JP5382052B2 - Bad breath odor suppressor and oral composition for suppressing bad breath - Google Patents
Bad breath odor suppressor and oral composition for suppressing bad breath Download PDFInfo
- Publication number
- JP5382052B2 JP5382052B2 JP2011090672A JP2011090672A JP5382052B2 JP 5382052 B2 JP5382052 B2 JP 5382052B2 JP 2011090672 A JP2011090672 A JP 2011090672A JP 2011090672 A JP2011090672 A JP 2011090672A JP 5382052 B2 JP5382052 B2 JP 5382052B2
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- bad breath
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- oral
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Landscapes
- Cosmetics (AREA)
Description
本発明は、口臭予防及び抑制効果が高く、しかもその効果の持続性が向上した口臭抑制剤及びこれを配合した口臭抑制用口腔内組成物に関する。 TECHNICAL FIELD The present invention relates to a bad breath suppressant having a high bad breath prevention and suppressing effect and having improved durability and an oral composition for suppressing bad breath containing the same.
口臭は、口腔の汚れ(食物残さ、剥離粘膜など)が口臭の原因菌により分解されて発生するメチルメルカプタンや硫化水素等である。従来の口臭予防は、(1)メチルメルカプタンを捕捉・消臭、(2)口臭原因菌の除去、(3)口臭原因菌の悪臭発生に働く酵素の阻害(菌代謝阻害)、(4)唾液分泌亢進することによる汚れの除去等の方法が各々あった。しかし、(1)においては速効性があるものの持続しなく、(2)においては菌を殺してしまうために口腔内菌叢を乱すことがあり、また、(3)においては持続性はあるものの、発生してしまった口臭については効果がなく、(4)においては唾液で汚れを流した後に発生する口臭に効果がない等、効果の面で不十分なものであった。
なお、本発明に関連する先行文献としては下記のものが挙げられる。
The bad breath is methyl mercaptan, hydrogen sulfide, or the like generated by decomposing oral dirt (food residue, exfoliated mucous membrane, etc.) by the bacteria that cause bad breath. Conventional bad breath prevention includes (1) capture and deodorization of methyl mercaptan, (2) removal of bad breath causing bacteria, (3) inhibition of enzymes that cause malodor of bad breath causing bacteria (bacterial metabolism inhibition), (4) saliva There were methods such as removal of dirt by increasing secretion. However, in (1), it is fast-acting but does not last. In (2), it kills the bacteria, which may disturb the oral flora, but in (3) it is persistent. The bad breath that has occurred is ineffective, and in (4), the bad breath that is generated after pouring dirt with saliva is not effective.
In addition, the following are mentioned as prior literature relevant to the present invention.
本発明は、口臭予防効果、口臭抑制効果に優れ、しかもその効果の持続性の高い口臭抑制剤及び口臭抑制用口腔内組成物を提供することを目的とする。 An object of the present invention is to provide a halitosis inhibitor and an oral composition for suppressing halitosis, which are excellent in halitosis prevention effect and halitosis suppression effect and have a long-lasting effect.
本発明者らは、上記目的を達成するため鋭意検討を行った結果、シソ科植物又はその抽出物にミカン科植物又はその抽出物、特にミカン科サンショウ属植物の種子又はその抽出物を併用することにより、口臭抑制効果が顕著に増大し、かつ口腔内適用後においてその口臭抑制効果が良好に発揮され、速効性及び持続性を向上させることができることを知見した。更に、アオギリ科コーラの植物又はその抽出物や、ウリ科羅漢果の植物又はその抽出物、メントール又はその誘導体、甘味剤、香料のうち1種又は2種以上を配合することにより、香味が良好な口腔内組成物、特に口腔内貼付剤が得られることを見出し、本発明をなすに至った。 As a result of intensive studies to achieve the above-mentioned object, the present inventors have combined use of a citrus plant or an extract thereof with a citrus plant or an extract thereof, in particular, a seed of the citrus family Salamander or an extract thereof. As a result, it has been found that the bad breath suppressing effect is remarkably increased, and that the bad breath suppressing effect can be satisfactorily exhibited after application in the oral cavity, thereby improving the rapid efficacy and sustainability. Furthermore, a flavor is good by mix | blending 1 type (s) or 2 or more types among the plant of Coriaceae cola or its extract, the plant of the cucurbitaceae rosaceae fruit or its extract, menthol or its derivative, a sweetener, and a fragrance | flavor. It has been found that an intraoral composition, particularly an intraoral patch, can be obtained, and the present invention has been made.
即ち、本発明は下記の口臭抑制剤及び口臭抑制用口腔内組成物を提供する。
[1]. (A)ローズマリー、セージ、タイム、メリッサ、シソから選ばれるシソ科の植物又はその抽出物と、(B)サンショウの種子又はその抽出物とからなり、前記(A)成分と(B)成分との配合比が質量比として1:100〜100:1である口臭抑制剤。
[2].(B)成分が、サンショウの種子を原料とし、粉砕して粉状にしたもの、又はこれを極性溶媒及び/又は非極性溶媒で抽出した抽出物である[1]に記載の口臭抑制剤。
[3].(B)成分が、非水溶性画分を含有する抽出物である[1]又は[2]に記載の口臭抑制剤。
[4].[1]〜[3]のいずれかに記載の口臭抑制剤を配合してなることを特徴とする口臭抑制用口腔内組成物(但し、口腔内貼付剤を除く)。
[5].(A)成分の含有量が0.01〜10質量%、(B)成分の含有量が0.01〜10質量%である[4]に記載の口臭抑制用口腔内組成物。
[6].更に、(C)成分として、アオギリ科コーラからなる植物及びその抽出物、ウリ科羅漢果からなる植物及びその抽出物から選ばれる1種又は2種以上を配合した[4]又は[5]に記載の口臭抑制用口腔内組成物。
[7].更に、トコトリエノール及び/又はラッカーゼを配合した[4]〜[6]のいずれかに記載の口臭抑制用口腔内組成物。
[8].更に、(D)成分として、メントール又はその誘導体を配合した[4]〜[7]のいずれかに記載の口臭抑制用口腔内組成物。
[9].歯磨剤、洗口剤、歯肉マッサージクリーム、口腔用軟膏、うがい用錠剤、トローチ、フィルム剤、チュアブル錠、キャンディ、チューインガム、チョコレート剤、ゲル剤から選ばれる製剤に調製された[4]〜[8]のいずれかに記載の口臭抑制用口腔内組成物。
That is, this invention provides the following bad breath inhibitor and the intraoral composition for bad breath suppression.
[1]. (A) A plant of Lamiaceae selected from rosemary, sage, thyme , melissa, perilla or an extract thereof, and (B) a salamander seed or an extract thereof, wherein (A) component and (B) Bad breath odor inhibitor whose compounding ratio with a component is 1: 100-100: 1 as mass ratio.
[2]. (B) The malodor control agent according to [1], wherein the component is an extract obtained by pulverizing powder from a salamander seed or a polar solvent and / or a nonpolar solvent. .
[3]. (B) The bad breath suppressant according to [1] or [2], wherein the component is an extract containing a water-insoluble fraction.
[4]. An oral composition for suppressing bad breath, comprising the bad breath suppressant according to any one of [1] to [3] (excluding an oral patch).
[5]. The oral cavity composition for bad breath suppression according to [4], wherein the content of the component (A) is 0.01 to 10% by mass and the content of the component (B) is 0.01 to 10% by mass.
[6]. Furthermore, as (C) component, 1 type or 2 or more types chosen from the plant which consists of a Coriaceae cola, and its extract, the plant which consists of Cucurbitaceae, and its extract are described in [4] or [5] An oral composition for suppressing bad breath.
