JPS611615A - External drug for athlete's foot - Google Patents
External drug for athlete's footInfo
- Publication number
- JPS611615A JPS611615A JP59121586A JP12158684A JPS611615A JP S611615 A JPS611615 A JP S611615A JP 59121586 A JP59121586 A JP 59121586A JP 12158684 A JP12158684 A JP 12158684A JP S611615 A JPS611615 A JP S611615A
- Authority
- JP
- Japan
- Prior art keywords
- urea
- athlete
- drug
- foot
- trichloro
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/17—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/04—Sulfur, selenium or tellurium; Compounds thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Inorganic Chemistry (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【発明の詳細な説明】
〔産業上の利用分野〕
この発明は、皮膚疾患の一種である水虫（汗庖状白癖）
の治療薬、特にその外用薬に関し。[Detailed Description of the Invention] [Industrial Field of Application] This invention is applicable to the treatment of athlete's foot (alcoholism), which is a type of skin disease.
regarding therapeutic drugs, especially its topical drugs.
医薬品製剤分野で利用されるものである。It is used in the pharmaceutical formulation field.
水虫は、′白癖菌が角層の厚い部分・１例えば足の裏や
手の平で発育して病変を生じる皮膚の病気である。Athlete's foot is a skin disease in which the fungus Leukoderma grows in thick parts of the stratum corneum, such as the soles of the feet and the palms of the hands, causing lesions.
従来、水虫外用薬としては多くの種類の薬剤が市販され
ているが、いずれも試験管内で白癖菌の発育を阻止する
作用があり、どれを使用し仝
ても薬の効力にそれほど差はない。但し、水虫は中々完
治しにくい皮膚病であり、治癒］〜たように見えても菌
は表皮角質層の深部等に生存していることが往々にして
あり、夏季になって再び発育してきたり、薬の塗布を止
めた後しばらくして発育してきたりして水虫が再発する
といったことがしばしば起こる。このように水虫が治り
にくいのは、菌が薬剤の浸透しにくい角質層中に寄生し
ていること、白解菌のうちでも薬剤に比較的抵抗力の強
い菌種による場合が多いこと等の理由による。このため
、実験室的薬剤効果がそのまま臨床的治療効果に結びつ
かないことが間々あり、一般に水虫は完治しにくい皮膚
病の１つであるとされている。そして治療法としては、
原因菌である白癖菌の種類を証明しその菌種に最も有効
な薬剤を選定し、それを根気よく塗布し続けるとともに
、常に手足を清潔に保ち、指間部等の乾燥に心掛けるこ
とが最良とされている。Conventionally, there are many types of external medicines for athlete's foot on the market, but all of them have the effect of inhibiting the growth of white fungus in vitro, and there is not much difference in the efficacy of the medicine no matter which one is used. do not have. However, athlete's foot is a skin disease that is difficult to cure completely, and even if it appears to be cured, the bacteria often survives deep within the stratum corneum of the epidermis, and may grow again in the summer. It often happens that athlete's foot grows again some time after the medication has been stopped. The reason why athlete's foot is so difficult to cure is that the bacteria are parasitic in the stratum corneum, which is difficult for drugs to penetrate, and that the fungi are often caused by bacterial species that are relatively resistant to drugs. Depends on the reason. For this reason, laboratory drug effects often do not directly translate into clinical therapeutic effects, and athlete's foot is generally considered to be one of the skin diseases that is difficult to completely cure. And as a treatment,
It is important to prove the type of fungus that is the causative agent, select the most effective drug for that type of bacteria, continue to apply it patiently, and keep your hands and feet clean at all times to avoid dryness between your fingers. considered to be the best.
従来の水虫治療薬は、白癖菌の種類によっては殆んど効
き目がなかったり、あるいは実験室における試験では顕
著な薬効を示しても、実際に人体に施蘂した場合、それ
ほどの治療効果を挙げ得ないことがある。そして一旦治
癒したように見えても後日再発することが少なからず起
こり、またその治療には長期間にわたる患者の非常な忍
耐を必要とする。Conventional drugs for treating athlete's foot may have little or no effect on certain types of fungi, or even if they show remarkable efficacy in laboratory tests, they do not have much therapeutic effect when applied to the human body. There are some things that cannot be mentioned. Even if the disease appears to be cured, it often occurs later, and its treatment requires great patience from the patient over a long period of time.
