JPH0441122B2 - - Google Patents

Info

Publication number
JPH0441122B2
JPH0441122B2 JP16435683A JP16435683A JPH0441122B2 JP H0441122 B2 JPH0441122 B2 JP H0441122B2 JP 16435683 A JP16435683 A JP 16435683A JP 16435683 A JP16435683 A JP 16435683A JP H0441122 B2 JPH0441122 B2 JP H0441122B2
Authority
JP
Japan
Prior art keywords
skin
present
acne
oxendrone
preparation
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
Application number
JP16435683A
Other languages
Japanese (ja)
Other versions
JPS6056921A (en
Inventor
Haruhiko Ueda
Hidekazu Toyoda
Minoru Fukuda
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
Takeda Pharmaceutical Co Ltd
Original Assignee
Shiseido Co Ltd
Takeda Chemical Industries 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, Takeda Chemical Industries Ltd filed Critical Shiseido Co Ltd
Priority to JP16435683A priority Critical patent/JPS6056921A/en
Priority to AU32434/84A priority patent/AU570998B2/en
Priority to GR80293A priority patent/GR80293B/en
Priority to DE8484110548T priority patent/DE3485408D1/en
Priority to EP19840110548 priority patent/EP0138029B1/en
Priority to CA000462563A priority patent/CA1224152A/en
Priority to ES535711A priority patent/ES8608535A1/en
Priority to US06/648,276 priority patent/US4657901A/en
Publication of JPS6056921A publication Critical patent/JPS6056921A/en
Publication of JPH0441122B2 publication Critical patent/JPH0441122B2/ja
Granted legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol

Landscapes

  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Cosmetics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)

Description

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

本発明はオキセンドロンを含有してなるニキビ
治療用の皮膚外用剤に関する。 ニキビは主として思春期に発現する皮膚疾患で
病名を尋常性座瘡といい、臨床的には“毛嚢脂腺
系を中心に毛孔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つている皮膚
疾患ではあるが一般には、皮脂分泌過剰、毛嚢角
化、毛嚢内細菌が重要な役割をはたしていると考
えられている。従つて、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
一般に多用されている。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つ
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
るものであるが、ホルモン剤がひきおこす副作用
は思春期の男女にとつ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、皮膚常在のニ
キビ菌であるプロピオニバクテリウムアクネス
(Propionibacterium acnes)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。 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、前立腺肥大症治療薬として公知のオキセン
ドロン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つた。 すなわち本発明は、オキセンドロンを含有して
なるニキビ治療用の皮膚外用剤を提供するもので
ある。 以下本発明の構成について詳述する。 本発明に用いられるオキセンドロンは、化学名
を16β−エチル−17β−ヒドロキシ−4−エスト
レン−3−オンといい、白色乃至淡黄白色、無臭
の粉末である。 オキセンドロンの配合量は、本発明の皮膚外用
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、2重量%程度で十
分である。 次に本発明を用いるオキセンドロンの急性毒性
試験結果を示す。
The present invention relates to an external skin preparation for acne treatment containing oxendrone. Acne is a skin disease that primarily occurs during adolescence, and is called acne vulgaris, and is clinically defined as ``chronic inflammatory changes that occur in the pores, mainly in the pilosebaceous system.'' The etiology of acne is currently not clear, and although it is a skin disease in which various factors are intricately intertwined, it is generally believed that excessive sebum secretion, hair follicle keratinization, and bacteria within the hair follicle play important roles. ing. Therefore, creams and ointments containing sebum secretion inhibitors, keratolytic agents, and antibacterial substances are commonly used as external medicines for acne treatment. However, existing anti-acne drugs 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, but the side effects caused by hormones are not desirable for adolescents.
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. Furthermore, antibacterial agents such as hexachlorophene, trichlorocarbanilide, and benzalkonium chloride have extremely high antibacterial activity in vitro against Propionibacterium acnes, an acne bacterium resident on the skin. However, when it is actually used in creams, ointments, etc. to treat acne, in most cases it does not exhibit the expected therapeutic effect. 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 excellent acne treatment effects. The present inventors have discovered that oxendron achieves the above object, and have completed the present invention. That is, the present invention provides an external skin preparation for acne treatment containing oxendrone. The configuration of the present invention will be explained in detail below. The chemical name of oxendrone used in the present invention is 16β-ethyl-17β-hydroxy-4-estren-3-one, and it is a white to pale yellowish-white, odorless powder. The amount of oxendrone blended is approximately 0.001 to 2% by weight in the skin external preparation of the present invention. 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. Next, the results of an acute toxicity test of oxendrone using the present invention will be shown.

