JP2020100576A - External composition for skin - Google Patents
External composition for skin Download PDFInfo
- Publication number
- JP2020100576A JP2020100576A JP2018238235A JP2018238235A JP2020100576A JP 2020100576 A JP2020100576 A JP 2020100576A JP 2018238235 A JP2018238235 A JP 2018238235A JP 2018238235 A JP2018238235 A JP 2018238235A JP 2020100576 A JP2020100576 A JP 2020100576A
- Authority
- JP
- Japan
- Prior art keywords
- skin
- retinol
- external composition
- acid
- 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.)
- Granted
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 71
- 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 claims abstract description 87
- 235000020944 retinol Nutrition 0.000 claims abstract description 45
- 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 claims abstract description 42
- 230000001139 anti-pruritic effect Effects 0.000 claims abstract description 42
- 239000011607 retinol Substances 0.000 claims abstract description 37
- 229960003471 retinol Drugs 0.000 claims abstract description 37
- POJWUDADGALRAB-UHFFFAOYSA-N allantoin Chemical compound NC(=O)NC1NC(=O)NC1=O POJWUDADGALRAB-UHFFFAOYSA-N 0.000 claims abstract description 36
- 229960000520 diphenhydramine Drugs 0.000 claims abstract description 19
- 150000003839 salts Chemical class 0.000 claims abstract description 18
- 229960000458 allantoin Drugs 0.000 claims abstract description 17
- POJWUDADGALRAB-PVQJCKRUSA-N Allantoin Natural products NC(=O)N[C@@H]1NC(=O)NC1=O POJWUDADGALRAB-PVQJCKRUSA-N 0.000 claims abstract description 16
- ZZVUWRFHKOJYTH-UHFFFAOYSA-N diphenhydramine Chemical compound C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 ZZVUWRFHKOJYTH-UHFFFAOYSA-N 0.000 claims abstract 3
- 238000000034 method Methods 0.000 claims description 17
- 239000003908 antipruritic agent Substances 0.000 claims description 10
- 238000002156 mixing Methods 0.000 abstract 1
- 210000003491 skin Anatomy 0.000 description 65
- -1 diphenyl disulfonate Chemical class 0.000 description 22
- 208000003251 Pruritus Diseases 0.000 description 21
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 18
- SPCKHVPPRJWQRZ-UHFFFAOYSA-N 2-benzhydryloxy-n,n-dimethylethanamine;2-hydroxypropane-1,2,3-tricarboxylic acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O.C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 SPCKHVPPRJWQRZ-UHFFFAOYSA-N 0.000 description 16
- 230000002393 scratching effect Effects 0.000 description 14
- 150000004347 all-trans-retinol derivatives Chemical class 0.000 description 12
- 150000002148 esters Chemical class 0.000 description 11
- 235000014113 dietary fatty acids Nutrition 0.000 description 10
- 239000000194 fatty acid Substances 0.000 description 10
- 229930195729 fatty acid Natural products 0.000 description 10
- 238000006748 scratching Methods 0.000 description 10
- 239000002202 Polyethylene glycol Substances 0.000 description 8
- 239000003814 drug Substances 0.000 description 8
- 229920001223 polyethylene glycol Polymers 0.000 description 8
- 150000004665 fatty acids Chemical class 0.000 description 7
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 6
- 229940079593 drug Drugs 0.000 description 6
- 230000007803 itching Effects 0.000 description 6
- 239000000126 substance Substances 0.000 description 6
- 229960001727 tretinoin Drugs 0.000 description 6
- 229930002330 retinoic acid Natural products 0.000 description 5
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 4
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 4
- FPIPGXGPPPQFEQ-BOOMUCAASA-N Vitamin A Natural products OC/C=C(/C)\C=C\C=C(\C)/C=C/C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-BOOMUCAASA-N 0.000 description 4
- 239000002253 acid Substances 0.000 description 4
- SHGAZHPCJJPHSC-YCNIQYBTSA-N all-trans-retinoic acid Chemical compound OC(=O)\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-YCNIQYBTSA-N 0.000 description 4
- 239000000739 antihistaminic agent Substances 0.000 description 4
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 4
- 238000009472 formulation Methods 0.000 description 4
- 230000001939 inductive effect Effects 0.000 description 4
- 239000003921 oil Substances 0.000 description 4
- 235000019198 oils Nutrition 0.000 description 4
- 235000019155 vitamin A Nutrition 0.000 description 4
- 239000011719 vitamin A Substances 0.000 description 4
- 229940045997 vitamin a Drugs 0.000 description 4
- 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 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- 201000004624 Dermatitis Diseases 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- 208000010201 Exanthema Diseases 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- 239000004166 Lanolin Substances 0.000 description 3
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- VYGQUTWHTHXGQB-FFHKNEKCSA-N Retinol Palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C VYGQUTWHTHXGQB-FFHKNEKCSA-N 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 239000000654 additive Substances 0.000 description 3
- 208000010668 atopic eczema Diseases 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
- GVJHHUAWPYXKBD-UHFFFAOYSA-N d-alpha-tocopherol Natural products OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 3
- 201000005884 exanthem Diseases 0.000 description 3
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 3
- 239000004615 ingredient Substances 0.000 description 3
- 235000019388 lanolin Nutrition 0.000 description 3
- 229940039717 lanolin Drugs 0.000 description 3
- 210000003141 lower extremity Anatomy 0.000 description 3
- 229920001451 polypropylene glycol Polymers 0.000 description 3
- 229920001296 polysiloxane Polymers 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- 206010037844 rash Diseases 0.000 description 3
- 230000017423 tissue regeneration Effects 0.000 description 3
- 235000010384 tocopherol Nutrition 0.000 description 3
- 229960001295 tocopherol Drugs 0.000 description 3
- 229930003799 tocopherol Natural products 0.000 description 3
- 239000011732 tocopherol Substances 0.000 description 3
- 239000001993 wax Substances 0.000 description 3
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 description 3
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 description 2
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 2
- 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 description 2
- DSSYKIVIOFKYAU-XCBNKYQSSA-N (R)-camphor Chemical compound C1C[C@@]2(C)C(=O)C[C@@H]1C2(C)C DSSYKIVIOFKYAU-XCBNKYQSSA-N 0.000 description 2
- FDCJDKXCCYFOCV-UHFFFAOYSA-N 1-hexadecoxyhexadecane Chemical compound CCCCCCCCCCCCCCCCOCCCCCCCCCCCCCCCC FDCJDKXCCYFOCV-UHFFFAOYSA-N 0.000 description 2
- ASKIVFGGGGIGKH-UHFFFAOYSA-N 2,3-dihydroxypropyl 16-methylheptadecanoate Chemical compound CC(C)CCCCCCCCCCCCCCC(=O)OCC(O)CO ASKIVFGGGGIGKH-UHFFFAOYSA-N 0.000 description 2
