JPH0533683B2 - - Google Patents
Info
- Publication number
- JPH0533683B2 JPH0533683B2 JP60049663A JP4966385A JPH0533683B2 JP H0533683 B2 JPH0533683 B2 JP H0533683B2 JP 60049663 A JP60049663 A JP 60049663A JP 4966385 A JP4966385 A JP 4966385A JP H0533683 B2 JPH0533683 B2 JP H0533683B2
- Authority
- JP
- Japan
- Prior art keywords
- ascorbic acid
- skin
- present
- examples
- appropriate amount
- 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.)
- Expired - Lifetime
Links
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims description 26
- 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 claims description 16
- 229960005070 ascorbic acid Drugs 0.000 claims description 12
- 235000000069 L-ascorbic acid Nutrition 0.000 claims description 10
- 239000002211 L-ascorbic acid Substances 0.000 claims description 9
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 15
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 14
- 230000002087 whitening effect Effects 0.000 description 11
- 239000006210 lotion Substances 0.000 description 9
- 238000002360 preparation method Methods 0.000 description 9
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 8
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 8
- 235000019441 ethanol Nutrition 0.000 description 8
- 230000004044 response Effects 0.000 description 8
- 229960000271 arbutin Drugs 0.000 description 7
- BJRNKVDFDLYUGJ-UHFFFAOYSA-N p-hydroxyphenyl beta-D-alloside Natural products OC1C(O)C(O)C(CO)OC1OC1=CC=C(O)C=C1 BJRNKVDFDLYUGJ-UHFFFAOYSA-N 0.000 description 7
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 7
- 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 6
- 239000003205 fragrance Substances 0.000 description 6
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 6
- 239000003755 preservative agent Substances 0.000 description 6
- 238000007796 conventional method Methods 0.000 description 5
- 239000012153 distilled water Substances 0.000 description 5
- 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 4
- XDBMXUKHMOFBPJ-ZAFYKAAXSA-N L-ascorbic acid 2-sulfate Chemical compound OC[C@H](O)[C@H]1OC(=O)C(OS(O)(=O)=O)=C1O XDBMXUKHMOFBPJ-ZAFYKAAXSA-N 0.000 description 4
- 230000009471 action Effects 0.000 description 4
- 229940072065 ascorbic acid 2-sulfate Drugs 0.000 description 4
- 230000001186 cumulative effect Effects 0.000 description 4
- 239000000839 emulsion Substances 0.000 description 4
- 235000011187 glycerol Nutrition 0.000 description 4
- -1 hydroquinone glycosides Chemical class 0.000 description 4
- 239000004615 ingredient Substances 0.000 description 4
- 229940057995 liquid paraffin Drugs 0.000 description 4
- 230000002335 preservative effect Effects 0.000 description 4
- 229910052708 sodium Inorganic materials 0.000 description 4
- 239000011734 sodium Substances 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- QIGBRXMKCJKVMJ-UHFFFAOYSA-N 1,4-Benzenediol Natural products OC1=CC=C(O)C=C1 QIGBRXMKCJKVMJ-UHFFFAOYSA-N 0.000 description 3
- FERWBXLFSBWTDE-UHFFFAOYSA-N 3-aminobutan-2-ol Chemical compound CC(N)C(C)O FERWBXLFSBWTDE-UHFFFAOYSA-N 0.000 description 3
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 3
- 150000000996 L-ascorbic acids Chemical class 0.000 description 3
- 229920002125 Sokalan® Polymers 0.000 description 3
- 235000010323 ascorbic acid Nutrition 0.000 description 3
- 239000011668 ascorbic acid Substances 0.000 description 3
- 229960000541 cetyl alcohol Drugs 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
- 150000002148 esters Chemical class 0.000 description 3
