TWI572365B - Cosmetics - Google Patents
Cosmetics Download PDFInfo
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- TWI572365B TWI572365B TW101100204A TW101100204A TWI572365B TW I572365 B TWI572365 B TW I572365B TW 101100204 A TW101100204 A TW 101100204A TW 101100204 A TW101100204 A TW 101100204A TW I572365 B TWI572365 B TW I572365B
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- cosmetic
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- 239000002537 cosmetic Substances 0.000 title claims description 41
- 229940106189 ceramide Drugs 0.000 claims description 31
- YDNKGFDKKRUKPY-JHOUSYSJSA-N C16 ceramide Natural products CCCCCCCCCCCCCCCC(=O)N[C@@H](CO)[C@H](O)C=CCCCCCCCCCCCCC YDNKGFDKKRUKPY-JHOUSYSJSA-N 0.000 claims description 26
- 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 description 26
- VVGIYYKRAMHVLU-UHFFFAOYSA-N newbouldiamide Natural products CCCCCCCCCCCCCCCCCCCC(O)C(O)C(O)C(CO)NC(=O)CCCCCCCCCCCCCCCCC VVGIYYKRAMHVLU-UHFFFAOYSA-N 0.000 claims description 26
- CRJGESKKUOMBCT-VQTJNVASSA-N N-acetylsphinganine Chemical compound CCCCCCCCCCCCCCC[C@@H](O)[C@H](CO)NC(C)=O CRJGESKKUOMBCT-VQTJNVASSA-N 0.000 claims description 25
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 15
- 239000000126 substance Substances 0.000 claims description 13
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims description 12
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims description 12
- 150000007524 organic acids Chemical class 0.000 claims description 11
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 claims description 9
- 238000002844 melting Methods 0.000 claims description 9
- 230000008018 melting Effects 0.000 claims description 9
- 238000010438 heat treatment Methods 0.000 claims description 8
- 238000004519 manufacturing process Methods 0.000 claims description 8
- 239000002253 acid Substances 0.000 claims description 7
- 238000002156 mixing Methods 0.000 claims description 7
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims description 6
- 235000012000 cholesterol Nutrition 0.000 claims description 6
- 150000001413 amino acids Chemical class 0.000 claims description 5
- 238000001816 cooling Methods 0.000 claims description 5
- 150000002148 esters Chemical class 0.000 claims description 5
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims description 3
- GYTGJCPXNGAJFT-UHFFFAOYSA-N 2-octadec-1-enylbutanedioic acid Chemical compound CCCCCCCCCCCCCCCCC=CC(C(O)=O)CC(O)=O GYTGJCPXNGAJFT-UHFFFAOYSA-N 0.000 claims 1
- AAHZZGHPCKJNNZ-UHFFFAOYSA-N Hexadecenylsuccinicacid Chemical compound CCCCCCCCCCCCCCC=CC(C(O)=O)CC(O)=O AAHZZGHPCKJNNZ-UHFFFAOYSA-N 0.000 claims 1
- 150000001991 dicarboxylic acids Chemical class 0.000 claims 1
- -1 pyridyl cation Chemical class 0.000 description 34
