JP5462430B2 - Anti-inflammatory and analgesic - Google Patents
Anti-inflammatory and analgesic Download PDFInfo
- Publication number
- JP5462430B2 JP5462430B2 JP2006202961A JP2006202961A JP5462430B2 JP 5462430 B2 JP5462430 B2 JP 5462430B2 JP 2006202961 A JP2006202961 A JP 2006202961A JP 2006202961 A JP2006202961 A JP 2006202961A JP 5462430 B2 JP5462430 B2 JP 5462430B2
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- Prior art keywords
- extract
- acid
- oil
- kiwi
- inflammatory
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Description
本発明は、関節炎等を予防又は治療するための抗炎症剤等に関するものである。 The present invention relates to an anti-inflammatory agent for preventing or treating arthritis and the like.
ヒトを含む哺乳類の関節は、運動により常に機械的刺激を受けていることから、容易に炎症や物理的破壊に見舞われる危険にさらされている。このような関節における障害(以下、単に「関節障害」という。)を惹起する要因には、感染、外傷、アレルギー、代謝異常、肥満、血流障害などがある。関節障害の発症率が加齢とともに上昇する傾向も指摘されており、高齢化が進む現代においては、関節障害はひとつの社会問題となりつつある。 The joints of mammals, including humans, are constantly exposed to mechanical stimuli from exercise and are therefore at risk of easily suffering from inflammation and physical destruction. Factors that cause such joint disorders (hereinafter simply referred to as “joint disorders”) include infection, trauma, allergies, metabolic abnormalities, obesity, and blood flow disorders. It has also been pointed out that the incidence of joint disorders increases with age, and in today's aging society, joint disorders are becoming a social problem.
関節障害は一般に炎症を伴うことから、現在多くの場合、関節障害に対しては抗炎症剤等による治療が行われている。 Since joint disorders generally involve inflammation, currently, in many cases, joint disorders are treated with anti-inflammatory agents and the like.
このような背景の下、本発明者は、キウイ種子の抽出物やそれに含有されるクエルシトリン、ケンフェロール3‐O‐ラムノシド等に抗炎症作用を有することを見出し、本発明を完成させた。 Under such a background, the present inventors have found that an extract of kiwi seeds, quercitrin, kaempferol 3-O-rhamnoside and the like contained therein have an anti-inflammatory action, and completed the present invention.
即ち、本発明は、天然物由来の安全で、副作用の少ない抗炎症剤及び鎮痛剤を提供とすることを目的とする。 That is, an object of the present invention is to provide an anti-inflammatory agent and an analgesic that are safe from natural products and have few side effects.
本発明の抗炎症剤及び鎮痛剤は、下記化学式(1)にて示される化合物を有効成分とすることを特徴とする。
以下、本発明を詳細に説明する。
本発明の、抗炎症剤及び鎮痛剤(以下、「抗炎症剤等」とする。)は、下記化学式(1)にて示される化合物を有効成分とするものである。
このような化合物としてクエルシトリン、及びケンフェロール3‐O‐ラムノシド等が挙げられるが、これらに限定されない。尚、これらは、1種のみを用いても良いし、2種以上を併用しても良い。ここで、クエルシトリンとは、上記化学式(1)においてRがHに置換された化合物である。更に、ケンフェロール3‐O‐ラムノシドとは化学式(1)において、RがOHに置換された化合物である。
Hereinafter, the present invention will be described in detail.
The anti-inflammatory agent and analgesic agent (hereinafter referred to as “anti-inflammatory agent etc.”) of the present invention comprises a compound represented by the following chemical formula (1) as an active ingredient.
Such compounds include, but are not limited to, quercitrin, kaempferol 3-O-rhamnoside, and the like. In addition, these may use only 1 type and may use 2 or more types together. Here, quercitrin is a compound in which R is substituted with H in the chemical formula (1). Furthermore, kaempferol 3-O-rhamnoside is a compound in which R is substituted with OH in the chemical formula (1).
上記化学式(1)にて示される化合物を得る方法は、特に限定されず、例えば、植物から抽出する方法、合成により得る方法等があるが、植物から抽出する方法が好ましい。容易に上記化合物を得ることができるからである。
上記化合物を植物によって抽出する場合、その原料として例えば、どくだみ、キウイ、イチョウ等があげられるが、キウイを原料とすることが好ましい。上記化学式(1)にて示される化合物を容易に抽出することができるからである。
The method for obtaining the compound represented by the chemical formula (1) is not particularly limited, and examples thereof include a method of extracting from a plant and a method of obtaining by synthesis, and a method of extracting from a plant is preferable. This is because the above compound can be easily obtained.
When the above compound is extracted by a plant, examples of the raw material include dokudomi, kiwi, ginkgo and the like, but it is preferable to use kiwi as a raw material. This is because the compound represented by the chemical formula (1) can be easily extracted.
また、本発明の抗炎症剤等は、キウイ種子抽出物を有効成分とすることを特徴とする。 キウイとは、キウイフルーツ(Actinidia chinensis Planch.)ともよばれ、中国の中・南部が原産である。中国では彌猴桃(ビコウトウ)と呼ばれ、漢方薬として用いられている。その後、20世紀に入ってからニュージーランドに渡り、優れた品種が多く育成されている。果実の外観がニュージーランドの国鳥「KIWI」の幼鳥に似ていることからキウイフルーツと名付けられた。日本では、1966年に紹介された後、1970年代後半から栽培が始まり、現在は年間4万t前後の生産量がある。 キウイは雌雄異株のつる性植物であり、果実は卵状もしくはほぼ球形の液果である。開花期は4〜6月で、8〜10月に結実する。自生品は、山の斜面、林の周辺、あるいは低木の茂みの中に生えるものである。 In addition, the anti-inflammatory agent and the like of the present invention is characterized by using kiwi seed extract as an active ingredient. Kiwi is also called Kiwi fruit (Actinidia chinensis Planch.) And is native to the middle and south of China. In China, it is called Bikotou and is used as a herbal medicine. Since then, since the beginning of the 20th century, many excellent varieties have been cultivated throughout New Zealand. It was named Kiwifruit because the appearance of the fruit resembles a young bird of New Zealand's national bird "KIWI". In Japan, after being introduced in 1966, cultivation began in the latter half of the 1970s, and there are currently around 40,000 tons of production. Kiwi is a hermaphroditic vine, and the fruits are egg-shaped or almost spherical berries. The flowering period is from April to June, and it will bear fruit from August to October. Native products grow on mountain slopes, around forests, or in bushes of shrubs.
本発明は、キウイの種子を用いることに限定したものであり、キウイの種子を用いる方法で有れば全ての効果を期待することができる。キウイ種子をそのまま用いても良いが、脱脂を行ったキウイ種子を用いることが好ましい。有効成分を容易に抽出することができるからである。 脱脂方法としては、例えば、キウイ種子を圧搾して油分を分離するだけでも良いし、上記油分を分離した後、圧搾物の残留油分を脱脂用溶媒(脂溶性有機溶媒)により抽出分離しても良い。 The present invention is limited to using kiwi seeds, and all effects can be expected if the method uses kiwi seeds. Kiwi seeds may be used as they are, but it is preferable to use kiwi seeds that have been defatted. It is because an active ingredient can be extracted easily. As the degreasing method, for example, the oil component may be separated by pressing the kiwi seeds, or after separating the oil component, the residual oil component of the pressed product may be extracted and separated with a degreasing solvent (fat-soluble organic solvent). good.
このとき、好ましい脱脂用溶媒としては、n−ヘキサン、アセトン等が挙げられる。特に、脱脂用溶媒としてn−ヘキサンを用いることが好ましい。抽出油分を食用油として使用し得るとともに、脱脂キウイ種子の抽出物を食品素材等に利用しやすくなるからである。尚、これらの脱脂用の溶媒は、1種のみを用いても良いし2種以上併用しても良い。 At this time, preferable degreasing solvents include n-hexane, acetone and the like. In particular, n-hexane is preferably used as a degreasing solvent. This is because the extracted oil can be used as an edible oil and the extract of defatted kiwi seeds can be easily used as a food material. These degreasing solvents may be used alone or in combination of two or more.
キウイ種子又は脱脂されたキウイ種子から有効成分を抽出する場合、極性有機溶媒を用いる方法がより良い方法である。用いる溶媒としては、水、メタノール、エタノール、イソプロパノール、アセトン、1,3−ブチレングリコール、エチレングリコール、プロピレングリコール、グリセリン、酢酸、酢酸エチル、エーテル、ヘキサン、二酸化炭素などをそのまま単一溶媒で用いるか、2種類以上を任意に混合して用いて、抽出物を作成する事も出来る。 When extracting an active ingredient from kiwi seed or defatted kiwi seed, a method using a polar organic solvent is a better method. As a solvent to be used, water, methanol, ethanol, isopropanol, acetone, 1,3-butylene glycol, ethylene glycol, propylene glycol, glycerin, acetic acid, ethyl acetate, ether, hexane, carbon dioxide or the like is used as a single solvent as it is. Two or more types can be arbitrarily mixed and used to create an extract.
抽出溶媒として水を使用する場合には、抽出温度20〜100℃、好ましくは80〜100℃程度で行うとよい。これは、抽出温度が低すぎると、有効成分が抽出されにくいためである。抽出用の水の種類は、特に限定されず、水道水、蒸留水、ミネラル水、アルカリイオン水等を使用することができる。好ましくは、抽出溶媒として、深層水(海洋深層水)を使用するとよい。 When water is used as the extraction solvent, the extraction temperature is 20 to 100 ° C., preferably about 80 to 100 ° C. This is because if the extraction temperature is too low, it is difficult to extract active ingredients. The kind of water for extraction is not particularly limited, and tap water, distilled water, mineral water, alkaline ionized water and the like can be used. Preferably, deep water (deep ocean water) is used as the extraction solvent.
抽出溶媒として含水エタノールを使用する場合、エタノール濃度30〜90wt%であることが好ましい。30wt%程度よりも少ないか、90wt%を超えると、有効成分の抽出量が低下しやすくなるからである。また、抽出温度は、20〜80℃、好ましくは50〜80℃程度で行うとよい。なお、含水エタノール抽出は、有効成分の含有率を向上させるため、種々の濃度で繰り返すとよい。 When hydrous ethanol is used as the extraction solvent, the ethanol concentration is preferably 30 to 90 wt%. This is because if the amount is less than about 30 wt% or exceeds 90 wt%, the extraction amount of the active ingredient tends to decrease. The extraction temperature is 20 to 80 ° C, preferably about 50 to 80 ° C. In addition, the water-containing ethanol extraction may be repeated at various concentrations in order to improve the content of the active ingredient.
本発明の抗炎症剤等の抽出方法としては、連続抽出、浸漬抽出、向流抽出、超臨界抽出など任意の方法を採用することができ、室温ないし還流加熱下において任意の装置を使用することができる。 As an extraction method for the anti-inflammatory agent and the like of the present invention, any method such as continuous extraction, immersion extraction, countercurrent extraction, supercritical extraction can be employed, and any apparatus can be used at room temperature or under reflux heating. Can do.
具体的な方法としては、抽出溶媒を満たした処理槽に抽出原料を投入し、攪拌しながら有効成分を溶出させる。例えば、抽出溶媒として水または含水エタノールを用いる場合には、抽出原料の5〜100倍量程度(重量比)の極性溶媒を使用し、30分〜5時間程度抽出を行う。溶媒中に有効成分を溶出させた後、ろ過して抽出残渣を除くことによって、抽出液を得る。その後、常法に従って抽出液に希釈、濃縮、乾燥、精製等の処理を施し、抗炎症剤等とする。 なお、精製方法としては、例えば、活性炭処理、樹脂吸着処理、イオン交換樹脂、液−液向流分配等の方法が挙げられるが、食品等に添加する場合には大量に使用するものではないから、未精製のままで使用してもよい。 As a specific method, an extraction raw material is put into a treatment tank filled with an extraction solvent, and an active ingredient is eluted while stirring. For example, when water or water-containing ethanol is used as the extraction solvent, the extraction is performed for about 30 minutes to 5 hours using a polar solvent of about 5 to 100 times (weight ratio) of the extraction raw material. The active ingredient is eluted in the solvent, and then filtered to remove the extraction residue to obtain an extract. Thereafter, the extract is subjected to treatments such as dilution, concentration, drying and purification according to a conventional method to obtain an anti-inflammatory agent or the like. Examples of the purification method include activated carbon treatment, resin adsorption treatment, ion exchange resin, liquid-liquid countercurrent distribution, and the like, but they are not used in large quantities when added to foods. It may be used unpurified.
