JP2011105690A - Liquid composition for oral cavity - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a liquid composition for oral cavity obtained by blending a water-soluble aluminum salt and a water-soluble potassium salt, improved in astringent taste and bitter taste, and also excellent in the preventing effect of hyperesthesia. <P>SOLUTION: The liquid composition for oral cavity includes (A) the water-soluble aluminum salt, (B) the water-soluble potassium salt, (C) an 8-11C linear aliphatic aldehyde and (D) a 6-12C lactone. <P>COPYRIGHT: (C)2011,JPO&INPIT

Description

  The present invention includes a water-soluble aluminum salt, particularly an aluminum lactate and a water-soluble potassium salt, particularly potassium nitrate, which is an active ingredient for preventing dentin hypersensitivity, and has a good feeling of use by improving astringency and bitterness. The present invention relates to an oral composition.

  The two major diseases of the oral cavity are dental caries and periodontal disease, and oral cleaning by brushing has been proposed as a preventive method, and for the purpose of further enhancing the effect of brushing, fluorine compounds are used for caries and fungicides are used for periodontal diseases. As a dentifrice containing an active ingredient such as an anti-inflammatory agent or a preparation that can be easily prevented, a mouthwash containing the same active ingredient has been introduced into the market.

  By the way, looking at the morbidity of the two major diseases by age group, the incidence of dental caries is high mainly among young people in overseas countries including Japan. The incidence of periodontal disease also tends to increase with the declining birthrate and the aging society.

  Under such circumstances, with the onset of periodontal disease, the gingiva is retracted and the cervical dentin is exposed, and an increase in new dentin hypersensitivity caused by cold air, cold water, brushing abrasion stimulation, etc. is attracting attention. The effective prevention method has been studied.

  Dentin hypersensitivity is different from persistent caries pain, and pain occurs when the above stimulation is applied. The effect of this is that oral cleaning such as brushing cleaning and brushing becomes insufficient, and the oral cavity becomes unclean. It causes a vicious circle in which dental caries and periodontal disease progress.

  Therefore, the development of active ingredients for preventing hypersensitivity has progressed in various companies, and several active ingredients have been developed so far and have been incorporated into dentifrices and mouthwashes.

  The main active ingredients include aluminum lactate as the aluminum salt and potassium nitrate and potassium citrate as the potassium salt.

  The preventive mechanism of aluminum salts is to block and block pain evangelism by depositing and blocking aluminum ions exposed dentin tubules.

  On the other hand, the prevention mechanism of potassium salt is to block pain stimulation by blunting action on nerve fibers which are the pathway of pain.

  The effects of these active ingredients have been proven in clinical trials, and it has been found that the combined use of two active ingredients exhibits a great effect in suppressing dentin hypersensitivity.

  However, when two active ingredients that have a problem with taste even in a single formulation are used simultaneously, the feeling of use is remarkably inferior due to the unique astringency and bitterness, especially when these active ingredients are blended in a liquid oral composition A great improvement was required in terms of palatability.

  To solve the above problems, for example, in Patent Document 1, aiming for improvement by blending a specific amount of an aluminum salt and a potassium salt, although certain effects on astringency and pain are recognized, It cannot be said that the improvement in usability has been obtained.

  In Patent Document 2, providing a liquid oral composition containing aluminum lactate and potassium nitrate with a nonionic surfactant and carboxymethyl cellulose provides a good feeling of use as well as an improvement in fat and oil stains in the oral cavity. Although it aimed, there is no mention about improvement of astringency and bitterness in a preparation using both aluminum lactate and potassium nitrate.

  Furthermore, Patent Document 3 and Patent Document 4 have been proposed as techniques related to oral compositions using aluminum lactate and potassium nitrate, which are related to the improvement of the effect of preventing hypersensitivity, and are related to the improvement of astringency and bitterness. There is no description at all.

