JP6723711B2 - 外用組成物 - Google Patents
外用組成物 Download PDFInfo
- Publication number
- JP6723711B2 JP6723711B2 JP2015190820A JP2015190820A JP6723711B2 JP 6723711 B2 JP6723711 B2 JP 6723711B2 JP 2015190820 A JP2015190820 A JP 2015190820A JP 2015190820 A JP2015190820 A JP 2015190820A JP 6723711 B2 JP6723711 B2 JP 6723711B2
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- JP
- Japan
- Prior art keywords
- hyaluronic acid
- salt
- feeling
- component
- composition
- 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.)
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- 239000000203 mixture Substances 0.000 title claims description 68
- 229920002674 hyaluronan Polymers 0.000 claims description 97
- 229960003160 hyaluronic acid Drugs 0.000 claims description 97
- -1 hyaluronic acid oligosaccharide Chemical class 0.000 claims description 95
- 229920001542 oligosaccharide Polymers 0.000 claims description 58
- 150000003839 salts Chemical class 0.000 claims description 57
- KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 claims description 50
- 239000002628 heparin derivative Substances 0.000 claims description 18
- 229940079593 drug Drugs 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 8
- 239000002537 cosmetic Substances 0.000 claims description 7
- 230000003020 moisturizing effect Effects 0.000 description 30
- 239000000194 fatty acid Substances 0.000 description 24
- 235000014113 dietary fatty acids Nutrition 0.000 description 23
- 229930195729 fatty acid Natural products 0.000 description 23
- 238000000034 method Methods 0.000 description 15
- 230000035515 penetration Effects 0.000 description 14
- 239000000047 product Substances 0.000 description 14
- 229910052708 sodium Inorganic materials 0.000 description 13
- 239000011734 sodium Substances 0.000 description 13
- 235000015424 sodium Nutrition 0.000 description 13
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 11
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 10
- 229910052799 carbon Inorganic materials 0.000 description 10
- 150000004665 fatty acids Chemical class 0.000 description 10
- 239000003921 oil Substances 0.000 description 10
- 235000019198 oils Nutrition 0.000 description 10
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 10
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 9
- 125000004432 carbon atom Chemical group C* 0.000 description 9
- 239000004359 castor oil Substances 0.000 description 9
- 238000011156 evaluation Methods 0.000 description 9
- 238000009472 formulation Methods 0.000 description 9
- 230000000052 comparative effect Effects 0.000 description 8
- 239000006210 lotion Substances 0.000 description 8
- 239000004166 Lanolin Substances 0.000 description 7
- 235000019438 castor oil Nutrition 0.000 description 7
- 239000002552 dosage form Substances 0.000 description 7
