JP6332902B2 - Cosmetic composition - Google Patents
Cosmetic composition Download PDFInfo
- Publication number
- JP6332902B2 JP6332902B2 JP2012237787A JP2012237787A JP6332902B2 JP 6332902 B2 JP6332902 B2 JP 6332902B2 JP 2012237787 A JP2012237787 A JP 2012237787A JP 2012237787 A JP2012237787 A JP 2012237787A JP 6332902 B2 JP6332902 B2 JP 6332902B2
- Authority
- JP
- Japan
- Prior art keywords
- skin
- acid
- cosmetic
- uridine
- composition
- 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.)
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- 239000002537 cosmetic Substances 0.000 title claims description 26
- 239000000203 mixture Substances 0.000 title claims description 25
- DRTQHJPVMGBUCF-XVFCMESISA-N Uridine Chemical compound O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C=C1 DRTQHJPVMGBUCF-XVFCMESISA-N 0.000 claims description 20
- -1 purine nucleic acid Chemical group 0.000 claims description 19
- IAJILQKETJEXLJ-UHFFFAOYSA-N Galacturonsaeure Natural products O=CC(O)C(O)C(O)C(O)C(O)=O IAJILQKETJEXLJ-UHFFFAOYSA-N 0.000 claims description 16
- 229940097043 glucuronic acid Drugs 0.000 claims description 15
- OVRNDRQMDRJTHS-FMDGEEDCSA-N N-acetyl-beta-D-glucosamine Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O OVRNDRQMDRJTHS-FMDGEEDCSA-N 0.000 claims description 14
- 229950006780 n-acetylglucosamine Drugs 0.000 claims description 14
- 150000003839 salts Chemical class 0.000 claims description 14
- DUKURNFHYQXCJG-UHFFFAOYSA-N Lewis A pentasaccharide Natural products OC1C(O)C(O)C(C)OC1OC1C(OC2C(C(O)C(O)C(CO)O2)O)C(NC(C)=O)C(OC2C(C(OC3C(OC(O)C(O)C3O)CO)OC(CO)C2O)O)OC1CO DUKURNFHYQXCJG-UHFFFAOYSA-N 0.000 claims description 13
- DRTQHJPVMGBUCF-PSQAKQOGSA-N beta-L-uridine Natural products O[C@H]1[C@@H](O)[C@H](CO)O[C@@H]1N1C(=O)NC(=O)C=C1 DRTQHJPVMGBUCF-PSQAKQOGSA-N 0.000 claims description 10
- DRTQHJPVMGBUCF-UHFFFAOYSA-N uracil arabinoside Natural products OC1C(O)C(CO)OC1N1C(=O)NC(=O)C=C1 DRTQHJPVMGBUCF-UHFFFAOYSA-N 0.000 claims description 10
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- 238000002360 preparation method Methods 0.000 claims description 4
- 239000000126 substance Substances 0.000 claims description 3
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- UDMBCSSLTHHNCD-UHFFFAOYSA-N Coenzym Q(11) Natural products C1=NC=2C(N)=NC=NC=2N1C1OC(COP(O)(O)=O)C(O)C1O UDMBCSSLTHHNCD-UHFFFAOYSA-N 0.000 claims 1
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- UDMBCSSLTHHNCD-KQYNXXCUSA-N adenosine 5'-monophosphate Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](COP(O)(O)=O)[C@@H](O)[C@H]1O UDMBCSSLTHHNCD-KQYNXXCUSA-N 0.000 claims 1
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- 229910019142 PO4 Inorganic materials 0.000 description 4
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 4
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- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 3
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- 238000002156 mixing Methods 0.000 description 3
- 125000002347 octyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 3
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- 150000003904 phospholipids Chemical class 0.000 description 3
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- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 2
- WNWHHMBRJJOGFJ-UHFFFAOYSA-N 16-methylheptadecan-1-ol Chemical compound CC(C)CCCCCCCCCCCCCCCO WNWHHMBRJJOGFJ-UHFFFAOYSA-N 0.000 description 2
- XDOFQFKRPWOURC-UHFFFAOYSA-N 16-methylheptadecanoic acid Chemical compound CC(C)CCCCCCCCCCCCCCC(O)=O XDOFQFKRPWOURC-UHFFFAOYSA-N 0.000 description 2
- PYMYPHUHKUWMLA-UHFFFAOYSA-N 2,3,4,5-tetrahydroxypentanal Chemical compound OCC(O)C(O)C(O)C=O PYMYPHUHKUWMLA-UHFFFAOYSA-N 0.000 description 2
- KWIUHFFTVRNATP-UHFFFAOYSA-N Betaine Natural products C[N+](C)(C)CC([O-])=O KWIUHFFTVRNATP-UHFFFAOYSA-N 0.000 description 2
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- WNFHGZLVUQBPMA-JSCKKFHOSA-M Sodium glucuronate Chemical compound [Na+].O=C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)C([O-])=O WNFHGZLVUQBPMA-JSCKKFHOSA-M 0.000 description 2
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Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Coloring Foods And Improving Nutritive Qualities (AREA)
- Cosmetics (AREA)
Description
本発明は、角質層水分量を増大させハリのある肌を得るための、医薬、化粧品、食品に適用する好適な美容用組成物に関する。 The present invention relates to a cosmetic composition suitable for pharmaceuticals, cosmetics, and foods for increasing the stratum corneum moisture content and obtaining firm skin.
