JPWO2019049964A1 - Anti-fatigue oral composition - Google Patents
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/115—Fatty acids or derivatives thereof; Fats or oils
- A23L33/12—Fatty acids or derivatives thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/164—Amides, e.g. hydroxamic acids of a carboxylic acid with an aminoalcohol, e.g. ceramides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/16—Emollients or protectives, e.g. against radiation
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/02—Nutrients, e.g. vitamins, minerals
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/06—Fungi, e.g. yeasts
- A61K36/062—Ascomycota
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/48—Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
Abstract
セラミドを含む抗疲労経口組成物が提供される。An anti-fatigue oral composition comprising ceramide is provided.
Description
本発明は、抗疲労経口組成物等に関する。 The present invention relates to an anti-fatigue oral composition and the like.
近年、セラミドはヒト表皮の細胞間脂質の主成分であることから、機能性化粧品素材等として市場を拡大している。加齢による角質セラミドは徐々に減少することが知られており、このため外用セラミドの補給が健康な肌を保つために重要ではないかと考えられている。また、角質層細胞間脂質として存在するセラミドは遊離型のフリーセラミドであることから、フリーセラミドにも注目が集まっている。 In recent years, ceramide has been expanding its market as a functional cosmetic material because it is a main component of intercellular lipids in human epidermis. It is known that keratin ceramide with age gradually decreases, and it is considered that supplementation of topical ceramide is important for maintaining healthy skin. In addition, since ceramide existing as an intercellular lipid in the stratum corneum is a free ceramide, free ceramide is also attracting attention.
これまでに、有用なセラミドを効率的に調製するための研究も行われてきている（例えば特許文献１）。 So far, studies have been conducted to efficiently prepare useful ceramides (for example, Patent Document 1).
セラミドについては、その肌への与える効果に関しては研究開発が盛んに行われているものの、その他の機能についてはほとんど研究開発はなされていない。 Regarding ceramide, although research and development has been actively carried out on its effect on the skin, little research and development has been carried out on other functions.
そこで、本発明は、セラミドの新たな機能を見出すことを課題とする。 Therefore, an object of the present invention is to find a new function of ceramide.
本発明者らは、セラミドを経口摂取することにより、抗疲労効果が奏される可能性を見出し、さらに改良を重ねて本発明を完成させるに至った。 The present inventors have found that oral ingestion of ceramide may exert an anti-fatigue effect, and have made further improvements to complete the present invention.
本発明は例えば以下の項に記載の主題を包含する。
項１．
セラミドを含む、抗疲労経口組成物。
項２．
フリーセラミドを含む、項１に記載の抗疲労経口組成物。
項３．
セラミド骨格が（ヒドロキシル基を３個有し、炭素数１８で、炭素間二重結合を０又は１個有するスフィンゴイド塩基）−（炭素数２２〜２６、炭素間二重結合が０、ヒドロキシル基を０、１、又は２個有する脂肪酸）の組み合わせであるフリーセラミド、並びに、セラミド骨格が（ヒドロキシル基を３個有し、炭素数２０で、炭素間二重結合を有さないスフィンゴイド塩基）−（炭素数２４又は２５、炭素間二重結合が０、ヒドロキシル基を０、１又は２個有する脂肪酸）の組み合わせであるフリーセラミド、
からなる群より選択される少なくとも１種のフリーセラミドを含む、
項２に記載の抗疲労経口組成物。
項４．
ｔ１８：０−２２：０ｈ、
ｔ１８：１−２２：０ｈ、
ｔ１８：０−２３：０ｈ、
ｔ１８：１−２３：０ｈ、
ｔ１８：０−２４：０ｈ、
ｔ１８：１−２４：０ｈ、
ｔ２０：０−２４：０ｈ、
ｔ１８：１−２６：０ｈ、
ｔ１８：０−２５：０ｈ、及び
ｔ１８：０−２４：０ｈ２
からなる群より選択される少なくとも１種のフリーセラミドを含む、
項３に記載の抗疲労経口組成物。
項５．
少なくとも、ｔ１８：０−２４：０ｈ、ｔ１８：１−２４：０ｈ、及びｔ２０：０−２４：０ｈを含む、項４に記載の抗疲労経口組成物。
項６．
ｔ１８：０−２４：０ｈ、ｔ１８：１−２４：０ｈ、及びｔ２０：０−２４：０ｈの合計量が、含有されるフリーセラミド全量の３０質量％以上である、
項５に記載の抗疲労経口組成物。
項７．
抗疲労が、体の疲れやすさ改善、及び／又は、全身倦怠感改善である、項１〜６のいずれかに記載の抗疲労経口組成物。
項８．
ｔ１８：０−２２：０ｈ、
ｔ１８：１−２２：０ｈ、
ｔ１８：０−２３：０ｈ、
ｔ１８：１−２３：０ｈ、
ｔ１８：０−２４：０ｈ、
ｔ１８：１−２４：０ｈ、
ｔ２０：０−２４：０ｈ、
ｔ１８：１−２６：０ｈ、
ｔ１８：０−２５：０ｈ、及び
ｔ１８：０−２４：０ｈ２
からなる群より選択される少なくとも１種のフリーセラミドを含む、経口セラミド組成物。
項９．
少なくとも、ｔ１８：０−２４：０ｈ、ｔ１８：１−２４：０ｈ、及びｔ２０：０−２４：０ｈを含む、項８に記載の経口セラミド組成物。
項１０．
ｔ１８：０−２４：０ｈ、ｔ１８：１−２４：０ｈ、及びｔ２０：０−２４：０ｈの合計量が、含有されるフリーセラミド全量の３０質量％以上である、
項９に記載の経口セラミド組成物。
項１１．
速攻吸収用である、項１〜１０のいずれかに記載の経口セラミド組成物。
項１２．
速効疲労回復用である、項１〜１０のいずれかに記載の経口セラミド組成物。The present invention includes, for example, the subjects described in the following sections.
An anti-fatigue oral composition comprising ceramide.
The ceramide skeleton is (a sphingoid base having 3 hydroxyl groups, 18 carbon atoms and 0 or 1 carbon-carbon double bond)-(22 to 26 carbon atoms, 0 carbon-carbon double bond, hydroxyl group. Free ceramide, which is a combination of (fatty acid having 0, 1, or 2), and ceramide skeleton (sphingoid base having 3 hydroxyl groups, 20 carbon atoms, and no intercarbon double bond). Free ceramide, which is a combination of-(fatty acid having 24 or 25 carbon atoms, 0 carbon-carbon double bond, 0, 1 or 2 hydroxyl groups).
Containing at least one free ceramide selected from the group consisting of
Item 4.
t18: 0-22: 0h,
t18: 1-22: 0h,
t18: 0-23: 0h,
t18: 1-23: 0h,
t18: 0-24: 0h,
t18: 1-24: 0h,
t20: 0-24: 0h,
t18: 1-26: 0h,
t18: 0-25: 0h, and t18: 0-24: 0h 2
Containing at least one free ceramide selected from the group consisting of
Item 5.
Item 4. The anti-fatigue oral composition according to Item 4, which comprises at least t18: 0-24: 0h, t18: 1-24: 0h, and t20: 0-24: 0h.
Item 6.
The total amount of t18: 0-24: 0h, t18: 1-24: 0h, and t20: 0-24: 0h is 30% by mass or more of the total amount of free ceramide contained.
Item 5. The anti-fatigue oral composition according to Item 5.