[7]. Furthermore, the oral cavity composition for bad breath suppression in any one of [4]-[6] which mix | blended tocotrienol and / or laccase.
[8]. Furthermore, the oral cavity composition for bad breath suppression in any one of [4]-[7] which mix | blended menthol or its derivative (s) as (D) component.
[9]. [4] to [8] prepared to a formulation selected from dentifrice, mouthwash, gingival massage cream, oral ointment, gargle tablet, troche, film, chewable tablet, candy, chewing gum, chocolate and gel. ] The oral cavity composition for bad breath suppression in any one of.
本発明によれば、シソ科植物又はその抽出物による口臭捕捉と、ミカン科サンショウ属植物の種子又はその抽出物による口臭原因菌代謝阻害の併用効果が得られ、口臭抑制効果が高く、しかも速効性と持続性に優れたものである。更に、アオギリ科コーラの植物又はその抽出物、メントール又はその誘導体、甘味剤、香料のうち1種又は2種以上を配合することにより、味を改善した口臭予防製剤を提供することができる。 According to the present invention, it is possible to obtain a combined effect of catching bad breath by a Labiatae plant or an extract thereof and inhibiting the metabolism of bad breath causing bacteria by the seeds of the Citrus Salamander plant or an extract thereof, and having a high bad breath suppressing effect, It has excellent rapidity and sustainability. Furthermore, the bad breath prevention preparation which improved the taste can be provided by mix | blending 1 type (s) or 2 or more types among the plant of Aogiri family cola, its extract, menthol or its derivative (s), a sweetener, and a fragrance | flavor.
本発明において用いられる(A)成分のシソ科植物又はその抽出物としては、従来より公知のものが使用でき、例えば、セージ、ローズマリー、タイム、メリッサ、シソの葉及び茎を原料とし、粉砕して粉状にしたものが使用でき、またその抽出物としては、上記粉状のシソ科植物、これを極性溶媒及び/又は非極性溶媒(例えば、水、エチルエーテル、エチレンクロライド、ジオキサン、アセトン、エタノール、メタノール、酢酸エチル、プロピレングリコール等の極性溶媒、あるいはn−ヘキサン、石油エーテル、リグロイン、シクロヘキサン、四塩化炭素、クロロホルム、ジクロルメタン、1,2−ジクロルエタン、トルエン、ベンゼン等の非極性溶媒、又はこれらの混合溶媒)で抽出することにより得られた抽出エキス及びその抽出残渣から選ばれる原料に対し溶媒抽出処理を行って得られた抽出物、並びに上記植物より単離されるカルノソール、カルノジン酸、7,11,12−トリヒドロキシ−6,10−(エポキシメタノ)アビエタ−8,11,13−トリエン−20−オン(ロズマノール)、及びこれらの塩等の消臭有効成分(特開昭57−203445号公報,特開昭57−204278号公報,特開昭59−103665号公報参照)である。これらのうち好ましいのは、セージ、ローズマリー、タイム、メリッサ、シソ及びこれらの抽出物である。なお、上記溶媒抽出処理に用いる溶媒は、上記公報に記載されているように、有機溶媒でも無機溶媒でも差し支えなく、また有機溶媒と無機溶媒との混合溶媒でもよい。有機溶媒の具体例としては、エチルエーテル、エチレンクロライド、ジオキサン、アセトン、エタノール、メタノール、酢酸エチル、プロピレングリコール、n−ヘキサン、石油エーテル、リグロイン、シクロヘキサン、四塩化炭素、クロロホルム、ジクロルメタン、1,2−ジクロルエタン、トルエン、ベンゼン等が挙げられる。また、無機溶媒としては水、それに酸、アルカリ又はこれらの塩の水溶液が使用でき、具体的には塩酸、硫酸、リン酸、硝酸、炭酸、水酸化ナトリウム、水酸化カリウム、水酸化アンモニウム、水酸化カルシウム、塩化ナトリウム、塩化カリウム、塩化アンモニウム、炭酸水素ナトリウム、炭酸ナトリウム、硫酸ナトリウム等が挙げられる。なお、これら酸、アルカリ、塩は2モル以下の濃度で使用することが好ましい。好ましい溶媒は、水、炭素数1〜3の低級アルコール、多価アルコールである。また、以上に挙げた溶媒の使用量は、原料に対し等容量以上とすることが好ましい。 As the Lamiaceae plant of component (A) used in the present invention or an extract thereof, conventionally known ones can be used. For example, sage, rosemary, thyme , melissa, perilla leaves and stems are used as raw materials and pulverized. The powdered Lamiaceae plant, which is a polar solvent and / or a nonpolar solvent (for example, water, ethyl ether, ethylene chloride, dioxane, acetone) can be used. , Polar solvents such as ethanol, methanol, ethyl acetate, propylene glycol, or nonpolar solvents such as n-hexane, petroleum ether, ligroin, cyclohexane, carbon tetrachloride, chloroform, dichloromethane, 1,2-dichloroethane, toluene, benzene, Or an extract obtained by extraction with a mixed solvent thereof) and its extraction Extract obtained by subjecting raw material selected from residue to solvent extraction, as well as carnosol, carnosic acid, 7,11,12-trihydroxy-6,10- (epoxymethano) abieter isolated from the above plant Deodorizing active ingredients such as 8,11,13-trien-20-one (Rosmanol) and their salts (Japanese Patent Laid-Open Nos. 57-203445, 57-204278, 59-103665) No. gazette). Of these, sage, rosemary, thyme , melissa, perilla and extracts thereof are preferred. The solvent used in the solvent extraction treatment may be an organic solvent or an inorganic solvent as described in the above publication, or may be a mixed solvent of an organic solvent and an inorganic solvent. Specific examples of the organic solvent include ethyl ether, ethylene chloride, dioxane, acetone, ethanol, methanol, ethyl acetate, propylene glycol, n-hexane, petroleum ether, ligroin, cyclohexane, carbon tetrachloride, chloroform, dichloromethane, 1,2 -Dichloroethane, toluene, benzene and the like. As the inorganic solvent, water, and an aqueous solution of acid, alkali or a salt thereof can be used. Specifically, hydrochloric acid, sulfuric acid, phosphoric acid, nitric acid, carbonic acid, sodium hydroxide, potassium hydroxide, ammonium hydroxide, water Examples include calcium oxide, sodium chloride, potassium chloride, ammonium chloride, sodium bicarbonate, sodium carbonate, sodium sulfate and the like. These acids, alkalis and salts are preferably used at a concentration of 2 mol or less. Preferred solvents are water, lower alcohols having 1 to 3 carbon atoms, and polyhydric alcohols. Moreover, it is preferable that the usage-amount of the solvent quoted above shall be equal capacity or more with respect to a raw material.
(B)成分のサンショウの種子又はその抽出物としては、ミカン科サンショウ属(Zanthoxylum)植物の種子を原料とし、粉砕して粉状にしたもの、又はこれを極性溶媒及び/又は非極性溶媒で抽出した抽出物である。特に非水溶性画分を含有する抽出物、又は2,6−ジメチル−3,7−オクタジエン−2,6−ジオール、2,6−ジメチル−1,7−オクタジエン−3,6−ジオール、3−アセトキシ−1−p−メンテン、8−アセトアミノ−1−p−メンテン、11−ハイドロキシ−8−オイデスメン、炭素数16以上の不飽和脂肪酸、炭素数6以上の不飽和アルデヒドのいずれか1種以上を有効成分とするものが好ましい。 Component (B), salamander seed or extract thereof, is made from seeds of Zanthoxylum plants, pulverized into powder, or a polar solvent and / or nonpolar An extract extracted with a solvent. In particular, an extract containing a water-insoluble fraction, or 2,6-dimethyl-3,7-octadiene-2,6-diol, 2,6-dimethyl-1,7-octadiene-3,6-diol, -Acetoxy-1-p-mentene, 8-acetamino-1-p-mentene, 11-hydroxy-8-eudesmen, unsaturated fatty acid having 16 or more carbon atoms, unsaturated aldehyde having 6 or more carbon atoms Those containing as an active ingredient are preferred.
