JP4854474B2 - 乳化剤形の皮膚外用剤 - Google Patents
乳化剤形の皮膚外用剤 Download PDFInfo
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- JP4854474B2 JP4854474B2 JP2006299874A JP2006299874A JP4854474B2 JP 4854474 B2 JP4854474 B2 JP 4854474B2 JP 2006299874 A JP2006299874 A JP 2006299874A JP 2006299874 A JP2006299874 A JP 2006299874A JP 4854474 B2 JP4854474 B2 JP 4854474B2
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- acid
- skin
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- extract
- oil
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Description
(1)1)N−アシルグルタミン酸のエステル及びN−アシルグリシンのエステルから選ばれる少なくとも1種と、2)水酸化レシチンと、3)硬化菜種油とを含有することを特徴とする、乳化剤形の皮膚外用剤。
(2)前記N−アシルグルタミン酸のエステルが、N−ラウロイル−L−グルタミン酸のエステルであることを特徴とする、(1)に記載の乳化剤形の皮膚外用剤。
(3)前記N−アシルグリシンのエステルが、N−カプリロイルグリシンのエステルであることを特徴とする、(1)又は(2)に記載の乳化剤形の皮膚外用剤。
(4)前記水酸化レシチンの含有量が、0.1〜1質量%であることを特徴とする、(1)〜(3)の何れかに記載の乳化剤形の皮膚外用剤。
本発明の皮膚外用剤は、乳化剤形であって、N−アシルアミノ酸のエステルを必須成分として含有することを特徴とする。N−アシルアミノ酸のエステルを構成するアシル基としては、炭素数8〜30の不飽和結合を有していても良い、脂肪族のアシル基が好適に例示でき、例えば、カプリロイル基、2−エチルヘキサノイル基、デカノイル基、ラウロイル基、ミリストイル基、パルミトイル基、ステアロイル基、ベヘノイル基、イソステアロイル基、オレオイル基などがより好適に例示できる。特に好ましいものはラウロイル基である。又、アシル化されるアミノ酸としては、アスパラギン酸やグルタミン酸などの酸性アミノ酸、グリシンやアラニンなどの中性アミノ酸、リシンやアルギニンなどの塩基性アミノ酸が例示でき、中でも、グルタミン酸とグリシンが好ましく、特にグリシンが好ましい。又、エステルを構成する炭化水素基は、コレステリル基、ベヘニル基、オクチルデシル基などが好適に例示できる。かかるN−アシルアミノ酸のエステルは酸性アミノ酸であればジエステルが好ましく、塩基性アミノ酸であればN,N’−ジアシルアミノ酸のエステルが好ましい。かかるN−アシルアミノ酸のエステルは、アミノ酸にアシルクロリドをアルカリ条件下で反応させ、N−アシルアミノ酸に誘導し、しかる後にアルカリ存在下アルキルハライド乃至はアルケニルはライドを反応させれば得ることが出来る。具体的な化合物例としては、N−アシルグリシンのエステルとしては、N−カプリロイルグリシンのベヘニルエステル、N−カプリロイルグリシンのオクチルドデシルエステルが例示でき、N−アシルグルタミン酸のエステルであれば、N−ラウロイル−L−グルタミン酸ジ(コレステリル/ベヘニル/オクチルドデシル)、N−ラウロイル−L−グルタミン酸ジ(コレステリル/オクチルドデシル)、N−ラウロイル−L−グルタミン酸ジ(フィトステリル/ベヘニル/オクチルドデシル)、N−ラウロイル−L−グルタミン酸ジ(フィトステリル/オクチルドデシル)等が好適に例示できる。これらの中では、N−カプリロイルグリシンオクチルドデシルエステル、N−ラウロイル−L−グルタミン酸ジ(コレステリル/オクチルドデシル)が特に好適に例示できる。N−アシルアミノ酸のエステルは、この様に合成したものを使用することも出来るが、既に化粧料原料などとして市販されているものも存し、この様な市販品を購入し利用することも出来る。