JP2013075880A - Methylmercaptan inhibitor - Google Patents
Methylmercaptan inhibitor Download PDFInfo
- Publication number
- JP2013075880A JP2013075880A JP2011218147A JP2011218147A JP2013075880A JP 2013075880 A JP2013075880 A JP 2013075880A JP 2011218147 A JP2011218147 A JP 2011218147A JP 2011218147 A JP2011218147 A JP 2011218147A JP 2013075880 A JP2013075880 A JP 2013075880A
- Authority
- JP
- Japan
- Prior art keywords
- extract
- methyl mercaptan
- oil
- inhibitor
- water
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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Abstract
Description
本発明は、メチルメルカプタンの抑制剤に関する。より詳細には、メチルメルカプタンの生成を抑制および/または、発生したメチルメルカプタンを除去する効果を有する植物エキスに関する。 The present invention relates to an inhibitor of methyl mercaptan. More specifically, the present invention relates to a plant extract having an effect of suppressing the production of methyl mercaptan and / or removing the generated methyl mercaptan.
メチルメルカプタンは、低濃度でも異臭を感じる臭気閾値の低いいわゆる悪臭物質として知られているが、生体に対しては種々の悪影響を与える物質でもある。
人体において、メチルメルカプタンは、たまねぎやキャベツのような含硫食品や含硫アミノ酸を含む蛋白質やペプチドなどを細菌が資化することにより、代謝産物として生成することが知られている。特に口腔や咽頭においては、種々の組織が複雑な形態を構成していることからメチルメルカプタンの発生源となりうる食物の残渣が残留しやすく、かつプラークなど物理的、化学的に除去しにくい細菌の繁殖環境が整いやすい部位であるためメチルメルカプタンが発生しやすい部位と考えられる。これら口腔や咽頭においてメチルメルカプタンが発生すると、口臭の発生をもたらす。
Methyl mercaptan is known as a so-called malodorous substance having a low odor threshold that gives off an odor even at low concentrations, but is also a substance that has various adverse effects on living bodies.
In the human body, it is known that methyl mercaptan is produced as a metabolite by bacteria assimilating sulfur-containing foods such as onions and cabbages, and proteins and peptides containing sulfur-containing amino acids. Especially in the oral cavity and pharynx, various tissues constitute complex forms, so food residues that can be sources of methyl mercaptan are likely to remain, and plaques and other bacteria that are difficult to physically and chemically remove. Since the breeding environment is easy to adjust, it is considered that methyl mercaptan is likely to be generated. When methyl mercaptan is generated in the oral cavity and pharynx, it causes the generation of bad breath.
そこで、従来よりメチルメルカプタンの除去・消臭や生成抑制によりメチルメルカプタンに由来する前記事象を防止する試みがなされている。例えば、メチルメルカプタンの除去・消臭の観点から、シクロデキストリン誘導体(特許文献1)、動植物抽出物(特許文献2、3)モリブデン(特許文献4)を利用する方法、また、メチルメルカプタンの生成抑制の観点から、特定の金属を塩基とする長鎖アルキロイルザルコシン塩(特許文献5)やマメ科植物抽出物と特定の化合物の組合せ(特許文献6)をメチルメルカプタンの生成細菌の一つであるフゾバクテリウム属に作用させる方法や、植物抽出物(特許文献7、8)や3−クロローDL−アラニン(非特許文献1)、塩化亜鉛(非特許文献2)、エピガロカテキンガレート(非特許文献3)などの化合物を配合することにより、メチルメルカプタンの産生に関与するメチオニナーゼの活性を阻害させる方法などがある。しかし、何れの方法も効果が十分でなかったり、十分な量を使用すると嗜好性に難を生じたり、安全性上の懸念を生じたりするといった理由から、未だ十分に問題を解決するに至っておらず、より安全性が高く、効果の優れた方法の提供が望まれている。 Therefore, attempts have been made to prevent the above-described phenomenon derived from methyl mercaptan by removing, deodorizing, and suppressing generation of methyl mercaptan. For example, from the viewpoint of removal and deodorization of methyl mercaptan, a method using a cyclodextrin derivative (Patent Document 1), an animal and plant extract (Patent Documents 2 and 3) molybdenum (Patent Document 4), and suppression of methyl mercaptan production In view of the above, a long-chain alkylylsarcosine salt having a specific metal as a base (Patent Document 5) or a combination of a legume extract and a specific compound (Patent Document 6) is one of the bacteria that produce methyl mercaptan. A method of acting on a genus Fusobacterium, plant extracts (Patent Documents 7 and 8), 3-chloro-DL-alanine (Non-Patent Document 1), zinc chloride (Non-Patent Document 2), epigallocatechin gallate (Non-Patent Documents) There is a method of inhibiting the activity of methioninase involved in the production of methyl mercaptan by adding a compound such as 3). However, none of these methods has been adequately solved because of the lack of effectiveness, the use of a sufficient amount, which causes difficulty in palatability and raises safety concerns. Therefore, it is desired to provide a safer and more effective method.
本発明は、口臭の主原因となるメチルメルカプタンの抑制剤およびそれを配合した口臭予防用の口腔用組成物を提供することを課題とする。 An object of the present invention is to provide an inhibitor of methyl mercaptan, which is a main cause of bad breath, and an oral composition for preventing bad breath containing the same.
本発明者らは、かかる事情に鑑み鋭意検討を重ねた結果、驚くべきことにオリーブ葉抽出物、キイチゴ果実抽出物、チョウジ花抽出物、アルガニアスピノサ葉抽出物、ビルベリー抽出物、油溶性カンゾウ抽出物、サクラ葉抽出物、バラ蕾抽出物および松樹皮抽出物に優れたメチルメルカプタン抑制効果が存在することを見出し、本発明を完成するに至った。 As a result of intensive studies in view of such circumstances, the present inventors have surprisingly found that olive leaf extract, raspberry fruit extract, clove flower extract, argania spinosa leaf extract, bilberry extract, oil-soluble licorice The present inventors have found that an extract, a cherry leaf extract, a rose bud extract and a pine bark extract have an excellent methyl mercaptan inhibitory effect and have completed the present invention.
すなわち、本発明は、特に以下の項1〜4のメチルメルカプタン抑制剤およびそれを配合した口腔用組成物を提供するものである。
項1.オリーブ葉抽出物、キイチゴ果実抽出物、チョウジ花抽出物、アルガニアスピノサ葉抽出物、ビルベリー抽出物、油溶性カンゾウ抽出物、サクラ葉抽出物、バラ蕾抽出物および松樹皮抽出物からなる群より選ばれる一種以上からなるメチルメルカプタン抑制剤。
項2.請求項1に記載のメチルメルカプタン抑制剤を配合したことを特徴とする口臭予防用の口腔用組成物。
項3.メチルメルカプタン抑制剤の配合量が、組成物全量に対して固形物換算で0.001〜10質量%であることを特徴とする請求項2に記載の口臭予防用の口腔用組成物。
項4.さらに、キシリトール、マルチトール、エリスリトール、パラチニットからなる群より選ばれる一種以上を配合することを特徴とする請求項2または3の何れか一項に記載の口臭予防用の口腔用組成物。
That is, this invention provides the methyl mercaptan inhibitor of the following items 1-4 especially, and the composition for oral cavity which mix | blended it.
Item 1. From the group consisting of olive leaf extract, raspberry fruit extract, clove flower extract, argania spinosa leaf extract, bilberry extract, oil-soluble licorice extract, cherry leaf extract, rose bud extract and pine bark extract A methyl mercaptan inhibitor comprising one or more selected.
Item 2. An oral composition for preventing bad breath, comprising the methyl mercaptan inhibitor according to claim 1.
Item 3. The oral cavity composition for preventing bad breath according to claim 2, wherein the amount of the methyl mercaptan inhibitor is 0.001 to 10% by mass in terms of solid matter with respect to the total amount of the composition.
Item 4. The oral composition for preventing bad breath according to any one of claims 2 and 3, further comprising at least one selected from the group consisting of xylitol, maltitol, erythritol, and palatinit.
本発明のメチルメルカプタン抑制剤は、口腔内におけるメチルメルカプタンの生成抑制により口臭を予防できる。また、食経験もある素材であることから、長期に摂取しても安全性の心配がないため、予防的に日常使用する口腔用組成物に適用し得る。 The methyl mercaptan inhibitor of the present invention can prevent bad breath by suppressing the production of methyl mercaptan in the oral cavity. In addition, since it is a material with experience of eating, there is no concern about safety even if ingested over a long period of time, and therefore it can be applied to oral compositions for daily use in a preventive manner.
本発明にメチルメルカプタン抑制剤は、オリーブ葉、キイチゴ、チョウジ花、アルガニアスピノサ葉、ビルベリー、カンゾウ、サクラ葉、バラ蕾および松樹皮を溶媒で抽出することにより得られる植物抽出物である。なお、本願明細書において配合比率は、特に断りのない限り配合質量比率を表す。 In the present invention, the methyl mercaptan inhibitor is a plant extract obtained by extracting olive leaves, raspberries, clove flowers, Arganian spinosa leaves, bilberries, licorice, cherry leaves, rose buds and pine bark with a solvent. In the present specification, the blending ratio represents the blending mass ratio unless otherwise specified.
