JP2016222556A - Liquid oral composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a liquid oral composition that allows the bactericidal effect of cetylpyridinium chloride to be sufficiently exhibited with its bitterness inhibited, and has a good taste, a low stimulus, and a good feeling in use.SOLUTION: A liquid oral composition comprises (A) cetylpyridinium chloride 0.02-0.1 mass%, (B) ethyl maltol 0.0003-0.005 mass%, and (C) l-menthol 0.0001-0.02 mass%, and has a pH of 5.5 or more and less than 7.5.SELECTED DRAWING: None

Description

  The present invention relates to a composition for a liquid oral cavity that exhibits a sufficient bactericidal effect of cetylpyridinium chloride, has a suppressed bitterness, has a good taste, low irritation, and a good feeling of use.

  Cetylpyridinium chloride (hereinafter abbreviated as CPC), which has an excellent bactericidal effect, is blended in oral compositions as a preventive measure for caries (Patent Documents 1 and 2), but has a problem that bitterness is strong and palatability is deteriorated. was there. Moreover, when the compounding quantity of CPC was reduced in order to improve palatability, sufficient sterilization effect was no longer acquired.

  On the other hand, regarding bitterness suppression, bitterness can be masked by adding l-menthol, but the amount of l-menthol that can sufficiently mask the bitterness of CPC, specifically more than 0.02% by mass. When formulated, it makes it difficult to feel fruity sweetness due to the irritation of l-menthol and the bitterness of the substance itself, and it is mild and less irritating. It was.

JP 60-255717 A JP 2005-68071 A JP 2003-55180 A

  Therefore, it has been desired to develop a technique that suppresses the bitter taste of CPC with a substance other than 1-menthol, and that sufficiently exhibits the bactericidal effect of CPC with a good taste, low irritation and mild feeling of use.

  The present invention has been made in view of the above circumstances, and provides a liquid oral composition that exhibits a sufficient sterilizing effect of CPC, suppresses bitterness, has good taste, low irritation, and has a good feeling of use. With the goal.

  As a result of intensive studies to achieve the above object, the present inventors have (B) a liquid oral composition containing 0.02 to 0.1% by mass of (A) cetylpyridinium chloride (CPC). 0.0003 to 0.005 mass% of ethyl maltol and 0.0001 to 0.02 mass% of (C) 1-menthol are blended, and the pH of the composition is 5.5 or more and less than 7.5 As a result, the sterilizing effect of CPC is fully exerted, bitterness is suppressed, irritation is also suppressed, the taste is good and a good feeling of use can be given with low irritation, and coloring of the preparation over time is also prevented. The present inventors have found that this can be done and have completed the present invention.

The inventors of the present invention have studied the ingredients that can mask the bitter taste of CPC other than l-menthol. When a small amount of l-menthol and ethyl maltol are combined with a specific amount of CPC, the present invention is surprisingly surprising. It was found that the bitter taste of CPC is masked, and the irritation caused by the combined use of CPC and 1-menthol is reduced and the aftertaste is improved. Furthermore, when a sufficient amount of ethyl maltol is added to mask the bitterness of CPC, there arises a problem that the liquid preparation is colored over time, but the coloration is generated by setting the pH of the composition to less than 7.5. The bitterness of CPC could be masked without any problems.
That is, in the present invention, when the components (A), (B), and (C) are combined in a specific amount, the component (B) acts specifically within a specific range of the amount of (C) 1-menthol. (A) Masking and improving the bitter taste of CPC, and (A) Crane and (C) Stimulation with 1-menthol are also suppressed, and furaneol is known as a masking ingredient for deteriorated odor in oral compositions (patent (Refer to Document 3) gives a remarkable effect that cannot be achieved by using ethylmaltol instead of ethylmaltol. Thus, in the present invention, the bactericidal effect of CPC against airborne bacteria in the mouth, appearance stability of liquid preparation over time (no coloring), no bitterness after use, no irritation after use, good aftertaste An excellent liquid oral composition can be provided, and the sterilizing effect of CPC can be satisfactorily exhibited under a good feeling of taste, low irritation and mildness.

Therefore, the present invention
(A) 0.02 to 0.1% by mass of cetylpyridinium chloride,
(B) 0.0003-0.005 mass% of ethyl maltol,
(C) 0.001 to 0.02 mass% of 1-menthol
Provided is a liquid oral composition containing pH 5.5 to less than 7.5.

  ADVANTAGE OF THE INVENTION According to this invention, the liquid oral cavity composition which has the favorable usability | use_condition which the bitterness is suppressed, the taste is good and there is little irritation | stimulation can be provided while the bactericidal effect of CPC is fully exhibited. In the present invention, a CPC sterilizing effect can be effectively imparted to children and women who are sensitive to bitterness and irritation with a pleasant feeling of use.