  On the other hand, as a technique related to astringency and bitterness improvement, a technique in which a hydroxy-2-pyridone derivative is combined with an aluminum lactate salt and a potassium salt is proposed in Patent Document 5, but this technique does not improve the effect of preventing hypersensitivity. Although it can be seen, there is room for further improvement with respect to the unique astringency and bitterness as in the above technique.

  In addition, although patent documents 6-8 are proposed as a technique using aldehydes and lactones, the technique disclosed by these is the astringency and bitterness of the liquid oral composition which used aluminum lactate and potassium nitrate together. It is different from what improves this, and improvement of the astringency and bitterness of the liquid oral composition which concerns from these patent documents 6-8 cannot be estimated.

JP 2001-172146 A JP 2000-178150 A Japanese Patent Laid-Open No. 7-165550 JP-A-61-36212 JP 2004-59563 A JP 2004-203872 A JP 2005-247713 A Japanese Patent Laid-Open No. 10-310512

  As described above, there are water-soluble aluminum salts (such as aluminum lactate) and water-soluble potassium salts (such as potassium nitrate) as active ingredients to prevent hypersensitivity, and the combination of these active ingredients has a high sensory effect, but is unique. The taste is inferior due to its astringent taste and bitterness. In this case, products with enhanced palatability by dentifrice masking technology are on the market, but they are not liquid preparations. Therefore, the palatability of liquid preparations using a combination of water-soluble aluminum salt and water-soluble potassium salt is increased. Development of liquid preparations that are effective and ensured effectiveness is a technical issue.

  The present invention has been made in view of the above circumstances. In a liquid preparation containing a water-soluble aluminum salt (such as aluminum lactate) and a water-soluble potassium salt (such as potassium nitrate), it improves astringency and bitterness and prevents hypersensitivity. It aims at providing the composition for liquid oral cavity which is excellent in an effect.

  As a result of intensive studies to improve the astringency and bitterness of a liquid oral composition comprising a combination of a water-soluble aluminum salt and a water-soluble potassium salt, the present inventors have surprisingly found that a direct carbon number of 8 to 11 is obtained. It has been clarified that the above problem can be solved by using a chain aliphatic aldehyde and a lactone having 6 to 12 carbon atoms in combination.

Accordingly, the present invention provides the following liquid oral composition.
Claim 1:
(A) a water-soluble aluminum salt, (B) a water-soluble potassium salt, (C) a linear aliphatic aldehyde having 8 to 11 carbon atoms, and (D) a lactone having 6 to 12 carbon atoms. Liquid oral composition.
Claim 2:
The liquid oral composition according to claim 1, wherein (A) the water-soluble aluminum salt is aluminum lactate and (B) the water-soluble potassium salt is potassium nitrate.
Claim 3:
(D) Component / (C) component is 0.005-2 by mass ratio, The composition for liquid oral cavity of Claim 1 or 2 characterized by the above-mentioned.
Claim 4:
The liquid oral composition according to claim 1, 2 or 3, wherein the component (C) is a linear aliphatic aldehyde having 9 or 10 carbon atoms.
Claim 5:
The liquid oral composition according to any one of claims 1 to 4, wherein the component (D) is a lactone having 10 or 11 carbon atoms.

  According to the present invention, it contains a water-soluble aluminum salt such as aluminum lactate, which is an active ingredient for preventing dentin hypersensitivity, and a water-soluble potassium salt such as potassium nitrate. It is possible to provide a liquid composition for oral cavity that has an excellent effect of suppressing hypersensitivity.

Hereinafter, the present invention will be described in more detail.
The composition for liquid oral cavity of the present invention comprises (A) a water-soluble aluminum salt, (B) a water-soluble potassium salt, (C) a linear aliphatic aldehyde having 8 to 11 carbon atoms, and (D) a 6 to 12 carbon atoms. It is characterized by containing a lactone.

  (A) As a water-soluble aluminum salt of a component, aluminum lactate, aluminum gluconate, aluminum malonate, aluminum malate, etc. are mentioned.

