JPH0461845B2 - - Google Patents

Description

[Detailed description of the invention]

INDUSTRIAL APPLICATION FIELD The present invention relates to an oral composition containing a stannous compound and a myo-inositol phosphate or a salt thereof and having a high caries preventive effect. Prior art and its problems When caries occurs, lactic acid is first generated as a metabolic product of bacteria such as S. mutans, and the acid dissolves hydroxyapatite on the tooth surface, forming partially softened enamel. When this softened enamel part is viewed with the naked eye, it appears cloudy (white spot). As caries progresses further, cavities develop in the teeth, which require treatment by a dentist. Therefore, if the softened enamel can be restored to a healthy tooth at this white spot stage (remineralization), it can greatly contribute to caries prevention. In addition, in the process of forming white spots (initial caries), acids elute Ca and P from the tooth surface, but drugs with remineralization ability have the effect of restoring the eluted Ca and P. Therefore, drugs with high remineralization ability naturally have the ability to prevent early dental caries. Conventionally, oral compositions containing a stannous compound such as stannous fluoride and myo-inositol phosphate or a salt thereof have been known as oral compositions that effectively prevent such early dental caries. (Special Publications No. 58-35965, No. 58-46483, No. 58-46484, etc.). However, according to studies by the present inventors, a system containing a stannous compound and a myo-inositol phosphate or a salt thereof has a strong sour taste. Since oral compositions are used in the oral cavity, they are desired to have a good taste. It is unfavorable in terms of feel when used, and therefore, from a practical standpoint, it is strongly desired to improve the sourness and improve the feel when used. SUMMARY OF THE INVENTION In view of the above circumstances, the present inventors conducted intensive research on improving the sour taste of systems containing stannous compounds, myo-inositol phosphate esters or salts thereof, and found that fatty acid alkanolamide and protein When combined with
It was discovered that the acidity of a system containing a tin compound, myo-inositol phosphate ester or a salt thereof is improved, and the usability is improved, leading to the present invention. The present invention will be explained in more detail below. Structure of the Invention The oral composition of the present invention is used as a toothpaste, a dentifrice such as a dentifrice, a mouthwash, etc.
It is made by blending fatty acid alkanolamide and protein with a stannous compound, myo-inositol phosphate ester or its salt. Here, as the stannous compound, soluble stannous
A tin compound or a sparingly soluble stannous compound may be used, or a soluble stannous compound and a sparingly soluble stannous compound may be used in combination. In this case, the soluble stannous compounds include stannous fluoride, stannous chloride, stannous chloride, stannous fluoride, stannous acetate, sodium stannous fluoride, and stannous fluoride.
Potassium tin, tin hexafluorozirconate,
One or more of stannous sulfate, stannous tartrate, stannous gluconate, etc. can be used. In addition, examples of poorly soluble stannous compounds include stannous pyrophosphate, stannous metaphosphate, stannous oxide, stannous oxalate,
One or more types of stannous phosphate can be used. Among these, stannous fluoride is particularly preferably used. The content of these stannous compounds is such that the stannous ions solubilized in the composition account for 0.03% of the total composition.
(% by weight, the same applies hereinafter) or more, particularly preferably 0.1% or more. In addition, the first
There is no particular upper limit to the amount of the tin compound blended, and there is no problem even if a part of the blended stannous compound precipitates in the composition and remains in an unresolved state, but solubilized stannous ions is less than 7% of the total composition, especially 5% of the total composition.
% or less. Here, when a soluble stannous compound and a poorly soluble stannous compound are used together, the composition is prepared by using the soluble stannous compound (in this case, this compound mainly serves as a source of dissolved stannous ions) as tin. Medium 0.03% or more, especially 0.1% or more,
A poorly soluble stannous compound (in this case, the precipitated poorly soluble stannous compound is a “reservoir” of stannous ions)
0.2 to 10 of tin
% is preferable. In addition, as myo-inositol phosphate ester, those obtained by converting 1 to 6 hydroxyl groups of myo-inositol into phosphoric esters are used, but in particular, 4 to 6 hydroxyl groups are used.
