JP4036739B2 - Cosmetics with reduced stinging - Google Patents
Cosmetics with reduced stinging Download PDFInfo
- Publication number
- JP4036739B2 JP4036739B2 JP2002363389A JP2002363389A JP4036739B2 JP 4036739 B2 JP4036739 B2 JP 4036739B2 JP 2002363389 A JP2002363389 A JP 2002363389A JP 2002363389 A JP2002363389 A JP 2002363389A JP 4036739 B2 JP4036739 B2 JP 4036739B2
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- Prior art keywords
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- skin
- acid
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- external preparation
- 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.)
- Expired - Lifetime
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Description
【０００１】
【発明の属する技術分野】
本発明は、皮膚外用剤に関し、更に詳細には、敏感肌の人用として好適な皮膚外用剤に関する。
【０００２】
【従来の技術】
乳化組成物は、親油性の成分も親水性の成分も含有可能であり、この為、油性成分と水性成分の両方の成分の処置の必要な分野においては有用な剤形となっている。このような分野としては、例えば化粧料、医薬、食品などの分野が特に好適に例示できる。この様な乳化組成物のうち、油中水乳化形態や多層乳化形態などの油相を外相に有する部分を有する乳化形態は、有効成分の経皮吸収性を向上させたり、皮膚とのなじみに優れ、皮膚のバリア機能を向上させるなどの効果を有するため、特に化粧料や皮膚外用医薬用の製剤として有用であることが知られている。
【０００３】
しかしながら、乳化系に於いては水性成分、油性成分が共存することから、対微生物汚染については他の剤形よりも脆弱性があり、防腐剤を使用することが通例となっている。防腐剤としては、その抗菌スペクトルと、油相水相への配向性から数種のパラベンを組み合わせて使用することが一般的になっている。確かにパラベン類は、安全性が高く、抗菌スペクトルの広い、優れた防腐剤であるが、近年の知見では、敏感肌の人に対して、一過性の刺激を感じさせやすい特質、所謂スティギング性があることが知られており、これを避けることが敏感肌用の化粧料では必要であると言われている。この様なスティギング対応としては、パラベン類が経皮吸収されるのを、高分子類で防ぐ方法（特開２００１−６４１８５、特開平１１−１０６３２７、特表平１１−５０２５０５）や抗菌性を有する、２，３−ブタンジオール、１，４−ブタンジオール、１，２−ペンタンジオールなどの多価アルコールを利用する技術が知られている（特開２００２−２１２０２１、特開２００２−１４５７１９、特開２００２−１２８６３３）。しかしながら、これらの技術で刺激発現物質を完全にシャットアウトすることは不可能であるし、抗菌性を多価アルコールのみで維持する為には、その使用量は、安定性に影響を与えるほど多くなってしまうのが常であった。即ち、皮膚外用剤に於いて、実際的なパラベンに依存しない防腐手段の開発が望まれていた。
【０００４】
一方、セラミドを含有する敏感肌用の化粧料としては、小麦胚芽より抽出されるセラミドを利用した化粧料（特開２００２−０５３４２８）、シスヘキサデセン酸と組み合わせた化粧料（特開２００１−０６４１５０）等の技術が知られている。しかしながら、１）セラミド乃至はその誘導体と２）フェノキシエタノールと３）中鎖・長鎖混合脂肪酸トリグリセライドとを含有する皮膚外用剤は全く知られていないし、この様な構成を取ることにより、パラベンフリーで充分な防腐力を具現化でき、以て敏感肌の人でもスティギングを起こしにくい皮膚外用剤になることも全く知られていなかった。
【０００５】
【発明が解決しようとする課題】
本発明は、この様な状況下為されたものであり、パラベンなどに起因するスティギングを抑制し、敏感肌の人でも使用可能な皮膚外用剤を提供することを課題とする。
【０００６】
【課題の解決手段】
この様な状況に鑑みて、本発明者らは、パラベンなどに起因するスティギングを抑制し、敏感肌の人でも使用可能な皮膚外用剤を求めて、鋭意研究努力を重ねた結果、１）特定のサブタイプのセラミド乃至はその誘導体から選択される皮膚修復素材と２）フェノキシエタノールと３）中鎖・長鎖混合脂肪酸トリグリセライドとを含有する皮膚外用剤がその様な特性を有していることを見出し、発明を完成させるに至った。即ち、本発明は、以下に示す技術に関するものである。
（１）１）サブタイプ１、２、３、５及び６から選択されるセラミド乃至はその誘導体から選択される皮膚修復素材と、２）フェノキシエタノールと、３）中鎖・長鎖混合脂肪酸トリグリセライドとを含有することを特徴とする、皮膚外用剤。
