JP2017214297A - Oral composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide an oral composition which is excellent in oral cavity absorption of a water soluble active ingredient, and in which tocopherol or a derivative thereof is stably formulated after storage, and which is effective for preventing or suppressing periodontal disease with good use feeling.SOLUTION: An oral composition contains: (A) at least one water soluble active ingredient; (B) 0.05 to 1 mass% of at least one selected from fatty acids and esters having a branched chain structure of carbon number 8-22; (C) tocopherol and/or a derivative thereof; (D) at least one selected from an alkali metal salt of an inorganic acid and/or an organic acid; and (E) polyoxyethylene alkyl ether; wherein the total amount of the components (D) and (E) is 2 mass% or more, and the mass ratio of (D)/(B) is 5 or more, and the mass ratio of (E)/(B) is 5 or less.SELECTED DRAWING: None

Description

  The present invention relates to an oral composition that is excellent in oral absorption of a water-soluble active ingredient and tocopherol or a derivative thereof is stabilized and blended even after storage, and is effective in preventing or suppressing periodontal disease.

  Water-soluble active ingredients such as allantoin and tranexamic acid are known as active ingredients for oral preparations, and are applied to the prevention or suppression of periodontal diseases. However, it differs from the skin in that the oral cavity is always supplied with saliva and wet, and oral preparations are often rinsed with water after application in the oral cavity. It is in an environment where it is difficult to retain and absorb water-soluble components. For this reason, the absorption improvement effect to the gum surface and the inside of a water-soluble active ingredient was not fully acquired.

  Therefore, the applicant, when blending the water-soluble active ingredient in the oral composition, by blending a fatty acid having a branched chain structure, a fatty acid ester having a linear or branched chain structure, a polyglycerin fatty acid ester, Patent Document 1 (Japanese Patent Laid-Open No. 2015-205826) proposed a technique for increasing the absorbability of an active ingredient into gums.

On the other hand, tocopherol or a derivative thereof is an active ingredient that promotes the circulation of toothpaste and has a preventive effect on gingivitis, and is incorporated in a dentifrice preparation for preventing periodontal disease, etc. Therefore, it becomes a problem to mix stably in a dentifrice preparation.
In response to these problems, polyoxyethylene hydrogenated castor oil having an average addition mole number of ethylene oxide of 3 to 8, a polyoxyethylene alkyl ether having an alkyl group of 16 to 18 carbon atoms, and an average addition mole number of ethylene oxide of 10 to 80 Can be prepared as a mixture of surfactants in a specific ratio to prepare a dentifrice composition with excellent stability of vitamin E or a derivative thereof, good foaming, and excellent formulation stability during storage at medium and high temperatures. Is disclosed in Patent Document 2 (Japanese Patent No. 4964429).

Japanese Patent Laying-Open No. 2015-205826 Japanese Patent No. 4496429

  However, a water-soluble active ingredient and a poorly water-soluble tocopherol or derivative thereof are blended in the oral composition at the same time, and the tocopherol or derivative thereof is stable over time while sufficiently maintaining the oral absorption of the water-soluble active ingredient. It was technically difficult to compound.

  The present invention has been made in view of the above circumstances, and is excellent in oral absorption of a water-soluble active ingredient and tocopherol or a derivative thereof is stabilized and blended even after storage, and is effective for prevention or suppression of periodontal disease. An object is to provide a composition.

  As a result of intensive studies, the present inventors have found that (A) a water-soluble active ingredient and (C) a tocopherol or a derivative thereof are mixed with an oral composition, (B) a specific fatty acid or ester, and (D) an inorganic substance. It discovered that the said objective was achieved by mix | blending appropriately the alkali metal salt of an acid and / or organic acid, and (E) polyoxyethylene alkyl ether. That is, according to the present invention, 0.05 to 1 mass of (A) at least one water-soluble active ingredient, (B) at least one selected from fatty acids and esters having a branched chain structure having 8 to 22 carbon atoms. %, (C) tocopherol and / or a derivative thereof, (D) at least one selected from an inorganic acid and / or an alkali metal salt of an organic acid, and (E) a polyoxyethylene alkyl ether, (D) and The total amount of the component (E) is 2% by mass or more, (D) / (B) is 5 or more as a mass ratio, and (E) / (B) is 5 or less as a mass ratio. The oral absorption of the active ingredient is excellent and tocopherol or its derivative is stabilized and blended even after storage, and an oral composition with a reduced oily odor and good usability can be obtained to prevent periodontal disease or Used effectively for suppression Heading the Rukoto, it has led to the completion of the present invention.