本発明に用いるオリーブ葉抽出物は、モクセイ科オリーブ属の植物の葉を抽出したものである。モクセイ科オリーブ属の植物としては、具体的には、オ
リーブ(Olea
europaea Linne)やその同属種(例えば、Olea welwitschii、Olea paniculataなど)を挙げることができ、500を超える品種が存在するが、品種の代表例としては、例えばネバディブロンコ、マンザニロ、ピクアル、ホジブランコ、アルベキナ、カタマラ、コロネイキ、ピッチョリーネ、パラゴン、ワッガベルダル、ミッション、ワシントン、ウエストオーストラリアミッション、サウスオーストラリアベンダル、アザパ、バルネア、コルニカブラ、ゴルダル、フラントイオ、レッチーノ、チプレッシーノ、ルッカ、アスコラーナテレナ、コレッジョッラ、モロイオロ、ブラックイタリアン、コラティーナ、ヘレナ、ロシオーラ、ワンセブンセブン、エルグレコ、ハーディズマンモスなどが挙げられる。オリーブ葉エキスは、これらモクセイ科オリーブ属の植物の葉を、有機溶剤、水または有機溶剤と水の混合物を用いて抽出することにより得られる。その中でも、特に水とエタノールの混液が好ましく、混液の混合比は例えば水:エタノールの体積比で約100:1〜約1:200が好ましく、約20:1〜1:20がより好ましく、約1:9〜1:1が最も好ましい。また、抽出時の溶媒の温度は約−4℃〜約200℃の範囲であればよいが、約30℃〜約150℃が好ましく、約40℃〜約80℃がより好ましい。これらのオリーブ葉抽出物は、オリーブ葉抽出物BG(50%1,3−ブチレングリコール水溶液:丸善製薬社製)、オリーブ葉乾燥エキス(粉末:アスク薬品社製)、オリーブ葉エキス(タマ生化学社製)、オピエース(粉末:エーザイフードケミカル社製)、オラリス(粉末:エーザイフードケミカル社製)、オリーブ葉エキス(30%エタノール水溶液:日本粉末薬品社製)、オリーブ葉エキスパウダー(粉末:日本粉末薬品社製)、オリーブ葉エキス(バイオアクティブズジャパン社製)などとして入手することができる。
The olive leaf extract used in the present invention is obtained by extracting leaves of plants belonging to the genus Oleaceae. As a plant belonging to the genus Oliveaceae, specifically, olive (Olea
europaea Linne) and its congeners (for example, Olea welwitschii, Olea paniculata, etc.), and there are over 500 varieties. Typical examples of varieties include Neva di Bronco, Manzanillo, Picual, Hogi Blanco, Albequina, Catamaran, Colonneck, Pitchorine, Paragon, Wagga Verdal, Mission, Washington, West Australia Mission, South Australia Bendal, Azapa, Balnea, Cornicabra, Gordal, Frantoio, Retcino, Chippressino, Lucca, Ascorana Terena, Correggiora, Moloioro, Black Italian, Colatina, Helena, Rossiola, One Seven Seven, El Greco, Hardys Mammoth and so on. The olive leaf extract can be obtained by extracting the leaves of these genus Oligoceae plants using an organic solvent, water, or a mixture of an organic solvent and water. Among them, a mixed solution of water and ethanol is particularly preferable, and the mixing ratio of the mixed solution is, for example, preferably about 100: 1 to about 1: 200 by volume ratio of water: ethanol, more preferably about 20: 1 to 1:20, about Most preferred is 1: 9 to 1: 1. The temperature of the solvent during extraction may be in the range of about -4 ° C to about 200 ° C, but is preferably about 30 ° C to about 150 ° C, more preferably about 40 ° C to about 80 ° C. These olive leaf extracts are olive leaf extract BG (50% 1,3-butylene glycol aqueous solution: manufactured by Maruzen Pharmaceutical Co., Ltd.), olive leaf dried extract (powder: manufactured by Ask Pharmaceutical Co., Ltd.), olive leaf extract (Tama Biochemistry) Opiace (powder: Eisai Food Chemical Co., Ltd.), Oralis (powder: Eisai Food Chemical Co., Ltd.), olive leaf extract (30% ethanol aqueous solution: manufactured by Nippon Powder Chemical Co., Ltd.), olive leaf extract powder (powder: Japan) Powdered chemicals), olive leaf extract (Bioactives Japan) and the like.
本発明に用いるキイチゴ果実抽出物は、バラ科キイチゴ属の植物の果実を抽出したものである。キイチゴ属植物としては、具体的には、モミジイチゴ(紅葉苺:Rubus palmatus var. coptophyllus)、カジイチゴ(構苺:Rubus trifidus)、ラズベリー(Rubus idaeus)、ブラックベリー(Rubus fruticosus)、フユイチゴ(冬苺:Rubus buergeri Miq.)ナワシロイチゴ(苗代苺:Rubus
parvifolius L.)、クサイチゴ(草苺:Rubus
hirsutus Thunb.)などが挙げられる。キイチゴ果実抽出物は、これらバラ科キイチゴ属の植物の果実を、有機溶剤、水または有機溶剤と水の混合物を用いて抽出することにより得られる。その中でも、特に水と1,3−ブチレングリコールまたはエタノールの混液が好ましく、水と1,3−ブチレングリコールの混液がより好ましい。これらのキイチゴ果実抽出物は、キイチゴBG(50%1,3−ブチレングリコール水溶液:丸善製薬社製)、キイチゴBG100(1,3−ブチレングリコール溶液:丸善製薬社製)、ファルコレックスキイチゴB(水/1,3−ブチレングリコール混液:一丸ファルコス社製)などとして入手することができる。
The raspberry fruit extract used in the present invention is an extract of the fruit of a plant belonging to the genus Rosaceae. Specific examples of the raspberry genus plants include maple strawberries (Rubus palmatus var. Coptophyllus), red strawberry (Rubus trifidus), raspberries (Rubus idaeus), blackberries (Rubus fruticosus), and Fuyu strawberries (winter strawberries: Rubus buergeri Miq.
parvifolius L.), wedge strawberries (Kusana: Rubus)
hirsutus Thunb.). The raspberry fruit extract can be obtained by extracting the fruit of the plant belonging to the genus Rubiaceae, using an organic solvent, water, or a mixture of an organic solvent and water. Among them, a mixed solution of water and 1,3-butylene glycol or ethanol is particularly preferable, and a mixed solution of water and 1,3-butylene glycol is more preferable. These raspberry fruit extracts are raspberry BG (50% 1,3-butylene glycol aqueous solution: manufactured by Maruzen Pharmaceutical Co., Ltd.), raspberry BG100 (1,3-butylene glycol solution: manufactured by Maruzen Pharmaceutical Co., Ltd.), Falco Rex raspberry B (water / 1,3-butylene glycol mixed solution: manufactured by Ichimaru Falcos Co., Ltd.).
本発明に用いるチョウジ花抽出物は、フトモモ科フトモモ属のチョウジの花若しくは花蕾を抽出したものである。チョウジは別名、クローブ、チョウコウ(丁香)、ヒャクリカ(百里香)とも言う。チョウジ花抽出物は、チョウジの花若しくは花蕾を、有機溶剤、水または有機溶剤と水の混合物を用いて抽出することにより得られる。その中でも、特に水または水とエタノールの混液が好ましい。これらのチョウジ花抽出物は、ファルコレックスチョウジ(水/エタノール混液:一丸ファルコス社製)、チョウジ抽出液-J(50%エタノール水溶液:丸善製薬社製)、チョウジ抽出液ET−50−D(水/エタノール混液:香栄興業社製)、などとして入手することができる。 The clove flower extract used in the present invention is obtained by extracting a clove flower or floret belonging to the genus Myrtaceae. Clove is also known as clove, butterfly (clover), or hyacinth. The clove flower extract is obtained by extracting a clove flower or floret with an organic solvent, water, or a mixture of an organic solvent and water. Among these, water or a mixed solution of water and ethanol is particularly preferable. These clove flower extracts are: Falco rex clove (water / ethanol mixture: manufactured by Ichimaru Falcos), clove extract-J (50% ethanol aqueous solution: manufactured by Maruzen Pharmaceutical), clove extract ET-50-D (water) / Ethanol mixed solution: manufactured by Koei Kogyo Co., Ltd.), etc.
本発明に用いるアルガニアスピノサ葉抽出物は、アカテツ科植物の葉を抽出したものである。アルガニアスピノサ(アルガニアスピノーザ;Argania spinosa (L.) Skeels)は別名、アルガン樹(アルガンツリー)とも言う。アルガニアスピノサ葉抽出物は、アルガニアスピノサの葉を、有機溶剤、水または有機溶剤と水の混合物を用いて抽出することにより得られる。その中でも、特に水または水とエタノールの混液が好ましい。これらのアルガニアスピノサ葉抽出物は、アルガニルLSF(水溶液:LABORATOIRES SEROBIOLOGIQUES社製)などとして入手することができる。 The Arganian spinosa leaf extract used in the present invention is obtained by extracting leaves of the Aceticaceae plant. Argania spinosa (Argania spinosa (L.) Skeels) is also known as the Argan tree. The Arganian spinosa leaf extract is obtained by extracting the Arganian spinosa leaf using an organic solvent, water or a mixture of an organic solvent and water. Among these, water or a mixed solution of water and ethanol is particularly preferable. These Arganian spinosa leaf extracts can be obtained as Arganyl LSF (aqueous solution: manufactured by LABORATOIRES SEROBIOLOGIQUES).
