JPS6028925A - External preparation for skin - Google Patents
External preparation for skinInfo
- Publication number
- JPS6028925A JPS6028925A JP13833883A JP13833883A JPS6028925A JP S6028925 A JPS6028925 A JP S6028925A JP 13833883 A JP13833883 A JP 13833883A JP 13833883 A JP13833883 A JP 13833883A JP S6028925 A JPS6028925 A JP S6028925A
- Authority
- JP
- Japan
- Prior art keywords
- skin
- external preparation
- testrosterone
- haloacetate
- 17beta
- 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】
本発明はテストステロン−１７β−ハロケン化アセテー
トを含有してなる二キビ治療用の皮膜外用剤に閃する。DETAILED DESCRIPTION OF THE INVENTION The present invention is directed to an external preparation for acne treatment containing testosterone-17β-halokenated acetate.
ニキビは主として思春期に発現する皮ｆｙｒＡｉＬ＋で
病名を尋常性産膜といい、臨床的にはパ名前脂綜系を中
心に石化に起る慢性の炎症性変化師と定義されている。Acne is a skin fyrAiL+ disease that mainly occurs during puberty, and is called perinatal membrane vulgaris, and is clinically defined as a chronic inflammatory change that occurs with mineralization mainly in the panacea.
ニキビの病因は現在まだ明らかではな（、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、名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Ｐｌｔｔ分泌抑制剤
、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ｂ）る。The etiology of acne is currently not clear (although it is a disease caused by a complex interplay of various factors, in general,
Excessive sebum secretion, cornification, and skin bacteria are thought to play important roles. Therefore, creams and ointments containing skin PLT secretion inhibitors, keratolytic agents, and antibacterial substances are often 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ｄ１療薬には
種々の欠点があった。たとえば、皮脂分泌抑制剤である
女性ホルモンは表皮の生長を抑制し、脂腺の分泌を減少
させるものである力（、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
７１溶解剤の代表例である硫黄および二硫化・ヒレ−７
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【Ｉロフエン、トリクロロカル
バニリド、およびベンザルコニウムクロリド等の抗菌剤
は、政府常在のニキビ菌であるプロピオニバクテリ言ン
ムアクネス（Ｐｒｏｐ＋ｏｎＩｂａｃｔｅｒ！ｕｍ ａ
ｃｎｅｓ）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
治療に川１．）ると、期待した油虫効果を発揮しないの
がほとんどである。However, existing acne d1 treatments containing various drugs have various drawbacks. For example, female hormones, which are sebum secretion inhibitors, suppress the growth of the epidermis and reduce the secretion of sebaceous glands. Sulfur and disulfide, which are typical examples of 71 dissolving agents, are 71
Although sulfur compounds such as these do not have hormone-like side effects, there are many cases where people complain of skin irritation, dry skin, etc. when used repeatedly. In addition, antibacterial agents such as hexachloride, trichlorocarbanilide, and benzalkonium chloride are effective against Prop+ on Ibacterium acnes, an endemic bacteria.
Although it shows extremely high antibacterial activity against Cnes) in vitro, it is actually used in creams, ointments, etc. to treat acne. ), most of them do not have the expected effect on oil bugs.
本発明者らは上記事情に鑑み、ホルモン様副作用を有さ
ず、皮膚に対して温和で、かつニキ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、テストステロン
−１フβ−ハロゲン化アセテートが上記目的を達成する
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 acne treatment effect. The present inventors have discovered that modified acetate achieves the above object, and have completed the present invention.
すなわち本発明は、テストステ「１７−１７β−ハロゲ
ン化アセデートを含（１’ Ｉ、てなるニキビ治療用の
皮膚外用剤を提供するものである。That is, the present invention provides an external skin preparation for the treatment of acne containing Testoste "17-17β-halogenated acedate (1'I).
り下水発明の構成についてｉｉＹ述する。The structure of the sewage invention will be described below.
本発明に用いられるブストステＩＩン〜１７β−ハロゲ
ン化アセテートは、下記（１力造式を有ず２化合物で、
白色及全淡黄白色、熱良の粉末である。Bustostein II-17β-halogenated acetate used in the present invention is as follows (two compounds without one formula,
It is a white or pale yellowish-white powder with good heat.
テストステロン−１７β−ハロゲン化アセテートの配合
量は、本発明の皮膚外用剤中０．００１〜２ｒｒＬ量％
程度である。０．００１重計％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
、２重量％程度で十分である。本発明の皮膚外用剤には
、上記したテストステロン−１７β−ハロゲン化アセデ
ートのほかにへキザクロロフェン、フェノール、ベンザ
ルコニウムクロリド、セヂルピリジニウノ、り１１リド
、つ／デシレン酸、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、ビクミ／Ａ酸、感光素、サリ
チル酸、亜鉛およびその化合物、乳酸等の薬剤埴角質溶
解剤、および性状によっても異なるが、油分、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 testosterone-17β-halogenated acetate is 0.001-2rrL amount% in the skin external preparation of the present invention.