この発明は、従来の水虫治療薬では満足し切れなかった
上記問題点を一挙に解決し、菌種にかかわらず、かつ短
期間で、極めて良好な臨床的治療効果を挙げ、しかも後
日再発するようなことなく水虫を完治することができる
水虫外用４を提供するためになされた、
〔問題点を解決するための手段〕
上記課題を解決する技術的手段として第１の発明では、
少くとも抗真菌剤の１種である２、４゜４’−１−ＩＪ
クロロ−２／−ヒドロキン ジフェニルエーテルと、角
質軟化剤である尿素とを親水軟膏基剤もしくはエタノー
ル水溶液に混和することによって水虫外用薬を調剤した
。This invention solves all of the above-mentioned problems that were unsatisfactory with conventional drugs for treating athlete's foot, achieves extremely good clinical therapeutic effects in a short period of time, regardless of bacterial species, and prevents recurrence at a later date. [Means for Solving the Problems] The first invention provides a technical means for solving the above-mentioned problems, which has been made to provide an external use for athlete's foot 4 that can completely cure athlete's foot without any problems.
2,4゜4'-1-IJ, which is at least one type of antifungal agent
A topical drug for athlete's foot was prepared by mixing chloro-2/-hydroquine diphenyl ether and urea, a keratin softener, into a hydrophilic ointment base or an aqueous ethanol solution.
ここで２．４．４’ −トリクロロ−２／−ヒドロキシ
ジフェニルエーテルは、スイスのチバガイギー社によっ
て開発された抗菌剤であり（商標名：イルガサンＤＰ３
００）、 実用上毒性が全くなく。Here, 2.4.4'-trichloro-2/-hydroxydiphenyl ether is an antibacterial agent developed by Ciba Geigy of Switzerland (trade name: Irgasan DP3).
00), has no practical toxicity.
皮膚毒性試験によって皮膚刺戟も感作も起こすことがな
い薬品で、皮膚への適合性に優れ、主に手指の殺菌消毒
剤として利用されている。（「医薬ジャーナルＪ Ａ
２６３０．日本医事新報、Ｐ１６３〜１６５等参照）こ
の２．４．４’−１−ジクロロ−２１−ヒドロキン ジ
フェニルエーテルの上記水虫外用薬中における含有割合
は、好ましくは０．２〜２．０重量％（もしくは０．２
〜２．０ Ｖ’／Ｑ％）特には１．０重量％（もしくは
１．０％・％）程度である。It is a drug that does not cause skin irritation or sensitization in skin toxicity tests, has excellent skin compatibility, and is mainly used as a disinfectant for hands and fingers. (“Pharmaceutical Journal JA
2630. The content of this 2.4.4'-1-dichloro-21-hydroquine diphenyl ether in the above external medicine for athlete's foot is preferably 0.2 to 2.0% by weight (or 0.2
~2.0 V'/Q%), particularly about 1.0% by weight (or 1.0%.%).
つぎに尿素は、極めて毒性の低いン全な角質軟化剤であ
り、上記゛水虫外用薬中における含有割合は、好ましく
は５〜４０重［Ｈもしくは５〜４０・；Ｗ／ル％）、特
には１０重量％（もしくは１０％％）程度である。Next, urea is a complete keratin softener with extremely low toxicity, and its content in the external medicine for athlete's foot is preferably 5 to 40% [H or 5 to 40%], especially is about 10% by weight (or 10%%).
１だ第２の発明に係る水虫外用薬は、上述しり２，４．
４Ｊ−トリクロロ−２１−ヒドロキン ジフェニルエー
テル及び尿素の他に、安定剤として少量の硫酸を含有し
てなるものである。1. The external medicine for athlete's foot according to the second invention is based on the above-mentioned items 2, 4.
4J-Trichloro-21-hydroquine In addition to diphenyl ether and urea, it contains a small amount of sulfuric acid as a stabilizer.
この発明に係る水虫外用薬においては、その組成成分の
１つである尿素により皮膚の水分保持能を高めて角質層
を膨潤軟化させ、角質層深部への薬剤の浸透を助けると
ともに、角質を溶解剥離（７，角質層自体の厚さを薄く
して薬剤の経皮吸収を増進させ、抗真菌剤によって角質
層中に寄生している白解菌を死滅させる。そして広範囲
の抗真菌スペクトルをもち、抗真菌作用の優れた２、４
．４’−トリクロロ−２／−′ヒドロキンジフェニルエ
ーテルにより９種々雑多の、捷た抵抗力の強い菌種であ
っても完全に死滅させる。In the topical medicine for athlete's foot according to the present invention, urea, which is one of its constituent ingredients, increases the water retention capacity of the skin, swells and softens the stratum corneum, helps the drug penetrate deep into the stratum corneum, and dissolves the stratum corneum. Peeling (7) It reduces the thickness of the stratum corneum itself to increase transdermal absorption of the drug, and uses an antifungal agent to kill the parasitic white bacteria in the stratum corneum.It also has a broad antifungal spectrum. , excellent antifungal effects 2, 4
．． 4'-trichloro-2/-'hydroquine diphenyl ether completely kills 9 different types of bacteria, even those with strong resistance.
