JP5845603B2 - Liquid or liquid oral composition and tongue coating adhesion inhibitor - Google Patents

Description

  The present invention relates to a liquid or liquid oral composition having a high effect of suppressing tongue coating adhesion and a tongue coating adhesion inhibitor.

  Conventionally, as a technique for removing tongue coating in the oral cavity or suppressing adhesion of tongue coating, a technique using actinidine (proteolytic enzyme) has been proposed in Patent Document 1 (International Publication No. 2003/090704 pamphlet). However, this technique may damage the oral mucosa.

Moreover, although the physical cleaning technique by a tongue cleaner is proposed by patent document 2 (Unexamined-Japanese-Patent No. 2001-161720), in this case, the cleaning property of the back of the tongue is insufficient, and depending on the brushing method, In some cases, the mucous membrane was damaged. Patent Document 3 (JP-A 10-18238 7 JP), but tongue coating removing technique using condensed phosphates are described, it is difficult to say that sufficient points of taste oral mucosa irritation, improved There was room.
Therefore, a composition for oral cavity with a good feeling of use that exhibits a high effect of suppressing adhesion of tongue coating is desired.

On the other hand, saliva is an important factor for cleansing the mouth, but it is thought that the decrease in saliva secretion by dry mouth such as dry mice affects tongue coating and accelerates tongue coating. The effectiveness of polyglutamate as a salivary secretion promoting component is described in Patent Document 4 (International Publication No. 2005/049050 pamphlet) and is known. Furthermore, organic acids or oral spray composition using a combination of the salt and glycerin such as citric acid polyglutamate is patent to be effective in the mouth of dryness improvement Document 5 (JP 2009-2749 6 7 No. Publication).

International Publication No. 2003/090704 Pamphlet JP 2001-161720 A Japanese Patent Laid-Open No. 10-182387 International Publication No. 2005/049050 Pamphlet JP 2009-274967 A

  The present invention has been made in view of the above circumstances, and an object of the present invention is to provide a liquid or liquid oral composition and tongue coating adhesion inhibitor that exhibits a high effect of suppressing tongue coating adhesion and has a good feeling of use.

  As a result of intensive studies to achieve the above object, the present inventors have determined that (A) a glycerin fatty acid ester having 8 to 14 carbon atoms in a fatty acid and (B) a polyglutamate, (B) component / ( By combining and blending the component A) in a mass ratio of 0.1 to 150, a liquid or liquid preparation having an excellent tongue coating adhesion-suppressing effect can be obtained. Thus, the present inventors have found that it has low irritation and good usability, and has made the present invention.

  That is, the present inventors surprisingly that the specific glycerin fatty acid ester of the component (A) has an effect of suppressing tongue coating adhesion, and the polyglutamate of the component (B) is appropriately combined with the component (A). In addition, synergistic increase in tongue coating adhesion suppression effect, excellent tongue coating adhesion suppression effect is exhibited, taste reduction and irritation caused by component (A) are eliminated, taste is good and low irritation to oral mucosa is good It has been found that it can be suitably applied to the tongue surface. It is known that polyglutamate has an effect of promoting salivary secretion, but by using polyglutamate together with a specific glycerin fatty acid ester, for example, spraying or dripping into the oral cavity, or washing the oral cavity is performed. It is a new finding of the inventors of the present application that by applying to the surface of the tongue by mouthing, an excellent effect of suppressing adhesion of tongue coating while maintaining a good feeling of use.

Accordingly, the present invention comprises (A) 0.01 to 2% by mass of glycerin fatty acid ester having 8 to 14 carbon atoms of fatty acid and (B) 0.05 to 5% by mass of polyglutamate, and (B ) Component / (A) component as a mass ratio in the range of 0.1 to 150, and liquid or liquid oral composition, and (A) glycerin fatty acid ester having 8 to 14 carbon atoms of fatty acid It contains 0.01 to 2% by mass and (B) 0.05 to 5% by mass of polyglutamate, and (B) component / (A) component is in the range of 0.1 to 150 as a mass ratio. Provided is a tongue coating adhesion inhibitor.

  ADVANTAGE OF THE INVENTION According to this invention, the liquid or liquid oral composition and tongue coating adhesion inhibitor which show a high tongue coating adhesion inhibitory effect, have a good taste, are low irritation | stimulation with respect to an oral mucosa, and have a favorable usability | use_condition can be provided.

