JP2004352627A - External preparation for skin - Google Patents
External preparation for skin Download PDFInfo
- Publication number
- JP2004352627A JP2004352627A JP2003150524A JP2003150524A JP2004352627A JP 2004352627 A JP2004352627 A JP 2004352627A JP 2003150524 A JP2003150524 A JP 2003150524A JP 2003150524 A JP2003150524 A JP 2003150524A JP 2004352627 A JP2004352627 A JP 2004352627A
- Authority
- JP
- Japan
- Prior art keywords
- mass
- parts
- skin
- external preparation
- salt
- 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.)
- Granted
Links
- 238000002360 preparation method Methods 0.000 title claims abstract description 52
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims abstract description 73
- 150000003839 salts Chemical class 0.000 claims abstract description 42
- 235000010323 ascorbic acid Nutrition 0.000 claims abstract description 40
- 239000011668 ascorbic acid Substances 0.000 claims abstract description 38
- 229960005070 ascorbic acid Drugs 0.000 claims abstract description 34
- CSHZYWUPJWVTMQ-UHFFFAOYSA-N 4-n-Butylresorcinol Chemical compound CCCCC1=CC=C(O)C=C1O CSHZYWUPJWVTMQ-UHFFFAOYSA-N 0.000 claims abstract description 30
- -1 ascorbic acid glucoside Chemical class 0.000 claims description 30
- 239000002537 cosmetic Substances 0.000 claims description 22
- 230000002087 whitening effect Effects 0.000 claims description 10
- 150000000996 L-ascorbic acids Chemical class 0.000 claims description 7
- 229910019142 PO4 Inorganic materials 0.000 claims description 6
- 239000010452 phosphate Substances 0.000 claims description 6
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 6
- 238000004519 manufacturing process Methods 0.000 claims description 5
- 229930182478 glucoside Natural products 0.000 claims description 4
- 238000004383 yellowing Methods 0.000 abstract description 7
- 230000019612 pigmentation Effects 0.000 abstract description 3
- 239000000049 pigment Substances 0.000 abstract description 2
- 229920000877 Melamine resin Polymers 0.000 abstract 1
- JDSHMPZPIAZGSV-UHFFFAOYSA-N melamine Chemical compound NC1=NC(N)=NC(N)=N1 JDSHMPZPIAZGSV-UHFFFAOYSA-N 0.000 abstract 1
- 210000003491 skin Anatomy 0.000 description 71
- 206010039897 Sedation Diseases 0.000 description 29
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 description 27
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 20
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 18
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 16
- 239000000686 essence Substances 0.000 description 13
- XUMBMVFBXHLACL-UHFFFAOYSA-N Melanin Chemical compound O=C1C(=O)C(C2=CNC3=C(C(C(=O)C4=C32)=O)C)=C2C4=CNC2=C1C XUMBMVFBXHLACL-UHFFFAOYSA-N 0.000 description 12
- 230000000052 comparative effect Effects 0.000 description 12
- 210000002510 keratinocyte Anatomy 0.000 description 12
- 230000000694 effects Effects 0.000 description 11
- FHKSXSQHXQEMOK-UHFFFAOYSA-N hexane-1,2-diol Chemical compound CCCCC(O)CO FHKSXSQHXQEMOK-UHFFFAOYSA-N 0.000 description 11
- NIXOWILDQLNWCW-UHFFFAOYSA-N acrylic acid group Chemical group C(C=C)(=O)O NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 10
- 229920001577 copolymer Polymers 0.000 description 10
- 229920002125 Sokalan® Polymers 0.000 description 9
- KGUHOFWIXKIURA-VQXBOQCVSA-N [(2r,3s,4s,5r,6r)-6-[(2s,3s,4s,5r)-3,4-dihydroxy-2,5-bis(hydroxymethyl)oxolan-2-yl]oxy-3,4,5-trihydroxyoxan-2-yl]methyl dodecanoate Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](COC(=O)CCCCCCCCCCC)O[C@@H]1O[C@@]1(CO)[C@@H](O)[C@H](O)[C@@H](CO)O1 KGUHOFWIXKIURA-VQXBOQCVSA-N 0.000 description 9
- 229940075507 glyceryl monostearate Drugs 0.000 description 9
- 238000000034 method Methods 0.000 description 9
- 239000000203 mixture Substances 0.000 description 9
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 description 9
- 229940032085 sucrose monolaurate Drugs 0.000 description 9
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 8
- 239000007864 aqueous solution Substances 0.000 description 8
- 238000009472 formulation Methods 0.000 description 8
- 229940093429 polyethylene glycol 6000 Drugs 0.000 description 8
- 229940099259 vaseline Drugs 0.000 description 8
- 229930182470 glycoside Natural products 0.000 description 7
- 230000006872 improvement Effects 0.000 description 7
- 150000002338 glycosides Chemical class 0.000 description 6
- 239000003795 chemical substances by application Substances 0.000 description 5
- 230000008099 melanin synthesis Effects 0.000 description 5
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 4
- 230000009471 action Effects 0.000 description 4
- 229940072107 ascorbate Drugs 0.000 description 4
- GVALZJMUIHGIMD-UHFFFAOYSA-H magnesium phosphate Chemical compound [Mg+2].[Mg+2].[Mg+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O GVALZJMUIHGIMD-UHFFFAOYSA-H 0.000 description 4
- 239000004137 magnesium phosphate Substances 0.000 description 4
- 229960002261 magnesium phosphate Drugs 0.000 description 4
- 229910000157 magnesium phosphate Inorganic materials 0.000 description 4
- 235000010994 magnesium phosphates Nutrition 0.000 description 4
- 239000000843 powder Substances 0.000 description 4
- GHMLBKRAJCXXBS-UHFFFAOYSA-N resorcinol Chemical compound OC1=CC=CC(O)=C1 GHMLBKRAJCXXBS-UHFFFAOYSA-N 0.000 description 4
- 150000005846 sugar alcohols Polymers 0.000 description 4
- JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical compound OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 description 3
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 230000032683 aging Effects 0.000 description 3
- 229910052783 alkali metal Inorganic materials 0.000 description 3
- 230000005540 biological transmission Effects 0.000 description 3
- 239000007844 bleaching agent Substances 0.000 description 3
- 235000014113 dietary fatty acids Nutrition 0.000 description 3
- 239000000194 fatty acid Substances 0.000 description 3
- 229930195729 fatty acid Natural products 0.000 description 3
- 239000003112 inhibitor Substances 0.000 description 3
- 230000002401 inhibitory effect Effects 0.000 description 3
- WCVRQHFDJLLWFE-UHFFFAOYSA-N pentane-1,2-diol Chemical compound CCCC(O)CO WCVRQHFDJLLWFE-UHFFFAOYSA-N 0.000 description 3
- PPASLZSBLFJQEF-RKJRWTFHSA-M sodium ascorbate Substances [Na+].OC[C@@H](O)[C@H]1OC(=O)C(O)=C1[O-] PPASLZSBLFJQEF-RKJRWTFHSA-M 0.000 description 3
- 235000010378 sodium ascorbate Nutrition 0.000 description 3
- 229960005055 sodium ascorbate Drugs 0.000 description 3
