JP7013645B2 - Lipase activity inhibitor - Google Patents
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Description
本発明は、リパーゼ活性阻害剤に関する。 The present invention relates to a lipase activity inhibitor.
リパーゼは、生体内で主に消化液（胃液、膵液等）に含まれる酵素で、トリアシルグリセロールを脂肪酸とグリセリンとに分解し、脂質の消化を行う消化酵素であり、食物の消化吸収を補助する働きを担うため、生体内の各組織を活動させるために重要なものである。
一方、皮膚においては、プロピオニバクテリウム アクネス（Propionibacterium acnes）により産生されたリパーゼと、皮脂に含まれるトリアシルグリセロールが反応し、生成した遊離脂肪酸が丘疹、膿疱、結節、嚢腫といった炎症性ざ瘡の発症に関与することが知られている。また、頭部や顔面において、皮脂中に含まれるトリアシルグリセロールが癜風菌等の真菌が産生するリパーゼにより分解されて生じた遊離脂肪酸が皮膚を刺激することが知られている。また、脂漏性皮膚炎の主な原因であるといわれており、遊離脂肪酸等により頭皮の剥離が引き起こされて、フケを生じる可能性も報告されている。
さらにまた、高カロリーの食品成分を摂取した際、リパーゼは脂質を消化し、食物の消化吸収を補助する働きを担うことから、脂質等を体内に吸収させることで、肥満の一因となることが知られている。
Lipase is an enzyme mainly contained in digestive juices (gastric juice, pancreatic juice, etc.) in the living body. It is a digestive enzyme that decomposes triacylglycerol into fatty acids and glycerin to digest lipids, and assists digestion and absorption of food. It is important for activating each tissue in the living body because it plays a role in the activity.
On the other hand, in the skin, lipase produced by Propionibacterium acnes reacts with triacylglycerol contained in sebum, and the produced free fatty acids are inflammatory acne such as papules, pustules, nodules, and cysts. It is known to be involved in the onset of. Further, it is known that free fatty acids produced by decomposition of triacylglycerol contained in sebum by lipase produced by fungi such as Tinea versicolor on the head and face irritate the skin. It is also said to be the main cause of seborrheic dermatitis, and it has been reported that free fatty acids and the like may cause exfoliation of the scalp and cause dandruff.
Furthermore, when ingesting high-calorie food ingredients, lipase digests lipids and assists in the digestion and absorption of foods. Therefore, by absorbing lipids into the body, it contributes to obesity. It has been known.
そのため、医薬品、医薬部外品、化粧品又は食品においては、リパーゼ活性を阻害することで、尋常性ざ瘡や脂漏性皮膚炎を改善し、フケの発生や肥満を防止し得る薬剤が求められている。
しかし、現状では、リパーゼの活性を阻害する薬剤の有効性は未だ十分に満足できるものではない。例えば、ビワの葉抽出物（特許文献１参照）等が報告されているが、他の配合成分との関係からリパーゼ阻害効果を発揮できず、有効性において、必ずしも満足し得ないものであった。
Therefore, in pharmaceuticals, quasi-drugs, cosmetics or foods, there is a demand for a drug that can improve dandruff and seborrheic dermatitis by inhibiting lipase activity and prevent the occurrence of dandruff and obesity. ing.
However, at present, the efficacy of drugs that inhibit the activity of lipase is not yet fully satisfactory. For example, a loquat leaf extract (see Patent Document 1) has been reported, but the lipase-inhibiting effect could not be exhibited due to the relationship with other compounding ingredients, and the effectiveness was not always satisfactory. ..
本発明の目的は、上記事情に鑑み、従来のものに比べて、安定性や有効性に優れるリパーゼ活性阻害剤を提供することである。 In view of the above circumstances, an object of the present invention is to provide a lipase activity inhibitor having excellent stability and effectiveness as compared with conventional ones.
