JP2973511B2 - Oral composition - Google Patents

Description

Description: TECHNICAL FIELD The present invention relates to an oral composition containing as an ascorbic acid derivative selected from ascorbic acid phosphate, ascorbic acid sulfate and salts thereof as an active ingredient, More specifically, the present invention relates to an oral composition that suppresses coloring that occurs when the ascorbic acid derivative is blended.

[Problems to be solved by conventional technology and invention]

Ascorbic acid plays an important role in the expression of various enzyme activities in living organisms, and is known 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. For this reason, it is useful for prevention and treatment of gingivitis and periodontitis accompanied by destruction of collagen, and it has been conventionally known to mix ascorbic acid and salts thereof in oral compositions.

However, since ascorbic acid is a strong reducing substance, it is extremely unstable in an aqueous solution, and it is practically difficult to mix it with an oral composition such as toothpaste. For these reasons, recently, various chemically stable ascorbic acid derivatives have been developed, and particularly, ascorbic acid phosphates, ascorbic acid sulfates, and salts thereof have attracted attention. Kaisho 52
-79032, 62-96408, 62-273910, 63-14
1921) and ascorbic acid sulfates (Japanese Unexamined Patent Publication No.
Nos. 62-273910 and 63-141921) have been proposed to be incorporated into oral compositions.

However, when ascorbic acid phosphates or ascorbic acid sulfates are blended in the oral composition, visually distinct coloring occurs, and discoloration occurs when stored for a long period of time. In this case, the above JP-A-63-1419
No. 21 proposes to mix water-soluble zinc salts to prevent discoloration even when stored for a long time,
It is not stated that the above-mentioned coloring is prevented. For this reason, it is desired to develop a method for effectively preventing coloring of the oral composition accompanying the addition of ascorbic acid phosphates and ascorbic acid sulfates. It is.

[Means and actions for solving the problem]

The present inventor has conducted various studies to meet the above-mentioned demands. As a result, ascorbic acid phosphates and ascorbic acid sulfates and ascorbic acid derivatives selected from the salts thereof were converted to aluminum hydroxide, calcium carbonate,
Along with blending abrasives such as silica and silicate, disodium phosphate is blended as a coloring inhibitor, and the pH of the oral composition is adjusted to 7 to 9, thereby coloring the oral composition and further coloring the oral composition. The inventors have found that discoloration due to decomposition of a substance can be effectively suppressed, and have accomplished the present invention.

As described above, it is known to incorporate ascorbic acid phosphates and ascorbic acid sulfates into an oral composition, and in particular, JP-A-63-141921 discloses discoloration due to the use of water-soluble zinc salts. It is proposed to prevent the use of such zinc salts, but not by adding an abrasive, and by further adding the above-mentioned coloring inhibitor, coloring by ascorbic acid phosphates or ascorbic acid sulfates. Preventing is related to a new finding of the present inventor.

 Hereinafter, the present invention will be described in more detail.

As the ascorbic acid phosphate ester and the sulfate ester incorporated in the oral composition of the present invention, one or more of the hydroxyl groups at the 2-, 3-, 5-, and 6-positions of ascorbic acid are phosphoric acid. Esters or sulfates can be used. For example, L-ascorbic acid-2-phosphate, L-ascorbic acid-3-phosphate, L-ascorbic acid-6-phosphate, L-ascorbic acid-2-sulfate, L-ascorbic acid- 3-sulfate, L-ascorbic acid-6-sulfate and the like. In addition, examples of such salts include sodium salt, potassium salt, calcium salt, magnesium salt and the like. One of these ascorbic acid phosphates and sulfates can be used alone or in combination of two or more.

The amount of the ascorbic acid phosphoric acid ester and the amount of the sulfuric acid ester are variously selected.
-10% (% by weight, hereinafter the same), more preferably 0.01-5%.

In the present invention, an abrasive is added to the oral composition containing the ascorbic acid derivative, and a specific coloring inhibitor is added.

Here, as the abrasive, aluminum hydroxide, second
Calcium phosphate (dihydrate and anhydride), monobasic calcium phosphate, tribasic calcium phosphate, calcium carbonate,
Examples thereof include silica, silicate, insoluble sodium metaphosphate, tribasic magnesium phosphate, and calcium sulfate. Among them, aluminum hydroxide, calcium carbonate, silica, and silicate are particularly preferably used.

The aluminum hydroxide may be an ordinary one or a modified aluminum hydroxide with an acid such as phosphoric acid. The calcium carbonate may be light or heavy, but heavy calcium carbonate is preferred. Examples of the silica include hydrated precipitated silica, silica xerogel, silica aerogel, and the like. Examples of the silicate include aluminosilicate and zirconosilicate (preferably, the amount of Zr is 0.1 to 10%, especially 0.2 to 2%).
%) And the like.

The above-mentioned abrasives can be used alone or in combination of two or more.
%, Particularly preferably 10 to 60%, and if the amount is less than 5%, the coloring prevention effect may not be sufficiently exhibited.

In addition, disodium phosphate is used as a coloring inhibitor.

