JP2006104101A - Composition for oral cavity - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To obtain a composition for oral cavity, having excellent use feeling and removal effect on cigarette tar. <P>SOLUTION: This composition for oral cavity is compounded with (A) a water-soluble pyrophosphate, (B) one or more polyvalent alcohols selected from polyethylene glycol, diethylene glycol, polypropylene glycol, dipropylene glycol and butylene glycol, (C) a lauryl sulfate salt, and (D) a betaine type amphoteric surfactant, of specific amounts at a specific mass ratio. <P>COPYRIGHT: (C)2006,JPO&NCIPI

Description

  The present invention relates to a composition for oral cavity which has a particularly good feeling of use and has an excellent tobacco dust removal effect.

  Dentifrice compositions aimed at whitening teeth by removing tobacco dust and the like have been known for some time. For example, toothpastes containing polyethylene glycol or polyvinylpyrrolidone as a dissolving agent for tobacco scum are generally commercially available. However, it is very difficult to remove the tobacco spider adhering to the tooth, and it has been difficult to remove it unless a high polishing effect by an abrasive is applied, and it has been necessary to pay attention to tooth wear. Moreover, it is known that a phytic acid compound has an effect of removing tobacco dust, and a composition for oral cavity such as a toothpaste containing the phytic acid compound has been proposed (Patent Documents 1 and 2: Patent No. 1354286, Patent No. 1). No. 1143565 publication). However, when phytic acid is blended into an oral composition, it tends to cause discoloration and flavor deterioration, making formulation difficult. On the other hand, pyrophosphate, which is a phosphoric acid compound similar to phytic acid, is useful for removing colored stains in oral compositions, but it is not effective enough for tobacco stains, which are strong stains. There wasn't. Furthermore, when these phosphoric acid compounds useful for removing colored stains are blended in the oral composition, there is a problem that the feeling of use becomes worse.

Japanese Patent No. 1354286 Japanese Patent No. 1423565

  As described above, there are problems in the conventional techniques for removing tobacco spider adhering to the teeth, and it cannot be said that it is sufficient yet. Development of a product is desired, and the present inventor has intensively studied to meet such a demand, and as a result, the present invention has been completed. That is, the present invention provides an oral composition such as a dentifrice composition that has little influence on tooth wear and formulation stability, has a good feeling in use, and has an excellent tobacco dust removal effect. It is an object to be solved and to provide a composition therefor.

  The present invention provides an oral composition such as a dentifrice for achieving the above-mentioned object, and the means newly adopted by the present inventors for this purpose is the removal of tobacco spider. Therefore, (A) a water-soluble pyrophosphate, (B) one or more polyhydric alcohols selected from polyethylene glycol, diethylene glycol, propylene glycol, dipropylene glycol, butylene glycol having an average molecular weight of 190 to 420, ( C) Including lauryl sulfate and further containing (D) betaine amphoteric active agent in a mass ratio of (C) / (D) of 1 to 4 in order to prevent deterioration of the feeling of use. However, when the water-soluble pyrophosphate exceeds 3.0% by mass, the feeling of use is also deteriorated. Therefore, (A) 0.1 to 3.0% by mass of a water-soluble pyrophosphate, (B) one kind selected from polyethylene glycol, diethylene glycol, propylene glycol, dipropylene glycol and butylene glycol having an average molecular weight of 190 to 420 Or the mass ratio of 2 or more types of polyhydric alcohol, (C) lauryl sulfate / (D) betaine type amphoteric activator is 1 to 4, and the total amount is 0.6 to 4.0% by mass. As a result, it has been found that the feeling of use is not deteriorated and that the effect of removing tobacco dust is synergistically increased, and the present invention has been made. In addition, some betaine-type amphoteric active agents can be obtained only as a mixture with water or the like, but the mass at the time of blending in the present invention is a pure content of the active agent excluding the solvent and the like.

  The oral composition of the present invention is one or two selected from (A) a water-soluble pyrophosphate, (B) polyethylene glycol having an average molecular weight of 190 to 420, diethylene glycol, propylene glycol, dipropylene glycol, and butylene glycol. By blending the above polyhydric alcohol, (C) lauryl sulfate and (D) betaine-type amphoteric active agent in a specific mass ratio and a specific amount, there is no problem in the feeling of use, and an excellent tobacco crab removal effect is expressed. be able to.

