other than the component (C) may not be added, and may be 0%.
The blending amount of the surfactant as the optional component described above is preferably in a range where the total blending amount with the surfactant of the component (C) is 0.5 to 6%.

  Examples of sweetening agents include saccharin sodium, stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidyl dihydrochalcone, perilartin, thaumatin, sucralose, acesulfame potassium, aspartame and the like.

  Examples of the preservative include parabens (paraoxybenzoic acid ester) such as methyl paraben, butyl paraben, and ethyl paraben, benzoic acid and its salt, salicylic acid and its ester or salt, and the like.

  As the active ingredient, the above components (A), (B), (D), (E), (F), dextranase, other than the fluoride ion source, for example, ascorbic acid and its derivatives, riboflavin, Vitamins such as pyridoxine hydrochloride, cyanocobalamin, β-carotene, ergocalciferol, menadione, ubiquinone, plant extracts such as lauren, ugone, hamamelis, clove, chamomile, latania, myrrh, cypress, rosemary, safflower, mutanase, lysozyme , Enzymes such as amylase, protease, lytic enzyme, superoxide dismutase, salts such as sodium chloride, potassium nitrate, sodium polyphosphate, carbonate, bicarbonate, sesquicarbonate, γ-oryzanol, dihydrocholesterol, α-bisabolol, azulene , Methoxye Lene / maleic anhydride copolymer, trichlorocarbanilide, alanine, glycine, proline, L-arginine, sodium L-aspartate, trimethylglycine, copper chlorophyllin sodium, copper gluconate, zinc chloride, zinc citrate, zeolite, One or more water-soluble inorganic phosphate compounds, aluminum lactate, and the like may be blended. The amount of the active ingredient added can be an effective amount as long as the effects of the present invention are not hindered.

  Examples of pH adjusters include citric acid, malic acid, lactic acid, tartaric acid, succinic acid, acetic acid, phosphoric acid, pyrophosphoric acid, glycerophosphoric acid, various salts such as potassium salt, sodium salt and ammonium salt, sodium hydroxide, hydrochloric acid Etc. These can be blended alone or in combination of two or more so that the pH of the composition is in the range of 5-9 (the blending amount is usually 0-2%).

  As colorants, Red No. 2, Red No. 3, Red No. 225, Red No. 226, Yellow No. 4, Yellow No. 5, Yellow No. 205, Blue No. 1, Blue No. 2, Blue No. 201, Blue No. 204, Green No. 3 and other legal dyes, safflower dyes, gardenia dyes, cochineal dyes, anato dyes, bengara, mica titanium, titanium oxide and the like.

  Perfumes include peppermint oil, spearmint oil, anise oil, eucalyptus oil, winter green oil, cassia oil, clove oil, thyme oil, sage oil, lemon oil, orange oil, peppermint oil, cardamom oil, coriander oil, mandarin oil, Lime oil, lavender oil, rosemary oil, laurel oil, camomil oil, caraway oil, marjoram oil, bay oil, lemongrass oil, origanum oil, pine needle oil, neroli oil, rose oil, jasmine oil, iris concrete, absolute Natural fragrances such as peppermint, absolute rose, orange flower, and processed natural fragrances such as front reservoir cut, rear reservoir cut, fractional distillation, liquid-liquid extraction, essence, powder fragrance, and the like, and Menthol, carvone, anethole, cineol, salicylic acid Til, cinnamic aldehyde, eugenol, 3-l-mentoxypropane-1,2-diol, linalool, linalyl acetate, limonene, menthone, menthyl acetate, N-substituted-paramentane-3-carboxamide, pinene, octylaldehyde, Citral, pulegone, carbyl acetate, anisaldehyde, ethyl acetate, ethyl butyrate, allylcyclohexane propionate, methyl anthranilate, ethyl methyl phenyl glycidate, vanillin, undecalactone, hexanal, ethyl alcohol, propyl alcohol, butanol , Isoamyl alcohol, hexenol, dimethyl sulfide, cycloten, furfural, trimethyl pyrazine, ethyl lactate, ethyl thioacetate, etc. Known flavors used in oral compositions such as single-flavored flavors, and other flavors such as strawberry flavor, apple flavor, banana flavor, pineapple flavor, grape flavor, mango flavor, butter flavor, milk flavor, fruit mix flavor, and tropical fruit flavor. Perfume materials can be used and is not limited to the perfume of the examples. Moreover, although a compounding quantity is not specifically limited, It is preferable to use said fragrance | flavor raw material 0.000001 to 1% in a formulation composition. Moreover, as a fragrance | flavor for fragrance | flavor using the said fragrance | flavor raw material, it is preferable to use 0.1 to 2.0% in a formulation composition.

