JP4535215B2 - Oral composition and method for improving stabilization of ascorbic acid ester or salt thereof in oral composition - Google Patents

Description

[0001]
BACKGROUND OF THE INVENTION
The present invention relates to a composition for oral cavity in which the residual rate of ascorbic acid ester or a salt thereof is prevented from decreasing over time, and a method for improving the stabilization of ascorbic acid ester or a salt thereof in the oral composition .
[0002]
[Prior art and problems to be solved by the invention]
Ascorbic acid and its derivatives are known as active ingredients for the prevention and treatment of periodontal diseases, and various oral compositions containing ascorbic acid and its derivatives have been proposed (Japanese Patent Laid-Open No. 62-96408). 62-273910, JP-A-1-21520, 4-217616, 4-217617, 4-217618, and 4-275213.
[0003]
However, when ascorbic acid and its derivatives are blended into an oral composition, there is a problem that the residual rate decreases with time. For this reason, development of a technique for stably blending ascorbic acid and its derivatives into an oral composition has been made. desired.
[0004]
In this case, the composition for oral cavity containing ascorbic acid or a derivative thereof has a problem of discoloration of the composition. Proposals for suppressing this discoloration (Japanese Patent Laid-Open Nos. 52-79032 and 63-141921, (Kaihei 3-127720) is also various, but these proposals suppress the degradation of ascorbic acid and its derivatives, which are thought to be the cause of the discoloration, and prevent the residual rate from being lowered. It is different from measuring stability.
[0005]
Accordingly, the present invention can prevent a decrease in residual ratio with time of the ascorbic acid ester or salt thereof, ascorbic in ascorbic acid ester or oral composition a salt thereof is blended stabilizing and oral compositions It aims at providing the stabilization improvement method of acid ester or its salt .
[0006]
Means for Solving the Problem and Embodiment of the Invention
In order to achieve the above-mentioned object, the present inventor has intensively studied to improve the storage stability of ascorbic acid esters or salts thereof, and as a result, any hydroxyl group at 2, 3, 5, 6 position of ascorbic acid. When an amine compound having two or more hydroxyl groups is added to an oral composition containing an ascorbic acid ester or a salt thereof in which one or more of the above becomes an ester of phosphoric acid or sulfuric acid, an ascorbic acid ester Or it became difficult for the residual rate of the salt to fall, and it discovered that it was effective in stabilization, and came to make this invention.
Therefore, this invention provides the stabilization composition improvement method of the ascorbic acid ester or its salt in the following oral cavity composition and oral cavity composition.
Claim 1; (A) An oral cavity containing an ascorbic acid ester or a salt thereof in which one or more of the hydroxyl groups at positions 2, 3, 5, and 6 of ascorbic acid are esters of phosphoric acid or sulfuric acid. A composition for oral cavity, wherein (B) an amine compound having two or more hydroxyl groups selected from (B) diethanolamine, triethanolamine, N-ethyldiethanolamine, dipropanolamine, and tripropanolamine is added to the composition for use. object.
[2] The composition for oral cavity according to [1], wherein (B) an amine compound having two or more hydroxyl groups is blended as a stabilizer for the component (A).
Claim 3; (A) Ascorbic acid ester is claim 1, characterized in that became 1 or 2 Tsugarin acid or ester of sulfuric acid 2,3-position or the hydroxyl groups of the ascorbic acid Or the composition for oral cavity of 2.
[4] The composition for oral cavity according to [1], [2] or [3], wherein the ascorbic acid ester is one in which the hydroxyl group of ascorbic acid is an ester of phosphoric acid.
[ 5] The blending amount of the component (A) is 0.01 to 5% by mass, and the blending amount of the component (B) is 0.1 to 5% by mass . The composition for oral cavity according to Item 1 .
The oral composition according to any one of claims 1 to 5, characterized in that is prepared as a dentifrice, claim 6.