Preferably used are those obtained by phosphoric acid esterification of 6 molecules, that is, myo-inositol hexaphosphate, myo-inotosyl pentaphosphate, and myo-inositol tetraphosphate. As a salt of myo-inositol phosphate ester, a salt in which some or all of the hydrogen atoms of the phosphate group of myo-inositol phosphate ester are replaced with a metal group, etc. can be used, and the types of salts include sodium salt, potassium salt, etc. salts, ammonium salts, calcium salts, magnesium salts, aluminum salts, barium salts and the like. Among these, penta and hexasodium salts, penta and hexapotassium salts, tetracalcium salts, pentamagnesium salts, pentabarium salts, etc. can be particularly preferably used, and double salts are also used, but those with high solubility in water are preferred, and alkali metal salts and ammonium salts are most preferably used. In addition, in the present invention, the above-mentioned myo-inositol phosphate ester and its salt may be used alone or in combination of two or more thereof. The amount of myo-inositol phosphate and its salts is preferably 0.05% or more, more preferably 0.1 to 20%, and even more preferably 0.2 to 10% of the total composition. The amount of myo-inositol phosphate and its salts is 0.01 to 4 mol, more preferably 0.02 to 3 mol, and even more preferably 0.03 to 2.5 mol per mol of stannous ion solubilized in the product. It is preferable to In the present invention, fatty acid alkanolamide and protein are blended in addition to the above-mentioned components, thereby improving the acidity of a system containing a stannous compound, myo-inositol phosphate ester, or a salt thereof. Here, examples of the fatty acid alkanolamide include capric acid monoethanolamide, lauric acid diethanolamide, myristic acid diethanolamide, palmitic acid diethanolamide, coconut oil fatty acid diethanolamide, and lauric acid monoisopropanolamide. Fatty acid alkanolamides having 8 to 18 carbon atoms and in which the alkanol group has 2 or 3 carbon atoms are preferably used. In addition, the fatty acid may be saturated or unsaturated, may be linear or have a molecular chain, and may even be a mixed fatty acid. The amount of fatty acid alkanolamide is
It is preferably 0.05 to 5%, particularly 0.3 to 3%. If the amount is less than 0.05%, acidity may not be improved satisfactorily, and if it is more than 5%, storage stability may be impaired. Examples of proteins include gelatin, ovalbumin, casein, and peptone, and one or more of these can be used. The blending amount thereof is preferably 0.01 to 10%, particularly 0.1 to 5% of the total composition. Note that the oral composition of the present invention may further contain a fluorine compound, thereby further improving the caries preventive effect. That is, by adding fluorine to the combination of stannous ions and myo-inositol phosphate or its salt in the present invention, the uptake of fluorine into teeth is significantly increased compared to conventional fluorine-containing oral compositions. Furthermore, with conventional fluorine-containing compounds, the appearance of fluoride incorporated into the teeth is often simply due to the precipitation of calcium fluoride on the surface layer of the teeth. However, in the present invention, fluorine is not precipitated as calcium fluoride on the tooth surface layer, but can be allowed to penetrate into the inside of the tooth. Therefore, in the present invention, the presence of fluorine allows a large amount of fluorine to be incorporated into the tooth surface without forming a precipitate of calcium fluoride, thereby fully utilizing the remineralizing ability of fluorine on the tooth. It is possible. In this case, as the fluorine compound, the above-mentioned fluorine-containing stannous tin compound can be used to simultaneously blend the stannous tin content and the fluorine content, but a fluorine compound that does not contain the stannous content , for example, sodium fluoride, potassium fluoride, lithium fluoride, ammonium fluoride, sodium monofluorophosphate, sodium monofluorohydrogenphosphate, potassium monofluorophosphate, ammonium monofluorophosphate, potassium hexafluorozirconate,
One or two of potassium hexafluorotitanate, etc.
