JPH05331031A - Composition for oral cavity - Google Patents

Abstract

PURPOSE:To obtain a composition for oral cavity having improved stability of guanidine type germicide, having excellent preventing effects on periodontal diseases by blending a source comprising a large amount of sodium chloride and an effective amount of the guanidine type germicide with a specific amount of a specific component. CONSTITUTION:(A) Sodium chloride having dehydrating action is blended with (B) a guanidine type germicide having inhibitory effects on activity of bacteria causing periodontal diseases such as chlorohexidine in the ratio of 25wt.% component A and 0.001-0.1wt.% component B, preferably 10-30wt.% component A and 0.001-0.05wt.% component B to give a composition for oral cavity having synergistically raised preventing effects on periodontal diseases, which is further mixed with (C) 10-100 times, preferably 10-60 times as much an allantoin such as allantoin or allantoin (chlorohydroxy or dihydroxy) aluminum as the component B by weight to stably retain the component B for a long period of time. Further the blend is mixed with (D) 0.01-10wt.% methyl or ethyl p-oxybenzoate as an antiseptic to further improve stability of the component B.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an oral composition, and more specifically, an oral composition containing 5% by weight or more of sodium chloride, which enables stable incorporation of a guanidine type bactericide. Regarding

[0002]

2. Description of the Related Art Periodontal diseases are two major diseases in the oral region along with caries. Chronic marginal periodontitis, that is, so-called alveolar pyorrhea is one of the periodontal diseases and has become a serious problem in the aging society today. Therefore, prevention and treatment thereof have a very important meaning in oral hygiene, and toothpaste containing sodium chloride as a dentifrice intended for them is on the market. Sodium chloride (salt) has been widely used as an oral cleaning agent since ancient times. Although there are various scientific reports on its effectiveness, the dehydration effect at the site of inflammation is particularly effective in preventing or improving alveolar pyorrhea.

As mentioned above, sodium chloride acts on the local inflammatory site and contributes to the prevention of periodontal disease. In order to prevent periodontal disease more positively, a bactericide is added to the dentifrice. Therefore, it is effective to suppress the activity of periodontal disease-causing bacteria, and many toothpastes containing a germicide are on the market. Therefore, if a bactericide is further added to the dentifrice containing sodium chloride, it is expected that the periodontal disease can be synergistically prevented by the dehydrating action of sodium chloride and the effect of the bactericide to suppress the activity of periodontal disease-causing bacteria.

[0004]

By the way, it is said that in order for sodium chloride to exert a sufficient dehydrating action in a dentifrice, a blending amount of 5% by weight or more is necessary.
When a bactericide, particularly a guanidine type bactericide, is added to a dentifrice formulation containing a large amount of sodium chloride as described above, there is a problem that decomposition of the bactericide is promoted. Therefore, it has been desired to develop a technique for stably incorporating a guanidine-type bactericide into an oral composition containing a large amount of sodium chloride.

[0005]

In view of such circumstances, the present inventors have added various components to a system in which a large amount of sodium chloride and an effective amount of a guanidine type bactericide are mixed to stabilize the guanidine type bactericide. As a result of studying the effect, surprisingly, allantoins were identified as guanidine type fungicides 10-1.
It was found that a guanidine-type bactericidal agent can be stably retained for a long period of time when blended in an amount of 100 parts by weight, and an oral composition excellent in the action of preventing periodontal disease can be obtained, thus completing the present invention.

That is, the present invention provides the following component (A),
(B) and (C): (A) sodium chloride 5% by weight or more, (B) guanidine type bactericide 0.001 to 0.1% by weight, (C) allantoins 10 to 100 times by weight of (B) component The invention provides a composition for oral cavity, which comprises:

[0007] In the present invention, sodium chloride (A) is required to be blended in the oral composition in an amount of 5% by weight (hereinafter referred to simply as "%") or more, but 10 to obtain a more sufficient dehydrating action. It is preferable to add 30%. When sodium chloride is added to a semisolid composition such as a toothpaste or a dental cream, it is described in Japanese Patent Publication No. 31222/1990 in addition to ordinary reagents and edible salts. It is preferable to use granular salt having a large particle size.

