JP2021001227A - 外用組成物 - Google Patents
外用組成物 Download PDFInfo
- Publication number
- JP2021001227A JP2021001227A JP2020168848A JP2020168848A JP2021001227A JP 2021001227 A JP2021001227 A JP 2021001227A JP 2020168848 A JP2020168848 A JP 2020168848A JP 2020168848 A JP2020168848 A JP 2020168848A JP 2021001227 A JP2021001227 A JP 2021001227A
- Authority
- JP
- Japan
- Prior art keywords
- magnolia
- extract
- weight
- external composition
- ascorbic acid
- 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.)
- Pending
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Abstract
Description
項1. (A)アスコルビン酸及び/又はその誘導体、並びに(B)モクレン科モクレン属植物の抽出物を含有することを特徴とする、外用組成物。
項2. 更に、(C)バラ科サクラ属植物の抽出物を含有する、項1に記載の外用組成物。
項3. 前記(B)成分が、ホオノキの抽出物である、項1又は2に記載の外用組成物。
項4. 前記(C)成分が、プルーンの抽出物である、項1〜3のいずれかに記載の外用組
成物。
項5. 前記(A)成分が、アスコルビン酸2−グルコシドである、項1〜4のいずれかに
記載の外用組成物。
項6. 美白用である、項1〜5のいずれかに記載の外用組成物。
本発明の外用組成物は、アスコルビン酸及び/又はその誘導体を含有する。アスコルビン酸及び/又はその誘導体は、抗酸化作用があり、美白効果が知られている公知の成分である。
本発明の外用組成物は、アスコルビン酸及び/又はその誘導体と共に、モクレン科モクレン属植物の抽出物を含有する。このように、アスコルビン酸及び/又はその誘導体とモクレン科モクレン属植物の抽出物とを併用することによって、メラニンの生成抑制作用が飛躍的に高まり、格段に優れた美白効果を奏することが可能になる。
また濃縮又は乾燥後、得られた濃縮物又は乾燥物を非溶解性溶媒で洗浄して精製して用いてもよく、またこれを更に適当な溶剤に溶解若しくは懸濁して用いることもできる。
本発明の外用組成物には、(A)成分及び(B)成分に加えて、バラ科サクラ属植物の抽出物((C)成分と表記することもある)が含まれていてもよい。(A)成分及び(B)成分と共に、バラ科サクラ属植物の抽出物が含まれている場合には、美白効果がより一層向上させることが可能になる。
有量として、(C)成分の乾燥重量換算で、好ましくは0.00005〜0.01重量%、更に好ましくは0.0001〜0.001重量%が挙げられる。
本発明の外用組成物は、前述する成分に加えて、水溶性増粘剤((D)成分と表記することもある)、多孔質粉体((E)成分と表記することもある)、及びトリメチルグリシン((F)成分と表記することもある)を含んでいてもよい。前述する成分と共に、これらの(D)〜(F)成分を一体として含む場合には、優れた美白効果に加え、塗布時に、しっかりとした塗布感がありながら、べたつきが抑制され、且つさっぱりとした感触があり、塗布後には、粉っぽさが抑えられ、しかも優れた保湿感を付与することが可能になる。
本発明の外用組成物には、保湿作用の増強等を目的として、必要に応じて、多価アルコールが含まれていてもよい。
本発明の外用組成物は、所望の製剤形態にするために、必要に応じて、基剤として水を含んでいてもよい。特に、前述する(D)及び(F)成分を含有させる場合には、それらの成分を溶解させるための基剤として水を含有させることが望ましい。
