JPH02292210A - Oral cavity composition - Google Patents

Abstract

PURPOSE:To obtain an oral cavity composition which is useful in prophylaxis and treatment for gingivatitis or periodontitis, because it causes no coloration or discoloration by decomposition of said colored substance, even when it is stored for a long period of time, by adding polyphosphoric acid, diphosphonic acid to a specific ascorbic acid derivative as an active ingredient. CONSTITUTION:A composition containing compounds selected from ascorbic acid phosphate ester, ascorbic acid esters, and their salts as an active ingredient is combined with 0.0001 to 10wt.%, preferably 0.001 to 5wt.%, based on the total composition, of a coloring depressant selected from polyphosphoric acid, diphosphonic acid, phytic acid, monofluorophosphoric acid, carboxylic acid such as malonic acid, oxalic acid and their salts, preferably pyrophosphoric acid, tripolyphosphoric acid. The amount of the coloring agent used is preferably 1/100 to 20 times the quantity of the active ingredient. Further addition of 0.01 to 10wt.% of an hydrogen carbonate alkali metal salt increases the effect to inhibit the coloration.

Description

Detailed Description of the Invention [Field of Industrial Application] The present invention relates to an oral composition containing as an active ingredient an ascorbic acid derivative selected from ascorbic acid phosphate, ascorbic acid sulfate, and salts thereof. More specifically, the present invention relates to an oral cavity composition that suppresses coloring that occurs when the above-mentioned ascorbic acid derivative is blended.

[Problems to be Solved by the Prior Art and the Invention 1 Ascorbic acid is known to play an important role in the expression of various enzyme activities in living organisms and to have various physiological activities. In particular, it acts as a coenzyme for prolyl and lysyl hydroxylase, and is said to be essential for collagen synthesis. Therefore, it is useful for the prevention and treatment of gingivitis and periodontitis, which are accompanied by collagen destruction, and it has been known to incorporate ascorbic acid and its salts into oral compositions.

However, ascorbic acid is a strong reducing substance,
It is extremely unstable in an aqueous solution and is practically difficult to incorporate into oral compositions such as toothpaste.

For this reason, various chemically stable ascorbic acid derivatives have been developed in recent years, and ascorbic acid phosphate esters, ascorbic acid sulfate esters, and their salts have attracted particular attention, and these ascorbic acid phosphate esters (especially JP-A-52-79032, JP-A-62-96408, JP-A-62-273910, JP-A-63-141921) and ascorbic acid sulfate esters (JP-A-62-2
No. 73910, No. 63-141921) has been proposed to be incorporated into oral compositions.

However, when ascorbic acid phosphate esters or ascorbic acid sulfate esters are blended into oral compositions, visually obvious coloring occurs, and discoloration occurs when stored for a long period of time. In this case, the above-mentioned JP-A-63-14
Publication No. 1921 proposes adding water-soluble zinc salts to prevent discoloration even after long-term storage, but does not mention preventing the above-mentioned discoloration. It is desired to develop a method for effectively preventing the discoloration of oral compositions caused by the inclusion of acid phosphate esters and ascorbic acid sulfate esters.

[Means and effects for solving the problem] As a result of various studies in order to meet the above-mentioned needs, the present inventors have found that polyphosphoric acid is added to an ascorbic acid derivative selected from ascorbic acid phosphate ester, ascorbic acid sulfate ester, and salts thereof. When a compound selected from , diphosphonic acid, phytic acid, monofluorophosphoric acid, carboxylic acid, and their salts is used together as a coloring inhibitor, the coloring of the oral composition,
Furthermore, it was discovered that the discoloration caused by the decomposition of the young colored material can be effectively suppressed, leading to the present invention.

As mentioned above, it is known to incorporate ascorbic acid phosphate esters and ascorbic acid sulfate esters into oral compositions, particularly as described in JP-A-63-141921
The publication proposes preventing discoloration by using water-soluble zinc salts, but without incorporating such zinc salts, the above-mentioned polyphosphoric acid, diphosphonic acid, phytic acid, monofluorophosphoric acid, carboxylic acid, and these acids are used. The fact that the salt prevents coloring caused by ascorbic acid phosphate esters and ascorbic acid sulfate esters is a new finding of the present inventors.

