JPS6056921A - Dermatic drug for external application - Google Patents
Dermatic drug for external applicationInfo
- Publication number
- JPS6056921A JPS6056921A JP16435683A JP16435683A JPS6056921A JP S6056921 A JPS6056921 A JP S6056921A JP 16435683 A JP16435683 A JP 16435683A JP 16435683 A JP16435683 A JP 16435683A JP S6056921 A JPS6056921 A JP S6056921A
- Authority
- JP
- Japan
- Prior art keywords
- skin
- agent
- oxendolone
- present
- external application
- 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
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds 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)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Cosmetics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
【発明の詳細な説明】
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。DETAILED DESCRIPTION OF THE INVENTION The present invention relates to an external skin preparation for treating acne containing oxendrone.
二キビは主として思春期に発現する皮膚疾患で病名を尋
常性座癒といい、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−p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。Acne is a skin disease that mainly 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. Therefore, creams and ointments containing sebum secretion inhibitors, keratolytic agents, and antibacterial substances are commonly used as external medicines for treating acne.
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、ヘキザクロロフェン、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(l
’rop+onibacterium acnas)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, 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 are effective against Propionibacterium acnes (l.
'rop + onibacterium acnas), even though it exhibits extremely high antibacterial activity in vitro.
When actually used in creams, ointments, etc. to treat acne, in most cases they 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仔さ
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(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った。In view of the above circumstances, the present inventors sought to obtain a drug that does not cause hormone-like side effects, is gentle on the skin, and has an excellent acne treatment effect. The inventors have discovered that a known oxendron achieves the above object, and have completed the present invention.
すなわち本発明は、オキセンドロンを含イ「してなるニ
キビ治療用の皮膚外用剤を提供する6のである。That is, the present invention provides an external skin preparation for treating acne, which contains oxendrone.
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オキセントロ/は、化学名ヲ10β
−エチルー17β−ヒドロキシ一番−エストレンー3−
オン といい、白色及至淡黄白色、無臭の粉末である。Oxentro/ used in the present invention has a chemical name of 10β
-Ethyl-17β-Hydroxy Ichiban-estrene-3-
It is a white to pale yellowish-white, odorless powder.
オキセントロ/の配合量は、本発明の皮に1外用剤中0
.001重2iln量%程度テアル。0.001in
Jil %未溝では本発明の効果を発揮しない。配合1
ルが多い程ニキビ治療効果は大きいが、2重lit%程
度で十分である。The compounding amount of Oxentro/ is 0 in 1 external preparation for the skin of the present invention.
.. The amount of 001 weight 2iln is about %. 0.001in
The effect of the present invention is not exhibited when Jil% is not grooved. Formulation 1
Although the acne treatment effect is greater as the number of particles increases, about 2 lit% is sufficient.
次に本発明に用いるオキセンド0/の急性毒性試験結果
を示す。Next, the results of an acute toxicity test for Oxendo 0/ used in the present invention will be shown.
単位:s+g/kg
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、ザリヂル酸、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、油分、界面活性剤、水、エタノ
ール、保湿剤、増結剤、香料、色素等を本発明の効果を
損わない範囲で適褌配合することができる。Unit: s+g/kg In addition to the above-mentioned oxendrone, the skin external preparation of the present invention also contains antibacterial agents such as hexachlorophene, phenol, benzalkonium chloride, cetylpyridinium chloride, undecylenic acid, trichlorocarbanilide, and bithionol. , vitamin A acid, photosensitizer, zarydylic acid, zinc and its compounds, lactic acid and other drugs and keratolytic agents, as well as oils, surfactants, water, ethanol, humectants, thickeners, fragrances, etc. Appropriate amounts of pigments and the like can be added 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、ローン
2)等外皮に適用できる性状のものであれぽいずれでも
良い。The external skin preparation of the present invention may be in any form that can be applied to the skin, such as cream, ointment, and lawn 2).
本発明に係る皮膚外用剤はその圧伏にもよるが、通常1
日に1重数回、1回に0.1−〜0.5g程度皮疹患部
に塗布すれば良い。The skin external preparation according to the present invention usually has a
It is sufficient to apply about 0.1 to 0.5 g at a time to the eruption-affected area 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、製造法で得たローションタイプの皮膚外用剤
を使用した。(Medicine used) A lotion-type skin external preparation obtained by the following formulation and manufacturing method was used.