本発明者らは、上記課題を解決するために、リパーゼ活性阻害剤について、様々な植物を用いて鋭意研究を重ねてきた。その結果、バラ科のアンズの果汁が優れたリパーゼ活性阻害作用を有し、しかも安定性にも優れることを見出した。さらに、アンズの果汁と、ペカン抽出物とを組み合わせることで、アンズの果汁を単独で用いる場合に比べてリパーゼ活性阻害作用がさらに高められることを見出し、本発明を完成するに至った。 In order to solve the above problems, the present inventors have been diligently studying lipase activity inhibitors using various plants. As a result, it was found that the juice of apricots of the Rosaceae family has an excellent lipase activity inhibitory action and is also excellent in stability. Furthermore, they have found that the combination of apricot juice and pecan extract further enhances the lipase activity inhibitory action as compared with the case where apricot juice is used alone, and completed the present invention.
すなわち、本発明は以下に関する。
［１］アンズの果汁を含有する、リパーゼ活性阻害剤。
［２］さらに、ペカン（Carya illinoensis）抽出物を含有する、［１］に記載のリパーゼ活性阻害剤。
That is, the present invention relates to the following.
[1] A lipase activity inhibitor containing apricot juice.
[2] The lipase activity inhibitor according to [1], which further contains a pecan (Carya illinoensis) extract.
本発明のリパーゼ活性阻害剤は、安定性および有効性に優れる。 The lipase activity inhibitor of the present invention is excellent in stability and efficacy.
以下、本発明の実施形態を説明する。本発明のリパーゼ活性阻害剤は、アンズ果汁を含有する。また、本発明のリパーゼ活性阻害剤は、さらにペカン抽出物を含有する。
まず本発明に用いられるアンズ果汁とペカン抽出物について説明する。
Hereinafter, embodiments of the present invention will be described. The lipase activity inhibitor of the present invention contains apricot juice. In addition, the lipase activity inhibitor of the present invention further contains a pecan extract.
First, apricot juice and pecan extract used in the present invention will be described.
［アンズ果汁］
本発明において用いるアンズ果汁は、バラ科（Ｒｏｓａｃｅａｅ）サクラ（Ｐｒｕｎｕｓ）属に属する落葉小高木であるホンアンズ（Ｐｒｕｎｕｓ ａｒｍｅｎｉｃａ Ｌ．）、ホンアンズの栽培品種であるアンズ（Ｐｒｕｎｕｓ ａｒｍｅｎｉａｃａ Ｌ．ｖａｒ． ａｎｓｕ Ｍａｘｉｍ．）、マンシュウアンズ（Ｐｒｕｎｕｓ ｍａｎｄｓｈｕｒｉｃａ Ｋｏｅｈｎｅ）およびモウコアンズ（Ｐｒｕｎｕｓ ｓｉｂｉｒｉｃａ Ｌ．）等の果実から得られる果汁である。
本発明の目的には、ホンアンズ、アンズおよびマンシュウアンズの果実から得られる果汁が好ましく、ホンアンズおよびアンズの果実から得られる果汁がより好ましい。
[Apricot juice]
The apricot juice used in the present invention is apricot (Prunus armenica L.), which is a deciduous small tree belonging to the genus Plum of the family Rosaceae, and an apricot (Prunus armeniaca L. var. Ansu Maxi), which is a cultivated variety of apricots. ), Prunus mandhurica Koehne and Prunus sibilica L., and the like.
For the purposes of the present invention, fruit juices obtained from fruits of apricots, apricots and apricots are preferable, and juices obtained from fruits of apricots and apricots are more preferable.
