JPH09110683A - Antibacterial agent for oral cavity and composition for oral cavity - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain an antibacterial agent for an oral cavity exhibiting excellent antibacterial activity against etiologic bacterium of periodontitis, halitosis and caries, and having high safety, and to obtain a composition for an oral cavity containing the antibacterial agent. SOLUTION: This antibacterial agent for an oral cavity contains one kind or more than two kinds of flavor selected from tetrahydrogeraniol, β-ionol, cedrene oxide, myrtenyl acetone and 9-oxocedrane as active components.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to a highly safe oral antibacterial agent which exhibits excellent antibacterial activity against periodontal disease, halitosis and dental caries-causing bacteria, and an oral composition containing the same.

[0002]

2. Description of the Related Art Conventionally, as a cause of periodontal disease, bad breath and dental caries, Porphyromonas
gingivalis), Fusobacterium nucleatu
m), Streptococcus mutans (Strepto)
It is known that oral bacteria such as coccus mutans are involved. Therefore, it has been practiced to add chlorhexidine, cetylpyridinium chloride or the like as a bactericide to the oral composition to remove the above-mentioned causative bacteria.

However, when a large amount of the above-mentioned bactericide is added to the oral composition, the bacterial flora in the oral cavity changes due to the strength of the antibacterial activity or the broad antibacterial spectrum, resulting in bacterial metaplasia and safety. There was a problem in terms of.

On the other hand, various attempts have been made to use a fragrance as an antibacterial agent for the oral cavity. In particular, Streptococcus mutans has been tried.
Many proposals have been made regarding fragrances having antibacterial activity against s) (JP-A-59-29618 and 59-29).
619, 59-175410, 63-8812.
No. 3, etc.) has sufficient antibacterial activity against any bacteria causing periodontal disease, halitosis, and dental caries.

Therefore, it has been desired to develop a highly safe oral antibacterial agent having excellent antibacterial activity against oral bacteria which cause periodontal disease, bad breath and dental caries.

The present invention has been made in view of the above circumstances, and uses an antibacterial agent for oral cavity which exhibits excellent antibacterial activity against periodontal disease, halitosis and bacteria causing dental caries, and is highly safe. It is intended to provide a composition for oral cavity.

[0007]

Means for Solving the Problems and Modes for Carrying Out the Invention The inventors of the present invention have conducted extensive studies in order to achieve the above object, and as a result, tetrahydrogeraniol, β-ionol,
One or more fragrances selected from sedrene oxide, myrenylacetone, and 9-oxocedrane exhibit excellent antibacterial activity against periodontal disease, halitosis and caries-causing bacteria, and have high safety I found out.

That is, when one or more kinds of fragrances selected from tetrahydrogeraniol, β-ionol, cedrene oxide, myrenylacetone and 9-oxocedrane are used as antibacterial agents for oral cavity, periodontal disease, halitosis and dental caries. Porphyromonas gingivali which is the causative fungus of Porphyromonas gingivalis
s), Fusobacterium nucleatum (Fusoba)
cterium nucleatum, Streptococcus mut
ans) has an excellent antibacterial property and can suppress its growth, and the above-mentioned oral antibacterial agent is a fragrance. Even if a large amount of this antibacterial agent is added to an oral composition, The present invention has been completed by discovering that the bacterial flora of No. 1 does not change and causes no bacterial metastasis, and that it is excellent in terms of safety.

Therefore, the present invention provides an oral antibacterial agent containing as an active ingredient one or more perfume selected from tetrahydrogeraniol, β-ionol, sedrene oxide, myrenylacetone and 9-oxocedrane. An oral composition comprising an oral antibacterial agent is provided.

The present invention will be described in more detail below. The oral antibacterial agent of the present invention comprises one or more selected from tetrahydrogeraniol, β-ionol, sedrene oxide, myrenylacetone and 9-oxocedrane. The fragrance is used as an active ingredient.

When the oral antibacterial agent of the present invention is used in an oral composition, the compounding amount thereof is 0.
0001 to 5% (weight%, the same below), especially 0.001
It is preferable to be 3%, and if it is less than 0.0001%, a satisfactory antibacterial effect may not be exhibited, and if it exceeds 5%, the stability or flavor of the composition may be impaired.

The antibacterial agent for oral cavity of the present invention may be used alone or in combination of two or more kinds, and existing antibacterial fragrances (eg α-bisabolol, farnesylacetone, thymol, etc.), or Further strong antibacterial properties can be exerted by using in combination with a synthetic antibacterial agent (for example, chlorhexidine salts, cetylpyridinium chloride, benzethonium chloride, trichlorocarbanilide, etc.) in a concentration that does not cause a safety problem.

In the oral composition of the present invention, it is possible to use the components other than the above-mentioned components which are usually used in oral compositions, and the addition amount of these components hinders the effect of the present invention. It can be a normal amount within the range not present.