【表】 本発明の皮膚外用剤には、上記したオキセンド
ロンのほかにヘキサクロロフエン、フエノール、
ベ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
つても異なるが、油分、界面活性剤、水、エタノ
ール、保湿剤、増粘剤、香料、色素等を本発明の
効果を損わない範囲で適宜配合することができ
る。 本発明の皮膚外用剤の性状は、クリーム、軟
膏、ローシヨ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。 本発明に係る皮膚外用剤はその病状にもよる
が、通常1日に1〜数回、1回に0.1mg〜0.5g程
度皮疹患部に塗布すれば良い。 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。 (使用薬剤) 下記処方、製造法で得たローシヨンタイプの皮
膚外用剤を使用した。 オキセンドロン0.25g、ポリオキシエチレン
(60モル)硬化ヒマシ油2.0g、グリセリン10.0
g、ジプロピレングリコール10.0g、1,3−ブ
チレングリコール5.0g、および5.0gのポリエチ
レングリコール1500を60℃で加熱溶解する。これ
にセチルイソオクタノエート10.0g、スクワラン
5.0gおよびメチルパラベン1.3gを同じく60℃に
加熱溶解したものを添加混合し、ホモミキサー処
理してゲルを作る。次にこのゲルにカルボキシビ
ニルポリマー0.3gおよびヘキサメタリン酸ソー
ダ0.03gを、イオン交換水11.0gに溶解せしめた
ものを徐添加しホモミキサーで分散した後、水酸
化カリウム0.12gをイオン交換水40.0gに溶解し
たものを添加混合し、ホモミキサーで乳化してロ
ーシヨンタイプの皮膚外用剤を得た。 (使用対象および観察期間) 15〜32歳までの男女計20名。 (使用方法) 化粧石鹸を用いて顔面をよく洗浄した後、皮疹
の上にのみ、前記したローシヨンタイプの皮膚外
用剤を1日に1〜3回塗布せしめた。 (観察項目および観察日) 面皰、丘疹、膿疱の3病状について観察し、そ
の個々の所見の程度をそれぞれ高度(4)、中程度(3)
軽度(2)、軽微(1)、なし(0)の5段階に分けて評
価した。またこれらの3病状の程度を総合して尋
常性座瘡の重篤度を、重症、中等症、軽症の3段
階に分けた。経過観察は、治療前、治療1週間
後、2週間後、3週間後、4週間後の各回に行つ
た。 (全般改善度) 使用前に比較して使用薬剤による病状の改善
度、著しく軽快()、かなり軽快()、やや軽
快(+)、不変(±)、増悪(−)の5段階に分け
た。 (有用性) 全般改善度から、きわめて有用()、かなり
有用()、やや有用(+)、無効(±)と判定し
た。 (結果)
[Table] In addition to the above-mentioned oxendrone, the skin external preparation of the present invention includes hexachlorophene, phenol,
Antibacterial agents such as benzalkonium chloride, cetylpyridinium chloride, undecylenic acid, trichlorocarbanilide, and bithionol, drugs and keratolytic agents such as vitamin A acid, photosensitizers, salicylic acid, zinc and its compounds, lactic acid, and properties. Although they may vary, 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. The skin external preparation of the present invention may be in any form as long as it can be applied to the skin, such as a cream, ointment, or lotion. The external preparation for skin according to the present invention may be applied to the skin affected area in an amount of 0.1 mg to 0.5 g at a time, usually once to several times a day, depending on the disease state. Next, the effects of the present invention will be explained in more detail by giving clinical examples. (Drug used) A lotion-type skin external preparation obtained by the following formulation and manufacturing method was used. Oxendrone 0.25g, polyoxyethylene (60mol) hydrogenated castor oil 2.0g, glycerin 10.0
g, 10.0 g of dipropylene glycol, 5.0 g of 1,3-butylene glycol, and 5.0 g of polyethylene glycol 1500 are heated and dissolved at 60°C. Add to this 10.0g of cetyl isooctanoate and squalane.
Add and mix 5.0 g and 1.3 g of methylparaben heated and dissolved at 60°C, and process with a homomixer to form a gel. Next, 0.3g of carboxyvinyl polymer and 0.03g of sodium hexametaphosphate dissolved in 11.0g of ion-exchanged water were gradually added to this gel and dispersed with a homomixer, and then 0.12g of potassium hydroxide was added to 40.0g of ion-exchanged water. The mixture was added and mixed and emulsified using a homomixer to obtain a lotion type skin preparation for external use. (Targets used and observation period) A total of 20 men and women aged 15 to 32. (How to use) After thoroughly washing the face with cosmetic soap, the above-mentioned lotion type skin preparation was applied 1 to 3 times a day only on the skin eruption. (Observation items and observation date) Observations were made for the three pathologies of comedones, papules, and pustules, and the severity of each finding was graded as high (4) and moderate (3).
The evaluation was divided into five levels: mild (2), slight (1), and none (0). In addition, the severity of acne vulgaris was divided into three levels: severe, moderate, and mild by combining the severity of these three conditions. Follow-up observation was performed before treatment, 1 week, 2 weeks, 3 weeks, and 4 weeks after treatment. (Overall improvement level) The degree of improvement in the condition due to the drug used compared to before use, divided into 5 levels: markedly improved (), considerably improved (), somewhat improved (+), unchanged (±), and worsened (-). . (Usefulness) Based on the overall degree of improvement, it was judged as extremely useful (), quite useful (), somewhat useful (+), and ineffective (±). (result)

