JP6451562B2 - Oral composition - Google Patents

Description

  The present invention relates to a composition for oral cavity containing a water-soluble metal salt which has an excellent effect of suppressing plaque formation.

  Conventionally, water-soluble metal salts such as copper salts, zinc salts, and tin salts are said to have a plaque-inhibiting effect, and proposals for oral compositions have been made (Patent Documents 1 to 3; International (Publication 2010/113688, JP 2007-126421 A, JP 5-930 A). In addition, since the said water-soluble metal salt has unpleasant tastes, such as a metal taste, in patent document 1, the unpleasant bitterness peculiar to copper compounds, such as copper gluconate, is suppressed, and it is the convergence which is an effective feeling of periodontal disease improvement. A feeling imparting effect is imparted, and in Patent Document 2, an unpleasant taste is suppressed by using a granulated product of a zinc compound, and a plaque formation inhibiting effect is imparted. Moreover, in patent document 3, the outstanding effect derived from the activity is provided by the stability improvement of tin fluoride.

  On the other hand, in oral compositions such as dentifrices, physical plaque removal is generally performed by the cleaning power of abrasives, and carbon dioxide is an abrasive that has relatively good cleaning and brushing feeling and excellent usability. Calcium is known.

International Publication No. 2010/113688 JP 2007-126421 A JP-A-5-930 JP, 2014-172908, A JP 2011-105650 A JP 2010-143846 A JP 2004-10497 A

  However, the dental plaque-suppressing effect of the oral composition containing a water-soluble metal salt is still not sufficient and there is room for improvement, and further improvement of the dental plaque-suppressing effect has been desired.

  This invention is made | formed in view of the said situation, and it aims at providing the composition for oral cavity containing the water-soluble metal salt which is excellent in the plaque formation inhibitory effect.

  As a result of intensive studies to achieve the above object, the present inventor has (A) one or two or more water-soluble metal salts selected from copper salts, zinc salts and tin salts, and (B) calcium carbonate. (C) An oral composition that has an excellent effect of inhibiting plaque formation by mixing an alkanediol having 5 to 10 carbon atoms, and also has a good feeling of use due to suppression of off-flavors. Has been found to yield the present invention.

That is, when the present inventor studied to improve the plaque-inhibiting effect of the water-soluble metal salt, when a water-soluble metal salt such as a copper salt is added to the oral composition, the plaque formation-inhibiting effect is deteriorated although the taste deteriorates. However, when calcium carbonate is blended as an abrasive together with the water-soluble metal salt, the effect of inhibiting the formation of plaque derived from the water-soluble metal salt is reduced and hardly exhibited. I understood it. Therefore, as a result of further investigation by the present inventor to solve the above problems, the (A), (B) component is the (C) component, and the (B) component / (C) component blending ratio is in a specific range. When combined in combination, the combination of components (A) and (B) does not cause a decrease in the effect of inhibiting the formation of plaque, and the effect of suppressing the formation of plaque derived from component (A) is greatly improved, resulting in excellent teeth. It was able to give an effect of inhibiting the formation of plaque and also to maintain a good taste by suppressing the taste.
In the present invention, alkanediol having 5 or more carbon atoms of component (C), which has almost no plaque formation inhibitory effect and has a unique taste, is specified by the blending ratio of component (B) / component (C). Within the range, the plaque formation inhibitory effect is specifically improved, and the off taste derived from the component (A) is suppressed, and propylene glycol is blended as a polyhydric alcohol as shown in Examples and Comparative Examples described later. Even if it does not contain the component (C), it provides a particularly remarkable effect that cannot be achieved.

  In addition, alkanediol is known as a compounding component of an oral composition, and is also known to be used as an antibacterial agent or preservative (Patent Documents 4 to 7; JP2014-172908A, JP2011). -105650, JP-A 2010-143846, and JP-A 2004-10497), these patent documents do not mention that alkanediol contributes to suppression of plaque formation of water-soluble metal salts. From the above patent document, it cannot be predicted that the effect of inhibiting the formation of plaque derived from a water-soluble metal salt is improved by a specific alkanediol.