- 159000000000 sodium salts Chemical class 0.000 description 3
- PPASLZSBLFJQEF-RXSVEWSESA-M sodium-L-ascorbate Chemical compound [Na+].OC[C@H](O)[C@H]1OC(=O)C(O)=C1[O-] PPASLZSBLFJQEF-RXSVEWSESA-M 0.000 description 3
- XDOFQFKRPWOURC-UHFFFAOYSA-N 16-methylheptadecanoic acid Chemical compound CC(C)CCCCCCCCCCCCCCC(O)=O XDOFQFKRPWOURC-UHFFFAOYSA-N 0.000 description 2
- MPDGHEJMBKOTSU-YKLVYJNSSA-N 18beta-glycyrrhetic acid Chemical compound C([C@H]1C2=CC(=O)[C@H]34)[C@@](C)(C(O)=O)CC[C@]1(C)CC[C@@]2(C)[C@]4(C)CC[C@@H]1[C@]3(C)CC[C@H](O)C1(C)C MPDGHEJMBKOTSU-YKLVYJNSSA-N 0.000 description 2
- LEEDMQGKBNGPDN-UHFFFAOYSA-N 2-methylnonadecane Chemical compound CCCCCCCCCCCCCCCCCC(C)C LEEDMQGKBNGPDN-UHFFFAOYSA-N 0.000 description 2
- NYARJMRXCRSQPJ-UHFFFAOYSA-N 4-(3-methylbutyl)benzene-1,3-diol Chemical group CC(C)CCC1=CC=C(O)C=C1O NYARJMRXCRSQPJ-UHFFFAOYSA-N 0.000 description 2
- DJDHQJFHXLBJNF-UHFFFAOYSA-N 4-propylbenzene-1,3-diol Chemical group CCCC1=CC=C(O)C=C1O DJDHQJFHXLBJNF-UHFFFAOYSA-N 0.000 description 2
- FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Chemical compound CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 description 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
- AFSDNFLWKVMVRB-UHFFFAOYSA-N Ellagic acid Chemical compound OC1=C(O)C(OC2=O)=C3C4=C2C=C(O)C(O)=C4OC(=O)C3=C1 AFSDNFLWKVMVRB-UHFFFAOYSA-N 0.000 description 2
- ATJXMQHAMYVHRX-CPCISQLKSA-N Ellagic acid Natural products OC1=C(O)[C@H]2OC(=O)c3cc(O)c(O)c4OC(=O)C(=C1)[C@H]2c34 ATJXMQHAMYVHRX-CPCISQLKSA-N 0.000 description 2
- 229920002079 Ellagic acid Polymers 0.000 description 2
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 2
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- UQSXHKLRYXJYBZ-UHFFFAOYSA-N Iron oxide Chemical compound [Fe]=O UQSXHKLRYXJYBZ-UHFFFAOYSA-N 0.000 description 2
- MLSJBGYKDYSOAE-DCWMUDTNSA-N L-Ascorbic acid-2-glucoside Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O[C@@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)=C1O MLSJBGYKDYSOAE-DCWMUDTNSA-N 0.000 description 2
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical class NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 description 2
- AUNGANRZJHBGPY-SCRDCRAPSA-N Riboflavin Chemical compound OC[C@@H](O)[C@@H](O)[C@@H](O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O AUNGANRZJHBGPY-SCRDCRAPSA-N 0.000 description 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 2
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 2
- RTAQQCXQSZGOHL-UHFFFAOYSA-N Titanium Chemical compound [Ti] RTAQQCXQSZGOHL-UHFFFAOYSA-N 0.000 description 2
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical class OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 description 2
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical class CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 2
- 229910052784 alkaline earth metal Inorganic materials 0.000 description 2
- FPIPGXGPPPQFEQ-OVSJKPMPSA-N all-trans-retinol Chemical compound OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-OVSJKPMPSA-N 0.000 description 2
- 150000003863 ammonium salts Chemical class 0.000 description 2
- 150000001483 arginine derivatives Chemical class 0.000 description 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 2
- OGBUMNBNEWYMNJ-UHFFFAOYSA-N batilol Chemical compound CCCCCCCCCCCCCCCCCCOCC(O)CO OGBUMNBNEWYMNJ-UHFFFAOYSA-N 0.000 description 2
- 230000017531 blood circulation Effects 0.000 description 2
- 159000000007 calcium salts Chemical class 0.000 description 2
- 239000004359 castor oil Substances 0.000 description 2
- 235000019438 castor oil Nutrition 0.000 description 2
- 230000004087 circulation Effects 0.000 description 2
- 239000003240 coconut oil Substances 0.000 description 2
- 235000019864 coconut oil Nutrition 0.000 description 2
- 238000007796 conventional method Methods 0.000 description 2
- NOPFSRXAKWQILS-UHFFFAOYSA-N docosan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCCCCCO NOPFSRXAKWQILS-UHFFFAOYSA-N 0.000 description 2
- UKMSUNONTOPOIO-UHFFFAOYSA-N docosanoic acid Chemical compound CCCCCCCCCCCCCCCCCCCCCC(O)=O UKMSUNONTOPOIO-UHFFFAOYSA-N 0.000 description 2
- POULHZVOKOAJMA-UHFFFAOYSA-N dodecanoic acid Chemical compound CCCCCCCCCCCC(O)=O POULHZVOKOAJMA-UHFFFAOYSA-N 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 229960002852 ellagic acid Drugs 0.000 description 2
- 235000004132 ellagic acid Nutrition 0.000 description 2
- 239000000839 emulsion Substances 0.000 description 2
- 150000008131 glucosides Chemical class 0.000 description 2
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 2
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 2
- BJRNKVDFDLYUGJ-RMPHRYRLSA-N hydroquinone O-beta-D-glucopyranoside Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=CC=C(O)C=C1 BJRNKVDFDLYUGJ-RMPHRYRLSA-N 0.000 description 2
- 230000001788 irregular Effects 0.000 description 2
- 229940074358 magnesium ascorbate Drugs 0.000 description 2
- 159000000003 magnesium salts Chemical class 0.000 description 2
- AIOKQVJVNPDJKA-ZZMNMWMASA-L magnesium;(2r)-2-[(1s)-1,2-dihydroxyethyl]-4-hydroxy-5-oxo-2h-furan-3-olate Chemical compound [Mg+2].OC[C@H](O)[C@H]1OC(=O)C(O)=C1[O-].OC[C@H](O)[C@H]1OC(=O)C(O)=C1[O-] AIOKQVJVNPDJKA-ZZMNMWMASA-L 0.000 description 2
- FAARLWTXUUQFSN-UHFFFAOYSA-N methylellagic acid Natural products O1C(=O)C2=CC(O)=C(O)C3=C2C2=C1C(OC)=C(O)C=C2C(=O)O3 FAARLWTXUUQFSN-UHFFFAOYSA-N 0.000 description 2
- 239000010445 mica Substances 0.000 description 2
- 229910052618 mica group Inorganic materials 0.000 description 2
- 230000003020 moisturizing effect Effects 0.000 description 2
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 2
- 239000001301 oxygen Substances 0.000 description 2
- 229910052760 oxygen Inorganic materials 0.000 description 2
- 150000003014 phosphoric acid esters Chemical class 0.000 description 2
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 description 2
- 229920001296 polysiloxane Polymers 0.000 description 2
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 2
- LXNHXLLTXMVWPM-UHFFFAOYSA-N pyridoxine Chemical compound CC1=NC=C(CO)C(CO)=C1O LXNHXLLTXMVWPM-UHFFFAOYSA-N 0.000 description 2
- 230000002000 scavenging effect Effects 0.000 description 2
- NDVLTYZPCACLMA-UHFFFAOYSA-N silver oxide Chemical compound [O-2].[Ag+].[Ag+] NDVLTYZPCACLMA-UHFFFAOYSA-N 0.000 description 2