  The composition for oral cavity of the present invention is applied to containers such as aluminum laminated tubes, glass-deposited plastic tubes, dispenser containers by mechanical or differential pressure, bottle containers such as polyethylene terephthalate and glass, and film packaging containers such as pillow packaging. Can be filled.

  EXAMPLES Hereinafter, although this invention is demonstrated concretely using an Example, a comparative example, and a formulation example, this invention is not restrict | limited to the following Example. In the following examples, the blending amount is mass%. In addition to the materials shown in Table 1, materials that conform to cosmetic raw material standards or quasi-drug raw material standards were used. In addition, the composition of a fragrance | flavor is as showing to Tables 9-15. Ethylene oxide was abbreviated as EO, and polyoxyethylene was abbreviated as POE.

[Examples and Comparative Examples]
The composition which mix | blended (A)-(C) component, (D) or (E) component, and also (F) component with the kind and compounding quantity as shown in Table 3-8 by the common composition shown in following Table 2. The dentifrice composition was degassed and mixed using a kneader and prepared by a conventional method. The amount of the dentifrice composition charged was 5 kg. The obtained dentifrice composition was filled in a tube A made of the material described later and evaluated by the following method. The results are shown in Tables 3-8.

Tube A (Dai Nippon Printing Co., Ltd.):
From the outermost layer, LDPE55 / PET12 / LDPE20 / white LDPE60 / EMAA20 / AL10 / EMAA30 / LDPE20 / LLDPE30 (thickness 257 μm, diameter 26 mm, filling amount 50 g)
A numerical value shows thickness (micrometer). The abbreviations are as follows.
LDPE: Low density polyethylene White LDPE: White low density polyethylene LLDPE: Linear low density polyethylene AL: Aluminum PET: Polyethylene terephthalate EMAA: Copolymer resin of ethylene / methacrylic acid

Evaluation of Periodontal Disease Inhibitory Effect A beagle dog (4 years old, female, 4 each group) was used for evaluation with bad breath and GCF amount as indicators. After the evaluation of halitosis and measurement of the amount of GCF before the start of the test, administration was performed twice a day for 1 month to evaluate halitosis and the amount of GCF. Administration of the test preparation was carried out by brushing the entire oral cavity of a beagle dog by taking 0.5 g of the test preparation in the case of a dentifrice and 0.5 mL in the case of a mouthwash. Details of the evaluation method are shown below.

Evaluation of halitosis from periodontal disease:
Five perfumers evaluated the bad breath at the start of the test according to the criteria described later, and the score was S1. After administering the test preparation for 1 month, five perfumers similarly evaluated the level of bad breath derived from periodontal disease according to the criteria described later, and the score was S2. The degree of improvement in bad breath derived from periodontal disease in each beagle dog was calculated according to the following formula, and the average value of 4 beagle dogs was determined.

Improvement degree of bad breath derived from periodontal disease = S1-S2
This average value was determined according to the criteria described below. It was judged that an oral composition having a degree of improvement in bad breath derived from periodontal disease was ◎ or ◯ was an oral composition having an effect of preventing or improving periodontal disease.