Accordingly, the present invention provides the following oral composition.
[1]
(A) One or two or more water-soluble metal salts selected from copper salts, zinc salts and tin salts, and (B) oral compositions containing calcium carbonate, (C) having 5 to 10 carbon atoms An oral composition comprising an alkanediol blended, wherein the component (B) / component (C) has a mass ratio of 5 to 250.
[2]
Furthermore, the composition for oral cavity as described in [1] whose (A) component / (C) component is 0.02-10 as mass ratio.
[3]
Component (A) is one or more water-soluble metal salts selected from copper gluconate, copper citrate, zinc citrate, zinc gluconate, zinc chloride, tin fluoride and tin chloride [1] Or the composition for oral cavity as described in [2].
[4]
The composition for oral cavity according to [1], [2] or [3], wherein the component (A) is a water-soluble copper salt.
[5]
Component (C) is one or more alkanediols selected from 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediol, and decylene glycol [1] to [4] ] The composition for oral cavity in any one of.
[6]
The component (A) is 0.01 to 3% by mass, the component (B) is 10 to 55% by mass, and the component (C) is 0.1 to 4% by mass. Oral composition.
[7]
The composition for oral cavity according to any one of [1] to [6], prepared as a dentifrice.

  ADVANTAGE OF THE INVENTION According to this invention, the oral cavity composition containing the water-soluble metal salt which is excellent in the plaque formation inhibitory effect, and also has a favorable feeling of use because the off-flavor is suppressed.

  The present invention will be described in further detail below. The composition for oral cavity of this invention is (A) 1 type, or 2 or more types of water-soluble metal salt chosen from a copper salt, a zinc salt, and a tin salt, (B) Calcium carbonate, (C) C5-C10. Contains alkanediol.

  Component (A) is one or more water-soluble metal salts selected from copper salts, zinc salts, and tin salts. For example, copper salts such as copper gluconate and copper citrate, zinc citrate, and glucone. Examples thereof include zinc salts such as zinc acid and zinc chloride, and tin salts such as tin fluoride and tin chloride. Of these, copper gluconate, copper citrate, zinc citrate and tin fluoride are preferred. These water-soluble metal salts can be used singly or in combination of two or more, but water-soluble copper salts are particularly preferable, and copper gluconate and copper citrate are more preferable.

The blending amount of the water-soluble metal salt of the component (A) is preferably 0.01 to 3% (mass%, the same applies hereinafter) of the whole composition, and more preferably 0.03 to 2.6%. When 0.01% or more is blended, a sufficient plaque formation inhibitory effect can be obtained. If it is 3% or less, the off-taste can be sufficiently suppressed.
In addition, within the range of the above blending amount, the blending amount of the copper salt as the water-soluble metal salt is preferably 0.01 to 3%, particularly 0.03 to 2% of the total composition as the copper salt, and the blending of the zinc salt The amount of zinc salt is preferably 0.1 to 3%, particularly 0.5 to 2% of the whole composition, and the amount of tin salt is preferably 0.1 to 1% of the whole composition as tin salt.

  (B) Calcium carbonate is mainly blended as an abrasive, and specifically, light calcium carbonate, heavy calcium carbonate, and the like are used, and heavy calcium carbonate is particularly preferable.

The average particle diameter of calcium carbonate is not particularly limited, but is preferably 1 to 15 μm, more preferably 3 to 12 μm.
The average particle diameter is a value measured by a microtrack particle size distribution measuring apparatus (Model 17995-1-10, Type SRA, manufactured by Nikkiso Co., Ltd.), and is measured by adjusting the turbidity (dV value) of the sample to be 0.5. (The same applies hereinafter).

  As such calcium carbonate, commercially available products such as trade name Softon 1500 manufactured by Bihoku Flour Chemical Co., Ltd. and calcium carbonate manufactured by Shiroishi Calcium Co., Ltd. can be used.

  (B) Content of calcium carbonate is 10 to 55% of the whole composition, More preferably, it is 15 to 50%, More preferably, it is 20 to 45%. When it is 10% or more, it is possible to sufficiently obtain the effect of suppressing the formation of plaque as well as the cleaning power and the brushing feeling. When the content is 55% or less, it is possible to prevent a decrease in the plaque formation inhibitory effect and further improve the plaque formation inhibitory effect.