The (A) water-soluble pyrophosphate which is the first tobacco crab removal component of the present invention is a dehydrated condensation of phosphoric acid represented by the chemical formula M ₄ · P ₂ O ₇ , where M is an alkali metal ion or an alkali It consists of metal + hydrogen ions. Specific examples of the compound include tetrasodium pyrophosphate, disodium dihydrogen pyrophosphate, 4 potassium pyrophosphate, and disodium 2 potassium pyrophosphate. About the compounding quantity of water-soluble pyrophosphate, 0.1-3.0 mass% of the whole composition is good, Preferably 0.5-2.0 mass% is good. If it is less than 0.1% by mass, the effect of removing tobacco dust is not sufficiently exhibited, and if it exceeds 3.0% by mass, the feeling of use is deteriorated.

  The second tobacco dust removing component of the present invention is (B) a polyhydric alcohol selected from polyethylene glycol, diethylene glycol, propylene glycol, dipropylene glycol and butylene glycol having an average molecular weight of 190 to 420. Here, the average molecular weight of polyethylene glycol indicates the average molecular weight of the cosmetic raw material standard (2nd edition comment), and includes polyethylene glycol 200 (average molecular weight 190 to 210), polyethylene glycol 300 (average molecular weight 280 to 320), polyethylene glycol 400. (Average molecular weight 380-420) corresponds. Depending on the product, there may be a # between polyethylene glycol and the numerical value, such as polyethylene glycol # 200. If the average molecular weight exceeds 420, the ability to remove tobacco dust is not sufficiently exhibited. Of these polyhydric alcohols, polyethylene glycol 300, polyethylene glycol 400, and propylene glycol are particularly preferable from the viewpoint of usability.

  In the case of toothpaste and liquid dentifrice, the blending amount of these polyhydric alcohols is preferably 0.5 to 50.0% by mass, and more preferably 1.0 to 20.0% by mass. If it is less than 0.5% by mass, the effect of removing tobacco dust may not be sufficiently exhibited. Moreover, when it exceeds 50.0 mass%, a usability | use_condition may worsen or formulation may become impossible. Moreover, in the case of a mouthwash, a dental cream, a patch, etc., 0.5-90.0 mass% is preferable, and 1.0-80.0 mass% is more preferable. If it is less than 0.5% by mass, the effect of removing tobacco dust may not be sufficiently exhibited. Moreover, when it exceeds 90.0 mass%, a usability | use_condition may worsen or formulation may become impossible.

  (C) Lauryl sulfate, which is the third tobacco crab removing component of the present invention, is an anionic activator having an average alkyl chain length of 12 synthesized from higher fatty acids. Specific examples include sodium lauryl sulfate, potassium lauryl sulfate, and ammonium lauryl sulfate. From the ease of blending into oral compositions, sodium lauryl sulfate (manufactured by Toho Chemical Industry Co., Ltd., Daiichi Pharmaceutical ( Etc.) are most preferred. The amount thereof is preferably 0.5 to 2.0% by mass, more preferably 0.8 to 1.6% by mass, based on the entire composition. When it exceeds 2.0 mass%, a feeling of use may deteriorate. If it is less than 0.5% by mass, the effect of removing tobacco dust may not be exhibited.

The (D) betaine-type amphoteric activator compounded as an ingredient for preventing deterioration of the feeling of use is an activator represented by R ₁ R ₂ R ₃ —N ⁺ —CH ₂ COO ⁻ , and R ₁ , R ₂ , R ₃ There are various types depending on the lipophilic group. Specifically, 2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolium betaine, lauryl dimethylaminoacetic acid betaine, lauryl sulfobetaine, coconut oil fatty acid amidopropyl betaine, N-alkyl-1-hydroxyethyl imidazoline betaine sodium These can be used, and one of these can be used alone or in combination of two or more. Among these, 2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolium betaine (made by Lion Co., Ltd., Nippon Oil & Fats Co., Ltd.) has a feeling of use and is incorporated into the oral composition. It is preferable because of ease of use.

