JPH0853339A - Dermal agent for external use - Google Patents
Dermal agent for external useInfo
- Publication number
- JPH0853339A JPH0853339A JP21041594A JP21041594A JPH0853339A JP H0853339 A JPH0853339 A JP H0853339A JP 21041594 A JP21041594 A JP 21041594A JP 21041594 A JP21041594 A JP 21041594A JP H0853339 A JPH0853339 A JP H0853339A
- Authority
- JP
- Japan
- Prior art keywords
- fatty acid
- trehalose
- agent
- acid ester
- acne
- 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
Landscapes
- Saccharide Compounds (AREA)
- Cosmetics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【０００１】[0001]
【産業上の利用分野】本発明は、にきびの防止あるいは
その治療に優れた効果を発揮する皮膚外用剤に関する。BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an external preparation for skin which exhibits excellent effects in preventing or treating acne.
【０００２】[0002]
【従来技術及び発明が解決しようとする課題】にきび
（痙瘡）は、皮膚の体裁を醜くし、且つ屡々厄介な症状
を伴い、特に皮脂腺に富む皮膚の領域、顔、頸、背に発
生する。にきびの発生因子はいまだ明確ではないが、皮
脂の過剰排出、皮脂成分異常、毛包脂腺系排出管の閉
塞、さらに毛包脂腺管内の常在細菌の関与などであると
されている。実際には、これらの発生因子が複合的に作
用して、にきびの面皰、丘疹、膿疱等の特徴的な症状が
現れる。にきびは病的な皮脂排出でなく、思春期におけ
る生理的な変調として皮脂排出の急激な増大時期など
に、特にその手入れを怠ると毛包脂腺管内の常在細菌、
即ち嫌気性細菌プロピオニバクテリウム・アクネス（Ｐ
ｒｏｐｉｏｎｉｂａｃｔｅｒｉｕｍ ａｃｎｅｓ）の異
常増殖がおこり、細菌由来の様々な炎症性物質が皮膚に
炎症をもたらし発生することになる。BACKGROUND OF THE INVENTION Acne (spasm) causes ugly skin appearance and is often accompanied by troublesome symptoms, especially on the skin area rich in sebaceous glands, face, neck and back. . Although the factors that cause acne are still unclear, it is thought to be due to excessive excretion of sebum, abnormal sebum components, obstruction of the pilosebaceous duct, and involvement of indigenous bacteria in the pilosebaceous duct. Actually, these development factors act in combination, and characteristic symptoms such as acne comedones, papules, and pustules appear. Acne is not a pathological sebum excretion, but is a physiological change in adolescence, such as during a period of rapid increase in sebum excretion.
That is, the anaerobic bacterium Propionibacterium acnes (P
Ropionobacteria acnes) is abnormally proliferated, and various inflammatory substances derived from bacteria cause inflammation on the skin and are generated.
【０００３】このような背景にあって、にきびの治療剤
としては、エリスロマイシン、テトラサイクリンなどの
抗生物質やイオウ、レゾルシン、サリチル酸などの角質
の剥離溶解剤が用いられている。Against this background, antibiotics such as erythromycin and tetracycline, and keratin exfoliating and dissolving agents such as sulfur, resorcin, and salicylic acid are used as therapeutic agents for acne.
【０００４】ところが、エリスロマイシン、テトラサイ
クリンなどの抗生物質は、抗菌スペクトルが広すぎる
為、プロピオニバクテリウム・アクネス以外の皮膚上の
有用微生物まで殺してしまい、また服用による副作用の
危険も懸念される。一方、イオウ、レゾルシン、サルチ
ル酸などにより期待される角質の剥離作用はたび重なる
塗布によってにきび周囲の皮膚に刺激を与え、治療効果
上の個人差も大きく、充分なものと言えない。このよう
に、既存のにきびの治療剤は十分満足されるものではな
い。However, antibiotics such as erythromycin and tetracycline have an extremely broad antibacterial spectrum, so that useful microorganisms on the skin other than Propionibacterium acnes are killed, and there is a risk of side effects due to administration. On the other hand, the exfoliating action of keratin expected by sulfur, resorcin, salicylic acid, etc. is not sufficient because repeated application causes irritation to the skin around acne, and there are large individual differences in therapeutic effect. Thus, existing acne treatments are not entirely satisfactory.
【０００５】したがって、確実な治療効果を発揮し、か
つ副作用の少ないにきび治療剤、例えばプロピオニバク
テリウム・アクネスのみに対して抗菌作用を示す低刺激
性の抗菌性組成物が望まれていた。そこで本発明の目的
は、殺菌作用によってにきびの防止あるいはその治療に
おいて優れた効果を発揮する皮膚外用剤を提供すること
にある。Therefore, a mild antibacterial composition that exhibits a certain therapeutic effect and has few side effects and has an antibacterial action against only Propionibacterium acnes has been desired. Therefore, it is an object of the present invention to provide a skin external preparation that exhibits excellent effects in preventing or treating acne by its bactericidal action.