  In addition, in this invention, in addition to (B) calcium carbonate, you may contain the other abrasive | polishing agent well-known for oral cavity compositions in the range which does not interfere with the effect of this invention. Specifically, abrasive anhydrous silicic acid, zeolite, aluminum hydroxide, calcium phosphate or the like can be added. These abrasives may not be added, but when added, addition in the range of 1 to 30%, particularly 2 to 20%, particularly 3 to 15% of the entire composition is preferable. Furthermore, (B) The total content with respect to the whole composition of the abrasive | polishing agent containing a calcium carbonate is 10 to 55%, Especially within 15 to 45% of range is preferable.

  Component (C) is an alkanediol having 5 to 10 carbon atoms, preferably 6 to 8 carbon atoms, and more preferably a 1,2-alkanediol having a hydroxyl group at the 1 and 2 positions.

  Examples of the alkanediol having 5 to 10 carbon atoms include 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediol, decylene glycol, and the like. 1,2-hexanediol, 1,2-octanediol and decylene glycol are preferred, and 1,2-hexanediol and 1,2-octanediol are more preferred. These alkanediols can be used alone or in combination of two or more in terms of effect.

  As the alkanediol, those produced using a known method can be used, but commercially available products such as Hydrolite-5 # 6166751, Hydrolite-6 # 841129 and Hydrolite-8 manufactured by Simrise, Inc. can be used. # 109169, SymDiol 68 # 108580, SymClariol # 344028, etc. can also be used.

  The blending amount of the alkanediol as the component (C) is preferably 0.1 to 4% of the entire composition, more preferably 0.2 to 3%, and still more preferably 0.3 to 3%. When the content is 0.1% or more, the effect of suppressing the formation of plaque can be sufficiently improved, and the metal taste can be sufficiently improved and the taste can be sufficiently suppressed. When it is 4% or less, it is possible to prevent the appearance of its own taste (bitterness) and to sufficiently suppress the taste.

  In this invention, the compounding ratio of (B) component / (C) component is 5-250 as mass ratio, Preferably it is 10-200, More preferably, it is 10-150. Within this range, the effect of suppressing plaque formation is excellent, and off-taste can also be suppressed. If it is less than 5, the alkanediol of the component (C) itself has an unpleasant taste (bitterness) and the unnatural taste is inferior. If it exceeds 250, the decrease in the plaque formation inhibiting effect due to the component (B) cannot be suppressed, and the plaque formation inhibiting effect is inferior.

  Furthermore, in this invention, it is preferable that the mixture ratio of (A) component / (C) component is 0.02-10 as mass ratio, More preferably, it is 0.03-5. Within this range, the plaque formation inhibitory effect is more excellent and the taste can be further suppressed. If it is less than 0.02, the taste (bitterness) of the alkanediol itself of the component (C) may appear and the taste of taste may be inferior. If it exceeds 10, the metallic taste of the component (A) may be strongly developed and the taste of taste may be inferior.

  Especially the composition for oral cavity of this invention is suitably prepared as dentifrice composition, such as toothpaste. In this case, in addition to the above-described components, other known components that are generally blended in the oral composition may be blended as necessary within a range that does not interfere with the effects of the present invention. For example, binders, thickeners, surfactants, and sweeteners, preservatives, colorants, fragrances, medicinal ingredients, and the like as necessary. These ingredients are mixed with water in the usual manner. Can be manufactured.

  Examples of the binder include organic binders such as sodium carboxymethyl cellulose, carrageenan, and xanthan gum. The compounding amount of the binder is usually 0.5 to 2.0%, particularly 0.8 to 1.5%.

  Examples of the thickener include sugar alcohols such as sorbitol, glycerin, ethylene glycol, propylene glycol and the like. The blending amount of the thickener is usually 10 to 45%, particularly 20 to 35%.

  As the surfactant, an anionic surfactant, a nonionic surfactant, an amphoteric surfactant, and the like that are generally used in oral compositions can be used.

Specifically, examples of the anionic surfactant include alkyl sulfates such as sodium lauryl sulfate and sodium myristyl sulfate, lauroyl taurine salt, lauroyl sarcosine salt, and α-olefin sulfonate.
Nonionic surfactants include sugar fatty acid esters, sugar alcohol fatty acid esters, glycerin fatty acid esters, polyglycerin fatty acid esters, sorbitan fatty acid esters, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene fatty acid esters such as polyoxyethylene hydrogenated castor oil, and the like. And polyoxyethylene higher alcohol ethers such as polyoxyethylene lauryl ether and fatty acid alkanolamides.
Examples of amphoteric surfactants include betaine types and imidazoline types.
The content of the surfactant is preferably from 0.1 to 10%, particularly preferably from 0.5 to 8%, based on the entire composition.