- 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 7
- 235000019388 lanolin Nutrition 0.000 description 7
- 229940039717 lanolin Drugs 0.000 description 7
- 239000007788 liquid Substances 0.000 description 7
- 230000035807 sensation Effects 0.000 description 7
- 235000000346 sugar Nutrition 0.000 description 7
- 150000001298 alcohols Chemical class 0.000 description 6
- 229910052783 alkali metal Inorganic materials 0.000 description 6
- 238000004519 manufacturing process Methods 0.000 description 6
- 159000000000 sodium salts Chemical class 0.000 description 6
- 239000000126 substance Substances 0.000 description 6
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 5
- 239000002585 base Substances 0.000 description 5
- 239000000470 constituent Substances 0.000 description 5
- 150000002016 disaccharides Chemical class 0.000 description 5
- RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 5
- 235000011187 glycerol Nutrition 0.000 description 5
- 150000002772 monosaccharides Chemical class 0.000 description 5
- 238000002360 preparation method Methods 0.000 description 5
- 150000008163 sugars Chemical class 0.000 description 5
- KWIUHFFTVRNATP-UHFFFAOYSA-N Betaine Natural products C[N+](C)(C)CC([O-])=O KWIUHFFTVRNATP-UHFFFAOYSA-N 0.000 description 4
- AEMOLEFTQBMNLQ-AQKNRBDQSA-N D-glucopyranuronic acid Chemical group OC1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O AEMOLEFTQBMNLQ-AQKNRBDQSA-N 0.000 description 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 4
- IAJILQKETJEXLJ-UHFFFAOYSA-N Galacturonsaeure Natural products O=CC(O)C(O)C(O)C(O)C(O)=O IAJILQKETJEXLJ-UHFFFAOYSA-N 0.000 description 4
- 229920001214 Polysorbate 60 Polymers 0.000 description 4
- 239000002253 acid Substances 0.000 description 4
- 229940024606 amino acid Drugs 0.000 description 4
- 239000002280 amphoteric surfactant Substances 0.000 description 4
- 229960003237 betaine Drugs 0.000 description 4
- 150000001720 carbohydrates Chemical class 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 229940097043 glucuronic acid Drugs 0.000 description 4
- 238000009629 microbiological culture Methods 0.000 description 4
- 238000002156 mixing Methods 0.000 description 4
- 239000007787 solid Substances 0.000 description 4
- 239000004094 surface-active agent Substances 0.000 description 4
- 239000001993 wax Substances 0.000 description 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 3
- 102000004190 Enzymes Human genes 0.000 description 3
- 108090000790 Enzymes Proteins 0.000 description 3
- 229920002683 Glycosaminoglycan Polymers 0.000 description 3
- 108010003272 Hyaluronate lyase Proteins 0.000 description 3
- 102000009066 Hyaluronoglucosaminidase Human genes 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
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical class CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 3
