JP7475718B2 - Oral Care Compositions - Google Patents

Description

The present invention relates to an oral composition that has the effect of preventing and improving periodontal disease.

Periodontal disease is an inflammatory disease caused by bacterial infection. Bacteria in dental plaque cause inflammation of the gums, and if left untreated, it can lead to tooth loss. It is also said that as periodontal disease progresses, periodontal bacteria can be carried to organs throughout the body through capillaries in the oral cavity, potentially causing systemic diseases such as diabetes, pneumonia, arteriosclerosis, and myocardial infarction.

As an oral composition for preventing and improving such periodontal disease, for example, a composition containing pine bark extract has been reported to be effective (see Patent Documents 1 and 2).

Although this pine bark extract has the effect of preventing and improving periodontal disease, further improvements in its effectiveness are required.

WO2005/089784 JP 2001-511153 A

The present invention has been made in consideration of these circumstances, and the objective of the present invention is to provide an oral composition that has excellent preventive and/or ameliorative effects against periodontal disease.

The inventors have been engaged in research into oral care, and as a result of intensive investigations into foods and medicines that can more effectively prevent and/or improve periodontal disease, they have discovered that certain plant materials enhance the effects of pine bark extract in preventing and improving periodontal disease, which led to the completion of the present invention.

That is, the present invention is as follows.
[1] An oral composition for oral care, comprising a pine bark extract and at least one plant material selected from the group consisting of coffee tree, linden tree, kudzu flower, young barley leaves, and young sweet potato leaves.
[2] An oral composition for oral care comprising a pine bark extract as an active ingredient, further comprising at least one plant material selected from the group consisting of coffee tree, linden tree, kudzu flower, young barley leaves, and young sweet potato leaves.
[3] An oral composition comprising a pine bark extract and at least one plant material selected from the group consisting of coffee trees and linden trees.

The oral composition of the present invention has excellent preventive and/or ameliorative effects against periodontal disease.

FIG. 1 shows the growth inhibitory effect of the composition of the present invention (pine bark extract + coffee) against Porphyromonas gingivalis. FIG. 1 shows the growth inhibitory effect of the composition of the present invention (pine bark extract + linden) against Porphyromonas gingivalis. FIG. 1 shows the growth inhibitory effect of the composition of the present invention (pine bark extract + kudzu flower) against Porphyromonas gingivalis. FIG. 1 is a graph showing the growth inhibitory effect of the composition of the present invention (pine bark extract + young barley leaves) against Porphyromonas gingivalis. FIG. 2 is a graph showing the growth inhibitory effect of the composition of the present invention (pine bark extract + young sweet potato leaves) against Porphyromonas gingivalis.

The oral composition of the present invention is characterized by containing a pine bark extract and at least one plant material (sometimes referred to as a secondary material) selected from coffee tree, linden tree, kudzu flower, young barley leaves, and young sweet potato leaves. The secondary material may be used alone (for example, only coffee tree) or in combination of two or more types. When using a combination of two or more types of secondary materials, it is preferable to combine secondary materials that are highly effective in enhancing the effect of the pine bark extract.

The combination of pine bark extract and plant material effectively inhibits the proliferation of Porphyromonas gingivalis, a bacterium that causes periodontal disease, and therefore the oral composition of the present invention can effectively prevent and/or ameliorate periodontal disease. In addition, the oral composition of the present invention can inhibit the bad odor that is generated when Porphyromonas gingivalis metabolizes proteins and amino acids, and can prevent and/or ameliorate the bad breath that is characteristic of periodontal disease.

[Pine bark extract]
The pine bark extract in the oral composition of the present invention contains proanthocyanidin as one of its main components. Proanthocyanidin is a group of compounds consisting of condensation polymers having a degree of polymerization of 2 or more, whose constituent units are flavan-3-ol and/or flavan-3,4-diol.