  Hereinafter, the present invention will be described in more detail. The present invention comprises (A) a glycerin fatty acid ester having 8 to 14 carbon atoms in a fatty acid and (B) a polyglutamate in combination with the (B) component in an appropriate ratio with respect to the (A) component. It is characterized by.

  The component (A) is a glycerin fatty acid ester having 8 to 14 carbon atoms, preferably 8 to 11 carbon atoms. Those having less than 8 carbon atoms are difficult to obtain, and those having more than 14 carbon atoms are insufficient in the effect of suppressing adhesion of tongue coating.

  Examples of such glycerin fatty acid esters include glyceryl caprylate, glyceryl caprate, glyceryl undecylenate, glyceryl laurate, and glyceryl caprylate, glyceryl caprate, and glyceryl undecylate from the viewpoint of the effect of suppressing adhesion of tongue coating. Is preferred.

  The blending amount of the glycerin fatty acid ester as the component (A) is 0.01 to 2% (mass%, the same applies hereinafter) of the whole composition, particularly in terms of the effect of keeping the mouth clean (inhibition of tongue coating). 1 to 1% is preferable. If it is less than 0.01%, the adhesion inhibitory effect of tongue coating may not be sufficiently exhibited, and if it exceeds 2%, an unpleasant taste may remain after use, and oral mucosal irritation may become strong.

  As the polyglutamate salt of component (B), a sodium salt or potassium salt of polyglutamic acid is preferably used. Α or γ-polyglutamic acid that is chemically synthesized, or sodium or potassium salt of natural α or γ-polyglutamic acid obtained as a fermentation product from various strains is preferable, and natural polyglutamate is particularly preferable. Preferably, γ-polyglutamate having high productivity as a raw material is more preferable.

  The viscosity of polyglutamate is not particularly limited, but the viscosity (25 ° C.) of a 4% aqueous solution by a measurement method using a B-type viscometer described later is in the range of 10 to 200 mPa · s, particularly 30 to 150 mPa · s. It is preferable. If it is less than 10 mPa · s, there is a case where there is not enough saliva secretion and the effect of removing tongue coating is not sufficiently exhibited, or an unpleasant taste and oral mucosal irritation may not be sufficiently reduced or suppressed. When it exceeds 200 mPa · s, the viscosity of the preparation becomes high, the dispersibility in the mouth is deteriorated, and a sufficient effect may not be exhibited.

Viscosity Measurement Method Take 96 g of water in a 200 mL beaker, and add 4.0 g of γ-polyglutamate to it while stirring with a stirrer to completely dissolve it. Next, after leaving still in a 25 degreeC thermostat for 1 hour, the viscosity after 1 minute is measured correctly using a BL type | mold viscometer.
BL type viscometer: Tokyo Keiki B type viscometer Model BL
Rotor: No. 2 Number of revolutions: 60 rpm Measurement temperature: 25 ° C

  (B) The compounding quantity of the polyglutamate of a component is 0.05 to 5% of the whole composition, and 0.1 to 2% is especially preferable. If it is less than 0.05%, the unpleasant taste and oral mucosal irritation of glycerin fatty acid ester may not be suppressed, or the secretion of saliva is not sufficiently promoted, so that the effect of suppressing adhesion of tongue coating may not be satisfactorily exhibited. When it exceeds 5%, the viscosity of the preparation becomes high, the preparation becomes difficult to spread throughout the mouth, and the tongue moss adhesion inhibitory effect may not be sufficiently exhibited.

  (B) / (A) is 0.1-150 as a mass ratio, and, as for the mixture ratio of (B) component with respect to (A) component, Preferably it is 0.2-15. Even if the blending amounts of component (A) and component (B) are within the above ranges, if the ratio (B) / (A) is less than 0.1, the unpleasant taste and oral mucosal irritation are sufficiently reduced. It cannot be suppressed. When it exceeds 150, the viscosity of the preparation becomes high, dispersibility in the mouth is deteriorated, and sufficient effects are not exhibited.

