JP2022021546A - Liquid composition for oral cavity - Google Patents

Abstract

To provide a liquid composition for oral cavity which can bring satisfactory use feeling while securing excellent adsorptivity of cationic bactericide even under the coexistence of polyoxyethylene hardened castor oil.SOLUTION: A liquid composition for oral cavity containing the following components (A) to (C): (A) cationic bactericide by 0.01 mass% or more and 1 mass% or less; (B) pyrophosphoric acid, citric acid, and one or more kinds of acid selected from salt thereof or a salt thereof by 0.01 mass% or more and 0.15 mass% or less in terms of the acid; and (C) polyoxyethylene hardened castor oil, in which a mass ratio ((C)/(A)) between the content of component (C) and the content of component (A) is 0.2 or more and 30 or less .SELECTED DRAWING: None

Description

The present invention relates to a liquid oral composition.

Liquid oral compositions such as mouthwash, dental rinse, and mouth spray are highly convenient compositions that can be applied by a simple method of gargle in the oral cavity and then spit out, so the number of users is increasing. It is in. Even in such liquid oral compositions, cationic bactericides such as cetylpyridinium chloride and benzethonium chloride are used from the viewpoint of caries prevention and the like, and various developments have been made to effectively exert the bactericidal effect. It has been done.

For example, Patent Document 1 discloses a liquid oral composition containing polyphosphoric acid or a salt thereof and a polyglycerin fatty acid ester together with a cationic bactericide, and Patent Document 2 describes cetylpyridinium chloride. , A liquid oral composition containing citric acid and tartrate acid in a specific amount has been disclosed, both of which enhance the adsorptivity of the bactericide to the tooth surface to enhance the bactericidal activity.
Further, Patent Document 3 discloses a liquid oral composition containing a cationic bactericide and calcium glycerophosphate and condensed phosphoric acid in a specific mass ratio, and an attempt is made to enhance the sustainability of the bactericidal effect. There is.

Japanese Unexamined Patent Publication No. 2006-117574 Japanese Unexamined Patent Publication No. 2016-108302 JP-A-2017-66036

By the way, in order to add an oil-soluble component such as a fragrance or a medicinal ingredient to such a liquid oral composition, a surfactant having excellent solubilizing ability, particularly a nonionic surfactant, is used to ensure the stability of the composition. However, the coexistence of polyoxyethylene hydrogenated castor oil and a cationic sterilizing agent may significantly impair the adsorptivity of the cationic sterilizing agent to the tooth surface. In addition, the bitterness and astringency derived from the cationic bactericide may be developed, or the irritating feeling and the squeaking feeling may be enhanced.
However, none of the above patent documents has made any study on these points, and there is still room for improvement in increasing the degree of freedom in the formulation design containing polyoxyethylene hydrogenated castor oil.

That is, the present invention relates to a liquid oral composition capable of providing a good usability while ensuring excellent adsorptivity of a cationic bactericide even in the coexistence of polyoxyethylene hydrogenated castor oil.

Therefore, as a result of various studies, the present inventor has found that a cationic bactericidal agent, a specific acid or a salt thereof, and a polyoxyethylene hydrogenated castor oil are contained in a specific content and mass ratio, so that the tooth of the cationic bactericidal agent can be used. It has been found that a liquid oral composition having both high adhesiveness to a surface and good usability can be obtained.

Therefore, in the present invention, the following components (A) to (C):
(A) Cationic bactericidal agent 0.01% by mass or more and 1% by mass or less (B) One or more kinds of acids selected from pyrophosphate, citric acid, and salts thereof, or 0. 01% by mass or more and 0.15% by mass or less (C) Contains polyoxyethylene hydrogenated castor oil, and the mass ratio of the content of the component (C) to the content of the component (A) ((C) / (A) )) Provides a liquid oral composition having a mass ratio of 0.2 or more and 30 or less.

According to the liquid oral composition of the present invention, in the presence of polyoxyethylene hydrogenated castor oil, not only can the cationic bactericide exhibit excellent adsorptivity to the tooth surface, but also astringency and bitterness, etc. It is possible to realize a good feeling of use without causing an unpleasant taste and without causing discomfort such as irritation or squeak.

