JP2004231602A - Buccal composition containing galenical extract having antioxidation activity - Google Patents
Buccal composition containing galenical extract having antioxidation activity Download PDFInfo
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- JP2004231602A JP2004231602A JP2003024796A JP2003024796A JP2004231602A JP 2004231602 A JP2004231602 A JP 2004231602A JP 2003024796 A JP2003024796 A JP 2003024796A JP 2003024796 A JP2003024796 A JP 2003024796A JP 2004231602 A JP2004231602 A JP 2004231602A
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- oral
- periodontal disease
- preventing
- extract
- oral composition
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Abstract
Description
【０００１】
【発明の属する技術分野】
本発明は、フリーラジカルによる口腔内の酸化的ダメージを予防又は改善するための口腔用組成物に関し、より詳細には、炎症等によって過剰生産される活性酸素を含むフリーラジカルを除去することによって歯周病を予防又は改善する口腔用組成物に関する。
【０００２】
【従来の技術】
現在、多くの病気が酸化的ストレスが原因で生じると言われている。体内で過剰に発生した活性酸素は、生体の構造や機能を担う成分である、脂質、蛋白質（酵素など）や、遺伝情報を担うＤＮＡを攻撃し、生体の構造や機能を乱し、それにより病気を発症させたり、老化を早めたりする。実際、ガンや、動脈硬化、高血圧、心筋梗塞、糖尿病等の生活習慣病と呼ばれる病気は、活性酸素による酸化的ストレスが原因で起こるとも言われている。
【０００３】
フリーラジカルによる酸化的ストレスを抑制するためには、活性酸素を含むフリーラジカル消去活性を有する薬剤（フリーラジカルスカベンジャー）、すなわち、抗酸化活性を有する薬剤を外部から投与することが考えられる。このような薬剤のうち、天然物としては、例えば、アスコルビン酸（ビタミンＣ）又はその誘導体、グルタチオン、尿酸などの水溶性物質や、ビタミンＥ、コエンザイムＱ１０などが知られている。
【０００４】
近年、茶カテキンや赤ワインのポリフェノール、いちょう葉に含まれるフラボノイド配糖体やギンコライドなどの植物エキスが、生活習慣病や免疫疾患などを引き起こす原因と言われている活性酸素を含むフリーラジカルの生成抑制あるいは消去に有用であることも明らかにされてきた。
【０００５】
一方、歯周病などによる炎症、喫煙等によって、口腔内においても過剰のフリーラジカルが発生し、口腔内のみならず生体全体に対して酸化的ダメージを与えることが知られている。
【０００６】
特許文献１には、アスコルビン酸又はその誘導体に油溶性抗酸化物質を配合した口腔用組成物の発明が記載されており、その製剤形態の１つとして歯肉マッサージクリームが記載されている。アスコルビン酸又はその誘導体は、経時的な変色が生じやすく、実用上問題があった。この発明において油溶性抗酸化物質は、アスコルビン酸又はその誘導体の変色の問題を解決するために加えられており、油溶性抗酸化剤自体の口腔内のフリーラジカル消去作用を目的としたものではない。また、油溶性抗酸化剤として、コエンザイムＱ１０には言及されていない。
【０００７】
特許文献２には、細菌感染時に生体防御の目的で産生される活性酸素の過剰産生による生体侵襲を防止することにより、歯周疾患を予防・治療するのに有用な、抗酸化剤の１種又は２種以上と、モノリン酸アデノシン又はその塩からなる口腔用組成物の発明が記載されている。この口腔用組成物に用いられる抗酸化剤には、生薬抽出物やコエンザイムＱ１０などは記載されていない。また、上記特定の組み合わせのみが歯周局所の活性酸素増加を伴う歯周疾患の予防及び治療に有効であると記載されている。
【０００８】
特許文献３には、還元されたグルタチオン、セレン源、抗酸化剤としてアスコルビン酸又はその誘導体等を含む、タバコ製品及び環境汚染物質により誘発されたフリーラジカルダメージを減少させる口腔用組成物の発明が記載されている。その製剤としてジェルを含む種々の形態が記載されている。また、喫煙が、崩壊的歯周（歯肉）病及び歯の欠損にも関連性があることを記載している。
【０００９】
脂溶性抗酸化剤であるコエンザイムＱ１０は、心臓、腎臓、肝臓、膵臓等のミトコンドリア内に多く存在し、また、動植物から微生物まで幅広く見出される物質である。コエンザイムＱ１０は、細胞の活性エネルギーを産生するミトコンドリア内膜に存在する呼吸鎖の必須構成成分であり、そのビタミン様の機能からビタミンＱとも呼ばれている。さらに、コエンザイムＱ１０には、酸化されたビタミンＥラジカルを還元しビタミンＥに戻す、抗酸化作用が有ることが知られている。
【００１０】
コエンザイムＱ１０は、生体内で合成されるが、加齢とともにその産生量が減少していくことが知られている。また、若年者であっても、マラソンや過度の運動を行った場合（疲労時）には、血清中のコエンザイムＱ１０量が低下することが知られている。このような場合に、減少したコエンザイムＱ１０を体外から補給することにより、電子伝達系が効率よく作動し、エネルギー産生が活発化される。
【００１１】
コエンザイムＱ１０は、日本では、心臓疾患の治療薬、脳の保護剤などとして使用されており、特に副作用の報告もなく、安全性の高い薬物であると認識されている。海外では、医薬品だけでなく栄養補助食品として、また、化粧品として加齢に伴う皮膚のシワ取り効果でもニーズが高い。さらに、歯肉炎や歯周病の予防のための歯磨き粉（練り歯磨きなど）に添加されている商品がある。
【００１２】
【特許文献１】特開２０００−２５６１５２号公報（請求項２、段落番号０００３、００１２等）
【特許文献２】特開平１１−１２４３２２号公報（請求項１、段落番号０００１、００１０、００１１等）
【特許文献３】特開２００２−５０７９７４号公報（請求項１等）
【００１３】
【発明が解決しようとする課題】
本発明は、生薬抽出物等天然物由来の薬効成分による歯周病予防・治療方法を探求してきた本発明者のこれまでの研究の経緯から、生薬抽出物等天然物由来の抗酸化活性を活かした、安全性及び有効性の高い歯周病の予防・治療方法を提供することを目的とする。
【００１４】
【課題を解決するための手段】
上記目的を達成するため、本発明者は、種々の生薬抽出物のフリーラジカル消去活性を調査した結果、非常に高い活性を示すものを見出した（後述する試験例１参照）。また、フリーラジカル消去活性を有する生薬抽出物と、コエンザイムＱ１０とを同時に使用すると、相乗的且つ持続的なフリーラジカル消去活性が得られることを見出し、本発明を完成させた。
【００１５】
すなわち、本発明は、
（１）抗酸化活性を有する生薬抽出物を含む口腔用組成物；
【００１６】
（２）抗酸化活性を有する生薬が、ボタンピ、ビンロウジ、ノギクカ、シコン、オウゴン、ヤクモソウ、オウバク、オウレン、ニクズク、ウコン及びローズマリーからなる群から選択される１種以上であることを特徴とする、上記（１）に記載の口腔用組成物；
【００１７】
（３）抗酸化活性を有する生薬が、ボタンピ、ビンロウジ及びノギクカからなる群から選択される１種以上であることを特徴とする、上記（２）に記載の口腔用組成物；
【００１８】
（４）さらにコエンザイムＱ１０を含むことを特徴とする、上記（１）〜（３）のいずれかに記載の口腔用組成物；