<Evaluation criteria for bad breath>
5: Extremely bad breath derived from periodontal disease 4: Strong bad breath derived from periodontal disease 3: Slightly bad breath derived from periodontal disease 2: Slightly bad breath derived from periodontal disease 1: Periodontal Almost no bad breath derived from disease 0: No bad breath derived from periodontal disease <Criteria for bad breath>
Improvement degree of bad breath derived from periodontal disease ◎: 3 or more and 5 or less ○: 2 or more and less than 3

Evaluation of periodontal disease prevention effect using gingival crevicular fluid (GCF) as an index:
Using 4 mandibular sites (P3, P4, M1 mesial, M2 centrifuge) in beagle dogs as test sites, the amount of GCF was measured before and after the start of the test. GCF was collected after evaluating bad breath. The amount of GCF was collected by inserting GCF collection strips (Periopaper (registered trademark), Yoshida Co., Ltd.) into the periodontal pocket selected at the start of the test for 30 seconds, and a GCF meter (Periotron (registered trademark)). , Yoshida Co., Ltd.). GCF change rate is calculated according to the following formula, the average value of 4 test sites of 4 beagle dogs is determined according to the criteria described later, periodontal disease with ◎, ○ oral composition as index of gingival crevicular fluid Judged to have a preventive effect.

GCF change rate (%) =
((GCF amount at start of test−GCF amount at end of test) / GCF amount at start of test) × 100

<Score of periodontal disease prevention effect>
GCF change rate ◎: 70% or more ○: 40% or more and less than 70% △: 20% or more and less than 40% ×: less than 20%

Evaluation of storage stability of ascorbic acid phosphate or its salt over time:
The test sample was stored for 1 month in a thermostatic bath at 50 ° C. Thereafter, the sample was allowed to stand at room temperature and then used for evaluating the storage stability of ascorbic acid phosphate ester or a salt thereof. The residual rate was calculated from the initial value on the day of manufacture. All reagents were manufactured by Kanto Chemical.

<Quantitative method>
When the test preparation is a dentifrice, 0.1 g is measured and 10 mmol / L phosphate buffer (1.5 mmol / L potassium dihydrogen phosphate, 23.5 mmol / L dipotassium hydrogen phosphate, pH 8.0) Ascorbic acid phosphate ester or a salt thereof is extracted, and high performance liquid chromatography (pump: JASCO PU1580, autosampler: Shimadzu SIL-10A, UV detector: Shimadzu SPD-6A, recording device: Shimadzu Using a factory C-R4A, a column thermostat: JASCO CO-966), the quantitative analysis was performed by the absolute calibration curve method. The mobile phase is a 25 mmol / L potassium dihydrogen phosphate + 5 mmol / L tetrabutylammonium / acetonitrile = 91/9 mixture (volume ratio), the column is a stainless steel tube having a diameter of about 4.6 mm and a length of about 150 mm, and a 5 μm liquid chromatograph. For example, TSK-gel ODS-80Ts (manufactured by Tosoh Corporation), column temperature of about 40 ° C., detection wavelength of 240 nm, and flow rate of 0.8 mL / min. In addition, in the case of a mouthwash, it diluted using the 10 mmol / L phosphate buffer, and measured on the same conditions. This result was determined according to the criteria described below, and it was determined that the oral composition of “◎” and “○” had secured the storage stability of the ascorbic acid phosphate ester salt.

Residual rate of ascorbic acid phosphate or salt thereof (%) =
(Evaluation sample value (%) / initial value (%)) × 100

<Score>
For the stability evaluation of ascorbic acid phosphate ester or a salt thereof, an average value of three repetitions was judged according to the following criteria.
Residual rate of ascorbic acid phosphate or salt thereof ◎: 95% or more ○: less than 95% △: less than 90% ×: less than 80%

Evaluation of storage stability of vitamin E or its derivatives over time:
The test sample was stored for 1 month in a thermostatic bath at 50 ° C. After leaving this to stand at room temperature, if the test preparation is a dentifrice or an oral pasta, 10 g is taken and extracted with methanol, followed by liquid chromatography (pump: JASCO PU-980, autosampler: JASCO) AS-950, detector: JASCO UV-970, recording device: system instrument Chromatocoder 21J, column thermostat: JASCO CO-966). The measurement conditions were as follows: a stainless steel tube with an inner diameter of 4.6 mm and a length of 15 cm was filled with a 5 μm octadecylsilylated silica gel for liquid chromatography, methanol was used as the mobile phase, the column temperature was 25 ° C., and 1.0 mL / min. Was measured by an absolute calibration curve method with an ultraviolet absorptiometry (measurement wavelength: 284 nm). In addition, in the case of a mouthwash, it diluted with methanol and measured on the same conditions. This result was determined according to the criteria described below, and it was determined that the storage stability of the vitamin E derivative was ensured for the oral compositions of A and B.

