JPH0242009A - External preparation - Google Patents
External preparationInfo
- Publication number
- JPH0242009A JPH0242009A JP19297188A JP19297188A JPH0242009A JP H0242009 A JPH0242009 A JP H0242009A JP 19297188 A JP19297188 A JP 19297188A JP 19297188 A JP19297188 A JP 19297188A JP H0242009 A JPH0242009 A JP H0242009A
- Authority
- JP
- Japan
- Prior art keywords
- rottlerin
- external preparation
- phase part
- lotion
- kamala
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 238000002360 preparation method Methods 0.000 title claims abstract description 11
- LHHQTXPEHJNOCX-UHFFFAOYSA-N Rottlerin Natural products CC(=O)c1c(O)c(C)c(O)c(Oc2c(O)c3C=CC(C)(C)Cc3c(C(=O)C=Cc4ccccc4)c2O)c1O LHHQTXPEHJNOCX-UHFFFAOYSA-N 0.000 claims abstract description 15
- DEZFNHCVIZBHBI-ZHACJKMWSA-N rottlerin Chemical compound CC(=O)C1=C(O)C(C)=C(O)C(CC=2C(=C(C(=O)\C=C\C=3C=CC=CC=3)C=3OC(C)(C)C=CC=3C=2O)O)=C1O DEZFNHCVIZBHBI-ZHACJKMWSA-N 0.000 claims abstract description 15
- 239000004480 active ingredient Substances 0.000 claims abstract description 14
- 239000000839 emulsion Substances 0.000 abstract description 8
- 239000006071 cream Substances 0.000 abstract description 7
- 210000003491 skin Anatomy 0.000 abstract description 7
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract description 7
- 240000003450 Mallotus philippensis Species 0.000 abstract description 6
- 239000009355 kamala Substances 0.000 abstract description 6
- 239000002537 cosmetic Substances 0.000 abstract description 5
- 239000006210 lotion Substances 0.000 abstract description 5
- 230000000694 effects Effects 0.000 abstract description 4
- 239000002674 ointment Substances 0.000 abstract description 4
- 208000003351 Melanosis Diseases 0.000 abstract description 3
- 229940079593 drug Drugs 0.000 abstract description 3
- 239000003814 drug Substances 0.000 abstract description 3
- 239000000865 liniment Substances 0.000 abstract description 3
- 208000010201 Exanthema Diseases 0.000 abstract description 2
- 235000013399 edible fruits Nutrition 0.000 abstract description 2
- 210000002615 epidermis Anatomy 0.000 abstract description 2
- 201000005884 exanthem Diseases 0.000 abstract description 2
- 206010037844 rash Diseases 0.000 abstract description 2
- 229930184510 Mallotus Natural products 0.000 abstract 1
- 241001060384 Mallotus <angiosperm> Species 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000001747 exhibiting effect Effects 0.000 abstract 1
- 238000000605 extraction Methods 0.000 abstract 1
- 239000000835 fiber Substances 0.000 abstract 1
- 210000004907 gland Anatomy 0.000 abstract 1
- 229940040145 liniment Drugs 0.000 abstract 1
- 238000002156 mixing Methods 0.000 abstract 1
- 238000000746 purification Methods 0.000 abstract 1
- 239000003921 oil Substances 0.000 description 14
- -1 Flavonol compounds Chemical class 0.000 description 10
- 230000008099 melanin synthesis Effects 0.000 description 7
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 6
- 239000012071 phase Substances 0.000 description 6
- 239000008213 purified water Substances 0.000 description 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 4
- 239000008346 aqueous phase Substances 0.000 description 4
- 239000007787 solid Substances 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- REFJWTPEDVJJIY-UHFFFAOYSA-N Quercetin Chemical compound C=1C(O)=CC(O)=C(C(C=2O)=O)C=1OC=2C1=CC=C(O)C(O)=C1 REFJWTPEDVJJIY-UHFFFAOYSA-N 0.000 description 3
- 235000013871 bee wax Nutrition 0.000 description 3
- 239000012166 beeswax Substances 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 239000003205 fragrance Substances 0.000 description 3
- 235000011187 glycerol Nutrition 0.000 description 3
- 230000002401 inhibitory effect Effects 0.000 description 3
- 229940057995 liquid paraffin Drugs 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 3
- 239000003755 preservative agent Substances 0.000 description 3
- 230000002087 whitening effect Effects 0.000 description 3