- FLPJVCMIKUWSDR-UHFFFAOYSA-N 2-(4-formylphenoxy)acetamide Chemical compound NC(=O)COC1=CC=C(C=O)C=C1 FLPJVCMIKUWSDR-UHFFFAOYSA-N 0.000 description 2
- LVYLCBNXHHHPSB-UHFFFAOYSA-N 2-hydroxyethyl salicylate Chemical compound OCCOC(=O)C1=CC=CC=C1O LVYLCBNXHHHPSB-UHFFFAOYSA-N 0.000 description 2
- QNAYBMKLOCPYGJ-UHFFFAOYSA-N Alanine Chemical compound CC([NH3+])C([O-])=O QNAYBMKLOCPYGJ-UHFFFAOYSA-N 0.000 description 2
- 239000005711 Benzoic acid Substances 0.000 description 2
- 241000723346 Cinnamomum camphora Species 0.000 description 2
- RGHNJXZEOKUKBD-SQOUGZDYSA-N D-gluconic acid Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O RGHNJXZEOKUKBD-SQOUGZDYSA-N 0.000 description 2
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 2
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 2
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 description 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 2
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 2
- 235000021355 Stearic acid Nutrition 0.000 description 2
- RAHZWNYVWXNFOC-UHFFFAOYSA-N Sulphur dioxide Chemical compound O=S=O RAHZWNYVWXNFOC-UHFFFAOYSA-N 0.000 description 2
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 description 2
- XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 description 2
- 239000004480 active ingredient Substances 0.000 description 2
- 125000000217 alkyl group Chemical group 0.000 description 2
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 2
- 230000001387 anti-histamine Effects 0.000 description 2
- 235000010233 benzoic acid Nutrition 0.000 description 2
- KVYGGMBOZFWZBQ-UHFFFAOYSA-N benzyl nicotinate Chemical compound C=1C=CN=CC=1C(=O)OCC1=CC=CC=C1 KVYGGMBOZFWZBQ-UHFFFAOYSA-N 0.000 description 2
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- YKPUWZUDDOIDPM-SOFGYWHQSA-N capsaicin Chemical compound COC1=CC(CNC(=O)CCCC\C=C\C(C)C)=CC=C1O YKPUWZUDDOIDPM-SOFGYWHQSA-N 0.000 description 2
- 125000004432 carbon atom Chemical group C* 0.000 description 2
- 239000004359 castor oil Substances 0.000 description 2
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- 229940074979 cetyl palmitate Drugs 0.000 description 2
- 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 description 2
- NEHNMFOYXAPHSD-UHFFFAOYSA-N citronellal Chemical compound O=CCC(C)CCC=C(C)C NEHNMFOYXAPHSD-UHFFFAOYSA-N 0.000 description 2
- 239000006071 cream Substances 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
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- 210000002919 epithelial cell Anatomy 0.000 description 2
- LNTHITQWFMADLM-UHFFFAOYSA-N gallic acid Chemical compound OC(=O)C1=CC(O)=C(O)C(O)=C1 LNTHITQWFMADLM-UHFFFAOYSA-N 0.000 description 2
- 235000011187 glycerol Nutrition 0.000 description 2
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- 229940075507 glyceryl monostearate Drugs 0.000 description 2
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 2
- PXDJXZJSCPSGGI-UHFFFAOYSA-N hexadecanoic acid hexadecyl ester Natural products CCCCCCCCCCCCCCCCOC(=O)CCCCCCCCCCCCCCC PXDJXZJSCPSGGI-UHFFFAOYSA-N 0.000 description 2
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- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 2
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- 239000001788 mono and diglycerides of fatty acids Substances 0.000 description 2
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 2
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- 230000000144 pharmacologic effect Effects 0.000 description 2
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- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 2
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- GEHJYWRUCIMESM-UHFFFAOYSA-L sodium sulfite Chemical compound [Na+].[Na+].[O-]S([O-])=O GEHJYWRUCIMESM-UHFFFAOYSA-L 0.000 description 2
- 239000002904 solvent 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
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- DSEKYWAQQVUQTP-XEWMWGOFSA-N (2r,4r,4as,6as,6as,6br,8ar,12ar,14as,14bs)-2-hydroxy-4,4a,6a,6b,8a,11,11,14a-octamethyl-2,4,5,6,6a,7,8,9,10,12,12a,13,14,14b-tetradecahydro-1h-picen-3-one Chemical compound C([C@H]1[C@]2(C)CC[C@@]34C)C(C)(C)CC[C@]1(C)CC[C@]2(C)[C@H]4CC[C@@]1(C)[C@H]3C[C@@H](O)C(=O)[C@@H]1C DSEKYWAQQVUQTP-XEWMWGOFSA-N 0.000 description 1
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- ALSTYHKOOCGGFT-KTKRTIGZSA-N (9Z)-octadecen-1-ol Chemical compound CCCCCCCC\C=C/CCCCCCCCO ALSTYHKOOCGGFT-KTKRTIGZSA-N 0.000 description 1
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- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 1
- FFJCNSLCJOQHKM-CLFAGFIQSA-N (z)-1-[(z)-octadec-9-enoxy]octadec-9-ene Chemical compound CCCCCCCC\C=C/CCCCCCCCOCCCCCCCC\C=C/CCCCCCCC FFJCNSLCJOQHKM-CLFAGFIQSA-N 0.000 description 1
- ZORQXIQZAOLNGE-UHFFFAOYSA-N 1,1-difluorocyclohexane Chemical compound FC1(F)CCCCC1 ZORQXIQZAOLNGE-UHFFFAOYSA-N 0.000 description 1
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Landscapes
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
本発明は、ジフェンヒドラミン及び／又はその塩、並びにレチノール及び／又はその誘導体を含有し、鎮痒効果が向上した皮膚外用組成物に関する。 The present invention relates to an external composition for skin containing diphenhydramine and/or a salt thereof and retinol and/or a derivative thereof and having an improved antipruritic effect.
ジフェンヒドラミン塩酸塩等のジフェンヒドラミン類は、皮膚の痒みなどのアレルギー症状を引き起こすヒスタミンの作用を抑制し得ることが知られ、抗ヒスタミン剤として医薬品又は医薬部外品の皮膚外用剤に配合して用いられている。 Diphenhydramines such as diphenhydramine hydrochloride are known to be able to suppress the action of histamine that causes allergic symptoms such as itching of the skin, and are used as an antihistamine agent in a drug or a quasi drug external skin preparation. ..
例えば、特許文献１には、有効成分として、吉草酸酢酸プレドニゾロンと、ジフェンヒドラミン及びその塩類等の抗ヒスタミン剤とを含む、湿疹、皮膚炎、虫さされ、かゆみ、あせも、かぶれ及びじんましん等に対する治療効果を有する皮膚外用剤が開示されている。 For example, Patent Document 1 contains, as an active ingredient, prednisolone valerate acetate and an antihistamine such as diphenhydramine and its salts, and has a therapeutic effect on eczema, dermatitis, insect bites, itch, rash, rash and urticaria. An external preparation for skin having the same is disclosed.
また、特許文献２には、ジフェンヒドラミンのような鎮痒剤が、ヒアルロン酸又はその塩の存在下で、更にトコフェロール又はその誘導体と共存させることで、鎮痒作用が増強されることも開示されている。 Patent Document 2 also discloses that an antipruritic agent such as diphenhydramine is coexistent with tocopherol or a derivative thereof in the presence of hyaluronic acid or a salt thereof to enhance the antipruritic effect.
一方、レチノール（ビタミンＡ）類は、皮膚の上皮細胞を正常に保ち角化を防止する作用、抗酸化作用等を有することが知られ、外用組成物の有効成分として広く用いられている。特許文献３には、ビタミンＡ類とヘパリン類似物質とを含む外用組成物が、荒れた肌に塗布した場合、効果的に荒れた肌を改善することが記載されている。 On the other hand, retinol (vitamin A) is known to have an action of keeping epithelial cells of the skin normal and preventing keratinization, an antioxidant action and the like, and is widely used as an active ingredient of an external composition. Patent Document 3 describes that an external composition containing vitamin A and a heparin-like substance effectively improves rough skin when applied to rough skin.