本発明に用いるビルベリー抽出物は、ツツジ科スノキ属Mytillus節の植物の果実や葉を有機溶剤、水または有機溶剤と水の混合物を用いて抽出することにより得られる。ツツジ科スノキ属Mytillus節の植物は、ビルベリー、セイヨウスノキ、ワートルベリー、ハックルベリーなどと呼ばれる。これらのビルベリー抽出物は、エコファームビルベリーリーフE(使用部位、葉:水/エタノール混液:一丸ファルコス社製)、キュアベリー(使用部位、葉:水/1,3−ブチレングリコール混液:一丸ファルコス社製)、ビルベロン(使用部位、果実:軟エキス:常盤植物研究所社製)、VEGETOL BILBERRY MCF 1838 HYDRO(使用部位、果実および葉:プロピレングリコール水溶液:GATTEFOSSÉ社製)などとして入手することができる。 The bilberry extract used in the present invention can be obtained by extracting the fruits and leaves of a plant of the genus Mytillus, using an organic solvent, water, or a mixture of an organic solvent and water. Plants of the genus Mytillus are called bilberries, cypresses, water berries, huckleberries, and the like. These bilberry extracts are Eco Farm Bilberry Leaf E (use site, leaf: water / ethanol mixture: Ichimaru Falcos), Cure Berry (use site, leaf: water / 1,3-butylene glycol mixture: Ichimaru Falcos) ), Bilberon (use part, fruit: soft extract: Tokiwa Plant Research Institute), VEGETOL BILBERRY MCF 1838 HYDRO (use part, fruit and leaf: propylene glycol aqueous solution: GATTEFOSS &Easy; made) .
本発明に用いる油溶性カンゾウ抽出物は、マメ科カンゾウ属の植物を抽出したものである。カンゾウ属の植物としては、ウラルカンゾウ(G. uralensis)、スペインカンゾウ(G. glabra)、新疆カンゾウ(G. inflata)、シナカンゾウ(G. echinata L.),イヌカンゾウ(G. pallidiflola MAX.)などが挙げられる。抽出部位は、主として、根、根茎、葉である。油溶性カンゾウ抽出物は、カンゾウ油性抽出物(常盤植物研究所社製)、油溶性甘草エキスP−T(丸善製薬社製)などとして入手することができる。 The oil-soluble licorice extract used in the present invention is an extract of leguminous licorice plants. As the plants of the licorice genus, there are G. uralensis, G. glabra, G. inflata, G. echinata L., G. pallidiflola MAX. Can be mentioned. Extraction sites are mainly roots, rhizomes, and leaves. The oil-soluble licorice extract can be obtained as licorice oil-based extract (manufactured by Tokiwa Plant Research Institute), oil-soluble licorice extract PT (manufactured by Maruzen Pharmaceutical Co., Ltd.) or the like.
本発明に用いるサクラ葉抽出物は、バラ科サクラ属の植物の葉を有機溶剤、水または有機溶剤と水の混合物を用いて抽出することにより得られる。これらのサクラ葉抽出物は、サクラエキスB(1,3−ブチレングリコール水溶液:一丸ファルコス社製)などとして入手することができる。 The cherry leaf extract used in the present invention is obtained by extracting leaves of a plant belonging to the genus Rosaceae using an organic solvent, water, or a mixture of an organic solvent and water. These cherry leaf extracts can be obtained as cherry extract B (1,3-butylene glycol aqueous solution: manufactured by Ichimaru Falcos).
本発明に用いるバラ蕾抽出物は、バラ科サクラ属の植物の花蕾を有機溶剤、水または有機溶剤と水の混合物を用いて抽出することにより得られる。これらのバラ蕾抽出物は、ローズバッツエキスパウダーMF(丸善製薬社製)、バラ蕾エキス末(丸栄トレーディング社製)などとして入手することができる。 The rose bud extract used in the present invention can be obtained by extracting florets of a plant belonging to the family Rosaceae using an organic solvent, water, or a mixture of an organic solvent and water. These rose bud extracts can be obtained as rose butts extract powder MF (manufactured by Maruzen Pharmaceutical Co., Ltd.), rose bud extract powder (manufactured by Maruei Trading).
本発明に用いる松樹皮抽出物は、マツ科マツ属のフランスカイガンショウ(フランス海岸松:Pinus pinaster )の樹皮を有機溶剤、水または有機溶剤と水の混合物を用いて抽出することにより得られ、フランスカイガンジョウ樹皮エキスとも称せられる。これらの松樹皮抽出物は、OLIGOPIN(DRT社製)、フラバンジェノール(東洋新薬社製)、ピクノジェノール(Horphag
Research社製)などとして入手することができる。
The pine bark extract used in the present invention is obtained by extracting the bark of Pinus pinaster from the Pinus pinaster using an organic solvent, water, or a mixture of organic solvent and water. , Also called the French cabbage bark extract. These pine bark extracts are OLIGOPIN (DRT), Flavangenol (Toyo Shinyaku), Pycnogenol (Horphag)
Research Inc.).
本発明のメチルメルカプタン抑制剤は、通常、口腔用組成物に配合することにより口腔内に適用される。配合できる口腔用組成物としては、特に限定するものではないが、練歯磨剤、ジェル剤、液体歯磨剤、洗口剤、スプレー剤、パスタ剤、軟ペースト剤(クリーム状製剤)、軟膏状製剤、錠剤、顆粒剤、チューイングガム剤、キャンディー剤、トローチ剤、タブレット剤、チュアブルタブレット剤、粒カプセル剤、飲料等の形態(剤形)として用いることができる。このなかでも、練歯磨剤、ジェル剤、液体歯磨剤、洗口剤、スプレー剤、パスタ剤、軟ペースト剤(クリーム状製剤)、タブレット剤、キャンディー剤などの形態が好ましく練歯磨剤、ジェル剤、液体歯磨剤、洗口剤、スプレー剤、タブレット剤、キャンディー剤などの形態が最も好ましい。 The methyl mercaptan inhibitor of this invention is normally applied in an oral cavity by mix | blending with an oral composition. Although it does not specifically limit as an oral composition which can be mix | blended, Toothpaste, a gel agent, a liquid dentifrice, a mouthwash, a spray agent, a pasta agent, a soft paste (cream-form preparation), an ointment-form preparation , Tablets, granules, chewing gum, candy, lozenges, tablets, chewable tablets, granule capsules, beverages, etc. (dosage forms). Of these, toothpastes, gels, liquid dentifrices, mouthwashes, sprays, pasta agents, soft pastes (cream formulations), tablets, candy agents and the like are preferred. , Liquid dentifrice, mouthwash, spray, tablet, candy and the like are most preferred.
メチルメルカプタン抑制剤は、通常、固形物換算でこれら口腔用組成物に対して、0.001〜10質量%、配合する。0.001質量%より少ないと所期の効果が期待できず、10質量%より多いと抽出物由来の香味(渋味など)が強く感じられるため、嗜好性が悪くなり好ましくない。 The methyl mercaptan inhibitor is usually blended in an amount of 0.001 to 10% by mass with respect to these oral compositions in terms of solid matter. If the amount is less than 0.001% by mass, the desired effect cannot be expected. If the amount is more than 10% by mass, the flavor (such as astringency) derived from the extract is strongly felt, and the palatability is deteriorated.
より至適な配合量は、メチルメルカプタン抑制剤の種類と口腔用組成物の財形によって相違し、具体的には以下の通りである。なお、配合量は全て口腔用組成物全量に対する固形分換算の質量%である。オリーブ葉抽出物の場合、練歯磨剤、ジェル剤は0.01〜1質量%、洗口剤や液体歯磨剤は0.001〜0.2質量%、スプレー剤、タブレット剤、キャンディー剤は0.1〜10質量%配合することが好ましい。ビルベリー抽出物の場合、練歯磨剤、ジェル剤、スプレー剤、タブレット剤、キャンディー剤は0.001〜0.02質量%、洗口剤や液体歯磨剤は0.001〜0.004質量%配合することが好ましい。アルガニアスピノサ葉抽出物の場合、練歯磨剤、ジェル剤、スプレー剤、タブレット剤、キャンディー剤は0.001〜0.25質量%、洗口剤や液体歯磨剤は0.001〜0.05質量%配合することが望ましい。 More optimal blending amounts differ depending on the type of methyl mercaptan inhibitor and the shape of the oral composition, and are specifically as follows. In addition, all compounding quantities are the mass% of solid content conversion with respect to the oral cavity composition whole quantity. In the case of olive leaf extract, toothpaste and gel are 0.01 to 1% by mass, mouthwash and liquid dentifrice are 0.001 to 0.2% by mass, spray, tablet and candy are 0. It is preferable to mix 1 to 10% by mass. In the case of bilberry extract, toothpaste, gel, spray, tablet, candy is 0.001-0.02% by mass, mouthwash and liquid dentifrice is 0.001-0.004% by mass It is preferable to do. In the case of Arganian spinosa leaf extract, 0.001-0.25 mass% for toothpaste, gel, spray, tablet, candy, 0.001-0.05 for mouthwash and liquid dentifrice. It is desirable to blend in mass%.