  The present invention will be described in further detail below. The composition for liquid oral cavity of the present invention contains (A) cetylpyridinium chloride (CPC), (B) ethyl maltol, and (C) 1-menthol, and has a pH of 5.5 or more and less than 7.5.

(A) CPC is important for expression of a bactericidal effect. A commercially available CPC can be used.
(A) The blending amount of CPC is 0.02 to 0.1% (mass%, the same applies hereinafter) of the entire composition, preferably 0.03 to 0.08%, more preferably 0.04 to 0.07%. If it exceeds 0.1%, the bitterness becomes strong and the bitterness cannot be improved. If it is less than 0.02%, a satisfactory blending effect cannot be obtained.

In the present invention, by using an appropriate amount of (B) ethyl maltol, (A) the effect of reducing the bitterness of CPC, particularly the bitterness remaining in the aftertaste, is given, and the liquid composition has a particularly low l-menthol content and within a specific range. , The effect of reducing the bitterness remaining in the aftertaste of CPC is excellent.
(B) The compounding quantity of ethyl maltol is 0.0003 to 0.005% of the whole composition, Preferably it is 0.0005 to 0.002%. If it exceeds 0.005%, strong coloring occurs over time, coloring cannot be improved, and sweetness remains in the aftertaste, resulting in poor usability. If it is less than 0.0003%, a satisfactory blending effect cannot be obtained, and bitterness cannot be reduced.

  (C) The compounding quantity of 1-menthol is 0.0001 to 0.02% of the whole composition, Preferably it is 0.0005 to 0.01%, More preferably, it is 0.0005 to 0.007%. If it exceeds 0.02%, the irritation is particularly strong in children and the feeling of use is poor. If it is less than 0.0001%, the bitterness is not sufficiently masked and the bad aftertaste cannot be reduced.

The pH of the composition is 5.5 or more and less than 7.5, preferably pH 5.5 to 7.4. If it is 7.5 or more, a satisfactory coloring suppression effect cannot be obtained, and the appearance stability over time is poor.
The pH was measured immediately after preparation using a pH meter (model number Hm-30S) manufactured by Toa Denpa Kogyo Co., Ltd. and showed a value after 3 minutes at 25 ° C. (the same applies hereinafter).
Moreover, although pH can be adjusted to the said range gradually, you may add a pH adjuster as needed. Examples of the pH adjuster include citric acid, sodium citrate, sodium dihydrogen phosphate, sodium hydroxide, and the like, and one or more of these may be used.

The composition for liquid oral cavity of the present invention is prepared as a liquid preparation in which compounding components are solubilized. For example, it is diluted with a mouthwash, a mouth freshener, or a concentrated type that is used as it is. It can be prepared into a mouthwash, a liquid dentifrice, and the like, and is particularly suitable as a mouthwash. It should be noted that, particularly in the mouthwash, bitterness, irritation and the like are particularly strongly expressed as compared with a paste-like preparation such as a dentifrice.In the present invention, the bitterness and irritation are reduced in such a liquid preparation, and a good feeling of use is obtained. Can be granted.
Further, in the composition of the present invention, other known components can be blended as necessary in addition to the above components within a range not impeding the effects of the present invention. Specifically, a wetting agent, a surfactant, a solvent, and a sweetener, a coloring agent, a fragrance, an active ingredient, and the like are blended as necessary.

  Examples of the wetting agent include sugar alcohols such as sorbitol, maltite, and xylit, and polyhydric alcohols such as glycerin. The amount of wetting agent is usually 2 to 20%.

As the surfactant, nonionic surfactants, anionic surfactants, cationic surfactants, amphoteric surfactants and the like that are generally used in liquid oral compositions can be used.
Nonionic surfactants include polyoxyethylene hydrogenated castor oil, sugar alcohol fatty acid esters such as sucrose fatty acid ester, polyhydric alcohol fatty acid esters such as glycerin fatty acid ester and polyglycerin fatty acid ester, and polyoxyethylene alkyl ether. It is done.
Examples of the anionic surfactant include alkyl sulfates such as sodium lauryl sulfate. Examples of the cationic surfactant include alkyl ammonium and alkyl benzyl ammonium salts, and examples of the amphoteric surfactant include betaine acetate type and imidazoline type.
The blending amount of the surfactant is preferably 0 to 10%, particularly preferably 0.1 to 5%.

  As the solvent, purified water is generally used. Further, lower alcohols such as ethanol, propylene glycol and the like may be added, but it is better not to add ethanol with irritation, and when ethanol is added, it is 1% or less, particularly 0.1% or less of the whole composition. desirable.