皮膚は外側から表皮、真皮、皮下組織からなっており、そのバリア機能により外界の刺激から生体を守る役割を有している。皮膚の真皮及び表皮は、表皮細胞、線維芽細胞、真皮細胞外マトリックス等によって構成されている。ヒアルロン酸は、コラーゲン、エラスチン等とともに真皮細胞外マトリックスを構成し、表皮細胞や線維芽細胞等の細胞の外にあって皮膚構造を支持している。若い皮膚では、これら皮膚組織の相互作用が恒常性を保つことによって、水分保持、柔軟性、弾力性等が確保され、外見的にもハリや艶がある状態が維持される。 The skin consists of the epidermis, dermis and subcutaneous tissue from the outside, and has a role of protecting the living body from external stimuli by its barrier function. The dermis and epidermis of the skin are composed of epidermal cells, fibroblasts, dermal extracellular matrix and the like. Hyaluronic acid forms a dermal extracellular matrix together with collagen, elastin and the like, and is outside of cells such as epidermis cells and fibroblasts and supports the skin structure. In the young skin, the interaction between these skin tissues maintains the homeostasis, so that moisture retention, flexibility, elasticity, etc. are ensured, and the appearance of elasticity and gloss is maintained.
表皮の最外層には、更に角質層が存在する。角質層は10〜20の層になった角質細胞からなる細胞が最後にたどりつく部分である。角質細胞内には、アミノ酸、尿素、乳酸等の天然保湿因子が存在し、これらが水と結合することで、水分を保持し、皮膚の柔軟性を保っている。角質層は、外側にいくほど、核のない死んだ細胞がみられるが、水分を保持し、乾燥を防ぐ働き等、角質層のバリア機能は肌の美しさに大きく関係している。 A stratum corneum further exists in the outermost layer of the epidermis. The stratum corneum is the part where cells consisting of stratum corneum in layers 10 to 20 arrive at the end. In keratinocytes, natural moisturizing factors such as amino acids, urea, and lactic acid are present, and these bind to water to retain moisture and maintain skin flexibility. As the stratum corneum goes to the outside, dead cells without nuclei are seen. However, the barrier function of the stratum corneum, such as the function of retaining moisture and preventing drying, is greatly related to the beauty of the skin.
しかしながら、角質層の水分量は、乾燥、紫外線等の外的要因や加齢、老化や内臓疾患、ストレス等の内的要因によって減少し、皮膚のバリア機能の低下をもたらし、肌荒れやドライスキン、各種皮膚炎を引き起こしているといわれている。そのため、化粧品分野や皮膚科の領域では、角質層水分量を維持する保湿剤の開発が不可欠である。 However, the amount of water in the stratum corneum decreases due to external factors such as dryness, ultraviolet rays, and internal factors such as aging, aging and visceral diseases, stress, etc., resulting in a decrease in the skin barrier function, rough skin and dry skin, It is said to cause various dermatitis. Therefore, it is indispensable to develop a moisturizing agent that maintains the stratum corneum moisture content in the cosmetics field and dermatological field.
従来より、ヒアルロン酸を配合した化粧品や食品を適用することにより、皮膚表面の保湿性を保つ方法がとられてきた。しかしながら、このヒアルロン酸は、N−アセチル−D−グルコサミンとD−グルクロン酸とからなる直鎖状の酸性ムコ多糖の一種であり、その高い分子量のため、特に外用剤とした場合、皮膚中に浸透することが困難である。そのため、ヒアルロン酸自体を配合した外用剤は皮膚表面における保湿効果を発揮するだけで、肌の状態の根本的改善は期待できない。そこで、アセチルグルコサミン、グルクロン酸等を化粧水に加え外用することが検討されているが(特許文献1〜3)、これらによる肌の保湿性の向上やハリの改善も未だ十分なものとは言えなかった。 Conventionally, a method of keeping the skin surface moisturized by applying a cosmetic or food containing hyaluronic acid has been used. However, this hyaluronic acid is a kind of linear acidic mucopolysaccharide composed of N-acetyl-D-glucosamine and D-glucuronic acid, and because of its high molecular weight, especially when it is used as an external preparation, Difficult to penetrate. Therefore, an external preparation containing hyaluronic acid itself only exhibits a moisturizing effect on the skin surface and cannot be expected to fundamentally improve the skin condition. Therefore, it has been studied to add acetylglucosamine, glucuronic acid, etc. to the skin lotion for external use (Patent Documents 1 to 3), but it can be said that the improvement of the moisture retention and the elasticity of the skin by these is still sufficient. There wasn't.
本発明は、上記事情に鑑みなされたもので、保湿性を改善し角質層水分量を増大させるとともに肌をハリのある状態に保つことを可能とする美容用組成物の提供を目的とする。 The present invention has been made in view of the above circumstances, and an object of the present invention is to provide a cosmetic composition capable of improving moisture retention, increasing the amount of moisture in the stratum corneum and keeping the skin firm.