この場合、上記溶媒としては、水、エチルエーテル、エチレンクロライド、ジオキサン、アセトン、エタノール、メタノール、酢酸エチル、プロピレングリコール等の極性溶媒、あるいはn−ヘキサン、石油エーテル、リグロイン、シクロヘキサン、四塩化炭素、クロロホルム、ジクロルメタン、1,2−ジクロルエタン、トルエン、ベンゼン等の非極性溶媒、又はこれらの混合溶媒が挙げられ、上記原料を通常の抽出法で抽出することによって得られる抽出物を使用することができる。 In this case, as the solvent, polar solvents such as water, ethyl ether, ethylene chloride, dioxane, acetone, ethanol, methanol, ethyl acetate, propylene glycol, or n-hexane, petroleum ether, ligroin, cyclohexane, carbon tetrachloride, Nonpolar solvents such as chloroform, dichloromethane, 1,2-dichloroethane, toluene, and benzene, or a mixed solvent thereof can be used, and an extract obtained by extracting the above raw materials by a usual extraction method can be used. .
なお、非水溶性画分を含む抽出物の場合、特開2003−26527号公報に記載されているように、溶媒としては、メタノール、エタノール、ブタノール、ヘキサン、ヘプタン、シクロヘキサン、酢酸エチル、アセトンなどの一般に用いられる有機溶媒などを挙げることができ、これらの1種を単独で又は2種以上を混合して、また、水溶性溶媒の場合、含水溶媒として使用することができる。これらの溶媒の中では、特にメタノール、エタノール、含水アルコールなどが好ましく、中でも水を10〜50%含有する含水エタノール溶液が特に好適である。なお、抽出処理は、通常、3〜70℃程度の温度で常法によって行うことができる。 In the case of an extract containing a water-insoluble fraction, as described in JP-A No. 2003-26527, as a solvent, methanol, ethanol, butanol, hexane, heptane, cyclohexane, ethyl acetate, acetone, etc. In general, the organic solvent can be used, and one of these can be used alone or in admixture of two or more, and in the case of a water-soluble solvent, it can be used as a hydrous solvent. Among these solvents, methanol, ethanol, hydrous alcohol and the like are particularly preferable, and hydrous ethanol solution containing 10 to 50% of water is particularly preferable. In addition, extraction processing can be normally performed at a temperature of about 3-70 degreeC by a conventional method.
上記(A),(B)成分を口腔内組成物に配合する場合には、それぞれの配合量は組成物全体の0.001〜50%(質量%、以下同様)、特に0.01〜10%とすることが好ましく、これに満たないと満足な効果が発揮されない場合があり、50%を超えると組成物の安定性又は香味を損なう場合がある。また、(A)成分と(B)成分の配合比は質量比として1:100〜100:1とするもので、これに満たないと満足な併用効果が発揮されない。また、これらの植物及びその抽出物のうち、好ましい配合の組合せは、ローズマリー及びサンショウの植物又はその抽出物、セージ及びサンショウの植物又はその抽出物、メリッサ及びサンショウの植物又はその抽出物、タイム及びサンショウの植物又はその抽出物であり、特に好ましいのはローズマリー及びサンショウの植物又はその抽出物、セージ及びサンショウの植物又はその抽出物である。 When the components (A) and (B) are blended in the oral composition, the blending amount is 0.001 to 50% (mass%, the same applies hereinafter) of the whole composition, particularly 0.01 to 10%. If it is less than this, a satisfactory effect may not be exhibited, and if it exceeds 50%, the stability or flavor of the composition may be impaired. The proportion of the component (A) and component (B) in the weight ratio 1: 100 to 100: in which the 1, when less than this satisfactory combined effect is not such to exhibit. Among these plants and extracts thereof, preferred combinations of combinations are rosemary and salamander plants or extracts thereof, sage and salamander plants or extracts thereof, Melissa and salamander plants or extracts thereof. , Thyme and salamander plants or extracts thereof, particularly preferred are rosemary and salamander plants or extracts thereof, sage and salamander plants or extracts thereof.
更に、本発明の口腔内組成物には、アオギリ科コーラ及びウリ科羅漢果の植物及びこれらの抽出物から選ばれる1種又は2種以上を配合し得、この配合により唾液分泌を亢進し、口中に残る不快な味を改善するという効果を与えることができる。ここで、アオギリ科コーラの植物又は抽出物としては、コーラノキ種子を原料とし、コラ・アクミナータ(学名:Cola acuminata)及びコラ・ニティダ(学名:Cola nitida A.Chev.)と呼ばれるコーラノキに属する木より採取される種子を粉砕して粉状にしたもの、又はこれの抽出物である。また、ウリ科羅漢果の植物又は抽出物としては、学名:Momordica grosvenori Swingleの果実を原料とし、そのチップ、粉末あるいはそれを溶媒で抽出することにより得られる抽出物を利用できる。なお、溶媒としては、上記シソ科植物やサンショウの種子の抽出物の調製で例示した溶媒が挙げられる。それぞれの配合量は組成物全体の0.001〜50%、特に0.01〜10%とすることが好ましく、これに満たないと満足な効果が発揮されない場合があり、50%を超えると組成物の安定性又は香味を損なう場合がある。 Furthermore, the oral composition of the present invention can be blended with one or more selected from the plant of Coriaceae cola and cucurbitaceae and their extracts, and this formulation enhances salivation, The effect of improving the unpleasant taste that remains can be given. Here, as a plant or an extract of Coleaceae cola, a cola tree seed is used as a raw material, and it is from a tree belonging to cola tree called Kola acuminata (scientific name: Cola acminata) and Kola nitida (scientific name: Cola nitida A. Chev.). The seeds to be collected are pulverized and powdered, or an extract thereof. In addition, as a plant or extract of the cucurbitaceae rosaceae fruit, a fruit of scientific name: Mormodica grosvenori Swingle is used as a raw material, and its chip, powder, or an extract obtained by extracting it with a solvent can be used. In addition, as a solvent, the solvent illustrated by the preparation of the extract of the said Lamiaceae plant and a salamander seed is mentioned. Each blending amount is preferably 0.001 to 50% of the entire composition, particularly preferably 0.01 to 10%. If less than this, a satisfactory effect may not be exhibited. The stability or flavor of the product may be impaired.
これらのコ−ラ、羅漢果又はこれらの抽出物を添加する場合、好ましい配合の組合せは、ローズマリー及びサンショウ並びにコラエの植物又はその抽出物、セージ及びサンショウ並びにコラエの植物又はその抽出物、メリッサ及びサンショウ並びにコラエの植物又はその抽出物、タイム及びサンショウ並びにコラエの植物又はその抽出物、ローズマリー及びサンショウ並びに羅漢果の植物又はその抽出物、セージ及びサンショウ並びに羅漢果の植物又はその抽出物、メリッサ及びサンショウ並びに羅漢果の植物又はその抽出物、タイム及びサンショウ並びに羅漢果の植物又はその抽出物、ローズマリー及びサンショウ並びにコラエの植物又はその抽出物、セージ及びサンショウ並びにコラエの植物又はその抽出物、ローズマリー及びサンショウ並びに羅漢果の植物又はその抽出物である。 When these colas, rahan fruit or extracts thereof are added, preferred combinations of combinations are rosemary and salamander and corae plants or extracts thereof, sage and salamander and corae plants or extracts thereof, Melissa and Salamander and Collae plant or extract thereof, Thyme and Salamander and Collae plant or extract thereof, Rosemary and Salamander and Luhan fruit plant or extract thereof, Sage and Salamander and Luhan fruit plant or its Extracts, Melissa and Salamander and Rakan fruit plants or extracts thereof, Thyme and Salamander and Rahan fruit plants or extracts thereof, Rosemary and Salamander and Collae plants or extracts thereof, Sage and Salamander and Collae Plants or extracts thereof, rosemary and sansho As well as plant or an extract thereof Lo Han Guo.
