JP2022039864A - Dentifrice composition - Google Patents

Abstract

To provide a dentifrice composition whereby: in the case where limonene, which is a key component of a citrus flavor generally used to improve the palatability of an oral composition, and tranexamic acid are used in combination, the residual amount of the tranexamic acid decreases with time.SOLUTION: A dentifrice composition contains (A) tranexamic acid, (B) limonene, and (C) thickening silica 4-10 mass%.SELECTED DRAWING: None

Description

The present invention relates to improving the stability of tranexamic acid in dentifrice compositions.

Antiplasmin agents such as tranexamic acid have excellent anti-inflammatory and hemostasis effects and are known to be effective in preventing periodontal disease. For example, in Patent Document 1, compounding in an oral composition. Has been examined and proposed.

It is known that tranexamic acid has a problem in stability during storage, and the residual amount in the formulation decreases with time. For example, Patent Document 2 describes powder such as titanium oxide, silicone oil, and silicone-based interface. It is described that the amount of tranexamic acid is maintained for a long period of time in the water-in-oil emulsified composition containing an activator and the like.

Japanese Unexamined Patent Publication No. 9-95429 Japanese Unexamined Patent Publication No. 2019-6712

However, a method for stably blending tranexamic acid in the dentifrice composition has not yet been proposed, and limonene, which is a main component of a citrus-based fragrance that is widely used to improve the palatability of the dentifrice composition, is used. When tranexamic acid is used in combination, there is a problem that the residual amount of tranexamic acid decreases with time.

As a result of diligent research in view of the above problems, the present inventors surprisingly obtained (C) thickening silica for a dentifrice composition containing (A) tranexamic acid and (B) limonene. It has been found that the above-mentioned problems can be solved by further blending.

The present invention includes, for example, the inventions described below.
Item 1.
A dentifrice composition containing (A) tranexamic acid, (B) limonene, and (C) 4 to 10% by mass of thickened silica.
Item 2.
Item 2. The dentifrice composition according to Item 1, wherein the content of the component (A) is 0.01 to 0.3% by mass, and the content of the component (B) is 0.001 to 1% by mass.
Item 3.
Item 2. The dentifrice composition according to Item 2, wherein the average particle size of (C) is 20 μm or less and the oil absorption amount is 1.5 to 5 mL / g.

Provided is a dentifrice composition containing tranexamic acid and suppressing a decrease in the amount of tranexamic acid over time.

The results of the tranexamic acid quantitative test are shown.

Hereinafter, each embodiment included in the present invention will be described in more detail. The present invention preferably includes, but is limited to, a dentifrice composition, particularly a dentifrice composition containing (A) tranexamic acid, (B) limonene, and (C) thickening silica. Rather, the invention includes everything disclosed herein and recognizable by those of skill in the art.

The (A) tranexamic acid used in the present invention can be used without particular limitation as long as it is usually used in pharmaceuticals, quasi-drugs, and cosmetics. The tranexamic acid is a trans-4-aminomethylcyclohexane-1-carboxylic acid, and examples of commercially available products include "Japanese Pharmacopoeia tranexamic acid" (Maruzen Pharmaceuticals Co., Ltd.). In addition to tranexamic acid, tranexamic acid salts (metal salts such as magnesium, calcium, sodium, potassium, phosphates, hydrochlorides, hydrogen bromides, sulfates, etc.), tranexamic acid esters (vitamin A ester, vitamin E ester, etc.) (Vitamin ester such as Vitamin C ester, alkyl ester), tranexamic acid amide, dimer of tranexamic acid and the like can also be used.

The blending amount of (A) tranexamic acid is preferably 0.01 to 0.3% by mass with respect to the total amount of the composition. If the blending amount is less than 0.01% by mass, the antiplasmin effect may not be exhibited. On the other hand, if the blending amount exceeds 0.3%, the usability of the composition may be deteriorated due to the bitterness peculiar to tranexamic acid. The blending amount of (A) tranexamic acid is more preferably 0.02 to 0.2% by mass, further preferably 0.03 to 0.1% by mass, and most preferably 0.05% by mass. The blending amounts of the component (A) are 0.02, 0.04, 0.06, 0.07, 0.08, 0.09, 0.1, 0.11, 0.12, 0.13, It may be 0.14, 0.15, 0.16, 0.17, 0.18, 0.19, 0.2, 0.25% by mass.

The (B) limonene used in the present invention is d-limonene and can be used without particular limitation as long as it is d-limonene and is usually used in pharmaceuticals, quasi-drugs and cosmetics. This can be suitably used as a single product or an essential oil. For the single product, chemically synthesized or refined oil is used, and as the essential oil, lemon oil, orange oil, grapefruit oil or the like containing d-limonene is used. be able to.

