WO2005099731A1 - Antibacterial agent derived from galenical and composition for external application containing the same - Google Patents

Antibacterial agent derived from galenical and composition for external application containing the same Download PDF

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Publication number
WO2005099731A1
WO2005099731A1 PCT/JP2004/013360 JP2004013360W WO2005099731A1 WO 2005099731 A1 WO2005099731 A1 WO 2005099731A1 JP 2004013360 W JP2004013360 W JP 2004013360W WO 2005099731 A1 WO2005099731 A1 WO 2005099731A1
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Prior art keywords
extract
antibacterial agent
present
mocco
composition
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PCT/JP2004/013360
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French (fr)
Japanese (ja)
Inventor
Katsuya Shimoo
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Kobayashi Pharmaceutical Co., Ltd.
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Publication of WO2005099731A1 publication Critical patent/WO2005099731A1/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9789—Magnoliopsida [dicotyledons]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • A61Q17/005—Antimicrobial preparations

Definitions

  • the present invention relates to an antibacterial agent containing mockup extract as an active ingredient and an external composition containing the same.
  • Acne vulgaris (acne vulgaris) refers to a superficial chronic inflammatory condition that occurs in pores mainly in the pilosebaceous system of the skin, and is often seen in adolescent men and women. Although the cause of acne remains largely unknown, one of the causes is thought to be related to Propionibacterium acnes, which is resident in the skin.
  • Propio-pacterium acnes is present in the pores of the skin and breaks down lipids (sebum) to produce free fatty acids. It is known that this free fatty acid has a comedone-forming action and an inflammation-inducing action. It is said that when sebum secretion becomes active during puberty due to the effects of sex hormones and the like, free fatty acids are excessively produced, resulting in the onset of millet.
  • Non-Patent Document 1 a female hormone agent having a sebum secretion inhibitory action and an antibiotic such as erythromycin and tetracycline having an antibacterial action cause gastrointestinal disorders.
  • Non-Patent Document 1 a female hormone agent having a sebum secretion inhibitory action and an antibiotic such as erythromycin and tetracycline having an antibacterial action cause gastrointestinal disorders.
  • iodine, camphor, sulfa drugs, etc. which have a keratolytic action, have a problem in that irritation to the skin around the affected area due to repeated application is strong.
  • Patent Document 1 JP-A-3-93710
  • Non-Patent Document 1 Today's Therapeutics 2003 Commentary and Handbook Nankodo
  • the present invention provides an antibacterial agent which has a high antibacterial activity against propio-batatherium acnes, which is a causative agent of acne, has excellent safety with few side effects such as skin irritation, and an external composition containing the same.
  • the main purpose is to provide things.
  • mocco extract has a high antibacterial activity against propio-batteri lactic acid, and have completed the present invention.
  • the present invention provides the following antibacterial agents and external compositions containing the same.
  • Item 1 An antibacterial agent for propio-battery bacterium containing mokko extract as an active ingredient.
  • Item 2 An external composition containing the antibacterial agent according to Item 1.
  • Item 3 The external composition according to Item 2, which is for piles and millet.
  • the mocco extract which is an active ingredient of the antibacterial agent of the present invention, is obtained from a large perennial plant of the family Asteraceae, called mocco.
  • mocco a large perennial plant of the family Asteraceae
  • the root of mocco it is preferable that the root of mocco can be obtained.
  • Leaf, rhizome, stem, root bark, etc. may be used.
  • a conventionally known method can be used for producing the mocco extract used in the present invention.
  • mocco or a dried product of mocco can be extracted with water or hot water, or extracted with an organic solvent and filtered. Method and the like.
  • the extraction conditions are not particularly limited as long as they are generally used for plant extraction.
  • the extract may be concentrated if necessary.
  • concentration method an ordinary method such as an evaporator can be used.
  • a commercially available mocco extract may be used.
  • a known solvent may be used.
  • water, methanol, ethanol, propanol, isopropanol, butanol, ethylene glycol, propylene glycol, 1,3- Organic solvents such as butylene glycol, diethylene glycol, dipropylene glycol, isoprene glycol, hexylene glycol, glycerin, methyl acetate, ethyl acetate, isopropyl acetate, ethyl ether, isopropyl ether, and acetone can be used, and water and ethanol are preferred. From these extraction solvents, one kind alone Or a mixture of two or more.
  • the extract thus obtained can be used as it is as the antibacterial agent of the present invention, or can be subjected to a purification operation such as deodorization and decolorization within a range not to lose the effects of the present invention. it can.
  • the antibacterial agent of the present invention can be used in the form of a powder by evaporating and drying the extraction solvent from the above extract, or can be used in the form of water, ethanol, propylene glycol, 1,3-butylene glycol, glycerin and the like. It can also be used after re-dissolving in a solvent.
