JP2005162654A - Composition for preventing or treating periodontal disease - Google Patents
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本発明は、歯肉の炎症に対する抗炎症効果が高く、歯周病の予防や治療効果に優れ、渋みの少ない歯周病予防又は治療用組成物に関する。 The present invention relates to a composition for preventing or treating periodontal disease, which has a high anti-inflammatory effect on inflammation of gingiva, is excellent in preventing and treating periodontal disease, and has little astringency.
歯周病は、作用因子、環境、宿主等からなる多因性疾患である。この予防や治療を目的として、例えば、局所的作用因子を対象にして、歯周病原細菌の殺菌、歯周組織の血流改善、組織賦活、炎症改善、出血防止等を目的としたトラネキサム酸、アラントイン、イプシロンアミノカプロン酸、リゾチーム、塩化ナトリウム、ジヒドロコレステロール、β−グリチルレチン酸等の薬効成分が使用されている。しかしながら、歯周病の病巣部では歯周病原細菌は、バイオフィルムを形成することで殺菌・抗菌剤に対する抵抗力を有しており、これらの薬効成分を用いても歯周病の予防治療効果は不充分であった（非特許文献１）。 Periodontal disease is a multifactorial disease consisting of an agent, environment, host and the like. For the purpose of this prevention and treatment, for example, targeting local agents, tranexamic acid for the purpose of sterilizing periodontopathic bacteria, improving blood flow of periodontal tissue, activating tissue, improving inflammation, preventing bleeding, Medicinal ingredients such as allantoin, epsilon aminocaproic acid, lysozyme, sodium chloride, dihydrocholesterol, β-glycyrrhetinic acid are used. However, periodontal pathogenic bacteria have a resistance to bactericidal and antibacterial agents by forming biofilms in the foci of periodontal diseases, and even if these medicinal ingredients are used, preventive and therapeutic effects on periodontal diseases Was insufficient (Non-patent Document 1).
また、歯周病の予防や治療を目的に、安全性の観点から食経験のある植物抽出物としてポリフェノールが検討されてきた。例えば、茶抽出物を含有する抗う蝕及び抗歯周病組成物（特許文献１）、果実ポリフェノール含有果汁を含むアレルギー抑制剤、抗う蝕剤、消臭剤（特許文献２）、ホップポリフェノールを含有する抗う蝕素材（特許文献３）、ブドウ種子抽出物とビタミンＣやＥを含有する歯周病の予防又は治療用の食品組成物、口腔用組成物（特許文献４）、５％茶カテキン含浸ストリップスの歯周病改善効果（非特許文献２）等が提案されている。しかし、いずれも歯周病の予防治療効果が不充分だったり、ポリフェノールの含有量が多いほど渋みが強すぎるという問題があった。 In addition, for the purpose of preventing and treating periodontal diseases, polyphenols have been studied as plant extracts with dietary experience from the viewpoint of safety. For example, an anti-cariogenic and anti-periodontal disease composition containing tea extract (Patent Document 1), an allergy inhibitor including fruit polyphenol-containing fruit juice, an anti-cariogenic agent, a deodorant (Patent Document 2), and a hop polyphenol Anti-Caries material (Patent Document 3), Grape seed extract and food composition for prevention or treatment of periodontal disease containing vitamins C and E, oral composition (Patent Document 4), 5% tea catechin impregnation The periodontal disease improving effect of Non-patent Document 2 (Non-Patent Document 2) has been proposed. However, there are problems that the preventive and therapeutic effects of periodontal disease are insufficient, and that the astringency is too strong as the polyphenol content increases.
一方、特定のナフタレン誘導体（リグナン類）やこれを含有するメギ科ポドフィルム属、セリ科ノトプテリジウム属、ヒノキ科アスナロ属の植物抽出物は、骨疾患の予防や治療効果を有すること（特許文献５、６）、アスナロ抽出物が細胞接着抑制効果を有することに関する報告はある（特許文献７）が、バイオフィルムが存在する歯肉における抗炎症効果については不明であった。
また、アスナロ属植物の抽出物がう蝕の原因菌とされるストレプトコッカス ミュータンスに対して抗菌作用を示すこと知られている（特許文献８）が、、歯周病の予防治療効果は知られていない。
In addition, it is known that an extract of the plant of the genus Asunaro has antibacterial activity against Streptococcus mutans, which is a causative agent of caries (Patent Document 8), but the preventive and therapeutic effect of periodontal disease is known. Not.