The blending amount of (B) limonene is preferably 0.001 to 1% by mass with respect to the total amount of the composition. The blending amount of (B) limonene is more preferably 0.01 to 0.5% by mass, further preferably 0.05 to 0.3% by mass, and most preferably 0.2% by mass. The blending amount of (B) limonene is 0.003, 0.005, 0.02, 0.03, 0.04, 0.06, 0.08, 0.1, 0.3, 0.4, It may be 0.5, 0.6, 0.7, 0.8, 0.9, 1% by mass.

The (C) thickening silica used in the present invention is a known component having a thickening action, and has a larger oil absorption than the silica used in a dentifrice composition as ordinary abrasive silica. The oil absorption of the thickened silica (C) is usually 1.5 mL / g or more, preferably 1.5 to 5 mL / g, and more preferably 2 to 4 mL / g. The average particle size of (C) thickening silica is usually 20 μm or less, preferably 1 to 18 μm, and more preferably 1.5 to 15 μm. The oil absorption amount indicates the amount of oil that silica can support, and the measuring method is specified by the method of JISK5101-13-2 (established in 2004) and the amount of oil absorbed in the boiled linseed oil. Means a value.

The blending amount of the thickening silica (C) is preferably 4 to 10% by mass, more preferably 5 to 8% by mass, based on the total amount of the composition. Further, the blending amount of (C) thickening silica may be 4.5, 5.5, 6, 6.5, 7, 8, 9, or 10% by mass.

The dentifrice composition of the present invention can be produced by a conventional method. Further, the dentifrice composition of the present invention can be used as a quasi-drug or a cosmetic product.

In the dentifrice composition of the present invention, known arbitrary components that can be generally blended in an oral composition may be further blended alone or in combination of two or more, as long as the effects of the present invention are not impaired. ..

Such known optional components include, for example, surfactants, fungicides, abrasives, wetting agents, thickeners, sweeteners, preservatives, colorants, pH regulators, stabilizers, flavoring agents, astringents. Examples include agents, fragrances, and other medicinal ingredients.

As the surfactant, for example, an anionic surfactant, a nonionic surfactant, or an amphoteric surfactant can be blended. Specifically, examples of the anionic surfactant include an alkyl sulfate ester salt, a polyoxyethylene alkyl ether sulfate ester salt, an alkyl sulfosuccinate, a polyoxyethylene alkyl ether sulfosuccinate, an N-acyl amino acid salt, and N-. Examples thereof include acyl taurine salt, alkyl ether carboxylate, alkyl phosphate, polyoxyethylene alkyl ether phosphate, fatty acid monoglyceride sulfate, and alkyl sulfoacetate. Examples of the nonionic surfactant include fatty acid esters, fatty acid alkanolamides, sorbitan fatty acid esters, fatty acid monoglycerides, polyglycerin fatty acid esters, polyoxyethylene alkylphenyl ethers, alkyl glycosides, diethyl sebacate, and polyoxyethylene hydrogenated castor oil. Examples thereof include fatty acid polyoxyethylene sorbitan. Examples of the amphoteric ion surfactant include alkyldimethylaminoacetic acid betaine, alkylamide propyldimethylaminoacetic acid betaine, N-acyl-N-carboxymethyl-N-hydroxyethylethylenediamine, N-alkylaminoethylglycine and the like. These surfactants can be blended alone or in combination of two or more. The blending amount is usually 0.1 to 5% by mass with respect to the total amount of the composition.

Examples of the bactericidal agent include cationic bactericides such as benzalkonium chloride, benzethonium chloride and chlorhexidine hydrochloride, vitamin Es such as dl-α-tocopherol acetate, tocopherol succinate, or tocopherol nicotinate, and todecyldiaminoethylglycine. Examples thereof include amphoteric bactericides such as triclosan and nonionic bactericides such as triclosan. These fungicides may be further blended alone or in combination of two or more.

As an abrasive, for example, dibasic calcium phosphate dihydrate and anhydrate, calcium phosphate, tertiary calcium phosphate, calcium carbonate, calcium pyrophosphate, aluminum hydroxide, alumina, silicic acid anhydride, silica gel, aluminum silicate, insoluble metaphosphoric acid. Examples thereof include sodium, tertiary magnesium phosphate, magnesium carbonate, calcium sulfate, polymethyl methacrylate, bentonite, zirconium silicate, hydroxyapatite, synthetic resin and the like. These abrasives can be blended alone or in combination of two or more.

