JPS6028924A - External preparation for skin - Google Patents
External preparation for skinInfo
- Publication number
- JPS6028924A JPS6028924A JP13834283A JP13834283A JPS6028924A JP S6028924 A JPS6028924 A JP S6028924A JP 13834283 A JP13834283 A JP 13834283A JP 13834283 A JP13834283 A JP 13834283A JP S6028924 A JPS6028924 A JP S6028924A
- Authority
- JP
- Japan
- Prior art keywords
- skin
- external preparation
- androsten
- carboxylic acid
- acid ester
- 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.)
- Pending
Links
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
Abstract
Description
【発明の詳細な説明】
本発明は4−アンドロステン−3−オン−17β−カル
ボン酸ニスデルを含有してなるニキビ治療用の皮膚外用
剤に関する。DETAILED DESCRIPTION OF THE INVENTION The present invention relates to an external skin preparation for treating acne, which contains nisder 4-androsten-3-one-17β-carboxylate.
ニキビは主として思春期に発現する政府疾忠で病名を尋
常性座癒といい、臨床的には“上前脂腺系を中心に名札
に起る慢性の炎症性変化”と定義されている。ニキビの
病因は現在まだ明らかではなく、種々の要因が複雑にか
らみあっている政府疾患ではあるが一般には、皮脂分泌
過剰、名前角化、上前内細菌が重要な役割をはたしてい
ると考えられている。従って、ニキビ治療の外用薬とし
ては、各要因に対応して皮脂分路抑制剤、角質溶解剤お
よび抗菌物質を配合したクリーム、軟膏が一般に多用さ
れている。Acne occurs mainly during adolescence and is called acne vulgaris by the government, and is clinically defined as ``chronic inflammatory changes that occur in the name tag, mainly in the anterior sebaceous gland system.'' The etiology of acne is still unclear, and although it is a disease caused by a complex interplay of various factors, it is generally believed that excessive sebum secretion, hyperkeratosis, and epidermal bacteria play important roles. There is. Therefore, creams and ointments containing sebum shunt inhibitors, keratolytic agents, and antibacterial substances are commonly used as external medicines for treating acne, depending on various factors.
しかし、既存の各種薬剤を配合したニキビ治療薬には種
々の欠点があった。たとえば、皮脂う)渇仰1t/J剤
である女性;1;ルモンは表皮の生長を抑制し、脂腺の
分泌を減少させるものであるが、ホルモン剤がひきおこ
す副作用は思春期の男女にとって好ましいものではない
。又、角質溶解剤の代表例である硫黄および二硫化セレ
ン等の硫黄化合物は、ホルモン様副作用はないが連用す
ることにより皮膚刺激、皮膚のかさつき等を訴えるケー
スが多い。更に、ヘキサクロロフェ/、トリクロロカル
バニリド、およびペンザルコニウムクロリド等の抗菌剤
は、皮病當在の二キビ閑であるプロピオニ−バクテリウ
ムアクネス(Propionibacteriuw a
cncs)に対して、試験管内では極めて高い抗菌力を
発揮しても、実際にクリーム、軟膏等に配合してニキビ
治療に用いると、期待した治愈効果を発揮しないのがほ
とんどである。However, existing anti-acne drugs containing various drugs have various drawbacks. For example, for women who are using a 1t/J drug to increase sebum production; 1; Lumon suppresses the growth of the epidermis and reduces the secretion of sebaceous glands, but the side effects caused by hormonal drugs are favorable for adolescent men and women. isn't it. Further, sulfur and sulfur compounds such as selenium disulfide, which are typical examples of keratolytic agents, do not have hormone-like side effects, but there are many cases where people complain of skin irritation, dry skin, etc. when used repeatedly. In addition, antibacterial agents such as hexachlorophenylene, trichlorocarbanilide, and penzalkonium chloride are effective against the acne-prone skin disease Propionibacterium acnes (Propionibacterium acnes).