That's about it. If the amount is less than 0.001% by weight, the effects of the present invention will not be exhibited. The larger the amount, the greater the acne treatment effect, but about 2% by weight is sufficient. In addition to the above-mentioned testosterone-17β-halogenated acedate, the skin external preparation of the present invention also contains hexachlorophene, phenol, benzalkonium chloride, cedylpyridinium, di-11-lide, di/decylenic acid, and trichlorocarbamate. Antibacterial agents such as Nilide' and bithionol, Bicumi/A acid, photosensitizers, salicylic acid, zinc and its compounds, lactic acid and other pharmaceutical agents, keratolytic agents, and oils, surfactants, water, Ethanol, humectants, thickeners, fragrances, pigments, and the like can be appropriately blended within the range that does not impair the effects of the present invention.
本発明の皮膚外用剤の性状は、クリーノ１、軟菩、ロー
シコン等外皮に適用できる性υ、のらのであればいずれ
でも良い。The external preparation for skin of the present invention may have any form as long as it can be applied to the skin, such as Kurino 1, Soft Bodhisattva, and Rhoshicon.
本発明に係る皮膚外用剤はその症状にもよるか、通常１
日に１〜数回、１回に０．１ｓｇ〜０．５ｇｆ″ｊ。The topical preparation for skin according to the present invention depends on the symptoms, but usually 1.
Once to several times a day, 0.1sg to 0.5gf''j at a time.
度皮疹患部に塗布すれば良い。It can be applied to the affected area of skin eruption.
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、製造法で得たローン９フタイプの皮膚外用剤
を使用した。(Drug used) A skin external preparation of Lawn 9F type obtained by the following formulation and manufacturing method was used.
テストステロン−１フβ−ハ１１ゲ／化アセデー） ０
．２５ｇ１ポリオキシエチレン（６０Ｉル）硬化ヒマシ
浦２．Ｏｇ、グリセリ／ ＩＯ，Ｏｇｌ ジブ【１ピレ
ングリコール１０−０ｇ１Ｌ３−ブチレングリコール５
．Ｏｇ、および５．０ｇのポリエチレングリ：１−ル１
５００を（ｉ０℃で加熱溶解する。これにカルボ４・ジ
ビニル、１！リマ−０，３ｇをイオン交換水４３．０ｇ
に溶解したものを添加混合し１，１．モミキザーで乳化
して【１−シ。Testosterone-1 beta-ha11ge/chemical acide) 0
．． 25g1 polyoxyethylene (60Il) hardened castor 2. Og, glycerin/IO, Ogl Jib [1 pyrene glycol 10-0g1L3-butylene glycol 5
．． Og, and 5.0 g of polyethylene glycol: 1-1
500 (i0℃). To this, add 0.3 g of Carbo 4 Divinyl and 1! Limer and 43.0 g of ion-exchanged water.
Add and mix what was dissolved in 1, 1. Emulsify with a rice mixer [1-shi].
７タイプの皮膚外用剤を得た。Seven types of skin preparations for external use were obtained.
（使用対象および観察期間） １５〜３２歳までの男女８１２０名。(Subject of use and observation period) 8,120 men and women between the ages of 15 and 32.
（使用方法）
化粧石ｍを用いて顔面をよく洗浄した後、皮疹の上にの
み、前記したローションタイプの皮膚外用剤を１日に１
〜３回塗布せしめた。(How to use) After thoroughly washing your face with cosmetic stone M, apply the above-mentioned lotion-type skin preparation once a day only on the skin eruption.
It was applied ~3 times.
（観察項目および観察口）
面飽、丘疹、膿厄の３症状について観察し、その個々の
所見の程度をそれぞれ高度（４）、”Ｉ’ Ｉ’Ｌ度（
３）軽度（２）、軽ｅ （１）、なしく０）の５段階に
分番ノで評価した。またこれらの３症状の程度を総合し
て尋常性座癒の重角度を、重症、中等症、軽症の３段階
に分けた。経過観察は、治療前、ｌｉ；療１週間後、２
週間後、３週間後、４週間後の各回に行った。(Observation items and observation points) Observe the three symptoms of skin irritation, papules, and impetigo, and rate the severity of each finding as high (4) and "I"I'L degree (
3) Evaluation was done on a five-point scale: mild (2), light e (1), and none (0). In addition, the degree of severity of sitting vulgaris was divided into three levels: severe, moderate, and mild, based on the severity of these three symptoms. Follow-up observation was before treatment, li; 1 week after treatment, 2
The test was carried out after 1 week, 3 weeks, and 4 weeks.