  • the antibacterial agent of the present invention may be one that also has the above-mentioned extract or its composition power, but further contains excipients, carriers, preservatives, antioxidants, stabilizers and the like. It may be. It may also contain other antibacterial agents.
  • the antibacterial agent of the present invention has good antibacterial activity, particularly against Propionibacterium acnes, as shown in Example 1 described below.
  • the effective amount of the antibacterial agent of the present invention is as follows if the extract containing the amount of the extract extracted from 4 g of the dry weight of “mocco” described in the Pharmacopoeia per lg of the extract is used as the mocco extract.
  • the effective amount of Mokko II extract is, for example, about 1% by weight or more, preferably about 5% by weight or more, more preferably about 10% by weight or more based on the total amount of the agent.
  • 100 g of the antibacterial agent of the present invention contains "mocco" power described in Pharmacopoeia in a dry weight of about 4 g or more, which is extracted with water or ethanol.
  • the extract contains about 20 g or more, more preferably about 40 g or more of the extracted component obtained from "Mocco".
  • the antibacterial agent of the present invention can be effectively used, for example, as an antibacterial component of an external composition for anti-acne.
  • a compound having an antibacterial action such as ethanol
  • the antibacterial effect can be obtained in a smaller amount than the above. Therefore, the range of the effective amount is not limited to about 1% by weight or more of Mokko extract.
  • the present invention further provides an external composition, particularly an anti-millet external composition, containing the above antibacterial agent.
  • an anti-millet external composition containing the above antibacterial agent.
  • the pile-millet is the prevention and prevention of millet.
  • composition for external use of the present invention can be prepared by blending the above antibacterial agent of the present invention as one component at any stage of the production process.
  • the dosage form of the composition for external use containing the antibacterial agent of the present invention is not particularly limited as long as the effect of the antibacterial agent can be obtained.
  • ointments, solutions, creams, patches, cataplasms, lotions, Widely used in aerosols, stones, bath preparations, detergents, knocking agents, lotions, emulsions, skin conditioners, creams, foundation cosmetics, foundations, concealers and other pharmaceuticals, quasi-drugs, cosmetics, etc. Can be
  • Mokko extract which is an active ingredient of the composition for external use of the present invention, has an antibacterial activity against propio-battereribacterium, a causative bacterium of acne, and therefore can be used as a pile-millet composition.
  • the mocco extract in the antibacterial agent of the present invention is used.
  • An effective amount based on the total amount of the agent, for example, 0. 5 to 100 weight 0/0 approximately or more, preferably more than about 1 one 100 wt%, more preferably above examples of extent 10 100% by weight .
  • the antimicrobial agent 100 g of the present invention contains an extractable component in an amount of about 2 to 400 g in terms of dry weight extracted from water or ethanol from "Mocco II" described in Pharmacopoeia. It is desirable to contain about 4 to 400 g, more preferably about 40 to 400 g of the extracted component obtained from "Mocco".
  • the antibacterial agent of the present invention is used as an external composition other than the anti-millet composition, those skilled in the art can easily determine the compounding amount and the like with reference to the above examples.
  • composition of the present invention may contain various components generally used in cosmetics, quasi-drugs, and pharmaceuticals, aqueous components, oil components, moisturizing components, excipients, Viscous agents, preservatives, antioxidants, PH adjusters, carriers, fragrances, coloring agents, chemicals, etc. may be used alone or as a mixture of two or more.
  • composition for external use of the present invention a known antibacterial agent as long as the effects of the present invention are not impaired.
  • antibacterial agents examples include iochi, hinokitiol, triclosan, trichlorocarbalide, haloca Lupine, chlorophenesin, benzethonium chloride, benzalkonium chloride, alkyldiaminoethylglycine hydrochloride, chlorhexidine hydrochloride, chlorhexidine dalconate, isopropylmethylphenol, benzoic acid, thymol, hexaclofen, berberine, resorcinol And its derivatives such as cetyl pyridium and its derivatives.
  • Examples of the keratin softener include zeolite, salicylic acid, resorcinol, urea and the like.
  • anti-inflammatory agents include ketoprofen, ibuprofen piconol, glycyrrhetinic acid, dipotassium glycyrrhizinate, glycyrrhizic acid, indomethacin, diclofenac, piroxicam, planoprofen, flurbiprofen, loxoprofen, cortisone acetate, hydrocortisone, dexamethasone , Prednisolone, betamethasone, felbinac and the like.
  • keratin softener and anti-inflammatory agent When used, they may be used alone or in combination of two or more. When used in combination with the antibacterial agent of the present invention, it is possible to reduce the amount of known bactericides, keratin softeners, and anti-inflammatory agents, which are problematic side effects, based on their favorable antibacterial activity. It is expected to enhance the safety as a composition.
  • a highly safe antibacterial agent having a high antibacterial activity against propio-batatherium bacterium, the causative bacterium of acne, and a mocco extract, which is a crude drug component, as an active ingredient.