Even if they exhibit extremely high antibacterial activity against cncs) in vitro, when they are actually incorporated into creams, ointments, etc. and used to treat acne, most of them do not exhibit the expected therapeutic effect.
本発明者らは上記事情に鑑み、ホルモン様副作用を在さ
ず、皮膚に対して温和で、かつ二・トビ治療効果に優れ
た薬剤を得るべく鋭意研究を重ねた結果、4−アンドロ
ステン−3−オン−17β−カルボン酸エステルがl
!i! [1的を達成することを見いだし、本発明を完
成するに至った。In view of the above circumstances, the present inventors conducted intensive research to obtain a drug that does not have hormone-like side effects, is gentle on the skin, and has an excellent therapeutic effect on 4-androstene. 3-one-17β-carboxylic acid ester is
! i! [We have found that one objective can be achieved and have completed the present invention.
すなわち本発明は4−アンドロステン−3−オ゛ ノー
1フβ−カルボン酸ニスデルを含イ1してなるニキビ治
療用の皮膚外用剤をtq供するものである。That is, the present invention provides an external skin preparation for treating acne, which contains Nisder 4-androstene-3-olylphenol-β-carboxylate.
以下本発明の構成について詳述する。The configuration of the present invention will be explained in detail below.
本発明に用いられる4−アンドロステン−3−オン−1
7β−カルボン酸エステルは、下記描造弐 〇
−OR
を有する化合物で、白色及全淡黄白色、無臭の粉末であ
る。4-androsten-3-one-1 used in the present invention
7β-carboxylic acid ester is a compound having the following drawing 2 〇-OR, and is a white, completely pale yellowish white, odorless powder.
4−アンドロステン−3−オン−17β−カルボン酸エ
ステルの配合量は、本発明の政府外用剤中0.001〜
2重量%程度である。0.001重量%未満では本発明
の効果を発揮しない。配合量が多い程ニキビ治療効果は
大きいが、2N1′r量%程度で十分である。本発明の
皮膚外用剤には、−1−記した4−アンドロステン−3
−オン−17β−カルボン酸エステルのほかにヘキ・す
゛クロロフェン、)罵ノール、ペンザルコニウムクロリ
ド、セチルピリジニウムクロリド、ウンデシレ/酸、ト
リクロロカルバニリド、およびビチオノール等の抗菌剤
、ビタミンA酸、感光素、サリチル酸、亜鉛およびその
化合物、乳酸等の薬剤や角質溶解剤、および性状によっ
ても異なるが、曲性、界面活性剤、水、エタノール、保
湿剤、増粘剤、香料、色素等が本発明の効果を損わない
範囲で適宜配合することができる。The blending amount of 4-androsten-3-one-17β-carboxylic acid ester is 0.001 to 0.001 in the government external preparation of the present invention.
It is about 2% by weight. If the amount is less than 0.001% by weight, the effects of the present invention will not be exhibited. The larger the amount added, the greater the acne treatment effect, but approximately 2N1'r amount % is sufficient. The skin external preparation of the present invention includes -1-4-androstene-3
In addition to -one-17β-carboxylic acid esters, antibacterial agents such as hex-su-chlorophene, )tinol, penzalkonium chloride, cetylpyridinium chloride, undecyle/acid, trichlorocarbanilide, and bithionol, and vitamin A acid , photosensitizers, salicylic acid, zinc and its compounds, drugs such as lactic acid, keratolytic agents, and although they vary depending on the properties, flexibilities, surfactants, water, ethanol, humectants, thickeners, fragrances, pigments, etc. They can be blended as appropriate within a range that does not impair the effects of the present invention.
本発明の皮膚外用剤の性状は、クリーム、軟膏、ローシ
ロン等外皮に適用できる性状のものであればいずれでも
良い。The external preparation for skin of the present invention may be in any form as long as it can be applied to the skin, such as cream, ointment, and lotion.
本発明に係る皮膚外用剤はその症吠にもよるが、通常1
日に1〜数回、1回に0.1■〜0.5g程度皮疹患部
に塗布すれば良い。The topical preparation for skin according to the present invention depends on the symptoms, but usually 1.