（全般改善度）
使用前に比較して使用薬剤による症状の改善度、著しく
軽快（＠）、かなり軽快（什）、やや軽快（＋）、不変
（±）、増悪（−）の５段階に分けた。(Overall improvement level) The degree of improvement in symptoms due to the drug used compared to before use, in 5 levels: markedly relieved (@), considerably relieved (什), somewhat relieved (+), unchanged (±), and worsened (-). divided.
（イ１゛用性）
全般改善度から、きわめてず１川（＠）、４ノ）なリ用
１川（什）、やや有用（十）、無効（±）と判定した。(1) Usability Based on the overall degree of improvement, it was judged to be extremely useful (@), 4) useful (1), somewhat useful (10), and ineffective (±).
（結果）
男１名、女１９名計２０名の臨床テスト結果ζよ→−（
やや有用）が６名（３０％）、＋（かなリ用１川）カ（
７名（３５％）、＠（きわめて有用）が５名（２５％）
、±（無効）が２名（１０％）であり、本発明の皮ｒ７
外川剤の効果が立証された。(Results) Clinical test results for 20 people (1 male and 19 females)→-(
6 people (30%) said that it was somewhat useful, and + (1 river for Kanari)
7 people (35%), 5 people (25%) said @ (very useful)
, ± (invalid) was 2 people (10%), and the skin of the present invention r7
The effectiveness of Togawa drug was proven.
特許出願人 株式会社 資生堂
手Ｔｒｈ ？市Ｊ−１三招：（１）−発）昭和５）（年
９月１牛１１
特ｆｌ庁長官若杉和人殿 、１′・
１、事件の表示
昭和５８年持具願第１３８３１ｉ１号
２、発明の名称
皮屑り１川剤
３、補正をする宵
）
４、？市ｊ［の文１象
明細書の発明の詳細な説明の欄
５、補正の内容
（１）明ｋＰｄ書第５頁第１４行目「これにカルボキシ
」とあるを、「これにセチルイソメククノＩ −ｔｌｏ
、０＋＋、スフソラン５．Ｏｇおよびメチルパラヘン１
．３ｇを同しく６０℃に加熱熔解したものを、添加混合
しボモミ；ト乃−処理してゲルを作る。次ぎにこのケル
にカルボキシ」とン重重しまず。Patent applicant Shiseido Co., Ltd. Trh? City J-1 Three Invitations: (1)-Showa 5) (September 1 Ushi 11 Mr. Kazuto Wakasugi, Director General of the Special FL Agency, 1'. 1, Indication of the Incident, 1981, Petition No. 13831i1, 2) , Name of the invention Skin shavings 1 River agent 3, Correction night) 4.? Detailed explanation of the invention column 5 in the description of the city jノI -tlo
,0++,Sufsolan5. Og and methylparahen 1
．． 3 g of the same mixture was heated and melted at 60°C, added and mixed, and treated to form a gel. Next, I thought, 'Carboxy to this Kel.'
（２）明細書第５頁第１５行目ＩＯ，３ｇをイオン」と
あるを、ｒｏ、３ｇおよびヘキザメタリン酸ソーダ０．
（１３ｇを・イ雅
オン交換水１１．０ｇに熔解せしめたものを幹添加し、
ポでミキサーで分散した後水酸化カリウム０．１２ｇを
・イ」ン」と補正しまず。(2) On page 5, line 15 of the specification, IO, 3g is replaced with RO, 3g and sodium hexametaphosphate 0.
(13g was dissolved in 11.0g of Igaon exchange water and added to the stem.
After dispersing with a mixer in a pot, add 0.12 g of potassium hydroxide.
（３）明細書第５頁第１５行目［イオン交換水４３．０
ｇＪとあるを、［イオン交換水４０．０ｇＪと補正しま
す。(3) Specification page 5 line 15 [ion exchange water 43.0
Correct gJ to 40.0gJ of ion exchange water.
Claims (1)
することを特徴とする皮膜外用剤External film preparation characterized by containing testosterone-17β-halogenated acedate
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP13833883A JPS6028925A (en) | 1983-07-28 | 1983-07-28 | External preparation for skin |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP13833883A JPS6028925A (en) | 1983-07-28 | 1983-07-28 | External preparation for skin |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPS6028925A true JPS6028925A (en) | 1985-02-14 |
Family
ID=15219574
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP13833883A Pending JPS6028925A (en) | 1983-07-28 | 1983-07-28 | External preparation for skin |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS6028925A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5910308A (en) * | 1982-03-15 | 1984-01-19 | Terumo Corp | Manufacture of semipermeable film |
-
1983
- 1983-07-28 JP JP13833883A patent/JPS6028925A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5910308A (en) * | 1982-03-15 | 1984-01-19 | Terumo Corp | Manufacture of semipermeable film |
| JPS6256765B2 (en) * | 1982-03-15 | 1987-11-27 | Terumo Corp |
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