  • An agent can be provided.
  • an external composition containing the antibacterial agent in particular, an external composition for piles and millet can be provided.
  • the antibacterial activity was evaluated by measuring the blocking circle diameter by the paper disk method.
  • Propio-batteridium acnes was applied to GAM agar medium, anaerobic culture was performed at 35 ° C for 24 hours, and after enrichment, it was suspended in sterile physiological saline so that Macfaland O.5 was obtained. Turned cloudy.
  • Mocco extract showed an equal or greater inhibition diameter than ozone extract, indicating that it was useful as an antibacterial agent against propiobacterium bacterium.
  • Table 1 shows the measurement results by the paper disk method.

Abstract

[PROBLEMS] To provide a highly safe antibacterial agent having high antibacterial activity against Propionibacterium acnes which is a causative bacterium of pimples. [MEANS FOR SOLVING PROBLEMS] There is provided an antibacterial agent against Propionibacterium acnes, comprising banksia extract as an active ingredient.

Description

明 細 書  Specification
生薬由来の抗菌剤及びこれを含有する外用組成物  Crude drug-derived antibacterial agent and external composition containing the same
技術分野  Technical field
[0001] 本発明は、モッコゥエキスを有効成分とする抗菌剤及びこれを含有する外用組成物 に関する。  The present invention relates to an antibacterial agent containing mockup extract as an active ingredient and an external composition containing the same.
背景技術  Background art
[0002] 二キビ (尋常性ざ瘡）は、皮膚の毛嚢脂腺系を中心とした毛孔におこる表在性の慢 性炎症状態を指し、思春期の男女に多く見られる。二キビの原因は、まだ不明な点が 多いが、その原因の 1つとして、皮膚に常在するプロピオ-バタテリゥム ァクネス（Pr opionibacterium acnes)が関与して 、ると考えられて 、る。  [0002] Acne vulgaris (acne vulgaris) refers to a superficial chronic inflammatory condition that occurs in pores mainly in the pilosebaceous system of the skin, and is often seen in adolescent men and women. Although the cause of acne remains largely unknown, one of the causes is thought to be related to Propionibacterium acnes, which is resident in the skin.
[0003] プロピオ-パクテリゥム ァクネスは、皮膚の毛孔内に存在し、脂質 (皮脂）を分解し て遊離脂肪酸を生成する。この遊離脂肪酸には、面皰形成作用、炎症惹起作用が あることが知られている。思春期に性ホルモン等の影響によって皮脂分泌が活発に なると、遊離脂肪酸が過剰に生成され、その結果-キビを発症するとされている。  [0003] Propio-pacterium acnes is present in the pores of the skin and breaks down lipids (sebum) to produce free fatty acids. It is known that this free fatty acid has a comedone-forming action and an inflammation-inducing action. It is said that when sebum secretion becomes active during puberty due to the effects of sex hormones and the like, free fatty acids are excessively produced, resulting in the onset of millet.
[0004] 従来、二キビ治療剤として、プロピオ-パクテリゥム ァクネスに対する抗菌作用をは じめ、皮脂分泌抑制作用、角質溶解作用を有するものが広く用いられてきた。  [0004] Conventionally, as agents for treating acne, those having an antibacterial action against propio-pacterium acnes, a sebum secretion inhibiting action, and a keratolytic action have been widely used.
[0005] し力しながら、これら既存の-キビ治療剤には、種々の副作用を伴う。例えば、皮脂 分泌抑制作用を有する女性ホルモン剤、及び抗菌作用を有するエリスロマイシン、テ トラサイクリン等の抗生物質等は、胃腸障害を引き起こすことが知られている (非特許 文献 1)。また、角質溶解作用を有するィォゥ、カンフル、サルファ剤等は、度重なる 塗布による患部周辺の皮膚に対する刺激が強ぐ力さっき等が問題となっている。  [0005] However, these existing-millet remedies are associated with various side effects. For example, it is known that a female hormone agent having a sebum secretion inhibitory action and an antibiotic such as erythromycin and tetracycline having an antibacterial action cause gastrointestinal disorders (Non-Patent Document 1). In addition, iodine, camphor, sulfa drugs, etc., which have a keratolytic action, have a problem in that irritation to the skin around the affected area due to repeated application is strong.