In the case of toothpaste, for example, an abrasive, a binder,
Various active ingredients such as a thickener, a surfactant, a sweetener, a preservative, and a coloring agent can be added, and these ingredients can be mixed with water to produce the composition.

Here, as the polishing agent, precipitated silica,
Silica-based abrasives such as silica gel, aluminosilicate, zirconosilicate, dibasic calcium phosphate dihydrate and anhydrate, calcium pyrophosphate, calcium carbonate,
Aluminum hydroxide, alumina, magnesium carbonate, tertiary magnesium phosphate, zeolite, zirconium silicate, synthetic resin-based abrasives and the like are preferably used.

As the thickener, glycerin, sorbitol, propylene glycol, polyethylene glycol,
Xylit, maltit, lactit, and the like are preferably used.

As the binder, sodium carboxymethylcellulose, hydroxyethylcellulose, carrageenan, sodium alginate, xanthan gum, carbopol, guar gum, montmorillonite, gelatin and the like are preferably used.

As the surface active agent, an anionic surface active agent, a cationic surface active agent, a nonionic surface active agent or the like may be blended, and specifically, sodium lauryl sulfate, α-
Sodium olefin sulfonate, N-acyl sarcosinate, N-acyl glutamate, 2-alkyl-N
-Carboxymethyl-N-hydroxyethyl imidazolinium betaine, N-acyl taurate, sucrose fatty acid ester, alkylol amide, polyoxyethylene hydrogenated castor oil, polyglycerin fatty acid ester, pluronic, polyoxyethylene sorbitan monostearate, etc. Is preferably used.

As sweeteners, sodium saccharin,
Examples thereof include stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidyl dihydrochalcone, perillartine and the like.

Examples of preservatives include paraoxybenzoic acid ester and sodium benzoate.

Other various active ingredients include sodium fluoride, potassium fluoride, ammonium fluoride, stannous fluoride, fluorides such as sodium monofluorophosphate, potassium salts of orthophosphoric acid, sodium salts and the like. Water-soluble phosphate compounds, allantoin chlorohydroxyaluminum, hinokitiol, ascorbic acid, lysozyme chloride, glycyrrhizic acid and its salts, sodium chloride,
Tranexamic acid, epsilon aminocaproic acid, acetic acid d
Copper compounds such as 1-tocopherol, azulene, glycyrrhetinic acid, sodium copper chlorophyllin, and copper gluconate, aluminum lactate, strontium chloride, potassium nitrate, berberine, hydroxamic acid and its derivatives, sodium tripolyphosphate, zeolite, dextranase, mutanase, amylase , Methoxyethylene, maleic anhydride copolymer, polyvinylpyrrolidone, epidihydrocholesterin, dihydrocholesterol, zinc citrate, touki, sorghum, clove, rosemary, sorghum, safflower and the like.

Suitable fragrances are terpenes such as 1-menthol, carvone, anethole and limonene, or their derivatives, and suitable colorants are Blue No. 1, Yellow No. 4 and titanium dioxide.

As the oral composition containing the oral antibacterial agent of the present invention, toothpaste such as toothpaste, liquid toothpaste and powder toothpaste, mouthwash, mouthwash, oral pasta, troche, Examples thereof include chewing gum and mouth cooling agents, and the food and drink include candy and the like, but are not limited thereto.

[0024]

INDUSTRIAL APPLICABILITY The antibacterial agent for oral cavity of the present invention has excellent antibacterial activity against periodontal disease-causing bacteria, halitosis-causing bacteria and caries-causing bacteria and is highly safe.

[0025]

EXAMPLES Hereinafter, the present invention will be described in detail with reference to Experimental Examples, Examples and Comparative Examples, but the present invention is not limited to the following Examples. In addition, all% in each example are weight%.

[Experimental Example] An antibacterial activity test (measurement of MIC) was carried out by the following method using the oral strain antibacterial agents shown in Table 1 using the following strains and liquid media.

Test tube containing 4 ml of liquid medium (13 x 1
0.04 ml of test antibacterial agent liquid changed stepwise to 00 mm)
Was added and mixed, and 0.04 ml of each bacterial solution precultured for one day was added and stirred. After anaerobic culture at 37 ° C for 3 days, 5
The growth amount of the bacteria was measured by the absorbance at 50 nm.
An absorbance of less than 0.05 is effective, and the minimum inhibitory concentration (M
IC). Table 1 shows the results. Strains to be used and liquid medium composition Porphyromonas gingivalis 381 (Porphyromonas gingivalis 381 (Pg)) Medium: Todd Hewid Broth (hereinafter abbreviated as THB) 3% Hemin 3 ppm Menadione 0.5 ppm Fusobacterium b. nucleatum 1436 (Fn)) medium: THB 3% L-cystine hydrochloride 0.05% Streptococcus mutans 6715 (Sm) medium: THB 3%

[0028]

[Table 1]

From the results of Table 1, the antibacterial agent for oral cavity of the present invention is higher in Pg, Fn and Sm which cause periodontal disease, bad breath and dental caries, as compared with other fragrances (Comparative Example). It was confirmed to have antibacterial activity.