  The blending amount of the water-soluble aluminum salt is preferably 0.02 to 0.3% (mass%, the same shall apply hereinafter) as aluminum with respect to the entire composition, and particularly preferably 0.05 to 0.1%. In the above-mentioned blending amount range, while giving a good hypersensitivity suppressing effect (blocking action of ivory finest) and giving a unique convergence effect and medicinal effect in terms of palatability, components (C) and (D) described later By blending, the bitterness and astringency that were problems in use feeling of the water-soluble aluminum salt are suppressed, and the bitterness and astringency can be eliminated. When the blending amount is less than 0.02%, the perceptual hypersensitivity suppressing effect is inferior, and when it exceeds 0.3%, a unique bitterness and astringency may occur even when the components (C) and (D) are blended.

  Examples of the water-soluble potassium salt of component (B) include potassium nitrate, potassium citrate, potassium chloride, and potassium sulfate.

  The compounding quantity of water-soluble potassium salt is 0.02 to 2% as potassium with respect to the whole composition, and 0.1 to 1.5% is especially preferable. In the above-mentioned blending range, it gives painless nerve dulling action, and the bitterness and astringency due to the water-soluble potassium salt can be suppressed by blending the components (C) and (D), and the bitterness and astringency can be eliminated. . If the blending amount is less than 0.02%, the perceptual hypersensitivity suppressing effect is poor, and if it exceeds 2%, astringency and bitterness may occur.

  Furthermore, in this invention, (C) component (C8-C11 linear aliphatic aldehyde) and (D) component (C6-C12 lactone) are used together. Thereby, the bitterness and astringency of water-soluble aluminum salt and water-soluble potassium salt can be reduced or suppressed, and palatability can be improved.

The component (C) is a linear aliphatic aldehyde having 8 to 11 carbon atoms, preferably 9 or 10 carbon atoms.
Specific examples include C8: octanal, C9: nonanal, C10: decanal, C11: undecanal, and one or more of these can be used. Among these, C9: nonanal and C10: decanal are particularly preferable.
In addition, as these linear aliphatic aldehydes, commercially available products such as those manufactured by Tokyo Chemical Industry Co., Ltd. can be used.

  The amount of component (C) is preferably 0.00001 to 0.001%, more preferably 0.00005 to 0.0005% of the total composition. When the blending amount is less than 0.00001%, even if the component (D) is used in combination, the water-soluble aluminum salt and water-soluble potassium salt have insufficient astringency and bitterness suppressing effects. Even when the component D) is used in combination, the bitterness or astringency may be emphasized.

The component (D) is a lactone having 6 to 12 carbon atoms, preferably 10 or 11 carbon atoms.
Specific examples include the following, and one or more of these can be used.
C6: γ-hexalactone, C7: γ-heptalactone, C8: γ-octalactone, C9: γ-nonalactone, C10: γ-decalactone, C11: γ-undecalactone, C12: dodecalactone, among these Particularly preferred are C10: γ-decalactone and C11: γ-undecalactone.
In addition, as these lactones, commercially available products such as those manufactured by Kamata Fragrance Co., Ltd. can be used.

  The blending amount of component (D) is preferably 0.000001 to 0.0001%, more preferably 0.000005 to 0.00005% of the entire composition. If the blending amount is less than 0.000001, even if the component (C) is used in combination, the water-soluble aluminum salt and water-soluble potassium salt have insufficient astringency and bitterness inhibiting effects. ) Even when ingredients are used in combination, bitterness and astringency may be emphasized.

  In the present invention, it is particularly preferable to use an aldehyde selected from C9: nonanal and C10: decanal and a lactone selected from C10: γ-decalactone and C11: γ-undecalactone.

  The total amount of the component (C) and the component (D) is preferably 0.000011 to 0.0011%, particularly preferably 0.000055 to 0.00055% of the entire composition. Astringency and bitterness can be effectively suppressed when the blending amount is within this range. When the blending amount is less than 0.000011%, the water-soluble aluminum salt and water-soluble potassium salt have insufficient astringency and bitterness suppression effects. When the blending amount exceeds 0.0011%, the bitterness and astringency are emphasized. There is.

