JPS63141921A - Composition for oral cavity application - Google Patents

Abstract

PURPOSE:To obtain a composition for oral cavity application and resistant to discoloration even after long-term storage, by compounding a water-soluble zinc salt together with ascorbic acid. CONSTITUTION:The objective composition is produced by compounding (A) ascorbic acid, ascorbic acid salt or ascorbic acid ester and (B) a water-soluble zinc compound, preferably zinc chloride, zinc sulfate, zinc acetate, zinc lactate or zinc nitrate to an oral cavity composition. The amounts of the components A and B in the composition are 0.01-10wt% and 0.1-10wt%, respectively.

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The present invention relates to an oral composition containing ascorbic acids that does not change color even after long-term storage.

[Conventional technology]

It has been reported that approximately 20% of patients with severe periodontal disease have a latent ascorbic acid deficiency. administration is encouraged. It has also been proposed to incorporate ascorbic acids into dentifrices for the purpose of stopping bleeding from the gums.

[Problem that the invention seeks to solve]

Ascorbic acids are highly susceptible to oxidative decomposition when made into an aqueous solution, and the decomposition is particularly accelerated in the presence of metal ions such as copper and iron. When decomposition occurs, brown decomposition products are produced, for example, in oral compositions such as toothpaste.
Even a slight decomposition of the ascorbic acids causes visual discoloration of the composition, resulting in a problem in that the quality of the composition is significantly impaired.

[Means for solving problems]

Therefore, the present inventors conducted extensive research in order to prevent browning of ascorbic acids, and as a result, they discovered that browning is significantly suppressed when water-soluble zinc salts are blended with ascorbic acids, and have completed the present invention.

That is, the present invention provides an oral composition containing one or more compounds selected from the group consisting of ascorbic acid, ascorbic acid salts, and ascorbic acid esters, and water-soluble zinc salts. be.

In the present invention, counter ions for ascorbic acid salts are not particularly limited as long as they are pharmaceutically acceptable, and include alkali metals and alkaline earth metals excluding highly toxic ones such as cadmium. can all be used.

In addition, ° ammonium ion and monoethanolamine,
Jetanolamine, as well as amino acids such as arginine and lysine, can also be used.

Furthermore, as esters, those in which one or more of the hydroxyl groups at the 2nd, 3rd, 5th, and 6th positions are fatty acid esters, sulfuric esters, or phosphoric esters can be used, such as ascorbic acid. Examples include -2-acetic acid ester, ascorbic d-2-[acid ester, ascorbic acid-2-phosphate ester, and ascorbic acid-2゜6-long chain fatty acid ester.

It is generally preferable to incorporate these into the oral composition in an amount of 0.01 to 10% by weight.

Water-soluble zinc salts that can be used in the present invention are not particularly limited as long as they are pharmaceutically acceptable when applied to the oral cavity, but include zinc chloride, zinc sulfate, zinc acetate, zinc lactate,
Zinc nitrate and zinc fluoride are preferred. The higher the blending ratio in the oral composition, the stronger the browning inhibiting effect, but the stronger the bitterness and astringency, so it is desirable to select from a range of 0.1 to 10 weight ratio.

Furthermore, in the present invention, components other than the above-mentioned ascorbic acids and water-soluble zinc salts can be those used in ordinary dentifrices. For example, in abrasives, calcium hydrogen phosphate,
Wetting agents include calcium carbonate, aluminum hydroxide, alumina, anhydrous silicic acid, hydrated silicic acid, insoluble sodium metaphosphate, calcium birophosphate, zeta-2, etc.;
Glycerin, zolopyrene glycol, sorbitol, xylitol, maltitol, salts of pyrrolidone cargonic acid, etc.; binders include sodium carboxymethylcellulose, sodium alginate, ? Foaming agents such as sodium acrylate, carrageenan, sulfated cellulose, hydroxyethyl cellulose, hydroxyzorobyl cellulose, xanthan gum, guar gum, pectin, pullulan, chondroitin sulfate, and hyaluronic acid include alkyl sulfate esters, salts of N-acylglutamic acid, etc. Amino acid surfactants, sucrose fatty acid esters, alkyl phosphate esters, N-acylgetanolamide, etc.; medicinal ingredients include tin fluoride, sodium fluoride,
Sodium heptanofluorophosphate, phytic acid, calcium β-glycerophosphate, ? lyphosphoric acid, cetylpyrizonium chloride, chlorhexicine gluconate, tJ [chlorhexicine, tenguinarine extract, zejutsu extract, zorozeri, dew bee, allantoin, tocopherol acetate,
Tocopherol nicotinate, ε-amitsukazoronic acid, tranexamic acid, chamomile extract, arnica extract, myrrh extract, zopotassium glycyrrhizinate, licorice extract,
Hinokitiol, safflower extract, vitamin B6, nicotinic acid and its esters, sodium chloride, etc. are used.