本発明のメチルメルカプタン抑制剤を配合する口腔用組成物には、本発明の効果を損なわない範囲であれば、通常口腔用組成物に配合し得る成分をさらに配合してもよい。 In the composition for oral cavity which mix | blends the methyl mercaptan inhibitor of this invention, if it is a range which does not impair the effect of this invention, you may further mix | blend the component which can be normally mix | blended with an oral composition.
界面活性剤としては、ノニオン界面活性剤、アニオン界面活性剤または両性界面活性剤を配合することができる。具体的には、ノニオン界面活性剤としてはショ糖脂肪酸エステル、マルトース脂肪酸エステル、ラクトース脂肪酸エステル等の糖脂肪酸エステル、脂肪酸アルカノールアミド類、ソルビタン脂肪酸エステル、脂肪酸モノグリセライド、ポリオキシエチレン付加係数が4〜15、アルキル基の炭素数が10〜18であるポリオキシエチレンアルキルエーテル系またはポリオキシエチレン付加係数が10〜18、アルキル基の炭素数が9であるポリオキシエチレンアルキルフェニルエーテル、セバシン酸ジエチル、ポリオキシエチレン硬化ヒマシ油、ポリオキシエチレンソルビタン脂肪酸エステル、ポリオキシエチレングリセリン脂肪酸エステル、ポリオキシエチレンソルビット脂肪酸エステル、ポリエチレングリコール脂肪酸エステル、ポリエチレンラノリン、ポリエチレンステロール、ポリエチレンラノリンアルコール、アルキルグルコシド、ポリオキシエチレンポリオキシプロピレンブロックコポリマー等が挙げられる。アニオン界面活性剤としては、ラウリル硫酸ナトリウム、ポリオキシエチレンラウリルエーテル硫酸ナトリウム等の硫酸エステル塩、ラウリルスルホコハク酸ナトリウム、ポリオキシエチレンラウリルエーテルスルホコハク酸ナトリウム等のスルホコハク酸塩、ココイルサルコシンナトリウム、ラウロイルメチルアラニンナトリウム等のアシルアミノ酸塩、ココイルメチルタウリンナトリウム等が挙げられる。両性イオン界面活性剤としては、ラウリルジメチルアミノ酢酸ベタイン、ヤシ油脂肪酸アミドプロピルジメチルアミノ酢酸ベタイン等の酢酸ベタイン型活性剤、N−ココイル−N−カルボキシメチル−N−ヒドロキシエチルエチレンジアミンナトリウム等のイミダゾリン型活性剤、N−ラウリルジアミノエチルグリシン等のアミノ酸型活性剤等が挙げられる。これらの界面活性剤は、単独であるいは2種以上を組み合わせて用いることができる。 As the surfactant, a nonionic surfactant, an anionic surfactant or an amphoteric surfactant can be blended. Specifically, nonionic surfactants include sugar fatty acid esters such as sucrose fatty acid esters, maltose fatty acid esters, and lactose fatty acid esters, fatty acid alkanolamides, sorbitan fatty acid esters, fatty acid monoglycerides, and polyoxyethylene addition coefficients of 4 to 15. A polyoxyethylene alkyl ether type having an alkyl group having 10 to 18 carbon atoms or a polyoxyethylene alkyl phenyl ether having a polyoxyethylene addition coefficient of 10 to 18 and an alkyl group having 9 carbon atoms, diethyl sebacate, poly Oxyethylene hydrogenated castor oil, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene glycerin fatty acid ester, polyoxyethylene sorbit fatty acid ester, polyethylene glycol fatty acid ester, polyester Renranorin, polyethylene sterols, polyethylene lanolin alcohols, alkyl glucosides, polyoxyethylene polyoxypropylene block copolymers, and the like. Anionic surfactants include sulfate esters such as sodium lauryl sulfate and polyoxyethylene lauryl ether sulfate, sodium lauryl sulfosuccinate, sulfosuccinates such as sodium polyoxyethylene lauryl ether sulfosuccinate, cocoyl sarcosine sodium, lauroylmethylalanine Examples include acyl amino acid salts such as sodium, cocoyl methyl taurine sodium and the like. Zwitterionic surfactants include betaine acetate type activators such as lauryl dimethylaminoacetic acid betaine, coconut oil fatty acid amidopropyldimethylaminoacetic acid betaine, and imidazoline type such as N-cocoyl-N-carboxymethyl-N-hydroxyethylethylenediamine sodium. Examples include activators and amino acid type activators such as N-lauryldiaminoethylglycine. These surfactants can be used alone or in combination of two or more.
香味剤としては、例えばメントール、カルボン、サリチル酸メチル、バニリン、ベンジルサクシネート、メチルオイゲノール、アネトール、リモネン、オシメン、n−デシルアルコール、メチルアセタート、シトロネニルアセテート、シネオール、エチルリナロール、ワニリン、タイム、ナツメグ、スペアミント油、ペパーミント油、レモン油、オレンジ油、セージ油、ローズマリー油、珪皮油、シソ油、冬緑油、丁子油、ユーカリ油、ピメント油、ティーツリー油、タバナ油、スターアニス油、フェンネル油、珪藻油、バジル油などが挙げられる。これら香料は、単独であるいは2種以上を組み合わせて用いることができる。 As a flavoring agent, for example, menthol, carvone, methyl salicylate, vanillin, benzyl succinate, methyl eugenol, anethole, limonene, ocimene, n-decyl alcohol, methyl acetate, citronenyl acetate, cineol, ethyl linalool, vanillin, thyme , Nutmeg, spearmint oil, peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, cinnamon oil, perilla oil, winter green oil, clove oil, eucalyptus oil, pimento oil, tea tree oil, tabana oil, star Examples include anise oil, fennel oil, diatom oil, and basil oil. These fragrance | flavors can be used individually or in combination of 2 or more types.
研磨剤としては、例えば研磨性沈降シリカ、研磨性ゲルシリカなどの研磨性シリカ、リン酸水素カルシウム・二水和物および無水物、リン酸カルシウム、第3リン酸カルシウム、第3リン酸マグネシウム、ピロリン酸カルシウム、ハイドロキシアパタイト、不溶性メタリン酸ナトリウム、ケイ酸アルミニウム、ケイ酸ジルコニウム、ケイ酸カルシウム、炭酸カルシウム、炭酸マグネシウム、アルミナ、水酸化アルミニウム、硫酸カルシウム、ポリメタクリル酸メチル、パミス(軽石)、ベントナイト、合成樹脂などが挙げられる。これら研磨剤は、単独であるいは2種以上を組み合わせて使用することができる。 Examples of the abrasive include abrasive silica such as abrasive precipitated silica and abrasive gel silica, calcium hydrogenphosphate dihydrate and anhydride, calcium phosphate, tertiary calcium phosphate, tertiary magnesium phosphate, calcium pyrophosphate, hydroxyapatite Insoluble sodium metaphosphate, aluminum silicate, zirconium silicate, calcium silicate, calcium carbonate, magnesium carbonate, alumina, aluminum hydroxide, calcium sulfate, polymethyl methacrylate, pumice, bentonite, synthetic resin, etc. It is done. These abrasive | polishing agents can be used individually or in combination of 2 or more types.
粘結剤としては、例えばカルボキシメチルセルロースナトリウム、カルボキシメチルエチルセルロース塩、ヒドロキシエチルセルロース、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロースなどのセルロース誘導体、キサンタンガム、ジェランガムなどの微生物産生高分子、トラガントガム、カラヤガム、アラビヤガム、カラギーナン、デキストリンなどの天然高分子または天然ゴム類、ポリビニルアルコール、ポリビニルピロリドンなどの合成高分子、増粘性シリカ、ビーガムなどの無機粘結剤、塩化O−[2−ヒドロキシ−3−(トリメチルアンモニオ)プロピル]ヒドロキシエチルセルロースなどのカチオン性粘結剤が挙げられる。これら粘結剤は、単独であるいは2種以上を組み合わせて使用することができる。 Examples of the binder include carboxymethyl cellulose sodium, carboxymethyl ethyl cellulose salt, cellulose derivatives such as hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, microbial polymer such as xanthan gum, gellan gum, tragacanth gum, karaya gum, arabiya gum, carrageenan, dextrin. Natural polymers such as natural rubbers, synthetic polymers such as polyvinyl alcohol and polyvinyl pyrrolidone, thickening silica, inorganic binders such as bee gum, O- [2-hydroxy-3- (trimethylammonio) propyl] chloride Cationic binders such as hydroxyethyl cellulose can be mentioned. These binders can be used alone or in combination of two or more.
甘味剤としては、例えばサッカリン、サッカリンナトリウム、アセスルファームカリウム、ステビアエキス、ステビオサイド、ネオヘスペリジルジヒドロカルコン、グリチルリチン、ペリラルチン、ソウマチン、アスパルチルフェニルアラニンメチルエステル、メトキシシンナミックアルデヒド、スクラロース、パラチノース、パラチニット、エリスリトール、マルチトール、キシリトール、ラクチトールなどが挙げられる。これら甘味剤は、単独であるいは2種以上を組み合わせて使用することができる。 Examples of sweeteners include saccharin, saccharin sodium, acesulfame potassium, stevia extract, stevioside, neohesperidyl dihydrochalcone, glycyrrhizin, perilartin, saumatine, aspartylphenylalanine methyl ester, methoxycinnamic aldehyde, sucralose, palatinose, palatinit, erythritol. , Maltitol, xylitol, lactitol and the like. These sweeteners can be used alone or in combination of two or more.
