JP2929305B2 - Skin whitening preparation for external use - Google Patents
Skin whitening preparation for external useInfo
- Publication number
- JP2929305B2 JP2929305B2 JP3219990A JP3219990A JP2929305B2 JP 2929305 B2 JP2929305 B2 JP 2929305B2 JP 3219990 A JP3219990 A JP 3219990A JP 3219990 A JP3219990 A JP 3219990A JP 2929305 B2 JP2929305 B2 JP 2929305B2
- Authority
- JP
- Japan
- Prior art keywords
- kojic acid
- skin
- guaiazulene
- inflammation
- external use
- 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
Description
【発明の詳細な説明】 〔産業上の利用分野〕 本発明は、優れた皮膚炎症防止効果、美白効果を有す
る美白用皮膚外用剤に関するものである。DETAILED DESCRIPTION OF THE INVENTION [Industrial Application Field] The present invention relates to a skin whitening external preparation having an excellent skin inflammation prevention effect and a whitening effect.
従来、日焼けによる皮膚の炎症を抑えるために、カラ
ミン等の抗炎症効果を有する薬剤が、また、日焼け後の
色素沈着を抑えるためには、アスコルビン酸、グルタチ
オン等の美白効果を有する薬剤が皮膚外用剤の成分とし
て用いられてきた。Conventionally, drugs having an anti-inflammatory effect such as calamine to suppress inflammation of the skin due to sunburn, and drugs having a whitening effect such as ascorbic acid and glutathione to suppress pigmentation after sunburn are used for external skin. It has been used as a component of agents.
しかしながら、これらの薬剤を含有する皮膚外用剤
は、抗炎症効果、美白効果が弱く、未だ充分満足すべき
ものではなかった。However, skin external preparations containing these agents have weak anti-inflammatory effects and whitening effects, and have not yet been fully satisfactory.
上記実情に鑑み、本発明者らは、鋭意研究を行った結
果、コウジ酸および／またはその誘導体と、特定の抗炎
症剤を配合することにより、前記問題点を解決し、日焼
けによる皮膚の炎症および日焼け後の色素沈着を抑える
効果が相乗的に改善した美白用皮膚外用剤が得られるこ
とを見出し、本発明を完成した。In view of the above circumstances, the present inventors have conducted intensive studies and as a result, the above problems were solved by blending kojic acid and / or a derivative thereof with a specific anti-inflammatory agent, and the inflammation of the skin due to sunburn was solved. Further, the present inventors have found that an external preparation for whitening skin having a synergistically improved effect of suppressing pigmentation after sunburn can be obtained, thereby completing the present invention.
すなわち、本発明は、次の成分（Ａ）および（Ｂ） （Ａ）コウジ酸および／またはコウジ酸誘導体 （Ｂ）グアイアズレンおよび／またはグアイアズレン誘
導体を含有することを特徴とする美白用皮膚外用剤を提
供するものである。That is, the present invention provides a whitening skin external preparation comprising the following components (A) and (B): (A) kojic acid and / or a kojic acid derivative; and (B) guaiazulene and / or a guaiazulene derivative. To provide.
本発明において、必須成分として用いられるコウジ酸
またはその誘導体は、次の一般式（Ｉ） （式中、R1およびR2は、同一または異なっても良く、水
素原子または炭素数３〜22のアシル基またはアルキル基
を示す） で表わされるものである。In the present invention, kojic acid or a derivative thereof used as an essential component is represented by the following general formula (I) (Wherein, R 1 and R 2 may be the same or different and each represent a hydrogen atom or an acyl group or an alkyl group having 3 to 22 carbon atoms).
コウジ酸は、アスペルギルス属、ペニシリウム属、ア
セトバクター属等の微生物などによる発酵生成物から抽
出、精製したものでも、精製工程を省いた粗抽出物のま
まのものでもよく、さらに、合成によって得られるもの
でもよい。Kojic acid may be extracted and purified from fermentation products of microorganisms such as Aspergillus, Penicillium, Acetobacter, etc., or may be a crude extract obtained without a purification step, and may be further obtained by synthesis. It may be something.