痒みは耐え難い不快な感覚であり、不可避的に掻破行動を起こさせる。掻破行動は皮膚に物理的刺激を与えるため、痒みが強いほど、掻破行動による物理刺激が角質層を傷め、皮膚のバリア機能の低下、痒みに対する一層の敏感性の増強といった悪循環を招来しやすくなる。これまでのジフェンヒドラミンを含有する皮膚外用組成物は、未だに鎮痒効果が十分とはいえない。従って、痒みに対しては、不快感の低減のみならず、掻破行動による悪循環を抑止する観点からも、鎮痒効果をより一層高める製剤処方が求められる。 Itching is an unbearable and unpleasant sensation that inevitably causes scratching behavior. Since scratching behavior causes physical irritation to the skin, the stronger the itching, the more physical irritation caused by scratching behavior damages the stratum corneum, leading to a vicious cycle such as a decrease in the barrier function of the skin and a further increase in sensitivity to itching. .. The conventional external composition for skin containing diphenhydramine cannot be said to have a sufficient antipruritic effect. Therefore, for pruritus, a pharmaceutical formulation that further enhances the antipruritic effect is required from the viewpoint of not only reducing discomfort but also suppressing the vicious circle caused by scratching behavior.
本発明は、鎮痒効果がより一層高められた皮膚外用組成物を提供することを目的とする。 An object of the present invention is to provide a composition for external use for skin, which has an even higher antipruritic effect.
本発明者は、鋭意検討の結果、鎮痒成分であるジフェンヒドラミン類を、掻破行動の物理刺激を受ける皮膚の上皮細胞を正常に保ち角化を防止する作用等を有するレチノール類と共に含む皮膚外用組成物に、組織修復作用が知られているアラントイン類を配合したところ、飛躍的に鎮痒効果が向上するという驚くべき知見を見出した。本発明は、この知見に基づいて更に検討を重ねることにより完成したものである。 The present inventor, as a result of diligent studies, an external skin composition containing diphenhydramines, which are antipruritic components, together with retinol having an action to prevent keratinization by keeping the epithelial cells of the skin that are physically stimulated by scratching behavior normal. The present inventors have found a surprising finding that the addition of allantoins, which are known to have a tissue repair action, dramatically improves the antipruritic effect. The present invention has been completed by further studies based on this finding.
即ち、本発明は、下記に掲げる態様の発明を提供する。
項１． （Ａ）ジフェンヒドラミン及び／又はその塩、（Ｂ）レチノール及び／又はその誘導体、並びに（Ｃ）アラントイン及び／又はその誘導体を含有する皮膚外用組成物。
項２． 鎮痒用途で使用される、項１に記載の皮膚外用組成物。
項３． 前記（Ｃ）成分の含有量が０．００１〜１０重量％である、項１又は２に記載の皮膚外用組成物。
項４． 前記（Ａ）成分１重量部当たりの前記（Ｃ）成分の含有量が０．００１〜１０重量部である、項１〜３のいずれかに記載の皮膚外用組成物。
項５． （Ａ）ジフェンヒドラミン及び／又はその塩並びに（Ｂ）レチノール及び／又はその誘導体を含む皮膚外用組成物において、鎮痒効果を向上させる方法であって、
皮膚外用組成物に、前記（Ａ）成分及び前記（Ｂ）成分とともに（Ｃ）アラントイン及び／又はその誘導体を配合する、鎮痒効果向上方法。
That is, the present invention provides the inventions of the following modes.
Item 1. An external skin composition containing (A) diphenhydramine and/or a salt thereof, (B) retinol and/or a derivative thereof, and (C) allantoin and/or a derivative thereof.
Item 2. Item 2. The external composition for skin according to Item 1, which is used for antipruritic use.
Item 3. Item 3. The external composition for skin according to Item 1 or 2, wherein the content of the component (C) is 0.001 to 10% by weight.
Item 4. Item 4. The external composition for skin according to any one of Items 1 to 3, wherein the content of the component (C) is 0.001 to 10 parts by weight per 1 part by weight of the component (A).
Item 5. A method for improving the antipruritic effect in an external composition for skin containing (A) diphenhydramine and/or a salt thereof and (B) retinol and/or a derivative thereof, comprising:
A method for improving the antipruritic effect, which comprises adding (C) allantoin and/or a derivative thereof together with the above component (A) and the above component (B) to a composition for external skin application.
本発明の皮膚外用組成物は、ジフェンヒドラミン類及びレチノール類にアラントイン類を配合することによって、鎮痒効果を向上させることができる。 The antiseptic effect of the external skin composition of the present invention can be improved by incorporating allantoins in diphenhydramines and retinols.
１．皮膚外用組成物
本発明の皮膚外用組成物は、（Ａ）ジフェンヒドラミン及び／又はその塩（以下、「（Ａ）成分」とも記載する。）、（Ｂ）レチノール及び／又はその誘導体（以下、「（Ｂ）成分」とも記載する。）、及び（Ｃ）アラントイン及び／又はその誘導体（以下「（Ｃ）成分」とも記載する。）を含有することを特徴とする。以下、本発明の皮膚外用組成物について詳述する。
1. External composition for skin The external composition for skin of the present invention comprises (A) diphenhydramine and/or a salt thereof (hereinafter, also referred to as "(A) component"), (B) retinol and/or a derivative thereof (hereinafter, " (Also referred to as “component (B)”) and (C) allantoin and/or its derivative (hereinafter also referred to as “component (C)”). Hereinafter, the external composition for skin of the present invention will be described in detail.
（Ａ）ジフェンヒドラミン及び／又はその塩
本発明の皮膚外用組成物は、（Ａ）成分としてジフェンヒドラミン及び／又はその塩（以下において、ジフェンヒドラミン類とも記載する）を含有する。ジフェンヒドラミンは、抗ヒスタミン作用があることが知られている公知の薬剤である。（Ａ）成分は単独でも鎮痒作用を奏するが、本発明の皮膚外用組成物は、更に向上した鎮痒性を発揮することが可能である。
(A) Diphenhydramine and/or its salt The external composition for skin of the present invention contains diphenhydramine and/or its salt (hereinafter, also referred to as diphenhydramines) as the component (A). Diphenhydramine is a known drug known to have an antihistamine effect. The component (A) exerts an antipruritic effect alone, but the external composition for skin of the present invention can exhibit further improved antipruritic properties.
ジフェンヒドラミンの塩としては、薬学的に許容されるものである限り特に制限されないが、具体的には、塩酸塩、クエン酸塩、コハク酸塩、酒石酸塩、フマル酸塩、マレイン酸塩、サリチル酸塩、ジフェニルジスルホン酸塩、タンニン酸塩、ラウリル硫酸塩、硫酸塩等の酸付加塩が挙げられる。これらの塩は、１種単独で使用してもよく、また２種以上を組み合わせて使用してもよい。 The salt of diphenhydramine is not particularly limited as long as it is pharmaceutically acceptable, but specifically, hydrochloride, citrate, succinate, tartrate, fumarate, maleate, salicylate. Acid addition salts such as diphenyl disulfonate, tannate, lauryl sulfate, and sulfate. These salts may be used alone or in combination of two or more.
本発明の皮膚外用組成物において、（Ａ）成分として、ジフェンヒドラミン及びその塩の中から１種を選択して使用してもよく、また２種以上を組み合わせて使用してもよい。 In the external composition for skin of the present invention, as the component (A), one type may be selected from diphenhydramine and salts thereof, or two or more types may be used in combination.
本発明の皮膚外用組成物における（Ａ）成分の含有量については、付与すべき薬効等に応じて適宜設定すればよいが、例えば、総量で０．０１〜１０重量％、好ましくは０．１〜５重量％、より好ましくは０．５〜３重量％が挙げられる。 The content of the component (A) in the external composition for skin of the present invention may be appropriately set according to the drug effect to be imparted, and for example, the total amount is 0.01 to 10% by weight, preferably 0.1. -5% by weight, more preferably 0.5-3% by weight.