本発明においては、ホンアンズ、アンズ等の果実を圧搾して得られた果汁をそのまま使用してもよく、あるいはそれをさらに濃縮した濃縮果汁を使用してもよい。また、果実を圧搾して得られた果汁やその濃縮果汁に、ろ過、遠心分離、各種溶媒による希釈、カラム等による分画等の処理を施して得られた処理物を使用することも可能である。すなわち、本発明における「果汁」とは、果実を圧搾して得た果汁そのもの、濃縮果汁若しくはこれらの処理物をいう。なお、果実から果汁を得るための手段および果汁に対する処理には、水や有機溶媒による抽出は含まれない。
本発明においては、アンズ果汁として、アンズの果実を圧搾して調製した果汁や、さらに濃縮または種々の処理を行って得られた果汁を用いることができるが、例えば、グリセリンを１５質量％、水を４５質量％含有するアンズ果汁である「アンズ果汁ＰＨ」（日油株式会社製）等の市販の製品を用いることもできる。
In the present invention, fruit juice obtained by pressing fruits such as apricots and apricots may be used as it is, or concentrated juice obtained by further concentrating the juice may be used. It is also possible to use a processed product obtained by subjecting a fruit juice obtained by pressing a fruit or a concentrated fruit juice thereof to treatments such as filtration, centrifugation, dilution with various solvents, and fractionation with a column or the like. be. That is, the "fruit juice" in the present invention refers to the fruit juice itself obtained by pressing the fruit, the concentrated fruit juice, or a processed product thereof. The means for obtaining fruit juice from the fruit and the treatment for the fruit juice do not include extraction with water or an organic solvent.
In the present invention, as the apricot juice, a fruit juice prepared by pressing the apricot fruit or a fruit juice obtained by further concentration or various treatments can be used. For example, 15% by mass of glycerin and water can be used. Commercially available products such as "Apricot juice PH" (manufactured by Nichiyu Co., Ltd.), which is an apricot juice containing 45% by mass of apricot juice, can also be used.
［ペカン抽出物］
本発明において用いられるペカン抽出物は、クルミ科ペカン属に属する落葉高木であるペカン（ピカンまたはピーカン）（Carya illinoensis）の抽出物である。本発明の目的には、果実、種子等の抽出物が好ましく用いられ、種子または種子殻の抽出物がより好ましく用いられる。
ペカンの抽出物は、種子または種子殻をそのままもしくは乾燥した後に、ヘキサン、ベンゼン等の炭化水素類、酢酸エチル等のエステル類、アセトン等のケトン類、ジエチルエーテル、テトラヒドロフラン等のエーテル類、クロロホルム、塩化メチレン等のハロゲン化炭化水素類、低級アルコール、多価アルコール等のアルコール類および水等の溶媒の１種または２種以上とともに加熱還流し、あるいは前記溶媒の１種又は２種以上により抽出して得られる。中でも、水およびメタノール、エタノール、プロパノール、イソプロパノール等の低級アルコールから選ばれる１種または２種以上で抽出して得た抽出物が好ましく、水で抽出して得た抽出物がさらに好ましい。
[Pecan extract]
The pecan extract used in the present invention is an extract of pecan (pican or pecan) (Carya illinoensis), which is a deciduous tree belonging to the genus Hickory of the family Walnut. For the purposes of the present invention, extracts such as fruits and seeds are preferably used, and extracts of seeds or seed husks are more preferably used.
The extract of pecan is obtained from the seeds or seed husks as they are or after drying, hydrocarbons such as hexane and benzene, esters such as ethyl acetate, ketones such as acetone, ethers such as diethyl ether and tetrahydrofuran, chloroform, etc. Heat-refluxed with one or more of a halogenated hydrocarbon such as methylene chloride, an alcohol such as a lower alcohol and a polyhydric alcohol, and a solvent such as water, or extracted with one or more of the above solvents. Obtained. Among them, an extract obtained by extracting with one or more kinds selected from water and lower alcohols such as methanol, ethanol, propanol and isopropanol is preferable, and an extract obtained by extracting with water is more preferable.
