JPH07196463A - Composition for oral cavity - Google Patents

Abstract

PURPOSE:To obtain the subject composition prevented from discoloration and deterioration with time, useful for preventing and treating periodontosis, by formulating a water-soluble zinc salt in a lysozyme-contg. composition for oral cavity. CONSTITUTION:This composition can be obtained by formulating a composition for oral cavity containing lysozyme or a salt thereof with 0.05-1wt.% of a water- soluble zinc salt (e.g. zinc sulfate), 0.5-3wt.% of a water-soluble nonionic surfactant (e.g. sucrose ester), and 0.1-1wt.% of an alkylimidazolinium betaine or a salt thereof. The lysozyme, which has germicidal and anti-inflammatory activity owing to its bacteriolytic activity, is useful for preventing and treating oral cavity diseases. By the combined use of the lysozyme with the alkylimidazolinium betaine and/or nonionic surfactant, this composition presents its germicidal and anti-inflammatory activity sufficiently and stably even after preserved for a long period of time without inhibiting lysozyme activity. This composition is highly foamable, being excellent in feeling during or after use without bitter or offensive taste.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to an oral composition containing lysozyme.

[0002]

2. Description of the Related Art Conventionally, the problems to be solved by the invention
Since lysozyme has a bactericidal action and an anti-inflammatory action due to bacteriolytic action, it is widely used for the prevention and treatment of oral diseases, particularly periodontal disease.

However, the oral composition containing lysozyme has a problem of coloring over time, and it has been desired to solve this problem.

Further, generally used oral compositions such as toothpaste are blended with anionic surfactants such as sodium lauryl sulfate which is a foaming agent as an essential component for enhancing the cleaning effect and usability. Therefore, when lysozyme is added to the oral composition, lysozyme interacts with the anionic surfactant to be inactivated, and there is a problem that the effect cannot be expected.

Therefore, in recent years, in oral compositions containing lysozyme, various anionic surfactants have been studied to have a foaming property and to stably exhibit the activity of lysozyme without inhibiting the activity of lysozyme. As the surfactant, polyoxyethylene secondary ether carboxylate (JP-A-3-167115) and polyoxyethylene alkyl ether phosphate (JP-A-3-157323).
Gazette), sulfosuccinic acid polyoxyethylene acyl diethanolamide ester salt (Japanese Patent Laid-Open No. 3-157322).
No. gazette) is proposed. However, these oral compositions are still insufficient in terms of foamability, high activity of lysozyme, and stability.

Further, an oral composition prepared only with a nonionic component such as a nonionic surfactant so as not to interact with lysozyme has been proposed, which has a low foaming property and a feeling of use. In addition to being very bad, the activity and stability of lysozyme are insufficient, and a sufficient effect cannot be expected.

For this reason, it has been desired to improve the stability of lysozyme and to impart high foamability.

Therefore, an object of the present invention is to provide a lysozyme-containing oral composition which is prevented from coloring over time.

Another object of the present invention is to provide an oral composition which exhibits stable activity even after long-term storage without inhibiting the activity of lysozyme, has high foamability, and has a good feeling in use. Is provided.

[0010]

Means and Actions for Solving the Problems As a result of intensive studies to achieve the above object, the present inventor has found that zinc sulfate, zinc chloride, zinc lactate is added to an oral composition containing lysozyme or a salt thereof. It was found that the color deterioration with time can be suppressed by adding a water-soluble zinc salt such as.

In addition to the above, a water-soluble nonionic surfactant and an alkylimidazolinium betaine or a salt thereof are used in combination to stabilize the activity of lysozyme without inhibiting it and preserve it for a long time. Even so, it has been found that the effect can be sufficiently exerted, and the composition for oral cavity having a good foaming property and an excellent feeling in use can be obtained.

[0012] Lysozyme strongly interacts with anionic surfactants such as sodium lauryl sulfate, which is usually added to oral compositions as a foaming agent, and loses its original activity such as antibacterial activity due to bacteriolytic action. Be seen.

On the other hand, nonionic surfactants and amphoteric surfactants have a weaker foaming power in the oral cavity than sodium lauryl sulfate, and the nonionic surfactants and amphoteric surfactants are not comparable. The agent may also suppress the activity of lysozyme or reduce its stability.