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- 206010014970 Ephelides Diseases 0.000 description 2
- 239000004166 Lanolin Substances 0.000 description 2
- ZVOLCUVKHLEPEV-UHFFFAOYSA-N Quercetagetin Natural products C1=C(O)C(O)=CC=C1C1=C(O)C(=O)C2=C(O)C(O)=C(O)C=C2O1 ZVOLCUVKHLEPEV-UHFFFAOYSA-N 0.000 description 2
- HWTZYBCRDDUBJY-UHFFFAOYSA-N Rhynchosin Natural products C1=C(O)C(O)=CC=C1C1=C(O)C(=O)C2=CC(O)=C(O)C=C2O1 HWTZYBCRDDUBJY-UHFFFAOYSA-N 0.000 description 2
- 229920002125 Sokalan® Polymers 0.000 description 2
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 2
- XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 description 2
- 229960000541 cetyl alcohol Drugs 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 235000014113 dietary fatty acids Nutrition 0.000 description 2
- 239000010696 ester oil Substances 0.000 description 2
- 239000000194 fatty acid Substances 0.000 description 2
- 229930195729 fatty acid Natural products 0.000 description 2
- XHEFDIBZLJXQHF-UHFFFAOYSA-N fisetin Chemical compound C=1C(O)=CC=C(C(C=2O)=O)C=1OC=2C1=CC=C(O)C(O)=C1 XHEFDIBZLJXQHF-UHFFFAOYSA-N 0.000 description 2
- 210000004209 hair Anatomy 0.000 description 2
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 2
- 239000003906 humectant Substances 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- MWDZOUNAPSSOEL-UHFFFAOYSA-N kaempferol Natural products OC1=C(C(=O)c2cc(O)cc(O)c2O1)c3ccc(O)cc3 MWDZOUNAPSSOEL-UHFFFAOYSA-N 0.000 description 2
- BEJNERDRQOWKJM-UHFFFAOYSA-N kojic acid Chemical compound OCC1=CC(=O)C(O)=CO1 BEJNERDRQOWKJM-UHFFFAOYSA-N 0.000 description 2
- 235000019388 lanolin Nutrition 0.000 description 2
- 229940039717 lanolin Drugs 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 239000012188 paraffin wax Substances 0.000 description 2
- 235000005875 quercetin Nutrition 0.000 description 2
- 229960001285 quercetin Drugs 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
- 239000004094 surface-active agent Substances 0.000 description 2
- 229940099259 vaseline Drugs 0.000 description 2
- 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
- RFVNOJDQRGSOEL-UHFFFAOYSA-N 2-hydroxyethyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCO RFVNOJDQRGSOEL-UHFFFAOYSA-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
- 239000005995 Aluminium silicate Substances 0.000 description 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
- 241000723346 Cinnamomum camphora Species 0.000 description 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
- 241000238631 Hexapoda Species 0.000 description 1
- 239000004909 Moisturizer Substances 0.000 description 1
- IKMDFBPHZNJCSN-UHFFFAOYSA-N Myricetin Chemical compound C=1C(O)=CC(O)=C(C(C=2O)=O)C=1OC=2C1=CC(O)=C(O)C(O)=C1 IKMDFBPHZNJCSN-UHFFFAOYSA-N 0.000 description 1
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 0.000 description 1
- CVBNMWXECPZOLM-UHFFFAOYSA-N Rhamnetin Natural products COc1cc(O)c2C(=O)C(=C(Oc2c1)c3ccc(O)c(O)c3O)O CVBNMWXECPZOLM-UHFFFAOYSA-N 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 235000012211 aluminium silicate Nutrition 0.000 description 1
- 230000000507 anthelmentic effect Effects 0.000 description 1
- 229910000019 calcium carbonate Inorganic materials 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 239000000084 colloidal system Substances 0.000 description 1
- 238000004945 emulsification Methods 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 235000011990 fisetin Nutrition 0.000 description 1
- HVQAJTFOCKOKIN-UHFFFAOYSA-N flavonol Natural products O1C2=CC=CC=C2C(=O)C(O)=C1C1=CC=CC=C1 HVQAJTFOCKOKIN-UHFFFAOYSA-N 0.000 description 1
- 235000011957 flavonols Nutrition 0.000 description 1
- 230000000762 glandular Effects 0.000 description 1
- 125000005456 glyceride group Chemical group 0.000 description 1
- YQEMORVAKMFKLG-UHFFFAOYSA-N glycerine monostearate Natural products CCCCCCCCCCCCCCCCCC(=O)OC(CO)CO YQEMORVAKMFKLG-UHFFFAOYSA-N 0.000 description 1
