KR20190076829A - Oral composition and method for inhibiting discoloration thereof - Google Patents

Abstract

The present invention relates to an oral composition containing tranexamic acid with suppressed preparation discoloration even after high temperature storage and excellent appearance stability, and a method for inhibiting discoloration thereof. The oral composition comprises (A) tranexamic acid, (B) cationized cellulose, and (C) tea extract, in which [(A)+(B)]/(C) is 0.5 to 200 as mass ratio, and (B)/(C) is 0.2 to 100 as mass ratio. The oral composition further comprises (D) at least one selected from 3-octanol, 3-octyl acetate, 3-octanone, and fenchone. The method for inhibiting discoloration of the oral composition mixes the (C) component in the oral composition mixed with the (A) and (B) components, in which the mass ratio of [(A)+(B)]/(C) and the mass ratio of (B)/(C) are each within the above range.

Description

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a composition for oral use and a method for inhibiting discoloration thereof,

The present invention relates to a composition for oral use containing tranexamic acid and a method for inhibiting discoloration thereof, the composition being discolored even after storage at high temperature and having excellent appearance stability.

Tranexamic acid is a functional ingredient having an anti-inflammatory effect of the gum, and is incorporated in an oral composition as a periodontal disease preventing ingredient (Patent Document 1: Japanese Patent Laid-Open Publication No. 2009-149565), and tranexamic acid Patent Document 2 (Japanese Patent Application Laid-Open No. 2001-226244) proposes that a hydroxyethyl cellulose dimethyldiallylammonium salt is effective for improving the retention in the mouth and improving the effect.

In addition, tranexamic acid has been proposed in Patent Documents 3 and 4 (Japanese Patent Application Laid-Open No. 2008-143870 and Japanese Patent Application Laid-open No. 60-130509) that can be applied to improvement of feeling on use of oral compositions.

However, there is a problem that in the case of tranexamic acid, the coloring of the preparation may occur with time depending on the components to be mixed. Patent Literatures 5 and 6 (Japanese Patent No. 4656299 and Japanese Patent No. 5842565) disclose a technique for suppressing discoloration. Patent Document 6 discloses a technique in which trinne triacane and cinnamic aldehyde In combination with a specific amount of sodium lauryl sulfate to suppress discoloration of the formulation over time, thereby improving the appearance stability.

Patent Document 1: JP-A-2009-149565 Patent Document 2: JP-A-2001-226244 Patent Document 3: Japanese Patent Application Laid-Open No. 2008-143870 Patent Document 4: Japanese Patent Application Laid-Open No. 60-130509 Patent Document 5: Japanese Patent No. 4656299 Patent Document 6: Japanese Patent No. 5842565

The present invention has been made in view of the above circumstances, and it is an object of the present invention to provide an oral composition containing tranexamic acid and a method for inhibiting discoloration thereof, which can suppress discoloration of a preparation even after preservation at a high temperature and provide excellent appearance stability.

The inventors of the present invention have conducted intensive studies in order to achieve the above object and as a result, it has been found that it is effective to blend tea extracts at a specific ratio in inhibiting discoloration of a preparation caused by blending of tranexamic acid and cationic cellulose in an oral composition Respectively. That is, in the present invention, (C) tea extract is compounded in an oral composition containing (A) a tranexamic acid and (B) (B) / (C) within a specific range, it is possible to provide a composition for oral cavity which suppresses discoloration of a preparation even after preservation at high temperature, gives excellent appearance stability and suppresses unpleasant taste, The present invention has been accomplished.

