JP5431157B2 - Composition for preventing UV injury for ingestion - Google Patents
Composition for preventing UV injury for ingestion Download PDFInfo
- Publication number
- JP5431157B2 JP5431157B2 JP2009526495A JP2009526495A JP5431157B2 JP 5431157 B2 JP5431157 B2 JP 5431157B2 JP 2009526495 A JP2009526495 A JP 2009526495A JP 2009526495 A JP2009526495 A JP 2009526495A JP 5431157 B2 JP5431157 B2 JP 5431157B2
- Authority
- JP
- Japan
- Prior art keywords
- composition
- preventing
- injury
- oral
- ultraviolet rays
- 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.)
- Expired - Fee Related
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Description
本発明は、経口摂取用紫外線傷害防止組成物に関し、更に詳しくは、特定の植物から得られた組成物から得られた経口摂取用の紫外線傷害防止組成物に関する。 The present invention relates to an ultraviolet injury prevention composition for oral consumption, and more particularly to an ultraviolet injury prevention composition for oral consumption obtained from a composition obtained from a specific plant.
皮膚が紫外線に暴露されると紅斑や浮腫等、様々な傷害が発生し、それらが皮膚の肥厚や弾性喪失、シワの発生、色素沈着異常等の光老化や皮膚がんの原因になると考えられている。そして、紫外線による傷害を防止する手段としては、紫外線を遮断する皮膚外用剤を皮膚に塗布することが一般的であった。 When skin is exposed to ultraviolet rays, various injuries such as erythema and edema occur, which may cause photoaging and skin cancer such as thickening and loss of elasticity, wrinkles, and abnormal pigmentation. ing. As a means for preventing injury due to ultraviolet rays, it has been common to apply a skin external preparation that blocks ultraviolet rays to the skin.
しかしながら、皮膚外用剤を身体の露出部分に塗布することは手間と時間がかかること、また発汗や水に触れると効果が消失することから、より手軽で有効な紫外線対策の手段が望まれていた。 However, applying a topical skin preparation to exposed parts of the body is time consuming and time consuming, and since the effect disappears when it is exposed to sweat or water, a simpler and more effective means for preventing ultraviolet rays has been desired. .
そこで、紫外線による皮膚の傷害を軽減することを目的に、経口摂取によって皮膚を紫外線から保護する効果のある薬理成分について研究がなされている。例えば、カロチノイドやビタミンEを経口摂取することにより、紫外線による皮膚の炎症(紅斑)が抑制されることが知られている。 Therefore, studies have been made on pharmacological components that have an effect of protecting the skin from ultraviolet rays by ingestion for the purpose of reducing skin damage caused by ultraviolet rays. For example, it is known that oral intake of carotenoids and vitamin E suppresses skin inflammation (erythema) caused by ultraviolet rays.
また、特許文献1には、バラやキクの抽出エキスを有効成分とする経口用メラニン生成抑制組成物が記載されている。また、特許文献2には、シリマリン等の抽出エキスを含有する経口美白剤が記載されている。また、特許文献3には、ローズマリー抽出エキス、セージ抽出エキス等を含有する経口投与用組成物とその組成物を含有する美白剤や飲食品が記載されている。また、特許文献4には、ジヒドロオイデスモール又はその配糖体を含有する経口美白剤が記載されている。また、特許文献5には、クリプトキサンチンとシステインを含有する経口投与組成物とそれを有効成分とする美白剤が記載されている。また、特許文献6には、オリーブの果実から得られる水溶液を含有する紫外線傷害予防剤が記載されている。また、特許文献7には、発芽ブロッコリー由来成分を含有する経口摂取が可能な美白用組成物が記載されている。
しかしながら、メロン抽出物を含有する経口摂取用の紫外線傷害防止組成物についての検討は数少ない。 However, there have been few studies on compositions for preventing UV injury for oral consumption containing melon extract.
一方、メロン抽出物を含有する外用剤や皮膚化粧料は知られている(特許文献8及び特許文献9)。しかしながら、上記したように、外用剤を塗布することは面倒であり、また発汗等により効果が消失するという問題点に加え、一般的な単なるメロン抽出物を含有するこれらは、外用剤や皮膚化粧料としても到底十分なものではなかった。 On the other hand, external preparations and skin cosmetics containing a melon extract are known (Patent Document 8 and Patent Document 9). However, as described above, it is troublesome to apply an external preparation, and in addition to the problem that the effect is lost due to perspiration, etc., these containing a general simple melon extract are used for external preparations and skin cosmetics. The fee was not enough.
メロンのなかでも、キューカミス・メロという品種のメロンにおいて、長期間放置しても果実表面に変化が起こらない変種が知られており、このキューカミス・メロの変種の果実からの抽出物よりなる「酸化防止能をもつ可溶性タンパク質抽出物」が知られている(特許文献10)。しかしながら、この文献は、該抽出物がスーパーオキシドジスムターゼ酵素活性を有することの基礎的検討に関するものであり、経口摂取用の紫外線傷害防止能については全く検討されていなかった。 Among the melons, there is a known variety of melons with the varieties of Kukamis and Melo that do not change on the fruit surface even if left for a long period of time. A “soluble protein extract having a preventive ability” is known (Patent Document 10). However, this document relates to a basic examination that the extract has a superoxide dismutase enzyme activity, and the ability to prevent UV damage for oral intake has not been studied at all.
また、このキューカミス・メロの変種の果実からの抽出物を含有した皮膚化粧料(スキンケア組成物)が知られている(特許文献11)。しかしながら、これは、外用剤や皮膚化粧料としてはある程度の効果はあるものの、経口摂取用のものではなく、キューカミス・メロの変種の果実からの抽出物を含有した経口摂取用の紫外線傷害防止組成物については全く検討されていなかった。 In addition, a skin cosmetic (skin care composition) containing an extract from the fruit of this Kukamis-Mello variety is known (Patent Document 11). However, although this is effective to some extent as an external preparation or a skin cosmetic, it is not intended for oral consumption, but it contains an extract from the fruit of a variety of Cucamis melo varieties, and it is an ultraviolet radiation injury prevention composition for oral consumption. The thing was not examined at all.
また、キューカミス・メロの変種の果実からの抽出物を経口摂取させたヒトに対して、1時間2.5気圧の純酸素吸入の条件に晒すと、経口摂取させていないヒトに比べて、白血球内のDNAの損傷が抑制されるという研究結果もあるが(非特許文献1)、紫外線傷害防止については全く検討がなされていなかった。 In addition, when humans that were orally ingested an extract from the fruit of a variety of Cucamis melo varieties were exposed to 2.5 atmospheres of pure oxygen inhalation for 1 hour, leukocytes were compared to humans that were not orally ingested. Although there is a research result that DNA damage is suppressed (Non-Patent Document 1), there has been no study on prevention of ultraviolet ray injury.
そこで、経口摂取することによって、紫外線による傷害を防止する効果に優れている組成物が望まれていた。 Therefore, there has been a demand for a composition that is excellent in the effect of preventing damage caused by ultraviolet rays when taken orally.
本発明は上記背景技術に鑑みてなされたものであり、その課題は、皮膚が紫外線に暴露されることにより誘発される傷害を効果的に防止及び/又は抑制する「経口摂取用の組成物」を提供することにある。また、紫外線による紅斑(発赤)発生前の肌の赤味を低くすることができ、美白効果がある「経口摂取用の組成物」を提供することにある。 The present invention has been made in view of the above-described background art, and the problem is that “a composition for oral consumption” effectively prevents and / or suppresses injury caused by exposure of the skin to ultraviolet rays. Is to provide. Another object of the present invention is to provide an “oral intake composition” that can reduce the redness of the skin before the occurrence of erythema (redness) due to ultraviolet rays and has a whitening effect.
本発明者は、上記の課題を解決すべく鋭意検討を重ねた結果、特定の植物の特定の変種の特定の部分から得られた組成物を含有することによって、経口摂取によって紫外線傷害を極めて効果的に防止できることを見出し、本発明を完成するに至った。 As a result of intensive studies to solve the above-mentioned problems, the inventor of the present invention contains a composition obtained from a specific part of a specific variety of a specific plant, so that it is extremely effective for UV damage by ingestion. As a result, the present invention has been completed.
すなわち本発明は、キューカミス・メロの変種の果実から得られた成分を含有することを特徴とする経口摂取用紫外線傷害防止組成物を提供するものである。 That is, the present invention provides a composition for preventing UV injury for oral consumption, which comprises a component obtained from the fruit of a variety of Cucumis melo.
また本発明は、上記の経口摂取用紫外線傷害防止組成物を腸溶被覆剤で被覆してなることを特徴とする経口剤を提供するものである。 The present invention also provides an oral preparation characterized by coating the above-mentioned composition for preventing UV injury for oral intake with an enteric coating agent.
また本発明は、上記の経口剤を含有することを特徴とする経口摂取用スキンケア品を提供するものである。また本発明は、上記の経口剤を含有することを特徴とする飲食品を提供するものである。 The present invention also provides a skin care product for ingestion characterized by containing the above-mentioned oral preparation. Moreover, this invention provides the food-drinks characterized by containing said oral preparation.
本発明によれば、経口摂取によって、優れた紫外線傷害抑制効果や紫外線傷害防止効果を有する組成物を提供することができる。また、紫外線照射による紅斑(発赤)発生前の肌の赤味を低くすることができ、すなわち美白効果がある「経口摂取用の組成物」を提供することができる。 ADVANTAGE OF THE INVENTION According to this invention, the composition which has the outstanding ultraviolet-ray injury inhibitory effect and ultraviolet-ray injury prevention effect by oral ingestion can be provided. Moreover, the redness of the skin before erythema (redness) generation | occurrence | production by ultraviolet irradiation can be made low, ie, the "composition for ingestion" with a whitening effect can be provided.
以下、本発明について説明するが、本発明は以下の実施の形態に限定されるものではなく、本発明の技術的範囲の範囲内で任意に変形したものも含まれるものである。 Hereinafter, the present invention will be described, but the present invention is not limited to the following embodiments, and includes any modifications within the technical scope of the present invention.
<キューカミス・メロの変種の果実から得られた成分>
[特定メロン]
本発明の経口摂取用紫外線傷害防止組成物は、「キューカミス・メロ」なるメロンの1品種の更にその特定の変種の果実(以下、「特定メロン」と略記する)から得られた組成物を含有する。本発明におけるキューカミス・メロの変種とは、その所有者が出願人である国際公開パンフレットWO92/02622に記載されているものをいう。また、ブダペスト協定に従って1990年7月19日に、第40310号として、NCIMBコレクション(National Collection of Industrial and Marine Bacteria‐ABERDEEN AB2 IRY(Scotland-GB)23 St.Machar Drive )に種子が寄託されているメロン株95LS444から出発し、ハイブリッド形成によって得られる、ヴァクルシーン(Vauclusien)、クリッパ(Clipper)又はサポータ(Supporter)タイプの変種をいう。<Ingredients obtained from the fruit of Kukamisu Melo variety>
[Specific melon]
The composition for preventing UV injury for oral consumption according to the present invention contains a composition obtained from the fruit of a specific variant of one melon of “Cucamis Melo” (hereinafter abbreviated as “specific melon”). To do. The variant of Cucumis melo in the present invention refers to that described in International Publication Pamphlet WO92 / 02622, the owner of which is the applicant. In addition, seeds were deposited in the NCIMB collection (National Collection of Industrial and Marine Bacteria-ABERDEEN AB2 IRY (Scotland-GB) 23 St. Machar Drive) as No. 40310 on July 19, 1990 in accordance with the Budapest Agreement. A variant of the Vauclusien, Clipper or Supporter type obtained from the melon strain 95LS444 and obtained by hybridization.
本発明におけるキューカミス・メロの変種として特に好適には、95LS444細胞株、95LS444細胞株由来のハイブリッド株等である。 Particularly preferred as a variant of Cucumis melo in the present invention is 95LS444 cell line, hybrid strain derived from 95LS444 cell line, and the like.