  As for the blending ratio of the component (D) and the component (C), (D) / (C) is preferably 0.005 to 2, particularly preferably 0.01 to 1, in terms of mass ratio. Astringency and bitterness can be effectively suppressed when the blending amount is within this range. If the blending ratio is less than 0.005 or exceeds 2, the astringent taste and bitterness suppressing effect of the water-soluble aluminum salt and water-soluble potassium salt may be insufficient.

  The composition for liquid oral cavity of the present invention can be prepared and applied as a mouthwash, a liquid dentifrice, and the like, and in addition to the above components, an appropriate optional component can be blended depending on the dosage form. For example, wetting agents, thickeners, pH adjusters, preservatives, sweeteners, perfumes other than the above components (C) and (D), surfactants, active ingredients other than water-soluble aluminum salts and water-soluble potassium salts, It can contain coloring agents.

  Examples of the wetting agent include polyhydric alcohols such as sugar alcohols such as glycerin, ethylene glycol, propylene glycol, butylene glycol, polyethylene glycol, sorbitol, xylit, maltite, and lactit. The blending amount is preferably 1 to 20%, particularly 3 to 15%, based on the total amount of the composition.

  As thickeners, carboxymethylcellulose sodium, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, hydroxymethylethylcellulose, methylcellulose and other cellulosic binders, xanthan gum, carrageenan, guar gum, sodium alginate, cationized cellulose, montmorillonite, gelatin And sodium polyacrylate, and the like, and one or more of them can be blended. A compounding quantity is 0.001-0.3% normally with respect to the composition whole quantity.

Examples of pH adjusters include phthalic acid, phosphoric acid, citric acid, succinic acid, acetic acid, fumaric acid, malic acid and carbonic acid and their potassium, sodium and ammonium salts, ribonucleic acid and its salts, and sodium hydroxide. 1 type (s) or 2 or more types can be used.
The liquid oral composition of the present invention preferably has a pH of 4 to 8, particularly 5 to 7.

As preservatives, effective amounts of paraoxybenzoic acid esters such as butylparaben and ethylparaben, sodium benzoate, alkyldiaminoethylglycine hydrochloride, potassium sorbate and the like are used.
Examples of the sweetening agent include saccharin sodium, aspartame, stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidyl dihydrochalcone, perilartin and the like.

  In addition to the component (C) and further the component (D), other fragrances include, for example, eucalyptus oil, winter green oil, cassia oil, clove oil, thyme oil, sage oil, basil oil, cardamom oil, coriander oil, Spearmint oil, lavender oil, rosemary oil, laurel oil, camomil oil, caraway oil, marjoram oil, celery oil, bay oil, origanum oil, pine needle oil, neroli oil, lemongrass oil, rose oil, jasmine oil, patchouli Natural fragrances such as oil, Iris concrete, rose absolute, orange flower absolute, vanilla absolute, mango absolute, patchouli absolute, ginger oleoresin, pepper oleoresin, capsicum oleoresin, pepper extract, etc. in front Part cut, rear cut, fractional distillation, liquid-liquid extraction, essence, powder fragrance, etc.) and limonene, pinene, butanol, isoamyl alcohol, n-hexenol, cis-3-hexenol, cis-6 -Nonenol, linalool, α-terpineol, benzyl alcohol, phenylethyl alcohol, anethole, thymol, methyl chevicol, eugenol, carvone, menthone, pregon, 1,8-cineol, yonon, caron, cinnamaldehyde, benzaldehyde, ethyl acetate, Ethyl butyrate, isoamyl acetate, hexyl acetate, ethyl 2-methyl butyrate, allyl hexanoate, allyl cyclohexane propionate, linalyl acetate, menthyl acetate, menthyl lactate Carbyl acetate, phenoxyethyl isobutyrate, methyl jasmonate, methyl salicylate, ethyl salicylate, methyl cinnamate, methyl anthranilate, phenyl ethyl glycidate, ethyl lactate, vanillin, maltol, amblet lidide, dimethyl sulfide, Trimethylpyrazine, ethyl β-methylthiopropionate, furaneol, ethylcyclopentenolone, cycloten, 2-methylbutyric acid, propionic acid, p-methoxycinnamic aldehyde, 3-l-menthoxypropane-1,2 -Single fragrances such as diol, menthone glycerin acetal, spiranthol, monomenthyl succinate, linalool oxide, vanillyl butyl ether, isopulegol, and ethyl Alcohol, propylene glycol, triacetin, perfumes solvents such as glycerin fatty acid ester, a combination of known perfume materials used in the oral composition may be used. Although the compounding quantity of these fragrance | flavor raw materials is not specifically limited, It is preferable to use 0.000001 to 1% in a composition. Moreover, as a fragrance | flavor for perfume using the said fragrance | flavor raw material, it is preferable to use 0.1 to 2.0% in a composition.