オキセンドロン0.25g1ポリオキシエチレン(60
エル)硬化ヒマシ油2.0g1グリセリンIO,Og。Oxendron 0.25g 1 polyoxyethylene (60
L) Hydrogenated castor oil 2.0 g 1 Glycerin IO, Og.
ジプロピレングリコール1o、og、 1.3−ゾヂレ
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、スクヮラン5.0
gおよびメチルパラベン1.3gを同じ< 60’C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およびヘキザメタリン酸ソーダ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ョンタイプの皮膚外用
剤を得た。5.0 g of dipropylene glycol 1o, og, 1,3-zoylene glycol, and 5.0 g of polyethylene glycol 1500 are heated and dissolved at 60°C. To this, 10.0 g of cetyl isooctanoate, 5.0 g of squalane
g and 1.3 g of methylparaben heated and dissolved at <60'C are added and mixed, and treated with a homomixer to form a gel. Next, 0.3 g of carboxyvinyl polymer and 0.03 g of sodium hexametaphosphate were added to this gel.
After gradually adding the solution dissolved in 11.0 g of ion-exchanged water and dispersing with a homomixer, 0.12 g of potassium hydroxide was added.
was dissolved in 40.0 g of ion-exchanged water and mixed, and emulsified with a homomixer to obtain a lotion-type skin preparation for external use.
(使用対象および観察期間) 15〜32歳までの男女3120名。(Subject of use and observation period) 3,120 men and women between the ages of 15 and 32.
(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 soap, apply the above 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)
面縮、丘疹、Il[の3症吠について観察し、その個々
の所見の程度をそれぞれ高II)’ (4)、中程度(
3)軽度輯)、軽微(I)、なしく0)の5段階に分け
て評価した。またこれらの3症状の程度を総合して尋常
性座瘉の重篤度を、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週間後の各回に行った。(Observation items and observation ports) Observations were made for the following three symptoms: facets, papules, and Il[, and the severity of each individual finding was graded as high II)' (4) and moderate (4).
3) Evaluation was divided into five stages: slight (slight), slight (I), 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 symptoms. Follow-up observation is before treatment, 1 week after treatment, 2 weeks after treatment, and 3 weeks after treatment.
The test was carried out once a week later and once again after 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(++)、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 (++), somewhat relieved (+), unchanged (±), and worsened (-). divided.
(作用性)
全般改善度から、きわめて有用(* ) 、かなリイJ
用(f)、ややを用(+)、無効(±)と判定した。(Effectiveness) Extremely useful (*) in terms of overall improvement level, Kanarii J
It was judged as useful (f), slightly useful (+), and invalid (±).
(結果)
男3名、女17名計20名の臨床テスト結果は+(やや
作用)が2名(10%)、廿(かなり有用)が8名(4
0%)、惟(きわめて有用)が8名(45%)、±(無
効)が1名(5%)であり、本発明の皮盾外用剤の効果
が立証された。(Results) The clinical test results of a total of 20 people (3 men and 17 women) were 2 (10%) who said + (slightly effective) and 8 (4) who said 廿 (quite useful).
0%), 8 people (45%) said it was extremely useful, and 1 person (5%) said it was ± (ineffective), proving the effectiveness of the topical preparation of the present invention.
特許出願人 株式会社 資生堂 武田薬品工業林式会社 19ワPatent applicant Shiseido Co., Ltd. Takeda Pharmaceutical Forest Company 19 wa
Claims (1)
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 true JPS6056921A (en) | 1985-04-02 |
JPH0441122B2 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) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS62201896A (en) * | 1986-02-28 | 1987-09-05 | Shiseido Co Ltd | Remedy for hypertrichosis |
-
1983
- 1983-09-07 JP JP16435683A patent/JPS6056921A/en active Granted
-
1984
- 1984-09-06 CA CA000462563A patent/CA1224152A/en not_active Expired
Cited By (1)
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 |
---|---|
CA1224152A (en) | 1987-07-14 |
JPH0441122B2 (en) | 1992-07-07 |
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