JPS63174910A - External drug for skin - Google Patents
External drug for skinInfo
- Publication number
- JPS63174910A JPS63174910A JP441887A JP441887A JPS63174910A JP S63174910 A JPS63174910 A JP S63174910A JP 441887 A JP441887 A JP 441887A JP 441887 A JP441887 A JP 441887A JP S63174910 A JPS63174910 A JP S63174910A
- Authority
- JP
- Japan
- Prior art keywords
- arbutin
- skin
- sodium bisulfite
- external drug
- drug
- 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
- 239000003814 drug Substances 0.000 title abstract description 5
- 229940079593 drug Drugs 0.000 title abstract 4
- 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 abstract description 46
- 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 claims abstract description 24
- 229960000271 arbutin Drugs 0.000 claims abstract description 23
- DWAQJAXMDSEUJJ-UHFFFAOYSA-M Sodium bisulfite Chemical compound [Na+].OS([O-])=O DWAQJAXMDSEUJJ-UHFFFAOYSA-M 0.000 claims abstract description 18
- 235000010267 sodium hydrogen sulphite Nutrition 0.000 claims abstract description 18
- 238000002360 preparation method Methods 0.000 claims description 14
- 230000000694 effects Effects 0.000 abstract description 9
- 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 abstract description 4
- 102000003425 Tyrosinase Human genes 0.000 abstract description 2
- 108060008724 Tyrosinase Proteins 0.000 abstract description 2
- SUSRLLXAXAIZPH-OBPIAQAESA-N hydroquinone beta-D-glucopyranoside Natural products OC[C@H]1O[C@@H](Cc2ccc(O)cc2)[C@H](O)[C@@H](O)[C@@H]1O SUSRLLXAXAIZPH-OBPIAQAESA-N 0.000 abstract description 2
- 239000000049 pigment Substances 0.000 abstract description 2
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 230000007547 defect Effects 0.000 abstract 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 8
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 6
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 description 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 6
- 238000004040 coloring Methods 0.000 description 5
- 239000003205 fragrance Substances 0.000 description 5
- 239000008213 purified water Substances 0.000 description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- -1 citric acid Chemical class 0.000 description 4
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 4
- ZAKOWWREFLAJOT-CEFNRUSXSA-N D-alpha-tocopherylacetate Chemical compound CC(=O)OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C ZAKOWWREFLAJOT-CEFNRUSXSA-N 0.000 description 3
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 239000006071 cream Substances 0.000 description 3
- 235000019441 ethanol Nutrition 0.000 description 3
- 229960001617 ethyl hydroxybenzoate Drugs 0.000 description 3
- 235000010228 ethyl p-hydroxybenzoate Nutrition 0.000 description 3
- 239000004403 ethyl p-hydroxybenzoate Substances 0.000 description 3
- NUVBSKCKDOMJSU-UHFFFAOYSA-N ethylparaben Chemical compound CCOC(=O)C1=CC=C(O)C=C1 NUVBSKCKDOMJSU-UHFFFAOYSA-N 0.000 description 3
- 235000011187 glycerol Nutrition 0.000 description 3
- 239000006210 lotion Substances 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 230000002087 whitening effect Effects 0.000 description 3
- MRAMPOPITCOOIN-VIFPVBQESA-N (2r)-n-(3-ethoxypropyl)-2,4-dihydroxy-3,3-dimethylbutanamide Chemical compound CCOCCCNC(=O)[C@H](O)C(C)(C)CO MRAMPOPITCOOIN-VIFPVBQESA-N 0.000 description 2
- QFOHBWFCKVYLES-UHFFFAOYSA-N Butylparaben Chemical compound CCCCOC(=O)C1=CC=C(O)C=C1 QFOHBWFCKVYLES-UHFFFAOYSA-N 0.000 description 2
- QIGBRXMKCJKVMJ-UHFFFAOYSA-N Hydroquinone Chemical compound OC1=CC=C(O)C=C1 QIGBRXMKCJKVMJ-UHFFFAOYSA-N 0.000 description 2
- ILRKKHJEINIICQ-OOFFSTKBSA-N Monoammonium glycyrrhizinate Chemical compound N.O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@H]1CC[C@]2(C)[C@H]3C(=O)C=C4[C@@H]5C[C@](C)(CC[C@@]5(CC[C@@]4(C)[C@]3(C)CC[C@H]2C1(C)C)C)C(O)=O)C(O)=O)[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O ILRKKHJEINIICQ-OOFFSTKBSA-N 0.000 description 2