- SVUQHVRAGMNPLW-UHFFFAOYSA-N glycerol monostearate Natural products CCCCCCCCCCCCCCCCC(=O)OCC(O)CO SVUQHVRAGMNPLW-UHFFFAOYSA-N 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- IPCSVZSSVZVIGE-UHFFFAOYSA-M hexadecanoate Chemical compound CCCCCCCCCCCCCCCC([O-])=O IPCSVZSSVZVIGE-UHFFFAOYSA-M 0.000 description 1
- MJKVTPMWOKAVMS-UHFFFAOYSA-N hydroxy-coumarin Natural products C1=CC=C2OC(=O)C(O)=CC2=C1 MJKVTPMWOKAVMS-UHFFFAOYSA-N 0.000 description 1
- 239000003112 inhibitor Substances 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
- 238000004898 kneading Methods 0.000 description 1
- 229960004705 kojic acid Drugs 0.000 description 1
- WZNJWVWKTVETCG-UHFFFAOYSA-N kojic acid Natural products OC(=O)C(N)CN1C=CC(=O)C(O)=C1 WZNJWVWKTVETCG-UHFFFAOYSA-N 0.000 description 1
- 201000001441 melanoma Diseases 0.000 description 1
- 239000004200 microcrystalline wax Substances 0.000 description 1
- 235000019808 microcrystalline wax Nutrition 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 230000001333 moisturizer Effects 0.000 description 1
- 210000003205 muscle Anatomy 0.000 description 1
- PCOBUQBNVYZTBU-UHFFFAOYSA-N myricetin Natural products OC1=C(O)C(O)=CC(C=2OC3=CC(O)=C(O)C(O)=C3C(=O)C=2)=C1 PCOBUQBNVYZTBU-UHFFFAOYSA-N 0.000 description 1
- 235000007743 myricetin Nutrition 0.000 description 1
- 229940116852 myricetin Drugs 0.000 description 1
- JXTPJDDICSTXJX-UHFFFAOYSA-N n-Triacontane Natural products CCCCCCCCCCCCCCCCCCCCCCCCCCCCCC JXTPJDDICSTXJX-UHFFFAOYSA-N 0.000 description 1
- 210000005036 nerve Anatomy 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
- 239000008363 phosphate buffer Substances 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- JGUZGNYPMHHYRK-UHFFFAOYSA-N rhamnetin Chemical compound C=1C(OC)=CC(O)=C(C(C=2O)=O)C=1OC=2C1=CC=C(O)C(O)=C1 JGUZGNYPMHHYRK-UHFFFAOYSA-N 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 231100000046 skin rash Toxicity 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 229940032094 squalane Drugs 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 239000003760 tallow Substances 0.000 description 1
- 229940098465 tincture Drugs 0.000 description 1
- 239000004408 titanium dioxide Substances 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 239000011787 zinc oxide 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
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/4973—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
- A61K8/498—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom having 6-membered rings or their condensed derivatives, e.g. coumarin
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Birds (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Cosmetics (AREA)
Abstract
Description
【発明の詳細な説明】
〔産業上の利用分野〕
本発明はカマラの成分であるロットレリンを有効成分と
した、シミ、ソバカスなどのメラニン生成による皮膚の
諸現象を防止すると共に、色白効果の優れた外用剤に関
するものである。[Detailed Description of the Invention] [Field of Industrial Application] The present invention uses rottlerin, a component of Kamala, as an active ingredient to prevent various skin phenomena caused by melanin production such as spots and freckles, and has an excellent skin whitening effect. This topic relates to external preparations.
従来、メラニン生成を抑制する物質としては、コウジ酸
、コウジ酸誘導体が知られてる。そして、それらの物質
を有効成分とした色白化粧料も、例えば特公昭56−1
8569号、特開昭56−7710 号、同56−77
76号、同56−79616号公報等に種々開示されて
いる。また、フラボノール系化合物も知られている。例
えば、クエルセチンを有効成分とした化粧料、皮膚塗布
剤としては、特開昭55−92305号、同57−14
517号公報に開示され、クエルセチン脂肪酸エステル
を有効成分としたものとしては、特公昭58−3447
7号公報に開示され、ミリセチン、フィセチン、グチス
セチン、ラムネチンなどを有効成分としたものとしては
、特開昭55−111411 号、同57−35506
号公報に開示されている。また、3−ヒドロキシクロモ
ン系化合物を有効成分としたものとしては、特開昭55
−111410 号、同55−143908 号公報に
それぞれ開示されている。Conventionally, kojic acid and kojic acid derivatives are known as substances that suppress melanin production. Furthermore, skin fairing cosmetics containing these substances as active ingredients were also produced, for example, in
No. 8569, JP-A-56-7710, JP-A No. 56-77
Various disclosures are made in No. 76, No. 56-79616, and the like. Flavonol compounds are also known. For example, cosmetics and skin liniments containing quercetin as an active ingredient include JP-A-55-92305 and JP-A-57-14.