As the surfactant, surfactants usually used in oral compositions such as anionic surfactants, nonionic surfactants, and amphoteric surfactants can be blended. For example, as an anionic surfactant, sodium alkylsulfate such as sodium lauryl sulfate and sodium myristyl sulfate, acyl sarcosine salts such as sodium lauroyl sarcosine, sodium myristoyl sarcosine, sodium dodecylbenzenesulfonate, sodium hydrogenated coconut fatty acid monoglyceride monosulfate, Examples include sodium lauryl sulfoacetate, N-acyl glutamate such as sodium N-palmitoyl glutamate, sodium N-methyl-N-acyl taurate, sodium N-methyl-N-acylalanine, sodium α-olefin sulfonate, and the like.
Examples of the nonionic surfactant include polyoxyethylene hydrogenated castor oil having an average addition mole number of ethylene oxide of 40 to 100 moles, an alkyl group having 16 to 18 carbon atoms, and an average addition mole number of ethylene oxide of 10 to 10. 40 mol of polyoxyethylene alkyl ether, sucrose fatty acid ester, alkylol amide, polyoxyethylene sorbitan monostearate, polyoxyethylene polyoxypropylene glycol, alkyl glucoside, fatty acid polyglyceride such as decaglyceryl laurate, etc. are used .
As the amphoteric surfactant, lauryldimethylaminoacetic acid betaine, N-coconut oil fatty acid acyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine, and the like are used, but are not limited thereto.
The blending amount of the surfactant is preferably 0.01 to 2% of the entire composition, and can be used within a range not impeding the effects of the present invention.

  As various active ingredients, in addition to the water-soluble aluminum salt of the component (A) and the water-soluble potassium salt of the component (B), other active ingredients such as sodium fluoride, sodium monofluorophosphate, tin fluoride, etc. Fluorine compounds, enzymes such as dextranase and mutanase, water-soluble phosphate compounds such as potassium phosphate and sodium salt of orthophosphate, isopropylmethylphenol, tranexamic acid, epsilon-aminocaproic acid, allantochlorhydroxyaluminum, hinokitiol, lauroyl sarcosine Sodium, ascorbic acid, dl-tocopherol acetate, dihydrocholesterol, α-bisabolol, chlorhexidine salts, azulene, glycyrrhetin, glycyrrhetinic acid, copper chlorophyllin sodium, chlorophyll, glycerophosphine Chelating phosphate compounds such as carbonate, copper compounds such as copper gluconate, strontium chloride, berberine, hydroxamic acid and its derivatives, sodium tripolyphosphate, zeolite, methoxyethylene, maleic anhydride copolymer, polyvinylpyrrolidone, epidihydro Examples thereof include extracts of cholesterin, cetylpyridinium chloride, benzethonium chloride, dihydrocholesterol, trichlorocarbanilide, zinc citrate, sweet cherry extract, duckweed extract, chamomile, clove, rosemary, red gon, safflower and the like. In addition, the compounding quantity of another active ingredient can be made into an effective quantity in the range which does not prevent the effect of this invention.