- 229920002125 Sokalan® Polymers 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 2
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 description 2
- 229960002216 methylparaben Drugs 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 230000002265 prevention Effects 0.000 description 2
- 210000002966 serum Anatomy 0.000 description 2
- 229940079827 sodium hydrogen sulfite Drugs 0.000 description 2
- GEHJYWRUCIMESM-UHFFFAOYSA-L sodium sulfite Chemical compound [Na+].[Na+].[O-]S([O-])=O GEHJYWRUCIMESM-UHFFFAOYSA-L 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
- 229940042585 tocopherol acetate Drugs 0.000 description 2
- 229940099259 vaseline Drugs 0.000 description 2
- 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
- HIQIXEFWDLTDED-UHFFFAOYSA-N 4-hydroxy-1-piperidin-4-ylpyrrolidin-2-one Chemical compound O=C1CC(O)CN1C1CCNCC1 HIQIXEFWDLTDED-UHFFFAOYSA-N 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- 239000005995 Aluminium silicate Substances 0.000 description 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
- PQUCIEFHOVEZAU-UHFFFAOYSA-N Diammonium sulfite Chemical compound [NH4+].[NH4+].[O-]S([O-])=O PQUCIEFHOVEZAU-UHFFFAOYSA-N 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 239000004166 Lanolin Substances 0.000 description 1
- 229920001213 Polysorbate 20 Polymers 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 0.000 description 1
- 229920002385 Sodium hyaluronate Polymers 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 235000012211 aluminium silicate Nutrition 0.000 description 1
- 239000008346 aqueous phase Substances 0.000 description 1
- 230000003796 beauty Effects 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- 229940067596 butylparaben Drugs 0.000 description 1
- GBAOBIBJACZTNA-UHFFFAOYSA-L calcium sulfite Chemical compound [Ca+2].[O-]S([O-])=O GBAOBIBJACZTNA-UHFFFAOYSA-L 0.000 description 1
- 235000010261 calcium sulphite Nutrition 0.000 description 1
- 239000004359 castor oil Substances 0.000 description 1
- 235000019438 castor oil Nutrition 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 239000002537 cosmetic Substances 0.000 description 1
- ZAKOWWREFLAJOT-UHFFFAOYSA-N d-alpha-Tocopheryl acetate Natural products CC(=O)OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C ZAKOWWREFLAJOT-UHFFFAOYSA-N 0.000 description 1
- SZXQTJUDPRGNJN-UHFFFAOYSA-N dipropylene glycol Chemical compound OCCCOCCCO SZXQTJUDPRGNJN-UHFFFAOYSA-N 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 235000008524 evening primrose extract Nutrition 0.000 description 1
- 229940089020 evening primrose oil Drugs 0.000 description 1
- 239000010475 evening primrose oil Substances 0.000 description 1
- FOYKKGHVWRFIBD-UHFFFAOYSA-N gamma-tocopherol acetate Natural products CC(=O)OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1 FOYKKGHVWRFIBD-UHFFFAOYSA-N 0.000 description 1
- 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 1
- 229940074774 glycyrrhizinate Drugs 0.000 description 1
- LPLVUJXQOOQHMX-QWBHMCJMSA-N glycyrrhizinic acid Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@@H]1C([C@H]2[C@]([C@@H]3[C@@]([C@@]4(CC[C@@]5(C)CC[C@@](C)(C[C@H]5C4=CC3=O)C(O)=O)C)(C)CC2)(C)CC1)(C)C)C(O)=O)[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O LPLVUJXQOOQHMX-QWBHMCJMSA-N 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- OIKBVOIOVNEVJR-UHFFFAOYSA-N hexadecyl 6-methylheptanoate Chemical compound CCCCCCCCCCCCCCCCOC(=O)CCCCC(C)C OIKBVOIOVNEVJR-UHFFFAOYSA-N 0.000 description 1
- 239000003906 humectant Substances 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 229940119170 jojoba wax Drugs 0.000 description 1
- NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 229940039717 lanolin Drugs 0.000 description 1
- 235000019388 lanolin Nutrition 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 239000004200 microcrystalline wax Substances 0.000 description 1
- 235000019808 microcrystalline wax Nutrition 0.000 description 1