  Further, the mass ratio [(C) / (D)] of lauryl sulfate (C), which is a surfactant, and betaine-type amphoteric active agent (D) is 1 to 4, particularly preferably 2 to 3. When the amount of lauryl sulfate exceeds this mass ratio, the feeling of use deteriorates. In addition, if the amount of lauryl sulfate is less than this mass ratio, the effect of removing tobacco crab is not exhibited. Moreover, the total amount of lauryl sulfate and betaine-type amphoteric active agent is 0.6 to 4.0% by mass of the entire composition, and 1.1 to 2.4% by mass is particularly preferable. When it exceeds 4.0 mass%, a feeling of use will deteriorate. Further, if it is less than 0.6% by mass, the effect of removing tobacco dust is not exhibited.

  Moreover, it is also possible for the composition for oral cavity of this invention to use a nonionic active agent individually or in combination of 2 or more types to such an extent that the effect is not spoiled. Nonionic surfactants include sucrose fatty acid esters, sucrose fatty acid esters such as maltose fatty acid ester, sugar alcohol fatty acid esters such as maltitol fatty acid ester, lactol fatty acid ester, alkylol amide, polyoxyethylene sorbitan monostearate, etc. Polyoxyethylene sorbitan fatty acid ester, polyoxyethylene fatty acid ester such as polyoxyethylene hydrogenated castor oil, fatty acid diethanolamide such as lauric acid mono- or diethanolamide, sorbitan fatty acid ester, polyoxyethylene higher alcohol ether, polyoxyethylene polyoxypropylene Examples include copolymers, polyoxyethylene polyoxypropylene fatty acid esters, polyglycerin fatty acid esters, and pluronics.

  The composition for oral cavity of the present invention can be applied to toothpaste, mouthwash, patch and the like. In that case, various components that are usually used in oral compositions can be blended, but the required components and blending amounts differ depending on the dosage form. It is necessary to carry out within the range that does not interfere with the effects of the present invention, as well as the case. For example, in the case of toothpaste, abrasives, thickeners, binders, sweeteners, preservatives, fragrances, various active ingredients, and the like can be mixed with water and produced according to conventional methods.

  As abrasives to be blended at that time, dibasic calcium phosphate (dihydrate or anhydride), primary calcium phosphate, tertiary calcium phosphate, calcium pyrophosphate, calcium carbonate, aluminum hydroxide, alumina, magnesium carbonate, tertiary phosphate Magnesium, insoluble sodium metaphosphate, insoluble potassium metaphosphate, titanium oxide, zeolite, anhydrous silicic acid, hydrous silicic acid, titanium silicate, zirconium silicate, synthetic resin-based abrasives, etc. Abrasives are preferred. In the case of a toothpaste which is a typical dosage form, the blending amount is 5 to 80% by mass, preferably 10 to 50% by mass.

  As the thickener, sugar alcohols such as glycerin, sorbitol, xylitol, maltitol, and lactol, polyethylene glycol having a high degree of polymerization such as polyethylene glycol 4000, and the like can be used in addition to the polyhydric alcohol described above.

  As thickeners, carrageenan, sodium carboxymethylcellulose, methylcellulose, sodium hydroxyethylcellulose, sodium alginate, xanthan gum, tragacanth gum, karaya gum, arabic gum, locust bean gum, polyvinyl alcohol, sodium polyacrylate, carboxyvinyl polymer, polyvinylpyrrolidone, carbopol , Silica gel, aluminum silica gel, bee gum, laponite and the like.

  Sweetening agents include saccharin sodium, stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidyl hydrochalcone, perlartin, glycyrrhizin, thaumatin, asparatylphenylalanine methyl ester and the like.

  As fragrances, menthol, anethole, carvone, eugenol, limonene, n-decyl alcohol, citronellol, α-terpineol, citronellyl acetate, cineol, linalool, ethyl linalool, crocodile, thymol, spearmint oil, peppermint oil, lemon oil, orange Oil, sage oil, rosemary oil, cinnamon oil, pimento oil, cinnamon oil, perilla oil, winter green oil, clove oil or eucalyptus oil.