本発明の口腔内組成物には、更にトコトリエノール及び/又はラッカーゼを配合することができ、これら成分の配合により更に高い口臭抑制効果を与えることができる。この場合、トコトリエノールの配合量は、組成物中0.001〜10%、特に0.01〜5%であることが好ましく、またラッカーゼの配合量は組成物中0.0005〜1%、特に0.001〜0.5%であることが好ましい。 The intraoral composition of the present invention can further contain tocotrienol and / or laccase, and can give a higher bad breath suppressing effect by blending these components. In this case, the amount of tocotrienol is preferably 0.001 to 10%, particularly 0.01 to 5% in the composition, and the amount of laccase is 0.0005 to 1%, particularly 0, in the composition. 0.001 to 0.5% is preferable.
本発明の口腔内組成物には、上記成分に加えて(D)成分としてメントール又はその誘導体を配合することができ、(E)成分として甘味剤、(F)成分として香料を配合することができる。 In the oral cavity composition of the present invention, menthol or a derivative thereof can be blended as the component (D) in addition to the above components, and a sweetener can be blended as the component (E) and a fragrance can be blended as the component (F). it can.
この場合、メントール又はメントール誘導体としては、植物等の精油から単離したものでも、化学的に合成されたものでもよく、また、メントールを含有するミント油等の精油をそのまま用いてもよい。ミント油としては、ハッカ油、ペパーミント油、スペアミント油等が挙げられ、1種以上を用いることができ、上記単離又は合成メントールと組合せて用いてもよい。メントール誘導体としては、l−イソプレゴール、l−メチルグリセリルエーテル、p−メンタン−3,8−ジオール等が挙げられ、そのうちl−イソプレゴールが好ましい。配合量は組成物全体の0.0001〜50%、好ましくは0.0005〜20%、更に好ましくは0.001〜10%とすることが好ましく、これに満たないと満足な効果が発揮されない場合があり、50%を超えると組成物の安定性又は香味を損なう場合がある。 In this case, the menthol or menthol derivative may be isolated from an essential oil such as a plant or chemically synthesized, or an essential oil such as mint oil containing menthol may be used as it is. Examples of mint oil include peppermint oil, peppermint oil, spearmint oil and the like, and one or more kinds can be used, and they may be used in combination with the above-mentioned isolated or synthetic menthol. Examples of the menthol derivative include l-isopulegol, l-methylglyceryl ether, p-menthane-3,8-diol, etc. Among them, l-isopulegol is preferable. The blending amount is 0.0001 to 50% of the entire composition, preferably 0.0005 to 20%, more preferably 0.001 to 10%. If the amount is less than this, a satisfactory effect is not exhibited. If it exceeds 50%, the stability or flavor of the composition may be impaired.
上記甘味剤としては、例えば、ショ糖、果糖、ブドウ糖、乳糖、還元麦芽糖水アメ、粉末還元麦芽糖水アメ、ブドウ糖果糖液糖、果糖ブドウ糖液糖、ハチミツ、ソルビトール、マルチトール、マンニトール、キシリトール、エリスリトール、アスパルテーム、サッカリン、及び、サッカリンナトリウムから選ばれる少なくとも1種を含有するのが好ましく、ショ糖、果糖、粉末還元麦芽糖水アメ、キシリトール、及び、エリスリトールから選ばれる少なくとも1種を含有するのがより好ましく、これらの中でも、風味の点で、ショ糖を含有するのが特に好ましく、還元糖の含有率が0.05%未満であるショ糖を含有するのが、風味が特に改善される点で最も好ましい。上記甘味剤の配合量は、組成物全体の0.001〜50%、特に0.01〜20%であることが好ましい。 Examples of the sweetener include sucrose, fructose, glucose, lactose, reduced maltose water candy, powdered reduced maltose water candy, glucose fructose liquid sugar, fructose glucose liquid sugar, honey, sorbitol, maltitol, mannitol, xylitol, erythritol. It preferably contains at least one selected from aspartame, saccharin and sodium saccharin, and more preferably contains at least one selected from sucrose, fructose, powdered reduced maltose water candy, xylitol, and erythritol. Among these, sucrose is particularly preferable in terms of flavor, and sucrose having a reducing sugar content of less than 0.05% is most preferable in that the flavor is particularly improved. preferable. The blending amount of the sweetening agent is preferably 0.001 to 50%, particularly 0.01 to 20% of the entire composition.
上記香料としては、(D)成分のメントール及びメントール誘導体以外の香料、特に歯磨、洗口剤、口中清涼剤、チューインガム等の口腔製品分野で通常用いられる香料成分を適宜選択して用いることができる。例えば、天然香料として、マスティック油、パセリ油、アニス油、ユーカリ油、ウィンターグリーン油、カシア油、レモン油、オレンジ油、カルダモン油、コリアンダー油、マンダリン油、ライム油、ラベンダー油、ローレル油、カモミル油、キャラウェイ油、ベイ油、レモングラス油、パインニードル油、ネロリ油、ローズ油、ジャスミン油、イリスコンクリート、アブソリュートペパーミント、アブソリュートローズ、オレンジフラワー等が挙げられる。 As said fragrance | flavor, fragrance | flavors other than the menthol and menthol derivative of (D) component, especially the fragrance | flavor component normally used in oral product field | areas, such as a toothpaste, a mouthwash, a mouth freshener, and a chewing gum, can be selected suitably and can be used. . For example, natural flavors include mastic oil, parsley oil, anise oil, eucalyptus oil, winter green oil, cassia oil, lemon oil, orange oil, cardamom oil, coriander oil, mandarin oil, lime oil, lavender oil, laurel oil, Examples include camomile oil, caraway oil, bay oil, lemongrass oil, pine needle oil, neroli oil, rose oil, jasmine oil, iris concrete, absolute peppermint, absolute rose, and orange flower.