Examples of sweeteners include saccharin, saccharin sodium, stevioside, aspartame and the like.
As a colorant, a highly safe water-soluble pigment such as Blue No. 1, Green No. 3, Yellow No. 4, and Red No. 105 can be added.

Natural flavors such as peppermint oil, spearmint oil, eucalyptus oil, wintergreen oil, clove oil, thyme oil, sage oil, cardamom oil, rosemary oil, marjoram oil, lemon oil, nutmeg oil, lavender oil, paracres oil, etc. Essential oils and l-carvone, cinnamic aldehyde, orange oil, anethole, 1,8-cineole, methyl salicylate, eugenol, thymol, linalool, limonene, menthone, menthyl acetate, citral, camphor, borneol, pinene, spiranthol, etc. Perfume ingredients contained in the above natural essential oils, ethyl acetate, ethyl butyrate, isoamyl acetate, hexanal, hexenal, methyl anthranilate, ethyl methyl phenyl glycidate, benzalde Perfume ingredients such as quinol, vanillin, ethyl vanillin, furaneol, gamma / delta decalactone, gamma / deltown decalactone, N-ethyl-p-menthane-3-carboxamide, menthyl lactate, ethylene glycol-1-menthyl carbonate, and the like Is a combination of several fragrance ingredients and natural essential oils. One of the flavors of apple, banana, strawberry, blueberry, melon, peach, pineapple, grape, muscat, wine, cherry, squash, coffee, brandy, yogurt, etc. Species or two or more can be used.
The blending amount of these fragrances is usually 0.00001 to 3%. In addition, the fragrance | flavor containing ethyl maltol and l-menthol can mix | blend the compounding quantity of (B) ethyl maltol and (C) 1-menthol within the said range.

  As an active ingredient, chlorhexidine hydrochloride, chlorhexidine gluconate, benzalkonium chloride, cationic fungicides other than cetylpyridinium chloride, anti-inflammatory agents such as tranexamic acid, epsilon-aminocaproic acid, amylase, protease, mutanase, Enzymes such as dextranase, lysozyme, lytic enzyme, lytechenzyme, fluorides such as sodium fluoride, sodium monofluorophosphate, stannous fluoride, aluminum chlorohydroxy allantoin, allantoin, azulene, lysozyme chloride, ascorbic acid, etc. Vitamin C, sodium chloride, dihydrocholesterol, glycyrrhetin salts, glycyrrhetinic acid, hydrocholesterol, chlorophyll, copper chlorophyllin sodium, thyme, o Emissions, clove, plant extracts such as hamamelis, copper gluconate, Karopeputaido, water-soluble inorganic phosphoric acid compounds, polyethylene glycol, sodium lauroyl sarcosinate, isopropyl methyl phenol, polyvinylpyrrolidone, potassium nitrate, and the like may be added aluminum lactate. In addition, the compounding quantity of these arbitrary components is an effective quantity in the range which does not prevent the effect of this invention.

  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]
Liquid oral compositions (mouth rinses) having the compositions shown in Tables 1 to 3 were prepared by a conventional method. About the obtained mouthwash, the bactericidal effect with respect to an airborne microbe, external appearance stability, and the usability | use_condition were evaluated by the following method and reference | standard. Results as shown in Tables 1 to 3 were obtained.
In addition, pH is measured using the pH meter (model number Hm-30s) by Toa Denpa Kogyo immediately after preparation of a composition, and is a value after 25 degreeC and 3 minutes.

Evaluation method of bactericidal effect against airborne bacteria;
The bacterial solution used was prepared by dissolving 30 g of trypticase soy broth (manufactured by Difco) as a culture solution in 1 L of purified water, using Streptococcus mutans ATCC 10449 strain as an oral resident bacterium, at 37 ° C. under anaerobic conditions. Saline was added so that the permeability at 550 nm of the liquid cultured for 1 day with (5 vol% carbon dioxide gas, 95 vol% nitrogen) was 20. Add 0.3 mL of the bacterial solution to 2.7 mL of the sample (liquid oral composition), stir, react at 37 ° C. for 1 minute, stir again, and then add five test tubes containing 2.7 mL of the culture solution in advance. Prepared, 0.3 mL was added to the first test tube and stirred. 0.3 mL of this solution was collected, added to the second test tube, and stirred. This operation was similarly performed on the third to fifth test tubes in the same manner. After stirring the culture solution in the first, third, and fifth test tubes, 50 μL of the culture solution was spread on a 10% cotton defibrinated blood-containing trypticase soy agar plate (manufactured by Difco) and cultured under anaerobic conditions.
The grown colonies were counted, and the number of remaining Streptococcus mutans bacteria (cfu) was determined and evaluated according to the following evaluation criteria.
Criteria for evaluation of bactericidal effect against airborne bacteria ◎: Number of living bacteria is less than 10 ² ○: Number of living bacteria is 10 ² or more and less than 10 ³ Δ: Number of living bacteria is 10 ³ or more and less than 10 ⁴ ×: Number of living bacteria is 10 ⁴ or more

