JP2005053830A - Preparation for external use for oral cavity disease - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a preparation for oral cavities useful for preventing and treating periodontoses. <P>SOLUTION: This preparation for external use for oral cavity diseases contains an extract from a plant belonging to the genus Thujopsis of the family cypress as the active ingredient. Specifically, in this preparation, the oral cavity diseases are periodontoses (pyorrhea alveolaris). <P>COPYRIGHT: (C)2005,JPO&NCIPI

Description

  The present invention relates to an oral and external preparation for oral diseases useful for the prevention and treatment of periodontal diseases such as periodontal disease (alveolar pyorrhea).

Periodontal disease is a disease caused by periodontopathic bacteria, and is a disease that occurs in the periodontal tissue composed of the gums, periodontal ligament, cementum and alveolar bone that support the teeth. As symptoms progress, strong connective tissue destruction (inflammation) occurs in the adherent epithelium, gingival connective tissue, periodontal ligament, and the like, resulting in absorption of the alveolar bone that supports the teeth, resulting in loss of teeth. This is the main cause of losing teeth. Conventionally, non-steroidal anti-inflammatory agents such as flurbiprofen (Non-patent document 1) and indomethacin (Non-patent document 2) have been reported to be effective as preventive or therapeutic agents for periodontal disease. . Furthermore, Patent Document 1 describes that ibuprofen and flurbiprofen have an alveolar bone resorption inhibitory effect.
J. Periodont. Res., 23, 166-169, 1988 J. Periodont. Res., 17, 90-100, 1982 JP-A-60-61524

  However, there is a concern that the use of these anti-inflammatory agents for a long time may cause harmful effects on the oral mucosa. For the prevention and treatment of periodontal disease, which is a chronic disease, it is desirable to use a drug that is safe even when used in the oral cavity for a long period of time. The development of an excellent drug has been desired.

  The present inventors have been searching for extracts of various medicinal plants using a periodontal disease model using the first molars of golden hamsters. It was found that the progression of periodontal disease is delayed by applying it externally in the oral cavity.

  That is, this invention provides the oral disease external preparation for oral diseases which uses the extract of a cypress Asunaro plant as an active ingredient.

  The intraoral external preparation for oral diseases of the present invention is useful for prevention or treatment of tooth loss caused by periodontal disease.

A hot water extract of a cypress Asunaro genus plant used in the oral cavity external preparation for oral diseases of the present invention, for example, a cypress Asunaro leaves, is used as a folk medicine for a strong liver.
Thus, although the raw material plant suitably used for obtaining the plant extract of the present invention is already known as a herbal medicine, its component has been effective for the prevention or treatment of periodontal disease so far. There was no finding that there was.

The extract of the Asanaro genus plant that is an active ingredient of the oral cavity external preparation for oral disease of the present invention is obtained by using a solvent that can effectively extract the active ingredient from the raw materials of the plant body such as leaves and twigs of the genus Asunaro. It can be obtained by extraction or partial purification of these.
The solvent used in this extraction is not particularly limited as long as it can efficiently extract the active ingredient, but for example, water or water such as lower alcohols such as acetone, methanol, ethanol, and propanol. It is preferable to use an organic solvent that is miscible with or a mixture thereof, esters such as ethyl acetate, and the like.
In the extraction of the active ingredient, the raw materials can be extracted as they are with these solvents, but it is preferable to extract these raw materials into fine pieces and then extract them with a solvent in order to increase the extraction efficiency. Furthermore, the extraction efficiency can be increased by repeating the extraction 2 to 4 times.
Furthermore, in order to increase the concentration of the active ingredient in the extract, the obtained extract may be further subjected to means such as concentration, liquid-liquid distribution, adsorption chromatography, normal phase or reverse phase chromatography, if desired. Is possible.

Next, the periodontal disease progression delaying effect of the extract of the genus Asunaro which is an active ingredient of the present invention will be described.
Golden hamster has been used by many researchers since it was used in the experimental system of Keyes et al. (Arch Oral Biol 9,377-400 (1964)) and has been highly evaluated as a periodontal disease model. This time, the present inventors created a periodontal disease model by wrapping silk thread around the mandibular first molar of a golden hamster with reference to the method of Mori et al. (Gifu Univ. 43; 758-767 (1995)). . When the silkworm is wound around the first molar of the lower jaw of a golden hamster, plaque is easily formed in the molar gingival crevice wound with the silk thread, and inflammation is caused. When this state is maintained for a long time, the alveolar bone supporting the teeth is absorbed, and a model having similarity to human periodontal disease can be created.
Using this periodontal disease model, the present inventors applied various medicinal plant extracts to the gums in which periodontal disease occurred daily, and the extract of the cypress Asunaro genus plant showed the progression of periodontal disease. I found it to suppress. That is, the extract of the genus Asnalo of the present invention suppresses alveolar bone resorption associated with the progression of periodontal disease, and is useful as an agent for oral diseases typified by periodontal disease.