（２）上記中鎖・長鎖混合脂肪酸トリグリセライドが、（カプリル酸／カプリン酸／ミリスチン酸／ステアリン酸）トリグリセライドであることを特徴とする、（１）に記載の皮膚外用剤。
（３）パラベンフリーであることを特徴とする、（１）又は（２）に記載の皮膚外用剤。
（４）敏感肌用の化粧料であることを特徴とする、（１）〜（３）の何れか１に記載の皮膚外用剤。
【０００７】
【発明の実施の形態】
（１）本発明の皮膚外用剤の必須成分である皮膚修復素材
本発明の皮膚外用剤は、皮膚修復素材を含有することを特徴とする。ここで、皮膚修復素材とは、皮膚構成成分と同じ乃至は類似した構造を有する成分であって、皮膚のバリア機能を高める作用を有する成分を意味し、具体的にはセラミド、セラミド誘導体が挙げられる。セラミドにはサブタイプとして１〜６があり、これらのうち、その効果よりサブタイプ１、サブタイプ２、サブタイプ３、サブタイプ５及びサブタイプ６が利用可能であるが、サブタイプ６が特に好ましい。これらは唯一種を含有させることもできるし、二種以上を組み合わせて含有させることも可能である。かかる成分は、防腐力を損なうことなく、又、フェノキシエタノールの連続相への移行を助け、フェノキシエタノールの防腐効果を増強しながら、皮膚のバリア機能を修復し高めることにより、スティギング誘起物質が皮膚に作用して、刺激を起こさせることを抑制する作用を有する。本発明の皮膚外用剤における、前記皮膚修復素材の好ましい含有量は、総量で皮膚外用剤全量に対して、０．０１〜１０重量％が好ましく、０．０５〜５重量％が更に好ましい。これは、少なすぎると防腐効果を更に付与する作用を損なう場合があり、多すぎると安定性や感触の良さを損なう場合があるからである。
【０００８】
（２）本発明の皮膚外用剤の必須成分であるフェノキシエタノール
本発明の皮膚外用剤は、フェノキシエタノールを含有することを特徴とする。フェノキシエタノールはスティギング性が低い防腐剤であるが、その抗菌性も低い。これを上記皮膚修復素材と組み合わせることにより、系全体に優れた防腐効果を付与する。本発明に於ける、かかるフェノキシエタノールの好適な含有量は、皮膚外用剤全量に対して、０．１〜５重量％であり、更に好ましくは０．２〜１重量％である。これは少なすぎると、防腐効果を発揮しない場合があり、多すぎると防腐効果が頭打ちになり、系の安定性などを損なう場合があるからである。
【０００９】
（３）本発明の皮膚外用剤の必須成分である中鎖・長鎖混合脂肪酸トリグリセライド
本発明の皮膚外用剤は、中鎖・長鎖混合脂肪酸トリグリセライドを必須成分として、含有することを特徴とする。かかる中鎖・長鎖脂肪酸トリグリセライドを構成する中鎖脂肪酸残基としては、炭素数６〜１０のアルキルカルボニルオキシ基乃至はアルケニルカルボニルオキシ基が好適に例示でき、カプロン酸残基、カプリル酸残基、カプリン酸残基、２−エチルヘキサン酸残基、デカン酸残基、デセン酸残基等が好適に例示でき、カプリル酸残基又はカプリン酸残基がより好ましく例示できる。又、長鎖脂肪酸残基としては、炭素数１２〜３０のアルキルカルボニルオキシ基又はアルケニルカルボニルオキシ基が好適に例示でき、例えば、ラウリン酸残基、ミリスチン酸残基、パルミチン酸残基、ステアリン酸残基、ベヘン酸残基、オレイン酸残基、リノール酸残基などが好適に例示でき、ミリスチン酸残基又はステアリン酸残基がより好適に例示できる。特に好ましいものとしては、トリ（カプリン酸・カプリル酸・ミリスチン酸・ステアリン酸）グリセライドが例示できる。かかる中鎖・長鎖混合脂肪酸トリグリセライドは、例えば、ステアリン酸モノグリセリドをトリエチルアミンなどのアルカリ存在下、中鎖脂肪酸と塩化チオニルを反応させて作成した中鎖脂肪酸クロリド、例えば、カプリン酸クロリド或いはカプリル酸クロリドともに縮合させることにより製造することが出来る。又、この様な中鎖・長鎖混合脂肪酸トリグリセライドには、市販品も存在しそれを購入して使用することも出来る。市販品としては、例えば、トリ（カプリン酸／カプリル酸／ミリスチン酸／ステアリン酸）グリセライドである「サラコス３３４」（オイリオ株式会社製）などが好適に例示できる。本発明の皮膚外用剤に於いて、かかる中鎖・長鎖混合脂肪酸トリグリセライドは、皮膚修復素材とともに働いて、皮膚バリア能を高め、スティギング誘起成分が、真皮内に到達しないように防御するとともに、乳化系に於いては、防腐成分であるフェノキシエタノールを連続相に配向するように作用し、その防腐力を、スティギングなどの刺激を発現させずに高める作用を有する。かかる効果を発現する為には、前記中鎖・長鎖混合脂肪酸トリグリセライドは、本発明の皮膚外用剤において、０．０１〜１０重量％含有されることが好ましく、更に好ましくは、０．０５〜０．５重量％含有されることが好ましい。これは少なすぎると前記の効果を発揮しない場合があり、多すぎると効果が頭打ちになり、時として系の安定性を損なう場合があるからである。
【００１０】
（４）本発明の皮膚外用剤
