WO2011074275A1 - Promoteur de fonction barrière cutanée - Google Patents

Promoteur de fonction barrière cutanée Download PDF

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Publication number
WO2011074275A1
WO2011074275A1 PCT/JP2010/050470 JP2010050470W WO2011074275A1 WO 2011074275 A1 WO2011074275 A1 WO 2011074275A1 JP 2010050470 W JP2010050470 W JP 2010050470W WO 2011074275 A1 WO2011074275 A1 WO 2011074275A1
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WO
WIPO (PCT)
Prior art keywords
preparation
barrier function
skin barrier
group
internal
Prior art date
Application number
PCT/JP2010/050470
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English (en)
Japanese (ja)
Inventor
久美 富永
信子 本江
栄次 山下
Original Assignee
富士化学工業株式会社
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by 富士化学工業株式会社 filed Critical 富士化学工業株式会社
Publication of WO2011074275A1 publication Critical patent/WO2011074275A1/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/35—Ketones, e.g. benzophenone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/37—Esters of carboxylic acids
    • A61K8/375—Esters of carboxylic acids the alcohol moiety containing more than one hydroxy group
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67—Vitamins
    • A61K8/678—Tocopherol, i.e. vitamin E
    • 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

Definitions

  • the present invention relates to an external preparation and an internal preparation effective for improvement by improvement of the skin barrier function and improvement of the skin barrier function (hereinafter collectively referred to as skin barrier function promotion) and a combination thereof.
  • Skin tissue is an important tissue that protects a living body from external chemical or physical stimuli. Such a skin barrier function is said to be normal when a stratum corneum cell is matured, sufficiently flattened, and a structure in which cells having a sufficiently large surface area are layered is formed.
  • Patent Documents 1 to 4 are known, but it is still not sufficient.
  • the applicant of the present application has been conducting research and product development on astaxanthin so far, and it has been clarified that the skin barrier function is promoted by combining astaxanthin with a predetermined other component.
  • Patent Document 5 discloses a cosmetic obtained by purifying a krill solvent extract.
  • the test method evaluates the decrease in the amount of exfoliated corneocytes due to tape peeling, and it is not necessarily clear whether the skin barrier function has been improved.
  • JP 2007-14294 A Japanese Patent Application Laid-Open No. 2005-119995 Japanese Patent Laid-Open No. 2007-1914 JP 2004-51543 A Japanese Patent Laid-Open No. 5-15536
  • the present invention aims to provide an external preparation and an internal preparation effective for promoting the skin barrier function and a combination thereof.
  • the present invention is characterized by an external preparation applied to the skin and an oral preparation by oral administration, and particularly when the external preparation and the internal preparation are used in combination, a significant improvement in the recovery of the skin barrier function or an improvement in the skin barrier function is observed. .
  • the skin barrier function promotion external preparation as an external preparation which concerns on this invention is characterized by containing one or both and astaxanthin among tocopherol and the glyceride represented by following General formula (1).
  • R 1 , R 2 and R 3 are each a linear or branched saturated or unsaturated alkyl group having 8 to 22 carbon atoms, which may be the same or different.
  • the internal preparation for promoting skin barrier function according to the present invention contains one or both of tocopherol and glyceride represented by the following general formula (1) and astaxanthin.
  • R 1 , R 2 and R 3 are each a linear or branched saturated or unsaturated alkyl group having 8 to 22 carbon atoms, which may be the same or different. That is, the combination of one or both of the glyceride and tocopherol represented by the general formula (1) with the astaxanthin according to the present invention can be used as an external preparation or an internal preparation, thereby improving the skin barrier function. Or improve.
  • tocopherol is also called vitamin E and is a methylated derivative of tocol.
  • ⁇ , ⁇ , ⁇ , and ⁇ depending on the position of the methyl group, and D- ⁇ -tocopherol exists widely in nature.
  • the tocopherol may be any of the above, or a mixed tocopherol mixed.
  • Astaxanthin is a kind of carotenoid classified into xanthophylls.
  • the IUPAC name is 3,3′-dihydroxy- ⁇ , ⁇ -carotene-4,4′dione, depending on the position of the hydroxy group at the 3 and 3 ′ positions, (3R, 3′R), (3R, 3 ′S) ) (Meso) and (3S, 3 ′S) isomers, and has cis-trans isomers of conjugated double bonds.
  • any astaxanthin may be used. Moreover, it can exist as a free type, a monoester type, and a diester type.