- 230000037394 skin elasticity Effects 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- PRAKJMSDJKAYCZ-UHFFFAOYSA-N squalane Chemical compound CC(C)CCCC(C)CCCC(C)CCCCC(C)CCCC(C)CCCC(C)C PRAKJMSDJKAYCZ-UHFFFAOYSA-N 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 230000008719 thickening Effects 0.000 description 2
- 239000010936 titanium Substances 0.000 description 2
- 229910052719 titanium Inorganic materials 0.000 description 2
- 238000002834 transmittance Methods 0.000 description 2
- 230000000007 visual effect Effects 0.000 description 2
- JIAARYAFYJHUJI-UHFFFAOYSA-L zinc dichloride Chemical compound [Cl-].[Cl-].[Zn+2] JIAARYAFYJHUJI-UHFFFAOYSA-L 0.000 description 2
- IMMBLRJLSYJQIZ-UNQGIHKMSA-N (2S)-7-[3,4-dihydroxy-5-[3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-6-[(3,4,5-trihydroxy-6-methyloxan-2-yl)oxymethyl]oxan-2-yl]oxy-5-hydroxy-2-(3-hydroxy-4-methoxyphenyl)-2,3-dihydrochromen-4-one Chemical compound COc1ccc(cc1O)[C@@H]1CC(=O)c2c(O)cc(OC3OC(COC4OC(C)C(O)C(O)C4O)C(OC4OC(CO)C(O)C(O)C4O)C(O)C3O)cc2O1 IMMBLRJLSYJQIZ-UNQGIHKMSA-N 0.000 description 1
- WCGUUGGRBIKTOS-GPOJBZKASA-N (3beta)-3-hydroxyurs-12-en-28-oic acid Chemical compound C1C[C@H](O)C(C)(C)[C@@H]2CC[C@@]3(C)[C@]4(C)CC[C@@]5(C(O)=O)CC[C@@H](C)[C@H](C)[C@H]5C4=CC[C@@H]3[C@]21C WCGUUGGRBIKTOS-GPOJBZKASA-N 0.000 description 1
- ALSTYHKOOCGGFT-KTKRTIGZSA-N (9Z)-octadecen-1-ol Chemical compound CCCCCCCC\C=C/CCCCCCCCO ALSTYHKOOCGGFT-KTKRTIGZSA-N 0.000 description 1
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 1
- ZORQXIQZAOLNGE-UHFFFAOYSA-N 1,1-difluorocyclohexane Chemical compound FC1(F)CCCCC1 ZORQXIQZAOLNGE-UHFFFAOYSA-N 0.000 description 1
- 229940015975 1,2-hexanediol Drugs 0.000 description 1
- QIZPVNNYFKFJAD-UHFFFAOYSA-N 1-chloro-2-prop-1-ynylbenzene Chemical compound CC#CC1=CC=CC=C1Cl QIZPVNNYFKFJAD-UHFFFAOYSA-N 0.000 description 1
- JQBCKRZQAMELAD-UHFFFAOYSA-N 1-hydroxypyrrolidin-2-one Chemical compound ON1CCCC1=O JQBCKRZQAMELAD-UHFFFAOYSA-N 0.000 description 1
- FPIPGXGPPPQFEQ-UHFFFAOYSA-N 13-cis retinol Natural products OCC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-UHFFFAOYSA-N 0.000 description 1
- ZONJATNKKGGVSU-UHFFFAOYSA-N 14-methylpentadecanoic acid Chemical compound CC(C)CCCCCCCCCCCCC(O)=O ZONJATNKKGGVSU-UHFFFAOYSA-N 0.000 description 1
- BFPYWIDHMRZLRN-UHFFFAOYSA-N 17alpha-ethynyl estradiol Natural products OC1=CC=C2C3CCC(C)(C(CC4)(O)C#C)C4C3CCC2=C1 BFPYWIDHMRZLRN-UHFFFAOYSA-N 0.000 description 1
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 description 1
- JNAYPSWVMNJOPQ-UHFFFAOYSA-N 2,3-bis(16-methylheptadecanoyloxy)propyl 16-methylheptadecanoate Chemical compound CC(C)CCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCC(C)C)COC(=O)CCCCCCCCCCCCCCC(C)C JNAYPSWVMNJOPQ-UHFFFAOYSA-N 0.000 description 1
- 239000000263 2,3-dihydroxypropyl (Z)-octadec-9-enoate Substances 0.000 description 1
- LRZBIPQJHILPJI-UHFFFAOYSA-N 2,3-dihydroxypropyl 2-(2,3-dihydroxypropyl)octadecanoate Chemical compound CCCCCCCCCCCCCCCCC(CC(O)CO)C(=O)OCC(O)CO LRZBIPQJHILPJI-UHFFFAOYSA-N 0.000 description 1
- GECRRQVLQHRVNH-MRCUWXFGSA-N 2-octyldodecyl (z)-octadec-9-enoate Chemical compound CCCCCCCCCCC(CCCCCCCC)COC(=O)CCCCCCC\C=C/CCCCCCCC GECRRQVLQHRVNH-MRCUWXFGSA-N 0.000 description 1
- QCDWFXQBSFUVSP-UHFFFAOYSA-N 2-phenoxyethanol Chemical compound OCCOC1=CC=CC=C1 QCDWFXQBSFUVSP-UHFFFAOYSA-N 0.000 description 1
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 1
- XPFCZYUVICHKDS-UHFFFAOYSA-N 3-methylbutane-1,3-diol Chemical compound CC(C)(O)CCO XPFCZYUVICHKDS-UHFFFAOYSA-N 0.000 description 1
- RZRNAYUHWVFMIP-GDCKJWNLSA-N 3-oleoyl-sn-glycerol Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@H](O)CO RZRNAYUHWVFMIP-GDCKJWNLSA-N 0.000 description 1
- MIJYXULNPSFWEK-GTOFXWBISA-N 3beta-hydroxyolean-12-en-28-oic acid Chemical compound C1C[C@H](O)C(C)(C)[C@@H]2CC[C@@]3(C)[C@]4(C)CC[C@@]5(C(O)=O)CCC(C)(C)C[C@H]5C4=CC[C@@H]3[C@]21C MIJYXULNPSFWEK-GTOFXWBISA-N 0.000 description 1
- HIQIXEFWDLTDED-UHFFFAOYSA-N 4-hydroxy-1-piperidin-4-ylpyrrolidin-2-one Chemical compound O=C1CC(O)CN1C1CCNCC1 HIQIXEFWDLTDED-UHFFFAOYSA-N 0.000 description 1
- OEOIWYCWCDBOPA-UHFFFAOYSA-N 6-methyl-heptanoic acid Chemical compound CC(C)CCCCC(O)=O OEOIWYCWCDBOPA-UHFFFAOYSA-N 0.000 description 1
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 description 1
- 208000002874 Acne Vulgaris Diseases 0.000 description 1
- 239000004925 Acrylic resin Substances 0.000 description 1
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Landscapes
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Abstract
Description
【０００１】
【発明の属する技術的分野】
本発明は、化粧料などの皮膚外用剤に関し、更に詳しくは、肌のくすみを改善するなどの効果に優れた美白用化粧料として好適な皮膚外用剤に関する。
【０００２】
【従来の技術】
肌を白く美しく保つことを望む人がいる。また、夏の間、小麦色の日焼け肌に装っていても、秋には白い肌に戻るように努力している人も少なくない。この様な背景から、化粧料分野では、皮膚のメラニンの産生を抑制する「美白剤」乃至は美白剤を含有する「美白化粧料」の開発が広く行われており、メラニン産生を抑制する成分である「美白剤」としては、プラセンタ−エキス、エラグ酸及び／又はその塩、アスコルビン酸及びその誘導体、トラネキサム酸及び／又はその塩、コウジ酸及び／又はその塩、アルブチン及び／又はその塩、４−ｎ−ブチルレゾルシノール及び／又はその塩等が既に開発されている。これらの美白剤は一般的には単味で用いられている。
【０００３】
その一方、メラニンの産生昂進によらない、或いは、メラニンの産生昂進以外のメカニズムも関与する、白い肌の阻害要因として、「肌のくすみ」が存在する。くすみは、血行不良による肌色の赤味の低下、皮膚弾力低下によって起こる皮膚表面の凹凸の影、角質細胞の肥厚などに起因する角質細胞の光透過性の低下、皮膚表面での乱反射によるツヤの低下、加齢に伴う皮膚の黄色化などが原因であるとされている。８〜９割の人が、自分の肌にくすみを感じ、これを何とかしたいと思っているという、市場でのニーズに従って、このくすみの問題は近年特に大きく取り上げられるようになっているが、くすみに対し、前記の美白剤は効を奏しにくいことから、くすみに対する改善方法の提供が望まれていた（例えば、非特許文献１参照）。
また、対症療法的に、保湿成分、シワ改善成分、血流改善成分などとともにメラニン産生抑制剤やα−ＭＳＨ抑制剤などを投与することが行われており、ある程度の効果は奏するものの、あまり明確な改善効果は得られていない。
【０００４】
くすみ改善の対症療法的な手段として、現在知られている技術の中から、いくつかの例を以下に挙げる。
１）カロチノイドとフィトステロールにより、ターンオーバーを速めて角質細胞を脱離させ、くすみを改善する技術（例えば、特許文献１参照）
２）ヒドロキシピロリドン等により角質細胞を剥離させ、且つ、エラグ酸によりメラニン産生を抑制し、くすみを改善する技術（例えば、特許文献２参照）
３）α−グルコシルヘスペリジンにより血流を改善し、くすみを改善する技術（例えば、特許文献３参照）
４）プロテアーゼにより角質細胞を剥離させ、くすみを改善する技術（例えば、特許文献４参照）
斯くのごとくに、くすみとは、肌の色調の明度低下の方向への変化でありながら、唯単にメラニン産生抑制剤を投与しても改善するものではないことがわかる。又、種々の方法である程度の改善は認められながらも、確固たる改善方法が見つけられていないことも、容易に窺い知ることが出来る。とりわけ、加齢に伴う皮膚の黄色化については、その改善手段は全く知られていない。これは皮膚の黄色化がかなり皮膚の深部まで及んでいるからである。
【０００５】
一方、本発明の皮膚外用剤の必須構成要素の内、４−ｎ−ブチルレゾルシノール又はその塩については、メラニン産生抑制作用（例えば、特許文献５参照）、雲脂抑制作用（例えば、特許文献６参照）、ニキビ抑制作用（例えば、特許文献７参照）、赤外線防護剤との併用による、日焼けと火照りの改善作用（例えば、特許文献８参照）、放射線照射後の瘢痕生成の抑制作用（例えば、特許文献９参照）、活性酸素消去作用（例えば、特許文献１０参照）、抗掻痒作用（例えば、特許文献１１参照）等が知られている。しかしながら、この物質のくすみに対する作用は全く知られていない。
【０００６】
一方、アスコルビン酸若しくはその誘導体又はそれらの塩については、美白作用（例えば、特許文献１２〜１４参照）、免疫賦活作用（例えば、特許文献１５参照）、活性酸素消去作用（例えば、特許文献１６参照）等の作用を有することが知られている。しかしながら、これらの物質のくすみに対する作用は全く知られていない。
【０００７】
また、１）４−ｎ−ブチルレゾルシノール及び／又はその塩と、２）アスコルビン酸若しくはその誘導体又はそれらの塩とを組み合わせて皮膚外用剤に含有させる技術も知られていない。
【０００８】
【非特許文献１】
武田ら監修「化粧品の有用性 評価技術の進歩と将来展望」、株式会社薬事日報社、２００１年３月３１日