【００１９】
（５）塗布剤又はチュアブル錠の形態であることを特徴とする、上記（１）〜（４）のいずれかに記載の口腔用組成物；
【００２０】
（６）塗布剤の形態である口腔用組成物を、歯肉マッサージに用いることを特徴とする、上記（５）に記載の口腔用組成物；
【００２１】
（７）塗布剤の形態がジェルであることを特徴とする、上記（６）に記載の口腔用組成物；
【００２２】
（８）フリーラジカルによる口腔内のダメージを予防又は改善することを目的とする、上記（１）〜（７）のいずれかに記載の口腔用組成物；
【００２３】
（９）フリーラジカルによる口腔内のダメージが、歯周病又は喫煙に起因するものであることを特徴とする、上記（８）に記載の口腔用組成物；
【００２４】
（１０）歯周病の予防又は改善を目的とすることを特徴とする、上記（１）〜（９）のいずれかに記載の口腔用組成物；
【００２５】
（１１）上記（６）〜（１０）のいずれかに記載の口腔内塗布剤を用いて、歯肉マッサージを行うことを特徴とする、フリーラジカルによる口腔内のダメージを予防又は改善する方法；
【００２６】
（１２）フリーラジカルによる口腔内のダメージが、歯周病又は喫煙に起因するものであることを特徴とする、上記（１１）に記載のフリーラジカルによる口腔内のダメージを予防又は改善する方法；
【００２７】
（１３）歯周病の予防又は改善を目的とすることを特徴とする、上記（１１）又は（１２）に記載のフリーラジカルによる口腔内のダメージを予防又は改善する方法；
【００２８】
（１４）マスティック（乳香）のオイル抽出エキス及び消炎剤を有効成分とする歯周病予防・治療用組成物を、市販の歯磨き剤に添加したものでブラッシングを行った後、及び／又はカンゾウ（甘草）、ビンロウジ（檳榔子）、ニクズク（肉蒄）及びヤクモソウ（益母草）からなる群から選択される１種以上の生薬抽出物を含む洗口含嗽剤でうがいを行った後に、上記（６）〜（１０）のいずれかに記載の塗布剤形態の口腔用組成物を用いて、歯肉マッサージを行うことを特徴とする歯周病予防・治療方法；及び
【００２９】
（１５）市販の歯磨き剤に添加するためのマスティック（乳香）のオイル抽出エキス及び消炎剤を有効成分とする歯周病予防・治療用組成物、及び／又はカンゾウ（甘草）、ビンロウジ（檳榔子）、ニクズク（肉蒄）及びヤクモソウ（益母草）からなる群から選択される１種以上の抽出物を含む洗口含嗽剤と、歯肉マッサージを行うための上記（６）〜（１０）に記載の塗布剤形態の口腔用組成物とを含む歯周病予防・治療用キット
を提供する。
【００３０】
【発明の実施の形態】
以下、本発明を詳細に説明する。
本発明の口腔用組成物は、抗酸化活性を有する生薬抽出物を主成分とする。抗酸化活性を有する生薬としては、例えば、ボタンピ、ビンロウジ、ノギクカ、シコン、オウゴン、ヤクモソウ、オウバク、オウレン、ニクズク、ウコン、ローズマリーなどが挙げられる。
【００３１】
後述する試験例１の結果から明らかなように、これらの生薬抽出物は、フリーラジカル消去活性を有している。ボタンピ、ビンロウジ及びノギクカは、特に高いフリーラジカル消去活性を有しており、本発明の口腔内塗布剤の主成分として好ましい。
【００３２】
フリーラジカル消去作用を有する上記生薬抽出物を口腔内に局所塗布することにより、歯周病に関連する炎症、喫煙、細菌感染等によって生じる過剰のフリーラジカルを消去し、口腔内の組織に対する酸化的ダメージを直接的に防止することができる。
【００３３】
また、本発明の口腔用組成物は、口腔内に適用するものであるから、口腔粘膜から吸収されるだけでなく、唾液と共に飲み込まれて胃粘膜等の消化管壁からも吸収される。従って、消化管から吸収された薬効成分の全身的なフリーラジカル消去活性も期待できる。
【００３４】
また、上記の生薬抽出物の中には、歯周病の原因菌に対する抗菌活性、口腔内の免疫力を高める作用、消炎作用など、歯周病の予防・治療に好ましい作用効果を有するものも含まれており、抗酸化活性との相乗的な歯周病予防・治療効果も期待できる（特開平６−１５７２５９号公報）。
【００３５】
本発明の口腔用組成物における抗酸化活性を有する生薬抽出物の配合量は、その原生薬の有するフリーラジカル消去活性に応じて適宜設定すべきであるが、通常５〜１２質量％、好ましくは１０〜１２質量％の範囲である。
【００３６】
本発明の口腔用組成物には、コエンザイムＱ１０をさらに含むことが好ましい。コエンザイムＱ１０は、上述のように生体内のエネルギー産生賦活作用と抗酸化作用とを有する。
【００３７】
上記の抗酸化活性を有する水溶性の生薬抽出物と脂溶性のコエンザイムＱ１０とを組み合わせて用いることにより、それぞれを単独で用いた場合に比べ、相乗的且つ持続的な抗酸化活性が得られる。
【００３８】
さらに、コエンザイムＱ１０の有するエネルギー産生賦活活性により、歯周病等で傷ついた組織の修復が局所的に促進される効果も期待できる。
【００３９】
本発明の口腔用組成物におけるコエンザイムＱ１０の配合量は、通常０．００１〜０．１質量％、好ましくは０．００５〜０．０５質量％の範囲、特に好ましくは０．０１質量％である。なお、コエンザイムの一日の摂取量は、３０〜６０ｍｇであるのが好ましい。
【００４０】
本発明の口腔用組成物は、口腔内に適用可能な種々の製剤形態とすることができるが、ジェル又は軟膏等の塗布剤又はチュアブル錠であることが好ましく、塗布剤であることがより好ましい。
【００４１】
塗布剤形態の本発明の口腔用組成物を、歯周病等によって炎症を起こしている歯肉に塗布し、さらに塗布した部分をマッサージすることにより優れたフリーラジカル消去効果が得られる。
【００４２】
特に、本発明の口腔用組成物を歯周病（特に歯肉炎を起こしている場合）の予防又は改善の目的で用いる場合には、歯肉マッサージによって、フリーラジカル消去効果のみでなく、歯肉マッサージによる歯肉の血行促進が歯周病予防・治療にとって特に好ましい。
【００４３】
塗布剤のうち、特にジェルの形態であることが特に好ましい。ジェルは、通常のペーストよりも粘度がゆるく、口腔内における使用部位（特に歯と歯茎の隙間、歯間等）に容易に侵入させることができ、塗布したい部位に確実に塗布することができる。また、ジェルは口腔内の適用部位に使用する際、均一且つスムーズに塗布できる利点を有する。
【００４４】
本発明の口腔用組成物には、生薬抽出物及びコエンザイムＱ１０のの他、種々の抗酸化活性を有する成分を含有することができる。本発明の口腔用組成物に添加できる抗酸化活性を有する成分としては、例えば、フェルラ酸、アスタキサンチン、ビタミンＥ、ビタミンＣ、ビタミンＡ、ＢＨＴ、ＢＨＡ、ＮＤＧＡ、没食子酸プロピル、ポリフェノール類（タンニン類）、エリソルビン酸等が挙げられる。
【００４５】
上記の任意に添加できる抗酸化活性を有する成分についても、特性の異なる多種類の成分を、生薬抽出物及びコエンザイムＱ１０と組み合わせることで、フリーラジカル消去活性の相乗効果及びその持続性の向上が期待できる。
【００４６】
本発明の口腔用組成物には、生薬抽出物及びコエンザイムＱ１０の効果を損なわない限り、上記抗酸化活性成分の他にさらに別の薬効成分を添加することができる。このような薬効成分としては、例えば、アズレンスルホン酸ナトリウム、ε−アミノカプロン酸、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、アラントインジヒドロキシアルミニウム、エピジヒドロコレステリン、ジヒドロコレステロール、塩化ナトリウム、グリチルリチン酸、グリチルリチン酸二アンモニウム、グリチルリチン酸二ナトリウム、グリチルリチン酸三ナトリウム、グリチルリチン酸ジカリウム、グリチルリチン酸モノアンモニウム、β−グリチルレチン酸、イソプロピルメチルフェノール、塩化セチルピリジニウム、塩化デカリニウム、塩化ベンザルコニウム、塩化ベンザルコニウム液、塩酸アルキルジアミノエチルグリシン液、塩酸クロルヘキシジン、トリクロサン、アスコルビン酸、アスコルビン酸ナトリウム、塩酸ピリドキシン、酢酸ｄｌ−α−トコフェロール、ニコチン酸ｄｌ−α−トコフェロール、ゼオライト、ピロリン酸二水素ナトリウム、ピロリン酸ナトリウム、無水ピロリン酸ナトリウム、リン酸一水素ナトリウム、リン酸三ナトリウム、ポリリン酸ナトリウム、フッ化ナトリウム、モノフルオロリン酸ナトリウム、ポリエチレングリコール２００、ポリエチレングリコール３００、ポリエチレングリコール４００、ポリエチレングリコール６００、ポリエチレングリコール１０００、ポリエチレングリコール１５００、ポリエチレングリコール１５４０、ポリエチレングリコール４０００、ポリエチレングリコール６０００、ポリエチレングリコール２００００、ポリビニルピロリドン、ポリビニルピロリドンＫ２５、ポリビニルピロリドンＫ３０、ポリビニルピロリドンＫ９０、塩化リゾチーム、銅クロロフィリンナトリウム、ヒノキチオール、ポリオキシエチレンラウリルエーテル、ラウロイルサルコシンナトリウム等が挙げられる。