Hereinafter, the present invention will be described in detail.
It should be noted that a good feeling of use means that when the liquid oral composition of the present invention is applied into the oral cavity, it does not cause an unpleasant taste such as astringency, bitterness or saltiness, and also has a stimulating feeling or a squeaky feeling. It means a feeling that is not accompanied by discomfort.

The liquid oral composition of the present invention contains 0.01% by mass or more and 1% by mass or less of a cationic bactericide as the component (A). Such component (A) is a component that exerts a bactericidal effect against bacteria that cause dental caries, periodontal disease, halitosis, etc., and is adsorbed on the surface of oral tissue, for example, the surface of teeth, the oral mucosa (including gums), and the like. Then, the effect can be enhanced.

Specific examples of the component (A) include one or more selected from cetylpyridinium chloride, benzethonium chloride, benzalkonium chloride, and chlorhexidine. Of these, cetylpyridinium chloride or benzethonium chloride is preferable, and cetylpyridinium chloride is more preferable, from the viewpoint of exerting sufficient bactericidal activity in the coexistence of the component (C).

The content of the component (A) is 0.01% by mass or more in the liquid oral composition of the present invention from the viewpoint of providing a sufficient bactericidal action while ensuring excellent adsorptivity to the tooth surface. It is preferably 0.02% by mass or more, and more preferably 0.03% by mass or more. Further, the content of the component (A) is 1% by mass or less in the liquid oral composition of the present invention from the viewpoint of suppressing the development of astringency, bitterness and irritation and ensuring a good usability. It is preferably 0.09% by mass or less, and more preferably 0.07% by mass or less. The content of the component (A) is 0.01% by mass or more and 1% by mass or less, preferably 0.02 to 0.09% by mass, in the liquid oral composition of the present invention. More preferably, it is 0.03 to 0.07% by mass.

The liquid oral composition of the present invention contains, as the component (B), one or more acids selected from pyrroline acid, citric acid, and salts thereof, or a salt thereof in an acid equivalent of 0.01% by mass. It contains 0.15% by mass or less. By containing the component (B) in such an amount, even in the coexistence of the component (C), while ensuring the excellent adsorptivity of the component (A) on the tooth surface, the appearance of an unpleasant taste can be achieved. The onset of discomfort can be effectively avoided. Examples of the salt of the component (B) include sodium salt and potassium salt, and sodium salt is preferable.
Among such components (B), pyrophosphoric acid or a salt thereof and citric acid or a salt thereof are contained from the viewpoint of effectively achieving both the adsorptivity of the component (A) to the tooth surface and a good usability. Is preferable.

The content of the component (B) is an acid in the liquid oral composition of the present invention from the viewpoint of effectively suppressing the development of off-flavor while ensuring the excellent adsorptivity of the component (A) to the tooth surface. The converted amount is 0.01% by mass or more, preferably 0.02% by mass or more, and more preferably 0.04% by mass or more. Further, the content of the component (B) is an acid equivalent amount in the liquid oral composition of the present invention from the viewpoint of effectively avoiding the development of irritation, squeaky feeling and salty taste to ensure a good usability. It is 0.15% by mass or less, preferably 0.13% by mass or less, more preferably 0.1% by mass or less, and preferably 0.1% by mass from the viewpoint of improving usability. % Or less, more preferably 0.09% by mass or less. The content of the component (B) in the liquid oral composition of the present invention is 0.01% by mass or more and 0.15% by mass or less in terms of acid, preferably 0.02 to 0. It is 13% by mass, more preferably 0.04 to 0.1% by mass, and from the viewpoint of improving usability, it is preferably 0.02 to 0.1% by mass, more preferably 0. It is 04 to 0.09% by mass or less.

The liquid oral composition of the present invention contains polyoxyethylene hydrogenated castor oil as the component (C). By containing the component (C), the component (A) can be stably contained in the liquid oral composition, and the inclusion of an oil-soluble component such as a medicinal component as another component is examined. Therefore, the degree of freedom in prescription design can be increased.

