JP2012136447A - Lipase inhibitor, and cosmetic, food/drink composition and pharmaceutical composition each containing the same - Google Patents
Lipase inhibitor, and cosmetic, food/drink composition and pharmaceutical composition each containing the same Download PDFInfo
- Publication number
- JP2012136447A JP2012136447A JP2010288208A JP2010288208A JP2012136447A JP 2012136447 A JP2012136447 A JP 2012136447A JP 2010288208 A JP2010288208 A JP 2010288208A JP 2010288208 A JP2010288208 A JP 2010288208A JP 2012136447 A JP2012136447 A JP 2012136447A
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- Prior art keywords
- lipase inhibitor
- lipase
- acid
- food
- extract
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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Abstract
Description
本発明はリパーゼ阻害剤に関し、詳しくは、アクネ菌などの皮膚常在菌によるニキビの改善予防効果及び治療効果に優れ、高脂肪食により誘発される肥満、高脂血症や糖尿病などの生活習慣病の改善予防効果及び治療効果に優れ、安定で安価なかつ安全性に優れるリパーゼ阻害剤に関する。また、このリパーゼ阻害剤を含有する化粧料、飲食品組成物及び医薬品組成物に関する。 The present invention relates to a lipase inhibitor, and in particular, is excellent in preventing and treating acne due to skin resident bacteria such as acne bacteria, and is a lifestyle habit such as obesity, hyperlipidemia and diabetes induced by a high fat diet. The present invention relates to a lipase inhibitor that is excellent in preventing and treating diseases and is effective, stable, inexpensive, and safe. Moreover, it is related with the cosmetics, food-drinks composition, and pharmaceutical composition containing this lipase inhibitor.
近年、食事の欧米化に伴い、肥満、高脂血症や糖尿病などの生活習慣病の発症が著しく増加しており、その対応が急務である。食事による肥満、高脂血症又は糖尿病の予防改善に向けて、リパーゼ阻害剤の開発及び応用が盛んに行われている。また、リパーゼ阻害剤は、アクネ菌などの皮膚常在菌によるニキビの予防改善にも有用であることが明らかになっている。 In recent years, with the westernization of meals, the onset of lifestyle-related diseases such as obesity, hyperlipidemia and diabetes has increased remarkably, and the response is urgently needed. In order to prevent and improve obesity, hyperlipidemia or diabetes caused by diet, lipase inhibitors have been actively developed and applied. Moreover, it has been clarified that lipase inhibitors are also useful for preventing and improving acne caused by skin resident bacteria such as acne bacteria.
これに対し、植物の果実やその皮、種子、葉や根茎などから抽出した様々なリパーゼ阻害剤が製造され、化粧品、医薬品や食品などへの配合が試みられているが、植物を原料とする場合、その原料の安全性や調達が問題であるという難点があった。 In contrast, various lipase inhibitors extracted from plant fruits, their skin, seeds, leaves, rhizomes, etc. have been manufactured and tried to be incorporated into cosmetics, pharmaceuticals, foods, etc. In some cases, the safety and procurement of the raw materials are problematic.
植物原料を由来とするリパーゼ阻害剤としては、ユッカ、高麗人参、ジャスミン茶、山査子、黄杞茶、ルイボス茶、大豆胚芽、生姜、及び杜仲茶などの抽出エキスを有効成分とするリパーゼ阻害剤(特許文献1参照)や、キラヤ(Quillaja saponaria MOLINA)樹皮の抽出物を有効成分とする膵リパーゼ阻害剤(特許文献2参照)や、栗皮抽出物を含有するリパーゼ阻害剤(特許文献3参照)などがある。 Lipase inhibitors derived from plant materials include lipase inhibitors containing extract extracts such as yucca, ginseng, jasmine tea, yamakoko, yellow ginger tea, rooibos tea, soybean germ, ginger, and chuchu tea (patent document) 1), pancreatic lipase inhibitor (see Patent Document 2) containing an extract of Quillaja saponaria MOLINA bark as an active ingredient, and a lipase inhibitor (see Patent Document 3) containing chestnut skin extract. is there.
一方、植物由来の原料としてオトギリソウ科フクギ属のマンゴスチン(Garcinia mangostana L.)も知られている。マンゴスチンを由来とする成分が有効に作用する剤も様々なものがあり、例えば、マンゴスティーンの果皮の濃縮抽出物を備える組成物がキサントン及びタンニンを含み、日焼け、光線過敏、皮膚−局在性アレルギー、免疫抑制、早老、乾癬、癌性損傷、前癌性損傷、細菌感染、ウイルス感染、菌類感染及び発疹などの皮膚の疾病の予防又は処置にとって十分な治療上の薬剤であること(例えば、特許文献4参照。)が知られている。その他にも、特定のキサントン誘導体には、抗ヘリコバクター・ピロリ作用があるもの(例えば、特許文献5又は特許文献6参照。)、グラム陽性菌に対する殺菌作用があるもの(例えば、特許文献7参照。)、トポイソメラーゼIおよびII阻害活性作用があるもの(例えば、特許文献8参照。)、血小板活性化因子抑制作用があるもの(例えば、特許文献9参照。)、抗酸化作用のあるもの(例えば、特許文献10又は特許文献11参照。)、美白作用のあるもの(例えば、特許文献12参照。)、コラーゲン増加作用があるもの(例えば、特許文献13参照。)などがある。また、α−マンゴスチンを含むキサントン誘導体混合物を含有する口腔洗浄液(例えば、特許文献14参照。)がある。 On the other hand, Mangosteen (Garcinia mangostana L.) belonging to the genus Hypericaceae is also known as a plant-derived raw material. There are various agents in which an ingredient derived from mangosteen effectively acts, for example, a composition comprising a concentrated extract of mangosteen peel contains xanthone and tannin, sunburn, photosensitivity, skin-localization Be a therapeutic agent sufficient for the prevention or treatment of skin diseases such as allergies, immunosuppression, premature aging, psoriasis, cancerous injury, precancerous injury, bacterial infection, viral infection, fungal infection and rash (e.g. Patent Document 4) is known. In addition, specific xanthone derivatives have an anti-Helicobacter pylori action (for example, see Patent Document 5 or Patent Document 6), and have a bactericidal action against Gram-positive bacteria (for example, see Patent Document 7). ), Those having a topoisomerase I and II inhibitory activity (for example, see Patent Document 8), those having a platelet activating factor inhibitory action (for example, see Patent Document 9), those having an antioxidant action (for example, Patent Document 10 or Patent Document 11), those having a whitening effect (for example, see Patent Document 12), those having a collagen increasing effect (for example, see Patent Document 13), and the like. Moreover, there is an oral cleansing liquid (for example, refer to Patent Document 14) containing a xanthone derivative mixture containing α-mangostin.
上記背景技術のように、マンゴスチンを由来とする成分に様々な作用があることは知られていたが、1−イソマンゴスチンにリパーゼ活性を阻害する作用があることは知られていなかった。 As in the above background art, it has been known that components derived from mangosteen have various actions, but it has not been known that 1-isomangosteen has an action to inhibit lipase activity.