Residual rate of vitamin E or its derivative (%) =
(Evaluation sample value (%) / initial value (%)) × 100

<Score>
For the stability evaluation of vitamin E or its derivatives, the average value of three repetitions was judged according to the following criteria.
Residual rate of vitamin E or its derivative ◎: 95% or more ○: 90% or more and less than 95% △: 80% or more and less than 90% ×: less than 80%

Evaluation of sterilizing power:
40 μL of the Porphyromonas gingivalis culture solution that was cryopreserved was Todd Hewitt broth (Becton and Dickinson) containing 5 mg / L hemin (manufactured by Sigma) and 1 mg / L vitamin K (manufactured by Wako Pure Chemical Industries, Ltd.). Added to 4 mL culture solution (THBHM) and anaerobic culture at 37 ° C. overnight (80 vol% nitrogen, 10 vol% carbon dioxide, 10 vol% hydrogen), and then adjusted to turbidity at a wavelength of 660 nm (OD660) = 1. The fungus solution was used.
When the test preparation was a dentifrice, 40 mL of artificial saliva was added to 10 g of the composition and stirred, followed by centrifugation (10,000 rotations / minute, 10 minutes), and the resulting supernatant was used as a sample stock solution. When the test preparation was a mouthwash, 40 mL of artificial saliva was added to 10 g of the composition and diluted to obtain a sample stock solution. After 2 mL of the sample stock solution was allowed to act on 2 mL of the bacterial solution for 30 seconds, 50 μL was collected to obtain a sample solution for bactericidal evaluation. Bactericidal power evaluation is performed by adding a bactericidal power evaluation sample solution (50 μL) to a THB liquid medium (4 mL) and culturing (37 ° C., 8 hours), and then measuring the amount of grown bacteria using turbidity (OD660) as an index. Evaluations were made on the assumption that a smaller number gave a higher bactericidal activity.

  As artificial saliva, 3.73 g of potassium chloride, 0.14 g of potassium dihydrogen phosphate, 0.15 g of calcium chloride dihydrate, and 0.02 g of magnesium chloride hexahydrate were purified. Dissolved in water and adjusted to pH 7 with potassium hydroxide to a volume of 1,000 mL was used.

<Judgment criteria for sterilizing power>
◎: OD660 is less than 1 ○: OD660 is 1 or more and less than 1.2 Δ: OD660 is 1.2 or more and less than 2 ×: OD660 is 2 or more

Evaluation of appearance stability (separation, discoloration) over time:
The test sample was stored for 1 month in a thermostatic bath at 50 ° C. Then, after leaving the sample to room temperature, it was used for evaluation of appearance stability. When the test sample was a toothpaste, the sample was extruded about 10 cm onto a straw half paper, and the presence or absence of separation and discoloration was observed and evaluated. When the test sample was a mouthwash, the container was allowed to stand for 1 day, and then the presence or absence of separation and discoloration was observed and evaluated. In addition, discoloration was evaluated on the basis of the thing which preserve | saved the test sample in the 5 degreeC thermostat. The evaluation criteria are as follows.

<Separation score>
A: Separation is not recognized at all. O: Separation is hardly observed. Δ: Separation is slightly observed. X: Remarkable separation is observed <Discoloration rating>
◎: No discoloration is observed at all. ○: Almost no discoloration is observed. △: Discoloration is slightly recognized. ×: Significant discoloration is observed.

  From the results of Tables 3 and 4, the composition for oral cavity of the present invention is effective in suppressing bad breath derived from periodontal disease, periodontal disease preventive effect using GCF as an index, bactericidal activity, ascorbic acid phosphate ester or salt thereof And Vitamin E or its derivatives have excellent storage stability over time and appearance stability (no separation, no discoloration), high periodontal disease prevention or improvement effect, and excellent storage stability over time It has been found. On the other hand, either (A), (B), or (D) component is missing, the total amount of these components, or the ratio of (C) / ((B) + (D)) is inappropriate In such a case, or when the chain length of the alkyl group of the surfactant or the number of moles of EO added is inappropriate, it is inferior to any of the above effects, and the effect of the present invention cannot be achieved. Comparative Example 12 is a reproduction of Example 23 of Japanese Patent Application Laid-Open No. 2005-187333, but the effect of the present invention could not be achieved. Similar results were obtained even when the fragrances B to I were used instead of the fragrance A.