本発明の目的は、バイオフィルムを形成している歯周病原細菌により誘発される歯周病に対して、歯肉の炎症に対する抗炎症効果が高く、歯周病予防治療効果の優れた、渋みの少ない歯周病予防又は治療用組成物を提供することにある。 The object of the present invention is to have a high anti-inflammatory effect on gingival inflammation against periodontal disease induced by periodontopathic bacteria forming a biofilm, and has an excellent periodontal disease prevention and treatment effect. The object is to provide a composition for the prevention or treatment of periodontal disease with a small amount.
本発明者は、特定のリグナン類又はこれを含有する植物抽出物が歯肉の炎症に対する抗炎症作用を有することを見出し、さらに検討した結果、ポリフェノールと特定のリグナン類又はこれらを含有する植物抽出物の併用がバイオフィルムの存在下でも歯肉の炎症に対する抗炎症効果が高く、歯周病の予防治療に極めて有効であることを見出した。 The present inventor has found that a specific lignan or a plant extract containing the same has an anti-inflammatory action on inflammation of gingiva, and as a result of further investigation, as a result of studying polyphenol and a specific lignan or a plant extract containing these. It has been found that the combined use has a high anti-inflammatory effect on gingival inflammation even in the presence of biofilm, and is extremely effective in preventing and treating periodontal disease.
すなわち、本発明は、ポリフェノール及び次の式（１） That is, the present invention provides a polyphenol and the following formula (1):
（式中、Ｒ1は水素原子又は水酸基を示し、Ｒ2、Ｒ3、Ｒ4及びＲ5は同一又は異なって水素原子、水酸基、炭素数１〜１０のアルキル基、炭素数１〜１０のヒドロキシアルキル基又は炭素数１〜１０のアルコキシ基を示す。）で表されるリグナン類又は当該リグナン類を含有する植物抽出物を含有する歯周病予防又は治療用組成物を提供するものである。 (In the formula, R 1 represents a hydrogen atom or a hydroxyl group, and R 2 , R 3 , R 4 and R 5 are the same or different and each represents a hydrogen atom, a hydroxyl group, an alkyl group having 1 to 10 carbon atoms, or a group having 1 to 10 carbon atoms. It represents a hydroxyalkyl group or an alkoxy group having 1 to 10 carbon atoms.) And a composition for preventing or treating periodontal disease comprising a lignan represented by the above or a plant extract containing the lignan. .
本発明によれば、短期間で歯周病を軽減改善できるという歯周病予防治療効果に優れた組成物が提供できる。また、本発明の歯周病予防又は治療用組成物は渋みが少なく使用感に優れているため長期間口腔への適用が可能である。 ADVANTAGE OF THE INVENTION According to this invention, the composition excellent in the periodontal disease prevention-treatment effect that periodontal disease can be reduced and improved in a short period can be provided. In addition, the composition for preventing or treating periodontal disease of the present invention has little astringency and excellent usability, and therefore can be applied to the oral cavity for a long period of time.
ポリフェノールとは、水酸基を２つ以上持つフェノール化合物の総称であり、本発明に使用されるポリフェノールは、特に限定されるものではないが、茶、ブドウ果実、リンゴ果実等の食経験のある植物からの抽出物が好ましく、中でも茶抽出物はその成分や機能性研究がなされており、商業的にも入手可能な点から特に好ましい。 Polyphenol is a general term for phenolic compounds having two or more hydroxyl groups, and the polyphenol used in the present invention is not particularly limited, but it is derived from plants having experience of eating such as tea, grape fruit and apple fruit. In particular, the tea extract has been studied for its components and functionality, and is particularly preferable from the viewpoint of being commercially available.