（Ｂ）レチノール及び／又はその誘導体
本発明の皮膚外用組成物は、（Ｂ）成分としてレチノール及び／又はその誘導体を含有する。レチノールは、ビタミンＡの１種であり、ビタミンＡアルコールとも称されることがある成分である。
(B) Retinol and/or its derivative The external composition for skin of the present invention contains retinol and/or its derivative as the component (B). Retinol is a type of vitamin A and is a component which is sometimes referred to as vitamin A alcohol.
レチノールの誘導体とは、レチノールと同じ骨格を有し、レチノールに置換基を付加することによって得られる成分である。レチノール誘導体の種類については、薬学的に許容されることを限度として、特に制限されないが、例えば、レチノールと脂肪酸とのエステル、レチノールと酢酸とのエステル（即ち、レチノール酢酸エステル）、レチノールの酸化物、及び当該酸化物のエステル等が挙げられる。 A retinol derivative has the same skeleton as retinol and is a component obtained by adding a substituent to retinol. The type of retinol derivative is not particularly limited as long as it is pharmaceutically acceptable. For example, an ester of retinol and a fatty acid, an ester of retinol and acetic acid (that is, retinol acetate ester), and an oxide of retinol. , And esters of the oxide.
レチノールと脂肪酸とのエステルとしては、具体的には、レチノールと、炭素数１〜３０、好ましくは２〜１８の脂肪酸とのエステルが挙げられる。レチノールと脂肪酸とのエステルとして、より具体的には、レチノール酢酸エステル、レチノールプロピオン酸エステル、レチノール酪酸エステル、レチノールオクチル酸エステル、レチノールラウリル酸エステル、レチノールパルミチン酸エステル、レチノールステアリン酸エステル、レチノールミリスチン酸エステル、レチノールオレイン酸エステル、レチノールリノレン酸エステル、レチノールリノール酸エステル等が挙げられる。これらのレチノールと脂肪酸とのエステルは、１種単独で使用してもよく、２種以上を組み合わせて使用してもよい。 Specific examples of the ester of retinol and fatty acid include esters of retinol and fatty acid having 1 to 30 carbon atoms, preferably 2 to 18 carbon atoms. As the ester of retinol and a fatty acid, more specifically, retinol acetate, retinol propionate, retinol butyrate, retinol octylate, retinol lauric acid ester, retinol palmitate, retinol stearic acid ester, retinol myristic acid. Examples thereof include esters, retinol oleate, retinol linolenate, retinol linoleate and the like. These esters of retinol and fatty acids may be used alone or in combination of two or more.
レチノールの酸化物としては、具体的には、レチノイン酸（「トレチノイン」と称することもある）、レチナール等が挙げられる。これらのレチノールの酸化物は、１種単独で使用してもよく、２種以上を組み合わせて使用してもよい。 Specific examples of the retinol oxide include retinoic acid (sometimes referred to as “tretinoin”) and retinal. These retinol oxides may be used alone or in combination of two or more.
レチノールの酸化物のエステルとしては、具体的には、レチノイン酸メチル、レチノイン酸エチル、レチノイン酸レチノール、レチノイン酸トコフェロール（トコフェロールは、α、β、γ、又はδのいずれであってもよい）等が挙げられる。これらのレチノールの酸化物のエステルは、１種単独で使用してもよく、２種以上を組み合わせて使用してもよい。 Specific examples of the retinol oxide ester include methyl retinoic acid, ethyl retinoic acid, retinol retinoic acid, and tocopherol retinoic acid (tocopherol may be any of α, β, γ, or δ) and the like. Are listed. These retinol oxide esters may be used alone or in combination of two or more.
これらの（Ｂ）成分は、その原料、製造方法、精製方法等は特に制限されず、動物等から自ら単離及び精製したものを用いてもよく、或いは市販品を用いてもよい。また、本発明の皮膚外用組成物において、（Ｂ）成分レチノール及びレチノールの誘導体の中から、１種を選択して使用してもよく、２種以上を組み合わせて使用してもよい。 These components (B) are not particularly limited in their raw materials, production methods, purification methods, etc., and those isolated and purified by themselves from animals or the like may be used, or commercially available products may be used. Further, in the external composition for skin of the present invention, one kind may be selected from the component (B) retinol and a derivative of retinol, or two or more kinds may be used in combination.
また、本発明において、レチノール類は、植物油等の油中に溶解させた状態で使用してもよい。このようにレチノール類を油中に溶解させたものは、「ビタミンＡ油」として知られている。ビタミンＡ油は、例えば日本薬局方に記載の方法に従って製造することができる。ビタミンＡ油としては、通常、レチノール及び／又はその誘導体の含有量が１０万〜２００万Ｉ.Ｕ.／ｇ、好ましくは５０万〜１７０万Ｉ.Ｕ.／ｇ、更に好ましくは５０万〜１００万Ｉ.Ｕ.／ｇのものを使用できる。なお、本明細書において、レチノール及び／又はその誘導体の含有量の単位「Ｉ.Ｕ.」は、国際単位を示す。 Further, in the present invention, the retinols may be used in a state of being dissolved in oil such as vegetable oil. Such retinols dissolved in oil are known as "vitamin A oils". Vitamin A oil can be produced, for example, according to the method described in the Japanese Pharmacopoeia. As vitamin A oil, the content of retinol and/or its derivative is usually 100,000 to 2,000,000 IU/g, preferably 500,000 to 1,700,000 IU/g, and more preferably 500,000 to. One million IU/g can be used. In addition, in this specification, the unit "I.U." of the content of retinol and/or its derivative shows an international unit.
これらの（Ｂ）成分の中でも、より一層向上した鎮痒性を得る観点から、好ましくはレチノールの誘導体、更に好ましくはレチノールと脂肪酸とのエステル、特に好ましくはレチノールパルミチン酸エステルが挙げられる。 Among these components (B), from the viewpoint of obtaining further improved antipruritic properties, a retinol derivative is preferable, an ester of retinol and a fatty acid is more preferable, and a retinol palmitate ester is particularly preferable.
本発明の皮膚外用組成物において、（Ｂ）成分の含有量については、特に制限されないが、例えば、本発明の皮膚外用組成物１００ｇ当たり、（Ｂ）成分が、０．１万〜１０００万Ｉ．Ｕ．、好ましくは１万〜５００万Ｉ．Ｕ．、より好ましくは１０万〜３００万Ｉ．Ｕ．、更に好ましくは１０万〜１５０万Ｉ．Ｕ．、特に好ましくは２５万〜１００万Ｉ．Ｕ．が挙げられる。 In the external composition for skin of the present invention, the content of the component (B) is not particularly limited, but, for example, per 100 g of the external composition for skin of the present invention, the amount of the component (B) is from 10 to 10 million I. ． U. , Preferably 10,000 to 5 million I.D. U. , And more preferably 100,000 to 3,000,000 I.D. U. , And more preferably 100,000 to 1.5 million I.D. U. , Particularly preferably 250,000 to 1,000,000 I.D. U. Are listed.
