JP2020105130A - 外用乳化組成物 - Google Patents
外用乳化組成物 Download PDFInfo
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- JP2020105130A JP2020105130A JP2018246716A JP2018246716A JP2020105130A JP 2020105130 A JP2020105130 A JP 2020105130A JP 2018246716 A JP2018246716 A JP 2018246716A JP 2018246716 A JP2018246716 A JP 2018246716A JP 2020105130 A JP2020105130 A JP 2020105130A
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- weight
- emulsion composition
- fatty acid
- oil
- ceramide
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- 239000000203 mixture Substances 0.000 title claims abstract description 132
- 239000000839 emulsion Substances 0.000 title claims abstract description 103
- 235000014113 dietary fatty acids Nutrition 0.000 claims abstract description 115
- 239000000194 fatty acid Substances 0.000 claims abstract description 115
- 229930195729 fatty acid Natural products 0.000 claims abstract description 115
- 150000004665 fatty acids Chemical class 0.000 claims abstract description 64
- 229940106189 ceramide Drugs 0.000 claims abstract description 57
- YDNKGFDKKRUKPY-JHOUSYSJSA-N C16 ceramide Natural products CCCCCCCCCCCCCCCC(=O)N[C@@H](CO)[C@H](O)C=CCCCCCCCCCCCCC YDNKGFDKKRUKPY-JHOUSYSJSA-N 0.000 claims abstract description 55
- CRJGESKKUOMBCT-VQTJNVASSA-N N-acetylsphinganine Chemical compound CCCCCCCCCCCCCCC[C@@H](O)[C@H](CO)NC(C)=O CRJGESKKUOMBCT-VQTJNVASSA-N 0.000 claims abstract description 55
- ZVEQCJWYRWKARO-UHFFFAOYSA-N ceramide Natural products CCCCCCCCCCCCCCC(O)C(=O)NC(CO)C(O)C=CCCC=C(C)CCCCCCCCC ZVEQCJWYRWKARO-UHFFFAOYSA-N 0.000 claims abstract description 55
- VVGIYYKRAMHVLU-UHFFFAOYSA-N newbouldiamide Natural products CCCCCCCCCCCCCCCCCCCC(O)C(O)C(O)C(CO)NC(=O)CCCCCCCCCCCCCCCCC VVGIYYKRAMHVLU-UHFFFAOYSA-N 0.000 claims abstract description 55
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 50
- 238000005191 phase separation Methods 0.000 claims abstract description 32
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- 125000004432 carbon atom Chemical group C* 0.000 claims description 22
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- 150000003839 salts Chemical class 0.000 description 5
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 4