また第２の発明に係る水虫外用薬においては。Further, in the external medicine for athlete's foot according to the second invention.
少量の硫酸を配合することによって９組成成分である２
、４．４’−ｈリクロロー２１−ヒドロキンジフェニル
エーテル及び尿素の両者を共に安定化させ、患部に薬剤
を塗布した際における薬効を長持ちさせる。By blending a small amount of sulfuric acid, 9 composition components 2
, 4.4'-hlichloro-21-hydroquine diphenyl ether and urea are both stabilized to prolong the efficacy of the drug when applied to the affected area.
以下、この発明の実施例、並びＫその実施例に係る水虫
外用薬の抗真菌性能に関し行なった比較試験の結果等に
ついて説明する。Examples of the present invention, as well as the results of comparative tests conducted regarding the antifungal performance of the external medicine for athlete's foot according to the examples, will be described below.
最初に、雑多な真菌に対する薬剤の有効率（抗真菌スペ
クトル）、及び平均有効阻止指数（抗真菌活性）を求め
る方法について第１図及び第２図を参照しながら説明す
る。First, a method for determining the effectiveness rate (antifungal spectrum) and average effective inhibition index (antifungal activity) of a drug against various fungi will be explained with reference to FIGS. 1 and 2.
まずシャーレ（１）内部に寒天を敷き、これを真菌用培
地（２）として、真菌を均等に接種する。次に直径６屡
の濾紙（３）に一定量の薬剤を浸み込ませた後郭燥させ
たものを真菌用培地（２）の表面に載置する。これによ
って濾紙（３）中に含浸された薬剤が寒天中に拡散して
ゆき、その薬剤が菌種に対する発育阻止作用を有してい
れば１週間培養後には、濾紙（３）と真菌の発育域部（
３）との間に真菌が全く発育しない阻止環帯［Ｆ］）が
形成される。First, agar is spread inside a Petri dish (1), and this is used as a fungal medium (2) to evenly inoculate the fungus. Next, a filter paper (3) with a diameter of 6 square meters is impregnated with a certain amount of the drug, and then dried and placed on the surface of the fungal culture medium (2). As a result, the drug impregnated in the filter paper (3) is diffused into the agar, and if the drug has a growth inhibiting effect on the fungal species, after one week of culture, the filter paper (3) and the fungus will grow. Area (
3), an inhibition ring [F]) is formed in which no fungi can grow at all.
この阻止環帯■の幅（１）を計測し９表−１に基づいて
それぞれの場合の有効単位を決定する。Measure the width (1) of this blocking ring zone (1) and determine the effective unit in each case based on Table 9-1.
表＝１
そして次式により、各種薬剤の有効率及び平均有効阻止
指数を算出する。Table=1 Then, the effectiveness rate and average effective inhibition index of various drugs are calculated using the following formula.
上式に基づいて各種薬剤の有効率（抗真菌スペクトル）
及び平均有効阻止指数（抗真菌活性）を求めた結果を第
３図及び表−２に示す。この発明に仔るものとしては、
２，４．４／ −トリクロロ−２′−ヒドロキン
ジフェニルエーテル１．０ｐト尿素ｓｏｙもしくはＩＯ
，Ｏｐとを５０％エタノール水溶液１００−に溶解させ
たもの、２例（図表中において、それぞれＩＲ（１，ｏ
％）＋ＵＢ、（ｓ％）、ＩＩ？（１，０％１−Ｈ］ＲＮ
ｏ％）として表示）について抗真菌性能を示した。また
参考として、 ２，４．４’−トリクロロ−２／−ヒ
ドロキシ ジフェニルエーテルをそれぞれ１０Ｗ／Ｖ・
鴨、 ｏ、ｓ ”／、％及び０．２５．Ｖ１／ｖ゛％、
５０％エタノール水溶液に含有させたもの（図表中にお
いて、それぞれＩＢ、（１，０％）、ＩＴ（（０，５％
）、ＩＲ，（０，２５％）として表示）についても抗真
菌作用を見た。さらに比較対照するため。Effectiveness rate (antifungal spectrum) of various drugs based on the above formula
The results of determining the average effective inhibition index (antifungal activity) are shown in Figure 3 and Table 2. As a result of this invention,
2,4.4/ -trichloro-2'-hydroquine
diphenyl ether 1.0p tourea soy or IO
, Op dissolved in 50% ethanol aqueous solution 100-, two examples (in the diagram, IR(1, o
%)+UB, (s%), II? (1,0%1-H]RN
(expressed as o%)). For reference, 2,4,4'-trichloro-2/-hydroxy diphenyl ether was used at 10 W/V.