また、（Ｂ）成分としてビタミンＡ油を使用する場合、本発明の皮膚外用組成物におけるビタミンＡ油の含有量については、ビタミンＡ油中のレチノール類の含有量に応じて、本発明の皮膚外用組成物中でレチノール類が前述する含有量を充足するように設定すればよい。具体的には、１００万Ｉ．Ｕ．／ｇのレチノール類を含有するビタミンＡ油を用いる場合であれば、本発明の皮膚外用組成物におけるビタミンＡ油の含有量については、０．００１〜１０重量％、好ましくは０．０１〜５重量％、より好ましくは０．１〜２重量％に設定すればよい。 When vitamin A oil is used as the component (B), the content of the vitamin A oil in the external composition for skin of the present invention depends on the content of the retinols in the vitamin A oil, and the skin of the present invention. It may be set so that the retinol compound in the external composition satisfies the above-mentioned content. Specifically, 1 million I.D. U. When using a vitamin A oil containing 1/g of retinols, the content of the vitamin A oil in the external composition for skin of the present invention is 0.001 to 10% by weight, preferably 0.01 to 5%. The weight ratio may be set to more preferably 0.1 to 2% by weight.
本発明の皮膚外用組成物において、（Ａ）成分と（Ｂ）成分の比率については特に制限されず、前述する（Ａ）成分及び（Ｂ）成分の各含有量に応じて決定されるが、より一層向上した鎮痒性を得る観点から、（Ａ）成分１重量部当たり、（Ｂ）成分が総量で０．１万〜１０００万Ｉ．Ｕ．、好ましくは１万〜５００万Ｉ．Ｕ．、より好ましくは１０万〜３００万Ｉ．Ｕ．、更に好ましくは１０万〜１５０万Ｉ．Ｕ．、一層好ましくは２５万〜１００万Ｉ．Ｕ．、特に好ましくは４０〜６０万Ｉ．Ｕ．が挙げられる。 In the external composition for skin of the present invention, the ratio of the component (A) and the component (B) is not particularly limited and is determined according to the content of each of the components (A) and (B) described above. From the viewpoint of obtaining further improved antipruritic properties, the total amount of the component (B) is 0.1 million to 10 million I.D. per 1 part by weight of the component (A). U. , Preferably 10,000 to 5 million I.D. U. , And more preferably 100,000 to 3,000,000 I.D. U. , And more preferably 100,000 to 1.5 million I.D. U. And more preferably 250,000 to 1,000,000 I.D. U. , Particularly preferably 400,000 to 600,000 I.D. U. Are listed.
（Ｃ）アラントイン及び／又はその誘導体
本発明の皮膚外用組成物は、（Ｃ）成分としてアラントイン及び／又はその誘導体（以下において、アラントイン類とも記載する）を含んでいてもよい。アラントイン類は組織修復作用で知られているが、本発明では、レチノール類の存在下でジフェンヒドラミン類と組み合わせられることで、ジフェンヒドラミン類による鎮痒作用を飛躍的に上回る、高い鎮痒効果を発現することができる。
(C) Allantoin and/or its derivative The external composition for skin of the present invention may contain allantoin and/or its derivative (hereinafter, also referred to as allantoins) as the component (C). Allantoins are known for their tissue repair action, but in the present invention, when combined with diphenhydramines in the presence of retinols, the antipruritic action by diphenhydramines is dramatically exceeded, and a high antipruritic effect can be expressed. it can.
アラントインは、５−ウレイドヒダントインとも称される化合物であり、抗炎症作用や組織修復作用等を有することが知られている公知の薬剤である。 Allantoin is a compound also called 5-ureidohydantoin, which is a known drug known to have an anti-inflammatory action, a tissue repair action, and the like.
アラントインの誘導体としては、薬学的に許容できることを限度として特に制限されないが、具体的には、アラントインクロルヒドロキシアルミニウム、アラントインヒドロキシアルミニウム等が挙げられる。これらのアラントインの誘導体は、１種単独で使用してもよく、また２種以上を組み合わせて使用してもよい。 The allantoin derivative is not particularly limited as long as it is pharmaceutically acceptable, and specific examples thereof include allantoin chlorhydroxyaluminum and allantoin hydroxyaluminum. These allantoin derivatives may be used alone or in combination of two or more.
本発明の皮膚外用組成物においては、アラントイン及びその誘導体の中から１種を単独で使用してもよく、また２種以上を組み合わせて使用してもよい。 In the external composition for skin of the present invention, one kind of allantoin and its derivative may be used alone, or two or more kinds may be used in combination.
これらの（Ｃ）成分の中でも、より一層向上した鎮痒性を得る観点から、好ましくはアラントインが挙げられる。 Among these (C) components, allantoin is preferable from the viewpoint of obtaining further improved antipruritic properties.
本発明の皮膚外用組成物において、（Ｃ）成分の含有量については、特に制限されないが、例えば、０．００１〜１０重量％が挙げられる。より一層向上した鎮痒性を得る観点から、（Ｃ）成分の含有量としては、好ましくは０．０１〜５重量％、更に好ましくは０．１〜２重量％が挙げられる。 In the external composition for skin of the present invention, the content of the component (C) is not particularly limited, and examples thereof include 0.001 to 10% by weight. From the viewpoint of obtaining further improved antipruritic properties, the content of the component (C) is preferably 0.01 to 5% by weight, more preferably 0.1 to 2% by weight.
本発明の皮膚外用組成物において、（Ａ）成分と（Ｃ）成分の比率については特に制限されず、前述する（Ａ）成分及び（Ｃ）成分の各含有量に応じて決定されるが、より一層向上した鎮痒性を得る観点から、（Ａ）成分１重量部当たり、（Ｃ）成分が総量で０．００１〜１０重量部、好ましくは０．０１〜５重量部、更に好ましくは０．１〜２重量部、特に好ましくは０．１〜０．５重量部が挙げられる。 In the external composition for skin of the present invention, the ratio of the component (A) and the component (C) is not particularly limited, and is determined according to the content of each of the above-mentioned (A) component and (C) component. From the viewpoint of obtaining further improved antipruritic properties, the total amount of the component (C) is 0.001 to 10 parts by weight, preferably 0.01 to 5 parts by weight, and more preferably 0. 1 to 2 parts by weight, particularly preferably 0.1 to 0.5 parts by weight.