Next, examples will be shown. [Example 1] Toothpaste Calcium carbonate 50.00% Glycerin 20.00 Carrageenan 0.50 Carboxymethyl cellulose 1.00 Lauryl diethanol amide 1.00 Sucrose monolaurate 2.00 Perfume 1.00 Saccharin 0.10 Miltenyl Acetone 0.20 Water Residual 100.00%

Example 2 Toothpaste Dicalcium Phosphate Dihydrate 50.00% Glycerin 20.00 Carboxymethyl Cellulose 2.00 Sodium Lauryl Sulfate 2.00 Perfume 1.00 Sodium Saccharin 0.10 9-Oxosedran 0.1 15 Tetrahydrogeraniol 0.05 Water Residual 100.00%

Example 3 Toothpaste Aluminum hydroxide 45.00% Gelling silica 2.00 Solbit 25.00 Carboxymethyl cellulose 1.00 Sodium lauryl sulfate 2.00 Fragrance 1.00 Sodium saccharin 0.10 β-ionol 0.10 Cedrene oxide 0.20 Water Residual total 100.00%

Example 4 Toothpaste Precipitable silica 25.00% Glycerin 25.00 Sorbit 25.00 Lauroyl polyglycerin ester 1.00 Polyoxyethylene sorbitan monolaurate 2.00 Perfume 1.00 Sodium saccharin 0.20 β-Ionol 0.10 Water Residual 100.00%

[Example 5] Liquid toothpaste Aluminum hydroxide 25.00% Glycerin 40.00 Solbit 15.00 Carboxymethyl cellulose 0.20 Propylene glycol 2.00 Sodium lauryl sulfate 1.50 Decaglyceryl monolaurate 1.00 Perfume 1 1.00 Sodium saccharin 0.10 α-ionone 0.10 Miltenylacetone 0.10 Water Residual 100.00%

[Example 6] Liquid dentifrice Precipitable silica 20.00% Glycerin 25.00 Solbit 35.00 Xanthan gum 0.20 Propylene glycol 2.00 Sodium lauryl sulfate 1.50 Decaglyceryl monolaurate 2.00 Fragrance 1. 00 Saccharin sodium 0.10 Tetrahydrogeraniol 0.10 Water Residual 100.00%

[Example 7] Oral ointment Liquid paraffin 15.00% Cetanol 10.00 Glycerin 20.00 Polyoxyethylene sorbitan fatty acid ester 5.00 Perfume 0.50 Saccharin sodium 0.10 9-oxocedrane 0.20 Water residue 100.00% in total

Example 8 Mouthwash Liquid Ethanol 20.00% Perfume 1.00 Polyoxyethylene hydrogenated castor oil 0.30 Sodium monofluorophosphate 0.10 Saccharin sodium 0.05 Miltenylacetone 0.20 Water Residual total 100.00%

Example 9 Mouthwash Tablet Sodium Bicarbonate 54.00% Citric Acid 17.00 Anhydrous Sodium Sulfate 12.80 Sodium Dibasic Phosphate 10.00 Polyethylene Glycol 3.00 Sodium Monofluorophosphate 0.10 Fragrance 2.00 Oleic acid 0.10 β-Ionol 1.00 Total 100.00%

[Example 10] troche glucose 35.00% palatinose 35.00 arabic gum 6.00 fragrance 1.00 β-ionol 1.00 water balance 100.00%

Example 11 candy sugar 50.00% starch syrup 33.00 organic acid 2.00 fragrance 0.20 9-oxocedrane 0.05 β-ionol 0.05 β-ionone 0.05 water balance 100. 00%

[Example 12] Chewing gum Sugar 53.00% Gum base 20.00 Glucose 10.00 Syrup 16.00 Fragrance 0.50 Tetrahydrogeraniol 0.50 Total 100.00%

[Example 13] Chewing gum Sugar 55.00% Gum base 20.00 Corn syrup 12.00 Syrup 12.30 Fragrance 0.50 Miltenylacetone 0.20 Total 100.00%

─────────────────────────────────────────────────── ─── Continuation of the front page (51) Int.Cl. ⁶ Identification code Internal reference number FI Technical display area A61K 9/08 A61K 9/08 U 9/20 9/20 U 9/68 9/68 31/12 ACK 31/12 ACK

Claims (2)

[Claims] 1. Tetrahydrogeraniol, β-ionol, cedrene oxide, myrenylacetone and 9
-An oral antibacterial agent containing, as an active ingredient, one or more perfumes selected from oxocedrane. 2. An oral composition comprising the oral antibacterial agent according to claim 1.