  • Examples of those derived from natural products include microalgae such as green algae Hematococcus, yeasts such as red yeast Phaffia, arthropods such as shrimp, krill, crab and daphnia, molluscs such as squid and octopus Viscera and gonads, various seafood skins, petals of the genus Fuchsia such as Natsuzaki Fukujusou, Paracoccus sp. N81106, Brevundimonas sp. SD212, Erythrobacter sp. ⁇ -proteobacteria such as PC6, Gordonia sp. Gordonia, such as KANMONKAZ-1129, Schizophytrium sp. Examples thereof include those obtained from Labyrinthulas (particularly Yabetaceae) such as KH105 and astaxanthin-producing genetically modified organisms. Natural extracts and chemically synthesized products are commercially available and are readily available.
  • the trifatty acid glyceride may be an ester of glycerin and a linear or branched fatty acid having 8 to 22 carbon atoms, and these may be saturated or unsaturated fatty acids.
  • An ester with a medium chain fatty acid having 8 to 12 carbon atoms is preferred.
  • the medium chain fatty acid include glyceryl tricaprylate, glyceryl tri-2-ethylhexanoate, glyceryl tri (capryl / capric acid), glyceryl triundecylate, glyceryl triisopaltiminate, and particularly preferably tri (capryl / Capric acid) glyceryl.
  • the form of the external preparation includes, but is not particularly limited to, the form of a skin external preparation for pharmaceuticals and cosmetics.
  • a skin external preparation for pharmaceuticals and cosmetics.
  • cosmetics for example, milky lotion, cream, lotion, pack, dispersion liquid, cleaning agent, makeup cosmetics, scalp / hair products.
  • cosmetics such as ointments, creams, and liquids for external use.
  • components commonly used in skin external preparations such as cosmetics and pharmaceuticals, such as whitening agents, moisturizers, various skin nutritional components, ultraviolet absorbers, antioxidants, oily components, surfactants, thickeners , Alcohols, coloring agents, water, preservatives, fragrances and the like can be appropriately blended as necessary. More specifically, examples include components described in Japanese Patent Application Laid-Open No. 2003-55188 filed earlier by the present applicant.
  • the oral preparation in the oral preparation according to the present invention, it should be used as supplements, health foods, health functional foods such as nutritional functional foods and foods for specified health use, special purpose foods, general foods, quasi drugs, and supplements for sports. Since it is easy to decide and easy to determine the amount of intake, supplements, sports supplements, functional health foods, special-purpose foods are preferred, the same form as the above-mentioned pharmaceuticals, tablets, intraoral rapidly disintegrating tablets, capsules, It can be taken in solid dosage forms such as granules, fine granules, and liquid dosage forms such as solutions, drinks, syrups and suspensions.
  • the effect of improving the skin barrier function is recognized even when only the above-mentioned external preparation or the internal preparation is used alone, when the external preparation and the internal preparation are used in combination, the skin barrier function is further improved.
  • R 1 , R 2 and R 3 are each a linear or branched saturated or unsaturated alkyl group having 8 to 22 carbon atoms, which may be the same or different. Furthermore, when these external preparations and internal preparations are used in combination, a skin barrier function improving effect is further recognized.
  • TEWL transepidermal water transpiration
  • Example 1 Use in four groups combining Example 1 (Group A) and Comparative Example 1 (Group P) as internal preparations and Example 2 (Group S) and Comparative Example 2 (Group C) as external preparations in Test Example 2
  • the change rate of TEWL 3 weeks after the start is shown.
  • the change rate of TEWL 6 weeks after the start is shown.
  • Test Example 2 the change ratio of the stratum corneum cell area after 6 weeks due to the use of the external preparation shown in Example 2 (S group) and Comparative Example 2 (C group) is shown.
  • Test Example 2 the change rate of the stratum corneum cell area after 6 weeks due to the use of the internal preparation shown in Example 1 (Group A) and Comparative Example 1 (Group P) is shown.
  • the change rate of the stratum corneum cell area 6 weeks after the start is shown.
  • Example 1 For 30 women, 200 mg capsules of the component ratio shown in Example 1 of Table 1 were taken as internal preparations by 1 capsule each morning and evening (2 capsules per day). At that time, it was shown in Example 2 of Table 2 0.5 ml (1 ml per day) of the external preparation at the blending ratio was applied to the face.
  • the Haematococcus alga extract shown in Table 1 contains 10 to 12% of diester type astaxanthin in terms of free type.
  • tri (capryl / capric acid) glyceryl is contained 10 times or more of astaxanthin as an internal preparation.
  • Biocera G is a product of Dainippon Kasei Co., Ltd. and is a blend of glycerin, sphingomonas extract and tocopherol. Biocera G contains 0.02% of tocopherol, and in Comparative Example 2, the value is 0.0002%.
  • the external preparation in this invention exists in the point which mix
  • the amount of tocopherol is required to be at least 0.1 times the amount of astaxanthin (in terms of free form) in the following mass, preferably 0.3 times the amount or more, but depending on other additive components, 1.5 times the amount. In some cases, it may be more than the amount, preferably more than twice, more preferably more than 5 times.