特定メロンは、遺伝子交差によって得られたメロン変種であり、約5日間という従来の種類の保存期間よりも長い保存期間(10〜14日以上)を有している。すなわち、特定メロンは、常温、常圧放置12日後でもメロン表面に皺ができない。特定メロンではない通常のメロンは、常温、常圧放置後約5日で、表面に皺等の変化が起きてしまうので、本発明には適していない。 The specific melon is a melon variant obtained by gene crossing and has a storage period (10 to 14 days or more) longer than the conventional type of storage period of about 5 days. That is, the specific melon does not wrinkle on the surface of the melon even after 12 days at room temperature and normal pressure. Ordinary melons that are not specific melons are not suitable for the present invention because wrinkles and the like change on the surface in about 5 days after standing at room temperature and pressure.
WO 92/02622に記載されているように、特定メロンでは組織構造が成熟によって破壊されないことが明らかにされている。すなわち、メロンの老化細胞に特徴的な、細胞の破壊、ガラス状態化、液状化等の何れも観察されていない。 As described in WO 92/02622, it has been clarified that the tissue structure of certain melons is not destroyed by maturation. That is, none of cell destruction, glazing, liquefaction, etc. characteristic of senescent cells of melon has been observed.
また、柑橘類、ブドウ類、苺類等は非クリマクテリック型果実といわれ、リンゴ、ナシ、トマト、メロン、バナナ等はクリマクテリック型果実といわれているが、クリマクテリック型果実は、成熟の開始点でエチレンを放出する。特定メロンは、エチレンクライシス後に少なくとも5日間、好適には少なくとも7日間のエチレンを定常的に放出する期間を有するものが好ましい。 Citrus fruits, grapes, grapes, etc. are said to be non-climacteric fruits, while apples, pears, tomatoes, melons, bananas, etc. are said to be climacteric fruits, but climacteric fruits are mature. Ethylene is released at the starting point. The specific melon is preferably one having a period during which ethylene is steadily released for at least 5 days, preferably at least 7 days after ethylene crisis.
当業者ならば、WO 92/02622及び上記記載を参考にして、本発明における「特定メロン」が何であるかを明確に特定できる。 A person skilled in the art can clearly identify what the “specific melon” in the present invention is referring to WO 92/02622 and the above description.
特定メロンは、好ましくは、そこからの可溶性タンパク質抽出物の酵素活性(例えば、スーパーオキシドジムスターゼ(SOD)活性やカタラーゼ活性)が、通常のメロンの2倍以上であるメロンである。具体的には、果肉の水溶性画分のスーパーオキシドジスムターゼ(SOD)活性が、10units/(mg水溶性画分)以上であり、カタラーゼ活性が1units/(mg水溶性画分)以上であり、グルタチオン活性が500μg/(100mg水溶性画分)以上であるメロンである。更に好ましくは、可溶性タンパク質抽出物のスーパーオキシドジスムターゼ(SOD)活性が、50units/(mgタンパク質)以上であり、カタラーゼ活性が60units/(mgタンパク質)以上であるメロンである。可溶性タンパク質抽出物、その酵素活性については、特許文献10に記載されている。
The specific melon is preferably a melon in which the enzyme activity (for example, superoxide dismutase (SOD) activity or catalase activity) of the soluble protein extract therefrom is twice or more that of a normal melon. Specifically, the superoxide dismutase (SOD) activity of the water-soluble fraction of the pulp is 10 units / (mg water-soluble fraction) or more, and the catalase activity is 1 units / (mg water-soluble fraction) or more, Melon having a glutathione activity of 500 μg / (100 mg water-soluble fraction) or more. More preferably, the soluble protein extract has a superoxide dismutase (SOD) activity of 50 units / (mg protein) or more and a catalase activity of 60 units / (mg protein) or more. The soluble protein extract and its enzyme activity are described in
[特定メロン中の成分]
本発明の経口摂取用紫外線傷害防止組成物に含有される成分は、特定メロンから任意の方法で得ることができる。例えば、特定メロンの果肉を粉砕又は加圧し、その上澄みを回収する方法等がある。効率良く特定メロンから抽出成分を得るためには、水溶性溶媒中で回収する方法が好ましい。その際の水溶液のpHは特に制限はないが、好ましくはpH5〜pH9であり、更に好ましくはpH7〜pH8である。pHが高すぎる又は低すぎると、特定メロン中に含まれている酵素が変性し酵素活性が低下し、本発明の効果を発揮しない場合がある。[Ingredients in specific melon]
The component contained in the composition for preventing UV injury for oral intake of the present invention can be obtained from the specific melon by any method. For example, there is a method of pulverizing or pressurizing the pulp of a specific melon and collecting the supernatant. In order to obtain an extraction component from specific melon efficiently, a method of recovering in an aqueous solvent is preferable. The pH of the aqueous solution at that time is not particularly limited, but is preferably pH 5 to pH 9, and more preferably
また、回収するための水溶性溶媒は特に制限はなく、水溶性であれば任意に選択できる。具体的には、例えば、
脱イオン水等の水類;
ヘキサン、ヘプタン、流動パラフィン等の炭化水素類;
メタノール、エタノール、1−プロパノール、2−プロパノール、1−ブタノール、2−ブタノール等の低級アルコール類;
1.3−ブチレングリコール、プロピレングリコール、グリセリン等の常温で液体の多価アルコール;
ジエチルエーテル、テトラヒドロフラン、ジプロピルエーテル等のエーテル類:
アセトン、メチルエチルケトン等のケトン類;
酢酸エチル、酢酸ブチル等のエステル類;
アセトニトリル等である。The water-soluble solvent for recovery is not particularly limited and can be arbitrarily selected as long as it is water-soluble. Specifically, for example,
Water such as deionized water;
Hydrocarbons such as hexane, heptane, liquid paraffin;
Lower alcohols such as methanol, ethanol, 1-propanol, 2-propanol, 1-butanol, 2-butanol;
1.3 Polyhydric alcohol that is liquid at room temperature, such as 3-butylene glycol, propylene glycol, glycerin;
Ethers such as diethyl ether, tetrahydrofuran and dipropyl ether:
Ketones such as acetone and methyl ethyl ketone;
Esters such as ethyl acetate and butyl acetate;
Acetonitrile and the like.
タンパク質等が含まれるため、好ましくは水類であり、特に好ましくは脱イオン水である。これらの水溶性溶媒は1種でも2種以上を混合して用いてもよい。 Since proteins and the like are included, water is preferable, and deionized water is particularly preferable. These water-soluble solvents may be used alone or in combination of two or more.
現在、特定メロンから上記方法で抽出された成分としては、実施例の表1記載の物質が判明しているが、本発明の効果を奏する物質はこれらには限定されず、他にもあることが予想される。従って、本発明の経口摂取用紫外線傷害防止組成物には、特定メロンから得られる成分を含有することは必須であるが、具体的成分は表1記載の物質には限定されない。 At present, as the components extracted from the specific melon by the above method, the substances listed in Table 1 of the examples have been found, but the substances having the effects of the present invention are not limited to these, and there are others. Is expected. Therefore, although it is essential to contain the component obtained from a specific melon in the composition for preventing UV injury for oral intake of the present invention, the specific components are not limited to the substances listed in Table 1.
水溶性溶媒中で回収した特定メロンから得られた成分は、その後の加工がしやすいように、濃縮、溶媒置換、溶媒留去等をしてもよい。特定メロンから得られた成分は、上記水溶性抽出溶媒に溶解した状態、それを濃縮した状態、溶媒置換した状態、溶媒留去したペースト状態、溶媒留去した粒子状態等で、経口摂取用紫外線傷害防止組成物中に含有される。 The component obtained from the specific melon recovered in the water-soluble solvent may be subjected to concentration, solvent replacement, solvent distillation, etc. so that subsequent processing is easy. Ingredients obtained from specific melons are dissolved in the water-soluble extraction solvent, concentrated, solvent-replaced, evaporated solvent paste, evaporated solvent particles, etc. It is contained in the injury preventing composition.
粒子状態の場合には、そのまま機械的に攪拌し経口摂取用紫外線傷害防止組成物中に含有される。また、粒子状態で経口摂取用紫外線傷害防止組成物中に含有される場合には、その体積平均粒径は特に限定はないが、50μm〜500μmが好ましく、150μm〜200μmが特に好ましい。 In the case of a particle state, it is mechanically stirred as it is and contained in the composition for preventing UV injury for oral intake. Moreover, when it contains in the ultraviolet injury prevention composition for oral intake in a particle | grain state, the volume average particle diameter does not have limitation in particular, However, 50 micrometers-500 micrometers are preferable, and 150 micrometers-200 micrometers are especially preferable.
上記特定メロンから得られた成分は、後述するように腸溶化合物(腸溶剤と腸溶被覆剤とを含む)で保護することが好ましいが、特定メロンから得られた成分が粒子状態のときには、かかる成分だけを腸溶剤で包摂することも好ましい。特定メロンから得られた成分のみの包摂に用いられる腸溶剤としては、後述のものが挙げられるが、好ましくは、パーム油脂等が、胃酸への抵抗性、酵素タンパクを安定化させる点で好ましい。 The component obtained from the specific melon is preferably protected with an enteric compound (including an enteric solvent and an enteric coating agent) as described later, but when the component obtained from the specific melon is in a particle state, It is also preferred to include only such ingredients with enteric solvents. Examples of the intestinal solvent used for the inclusion of only the components obtained from the specific melon include those described below, but palm oils and fats are preferred in terms of resistance to gastric acid and stabilizing enzyme proteins.
上記特定メロンから得られた成分は、経口摂取によって、皮膚への紫外線照射により誘発される傷害を効果的に防止及び/又は抑制する。また、紫外線による紅斑(発赤)発生前の肌の赤味を低くすることができ、すなわち経口摂取による美白効果も有する。 The component obtained from the specific melon effectively prevents and / or suppresses damage induced by ultraviolet irradiation of the skin by ingestion. In addition, the redness of the skin before the occurrence of erythema (redness) due to ultraviolet rays can be lowered, that is, it has a whitening effect by oral intake.
本発明の経口摂取用紫外線傷害防止組成物には、上記の特定メロンから得られた成分以外に、更にポリフェノール成分を含有することが、本発明の効果を相乗的に発揮させるために好ましい。「ポリフェノール成分」は特に限定はないが、下記する「赤ワイン成分」及び/又は「松樹皮から得られた成分」であることが、本発明の上記効果がより顕著にまた相乗的に得られるために特に好ましい。 In addition to the component obtained from the specific melon, the composition for preventing ultraviolet injury for oral intake of the present invention preferably further contains a polyphenol component in order to synergistically exert the effects of the present invention. The “polyphenol component” is not particularly limited, but the following “red wine component” and / or “component obtained from pine bark” can provide the above effect of the present invention more remarkably and synergistically. Is particularly preferred.
<赤ワイン成分>
本発明の経口摂取用紫外線傷害防止組成物は、上記の特定メロンから得られた成分以外に、更に「ブドウの果肉、果皮若しくは種子を発酵して得られる赤ワイン中に含まれるポリフェノール成分」(以下、「赤ワイン成分」と略記する)を含有することが、本発明の前記効果を相乗的に発揮させるために好ましい。<Red wine ingredient>
In addition to the components obtained from the above-mentioned specific melon, the composition for preventing ultraviolet injury for oral intake of the present invention is further “a polyphenol component contained in red wine obtained by fermenting grape flesh, pericarp or seed” (hereinafter referred to as “polyphenol component”). And abbreviated as “red wine component”) in order to synergistically exhibit the effects of the present invention.