- 239000000654 additive Substances 0.000 description 3
- 239000007864 aqueous solution Substances 0.000 description 3
- 230000017531 blood circulation Effects 0.000 description 3
- 159000000007 calcium salts Chemical class 0.000 description 3
- 235000014633 carbohydrates Nutrition 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 239000011248 coating agent Substances 0.000 description 3
- 238000000576 coating method Methods 0.000 description 3
- 239000003240 coconut oil Substances 0.000 description 3
- 235000019864 coconut oil Nutrition 0.000 description 3
- 239000006071 cream Substances 0.000 description 3
- 238000000354 decomposition reaction Methods 0.000 description 3
- 238000004090 dissolution Methods 0.000 description 3
- 229940088598 enzyme Drugs 0.000 description 3
- 239000000499 gel Substances 0.000 description 3
- 229960002773 hyaluronidase Drugs 0.000 description 3
- 230000003301 hydrolyzing effect Effects 0.000 description 3
- 159000000003 magnesium salts Chemical class 0.000 description 3
- 239000011259 mixed solution Substances 0.000 description 3
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 3
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 3
- 239000003755 preservative agent Substances 0.000 description 3
- 230000001737 promoting effect Effects 0.000 description 3
- 150000003222 pyridines Chemical class 0.000 description 3
- 238000011160 research Methods 0.000 description 3
- 239000001593 sorbitan monooleate Substances 0.000 description 3
- 229940035049 sorbitan monooleate Drugs 0.000 description 3
- 238000003786 synthesis reaction Methods 0.000 description 3
- XOAAWQZATWQOTB-UHFFFAOYSA-N taurine Chemical compound NCCS(O)(=O)=O XOAAWQZATWQOTB-UHFFFAOYSA-N 0.000 description 3
- 239000002562 thickening agent Substances 0.000 description 3
- IMFACGCPASFAPR-UHFFFAOYSA-N tributylamine Chemical class CCCCN(CCCC)CCCC IMFACGCPASFAPR-UHFFFAOYSA-N 0.000 description 3
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-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
- XDOFQFKRPWOURC-UHFFFAOYSA-N 16-methylheptadecanoic acid Chemical compound CC(C)CCCCCCCCCCCCCCC(O)=O XDOFQFKRPWOURC-UHFFFAOYSA-N 0.000 description 2
- 229920002567 Chondroitin Polymers 0.000 description 2
- YCKRFDGAMUMZLT-UHFFFAOYSA-N Fluorine atom Chemical compound [F] YCKRFDGAMUMZLT-UHFFFAOYSA-N 0.000 description 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- QZXSMBBFBXPQHI-UHFFFAOYSA-N N-(dodecanoyl)ethanolamine Chemical compound CCCCCCCCCCCC(=O)NCCO QZXSMBBFBXPQHI-UHFFFAOYSA-N 0.000 description 2
- OVRNDRQMDRJTHS-UHFFFAOYSA-N N-acelyl-D-glucosamine Natural products CC(=O)NC1C(O)OC(CO)C(O)C1O OVRNDRQMDRJTHS-UHFFFAOYSA-N 0.000 description 2
- OVRNDRQMDRJTHS-FMDGEEDCSA-N N-acetyl-beta-D-glucosamine Chemical group CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O OVRNDRQMDRJTHS-FMDGEEDCSA-N 0.000 description 2