- 239000004166 Lanolin Substances 0.000 description 4
- 239000005639 Lauric acid Substances 0.000 description 4
- 239000000654 additive Substances 0.000 description 4
- 230000004888 barrier function Effects 0.000 description 4
- 150000001875 compounds Chemical class 0.000 description 4
- GHVNFZFCNZKVNT-UHFFFAOYSA-N decanoic acid Chemical compound CCCCCCCCCC(O)=O GHVNFZFCNZKVNT-UHFFFAOYSA-N 0.000 description 4
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- KWIUHFFTVRNATP-UHFFFAOYSA-N Betaine Natural products C[N+](C)(C)CC([O-])=O KWIUHFFTVRNATP-UHFFFAOYSA-N 0.000 description 3
- 239000004375 Dextrin Substances 0.000 description 3
- 229920001353 Dextrin Polymers 0.000 description 3
- KWIUHFFTVRNATP-UHFFFAOYSA-O N,N,N-trimethylglycinium Chemical compound C[N+](C)(C)CC(O)=O KWIUHFFTVRNATP-UHFFFAOYSA-O 0.000 description 3
- 229910019142 PO4 Inorganic materials 0.000 description 3
- 235000019482 Palm oil Nutrition 0.000 description 3
- ULUAUXLGCMPNKK-UHFFFAOYSA-N Sulfobutanedioic acid Chemical class OC(=O)CC(C(O)=O)S(O)(=O)=O ULUAUXLGCMPNKK-UHFFFAOYSA-N 0.000 description 3
- PHYFQTYBJUILEZ-UHFFFAOYSA-N Trioleoylglycerol Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC(OC(=O)CCCCCCCC=CCCCCCCCC)COC(=O)CCCCCCCC=CCCCCCCCC PHYFQTYBJUILEZ-UHFFFAOYSA-N 0.000 description 3
- WNLRTRBMVRJNCN-UHFFFAOYSA-L adipate(2-) Chemical compound [O-]C(=O)CCCCC([O-])=O WNLRTRBMVRJNCN-UHFFFAOYSA-L 0.000 description 3
- 125000000217 alkyl group Chemical group 0.000 description 3
- 235000001014 amino acid Nutrition 0.000 description 3
- 239000003945 anionic surfactant Substances 0.000 description 3
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- 239000003093 cationic surfactant Substances 0.000 description 3
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- 235000019864 coconut oil Nutrition 0.000 description 3
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- 235000019425 dextrin Nutrition 0.000 description 3
- MTHSVFCYNBDYFN-UHFFFAOYSA-N diethylene glycol Chemical compound OCCOCCO MTHSVFCYNBDYFN-UHFFFAOYSA-N 0.000 description 3
- PRAKJMSDJKAYCZ-UHFFFAOYSA-N dodecahydrosqualene Natural products CC(C)CCCC(C)CCCC(C)CCCCC(C)CCCC(C)CCCC(C)C PRAKJMSDJKAYCZ-UHFFFAOYSA-N 0.000 description 3