  As a colorant, a highly safe water-soluble dye such as Blue No. 1, Green No. 3, Yellow No. 4, Red No. 105 can be added.

  In addition, although ethyl alcohol is normally mix | blended in order to raise a refreshing feeling, in this invention, ethyl alcohol may not be mix | blended in order to provide a mild feeling of use.

  PET (polyethylene terephthalate), glass, polypropylene, polyethylene, and the like can be used as a container for storing the liquid oral cavity composition of the present invention. From the viewpoint of suppressing the adsorption of fragrances, the use of PET or glass is preferred.

  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,% is mass% unless otherwise specified.

[Examples and Comparative Examples]
Liquid oral compositions (mouthwashes) having the compositions shown in Tables 1 and 2 were prepared by conventional methods and evaluated by the following methods. The results are shown in Tables 1 and 2.

Usability evaluation:
Each mouthwash (mouthwash) was used by 15 people with hypersensitivity to dentin perception for 20 weeks after eating twice a day, and the astringent taste and bitterness after use were sensed according to the following criteria. evaluated.
A: No astringency or bitterness is felt, and the feeling of use is extremely good.
○: Astringency and bitterness are not felt, and the feeling of use is good.
Δ: Astringency and bitterness are felt, and the feeling of use is somewhat uncomfortable.
X: Astringency and bitterness are strongly felt, and the feeling of use is uncomfortable.

Evaluation of inhibitory effect on hypersensitivity:
Each mouthwash was used by 15 people with dentine hypersensitivity for 1 month, and the inhibitory effect on hypersensitivity was evaluated according to the following criteria.
A: Both pains of cold water stimulation and cold air stimulation were improved.
○: Both cold and cold pains were significantly improved.
(Triangle | delta): Although cold water irritation | stimulation improved, the pain by cold irritation | stimulation did not improve.
×: Neither pain of cold water stimulation nor cold air stimulation was improved.

Details of the components used in the following examples are shown below.
Aluminum lactate (Musashino Chemical Laboratory Co., Ltd.)
Potassium nitrate (Otsuka Pharmaceutical Co., Ltd.)
Polyethylene glycol 400 (manufactured by Lion Chemical Co., Ltd.)
Glycerin (Lion Oleochemical Co., Ltd.)
Propylene glycol (manufactured by ADEKA Corporation)
Xylitol (manufactured by Rocket Japan)
Polyoxyethylene (60) hydrogenated castor oil (average added mole number of ethylene oxide 60, manufactured by BASF)
Isopropylmethylphenol (manufactured by Osaka Kasei Co., Ltd.)
Dipotassium glycyrrhizinate (manufactured by Maruzen Pharmaceutical Co., Ltd.)
C7: heptanal, C8: octanal, C9: nonanal, C10: decanal, C11: undecanal, C12: dodecanal (manufactured by Tokyo Chemical Industry Co., Ltd.)
C5: γ-pentalactone (γ-valerolactone), C6: γ-hexalactone, C10: γ-decalactone, C11: γ-undecalactone, C12: γ-dodecalactone, C13: γ-tridecalactone (Iwata) Perfume Co., Ltd.)

Claims (5)

  (A) a water-soluble aluminum salt, (B) a water-soluble potassium salt, (C) a linear aliphatic aldehyde having 8 to 11 carbon atoms, and (D) a lactone having 6 to 12 carbon atoms. Liquid oral composition.   The liquid oral composition according to claim 1, wherein (A) the water-soluble aluminum salt is aluminum lactate and (B) the water-soluble potassium salt is potassium nitrate.   (D) Component / (C) component is 0.005-2 by mass ratio, The composition for liquid oral cavity of Claim 1 or 2 characterized by the above-mentioned.   The liquid oral composition according to claim 1, 2 or 3, wherein the component (C) is a linear aliphatic aldehyde having 9 or 10 carbon atoms.   The liquid oral composition according to any one of claims 1 to 4, wherein the component (D) is a lactone having 10 or 11 carbon atoms.