Examples of the guanidine type bactericide (B) include chlorhexidine and salts thereof, and chlorhexidine hydrochloride and chlorhexidine gluconate are particularly preferable. The amount of these components (B) exerting a bactericidal action in the oral cavity, that is, 0.001 in the oral composition.
~ 0.1% may be blended, but especially 0.001 to 0.0
It is preferable to add 5%.

Allantoins (C) used in the present invention
Is usually added as an anti-inflammatory agent, but in the present invention, it also acts as a stabilizer for the guanidine type bactericide (B). Such allantoins (C)
Examples thereof include allantoin, allantoin chlorhydroxyaluminum, and allantoin dihydroxyaluminum. The component (C) may be added to the oral composition in an amount of 10 to 100 times by weight that of the component (B), and particularly preferably 10 to 60 times by weight. When the amount of component (C) is less than 10 times by weight that of component (B), the stabilizing effect of the guanidine-type fungicide is not sufficient, and when it exceeds 100 times by weight, the bitterness of the guanidine-type fungicide and the astringent taste of allantoins overlap. It is not preferable because it gives an unpleasant taste.

It is preferable to add an antiseptic agent to the oral composition of the present invention, but the stability of the guanidine type fungicide is further improved by adding methyl paraoxybenzoate or ethyl paraoxybenzoate among the antiseptics. To do. The amount of such methyl paraoxybenzoate or ethyl paraoxybenzoate to be compounded is not particularly limited as long as it has an antiseptic effect, but is preferably 0.01 to 0.5% in the oral composition.

Various known components can be added to the oral composition of the present invention depending on its form. For example, dibasic calcium phosphate dihydrate and anhydride, monobasic calcium phosphate, tribasic calcium phosphate, aluminum hydroxide, alumina, calcium carbonate, calcium pyrophosphate, insoluble sodium metaphosphate, anhydrous silicic acid, hydrous silicic acid, aluminum silicate, Magnesium phosphate, magnesium carbonate, calcium sulfate, polymethyl acrylate, bentonite, zeolite, zirconium silicate,
Abrasives such as synthetic resins and crystallized cellulose; glycerin,
Wetting agents such as sorbit, propylene glycol, 1,3-butylene glycol, ethylene glycol, polyethylene glycol, polypropylene glycol, xylit, maltite, lactit; degree of etherification of 0.5-
Carboxymethyl cellulose of 1.5 and salts thereof, methyl cellulose, hydroxyethyl cellulose, carrageenan, sodium polyacrylate, hydroxypropyl cellulose, carboxymethyl hydroxyethyl cellulose sodium, sodium alginate, propylene glycol alginate ester, xanthan gum, tragacanth gum, karaya gum, arabiya gum, polyvinyl alcohol. , Polyvinylpyrrolidone, veegum, laponite and other binders; sodium monofluorophosphate, tin fluoride, sodium fluoride and other tooth strengthening agents; triclosan, trichlorocarbanilide, cetylpyridinium chloride,
Benzethonium chloride, benzalkonium chloride, decalinium chloride, alkyldiaminoethylglycine chloride, other fungicides other than guanidine type, pH adjusting agents such as sodium phosphate, enzymes such as dextranase, amylase, protease, lysozyme mutanase, hinokitiol , Ε−
Aminocaproic acid, tranexamic acid, tocopherols, dihydrocholesterol, glycyrrhetinic acid, glycyrrhizic acid and its salts, glycerophosphate, chlorophyll, water-soluble inorganic phosphate compounds, azulene, chamomile, toki, kawayumi, anti-inflammatory agents such as crude drugs・ Blood circulation promoter;
Lauryl sulfate, myristyl sulfate, α-olefin sulfonate, N-acyl amino acid salt, acyl monoglyceride sulfate, soap, fatty acid monoglyceride, fatty acid monoalkanolamide, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene hydrogenated castor oil, Alkyl glycoside, imidazolinium betaine, alkyl betaine, alkylamido betaine, sulfobetaine,
Surfactants such as amine oxide; sweeteners such as saccharin sodium, stevioside, thaumatin, asparatyl phenylalanine methyl ester; preservatives such as propyl paraoxybenzoate, butyl paraoxybenzoate, sodium benzoate; coloring agents and pigments such as titanium dioxide. Kinds; peppermint oil, spearmint oil, menthol, carvone, anethole, eugenol, methyl salicylate, limonene, ocimene, n-decyl alcohol, citronellol, α-terpineol, methyl acetate,
Citronellyl acetate, methyl eugenol, cineole, linalool, ethyl linalool, wanillin, thymol, anise oil, lemon oil, orange oil, sage oil, rosemary oil, cinnamon oil, piment oil, laurel oil, perilla oil,
Flavors such as wintergreen oil, clove oil, and eucalyptus oil can be appropriately mixed.