【００４７】
次に、本発明の口腔用組成物の製造方法を説明する。
本発明の口腔用組成物の主成分である抗酸化活性を有する生薬抽出物の製造方法は以下の通りである。
【００４８】
ボタンピ、ビンロウジ、ノギクカ、シコン、オウゴン、ヤクモソウ、オウバク、オウレン、ニクズク、ウコン及びローズマリーの抽出物を得る方法には特に制限はなく、生薬の有効成分を抽出するために用いられる通常の方法を用いることができる。例えば、温湯を用いて抽出（一般的なエキス状）してもよいし、パーコレーション法によって抽出（流エキス）してもよい。また、生薬抽出物の性状も特に制限されず、液状、軟稠エキス状、粉末状、顆粒状等のものを用いることができる。また、エタノールによって抽出したエキスを用いることもできる。
【００４９】
水による抽出方法としては、例えば、各生薬を、それぞれ個別に煎じた後、固形物を濾別し、得られた濾液を濃縮して軟稠なエキスとする。これらの軟稠エキスのいずれか１種を、又は２種以上を適当な割合で混練した後、例えば、乾燥して細粒化する。あるいは、上記生薬のいずれか２種以上を適当な割合で混合したものを煎じた後、固形物を濾別し、濾液を濃縮して軟調なエキスとしてもよい。
【００５０】
次に、本発明の口腔用組成物が抗酸化活性を有する生薬の抽出物とコエンザイムＱ１０とを含有し、且つジェルの形態を有する場合を例として、その製造方法を説明する。なお、下記の製造方法は、製剤製造中に抗酸化剤が変質することを避けるため、製造時に加熱を行わないことを特徴とする。
【００５１】
まず、コエンザイムＱ１０等の油溶性抗酸化剤を、これを溶解する油（溶剤）に溶解して塗布油液を製造する。得られた抗酸化剤塗布油液に、界面活性剤を加えて均一に混合し、油相溶液を得る。油相溶液にゲル化剤（増粘剤）を加えて撹拌し、分散液を得る。
【００５２】
次に、抗酸化活性を有する生薬の抽出物に、水、エタノール等の溶媒を混合し、均一に溶解して水相溶液を得る。上記分散液に水相溶液を加えて強く撹拌することにより、ジェル形態の製剤を得ることができる。
【００５３】
また、製造時に減圧を行い、製剤に含まれる酸素などを脱泡して安定化していもよい。
【００５４】
本発明の口腔用組成物を製造する際には、上記薬効成分の他、湿潤剤、溶剤、増粘剤、界面活性剤、香味剤、その他の通常口腔用に用いられている添加剤（例えば、清涼剤、甘味剤、着色剤、ｐＨ調整剤、防腐剤）を用いることができる。
【００５５】
湿潤剤としては、濃グリセリン、ソルビット液などが挙げられる。
【００５６】
溶剤としては、エタノール、水、オリーブ油、ヤシ油、大豆油、綿実油、トウモロコシ油、ゴマ油、ナタネ油、落花生油、ツバキ油等の食用油などが挙げられる。
【００５７】
増粘剤としては、キサンタンガム、カラギーナン、カルボキシメチルセルロースナトリウム、ヒドロキシエチルセルロース、ミツロウなどが挙げられる。
【００５８】
界面活性剤としては、ショ糖脂肪酸エステル、ラウリル硫酸ナトリウム、ラウロイルサルコシンナトリウムなどが挙げられる。
【００５９】
香味剤としては、メントール、ペパーミント油、スペアミント油、オレンジ油、レモン油、ユーカリ油、ハッカ油、アカシア油、ウイキョウ油、クエントウ油、カラムス油、ショウノウ油、ニッケイ油、ケイ皮油、ケイ葉油、バラ油、ビャクダン油、チョウジ油、ハーブ油、バナナ油、リンゴ油、サリチル酸メチル、カルボン、アネトール、リモネン等のテルペン類などの香料及び調合香料が挙げられる。
【００６０】
次に、本発明の口腔用組成物をより効果的に歯周病の予防・治療のために用いる方法について説明する。
【００６１】
本発明者は、特願２００２−２４４２８６号。明細書において、マスティック（乳香）のオイル抽出エキス及び消炎剤を有効成分とする歯周病予防・治療用組成物を、市販の歯磨き剤に添加したものでブラッシングを行った後、カンゾウ（甘草）、ビンロウジ（檳榔子）、ニクズク（肉蒄）及びヤクモソウ（益母草）からなる群から選択される１種以上の生薬抽出物を含む洗口含嗽剤でうがいを行う歯周病の予防・治療方法（以下、先願発明の方法という）を提案した。
【００６２】
本発明の方法においては、上記ブラッシング及び／又はうがいを行った後に、上記塗布剤形態の本発明の口腔用組成物を用いて、歯肉マッサージを行うことを特徴とする。先願発明の方法によって、歯周病原因菌を抑制し、口腔内の免疫力を高め、さらに本発明の口腔用組成物を用いた歯肉マッサージによって、フリーラジカルを消去すると同時に歯肉の血行を促す。これによって、先願発明の方法よりもさらに優れた歯周病の予防・治療効果が得られる。
【００６３】
上記本発明の方法を実行するためには、市販の歯磨き剤に添加するためのマスティック（乳香）のオイル抽出エキス及び消炎剤を有効成分とする歯周病予防・治療用組成物、及び／又はカンゾウ（甘草）、ビンロウジ（檳榔子）、ニクズク（肉蒄）及びヤクモソウ（益母草）からなる群から選択される１種以上の抽出物を含む洗口含嗽剤と、歯肉マッサージを行うための上記塗布剤形態の本発明の口腔用組成物とを含む歯周病予防・治療用キットを用いることが便利であり、好ましい。
【００６４】
【実施例】
以下、試験例、製造例を記載して本発明をより具体的に説明するが、本発明はこれら試験例、製造例によってなんら限定されるものではない。
【００６５】
試験例１：生薬抽出物のフリーラジカル消去活性
ボタンピ、ビンロウジ、ノギクカ、シコン、オウゴン、ヤクモソウ、オウバク、オウレン、ニクズク、ウコン及びローズマリーの水による抽出エキス（通常のエキス及び流エキスを含む）及びエタノールによる抽出エキスを実験に供した。
【００６６】
これらの生薬抽出エキスのスーパーオキシド消去活性を、スピントラッピング−電子スピン共鳴法（ＥＳＲ法）を用いて測定した。スーパーオキシド（ＳＯＤ）の発生系は、ヒポキサンチン（ＨＰＸ）とキサンチン酸化酵素（ＸＯＤ）を用い、試薬濃度及び測定の調整は以下のとおりであった。
【００６７】
２ｍＭ ＨＰＸ：５０μＬ
５．５ｍＭ ＤＴＰＡ：３０μＬ
ＳＯＤ又は生薬抽出エキス（サンプル）：５０μＬ
ＤＭＰＯ（１：１）：２０μＬ
０．４Ｕ／ｍＬ ＸＯＤ：５０μＬ
【００６８】
各試料とも、上記の試薬を順に添加し、ＸＯＤ添加６０秒後に電子スピン共鳴（ＥＳＲ）装置を用いて、そのシグナルを観測した。試薬は、０．１Ｍリン酸バッファー（ＰＢ）（ｐＨ７．４）を用いて希釈した。また、ＳＯＤ標準試薬（ＳＩＧＭＡ社製、ウシ赤血球由来）は、ＰＢで希釈し、２５、１２．５、６．２５、３．１３、１．５６及び０（ブランク；ＰＢ）Ｕ（単位）／ｍＬとした。
【００６９】
ＥＳＲの測定条件は、以下のとおりであった。
出力（Ｐｏｗｅｒ）：８ｍＷ
領域中心（Ｆｉｅｌｄ Ｃｅｎｔｅｒ）：３３５．７００ ｍＴ ＋／− ５ ｍＴ
掃引時間（Ｓｗｅｅｐ Ｔｉｍｅ）：２．０分
モッド幅（Ｍｏｄ Ｗｉｄｔｈ）：０．０７ｍＴ
振幅（Ａｍｐｌｉｔｕｄｅ）：３００
時定数（Ｔｉｍｅ Ｃｏｎｓｔ）：０．１秒
【００７０】
スーパーオキシド消去活性（ＳＯＳＡ）を測定するための検量線は、マンガン・マーカー（Ｍｎ ｍａｋｅｒ）シグナルに対するスーパーオキシド（ＤＭＰＯ−ＯＯＨ）スペクトルの第１ピークの強度を相対シグナル強度（Ｉ）とし、濃度（活性）既知のＳＯＤを用い、各濃度のＳＯＤに対する