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 3
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 3
- 239000000203 mixture Substances 0.000 description 3
- 229920001296 polysiloxane Polymers 0.000 description 3
- QOXOZONBQWIKDA-UHFFFAOYSA-N 3-hydroxypropyl Chemical group [CH2]CCO QOXOZONBQWIKDA-UHFFFAOYSA-N 0.000 description 2
- ZZZCUOFIHGPKAK-UHFFFAOYSA-N D-erythro-ascorbic acid Natural products OCC1OC(=O)C(O)=C1O ZZZCUOFIHGPKAK-UHFFFAOYSA-N 0.000 description 2
- 206010014970 Ephelides Diseases 0.000 description 2
- 208000003351 Melanosis Diseases 0.000 description 2
- 229930003268 Vitamin C Natural products 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- 230000000052 comparative effect Effects 0.000 description 2
- 239000006071 cream Substances 0.000 description 2
- RWSXRVCMGQZWBV-WDSKDSINSA-N glutathione Chemical compound OC(=O)[C@@H](N)CCC(=O)N[C@@H](CS)C(=O)NCC(O)=O RWSXRVCMGQZWBV-WDSKDSINSA-N 0.000 description 2
- 229930182470 glycoside Natural products 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- 239000002674 ointment 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
- 235000019154 vitamin C Nutrition 0.000 description 2
- 239000011718 vitamin C Substances 0.000 description 2
- AFQOCSDOKGNDNA-OBEHBXMUSA-N (2R)-2-[(1S)-1,2-dihydroxyethyl]-3,4-dihydroxy-2H-furan-5-one (Z)-octadec-9-enoic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O.CCCCCCCC\C=C/CCCCCCCC(O)=O AFQOCSDOKGNDNA-OBEHBXMUSA-N 0.000 description 1
- VBURMNYQYXSQEL-VFAVKCLXSA-N (2R)-2-[(1S)-1,2-dihydroxyethyl]-3,4-dihydroxy-2H-furan-5-one (Z)-octadec-9-enoic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O.CCCCCCCC\C=C/CCCCCCCC(O)=O.CCCCCCCC\C=C/CCCCCCCC(O)=O VBURMNYQYXSQEL-VFAVKCLXSA-N 0.000 description 1
- IRVNEGRHQKGRGD-WPXUHFOISA-N (2r)-2-[(1s)-1,2-dihydroxyethyl]-3,4-dihydroxy-2h-furan-5-one;hexadecanoic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O.CCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCC(O)=O IRVNEGRHQKGRGD-WPXUHFOISA-N 0.000 description 1
- PBTPTBMYJPCXRQ-MGMRMFRLSA-N (2r)-2-[(1s)-1,2-dihydroxyethyl]-3,4-dihydroxy-2h-furan-5-one;hexadecanoic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O.CCCCCCCCCCCCCCCC(O)=O PBTPTBMYJPCXRQ-MGMRMFRLSA-N 0.000 description 1
- MHUOEHQATDLJFZ-WPXUHFOISA-N (2r)-2-[(1s)-1,2-dihydroxyethyl]-3,4-dihydroxy-2h-furan-5-one;octadecanoic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O.CCCCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCCCC(O)=O MHUOEHQATDLJFZ-WPXUHFOISA-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
- CMCBDXRRFKYBDG-UHFFFAOYSA-N 1-dodecoxydodecane Chemical compound CCCCCCCCCCCCOCCCCCCCCCCCC CMCBDXRRFKYBDG-UHFFFAOYSA-N 0.000 description 1
- LITUBCVUXPBCGA-WMZHIEFXSA-N Ascorbyl stearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@H](O)[C@H]1OC(=O)C(O)=C1O LITUBCVUXPBCGA-WMZHIEFXSA-N 0.000 description 1
- 102000008186 Collagen Human genes 0.000 description 1
- 108010035532 Collagen Proteins 0.000 description 1
- 208000034656 Contusions Diseases 0.000 description 1
- 125000002353 D-glucosyl group Chemical group C1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)* 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 108010024636 Glutathione Proteins 0.000 description 1
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 description 1
- 239000004166 Lanolin Substances 0.000 description 1
- 239000004909 Moisturizer Substances 0.000 description 1