本発明で使用されるポリフェノールは、歯周病予防治療効果の点からは本発明の組成物中に０．００００１重量％以上含有することが好ましく、ポリフェノールの渋み軽減の点から、その含有量は８重量％以下が好ましい。さらに好ましくは０．０００１〜４重量％であり、０．００１〜２重量％含有させるのが特に好ましい。 The polyphenol used in the present invention is preferably contained in the composition of the present invention in an amount of 0.00001% by weight or more from the viewpoint of periodontal disease prevention and treatment effect, and from the viewpoint of reducing the astringency of the polyphenol, its content is It is preferably 8% by weight or less. More preferably, it is 0.0001 to 4 weight%, and it is especially preferable to make it contain 0.001 to 2 weight%.
本発明で使用するリグナン類は、前記式（１）で表されるものである。式（１）中、炭素数１〜１０のアルキル基とは直鎖又は分岐鎖のアルキル基を意味し、例えばメチル基、エチル基、プロピル基、イソプロピル基、ブチル基、イソブチル基、tert−ブチル基、ペンチル基、ヘキシル基、ヘプチル基、オクチル基、ノニル基、デシル基等が挙げられる。炭素数１〜１０のヒドロキシアルキル基とは、直鎖又は分岐鎖のアルキル基を意味し、例えば、ヒドロキシメチル基、ヒドロキシエチル基、ヒドロキシプロピル基、ヒドロキシイソプロピル基、ヒドロキシブチル基、ヒドロキシイソブチル基、ヒドロキシｔｅｒｔ−ブチル基、ヒドロキシペンチル基、ヒドロキシヘキシル基、ヒドロキシヘプチル基、ヒドロキシオクチル基、ヒドロキシノニル基、ヒドロキシデシル基等を挙げることができる。また炭素数１〜１０のアルコキシ基とは直鎖又は分岐鎖のアルコキシ基を意味し、例えばメトキシ基、エトキシ基、ｎ−プロピルオキシ基、イソプロピルオキシ基、ｎ−ブチルオキシ基、sec−ブチルオキシ基、tert−ブチルオキシ基、ペンチルオキシ基、ヘキシルオキシ基、ヘプチルオキシ基、オクチルオキシ基、ノニルオキシ基、デシルオキシ基等を挙げることができる。 The lignans used in the present invention are those represented by the above formula (1). In formula (1), a C1-C10 alkyl group means a linear or branched alkyl group, for example, a methyl group, an ethyl group, a propyl group, an isopropyl group, a butyl group, an isobutyl group, tert-butyl. Group, pentyl group, hexyl group, heptyl group, octyl group, nonyl group, decyl group and the like. A C1-C10 hydroxyalkyl group means a linear or branched alkyl group, for example, a hydroxymethyl group, a hydroxyethyl group, a hydroxypropyl group, a hydroxyisopropyl group, a hydroxybutyl group, a hydroxyisobutyl group, A hydroxy tert-butyl group, a hydroxypentyl group, a hydroxyhexyl group, a hydroxyheptyl group, a hydroxyoctyl group, a hydroxynonyl group, a hydroxydecyl group, and the like can be given. Moreover, a C1-C10 alkoxy group means a linear or branched alkoxy group, for example, a methoxy group, an ethoxy group, n-propyloxy group, isopropyloxy group, n-butyloxy group, sec-butyloxy group, Examples thereof include a tert-butyloxy group, a pentyloxy group, a hexyloxy group, a heptyloxy group, an octyloxy group, a nonyloxy group, and a decyloxy group.
式（１）中、Ｒ2としては水素原子、水酸基又は炭素数１〜３のアルコキシ基がより好ましく、水素原子が特に好ましい。Ｒ3、Ｒ4及びＲ5としては、水酸基又は炭素数１〜３のアルコキシ基がより好ましく、メトキシ基が特に好ましい。 In formula (1), R 2 is more preferably a hydrogen atom, a hydroxyl group or an alkoxy group having 1 to 3 carbon atoms, and particularly preferably a hydrogen atom. R 3 , R 4 and R 5 are more preferably a hydroxyl group or an alkoxy group having 1 to 3 carbon atoms, and particularly preferably a methoxy group.