  • tri (capryl / capric acid) glyceryl is an oily component and has an action of diluting and stabilizing astaxanthin.
  • this tri (caprylic / capric acid) glyceryl may not be an essential component, but in this example, tri (caprylic / capric acid) glyceryl is contained in an amount of 10.4 times that of astaxanthin. It is. Moreover, when the compounding quantity of astaxanthin becomes less than 0.0042% of a present Example, it may exceed 10 times amount relatively and may become a 100 times amount level or more.
  • TEWL transepidermal water transpiration
  • ⁇ m 2 stratum corneum cell area
  • TEWL transepidermal water transpiration
  • the collected horny layer cells were stained with a hematoxylin / eosin staining method (Mayers Hematoxylin Solution, 1% EosinY Solution: manufactured by Wako Pure Chemical Industries, Ltd.).
  • Microscopic images of stained horny layer cells were analyzed by image processing software (ImageJ: developed by National Institutes of Health), and the area of horny layer cells was measured. At that time, approximately 30 stratum corneum cells per subject were randomly selected and the area was averaged to obtain the stratum corneum cell area for each subject.
  • FIG. 1 shows a graph of the TEWL value of). Moreover, the graph of the value of a stratum corneum cell area is shown in FIG. In addition, a value shows the average value of 30 women. The TEWL value greatly decreased.
  • the difference between the mean values was t-tested, it became highly significant at a risk rate of 1%, and the stratum corneum cell area increased and became significant at a risk rate of 5%. Thereby, it became clear that a skin barrier function improves by using the internal preparation and external preparation which concern on this invention together.
  • ⁇ Test Example 2> First, 37 males were divided into 18 Active group (Group A) and 19 Placebo group (P group), and A group was given one capsule (1 mg / day) 2 capsules per day), and 200 mg capsules shown in Comparative Example 1 were similarly taken in the morning and evening (2 capsules per day) in the P group.
  • the topical preparation of Example 2 shown in Table 2 above as the Subject group (S group) was applied to the A group and the P group on the face half as shown in FIG.
  • the external preparation of Comparative Example 2 was applied twice in the morning and evening twice as a Compared group (Group C) to the remaining half of the face.
  • the graph shown in FIG. 4 excludes one of the group C [A / C + P / C (37 persons)] and the group S [A / S + P / S (37 persons)] to investigate the effect of the external preparation.
  • the change ratio (average value) 6 weeks after the start of use of the TEWL value is shown.
  • the graph shown in FIG. 7 shows the change in TEWL value after 6 weeks of use relative to the start of the test. Indicates the ratio.
  • the external preparation and the internal use according to the present invention both in the presence / absence of use of the external preparation according to the present invention (comparison between the S group and the C group) and the use or non-use of internal use (comparison between the A group and the P group).
  • the TEWL value is decreased by the use of the agent, as shown in FIGS. 6 and 7, the TEWL value of the A / S group in which the external preparation and the internal preparation according to the present invention are used together is the largest decrease. Therefore, it has been clarified that the external preparation and the internal preparation according to the present invention have a skin barrier function promoting effect even when used alone, and when both are used in combination, there is a greater effect.
  • the graph shown in FIG. 8 shows the difference in the external preparation, the sixth week of use relative to the start of the test between group C [A / C + P / C (37 persons)] and group S [A / S + P / S (37 persons)].
  • the change rate of the stratum corneum cell area is shown, and the graph shown in FIG. 9 shows the difference in the internal use, group P [P / S + P / C (38 persons)] and group A [A / S + A / C (36 persons)].
  • the change ratio of the stratum corneum cell area after 6 weeks of use relative to the start of the test is shown.
  • FIG. 10 shows the stratum corneum at the 6th week of use at the start of each of four groups, P / C, P / S, A / C, and A / S, in which external preparations and internal preparations are combined.
  • the cell area change ratio is shown.
  • the use effect of the external preparation according to the present invention is greatly expressed as shown in FIG. 8, and the internal preparation and external preparation according to the present invention are used in combination as shown in FIG.
  • the A / S group showed the largest area improvement change.
  • the present invention is an external preparation or internal preparation effective for recovery and improvement of the skin barrier function.
  • the external preparation include skin external preparations for pharmaceuticals and cosmetics
  • examples of internal preparations include supplements, health foods, nutritional functional foods, quasi drugs, and general foods. .