Approximately 0.1 to 0.5 g may be applied to the affected area of the skin once to several times a day.
次に臨床例をあげて本発明の効果を更に詳細に説明する
。Next, the effects of the present invention will be explained in more detail by giving clinical examples.
(使用薬剤)
下記処方、製造法で得たrJ−シクンクイプの皮膚外用
剤を使用した。(Drug used) An external skin preparation of rJ-Shikunquip obtained by the following formulation and manufacturing method was used.
4−アンドロステン−3−オン−17β−ノノルボン酸
エステルを0.25g1ポリオキシエチレン(60(ル
)硬化ヒマシ油2.Ogsグリセリン+0.0gs ジ
プロピレングリコール10.0g、1.3−ブチレッグ
+7コール5 、0 g sおよび5.0gのポリニブ
−レンゲIJコール1500を60℃で加熱溶解する。0.25 g of 4-androsten-3-one-17β-nonorboxylic acid ester 1 polyoxyethylene (60 L) hydrogenated castor oil 2.0 gs glycerin + 0.0 gs dipropylene glycol 10.0 g, 1.3-butylene glycol + 7 coles 5, 0 g s and 5.0 g of Polynib-Astragalus IJ Cole 1500 are heated and dissolved at 60°C.
こitζごカル;1τキシビニルポリマー0.3gをイ
]ン交換水43.0−二溶解したものを添加混合し、ホ
モミキ号−一で乳化してV−ジョンタイプの皮病外Jr
l 六lIをi5た。Add and mix 0.3 g of 1τ xyvinyl polymer dissolved in 43.0 g of ion-exchanged water, emulsify with Homo Miki No. 1, and make V-John type skin disease Jr.
l six lI i5.
(使用対象および観察期間) 16〜30歳までの男女計20名。(Subject of use and observation period) A total of 20 men and women between the ages of 16 and 30.
(使用方法)
化粧石船を用いて顔面をよく洗浄した後、Jk疹の土に
のみ、前記した一シqンタイプの皮膚外用剤を1日に1
〜3回塗布せしめtご。(How to use) After thoroughly washing your face with a cosmetic stone boat, apply the above-mentioned one-skin type external skin preparation once a day only to the soil of JK eruption.
~Apply 3 times.
(観察項目および観察口)
面飽、丘疹、膿厄の3症状につ0て観察し、その個々の
所見の程度をそれぞれ高度(4)、rliv度(3)軽
度(2)、軽微(1)、なしく0)の5段階ζ:分()
て評価した。またこれらの3症状の程度を1拉合して尋
′)S性座療の重篤度を、重症、中等j+’+i、雫Y
症の3段階に分けた。経過観察は、治療前、lr;療1
週間後、2週間後、3週間後、4i!!間後の各回に行
った。(Observation items and observation ports) Observations were made for the three symptoms of skin irritation, papules, and impetigo, and the severity of each finding was evaluated as severe (4), rliv (3), mild (2), and minor (1). ), 0), 5 steps ζ: minute ()
It was evaluated. In addition, the severity of these three symptoms is combined to indicate the severity of S-sexual sedentary symptoms: severe, moderate j+'+i, and drop Y.
The disease was divided into three stages. Follow-up was before treatment, lr; treatment 1
Weeks later, 2 weeks later, 3 weeks later, 4i! ! I went to each session after the interval.
(全般改善度)
使用前に比較して使用薬剤による症吠の改善度、著しく
軽快(世)、かなり軽快(H)、やや軽快(+)、不変
(±)、増悪(−)の5段階に分けた。(Overall improvement level) The degree of improvement in barking due to the drug used compared to before use, 5 levels: markedly improved (World), considerably improved (H), somewhat improved (+), unchanged (±), and worsened (-). Divided into.