【０００６】[0006]
【課題を解決する手段】本発明者は、上記事情に鑑み、
鋭意研究を重ねた結果、トレハロース−６−脂肪酸エス
テルは、安全性が高く、プロピオニバクテリウム・アク
ネスに対して特異的に抗菌活性を示し、さらにこれを配
合する化粧料がにきびに有用であることを見出し、本発
明を完成するに至った。即ち、本発明の請求項１は、ト
レハロース−６−脂肪酸エステルを配合してなる皮膚外
用剤である。また、本発明の請求項２は、トレハロース
−６−脂肪酸エステルを配合することを特徴とする化粧
水である。In view of the above circumstances, the present inventor has
As a result of intensive studies, trehalose-6-fatty acid ester has high safety and shows specific antibacterial activity against Propionibacterium acnes, and cosmetics containing it are useful for acne. This has led to the completion of the present invention. That is, claim 1 of the present invention is an external preparation for skin, which comprises trehalose-6-fatty acid ester. Further, a second aspect of the present invention is a lotion containing trehalose-6-fatty acid ester.
【０００７】本発明の皮膚外用剤又は化粧水に配合する
トレハロース−６−脂肪酸エステルは、トレハロースと
脂肪酸の低級アルキルエステルとのエステル交換によっ
て得ることができる。また、脂肪酸低級エステルとして
は、大豆脂肪、牛脂、ヤシ油、オリーブ油等の天然由来
の脂肪酸と低級アルコールとの通常の方法（ＵＳＰ２８
９３９９０号公報、特開昭３６−２１７１７号公報、Ｕ
ＳＰ３４８０６１６号公報、特開昭５３−６１３０号公
報、ＵＳＰ３９６３６９９号公報）による脂肪酸エステ
ルを用いることもできる。The trehalose-6-fatty acid ester to be incorporated in the external preparation for skin or lotion of the present invention can be obtained by transesterification of trehalose with a lower alkyl ester of a fatty acid. As the fatty acid lower ester, a naturally occurring fatty acid such as soybean fat, beef tallow, coconut oil and olive oil and a lower alcohol can be used in the usual method (USP28
93990, JP-A-36-21717, U
The fatty acid ester according to SP3480616, JP-A-53-6130 and USP3963699) can also be used.
【０００８】この具体的な製造例は、特開平５−１６８
８９３号公報に詳述されている。これらの方法によって
得られた主反応生成物として、本発明のトレハロース−
６−脂肪酸エステルを得ることができる。また、未反応
のトレハロースや副生成物としてトレハロース−６，
６’−脂肪酸ジエステルも生成されるが、これらが混在
した状態でも本発明の効果は維持されるために問題には
ならない。This specific manufacturing example is disclosed in Japanese Patent Laid-Open No. 5-168.
This is described in detail in Japanese Patent No. 893. As the main reaction product obtained by these methods, trehalose of the present invention-
A 6-fatty acid ester can be obtained. In addition, unreacted trehalose and trehalose-6 as a by-product
6'-fatty acid diesters are also produced, but even if they are mixed, the effect of the present invention is maintained, so there is no problem.
【０００９】本発明に使用するトレハロース−６−脂肪
酸エステルはプロピオニバクテリウム・アクネス（アク
ネ菌）に対して特異的に抗菌活性を示すことが本発明で
見出された。It was found in the present invention that the trehalose-6-fatty acid ester used in the present invention shows a specific antibacterial activity against Propionibacterium acnes.
【００１０】本発明のトレハロース−６−脂肪酸エステ
ルの皮膚外用剤又は化粧水への配合量は特に限定されず
広範囲に選択することができるが、実効濃度や経済性を
考慮して、化粧料の総量を基準として０．０２５〜３０
重量％とするのが好ましい。The amount of the trehalose-6-fatty acid ester of the present invention to be added to the external preparation for skin or lotion can be selected within a wide range, but in consideration of effective concentration and economical efficiency, 0.025-30 based on the total amount
It is preferably set to wt%.
【００１１】本発明の皮膚外用剤は、常法に従って、乳
液類、クリーム類、軟膏類、パック類、パウダー類、洗
顔料類、石けん類等の剤型にすることが可能であるが、
その特性上化粧水類が特に望ましい。The external preparation for skin of the present invention can be formulated into emulsions, creams, ointments, packs, powders, face washes, soaps, etc. according to a conventional method.
Lotions are particularly desirable due to their characteristics.