本発明の経口摂取用紫外線傷害防止組成物に好適に含有される「赤ワイン成分」とは、ブドウの果肉、果皮若しくは種子を発酵して得られる赤ワイン中に含まれるポリフェノール成分であれば特に限定はされないが、具体的には、例えば、カテキン類、アントシアニン、フラバノール、フラボノール等のフラバン誘導体等のフェノール成分又は「ブドウの果肉、果皮若しくは種子を発酵して得られる赤ワイン中に含まれる全ての成分」が挙げられる。また、これらの成分を1種でも2種以上を含有していてもよい。 The “red wine component” suitably contained in the composition for preventing UV injury for oral consumption of the present invention is not particularly limited as long as it is a polyphenol component contained in red wine obtained by fermenting grape flesh, pericarp or seeds. Specifically, for example, phenolic components such as catechins, flavan derivatives such as anthocyanins, flavanols and flavonols, or “all components contained in red wine obtained by fermenting grape pulp, pericarp or seed” Is mentioned. Moreover, these components may contain 1 type, or 2 or more types.
本発明における「赤ワイン成分」の形状も特に制限はないが、加工性、取り扱いが容易な点で、粉末、微小顆粒のものが好ましい。 The shape of the “red wine component” in the present invention is not particularly limited, but powders and fine granules are preferred from the viewpoint of processability and easy handling.
<松樹皮から得られた成分>
本発明の経口摂取用紫外線傷害防止組成物は、前記の特定メロンから得られた成分以外に、更に「松樹皮から得られた成分」を含有することが、本発明の効果を相乗的に発揮させるために好ましい。<Ingredients obtained from pine bark>
In addition to the component obtained from the specific melon, the composition for preventing UV injury for oral intake according to the present invention further contains “the component obtained from pine bark” to exhibit the effect of the present invention synergistically. This is preferable.
松樹皮からかかる成分を得る方法としては特に限定はないが、例えば、松の木をたたいて含油樹脂成分を回収する方法、松樹皮を剥がして含油樹脂成分を回収する方法、幹に傷をつけて含油樹脂成分を回収する方法等が挙げられる。更にこれらから、水蒸気蒸留、溶媒抽出、熱水抽出等をして得ることもできる。 The method for obtaining such components from pine bark is not particularly limited. For example, a method for collecting oil-containing resin components by hitting a pine tree, a method for removing oil-containing resin components by peeling pine bark, and damaging the trunk. Examples thereof include a method for recovering the oil-containing resin component. Further, from these, steam distillation, solvent extraction, hot water extraction and the like can also be obtained.
特に好ましくは、熱水抽出によって成分を取り出すことである。すなわち、本発明の経口摂取用紫外線傷害防止組成物には、前記の特定メロンから得られた成分以外に、更に「松樹皮を熱水抽出して得られた成分」を含有することが、本発明の効果を相乗的に発揮させるために好ましい。 Particularly preferably, the component is taken out by hot water extraction. That is, the composition for preventing UV injury for oral intake of the present invention contains, in addition to the component obtained from the specific melon, the “component obtained by hot water extraction of pine bark”. This is preferable for synergistically exhibiting the effects of the invention.
かかる成分は、まず、松樹皮を熱水抽出し、要すれば水を留去し、次いで要すれば溶媒で抽出する。また、更に精製工程を加えてもよい。また、最後に乾燥して固体とすることが好ましい。 Such components are first extracted with hot water from pine bark, distilled off if necessary, and then extracted with a solvent if necessary. Further, a purification step may be further added. Moreover, it is preferable that it is finally dried to be a solid.
松樹皮を得るための松の種類、産地、大きさ等には特に限定はなく任意に選択することができる。松の木の好ましい属種としては、フランスカイガンショウ(P.pinaster)であり、より好ましくはフランス南部に生育する、特に好ましくはフランス南部のランド地方に生育するフランスカイガンショウ(P.pinaster)である。松の木の高さとしては、好ましくは8m以上30m以下であり、特に好ましくは10m以上25m以下である。また、松の木の直径としては、好ましくは50cm以上100cm以下である。上記要件を満たす松の場合に、本発明の効果をより発揮する。 There are no particular limitations on the type, location, size, and the like of the pine for obtaining the pine bark, and it can be arbitrarily selected. The preferred genus of the pine tree is the French caliper (P. pinaster), more preferably it grows in the southern part of France, particularly preferably the French caliper (P. pinaster) that grows in the land region in the southern part of France. is there. The height of the pine tree is preferably 8 m or more and 30 m or less, and particularly preferably 10 m or more and 25 m or less. The diameter of the pine tree is preferably 50 cm or more and 100 cm or less. In the case of a pine that satisfies the above requirements, the effect of the present invention is more exhibited.
[ヒドロキシフラバン若しくはその誘導体又はそれらのオリゴマー]
松樹皮から得られる上記成分の具体的化合物は特に限定はないが、ヒドロキシフラバン若しくはその誘導体又はそれらのオリゴマーであることが好ましい。また、上記松樹皮中に含まれる未知の成分も好ましい。[Hydroxyflavan or derivative thereof or oligomer thereof]
Although the specific compound of the said component obtained from a pine bark does not have limitation in particular, It is preferable that it is a hydroxy flavan or its derivative (s), or those oligomers. Moreover, the unknown component contained in the said pine bark is also preferable.
ヒドロキシフラバンとしては特に限定はないが、フラバン−3−オール(3−ヒドロキシフラバン)、フラバン−3,4−ジオール(3,4−ヒドロキシフラバン)、フラバン−3,5,7−トリオール(3,5,7−ヒドロキシフラバン)、フラバン−3,4,5,7−テトラオール(3,4,5,7−ヒドロキシフラバン)、フラバン−3,5,7,3’,4’−ペンタオール(3,5,7,3’,4’−ヒドロキシフラバン)又はそれらの誘導体が挙げられる。また、それらのダイマー、トリマー、テトラマー等のオリゴマー等が挙げられる。 Although it does not specifically limit as hydroxyflavan, Flavan-3-ol (3-hydroxyflavan), flavan-3,4-diol (3,4-hydroxyflavan), flavan-3,5,7-triol (3,3) 5,7-hydroxyflavan), flavan-3,4,5,7-tetraol (3,4,5,7-hydroxyflavan), flavan-3,5,7,3 ′, 4′-pentaol ( 3,5,7,3 ', 4'-hydroxyflavan) or derivatives thereof. Moreover, oligomers, such as those dimers, trimers, and tetramers, etc. are mentioned.
具体的には、例えば、下記式で表わされるものが挙げられる。
本発明における松樹皮から抽出した「ヒドロキシフラバン若しくはその誘導体又はそれらのオリゴマー」の具体的慣用名としては、例えば、カテキン、エピカテキン、ガリック酸、アントシアニジン、アントシアニン又はそれらの誘導体、それらのダイマー、トリマー、テトラマー等のオリゴマー等である。これらの成分を1種でも2種以上を含有していてもよい。 Specific names of “hydroxyflavan or derivatives thereof or oligomers thereof” extracted from pine bark in the present invention include, for example, catechin, epicatechin, gallic acid, anthocyanidins, anthocyanins or derivatives thereof, dimers and trimers thereof. And oligomers such as tetramers. These components may be used alone or in combination of two or more.
本発明における「松樹皮から得られた成分」や「ヒドロキシフラバン若しくはその誘導体又はそれらのオリゴマー」の形状は特に制限はないが、加工性、入手が容易等の点で、粉末のものが好ましい。具体的には、体積平均粒径が50μm〜500μmのものが好ましく、50μm〜200μmのものが特に好ましい。 The shape of the “component obtained from pine bark” or “hydroxyflavan or a derivative thereof or an oligomer thereof” in the present invention is not particularly limited, but is preferably a powder in terms of processability and availability. Specifically, those having a volume average particle diameter of 50 μm to 500 μm are preferable, and those having a volume average particle diameter of 50 μm to 200 μm are particularly preferable.
<ビタミンC>
本発明の経口摂取用紫外線傷害防止組成物は、前記の特定メロンから得られた成分以外に、更にビタミンCを含有することが、本発明の効果を相乗的に発揮させるために好ましい。<Vitamin C>
In addition to the component obtained from the specific melon, the composition for preventing UV injury for oral intake of the present invention preferably further contains vitamin C in order to synergistically exert the effects of the present invention.
本発明の経口摂取用紫外線傷害防止組成物に含有されるビタミンCは、特に制限はなく一般的に入手可能なものを任意に用いることができる。具体的には、例えば、アスコルビン酸;アスコルビン酸ナトリウム、アスコルビン酸カリウム等のアスコルビン酸アルカリ金属塩:アスコルビン酸カルシウム、アスコルビン酸マグネシウム等のアスコルビン酸アルカリ土類金属塩等が挙げられる。中でもアスコルビン酸、アスコルビン酸ナトリウム、アスコルビン酸カルシウムが好ましく、アスコルビン酸が更に好ましい。 The vitamin C contained in the composition for preventing UV injury for oral intake of the present invention is not particularly limited, and generally available vitamin C can be used. Specifically, for example, ascorbic acid; ascorbic acid alkali metal salts such as sodium ascorbate and potassium ascorbate: alkaline earth metal salts of ascorbic acid such as calcium ascorbate and magnesium ascorbate. Among them, ascorbic acid, sodium ascorbate, and calcium ascorbate are preferable, and ascorbic acid is more preferable.
本発明におけるビタミンCの、形状も特に制限はないが、加工性、取り扱いが容易な点で、粉末のものが好ましい。 The shape of vitamin C in the present invention is not particularly limited, but a powder is preferable in terms of processability and easy handling.
<成分の組み合わせ>
本発明の経口摂取用紫外線傷害防止組成物は、上記の「特定メロンから得られた成分」以外に、上記の「赤ワイン成分」、「ヒドロキシフラバン若しくはその誘導体又はそれらのオリゴマー等の『松樹皮から得られた成分』」及び/又は「ビタミンC」を必須成分として含有する。「特定メロンから得られた成分」との組み合わせに特に制限はなく、任意の組み合わせを用いることができるが、好ましくは、
「特定メロンから得られた成分」及び「赤ワイン成分」、
「特定メロンから得られた成分」及び「松樹皮から得られた成分」、
「特定メロンから得られた成分」及び「赤ワイン成分」及び「松樹皮から得られた成分」の組み合わせである。
更に好ましくは、「特定メロンから得られた成分」、「赤ワイン成分」、「松樹皮から得られた成分」及び「ビタミンC」の組み合わせである。<Combination of ingredients>
In addition to the above-mentioned “component obtained from the specific melon”, the composition for preventing UV injury for ingestion of the present invention includes “red wine component”, “hydroxyflavan or a derivative thereof or oligomer thereof” such as “from pine bark. The obtained component ”” and / or “vitamin C” is contained as an essential component. There is no particular limitation on the combination with the “component obtained from the specific melon”, and any combination can be used.
"Ingredients obtained from specific melons" and "Red wine ingredients",
"Ingredients obtained from specific melon" and "Ingredients obtained from pine bark",
It is a combination of “component obtained from specific melon” and “red wine component” and “component obtained from pine bark”.
More preferably, it is a combination of “component obtained from specific melon”, “red wine component”, “component obtained from pine bark” and “vitamin C”.