- MBLBDJOUHNCFQT-LXGUWJNJSA-N N-acetylglucosamine Natural products CC(=O)N[C@@H](C=O)[C@@H](O)[C@H](O)[C@H](O)CO MBLBDJOUHNCFQT-LXGUWJNJSA-N 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- 239000002202 Polyethylene glycol Substances 0.000 description 2
- 239000004373 Pullulan Substances 0.000 description 2
- 229920001218 Pullulan Polymers 0.000 description 2
- 241001524200 Sinomonas atrocyanea Species 0.000 description 2
- 229920002385 Sodium hyaluronate Polymers 0.000 description 2
- 241000187747 Streptomyces Species 0.000 description 2
- 229930006000 Sucrose Natural products 0.000 description 2
- ULUAUXLGCMPNKK-UHFFFAOYSA-N Sulfobutanedioic acid Chemical compound OC(=O)CC(C(O)=O)S(O)(=O)=O ULUAUXLGCMPNKK-UHFFFAOYSA-N 0.000 description 2
- 239000006096 absorbing agent Substances 0.000 description 2
- 229910052784 alkaline earth metal Inorganic materials 0.000 description 2
- 239000003945 anionic surfactant Substances 0.000 description 2
- 230000003110 anti-inflammatory effect Effects 0.000 description 2
- 230000003796 beauty Effects 0.000 description 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 2
- 239000003093 cationic surfactant Substances 0.000 description 2
- OSASVXMJTNOKOY-UHFFFAOYSA-N chlorobutanol Chemical compound CC(C)(O)C(Cl)(Cl)Cl OSASVXMJTNOKOY-UHFFFAOYSA-N 0.000 description 2
- DLGJWSVWTWEWBJ-HGGSSLSASA-N chondroitin Chemical compound CC(O)=N[C@@H]1[C@H](O)O[C@H](CO)[C@H](O)[C@@H]1OC1[C@H](O)[C@H](O)C=C(C(O)=O)O1 DLGJWSVWTWEWBJ-HGGSSLSASA-N 0.000 description 2
- 230000000593 degrading effect Effects 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
- YRIUSKIDOIARQF-UHFFFAOYSA-N dodecyl benzenesulfonate Chemical compound CCCCCCCCCCCCOS(=O)(=O)C1=CC=CC=C1 YRIUSKIDOIARQF-UHFFFAOYSA-N 0.000 description 2
- 229940071161 dodecylbenzenesulfonate Drugs 0.000 description 2
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- 238000010438 heat treatment Methods 0.000 description 2
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 2
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- 150000002430 hydrocarbons Chemical class 0.000 description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 2
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- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 2
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- 229920006395 saturated elastomer Polymers 0.000 description 2
- 229940010747 sodium hyaluronate Drugs 0.000 description 2
- YWIVKILSMZOHHF-QJZPQSOGSA-N sodium;(2s,3s,4s,5r,6r)-6-[(2s,3r,4r,5s,6r)-3-acetamido-2-[(2s,3s,4r,5r,6r)-6-[(2r,3r,4r,5s,6r)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2- Chemical compound [Na+].CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 YWIVKILSMZOHHF-QJZPQSOGSA-N 0.000 description 2
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- 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