- JXTPJDDICSTXJX-UHFFFAOYSA-N n-Triacontane Natural products CCCCCCCCCCCCCCCCCCCCCCCCCCCCCC JXTPJDDICSTXJX-UHFFFAOYSA-N 0.000 description 1
- 230000007935 neutral effect Effects 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
- 239000003921 oil Substances 0.000 description 1
- 235000019198 oils Nutrition 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 239000004006 olive oil Substances 0.000 description 1
- 235000008390 olive oil Nutrition 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 239000012071 phase Substances 0.000 description 1
- 238000006116 polymerization reaction Methods 0.000 description 1
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 239000011148 porous material Substances 0.000 description 1
- BHZRJJOHZFYXTO-UHFFFAOYSA-L potassium sulfite Chemical compound [K+].[K+].[O-]S([O-])=O BHZRJJOHZFYXTO-UHFFFAOYSA-L 0.000 description 1
- 235000019252 potassium sulphite Nutrition 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 238000007127 saponification reaction Methods 0.000 description 1
- 239000001509 sodium citrate Substances 0.000 description 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
- 229940010747 sodium hyaluronate Drugs 0.000 description 1
- 235000010265 sodium sulphite Nutrition 0.000 description 1
- 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 1
- 229940032094 squalane Drugs 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 239000006097 ultraviolet radiation absorber Substances 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
Classifications
-
- 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
-
- 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
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/74—Biological properties of particular ingredients
- A61K2800/78—Enzyme modulators, e.g. Enzyme agonists
- A61K2800/782—Enzyme inhibitors; Enzyme antagonists
Abstract
Description
【発明の詳細な説明】
〔産業上の利用分野〕
本発明はアルブチンを配合してなる皮膚外用剤の着色に
対する安定性を増し、美白効果にすぐれた安全性の高い
皮膚外用剤に関するものである。[Detailed Description of the Invention] [Field of Industrial Application] The present invention relates to a highly safe external skin preparation containing arbutin that has increased stability against coloring and has excellent whitening effects. .
アルブチンはハイドロキノンにＤ−グルコースがβ−配
合したハイドロキノン−β−Ｄ−グルコピラノシドであ
る。この化合物は皮膚のじみやほぼかすなどの原因とな
るメラニン色素の生成に関与する酵素チロシナーゼを阻
害する作用を有するので美白効果を有する。この作用を
利用してアルブチンを有効成分とした皮膚外用剤の特許
が開示されている。（特開昭６０−５６９１２号公報、
特開昭６０−１６９０６公報等）
〔発明が解決しようとする問題点〕
ところが、アルブチンは、製剤の基材に配合し日光暴露
条件下や高温下に保存すると、始め淡黄色に着色し、そ
の着色度は経時的に増大し褐変化する傾向がある。この
着色によって商品価値が低下することは避けられない。Arbutin is hydroquinone-β-D-glucopyranoside, which is a combination of hydroquinone and D-glucose. This compound has a whitening effect because it has the effect of inhibiting the enzyme tyrosinase, which is involved in the production of melanin pigment, which causes skin blemishes and blemishes. A patent for an external skin preparation containing arbutin as an active ingredient has been disclosed by utilizing this effect. (Japanese Patent Application Laid-Open No. 60-56912,
[Problems to be solved by the invention] However, when arbutin is added to the base material of a preparation and stored under conditions of exposure to sunlight or high temperatures, it initially becomes pale yellow in color, The degree of coloration tends to increase over time and turn brown. This coloring inevitably reduces the product value.
本発明者らはアルブチンの着色が経時的に増大するのを
防止する目的で、さまざまな有機酸、例えばクエン酸、
酒石酸、乳酸、亜硫酸水素ナトリウム、亜硫酸アンモニ
ウム、亜硫酸カリウム、亜硫酸ナトリウムあるいは亜硫
酸カルシウム等についてそれらの効果を検討した結果、
亜硫酸水素すトリウムに優れた着色防止効果があること
を見い出し、特に亜硫酸水素ナトリウムをｐＨ４〜７の
弱酸性から中性領域で使用することによって著しく着色
が防止されることを見い出し、本発明を完成するに至っ
た。In order to prevent the coloration of arbutin from increasing over time, the present inventors used various organic acids, such as citric acid,
As a result of examining the effects of tartaric acid, lactic acid, sodium bisulfite, ammonium sulfite, potassium sulfite, sodium sulfite, calcium sulfite, etc.