具体的な抽出方法としては、特開２０００－０７２６８６号公報に記載された以下の方法が挙げられる。
まず、種子または種子殻をそのままあるいは乾燥処理した後破砕し、その重量の５倍～１００倍量程度の抽出溶媒に浸漬し、又は前記溶媒中で撹拌、破砕等を行うことにより抽出する。抽出温度は、使用する抽出溶媒の種類に応じて適宜決定される。例えば抽出溶媒が水である場合には、抽出温度は通常２０℃～１２０℃程度であり、抽出溶媒が低級アルコールの場合、通常２０℃～５０℃程度、好ましくは室温である。抽出処理後、ろ過、遠心分離などの手段により固液分離して抽出物を得る。
Specific examples of the extraction method include the following methods described in Japanese Patent Application Laid-Open No. 2000-072686.
First, the seeds or seed husks are extracted as they are or after being dried and crushed, immersed in an extraction solvent having an amount of about 5 to 100 times the weight thereof, or stirred or crushed in the solvent. The extraction temperature is appropriately determined according to the type of extraction solvent used. For example, when the extraction solvent is water, the extraction temperature is usually about 20 ° C. to 120 ° C., and when the extraction solvent is a lower alcohol, it is usually about 20 ° C. to 50 ° C., preferably room temperature. After the extraction treatment, solid-liquid separation is performed by means such as filtration and centrifugation to obtain an extract.
抽出物はそのまま用いてもよく、常法に従って抽出溶媒を留去して濃縮し、必要に応じて精製、乾燥等の処理を行って用いてもよい。また、乾燥した抽出物を、水、エタノール、１，３－ブチレングリコール等の１種または２種以上の溶媒で溶解して用いてもよい。
本発明においては、ペカンから上記の方法により抽出物を得て用いてもよいが、「ピーカンナッツエキスＢＧ－２」（日油株式会社製）等の市販の製品を用いることもできる。
The extract may be used as it is, or the extraction solvent may be distilled off and concentrated according to a conventional method, and if necessary, treatments such as purification and drying may be performed before use. Further, the dried extract may be used by dissolving it in one or more kinds of solvents such as water, ethanol and 1,3-butylene glycol.
In the present invention, an extract may be obtained from Pecan by the above method and used, but a commercially available product such as "Pecan Nut Extract BG-2" (manufactured by NOF CORPORATION) can also be used.
［リパーゼ活性阻害剤］
本発明のリパーゼ活性阻害剤は、上記のアンズ果汁、あるいは上記のアンズ果汁およびペカン抽出物に、必要に応じて、製剤化に際して汎用される一般的な添加剤を加え、通常の製剤化手段、たとえば第十七改正日本薬局方製剤総則［３］製剤各条に記載された方法等に従って、液状、懸濁液状、乳液状、クリーム状、ゲル状、粉末状、顆粒状、タブレット状、カプセル状等の種々の形態の製剤とすることができる。
[Lipase activity inhibitor]
The lipase activity inhibitor of the present invention is prepared by adding, if necessary, a general additive commonly used for formulation to the above-mentioned apricot juice or the above-mentioned apricot juice and pecan extract, and the usual formulation means. For example, according to the method described in the 17th revised Japanese Pharmacopoeia General Provisions [3] Formulation Articles, liquid, suspension, milky, cream, gel, powder, granule, tablet, capsule. It can be prepared in various forms such as.
本発明のリパーゼ活性阻害剤におけるアンズ果汁の含有量は、リパーゼ活性阻害剤の全量に対し、乾燥残留物重量にして好ましくは０．０４重量％～４０重量％であり、より好ましくは０．４重量％～１０重量％である。
また、本発明のリパーゼ活性阻害剤がさらにペカン抽出物を含有する場合、ペカン抽出物の含有量は、リパーゼ活性阻害剤の全量に対し、乾燥残留物重量にして好ましくは０．００１重量％～１重量％であり、より好ましくは０．０１重量％～０．５重量％である。
アンズ果汁とペカン抽出物との含有量比（アンズ果汁：ペカン抽出物）は、乾燥残留物の重量比にして１０００:１～１：１であることが好ましく、４００：１～４：１であることがより好ましい。
なお、ここで「乾燥残留物重量」とは、各抽出物を乾固した際の残留分の重量をいう。
The content of apricot juice in the lipase activity inhibitor of the present invention is preferably 0.04% by weight to 40% by weight, more preferably 0.4% by weight, based on the total amount of the lipase activity inhibitor. It is 10% by weight by weight.
