JPS61151113A - Composition for oral cavity application - Google Patents

Abstract

PURPOSE:To obtain a composition for oral cavity application, effective to suppress the formation of tartar for a long period, by compounding a straight-chain sodium polyphosphate having a specific average polymerization degree with an abrasive selected from silica, alumina, aluminum hydroxide and titanium oxide. CONSTITUTION:The objective composition for oral cavity application is produced by compounding (A) a sodium polyphosphate having an average polymerization degree of >=20, especially 40-70 and exhibiting high stability in the composition and excellent tartar-preventive effect with (B) one or more abrasives selected from silica, alumina, alumina hydroxide and titanium oxide to improve the stability of the component A in the composition, and preferably (C) a water-soluble polyvalent metal salt having high compatibility to the component A and tartar-preventing effect, especially a water-soluble magnesium salt to improve the tartar-preventing effect. The amounts of the components A, B and C in the whole composition are preferably 5-40wt%, 0.1-5wt% and 0.01-2wt%, respectively.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to an oral cavity composition containing linear sodium polyphosphate having an average degree of polymerization of 20 or more as an active ingredient and suppressing the formation of tartar over a long period of time.

Tartar is a hard deposit with high mineral content that forms on the tooth surface and is a major cause of gingivitis, periodontitis, etc. Therefore, suppressing the formation of tartar is an effective way to prevent periodontal disease. , which is very effective therapeutically. In this case, regular brushing of the teeth can prevent rapid accumulation of tartar, but is not sufficient to remove all the tartar deposited on the teeth.

The formation of this dental calculus is thought to occur when amorphous or microcrystalline calcium phosphate is deposited on the bacterial membrane system and #1 interfungal substances in dental plaque, and gradually becomes more dense and transforms into hydroxyapatite. Therefore, in order to suppress the formation of tartar, it is sufficient to inhibit the crystal growth of hydroxia/IPtite, and therefore, it is desirable to develop an oral composition that can effectively suppress the formation of hydroxia/IPtite. Rarely.

In the past, various proposals have been made to prevent tartar, such as Japanese Patent Publication No. 45-23637 and Japanese Patent Publication No. 49 of 1973.
Japanese Patent Publication No. 27339 discloses many mesophosphonic acids, type compounds, and pharmaceutically acceptable salts thereof as tartar preventive agents. Also r Arch.

0ra1. Biol, Vol, 15, p, 8
9:3-896 (1970), the effectiveness of soluble phosphates against dental calculus, r Arch, 0
ra1. Biol, Vol. 20, p. 803
(1975)” contains magnesium ions (Mg”).
) has been shown to stabilize the precursors of hydroxyapatite and slow the rate of crystallization to hydroxyano and tight. Furthermore, JP-A-52-10802
No. 9 discloses poly-1717 acid salts (especially those with an average degree of polymerization of 2 to 2).
.

It has been disclosed that dental calculus can be prevented by combining 20) with polyvalent cations.

Summary of the Invention In addition to the above proposal, the present inventors have conducted intensive research into oral compositions that have even higher stability and more effectively suppress the formation of tartar over a long period of time. When one or more selected from silica, alumina, aluminum hydroxide and titanium oxide is blended into the composition as an abrasive, and linear sodium polyphosphate having an average degree of polymerization of 20 or more is blended, In particular, it has been found that the above object can be effectively achieved when the above sodium phosphate and a water-soluble polyvalent metal salt such as a water-soluble magnesium salt are used in combination.

That is, the sodium polyphosphate used in the present invention is represented by the following formula (1) % formula % (1) (where n (average degree of polymerization) is 20 or more). Sodium polyacrylates with an average degree of polymerization of 20 or more have higher stability in oral compositions than those with an average degree of polymerization lower than 20, and have excellent tartar preventive effects, and are also equally excellent. It has been found that this material has excellent compatibility with water-soluble polyvalent metal salts that have a tartar preventive effect. When blending into the above-mentioned sodium polyphosphate whole oral cavity composition, one or more of silica, alumina, aluminum hydroxide, and titanium oxide, which do not contain soluble Ca ions, is used as an abrasive, and the abrasive is used in combination with this abrasive. In this case, it is possible to obtain an oral composition in which the above-mentioned sodium polyacrylate is particularly stably blended, which reliably exhibits its soaked tartar preventive effect over a long period of time, and which acts effectively to prevent tartar formation over a long period of time. In addition, as mentioned above, sodium phosphate with an average degree of polymerization of 20 or more has excellent compatibility with water-soluble polyvalent metal salts, so when water-soluble polyvalent metal salts are further used together, We have found that since this is stably blended and reliably exhibits its effects, it is possible to obtain an oral composition that effectively prevents tartar formation over a long period of time, and has thus achieved the present invention. is.

