JP2017007992A - Composition for oral cavity and method for improving bactericidal activity thereof - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a composition for oral cavity containing benzalkonium chloride which improves bactericidal activity against pathogenic bacteria in the oral cavity, exhibits an excellent foul breath inhibiting effect, and has a suppressed bitter taste and also has good use feeling, and to provide a method for improving bactericidal activity of the composition.SOLUTION: The composition for oral cavity, in which (C) ascorbic acid phosphate or a salt thereof is formulated with the composition for oral cavity containing (A) benzalkonium chloride and (B) sodium lauroylsarcosine, and a method for improving bactericidal activity of the composition for oral cavity, in which the component (C) is formulated with the composition for oral cavity containing the component (A) and the component (B).SELECTED DRAWING: None

Description

  The present invention improves the bactericidal power against pathogenic bacteria in the oral cavity, has an excellent halitosis suppression effect, has a bitter taste suppressed, and has a good feeling of use, and an oral composition containing benzalkonium chloride and its bactericidal effect It relates to a method for improving power

  Among the medicinal ingredients used in oral care, cationic fungicides have good retention in the oral cavity, give high bactericidal power, and are attracting attention as a bad breath prevention ingredient, but as a cationic fungicide, Cetylpyridinium chloride and the like were used in terms of bactericidal power and taste, and the use of benzalkonium chloride was limited. This benzalkonium chloride has a drawback of relatively strong bitterness.

  Patent Document 1 discloses that the bitterness derived from a cationic fungicide is reduced by blending polyglutamic acid or a salt thereof and an acyl sarcosine salt in a cationic fungicide, and has an effect of suppressing bad breath and dry mouth. An excellent oral composition is proposed, and a mouthwash containing benzalkonium chloride is described as an example, but cetylpyridinium chloride and acyl sarcosine salt of Comparative Example 2 are blended, and polyglutamic acid or a salt thereof is added. The mouthwash that does not contain has a strong bitter taste.

  On the other hand, various techniques for blending an ascorbic acid derivative such as ascorbic acid phosphate with an oral composition and effectively imparting the effectiveness thereof have been proposed and disclosed in Patent Documents 2 to 4, etc. Does not mention improvement in bitterness of benzalkonium chloride.

JP 2012-201607 A JP2013-129601A JP 2009-149565 A JP 2013-256466 A

  Therefore, it has been desired to develop a technique for solving the problem of bactericidal power and bitterness of benzalkonium chloride and applying it to an oral composition more effectively.

  The present invention has been made in view of the above circumstances, has improved bactericidal power against pathogenic bacteria in the oral cavity, has an excellent halitosis suppression effect, has a reduced bitterness, and has a good feeling of use. It aims at providing the composition for oral cavity containing, and its bactericidal power improvement method.

  As a result of intensive studies to achieve the above object, the inventor of the present invention has (C) ascorbic acid phosphate ester or (C) ascorbic acid phosphate ester or (B) an oral composition containing sodium lauroyl sarcosine. When the salt is added, the bactericidal power against pathogenic bacteria in the oral cavity is improved, an excellent halitosis suppression effect is achieved, and the bitterness is reduced to give a good feeling of use. It was discovered that a product was obtained, and the present invention was made.