本発明の皮膚外用剤は、上記必須成分を含有することを特徴とする。本発明に言う、皮膚外用剤とは、皮膚外用に適用される組成物の総称であり、例えば、化粧料（医薬部外品を含む）、皮膚外用医薬、皮膚外用雑貨等が例示できる。本発明の皮膚外用剤としては化粧料が好適であり、スティギング性が低い特性から、敏感肌用の化粧料に適用することが特に好適である。本発明の皮膚外用剤に於いては、上記必須成分以外に、皮膚外用剤で使用される任意成分を、本発明の効果を損ねない範囲に於いて含有することが出来る。かかる任意成分としては、例えば、スクワラン、流動パラフィン、軽質流動イソパラフィン、重質流動イソパラフィン、マイクロクリスタリンワックス、固形パラフィンなどの炭化水素類、ジメチコン、フェメチコン、シクロメチコン、アモジメチコン、ポリエーテル変性シリコーンなどのシリコーン類、ホホバ油、カルナウバワックス、モクロウ、ミツロウ、ゲイロウ、オレイン酸オクチルドデシル、イソプロピルミリステート、ネオペンチルグリコールジイソステアレート、リンゴ酸ジイソステアレートなどのエステル類、ステアリン酸、ラウリン酸、ミリスチン酸、パルミチン酸、イソステアリン酸、イソパルミチン酸、ベヘン酸、オレイン酸などの脂肪酸類、ベヘニルアルコール、セタノール、オレイルアルコール、オクタデシルアルコールなどの高級アルコール類、ヒマシ油、椰子油、水添椰子油、椿油、小麦胚芽油、イソステアリン酸トリグリセライド、イソオクタン酸トリグリセライド、オリーブオイル等の中鎖・長鎖混合脂肪酸トリグリセライドに分類されないトリグリセライド類、１，３−ブタンジオール、グリセリン、ジグリセリン、ジプロピレングリコール、ポリエチレングリコール、１，２−ペンタンジオール、１，２−ヘキシレングリコール、イソプレングリコールなどの多価アルコール、ソルビタンセスキオレート、ソルビタンモノオレート、ソルビタントリオレート、ソルビタンセスキステアレート、ソルビタンモノステアレート、ポリオキシエチレンソルビタンモノオレート、ポリオキシエチレンソルビタンモノステアレート、ポリオキシエチレンステアレート、ポリオキシエチレンオレート、ポリオキシエチレングリセリル脂肪酸エステル、ポリエキシエチレンアルキルエーテル、ポリオキシエチレン硬化ヒマシ油等の非イオン界面活性剤、ソジウムラウリルステアレート、ポリオキシエチレンアルキル硫酸塩、スルホコハク酸エステル塩などのアニオン界面活性剤、４級アルキルアンモニウム塩等のカチオン界面活性剤類、アルキルベタイン等の両性界面活性剤類、結晶セルロースや架橋型メチルポリシロキサン、ポリエチレン粉末、アクリル樹脂粉体等の有機粉体類、タルク、マイカ、セリサイト、炭酸マグネシウム、炭酸カルシウム、二酸化チタン、酸化鉄、紺青、群青、チタンマイカ、チタンセリサイト、シリカ等の表面処理されていても良い粉体類、アクリル酸・メタクリル酸アルキルコポリマー及び／又はその塩、カルボキシビニルポリマー及び／又はその塩、キサンタンガムやヒドロキシプロピルセルロースなどの増粘剤、レチノール、レチノイン酸、トコフェロール、リボフラビン、ピリドキシン、アスコルビン酸、アスコルビン酸リン酸エステル塩などのビタミンやグリチルリチン酸塩、グリチルレチン、ウルソール酸、オレアノール酸などのテルペン類、エストラジオール、エチニルエストラジオール、エストリオールなどのステロイド類などの有効成分、ジメチルアミノ安息香酸エステル類、桂皮酸エステル類、ベンゾフェノン類などの紫外線吸収剤などが好ましく例示できる。特に好ましい形態としては、パラベンフリーの形態である。又、フェノキシエタノールの防腐力を更に高める意味で、１，３−ブタンジオール、イソプレングリコール、１，２−ペンタンジオール、１，２−ヘキシレングリコール等の成分を含有することは極めて有利であり、好ましい。かかる抗菌性多価アルコール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することも出来る。特に好ましい形態は１，２−ヘキシレングリコールを含有する形態である。かかる抗菌性多価アルコールの好ましい含有量は、総量で、皮膚外用剤全量に対して、１〜２０重量％であり、更に好ましくは、２〜１０重量％である。これは、少なすぎると添加効果が得られない場合があり、多すぎると効果が頭打ちになり、徒に系の安定性を損なう場合があるからである。更に、本発明の皮膚外用剤の剤形は乳化形態であり、油相を外相に有する形態を含む乳化形態であることが好ましく、油中水乳化形態乃至は多層乳化形態であることが更に好ましい。これは、本発明の皮膚外用剤の必須成分である、中鎖・長鎖脂肪酸トリグリセライドが乳化系に於いて、防腐剤であるフェノキシエタノールを連続相に配向させる作用を有する為である。特に、油中水中油乳化形態或いは水中油中水乳化形態等の多層乳化形態に於いて連続相にフェノキシエタノールを配向させることは、通常の乳化系に比して微生物に対する安定性に大きく寄与するので重大であり、その意味で、本発明の皮膚外用剤を多層乳化形態で具現化することは意義深い。本発明の皮膚外用剤は、上記必須成分及び任意成分を、常法に従って処理することにより製造することが出来る。
【００１１】
【実施例】
以下に実施例をあげて本発明について更に詳細に説明を加えるが、本発明がこれら実施例にのみ限定されないことはいうまでもない。
【００１２】
＜実施例１＞