Item 4. The anti-fatigue oral composition according to any one of
Item 8.
t18: 0-22: 0h,
t18: 1-22: 0h,
t18: 0-23: 0h,
t18: 1-23: 0h,
t18: 0-24: 0h,
t18: 1-24: 0h,
t20: 0-24: 0h,
t18: 1-26: 0h,
t18: 0-25: 0h, and t18: 0-24: 0h 2
An oral ceramide composition comprising at least one free ceramide selected from the group consisting of.
Item 9.
Item 8. The oral ceramide composition according to Item 8, which comprises at least t18: 0-24: 0h, t18: 1-24: 0h, and t20: 0-24: 0h.
The total amount of t18: 0-24: 0h, t18: 1-24: 0h, and t20: 0-24: 0h is 30% by mass or more of the total amount of free ceramide contained.
Item 9. The oral ceramide composition according to Item 9.
Item 8. The oral ceramide composition according to any one of
Item 8. The oral ceramide composition according to any one of
本発明により、抗疲労経口組成物が提供される。当該抗疲労経口組成物は経口摂取により、疲労を改善させ得る。 The present invention provides an anti-fatigue oral composition. The anti-fatigue oral composition can improve fatigue by ingestion.
また、セラミドの経口摂取による抗疲労効果を見出すにあたり、本発明者らは特定のセラミドが経口摂取時に極めて速やかに吸収され血中にとりこまれ得ることをも見出し、この点についても検討を重ね、特定のセラミドを含むセラミド経口組成物についても発明をするに至った。本発明に包含される経口セラミド組成物は、特定のセラミドを含むことにより、特に腸管吸収性及び血中移行性に優れる。よって、これら特定のフリーセラミド種を含有する経口組成物は、他のセラミドと比べ、経口摂取時に速効性が高いと考えられる。また、公知のセラミドの効果についても、他のセラミドに比べて、経口摂取時に得られる効果は高いと考えられる。 In finding the anti-fatigue effect of oral ingestion of ceramide, the present inventors have also found that a specific ceramide can be absorbed very quickly and taken into the blood when ingested, and this point has also been studied repeatedly. He has also invented an oral ceramide composition containing a specific ceramide. The oral ceramide composition included in the present invention is particularly excellent in intestinal absorption and blood transferability by containing a specific ceramide. Therefore, it is considered that the oral composition containing these specific free ceramide species has a higher immediate effect when ingested as compared with other ceramides. In addition, regarding the effects of known ceramides, it is considered that the effects obtained by oral ingestion are higher than those of other ceramides.
以下、本発明の各実施形態について、さらに詳細に説明する。 Hereinafter, each embodiment of the present invention will be described in more detail.
本発明は抗疲労経口組成物を包含する。当該抗疲労経口組成物はセラミドを含む。セラミドはスフィンゴイド塩基のアミノ基（−ＮＨ２）に脂肪酸のカルボキシル基（−ＣＯＯＨ）が結合した構造（−ＮＨ−ＣＯ−）を有する化合物である。セラミドのスフィンゴイド塩基のアルコール性ヒドロキシル基（−ＯＨ）に、更に糖及びリン酸などの極性基が結合し、それぞれスフィンゴ糖脂質及びスフィンゴリン脂質となる。ここで、糖が結合したものを特にグリコシルセラミドと呼び、特に糖がグルコースである場合グルコシルセラミドと呼ぶ。セラミドに糖及びリン酸が結合していない場合を特にフリーセラミドと呼ぶ。本発明の抗疲労経口組成物に含まれるセラミドとしては、フリーセラミドが好適である。The present invention includes anti-fatigue oral compositions. The anti-fatigue oral composition comprises ceramide. Ceramide is a compound having a structure (-NH-CO-) in which a carboxyl group (-COOH) of a fatty acid is bonded to an amino group (-NH 2 ) of a sphingoid base. Polar groups such as sugar and phosphoric acid are further bonded to the alcoholic hydroxyl group (-OH) of the sphingoid base of ceramide to form glycosphingolipid and sphingolipid, respectively. Here, the sugar-bound substance is particularly called glycosylceramide, and particularly when the sugar is glucose, it is called glucosylceramide. The case where sugar and phosphoric acid are not bound to ceramide is particularly called free ceramide. Free ceramide is suitable as the ceramide contained in the anti-fatigue oral composition of the present invention.
フリーセラミドを構成するスフィンゴイド塩基としては、ヒドロキシル基を２又は３個有するものが好ましく、３個有するものがより好ましい。また、当該スフィンゴイド塩基は、炭素数１４〜２２（１４、１５、１６、１７、１８、１９、２０、２１、又は２２）であるものが好ましく、炭素数１６〜２０であるものがより好ましく、炭素数１８又は２０であるものがさらに好ましい。また、炭素間二重結合を０又は１有するものが好ましい。より具体的な好ましいスフィンゴイド塩基としては、例えばスフィンゴシン、ジヒドロスフィンゴシン、フィトスフィンゴシン等が挙げられる。 As the sphingoid base constituting the free ceramide, a sphingoid base having 2 or 3 hydroxyl groups is preferable, and a sphingoid base having 3 hydroxyl groups is more preferable. Further, the sphingoid base preferably has 14 to 22 carbon atoms (14, 15, 16, 17, 18, 19, 20, 21, or 22), and more preferably 16 to 20 carbon atoms. , 18 or 20 carbon atoms are more preferable. Further, those having 0 or 1 carbon-carbon double bond are preferable. More specific preferred sphingoid bases include, for example, sphingosine, dihydrosphingosine, phytosphingosine and the like.
フリーセラミドを構成する脂肪酸としては、炭素数１６〜３０（１６、１７、１８、１９、２０、２１、２２、２３、２４、２５、２６、２７、２８、２９、又は３０）の脂肪酸が好ましく、炭素数１８〜２８の脂肪酸がより好ましく、炭素数２０〜２６の脂肪酸がさらに好ましく、炭素数２２〜２６の脂肪酸がよりさらに好ましい。また、炭素間二重結合を０又は１個有する脂肪酸が好ましく、０個有する脂肪酸（すなわち飽和脂肪酸）がより好ましい。また、ヒドロキシル基を０、１、又は２個有する脂肪酸が好ましく、１又は２個有する脂肪酸がより好ましい。特に制限されないが、ヒドロキシル基を有する場合、α−ヒドロキシル基であることが好ましい。 As the fatty acid constituting the free ceramide, a fatty acid having 16 to 30 carbon atoms (16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, or 30) is preferable. , Fatty acids having 18 to 28 carbon atoms are more preferable, fatty acids having 20 to 26 carbon atoms are further preferable, and fatty acids having 22 to 26 carbon atoms are even more preferable. Further, a fatty acid having 0 or 1 carbon-carbon double bond is preferable, and a fatty acid having 0 (that is, a saturated fatty acid) is more preferable. Further, a fatty acid having 0, 1, or 2 hydroxyl groups is preferable, and a fatty acid having 1 or 2 hydroxyl groups is more preferable. Although not particularly limited, when it has a hydroxyl group, it is preferably an α-hydroxyl group.
フリーセラミドにおいて、セラミド骨格の（スフィンゴイド塩基）−（脂肪酸）の組み合わせは、上記のスフィンゴイド塩基及び脂肪酸をどのように組み合わせたものであってもよい。中でも好ましい組み合わせとして、例えば、（ヒドロキシル基を２又は３（特に３）個有するスフィンゴイド塩基）−（ヒドロキシル基を有する（特にα−ヒドロキシル基を有する）脂肪酸）の組み合わせが挙げられる。当該脂肪酸のヒドロキシル基数は０、１、又は２が好ましく、１又は２がより好ましい。 In free ceramide, the combination of (sphingoid base)-(fatty acid) of the ceramide skeleton may be any combination of the above-mentioned sphingoid base and fatty acid. Among them, a preferable combination is, for example, a combination of (sphingoid base having 2 or 3 (particularly 3) hydroxyl groups)-(fatty acid having a hydroxyl group (particularly α-hydroxyl group)). The number of hydroxyl groups of the fatty acid is preferably 0, 1, or 2, and more preferably 1 or 2.
