JPH07165547A - Composition for oral cavity - Google Patents

Abstract

PURPOSE:To obtain the subject composition containing a rutin or a glycoside thereof and perfume(s), suppressing the excessive production of active oxygen from the living body infected with bacteria, preventing collagen destruction and inflammation, thus useful for preventing and treating periodontosis. CONSTITUTION:This composition for oral cavity contains, as active ingredients, 0.001-5wt.% of a rutin or a glycoside thereof (e.g. alpha-glucosylrutin) and 0.001-5wt.% of at least one kind of perfume selected from limonene, cineole, isoeugenol and menthone. Other ingredients to be formulated in this composition are as follows: abrasive agent, caking agent, thickening agent, surfactant, sweetener, preservative, colorant, etc. This composition is prepared into toothpaste, tooth wash, other dentifrice, pasta for oral cavity, mouthwash, troche for oral cavity, etc.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION The present invention can effectively suppress the production of active enzyme from the living body during bacterial infection such as periodontal disease-causing bacteria and prevent destruction of collagen and exacerbation of inflammation. The present invention relates to an oral composition effective for prevention and treatment of diseases.

[0002]

BACKGROUND OF THE INVENTION Plaque that adheres to the surface of teeth has about 70% bacteria, about 20% polysaccharide formed by the bacteria, and the remaining about 10%.
Is composed of food residues and is firmly stuck to the tooth surface. Furthermore, plaque is characterized by the fact that the acid stored inside decalcifies enamel and causes caries, and that the bacteria and toxins produced cause gingivitis, periodontitis, and alveolar pyorrhea. It is said that, therefore, it is attracting attention as a cause of caries and periodontal disease, which are the two major diseases of the oral cavity.

This dental plaque was initially Streptococcus
It is formed by using sucrose existing in the oral cavity by oral bacteria centering on mutans, and further, due to the anaerobic state inside the plaque, Porphyromonas gingivalis, Bacteroides intermedius, etc. Various periodontal disease pathogenic bacteria grow. Carcasses of these bacteria and various substances and toxins produced adversely affect the gingiva, and periodontal pockets are formed and grown around the teeth, and further, bacteria adhere to and grow in the periodontal pockets. The periodontal disease will progress and worsen.

On the other hand, the living body mobilizes biological defense factors such as polymorphonuclear leukocytes and macrophages, which are one of the blood cell components, against the infection and invasion of these bacteria and eliminates the bacteria. Collagenase is produced and released from bacteria and polymorphonuclear leukocytes, and active enzyme that contributes to the bactericidal activity of tissues in a small amount but invades tissues in a large amount is produced and released from polymorphonuclear leukocytes. It has been known.

During a series of pathological process of periodontal disease,
Excessively produced collagenase and active oxygen destroy collagen existing relatively in superficial layers such as epithelium and connective tissue of gingival tissue and exacerbate local inflammation. And the condition is
After gingivitis such as gingival swelling and bleeding, it eventually progresses to periodontal disease with alveolar bone resorption.

Conventionally, the above-mentioned agents for preventing periodontal disease include:
Chlorhexidine (J. of Clin. Period)
ontol. 1988; 15: 60-67), lysozyme chloride (Journal of the Japanese Society of Periodontology, Vol. 25, No. 1, p24).
5), tranexamic acid (compound of tranexamic acid in toothpaste, Japanese Patent No. 989853) and the like have been reported.

However, despite the development of these preventive and therapeutic means for periodontal disease, unfortunately, the prevalence of periodontal disease in Japan is still high at 50% or more. Therefore, the development of safer, simpler and more efficient preventive and therapeutic techniques is desired.

The present invention has been made in view of the above circumstances.
It has an activity of inhibiting the production of active oxygen from the body during bacterial infections such as periodontal disease-causing bacteria, and therefore suppresses the excessive production of active oxygen and prevents the destruction of collagen and the exacerbation of inflammation that occurs during active oxygen overproduction. Therefore, it is an object of the present invention to provide an oral composition effective for preventing and treating periodontal disease.