その他の成分
本発明の皮膚外用組成物は、前述する成分の他に、必要に応じて、他の薬理成分を含んでもよい。このような薬理成分としては、例えば、抗ヒスタミン剤（マレイン酸クロルフェニラミン等）、局所麻酔剤（リドカイン、ジブカイン、プロカイン、テトラカイン、ブピバカイン、メピバカイン、クロロプロカイン、プロパラカイン、メプリルカイン又はこれらの塩、安息香酸アルキルエステル（例えばアミノ安息香酸エチル、塩酸パラブチルアミノ安息香酸ジエチルアミノエチル）、オルソカイン、オキセサゼイン、オキシポリエントキシデカン、ロートエキス、ペルカミンパーゼ、テシットデシチン等）、抗炎症剤（ウフェナマート、グリチルレチン酸、グリチルレチン酸塩、サリチル酸、サリチル酸グリコール、サリチル酸メチル、インドメタシン、フェルビナク、ジクロフェナクナトリウム、ロキソプロフェンナトリウム等）、殺菌剤（酸化亜鉛、塩化ベンザルコニウム、塩化デカリニウム、塩化ベンゼトニウム、塩化セチルピリジニウム、イソプロピルメチルフェノール、塩酸クロルヘキシジン、グルコン酸クロルヘキシジン、アンモニア水、スルファジアジン、乳酸、フェノール等）、鎮痒剤（クロタミトン、チアントール等）、皮膚保護剤（コロジオン、ヒマシ油等）、血行促進成分（ノニル酸ワニリルアミド、ニコチン酸ベンジルエステル、カプサイシン、トウガラシエキス等）、清涼化剤（メントール、カンフル等）、ビタミン類（ビタミンＢ，Ｃ，Ｄ，Ｅ等）、ムコ多糖類（コンドロイチン硫酸ナトリウム、ヒアルロン酸等）等が挙げられる。
Other Ingredients The external composition for skin of the present invention may contain other pharmacological ingredients, if necessary, in addition to the above-mentioned ingredients. Such pharmacological components include, for example, antihistamines (chlorpheniramine maleate, etc.), local anesthetics (lidocaine, dibucaine, procaine, tetracaine, bupivacaine, mepivacaine, chloroprocaine, proparacaine, meprilcaine or salts thereof, benzoic acid. Alkyl ester (eg, ethyl aminobenzoate, diethylaminoethyl parabutylaminobenzoate hydrochloride), orthocaine, oxesazein, oxypolyentoxydecane, funnel extract, percaminpase, tesit decithin, etc., anti-inflammatory agent (ufenamate, glycyrrhetinic acid, glycyrrhetinate, Salicylic acid, glycol salicylate, methyl salicylate, indomethacin, felbinac, diclofenac sodium, loxoprofen sodium, etc., fungicides (zinc oxide, benzalkonium chloride, decalinium chloride, benzethonium chloride, cetylpyridinium chloride, isopropylmethylphenol, chlorhexidine hydrochloride, gluconic acid) Chlorhexidine, ammonia water, sulfadiazine, lactic acid, phenol, etc., antipruritic agents (crotamiton, thiantol, etc.), skin protectants (colodion, castor oil, etc.), blood circulation promoting components (nonyl acid vanillyl amide, nicotinic acid benzyl ester, capsaicin, capsicum extract) Etc.), a cooling agent (menthol, camphor, etc.), vitamins (vitamins B, C, D, E, etc.), mucopolysaccharides (sodium chondroitin sulfate, hyaluronic acid, etc.) and the like.
前述する成分の他に、必要に応じて、皮膚外用剤等に通常使用される他の基剤や添加剤を含んでもよい。このような基材や添加剤としては、薬学的に許容されることを限度として特に制限されないが、例えば、水、低級アルコール（例えば、イソプロパノール）、多価アルコール（グリセリン、プロピレングリコール、ジプロピレングリコール、１，３−ブチレングリコール等）等の水性基剤；油類（オリーブ油、サフラワー油、大豆油、つばき油、とうもろこし油、なたね油、ひまわり油、綿実油、落花生油、ラード、スクワラン、魚油等）、鉱物油（流動パラフィン、パラフィン、ゲル化炭化水素、ワセリン等）、ワックス類・ロウ類（ミツロウ、カルナウバロウ、キャンデリラロウ、セレシン、ライスワックス、マイクロクリスタリンワックス等）、エステル油（ミリスチン酸イソプロピル、アジピン酸イソプロピル、セバシン酸ジエチル、セバシン酸イソプロピル、パルミチン酸イソプロピル、パルミチン酸セチル、オレイン酸エチル等）、脂肪酸アルキルエステル、脂肪酸（ステアリン酸、オレイン酸、パルミチン酸、ベヘン酸、リノール酸、ラノリン等）、脂肪酸エステル（パルミチン酸セチル、パルミチン酸イソプロピル、リノール酸エチル等）、高級アルコール（ステアリルアルコール、セタノール、ベヘニルアルコール、ミリスチルアルコール、オレイルアルコール、ヘキサデシルアルコール、ラノリンアルコール等）、コレステロール、トリ２−エチルヘキサン酸グリセリル、２−エチルヘキサン酸セチル、シリコーンオイル（ジメチルポリシロキサン、環状シリコーン等）等の油性基剤；ＰＯＥ（１０〜５０モル）フィトステロールエーテル、ＰＯＥ（１０〜５０モル）ジヒドロコレステロールエーテル、ＰＯＥ（１０〜５０モル）２−オクチルドデシルエーテル、ＰＯＥ（１０〜５０モル）デシルテトラデシルエーテル、ＰＯＥ（１０〜５０モル）オレイルエーテル、ＰＯＥ（２〜５０モル）セチルエーテル、ＰＯＥ（５〜５０モル）ベヘニルエーテル、ＰＯＥ（５〜３０モル）ポリオキシプロピレン（５〜３０モル）２−デシルテトラデシルエーテル、ＰＯＥ（１０〜５０モル）ポリオキシプロピレン（２〜３０モル）セチルエーテルなどのポリオキシエチレンアルキルエーテル、これらのリン酸・リン酸塩（ＰＯＥセチルエーテルリン酸ナトリウムなど）、ＰＯＥ（２０〜６０モル）ソルビタンモノオレート、ＰＯＥ（１０〜６０モル）ソルビタンモノイソステアレート、ＰＯＥ（１０〜８０モル）グリセリルモノイソステアレート、ＰＯＥ（１０〜３０モル）グリセリルモノステアレート、ＰＯＥ（２０〜１００モル）・ポリオキシプロピレン変性シリコーン、ＰＯＥ・アルキル変性シリコーン、モノラウリン酸ポリエチレングリコール、モノパルミチン酸ポリエチレングリコール、モノステアリン酸ポリエチレングリコール、ジラウリン酸ポリエチレングリコール、ジパルミチン酸ポリエチレングリコール、ジステアリン酸ポリエチレングリコール、ジオレイン酸ポリエチレングリコール、ジリシノレイン酸ポリエチレングリコール、ポリオキシエチレン硬化ヒマシ油（５〜１００）、ポリソルベート（２０〜８５）、グリセリン脂肪酸エステル（モノステアリン酸グリセリン等）、水素添加大豆リン脂質、水素添加ラノリンアルコール等の界面活性剤；清涼化剤（メントール、カンフル、ボルネオール、ハッカ水、ハッカ油等）、防腐剤（メチルパラベン、プロピルパラベン、安息香酸、安息香酸ナトリウム、ソルビン酸等）、着香剤（シトラール、１，８−シオネール、シトロネラール、ファルネソール等）、着色剤（タール色素（褐色２０１号、青色２０１号、黄色４号、黄色４０３号等）、カカオ色素、クロロフィル、酸化アルミニウム等）、粘稠剤（カルボキシビニルポリマー、ヒプロメロース、ポリビニルピロリドン、アルギン酸ナトリウム、エチルセルロース、ヒドロキシエチルセルロース、カルボキシメチルセルロースナトリウム、キサンタンガム、カラギーナン等）、ｐＨ調整剤（リン酸、塩酸、クエン酸、クエン酸ナトリウム、コハク酸、酒石酸、水酸化ナトリウム、水酸化カリウム、トリエタノールアミン、トリイソプロパノールアミン等）、湿潤剤（ｄｌ−ピロリドンカルボン酸ナトリウム液、Ｄ−ソルビトール液、マクロゴール等）、安定化剤（ジブチルヒドロキシトルエン、ブチルヒドロキシアニソール、エデト酸ナトリウム、メタリン酸ナトリウム、Ｌ−アルギニン、Ｌ−アスパラギン酸、ＤＬ−アラニン、グリシン、エリソルビン酸ナトリウム、没食子酸プロピル、亜硫酸ナトリウム、二酸化硫黄、クロロゲン酸、カテキン、ローズマリー抽出物等）、酸化防止剤、紫外線吸収剤、キレート剤、粘着剤、緩衝剤、溶解補助剤、可溶化剤、保存剤等の添加剤が挙げられる。 In addition to the above-mentioned components, other bases and additives usually used for external preparations for skin and the like may be contained, if necessary. Such base materials and additives are not particularly limited as long as they are pharmaceutically acceptable. For example, water, lower alcohol (eg, isopropanol), polyhydric alcohol (glycerin, propylene glycol, dipropylene glycol) , 1,3-butylene glycol, etc.); oils (olive oil, safflower oil, soybean oil, camellia oil, corn oil, rapeseed oil, sunflower oil, cottonseed oil, peanut oil, lard, squalane, fish oil, etc.) , Mineral oil (liquid paraffin, paraffin, gelled hydrocarbon, vaseline, etc.), waxes and waxes (beeswax, carnauba wax, candelilla wax, ceresin, rice wax, microcrystalline wax, etc.), ester oil (isopropyl myristate, Isopropyl adipate, diethyl sebacate, isopropyl sebacate, isopropyl palmitate, cetyl palmitate, ethyl oleate, etc.), fatty acid alkyl esters, fatty acids (stearic acid, oleic acid, palmitic acid, behenic acid, linoleic acid, lanolin, etc.) , Fatty acid esters (cetyl palmitate, isopropyl palmitate, ethyl linoleate, etc.), higher alcohols (stearyl alcohol, cetanol, behenyl alcohol, myristyl alcohol, oleyl alcohol, hexadecyl alcohol, lanolin alcohol, etc.), cholesterol, tri-2-ethylhexane Oily bases such as glyceryl acid salt, cetyl 2-ethylhexanoate, silicone oil (dimethylpolysiloxane, cyclic silicone, etc.); POE (10 to 50 mol) phytosterol