  In addition to these components, the composition for oral cavity of the present invention includes medicinal or active ingredients such as dextranase, amylase, proteinase, and mutanase enzymes, alkali metal monofluorophosphates such as sodium monofluorophosphate, Fluorides such as sodium fluoride and stannous fluoride, tranexamic acid, epsilon aminocaproic acid, aluminum chlorohydroxy allantoin, azulene, glycyrrhizinate, glycyrrhetinic acid, sodium chloride, vitamins and other anti-inflammatory agents, copper chlorophyll, glucone Bactericides such as copper acid, cetylpyridinium chloride, benzalkonium chloride, triclosan, hinokitiol, lysozyme chloride, polyphosphates other than pyrophosphate, and calculus preventives such as zeolite can also be added.

  Hereinafter, an experimental example of the effect of removing the tobacco dust using the composition example (that is, the example) corresponding to the composition for oral cavity of the present invention and the composition example (comparative example) not corresponding is shown, and the features and excellent features of the present invention However, the present invention is not limited to this embodiment.

[Experimental example]
[Examples 1 to 5, Comparative Examples 1 to 10]
Test dentifrices containing the ingredients shown in Tables 1 and 2 were prepared by a conventional method, and the effect of removing tobacco dust and the feeling of use were evaluated by the following methods.

[Tobacco crab removal test method]
The surface of the hydroxyapatite pellets (Pentax, diameter 7 mm × thickness 3.5 mm) was treated with sand blasting, and then washed with an ultrasonic cleaner in a neutral detergent solution. The surface was etched with a 30% phosphoric acid aqueous solution (for 10 minutes), washed with water, and naturally dried. After measuring the Lab value (L0) of the pellet before adhering to tobacco, after the tobacco (peace (produced by Nippon Tobacco Inc. (JT))) to which tobacco was adhering was burned out, suction was stopped and left for 3 minutes. . Repeat this operation 3 times]. It was dried at 100 ° C. for 1 hour, allowed to cool, and then immersed in a 37 ° C. water bath for 3 hours. After washing with water, it was dried at 150 ° C. for 3 hours. After standing to cool, it was lightly brushed 20 times with a toothbrush (flat cut), the surface moisture was removed, and the Lab value (L1) of the pellet after the tobacco dust adhered was measured. Next, the tobacco affixed hydroxyapatite pellet prepared by the above method was immersed in the toothpaste shown in Tables 1 and 2 for 15 minutes, and then the surface was lightly brushed with a toothbrush (flat cut) 20 times, and the Lab value of the pellet (L2 ) Was measured. The tobacco removal rate was obtained from the following equation.
Tobacco dust removal rate (%) = [(L2-L1) / (L0-L1)] × 100
According to the following criteria, the tobacco dust removal effect was evaluated from the tobacco stain removal rate.
◎: Tobacco dust removal rate 15% or more ○: Tobacco dust removal rate 10% or more and less than 15% △: Tobacco dust removal rate 5% or more and less than 10% ×: Tobacco dust removal rate less than 5%

[Method for evaluating the feeling of use during dentifrice]
When using 10 subjects, about 1g of the toothpaste shown in Tables 1 and 2 was taken on a toothbrush and brushed for 3 minutes, and whether or not there was any discomfort in the oral cavity after brushing (1), (2) a little (3) No response was obtained in three stages. Among these answers, (1) with 1 point, (2) with a little with 2 points, and (3) without with 3 points, the usability was evaluated from the average score of 10 people according to the following criteria.
◎: Average point 2.5 points or more and 3.0 points or less ○: Average point 2.0 points or more and less than 2.5 points △: Average point 1.5 points or more and less than 2.0 points ×: Average point 1.0 points More than 1.5 points

4 sodium pyrophosphate: Propylene glycol manufactured by Ohira Chemical Industry Co., Ltd .: Polyethylene glycol 400 manufactured by Dow Chemical Co., Ltd .: Polyethylene glycol 600 manufactured by Lion Co., Ltd. (comparative product): Sodium lauryl sulfate manufactured by Lion Co., Ltd. Toho Chemical Co., Ltd. ) Imidazoline betaine (2-alkyl-N-carboxymethyl-N-hydroxyethyl imidazolium betaine (pure 30%)): manufactured by Lion Co., Ltd. (however, the compounding amounts described in Tables 1 and 2 are 2- (The amount of alkyl-N-carboxymethyl-N-hydroxyethylimidazolium betaine in terms of pure content is shown.)