- YQINWFJNFJEWHH-UCLHFMLVSA-N OC[C@H](O)[C@H]1OC(=O)C(O)=C1O.CCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCC(O)=O Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O.CCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCC(O)=O YQINWFJNFJEWHH-UCLHFMLVSA-N 0.000 description 1
- NGUBAXUPKACQCL-UCLHFMLVSA-N OC[C@H](O)[C@H]1OC(=O)C(O)=C1O.CCCCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCCCC(O)=O Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O.CCCCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCCCC(O)=O NGUBAXUPKACQCL-UCLHFMLVSA-N 0.000 description 1
- GAKOHFNTEXOHTP-RXSVEWSESA-N OC[C@H](O)[C@H]1OC(=O)C(O)=C1O.OP(O)(=O)OP(O)(=O)OP(O)(O)=O Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O.OP(O)(=O)OP(O)(=O)OP(O)(O)=O GAKOHFNTEXOHTP-RXSVEWSESA-N 0.000 description 1
- BLQKIGOLRJPVAW-RXSVEWSESA-N OP(O)(=O)OP(O)(O)=O.OC[C@H](O)[C@H]1OC(=O)C(O)=C1O Chemical class OP(O)(=O)OP(O)(O)=O.OC[C@H](O)[C@H]1OC(=O)C(O)=C1O BLQKIGOLRJPVAW-RXSVEWSESA-N 0.000 description 1
- 208000012641 Pigmentation disease Diseases 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 description 1
- 230000005856 abnormality Effects 0.000 description 1
- 239000006096 absorbing agent Substances 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 235000006708 antioxidants Nutrition 0.000 description 1
- 239000008346 aqueous phase Substances 0.000 description 1
- 230000004098 cellular respiration Effects 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 229920001436 collagen Polymers 0.000 description 1
- 239000002537 cosmetic Substances 0.000 description 1
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 description 1
- 235000018417 cysteine Nutrition 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000008030 elimination Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 230000003631 expected effect Effects 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- 229960003180 glutathione Drugs 0.000 description 1
- 230000003054 hormonal effect Effects 0.000 description 1
- 239000003906 humectant Substances 0.000 description 1
- 125000000687 hydroquinonyl group Chemical group C1(O)=C(C=C(O)C=C1)* 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 238000005342 ion exchange Methods 0.000 description 1
- 229940039717 lanolin Drugs 0.000 description 1
- 235000019388 lanolin Nutrition 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 230000008099 melanin synthesis Effects 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 230000001333 moisturizer Effects 0.000 description 1
- JXTPJDDICSTXJX-UHFFFAOYSA-N n-Triacontane Natural products CCCCCCCCCCCCCCCCCCCCCCCCCCCCCC JXTPJDDICSTXJX-UHFFFAOYSA-N 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 229940055577 oleyl alcohol Drugs 0.000 description 1
- XMLQWXUVTXCDDL-UHFFFAOYSA-N oleyl alcohol Natural products CCCCCCC=CCCCCCCCCCCO XMLQWXUVTXCDDL-UHFFFAOYSA-N 0.000 description 1
- 239000012071 phase Substances 0.000 description 1
- 239000000049 pigment Substances 0.000 description 1
- 230000019612 pigmentation Effects 0.000 description 1
- 229940093430 polyethylene glycol 1500 Drugs 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 230000001603 reducing effect Effects 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 229940032094 squalane Drugs 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-N sulfuric acid Substances OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 238000011282 treatment Methods 0.000 description 1
- 229940099259 vaseline Drugs 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/60—Sugars; Derivatives thereof
