JPH0358326B2 - - Google Patents

Info

Publication number
JPH0358326B2
JPH0358326B2 JP60050853A JP5085385A JPH0358326B2 JP H0358326 B2 JPH0358326 B2 JP H0358326B2 JP 60050853 A JP60050853 A JP 60050853A JP 5085385 A JP5085385 A JP 5085385A JP H0358326 B2 JPH0358326 B2 JP H0358326B2
Authority
JP
Japan
Prior art keywords
hydroquinone
vitamin
tocopherol
glucose
weight
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
Application number
JP60050853A
Other languages
Japanese (ja)
Other versions
JPS61210010A (en
Inventor
Tomohisa Asahara
Shintaro Abe
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Shiseido Co Ltd
Original Assignee
Shiseido Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Shiseido Co Ltd filed Critical Shiseido Co Ltd
Priority to JP5085385A priority Critical patent/JPS61210010A/en
Publication of JPS61210010A publication Critical patent/JPS61210010A/en
Publication of JPH0358326B2 publication Critical patent/JPH0358326B2/ja
Granted legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60Sugars; Derivatives thereof
    • A61K8/602Glycosides, e.g. rutin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67Vitamins
    • A61K8/676Ascorbic acid, i.e. vitamin C
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67Vitamins
    • A61K8/678Tocopherol, i.e. vitamin E
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/02Preparations for care of the skin for chemically bleaching or whitening the skin

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)
  • Medicinal Preparation (AREA)
  • Cosmetics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Description

【発明の詳細な説明】[Detailed description of the invention]