species or more can be suitably used, and cesium fluoride,
Aluminum fluoride, copper fluoride, lead fluoride, iron fluoride, nickel fluoride, zirconium fluoride, silver fluoride, as well as hexylamine hydrofluoride, laurylamine hydrofluoride, cetylamine hydrofluoride, glycine hydrofluoride Fluoride, lysine hydrofluoride, alanine hydrofluoride, etc. may also be used. The fluorine content is desirably blended into the oral composition so that the total fluorine concentration is preferably 50 to 10,000 ppm, more preferably 200 to 10,000 ppm. When manufacturing a dentifrice, the total amount of fluorine is preferably 1000 ppm or less. As other components of the present invention, appropriate components are used depending on the type of oral composition. For example, in the case of toothpaste, dibasic calcium phosphate dihydrate and anhydride, calcium carbonate, calcium pyrophosphate, insoluble sodium metaphosphate, silica-based abrasives such as amorphous silica and aluminosilicate, aluminum oxide, water Abrasives such as aluminum oxide, microcrystalline cellulose, resin, tertiary magnesium phosphate, magnesium carbonate, etc. (compounding amount is usually 10-90% of the total, especially in the case of toothpaste)
20-60%) may be blended. In addition, when using a silica-based abrasive as an abrasive, Hi-sil T-600 (U.S.
PPG INDUSTRES), Silcron G-100F,
Silcron G-910 (GLIDDEN, USA)
PIGMENTS), Gasil 23TP, Gasil 200TP
(Joseph Crosfield, USA), Sident 12,
Sident 12DS (West German DEGGUSSA),
Tix-o-sil 53 (RHONE POULENC, France),
Syloid 244, Syloid Sylopore 35, Syloid 63 (Fuji Deiveson), Syloid 81,
Syloblance 82 (Grace, USA), Zeodent
113, Zeo 49 (manufactured by HUBER, USA), etc. are preferably used. In the case of paste or gel compositions such as toothpaste, binders such as carrageenan, cellulose derivatives such as sodium carboxymethyl cellulose, alkali metal alginates such as sodium alginate, gums such as xanthan gum, and polyvinyl alcohol are used as binders. One or more types of inorganic binders such as synthetic binders, gelatinous silica, vegum, gelatinous aluminum silicate, etc. may be blended (compounding amount usually 0.3 to 5%). Furthermore, the paste,
In the case of gel or liquid compositions, sorbitol, glycerin, ethylene glycol,
One or more of propylene glycol, 1,3-butylene glycol, polyethylene glycol, xyrite, maltite, lactite, etc. may be blended (the blending amount is usually 10 to 70%). Furthermore, the oral composition of the present invention may contain essential oils such as peppermint and spearmint, l-menthol, carvone, eugenol, etc. as fragrances, if necessary.
Flavoring materials such as anethole may be blended singly or in combination at a rate of 0.1 to 5% of the total, and sweeteners such as saccharin sodium, stevioside, neohesperidyl dihydrochalcone, glycyrrhizin, perillartine, p-methoxycinnamic aldehyde, etc. agents and other ingredients may be added. In addition, in the present invention, 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, sodium lauryl monoglyceride sulfonate, sodium coconut monoglyceride sulfonate, etc. The number of carbon atoms in the fatty acid group is 10~
Water-soluble salt of higher fatty acid monoglyceride sulfonate, higher fatty acid sodium monoglyceride monosulfate, sodium-N-methyl-
N-palmitoyl tauride, sodium-N-lauroyl sarcosinate, sodium-N-lauroyl-β-alanine, etc., whose fatty acid group has 12 or more carbon atoms
Anion activators such as salts of amides of higher fatty acids and lower aliphatic amino acids, sucrose fatty acid esters and lactose fatty acid esters in which the fatty acid group has 12 to 18 carbon atoms, such as stearyl monoglyceride, sucrose mono- and dilaurate. , lactitol fatty acid ester, maltitol fatty acid ester, sorbitan monostearate condensate with about 60 moles of ethylene glycol added, a polymer of ethylene oxide and propylene oxide, and derivatives such as polyoxyethylene polyoxypropylene monolauryl ester and other nonions. One or more surfactants such as surfactants, betaine type, amino acid type etc.
7%, especially 0.1 to 4%). Furthermore, as active ingredients, in addition to the stannous compound and myo-inositol phosphate ester or its salt, enzymes such as dextranase, amylase, protease, mutanase, lysozyme chloride, and lytic enzyme, chlorhexidine salts, epsilon aminocaproic acid,
Tranexamic acid, sorbic acid, alexidine, hinokitiol, cetylpyridinium chloride,
Water-soluble inorganic phosphoric acid compounds such as alkylglycines, alkyldiaminoethylglycine salts, aluminum chlorohydroxylalantoin, dihydrocholesterol, glycyrrhizin salts, glycerophosphate, sodium chloride, sodium bromide, water-soluble primary or secondary phosphates, One or more types of active ingredients such as quaternary ammonium compounds may be blended. The oral composition of the present invention is prepared using the above-mentioned appropriate ingredients, and in this case, the composition has a pH of 3 to 3.