- A61K8/602—Glycosides, e.g. rutin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/67—Vitamins
- A61K8/676—Ascorbic acid, i.e. vitamin C
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
Description
［産業上の利用分野］
本発明は皮膚美白効果が著しく改良された安全
性の高い皮膚外用剤に関する。
［従来の技術］
皮膚のしみなどの発生機序については不明な点
もあるが、一般には、ホルモンの異常や日光から
の紫外線の刺激が原因となつてメラニン色素が形
成され、これが皮膚内に異常沈着するものと考え
られている。このようなしみやあざの治療法には
メラニンの生成を抑制する物質、例えばビタミン
Ｃを大量に投与する方法、グルタチオン等を注射
する方法あるいはＬ−アスコルビン酸、システイ
ンなどを軟膏、クリーム、ローシヨンなどの形態
にして、局所に塗布するなどの方法がとられてい
る。
［発明が解決しようとする問題点］
しかしながら、これらのものの多くは、安定
性、安全性、匂い等の面において問題があり、ま
た期待できる効果は弱く、未だ満足のいくもので
はなかつた。
本発明者等は、このような事情に鑑み、真に優
れた美白効果を有する皮膚外用剤を得るべく鋭意
研究を重ねた結果、Ｌ−アスコルビン酸類とハイ
ドロキノンの配糖体とを併用すると相乗的な美白
効果が得られることを見出し、本発明を完成する
に至つた。
［問題点を解決するための手段］
すなわち、本発明はＬ−アスコルビン酸および
その誘導体よりなる群から選ばれた１種または２
種以上を0.01〜10重量％と、ハイドロキノン−β
−Ｄ−グルコシドを0.1〜20重量％とを皮膚外用
剤に含有するものである。
以下、本発明の構成について詳述する。
本発明で使用するＬ−アスコルビン酸は、一般
にビタミンＣといわれ、その強い還元作用により
細胞呼吸作用、酵素賦活作用、膠原形成作用を有
し、かつメラニン還元作用を有する。又、Ｌ−ア
スコルビン酸の誘導体としては、例えば、Ｌ−ア
スコルビン酸モノステアレート、Ｌ−アスコルビ
ン酸モノパルミテート、Ｌ−アスコルビン酸モノ
オレート等のＬ−アスコルビン酸モノアルキルエ
ステル類、Ｌ−アスコルビン酸モノリン酸エステ
ル、Ｌ−アスコルビン酸−２−硫酸のようなＬ−
アスコルビン酸モノエステル誘導体、Ｌ−アスコ
ルビン酸ジステアレート、Ｌ−アスコルビン酸ジ
パルミテート、Ｌ−アスコルビン酸ジオレート等
のＬ−アスコルビン酸ジリン酸エステルのような
Ｌ−アスコルビン酸ジエステル誘導体、Ｌ−アス
コルビン酸トリステアレート、Ｌ−アスコルビン
酸トリパルミテート、Ｌ−アスコルビン酸トリオ
レート等のトリアルキルエステル類、Ｌ−アスコ
ルビン酸トリリン酸エステル等のアスコルビン酸
トリエステル誘導体等をあげることができる。本
発明の実施に当たつてはこれらの中から１種又は
２種以上が適宜選択され配合される。
Ｌ−アスコルビン酸又はＬ−アスコルビン酸の
誘導体は、皮膚外用中に、0.01重量％以上配合す
ると効果があらわれ、本発明の効果を発揮するた
めには10重量％程度で十分である。
本発明に用いられるハイドロキノンの配糖体は
下記一般式であらわされる。
すなわち式中、ＲがＤ−グルコース残基でハイ
ドロキノンにβ結合した、ハイドロキノン−β−
Ｄ−グルコシド（一般名：アルブチン）である。
配合量は皮膚外用全量中の0.1〜20重量％であ
る。
本発明の皮膚外用剤には上記した必須成分の他
に通常化粧品や医薬品等の皮膚外用剤に用いられ
る他の成分、例えば油分、湿潤剤、紫外線吸収
剤、酸化防止剤、界面活性剤、防腐剤、保湿剤、
香料、水、アルコール、増粘剤等を必要に応じて
適宜配合することができる。
本発明に係る皮膚外用剤の剤型は任意であり、
例えば化粧水などの可溶化系、乳液、クリームな
どの乳化剤、又は軟膏、分散液などの任意の剤型
をとることができる。
［実施例］
次に実施例をあげて本発明をさらに詳細に説明
する。本発明はこれにより限定されるものではな
い。配合量は重量％である。
尚、美白効果は、累積塗布による皮膚に対する
色白効果、シミ、ソバカスの解消などの使用テス
トから判定した。
累積塗布による美白効果試験
（試験方法）
色黒、しみ、そばかす等に悩む、被試験者、１
群20名として、１つの試料ローシヨンを朝夕、３
ケ月間、毎日顔面に塗布し、３ケ月目にその美白
効果を調べた。
（判定基準）
著 効：色素沈着がほとんど目立たなくなつ
た。
有 効：非常にうすくなつた。
やや有効：ややうすくなつた。
無 効：変化無し
（判定）
◎：被試験者のうち著効、有効の示す割合
（有効率）が80％以上の場合
○：被試験者のうち著効、有効の示す割合
（有効率）が60％以上80％未満の場合
△：被試験者のうち著効、有効の示す割合
（有効率）が40％以上60％未満の場合
×：被試験者のうち著効、有効の示す割合
（有効率）が40％未満の場合
実施例１、２、比較例１〜３についてのべる。
次の配合組成よりなるローシヨンを調整し、そ
の累積塗布による美白効果について調べた。
処方と製法は以下のとおりである。即ち95％エ
チルアルコール10ｇに、POE（20）ラウリルエー
テル0.5ｇおよび香料を混合紙、次いでこの中に
あらかじめグリセイン２ｇとプロピレングリコー
ル１ｇ特許請求の範囲、クエン酸0.2ｇ、Ｌ−ア
スコルビン酸またはその誘導体及びアルブチンと
を加え、さらに、蒸留水を全重量が100ｇになる
ように必要量を添加し混合して調整した。
[Industrial Application Field] The present invention relates to a highly safe external skin preparation with significantly improved skin whitening effects. [Conventional technology] Although there are some points that are unclear about the mechanism by which skin spots occur, in general, melanin pigments are formed due to hormonal abnormalities or stimulation of ultraviolet rays from sunlight, and this is caused by the formation of melanin within the skin. It is thought that it is abnormally deposited. Treatments for these spots and bruises include administering large amounts of substances that suppress melanin production, such as large doses of vitamin C, injections of glutathione, or the use of ointments, creams, and lotions containing L-ascorbic acid, cysteine, etc. Methods such as making it into a form and applying it locally are used. [Problems to be Solved by the Invention] However, many of these products have problems in terms of stability, safety, odor, etc., and the expected effects are weak, so they are not yet satisfactory. In view of these circumstances, the present inventors have conducted intensive research to obtain a skin external preparation with truly excellent whitening effects, and have found that the combination of L-ascorbic acids and hydroquinone glycosides has a synergistic effect. The present inventors have discovered that a skin whitening effect can be obtained, and have completed the present invention. [Means for Solving the Problems] That is, the present invention provides one or two selected from the group consisting of L-ascorbic acid and its derivatives.