【００１２】本発明の皮膚外用剤又は化粧水には、界面
活性剤、保湿剤、ｐＨ調整剤、増粘剤、色素、香料、殺
菌剤、防腐剤、角質溶解剤、消炎剤、抗酸化剤、紫外線
吸収剤、顔料等を本発明の目的を達成する範囲内で適宜
配合することができる。The external preparation for skin or the lotion of the present invention contains a surfactant, a moisturizer, a pH adjuster, a thickener, a pigment, a fragrance, a bactericide, an antiseptic, a keratolytic agent, an anti-inflammatory agent and an antioxidant. , UV absorbers, pigments and the like can be appropriately blended within a range that achieves the object of the present invention.
【００１３】[0013]
【実施例】以下、実施例および比較例に基づいて本発明
を詳説する。実施例に記載したヒト皮膚貼布試験、にき
び治療効果試験の方法は次の通りである。EXAMPLES The present invention will be described in detail below based on examples and comparative examples. The methods of the human skin patch test and the acne treatment effect test described in Examples are as follows.
【００１４】（１）ヒト皮膚貼布試験 被検者２５名の前腕屈側部皮膚に試料０．０５ｇを直径
１．０ｃｍの円型のリント布のついた貼布試験用絆創膏
を用いて２４時間の閉塞貼布した。次いで、表１の判定
基準に従って、絆創膏除去１時間後、２４時間後の判定
を実施した。判定結果は、反応の強い方の評価を採用
し、被検者２５名のうち評価が（±）以上と判定された
人の数で示した。(1) Human skin patch test Twenty-five subjects were tested on a forearm flexion side skin with 0.05 g of a sample using a bandage patch for patch test with a circular lint cloth having a diameter of 1.0 cm. Timed occlusion patch was applied. Then, according to the criteria of Table 1, the determination was carried out 1 hour and 24 hours after the removal of the bandage. The evaluation results were evaluated by adopting the evaluation with the stronger reaction, and indicated by the number of people among the 25 subjects who were evaluated as (±) or higher.
【００１５】[0015]
【表１】 [Table 1]
【００１６】（２）にきび治療効果試験 顔面ににきび症状を有する被検者２０名の顔面の左部に
対照品（基剤のみの組成物）を、右部には実施例あるい
は比較例の試験品を各々１日に朝夕２回ずつ１ヶ月間連
続塗布した。次いで、にきび症患部の治療効果を表２の
判定基準に従って、半顔比較法にて判定した。判定結果
は、評価点の平均値で示した。(2) Acne treatment effect test A reference product (composition containing only the base) was tested on the left part of the face of 20 subjects with acne symptoms on the face, and a test of the example or comparative example was tested on the right part. Each product was continuously applied twice a day, morning and evening, for 1 month. Then, the therapeutic effect on the affected part of acne was determined by the half-face comparison method according to the criteria of Table 2. The judgment result is shown by the average value of the evaluation points.
【００１７】[0017]
【表２】 [Table 2]
【００１８】実施例１〜７，比較例１〜４ 表３に記載の成分組成において、各種トレハロース−６
−脂肪酸エステルを配合して各々の化粧水を常法により
調整し、ヒト皮膚貼布試験及びにきび治療効果試験を実
施し、その結果を表４に示した。Examples 1 to 7 and Comparative Examples 1 to 4 Various trehalose-6 were prepared in the composition shown in Table 3.
-A fatty acid ester was blended to prepare each lotion by a conventional method, and a human skin patch test and an acne treatment effect test were carried out. The results are shown in Table 4.
【００１９】[0019]
【表３】 [Table 3]
【００２０】[0020]
【表４】 [Table 4]
【００２１】この結果から、トレハロース−６−脂肪酸
エステルを配合した本発明のにきび用化粧水は（実施例
１〜７）は明らかに皮膚刺激もなく、にきび治療効果が
認められた。From these results, the acne lotion of the present invention containing trehalose-6-fatty acid ester (Examples 1 to 7) clearly showed no skin irritation, and the effect of treating acne was recognized.