The present inventors have studied to combine tocopherol or a derivative thereof with a water-soluble active ingredient with the aim of further improving the prevention or suppression effect of periodontal disease, and promote the oral absorption of the water-soluble active ingredient. Therefore, when a fatty acid or ester having a branched chain structure is used in combination and tocopherol or a derivative thereof is blended, the oily odor is significantly enhanced and used by the combined use of the fatty acid or ester, tocopherol or a derivative thereof, which is an oil component. It was found that the feeling worsened. Furthermore, when the formulation of a nonionic surfactant, particularly polyoxyethylene alkyl ether, was investigated for the stabilization of tocopherol or its derivative, the effect of stabilizing the tocopherol or its derivative was sufficiently due to the influence of the fatty acid or ester. It has not been demonstrated, and it has been found that the prior art has insufficient stability. In addition, if a nonionic surfactant, especially polyoxyethylene alkyl ether, is blended inappropriately, even if the fatty acid or ester is blended, absorption in the oral cavity of the water-soluble active ingredient is inhibited, resulting in poor absorption. There was found. Therefore, as a result of further investigation to solve these problems, when the components (B), (D), and (E) are combined with the components (A) and (C), the components (D) and (E) When the total amount is equal to or greater than the specific value, the mass ratio of (D) / (B) is equal to or greater than the specific value, and the mass ratio of (E) / (B) is equal to or less than the specific value, the combination of the components (D) and (E) Specifically, without causing problems related to the oily odor, stability of water-soluble active ingredients and absorbability, (A) high oral absorption rate of component (A) and excellent storage stability of component (C) Are compatible and exhibit the above-mentioned special effects.
According to this invention, the further improvement of the prevention or suppression effect of a periodontal disease can also be anticipated by improving the absorption rate of (A) component and the stability of (C) component.

  From Patent Documents 1 and 2, which are not supposed and are not mentioned about simultaneous blending of a water-soluble active ingredient and tocopherol or a derivative thereof, (A), (B), (C), (D), (E) By combining the components, the improvement in the absorbability of the component (A) and the stability of the component (D) cannot be predicted.

Accordingly, the present invention provides the following oral composition.
(A) at least one water-soluble active ingredient,
(B) 0.05 to 1% by mass of at least one selected from fatty acids and esters having a branched chain structure having 8 to 22 carbon atoms,
(C) Tocopherol and / or its derivative,
(D) containing at least one selected from alkali metal salts of inorganic acids and / or organic acids, and (E) polyoxyethylene alkyl ether,
The total amount of components (D) and (E) is 2% by mass or more, (D) / (B) is 5 or more as a mass ratio, and (E) / (B) is 5 or less as a mass ratio. An oral composition characterized by the above.

  According to the present invention, the oral absorption of the water-soluble active ingredient is excellent and the tocopherol or a derivative thereof is stabilized and blended, the oily odor is suppressed and the feeling of use is good, and periodontal disease is prevented or suppressed. An effective oral composition can be provided.

The present invention will be described in further detail below. The composition for oral cavity of the present invention is
(A) a water-soluble active ingredient,
(B) one or more selected from fatty acids and esters having a branched chain structure having 8 to 22 carbon atoms,
(C) Tocopherol and / or its derivative,
(D) one or more selected from alkali metal salts of inorganic acids and / or organic acids,
And (E) a polyoxyethylene alkyl ether.

  The water-soluble active ingredient (A) is a medicinal ingredient having a preventive or inhibitory action on periodontal disease. Specifically, allantoin such as tranexamic acid, allantoin, allantoinchlorohydroxyaluminum, allantoindihydroxyaluminum or derivatives thereof, ε-aminocaproic acid, sodium azulene sulfonate, glycyrrhizinate, ascorbate, pyridoxine hydrochloride, abouc extract, etc. These may be used alone or in combination of two or more. Among them, those having an amino group in the structure are preferable from the viewpoint of interaction with the component (B), more preferably tranexamic acid, allantoin or a derivative thereof, and ε-aminocaproic acid, and further preferably tranexam. It is an acid.