- 238000003756 stirring Methods 0.000 description 2
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- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 description 2
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- WFXHUBZUIFLWCV-UHFFFAOYSA-N (2,2-dimethyl-3-octanoyloxypropyl) octanoate Chemical compound CCCCCCCC(=O)OCC(C)(C)COC(=O)CCCCCCC WFXHUBZUIFLWCV-UHFFFAOYSA-N 0.000 description 1
- CUNWUEBNSZSNRX-RKGWDQTMSA-N (2r,3r,4r,5s)-hexane-1,2,3,4,5,6-hexol;(z)-octadec-9-enoic acid Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.CCCCCCCC\C=C/CCCCCCCC(O)=O.CCCCCCCC\C=C/CCCCCCCC(O)=O.CCCCCCCC\C=C/CCCCCCCC(O)=O CUNWUEBNSZSNRX-RKGWDQTMSA-N 0.000 description 1
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 description 1
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- FCAXDVKLWVSHGT-KVVVOXFISA-N (z)-docos-13-enoic acid;propane-1,2,3-triol Chemical compound OCC(O)CO.CCCCCCCC\C=C/CCCCCCCCCCCC(O)=O FCAXDVKLWVSHGT-KVVVOXFISA-N 0.000 description 1
- ZORQXIQZAOLNGE-UHFFFAOYSA-N 1,1-difluorocyclohexane Chemical compound FC1(F)CCCCC1 ZORQXIQZAOLNGE-UHFFFAOYSA-N 0.000 description 1
- DMBUODUULYCPAK-UHFFFAOYSA-N 1,3-bis(docosanoyloxy)propan-2-yl docosanoate Chemical compound CCCCCCCCCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCCCCCCCCCC DMBUODUULYCPAK-UHFFFAOYSA-N 0.000 description 1
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- 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
- XPALGXXLALUMLE-UHFFFAOYSA-N 2-(dimethylamino)tetradecanoic acid Chemical compound CCCCCCCCCCCCC(N(C)C)C(O)=O XPALGXXLALUMLE-UHFFFAOYSA-N 0.000 description 1
- AVBJHQDHVYGQLS-UHFFFAOYSA-N 2-(dodecanoylamino)pentanedioic acid Chemical compound CCCCCCCCCCCC(=O)NC(C(O)=O)CCC(O)=O AVBJHQDHVYGQLS-UHFFFAOYSA-N 0.000 description 1
- FKOKUHFZNIUSLW-UHFFFAOYSA-N 2-Hydroxypropyl stearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(C)O FKOKUHFZNIUSLW-UHFFFAOYSA-N 0.000 description 1
- LNCJHVLXANMHHD-UHFFFAOYSA-N 2-[2-heptadecyl-1-(2-hydroxyethyl)-4,5-dihydroimidazol-1-ium-1-yl]acetate Chemical compound CCCCCCCCCCCCCCCCCC1=NCC[N+]1(CCO)CC([O-])=O LNCJHVLXANMHHD-UHFFFAOYSA-N 0.000 description 1
- WBIQQQGBSDOWNP-UHFFFAOYSA-N 2-dodecylbenzenesulfonic acid Chemical compound CCCCCCCCCCCCC1=CC=CC=C1S(O)(=O)=O WBIQQQGBSDOWNP-UHFFFAOYSA-N 0.000 description 1
- JGUMTYWKIBJSTN-UHFFFAOYSA-N 2-ethylhexyl 4-[[4,6-bis[4-(2-ethylhexoxycarbonyl)anilino]-1,3,5-triazin-2-yl]amino]benzoate Chemical compound C1=CC(C(=O)OCC(CC)CCCC)=CC=C1NC1=NC(NC=2C=CC(=CC=2)C(=O)OCC(CC)CCCC)=NC(NC=2C=CC(=CC=2)C(=O)OCC(CC)CCCC)=N1 JGUMTYWKIBJSTN-UHFFFAOYSA-N 0.000 description 1
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- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 1
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Description
項1. (A)ヘパリン類似物質と、(B)ヒアルロン酸オリゴ糖及び/又はその塩を含有する、外用組成物。
項2. 前記(A)成分が0.05〜3重量%である、項1記載の外用組成物。
