KR102531788B1 - Oral composition and method for inhibiting discoloration thereof - Google Patents

Abstract

Provided is an oral composition containing tranexamic acid that suppresses discoloration of formulations even after storage at a high temperature and provides excellent external appearance stability, and a method for suppressing discoloration thereof.
(A) contains tranexamic acid, (B) cationized cellulose, and (C) tea extract, [(A)+(B)]/(C) is 0.5 to 200 as a mass ratio, and further (B)/(C) ) is a composition for oral cavity characterized in that the mass ratio is 0.2 to 100, and (D) the composition for oral cavity containing at least one selected from 3-octanol, 3-octyl acetate, 3-octanone and pencon. And to the composition for oral cavity containing the above (A) and (B) components, (C) component is blended, and the mass ratio of [(A) + (B)] / (C) and (B) / (C) Discoloration suppression method of the said composition for oral cavity characterized by making mass ratio into the said range, respectively.

Description

Oral composition and method for inhibiting discoloration thereof {ORAL COMPOSITION AND METHOD FOR INHIBITING DISCOLORATION THEREOF}

The present invention relates to a composition for oral use containing tranexamic acid that suppresses discoloration of a formulation even after storage at a high temperature and has excellent external appearance stability, and a method for suppressing discoloration thereof.

Tranexamic acid is a functional component having an anti-inflammatory effect on the gums, and is blended into oral compositions as a periodontal disease preventive component (Patent Document 1; Japanese Unexamined Patent Publication No. 2009-149565), and tranexamic acid blended into dentifrice compositions It is proposed in Patent Document 2 (Japanese Patent Laid-Open No. 2001-226244) that hydroxyethyl cellulose-dimethyldiallylammonium salt achieves an effect in order to improve the retention in the oral cavity and improve the effect.

In addition, patent documents 3 and 4 (Japanese Unexamined Patent Publication Nos. 2008-143870 and 60-130509) suggest that tranexamic acid can be applied to improve the feeling of use of oral compositions.

However, tranexamic acid has a problem that it may cause discoloration of the formulation over time depending on the ingredients. Techniques for suppressing discoloration are proposed in Patent Documents 5 and 6 (Japanese Patent No. 4656299 and Japanese Patent No. 5842565), and in Patent Document 6, tranexamic acid and cinnamic aldehyde, which is a fragrance ingredient, are used in mouthwash. In order to suppress the discoloration of the formulation over time caused by blending together, a specific amount of sodium lauryl sulfate is blended to improve the external appearance stability.

Patent Document 1: Japanese Patent Laid-Open No. 2009-149565 Patent Document 2: Japanese Patent Laid-Open No. 2001-226244 Patent Document 3: Japanese Patent Laid-Open No. 2008-143870 Patent Document 4: Japanese Patent 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 an object of the present invention is to provide a composition for oral use containing tranexamic acid that suppresses discoloration of formulations even after storage at a high temperature and gives excellent external appearance stability, and a method for suppressing discoloration thereof.

As a result of intensive studies to achieve the above object, the inventors of the present invention have found that blending a tea extract in a specific ratio is effective for inhibiting discoloration of the formulation that occurs when tranexamic acid and cationized cellulose are blended into an oral composition. did That is, in the present invention, (A) a composition for oral cavity containing tranexamic acid and (B) cationized cellulose is blended with (C) tea extract, and [(A)+(B)]/(C) When the mass ratio and the mass ratio of (B)/(C) are within a specific range, discoloration of the formulation is suppressed even after storage at high temperature, excellent external appearance stability is given, and an unpleasant taste is suppressed to give a pleasant feeling of use. Oral composition It was found that it was possible to provide, and came to achieve the present invention.