It was discovered that sodium bisulfite has an excellent coloring prevention effect, and in particular, it was discovered that coloring can be significantly prevented by using sodium hydrogensulfite in the weakly acidic to neutral pH range of 4 to 7, and the present invention was completed. I ended up doing it.
すなわち、本発明は亜硫酸水素ナトリウムとアルブチン
とを配合することを特徴とする皮膚外用剤である。That is, the present invention is an external skin preparation characterized by containing sodium bisulfite and arbutin.
本発明に係る皮膚外用剤に配合される亜硫酸水素ナトリ
ウムの配合量はアルブチン１ｆｆｉＥｔ部に対して０．
０００１〜１重量部、好ましくは０．００１〜０．１重
量部である。The amount of sodium bisulfite to be blended into the skin external preparation according to the present invention is 0.000% per 1ffiEt part of arbutin.
0001 to 1 part by weight, preferably 0.001 to 0.1 part by weight.
また本発明に用いられるアルブチンの皮膚外用剤全量に
対する配合量は通常０．１〜３０重量％であり、好まし
くは１〜２０重量％である。Further, the amount of arbutin used in the present invention is usually 0.1 to 30% by weight, preferably 1 to 20% by weight, based on the total amount of the skin external preparation.
本発明の皮膚外用剤においては前記必須構成成分の他に
、化粧品、医薬品等に一般に用いられる各種成分、すな
わち水性成分、粉末成分、界面活性剤、保湿剤、増粘剤
、紫外線吸収剤、色剤、皮Ｈ栄養剤（酢酸１−コフエロ
ール、パントテニールエチルエーテル、グリチルリチン
酸塩など）、香料等を配合することができる。もちろん
これらは本発明の効果を損なわない量的、質的範囲内で
使用されなければないない。In addition to the above-mentioned essential components, the external skin preparation of the present invention contains various components commonly used in cosmetics, pharmaceuticals, etc., namely, an aqueous component, a powder component, a surfactant, a humectant, a thickener, an ultraviolet absorber, and a color. Agents, skin nourishing agents (1-cophyerol acetate, pantothenyl ethyl ether, glycyrrhizinate, etc.), fragrances, etc. can be blended. Of course, these must be used within a quantitative and qualitative range that does not impair the effects of the present invention.
本発明の皮膚外用剤の剤型は任意であり、例えば化粧水
等の可溶化系、乳液、クリーム等の乳化系あるいは軟膏
、分散液等の剤型をとることができる。The formulation for external use on the skin of the present invention may be in any form, and may be, for example, a solubilized system such as a lotion, an emulsified system such as a milky lotion or a cream, or a dosage form such as an ointment or a dispersion.
つぎに実施例を挙げて本発明の効果について説明する。 Next, the effects of the present invention will be explained with reference to Examples.
本発明はこれによって限定されるものではない。The present invention is not limited thereby.
実施例１：クリーム
（Ａ）セタノール ５．０マ
イクロクリスタリンワツクス ２．０ワセリン
５．０スクワラン
５．０イソオクタン酸セチル
３．０ホホバ油 ２．０
ポリオキシエチレン（２０）
ソルビタンモノラウリン酸エステル ２．０酢酸トコフ
エロール ０．０５パントテニールエチ
ルエーテル ０．１香料
０．３エチルパラベン ０．
３（Ｂ）アルブチン ５．０亜
硫酸水素ナトリウム ０．０１１．３−ブ
チレングリコール ５．０プロピレングリコール
５．０グリチルリチン酸
モノアンモニウム塩 ０．０５精製水
残余油相部Ａを７０℃にて溶解す
る。水相部Ｂを７０℃にて熔解し、ＢにＡを混合し、乳
化機にて乳化後孔化物を熱交換器にて３０℃まで冷却し
たのち充填を行う。Example 1: Cream (A) Setanol 5.0 Microcrystalline wax 2.0 Vaseline
5.0 squalane
5.0 Cetyl isooctanoate
3.0 jojoba oil 2.0
Polyoxyethylene (20) Sorbitan monolaurate 2.0 Tocopheryl acetate 0.05 Pantothenyl ethyl ether 0.1 Fragrance
0.3 Ethylparaben 0.
3(B) Arbutin 5.0 Sodium bisulfite 0.01 1.3-Butylene glycol 5.0 Propylene glycol 5.0 Glycyrrhizic acid monoammonium salt 0.05 Purified water
The remaining oil phase A is dissolved at 70°C. Aqueous phase B is melted at 70°C, A is mixed with B, emulsified in an emulsifier, the porous material is cooled to 30°C in a heat exchanger, and then filled.