  The oral composition of the present invention has a liquid or liquid form. Here, the liquid oral composition is a transparent or translucent preparation in which the blending components are solubilized, and solid components that are not solubilized such as abrasives are not usually blended, such as wetting agents, surfactants, A solvent, and if necessary, a sweetener, a fragrance, an active ingredient and the like are blended. The liquid oral composition is a gel-like preparation having low shape retention and fluidity, and a solid component such as an abrasive may be dispersed without being solubilized. For example, a polishing agent, a wetting agent, a thickening agent, a surfactant, a solvent, and a sweetener, a fragrance, an active ingredient, and the like are blended if necessary.

  The composition of the present invention is preferably used so that it can be directly applied to the tongue surface by spraying, dripping, or rinsing the oral cavity in the oral cavity, particularly the tongue surface. You may brush with a toothbrush. The dosage form is preferably a dosage form suitable for such use, specifically, mouthwash such as mouthwash, dentifrice such as liquid dentifrice, liquid dentifrice, spray, dripping agent, capsule, etc. Among them, it is particularly preferable to use it as a spray agent or a dripping agent from the viewpoint of portability where an appropriate amount can be freely used anytime and anywhere.

  In the composition of the present invention, other known components other than the above components (A) and (B) can be blended as necessary, as long as the effects of the present invention are not hindered depending on the form and dosage form. A component and water can be mixed and prepared by a conventional method.

  As an abrasive | polishing agent, the abrasive | polishing agent normally used for the composition for oral cavity can be used. Specifically, silica-based abrasives such as precipitated silica, aluminosilicate, dicalcium phosphate dihydrate and hydrates, calcium phosphate compounds such as primary calcium phosphate, tertiary calcium phosphate, calcium pyrophosphate, calcium carbonate, 1 type (s) or 2 or more types, such as a calcium hydroxide and aluminum hydroxide salt, can be mix | blended (a compounding quantity is 0-50% normally, especially 10-50%).

As the surfactant, an anionic surfactant, a nonionic surfactant, and an amphoteric surfactant can be blended.
Examples of the anionic surfactant include sodium alkyl sulfates such as sodium lauryl sulfate and sodium myristyl sulfate, and N-acyl sarcosine sodium such as N-lauroyl sarcosine sodium and N-myristoyl sarcosine sodium.
Nonionic surfactants include polyoxyethylene hydrogenated castor oil, sorbitan fatty acid ester, polyoxyethylene sorbitan fatty acid ester, sugar alcohol fatty acid esters such as sucrose fatty acid ester, polyoxyethylene glycerin fatty acid ester, polyethylene glycol fatty acid ester, etc. Polyhydric alcohol fatty acid esters, polyoxyethylene alkyl ethers, polyoxyethylene polyoxypropylene copolymers, ether type or ester type surfactants such as polyoxyethylene alkylphenyl ether, fatty acid alkanolamides such as lauric acid diethanolamide Kind. Examples of the cationic surfactant include alkyl ammonium and alkyl benzyl ammonium salts.
Examples of amphoteric surfactants include betaine acetate type amphoteric surfactants and imidazoline type amphoteric surfactants.
The blending amount of these surfactants can be 0 to 10%, particularly 0.1 to 5.0%.

  Examples of the thickener include xanthan gum, carrageenan, hydroxyethyl cellulose, sodium alginate, polyvinyl alcohol, sodium carboxymethyl cellulose and the like (the amount is usually 0 to 5%, particularly 0.5 to 3%).

  Examples of the wetting agent include sugar alcohols such as sorbitol, malt, and lactit, and polyhydric alcohols such as glycerin, ethylene glycol, polyethylene glycol, propylene glycol, and 1,3-butylene glycol (the amount is usually 2 to 70%). ).

  As the solvent, water is usually used, and the content thereof can be 20% or more. Furthermore, alcohols, such as C2-C4 lower monohydric alcohols, such as ethanol, isopropanol, butanol, propanol, etc. can also be mix | blended, and the compounding quantity can be 0-20%.

As sweetening agents, xylitol, maltitol, saccharin, sodium saccharin, stevioside, aspartame and the like can be blended.
As a colorant, a highly safe water-soluble pigment such as Blue No. 1, Green No. 3, Yellow No. 4, Red No. 105, and the like can be added.
Furthermore, citric acid, malic acid, tartaric acid, succinic acid and salts thereof, phosphoric acid, phosphates (sodium dihydrogen phosphate, disodium hydrogen phosphate, trisodium phosphate, etc.), carbonates, Bicarbonate and the like can be added.
The pH of the composition is preferably 3 to 10, particularly 5 to 8.