More specifically, in order to improve the bactericidal power of benzalkonium chloride, when combined with an anionic surfactant lauroyl sarcosine sodium having a bactericidal power in an oral composition, particularly a dentifrice such as a toothpaste. Although the bactericidal power is considered to be improved, the combined use of both components reduces the bactericidal power, making it impossible to disinfect pathogenic bacteria in the oral cavity. In addition, the bitterness derived from benzalkonium chloride, which is originally bitter. A new problem has arisen that is more strongly expressed and is not suitable for use. Then, when further examination was advanced in order to eliminate such a subject, when (C) ascorbic acid phosphate ester or its salt was mix | blended with the combined use system of (A) component and (B) component, the above-mentioned unexpectedly, The problem is also solved and the bactericidal power against pathogenic bacteria in the oral cavity is improved, and in particular, the high bactericidal power that significantly reduces the number of floating bacteria in the oral cavity such as Polyphyromonas gingivalis, (A) or (B) The effect of suppressing halitosis beyond that of single use was enhanced, the bitterness was suppressed, the taste was remarkably improved, and a preparation suitable for use could be obtained. In the present invention, the (C) component ascorbic acid phosphate ester or a salt thereof specifically acts to effectively suppress the coupling reaction of the (A) and (B) components. It is speculated that it will give a good effect.
In Patent Document 1, the bitterness of a cationic fungicide is reduced by a combined system of polyglutamic acid or a salt thereof and an acyl sarcosine salt, and as shown in Comparative Example 2, the cationic fungicide is chlorinated. Even if cetylpyridinium and an acyl sarcosine salt are blended, a mouthwash that does not contain polyglutamic acid or a salt thereof has a strong bitter taste. Furthermore, Patent Document 1 does not mention anything about blending of ascorbic acid phosphate ester or a salt thereof. From this patent document 1, it cannot be predicted that ascorbic acid phosphate or a salt thereof improves the bactericidal power of benzalkonium chloride and suppresses bitterness.

Accordingly, the present invention provides the following oral composition and method for improving the bactericidal power thereof.
[1] An oral composition comprising (C) ascorbic acid phosphate or a salt thereof in an oral composition containing (A) benzalkonium chloride and (B) sodium lauroyl sarcosine.
[2] Improving the bactericidal activity of the oral composition comprising (C) ascorbic acid phosphate or a salt thereof in an oral composition containing (A) benzalkonium chloride and (B) sodium lauroyl sarcosine Method.

  According to the present invention, the bactericidal power against pathogenic bacteria in the oral cavity is improved, an excellent halitosis suppression effect is achieved, the bitterness is suppressed and the usability is good, and the oral composition containing benzalkonium chloride and A method for improving the sterilizing power can be provided.

  The composition for oral cavity of this invention contains (A) benzalkonium chloride, (B) lauroyl sarcosine sodium, (C) ascorbic acid phosphate ester or its salt.

  The blending amount of the component (A) benzalkonium chloride is preferably 0.005 to 0.1% (mass%, the same applies hereinafter) of the entire composition, more preferably 0.006 to 0.05%. . When the blending amount is 0.005% or more, a sufficient bactericidal effect can be given, but 0.1% or less is suitable for preventing the bitterness from becoming strong and preventing the deterioration of usability. is there.

  (B) 0.05 to 2% of the whole composition is preferable, and, as for the compounding quantity of lauroyl sarcosine sodium of a component, More preferably, it is 0.1 to 1%, More preferably, it is 0.1 to 0.9%. If the blending amount is 0.05% or more, a sufficient bactericidal effect can be given, but 2% or less is suitable for suppressing bitterness, and also suppresses mucous membrane irritation and provides a feeling of use. It is also suitable for preventing adverse effects.

  (C) Ascorbic acid phosphate of component (C) or a salt thereof, ascorbic acid phosphate is phosphoric acid or polyphosphoric acid in which one or two or more hydroxyl groups at positions 2, 3, 5, and 6 of ascorbic acid are phosphoric acid. For example, ascorbic acid-2-phosphate ester, ascorbic acid-3-phosphate ester, ascorbic acid-6-phosphate ester, ascorbic acid-2-polyphosphorus And acid esters, ascorbic acid-2-sulfate, and the like. Examples of the salts include alkali metal salts such as sodium salt, potassium salt, calcium salt, and magnesium salt, and alkaline earth metal salts. Of these, magnesium salts and sodium salts of ascorbic acid phosphate are more preferable from the viewpoint of prevention of gingivitis, as well as those used for the oral cavity.

  The blending amount of ascorbic acid phosphate or a salt thereof is preferably 0.1 to 2% of the entire composition, more preferably 0.2 to 1%, and still more preferably 0.2 to 0.5%. is there. When it is 0.1% or more, the bactericidal power and the bad breath suppression effect are sufficiently improved, and the bitterness can be effectively reduced. 2% or less is suitable for preventing deterioration of taste due to discoloration or unique bitterness.