上記方法により製造されたキウイ種子抽出物は、キウイ種子抽出物の全質量を100wt%とした場合、ポリフェノールを2wt%以上、好ましくは5wt%以上、より好ましくは10wt%以上含有することができる。 また、上記キウイ種子抽出物は、クエルシトリン及びケンフェロール3‐O‐ラムノシドのうちの少なくとも一方を含有するものである。このとき、上記キウイ種子抽出物の全質量を100wt%とした場合、クエルシトリンを0.02wt%以上、好ましくは0.04wt%以上、より好ましくは0.06wt%以上含有することができる。 The kiwi seed extract produced by the above method can contain 2 wt% or more, preferably 5 wt% or more, more preferably 10 wt% or more of polyphenol when the total mass of the kiwi seed extract is 100 wt%. The kiwi seed extract contains at least one of quercitrin and kaempferol 3-O-rhamnoside. At this time, when the total mass of the kiwi seed extract is 100 wt%, quercitrin can be contained in an amount of 0.02 wt% or more, preferably 0.04 wt% or more, more preferably 0.06 wt% or more.
本発明の抗炎症剤等は、各種飲食品の素材として使用することができる。飲食品としては、例えば、食用油(サラダ油)、菓子類(ガム、キャンディー、キャラメル、チョコレート、クッキー、スナック、ゼリー、グミ、錠菓等)、麺類(そば、うどん、ラーメン等)、乳製品(ミルク、アイスクリーム、ヨーグルト等)、調味料(味噌、醤油等)、スープ類、飲料(ジュース、コーヒー、紅茶、茶、炭酸飲料、スポーツ飲料等)をはじめとする一般食品や、健康食品(錠剤、カプセル等)、栄養補助食品(栄養ドリンク等)が挙げられる。これらの飲食品に本発明の抗炎症剤等を適宜配合するとよい。 The anti-inflammatory agent etc. of this invention can be used as a raw material of various food-drinks. Examples of the food and drink include edible oil (salad oil), confectionery (gum, candy, caramel, chocolate, cookie, snack, jelly, gummy, tablet confection etc.), noodles (soba, udon, ramen etc.), and dairy products ( Milk, ice cream, yogurt, etc.), seasonings (miso, soy sauce, etc.), soups, beverages (juice, coffee, tea, tea, carbonated drinks, sports drinks, etc.) and health foods (tablets , Capsules, etc.) and nutritional supplements (nutrient drinks, etc.). The anti-inflammatory agent of this invention etc. are mix | blended suitably with these food / beverage products.
これら飲食品には、その種類に応じて種々の成分を配合することができ、例えば、ブドウ糖、果糖、ショ糖、マルトース、ソルビトール、ステビオサイド、コーンシロップ、乳糖、クエン酸、酒石酸、リンゴ酸、コハク酸、乳酸、L−アスコルビン酸、dl−α−トコフェロール、エリソルビン酸ナトリウム、グリセリン、プロピレングリコール、グリセリン脂肪酸エステル、ポリグリセリン脂肪酸エステル、ショ糖脂肪酸エステル、ソルビタン脂肪酸エステル、プロピレングリコール脂肪酸エステル、アラビアガム、カラギーナン、カゼイン、ゼラチン、ペクチン、寒天、ビタミンB類、ニコチン酸アミド、パントテン酸カルシウム、アミノ酸類、カルシウム塩類、色素、香料、保存剤等の食品素材を使用することができる。さらに、健康維持機能をもった本抗炎症剤等には、他の抗酸化物質や健康食品素材などの配剤、例えば、抗酸化物質(還元型アスコルビン酸(ビタミンC)、ビタミンE、還元型グルタチン、トコトリエノール、ビタミンA誘導体、リコピン、ルテイン、アスタキサンチン、ゼアキサンチン、フコキサンチン、尿酸、ユビキノン、コエンザイムQ10、葉酸、ニンニクエキス、アリシン、セサミン、リグナン類、カテキン、イソフラボン、カルコン、タンニン類、フラボノイド類、クマリン、イソクマリン類、ブルーベリーエキス)、健康食品素材(V.(ビタミン)A、V.B1、V.B2、V.B6、V.B12、V.C、V.D、V.E、V.P、コリン、ナイアシン、パントテン酸、葉酸カルシウム、EPA、オリゴ糖、食物繊維、スクアレン、大豆レシチン、タウリン、ドナリエラ、プロテイン、オクタコサノール、DHA、卵黄レシチン、リノール酸、ラクトフェリン、マグネシウム、亜鉛、クロム、セレン、カリウム、ヘム鉄、カキ肉エキス、キトサン、キチンオリゴ糖、コラーゲン、コンドロイチン、ウコン、カンゾウ、クコシ、ケイヒ、サンザシ、生姜、霊芝、シジミエキス、スッポン、カンゾウ、クコシ、ケイヒ、サンザシ、生姜、霊芝、オオバコ、カミツレ、カモミール、セイヨウタンポポ、ハイビスカス、ハチミツ、ボーレン、ローヤルゼリー、ライム、ラベンダー、ローズヒップ、ローズマリー、セージ、ビフィズス菌、フェーカリス菌、ラクリス、小麦胚芽油、ゴマ油、シソ油、大豆油、中鎖脂肪酸、アガリクス、イチョウ葉エキス、ウコン、コンドロイチン、玄米胚芽エキス、レイシ、タマネギ、DHA、 EPA、 DPA、 甜茶、冬虫夏草、ニンニク、蜂の子、パパイヤ、プーアル、プロポリス、メグスリの木、ヤブシタケ、ロイヤルゼリー、ノコギリヤシ、ヒアルロン酸、コラーゲン、ギャバ、ハープシールオイル、サメ軟骨、グルコサミン、レシチン、ホスファチジルセリン、田七ニンジン、桑葉、大豆抽出物、エキナセア、エゾウコギ、大麦抽出物、オリーブ葉、オリーブ実、ギムネマ、バナバ、サラシア、ガルシニア、キトサン、セントジョーンズワート、ナツメ、ニンジン、パッションフラワー、ブロッコリー、プラセンタ、ハトムギ、ブドウ種子、ピーナッツ種皮、ビルベリー、ブラックコホシュ、マリアアザミ、月桂樹、セージ、ローズマリー、ラフマ、黒酢、ゴーヤー、マカ、紅花、亜麻、ウーロン茶、花棘、カフェイン、カプサイシン、キシロオリゴ糖、グルコサミン、ソバ、シトラス、食物繊維、プロテイン、プルーン、スピルリナ、大麦若葉、核酸、酵母、椎茸、梅肉、アミノ酸、深海鮫抽出物、ノニ、カキ肉、スッポン、シャンピニオン、オオバコ、アセロラ、パイナップル、バナナ、モモ、アンズ、メロン、イチゴ、ラズベリー、オレンジ、フコイダン、メシマコブ、クランベリー、コンドロイチン硫酸、亜鉛、鉄、セラミド、シルクペプチド、グリシン、ナイアシン、チェストツリー、L-システイン、赤ワイン葉、ミレット、ホーステール、ビオチン、センテラアジアティカ、ハスカップ、ピクノジェノール、フキ、ルバーブ、クローブ、ローズマリー、カテキン、プーアル、クエン酸、ビール酵母、メリロート、ブラックジンガー、ショウガ、ガジュツ、ナットウキナーゼ、ベニコウジ、トコトリエノール、ラクトフェリン、シナモン、韃靼ソバ、ココア、ユズ種子エキス、シソの実エキス、ライチ種子エキス、月見草エキス、黒米エキス、α−リポ酸、生コーヒー豆エキス)なども配合することができる。 These foods and drinks can be blended with various ingredients depending on the type, for example, glucose, fructose, sucrose, maltose, sorbitol, stevioside, corn syrup, lactose, citric acid, tartaric acid, malic acid, succinic acid. Acid, lactic acid, L-ascorbic acid, dl-α-tocopherol, sodium erythorbate, glycerin, propylene glycol, glycerin fatty acid ester, polyglycerin fatty acid ester, sucrose fatty acid ester, sorbitan fatty acid ester, propylene glycol fatty acid ester, gum arabic, Food materials such as carrageenan, casein, gelatin, pectin, agar, vitamin Bs, nicotinic acid amide, calcium pantothenate, amino acids, calcium salts, pigments, fragrances and preservatives can be used. In addition, this anti-inflammatory agent with health maintenance function includes other antioxidants and health food ingredients such as antioxidants (reduced ascorbic acid (vitamin C), vitamin E, reduced glutatin) , Tocotrienol, vitamin A derivatives, lycopene, lutein, astaxanthin, zeaxanthin, fucoxanthin, uric acid, ubiquinone, coenzyme Q10, folic acid, garlic extract, allicin, sesamin, lignans, catechin, isoflavone, chalcone, tannins, flavonoids, coumarin , Isocoumarins, blueberry extract), health food ingredients (V. (vitamin) A, V.B1, V.B2, V.B6, V.B12, VC, VD, VE, VP, choline, niacin, pantothenic acid, Calcium folate, EPA, oligosaccharide, dietary fiber, squalene, soybean lecithin, taurine, donariella Thein, octacosanol, DHA, egg yolk lecithin, linoleic acid, lactoferrin, magnesium, zinc, chromium, selenium, potassium, heme iron, oyster meat extract, chitosan, chitin oligosaccharides, collagen, chondroitin, turmeric, licorice, kokushi, keihi, hawthorn , Ginger, ganoderma, swordfish extract, suppon, licorice, kokushi, keihi, hawthorn, ginger, ganoderma, plantain, chamomile, chamomile, dandelion, hibiscus, honey, boren, royal jelly, lime, lavender, rosehip, rosemary, Sage, bifidobacteria, faecalis, lacris, wheat germ oil, sesame oil, perilla oil, soybean oil, medium chain fatty acid, agaricus, ginkgo biloba extract, turmeric, chondroitin, brown rice germ extract, litchi, onion, DHA, EPA, DPA甜 Tea, Cordyceps, Garlic, Bee, Papaya, Puaru, Propolis, Meguri Tree, Yabushitake, Royal Jelly, Saw Palmetto, Hyaluronic Acid, Collagen, Gabba, Harpseal Oil, Shark Cartilage, Glucosamine, Lecithin, Phosphatidylserine, Tabashi Carrot, mulberry leaf, soy extract, echinacea, sorghum, barley extract, olive leaf, olive fruit, gymnema, banaba, salacia, garcinia, chitosan, st jones wort, jujube, carrot, passion flower, broccoli, placenta, pearl barley, grape Seeds, peanut seed coat, bilberry, black cohosh, maria thistle, laurel, sage, rosemary, raffma, black vinegar, bitter gourd, maca, safflower, flax, oolong tea, flower spine, caffeine, capsaicin, xy Oligosaccharide, Glucosamine, Buckwheat, Citrus, Dietary fiber, Protein, Prunes, Spirulina, Barley young leaves, Nucleic acid, Yeast, Shiitake, Plum meat, Amino acid, Deep sea potato extract, Noni, Oyster meat, Suppon, Champignon, Psyllium, Acerola, Pineapple, banana, peach, apricot, melon, strawberry, raspberry, orange, fucoidan, mesimacob, cranberry, chondroitin sulfate, zinc, iron, ceramide, silk peptide, glycine, niacin, chesttree, L-cysteine, red wine leaf, millet, Horsetail, Biotin, Centella Asiatica, Lotus Cup, Pycnogenol, Japanese cypress, Rhubarb, Clove, Rosemary, Catechin, Pual, Citric Acid, Beer Yeast, Merirot, Black Zinger, Ginger, Gajutsu, Nattokina Zeo, Benikouji, Tocotrienol, Lactoferrin, Cinnamon, Straw Buckwheat, Cocoa, Yuzu Seed Extract, Perilla Seed Extract, Lychee Seed Extract, Evening Primrose Extract, Black Rice Extract, α-Lipoic Acid, Raw Coffee Bean Extract) it can.
具体的な製法としては、抗炎症剤等を粉末セルロースとともにスプレードライまたは凍結乾燥し、これを粉末、顆粒、打錠または溶液にすることで容易に飲食品(インスタント食品等)に含有させることができる。また、抗炎症剤等を、例えば、油脂、エタノール、グリセリンあるいはこれらの混合物に溶解して液状にし、飲料に添加するか、固形食品に添加することが可能である。必要に応じてアラビアガム、デキストリン等のバインダーと混合して粉末状あるいは顆粒状にし、飲料に添加するか固形食品に添加することも可能である。 As a specific production method, an anti-inflammatory agent or the like is spray-dried or freeze-dried together with powdered cellulose, and this can be easily contained in a food or drink (instant food etc.) by making it into powder, granule, tableting or solution. it can. Further, for example, an anti-inflammatory agent or the like can be dissolved in oil, fat, ethanol, glycerin or a mixture thereof to form a liquid and added to a beverage or added to a solid food. If necessary, it can be mixed with a binder such as gum arabic or dextrin to form a powder or granules and added to a beverage or a solid food.
本発明の抗炎症剤等を飲食品に適用する場合の添加量としては、健康を維持することが主な目的であるので、飲食品に対して有効成分の含量が合計1〜20wt%であるのが好ましい。 As the addition amount when the anti-inflammatory agent or the like of the present invention is applied to foods and drinks, the main purpose is to maintain health, so the total content of active ingredients is 1 to 20 wt% with respect to the food and drinks. Is preferred.