湿潤剤としては、例えばグリセリン、エチレングリコール、プロピレングリコール、1,3−プロパンジオール、1,3−ブチレングリコール、ソルビット、ポリエチレングリコール、ポリプロピレングリコールなどを単独であるいは2種以上を組み合わせて使用することができる。 As the wetting agent, for example, glycerin, ethylene glycol, propylene glycol, 1,3-propanediol, 1,3-butylene glycol, sorbit, polyethylene glycol, polypropylene glycol and the like may be used alone or in combination of two or more. it can.
保存剤としては、例えばメチルパラベン、プロピルパラベンなどのパラベン類、安息香酸ナトリウムなどの安息香酸塩などが挙げられる。これらの保存剤は、単独であるいは2種以上を組み合わせて使用することができる。 Examples of the preservative include parabens such as methylparaben and propylparaben, and benzoates such as sodium benzoate. These preservatives can be used alone or in combination of two or more.
またpH調整剤としては、クエン酸、リン酸、リンゴ酸、グルコン酸、マレイン酸、アスパラギン酸、コハク酸、グルクロン酸、フマル酸、グルタミン酸、アジピン酸、およびこれらの塩や、塩酸、水酸化ナトリウム、水酸化カリウム、ケイ酸ナトリウムなどが挙げられる。これらの成分は単独あるいは2種以上を組合せて本発明の口腔用組成物に含ませることができる。なお、本発明の口腔用組成物は、口腔内で使用できる範囲であれば、そのpHは特に制限されないが、通常pH3.0〜10.5、好ましくはpH5.5〜8.0である。 Examples of pH adjusters include citric acid, phosphoric acid, malic acid, gluconic acid, maleic acid, aspartic acid, succinic acid, glucuronic acid, fumaric acid, glutamic acid, adipic acid, and salts thereof, hydrochloric acid, sodium hydroxide , Potassium hydroxide, sodium silicate and the like. These components can be contained in the oral composition of the present invention alone or in combination of two or more. In addition, as long as the composition for oral cavity of this invention is a range which can be used in an oral cavity, the pH will not be restrict | limited, However, Usually, pH is 3.0-10.5, Preferably it is pH 5.5-8.0.
薬効成分としては、殺菌剤として塩化セチルピリジニウム以外にも例えば塩酸クロルヘキシジン、グルコン酸クロルヘキシジン、塩化ベンゼトニウム、塩化ベンザルコニウムなどのカチオン性殺菌剤;ドデシルジアミノエチルグリシンなどの両性殺菌剤;イソプロピルメチルフェノール、トリクロサンなどの非イオン殺菌剤;デキストラナーゼ、アミラーゼ、プロテアーゼ、ムタナーゼ、リゾチーム、溶菌酵素(リテックエンザイム)などの酵素;抗炎症剤としてグリチルレチン酸、グリチルリチン酸ジカリウムなどのグリチルリチン酸塩;血行促進剤としてニコチン酸または酢酸トコフェロールなど;抗プラスミン剤としてトラネキサム酸、イプシロンアミノカプロン酸など;出血改善剤としてアスコルビン酸など;組織修復剤としてアラントインなど;再石灰化剤としてフッ化ナトリウムなどのフッ素化合物;その他、水溶性溶媒で抽出された植物抽出物、クロロフィル、塩化ナトリウム、カロペプタイド、塩化亜鉛、ヒノキチオールなどが挙げられ、これらを単独あるいは2種以上を組み合わせて配合することができる。 As a medicinal component, in addition to cetylpyridinium chloride as a bactericidal agent, for example, cationic bactericides such as chlorhexidine hydrochloride, chlorhexidine gluconate, benzethonium chloride, benzalkonium chloride; amphoteric bactericides such as dodecyldiaminoethylglycine; isopropylmethylphenol, Nonionic fungicides such as triclosan; Enzymes such as dextranase, amylase, protease, mutanase, lysozyme, lytic enzyme (lytechenzyme); Glycyrrhizic acid salts such as glycyrrhetinic acid and dipotassium glycyrrhizinate as anti-inflammatory agents; Nicotinic acid or tocopherol acetate, etc .; Tranexamic acid, epsilon aminocaproic acid, etc. as antiplasmin agent; Ascorbic acid, etc. as bleeding remedy; Fluorine compounds such as sodium fluoride as remineralizing agents; plant extracts extracted with water-soluble solvents, chlorophyll, sodium chloride, caropeptides, zinc chloride, hinokitiol, etc. It can mix | blend combining a seed | species or more.
上記の成分のうち、キシリトール、マルチトール、エリスリトール、パラチニットを配合した口腔用組成物は、口腔用組成物に配合されたメチルメルカプタン抑制剤の渋みや苦味を抑制し、口腔用組成物の嗜好性を高めるため好ましい。特に渋みや苦味を感じやすい液体歯磨剤、洗口剤、スプレー剤において効果が得られやすく、組成物全量に対して、1〜10質量%配合することが好ましく、5〜10質量%配合することがより好ましい。なお、10質量%より多く配合した場合、口腔用組成物の使用時に、容器の吐出口やキャップ内部に付着した組成物からキシリトールなどの結晶の析出が生じる可能性が高まるため好ましくない。 Among the above components, the oral composition containing xylitol, maltitol, erythritol, and palatinit suppresses the astringency and bitterness of the methyl mercaptan inhibitor contained in the oral composition, and the palatability of the oral composition Is preferable in order to increase. In particular, effects are easily obtained in liquid dentifrices, mouthwashes, and sprays that tend to feel astringency and bitterness, and it is preferably blended in an amount of 1 to 10% by weight, preferably 5 to 10% by weight based on the total amount of the composition. Is more preferable. In addition, it is not preferable to add more than 10% by mass since the possibility of precipitation of crystals such as xylitol from the composition adhering to the discharge port of the container or the inside of the cap increases when the oral composition is used.
以下、本発明を具体的に説明するが、本発明は下記の例に限定されるものではない。なお、以下特に断りのない限り「%」は「質量%」を示す。 Hereinafter, the present invention will be specifically described, but the present invention is not limited to the following examples. In the following, “%” means “mass%” unless otherwise specified.
メチルメルカプタンの除去効果の評価
以下の方法に従い、メチルメルカプタンの除去効果を測定した。
15mL容量のガラスビンに0.1Mリン酸緩衝液(pH7.5)1.5mL試験用液1.0mLを加えボルテックスミキサーで5秒攪拌した。1μg/mLメチルメルカプタン溶液0.5mLを加えボルテックスミキサーで5秒攪拌後、37℃の恒温層で6分間保温した。ガスタイトシリンジで空気を1mL注入、ボルテックスミキサーで5秒間攪拌後、ガラスビンのヘッドスペースから気体を1mLを抜き取り、ガスクロマトグラフに注入しメチルメルカプタン量を測定した。なお分析条件は以下に示す。メチルメルカプタンの除去率は、被検溶液を入れた際のメチルメルカプタン量をKi、試験溶液の代わりエタノール:水=4:1(容量比)を入れた際のメチルメルカプタン量をK0とし、下記の式に従って算出した。なお、ブランクにはエタノール:蒸留水=4:1(容量比)を用いた。得られた結果を表1に示す。
カラム :SUPELCO、Supel−QPLOT 0.53mm×30m
カラム温度 :50℃ hold 1min 50-130℃ 10℃/min
検出器 :炎光光度検出器
注入量 :1mL
使用機器 :Auto system XL
吸着除去率(%)=[(K0-Ki) /K0]×100
評価に使用した被検溶液および1μg/mLメチルメルカプタン溶液(1μg/mLMeSH溶液)は下記の方法で調製した。
被検体の調製:各被検体を、エタノール:蒸留水=4:1(容量比)で混合した溶液で溶解又は希釈し、被検体に含有される固形物換算濃度が0.1質量%となるように調製した。
1μg/mLMeSH溶液の調製:1μg/μLMeSH標準液(和光純薬製 悪臭物質試験用)2mLにエタノールを加え200mLとした。さらに、当該溶液2mLに蒸留水を加え、全量を20mLに調整し、1μg/mLMeSH溶液とした。
被検体は下記のものを使用した。
オリーブ葉抽出物:オピエース(粉末:エーザイフードケミカル社製)
キイチゴ果実抽出物:キイチゴ抽出物BG(丸善製薬社製)
チョウジ花抽出物:ファルコレックスチョウジ(水/エタノール混液:一丸ファルコス社製)
アルガニアスピノサ葉抽出物:アルガニルLSF(水溶液:LABORATOIRES SEROBIOLOGIQUES社製)
ビルベリー抽出物:エコファームビルベリーリーフE(使用部位、葉:水/エタノール混液:一丸ファルコス社製)
油溶性カンゾウ抽出物:油溶性甘草エキスP−T(丸善製薬社製)
サクラ葉抽出物:サクラエキスB(1,3−ブチレングリコール水溶液:一丸ファルコス社製)
バラ蕾抽出物:ローズバッツエキスパウダーMF(丸善製薬社製)
松樹皮抽出物:ピクノジェノール(Horphag Research社製)
米糠エキス:紫玄米ヌカエキスBG(丸善製薬社製)
ウコンエキス:ファルコレックスウコンB(一丸ファルコス社製)
リンゴ果実エキス:ファルコレックスリンゴB(一丸ファルコス社製)
Evaluation of removal effect of methyl mercaptan The removal effect of methyl mercaptan was measured according to the following method.