[産業上の利用分野] 本発明はハイドロキノン−β−D−グルコース
とビタミンE類の一種又は二種以上とを含有して
なる保存安定性に優れた組成物に関し、化粧品、
医薬品、医薬部外品等の分野に有用な皮膚外用剤
を提供することを目的とする。 [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。 このようなしみの治療法にはメラニンの生成を
抑制する物質、たとえばビタミンC、グルタチオ
ン、システインあるいはハイドロキノンなどを配
合した内服や外用製剤が用いられている。 しかしながら、ビタミンC、グルタチオン、シ
ステインは安定性に問題があつたり、異臭が強か
つたりして製剤化が難しい。また、これらは効果
の発現がきわめて緩慢であるという欠点も有して
いる。また、ハイドロキノンは効果は一応認めら
れているものの、感作性があり、一般には使用が
制限されている。 本発明者らは、美白作用を有する物質について
長年の間検討を続けてきたが、特定のハイドロキ
ノンの配糖体が優れた美白作用を有し、安定性、
安全性も良好であることを見いだし、さきに特許
出願を行つた(特願昭58−164815号)。 [発明が解決しようとする問題点] 本発明者らが、その後検討を続けた結果、上記
ハイドロキノンの配糖体は苛酷な条件下で長期に
保存した場合には次第に変色を起こすことが判明
した。化粧品や医薬品などの基剤中に配合した場
合には、その傾向が強い。 本発明者らは上記事情に鑑み、これらハイドロ
キノンの配糖体を安定に系中に配合することを目
的に検討を重ねた結果、ビタミンE類が優れた効
果を発揮することを見いだし、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、本発明はハイドロキノン−β−D−
グルコースと、ハイドロキノン−β−D−グルコ
ース1重量部に対して、0.001〜1重量部のビタ
ミンE類を含有することを特徴とする皮膚外用剤
を提供するものである。 以下、本発明について詳述する。 本発明で用いられるハイドロキノン−β−D−
グルコースは、一般名をアルブチンといい、ハイ
ドロキノンにD−グルコースがβ結合したもので
ある。 ハイドロキノン−β−D−グルコースの配合量
は、皮膚外用剤全量中の0.1〜30重量%、好まし
くは6〜20重量%であり、また6重量%以上の配
合においてビタミンE類の添加効果が顕著であ
る。 本発明の、もう一方の必須構成成分はビタミン
E類である。具体例を挙げるならば、α−トコフ
エロール、β−トコフエロール、γ−トコフエロ
ール、δ−トコフエロール、酢酸トコフエロー
ル、ニコチン酸トコフエロールなどが例示され
る。本発明においては、これらの中から任意の一
種又は二種以上が選ばれて用いられる。これらの
ビタミンE類は天然由来でも合成品でも構わな
い。天然由来のビタミンE(d−α−トコフエロ
ール)を用いる場合は粗ビタミンEでも精製品で
もよいが、トコフエロールとして下記配合量の範
囲内であることが必要なので、トコフエロール含
量が高いことが望ましい。また、トコフエロール
以外に、たとえば、トリグリセライド、レシチ
ン、ビタミンK類、ビタミンA類、ユビキノンな
どが含まれていても構わない。 配合量は、皮膚外用剤全量中の0.01〜2重量%
程度、好ましくは0.05〜0.2重量%であり、ハイ
ドロキノン−β−D−グルコース1重量部に対し
て0.001〜1重量部で顕著な効果が発揮される。 ハイドロキノン−β−D−グルコースとビタミ
ンE類とを配合できる皮膚外用剤は、通常の皮膚
外用剤、たとえば、水溶液系、可溶化系、乳化
系、粉末分散系、水−油2層系、水−油−粉末3
層系などの広い範囲の基剤であり、用途も化粧
水、乳液、クリーム、パツクなどの基礎化粧料、
口紅、フアンデーシヨンなどのメーキヤツプ化粧
料、シヤンプー、リンス、ヘアトニツクなどの頭
髪化粧料などの化粧料のほか、医薬品、医薬部外
品など多岐にわたる。 本発明の皮膚外用剤には必要に応じて、本発明
の効果を損なわない範囲で、保湿剤、増粘剤、油
分、防腐剤、乳化剤、酸化防止剤、金属イオン封
鎖剤、紫外線吸収剤、粉末、薬剤、色剤、香料な
どを配合できる。 [発明の効果] 本発明の皮膚外用剤は美白剤として有用なハイ
ドロキノン−β−D−グルコースを含有し、かつ
経日の変色もない安定性良好な皮膚外用剤であ
る。 [実施例] 次に実施例によつて本発明をさらに詳細に説明
する。配合量は重量%である。 実施例1〜3、比較例1
[Industrial Field of Application] The present invention relates to a composition with excellent storage stability containing hydroquinone-β-D-glucose and one or more kinds of vitamin E, and relates to a composition for use in cosmetics,
The aim is to provide external skin preparations that are useful in the fields of pharmaceuticals and quasi-drugs. [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. To treat such age spots, oral or external preparations containing substances that inhibit melanin production, such as vitamin C, glutathione, cysteine, or hydroquinone, are used. However, vitamin C, glutathione, and cysteine have problems with stability and have strong off-odors, making it difficult to formulate them into formulations. They also have the disadvantage that the onset of their effects is extremely slow. Furthermore, although hydroquinone has been shown to be effective, its use is generally restricted due to its sensitizing properties. The present inventors have been studying substances with whitening effects for many years, and found that a specific hydroquinone glycoside has an excellent whitening effect, has a high stability,
They found that the product was safe and immediately filed a patent application (Japanese Patent Application No. 164815-1981). [Problems to be Solved by the Invention] As a result of subsequent studies by the present inventors, it was found that the above-mentioned hydroquinone glycoside gradually changes color when stored for a long period of time under harsh conditions. . This tendency is strong when it is blended into the base of cosmetics, pharmaceuticals, etc. In view of the above circumstances, the present inventors conducted repeated studies with the aim of stably incorporating these hydroquinone glycosides into the system, and as a result, they discovered that vitamin E exhibits excellent effects, and the present invention I was able to complete it. [Means for solving the problems] That is, the present invention provides hydroquinone-β-D-
The present invention provides an external skin preparation characterized by containing 0.001 to 1 part by weight of vitamin E based on 1 part by weight of glucose and hydroquinone-β-D-glucose. The present invention will be explained in detail below. Hydroquinone-β-D- used in the present invention
Glucose, whose common name is arbutin, is a product in which D-glucose is β-bonded to hydroquinone. The blending amount of hydroquinone-β-D-glucose is 0.1 to 30% by weight, preferably 6 to 20% by weight of the total amount of the skin external preparation, and the effect of adding vitamin E is remarkable when it is blended at 6% by weight or more. It is. Another essential component of the present invention is vitamin E. Specific examples include α-tocopherol, β-tocopherol, γ-tocopherol, δ-tocopherol, tocopherol acetate, and tocopherol nicotinate. In the present invention, one or more of these may be selected and used. These vitamin E types may be of natural origin or synthetic products. When naturally-derived vitamin E (d-α-tocopherol) is used, either crude vitamin E or a purified product may be used, but the tocopherol content must be within the following range, so it is desirable to have a high tocopherol content. In addition to tocopherols, for example, triglycerides, lecithin, vitamins K, vitamins A, ubiquinone, and the like may be contained. The blending amount is 0.01 to 2% by weight of the total amount of the skin external preparation.
The amount is preferably 0.05 to 0.2% by weight, and a remarkable effect is exhibited at 0.001 to 1 part by weight per 1 part by weight of hydroquinone-β-D-glucose. External skin preparations that can contain hydroquinone-β-D-glucose and vitamin E include the usual external skin preparations, such as aqueous solutions, solubilized systems, emulsified systems, powder dispersion systems, water-oil two-layer systems, and water-oil systems. -Oil-Powder 3
It is a wide range of bases such as layered products, and can be used in basic cosmetics such as lotions, milky lotions, creams, and packs.
In addition to cosmetics such as makeup cosmetics such as lipsticks and foundations, and hair cosmetics such as shampoos, conditioners, and hair tonics, our products range from pharmaceuticals to quasi-drugs. The skin external preparation of the present invention may contain, as necessary, a humectant, a thickener, an oil, a preservative, an emulsifier, an antioxidant, a sequestering agent, an ultraviolet absorber, and the like, within a range that does not impair the effects of the present invention. Powders, drugs, colorants, fragrances, etc. can be added. [Effects of the Invention] The external skin preparation of the present invention contains hydroquinone-β-D-glucose, which is useful as a whitening agent, and has good stability without discoloration over time. [Example] Next, the present invention will be explained in more detail with reference to Examples. The blending amount is in weight%. Examples 1 to 3, Comparative Example 1