例えば、フィトスフィンゴシン（Ｐ）とヒドロキシル基数１の脂肪酸（Ａ）の組み合わせであるセラミドＡＰ、フィトスフィンゴシン（Ｐ）とヒドロキシル基数０脂肪酸（Ｎ）の組み合わせであるセラミドＮＰ等が好ましく挙げられる。またさらに、フィトスフィンゴシン（Ｐ）とヒドロキシル基数２の脂肪酸（Ｄ）の組み合わせであるセラミドＤＰも好ましく例示できる。なお、セラミドＡＰ、及びセラミドＮＰは一般に使用される用語であるが、セラミドＤＰは本明細書中で使用する用語であって、一般に使用される用語ではない。セラミドＤＰとしては、具体的には例えば、ジヒドロキシリグノセロイルフィトスフィンゴシン等が挙げられる。 For example, ceramide AP, which is a combination of phytosphingosine (P) and a fatty acid (A) having a hydroxyl group number of 1, and ceramide NP, which is a combination of phytosphingosine (P) and a fatty acid (N) having a hydroxyl group number of 1, are preferably mentioned. Furthermore, ceramide DP, which is a combination of phytosphingosine (P) and a fatty acid (D) having a hydroxyl group number of 2, can also be preferably exemplified. Although ceramide AP and ceramide NP are commonly used terms, ceramide DP is a term used in the present specification and is not a commonly used term. Specific examples of the ceramide DP include dihydroxylignoseroyl phytosphingosine and the like.
これらのなかでも、フリーセラミドとして、（ｉ）セラミド骨格が（ヒドロキシル基を３個有し、炭素数１８で、炭素間二重結合を０又は１個有するスフィンゴイド塩基）−（炭素数２２〜２６、炭素間二重結合が０、ヒドロキシル基を０、１、又は２個有する脂肪酸）の組み合わせであるフリーセラミド、並びに、（ｉｉ）セラミド骨格が（ヒドロキシル基を３個有し、炭素数２０で、炭素間二重結合を有さないスフィンゴイド塩基）−（炭素数２４又は２５、炭素間二重結合が０、ヒドロキシル基を０、１、又は２個有する脂肪酸）の組み合わせであるフリーセラミド、が好ましい。なかでも、より具体的には例えば、ｔ１８：０−２２：０ｈ、ｔ１８：１−２２：０ｈ、ｔ１８：０−２３：０ｈ、ｔ１８：１−２３：０ｈ、ｔ１８：０−２４：０ｈ、ｔ１８：１−２４：０ｈ、ｔ２０：０−２４：０ｈ、ｔ１８：１−２６：０ｈ、ｔ１８：０−２５：０ｈ、及びｔ１８：０−２４：０ｈ２等が好ましい。なお、当該表記について「ｔ１８：０−２２：０ｈ」を例に挙げて説明すると、この前半部分の「ｔ１８：０」がスフィンゴイド塩基についての情報であって、ヒドロキシル基を３個（「ｔ」）有し、炭素数が「１８」で、炭素間二重結合を「０」個有する（すなわち、炭素間二重結合を有さない）スフィンゴイド塩基を示している。また、この後半部分「２２：０ｈ」が脂肪酸についての情報であって、炭素数「２２」、炭素間二重結合が「０」、ヒドロキシル基を１個有する（「ｈ」）脂肪酸である脂肪酸であることを示している。なお、「ｈ２」はヒドロキシル基を２個有することを示す。Among these, as free ceramide, (i) a ceramide skeleton (a sphingoid base having 3 hydroxyl groups, 18 carbon atoms and 0 or 1 carbon-carbon double bond)-(22 to 22 carbon atoms). 26, free ceramide which is a combination of 0 carbon-carbon double bonds, 0, 1, or 2 hydroxyl groups), and (ii) ceramide skeleton (having 3 hydroxyl groups and 20 carbon atoms). Free ceramide which is a combination of (sphingoid base having no intercarbon double bond)-(fatty acid having 24 or 25 carbon atoms, 0 intercarbon double bond, 0, 1, or 2 hydroxyl groups). , Are preferred. Among them, more specifically, for example, t18: 0-22: 0h, t18: 1-22: 0h, t18: 0-23: 0h, t18: 1-23: 0h, t18: 0-24: 0h, T18: 1-24: 0h, t20: 0-24: 0h, t18: 1-26: 0h, t18: 0-25: 0h, t18: 0-24: 0h 2 and the like are preferable. When the notation is explained by taking "t18: 0-22: 0h" as an example, "t18: 0" in the first half is information about a sphingoid base and has three hydroxyl groups ("t"). It shows a sphingoid base having "18" carbon atoms and having "0" carbon-carbon double bonds (ie, no carbon-carbon double bonds). Further, the latter half "22: 0h" is information about the fatty acid, which is a fatty acid having a carbon number of "22", an intercarbon double bond of "0", and one hydroxyl group ("h"). It shows that. In addition, "h 2 " indicates that it has two hydroxyl groups.
上記具体的なフリーセラミドの中でも、特にｔ１８：０−２４：０ｈ、ｔ１８：１−２４：０ｈ、及びｔ２０：０−２４：０ｈが好ましい。 Among the above-mentioned specific free ceramides, t18: 0-24: 0h, t18: 1-24: 0h, and t20: 0-24: 0h are particularly preferable.
また、本発明の抗疲労経口組成物には、少なくともフリーセラミドとしてｔ１８：０−２４：０ｈ、ｔ１８：１−２４：０ｈ、及びｔ２０：０−２４：０ｈが含まれることが好ましく、当該組成物に含まれるフリーセラミド全量に対して、ｔ１８：０−２４：０ｈ、ｔ１８：１−２４：０ｈ、及びｔ２０：０−２４：０ｈの合計量が３０質量％、４０質量％、又は５０質量％以上となることがより好ましい。 Further, the anti-fatigue oral composition of the present invention preferably contains at least t18: 0-24: 0h, t18: 1-24: 0h, and t20: 0-24: 0h as free ceramide, and the composition thereof. The total amount of t18: 0-24: 0h, t18: 1-24: 0h, and t20: 0-24: 0h is 30% by mass, 40% by mass, or 50% by mass with respect to the total amount of free ceramide contained in the product. More preferably, it is% or more.