Claim 7; (A) the oral cavity containing one or more ascorbic acid ester or salt thereof became esters of phosphoric acid or sulfuric acid or the hydroxyl groups at position 2,3,5,6 ascorbate to use the composition, (B) diethanolamine, triethanolamine, N- ethyl-diethanolamine, di-propanolamine, blending an amine compound having two or more hydroxyl groups selected from tripropanolamine as a stabilizer of component (a) A method for improving the stability of an ascorbic acid ester or a salt thereof in the composition for oral cavity.
[0007]
Hereinafter, the present invention will be described in more detail.
The composition for oral cavity of this invention contains ascorbic acid ester or its salt . In this case, as the ascorbic acid ester or salt thereof, one or more phosphoric acid or a hydroxyl group of 2,3,5,6-position of ascorbic acid is that a ester of sulfuric acid can be used. Examples include ascorbic acid-2-phosphate, ascorbic acid-3-phosphate, ascorbic acid-6-phosphate , ascorbic acid-2-sulfate, and the like . In addition, examples of the salts include sodium salts, potassium salts, calcium salts, and magnesium salts.
[0008]
These ascorbic acid and its derivatives can be blended in one or a combination of two or more, and among the ascorbic acid derivatives, the hydroxyl group at the 2- or 3-position of ascorbic acid is esterified particularly from the viewpoint of the stability of the composition. Are preferably used.
[0009]
The compounding amount of the ascorbic acid ester or a salt thereof is preferably 0.001 to 10% (mass percentage, the same applies hereinafter), particularly 0.01 to 5% of the entire composition. If the amount is less than 0.001%, the effect may not be sufficient, while if it exceeds 10%, the feeling of use of the oral composition may be adversely affected.
[0010]
In the composition for oral cavity of this invention, the amine compound which has a 2 or more hydroxyl group is mix | blended as a stabilizer of ascorbic acid ester or its salt . Examples of the amine compound include diethanolamine, triethanolamine, N-ethyldiethanolamine, dipropanolamine, and tripropanolamine. The compounding quantity of these amine compounds can be mix | blended in the range of 0.001-10% of the whole composition, and it is desirable to mix | blend especially 0.1-5%. In this case, the amine compound is desirably blended in an amount of 1 to 25 parts by weight with respect to 1 part by weight of ascorbic acid ester or a salt thereof .
[0011]
The oral composition of the present invention is, for example, a toothpaste, a liquid dentifrice, a liquid dentifrice, a dentifrice such as a toothpaste, a powder dentifrice, a mouthwash, a tablet, a mouth freshener, a chewing gum, a pasta, It is suitably prepared as a denture cleaning agent or the like, and other additives can be blended as optional components in addition to the essential components according to the dosage form.
[0012]
That is, when used for dentifrice, it can be produced by mixing components such as abrasives, thickeners, sweeteners, preservatives, dyes, pH adjusters, various active ingredients, fragrances and solvents.
[0013]
Here, as abrasives, silica-based abrasives such as precipitated silica, silica gel, aluminosilicate, zirconosilicate, aluminum hydroxide, calcium hydrogen phosphate dihydrate and anhydrous salts, calcium pyrophosphate, sodium metaphosphate, hydroxy Apatite, heavy and light calcium carbonate, zirconium silicate, alumina, magnesium carbonate, tribasic magnesium phosphate, synthetic resin abrasive and the like are preferably used.