The oral composition of the present invention can be produced according to a conventional method, and is in the form of toothpaste such as toothpaste, moisturized toothpaste, liquid toothpaste, mouthwash, dental cream, gingival massage cream and the like. Prepared and applied to.

[0013]

The present invention will now be described in detail with reference to examples, but the present invention is not limited to these examples.

Example 1 Various additives and chlorhexidine hydrochloride were added to a dentifrice composition containing 15% of sodium chloride, and after storage at 40 ° C. for one month, the amount of chlorhexidine hydrochloride in each composition was measured. The results are shown in Table 1.

[0015]

[Table 1]

From the above results, dentifrice compositions A, F containing allantoinchlorohydroxyaluminum,
For G and I, the residual rate of chlorhexidine hydrochloride was almost 100% even after storage at 40 ° C. for 1 month.

Example 2 To a dentifrice composition containing 15 to 30% of sodium chloride, allantoin chlorohydroxyaluminum and chlorhexidine hydrochloride were mixed and stored at 40 ° C. for 1 month.
The amount of chlorhexidine hydrochloride in each composition was measured. The results are shown in Table 2.

[0018]

[Table 2]

From the above results, allantoin chlorhydroxyaluminum was 1% with respect to chlorhexidine hydrochloride.
In the case of the dentifrice compositions L, N, Q, R and S blended in an amount of 0 weight times or more, the residual ratio of chlorhexidine hydrochloride is almost 100.
%Met. Similar results were obtained by using allantoin instead of allantoin chlorohydroxyaluminum.

Example 3 In a dentifrice composition containing 15% sodium chloride and 0.01% chlorhexidine hydrochloride, the compounding ratio of allantoin chlorhydroxyaluminum was changed, and the flavor of each composition was sensory evaluated according to the following criteria. It was
The results are shown in Table 3. (Evaluation Criteria) ◯: The toothpaste has a good flavor and is excellent in usability. Δ: There is no problem as a dentifrice, but a slightly bitter and astringent taste is strongly felt. X: Strong bitterness and astringency are felt, and it is unsuitable as a dentifrice.

[0021]

[Table 3]

From the above results, when the weight ratio of allantoin chlorhydroxyaluminum to chlorhexidine hydrochloride was mixed in 70 times or more, bitterness and astringency became stronger in flavor, and when it exceeded 100 times, it was durable as a dentifrice. I know there isn't.

Example 4 Sodium chloride was added at 15% and chlorhexidine hydrochloride was added at 0.
Various preservatives were added to a dentifrice composition containing 01% and allantoin chlorhydroxyaluminum 0.1%, and after storage at 40 ° C. for 1 month, the amount of chlorhexidine hydrochloride in each composition was measured. The results are shown in Table 4.