本発明の抗炎症剤等は、薬品(医薬品および医薬部外品を含む。)の素材として用いてもよい。薬品製剤用の原料に、本発明の抗炎症剤等を適宜配合して製造することができる。本発明の抗炎症剤等に配合しうる製剤原料としては、例えば、賦形剤(ブドウ糖、乳糖、白糖、塩化ナトリウム、デンプン、炭酸カルシウム、カオリン、結晶セルロース、カカオ脂、硬化植物油、カオリン、タルク等)、結合剤(蒸留水、生理食塩水、エタノール水、単シロップ、ブドウ糖液、デンプン液、ゼラチン溶液、カルボキシメチルセルロース、リン酸カリウム、ポリビニルピロリドン等)、崩壊剤(アルギン酸ナトリウム、カンテン、炭酸水素ナトリウム、炭酸カルシウム、ラウリル硫酸ナトリウム、ステアリン酸モノグリセリド、デンプン、乳糖、アラビアゴム末、ゼラチン、エタノール等)、崩壊抑制剤(白糖、ステアリン、カカオ脂、水素添加油等)、吸収促進剤(第四級アンモニウム塩基、ラウリル硫酸ナトリウム等)、吸着剤(グリセリン、デンプン、乳糖、カオリン、ベントナイト、硅酸等)、滑沢剤(精製タルク、ステアリン酸塩、ポリエチレングリコール等)などが挙げられる。 The anti-inflammatory agent or the like of the present invention may be used as a raw material for medicines (including pharmaceuticals and quasi drugs). It can be produced by appropriately blending the anti-inflammatory agent of the present invention with a raw material for a pharmaceutical preparation. Examples of the raw material for preparation that can be blended in the anti-inflammatory agent of the present invention include, for example, excipients (glucose, lactose, sucrose, sodium chloride, starch, calcium carbonate, kaolin, crystalline cellulose, cacao butter, hydrogenated vegetable oil, kaolin, talc. Etc.), binder (distilled water, physiological saline, ethanol water, simple syrup, glucose solution, starch solution, gelatin solution, carboxymethylcellulose, potassium phosphate, polyvinylpyrrolidone, etc.), disintegrant (sodium alginate, agar, hydrogen carbonate) Sodium, calcium carbonate, sodium lauryl sulfate, stearic acid monoglyceride, starch, lactose, gum arabic powder, gelatin, ethanol, etc.), disintegration inhibitors (sucrose, stearin, cocoa butter, hydrogenated oil, etc.), absorption enhancers (fourth) Grade ammonium base, sodium lauryl sulfate, etc.), Chakuzai (glycerin, starch, lactose, kaolin, bentonite, silicic acid, etc.), lubricants (purified talc, stearates, polyethylene glycol, and the like) and the like.
本発明による抗炎症剤等の投与方法は、一般的には、錠剤、丸剤、軟・硬カプセル剤、細粒剤、散剤、顆粒剤、液剤等の形態で経口投与することができるが、非経口投与であってもよい。非経口剤として投与する場合は、溶液の状態、または分散剤、懸濁剤、安定剤などを添加した状態で、ハップ剤、ローション剤、軟膏剤、チンキ剤、クリーム剤などの剤形で適用することができる。 投与量は、投与方法、病状、患者の年齢等によって変化し得るが、大人で
は、通常、1日当たり有効成分として0.5〜1000mg、子供では通常0.5〜500mg程度投与することができる。 抗炎症剤等の配合比は、剤型によって適宜変更することが可能であるが、通常、経口または粘膜吸収により投与される場合は約0.3〜15.0wt%、非経口投与による場合は、0.01〜10wt%程度にするとよい。なお、投与量は種々の条件で異なるので、前記投与量より少ない量で十分な場合もあるし、また、範囲を超えて投与する必要のある場合もある。
The administration method of the anti-inflammatory agent and the like according to the present invention can be generally administered orally in the form of tablets, pills, soft / hard capsules, fine granules, powders, granules, liquids, etc. It may be administered parenterally. When administered as a parenteral agent, it can be applied in the form of a solution, or in the form of a haptic agent, lotion agent, ointment, tincture, cream, etc. with the addition of a dispersant, suspension, stabilizer, etc. can do. The dosage may vary depending on the administration method, medical condition, age of patient, etc., but for adults, it can be generally administered as 0.5 to 1000 mg as an active ingredient per day, and for children, about 0.5 to 500 mg can be usually administered. The mixing ratio of the anti-inflammatory agent and the like can be appropriately changed depending on the dosage form, but is usually about 0.3 to 15.0 wt% when administered orally or by mucosal absorption, and when administered parenterally. About 0.01 to 10 wt% is preferable. In addition, since the dose varies depending on various conditions, a dose smaller than the above dose may be sufficient, or it may be necessary to administer beyond the range.
本発明の本発明の抗炎症剤等は、皮膚外用剤(化粧品、医薬品および医薬部外品を含む。)として用いても、抗炎症効果を期待することができる。 本発明の抗炎症剤等を配合しうる皮膚外用剤の形態としては、例えば、乳液、石鹸、洗顔料、入浴剤、クリーム、乳液、化粧水、オーデコロン、ひげ剃り用クリーム、ひげ剃り用ローション、化粧油、日焼け・日焼け止めローション、おしろいパウダー、ファンデーション、香水、パック、爪クリーム、エナメル、エナメル除去液、眉墨、ほお紅、アイクリーム、アイシャドー、マスカラ、アイライナー、口紅、リップクリーム、シャンプー、リンス、染毛料、分散液、洗浄料等が挙げられる。 また、本発明の抗炎症剤等を配合しうる医薬品または医薬部外品の形態としては、軟膏剤、クリーム剤、外用液剤等が挙げられる。 The anti-inflammatory agent of the present invention of the present invention can be expected to have an anti-inflammatory effect even when used as a skin external preparation (including cosmetics, pharmaceuticals and quasi drugs). Examples of the form of the external preparation for skin to which the anti-inflammatory agent and the like of the present invention can be formulated include, for example, emulsion, soap, facial cleanser, bath preparation, cream, emulsion, lotion, eau de cologne, shaving cream, shaving lotion, Cosmetic oil, suntan / sunscreen lotion, powder, foundation, perfume, pack, nail cream, enamel, enamel remover, eyebrow, blusher, eye cream, eye shadow, mascara, eyeliner, lipstick, lip balm, shampoo, rinse , Hair dyes, dispersions, cleaning agents and the like. Examples of the form of pharmaceuticals or quasi drugs that can contain the anti-inflammatory agent of the present invention include ointments, creams, liquids for external use and the like.
上記形態の皮膚外用剤には、本発明による抗炎症剤等の他に、その抗炎症効果を損なわない範囲で化粧品、医薬部外品などの皮膚外用剤に配合される成分、油分、高級アルコール、脂肪酸、紫外線吸収剤、粉体、顔料、界面活性剤、多価アルコール・糖、高分子、生理活性成分、溶媒、酸化防止剤、香料、防腐剤等を配合することができる。 例を以下に羅列するが、本発明はこれらの例に限定されるものではない。 In addition to the anti-inflammatory agent according to the present invention, the external preparation for skin of the above form includes components, oils, and higher alcohols that are blended in external preparations for skin such as cosmetics and quasi-drugs as long as the anti-inflammatory effect is not impaired. Fatty acids, ultraviolet absorbers, powders, pigments, surfactants, polyhydric alcohols / sugars, polymers, physiologically active ingredients, solvents, antioxidants, fragrances, preservatives, and the like can be blended. Examples are listed below, but the present invention is not limited to these examples.
(1)油分の例エステル系の油相成分:トリ2-エチルヘキサン酸グリセリル、2-エチルヘキサン酸セチル、ミリスチン酸イソプロピル、ミリスチン酸ブチル、パルミチン酸イソプロピル、ステアリン酸エチル、パルミチン酸オクチル、イソステアリン酸イソセチル、ステアリン酸ブチル、ミリスチン酸ブチル、リノール酸エチル、リノール酸イソプロピル、オレイン酸エチル、ミリスチン酸イソセチル、ミリスチン酸イソステアリル、パルミチン酸イソステアリル、ミリスチン酸オクチルドデシル、イソステアリン酸イソセチル、セバシン酸ジエチル、アジピン酸ジイソプロピル、ネオペンタン酸イソアラキル、トリ(カプリル・カプリン酸)グリセリル、トリ2-エチルヘキサン酸トリメチロールプロパン、トリイソステアリン酸トリメチロールプロパン、テトラ2-エチルヘキサン酸ペンタエリスリトール、カプリル酸セチル、ラウリン酸デシル、ラウリン酸ヘキシル、ミリスチン酸デシル、ミリスチン酸ミリスチル、ミリスチン酸セチル、ステアリン酸ステアリル、オレイン酸デシル、リシノレイン酸セチル、ラウリン酸イソステアリル、ミリスチン酸イソトリデシル、ミリスチン酸イソセチル、ミリスチン酸イソステアリル、パルミチン酸イソセチル、パルミチン酸イソステアリル、ステアリン酸オクチル、ステアリン酸イソセチル、オレイン酸イソデシル、オレイン酸オクチルドデシル、リノール酸オクチルドデシル、イソステアリン酸イソプロピル、2-エチルヘキサン酸セトステアリル、2-エチルヘキサン酸ステアリル、イソステアリン酸ヘキシル、ジオクタン酸エチレングリコール、ジオレイン酸エチレングリコール、ジカプリン酸プロピレングリコール、ジ(カプリル・カプリン酸)プロピレングリコール、ジカプリル酸プロピレングリコール、ジカプリン酸ネオペンチルグリコール、ジオクタン酸ネオペンチルグリコール、トリカプリル酸グリセリル、トリウンデシル酸グリセリル、トリイソパルミチン酸グリセリル、トリイソステアリン酸グリセリル、ネオペンタン酸オクチルドデシル、オクタン酸イソステアリル、イソノナン酸オクチル、ネオデカン酸ヘキシルデシル、ネオデカン酸オクチルドデシル、イソステアリン酸イソセチル、イソステアリン酸イソステアリル、イソステアリン酸オクチルデシル、ポリグリセリンオレイン酸エステル、ポリグリセリンイソステアリン酸エステル、炭酸ジプロピル、炭酸ジアルキル(C12-18)、クエン酸トリイソセチル、クエン酸トリイソアラキル、クエン酸トリイソオクチル、乳酸ラウリル、乳酸ミリスチル、乳酸セチル、乳酸オクチルデシル、クエン酸トリエチル、クエン酸アセチルトリエチル、クエン酸アセチルトリブチル、クエン酸トリオクチル、リンゴ酸ジイソステアリル、ヒドロキシステアリン酸2-エチルヘキシル、コハク酸ジ2-エチルヘキシル、アジピン酸ジイソブチル、セバシン酸ジイソプロピル、セバシン酸ジオクチル、ステアリン酸コレステリル、イソステアリン酸コレステリル、ヒドロキシステアリン酸コレステリル、オレイン酸コレステリル、オレイン酸ジヒドロコレステリル、イソステアリン酸フィトステリル、オレイン酸フィトステリル、12-ステアロイルヒドロキシステアリン酸イソセチル、12-ステアロイルヒドロキシステアリン酸ステアリル、12-ステアロイルヒドロキシステアリン酸イソステアリル等が挙げられる。炭化水素系の油相成分:スクワラン、流動パラフィン、α-オレフィンオリゴマー、イソパラフィン、セレシン、パラフィン、流動イソパラフィン、ポリブテン、マイクロクリスタリンワックス、ワセリン等が挙げられる。動植物油とその硬化油、および天然由来のロウ:牛脂、硬化牛脂、豚脂、硬化豚脂、馬油、硬化馬油、ミンク油、オレンジラフィー油、魚油、硬化魚油、卵黄油等の動物油およびその硬化油、アボカド油、アルモンド油、オリーブ油、カカオ脂、キウイ種子油、杏仁油、ククイナッツ油、ゴマ油、小麦胚芽油、コメ胚芽油、コメヌカ油、サフラワー油、シアバター、大豆油、月見草油、シソ油、茶実油、ツバキ油、トウモロコシ油、ナタネ油、硬化ナタネ油、パーム核油、硬化パーム核油、パーム油、硬化パーム油、ピーナッツ油、硬化ピーナッツ油、ヒマシ油、硬化ヒマシ油、ヒマワリ油、ブドウ種子油、ホホバ油、硬化ホホバ油、マカデミアナッツ油、メドホーム油、綿実油、硬化綿実油、ヤシ油、硬化ヤシ油等の植物油およびその硬化油、ミツロウ、高酸価ミツロウ、ラノリン、還元ラノリン、硬化ラノリン、液状ラノリン、カルナバロウ、モンタンロウ等のロウ等が挙げられる。シリコーン系の油相成分:ジメチルポリシロキサン、メチルフェニルポリシロキサン、メチルシクロポリシロキサン、オクタメチルポリシロキサン、デカメチルポリシロキサン、ドデカメチルシクロシロキサン、メチルハイドロジェンポリシロキサン、ポリエーテル変性オルガノポリシロキサン、ジメチルシロキサン・メチルセチルオキシシロキサン共重合体、ジメチルシロキサン・メチルステアロキシシロキサン共重合体、アルキル変性オルガノポリシロキサン、末端変性オルガノポリシロキサン、アミノ変性シリコーン油、アミノ変性オルガノポリシロキサン、ジメチコノール、シリコーンゲル、アクリルシリコーン、トリメチルシロキシケイ酸、シリコーンRTVゴム等が挙げられる。