本発明の目的は、アクネ菌などの皮膚常在菌により引き起こされるニキビの予防改善効果及び治療効果に優れ、日常生活のなかで高脂肪食により誘発される肥満、高脂血症や糖尿病などの生活習慣病の改善予防効果及び治療効果に優れ、安定で安価なかつ安全性に優れるリパーゼ阻害剤を提供することにある。また、このリパーゼ阻害剤を含有する化粧料、飲食品組成物及び医薬品組成物を提供することも副次的な目的とする。 The object of the present invention is excellent in preventing and improving acne caused by resident skin bacteria such as acne, and is effective in treating and preventing obesity, hyperlipidemia and diabetes induced by a high fat diet in daily life. An object of the present invention is to provide a lipase inhibitor that is excellent in preventing and treating lifestyle-related diseases, is stable, inexpensive, and has excellent safety. Another object is to provide a cosmetic, a food / beverage composition and a pharmaceutical composition containing the lipase inhibitor.
本発明者らは、上記事情に鑑み鋭意研究を行った結果、1−イソマンゴスチンが膵臓由来のリパーゼ及びアクネ菌由来のリパーゼを阻害する作用を有することを見出し、さらに1−イソマンゴスチンを化粧料、飲食品組成物及び医薬品組成物に配合したところ、日常生活の中で引き起こされた各種皮膚トラブルや生活習慣病などの予防改善、治療に関して、顕著な作用を及ぼすことを見出した。 As a result of intensive studies in view of the above circumstances, the present inventors have found that 1-isomangostin has an action of inhibiting lipase derived from pancreas and lipase derived from acne bacteria, and further, 1-isomangosteen is used as a cosmetic. They were found to have a remarkable effect on prevention and improvement and treatment of various skin troubles and lifestyle-related diseases caused in daily life when formulated in food and beverage compositions and pharmaceutical compositions.
すなわち、本発明のリパーゼ阻害剤は1−イソマンゴスチンを有効成分として含有することを特徴とするものである。さらに、本発明は上記リパーゼ阻害剤を含有する化粧料、飲食品組成物及び医薬品組成物でもある。 That is, the lipase inhibitor of the present invention is characterized by containing 1-isomangostin as an active ingredient. Furthermore, this invention is also cosmetics, food-drinks composition, and pharmaceutical composition containing the said lipase inhibitor.
本発明によれば、アクネ菌などの皮膚常在菌により引き起こされるニキビの予防改善効果及び治療効果に優れ、日常生活のなかで高脂肪食により誘発される肥満、高脂血症や糖尿病などの生活習慣病の改善予防効果及び治療効果に優れ、安定で安価なかつ安全性に優れるリパーゼ阻害剤を提供することができる。そして、このリパーゼ阻害剤は化粧料、飲食品組成物及び医薬品組成物に配合して好適であり、これらもアクネ菌などの皮膚常在菌により引き起こされるニキビの予防改善効果及び治療効果に優れ、日常生活のなかで高脂肪食により誘発される肥満、高脂血症や糖尿病などの生活習慣病の改善予防効果及び治療効果に優れる。 According to the present invention, it is excellent in preventing and improving acne caused by skin resident bacteria such as acne, and is effective in treating and preventing obesity, hyperlipidemia and diabetes induced by a high-fat diet in daily life. It is possible to provide a lipase inhibitor which is excellent in preventing and treating lifestyle-related diseases and is stable, inexpensive and excellent in safety. And this lipase inhibitor is suitable for blending in cosmetics, food and beverage compositions and pharmaceutical compositions, and these are also excellent in preventing and improving acne caused by skin resident bacteria such as acne bacteria, Excellent in preventing and treating lifestyle-related diseases such as obesity, hyperlipidemia and diabetes induced by a high fat diet in daily life.
以下、本発明を詳細に説明する。 Hereinafter, the present invention will be described in detail.
本発明のリパーゼ阻害剤に使用する1−イソマンゴスチンとは、下記一般式で示されるキサントン類化合物である。 1-Isomangostin used for the lipase inhibitor of the present invention is a xanthone compound represented by the following general formula.
1−イソマンゴスチンは、マンゴスチン果実の外皮などにも含まれており、例えば、マンゴスチン外皮から溶媒抽出することにより得ることもできる。また、1−イソマンゴスチンは、市販品を用いてもよく、例えば、Sichuan Weikeqi Biological Technology Co., Ltd社の「1−イソマンゴスチン」、Chem Blink Inc.社の「1−イソマンゴスチン」などがある。マンゴスチン外皮から溶媒抽出する場合、その方法は特に限定されないが、溶媒で抽出するに際しては、マンゴスチン外皮を乾燥させてから用いても、乾燥させることなく用いてもよい。さらに乾燥に関係なくマンゴスチン外皮をそのまま用いても、切断または粉砕などにより細かくしてから用いてもよい。抽出効率の面から、マンゴスチン外皮を乾燥後、粉末化したものを用いて溶媒抽出するのが好適である。1−イソマンゴスチンを溶媒抽出する場合に使用する溶媒は、水、水溶性有機溶媒またはこれらの混合溶媒で溶解するのが望ましい。水溶性有機溶媒としては、例えば、メタノール、エタノール、プロパノール、n−ブタノール、1,3−ブチレングリコール等の低級アルコール、ベンゼン、エチルエーテル、クロロホルム、酢酸エチル、酢酸ブチル、アセトンなどが挙げられる。これらのなかではエタノールが好ましく、特に水との混合溶媒である含水エタノールが、リパーゼ阻害作用が強く特に好ましい。 1-Isomangosteen is also contained in mangosteen fruit hulls, and can also be obtained, for example, by solvent extraction from mangosteen hulls. 1-Isomangostin may be a commercially available product, for example, “1-Isomangostin” from Sichuan Weikeqi Biological Technology Co., Ltd, “1-Isomangosteen” from Chem Blink Inc. . In the case of solvent extraction from mangosteen rind, the method is not particularly limited, but when extracting with a solvent, mangosteen rind may be used after drying or without drying. Further, the mangosteen rind may be used as it is regardless of drying, or may be used after being finely cut or pulverized. From the viewpoint of extraction efficiency, it is preferable to perform solvent extraction using a powdered mangosteen skin after drying. It is desirable that the solvent used for solvent extraction of 1-isomangosteen is dissolved in water, a water-soluble organic solvent, or a mixed solvent thereof. Examples of the water-soluble organic solvent include lower alcohols such as methanol, ethanol, propanol, n-butanol, and 1,3-butylene glycol, benzene, ethyl ether, chloroform, ethyl acetate, butyl acetate, and acetone. Among these, ethanol is preferable, and water-containing ethanol which is a mixed solvent with water is particularly preferable because of its strong lipase inhibitory action.
溶媒抽出時に用いる装置は特に限定されず、通常のタンクやミキサーを用いてもよく、またソックスレー抽出器などの抽出器を用いてもよい。抽出時の温度や抽出時間も特に限定されない。溶媒抽出後に、濾過、吸着樹脂による処理、活性炭処理等によって不純物を除去してもよい。さらに液体高速クロマトグラフィーにて、カラムYMC−Pack C8(SH−243−5、株式会社ワイエムシイ製)、流動相(75%アセトニトリル)を用いて温度25℃で1−イソマンゴスチンを分取することができる。 The apparatus used at the time of solvent extraction is not specifically limited, A normal tank and a mixer may be used, and extractors, such as a Soxhlet extractor, may be used. The temperature at the time of extraction and the extraction time are not particularly limited. After solvent extraction, impurities may be removed by filtration, treatment with an adsorbent resin, activated carbon treatment, or the like. Furthermore, 1-isomangostin can be fractionated at a temperature of 25 ° C. using a column YMC-Pack C8 (SH-243-5, manufactured by YMC Co., Ltd.) and a fluid phase (75% acetonitrile) by liquid high performance chromatography. it can.