(有用性)
全般改善度から、きわめてイT Jll (H4)、か
なり有用(+1)、やや有用(+)、無効(±)と判定
した。(Utility) Based on the overall degree of improvement, it was judged as extremely useful (H4), quite useful (+1), somewhat useful (+), and ineffective (±).
(結果)
男2名、女18名at 20名の臨床テスト結果は+(
やや有用)が5名(25%)、廿(がなりイr用)が7
名(35%)、# (きわめてイ1゛用)が7活部X)
、±(無効)が1名(5%)であり、本発明の皮膜外用
剤の効果が立証された。(Results) The clinical test results for 20 people, 2 males and 18 females, were +(
5 people (25%) said it was somewhat useful, and 7 people said it was useful.
Name (35%), # (for very good 1゛) is 7 active club X)
, ± (ineffective) was given by 1 person (5%), proving the effectiveness of the external film preparation of the present invention.
特許出願人 株式会社 資生堂
手続補正書(自発)
昭和58年9月件「1
1、事件の表示
昭和58年持具願第138342号
2、発明の名称
皮膚外用剤
3、補正をする者
4、補正の対象
明細書の発明の詳細な説明の爛
5.補正の内容
(1)明細書第6頁第4行〜5行目「これにカルボキシ
」とあるを、「これにセチル・インオクタノニー110
、Og、スクワラン5.0gおよびメチルパラベン1.
3gを同じり60℃に加熱熔解したものを、添加混合し
ホモミキラー処理してゲルを作る。次ぎにこのゲルにカ
ルボキシ]と補正しまず。Patent Applicant: Shiseido Co., Ltd. Procedural Amendment (Voluntary) September 1988 Case 1 1. Indication of the case: 1981 Provisional Application No. 138342 2. Name of the invention: Skin external preparation 3. Person making the amendment: 4. Detailed description of the invention in the specification to be amended 5. Contents of the amendment (1) On page 6, lines 4 to 5 of the specification, the phrase “carboxy” was replaced with “cetyl inoctanony” 110
, Og, squalane 5.0g and methylparaben 1.
3g of the same was heated and melted at 60°C, added and mixed, and subjected to homomixir treatment to form a gel. Next, this gel is first corrected with carboxy.
(2)明細書第6頁第5行目r 0.3gを・イオン」
とあイ)モミキリ−で分散した後水酸化カリウムO,1
2gを・イメン」と補正しまず。(2) Specification page 6 line 5 r 0.3g ion
Toai) Potassium hydroxide O,1 after dispersing with a fir tree
First, I corrected the 2g by saying, ``Imen''.
(3)明細書第6頁第5行目[イオン交換水43.hJ
とあるを、「・イオン交換水40.OT!Jと補正しま
ず。(3) Specification, page 6, line 5 [ion exchange water 43. hJ
It says, ``-Ion-exchanged water 40.OT!J'' is corrected first.
Claims (1)
ン−17β−カルボン酸エステルを含有することを特徴
とする皮膜外用剤A film external preparation characterized by containing androstene-3-one-17β-carboxylic acid ester according to the following Mizozo formula:
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP13834283A JPS6028924A (en) | 1983-07-28 | 1983-07-28 | External preparation for skin |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP13834283A JPS6028924A (en) | 1983-07-28 | 1983-07-28 | External preparation for skin |
Publications (1)
Publication Number | Publication Date |
---|---|
JPS6028924A true JPS6028924A (en) | 1985-02-14 |
Family
ID=15219673
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP13834283A Pending JPS6028924A (en) | 1983-07-28 | 1983-07-28 | External preparation for skin |
Country Status (1)
Country | Link |
---|---|
JP (1) | JPS6028924A (en) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0660720A4 (en) * | 1992-09-14 | 1996-12-27 | Walter P Smith | Skin-conditioning composition, its application and manufacture. |
-
1983
- 1983-07-28 JP JP13834283A patent/JPS6028924A/en active Pending
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0660720A4 (en) * | 1992-09-14 | 1996-12-27 | Walter P Smith | Skin-conditioning composition, its application and manufacture. |
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