  Examples of the sweetener include saccharin sodium, and examples of the preservative include paraoxybenzoic acid ester and sodium benzoate. Examples of the colorant include Red No. 2, No. 3, Yellow No. 4, Blue No. 1, and the like.

Perfumes include peppermint oil, spearmint oil, anise oil, eucalyptus oil, winter green oil, cassia oil, clove oil, thyme oil, sage oil, lemon oil, orange oil, peppermint oil, cardamom oil, coriander oil, mandarin oil, Lime oil, lavender oil, rosemary oil, laurel oil, camomil oil, caraway oil, marjoram oil, bay oil, lemongrass oil, origanum oil, pine needle oil, neroli oil, rose oil, jasmine oil, iris concrete, absolute Natural fragrances such as peppermint, absolute rose, orange flower, and fragrances processed by these natural fragrances (front reservoir cut, rear reservoir cut, fractional distillation, liquid-liquid extraction, essence, powder fragrance, etc.) And menthol, carvone, anethole, cineole, salichi Methyl acid, cinnamic aldehyde, eugenol, 3-1-menthoxypropane-1,2-diol, thymol, linalool, linalyl acetate, limonene, menthone, menthyl acetate, N-substituted-paramentane-3-carboxamide, pinene, Octyl acetate, citral, pulegone, calbeetoacetate, anisaldehyde, ethyl acetate, ethyl butyrate, allylcyclohexanepropionate, methyl anthranilate, ethyl methyl phenyl glycidate, vanillin, undecalactone, hexanal, ethyl alcohol, Propyl alcohol, butanol, isoamyl alcohol, hexenol, dimethyl sulfide, cycloten, furfural, trimethylpyrazine, ethyl lactate, methyl lath Oral flavors such as tate and ethyl thioacetate, as well as strawberry flavor, apple flavor, banana flavor, pineapple flavor, grape flavor, mango flavor, butter flavor, milk flavor, fruit mix flavor, tropical fruit flavor, etc. The well-known fragrance | flavor raw material used for the composition for cosmetics can be used, It is not limited to the fragrance | flavor of an Example.
Moreover, although a compounding quantity is not specifically limited, It is preferable to use said fragrance | flavor raw material 0.000001 to 1% in a formulation composition. Moreover, as a fragrance | flavor for fragrance | flavor which uses the said fragrance | flavor raw material, it is preferable to use 0.1 to 2% in an oral composition.

  Medicinal ingredients include fluorides such as sodium fluoride and sodium monofluorophosphate, cationic fungicides such as cetylpyridinium chloride, benzalkonium chloride and benzethonium chloride, nonionic fungicides such as isopropylmethylphenol, dextran Enzymes such as enzymes, tranexamic acid, epsilon aminocaproic acid, allantoin, glycyrrhizic acid, glycyrrhetinic acid and other anti-inflammatory substances, inorganic salts, vitamins and the like. The compounding quantity of these active ingredients can be made into an effective quantity in the range which does not prevent the effect of this invention.

  EXAMPLES Hereinafter, although an Example and a comparative example are shown and this invention is demonstrated concretely, this invention is not restrict | limited to the following Example. In the following examples, “%” means “% by mass” unless otherwise specified.

[Examples and Comparative Examples]
Oral compositions (dentifrices) having the compositions shown in Tables 1 to 3 were prepared by a conventional method and evaluated by the following methods. The results are shown in the table.