単品香料としては、カルボン、アネトール、サリチル酸メチル、シンナミックアルデヒド、リナロール、リナリールアセテート、リモネン、メントン、メンチルアセテート、ピネン、オクチルアルデヒド、シトラール、プレゴン、カルビールアセテート、アニスアルデヒド、更に、エチルアセテート、エチルブチレート、アリルシクロヘキサンプロピオネート、メチルアンスラニレート、エチルメチルアンスラニレート、バニリン、ウンデカラクトン、ヘキサナール、エチノンアルコール、プロピルアルコール、ブタノール、イソアミルアルコール、ヘキセノール、ジメチルサルファイド、シクロテン、フルフラールトリメチルピラジン、エチルラクテート、エチルチオアセテート等が挙げられる。単品香料及び/又は天然香料も含む調合香料として、ストロベリーフレーバー、アップルフレーバー、バナナフレーバー、パイナップルフレーバー、グレープフレーバー、マンゴーフレーバー、トロピカルフルーツフレーバー、バターフレーバー、ミルクフレーバー、フルーツミックスフレーバー等が挙げられる。また、香料の形態は、精油、抽出物、固形物、又はこれらを噴霧乾燥した粉体でも構わない。 Single flavors include carvone, anethole, methyl salicylate, cinnamic aldehyde, linalool, linalyl acetate, limonene, menthone, menthyl acetate, pinene, octyl aldehyde, citral, pregon, carbyl acetate, anisaldehyde, ethyl acetate, Ethyl butyrate, allyl cyclohexane propionate, methyl anthranilate, ethyl methyl anthranilate, vanillin, undecalactone, hexanal, ethinone alcohol, propyl alcohol, butanol, isoamyl alcohol, hexenol, dimethyl sulfide, cycloten, furfural trimethyl Examples include pyrazine, ethyl lactate, and ethyl thioacetate. Examples of blended fragrances including single fragrances and / or natural fragrances include strawberry flavor, apple flavor, banana flavor, pineapple flavor, grape flavor, mango flavor, tropical fruit flavor, butter flavor, milk flavor, fruit mix flavor and the like. Moreover, the form of a fragrance | flavor may be an essential oil, an extract, a solid substance, or the powder which spray-dried these.
配合量は組成物全体の0.0001〜50%、特に0.001〜10%とすることが好ましく、これに満たないと満足な効果が発揮されない場合があり、50%を超えると組成物の香味を損なう場合がある。 The blending amount is preferably 0.0001 to 50% of the entire composition, particularly preferably 0.001 to 10%. If less than this, a satisfactory effect may not be exhibited. The flavor may be impaired.
本発明の口腔内組成物は、歯磨類(練歯磨、粉歯磨、水歯磨、マウスウォッシュ等)、洗口剤、歯肉マッサージクリーム、口腔用軟膏、うがい用錠剤、トローチ、フィルム剤、チュアブル錠、キャンディ、チューインガム、チョコレート剤、ゲル剤などとして調製でき、その種類、剤型に応じ、上記必須成分に加えて任意成分としてその他の公知の添加剤を配合し、常法に準じて調製することができる。好ましくは、本発明はフィルム剤、特に粘膜に貼付する口腔内貼付剤とすることが好適である。即ち、本組成は、口腔内粘膜に一定時間貼付しても薬物などの刺激が少なく、苦味も抑制されるため、口腔内貼付剤として好適である。 The oral composition of the present invention includes dentifrices (toothpaste, powder toothpaste, water toothpaste, mouthwash, etc.), mouthwash, gum massage cream, oral ointment, gargle tablet, troche, film agent, chewable tablet, Can be prepared as candy, chewing gum, chocolate agent, gel agent, etc., according to its type and dosage form, other known additives can be blended as optional components in addition to the above essential components, and prepared according to conventional methods it can. Preferably, the present invention is suitably a film agent, particularly an intraoral patch to be applied to the mucous membrane. That is, this composition is suitable as an intraoral patch because it is less irritating to drugs and the bitterness is suppressed even if it is applied to the oral mucosa for a certain period of time.
口腔内貼付剤などのフィルム剤の場合には、フィルム形成能を有し、可食性であるものを使用し、合成高分子物質、例えば、ポリビニルピロリドン(以下“PVP”と記す)、カルボキシビニルポリマー(以下“CVP”と記す)、ポリビニルアルコール(以下“PVA”と記す)など;セルロース誘導体、例えば、ヒドロキシプロピルメチルセルロース(以下“HPMC”と記す)、ヒドロキシプロピルセルロース(以下“HPC”と記す)、ヒドロキシエチルセルロース(以下“HEC”と記す)、メチルセルロース(以下“MC”と記す)、エチルセルロース(以下“EC”と記す)など;天然物より得られる高分子物質、例えばアルギン酸ソーダ、デキストラン、カゼイン、プルラン、ペクチン、アラビアゴム、カラヤガム、デンプンなどを挙げることができる。特に好ましいのはPVP、HPC、デンプン、ローカストビーンガム、カラギーナン、ジェランガムである。これらの物質は単独であるいは2種以上の組み合わせで使用することができる。配合量は全体でフィルムの乾質量の20〜90%、好適には25〜80%である。更に、上記高分子物質に加えて可塑剤を配合することができる。可塑剤としては、上記高分子物質と相溶性があり、これを軟化させる化合物が用いられ、例えば、グリセリン、ジグリセリン、トリグリセリン、ポリグリセリン、ソルビトール、マルチトール、キシリトール、ポリエチレングリコール、プロピレングリコール、ブチレングリコール、ヘキシレングリコール、ペンチレングリコール、ポリオキシエチレンポリオキシプロピレングリコール、アセチルエタノールアミン等が例示されるが、特にプロピレングリコール、グリセリン、ソルビトール、キシリトール、ポリエチレングリコールが好ましい。可塑剤の添加量はフィルムの乾質量の1〜30%であり、更には5〜20%が最も好ましい。 In the case of a film preparation such as an intraoral patch, a film having the ability to form a film and edible is used, and a synthetic polymer substance such as polyvinyl pyrrolidone (hereinafter referred to as “PVP”), carboxyvinyl polymer (Hereinafter referred to as “CVP”), polyvinyl alcohol (hereinafter referred to as “PVA”) and the like; cellulose derivatives such as hydroxypropylmethylcellulose (hereinafter referred to as “HPMC”), hydroxypropylcellulose (hereinafter referred to as “HPC”), Hydroxyethyl cellulose (hereinafter referred to as “HEC”), methyl cellulose (hereinafter referred to as “MC”), ethyl cellulose (hereinafter referred to as “EC”), etc .; high molecular substances obtained from natural products such as sodium alginate, dextran, casein, pullulan , Pectin, gum arabic, karaya gum, denp And the like. Particularly preferred are PVP, HPC, starch, locust bean gum, carrageenan and gellan gum. These substances can be used alone or in combination of two or more. The total amount is 20 to 90%, preferably 25 to 80% of the dry mass of the film. Furthermore, a plasticizer can be blended in addition to the polymer substance. As the plasticizer, a compound that is compatible with the above-described polymer substance and softens it is used. For example, glycerin, diglycerin, triglycerin, polyglycerin, sorbitol, maltitol, xylitol, polyethylene glycol, propylene glycol, Examples include butylene glycol, hexylene glycol, pentylene glycol, polyoxyethylene polyoxypropylene glycol, and acetylethanolamine, with propylene glycol, glycerin, sorbitol, xylitol, and polyethylene glycol being particularly preferable. The addition amount of the plasticizer is 1 to 30% of the dry mass of the film, and more preferably 5 to 20%.