Specific examples of the component (C) include polyoxyethylene hydrogenated castor oil having an average added mole number of ethylene oxide of 100, polyoxyethylene hydrogenated castor oil having an average added mole number of ethylene oxide of 80, and ethylene oxide. Polyoxyethylene hydrogenated castor oil having an average added mole number of 60, polyoxyethylene hydrogenated castor oil having an average ethylene oxide addition mole number of 40, and polyoxyethylene hydrogenated castor oil having an average ethylene oxide addition mole number of 20. Can be mentioned. Among them, polyoxyethylene hydrogenated castor oil having an average number of added moles of ethylene oxide of 20, polyoxyethylene hydrogenated castor oil having an average number of added moles of ethylene oxide of 40, and polyoxy having an average number of added moles of ethylene oxide of 60. Ethylene-hardened castor oil is more preferable, and polyoxyethylene-cured castor oil having an average ethylene oxide addition molar number of 20 and polyoxyethylene-cured castor oil having an average ethylene oxide addition mole number of 40 are even more preferable.

The content of the component (C) is preferably 0.05% by mass or more in the liquid oral composition of the present invention from the viewpoint of effectively ensuring the excellent adsorptivity of the component (A) to the tooth surface. Yes, more preferably 0.1% by mass or more, still more preferably 0.15% by mass or more. Further, the content of the component (C) is preferably 1.5% by mass or less in the liquid oral composition of the present invention from the viewpoint of effectively suppressing the development of unpleasant taste and the development of discomfort. It is preferably 1.2% by mass or less, more preferably 1% by mass or less, preferably 0.9% by mass or less, more preferably 0.7% by mass or less, still more preferably 0.5% by mass. It is 0% by mass or less, more preferably 0.3% by mass or less. The content of the component (C) is preferably 0.05 to 1.5% by mass, more preferably 0.1 to 1.2% by mass in the liquid oral composition of the present invention. , More preferably 0.15 to 1% by mass, still more preferably 0.15 to 0.9% by mass, still more preferably 0.15 to 0.7% by mass, still more preferably 0.15. It is about 0.5% by mass, more preferably 0.15 to 0.3% by mass.

In the liquid oral composition of the present invention, the mass ratio ((C) / (A)) of the content of the component (C) to the content of the component (A) is 0.2 or more and 30 or less. As a result, even in the coexistence of the component (C), the expression of the off-flavor can be effectively suppressed while ensuring the excellent adsorptivity of the component (A) on the tooth surface.

The mass ratio ((C) / (A)) of the content of the component (C) to the content of the component (A) is 0.2 or more, preferably 1 or more, and more preferably 2 or more. It is more preferably 3 or more. The mass ratio ((C) / (A)) of the content of the component (C) to the content of the component (A) is 30 or less, preferably 20 or less, and more preferably 15 or less. Yes, more preferably 11 or less, still more preferably 7 or less. The mass ratio ((C) / (A)) of the content of the component (C) to the content of the component (A) is 0.2 or more and 30 or less, preferably 1 to 20. It is more preferably 2 to 15, still more preferably 3 to 11, and even more preferably 3 to 7.

In the liquid oral composition of the present invention, the mass ratio ((B) / (C)) of the content of the component (B) to the content of the component (C) is effective in expressing an unpleasant taste and an unpleasant sensation. From the viewpoint of suppressing the above, it is preferably 0.001 or more, more preferably 0.01 or more, more preferably 0.06 or more, still more preferably 0.08 or more, still more preferably 0. It is 12 or more, preferably 1 or less, more preferably 0.5 or less, and further preferably 0.4 or less.

The liquid oral composition of the present invention preferably contains water (D). As a result, it is possible to promote the solubilization or dispersion of the contained component, effectively enhance the adsorptivity of the component (A) to the tooth surface, and bring about a good usability.

The content of the component (D) is preferably 60% by mass in the liquid oral composition of the present invention from the viewpoint of sufficiently increasing the content of water and achieving good solubilization or dispersion of the contained components. % Or more, more preferably 65% by mass or more, further preferably 70% by mass or more, preferably 99.9% by mass or less, still more preferably 99.7% by mass or less, still more preferable. Is 99.5% by mass or less.

The liquid oral composition of the present invention can further contain a fragrance (E). The liquid oral composition of the present invention may contain a component (C) having excellent solubilizing ability, and even if such a component (E) is contained, the stability of the liquid oral composition is effective. Can be secured.