下記に示す処方に従って、本発明の皮膚外用剤１（油中水中油乳化形態の化粧料）を作成した。即ち、イ、ロをそれぞれ７０℃に加熱し、イにロを徐々に加えて中間水中油乳化物を得た。これを用いて、更にハ、ニ、ホをそれぞれ８０℃に加熱し、ハにニを徐々に加え、最後にホを加え攪拌冷却して本発明の皮膚外用剤１（油中水中油乳化形態の化粧料）を得た。このものは、更に滑らかなのび特性を有しており、化粧料として好適であった。このものの中鎖・長鎖混合脂肪酸である、トリ（カプリン酸・カプリル酸・ミリスチン酸・ステアリン酸）グリセライドをグリセリルトリステアレートに置換した比較例１とフェノキシエタノールを水０．２重量部とメチルパラベン０．３重量部に置換した比較例２を、トリ（カプリン酸・カプリル酸・ミリスチン酸・ステアリン酸）グリセライドをグリセリルトリステアレートに、且つ、フェノキシエタノールを水０．２重量部とメチルパラベン０．３重量部に置換した比較例３を作成し、これらのスティギング性をマウス尻尾スティギングモデルを用いて評価した。即ち、ＩＣＲマウス１群５匹の尻尾をサンドペーパーで処理し、スティギングを感じやすい状態にした。このモデルに１０μｌの化粧料をエッペンドルフで滴下し、滴下によって跳躍する距離を求め、群ごとに平均を算出した。結果を表１に示す。これより本発明の皮膚外用剤は、スティギングを非常に誘起しにくいことがわかる。又、これらについて、微生物汚染に対する抵抗性（防腐効果）を調べた。防腐効果は、これらの化粧料２０ｍｌに対し、予備培養後、菌体乃至は分生子をＰＢＳで１×１０６個／ｍｌ（終濃度）になるように菌液を加え、これをトリプトソイ寒天（ＴＳＡ）培地、サブロー寒天（ＳＤＡ）培地に２０μｌ播種して、３５℃で２４〜４８時間培養し、コロニー数をカウントした。この結果も表１にしめす。
イ
１０％水酸化カリウム水溶液 ０．１ 重量部
１，３−ブタンジオール ３ 重量部
キサンタンガム ０．１ 重量部
水 １５ 重量部
ロ
ベヘニルアルコール ０．４ 重量部
ステアリン酸クエン酸グリセリル ０．５ 重量部
グリセリルモノステアレート ０．１ 重量部
スクワラン ４．５ 重量部
ショ糖パルミチン酸エステル ２ 重量部
フェノキシエタノール ０．５ 重量部
混合脂肪酸トリグリセライド＊＊＊ ０．１ 重量部
ベヘン酸 ０．１ 重量部
ステアリン酸 ０．５ 重量部
グリセリン ３ 重量部
ハ
１，２−ヘキシレングリコール ５ 重量部
グリセリン ５ 重量部
ポリエチレングリコール１５００ １ 重量部
水 ２６．８８重量部
ニ
「アラセルＰ−１３５」 １ 重量部
「エルデュウＰＳ−３０４」 ０．１ 重量部
マカデミア脂肪酸フィトステリル ０．５ 重量部
椿油 ０．４ 重量部
セラミド（タイプ６） ０．１ 重量部
デカメチルシクロペンタシロキサン ４ 重量部
２−エチルヘキサン酸セチル １９ 重量部
「クロピュアＯＬ」 １ 重量部
イソステアリン酸ソルビット １ 重量部
δトコフェロール ０．０２重量部
ホ
中間水中油乳化物 ３０ 重量部
トウキエキス １ 重量部
チョレイエキス ０．７ 重量部
トウニンエキス ０．８ 重量部
チンピエキス ０．５ 重量部
＊＊＊トリ（カプリン酸・カプリル酸・ミリスチン酸・ステアリン酸）グリセライド
（「サラコス３３４」オイリオ株式会社製）
【００１３】
【表１】
＜参考試験例１＞
実施例１のセラミド（タイプ６）を椿油に置換した比較例４、セラミド（タイプ６）と中鎖・長鎖脂肪酸トリグリセライドを椿油に置換した比較例５とを作成し、マウス・スティギングモデルでテストした。結果を表２に示す。これより、セラミドなどの皮膚修復素材と中鎖・長鎖脂肪酸トリグリセライドの両方が存在することが好ましいことがわかる。
【００１５】
【表２】
＜実施例２〜５＞
下記に示す処方に従って、皮膚修復素材の種類を変えて、実施例１と同様に皮膚外用剤（油中水中油乳化形態の化粧料）を作成し、スティギングを調べた。
イ
１０％水酸化カリウム水溶液 ０．１ 重量部
１，３−ブタンジオール ３ 重量部
キサンタンガム ０．１ 重量部
水 １５ 重量部
ロ
ベヘニルアルコール ０．４ 重量部
ステアリン酸クエン酸グリセリル ０．５ 重量部
グリセリルモノステアレート ０．１ 重量部
スクワラン ４．５ 重量部
ショ糖パルミチン酸エステル ２ 重量部
フェノキシエタノール ０．５ 重量部
混合脂肪酸トリグリセライド＊＊＊ ０．１ 重量部
ベヘン酸 ０．１ 重量部
ステアリン酸 ０．５ 重量部
グリセリン ３ 重量部
ハ
１，２−ヘキシレングリコール ５ 重量部
グリセリン ５ 重量部
ポリエチレングリコール１５００ １ 重量部
水 ２６．８８重量部
ニ
「アラセルＰ−１３５」 １ 重量部
「エルデュウＰＳ−３０４」 ０．１ 重量部
マカデミア脂肪酸フィトステリル ０．５ 重量部
椿油 ０．４ 重量部
表３に記載の成分 ０．１ 重量部
デカメチルシクロペンタシロキサン ４ 重量部
２−エチルヘキサン酸セチル １９ 重量部
「クロピュアＯＬ」 １ 重量部
イソステアリン酸ソルビット １ 重量部
δトコフェロール ０．０２重量部
ホ
中間水中油乳化物 ３０ 重量部
トウキエキス １ 重量部
チョレイエキス ０．７ 重量部
トウニンエキス ０．８ 重量部
チンピエキス ０．５ 重量部
＊＊＊トリ（カプリン酸・カプリル酸・ミリスチン酸・ステアリン酸）グリセライド
（「サラコス３３４」オイリオ株式会社製）
【００１７】
【表３】
【発明の効果】
本発明によれば、パラベンなどに起因するスティギングを抑制し、敏感肌の人でも使用可能な皮膚外用剤を提供することが出来る。[0001]
BACKGROUND OF THE INVENTION
The present invention relates to a skin external preparation, and more particularly to suitable skin external preparation as a for humans with sensitive skin.