On the other hand, the present inventor has studied various surfactants, and as a result, alkyl imidazolinium betaine did not suppress the activity of lysozyme, and did not lower the stability of the alkyl imidazolinium betaine. By blending betaine in combination with a water-soluble nonionic surfactant, both components unexpectedly act synergistically and their bactericidal and anti-inflammatory effects are retained even after long-term storage without inhibiting the activity of lysozyme. The present invention has been accomplished, and it was found that the foaming power is enhanced and the bitterness and off-taste derived from alkylimidazolinium betaine can be suppressed, and the present invention has been completed.

Therefore, the present invention provides an oral composition comprising an oral composition containing lysozyme or a salt thereof, and a water-soluble zinc salt, and a water-soluble nonionic surfactant. Provided is a composition for oral cavity in which an agent and an alkylimidazolinium betaine or a salt thereof are used in combination.

The present invention will be described in more detail below. The oral composition of the present invention is prepared as a toothpaste such as a toothpaste, a liquid toothpaste, a water toothpaste, a massage ointment, a mouthwash and a mouthwash. The present invention contains lysozyme or a salt thereof as an active ingredient and further contains a water-soluble zinc salt, more preferably a water-soluble nonionic surfactant, an alkylimidazolinium betaine or a salt thereof.

Here, lysozyme can be usually obtained by extracting and purifying egg white of chicken eggs by a general method, and examples of the salt thereof include lysozyme chloride.

The content of lysozyme or a salt thereof is preferably 0.05 to 5% (weight%, the same hereinafter), particularly 0.1 to 2% with respect to the total amount of the oral composition, and 0.0
If it is less than 5%, its bactericidal action and anti-inflammatory action may not be sufficiently exerted and a satisfactory effect may not be obtained. If it exceeds 5%, it may be economically disadvantageous.

On the other hand, as the water-soluble zinc salt, it is preferable to use at least one selected from zinc sulfate, zinc chloride and zinc lactate.

The amount of the water-soluble zinc salt compounded is preferably 0.05 to 1%, more preferably 0.1 to 0.5% of the total composition,
If it is less than 0.05%, the coloring of the composition may not be prevented, and if it exceeds 1%, the foamability may be lowered or the astringency may be increased.

Specific examples of the water-soluble nonionic surfactant include sucrose ester, stearic acid polyoxyethylene sorbitan ester, oleic acid polyoxyethylene sorbitan ester, and polyoxyethylene hydrogenated castor oil. .

The content of the above water-soluble nonionic surfactant is preferably 0.5 to 3%, particularly 0.5 to 2% of the total composition, and if less than 0.5%, alkyl imidazolinium betaine or The synergistic effect with the salt may not be exhibited, and the foaming power may be insufficient. If it exceeds 3%, the stability of the activity of lysozyme may be reduced, or the off-taste may be increased.

As the alkyl imidazolinium betaine, the alkyl group has 9 to 15 carbon atoms, particularly 9 to 1 carbon atoms.
3 is preferable, and those having less than 9 carbon atoms may not be preferable in terms of mucous membrane irritation and off-flavours.
Larger particles may be unfavorable in terms of foaming power and solubility.

Specific examples of such an alkyl imidazolinium betaine include 2-alkyl-N-carboxymethyl-N-hydroxyethyl imidazolinium betaine and 2-alkyl-N-carboxyethyl-N-hydroxyethyl imidazoline. Nium betaine, 2-alkyl-
N-sodium carboxymethyl-N-carboxymethyloxyethyl imidazolinium betaine and the like can be used, and specifically, it is Obazoline 662N manufactured by Toho Chemical Industry Co., Ltd.
Are used. As the salt of alkyl imidazolinium betaine, the sodium salt, potassium salt and the like of the above alkyl imidazolinium betaine are used.

The amount of the alkyl imidazolinium betaine or its salt to be compounded is 0.1 to 1% of the total composition, particularly 0.1.
The range of 2 to 0.5% is preferable, and if it is less than 0.1%, the decrease in the activity of lysozyme due to the water-soluble nonionic surfactant cannot be suppressed, When used in combination, the synergistic effect of improving the foamability may not be obtained, and the foaming power may be insufficient. If it exceeds 1%, bitterness may be increased and the usability may be poor.

In addition to the above-mentioned components, the oral composition of the present invention may contain optional components depending on its dosage form. As an optional ingredient, for example, prevention of normal oral diseases
Antiseptic agents used for treatment, anti-inflammatory agents, hemostatic agents, tissue activating agents, perfume as a refreshing agent and active ingredients such as local anesthetics, binders, wetting agents, sweeteners, preservatives, polishing agents, Excipients such as alcohol are appropriately mixed. In addition, the compounding amounts of these components can be set to normal amounts as long as the effects of the present invention are not impaired.