[0014]
Also thickeners such as glycerin, sorbit, propylene glycol, polyethylene glycol, xylit, malt, lactit, sodium carboxymethylcellulose, carrageenan, sodium alginate, sodium polyacrylate, carbopol, hydroxyethylcellulose, hydroxypropylcellulose, methylcellulose, montmorillonite , Gua gum, Bee gum, Toraya gum, Arabic gum, Locust bean gum, Gelatin, Polyvinyl alcohol, Polyvinyl pyrrolidone, Copolymers of methoxyethylene and maleic anhydride, Laponite, Thickening silica and other binders, Fatty acids, Direct Chain alkylbenzene, alpha olefin, normal paraffin, and higher alcohol anionic surfactants, sucrose fatty acid ester Nonionic surfactants such as tellurium, fatty acid alkanolamide, polyglycerin fatty acid ester, polyoxyethylene alkyl ether, polyoxyethylene fatty acid ester, polyoxyethylene hydrogenated castor oil, polyoxyethylene polyhydric alcohol fatty acid ester, sorbitan fatty acid ester, imidazoline -Based, betaine-based zwitterionic surfactants, amine-based, quaternary ammonium salt-based anionic surfactants, foaming agents and foaming aids, saccharin sodium, stevioside, stevia extract, paramethoxycinnamic aldehyde, neohe Sweeteners such as superidyl dihydrochalcone, perilartin, aspartylphenylalanine methyl ester, thaumatin, palatinose, licorice powder, paraoxybenzoic acid ester, sodium benzoate Preservatives such as lower fatty acid monoglyceride and p-hydroxybenzoic acid, Blue No. 1, Blue No. 2, Blue No. 201, Blue No. 205, Green No. 3, Green No. 201, Green No. 202, Green No. 204, Yellow No. 4 Substances having pH buffering action such as yellow No. 5, yellow No. 203, red No. 2, red No. 213, caramel dyes, dyes such as titanium dioxide, alkali metal salts of orthophosphoric acid, alkali metal salts of citric acid, etc. Other examples include pH adjusters composed of acids and alkalis such as hydrochloric acid and sodium hydroxide, fragrances such as terpenes such as l-menthol, carvone, limonene and anethole or derivatives thereof, and solvents such as water, ethanol and cetanol. The
[0015]
Various active ingredients include fluorides such as sodium fluoride, stannous fluoride, potassium fluoride, ammonium fluoride, sodium monofluorophosphate, allantoin, allantochlorohydroxyaluminum, glycyrrhizic acid and its salts, acetic acid and nicotine Tocopherol acid, zeolite, sodium polyphosphate, sodium pyrophosphate, tranexamic acid, epsilon aminocaproic acid, 4-aminomethylcyclohexanecarboxylic acid, β-glycyrrhetinic acid, lysozyme chloride, α-bisabolol, ibuprofen, azulene, sodium guaiazulene sulfonate, epi Dihydrocholesterin, taurine, sodium chloride, dextranase, mutanase, amylase, lytic enzyme, aluminum lactate, strontium chloride, potassium nitrate, Dihydrocholestanol, trichlorocarbanilide, berberine-containing plant extracts such as Citrus and Ranunculaceae extracts, soft sugar beet extract, duckweed, clove, oxon, rosemary, safflower, chamomile, rutin or Its derivatives, hydroxamic acid and its derivatives, copper chlorophyllin sodium, baking soda, zinc citrate, halogenated diphenyl ether, isopropylmethylphenol, thymol, hinokitiol, cetylpyridinium chloride, benzethonium chloride, benzalkonium chloride, decalinium chloride, hydrochloric acid and gluconic acid Examples include chlorhexidine and the like.
[0016]
In addition, since ascorbic acid and its derivative are easily oxidatively decomposed, it is desirable not to add an oxidizing agent such as peroxide.
[0017]
In addition to the above, liquid paraffin, microcrystalline wax, paraffin wax, starch, corn starch, and other ingredients used in oral compositions other than dentifrices, such as mouthwashes, denture stabilizers, oral pasta, mouth fresheners, etc. , Lactose, powdered sugar, gum base, starch syrup and the like.
[0018]
In addition, the compounding quantity of these arbitrary components can be made into a normal quantity in the range which does not prevent the effect of this invention.
[0019]
The composition for oral cavity of the present invention is a tube such as an aluminum laminated tube or a glass-deposited plastic tube as a container, a dispenser container by mechanical or differential pressure, a film packaging container such as pillow packaging, injection, hollow, press, vacuum It is also possible to fill a bottle or the like formed by molding.
