JP5906194B2 - 皮膚外用剤 - Google Patents
皮膚外用剤 Download PDFInfo
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- JP5906194B2 JP5906194B2 JP2012552734A JP2012552734A JP5906194B2 JP 5906194 B2 JP5906194 B2 JP 5906194B2 JP 2012552734 A JP2012552734 A JP 2012552734A JP 2012552734 A JP2012552734 A JP 2012552734A JP 5906194 B2 JP5906194 B2 JP 5906194B2
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- Prior art keywords
- derivatives
- skin
- physiologically active
- surfactin
- salt
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- 125000002889 tridecyl 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])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- QNTNKSLOFHEFPK-UPTCCGCDSA-N ubiquinol-10 Chemical compound COC1=C(O)C(C)=C(C\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CCC=C(C)C)C(O)=C1OC QNTNKSLOFHEFPK-UPTCCGCDSA-N 0.000 description 1
- 125000002948 undecyl 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])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 235000019155 vitamin A Nutrition 0.000 description 1
- 239000011719 vitamin A Substances 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 229940046009 vitamin E Drugs 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
- 229940045997 vitamin a Drugs 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
- 229960002675 xylitol Drugs 0.000 description 1
- 125000005023 xylyl group Chemical group 0.000 description 1
- 239000010457 zeolite Substances 0.000 description 1
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 description 1
- OENHQHLEOONYIE-JLTXGRSLSA-N β-Carotene Chemical compound CC=1CCCC(C)(C)C=1\C=C\C(\C)=C\C=C\C(\C)=C\C=C\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C OENHQHLEOONYIE-JLTXGRSLSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/42—Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein
-
- 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
- A61K8/64—Proteins; Peptides; Derivatives or degradation products thereof
-
- 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
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/10—General cosmetic use
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Dermatology (AREA)
- Birds (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Inorganic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Cosmetics (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Description
本発明の課題は、低皮膚刺激性であって、生理活性成分の経皮吸収を十分に促進できる経皮吸収促進剤及び皮膚外用剤を提供することにある。
また本発明には、logP値が−5.5〜1.0の生理活性成分にリポペプチド化合物またはその塩を混ぜる生理活性物質の経皮吸収促進方法も含まれる。
好ましいMは、アルカリ金属(ナトリウム、カリウムなど)、特にナトリウムである。