Examples of the wetting agent include ethylene glycol, propylene glycol, 1,3-butylene glycol, polypropylene glycol, xylit, martit, lacchit, palatinit, polyethylene glycol and the like. These wetting agents can be blended alone or in combination of two or more.

Examples of the preservative include parabens such as methylparaben, ethylparaben, propylparaben and butylparaben, sodium benzoate, phenoxyethanol, alkyldiaminoethylglycine hydrochloride and the like. These preservatives can be blended alone or in combination of two or more.

Examples of the pH adjuster include citric acid, phosphoric acid, malic acid, pyrophosphate, lactic acid, tartaric acid, glycerophosphate, acetic acid, nitric acid, chemically possible salts thereof, sodium hydroxide and the like. These pH adjusting agents can be blended alone or in combination of two or more.

Examples of the stabilizer include sodium edetate, sodium thiosulfate, sodium sulfite, sodium chloride, calcium lactate, lanolin, triacetin, castor oil, magnesium sulfate and the like. These stabilizers can be blended alone or in combination of two or more.

Examples of the flavoring agent include tea extract, tea dry distillate, propolis extract, monosodium glutamate and the like.

Examples of the astringent include baking soda, aluminum lactate and the like.

Other medicinal agents include fluorine compounds such as sodium fluoride, sodium monofluorophosphate and stannous fluoride; enzymes such as dextranase, mutanase, amylases, proteases and lytic enzymes (Litec Enzyme); ε-aminocapron. Acids, aluminum chlorhydroxyalantin, allantoin, dihydrocholesterol, glycyrrhizinic acids, glycyrrhetinic acid, bisabolol, glycerophosphate, chlorophyll, copper gluconate, sodium chloride, water-soluble inorganic phosphate compounds; vitamins such as pyridoxin acetate, ascorbic acid or salts thereof. Kind is mentioned.

Furthermore, the present invention also includes a method of suppressing a decrease in the residual amount of (A) tranexamic acid in the presence of (B) limonene by (C) thickening silica. Even in this case, the blending amount of each component is preferably in the above range.

Hereinafter, the present invention will be described in detail based on examples, but the present invention is not limited to these examples.

<Preparation and storage of test composition>
The test composition was prepared by a conventional method according to the formulation shown in Table 1. 25 g of each test composition was filled in an aluminum laminated tube (body diameter: 22 mm) having a shoulder made of high-density polyethylene, and stored at 65 ° C. for 5 days. After 5 days, 2 g of each test composition was separated from the laminated tube of each dentifrice composition, and tranexamic acid was quantified by a liquid chromatography method. The thickening silica used in this example is Sorbosil TC15 (manufactured by PQ Corporation), the average particle size thereof is 17 μm or less, and the oil absorption amount is 2.1 to 3.4 mL / g.

<Method for quantifying tranexamic acid>
Water was added to 2 g of the test composition to make 100 mL, which was used as a sample solution. In addition, as a standard solution, the standard tranexamic acid was weighed, water was added, and the solution was accurately measured.

<High Performance Liquid Chromatography Measurement Conditions>
Detector: Two pumps for mobile phase and reaction reagent delivery, sample introduction part, column, reaction unit, detector and recording device, and the reaction unit was kept at a constant temperature.
Equipment: Fluorometer (excitation wavelength: 348 nm, fluorescence wavelength: 456 nm)
Column: Octadecylsilylated silica gel for liquid chromatography Column temperature: 40 ° C
Mobile phase: Sodium perchlorate mixed solution Reaction reagent: o-phthalaldehyde reagent

<Calculation of tranexamic acid reduction>
Then, the reduction amount (%) of tranexamic acid in each dentifrice composition after storage was calculated based on the blending amount of tranexamic acid at the time of preparation of each dentifrice composition (100%).

Hereinafter, Table 1 and FIG. 1 show the results of the examples of the present invention and the tranexamic acid quantitative test.

As shown in Table 1, by containing a certain amount of thickening silica in addition to tranexamic acid and limonene, the decrease in the amount of tranexamic acid when stored at 65 ° C. for 5 days was suppressed.

Hereinafter, Tables 2 to 5 show formulation examples of the oral composition of the present invention.

Claims (3)

(A) Tranexamic acid (B) Limonene (C) Viscous silica 4-10% by mass
A dentifrice composition containing. The content of the component (A) is 0.01 to 0.3% by mass,
The dentifrice composition according to claim 1, wherein the content of the component (B) is 0.001 to 1% by mass. The dentifrice composition according to claim 2, wherein the average particle size of (C) is 20 μm or less and the oil absorption amount is 1.5 to 5 mL / g.

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