前記の成分に加えて、更にその組成物の形態等に応じて適宜な成分を配合することができる。例えば、非イオン性界面活性剤として、糖又は糖アルコールの脂肪酸エステルであって、それぞれ脂肪酸残基の炭素数が12〜18、平均エステル化度が1.1〜2.5、好ましくは1.2〜1.9のものが使用できる。該糖又は糖アルコールの脂肪酸エステルとしては、例えば、ショ糖脂肪酸エステル、マルトース脂肪酸エステル、マルチトール脂肪酸エステル、マルトトリイトール脂肪酸エステル、マルトテトライトール脂肪酸エステル、マルトペンタイトール脂肪酸エステル、マルトヘキサイトール脂肪酸エステル、マルトヘプタイトール脂肪酸エステル、ソルビタン脂肪酸エステル、ラクトース脂肪酸エステル、ラクチトール脂肪酸エステルが挙げられる。また、非イオン界面活性剤としては、この他に、ポリオキシエチレンソルビタンモノラウレート、ポリオキシエチレンソルビタンモノステアレート等の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硬化ヒマシ油、ポリオキシエチレン脂肪酸エステル、脂肪酸モノグリセライド、ポリオキシエチレン高級アルコールエーテル、ポリオキシエチレンポリオキシプロピレン脂肪酸エステルなども使用され得る。 In addition to the above components, appropriate components can be further blended depending on the form of the composition. For example, as the nonionic surfactant, a fatty acid ester of sugar or sugar alcohol, each having a fatty acid residue having 12 to 18 carbon atoms and an average degree of esterification of 1.1 to 2.5, preferably 1. 2 to 1.9 can be used. Examples of the fatty acid ester of the sugar or sugar alcohol include sucrose fatty acid ester, maltose fatty acid ester, maltitol fatty acid ester, maltotriitol fatty acid ester, maltotetritol fatty acid ester, maltopentytitol fatty acid ester, maltohexai Examples include tall fatty acid esters, maltoheptitol fatty acid esters, sorbitan fatty acid esters, lactose fatty acid esters, and lactitol fatty acid esters. Other nonionic surfactants include polyoxyethylene sorbitan monolaurate, polyoxyethylene sorbitan fatty acid ester such as polyoxyethylene sorbitan monostearate, polyoxyethylene hydrogenated castor oil, polyoxyethylene fatty acid ester. Fatty acid monoglycerides, polyoxyethylene higher alcohol ethers, polyoxyethylene polyoxypropylene fatty acid esters and the like can also be used.
また、アニオン界面活性剤として、例えば、ソジウム−N−メチル−N−パルミトイルタウライド、ソジウム−N−ラウロイル−β−アラニネート、ラウロイルサルコシンナトリウム、ソジウム−N−長鎖アシル塩基性アミノ酸等が用いられる。更に、両性界面活性剤として、例えば、2−アルキル−N−カルボキシメチル−N−ヒドロキシルエチルイミダゾリニウムベタイン、塩酸アルキルジアミノエチルグリシン、ラウリルジメチルアミノ酢酸ベタイン等が用いられる。 Examples of the anionic surfactant include sodium-N-methyl-N-palmitoyl tauride, sodium-N-lauroyl-β-alaninate, sodium lauroyl sarcosine, sodium-N-long chain acyl basic amino acid, and the like. . Furthermore, as the amphoteric surfactant, for example, 2-alkyl-N-carboxymethyl-N-hydroxylethylimidazolinium betaine, alkyldiaminoethylglycine hydrochloride, lauryldimethylaminoacetic acid betaine, and the like are used.
なお、これらの界面活性剤はその1種を単独で用いても2種以上を併用しても差し支えない。界面活性剤の配合量は、通常、組成物全体の0.01〜5%、好ましくは0.05〜3%である。 These surfactants may be used alone or in combination of two or more. The compounding quantity of surfactant is 0.01 to 5% of the whole composition normally, Preferably it is 0.05 to 3%.
本発明の口腔内組成物には、例えば、軟膏剤のようなペースト状組成物の場合には粘結剤としてカラゲナン、カルボキシメチルセルロースナトリウム、カルボキシメチルヒドロキシルエチルセルロースナトリウムなどのアニオン性セルロース誘導体、アルギン酸ナトリウムなどのアルカリ金属アルギネート、アルギン酸プロピレングリコールエステル、キサンタンガム、トラガカントガム、カラヤガム、アラビヤガムなどのガム類、ポリビニルアルコール、ポリアクリル酸ナトリウム、カルボキシビニルポリマー、ポリビニルピロリドンなどの合成粘結剤、シリカゲル、アルミニウムシリカゲル、ビーガム、ラポナイトなどの無機粘結剤等の1種又は2種以上が配合され得る。これらの配合量は通常、組成物全体の0.3〜5%である。 In the oral cavity composition of the present invention, for example, in the case of a paste-like composition such as an ointment, an anionic cellulose derivative such as carrageenan, sodium carboxymethylcellulose, sodium carboxymethylhydroxylethylcellulose, sodium alginate, etc. Alkali metal alginate, propylene glycol alginate ester, xanthan gum, tragacanth gum, karaya gum, gum arabic gum and other gums, polyvinyl alcohol, sodium polyacrylate, carboxyvinyl polymer, polyvinylpyrrolidone and other synthetic binders, silica gel, aluminum silica gel, beegum, 1 type, or 2 or more types, such as inorganic binders, such as a laponite, may be mix | blended. These compounding quantities are 0.3 to 5% of the whole composition normally.
更に、ペースト状や液状口腔内組成物の製造において、粘稠剤としてソルビット、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−ブチレングリコール、ポリエチレングリコール、ポリプロピレングリコール、キシリット、マルチット、ラクチット等の1種又は2種以上を配合し得る。これらの配合量は通常、組成物全体の10〜70%である。 Furthermore, in the production of paste-like and liquid oral compositions, one kind of thickener such as sorbit, glycerin, ethylene glycol, propylene glycol, 1,3-butylene glycol, polyethylene glycol, polypropylene glycol, xylit, maltite, lactit, etc. Or 2 or more types may be mix | blended. These compounding quantities are 10 to 70% of the whole composition normally.
また、歯磨類の場合には、第二リン酸カルシウム・二水和物及び無水物、第一リン酸カルシウム、第三リン酸カルシウム、炭酸カルシウム、ピロリン酸カルシウム、水酸化アルミニウム、アルミナ、無水ケイ酸、シリカゲル、ケイ酸アルミニウム、不溶性メタリン酸ナトリウム、第三リン酸マグネシウム、炭酸マグネシウム、硫酸カルシウム、ポリメタクリル酸メチル、ベントナイト、ケイ酸ジルコニウム、合成樹脂等の1種又は2種以上を配合することができ、配合量は通常、組成物全体の5〜90%、練歯磨の場合には5〜60%である。 In the case of dentifrice, dicalcium phosphate dihydrate and anhydride, primary calcium phosphate, tricalcium phosphate, calcium carbonate, calcium pyrophosphate, aluminum hydroxide, alumina, anhydrous silicic acid, silica gel, aluminum silicate Insoluble sodium metaphosphate, tribasic magnesium phosphate, magnesium carbonate, calcium sulfate, polymethyl methacrylate, bentonite, zirconium silicate, synthetic resin and the like can be blended in one or more, and the blending amount is usually In the case of a toothpaste, it is 5 to 60%.