ether, POE (10 to 50 mol) dihydrocholesterol ether, POE( 10 to 50 mol) 2-octyldodecyl ether, POE (10 to 50 mol) decyl tetradecyl ether, POE (10 to 50 mol) oleyl ether, POE (2 to 50 mol) cetyl ether, POE (5 to 50 mol) Polyoxyethylene alkyl such as behenyl ether, POE (5 to 30 mol) polyoxypropylene (5 to 30 mol) 2-decyl tetradecyl ether, POE (10 to 50 mol) polyoxypropylene (2 to 30 mol) cetyl ether Ether, phosphoric acid/phosphates thereof (POE cetyl ether sodium phosphate, etc.), POE (20-60 mol) sorbitan monooleate, POE (10-60 mol) sorbitan monoisostearate, POE (10-80 mol) ) Glyceryl monoisostearate, POE (10 to 30 mol) glyceryl monostearate, POE (20 to 100 mol) polyoxypropylene modified silicone, POE/alkyl modified silicone, polyethylene glycol monolaurate, polyethylene glycol monopalmitate, Polyethylene glycol monostearate, polyethylene glycol dilaurate, polyethylene glycol dipalmitate, polyethylene glycol distearate, polyethylene glycol dioleate, polyethylene glycol diricinoleate, polyoxyethylene hydrogenated castor oil (5-100), polysorbate (20-85) ), glycerin fatty acid ester (glyceryl monostearate, etc.), hydrogenated soybean phospholipid, hydrogenated lanolin alcohol, etc.; refreshing agents (menthol, camphor, borneol, peppermint water, peppermint oil, etc.), preservatives ( Methylparaben, propylparaben, benzoic acid, sodium benzoate, sorbic acid, etc., flavoring agents (citral, 1,8-cioneal, citronellal, farnesol, etc.), colorants (tar dyes (brown 201, blue 201, yellow) No. 4, yellow No. 403, etc.), cocoa dye, chlorophyll, aluminum oxide, etc.), a thickener (carboxyvinyl polymer, hypromellose, polyvinylpyrrolidone, sodium alginate, ethyl cellulose, hydroxyethyl cellulose, sodium carboxymethyl cellulose, xanthan gum, carrageenan, etc.) pH adjuster (phosphoric acid, hydrochloric acid, citric acid, sodium citrate, succinic acid, tartaric acid, sodium hydroxide, potassium hydroxide, triethanolamine, triisopropanolamine, etc.), wetting agent (dl-pyrrolidonecarboxylate sodium solution, D-sorbitol solution, macrogol, etc., stabilizer (dibutylhydroxytoluene, butylhydroxyanisole, sodium edetate, sodium metaphosphate, L-arginine, L-aspartic acid, DL-alanine, glycine, sodium erythorbate, gallic acid Acid propyl, sodium sulfite, sulfur dioxide, chlorogenic acid, catechin, rosemary extract, etc.), antioxidants, UV absorbers, chelating agents, adhesives, buffers, solubilizers, solubilizers, preservatives, etc. Examples include additives.
性状・製剤形態等
本発明の皮膚外用組成物の性状としては特に限定されず、水性液状組成物、水性ゲル状組成物、油性ゲル状組成物、油性組成物、乳化組成物等が挙げられる。これらの性状の中でも、好ましくは乳化組成物が挙げられる。
Properties, Formulation Form, etc. The properties of the external composition for skin of the present invention are not particularly limited, and examples thereof include an aqueous liquid composition, an aqueous gel composition, an oily gel composition, an oily composition, and an emulsion composition. Among these properties, the emulsified composition is preferable.
本発明の皮膚外用組成物の製剤形態については特に制限されず、例えば、ローション剤、乳液剤、軟膏剤、クリーム剤等が挙げられる。これらの製剤形態の中でも、好ましくはクリーム剤が挙げられる。 The formulation form of the external composition for skin of the present invention is not particularly limited, and examples thereof include lotions, emulsions, ointments and creams. Among these formulation forms, creams are preferred.
本発明の皮膚外用組成物としては、具体的には、医薬品、医薬部外品、化粧品等が挙げられる。これらの製剤形態の中でも、好ましくは医薬品、医薬部外品が挙げられる。 Specific examples of the external composition for skin of the present invention include pharmaceuticals, quasi drugs, cosmetics and the like. Among these dosage forms, preferred are pharmaceuticals and quasi drugs.
使用方法
本発明の皮膚外用組成物は、鎮痒用途に使用することができ、痒みを感じる皮膚の部位又は掻痒を防止すべき皮膚の部位に塗布することにより使用される。本発明の皮膚外用組成物が適用される皮膚の部位における皮膚症状としては、痒みが惹起される症状であれば特に限定されないが、毛穴炎症、赤み、湿疹、かぶれに対して好ましく適用される。
Method of Use The external composition for skin of the present invention can be used for antipruritic use, and it is used by applying it to the part of the skin where itching is felt or the part of the skin where itching is to be prevented. The skin condition at the site of the skin to which the external composition for skin of the present invention is applied is not particularly limited as long as it causes itch, but it is preferably applied to pore inflammation, redness, eczema, and rash.
本発明の皮膚外用組成物は、皮膚部位１００ｃｍ2当たり、例えば０．１〜０．５ｇを、１日に１〜２回塗布することで適用することができる。 The external composition for skin of the present invention can be applied by applying, for example, 0.1 to 0.5 g per 100 cm 2 of the skin site once or twice a day.
２．鎮痒効果向上方法
上述するように、アラントイン類は、ジフェンヒドラミン類及びレチノール類を含む皮膚外用組成物の鎮痒効果を飛躍的に向上させる。従って、本発明は、更に、ジフェンヒドラミン類及びレチノール類を含む皮膚外用組成物の鎮痒効果を向上させる方法を提供する。具体的には、本発明の鎮痒効果向上方法は、皮膚外用組成物に、（Ａ）ジフェンヒドラミン及び／又はその塩、並びに（Ｂ）レチノール及び／又はその誘導体とともに（Ｃ）アラントイン及び／又はその誘導体を配合することを特徴とする。本発明の鎮痒効果向上方法において、使用される成分の種類や配合量、皮膚外用組成物の性状・製剤形態、使用方法等については、前記「１．皮膚外用組成物」の欄に記載の通りである。
2. Method for Improving Antipruritic Effect As described above, allantoins dramatically improve the antipruritic effect of the external composition for skin containing diphenhydramines and retinols. Therefore, the present invention further provides a method for improving the antipruritic effect of the external composition for skin containing diphenhydramines and retinols. Specifically, the antipruritic effect improving method of the present invention comprises: (A) diphenhydramine and/or a salt thereof; Is blended. In the method for improving the antipruritic effect of the present invention, the types and amounts of the components used, the properties and formulation forms of the external composition for skin, the method of use, etc. are as described in the section of "1. External composition for skin". Is.