なお、各セラミドは、１種単独で又は２種以上を組み合わせて用いることができる。また、各セラミドは、公知の方法か、又は公知の方法から容易に想到できる方法により、調製することができる。また、市販されるセラミドを購入して用いることもできる。例えば、株式会社ジェヌインＲ＆Ｄから外用美容素材として販売される天然ヒト型セラミドは、本発明に係る組成物に用いるために好ましいセラミド種を多く含んでおり、好適である。また例えば、上記特許文献１に記載の方法により、本発明の抗疲労経口組成物に好適なセラミド種を含有する組成物を得ることができる。
In addition, each ceramide can be used individually by 1 type or in combination of 2 or more types. In addition, each ceramide can be prepared by a known method or a method that can be easily conceived from a known method. It is also possible to purchase and use a commercially available ceramide. For example, the natural human ceramide sold by Genuin R & D Co., Ltd. as a beauty material for external use contains a large amount of ceramide species preferable for use in the composition according to the present invention, and is suitable. Further, for example, a composition containing a ceramide species suitable for the anti-fatigue oral composition of the present invention can be obtained by the method described in
本発明に係る抗疲労経口組成物は、疲労回復及び／又は疲労予防等のために好適に用いることができる。疲労としては、特に限定されないが、例えば眠気（特に昼間の眠気）、多忙感、疲労感（例えば、体が疲れやすい、横になっていたい、ぐったりしている、身体がだるい、緊張する、等といった感覚）、積極性の欠如、充実感（元気がいっぱい、活気がわいてくる、等と行った感覚）の欠如、等が挙げられ、これらの回復及び／又は予防のために本発明に係る抗疲労経口組成物を好ましく用いることができる。 The anti-fatigue oral composition according to the present invention can be suitably used for fatigue recovery and / or fatigue prevention and the like. Fatigue is not particularly limited, but is, for example, drowsiness (especially daytime sleepiness), busyness, tiredness (for example, the body is easily tired, wants to lie down, is tired, feels tired, is tense, etc.) Sense), lack of positivity, lack of fulfillment (feeling of full energy, vitality, etc.), etc., and anti-fatigue according to the present invention for recovery and / or prevention of these. Oral compositions can be preferably used.
本発明に係る抗疲労経口組成物は、例えば、医薬分野及び食品分野で好ましく用いられる。当該組成物は、以下に詳述するように、セラミドのみからなるものでもよいし、セラミド及び他の成分（各種基剤、担体、添加剤等）を含む組成物であってもよい。セラミド含有生体組織抽出物そのものも当該組成物に含まれる。つまり、セラミド含有生体組織抽出物（及び必要に応じてさらに他の成分が配合されたもの）も本発明に係る抗疲労経口組成物として用い得る。 The anti-fatigue oral composition according to the present invention is preferably used, for example, in the fields of medicine and food. As described in detail below, the composition may consist only of ceramide, or may be a composition containing ceramide and other components (various bases, carriers, additives, etc.). The ceramide-containing biological tissue extract itself is also included in the composition. That is, a ceramide-containing biological tissue extract (and, if necessary, other components are blended) can also be used as the anti-fatigue oral composition according to the present invention.
本発明に係る抗疲労経口組成物を医薬分野（医薬品及び医薬部外品を含む）にて用いる場合、当該組成物（以下「本発明に係る医薬組成物」と記載することがある）は、各種セラミドのみからなるものでもよいし、他の成分を配合した医薬組成物でもよい。例えば、本発明に係る医薬組成物においては、有効成分であるセラミドに、必要に応じて薬学的に許容される基剤、担体、添加剤（例えば賦形剤、結合剤、崩壊剤、滑沢剤、溶剤、甘味剤、着色剤、矯味剤、矯臭剤、界面活性剤、保湿剤、保存剤、ｐＨ調整剤、粘稠化剤等）等を配合することができる。このような基材、担体、添加剤等は、例えば医薬品添加物辞典２０１６（株式会社薬事日報社）に具体的に記載されており、例えばこれに記載されるものを用いることができる。また製剤形態も特に制限されず、常法により有効成分及びその他の成分を混合し、例えば錠剤、被覆錠剤、散剤、顆粒剤、細粒剤、カプセル剤、丸剤、液剤、懸濁剤、乳剤、ゼリー剤、チュアブル剤、ソフト錠剤等の製剤に調製することができる。例えば、錠剤の製造は打錠法により行い得る。混合した原料をそのまま打錠する直接打錠法、混合した原料を顆粒にしてから打錠する顆粒打錠法、のいずれも用い得る。また例えば、カプセル剤の場合はソフトカプセル及びハードカプセルのいずれであってもよい。 When the anti-fatigue oral composition according to the present invention is used in the pharmaceutical field (including pharmaceuticals and quasi-drugs), the composition (hereinafter, may be referred to as "pharmaceutical composition according to the present invention") is used. It may be composed of only various ceramides, or may be a pharmaceutical composition containing other ingredients. For example, in the pharmaceutical composition according to the present invention, the active ingredient ceramide is optionally pharmaceutically acceptable base, carrier, additive (eg, excipient, binder, disintegrant, lubricant). Agents, solvents, sweeteners, colorants, flavoring agents, odorants, surfactants, moisturizers, preservatives, pH adjusters, thickening agents, etc.) and the like can be blended. Such base materials, carriers, additives and the like are specifically described in, for example, the Pharmaceutical Additives Dictionary 2016 (Yakuji Nippo Co., Ltd.), and those described therein can be used, for example. The formulation form is also not particularly limited, and the active ingredient and other ingredients are mixed by a conventional method, for example, tablets, coated tablets, powders, granules, fine granules, capsules, pills, liquids, suspensions, emulsions. , Jelly agents, chewable agents, soft tablets and the like. For example, tablets can be produced by the tableting method. Either a direct tableting method in which the mixed raw material is tableted as it is or a granule tableting method in which the mixed raw material is granulated and then tableted can be used. Further, for example, in the case of a capsule, it may be either a soft capsule or a hard capsule.
本発明に係る医薬組成物におけるセラミドの配合量は、抗疲労効果が発揮される限り特に制限されず、対象者に応じて適宜設定できる。好ましくは０．０００５〜１００質量％、より好ましくは０．００５〜９０質量％、さらに好ましくは０．０５〜８０質量％である。なお、下限は１０質量％、２０質量％、３０質量％、４０質量％、５０質量％、６０質量％、７０質量％、又は８０質量％程度であってもよい。 The blending amount of ceramide in the pharmaceutical composition according to the present invention is not particularly limited as long as the anti-fatigue effect is exhibited, and can be appropriately set according to the subject. It is preferably 0.0005 to 100% by mass, more preferably 0.005 to 90% by mass, and further preferably 0.05 to 80% by mass. The lower limit may be about 10% by mass, 20% by mass, 30% by mass, 40% by mass, 50% by mass, 60% by mass, 70% by mass, or about 80% by mass.
本発明に係る医薬組成物を投与する対象としては、制限はされないが、疲労感を感じているヒトが好適である。疲労感は若干感じる程度でも強く感じる程度であってもよい。またさらに、近い将来に肉体的及び／又は精神的疲労を生じることが予測される場合に、予防的に用いることもできる。 The subject to which the pharmaceutical composition according to the present invention is administered is not limited, but a human who feels tired is preferable. The feeling of fatigue may be slightly felt or strongly felt. Furthermore, it can also be used prophylactically when it is predicted that physical and / or mental fatigue will occur in the near future.
さらには、本発明に係る医薬組成物を投与する対象には、ヒトのみならず、非ヒト哺乳動物も含まれる。疲労を示す哺乳動物が例示でき、特にペット及び家畜として飼育される哺乳動物が好ましい。具体的には、イヌ、ネコ、サル、ウシ、ウマ、ヒツジ、ヤギ、ブタ、ウサギ、マウス、ラット、ラクダ、リャマ等が例示できる。哺乳動物の場合も、人の場合と同様、本発明に係る医薬組成物を予防的に用いることもできる。 Furthermore, the subject to which the pharmaceutical composition according to the present invention is administered includes not only humans but also non-human mammals. Mammals exhibiting fatigue can be exemplified, and mammals bred as pets and livestock are particularly preferable. Specific examples thereof include dogs, cats, monkeys, cows, horses, sheep, goats, pigs, rabbits, mice, rats, camels, and llamas. In the case of mammals as well as in the case of humans, the pharmaceutical composition according to the present invention can be used prophylactically.