【特許文献１】
特開２００２−３７０９６１号公報
【特許文献２】
特開２００２−３３８４２６号公報
【特許文献３】
特開２００２−２５５８２７号公報
【特許文献４】
特開２００２−２３４８４５号公報
【特許文献５】
特開平０２−４９７１５号公報
【特許文献６】
特開平０４−１６９５１６号公報
【特許文献７】
特開平０４−１６９５１１号公報
【特許文献８】
特開平０５−４９０５号公報
【特許文献９】
特開２００１−２０６８１３号公報
【特許文献１０】
特開２００１−３０２５０５号公報
【特許文献１１】
特開２００１−３０２５０６号公報
【特許文献１２】
特開２００２−１４５７５１号公報
【特許文献１３】
特開２０００−１６９１７号公報
【特許文献１４】
特開平１１−３０１２５号公報
【特許文献１５】
特開２００１−３５４５７０号公報
【特許文献１６】
特開２００１−３２２９９０号公報
【０００９】
【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、皮膚の黄色化によって生じるくすみ等を改善する、即ち、メラニン色素沈着によるもの以外に対しても視覚的にくすんで見える現象（肌のくすみ）を改善することができる皮膚外用剤を提供することを課題とする。
【００１０】
【課題を解決するための手段】
本発明者らは、この様な実情に鑑みて、鋭意研究努力を重ねた結果、１）４−ｎ−ブチルレゾルシノール及び／又はその塩と、２）アスコルビン酸若しくはその誘導体又はそれらの塩とを含有する皮膚外用剤がくすみ改善作用を示すことを見出し、本発明を完成させるに至った。
即ち、本発明は以下のとおりである。
（１）１）４−ｎ−ブチルレゾルシノール及び／又はその塩と、２）アスコルビン酸及びその誘導体並びにそれらの塩からなる群から選ばれる少なくとも１種とを含有することを特徴とする皮膚外用剤。
（２）４−ｎ−ブチルレゾルシノール及び／又はその塩の含有量が、皮膚外用剤全量に対して、０．１〜０．５質量％であることを特徴とする（１）に記載の皮膚外用剤。
（３）アスコルビン酸の誘導体が、アスコルビン酸グルコシド及びアスコルビン酸リン酸エステルから選ばれることを特徴とする（１）又は（２）に記載の皮膚外用剤。
（４）アスコルビン酸若しくはその誘導体又はそれらの塩の含有量が、皮膚外用剤全量に対して、０．１〜１０質量％であることを特徴とする（１）〜（３）の何れか１項に記載の皮膚外用剤。
（５）美白用の化粧料であることを特徴とする、（１）〜（４）の何れか１項に記載の皮膚外用剤。
（６）肌のくすみ部位に適用する化粧料の製造における、１）４−ｎ−ブチルレゾルシノール及び／又はその塩と、２）アスコルビン酸及びその誘導体並びにそれらの塩からなる群から選ばれる少なくとも１種との使用。
【００１１】
【発明の実施の形態】
以下、本発明を詳細に説明する。
本発明の皮膚外用剤は、１）４−ｎ−ブチルレゾルシノール及び／又はその塩（以下、「４−ｎ−ブチルレゾルシノール等」ともいう）と、２）アスコルビン酸及びその誘導体並びにそれらの塩からなる群から選ばれる少なくとも１種（以下、「アスコルビン酸等」ともいう）とを含有することを特徴とする。
【００１２】
＜１＞本発明の皮膚外用剤の必須成分である４−ｎ−ブチルレゾルシノール及び／又はその塩について
本発明の皮膚外用剤は、４−ｎ−ブチルレゾルシノール等を含有する。
４−ｎ−ブチルレゾルシノールは、常法に従って製造することが出来、例えば、Ｌｉｌｌｅ，Ｊ．；Ｂｉｔｔｅｒ，Ｌ．Ａ．；Ｐｅｉｎｅｒ，Ｖ． Ｔｒｕｄｙ−Ｎａｕｃｈｏｎｏ−Ｉｓｓｌｅｄｏｖａｔｅｌ’ｓｋｉｉ Ｉｎｓｔｉｔｕｔ Ｓｌａｎｔｓｅｖ （１９６９）， Ｎｏ．１８， １２７−３４に記載された方法に従うことができる。
即ち、レゾルシンとブタン酸を塩化亜鉛の存在下縮合し、亜鉛アマルガム／塩酸で還元する方法や、レゾルシンとｎ−ブチルアルコールとを２００〜４００℃の高温下で縮合させる方法が例示できる。
【００１３】
このようにして得られた４−ｎ−ブチルレゾルシノールは種々の塩基性化合物と反応させることにより塩とすることが出来る。このような塩としては、生理的に許容されるものであれば特段の限定はされず、例えば、ナトリウム塩、カリウム塩などのアルカリ金属塩、カルシウム塩、マグネシウム塩などのアルカリ土類金属塩、アンモニウム塩、トリエタノールアミン塩やトリエチルアミン塩等の有機アミン塩、リジン塩やアルギニン塩等の塩基性アミノ酸塩などが好ましく例示できる。これらの塩の内、特に好ましいものはアルカリ金属塩であり、中でもナトリウム塩が特に好ましい。
本発明の皮膚外用剤に於いて、４−ｎ−ブチルレゾルシノール等は単独で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できる。
本発明の皮膚外用剤中に於ける４−ｎ−ブチルレゾルシノール等の好ましい含有量は、皮膚外用剤全量に対して総量で、０．０５〜１質量％であり、０．１〜０．５質量％が更に好ましい。これは、少なすぎると効果を発揮しない場合があり、多すぎても効果が頭打ちになる場合があるからである。
【００１４】
＜２＞本発明の皮膚外用剤の必須成分であるアスコルビン酸若しくはその誘導体又はそれらの塩について
本発明の皮膚外用剤は、アスコルビン酸等を含有する。
アスコルビン酸の誘導体としては、アスコルビン酸のリン酸エステル、又はアスコルビン酸の配糖体等が挙げられる。またその他、アスコルビン酸の誘導体として、アスコルビン酸、アスコルビン酸のリン酸エステル又はアスコルビン酸の配糖体のアシル化物若しくはアルキル化物なども挙げられる。上記配糖体の種類としては、グルコシド、マルトシド、リボシド、デオキシリボシド又はアラビノシドなどが挙げられる。また、上記アシル化物としては、アセチル化物、ホルミル化物又はラウロイル化物などが挙げられる。また、上記アルキル化物としては、メチル化物又はエチル化物などが挙げられる。
【００１５】
アスコルビン酸の配糖体は、アスコルビン酸と糖とをグルコシダーゼ等の酵素で縮合させることによっても製造できる。また、糖のアシル化物とアスコルビン酸とを酸化銀触媒を用いて縮合することによっても製造できる。更に、アスコルビン酸の配糖体にアシルクロライド等を反応させれば、アシル化物へと誘導することも出来る。
上記アスコルビン酸の誘導体のより好ましいものとして、アスコルビン酸リン酸エステル又はアスコルビン酸の配糖体が挙げられる。中でも配糖体がグルコシドであると、このものは市販もされており、入手の点からも特に好ましい。
【００１６】
又、これらのアスコルビン酸又はその誘導体は、塩であってもよい。塩としては、生理的に許容されるものであれば特段の限定無く使用することが出来、例えば、ナトリウム塩やカリウム塩などのアルカリ金属塩、カルシウム塩やマグネシウム塩などのアルカリ土類金属塩、アンモニウム塩、トリエタノールアミン塩やトリエチルアミン塩などの有機アミン塩、リジン塩やアルギニン塩などの塩基性アミノ酸塩などが好ましく例示できる。
これらの塩の内、入手し易さの面又は使用実績の面で、アスコルビン酸リン酸マグネシウム又はアスコルビン酸リン酸ナトリウムが好ましく挙げられる。これらは何れも市販されている。
【００１７】
本発明の皮膚外用剤に於いて、アスコルビン酸若しくはその誘導体又はそれらの塩は単独で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できる。
本発明の皮膚外用剤に於ける、アスコルビン酸若しくはその誘導体又はそれらの塩の好ましい含有量は、皮膚外用剤全量に対して総量で、０．０１〜１０質量％であり、更に好ましくは、０．１〜１０質量％である。
尚、本発明の皮膚外用剤における、１）４−ｎ−ブチルレゾルシノール及び／又はその塩と２）アスコルビン酸若しくはその誘導体又はそれらの塩との配合割合は、１：１０〜１：３が好ましい。
【００１８】
＜３＞本発明の皮膚外用剤について
本発明の皮膚外用剤は、上記必須成分である、１）４−ｎ−ブチルレゾルシノール等と２）アスコルビン酸等とを含有する。
本発明の皮膚外用剤は、かかる構成を採ることにより、くすみに対して優れた改善効果を有する。従って、本発明の皮膚外用剤は、美白用のものとして用いることが特に好ましい。
ここで、「美白」とは、血行不良による肌色の赤味の低下、皮膚弾力低下によって起こる皮膚表面の凹凸の影、角質細胞の肥厚などに起因する角質細胞の光透過性の低下、皮膚表面での乱反射によるツヤの低下、加齢に伴う皮膚の黄色化などによって生じるくすみを少なくとも改善することをいう。尚、メラニン色素異常の改善を含んでいてもよい。
また、本発明でいう皮膚外用剤は、皮膚に外用で用いられる製剤全般を示し、化粧料、皮膚外用医薬、皮膚外用雑貨等を含むものである。本発明の皮膚外用剤で特に好ましいものは、化粧料（但し、医薬部外品を含む）である。特に、上記の観点から、肌のくすみ改善のために用いる美白用の化粧料として適用するのが好ましい。
【００１９】
本発明の皮膚外用剤においては、前記必須成分以外に、通常、皮膚外用剤で使用される任意成分を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リルなどのエステル類、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、バチルアルコールやセラルキルアルコールなどのアルキル（アルケニル）グリセリルエーテル類、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、グリセリルモノステアレート、グリセリルモノオレート、ジグリセリルモノステアレート、ジグリセリルモノオレート、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ン脂肪酸エステル、ポリオ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、ショ糖モノラウリン酸エステル、ショ糖モノステアリン酸エステルなどのショ糖脂肪酸エステル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、水酸化カリウム、水酸化ナトリウムなどのアルカリ剤、レチノール、レチノイン酸、トコフェロール、リボフラビン、ピリドキシンなどのアスコルビン酸類以外のビタミンやグリチルリチン酸塩、グリチルレチン酸、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、フェノキシエタノール、パラベン類、ヒビテングルコネート、塩化ベンザルコニウム等の防腐剤、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。
【００２０】
特に好ましいものは、多価アルコールであり、中でも、１，３−ブタンジオール、１，２−ペンタンジオール、１，２−ヘキシレングリコール等が好ましく、１，２−ペンタンジオール、１，２−ヘキシレングリコールが特に好ましい。これらは、保湿作用を発揮しながら防腐効果を付与する作用を有する。かかる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させることも出来る。多価アルコールの好ましい含有量は、皮膚外用剤全量に対して総量で、１〜１０質量％である。
本発明の皮膚外用剤は、上記した必須成分と、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。
本発明の皮膚外用剤の剤形としては、皮膚外用剤で知られている剤形であれば特段の限定無く適用することが出来、例えば、ローション、エッセンス、乳液、クリーム、ジェル等が好ましく例示できる。
【００２１】
【実施例】
以下に、実施例を挙げて、本発明について更に具体的に説明を加えるが、本発明が、かかる実施例にのみ限定されないことは言うまでもない。
【００２２】
＜実施例１＞
下記に示す処方に従って、本発明の皮膚外用剤である乳化タイプの高粘度エッセンス１（化粧料）を作製した。
即ち、処方成分イ）、ロ）及びハ）をそれぞれ７０℃に加熱し、イ）にロ）を加え中和し、これに徐々にハ）を加えて乳化し、ホモジナイザーで乳化粒子を整え、攪拌冷却し、エッセンス１を得た。
【００２３】
イ）
アクリル酸−メタクリル酸アルキル（アルキル基の炭素数１０〜３０）コポリマー（以下、アクリル酸−メタクリル酸アルキルコポリマーともいう）
（商品名「ペムレンＴＲ−２」、グッドリッチ社製） ０．２質量部
カルボキシビニルポリマー ０．２質量部
１，３−ブタンジオール ５ 質量部
１，２−ヘキシレングリコール ２ 質量部
ポリエチレングリコール６０００ ２ 質量部
アスコルビン酸リン酸ナトリウム ０．３質量部
４−ｎ−ブチルレゾルシノール ０．３質量部
水 ３０ 質量部
ロ）
水酸化カリウム１０質量％水溶液 ３ 質量部
水 ４９．９質量部
ハ）
セラキルアルコール １．５質量部
グリセリルモノステアレート ０．５質量部
ショ糖モノラウリン酸エステル ０．１質量部
ワセリン ５ 質量部
【００２４】
＜実施例２＞
実施例１と同様に操作して、下記処方に従って、乳化タイプの高粘度エッセンス２（化粧料）を作製した。
【００２５】
イ）
アクリル酸−メタクリル酸アルキルコポリマー
（商品名「ペムレンＴＲ−２」、グッドリッチ社製） ０．２質量部
カルボキシビニルポリマー ０．２質量部
１，３−ブタンジオール ５ 質量部
１，２−ヘキシレングリコール ２ 質量部
ポリエチレングリコール６０００ ２ 質量部
アスコルビン酸リン酸マグネシウム ０．３質量部
４−ｎ−ブチルレゾルシノール ０．３質量部
水 ３０ 質量部
ロ）
水酸化カリウム１０質量％水溶液 ３ 質量部
水 ４９．９質量部
ハ）
セラキルアルコール １．５質量部
グリセリルモノステアレート ０．５質量部
ショ糖モノラウリン酸エステル ０．１質量部
ワセリン ５ 質量部
【００２６】
＜実施例３＞
実施例１と同様に操作して、下記処方に従って、乳化タイプの高粘度エッセンス３（化粧料）を作製した。
【００２７】
イ）
アクリル酸−メタクリル酸アルキルコポリマー
（商品名「ペムレンＴＲ−２」、グッドリッチ社製） ０．２質量部
カルボキシビニルポリマー ０．２質量部
１，３−ブタンジオール ５ 質量部
１，２−ヘキシレングリコール ２ 質量部
ポリエチレングリコール６０００ ２ 質量部
アスコルビン酸−２−グルコシド ０．３質量部
４−ｎ−ブチルレゾルシノール ０．３質量部
水 ３０ 質量部
ロ）
水酸化カリウム１０質量％水溶液 ３ 質量部
水 ４９．９質量部
ハ）
セラキルアルコール １．５質量部
グリセリルモノステアレート ０．５質量部
ショ糖モノラウリン酸エステル ０．１質量部
ワセリン ５ 質量部
【００２８】