- 239000000203 mixture Substances 0.000 description 20
- 210000003491 skin Anatomy 0.000 description 19
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 15
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 15
- 239000004094 surface-active agent Substances 0.000 description 13
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 12
- 125000000217 alkyl group Chemical group 0.000 description 12
- 229910052799 carbon Inorganic materials 0.000 description 12
- 125000004432 carbon atom Chemical group C* 0.000 description 12
- 235000014113 dietary fatty acids Nutrition 0.000 description 11
- 229930195729 fatty acid Natural products 0.000 description 11
- 239000000194 fatty acid Substances 0.000 description 11
- 210000000434 stratum corneum Anatomy 0.000 description 10
- 150000002430 hydrocarbons Chemical group 0.000 description 8
- 230000014759 maintenance of location Effects 0.000 description 8
- 230000000694 effects Effects 0.000 description 7
- 150000002632 lipids Chemical class 0.000 description 7
- 229920006395 saturated elastomer Polymers 0.000 description 7
- 238000005406 washing Methods 0.000 description 7
- 229930182558 Sterol Natural products 0.000 description 6
- 239000002585 base Substances 0.000 description 6
- 125000000913 palmityl 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])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 6
- 150000003432 sterols Chemical class 0.000 description 6
- 235000003702 sterols Nutrition 0.000 description 6
- 125000004122 cyclic group Chemical group 0.000 description 5
- 150000004665 fatty acids Chemical class 0.000 description 5
- 239000000463 material Substances 0.000 description 5
- 229930195734 saturated hydrocarbon Natural products 0.000 description 5
- 229930195735 unsaturated hydrocarbon Natural products 0.000 description 5
- 206010013786 Dry skin Diseases 0.000 description 4
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerol Natural products OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 4
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 4
- OFOBLEOULBTSOW-UHFFFAOYSA-N Malonic acid Chemical compound OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 4
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 4
- 125000003545 alkoxy group Chemical group 0.000 description 4
- 229940024606 amino acid Drugs 0.000 description 4
- 235000001014 amino acid Nutrition 0.000 description 4
- 150000001783 ceramides Chemical class 0.000 description 4
- 150000001875 compounds Chemical class 0.000 description 4
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 description 4
- 125000005113 hydroxyalkoxy group Chemical group 0.000 description 4
- 239000004615 ingredient Substances 0.000 description 4
- 238000010979 pH adjustment Methods 0.000 description 4