When the lipase activity inhibitor of the present invention further contains a pecan extract, the content of the pecan extract is preferably 0.001% by weight or more in terms of the weight of the dry residue with respect to the total amount of the lipase activity inhibitor. It is 1% by weight, more preferably 0.01% by weight to 0.5% by weight.
The content ratio of apricot juice to pecan extract (apricot juice: pecan extract) is preferably 1000: 1 to 1: 1 and 400: 1 to 4: 1 in terms of the weight ratio of the dry residue. It is more preferable to have.
Here, the "weight of dry residue" means the weight of the residue when each extract is dried to dryness.
本発明のリパーゼ活性阻害剤に含有され得る添加剤としては、賦形剤、結合剤、崩壊剤、滑沢剤、被覆剤、基剤、溶剤、溶解補助剤、可溶化剤、懸濁化剤、分散剤、乳化剤、安定化剤、抗酸化剤、粘稠化剤、保存剤、ｐＨ調整剤、矯味剤、香料、着色剤等が挙げられ、これらは、本発明の特徴を損なわない範囲で、１種または２種以上を用いることができる。 Additives that can be contained in the lipase activity inhibitor of the present invention include excipients, binders, disintegrants, lubricants, coatings, bases, solvents, lysis aids, solubilizers and suspending agents. , Dispersants, emulsifiers, stabilizers, antioxidants, thickeners, preservatives, pH regulators, flavoring agents, fragrances, colorants, etc., as long as they do not impair the characteristics of the present invention. One kind or two or more kinds can be used.
本発明のリパーゼ活性阻害剤は、そのまま、または必要に応じて上記した一般的な添加剤を加えて、医薬品、医薬部外品、食品、化粧品等とすることができる。 The lipase activity inhibitor of the present invention can be made into a drug, a quasi-drug, a food, a cosmetic, etc. as it is or by adding the above-mentioned general additives as needed.
以下、実施例および比較例を挙げて、本発明をさらに具体的に説明する。 Hereinafter, the present invention will be described in more detail with reference to Examples and Comparative Examples.
［実施例１～４］リパーゼ活性阻害剤
表１に示す処方に従い、実施例１～４のリパーゼ活性阻害剤および比較例１～３の組成物を調製した。その際に用いたアンズ果汁［（ａ）成分］およびペカン抽出物［（ｂ）成分］、ならびに、アンズと同様にバラ科（Rosaceae）の植物であるモモ（Amygdalus persica L.）およびリンゴ（Malus pumila）の果汁［（ａ’）成分］については、以下の通りである。
（ａ）成分：アンズ果汁
アンズ果汁としては、「アンズ果汁ＰＨ」（日油株式会社製）を使用した。なお、該果汁の乾燥残留物量は、４０質量％であった。
（ａ’）成分：モモ果汁、リンゴ果汁
モモ果汁としては、「Ｈｏｒｍｏ Ｆｒｕｉｔ Ｐｅａｃｈ／Ｎ」（香栄興業株式会社製）、リンゴ果汁としては、「Ｈｏｒｍｏ Ｆｒｕｉｔ Ａｐｐｌｅ／Ｎ」（香栄興業株式会社製）を使用した。なお、該果汁の乾燥残留物量は、それぞれ３０質量％であった。
（ｂ）成分：ペカン抽出物
ペカン抽出物としては、「ピーカンナッツエキスＢＧ－２」（日油株式会社製）を使用した。なお、該抽出物の乾燥残留物量は、１．０質量％であった。
[Examples 1 to 4] Lipase activity inhibitor According to the formulation shown in Table 1, the lipase activity inhibitor of Examples 1 to 4 and the composition of Comparative Examples 1 to 3 were prepared. The apricot juice [(a) component] and pecan extract [(b) component] used at that time, and peaches (Amygdalus persica L.) and apples (Malus), which are plants of the Rosaceae family (Rosaceae) as well as apricots. The fruit juice [(a') component] of pumila) is as follows.