In the present invention, when the (C) component is combined in an appropriate ratio with the combined system of the (A) and (B) components, a more excellent effect can be imparted.
In this case, ((A) + (B)) / (C) indicating the ratio of the total amount of component (A) and component (B) to the amount of component (C) is 0.1 as the mass ratio. It is preferable that it is -15, More preferably, it is 0.1-7, More preferably, it is 0.2-0.9. Within this range, the bactericidal power and bad breath suppression effect are more excellent, and the bitterness can be further suppressed.

  The composition for oral cavity of the present invention is suitable as a toothpaste such as a toothpaste, a liquid toothpaste, and a toothpaste, a mouthwash, etc., and particularly as a toothpaste, and can be prepared by a usual method. Further, in the composition of the present invention, other known components in addition to the above components can be blended according to the dosage form, if necessary, as long as the effects of the present invention are not hindered. For example, abrasives, thickeners, binders, surfactants, and, if necessary, colorants, sweeteners, preservatives, fragrances, pH adjusters, active ingredients, and the like are added to dentifrices such as toothpastes. be able to.

As abrasives, silica-based abrasives such as silica gel, precipitated silica, aluminosilicate, zirconosilicate, calcium-based abrasives such as calcium pyrophosphate and calcium carbonate, aluminum hydroxide, alumina, magnesium carbonate, tribasic magnesium phosphate, Zeolite, zirconium silicate, hydroxyapatite, various synthetic resin-based abrasives and the like can be mentioned, among which silica-based abrasives are preferable. The blending amount of the abrasive is preferably 5 to 50%, particularly preferably 5 to 30%.
In the present invention, the silica-based abrasive is preferably the main abrasive, and when an abrasive species other than the silica-based abrasive, for example, a calcium-based abrasive, aluminum hydroxide or the like is selected as the main abrasive. In some cases, ascorbic acid phosphate or a salt thereof cannot be blended stably due to the influence of metal ions derived from the abrasive, and the bactericidal power cannot be sufficiently improved.

  Examples of the thickening agent include polyhydric alcohols such as propylene glycol, ethylene glycol, 1,3-butylene glycol, and glycerin, reduced starch saccharified products, sugar alcohols such as sorbitol, xylitol, and erythritol. The blending amount of the thickener is usually 0.1 to 50%, particularly 0.1 to 30%.

  As binder, cellulose binder such as sodium carboxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, methyl cellulose, cationized cellulose, etc. as organic binder, gums such as carrageenan, xanthan gum, guar gum, sodium alginate, gelatin, Examples of sodium polyacrylate and inorganic binder include gelling silica, gelling aluminum silica, and montmorillonite. The compounding amount of the binder is usually 0.1 to 6%, particularly 0.1 to 3%.

As the surfactant, anionic surfactants other than lauroyl sarcosine sodium, cationic surfactants, nonionic surfactants, and amphoteric surfactants can be used. Specifically, those shown below can be blended. .
Anionic surfactant: alkyl sulfates such as sodium lauryl sulfate and sodium myristyl sulfate, sodium N-myristol sarcosine, sodium lauroylmethyl taurate, sodium dodecylbenzenesulfonate, hydrogenated coconut fatty acid monoglyceride sodium monosulfate, sodium lauryl sulfoacetate N-acyl glutamate such as sodium N-palmitoyl glutamate, sodium α-olefin sulfonate, sodium N-methyl-N-acylalanine Cationic surfactant: distearylmethylammonium chloride, stearyldimethylbenzylammonium chloride Nonionic Surfactant: Sugar alcohol fat such as sorbitan fatty acid ester, polyoxyethylene sorbitan fatty acid ester, sucrose fatty acid ester Acid ester, glycerin fatty acid ester, polyglycerin fatty acid ester, polyoxyethylene glycerin fatty acid ester, polyhydric alcohol fatty acid ester such as polyethylene glycol fatty acid ester, polyoxyethylene alkyl ether, polyoxyethylene polyoxypropylene copolymer, polyoxyethylene Ether type or ester type surfactants such as alkylphenyl ether, polyoxyethylene hydrogenated castor oil, fatty acid alkanolamides such as lauric acid diethanolamide Amphoteric surfactant: 2-alkyl-N-carboxymethyl-N-hydroxyethylimidazo Betaine surfactants such as sodium betaine, sodium N-alkyl-1-hydroxyethylimidazoline betaine, N-lauryldiaminoethylglycine, N -N-alkyldiaminoethylglycine such as myristyldiaminoethylglycine The blending amount of the surfactant is usually 0.1 to 10%, particularly preferably 0.1 to 5%.