More specifically, as described above, it is known that hydroxyethylcellulose-dimethyldiallylammonium salt of cationized cellulose is effective in improving the retention of tranexamic acid in the oral cavity in the dentifrice composition (Patent Document 2), When the present inventors blended (A) tranexamic acid with (B) cationized cellulose in combination to improve oral retention in a composition for oral cavity, browning occurs after storage at high temperature and the problem of discoloration of the formulation is In addition, it was also found that the discoloration of the formulation due to browning described above is not recognized when carboxymethylcellulose sodium is used even for a cellulose derivative, and is a unique problem that occurs when components (A) and (B) are used in combination. So, the inventors of the present invention, as a result of conducting examinations to solve these problems, when combining (C) component with the combined use system of (A) and (B) components, [(A) + (B)] / (C) Component (C) acts specifically within a specific range of the mass ratio of and the mass ratio of (B)/(C), so that discoloration of the formulation due to the combination system is suppressed, thereby preventing discoloration of the formulation even after storage at a high temperature. It was suppressed and could give excellent appearance stability. In this case, when components (A) and (B) are used together, a unique unpleasant taste may remain in the oral cavity after use. could be given

As is clear from the results of comparative examples described later, the action and effect of the present invention are [(A)+(B)]/(C) even when components (A), (B) and (C) are used in combination. ) and if either of the mass ratios of (B)/(C) is inappropriate, it will be inferior, and in place of the (C) component in (A) and (B) components, it has an antioxidant action similar to that of tea extract. When used in combination with licorice extract, which is a plant extract, it was inferior.

In addition, the dentifrice composition of Patent Document 2 contains tranexamic acid and an anionic surfactant together with hydroxyethylcellulose dimethyldiallylammonium salt, anethol, carbon, cineol, methyl salicylate, eugenol, It contains a specific flavor component selected from ethyl butyrate and cinnamic aldehyde, and the oral retention and storage stability (liquid separation) of tranexamic acid are improved. On the other hand, the composition for oral cavity containing the components (A), (B) and (C) of the present invention suppresses the discoloration of the preparation due to the component (A), even after storage at a high temperature, even if the above specific fragrance component is not contained. Excellent appearance stability (discoloration) and good taste.

Accordingly, the present invention provides the composition for oral cavity described below and a method for suppressing discoloration thereof.

[1] (A) tranexamic acid;

(B) cationized cellulose and

(C) contains tea extract, [(A)+(B)]/(C) is 0.5 to 200 as a mass ratio, and (B)/(C) is a mass ratio of 0.2 to 100, characterized in that for oral use composition.

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

[3] The oral cavity according to [1] or [2], containing 0.01 to 0.2% by mass of component (A), 0.01 to 0.2% by mass of component (B), and 0.0005 to 0.2% by mass of component (C) as pure extract. composition for.

[4] Further, (D) any one of [1] to [3], containing 0.0001 to 0.1% by mass of at least one selected from 3-octanol, 3-octyl acetate, 3-octanone, and pencon. Compositions for oral use.

[5] The composition for oral cavity according to any one of [1] to [4], which is a dentifrice or mouthwash.

[6] A composition for oral cavity containing (A) tranexamic acid and (B) cationized cellulose was mixed with (C) tea extract, and [(A) + (B)]/(C) was used as a mass ratio of 0.5 to 200, and (B)/(C) as a mass ratio of 0.2 to 100.

[7] The oral composition according to [6], comprising 0.01 to 0.2% by mass of component (A), 0.01 to 0.2% by mass of component (B), and 0.0005 to 0.2% by mass of component (C) as pure extract. Discoloration inhibition method of

According to the present invention, it is possible to provide an oral composition containing tranexamic acid that suppresses discoloration of the formulation even after storage at a high temperature, gives excellent external appearance stability, and suppresses an unpleasant taste to give a pleasant feeling of use. The composition for oral cavity of the present invention has good retention of tranexamic acid in the oral cavity and anti-inflammatory effect can be expected, so it is suitable for gum care for suppressing gingivitis.

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

(A) Tranexamic acid is an active ingredient and has an anti-inflammatory action. (A) The blending amount of tranexamic acid is preferably 0.01 to 0.2% (% by mass, the same applies below) of the total composition, and more preferably 0.03 to 0.1% in terms of anti-inflammatory effect and discoloration inhibition. Within this range, discoloration of the formulation is sufficiently suppressed, and unpleasant taste is sufficiently improved.