(A) Ingredient: Apricot juice As the apricot juice, "Apricot juice PH" (manufactured by NOF CORPORATION) was used. The amount of dry residue of the fruit juice was 40% by mass.
(A') Ingredients: peach juice, apple juice As peach juice, "Hormo Fruit Peach / N" (manufactured by Koei Kogyo Co., Ltd.), and as apple juice, "Hormo Fruit Apple / N" (Koei Kogyo Co., Ltd.) Made) was used. The amount of dry residue of the fruit juice was 30% by mass, respectively.
(B) Ingredient: Pecan extract As the pecan extract, "pecan nut extract BG-2" (manufactured by NOF CORPORATION) was used. The amount of dry residue of the extract was 1.0% by mass.
［試験例１］リパーゼ活性阻害試験
実施例１～４の各リパーゼ活性阻害剤および比較例１～３の組成物について、下記の方法によりリパーゼ活性阻害試験を行った。
リパーゼ阻害活性の測定は、ブタ膵臓由来リパーゼ（シグマアルドリッチ社製）および「リパーゼキットＳ」（大日本住友製薬株式会社製）を用いて行った。測定は、製造者の説明書を一部改変して行った。
すなわち、９６ウェルプレートに、各試料溶液（実施例のリパーゼ活性阻害剤および比較例の組成物）１０μＬ（盲検用は５０体積％１，３－ブチレングリコール水溶液１０μＬ）、酵素溶液（ブタ膵臓由来リパーゼ０．１２５ｍｇ／ｍＬ、０．１Ｍクエン酸緩衝液（ｐＨ＝６．０）の溶液）１０μＬ、発色液（０．５ｍｇ／ｍＬの５，５’－ジチオビス（２－ニトロ安息香酸）を含む緩衝液）７０μＬ、エラスターゼ活性阻害剤（フェニルメチルスルホニルフルオキシド）２μＬを入れた後、３０℃で５分間予熱し、基質液（三酪酸ジメルカプロール＋ドデシル硫酸ナトリウム）８μＬを加えた後、遮光下にて３０℃で３０分間反応させた。その後、反応停止液１５０μＬを添加して反応を停止させた。
ブランクとしては、試料溶液、酵素溶液、エラスターゼ活性阻害剤、発色液を添加して３０℃で５分間予熱し、３０℃で３０分間加熱した。３０分後、基質液を添加した後、直ちに反応停止液を加えた。
各試料の吸光度を波長４１２ｎｍで測定し、リパーゼ活性阻害率を下記の式を用いて算出した。その結果を表１に併せて示した。
[Test Example 1] Lipase activity inhibition test A lipase activity inhibition test was carried out for each lipase activity inhibitor of Examples 1 to 4 and the compositions of Comparative Examples 1 to 3 by the following method.
The lipase inhibitory activity was measured using porcine pancreas-derived lipase (manufactured by Sigma-Aldrich) and "Lipase Kit S" (manufactured by Sumitomo Dainippon Pharma Co., Ltd.). The measurement was performed by partially modifying the manufacturer's instruction manual.
That is, in a 96-well plate, 10 μL of each sample solution (lipase activity inhibitor of Example and composition of Comparative Example) (50% by volume 1,3-butylene glycol aqueous solution 10 μL for blinding), enzyme solution (derived from porcine pancreas). Contains 10 μL of lipase 0.125 mg / mL, 0.1 M citrate buffer (pH = 6.0) solution), and color-developing solution (0.5 mg / mL 5,5'-dithiobis (2-nitrobenzoic acid). After adding 70 μL of buffer solution and 2 μL of elastase activity inhibitor (phenylmethylsulfonylfluoride), preheat at 30 ° C. for 5 minutes, add 8 μL of substrate solution (dimercaprol tributyrate + sodium dodecyl sulfate), and then shield from light. The reaction was carried out at 30 ° C. for 30 minutes underneath. Then, 150 μL of the reaction stop solution was added to stop the reaction.