  The blending amount of the water-soluble active ingredient (A) is preferably 0.001 to 0.5% (mass%, the same applies hereinafter) of the whole composition. The higher the compounding amount, the higher the medicinal effect, and if it is 0.001% or more, sufficient medicinal effect can be imparted, but 0.5% or less is suitable for suppressing adverse effects on formulation stability such as discoloration. It is.

  The component (B) is an oral absorption enhancer of the component (A), and (B-1) a fatty acid having a branched chain structure having 8 to 22 carbon atoms and / or (B-2) having 8 to 22 carbon atoms. Esters having a branched chain structure can be used. These may be used alone or in combination of two or more. Moreover, even if it is (B-1) component or (B-2) component, (B-1) component and (B-2) component may be sufficient.

The (B-1) component fatty acid has a branched chain structure having 8 to 22 carbon atoms, and the preferred carbon number is 12 to 20 from the viewpoint of skin affinity.
Specific examples include isodecanoic acid, isotridecanoic acid, isomyristic acid, isopalmitic acid, and isostearic acid. Of these, isostearic acid is preferred.

The (B-2) component ester has a branched chain structure having 8 to 22 carbon atoms, and the preferred carbon number is 12 to 20 from the viewpoint of skin affinity. In particular, those having a branched chain structure are preferred, and acylamino acid esters and / or fatty acid esters in which either an acid residue or an alcohol residue has a branched chain structure are preferred, and fatty acid esters are more preferred. In this case, the branched chain structure may be an acid residue or an alcohol residue, or may be both.
As the type of ester, a sterol ester having a sterol skeleton is particularly preferable, among which phytosterol ester and cholesterol ester are preferable, and phytosterol ester is most preferable.
Specifically, N-acylamino acid sterol esters such as N-lauroyl-L-glutamate di (cholesteryl / octyldodecyl) N-lauroyl-L-glutamate (cholesteryl / behenyl / octyldodecyl), cholesteryl butyrate, and cholesteryl stearate And fatty acid sterol esters such as cholesteryl isostearate, phytosteryl isostearate, cholesteryl hydroxystearate, cholesteryl oleate, and macadamia nut oil fatty acid cholesteryl, among which phytosteryl isostearate is preferred.

  (B) The compounding quantity of a component is 0.05 to 1% of the whole composition, Preferably it is 0.1 to 0.8%, More preferably, it is 0.1 to 0.5%. As the blending amount increases, the absorption promoting effect increases, and if it is less than 0.05%, the absorption promoting effect cannot be obtained. If it exceeds 1%, the oily odor becomes so strong that it is difficult to mask, and the feeling of use is poor.

Component (C), tocopherol and / or a derivative thereof, has an effect of promoting blood circulation, and is an effective component for preventing or suppressing periodontal disease. Specific examples include tocopherol, tocopherol acetate, tocopherol nicotinate, tocopherol succinate and the like, and these may be used alone or in combination of two or more. In particular, tocopherol acetate which is an acetic ester of tocopherol is preferable.
The compounding amount of the component (C) is preferably 0.01 to 2%, more preferably 0.05 to 1% of the entire composition. Effectiveness increases as the blending amount increases, and if it is 0.01% or more, sufficient effectiveness is obtained. 2% or less is more suitable for sufficient masking of the oily odor.

(D) A component is at least 1 sort (s) chosen from the alkali metal salt of an inorganic acid and / or organic acid. In the present invention, if the component (D) is not contained, the oily odor is not suppressed and the feeling of use is inferior, and the storage stability of the component (C) becomes insufficient.
Examples of the inorganic acid include hydrochloric acid, sulfuric acid, phosphoric acid, nitric acid, carbonic acid, and bicarbonate. Examples of the organic acid include lactic acid, malic acid, tartaric acid, citric acid, succinic acid, fumaric acid, and acetic acid. The alkali metal salt is a sodium salt or a potassium salt. Specific examples of the compound include chloride salts such as sodium chloride and potassium chloride, sulfates such as sodium sulfate, sodium monohydrogen phosphate, disodium hydrogen phosphate, dipotassium hydrogen phosphate, trisodium phosphate, and the like. Phosphate, malate such as sodium malate, citrate such as sodium citrate, succinate such as monosodium succinate and disodium succinate, acetate such as sodium acetate, tartaric acid such as sodium tartrate Examples thereof include salts, nitrates such as sodium nitrate, carbonates such as sodium hydrogen carbonate, lactates such as sodium lactate, fumarate such as sodium fumarate, etc., and one or more can be used.
Among these, the preferred component (D) is an alkali metal chloride salt, sulfate salt or lactate salt, and more preferably a chloride salt or sulfate salt. Particularly preferred are sodium chloride, potassium chloride and sodium sulfate, with sodium chloride and sodium sulfate being particularly preferred. In addition, you may use 1 type chosen from a chloride salt, a sulfate, and a lactate individually or in combination of 2 or more types.