Examples of the colorant include legal pigments such as Blue No. 1, Blue No. 4, and Green No. 3, natural pigments such as caramel, and titanium oxide.
Examples of the sweetener include saccharin sodium, aspartame, stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidyl dihydrochalcone, and perilartin.
Examples of the preservative include paraoxybenzoic acid ester, benzoic acid or a salt thereof.

  As a fragrance | flavor, the fragrance | flavor component generally used for the composition for oral cavity can be used. For example, menthol, anethole, carvone, eugenol, limonene, n-decyl alcohol, citronellol, α-terpineol, citronellyl acetate, cineol, linalool, ethyl linalool, vanillin, thymol, spearmint oil, peppermint oil, lemon oil, orange oil, Sage oil, rosemary oil, cinnamon oil, pimento oil, cinnamon oil, perilla oil, winter green oil, clove oil, eucalyptus oil and the like.

  Examples of the pH adjuster include organic compounds such as citric acid, lactic acid, and malic acid and salts thereof, and inorganic compounds such as hydrochloric acid, sodium hydroxide, potassium hydroxide, disodium hydrogen phosphate, and sodium dihydrogen phosphate.

  Active ingredients include enzymes such as dextranase, amylase, protease and mutanase, alkali metal monofluorophosphates such as sodium monofluorophosphate, fluorides such as sodium fluoride and stannous fluoride, tranexamic acid, aluminum Chlorhydroxy allantoin, azulene, glycyrrhizinate, glycyrrhetinic acid, sodium chloride, vitamins and other anti-inflammatory agents, triclosan, hinokitiol, lysozyme chloride and other antibacterial agents, polyphosphates and other anticalculus agents, polyvinyl pyrrolidone and other tobacco removal And amino acids such as glycine and proline.

  EXAMPLES Hereinafter, although an Example and a comparative example are 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]
Oral compositions (toothpaste) having the compositions shown in Tables 1 to 3 were prepared by a conventional method and evaluated by the following methods. The results are shown in the table.

(1) Evaluation of bad breath suppression effect The bad breath was evaluated with the following method with respect to the adult who is worried about bad breath, and the person whose intensity of bad breath was 2 to 3 points was selected as a subject. Subjects were divided so that the average of bad breath scores was almost the same value (5 people in each group). The test subject used about 1 g of the composition for oral cavity, and evaluated bad breath again after oral cleaning and stopping for 2 hours after eating and drinking.
Evaluation method of bad breath The professional evaluator made a sensory evaluation on the bad breath strength of 1 liter of breath collected in a Tedora bag according to the following criteria.
Score standard 0 points: No bad breath 1 point: Slight bad breath 2 points: Bad breath 3 points: Remarkable bad breath

Furthermore, the bad breath improvement degree was calculated | required by the following formula, and the bad breath suppression effect was calculated | required by the following criterion. In addition, a bad breath intensity average value is the value which averaged the bad breath intensity of the test subject of each group.
<Calculation formula of bad breath improvement>
(Degree of bad breath improvement) = (Average value of bad breath before test start)-(Average bad breath intensity after test)

Judgment criteria for bad breath suppression effect ◎: The bad breath improvement degree is 1.5 points or more, and there is a remarkable effect. ○: The bad breath improvement degree is 1.0 point or more and less than 1.5 points, and there is an effect. : Bad breath improvement degree was 0.5 point or more and less than 1.0 point, and there was a little effect ×: Bad breath improvement degree was less than 0.5 point and there was no effect