[0006] なお、上記の他に、ゲレップ、蘇方木、矢車の実、ログウッド等力 得られた植物ェ キスを有効成分とする二キビ治療剤も知られている（例えば、特許文献 1参照)。 特許文献 1：特開平 3—93710  [0006] In addition to the above, there is also known a remedy for acne containing a plant extract obtained as an active ingredient, such as gerep, soho tree, yam, logwood, etc. (for example, Patent Document 1 reference). Patent Document 1: JP-A-3-93710
非特許文献 1 :今日の治療薬 2003 解説と便覧 南江堂  Non-Patent Document 1: Today's Therapeutics 2003 Commentary and Handbook Nankodo
発明の開示  Disclosure of the invention
発明が解決しょうとする課題 [0007] 本発明は、二キビの原因菌であるプロピオ-バタテリゥム ァクネスに対して高い抗 菌作用を有し、皮膚刺激等の副作用の少ない安全性に優れた抗菌剤及びこれを含 有する外用組成物を提供することを主な目的とする。 Problems the invention is trying to solve [0007] The present invention provides an antibacterial agent which has a high antibacterial activity against propio-batatherium acnes, which is a causative agent of acne, has excellent safety with few side effects such as skin irritation, and an external composition containing the same. The main purpose is to provide things.
課題を解決するための手段  Means for solving the problem
[0008] 本発明者らは、モッコゥエキスがプロピオ-バタテリゥム ァクネスに対して高い抗菌 作用を有することを見出し、本発明を完成するに至った。 [0008] The present inventors have found that mocco extract has a high antibacterial activity against propio-batteri lactic acid, and have completed the present invention.
[0009] 本発明は、以下の抗菌剤及びこれを含有する外用組成物を提供する。 [0009] The present invention provides the following antibacterial agents and external compositions containing the same.
項 1.モッコゥエキスを有効成分とするプロピオ-バタテリゥム ァクネスに対する抗菌 剤。  Item 1. An antibacterial agent for propio-battery bacterium containing mokko extract as an active ingredient.
項 2.項 1に記載の抗菌剤を含む外用組成物。  Item 2. An external composition containing the antibacterial agent according to Item 1.
項 3.杭-キビ用である項 2に記載の外用組成物。  Item 3. The external composition according to Item 2, which is for piles and millet.
[0010] 本発明の抗菌剤の有効成分であるモッコゥエキスは、モッコゥ（木香）と呼ばれるキ ク科の大形多年草から得られる。モッコゥエキスとしては、モッコゥの根力も得られるも のが好ましいが、プロピオ-バタテリゥム ァクネスに対する抗菌効果が得られるもの であれば、モッコゥの植物体全体 (全草)又は根以外の任意の部分 (例えば、葉、根 茎、茎、根皮等)から抽出されたものを用いてもよい。 [0010] The mocco extract, which is an active ingredient of the antibacterial agent of the present invention, is obtained from a large perennial plant of the family Asteraceae, called mocco. As the mocco extract, it is preferable that the root of mocco can be obtained. Leaf, rhizome, stem, root bark, etc.) may be used.
[0011] 本発明で用いるモッコゥエキスの製造方法としては、従来公知の方法を使用するこ とができ、例えば、モッコゥ又はモッコゥの乾燥物を水又は熱水抽出、あるいは有機 溶媒で抽出し、濾過する方法等があげられる。抽出の条件としては、一般的に植物 抽出に用いられるものであれば特に限定されない。さらに、抽出、濾過の後、必要に 応じて該エキスを濃縮してもよい。濃縮の方法としては、エバポレーター等の常法を 用いることができる。また、巿販のモッコゥエキスを用いてもよい。  [0011] A conventionally known method can be used for producing the mocco extract used in the present invention. For example, mocco or a dried product of mocco can be extracted with water or hot water, or extracted with an organic solvent and filtered. Method and the like. The extraction conditions are not particularly limited as long as they are generally used for plant extraction. Further, after extraction and filtration, the extract may be concentrated if necessary. As a concentration method, an ordinary method such as an evaporator can be used. Alternatively, a commercially available mocco extract may be used.
[0012] 抽出に用いる溶媒としては、公知のものを用いればよぐ例えば、水、メタノール、ェ タノ一ノレ、プロパノーノレ、イソプロパノーノレ、ブタノーノレ、エチレングリコーノレ、プロピレ ングリコール、 1, 3—ブチレングリコール、ジエチレングリコール、ジプロピレングリコー ル、イソプレングリコール、へキシレングリコール、グリセリン、酢酸メチル、酢酸ェチル 、酢酸イソプロピル、ェチルエーテル、イソプロピルエーテル、アセトン等の有機溶媒 を用いることができ、水、エタノールが好ましい。これらの抽出溶媒から、 1種を単独で 、又は 2種以上を混合して使用する。 As the solvent used for the extraction, a known solvent may be used. For example, water, methanol, ethanol, propanol, isopropanol, butanol, ethylene glycol, propylene glycol, 1,3- Organic solvents such as butylene glycol, diethylene glycol, dipropylene glycol, isoprene glycol, hexylene glycol, glycerin, methyl acetate, ethyl acetate, isopropyl acetate, ethyl ether, isopropyl ether, and acetone can be used, and water and ethanol are preferred. From these extraction solvents, one kind alone Or a mixture of two or more.