The raw material for the pine bark extract may be French maritime pine (Pinus Martima), larch, black pine, red pine, Japanese white pine, Japanese white pine, Korean pine, Japanese stone pine, Ryukyu pine, Japanese white pine, giant pine, white pine, etc., of which French maritime pine is preferred. The obtained extract may be concentrated or dried as necessary to form a liquid, paste, or powder. In addition, commercially available pine bark extracts may be used, for example, pine bark extract (Flavangenol (registered trademark)) manufactured by Toyo Shinyaku Co., Ltd.

The pine bark extract in the oral composition of the present invention preferably contains a condensation polymer having a degree of polymerization of 2 or more as a proanthocyanidin. In particular, proanthocyanidins containing a large amount of condensation polymers having a low degree of polymerization are preferred. Examples of condensation polymers having a low degree of polymerization include condensation polymers having a degree of polymerization of 2 to 30 (dimers to 30-mers), preferably condensation polymers having a degree of polymerization of 2 to 10 (dimers to 10-mers), and more preferably condensation polymers having a degree of polymerization of 2 to 4 (dimers to tetramers). In this specification, polymers having a degree of polymerization of 2 to 4 are referred to as OPCs (oligomeric proanthocyanidins). The pine bark extract in the oral composition of the present invention preferably contains 20% by mass or more of OPCs, more preferably 30% by mass or more, and even more preferably 40% by mass or more.

Pine bark extract is obtained by extracting pine bark with water or an organic solvent. When water is used, warm water or hot water is preferably used. As the organic solvent used for extraction, organic solvents acceptable for the production of food or medicine, such as methanol, ethanol, 1-propanol, 2-propanol, 1-butanol, 2-butanol, butane, acetone, hexane, cyclohexane, propylene glycol, aqueous ethanol, aqueous propylene glycol, etc., are preferably used. These water and organic solvents may be used alone or in combination of two or more solvents. In particular, water-soluble solvents such as water, ethanol, aqueous ethanol, etc. are preferably used.

[Plant materials (secondary materials)]
In the present invention, the plant material (secondary material) may be the plant material itself, or a processed product such as crushed product, juice, or extract. Examples of crushed products include powder and granules. The juice or extract may be in liquid form, but can also be used as a paste or dry powder. The extract can be obtained by extraction using a suitable solvent, and examples of the solvent that can be used include water-soluble solvents such as water, ethanol, and aqueous ethanol.
Each plant material will be described below.

(Coffee tree)
The "coffee tree" used in the present invention refers to a plant of the Rubiaceae family and the Coffea genus, and examples that can be used include Coffee arabica, Coffee canephora Pierr., Coffee robusta, and Coffee liberica. The part of the plant used as the plant material of the present invention is preferably the seeds (coffee beans), and although roasted seeds may be used, it is more preferable to use raw, unroasted seeds.

(linden)
Linden trees are plants of the Tiliaceae family, and examples of linden trees that can be used in the present invention include plants of the Tilia genus and Tilia family, such as Tilia platyphyllos Scop., Tilia cordata Mill., and Tilia europaea L. The part of the plant that can be used as the plant material in the present invention is preferably the flower.

(Kudzu flower)
As the kudzu flower, the flower of a plant belonging to the genus Pueraria of the family Fabaceae is used. Kudzu is a creeping perennial plant belonging to the genus Pueraria of the family Fabaceae. As the kudzu flower, the one collected at any stage from bud to fully opened flower can be used, and the ones collected at each stage can be mixed and used. The type of kudzu is not particularly limited, but can be exemplified by Pueraria thomsonii, Pueraria lobata, Pueraria thunbergiana, etc., and Pueraria thomsonii is preferred.

(Young barley leaves)
Barley (Hordeum vulgare L.) is an annual or biennial herb belonging to the family Poaceae, said to be native to Central Asia, and is broadly classified into two-row barley, six-row barley, etc., depending on the panicle shape. The young barley leaves used as the plant material of the present invention are not particularly limited as long as they are normally available, and any young barley leaves, such as two-row barley or six-row barley leaves, may be used. Any variety of young barley leaves may be used. The young barley leaves may include barley leaves, and may also include other parts such as stems.