フッ素系の油相成分:パーフルオロポリエーテル、フッ素変性オルガノポリシロキサン、フッ化ピッチ、フルオロカーボン、フルオロアルコール、フルオロアルキル・ポリオキシアルキレン共変性オルガノポリシロキサン等が挙げられる。 (1) Examples of oil components Ester-based oil phase components: glyceryl tri-2-ethylhexanoate, cetyl 2-ethylhexanoate, isopropyl myristate, butyl myristate, isopropyl palmitate, ethyl stearate, octyl palmitate, isostearic acid Isocetyl, butyl stearate, butyl myristate, ethyl linoleate, isopropyl linoleate, ethyl oleate, isocetyl myristate, isostearyl myristate, isostearyl palmitate, octyldodecyl myristate, isocetyl isostearate, diethyl sebacate, adipine Diisopropyl acid, isoaralkyl neopentanoate, glyceryl tri (capryl / caprate), trimethylolpropane tri-2-ethylhexanoate, trimethylol triisostearate Propane, pentaerythritol tetra-2-ethylhexanoate, cetyl caprylate, decyl laurate, hexyl laurate, decyl myristate, myristyl myristate, cetyl myristate, stearyl stearate, decyl oleate, cetyl ricinoleate, isolaurate Stearyl, isotridecyl myristate, isocetyl myristate, isostearyl myristate, isocetyl palmitate, isostearyl palmitate, octyl stearate, isocetyl stearate, isodecyl oleate, octyldodecyl linoleate, octyldodecyl isoleate, isopropyl isostearate Cetostearyl 2-ethylhexanoate, stearyl 2-ethylhexanoate, hexyl isostearate, ethyleneglycol dioctanoate , Ethylene glycol dioleate, propylene glycol dicaprate, propylene glycol di (capryl / capric acid), propylene glycol dicaprylate, neopentyl glycol dicaprate, neopentyl glycol dioctanoate, glyceryl tricaprylate, glyceryl triundecylate, triisopalmitine Glyceryl acid, glyceryl triisostearate, octyldodecyl neopentanoate, isostearyl octanoate, octyl isononanoate, hexyl decyl neodecanoate, octyldodecyl neodecanoate, isocetyl isostearate, isostearyl isostearate, octyldecyl isostearate, polyglycerin oleic acid Ester, polyglycerol isostearate, dipropyl carbonate, charcoal Dialkyl (C12-18), triisocetyl citrate, triisoaralkyl citrate, triisooctyl citrate, lauryl lactate, myristyl lactate, cetyl lactate, octyl decyl lactate, triethyl citrate, acetyl triethyl citrate, acetyl tributyl citrate, Trioctyl citrate, diisostearyl malate, 2-ethylhexyl hydroxystearate, di-2-ethylhexyl succinate, diisobutyl adipate, diisopropyl sebacate, dioctyl sebacate, cholesteryl stearate, cholesteryl isostearate, cholesteryl hydroxystearate, olein Cholesteryl acid, dihydrocholesteryl oleate, phytosteryl isostearate, phytosteryl oleate, 12-stearoyl hydroxystearate Cetyl, 12-stearoyl-hydroxystearic acid stearyl 12-stearoyl-hydroxystearic acid isostearate, and the like. Hydrocarbon oil phase components: squalane, liquid paraffin, α-olefin oligomer, isoparaffin, ceresin, paraffin, liquid isoparaffin, polybutene, microcrystalline wax, petrolatum and the like. Animal and vegetable oils and their hydrogenated oils, and naturally occurring waxes: beef tallow, hydrogenated beef tallow, lard, hydrogenated tallow, horse oil, hydrogenated horse oil, mink oil, orange luffy oil, fish oil, hydrogenated fish oil, egg yolk oil and other animal oils and Its hardened oil, avocado oil, almond oil, olive oil, cacao butter, kiwi seed oil, apricot oil, kukui nut oil, sesame oil, wheat germ oil, rice germ oil, rice bran oil, safflower oil, shea butter, soybean oil, evening primrose oil , Perilla oil, tea seed oil, camellia oil, corn oil, rapeseed oil, hydrogenated rapeseed oil, palm kernel oil, hydrogenated palm kernel oil, palm oil, hydrogenated palm oil, peanut oil, hydrogenated peanut oil, castor oil, hydrogenated castor oil , Vegetable oils such as sunflower oil, grape seed oil, jojoba oil, hardened jojoba oil, macadamia nut oil, medhome oil, cottonseed oil, hardened cottonseed oil, coconut oil, hardened coconut oil and its hardened , Beeswax, high acid value beeswax, lanolin, reduced lanolin, hydrogenated lanolin, liquid lanolin, carnauba wax and montan wax. Silicone oil phase components: dimethylpolysiloxane, methylphenylpolysiloxane, methylcyclopolysiloxane, octamethylpolysiloxane, decamethylpolysiloxane, dodecamethylcyclosiloxane, methylhydrogenpolysiloxane, polyether-modified organopolysiloxane, dimethyl Siloxane / methylcetyloxysiloxane copolymer, dimethylsiloxane / methylstearoxysiloxane copolymer, alkyl-modified organopolysiloxane, terminal-modified organopolysiloxane, amino-modified silicone oil, amino-modified organopolysiloxane, dimethiconol, silicone gel, acrylic Examples include silicone, trimethylsiloxysilicic acid, and silicone RTV rubber. Fluorine oil phase components: perfluoropolyether, fluorine-modified organopolysiloxane, fluorinated pitch, fluorocarbon, fluoroalcohol, fluoroalkyl / polyoxyalkylene co-modified organopolysiloxane, and the like.
(2)高級アルコールの例 ラウリルアルコール、ミリスチルアルコール、セチルアルコール、ステアリルアルコール、イソステアリルアルコール、オレイルアルコール、ベヘニルアルコール、2-エチルヘキサノール、ヘキサデシルアルコール、オクチルドデカノール等が挙げられる。 (2) Examples of higher alcohols Lauryl alcohol, myristyl alcohol, cetyl alcohol, stearyl alcohol, isostearyl alcohol, oleyl alcohol, behenyl alcohol, 2-ethylhexanol, hexadecyl alcohol, octyldodecanol and the like can be mentioned.
(3)脂肪酸の例 カプリル酸、カプリン酸、ウンデシレン酸、ラウリン酸、ミリスチン酸、パルミチン酸、パルミトレイン酸、ステアリン酸、イソステアリン酸、オレイン酸、リノール酸、リノレン酸、アラキン酸、アラキドン酸、ベヘン酸、エルカ酸、2-エチルヘキサン酸等が挙げられる。 (3) Examples of fatty acids Caprylic acid, capric acid, undecylenic acid, lauric acid, myristic acid, palmitic acid, palmitoleic acid, stearic acid, isostearic acid, oleic acid, linoleic acid, linolenic acid, arachidic acid, arachidonic acid, behenic acid , Erucic acid, 2-ethylhexanoic acid and the like.
(4)紫外線吸収剤の例 パラアミノ安息香酸、パラアミノ安息香酸アミル、パラアミノ安息香酸エチルジヒドロキシプロピル、パラアミノ安息香酸グリセリル、パラアミノ安息香酸エチル、パラアミノ安息香酸オクチル、パラアミノ安息香酸オクチルジメチル、サリチル酸エチレングリコール、サリチル酸オクチル、サリチル酸トリエタノールアミン、サリチル酸フェニル、サリチル酸ブチルフェニル、サリチル酸ベンジル、サリチル酸ホモメンチル、ケイ皮酸ベンジル、パラメトキシケイ皮酸オクチル、パラメトキシケイ皮酸2-エチルヘキシル、ジパラメトキシケイ皮酸モノ2-エチルヘキサン酸グリセリル、パラメトキシケイ皮酸イソプロピル、パラメトキシヒドロケイ皮酸ジエタノールアミン塩、ジイソプロピル・ジイソプロピルケイ皮酸エステル混合物、ウロカニン酸、ウロカニン酸エチル、ヒドロキシメトキシベンゾフェノン、ヒドロキシメトキシベンゾフェノンスルホン酸及びその塩、ジヒドロキシメトキシベンゾフェノン、ジヒドロキシメトキシベンゾフェノンジスルホン酸ナトリウム、ジヒドロキシベンゾフェノン、ジヒドロキシジメトキシベンゾフェノン、ヒドロキシオクトキシベンゾフェノン、テトラヒドロキシベンゾフェノン、ブチルメトキシジベンゾイルメタン、2、4、6-トリアニリノ-p-(カルボ-2-エチルヘキシル-1-オキシ)-1、3、5-トリアジン、2-(2-ヒドロキシ-5-メチルフェニル)ベンゾトリアゾール、メチル-O-アミノベンゾエート、2-エチルヘキシル-2-シアノ-3、3-ジフェニルアクリレート、フェニルベンゾイミダゾール硫酸、3-(4-メチルベンジリデン)カンフル、イソプロピルジベンゾイルメタン、4-(3、4-ジメトキシフェニルメチレン)-2、5-ジオキソ-1-イミダゾリジンプロピオン酸2-エチルヘキシル等、およびこれらの高分子誘導体やシラン誘導体等が挙げられる。 (4) Examples of UV absorbers Paraaminobenzoic acid, amyl paraaminobenzoate, ethyldihydroxypropyl paraaminobenzoate, glyceryl paraaminobenzoate, ethyl paraaminobenzoate, octyl paraaminobenzoate, octyldimethyl paraaminobenzoate, ethylene glycol salicylate, salicylic acid Octyl, triethanolamine salicylate, phenyl salicylate, butylphenyl salicylate, benzyl salicylate, homomenthyl salicylate, benzyl cinnamate, octyl paramethoxycinnamate, 2-ethylhexyl paramethoxycinnamate, mono-2-diparamethoxycinnamate Glyceryl ethylhexanoate, isopropyl paramethoxycinnamate, diethanolamine salt of paramethoxyhydrocinnamic acid, diisopropyl diisopropylcinnamic acid Ester mixture, urocanic acid, ethyl urocanate, hydroxymethoxybenzophenone, hydroxymethoxybenzophenonesulfonic acid and its salts, dihydroxymethoxybenzophenone, dihydroxymethoxybenzophenone sodium disulfonate, dihydroxybenzophenone, dihydroxydimethoxybenzophenone, hydroxyoctoxybenzophenone, tetrahydroxybenzophenone, Butylmethoxydibenzoylmethane, 2,4,6-trianilino-p- (carbo-2-ethylhexyl-1-oxy) -1,3,5-triazine, 2- (2-hydroxy-5-methylphenyl) benzotriazole , Methyl-O-aminobenzoate, 2-ethylhexyl-2-cyano-3, 3-diphenyl acrylate, phenylbenzimidazole sulfate, 3- (4-methylbenzylidene) carbonate Full, isopropyl dibenzoylmethane, 4- (3,4-dimethoxyphenyl methylene) 2-ethylhexyl-2,5-dioxo-1-imidazolidin propionate,, and polymer derivatives and silane derivatives thereof.