【表】 表−1において、基剤は下記の化粧水、変色度
合は50℃1カ月保存後のものを下記の基準で判定
した結果である。 (基剤) エタノール 13.0 1,3−ブチレングリコール 10.0 POE(ポリオキシエチレン、以下同じ、15モル)
オレイルエーテル 1.0 エチルパラベン 0.1 香 料 0.05 精製水 残余 (変色度合) ◎ 変色が全くない ○ やや変色した △ かなり変色した × 変色が著しい 実施例 4 ナイトクリーム A セタノール 4.0 ワセリン 7.0 スクワラン 21.0 ステアリン酸モノグリセライド 2.2 POE(20)ソルビタンモノステアレート 2.8 イソプロピルミリステート 6.0 β−トコフエロール 1.0 エチルパラベン 0.3 香 料 0.2 B プロピレングリコール 10.0 1,3−ブチレングリコール 5.0 アルブチン 1.0 精製水 残余 (製法)Aに属する油相部の成分とBに属する
水相部の成分とをそれぞれ別々に加熱溶解し、
油相部を水相部中に混合して乳化し、室温まで
冷却してクリームを得た。 実施例 5 フアンデーシヨン A セタノール 3.5 脱臭ラノリン 4.0 ホホバ油 5.0 ワセリン 2.0 スクワラン 6.0 ステアリン酸モノグリセライド 2.5 酢酸トコフエロール 0.05 POE(60)硬化ヒマシ油 1.5 POE(25)セチルエーテル 1.0 香 料 0.2 B グリセリン 3.0 プロピレングリコール 8.0 調合粉末 12.0 アルブチン 0.5 精製水 残余 (製法)Aに属する油相部の成分を加熱溶解す
る。これとは別に、調合粉末を除くBに属する
水相部の成分を加熱溶解し、これに調合粉末を
分散する。油相部を水相部中に混合して乳化
し、室温まで冷却してフアンデーシヨンクリー
ムを得た。 実施例 6 乳 液 A ステアリン酸 2.5 セタノール 1.5 ワセリン 5.0 流動パラフイン 10.0 酢酸トコフエロール 0.1 POE(10)オレエート 2.0 プロピルパラベン 0.1 香 料 0.2 B ポリエチレングリコール1500 3.0 トリエタノールアミン 1.0 アルブチン 1.0 ハイドロキノン−β−D−アラビノース 0.1 精製水 残余 (製法)実施例4に準じる。 実施例 7 吸水軟こう ワセリン 40.0 ステアリルアルコール 15.0 モクロウ 15.0 POE(10)オレエート 0.25 ステアリン酸モノグリセライド 0.25 α−トコフエロール 1.0 アルブチン 1.0 精製水 残余 (製法)実施例4に準じる。 実施例 8 化粧水 エタノール 25.0 プロピレングリコール 10.0 POE(15)オレイルエーテル 1.0 酢酸トコフエロール 0.2 アルブチン 15.0 クエン酸 0.05 クエン酸ナトリウム 0.1 エチルパラベン 0.1 香 料 0.05 精製水 残余 (製法)実施例1に準じる。 実施例4〜実施例8は、いずれも経日安定性良
好で、使用性、安全性にも優れていた。
[Table] In Table 1, the base is the following lotion, and the degree of discoloration is the result of the lotion after storage at 50°C for 1 month, as determined by the following criteria. (Base) Ethanol 13.0 1,3-butylene glycol 10.0 POE (polyoxyethylene, same below, 15 mol)
Oleyl ether 1.0 Ethylparaben 0.1 Fragrance 0.05 Purified water Residual (degree of discoloration) ◎ No discoloration ○ Slight discoloration △ Considerable discoloration × Example with significant discoloration 4 Night cream A Setanol 4.0 Vaseline 7.0 Squalane 21.0 Stearic acid monoglyceride 2.2 POE (20) Sorbitan monostearate 2.8 Isopropyl myristate 6.0 β-tocopherol 1.0 Ethylparaben 0.3 Fragrance 0.2 B Propylene glycol 10.0 1,3-butylene glycol 5.0 Arbutin 1.0 Purified water Remainder (manufacturing method) Components of the oil phase belonging to A The components of the aqueous phase belonging to B are separately heated and dissolved,
The oil phase was mixed into the water phase and emulsified, and the mixture was cooled to room temperature to obtain a cream. Example 5 Foundation A Setanol 3.5 Deodorized lanolin 4.0 Jojoba oil 5.0 Vaseline 2.0 Squalane 6.0 Stearic acid monoglyceride 2.5 Tocopheryl acetate 0.05 POE (60) Hydrogenated castor oil 1.5 POE (25) Cetyl ether 1.0 Fragrance 0.2 B Glycerin 3.0 Pro Pyrene glycol 8.0 Mixed powder 12.0 Arbutin 0.5 Purified water Heat and dissolve the remaining oil phase components belonging to (manufacturing method) A. Separately, the components of the aqueous phase belonging to B, excluding the blended powder, are heated and dissolved, and the blended powder is dispersed therein. The oil phase was mixed into the water phase, emulsified, and cooled to room temperature to obtain a foundation cream. Example 6 Emulsion A Stearic acid 2.5 Setanol 1.5 Vaseline 5.0 Liquid paraffin 10.0 Tocopheryl acetate 0.1 POE (10) oleate 2.0 Propyl paraben 0.1 Fragrance 0.2 B Polyethylene glycol 1500 3.0 Triethanolamine 1.0 Arbutin 1.0 Hydroquinone-β-D-arabi North 0.1 Purified water Residual (manufacturing method) Same as Example 4. Example 7 Water-absorbing ointment vaseline 40.0 Stearyl alcohol 15.0 Mokuro 15.0 POE (10) oleate 0.25 Stearic acid monoglyceride 0.25 α-tocopherol 1.0 Arbutin 1.0 Purified water Remaining material (manufacturing method) according to Example 4. Example 8 Toner lotion ethanol 25.0 Propylene glycol 10.0 POE (15) oleyl ether 1.0 Tocopherol acetate 0.2 Arbutin 15.0 Citric acid 0.05 Sodium citrate 0.1 Ethylparaben 0.1 Fragrance 0.05 Purified water Residue (manufacturing method) as in Example 1. Examples 4 to 8 all had good stability over time and were excellent in usability and safety.