【表】【table】

【表】 男3名、女17名計20名の臨床テスト結果は+
(やや有用)が2名(10%)、(かなり有用)が
8名(40%)、(きわめて有用)が9名(45
%)、±(無効)が1名(5%)であり、本発明の
皮膚外用剤の効果が立証された。
[Table] The clinical test results for a total of 20 people, 3 males and 17 females, were positive.
(somewhat useful) 2 (10%), (very useful) 8 (40%), (very useful) 9 (45)
%), ± (ineffective) for 1 person (5%), proving the effectiveness of the skin external preparation of the present invention.

Claims (1)

【特許請求の範囲】[Claims] 1 オキセンドロン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 oxendrone.
JP16435683A 1983-09-07 1983-09-07 Dermatic drug for external application Granted JPS6056921A (en)

Priority Applications (8)

Application Number Priority Date Filing Date Title
JP16435683A JPS6056921A (en) 1983-09-07 1983-09-07 Dermatic drug for external application
AU32434/84A AU570998B2 (en) 1983-09-07 1984-08-27 Topical steroid compositions for acne
GR80293A GR80293B (en) 1983-09-07 1984-09-05 Pharmaceutical composition
DE8484110548T DE3485408D1 (en) 1983-09-07 1984-09-05 PHARMACEUTICAL COMPOSITION.
EP19840110548 EP0138029B1 (en) 1983-09-07 1984-09-05 Pharmaceutical composition
CA000462563A CA1224152A (en) 1983-09-07 1984-09-06 Topical treatment of acne
ES535711A ES8608535A1 (en) 1983-09-07 1984-09-06 Pharmaceutical composition.
US06/648,276 US4657901A (en) 1983-09-07 1984-09-07 Pharmaceutical composition

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP16435683A JPS6056921A (en) 1983-09-07 1983-09-07 Dermatic drug for external application

Publications (2)

Publication Number Publication Date
JPS6056921A JPS6056921A (en) 1985-04-02
JPH0441122B2 true JPH0441122B2 (en) 1992-07-07

Family

ID=15791590

Family Applications (1)

Application Number Title Priority Date Filing Date
JP16435683A Granted JPS6056921A (en) 1983-09-07 1983-09-07 Dermatic drug for external application

Country Status (2)

Country Link
JP (1) JPS6056921A (en)
CA (1) CA1224152A (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS62201896A (en) * 1986-02-28 1987-09-05 Shiseido Co Ltd Remedy for hypertrichosis

Also Published As

Publication number Publication date
JPS6056921A (en) 1985-04-02
CA1224152A (en) 1987-07-14

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