Evaluation method of appearance stability (no coloring);
Put 80 mL of each mouthwash shown in the table into a 100 mL PET bottle and store it in a 50 ° C constant temperature bath, and compare the appearance after 4 weeks with the control product (PET container filled with purified water in the same manner). Visual evaluation was made according to the following criteria. The average value of 5 samples was calculated and evaluated according to the following evaluation criteria.
Criteria for appearance stability (no coloration) 4: No coloration 3: Slight coloration is observed, but there is no problem 2: Coloration is observed in the whole preparation 1: The whole preparation is markedly colored Evaluation criteria for appearance stability (no coloration) ◎: Average point 3.5 to 4.0 point ○: Average point 3.0 point to less than 3.5 point △: Average point 2.0 point to 3 Less than 0 point x: Average point less than 2.0 point

Evaluation method of feeling of use (no bitterness);
10 mL of each mouthwash shown in the table was included in the mouth, rinsed for 30 seconds, and then 5 children aged 3 to 9 years were subjected to a sensory test on the bitterness after the mouthwash according to the following criteria. The average value of 5 persons was calculated | required and evaluated according to the following evaluation criteria.
Criteria for lack of bitterness after mouthwash 4 points: no bitterness 3 points: little bitterness 2 points: bitterness slightly 1 point: bitterness was considerable 1 evaluation of bitterness after mouthwash Standard ◎: Average point 3.5 points or more and 4.0 points or less ○: Average point 3.0 points or more and less than 3.5 points △: Average point 2.0 points or more and less than 3.0 points ×: Average point 2.0 Less than

Evaluation method of feeling of use (no stimulation);
10 mL of each mouthwash shown in the table was included in the mouth, rinsed for 30 seconds, and then 5 to 9-year-old children were subjected to a sensory test for stimulation after mouthwash according to the following criteria. The average value of 5 persons was calculated | required and evaluated according to the following evaluation criteria.
Evaluation criteria for non-irritation after mouth washing 4 points: No irritation 3 points: Almost no irritation 2 points: Slight irritation 1 point: There was considerable irritation Evaluation of no irritation after mouth washing Standard ◎: Average point 3.5 points or more and 4.0 points or less ○: Average point 3.0 points or more and less than 3.5 points △: Average point 2.0 points or more and less than 3.0 points ×: Average point 2.0 Less than

Evaluation method of feeling of use (good aftertaste);
10 mL of each mouthwash shown in the table was included in the mouth, rinsed for 30 seconds, and after schooling, 5 children aged 3 to 9 conducted a sensory test according to the following rating criteria. The average value of 5 persons was calculated | required and evaluated according to the following evaluation criteria.
Evaluation criteria for good aftertaste after mouthwash 4 points: Very good aftertaste 3 points: Good aftertaste 2 points: Slightly bad aftertaste 1 point: Poor aftertaste Evaluation criteria for good aftertaste after mouthwash ◎: Average 3.5 points or more and 4.0 points or less ○: Average point 3.0 points or more and less than 3.5 points △: Average point 2.0 points or more and less than 3.0 points ×: Average point less than 2.0 points

Details of the raw materials used are shown below.
<(A) component>
Cetylpyridinium chloride (manufactured by Wako Pure Chemical Industries, Ltd.)
<(B) component>
Ethyl maltol (Pfizer)
Furaneol (comparative product, manufactured by Iwata Inc.)
Ethyl butyrate (comparative product, manufactured by Inoue Fragrance Co., Ltd.)
<(C) component>
l-menthol (manufactured by Takasago International Corporation)

[Formulation example] Mouthwash (A) Cetylpyridinium chloride 0.05%
(B) Ethyl maltol 0.002
(C) l-Menthol 0.005
Glycerin 5
Propylene glycol 5
Polyoxyethylene hydrogenated castor oil 0.5
Xylit 4
Saccharin sodium 0.01
Citric acid 0.03
Sodium citrate 0.25
Fragrance 0.1
Purified water 85.053
Total 100.00%

Claims (2)

(A) 0.02 to 0.1% by mass of cetylpyridinium chloride,
(B) 0.0003-0.005 mass% of ethyl maltol,
(C) 0.001 to 0.02 mass% of 1-menthol
A composition for liquid oral cavity containing pH 5.5 to less than 7.5.   The liquid oral cavity composition according to claim 1, which is prepared as a mouthwash.