[0009]

MEANS TO SOLVE THE PROBLEMS As a result of intensive studies to achieve the above-mentioned object, the present inventor has found that rutin or a glycoside thereof and one kind selected from limonene, cineole, isoeugenol and menthone or Surprisingly, the combined use of two or more fragrances synergistically enhances the antioxidative effect of rutin or its glycosides. Therefore, active oxygen from the living body at the time of infection by bacteria such as periodontal disease-causing bacteria. It is possible to extremely effectively suppress the production of the active oxygen and prevent the overproduction of such active oxygen, resulting in the destruction or local destruction of collagen existing relatively in the superficial layer such as epithelium and connective tissue of gingival tissue which occurs when the active oxygen is overproduced. It was found that the exacerbation of inflammation can be prevented, and therefore, an oral composition effective for the prevention and treatment of periodontal disease can be obtained, and the present invention has been completed.

JP-A-58-213706 discloses an oral composition containing a compound selected from amygdalin, indigo, sanshool, bisabolol and rutin, and JP-A-62-51613 discloses flavonol and chrysin. And dentifrice composition containing a compound selected from hesperesin and hesperidin, JP-A-59-1372
Japanese Patent Laid-Open No. 1-6 proposes a dental moss formation inhibitor composed of flavonoids, and a water-soluble flavonol glycoside is disclosed in JP-A-4-6.
No. 6097, and a method for producing α-glycosyl rutin and its use are described in JP-A-3-58790. However, rutin or a glycoside thereof, limonene, cineol, isoeugenol and A composition for oral cavity containing one or more fragrances selected from menthol can extremely effectively suppress excessive production of active oxygen from the living body during infection with bacteria such as periodontal disease-causing bacteria. That is a new finding of the present inventor.

Therefore, the present invention comprises a composition for the oral cavity which comprises a combination of rutin or a glycoside thereof and one or more flavors selected from limonene, cineol, isoeugenol and menthone. I will provide a.

The present invention will be described in more detail below. The oral composition of the present invention is prepared as toothpaste such as toothpaste, liquid toothpaste, moisturized toothpaste, oral pasta, mouthwash, oral troche and the like. It is possible that rutin or a glycoside thereof is used as an active ingredient together with a fragrance selected from limonene, cineol, isoeugenol and menthone.

Here, as rutin or a glycoside thereof,
Examples thereof include rutin and α-glucosylrutin, and α-glucosylrutin is particularly preferably used. The amount of the above-mentioned rutin or its glycoside is 0.001 to 0.001 of the total composition.
5% (% by weight, the same applies below), particularly preferably 0.01 to 1%, and if the blending amount is less than 0.001%, the anti-inflammatory effect at the local gingiva may not be sufficiently exerted,
If it exceeds 5%, the use feeling may be adversely affected.

As the fragrance, one kind selected from limonene, cineole, isoeugenol and menthone may be used alone or two or more kinds may be mixed and used. Further, as these flavors, either those isolated from essential oils or synthetic products may be blended, and further essential oils containing these may be blended. The blending amount of the above-mentioned fragrance is 0.001 to 5%, especially 0.0
1 to 1% is preferable, and the blending amount is 0.001%
If the amount is less than 5%, the combined effect may not be sufficient, and if it exceeds 5%, the usability may be adversely affected.

The oral composition of the present invention may contain other additives as optional components in addition to the above-mentioned essential components depending on the dosage form.

In the case of toothpaste, for example, an abrasive, a binder,
Thickeners, surfactants, sweeteners, preservatives, colorants, various active ingredients other than the above-mentioned essential ingredients, flavors and the like may be added.

As the abrasive, silica-based abrasives such as precipitated silica, silica gel, aluminosilicate, zirconosilicate, dicalcium phosphate dihydrate and anhydrate, calcium pyrophosphate, calcium carbonate, aluminum hydroxide. , Alumina, magnesium carbonate, third
Magnesium phosphate, zeolite, zirconium silicate, synthetic resin-based abrasive, etc. are preferably used.