- 125000002958 pentadecyl 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])C([H])([H])C([H])([H])[H] 0.000 description 4
- 238000003860 storage Methods 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- ATGQXSBKTQANOH-UWVGARPKSA-N N-oleoylphytosphingosine Chemical compound CCCCCCCCCCCCCC[C@@H](O)[C@@H](O)[C@H](CO)NC(=O)CCCCCCC\C=C/CCCCCCCC ATGQXSBKTQANOH-UWVGARPKSA-N 0.000 description 3
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 description 3
- 229920002125 Sokalan® Polymers 0.000 description 3
- 125000003342 alkenyl group Chemical group 0.000 description 3
- 150000001408 amides Chemical class 0.000 description 3
- 239000003945 anionic surfactant Substances 0.000 description 3
- 230000002490 cerebral effect Effects 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 230000000052 comparative effect Effects 0.000 description 3
- 238000002425 crystallisation Methods 0.000 description 3
- 230000008025 crystallization Effects 0.000 description 3
- 230000007794 irritation Effects 0.000 description 3
- 210000002510 keratinocyte Anatomy 0.000 description 3
- 150000007522 mineralic acids Chemical class 0.000 description 3
- 239000002736 nonionic surfactant Substances 0.000 description 3
- 239000003921 oil Substances 0.000 description 3
- 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 description 3
- 230000035699 permeability Effects 0.000 description 3
- 150000003904 phospholipids Chemical class 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- WWUZIQQURGPMPG-KRWOKUGFSA-N sphingosine Chemical compound CCCCCCCCCCCCC\C=C\[C@@H](O)[C@@H](N)CO WWUZIQQURGPMPG-KRWOKUGFSA-N 0.000 description 3
- WWUZIQQURGPMPG-UHFFFAOYSA-N (-)-D-erythro-Sphingosine Natural products CCCCCCCCCCCCCC=CC(O)C(N)CO WWUZIQQURGPMPG-UHFFFAOYSA-N 0.000 description 2
- BQPPJGMMIYJVBR-UHFFFAOYSA-N (10S)-3c-Acetoxy-4.4.10r.13c.14t-pentamethyl-17c-((R)-1.5-dimethyl-hexen-(4)-yl)-(5tH)-Delta8-tetradecahydro-1H-cyclopenta[a]phenanthren Natural products CC12CCC(OC(C)=O)C(C)(C)C1CCC1=C2CCC2(C)C(C(CCC=C(C)C)C)CCC21C BQPPJGMMIYJVBR-UHFFFAOYSA-N 0.000 description 2
- CHGIKSSZNBCNDW-UHFFFAOYSA-N (3beta,5alpha)-4,4-Dimethylcholesta-8,24-dien-3-ol Natural products CC12CCC(O)C(C)(C)C1CCC1=C2CCC2(C)C(C(CCC=C(C)C)C)CCC21 CHGIKSSZNBCNDW-UHFFFAOYSA-N 0.000 description 2
- ULQISTXYYBZJSJ-UHFFFAOYSA-N 12-hydroxyoctadecanoic acid Chemical compound CCCCCCC(O)CCCCCCCCCCC(O)=O ULQISTXYYBZJSJ-UHFFFAOYSA-N 0.000 description 2
- XYTLYKGXLMKYMV-UHFFFAOYSA-N 14alpha-methylzymosterol Natural products CC12CCC(O)CC1CCC1=C2CCC2(C)C(C(CCC=C(C)C)C)CCC21C XYTLYKGXLMKYMV-UHFFFAOYSA-N 0.000 description 2
- XDOFQFKRPWOURC-UHFFFAOYSA-N 16-methylheptadecanoic acid Chemical group CC(C)CCCCCCCCCCCCCCC(O)=O XDOFQFKRPWOURC-UHFFFAOYSA-N 0.000 description 2