  The intraoral external preparation for oral diseases of the present invention is an external preparation to which an active ingredient can be applied in the oral cavity. As the dosage form of such an oral preparation for oral use, dentifrice, liquid dentifrice, liquid dentifrice, moisturized dentifrice, mouthwash, mouthwash, mouthspray, ointment, cream and the like can be used. The oral cavity external preparation for oral diseases of the present invention is a component used in oral compositions, such as foaming agents, foaming aids, surfactants, abrasives, bulking agents, sweeteners, preservatives, other medicinal ingredients, A pH adjuster, an adhesive, a pigment, a coloring matter, a fragrance, and the like can be appropriately blended. Moreover, the intraoral external preparation of this invention can also supply an agent in an oral cavity with the form of chewing gum.

  Examples of other medicinal ingredients include fungicides such as triclosan, chlorhexidine and benzethonium chloride, enzyme inhibitors such as polyphenols (glucosyltransferase inhibitory action), and anti-inflammatory agents such as dipotassium glycyrrhizinate.

  Sweeteners include oligosaccharides or sugar alcohols such as xylo-oligosaccharides, fructooligosaccharides, galactooligosaccharides, soybean oligosaccharides, isomalto-oligosaccharides, dairy oligosaccharides, lactulose, raffinose, trehalose, glucosyl sucrose, maltosilche. Claus, palatinose, maltitol, erythritol, reduced palatinose, xylitol and the like are preferable examples.

  The content of the Asanaro plant extract in the oral cavity external preparation for oral disease of the present invention is 0.001 to 10% by mass, further 0.1 to 5% by mass, particularly 0.5 to 3% by mass in terms of dry matter. Is preferred.

Production Example 1
Production of Asunaro Extract (1): 1 kg of Asunaro (leaf / twig mixture) pulverized product was immersed in 8 liters of ethanol at room temperature for 7 days to extract ethanol-soluble components. Subsequently, the same operation was performed again on the residue from which the extract was separated, and a total of 16 liters of extract was obtained. The solvent of this extract was distilled off and dried under reduced pressure to obtain 80 g of an extract.

Production Example 2
Production of Asunaro Extract (2): 1 kg of Asunaro (leaf / twig mixture) pulverized product was immersed in 8 liters of ethanol at room temperature for 7 days to extract ethanol-soluble components. Subsequently, the same operation was performed again for the residue separated from the extract to obtain a total of 16 liters of extract. After distilling off the solvent of this extract and concentrating to 1 liter, 30 g of activated carbon was added, and the mixture was stirred for 6 hours, subjected to deodorization / decoloration treatment, then the activated carbon was filtered off, and the filtrate was concentrated under reduced pressure. 65 g of product was obtained as a syrup.

Test example 1
Periodontal disease progression delay effect using a golden hamster periodontal disease model A double silk thread was tied to the neck of the first molar of the right lower jaw of a golden hamster (9 weeks old). In this state, Diet2000 (made by Oriental) and drinking water were reared for 3 weeks under free feeding. Three weeks after the breeding, the silk of the first molar was removed, and the following agents were injected into the formed periodontal pocket once / day with a root canal syringe. (5mg)

(1) Control: white petrolatum that is an ointment base material (2) Asnalo extract: kneaded so that the white salmon extract that is an ointment base material is 5% by mass of the asunalo extract extracted in Production Example 2

  Three weeks later, the mandible was removed, the mandible was stained with toluidine blue, image analysis was performed, and the remaining area of the alveolar bone was determined and compared with the control treatment group.

  As a result, as shown in FIG. 1, it was found that the treatment with Asunaro extract showed an effect of suppressing mandible resorption. Therefore, asunalo extract suppresses alveolar bone resorption associated with the progression of periodontal disease, and asunalo extract is useful as a prophylactic / therapeutic agent for periodontal disease.

Example 1
A dentifrice was prepared according to a conventional method using the following ingredients.
Asunaro extract 1.0 (mass%)
Silica 30
Sorbitol 30
Sodium lauryl sulfate 1.0
Carboxymethylcellulose 1.0
Saccharin 0.1
Perfume appropriate amount water balance
100% by mass

Example 2
A mouthwash was prepared according to a conventional method using the following components.
Asunaro extract 1.0 (mass%)
Ethanol 20
Sodium pyrophosphate 2
Saccharin 0.1
Perfume appropriate amount water balance
100% by mass

It is a figure which shows the alveolar bone resorption suppression effect of an asunalo extract.

Claims (2)

  An intraoral external preparation for oral diseases comprising an extract of a cypress Asunaro genus plant as an active ingredient.   The oral preparation for oral use according to claim 1, wherein the oral disease is periodontal disease (alveolar pyorrhea).

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