To a glass bottle of 15 mL capacity, 0.1 mL of a 0.1 M phosphate buffer (pH 7.5) 1.5 mL test solution was added and stirred for 5 seconds with a vortex mixer. 0.5 mL of a 1 μg / mL methyl mercaptan solution was added, and the mixture was stirred for 5 seconds with a vortex mixer, and then kept at a constant temperature layer of 37 ° C. for 6 minutes. After injecting 1 mL of air with a gas tight syringe and stirring for 5 seconds with a vortex mixer, 1 mL of gas was extracted from the head space of the glass bottle and injected into a gas chromatograph to measure the amount of methyl mercaptan. The analysis conditions are shown below. The methyl mercaptan removal rate is defined as follows: Ki is the amount of methyl mercaptan when the test solution is added, and K0 is the amount of methyl mercaptan when ethanol: water = 4: 1 (volume ratio) is used instead of the test solution. Calculated according to the formula. In addition, ethanol: distilled water = 4: 1 (volume ratio) was used for the blank. The obtained results are shown in Table 1.
Column: SUPELCO, Supel-QPLOT 0.53mm × 30m
Column temperature: 50 ° C hold 1min 50-130 ° C 10 ° C / min
Detector: Flame photometric detector Injection volume: 1 mL
Equipment used: Auto system XL
Adsorption removal rate (%) = [(K0−Ki) / K0] × 100
The test solution and 1 μg / mL methyl mercaptan solution (1 μg / mL MeSH solution) used for evaluation were prepared by the following method.
Preparation of specimen: Each specimen is dissolved or diluted with a solution mixed with ethanol: distilled water = 4: 1 (volume ratio), and the solid equivalent concentration contained in the specimen is 0.1% by mass. It was prepared as follows.
Preparation of 1 μg / mL MeSH solution: Ethanol was added to 200 mL to 2 mL of a standard solution of 1 μg / μL MeSH (for Wodor Pure Chemicals test for malodorous substance). Furthermore, distilled water was added to 2 mL of the solution to adjust the total volume to 20 mL, and a 1 μg / mL MeSH solution was obtained.
The following samples were used.
Olive leaf extract: Opiace (powder: Eisai Food Chemical Co., Ltd.)
Raspberry fruit extract: Raspberry extract BG (Maruzen Pharmaceutical Co., Ltd.)
Clove flower extract: Falco Rex clove (water / ethanol mixture: Ichimaru Falcos)
Arganian spinosa leaf extract: Arganyl LSF (aqueous solution: LABORATOIRES SEROBIOLOGIQUES)
Bilberry extract: Eco Farm Bilberry Leaf E (use site, leaf: water / ethanol mixture: Ichimaru Falcos)
Oil-soluble licorice extract: Oil-soluble licorice extract PT (manufactured by Maruzen Pharmaceutical Co., Ltd.)
Sakura leaf extract: Sakura extract B (1,3-butylene glycol aqueous solution: manufactured by Ichimaru Falcos)
Rose bud extract: Rose butts extract powder MF (Maruzen Pharmaceutical Co., Ltd.)
Pine bark extract: Pycnogenol (Horphag Research)
Rice bran extract: Purple brown rice nuka extract BG (manufactured by Maruzen Pharmaceutical Co., Ltd.)
Turmeric extract: Falco Rex Turmeric B (Ichimaru Falcos)
Apple fruit extract: Falco Rex Apple B (Ichimaru Falcos)
表1に示したとおり、オリーブ葉抽出物、キイチゴ果実抽出物、チョウジ花抽出物、アルガニアスピノサ葉抽出物、ビルベリー抽出物、油溶性カンゾウ抽出物、サクラ葉抽出物、バラ蕾抽出物、松樹皮抽出物には優れたメチルメルカプタン除去効果があることがわかった。特に、オリーブ葉抽出物、キイチゴ果実抽出物、チョウジ花抽出物、アルガニアスピノサ葉抽出物、ビルベリー抽出物は高い効果を示し、その中でも、オリーブ葉抽出物、キイチゴ果実抽出物、チョウジ花抽出物は顕著な効果を示すことがわかった。一方、米糠エキス、ウコンエキス、リンゴ果実エキスには大きな除去効果が得られないことが判った。 As shown in Table 1, olive leaf extract, raspberry fruit extract, clove flower extract, Arganian spinosa leaf extract, bilberry extract, oil-soluble licorice extract, cherry leaf extract, rose bud extract, pine The bark extract was found to have an excellent methyl mercaptan removal effect. In particular, olive leaf extract, raspberry fruit extract, clove flower extract, argania spinosa leaf extract, bilberry extract show high effects, among them olive leaf extract, raspberry fruit extract, clove flower extract Was found to show a remarkable effect. On the other hand, it was found that the rice bran extract, turmeric extract, and apple fruit extract do not have a large removal effect.
メチルメルカプタンの発生抑制効果の評価
以下の方法に従い、メチルメルカプタンの発生抑制効果を測定した。
15mL容量のガラスビンに塩緩衝液770μL、被検溶液100μL、菌懸濁液100μLを加え手で軽く振とうしたのち、33mML−メチオニン塩緩衝溶液30μLを加え、37℃で90分培養した。培養後、直ちに3Mリン酸水溶液500μLを加えて攪拌し、10分静置した後に、ガラスビンのヘッドスペースから気体を1mL採取し、ガスクロマトグラフに注入しメチルメルカプタンを定量した。なお、分析条件は前記のメチルメルカプタンの除去効果の評価に記載の条件と同じである。メチルメルカプタンの発生抑制率(%)は、被検溶液を入れた場合のメチルメルカプタン量をKi、
被検溶液の代わりに塩緩衝液を入れた場合のメチルメルカプタン量をK0とし、下記の式を用いて算出した。なお、ブランクとしては、50mM塩化ナトリウムを添加した40mMリン酸カリウム緩衝液(pH7.7)を用いた。得られた結果を表2に示す。
発生抑制率(%)=[(K0-Ki) /K0]×100
当該試験に使用した菌、試薬、被検溶液、培地、菌懸濁液は下記に従った。
使用細菌:ポルフィロモナス・ジンジバリスW83株(以下、P.g.と略す場合がある)
塩緩衝液:40mMリン酸水素2カリウム水溶液に、40mMリン酸2水素カリウム水溶液を加えpH7.7に調整した。当該溶液1Lをとり、塩化ナトリウム2.92gを加え、加熱滅菌したものを用いた。
被検溶液:各被検体を、塩緩衝液を用いて固形物換算で各々の規定濃度になるように調製した。
培地:まず、hemin0.25gを1N水酸化ナトリウム5mLに溶解し、さらに蒸留水20mLを加えたものをA液とした。またmenadione0.025gを99%エチルアルコール25mLに溶解したものをB液とした。前記A液とB液を混合してhemin, menadione溶液を調製した。培地は、TSB40g、hemin, menadione溶液1mL、Yeast product1gを蒸留水0.9Lに溶解し、オートクレーブ処理を行ったものを用いた。この培地を、以下、「TSB+h,m,y」と称する。
菌懸濁液:P.g.をTSB+h,m,y10mlに植菌し、37℃で24〜48hr嫌気培養した後、この培養溶液を新たなTSB+h,m,y 100mlに添加し、37℃で24〜48hr嫌気培養した。この菌培養液を8000×gで10分間遠心後、塩緩衝液で洗浄したのち、塩緩衝液で懸濁しOD550nmで約0.3に合わせたものを用いた
33mML−メチオニン塩緩衝溶液:L−メチオニンを、前記塩緩衝溶液を用いて、最終濃度が33mMになるように調製し、ろ過滅菌したものを用いた。
3Mリン酸水溶液:リン酸と蒸留水を用いて、最終濃度が3Mとなるように調製したものを用いた。
被検体は下記のものを使用した。
オリーブ葉抽出物:オピエース(粉末:エーザイフードケミカル社製)
キイチゴ果実抽出物:キイチゴ抽出物BG(丸善製薬社製)
チョウジ花抽出物:ファルコレックスチョウジ(水/エタノール混液:一丸ファルコス社製)
アルガニアスピノサ葉抽出物:アルガニルLSF(水溶液:LABORATOIRES SEROBIOLOGIQUES社製)
ビルベリー抽出物:エコファームビルベリーリーフE(使用部位、葉:水/エタノール混液:一丸ファルコス社製)
油溶性カンゾウ抽出物:油溶性甘草エキスP−T(丸善製薬社製)
サクラ葉抽出物:サクラエキスB(1,3−ブチレングリコール水溶液:一丸ファルコス社製)
ノバラ果実エキス:ファルコレックスノバラB(一丸ファルコス社製)
セイヨウサンザシエキス:ファルコレックスセイヨウサンザシB(一丸ファルコス社製)
Evaluation of Methyl Mercaptan Generation Suppression Effect The methyl mercaptan generation suppression effect was measured according to the following method.