- FPTJELQXIUUCEY-UHFFFAOYSA-N 3beta-Hydroxy-lanostan Natural products C1CC2C(C)(C)C(O)CCC2(C)C2C1C1(C)CCC(C(C)CCCC(C)C)C1(C)CC2 FPTJELQXIUUCEY-UHFFFAOYSA-N 0.000 description 2
- FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Chemical compound CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 2
- BKLIAINBCQPSOV-UHFFFAOYSA-N Gluanol Natural products CC(C)CC=CC(C)C1CCC2(C)C3=C(CCC12C)C4(C)CCC(O)C(C)(C)C4CC3 BKLIAINBCQPSOV-UHFFFAOYSA-N 0.000 description 2
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 description 2
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- ODKSFYDXXFIFQN-BYPYZUCNSA-N L-arginine Chemical compound OC(=O)[C@@H](N)CCCN=C(N)N ODKSFYDXXFIFQN-BYPYZUCNSA-N 0.000 description 2
- 229930064664 L-arginine Natural products 0.000 description 2
- 235000014852 L-arginine Nutrition 0.000 description 2
- LOPKHWOTGJIQLC-UHFFFAOYSA-N Lanosterol Natural products CC(CCC=C(C)C)C1CCC2(C)C3=C(CCC12C)C4(C)CCC(C)(O)C(C)(C)C4CC3 LOPKHWOTGJIQLC-UHFFFAOYSA-N 0.000 description 2
- OYHQOLUKZRVURQ-HZJYTTRNSA-N Linoleic acid Chemical compound CCCCC\C=C/C\C=C/CCCCCCCC(O)=O OYHQOLUKZRVURQ-HZJYTTRNSA-N 0.000 description 2
- BBAFBDLICMHBNU-MFZOPHKMSA-N N-(2-hydroxyoctadecanoyl)-4-hydroxysphinganine Chemical compound CCCCCCCCCCCCCCCCC(O)C(=O)N[C@@H](CO)[C@H](O)[C@H](O)CCCCCCCCCCCCCC BBAFBDLICMHBNU-MFZOPHKMSA-N 0.000 description 2
- CAHGCLMLTWQZNJ-UHFFFAOYSA-N Nerifoliol Natural products CC12CCC(O)C(C)(C)C1CCC1=C2CCC2(C)C(C(CCC=C(C)C)C)CCC21C CAHGCLMLTWQZNJ-UHFFFAOYSA-N 0.000 description 2
- LCTONWCANYUPML-UHFFFAOYSA-N Pyruvic acid Chemical compound CC(=O)C(O)=O LCTONWCANYUPML-UHFFFAOYSA-N 0.000 description 2
- 239000013543 active substance Substances 0.000 description 2
- 150000005215 alkyl ethers Chemical class 0.000 description 2
- 125000000129 anionic group Chemical group 0.000 description 2
- 229940099417 ceramide 2 Drugs 0.000 description 2
- 150000001840 cholesterol esters Chemical class 0.000 description 2
- 238000004140 cleaning Methods 0.000 description 2
- 125000002704 decyl group Chemical group [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])* 0.000 description 2
- QBSJHOGDIUQWTH-UHFFFAOYSA-N dihydrolanosterol Natural products CC(C)CCCC(C)C1CCC2(C)C3=C(CCC12C)C4(C)CCC(C)(O)C(C)(C)C4CC3 QBSJHOGDIUQWTH-UHFFFAOYSA-N 0.000 description 2
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 description 2
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- 229940049906 glutamate Drugs 0.000 description 2
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- 125000003976 glyceryl group Chemical group [H]C([*])([H])C(O[H])([H])C(O[H])([H])[H] 0.000 description 2
- CBFCDTFDPHXCNY-UHFFFAOYSA-N icosane Chemical compound CCCCCCCCCCCCCCCCCCCC CBFCDTFDPHXCNY-UHFFFAOYSA-N 0.000 description 2
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- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