＜比較例１＞
実施例２と同様に操作して、下記処方に従って、４−ｎ−ブチルレゾルシノールをアスコルビン酸リン酸マグネシウムに置換した、乳化タイプの高粘度比較エッセンス１（化粧料）を作製した。
【００２９】
イ）
アクリル酸−メタクリル酸アルキルコポリマー
（商品名「ペムレンＴＲ−２」、グッドリッチ社製） ０．２質量部
カルボキシビニルポリマー ０．２質量部
１，３−ブタンジオール ５ 質量部
１，２−ヘキシレングリコール ２ 質量部
ポリエチレングリコール６０００ ２ 質量部
アスコルビン酸リン酸マグネシウム ０．６質量部
水 ３０ 質量部
ロ）
水酸化カリウム１０質量％水溶液 ３ 質量部
水 ４９．９質量部
ハ）
セラキルアルコール １．５質量部
グリセリルモノステアレート ０．５質量部
ショ糖モノラウリン酸エステル ０．１質量部
ワセリン ５ 質量部
【００３０】
＜比較例２＞
実施例１と同様に操作して、下記処方に従って、アスコルビン酸リン酸ナトリウムを４−ｎ−ブチルレゾルシノールに置換した、乳化タイプの高粘度比較エッセンス２（化粧料）を作製した。
【００３１】
イ）
アクリル酸−メタクリル酸アルキルコポリマー
（商品名「ペムレンＴＲ−２」、グッドリッチ社製） ０．２質量部
カルボキシビニルポリマー ０．２質量部
１，３−ブタンジオール ５ 質量部
１，２−ヘキシレングリコール ２ 質量部
ポリエチレングリコール６０００ ２ 質量部
４−ｎ−ブチルレゾルシノール ０．６質量部
水 ３０ 質量部
ロ）
水酸化カリウム１０質量％水溶液 ３ 質量部
水 ４９．９質量部
ハ）
セラキルアルコール １．５質量部
グリセリルモノステアレート ０．５質量部
ショ糖モノラウリン酸エステル ０．１質量部
ワセリン ５ 質量部
【００３２】
＜比較例３＞
実施例２と同様に操作して、下記処方に従って、４−ｎ−ブチルレゾルシノールを４−イソアミルレゾルシノールに置換した、乳化タイプの高粘度比較エッセンス３（化粧料）を作製した。
【００３３】
イ）
アクリル酸−メタクリル酸アルキルコポリマー
（商品名「ペムレンＴＲ−２」、グッドリッチ社製） ０．２質量部
カルボキシビニルポリマー ０．２質量部
１，３−ブタンジオール ５ 質量部
１，２−ヘキシレングリコール ２ 質量部
ポリエチレングリコール６０００ ２ 質量部
アスコルビン酸リン酸マグネシウム ０．３質量部
４−イソアミルレゾルシノール ０．３質量部
水 ３０ 質量部
ロ）
水酸化カリウム１０質量％水溶液 ３ 質量部
水 ４９．９質量部
ハ）
セラキルアルコール １．５質量部
グリセリルモノステアレート ０．５質量部
ショ糖モノラウリン酸エステル ０．１質量部
ワセリン ５ 質量部
【００３４】
＜比較例４＞
実施例２と同様に操作して、下記処方に従って、４−ｎ−ブチルレゾルシノールを４−ｎ−プロピルレゾルシノールに置換した、乳化タイプの高粘度比較エッセンス４（化粧料）を作製した。
【００３５】
イ）
アクリル酸−メタクリル酸アルキルコポリマー
（商品名「ペムレンＴＲ−２」、グッドリッチ社製） ０．２質量部
カルボキシビニルポリマー ０．２質量部
１，３−ブタンジオール ５ 質量部
１，２−ヘキシレングリコール ２ 質量部
ポリエチレングリコール６０００ ２ 質量部
アスコルビン酸リン酸マグネシウム ０．３質量部
４−ｎ−プロピルレゾルシノール ０．３質量部
水 ３０ 質量部
ロ）
水酸化カリウム１０質量％水溶液 ３ 質量部
水 ４９．９質量部
ハ）
セラキルアルコール １．５質量部
グリセリルモノステアレート ０．５質量部
ショ糖モノラウリン酸エステル ０．１質量部
ワセリン ５ 質量部
【００３６】
＜試験例１＞
くすみに悩む人７０人を集めて、上記実施例１〜３、比較例１〜４のエッセンス（化粧料）のくすみ改善効果を試験した。パネラー７０名は年齢、くすみの程度などの特性値に偏りがないように１０名ずつ７群に分けた。各群にそれぞれ１種ずつ化粧料を配り、連日朝晩２回、８週間投与してもらった。試験開始時及び試験終了時に上腕内側部と頬部から粘着テープを用いて角質細胞を採取した。又、その時同時に専門家（３名）の目視判定でくすみの程度を判定した。
【００３７】
くすみの程度の判定は、下記の基準で行った。
スコア１：くすみが全く感じられない
スコア２：僅かにくすみが感じられる
スコア３：少しくすみが感じられる
スコア４：くすみが明確に感じられる
スコア５：くすみが目立つ
【００３８】
結果を平均スコアとして表１に示す。これより本発明の皮膚外用剤（実施例１〜３のエッセンス１〜３）により、くすみが改善されていることがわかる。又、角質細胞はモリテックス株式会社製のビデオマイクロスコープを用いて、画像として取り込み、この画像のＲＧＢ成分の内のＢ成分のみを取りだしたＢ画像とし、角質細胞に於ける輝度を測定し、頬部の輝度を上腕内側部の輝度で除した値（Ｂ透過損失比）を求めた。この平均値を表１に示す。この値は１未満であり、頬部の角質細胞においては、上腕内側部に比して、Ｂ成分の少ない反射光を観察した。言い換えれば、頬部の角質細胞は、上腕内側部に比して、黄色乃至は褐色がかった色をしていることがわかる。この頬部の角質細胞の黄色乃至は褐色の着色は、本発明の皮膚外用剤を投与することにより改善され、Ｂ透過損失比も１に近づいていることがわかる。比較例（比較例１〜４の比較エッセンス１〜４）ではこの効果は顕著には認められていない。
【００３９】
【表１】
＜実施例４＞
実施例１と同様に、以下に示す処方に従って、本発明の皮膚外用剤のエッセンス（化粧料）を作製した。試験例１と同様の検討において、Ｂ透過損失比は、０．５５から０．８３へと変化した。
【００４１】
イ）
アクリル酸−メタクリル酸アルキルコポリマー
（商品名「ペムレンＴＲ−２」、グッドリッチ社製） ０．２質量部
カルボキシビニルポリマー ０．２重量部
１，３−ブタンジオール ５ 重量部
１，２−ヘキシレングリコール ２ 重量部
ポリエチレングリコール６０００ ２ 重量部
アスコルビン酸−２−グルコシド １ 重量部
４−ｎ−ブチルレゾルシノール ０．５重量部
水 ３０ 重量部
ロ）
水酸化カリウム１０質量％水溶液 ３ 重量部
水 ４９ 重量部
ハ）
セラキルアルコール １．５重量部
グリセリルモノステアレート ０．５重量部
ショ糖モノラウリン酸エステル ０．１重量部
ワセリン ５ 重量部
【００４２】
【発明の効果】
本発明によれば、皮膚の黄色化によって生じるくすみ等を改善する、即ち、メラニン色素沈着によるもの以外に対しても視覚的にくすんで見える現象（肌のくすみ）を改善することができる皮膚外用剤を提供することができる。[0001]
TECHNICAL FIELD OF THE INVENTION
The present invention relates to an external preparation for skin such as cosmetics, and more particularly, to an external preparation for skin suitable as a whitening cosmetic having excellent effects such as improvement of dull skin.
[0002]
[Prior art]
Some people want to keep their skin white and beautiful. Also, many people are trying to return to white skin in the fall, even if they wear tan skin during the summer. Against this background, in the field of cosmetics, "whitening agents" that suppress the production of skin melanin or "whitening cosmetics" containing whitening agents have been widely developed, and components that suppress melanin production. Examples of the “whitening agent” include placenta extract, ellagic acid and / or its salt, ascorbic acid and its derivative, tranexamic acid and / or its salt, kojic acid and / or its salt, arbutin and / or its salt, 4-n-butyl resorcinol and / or a salt thereof have already been developed. These whitening agents are generally used alone.
[0003]
On the other hand, "dull skin" exists as a factor inhibiting white skin, which is not due to increased production of melanin or involves a mechanism other than increased production of melanin. Dullness is a decrease in redness of skin color due to poor circulation, shadows of irregularities on the skin surface caused by a decrease in skin elasticity, a decrease in light transmittance of keratinocytes due to thickening of keratinocytes, etc., and a gloss due to irregular reflection on the skin surface. It is said that the cause is a decrease and yellowing of the skin with aging. According to the needs in the market, where 80 to 90% of people feel dullness in their skin and want to manage it, the problem of dullness has been particularly highlighted in recent years. On the other hand, since the above-mentioned whitening agent is hardly effective, it has been desired to provide a method for improving dullness (for example, see Non-Patent Document 1).
In addition, as a symptomatic treatment, a melanin production inhibitor and an α-MSH inhibitor are administered together with a moisturizing component, a wrinkle improving component, a blood flow improving component, and the like. No significant improvement effect has been obtained.
[0004]
Some examples of currently known techniques as symptomatic means for improving dullness are given below.
1) Technology for speeding up turnover and detaching keratinocytes with carotenoids and phytosterols to improve dullness (for example, see Patent Document 1)
2) A technique for exfoliating keratinocytes with hydroxypyrrolidone or the like and suppressing melanin production with ellagic acid to improve dullness (for example, see Patent Document 2)
3) Technology for improving blood flow and improving dullness with α-glucosyl hesperidin (for example, see Patent Document 3)
4) A technique for removing keratinocytes with a protease to improve dullness (for example, see Patent Document 4)
As described above, it can be understood that dullness is a change in the tone of the skin in the direction of decreasing lightness, but does not improve even if the melanin production inhibitor is simply administered. In addition, although some improvement is recognized by various methods, it can be easily understood that no solid improvement method has been found. In particular, there is no known means for improving the yellowing of the skin with aging. This is because the yellowing of the skin extends considerably deep into the skin.