本発明のリパーゼ阻害剤の剤型としては、溶媒抽出によって得られた液状抽出物の他に、液状抽出物を減圧乾燥や凍結乾燥等の通常の乾燥方法や濃縮方法等により乾固または濃縮したものであってもよい。また、必要に応じてその効力に影響がない範囲で脱臭、脱色等の精製処理をしてから用いても良く、また適宜賦形剤を用いて顆粒状にする等、使用し易い状態に製剤化されたものを用いればよい。 As the dosage form of the lipase inhibitor of the present invention, in addition to the liquid extract obtained by solvent extraction, the liquid extract was dried or concentrated by a normal drying method such as reduced pressure drying or freeze drying or a concentration method. It may be a thing. In addition, if necessary, it may be used after purification treatment such as deodorization and decoloration within a range that does not affect its efficacy, and it is formulated in a state that is easy to use, such as granulated with an appropriate excipient. What is necessary is just to use.
本発明のリパーゼ阻害剤には、1−イソマンゴスチン以外に、目的に応じて化粧料、飲食品組成物または医薬品組成物に通常使用されている成分または使用が許容されている成分を、本発明の効果を損なわない範囲内で適宜配合することができる。 The lipase inhibitor of the present invention includes, in addition to 1-isomangostin, components that are usually used in cosmetics, food and beverage compositions or pharmaceutical compositions, or components that are allowed to be used, depending on the purpose. It can mix | blend suitably within the range which does not impair the effect.
本発明のリパーゼ阻害剤を含有する化粧料、飲食品組成物または医薬品組成物における1−イソマンゴスチンの配合量は、化粧料、飲食品組成物または医薬品組成物の総量を基準として、乾燥固形分換算で0.005wt%(質量%の略称)以上、10wt%以下が効果の発現性や原価の点から考えて好ましい。特に0.005wt%以上、5wt%以下が製品に配合して応用する際に好ましい。 The blending amount of 1-isomangostin in the cosmetic, food / beverage composition or pharmaceutical composition containing the lipase inhibitor of the present invention is based on the total amount of the cosmetic, the food / beverage composition or the pharmaceutical composition, and the dry solid content. 0.005 wt% (abbreviation of mass%) or more and 10 wt% or less in terms of conversion is preferable from the viewpoint of the effect and cost. In particular, 0.005 wt% or more and 5 wt% or less is preferable when blended and applied to a product.
本発明の化粧料は特に限定されず、皮膚化粧料、浴用化粧料、洗浄用化粧料、痩身用化粧料、ニキビ用化粧料等を挙げることができ、その形態としては、乳液、ジェル、スティッ
ク、シート、パップ、ジェル、粉末、液体、顆粒、クリーム状、ペースト状、固形等を挙げることができる。これらの化粧料は常法により製造することができ、必要に応じて、一般に化粧料で用いられている賦形剤、香料などをはじめ、油脂類、界面活性剤、保湿剤、美白剤、pH調整剤、粘結剤類、多価アルコール類、精油及び香料類、増粘剤、防腐剤、抗酸化剤、紫外線吸収剤、顔料、植物粉砕物及び生薬類、無機塩類及び無機酸類、洗浄剤、乳化剤などの各種化粧料成分を適宜配合することができる。
The cosmetics of the present invention are not particularly limited, and examples thereof include skin cosmetics, bath cosmetics, cleaning cosmetics, slimming cosmetics, acne cosmetics, and the forms thereof are emulsions, gels, sticks. , Sheets, pops, gels, powders, liquids, granules, creams, pastes, solids, and the like. These cosmetics can be manufactured by a conventional method, and if necessary, generally used in cosmetics such as excipients and fragrances, fats and oils, surfactants, moisturizers, whitening agents, pH Conditioning agents, binders, polyhydric alcohols, essential oils and fragrances, thickeners, preservatives, antioxidants, UV absorbers, pigments, plant pulverized products and herbal medicines, inorganic salts and inorganic acids, cleaning agents Various cosmetic ingredients such as emulsifiers can be appropriately blended.
本発明の飲食品組成物の種類としても特に限定されず、例えば、菓子類(チューインガム、キャンディ、グミ、タブレット、チョコレート、ゼリー等)、氷菓(アイスキャンディー、アイスクリーム、シャーベット等)、冷菓(ゼリー、プリン、水ようかん等)、麺類をはじめとする澱粉系食品、粉末飲食品、飲料(スープ、コーヒー、茶類、ジュース、炭酸飲料、ココア、アルコール飲料、ゼリー状ドリンク等)、ベーカリー食品(クッキー、ビスケット、パン、パイ、ケーキ等)、油脂食品(マーガリン、ショートニング、ファットスプレッド等)、乳製品(牛乳、ヨーグルト、乳清飲料、乳酸菌飲料、バター、クリーム、チーズ等)等を挙げることができる。 The type of the food / beverage composition of the present invention is not particularly limited, and examples thereof include confectionery (chewing gum, candy, gummi, tablet, chocolate, jelly, etc.), ice confectionery (ice candy, ice cream, sorbet, etc.), frozen confectionery (jelly). , Pudding, water yokan, etc.), starch-based foods such as noodles, powdered foods and drinks, beverages (soup, coffee, teas, juice, carbonated beverages, cocoa, alcoholic beverages, jelly drinks, etc.), bakery foods (cookies) , Biscuits, breads, pies, cakes, etc.), oil and fat foods (margarine, shortening, fat spreads, etc.), dairy products (milk, yogurt, whey drinks, lactic acid bacteria beverages, butter, cream, cheese, etc.) .
