JP3240738B2 - Oral composition - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an oral composition which has an excellent alveolar bone resorption inhibiting effect, is safe even when used for a long period of time, and is effective for the prevention and treatment of periodontal diseases.

[0002]

BACKGROUND OF THE INVENTION Periodontal disease is a disease of the periodontal tissue caused by periodontopathogenic bacteria, and as the symptoms progress, the inflammation of the soft tissue in the periodontal tissue worsens, It is a disease in which alveolar bone resorption occurs and eventually leads to tooth loss.

[0003] Conventionally, flurbiprofen (J. Perodont. Res. 19) has been used as an alveolar bone resorption inhibitor.
88 (23) 166-169), indomethacin (J.
Periodont. Res. 1982 (17) 90-1
It has been reported that non-steroidal anti-inflammatory agents such as 00) are effective. JP-A-60-61524 describes that ibuprofen and flurbiprofen have an effect of inhibiting alveolar bone resorption. ing.

[0004] However, there is a concern that long-term use of these drugs may cause harmful effects on the oral mucosa. For prevention and prevention of alveolar bone resorption caused by periodontal disease which is a chronic disease, it is particularly desirable to use a drug which is safe even when used in the oral cavity for a long period of time. Further, it is necessary to develop a drug having an excellent alveolar bone resorption inhibiting effect.

[0005] The present invention has been made in view of the above circumstances,
An object of the present invention is to provide an oral composition which has an excellent alveolar bone resorption inhibitory effect, is safe even when used in the oral cavity for a long period of time, and is effective for the prevention and treatment of periodontal disease.

[0006]

The present inventors have made intensive studies to achieve the above object, and as a result, surprisingly, taurine has an excellent alveolar bone resorption inhibitory effect, and this taurine and menthol, carvone, When used in combination with one or more fragrances selected from limonene, cineol and menthone, the effect of taurine on inhibiting alveolar bone resorption can be remarkably improved, even though these fragrances themselves do not have the effect. Accordingly, one or two selected from taurine and menthol, carvone, limonene, cineol and menthon
Combination use of more than one kind of fragrance provides an oral composition which has an excellent effect of inhibiting alveolar bone resorption and is highly safe even when used in the oral cavity for a long period of time, and is effective for prevention and treatment of periodontal disease. That is, the present invention has been accomplished.

[0007] It has been known for a long time that taurine is blended in an oral composition, as disclosed in JP-A-63-13282.
No. 0 publication proposes an oral composition containing taurine. The combination of taurine and a specific fragrance is combined, and the above-mentioned special effects are obtained by the combined use of both components. That is obtained is a new finding of the present inventors.

Accordingly, the present invention provides an oral composition comprising taurine in combination with one or more flavors selected from menthol, carvone, limonene, cineol and mentone.

Hereinafter, the present invention will be described in more detail. In the oral composition of the present invention, the amount of taurine is 0.001 to 15% (% by weight, hereinafter the same) of the whole composition, particularly 0.1%. When the amount is less than 0.001%, a sufficient alveolar bone resorption inhibitory effect may not be obtained, and when the amount exceeds 15%, there is a problem in use feeling. There is.

Menthol, carvone, limonene,
The blending amount of one or more fragrances selected from cineol and mentone is preferably 0.001 to 5% (% by weight, hereinafter the same), particularly preferably 0.1 to 1% of the whole composition.

The oral composition of the present invention can be prepared as a dentifrice such as toothpaste, a mouthwash, a mouthwash, etc. In addition to the above-mentioned components, the composition further depends on the purpose of use and the dosage form of the composition. Any appropriate component can be added.

The optional components include, for example, a mouthwash and, in the case of mouthwash, non-ionic such as polyoxyethylene fatty acid esters such as polyoxyethylene hydrogenated castor oil, sugar fatty acid esters such as sucrose fatty acid ester and maltose fatty acid ester. Anionic surfactants, thickeners such as sorbit, glycerin, ethylene glycol and propylene glycol, and sweeteners such as saccharin sodium can be added. Further, in the case of toothpastes such as toothpaste, etc., in addition to the above-mentioned various additives, dibasic calcium phosphate.
Dihydrate or anhydride, calcium carbonate, calcium pyrophosphate, aluminum hydroxide, alumina, silicic anhydride,
Precipitating silica such as aluminum silicate, abrasive such as gelling silica, carrageenan, cellulose derivatives such as carboxymethyl cellulose, alkali metal alginate such as sodium alginate, xanthan gum, tragacanth gum, gums such as gum arabic, gums such as polyvinyl alcohol, etc. Synthetic binders, inorganic binders such as silica gel, aluminum silica gel and the like can be blended.

The amount of these optional components can be any ordinary amount as long as the effects of the present invention are not impaired.

Although the pH of the composition of the present invention is not particularly limited, it is preferable to set the pH to 5 to 7 in order to obtain a high alveolar bone resorption inhibiting effect.