本発明で使用する式（１）のリグナン類の具体例としては、α−ペルタチン、β−ペルタチン、デオキシ−β−ペルタチン、β−ペルタチン メチルエーテル、ポドフィロトキシン、デソキシポドフィロトキシン、４′−デメチルポドフィロトキシン等が挙げられる。このうち、α−ペルタチン、β−ペルタチン、デオキシ−β−ペルタチン、β−ペルタチン メチルエーテルが好ましい。ここで式（１）のリグナン類は、歯肉の細胞においてバイオフィルム中の細菌からのＬＰＳなどの刺激物質により誘導されるＩＬ−１などの炎症性サイトカインの産生を抑えることで抗炎症効果も発揮するものと考えられる。 Specific examples of the lignans of the formula (1) used in the present invention include α-pertatin, β-pertatin, deoxy-β-pertatin, β-pertatin methyl ether, podophyllotoxin, desoxypodophyllotoxin, Examples include 4'-demethylpodophyllotoxin. Of these, α-pertatin, β-pertatin, deoxy-β-pertatin and β-pertatin methyl ether are preferred. Here, the lignans of formula (1) also exert anti-inflammatory effects by suppressing the production of inflammatory cytokines such as IL-1 induced by stimulating substances such as LPS from bacteria in biofilms in gingival cells. It is thought to do.
式（１）で表されるリグナン類は、文献記載の方法（Natural Product Report, 183-185(1995)、Tetrahedron Lett. 2759-2762(1969)、Chem. Pharm. Bull. 18(6)1150-1155(1972)等）により合成することもできる。 The lignans represented by formula (1) can be obtained by methods described in the literature (Natural Product Report, 183-185 (1995), Tetrahedron Lett. 2759-2762 (1969), Chem. Pharm. Bull. 18 (6) 1150- 1155 (1972) etc.).
本発明で使用する植物抽出物としては、前記式（１）のリグナン類を含有していれば特に制限されないが、ヒノキ科アスナロ属、メギ科ポドフィルム属及びセリ科ノトプテリジウム属から選ばれる１種又は２種以上の植物の抽出物が好ましい。当該ヒノキ科アスナロ属植物の抽出物は、ヒノキ科のアスナロ（Thujopsis dolabrata）の葉部や小枝部等から、メギ科ポドフィルム属植物の抽出物は、ポドフィルム・ペルタタム（Podophyllum Peltatum）、ポドフィルム・エモディ（Podophyllum emodi）、ミヤオソウ（Podophyllum pleianthum）、ポドフィルム・ベルシピレ（Podophyllum versipelle）の根茎部等から、セリ科ノトプテリジウム属の植物の抽出物は、漢方名・羌活（Notopterygium insisum）、同・寛葉羌活（Notopterygium forbesii）、同・川羌活（Notopterygium franchetii）の根茎部等から抽出されるものが好ましい。 The plant extract used in the present invention is not particularly limited as long as it contains the lignans of the above formula (1), but one or more species selected from the genus Asaro, Cypressaceae, Two or more plant extracts are preferred. The cypress Asunaro plant extracts are from the leaves and twigs of the cypress Asunaro (Thujopsis dolabrata). From the rhizomes of Podophyllum emodi, Podophyllum pleianthum, and Podophyllum versipelle, the extracts of the genus Nottopteridium belong to the Chinese name, Notopterygium insisum, Notopterygium forbesii), and those extracted from the rhizomes of Notopterygium franchetii.
本発明で使用する前記植物抽出物は、葉部や小枝部等（以下「原体」と称する）を乾燥又は乾燥することなく粉砕した後、常温下又は加温下で溶剤により、又はソックスレー抽出器等の抽出器具を用いて抽出することにより得ることができる。なお、本発明における植物抽出物としては、各種溶媒抽出液又はその希釈液、濃縮液もしくは乾燥末が好ましい。 The plant extract used in the present invention is obtained by pulverizing a leaf portion, a twig portion or the like (hereinafter referred to as “raw material”) without drying or drying, and then using a solvent at room temperature or under heating, or Soxhlet extraction. It can obtain by extracting using extraction tools, such as a container. In addition, as a plant extract in this invention, various solvent extracts, its dilution liquid, a concentrate, or a dry powder is preferable.