(B) Cationized cellulose has an effect of improving the retention of the component (A) in the oral cavity. (B) As cationized cellulose, what added dimethyldiallylammonium, 2-hydroxy-3 (trimethylammonio) propyl, etc. as a cation group to a cellulose derivative, etc. are mentioned. For example, hydroxyethyl cellulose dimethyl diallyl ammonium chloride, chloride O-[2-hydroxy-3-(trimethylammonio) propyl] hydroxyethyl cellulose, etc. are mentioned. The nitrogen content is preferably 0.1 to 3%, more preferably 0.5 to 2. 5%.

Specifically, hydroxyethyl cellulose dimethyl diallyl ammonium chloride is obtained by graft polymerization of dimethyl diallyl ammonium salt on hydroxyethyl cellulose, and has a viscosity of 10 to 3,000 mPa s in a 2% aqueous solution (BH type Brookfield viscometer , Rotor No. 2, 20 rotations, 21°C) can be used. For example, Celcoat L-200 manufactured by Akzo Nobel Co., Ltd. (viscosity of 2% aqueous solution: 35 to 350 mPa s, BH type Brookfield viscometer, rotor No. 2, 20 rotations, 21 ° C., measurement time 1 minute) , Cellcoat H-100 (viscosity of 2% aqueous solution: 500 to 2,750 mPa·s, BH type Brookfield viscometer, rotor No. 2, 20 rotations, 21° C., measurement time 1 minute); and the like.

In addition, the viscosity of O-[2-hydroxy-3-(trimethylammonio)propyl]hydroxyethyl cellulose chloride can be measured in 1% or 2% aqueous solution, and the viscosity of 1% aqueous solution is 500 to 2,600 mPa.・s (BH type Brookfield viscometer, rotor No. 2, 20 rotations, 25° C.), or a 2% aqueous solution having a viscosity of 5 to 800 mPa s (BL type viscometer, rotor No. 2, 30 rotations, 25° C.) can be used. For example, Leoguard KGP (2% aqueous solution viscosity: 5 to 50 mPa s) manufactured by Lion Co., Ltd., Leoguard G (2% aqueous solution viscosity: 100 to 600 mPa s), Leoguard GP (2% aqueous solution viscosity : 100 to 600 mPa s), Leoguard LP (2% aqueous solution viscosity: 300 to 800 mPa s), Lion Co., Ltd. Leoguard MGP (1% aqueous solution viscosity: 500 to 1,200 mPa s), Leo Guard mlP (viscosity of 1% aqueous solution: 1,000 to 2,600 mPa·s); and the like.

Among these cationized celluloses, hydroxyethyl cellulose dimethyl diallyl ammonium chloride (A) is preferable from the viewpoint of retention tendency of tranexamic acid in the oral cavity.

(B) The blending amount of cationized cellulose is preferably 0.01 to 0.2%, more preferably 0.03 to 0.1% of the total composition, from the viewpoint of the effect of suppressing discoloration of the formulation and unpleasant taste. Within this range, discoloration of the formulation is sufficiently suppressed, and unpleasant taste is sufficiently improved. When it exceeds 0.2%, the unpleasant taste by itself becomes strong, and the improvement effect of an unpleasant taste may not fully be acquired.

In the present invention, (C) tea extract acts as an inhibitor of discoloration of formulations and also acts as an unpleasant taste improver.

C) As tea extract, a commercial product or one obtained by a known method can be used. Specifically, green tea can be used as the raw material. A hydrophilic solvent may be used as the extraction solvent, and hydrophilic solvents such as water, lower monohydric alcohols such as ethanol and propanol, and polyhydric alcohols such as 1,3-butylene glycol and propylene glycol may be used. One single solvent or two or more mixed solvents may be used. Extraction conditions and post-processing can employ conventional methods.