（Ｉ０／Ｉｘ）−１
の値をプロットすることによって作成した。ここで、Ｉ０は、ブランク（ＰＢ）測定時の相対シグナル強度であり、Ｉｘは、ＳＯＤ添加時の相対シグナル強度である。
【００７１】
本実験におけるＩＣ５０に相当するＳＯＤ活性は０．８４Ｕ（単位）／ｍＬであった。スーパーオキシド消去活性（１サンプルについて２回測定を実施）は、上記ＨＰＸ−ＸＯＤ系にサンプル５０μＬを添加して求めた。ＥＳＲ測定条件は上記と同様とした。
【００７２】
各サンプルの相対シグナル強度及び（Ｉ０／Ｉｘ）−１値を算出し、スーパーオキシド（Ｏ２ −・）消去能を、ＳＯＤ活性に換算して評価した。
【００７３】
その結果、特にボタンピ、ビンロウジ、ノギクカは、１６００〜５３００（ＳＯＤ Ｕ（単位）／ｍＬ）の範囲の高いスーパーオキシド消去活性を示し、その他の生薬抽出エキスもスーパーオキシド消去活性を示すことがわかった。特に、ボタンピのスーパーオキシド消去活性は、５３００ ＳＯＤ Ｕ／ｍＬと非常に高いことが明らかになった。
【００７４】
最も高いスーパーオキシド消去活性を示したボタンピの活性を１００としたときの、各生薬抽出エキスの相対的なスーパーオキシド消去活性（ＳＯＤ活性に換算）を、図１にグラフとして示す。
【００７５】
製造例：口腔内塗布用ジェルの製造方法
（１）ボタンピ抽出物の製造
ボタンピの原料生薬２０ｋｇに適量の水を加え、水抽出を行い、濾過してボタンピ抽出液を得た。この抽出液を減圧下に濃縮し、最終抽出物中のエタノール濃度が２％となる量のエタノールを添加・混合した後、滅菌を行い、ボタンピ抽出物２０Ｌを得た。
【００７６】
（２）上記（１）で製造したボタンピ抽出物を用い、下記表１に示す処方に従って口腔塗布用ジェルを製造した。製造方法は次のとおりである。
コエンザイムＱ１０、アスタキサンチン及びビタミンＣをヤシ油に溶解し、ミツロウを加えた油液を得た。この油液に、ショ糖脂肪酸エステルを加えて均一に混合し、油相溶液を得た。この油相溶液にキサンタンガム、ミツロウ、濃グリセリンを加えて撹拌し、分散液を得た。次に、ボタンピ抽出物、ビタミンＣ及びフェルラ酸に、水及びエタノールを混合して均一に溶解し、水相溶液を得た。上記分散液に水相溶液を加えて強く撹拌し、口腔塗布用ジェルを得た。
【００７７】
【表１】
【発明の効果】
本発明の口腔用組成物によれば、生薬抽出物等天然物由来の抗酸化活性を活かして、歯周病を含む口腔内の酸化的ダメージを防止又は改善することができる。
【００７９】
特に、生薬抽出物及びコエンザイムＱ１０を含む本発明の口腔用組成物は、相乗的且つ持続的なスーパーオキシド消去活性を有し、歯周病を含む口腔内の酸化的ダメージをより効果的に防止又は改善することができる。
【００８０】
本発明の口腔用組成物による歯肉マッサージは、歯周病による酸化的ダメージを防止又は改善すると共に、歯肉の血行を促すことで歯周病の予防・治療に効果的である。
【００８１】
マスティックのオイル抽出物を含む歯周病予防・治療用組成物を市販の歯磨き剤に添加してブラッシングした後、及び／又は生薬抽出物からなる洗口含嗽剤でうがいを行った後に、本発明の口腔用組成物を用いて歯肉マッサージを行うことにより、効果的な歯周病の予防・治療が可能となる。
【図面の簡単な説明】
【図１】ボタンピのスーパーオキシド消去活性を１００としたときの、各生薬抽出エキスの相対的なスーパーオキシド消去活性を示すグラフである。[0001]
TECHNICAL FIELD OF THE INVENTION
The present invention relates to an oral composition for preventing or ameliorating oxidative damage in the oral cavity due to free radicals, and more particularly, to a dental composition by removing free radicals containing active oxygen overproduced by inflammation or the like. The present invention relates to an oral composition for preventing or ameliorating periodontal disease.
[0002]
[Prior art]
At present, it is said that many diseases are caused by oxidative stress. Reactive oxygen generated excessively in the body attacks the lipids, proteins (enzymes, etc.), which are the components responsible for the structure and function of the living body, and the DNA that carries the genetic information, and disrupts the structure and function of the living body. It causes disease and accelerates aging. In fact, it is also said that diseases called lifestyle-related diseases such as cancer, arteriosclerosis, hypertension, myocardial infarction, and diabetes are caused by oxidative stress due to active oxygen.
[0003]
In order to suppress oxidative stress due to free radicals, it is conceivable to externally administer a drug having free radical scavenging activity containing free oxygen (free radical scavenger), that is, a drug having antioxidant activity. Among such drugs, as a natural product, for example, ascorbic acid (vitamin C) or a derivative thereof, water-soluble substances such as glutathione and uric acid, vitamin E, coenzyme Q10, and the like are known.
[0004]
In recent years, tea catechins, polyphenols of red wine, plant extracts such as flavonoid glycosides and ginkgolides contained in ginkgo biloba, suppress the generation of free radicals including active oxygen, which are said to cause lifestyle-related diseases and immune diseases. Alternatively, it has also been shown to be useful for erasure.
[0005]