本発明者らは、(A)ウリジン又はその誘導体と、(B)アセチルグルコサミン、グルクロン酸及びそれらの誘導体から選択されるいずれか一種以上の化合物とを含む組成物を医薬や化粧品や食品用途で使用すると、角質層水分量を増大させて保湿性の向上を図ることができ、美容用として好適であることを見出し、本発明を完成するに至った。具体的に、本発明は以下のようなものを提供する。 The inventors of the present invention provide a composition containing (A) uridine or a derivative thereof and (B) any one or more compounds selected from acetylglucosamine, glucuronic acid, and derivatives thereof for pharmaceutical, cosmetic, and food applications. When used, the moisture content of the stratum corneum can be increased to improve the moisture retention, and it has been found that it is suitable for cosmetic use, and the present invention has been completed. Specifically, the present invention provides the following.
(1)(A)ウリジン又はその誘導体と、(B)アセチルグルコサミン、グルクロン酸、グルクロン酸の塩、及び、それらの誘導体から選択される少なくとも1種と、を含むことを特徴とする美容用組成物。
(2)(A)ウリジン又はその誘導体と、(B1)アセチルグルコサミン又はその誘導体と、(B2)グルクロン酸、グルクロン酸の塩、及び、それらの誘導体から選択される少なくとも1種と、を含むことを特徴とする(1)に記載の美容用組成物。
(3)(A)成分は、ウリジンリン酸又はその塩であることを特徴とする(1)又は(2)に記載の美容用組成物。
(4)リポソーム内に封入されていることを特徴とする(1)に記載の美容用組成物。
(5)(1)〜(4)いずれかひとつ記載の美容用組成物を含むことを特徴とする、医薬、化粧品又は食品。
(1) A cosmetic composition comprising (A) uridine or a derivative thereof and (B) at least one selected from acetylglucosamine, glucuronic acid, a salt of glucuronic acid, and derivatives thereof. object.
(2) containing (A) uridine or a derivative thereof; (B1) acetylglucosamine or a derivative thereof; and (B2) glucuronic acid, a salt of glucuronic acid, and at least one selected from these derivatives. The cosmetic composition according to (1), characterized in that
(3) The cosmetic composition according to (1) or (2), wherein the component (A) is uridine phosphoric acid or a salt thereof.
(4) The cosmetic composition according to (1), which is encapsulated in a liposome.
(5) A medicine, cosmetic or food comprising the cosmetic composition according to any one of (1) to (4).
本発明によれば、保湿性を向上して角質層水分量を増大させるとともに肌のハリを保つことができ、美容用として好適に使用できる。 ADVANTAGE OF THE INVENTION According to this invention, moisture retention can be improved and the amount of stratum corneum moisture can be increased, and the firmness of the skin can be maintained, which can be suitably used for cosmetic purposes.
以下、本発明の実施形態について説明するが、本発明は、これらに何ら限定されるものではない。 Hereinafter, although embodiment of this invention is described, this invention is not limited to these at all.
本発明の美容用組成物は、(A)ウリジン又はその誘導体と、(B)アセチルグルコサミン、グルクロン酸、グルクロン酸の塩、及びそれらの誘導体から選択される少なくとも1種以上の化合物とを含む。 The cosmetic composition of the present invention comprises (A) uridine or a derivative thereof and (B) at least one compound selected from acetylglucosamine, glucuronic acid, a salt of glucuronic acid, and derivatives thereof.
ウリジンは、ピリミジンヌクレオシドの1つであって、ウラシルがリボース環にβ−N1−グリコシド結合で接続した構造をもつヌクレシドのひとつである。本発明において使用できるウリジンの誘導体としては、ウリジン一リン酸(ウリジル酸)、ウリジン二リン酸、ウリジン三リン酸等のウリジンのリン酸エステル類等、又は、その生理学的に許容される塩が挙げられる。塩としては、カリウム、ナトリウム等の金属塩が使用可能である。本発明の組成物には、これらのうち一種又は二種以上を併用してもよい。 Uridine is one of pyrimidine nucleosides and is one of nucleosides having a structure in which uracil is connected to the ribose ring by a β-N1-glycoside bond. Examples of uridine derivatives that can be used in the present invention include uridine phosphates such as uridine monophosphate (uridylic acid), uridine diphosphate, and uridine triphosphate, or physiologically acceptable salts thereof. Can be mentioned. As the salt, metal salts such as potassium and sodium can be used. You may use together 1 type, or 2 or more types among these in the composition of this invention.
組成物中の成分(A)の配合量は、成分(B)の角質層におけるヒアルロン酸量を増大する働きを助けるに十分であれば特に限定されないが、組成物総量を基準として、0.000001質量%以上とするのが好ましく、0.00001質量%以上とすることが更に好ましい。その上限は、10質量%以下とするのが好ましく、5質量%以下とすることが更に好ましい。また、成分(A)と(B)とのモル比は、1:2〜2:1の範囲で用いられることが好ましい。 The amount of component (A) in the composition is not particularly limited as long as it is sufficient to help increase the amount of hyaluronic acid in the stratum corneum of component (B), but is 0.000001 based on the total amount of the composition. It is preferable to set it as mass% or more, and it is still more preferable to set it as 0.00001 mass% or more. The upper limit is preferably 10% by mass or less, and more preferably 5% by mass or less. Moreover, it is preferable that the molar ratio of component (A) and (B) is used in the range of 1: 2 to 2: 1.