As disclosed in Japanese Patent Publication No. 517 and containing quercetin fatty acid ester as an active ingredient, Japanese Patent Publication No. 58-3447
7, which contains myricetin, fisetin, gutiscetin, rhamnetin, etc. as active ingredients, include JP-A-55-111411 and JP-A-57-35506.
It is disclosed in the publication No. In addition, as an active ingredient of 3-hydroxychromone compound, there is
-111410 and No. 55-143908, respectively.
本発明は安全かつ有効なメラニン生成抑制効果を有する
新たな外用剤を提供することを目的とするものである。The object of the present invention is to provide a new external preparation that has a safe and effective melanin production inhibiting effect.
本発明者は、新たなメラニン生成抑制物質を広く検索、
研究を重ねたところ、本発明者が先にメラニン生成抑制
物質として見出したカマラチンキ(特開昭63−291
3 号公報参照)の成分であるロットレリンが優れたメ
ラニン生成抑制作用を有することを見出し本発明を完成
した。The present inventor conducted a wide search for new melanin production inhibitors,
After repeated research, the present inventor discovered Kamala tincture (Japanese Patent Application Laid-Open No. 63-291
The present invention was completed based on the discovery that rottlerin, a component of the product (see Publication No. 3), has an excellent melanin production inhibiting effect.
本発明はロットレリンを有効成分とする外用剤である。The present invention is an external preparation containing rottlerin as an active ingredient.
本発明のロットレリンは下記構造式を有する化合物であ
る。Rottlerin of the present invention is a compound having the following structural formula.
この化合物はクスノキガシワの果実の表皮に生じた腺毛
及び束毛であるカマラを原料として抽出精製した公知の
物質である。This compound is a known substance extracted and purified from Kamala, which is the glandular hairs and bundles of hairs produced on the epidermis of the camphor tree fruit.
原料のカマラは虫体の運動神経及び筋を麻痺させること
により駆虫効果を現し、また瀉下作用を有することが知
られている。Kamala, the raw material, is known to have an anthelmintic effect by paralyzing the motor nerves and muscles of the insect body, and also to have a cathartic effect.
本発明の外用剤はクリーム、化粧水、パック等の化粧料
の他、乳剤、ローション剤、リニメント剤等の外用に用
いられる医薬部外品を含む意味に用いられる。The external preparations of the present invention include cosmetics such as creams, lotions, and packs, as well as quasi-drugs used for external use such as emulsions, lotions, and liniments.
本発明の外用剤は、有効成分であるロットレリンを、化
粧料の場合は5〜0.001%(重量)、好ましくは1
〜0.01%(重量)、医薬部外品の場合は、10〜0
.001%(重量)、好ましくは1〜0.01%(重M
)含有する。The external preparation of the present invention contains rottlerin as an active ingredient, in the case of cosmetics, 5 to 0.001% (by weight), preferably 1% (by weight).
~0.01% (weight), 10-0 for quasi-drugs
.. 001% (by weight), preferably 1-0.01% (by weight)
)contains.
外用剤に製剤化する場合、クリーム又は軟膏においては
、精製水に親水性成分例えば、グリセリン、ソルビット
などの保湿剤を添加して水相部とし、油相部はミツロウ
、パラフィン、マイクロクリスタリンワックス、セレシ
ン、高級脂肪酸、硬化油などの固形油分、ワセリン、ラ
ノリン、グリセリドなどの半固形油分、それにククワラ
ン、流動パラフィン、各種エステル油などの液状油分に
防腐剤、界面活性剤などの油成分を添加して調製する。When formulating into external preparations, creams or ointments, hydrophilic ingredients such as humectants such as glycerin and sorbitol are added to purified water to form the aqueous phase, and the oil phase consists of beeswax, paraffin, microcrystalline wax, etc. Oil components such as preservatives and surfactants are added to solid oils such as ceresin, higher fatty acids, and hydrogenated oils, semi-solid oils such as vaseline, lanolin, and glycerides, and liquid oils such as cuqualane, liquid paraffin, and various ester oils. Prepare.