[Effect]

Next, ascorbic acids with water-soluble zinc salts? I! As a result of experimenting with the inhibitory effect on the depressant side, first, ascorbic acid was used in 1. os
w Mix the test drug of the type and amount shown in Table 2 with the blended dentifrice (the composition is shown in Table 1), fill it into a laminated tube, and then keep it at a constant temperature of 50 degrees Celsius to promote decomposition and browning. It was stored in a tank for 2 weeks, and then the degree of corner change was visually determined. Judgment criteria are: ◎No browning, O: Slight browning,
There are four stages: Δ clearly browned and X markedly browned. At the same time, ascorbic acid was also quantified. For this determination, the titration method of ascorbic acid using 2,6-dichlorophenolindophenol sodium according to the 11th edition of the Japanese Pharmacopoeia was applied.

First, a dentifrice sample containing approximately o, o s t of ascorbic acid was accurately weighed, dispersed in a metaphosphoric acid/acetic acid test solution (3% metaphosphoric acid, 8 thiosulfuric acid fI!,), and then diluted to 100 -. Take 2- of this sample solution with a volumetric pipette, add 8 d of metaphosphoric acid/acetic acid test solution and 3% hydrogen peroxide solution 2-,
Titration was performed with a 216-dichlorophenol indophenol sodium test solution (0,025%) for titration until a light pink color persisted for 5 seconds. Standardization was performed by accurately measuring approximately 0.05 f of a sufficiently dried standard ascorbic acid sample and titrating it in the same manner. T! ! The residual rate of ascorbic acid was calculated from the 7scorbic acid content immediately after the polishing agent was manufactured and the content after storage. The results are shown in Table 2. There was no significant difference in the residual rate of ascorbic acid even without the addition of the drug, but browning was significantly suppressed with the addition of the test drug.

Table 1 Composition of dentifrice used in experiments [Examples] Next, the present invention will be explained in more detail with reference to Examples, but the present invention is not limited to these Examples.

Example 1 Ascorbic acid 0.5% by weight Zinc chloride 0.3 Calcium hydrogen phosphate for toothpaste 45.0 Silicic anhydride
ZO Ludoxymethylcellulose Sodium 2.0 Glycerin 1
0.070 sorbitol solution 15
．． 0 Methyl Q Laben 0.1 Saccharin Sodium 0.1 Sodium Lauryl Sulfate 1.5 Flavor
0゜5 purified water
balance meter ioo,
The above composition was deaerated and kneaded to obtain a polished finish.

Example 2 Sodium ascorbate 0.5 weight i%
Zinc acetate 0.2 Silicic anhydride 20.0 Glycerin
25.070% sorbitol liquid
40.0 Sodium carboxymethyl cellulose 1.0 Titanium oxide 5
．． 0 Methyl-Q Lapen 0.1 Saccharin Sodium 0.1 Sodium Lauryl Sulfate 1.5 Fragrance
0.5 purified water
Balance meter: 100.0 weight The above composition was deaerated and kneaded to obtain a toothpaste.

[Effects of the Invention] The present invention can prevent browning and provide a dentifrice with high commercial value by incorporating water-soluble zinc salts into a dentifrice containing ascorbic acid, its salt, or its ester compound. can.

that's all

Claims (1)

[Scope of Claims] 1. An oral cavity product characterized by containing one or more compounds selected from the group consisting of ascorbic acid, ascorbic acid salts, and ascorbic acid esters, and water-soluble zinc salts. Composition. 2. The oral cavity according to claim 1, wherein the water-soluble zinc salt is one or more zinc compounds selected from the group consisting of zinc chloride, zinc sulfate, zinc acetate, zinc lactate, and zinc nitrate. Composition.