More specifically, as described above, it is not known that the hydroxyethyl cellulose-dimethyldiallylammonium salt of cationic cellulose is effective for improving retention of tranexamic acid in the oral cavity in the dentifrice composition (Patent Document 2) The inventors of the present invention have found that (A) tranexamic acid is blended with an oral composition in combination with (C) cationic cellulose to improve retention in the oral cavity, and the problem that browning occurs after storage at high temperature, Furthermore, it has also been found that the above-mentioned discoloration of the preparation due to browning is not recognized when sodium carboxymethyl cellulose is used as the cellulose derivative, and is a unique problem to be caused when the components (A) and (B) are used in combination. (A) + (B)] / (C) by combining the component (C) with the combination system of the components (A) and (B). As a result, Component (C) specifically acts within a specific range of the mass ratio of (B) / (C), thereby suppressing discoloration of the preparation by the combination system, So that excellent appearance stability could be obtained. In this case, when the components (A) and (B) are used in combination in this case, unpleasant tastes unique to the mouth may remain after use, but the aftertaste of this unpleasant taste is also improved by the component (C) .

(A) + (B)] / (C), even when the components (A), (B) and (C) are used in combination, the effect of the present invention ) And the mass ratio of (B) / (C) is inadequate, and in addition to the components (A) and (B) When the licorice extract, which is a plant extract, was used in combination, it was inferior.

In addition, the dentifrice composition of Patent Document 2 contains hydroxyethyl cellulose dimethyldiallylammonium salt together with tranexamic acid and anionic surfactant and anionic surfactant such as anethole, carbone, cineol, methyl salicylate, Ethyl butyrate and cinnamic aldehyde, and the retention properties and storage stability (liquid separation) of tranexamic acid in oral cavity are improved. On the other hand, in the oral composition containing the components (A), (B) and (C) of the present invention, the composition discoloration due to the component (A) is suppressed even after the above- Excellent appearance stability (discoloration) and good taste.

Accordingly, the present invention provides the following composition for oral use and a method for suppressing discoloration thereof.

[1] (A) Tranexamic acid,

(B) cationic cellulose and

(B) / (C) is in a mass ratio of 0.5 to 200, and (B) / (C) is in a mass ratio of 0.2 to 100, Composition.

[2] The oral composition according to [1], wherein the cationic cellulose (B) is hydroxyethyl cellulose dimethyldiallylammonium chloride.

[3] The oral cavity according to [1] or [2], which contains 0.01 to 0.2% by mass of the component (A), 0.01 to 0.2% by mass of the component (B), and 0.0005 to 0.2% by mass of the component (C) / RTI >

[4] The composition according to any one of [1] to [3], which further comprises 0.0001 to 0.1% by mass of at least one selected from the group consisting of 3-octanol, 3-octyl acetate, Oral composition.

[5] The oral composition according to any one of [1] to [4], which is a skirt or a remedy.

(C) tea extract is added to an oral composition containing (A) tranexamic acid and (B) cationic cellulose, and the ratio of [(A) + (B)] / (C) To 200, and (B) / (C) in a mass ratio of 0.2 to 100.

[7] The oral composition according to [6], wherein the composition for oral cavity according to [6], which comprises 0.01 to 0.2 mass% of component (A), 0.01 to 0.2 mass% of component (B), and 0.0005 to 0.2 mass% / RTI >

According to the present invention, it is possible to provide a composition for oral care containing tranexamic acid, which is capable of suppressing discoloration of the preparation even after storage at a high temperature, imparting excellent appearance stability, and suppressing unpleasant taste and providing a pleasant taste. The composition for oral use of the present invention is suitable for gingival care which suppresses the oral gingivitis because of its excellent retention in the oral cavity of the tranexamic acid and anti-inflammatory effect.

Hereinafter, the present invention will be described in more detail. The oral composition of the present invention contains (A) tranexamic acid, (B) cationic cellulose and (C) tea extract.

(A) Tranexamic acid is an effective ingredient and has an anti-inflammatory action. The blending amount of (A) tranexamic acid is preferably 0.01 to 0.2% (mass%, the same applies hereinafter) of the whole composition, more preferably 0.03 to 0.1% from the viewpoint of anti-inflammatory effect and discoloration inhibition. Within this range, the discoloration of the preparation is sufficiently inhibited, and the unpleasant taste is sufficiently improved.