(5)粉体・顔料の例 赤色104号、赤色201号、黄色4号、青色1号、黒色401号等の色素、黄色4号ALレーキ、黄色203号BAレーキ等のレーキ色素、ナイロンパウダー、シルクパウダー、ウレタンパウダー、テフロン(登録商標)パウダー、シリコーンパウダー、ポリメタクリル酸メチルパウダー、セルロースパウダー、デンプン、シリコーンエラストマー球状粉体、ポリエチレン末等の高分子、黄酸化鉄、赤色酸化鉄、黒酸化鉄、酸化クロム、カーボンブラック、群青、紺青等の有色顔料、酸化亜鉛、酸化チタン、酸化セリウム等の白色顔料、タルク、マイカ、セリサイト、カオリン、板状硫酸バリウム等の体質顔料、雲母チタン等のパール顔料、硫酸バリウム、炭酸カルシウム、炭酸マグネシウム、珪酸アルミニウム、珪酸マグネシウム等の金属塩、シリカ、アルミナ等の無機粉体、ステアリン酸アルミニウム、ステアリン酸マグネシウム、パルミチン酸亜鉛、ミリスチン酸亜鉛、ミリスチン酸マグネシウム、ラウリン酸亜鉛、ウンデシレン酸亜鉛等の金属セッケン、ベントナイト、スメクタイト、窒化ホウ素等が挙げられる。これらの粉体の形状(球状、棒状、針状、板状、不定形状、燐片状、紡錘状等)および粒子径に特に制限はない。なおこれらの粉体は、従来公知の表面処理、例えばフッ素化合物処理、シリコーン処理、シリコーン樹脂処理、ペンダント処理、シランカップリング剤処理、チタンカップリング剤処理、油剤処理、N-アシル化リジン処理、ポリアクリル酸処理、金属セッケン処理、アミノ酸処理、レシチン処理、無機化合物処理、プラズマ処理、メカノケミカル処理等によって事前に表面処理されていてもいなくても構わない。 (5) Examples of powders and pigments Red 104, Red 201, Yellow 4, Blue 1, Black 401 and other dyes, Yellow 4 AL lake, Yellow 203 BA lake and other lake dyes, nylon powder , Silk powder, urethane powder, Teflon (registered trademark) powder, silicone powder, polymethyl methacrylate powder, cellulose powder, starch, silicone elastomer spherical powder, polyethylene powder, yellow iron oxide, red iron oxide, black Colored pigments such as iron oxide, chromium oxide, carbon black, ultramarine and bitumen, white pigments such as zinc oxide, titanium oxide and cerium oxide, extender pigments such as talc, mica, sericite, kaolin and barium sulfate plate, titanium mica Pearl pigments such as barium sulfate, calcium carbonate, magnesium carbonate, aluminum silicate, metal salts such as magnesium silicate, Inorganic powders such as silica and alumina, metal soap such as aluminum stearate, magnesium stearate, zinc palmitate, zinc myristate, magnesium myristate, zinc laurate, zinc undecylenate, bentonite, smectite, boron nitride, etc. It is done. There are no particular restrictions on the shape of these powders (spherical, rod-like, needle-like, plate-like, irregular shape, flake-like, spindle-like, etc.) and particle diameter. These powders are conventionally known surface treatments such as fluorine compound treatment, silicone treatment, silicone resin treatment, pendant treatment, silane coupling agent treatment, titanium coupling agent treatment, oil agent treatment, N-acylated lysine treatment, The surface treatment may or may not be performed in advance by polyacrylic acid treatment, metal soap treatment, amino acid treatment, lecithin treatment, inorganic compound treatment, plasma treatment, mechanochemical treatment or the like.
(6)界面活性剤の例アニオン性界面活性剤:脂肪酸セッケン、α-アシルスルホン酸塩、アルキルスルホン酸塩、アルキルアリルスルホン酸塩、アルキルナフタレンスルホン酸塩、アルキル硫酸塩、POEアルキルエーテル硫酸塩、アルキルアミド硫酸塩、アルキルリン酸塩、POEアルキルリン酸塩、アルキルアミドリン酸塩、アルキロイルアルキルタウリン塩、N-アシルアミノ酸塩、POEアルキルエーテルカルボン酸塩、アルキルスルホコハク酸塩、アルキルスルホ酢酸ナトリウム、アシル化加水分解コラーゲンペプチド塩、パーフルオロアルキルリン酸エステル等が挙げられる。カチオ
ン性界面活性剤:塩化アルキルトリメチルアンモニウム、塩化ステアリルトリメチルアンモニウム、臭化ステアリルトリメチルアンモニウム、塩化セトステアリルトリメチルアンモニウム、塩化ジステアリルジメチルアンモニウム、塩化ステアリルジメチルベンジルアンモニウム、臭化ベヘニルトリメチルアンモニウム、塩化ベンザルコニウム、塩化ベヘニン酸アミドプロピルジメチルヒドロキシプロピルアンモニウム、ステアリン酸ジエチルアミノエチルアミド、ステアリン酸ジメチルアミノプロピルアミド、ラノリン誘導体第四級アンモニウム塩等が挙げられる。両性界面活性剤:カルボキシベタイン型、アミドベタイン型、スルホベタイン型、ヒドロキシスルホベタイン型、アミドスルホベタイン型、ホスホベタイン型、アミノカルボン酸塩型、イミダゾリン誘導体型、アミドアミン型等が挙げられる。ノニオン性界面活性剤:プロピレングリコール脂肪酸エステル、グリセリン脂肪酸エステル、ポリグリセリン脂肪酸エステル、ソルビタン脂肪酸エステル、POEソルビタン脂肪酸エステル、POEソルビット脂肪酸エステル、POEグリセリン脂肪酸エステル、POEアルキルエーテル、POE脂肪酸エステル、POE硬化ヒマシ油、POEヒマシ油、POE・POP共重合体、POE・POPアルキルエーテル、ポリエーテル変性シリコーンラウリン酸アルカノールアミド、アルキルアミンオキシド、水素添加大豆リン脂質等が挙げられる。天然系界面活性剤:レシチン、サポニン、糖系界面活性剤等が挙げられる。
(6) Examples of surfactants Anionic surfactants: fatty acid soap, α-acyl sulfonate, alkyl sulfonate, alkyl allyl sulfonate, alkyl naphthalene sulfonate, alkyl sulfate, POE alkyl ether sulfate , Alkylamide sulfate, alkyl phosphate, POE alkyl phosphate, alkylamide phosphate, alkyloylalkyl taurine salt, N-acyl amino acid salt, POE alkyl ether carboxylate, alkyl sulfosuccinate, alkyl sulfoacetic acid Sodium, acylated hydrolyzed collagen peptide salt, perfluoroalkyl phosphate, etc. are mentioned. Cationic surfactant: alkyltrimethylammonium chloride, stearyltrimethylammonium chloride, stearyltrimethylammonium bromide, cetostearyltrimethylammonium chloride, distearyldimethylammonium chloride, stearyldimethylbenzylammonium chloride, behenyltrimethylammonium bromide, benzalkonium chloride , Behenic acid amidopropyldimethylhydroxypropylammonium chloride, stearic acid diethylaminoethylamide, stearic acid dimethylaminopropylamide, lanolin derivative quaternary ammonium salts, and the like. Amphoteric surfactants: carboxybetaine type, amide betaine type, sulfobetaine type, hydroxysulfobetaine type, amide sulfobetaine type, phosphobetaine type, aminocarboxylate type, imidazoline derivative type, amidoamine type and the like. Nonionic surfactant: propylene glycol fatty acid ester, glycerin fatty acid ester, polyglycerin fatty acid ester, sorbitan fatty acid ester, POE sorbitan fatty acid ester, POE sorbitol fatty acid ester, POE glycerin fatty acid ester, POE alkyl ether, POE fatty acid ester, POE cured castor Oil, POE castor oil, POE / POP copolymer, POE / POP alkyl ether, polyether-modified silicone lauric acid alkanolamide, alkylamine oxide, hydrogenated soybean phospholipid, and the like. Natural surfactant: lecithin, saponin, sugar surfactant and the like.
(7)多価アルコール、糖の例 エチレングリコール、ジエチレングリコール、ポリエチレングリコール、プロピレングリコール、ジプロピレングリコール、ポリプロピレングリコール、グリセリン、ジグリセリン、ポリグリセリン、3-メチル-1、3-ブタンジオール、1、3-ブチレングリコール、ソルビトール、マンニトール、ラフィノース、エリスリトール、グルコース、ショ糖、果糖、キシリトール、ラクトース、マルトース、マルチトール、トレハロース、アルキル化トレハロース、混合異性化糖、硫酸化トレハロース、プルラン等が挙げられる。またこれらの化学修飾体等も使用可能である。 (7) Examples of polyhydric alcohols and sugars Ethylene glycol, diethylene glycol, polyethylene glycol, propylene glycol, dipropylene glycol, polypropylene glycol, glycerin, diglycerin, polyglycerin, 3-methyl-1,3-butanediol, 1, 3 -Butylene glycol, sorbitol, mannitol, raffinose, erythritol, glucose, sucrose, fructose, xylitol, lactose, maltose, maltitol, trehalose, alkylated trehalose, mixed isomerized sugar, sulfated trehalose, pullulan and the like. These chemically modified compounds can also be used.
(8)高分子の例 アクリル酸エステル/メタクリル酸エステル共重合体(プラスサイズ、互応化学社製)、酢酸ビニル/クロトン酸共重合体(レジン28-1310、NSC社製)、酢酸ビニル/クロトン酸/ビニルネオデカネート共重合体(28-2930、NSC社製)、メチルビニルエーテルマレイン酸ハーフエステル(ガントレッツES、ISP社製)、T-ブチルアクリレート/アクリル酸エチル/メタクリル酸共重合体(ルビマー、BASF社製)、ビニルピロリドン/ビニルアセテート/ビニルプロピオネート共重合体(ルビスコールVAP、BASF社製)、ビニルアセテート/クロトン酸共重合体(ルビセットCA、BASF社製)、ビニルアセテート/クロトン酸/ビニルピロリドン共重合体(ルビセットCAP、BASF社製)、ビニルピロリドン/アクリレート共重合体(ルビフレックス、BASF社製)、アクリレート/アクリルアミド共重合体(ウルトラホールド、BASF社製)、ビニルアセテート/ブチルマレエート/イソボルニルアクリラート共重合体(アドバンテージ、ISP社製)、カルボキシビニルポリマー(カーボポール、BFGoodrich社製)、アクリル酸・メタクリル酸アルキル共重合体(ペミュレン、BF Goodrich社製)等のアニオン性高分子化合物や、ジアルキルアミノエチルメタクリレート重合体の酢酸両性化物(ユカフォーマー、三菱化学社製)、アクリル酸オクチルアクリルアミド/アクリル酸ヒドロキシプロピル/メタクリル酸ブチルアミノエチル共重合体(AMPHOMER、NSC社製)等の両性高分子化合物、ビニルピロリドン/ジメチルアミノエチルメタクリレートの4級化物(GAFQUAT、ISP社製)、メチルビニルイミダゾリウムクロリド/ビニルピロリドン共重合体(ルビコート、BASF社製)等のカチオン性高分子化合物、ポリビニルピロリドン(ルビスコールK、BASF社製)、ビニルピロリドン/酢酸ビニル共重合体(ルビスコールVA、BASF社製)、ビニルピロリドン/ジメチルアミノエチルメタクリレート共重合体(コポリマー937、ISP社製)、ビニルカプロラクタム/ビニルピロリドン/ジメチルアミノエチルメタクリレート共重合体(コポリマーVC713、ISP社製)等のノニオン性高分子化合物等がある。また、セルロースまたはその誘導体、ケラチン及びコラーゲンまたはその誘導体、アルギン酸カルシウム、プルラン、寒天、ゼラチン、タマリンド種子多糖類、キサンタンガム、カラギーナン、ハイメトキシルペクチン、ローメトキシルペクチン、グアーガム、アラビアゴム、結晶セルロース、アラビノガラクタン、カラヤガム、トラガカントガム、アルギン酸、アルブミン、カゼイン、カードラン、ジェランガム、デキストラン等の天然由来高分子化合物も好適に用いることができる。 (8) Examples of polymers Acrylic ester / methacrylic acid ester copolymer (plus size, manufactured by Kyoyo Chemical), vinyl acetate / crotonic acid copolymer (resin 28-1310, manufactured by NSC), vinyl acetate / croton Acid / vinyl neodecanate copolymer (28-2930, manufactured by NSC), methyl vinyl ether maleic acid half ester (Gantrez ES, manufactured by ISP), T-butyl acrylate / ethyl acrylate / methacrylic acid copolymer (rubymer) , BASF), vinyl pyrrolidone / vinyl acetate / vinyl propionate copolymer (Rubicol VAP, BASF), vinyl acetate / crotonic acid copolymer (Rubiset CA, BASF), vinyl acetate / croton Acid / vinyl pyrrolidone copolymer (Rubiset CAP, manufactured by BASF), vinyl pyrrolidone / acrylate copolymer (Rubiflex, B ASF), acrylate / acrylamide copolymer (Ultrahold, BASF), vinyl acetate / butyl maleate / isobornyl acrylate copolymer (Advantage, ISP), carboxy vinyl polymer (Carbopol, BF Goodrich), anionic polymer compounds such as acrylic acid / alkyl methacrylate copolymer (Pemulene, BF Goodrich), and acetic acid amphoteric products of dialkylaminoethyl methacrylate polymers (Yukaformer, Mitsubishi Chemical) Amphoteric polymer compounds such as octyl acrylate acrylate / hydroxypropyl acrylate / butylaminoethyl methacrylate copolymer (AMPHOMER, NSC), quaternized vinylpyrrolidone / dimethylaminoethyl methacrylate (GAFQUAT, ISP) , Methyl vinyl imidazolium black Cationic polymer compounds such as vinyl / vinylpyrrolidone copolymer (rubicoat, manufactured by BASF), polyvinylpyrrolidone (rubiscol K, manufactured by BASF), vinylpyrrolidone / vinyl acetate copolymer (rubiscol VA, manufactured by BASF) ), Nonionic polymer compounds such as vinylpyrrolidone / dimethylaminoethyl methacrylate copolymer (copolymer 937, manufactured by ISP), vinylcaprolactam / vinylpyrrolidone / dimethylaminoethyl methacrylate copolymer (copolymer VC713, manufactured by ISP), etc. There is. Cellulose or derivatives thereof, keratin and collagen or derivatives thereof, calcium alginate, pullulan, agar, gelatin, tamarind seed polysaccharide, xanthan gum, carrageenan, high methoxyl pectin, low methoxyl pectin, guar gum, gum arabic, crystalline cellulose, arabino Naturally derived polymer compounds such as galactan, gum karaya, gum tragacanth, alginic acid, albumin, casein, curdlan, gellan gum and dextran can also be suitably used.