項3. 前記(A)成分1重量部あたり、前記(B)成分が0.002〜2重量部である、項1又は2記載の外用組成物。
項4. 医薬品又は化粧料である、項1〜3のいずれかに記載の外用組成物。
本発明の外用組成物は、ヘパリン類似物質((A)成分と表記することもある)と、ヒアルロン酸オリゴ糖及び/又はその塩((B)成分と表記することもある)を含有することを特徴とする。以下、本発明の外用組成物について詳述する。
ヘパリン類似物質とは、コンドロイチン多硫酸等の多硫酸化ムコ多糖であり、保湿作用、抗炎症作用、血行促進作用等を有することが知られている公知の薬剤である。
本発明の外用組成物は、前記(A)成分と共に、ヒアルロン酸オリゴ糖及び/又はその塩を含有する。ヒアルロン酸オリゴ糖及び/又はその塩を使用することにより、(A)成分が配合されているにもかかわらず、塗布時のぬるつき感を抑制えることで肌馴染みに優れ、かつ満足のいく浸透感及び保湿感を備えさせることが可能になる。
本発明の外用組成物は、重厚な塗布感及び保湿感を備えさせるために、必要に応じて、ヒアルロン酸及び/又はその塩((C-1)成分と表記することもある)を含んでいてもよい。
本発明の外用組成物は、水を基剤として用いて所望の剤型に調製される。本発明の外用組成物において、水の配合量については、外用組成物の剤型等に応じて適宜設定すればよいが、例えば20〜95重量%、好ましくは30〜95重量%、更に好ましくは35〜95重量%が挙げられる。
本発明の外用組成物は、前述する成分の他に、必要に応じて、生理学的に有用な機能性を示す機能性成分が含まれていてもよい。このような機能性成分としては、化粧料や外用医薬品等に配合可能なものであることを限度として特に制限されないが、例えば、水溶性のビタミン類、油溶性のビタミン類、酵素、ペプチド、アミノ酸、ホルモン、各種サイトカイン、各種動植物抽出物、ステロイド剤、保湿剤、美白剤、生薬、抗ヒスタミン剤、収斂剤、細胞賦活剤、角質軟化剤、局所麻酔剤、抗炎症剤、酸化防止剤、抗菌剤、鎮痒剤、皮膚保護剤、血行促進剤、ステロール類等が挙げられる。
本発明の外用組成物は、前記(A)及び(B)成分と共に、必要に応じて添加される(C-1)成分及び/又は(C-2)成分、他の機能性成分、基剤、添加剤等を混合し、所望の製剤形態に調製することによって得ることができる。また、前記(C-1)成分及び/又は(C-2)成分は、(B)成分によって水への溶解性が向上するので、本発明の外用組成物の製造において、(C-1)成分及び/又は(C-2)成分を水に溶解させる際に、(B)成分を共存させることが好ましい。(C-1)成分及び/又は(C-2)成分を水に溶解させる際に(B)成分を共存させる方法としては、例えば、(C-1)成分及び/又は(C-2)成分、並びに(B)成分を同時に水に添加する方法;水に(C-1)成分及び/又は(C-2)成分を添加し、(C-1)成分及び/又は(C-2)成分が溶解するまでに(B)成分を添加する方法;水に(B)成分を添加した後に(C-1)成分及び/又は(C-2)成分を添加する方法が挙げられる。
本発明の外用組成物は、液状、固形状、クリーム状、ジェル状等のいずれの剤型であってもよい。これらの剤型の中でも、液状の外用組成物は、塗布時のぬるつき感のなさ(肌馴染みの良さ)、浸透感及び保湿感等の効果を実感し易いため、本発明の外用組成物の剤型として好適である。
以下に示す実施例、比較例、及び処方例において、「ヒアルロン酸オリゴ糖」は、特開2008−35858号公報に記載の方法に従って製造したものを使用した。具体的には、ヒアルロン酸ナトリウムの1重量%水溶液中で、アースロバクター アトロシアネウスJU-01(Arthrobacter atrocyaneus JU-01)株(独立行政法人製品評価技術基盤機構 特許微生物寄託センター 受託番号:NITE P−245)を25℃で120時間静置培養した。その後、0.22μmのメンブレンフィルターで当該菌株を除去し、凍結乾燥することにより不飽和型ヒアルロン酸オリゴ糖を得た。得られたヒアルロン酸オリゴ糖は、2糖(構成単糖数が2)であり、非還元末端に位置するグルクロン酸の4位の炭素原子に結合している水酸基が除去され、4位の炭素原子と5位の炭素原子が二重結合で結合している不飽和型の構造を有していた。
表1に示す組成の外用組成物を調製した。具体的には、室温の水に、全ての成分を同時に所定量添加し、室温でプロペラ攪拌機にて500rpmの速度で撹拌することにより、全ての成分を完全に溶解させた外用組成物を製造した。
<ぬるつき感のなさ>
1点:塗布時に滑りがあり、肌馴染みが悪い。
10点:塗布時に滑りがなく、肌馴染みが良い。
<浸透感>
1点:塗布から15秒後に浸透感がない。
10点:塗布から15秒後に浸透感がある。
<保湿感>
1点:塗布から15秒後にしっとりとした感じがない。
10点:塗布から15秒後にしっとりとした感じがある。
表2及び3に示す組成の化粧水を常法に従って調製した。具体的には、まず表2及び3の(II)に示す成分を、プロペラ撹拌機にて500rmpの速度で撹拌混合することにより溶解し、混合液(II)を調製した。ついで、(I)及び(III)に示す成分をそれぞれ撹拌、溶解し、混合液(I)及び(III)を調製した。混合液(III)を撹拌しながら、混合液(I)及び(II)を加えて溶解させることにより、化粧水を調製した。得られた化粧水は、いずれも、ヒアルロン酸オリゴ糖を含有しない場合に比べて、塗布時のぬるつき感のなさ並びに塗布後の浸透感及び保湿感に優れていた。また、処方例4〜20については、混合液(II)の調製の際、ヒアルロン酸オリゴ糖の存在下でヒアルロン酸ナトリウムを溶解させることで、ヒアルロン酸オリゴ糖を含まない場合に比べて、ヒアルロン酸ナトリウムの溶解時間を約半分に短縮できた。具体的には、処方例4では溶解時間は35分程度であったが、処方例4からヒアルロン酸オリゴ糖を除いた場合には80分程度要した。
Claims (4)
- (A)ヘパリン類似物質と、(B)ヒアルロン酸オリゴ糖及び/又はその塩を含有する、外用組成物(但し、養毛化粧料と、カチオン化ヒアルロン酸及び/又はその塩を含有する場合とを除く)。
- 前記(A)成分が0.05〜3重量%である、請求項1記載の外用組成物。
- 前記(A)成分1重量部あたり、前記(B)成分が0.002〜2重量部である、請求項1又は2記載の外用組成物。
- 医薬品又は化粧料である、請求項1〜3のいずれかに記載の外用組成物。
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