<Evaluation method of plaque formation inhibitory effect>
(1) Into a 24-well multiplate, 2 mL each of a solution obtained by dispersing and diluting a dentifrice 4 times with water was added, and each was mirror-polished hydroxyapatite plate made by Pentax (radius 0.35 cm x height 0.35 cm) Hereinafter, abbreviated as HAP plate.) Three pieces were immersed for 3 minutes.
(2) 2 mL of a buffer solution ^{* 1 in} which Streptococcus mutans strain 10449 is dispersed so that the turbidity at a wavelength of 660 nm is 0.35 is placed in the 24-well multiplate, and the HAP plate is added. Three pieces were immersed, and allowed to stand at 37 ° C. for 2 hours to allow the bacteria to adhere.
(3) The HAP plate was taken out and washed with sterilized water, and then the washed HAP plates were immersed in ² mL each of liquid medium ^{* 2 at} 37 ° C. for 8 hours to culture adherent bacteria.
(4) The HAP plate was taken out, washed with distilled water, and again immersed in 2 mL of a solution obtained by diluting and dispersing the dentifrice with 3 times the amount of water for 3 minutes.
(5) The immersed HAP plate was washed with distilled water, dyed with plaque staining solution, and the a value was measured with a color difference meter. The average value of the three sheets was calculated and evaluated according to the following criteria. It was judged that the average value of a value is less than 7.5 ((circle) or (double-circle)) that the plaque formation inhibitory effect is excellent.
Evaluation criteria for plaque formation inhibitory effect:
A: Average value of a value is less than 5 ○: Average value of a value is 5 or more and less than 7.5 Δ: Average value of a value is 7.5 or more and less than 10 ×: Average value of a value is 10 or more

* 1; Buffer 3.37 g of potassium chloride (KCl), 0.14 g of potassium dihydrogen phosphate (KH ₂ PO ₄ ), 0.11 g of calcium chloride (CaCl ₂ ), and 0.12 g of magnesium chloride (MgCl ₂ ) 02 g was dissolved in 800 mL of purified water, the pH was adjusted to 7.0 with potassium hydroxide (KOH), and the volume was adjusted to 1 L with purified water.
* 2: Liquid medium 100 mL of purified water was dissolved in 3 g of Tryptic Soy Broth and 0.5 g of sucrose.

<Evaluation method of tastelessness after use>
Put 0.5g of dentifrice on a toothbrush (3 rows of Clinica Habrush, hardness: normal, manufactured by Lion Co., Ltd.), brush for 3 minutes, rinse the mouth with water, It was judged in 5 stages. The average score of 10 people was obtained and evaluated according to the following criteria, and indicated by た, ○, Δ, × in the table. Those having an average score of 4.0 or more (◯ or ◎) were judged to have a good taste because the taste was suppressed.
Judgment criteria;
5: Does not feel a strange taste 4: Feels a little strange taste 3: Feels a strange taste 2: Feels a strong taste 1: Feels a very strong taste Evaluation criteria;
◎: Average point 4.5 points or more ○: Average point 4.0 points or more and less than 4.5 points △: Average point 3.0 points or more and less than 4.0 points ×: Average point 1.0 points or more and 3.0 points Less than

Details of the raw materials used are shown below. The average particle size of calcium carbonate was measured with a Microtrac particle size distribution analyzer as described above.
(A) Copper gluconate; manufactured by Kanto Scientific Co., Ltd. (A) zinc citrate; manufactured by Kanto Scientific Co., Ltd. (A) tin fluoride; manufactured by Wako Pure Chemical Industries, Ltd. (B) calcium carbonate; average particle size Within the range of 3 to 7 μm, Shiraishi Calcium Co., Ltd. (C) 1,2-pentanediol; Simrise Inc. (C) 1,2-hexanediol; Simrise Inc. (C) 1,2- Octanediol; Simrise Inc. (C) Decylene glycol; Simrise Inc.

Claims (7)

  (A) One or two or more water-soluble metal salts selected from copper salts, zinc salts and tin salts, and (B) oral compositions containing calcium carbonate, (C) having 5 to 10 carbon atoms An oral composition comprising an alkanediol blended, wherein the component (B) / component (C) has a mass ratio of 5 to 250.   Furthermore, the composition for oral cavity of Claim 1 whose (A) component / (C) component is 0.02-10 as mass ratio.   The component (A) is one or more water-soluble metal salts selected from copper gluconate, copper citrate, zinc citrate, zinc gluconate, zinc chloride, tin fluoride and tin chloride. Or the composition for oral cavity of 2.   The composition for oral cavity according to claim 1, 2 or 3, wherein the component (A) is a water-soluble copper salt.   The component (C) is one or more alkanediols selected from 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediol, and decylene glycol. The composition for oral cavity of any one of Claims.   The component (A) is contained in an amount of 0.01 to 3% by mass, the component (B) is contained in an amount of 10 to 55% by mass, and the component (C) is contained in an amount of 0.1 to 4% by mass. Oral composition.   The composition for oral cavity of any one of Claims 1-6 prepared as a dentifrice.