(9)生理活性成分の例 生理活性成分としては、皮膚に塗布した場合に皮膚に何らかの生理活性を与える物質が挙げられる。例えば、美白成分、抗炎症剤等、老化防止剤、紫外線防御剤、スリミング剤、ひきしめ剤、抗酸化剤、発毛剤、育毛剤、保湿剤、血行促進剤、抗菌剤、殺菌剤、乾燥剤、冷感剤、温感剤、ビタミン類、アミノ酸、創傷治癒促進剤、刺激緩和剤、鎮痛剤、細胞賦活剤、酵素成分等が挙げられる。これらの好適な配合成分の例としては、例えばアシタバエキス、アボカドエキス、アマチャエキス、アルテアエキス、アルニカエキス、アロエエキス、アンズエキス、アンズ核エキス、イチョウエキス、ウイキョウエキス、ウコンエキス、ウーロン茶エキス、エイジツエキス、エチナシ葉エキス、オウゴンエキス、オウバクエキス、オウレンエキス、オオムギエキス、オトギリソウエキス、オドリコソウエキス、オランダカラシエキス、オレンジエキス、海水乾燥物、海藻エキス、加水分解エラスチン、加水分解コムギ末、加水分解シルク、カモミラエキス、カロットエキス、カワラヨモギエキス、甘草エキス、カルカデエキス、カキョクエキス、キナエキス、キューカンバ-エキス、グアノシン、クチナシエキス、クマザサエキス、クララエキス、クルミエキス、グレープフルーツエキス、クレマティスエキス、クロレラエキス、クワエキス、ゲンチアナエキス、紅茶エキス、酵母エキス、ゴボウエキス、コメヌカ発酵エキス、コメ胚芽油、コンフリーエキス、コラーゲン、コケモモエキス、サイシンエキス、サイコエキス、サイタイ抽出液、サルビアエキス、サボンソウエキス、ササエキス、サンザシエキス、サンショウエキス、シイタケエキス、ジオウエキス、シコンエキス、シソエキス、シナノキエキス、シモツケソウエキス、シャクヤクエキス、ショウブ根エキス、シラカバエキス、スギナエキス、セイヨウキズタエキス、セイヨウサンザシエキス、セイヨウニワトコエキス、セイヨウノコギリソウエキス、セイヨウハッカエキス、セ-ジエキス、ゼニアオイエキス、センキュウエキス、センブリエキス、ダイズエキス、タイソウエキス、タイムエキス、茶エキス、チョウジエキス、チガヤエキス、チンピエキス、トウキエキス、トウキンセンカエキス、トウニンエキス、トウヒエキス、ドクダミエキス、トマトエキス、納豆エキス、ニンジンエキス、ニンニクエキス、ノバラエキス、ハイビスカスエキス、バクモンドウエキス、パセリエキス、蜂蜜、ハマメリスエキス、パリエタリアエキス、ヒキオコシエキス、ビサボロール、ビワエキス、フキタンポポエキス、フキノトウエキス、ブクリョウエキス、ブッチャーブルームエキス、ブドウエキス、プロポリス、ヘチマエキス、ベニバナエキス、ペパーミントエキス、ボダイジュエキス、ボタンエキス、ホップエキス、マツエキス、マロニエエキス、ミズバショウエキス、ムクロジエキス、メリッサエキス、モモエキス、ヤグルマギクエキス、ユーカリエキス、ユキノシタエキス、ヨクイニンエキス、ヨモギエキス、ラベンダーエキス、リンゴエキス、レタスエキス、レモンエキス、レンゲソウエキス、ローズエキス、ローズマリーエキス、ローマカミツレエキス、ローヤルゼリーエキス等を挙げることができる。 また、デオキシリボ核酸、ムコ多糖類、ヒアルロン酸ナトリウム、コンドロイチン硫酸ナトリウム、コラーゲン、エラスチン、キチン、キトサン、加水分解卵殻膜などの生体高分子、アミノ酸、加水分解ペプチド、乳酸ナトリウム、尿素、ピロリドンカルボン酸ナトリウム、ベタイン、ホエイ、トリメチルグリシンなどの保湿成分、スフィンゴ脂質、セラミド、フィトスフィンゴシン、コレステロール、コレステロール誘導体、リン脂質などの油性成分、ε-アミノカプロン酸、グリチルリチン酸、β-グリチルレチン酸、塩化リゾチーム、グアイアズレン、ヒドロコールチゾン等の抗炎症剤等、ビタミンA、ビタミンB2、ビタミンB6、ビタミンC、ビタミンD、ビタミンE、パントテン酸カルシウム、ビオチン、ニコチン酸アミド、ビタミンCエステル等のビタミン類、アラントイン、ジイソプロピルアミンジクロロアセテート、4-アミノメチルシクロヘキサンカルボン酸等の活性成分、トコフェロール、カロチノイド、フラボノイド、タンニン、リグナン、サポニン等の抗酸化剤、α-ヒドロキシ酸、β-ヒドロキシ酸などの細胞賦活剤、γ-オリザノール、ビタミンE誘導体などの血行促進剤、レチノール、レチノール誘導体等の創傷治癒剤、アルブチン、コウジ酸、プラセンタエキス、イオウ、エラグ酸、リノール酸、トラネキサム酸、グルタチオン等の美白剤、セファランチン、カンゾウ抽出物、トウガラシチンキ、ヒノキチオール、ヨウ化ニンニクエキス、塩酸ピリドキシン、DL-α-トコフェロール、酢酸DL-α-トコフェロール、ニコチン酸、ニコチン酸誘導体、パントテン酸カルシウム、D-パントテニルアルコール、アセチルパントテニルエチルエーテル、ビオチン、アラントイン、イソプロピルメチルフェノール、エストラジオール、エチニルエストラジオール、塩化カプロニウム、塩化ベンザルコニウム、塩酸ジフェンヒドラミン、タカナール、カンフル、サリチル酸、ノニル酸バニリルアミド、ノナン酸バニリルアミド、ピロクトンオラミン、ペンタデカン酸グリセリル、L-メントール、モノニトログアヤコール、レゾルシン、γ-アミノ酪酸、塩化ベンゼトニウム、塩酸メキシレチン、オーキシン、女性ホルモン、カンタリスチンキ、シクロスポリン、ジンクピリチオン、ヒドロコールチゾン、ミノキシジル、モノステアリン酸ポリオキシエチレンソルビタン、ハッカ油、ササニシキエキス等の育毛剤などが挙げられる。 (9) Examples of physiologically active ingredients Examples of physiologically active ingredients include substances that impart some physiological activity to the skin when applied to the skin. For example, whitening ingredients, anti-inflammatory agents, anti-aging agents, UV protection agents, slimming agents, tanning agents, antioxidants, hair growth agents, hair restorers, moisturizers, blood circulation promoters, antibacterial agents, bactericides, desiccants , A cooling sensation agent, a warming sensation agent, vitamins, amino acids, a wound healing promoter, a stimulus relaxation agent, an analgesic agent, a cell activator, an enzyme component, and the like. Examples of these suitable ingredients include, for example, ashitaba extract, avocado extract, amateur extract, altea extract, arnica extract, aloe extract, apricot extract, apricot kernel extract, ginkgo biloba extract, fennel extract, turmeric extract, oolong tea extract, ages Extract, Echinacea leaf extract, Ogon extract, Oat extract, Oen extract, Barley extract, Hypericum extract, Oyster extract, Dutch mustard extract, Orange extract, Seawater dried product, Seaweed extract, Hydrolyzed elastin, Hydrolyzed wheat powder, Hydrolyzed silk , Chamomile extract, Carrot extract, Kawara mugwort extract, Licorice extract, Calcade extract, Oyster extract, Kina extract, Cucumber extract, Guanosine, Gardenia extract, Kumazasa extract, Clarae Kiss, walnut extract, grapefruit extract, clematis extract, chlorella extract, mulberry extract, gentian extract, tea extract, yeast extract, burdock extract, fermented rice bran extract, rice germ oil, comfrey extract, collagen, bilberry extract, saicin extract, psycho extract Extract Kizuta extract, hawthorn extract, elderberry extract, yarrow extract, mint extract, sage extract, mallow extract, senki Sue extract, assembly extract, soybean extract, tiso extract, thyme extract, tea extract, clove extract, chigaya extract, chimpi extract, touki extract, toshinsen extract, tonin extract, spruce extract, dokudami extract, tomato extract, natto extract, carrot extract, garlic extract, Novara extract, hibiscus extract, bacmond extract, parsley extract, honey, hamamelis extract, parietalia extract, toad extract, bisabolol, loquat extract, dandelion extract, burdock extract, bukuro extract, butcher bloom extract, grape extract, propolis, loofah extract, Safflower extract, peppermint extract, bodaige extract, button extract, hop extract, pine extract, marronnier extract, mizubasho Kiss, Mukuroji extract, Melissa extract, Peach extract, Cornflower extract, Eucalyptus extract, Yukinoshita extract, Yokuinin extract, Artemisia extract, Lavender extract, Apple extract, Lettuce extract, Lemon extract, Lotus root extract, Rose extract, Rosemary extract, Roman chamomile extract And royal jelly extract. Biopolymers such as deoxyribonucleic acid, mucopolysaccharide, sodium hyaluronate, sodium chondroitin sulfate, collagen, elastin, chitin, chitosan, hydrolyzed eggshell membranes, amino acids, hydrolyzed peptides, sodium lactate, urea, sodium pyrrolidonecarboxylate , Moisturizing ingredients such as betaine, whey, trimethylglycine, oily ingredients such as sphingolipid, ceramide, phytosphingosine, cholesterol, cholesterol derivatives, phospholipids, ε-aminocaproic acid, glycyrrhizic acid, β-glycyrrhetinic acid, lysozyme chloride, guaiazulene, Anti-inflammatory agents such as hydrocortisone, vitamin A, vitamin B2, vitamin B6, vitamin C, vitamin D, vitamin E, calcium pantothenate, biotin, nicotinamide, vitamin C ester Vitamins, active ingredients such as allantoin, diisopropylamine dichloroacetate, 4-aminomethylcyclohexanecarboxylic acid, antioxidants such as tocopherol, carotenoid, flavonoid, tannin, lignan, saponin, α-hydroxy acid, β-hydroxy acid, etc. Cell activators, blood circulation promoters such as γ-oryzanol and vitamin E derivatives, wound healing agents such as retinol and retinol derivatives, arbutin, kojic acid, placenta extract, sulfur, ellagic acid, linoleic acid, tranexamic acid, glutathione, etc. Whitening agent, cephalanthin, licorice extract, red pepper tincture, hinokitiol, garlic iodide extract, pyridoxine hydrochloride, DL-α-tocopherol, DL-α-tocopherol acetate, nicotinic acid, nicotinic acid derivative, calcium pantothenate, D-pan Tothenyl alcohol, acetyl pantothenyl ethyl ether, biotin, allantoin, isopropylmethylphenol, estradiol, ethinyl estradiol, capronium chloride, benzalkonium chloride, diphenhydramine hydrochloride, takanal, camphor, salicylic acid, nonyl acid vanillylamide, nonanoic acid vanillylamide, pyroctone Olamine, glyceryl pentadecanoate, L-menthol, mononitroguaiacol, resorcin, γ-aminobutyric acid, benzethonium chloride, mexiletine hydrochloride, auxin, female hormone, cantalis tincture, cyclosporine, zinc pyrithione, hydrocortisone, minoxidil, monostearic acid Examples include hair growth agents such as polyoxyethylene sorbitan, mint oil, and Sasanishiki extract.
(10)酸化防止剤の例 亜硫酸水素ナトリウム、亜硫酸ナトリウム、エリソルビン酸、エリソルビン酸ナトリウム、チオジプロピオン酸ジラウリル、トコフェロール、トリルビグアナイド、ノルジヒドログアヤレチン酸、パラヒドロキシアニソール、ブチルヒドロキシアニソール、ジブチルヒドロキシトルエン、ステアリン酸アスコルビル、パルミチン酸アスコルビル、没食子酸オクチル、没食子酸プロピル、カロチノイド、フラボノイド、タンニン、リグナン、サポニン、リンゴエキスやチョウジエキスなどの酸化防止効果の認められる植物エキス等が挙げられる。 (10) Examples of antioxidants Sodium bisulfite, sodium sulfite, erythorbic acid, sodium erythorbate, dilauryl thiodipropionate, tocopherol, tolyl biguanide, nordihydroguaiaretic acid, parahydroxyanisole, butylhydroxyanisole, dibutylhydroxy Examples include plant extracts having an antioxidant effect such as toluene, ascorbyl stearate, ascorbyl palmitate, octyl gallate, propyl gallate, carotenoid, flavonoid, tannin, lignan, saponin, apple extract and clove extract.