- POULHZVOKOAJMA-UHFFFAOYSA-M dodecanoate Chemical compound CCCCCCCCCCCC([O-])=O POULHZVOKOAJMA-UHFFFAOYSA-M 0.000 description 3
- YRIUSKIDOIARQF-UHFFFAOYSA-N dodecyl benzenesulfonate Chemical compound CCCCCCCCCCCCOS(=O)(=O)C1=CC=CC=C1 YRIUSKIDOIARQF-UHFFFAOYSA-N 0.000 description 3
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- ASWBNKHCZGQVJV-UHFFFAOYSA-N (3-hexadecanoyloxy-2-hydroxypropyl) 2-(trimethylazaniumyl)ethyl phosphate Chemical compound CCCCCCCCCCCCCCCC(=O)OCC(O)COP([O-])(=O)OCC[N+](C)(C)C ASWBNKHCZGQVJV-UHFFFAOYSA-N 0.000 description 2
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 2
- FFJCNSLCJOQHKM-CLFAGFIQSA-N (z)-1-[(z)-octadec-9-enoxy]octadec-9-ene Chemical compound CCCCCCCC\C=C/CCCCCCCCOCCCCCCCC\C=C/CCCCCCCC FFJCNSLCJOQHKM-CLFAGFIQSA-N 0.000 description 2
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- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 2
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- 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
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
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- A—HUMAN NECESSITIES
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- 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
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
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Abstract
Description
項1. (A)セラミド2重量%以上、(B)高級アルコール、(C)高級脂肪酸、及び(D)非イオン性界面活性剤を含有する、外用乳化組成物。
項2. 前記(B)成分として、少なくとも炭素数10〜24の直鎖状アルコールを含む、項1に記載の外用乳化組成物。
項3. 前記(B)成分として、炭素数10〜24の直鎖状アルコール及び炭素数10〜24の分岐状アルコールを含む、項1又は2に記載の外用乳化組成物。
項4. 前記(C)成分が、炭素数10〜24の脂肪酸である、項1〜3のいずれかに記載の外用乳化組成物。
項5. 前記(D)成分として、少なくともポリグリセリン脂肪酸エステルを含む、項1〜4のいずれかに記載の外用乳化組成物。
項6. 前記(D)成分として、ポリグリセリン脂肪酸エステル及びグリセリン脂肪酸エステルを含む、項1〜5のいずれかに記載の外用乳化組成物。
項7. 水中油型乳化形態である、項1〜6のいずれかに記載の外用乳化組成物。
項8. 前記(A)成分を2〜10重量%、前記(B)成分を3〜12.5重量%、前記(C)成分を0.5〜5重量%、及び前記(D)成分を0.5〜3重量%含む、項7に記載の外用乳化組成物。
項9. 前記(A)成分1重量部当たり、前記(B)成分を0.3〜6.25重量部、前記(C)成分を0.05〜2.5重量部、及び前記(D)成分を0.05〜1.5重量部の比率で含む、項7又は8に記載の外用乳化組成物。
項10. セラミドを2重量%以上含む外用乳化組成物において析出物の生成を抑制する方法であって、
外用乳化組成物において、(A)セラミド2重量%以上と共に、(B)高級アルコール、(C)高級脂肪酸、及び(D)非イオン性界面活性剤を配合する、析出物の生成抑制方法。
項11. セラミドを2重量%以上含む外用乳化組成物において相分離を抑制する方法であって、
外用乳化組成物において、(A)セラミド2重量%以上と共に、(B)高級アルコール、(C)高級脂肪酸、及び(D)非イオン性界面活性剤を配合する、相分離の抑制方法。