また、コウジ酸誘導体としては、上記コウジ酸から合
成されるものが使用でき、そのエステルとしては、例え
ばコウジ酸モノブチレート、コウジ酸モノカプレート、
コウジ酸モノパルミテート、コウジ酸モノステアレー
ト、コウジ酸モノシンナメートまたはコウジ酸モノベン
ゾエートなどのモノエステル；コウジ酸ジブチレート、
コウジ酸ジパルミテート、コウジ酸ジステアレートまた
はコウジ酸ジオレエートなどのジエステル等が挙げられ
る。As the kojic acid derivative, those synthesized from the above-mentioned kojic acid can be used, and as the ester thereof, for example, kojic acid monobutyrate, kojic acid monocaprate,
Monoesters such as kojic acid monopalmitate, kojic acid monostearate, kojic acid monocinnamate or kojic acid monobenzoate; kojic acid dibutyrate;
And diesters such as kojic acid dipalmitate, kojic acid distearate or kojic acid dioleate.
これらコウジ酸またはその誘導体は、１種または２種
以上を組合わせて用いることができる。These kojic acids or derivatives thereof can be used alone or in combination of two or more.
これらのコウジ酸またはその誘導体は、メラニンの生
成機構におけるチロシンをドーパに、そしてドーパをド
ーパキノンに変換する酵素であるチロシナーゼの活性を
抑制する作用があり、その結果メラニンの生成を抑制す
る。配合量は、本発明皮膚外用剤の美白効果および経時
安定性を考慮すれば、皮膚外用剤全量中の0.0001〜５重
量％、特に0.01〜３重量％が好ましい。These kojic acid or a derivative thereof has an action of suppressing the activity of tyrosinase, an enzyme that converts tyrosine into dopa and dopa into dopaquinone in the mechanism of melanin production, and thereby suppresses melanin production. Considering the whitening effect and temporal stability of the external preparation for skin of the present invention, the amount is preferably 0.0001 to 5% by weight, more preferably 0.01 to 3% by weight, based on the total amount of the external preparation for skin.
グアイアズレンまたはその誘導体としてはグアイアズ
レン、グアイアズレンスルホン酸、その塩、そのエステ
ル等が挙げられ、具体的にはグアイアズレン、グアイア
ズレンスルホン酸エチル、グアイアズレンスルホン酸ナ
トリウムなどが例示される。配合量は、皮膚外用剤全量
中0.001〜８重量％、特に0.1〜５重量％が好ましい。Examples of guaiazulene or a derivative thereof include guaiazulene, guaiazulene sulfonic acid, a salt thereof, and an ester thereof, and specific examples thereof include guaiazulene, ethyl guaiazulene sulphonate, sodium guaiazulene sulphonate and the like. The compounding amount is preferably 0.001 to 8% by weight, particularly preferably 0.1 to 5% by weight based on the total amount of the external preparation for skin.
これらグアイアズレンまたはその誘導体は、１種また
は２種以上を組み合わせて用いることができる。These guaiazulene or derivatives thereof can be used alone or in combination of two or more.
さらに、本発明の美白用皮膚外用剤には、前記必須成
分の他、通常の皮膚外用剤に用いられる水性成分、界面
活性剤、油剤、保湿剤、アルコール類、pH調整剤、防腐
剤、色素、酸化防止剤、増粘剤、香料等を必要に応じて
適宜配合することができる。Furthermore, in addition to the essential components, the skin whitening preparation for external use of the present invention includes aqueous components, surfactants, oils, humectants, alcohols, pH adjusters, preservatives, and pigments used in ordinary skin preparations , An antioxidant, a thickener, a fragrance and the like can be appropriately compounded as required.
