JP2001206830A - Composition for oral cavity - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a composition for the oral cavity having a highly inhibitory effect on dental plaque formation, capable of increasing nonspecific biological response, suitable for preventing periodontosis. SOLUTION: This composition for the oral cavity is characterized in that the composition uses both a water-insoluble or sparingly water-soluble β-D-glucan and one or more kinds selected from compounds belonging to monoterpene, sesquiterpene, diterpene and triterpene.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an oral composition which can suppress plaque formation and enhance nonspecific biological response, and is therefore effective for the prevention or treatment of periodontal disease. .

[0002]

2. Description of the Related Art There are more than 300 kinds of bacteria in the oral cavity, and they are complicatedly intertwined to form plaque. It is known that periodontal disease progresses as a result of the interaction between the formed plaque and the host organism. Therefore, conventionally, it is effective for periodontal disease to suppress plaque bacteria as a whole with a bactericide such as cetylpyridinium chloride or triclosan, or to suppress inflammation caused by a nonsteroidal anti-inflammatory agent represented by ibuprofen or the like. It is known that there is. Attempts have also been made to prevent periodontal disease by using these specific antibodies against plaque bacteria to suppress adhesion and enhance immune response.

[0003] On the other hand, β-glucan has also been applied to oral compositions by using β (1,3) -glucan in order to suppress the destruction of oral tissues due to the stimulation of infection (Japanese Unexamined Patent Publication No. Hei 8- 27709) and for the purpose of improving the texture of the composition (JP-A-10-28753).
No. 6) has been proposed. Also, JP-A-3-312
No. 10 also discloses a β-glucan compound in a composition containing a polysaccharide having an immunomodulatory action. However, the molecular weight of these β-glucans is large, and when incorporated into the composition, no solubility is obtained or a gel is exhibited. Therefore, when used in a usual oral composition, the effect is sufficient. It is not recognized in.

[0004] The present invention effectively inhibits the formation of plaque,
It is another object of the present invention to provide a composition for oral cavity capable of enhancing nonspecific biological response ability.

[0005]

Means for Solving the Problems and Embodiments of the Invention As a result of diligent studies to achieve the above object, the present inventors have found that water-insoluble or hardly soluble β-D-glucan can be added to monoterpenes, sesquis By using one or more of terpene compounds belonging to terpenes, diterpenes and triterpenes in combination, they act synergistically to obtain a higher plaque formation inhibitory effect and a higher biological response ability promoting effect. Having found this, the present invention has been accomplished.

Hereinafter, the present invention will be described in more detail. The oral composition of the present invention contains water-insoluble or hardly soluble β-D-glucan and a specific terpene compound as active ingredients.

In this case, a β-D-glucan having a straight chain or a chain having a side chain can be suitably used.

[0008] The source of β-glucan that can be used in the present invention may be derived from animals and plants or microorganisms, and can be used without any particular limitation. In addition, the binding mode of glucose is β (1 → 2) bond, β (1
→ 3) bond, β (1 → 4) bond, β (1 → 6) bond, etc.
Although there is no particular limitation, those having a large ratio of β (1 → 3) bond and β (1 → 6) bond have high effects and can be suitably used.

Among these, sclerlotium ( Sc)
lerotium) genus Saccharomyces (Sacch
aromyces ), Alkaline genus ( Alcals)
igenus) genus, Penishirikumu (Penicilli
cum ), Agrobacterium
rium) genus Rhizobium (Rhizobium) microorganisms of the genus, etc., Rentinasu edodes (Lentinus
edodes ), Coriolis-Bersicolor ( Cor)
iorus versicolor ), Shizo film
Komue ( Schizophyllum commu)
e ), Poria coccs , Agaricus blaze
i), Suparashisu-Kurisupa (Sparassis c
rispa) Basidiomycetes such as, Setoraria-Isurandika (Cetraria islandica), Usunea-Ronjishima (Usnea longissim
a ), Gyrophora esculenta
esculenta ), Umbilica ( Umbil )
icaria ), Laminaria ( Laminaria )
Those derived from plants such as the genus Eisenia and the genus Eisenia can be particularly preferably used. In addition, its structure has already been specified, for example, lichenan, sclerotan, laminaran, curdlan, pakiman, paramylon, pustulan, yeast β-glucan, crown gar polysaccharide, callose, luteose, or barley, oats, wheat, rye, etc. Β-glucan obtained from the seeds of Poaceae can also be suitably used.

The β-D-glucan thus obtained can be used alone or in combination of two or more.

The amount of these β-D-glucans in the composition of the present invention is desirably 0.001% of the whole composition.
To 10% (% by weight, the same applies hereinafter), particularly 0.01 to 10%.
3% is preferred.