本発明に係る医薬組成物の投与時期は特に限定されず、例えば製剤形態、投与対象の年齢、投与対象の症状の程度等を考慮して適宜投与時期を選択することが可能である。なお、投与形態は経口投与である。 The administration time of the pharmaceutical composition according to the present invention is not particularly limited, and it is possible to appropriately select the administration time in consideration of, for example, the formulation form, the age of the administration target, the degree of symptoms of the administration target, and the like. The administration form is oral administration.
本発明に係る医薬組成物の投与量は、投与対象の年齢、投与対象の症状の程度、その他の条件等に応じて適宜選択され得る。特に含まれるセラミド量を基準として、本発明の効果が損なわれない範囲で適宜設定することができる。なお、１日１回又は複数回（好ましくは２〜３回）に分けて投与することができる。哺乳動物の場合も、当該人の場合を参考として適宜投与量を設定できる。 The dose of the pharmaceutical composition according to the present invention can be appropriately selected depending on the age of the subject to be administered, the degree of symptoms of the subject to be administered, other conditions and the like. In particular, the amount of ceramide contained can be appropriately set as a reference within a range in which the effects of the present invention are not impaired. In addition, it can be administered once a day or divided into a plurality of times (preferably 2 to 3 times). In the case of mammals as well, the dose can be appropriately set with reference to the case of the person concerned.
本発明に係る抗疲労経口組成物を食品組成物（例えば飲食品や食品添加物）として用いる場合、当該組成物（以下「本発明に係る食品組成物」と記載することがある）は、セラミド、及び食品衛生学上許容される基剤、担体、添加剤、その他飲食品として利用され得る成分・材料等が適宜配合されたものである。例えば、セラミドを含む、疲労改善用若しくは予防用の加工食品、飲料、健康食品（栄養機能食品、特定保健用食品等）、サプリメント、病者用食品（病院食、病人食又は介護食等）等の食品組成物が例示できる。特に制限はされないが、当該食品組成物に配合されるセラミドが生物（特に動物又は植物）組織から抽出された生体組織抽出セラミドである場合は、例えば当該セラミドが配合された加工食品、健康食品（栄養機能食品、特定保健用食品等）、サプリメント、病者用食品等であることが好ましい。また、セラミドを例えば粉末状にする等して、飲料類（ジュース等）、菓子類、パン類、スープ類（粉末スープ等を含む）、加工食品等の各種飲食品に含有させたものであってもよい。 When the anti-fatigue oral composition according to the present invention is used as a food composition (for example, food or drink or food additive), the composition (hereinafter, may be referred to as “food composition according to the present invention”) is ceramide. , And bases, carriers, additives, and other ingredients / materials that can be used as foods and drinks, which are permitted in terms of food hygiene, are appropriately blended. For example, processed foods for improving or preventing fatigue, beverages, health foods (foods with nutritional function, foods for specified health use, etc.), supplements, foods for the sick (hospital foods, sick foods, nursing foods, etc.) containing ceramide, etc. The food composition of the above can be exemplified. Although not particularly limited, when the ceramide contained in the food composition is a biological tissue-extracted ceramide extracted from a biological (particularly animal or plant) tissue, for example, a processed food or a health food containing the ceramide ( Foods with nutritional function, foods for specified health use, etc.), supplements, foods for the sick, etc. are preferable. In addition, ceramide is powdered, for example, and contained in various foods and drinks such as beverages (juice, etc.), confectionery, breads, soups (including powdered soup, etc.), processed foods, etc. You may.
なお、健康食品（栄養機能食品、特定保健用食品等）、サプリメントとして、本発明に係る食品組成物を調製する場合は、継続的な摂取が行いやすいように、例えば顆粒、カプセル、錠剤（チュアブル剤等を含む）、飲料（ドリンク剤）等の形態に調製することが好ましく、なかでもカプセル、タブレット、錠剤の形態が摂取の簡便さの点からは好ましいが、特にこれらに限定されるものではない。顆粒、カプセル、錠剤等の形態の、本発明に係る食品組成物は、薬学的及び／又は食品衛生学的に許容される担体等を用いて、常法に従って適宜調製することができる。また、他の形態に調製する場合であっても、従来の方法に従えばよい。 When preparing a food composition according to the present invention as a health food (food with nutritional function, food for specified health use, etc.) or supplement, for example, granules, capsules, tablets (chewable) so as to facilitate continuous ingestion. It is preferable to prepare in the form of (including agents), beverages (drinks), etc. Among them, the forms of capsules, tablets, and tablets are preferable from the viewpoint of ease of ingestion, but are not particularly limited thereto. Absent. The food composition according to the present invention in the form of granules, capsules, tablets and the like can be appropriately prepared according to a conventional method using a carrier or the like which is pharmaceutically and / or food hygiene acceptable. Further, even when the preparation is made into another form, the conventional method may be followed.
本発明に係る食品組成物におけるセラミドの配合量は、抗疲労効果が発揮され得る限り特に制限されない。、好ましくは０．０００５〜１００質量％、より好ましくは０．００５〜９０質量％、さらに好ましくは０．０５〜８０質量％である。なお、下限は１０質量％、２０質量％、３０質量％、４０質量％、５０質量％、６０質量％、７０質量％、又は８０質量％程度であってもよい。 The blending amount of ceramide in the food composition according to the present invention is not particularly limited as long as the anti-fatigue effect can be exhibited. It is preferably 0.0005 to 100% by mass, more preferably 0.005 to 90% by mass, and further preferably 0.05 to 80% by mass. The lower limit may be about 10% by mass, 20% by mass, 30% by mass, 40% by mass, 50% by mass, 60% by mass, 70% by mass, or about 80% by mass.
本発明に係る食品組成物は、疲労症状改善又は予防のために好ましく用いることができる。また、摂取量、摂取対象等は、例えば上述した本発明に係る医薬組成物と同様であることが好ましい。 The food composition according to the present invention can be preferably used for improving or preventing fatigue symptoms. Moreover, it is preferable that the intake amount, the intake target, etc. are the same as those of the above-mentioned pharmaceutical composition according to the present invention.
なお、病院食とは病院に入院した際に供される食事であり、病人食は病人用の食事であり、介護食とは被介護者用の食事である。本発明に係る食品組成物は、特に入院、自宅療養等されている患者、あるいは介護を受けられている患者であって疲労を感じている対象者用の病院食、病人食又は介護食として好ましく用いることができる。また、近い将来に肉体的及び／又は精神的疲労を生じることが予測される場合に、予防的に用いることもできる。 The hospital food is a meal provided when the patient is admitted to the hospital, the sick person's meal is a meal for the sick, and the care food is a meal for the care recipient. The food composition according to the present invention is particularly preferable as a hospital food, a sick person's food, or a nursing food for a patient who is hospitalized, is receiving medical treatment at home, or is receiving care and is feeling tired. Can be used. It can also be used prophylactically when it is predicted that physical and / or mental fatigue will occur in the near future.
本発明はまた、セラミドを含む経口セラミド組成物も包含する。当該経口セラミド組成物は、上記のセラミドを含む抗疲労経口組成物をも包含する。換言すれば、上記抗疲労経口組成物は、当該経口セラミド組成物の好ましい一態様であって、特に抗疲労という用途に用いるものであるといえる。 The present invention also includes an oral ceramide composition comprising a ceramide. The oral ceramide composition also includes an anti-fatigue oral composition containing the above-mentioned ceramide. In other words, it can be said that the anti-fatigue oral composition is a preferred embodiment of the oral ceramide composition, and is particularly used for anti-fatigue applications.