また、アセチルグルコサミンは、グルコースの2位ヒドロキシル基がアセチルアミノ基に置換された単糖である。合成物や発酵産物、カニ、えび等のキチン分解から得られる分解産物等いずれのものも使用可能であり、特に限定されるものではない。また、その誘導体としては、下記化学式(1)のようなものが挙げられる。
より具体的には、オクチル(2−アセトアミド−2−デオキシ)β−D−グルコピラノシド、2−アセトアミド−1,3,4,6−テトラ−O−アセチル−2−デオキシ−β−D−グルコピラノシド、2−アセトアミド−2−デオキシ−6−O−オクタノイル−α−D−グルコピラノース、オクチル(2−アセトアミド−2−デオキシ−6−O−オクタノイル)β−D−グルコピラノシド、ブチル(2−アセトアミド−2−デオキシ)β−D−グルコピラノシド、ペンチル(2−アセトアミド−2−デオキシ)β−D−グルコピラノシド、ラウリル(2−アセトアミド−2−デオキシ)β−D−グルコピラノシド、2−アセトアミド−2−デオキシ−6−O−パルミトイル−α−D−グルコピラノース、ゲラニル(2−アセトアミド−2−デオキシ)β−D−グルコピラノシド、エチル(2−アセトアミド−3,4,6−トリ−O−アセチル−2−デオキシ)β−D−グルコピラノシド、ペンチル(2−アセトアミド−3,4,6−トリ−O−アセチル−2−デオキシ)β−D−グルコピラノシド、オクチル(2−アセトアミド−3,4,6−トリ−O−アセチル−2−デオキシ)β−D−グルコピラノシド、ゲラニル(2−アセトアミド−3,4,6−トリ−O−アセチル−2−デオキシ)β−D−グルコピラノシド等が挙げられるが、これらに限られるものではない。また、これらは、二種以上を併用してもよい。 More specifically, octyl (2-acetamido-2-deoxy) β-D-glucopyranoside, 2-acetamido-1,3,4,6-tetra-O-acetyl-2-deoxy-β-D-glucopyranoside, 2-acetamido-2-deoxy-6-O-octanoyl-α-D-glucopyranose, octyl (2-acetamido-2-deoxy-6-O-octanoyl) β-D-glucopyranoside, butyl (2-acetamido-2 -Deoxy) β-D-glucopyranoside, pentyl (2-acetamido-2-deoxy) β-D-glucopyranoside, lauryl (2-acetamido-2-deoxy) β-D-glucopyranoside, 2-acetamido-2-deoxy-6 -O-palmitoyl-α-D-glucopyranose, geranyl (2-acetamido-2-deoxy ) Β-D-glucopyranoside, ethyl (2-acetamido-3,4,6-tri-O-acetyl-2-deoxy) β-D-glucopyranoside, pentyl (2-acetamido-3,4,6-tri-O) -Acetyl-2-deoxy) β-D-glucopyranoside, octyl (2-acetamido-3,4,6-tri-O-acetyl-2-deoxy) β-D-glucopyranoside, geranyl (2-acetamido-3,4 , 6-tri-O-acetyl-2-deoxy) β-D-glucopyranoside and the like, but are not limited thereto. Moreover, these may use 2 or more types together.
グルクロン酸は,炭素数6個のグルコースの骨格構造とC6位のカルボキシル基を持つ糖であり、代表的なウロン酸のひとつである。硝酸や強酸を使用し澱粉等からグルコース誘導体を選択的に酸化してカルボン酸に変換し、その酸化生成物を加水分解して得たものや、グルコースを微生物により直接グルクロン酸に変換したもの等、いずれのものも使用可能であり特に限定されるものではない。また、そのカリウム塩、ナトリウム塩、その他生理学的に許容される塩が使用可能である。更に、誘導体としては、グルクロノラクトン、グルクロノキシラン等が挙げられる。これらは、二種以上を併用してもよい。 Glucuronic acid is a sugar having a skeleton structure of glucose having 6 carbon atoms and a carboxyl group at the C6 position, and is one of typical uronic acids. A product obtained by selectively oxidizing glucose derivatives from starch, etc. using nitric acid or strong acid to convert them to carboxylic acids, hydrolyzing the oxidation products, or by converting glucose directly to glucuronic acid by microorganisms, etc. Any of these can be used and is not particularly limited. In addition, potassium salts, sodium salts, and other physiologically acceptable salts thereof can be used. Further, examples of the derivative include glucuronolactone, glucuronoxylan and the like. Two or more of these may be used in combination.