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Birds (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Toxicology (AREA)
  • Cosmetics (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention porte sur une préparation pour une application externe et sur une préparation pour une application interne qui sont toutes deux efficaces pour favoriser la fonction de barrière cutanée. L'invention porte également sur une combinaison de la préparation pour une application externe et de la préparation pour une application interne. La préparation pour une application externe et la préparation pour application une interne sont caractérisées en ce qu'elles comprennent du tocophérol et/ou un glycéride représenté par la formule générale (1) et de l'astaxanthine. (Dans la formule, R1, R2 et R3 peuvent être identiques les uns aux autres ou différents les uns des autres et représentent chacun indépendamment un groupe alkyle linéaire ou ramifié, saturé ou insaturé ayant 8 à 22 atomes de carbone.)
PCT/JP2010/050470 2009-12-18 2010-01-18 Promoteur de fonction barrière cutanée WO2011074275A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2009287231A JP5912215B2 (ja) 2009-12-18 2009-12-18 皮膚バリア機能促進剤
JP2009-287231 2009-12-18

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018212147A1 (fr) 2017-05-15 2018-11-22 江崎グリコ株式会社 Agent d'élimination de l'aspect terne de la peau, et agent de maintien ou d'amélioration de la fonction barrière de la peau

Families Citing this family (2)

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Publication number Priority date Publication date Assignee Title
JP2013107832A (ja) * 2011-11-17 2013-06-06 Tsubaki:Kk 化粧料組成物及びその製造方法
JP6480216B2 (ja) * 2014-03-10 2019-03-06 株式会社コーセー カロテノイド含有組成物、並びにカロテノイドの劣化抑制剤及びカロテノイドの劣化抑制方法

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JP2004051543A (ja) * 2002-07-19 2004-02-19 Naris Cosmetics Co Ltd 皮膚化粧料
JP2005027589A (ja) * 2003-07-08 2005-02-03 Medi Cube Co Ltd スキンケア用の内服組成物
JP2007001914A (ja) * 2005-06-23 2007-01-11 Nippon Menaade Keshohin Kk 皮膚バリア機能改善剤
JP2008100991A (ja) * 2006-09-22 2008-05-01 Rohto Pharmaceut Co Ltd カロテノイドが安定化された水性製剤
JP2008154577A (ja) * 2006-12-01 2008-07-10 Fujifilm Corp エマルション組成物、該エマルション組成物を含む食品及び化粧品
WO2009075383A1 (fr) * 2007-12-12 2009-06-18 Fujifilm Corporation Préparation externe pour la peau et son procédé de fabrication
JP2009143961A (ja) * 2009-03-19 2009-07-02 Fuji Chem Ind Co Ltd 経口用美肌用剤
JP2009173581A (ja) * 2008-01-24 2009-08-06 Fujifilm Corp エマルション組成物およびその製造方法、ならびに化粧品

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JP2003306446A (ja) * 2002-02-14 2003-10-28 Fancl Corp 皮膚老化防止剤及び／又はニキビ改善剤キット
JP2003335668A (ja) * 2002-05-21 2003-11-25 Fuji Chem Ind Co Ltd 経口用美肌用剤
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JP2004051543A (ja) * 2002-07-19 2004-02-19 Naris Cosmetics Co Ltd 皮膚化粧料
JP2005027589A (ja) * 2003-07-08 2005-02-03 Medi Cube Co Ltd スキンケア用の内服組成物
JP2007001914A (ja) * 2005-06-23 2007-01-11 Nippon Menaade Keshohin Kk 皮膚バリア機能改善剤
JP2008100991A (ja) * 2006-09-22 2008-05-01 Rohto Pharmaceut Co Ltd カロテノイドが安定化された水性製剤
JP2008154577A (ja) * 2006-12-01 2008-07-10 Fujifilm Corp エマルション組成物、該エマルション組成物を含む食品及び化粧品
WO2009075383A1 (fr) * 2007-12-12 2009-06-18 Fujifilm Corporation Préparation externe pour la peau et son procédé de fabrication
JP2009173581A (ja) * 2008-01-24 2009-08-06 Fujifilm Corp エマルション組成物およびその製造方法、ならびに化粧品
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018212147A1 (fr) 2017-05-15 2018-11-22 江崎グリコ株式会社 Agent d'élimination de l'aspect terne de la peau, et agent de maintien ou d'amélioration de la fonction barrière de la peau

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