(Young sweet potato leaves)
Sweet potato is a plant belonging to the Convolvulaceae family, and is generally called "sweet potato." There are no particular limitations on the variety of sweet potato, and examples of the variety include Suio, Joy White, Koganesengan, Shiroyutaka, Satsuma Sachi, and Ayamurasaki.
Among them, sweet potato leaves with high polyphenol content are preferred. The young sweet potato leaves used as the plant material of the present invention may contain young sweet potato leaves, and may also contain other parts such as stems. In particular, the tip part of the stems and leaves (young stems and leaves) is preferred, and young stems and leaves that retain a yellowish green color are even more preferred.

[Oral Composition of the Present Invention]
The oral composition of the present invention can be used, for example, as a medicine (including quasi-drugs), a so-called health food such as a functional food whose efficacy has been approved by a designated organization, such as a food for specified health uses, a food with nutrient function claims, or a food with functional claims, or as a general food, a food additive, a feed, or the like.

The oral composition of the present invention can be used for oral care, particularly for the prevention and/or improvement of periodontal disease. There are no particular limitations on such oral compositions for oral care or for the prevention and/or improvement of periodontal disease, so long as they contain pine resin extract and plant material and can be distinguished from other products as a product in that they are used for oral care or for the prevention and/or improvement of periodontal disease. For example, the scope of the present invention includes products that display on the main body, packaging, instructions, or advertising materials of the product according to the present invention that they are effective for oral care or that they have the effect of preventing and/or improving periodontal disease.

The oral composition for oral care and the oral composition for preventing and/or improving periodontal disease of the present invention are not limited to those labeled on the product packaging, etc., with the combined components of the present invention (pine bark extract + auxiliary material) as the active ingredients for oral care and prevention and/or improvement of periodontal disease. For example, the active ingredient may not be specified. Also, the oral composition may be labeled with only pine bark extract as the active ingredient. In other words, one form of the oral composition for oral care and the oral composition for preventing and/or improving periodontal disease of the present invention may be one that contains pine bark extract as an active ingredient and at least one plant material selected from coffee tree, linden tree, kudzu flower, young barley leaves, and young sweet potato leaves.

Specific examples of the oral composition for oral care and the oral composition for preventing and/or improving periodontal disease of the present invention include medicines (including quasi-drugs) and so-called health foods. Examples of so-called foods include those that are labeled as having an effect of preventing and/or improving periodontal disease, such as "maintaining healthy gums," "suppressing bleeding from the gums," and "reducing periodontal pocket depth."

The oral composition of the present invention may be in the form of, for example, a tablet, capsule, powder, granules, liquid, grain, rod, plate, block, solid, round, paste, cream, caplet, gel, chewable, stick, etc.

The oral composition of the present invention is preferably in the form of an easy-to-ingest tablet, capsule, powder, granule, or liquid, and is particularly preferably in the form of a beverage, chewable tablet, candy, chewing gum, etc. that remains in the oral cavity for a certain period of time. Specific examples include supplements that dissolve in the oral cavity, packaged beverages filled in PET bottles, cans, jars, etc., instant beverages that are dissolved in water (hot water), milk, fruit juice, green juice, etc., and candy, chewing gum, etc. These are preferred because they are easy to drink after meals and can increase palatability.

The content of the pine bark extract and plant material (ingredients of the present invention) in the oral composition of the present invention may be appropriately determined within the range in which the desired effect is achieved.

In general, when the oral composition of the present invention is a pharmaceutical or supplement, the components of the present invention are preferably contained in an amount of 0.1 to 100% by mass, more preferably 1 to 85% by mass, and even more preferably 5 to 70% by mass, of the total mass calculated on a dry weight basis.