経口摂取用紫外線傷害防止組成物中の各成分の好ましい含有量は、固形分換算で、
上記特定メロンから得られた成分 1質量部〜 100質量部
上記赤ワイン成分 0質量部〜 300質量部
上記松樹皮から得られた成分 0質量部〜 180質量部
上記ビタミンC 0質量部〜 200質量部
であり、より好ましい含有量は、固形分換算で、
上記特定メロンから得られた成分 1質量部〜 50質量部
上記赤ワイン成分 5質量部〜 300質量部
上記松樹皮から得られた成分 5質量部〜 180質量部
上記ビタミンC 0質量部〜 200質量部
であり、特に好ましい含有量は、固形分換算で、
上記特定メロンから得られた成分 2質量部〜 20質量部
上記赤ワイン成分 10質量部〜 200質量部
上記松樹皮から得られた成分 10質量部〜 120質量部
上記ビタミンC 1質量部〜 200質量部
である。The preferred content of each component in the composition for preventing UV injury for oral intake is, in terms of solid content,
Components obtained from the
Ingredients obtained from the
Ingredients obtained from the
上記特定メロンから得られた成分が少な過ぎる場合には、本発明の前記効果が得られない場合があり、また、上記赤ワイン成分が少な過ぎる場合には、本発明の前記効果が得られない場合があり、また、上記松樹皮から得られた成分が少な過ぎる場合には、本発明の前記効果が得られない場合があり、一方、上記特定メロンから得られた成分が多すぎる場合には、体内で活性を発現せずに排泄されてしまう場合がある。 When the component obtained from the specific melon is too small, the effect of the present invention may not be obtained. When the red wine component is too small, the effect of the present invention may not be obtained. In addition, when there are too few components obtained from the pine bark, the effect of the present invention may not be obtained, while when there are too many components obtained from the specific melon, It may be excreted without expressing activity in the body.
<腸溶化合物>
本発明においては、腸溶化合物を併用することが、より本発明の効果を得るために好ましい。本発明における腸溶化合物とは、腸内での酵素活性をより高めるために、胃ではなく小腸に入ってから溶解するような、腸溶性を有する物質である。本発明における腸溶化合物は、pH7.5以上で分解又は溶解するものであることが好ましい。また、本発明における「腸溶化合物」とは、以下の腸溶剤及び腸溶被覆剤の両方を指すものとする。<Enteric compound>
In the present invention, it is preferable to use an enteric compound in order to obtain the effect of the present invention. The enteric compound in the present invention is an enteric substance that dissolves after entering the small intestine instead of the stomach in order to further increase the enzyme activity in the intestine. The enteric compound in the present invention is preferably one that decomposes or dissolves at pH 7.5 or higher. Further, the “enteric compound” in the present invention refers to both the following enteric solvents and enteric coating agents.
(腸溶剤)
本発明においては、「特定メロンから得られた成分」を胃液から保護するために包摂する化合物を腸溶剤という。本発明の経口摂取用紫外線傷害防止組成物は、そのまま経口摂取してもよいが、腸内での酵素活性をより高めるために、また、胃ではなく小腸に入ってから溶解するように、腸溶剤によって保護するために包摂することが好ましい。上記特定メロンから得られた成分の内、酵素成分はタンパク質であるため、胃酸で分解し易く、酵素活性が発現する前に分解し易いため、腸溶剤との併用によって、確実に経口摂取用紫外線傷害防止組成物を腸まで到達させることができるという効果がある。(Enteric solvent)
In the present invention, a compound that is included to protect the “component obtained from a specific melon” from gastric juice is referred to as an intestinal solvent. The ultraviolet ray injury preventing composition for oral intake of the present invention may be taken orally as it is, but in order to further enhance the enzyme activity in the intestine and to dissolve after entering the small intestine instead of the stomach, Inclusion is preferred to protect with a solvent. Among the components obtained from the above specific melon, the enzyme component is a protein, so it is easily decomposed by gastric acid and easily decomposed before the enzyme activity is expressed. There is an effect that the composition for preventing injury can reach the intestines.
腸溶剤の含有量としては、腸溶剤の種類により適宜調整が可能であるが、「特定メロンから得られた成分」100質量部に対して、100質量部〜5000質量部が好ましく、100質量部〜1000質量部がより好ましく、200質量部〜500質量部が特に好ましい。腸溶剤が多すぎる場合は、質量部当たりの酵素活性である比活性が低下し、摂取量が過大となる場合があり、少なすぎる場合は、摂取者の条件によっては殆どの経口摂取用紫外線傷害防止組成物のタンパク質成分が胃内で分解されることが考えられるため、酵素の活性が失活してしまい、本発明の効果が減じてしまう場合がある。 The content of the enteric solvent can be appropriately adjusted depending on the type of enteric solvent, but is preferably 100 parts by mass to 5000 parts by mass with respect to 100 parts by mass of the “component obtained from the specific melon”, and 100 parts by mass. -1000 mass parts is more preferable, and 200 mass parts-500 mass parts is especially preferable. If too much enteric solvent is present, the specific activity, which is the enzyme activity per part by mass, may be reduced, resulting in an excessive intake. Since the protein component of the prevention composition is considered to be degraded in the stomach, the activity of the enzyme is deactivated, and the effect of the present invention may be reduced.
「腸溶剤」としては、ペクチン、アルギン酸、セルロース類(例えば、カルボキシメチルセルロース、セルロースアセテートフタレート等)、(メタ)アクリル酸コポリマー、パーム油脂、ヤシ油脂、ゼイン等の食用油に用いられる油脂が挙げられる。好ましくは、上記効果を奏する点でパーム油脂である。腸溶剤で保護する方法としては、常套な手段を用いればよく、具体的には、経口摂取用紫外線傷害防止組成物と混合する方法等が挙げられる。 Examples of the “enteric solvent” include fats and oils used in edible oils such as pectin, alginic acid, celluloses (for example, carboxymethylcellulose, cellulose acetate phthalate, etc.), (meth) acrylic acid copolymers, palm fats and oils, palm fats and oils, zein and the like. . Preferably, it is palm fats and oils at the point which shows the said effect. As a method of protecting with an intestinal solvent, a conventional means may be used, and specifically, a method of mixing with an ultraviolet-injury-preventing composition for ingestion and the like can be mentioned.
(腸溶被覆剤)
本発明においては、「経口摂取用紫外線傷害防止組成物」を胃液から保護するために被覆する化合物を腸溶被覆剤という。特定メロンから得られた成分が既に腸溶剤で包摂されていてもいなくても、更に、それが含有される経口摂取用紫外線傷害防止組成物を、要すれば、ハードカプセル、ソフトカプセル等に封入し、それら内容物の表面を噴霧、浸漬、蒸着等の常套のコーティング手段で、腸溶被覆剤によって被覆することが好ましい。均一に被覆できる点、低温で保持できる点で、内容物の表面を噴霧する方法が好ましい。腸溶被覆剤との併用によって、摂取者の条件に影響を受けることなく確実に経口摂取用紫外線傷害防止組成物を腸まで到達させる効果が特にある。従って、腸溶被覆剤を用いない場合は、摂取者の条件によっては殆どの経口摂取用紫外線傷害防止組成物のタンパク質成分が胃内で分解されることが考えられるため、酵素の活性が失活してしまい、本発明の効果が減じてしまう場合がある。(Enteric coating)
In the present invention, the compound that coats the “UV damage preventing composition for ingestion” to protect it from gastric juice is referred to as an enteric coating agent. Whether or not the component obtained from the specific melon is already encapsulated in the intestinal solvent, and further contains an ultraviolet ray injury preventing composition for ingestion containing it, if necessary, encapsulated in a hard capsule, soft capsule, etc. The surface of these contents is preferably coated with an enteric coating agent by a conventional coating means such as spraying, dipping or vapor deposition. A method of spraying the surface of the contents is preferable in that it can be uniformly coated and can be kept at a low temperature. The combined use with an enteric coating has an effect of reliably reaching the intestinal ultraviolet injury preventing composition for oral intake without being affected by the conditions of the ingestor. Therefore, when no enteric coating is used, the protein activity of most UV-injured compositions for oral consumption can be degraded in the stomach depending on the condition of the intake, so that the enzyme activity is deactivated. As a result, the effect of the present invention may be reduced.
腸溶被覆剤としては、エチルセルロース、ヒドロキシプロピルメチルセルロースフタレート、ヒドロキシプロピルメチルセルロースアセテートサクシネート、カルボキシメチルセルロース、セルロースアセテートフタレート等のセルロース類、シェラック、ゼイン、ラクトフェリン、ポリグリコ乳酸(polyglycolactic acid)、ポリ乳酸、乳酸・グリコール酸共重合体(polylactide-co-glycolide)、メタクリル酸コポリマー、アミノアルキルメタクリレートポリマー等が挙げられ、食品用の腸溶被覆剤としては、シェラック又はゼインが好ましく、特に好ましくは、天然タンパク質である点でゼインである。 Enteric coatings include celluloses such as ethyl cellulose, hydroxypropylmethylcellulose phthalate, hydroxypropylmethylcellulose acetate succinate, carboxymethylcellulose, cellulose acetate phthalate, shellac, zein, lactoferrin, polyglycolactic acid, polylactic acid, lactic acid Examples include glycolic acid copolymers (polylactide-co-glycolide), methacrylic acid copolymers, aminoalkyl methacrylate polymers, etc. As food enteric coatings, shellac or zein is preferable, and natural proteins are particularly preferable. Zein in terms.
また、腸溶被覆剤により被覆したときの腸溶被覆剤の層の厚さは、0.1μm〜50μmであり、好ましくは、1μm〜20μmであり、更に好ましくは1μm〜10μmである。層の厚さが厚すぎる場合は、腸内での溶解が遅延する場合があり、薄すぎる場合は、胃で溶解してしまう、腸内の酵素活性が不十分である等の場合がある。 Moreover, the thickness of the layer of the enteric coating agent when coated with the enteric coating agent is 0.1 μm to 50 μm, preferably 1 μm to 20 μm, and more preferably 1 μm to 10 μm. If the thickness of the layer is too thick, dissolution in the intestine may be delayed, and if it is too thin, it may dissolve in the stomach, or the enzyme activity in the intestine may be insufficient.
<その他の成分>
本発明の経口摂取用紫外線傷害防止組成物には、上記の成分以外に、他の薬物、更に経口投与用製剤に通常使用される成分を適宜その目的に応じて配合してもよい。例えば、賦形剤、希釈剤、結合剤、崩壊剤、甘味剤、張化剤、防腐剤、湿潤剤、乳化剤、分散剤、安定化剤、溶解補助剤、緩衝剤、滑沢剤、懸濁化剤、着色剤、着香剤等が挙げられる。<Other ingredients>
In addition to the above-mentioned components, the ultraviolet ray injury preventing composition for oral ingestion of the present invention may be blended with other drugs and further components normally used in oral administration preparations depending on the purpose. For example, excipients, diluents, binders, disintegrants, sweeteners, tonics, preservatives, wetting agents, emulsifiers, dispersants, stabilizers, solubilizers, buffers, lubricants, suspensions Examples thereof include an agent, a coloring agent, and a flavoring agent.
ここで、賦形剤としては、例えばラクトース、グルコース、乳糖、精製白糖、ブドウ糖等の糖類;プルラン、デキストリン等の多糖類:D−マンニトール、ソルビトール、キシリトール、エリスリトール等の糖アルコール;トウモロコシデンプン等のデンプン類等が挙げられる。結合剤としては、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロース、メチルセルロース、ポリビニルピロリドン、デキストリン、アルファー化デンプン等が挙げられる。崩壊剤としては、結晶セルロース、カルボキシメチルセルロース、カルボキシメチルセルロースナトリウム、アルファー化デンプン、コムギデンプン及びトウモロコシデンプン等のデンプン類、ケイ酸マグネシウム、軟質無水ケイ酸、合成ケイ酸アルミニウム、ステアリン酸カルシウム、炭酸マグネシウム、アクチゾル、プリモジェル、エクスプロタグ、メタケイ酸アルミン酸マグネシウム等が挙げられる。滑沢剤としては、ステアリン酸マグネシウム、タルク等が挙げられ、懸濁化剤としては、トラガント、アラビアゴム、キサンタンガム、アルギン酸ナトリウム等が挙げられる。甘味剤としては、サッカリンナトリウムやアスパルテーム等が挙げられる。着香剤としては、オレンジやレモン等の柑橘系香料やメントールやハッカ油等が挙げられる。着色剤としては、天然色素や合成色素等が挙げられる。これらは、天然物から選択されることが特に好ましい。 Here, examples of the excipient include sugars such as lactose, glucose, lactose, purified white sugar, and glucose; polysaccharides such as pullulan and dextrin: sugar alcohols such as D-mannitol, sorbitol, xylitol, and erythritol; Examples include starches. Examples of the binder include hydroxypropylcellulose, hydroxypropylmethylcellulose, methylcellulose, polyvinylpyrrolidone, dextrin, pregelatinized starch and the like. Disintegrants include crystalline cellulose, carboxymethylcellulose, sodium carboxymethylcellulose, pregelatinized starch, wheat starch, corn starch and other starches, magnesium silicate, soft anhydrous silicic acid, synthetic aluminum silicate, calcium stearate, magnesium carbonate, actisol , Primogel, ExproTag, magnesium aluminate metasilicate, and the like. Lubricants include magnesium stearate, talc and the like, and suspending agents include tragacanth, gum arabic, xanthan gum, sodium alginate and the like. Examples of the sweetener include saccharin sodium and aspartame. Examples of flavoring agents include citrus flavors such as orange and lemon, menthol and peppermint oil. Examples of the colorant include natural pigments and synthetic pigments. These are particularly preferably selected from natural products.