本発明の前記飲食品組成物はそれぞれ常法により製造することができ、必要に応じて、本発明の目的を損なわない範囲で下記の成分を適宜選択して1−マンゴスチンを含有するリパーゼ阻害剤とともに配合できる。例えば、糖質甘味料(果糖、ブドウ糖、タガトース、アラビノース等の単糖類、乳糖、オリゴ糖、麦芽糖、トレハロース等の少糖類、粉末水あめ、デキストリン、糖アルコール等)、高甘味度甘味料(スクラロース、アセスルファムK、ステビア等)、でん粉等の多糖類、油脂類、乳製品、安定剤、乳化剤、香料(バニリン、リナロール、天然香料等)、色素、着色料、酸味料、風味原料(卵、コーヒー、茶類、ココア、果汁果肉、ヨーグルト、酒類等)、香味料(ラズベリーフレーバー、アップルフレーバー、コーヒーフレーバー等)、湿化防止剤、電解質、抗酸化剤、保存料、湿潤剤、蛋白質、アミノ酸、ペプチド、食物繊維、有機酸(クエン酸、リンゴ酸、フマル酸、マロン酸、コハク酸、酒石酸、乳酸等)、ビタミン類(L−アスコルビン酸、dl−α−トコフェロール、ビタミンB1、ビタミンB2、ナイアシン、パントテン酸、ビタミンB6、ビタミンB12、葉酸、ビオチン、イノシトール等)、ミネラル(亜鉛、鉄、カルシウム、マグネシウム、クロム、セレン、カリウム、ナトリウム等)、グルコサミン、酵母、卵殻膜、リコピン、アスタキサンチン、その他カロテノイド、シルク、コンドロイチン、セラミド、プラセンタエキス、フカヒレエキス、深海鮫エキス、スクワレン、γ−アミノ酪酸、カゼインドデカペプチド、生栗皮抽出物、栗の葉抽出物、栗のいが抽出物、栗果肉抽出物、栗樹皮抽出物、キャベツ発酵エキス、バラの花びら抽出物、ブドウ葉抽出物、ブドウ種子抽出物、りんごポリフェノール、カミツレエキス、ライチ種子エキス、ゴツコラエキス、月桃葉エキス、ハス胚芽エキス、スターフルーツ葉エキス、桑葉抽出物、グァバ茶抽出物、赤ワイン、緑茶、紅茶、ウーロン茶、コーヒー、ココア、チョコレート、黒ゴマ、豆類、豆乳、ナッツ類、きのこ類、緑黄食野菜類、ヨード卵等の卵由来原料、カテキン類、その他ポリフェノール類、ラズベリーケトン、低分子アルギン酸、サイリウム種皮、イチョウ葉抽出物、松樹皮抽出物、ナットウキナーゼ、植物ステロール、ジアシルグリセロール、キトサン、ヒアルロン酸、メチルスルフォニルメタン、コウジ酸、エラグ酸、アルブチン、ルシノール、マグノリグナン、リン酸L−アスコルビン酸マグネシウム、CoQ10、α−リポ酸等が挙げられる。 The said food-drinks composition of this invention can be manufactured by a conventional method, respectively, The lipase inhibitor containing 1-mangostin by selecting suitably the following component in the range which does not impair the objective of this invention as needed. Can be blended together. For example, sugar sweeteners (monosaccharides such as fructose, glucose, tagatose and arabinose, oligosaccharides such as lactose, oligosaccharides, maltose and trehalose, powdered starch syrup, dextrin, sugar alcohol etc.), high sweetness sweeteners (sucralose, Acesulfame K, stevia, etc.), polysaccharides such as starch, fats and oils, dairy products, stabilizers, emulsifiers, fragrances (vanillin, linalool, natural fragrances, etc.), pigments, colorants, acidulants, flavor ingredients (eggs, coffee, Tea, cocoa, fruit pulp, yogurt, alcoholic beverages, etc.), flavoring (raspberry flavor, apple flavor, coffee flavor, etc.), anti-wetting agent, electrolyte, antioxidant, preservative, wetting agent, protein, amino acid, peptide , Dietary fiber, organic acids (citric acid, malic acid, fumaric acid, malonic acid, succinic acid, tartaric acid, lactic acid, etc.), vitamins (L-Asco Binic acid, dl-α-tocopherol, vitamin B1, vitamin B2, niacin, pantothenic acid, vitamin B6, vitamin B12, folic acid, biotin, inositol, etc., mineral (zinc, iron, calcium, magnesium, chromium, selenium, potassium, Sodium, etc.), glucosamine, yeast, eggshell membrane, lycopene, astaxanthin, other carotenoids, silk, chondroitin, ceramide, placenta extract, shark fin extract, deep-sea cocoon extract, squalene, γ-aminobutyric acid, casein decapeptide, raw chestnut skin extract , Chestnut leaf extract, chestnut potato extract, chestnut pulp extract, chestnut bark extract, cabbage ferment extract, rose petal extract, grape leaf extract, grape seed extract, apple polyphenol, chamomile extract, Lychee seed extract, Gotsukola extract Moon peach leaf extract, lotus germ extract, star fruit leaf extract, mulberry leaf extract, guava tea extract, red wine, green tea, black tea, oolong tea, coffee, cocoa, chocolate, black sesame, beans, soy milk, nuts, mushrooms, Green-yellow vegetables, egg-derived raw materials such as iodine eggs, catechins, other polyphenols, raspberry ketone, low molecular weight alginic acid, psyllium seed coat, ginkgo biloba extract, pine bark extract, nattokinase, plant sterol, diacylglycerol, chitosan, Examples include hyaluronic acid, methylsulfonylmethane, kojic acid, ellagic acid, arbutin, lucinol, magnolignan, magnesium phosphate L-ascorbate, CoQ10, and α-lipoic acid.
本発明の医薬品組成物の剤型としては特に限定されず、経口投与製剤でも非経口投与製剤のいずれであっても構わない。具体的には、エアゾール剤、液剤、エキス剤、エリキシル剤、カプセル剤(ハードカプセル、ソフトカプセル、マイクロカプセル)、顆粒剤、丸剤、眼軟膏剤、経皮吸収型製剤、懸濁剤、乳剤、坐剤(含膣剤)、散剤、酒精剤、錠剤(素錠、コーティング錠、特殊錠)、シロップ剤、浸剤・煎剤、注射剤(水溶性注射剤、非水溶性注射剤)、貼付剤、チンキ剤、点眼剤、トローチ剤、軟膏剤、パップ剤、芳香水剤、
リニメント剤、リモナーデ剤、流エキス剤、ローション剤などが挙げられる。これらの製剤は、製剤技術分野における慣用方法にて製造でき、例えば日本薬局方記載の方法で製造することができる。これらの製剤は、ヒトを含む哺乳動物に対して安全に投与することができるものである。
The dosage form of the pharmaceutical composition of the present invention is not particularly limited, and it may be an oral administration formulation or a parenteral administration formulation. Specifically, aerosols, liquids, extracts, elixirs, capsules (hard capsules, soft capsules, microcapsules), granules, pills, ophthalmic ointments, transdermal preparations, suspensions, emulsions, seats Preparation (vaginal preparation), powder, spirits, tablets (plain tablet, coated tablet, special tablet), syrup, soaking agent, decoction, injection (water-soluble injection, water-insoluble injection), patch, tincture Preparations, eye drops, lozenges, ointments, poultices, fragrances,
Examples include liniments, limonades, flow extracts, and lotions. These preparations can be produced by a conventional method in the pharmaceutical technical field, for example, by the method described in the Japanese Pharmacopoeia. These preparations can be safely administered to mammals including humans.
本発明の1−イソマンゴスチンを含有するリパーゼ阻害剤は、生物に対する毒性が低い化合物であることから、そのまま、または薬理学的に許容される無毒性かつ不活性の担体等を併用して、ヒトを含む哺乳動物(例えば、マウス、ラット、ウサギ、イヌ、ネコ、ウシ、ウマ、ブタ、サルなど)、魚類等に対して、医薬品組成物(動物薬含む)として適用することができる。 Since the lipase inhibitor containing 1-isomangosteen of the present invention is a compound having low toxicity to living organisms, it can be used as it is or in combination with a pharmacologically acceptable non-toxic and inert carrier. Can be applied as a pharmaceutical composition (including animal drugs) to mammals (eg, mice, rats, rabbits, dogs, cats, cows, horses, pigs, monkeys, etc.), fish, and the like.
前記薬理学的に許容される担体としては特に限定されず、製剤素材として公知である各種担体物質を使用することができる。前記担体物質としては特に限定されず、例えば、固形製剤においては、賦形剤、滑沢剤、結合剤、崩壊剤等を挙げることができる。前記担体物質に加えて、更に、防腐剤、着色剤、天然色素、甘味剤等の製剤添加物も必要に応じて用いることができる。これらの物質として、乳糖、ヒドロキシプロピルメチルセルロース、ヒドロキシプロピルセルロース、低置換度ヒドロキシプロピルセルロース、エチルセルロース、トウモロコシデンプン、結晶セルロース、カルメロースカルシウム、無水ケイ酸、合成ケイ酸アルミニウム、ステアリン酸マグネシウム、タルク等が具体的に例示できるが、これらに限られるものではない。 The pharmacologically acceptable carrier is not particularly limited, and various carrier substances known as pharmaceutical materials can be used. The carrier substance is not particularly limited, and examples of solid carriers include excipients, lubricants, binders, and disintegrants. In addition to the carrier substance, formulation additives such as preservatives, colorants, natural pigments, sweeteners and the like can be used as necessary. These substances include lactose, hydroxypropylmethylcellulose, hydroxypropylcellulose, low-substituted hydroxypropylcellulose, ethylcellulose, corn starch, crystalline cellulose, carmellose calcium, anhydrous silicic acid, synthetic aluminum silicate, magnesium stearate, talc, etc. Although it can illustrate concretely, it is not restricted to these.