[0002]
[Prior art]
The emulsified composition can contain both a lipophilic component and a hydrophilic component. Therefore, the emulsified composition is a useful dosage form in a field requiring treatment of both an oily component and an aqueous component . As such fields, for example, fields such as cosmetics, medicines, and foods can be particularly preferably exemplified. Among such emulsified compositions , an emulsified form having a part having an oil phase in the outer phase, such as a water-in-oil emulsified form or a multilayer emulsified form, improves the transdermal absorbability of the active ingredient or is familiar with the skin. It is known to be particularly useful as a preparation for cosmetics and external skin medicines because of its excellent effects such as improving the barrier function of the skin.
[0003]
However, since an aqueous component and an oily component coexist in an emulsified system, it is more fragile than other dosage forms with respect to microbial contamination, and it is customary to use a preservative. As a preservative, it is common to use a combination of several types of parabens because of its antibacterial spectrum and orientation to the oily phase. Certainly, parabens are excellent preservatives with high safety and a broad antibacterial spectrum, but recent knowledge has shown that it is a characteristic that makes people with sensitive skin feel transient irritation, so-called stigging. It is known that there is a sex, and it is said that avoiding this is necessary for cosmetics for sensitive skin. In order to cope with such stinging, a method for preventing parabens from being percutaneously absorbed by a polymer (JP 2001-64185, JP 11-106327, JP 11-502505) and antibacterial properties are provided. , 2,3-butanediol, 1,4-butanediol, that is known a technique of utilizing a polyhydric alcohol such as 1,2-pentanediol (JP 2002-212021, JP 2002-145719, JP 2002-128633) . However, it is impossible to completely shut out stimulating substances with these technologies, and in order to maintain antibacterial properties only with polyhydric alcohols, the amount used is so large as to affect stability. It used to be. That is, it has been desired to develop an antiseptic means that does not depend on actual parabens in an external preparation for skin.
[0004]
On the other hand, as cosmetics for sensitive skin containing ceramide, cosmetics using ceramide extracted from wheat germ (JP 2002-053428), cosmetics combined with cis hexadecenoic acid (JP 2001-064150 ) Such techniques are known. However, there is no known skin external preparation containing 1) ceramide or a derivative thereof, 2) phenoxyethanol, and 3) a medium chain / long chain mixed fatty acid triglyceride. It has not been known at all that it can realize a sufficient antiseptic power and thus becomes a skin external preparation that is difficult to cause sting even for people with sensitive skin.
[0005]
[Problems to be solved by the invention]
The present invention has been made under such circumstances, and an object of the present invention is to provide a skin external preparation that can be used even by people with sensitive skin while suppressing staging caused by parabens.
[0006]
[Means for solving problems]
In view of such circumstances, the present inventors have found that, as a result of suppressing the Sutigingu caused such as parabens, also asked the skin external agent that can be used by people with sensitive skin, diligent research effort, 1) specific A skin external preparation containing a skin repair material selected from ceramides or derivatives thereof of 2), 2) phenoxyethanol, and 3) a medium- and long-chain mixed fatty acid triglyceride has such characteristics. The headline and invention were completed. That is, this invention relates to the technique shown below.
(1) 1) Skin repair material selected from ceramide selected from subtypes 1, 2, 3, 5 and 6 or derivatives thereof, 2) phenoxyethanol, 3) medium chain / long chain mixed fatty acid triglyceride An external preparation for skin, comprising:
(2) The external preparation for skin according to (1), wherein the medium chain / long chain mixed fatty acid triglyceride is (caprylic acid / capric acid / myristic acid / stearic acid) triglyceride.
(3) The external preparation for skin according to (1) or (2), which is paraben-free.
(4) The external preparation for skin according to any one of (1) to (3), which is a cosmetic for sensitive skin.