ここで溶媒抽出物は、原体又はその乾燥末を水、有機溶媒（石油エーテル、ｎ−ヘキサン、シクロヘキサン、トルエン、ベンゼン等の炭化水素系溶媒；ジクロロメタン、クロロホルム、四塩化炭素等のハロゲン化炭化水素類；ジエチルエーテル等のエーテル系溶媒；酢酸エチル等のエステル系溶媒；アセトン等のケトン類；ピリジン等の塩基性溶媒；ブタノール、プロパノール、エタノール、メタノール、ポリエチレングリコール、プロピレングリコール、ブチレングリコール等の一価又は多価アルコール系溶媒など）、水性アルコール等を用い、通常３〜７０℃で抽出処理することにより得られる。 Here, the solvent extract is the raw material or its dry powder, water, organic solvent (hydrocarbon solvents such as petroleum ether, n-hexane, cyclohexane, toluene, benzene; halogenated carbonization such as dichloromethane, chloroform, carbon tetrachloride, etc. Hydrogen; ether solvents such as diethyl ether; ester solvents such as ethyl acetate; ketones such as acetone; basic solvents such as pyridine; butanol, propanol, ethanol, methanol, polyethylene glycol, propylene glycol, butylene glycol, etc. Monovalent or polyhydric alcohol solvents, etc.), aqueous alcohols, etc., are usually used for extraction treatment at 3 to 70 ° C.
原体からの好ましい具体的抽出例としては、乾燥粉砕物１００ｇをエタノール１リットルに浸漬し、室温で時々撹拌しながら７日間抽出を行い、得られた抽出液をろ過し、ろ液を５℃で３日間静置した後、再度ろ過して上澄みを得る方法が挙げられる。 As a preferable specific example of extraction from the raw material, 100 g of a dry pulverized product is immersed in 1 liter of ethanol, extracted for 7 days with occasional stirring at room temperature, the obtained extract is filtered, and the filtrate is 5 ° C. And a method of obtaining a supernatant by filtering again after standing for 3 days.
得られた植物抽出物は、そのまま、又は希釈、濃縮もしくは凍結乾燥した後、粉末状又はペースト状に調製し、適宜製剤化して用いることができる。また、さらに必要により活性炭等を用いて脱臭、脱色等の精製処理を施してから用いることもできる。 The obtained plant extract can be used as it is or after diluting, concentrating or lyophilizing it, preparing it in powder form or paste form, and formulating it appropriately. Further, if necessary, the product can be used after subjecting it to purification treatment such as deodorization and decoloration using activated carbon or the like.
式（１）で表されるリグナン類は、本発明の組成物中に０．００００１〜２重量％、さらに０．０００１〜１重量％、特に０．００１〜０．５重量％含有させるのが好ましい。一般的な方法で調製した前記の植物抽出物の中には、式（１）のリグナン類を０．０００１〜１０重量％含有することから、前記植物抽出物は、本発明の組成物中に０．０００１〜９０重量％、さらに０．００１〜５０重量％、特に０．０１〜５重量％含有させるのが好ましい。 The lignan represented by the formula (1) is contained in the composition of the present invention in an amount of 0.00001 to 2% by weight, more preferably 0.0001 to 1% by weight, particularly 0.001 to 0.5% by weight. preferable. The plant extract prepared by a general method contains 0.0001 to 10% by weight of the lignans of the formula (1). Therefore, the plant extract is contained in the composition of the present invention. It is preferable to contain 0.0001 to 90% by weight, further 0.001 to 50% by weight, and particularly 0.01 to 5% by weight.
本発明歯周病予防又は治療用組成物においては、歯周病原因菌バイオフィルムが形成されていても歯肉の炎症に対する抗炎症効果を高めるという点から、式（１）のリグナン類：ポリフェノールの含有比（重量比）が １：１０００〜１００：１であることが好ましく、 １：１００〜１０：１が特に好ましい。 In the composition for preventing or treating periodontal disease of the present invention, the lignans of the formula (1): polyphenols are used because they increase the anti-inflammatory effect against inflammation of the gums even if periodontal disease-causing biofilms are formed. The content ratio (weight ratio) is preferably 1: 1000 to 100: 1, particularly preferably 1: 100 to 10: 1.