(2) Evaluation of bactericidal power against oral bacteria (flocculating bacteria) 10 g of the composition for oral cavity was measured, and a suspension obtained by adding artificial saliva (100 ml) and stirring until uniform was used as a sample solution. Todd Hewitt Bros (Nippon Becton Dickinson Co., Ltd.) with hemin (Wako Pure Chemical Industries, 500 μg / ml) and menadione (Wako Pure Chemicals, 100 μg / ml) added A bacterial suspension was prepared so that the pre-cultured Porphyromonas gingivalis strain ATCC33277 was 1 × 10 ⁹ cells / ml with physiological saline. The bacterial solution and sample solution were mixed at 1: 1 (volume ratio) and allowed to stand for 3 minutes. Thereafter, serial dilution was performed 10 times with physiological saline, and smeared on a blood agar plate using a spiral plater. As a control, a mixture of physiological saline and bacterial solution at 1: 1 (volume ratio) instead of the drug was used. The blood plate was cultured at 37 ° C. under anaerobic conditions (80 vol% nitrogen, 10 vol% carbon dioxide, 10 vol% hydrogen) for 5 days, and the number of colonies formed was counted. The oral bacteria sterilization test was performed with n = 5.
The bactericidal power against airborne bacteria was evaluated from the average value of the number of colonies according to the following criteria.
Evaluation standard of bactericidal power ◎: Viable count decreased to less than 1/1000 compared to control ○: Viable count decreased to less than 1/100 to 1/1000 or more compared to control Δ: The number of viable cells decreased to less than 1/10 to 1/100 or more as compared with the control. ×: The number of viable cells did not decrease compared with the control or the number of viable cells was decreased to 1/10 or more.

(3) Evaluation of bitterness The bitterness of the composition for oral cavity was sensory-evaluated by the panel of five test subjects according to the following rating criteria. In addition, it evaluated by taking 1g of compositions for oral cavity on a toothbrush, and brushing for 3 minutes. The bitterness was evaluated from the average of 5 persons based on the following evaluation criteria.
Bitterness score 5 points: No bitterness 4 points: Very slightly bitterness 3 points: Somewhat bitterness 2 points: Bitterness 1 point: Strong bitterness Bitterness evaluation criteria ◎: Average value 4 ≥: 5 points or less ○: Average value of 3 points or more and less than 4 points △: Average value of 2 points or more and less than 3 points ×: Average value of 1 point or more and less than 2 points

  A prescription example is shown below.

[Formulation Example 1] Mouthwash (A) Benzalkonium chloride 0.01
(B) Lauroyl sarcosine sodium 0.2
(C) Ascorbic acid-2-phosphate magnesium 0.3
Polyoxyethylene (60) hydrogenated castor oil 0.5
Propylene glycol 3
Glycerin 4.5
Xylitol 3
Ethanol 2
Citric acid 0.07
Sodium citrate 0.25
Saccharin sodium 0.004
Fragrance 0.2
Purified water balance
Total 100.0%
((A) + (B)) / (C) = 0.7

[Prescription Example 2] Toothpaste (A) Benzalkonium chloride 0.01
(B) Lauroyl sarcosine sodium 0.2
(C) Ascorbic acid-2-phosphate magnesium 0.3
Silicic anhydride 18
70% sorbit solution 50
Saccharin sodium 0.2
Sodium monofluorophosphate 0.73
Sodium lauryl sulfate 1.4
Propylene glycol 3
Sodium carboxymethylcellulose 1
Carrageenan 0.4
Sodium hydroxide 0.1
Citric acid 0.1
Fragrance 0.8
Purified water balance
Total 100.0%
((A) + (B)) / (C) = 0.7

Claims (6)

  An oral composition comprising (C) ascorbic acid phosphate or a salt thereof in an oral composition containing (A) benzalkonium chloride and (B) sodium lauroyl sarcosine.   The composition for oral cavity according to claim 1, wherein ((A) + (B)) / (C) is 0.1 to 15 as a mass ratio.   (C) The composition for oral cavity of Claim 1 or 2 which mix | blended 0.1-2 mass% component.   The composition for oral cavity according to claim 1, 2 or 3, wherein the content of the component (A) is 0.005 to 0.1% by mass, and the content of the component (B) is 0.05 to 2% by mass.   (A) The bactericidal activity improvement method of the said composition for oral cavity which mix | blends (C) ascorbic acid phosphate ester or its salt with the composition for oral cavity containing a benzalkonium chloride and (B) sodium lauroyl sarcosine.   6. The method for improving bactericidal activity of an oral composition according to claim 5, wherein ((A) + (B)) / (C) is 0.1 to 15 as a mass ratio.