(11)溶媒の例 精製水、エタノール、低級アルコール、エーテル類、LPG、フルオロカーボン、N-メチルピロリドン、フルオロアルコール、揮発性直鎖状シリコーン、次世代フロン等が挙げられる。 (11) Examples of solvents Purified water, ethanol, lower alcohol, ethers, LPG, fluorocarbon, N-methylpyrrolidone, fluoroalcohol, volatile linear silicone, next-generation chlorofluorocarbon and the like.
本発明の抗炎症剤等は、急性炎症試験(Whittle試験法)において、writhingへの抑制作用を有する。これにより、鎮痛作用を有することが判る。更に、色素漏出を抑制するので、急性炎症に対する抗炎症作用を有することが判る。 更に、本発明の抗炎症剤等は、LPS刺激によるRAW264.7細胞のPGE2産生への抑制作用を有する。これにより、本発明の抗炎症剤等は、抗炎症作用を有することが判る。また、本発明の抗炎症剤等は、多くの国で食されているキウイ種子から抽出されたものである。従って、天然由来の安全な抗炎症剤等を提供することができる。 The anti-inflammatory agent or the like of the present invention has an inhibitory effect on writing in an acute inflammation test (White test method). Thereby, it turns out that it has an analgesic effect. Furthermore, since pigment | dye leakage is suppressed, it turns out that it has an anti-inflammatory action with respect to acute inflammation. Furthermore, the anti-inflammatory agent and the like of the present invention have an inhibitory action on PGE 2 production of RAW264.7 cells by LPS stimulation. Thereby, it turns out that the anti-inflammatory agent etc. of this invention have an anti-inflammatory action. Further, the anti-inflammatory agent and the like of the present invention are extracted from kiwi seeds eaten in many countries. Accordingly, it is possible to provide a naturally occurring safe anti-inflammatory agent and the like.
以下、抗炎症剤等を実施例に基づいて具体的に説明する。尚、本発明は、下記実施例に限定されない。 The anti-inflammatory agent and the like will be specifically described below based on examples. The present invention is not limited to the following examples.
実施例1:キウイ種子抽出物の製造本実施例のキウイ種子抽出物を以
下の方法にて製造した。 原料としてキウイ種子は、中国産のものを用いた。まず、キウイ種子を圧搾して油分を分離し、圧搾物1kgを得た。この圧搾物1kgを破砕し、N−ヘキサンで還流し、圧搾物に残存する油分を除いて脱脂物とした。次いで、この脱脂物をエタノール濃度70wt%の含水エタノール80℃で3時間抽出し、エタノール抽出液を乾固させてキウイ種子抽出物(実施例)20gを得た。
Example 1 Production of Kiwi Seed Extract The kiwi seed extract of this example was produced by the following method. Kiwi seeds were used as raw materials from China. First, kiwi seeds were squeezed to separate the oil, and 1 kg of squeezed product was obtained. 1 kg of this pressed product was crushed and refluxed with N-hexane, and the oil remaining in the pressed product was removed to obtain a defatted product. Subsequently, this defatted product was extracted at 80 ° C. with hydrous ethanol having an ethanol concentration of 70 wt% for 3 hours, and the ethanol extract was dried to obtain 20 g of kiwi seed extract (Example).
実施例2:クエルシトリンの製造
上記キウイ種子抽出物から以下の条件にてHPLCでクエルシトリンを分離した。
(HPLC条件)
検出器:紫外分光光度計,測定波長256nm
カラム:GLサイエンス社イナートシルC18,φ9.0×250mm
移動相:40%メタノール
流速:2.5mL/min
Example 2 Production of Quercitrin Quercitrin was separated from the kiwi seed extract by HPLC under the following conditions.
(HPLC conditions)
Detector: UV spectrophotometer, measurement wavelength 256nm
Column: GL Sciences Inert Sil C18, φ9.0 × 250mm
Mobile phase: 40% methanol Flow rate: 2.5 mL / min
実施例3:ケンフェロール3‐O‐ラムノシドの製造
上記ケンフェロール3‐O‐ラムノシドは、上記クエルシトリンと同様にしてHPLCを用いて実施例1のキウイ種子抽出物から分離した。
Example 3: Preparation of kaempferol 3-O-rhamnoside The kaempferol 3-O-rhamnoside was separated from the kiwi seed extract of Example 1 using HPLC in the same manner as quercitrin.
試験例1:Writhingモデル(抗急性炎症試験)(1)実験材料 実施例1のキウイ種子抽出物(brix)(以下、試験例1においては、「KSE」という。)および甘草抽出物(以下、単に「GE」という。)を用いた。5w−6wのddy系雄性マウスを一群11匹として実験を行った。 Test Example 1: Writhing Model (Anti-Acute Inflammation Test) (1) Experimental Material Kiwi seed extract (brix) of Example 1 (hereinafter referred to as “KSE” in Test Example 1) and licorice extract (hereinafter referred to as “Kisse”) Simply “GE”). The experiment was conducted using 5 male and 6 male male mice of 5w-6w as 11 groups.
(2)試験方法 試験法としては、Whittle法を用いた。即ち、KSEおよびGEをそれぞれ蒸留水に懸濁してサンプルとした。サンプルをそれぞれの投与量(100、200および400mg/kg)でマウスに経口投与(P.O.)し、その55分後に2% pontamine sky blueを尾静脈注射(i.v.)により10mL/kgで投与した。その5分後に1%酢酸を10mL/kgで腹腔注射(i.p.)により投与した。1%酢酸を投与してから15分間のwrithing数を測定した。その結果を図1に示す。 2% pontamine sky blueを投与してから、20分後に頚髄脱臼をし、すぐに腹腔を開いて、10mLの生理食塩水で腹腔をよく洗い、その洗浄液を脱脂綿で濾過後収集して、0.1mLの1N NaOH水溶液を添加した。さらに、生理食塩水で12mLにメスアップした。分光光度計を用いて590nmにて吸光度を測定し、腹腔内漏出色素量を算出した。その結果を図2に示す。 (2) Test method As a test method, the White method was used. That is, KSE and GE were each suspended in distilled water and used as samples. Samples were orally administered (PO) to mice at respective doses (100, 200 and 400 mg / kg) and 55 minutes later, 2% pontamine blue was injected by tail vein injection (iv) at 10 mL / Administered in kg. Five minutes later, 1% acetic acid was administered at 10 mL / kg by intraperitoneal injection (ip). The number of writings for 15 minutes after the administration of 1% acetic acid was measured. The result is shown in FIG. After administration of 2% pontine sky blue, cervical spinal dislocation was performed 20 minutes later, the abdominal cavity was immediately opened, the abdominal cavity was washed thoroughly with 10 mL of physiological saline, and the washings were collected by filtration with absorbent cotton and collected. 1 mL of 1N aqueous NaOH was added. Further, the volume was made up to 12 mL with physiological saline. Absorbance was measured at 590 nm using a spectrophotometer, and the amount of dye leaked into the peritoneal cavity was calculated. The result is shown in FIG.
(3)結果実験の結果、KSEは、100〜400mg/kg投与群において、controlと比べて、writhingへの抑制傾向が認められたが有意差はみられなかった。一方、GEは100〜400mg/kg投与群においてwrithingへの抑制作用は認められなかった(図1)。 酢酸による血管透過性増加への作用において、KSEは100〜400mg/kg投与群において、Controlと比べて、有意に色素漏出を抑制した(p<0.05)。また、GEも100〜400mg/kg投与群において、controlと比べて、有意に色素漏出を抑制した(p<0.01)(図2)。KSEとGEを比較すると、writhingへの抑制作用(鎮痛作用)はKSEが強かったが、抗炎症作用(色素漏出量)は僅かにGEが強くなった。しかし、KSEとGEとのいずれの群間でも有意差はみられなかった。 (3) Results As a result of the experiment, KSE showed a tendency to suppress to writing compared with control in the 100 to 400 mg / kg administration group, but no significant difference was observed. On the other hand, GE showed no inhibitory effect on writing in the 100-400 mg / kg administration group (FIG. 1). In the effect of acetic acid on the increase in vascular permeability, KSE significantly suppressed pigment leakage in the 100 to 400 mg / kg administration group compared to Control (p <0.05). In addition, GE also significantly suppressed pigment leakage in the 100 to 400 mg / kg administration group as compared to control (p <0.01) (FIG. 2). When KSE and GE were compared, KSE was strong in the inhibitory action (analgesic action) on writing, but GE was slightly stronger in the anti-inflammatory action (pigment leakage). However, there was no significant difference between any groups of KSE and GE.
(4)効果 以上の結果から、KSEは酢酸による引き起こすマウス急性炎症に対する鎮痛、抗炎症効果を有することが確認された。また、抗炎症作用が強いと報告されているGEと比較した結果、鎮痛作用はKSEが強く抑制する傾向がみられた。また、色素漏出抑制作用では僅かにKSEが劣るものの、GEとの有意差はみられなかったので、キウイ種子抽出物の抗炎症作用も強いと考えられる。 (4) Effect From the above results, it was confirmed that KSE has an analgesic and anti-inflammatory effect on mouse acute inflammation caused by acetic acid. In addition, as a result of comparison with GE, which is reported to have a strong anti-inflammatory effect, KSE strongly suppressed the analgesic action. Moreover, although KSE was slightly inferior in the pigment leakage inhibitory action, no significant difference from GE was observed, so it is considered that the anti-inflammatory action of the kiwi seed extract is also strong.
試験例2−1:細胞RAW264.7におけるLPS刺激によるPGE2産生に及ぼす作用の測定(実施例1)(1)試験方法 マウス由来のマクロファージ様細胞RAW264.7を0.1mM非必須アミノ酸混合物、10%牛胎児血清(FCS)、ペニシリン(100units/mL)およびストレプトマイシン(100μg/mL)を含有するMinimum Essential Medium(MEM)培地に1×106 cells/mLの濃度でサスペンドし、48穴プレートに200μLずつ播種した。 Test Example 2-1: Measurement of an effect on PGE 2 production by LPS stimulation in cell RAW264.7 (Example 1) (1) Test method A mouse-derived macrophage-like cell RAW264.7 was mixed with a 0.1 mM non-essential amino acid mixture, Suspend at a concentration of 1 × 10 6 cells / mL in Minimum Essential Medium (MEM) medium containing 10% fetal calf serum (FCS), penicillin (100 units / mL) and streptomycin (100 μg / mL), and in a 48-well plate 200 μL each was seeded.
48〜72時間培養した後、培地を吸引により取り除いた。無血清培地(FCSを入れていない培地)で3回洗浄後、新たに無血清培地160μLを各ウェルに加えた。その後、100μg/mLに調整したLPS溶液を20μL加えた(終濃度10μg/mL)。さらに、各濃度に調製した実施例1のキウイ種子抽出物サンプル液および10μg/mL濃度のIndomethacinを20μLずつ加えた(キウイ種子抽出物終濃度1、3、10、30及び100μg/mL、Indomethacin終濃度1μg/mL)。Non(LPS−)のウェルには無血清培地(180μL)および媒体(20μL)を加えた。 After culturing for 48 to 72 hours, the medium was removed by aspiration. After washing 3 times with serum-free medium (medium without FCS), 160 μL of serum-free medium was newly added to each well. Then, 20 μL of LPS solution adjusted to 100 μg / mL was added (final concentration 10 μg / mL). Furthermore, 20 μL each of the kiwi seed extract sample solution prepared in Example 1 and 10 μg / mL concentration of Indomethacin were added to each concentration (kiwi seed extract final concentrations 1, 3, 10, 30 and 100 μg / mL, Indomethacin end concentration. Concentration 1 μg / mL). Serum-free medium (180 μL) and vehicle (20 μL) were added to Non (LPS-) wells.
そして、20時間培養し、その後、培養上清を収集して、培養上清中のPGE2濃度を測定した。PGE2の測定は、Prostaglandin E2 EIA Kit−Monoclonalに添付していた説明書にしたがって行った。その結果を図3に示す。尚、図3において、Ind.1は、Indomethacin終濃度1μg/mLのことである。 Then, cultured for 20 hours, then collect the culture supernatant was measured PGE 2 concentration in the culture supernatant. PGE 2 was measured according to the instructions attached to Prostaglandin E2 EIA Kit-Monoclonal. The result is shown in FIG. In FIG. 3, Ind. 1 is the final concentration of Indomethacin 1 μg / mL.