[0015]

Industrial Applicability The oral composition of the present invention is excellent in the effect of inhibiting alveolar bone resorption and has high safety even when used for a long period of time, and is effective for prevention and treatment of various periodontal diseases.

[0016]

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. In addition, all% in each example are weight%. [Experimental example] A skull of a newborn mouse was used as a substitute for alveolar bone. That is, the skull of a mouse about 6 days old was cut out, immersed in 2 ml of α-MEM medium, and cultured overnight in a carbon dioxide incubator (CO ₂ 5%). next day,
2 ml of α-MEM medium containing endotoxin (1 μg / ml) of actinobaratosis actinomycetemcomitans, which is a periodontopathogenic bacterium, or endotoxin, taurine or taurine at a predetermined concentration, and a specific flavor And the same amount of α-M containing
Transferred to EM medium (see Table 1). Then, after culturing for 48 hours in a carbon dioxide gas incubator, the culture solution was collected, and the amount of Ca released during the culturing was determined by Ciba Corning 55
It measured using 0. The group to which only endotoxin was added was used as a control group, and the bone resorption inhibition rate of each drug was determined by the following formula. Table 1 shows the results.

[0017]

(Equation 1)

According to the results shown in Table 1, taurine and menthol,
It was confirmed that a high bone resorption inhibiting effect was obtained when used in combination with one or more flavors selected from carvone, limonene, cineol and menthone.

Further, from the results shown in Table 2, it was confirmed that menthol, carvone, limonene, cineol and mentone had no bone resorption inhibiting effect.

[0020]

[Table 1]

[0021]

[Table 2]

[Example 1] Toothpaste Aluminum hydroxide 45.0% Gelling silica 5.0 Sorbit 25.0 Sodium carboxymethyl cellulose 1.0 Sucrose monopalmitate 1.0 Sodium lauryl sulfate 1.5 Saccharin sodium 0 0.05 Taurine 3.0 Menthol 0.2 Fragrance 0.8 Water Balance 100.00

Example 2 Toothpaste Precipitable silica 45.0% Sorbit 25.0 Glycerin 25.0 Polyvinylpyrrolidone 1.0 Lauroyl polyglycerin ester 1.0 Polyoxyethylene (60 mol) Sorbitan monolaurate 5 Saccharin sodium 0.05 Ethyl parahydroxybenzoate 0.1 Tranexamic acid 0.1 Taurine 0.3 Carvone 0.2 Fragrance 0.8 Water Balance 100.00

[Example 3] Toothpaste dicalcium phosphate dihydrate 40.0% dicalcium phosphate dihydrate 20.0 gelling silica 2.0 sorbit 25.0 propylene glycol 2.0 carboxymethyl cellulose Sodium 1.0 lauryl diethanol amide 1.0 sodium lauryl sulfate 1.5 lauroyl sarcosinate 1.5 sodium saccharin 0.1 ethyl parahydroxybenzoate 0.1 taurine 1.0 limonene 0.5 perfume 1.0 water balance 100 .00

Example 4 Toothpaste Aluminum hydroxide 55.0% Sorbit 35.0 Sodium carboxymethyl cellulose 1.0 Sucrose monopalmitate 1.0 Sodium lauryl sulfate 1.0 Saccharin sodium 0.1 Sodium fluoride 2 Taurine 1.2 Cineol 0.2 Fragrance 0.8 Water Balance 100.00

Example 5 Toothpaste Dicalcium phosphate dihydrate 35.0% Dicalcium phosphate dihydrate 20.0 Gelling silica 2.0 Sorbit 25.0 Propylene glycol 2.0 Carboxymethyl cellulose Sodium 1.0 Lauryl diethanolamide 1.0 Sodium lauryl sulfate 1.5 Lauroyl sarcosinate 1.5 Saccharin sodium 0.1 Ethyl parahydroxybenzoate 0.1 Dextranase 2.0 Taurine 0.5 Mentone 0.2 Perfume 1 0.0 water balance 100.00

Example 6 Mouthwash Sorvite 10.0% Polyoxyethylene (60 mol) hydrogenated castor oil 1.0 Ethanol 10.0 Sucrose monopalmitate 1.0 Saccharin sodium 0.2 Taurine 1.0 Menthol 0 .2 Perfume 0.2 water balance 100.00

Continuation of the front page (56) References JP-A-2-69411 (JP, A) JP-A-62-293219 (JP, A) JP-A-1-308219 (JP, A) JP-A-2-233607 (JP) JP-A-3-38516 (JP, A) JP-A-3-200715 (JP, A) JP-A-5-201878 (JP, A) JP-A-59-5109 (JP, A) 2-45413 (JP, A) JP-A-4-59737 (JP, A) JP-A-63-132820 (JP, A) (58) Fields investigated (Int. Cl. ⁷ , DB name) A61K 7/00 -7/50 CA (STN)

Claims (1)

(57) [Claims] 1. One or two selected from taurine and menthol, carvone, limonene, cineol and menthone
An oral composition characterized by being used in combination with at least one kind of fragrance.