[0020]
【The invention's effect】
The composition for oral cavity of the present invention is highly stable because the ascorbic acid ester or a salt thereof is prevented from decreasing in the residual rate over time.
[0021]
【Example】
EXAMPLES Hereinafter, although an experiment example and an Example are shown and this invention is demonstrated concretely, this invention is not restrict | limited to the following Example.
[0022]
[Experimental example]
A dentifrice formulated with the following dentifrice base and the following amine compound or a glycol having a similar structure as a comparison, and a blank preparation as a control were prepared. 90 g of each of these 6 compositions of dentifrice was placed in an aluminum laminated tube and stored in a constant temperature bath at 40 ° C., and the residual rate of ascorbic acid phosphate magnesium salt after 6 months was measured. The results are shown below.
[0023]
Dentifrice base <br/> 3% propylene glycol
Carboxymethylcellulose 2%
Paraben 0.8%
Ascorbic acid phosphate magnesium salt 0.1%
Saccharin sodium 0.2%
Sorbit 30%
Silicic anhydride 15%
Fragrance 1%
Sodium lauryl sulfate 1.2%
Water remaining
Added compound Triethanolamine 3.0%
Diethanolamine 3.0%
Ethylene glycol 3.0%
Ethanolamine 3.0%
Diethylene glycol 3.0%
[0024]
<Ascorbic acid phosphate magnesium salt remaining rate of each sample>
(1) 94.9% triethanolamine
(2) Diethanolamine 92.7%
(3) Ethylene glycol 75.1%
(4) Ethanolamine 59.9%
(5) Diethylene glycol 79.6%
(6) Control 80.3%
[0025]
Examples are shown below.
[Example 1] Toothpaste propylene glycol 5%
Sorbit 40
Carrageenan 1.2
Saccharin sodium 0.2
Sodium lauryl sulfate 1.2
Ethyl paraoxybenzoate 0.1
Ascorbic acid-2-phosphate magnesium salt 0.2
Citric acid monohydrate 0.2
Triethanolamine 3
Sodium hydroxide 0.05
Silicic anhydride 15
Fragrance 0.9
Purified water remaining
Total 100.0%
[0026]
[Example 2] Toothpaste polyethylene glycol 400 5%
Glycerin 20
Xanthan gum 1.1
Xylit 10
Sodium lauryl sulfate 0.9
Myristic acid diethanolamide 0.6
Palmitic acid 0.5
Ascorbic acid-2-phosphate sodium salt 1
Citric acid monohydrate 0.5
Diethanolamine 0.5
Ethyl paraoxybenzoate 0.1
Aluminum hydroxide 40
Fragrance 1.2
Purified water remaining
Total 100.0%
[0028]
[Example 3 ] Toothpaste, propylene glycol 5%
Sorbit 35
Sodium alginate 3
Saccharin sodium 0.15
Sodium lauryl sulfate 1
Butyl paraoxybenzoate 0.5
Sodium hydroxide 0.05
Triclosan 0.1
Ascorbic acid-3-phosphate 0.05
Triethanolamine 2
Diethanolamine 1
Tripolyphosphoric acid 1
Sodium myristate 0.2
Silicic anhydride 20
Fragrance 1
Purified water remaining
Total 100.0%
[0029]
[Example 4 ] Toothpaste Sodium polyacrylate 0.5%
Xanthan gum 0.5
Propylene glycol 5
70% sorbite solution 20
Saccharin sodium 0.1
Sodium benzoate 0.3
Sodium lauryl sulfate 1.5
Tranexamic acid 0.1
Ascorbic acid-2-phosphate sodium salt 0.5
Triethanolamine 2.5
Tartaric acid 2
dl-α-tocopherol 0.2
Oat extract 0.05
Sodium fluoride 0.2
Silicic anhydride 20
Fragrance 1
Purified water remaining
Total 100.0%
[0030]
[Example 5 ] Liquid dentifrice Silicic anhydride 10%
Xanthan gum 1
Saccharin sodium 0.1