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- CAHGCLMLTWQZNJ-RGEKOYMOSA-N lanosterol Chemical compound C([C@]12C)C[C@@H](O)C(C)(C)[C@H]1CCC1=C2CC[C@]2(C)[C@H]([C@H](CCC=C(C)C)C)CC[C@@]21C CAHGCLMLTWQZNJ-RGEKOYMOSA-N 0.000 description 2
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- 125000001434 methanylylidene group Chemical group [H]C#[*] 0.000 description 2
- 125000001421 myristyl 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])C([H])([H])[H] 0.000 description 2
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- 125000004079 stearyl 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])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 2
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- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
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- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
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- 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
- A61K8/63—Steroids; Derivatives thereof
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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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
- A61K8/68—Sphingolipids, e.g. ceramides, cerebrosides, gangliosides
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- A—HUMAN NECESSITIES
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- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
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Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
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Description
本發明係關於一種化粧料。
存在於皮膚之最外層中之角質層具有如下功能:藉由抑制來自外部之物質之進入、來自皮膚內部之水分之蒸發,同時自身保持水分,而保持皮膚之柔軟性或光滑外觀。被稱作角質細胞間脂質(以下,記載為角質層ICL(intercellular lipid,細胞間脂質))之脂質以填補角質細胞之間隙的方式存在於構成角質層之角質細胞之間隙中。
該角質層ICL之脂質組成之約50%為腦醯胺,其他包含膽固醇、膽固醇酯、脂肪酸等。已知,通常若角質層ICL、尤其是腦醯胺減少,則會引起粗糙皮膚、乾燥皮膚、老化皮膚等欠佳之皮膚狀態,藉由以外用之方式補充腦醯胺作為角質層功能之改善成分,可改善功能下降之角質層狀態(非專利文獻1、非專利文獻2)。
然而,由於腦醯胺結晶性較強,且熔點較高,故而存在難以於製劑中穩定化之問題。因此,為於皮膚外用劑中穩定地調配腦醯胺,需要與界面活性劑或多種、多量之油劑等併用,其結果為無法避免使用感之下降、製劑之性狀受到限定。
於專利文獻1中,雖然記載有以磷脂質或合成界面活性劑等使包含腦醯胺之角質層ICL穩定化,但由於使用合成界面活性劑,故而於安全性及使用感之方面存在問題。又,磷脂質本身亦存在易引起氧化或分解等問題。
又,於專利文獻2中,記載有若以存在於角質層ICL中之脂質之神經鞘胺醇類與酸來乳化腦醯胺類,則可穩定地保持腦醯胺類而使其不會結晶化。然而,若組合神經鞘胺醇類與酸,則顯示陽離子性,故而存在無法使陰離子性之物質共存等問題。
另一方面,雖然含固醇基之有機酸並非存在於角質層ICL中之脂質,但由於具有與膽固醇硫酸或膽固醇酯類似之結構,故而為與角質層之親和性較佳,滲透性較高者。
[非專利文獻1] J. Invest. Dermatol.,84: 282(1985)
[非專利文獻2] J. Invest. Dermatol.,87: 758(1986)
[專利文獻1]日本專利特開2001-48721號公報
[專利文獻2]日本專利特開2003-171269號公報
本發明提供一種化粧料,其含有如下成分(A)、(B)、(C)及(D):
(A)以通式(1)表示之有機酸0.001~50重量%
[化1]
[式中,R1表示具有1個羥基之天然固醇或其氫化物(以下稱作固醇類)、或者膽汁酸之去除羥基的氫原子後殘留之殘基,R2表示碳數1~24之2價烴基,M表示氫原子、鹼金屬、鹼土金屬、銨、總碳數2~9之烷醇銨、總碳數1~22之烷基銨或烯基銨、經碳數1~18之烷基或烯基取代之吡啶陽離子、或鹼性胺基酸]、
(B)鹼0.001~20重量%、
(C)腦醯胺類0.0001~50重量%、
(D)水,且