(2)結果 図3によれば、キウイ種子抽出物は、1〜100μg/mLの濃度において、LPS刺激によるRAW264.7細胞のPGE2産生への抑制作用を認めた。ここで、Control(LPS+)群に対する抑制率は、キウイ種子エキス1、3、10、30、100μg/mLにおいて、各々30.4%、65.7%、44.8%、40.3%、49.8%であり、また、Indomethacin(1μg/mL)では、90.2%であった。このとき、Control(LPS+)群と比べて、キウイ種子抽出物1μg/mLの濃度において、p<0.05、3〜100μg/mLの濃度において、p<0.01の有意差がみられた。また、Indomethacinにも有意差がみられた(p<0.01)。(3)効果 これにより、キウイ種子抽出物は、1〜100μg/mLの濃度において、LPS刺激によるRAW264.7細胞のPGE2産生への抑制作用を有することが確認された。それで、抗炎症作用の一つのメカニズムとして、キウイ種子抽出物が、2型のシクロオキシゲナーゼ(COX2)の活性を阻害し、炎症因子PGE2の産生を抑制したことによるものと考えられる。 (2) Results According to FIG. 3, the kiwi seed extract showed an inhibitory action on PGE 2 production of RAW264.7 cells by LPS stimulation at a concentration of 1 to 100 μg / mL. Here, the suppression rate for the Control (LPS +) group was 30.4%, 65.7%, 44.8%, 40.3%, respectively, in the kiwi seed extract 1, 3, 10, 30, 100 μg / mL. It was 49.8%, and that of Indomethacin (1 μg / mL) was 90.2%. At this time, as compared with the Control (LPS +) group, a significant difference of p <0.01 was observed at a concentration of 1 μg / mL of kiwi seed extract, and p <0.05 at a concentration of 3 to 100 μg / mL. . There was also a significant difference in Indomethacin (p <0.01). (3) Effect Thereby, it was confirmed that the kiwi seed extract has an inhibitory action on PGE 2 production of RAW264.7 cells by LPS stimulation at a concentration of 1 to 100 μg / mL. So, as one of the mechanisms of anti-inflammatory action, kiwi seed extract, inhibit the activity of type 2 cyclooxygenase (COX2), it is believed to be due to inhibited production of inflammatory factor PGE 2.
試験例2−2:細胞RAW264.7におけるLPS刺激によるPGE2産生に及ぼす作用の測定(実施例2及び実施例3)(1)試験方法 上記試験例2−1と同様の方法にて、実施例2のクエルシトリンのサンプル及び実施例3のケンフェロール3‐O‐ラムノシドのサンプルで終濃度10、30および100μg/mLにて、それぞれ測定した。実施例2及び実施例3の測定結果からコントロールに対するPEG2産生の抑制率を算出した。その結果を下記表1に示す。 Test Example 2-2: Measurement of the effect on the PGE 2 production by LPS stimulation in the cell RAW264.7 (Example 2 and Example 3) (1) Test method The test method was carried out in the same manner as in Test Example 2-1. The quercitrin sample of Example 2 and the kaempferol 3-O-rhamnoside sample of Example 3 were measured at final concentrations of 10, 30 and 100 μg / mL, respectively. From the measurement results of Example 2 and Example 3, the inhibition rate of PEG 2 production relative to the control was calculated. The results are shown in Table 1 below.
(2)結果
上記表1の結果、クエルシトリン(10〜100g/mL)およびケンフェロール3‐O‐ラムノシド(10〜100g/mL)は、LPS刺激によるRAW264.7細胞のPGE2産生への抑制作用を認めた。また、Control(LPS+)群と比べて、ケンフェロール3‐O‐ラムノシド(100g/mL)及びクエルシトリン(100g/mL)において、有意差がみられた(p<0.01)。
(2) Results As a result of Table 1 above, quercitrin (10 to 100 g / mL) and kaempferol 3-O-rhamnoside (10 to 100 g / mL) were suppressed to PGE 2 production of RAW264.7 cells by LPS stimulation. The effect was recognized. Moreover, compared with the Control (LPS +) group, a significant difference was observed in kaempferol 3-O-rhamnoside (100 g / mL) and quercitrin (100 g / mL) (p <0.01).
(3)効果
以上の結果から、ケンフェロール3‐O‐ラムノシドおよびクエルシトリンは、炎症因子PGE2の産生を抑制することが認められた。これにより、キウイ種子エキスの抗炎症作用に、これらの成分が関与していることが判る。また、ケンフェロール3‐O‐ラムノシドは、30〜100g/mLの濃度において急激にPGE2の産生を抑制するのに対し、クエルシトリンは10〜100g/mLの濃度において緩やかにPGE2の産生を抑制する傾向が認められた。
(3) Effect As a result, kaempferol 3-O-rhamnoside and quercitrin, it was found to inhibit the production of inflammatory factor PGE 2. Thereby, it turns out that these components are concerned in the anti-inflammatory action of kiwi seed extract. Kaempferol 3-O-rhamnoside rapidly suppresses the production of PGE 2 at a concentration of 30 to 100 g / mL, whereas quercitrin slowly increases the production of PGE 2 at a concentration of 10 to 100 g / mL. A tendency to suppress was observed.
〔配合例〕
以下に本発明の抗炎症剤等(キウイ種子抽出物)の配合例を挙げるが、下記配合例は本発明を限定するものではない。
配合例1:チューインガム
砂糖 53.0wt%
ガムベース 20.0
グルコース 10.0
水飴 16.0
香料 0.5
キウイ種子抽出物 0.5
100.0wt%
[Example of formulation]
Although the compounding example of the anti-inflammatory agent etc. (kiwi seed extract) of this invention is given to the following, the following compounding example does not limit this invention.
Formulation Example 1: Chewing gum
53.0wt% sugar
Gum base 20.0
Glucose 10.0
Minamata 16.0
Fragrance 0.5
Kiwi seed extract 0.5
100.0wt%
配合例2:グミ
還元水飴 40.0wt%
グラニュー糖 20.0
ブドウ糖 20.0
ゼラチン 4.7
水 9.68
キウイ果汁 4.0
キウイフレーバー 0.6
色素 0.02
キウイ種子抽出物 1.0
100.0wt%
Formulation Example 2: Gummy
Reduced water tank 40.0wt%
Granulated sugar 20.0
Glucose 20.0
Gelatin 4.7
Water 9.68
Kiwi juice 4.0
Kiwi flavor 0.6
Dye 0.02
Kiwi seed extract 1.0
100.0wt%
配合例3:キャンディー
砂糖 50.0wt%
水飴 33.0
水 14.4
有機酸 2.0
香料 0.2
キウイ種子抽出物 0.4
100.0wt%
Formulation Example 3: Candy
50.0 wt% sugar
Minamata 33.0
Water 14.4
Organic acid 2.0
Fragrance 0.2
Kiwi seed extract 0.4
100.0wt%
配合例4:ヨーグルト(ハード・ソフト)
牛乳 41.5wt%
脱脂粉乳 5.8
砂糖 8.0
寒天 0.15
ゼラチン 0.1
乳酸菌 0.005
キウイ種子抽出物 0.4
香料 微量
水 残余
100.0wt%
Formulation Example 4: Yogurt (hard / soft)
Milk 41.5wt%
Nonfat dry milk 5.8
Sugar 8.0
Agar 0.15
Gelatin 0.1
Lactic acid bacteria 0.005
Kiwi seed extract 0.4
Perfume
Water residue
100.0 wt%
配合例5:ソフトカプセル
キウイ種子油 87.0wt%
乳化剤 12.0
キウイ種子抽出物 1.0
100.0wt%
Formulation Example 5: Soft capsule
Kiwi seed oil 87.0wt%
Emulsifier 12.0
Kiwi seed extract 1.0
100.0wt%
配合例6:清涼飲料
果糖ブドウ糖液糖 30.0wt%
乳化剤 0.5
キウイ種子抽出物 0.05
香料 適量
精製水 残余
100.0wt%
Formulation Example 6: Soft drink
Fructose glucose liquid sugar 30.0wt%
Emulsifier 0.5
Kiwi seed extract 0.05
Perfume
Purified water residue
100.0 wt%
配合例7:錠剤
乳糖 54.0wt%
結晶セルロース 30.0
澱粉分解物 10.0
グリセリン脂肪酸エステル 5.0
キウイ種子抽出物 1.0
100.0wt%
Formulation Example 7: Tablet
Lactose 54.0wt%
Crystalline cellulose 30.0
Starch degradation product 10.0
Glycerin fatty acid ester 5.0
Kiwi seed extract 1.0
100.0 wt%
配合例8:錠菓
砂糖 76.4wt%
グルコース 19.0
ショ糖脂肪酸エステル 0.2
キウイ種子抽出物 0.5
精製水 3.9
100.0wt%
Formulation Example 8: Tablet
76.4 wt% sugar
Glucose 19.0
Sucrose fatty acid ester 0.2
Kiwi seed extract 0.5
Purified water 3.9
100.0 wt%
配合例9:化粧クリーム
スクワラン 20.0wt%
ミツロウ 5.0
精製ホホバ油 5.0
グリセリン 5.0
グリセリンモノステアレート 2.0
ポリオキシエチレン(20)ソルビタン-
モノステアレート 2.0
キウイ種子抽出物 2.0
防腐剤 適量
香料 適量
精製水 残余
100.0wt%
Formulation Example 9: Cosmetic cream
Squalane 20.0wt%
Beeswax 5.0
Refined jojoba oil 5.0
Glycerin 5.0
Glycerol monostearate 2.0
Polyoxyethylene (20) sorbitan-
Monostearate 2.0
Kiwi seed extract 2.0
Preservative appropriate amount
Perfume
Purified water residue
100.0wt%
配合例10:化粧水
エタノール 5.0wt%
グリセリン 2.0
1,3−ブチレングリコール
2.0
ポリエチレンオレイルエーテル 0.5
クエン酸ナトリウム 0.1
クエン酸 0.1
キウイ種子抽出物 0.1
精製水 残余
100.0wt%
Formulation Example 10: lotion
Ethanol 5.0wt%
Glycerin 2.0
1,3-butylene glycol
2.0
Polyethylene oleyl ether 0.5
Sodium citrate 0.1
Citric acid 0.1
Kiwi seed extract 0.1
Purified water residue
100.0wt%
配合例11:ボディージェル
マカデミアナッツ油 2.0wt%
ミリスチン酸オクチルドデシル 10.0
メチルフェニルポリシロキサン 5.0
ベヘニルアルコール 3.0
ステアリン酸 3.0
バチルアルコール 1.0
モノステアリン酸グリセリル 1.0
テトラオレイン酸ポリオキシエチレンソルビット 2.0
水素添加大豆リン脂質 1.0
セラミド 0.1
パルミチン酸レチノール 0.1
防腐剤 適量
ツボクサ抽出物 1.0
キウイ種子抽出物 1.0
1、3−ブチレングリコール 5.0
精製水 残余
100.0wt%
Formulation Example 11: Body gel
Macadamia nut oil 2.0wt%
Octyldodecyl myristate 10.0
Methylphenylpolysiloxane 5.0
Behenyl alcohol 3.0
Stearic acid 3.0
Batyl alcohol 1.0
Glyceryl monostearate 1.0
Tetraoleic acid polyoxyethylene sorbit 2.0
Hydrogenated soybean phospholipid 1.0
Ceramide 0.1
Retinol palmitate 0.1
Preservative appropriate amount
Centella extract 1.0
Kiwi seed extract 1.0
1,3-butylene glycol 5.0
Purified water residue
100.0wt%
配合例12:乳液
スクワラン 4.0wt%
ワセリン 2.5
セタノール 2.0
グリセリン 2.0
親油型モノステアリン酸グリセリン 1.0
ステアリン酸 1.0
L−アルギニン 1.0
キウイ種子抽出物 0.5
水酸化カリウム 0.1
香料 微量
精製水 残余
100.0wt%
Formulation Example 12: Emulsion
Squalane 4.0wt%
Vaseline 2.5
Cetanol 2.0
Glycerin 2.0
Lipophilic glyceryl monostearate 1.0
Stearic acid 1.0
L-Arginine 1.0
Kiwi seed extract 0.5
Potassium hydroxide 0.1
Perfume
Purified water residue
100.0wt%
配合例13:浴用剤(液状)
プロピレングリコール 50.0wt%
エタノール 20.0
硫酸ナトリウム 5.0
キウイ種子抽出物 0.5
ラノリン 0.5
アボガド油 0.5
色素 1.5
香料 22.0
100.0wt%
Formulation Example 13: Bath agent (liquid)
Propylene glycol 50.0wt%
Ethanol 20.0
Sodium sulfate 5.0
Kiwi seed extract 0.5
Lanolin 0.5
Avocado oil 0.5
Dye 1.5
Fragrance 22.0
100.0wt%
以上説明したように、本発明はキウイ種子から抽出された成分を用いているので、安全であり、副作用が少ない抗炎症剤等を提供することができる。 As described above, since the present invention uses components extracted from kiwi seeds, an anti-inflammatory agent or the like that is safe and has few side effects can be provided.
Claims (1)
A PGE 2 production inhibitor comprising as an active ingredient a kiwi seed extract obtained by extracting degreased kiwi (Actinidia chinensis Planch.) Seeds with aqueous ethanol.
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WO2012078587A1 (en) | 2010-12-07 | 2012-06-14 | University Of Oslo | Cardio-protective agents from kiwifruits |
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