本発明の歯周病予防又は治療用組成物は、ポリフェノール及び式（１）のリグナン類又はこれを含有する植物抽出物の他に、通常の口腔用組成物に配合される成分を用いることで、軟膏、練歯磨剤、液体歯磨剤、洗口剤、口腔用パスタ、歯ぐきマッサージクリーム等の態様にすることができる。また、本発明の他の成分としては、上記の口腔用組成物の種類、使用目的等に応じて通常使用される適宜な成分が配合され得る。 The composition for preventing or treating periodontal disease of the present invention is obtained by using components blended in a normal oral composition in addition to polyphenols and lignans of formula (1) or plant extracts containing the same. , Ointments, toothpastes, liquid dentifrices, mouthwashes, oral pasta, gum massage creams and the like. In addition, as other components of the present invention, appropriate components that are usually used may be blended depending on the type of oral composition and the purpose of use.
本発明の組成物には、さらにポリオールを含有させることでポリフェノールによる渋みが低減される。ポリオールとしては、例えば、グリセリン、ソルビトール、キシリトール、エリスリトール、パラチトール、トレハロース等が挙げられる。ポリオールの含有量は、本発明の組成物中、１〜９０重量％、さらに５〜７０重量％、特に１０〜５０重量％が好ましい。 By adding a polyol to the composition of the present invention, the astringency due to polyphenol is reduced. Examples of the polyol include glycerin, sorbitol, xylitol, erythritol, paratitol, trehalose and the like. The content of the polyol is preferably 1 to 90% by weight, more preferably 5 to 70% by weight, and particularly preferably 10 to 50% by weight in the composition of the present invention.
また、ポリフェノールを含む抽出物は酸化重合しやすいため、本発明の組成物中には、ｌ−アスコルビン酸やｌ−アスコルビン酸ナトリウムなどの酸化防止剤を配合することが好ましい。 Moreover, since the extract containing a polyphenol is easy to oxidatively polymerize, it is preferable to mix | blend antioxidants, such as l-ascorbic acid and sodium l-ascorbate, in the composition of this invention.
使用目的に応じて適量使用される成分のうち、特に配合が好ましい成分としては、バイオフィルム除去するプラークコントロールによる相乗効果が期待される炭酸カルシウム、水酸化アルミニウム、無水ケイ酸、含水ケイ酸、第２リン酸カルシウム・２水和物、第２リン酸カルシウム（無水物）、アルミナ等の研磨剤や塩化ベンゼトニウム、塩化ベンザルコニウム、塩化セチルピリジニウム、トリクロサン、塩酸クロルヘキシジン、グルコン酸クロルヘキシジン、イソプロピルメチルフェノール、塩酸アルキルジアミノエチルグリシン、塩化デカリニウム等の殺菌剤が挙げられる。さらに、アラントイン、アラントインクロルヒドロキシアルミニウム、グリチルリチン酸ジカリウム、β−グリチルレチン酸、ジヒドロコレステロール、塩化リゾチーム、酢酸トコフェロール等の抗炎症剤も挙げられる。また、歯の脱灰抑制や再石灰化促進のために、フッ化ナトリウム、フッ化スズ、モノフルオロリン酸ナトリウム等のフッ化物を用いることができる。 Among the components to be used in an appropriate amount depending on the purpose of use, the components that are particularly preferable to be blended are calcium carbonate, aluminum hydroxide, anhydrous silicic acid, hydrous silicic acid, Abrasives such as dicalcium phosphate dihydrate, dicalcium phosphate (anhydride), alumina, benzethonium chloride, benzalkonium chloride, cetylpyridinium chloride, triclosan, chlorhexidine hydrochloride, chlorhexidine gluconate, isopropylmethylphenol, alkyldiamino hydrochloride Examples include bactericides such as ethyl glycine and decalinium chloride. Furthermore, anti-inflammatory agents such as allantoin, allantoinchlorohydroxyaluminum, dipotassium glycyrrhizinate, β-glycyrrhetinic acid, dihydrocholesterol, lysozyme chloride, tocopherol acetate and the like can also be mentioned. Further, fluorides such as sodium fluoride, tin fluoride and sodium monofluorophosphate can be used to suppress decalcification of teeth and promote remineralization.