実施例２：乳液
（Ａ）ステアリン酸 １．０ピー
スワツクス １．０ワセリン
２．５脱臭ラノリン
１．０月見草油
２．０ミリスチン酸イソプロピル ５．０ポリ
オキシエチレン（６０）
硬化ヒマシ油 ２．０
酢酸トコフェロール ０．０５エチルパ
ラベン ０．２ブチルパラベン
０．１香料
０．２（Ｂ）アルブチン
１０．０亜硫酸水素ナトリウム １．０
グリセリン ５．０ヒアルロン酸
ナトリウム ０．０１カルボキシビニルポ
リマー ０．２水酸化カリウム
０．２精製水 残余
製造法はクリームに準する。Example 2: Emulsion (A) Stearic acid 1.0 Piece Wax 1.0 Vaseline
2.5 Deodorized lanolin
1.0 Evening primrose oil
2.0 Isopropyl myristate 5.0 Polyoxyethylene (60) Hydrogenated castor oil 2.0 Tocopherol acetate 0.05 Ethylparaben 0.2 Butylparaben
0.1 fragrance
0.2(B) Arbutin
10.0 Sodium bisulfite 1.0
Glycerin 5.0 Sodium hyaluronate 0.01 Carboxyvinyl polymer 0.2 Potassium hydroxide
0.2 Purified water The remaining manufacturing method is similar to cream.
実施例３：美容液
（Ａ）エタノール（９５％） １０．
０ポリオキシエチレン（２０） １．０オレ
イルエーテル １０．０
メチルパラベン ０．１５−パント
テニルエチルエーテル ０．１（Ｂ）水酸化カリ
ウム ０．１（Ｃ）グリセリン
５．０ジプロピレングリコール
１０．０亜硫酸水素ナトリウム
０．０３アルブチン ７．０カ
ルボキシビニルポリマー ０．２精製水
残余Ａ、Ｃをそれぞれ均一に溶
解し、ＣにＡを加えて可溶化する。ついでＢを加えたの
ち充填をおこなう。Example 3: Beauty serum (A) Ethanol (95%) 10.
0 polyoxyethylene (20) 1.0 oleyl ether 10.0 methylparaben 0.15-pantothenyl ethyl ether 0.1 (B) Potassium hydroxide 0.1 (C) Glycerin
5.0 dipropylene glycol
10.0 Sodium bisulfite
0.03 Arbutin 7.0 Carboxyvinyl polymer 0.2 Purified water
Dissolve the remaining A and C uniformly, and add A to C to solubilize. Then, after adding B, filling is performed.
実施例４：パック
アルブチン ３．０亜硫酸水素
ナトリウム ０．３ポリビニルアルコール
１３．０（ケン化度９０、重合度２，０
００）
エチルアルコール（９５％）７，０
グリセリン １０．０オリーブ油
３．０酢酸トコフエロール
０．２エチルパラベン
０．２香料 ０．２
精製水 残余各成分を８０
℃で加熱混合したのち充填をおこなう。Example 4: Pack arbutin 3.0 Sodium hydrogen sulfite 0.3 Polyvinyl alcohol 13.0 (Saponification degree 90, Polymerization degree 2.0
00) Ethyl alcohol (95%) 7.0 Glycerin 10.0 Olive oil
3.0 Tocopherol acetate
0.2 ethylparaben
0.2 Fragrance 0.2
Purified water 80% of each remaining ingredient
Filling is performed after heating and mixing at ℃.