Duck, o,s''/,% and 0.25.V1/v゛%,
Contained in a 50% ethanol aqueous solution (in the diagram, IB, (1,0%), IT ((0,5%), respectively)
), IR, expressed as (0,25%)) also showed antifungal activity. To further compare and contrast.
市販されている水虫外用ｉ９種について抗真菌性能を調
べた。The antifungal performance of nine commercially available i types for external use for athlete's foot was investigated.
第３図及び上表からも分かるように、この発明に係る薬
剤は、市販水虫治療薬と比較しても極めて高い有効率を
示す。すなわち２．４．４／ −トリクロロ−２１ヒド
ロキシ ジフェニルエーテルと尿素とを含有した薬剤は
、広範囲の抗真菌スペクトルをもち、この点において市
販薬よりも優れている。またこの発明に係る薬剤は、市
販Ａ薬、Ｂ−ＪＲ（いずれもイミダゾール系薬剤）と同
等の高い抗真菌活性が認められた。尚、２．４゜４’−
ｔ−リクロロー２−−ヒドロキン ジフェニルて抗真菌
活性も高くなる。但し１図表中には示さなかったが、ａ
度が２．０いワ９％を越えると濃度上昇に伴う抗真菌活
性の変化はみられなくなる。また、２，４．４’−トリ
クロロ−２／−ヒドロキン ジフェニルエーテｗ’ｉｒ
単独で用いるよりは。As can be seen from FIG. 3 and the table above, the drug according to the present invention exhibits an extremely high efficacy rate compared to commercially available drugs for treating athlete's foot. Thus, the drug containing 2.4.4/-trichloro-21 hydroxy diphenyl ether and urea has a broad antifungal spectrum and is superior to commercially available drugs in this respect. Furthermore, the drug according to the present invention was found to have high antifungal activity equivalent to commercially available drugs A and B-JR (both imidazole drugs). In addition, 2.4°4'-
The antifungal activity of t-lichloro-2-hydroquine diphenyl is also increased. However, although not shown in Figure 1, a
When the degree exceeds 2.0% and 9%, no change in antifungal activity is observed as the concentration increases. Also, 2,4,4'-trichloro-2/-hydroquine diphenyl ether w'ir
Rather than using it alone.
尿素併用剤の方が抗真菌活性が高い。The antifungal activity is higher when combined with urea.
尿素の濃度に関しては、１０Ｗ／ｙ％と２０ヅνるとに
おける皮膚の角質溶解剥離作用についての有意差は認め
られなかったが２５°η％と１０ ’ ”／、−％とに
おいては、臨床的見地からみて１０’、ヅＹ・％の濃度
の方が優位であった。Concerning the concentration of urea, no significant difference was observed in the skin keratolytic exfoliation effect between 10 W/y% and 20㎜%, but clinical From an objective point of view, the concentration of 10', 2% was superior.
この発明に係る水虫外用藁の用法の１例を簡単に記すと
、 ２．４．４’−１−リクロロー２１−ヒドロキン
ジフェニルエーテル１．０ Ｐ ト）尿素１０．ＯＳ
’とを親水軟膏基剤８９．０ｐに混練し、これを１日１
回、風呂上りにタオル等でふやけた表皮をこすり取って
患部を清浄にした後、塗布する。An example of how to use the straw for external use for athlete's foot according to the present invention will be briefly described as follows: 2.4.4'-1-lichloro-21-hydroquine diphenyl ether 1.0 P g) Urea 10. OS
' and into 89.0p of hydrophilic ointment base and apply this once a day.
After taking a bath, rub off the soggy epidermis with a towel, clean the affected area, and then apply.