[0005]
On the other hand, among the essential components of the external preparation for skin of the present invention, 4-n-butylresorcinol or a salt thereof has a melanin production inhibitory action (for example, see Patent Document 5) and a cloud fat inhibitory action (for example, Patent Document 6). ), Acne-suppressing action (see, for example, Patent Document 7), sunburn and hot flashes improving action by combined use with an infrared protective agent (see, for example, Patent Document 8), and suppressing action of scar formation after irradiation (for example, see Patent Document 8). Known are an active oxygen scavenging effect (see, for example, Patent Document 10), an antipruritic effect (for example, see Patent Document 11), and the like. However, the effect of this substance on dullness is not known at all.
[0006]
On the other hand, ascorbic acid or a derivative thereof or a salt thereof has a whitening effect (for example, see Patent Documents 12 to 14), an immunostimulating effect (for example, see Patent Document 15), and an active oxygen scavenging effect (for example, see Patent Document 16). ) Are known. However, the effect of these substances on dullness is not known at all.
[0007]
Further, there is no known technique for combining 1) 4-n-butyl resorcinol and / or a salt thereof and 2) ascorbic acid or a derivative thereof or a salt thereof to cause the composition to be contained in an external preparation for skin.
[0008]
[Non-patent document 1]
Takeda et al., Supervision, "Progress and Future Prospects of Cosmetic Usefulness Evaluation Technology", Yakuji Nippo Co., Ltd., March 31, 2001
[Patent Document 1]
JP 2002-370961 A
[Patent Document 2]
JP-A-2002-338426
[Patent Document 3]
JP-A-2002-255827
[Patent Document 4]
JP-A-2002-234845
[Patent Document 5]
JP-A-02-49715
[Patent Document 6]
JP 04-169516 A
[Patent Document 7]
JP 04-169511 A
[Patent Document 8]
JP 05-4905 A
[Patent Document 9]
JP 2001-206813 A
[Patent Document 10]
JP 2001-302505 A
[Patent Document 11]
JP 2001-302506 A
[Patent Document 12]
JP-A-2002-145751
[Patent Document 13]
JP 2000-16917 A
[Patent Document 14]
JP-A-11-30125
[Patent Document 15]
JP 2001-354570A
[Patent Document 16]
JP 2001-322990 A
[0009]
[Problems to be solved by the invention]
The present invention has been made under such circumstances, and it is intended to improve dullness caused by yellowing of the skin, that is, a phenomenon (visual appearance of skin) that appears visually other than due to melanin pigmentation. An object of the present invention is to provide a skin external preparation capable of improving dullness.
[0010]
[Means for Solving the Problems]
In view of such circumstances, the present inventors have made intensive studies and as a result, have found that 1) 4-n-butylresorcinol and / or a salt thereof and 2) ascorbic acid or a derivative thereof or a salt thereof. The present inventors have found that the contained external preparation for skin shows a dullness-improving effect, and have completed the present invention.
That is, the present invention is as follows.
(1) An external preparation for skin, comprising: 1) 4-n-butyl resorcinol and / or a salt thereof; and 2) at least one selected from the group consisting of ascorbic acid and its derivatives and salts thereof. .
(2) The skin according to (1), wherein the content of 4-n-butyl resorcinol and / or a salt thereof is 0.1 to 0.5% by mass based on the total amount of the external preparation for skin. External preparation.
(3) The external preparation for skin according to (1) or (2), wherein the derivative of ascorbic acid is selected from ascorbic acid glucoside and ascorbic acid phosphate.
(4) Any one of (1) to (3), wherein the content of ascorbic acid or a derivative thereof or a salt thereof is 0.1 to 10% by mass relative to the total amount of the external preparation for skin. An external preparation for skin according to Item.
(5) The skin external preparation according to any one of (1) to (4), which is a cosmetic for whitening.
(6) At least one selected from the group consisting of 1) 4-n-butyl resorcinol and / or a salt thereof, and 2) ascorbic acid and a derivative thereof and a salt thereof in the production of a cosmetic applied to a dull skin site. Use with seeds.
[0011]
BEST MODE FOR CARRYING OUT THE INVENTION
Hereinafter, the present invention will be described in detail.
The external preparation for skin of the present invention comprises 1) 4-n-butyl resorcinol and / or a salt thereof (hereinafter, also referred to as “4-n-butyl resorcinol or the like”), and 2) ascorbic acid, a derivative thereof, and a salt thereof. And at least one member selected from the group consisting of (hereinafter, also referred to as “ascorbic acid or the like”).
[0012]
<1> Regarding 4-n-butyl resorcinol and / or a salt thereof, which are essential components of the external preparation for skin of the present invention.
The external preparation for skin of the present invention contains 4-n-butyl resorcinol and the like.
4-n-butyl resorcinol can be produced according to a conventional method. Bitter, L .; A. Peiner, V .; Trudy-Nauchono-Isslevovatel'skii Institute Slitsev (1969), no. 18, 127-34.
That is, a method of condensing resorcinol and butanoic acid in the presence of zinc chloride and reducing it with zinc amalgam / hydrochloric acid, and a method of condensing resorcinol and n-butyl alcohol at a high temperature of 200 to 400 ° C can be exemplified.
[0013]
The thus obtained 4-n-butyl resorcinol can be converted into a salt by reacting with various basic compounds. Such salts are not particularly limited as long as they are physiologically acceptable, and include, for example, alkali metal salts such as sodium salt and potassium salt, alkaline earth metal salts such as calcium salt and magnesium salt, Preferred examples include ammonium salts, organic amine salts such as triethanolamine salts and triethylamine salts, and basic amino acid salts such as lysine salts and arginine salts. Among these salts, particularly preferred are alkali metal salts, and among them, sodium salt is particularly preferred.
In the skin external preparation of the present invention, 4-n-butyl resorcinol and the like can be contained alone or in combination of two or more.
The preferred content of 4-n-butyl resorcinol and the like in the external preparation for skin of the present invention is 0.05 to 1% by mass based on the total amount of the external preparation for skin, and 0.1 to 0.5% by mass. % Is more preferred. This is because if the amount is too small, the effect may not be exhibited, and if the amount is too large, the effect may reach a plateau.
[0014]
<2> Regarding ascorbic acid or a derivative thereof or a salt thereof, which is an essential component of the skin external preparation of the present invention
The external preparation for skin of the present invention contains ascorbic acid and the like.
Examples of the derivatives of ascorbic acid include phosphate esters of ascorbic acid and glycosides of ascorbic acid. In addition, examples of the derivative of ascorbic acid include acylated or alkylated products of ascorbic acid, a phosphoric acid ester of ascorbic acid, and a glycoside of ascorbic acid. Examples of the type of glycoside include glucoside, maltoside, riboside, deoxyriboside, and arabinoside. Examples of the acylated product include an acetylated product, a formylated product, and a lauroylated product. Examples of the alkylated product include a methylated product and an ethylated product.
[0015]
Glycosides of ascorbic acid can also be produced by condensing ascorbic acid and sugar with an enzyme such as glucosidase. It can also be produced by condensing an acylated saccharide with ascorbic acid using a silver oxide catalyst. Further, by reacting an ascorbic acid glycoside with an acyl chloride or the like, an acylated product can be obtained.
More preferred ascorbic acid derivatives include ascorbic acid phosphate and glycosides of ascorbic acid. Among them, when the glycoside is glucoside, it is commercially available, and it is particularly preferable from the viewpoint of availability.
[0016]
These ascorbic acids or derivatives thereof may be salts. As the salt, any physiologically acceptable salt can be used without particular limitation, for example, alkali metal salts such as sodium salt and potassium salt, alkaline earth metal salts such as calcium salt and magnesium salt, Preferred examples include ammonium salts, organic amine salts such as triethanolamine salts and triethylamine salts, and basic amino acid salts such as lysine salts and arginine salts.
Among these salts, preferred are magnesium ascorbate phosphate and sodium ascorbate phosphate in terms of availability and use results. These are all commercially available.
[0017]
In the external preparation for skin of the present invention, ascorbic acid or a derivative thereof or a salt thereof can be contained alone or in combination of two or more.
The preferable content of ascorbic acid or a derivative thereof or a salt thereof in the external preparation for skin of the present invention is 0.01 to 10% by mass, more preferably 0 to 10% by mass, based on the total amount of the external preparation for skin. 0.1 to 10% by mass.
In the external preparation for skin of the present invention, the mixing ratio of 1) 4-n-butyl resorcinol and / or a salt thereof and 2) ascorbic acid or a derivative thereof or a salt thereof is preferably 1:10 to 1: 3. .
[0018]
<3> About the skin external preparation of the present invention
The external preparation for skin of the present invention contains the essential components described above, such as 1) 4-n-butyl resorcinol and 2) ascorbic acid.
The external preparation for skin of the present invention has an excellent improvement effect on dullness by adopting such a constitution. Therefore, it is particularly preferable to use the skin external preparation of the present invention as a whitening agent.
Here, “whitening” refers to a reduction in skin color redness due to poor circulation, a shadow of unevenness on the skin surface caused by a decrease in skin elasticity, a decrease in light transmittance of keratinocytes due to a thickening of keratinocytes, a skin surface It refers to at least the improvement of dullness caused by a decrease in gloss due to irregular reflection in the skin and yellowing of the skin with aging. In addition, improvement of melanin pigment abnormality may be included.
Further, the external preparation for skin referred to in the present invention refers to all preparations used externally for the skin, and includes cosmetics, external medicine for skin, sundry miscellaneous goods and the like. Particularly preferred skin external preparations of the present invention are cosmetics (including quasi-drugs). In particular, from the above viewpoint, it is preferable to apply as a whitening cosmetic used for improving dull skin.