On the other hand, it is known that excessive free radicals are generated in the oral cavity due to inflammation due to periodontal disease, smoking, and the like, and cause oxidative damage not only to the oral cavity but also to the entire living body.
[0006]
Patent Document 1 describes an invention of an oral composition in which an oil-soluble antioxidant is mixed with ascorbic acid or a derivative thereof, and describes a gingival massage cream as one of the formulations. Ascorbic acid or a derivative thereof is liable to undergo discoloration over time, and has a practical problem. In the present invention, the oil-soluble antioxidant is added to solve the problem of discoloration of ascorbic acid or a derivative thereof, and is not intended to eliminate the free radicals in the oral cavity of the oil-soluble antioxidant itself. . Further, Coenzyme Q10 is not mentioned as an oil-soluble antioxidant.
[0007]
Patent Literature 2 discloses a type of antioxidant useful for preventing and treating periodontal disease by preventing biological invasion due to excessive production of active oxygen produced for the purpose of host defense at the time of bacterial infection. Or, the invention of an oral composition comprising two or more kinds and adenosine monophosphate or a salt thereof is described. The antioxidant used in the oral composition does not describe a crude drug extract or coenzyme Q10. Further, it is described that only the above-mentioned specific combination is effective for the prevention and treatment of periodontal disease accompanied by an increase in active periodontal active oxygen.
[0008]
Patent Document 3 discloses an invention of an oral composition for reducing free radical damage induced by tobacco products and environmental pollutants, including reduced glutathione, a selenium source, ascorbic acid or a derivative thereof as an antioxidant, and the like. Has been described. Various forms including gels are described as the preparation. It also states that smoking is also associated with destructive periodontal (gingival) disease and tooth loss.
[0009]
Coenzyme Q10, which is a fat-soluble antioxidant, is a substance that is abundantly found in mitochondria such as heart, kidney, liver, and pancreas, and is widely found from animals and plants to microorganisms. Coenzyme Q10 is an essential component of the respiratory chain present in the inner mitochondrial membrane that produces active energy of cells, and is also called vitamin Q because of its vitamin-like function. Furthermore, it is known that coenzyme Q10 has an antioxidant effect of reducing oxidized vitamin E radicals and returning them to vitamin E.
[0010]
Coenzyme Q10 is synthesized in a living body, but it is known that its production decreases with aging. In addition, it is known that even in a young person, when a marathon or excessive exercise is performed (at the time of fatigue), the amount of coenzyme Q10 in serum decreases. In such a case, by supplying the reduced coenzyme Q10 from outside the body, the electron transfer system operates efficiently and energy production is activated.
[0011]
Coenzyme Q10 is used in Japan as a therapeutic drug for heart disease, a brain protective agent, and the like, and is recognized as a highly safe drug with no reported side effects. Overseas, there is a high need for not only pharmaceuticals but also nutritional supplements and cosmetics as well as the effect of removing skin wrinkles with aging. Furthermore, there are products that are added to toothpastes (such as toothpastes) for preventing gingivitis and periodontal disease.