The component (D) is blended for the purpose of further improving the stabilizing effect of the component (C) by the component (E) by suppressing the oily odor and using the component (E) in combination.
(D) As for the compounding quantity of a component, 1-10% of the whole composition is preferable, 1-8% is more preferable, More preferably, it is 2-6%. When it is 1% or more, the oily odor of the component (A) is sufficiently suppressed, and the effect of stabilizing the component (C) by the component (E) can be improved. The upper limit is not particularly limited with respect to the effect of the present invention, but if it exceeds 10%, the preparation stability such as liquid separation during storage may be inferior.

(E) The polyoxyethylene alkyl ether preferably has an average added mole number of ethylene oxide of 3 to 8 moles and an alkyl group having 16 to 18 carbon atoms.
Specifically, polyoxyethylene (3) cetyl ether, polyoxyethylene (5) cetyl ether, polyoxyethylene (7) cetyl ether, polyoxyethylene (3) stearyl ether, polyoxyethylene (4) stearyl ether, Examples include polyoxyethylene (5) stearyl ether, polyoxyethylene (6) stearyl ether, polyoxyethylene (7) stearyl ether, polyoxyethylene (8) stearyl ether, and these may be used alone or in combination of two or more. You may combine. Among them, polyoxyethylene (5) stearyl ether, polyoxyethylene (8) stearyl ether, polyoxyethylene (3) cetyl ether, particularly polyoxyethylene (5) stearyl ether and polyoxyethylene (3) cetyl ether are preferable. In addition, the numerical value in () is the average added mole number of ethylene oxide (the same applies hereinafter).
As these polyoxyethylene alkyl ethers, for example, those commercialized from Nippon Emulsion Co., Ltd. or Nikko Chemicals Co., Ltd. can be used.

  The amount of component (E) is preferably 0.05 to 2%, more preferably 0.1 to 1.5%, still more preferably 0.1 to 0.8%, especially 0.1. ~ 0.4% is preferred. If it is less than 0.05%, the stabilizing effect of the component (C) does not appear. Moreover, when there are too many compounding quantities, there exists a possibility that it may be inferior to foaming property, and it is suitable in order to fully maintain foaming property that it is 2% or less.

  In the present invention, the total amount of the component (D) and the component (E) is important for the storage stability of the component (C). (D) + (E) which shows the total amount of (D) component and (E) component is 2% or more with respect to the whole composition, 2.5% or more is preferable and 3% or more is more preferable. Storage stability of (C) component is fully acquired as it is 2% or more. An upper limit is good as a sum total of each compounding quantity upper limit of (D) and (E) component.

  In the present invention, (D) / (B) indicating the blending ratio of the component (D) to the component (B) is 5 or more, preferably 6 or more, more preferably 10 or more, and still more preferably. 100 or less, particularly 80 or less, especially 50 or less. In 5 or more, an oily odor is suppressed and a favorable usability is obtained. If it is less than 5, the oily odor is not masked and the usability is poor. Moreover, when it exceeds 100, saltiness is too strong and a usability | use_condition may be inferior.

  In the present invention, (E) / (B) indicating the blending ratio of the (E) component to the (B) component is 5 or less, preferably 4 or less, more preferably 3 or less, and still more preferably. 0.4 or more, particularly 0.5 or more, particularly 0.8 or more. By being 5 or less, the absorptivity of (A) component is fully maintained. If it exceeds 5, the absorption promoting effect of the component (A) by the component (B) is inhibited and the absorption rate is lowered. In addition, the lower limit is not particularly limited for the effect of the present invention, but if it is less than 0.4, the dispersibility of the component (A) in the preparation deteriorates, and uniformity in the preparation cannot be maintained. There is a risk of damaging the appearance.