In the present invention, a terpene compound is used in combination with the above β-D-glucan. As the terpene compound to be compounded in combination with the present invention, one or more compounds selected from naturally classified monoterpenes, sesquiterpenes, diterpenes, and triterpene compounds may be selected and compounded. it can.

Among these terpene compounds, limonene, α-pinene, β-pinene, menthone, camphene,
Carvacrol, nerolidol, farnesol, bisabolol, caryophyllene, phytol, stevioside, hederagenin, glycyrrhetinic acid, and also triterpenes obtained from higher fungi (mycelia) such as bukuro, chorei, etc. It can be suitably used.

The compounding amount of these terpene compounds is preferably 0.0001 to 3% of the whole composition, particularly preferably 0.001 to 1%.

The oral composition of the present invention can be made into various dosage forms such as dentifrice such as toothpaste, gum massage cream, topical application, mouthwash, troche and chewing gum. In this case, in addition to the above-mentioned components, various base components used in ordinary oral compositions can be blended with the oral composition of the present invention. For example, in the case of a dentifrice, an abrasive, a binder, a thickener, a sweetener, a flavor, and the like can be blended in a usual amount.

For example, abrasives include calcium hydrogen phosphate dihydrate, tribasic calcium phosphate, calcium carbonate, calcium pyrophosphate, aluminum hydroxide, silicic anhydride, aluminum silicate, insoluble sodium metaphosphate, tertiary phosphorus Magnesium acid, magnesium carbonate,
Calcium sulfate, bentonite, zirconium silicate,
One or more of polymethyl methacrylate, other synthetic resins, and the like may be blended within a range that does not impair the effects of the present invention.

Examples of the binder include cellulose derivatives such as carrageenan, sodium carboxymethylcellulose, methylcellulose and hydroxyethylcellulose; alginic acid derivatives such as sodium alginate and propylene glycol alginate; gums such as xanthan gum, gellan gum, tragacanth gum and karaya gum; One or more kinds of synthetic binders such as alcohol, sodium polyacrylate, and carboxyvinyl polymer, and inorganic binders such as silica gel, veegum, and laponite may be blended.

As humectants, glycerin, sorbitol, propylene glycol, polyethylene glycol,
One or more polyhydric alcohols such as xylitol, maltitol and lactitol may be blended.

As the surfactant, an anionic surfactant such as sodium lauryl sulfate, a nonionic surfactant such as decaglyceryl laurate and diethanolamide myristate, and an amphoteric surfactant such as betaine can be blended. .

As the flavor component, menthol, anethole, carvone, eugenol, n-decyl alcohol,
Citronellol, α-terpineol, cineol, linalool, ethyl linalool, crocodile, thymol, peppermint oil, spearmint oil, wintergreen oil, clove oil, eucalyptus oil and other fragrances can be used alone or in combination.Saccharin sodium, perillartin, Sweeteners such as thaumatin may be included.

The present invention also relates to a bactericide such as chlorhexidine, benzethonium chloride, benzalkonium chloride, cetylpyridinium chloride, decalinium chloride, a phenolic compound such as triclosan, hinokitiol, and biosol, dextranase, and mutanase. , Lysozyme, amylase, protease, lytic enzyme, SO
Enzymes such as D, sodium monofluorophosphate, alkali metal monofluorophosphates such as potassium monofluorophosphate, sodium fluoride, fluorides such as stannous fluoride, tranexamic acid, epsilon aminocaproic acid,
Allantoin, dihydrocholestanol, glycerophosphate, chlorophyll, sodium chloride, xylitol, zinc chloride, water-soluble inorganic phosphate compounds, vitamins such as vitamin A, vitamin B group, vitamin C, vitamin E, and derivatives thereof, etc. One or more active ingredients can be blended.

[0022]

EFFECT OF THE INVENTION The oral composition of the present invention has a high effect of inhibiting plaque formation and can enhance nonspecific biological response, and is suitable for prevention of periodontal disease.

[0023]

EXAMPLES Hereinafter, the present invention will be described in detail with reference to experimental examples and examples, but the present invention is not limited to the following examples.

[Experimental Example 1] Polymorphonuclear leukocyte phagocytosis sterilization test Hartley guinea pigs (8 weeks old, male) had 2%
The casein solution was injected, and 16 hours later, the migrated polymorphonuclear leukocytes (PMN) were collected. This one is Ficol
After 1-Paque (Pharmacia) specific gravity centrifugation, hypotonic Na
The mixed red blood cells were removed by Cl solution treatment, and the suspension was used in Hanks' solution (HBSS) for the experiment.
The phagocytic bacteria include GAM with hemin and menadione.
Cultured anaerobically for 24 hours in Bouillon (Nissui Pharmaceutical), centrifuged and collected, and then suspended in HBSS ( Polyphyromonas gingivalis) .
lis ) ATCC 33277 strain was used.