この操作を、軽症の易合で４〜５日間、かなりの重症の
場合でも２〜３週間程度続けることによって水虫は完治
する。Athlete's foot can be completely cured by continuing this procedure for 4 to 5 days in mild cases and 2 to 3 weeks in very severe cases.
尚、上記の処方は皮膚への適用例であるが。Note that the above prescription is an example of application to the skin.
爪白癖に対する処方の１例を示すと、 ２．４．４’
−トリクロロ−２１−ヒドロキン ジフェニルエーテル
１，０免尿素４０．０ｐ、精製ラノリン２４０Ｆ。An example of a prescription for nail whiteness is as follows: 2.4.4'
-Trichloro-21-hydroquine diphenyl ether 1,0 urea 40.0p, purified lanolin 240F.
白色ワセリン２５．０ｇ−、及びサランミツロウ１０．
０７を混和して罹患風に塗布する。25.0g of white petrolatum, and 10.0g of Saran beeswax.
Mix 07 and apply to the affected area.
次に、２．４．４７−ドリクロロー２〆−１ニトロキシ
ジフエニルエーテル及び尿素の併有剤において。Next, in the combination agent of 2.4.47-dolichloro-2〆-1 nitroxydiphenyl ether and urea.
両物質を同時に安定化させる安定剤について説明する。A stabilizer that simultaneously stabilizes both substances will be explained.
。その検討は９表−３に示す４種の溶液を調製・、シて
行なった（表中、２％Ｉ Ｂエタノール溶液とあるのは
、２．４．４’−１−リクロロー２’−ヒドロキシ ジ
フェニルエーテルの２’、”／ｊ ％エタノール（９９
，５％）溶液を示す）。. The study was carried out by preparing four types of solutions shown in Table 9-3 (in the table, 2% IB ethanol solution refers to 2′ of diphenyl ether,”/j% ethanol (99
, 5%) solution).
表−３
薬剤の安定性は、各調製溶液２．５５−を３７゛Ｃで７
２時間放置した後における尿素及び２．４．４’−トＩ
Ｊ クロロ−２７−ｔ： ｌ’ロキン ジフェニルエー
テルの、それぞれの分解量を求めることによって調べた
。Table 3 The stability of the drug was determined by measuring 2.55% of each prepared solution at 37°C.
Urea and 2.4.4'-I after standing for 2 hours
J Chloro-27-t: l'loquine This was investigated by determining the amount of decomposition of each diphenyl ether.
まず尿素については、尿素が分解するとアンモニアを生
成するので、その生成アンモニア量を測定することによ
って尿素の安定性をみた。First, regarding urea, since ammonia is produced when urea decomposes, the stability of urea was examined by measuring the amount of ammonia produced.
ここで、調製溶液Ｉｄ中にはｏ７ｓ４３ｙ の尿素を含
有し、仮にこの尿素が１００％分解した場合には０．４
４４８ｐのアンモニアを生成すること測定アンモニア量
（２）
となる。従って 。４４４８ノ Ｘ １００（％
）としてアンモニア生成率を算出した。尚、アンモニア
測定法とｑでは藤井・奥田法変法を用いた。その結果を
表−４に示す。Here, the prepared solution Id contains o7s43y of urea, and if this urea is 100% decomposed, 0.4
The amount of measured ammonia (2) is that 448p of ammonia is generated. Therefore. 4448×100(%
) was calculated as the ammonia production rate. In addition, a modified Fujii-Okuda method was used for the ammonia measurement method and q. The results are shown in Table 4.
上表からも分かるように、硫酸を少量添加した調製溶液
において尿素の安定性が優れ、酢酸を添加したものは尿
素の安定性で若干劣る。尚。As can be seen from the above table, the stability of urea is excellent in the prepared solution in which a small amount of sulfuric acid is added, and the stability of urea is slightly inferior in the solution in which acetic acid is added. still.
硫酸、酢酸以外では、乳酸から酸化１還元反応によって
生成するピルビン酸は、その濃度が高くなるに従って尿
素の分解が進行するので尿素安定剤としては不適当であ
る。また塩酸は塩を作って結晶沈澱を起こしやすく、ク
エン酸、ＥＤＴＡ ・２Ｎａ、ＥＤＴＡ ・２には皮膚
の表面のカルンウムイオンと反応してキレート化合物を
生成するので、いずれも尿素安定剤として用いても意味
が無い。Other than sulfuric acid and acetic acid, pyruvic acid, which is produced from lactic acid by an oxidation-1-reduction reaction, is unsuitable as a urea stabilizer because the decomposition of urea progresses as its concentration increases. In addition, hydrochloric acid tends to form salts and cause crystal precipitation, and citric acid, EDTA・2Na, and EDTA・2 react with carunium ions on the surface of the skin to form chelate compounds, so they are all used as urea stabilizers. is also meaningless.
