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SKIN INTRODUCTION SYSTEM AND LIGHTENING AGENT COMBINING CELL INTRODUCTION PEPTIDE AND SKIN INTRODUCTION ACCELERATOR

Foreign code F130007533
Posted date Jul 16, 2013
Country WIPO
International application number 2012JP071845
International publication number WO 2013031833
Date of international filing Aug 29, 2012
Date of international publication Mar 7, 2013
Priority data
  • P2011-189687 (Aug 31, 2011) JP
Title SKIN INTRODUCTION SYSTEM AND LIGHTENING AGENT COMBINING CELL INTRODUCTION PEPTIDE AND SKIN INTRODUCTION ACCELERATOR
Abstract Provided is a skin introduction system capable of introducing a broad range of drugs efficiently into individual cells of each of the tissues of the skin. Also provided is a lightening agent that provides highly effective lightening using the system. The skin introduction system is characterized in combining a skin introduction accelerator into a peptide derivative obtained by adding to a drug a peptide comprising an amino acid sequence in which 3 to 13 residual groups of arginine are concatenated. The lightening agent includes a peptide derivative of hydroquinone obtained by adding to hydroquinone a peptide comprising an amino acid sequence in which 3 to 13 residual groups of arginine are concatenated, the lightening agent characterized in being combined with a skin introduction accelerator.
Outline of related art and contending technology BACKGROUND ART
Specifically absorbed drug transdermally in general as a method, adding the functional group and a lipophilic targeting agents, ester or a surfactant, such as an enzyme reagent used at the same time the chemical absorption facilitation (Patent Document 1) or, non-ionic surfactant, a medium chain aliphatic single glycerin ester, absorption enhancers such as the amide compound or a combination of ultrasound and microneedles (Patent Document 2) formed by small holes such as the stratum corneum by physical absorption or absorption method (patent document 3) facilitation and the like.
However, promote the chemical absorption method, a sufficient effect is currently has not been achieved, in addition, to promote physical absorption method, for introduction into the devices is required, can cause injury to the skin further pointed out.
On the other hand, arginine peptide having the amino acid sequence in a row passes through the biological membrane functions as a signal sequence, a cell-membrane permeable have been reported (patent document 4). However, when applied to the skin, the degree to which the individual cells of the skin tissue and the like are introduced into, not heretofore reported No.
In particular, molecular weight 500Da or more of the compounds or the non-fat-soluble drug skin such as for the introduction, the introduction system includes effective so far not been reported.
In addition, the mechanism of transport is melanin production and melanin, the basic research, as well as applied research for a person, people that is widely and generally non-exhaustive list of interest is constantly in the topic. Ultraviolet rays such as excessive by tanning of the strong stimulation of the tyrosinase is abnormally activated, becomes very high when the melanin synthesis function, cannot be metabolized from the amount of melanin skin left on the skin to reach the base layer. By repeating this for many years, of a blemish at appears.
(Hereinafter, referred to also HQ) hydroquinone is lightening ingredients USA Food and Drug Administration (FDA) but was the only component, skin irritation is very high for more than 4% is required for the prescription of a physician. Therefore, in general commercially available cosmetics blended hydroquinone concentration is much less than the effective concentration, the effect can not be expected.
In addition, at a concentration of the whitening effect in the case of using hydroquinone, 'white' is very white portion referred to as decolorization of the dye becomes mottled can exhibit side effects such as have been reported. This is because, in particular the use of sensitive skin in consideration to a female, a fatal problem point.
Therefore, non-fat-soluble low-molecular-weight compound, various polymer compounds such as proteins more effectively to the skin active ingredient can be introduced to a new system been desired earnestly.
Scope of claims (In Japanese)請求の範囲 [請求項1]
アルギニン3~13残基が連続したアミノ酸配列からなるペプチドを薬物に付加したペプチド誘導体に、皮膚導入促進剤を組み合わせることを特徴とする皮膚導入システム。

[請求項2]
皮膚導入促進剤が1-ピレン酪酸である請求項1記載の皮膚導入システム。

[請求項3]
アルギニンの残基数が9~13である請求項1または2記載の皮膚導入システム。

[請求項4]
前記薬物が、タンパク質、ペプチド、低分子化合物から選択される請求項1~3のいずれか1項に記載の皮膚導入システム。

[請求項5]
前記タンパク質がEGFPである請求項4記載の皮膚導入システム。

[請求項6]
前記低分子化合物がハイドロキノンである請求項4記載の皮膚導入システム。

[請求項7]
ハイドロキノンにアルギニン3~13残基が連続したアミノ酸配列からなるペプチドを付加したハイドロキノンのペプチド誘導体を含む美白剤であって、皮膚導入促進剤との組み合わせを特徴とする美白剤。

[請求項8]
皮膚導入促進剤が1-ピレン酪酸である請求項7記載の美白剤。

[請求項9]
医薬品、医薬部外品または化粧料に添加して用いられる請求項7または8記載の美白剤。

  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • National University Corporation Okayama University
  • Inventor
  • MATSUI, Hideki
  • MICHIUE, Hiroyuki
  • ISHIKAWA, Sanae
IPC(International Patent Classification)
Specified countries National States: AE AG AL AM AO AT AU AZ BA BB BG BH BN BR BW BY BZ CA CH CL CN CO CR CU CZ DE DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IS JP KE KG KM KN KP KR KZ LA LC LK LR LS LT LU LY MA MD ME MG MK MN MW MX MY MZ NA NG NI NO NZ OM PE PG PH PL PT QA RO RS RU RW SC SD SE SG SK SL SM ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN ZA ZM ZW
ARIPO: BW GH GM KE LR LS MW MZ NA RW SD SL SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ RU TJ TM
EPO: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
OAPI: BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

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