0.01-10% by weight of seeds or more, hydroquinone-β
The skin external preparation contains 0.1 to 20% by weight of -D-glucoside. Hereinafter, the configuration of the present invention will be explained in detail. L-ascorbic acid used in the present invention is generally referred to as vitamin C, and due to its strong reducing action, it has cellular respiration action, enzyme activation action, collagen formation action, and melanin reduction action. Examples of derivatives of L-ascorbic acid include L-ascorbic acid monoalkyl esters such as L-ascorbic acid monostearate, L-ascorbic acid monopalmitate, and L-ascorbic acid monooleate; L-acid esters, such as L-ascorbic acid-2-sulfuric acid
Ascorbic acid monoester derivatives, L-ascorbic acid diester derivatives such as L-ascorbic acid diphosphate esters such as L-ascorbic acid distearate, L-ascorbic acid dipalmitate, L-ascorbic acid dioleate, L-ascorbic acid tristearate, Examples include trialkyl esters such as L-ascorbic acid tripalmitate and L-ascorbic acid triolate, and ascorbic acid triester derivatives such as L-ascorbic acid triphosphate. In carrying out the present invention, one or more of these may be appropriately selected and blended. L-ascorbic acid or a derivative of L-ascorbic acid is effective when added in an amount of 0.01% by weight or more during external use on the skin, and about 10% by weight is sufficient to exhibit the effects of the present invention. The hydroquinone glycoside used in the present invention is represented by the following general formula. That is, in the formula, R is a D-glucose residue β-bonded to hydroquinone, hydroquinone-β-
D-glucoside (generic name: arbutin). The blending amount is 0.1 to 20% by weight based on the total amount for external use on the skin. In addition to the above-mentioned essential ingredients, the external skin preparation of the present invention contains other ingredients normally used in external skin preparations such as cosmetics and pharmaceuticals, such as oil, humectants, ultraviolet absorbers, antioxidants, surfactants, and preservatives. agent, moisturizer,
Flavors, water, alcohol, thickeners, etc. can be added as appropriate. The dosage form of the skin external preparation according to the present invention is arbitrary,
For example, it can take any form such as a solubilized system such as a lotion, an emulsifier such as a milky lotion or a cream, or an ointment or a dispersion. [Example] Next, the present invention will be explained in more detail by giving examples. The present invention is not limited thereby. The blending amount is in weight%. The whitening effect was determined from usage tests such as the whitening effect on the skin after cumulative application, and the elimination of spots and freckles. Whitening effect test by cumulative application (test method) Test subject suffering from dark skin, age spots, freckles, etc., 1
As a group of 20 people, one sample lotion was given 3 times in the morning and evening.