[0007]
DETAILED DESCRIPTION OF THE INVENTION
(1) Skin repair material which is an essential component of the skin external preparation of the present invention The skin external preparation of the present invention is characterized by containing a skin repair material. Here, the skin repair material means a component having the same or similar structure as the skin component, and has a function of enhancing the skin barrier function, and specifically includes ceramide and ceramide derivatives. It is done. The ceramide has 1-6 as subtypes of these, subtype 1 than its effect, subtype 2, subtype 3, but subtype 5 and subtype 6 is available, subtype 6 is particularly preferable. These may contain only one species, or may contain two or more species in combination. Such ingredients do not impair the antiseptic power, help the transition of the phenoxyethanol to the continuous phase, and enhance the antiseptic effect of phenoxyethanol, repairing and enhancing the barrier function of the skin, thereby causing the stigging inducer to act on the skin. And it has the effect | action which suppresses raising a stimulus. The preferable content of the skin repair material in the external preparation for skin of the present invention is preferably 0.01 to 10% by weight, and more preferably 0.05 to 5% by weight, based on the total amount of the external preparation for skin. This is because if the amount is too small, the action of further imparting an antiseptic effect may be impaired, and if the amount is too large, the stability and feel may be impaired.
[0008]
(2) Phenoxyethanol as an essential component of the external preparation for skin of the present invention The external preparation for skin of the present invention is characterized by containing phenoxyethanol. Phenoxyethanol is a preservative with low stigging properties, but its antibacterial properties are also low. By combining this with the above skin repair material , an excellent antiseptic effect is imparted to the entire system. The suitable content of such phenoxyethanol in the present invention is 0.1 to 5% by weight, more preferably 0.2 to 1% by weight, based on the total amount of the external preparation for skin. This is because if the amount is too small, the antiseptic effect may not be exhibited. If the amount is too large, the antiseptic effect may reach its peak, and the stability of the system may be impaired.
[0009]
(3) Medium- and long-chain mixed fatty acid triglyceride, which is an essential component of the skin external preparation of the present invention The skin external preparation of the present invention contains a medium-chain and long-chain mixed fatty acid triglyceride as an essential component. . Preferred examples of the medium chain fatty acid residue constituting the medium chain / long chain fatty acid triglyceride include an alkylcarbonyloxy group or alkenylcarbonyloxy group having 6 to 10 carbon atoms, and a caproic acid residue and a caprylic acid residue. , Capric acid residue, 2-ethylhexanoic acid residue, decanoic acid residue, decenoic acid residue and the like can be preferably exemplified, and caprylic acid residue or capric acid residue can be more preferably exemplified. Further, examples of the long-chain fatty acid residue include an alkylcarbonyloxy group or an alkenylcarbonyloxy group having 12 to 30 carbon atoms. For example, lauric acid residue, myristic acid residue, palmitic acid residue, stearic acid Residues, behenic acid residues, oleic acid residues, linoleic acid residues and the like can be preferably exemplified, and myristic acid residue or stearic acid residue can be more suitably exemplified. Particularly preferred is tri (capric acid / caprylic acid / myristic acid / stearic acid) glyceride. Such medium chain / long chain mixed fatty acid triglycerides are, for example, medium chain fatty acid chlorides prepared by reacting stearic acid monoglyceride with thionyl chloride in the presence of alkali such as triethylamine, for example, capric acid chloride or caprylic acid chloride. It can be produced by condensing together. In addition, such medium chain / long chain mixed fatty acid triglycerides are commercially available and can be purchased and used. As a commercially available product, for example, “Saracos 334” (manufactured by Eulio Co., Ltd.) which is tri (capric acid / caprylic acid / myristic acid / stearic acid) glyceride can be preferably exemplified. In the external preparation for skin of the present invention, such a medium chain / long chain mixed fatty acid triglyceride works with a skin repair material to enhance the skin barrier ability and prevent the staging inducing component from reaching the dermis, In the emulsification system, it acts to orient the phenoxyethanol, which is a preservative component, in a continuous phase, and has the effect of enhancing its preservative power without expressing any stimulus such as stigging. In order to express such an effect, the medium chain / long chain mixed fatty acid triglyceride is preferably contained in an amount of 0.01 to 10% by weight in the skin external preparation of the present invention, more preferably 0.05 to It is preferable to contain 0.5% by weight. This is because if the amount is too small, the above-mentioned effect may not be exhibited, and if the amount is too large, the effect reaches a peak and sometimes the stability of the system may be impaired.