The phagocytic bactericidal reaction was carried out using the samples (β-glucan (1 mg / ml), terpene compound (0.01 mg / ml)) described in Tables 1 and 2 in the presence of 10% serum, and
N: Porphyromonas gingivali
s = 1: 50 in anaerobic conditions (10% CO ₂ , 10
% H ₂ , 80% N ₂ ) for 60 minutes. After completion of the reaction, the reaction solution was spread on a blood plate, and the colonies formed by culturing were counted to determine the number of remaining viable cells. At the same time, the test was performed on the remaining viable cells obtained from the reaction system without the addition of PMN. The rate (%) was calculated by the following equation.

[0026]

(Equation 1)

[0027]

[Table 1]

[0028]

[Table 2]

[Experimental Example 2] Beagle dog plaque inhibition test A total of 6 of the left and right lower jaws P2 to P4 of four male beagle dogs
An experiment was performed using the tooth as a target tooth. After scaling and polishing the target teeth to completely remove the plaque and tartar, the base (a saline containing 0.5% sodium lauryl sulfate (SDS)) was used as a control in one jaw, and the other was used as a control. The test sample (β-glucan (1 mg / ml), terpene compound (0.01 mg / ml)) solution shown in Table 3 was administered to the chin twice a day by spraying. After thoroughly washing the oral cavity on the fourth day of the experiment, the formed plaque was scraped off, the amount of formed plaque was determined by measuring the amount of protein by the Lowry method, and the inhibition rate relative to the control (physiological saline administration site). (%) Was calculated.

[0030]

[Table 3]

Examples will be described below. [Example 1] Toothpaste Aluminum hydroxide 45.0% by weight Gelling silica 2.0 Sorbit 25.0 Sodium carboxymethylcellulose 1.0 Sucrose monopalmitate 1.0 Sodium lauryl sulfate 1.5 Sodium saccharin 0.2 Ethanol 0.1 Sodium benzoate 0.1 Pakiman 0.2 β-pinene 0.01 Limonene 0.001 Fragrance 1.0 Water Balance 100.0% by weight

Example 2 Toothpaste Precipitable silica 25.0% by weight Sorbit 25.0 Glycerin 25.0 Polyvinylpyrrolidone 1.0 Lauroyl polyglycerin ester 1.0 Polyoxyethylene (60 mol) Sorbitan monolaurate 5 sodium saccharin 0.2 ethyl parahydroxybenzoate 0.1 chlorhexidine hydrochloride 0.1 β-glucan from Agaricus blazei 1.0 laminaran 0.2 menthon 0.02 limonene 0.01 perfume 1.0 water balance 100.0 weight %

Example 3 Toothpaste Dibasic calcium phosphate dihydrate 20.0% by weight Dicalcium phosphate anhydrous 20.0 Gelling silica 2.0 Sorvit 20.0 Propylene glycol 2.5 Sodium carboxymethylcellulose 1.0 lauryl diethanolamide 1.0 sodium lauryl sulfate 1.0 sodium lauroyl sarcosine 0.3 sodium saccharin 0.1 ethyl parahydroxybenzoate 0.1 curdlan 0.2 farnesol 0.1 fragrance 1.0 water balance 100. 0% by weight

Example 4 Toothpaste Calcium Carbonate 45.0% by Weight Sorbite 25.0 Sodium Lauryl Sulfate 1.5 Carboxymethyl Cellulose (CMC) 1.2 Saccharin Sodium 0.1 Sodium Monofluorophosphate 0.5 Propylene Glycol 0 curdlan 0.2 glycyrrhetinic acid 0.05 perfume 1.0 water balance 100.0% by weight

Example 5 Toothpaste Silica 17.0% by weight Xanthan gum 0.5 Sodium alginate 0.3 Sorbite 65.0 Sodium lauroyl sarcosine 0.3 Sodium lauryl sulfate 1.0 Sodium saccharin 0.2 Silicic anhydride 3.0 Agaricus blazei- derived β-glucan 1.0 Stevioside 0.5 Carvacrol 0.02 Fragrance 1.0 Water Balance 100.0% by weight

Example 6 Toothpaste Dicalcium phosphate 25.0% by weight Propylene glycol 4.0 Sorbit 24.0 Carrageenan 0.2 CMC 0.8 Lauroyl sarcosine sodium 0.3 Sodium lauryl sulfate 1.2 Saccharin sodium 0.2 Silicic anhydride 3.0 β (1,3) glucan 0.3 Paramylon 0.5 Limonene 0.02 Pakimic acid 0.01 Fragrance 1.0 Water Balance 100.0% by weight