Examples of the thickener include glycerin, sorbit, propylene glycol, polyethylene glycol,
Xylit, maltite, lactit, etc., as binding agents, sodium carboxymethyl cellulose, hydroxyethyl cellulose, carrageenan, sodium alginate, xanthan gum, garbopol, guar gum, montmorillonite, gelatin, etc.As surfactants, anionic surfactants, cationic surfactants Agents, nonionic surfactants, and the like, and specifically, sodium lauryl sulfate, sodium α-olefinsulfonate, 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,
Pluronics, polyoxyethylene sorbitan monostearate, and other sweeteners include saccharin sodium,
Stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidyl dihydrochalcone, perillartine, etc. as preservatives, paraoxybenzoic acid ester, sodium benzoate, etc., and various active ingredients such as sodium fluoride, potassium fluoride, fluorine. Ammonium chloride, stannous fluoride, fluorides such as sodium monofluorophosphate, potassium salts of orthophosphoric acid, water-soluble phosphate compounds such as sodium salts, allantoinchlorohydroxyaluminum, hinokitiol, ascorbic acid, lysozyme chloride, glycyrrhizin Acid and its salts,
Sodium chloride, tranexamic acid, epsilon aminocaproic acid, dl-tocopherol acetate, α-bisavonol, isopropylmethylphenol, chlorohexidine salts, cetylpyridinium chloride, azulene, glycyrrhetinic acid, copper compounds such as copper chlorophyllin sodium, 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, benzethonium chloride, dihydrocholesterol, trichlorocarbanilide, zinc citrate, soft extract of touki, oat extract, clove,
Examples of colorants such as extracts of rosemary, sardine, safflower and the like include Blue No. 1, Yellow No. 4, titanium dioxide, alumina oxide and the like. 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.

[0019]

INDUSTRIAL APPLICABILITY The oral composition of the present invention can very effectively suppress the production of active oxygen from the living body during bacterial infection and prevent the overproduction of active oxygen. It is possible to prevent the destruction of collagen existing relatively in the surface layer such as epithelium and connective tissue of gingival tissue and exacerbation of local inflammation, which is effective for the prevention and treatment of periodontal disease.

[0020]

EXAMPLES The present invention will be specifically described below with reference to experimental examples and examples, but the present invention is not limited to the following examples.

[Experimental Example] Peripheral blood polymorphonuclear leukocytes collected from peripheral blood of ODU rat by specific gravity centrifugation were 2.5 × 10 5.
Adjusted to ⁶ / ml. 50 μm of this cell suspension was added to Table 1.
50 μl of each of the test agents shown in 1) and 50 μl of luminol solution were added, and incubated at 37 ° C. for 1 minute.
A) (50 μl) was added, and the produced active oxygen was immediately measured with a Lumiphotometer (TD-4000). Furthermore,
The active oxygen production inhibition rate (%) of each drug was determined using the control as a control. The results are shown in Table 1.

From the results shown in Table 1, it is possible to effectively suppress active oxygen by using rutin or a glycoside thereof in combination with one or more perfume selected from limonene, cineole, isoeugenol and menthone. I understood.

[0023]

[Table 1]

[Example 1] Toothpaste Aluminum hydroxide 45.0% Gelling silica 2.0 Sorbit 25.0 Sodium carboxymethyl cellulose 1.0 Sucrose monopalmitate 1.0 Sodium lauryl sulfate 1.5 Sodium saccharin 0 .2 ethanol 0.1 sodium benzoate 0.1 rutin 0.1 methyl salicylate 0.2 menthone 1.0 water balance 100.0%

Example 2 Toothpaste Precipitable silica 25.0% sorbit 25.0 Glycerin 25.0 Polyvinylpyrrolidone 1.0 Lauroyl polyglycerin ester 1.0 Polyoxyethylene (60 mol) sorbitan monolaurate 0. 5 Saccharin sodium 0.2 Ethyl paraoxybenzoate 0.1 Chlorhexidine hydrochloride 0.1 α-Glucosyl rutin 0.05 ε-Aminocaproic acid 0.05 Methyl salicylate 0.2 Cineol 0.1 Perfume 1.0 Water balance 100. 0%