After adding 770 μL of the salt buffer, 100 μL of the test solution, and 100 μL of the bacterial suspension to a glass bottle of 15 mL volume, and shaking lightly by hand, 30 μL of 33 mM L-methionine salt buffer was added, followed by incubation at 37 ° C. for 90 minutes. Immediately after culturing, 500 μL of 3M phosphoric acid aqueous solution was added and stirred, and allowed to stand for 10 minutes. Then, 1 mL of gas was sampled from the head space of the glass bottle, and injected into a gas chromatograph to quantify methyl mercaptan. The analysis conditions are the same as those described in the evaluation of the removal effect of methyl mercaptan. The methyl mercaptan generation inhibition rate (%) is defined as the amount of methyl mercaptan when the test solution is added, Ki,
The amount of methyl mercaptan when a salt buffer was added instead of the test solution was defined as K0 and calculated using the following formula. As a blank, 40 mM potassium phosphate buffer (pH 7.7) to which 50 mM sodium chloride was added was used. The obtained results are shown in Table 2.
Occurrence suppression rate (%) = [(K0−Ki) / K0] × 100
The bacteria, reagents, test solution, culture medium, and bacterial suspension used in the test were as follows.
Bacteria used: Porphyromonas gingivalis strain W83 (hereinafter sometimes abbreviated as Pg)
Salt buffer solution: 40 mM aqueous potassium dihydrogen phosphate solution was added to 40 mM aqueous dipotassium hydrogen phosphate solution to adjust the pH to 7.7. 1 L of the solution was taken and 2.92 g of sodium chloride was added and heat sterilized.
Test solution: Each test sample was prepared using a salt buffer so as to have a prescribed concentration in terms of solid matter.
Medium: First, 0.25 g of hemin was dissolved in 5 mL of 1N sodium hydroxide, and 20 mL of distilled water was further added to make solution A. A solution B was prepared by dissolving 0.025 g of menadione in 25 mL of 99% ethyl alcohol. The solutions A and B were mixed to prepare a hemin and menadione solution. The medium used was an autoclaved solution obtained by dissolving 40 g of TSB, 1 mL of hemin, menadione solution and 1 g of Yeast product in 0.9 L of distilled water. This medium is hereinafter referred to as “TSB + h, m, y”.
Bacterial suspension: Pg was inoculated into TSB + h, m, y 10 ml, anaerobically cultured at 37 ° C. for 24-48 hr, and then this culture solution was added to fresh TSB + h, m, y 100 ml, and at 37 ° C., 24-48 hr. Anaerobic culture was performed. This bacterial culture was centrifuged at 8000 × g for 10 minutes, washed with a salt buffer, suspended in a salt buffer, and adjusted to about 0.3 at an OD550 nm of 33 mM L-methionine salt buffer solution: L- Methionine was prepared using the salt buffer solution so as to have a final concentration of 33 mM and sterilized by filtration.
3M phosphoric acid aqueous solution: A phosphoric acid and distilled water were used to prepare a final concentration of 3M.
The following samples were used.
Olive leaf extract: Opiace (powder: Eisai Food Chemical Co., Ltd.)
Raspberry fruit extract: Raspberry extract BG (Maruzen Pharmaceutical Co., Ltd.)
Clove flower extract: Falco Rex clove (water / ethanol mixture: Ichimaru Falcos)
Arganian spinosa leaf extract: Arganyl LSF (aqueous solution: LABORATOIRES SEROBIOLOGIQUES)
Bilberry extract: Eco Farm Bilberry Leaf E (use site, leaf: water / ethanol mixture: Ichimaru Falcos)
Oil-soluble licorice extract: Oil-soluble licorice extract PT (manufactured by Maruzen Pharmaceutical Co., Ltd.)
Sakura leaf extract: Sakura extract B (1,3-butylene glycol aqueous solution: manufactured by Ichimaru Falcos)
Novara fruit extract: Falco Rex Novara B (manufactured by Ichimaru Falcos)
Hawthorn Extract: Falco Rex Hawthorn B (manufactured by Ichimaru Falcos)
表2に示したとおり、オリーブ葉抽出物、キイチゴ果実抽出物、チョウジ花抽出物、アルガニアスピノサ葉抽出物、ビルベリー抽出物、油溶性カンゾウ抽出物、サクラ葉抽出物には優れたメチルメルカプタン発生抑制効果があることがわかった。特に、0.001質量%以上配合すると、50%以上の抑制効果が得られ、0.01質量以上配合すると、75%以上の抑制効果が得られることが判った。一方、ノバラ果実エキスやセイヨウサンザシエキスは、0.01質量%以上配合したにもかかわらず、抑制効果が全く得られないことが判った。 As shown in Table 2, excellent methyl mercaptan generation in olive leaf extract, raspberry fruit extract, clove flower extract, Arganian spinosa leaf extract, bilberry extract, oil-soluble licorice extract, and cherry leaf extract It was found that there is a suppression effect. In particular, it was found that when 0.001% by mass or more is blended, an inhibitory effect of 50% or more is obtained, and when 0.01% or more is blended, a suppressive effect of 75% or more is obtained. On the other hand, it was found that nocturnal fruit extract or hawthorn extract could not obtain any inhibitory effect despite the blending of 0.01% by mass or more.
苦味・渋味の抑制効果の評価
以下の方法に従い、メチルメルカプタン抑制剤を配合した口腔用組成物の苦味・渋味の抑制効果を評価した。
常法により製造した実施例1〜6及び比較例1を、専門パネル5名を用いて下記基準の5段階の評点による絶対評価を実施した。評価は、各被検体を10ml取り、口中に約20秒間含んだ後に吐き出し、その直後の感覚で評価した。得られた各評価点を集計し、個々の評価項目毎に評価点の平均値を算出し、結果を表3に示した。
評価点 5 : 弱く感じる
4 : やや弱く感じる
3 : どちらともいえない
2 : やや強く感じる
1 : 強く感じる
Evaluation of Bitterness / Astringency Suppression Effect According to the following method, the bitterness / astringency suppression effect of an oral composition containing a methyl mercaptan inhibitor was evaluated.
Examples 1 to 6 and Comparative Example 1 produced by a conventional method were subjected to absolute evaluation using five grades based on the following criteria using five specialist panels. For the evaluation, 10 ml of each subject was taken and contained in the mouth for about 20 seconds. The obtained evaluation points were totaled, the average value of the evaluation points was calculated for each evaluation item, and the results are shown in Table 3.
Evaluation point 5: Feel weak
4: Feel somewhat weak
3: Neither can be said
2: I feel a little stronger
1: Feel strong
表3に示したとおり、キシリトール、マルチトール、エリスリトールを、口腔用組成物全量に対して、1〜10質量%配合するとオリーブ葉エキスを配合した口腔用組成物の苦味や渋味を著しく抑制することがわかった。 As shown in Table 3, when 1 to 10% by mass of xylitol, maltitol, and erythritol is added to the total amount of the oral composition, the bitterness and astringency of the oral composition containing the olive leaf extract are remarkably suppressed. I understood it.
以下、本発明に係るメチルメルカプタン抑制剤を配合した口腔用組成物の実施例の処方を挙げるが、本発明は下記の処方に限定されるものではない。 Hereinafter, although the prescription of the Example of the composition for oral cavity which mix | blended the methyl mercaptan inhibitor which concerns on this invention is given, this invention is not limited to the following prescription.
処方例1
常法に従って、練歯磨を調製した。
成 分 配 合 量
塩化セチルピリジニウム 0.05
ポリオキシエチレン(40)硬化ヒマシ油 0.5
アルガニアスピノサ葉抽出物 0.5
研磨性シリカ 18.0
増粘性シリカ 3.0
ソルビトール 40.0
キシリトール 5.0
ポリエチレングリコール400 3.0
香料 1.0
サッカリンナトリウム 0.2
カルボキシメチルセルロースナトリウム 0.4
フッ化ナトリウム 0.2
イソプロピルメチルフェノール 0.05
pH調整剤 適 量
精製水 残 部
合 計 100
Formulation Example 1
A toothpaste was prepared according to a conventional method.
Component amount
Cetylpyridinium chloride 0.05
Polyoxyethylene (40) hydrogenated castor oil 0.5
Argania spinosa leaf extract 0.5
Abrasive silica 18.0
Thickening silica 3.0
Sorbitol 40.0
Xylitol 5.0
Polyethylene glycol 400 3.0
Fragrance 1.0
Saccharin sodium 0.2
Sodium carboxymethylcellulose 0.4
Sodium fluoride 0.2
Isopropyl methylphenol 0.05
pH adjusting agent
Purified water balance
Total 100
処方例2
常法に従って、ジェル剤を調製した。
成 分 配 合 量
ビルベリー抽出物 1.0
グリセリン 10.0
プロピレングリコール 9.0
マルチトール 1.0
ヒドロキシエチルセルロース 1.0
グリチルリチン酸ジカリウム 0.05
ポリオキシエチレン(60E.O.)硬化ヒマシ油 0.4
クエン酸 0.01
クエン酸3ナトリウム 0.1
香料 0.4
パラオキシ安息香酸メチル 0.1
スクラロース 0.02
精製水 残 部
合 計 100
Formulation example 2
A gel was prepared according to a conventional method.