<剤型>
経口投与のための製剤(経口剤)としては、錠剤、丸剤、顆粒剤、カプセル剤、散剤、液剤、懸濁剤、シロップ剤等が挙げられ、何れも好適に用いられるが、安定、簡便な点で、カプセル剤等が好ましい。<Dosage form>
Examples of preparations for oral administration (oral preparations) include tablets, pills, granules, capsules, powders, solutions, suspensions, syrups, etc., all of which are preferably used, but stable and simple. In particular, capsules and the like are preferable.
製剤化に際しては、製薬上許容される担体を混合することが可能である。例えば、液状担体としては、水、アルコール、食用油等を用いることができる。固体担体としては、リジン等のアミノ酸類、シクロデキストリン等の多糖類、ステアリン酸マグネシウム等の有機酸塩類、ヒドロキシルプロピルセルロース等のセルロース誘導体等を用いることができる。更に、各種医薬用添加剤を配合することもできる。 In formulating, a pharmaceutically acceptable carrier can be mixed. For example, water, alcohol, edible oil, or the like can be used as the liquid carrier. As the solid carrier, amino acids such as lysine, polysaccharides such as cyclodextrin, organic acid salts such as magnesium stearate, cellulose derivatives such as hydroxylpropylcellulose, and the like can be used. Furthermore, various pharmaceutical additives can be blended.
<経口摂取用紫外線傷害防止組成物の加工方法>
本発明の経口摂取用紫外線傷害防止組成物は、上記成分から適宜選択された成分を、任意の方法で加工し製造される。例えば、水溶性媒体中で練り合わせ、次いで湿式造粒する方法、顆粒成分を任意の賦形剤等とともに機械的に攪拌し、乾式造粒する方法、粒体成分を機械的に攪拌し、カプセルに充填する方法等がある。経口摂取用紫外線傷害防止組成物のタンパク質成分が安定に確保できるという点で、粒体成分を機械的に攪拌し、カプセルに充填する方法が好ましい。<Processing Method for UV Injury Prevention Composition for Oral Ingestion>
The composition for preventing UV injury for oral intake of the present invention is produced by processing a component appropriately selected from the above components by any method. For example, a method of kneading in an aqueous medium and then wet granulation, a method in which the granule components are mechanically stirred together with an optional excipient, etc., a dry granulation method, a particle component is mechanically stirred, and a capsule There is a method of filling. A method in which the granular component is mechanically stirred and filled into a capsule is preferable in that the protein component of the composition for preventing UV injury for oral intake can be stably secured.
得られた顆粒をそのまま摂取することも可能だが、摂取のしやすさからカプセル剤等に封入してもよい。カプセル剤等に封入しない場合は、ヨーグルト、食物繊維及びマヨネーズやバター等の油脂に混ぜて摂取することが、胃液による分解を防げる点で好ましい。また、カプセル剤としては、特に制限はなく、経口摂取用として用いられるものであれば任意に選択することができる。具体的には、例えば、硬カプセル剤、軟カプセル剤、マイクロカプセル剤等であり、好ましくはゼラチン製の軟カプセル剤であり、更に好ましくは、ブタゼラチン製のカプセルである。更に、服用感や薬物の安定性等を考慮して糖類や高分子等でカプセル表面を被覆してもよい。また更に、前記したように腸溶被覆剤で被覆すると、本発明の前記効果が相乗的に増大する。 The obtained granules can be ingested as they are, but may be encapsulated in a capsule or the like for ease of ingestion. When not encapsulated in a capsule or the like, it is preferable to take it mixed with yoghurt, dietary fiber and oils and fats such as mayonnaise and butter from the viewpoint of preventing decomposition by gastric juice. Moreover, there is no restriction | limiting in particular as a capsule, If it is used for oral intake, it can select arbitrarily. Specifically, for example, hard capsules, soft capsules, microcapsules, etc., preferably soft capsules made of gelatin, more preferably capsules made of porcine gelatin. Furthermore, the capsule surface may be coated with saccharides, polymers, etc. in consideration of the feeling of medication and drug stability. Furthermore, as described above, coating with an enteric coating agent synergistically increases the effects of the present invention.
<摂取量、用途>
経口摂取用紫外線傷害防止組成物の経口摂取量は特に限定はないが、20mg/日〜1g/日が好ましく、50mg/日〜800mg/日がより好ましく、200mg/日〜500mg/日が特に好ましい。1日の経口摂取量を1度に摂取する必要はなく、数回に分けて摂取してもよい。1度に服用し易い点から、10mg/回〜0.5g/回が好ましく、25mg/回〜400mg/回がより好ましく、100mg/回〜250mg/回が特に好ましい。カプセル等の経口剤1個あたりに含有される本発明の経口摂取用紫外線傷害防止組成物は、10mg/経口剤〜0.5g/経口剤が好ましく、25mg/経口剤〜400mg/経口剤がより好ましく、100mg/経口剤〜250mg/経口剤が特に好ましい。<Intake and use>
The amount of oral intake of the composition for preventing UV injury for oral intake is not particularly limited, but is preferably 20 mg / day to 1 g / day, more preferably 50 mg / day to 800 mg / day, and particularly preferably 200 mg / day to 500 mg / day. . It is not necessary to take the daily oral intake at a time, and it may be taken in several divided doses. From the point of being easy to take at a time, 10 mg / dose to 0.5 g / dose is preferred, 25 mg / dose to 400 mg / dose is more preferred, and 100 mg / dose to 250 mg / dose is particularly preferred. The ultraviolet ray injury preventing composition for oral intake of the present invention contained per oral preparation such as a capsule is preferably 10 mg / oral preparation to 0.5 g / oral preparation, more preferably 25 mg / oral preparation to 400 mg / oral preparation. 100 mg / oral to 250 mg / oral is particularly preferable.
また、経口摂取用紫外線傷害防止組成物中の各成分の経口摂取量も特に限定はないが、固形分換算で、
上記特定メロンから得られた成分 0.1mg〜100mg/日が好ましく、
1mg〜 20mg/日がより好ましく、
上記赤ワイン成分 0mg〜350mg/日が好ましく、
10mg〜200mg/日がより好ましく、
上記松樹皮から得られた成分 0mg〜200mg/日が好ましく、
10mg〜120mg/日がより好ましく、
上記ビタミンC 0mg〜350mg/日が好ましく、
1mg〜200mg/日がより好ましい。In addition, the oral intake of each component in the composition for preventing UV injury for oral intake is not particularly limited, but in terms of solid content,
The component obtained from the specific melon is preferably 0.1 mg to 100 mg / day,
1 mg to 20 mg / day is more preferable,
The red wine component is preferably 0 mg to 350 mg / day,
10 mg to 200 mg / day is more preferable,
The component obtained from the pine bark is preferably 0 mg to 200 mg / day,
10 mg to 120 mg / day is more preferable,
The above vitamin C is preferably 0 mg to 350 mg / day,
1 mg to 200 mg / day is more preferable.
カプセル等の経口剤1個あたりに含有される上記各成分の量は、上記1日の摂取量の(より)好ましい範囲の、各半分(1/2)の量が好ましい。 The amount of each component contained per oral preparation such as a capsule is preferably a half (1/2) of each (more) preferable range of the daily intake.
また、摂取期間は、14日以上が好ましく、30日以上がより好ましく、90日以上が特に好ましい。また、継続摂取が好ましい。摂取量が少な過ぎると前記効果が発揮されない場合があり、また、多すぎると、それ以上の効果が期待できないため無駄になる場合がある。 The intake period is preferably 14 days or longer, more preferably 30 days or longer, and particularly preferably 90 days or longer. Moreover, continuous intake is preferable. If the amount is too small, the above effect may not be exhibited. If the amount is too large, a further effect cannot be expected, which may be useless.
本発明の経口摂取用紫外線傷害防止組成物や経口剤は、紫外線障害の治療、予防等に薬剤として使用されるだけではなく、美白化粧料、スキンケア化粧料等のスキンケア品、経口摂取用スキンケア品、飲食品、飲食品の原料等にも好適に配合されて使用される。 The composition for preventing UV injury for oral intake and the oral preparation of the present invention are not only used as a drug for treatment and prevention of UV damage, but also skin care products such as whitening cosmetics and skin care cosmetics, and skin care products for oral intake. , Foods and drinks, food ingredients and other ingredients are also suitably blended and used.
<作用>
本発明における経口摂取用紫外線傷害防止組成物を摂取することにより、紫外線傷害を抑制・防止できる作用・原理は明らかではなく、また、本発明は、かかる作用・原理の範囲に限定されるわけではないが、以下のことが考えられる。すなわち、本発明の経口摂取用紫外線傷害防止組成物のうち、キューカミス・メロの変種の果実から得られた成分は、SOD(スーパーオキサイドデスミューターゼ)、カタラーゼ等を主成分としており、摂取後、腸内で脂肪等の食物や食品由来の化学合成物等により発生する活性酸素を、過酸化水素を経て水に変換する。また一般に酸素ストレスにさらされた生体は抗活性酸素能力が高まることが知られており、腸内で発生する活性酸素→過酸化水素→水への一反応物或いは複数の反応物が生体の高酸素ストレス機能の強化を誘導したと考えられる。キューカミス・メロの変種の果実から得られた成分は、直接活性酸素を無害化するとともに、この反応過程が何らかの作用機構で紫外線傷害防止効果を発揮するようになったと推察している。<Action>
The action / principle of suppressing or preventing UV damage by ingesting the UV damage preventing composition for oral consumption according to the present invention is not clear, and the present invention is not limited to the scope of such action / principle. The following are possible. That is, in the composition for preventing UV injury for oral ingestion of the present invention, the components obtained from the fruit of the variety of Cucumis melo are mainly composed of SOD (superoxide desmutase), catalase, etc. Active oxygen generated by foods such as fat and food-derived chemical compounds in the intestine is converted to water through hydrogen peroxide. In addition, it is generally known that a living body exposed to oxygen stress has an increased ability to react with active oxygen, and one or more reactants of active oxygen → hydrogen peroxide → water generated in the intestine are high in the living body. It is thought that the enhancement of the oxygen stress function was induced. It is presumed that the components obtained from the fruit of the variety of Cucumis melo detoxify the active oxygen directly, and that this reaction process has exerted a UV damage prevention effect by some mechanism of action.
更に、ビタミンC、及び/又は、ブドウの果皮若しくは種子由来のポリフェノール成分等を含有する赤ワイン成分、及び/又は、ヒドロキシフラバン若しくはその誘導体又はそれらのオリゴマー等の松樹皮から得られた成分と組み合わされることで、本発明の前記効果がより顕著に現れるようになったのは、活性酸素により誘導された核酸、蛋白質、脂質の過酸化反応が連鎖的に起こることを同時に抑制することで、ヒドロキシラジカルによる一連の反応の抑制が相乗的に高まったためであると考えられる。 Further, vitamin C and / or a red wine component containing a polyphenol component derived from grape skin or seed and / or a component obtained from pine bark such as hydroxyflavan or a derivative thereof or an oligomer thereof. As a result, the effect of the present invention appears more prominently by simultaneously suppressing the occurrence of chain oxidation of peroxidation reactions of nucleic acids, proteins and lipids induced by active oxygen. This is thought to be due to the synergistic increase in suppression of the series of reactions caused by.