液状製剤における前記担体物質としては特に限定されず、例えば、溶剤、溶解補助剤、懸濁化剤、等張化剤、緩衝剤等として配合されるもの等を挙げることができる。更に、防腐剤、着色剤、水不溶性レーキ色素、甘味剤等の製剤添加物も必要に応じて用いることができる。これらの物質として、マンニトール、塩化ナトリウム、グルコース、ソルビトール、グリセロール、キシリトール、フルクトース、マルトース、マンノース等の等張化剤、亜硫酸ナトリウム等の安定化剤、ベンジルアルコール、パラヒドロキシ安息香酸メチル等の保存剤等の他、溶解補助剤、無痛化剤やpH調整剤等が具体的に例示できるが、これらに限られるものではない。 The carrier substance in the liquid preparation is not particularly limited, and examples thereof include a solvent, a solubilizing agent, a suspending agent, a tonicity agent, a buffering agent, and the like. Furthermore, formulation additives such as preservatives, colorants, water-insoluble lake pigments, sweeteners and the like can be used as necessary. These substances include isotonic agents such as mannitol, sodium chloride, glucose, sorbitol, glycerol, xylitol, fructose, maltose, mannose, stabilizers such as sodium sulfite, preservatives such as benzyl alcohol and methyl parahydroxybenzoate. In addition to the above, a solubilizer, a soothing agent, a pH adjuster and the like can be specifically exemplified, but are not limited thereto.
以下、実施例及び比較例を例示することにより、本発明を具体的に説明する。なお、本発明はこれら実施例により何ら限定されるものではない。 Hereinafter, the present invention will be specifically described by illustrating examples and comparative examples. In addition, this invention is not limited at all by these Examples.
・1−イソマンゴスチンの調製
新鮮なマンゴスチン果実を切り開いて中身を丸ごと取り出し、中身を取り除いた後のマンゴスチン外皮を細かく切断して25℃にて乾燥した。乾燥した外皮20gをビーカーに投入した後、50%エタノール水溶液100mlを加えて48時間攪拌して溶媒抽出液を得た。抽出液は、必要に応じて減圧下でエタノールを留去した後、凍結乾燥して乾燥物とした。乾燥物1gを75%アセトニトリルで溶解した。溶解液を液体高速クロマトグラフィーにて、カラムYMC−Pack C8(SH−243−5、株式会社ワイエムシイ製)、流動相(75%アセトニトリル)を用いて温度25℃で分離精製し、1−イソマンゴスチンを得た。
-Preparation of 1-isomangosteen A fresh mangosteen fruit was cut open, the entire contents were taken out, and the mangosteen outer skin after the contents were removed was cut into small pieces and dried at 25 ° C. After putting 20 g of dried skin into a beaker, 100 ml of 50% aqueous ethanol solution was added and stirred for 48 hours to obtain a solvent extract. Ethanol was distilled off under reduced pressure as necessary, and the extract was freeze-dried to obtain a dried product. 1 g of the dried product was dissolved in 75% acetonitrile. The lysate was separated and purified at 25 ° C. by liquid high performance chromatography using a column YMC-Pack C8 (SH-243-5, manufactured by YMC Co., Ltd.) and a fluid phase (75% acetonitrile), and 1-isomangosteen Got.
・実施例1〜3、比較例1
表1及び表2に示す各実施例の濃度となるように、上記調製した1−イソマンゴスチンを0.1mol/Lのトリス−塩酸緩衝液(pH8.0)で調製し、試料溶液を得た。比較例1の試料溶液は緩衝液のみとした。
Examples 1 to 3 and Comparative Example 1
The 1-isomangostin prepared above was prepared with 0.1 mol / L Tris-hydrochloric acid buffer (pH 8.0) so as to obtain the concentration of each Example shown in Table 1 and Table 2, and a sample solution was obtained. . The sample solution of Comparative Example 1 was a buffer solution only.
試験例1 豚膵臓由来のリパーゼ阻害作用の測定
リパーゼ活性はトリオレインからのオレイン酸遊離量を測定することによって算出した。トリオレイン(SIGMA Chemical Co.(米国製))80mg、レシチン10mg(和光純薬工業株式会社製)、胆汁酸(SIGMA Chemical Co.(米国製))5mgを9mlの0.1mol(M)TES緩衝液(pH7.0)中で10分間超音波処理を行うことで均一な懸濁液とし、これを基質液として用いた。基質液0.1mlに豚膵臓由来リパーゼ液(SIGMA Chemical Co.(米国製))0.05ml(最終濃度1μg/ml)及び被検物質0.1mlを加え、37℃、30分間反応させ、遊離した脂肪酸を銅試薬法で定量測定した。豚膵臓由来のリパーゼ活性値は検体無添加(コントロール)の値を100%として各検体のリパーゼ活性値及び標準偏差を算出した。活性値が低いほどリパーゼ阻害作用が強いことを示す。
Test Example 1 Measurement of lipase inhibitory action derived from porcine pancreas The lipase activity was calculated by measuring the amount of oleic acid released from triolein. Triolein (SIGMA Chemical Co. (US)) 80 mg, lecithin 10 mg (Wako Pure Chemical Industries, Ltd.), bile acid (SIGMA Chemical Co. (US)) 5 mg, 9 ml of 0.1 mol (M) TES buffer A uniform suspension was obtained by sonication in a liquid (pH 7.0) for 10 minutes, and this was used as a substrate liquid. Add 0.1 ml of porcine pancreas-derived lipase solution (SIGMA Chemical Co. (US)) and 0.1 ml of the test substance to 0.1 ml of the substrate solution and react at 37 ° C. for 30 minutes to release. The measured fatty acid was quantitatively measured by a copper reagent method. For the lipase activity value derived from porcine pancreas, the lipase activity value and standard deviation of each sample were calculated with the value of no sample (control) added as 100%. The lower the activity value, the stronger the lipase inhibitory action.
表1に示すように、1−イソマンゴスチンが濃度依存的に膵臓由来のリパーゼ活性を阻害した。 As shown in Table 1, 1-isomangostin inhibited pancreatic lipase activity in a concentration-dependent manner.