(B) Cationic cellulose has an effect of improving the retention of the component (A) in the oral cavity. Examples of the cationic cellulose (B) include dimethyldiallylammonium, 2-hydroxy-3 (trimethylammonio) propyl and the like added as a cationizing agent to a cellulose derivative. For example, hydroxyethyl cellulose dimethyldiallylammonium chloride, chlorinated O- [2-hydroxy-3- (trimethylammonio) propyl] hydroxyethyl cellulose, and the like. The nitrogen content is preferably from 0.1 to 3%, more preferably from 0.5 to 2%. 5%.

Specifically, hydroxyethyl cellulose dimethyldiallylammonium chloride is a product obtained by graft-polymerizing dimethyldiallylammonium salt on hydroxyethyl cellulose, and having a viscosity of 10 to 3,000 mPa · s in a 2% aqueous solution (BH Brookfield viscometer , Rotor No. 2, 20 revolutions, 21 캜) can be used. For example, Cellcoat L-200 (2% aqueous solution viscosity: 35 to 350 mPa s, BH Brookfield viscometer, rotor No. 2, 20 revolutions, 21 캜, measuring time 1 minute) manufactured by Akzo Nobel Co., , Cell coat H-100 (viscosity of 2% aqueous solution: 500 to 2,750 mPa 揃 s, BH type Brookfield viscometer, rotor No. 2, 20 revolutions, 21 캜, measuring time of 1 minute).

The viscosity of O- [2-hydroxy-3- (trimethylammonio) propyl] hydroxyethylcellulose chloride can be measured with a 1% or 2% aqueous solution and a viscosity of 1% aqueous solution of 500 to 2,600 mPa (BH type Brookfield viscometer, rotor No. 2, 20 revolutions, 25 캜) or a 2% aqueous solution having a viscosity of 5 to 800 mPa ((BL type viscometer, rotor No. 2, 25 DEG C) can be used. For example, Leogard KGP (2% aqueous solution viscosity: 5 to 50 mPa.s), Leogard G (2% aqueous solution viscosity: 100 to 600 mPa.s) : Leogard LP (2% aqueous solution viscosity: 300 to 800 mPa.s), Leogard MGP (1% aqueous solution viscosity: 500 to 1, 200 mPa.s) manufactured by Lion Corp., (Viscosity of 1% aqueous solution: 1,000 to 2, 600 mPa s), and the like.

Among these cationic cellulose, particularly hydroxyethyl cellulose dimethyldiallylammonium chloride is suitable in view of the retention tendency of (A) tranexamic acid in the mouth.

The blending amount of the (C) cationic cellulose is preferably 0.01 to 0.2%, more preferably 0.03 to 0.1%, from the viewpoint of the effect of discoloring the preparation and suppressing the unpleasant taste. Within this range, the discoloration of the preparation is sufficiently inhibited, and the unpleasant taste is sufficiently improved. If it exceeds 0.2%, the unpleasant taste by itself becomes strong, and the effect of improving the unpleasant taste may not be sufficiently obtained.

In the present invention, (C) tea extract acts as an inhibitor of discoloration of the preparation and also serves as an improper agent for improving taste.

C) The tea extract may be a commercially available product or a product obtained by a known method. Specifically, green tea can be used as a raw material. As the extraction solvent, a hydrophilic solvent can be used, and examples thereof include water, hydrophilic solvents such as lower monohydric alcohols such as ethanol and propanol, and polyhydric alcohols such as 1,3-butylene glycol and propylene glycol. One kind of a single solvent or a mixed solvent of two or more kinds can be used. The extraction conditions and the post-treatment can be carried out by conventional methods.

As a commercially available product, green tea extract (trade name: "may ism", 0.2% of extract, solvent: 50% of butylene glycol aqueous solution, manufactured by Maruzen Pharmaceutical Co., Ltd.) can be used.

The blending amount of the tea extract (C) is preferably 0.0005 to 0.2%, more preferably 0.001 to 0.1%, of the entire composition as the pure extract of the extract excluding the solvent. When the amount is more than 0.0005%, the discoloration of the preparation is sufficiently inhibited to obtain excellent appearance stability, the unpleasant taste is suppressed sufficiently, and the taste is improved. If it is 0.2% or less, the influence of the taste of the component (C) itself can be sufficiently prevented.