以下に、実施例及び比較例を挙げて本発明を更に具体的に説明するが、本発明は、その要旨を超えない限りこれらの実施例に限定されるものではない。 EXAMPLES Hereinafter, the present invention will be described more specifically with reference to examples and comparative examples. However, the present invention is not limited to these examples unless it exceeds the gist.
<経口摂取用紫外線傷害防止組成物の調製>
(キューカミス・メロの変種の果実(特定メロン)から得られた成分の調製)
前記のキューカミス・メロの変種の果肉100質量部を、脱イオン水100質量部と共に0.5時間粉砕した。このときブレンダーを用いて、氷零温度、pH6.5〜7.5、常圧の条件下で粉砕した。粉砕の後、上澄み液(水溶性画分)だけを回収し、凍結乾燥機を用いて濃縮、乾燥をし、粉末状の体積平均粒径200μmの組成物20質量部を得た。得られた組成物に、腸溶剤としてパーム油脂80質量部を混合し、パーム油脂で包摂した。<Preparation of composition for preventing UV injury for oral consumption>
(Preparation of ingredients obtained from the fruit (special melon) of Kukamisu Melo varieties)
100 parts by weight of the above-mentioned Kukamis-Mello variant pulp was ground with 100 parts by weight of deionized water for 0.5 hour. At this time, it grind | pulverized on the conditions of zero ice temperature, pH 6.5-7.5, and normal pressure using the blender. After pulverization, only the supernatant (water-soluble fraction) was collected and concentrated and dried using a freeze dryer to obtain 20 parts by mass of a powdery volume
ここで得られた組成物の主成分を表1に示すが、本発明はこれに限定されるものではなく、本発明の特定メロンから得られた組成物の含有成分、真の有効成分の詳細については不明である。 The main components of the composition obtained here are shown in Table 1, but the present invention is not limited to this. Details of the components contained in the composition obtained from the specific melon of the present invention and the true active ingredients Is unknown.
(経口摂取用紫外線傷害防止組成物の加工)
上記「特定メロンから得られた成分の調製」で調製されたものと同じものである、キューカミス・メロの変種の果実(特定メロン)から得られた成分(Extramel(登録商標)、Sedaherb Japan社より入手)70質量部及びビタミンC(DSM Nutritional Products (UK) Limited Dalry社製)100質量部、赤ワイン成分(商品名:プロビノール(Provinols(登録商標))、Sedaherb Japan社より入手)100質量部、ヒドロキシフラバン若しくはその誘導体又はそれらのオリゴマー等の松樹皮から得られた成分(商品名:ポリパイン(POLY-PINE(登録商標))、Sedaherb Japan社より入手)60質量部、セルロース110質量部を、ロッキングミキサーV型混合機を用いて均一分散の状態になるまで混合した。(Processing of UV injury prevention composition for ingestion)
Ingredients obtained from the fruit (special melon) of Kukamisu melo varieties (extramel (registered trademark), from Sedaherb Japan), which is the same as that prepared in the above-mentioned “Preparation of Ingredients from Specific Melon” Obtained) 70 parts by weight and 100 parts by weight of vitamin C (DSM Nutritional Products (UK) Limited Dalry), red wine ingredients (trade name: Provinols (registered trademark), 100 parts by Sedaherb Japan), hydroxy Ingredients obtained from pine bark such as flavan or derivatives thereof or oligomers thereof (trade name: POLY-PINE (registered trademark), obtained from Sedaherb Japan) 60 parts by weight, cellulose 110 parts by weight, rocking mixer It mixed until it became the state of uniform dispersion using the V type mixer.
その後、220mgの上記の混合物を、ブタゼラチン製のカプセルに封入し、腸溶被覆剤として、ゼイン(小川香料株式会社製)を噴霧し、腸溶被覆剤の5〜10μmの層を形成させ、乾燥させて経口摂取用紫外線傷害防止組成物とした。 Thereafter, 220 mg of the above mixture is encapsulated in a capsule made of porcine gelatin, and zein (manufactured by Ogawa Fragrance Co., Ltd.) is sprayed as an enteric coating agent to form a 5 to 10 μm layer of the enteric coating agent. The composition was dried to obtain a composition for preventing UV injury for oral consumption.
実施例1
健康な35歳から45歳の女性7人(被験者No.1〜No.7)に、上記で得られた経口摂取用紫外線傷害防止組成物2カプセル(セルロース、カプセル及び腸溶被覆剤を除いた有効成分330mg相当)を、1日1回28日間摂取させた後、紫外線照射装置USHIO Optical Modulexを用いて、紫外線を背中に照射した。このときの紫外線照射は、図1の摂取[1]の部分、摂取[2]の部分の中に、それぞれ直径約1cmの円形範囲を6つ設け、計12箇所の部位に、表2に示す相対紫外線照射量で紫外線照射を行った。照射紫外線照射波長は、比較的長波長のUVAと比較的短波長のUVBの両方の波長域を含むものである。詳細は下記に示す。ここで、表2に示す数値(相対紫外線照射量)の単位は、5.83[μW/(cm2/hr)]である。Example 1
To 7 healthy women aged 35 to 45 (subjects No. 1 to No. 7), 2 capsules for preventing UV injury for oral intake obtained above (cellulose, capsule and enteric coating were excluded) (Equivalent to 330 mg of active ingredient) was ingested once a day for 28 days, and then the back was irradiated with ultraviolet rays using an ultraviolet irradiation apparatus USHIO Optical Module. The ultraviolet irradiation at this time is provided with six circular ranges each having a diameter of about 1 cm in the intake [1] portion and the intake [2] portion of FIG. Ultraviolet irradiation was performed with a relative ultraviolet irradiation amount. The irradiation ultraviolet irradiation wavelength includes both a wavelength range of UVA having a relatively long wavelength and UVB having a relatively short wavelength. Details are shown below. Here, the unit of the numerical values (relative ultraviolet irradiation amount) shown in Table 2 is 5.83 [μW / (cm 2 / hr)].
照射1日後に紅斑(発赤)の程度、照射7日後にメラニン沈着の程度を、それぞれ、目視観察及びメグサメーターを用いて測定した。なお、照射前28日間に加えて照射7日後まで、上記で得られた経口摂取用紫外線傷害防止組成物有効成分330mg、すなわち2カプセルを、1日1回、紫外線照射前と同じ量で摂取し続けた。 The degree of erythema (redness) after 1 day of irradiation and the degree of melanin deposition after 7 days of irradiation were measured using visual observation and a megsometer, respectively. In addition to the 28 days prior to irradiation, until 7 days after irradiation, 330 mg of the active ingredient for ultraviolet injury prevention composition for oral consumption obtained above, that is, 2 capsules, was taken once a day in the same amount as before ultraviolet irradiation. Continued.
比較例1
経口摂取用紫外線傷害防止組成物を摂取しない以外は、実施例1と同様にして紫外線を照射し評価を行った。このときの紫外線照射は、図1の非摂取[1]の部分、非摂取[2]の部分に、同様に表2に示す照射量で行った。Comparative Example 1
Evaluation was performed by irradiating with ultraviolet rays in the same manner as in Example 1 except that the composition for preventing oral injury of ultraviolet rays was not taken. The ultraviolet irradiation at this time was similarly performed at the doses shown in Table 2 in the non-intake [1] and non-intake [2] portions of FIG.
実施例2
カプセルを腸溶被覆剤で被覆しない以外は、実施例1と同様に経口摂取用紫外線傷害防止組成物を調製し、実施例1と同様に、ただし、目視判定のみの簡便な評価を行った。Example 2
Except that the capsule was not coated with an enteric coating agent, a composition for preventing UV injury for oral consumption was prepared in the same manner as in Example 1, and the same evaluation as in Example 1 was carried out, but only a simple visual evaluation was performed.
実施例3
実施例1と同様にして、キューカミス・メロの変種の果実(特定メロン)から得られた成分を調製し、それのみを実施例1と同様に腸溶被覆剤としてゼイン(小川香料株式会社製)を用いて被覆し、経口摂取用紫外線傷害防止組成物を調製し、実施例1と同様に、ただし、目視判定のみの簡便な評価を行った。Example 3
In the same manner as in Example 1, a component obtained from a variety of Cucamis melo varieties (specific melon) was prepared, and only that was used as an enteric coating in the same manner as in Example 1 to produce zein (manufactured by Ogawa Fragrance Co., Ltd.). Was used to prepare a composition for preventing UV injury for oral ingestion, and the same evaluation as in Example 1 was carried out, but a simple evaluation only for visual judgment was performed.
比較例2
経口摂取用紫外線傷害防止組成物を摂取する代わりに、ビタミンCのみ330mgを摂取する以外は実施例1と同様にして紫外線を照射し評価を行った。Comparative Example 2
Evaluation was performed by irradiating ultraviolet rays in the same manner as in Example 1 except that 330 mg of vitamin C alone was taken instead of taking the ultraviolet ray injury preventing composition for oral intake.
比較例3
経口摂取用紫外線傷害防止組成物を摂取する代わりに、商品名:プロビノール(Provinols(登録商標))(Sedaherb Japanより入手)のみ330mgを摂取する以外は、実施例1と同様にして紫外線を照射し評価を行った。Comparative Example 3
Instead of ingesting the UV injury prevention composition for oral consumption, the product name: Provinols (registered trademark) (obtained from Sedaherb Japan) was irradiated in the same manner as in Example 1 except that 330 mg was ingested. Evaluation was performed.
比較例4
経口摂取用紫外線傷害防止組成物を摂取する代わりに、商品名:ポリパイン(POLY-PINE(登録商標))(Sedaherb Japanより入手)のみ330mgを摂取する以外は、実施例1と同様にして紫外線を照射し評価を行った。Comparative Example 4
Instead of ingesting the UV injury prevention composition for oral consumption, UV light was applied in the same manner as in Example 1, except that only 330 mg of the trade name: POLY-PINE (registered trademark) (obtained from Sedaherb Japan) was ingested. Irradiated and evaluated.
以下、実施例1で調製した経口摂取用紫外線傷害防止組成物の評価結果を、比較例1の評価結果と併せて示す。
<評価1:紅斑(発赤)、メラニン沈着の目視判定>
紫外線照射1日後に紅斑(発赤)の発生、7日後にメラニン沈着の有無を以下の4段階に分けて各部位の目視判定を行った。結果を表3に示す。
− :紅斑(発赤)、或いはメラニン沈着なし
± :紅斑(発赤)、或いはメラニン沈着の有無が判断つかず
+ :紅斑(発赤)、或いはメラニン沈着あり
++:顕著に紅斑(発赤)、或いはメラニン沈着ありHereinafter, the evaluation result of the composition for preventing UV injury for oral intake prepared in Example 1 is shown together with the evaluation result of Comparative Example 1.
<Evaluation 1: Visual determination of erythema (redness) and melanin deposition>
After 1 day of ultraviolet irradiation, the occurrence of erythema (redness) was observed, and 7 days later, the presence or absence of melanin deposition was divided into the following four stages, and each part was visually judged. The results are shown in Table 3.