[0010]
(4) External preparation for skin of the present invention The external preparation for skin of the present invention is characterized by containing the above essential components. The topical skin preparation referred to in the present invention is a general term for compositions that are applied to the topical skin. Examples thereof include cosmetics (including quasi-drugs), topical pharmaceuticals for skin and sundry items. As the external preparation for skin of the present invention, a cosmetic is suitable, and it is particularly suitable to be applied to a cosmetic for sensitive skin because of its low stigging property. In the skin external preparation of the present invention, in addition to the above essential components, optional components used in the skin external preparation can contain at a range that does not impair the effects of the present invention. Such optional components include, for example, hydrocarbons such as squalane, liquid paraffin, light liquid isoparaffin, heavy liquid isoparaffin, microcrystalline wax, solid paraffin, dimethicone, femethicone, cyclomethicone, amodimethicone, polyether-modified silicone, etc. Silicones, jojoba oil, carnauba wax, owl, beeswax, geiwa, octyldodecyl oleate, isopropyl myristate, esters such as neopentyl glycol diisostearate, diisostearate malate, stearic acid, lauric acid, Fatty acids such as myristic acid, palmitic acid, isostearic acid, isopalmitic acid, behenic acid, oleic acid, behenyl alcohol, cetanol, oleyl alcohol, octadecyl alcohol Higher alcohols such as coal, castor oil, coconut oil, hydrogenated coconut oil, coconut oil, wheat germ oil, isostearic acid triglyceride, isooctanoic acid triglyceride, triglycerides not classified as medium- and long-chain mixed fatty acid triglycerides such as olive oil, 1,3-butanediol, glycerin, diglycerin, dipropylene glycol, polyethylene glycol, 1,2-pentanediol, 1,2-hexylene glycol, isoprene glycol and other polyhydric alcohols, sorbitan sesquioleate, sorbitan monooleate, Sorbitan trioleate, sorbitan sesquistearate, sorbitan monostearate, polyoxyethylene sorbitan monooleate, polyoxyethylene sorbitan monostearate, polyoxyethylene Nonionic surfactants such as stearate, polyoxyethylene oleate, polyoxyethylene glyceryl fatty acid ester, polyoxyethylene alkyl ether, polyoxyethylene hydrogenated castor oil, sodium lauryl stearate, polyoxyethylene alkyl sulfate, sulfosuccinic acid Anionic surfactants such as ester salts, cationic surfactants such as quaternary alkyl ammonium salts, amphoteric surfactants such as alkyl betaines, crystalline cellulose, cross-linked methylpolysiloxane, polyethylene powder, acrylic resin powder, etc. Organic powders, talc, mica, sericite, magnesium carbonate, calcium carbonate, titanium dioxide, iron oxide, bitumen, ultramarine, titanium mica, titanium sericite, silica and other surface-treated powders, acrylic Acid / Methacryl Acid alkyl copolymer and / or salt thereof, carboxyvinyl polymer and / or salt thereof, thickener such as xanthan gum or hydroxypropyl cellulose, retinol, retinoic acid, tocopherol, riboflavin, pyridoxine, ascorbic acid, ascorbic acid phosphate ester salt, etc. Vitamins, glycyrrhizinate, glycyrrhetin, terpenes such as ursolic acid and oleanolic acid, steroids such as estradiol, ethinylestradiol and estriol, dimethylaminobenzoic acid esters, cinnamic acid esters, benzophenones, etc. The ultraviolet absorbers and the like can be preferably exemplified. A particularly preferred form is a paraben-free form. In addition, it is extremely advantageous and preferable to contain components such as 1,3-butanediol, isoprene glycol, 1,2-pentanediol, 1,2-hexylene glycol in order to further increase the preservative power of phenoxyethanol. . Such an antibacterial polyhydric alcohol can contain only one species or a combination of two or more species. A particularly preferred form is a form containing 1,2-hexylene glycol. The total content of the antibacterial polyhydric alcohol is 1 to 20% by weight, more preferably 2 to 10% by weight, based on the total amount of the external preparation for skin. This is because if the amount is too small, the effect of addition may not be obtained, and if the amount is too large, the effect reaches a peak, and the stability of the system may be impaired. Furthermore, the dosage form of the external preparation for skin of the present invention are emulsified form, is preferably a emulsified form comprising Form with oil phase into the external phase, it is water emulsified form to the oil a multi-layer emulsified form further preferable. This is because the medium- and long-chain fatty acid triglyceride, which is an essential component of the external preparation for skin of the present invention, has an action of orienting phenoxyethanol, which is a preservative, in a continuous phase in an emulsion system. In particular, to orient the phenoxyethanol in the continuous phase at the multi-layer emulsified form, such as a water emulsified form oil-in-water-oil emulsion form or oil-in-water contributes significantly to the stability against microbial compared to ordinary emulsion system since a serious, in that sense, it is embodied skin external preparation of the present invention in a multi-layer emulsified form Significantly. The skin external preparation of this invention can be manufactured by processing the said essential component and arbitrary components in accordance with a conventional method.
[0011]
【Example】
Hereinafter, the present invention will be described in more detail with reference to examples, but it is needless to say that the present invention is not limited to these examples.
[0012]
<Example 1>
According to the formulation shown below, the skin external preparation 1 of the present invention (a cosmetic in the form of an oil-in-water-in-oil emulsion) was prepared. That is, a and b were each heated to 70 ° C., and b was gradually added to i to obtain an intermediate oil-in-water emulsion . Using this, each of C, D and E is further heated to 80 ° C., D is gradually added to C, and finally H is added and stirred and cooled to prepare the external preparation for skin 1 (oil-in-water oil-in-water emulsion form). Cosmetics) . This product has a smooth and smooth characteristic and is suitable as a cosmetic. Comparative Example 1 in which tri (capric acid, caprylic acid, myristic acid, stearic acid) glyceride, which is a medium chain / long chain mixed fatty acid, was substituted with glyceryl tristearate, 0.2 parts by weight of water and methyl paraben 0 Comparative Example 2 substituted with 3 parts by weight was prepared by adding tri (capric acid / caprylic acid / myristic acid / stearic acid) glyceride to glyceryl tristearate, phenoxyethanol 0.2 parts by weight of water and methyl paraben 0.3 parts by weight. Comparative Example 3 with the part replaced was prepared, and their stigging properties were evaluated using a mouse tail stigging model. That is, the tails of 5 ICR mice per group were treated with sandpaper to make it easy to feel stinging. To this model, 10 μl of cosmetic material was dropped with Eppendorf, the jumping distance was determined, and the average was calculated for each group. The results are shown in Table 1. This shows that the skin external preparation of the present invention hardly induces staging. In addition, about these, it was examined resistance to microbial contamination (the antiseptic effect). The antiseptic effect is that, after pre-culture, 20 ml of these cosmetics are added with a bacterial solution or conidia in PBS to a concentration of 1 × 10 6 cells / ml (final concentration), and this is added to tryptosoy agar (TSA). ) 20 μl of the medium and Sabouraud agar (SDA) medium was inoculated and cultured at 35 ° C. for 24-48 hours, and the number of colonies was counted. The results are also shown in Table 1.