In order to more effectively exert the effects of the present invention, the components of the present invention are preferably contained in an amount of 80% or more, more preferably 90% or more, even more preferably 95% or more, and particularly preferably 100% of the total oral composition of the present invention, calculated on a dry mass basis.

The mass ratio of the pine bark extract to the plant material in the oral composition of the present invention is preferably in the range of 1:0.001 to 1:1000, more preferably in the range of 1:0.01 to 1:500, and even more preferably in the range of 1:0.1 to 1:200, calculated on a dry mass basis.

There is no particular limit to the amount of intake of the oral composition of the present invention, but from the viewpoint of more significantly exerting the effects of the present invention, it is preferable for an adult to take pine bark extract in an amount of 0.5 mg/day or more, more preferably 1 mg/day or more, and even more preferably 1.5 mg/day or more per day. The upper limit is, for example, 500 mg/day, preferably 400 mg/day. The oral composition of the present invention is not particularly limited as long as it is for those who require oral care, but it is preferable for it to be taken by adults in their 30s and 40s, about 80% of whom are said to suffer from periodontal disease, and elderly people with weakened gums.

The oral composition of the present invention can be stored as a daily dose in a single container or divided into multiple containers, for example, 2 to 3, so that the daily intake amount is the above-mentioned amount.

The oral composition of the present invention can be produced by a known method by adding, as necessary, components other than the components of the present invention that are acceptable for oral use. Examples of components other than the components of the present invention include vitamins such as water-soluble vitamins (vitamins B1, B2, B3, B5, B6, B12, B13, B15, B17, biotin, choline, folic acid, inositol, PABA, vitamin C, vitamin P) and oil-soluble vitamins (vitamins A, D, E, K); minerals such as calcium, magnesium, phosphorus, and iron; sulfur-containing compounds contained in taurine and garlic; flavanoids or flavonoids such as hesperidin and quercetin; proteins such as collagen; peptides; amino acids; animal fats and oils; vegetable fats and oils; crushed products or extracts of animals and plants, etc.

The present invention will now be described with reference to examples.

[Example 1]
(Test method)
Porphyromonas gingivalis (hereinafter referred to as P. gingivalis) was cultured at 37°C in modified GAM bouillon (manufactured by Nissui Pharmaceutical Co., Ltd.) that had been sterilized by high-pressure steam, in an anaerobic environment created using Anaeropack Kenki (manufactured by Mitsubishi Chemical Corporation) and a square jar (manufactured by Mitsubishi Chemical Corporation).
P. gingivalis was diluted with Dulbecco's phosphate buffered saline (Nacalai Tesque, Inc.) to adjust the turbidity to 0.5 McFarland standard (Sysmex bioMérieux, Inc.) was used as an index of turbidity.

Modified GAM agar medium (manufactured by Nissui Pharmaceutical Co., Ltd.) was sterilized by high-pressure steam and poured into a sterile petri dish to prepare a plate medium. P. gingivalis prepared to the above 0.5 McFarland concentration was evenly applied to the plate medium.

The test substance (pine bark extract and/or secondary material) was prepared to a specified concentration using PBS or DMSO. 15 μL of the test substance was dropped onto 6 mm antibiotic test filter paper (GE Healthcare), which was then attached to the petri dish coated with P. gingivalis.

The bacteria were cultured for 2-3 days in an anaerobic environment at 37°C using Anaeropack Kenki, a square jar, and an incubator.

The diameter of the inhibition circle formed by each test substance in the petri dish was measured and divided by the diameter (6 mm) of the filter paper for antibiotics testing. The growth inhibitory effect of each test substance was corrected by the value obtained by dividing the diameter of the inhibition circle of Isodine, which was placed on each plate as a positive control, by 6 mm (diameter of inhibition circle of test substance - 6 mm (mm) / diameter of inhibition circle of Isodine - 6 mm (mm)). The growth inhibitory effect of each test substance was calculated as a ratio to that of the pine bark extract alone (50 or 100 mg/mL), and the growth inhibitory effect of each test substance against P. gingivalis was evaluated.