As a commercial product, green tea extract (trade name "Hwaism", extract content 0.2%, solvent: 50% butylene glycol aqueous solution, manufactured by Maruzen Pharmaceutical Co., Ltd.) can be used.

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

In the present invention, [(A) + (B)] / (C), which represents the ratio between the blending amount of components (A) and (B) and the blending amount of component (C) (pure amount of extract excluding the solvent), is a mass ratio It is 0.5-200, Preferably it is 1-100. If the mass ratio of [(A) + (B)]/(C) is less than 0.5, the feeling of use is impaired due to the taste of the component (C) itself, and if it exceeds 200, the effect of suppressing discoloration of the formulation and the improvement of unpleasant taste falls behind

In addition, (B)/(C), which represents the ratio between the compounding amount of component (B) and the compounding amount of component (C) (pure amount of extract excluding the solvent), is 0.2 to 100 as a mass ratio, preferably 0.5 to 50 am. (B) When the mass ratio of /(C) is less than 0.2, the feeling of use is impaired by the taste of the component (C) itself. When 100 is exceeded, the improvement effect of an unpleasant taste is inferior.

In the present invention, it is also preferable to blend (D) one or two or more flavor components selected from 3-octanol, 3-octyl acetate, 3-octanone and pencon. When (D)component is mix|blended with (C)component, the improvement effect of an unpleasant taste will increase, and the unpleasant aftertaste can be improved more. In addition, even if it is octanol, 1-octanol which is common as a flavoring agent for a dentifrice composition cannot satisfactorily obtain the target unpleasant taste improvement effect. (D) A commercial item can be used for component. For example, 3-octanol is manufactured by Shiono Fragrance Co., Ltd., 3-octyl acetate and 3-octanone are manufactured by Inoue Fragrance Manufacturing Co., Ltd., and pencon is manufactured by Koei Hungup Co., Ltd. .

(D) The blending amount of component is preferably 0.0001 to 0.1%, more preferably 0.0001 to 0.05%. When it is 0.0001% or more, the improvement effect of unpleasant taste is sufficiently improved. If it is 0.1% or less, expression of the unpleasant taste of (D) component itself can fully be prevented. It is preferable that the total compounding amount of (D)component is within the said range, and each component can be mix|blended within this range.

The composition for oral cavity of the present invention is preferably prepared as a dentifrice such as a soft skirt, a liquid skirt, or a polished skirt, particularly a soft skirt, or a mouthwash. In addition to the above essential components, other known additives may be incorporated as optional components within a range that does not interfere with the effects of the present invention. For example, in the case of a soft skirt, an abrasive, a viscous agent, a binder, a surfactant, and furthermore, a sweetener, an antiseptic, an active ingredient, a colorant, a fragrance, etc. can be mixed as needed. can be produced in this way. In the case of mouthwash, viscous agents, binders, surfactants, and furthermore, sweeteners, preservatives, colorants, fragrances, active ingredients and the like can be blended as needed.

Examples of the abrasive include silica-based abrasives such as anhydrous silicic acid, silica gel, aluminosilicate, and zirconosilicate, dibasic calcium phosphate dihydrate, dibasic calcium phosphate anhydrate, tricalcium phosphate, quaternary calcium phosphate, octacalcium phosphate, Calcium pyrophosphate, aluminum hydroxide, alumina, titanium dioxide, crystalline zirconium silicate, polymethyl methacrylate, insoluble calcium metaphosphate, light calcium carbonate, heavy calcium carbonate, magnesium carbonate, tribasic magnesium phosphate, zeolite, zirconium silicate, hydroxyapatite, fluoroapatite, calcium-deficient apatite, and synthetic resin-based abrasives (the compounding amount is usually 2 to 50%, particularly 10 to 40%).

Examples of the viscous agent include polyhydric alcohols such as glycerin, propylene glycol, polyethylene glycol having an average molecular weight of 200 to 6,000 (average molecular weight as described in Quasi-Drug Ingredients Standards 2006), ethylene glycol, and sugar alcohols such as sorbitol and reduced starch saccharide. These 1 type, or 2 or more types can be used (the compounding amount is 5 to 70% normally).