In the present invention, [(A) + (B)] / (C), which represents the ratio of the blending amount of the components (A) and (B) to the blending amount of the component (C) 0.5 to 200, and preferably 1 to 100. If the mass ratio of [(A) + (B)] / (C) is less than 0.5, the feeling of use is impaired by the taste of the component (C) itself, and if it exceeds 200, .

(B) / (C) representing the ratio of the blending amount of the component (B) to the blending amount of the component (C) (the amount of the extracted extract excluding the solvent) is 0.2 to 100 in mass ratio, to be. If the mass ratio of (B) / (C) is less than 0.2, the feeling of use is impaired by the taste of the component (C) itself. If it exceeds 100, the effect of improving the unpleasant taste is inferior.

In the present invention, it is also preferable to incorporate one or more perfume ingredients selected from (D) 3-octanol, 3-octyl acetate, 3-octanone and fencone. When the component (D) is mixed with the component (C), the effect of improving the unpleasant taste is enhanced, and the aftertaste of the unpleasant taste can be further improved. Even with octanol, general 1-octanol as a flavoring agent for a dentifrice composition can not satisfactorily satisfy the object of improving the unpleasant taste. As the component (D), commercially available products can be used. For example, 3-octanol may be manufactured by Shiono Perfume Co., Ltd., 3-octyl acetate and 3-octanone may be manufactured by Inoue Flavor Manufacture Co., Ltd., and Pencon may be manufactured by Koei Kogyo Co., .

The blending amount of the component (D) is preferably 0.0001 to 0.1%, more preferably 0.0001 to 0.05%. If it is 0.0001% or more, the effect of improving the unpleasant taste is sufficiently improved. If it is less than 0.1%, the unpleasant taste of the component (D) itself can be sufficiently prevented from being expressed. The total amount of the component (D) is preferably within the above range, and each component can be compounded within this range.

The oral composition of the present invention is particularly preferably prepared as a dentifrice such as a continuous skirt, a liquid skirt, a skimmed skirt, especially a continuous skirt, or a mouthwash. Further, in addition to the above-mentioned essential components, other known additives, which are given as optional ingredients in accordance with the formulation and the like, may be compounded in such a range as not to interfere with the effect of the present invention. For example, in the case of a continuous skirt, a sweetener, an antiseptic, an effective ingredient, a coloring agent, a perfume, and the like may be blended in accordance with an abrasive, a tackifier, a binder, a surfactant, ≪ / RTI > In the case of a detergent, a sweetening agent, a preservative, a coloring agent, a flavoring agent, an effective ingredient, and the like may be compounded in accordance with a viscous agent, a binder, a surfactant, and furthermore, a necessity.

Examples of the abrasive include silica-based abrasives such as silicic anhydride, silica gel, aluminosilicate, and zirconosilicate, calcium secondary diborate dihydrate, calcium secondary diborate anhydride, calcium tertiary phosphate, calcium diphosphate, Magnesium carbonate, magnesium carbonate, zeolite, zirconium silicate, zirconium silicate, zirconium silicate, zirconium silicate, zirconium silicate, zirconium silicate, zirconium silicate, zirconium silicate, zirconium silicate, zirconium silicate, Hydroxyapatite, fluoroapatite, calcium-deficient apatite, and synthetic resin-based abrasive (blended amount is usually 2 to 50%, particularly 10 to 40%).

Examples of the viscosifier include glycerin, propylene glycol, sugar alcohols such as polyethylene glycol, an ethylene glycol and other polyhydric alcohols having a molecular weight of 200 to 6,000 and an average molecular weight of 200 to 6,000, and sorbit, One or more of these may be used (the blending amount is usually 5 to 70%).