The test substances used were the commercially available products or preparations shown below.
[Pine bark extract]
French maritime pine bark extract (Toyo Shinyaku Co., Ltd.; Flavangenol (registered trademark)) was used.

[Secondary material]
For Coffee robusta, commercially available extract powder of coffee seeds (green coffee beans) was used.
For linden tree (Tilia cordata Mill.), a commercially available flower extract powder was used.
For kudzu flowers (Pueraria thomsonii), a powdered extract of the flowers extracted with hot water (Toyo Shinyaku Co., Ltd.) was used.
For the barley leaves, an extract powder was used, which was obtained by extracting crushed barley leaves (Toyo Shinyaku Co., Ltd.) with aqueous ethanol.
For the young sweet potato leaves, an extract powder was used, which was obtained by extracting crushed powder (Toyo Shinyaku Co., Ltd.) with aqueous ethanol.

The evaluation results of the growth inhibitory effect of each test substance on P. gingivalis are shown in Figures 1 to 5. In the figures, FVG stands for pine bark extract (Flavangenol (registered trademark)).

As shown in Figures 1 to 5, it can be seen that the growth of P. gingivalis is effectively inhibited by combining pine bark extract with specific plant materials. In particular, although coffee tree, linden tree, young barley leaves, and young sweet potato leaves have weak or no effect when used alone, when combined with pine bark extract, the growth inhibitory effect against P. gingivalis is effectively enhanced. Kudzu flower itself has a growth inhibitory effect, but this effect is further enhanced when combined with pine bark extract. Therefore, it can be seen that the oral composition of the present invention is an excellent oral composition for oral care that effectively inhibits the growth of P. gingivalis, thereby preventing and/or improving periodontal disease and preventing and/or improving bad breath that is specific to periodontal disease.

[Example 2] (Preparation of tablets)
Pine bark extract 12mg
Linden extract powder (flower derived) 200mg
Sucrose fatty acid ester 350mg
Shellac 10mg
Fragrance 2mg
Reduced maltose remainder
The mixture was compressed into four 300 mg tablets.

[Example 3] (Production of chewable tablets)
Pine bark extract 1.5mg
Coffee extract powder (derived from green coffee beans) 150mg
Hydroxypropyl cellulose 250mg
Sucrose fatty acid ester 50mg
Aspartame 30mg
Fragrance 3mg
Reduced maltose remainder
The mixture was compressed into two 500 mg chewable tablets.

[Example 4] (Preparation of granules)
Pine bark extract 50mg
Barley leaf powder 2000mg
Fructooligosaccharides 200mg
Reduced maltose remainder
The mixture was mixed and then granulated to produce 3 g of granules.

[Example 5] (Preparation of powder)
Pine bark extract 100mg
Sweet potato leaf powder 1500mg
Tea extract 50mg
Dextrin Remainder
The mixture was mixed to prepare 3 g of a powder.

[Example 6] (Production of candy)
Pine bark extract 30mg
Coffee extract powder (derived from green coffee beans) 50mg
Linden extract powder (flower derived) 20mg
Sweeteners (aspartame, L-phenylalanine compounds,
Acesulfame K, stevia) 30mg
Fragrance 10mg
Reduced maltose syrup Remainder
One candy weighing 3 g was prepared according to a conventional method.

[Example 7] (Production of bottled beverage)
Pine bark extract 200mg
Kudzu flower extract 35mg
Black tea leaf extract powder 500mg
Sodium ascorbate 50mg
Water Remaining
A 350 ml bottled beverage consisting of the above was produced in a conventional manner.

The oral composition of the present invention can be used as a health food or the like that has a high periodontal disease prevention and/or improvement effect, and therefore the present invention is highly useful industrially.

Claims (1)

An oral composition for oral care comprising a pine bark extract as an active ingredient, the oral composition further comprising linden.