[0013] この様にして得られた抽出物は、本発明の抗菌剤としてそのまま用いることもできる し、また、本発明の効果を失わない範囲内で脱臭、脱色等の精製操作を加えることも できる。さらに、本発明の抗菌剤は、上記の抽出物から抽出溶媒を蒸発、乾固させて 粉末状で用いることもでき、又は水、エタノール、プロピレングリコール、 1, 3—ブチレ ングリコール、グリセリン等の溶媒に再溶解して用いることもできる。 [0013] The extract thus obtained can be used as it is as the antibacterial agent of the present invention, or can be subjected to a purification operation such as deodorization and decolorization within a range not to lose the effects of the present invention. it can. Further, the antibacterial agent of the present invention can be used in the form of a powder by evaporating and drying the extraction solvent from the above extract, or can be used in the form of water, ethanol, propylene glycol, 1,3-butylene glycol, glycerin and the like. It can also be used after re-dissolving in a solvent.
[0014] 本発明の抗菌剤は、上記抽出物又はその組成物力もなるものであってもよいが、さ らに賦形剤、担体、防腐剤、抗酸化剤、安定化剤等を含んでいてもよい。また、他の 抗菌剤を含んでいてもよい。  [0014] The antibacterial agent of the present invention may be one that also has the above-mentioned extract or its composition power, but further contains excipients, carriers, preservatives, antioxidants, stabilizers and the like. It may be. It may also contain other antibacterial agents.
[0015] 本発明の抗菌剤は、後述する実施例 1で示すように、特にプロピオ-パクテリゥム ァクネス（Propionibacterium acnes)に対して良好な抗菌活性を有している。その 有効量は、モッコゥエキスとして、該エキス lgあたり、局方記載の「モッコゥ」の乾燥重 量 4gから抽出される量の抽出成分を含むものを使用する場合であれば、本発明の 抗菌剤におけるモッコゥエキスの有効量は、該剤の総量に対して、例えば 1重量％程 度以上、好ましくは 5重量％程度以上、更に好ましくは 10重量％程度以上が例示さ れる。  [0015] The antibacterial agent of the present invention has good antibacterial activity, particularly against Propionibacterium acnes, as shown in Example 1 described below. The effective amount of the antibacterial agent of the present invention is as follows if the extract containing the amount of the extract extracted from 4 g of the dry weight of “mocco” described in the Pharmacopoeia per lg of the extract is used as the mocco extract. The effective amount of Mokko II extract is, for example, about 1% by weight or more, preferably about 5% by weight or more, more preferably about 10% by weight or more based on the total amount of the agent.
[0016] また、本発明の抗菌剤 100g中に、乾燥重量 4g程度以上の局方記載の「モッコゥ」 力 水又はエタノールで抽出される量の抽出成分を含んでいることが望ましぐ好まし くは 20g程度以上、さらに好ましくは 40g程度以上の「モッコゥ」から得られる該抽出 成分を含むことが望ましい。  [0016] Further, it is preferable that 100 g of the antibacterial agent of the present invention contains "mocco" power described in Pharmacopoeia in a dry weight of about 4 g or more, which is extracted with water or ethanol. Preferably, the extract contains about 20 g or more, more preferably about 40 g or more of the extracted component obtained from "Mocco".
[0017] ゆえに、本発明の抗菌剤は、例えば、抗ニキビを目的とする外用組成物の抗菌成 分として有効に用いることができる。また、本発明の抗菌剤に、他の抗菌剤及び抗菌 作用を有する化合物（エタノール等）を加える場合は、上記よりも少な 、量で抗菌効 果を得ることができる。よって、該有効量の範囲は、モッコゥエキスとして 1重量％程度 以上に限定されない。  Therefore, the antibacterial agent of the present invention can be effectively used, for example, as an antibacterial component of an external composition for anti-acne. When other antibacterial agents and a compound having an antibacterial action (such as ethanol) are added to the antibacterial agent of the present invention, the antibacterial effect can be obtained in a smaller amount than the above. Therefore, the range of the effective amount is not limited to about 1% by weight or more of Mokko extract.
[0018] 従って、本発明は、さらに、上記の抗菌剤を含有する外用組成物、特に抗-キビ用 の外用組成物を提供する。なお、本発明において杭-キビとは、二キビの予防及び [0018] Accordingly, the present invention further provides an external composition, particularly an anti-millet external composition, containing the above antibacterial agent. In the present invention, the pile-millet is the prevention and prevention of millet.