  As can be seen from the results of Tables 1 and 2, in Examples 1 to 5, (A) 0.1 to 3.0% by mass water-soluble pyrophosphate, (B) polyethylene glycol having an average molecular weight of 190 to 420 , One or more polyhydric alcohols selected from diethylene glycol, propylene glycol, dipropylene glycol, butylene glycol, and (C) lauryl sulfate and (D) a betaine-type amphoteric active agent at a specific mass ratio and specific amount. The dentifrice composition contained was good in both the effect of removing tobacco dust and the feeling of use during dentifrice. On the other hand, in Comparative Examples 1-10, sufficient effect was not exhibited in any point of the tobacco dust removal effect and the usability at the time of toothpaste. In these examples, the abrasiveness was the same as when no tobacco dust removing components (A), (B), (C) were blended. Further, as a result of conducting a storage stability test (comparing a product stored at 40 ° C. for one month with a product stored at room temperature), there was no significant discoloration or flavor deterioration.

[Examples 6 to 13]
Examples 6 to 13 of the dentifrice having a composition corresponding to the composition for oral cavity of the present invention are shown below. In these examples, (A) 0.1 to 3.0% by mass of water-soluble pyrophosphate Salt, (B) one or more polyhydric alcohols selected from polyethylene glycol, diethylene glycol, propylene glycol, dipropylene glycol, butylene glycol having an average molecular weight of 190 to 420, and (C) lauryl sulfate and (D ) Betaine amphoteric activator was blended in a specific mass ratio and a specific amount, and it was confirmed that there was no problem in use feeling as in Examples 1 to 5 and an excellent tobacco dust removal effect. Further, no problems were observed in discoloration and flavor deterioration in the storage stability test. In the following examples,% indicates mass%.

Example 6 Toothpaste:
(A) Tetrasodium pyrophosphate 1.5%
(B) Butylene glycol 10.0%
(C) Sodium lauryl sulfate 1.2%
(D) Lauryldimethylaminoacetic acid betaine 0.6%
Precipitated silica 25.0%
70% sorbitol solution 20.0%
Sodium carboxymethylcellulose 1.4%
Saccharin sodium 0.1%
Potassium glycyrrhizinate 1.0%
Tranexamic acid 0.05%
α-Alumina Anhydride 3.0%
Methylparaben 0.05
Benzethonium chloride 0.25%
Fragrance 1.0%
Disodium hydrogen phosphate 1.0%
Water remaining
Total 100.0%
(C) / (D) = 2, tobacco dust removal effect: ◎, usability evaluation: ○

Example 7 Toothpaste:
(A) Disodium pyrophosphate 2 potassium 1.0%
(B) Polyethylene glycol 200 2.0%
(C) Sodium lauryl sulfate 1.2%
(D) Lauryl sulfobetaine 0.4%
Aluminum hydroxide 35.0%
Titanium oxide 2.0%
Glycerin 20.0%
Hydroxyethylcellulose sodium 1.4%
Saccharin sodium 0.1%
Colloidal silica 3.0%
Sodium fluoride 0.22%
Triclosan 0.1%
Methylparaben 0.05%
Fragrance 1.0%
Water remaining
Total 100.0%
(C) / (D) = 3, tobacco dust removal effect: ◎, usability evaluation: ○

[Example 8] Toothpaste:
(A) Tetrasodium pyrophosphate 0.8%
(B) Propylene glycol 3.0%
(C) Sodium lauryl sulfate 0.9%
(D) 2-alkyl-N-carboxymethyl 0.3%
-N-hydroxyimidazolinium betaine
Silicic anhydride 30.0%
Sorbitol 20.0%
Glycerin 10.0%
Sodium polyacrylate 1.5%
Saccharin sodium 0.2%
Sodium benzoate 0.3%
Methyl paraoxybenzoate 0.1%
Sodium monofluorophosphate 0.76%
Tocopherol acetate 0.1%
Fragrance 1.0%
Water remaining
Total 100.0%
(C) / (D) = 3, tobacco dust removal effect: ○, usability evaluation: ◎