It was applied to the face every day for several months, and its whitening effect was examined after the third month. (Judgment criteria) Results: Pigmentation became almost invisible. Effective: Very pale. Slightly effective: Slightly less effective. Ineffective: No change (judgment) ◎: When the percentage of test subjects who show an excellent response or effective response (effective rate) is 80% or more ○: The percentage of test subjects who show an excellent response or effective response (effective rate) is 60% or more and less than 80% △: Proportion of test subjects with excellent response or effective response (efficacy rate) is 40% or more and less than 60% ×: Proportion of test subjects with excellent response or effective response (Effective rate) is less than 40% Examples 1 and 2 and Comparative Examples 1 to 3 will be described. A lotion with the following composition was prepared and the whitening effect of cumulative application was investigated. The prescription and manufacturing method are as follows. That is, mix paper with 10 g of 95% ethyl alcohol, 0.5 g of POE (20) lauryl ether, and fragrance, and then add 2 g of glycein and 1 g of propylene glycol in advance, 0.2 g of citric acid, and L-ascorbic acid or its derivatives. and arbutin were added, and the necessary amount of distilled water was added so that the total weight was 100 g, and the mixture was mixed and adjusted.
【表】
実施例１、２、比較例１、２、３から明らかな
ように、本発明の皮膚外用剤は美白効果に優れる
新規な皮膚外用剤である。
実施例 ３
乳液
次の処方に従い、常法により乳液を製造した。
POE（20）POP（２）セチルアルコールエーテル
1.0
シリコーンKF96（20cs）（信越化学） 2.0
流動パラフイン 3.0
プロピレングリコール 5.0
グリセリン 2.0
エチルアルコール 5.0
カルボキシビニルポリマー 0.3
ヒドロキシプロピルセルロース 0.1
２−アミノメチルプロパノール 0.1
アスコルビン酸−２−硫酸Na 1.0
アルブチン 1.0
防腐剤 適量
香 料 適量
蒸留水 残量
実施例 ４
乳液
次の処方に従い、常法により乳液を製造した。
POE（20）POP（２）セチルアルコールエーテル
1.0
シリコーンKF96（20cs）（信越化学） 2.0
流動パラフイン 3.0
プロピレングリコール 5.0
グリセリン 2.0
エチルアルコール 15.0
カルボキシビニルポリマー 3.0
ヒドロキシプロピルセルロース 0.1
２−アミノメチルプロパノール 0.1
アスコルビン酸−２−硫酸Na 1.0
アルブチン 10.0
防腐剤 適量
香 料 適量
蒸留水 残量
実施例３および４を実施例１、２と同様に累積
塗布による美白効果を測定した。結果を表２に示
す。[Table] As is clear from Examples 1 and 2 and Comparative Examples 1, 2, and 3, the skin external preparation of the present invention is a novel skin external preparation with excellent whitening effects. Example 3 Emulsion A milky lotion was produced by a conventional method according to the following recipe. POE (20) POP (2) Cetyl alcohol ether
1.0 Silicone KF96 (20cs) (Shin-Etsu Chemical) 2.0 Liquid paraffin 3.0 Propylene glycol 5.0 Glycerin 2.0 Ethyl alcohol 5.0 Carboxy vinyl polymer 0.3 Hydroxypropyl cellulose 0.1 2-aminomethylpropanol 0.1 Sodium ascorbic acid-2-sulfate 1.0 Arbutin 1.0 Preservative Appropriate amount of fragrance Ingredients: Appropriate amount of distilled water Remaining amount Example 4 Emulsion A milky lotion was produced by a conventional method according to the following recipe. POE (20) POP (2) Cetyl alcohol ether
1.0 Silicone KF96 (20cs) (Shin-Etsu Chemical) 2.0 Liquid paraffin 3.0 Propylene glycol 5.0 Glycerin 2.0 Ethyl alcohol 15.0 Carboxy vinyl polymer 3.0 Hydroxypropyl cellulose 0.1 2-aminomethylpropanol 0.1 Sodium ascorbic acid-2-sulfate 1.0 Arbutin 10.0 Preservative Appropriate amount of fragrance Material: Appropriate amount of distilled water Remaining amount: The whitening effect of Examples 3 and 4 was measured by cumulative application in the same manner as Examples 1 and 2. The results are shown in Table 2.