[0012]
[Patent Document 1] Japanese Patent Application Laid-Open No. 2000-256152 (Claim 2, paragraph numbers 0003, 0012, etc.)
[Patent Document 2] JP-A-11-124322 (Claim 1, paragraph numbers 0001, 0010, 0011, etc.)
[Patent Document 3] Japanese Patent Application Laid-Open No. 2002-507974 (Claim 1 etc.)
[0013]
[Problems to be solved by the invention]
The present invention is based on the history of research conducted by the present inventor who has been searching for a method for preventing and treating periodontal disease using a medicinal component derived from a natural product such as a crude drug extract. It is an object of the present invention to provide a safe and effective method for preventing and treating periodontal disease that is utilized.
[0014]
[Means for Solving the Problems]
In order to achieve the above object, the present inventor investigated the free radical scavenging activity of various crude drug extracts, and as a result, found one exhibiting extremely high activity (see Test Example 1 described later). In addition, they have found that when a herbal extract having free radical scavenging activity and coenzyme Q10 are used at the same time, a synergistic and sustained free radical scavenging activity can be obtained, thereby completing the present invention.
[0015]
That is, the present invention
(1) an oral composition containing a crude drug extract having antioxidant activity;
[0016]
(2) The crude drug having antioxidant activity is characterized by being at least one selected from the group consisting of buttonpicks, areca, sagebrush, sicon, giant gourd, yakumoso, oubaku, suzuki, nikuzuku, turmeric and rosemary. The oral composition according to the above (1);
[0017]
(3) The composition for oral cavity according to (2), wherein the crude drug having antioxidant activity is at least one selected from the group consisting of buttonpicks, areca, and sagebrush;
[0018]
(4) The oral composition according to any one of (1) to (3), further comprising Coenzyme Q10;
[0019]
(5) The oral composition according to any one of (1) to (4) above, which is in the form of a coating agent or a chewable tablet;
[0020]
(6) The oral composition according to the above (5), wherein the oral composition in the form of a coating agent is used for gingival massage;
[0021]
(7) The composition for oral cavity according to the above (6), wherein the form of the coating agent is a gel;
[0022]
(8) The oral composition according to any one of (1) to (7) above, which is intended to prevent or improve damage in the oral cavity due to free radicals;
[0023]
(9) The oral composition according to (8), wherein the damage in the oral cavity due to free radicals is caused by periodontal disease or smoking;
[0024]
(10) The oral composition according to any of (1) to (9) above, which is intended for preventing or improving periodontal disease;
[0025]
(11) A method for preventing or improving damage in the oral cavity due to free radicals, comprising performing gingival massage using the oral application agent according to any of (6) to (10) above;
[0026]
(12) The method for preventing or improving the damage in the oral cavity according to the above (11), wherein the damage in the oral cavity due to free radicals is caused by periodontal disease or smoking;
[0027]
(13) A method for preventing or improving damage in the oral cavity due to free radicals according to (11) or (12), wherein the method is aimed at preventing or improving periodontal disease;
[0028]
(14) After brushing with a commercially available dentifrice, a composition for preventing or treating periodontal disease containing an oil extract of mastic (frankincense) and an anti-inflammatory agent as active ingredients, and / or liquorice (Licorice), betel nut (beetle root), nutmeg (meat meg) and yakumoso (mass mother grass), after gargle with a mouthwash gargle containing at least one crude drug extract selected from the group consisting of: ) A method for preventing / treating periodontal disease, characterized by performing gingival massage using the composition for oral cavity in the form of an application according to any one of (1) to (10);
[0029]
(15) A composition for preventing or treating periodontal disease containing an oil extract of mastic (frankincense) and an anti-inflammatory agent as active ingredients for addition to commercially available dentifrices, and / or licorice (licorice), areca nut Mouthwash containing at least one extract selected from the group consisting of sapling), nutmeg (meat meg) and yakumoso (mother grass), and the above (6) to (10) for performing gingival massage. For prevention and treatment of periodontal disease, comprising an oral composition in the form of a coating preparation
I will provide a.
[0030]
BEST MODE FOR CARRYING OUT THE INVENTION
Hereinafter, the present invention will be described in detail.
The oral composition of the present invention contains a crude drug extract having antioxidant activity as a main component. Crude drugs having antioxidant activity include, for example, carp, betel nut, sage beetle, sicon, ogon, yakumoso, oubak, uren, nutmeg, turmeric, rosemary and the like.
[0031]
As is clear from the results of Test Example 1 described below, these crude drug extracts have free radical scavenging activity. Button bolls, areca and cabbage have particularly high free radical scavenging activities, and are preferred as the main components of the orally applied agent of the present invention.
[0032]
By topically applying the crude drug extract having a free radical scavenging action to the oral cavity, it eliminates excess free radicals caused by periodontal disease-related inflammation, smoking, bacterial infection, etc., and oxidizes the oral tissues. Damage can be prevented directly.
[0033]
Further, since the oral composition of the present invention is applied to the oral cavity, it is absorbed not only from the oral mucosa but also swallowed with saliva and absorbed from the digestive tract wall such as the gastric mucosa. Therefore, a systemic free radical scavenging activity of the medicinal component absorbed from the digestive tract can be expected.
[0034]
In addition, some of the crude drug extracts described above have antibacterial activity against the causative bacteria of periodontal disease, an effect of enhancing immunity in the oral cavity, an anti-inflammatory effect, and the like, which have a favorable effect on the prevention and treatment of periodontal disease. It is also expected to have a synergistic effect with periodontal disease prevention and treatment with antioxidant activity (JP-A-6-157259).
[0035]
The amount of the crude drug extract having antioxidant activity in the oral composition of the present invention should be appropriately set according to the free radical scavenging activity of the crude drug, but is usually 5 to 12% by mass, preferably It is in the range of 10 to 12% by mass.
[0036]
The oral composition of the present invention preferably further contains coenzyme Q10. Coenzyme Q10 has an in vivo energy production activating action and an antioxidant action as described above.
[0037]
By using the water-soluble herbal extract having antioxidant activity and the fat-soluble coenzyme Q10 in combination, a synergistic and sustained antioxidant activity can be obtained as compared with the case of using each alone.
[0038]
In addition, the effect of coenzyme Q10 on activation of energy production has the effect of locally promoting the repair of tissue damaged by periodontal disease or the like.
[0039]
The compounding amount of coenzyme Q10 in the oral composition of the present invention is usually 0.001 to 0.1% by mass, preferably 0.005 to 0.05% by mass, and particularly preferably 0.01% by mass. . The daily intake of coenzyme is preferably 30 to 60 mg.
[0040]
The composition for the oral cavity of the present invention can be made into various preparation forms applicable to the oral cavity, but is preferably a coating agent such as a gel or an ointment or a chewable tablet, and more preferably a coating agent. .