試験例2 アクネ菌由来のリパーゼ阻害作用の測定
アクネ菌由来のリパーゼの調製は、Pabloらの方法(Gary Pabloら著、「CHARACTERISTICS OF THE EXTRACELLULAR LIPASES FROM CORYNEBACTERIUM ACNES AND STAPHYLOCOCCUS
EPIDERMIS FREE」Journal of Investigative Dermatology誌、The Williams &Wilkins Co.社、1974年8月、Vol.63 No.2 p.231-238)に準じてリパーゼを精製した。操作としては、ブレイン・ハート・インフュージョンブイヨン培地中にヒト顔面から分離したプロピオニバクテリウム・アクネス(Propionibacterium acnes)の1白金耳を接種し、37℃で7日間嫌気的に培養し、培養終了後、培養液を4℃、3000rpm、20分間遠心分離した。その上清500ml中に−20℃、95%エタノールを500ml添加し、−10℃1時間スターラーで攪拌した後、4℃、1000rpm、20分間遠心分離し、沈殿を凍結乾燥して粗リパーゼとして試験に供した。リパーゼ活性阻害の測定には、4−メチルウンベリフェロンのオレイン酸エステル(4−MUO)を基質として用いた。0.1mlの4−MUO溶液に0.1mlの1−イソマンゴスチンを加え混合した後に、0.05mlのアクネ菌由来のリパーゼ溶液を添加し、30分間反応させた後に、0.25mlの0.1Mクエン酸緩衝液(pH4.2)を加え、反応を停止させた。反応によって生じた4−メチルウンベリフェロンの蛍光(励起波長355nm、蛍光波長460nm)を蛍光マイクロプレートリーダーにて測定した。活性値は検体無添加の値を100%として各検体の活性値を算出した。
Test Example 2 Measurement of Acne Bacterial Lipase Inhibition The preparation of Acne bacteria-derived lipase was carried out according to the method of Pablo et al. (Gary Pablo et al., “CHARACTERISTICS OF THE EXTRACE
The lipase was purified according to EPIDERMIS FREE, Journal of Investigative Dermatology, The Williams & Wilkins Co., August 1974, Vol. 63 No. 2 p.231-238). As an operation, inoculate 1 platinum ear of Propionibacterium acnes isolated from human face in brain heart infusion broth medium, and culture anaerobically at 37 ° C for 7 days. Thereafter, the culture solution was centrifuged at 3000 rpm for 20 minutes at 4 ° C. Add 500 ml of −20 ° C. and 95% ethanol to 500 ml of the supernatant, stir with a stirrer at −10 ° C. for 1 hour, centrifuge at 4 ° C. and 1000 rpm for 20 minutes, freeze-dry the precipitate, and test as crude lipase It was used for. For measurement of lipase activity inhibition, 4-methylumbelliferone oleate (4-MUO) was used as a substrate. After adding 0.1 ml of 1-isomangostin to 0.1 ml of 4-MUO solution and mixing, 0.05 ml of a lipase solution derived from acne is added and allowed to react for 30 minutes. 1M citrate buffer (pH 4.2) was added to stop the reaction. The fluorescence (excitation wavelength: 355 nm, fluorescence wavelength: 460 nm) of 4-methylumbelliferone generated by the reaction was measured with a fluorescence microplate reader. As the activity value, the activity value of each sample was calculated with the value of no sample being added as 100%.
表2に示すように、1−イソマンゴスチンが濃度依存的にアクネ菌由来のリパーゼ活性を
阻害した。
As shown in Table 2, 1-isomangostin inhibited lipase activity derived from Acne bacteria in a concentration-dependent manner.
以上の結果から、1−イソマンゴスチンは優れたリパーゼ阻害効果を有し、脂質の腸管吸収を遅らせることや、アクネ菌などの皮膚常在菌の活性を阻害することが期待できる。これによって1−イソマンゴスチンを含有する組成物が、ニキビの発生や、脂肪の蓄積を抑制し、各種疾患の予防、改善、治療効果を有するものであることが考えられる。 From the above results, 1-isomangosteen has an excellent lipase inhibitory effect, and can be expected to delay intestinal absorption of lipids and inhibit the activity of skin resident bacteria such as acne. Thus, it is considered that the composition containing 1-isomangosteen suppresses the occurrence of acne and fat accumulation, and has preventive, ameliorating, and therapeutic effects for various diseases.
以下に、本発明のリパーゼ阻害剤を含有する飲食品組成物、化粧料及び医薬品組成物の実施例を示す。組成は質量%で示す。 Below, the Example of the food-drinks composition containing the lipase inhibitor of this invention, cosmetics, and a pharmaceutical composition is shown. The composition is expressed in mass%.
実施例4 チューインガム
下記組成のチューインガムを常法により調製した。
1−イソマンゴスチン 2.0
ガムベース 20.0
還元水あめ 4.0
アップル香料 0.5
マルチトール TO 100
Example 4 Chewing gum A chewing gum having the following composition was prepared by a conventional method.
1-Isomangosteen 2.0
Gum base 20.0
Reduced water candy 4.0
Apple flavoring 0.5
Maltitol TO 100
体重の増加に悩むモニターが、1粒1500mgとした上記チューインガムを1回1粒、1日3回、3ヶ月摂取したところ、それまでに比べ体重の増加が抑制された。 When a monitor suffering from weight gain took the above chewing gum, which was 1500 mg per tablet, once a day, three times a day, for three months, the increase in body weight was suppressed compared to before.
実施例5 錠菓
下記組成での錠菓を常法により調製した。
1−イソマンゴスチン 5.0
ショ糖脂肪酸エステル 4.0
ラズベリー香料 0.1
ソルビトール TO 100
Example 5 Tablet confectionery A tablet confection having the following composition was prepared by a conventional method.
1-Isomangostin 5.0
Sucrose fatty acid ester 4.0
Raspberry flavor 0.1
Sorbitol TO 100
体重の増加に悩むモニターが、1錠2000mgとした上記錠菓を1回1錠、1日3回、3ヶ月間摂取したところ、それまでに比べ体重の増加が抑制された。 When a monitor suffering from an increase in body weight took 1 tablet of 2000 mg of the above tablet confection once a day, 3 times a day for 3 months, the increase in body weight was suppressed compared to before.