【表】
実施例 ５
乳液
次の処方に従い、常法により乳液を製造した。
ステアリン酸 2.0
セタノール 1.0
ワセリン 3.0
ラノリンアルコール 2.0
流動パラフイン 8.0
スクワラン 3.0
アスコルビン酸−２−硫酸Na 0.1
アルブチン 0.1
POE（10）モノオレート 2.5
トリエタノールアミン 1.0
プロピレングリコール 5.0
防腐剤 適量
香 料 適量
蒸留水 残量
実施例 ６
ピールオフ型パツク
次の処方に従い、常法によりパツクを製造し
た。
（アルコール相）
95％エタノール 10.0
POE（15）オレイルアルコールエーテル 2.0
防腐剤 適量
香 料 適量
（水相）
アスコルビン酸 1.0
アルブチン 6.0
ポリビニルアルコール 12.0
グリセリン 3.0
ポリエチレングリコール1500 1.0
イオン交換水 残余
実施例 ７
乳液
次の処方に従い、常法により乳液を製造した。
POE（20）POP（２）セチルアルコールエーテル
1.0
シリコーンKF96（20cs）（信越化学） 2.0
流動パラフイン 3.0
プロピレングリコール 5.0
グリセリン 2.0
エチルアルコール 15.0
カルボキシビニルポリマー 0.3
ヒドロキシプロピルセルロース 0.1
２−アミノメチルプロパノール 0.1
アスコルビン酸−２−硫酸Na 0.1
アルブチン 20.0
防腐剤 適量
香 料 適量
蒸留水 残量
実施例５〜７の皮膚外用剤は、累積塗布による
美白効果に優れていた。[Table] Example 5 Emulsion A milky lotion was produced by a conventional method according to the following recipe. Stearic acid 2.0 Setanol 1.0 Vaseline 3.0 Lanolin alcohol 2.0 Liquid paraffin 8.0 Squalane 3.0 Sodium ascorbic acid-2-sulfate 0.1 Arbutin 0.1 POE (10) monooleate 2.5 Triethanolamine 1.0 Propylene glycol 5.0 Preservative Appropriate amount Fragrance Appropriate amount Distilled water Remaining amount examples 6. Peel-off type pack A pack was manufactured by a conventional method according to the following recipe. (Alcohol phase) 95% ethanol 10.0 POE (15) Oleyl alcohol ether 2.0 Preservatives Appropriate amount Fragrance Appropriate amount (Aqueous phase) Ascorbic acid 1.0 Arbutin 6.0 Polyvinyl alcohol 12.0 Glycerin 3.0 Polyethylene glycol 1500 1.0 Ion exchange water Remaining example 7 Emulsion Next A milky lotion was produced by a conventional method according to the prescription. POE (20) POP (2) Cetyl alcohol ether
1.0 Silicone KF96 (20cs) (Shin-Etsu Chemical) 2.0 Liquid paraffin 3.0 Propylene glycol 5.0 Glycerin 2.0 Ethyl alcohol 15.0 Carboxy vinyl polymer 0.3 Hydroxypropyl cellulose 0.1 2-aminomethylpropanol 0.1 Sodium ascorbic acid-2-sulfate 0.1 Arbutin 20.0 Preservative Appropriate amount fragrance Ingredients: Appropriate amount of distilled water Remaining amount The skin external preparations of Examples 5 to 7 had excellent whitening effects when applied cumulatively.