The amount of the coloring inhibitor used is preferably 0.001% or more, especially 0.01% or more of the whole composition, from the viewpoint of the coloring suppressing effect, and the upper limit is 10%, particularly 5% from the viewpoint of feeling of use.
It is. In addition, by adjusting the pH of the composition to the range of 7 to 9, the coloring suppression effect is more effectively exhibited.

The oral solution composition of the present invention may further contain appropriate components according to the type and the like. For example, when obtaining a dentifrice, a binder, a thickener, a surfactant, a sweetener,
Perfumes, preservatives, and various active ingredients can be blended.

〔The invention's effect〕

ADVANTAGE OF THE INVENTION According to the oral solution composition of this invention, the coloring by mix | blending an ascorbic acid phosphate or an ascorbic acid sulfate, Furthermore, the discoloration by decomposition | disassembly of the coloring can be prevented, and commercial value can be improved.

Next, the effects of the present invention will be specifically described with reference to experimental examples.

[Experimental Example 1] 1 g of a 0.3% aqueous solution of distilled water or a coloring inhibitor shown in the same table, 2.0 ml of a 60% sorbite solution, 1.0 ml of a 5% sodium lauryl sulfate solution, and 0.5% ascorbic acid were added to 4 g of the abrasive shown in Table 1 1.0 ml of a phosphate magnesium salt solution or a 0.5% ascorbic acid sulfate dipotassium salt solution was added.

Next, the mixed solution (sample) was allowed to stand at 40 ° C. for 24 hours, the absorbance at 450 nm of the centrifuged supernatant was measured to check the degree of coloring, and the coloring inhibition rate was calculated from the following equation.

However, the control is a mixture containing no abrasive and no coloring inhibitor.

As is clear from Table 1, it is recognized that the coloring can be suppressed to some extent by adding an abrasive to the ascorbic acid derivatives, and the effect is further enhanced by adding disodium phosphate.

[Experimental Example 2] A dentifrice having the following formulation was prepared, filled in a laminate tube, and allowed to stand at 40 ° C for 24 hours. Then, the degree of coloring of the dentifrice was visually determined according to the following criteria. The shape retention after storing the dentifrice at 50 ° C. for one month was determined according to the following criteria. The results are shown in Table 2.

Dentifrice formulation Ascorbic acid phosphate magnesium salt 0.2% Abrasives shown in Table 2 45.0 Gelling silica 2.0 Sorvite 25.0 Carboxymethylcellulose sodium 1.0 Sodium lauryl sulfate 1.5 Sucrose monopalmitate 1.0 Saccharin sodium 0.2 Ethanol 0.1 Sodium benzoate 0.1 Perfume 1.0 Coloring inhibitor shown in Table 2 Purified water shown in Table 2 Balance meter 100.0% Judgment criteria Coloring degree No coloring:-Slight coloring is observed: ± Clearly 〃: + markedly 〃: Good shape retention Good ： ○ Flows down slightly from toothbrush ： △ Flows down from toothbrush ： × Examples will be described below.

[Example 1] Toothpaste Aluminum hydroxide 45.0% Gelling silica 2.0 Sorbit 25.0 Sodium carboxymethyl cellulose 1.0 Sucrose monopalmitate 1.0 Sodium lauryl sulfate 1.5 Saccharin sodium 0.2 Ethanol 0.1 Sodium benzoate 0.1 Ascorbic acid sulfate dipotassium salt 0.05 Ascorbic acid Phosphate ester magnesium salt 0.1 Disodium phosphate 0.3 Trisodium citrate 0.1 Perfume 1.0 Water balance 100.0% pH 7.98 [Example 2] Toothpaste Precipitated silica 25.0% Sorbit 25.0 Glycerin 25.0 Polyvinylpyrrolidone 1.0 Lauroyl polyglycerin ester 1.0 Poly Oxyethylene (60 mol) sorbitan monolaurate 0.5 Saccharin sodium 0.2 Ethyl parahydroxybenzoate 0.1 Chlorhexidine hydrochloride 0.1 Phosphate ascorbate Umushio 0.05 sodium phosphate dibasic 0.5 Perfume 1.0 Water remaining Total 100.0% pH 8.12 Example 3 20.0% toothpaste dicalcium phosphate dihydrate, calcium carbonate 20.0 gelled silica 2.0 sorbitol 20.0 propylene glycol 2.5 Sodium carboxymethyl cellulose 1.0 Lauroyl diethanolamide 1.0 Sodium lauryl sulfate 1.5 Lauroyl sarcosine sodium 0.3 Saccharin sodium 0.1 Ethyl parahydroxybenzoate 0.1 Ascorbic acid phosphate magnesium salt 0.2 Trisodium citrate 0.3 Disodium phosphate 0.2 Perfume 0.8 Water Balance 100.0% pH 8.38

Continuation of front page (58) Field surveyed (Int.Cl. ⁶ , DB name) A61K 7/00-7/50

Claims (1)

(57) [Claims] 1. An abrasive composition is added to an oral composition containing an ascorbic acid derivative selected from ascorbic acid phosphate, ascorbic acid sulfate and salts thereof, and disodium phosphate is added as a coloring inhibitor. A composition for oral cavity in which coloring due to blending of the ascorbic acid derivative is suppressed, and the pH is adjusted to a range of 7 to 9.