Examples of the viscous liquid include those other than cationic cellulose such as sodium polyacrylate, xanthan gum, sodium alginate, propylene glycol alginate, sodium carboxymethyl cellulose, hydroxyethyl cellulose, carbopol, guar gum, gelatin, Organic montmorillonite, montmorillonite, kaolin, and bentonite (the blending amount is usually 0 to 10%).

Examples of the surfactant include amphoteric surfactants such as sodium lauryl sulfate, lauroyl sarcosine sodium, polyoxyethylene alkyl sulfate, N-lauroyl taurine salt and? -Olefin sulfonate, N-acyl glutamate, 2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine, and palm oil fatty acid amide propyl betaine. Examples of the nonionic surfactant include alkyl glycosides, sucrose fatty acid esters, Polyoxyethylene sorbitan monostearate, polyoxyethylene polyoxypropylene glycol, polyoxyethylene alkyl ether, lauric acid decaglyceryl, and polyoxyethylene hydrogenated castor oil (the amount of the compound is usually 0.01 to 10 parts by weight, 0.1 to 5%).

Examples of the sweetening agent include paraffin (paroxybenzoic acid ester) such as saccharin, aspartame, stevioside, stevia extract, paramethoxycinnamic aldehyde, neoheperidin dihydrochalcone, perylate, and preservatives such as ethylparaben, butylparaben, , And sodium benzoate. Examples of the colorant include blue No. 1, yellow No. 4, and green No. 3.

In addition to the component (D), the perfume can be blended with any other perfume ingredient common for other dentifrice compositions. As the perfume, perfumes containing at least menthol and / or carboxy are preferable, and they are preferably contained in the composition in the range of 0.01 to 1%.

Examples of the effective ingredient include those other than tranexamic acid, for example, fluorides such as sodium fluoride, potassium fluoride, 1 tin fluoride, strontium fluoride, and sodium monofluorophosphate; Soluble phosphoric acid compounds such as potassium salts and sodium salts of orthophosphoric acid; But are not limited to, epsilon-aminocaproic acid, allantoin chlorohydroxyammini, hinokin thiol, ascorbic acid, dl-tocopherol acetate, dihydrocholesterol, a-bisabolol, chlorhexidine salts, azulene, glycyrrhetin, glycyrrhetinic acid Or a chiral phosphate compound such as copper chlorophyllin sodium, chlorophyll, glycerophosphate and the like; Copper compounds such as copper gluconate; But are not limited to, sodium chloride, strontium chloride, potassium nitrate, hydroxamic acid or a derivative thereof, sodium tripolyphosphate, zeolite, methoxyethylene, epidihydrocholesterine, benzethonium chloride, dihydrocholesterol, trichlorocarbonylide, zinc citrate, zinc oxide, (Soft) extract, yellowish white extract, and furthermore, plant extracts such as camomile, sperm, rosemary, golden, and safflower. The blending amount of these effective ingredients can be an effective amount within a range not hindering the effect of the present invention.

The method for inhibiting discoloration of an oral composition of the present invention is a method for inhibiting discoloration of an oral composition comprising (C) a tea extract and (A) + ((A)) an antioxidant in an oral composition comprising (A) a tranexamic acid and B)] / (C) in a mass ratio of 0.5 to 200, and (B) / (C) in a mass ratio of 0.2 to 100. Further, the details of the compounding ingredients, the amount thereof, the amount ratio (amount ratio) and the like are the same as those described above.

[Example]

Hereinafter, examples and comparative examples will be shown and the present invention will be described in detail, but the present invention is not limited to the following examples. In the following examples,% represents mass% unless otherwise specified.

[Practical example, comparative example]

A skirt (skirt) or scouring agent having the compositions shown in Tables 1 to 5 was prepared by a routine method, and these were evaluated as the test composition by the following method. The results are listed in the table.

(1) Evaluation method of appearance stability (discoloration inhibiting effect)

The appearance of the test composition immediately after the preparation and the appearance after storage for 3 months under an environment of 50 캜 were visually confirmed by visual inspection, and on the basis of the following evaluation criteria, Respectively. ? Or? Was judged to be a test composition having good appearance stability without discoloration.