特に好ましい市販品としては味の素株式会社より販売されている「エルデュウPS203」(N−ラウロイル−L−グルタミン酸ジ(フィトステリル/オクチルデシル))、「エルデュウCL−301」(N−ラウロイルグルタミン酸ジ(コレステリル/ベヘニル/オクチルドデシル))、「エルデュウCL−202」(N−ラウロイルグルタミン酸ジ(コレステリル/オクチルドデシル))、「エルデュウPS−304」(N−ラウロイルグルタミン酸ジ(フィトステリル/ベヘニル/オクチルドデシル))などが例示でき、中でも、「エルデュウPS203」が特に好ましい。が例示できる。かかる成分は唯一種含有させることも出来るし、二種以上を組み合わせて含有させることも出来る。好ましい含有量は、総量で、皮膚外用剤全量に対し、0.005〜5質量%であり、より好ましくは0.01〜10質量%であり、より好ましくは0.1〜5質量%である。かかる成分は、後記水酸化リン脂質とともに油性成分を角層内に移行せしめる作用に優れる。
本発明の皮膚外用剤は水酸化リン脂質を必須成分として含有することを特徴とする。本発明に言う水酸化リン脂質とは、リン脂質のアシル基に存する不飽和結合を酸化してジヒドロキシ体としたもので、基体となるリン脂質は、通常化粧料等で使用されるものであれば特段の限定はなく、例えば、レシチン、フォスファチジン酸、フォスファチジルグリセロール、フォスファチジルエタノールアミン、フォスファチジルイノシトール、フォスファチジルセリン或いはこれらのリゾ体が好ましく例示できる。かかるリン脂質のアシル基の二重結合を過酸化ベンゾイルなどの酸化剤を用いてエポキシドとなし、次いで水を付加させてジヒドロキシ体へ導いたものを水酸化リン脂質と定義する。この様な水酸化リン脂質には既に市販されているものが存し、かかる市販品を購入して用いることも出来る。好ましい市販品としては、例えば、ダイズを基源とする、水酸化レシチンとグリセリンの等量混合物である、「NIKKOL レシノール SH50」(日本サーファクタント工業株式会社製)等が好ましく例示できる。これらの水酸化リン脂質は、唯一種を含有することも出来るし、二種以上を組み合わせて含有させることも出来る。かかる成分は、乳化系に於いて、前記他方の必須成分である、N−アシルアミノ酸のエステルとともに働いて、皮膚内への油性成分の移行を向上させる作用を有する。この様な作用を奏するためには、かかるリン脂質は、総量で化粧料全量に対し、0.01〜2質量%含有することが好ましく、0.05〜1質量%含有することがより好ましい。
本発明の皮膚外用剤は、前記成分を必須成分として含有し、乳化剤形であることを特徴とする。かかる乳化剤形としては、水中油乳化剤形、油中水乳化剤形、これらの複合化した多層乳化剤形などが好ましく例示でき、水中油乳化剤形がこれらの中では特に好ましい。これは本発明の効果が、水中油乳化剤形では特に如実にあらわれるからである。ここで、本発明における、皮膚外用剤とは、皮膚を健やかに保つ経皮投与組成物であって、医薬用途のものを除くものであり、医薬部外品については包含する。
化鉄、酸化コバルト、群青、紺青、酸化チタン、酸化亜鉛の無機顔料類;表面を処理されていても良い、雲母チタン、魚燐箔、オキシ塩化ビスマス等のパール剤類;レーキ化されていても良い赤色202号、赤色228号、赤色226号、黄色4号、青色404号、黄色5号、赤色505号、赤色230号、赤色223号、橙色201号、赤色213号、黄色204号、黄色203号、青色1号、緑色201号、紫色201号、赤色204号等の有機色素類;ポリエチレン末、ポリメタクリル酸メチル、ナイロン粉末、オルガノポリシロキサンエラストマー等の有機粉体類;パラアミノ安息香酸系紫外線吸収剤;アントラニル酸系紫外線吸収剤;サリチル酸系紫外線吸収剤;桂皮酸系紫外線吸収剤;ベンゾフェノン系紫外線吸収剤;糖系紫外線吸収剤;2−(2’−ヒドロキシ−5’−t−オクチルフェニル)ベンゾトリアゾール、4−メトキシ−4’−t−ブチルジベンゾイルメタン等の紫外線吸収剤類;エタノール、イソプロパノール等の低級アルコール類;ビタミンA又はその誘導体、ビタミンB 6 塩酸塩、ビタミンB 6 トリパルミテート、ビタミンB 6 ジオクタノエート、ビタミンB 2 又はその誘導体、ビタミンB 12 、ビタミンB 15 又はその誘導体等のビタミンB類;α−トコフェロール、β−トコフェロール、γ−トコフェロール、ビタミンEアセテート等のビタミンE類、ビタミンD類、ビタミンH、パントテン酸、パンテチン、ピロロキノリンキノン等のビタミン類等;フェノキシエタノール等の抗菌剤などが好ましく例示できる。