Examples of binders other than cationized cellulose include sodium polyacrylate, xanthan gum, sodium alginate, propylene glycol alginate, carboxymethyl cellulose sodium, hydroxyethyl cellulose, carbopol, guar gum, gelatin, Avicel, etc. and inorganic binders such as montmorillonite, kaolin, and bentonite.

The surfactant is an anionic surfactant, for example, sodium lauryl sulfate, sodium lauroyl sarcosine, polyoxyethylene alkyl sulfate, N-lauroyl taurine salt, α-olefin sulfonate, etc., as an amphoteric surfactant, for example Examples of nonionic surfactants such as N-acylglutamate, 2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine, and coconut oil fatty acid amide propyl betaine include alkylglycosides, sucrose fatty acid esters, Alkylolamide, polyoxyethylene sorbitan monostearate, polyoxyethylene polyoxypropylene glycol, polyoxyethylene alkyl ether, decaglyceryl laurate, polyoxyethylene hydrogenated castor oil, etc. (the mixing amount is usually, 0.1-5%).

Examples of sweeteners include saccharinthium, aspartame, stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidindihydrochalcone, perilartine, and preservatives, parabens such as ethylparaben and butylparaben (para-hydroxybenzoate). , sodium benzoate. As a coloring agent, Blue No. 1, Yellow No. 4, and Green No. 3 are illustrated.

In addition to the component (D), the fragrance can contain any general fragrance component for other dentifrice compositions. As the fragrance, a fragrance containing at least menthol and/or carbon is preferable, and it is preferable to contain these in the range of 0.01 to 1% in the composition.

Examples of the active ingredient include fluorides other than tranexamic acid, such as sodium fluoride, potassium fluoride, stannous fluoride, strontium fluoride, and sodium monofluorophosphate; water-soluble phosphoric acid compounds such as potassium salt and sodium salt of orthophosphoric acid; Epsilon-aminocaproic acid, allantoin chlorhydroxyaluminium, hinogitiol, ascorbic acid, dl-tocopherol acetate, dihydrocholesterol, α-bisabolol, chlorhexidine salts, azulene, glycyrrhetin, glycyrrhetinic acid chelating phosphoric acid compounds such as sodium copper chlorophyllin, chlorophyll, and glycerophosphate; copper compounds such as copper gluconate; Strontium chloride, potassium nitrate, hydroxamic acid or its derivatives, sodium tripolyphosphate, zeolite, methoxyethylene, epidihydrocholesterin, benzethonium chloride, dihydrocholesterol, trichlorocarbanilide, zinc citrate, zinc oxide, sugar cane and plant extracts such as chamomile, sperm, rosemary, gold, and safflower. In addition, the compounding quantity of these active ingredients can be made into an effective amount within the range which does not impede the effect of this invention.

Further, the method for inhibiting discoloration of the composition for oral cavity of the present invention is to mix (C) tea extract with a composition for oral cavity in which (A) tranexamic acid and (B) cationized cellulose are blended, [(A)+( B)]/(C) as a mass ratio of 0.5 to 200, and (B)/(C) as a mass ratio of 0.2 to 100. In addition, details, such as a compounding component, its compounding quantity, and quantity ratio, are the same as those mentioned 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. Incidentally, in the following examples, all percentages represent mass % unless otherwise specified.

[Examples, comparative examples]

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

(1) Evaluation method for appearance stability (discoloration inhibitory effect)

The dentifrice of the test composition was filled in a laminate tube and the dentifrice was filled in a plastic bottle, and the appearance immediately after manufacture and the appearance after storage for 3 months in a 50 ° C environment were visually checked, respectively, and based on the following evaluation criteria, regarding discoloration evaluated. What secured evaluation of ○ or ◎ was judged to be a test composition with good external appearance stability in which discoloration was not recognized.