8, particularly preferably 4 to 6.5. Effects of the Invention The oral composition according to the present invention can improve acidity when used in the oral cavity by using a stannous compound, a myo-inositol phosphate ester or a salt thereof together with a fatty acid alkanolamide and a protein. It is something that Next, Examples and Comparative Examples will be shown to specifically explain the effects of the present invention. In addition, in the following examples, PH was adjusted using sodium hydroxide or hydrochloric acid. Examples 1 to 5, Comparative Examples 1 to 3 A mouthwash with the formulation shown in Table 1 was prepared, and the sourness when gargling for 3 minutes with this mouthwash was 10.
Sensory evaluation was conducted by a specialized panel of experts. The results are also listed in Table 1.

[Table] From the results in Table 1, the stannous compound and myo-inositol phosphate ester type gave a sour taste when used in the oral cavity, but by adding fatty acid diethanolamide and protein to it, It was found that acidity can be improved. Example 6 Mouthwash Stannous chloride dihydrate 1.5% Sodium fluoride 0.66 Myo-inositol tetraphosphate 5Na 2.0 Peppermint fragrance 0.02 Sodium saccharin 0.01 Ethanol 10.0 Sodium lauryl sulfate 1.0 Lauric acid diethanolamide 1.0 Gelatin 0.7 Water balance 100.0% Example 7 Mouthwash Stannous chloride dihydrate 1.5% Sodium fluoride 0.66 Myo-inositol tetraphosphate 5Na 2.0 Peppermint fragrance 0.02 Sodium saccharin 0.01 Ethanol 10.0 Sodium lauryl sulfate 1.0 Lauric acid diethanolamide 1.0 Gelatin 1.2 Water remaining 100.0% Example 8 Toothpaste gelatin 0.5% Myristate diethanolamide 1.0 Stannous fluoride 0.4 Myo-inositol pentaphosphate 5Na 2.0 Sodium lauryl sulfate 2.0 Propylene glycol 3.0 Glycerin 20.0 Xanthan gum 0.4 Carrageenan 0.8 Silica airgel 3.0 Hydroxylation Aluminum 30.0 Satucalin sodium 0.2 Wintergreen fragrance 1.0 Water Remaining 100.0% PH=4.5 Example 9 Toothpaste casein 0.5% Lauric acid diethanolamide 1.0 Stannous chloride dihydrate 1.5 Sodium fluoride 0.66 Myo-inositol hexaphosphate 12Na 1.0 Myristyl Sodium sulfate 2.0 Propylene glycol 3.0 Sorbit (60%) 35.0 Sodium carboxymethyl cellulose 1.5 Silica airgel 3.0 Insoluble sodium metaphosphate 40.0 Sodium saccharin 0.2 Peppermint flavor 1.0 Water remaining 100.0% PH=5.0 Example 10 Toothpaste gelatin 0.5% Palm Oil fatty acid diethanolamide 1.0 Stannous fluoride 0.4 Myo-inositol tetraphosphate 5NH ₄ 2.0 Sodium myristyl sulfate 1.5 Propylene glycol 2.0 Sorbit (60%) 40.0 Sodium carboxymethylcellulose 0.6 Carrageenan 0.6 Silica airgel 2.0 Aluminum hydroxide 3.0 Sodium saccharin 0.2 Spearmint fragrance 1.0 Water Remaining 100.0% PH=5.0 Example 11 Toothpaste gelatin 0.5% Myristic acid diethanolamide 1.0 Stannous fluoride 0.4 Myo-inositol pentaphosphate Ca 1.5 Myo-inositol hexaphosphate Mg 0.5 Sodium lauryl sulfate 2.0 Propylene glycol 3.0 Glycerin 30.0 Sodium carboxymethylcellulose 0.5 Hydroxyethylcellulose 0.5 Aluminum hydroxide 40.0 Sodium