本発明に係る経口セラミド組成物において、含まれるセラミド種、その他成分等については、上記の抗疲労経口組成物についてのそれらと同様である。ただし、投与対象としては特に制限されない。抗疲労効果を必要とする対象のみならず、例えば、肌機能改善効果を必要とする対象等も包含される。 The ceramide species and other components contained in the oral ceramide composition according to the present invention are the same as those for the above-mentioned anti-fatigue oral composition. However, the administration target is not particularly limited. It includes not only subjects that require an anti-fatigue effect, but also subjects that require a skin function improving effect, for example.
本発明に係る経口セラミド組成物に含まれるセラミド種としてはフリーセラミドが好ましく、中でも好ましいのは、ｔ１８：０−２２：０ｈ、ｔ１８：１−２２：０ｈ、ｔ１８：０−２３：０ｈ、ｔ１８：１−２３：０ｈ、ｔ１８：０−２４：０ｈ、ｔ１８：１−２４：０ｈ、ｔ２０：０−２４：０ｈ、ｔ１８：１−２６：０ｈ、ｔ１８：０−２５：０ｈ、及びｔ１８：０−２４：０ｈ２等であり、特にｔ１８：０−２４：０ｈ、ｔ１８：１−２４：０ｈ、及びｔ２０：０−２４：０ｈが好ましい。また、少なくともフリーセラミドとしてｔ１８：０−２４：０ｈ、ｔ１８：１−２４：０ｈ、及びｔ２０：０−２４：０ｈが含まれることが好ましく、当該組成物に含まれるフリーセラミド全量に対して、ｔ１８：０−２４：０ｈ、ｔ１８：１−２４：０ｈ、及びｔ２０：０−２４：０ｈの合計量が３０質量％、４０質量％、又は５０質量％以上となることがより好ましい。Free ceramide is preferable as the ceramide species contained in the oral ceramide composition according to the present invention, and among them, t18: 0-22: 0h, t18: 1-22: 0h, t18: 0-23: 0h, t18 are preferable. : 1-23: 0h, t18: 0-24: 0h, t18: 1-24: 0h, t20: 0-24: 0h, t18: 1-26: 0h, t18: 0-25: 0h, and t18: 0-24: a 0h 2 etc., particularly t18: 0-24: 0h, t18: 1-24: 0h, and t20: 0-24: 0h is preferred. Further, it is preferable that at least t18: 0-24: 0h, t18: 1-24: 0h, and t20: 0-24: 0h are contained as free ceramides, and the total amount of free ceramides contained in the composition is more. It is more preferable that the total amount of t18: 0-24: 0h, t18: 1-24: 0h, and t20: 0-24: 0h is 30% by mass, 40% by mass, or 50% by mass or more.
上記特定のフリーセラミド種を含有することにより、本発明に係る経口セラミド組成物は、特に腸管吸収性及び血中移行性に優れる。よって、これら特定のフリーセラミド種を含有する経口組成物は、他のセラミドと比べ、経口摂取時に速効性が高いと考えられる。また、公知のセラミドの効果についても、他のセラミドに比べて、経口摂取時に得られる効果は高いと考えられる。 By containing the above-mentioned specific free ceramide species, the oral ceramide composition according to the present invention is particularly excellent in intestinal absorption and blood transferability. Therefore, it is considered that the oral composition containing these specific free ceramide species has a higher immediate effect when ingested as compared with other ceramides. In addition, regarding the effects of known ceramides, it is considered that the effects obtained by oral ingestion are higher than those of other ceramides.
なお、本明細書において「含む」とは、「本質的にからなる」と、「からなる」をも包含する（The term "comprising" includes "consisting essentially of” and "consisting of."）。 In addition, in this specification, "including" also includes "consisting essentially" and "consisting of" (The term "comprising" includes "consisting essentially of" and "consisting of.").
以下、本発明をより具体的に説明するが、本発明は下記の例に限定されるものではない。
セラミド組成物の調製
特開２０１２−１２６９１０号公報に記載の方法を参考に、醤油の搾り粕をエタノール抽出し、溶媒分画して高純度フリーセラミドを精製して、セラミド組成物を得た。Hereinafter, the present invention will be described in more detail, but the present invention is not limited to the following examples.
Preparation of ceramide composition With reference to the method described in Japanese Patent Application Laid-Open No. 2012-126910, soy sauce pomace was extracted with ethanol and fractionated with a solvent to purify high-purity free ceramide to obtain a ceramide composition.
より具体的には、次のようにして当該調製を行った。すなわち、常法により製造された醤油の副産物である圧搾粕の乾燥物についてエタノール抽出を行い、得られた抽出物をエタノール及び水を用いて固液分離して固形部を得た。さらに当該固形部をアセトン、エタノール、及び水で洗浄し、乾燥及び粉砕してさらに水、アセトン、及びヘキサンで洗浄したのち、再度エタノール抽出して得られた固形部をセラミド組成物として得た。 More specifically, the preparation was carried out as follows. That is, ethanol extraction was performed on the dried product of pressed lees, which is a by-product of soy sauce produced by a conventional method, and the obtained extract was solid-liquid separated using ethanol and water to obtain a solid portion. Further, the solid portion was washed with acetone, ethanol and water, dried and pulverized, further washed with water, acetone and hexane, and then ethanol-extracted again to obtain a solid portion obtained as a ceramide composition.
セラミド組成物の経口摂取による抗疲労効果検討１
１カプセル当たり、セラミド組成物２ｍｇ又は１０ｍｇを含むサプリメントカプセルを調製した。具体的には、乳糖とセラミド組成物を混合した後、当該混合物をプルランハードカプセルに充填してサプリメントカプセルを調製した。また、セラミド組成物を含まないカプセル（乳糖のみを充填）も調製した。 Examination of anti-fatigue effect by oral ingestion of
Supplement capsules containing 2 mg or 10 mg of ceramide composition per capsule were prepared. Specifically, after mixing lactose and a ceramide composition, the mixture was filled into pullulan hard capsules to prepare supplement capsules. In addition, capsules containing no ceramide composition (filled with lactose only) were also prepared.
健康な成人４０人を、プラセボ群１３人、低用量群１４人、高用量群１３人に群分けし、プラセボ群にはセラミド組成物非含有カプセルを、低用量群にはセラミド組成物２ｍｇ含有カプセルを、高用量群にはセラミド組成物１０ｍｇ含有カプセルを、それぞれ１日１カプセルずつ、２８日間摂取させた（二重盲検法）。当該摂取開始前及び摂取後において、ＰＯＭＳ（Ｐｒｏｆｉｌｅ ｏｆ Ｍｏｏｄ Ｓｔａｔｅｓ）を用いて気分尺度アンケートをとった。「体が疲れやすい」か、及び「全身がだるい」か、について評価した。ＰＯＭＳにおけるこれらの項目は、５段階評価アンケートに回答してもらう形式であり、各群における回答の平均値を解析した結果を、図１及び図２に示す。 Forty healthy adults were divided into 13 placebo groups, 14 low-dose groups, and 13 high-dose groups. The placebo group contained capsules free of ceramide composition, and the low-dose group contained 2 mg of ceramide composition. Capsules and capsules containing 10 mg of ceramide composition in the high dose group were ingested one capsule daily for 28 days (double-blind method). A mood scale questionnaire was taken using POMS (Profile of Mood States) before and after the ingestion. We evaluated whether "the body is easily tired" and "the whole body is tired". These items in POMS are in the form of having them answer a 5-grade evaluation questionnaire, and the results of analyzing the average value of the answers in each group are shown in FIGS. 1 and 2.
当該結果から、セラミド組成物を経口摂取することにより、抗疲労効果が得られることがわかった。 From the results, it was found that an anti-fatigue effect can be obtained by ingesting the ceramide composition orally.