【００２２】実施例８（乳液） 次の配合組成からなる乳液を調製した。 ステアリン酸 １．５重量％ セチルアルコール １ ワセリン ４ 液状パラフィン ８ ＰＯＥモノオレート（Ｅ．Ｏ．：２０） ２ トリエタノールアミン １ ６−ウンデシノイルトレハロース １ 香料 適量 イオン交換水 残量Example 8 (Emulsion) An emulsion having the following composition was prepared. Stearic acid 1.5% by weight Cetyl alcohol 1 Vaseline 4 Liquid paraffin 8 POE monooleate (EO: 20) 2 Triethanolamine 16-undecinoyltrehalose 1 Perfume proper amount Ion-exchanged water Remaining amount
【００２３】実施例９（クリーム） 次の配合組成からなるクリームを調製した。 ステアリン酸 ７重量％ セチルアルコール ３ ミツロウ ２ オリーブ油 １５ ＰＯＥソルビタンモノオレート（Ｅ．Ｏ．：２０） ２ ６−ラウロイルトレハロース １ イオン交換水 残量Example 9 (Cream) A cream having the following composition was prepared. Stearic acid 7% by weight Cetyl alcohol 3 Beeswax 2 Olive oil 15 POE sorbitan monooleate (EO: 20) 2 6-Lauroyltrehalose 1 Ion-exchanged water Remaining amount
【００２４】実施例１０（洗顔料） 次の配合組成からなる洗顔料を調製した。 ミリスチン酸 １５重量％ ラウリン酸 ８ グリセリン ２０ 水酸化カリウム ５ ６−ミリストイルトレハロース ５ イオン交換水 残量Example 10 (Facial cleanser) A facial cleanser having the following composition was prepared. Myristic acid 15% by weight Lauric acid 8 Glycerin 20 Potassium hydroxide 5 6-Myristoyltrehalose 5 Ion-exchanged water Remaining amount
【００２５】実施例１１（身体洗浄料） 次の配合組成からなる身体洗浄料を調製した。 ヤシ油脂肪酸カリウム ２０重量％ ヤシ油脂肪酸ジエタノールアミド ５ プロピレングリコール ５ トレハロース−６−ヤシ油脂肪酸 ５ 香料 適量 イオン交換水 残量Example 11 (Body wash) A body wash having the following composition was prepared. Palm oil fatty acid potassium 20% by weight Palm oil fatty acid diethanolamide 5 Propylene glycol 5 Trehalose-6-coconut oil fatty acid 5 Fragrance Suitable amount Ion-exchanged water Remaining amount
【００２６】実施例８〜１１の乳液、クリーム、洗顔
料、身体洗浄料はトレハロース脂肪酸エステルを配合し
ないものに比べてにきびの防止あるいはその治療効果に
すぐれていた。The emulsions, creams, facial cleansers and body cleansers of Examples 8 to 11 were superior in the prevention or treatment of acne as compared with those containing no trehalose fatty acid ester.
【００２７】[0027]
【発明の効果】以上記載の如く、本発明が、殺菌作用に
よりにきびの防止あるいはその治療に用いて優れた効果
を発揮する皮膚外用剤を提供することは明らかである。As described above, it is apparent that the present invention provides a skin external preparation that exerts an excellent effect when used for the prevention or treatment of acne due to its bactericidal action.
───────────────────────────────────────────────────── フロントページの続き (51)Int.Cl.6 識別記号 庁内整理番号 ＦＩ 技術表示箇所 Ｃ０７Ｈ 3/04 13/06 ─────────────────────────────────────────────────── ─── Continuation of the front page (51) Int.Cl. 6 Identification code Internal reference number FI technical display area C07H 3/04 13/06
Claims (2)
合することを特徴とする皮膚外用剤。1. An external preparation for skin, comprising trehalose-6-fatty acid ester.
合することを特徴とする化粧水。2. A lotion containing trehalose-6-fatty acid ester.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP21041594A JP3202136B2 (en) | 1994-08-10 | 1994-08-10 | External preparation for skin |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP21041594A JP3202136B2 (en) | 1994-08-10 | 1994-08-10 | External preparation for skin |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH0853339A true JPH0853339A (en) | 1996-02-27 |
| JP3202136B2 JP3202136B2 (en) | 2001-08-27 |
Family
ID=16588942
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP21041594A Expired - Fee Related JP3202136B2 (en) | 1994-08-10 | 1994-08-10 | External preparation for skin |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP3202136B2 (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH1045560A (en) * | 1996-08-06 | 1998-02-17 | Kanebo Ltd | Skin mucous membrane-stimulation emollient |
| JP2007326791A (en) * | 2006-06-06 | 2007-12-20 | Toyobo Co Ltd | Treating agent for acne |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1340486A1 (en) * | 2002-03-01 | 2003-09-03 | Cognis France S.A. | Use of sugar esters |
-
1994
- 1994-08-10 JP JP21041594A patent/JP3202136B2/en not_active Expired - Fee Related
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH1045560A (en) * | 1996-08-06 | 1998-02-17 | Kanebo Ltd | Skin mucous membrane-stimulation emollient |
| JP2007326791A (en) * | 2006-06-06 | 2007-12-20 | Toyobo Co Ltd | Treating agent for acne |
Also Published As
| Publication number | Publication date |
|---|---|
| JP3202136B2 (en) | 2001-08-27 |
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