これらの成分の内、特に好ましいものは、肌の柔軟化に好適な、コラーゲンの弾性消失の原因である、炎症を抑える、有効成分、或いは、線維芽細胞のコラーゲンの産生能を高める作用を有する、有効成分等であり、具体的には、グリチルレチン酸誘導体、オトギリソウ抽出物、ローヤルゼリー抽出物、クジン抽出物、ソウハクヒ抽出物、セイヨウノコギリソウ抽出物、ツボクサ抽出物、イガイ抽出物、真珠抽出物、ダイズ抽出物、チョウジ抽出物、バクモンドウ抽出物、マルバハギ抽出物、コウキ抽出物、シラカバ抽出物、ローズマリー抽出物、セージ抽出物、ジンセン抽出物、セイヨウトチノキ抽出物、油溶性カンゾウ抽出物、ビタミンE並びにその誘導体、アルブチン、ビタミンC並びにその誘導体及びベニバナ抽出物から選択されるものである。グリチルレチン酸誘導体としては、グリチルレチン酸ステアリルなどのグリチルレチン酸のエステル、グリチルレチン酸の配糖体の塩である、グリチルリチン酸ジカリウムなどが好ましく例示でき、その含有量は0.03〜0.3質量%が好ましい。これらはカンゾウの抽出物として含有させることも出来る。オトギリソウの抽出物はファレロールを少なくとも100μM含有する形で含有させることが好ましい。ローヤルゼリー抽出物は1)ローヤルゼリー中のタンパク質の非変性ポリアクリルアミドゲル電気泳永動において単一バンドを形成する、2)還元条件下でのSDS−ポリアクリルアミドゲル電気泳動により測定される分子量が約57キロダルトンである、蛋白を(例えば、特許文献6を参照)、総蛋白に対して少なくとも9質量%含有するものを0.001〜0.1質量%含有することが好ましい。クジン抽出物は、ソフォラフラバノンGを少なくとも100μM含有するものを少なくとも0.001質量%含有することが好ましい。セイヨウノコギリソウはセンタウレイジンを少なくとも100μM含有するものを0.01〜1質量%含有することが好ましい。ダイズ抽出物としては、大豆蛋白を酵素加水分解したもの、ダイズイソフラボンが好ましく、かかる成分の好ましい含有量は、総量で0.01〜0.2質量%である。イガイ抽出物は、イガイの貝柱乃至はヒモのグリコーゲンを抽出したものが好ましく、その含有量は0.001〜0.2質量%が好ましい。チョウジ抽出物はオイゲノールを0.1〜1質量%含有するものが好ましく、かかる抽出物を0.01〜0.3質量%含有することが好ましい。バクモンドウはオフィオポゴナノンBを0.01〜0.1質量%含有するものを0.01〜0.2質量%含有することが好ましい。シラカバ抽出物は、ベツリン乃至はベツリン酸を200μM以上含有するものが好ましく、かかる抽出物を0.01〜0.1質量%含有することが好ましい。セイヨウトチノキ抽出物は、果実の抽出物が好ましく、中でもエスシンを0.01〜1質量%含有するものを0.01〜1質量%含有することが好ましい。油溶性カンゾウは、グラブリジンを0.01〜1質量%含有するものを0.01〜0.1質量%含有することが好ましい。ベニバナ抽出物は、カーサミンを含有すれば良く、カーサミン含有量に換算して、0.01〜0.2質量%含有することが好ましい。ローズマリーはロ
スマリン酸を0.001〜0.1質量%含有するものが好ましい。ビタミンCは1〜5質量%含有することが好ましく、アルブチン乃至はその塩は1〜10質量%含有することが好ましい。更に、化粧料の使用後感を向上させ、肌の柔軟性の向上を使用者に認識させるためには、パルミチン酸セチルを0.1〜1質量%含有させることが好ましい。
乳液1、比較例1、2を用いて、肌柔軟化作用を比較した。即ち、パネラー1群10名、計30名を用意し、Day0に「ヴィーナストロン」で肌の柔軟性を測定した後、1日朝晩2回、それぞれの化粧料で処理した。この作業を2週間連続して行った後、再度「ヴィーナストロン」で肌の柔軟性を測定した。(差分1)、測定後に、測定部位をアセトンで拭き取り、表面の油脂を除去し再々度肌の柔軟性を測定した。(差分2)処理後の数値から、処理前の数値を減じた値(差分)を求めた。結果を表2に示す。これより、本発明の化粧料は持続的な柔軟性の維持作用に優れることがわかる。
Claims (4)
- 1)N−アシルグルタミン酸のエステル及びN−アシルグリシンのエステルから選ばれる少なくとも1種と、2)水酸化レシチンと、3)硬化菜種油とを含有することを特徴とする、乳化剤形の皮膚外用剤。
- 前記N−アシルグルタミン酸のエステルが、N−ラウロイル−L−グルタミン酸のエステルであることを特徴とする、請求項1に記載の乳化剤形の皮膚外用剤。
- 前記N−アシルグリシンのエステルが、N−カプリロイルグリシンのエステルであることを特徴とする、請求項1又は2に記載の乳化剤形の皮膚外用剤。
- 前記水酸化レシチンの含有量が、0.1〜1質量%であることを特徴とする、請求項1〜3の何れか1項に記載の乳化剤形の皮膚外用剤。
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