本発明の美白用皮膚外用剤は、必須成分であるコウジ
酸およびその誘導体の１種または２種以上とグアイアズ
レンおよびその誘導体の１種または２種以上を配合し、
常法に従って製造することができる。そして、乳液、ク
リーム、化粧水、パック、ファンデーション、毛髪化粧
料、洗浄料等の他、分散液状、軟膏状、顆粒状等の医薬
用、医薬部外用または化粧用の製剤とすることができ
る。The skin whitening agent for external use of the present invention comprises one or more of kojic acid and its derivatives as essential components and one or more of guaiazulene and its derivatives,
It can be manufactured according to a conventional method. In addition to emulsions, creams, lotions, packs, foundations, hair cosmetics, cleaning agents, and the like, pharmaceuticals such as dispersed liquids, ointments, granules, and the like can be used as pharmaceutical, quasi-drug, or cosmetic preparations.
次に試験例および実施例を挙げて本発明を更に詳細に
説明するが、本発明はこれらに限定されるものではな
い。Next, the present invention will be described in more detail with reference to Test Examples and Examples, but the present invention is not limited thereto.
試験例 表１に示した薬剤およびエタノールを15重量％含み、
残部が精製水からなる化粧水を調製し、有色モルモット
背部に塗布してその日焼けによる炎症、色素沈着に対す
る効果を調べた。Test Example Contains 15% by weight of the drugs and ethanol shown in Table 1,
A lotion consisting of purified water was prepared for the rest, applied to the back of a colored guinea pig, and examined for its effects on inflammation and pigmentation due to sunburn.
（試験方法） 有色モルモット（各群10匹）の背部を剃毛し、麻酔下
紫外線を照射した。紫外線照射は、東芝（株）製FL20S
・BLBランプとFL20S・E30ランプを３本ずつ同時に照射
し、紫外線量は、4.8×106erg/cm2とした。紫外線照射2
4時間前と照射直後および照射12時間後、24時間後にモ
ルモット背部の４箇所に試料を0.2mlずつよくすりこん
だ。但し、照射前には塗布部位を温水で良く洗浄した。
照射の24時間後に炎症の程度を、そして７日後に色素沈
着の程度を観察し、以下の判定基準で判定した。(Test Method) The backs of colored guinea pigs (10 per group) were shaved and irradiated with ultraviolet light under anesthesia. UV irradiation, FL20S manufactured by Toshiba Corporation
The BLB lamp and the FL20S / E30 lamp were simultaneously irradiated with three lamps at a time, and the amount of ultraviolet rays was 4.8 × 10 6 erg / cm 2 . UV irradiation 2
Four hours before, immediately after irradiation, and 12 hours and 24 hours after irradiation, the sample was thoroughly rubbed into the four parts on the back of the guinea pig by 0.2 ml. However, before irradiation, the application site was thoroughly washed with warm water.
The degree of inflammation was observed 24 hours after irradiation, and the degree of pigmentation was observed 7 days after irradiation.
（判定基準） 炎症についての判定基準（抗炎症効果）： 0:炎症がまったく認められない。(Criteria) Criteria for inflammation (anti-inflammatory effect): 0: No inflammation is observed.
1:ごく僅か炎症が認められる。1: Very slight inflammation is observed.
2:炎症が認められるが、非照射部位との境界は不明瞭。2: Inflammation is observed, but the boundary with the non-irradiated site is unclear.
3:炎症が認められ、非照射部位との境界は鮮明。3: Inflammation was observed, and the boundary with the non-irradiated part was clear.
色素沈着についての判定基準（美白効果）： 0:色素沈着がまったく認められない。Criteria for pigmentation (whitening effect): 0: No pigmentation was observed.
1:ごく僅か色素沈着が認められる。1: Very slight pigmentation is observed.
2:色素沈着が認められるが、非照射部位との境界は不明
瞭。2: Pigmentation is observed, but the boundary with the non-irradiated part is unclear.
3:色素沈着が認められ、非照射部位との境界は鮮明。3: Pigmentation was observed, and the boundary with the non-irradiated part was clear.