Hereinafter, the present invention will be explained in detail.

Structure of the Invention The oral composition according to the present invention is prepared and applied as a dentifrice such as a toothpaste or a moisturizing toothpaste, and contains one or two selected from silica, alumina, aluminum hydroxide, and titanium oxide. The formation of abrasives and dental calculus is well suppressed.

In this case, as the silica, precipitated silica, Serodal in silica, Aerodel silica, igneous silica, etc. can be used. Specifically, Zoo of Hubsr, Inc.
49, Zeodent 113. USA W, R, Gr.
ace's 5yloid AL-1, 63, 74, 40
4. UK J.

Neosyl from Crossfled & 5ons
IT, Germany Deguagatl-5idsnt
3.20 etc. are mentioned.

Incidentally, in the present invention, polishing agents other than the above-mentioned silica, alumina, aluminum hydroxide, and titanium oxide may be blended, but in this case, soluble Ca2+ ions are not included at all, or their content is less than the effect of the present invention. It is preferable to use a small amount that does not cause t-inhibition.

In addition, the amount of abrasive compounded is 70% (wt%) of the entire composition.
(the same applies hereinafter) or less, particularly preferably from 5 to 40%.

Furthermore, the sodium polyphosphate used in the present invention has an average degree of polymerization of 20 or more, but particularly has an average degree of polymerization of 40 or more.
~70 is preferred. The average degree of polymerization is, for example, “Inorganic Chemistry Complete Book Y-69, edited by Shigeru Ohashi (1965), Maruzen,
It was determined by the terminal group determination method described in J.P., 50 J.

Here, the blending amount of sodium lyphosphate is not necessarily limited, but is preferably 0.601 to 10% of the total composition, especially 0.01% to 10% of the total composition.
It is preferably 1 to 5%.

Furthermore, water-soluble polyvalent metal salts can be effectively blended into the oral composition of the present invention since they have good compatibility with linear sodium polyphosphate having an average degree of polymerization of 20 or more, and can be effectively incorporated into the oral compositions of the present invention. The preventive effect can be further enhanced. In this case, polyvalent metal salts include chlorides, sulfates, acetates, nitrates, etc. of magnesium, barium, strontium, etc., and one or more of these may be used, but chlorides are particularly preferred. preferable. In addition, it is particularly preferable to use water-soluble magnesium salts, such as magnesium chloride anhydrous salt, magnesium chloride hexahydrate, magnesium sulfate heptahydrate, magnesium acetate tetrahydrate, magnesium nitrate hexahydrate, etc. A species or two or more species may be suitably used.

The amount of the water-soluble polyvalent metal salt to be blended is not particularly limited, but it is preferably 0.01 to 5%, particularly 0.01 to 2% of the total composition. Further, from the viewpoint of compatibility, it is preferable that the amount of the water-soluble polyvalent metal salt is less than or equal to the IA of the sodium polyphosphate.

As other components of the present invention, appropriate components commonly used may be blended depending on the type of oral composition, purpose of use, etc.

For example, in the case of an oral composition in the form of a paste such as a toothpaste, the binder may be carrageen 0nan, carboxymethyl cellulose sodium, methyl cellulose, hydroxyethyl cellulose, Cal? Cellulose visiting conductors such as sodium oxymethyl hydroxyethyl cellulose, alkali metal alginates such as sodium alginate, propylene glycol alinate, xanthan gum,
Tora gums such as canth gum, karaya gum, gum arabic, polyvinyl alcohol, sodium polyacrylate, cal? IWi or two or more of synthetic binders such as xyvinyl polymer and polyvinylpyrrolidone, and inorganic binders such as aluminum silica dal, beamam, and labnite may be blended (the amount usually ranges from 0.5 to 5%). ).