  The dosage form and shape of the composition for oral cavity of the present invention are not particularly limited. For example, emulsion (emulsion, suspension, etc.), semi-solid (gel, cream, paste, etc.), solid (tablet, particulate agent, Capsules, films, kneaded materials, molten solids, waxy solids, elastic solids, etc.). Moreover, according to a dosage form etc., well-known components other than the said component can be mix | blended suitably as needed, and can be prepared by a conventional method. For example, abrasives, thickeners, binders, surfactants other than component (E), sweeteners, preservatives, fragrances, colorants, pH adjusters, active ingredients other than components (A) and (C), etc. Is mentioned.

  As abrasives, silica-based abrasives such as silicic anhydride, crystalline silica, amorphous silica, silica gel, aluminosilicate, etc., zeolite, calcium hydrogen phosphate anhydrous, calcium hydrogen phosphate dihydrate, calcium pyrophosphate , Calcium carbonate, sodium hydrogen carbonate, aluminum hydroxide, alumina, magnesium carbonate, tertiary magnesium phosphate, zirconium silicate, tertiary calcium phosphate, hydroxyapatite, quaternary calcium phosphate, synthetic resin-based abrasive and the like. The abrasive may be unblended (0%), but when the abrasive is blended, the blending amount is usually 1 to 50%, particularly 10 to 30% of the entire composition.

  As the thickening agent, sugar alcohol such as sorbit, glycerin, xylit, reduced starch saccharified product, propylene glycol, average molecular weight 200 to 6,000 (average molecular weight described in Quasi-drug Raw Material Standard 2006, the same applies hereinafter) polyethylene. Examples thereof include polyhydric alcohols such as glycol and ethylene glycol. These amounts are usually 1-60%, especially 10-55% of the total composition.

  As binder, pullulan, gelatin, methylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, sodium carboxymethylcellulose, carrageenan, sodium alginate, xanthan gum, sodium polyacrylate, gum arabic, guar gum, locust bean gum, polyvinyl alcohol, polyvinylpyrrolidone, Examples thereof include organic binders such as carboxyvinyl polymer, and inorganic binders such as thickening silicic anhydride and bentonite. These compounding quantities are 0.1 to 5% of the whole composition normally.

As the surfactant, a general anionic surfactant for oral preparations, nonionic surfactants other than the component (E), cationic surfactants, and amphoteric surfactants can be blended.
Examples of the anionic surfactant include N-acyl amino acid salts, N-acyl taurine salts, α-olefin sulfonates, N-acyl sulfonates, alkyl sulfates, sulfates of glycerol fatty acid esters, and the like. . Among these, N-acylamino acid salts, N-acyl taurine salts, α-olefin sulfonates, alkyl sulfates and the like are preferable in terms of versatility, and lauroyl sarcosine sodium in terms of foamability and hard water resistance. More preferred are sodium lauroylmethyl taurine, sodium α-olefin sulfonate having 10 to 16 carbon atoms as the carbon chain length of the alkyl chain, and sodium lauryl sulfate.
Nonionic surfactants include sugar fatty acid esters such as sucrose fatty acid esters, sugar alcohol fatty acid esters such as maltitol fatty acid esters, sorbitan fatty acid esters, glycerin fatty acid esters, polyglycerin fatty acid esters, polyoxyethylene hydrogenated castor oil, and the like. Can be mentioned. In addition, the said ester is different from the ester of (B) component.
Examples of cationic surfactants include alkylammonium and alkylbenzylammonium salts. Amphoteric surfactants include betaine types such as alkylbetaines and fatty acid amidopropylbetaines, betaine types such as alkylimidazolinium betaines, Examples include imidazoline type.
The blending amount of the surfactant is usually 0.001 to 10%, particularly 0.01 to 5% of the whole composition, and the total amount including the blending amount of the component (E) is preferably within the above range.

  Examples of the sweetening agent include saccharin sodium, stevioside, neohesperidin dihydrochalcone, glycyrrhizin, perilartin, p-methoxycinnamic aldehyde, thaumatin, palatinose, maltitol, xylitol, arabitol and the like. A sweetener can be used individually by 1 type or in combination of 2 or more types. When a sweetener is used, the blending amount can be appropriately determined within a range not impairing the effects of the present invention.