このようにして得られた水相部を加温して、緩やかに攪
拌しつつ同温度に加温された油相部を徐々に添加し乳化
してクリーム又は軟膏とする一般のクリーム又は軟膏の
製造において、油相部に有効成分であるロットレリンを
加えてクリーム又は軟膏とする。A general cream or ointment is prepared by heating the aqueous phase obtained in this way and gradually adding the oil phase heated to the same temperature while stirring gently to emulsify it. During production, the active ingredient rottlerin is added to the oil phase to form a cream or ointment.
乳剤においては、精製水にグリセリンなどの保湿剤、酸
又はアルカリのpH調整剤などを加え、加温混合してエ
タノールを加え水相部とし、ミツロウ パラフィンなど
の固形油分、ワセリン、ラノリンなどの半固形油分、ス
クワラン、流動パラフィン、各種エステル油などの液状
油分に、防腐剤、界面活性剤などの油性成分を添加して
混合加熱し油相部とし、油相部を水相部に加えて予備乳
化を行い、これにカルボキシビニルポリマー、カルボキ
シメチルセルロースなどの保護コロイド剤を加え、ホモ
ミキサーで均一に乳化して乳剤とする一般の乳剤の製造
において、油相部に有効成分であるロットレリンを加え
て乳剤とする。In the case of emulsions, humectants such as glycerin, acidic or alkaline pH adjusters, etc. are added to purified water, heated and mixed, ethanol is added to form the aqueous phase, and solid oils such as beeswax and paraffin, semi-containing substances such as vaseline and lanolin are added. Oily components such as preservatives and surfactants are added to liquid oils such as solid oils, squalane, liquid paraffin, and various ester oils, mixed and heated to form an oil phase, and the oil phase is added to the aqueous phase to form a reserve. In the production of general emulsions, in which emulsification is performed, a protective colloid such as carboxyvinyl polymer or carboxymethyl cellulose is added to the emulsion, and the emulsion is homogeneously emulsified using a homomixer, rottlerin, an active ingredient, is added to the oil phase. Make it into an emulsion.
パンク剤においては、精製水にグリセリンなどの保湿剤
、ポリビニルアルコール、ビーガムなどの皮膜剤などを
加えて膨潤させ、これに必要があればカオリン、タルク
、酸化亜鉛などの粉末を加え、香料、防腐剤などを溶解
したエタノールを加えてペースト状となるまで混練する
一般のパック剤の製造において、有効成分であるロット
レリンを加えてパック剤とする。For puncture agents, moisturizers such as glycerin, film agents such as polyvinyl alcohol, and vegum are added to purified water to swell it, and if necessary, powders such as kaolin, talc, and zinc oxide are added to add fragrance and preservatives. In the production of general packs, which involve adding ethanol in which ingredients have been dissolved and kneading the mixture until it becomes a paste, rottlerin, an active ingredient, is added to form a pack.
次に本発明の実施例を挙げる。Next, examples of the present invention will be described.
例1 クリーム
ロフトレリン 0.1%ポリオキシエ
チレンステアリルエーテル2.0%
ポリオキシエチレンセチルエーテル
2.0%
ミツロウ 6.0にセタノール
6.0%イソプロビルパルミテー
) 10.0%流動パラフィン 30
.0%ポリエチレングリコールモノステアレート1.0
%
バラオキシ安息酸メチル 0.2%精製水で全量
を100 とする。Example 1 Cream loftrelin 0.1% polyoxyethylene stearyl ether 2.0% polyoxyethylene cetyl ether 2.0% beeswax 6.0% cetanol 6.0% isoprobyl palmitate) 10.0% liquid paraffin 30
.. 0% polyethylene glycol monostearate 1.0
% Methyl roseoxybenzoate 0.2% Make the total volume to 100 with purified water.
例2 乳剤
ロットレリン 0.01%自己乳化型
グリセロールモノステアレート0.5%
ポリオキシエチレンセヂルエーテル
2.0%
MCステアリン酸 2.0%セタノール
1.5%イソプロピルミリステー)
10.0%バラオキシ安息呑酸メチル 0.
2%香料 微量
精製水で全量を100 とする。Example 2 Emulsion Rottlerin 0.01% Self-emulsifying glycerol monostearate 0.5% Polyoxyethylene cedyl ether 2.0% MC stearic acid 2.0% Cetanol
1.5% isopropyl myristate)
10.0% Methyl roseoxybenzoate 0.