本発明の外用乳化組成物は、セラミド(以下、(A)成分と表記することもある)2重量%以上、高級アルコール(以下、(B)成分と表記することもある)、高級脂肪酸(以下、(C)成分と表記することもある)、及び非イオン性界面活性剤(以下、(D)成分と表記することもある)を含むことを特徴とする。以下、本発明の外用乳化組成物について詳述する。
本発明の外用乳化組成物は、2重量%以上のセラミドを含む。本発明の外用乳化組成物において、セラミドは油相に含まれる。
本発明の外用乳化組成物は、高級アルコールを含む。本発明の外用乳化組成物において、高級アルコールは油相に含まれる。
本発明の外用乳化組成物は、高級脂肪酸を含む。本発明の外用乳化組成物において、高級脂肪酸は油相に含まれる。
本発明の外用乳化組成物は、非イオン性界面活性剤を含む。本発明の外用乳化組成物において、非イオン性界面活性剤は、乳化粒子を形成させ、乳化状態にする役割を果たす。
ポリオキシエチレンポリオキシプロピレンアルキルエーテルとしては、具体的には、PPG−4セテス−1等が挙げられる。
本発明の外用乳化組成物は、油相には、前記成分に加えて、更に液状油(前記(B)又は(C)成分に該当しない油分)を含んでいてもよい。液状油とは、25℃において液状の形態を保つ油である。
本発明の外用乳化組成物は、油相には、前記成分に加えて、更に固形油(前記(B)又は(C)成分に該当しない油分)を含んでいてもよい。固形油とは、25℃において固形の形態を保つ油である。
本発明の外用乳化組成物には、保湿性の向上等のために、必要に応じて多価アルコールが含まれていてもよい。本発明の外用乳化組成物において、多価アルコールは水相に含有される。
本発明の外用乳化組成物は、前述する成分の他に、粘性の調節等のために、必要に応じて、増粘剤が含まれていてもよい。本発明の外用乳化組成物において、増粘剤は水相に含有される。
本発明の外用乳化組成物には、必要に応じて、前記(C)成分以外の界面活性剤が含まれていてもよい。このような界面活性剤としては、具体的には、陰イオン性界面活性剤、陽イオン性界面活性剤、両性界面活性剤等が挙げられる。
本発明の外用乳化組成物は、乳化された状態で水相を形成するために、水を含有する。
本発明の外用乳化組成物は、前述する成分の他に、薬学的又は香粧学的な生理機能を発揮できる薬効成分が、必要に応じて、含まれていてもよい。このような薬効成分としては、例えば、ステロイド剤(デキサメタゾン、塩酸デキサメタゾン、酢酸デキサメタゾン、塩酸ヒドロコルチゾン、吉草酸プレドニゾロン、酢酸プレドニゾロン等)、抗ヒスタミン剤(ジフェンヒドラミン、塩酸ジフェンヒドラミン、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、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、安息香酸アルキルエステル(例えばアミノ安息香酸エチル、塩酸パラブチルアミノ安息香酸ジエチルアミノエチル)、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、サリチル酸、サリチル酸グリコール、サリチル酸メチル、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等)、殺菌剤(塩化ベンザルコニウム、塩化デカリニウム、塩化ベンゼトニウム、塩化セチルピリジニウム、イソプロピルメチルフェノール、塩酸クロルヘキシジン、グルコン酸クロルヘキシジン、アンモニア水、スルファジアジン、乳酸、フェノール等)、鎮痒剤(クロタミトン、チアントール等)、皮膚保護剤(コロジオン、ヒマシ油等)、血行促進成分(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)、ビタミン類(ビタミンA,B,C,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。これらの薬効成分は、1種単独で使用してもよく、また2種以上を組み合わせて使用してもよい。また、本発明の外用乳化組成物において、これらの薬効成分を含有させる場合、その濃度については、使用する薬効成分の種類、期待する効果等に応じて適宜設定すればよい。
本発明の外用乳化組成物は、水中油型又は油中水型のいずれの乳化形態であってもよいが、析出や相分離の抑制効果、保湿効果及び使用感をより一層向上させるという観点から、好ましくは水中油型が挙げられる。
本発明の乳外用化組成物は、公知の乳化製剤の製造方法に従って製造することができる。本発明の外用乳化組成物の製造方法として、例えば、以下に示す方法が挙げられる。先ず、(A)成分、(B)成分、(C)成分、及び必要に応じて添加される他の油性成分を混合して油相用組成物を調製する。別途、水、及び必要に応じて添加される他の水溶性成分を混合して水相用組成物を調製する。なお、(D)成分は、前記水相用組成物又は油相用組成物のいずれか一方又は双方に配合していればよいが、水中油型の乳化形態の場合であれば前記油相用組成物に配合し、油中水型の乳化形態の場合であれば前記水相用組成物に配合しておくことが好ましい。次いで、得られた水相用組成物と油相用組成物を混合し、ホモジナイザー等の乳化手法によって乳化させることにより、本発明の外用乳化組成物が得られる。