  From the results of Tables 5 and 6, the composition for oral cavity of the present invention is effective in preventing bad breath derived from periodontal disease, periodontal disease preventive effect using GCF as an index, bactericidal activity, ascorbic acid phosphate ester or salt thereof And Vitamin E or its derivatives have excellent storage stability over time and appearance stability (no separation, no discoloration), high periodontal disease prevention or improvement effect, and excellent storage stability over time It has been found. On the other hand, either (A), (B), or (E) is missing, the total amount of these components, or the ratio of (C) / ((B) + (E)) is inappropriate In such a case, or when the chain length of the alkyl group of the surfactant or the average number of moles of EO added is inadequate, one of the above effects is inferior, and the effect of the present invention cannot be achieved. Comparative Example 25 is a reproduction of Example 9 of Japanese Patent Application Laid-Open No. 2005-247786, but the effect of the present invention could not be achieved. Similar results were obtained even when the fragrances B to I were used instead of the fragrance A.

  From the results of Tables 7 and 8, the composition for oral cavity of the present invention is a periodontal disease using GCF as an index by further blending glycyrrhetinic acid, ε-aminocaproic acid, glycyrrhizic acid salt, tranexamic acid, buckwheat extract or allantoins. It was found that the prevention / improvement effect is improved. Similar results were obtained even when the fragrances B to I were used instead of the fragrance A.

Below, the formulation example using this invention is shown.
When oral compositions having the following compositions were prepared and evaluated in the same manner as described above, all oral compositions were effective in preventing bad breath derived from periodontal diseases, periodontal disease preventing effects using GCF as an index, ascorbine It was excellent in storage stability of acid phosphate ester or a salt thereof, storage stability of vitamin E or a derivative thereof, bactericidal activity, and appearance stability (no separation, no discoloration). Further, the dextranase-containing composition was excellent in plaque removal effect, and the fluoride ion source-containing composition was excellent in preventing or improving root caries.

[Prescription Example 1] Toothpaste (A) L-ascorbyl magnesium phosphate 0.3%
(B) dl-α-tocopherol acetate 0.1
(C) POE stearyl ether 1
(EO average added mole number 5)
(C) POE hydrogenated castor oil 1
(EO average added mole number 20)
(D) Isopropylmethylphenol 0.05
β-glycyrrhetinic acid 0.05
Dextranase (13,000 units / g) 0.16
Sodium fluoride 0.21
Sodium lauryl sulfate 1.5
Precipitated silica 15
Thickening silica 4
Xanthan gum 0.5
Carrageenan 0.5
Sodium polyacrylate 0.2
70% sorbit solution 45
Propylene glycol 3
Sodium hydroxide 0.4
Saccharin sodium 0.15
Titanium oxide 0.5
Fragrance A 1
Blue No. 1 0.0001
Purified water balance
Total 100.00%
A + B + D = 0.45%
C / (B + D) = 13.3

[Prescription Example 2] Toothpaste (A) L-ascorbyl magnesium phosphate 0.3%
(B) dl-α-tocopherol acetate 0.1
(C) POE stearyl ether 1
(EO average added mole number 5)
(C) POE hydrogenated castor oil 1
(EO average added mole number 20)
(D) Isopropylmethylphenol 0.05
β-glycyrrhetinic acid 0.05
Dextranase (13,000 units / g) 0.16
Sodium monofluorophosphate 0.73
Sodium lauryl sulfate 1.5
Precipitated silica 15
Thickening silica 4
Xanthan gum 0.5
Carrageenan 0.5
Sodium polyacrylate 0.2
70% sorbit solution 45
Propylene glycol 3
Sodium hydroxide 0.4
Saccharin sodium 0.15
Titanium oxide 0.5
Fragrance A 1
Blue No. 1 0.0001
Purified water balance
Total 100.00%
A + B + D = 0.45%
C / (B + D) = 13.3