As a blank, a sample solution, an enzyme solution, an elastase activity inhibitor, and a color-developing solution were added and preheated at 30 ° C. for 5 minutes, and then heated at 30 ° C. for 30 minutes. After 30 minutes, the substrate solution was added, and then the reaction stop solution was immediately added.
The absorbance of each sample was measured at a wavelength of 412 nm, and the lipase activity inhibition rate was calculated using the following formula. The results are also shown in Table 1.
リパーゼ活性阻害率（％）＝１００－（Ａ－Ｃ１）／（Ｂ－Ｃ２）×１００
Ａ：実施例および比較例の各試料を用い３０分間反応させた時の吸光度
Ｂ：５０体積％１，３－ブチレングリコール水溶液を用い３０分間反応させた時の吸光度
Ｃ１：実施例および比較例の各試料を用い、かつ基質液を添加しないで３０分間反応させた時の吸光度
Ｃ２：５０体積％１，３－ブチレングリコール水溶液を用い、かつ基質液を添加しないで３０分間反応させた時の吸光度
Lipase activity inhibition rate (%) = 100- (AC 1 ) / (BC 2 ) x 100
A: Absorbance when reacted for 30 minutes using each sample of Example and Comparative Example B: Absorbance when reacting for 30 minutes using 50% by volume 1,3-butylene glycol aqueous solution C 1 : Examples and Comparative Example Absorbance when reacted for 30 minutes without adding the substrate solution using each sample of C 2 : 50% by volume When using an aqueous solution of 1,3-butylene glycol and reacting for 30 minutes without adding the substrate solution Absorbance of
表１に示されるように、アンズ果汁を含有する実施例１、２のリパーゼ活性阻害剤は、良好なリパーゼ活性阻害作用を有しており、アンズ果汁の濃度依存的にリパーゼ活性阻害作用が向上することが認められた。
一方、アンズと同様にバラ科の植物であるリンゴやモモの果汁を含有する比較例１、２の各組成物については、有効なリパーゼ阻害作用は認められなかった。
また、アンズ果汁とペカン抽出物を含有する実施例３、４のリパーゼ活性阻害剤では、アンズ果汁を単独で含有する場合に比べ、更にリパーゼ活性阻害作用が向上することが示された。
これに対し、ペカン抽出物のみを含有する比較例３の組成物については、有効なリパーゼ活性の阻害作用は認められなかった。
As shown in Table 1, the lipase activity inhibitors of Examples 1 and 2 containing apricot juice have a good lipase activity inhibitory action, and the lipase activity inhibitory action is improved depending on the concentration of apricot juice. Was allowed to do.
On the other hand, no effective lipase-inhibiting effect was observed in each of the compositions of Comparative Examples 1 and 2 containing the juices of apples and peaches, which are plants of the Rosaceae family as in apricots.
Further, it was shown that the lipase activity inhibitor of Examples 3 and 4 containing apricot juice and pecan extract further improved the lipase activity inhibitory action as compared with the case of containing apricot juice alone.
On the other hand, no effective inhibitory effect on lipase activity was observed in the composition of Comparative Example 3 containing only the pecan extract.