Claims (1)
る群から選ばれた１種または２種以上を0.1〜10
重量％と、ハイドロキノン−β−Ｄ−グルコシド
を0.1〜20重量％含有することを特徴とする皮膚
外用剤。1 0.1 to 10 of one or more selected from the group consisting of L-ascorbic acid and its derivatives
% by weight and 0.1 to 20% by weight of hydroquinone-β-D-glucoside.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP60049663A JPS61207316A (en) | 1985-03-13 | 1985-03-13 | External agent for skin |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP60049663A JPS61207316A (en) | 1985-03-13 | 1985-03-13 | External agent for skin |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS61207316A JPS61207316A (en) | 1986-09-13 |
| JPH0533683B2 true JPH0533683B2 (en) | 1993-05-20 |
Family
ID=12837417
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP60049663A Granted JPS61207316A (en) | 1985-03-13 | 1985-03-13 | External agent for skin |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS61207316A (en) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU618517B2 (en) * | 1986-12-23 | 1992-01-02 | Eugene J. Van Scott | Additives enhancing topical actions of therapeutic agents |
| JP3004707B2 (en) * | 1990-11-01 | 2000-01-31 | 株式会社資生堂 | External preparation for skin |
| US6037481A (en) * | 1997-08-08 | 2000-03-14 | Industria E Comercio De Cosmeticos Natura Ltda | Process for stabilizing levogyre ascorbic acid (LAA), a stable aqueous LAA composition, a process for preparing a stable topical solution, an emulsion, a vitamin product, and a method for cosmetic, pharmaceutical or nutritional treatment |
| JP2000095641A (en) * | 1998-09-25 | 2000-04-04 | Kanebo Ltd | Bleaching preparation |
| EP1153602B1 (en) * | 1999-12-20 | 2008-11-05 | Shiseido Company Limited | Skin preparations for external use comprising diethoxyethyl succinate |
| JP4410971B2 (en) * | 2002-02-08 | 2010-02-10 | 小川香料株式会社 | Naphthol glycoside and whitening external preparation composition containing the same |
| JP2006063067A (en) * | 2004-07-30 | 2006-03-09 | Ezaki Glico Co Ltd | Skin care preparation for external use |
| US9168398B2 (en) | 2007-11-14 | 2015-10-27 | Omp, Inc. | Skin treatment compositions |
| JP2012158554A (en) * | 2011-02-01 | 2012-08-23 | Mikimoto Pharmaceut Co Ltd | Skin care preparation |
| JP2012171908A (en) * | 2011-02-22 | 2012-09-10 | Mikimoto Pharmaceut Co Ltd | Whitening cosmetic |
| JP6830000B2 (en) * | 2017-02-01 | 2021-02-17 | ちふれホールディングス株式会社 | Composition for suppressing pheomelanin |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS4986554A (en) * | 1972-12-25 | 1974-08-19 | ||
| JPS5520739A (en) * | 1978-07-31 | 1980-02-14 | Kanebo Ltd | Oily beautiful and white cosmetic |
| JPS56120612A (en) * | 1980-02-27 | 1981-09-22 | Kanebo Keshohin Kk | Beautifying cosmetic |
| JPS59104308A (en) * | 1982-12-06 | 1984-06-16 | Kanebo Ltd | Pasty cosmetic for whitening skin color |
| JPS6016906A (en) * | 1983-07-07 | 1985-01-28 | Pola Chem Ind Inc | External drug for skin |
-
1985
- 1985-03-13 JP JP60049663A patent/JPS61207316A/en active Granted
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS4986554A (en) * | 1972-12-25 | 1974-08-19 | ||
| JPS5520739A (en) * | 1978-07-31 | 1980-02-14 | Kanebo Ltd | Oily beautiful and white cosmetic |
| JPS56120612A (en) * | 1980-02-27 | 1981-09-22 | Kanebo Keshohin Kk | Beautifying cosmetic |
| JPS59104308A (en) * | 1982-12-06 | 1984-06-16 | Kanebo Ltd | Pasty cosmetic for whitening skin color |
| JPS6016906A (en) * | 1983-07-07 | 1985-01-28 | Pola Chem Ind Inc | External drug for skin |
Also Published As
| Publication number | Publication date |
|---|---|
| JPS61207316A (en) | 1986-09-13 |
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| EXPY | Cancellation because of completion of term |