含有成分(A)以外之酸作為成分(E),其含量為0≦(E)/(A)<0.2,且組合物之pH值為6~11。
本發明之化粧料係可穩定地乳化腦醯胺類,穩定性優異,且粗糙皮膚改善效果較高者。又,為以特定之有機酸與鹼使其穩定化,亦可使陰離子性之物質共存。
本發明係關於一種可穩定地乳化腦醯胺類而使其不會結晶化,且皮膚粗糙改善效果較高之化粧料。
本發明者等人發現,只要以特定之有機酸與鹼來乳化腦醯胺類,則可穩定地乳化腦醯胺類而使其不會結晶化,進而可不添加天然或合成之界面活性劑或磷脂質等而穩定地保持腦醯胺,從而可獲得穩定性優異,且皮膚粗糙改善效果較高之化粧料。
本發明中所使用之成分(A)之有機酸係以上述通式(1)表示者。
於通式(1)中,作為以R1表示之具有1個羥基之天然固醇,例如可列舉:膽固醇、豆固醇、穀固醇、菜油固醇、羊毛固醇、羊毛固醇等,其中較佳為膽固醇。
又,於通式(1)中,R2為碳數1~24之2價烴基,可列舉直鏈或支鏈之伸烷基或伸烯基,較佳為以下式
[化2]
(式中,R3表示碳數6~20之直鏈或支鏈之烷基或烯基)表示之基(再者,均於右側之支鏈上鍵結有羧基)。
作為R3,可列舉:直鏈或支鏈之2-己烯基、2-辛烯基、2-癸烯基、2-十二烯基、2-十四烯基、2-十六烯基、2-十八烯基、2-二十烯基、己基、辛基、癸基、十二烷基、十四烷基、十六烷基、十八烷基、二十烷基等,其中較佳為2-十四烯基、2-十六烯基、2-十八烯基、2-二十烯基、十四烷基、十六烷基、十八烷基、二十烷基。
上述有機酸(1)例如可藉由根據日本專利特開平5-294989號公報中所記載之方法,使固醇類與烯基琥珀酸酐或烷基琥珀酸酐反應,並視需要以鹼性物質進行中和而獲得。
成分(A)可使用1種或2種以上,於總組成中含有0.001~50重量%,較佳為含有0.01~25重量%,更佳為含有0.1~10重量%。只要為該範圍內,則可獲得發黏等使用感之問題得到抑制之化粧料。
成分(A)藉由與下述成分(B)之作用可表現出如界面活性劑之功能,即便不含其他界面活性劑,亦可穩定地乳化成分(C)之腦醯胺類。因此,為乳化成分(C)之腦醯胺類,亦可不含其他界面活性劑。
作為本發明中所使用之成分(B)之鹼,只要為水溶性者,則並無限制,可為有機鹼,亦可為無機鹼。
作為有機鹼,較佳為選自L-精胺酸、離胺酸、組胺酸等鹼性胺基酸;單乙醇胺、二乙醇胺、三乙醇胺、胺基甲基丙醇、胺基甲基丙二醇、胺基乙基丙二醇、三羥基甲基胺基乙烷等烷醇胺中之1種或2種以上。又,作為無機鹼,較佳為選自氫氧化鈉、氫氧化鉀中之1種或2種。
於該等之中,較佳為選自鹼性胺基酸、氫氧化鈉、氫氧化鉀中之1種或2種以上,進而更佳為選自L-精胺酸、氫氧化鈉、氫氧化鉀中之1種或2種以上。
成分(B)之鹼可使用1種或組合2種以上使用,於總組成中含有0.001~20重量%,較佳為含有0.01~5重量%,更佳為含有0.01~3重量%。
成分(B)中和成分(A)而形成鹽。因此,成分(A)可引出如界面活性劑之作用。又,具有調整組合物整體之pH值之作用。
作為本發明中所使用之成分(C)之腦醯胺類,較佳為選自以如下通式(2)或(3)表示者中之1種或2種以上。
(I)以通式(2)表示之化合物亦可為源自天然之腦醯胺類或相同結構之合成物。
[化3]
(式中,R11表示可經羥基取代之碳數7~19之直鏈、支鏈或環狀的飽和或不飽和之烴基;Z1表示亞甲基或次甲基;X1、X2、及X3各自獨立地表示氫原子、羥基或乙醯氧基;X4表示氫原子,或與鄰接之氧原子一同形成側氧基(其中,於Z1為次甲基時,X1與X2之任一者為氫原子,另一者不存在。於X4形成側氧基時,X3不存在);R12表示羥基甲基或乙醯氧甲基;R13表示氫原子,或表示碳數1~4之烷基;R14為可經羥基取代之碳數5~30之直鏈、支鏈或環狀的飽和或不飽和之烴基,或表示於該烷基之ω末端酯鍵結有可經羥基取代之碳數8~22之直鏈或支鏈的飽和或不飽和之脂肪酸者;虛線部分表示亦可為不飽和鍵)。
較佳為列舉如下化合物:R11為碳數7~19、更佳為碳數13~15之直鏈烷基;R14為可經羥基取代之碳數9~27之直鏈烷基、或酯鍵結有亞麻油酸之碳數9~27之直鏈烷基。又,較佳為X4表示氫原子,或與氧原子一同形成側氧基。作為R14,較佳為二十三烷基、1-羥基十五烷基、1-羥基二十三烷基、十七烷基、1-羥基十一烷基、於ω位上酯鍵結有亞麻油酸之二十九烷基。
天然型腦醯胺較佳為選自神經鞘胺醇、二羥基神經鞘胺醇、植物神經鞘胺醇或鞘胺二醇(sphingadienine)經醯胺化之腦醯胺1~7型(例如J. Lipid Res.,24: 759(1983)之圖2、及J. Lipid. Res.,35: 2069(1994)之圖4所記載的豬及人類之腦醯胺類)中之1種或2種以上。
進而亦包含該等之N-烷基體(例如N-甲基體)。
該等腦醯胺可使用天然型(D(-)體)之光學活性物質,亦可使用非天然型(L(+)體)之光學活性物質,進而亦可使用天然型與非天然型之混合物。關於上述化合物之相對立體構型,可為天然型之立體構型者,亦可為其以外之非天然型之立體構型者,又,亦可為該等之混合物。其中,較佳為選自CERAMIDE 1、CERAMIDE 2、CERAMIDE 3、CERAMIDE 5、CERAMIDE 6II之化合物(以上記載於INCI(International Nomenclature of Cosmetic Ingredients,國際化妝品原料命名),第8版)及以下式表示者中之1種或2種以上。
[化4]
該等可為來自天然之萃取物及合成物中之任一種,可使用市售品。
於使用上述天然型腦醯胺之市售品之情形時,較佳為選自Ceramide I、Ceramide III、Ceramide IIIA、Ceramide IIIB、Ceramide IIIC、Ceramide VI(以上由Cosmofarm公司製造)、Ceramide TIC-001(高砂香料公司)、CERAMIDE II(Quest International公司)、DS-Ceramide VI、DS-CLA-Phytoceramide、C6-Phytoceramide、DS-ceramide Y3S(DOOSAN公司)、CERAMIDE 2(SEDERMA公司)中之1種或2種以上。
[化5]
(II)以通式(3)表示之模擬型腦醯胺。
[化6]
(式中,R15表示可經羥基取代之碳數10~22之直鏈、支鏈或環狀的飽和或不飽和之烴基或氫原子;X5表示氫原子、乙醯基或甘油基;R16為可經羥基或胺基取代之碳數5~22之直鏈、支鏈或環狀的飽和或不飽和之烴基,或表示於該烴基之ω末端酯鍵結有可經羥基取代之碳數8~22之直鏈或支鏈之飽和或不飽和的脂肪酸者;R17表示氫原子,或表示可經羥基、羥基烷氧基、烷氧基或乙醯氧基取代之總碳數1~30之烷基)