次に２．４．４’−トリクロロ−２１−ヒドロキンジフ
ェニルエーテルの安定剤について述べる。Next, the stabilizer for 2.4.4'-trichloro-21-hydroquine diphenyl ether will be described.
ここで、フェノール系化合物はメタ過ヨウ素酸ナトリウ
ムの存在下で、４−アミノアノチビリンと縮合反応を起
こし、キノン型色素を生成するので、その吸光度を５０
０鳩（もしくは５７−）で測定することによって２．４
．４’ −トリクロロ−２／−ヒドロキシ ジフェニル
エーテルの定量分析を行った。そして、３７’Ｃで７２
時間放置する前後における定量差から分解率を算出した
。その結果を表−４に示す（表中、ＩＲ分解率とあるの
が２．４．４’−１−リクロロー２／−ヒドロキンジフ
ェニルエーテルの分解率である）。Here, the phenolic compound causes a condensation reaction with 4-aminoanotibiline in the presence of sodium metaperiodate to produce a quinone type dye, so its absorbance is reduced to 50
2.4 by measuring with 0 pigeons (or 57-)
．． Quantitative analysis of 4'-trichloro-2/-hydroxy diphenyl ether was performed. And 72 at 37'C
The decomposition rate was calculated from the quantitative difference before and after standing for a period of time. The results are shown in Table 4 (in the table, IR decomposition rate is the decomposition rate of 2.4.4'-1-lichloro-2/-hydroquine diphenyl ether).
表−４から明らかなように、硫酸を少量添加した調製溶
液における安定性が際立って優れている。そして硫酸を
少量添加したものにあっては、上述したように尿素の安
定性の点でも優れており２両物質を配合した製剤におい
て１両物質を同時に安定化させる安定剤としては、少量
の硫酸が好適である。As is clear from Table 4, the stability in the prepared solution to which a small amount of sulfuric acid was added was outstanding. As mentioned above, products containing a small amount of sulfuric acid are superior in terms of stability of urea, and in preparations containing both substances, a small amount of sulfuric acid is used as a stabilizer to stabilize both substances at the same time. is suitable.
この発明は以上のような構成を有するので。 This invention has the above configuration.
この発明に係る水虫外用薬を水虫治療に用いた場合には
、白癖菌の種類の如何を問わないで極めて良好な治療効
果を挙げ、短期間で水虫を治癒させることができる。し
かも後日水虫が再発するようなこともなく完治でき、ま
た完治までにそれほどの期間を要しないため、患者の精
神的負担も大幅に軽減する。When the external medicine for athlete's foot according to the present invention is used for the treatment of athlete's foot, an extremely good therapeutic effect can be obtained regardless of the type of fungus, and athlete's foot can be cured in a short period of time. Moreover, the athlete's foot can be completely cured without recurrence at a later date, and it does not take a long time to completely recover, which greatly reduces the mental burden on the patient.
さらに、安定剤として少量の硫酸を添加したものにあっ
ては、有効成分の分解を極めて低く抑えることができる
ので、薬剤の塗布は１日１回程度で十分であり、治療の
ための煩わしさもそれほど無い。Furthermore, with the addition of a small amount of sulfuric acid as a stabilizer, the decomposition of the active ingredient can be kept to an extremely low level, so it is sufficient to apply the drug once a day, reducing the hassle of treatment. Not that much.
第１図は、水虫外用薬の抗真菌性能を調べる方法を説明
するための平面図、第２図はその縦断面図であシ、第３
図は、この発明の実施例に係る水虫外用薬と他の薬剤と
における抗真菌性能を比較した抗真菌スペクトル図であ
る。Figure 1 is a plan view for explaining the method for examining the antifungal performance of external medicine for athlete's foot, Figure 2 is its longitudinal cross-sectional view, and Figure 3 is a longitudinal cross-sectional view.
The figure is an antifungal spectrum diagram comparing the antifungal performance of the external medicine for athlete's foot according to an example of the present invention and other medicines.