賦形剤や粘結剤として、カルボキシメチルセルロース、ヒドロキシエチルセルロース、カラギーナン、キサンタンガム、アルギン酸ナトリウム、ポリアクリル酸ナトリウム、ポリチレングリコール、ポリビニルピロリドン、シリカゲル、ゲル化炭化水素（流動パラフィンをポリエチレン樹脂でゲル化したもの）、ワセリン等を配合することが好ましい。 As excipients and binders, carboxymethylcellulose, hydroxyethylcellulose, carrageenan, xanthan gum, sodium alginate, sodium polyacrylate, polyethylene glycol, polyvinylpyrrolidone, silica gel, gelled hydrocarbon (liquid paraffin gelled with polyethylene resin 1), petrolatum and the like are preferably blended.
独特の風味をマスキングしたり、嗜好性を上げるために、ｌ−メントール、アネトール等の香料素材、ハッカ油、スペアミント油、ペパーミント油、クローブ油、シナモン油、オレンジ油、アニス油、レモン油、アネトール、カシア油等の精油、サッカリンナトリウム、ステビオサイド、アスパルテーム等の甘味剤の配合が好ましい。 In order to mask unique flavors and enhance palatability, flavoring materials such as l-menthol and anethole, mint oil, spearmint oil, peppermint oil, clove oil, cinnamon oil, orange oil, anise oil, lemon oil, and anethole In addition, blending of essential oils such as cassia oil and sweeteners such as sodium saccharin, stevioside, aspartame is preferable.
その他、プロピレングリコール、ポリエチレングリコール等の湿潤剤やパラベン類、安息香酸ナトリウム等の防腐剤を適宜配合することが好ましい。 In addition, it is preferable to appropriately mix a wetting agent such as propylene glycol and polyethylene glycol and a preservative such as parabens and sodium benzoate.
表１の実施例１、２及び比較例１〜３の歯肉塗布剤を製造した。ここで、アスナロエキスは、アスナロの小枝の粉砕物から１０倍量のエタノールを溶媒にして抽出した後に溶媒を留去したものであり、β−ペルタチンを０．７重量％、デオキシ−β−ペルタチンを０．３重量％、β−ペルタチンＡ メチルエーテルを０．８重量％含有する。 The gingival coating agents of Examples 1 and 2 and Comparative Examples 1 to 3 in Table 1 were produced. Here, the asunalo extract is a product obtained by extracting 10 times the amount of ethanol from a pulverized asnalo twig using a solvent and then distilling off the solvent. 0.7% by weight of β-pertatin, deoxy-β-pertatin 0.3% by weight and β-pertatin A methyl ether 0.8% by weight.
歯周病に対する効果
歯周病に対する効果の試験は、試験体の投与手段をより使用実態に近い塗布法で行った。すなわち、歯周病を有する男性５名を被験者に選び、表１の歯肉塗布剤から選ばれるいずれか０．５ｇを、朝夕１２時間毎に歯ぐきに塗布した。その後、２週間あけた後、他の歯肉塗布剤を用いて同様に試験を繰り返した。歯ぐきの状態を触診及び視診により診断し、次の評価基準により指数化し、評価基準２の部位数を比較した。この試験に際しては、バイオフィルム除去のためにスケーリング等の操作は行なわなかった。
The effect on periodontal disease The test on the effect on periodontal disease was carried out by the application method of the test body closer to the actual use. That is, five males having periodontal disease were selected as subjects, and 0.5 g selected from the gingival coating agents in Table 1 was applied to the gums every 12 hours in the morning and evening. Thereafter, after 2 weeks, the test was repeated in the same manner using another gingival coating agent. The state of gums was diagnosed by palpation and visual inspection, indexed according to the following evaluation criteria, and the number of sites of evaluation criteria 2 was compared. In this test, operations such as scaling were not performed to remove the biofilm.
評価基準０：炎症なし。
評価基準１：軽度の炎症−歯肉の色調と表面の形態のわずかな変化あり。
評価基準２：中等度の炎症−中等度の歯肉表面の光沢、発赤、浮腫、及び腫脹。圧迫による出血あり。
評価基準３：重度の炎症−著しい発赤と腫脹、突発性出血の傾向、及び潰瘍あり。
Evaluation criteria 0: No inflammation.
Evaluation criteria 1: Mild inflammation-slight change in gingival color and surface morphology.