Specific examples of the component (E) include menthol, pregol, carboxylic, anetol, cineole, methyl salicylate, cinnamic aldehyde, eugenol, 3-1-mentoxypropane-1,2-diol, timol, and citro. Neryl Acetate, Linarol, Linaryl Acetate, Geraniol, Geranyl Acetate, Citronerol, Limonen, Menton, Mentil Acetate, N-Substituted Paramentan-3-Carboxamide, Pinen, Octylaldehyde, Citral, Pregon, Calvir Acetate, Dihydrocarbyl Acetate, Anis Alaldehyde, benzaldehyde, camphor, lactone, ethyl acetate, ethyl butyrate, allylcyclohexylpropionate, methylanthranilate, ethylmethylphenylglycidate, vanillin, undecalactone, hexanal, butyl acetate, isoamyl acetate, hexenol, dimethyl sulfide , Cycloten, flufural, trimethylpyrazine, ethyllactate, methyllactate, ethylthioacetate and other single fragrance ingredients; strawberry flavor, apple flavor, banana flavor, pineapple flavor, grape flavor, mango flavor, butter flavor, milk flavor, fruit mix flavor , Tropical fruit flavors and other blended fragrance ingredients, which also include peppermint oil, sparemint oil, cinnamon oil, anis oil, eucalyptus oil, winter green oil, cassia oil, clove oil, thyme oil, sage oil, sage. Clary oil, nutmeg oil, funnel oil, lemon oil, orange oil, peppermint oil, cardamon oil, coriander oil, basil oil, mandarin oil, lime oil, lavender oil, rosemary oil, ginger oil, grapefruit oil, laurel oil, Natural fragrance ingredients such as camomill oil, caraway oil, majorum oil, bay oil, lemongrass oil, lemon balm oil, pimentoberry oil, palmarosa oil, olivernum oil, pine needle oil, petiglen oil, neroli oil, rose oil, jasmine oil, etc. It may be, and it may be a fragrance component obtained by processing these natural fragrance components.

The content of the component (E) is preferably 0.01% by mass or more, more preferably 0.05% by mass or more, still more preferably 0.08% by mass in the liquid oral composition of the present invention. % Or more, preferably 1% by mass or less, more preferably 0.7% by mass or less, still more preferably 0.5% by mass or less.

In the liquid oral composition of the present invention, from the viewpoint of effectively achieving both the development of excellent adsorptivity of the component (A) on the tooth surface and the provision of a good usability, the polyvalent metal or the polyvalent metal It is preferable to limit the content of the contained compound. Examples of such polyvalent metals include one or more selected from strontium, magnesium, aluminum, calcium, zirconium, iron, copper, zinc, and manganese. The polyvalent metal-containing compound is selected from water-insoluble calcium compounds such as calcium carbonate, calcium hydrogen phosphate, insoluble potassium metaphosphate, aluminum silicate, zirconium silicate, aluminum oxide, aluminum hydroxide, zinc oxide and the like. One kind or two or more kinds are mentioned.

The content of the polyvalent metal or the polyvalent metal-containing compound is preferably 0.1% by mass or less, more preferably 0.05% by mass, in terms of metal atom equivalent in the liquid oral composition of the present invention. % Or less, more preferably 0.01% by mass or less, still more preferably 0.001% by mass or less, or the liquid oral composition of the present invention contains a polyvalent metal or a polyvalent metal-containing compound. It is preferably not contained substantially.

The liquid oral composition of the present invention may also contain ethanol from the viewpoint of improving the refreshing sensation. The content of ethanol is preferably 0 to 20% by mass in the liquid oral composition of the present invention.

The liquid oral composition of the present invention contains an anionic surfactant from the viewpoint of effectively achieving both the development of excellent adsorptivity of the component (A) on the tooth surface and the provision of a good usability. It is preferable to limit it. Examples of such anionic surfactants include alkyl sulfate ester salts such as sodium alkyl sulfate, acyl amino acid salts such as sodium acylglutamate and sodium acylsarcosine, N-methyl long chain acyl taurine sodium salts such as laurylmethyl taurine sodium, and alkyl. Examples thereof include one or more selected from alkyl phosphates such as sodium phosphate, higher fatty acid sulfonated monoglycerides, fatty acid ester salts of isethionic acid, and polyoxyethylene monoalkyl phosphates.