Claims (1)
ェニルエーテルと尿素とを含有してなる水虫外用薬。 ２、２，４，４′−トリクロロ−２′−ヒドロキシジフ
ェニルエーテルと尿素と少量の硫酸とを含有してなる水
虫外用薬。 ３、０．２〜２．０重量％の２，４，４′−トリクロロ
−２′−ヒドロキシジフェニルエーテルと５〜４０重量
％の尿素とが親水軟膏基剤に混和されてなる特許請求の
範囲第１項又は第２項記載の水虫外用薬。 ４、１．０重量％の２，４，４′−トリクロロ−２′−
ヒドロキシジフェニルエーテルと１０重量％の尿素とを
含有した特許請求の範囲第３項記載の水虫外用薬。 ５、０．２〜２．０Ｗ／Ｖ％の２，４，４′−トリクロ
ロ−２′−ヒドロキシジフェニルエーテルと５〜４０Ｗ
／Ｖ％の尿素とが５０％エタノール水溶液に溶解されて
なる特許請求の範囲第１項又は第２項記載の水虫外用薬
。 ６、１．０Ｗ／Ｖ％の２，４，４′−トリクロロ−２′
−ヒドロキシジフェニルエーテルと１０Ｗ／Ｖ％の尿素
とを含有した特許請求の範囲第５項記載の水虫外用薬。[Scope of Claims] An external medicine for athlete's foot containing 1,2,4,4'-trichloro-2'-hydroxydiphenyl ether and urea. An external medicine for athlete's foot containing 2,2,4,4'-trichloro-2'-hydroxydiphenyl ether, urea and a small amount of sulfuric acid. 3. Claim No. 3, wherein 0.2 to 2.0% by weight of 2,4,4'-trichloro-2'-hydroxydiphenyl ether and 5 to 40% by weight of urea are mixed in a hydrophilic ointment base. The external medicine for athlete's foot according to item 1 or 2. 4, 1.0% by weight of 2,4,4'-trichloro-2'-
The external medicine for athlete's foot according to claim 3, which contains hydroxydiphenyl ether and 10% by weight of urea. 5, 0.2-2.0 W/V% 2,4,4'-trichloro-2'-hydroxydiphenyl ether and 5-40 W
/V% of urea is dissolved in a 50% aqueous ethanol solution. 6, 1.0 W/V% 2,4,4'-trichloro-2'
The external medicine for athlete's foot according to claim 5, which contains -hydroxydiphenyl ether and 10 W/V% urea.
Priority Applications (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP59121586A JPS611615A (en) | 1984-06-12 | 1984-06-12 | External drug for athlete's foot |
| CH2387/85A CH664084A5 (en) | 1984-06-12 | 1985-06-05 | MEDICATION FOR EXTERNAL USE FOR THE ATHLETE'S FOOT. |
| DE19853520325 DE3520325A1 (en) | 1984-06-12 | 1985-06-07 | EXTERNAL APPLICABLE MEDICINE AGAINST FOOTWEAR |
| FR8509273A FR2565486B1 (en) | 1984-06-12 | 1985-06-11 | MEDICINE FOR EXTERNAL APPLICATION FOR DERMATOPHYTOSIS OR SPORT-LIKE MYCOSIS |
| GB08514792A GB2160099B (en) | 1984-06-12 | 1985-06-11 | Treatment of athlete's foot |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP59121586A JPS611615A (en) | 1984-06-12 | 1984-06-12 | External drug for athlete's foot |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS611615A true JPS611615A (en) | 1986-01-07 |
| JPS6344724B2 JPS6344724B2 (en) | 1988-09-06 |
Family
ID=14814907
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP59121586A Granted JPS611615A (en) | 1984-06-12 | 1984-06-12 | External drug for athlete's foot |
Country Status (5)
| Country | Link |
|---|---|
| JP (1) | JPS611615A (en) |
| CH (1) | CH664084A5 (en) |
| DE (1) | DE3520325A1 (en) |
| FR (1) | FR2565486B1 (en) |
| GB (1) | GB2160099B (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6388120A (en) * | 1986-09-19 | 1988-04-19 | ファイザー・インコーポレーテッド | Medicine-containing dermal drug |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0992238B1 (en) * | 1998-10-06 | 2004-10-13 | I-Dent International Corporation | Use of triclosan for preventing and treating mucositis |
| EP2007390A4 (en) * | 2006-04-04 | 2009-11-25 | Avner Shemer | Kit for treating skin infection |
Citations (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3605163A (en) * | 1969-01-10 | 1971-09-20 | Chemway Corp | Bacteriostatic toothbrushes |
| US3629477A (en) * | 1966-08-08 | 1971-12-21 | Geigy Chem Corp | Halogenated diphenyether-containing compositions and control of pests therewith |