セラミド組成物のＬＣ−ＭＳによる組成分析
セラミド組成物をＬＣ−ＭＳ（高速液体クロマトグラフ質量分析計）にて解析し、当該セラミド組成物に含まれる各種フリーセラミド種について分析した。当該分析から解った、当該セラミド組成物における各種フリーセラミド種の含有割合（質量％）について、図３に示す。ｔ１８：０−２４：０ｈ、ｔ１８：１−２４：０ｈ、及びｔ２０：０−２４：０ｈの３種のフリーセラミド種で、当該セラミド組成物の５０質量％以上を占めていた。また、その他にもフリーセラミドが含まれることがわかった。 Composition analysis of ceramide composition by LC-MS The ceramide composition was analyzed by LC-MS (High Performance Liquid Chromatograph Mass Spectrometer), and various free ceramide species contained in the ceramide composition were analyzed. The content ratio (mass%) of various free ceramide species in the ceramide composition found from the analysis is shown in FIG. Three types of free ceramide species, t18: 0-24: 0h, t18: 1-24: 0h, and t20: 0-24: 0h, accounted for 50% by mass or more of the ceramide composition. In addition, it was found that free ceramide was also contained.
セラミド組成物の経口摂取による肌への影響の検討
ヘアレスマウス（雌、７週齢）を用いて、セラミド組成物の経口摂取による肌への影響を検討した。食餌にセラミド組成物を０．１重量％配合して、ヘアレスマウス（ｎ＝５）に２週間与えた。同様に、食餌にトウモロコシ由来植物グルコシルセラミド（長良サイエンス株式会社）を０．１重量％配合して、ヘアレスマウス（ｎ＝５）に２週間与えた。また、通常の食餌を２週間与えたヘアレスマウス（ｎ＝５）をコントロールとした。 Examination of the effect of oral ingestion of ceramide composition on the skin Using hairless mice (female, 7 weeks old), the effect of oral ingestion of ceramide composition on the skin was examined. The diet was mixed with 0.1% by weight of the ceramide composition and fed to hairless mice (n = 5) for 2 weeks. Similarly, 0.1% by weight of corn-derived plant glucosylceramide (Nagara Science Co., Ltd.) was added to the diet and fed to hairless mice (n = 5) for 2 weeks. In addition, hairless mice (n = 5) fed a normal diet for 2 weeks were used as controls.
この検討期間、検討初日、７日目、１１日目、及び１４日目に、各ヘアレスマウスの経皮水分蒸散量（ＴＥＷＬ）をＴｅｗａｍｅｔｅｒ（Ｃｏｕｒａｇｅ＋Ｋｈａｚａｋａ社製）を用いて測定した。結果を図４に示す。図４では、セラミド組成物は「セラミド」、トウモロコシ由来植物グルコシルセラミドは「グルコシルセラミド」と、表す。 During this study period, on the first day, the seventh day, the eleventh day, and the fourteenth day of the study, the transepidermal water loss (TEWL) of each hairless mouse was measured using a Tewameter (manufactured by Course + Khazaka). The results are shown in FIG. In FIG. 4, the ceramide composition is represented as "ceramide", and the corn-derived plant glucosylceramide is represented as "glucosylceramide".
当該結果から、用いたセラミド組成物からは経口摂取により経皮水分蒸散量（ＴＥＷＬ）改善効果が得られること、及びその効果は、植物由来セラミド（トウモロコシ由来植物グルコシルセラミド）に比べて高いこと、が分かった。 From the results, it was found that the ceramide composition used had an effect of improving transepidermal water loss (TEWL) by oral ingestion, and that the effect was higher than that of plant-derived ceramide (corn-derived plant glucosylceramide). I understood.
セラミド組成物の腸管からの吸収効率の検討
ＩＣＲマウスにセラミド組成物３ｍｇを経口投与し、投与３時間後に採血して、血漿中に存在する各フリーセラミド種をＬＣ−ＭＳにより解析した。セラミド組成物を投与していないＩＣＲマウスからも血液を採取して同様の解析を行った。結果を図５に示す。図５において、セラミド組成物は「ＷＳＳ」と表記される。また、黄色マーカーが付されたフリーセラミド種は、ＭＳ／ＭＳで確認を行ったものを示す（それ以外のフリーセラミド種は分子イオンから推定したものである）。投与したセラミド組成物と類似した分子種が血液中から多く検出されており、投与３時間後という短時間後の解析結果であることをふまえると、投与した各フリーセラミド種は、そのまま腸管から吸収されている可能性が示唆された。また、仮に腸管吸収前に一度分解され、吸収後に再合成されていると考えても、投与した各フリーセラミド種が血中に素早く取り込まれることに変わりはない。従って、用いたセラミド組成物に含まれる各フリーセラミド、中でもｔ１８：０−２４：０ｈ、ｔ１８：１−２４：０ｈ、及びｔ２０：０−２４：０ｈの３種は特に腸管吸収性及び血中移行性に優れていることがわかった。このことから、これら特定のフリーセラミド種を含有する組成物については、セラミドの中でも経口摂取時に速効性が高いことが示唆された。 Examination of absorption efficiency of ceramide composition from
セラミド組成物の経口摂取による抗疲労効果検討２
１カプセル当たり、セラミド組成物２ｍｇを含むサプリメントカプセルを調製した。具体的には、デキストランとセラミド組成物を混合した後、プルランハードカプセルに充填してサプリメントカプセルを調製した。また、セラミド組成物を含まないカプセル（デキストランのみ充填）も調製した。
健康な成人４０人を、プラセボ群１９人、セラミド群２０人に群分けし、プラセボ群にはセラミド組成物非含有カプセルを、セラミド群にはセラミド組成物２ｍｇ含有カプセルを、それぞれ１日１カプセルずつ、８４日間摂取させた（二重盲検法）。当該摂取開始前及び摂取後において、気分尺度アンケート（ＳＤ法（Semantic Differential Technique）による）、ＣＦＳ（Ｃａｎｃｅｒ Ｆａｔｉｇｕｅ Ｓｃａｌｅ：がん患者の倦怠感を評価する質問票）、及びＰＯＭＳ（Ｐｒｏｆｉｌｅ ｏｆ Ｍｏｏｄ Ｓｔａｔｅｓ）による評価を行った。具体的には、気分尺度アンケートでは１６問、ＣＦＳでは１５問、ＰＯＭＳでは３０問の項目を有するアンケートについて、被験者に回答してもらい、集計した。以下に各アンケートの特定のアンケート項目及び評価結果について記載する。 Examination of anti-fatigue effect by oral ingestion of
Supplement capsules containing 2 mg of ceramide composition per capsule were prepared. Specifically, after mixing dextran and a ceramide composition, pullulan hard capsules were filled to prepare supplement capsules. In addition, capsules containing no ceramide composition (filled with dextran only) were also prepared.
Forty healthy adults were divided into 19 placebo groups and 20 ceramide groups, with the placebo group containing ceramide composition-free capsules and the ceramide group containing 2 mg ceramide composition capsules, one capsule per day. They were ingested for 84 days each (double-blind method). Before and after the ingestion, a mood scale questionnaire (using the SD method (Semantic Differential Technique)), CFS (Cancer Fatigue Scale), and POMS (Profile of Mood States). Was evaluated by. Specifically, the subjects were asked to answer a questionnaire having 16 questions in the mood scale questionnaire, 15 questions in the CFS, and 30 questions in the POMS, and totaled. The specific questionnaire items and evaluation results of each questionnaire are described below.