Evaluation criteria 2: Moderate inflammation-moderate gingival surface gloss, redness, edema, and swelling. There is bleeding due to pressure.
Evaluation Criteria 3: Severe inflammation-significant redness and swelling, tendency for sudden bleeding, and ulcers.
表１に使用試験の結果を示すが、本発明の実施例１及び実施例２は、短期間で顕著な歯周病改善効果を認めた。これらは、試験開始前に評価点２の炎症が認められた部位が、塗布開始７日目にはすべて評価点１以下に改善されたことから、特に中程度及び重度の炎症に対して顕著な歯周病改善効果があると考えられる。ここで、式（１）のリグナン類だけでも抗炎症効果が認められたが、ポリフェノールとの併用効果が顕著であるのは、バイオフィルムや歯肉の炎症部位への浸透性が高まったためと考えられる。この歯周病改善効果は、ポリフェノール又は式（１）のリグナン類単独における効果に比べて極めて顕著であり、これらの成分が相乗的に作用していることは明らかである。式（１）のリグナン類は、転写系のＮＦ−κＢの活性化を阻害することでＩＬ−１などの炎症性サイトカインの産生を抑える作用が推測されていることから、歯肉の炎症部位へ浸透したことで、中程度及び重度の炎症に対しても顕著な歯周病改善効果を発揮したと考えられる。 Table 1 shows the results of the use test. In Example 1 and Example 2 of the present invention, a significant periodontal disease improving effect was recognized in a short period of time. These were particularly noticeable for moderate and severe inflammation, since the sites where inflammation at a score of 2 was observed before the start of the test were all improved to a score of 1 or less on the 7th day from the start of application. It is thought to have an effect of improving periodontal disease. Here, although the anti-inflammatory effect was recognized only by the lignans of Formula (1), the combined use effect with polyphenol is considered to be because the permeability to the inflamed site of biofilm and gingiva increased. . This periodontal disease improving effect is extremely remarkable as compared with the effect of polyphenol or the lignans of formula (1) alone, and it is clear that these components act synergistically. Since the lignans of formula (1) are supposed to suppress the production of inflammatory cytokines such as IL-1 by inhibiting the activation of NF-κB in the transcription system, they penetrate into the inflamed site of gingiva. Thus, it is considered that a significant periodontal disease improving effect was exhibited even for moderate and severe inflammation.
表２の実施例３の歯ぐきマッサージクリームを製造した。ここで、アスナロエキスは実施例２と同一のものを用いた。この歯ぐきマッサージクリームは、顕著な歯周病改善効果を有していた。 The gum massage cream of Example 3 of Table 2 was manufactured. Here, the same asnalo extract was used as in Example 2. This gum massage cream had a remarkable periodontal disease improving effect.
表３の実施例４の洗口剤を製造した。ここで、アスナロ抽出液はアスナロの枝葉を１０倍量の５０％エタノール水溶液を溶媒にして抽出したものであり、茶ポリフェノールはサンフェノン１００Ｓ（太陽化学製）を用いた。 The mouthwash of Example 4 in Table 3 was produced. Here, the asunaro extract was obtained by extracting asunaro branches and leaves using a 10-fold amount of 50% ethanol aqueous solution as a solvent, and sanphenone 100S (manufactured by Taiyo Kagaku) was used as the tea polyphenol.
表４の実施例５及び比較例４、５の練歯磨剤を製造した。ここで、アスナロ抽出液と茶ポリフェノールは実施例４と同一のものを用いた。 The toothpastes of Example 5 and Comparative Examples 4 and 5 in Table 4 were produced. Here, the same asnalo extract and tea polyphenol were used as in Example 4.
表４の練歯磨剤を使用させ、すすいだ後の渋みの程度について官能評価を行なった結果、実施例５の渋みは問題のないレベルだったが、比較例４と５は渋すぎることがわかった。
As a result of performing sensory evaluation on the degree of astringency after rinsing using the toothpaste of Table 4, the astringency of Example 5 was a level with no problem, but it was found that Comparative Examples 4 and 5 were too astringent. It was.
Claims (6)
Furthermore, the composition for periodontal disease prevention or treatment in any one of Claims 1-5 containing a polyol.
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