Example 3 Toothpaste Dicalcium Phosphate Dihydrate 20.0% Dicalcium Phosphate Anhydrate 20.0 Gelling Silica 2.0 Sorbit 20.0 Propylene Glycol 2.5 Carboxymethyl Cellulose Sodium 1.0 Lauryl diethanol amide 1.0 Sodium lauryl sulfate 1.5 Lauroyl sarcosine sodium 0.3 Saccharin sodium 0.1 Ethyl paraoxybenzoate 0.1 α-Glucosyl rutin 0.2 Isoeugenol 0.05 Anethole 0.2 Perfume 0.8 Water balance 100.0%

[Example 4] Liquid dentifrice Precipitable silica 20.0% Butyl paraoxybenzoate 0.01 Xanthan gum 0.2 Sodium polyacrylate 0.15 Propylene glycol 2.0 Solbit 35.0 Glycerin 25.0 Saccharin sodium 0 .1 Fragrance 1.0 Dye (Brilliant Blue) 0.001 Sodium lauryl sulfate 1.5 Decaglyceryl monolaurate 2.0 α-Glucosylrutin 0.2 Isoeugenol 0.05 Anethole 0.2 Water Residual 100.0%

Example 5 Liquid Toothpaste Aluminum Hydroxide 25.0% Sodium Polyacrylate 0.1 Carboxymethyl Cellulose Sodium 0.2 Propylene Glycol 2.0 Sorbit 15.0 Glycerin 40.0 Saccharin Sodium 0.1 Perfume 1. 0 Sodium lauryl sulfate 1.5 Decaglyceryl monolaurate 1.0 Rutin 0.2 Isoeugenol 0.05 Mentone 0.2 Water Residual 100.0%

Example 6 Oral Pasta Cetanol 10.0% Squalane 20.0 Precipitable Silica 5.0 Polyoxyethylene (40 mol) Hydrogenated Castor Oil 0.1 Sorbitan Monooleate 1.0 Sodium Lauryl Sulfate 0.2 Glycyrrhetinic acid 0.1 Sodium saccharin 0.6 Rutin 0.3 ε-Aminocaproic acid 0.5 Ethyl salicylate 0.2 Isoeugenol 0.1 Mentone 0.05 Perfume 0.6 Water Residual 100.0%

[Example 7] Oral pasta Liquid paraffin 15.0% Cetanol 10.0 Glycerin 20.0 Sorbitan monopalmitate 0.6 Polyoxyethylene (40 mol) sorbitan monostearate 5.0 Sodium lauryl sulfate 0 .1 saccharin sodium 0.5 benzethonium chloride 0.1 α-glucosyl rutin 0.2 ε-aminocaproic acid 0.1 methyl salicylate 0.2 limonene 0.1 perfume 0.5 water balance 100.0%

[Example 8] Mouthwash Sorbit 10.0% Ethanol 5.0 Polyoxyethylene (60 mol) hydrogenated castor oil 0.1 Sucrose monopalmitate 0.2 Sodium lauryl sulfate 0.05 Saccharin sodium 0.2 α-Glucosyl rutin 0.05 Mentone 0.05 Ethyl salicylate 0.1 Limonene 0.05 Perfume 0.6 Water Residual 100.0%

[Example 9] Lozenge for oral cavity Lactose 97.0% Polyoxyethylene (60 mol) monostearate 0.2 Sodium lauryl sulfate 0.05 Chlorhexidine gluconate 0.02 Stevia extract 0.2 Rutin 0 .1 Methyl salicylate 0.2 Isoeugenol 0.05 Perfume 0.02 Hydroxyethyl cellulose Residual 100.0%

Claims (1)

[Claims] 1. An oral composition comprising rutin or a glycoside thereof in combination with one or more fragrances selected from limonene, cineol, isoeugenol and menthone.