実施例6 乳液状皮膚化粧料
1−イソマンゴスチン 0.1
流動パラフィン 8.0
ステアリルアルコール 3.0
カラギーナン 0.2
パラベン 0.1
ポリオキシエチレン(60)硬化ヒマシ油 0.1
香料(ヒノキ油) 適 量
精製水 TO 100
Example 6 Milky skin cosmetic 1-Isomangostin 0.1
Liquid paraffin 8.0
Stearyl alcohol 3.0
Carrageenan 0.2
Paraben 0.1
Polyoxyethylene (60) hydrogenated castor oil 0.1
Perfume (Japanese cypress oil) Appropriate amount of purified water TO 100
実施例7 角栓除去シート、
1−イソマンゴスチン 1.0
ポリアクリル酸 27.6
アクリル酸メタクリル酸共重合体 35.0
ポリビニルアルコール 5.4
ポリビニルピロリドン 18.8
グリセリン 4.2
酸化チタン 3.0
シリカ 5.0
パラオキシ安息香酸メチル 0.2
エタノール 2.4
香料 0.5
精製水 TO 100
Example 7 Square plug removal sheet,
1-Isomangosteen 1.0
Polyacrylic acid 27.6
Acrylic acid / methacrylic acid copolymer 35.0
Polyvinyl alcohol 5.4
Polyvinylpyrrolidone 18.8
Glycerin 4.2
Titanium oxide 3.0
Silica 5.0
Methyl paraoxybenzoate 0.2
Ethanol 2.4
Fragrance 0.5
Purified water TO 100
実施例8 パップ
1−イソマンゴスチン 1.0
グリセリン 25.0
ポリアクリル酸ナトリウム 3.0
ポリビニルアルコール 2.0
ゼラチン 1.5
カルボキシメチルセルロースナトリウム 0.5
エタノール 1.0
エデト酸ニナトリウム 0.1
メチルパラベン 0.05
プロピルパラベン 0.05
精製水 TO 100
Example 8 Pap 1-Isomangostin 1.0
Glycerin 25.0
Sodium polyacrylate 3.0
Polyvinyl alcohol 2.0
Gelatin 1.5
Sodium carboxymethylcellulose 0.5
Ethanol 1.0
Edetate disodium 0.1
Methylparaben 0.05
Propylparaben 0.05
Purified water TO 100
実施例9 ジェル状ニキビ用化粧料
1−イソマンゴスチン 2.0
ポリエチレングリコール4000 30.0
ポリビニルアルコール 15.0
グリセリン 15.0
3−BG 10.0
カルボキシビニルポリマー 2.0
カチオン化セルロース 0.2
アルコール 10.0
パラベン 0.1
香料 微 量
精製水 TO 100
Example 9 Gel Acne Cosmetic 1-Isomangostin 2.0
Polyethylene glycol 4000 30.0
Polyvinyl alcohol 15.0
Glycerin 15.0
3-BG 10.0
Carboxyvinyl polymer 2.0
Cationized cellulose 0.2
Alcohol 10.0
Paraben 0.1
Fragrance Slightly purified water TO 100
実施例10 クリーム状栄養クリーム
1−イソマンゴスチン 4.0
ステアリン酸 2.5
ステアリルアルコール 8.0
スクワラン 5.0
オクチルドデカノール 7.0
グリセリルモノステアレート 4.0
防腐剤 適 量
香料 適 量
グリセリン 6.0
ソルビトール 13.0
乳酸カリウム 0.5
精製水 TO 100
Example 10 Creamy Nutritional Cream 1-Isomangosteen 4.0
Stearic acid 2.5
Stearyl alcohol 8.0
Squalane 5.0
Octyldodecanol 7.0
Glyceryl monostearate 4.0
Preservative Appropriate amount of perfume Appropriate amount of glycerin 6.0
Sorbitol 13.0
Potassium lactate 0.5
Purified water TO 100
実施例11 スティックリップトリートメント
1−イソマンゴスチン 1.0
キャンデリラロウ 12.0
固形パラフィン 8.0
ミツロウ 5.0
カルナバロウ 2.0
ラノリン 14.0
マンニット 15.0
イソプロピルミリステート 10.0
香料 適 量
酸化防止剤 適 量
ヒマシ油 TO 100
Example 11 Stick Lip Treatment 1-Isomangosteen 1.0
Candelilla Row 12.0
Solid paraffin 8.0
Beeswax 5.0
Carnavalo 2.0
Lanolin 14.0
Mannit 15.0
Isopropyl myristate 10.0
Perfume Appropriate amount Antioxidant Appropriate amount Castor oil TO 100
実施例12 乳液状皮膚化粧料
1−イソマンゴスチン 5.0
ステアリン酸 2.0
セタノール 2.0
ワセリン 2.0
ラノリンアルコール 1.5
流動パラフィン 9.0
スクワラン 3.5
ソルビトール 10.0
トリエタノールアミン 1.0
プロピレングリコール 5.0
防腐剤 適 量
香料 適 量
精製水 TO 100
Example 12 Emulsion skin cosmetic 1-Isomangostin 5.0
Stearic acid 2.0
Cetanol 2.0
Vaseline 2.0
Lanolin alcohol 1.5
Liquid paraffin 9.0
Squalane 3.5
Sorbitol 10.0
Triethanolamine 1.0
Propylene glycol 5.0
Preservative appropriate amount perfume appropriate amount purified water TO 100
実施例13 ペースト状栄養クリーム
1−イソマンゴスチン 2.0
ステアリン酸 2.0
ステアリルアルコール 8.0
還元ラノリン 2.0
スクワラン 8.0
オクチルドデカノール 6.0
防腐剤 適 量
香料 適 量
プロピレングリコール 5.0
グリセリン 3.0
乳酸 0.3
クエン酸ナトリウム 0.5
精製水 TO 100
Example 13 Pasty nourishing cream 1-isomangosteen 2.0
Stearic acid 2.0
Stearyl alcohol 8.0
Reduced lanolin 2.0
Squalane 8.0
Octyldodecanol 6.0
Preservatives Appropriate perfumes Appropriate propylene glycol 5.0
Glycerin 3.0
Lactic acid 0.3
Sodium citrate 0.5
Purified water TO 100
実施例14 液体スリミングマッサージソープ
1−イソマンゴスチン 5.0
ラウリン酸 10.0
水酸化カリウム 2.8
ヤシ油脂肪酸カリウム液 30.0
エデト酸2ナトリウム 0.15
メチルセルロース 0.5
ラウリン酸アミノプロピルベタイン液 2.0
グリセリン 8.0
香料 適 量
精製水 TO 100
Example 14 Liquid Slimming Massage Soap 1-Isomangosteen 5.0
Lauric acid 10.0
Potassium hydroxide 2.8
Coconut oil fatty acid potassium 30.0
Edetate disodium 0.15
Methylcellulose 0.5
Aminopropyl betaine laurate solution 2.0
Glycerin 8.0
Perfume proper amount purified water TO 100
実施例15 マッサージ用ジェル
1−イソマンゴスチン 10.0
カフェイン 0.1
カルボキシビニルポリマー 0.5
ポリビニルアルコール 3.0
グリセリン 35.0
ポリエチレングリコール400 45.0
エタノール 適 量
防腐剤 適 量
精製水 TO 100
Example 15 Massage Gel 1-Isomangosteen 10.0
Caffeine 0.1
Carboxyvinyl polymer 0.5
Polyvinyl alcohol 3.0
Glycerin 35.0
Polyethylene glycol 400 45.0
Ethanol appropriate amount Preservative appropriate amount purified water TO 100
実施例16 入浴用固形錠剤
炭酸水素ナトリウム 40.0
コハク酸 10.0
無水クエン酸 10.0
精製白糖 10.0
乳糖 10.0
デキストリン 5.0
ポリエチレン6000 5.0
カルボキシメチルセルロースナトリウム 4.0
テトラデセン酸ナトリウム 4.0
L−システイン塩酸塩 0.2
エデト酸2ナトリウム 0.2
香料 0.2
酸化チタン 0.2
カオリン 0.2
ラウリル硫酸ナトリウム 0.1
シュウ酸ナトリウム 0.1
天然ビタミンE 0.1
1−イソマンゴスチン 0.5
着色料 微 量
無水硫酸ナトリウム TO 100
Example 16 Bathing Solid Tablet Sodium Bicarbonate 40.0
Succinic acid 10.0
Anhydrous citric acid 10.0
Purified white sugar 10.0
Lactose 10.0
Dextrin 5.0
Polyethylene 6000 5.0
Sodium carboxymethylcellulose 4.0
Sodium tetradecenoate 4.0
L-cysteine hydrochloride 0.2
Edetic acid disodium 0.2
Fragrance 0.2
Titanium oxide 0.2
Kaolin 0.2
Sodium lauryl sulfate 0.1
Sodium oxalate 0.1
Natural vitamin E 0.1
1-Isomangostin 0.5
Colorant Slightly anhydrous sodium sulfate TO 100
実施例17 入浴用粉末
炭酸水素ナトリウム 40.0
無水珪酸 0.5
塩化ナトリウム 10.0
1−イソマンゴスチン 0.5
香料 1.0
着色料 微 量
無水硫酸ナトリウム TO 100
Example 17 Powdered Sodium Bicarbonate for Bath 40.0
Silicic anhydride 0.5
Sodium chloride 10.0
1-Isomangostin 0.5
Fragrance 1.0
Colorant Slightly anhydrous sodium sulfate TO 100
実施例18 顆粒粉末洗浄剤
粒状糖類* 10.0
1−イソマンゴスチン 1.0
炭酸水素ナトリウム 30.0
乾燥硫酸ナトリウム 30.0
ラウリル硫酸ナトリウム 1.5
PEG6000P 5.0
PVP 0.1
香料 適 量
デキストリン TO 100
*白糖、乳糖及びデキストリンを含み、高圧ガスが封入された明治製菓製の粒状糖類を使用した。
Example 18 Granule powder detergent granular saccharide * 10.0
1-Isomangosteen 1.0
Sodium bicarbonate 30.0
Dry sodium sulfate 30.0
Sodium lauryl sulfate 1.5
PEG6000P 5.0
PVP 0.1
Perfume appropriate amount dextrin TO 100
* Granular saccharides manufactured by Meiji Seika containing white sugar, lactose and dextrin and encapsulating high-pressure gas were used.