Claims (1)

【特許請求の範囲】[Claims] 1 ハイドロキノン−β−D−グルコースと、ハ
イドロキノン−β−D−グルコース1重量部に対
して0.001〜1重量部のビタミンE類を含有する
ことを特徴とする皮膚外用剤。
1. A skin external preparation characterized by containing hydroquinone-β-D-glucose and 0.001 to 1 part by weight of vitamin E based on 1 part by weight of hydroquinone-β-D-glucose.
JP5085385A 1985-03-14 1985-03-14 External preparation for skin Granted JPS61210010A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP5085385A JPS61210010A (en) 1985-03-14 1985-03-14 External preparation for skin

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP5085385A JPS61210010A (en) 1985-03-14 1985-03-14 External preparation for skin

Publications (2)

Publication Number Publication Date
JPS61210010A JPS61210010A (en) 1986-09-18
JPH0358326B2 true JPH0358326B2 (en) 1991-09-05

Family

ID=12870277

Family Applications (1)

Application Number Title Priority Date Filing Date
JP5085385A Granted JPS61210010A (en) 1985-03-14 1985-03-14 External preparation for skin

Country Status (1)

Country Link
JP (1) JPS61210010A (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011503205A (en) * 2007-11-14 2011-01-27 オーエムピー インコーポレイテッド Skin treatment composition

Families Citing this family (2)

* Cited by examiner, † Cited by third party
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
JP2001316268A (en) * 2000-02-21 2001-11-13 Ezaki Glico Co Ltd Skin care preparation

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5781410A (en) * 1980-11-11 1982-05-21 Tokitaka Mori Remedy for skin pigmentation
JPS6016906A (en) * 1983-07-07 1985-01-28 Pola Chem Ind Inc External drug for skin

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5781410A (en) * 1980-11-11 1982-05-21 Tokitaka Mori Remedy for skin pigmentation
JPS6016906A (en) * 1983-07-07 1985-01-28 Pola Chem Ind Inc External drug for skin

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011503205A (en) * 2007-11-14 2011-01-27 オーエムピー インコーポレイテッド Skin treatment composition

Also Published As

Publication number Publication date
JPS61210010A (en) 1986-09-18

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