作為R16,較佳為壬基、十三烷基、十五烷基、於ω位上酯鍵結有亞麻油酸之十一烷基、於ω位上酯鍵結有亞麻油酸之十五烷基、於ω位上酯鍵結有12-羥基硬脂酸之十五烷基、於ω位上醯胺鍵結有甲基支鏈異硬脂酸之十一烷基。
R17較佳為於R15為氫原子之情形時,為可經羥基、羥基烷氧基、烷氧基或乙醯氧基取代之總碳數10~30之烷基、較佳為總碳數12~20之烷基,於R15為可經羥基取代之碳數10~22之直鏈、支鏈或環狀的飽和或不飽和之烴基之情形時,表示氫原子,或表示可經羥基、羥基烷氧基、烷氧基或乙醯氧基取代之總碳數1~8之烷基。作為R17之羥基烷氧基或烷氧基,較佳為碳數1~7者。
[化7]
作為通式(3),較佳為R15為十六烷基,X5為氫原子,R16為十五烷基,R17為羥基乙基者;R15為十六烷基,X5為氫原子,R16為壬基,R17為羥基乙基者;或R15為十六烷基,X5為甘油基,R16為十三烷基,R17為3-甲氧基丙基之模擬型腦醯胺類,更佳為通式(3)之R15為十六烷基,X5為氫原子,R16為十五烷基,R17為羥基乙基者(N-(十六烷氧基羥基丙基)-N-羥基乙基十六烷醯胺)。
[化8]
成分(C)之腦醯胺類可使用1種以上,於總組成中含有0.0001~50重量%,較佳為含有0.001~20重量%,更佳為含有0.01~10重量%,進而較佳為含有0.1~8重量%。就有效地對皮膚賦予保濕效果之觀點、及抑制發黏等使用感之不良情況之方面而言,較佳為於該範圍內含有成分(C)之腦醯胺類。
又,成分(A)及(C)之重量比例較佳為(A)/(C)≧0.001,更佳為(A)/(C)≧0.01,為抑制腦醯胺類之結晶化,形成並維持穩定之液晶,進而較佳為(A)/(C)≧0.1。其結果,可促進對皮膚之滲透,提昇水分保持量。又,較佳為(A)/(C)≦100以下,更佳為(A)/(C)≦10。
本發明中所使用之成分(D)之水於總組成中含有10~99重量%,更佳為含有40~95重量%,進而較佳為含有40~88質量%。
本發明之化粧料可進而含有成分(A)以外之酸作為成分(E)。作為該酸,只要為降低化粧料之pH值者,則並無限制,可為有機酸、無機酸中之任一種。
作為有機酸,較佳為選自乙酸、丙酸、丁酸等一元羧酸;琥珀酸、鄰苯二甲酸、反丁烯二酸、乙二酸、丙二酸、戊二酸等二羧酸;乙醇酸、檸檬酸、乳酸、丙酮酸、蘋果酸、酒石酸等羥基羧酸;麩胺酸、天冬醯胺酸等胺基酸中之1種或2種以上。
又,作為無機酸,較佳為選自鹽酸、硝酸、亞硝酸、硫酸、亞硫酸、磷酸、膦酸、次膦酸中之1種或2種以上。
於該等之中,作為有機酸,更佳為二羧酸,作為無機酸,更佳為磷酸。
於本發明中,較佳為不含成分(E),或於總組成中含有0~1重量%。成分(E)係將經成分(A)、(B)、(C)及(D)乳化之組合物調整成適當之pH值者。更具體而言,經成分(A)、(B)、(C)及(D)乳化之組合物由於pH值較高,故而可添加成分(E)而調整成適度之pH值。
就防止因鹽析引起之成分(A)之界面活性能的下降,提昇皮膚之水分保持量之觀點而言,與成分(A)之重量比例為0≦(E)/(A)<0.2,較佳為0≦(E)/(A)≦0.1,更佳為0≦(E)/(A)≦0.08,進而就長期之保存穩定性與水分保持量之提昇的觀點而言,較佳為0≦(E)/(A)≦0.05。
本發明之化粧料可進而含有通常之化粧料中所使用之成分,例如油性成分、低級醇、羧乙烯聚合物等水溶性高分子、保濕劑、抗氧化劑、防腐劑、美白劑、紫外線吸收劑、維生素類、其他各種藥效成分、粉體、香料、有色材料等。
又,本發明之化粧料較佳為實質上不含上述以外之界面活性劑,上述以外之界面活性劑之含量於總組成中較佳為1.5重量%以下,更佳為1.0重量%以下,進而較佳為0.5重量%以下,進而就低刺激性方面而言,更佳為0.2重量%以下。
作為上述以外之界面活性劑,可列舉非離子界面活性劑、陰離子界面活性劑。作為上述以外之界面活性劑,就刺激性方面而言,較佳為不含陽離子界面活性劑,或總組成中之含量為0.01質量%以下。
作為非離子界面活性劑,可列舉選自聚氧伸烷基山梨糖醇酐脂肪酸酯、聚氧伸烷基山梨糖醇脂肪酸酯、聚氧伸烷基甘油脂肪酸酯、聚氧伸烷基脂肪酸酯、聚氧伸烷基烷基醚、聚氧伸烷基烷基苯醚、聚氧伸烷基(氫化)蓖麻油、蔗糖脂肪酸酯、聚甘油烷基醚、聚甘油脂肪酸酯、脂肪酸烷醇醯胺、烷基糖苷中之1種以上。
進而,就形成為低刺激之方面及使用感之提昇方面而言,非離子界面活性劑之含量於總組成中較佳為1.0重量%以下,更佳為0.5重量%以下,更佳為0.2重量%以下。
作為陰離子界面活性劑,可列舉選自源自月桂酸鈉、棕櫚酸鉀等碳數8以上之脂肪酸之脂肪酸鹽;月桂基硫酸鈉、月桂基硫酸鉀、硬脂基硫酸鈉等烷基硫酸酯鹽;聚氧乙烯月桂基硫酸三乙醇胺等烷基醚硫酸酯鹽;月桂醯基肌胺酸鈉等N-醯基肌胺酸鹽;N-肉豆蔻醯基-N-甲基牛磺酸鈉等脂肪酸醯胺磺酸鹽;單硬脂基磷酸鈉、聚氧乙烯油醚磷酸鈉、聚氧乙烯硬脂醚磷酸鈉等磷酸酯鹽;二-2-乙基己基磺基琥珀酸鈉等磺基琥珀酸鹽;線性十二烷基苯磺酸鈉、線性十二烷基苯磺酸三乙醇胺等烷基苯磺酸鹽;N-月桂醯麩胺酸單鈉、N-硬脂醯基麩胺酸二鈉、N-肉豆蔻醯基-L-麩胺酸單鈉等N-醯基麩胺酸鹽中之1種以上。
就進一步減少刺激之方面而言,陰離子界面活性劑之含量於總組成中較佳為0.5重量%以下,更佳為0.2重量%以下,進而較佳為0.1重量%以下。
本發明之化粧料之製造方法係於將成分(A)、(B)、(C)及(D)加熱至成分(A)及(C)之任一較高熔點以上而進行混合之步驟後,包括冷卻至50℃以下之步驟,而獲得pH值為6~11之化粧料者。又,本發明之化粧料之製造方法可於冷卻至50℃以下之步驟後進而包括將pH值調整成6~11之pH值調整步驟。
混合成分(A)、(B)、(C)及(D)之步驟較佳為於將成分(A)、成分(B)及成分(D)之一部分之水(D1)加以混合,並加熱至成分(A)之熔點以上而進行混合之步驟1後,包括將含有成分(C)與其他油性成分之油相加熱至所有成分中最高熔點以上而進行混合之步驟2。再者,於上述步驟2中,亦可於添加成分(C)後添加其他油性成分。
又,混合成分(A)、(B)、(C)及(D)之步驟可於將成分(A)及(C)加熱至任一較高熔點以上而進行混合之步驟1後,包括添加成分(B)與成分(D)之一部分之水(D1)的混合液,一面加熱一面混合之步驟2。添加其他油性成分之步驟可於步驟2後包括加熱至所有油性成分中最高熔點以上而進行混合之步驟。