60% sorbite solution 40
Glycerin 20
Propylene glycol 3
Sodium lauryl sulfate 1.2
Sodium bicarbonate 2
Decaglyceryl laurate 0.5
Sodium fluoride 0.2
Triclosan 0.1
Ascorbic acid-2-phosphate magnesium salt 1.5
Triethanolamine 0.5
Fragrance 0.8
Blue No. 1 0.001
Purified water remaining
Total 100.0%
[0031]
[Example 6 ] Oral pasta Cetanol 20%
Squalane 5
P. O. E (40) hydrogenated castor oil 0.1
Sorbitan monooleate 1
Sodium lauryl sulfate 0.2
Glycyrrhetinic acid 0.1
Saccharin sodium 0.6
Ascorbic acid phosphate 0.3
Citric acid 0.5
Diethanolamine 0.5
Calcium hydrogen phosphate 5
Fragrance 0.3
Purified water remaining
Total 100.0%
[0032]
[Example 7 ] Mouthwash ethanol 5%
Sorbit 10
Sucrose monopalmitate 0.2
P. O. E (60) hydrogenated castor oil 0.1
Methyl paraoxybenzoate 0.01
Saccharin sodium 0.7
Tranexamic acid 0.5
Cetylpyridinium chloride 0.2
Ascorbic acid-2-sulfate sodium salt 0.2
Citric acid 0.5
Diethanolamine 0.5
Sodium monofluorophosphate 0.7
Oat extract 0.1
Fragrance 1
Purified water remaining
Total 100.0%
[0033]
[Example 8 ] Mouthwash ethanol 10%
Glycerin 10
P. O. E (60) hydrogenated castor oil 5
Saccharin sodium 0.7
Tranexamic acid 0.15
Ascorbic acid-2-phosphate magnesium salt 1
Sodium tartrate 0.5
Triethanolamine 0.25
Fragrance 1
Purified water remaining
Total 100.0%

Claims (7)

To one or more ascorbic acid ester was the esters of phosphoric acid or sulfuric acid or an oral composition containing a salt of any of the hydroxyl groups at position 2,3,5,6 of (A) Ascorbic acid (B) The composition for oral cavity which mix | blended the amine compound which has a 2 or more hydroxyl group chosen from a diethanolamine, a triethanolamine, N-ethyl diethanolamine, a dipropanolamine, and a tripropanolamine . (B) The composition for oral cavity of Claim 1 which mix | blended the amine compound which has a 2 or more hydroxyl group as a stabilizer of (A) component. (A) Ascorbic acid esters, according to claim 2, characterized in that became 1 or 2 Tsugarin acid or ester of sulfuric acid 2,3-position or the hydroxyl groups of the ascorbic acid Oral composition. The composition for oral cavity according to claim 1, 2 or 3, wherein the ascorbic acid ester is one in which the hydroxyl group of ascorbic acid is an ester of phosphoric acid. The blending amount of component (A) is 0.01 to 5% by mass, and the blending amount of component (B) is 0.1 to 5% by mass, according to any one of claims 1 to 4. Oral composition. It is prepared as a dentifrice, The composition for oral cavity of any one of Claims 1-5 characterized by the above-mentioned. To one or more ascorbic acid ester was the esters of phosphoric acid or sulfuric acid or an oral composition containing a salt of any of the hydroxyl groups at position 2,3,5,6 of (A) Ascorbic acid , characterized by blending (B) diethanolamine, triethanolamine, N- ethyl-diethanolamine, di-propanolamine, an amine compound having two or more hydroxyl groups selected from tripropanolamine as a stabilizer of component (a) A method for improving the stability of an ascorbic acid ester or a salt thereof in the oral composition.