薬効成分として、クロルヘキシジン、ベンゼトニウムクロライド、ベンザルコニウムクロライド、セチルピリジニウムクロライド、デカリニウムクロライド等の陽イオン性殺菌剤、トリクロサン、ヒノキチオール、ビオゾール等のフェノール性化合物、デキストラナーゼ、ムタナーゼ、リゾチーム、アミラーゼ、プロテアーゼ、溶菌酵素、スーパーオキシドジスムターゼ等の酵素、ビタミンC等のビタミン類、モノフルオロリン酸ナトリウム、モノフルオロリン酸カリウム等のアルカリ金属モノフルオロリン酸塩、フッ化ナトリウム、フッ化第1スズ等のフッ化物、トラネキサム酸、イプシロンアミノカプロン酸、アルミニウムクロルヒドロキシアラントイン、ジヒドロコレステロール、グリチルリチン酸、グリチルレチン酸、アズレン、ビサボロール、グリセロフォスフェート、クロロフィル、塩化ナトリウム、水溶性無機リン酸化合物、グルコン酸銅等の銅化合物、乳酸アルミニウム、塩化ストロンチウム、硝酸カリウム、ベルベリン、ヒドロキサム酸及びその誘導体、トリポリリン酸ナトリウム、ゼオライト、メトキシエチレン・無水マレイン酸共重合体、エピジヒドロコレステリン、トリクロロカルバニド、クエン酸亜鉛、トウキ、オウバク、カミツレ、チョウジ、オウゴン、ベニバナ等の抽出物等の公知の有効成分を1種又は2種以上配合し得る。これらの物質は単独であるいは2種以上の組み合わせで使用することができる。これら薬効成分を配合する場合、配合量は組成物全体の0.005〜30%、好適には0.01〜20%である。 Medicinal ingredients include cationic fungicides such as chlorhexidine, benzethonium chloride, benzalkonium chloride, cetylpyridinium chloride, decalinium chloride, phenolic compounds such as triclosan, hinokitiol, biozol, dextranase, mutanase, lysozyme, amylase Enzymes such as protease, lytic enzyme, superoxide dismutase, vitamins such as vitamin C, alkali metal monofluorophosphates such as sodium monofluorophosphate and potassium monofluorophosphate, sodium fluoride, stannous fluoride Such as fluoride, tranexamic acid, epsilon aminocaproic acid, aluminum chlorohydroxy allantoin, dihydrocholesterol, glycyrrhizic acid, glycyrrhetinic acid, azulene, biphenyl Borol, glycerophosphate, chlorophyll, sodium chloride, water-soluble inorganic phosphate compounds, copper compounds such as copper gluconate, aluminum lactate, strontium chloride, potassium nitrate, berberine, hydroxamic acid and its derivatives, sodium tripolyphosphate, zeolite, methoxyethylene・ Contains one or more known active ingredients such as maleic anhydride copolymer, epidihydrocholesterin, trichlorocarbanide, zinc citrate, sugarcane, duckweed, chamomile, clove, ogon, safflower extract Can do. These substances can be used alone or in combination of two or more. When blending these medicinal ingredients, the blending amount is 0.005 to 30%, preferably 0.01 to 20% of the entire composition.
また、一般の医薬用組成物として、抗菌物質、抗ヒスタミン剤、抗炎症剤、抗ウイルス剤、抗真菌生物剤、麻酔剤、免疫抑制剤、代謝拮抗剤、駆虫剤、アメーバ撲滅剤、鎮痛剤、抗関節炎剤、抗精神病剤、抗高血圧剤、筋弛緩剤等が挙げられ、更に具体的には、ホセキシチン、N−ホルムアミドイルチェナマイシン、テトラサイクリン、クロラムフェニコール、ネオマイシン、カルベニシリン、コリスチン、ペニシリンG、ポリマイキシンB、バンコマイシン、セハゾリン、セファロリジン、チブロリハマイシン、グラミシジン、バシトラシン、スルホンアミド、ゲンタマイシン、カナマイシン、アミカシン、シソミシン、トブラマイシン、ナリジキシックアシッド、ノルフロキサシン、フルダラニン、ニトロフラゾン、ピリルアミン、クロルフェニラミン、テトラヒドラゾリン、アンタゾリン、コルチゾン、ヒドロコルチゾン、酢酸コルチゾン、ベータメタソン、デキサメタソン、デキサメタソンリン酸ナトリウム、プレドニソン、メチルプレドニソロン、メドリソン、フルオロメトロン、フルオコルトロン、プレドニソロン、プレドニソロンリン酸ナトリウム、トリアムシノロン、インドメタシン、スリンダック、エコチオフェート、ピロカルピン、サリチル酸フィソスチグミン、ジイソプロピルフルオロフォスファート、エピネフリン、ジピボリルエピネフリン、ネオスチグミン、ヨウ化エコチオペート、臭化デメカリウム、カルバコール、メタコリン、ベタネコール、アトロピン、ホマトロピン、スコポラミン、ヒドロキシアンフェタミン、エフェドリン、コカイン、トロピカミド、フェニルエフリン、シクロペントレート、オキシフェノニウム、オイカトロピン、チモロール、グリセロール、尿素、イベルメクチン、ピリメタミン、トリサルファピリミジン、クリンダマイシン、アシクロビル、5−ヨード−2−デオキシウリジン、アデノシンアラビノシド、トリフルオロチミジン、インターフェロン、アセタゾールアミド、ジクロルフェンアミド、アムフォテリシンB、ニスタチン、フルシトシン、ナタマイシン、ミコナゾール、エチドカインコカイン、ベノキシネート、塩酸ジブカイン、塩酸ジクロニン、ナエパイン、塩酸フェナカイン、ピペロカイン、塩酸プロパラカイン、塩酸テトラカイン、ヘキシルカイン、ブピバカイン、リドカイン、メピバカイン、ローズベンガル、アドレナリン、ヒドロキシアンフェタミン、ピロカルピン、キモトリプシン、EDTA、デフェロキサミン、メソトレキセート、シクロフォスファミド、アザチオプリン、インシュリン、リドカイン等が例示される。これらの物質は単独であるいは2種以上の組み合わせで使用することができる。これら成分を配合する場合、配合量は組成物全体の0.005〜30%、好適には0.01〜20%である。 In addition, general pharmaceutical compositions include antibacterial substances, antihistamines, anti-inflammatory agents, antiviral agents, antifungal biological agents, anesthetics, immunosuppressants, antimetabolites, anthelmintics, amoeba eradication agents, analgesics, anti Arthritis agent, antipsychotic agent, antihypertensive agent, muscle relaxant and the like, more specifically, fosexitin, N-formamidoylchenamicin, tetracycline, chloramphenicol, neomycin, carbenicillin, colistin, penicillin G, Polymyxin B, vancomycin, sehazoline, cephaloridine, tibrolihamycin, gramicidin, bacitracin, sulfonamide, gentamicin, kanamycin, amikacin, sisomicin, tobramycin, nalidixic acid, norfloxacin, fludaranin, nitrofurazone, pyrilamine, chloroamine Phenylamine, tetrahydrazoline, antazoline, cortisone, hydrocortisone, cortisone acetate, betamethasone, dexamethasone, dexamethasone sodium phosphate, prednisone, methylprednisolone, medrison, fluorometholone, fluocortron, prednisolone, sodium prednisolone phosphate, triamcinolone, indomethacin , Sulindac, ecothiophene, pilocarpine, physostigmine salicylate, diisopropylfluorophosphate, epinephrine, dipivoryl epinephrine, neostigmine, ecothiopate iodide, demepotassium bromide, carbachol, methacholine, betanecol, atropine, homatropine, scopolamine, hydroxyamphetamine, hydroxyamphetamine , Cocaine, toro Camide, phenylephrine, cyclopentrate, oxyphenonium, eucatropine, timolol, glycerol, urea, ivermectin, pyrimethamine, trisulfapyrimidine, clindamycin, acyclovir, 5-iodo-2-deoxyuridine, adenosine arabinoside, tri Fluorothymidine, interferon, acetazolamide, dichlorofenamide, amphotericin B, nystatin, flucytosine, natamycin, miconazole, etidocaine cocaine, benoxinate, dibucaine hydrochloride, dichronin hydrochloride, naepine, phenacine hydrochloride, piperocaine, proparacaine hydrochloride, hydrochloric acid Tetracaine, hexylcaine, bupivacaine, lidocaine, mepivacaine, rose bengal, adrenaline, hydroxyan Examples include fetamine, pilocarpine, chymotrypsin, EDTA, deferoxamine, methotrexate, cyclophosphamide, azathioprine, insulin, lidocaine and the like. These substances can be used alone or in combination of two or more. When these components are blended, the blending amount is 0.005 to 30%, preferably 0.01 to 20% of the entire composition.
以下、実施例及び比較例を示し、本発明を具体的に説明するが、本発明は下記の実施例に制限されるものではない。 EXAMPLES Hereinafter, although an Example and a comparative example are shown and this invention is demonstrated concretely, this invention is not restrict | limited to the following Example.