［実施例５～８および比較例４］リパーゼ活性阻害剤（化粧水）
表２に示す処方に従い、リパーゼ活性阻害剤を化粧水として調製した。
その際に用いたアンズ果汁［（ａ）成分］およびペカン抽出物［（ｂ）成分］については、上記実施例１～４のリパーゼ活性阻害剤の調製に用いたものと同様である。また、特許文献１にてリパーゼ活性阻害効果が報告されているビワの葉抽出物［（ａ’）成分］として、「ビワ抽出液ＢＧ－Ｊ」（乾燥残留物量＝１．５質量％、丸善製薬株式会社製）を用いた。
＜製造方法＞
まず、ペンチレングリコール及びグリセリンをイオン交換水に添加して混合し、７５℃～８５℃で加熱溶解した。均一に溶解した後、冷却して、（ａ）成分、（ａ’）成分、（ｂ）成分およびフェノキシエタノールを添加して混合し、化粧水を得た。
[Examples 5 to 8 and Comparative Example 4] Lipase activity inhibitor (toner)
A lipase activity inhibitor was prepared as a lotion according to the formulation shown in Table 2.
The apricot juice [(a) component] and the pecan extract [(b) component] used at that time are the same as those used for preparing the lipase activity inhibitors of Examples 1 to 4 above. Further, as the loquat leaf extract [(a') component] for which the lipase activity inhibitory effect has been reported in Patent Document 1, "loquat extract BG-J" (dry residue amount = 1.5% by mass, Maruzen) (Manufactured by Pharmaceutical Co., Ltd.) was used.
<Manufacturing method>
First, pentylene glycol and glycerin were added to ion-exchanged water, mixed, and dissolved by heating at 75 ° C to 85 ° C. After uniformly dissolving, the mixture was cooled, and the component (a), the component (a'), the component (b) and phenoxyethanol were added and mixed to obtain a cosmetic water.
これらの経時安定性について、各化粧水を透明ガラス容器に密封して０℃、２５℃、４０℃でそれぞれ３ヶ月間保存し、その外観を観察して、下記評価基準により評価し、判定を行った。結果を表２に併せて示した。
＜評価基準＞
○：安定性良好（いずれの温度においても外観の変化がない。）
×：安定性不良（いずれかの温度において澱（おり）、沈殿を生じるもしくは分離する、または変色が著しい。）
Regarding these stability over time, each lotion is sealed in a transparent glass container and stored at 0 ° C, 25 ° C, and 40 ° C for 3 months, respectively, and the appearance is observed and evaluated according to the following evaluation criteria to make a judgment. went. The results are also shown in Table 2.
<Evaluation criteria>
◯: Good stability (the appearance does not change at any temperature)
X: Poor stability (precipitation occurs or separates at any temperature, or discoloration is significant)
表２に示されるように、アンズ果汁を含有する実施例５、６、アンズ果汁とペカン抽出物を含有する実施例７、８の各リパーゼ活性阻害剤は、化粧水として調製した場合において、いずれも経時安定性に優れていることが認められた。
一方、（ａ）成分の代わりに、特許文献１にてリパーゼ活性阻害効果が報告されているビワの葉抽出物を含有する比較例４のリパーゼ活性阻害剤は、化粧水として調製した場合、経時で澱の発生が確認され、経時的な安定性に劣ることが認められた。
As shown in Table 2, each lipase activity inhibitor of Examples 5 and 6 containing apricot juice and Examples 7 and 8 containing apricot juice and pecan extract was prepared as a lotion, and any of them Was also found to be excellent in stability over time.
On the other hand, the lipase activity inhibitor of Comparative Example 4, which contains a loquat leaf extract whose lipase activity inhibitory effect has been reported in Patent Document 1 instead of the component (a), is prepared as a cosmetic water over time. The occurrence of starch was confirmed in the plant, and it was confirmed that the stability over time was inferior.
以上詳述したように、本発明により、安定性および有効性に優れるリパーゼ活性阻害剤を提供することができる。
本発明のリパーゼ活性阻害剤は、医薬品、医薬部外品、化粧品または食品として利用することができる。
As described in detail above, the present invention can provide a lipase activity inhibitor having excellent stability and effectiveness.
The lipase activity inhibitor of the present invention can be used as a pharmaceutical product, a quasi drug, a cosmetic product or a food product.
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