[0041]
An excellent free radical scavenging effect can be obtained by applying the oral composition of the present invention in the form of a coating composition to gingiva that is inflamed due to periodontal disease or the like, and then massaging the applied part.
[0042]
In particular, when the oral composition of the present invention is used for the purpose of preventing or improving periodontal disease (particularly when gingivitis is caused), not only free radical scavenging effect but also gingival massage Gum circulation promotion is particularly preferred for periodontal disease prevention and treatment.
[0043]
Among the coating agents, it is particularly preferable that the coating agent is in the form of a gel. The gel has a viscosity lower than that of a normal paste, and can easily penetrate into the site of use in the oral cavity (especially, a gap between teeth and gums, between teeth, etc.), and can be applied reliably to the site to be applied. Further, the gel has an advantage that it can be applied uniformly and smoothly when used on an application site in the oral cavity.
[0044]
The oral composition of the present invention can contain various components having an antioxidant activity in addition to the crude drug extract and coenzyme Q10. Components having antioxidant activity that can be added to the oral composition of the present invention include, for example, ferulic acid, astaxanthin, vitamin E, vitamin C, vitamin A, BHT, BHA, NDGA, propyl gallate, polyphenols (tannins) ), Erythorbic acid and the like.
[0045]
Regarding the components having antioxidant activity that can be arbitrarily added, a synergistic effect of free radical scavenging activity and improvement of the sustainability thereof are expected by combining various components having different properties with the crude drug extract and coenzyme Q10. it can.
[0046]
To the oral composition of the present invention, other medicinal ingredients can be added in addition to the above-mentioned antioxidant active ingredients, as long as the effects of the herbal extract and coenzyme Q10 are not impaired. Examples of such medicinal ingredients include sodium azulene sulfonate, ε-aminocaproic acid, allantoin, allantoinchlorohydroxyaluminum, allantoindihydroxyaluminum, epidihydrocholesterin, dihydrocholesterol, sodium chloride, glycyrrhizic acid, diammonium glycyrrhizinate, Disodium glycyrrhizinate, trisodium glycyrrhizinate, dipotassium glycyrrhizinate, monoammonium glycyrrhizinate, β-glycyrrhetinic acid, isopropylmethylphenol, cetylpyridinium chloride, decalinium chloride, benzalkonium chloride, benzalkonium chloride liquid, alkyldiaminoethyl hydrochloride Glycine solution, chlorhexidine hydrochloride, triclosan, ascorbic acid, sodium ascorbate Lium, pyridoxine hydrochloride, dl-α-tocopherol acetate, dl-α-tocopherol nicotinate, zeolite, sodium dihydrogen pyrophosphate, sodium pyrophosphate, anhydrous sodium pyrophosphate, sodium monohydrogen phosphate, trisodium phosphate, polyphosphoric acid Sodium, sodium fluoride, sodium monofluorophosphate, polyethylene glycol 200, polyethylene glycol 300, polyethylene glycol 400, polyethylene glycol 600, polyethylene glycol 1000, polyethylene glycol 1500, polyethylene glycol 1540, polyethylene glycol 4000, polyethylene glycol 6000, polyethylene glycol 20000, polyvinylpyrrolidone, polyvinylpyrrolidone K25, polyvinyl Pyrrolidone K30, polyvinylpyrrolidone K90, lysozyme chloride, copper chlorophyllin sodium, hinokitiol, polyoxyethylene lauryl ether, sodium lauroyl sarcosine and the like.
[0047]
Next, a method for producing the oral composition of the present invention will be described.
The method for producing a crude drug extract having antioxidant activity, which is a main component of the oral composition of the present invention, is as follows.
[0048]
There is no particular limitation on the method of obtaining the extracts of botanic piste, areca, sycamore, siconi, ogon, yakumoso, oubaku, spinach, nutmeg, turmeric and rosemary, and the usual method used for extracting the active ingredient of crude drug is used. Can be used. For example, it may be extracted using hot water (general extract form), or may be extracted by a percolation method (flow extract). The properties of the crude drug extract are also not particularly limited, and liquid, soft extract, powder, granule, and the like can be used. An extract extracted with ethanol can also be used.
[0049]
As a method of extraction with water, for example, each crude drug is individually decocted, then the solid matter is filtered off, and the obtained filtrate is concentrated to a soft extract. After kneading one kind or two or more kinds of these soft extracts at an appropriate ratio, for example, the mixture is dried and finely divided. Alternatively, after decocting a mixture obtained by mixing any two or more of the above crude drugs in an appropriate ratio, a solid substance is separated by filtration, and the filtrate is concentrated to obtain a soft extract.
[0050]
Next, a method for producing the composition for oral cavity of the present invention will be described by taking, as an example, a case where the composition for oral cavity contains an extract of a crude drug having antioxidant activity and coenzyme Q10 and has a gel form. In addition, the following manufacturing method is characterized in that heating is not performed at the time of manufacture in order to avoid deterioration of the antioxidant during manufacture of the preparation.
[0051]
First, an oil-soluble antioxidant such as coenzyme Q10 is dissolved in an oil (solvent) in which the oil-soluble antioxidant is dissolved to produce a coating oil solution. A surfactant is added to the obtained antioxidant-coated oil solution and uniformly mixed to obtain an oil phase solution. A gelling agent (thickener) is added to the oil phase solution and stirred to obtain a dispersion.
[0052]
Next, a solvent such as water or ethanol is mixed with the extract of the crude drug having antioxidant activity, and the mixture is uniformly dissolved to obtain an aqueous phase solution. A gel-form preparation can be obtained by adding the aqueous phase solution to the dispersion and stirring it vigorously.
[0053]
Further, the pressure may be reduced during the production, and oxygen and the like contained in the preparation may be defoamed and stabilized.
[0054]
When producing the oral composition of the present invention, in addition to the above-mentioned medicinal ingredients, wetting agents, solvents, thickeners, surfactants, flavoring agents, and other additives commonly used for the oral cavity (for example, , A refreshing agent, a sweetening agent, a coloring agent, a pH adjusting agent, a preservative).
[0055]
Examples of the humectant include concentrated glycerin and sorbitol solution.
[0056]
Examples of the solvent include edible oils such as ethanol, water, olive oil, coconut oil, soybean oil, cottonseed oil, corn oil, sesame oil, rapeseed oil, peanut oil and camellia oil.
[0057]
Examples of the thickener include xanthan gum, carrageenan, sodium carboxymethylcellulose, hydroxyethylcellulose, and beeswax.
[0058]
Examples of the surfactant include sucrose fatty acid ester, sodium lauryl sulfate, sodium lauroyl sarcosine and the like.
[0059]
As a flavoring agent, menthol, peppermint oil, spearmint oil, orange oil, lemon oil, eucalyptus oil, mentha oil, acacia oil, fennel oil, kento oil, column oil, camphor oil, Nikkei oil, cinnamon oil, silica leaf oil And fragrances such as terpenes such as rose oil, sandalwood oil, clove oil, herb oil, banana oil, apple oil, methyl salicylate, carvone, anethole, limonene, and the like.