[0019]
The external preparation for skin of the present invention may contain, in addition to the above essential components, optional components usually used in external preparations for skin. Such optional components include, for example, squalane, liquid paraffin, light liquid isoparaffin, heavy liquid isoparaffin, microcrystalline wax, hydrocarbons such as solid paraffin, dimethicone, femethicone, cyclomethicone, amodimethicone, and polyether-modified silicone. Silicones, jojoba oil, carnauba wax, mokuro, beeswax, gay wax, octyldodecyl oleate, isopropyl myristate, neopentyl glycol diisostearate, diisostearyl malate and other esters, stearic acid, lauric acid, myristine Acids, palmitic acid, isostearic acid, isopalmitic acid, behenic acid, fatty acids such as oleic acid, behenyl alcohol, cetanol, oleyl alcohol, octadecyl alcohol Alkenyl glyceryl ethers such as batyl alcohol and aralkyl alcohol, castor oil, coconut oil, hydrogenated coconut oil, camellia oil, wheat germ oil, isostearic acid triglyceride, isooctanoic acid triglyceride, olive Triglycerides such as oils, polyhydric alcohols such as 1,3-butanediol, glycerin, diglycerin, dipropylene glycol, polyethylene glycol, 1,2-pentanediol, 1,2-hexylene glycol, isoprene glycol, glyceryl mono Stearate, glyceryl monooleate, diglyceryl monostearate, diglyceryl monooleate, sorbitan sesquiolate, sorbitan monooleate, sorbitan triolate, sorbitan sesquis Allate, sorbitan monostearate, polyoxyethylene sorbitan monooleate, polyoxyethylene sorbitan monostearate, polyoxyethylene stearate, polyoxyethylene oleate, polyoxyethylene glycerin fatty acid ester, polyoxyethylene alkyl ether, polyoxyethylene cured Nonionic surfactants such as castor oil, sucrose fatty acid esters such as sucrose monolaurate and sucrose monostearate, and anionic interfaces such as sodium lauryl stearate, polyoxyethylene alkyl sulfate, and sulfosuccinate. Surfactants, cationic surfactants such as quaternary alkylammonium salts, amphoteric surfactants such as alkyl betaine, crystalline cellulose, cross-linked methylpolysiloxane, polyethylene Powders, organic powders such as acrylic resin powder, talc, mica, sericite, magnesium carbonate, calcium carbonate, titanium dioxide, iron oxide, navy blue, ultramarine, titanium mica, titanium sericite, silica, etc. Powders, acrylic acid-alkyl methacrylate copolymers and / or salts thereof, carboxyvinyl polymers and / or salts thereof, thickeners such as xanthan gum and hydroxypropyl cellulose, potassium hydroxide, sodium hydroxide and the like. Alkaline agents, vitamins other than ascorbic acids such as retinol, retinoic acid, tocopherol, riboflavin, pyridoxine and terpenes such as glycyrrhizinate, glycyrrhetinic acid, ursolic acid and oleanolic acid, estradiol, ethinylestradiol, estrio Preferred examples include active ingredients such as steroids, preservatives such as phenoxyethanol, parabens, hibitene gluconate, benzalkonium chloride, and ultraviolet absorbers such as dimethylaminobenzoate, cinnamate, and benzophenone. it can.
[0020]
Particularly preferred are polyhydric alcohols, among which 1,3-butanediol, 1,2-pentanediol, 1,2-hexylene glycol and the like are preferred, and 1,2-pentanediol, 1,2-hexanediol and the like are preferable. Xylene glycol is particularly preferred. These have an action of imparting a preservative effect while exerting a moisturizing action. Such polyhydric alcohols may contain only one kind or two or more kinds in combination. The preferred content of the polyhydric alcohol is 1 to 10% by mass in total with respect to the total amount of the external preparation for skin.
The external preparation for skin of the present invention can be produced by treating the above-mentioned essential components and optional components according to a conventional method.
The dosage form of the external preparation for skin of the present invention can be applied without any particular limitation as long as it is a dosage form known as an external preparation for skin, and examples thereof include lotions, essences, emulsions, creams, and gels. it can.
[0021]
【Example】
Hereinafter, the present invention will be described more specifically with reference to examples. However, it is needless to say that the present invention is not limited only to the examples.
[0022]
<Example 1>
According to the formulation shown below, an emulsion type high viscosity essence 1 (cosmetic), which is a skin external preparation of the present invention, was prepared.
That is, prescription components a), b) and c) are each heated to 70 ° C, b) is added to b) for neutralization, c) is gradually added thereto and emulsified, and emulsified particles are prepared with a homogenizer. After stirring and cooling, essence 1 was obtained.
[0023]
I)
Acrylic acid-alkyl methacrylate (alkyl group having 10 to 30 carbon atoms) copolymer (hereinafter also referred to as acrylic acid-alkyl methacrylate copolymer)
(Trade name "Pemren TR-2", manufactured by Goodrich) 0.2 parts by mass
Carboxyvinyl polymer 0.2 parts by mass
1,3-butanediol 5 parts by mass
1,2-hexylene glycol 2 parts by mass
Polyethylene glycol 6000 2 parts by mass
0.3 parts by mass of sodium ascorbate phosphate
0.3 parts by mass of 4-n-butyl resorcinol
Water 30 parts by mass
B)
10 mass% aqueous solution of potassium hydroxide 3 mass parts
49.9 parts by mass of water
C)
Seraquil alcohol 1.5 parts by mass
Glyceryl monostearate 0.5 parts by mass
Sucrose monolaurate 0.1 parts by mass
Vaseline 5 parts by mass
[0024]
<Example 2>
By operating in the same manner as in Example 1, emulsification type high viscosity essence 2 (cosmetic) was prepared according to the following formulation.
[0025]
I)
Acrylic acid-alkyl methacrylate copolymer
(Trade name "Pemren TR-2", manufactured by Goodrich) 0.2 parts by mass
Carboxyvinyl polymer 0.2 parts by mass
1,3-butanediol 5 parts by mass
1,2-hexylene glycol 2 parts by mass
Polyethylene glycol 6000 2 parts by mass
Magnesium phosphate ascorbate 0.3 parts by mass
0.3 parts by mass of 4-n-butyl resorcinol
Water 30 parts by mass
B)
10 mass% aqueous solution of potassium hydroxide 3 mass parts
49.9 parts by mass of water
C)
Seraquil alcohol 1.5 parts by mass
Glyceryl monostearate 0.5 parts by mass
Sucrose monolaurate 0.1 parts by mass
Vaseline 5 parts by mass
[0026]
<Example 3>
By operating in the same manner as in Example 1, emulsified high-viscosity essence 3 (cosmetic) was prepared according to the following formulation.
[0027]
I)
Acrylic acid-alkyl methacrylate copolymer
(Trade name "Pemren TR-2", manufactured by Goodrich) 0.2 parts by mass
Carboxyvinyl polymer 0.2 parts by mass
1,3-butanediol 5 parts by mass
1,2-hexylene glycol 2 parts by mass
Polyethylene glycol 6000 2 parts by mass
0.3 parts by mass of ascorbic acid-2-glucoside
0.3 parts by mass of 4-n-butyl resorcinol
Water 30 parts by mass
B)
10 mass% aqueous solution of potassium hydroxide 3 mass parts
49.9 parts by mass of water
C)
Seraquil alcohol 1.5 parts by mass
Glyceryl monostearate 0.5 parts by mass
Sucrose monolaurate 0.1 parts by mass
Vaseline 5 parts by mass
[0028]
<Comparative Example 1>
In the same manner as in Example 2, emulsified high-viscosity comparative essence 1 (cosmetic) in which 4-n-butyl resorcinol was replaced with magnesium ascorbate according to the following formulation was prepared.
[0029]
I)
Acrylic acid-alkyl methacrylate copolymer
(Trade name "Pemren TR-2", manufactured by Goodrich) 0.2 parts by mass
Carboxyvinyl polymer 0.2 parts by mass
1,3-butanediol 5 parts by mass
1,2-hexylene glycol 2 parts by mass
Polyethylene glycol 6000 2 parts by mass
Magnesium phosphate ascorbate 0.6 parts by mass
Water 30 parts by mass
B)
10 mass% aqueous solution of potassium hydroxide 3 mass parts
49.9 parts by mass of water
C)
Seraquil alcohol 1.5 parts by mass
Glyceryl monostearate 0.5 parts by mass
Sucrose monolaurate 0.1 parts by mass
Vaseline 5 parts by mass
[0030]
<Comparative Example 2>
By operating in the same manner as in Example 1, an emulsified type high viscosity comparative essence 2 (cosmetic) in which sodium ascorbate was replaced with 4-n-butyl resorcinol according to the following formulation was prepared.
[0031]
I)
Acrylic acid-alkyl methacrylate copolymer
(Trade name "Pemren TR-2", manufactured by Goodrich) 0.2 parts by mass
Carboxyvinyl polymer 0.2 parts by mass
1,3-butanediol 5 parts by mass
1,2-hexylene glycol 2 parts by mass
Polyethylene glycol 6000 2 parts by mass
0.6 parts by mass of 4-n-butyl resorcinol
Water 30 parts by mass
B)
10 mass% aqueous solution of potassium hydroxide 3 mass parts
49.9 parts by mass of water
C)
Seraquil alcohol 1.5 parts by mass
Glyceryl monostearate 0.5 parts by mass
Sucrose monolaurate 0.1 parts by mass
Vaseline 5 parts by mass
[0032]
<Comparative Example 3>
The same operation as in Example 2 was carried out to prepare an emulsified high-viscosity comparative essence 3 (cosmetic) in which 4-n-butyl resorcinol was replaced with 4-isoamyl resorcinol according to the following formulation.
[0033]
I)
Acrylic acid-alkyl methacrylate copolymer
(Trade name "Pemren TR-2", manufactured by Goodrich) 0.2 parts by mass
Carboxyvinyl polymer 0.2 parts by mass
1,3-butanediol 5 parts by mass
1,2-hexylene glycol 2 parts by mass
Polyethylene glycol 6000 2 parts by mass
Magnesium phosphate ascorbate 0.3 parts by mass
0.3 parts by mass of 4-isoamyl resorcinol
Water 30 parts by mass
B)
10 mass% aqueous solution of potassium hydroxide 3 mass parts
49.9 parts by mass of water
C)
Seraquil alcohol 1.5 parts by mass
Glyceryl monostearate 0.5 parts by mass
Sucrose monolaurate 0.1 parts by mass
Vaseline 5 parts by mass
[0034]
<Comparative Example 4>
The same operation as in Example 2 was carried out to prepare an emulsified high-viscosity comparative essence 4 (cosmetic) in which 4-n-butyl resorcinol was replaced with 4-n-propyl resorcinol according to the following formulation.