[0027]

INDUSTRIAL APPLICABILITY The lysozyme-containing oral composition of the present invention is one in which coloring with time is prevented by the addition of a water-soluble zinc salt. Further, by using in combination with a nonionic surfactant and an alkylimidazolinium betaine or a salt thereof, the bactericidal action, the anti-inflammatory action and the like of the lysozyme can be sufficiently and stably exhibited without being inhibited by the activity of lysozyme. In addition, it has high effervescence and is free from bitterness and off-taste and has excellent usability, and can be widely used for prevention and treatment of oral diseases, especially oral soft tissue diseases such as periodontal disease.

[0028]

EXAMPLES The present invention will be specifically described below with reference to Examples and Comparative Examples, but the present invention is not limited to the following Examples. In addition,% in each example is% by weight.

[Examples 1 to 4, Comparative Examples 1 to 9] Tables 1 and 2
To produce an oral composition by mixing the components shown in, the activity of lysozyme during the production of each oral composition, foaming, taste, stability of the activity of lysozyme after long-term storage and color deterioration by the following method. evaluated. The results are shown in Tables 1 and 2. Lysozyme activity evaluation method : Lysozyme bacteriolytic activity was measured by the turbidity method, and the activity of the lysozyme chloride standard product was 100%.
Is shown as a ratio (%) to the standard product. Evaluation method of foamability and taste : All were evaluated according to the following criteria by sensory evaluation. Effervescence: ◎ Extremely good, ○ Good, △ Insufficient foaming, × No foaming Taste: ○ No bitterness, △ Slightly bitterness,
B. Stability evaluation method for bitter lysozyme activity : After storage at 40 ° C. for 6 months, lysozyme activity was evaluated according to the above evaluation method. Evaluation method of coloring deterioration : The degree of coloring after storage for 6 months at 40 ° C. was evaluated by sensory evaluation according to the following criteria. ○ Not colored, △ Slightly colored, × colored

[0030]

[Table 1]

[0031]

[Table 2]

From the results shown in Tables 1 and 2, it was confirmed that the comparative examples in which zinc sulfate was not mixed were colored, whereas the coloring was prevented by mixing zinc sulfate. . In addition, when sodium lauryl sulfate and other surfactants are blended (Comparative Examples 1 to 4), the activity of lysozyme is inhibited or unstable, the foamability is poor, and a water-soluble nonionic surfactant alone is blended. In Comparative Examples 5 to 7, the lysozyme activity was not inhibited, but its stability and foamability were poor, and the alkyl imidazolinium betaine alone formulation (Comparative Example 8) had a bad taste. On the other hand, when a water-soluble nonionic surfactant and an alkylimidazolinium betaine are used in combination (Examples 1 to 4),
It was found that the lysozyme activity was not impaired, the lysozyme activity was sufficiently and stably exhibited even after long-term storage, the foamability was high, and the usability was good.

[Examples 5 and 6, Comparative Examples 10 and 11] Table 3
The oral composition shown in 1 was prepared and evaluated by the above method. The results are shown in Table 3. From the results shown in Table 3, it was confirmed that the oral composition of the present invention was excellent in stability of lysozyme activity, foamability, and feeling of use, had no color after storage, and had high quality.

[0034]

[Table 3]

Example 7 The following massage ointment for treating periodontal disease was produced. Lysozyme chloride 0.5% Cetylpyridinium chloride 0.05 Zinc sulfate 0.2 Sodium chloride 2 Ethanol 7 Polyethylene glycol 400 4 Glycerin 20 Carmellose sodium 1.4 Polyoxyethylene hydrogenated castor oil 2 Alkyl imidazolinium betaine 0.5 Butyl Paraben 0.01 Perfume Micro purified water Balance 100%

Example 8 The following mouthwash for oral diseases was produced. Lysozyme chloride 0.5% Cetylpyridinium chloride 0.05 Zinc sulfate 0.2 Sodium chloride 2 Ethanol 7 Glycerin 10 Polyoxyethylene hydrogenated castor oil 2 Alkylimidazolinium betaine 0.5 Butylparaben 0.01 Perfume Fine amount Purified water balance 100% in total

Claims (3)

[Claims] 1. An oral composition comprising an oral composition containing lysozyme or a salt thereof and water-soluble zinc salts. 2. The oral composition according to claim 1, wherein the water-soluble zinc salt is one or more selected from zinc sulfate, zinc chloride and zinc lactate. 3. The oral composition according to claim 1, further comprising a water-soluble nonionic surfactant and an alkylimidazolinium betaine or a salt thereof.