実施例５；二層化粧水
アルブチン １．０亜硫酸水素
ナトリウム ０．００１エタノール（９５
％） １０．０ポリオキシエチレン（
２Ｑ）−２−
オクチルドデシルエーテル １．０
クエン酸 ０．０１クエ
ン酸ソーダ ０．０９カオリン
０．２ベンガラ
０．５グリチルリチン酸
モノアンモニウム塩 ０．０５
メチルパラベン ０．２香料
０・１精製水
残余各成分を混合したのち充填を行う。Example 5; Two-layer lotion Arbutin 1.0 Sodium bisulfite 0.001 Ethanol (95
%) 10.0 polyoxyethylene (
2Q)-2- Octyl dodecyl ether 1.0 Citric acid 0.01 Sodium citrate 0.09 Kaolin
0.2 Red Gara
0.5 Glycyrrhizic acid monoammonium salt 0.05 Methylparaben 0.2 Fragrance
0.1 purified water
After mixing the remaining components, filling is performed.
本発明の皮膚外用剤は美白硬化を有するアルブチンの経
時での褐変を防止する硬化に優れた皮膚外用剤である。The skin external preparation of the present invention is a skin external preparation with excellent curing properties that prevents browning of arbutin over time, which has whitening properties.
以下、着色防止硬化試験について記す。The coloring prevention curing test will be described below.
（１）試料
実施例３の美容液の処方で亜硫酸水素ナトリウムの添加
量をＡ（０％） 、Ｂ （０，０１％）、Ｃ（０，０３
％）とした。(1) In the serum formulation of Sample Example 3, the amount of sodium bisulfite added was A (0%), B (0.01%), and C (0.03%).
%).
（２）試験方法
６０℃の恒温層に１力月間放置したのち、３Ｍカラーコ
ンピューター（モデル ５Ｍ−４）（スガ試験機株式会
社）を使用して、△Ｅを測定した。(2) Test method After leaving the sample in a constant temperature bath at 60° C. for one month, ΔE was measured using a 3M color computer (model 5M-4) (Suga Test Instruments Co., Ltd.).
基準値は試作当日に測定した数値を用いた。The reference value used was the value measured on the day of trial production.
（３）試験結果
結果を表１に示す。 表１に示す結果から亜硫酸水素ナ
トリウムが着色防止にきわめて効果があることがわかる
。(3) Test results The results are shown in Table 1. The results shown in Table 1 show that sodium bisulfite is extremely effective in preventing coloration.
Claims (3)
ことを特徴とする皮膚外用剤。(1) A skin external preparation characterized by containing sodium bisulfite and arbutin.
ルブチン１重量部に対して０．０００１〜１重量部であ
る第１項記載の皮膚外用剤。(2) The skin external preparation according to item 1, wherein the content of sodium bisulfite in the skin external preparation is 0.0001 to 1 part by weight per 1 part by weight of arbutin.
ルブチン１重量部に対して０．００１〜０．１重量部で
ある第１項記載の皮膚外用剤。(3) The skin external preparation according to item 1, wherein the content of sodium bisulfite in the skin external preparation is 0.001 to 0.1 part by weight per 1 part by weight of arbutin.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP441887A JPH07121853B2 (en) | 1987-01-12 | 1987-01-12 | Topical skin |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP441887A JPH07121853B2 (en) | 1987-01-12 | 1987-01-12 | Topical skin |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS63174910A true JPS63174910A (en) | 1988-07-19 |
| JPH07121853B2 JPH07121853B2 (en) | 1995-12-25 |
Family
ID=11583736
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP441887A Expired - Fee Related JPH07121853B2 (en) | 1987-01-12 | 1987-01-12 | Topical skin |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH07121853B2 (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1996033722A1 (en) * | 1995-04-27 | 1996-10-31 | Kanebo, Ltd. | External preparation containing emedastine |
| US6497860B1 (en) | 1996-11-04 | 2002-12-24 | Children's Hospital Medical Center | Skin lightening compositions |
| JP2012126684A (en) * | 2010-12-16 | 2012-07-05 | Gekkeikan Sake Co Ltd | Melanin inhibitor and its application |
-
1987
- 1987-01-12 JP JP441887A patent/JPH07121853B2/en not_active Expired - Fee Related
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1996033722A1 (en) * | 1995-04-27 | 1996-10-31 | Kanebo, Ltd. | External preparation containing emedastine |
| US6497860B1 (en) | 1996-11-04 | 2002-12-24 | Children's Hospital Medical Center | Skin lightening compositions |
| JP2012126684A (en) * | 2010-12-16 | 2012-07-05 | Gekkeikan Sake Co Ltd | Melanin inhibitor and its application |
Also Published As
| Publication number | Publication date |
|---|---|
| JPH07121853B2 (en) | 1995-12-25 |
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