The present invention will be explained in more detail below.

As for the ascorbic acid phosphate ester and sulfuric acid ester blended in the oral composition of the present invention, any one or more of the hydroxyl groups at the 2-position, 3-position, 5-position, and 6-position of ascorbic acid is phosphoric acid. You can use esthetics or sulfate esters. For example, L-ascorbic acid-2-phosphate, L-ascorbic acid-3-phosphate,
L-ascorbic acid-6-phosphate, L-ascorbic acid-2-sulfate, L-ascorbic a-3
-am ester, L-ascorbic acid-6-sulfate ester, and the like. In addition, examples of the salts include sodium salts, potassium salts, calcium salts, magnesium salts, and the like. These ascorbic acid phosphate esters and sulfuric acid esters can be used alone or in combination of two or more. The blending amount of the ascorbic acid phosphate ester and sulfuric acid ester is variously selected, but is 0.00% of the total composition.
It is preferably in the range of 1 to 10% (by weight, the same hereinafter), more preferably 0.01 to 5%.

In the present invention, a compound selected from polyphosphoric acid, diphosphonic acid, phytic acid, monofluorophosphoric acid, carboxylic acid, and salts thereof is blended as a coloring inhibitor for the ascorbic acid derivative.

In this case, as the polyphosphoric acid, linear and cyclic polyphosphoric acids having an average chain length of 2 to 100 can be used, and as the diphosphonic acid, the following formulas R, H, etc. can be used. O, P-C-PO. H2 l R2 (R1: OH, CQ or F, R2: H, CQ, F or an alkyl group having 1 to 4 carbon atoms) is used, and as the carboxylic acid,
malonic acid, oxalic acid, succinic acid, malic acid, citric acid,
Glycolic acid, glycolic acid, pantothenic acid, threonic acid, xylonic acid, tartronic acid, etc. are used. Further, examples of the salt include sodium salt, potassium salt, and the like. Among these, the average ll4 length is 20
The following linear polyphosphoric acids, such as pyrophosphoric acid, tripolyphosphoric acid, tetrapolyphosphoric acid, and metaphosphoric acid, monofluorophosphoric acid, phytic acid, oxalic acid, tartronic acid, and their salts are preferably used, especially pyrophosphoric acid, tripolyphosphoric acid, and salts thereof. and their salts are most preferred.

The blending amount of the above coloring inhibitor is 0.0001% of the total composition.
~10%, particularly preferably 0.001~5%, and 1/1000 of the above ascorbic acid derivative
It is effective to use up to 100 times the amount, especially 1/100 to 20 times the amount.

Note that an alkali metal bicarbonate salt can be used in combination with the coloring inhibitor, and the coloring inhibiting effect can be further improved by the combined use. In this case, the amount of the alkali metal bicarbonate salt is preferably 0.01 to 10% of the total composition.

The oral composition of the present invention may further contain appropriate components depending on the type thereof. For example, when obtaining a dentifrice, abrasives, binders, thickeners, surfactants, sweeteners, fragrances, preservatives, and various active ingredients can be added.

〔Effect of the invention〕

According to the oral composition of the present invention, it is possible to prevent discoloration due to the blending of ascorbic acid phosphate esters or ascorbic acid sulfate esters, and furthermore, to prevent discoloration due to decomposition of the colored substances, thereby increasing the commercial value. Next, an experimental example will be shown to specifically explain the effects of the present invention. [Experimental Example 1] In 1 mQ of 0.25 molar acetic acid buffer (pH 6.0) containing the additives shown in Table 1 at 1% concentration, 2.0 d of 60% sorbitol solution, 1.0 d of 5% sodium lauryl sulfate solution, Od
and 0.5% ascorbic acid phosphate magnesium salt solution or Q. 5% ascorbic acid sulfate dipotassium salt ml 1. OIIIll was added. Next, the above mixed solution (sample) was left at 40°C for 24 hours.
The degree of coloring was determined by measuring the absorbance at 450 nm, and the coloring suppression rate was calculated from the following formula.