静置型フランツセル(拡散有効膜面積約1.77cm2)を用いて、各生理活性成分の皮膚透過性試験を行った。マグネチックスターラーの回転子を入れたフランツセルのレセプター槽(容量約10mL)に、レセプター液(生理食塩水/エタノール=10/1)を満たした。ラット皮膚(適用実施例には表1中の皮膚欄に「a」と記載)または培養ヒト皮膚モデル(東洋紡績社製「TESTSKIN」(商標)。適用実施例には表1中の皮膚欄に「b」と記載)を、フランツセルのジョイント部にセットし、フランツセルのジャケット内を37℃に保った。ドナー槽(容量約10mL)に生理活性成分を含む試料0.7mLを入れ、試験を開始した。前記試料の組成は、サーファクチンNa:2重量%(ラット皮膚「a」の場合)又は1wt%(培養ヒト皮膚モデル「b」の場合)、生理活性成分:1重量%、グリセリン:10重量%、水:残余である。レセプター液をサンプリングし、皮膚を透過した生理活性成分の量(W1)を表1に記載の分析条件にて定量した。
サーファクチンナトリウムを未添加にする以外は実施例1〜13及び比較例1と同様の試験(コントロール)を実施し、皮膚を透過した生理活性成分の量(W2)を定量した。
なお下記表中、分析条件I〜IIIは、それぞれ、以下の内容を指す。
分析条件I:HPLC(装置:島津製作所社製20Aシリーズ、カラム:ナカライテスク社製 Cosmosil(登録商標)AR2(4.6mm i.d.×250mm)、カラム温度:30℃、検出:UV210nm、移動相:0.1重量%リン酸水溶液/アセトニトリル=98/2(体積比)から40/60(体積比)へのグラジエント、流速:1ml/min)
分析条件II:HPLC(装置:島津製作所社製20Aシリーズ、カラム:ナカライテスク社製 Cosmosil(登録商標)HILIC(4.6mmi.d.×250mm)、カラム温度:30℃、検出:RI、移動相:100mM酢酸アンモニウム水溶液/アセトニトリル=30/70(体積比)、流速:1ml/min)
分析条件III:HPLC(装置:島津製作所社製20Aシリーズ、カラム:資生堂社製 Capcellpak(商品名)SCX(4.6mmi.d.×250mm)、カラム温度:30℃、検出:荷電子化粒子検出器、移動相:2重量%トリフルオロ酢酸水溶液、流速:1ml/min)
表1に、試験開始24時間後における各生理活性成分の添加効果を示す。なお、表1中の「添加効果」とは、(サーファクチンNa添加区における生理活性成分の透過量(W1))/(サーファクチンNa未添加区における生理活性成分の透過量(W2))である。促進倍率とは、前記添加効果/サーファクチンNa添加区におけるサーファクチンNa濃度(重量%)である。また、表中のlogP値はCS Chem3D(商品名)ver.9.0を用いて求められた、各生理活性成分の計算値である。具体的には、上記関連ソフトウェアであるCS ChemDraw(商品名)で各生理活性成分の化学構造式を描き、上記Chem3D(商品名)に読み込ませることで、logP値を求めた。
Claims (4)
- 下記式(1):
logP値が−5.5〜1.0の生理活性成分(ただし、アシクロビルを除く)を含むことを特徴とする皮膚外用剤。 - 前記経皮吸収促進剤が、logP値が−5.5〜1.0の生理活性成分の静置型フランツセルを用いた試験での皮膚透過率を、サーファクチンまたはその塩1重量%あたり、サーファクチンまたはその塩未添加の場合に比べて2倍以上に促進するものである請求項1に記載の皮膚外用剤。
- 前記生理活性成分のlogP値が−5.5〜−1.4である請求項1又は2に記載の皮膚外用剤。
- 前記サーファクチンまたはその塩が、前記生理活性成分1重量部に対して、0.1〜100重量部であることを特徴とする請求項1〜3のいずれかに記載の皮膚外用剤。
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PCT/JP2012/050324 WO2012096276A1 (ja) | 2011-01-13 | 2012-01-11 | 経皮吸収促進剤及び皮膚外用剤 |
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JP6516083B2 (ja) * | 2013-06-05 | 2019-05-22 | 国立大学法人九州大学 | 経皮吸収基材 |
JP6975516B2 (ja) * | 2014-06-30 | 2021-12-01 | ロート製薬株式会社 | 外用組成物、化粧料、経皮吸収促進用組成物、外用組成物における有効成分の経皮吸収性を高める方法、経皮投与型医薬及び点眼用組成物 |
US10835572B2 (en) | 2014-06-30 | 2020-11-17 | Rohto Pharmaceutical Co., Ltd. | Composition for external application |
US9364413B2 (en) * | 2014-07-31 | 2016-06-14 | Umo International Co., Ltd. | Method for anti-aging treatment by surfactin in cosmetics via enhancing sirtuin |
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WO2016114340A1 (ja) * | 2015-01-15 | 2016-07-21 | 株式会社カネカ | 紫外線防御剤 |
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JP2009062288A (ja) * | 2007-09-04 | 2009-03-26 | National Institute Of Advanced Industrial & Technology | ソホロリピッドを含む経皮吸収制御剤及びその製造方法 |
WO2009044279A2 (en) * | 2007-09-30 | 2009-04-09 | Umo Inc., Co. Ltd. | Peptides having antimicrobial and/or biosurfactant properties |
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JP2000327591A (ja) * | 1998-05-29 | 2000-11-28 | Showa Denko Kk | 皮膚外用剤用界面活性剤及びそれを含有する皮膚外用剤 |
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