Evaluation standard :

◎: discoloration is not recognized

○: Discoloration is slightly recognized, but problem-free level

?: Discoloration is recognized

X: Discoloration was recognized remarkably.

(2) Evaluation method of unpleasant aftertaste (unpleasant taste improving effect)

The test composition was subjected to sensory evaluation by using a professional panelist 10 as a subject.

The dentifrice was prepared by extruding a dentifrice composition filled in a laminate tube onto a toothbrush and extruding the dentifrice composition onto the toothbrush for 3 minutes in the same manner as usual. The dentifrice was filled with about 10 ml for about 20 seconds, Respectively. The unpleasant taste remaining in the mouth after 10 minutes of use was evaluated based on the following rating criteria.

Rated by:

1 point: I feel very unpleasant taste.

2 points: I feel unpleasant taste

3 points: I feel a bit of an unpleasant taste, but it is a problem-free level

4 points: I do not feel any unpleasant taste at all

 The average value of the results of the evaluation by the 10 professional panelists was calculated and evaluated based on the following evaluation criteria.

, &Amp; cir &, and & cir & were secured, and it was judged that the test composition did not feel unpleasant aftertaste after use.

Evaluation standard :

☆: Average point 4 points

◎: Average point 3.5 points or more and less than 4.0 points

○: 3.0 points or more and less than 3.5 points

△: Average point of 2.0 points or more and less than 3.0 points

X: Average point is 1.0 or more and less than 2.0 point

Details of the raw materials used are shown below.

(A) Tranexamic acid: manufactured by Shimik CMO Co., Ltd.

(B) Cationic Cellulose:

Trade name: Cellcoat L-200, manufactured by Akzo Nobel Co., Ltd.

(C) Tea extract

Green tea extract, trade name " ism, " 0.2% extract, solvent: 50% butylene glycol aqueous solution,

(D) 3-octanoloxy perfume

(D) 3-octyl acetate: manufactured by Inoue Flavor Manufacture Co., Ltd.

(D) 3-Octanone: manufactured by Inoue Flavor Manufacture Co., Ltd.

(D) Pencon: manufactured by Koei Kogyo Co., Ltd. Also,

The composition of the perfume A used is as follows.

Composition of perfume A:

Carbon 20%

l-menthol 66

Methyl butanal 5

Citronellal 2

Perylaldehyde 2

Unsensual 1

Linalool 0.5

Orange oil 0.5

Ethanol 3

Total 100%

[Table 1]

*; (C) represents the net amount of tea extract (hereinafter the same).

[Table 2]

[Table 3]

[Table 4]

[Table 5]

Claims (7)

(A) Tranexamic acid,
(B) cationic cellulose and
(B) / (C) is in a mass ratio of 0.5 to 200, and (B) / (C) is in a mass ratio of 0.2 to 100, Composition. The method of claim 1, wherein
(B) the cationic cellulose is hydroxyethyl cellulose dimethyldiallylammonium chloride. The method according to claim 1 or 2, wherein
Wherein the composition contains 0.01 to 0.2 mass% of component (A), 0.01 to 0.2 mass% of component (B), and 0.0005 to 0.2 mass% of component (C) as pure pure extract. 4. The method according to any one of claims 1 to 3, wherein
Further, the composition for oral use is characterized by containing at least 0.0001 to 0.1 mass% of at least one selected from (D) 3-octanol, 3-octyl acetate, 3-octanone and ficcon. The method according to any one of claims 1 to 4, wherein
Wherein the oral composition is a cosmetic or dermatological agent. (A) + (B)] / (C) in a mass ratio of 0.5 to 200, and (B) / (C) in an oral composition containing (A) And (B) / (C) in a weight ratio of 0.2 to 100. The method of claim 6, wherein
(B) is contained in an amount of 0.01 to 0.2% by mass, and the component (C) is added in an amount of 0.0005 to 0.2% by mass as pure extract of the extract.