これらアセチルグルコサミン、グルクロン酸又はそれらの誘導体から選ばれる成分(B)の本発明の組成物への配合量は、肌のハリ、水分量を増大させるのに十分であれば特に限定されない。組成物総量を基準として、0.000001質量%以上とするのが好ましく、0.00001質量%以上とすることが更に好ましい。その上限は、10質量%以下とするのが好ましく、5質量%以下とすることが更に好ましい。 The amount of the component (B) selected from these acetylglucosamine, glucuronic acid or derivatives thereof to the composition of the present invention is not particularly limited as long as it is sufficient to increase the firmness and moisture content of the skin. Based on the total amount of the composition, it is preferably 0.000001% by mass or more, and more preferably 0.00001% by mass or more. The upper limit is preferably 10% by mass or less, and more preferably 5% by mass or less.
本発明の組成物は、アセチルグルコサミン又はその誘導体(B1)、あるいは、グルクロン酸及びその誘導体(B2)のいずれかを含有すればよいが、成分(B1)と成分(B2)とを併用することが好ましい。この場合、成分(B1)と成分(B2)との比は、モル比で、2:1〜1:2の範囲で用いられればよい。 The composition of the present invention may contain either acetylglucosamine or a derivative thereof (B1), or glucuronic acid and a derivative thereof (B2), but the component (B1) and the component (B2) are used in combination. Is preferred. In this case, the ratio of the component (B1) to the component (B2) may be a molar ratio in the range of 2: 1 to 1: 2.
本発明の組成物は、皮膚の角質層水分量を増大させて保湿性を向上するとともに、肌のハリの改善又は良好な肌の状態を保つことができる。本組成物は、医薬、化粧品又は食品に使用することができる。その形態も、目的に応じて任意に選択することができる。すなわち、錠剤、クリーム、軟膏、乳液、溶液、ゲル等の剤形やパック、ローション(化粧水)、パウダー、スティック等のさまざまな形態をとることが可能である。特に化粧品として用いる場合には、皮膚外用剤として用いることが使用しやすさの面から好ましい。 The composition of the present invention increases the moisture content of the stratum corneum of the skin to improve the moisture retention, and can improve the firmness of the skin or maintain a good skin state. The composition can be used in medicine, cosmetics or food. The form can also be arbitrarily selected according to the purpose. In other words, it can take various forms such as tablets, creams, ointments, emulsions, solutions, gels and the like, packs, lotions (skin lotions), powders, sticks, and the like. In particular, when used as a cosmetic, use as a skin external preparation is preferable from the viewpoint of ease of use.
本発明の組成物はそのままの形で医薬、化粧品、又は食品に加えてもよいが、マイクロカプセル中に封入した上で加えてもよい。例えば、リン脂質からなる数10〜数100nmの粒径の微小なカプセルである、リポソームを用いることが、上記成分の効果を最大限に引き出すために好ましい。 The composition of the present invention may be added as it is to a pharmaceutical, cosmetic, or food, but may be added after encapsulating in a microcapsule. For example, it is preferable to use liposome, which is a microcapsule made of phospholipid and having a particle size of several tens to several hundreds of nm, in order to maximize the effects of the above components.
リポソームとは、主にリン脂質から成る脂質二重層あるいは多重層であり、細胞膜に類似した構造を有し、従来より、化粧品分野では、美白、保湿、抗酸化効果を有する有効成分を肌へ届ける手段として有効成分をリポソームに内包させることがよく行われてきた。本発明の上記有効成分は、例えば、リポソームの内水相に取り込まれ、カプセル化される。 Liposomes are lipid bilayers or multilayers composed mainly of phospholipids, and have a structure similar to that of cell membranes. In the cosmetics field, traditionally, active ingredients with whitening, moisturizing and antioxidant effects have been delivered to the skin. As a means, it has been common to encapsulate active ingredients in liposomes. The above-mentioned active ingredient of the present invention is encapsulated in, for example, an internal aqueous phase of liposome.
本発明において、適用できるリポソームの製法としては、公知の種々の方法が特に限定されることなく採用できる。例えば、(1)脂質を有機溶媒に溶解し、溶媒を減圧除去して薄膜を形成した後、緩衝液等の水溶液を加えて振とう膨潤させ、更に機械的撹拌手段により薄膜をはがすことで調製する方法、(2)脂質をエーテル又はエタノール等の有機溶媒に溶解し、緩衝液等の水溶液中に注入した後、溶媒を除去することにより調製する方法、更に、機械的な方法として、(3)超音波処理による方法、(4)高圧ホモジナイザーや高速回転分散機による方法、(5)ポリカーボネイト製メンブランフィルターを用いた高圧ろ過による方法、(6)水相の上部に脂質を溶解させた油相を用意し、油相に液滴を導入し、遠心分離による力で液滴を水相に引きずり込む方法等が知られている。そのほかに、(7)脂質をエタノール等の水と相溶する有機溶媒に溶解した後、透析膜を介して水と置換する方法等が挙げられる。 In the present invention, various known methods can be adopted without particular limitation as applicable liposome production methods. For example, (1) prepared by dissolving lipid in an organic solvent, removing the solvent under reduced pressure to form a thin film, adding an aqueous solution such as a buffer solution to swell with shaking, and further peeling the thin film with a mechanical stirring means (2) A method in which a lipid is dissolved in an organic solvent such as ether or ethanol, poured into an aqueous solution such as a buffer solution, and then prepared by removing the solvent. Further, as a mechanical method, (3 ) Method by sonication, (4) Method by high-pressure homogenizer or high-speed rotary disperser, (5) Method by high-pressure filtration using polycarbonate membrane filter, (6) Oil phase with lipid dissolved in the upper part of water phase There is known a method in which a droplet is introduced into an oil phase, and the droplet is dragged into a water phase by a force of centrifugation. In addition, (7) a method in which lipid is dissolved in an organic solvent compatible with water, such as ethanol, and then replaced with water through a dialysis membrane.