2% fragrance Make the total volume to 100% with a small amount of purified water.
例3 バック剤
ロットレリン 1.0%パラオキシ
安安息醋酸メチル 0.08%カルボキシビニルポリ
マー 1.0%炭酸カルシウム 0
.6%二酸化チタン 0.02%香料
微量精製水で全量を10
(l とする。Example 3 Backing agent Rottlerin 1.0% Methyl paraoxybenzoate 0.08% Carboxyvinyl polymer 1.0% Calcium carbonate 0
.. 6% titanium dioxide 0.02% fragrance A small amount of purified water makes the total amount 10%
(Let it be l.
なお、本実施例の%は重量%である。Note that % in this example is % by weight.
本発明の有効成分であるロソトレリンのメラニン生成抑
制作用について下記の試験により明らかにする。The melanin production inhibiting effect of losotorelin, the active ingredient of the present invention, will be clarified by the following test.
試験例
Bi6細胞のメラニン生成試験
マウスメラノーマ由来B16細胞4X10’ 個を10
%牛脂児血清10m1を含んだイーグルMε;4培地に
懸濁し、25cm”培養用ルー瓶にて5%C02存在下
37℃で培養する。0日目及び3日目にロソトレリンを
それぞれ0,25μ!J/ 1 jI!、0.50 μ
M/1β、1.0μ:A/1β含む培地で交換し、5日
間培養する。細胞を0、8W/V食塩を含有するリン酸
緩衝液(pH7,2)で洗浄し、後トリプシン及びBD
TA含有溶液を使用して剥離し、濾過により細胞を回収
した。濾紙上に回収された細胞はデンシトメーターによ
り500nm における反射光度(黒色度)を求めた。Test Example Melanin production test of Bi6 cells 4 x 10' mouse melanoma-derived B16 cells were
Suspended in Eagle Mε;4 medium containing 10 ml of % tallow serum and cultured at 37°C in the presence of 5% CO2 in a 25 cm” culture bottle. !J/ 1 jI!, 0.50 μ
M/1β, 1.0 μ: Replace with medium containing A/1β and culture for 5 days. Cells were washed with phosphate buffer (pH 7.2) containing 0.8 W/V saline, then trypsinized and BD
Cells were harvested by detachment using a TA-containing solution and filtration. The reflected light intensity (blackness) at 500 nm of the cells collected on the filter paper was determined using a densitometer.
試験結果は下記表1の通りであった。The test results were as shown in Table 1 below.
表 1
:変化なし +:やや薄い ++:明瞭に薄い +十十
:非常に薄い
以上の結果ロットレリン添加濃度に依存し、細胞の白色
化が認められた。Table 1: No change +: Slightly thin ++: Clearly thin +10: Very thin As a result, whitening of cells was observed depending on the concentration of rottlerin added.
本発明の外用剤は肌あれ、皮膚のカブレなどの障害を起
こすことなく安全に使用でき、皮膚の色白効果、シミ、
ソバカス等を防止する効果を有する極めて有用な発明で
ある。The topical preparation of the present invention can be safely used without causing any problems such as rough skin or skin rash, and has a whitening effect on the skin, preventing spots and
This is an extremely useful invention that has the effect of preventing freckles and the like.
Claims (1)
用剤。1. An external preparation characterized by containing rottlerin as an active ingredient.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP19297188A JP2610310B2 (en) | 1988-08-01 | 1988-08-01 | External preparation |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP19297188A JP2610310B2 (en) | 1988-08-01 | 1988-08-01 | External preparation |
Publications (2)
Publication Number | Publication Date |
---|---|
JPH0242009A true JPH0242009A (en) | 1990-02-13 |
JP2610310B2 JP2610310B2 (en) | 1997-05-14 |
Family
ID=16300091
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP19297188A Expired - Lifetime JP2610310B2 (en) | 1988-08-01 | 1988-08-01 | External preparation |
Country Status (1)
Country | Link |
---|---|
JP (1) | JP2610310B2 (en) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102988190A (en) * | 2012-12-28 | 2013-03-27 | 广州市白云区新东方日用化工品厂 | Whitening combination and application thereof |
-
1988
- 1988-08-01 JP JP19297188A patent/JP2610310B2/en not_active Expired - Lifetime
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102988190A (en) * | 2012-12-28 | 2013-03-27 | 广州市白云区新东方日用化工品厂 | Whitening combination and application thereof |
Also Published As
Publication number | Publication date |
---|---|
JP2610310B2 (en) | 1997-05-14 |
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