Example 9 Dental cream:
(A) Tetrasodium pyrophosphate 1.8%
(B) Diethylene glycol 1.0%
(C) Sodium lauryl sulfate 0.8%
(D) Lauryl sulfobetaine 0.2%
Sorbitol 20.0%
Sodium carboxymethylcellulose 1.0%
Saccharin sodium 0.1%
Ethyl paraoxybenzoate 0.1%
Benzalkonium chloride 0.5%
Fragrance 0.8%
Water remaining
Total 100.0%
(C) / (D) = 4, tobacco dust removal effect: ◎, usability evaluation: ○

[Example 10] Liquid dentifrice:
(A) Tetrasodium pyrophosphate 1.0%
(B) Dipropylene glycol 3.0%
(C) Sodium lauryl sulfate 1.0%
(D) Palm oil fatty acid amidopropyl betaine 0.4%
Silica anhydride 15.0%
60% sorbite solution 30.0%
Glycerin 35.0%
Xanthan gum 0.2%
Carrageenan 0.5%
Sodium alginate 1.0%
Sodium monofluorophosphate 0.76%
Dextranase (1 million u / g) 0.5%
Saccharin sodium 0.1%
Fragrance 1.0%
Water remaining
Total 100.0%
(C) / (D) = 2.5, tobacco dust removal effect: ◎, usability evaluation: ○

Example 11 Dental cream:
(A) 4 potassium pyrophosphate 1.2%
(B) Polyethylene glycol 200 10.0%
(B) Diethylene glycol 5.0%
(C) Sodium lauryl sulfate 1.0%
(D) Lauryldimethylaminoacetic acid betaine 0.8%
60% sorbite solution 30.0%
Glycerin 30.0%
Carrageenan 0.5%
Sodium alginate 1.0%
Sodium fluoride 0.21%
Potassium nitrate 5.0%
Saccharin sodium 0.1%
Cetylpyridinium chloride 0.3%
Fragrance 1.0%
Water remaining
Total 100.0%
(C) / (D) = 1.25, tobacco dust removal effect: ○, feeling of use evaluation: ○

Example 12 Mouthwash:
(A) Tetrasodium pyrophosphate 0.8%
(B) Polyethylene glycol 400 5.0%
(C) Sodium lauryl sulfate 0.4%
(D) 2-Undecyl-N-carboxymethyl 0.4%
-N-hydroxyethylimidazolinium betaine
Ethanol 10.0%
Glycerin 10.0%
Saccharin sodium 0.05%
Sodium monofluorophosphate 0.05%
Chlorhexidine gluconate 0.01%
Yellow No. 4 0.0001%
Methyl paraoxybenzoate 0.1%
Sodium benzoate 0.2%
Fragrance 0.3%
Trisodium citrate 0.2%
Benzethonium chloride 0.2%
Water remaining
Total 100.0%
(C) / (D) = 1, tobacco dust removal effect: ○, usability evaluation: ◎

Example 13 Toothpaste:
(A) Tetrasodium pyrophosphate 1.0%
(B) Propylene glycol 3.0%
(C) Sodium lauryl sulfate 0.9%
(D) 2-Undecyl-N-carboxymethyl 0.3%
-N-hydroxyethylimidazolinium betaine sodium carboxymethylcellulose 1.2%
70% sorbite solution 30.0%
Silica anhydride 25.0%
Sodium fluoride 0.21%
Blue No. 1 0.0001%
Fragrance 1.3%
Aluminum oxide 2.0%
4A type zeolite 1.5%
Saccharin sodium 0.2%
Titanium oxide 0.2%
Water remaining
Total 100.0%
(C) / (D) = 3, tobacco dust removal effect: ◎, usability evaluation: ◎

Claims (1)

  (A) water-soluble pyrophosphate, (B) one or more polyhydric alcohols selected from polyethylene glycol, diethylene glycol, propylene glycol, dipropylene glycol, butylene glycol having an average molecular weight of 190 to 420, (C) It contains lauryl sulfate and (D) a betaine-type amphoteric active agent, and the water-soluble pyrophosphate content of component (A) is 0.1 to 3.0% by mass of the total composition, The mass ratio [(C) / (D)] of (C) component lauryl sulfate to (D) component betaine-type amphoteric active agent is 1 to 4, and the sum of (C) component and (D) component Content for oral cavity composition characterized by being content 0.6-4.0 mass% of the whole composition.