[0035]
I)
Acrylic acid-alkyl methacrylate copolymer
(Trade name "Pemren TR-2", manufactured by Goodrich) 0.2 parts by mass
Carboxyvinyl polymer 0.2 parts by mass
1,3-butanediol 5 parts by mass
1,2-hexylene glycol 2 parts by mass
Polyethylene glycol 6000 2 parts by mass
Magnesium phosphate ascorbate 0.3 parts by mass
0.3 parts by mass of 4-n-propyl resorcinol
Water 30 parts by mass
B)
10 mass% aqueous solution of potassium hydroxide 3 mass parts
49.9 parts by mass of water
C)
Seraquil alcohol 1.5 parts by mass
Glyceryl monostearate 0.5 parts by mass
Sucrose monolaurate 0.1 parts by mass
Vaseline 5 parts by mass
[0036]
<Test Example 1>
Seventy persons suffering from dullness were collected and tested for the dullness-improving effect of the essences (cosmetics) of Examples 1 to 3 and Comparative Examples 1 to 4. Seventy panelists were divided into seven groups of ten persons so that characteristic values such as age and degree of dullness were not biased. One cosmetic was distributed to each group, and each group was administered twice a day in the morning and evening for eight weeks. At the start of the test and at the end of the test, keratinocytes were collected from the inside of the upper arm and the cheek using an adhesive tape. At the same time, the degree of dullness was judged by visual judgment of three experts.
[0037]
The degree of dullness was determined according to the following criteria.
Score 1: No dullness is felt
Score 2: slightly dull
Score 3: a little dullness is felt
Score 4: Dullness is clearly felt
Score 5: Dullness is noticeable
[0038]
The results are shown in Table 1 as average scores. This shows that the skin external preparation of the present invention (essences 1 to 3 of Examples 1 to 3) has improved dullness. The keratinocytes were captured as an image using a video microscope manufactured by Moritex Corporation, and a B image was obtained by extracting only the B component from the RGB components of the image. A value (B transmission loss ratio) was obtained by dividing the luminance of the part by the luminance of the inner part of the upper arm. Table 1 shows the average value. This value was less than 1, and reflected light having less B component was observed in the keratinocytes of the cheek than in the inner part of the upper arm. In other words, it can be seen that the keratinocytes of the cheek have a yellow or brownish color compared to the inner part of the upper arm. It can be seen that the yellow or brown coloring of the keratinocytes in the cheeks was improved by administering the skin external preparation of the present invention, and the B transmission loss ratio was close to 1. In Comparative Examples (Comparative Essences 1 to 4 of Comparative Examples 1 to 4), this effect was not significantly observed.
[0039]
[Table 1]
<Example 4>
In the same manner as in Example 1, an essence (cosmetic) of the skin external preparation of the present invention was prepared according to the following formulation. In the same study as in Test Example 1, the B transmission loss ratio changed from 0.55 to 0.83.
[0041]
I)
Acrylic acid-alkyl methacrylate copolymer
(Trade name "Pemren TR-2", manufactured by Goodrich) 0.2 parts by mass
Carboxyvinyl polymer 0.2 parts by weight
1,3-butanediol 5 parts by weight
1,2-hexylene glycol 2 parts by weight
Polyethylene glycol 6000 2 parts by weight
Ascorbic acid-2-glucoside 1 part by weight
0.5 parts by weight of 4-n-butyl resorcinol
30 parts by weight of water
B)
10% by weight aqueous solution of potassium hydroxide 3 parts by weight
49 parts by weight of water
C)
Seraquil alcohol 1.5 parts by weight
Glyceryl monostearate 0.5 parts by weight
0.1 parts by weight of sucrose monolaurate
Vaseline 5 parts by weight
[0042]
【The invention's effect】
ADVANTAGE OF THE INVENTION According to this invention, the external use for skin which can improve the dullness etc. which generate | occur | produces by the yellowing of skin, ie, can improve the phenomenon (dullness of skin) which looks visually dull also other than what is caused by melanin pigmentation. An agent can be provided.
Claims (6)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2003150524A JP4080946B2 (en) | 2003-05-28 | 2003-05-28 | Skin preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2003150524A JP4080946B2 (en) | 2003-05-28 | 2003-05-28 | Skin preparation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004352627A true JP2004352627A (en) | 2004-12-16 |
| JP4080946B2 JP4080946B2 (en) | 2008-04-23 |
Family
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|---|---|---|---|
| JP2003150524A Expired - Fee Related JP4080946B2 (en) | 2003-05-28 | 2003-05-28 | Skin preparation |
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| Country | Link |
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Cited By (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2006282554A (en) * | 2005-03-31 | 2006-10-19 | Kuraray Co Ltd | External preparation for skin of dosage form of essence |
| JP2006328026A (en) * | 2005-05-30 | 2006-12-07 | Kuraray Co Ltd | Liposome and skin care preparation containing the same |
| JP2009023947A (en) * | 2007-07-19 | 2009-02-05 | Kuraray Co Ltd | Skin care preparation for external use |
| WO2009145300A1 (en) * | 2008-05-29 | 2009-12-03 | 株式会社資生堂 | External preparation for skin |
| JP2009286735A (en) * | 2008-05-29 | 2009-12-10 | Shiseido Co Ltd | Skin care preparation |
| JP2012254957A (en) * | 2011-06-09 | 2012-12-27 | Showa Denko Kk | External skin preparation and production method thereof |
| JP2013216640A (en) * | 2012-04-12 | 2013-10-24 | Pola Chemical Industries Inc | Skin care composition |
| FR2993775A1 (en) * | 2012-07-24 | 2014-01-31 | Cfeb Sisley | Cosmetic composition, useful for depigmenting skin exposed to sun, comprises a synergistic combination of a melanogenesis inhibitor of resorcinol, a stable antioxidant derived from oxidation of ascorbic acid and rhubarb root extract |
| JP2015209377A (en) * | 2014-04-24 | 2015-11-24 | ポーラ化成工業株式会社 | Oil-in-water emulsion composition |
| WO2017038951A1 (en) * | 2015-09-02 | 2017-03-09 | 株式会社林原 | External preparation for skin for reducing skin yellowness |
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| JP2000256131A (en) * | 1999-03-09 | 2000-09-19 | Kose Corp | Tyrosinase production inhibitor and skin lotion containing the same |
| JP2001158730A (en) * | 1999-12-03 | 2001-06-12 | Pola Chem Ind Inc | Cosmetic for improving dark skin color |
| JP2002541074A (en) * | 1999-03-24 | 2002-12-03 | ラ・ロッシュ・ポセイ・ラボラトワール・ファーマスティーク | Use of vitamin C analogs for increasing the level of skin cell differentiation and / or proliferation |
| JP2004277352A (en) * | 2003-03-17 | 2004-10-07 | Sansho Seiyaku Co Ltd | External preparation for skin |
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| JPH0249715A (en) * | 1988-05-09 | 1990-02-20 | Kuraray Co Ltd | Beautifying agent |
| JPH0278611A (en) * | 1988-09-13 | 1990-03-19 | Kansai Paint Co Ltd | Skin cleaning agent |
| JPH03127724A (en) * | 1989-10-11 | 1991-05-30 | Kansai Paint Co Ltd | Bath agent |
| JPH054905A (en) * | 1990-10-31 | 1993-01-14 | Pola Chem Ind Inc | Cosmetic |
| JPH0616532A (en) * | 1992-03-17 | 1994-01-25 | Eisai Co Ltd | Whitening and beautifying agent |
| JP2000038334A (en) * | 1998-07-21 | 2000-02-08 | Pola Chem Ind Inc | Bleaching cosmetic containing resorcinol derivative |
| JP2000128762A (en) * | 1998-10-28 | 2000-05-09 | Kose Corp | Melanogenesis inhibitor and skin preparation for external use for beautifying containing the same |
| JP2000256131A (en) * | 1999-03-09 | 2000-09-19 | Kose Corp | Tyrosinase production inhibitor and skin lotion containing the same |
| JP2002541074A (en) * | 1999-03-24 | 2002-12-03 | ラ・ロッシュ・ポセイ・ラボラトワール・ファーマスティーク | Use of vitamin C analogs for increasing the level of skin cell differentiation and / or proliferation |
| JP2001158730A (en) * | 1999-12-03 | 2001-06-12 | Pola Chem Ind Inc | Cosmetic for improving dark skin color |
| JP2004277352A (en) * | 2003-03-17 | 2004-10-07 | Sansho Seiyaku Co Ltd | External preparation for skin |
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| JP2006282554A (en) * | 2005-03-31 | 2006-10-19 | Kuraray Co Ltd | External preparation for skin of dosage form of essence |
| JP2006328026A (en) * | 2005-05-30 | 2006-12-07 | Kuraray Co Ltd | Liposome and skin care preparation containing the same |
| JP2009023947A (en) * | 2007-07-19 | 2009-02-05 | Kuraray Co Ltd | Skin care preparation for external use |
| WO2009145300A1 (en) * | 2008-05-29 | 2009-12-03 | 株式会社資生堂 | External preparation for skin |
| JP2009286735A (en) * | 2008-05-29 | 2009-12-10 | Shiseido Co Ltd | Skin care preparation |
| JP2012254957A (en) * | 2011-06-09 | 2012-12-27 | Showa Denko Kk | External skin preparation and production method thereof |
| JP2013216640A (en) * | 2012-04-12 | 2013-10-24 | Pola Chemical Industries Inc | Skin care composition |
| FR2993775A1 (en) * | 2012-07-24 | 2014-01-31 | Cfeb Sisley | Cosmetic composition, useful for depigmenting skin exposed to sun, comprises a synergistic combination of a melanogenesis inhibitor of resorcinol, a stable antioxidant derived from oxidation of ascorbic acid and rhubarb root extract |
| JP2015209377A (en) * | 2014-04-24 | 2015-11-24 | ポーラ化成工業株式会社 | Oil-in-water emulsion composition |
| WO2017038951A1 (en) * | 2015-09-02 | 2017-03-09 | 株式会社林原 | External preparation for skin for reducing skin yellowness |
| CN107920981A (en) * | 2015-09-02 | 2018-04-17 | 株式会社林原 | Dark yellow reduction skin preparations for extenal use |
| JPWO2017038951A1 (en) * | 2015-09-02 | 2018-06-14 | 株式会社林原 | Skin external preparation for reducing yellowing |
| US10568827B2 (en) | 2015-09-02 | 2020-02-25 | Hayashibara Co., Ltd. | External dermal agent for reducing yellowish dullness |
| JP2021073320A (en) * | 2015-09-02 | 2021-05-13 | 株式会社林原 | External dermal agent for reducing skin yellowness |
| JP7049496B2 (en) | 2015-09-02 | 2022-04-06 | 株式会社林原 | External skin agent for reducing yellowing |
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