Evaluation standard :

◎: Discoloration is not recognized

○: Slight discoloration is recognized, but it is a problem-free level

△: Discoloration is recognized

x: Discoloration is recognized notably.

(2) Evaluation method for no unpleasant aftertaste (unpleasant taste improvement effect)

The test composition was sensory evaluated using 10 expert panelists as subjects.

For the dentifrice, about 1 g of the dentifrice composition filled in the laminate tube is extruded on the toothbrush, brushed teeth in the same way as usual for 3 minutes, and the mouthwash is about 10 ml for about 20 seconds. and used it. The unpleasant taste remaining in the mouth after 10 minutes of use was evaluated based on the following rating criteria.

Rating by:

1 point: Very unpleasant taste

2 points: unpleasant taste

3 points: I feel a little unpleasant taste, but it is at a level that is not a problem.

4 points: I do not feel any unpleasant taste

A value obtained by averaging the evaluation results of 10 professional panelists was calculated and evaluated based on the following evaluation criteria.

It was judged that what the evaluation of ☆, ◎, and ○ was secured was a test composition in which an unpleasant aftertaste was not felt after use.

Evaluation standard :

☆ : average score of 4 points

◎: average score of 3.5 or more and less than 4.0

○: Average score of 3.0 or more and less than 3.5

△: Average score of 2.0 or more and less than 3.0

×: average score of 1.0 or more and less than 2.0

Details of the raw materials used are shown below.

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

(B) cationized cellulose:

Product Name: Cellcoat L-200, manufactured by Akzo Nobel Co., Ltd.

(C) tea extract

Green tea extract, trade name "Waism", extract content 0.2%, solvent: 50% butylene glycol aqueous solution, manufactured by Maruzen Pharmaceutical Co., Ltd.

(D) 3-octanol Shiono Fragrance Co., Ltd. product

(D) 3-octyl acetate: manufactured by Inoue Fragrance Manufacturing Co., Ltd.

(D) 3-octanone: manufactured by Inoue Fragrance Manufacturing Co., Ltd.

(D) Pencon: manufactured by Koei Heung-up Co., Ltd. Also,

The composition of the used spice A is as follows.

Composition of perfume A:

Carbon 20%

l-menthol 66

Methylbutanal 5

Citroneral 2

Perylaldehyde 2

undecenal 1

Linalool 0.5

Orange oil 0.5

ethanol 3

Total 100%

[Table 1]

* ; (C) The compounding quantity of a component shows the pure quantity of tea extract (it is the same hereafter).

[Table 2]

[Table 3]

[Table 4]

[Table 5]

Claims (7)

(A) tranexamic acid;
(B) cationized cellulose and
(C) contains tea extract, which is a hydrophilic solvent extract of green tea, wherein [(A) + (B)]/(C) is a mass ratio of 0.5 to 200, and (B)/(C) is a mass ratio of 0.2 to 100 Oral composition, characterized in that. According to claim 1,
(B) A composition for oral cavity characterized in that the cationized cellulose is hydroxyethyl cellulose dimethyldiallylammonium chloride. According to claim 1 or 2,
The composition for oral cavity characterized by containing 0.01-0.2 mass % of (A) component, 0.01-0.2 mass % of (B) component, and 0.0005-0.2 mass % of (C) component as an extract pure content remove|excluding solvent. According to claim 1 or 2,
Further, (D) a composition for oral cavity characterized by containing 0.0001 to 0.1% by mass of at least one selected from 3-octanol, 3-octyl acetate, 3-octanone and pencon. According to claim 1 or 2,
Oral composition, characterized in that the dentifrice or mouthwash. [(A)+(B)]/(C) 0.5 to 200 as mass ratio, and (B)/(C) to 0.2 to 100 as mass ratio, characterized in that the method for suppressing discoloration of the composition for oral cavity. According to claim 6,
0.01 to 0.2% by mass of component (A), 0.01 to 0.2% by mass of component (B), and 0.0005 to 0.2% by mass of component (C) as pure extract excluding the solvent. suppression method.