JPH02264711A - Dentifrice composition - Google Patents

Abstract

PURPOSE:To obtain a dentifrice composition having long-term stability, the same function and feeling in use as those of ordinary dentifrice, preventing and treating effects on diseases in the oral cavity by blending lysozyme with allantoin and dihydrogenphosphate and adjusting pH of the blend to a specific neutral range. CONSTITUTION:0.05-5wt.% lysozyme (preferably hen's albumen lysozyme hydrochloride) is blended with 0.05-2wt.% allantoin and 0.1-3wt.% dihydrogenphosphate (preferably Na salt or K salt) and adjusted to pH6.0-6.9 to give a dentifrice composition. The composition can be stabilized for a long period of time by addition of dihydrogenphosphate as a stabilizer. The composition may be mixed with a surfactant, a binder, an abradant, a wetting agent, spice, a sweetener and, if necessary, vitamin E, tranexamic acid, essence of crude drug, etc.

Description

DETAILED DESCRIPTION OF THE INVENTION Field of the Invention The present invention relates to a dentifrice composition effective in preventing and treating oral diseases.

Prior art and its problems Lysozyme is a mucopolysaccharide hydrolase, and by its mucopolysaccharide decomposition action, it exhibits a bactericidal (lysing) action against microorganisms that cause inflammation, and also has a strong anti-inflammatory action. For this reason, lysozyme is effective in the prevention and treatment of both infectious and non-infectious inflammation, and plays a very important role in the prevention, progression, and treatment of oral diseases, especially periodontal diseases such as pyorrhea. It is incorporated into various oral preparations and external preparations such as toothpaste.

When such lysozyme is incorporated into an aqueous formulation, I)
) It is relatively stable at 13 to 5, but becomes unstable on the alkali side. For example, JP-A No. 52-54037 reports that lysozyme is stabilized in the presence of sodium fluoride in toothpastes containing anionic isomer agents and diaphragms, but the stability as a J product is still insufficient. It is.

Further, Japanese Patent Publication No. 1765/1983 proposes a method of stabilizing lysozyme with hydroxyethyl cellulose, a nonionic surfactant, or the like.

On the other hand, alan) has a necrotic tissue removal effect and tissue repair effect, and is itself low toxicity, non-irritant, anti-irritant, and anti-allergic, so it is widely used as a medicinal agent in pharmaceuticals and cosmetics. It is also used in toothpaste compositions to prevent alveolar pyorrhea and gingivitis.

However, such allantoin is also very unstable in the presence of water, and external preparations containing allantoin stably at a pH of 5.5 or less (Japanese Patent Application Laid-Open No. 140013/1982) are known.

Therefore, from such conventional knowledge, in order to stabilize both lysozyme and allantoin in a system where they coexist, it is necessary to set the pH to 3 to 5. However, formulations that are applied directly into the oral cavity, such as toothpaste, have a pH of 6.
It is necessary to maintain it at approximately neutrality of 0 to 7°5. For this reason, it has not been possible to stably maintain both lysozyme and allantoin in a dentifrice composition for a long period of time.

An object of the present invention is to provide a dentifrice composition in which both lysozyme and allantoin are stably blended for a long period of time under substantially neutral conditions.

In order to solve the problem, the present inventors conducted various studies in view of the above purpose, and found that
The inventors have discovered that long-term stabilization can be achieved by adding dihydrogen phosphate as a stabilizer to a toothpaste composition containing lysozyme and allantoin as medicinal ingredients, and have completed the present invention.

That is, the present invention provides a dentifrice composition containing lysozyme, allantoin, and dihydrogen phosphate, and having a pH adjusted to 6.0 to 6.9.

Dihydrogen phosphate is employed as the stabilizer blended into the dentifrice composition of the present invention. As the dihydrogen phosphate used in the present invention, sodium salts and potassium salts are preferred. The amount of dihydrogen phosphate compounded in the composition is preferably 0.1 to 3% by weight.

If the blending amount is outside this range, the dentifrice composition will not reach the desired pH.
It becomes difficult to control.

Note that phosphates other than dihydrogen phosphate are not used in the composition of the present invention. For example, metaphosphate is a condensed ring, and is known to change from polymetal salt → tripoly salt → pyro salt → ortho salt, and the taste of toothpaste is not constant. Furthermore, when organic acids such as citric acid, tartaric acid, and ascorbic acid are used, coloring is observed during long-term storage.