本發明之化粧料亦可進而添加羧乙烯聚合物等聚合物,可於步驟2後包括添加該等聚合物與成分(D)之一部分之水(D2)的混合液之步驟3。
上述pH值調整步驟可藉由在步驟3中將成分(E)調配於一部分之水(D2)中而包含於步驟3中,亦可於步驟3之前或之後包含該步驟。再者,pH值之調整亦可根據成分(B)之含量而進行調整,上述pH值調整步驟為藉由添加成分(E)與成分(D)之一部分之水而進行之步驟。
又,本發明之化粧料之製造方法亦可進而包括添加含有其他水溶性成分及成分(D)之一部分之水(D3)的水相而進行混合之步驟。再者,成分(D1)、(D2)及(D3)之含量之合計為成分(D)之含量。
本發明之化粧料例如可以如下方式製造,而獲得水中油型乳化化粧料,即,調整成分(B)之含量,以較佳為將pH值設為7以上、更佳為將pH值設為7.5以上、進而較佳為將pH值設為8以上且較佳為將pH值設為13以下、更佳為使pH值成為12之方式混合成分(A)、(B)、(C)及(D),並加熱至成分(A)及(C)之任一較高熔點以上而均勻地進行混合,於該步驟後包括冷卻至50℃以下之步驟,其後藉由添加成分(E)將pH值調整成6~11之步驟進行製造。
本發明之化粧料之pH值為6~11,就化粧料之使用性與進一步減少刺激之方面而言,較佳為pH值6~8,就提昇對皮膚之水分保持量之方面而言,較佳為pH值7~9。
再者,pH值係使用HORIBA公司製造之COMPACT pH METER B-212,於25℃下不稀釋各化粧料而進行直接測定者。
製造表1及表2中所示組成之化粧料,並評價保存穩定性。將結果一併示於表1及表2中。
於80~90℃下加熱攪拌成分(A)及(C)使其均勻化,一面以450 rpm之螺旋槳進行攪拌,一面緩緩地添加於80℃下均勻化之成分(B)與15重量%之成分(D)。繼而,同樣地一面攪拌一面添加其他油性成分。進而,一面進行攪拌一面冷卻至30℃,獲得溶液I。繼而,於10重量%之成分(D)中溶解對羥苯甲酸甲酯、甘油,並添加至溶液I中,獲得溶液II。將此時之pH值設為含有成分(E)前之各成分(A)~(D)均勻溶解時之pH值。繼而,使成分(E)及羧乙烯聚合物溶解或分散於剩餘之成分(D)中,並添加至溶液II中使其均勻化。其後,冷卻至25℃而獲得化粧料。
肉眼觀察將各化粧料分別於50℃、25℃及-5℃下保存1週後之外觀。進而,利用光學顯微鏡(400倍)進行觀察,確認有無結晶之析出。關於結果,將於任一溫度下均未發現乳化分離或結晶析出,穩定性優異者以「○」表示,將於任一溫度下均發現乳化分離或結晶析出,不穩定者以「×」表示。
根據表1及表2之結果,本發明之化粧料均為保存穩定性優異者。又,將該等實施例之化粧料塗佈於皮膚上,結果對皮膚之滲透性良好,且皮膚粗糙改善效果亦良好。
於上述實施例及比較例之化粧料之中,對表3所示之化粧料評價水分保持量。將結果一併示於表3中。
皮膚之水分量測定係藉由以皮膚水分測試儀(CORNEOMETER CM825,Integral股份有限公司製造)對前腕部之3個部位測定各部位之附近4處合計12處而進行,使用皮膚水分測試儀所顯示之數值作為水分量。首先,以洗顏料(碧柔洗顏泡沫,花王股份有限公司製造)清洗前腕部,將去除水分10分鐘後測定之水分量作為初始值。繼而,塗佈各化粧料,於6.5小時後不清洗而測定水分量,將自測定值中減去初始值之數值作為水分保持量。又,於清洗後之早晨、及沐浴後塗佈各化粧料,於24小時後不進行清洗而測定水分量,將自測定值中減去初始值之數值作為「於24小時後未清洗」之水分保持量。同樣地於24小時後,於測定前進行清洗後測定水分量,將自測定值中減去初始值之數值作為「於24小時後進行清洗」之水分保持量。
如表3所示,無論於塗佈6.5小時後抑或24小時後,與比較例相比,實施例均可獲得水分保持量較高之結果。又,可認為:實施例5、7係於24小時後,清洗前水分保持量極多,化粧料即便於24小時後仍殘留於皮膚上者。又,可認為:於24小時後,即便進行清洗後,實施例仍可獲得水分保持量較高之結果,對皮膚之滲透性較高。
Claims (9)
- 一種化板料,其含有如下成分(A)、(B)、(C)及(D):(A)選自膽固醇正十八烯基琥珀酸單酯及膽固醇正十六烯基琥珀酸單酯之有機酸0.001~50重量%、(B)鹼0.001~20重量%、(C)腦醯胺類0.0001~50重量%、(D)水,且作為成分(E)之成分(A)以外的酸之含量為0≦(E)/(A)≦0.08,且pH值為6~11。
- 如請求項1之化粧料,其中成分(A)及(C)之重量比例為(A)/(C)≧0.001。
- 如請求項1或2之化粧料,其中成分(E)為選自二羧酸及磷酸中之酸。
- 如請求項1之化粧料,其含有成分(A)0.1~10重量%。
- 如請求項1之化粧料,其含有成分(B)0.01~5重量%。
- 如請求項1之化粧料,其含有成分(C)0.01~10重量%。
- 如請求項1之化粧料,其中成分(B)為選自鹼性胺基酸、烷醇胺、氫氧化鈉及氫氧化鉀中之1種或2種以上。
- 一種化粧料之製造方法,其係如請求項1之化粧料之製造方法,於將成分(A)、(B)、(C)及(D)加熱至成分(A)及(C)之任一較高熔點以上而均勻地混合之步驟後,包括冷卻至50℃以下之步驟,且將pH值調整成6~11。
- 一種化板料之製造方法,其係如請求項1之化粧料之製造方法,於調整成分(B)之含量,以pH值成為7以上之方 式將成分(A)、(B)、(C)及(D)混合,並加熱至成分(A)及(C)之任一較高熔點以上而均勻地混合之步驟後,包括冷卻至50℃以下之步驟,其後添加成分(E)將pH值調整成6~11。
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| US20130303483A1 (en) | 2013-11-14 |
| EP2662071A1 (en) | 2013-11-13 |
| WO2012093643A1 (ja) | 2012-07-12 |
| CN103370048B (zh) | 2016-06-01 |
| JP5917414B2 (ja) | 2016-05-11 |
| CN103370048A (zh) | 2013-10-23 |
| US9161896B2 (en) | 2015-10-20 |
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| TW201231076A (en) | 2012-08-01 |
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