| US3723326A (en) * | 1970-09-11 | 1973-03-27 | Lever Brothers Ltd | Detergent compositions |
| US3725547A (en) * | 1970-10-08 | 1973-04-03 | Procter & Gamble | Synergistic antibacterial combination |
| DE2254663A1 (en) * | 1971-11-08 | 1973-05-10 | Armour Pharma | MIXTURES CONTAINING ANTIMICROBIC ALUMINUM HALOGENIDE COMPOUNDS |
| US3794587A (en) * | 1972-03-24 | 1974-02-26 | Armour Dial Inc | Synergistic antiseptic compositions |
| JPS5210424A (en) * | 1975-07-09 | 1977-01-26 | Taisho Pharmaceut Co Ltd | A method for preparing a remedy against cutaneous fungi |
| JPS5287235A (en) * | 1976-01-06 | 1977-07-20 | Taisho Pharmaceut Co Ltd | Remedies for dermatomycosis |
| US4294855A (en) * | 1975-11-26 | 1981-10-13 | Desoto, Inc. | Emollient and/or dyed prilled urea bath bead composition |
| JPS58150509A (en) * | 1982-03-03 | 1983-09-07 | Taisho Pharmaceut Co Ltd | Remedy for trichophytosis |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CH431780A (en) * | 1963-02-22 | 1967-03-15 | Geigy Ag J R | cleaning supplies |
| FR2505325A1 (en) * | 1981-05-08 | 1982-11-12 | Reisacher Fils Laboratoires A | METHOD AND SOLUTION FOR AVOIDING FOOT SWEATING ODORS |
-
1984
- 1984-06-12 JP JP59121586A patent/JPS611615A/en active Granted
-
1985
- 1985-06-05 CH CH2387/85A patent/CH664084A5/en not_active IP Right Cessation
- 1985-06-07 DE DE19853520325 patent/DE3520325A1/en active Granted
- 1985-06-11 FR FR8509273A patent/FR2565486B1/en not_active Expired
- 1985-06-11 GB GB08514792A patent/GB2160099B/en not_active Expired
Patent Citations (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3629477A (en) * | 1966-08-08 | 1971-12-21 | Geigy Chem Corp | Halogenated diphenyether-containing compositions and control of pests therewith |
| US3605163A (en) * | 1969-01-10 | 1971-09-20 | Chemway Corp | Bacteriostatic toothbrushes |
| US3723326A (en) * | 1970-09-11 | 1973-03-27 | Lever Brothers Ltd | Detergent compositions |
| US3725547A (en) * | 1970-10-08 | 1973-04-03 | Procter & Gamble | Synergistic antibacterial combination |
| DE2254663A1 (en) * | 1971-11-08 | 1973-05-10 | Armour Pharma | MIXTURES CONTAINING ANTIMICROBIC ALUMINUM HALOGENIDE COMPOUNDS |
| US3794587A (en) * | 1972-03-24 | 1974-02-26 | Armour Dial Inc | Synergistic antiseptic compositions |
| JPS5210424A (en) * | 1975-07-09 | 1977-01-26 | Taisho Pharmaceut Co Ltd | A method for preparing a remedy against cutaneous fungi |
| US4294855A (en) * | 1975-11-26 | 1981-10-13 | Desoto, Inc. | Emollient and/or dyed prilled urea bath bead composition |
| JPS5287235A (en) * | 1976-01-06 | 1977-07-20 | Taisho Pharmaceut Co Ltd | Remedies for dermatomycosis |
| JPS58150509A (en) * | 1982-03-03 | 1983-09-07 | Taisho Pharmaceut Co Ltd | Remedy for trichophytosis |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6388120A (en) * | 1986-09-19 | 1988-04-19 | ファイザー・インコーポレーテッド | Medicine-containing dermal drug |
| JPH0476967B2 (en) * | 1986-09-19 | 1992-12-07 | Pfizer |
Also Published As
| Publication number | Publication date |
|---|---|
| GB2160099A (en) | 1985-12-18 |
| FR2565486B1 (en) | 1988-12-02 |
| DE3520325A1 (en) | 1985-12-12 |
| DE3520325C2 (en) | 1988-08-04 |
| GB2160099B (en) | 1988-01-20 |
| FR2565486A1 (en) | 1985-12-13 |
| CH664084A5 (en) | 1988-02-15 |
| GB8514792D0 (en) | 1985-07-10 |
| JPS6344724B2 (en) | 1988-09-06 |
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