  Examples of the preservative include paraoxybenzoic acid esters such as sodium benzoate, methylparaben, ethylparaben, and butylparaben, ethylenediaminetetraacetate, benzalkonium chloride, and the like. A preservative can be used individually by 1 type or in combination of 2 or more types. When a preservative is used, the blending amount can be appropriately determined within a range not impairing the effects of the present invention.

As a fragrance | flavor, the fragrance | flavor component which can be used for an oral formulation can be used individually or as a fragrance | flavor composition which combined multiple.
For example, 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, grapefruit oil, sweetie oil, Natural fragrances such as coconut oil, Iris concrete, absolute peppermint, absolute rose, orange flower, and processing of these natural fragrances (front reservoir cut, rear reservoir cut, fractional distillation, liquid-liquid extraction, essence, powdered fragrance Etc.) fragrance, menthol, carvone Anethole, cineol, methyl salicylate, cinnamic aldehyde, eugenol, 3-l-menthoxypropane-1,2-diol, thymol, linalool, linalyl acetate, limonene, menthone, menthyl acetate, N-substituted paramentan-3- Carboxamide, pinene, octylaldehyde, citral, pulegone, carbyl acetate, anisaldehyde, ethyl acetate, ethyl butyrate, allylcyclohexane propionate, methyl anthranilate, ethyl methyl phenyl glycidate, vanillin, undecalactone, hexanal, Butanol, isoamyl alcohol, hexenol, dimethyl sulfide, cycloten, furfural, trimethylpyrazine, ethyl lactate, ethylthioacetate Oral composition such as strawberry flavor, apple flavor, banana flavor, pineapple flavor, grape flavor, mango flavor, butter flavor, milk flavor, fruit mix flavor, tropical fruit flavor, etc. The known fragrance materials used in the above can be used in combination, but are not limited to the fragrances described in the examples. The blending amount is not particularly limited, however, the above fragrance material is preferably used in the composition in an amount of 0.000001 to 1%, and the fragrance material using the above fragrance material is 0.1% in the composition. It is preferred to use ~ 2%.

  Examples of the colorant include natural pigments such as safflower red pigment, gardenia yellow pigment, gardenia blue pigment, perilla pigment, red potato pigment, red cabbage pigment, carrot pigment, hibiscus pigment, cacao pigment, spirulina pigment, and coumarindo pigment. Red 3, No. 104, Red No. 105, Red No. 106, Yellow No. 4, Yellow No. 5, Green No. 3, Blue No. 1 and other legal dyes, riboflavin, copper chlorofin sodium, titanium dioxide and the like. . When mix | blending a coloring agent, it is preferable that the compounding quantity is 0.00001 to 3% of the whole composition.

  The pH (20 ° C.) of the oral composition of the present invention is usually 6 to 10, preferably 6 to 8. Examples of the pH adjuster include acids and alkalis such as acetic acid, hydrochloric acid, sulfuric acid, nitric acid, citric acid, phosphoric acid, malic acid, gluconic acid, maleic acid, succinic acid, glutamic acid, sodium hydroxide, and potassium hydroxide. It is done. When a pH adjuster is blended, the blending amount can be appropriately determined within a range not impairing the effects of the present invention.

Examples of active ingredients other than the components (A) and (C) include anti-inflammatory agents, tissue activators, vitamins, bactericides, astringents, and fluorine. Specific examples include fungicides such as isopropylmethylphenol and cetylpyridinium chloride, and fluorides such as sodium fluoride and sodium monofluorophosphate. These can be blended in an effective amount as long as the effects of the present invention are not hindered.
The liquid medium is usually water, and a monovalent lower alcohol having 1 to 3 carbon atoms such as ethanol may be added.

  EXAMPLES Hereinafter, although an Example, a comparative example, a formulation example is shown and this invention is demonstrated concretely, this invention is not restrict | limited to the following Example. In the following examples, “%” means “% by mass” unless otherwise specified.

[Examples and Comparative Examples]
Dentifrice compositions having the compositions shown in Tables 1 to 3 were prepared by conventional methods and evaluated by the following methods. The results are shown in Tables 1-3.