-: No erythema (redness) or melanin deposition ±: Cannot be judged whether erythema (redness) or melanin deposition +: Erythema (redness) or melanin deposition ++: Remarkably erythema (redness) or melanin deposition Yes
<評価2:メグサメーターによる紅斑(発赤)及びメラニン沈着の測定>
紫外線照射1日後に紅斑(発赤)の発生を、メグサメーターMX18(Courage+Khazaka Elctronic Gmbh製)を用いて測定した。紅斑(発赤)の発生については、波長660nmにおける各部位の反射光強度(エリスマ値)を評価に用いた。基準(Reference)としては、波長880nmにおける各部位の反射光強度を用いた。結果を図2、図3に示す。ここで、図3の縦軸は「Δエリスマ値」であり、図2の3点移動平均曲線から得られる極小値との差の値である。図2と図3の横軸(相対紫外線照射量)の単位は、5.83[μW/(cm2/hr)]である。<Evaluation 2: Measurement of erythema (redness) and melanin deposition by meggameter>
The occurrence of erythema (redness) 1 day after UV irradiation was measured using a megsometer MX18 (Courage + Khazaka Elctronic Gmbh). For the occurrence of erythema (redness), the reflected light intensity (erythma value) of each part at a wavelength of 660 nm was used for evaluation. As the reference, the reflected light intensity of each part at a wavelength of 880 nm was used. The results are shown in FIGS. Here, the vertical axis of FIG. 3 is the “Δ erythma value”, which is a difference value from the minimum value obtained from the three-point moving average curve of FIG. The unit of the horizontal axis (relative ultraviolet irradiation amount) in FIGS. 2 and 3 is 5.83 [μW / (cm 2 / hr)].
図4に示す解析方法によって、図2、図3及び表3に示した紅斑(発赤)の発生結果を考察した。その考察結果を表4、表5、図5に示す。ここで、
図4記載のy軸は、Δエリスマ値又は4段階に分けた目視判定結果、
bは、比較例1の目視判定結果が−から±に変化する紫外線照射量、或いはメグサメーターから得られたΔエリスマ値を直線近似したときのx切片の値、
dは、実施例1の目視判定結果が−から±に変化する紫外線照射量、或いはメグサメーターから得られたΔエリスマ値を直線近似したときのx切片の値、
b20は、比較例1のΔエリスマ値が20上昇した時の相対紫外線照射量の照射量、
d20は、実施例1のΔエリスマ値が20上昇した時の相対紫外線照射量の照射量、
MEDは、比較例1の目視判定が±から+に変化したとき、つまり目視で紅斑(発赤)を確認できる最低の紫外線照射量、
HEDは、比較例1の目視判定が+から++に変化したときの紫外線照射量、
ΔMEDは、(実施例1における目視で紅斑(発赤)を確認できる最低の紫外線照射量)−(比較例1における目視で紅斑(発赤)を確認できる最低の紫外線照射量)、
ΔHEDは、(実施例1の紅斑(発赤)の目視判定が+から++に変化したときの紫外線照射量)−(比較例1の紅斑(発赤)の目視判定が+から++に変化したときの紫外線照射量)
をそれぞれ表し、実施例1のエリスマ値の結果を直線近似したときの近似式を、y=c(x−d)、比較例1のエリスマ値の結果を直線近似したときの近似式をy=a(x−b)とした。
ΔMMDは、(実施例1における目視でメラニン沈着を確認できる最低の紫外線照射量)−(比較例1における目視でメラニン沈着を確認できる最低の紫外線照射量)、
ΔHMDは、(実施例1のメラニン沈着の目視判定が+から++に変化したときの紫外線照射量)−(比較例1のメラニン沈着の目視判定が+から++に変化したときの紫外線照射量)With the analysis method shown in FIG. 4, the results of the occurrence of erythema (redness) shown in FIG. 2, FIG. 3 and Table 3 were considered. The consideration results are shown in Table 4, Table 5, and FIG. here,
The y-axis shown in FIG. 4 is the Δ erythma value or the visual judgment result divided into four stages,
b is the ultraviolet ray irradiation amount in which the visual determination result of Comparative Example 1 changes from − to ±, or the value of the x intercept when linearly approximating the Δ erythma value obtained from the megsometer,
d is the UV irradiation amount at which the visual judgment result of Example 1 changes from − to ±, or the value of the x intercept when linearly approximating the Δ erythma value obtained from the megsometer,
b20 is the irradiation amount of the relative ultraviolet irradiation amount when the Δ-erythma value of Comparative Example 1 is increased by 20,
d20 is the irradiation amount of the relative ultraviolet irradiation amount when the Δ-erythma value of Example 1 is increased by 20,
MED is the lowest UV irradiation amount that can confirm erythema (redness) visually when the visual judgment of Comparative Example 1 changes from ± to +, that is,
HED is the amount of UV irradiation when the visual judgment in Comparative Example 1 changes from + to ++,
ΔMED is (the lowest UV irradiation amount that can visually confirm erythema (redness) in Example 1)-(the lowest UV radiation amount that can visually confirm erythema (redness) in Comparative Example 1),
ΔHED is (the amount of ultraviolet irradiation when the visual judgment of erythema (redness) in Example 1 changes from + to ++) − (when the visual judgment of erythema (redness) in Comparative Example 1 changes from + to ++. UV irradiation)
Respectively, y = c (x−d) is an approximate expression when the result of the elliptic value of Example 1 is linearly approximated, and y = c (x−d) is an approximate expression when the result of the elliptic value of Comparative Example 1 is linearly approximated. It was set as a (xb).
ΔMMD is (the lowest UV irradiation amount at which melanin deposition can be confirmed visually in Example 1)-(the lowest UV irradiation amount at which melanin deposition can be confirmed visually in Comparative Example 1),
ΔHMD is (the amount of UV irradiation when the visual judgment of melanin deposition in Example 1 changes from + to ++) − (the amount of UV irradiation when the visual judgment of melanin deposition in Comparative Example 1 changes from + to ++)
また、目視判定においては、「ΔMED」及び「ΔHED」の値が0以上である場合に、効果ありとし、これらの中で「ΔHED」が0より大きい場合には著効とした。メグサメーターによる判定においては、紫外線照射量の依存性があり、「d−b」及び「d20−b20」の値が0以上である場合に、効果ありとし、「d−b」及び「d20−b20」の値が共に0より大きい場合には著効とした。更に総合判定としては、目視判定及びメグサメーターによる判定結果の何れかで効果が認められたときに効果ありとし、目視判定及びメグサメーターによる判定が共に著効の場合には、総合判定は著効とした。 Further, in the visual judgment, when the values of “ΔMED” and “ΔHED” are 0 or more, it is considered effective, and when “ΔHED” is larger than 0, it is markedly effective. In the determination by the megsometer, there is dependency on the amount of ultraviolet irradiation, and when the values of “db” and “d20-b20” are 0 or more, it is considered effective, and “db” and “d20-b20”. When both values were greater than 0, the results were markedly effective. In addition, the overall judgment is effective when the effect is recognized by either the visual judgment or the judgment result by the meggameter. If both the visual judgment and the judgment by the meggameter are both effective, the overall judgment is markedly effective. .
紅斑(発赤)の解析結果を以下の表4に示す。表4に示す数値(相対紫外線照射量)の単位は、5.83[μW/(cm2/hr)]である。
メラニン沈着の解析結果を以下の表5に示す。表5に示す数値(相対紫外線照射量)の単位は、5.83[μW/(cm2/hr)]である。また、表5中「SD」は、標準偏差を示す。
表4より、メグサメーターによる紅斑(発赤)の測定結果は、目視判定と同様の傾向を示すことが分かった。これらの結果、7人全員が総合判定で効果が認められ、28日間本発明の経口摂取用紫外線傷害防止組成物を摂取することで、紫外線照射により誘発される傷害を防止する効果がみられることが分かった。また、特に顕著な効果がみられた被験者No.1、No.6及びNo.7では、目視判定とメグサメーターによる判定結果が定量的にも近い結果が得られた。 From Table 4, it was found that the measurement result of erythema (redness) by the meggameter showed the same tendency as the visual judgment. As a result of these, all 7 people have an effect in the comprehensive judgment, and by taking the ultraviolet ray injury preventing composition for oral intake of the present invention for 28 days, the effect of preventing the injury induced by ultraviolet irradiation is seen. I understood. In addition, the subject No. in which a particularly remarkable effect was observed. 1, no. 6 and no. In No. 7, the visual determination and the determination result by the meggameter were quantitatively close.
また、図4に示した解析方法を用いて全ての被験者の結果を平均化したものを図5に示した。図3及び図5からも分かるように、本発明の経口摂取用紫外線傷害防止組成物を摂取すると、エリスマ値の変化が小さくなる効果、つまり、紫外線照射による傷害を防止する効果があることが分かった。 Moreover, what averaged the result of all the test subjects using the analysis method shown in FIG. 4 was shown in FIG. As can be seen from FIG. 3 and FIG. 5, it can be seen that when the composition for preventing UV injury for oral consumption of the present invention is ingested, the effect of reducing the change in the erythema value, that is, the effect of preventing injury due to UV irradiation. It was.
メラニン沈着の測定結果に関しても、目視判定では、7人中6人に効果が認められ、28日間本発明の経口摂取用紫外線傷害防止組成物を摂取することで、紫外線照射により誘発されるメラニン沈着を防止する効果がみられることが分かった(表5)。 Regarding the measurement result of melanin deposition, an effect was recognized in 6 out of 7 people by visual judgment, and melanin deposition induced by ultraviolet irradiation by ingesting the UV injury prevention composition for oral consumption of the present invention for 28 days. It was found that the effect of preventing the occurrence was observed (Table 5).
腸溶剤としてパーム油脂で包摂はしてあるが、腸溶被覆剤で被覆していない実施例2の経口摂取用紫外線傷害防止組成物の場合は、紫外線照射により誘発される傷害を防止する効果が実施例1のものより劣っていたが、やはり効果を奏するものであった。実施例1と実施例2を比較することで、腸溶被覆剤による被覆に効果があることが確かめられた。 In the case of the UV injury-preventing composition for ingestion of Example 2 that is included in palm oil or fat as an intestinal solvent but is not coated with an enteric coating agent, it has the effect of preventing damage induced by UV irradiation. Although it was inferior to that of Example 1, it was still effective. By comparing Example 1 and Example 2, it was confirmed that the coating with an enteric coating was effective.
キューカミス・メロの変種の果実(特定メロン)から得られた成分のみを、腸溶剤としてパーム油脂で包摂し、腸溶被覆剤としてゼインで被覆した実施例3の経口摂取用紫外線傷害防止組成物は、紫外線照射により誘発される傷害を防止する効果が実施例1のものより若干劣ってはいたが、やはり顕著な効果を奏するものであった。 The composition for preventing UV injury of orally ingested Example 3 in which only the components obtained from the fruit of a variety of Cucumis melo (specific melon) were included with palm oil as an intestinal solvent and coated with zein as an enteric coating agent, Although the effect of preventing injury induced by ultraviolet irradiation was slightly inferior to that of Example 1, it still showed a remarkable effect.
また、実施例3において、腸溶被覆剤としてゼインで被覆していないものも、紫外線照射により誘発される傷害を防止する効果を奏した。ただし、実施例3の経口摂取用紫外線傷害防止組成物に比べ、胃で分解が起こったためと考えられるが、紫外線照射により誘発される傷害を防止する効果が劣っていた。 Moreover, in Example 3, what was not coat | covered with zein as an enteric coating agent also had the effect which prevents the injury induced by ultraviolet irradiation. However, although it is considered that decomposition occurred in the stomach as compared with the ultraviolet ray injury preventing composition for oral intake of Example 3, the effect of preventing injury induced by ultraviolet irradiation was inferior.
特定メロンから得られた成分に、ビタミンC、ブドウの果皮若しくは種子由来のポリフェノール成分等を含有する赤ワイン成分、及び/又は、ヒドロキシフラバン若しくはその誘導体又はそれらのオリゴマー等の松樹皮から得られた成分を組み合わすことで、相乗的に効果が向上していることが分かった。 Ingredients obtained from specific melon, vitamin C, red wine ingredient containing grape skin or seed-derived polyphenol ingredients, and / or ingredients obtained from pine bark such as hydroxyflavan or derivatives thereof or oligomers thereof It was found that the effect was synergistically improved by combining.