Z又は治療を目的として用いることを指す。 [0019] 本発明の外用組成物は、上記本発明の抗菌剤を 1成分として、製造過程の任意の 段階で配合することによって調製することができる。本発明の抗菌剤を含有する外用 組成物の剤型は、該抗菌剤の効果が得られるものであれば特に限定されず、例えば 、軟膏、液剤、クリーム、貼付剤、パップ剤、ローション剤、エアゾール剤、石鹼、浴用 剤、洗浄剤、ノック剤、化粧水、乳液、スキンコンディショナー、クリーム、下地化粧料 、ファンデーション、コンシ一ラー等の医薬品、医薬部外品、化粧料等に広く使用さ れ得る。 Z or refers to use for therapeutic purposes. The composition for external use of the present invention can be prepared by blending the above antibacterial agent of the present invention as one component at any stage of the production process. The dosage form of the composition for external use containing the antibacterial agent of the present invention is not particularly limited as long as the effect of the antibacterial agent can be obtained.For example, ointments, solutions, creams, patches, cataplasms, lotions, Widely used in aerosols, stones, bath preparations, detergents, knocking agents, lotions, emulsions, skin conditioners, creams, foundation cosmetics, foundations, concealers and other pharmaceuticals, quasi-drugs, cosmetics, etc. Can be
[0020] 特に、本発明の外用組成物の有効成分であるモッコゥエキスは、ニキビの原因菌で あるプロピオ-バタテリゥム ァクネスに対する抗菌作用を有することから、杭-キビ組 成物として使用することができる。  [0020] In particular, Mokko extract, which is an active ingredient of the composition for external use of the present invention, has an antibacterial activity against propio-battereribacterium, a causative bacterium of acne, and therefore can be used as a pile-millet composition.
[0021] モッコゥエキスとして、該エキス lgあたり、局方記載の「モッコゥ」の乾燥重量 4gから 抽出される量の抽出成分を含むものを使用する場合であれば、本発明の抗菌剤に おけるモッコゥエキスの有効量は、該剤の総量に対して、例えば 0. 5— 100重量0 /0 程度以上、好ましくは 1一 100重量％程度以上、さらに好ましくは 10— 100重量％程 度以上が例示される。 [0021] If the extract containing the amount of the extract extracted from 4 g of the dry weight of "Mocco" described in the Pharmacopoeia per lg of the extract is used as the mocco extract, the mocco extract in the antibacterial agent of the present invention is used. An effective amount, based on the total amount of the agent, for example, 0. 5 to 100 weight 0/0 approximately or more, preferably more than about 1 one 100 wt%, more preferably above examples of extent 10 100% by weight .
[0022] また、例えば、本発明の抗菌剤 lOOg中に、乾燥重量 2— 400g程度の局方記載の 「モッコゥ」から水又はエタノールで抽出される量の抽出成分を含んでいることが望ま しぐ好ましくは 4一 400g程度、より好ましくは 40— 400g程度の「モッコゥ」から得ら れる該抽出成分を含むことが望ましい。  [0022] For example, it is desirable that the antimicrobial agent 100 g of the present invention contains an extractable component in an amount of about 2 to 400 g in terms of dry weight extracted from water or ethanol from "Mocco II" described in Pharmacopoeia. It is desirable to contain about 4 to 400 g, more preferably about 40 to 400 g of the extracted component obtained from "Mocco".
[0023] 抗-キビ組成物以外の外用組成物として本発明の抗菌剤を用いる場合には、当業 者であれば、上記の例を参考に容易に配合量等を決定することができる。 When the antibacterial agent of the present invention is used as an external composition other than the anti-millet composition, those skilled in the art can easily determine the compounding amount and the like with reference to the above examples.
[0024] また、本発明の組成物には、必要に応じて、化粧料、医薬部外品、医薬品に一般 的に用いられる各種成分、水性成分、油性成分、保湿成分、賦形剤、増粘剤、防腐 剤、酸化防止剤、 PH調整剤、担体、香料、色剤、薬剤等を単独又は 2種以上を混合 して用いてもよい。 [0024] Further, the composition of the present invention may contain various components generally used in cosmetics, quasi-drugs, and pharmaceuticals, aqueous components, oil components, moisturizing components, excipients, Viscous agents, preservatives, antioxidants, PH adjusters, carriers, fragrances, coloring agents, chemicals, etc. may be used alone or as a mixture of two or more.
[0025] 本発明の外用組成物として、本発明の効果を損なわない範囲内で、公知の抗菌剤 [0025] As the composition for external use of the present invention, a known antibacterial agent as long as the effects of the present invention are not impaired.
、角質軟化剤及び消炎剤を含んでもよい。 Keratin softeners and anti-inflammatory agents.