(1) Test method for absorbability of water-soluble active ingredients <Experimental method>
Hamster teak pouch (Japan SLC, 6 weeks old cocoon) was immersed in artificial saliva (50 mM KCl, 1 mM KH ₂ PO ₄ , 1 mM CaCl ₂ , 0.1 mM MgCl ₂ , pH 7.0) for 24 hours and then placed in Franz cell. After filling the receptor side with physiological saline, 500 μL of a test sample (dentifrice 3 times diluted artificial saliva diluted solution) was added to the donor side. After 24 hours, the amount of the water-soluble active ingredient (tranexamic acid) in the receptor solution was measured by HPLC.
Tranexamic acid was quantified using HPLC according to the following test conditions. The absorption rate when the absorption rate of tranexamic acid of the blank preparation not containing the (B) component isostearic acid and phytosteryl isostearate was taken as 100% was calculated, and the absorbability of tranexamic acid was determined according to the following criteria.

Measurement condition;
The HPLC conditions for quantifying tranexamic acid are as follows.
Column: CAPCELL PAK C18 MG-II S-3
-Column temperature: 40 ° C
・ Mobile phase: 0.2% phosphoric acid solution 5% methanol ・ Detector: UV absorption photometer (measurement wavelength: 210 nm)
Used equipment;
・ Pump: JASCO PU-980
・ Sample introduction part: Kyowa Precision Co., Ltd. KSP-100X
-Detector: JASCO Corporation UV-970
Column thermostat: Senshu Science Co., Ltd. SCC-2100
・ Flow rate: 1 mL / min

Judgment criteria;
◎: 200% or more ○: 150% or more and less than 200% △: 110% or more and less than 150% ×: less than 110%

(2) Evaluation method of storage stability of tocopherol or derivative thereof Tocopherol acetic acid using HPLC according to the following test conditions for dentifrice composition after filling tube with 50 g of dentifrice composition and storing at 60 ° C. for 1 month The ester concentration was measured. The residual ratio when the concentration of tocopherol acetate immediately after production of each sample was 100% was calculated, and the effect of inhibiting decomposition of tocopherol acetate was determined according to the following criteria.
Measurement condition;
Column: TSK-GEL ODS-80Ts 4.6 × 150 mm
-Column temperature: 25 ° C
-Mobile phase: Methanol-Detector: Ultraviolet absorptiometer (measurement wavelength: 284 nm)
Used equipment;
・ Pump: JASCO PU-980
・ Sample introduction part: Kyowa Precision Co., Ltd. KSP-100X
-Detector: JASCO Corporation UV-970
Column thermostat: Senshu Science Co., Ltd. SCC-2100
・ Flow rate: 1 mL / min

Judgment criteria;
◎: 95% or more and 100% or less ○: 90% or more and less than 95% △; 85% or more and less than 90% ×: less than 85%

(3) Usability Evaluation Method Ten expert panelists put the dentifrice composition on a toothbrush and used it to clean the mouth. evaluated. The average of 10 evaluation points was classified into the following criteria.
Odor evaluation criteria;
4 points: Feels no oily smell in the oral cavity 3 points: Feels almost no oily smell in the oral cavity 2 points: Feels the oily smell somewhat uncomfortable in the oral cavity 1 point: Oily smell in the oral cavity Criteria for smells that feel very uncomfortable;
◎: Average point 3.5 points or more ○: Average point 3.0 points or more and less than 3.5 points Δ: Average point 2.0 points or more and less than 3.0 points ×: Average point less than 2.0 points

  In addition, the taste and external appearance of the dentifrice composition of Examples 1-17 were favorable.

  A prescription example is shown below. The composition for oral cavity of the formulation example was excellent in the absorbability of the water-soluble active ingredient, the storage stability of tocopherol or a derivative thereof, and the oily odor was suppressed and the usability was good.

[Prescription Example 1] Toothpaste (A) Tranexamic acid 0.1%
(A) Oat extract 0.1
(B) Isostearic acid 0.3
(C) Tocopherol acetate 0.1
(D) Sodium chloride 5
(E) Polyoxyethylene (5) stearyl ether 0.4
Oat extract 0.1
Isopropylmethylphenol 0.1
Lauroyl sarcosine sodium 0.2
Sodium monofluorophosphate 0.73
Sorbit liquid (70%) 45
Polyoxyethylene (20) hydrogenated castor oil 0.4
Propylene glycol 4
Silicic anhydride (abrasive) 10
Silicic anhydride (thickening) 2
Xanthan gum 0.3
Sodium alginate 0.7
Carrageenan 0.7
Sodium lauryl sulfate 1.0
Palm oil fatty acid amidopropyl betaine 0.1
Methyl paraoxybenzoate 0.2
Saccharin sodium 0.07
Titanium oxide 0.4
Potassium aluminum sulfate 2
Sodium citrate 0.2
Sodium hydroxide 0.3
Fragrance 1.2
Purified water remaining
Total 100.0%
(D) / (B) = 16.67, (E) / (B) = 1.33, (D) + (E) = 5.4