[実施例1〜7、比較例1〜3]
表1に示す組成に従い、適量のエタノールに植物エタノール抽出エキス又は植物粉末、ヒドロキシプロピルセルロース、ポリエチレングリコール、水等の成分を加えて撹拌溶解し、これをポリエステル剥離フィルム上に展延乾燥して、厚さ約300μmのフィルムを製造した。得られたフィルムを直径14mmの丸形に裁断し、口腔内貼付剤を得た。
調製したサンプルについて、下記の手順で、口臭抑制評価を行った。結果を表1に示す。
方法:口臭の強い男女20名について、サンプル貼付前と、貼付後10分後と、製剤が口中からなくなった後60分後との呼気をテドラーバッグに1リットル採取し、口臭の強さを専門評価者によって評価した。評価は、貼付前との比較で下記の4段階で評価し、○以上を良好なレベルと判断した。
◎:非常に抑制した
○:抑制した
×:変わらなかった
<使用感(味覚)>
男女20名により、貼付時の使用感について評価した。
◎:苦味なし
○:やや苦味あり
×:苦味あり
[Examples 1-7, Comparative Examples 1-3]
According to the composition shown in Table 1, ingredients such as plant ethanol extract or plant powder, hydroxypropylcellulose, polyethylene glycol, water and the like are added to an appropriate amount of ethanol and dissolved by stirring, and this is spread and dried on a polyester release film, A film about 300 μm thick was produced. The obtained film was cut into a round shape having a diameter of 14 mm to obtain an intraoral patch.
About the prepared sample, bad breath suppression evaluation was performed in the following procedure. The results are shown in Table 1.
Method: For 20 men and women with strong bad breath, 1 liter of exhaled breath was collected in a Tedlar bag before applying the sample, 10 minutes after applying, and 60 minutes after the product disappeared from the mouth, and the intensity of bad breath was evaluated. Evaluated by the person. Evaluation was evaluated in the following four stages in comparison with the state before pasting, and a value of ○ or higher was judged as a good level.
◎: Suppressed very much ○: Suppressed ×: Not changed <Usage (taste)>
Twenty men and women evaluated the feeling of use at the time of sticking.
◎: No bitterness ○: Some bitterness ×: Bitterness
[実施例8] トローチ
キシリトール 77.3 %
アラビアゴム 5.0
タルク 2.0
ステアリン酸マグネシウム 0.7
ローズマリーの水抽出物(豊玉香料(株)製) 5.0
サンショウ種子粉末 1.0
ハッカ油 2.0
水 残
計 100.0
[Example 8] Troche Xylitol 77.3%
Arabic gum 5.0
Talc 2.0
Magnesium stearate 0.7
Rosemary water extract (Toyotama Fragrance Co., Ltd.) 5.0
Salam seed powder 1.0
Peppermint oil 2.0
Water remaining
Total 100.0
[実施例9] 口腔用軟膏
流動パラフィン 15.0 %
セタノール 10.0
グリセリン 20.0
ポリオキシエチレンソルビタン脂肪酸エステル 5.0
スペアミント油 0.01
サッカリンナトリウム 0.1
メリッサのエタノール抽出物 3.0
サンショウのエタノール抽出物((株)京都食品研究所製) 0.1
コ−ラのエタノール抽出物(三栄源エフ・エフ・アイ(株)製) 1.0
メントール 0.5
水 残
計 100.0
[Example 9] Oral ointment Liquid paraffin 15.0%
Cetanol 10.0
Glycerin 20.0
Polyoxyethylene sorbitan fatty acid ester 5.0
Spearmint oil 0.01
Saccharin sodium 0.1
Melissa's ethanol extract 3.0
Salamander ethanol extract (Kyoto Food Research Co., Ltd.) 0.1
Ethanol extract of cola (manufactured by Saneigen FFI Co., Ltd.) 1.0
Menthol 0.5
Water remaining
Total 100.0
[実施例10] 口腔内貼付剤
l−メントール 5.0 %
プルラン 52.2
キサンタンガム 5.9
ソルビット 8.4
濃グリセリン 9.0
プロピレングリコール 2.7
モノステアリン酸デカグリセリル 1.0
アセスルファムカリウム 0.24
スクラロース 0.16
アスパルテーム 2.0
ローズマリーの水抽出物(豊玉香料(株)製) 1.0
サンショウのエタノール抽出物((株)京都食品研究所製) 0.5
羅漢果抽出物 1.0
パセリ油 0.05
水 残
計 100.0
[Example 10] Oral patch 1-menthol 5.0%
Pullulan 52.2
Xanthan gum 5.9
Sorbit 8.4
Concentrated glycerin 9.0
Propylene glycol 2.7
Decaglyceryl monostearate 1.0
Acesulfame potassium 0.24
Sucralose 0.16
Aspartame 2.0
Rosemary water extract (Toyotama Fragrance Co., Ltd.) 1.0
Salam ethanol extract (Kyoto Food Research Co., Ltd.) 0.5
Rahan fruit extract 1.0
Parsley oil 0.05
Water remaining
Total 100.0
[実施例11] 洗口剤
ジェランガム 0.1 %
グリセリン 10.0
デキストラナーゼ 0.2
サッカリン 0.1
ラウリン酸デカグリセリル 0.5
エタノール 5.0
セージの水抽出物 0.5
サンショウのエタノール抽出物((株)京都食品研究所製) 0.3
ペパーミント油 0.05
l−メントール 0.1
水 残
計 100.0
[Example 11] Mouthwash Gellan gum 0.1%
Glycerin 10.0
Dextranase 0.2
Saccharin 0.1
Decaglyceryl laurate 0.5
Ethanol 5.0
Sage water extract 0.5
Salamander ethanol extract (Kyoto Food Research Institute Co., Ltd.) 0.3
Peppermint oil 0.05
l-Menthol 0.1
Water remaining
Total 100.0
実施例8〜11について、これを常法により適用し、実施例1〜7と同様の口臭試験を実施した結果、表2に示す通り、優れた口臭抑制効果が認められた。 About Example 8-11, this was applied by the conventional method, As a result of implementing the same bad breath test as Example 1-7, as shown in Table 2, the outstanding bad breath suppression effect was recognized.
[実施例12] 口腔内貼付剤
プルラン 2.0 %
ヒドロキシプロピルセルロース 28.0
ヒドロキシプロピルメチルセルロース 25.0
ポリビニルアルコール 1.0
キサンタンガム 6.0
D−ソルビトール 8.0
濃グリセリン 10.0
アスパルテーム 0.05
モノステアリン酸ソルビタン 0.5
塩化セチルピリジニウム 2.0
グリチルリチン酸ジカリウム 3.5
エタノール 5.0
ローズマリーの水抽出物(豊玉香料(株)製) 0.02
サンショウのエタノール抽出物((株)京都食品研究所製) 0.3
l−メントール 1.0
水 残
計 100.0
[Example 12] Oral patch Pullulan 2.0%
Hydroxypropylcellulose 28.0
Hydroxypropyl methylcellulose 25.0
Polyvinyl alcohol 1.0
Xanthan gum 6.0
D-sorbitol 8.0
Concentrated glycerin 10.0
Aspartame 0.05
Sorbitan monostearate 0.5
Cetylpyridinium chloride 2.0
Dipotassium glycyrrhizinate 3.5
Ethanol 5.0
Rosemary water extract (made by Toyoda Fragrance Co., Ltd.) 0.02
Salamander ethanol extract (Kyoto Food Research Institute Co., Ltd.) 0.3
l-Menthol 1.0
Water remaining
Total 100.0
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