Furthermore, in the production of dentifrices and other oral compositions,
As a thickening agent, one or more of sorbitol, glycerin, ethylene glycol, glopylene glycol, 1,3-butylene glycol, ylcrytylene glycol, polypropylene dalycol, xylit, maltit, laftit, etc. may be blended (compounding). Amount usually 10-70%)
. In addition, water-soluble salts of higher alkyl sulfates whose alkyl group has 8 to 18 carbon atoms such as sodium lauryl sulfate and sodium myristyl sulfate, water-soluble higher fatty acid monoglyceride monoglycerides such as sodium 7-oil fatty acid monoglyceride monosulfate, etc. sulfates, alkylaryl sulfonates such as sodium dodecylbenzenesulfonate, higher fatty acid esters of higher alkyl sulfonic acids tX, anionic activators such as substantially saturated higher aliphatic acylamides of lower aliphatic aminocarganic acid compounds such as the sodium, potassium or ethanolamine salts of 4'lumitoyl sarcosine, fatty acid groups such as mono- and dilaurate sugars; carbon number is 12
~18 sucrose fatty acid ester, lactose fatty acid ester, lactitol fatty acid ester, maltitol fatty acid ester, stearic acid monoglyceride, prioxyethylene sorbitan monolaurate, polyoxyethylene sorbitan monostearate, polyoxyethylene (10, 20, (40, 60, 80, 100 mol) hydrogenated castor oil, a mixture of ethylene oxide 9 and pyrene oxide, and polyethylene oxide such as polyoxyethylene polyoxyglopyrene monolauryl ester, fatty acids, fatty alcohols, polyhydric alcohols, and One or more surfactants (compounding amount usually 0 to 7
%, preferably 0.5 to 5%).

The oral composition of the present invention includes furthermore, quince sodium, steviocydo, neohesberisol dihydrochalcone, glycyrrhizin, Kliraltin-thaumatin, asunoya 2-methylphenylalanine methyl ester, p-methoxycinnamic Aldehyde, nah! Sweeteners such as sugar, lactose, fructose, sodium cyclamate (0 to 1 t, preferably 0.01 to 0.5 t), and if necessary, oxysyl-hydroxymethylbenzoic acid, p-hydroxyethylbenzoic acid, Quacid, p-hydroxypropyl benzoic acid, p-hydroxydityl benzoic acid, sodium benzoate, preservatives such as lower fatty acid monoglycerides, wintergreen oil, suiamint oil, () f-mint oil, sweetsafras oil, cloves, Flavoring agents such as eucalyptus oil, gelatin, whitening agents (such as gum, arginine hydrochloride, albumin, casein, etc.), silicones, pigments, and other ingredients may be added. For example, in the case of toothpaste, the desired ingredients listed above may be added. It can be produced by mixing with an appropriate amount of water.

Moreover, when producing other oral compositions, they can be produced according to conventional methods using appropriate commonly used ingredients.

Furthermore, in the present invention, enzymes such as allantoin, ibusilone aminocaproic acid, tranexamic acid, dextranase, amylase, protease, mutanase, lysozyme, lytic enzyme, lyte, quendeime, sodium nofluorophosphate, potassium monofluorophosphate, etc. alkali metal monofluorophosphate, ), sodium chloride, ammonium fluoride, 7. Fluorides such as stannous oxide, chlorinone salts, dihydrocholesterol, glycyrrhetinic salts, glycyrrhetinic acid, glycerophosphate, chlorophyll, calopeptide, water-soluble inorganic phosphoric acid compounds, vitamins, other anti-tartar agents, antibacterial agents, One or more active ingredients such as plaque inhibitors may be included.