The lysozyme to be blended into the dentifrice composition of the present invention may be any commonly used lysozyme, and is not particularly limited, but chicken egg white lysozyme is usually used, and its hydrochloride is generally used.

Further, the amount of lysozyme and allantoin in the composition may be selected as appropriate, but usually 0.05 lysozyme
It is preferable to incorporate the drug in an amount of 5% by weight and allantoin 0805 to 2% by weight in terms of the effectiveness of the drug.

Any other known appropriate dentifrice ingredients may be included in the dentifrice composition of the present invention as long as they do not impede the effects thereof.

For example, the surfactant and binder are preferably nonionic ones that have little effect on the stability of the enzyme. That is, the surfactant is preferably an alkylene oxide addition type surfactant such as polyoxyethylene hardened castorum, polyoxyethylene glycerin monofatty acid ester, or polyoxyethylene sorbitan fatty acid ester.

In addition, as a binder, hydroxyethyl cellulose,
Nonionic water-soluble polymers such as hydroxypropyl cellulose and methyl cellulose are preferred.

As the abrasive, commonly used abrasives may be used, such as calcium phosphate, silicic anhydride, aluminum hydroxide, and the like.

As the wetting agent, any commonly used wetting agent may be used, such as glycerin, propylene glycol, sorbitol, polyethylene glycol, and the like.

Additionally, known flavors and sweeteners can be blended in the usual proportions.

Furthermore, the dentifrice composition of the present invention may optionally contain vitamin E.
Other medicinal agents such as tranexamic acid, ε-aminocaproic acid, glycyrrhizinic acid, chlorhexidine, cetylpyridinium, azulene, hinokitiol, enzymes such as mutanase, sodium chloride, herbal medicine extracts such as Toki, Shikon, etc. May be blended.

The dentifrice composition of the present invention can be produced by mixing the above-mentioned components by a known method.

EXAMPLES Next, the present invention will be explained in more detail with reference to Examples and Comparative Examples, but the present invention is not limited thereto. In addition, the obtained dentifrice composition was evaluated by the following method.

Appearance and Taste: Ten volunteers conducted an appearance test and sensory evaluation of the taste after brushing their teeth for 3 minutes.

1 (: Take 2g of toothpaste composition, add 20me of water,
After color separation, the mixture was centrifuged, filtered, and the pi-i of the supernatant was measured.

Stability of Lysozyme 2g of the dentifrice composition was taken, extracted with a phosphate buffer solution of pH 6.2, and then measured in accordance with the method for quantifying lysozyme chloride in the Japanese Pharmaceutical Ingredients Standards outside the Japanese Pharmacopoeia. Content at the start of evaluation is 100
%.

Stability of allantoin: 2 g of the dentifrice composition was taken, extracted with water, and then quantified by high-performance liquid chromatography. Content at the start of evaluation is 100%
And so.

Example 1 A toothpaste was kneaded in a conventional manner according to the formulation shown in Table 1 below. The results obtained are shown in Table 3.

Table 1 Ingredients Weight % Lysozyme chloride 1.0 Allantoin 1.0 Calcium hydrogen phosphate 1010 Silicic anhydride
2.0 concentrated glycerin
40.0 Purified water 40.2 Hydroxyethyl cellulose 2.0 Polyoxyethylene hydrogenated castor oil 2.0 Titanium oxide
0.2 Butyl paraoxybenzoate 0.1 Sodium dihydrogen phosphate
0.5 total 100°0 Comparative Examples 1 to 3 In the same manner, toothpaste compositions were kneaded according to the formulations shown in Table 2 below. The results are shown in Table 3 below.

Examples 2 to 4 Toothpastes were kneaded in a conventional manner based on the formulations shown in Table 4 below, and the appearance, taste, pH, and stability of lysozyme and allantoin were evaluated.

Advantages of the Invention The dentifrice composition of the present invention stably contains lysozyme and allantoin, and prevents oral diseases such as gingivitis while maintaining the same feeling of use as regular toothpaste without impairing its function as a dentifrice. , showing great therapeutic effects.

Patent applicant: Sunstar Co., Ltd.

Claims (1)

[Claims] A dentifrice composition comprising lysozyme, allantoin and dihydrogen phosphate, and the pH thereof is adjusted to 6.0 to 6.9.