Example 7 Toothpaste Aluminum hydroxide 40.0% by weight CMC 1.3 Glycerin 20.0 Myristoyl sarcosine sodium 0.1 Sodium lauryl sulfate 1.0 Saccharin sodium 0.02 Silicic anhydride 3.0 Derived from Spassis crispa β-glucan 0.5 α-pinene 0.01 β-pinene 0.01 perfume 1.0 water balance 100.0% by weight

Example 8 Toothpaste Silica 13.0% by weight Sorvit 55.0 Glycerin 18.0 Sodium lauryl sulfate 1.0 Xanthan gum 0.3 Saccharin sodium 0.1 Gelatin 0.2 Diethanolamide laurate 1.0 Propylene glycol 2.0 Callose 0.2 Caryophyllene 0.005 Camphen 0.01 Fragrance 1.3 0.1% Blue No. 1 0.8 Water Balance 100.0% by weight

Example 9 Mouthwash Denatured ethanol 18.0% by weight Polyoxyethylene hydrogenated castor oil 2.0 Glycerin 10.0 Palmitoyl sarcosine sodium 0.1 Citric acid 0.01 Trisodium citrate 0.3 Sclerotan 0 .1 Lichenan 0.1 α-Bisabolol 0.03 Mentone 0.01 Fragrance 0.5 0.1% Green 201 0.8 Water balance 100.0% by weight

Example 10 Mouthwash 90% ethanol 18.0% by weight Polyoxyethylene (80 mol) Sorbitan monotaurate 2.0 Pustulan 0.2 Limonene 0.01 Stevioside 0.2 Perfume 1.20. 1% yellow No. 4 1.0 water balance 100.0% by weight

Example 11 Mouthwash Sorvit 10.0% by weight Ethanol 5.0 Polyoxyethylene (60 mol) hydrogenated castor oil 0.1 Sucrose monopalmitate 0.2 Sodium lauryl sulfate 0.05 Saccharin sodium 2 β-glucan 0.5 farnesol 0.02 nerolidol 0.001 fragrance 0.6 water balance 100.0% by weight

Example 12 Oral Pasta Hydroxyethyl Cellulose 3.0% by Weight Carrageenan 1.0 Sorbit 40.0 Sucrose Palmitate Monoester 2.0 Lauroyl Sarcosine Sodium 0.3 Aluminum Lactate 3.0 0.1% Yellow No. 5 0.8 Saccharin sodium 0.1 Luteose 1.0 Phytol 0.1 Campfen 0.01 Fragrance 1.0 Water Balance 100.0% by weight

Example 13 Oral Pasta Cetanol 10.0% by Weight Squalane 20.0 Precipitable Silica 5.0 Polyoxyethylene (40 mol) Hydrogenated Castor Oil 0.1 Sorbitan Monooleate 1.0 Lauryl Sulfate Sodium 0.2 Glycyrrhetinic acid 0.1 Saccharin sodium 0.6 β-glucan from grasses 0.3 β-pinene 0.02 Caryophyllene 0.01 Perfume 0.6 Water Residue 100.0% by weight

Example 14 Oral Lozenges Lactose 97.0% by weight Polyoxyethylene (60 mol) monostearate 0.2 Sodium lauryl sulfate 0.05 Chlorhexidine gluconate 0.02 Stevia extract 0.2 Glycyrrhetin Acid 0.05 β-glucan 1.0 Limonene 0.02 Fragrance 0.02 Hydroxyethylcellulose Balance 100.0% by weight

[Example 15] Oral lozenges Arabic gum 6.0% by weight Glucose 36.0 Palatinose 36.0 Laminaran 0.1 Sparassis crispa- derived β-glucan 0.2 Perfume 1.3 Water balance 100.0% by weight %

Example 16 Chewing gum Gum base 20.0% by weight Sugar 15.0 Isomaltose 20.0 Palatinose 10.0 Xylitol 10.0 Corn syrup 12.0 β-glucan from Agaricus blazei 0.8 Limonene 0.05 Mentone 0.05 Perfume 0.6 Candy starch Total 100.0% by weight

 ──────────────────────────────────────────────────続 き Continued on the front page F term (reference) 4C083 AA112 AB172 AB222 AB292 AB472 AC102 AC122 AC132 AC302 AC312 AC422 AC432 AC442 AC482 AC642 AC662 AC742 AC782 AC792 AC862 AD072 AD202 AD211 AD212 AD222 AD272 AD282 AD302 AD352 AD531 AD532 CC41 DD15 DD22 DD23 EE33 33

Claims (1)

[Claims] 1. An oral composition comprising a water-insoluble or sparingly soluble β-D-glucan and one or more compounds selected from monoterpenes, sesquiterpenes, diterpenes and triterpenes in combination. .