また、本発明の経口摂取用紫外線傷害防止組成物ではなく、ビタミンCのみ(比較例2)、赤ワイン成分のみ(比較例3)、松樹皮から得られた成分のみ(比較例4)を、同量摂取しても、比較例1と同程度の結果であり、実施例のような顕著な効果は全く見られなかった。 In addition, the composition of the present invention is not the composition for preventing UV injury for oral intake, but only vitamin C (Comparative Example 2), only the red wine component (Comparative Example 3), and only the component obtained from pine bark (Comparative Example 4). Even when the amount was ingested, the result was similar to that of Comparative Example 1, and no significant effect as in the Example was observed.
実施例4
更に、健康な35歳から45歳の女性4人(被験者No.8〜No.11)について、実施例1と同様の経口摂取用紫外線傷害防止組成物を、実施例1と同様に摂取させ、同様に紫外線を照射し評価を行った。Example 4
Further, for four healthy 35- to 45-year-old women (subjects No. 8 to No. 11), the same composition for oral injury as in Example 1 was ingested in the same manner as in Example 1, Similarly, ultraviolet rays were irradiated for evaluation.
比較例5
経口摂取用紫外線傷害防止組成物を摂取させない以外は、実施例4と同様にして紫外線を照射し評価を行った。このときの紫外線照射は、図1の非摂取[1]の部分、非摂取[2]の部分に、実施例1と同様に表2に示す照射量で行った。Comparative Example 5
Evaluation was performed by irradiating with ultraviolet rays in the same manner as in Example 4 except that the composition for preventing oral injury of ultraviolet rays was not ingested. The ultraviolet irradiation at this time was performed at the doses shown in Table 2 in the same manner as in Example 1 in the non-intake [1] and non-intake [2] portions of FIG.
<評価3:紅斑(発赤)、メラニン沈着の目視判定>
紫外線照射1日後に紅斑(発赤)の発生、7日後にメラニン沈着の有無を、以下の4段階に分けて各部位の目視判定を行った。実施例4と比較例5の評価結果を併せて表6に示す。
− :紅斑(発赤)、或いはメラニン沈着なし
± :紅斑(発赤)、或いはメラニン沈着の有無が判断つかず
+ :紅斑(発赤)、或いはメラニン沈着あり
++:顕著に紅斑(発赤)、或いはメラニン沈着あり<Evaluation 3: Visual determination of erythema (redness) and melanin deposition>
The appearance of erythema (redness) occurred 1 day after UV irradiation, and the presence or absence of melanin deposition after 7 days, was visually determined for each site in the following four stages. The evaluation results of Example 4 and Comparative Example 5 are shown together in Table 6.
-: No erythema (redness) or melanin deposition ±: Cannot be judged whether erythema (redness) or melanin deposition +: Erythema (redness) or melanin deposition ++: Remarkably erythema (redness) or melanin deposition Yes
<評価4:メグサメーターによる紅斑(発赤)の測定>
紫外線照射1日後に紅斑(発赤)の発生を、メグサメーターMX18(Courage+Khazaka Elctronic Gmbh社製)を用いて測定した。紅斑(発赤)の発生については、波長660nmにおける各部位の反射光強度(エリスマ値)を評価に用いた。基準(Reference)としては、波長880nmにおける各部位の反射光強度を用いた。結果を図6と図7に示す。図6と図7の横軸の単位(相対照射紫外線量)(MED)は、1[MED]=5.83[μW/(cm2/hr)]である。<Evaluation 4: Measurement of erythema (redness) by meggameter>
The occurrence of erythema (redness) 1 day after the ultraviolet irradiation was measured using a meggameter MX18 (Courage + Khazaka Elctronic Gmbh). For the occurrence of erythema (redness), the reflected light intensity (erythma value) of each part at a wavelength of 660 nm was used for evaluation. As the reference, the reflected light intensity of each part at a wavelength of 880 nm was used. The results are shown in FIGS. 6 and 7, the unit of the horizontal axis (relative irradiation ultraviolet ray amount) (MED) is 1 [MED] = 5.83 [μW / (cm 2 / hr)].
<評価5:紫外線照射による紅斑(発赤)防止効果の確認>
更に、本発明の効果を確認するため、以下の評価を行った。上記評価1、評価3で得られた目視判定において、紫外線照射1日後の紅斑(発赤)の目視判定で(±)を与える紫外線量の2段階下の紫外線量(以下、「紅斑生成検出線量」と略記する)を各被験者で求めた。次に、評価2、評価4の結果をもとに、紫外線量0から紅斑生成検出線量までのエリスマ値の平均値を各被験者で求めた。エリスマ値は1被験者あたり2か所以上で測定、1箇所でのエリスマ値は5回測定の平均値である。結果を表7に示す。<Evaluation 5: Confirmation of erythema (redness) prevention effect by ultraviolet irradiation>
Furthermore, in order to confirm the effect of the present invention, the following evaluation was performed. In the visual judgment obtained in the above-mentioned
なお、表7中の「SD」は、標準偏差を示し、「P値」(P−value)」は、帰無仮説を「非摂取と摂取とでエリスマ値の平均値に差がない」としたときの有意確率である。通常、P値が0.05以下なら、帰無仮説は棄却されて両分布には有意差があるとされ、0.01以下なら極めて有意差があるとされる。 In Table 7, “SD” indicates standard deviation, and “P value” (P-value) indicates that the null hypothesis is that there is no difference in the average value of the erythema value between non-intake and intake. This is the significance probability. Normally, if the P value is 0.05 or less, the null hypothesis is rejected, and both distributions are considered to have a significant difference, and if it is 0.01 or less, it is assumed that there is a very significant difference.
表7の結果から明らかなように、本発明の経口摂取用紫外線傷害防止組成物を摂取した場合(実施例1、4)は、非摂取の場合(比較例1、5)と比較して、評価5におけるエリスマ値の平均値がほぼ全ての被験者において小さかった。また、P値が0.0028であったことから、帰無仮説「非摂取と摂取とでエリスマ値の平均値に差がない」は、0.0028の確率でしか正しくないことが分かった。すなわち、上記帰無仮説は棄却されて両分布には有意差があることが分かった。言い換えると、本発明の経口摂取用紫外線傷害防止組成物を摂取した場合は、非摂取の場合と比較して、有意差ありでエリスマ値の平均値が小さくなることが分かった。 As is clear from the results of Table 7, when the composition for preventing UV injury of oral intake of the present invention was ingested (Examples 1 and 4), compared with the case of non-ingestion (Comparative Examples 1 and 5), The average value of the erythema value in Evaluation 5 was small in almost all subjects. Further, since the P value was 0.0028, it was found that the null hypothesis “there is no difference in the average value of the erythema value between non-intake and intake” is only correct with a probability of 0.0028. In other words, the null hypothesis was rejected and it was found that there was a significant difference between the two distributions. In other words, it was found that when the composition for preventing UV injury for oral intake of the present invention was ingested, the average value of the erythema value was small with a significant difference compared to the case of non-ingestion.
すなわち、紫外線照射による紅斑(発赤)生成に至らない程度の紫外線量(紫外線量0から紅斑生成検出線量)を照射させた場合であっても、本発明の経口摂取用紫外線傷害防止組成物を摂取した場合は、非摂取の場合と比較して、照射部位のエリスマ値が有意に低下しており、紅斑生成検出線量を照射していない肌の赤味(エリスマ値)が低下していたことが帰結された。 That is, even when the amount of ultraviolet rays that does not lead to the generation of erythema (redness) due to ultraviolet irradiation (irradiation detection dose from 0 to the amount of ultraviolet rays) is irradiated, the composition for preventing UV injury of the present invention is ingested. In that case, compared to the case of non-ingestion, the erythema value of the irradiated site was significantly reduced, and the redness (erythma value) of the skin not irradiated with the erythema production detection dose was reduced. As a result.
以上より、本発明の経口摂取用紫外線傷害防止組成物を経口摂取することで、紫外線照射により誘発される傷害、例えば紅斑(発赤)の発生やメラニン沈着を抑制する効果がみられることが分かった(実施例1〜3、比較例1〜4、評価1、2)。更に、紫外線照射による傷害が目視で観察できる程度にまで至らない場合であっても、かかる紫外線照射量で照射した部位のエリスマ値が、摂取後は摂取前と比較して有意に低下しており、すなわち、摂取後は美白効果が認められた(実施例4、比較例4、評価3〜5)。
From the above, it was found that by ingesting the ultraviolet ray injury preventing composition for oral consumption of the present invention, the effects of suppressing the occurrence of damage induced by ultraviolet irradiation, such as erythema (redness) and melanin deposition, were observed. (Examples 1 to 3, Comparative Examples 1 to 4,
本発明の経口摂取用紫外線傷害防止組成物は、生体に本来備わった抗活性酸素の機能を促進する効果があり、活性酸素及び酸化に由来する老化や疾病の予防等に広く利用されるものである。例えば、循環器系、呼吸器系、脳神経系、消化器系、血液系、内分泌系、泌尿器系、支持組織系、生殖器系等の疾患及び皮膚のシミ、皺、火傷や老人斑の防止、保湿性、ストレスに対する抵抗性、農薬、有機溶剤や合成化合物等によるアトピーやアレルギーの抑制等の予防に広く利用されるものである。 The composition for preventing UV injury of oral intake of the present invention has an effect of promoting the function of anti-active oxygen inherent in the living body, and is widely used for the prevention of aging and diseases derived from active oxygen and oxidation. is there. For example, diseases of the circulatory system, respiratory system, cranial nervous system, digestive system, blood system, endocrine system, urinary system, supporting tissue system, genital system, etc. and prevention of skin spots, wrinkles, burns and senile plaques, moisturizing It is widely used for the prevention of atopy and allergy suppression by sex, resistance to stress, agricultural chemicals, organic solvents and synthetic compounds.
本願は、2007年8月9日に出願した日本の特許出願である特願2007−208434に基づくものであり、それらの出願の全ての内容はここに引用し、本発明の明細書の開示として取り込まれるものである。 This application is based on Japanese Patent Application No. 2007-208434 filed on August 9, 2007, the entire contents of which are hereby incorporated by reference herein as disclosure of the specification of the present invention. It is taken in.
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| PCT/JP2008/064254 WO2009020192A1 (en) | 2007-08-09 | 2008-08-07 | Composition for oral intake for preventing ultraviolet damage |
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|---|---|---|---|---|
| JP2000069938A (en) * | 1998-08-31 | 2000-03-07 | Bizen Kasei Kk | Skin whitening agent for oral intake and its use |
| JP2000125823A (en) * | 1998-10-16 | 2000-05-09 | Fiburo Seiyaku Kk | Red grape extract powder, grape seed extract powder, method for producing beverage containing galacto-oligosaccharide as a main component, and red grape extract powder and grape seed extract powder used in the method |
| JP2003002840A (en) * | 2001-03-20 | 2003-01-08 | Bio-Obtention Sc | Cucumismelo extract coated and / or microencapsulated in a fat-soluble agent based on fatty substances |
| JP2005170834A (en) * | 2003-12-10 | 2005-06-30 | Taiyo Yakuhin Kogyo Kk | Skin ameliorating preparation |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2000069938A (en) * | 1998-08-31 | 2000-03-07 | Bizen Kasei Kk | Skin whitening agent for oral intake and its use |
| JP2000125823A (en) * | 1998-10-16 | 2000-05-09 | Fiburo Seiyaku Kk | Red grape extract powder, grape seed extract powder, method for producing beverage containing galacto-oligosaccharide as a main component, and red grape extract powder and grape seed extract powder used in the method |
| JP2003002840A (en) * | 2001-03-20 | 2003-01-08 | Bio-Obtention Sc | Cucumismelo extract coated and / or microencapsulated in a fat-soluble agent based on fatty substances |
| JP2005170834A (en) * | 2003-12-10 | 2005-06-30 | Taiyo Yakuhin Kogyo Kk | Skin ameliorating preparation |
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