以下に実施例を示して本発明をより具体的に説明するが、本発明はこれらに限定されるものではない。 Hereinafter, the present invention will be described more specifically with reference to Examples, but the present invention is not limited thereto.
試験例１
表１に示す組成の皮膚外用組成物を調製した。具体的には、表１に示す各成分を秤量及び混合し、６５〜７５℃で均一溶解状態とした。その後、放置して室温まで冷却し、皮膚外用組成物を得た。
Test example 1
The external composition for skin having the composition shown in Table 1 was prepared. Specifically, the components shown in Table 1 were weighed and mixed, and a homogeneous dissolution state was obtained at 65 to 75°C. Then, it was left to stand and cooled to room temperature to obtain a composition for external use on the skin.
得られた皮膚外用組成物を、掻痒惹起物質を投与して作製した掻痒モデルマウスに適用し、掻痒試験を行った。掻痒試験では、マウスの掻き動作の回数をカウントし、鎮痒指数を導出することで鎮痒効果を評価した。掻痒モデルマウス、適用方法、掻き動作回数のカウント方法、及び鎮痒指数の導出方法の詳細は以下の通りである。 The obtained external composition for skin was applied to a pruritus model mouse prepared by administering a pruritus-inducing substance, and a pruritus test was conducted. In the pruritus test, the antipruritic effect was evaluated by counting the number of scratching movements of the mouse and deriving the pruritus index. The details of the pruritus model mouse, the application method, the method of counting the number of scratching movements, and the method of deriving the antipruritic index are as follows.
・掻痒モデルマウス
使用動物
種 マウス
系統 Slc：ＩＣＲ
週齢 ５週齢
入手元 日本エスエルシー（株）
掻痒惹起物質の投与
掻痒惹起物質 Ｃｏｍｐｏｕｎｄ ４８／８０
入手元 Ｓｉｇｍａ−Ａｌｄｒｉｃｈ Ｃｏ．
投与経路 皮内投与
投与用量 ５０μｇ／ｓｉｔｅ
投与方法 ガラス製注射筒（（株）トップ）及び３０Ｇニードル（（株）デントロニクス）を用いて、剃毛し皮膚外用組成物を塗布した直後の背部に投与した。
投与回数 １回
・Pruritus model mouse Animal species Mouse strain Slc:ICR
5 weeks old Obtained from Japan SLC, Inc.
Administration of Pruritus-Inducing Substance Pruritus-Inducing Substance Compound 48/80
Obtained from Sigma-Aldrich Co.
Route of administration Intradermal administration Dose 50 μg/site
Administration method Using a glass syringe (Top Co., Ltd.) and a 30G needle (Dentronics Co., Ltd.), administration was performed on the back immediately after shaving and application of the external composition for skin.
Number of administrations 1 time
・皮膚外用組成物の適用
投与経路 塗布
投与用量 １００ｍｇ／マウス
投与方法 掻痒惹起物質投与直前に、ゴム手袋をした指で、剃毛した背部全体に塗り広げた。
投与回数 １回
-Application of external composition for skin Administration route Application Administration dose 100 mg/mouse Administration method Immediately before administration of the pruritus-inducing substance, it was spread over the entire shaved back with fingers wearing rubber gloves.
Number of administrations 1 time
・掻き動作のカウント
Windows Media Player（バージョン：12.0.7601.23517）によりビデオ映像中のマウスの行動を観察し、マウス後肢によるマウスの背部への掻き動作を、掻痒惹起物質投与直後〜掻痒惹起物質投与後１５分経過時の間で、何回行ったかをカウントした。掻き動作の回数は、マウスが引っ掻くために後肢を上げ、引っ掻き行動を行って再び後肢を下す一連の動作を完了した時点で１回とした。カウントには連式数取器（DS-404：高野計器（株））を使用し、映像が途中で切れていないことを映像中のタイマー表示で確認した。
・Count of scraping motion
The behavior of the mouse in the video image was observed with Windows Media Player (version: 12.0.7601.23517), and the scratching action on the back of the mouse by the mouse hind limb was observed between immediately after the administration of the pruritus-inducing substance and 15 minutes after the administration of the pruritus-inducing substance. , I counted how many times I went. The number of scratching movements was once when the series of movements of raising the hind limb for scratching the mouse, performing the scratching behavior, and lowering the hind limb again was completed. A continuous counting device (DS-404: Takano Keiki Co., Ltd.) was used for counting, and it was confirmed by the timer display in the image that the image was not cut in the middle.
・鎮痒指数の導出
カウントした掻き動作回数と、参考例１（コントロール）における掻き動作回数と、比較例１における掻き動作回数とから、以下に基づいて鎮痒指数を導出した。鎮痒指数が高いほど、鎮痒効果が高いことを示す。結果を表１に示す。
Derivation of antipruritic index The antipruritic index was derived based on the following from the counted number of scratching actions, the number of scratching actions in Reference Example 1 (control), and the number of scratching actions in Comparative Example 1. The higher the antipruritic index, the higher the antipruritic effect. The results are shown in Table 1.
ジフェンヒドラミンをビタミンＡ油と共に含む皮膚外用組成物（比較例１）は、参考例１（コントロール）に比べて鎮痒効果を奏した。また、アラントインを含む皮膚外用組成物（比較例２）も（コントロール）に比べて鎮痒効果を奏した。しかしながら、それらの鎮痒効果は不十分であった。表１から明らかなように、ジフェンヒドラミン及びビタミンＡ油に更にアラントインを組み合わせた皮膚外用組成物（実施例１）では、ビタミンＡ油存在下でのジフェンヒドラミン単独による鎮痒効果とアラントイン単独による鎮痒効果との相加効果をはるかに凌ぐ、極めて高い鎮痒効果を示した。 The external composition for skin containing diphenhydramine together with vitamin A oil (Comparative Example 1) exhibited an antipruritic effect as compared with Reference Example 1 (control). Moreover, the external composition for skin containing allantoin (Comparative Example 2) also exhibited an antipruritic effect as compared with the (control). However, their antipruritic effect was insufficient. As is clear from Table 1, in the composition for external use for skin in which diphenhydramine and vitamin A oil were further combined with allantoin (Example 1), the antipruritic effect by diphenhydramine alone and the antipruritic effect by allantoin alone in the presence of vitamin A oil were obtained. The antipruritic effect was extremely high, far exceeding the additive effect.
Claims (5)
皮膚外用組成物に、前記（Ａ）成分及び前記（Ｂ）成分とともに（Ｃ）アラントイン及び／又はその誘導体を配合する、鎮痒効果向上方法。 A method for improving the antipruritic effect in an external composition for skin containing (A) diphenhydramine and/or a salt thereof and (B) retinol and/or a derivative thereof, comprising:
A method for improving the antipruritic effect, which comprises adding (C) allantoin and/or a derivative thereof together with the above component (A) and the above component (B) to a composition for external skin application.
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| JP2011144123A (en) * | 2010-01-13 | 2011-07-28 | Ikeda Mohando:Kk | Skin care preparation |
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