（判定） それぞれの評点が、１点以下のモルモットが10匹中 ８匹以上：著効 ６匹以上：有効 ４匹以上：やや有効 ３匹以下：無効 結果を表２に示した。 (Judgment) Guinea pigs with a score of 1 or less 8 or more out of 10: Excellent 6 or more: Effective 4 or more: Somewhat effective 3 or less: Invalid The results are shown in Table 2.
表２の結果から、コウジ酸とグアイアズレンを配合し
た本発明の化粧水は、それぞれを単独で含む化粧水に比
べて抗炎症効果および美白効果が優れていることがわか
る。 From the results in Table 2, it can be seen that the lotion of the present invention containing kojic acid and guaiazulene has superior anti-inflammatory effect and whitening effect as compared to a lotion containing each of them alone.
実施例１ 〔発明の効果〕 以上詳述した如く、本発明の美白用皮膚外用剤は日焼
けによる皮膚の炎症および日焼け後の色素沈着の抑制効
果に優れたものである。Example 1 [Effects of the Invention] As described in detail above, the skin whitening preparation of the present invention is excellent in suppressing skin inflammation due to sunburn and pigmentation after sunburn.
フロントページの続き (56)参考文献 特開 平２−28105（ＪＰ，Ａ) 特開 平１−121207（ＪＰ，Ａ) 特開 平１−96109（ＪＰ，Ａ) 特開 平１−113314（ＪＰ，Ａ) 特開 平１−121206（ＪＰ，Ａ) 特開 昭61−215308（ＪＰ，Ａ) 特開 昭63−280006（ＪＰ，Ａ) 特開 昭63−22506（ＪＰ，Ａ) 特開 昭63−188628（ＪＰ，Ａ) 特開 昭61−68414（ＪＰ，Ａ) (58)調査した分野(Int.Cl.6，ＤＢ名) A61K 7/00 A61K 31/35 A61K 31/015 A61K 31/70 A61K 31/095 ＣＡ（ＳＴＮ)Continuation of the front page (56) References JP-A-2-28105 (JP, A) JP-A-1-121207 (JP, A) JP-A-1-96109 (JP, A) JP-A-1-113314 (JP) JP-A-1-121206 (JP, A) JP-A-61-215308 (JP, A) JP-A-63-280006 (JP, A) JP-A-63-22506 (JP, A) 63-188628 (JP, A) JP-A-61-68414 (JP, A) (58) Fields investigated (Int. Cl. 6 , DB name) A61K 7/00 A61K 31/35 A61K 31/015 A61K 31 / 70 A61K 31/095 CA (STN)
Claims (1)
導体を含有することを特徴とする美白用皮膚外用剤。An external preparation for whitening skin, comprising the following components (A) and (B): (A) kojic acid and / or a kojic acid derivative; and (B) guaiazulene and / or a guaiazulene derivative.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP3219990A JP2929305B2 (en) | 1990-02-13 | 1990-02-13 | Skin whitening preparation for external use |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP3219990A JP2929305B2 (en) | 1990-02-13 | 1990-02-13 | Skin whitening preparation for external use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH03236323A JPH03236323A (en) | 1991-10-22 |
| JP2929305B2 true JP2929305B2 (en) | 1999-08-03 |
Family
ID=12352238
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP3219990A Expired - Lifetime JP2929305B2 (en) | 1990-02-13 | 1990-02-13 | Skin whitening preparation for external use |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP2929305B2 (en) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3119491B2 (en) * | 1991-02-16 | 2000-12-18 | 三省製薬株式会社 | Topical melanin production inhibitor |
| HU209370B (en) * | 1992-06-18 | 1994-05-30 | Fabulon Rg Kozmetikai Kft | Preparatives for treatment and preventing inflammations and other damages of skin caused by bacteria, viruses or reactive free radicals of oxygen, as well as method for making said preparatives |
| JP2000351722A (en) * | 1999-06-07 | 2000-12-19 | Tekunooburu:Kk | Skin cosmetic |
-
1990
- 1990-02-13 JP JP3219990A patent/JP2929305B2/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| JPH03236323A (en) | 1991-10-22 |
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