[Prescription Example 2] Toothpaste (A) Tranexamic acid 0.1%
(B) Phytosteryl isostearate 0.2
(C) Tocopherol acetate 0.1
(D) Sodium sulfate 2
(E) Polyoxyethylene (5) Stearyl ether 0.75
Isopropylmethylphenol 0.1
Lauroyl sarcosine sodium 0.2
Sodium fluoride 0.21
Sorbit liquid (70%) 55
Polyoxyethylene (20) hydrogenated castor oil 0.75
Propylene glycol 3.5
Silicic anhydride (thickening) 6
Xanthan gum 1.2
Sodium alginate 0.3
Sodium lauryl sulfate 1
Methyl paraoxybenzoate 0.2
Saccharin sodium 0.09
Fragrance 1.2
Purified water remaining
Total 100.0%
(D) / (B) = 10, (E) / (B) = 3.75, (D) + (E) = 2.75

[Prescription Example 3] Toothpaste (A) Dipotassium glycyrrhizinate 0.1%
(A) ε-aminocaproic acid 0.1
(B) Isostearic acid 0.1
(C) Tocopherol acetate 0.1
(D) Sodium chloride 4
(D) Sodium sulfate (2Na) 1
(E) Polyoxyethylene (3) Cetyl ether 0.5
Cetylpyridinium chloride 0.1
Sodium fluoride 0.21
Sorbit liquid (70%) 45
Propylene glycol 3
Silicic anhydride (abrasive) 15
Silicic anhydride (thickening) 4
Xanthan gum 0.4
Sodium carboxymethylcellulose 1
Lauroylmethyl taurine sodium 1.2
Palm oil fatty acid amidopropyl betaine 1
Methyl paraoxybenzoate 0.2
Saccharin sodium 0.18
Titanium oxide 0.1
Sodium citrate 0.5
Citric acid 0.4
Fragrance 1
Purified water remaining
Total 100.0%
(D) / (B) = 50, (E) / (B) = 5, (D) + (E) = 5.5

Claims (9)

(A) at least one water-soluble active ingredient,
(B) 0.05 to 1% by mass of at least one selected from fatty acids and esters having a branched chain structure having 8 to 22 carbon atoms,
(C) Tocopherol and / or its derivative,
(D) containing at least one selected from alkali metal salts of inorganic acids and / or organic acids, and (E) polyoxyethylene alkyl ether,
The total amount of components (D) and (E) is 2% by mass or more, (D) / (B) is 5 or more as a mass ratio, and (E) / (B) is 5 or less as a mass ratio. An oral composition characterized by the above.   The water-soluble active ingredient (A) is at least one selected from tranexamic acid, allantoin and its derivatives, ε-aminocaproic acid, sodium azulenesulfonate, glycyrrhizinate, ascorbate, pyridoxine hydrochloride and a buckthorn extract. The composition for oral cavity according to claim 1.   The composition for oral cavity according to claim 1 or 2, wherein the component (B) is isostearic acid and / or phytosteryl isostearate.   The oral composition according to any one of claims 1 to 3, wherein the component (D) is selected from alkali metal chloride salts, sulfate salts, and lactate salts.   The oral composition according to any one of claims 1 to 4, wherein the component (D) is selected from alkali metal chlorides and sulfates.   The component (E) is a polyoxyethylene alkyl ether having an average added mole number of ethylene oxide of 3 to 8 moles and an alkyl group having 16 to 18 carbon atoms, or the oral cavity according to any one of claims 1 to 5. Composition.   The composition for oral cavity according to any one of claims 1 to 6, comprising 1 to 10% by mass of component (D) and 0.05 to 2% by mass of component (E).   The composition for oral cavity according to any one of claims 1 to 7, wherein (D) / (B) is from 5 to 100 in terms of mass ratio, and (E) / (B) is from 0.4 to 5 in terms of mass ratio. object.   The composition for oral cavity according to any one of claims 1 to 8, comprising 0.001 to 0.5 mass% of the component (A) and 0.01 to 2 mass% of the component (C).