医薬、化粧品又は食品として使用する場合、上述した成分を必須の構成成分とするほか、本発明の目的を損なわない範囲で他の成分、例えば、陰イオン性界面活性剤、両性界面活性剤、非イオン性界面活性剤、粘度調整剤、油剤、粉体(色素、樹脂、顔料等)、防腐剤、香料、保湿剤、生理活性成分、塩類、溶媒、酸化防止剤、キレート剤、パール化剤、中和剤、pH調整剤、酵素等の成分を適宜配合することができる。以下に配合成分の具体例を示すが、これらに限られるものではない。 When used as a medicine, cosmetics or food, the above-mentioned components are essential components, and other components such as an anionic surfactant, an amphoteric surfactant, Ionic surfactants, viscosity modifiers, oils, powders (dyes, resins, pigments, etc.), preservatives, fragrances, moisturizers, physiologically active ingredients, salts, solvents, antioxidants, chelating agents, pearling agents, Components such as a neutralizer, a pH adjuster, and an enzyme can be appropriately blended. Although the specific example of a mixing | blending component is shown below, it is not restricted to these.
上記陰イオン性界面活性剤としては、α−アシルスルホン酸塩、アルキルスルホン酸塩、アルキルアリルスルホン酸塩、アルキルナフタレンスルホン酸塩、アルキル硫酸塩、アルキルエーテル硫酸塩、アルキルアミド硫酸塩、ポリオキシエチレンアルキルエーテル硫酸塩、ポリオキシエチレンアルキルアミドエーテル硫酸塩、アルキルリン酸塩、アルキルアミドリン酸塩、アルキロイルアルキルタウリン塩、N−アシルアミノ酸塩、スルホコハク酸塩、パーフルオロアルキルリン酸エステル等が挙げられる。 Examples of the anionic surfactant include α-acyl sulfonate, alkyl sulfonate, alkyl allyl sulfonate, alkyl naphthalene sulfonate, alkyl sulfate, alkyl ether sulfate, alkyl amide sulfate, polyoxy Ethylene alkyl ether sulfate, polyoxyethylene alkylamide ether sulfate, alkyl phosphate, alkylamide phosphate, alkyloylalkyl taurate, N-acyl amino acid salt, sulfosuccinate, perfluoroalkyl phosphate, etc. Can be mentioned.
また、両性界面活性剤としては、グリシン型、アミノプロピオン酸型、カルボキシベタイン型、スルホベタイン型、スルホン酸型、硫酸型、リン酸型等が挙げられ、好適なものとして2−アルキル−N−カルボキシメチル−N−ヒドロキシエチルイミダゾリニウムベタイン、ヤシ油脂肪酸アミドプロピルベタイン等が例示できる。また、レシチン等のリン脂質を、リポソームを形成することを目的とする以外に使用することもできる。 Examples of amphoteric surfactants include glycine type, aminopropionic acid type, carboxybetaine type, sulfobetaine type, sulfonic acid type, sulfuric acid type, phosphoric acid type, and the like. 2-alkyl-N- is preferable. Examples thereof include carboxymethyl-N-hydroxyethylimidazolinium betaine, coconut oil fatty acid amidopropyl betaine and the like. Also, phospholipids such as lecithin can be used in addition to the purpose of forming liposomes.
非イオン性界面活性剤としては、脂肪酸アルカノールアミド、ポリオキシエチレン硬化ヒマシ油、ポリオキシエチレンソルビタン脂肪酸エステル、ポリオキシエチレンアルキルエーテル、ポリオキシエチレンアルキルエステル、ショ糖脂肪酸エステル、ポリグリセリン脂肪酸エステル、アルキルアミンオキシド等が挙げられる。 Nonionic surfactants include fatty acid alkanolamide, polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene alkyl ether, polyoxyethylene alkyl ester, sucrose fatty acid ester, polyglycerin fatty acid ester, alkyl An amine oxide etc. are mentioned.
粘度調整剤の例としては、アクリル酸アミド及びその誘導体、カルボキシビニルポリマー、アルキル変性カルボキシビニルポリマー、セルロース、ケラチン及びコラーゲン又はその誘導体、アルギン酸カルシウム、プルラン、寒天、ゼラチン、タマリンド種子多糖類、キサンタンガム、カラギーナン、ハイメトキシルペクチン、ローメトキシルペクチン、グァーガム、アラビアゴム、結晶セルロース、アラビノガラクタン、カラヤガム、トラガカントガム、アルギン酸、アルブミン、カゼイン、カードラン、ジェランガム、デキストラン等が挙げられる。 Examples of viscosity modifiers include acrylic amides and derivatives thereof, carboxyvinyl polymers, alkyl-modified carboxyvinyl polymers, cellulose, keratin and collagen or derivatives thereof, calcium alginate, pullulan, agar, gelatin, tamarind seed polysaccharide, xanthan gum, Carrageenan, high methoxyl pectin, low methoxyl pectin, guar gum, gum arabic, crystalline cellulose, arabinogalactan, caraya gum, tragacanth gum, alginic acid, albumin, casein, curdlan, gellan gum, dextran and the like.