本発明の外用組成物は、前述する成分以外に、必要に応じて、他の薬理成分を含有していてもよい。このような薬理成分としては、例えば、抗ヒスタミン剤(ジフェンヒドラミン、ジフェンヒドラミン塩酸塩、マレイン酸クロルフェニラミン等)、局所麻酔剤(リドカイン、ジブカイン、アミノ安息香酸メチル、プロカイン、テトラカイン、ブピパカイン、メピパカイン、クロロプロカイン、プロパラカイン、メプリルカイン又はこれらの塩、オルソカイン、オキセサゼイン、オキシポリエントキシデカン、ロートエキス、ペルカミンパーゼ、テシットデシチン等)、抗炎症剤(アラントイン、グリチルリチン酸、グリチルリチン酸メチル、グリチルリチン酸ステアリル、グリチルリチン酸ジカリウム、グリチルリチン酸モノアンモニウム、グリチルレチン酸、グリチルレチン酸ピリドキシン、グリチルレチン酸ステアリル、グリチルレチン酸グリセリル、グリチルレチン酸モノグルクロニド、サリチル酸、サリチル酸メチル、サリチル酸グリコール、インドメタシン、フェルビナク、ジクロフェナクナトリウム、ロキソプロフェンナトリウム、ウフェナマート、イブプロフェンピコノール、スプロフェン、ベンダザック、スプロフェン、ブフェキサマク等)、殺菌剤(ベンザルコニウム塩化物、デカリニウム塩化物、ベンゼトニウム塩化物、セチルピリジニウム塩化物、クロルヘキシジン塩化物、グルコン酸クロルヘキシジン、イソプロピルメチルフェノール、アンモニア水、スルファジアジン、乳酸、フェノール等)、皮膚保護剤(コロジオン、ヒマシ油等)、血行促進剤(ノニル酸ワニリルアミド、ニコチン酸ベンジルエステル、カプサイシン、トウガラシエキス等)、清涼化剤(メントール、カンフル等)、ビタミン類(ビタミンA、B、D等)、ムコ多糖類(コンドロイチン硫酸ナトリウム、グルコサミン、ヒアルロン酸等)等が挙げられる。
前記外用組成物は、経皮適用できる製剤形態である限り、その製剤形態については、特に制限されず、液状、固形状、半固形状(クリーム状、ゲル状、軟膏状、ペースト状)等のいずれであってもよい。また、本発明の外用組成物は、水性製剤、油性製剤等の非乳化製剤であってもよく、また水中油型乳化製剤、油中水型乳化製剤等の乳化製剤であってもよい。
本発明の外用組成物は、メラニンの生成を抑制でき、皮膚のシミ、そばかす、くすみ、肝斑、老人性色素斑、物理的刺激による黒ずみ等の予防や改善が可能になっているので、美白用の外用組成物として好適に使用される。
L−アスコルビン酸2−グルコシド:商品名「AA2G」(株式会社林原製)
ホオノキ抽出物:商品名「ファルコレックス ホオノキB」(一丸ファルコス株式会社製)、液状、乾燥固形分濃度0.175重量%、ホオノキ(Magnolia obovata Thunberg(Magnoliaceae))の樹皮(和厚朴)を1,3−ブチレングリコール水溶液を用いて溶媒抽出処理して得られた抽出物
プルーン抽出物:商品名「クレアージュ」(一丸ファルコス株式会社製)、液状、乾燥固形分濃度7.78重量%、プルーン(セイヨウスモモ(Prunus domestica Lindl.(Rosaceae)))の果肉を繊維素分解酵素で分解して得られるものに、水及び1,3−ブチレングリコールを加えることにより得られた抽出物
アーティチョーク葉抽出物:商品名「バイオベネフィティ」(一丸ファルコス株式会社製)、液状、乾燥固形分濃度0.08重量%、チョウセンアザミ(Cynara scolymus L.(Compositae))の葉をエタノール溶液にて抽出して得られるエキスを濃縮、乾固して、1,3−ブチレングリコール溶液を加えることにより得られた抽出物
ヒメフウロ抽出物:商品名「プリンセスケア」(一丸ファルコス株式会社製)、液状、乾燥固形分濃度1重量%、ヒメフウロ(Geranium robertianum L.(Geraniaceae))の全草から1,3−ブチレングリコール溶液で抽出して得られた抽出物
アルピニア・カツマダイ種子抽出物:商品名「アルピニアホワイト」(一丸ファルコス株式会社製)、液状、乾燥固形分濃度0.2重量%、アルピニア・カツマダイ(Alpinia katsumadai Hayata(Zingiberaceae))の種子からエタノール溶液で抽出して得られるエキスを濃縮し、1,3−ブチレングリコール溶液を加えることにより得られた抽出物
チンピ抽出物:商品名「マンダリンクリア」(一丸ファルコス株式会社製)、液状、乾燥固形分濃度3重量%、マンダリンオレンジ(Citrus reticulate Blanco(Rutaceae))の成熟した果皮を1,3−ブチレングリコール溶液にて抽出して得られた抽出物
ビルベリー葉抽出物:商品名「キュアベリー」(一丸ファルコス株式会社製)、液状、乾燥固形分濃度0.2重量%、ビルベリー(Vaccinium myrtillus L.(Ericaceae))の葉から1,3−ブチレングリコール溶液で抽出して得られた抽出物
カルボキシビニルポリマー:商品名「「カーボポール980」(Lubrizol Advanced Materials社製)
アルキル変性カルボキシビニルポリマー:商品名「カーボポールultrez20」(Lubrizol Advanced Materials社製、アルキル基の炭素数:10〜30)