However, the control was a mixture containing no additives.

Table 1 [Experimental Example 2] A dentifrice with the following formulation was prepared, filled into a laminate tube, and left at 40°C for 24 hours.The degree of coloration of the dentifrice was visually judged using the following criteria. . The results are shown in Table 2.

Aluminum hydroxide gelling silica sorbitol 4 5.0 2.0 2 5.0 Sodium lauryl sulfate Sucrose monopalmitate ester Saccharin Sodium Ethanol Sodium benzoate Flavor Additives shown in Table 2 Purification 1.5 1.0 0 .2 0.1 0.1 1.0 Quantity balance shown in Table 2 1 0 0.0% Total No coloration Slight coloration; ± Clearly 〃:+ Significantly:+ Below, Examples is shown. [Example 1] Toothpaste Aluminum hydroxide Gellable silica sorbitol 45.0% 2.0 25.0 Table 2 Sucrose monobalmitate Sodium lauryl sulfate Sodium saccharin Ethanol Sodium benzoate 1.0 1.5 0. 2 0.1 0.1 Sodium tripolyphosphate flavored water total 0. 2 1.0 1 0 0.0% [Example 2] Toothpaste precipitated silica sorbisotoglycerin polyvinylpyrrolidone 25.0% 25.0 25.0 1.0 [Example 3] Toothpaste dibasic calcium phosphate 2 Hydrate Dibasic Calcium Phosphate/Anhydrate Gellable Silica Sorbit Propylene Glycol 2 0.0% 20.0 2.0 20.0 Sodium Saccharin Paraoxybenzoate Ethylchlorhexidine Hydrochloride Monofluoro Sodium Phosphate Oxalic Acid Flavored Water Meter 0.2 0.1 0.1 0.1 0.05 1.0 1 0 0.0% Lauroyl diethanolamide Sodium lauryl sulfate Sodium lauroyl sarcosine Sodium saccharin Sodium paraoxybenzoate Ethyl malonate Sodium bicarbonate Perfume water 1.0 1,5 0.3 0.1 0.1 0.2 0.2 0.8 Remaining total 1 0 0.0% [Example 4] Pastacetanol squalane precipitated silica lauryl sulfate sodium glycyrrhetinic acid for oral cavity Saccharin Sodium Tartronate Monocalcium EDTA Flavor [Example 5] Oral Pasta Liquid Paraffin 1 0.0% 20.0 5.0 0.2 0.1 0.6 0.2 0.1 0.6 15. 0% Setanol Glycerin Sorbitan Monopalmitate Sodium Lauryl Sulfate Saccharin Sodium Chloride Penzethonium Citrate Sodium Bicarbonate Flavor [Example 6] Mouthwash Sorbitol Ethanol 1 0.0 20.0 0.6 0.1 0.5 0 .1 0.2 0.2 0.5 1 0.0% 5.0 Sucrose monopalmitate Sodium lauryl sulfate Sodium saccharin Sodium tetrabolyphosphate 0.2 0.0 5 0. O5 Monofluorinated sodium phosphate゜ 0.1 tartronic acid 0.1 fragrance
0.02 Sodium bicarbonate EDTA monocalcium flavor 0.05 0.05 0.6 Applicant Lion Co., Ltd. Agent Patent attorney Takashi Kojima (1 other person) [Example 7] Oral lozenge milk Sugar 97.0%

Claims (1)

[Claims] 1. An oral composition containing an ascorbic acid derivative selected from ascorbic acid phosphate, ascorbic acid sulfate, and their salts, including polyphosphoric acid, diphosphonic acid, phytic acid, monofluorophosphoric acid, carboxylic acid, and their salts. An oral composition comprising a coloring inhibitor selected from the following.