The content of the anionic surfactant in the liquid oral composition of the present invention is preferably 1% by mass or less, more preferably 0.5% by mass or less, still more preferably 0.1% by mass or less. It is more preferably 0.05% by mass or less, still more preferably 0.03% by mass or less, or the liquid oral composition of the present invention does not substantially contain an anionic surfactant. preferable.

The liquid oral composition of the present invention is a wetting agent such as glycerin, propylene glycol, butylene glycol, ethylene glycol, polyethylene glycol, xylitol, sorbitol, and erythritol, in addition to the above components, as long as the effects of the present invention are not impaired. And sweeteners; pigments; pigments and the like.

The pH of the liquid oral composition of the present invention at 25 ° C. is preferably 4 to 9 from the viewpoint of ensuring a good usability while sufficiently exerting the bactericidal effect of the component (A), and more preferably. It is 5 to 8, and more preferably 5.5 to 7.

Hereinafter, the present invention will be specifically described based on examples. Unless otherwise specified in the table, the content of each component indicates mass%.

[Examples 1 to 15, Comparative Examples 1 to 7]
Each component shown in Tables 1 and 2 was mixed to prepare a liquid oral composition. The pH of the obtained liquid oral composition at 25 ° C. was 6.0 ± 0.2. The obtained liquid oral composition was evaluated according to the following method.
The results are shown in Tables 1 and 2.

<< Adsorption rate of component (A) >>
Hydroxyapatite (Hap) powder (Taipei Kagaku Sangyo; hereinafter abbreviated as Hap), which is the main component of enamel, was used as a tooth model. Add 5 mL of each liquid oral composition shown in Tables 1 and 2 to 1.0 g of Hap, stir for 30 seconds, centrifuge (4000 rpm, 10 minutes), and use high performance liquid chromatography (HPLC) for absolute calibration. The concentration of the bactericide in the supernatant was quantified by the linear method), and the adsorption rate was calculated by the following formula.
Adsorption rate [%] = [1- (Fungicide concentration in each liquid oral composition) / (Fungicide concentration in supernatant)] x 100

<< Evaluation of usability >>
A specialized panelist contained 10 mL of each liquid oral composition in the mouth, and after gargle for 30 seconds, the feeling of use (presence or absence of astringency, bitterness, saltiness, irritation, and squeaky feeling) was sensory evaluated according to the following criteria. ..
The number of specialized panelists was 5, and if the calculated average value was 2.0 points or more, it was judged to be acceptable.

4 points: No astringency, bitterness or saltiness, no irritation or squeaky feeling 3 points: No astringency, bitterness or saltiness, almost no irritation or squeaky feeling 2 points: Astringency, Slightly felt at least one of bitterness, saltiness, irritation, and squeak. 1 point: Strongly felt at least one of astringency, bitterness, saltiness, irritation, and squeak.

Claims (6)

The following components (A) to (C):
(A) Cationic bactericidal agent 0.01% by mass or more and 1% by mass or less (B) One or more kinds of acids selected from pyrophosphate, citric acid, and salts thereof, or 0. 01% by mass or more and 0.15% by mass or less (C) Contains polyoxyethylene hydrogenated castor oil, and the mass ratio of the content of the component (C) to the content of the component (A) ((C) / (A) )) Is a liquid oral composition of 0.2 or more and 30 or less. The liquid oral composition according to claim 1, wherein the content of the polyvalent metal or the polyvalent metal-containing compound is 0.1% by mass or less in terms of metal atom equivalent. The liquid oral composition according to claim 1 or 2, wherein the mass ratio ((B) / (C)) of the content of the component (B) to the content of the component (C) is 0.001 or more and 1 or less. thing. The liquid oral composition according to any one of claims 1 to 3, wherein the component (A) is one or more selected from cetylpyridinium chloride, benzethonium chloride, benzalkonium chloride, and chlorhexidine. The liquid oral composition according to any one of claims 1 to 4, wherein the content of water (D) is 60% by mass or more and 99.9% by mass or less. The liquid oral composition according to any one of claims 1 to 5, further comprising 0.01% by mass or more and 1% by mass or less of the fragrance (E).