[Prescription Example 3] Toothpaste (A) L-ascorbyl magnesium phosphate 0.3%
(B) dl-α-tocopherol acetate 0.1
(C) POE stearyl ether 1
(EO average added mole number 5)
(C) POE hydrogenated castor oil 1
(EO average added mole number 20)
(E) Cetylpyridinium chloride 0.01
β-glycyrrhetinic acid 0.05
Dextranase (13,000 units / g) 0.16
Sodium fluoride 0.21
Sodium lauryl sulfate 1.5
Precipitated silica 15
Thickening silica 4
Xanthan gum 0.5
Carrageenan 0.5
Sodium polyacrylate 0.2
70% sorbit solution 45
Propylene glycol 3
Sodium hydroxide 0.4
Saccharin sodium 0.15
Titanium oxide 0.5
Fragrance A 1
Blue No. 1 0.0001
Purified water balance
Total 100.00%
A + B + E = 0.41%
C / (B + E) = 12.7

[Prescription Example 4] Toothpaste (A) L-ascorbyl magnesium phosphate 0.3%
(B) dl-α-tocopherol acetate 0.1
(C) POE stearyl ether 1
(EO average added mole number 5)
(C) POE hydrogenated castor oil 1
(EO average added mole number 20)
(E) Cetylpyridinium chloride 0.01
β-glycyrrhetinic acid 0.05
Dextranase (13,000 units / g) 0.16
Sodium monofluorophosphate 0.73
Sodium lauryl sulfate 1.5
Precipitated silica 15
Thickening silica 4
Xanthan gum 0.5
Carrageenan 0.5
Sodium polyacrylate 0.2
70% sorbit solution 45
Propylene glycol 3
Sodium hydroxide 0.4
Saccharin sodium 0.15
Titanium oxide 0.5
Fragrance A 1
Blue No. 1 0.0001
Purified water balance
Total 100.00%
A + B + E = 0.41%
C / (B + E) = 12.7

[Prescription Example 5] Toothpaste (A) L-ascorbyl magnesium phosphate 0.5%
(B) dl-α-tocopherol acetate 0.1
(C) Decylglucoside 1
(C) Lauryl glucoside 1
(E) Cetylpyridinium chloride 0.05
Sodium monofluorophosphate 0.7
Sodium lauryl sulfate 1.5
Dentifrice Calcium Hydrogen Phosphate 40
Thickening silica 4
Xanthan gum 0.5
Carrageenan 0.5
Sodium polyacrylate 0.2
70% sorbite solution 20
Paratinit 2
Propylene glycol 3
Sodium hydroxide 0.4
Saccharin sodium 0.15
Titanium oxide 0.5
Fragrance A 1
Purified water balance
Total 100.00%
A + B + E = 0.65%
C / (B + E) = 13.3

[Prescription Example 6] Toothpaste (A) L-ascorbyl magnesium phosphate 0.5%
(B) dl-α-tocopherol acetate 0.1
(C) Decylglucoside 1
(C) Lauryl glucoside 1
(E) Cetylpyridinium chloride 0.05
Sodium fluoride 0.21
Sodium lauryl sulfate 1.5
Dentifrice Calcium Hydrogen Phosphate 40
Thickening silica 4
Xanthan gum 0.5
Carrageenan 0.5
Sodium polyacrylate 0.2
70% sorbite solution 20
Paratinit 2
Propylene glycol 3
Sodium hydroxide 0.4
Saccharin sodium 0.15
Titanium oxide 0.5
Fragrance A 1
Purified water balance
Total 100.00%
A + B + E = 0.65%
C / (B + E) = 13.3