[0060]
Next, a method of using the oral composition of the present invention more effectively for prevention and treatment of periodontal disease will be described.
[0061]
The present inventor has filed Japanese Patent Application No. 2002-244286. In the specification, after brushing with a commercially available dentifrice, a composition for preventing and treating periodontal disease containing an oil extract of mastic (frankincense) and an anti-inflammatory agent as active ingredients is used, and then licorice (licorice) ), Method of preventing and treating periodontal disease by gargle with mouthwash gargle containing at least one kind of crude drug extract selected from the group consisting of betel nut, betel nut, meat muck, and primrose (Hereinafter referred to as the method of the invention of the prior application).
[0062]
The method of the present invention is characterized in that after the above-mentioned brushing and / or gargle is performed, gingival massage is performed using the oral composition of the present invention in the form of the above-mentioned application preparation. By the method of the prior application, periodontal disease-causing bacteria are suppressed, immunity in the oral cavity is enhanced, and gingival massage using the oral composition of the present invention eliminates free radicals and promotes gingival blood circulation. . As a result, a more effective prevention and treatment of periodontal disease than the method of the invention of the prior application can be obtained.
[0063]
In order to carry out the above-mentioned method of the present invention, a composition for preventing and treating periodontal disease containing an oil extract of mastic (frankincense) and an anti-inflammatory agent as active ingredients for addition to a commercially available dentifrice, Or, a mouth rinse containing at least one extract selected from the group consisting of licorice (licorice), areca (betelrot), nutmeg (meat meg), and yakumoso (mass mother grass), and the above for performing gingival massage It is convenient and preferable to use a kit for preventing and treating periodontal disease, which comprises the oral composition of the present invention in the form of a coating preparation.
[0064]
【Example】
Hereinafter, the present invention will be described more specifically with reference to Test Examples and Production Examples, but the present invention is not limited to these Test Examples and Production Examples.
[0065]
Test Example 1: Free radical scavenging activity of crude drug extract
Extracts of water (including ordinary extracts and liquid extracts) and extracts of ethanol of ethanol, watermelon, oak, oak, oak, oak, oak, nutmeg, turmeric and rosemary were subjected to the experiment.
[0066]
The superoxide scavenging activity of these crude drug extracts was measured using spin trapping-electron spin resonance (ESR). The generation system of superoxide (SOD) used hypoxanthine (HPX) and xanthine oxidase (XOD), and the adjustment of the reagent concentration and the measurement were as follows.
[0067]
2 mM HPX: 50 μL
5.5 mM DTPA: 30 μL
SOD or crude drug extract (sample): 50 μL
DMPO (1: 1): 20 μL
0.4 U / mL XOD: 50 μL
[0068]
For each sample, the above reagents were added in order, and signals were observed using an electron spin resonance (ESR)
[0069]
The ESR measurement conditions were as follows.
Output (Power): 8mW
Field Center: 335.700 mT +/- 5 mT
Sweep time (Sweep Time): 2.0 minutes
Mod Width: 0.07mT
Amplitude: 300
Time constant (Time Const): 0.1 second
[0070]
The calibration curve for measuring the superoxide scavenging activity (SOSA) is defined as the relative signal intensity (I) of the intensity of the first peak of the superoxide (DMPO-OOH) spectrum with respect to the manganese marker (Mn marker) signal, and the concentration ( Activity) Using known SOD, against each concentration of SOD
(I0/ Ix) -1
Was created by plotting the values of Where I0Is the relative signal intensity at the time of blank (PB) measurement,xIs the relative signal intensity at the time of SOD addition.
[0071]
IC in this experiment50Was 0.84 U (unit) / mL. Superoxide scavenging activity (measured twice per sample) was determined by adding 50 μL of the sample to the HPX-XOD system. The ESR measurement conditions were the same as above.
[0072]
The relative signal intensity of each sample and (I0/ Ix) -1 value is calculated, and superoxide (O2 −-) The scavenging ability was evaluated in terms of SOD activity.
[0073]
As a result, it was found that buttonpi, betel nut, and Nogikuka in particular show high superoxide scavenging activity in the range of 1600 to 5300 (SODU (unit) / mL), and that other crude drug extracts also exhibit superoxide scavenging activity. . In particular, it was revealed that the superoxide extinction activity of buttonpi was as high as 5300 SOD U / mL.
[0074]
The relative superoxide scavenging activity (converted to SOD activity) of each crude drug extract when the activity of the buttonpi showing the highest superoxide scavenging activity is set to 100 is shown as a graph in FIG.
[0075]
Production example: Method for producing gel for oral application
(1) Production of peanut extract
An appropriate amount of water was added to 20 kg of the raw crude drug of buttonpi, extracted with water, and filtered to obtain a buttonpi extract. This extract was concentrated under reduced pressure, and ethanol was added and mixed in an amount such that the ethanol concentration in the final extract became 2%, followed by sterilization to obtain 20 L of a peanut extract.
[0076]
(2) A gel for oral application was produced according to the formulation shown in Table 1 below using the red bean extract prepared in (1) above. The manufacturing method is as follows.
Coenzyme Q10, astaxanthin and vitamin C were dissolved in coconut oil to obtain an oil solution to which beeswax was added. A sucrose fatty acid ester was added to this oil solution and mixed uniformly to obtain an oil phase solution. Xanthan gum, beeswax and concentrated glycerin were added to this oil phase solution and stirred to obtain a dispersion. Next, water and ethanol were mixed and uniformly dissolved in the buttonpi extract, vitamin C and ferulic acid to obtain an aqueous phase solution. The aqueous phase solution was added to the above dispersion and stirred vigorously to obtain a gel for oral application.
[0077]
[Table 1]
【The invention's effect】
ADVANTAGE OF THE INVENTION According to the composition for oral cavity of this invention, oxidative damage in the oral cavity including a periodontal disease can be prevented or improved making use of the antioxidant activity derived from natural products, such as a crude drug extract.
[0079]
In particular, the oral composition of the present invention containing a crude drug extract and coenzyme Q10 has a synergistic and sustained superoxide scavenging activity and more effectively prevents oxidative damage in the oral cavity including periodontal disease. Or it can be improved.
[0080]
Gingival massage with the oral composition of the present invention is effective for preventing or improving oxidative damage due to periodontal disease and for preventing and treating periodontal disease by promoting gingival blood circulation.
[0081]
After adding a composition for preventing or treating periodontal disease containing an oil extract of mastic to a commercially available dentifrice and brushing it, and / or after gargle with a mouthwash comprising a crude drug extract, By performing gingival massage using the oral composition of the present invention, it is possible to effectively prevent and treat periodontal disease.
[Brief description of the drawings]
FIG. 1 is a graph showing the relative superoxide scavenging activity of each herbal extract when the superoxide scavenging activity of pomace is set at 100.
Claims (15)
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