本発明の析出物の生成抑制方法は、セラミドを2重量%以上含む外用乳化組成物において析出物の生成を抑制する方法であって、外用乳化組成物において、(A)セラミド2重量%以上と共に、(B)高級アルコール、(C)高級脂肪酸、及び(D)非イオン性界面活性剤を配合することを特徴とする。
表1に示す組成の外用乳化組成物(水中油型)を以下の手順で製造した。先ず、表1に示す各油相成分及び(D)成分を混合し、85℃で加熱溶解することにより、油相用組成物を調製した。また、別途、表1に示す各水相成分を混合し、85℃で加熱溶解することにより、水相用組成物を調製した。85℃に加熱した水相用組成物に、85℃に加熱した油相用組成物を徐々に添加しホモミキサーを用いて乳化させ、水中油型の外用乳化組成物を得た。
専門家の評価パネラー5名によって各外用乳化組成物の保湿効果及び使用感(柔らかさ)について評価した。具体的には、各外用乳化組成物0.5gを全顔に塗布し、保湿効果及び使用感(柔らかさ)について評価した。保湿効果の評価は、「塗布後の保湿効果の総合的な評価」が「良い」を5点、「やや良い」を4点、「どちらでもない」を3点、「やや悪い」を2点、「悪い」を1点として、1〜5点の5段階で評点化することにより行った。また、使用感(柔らかさ)の評価は、「外用乳化組成物の柔らかさと塗布時の肌に馴染ませ易さの総合的な評価」が「良い」を5点、「やや良い」を4点、「どちらでもない」を3点、「やや悪い」を2点、「悪い」を1点として、1〜5点の5段階で評点化することにより行った。評価パネラー5名の各評点を合計し、以下の分類に従って判定した。
(保湿効果及び使用感(柔らかさ)の分類基準)
○:評点の合計が20以上
△:評点の合計が15以上20未満
×:評点の合計が15未満
製造直後の各外用乳化組成物の外観を目視で観察し、以下の分類に従って判定した。
(析出抑制効果の分類基準)
○:析出物が全く認められない。
△:僅かにだけ析出物が認められる。
×:多くの析出物が認められる。
製造直後の各外用乳化組成物を、遮光条件下において40℃で60日間保存した。保存後の各外用乳化組成物の外観を目視で観察し、以下の分類に従って判定した。なお、以下の分類に示す「相分離」とは、外観上一様でなく複数の領域に分離して見えることをいう。
(保存安定性(相分離の程度)の分類基準)
○:相分離が認められず、製造直後と同じ乳化状態を維持している。
△:僅かにだけ相分離が認められるが、製造直後とほとんど同じ乳化状態を維持している。
×:著しい相分離が認められ、乳化状態を安定に維持できていない。
表2に示す組成の外用乳化組成物(水中油型)を前記試験例1と同様の方法で調製した。得られた外用乳化組成物を前記試験例1と同様の方法で評価したところ、いずれも、優れた保湿効果、使用感(柔らかさ)、析出抑制効果、及び保存安定性(相分離の程度)を有していた。
Claims (11)
- (A)セラミド2重量%以上、(B)高級アルコール、(C)高級脂肪酸、及び(D)非イオン性界面活性剤を含有する、外用乳化組成物。
- 前記(B)成分として、少なくとも炭素数10〜24の直鎖状アルコールを含む、請求項1に記載の外用乳化組成物。
- 前記(B)成分として、炭素数10〜24の直鎖状アルコール及び炭素数10〜24の分岐状アルコールを含む、請求項1又は2に記載の外用乳化組成物。
- 前記(C)成分が、炭素数10〜24の脂肪酸である、請求項1〜3のいずれかに記載の外用乳化組成物。
- 前記(D)成分として、少なくともポリグリセリン脂肪酸エステルを含む、請求項1〜4のいずれかに記載の外用乳化組成物。
- 前記(D)成分として、ポリグリセリン脂肪酸エステル及びグリセリン脂肪酸エステルを含む、請求項1〜5のいずれかに記載の外用乳化組成物。
- 水中油型乳化形態である、請求項1〜6のいずれかに記載の外用乳化組成物。
- 前記(A)成分を2〜10重量%、前記(B)成分を3〜12.5重量%、前記(C)成分を0.5〜5重量%、及び前記(D)成分を0.5〜3重量%含む、請求項7に記載の外用乳化組成物。
- 前記(A)成分1重量部当たり、前記(B)成分を0.3〜6.25重量部、前記(C)成分を0.05〜2.5重量部、及び前記(D)成分を0.05〜1.5重量部の比率で含む、請求項7又は8に記載の外用乳化組成物。
- セラミドを2重量%以上含む外用乳化組成物において析出物の生成を抑制する方法であって、
外用乳化組成物において、(A)セラミド2重量%以上と共に、(B)高級アルコール、(C)高級脂肪酸、及び(D)非イオン性界面活性剤を配合する、析出物の生成抑制方法。 - セラミドを2重量%以上含む外用乳化組成物において相分離を抑制する方法であって、
外用乳化組成物において、(A)セラミド2重量%以上と共に、(B)高級アルコール、(C)高級脂肪酸、及び(D)非イオン性界面活性剤を配合する、相分離の抑制方法。
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