油剤としては、通常化粧料に用いられる揮発性及び不揮発性の油剤、溶剤及び樹脂が挙げられ、常温で液体、ペースト、固体であっても構わない。油剤の例としては、例えばセチルアルコール、イソステアリルアルコール、ラウリルアルコール、ヘキサデシルアルコール、オクチルドデカノール等の高級アルコール、イソステアリン酸、ウンデシレン酸、オレイン酸等の脂肪酸、ミリスチン酸ミリスチル、ラウリン酸ヘキシル、ミリスチン酸オクチルドデシル、オレイン酸デシル、ミリスチン酸イソプロピル、ジメチルオクタン酸へキシルデシル、モノステアリン酸グリセリン、トリオクタン酸グリセリン、フタル酸ジエチル、モノステアリン酸エチレングリコール、オキシステアリン酸オクチル等のエステル類、ステアリン酸コレステリル、オレイン酸コレステリル、分岐脂肪酸コレステリル等のコレステロールエステル、流動パラフィン、ワセリン、スクワラン等の炭化水素、ラノリン、還元ラノリン、カルナバロウ等のロウ、ミンク油、カカオ脂、ヤシ油、パーム核油、ツバキ油、ゴマ油、ヒマシ油、オリーブ油等の油脂、ジメチルポリシロキサン、環状ジメチルポリシロキサン、メチルフェニルポリシロキサン等のシリコーン油等が挙げられる。 Examples of the oil agent include volatile and non-volatile oil agents, solvents, and resins that are usually used in cosmetics, and may be liquid, paste, or solid at room temperature. Examples of oils include higher alcohols such as cetyl alcohol, isostearyl alcohol, lauryl alcohol, hexadecyl alcohol, octyldodecanol, fatty acids such as isostearic acid, undecylenic acid, oleic acid, myristyl myristate, hexyl laurate, myristine Octyldodecyl acid, decyl oleate, isopropyl myristate, hexyl decyl dimethyloctanoate, glyceryl monostearate, glyceryl trioctanoate, diethyl phthalate, ethylene glycol monostearate, octyl oxystearate, cholesteryl stearate, Cholesterol esters such as cholesteryl oleate and branched fatty acid cholesteryl, hydrocarbons such as liquid paraffin, petroleum jelly and squalane, lanoli Waxes such as reduced lanolin, carnauba wax, mink oil, cacao butter, palm oil, palm kernel oil, camellia oil, sesame oil, castor oil, olive oil, dimethylpolysiloxane, cyclic dimethylpolysiloxane, methylphenylpolysiloxane, etc. Silicone oil etc. are mentioned.
粉体の例としては、赤色201号、黄色4号、青色1号、黒色401号等の色素、黄色4号Alレーキ、黄色203号Baレーキ等のレーキ色素、ナイロンパウダー、シルクパウダー、シリコーンパウダー、セルロースパウダー、シリコーンエラストマー球状粉体、ポリエチレン末等の樹脂、黄酸化鉄、赤色酸化鉄、酸化クロム、カーボンブラック、群青、紺青等の有色顔料、酸化亜鉛、酸化チタン等の白色顔料、タルク、マイカ、セリサイト、カオリン等の体質顔料、雲母チタン等のパール顔料の顔料、硫酸バリウム、炭酸カルシウム、炭酸マグネシウム、珪酸マグネシウム等の金属塩、シリカ、アルミナ等の無機粉体、ベントナイト、スメクタイト、窒化ホウ素等が挙げられる。これらの粉体の形状(球状、棒状、針状、板状、不定形状、燐片状、紡錘状等)に特に制限はない。 Examples of powders include red No. 201, yellow No. 4, blue No. 1, black No. 401 and other dyes, yellow No. 4 Al lake, yellow No. 203 Ba lake and other lake dyes, nylon powder, silk powder and silicone powder. , Cellulose powder, silicone elastomer spherical powder, resin such as polyethylene powder, yellow iron oxide, red iron oxide, chromium oxide, carbon black, colored pigments such as ultramarine and bitumen, white pigments such as zinc oxide and titanium oxide, talc, Body pigments such as mica, sericite, kaolin, pearl pigments such as titanium mica, metal salts such as barium sulfate, calcium carbonate, magnesium carbonate, magnesium silicate, inorganic powders such as silica and alumina, bentonite, smectite, nitriding Boron etc. are mentioned. There are no particular restrictions on the shape of these powders (spherical, rod-like, needle-like, plate-like, indeterminate, flake-like, spindle-like, etc.).