A 10% aqueous potassium hydroxide solution 0.1 parts by weight 1,3-butanediol 3 parts by weight xanthan gum 0.1 part by weight water 15 parts by weight lobehenyl alcohol 0.4 parts by weight glyceryl stearate 0.5 parts by weight glyceryl mono Stearate 0.1 parts by weight squalane 4.5 parts by weight sucrose palmitate 2 parts by weight phenoxyethanol 0.5 parts by weight mixed fatty acid triglyceride *** 0.1 parts by weight behenic acid 0.1 parts by weight stearic acid 0.5 Parts by weight glycerin 3 parts by weight c 1,2-hexylene glycol 5 parts by weight glycerin 5 parts by weight polyethylene glycol 1500 1 part by weight water 26.88 parts by weight d "Aracel P-135" 1 part by weight "El Dew PS-304" 0 .1 part by weight Macadamia fatty acid phytosteryl 0.5 part by weight Oil 0.4 parts by weight Ceramide (type 6) 0.1 part by weight Decamethylcyclopentasiloxane 4 parts by weight 2-ethylhexanoate cetyl 19 parts by weight “Cropure OL” 1 part by weight Sorbite isostearate 1 part by weight δ Tocopherol 0. 02 parts by weight
Intermediate oil-in-water emulsion 30 parts by weight Toki extract 1 part by weight Chorei extract 0.7 parts by weight Tonin extract 0.8 parts by weight Chinpi extract 0.5 parts by weight *** Tri (capric acid, caprylic acid, myristic acid, stearic acid) Glyceride ("Saracos 334" manufactured by Oilio Co., Ltd.)
[0013]
[Table 1]
<Reference Test Example 1>
Comparative Example 4 in which ceramide (type 6) in Example 1 was replaced with cocoon oil, Comparative Example 5 in which ceramide (type 6) and medium- and long-chain fatty acid triglycerides were replaced with cocoon oil were prepared, and a mouse stigging model was used. Tested. The results are shown in Table 2. This indicates that it is preferable that both a skin repair material such as ceramide and a medium chain / long chain fatty acid triglyceride exist.
[0015]
[Table 2]
<Examples 2 to 5 >
According to the formulation shown below, the type of skin repair material was changed, skin external preparations (cosmetics in the form of an oil-in-water-in-oil emulsion) were prepared in the same manner as in Example 1, and stigging was examined.
A 10% aqueous potassium hydroxide solution 0.1 parts by weight 1,3-butanediol 3 parts by weight xanthan gum 0.1 part by weight water 15 parts by weight lobehenyl alcohol 0.4 parts by weight glyceryl stearate 0.5 parts by weight glyceryl mono Stearate 0.1 parts by weight squalane 4.5 parts by weight sucrose palmitate 2 parts by weight phenoxyethanol 0.5 parts by weight mixed fatty acid triglyceride *** 0.1 parts by weight behenic acid 0.1 parts by weight stearic acid 0.5 Parts by weight glycerin 3 parts by weight c 1,2-hexylene glycol 5 parts by weight glycerin 5 parts by weight polyethylene glycol 1500 1 part by weight water 26.88 parts by weight d "Aracel P-135" 1 part by weight "El Dew PS-304" 0 .1 part by weight Macadamia fatty acid phytosteryl 0.5 part by weight Oil 0.4 parts by weight Ingredients listed in Table 3 0.1 parts by weight Decamethylcyclopentasiloxane 4 parts by weight 2-ethylhexanoic acid cetyl 19 parts by weight “Cropure OL” 1 part by weight Sorbite isostearate 1 part by weight δ Tocopherol 0 .02 parts by weight of intermediate oil-in-water emulsion 30 parts by weight Toki extract 1 part by weight Chorei extract 0.7 parts by weight Tonin extract 0.8 parts by weight chimpi extract 0.5 parts by weight *** Tri (capric acid / caprylic acid / myristin Acid / stearic acid) glyceride ("Saracos 334" manufactured by Oilio Co., Ltd.)
[0017]
[Table 3]
【The invention's effect】
ADVANTAGE OF THE INVENTION According to this invention, the skin external preparation which can suppress the stigging resulting from paraben etc. and can be used also by the person with sensitive skin can be provided.
Claims (4)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| JP2002363389A JP4036739B2 (en) | 2002-12-16 | 2002-12-16 | Cosmetics with reduced stinging |
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| JP2002363389A JP4036739B2 (en) | 2002-12-16 | 2002-12-16 | Cosmetics with reduced stinging |
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| JP2004196665A JP2004196665A (en) | 2004-07-15 |
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| JP5432470B2 (en) * | 2007-05-01 | 2014-03-05 | 株式会社ファンケル | Ceramide solution and external preparation for skin |
| CN110269929B (en) * | 2019-08-13 | 2021-11-02 | 昌正医疗(苏州)有限公司 | Composition with skin repairing effect and application thereof in cosmetics |
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