[0026] 抗菌剤としては、ィォゥ、ヒノキチオール、トリクロサン、トリクロロカルバ-リド、ハロカ ルパン、クロロフヱネシン、塩化べンゼトニゥム、塩化ベンザルコニゥム、塩酸アルキ ルジアミノエチルグリシン、塩酸クロルへキシジン、ダルコン酸クロルへキシジン、イソ プロピルメチルフエノール、安息香酸、チモール、へキサクロ口フェン、ベルべリン、レ ゾルシン、塩ィ匕セチルピリジ-ゥム及びこれらの誘導体等があげられる。 [0026] Examples of antibacterial agents include iochi, hinokitiol, triclosan, trichlorocarbalide, haloca Lupine, chlorophenesin, benzethonium chloride, benzalkonium chloride, alkyldiaminoethylglycine hydrochloride, chlorhexidine hydrochloride, chlorhexidine dalconate, isopropylmethylphenol, benzoic acid, thymol, hexaclofen, berberine, resorcinol And its derivatives such as cetyl pyridium and its derivatives.
[0027] 角質軟化剤としては、ィォゥ、サリチル酸、レゾルシン、尿素等があげられる。  [0027] Examples of the keratin softener include zeolite, salicylic acid, resorcinol, urea and the like.
[0028] 消炎剤としては、ケトプロフェン、イブプロフェンピコノール、グリチルレチン酸、グリ チルリチン酸ジカリウム、グリチルリチン酸、インドメタシン、ジクロフエナック、ピロキシ カム、プラノプロフェン、フルルビプロフェン、ロキソプロフェン、酢酸コルチゾン、ヒドロ コルチゾン、デキサメタゾン、プレドニゾロン、ベタメタゾン、フェルビナク等があげられ る。 [0028] Examples of anti-inflammatory agents include ketoprofen, ibuprofen piconol, glycyrrhetinic acid, dipotassium glycyrrhizinate, glycyrrhizic acid, indomethacin, diclofenac, piroxicam, planoprofen, flurbiprofen, loxoprofen, cortisone acetate, hydrocortisone, dexamethasone , Prednisolone, betamethasone, felbinac and the like.
[0029] 上記の抗菌剤、角質軟化剤及び消炎剤を用いる場合、単独で使用してもよぐ 2種 以上を組み合わせて使用してもよい。本発明の抗菌剤と併用することにより、その良 好な抗菌活性に基づいて、副作用が問題となっている既知の殺菌剤、角質軟化剤、 消炎剤の量を減じることも可能であり、外用組成物としての安全性を高めることが期 待される。  When the above-mentioned antibacterial agent, keratin softener and anti-inflammatory agent are used, they may be used alone or in combination of two or more. When used in combination with the antibacterial agent of the present invention, it is possible to reduce the amount of known bactericides, keratin softeners, and anti-inflammatory agents, which are problematic side effects, based on their favorable antibacterial activity. It is expected to enhance the safety as a composition.
発明の効果  The invention's effect
[0030] 本発明によれば、二キビの原因菌であるプロピオ-バタテリゥム ァクネスに対して 高い抗菌作用を有し、かつ生薬成分であるモッコゥ抽出物を有効成分とすることから 安全性の高い抗菌剤を提供することができる。また、該抗菌剤を含有する外用組成 物、特に杭-キビ用外用組成物を提供することができる。  According to the present invention, a highly safe antibacterial agent having a high antibacterial activity against propio-batatherium bacterium, the causative bacterium of acne, and a mocco extract, which is a crude drug component, as an active ingredient. An agent can be provided. In addition, an external composition containing the antibacterial agent, in particular, an external composition for piles and millet can be provided.
発明を実施するための最良の形態  BEST MODE FOR CARRYING OUT THE INVENTION
[0031] 以下、実施例をあげて本発明を具体的に説明するが、本発明はこれらの実施例に 何ら限定されるものではな 、。 Hereinafter, the present invention will be described specifically with reference to Examples, but the present invention is not limited to these Examples.
実施例 1  Example 1
[0032] 試験方法  [0032] Test method
ペーパーディスク法による阻止円径の測定により抗菌力を評価した。  The antibacterial activity was evaluated by measuring the blocking circle diameter by the paper disk method.
[0033] プロピオ-バタテリゥム ァクネスを、 GAM寒天培地に塗布し、 35°Cにて 24時間、 嫌気培養を行い、増菌させた後、減菌生理食塩水に MacfalandO. 5になるように懸 濁させた。 [0033] Propio-batteridium acnes was applied to GAM agar medium, anaerobic culture was performed at 35 ° C for 24 hours, and after enrichment, it was suspended in sterile physiological saline so that Macfaland O.5 was obtained. Turned cloudy.
[0034] シャーレ中の GAM寒天培地上に、この懸濁液 0. 05mlをコンラージ棒で均一に塗 布し、その上にペーパーディスク（直径 8mm)を置 、て試料（モッコゥエキス又はォゥ ゴンエキス) 0. 1mlを含浸させた。これを 35°Cにて 48時間嫌気培養後、阻止円の有 無とその直径を測定した。比較例として、プロピオ-バタテリゥム ァクネスに対する抗 菌効果が公知である、ォゥゴンエキスを使用した。  [0034] On a GAM agar medium in a petri dish, 0.05 ml of this suspension was evenly applied with a conical rod, and a paper disk (diameter 8 mm) was placed thereon, and a sample (mocco extract or ozone extract) was placed. 0.1 ml was impregnated. This was anaerobically cultured at 35 ° C for 48 hours, and then the presence or absence of an inhibition circle and its diameter were measured. As a comparative example, an oegone extract, whose antibacterial effect against propio-batteridium acnes was known, was used.