  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 oil, and l-menthol, l-carvone, cinnamic aldehyde, orange oil, anethole, 1,8-cineole, methyl salicylate, eugenol, thymol, linalool, limonene, menthone, menthyl acetate, citral, camphor, borneol, pinene, Perfume ingredients contained in the above natural essential oils such as spiranthol, ethyl acetate, ethyl butyrate, isoamyl acetate, hexanal, hexenal, methyl anthranilate, ethyl methyl phenyl glycidate Benzaldehyde, vanillin, ethyl vanillin, furaneol, maltol, ethyl maltol, gamma / delta decalactone, gamma / deltown decalactone, N-ethyl-p-menthane-3-carboxamide, menthyl lactate, ethylene glycol 1-menthyl carbonate Perfume ingredients such as apple, banana, strawberry, blueberry, melon, peach, pineapple, grape, muscat, wine, cherry, squash, coffee, brandy, yogurt 1 type, or 2 or more types of blended flavors such as those described above can be used within a range not impeding the effects of the present invention, and can be usually contained in the composition from 0.00001 to 3%.

As the active ingredient, such as cetyl pyridinium chloride, chlorhexidine hydrochloride, chlorhexidine gluconate, benzalkonium chloride, cationic bactericidal agent, such as benzethonium chloride, nonionic bactericide and isopropyl methylphenol, tranexamic acid, epsilon - and aminocaproic acid Anti-inflammatory agents, enzymes such as dextranase and mutanase, fluorides such as sodium fluoride, sodium monofluorophosphate, stannous fluoride, vitamin C such as ascorbic acid, dihydrocholesterol, glycyrrhetin salts, glycyrrhetinic acids , Hydrocholesterol, Chlorophyll, Copper Chlorophyllin Sodium, Thyme, Ogon, Clove, Hamamelis and other plant extracts, Copper Gluconate, Caropeptide, Sodium Polyphosphate, Water-soluble inorganic phosphorylation Things, polyvinylpyrrolidone, anti-tartar agents, anti-plaque agents, potassium nitrate, may be added to aluminum lactate and the like. In addition, the addition amount of these active ingredients can be made into the range which does not prevent the effect of this invention.

As the storage container, a known container suitable for storing the oral composition can be used. Examples of the material include polyethylene, polypropylene, polyethylene terephthalate, polyacetal and the like, and a container corresponding to the dosage form is used.
About a spray agent, if it is a container which has a structure which can spray a medicine, it will not be restricted in particular. Specifically, it is equipped with a container body such as a plastic bottle that contains the contents and a spray part having a spray mechanism such as a pump dispenser, and presses the pressing part of the spray part that is mounted in close contact with the upper opening of the container body What is sprayed by doing, or the container sprayed by pushing the container main body which stores the contents etc. can be used.
A dripping agent will not be restrict | limited especially if it is a container which has a structure which can be applied to an intraoral area, especially the tongue surface as a droplet. It is possible to use a dropper nozzle cap that pushes the container body into droplets or a dropper that drops into droplets.

  In the present invention, (A) a glycerin fatty acid ester having 8 to 14 carbon atoms in fatty acid and (B) polyglutamate, and (B) component / (A) component is 0.1 to 150 as a mass ratio. The tongue coating adhesion inhibitor which is the range can be provided. In this case, the details of the blending components, blending amounts, ratios, etc. are the same as described above.

  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. The following viscosities are values measured with a B-type viscometer in the same manner as described above.

[Examples 1 to 18, Comparative Examples 1 to 6]
The composition for oral cavity of the composition shown in Tables 1-4 was prepared by the following method, and the following evaluation was performed. The results are also shown in Tables 1-4.

<Preparation of formulation>
Each component was weighed and prepared by mixing with a stirrer. About 30 mL of the prepared liquid was filled in a spray container (Yoshino Kogyo, Y-70 dispenser, capacity 30 mL, polyethylene terephthalate bottle) to obtain a test preparation.

<Evaluation of tongue coating adhesion, feeling of use (taste), and oral mucosal irritation>
The test was carried out by 10 panelists who were worried about dry mouth. First, an expert started using the toothbrush to cleanly remove the tongue coating from the panel, and then started the test. The test formulation was sprayed 5 pushes towards the tongue. Used 6 to 10 times a day for 2 days. During the test period, cleaning of the tongue and use of mouthwash and mouth preparations were discontinued. After completion of the test, the person in charge observed the tongue of the panel, calculated the ratio (%) of the area covered with tongue coating, and evaluated ◎ to × based on the following criteria from the average value of the panel.
For the feeling of use (taste) and oral mucosal irritation, the panel itself evaluated based on the following criteria (7 levels), the average value of the scores was calculated, and ◎ to × were evaluated based on the following criteria. .