生理活性成分としては、皮膚に塗布した場合に皮膚に何らかの生理活性を与える物質が挙げられる。例えば、老化防止剤、紫外線防御剤、ひきしめ剤、抗酸化剤、保湿剤、血行促進剤、抗菌剤、殺菌剤、乾燥剤、冷感剤、温感剤、ビタミン類、アミノ酸、創傷治癒促進剤、刺激緩和剤、鎮痛剤、細胞賦活剤、酵素成分等が挙げられる。 Examples of the physiologically active ingredient include substances that impart some physiological activity to the skin when applied to the skin. For example, anti-aging agents, UV protection agents, squeeze agents, antioxidants, moisturizers, blood circulation promoters, antibacterial agents, bactericides, desiccants, cooling agents, warming agents, vitamins, amino acids, wound healing promoters , Stimulation mitigating agents, analgesics, cell activators, enzyme components and the like.
次に、本発明を実施例に基づいて更に詳細に説明するが、本発明はこれに限定されるものではない。 Next, the present invention will be described in more detail based on examples, but the present invention is not limited thereto.
(実施例1、比較例1〜5)
表1の組成の溶液を調製し、マイクロフルイダイザーで当該溶液を処理することにより、ウリジン、アセチルグルコサミンあるいはグルクロン酸を含んだ、実施例及び比較例で使用する各脂質二分子膜小胞を調製した。なお、表1における非リポソーム液は、アセチルグルコサミンと精製水とを混合しただけものである。
(Example 1, Comparative Examples 1-5)
By preparing a solution having the composition shown in Table 1 and treating the solution with a microfluidizer, each lipid bilayer vesicle used in Examples and Comparative Examples containing uridine, acetylglucosamine or glucuronic acid was prepared. did. The non-liposome solution in Table 1 is a mixture of acetylglucosamine and purified water.
上記の脂質二分子膜小胞を用い、表2の配合割合にて、実施例及び比較例の化粧水を常法により調製した。
<評価方法>
10名のモニタ−を任意に抽出し、その前腕の内側に塗布部位を設定し、被験サンプルを朝・夕の2回、適当量を塗布した。また、使用期間は1週間とした。
<Evaluation method>
Ten monitors were arbitrarily extracted, an application site was set inside the forearm, and an appropriate amount of the test sample was applied twice in the morning and evening. The period of use was one week.
未塗布時と、各評価サンプル塗布1週間後の角層水分量を角層水分量計SKICON−200EX(I.B.S.製)を用いて測定した。塗布前の角層水分量を100とした時の、塗布後の角層水分量の増減割合を算出した。 The stratum corneum moisture content was measured using a stratum corneum moisture meter SKICON-200EX (made by IBS) when not applied and one week after application of each evaluation sample. When the stratum corneum water content before coating was 100, the increase / decrease ratio of the stratum corneum water content after coating was calculated.
また、同時に、「肌ハリ」が改善したかのアンケート調査を、下記基準を用いて行った。
改善した:1点、改善しなかった:0点とし、スコアの合計により評価した。
At the same time, a questionnaire survey on the improvement of “skin elasticity” was conducted using the following criteria.
Improved: 1 point, not improved: 0 point, evaluated by the total score.
上記検討結果より、ウリジンリン酸2ナトリウム、アセチルグルコサミン、グルクロン酸ナトリウムを脂質二分子膜小包に内包させた単体よりも、ウリジンリン酸2ナトリウム、アセチルグルコサミン、グルクロン酸ナトリウムを一緒に脂質二分子膜小包に内包したもののほうが、角層水分量が上昇することが確認された。また、同様の結果が肌ハリ改善にも見られた。更に比較例2と5とから、脂質二分子膜小胞に内包させるほうが、わずかながら水分量の向上が見られた。 From the above results, it was found that disodium uridine phosphate, acetylglucosamine, and sodium glucuronate were combined together into a lipid bilayer membrane rather than a single body in which disodium uridine phosphate, acetylglucosamine, and sodium glucuronate were encapsulated in a lipid bilayer membrane. It was confirmed that the amount of moisture contained in the stratum corneum increased with the inclusion. Similar results were also seen in improving skin firmness. Furthermore, from Comparative Examples 2 and 5, the moisture content was slightly improved when encapsulated in lipid bilayer vesicles.
Claims (3)
(B1)アセチルグルコサミン又はその誘導体と、
(B2)グルクロン酸、グルクロン酸の塩、及び、それらの誘導体から選択される少なくとも1種と、
を含み、リポソーム内に封入されていることを特徴とする美容用皮膚外用組成物(ただし、タイソウ抽出物を必須成分として含有する皮膚外用剤、並びに、アデノシン5’−一リン酸及びその塩からなる群から選択される少なくとも1種のプリン系核酸関連物質を含有するコラーゲン産生促進用組成物は除く。)。 (A) uridine or a derivative thereof;
(B 1 ) acetylglucosamine or a derivative thereof;
(B2) at least one selected from glucuronic acid, a salt of glucuronic acid, and derivatives thereof;
Only including, cosmetic skin external composition characterized in that it is encapsulated in liposomes (where a skin external preparation containing a gymnastics extract as an essential component, and, adenosine 5'-monophosphate and a salt thereof Except for the composition for promoting collagen production containing at least one purine nucleic acid-related substance selected from the group consisting of:
A pharmaceutical or cosmetic product comprising the cosmetic external composition for skin according to claim 1 or 2 .
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