[0035] 試験結果  [0035] Test results
モッコゥエキスは、ォゥゴンエキスと比較して同等以上の阻止円径を示し、プロピオ -バクテリゥム ァクネスに対する抗菌剤として有用であることがわ力つた。  Mocco extract showed an equal or greater inhibition diameter than ozone extract, indicating that it was useful as an antibacterial agent against propiobacterium bacterium.
[0036] ペーパーディスク法による測定結果を表 1に示す。 Table 1 shows the measurement results by the paper disk method.
[0037] [表 1] [Table 1]
Figure imgf000007_0001
Figure imgf000007_0001
(-：阻止円無形成) 実施例 2 (-: No blocking circle formed)
[0038] 以下、モッコゥエキスを用いた製剤の処方例を示すが、本発明はこれに限定される ものではない。  [0038] Hereinafter, formulation examples of preparations using Mokko II extract are shown, but the present invention is not limited thereto.
[0039] [処方例 1]  [0039] [Prescription example 1]
軟膏 [g]  Ointment [g]
モッコゥエキス 10  Mokko Extract 10
グリチルリチン酸ジカリウム 0. 5  Dipotassium glycyrrhizinate 0.5
ベントナイト 20  Bentonite 20
カオリン 20 グリセリン 10 プロピレングリコール 5 精製水 34. 5 合計 100 Kaolin 20 Glycerin 10 Propylene glycol 5 Purified water 34.5 Total 100
[0040] [処方例 2] [Formula 2]
軟膏 [g] モッコゥエキス 10 ィォゥ 2 グリチルリチン酸ジカリウム 0. 5 ベントナイト 20 カオリン 20 グリセリン 10 プロピレングリコール 5 精製水 32. 5 合計 100  Ointment [g] Mocco extract 10 io 2 Dipotassium glycyrrhizinate 0.5 Bentonite 20 Kaolin 20 Glycerin 10 Propylene glycol 5 Purified water 32.5 Total 100
[0041] [処方例 3] [Formula 3]
液剤 [g] モッコゥエキス 10 ポリオキシエチレンォレイルエーテル 1 エタノール 10 パラベン 0. 1 精製水 78. 9  Solution [g] Mokko II extract 10 Polyoxyethylene oleyl ether 1 Ethanol 10 Paraben 0.1 Purified water 78. 9
A斗 A doo
O B I 100 O B I 100
[処方例 4] [Prescription example 4]
エアゾール [g] モッコゥエキス 5 イソプロピルメチルフエノール 0. 1 エタノール 20 精製水 24. 9 液化石油ガス 50 Aerosol [g] Mokko II extract 5 Isopropylmethylphenol 0.1 Ethanol 20 Purified water 24.9 Liquefied petroleum gas 50
A斗 A doo
O B I 100 O B I 100

Claims

請求の範囲 The scope of the claims
[1] モッコゥエキスを有効成分とするプロピオ-バタテリゥム ァクネスに対する抗菌剤,  [1] An antibacterial agent for propio-batterylum acnes containing mocco extract as an active ingredient,
[2] 請求項 1に記載の抗菌剤を含む外用組成物。 [2] An external composition comprising the antibacterial agent according to claim 1.
[3] 抗ニキビ用である請求項 2に記載の外用組成物。 [3] The external composition according to claim 2, which is used for anti-acne.
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JPH06227960A (en) * 1993-02-01 1994-08-16 Yakult Honsha Co Ltd Melanin formation inhibitor and skin cosmetic
JP2000136141A (en) * 1998-10-30 2000-05-16 Sumitomo Forestry Co Ltd Antibacterial agent
JP2001322940A (en) * 2000-05-12 2001-11-20 Kao Corp Cathepsin d production facilitative agent
JP2003335696A (en) * 2002-05-14 2003-11-25 Jakwang Co Ltd Natural cell transmitter comprising water soluble chitosan and extract of inula helenium l.

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JPH06227960A (en) * 1993-02-01 1994-08-16 Yakult Honsha Co Ltd Melanin formation inhibitor and skin cosmetic
JP2000136141A (en) * 1998-10-30 2000-05-16 Sumitomo Forestry Co Ltd Antibacterial agent
JP2001322940A (en) * 2000-05-12 2001-11-20 Kao Corp Cathepsin d production facilitative agent
JP2003335696A (en) * 2002-05-14 2003-11-25 Jakwang Co Ltd Natural cell transmitter comprising water soluble chitosan and extract of inula helenium l.

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