saccharin 0.2 Spearmint fragrance 1.0 Water Remaining 100.0% PH=5.0 Example 12 Toothpaste casein 0.5% Lauric acid diethanolamide 1.2 Stannous chloride dihydrate 1.2 Sodium fluoride 0.3 Myo-inositol pentaphosphate 5K 1.0 Sodium lauryl sulfate 1.5 Propylene glycol 3.0 Glycerin 30.0 Carrageenan 1.5 Silica airgel 3.0 Aluminum hydroxide 40.0 Sodium saccharin 0.2 Peppermint flavor 0.5 Spearmint flavor 0.5 Water Remaining 100.0% PH= 4.5 Example 13 Toothpaste gelatin 0.5% Lauric acid diethanolamide 1.0 Stannous fluoride 0.4 Myo-inositol pentaphosphate 10Na 1.0 Sodium lauryl sulfate 2.0 Propylene glycol 3.0 Glycerin 30.0 Sodium carboxymethyl cellulose 1.5 Silica erogel 3.0 Silica-based abrasive (Zeodent 113) 25.0 Titanium oxide 1.0 Satucharin sodium 0.2 Spearmint flavor 1.0 Water Remaining 100.0% PH=5.0 Example 14 Toothpaste gelatin 0.5% Myristate diethanolamide 1.5 Stannous fluoride 0.4 Myo-inositol pentaphosphate 10Na 1.0 Myo-inositol hexaphosphate 12NA 0.5 Lauril sodium sodium sulfate 2.0 propylene glycol 3.0 Sorbitzo 40.0 Calvoxymethylcerus Snatrium 1.5 silica erogel 3.0 silica -based abrasive (SILCRON G -910) 30.0 Titanium 1.0 Satsukarin Snatrium 0.2 Spearmint fragrances 1.0 Water remaining 100.0 % pH = 5.5 Examples 15 Toothpaste casein 0.6% Lauric acid diethanolamide 1.0 Stannous chloride dihydrate 1.5 Sodium fluoride 1.66 Myo-inositol tetraphosphate (acid) 1.5 Sodium myristyl sulfate 2.0 Propylene glycol 3.0 Sorbiturate 40.0 Xanthan gum 0.4 Carrageenan 0.8 Silica airgel 2 .0 Silica-based abrasive (Gasil 23TP) 35.0 Titanium oxide 1.0 Satucharin sodium 0.2 Peppermint flavor 0.5 Spearmint flavor 0.5 Water Remaining 100.0% PH=4.5 Example 16 Toothpaste casein 0.5% Lauric acid diethanolamide 1.0 Stannous fluoride 0.4 Myo-inositol pentaphosphate 5Na 1.0 Myo-inositol hexaphosphate 5Na 1.0 Sodium myristyl sulfate 2.0 Propylene glycol 3.0 Glycerin 30.0 Hydroxyethyl cellulose 1.2 Silica airgel 3.0 Silica-based abrasive (Zeo 49) 25.0 Titanium oxide 1.0 Satucalin sodium 0.2 Spearmint flavor 1 .0 Water Remaining 100.0% PH=6.0 Example 17 Toothpaste gelatin 0.7% Lauric acid diethanolamide 1.5 Stannous fluoride 0.4 Myo-inositol pentaphosphate (acid) 3.0 Sodium lauryl sulfate 1.8 Propylene glycol 3.0 Glycerin 30.0 Carrageenan 1.2 Silica airgel 3.0 Silica-based abrasive (Zeodent 113) 30.0 Titanium oxide 1.0 Sodium saccharin 0.2 Wintergreen flavoring 1.0 Water Remaining 100.0% PH=4.5 Examples 5 to 16 all had good acidity improvement and excellent abrasiveness. It has an anti-erosion effect. In addition, in Example 16, instead of the silica-based abrasive (Zeodent 113) used there,
Even if other silica-based abrasives are used as described on page 1, acidity can be improved satisfactorily.

Claims (1)

[Scope of Claims] 1. An oral composition comprising a fatty acid alkanolamide and a protein added to an oral composition containing a stannous compound and a myo-inositol phosphate or a salt thereof. 2. The oral composition according to claim 1, which contains fluorine.