Component amount
Bilberry extract 1.0
Glycerin 10.0
Propylene glycol 9.0
Maltitol 1.0
Hydroxyethyl cellulose 1.0
Dipotassium glycyrrhizinate 0.05
Polyoxyethylene (60E.O.) hydrogenated castor oil 0.4
Citric acid 0.01
Trisodium citrate 0.1
Fragrance 0.4
Methyl paraoxybenzoate 0.1
Sucralose 0.02
Purified water balance
Total 100
処方例3
常法に従って、液体歯磨を調製した。
成 分 配 合 量
アルガニアスピノサ葉抽出物 0.02
グリセリン 10.0
エタノール 10.0
キシリトール 7.0
ポリオキシエチレン(60E.O.)硬化ヒマシ油 0.4
塩化セチルピリジニウム 0.3
トラネキサム酸 0.05
クエン酸 0.01
クエン酸3ナトリウム 0.1
パラオキシ安息香酸メチル 0.1
香料 0.2
精製水 残 部
合 計 100
Formulation Example 3
A liquid dentifrice was prepared according to a conventional method.
Component amount
Argania spinosa leaf extract 0.02
Glycerin 10.0
Ethanol 10.0
Xylitol 7.0
Polyoxyethylene (60E.O.) hydrogenated castor oil 0.4
Cetylpyridinium chloride 0.3
Tranexamic acid 0.05
Citric acid 0.01
Trisodium citrate 0.1
Methyl paraoxybenzoate 0.1
Fragrance 0.2
Purified water balance
Total 100
処方例4
常法に従って、洗口液を調製した。
成 分 配 合 量
オリーブ葉抽出物 0.001
マルチトール 10.0
グリセリン 5.0
ポリオキシエチレン(60E.O.)硬化ヒマシ油 0.5
塩化セチルピリジニウム 0.1
クエン酸ナトリウム 0.1
サッカリン 0.05
香料 0.2
精製水 残 部
合 計 100
Formulation Example 4
A mouthwash was prepared according to a conventional method.
Component amount
Olive leaf extract 0.001
Maltitol 10.0
Glycerin 5.0
Polyoxyethylene (60E.O.) hydrogenated castor oil 0.5
Cetylpyridinium chloride 0.1
Sodium citrate 0.1
Saccharin 0.05
Fragrance 0.2
Purified water balance
Total 100
処方例5
常法に従って、マウススプレーを調製した。
成 分 配 合 量
オリーブ葉抽出物 1.0
エタノール 30.0
グリセリン 15.0
ポリオキシエチレン(60E.O.)硬化ヒマシ油 1.5
メントール 1.0
サッカリン 0.1
クエン酸ナトリウム 0.2
精製水 残 部
合 計 100
Formulation Example 5
A mouse spray was prepared according to a conventional method.
Component amount
Olive leaf extract 1.0
Ethanol 30.0
Glycerin 15.0
Polyoxyethylene (60E.O.) hydrogenated castor oil 1.5
Menthol 1.0
Saccharin 0.1
Sodium citrate 0.2
Purified water balance
Total 100
処方例6
常法に従って、タブレット剤を調製した。
成 分 配 合 量
パラチニット 35.0
ショ糖脂肪酸エステル 2.0
オリーブ葉抽出物 2.0
スクラロース 0.1
アセスルファムカリウム 0.05
香料 1.5
マルチトール 残 部
合 計 100
Formulation Example 6
A tablet was prepared according to a conventional method.
Component amount
Palatinit 35.0
Sucrose fatty acid ester 2.0
Olive leaf extract 2.0
Sucralose 0.1
Acesulfame potassium 0.05
Fragrance 1.5
Maltitol balance
Total 100
処方例7
常法に従って、キャンディーを調製した。
成 分 配 合 量
ビルベリー抽出物 2.0
マルチトール 10.0
アスパルテーム 0.1
香料 0.2
パラチニット 残 部
合 計 100
Formulation Example 7
Candy was prepared according to a conventional method.
Component amount
Bilberry extract 2.0
Maltitol 10.0
Aspartame 0.1
Fragrance 0.2
Palatinit rest
Total 100
処方例8
常法に従って、粒カプセル剤を調製した。
ゼラチンおよびソルビトールからなる内カプセル皮膜40重量部でカプセル内溶液60重量部を被包し、さらに糖質からなる外カプセル皮膜110重量部で糖衣することにより粒カプセルを調製した。
カプセル内溶液
成 分 配 合 量
オリーブ葉抽出物 10.0
ビタミンC 7.2
ビタミンE 2.4
グリセリン脂肪酸エステル 1.0
紅花油 残 部
合 計 60
内カプセル皮膜
成 分 配 合 量
ゼラチン 36.0
ソルビトール 残 部
合 計 40
外カプセル皮膜
成 分 配 合 量
卵殻カルシウム 1.0
アラビアガム 0.6
シェラック 0.3
ゼラチン 0.2
カルバナワックス 0.1
アスパルテーム 0.1
香料 0.4
パラチニット 残 部
合計 110
Formulation Example 8
Granule capsules were prepared according to a conventional method.
Granule capsules were prepared by encapsulating 60 parts by weight of the solution in the capsule with 40 parts by weight of the inner capsule film made of gelatin and sorbitol, and sugar coating with 110 parts by weight of the outer capsule film made of sugar.
Solution in capsule
Component amount
Olive leaf extract 10.0
Vitamin C 7.2
Vitamin E 2.4
Glycerin fatty acid ester 1.0
Safflower oil balance
Total 60
Inner capsule film
Component amount
Gelatin 36.0
Sorbitol balance
Total 40
Outer capsule coating
Component amount
Eggshell calcium 1.0
Gum arabic 0.6
Shellac 0.3
Gelatin 0.2
Carbana wax 0.1
Aspartame 0.1
Fragrance 0.4
Palatinit rest
Total 110
処方例9
常法に従って、口腔用パスタ剤を調製した。
成 分 配 合 量
グリセリン 20.0
流動パラフィン 11.0
セタノール 9.0
ポリオキシエチレンソルビタンモノステアレート 4.0
塩化セチルトリメチルアンモニウム 2.0
レシチン 2.0
ソルビタンモノパルミテート 1.0
ニコチン酸トコフェロール 1.0
ビルベリー抽出物 1.0
ラウリル硫酸ナトリウム 0.3
塩化ベンゼトニウム 0.2
塩化セチルベンゼトニウム 0.1
サリチル酸メチル 0.15
塩化セチルピリジニウム 0.05
サッカリン 0.05
香料 0.3
精製水 残 部
合 計 100
Formulation Example 9
An oral pasta preparation was prepared according to a conventional method.
Component amount
Glycerin 20.0
Liquid paraffin 11.0
Cetanol 9.0
Polyoxyethylene sorbitan monostearate 4.0
Cetyltrimethylammonium chloride 2.0
Lecithin 2.0
Sorbitan monopalmitate 1.0
Tocopherol nicotinate 1.0
Bilberry extract 1.0
Sodium lauryl sulfate 0.3
Benzethonium chloride 0.2
Cetylbenzethonium chloride 0.1
Methyl salicylate 0.15
Cetylpyridinium chloride 0.05
Saccharin 0.05
Fragrance 0.3
Purified water balance
Total 100
処方例10
常法に従って、チューイングガムを調製した。
成 分 配 合 量
キシリトール 58.0
マルチトール 8.0
炭酸カルシウム 7.0
香料 3.0
アルガニアスピノサ葉抽出物 1.0
ガムベース 残 部
合 計 100
Formulation Example 10
Chewing gum was prepared according to a conventional method.
Component amount
Xylitol 58.0
Maltitol 8.0
Calcium carbonate 7.0
Fragrance 3.0
Argania spinosa leaf extract 1.0
The rest of the gum base
Total 100
処方例11
常法に従って、チュアブルタブレットを調製した。
成 分 配 合 量
ビルベリー抽出物 2.0
アラビアガム 1.2
ショ糖脂肪酸エステル 1.8
香料 3.0
パラチニット 残 部
合 計 100
Formulation Example 11
Chewable tablets were prepared according to a conventional method.
Component amount
Bilberry extract 2.0
Gum arabic 1.2
Sucrose fatty acid ester 1.8
Fragrance 3.0
Palatinit rest
Total 100
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JP2013163648A (en) * | 2012-02-09 | 2013-08-22 | Arimino Kagaku Kk | Deodorant for hair reshaping treatment |
JP2015044773A (en) * | 2013-08-29 | 2015-03-12 | 一丸ファルコス株式会社 | Preventing and improving agent for skin aging caused by blue light irradiation |
WO2015125822A1 (en) * | 2014-02-20 | 2015-08-27 | ライオン株式会社 | Oral biofilm calcification inhibitor and oral composition |
JP2016023142A (en) * | 2014-07-16 | 2016-02-08 | 株式会社ロッテ | Bad breath inhibitor |
CN110691583A (en) * | 2017-05-31 | 2020-01-14 | 狮王株式会社 | Oral composition |
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