シリカ:商品名「ゴッドボールD−25C」(鈴木油脂工業株式会社製)、平均粒子径7〜10μm、比表面積300〜500m2/g、吸油量70〜110ml/100g
三次元培養皮膚モデル(MEL−300−A、MatTek社製)を用いて、メラニン生成抑制効果については評価した。具体的な試験方法は以下の通りである。
MTT試験により細胞生存率を測定した。具体的には、0.75mlのMTT試験薬と8.25mlの維持培地(EPI-100LLMM)を混合し、1ウェル当たり300μlとなるように添加した。皮膚モデルカップを、前記で調製したMTTの入った培地に移し、正確に3時間インキュベーターにて培養した。その後、組織の底面をPBS洗浄液で軽く洗浄して新しいプレートに移した。0.04N HCl酸性イソプロパノールを1mlずつ皮膚モデルカップの内側に添加し、蒸発しないようにプレートにカバーシールを貼り遮光して一晩インキュベーターにてブルーホルマザンを抽出した。抽出後、イソプロパノールをよく混ぜ合わせ、その内の200μlを96ウェルプレートに移した。マイクロプレートリーダーで570nmと620nmの光学濃度を測定し、それらの差をもって細胞活性とした。
MEL-300皮膚モデルカップをPBSで洗浄後、メスで細胞組織を剥離して回収した。得られた細胞組織をPBSに浸し、破砕及び遠心(2,000rpm、10分)を行った。その後、上清を取り除き、更にエタノールとジメチルエーテルの混合液(エタノール:ジメチルエーテル=3:1(容量比))を加えて、撹拌及び遠心(2,000rpm、10分)を行った。次いで、上清を取り除き、乾燥させた。乾燥物に1N水酸化ナトリウム水溶液(10重量%DMSO含有)を添加し、90℃の水浴にて20分間処理し、加熱溶融させた。その後、加熱溶融させた溶液をボルテックスにて軽く撹拌し、室温まで冷却した後に、405nmの吸光度を測定し、メラニン生成量を求めた。
表3及び4に示す組成の皮膚化粧料(液剤)を調製した。具体的には、製造手順は以下の通りである。精製水にカルボキシビニルポリマー及びアルキル変性カルボキシビニルポリマーを撹拌溶解させた後に、グリセリンを加えて撹拌溶解させて、調製物Aを得た。別途、1,3−ブチレングリコールに、トリメチルグリシン及び/又はシリカを加え、撹拌混合して均一化し、調製物Bを得た。次いで、調製物Aを撹拌しながら、調製物Bを加え、ホモミキサーで撹拌し、均一化した。更に、水酸化カリウムを加えてpHを6.5に調整した後に、L−アスコルビン酸2−グルコシド、ホオノキ抽出物、及びプルーン抽出物を加えて撹拌し、均一化することにより、皮膚化粧料を調製した。
<塗布時>
・塗布感
絡み付くような塗布感/ゲルを潰すような塗布感がない「1」
絡み付くような塗布感/ゲルを潰すような塗布感がある「10」
・さっぱり感
さっぱりとした感じがない「1」
さっぱりとした感じがある「10」
・べたつき感のなさ
べたつきを感じる「1」
べたつきを感じない「10」
<塗布から30秒後>
・粉っぽさのなさ
粉っぽさを感じる「1」
粉っぽさを感じない「10」
・保湿感
保湿感(しっとりとした感じ)がない「1」
保湿感(しっとりとした感じ)がある「l0」
表5に記載の処方に従い、常法にて皮膚化粧料を調製した(処方例1〜6はpH6.5、処方例7〜9はpH4.5)。
表6に記載の処方に従い、以下の手順で皮膚化粧料を調製した。
工程(1):精製水にL−アスコルビン酸2−グルコシド又はリン酸L−アスコルビルマグネシウムを溶解し、次いで、精製水に水酸化カリウムを溶解した液でpHを6に調整した(調製物(A−1))。
工程(2):(B)、(C)をそれぞれ加熱撹拌溶解した(調製物(B)、調製物(C))。
工程(3):調製物(B)を加熱撹拌しながら調製物(C)を加え、ホモミキサーで撹拌均一化した。
工程(4):その後、撹拌しながら徐々に40℃以下まで冷却し、調製物(A−1)と(A)の残りを加え、撹拌均一化し皮膚化粧料を調製した。
Claims (6)
- (A)アスコルビン酸及び/又はその誘導体、並びに(B)モクレン科モクレン属植物の抽出物を含有することを特徴とする、外用組成物。
- 更に、(C)バラ科サクラ属植物の抽出物を含有する、請求項1に記載の外用組成物。
- 前記(B)成分が、ホオノキの抽出物である、請求項1又は2に記載の外用組成物。
- 前記(C)成分が、プルーンの抽出物である、請求項1〜3のいずれかに記載の外用組成物。
- 前記(A)成分が、アスコルビン酸2−グルコシドである、請求項1〜4のいずれかに記載の外用組成物。
- 美白用である、請求項1〜5のいずれかに記載の外用組成物。
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