[0024]

[Table 4]

From the above results, the stability of chlorhexidine hydrochloride is improved when methyl paraoxybenzoate or ethyl paraoxybenzoate is added as a preservative, as compared with the case where other preservatives are added. Although chlorhexidine hydrochloride was used as the guanidine type bactericide in Examples 1 to 4 described above, similar results were obtained in the experimental system using chlorhexidine gluconate.

Example 5 (toothpaste)

[0027]

[Table 5] Sodium chloride 15.0 (%) Dicalcium phosphate dihydrate 25.0 Glycerin 15.0 Carboxymethyl cellulose sodium 2.0 Carrageenan 0.5 Sodium lauryl sulfate 1.5 Methyl paraoxybenzoate 0.1 Saccharin sodium 0.2 Sodium monofluorophosphate 0.5 Allantoin chlorohydroxyaluminum 0.1 Chlorhexidine hydrochloride 0.01 Perfume 0.8 Water residue

Example 6 (toothpaste)

[0029]

Table 6 Sodium chloride 15.0 (%) Aluminum hydroxide 30.0 Sorbitol 20.0 Glycerin 10.0 Carrageenan 1.0 Sodium lauryl sulfate 1.0 Ethyl paraoxybenzoate 0.1 Sodium saccharin 0.1 Allantoin chlorhydroxy Aluminum 0.5 Chlorhexidine gluconate 0.03 Perfume 0.9 Water residue

Example 7 (toothpaste)

[0031]

[Table 7] Sodium chloride 15.0 (%) Calcium carbonate 20.0 Sorbitol 20.0 Propylene glycol 5.0 Carbopol 0.5 Carboxymethyl cellulose sodium 0.6 Carrageenan 0.9 Sodium lauryl sulfate 1.0 Polyoxyethylene Hydrogenated castor oil (60 EO) 0.5 Methyl paraoxybenzoate 0.1 Sodium saccharin 0.03 Allantoin dihydroxyaluminum 0.5 Chlorhexidine hydrochloride 0.03 Perfume 0.9 Water residue

Example 8 (dental cream)

[0033]

Table 8 Sodium chloride 5.0 (%) White petrolatum 8.0 Propylene glycol 4.0 Carrageenan 0.5 Sodium carboxymethyl cellulose 0.7 Polyethylene glycol 400 35.0 Polyoxyethylene hydrogenated castor oil 2.0 Allantoin 0. 3 Chlorhexidine hydrochloride 0.01 Perfume 0.3 Water residue

[0034]

EFFECTS OF THE INVENTION The oral composition of the present invention contains an effective amount of sodium chloride and a guanidine type bactericide in a stable manner. Due to the synergistic action of these components, it is excellent in teeth such as alveolar pyorrhea and gingivitis. Peripheral disease preventive action is obtained.

 ─────────────────────────────────────────────────── ─── Continuation of the front page (72) Inventor Shinji Kiji 4954 Kagami-shi, Kaiga-cho, Haga-gun, Tochigi Prefecture Kao-jo Castle Dormitory D-402 (72) Inventor Ryozo Nakai 357-9 Hiramatsumoto-cho, Utsunomiya-shi, Tochigi Prefecture (72) Inventor Yasuki Eguchi 2-4-12 Izumigaoka, Utsunomiya City, Tochigi Prefecture Izumigaoka Heights 501

Claims (2)

[Claims] 1. The following components (A), (B) and (C): (A) sodium chloride 5% by weight or more, (B) guanidine type bactericide 0.001-0.1% by weight, (C) A composition for oral cavity, which comprises 10 to 100 times by weight of the allantoins (B) component. 2. The following components (A), (B), (C) and (D): (A) sodium chloride 5% by weight or more, (B) guanidine type bactericide 0.001-0.1% by weight. And (C) allantoin (B) component 10 to 100 times by weight, (D) methyl paraoxybenzoate or ethyl paraoxybenzoate 0.01 to 1.0% by weight, oral composition characterized by containing object.