実施例19 粉末パック
1−イソマンゴスチン 3.5
タルク 25.0
プロピレングリコール 6.0
KCl 1.0
香料 0.5
カオリン TO 100
Example 19 Powder Pack 1-Isomangostin 3.5
Talc 25.0
Propylene glycol 6.0
KCl 1.0
Fragrance 0.5
Kaolin TO 100
実施例20 ニキビ用ジェル(皮膚外用医薬品組成物)
1−イソマンゴスチン 10.0
カフェイン 0.1
カルボキシビニルポリマー 0.5
ポリビニルアルコール 3.0
グリセリン 35.0
ポリエチレングリコール400 45.0
エタノール 適 量
防腐剤 適 量
精製水 TO 100
Example 20 Acne Gel (External Pharmaceutical Composition)
1-Isomangosteen 10.0
Caffeine 0.1
Carboxyvinyl polymer 0.5
Polyvinyl alcohol 3.0
Glycerin 35.0
Polyethylene glycol 400 45.0
Ethanol appropriate amount Preservative appropriate amount purified water TO 100
実施例6〜20の各化粧料は常法により調製した。いずれも皮膚に対し刺激性がなく、リパーゼ防止効果、ニキビ改善効果に優れ、使用感も優れていた。 Each cosmetic of Examples 6 to 20 was prepared by a conventional method. All of them were not irritating to the skin, were excellent in the lipase prevention effect, the acne improvement effect, and the feeling in use was also excellent.
実施例20 錠剤(医薬品組成物)
1−イソマンゴスチン 10.0
ビタミンC 20.0
ビタミンB1 0.5
ビタミンB2 0.5
乳糖 40.0
デキストリン 23.0
合成ケイ酸アルミニウム 5.0
ステアリン酸マグネシウム 1.0
Example 20 Tablet (Pharmaceutical Composition)
1-Isomangosteen 10.0
Vitamin C 20.0
Vitamin B1 0.5
Vitamin B2 0.5
Lactose 40.0
Dextrin 23.0
Synthetic aluminum silicate 5.0
Magnesium stearate 1.0
(操作)
上記の各成分を混合し、その混合物を打錠機で1錠500mgに打錠して1錠中に1−イソマンゴスチン50mgを含む錠剤を得た。
(operation)
Each of the above components was mixed, and the mixture was tableted into 500 mg per tablet with a tableting machine to obtain a tablet containing 1 mg of 1-isomangostin in one tablet.
高脂血症の患者が、上記錠剤を1回1錠、1日3回3ヶ月日間服用したところ、血中脂肪量が減少した。 When a patient with hyperlipidemia took the above tablet once a day, 3 times a day for 3 months, the blood fat level decreased.
本発明のリパーゼ阻害剤は、アクネ菌などの皮膚常在菌に対して作用することによりニキビの発生を抑制し、また脂肪分解抑制剤として作用することによって、体内での脂肪の消化吸収を抑制し、体内での脂肪の蓄積を予防・治療・改善することができるものである。これによって、本発明のリパーゼ阻害剤を配合した化粧料、飲食品組成物及び医薬品組成物は、ニキビ、肥満、高脂血症、脂肪肝の予防・治療・改善に使用することができるもの
である。
The lipase inhibitor of the present invention suppresses the occurrence of acne by acting on skin resident bacteria such as acne, and also suppresses digestion and absorption of fat in the body by acting as a lipolysis inhibitor. In addition, fat accumulation in the body can be prevented, treated, and improved. As a result, cosmetics, food and beverage compositions and pharmaceutical compositions containing the lipase inhibitor of the present invention can be used for the prevention, treatment and improvement of acne, obesity, hyperlipidemia, and fatty liver. is there.
Claims (4)
Priority Applications (1)
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Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
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JP2016028573A (en) * | 2013-01-21 | 2016-03-03 | レジリオ株式会社 | Therapeutic agent and therapeutic method to which 1,25d3-marrs of nervous disease including alzheimer disease is related |
KR101757841B1 (en) * | 2014-11-12 | 2017-07-14 | 한국생명공학연구원 | Composition for inhibiting obesity comprising complex salt of baicalin and zinc |
CN110585114A (en) * | 2019-09-30 | 2019-12-20 | 华熙生物科技股份有限公司 | Bactericidal composition for regulating skin microbial flora and application thereof |
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JPH08217672A (en) * | 1995-02-08 | 1996-08-27 | Terumo Corp | Antihelicobacter pylori agent containing xanthone derivative |
JP2003119150A (en) * | 2001-08-08 | 2003-04-23 | Oji Paper Co Ltd | Lipase inhibitor |
JP2003231607A (en) * | 2002-02-05 | 2003-08-19 | Hosoda Shc:Kk | Mangosteen extract and antimicrobial deodorant containing the same |
JP2008520585A (en) * | 2004-11-16 | 2008-06-19 | ルネサンス ハーブス インコーポレイテッド | Pharmaceutical and therapeutic composition derived from Garcinia mangostana L plant |
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JPH0517365A (en) * | 1991-07-03 | 1993-01-26 | Nonogawa Shoji Kk | Testosterone 5alpha-reductase inhibitor |
JPH08217672A (en) * | 1995-02-08 | 1996-08-27 | Terumo Corp | Antihelicobacter pylori agent containing xanthone derivative |
JP2003119150A (en) * | 2001-08-08 | 2003-04-23 | Oji Paper Co Ltd | Lipase inhibitor |
JP2003231607A (en) * | 2002-02-05 | 2003-08-19 | Hosoda Shc:Kk | Mangosteen extract and antimicrobial deodorant containing the same |
JP2008520585A (en) * | 2004-11-16 | 2008-06-19 | ルネサンス ハーブス インコーポレイテッド | Pharmaceutical and therapeutic composition derived from Garcinia mangostana L plant |
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JP2016028573A (en) * | 2013-01-21 | 2016-03-03 | レジリオ株式会社 | Therapeutic agent and therapeutic method to which 1,25d3-marrs of nervous disease including alzheimer disease is related |
KR101757841B1 (en) * | 2014-11-12 | 2017-07-14 | 한국생명공학연구원 | Composition for inhibiting obesity comprising complex salt of baicalin and zinc |
CN110585114A (en) * | 2019-09-30 | 2019-12-20 | 华熙生物科技股份有限公司 | Bactericidal composition for regulating skin microbial flora and application thereof |
CN110585114B (en) * | 2019-09-30 | 2022-06-10 | 华熙生物科技股份有限公司 | Bactericidal composition for regulating skin microbial flora and application thereof |
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