Evaluation criteria for tongue coating adhesion inhibitory effect;
◎ 0 or more and less than 15% ○ 15% or more and less than 30% △ 30% or more and less than 40% × 40% or more

Evaluation criteria for feeling of use (taste);
7 points No unpleasant nasty taste 6 points Almost unpleasant nasty taste 5 points No unpleasant nasty taste 4 points Neither feels uncomfortable 3 points Somewhat unpleasant taste 2 Feels a very unpleasant taste 1 Do you feel a very unpleasant taste

Evaluation criteria for oral mucosal irritation;
7 points I don't feel any stimulation 6 points I don't feel much stimulation 5 points I don't feel much stimulation 4 points I can't say either 3 points I feel a little stimulation 2 points I feel a lot of stimulation 1 point I feel a lot of stimulation

The average score of each evaluation was calculated and judged according to the following criteria.
◎ 6 points or more ○ 4.5 points or more and less than 6 points △ 3.5 points or more and less than 4.5 points × less than 3.5 points

[Examples 19 to 31]
Oral compositions having the compositions shown in Tables 5 to 7 were prepared by the same production method as described above. About Examples 19-23, it fills with the same spray container as the above, About Examples 24-28, it fills with a dripping agent container (Nippei Resin Industry Co., Ltd. product, Essence series DE20, material: Polyethylene, 20 mL), and implements. About Examples 29-31, it filled with the mouth-wash liquid container (The product made from Yoshino Kogyosho, the product made from a polyethylene terephthalate, 250 mL), and evaluated by said evaluation method.
In addition, about dripping, after removing tongue coating by the method similar to the case of the above-mentioned evaluation of tongue coating adhesion inhibitory effect, it is used by the method of dripping 3 drops on the tongue, and about mouthwash, After removing, the mouth was rinsed at about 10 mL for about 30 seconds and then used in a method of discharging and evaluated by the above method. The results are shown in Tables 5-7.

The details of the raw materials used are as follows.
Glyceryl caprylate: manufactured by Taiyo Kagaku Co., Ltd., trade name Sunsoft 700P-2
Glyceryl caprate: manufactured by Taiyo Chemical Co., Ltd., Sunsoft 760
Glyceryl undecylenate: Nikko Chemicals, trade name NIKKOL MGU
Glyceryl laurate: manufactured by Taiyo Kagaku Co., Ltd., trade name Sunsoft 750
Glyceryl palmitate: Nippon Emulsion Co., Ltd., trade name GMS-P
Sodium polyglutamate: Meiji Food Materia Co., Ltd., trade name: Meiji Polyglutamate
Minic acid and viscosity are as described in the table.
Potassium polyglutamate: manufactured by Meiji Food Materia Co., Ltd., viscosity is as described in the table.
Sodium pyrophosphate: manufactured by Taihei Chemical Industry Co., Ltd. Further, as perfumes A to F, those shown in Tables 8 to 14 were used.

表中、部は質量部である（以下、同様。）。

In the table, parts are parts by mass (the same applies hereinafter).

Claims (4)

(A) the number of carbon atoms of the fatty acid and 0.01 to 2 wt% 8-14 of glycerol fatty acid ester (B) containing a polyglutamate 0.05-5% by weight and component (B) / (A) A liquid or liquid oral composition, wherein the components are in the range of 0.1 to 150 in terms of mass ratio.   The composition for oral cavity according to claim 1, wherein the component (A) is a glycerin fatty acid ester having 8 to 11 carbon atoms in the fatty acid. The composition for oral cavity according to claim 1 or 2 , wherein the composition is applied to the surface of the tongue by spraying or dripping into the oral cavity or rinsing the oral cavity. (A) the number of carbon atoms of the fatty acids contain 8 to 14 of glycerol fatty acid ester 0.01 wt% and (B) polyglutamate 0.05-5%, component (B) / (A) component A tongue coating adhesion inhibitor characterized by having a mass ratio of 0.1 to 150.