気分尺度アンケート項目「昼間の眠気が強い」及び「多忙感」、ＣＦＳアンケート項目「横になっていたいと感じますか」、「ぐったりと感じますか」、及び「身体がだるいと感じますか」、並びにＰＯＭＳアンケート項目「緊張する」、「積極的な気分だ」、「元気がいっぱいだ」、「活気がわいてくる」、「疲れた」、及び「だるい」、についての回答を集計し評価した。なお、これら項目のアンケートは、次の５段階又は４段階のいずれに当てはまるかを選択してもらう形式で行った。
気分尺度アンケート（「昼間の眠気が強い」）：「全くあてはまらない」１点、「わずかにあてはまる」２点、「少しあてはまる」３点、「かなりあてはまる」４点、「非常にあてはまる」５点
気分尺度アンケート（「多忙感」）：「全く忙しくない」１点、「さほど忙しくない」２点、「忙しい」３点、「大変忙しい」４点
ＣＦＳアンケート：「いいえ」１点、「少し」２点、「まあまあ」３点、「かなり」４点、「とても」５点
ＰＯＭＳアンケート：「まったくなかった」１点、「すこしあった」２点、「まあまああった」３点、「かなりあった」４点、「非常に多くあった」５点Mood scale questionnaire items "daytime sleepiness" and "busy feeling", CFS questionnaire items "do you want to lie down", "do you feel tired", and "do you feel tired", In addition, the answers to the POMS questionnaire items "tense", "active mood", "full of energy", "lively", "tired", and "dull" were aggregated and evaluated. .. In addition, the questionnaire of these items was conducted in a format in which the applicant was asked to select which of the following 5 stages or 4 stages was applicable.
Mood Scale Questionnaire ("Daytime sleepiness"): "Not at all" 1 point, "Slightly applicable" 2 points, "Slightly applicable" 3 points, "Quite applicable" 4 points, "Very applicable" 5 points Mood scale questionnaire ("busy"): "not busy at all" 1 point, "not very busy" 2 points, "busy" 3 points, "very busy" 4 points CFS questionnaire: "no" 1 point, "a little" 2 points, "OK" 3 points, "Quite" 4 points, "Very" 5 points POMS questionnaire: "Not at all" 1 point, "Slightly met" 2 points, "OK" 3 points, "Okay""There was quite a lot" 4 points, "There was a lot" 5 points
各項目のプラセボ群及びセラミド群における回答を解析した結果を図７〜１７に示す。なお、これらの図ではセラミド群は２ｍｇ群と表記する。また、摂取開始前及び摂取後をそれぞれ事前及び事後と表記する。 The results of analyzing the responses of each item in the placebo group and the ceramide group are shown in FIGS. 7 to 17. In these figures, the ceramide group is referred to as the 2 mg group. In addition, before and after the start of ingestion are referred to as pre- and post-ingestion, respectively.
図７〜１７に示すように、上記アンケート項目全てにおいて、摂取開始前と摂取後とでは、プラセボ群では有意差はなかったが、セラミド群では有意差があった。当該結果からも、セラミド組成物を経口摂取することにより、抗疲労効果が得られることが確認できた。
As shown in FIGS. 7 to 17, in all the above questionnaire items, there was no significant difference between the placebo group before the start of ingestion and after the ingestion, but there was a significant difference in the ceramide group. From the results, it was confirmed that the anti-fatigue effect can be obtained by ingesting the ceramide composition orally.
Claims (10)
からなる群より選択される少なくとも１種のフリーセラミドを含む、
請求項２に記載の抗疲労経口組成物。The ceramide skeleton is (a sphingoid base having 3 hydroxyl groups, 18 carbon atoms and 0 or 1 carbon-carbon double bond)-(22 to 26 carbon atoms, 0 carbon-carbon double bond, hydroxyl group. Free ceramide, which is a combination of (fatty acid having 0, 1, or 2), and ceramide skeleton (sphingoid base having 3 hydroxyl groups, 20 carbon atoms, and no intercarbon double bond). Free ceramide, which is a combination of-(fatty acid having 24 or 25 carbon atoms, 0 carbon-carbon double bond, 0, 1 or 2 hydroxyl groups).
Containing at least one free ceramide selected from the group consisting of
The anti-fatigue oral composition according to claim 2.
ｔ１８：１−２２：０ｈ、
ｔ１８：０−２３：０ｈ、
ｔ１８：１−２３：０ｈ、
ｔ１８：０−２４：０ｈ、
ｔ１８：１−２４：０ｈ、
ｔ２０：０−２４：０ｈ、
ｔ１８：１−２６：０ｈ、
ｔ１８：０−２５：０ｈ、及び
ｔ１８：０−２４：０ｈ２
からなる群より選択される少なくとも１種のフリーセラミドを含む、
請求項３に記載の抗疲労経口組成物。t18: 0-22: 0h,
t18: 1-22: 0h,
t18: 0-23: 0h,
t18: 1-23: 0h,
t18: 0-24: 0h,
t18: 1-24: 0h,
t20: 0-24: 0h,
t18: 1-26: 0h,
t18: 0-25: 0h, and t18: 0-24: 0h 2
Containing at least one free ceramide selected from the group consisting of
The anti-fatigue oral composition according to claim 3.
請求項５に記載の抗疲労経口組成物。The total amount of t18: 0-24: 0h, t18: 1-24: 0h, and t20: 0-24: 0h is 30% by mass or more of the total amount of free ceramide contained.
The anti-fatigue oral composition according to claim 5.
ｔ１８：１−２２：０ｈ、
ｔ１８：０−２３：０ｈ、
ｔ１８：１−２３：０ｈ、
ｔ１８：０−２４：０ｈ、
ｔ１８：１−２４：０ｈ、
ｔ２０：０−２４：０ｈ、
ｔ１８：１−２６：０ｈ、
ｔ１８：０−２５：０ｈ、及び
ｔ１８：０−２４：０ｈ２
からなる群より選択される少なくとも１種のフリーセラミドを含む、経口セラミド組成物。t18: 0-22: 0h,
t18: 1-22: 0h,
t18: 0-23: 0h,
t18: 1-23: 0h,
t18: 0-24: 0h,
t18: 1-24: 0h,
t20: 0-24: 0h,
t18: 1-26: 0h,
t18: 0-25: 0h, and t18: 0-24: 0h 2
An oral ceramide composition comprising at least one free ceramide selected from the group consisting of.
請求項９に記載の経口セラミド組成物。 The total amount of t18: 0-24: 0h, t18: 1-24: 0h, and t20: 0-24: 0h is 30% by mass or more of the total amount of free ceramide contained.
The oral ceramide composition according to claim 9.
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| JP2004254632A (en) * | 2003-02-27 | 2004-09-16 | Fuji Oil Co Ltd | Food for beauty |
| JP2012126910A (en) * | 2010-07-23 | 2012-07-05 | Miyanabe Masakatsu | Sphingolipid derived from fermentation lees |
| JP2012180311A (en) * | 2011-03-02 | 2012-09-20 | Kao Corp | Endurance improver |
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| JP2004254632A (en) * | 2003-02-27 | 2004-09-16 | Fuji Oil Co Ltd | Food for beauty |
| JP2012126910A (en) * | 2010-07-23 | 2012-07-05 | Miyanabe Masakatsu | Sphingolipid derived from fermentation lees |
| JP2012180311A (en) * | 2011-03-02 | 2012-09-20 | Kao Corp | Endurance improver |
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| Title |
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| FRAGRANCE JOURNAL, vol. 41, no. 12, JPN6022028827, 2013, pages 44 - 49, ISSN: 0004823491 * |
| 福岡県リサイクル総合研究事業化センター成果発表会, JPN6022028831, 16 June 2016 (2016-06-16), pages 1 - 19, ISSN: 0004823490 * |
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