[Prescription Example 7] Toothpaste (A) L-ascorbyl magnesium phosphate 0.5%
(B) dl-α-tocopherol acetate 0.1
(C) Polyoxyethylene hydrogenated castor oil 2
(EO average added mole number 20)
(E) Benzethonium chloride 0.05
β-glycyrrhetinic acid 0.05
Sodium monofluorophosphate 0.7
Sodium lauryl sulfate 1.5
Calcium carbonate 40
Thickening silica 4
Xanthan gum 0.5
Carrageenan 0.5
Sodium polyacrylate 0.2
70% sorbite solution 20
Erythritol 2
Propylene glycol 3
Sodium hydroxide 0.4
Saccharin sodium 0.15
Titanium oxide 0.5
Fragrance A 1
Purified water balance
Total 100.00%
A + B + E = 0.65%
C / (B + E) = 13.3

[Prescription Example 8] Mouthwash (A) L-ascorbyl magnesium phosphate 0.5%
(B) Nicotinic acid dl-α-tocopherol 0.1
(C) Lauryl glucoside 1
(E) Cetylpyridinium chloride 0.01
β-glycyrrhetinic acid 0.2
Dextranase (13,000 units / g) 0.2
Sodium lauryl sulfate 0.5
Ethanol 10
Glycerin 10
Sodium hydroxide 0.4
Saccharin sodium 0.01
Fragrance A 0.5
Purified water balance
Total 100.00%
A + B + E = 0.61%
C / (B + E) = 9.1

[Prescription Example 9] Mouthwash (A) L-ascorbyl magnesium phosphate 0.5%
(B) Nicotinic acid dl-α-tocopherol 0.1
(C) Polyoxyethylene hydrogenated castor oil 1
(EO average added mole number 60)
(E) Cetylpyridinium chloride 0.01
β-glycyrrhetinic acid 0.2
Dextranase (13,000 units / g) 0.2
Sodium lauryl sulfate 0.5
Ethanol 10
Glycerin 10
Sodium hydroxide 0.4
Saccharin sodium 0.01
Fragrance A 0.5
Purified water balance
Total 100.00%
A + B + E = 0.61%
C / (B + E) = 9.1

Claims (6)

(A) Ascorbic acid phosphate or a salt thereof,
(B) Vitamin E or a derivative thereof,
(C) Polyoxyethylene hydrogenated castor oil having an average addition mole number of ethylene oxide of 10 to 60 moles, polyoxyethylene alkyl having an alkyl group of 14 to 18 carbon atoms and an average addition mole number of ethylene oxide of 5 to 8 moles One or more surfactants selected from ethers and alkyl glucosides having 10 to 14 carbon atoms in the alkyl group,
(D) contains a nonionic fungicide, the total content of components (A), (B) and (D) is 0.2 to 1.5% by mass, and (C) / ((B) + (D)) is 8-20 by mass ratio, The composition for oral cavity characterized by the above-mentioned.   (D) The composition for oral cavity according to claim 1, wherein the nonionic fungicide is isopropylmethylphenol or triclosan. (A) Ascorbic acid phosphate or a salt thereof,
(B) Vitamin E or a derivative thereof,
(C) Polyoxyethylene hydrogenated castor oil having an average addition mole number of ethylene oxide of 10 to 60 moles, polyoxyethylene alkyl having an alkyl group of 14 to 18 carbon atoms and an average addition mole number of ethylene oxide of 5 to 8 moles One or more surfactants selected from ethers and alkyl glucosides having 10 to 14 carbon atoms in the alkyl group,
(E) contains a cationic fungicide, the total content of components (A), (B) and (E) is 0.2 to 1.3% by mass, and (C) / ((B) + (E)) is 8-18 by mass ratio, The composition for oral cavity characterized by the above-mentioned.   (E) The composition for oral cavity according to claim 3, wherein the cationic fungicide is at least one selected from cetylpyridinium chloride, benzethonium chloride, benzalkonium chloride, chlorhexidine gluconate, and chlorhexidine hydrochloride.   The total content of the component (A), the component (B), and the component (D) or (E) is 0.2 to 1.0% by mass, and (C) / [(B) + (( The composition for oral cavity according to any one of claims 1 to 4, wherein D) or (E))] is 8 to 15 in terms of mass ratio.   Furthermore, (F) 1 or more types chosen from glycyrrhetinic acid, (epsilon) -aminocaproic acid, a glycyrrhizinate, tranexamic acid, a buckwheat extract, and allantoins are contained, The any one of Claims 1 thru | or 5 characterized by the above-mentioned. Oral composition.