As described in detail, the oral composition of the present invention comprises an abrasive selected from silica, alumina, aluminum hydroxide, and titanium oxide, and linear sodium polyphosphate having an average degree of polymerization of 20 or more. By incorporating it, it is effective in preventing tartar formation over a long period of time. In addition, since the above-mentioned sodium I lyphosphate has excellent compatibility with water-soluble polyvalent metal salts, water-soluble polyvalent metal salts having a tartar preventive effect can be stably incorporated into the oral composition of the present invention. I'll go.

Next, an experimental example will be shown to concretely demonstrate the effects of the present invention. % water bath solution was prepared, and the pH was adjusted to 7 with an aqueous NaQH solution. After storing these aqueous solutions at room temperature, 40°C, and 50°C for 24 days, the amount of orthophosphoric acid liberated into the solution as a result of hydrolysis was determined by the molyzoden blue method, and the remaining amount of sodium I lyphosphate was determined. Examined. The results are shown in Table 1.

From the results shown in Table 1, it was found that poly-17 sodium phosphate having an average degree of polymerization of 56 had higher stability during storage than that having an average degree of polymerization of 16.

[Experimental Example 2] Aqueous solution containing 1.2% of polyphosphorus sodium hydroxide with an average degree of polymerization (n) of n-16 and 0.2% of magnesium chloride hexahydrate, and sodium lyphosphate with an average degree of polymerization (n) of n-56. Water-soluble coins containing 1.2% and 0.2% of 7ium magnesium chloride and 0.2% of magnesium chloride, respectively, were prepared, and the pH was adjusted to 7 with an aqueous NaOH solution. These aqueous solutions were stored at room temperature, 40° C., and 50° C. for the periods shown in Table 2, respectively, and then the formation of precipitates was investigated. Result X: Precipitate is formed.

○: No precipitate is formed, and the bath liquid is transparent.

From the results shown in Table 2, it was recognized that sodium polycarbonate having an average degree of polymerization of 56 was less compatible with water column magnesium salts than those having an average degree of polymerization of 16.

Examples are shown below.

[Example 1] Toothpaste precipitated silica 10% igneous silica 4185% glycerin
35 〃70% Sorbiy)
30//Polyethylene glycol 400
5 tt Sodium carboxymethylcellulose 0.41 Carrageenan
0.8/F Sodium lauryl sulfate
1.5〃I Sodium lyphosphate (average degree of polymerization n = 59) 1.5 p Sodium saccharin 0.1〃Fragrance 1.2〃 Sodium monofluorophosphate o, 8〃
Sperm water residual gold needle 100.0% [Example 2]
Toothpaste precipitated silica 15% igneous silica 3 Titanium oxide
0.5 85% glycerin 3
0 〃70 Thisolbit 30
〃I-lyethylene glycol 400
7 # Carboxymethyl cellulose sodium
1 Sodium lauryl sulfate
1.5〃Sodium polyphosphate (average degree of polymerization n=45) 0.5 psu, quince sodium 0.1〃Fragrance 1.
1. Chlorhexidine hydrochloride 0.1
[Example 3] Toothpaste aluminum hydroxide 25% igneous silica 3 〃70% sorbitol
30 Teriethylene glycol
400 5% Sodium carboxymethyl cellulose 0.8 α-olefin sulfone) 1,5
tt Sodium polyphosphate (average degree of polymerization n=59)
2.5 ttsu, quince sodium
o, 1〃Fragrance book〃 Tranegisamic acid 0. ．． 1 N
Purified water Balance wire 100.0% [Example 4] Toothpaste aluminum hydroxide 40% Igneous silica 1 70% Sorbit
35 Polyethylene glycol 400 5 p Sodium carboxymethyl cellulose 0.4 Carrageenan o, 3 Xanthan gum o, 3 Lau, sodium lylsulfate 1 Sodium polyphosphate (average degree of polymerization n = 59) 0.5
tt saccharin sodium 0.1
%Fragrance 1.1 Glycyrrhizin o, 1 Purified water
Balance meter 100.0 [Example 5] Toothpaste precipitated silica 20% igneous silica 3 Titanium oxide
5185% glycerin 251
70% sorbitol 23 N polyethylene glycol 400 3
tt Carrageenan o, 8 Sodium alginate o, 3 Sodium lauryl sulfate 1.7 Sodium polyphosphate (average degree of polymerization n = 45) l
p-saccharin sodium 0.1
#Fragrance IN Hydroxy Albanium Allantoin 0.
1# Magnesium chloride hexahydrate 0.2% purified water
Remaining balance 100.0% [Example 6] Toothpaste precipitated silica 25% Igneous silica 2 185% Glycerin
33 170% sorbitol
33 Sodium carboxymethyl cellulose 1 Sodium laurate
1.7 Sodium polyphosphate (
Average degree of polymerization n = 45) 1.5 p Sodium saccharin 0.1 Flavor
1 〃 Ibushironoa 5 Tsukaproic acid 0.1〃
Magnesium chloride hexahydrate 0.2
Purified water balance meter 100.0% [Example 7
] Toothpaste Precipitated Silica 20% Igneous Silica 3 Titanium Oxide
31 85% glycerin 33 170% Sorbi,) 33 #Carboxymethylcellulose sodium O65〃
Carrageenan 0.5 α-olefin sulfonate 1 Sodium polyphosphate (average degree of polymerization n=59) 2
N-saccharin sodium 0.
1.Fragrance 1.Sodium fluoride 0.22//Magnesium chloride hexahydrate 0.3.Purified water Balance meter 100.0% [Example 8]
Toothpaste precipitated silica 25% large-scale silica 3 85 tiglycerin 38% 70% sorbitol, triglyceride
19 /I Sodium Caldexymethyl Cellulose 0.51 Carrageenan
0.5 Sodium lauryl sulfate
l, 5 Sodium polyphosphate (average degree of polymerization n = 45) 2 tt Sodium saccharin o, 1 Flavor 1.1
〃 Magnesium chloride hexahydrate o, 2〃Purified water Balance meter 100.0% [Example 9
]Toothpaste Precipitated Silica 3o% Igneous Silica 3185% Glycerin
19170% sorbitol
38 Sodium R-xymethylcellulose
1 〃Rau, Sodium Ryl Sulfate
1.5〃Sodium polyphosphate (average degree of polymerization n = 59) '; l, 5 tt Sodium saccharin 0.1% Flavor
1.1〃 Magnesium chloride hexahydrate o, 5〃Purified water Remaining total 100.0'ch Example 1 ~
To make the toothpaste in step 9, use a spring from which tartar has been removed.
After using it for a month, the accumulation of tartar was suppressed in all cases. 3 Applicant: Lion Corporation Representative: Takashi Kojima
4 Procedural amendment (voluntary) July 16, 1985, indication of the case 1988 Patent Application No. 272392, name of the invention Oral composition, person making the amendment Relationship with the case Patent applicant Place Tokyo 1-3-7 Honjo, Sumida-ku Name (676) Lion Co., Ltd. Representative Atsushi Kobayashi, Agent 104 Address 5th floor, Dapa Create Building, 3-11-14 Ginza, Chuo-ku, Tokyo Telephone (545) 64546, Contents of amendment (2) "Sodium polyacrylate" in the second line from the bottom of page 4 and in line 9 of page 5 of the specification are both changed to "sodium polyphosphate." I am corrected.

(3) “Sodium laurate”, page 20, line 10
Correct the text to read ``sodium lauryl sulfate.''

that's all

Claims (1)

[Claims] 1. Contains one or more abrasives selected from silica, alumina, aluminum hydroxide, and titanium oxide, and linear sodium polyphosphate having an average degree of polymerization of 20 or more. An oral composition characterized by: 2. The oral composition according to claim 1, wherein the sodium polyphosphate has an average degree of polymerization of 40 to 70. 3. The amount of sodium polyphosphate in the entire composition is 0.
The oral composition according to claim 1 or 2, which contains 1 to 5% by weight. 4. The oral cavity composition according to any one of claims 1 to 3, which contains a water-soluble polyvalent metal salt. 5. The oral composition according to claim 4, wherein the water-soluble polyvalent metal salt is a water-soluble magnesium salt. 6. The amount of water-soluble polyvalent metal salt is 0.01 of the total composition
The oral composition according to claim 4 or 5, wherein the amount is 2% by weight.