JPS6130644B2 - - Google Patents

Info

Publication number
JPS6130644B2
JPS6130644B2 JP10887979A JP10887979A JPS6130644B2 JP S6130644 B2 JPS6130644 B2 JP S6130644B2 JP 10887979 A JP10887979 A JP 10887979A JP 10887979 A JP10887979 A JP 10887979A JP S6130644 B2 JPS6130644 B2 JP S6130644B2
Authority
JP
Japan
Prior art keywords
filter paper
minutes
carpronium chloride
sebum
therapeutic agent
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
JP10887979A
Other languages
Japanese (ja)
Other versions
JPS5632415A (en
Inventor
Hidehiko Takahashi
Minoru Kuroda
Masanori Fukui
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.)
Daiichi Pharmaceutical Co Ltd
Original Assignee
Daiichi Pharmaceutical Co 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 Daiichi Pharmaceutical Co Ltd filed Critical Daiichi Pharmaceutical Co Ltd
Priority to JP10887979A priority Critical patent/JPS5632415A/en
Publication of JPS5632415A publication Critical patent/JPS5632415A/en
Publication of JPS6130644B2 publication Critical patent/JPS6130644B2/ja
Granted legal-status Critical Current

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  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Description

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

本発明は塩化カルプロニウムを含有する皮膚疾
患治療剤に関する。 副交感神経刺激剤として開発され、胃炎、無酸
症等の消化器疾患に使用されている塩化カルプロ
ニウムは、本発明者らの研究により、外用塗布剤
として各種皮膚疾患にも有効であることが見いだ
され本願発明は完成された。 本薬剤を本発明の目的の為に使用するには、通
常の軟膏もしくはクリーム剤として0.1〜3%の
範囲内で含有せしめて使用すればよい。特に0.4
〜1%程度が好適である。 本剤が著効を示す適応症としては、洗剤等によ
る接触性皮膚炎を包括する家婦湿疹、進行性指掌
角皮症、輝裂性湿疹(ひび、あかぎれ)及び冬期
癈痒症等からなる湿疹・皮膚炎群その他凍瘡等で
ある。 先述の如く本薬剤は元来副交感神経刺激剤であ
り、一般にその基本的に想定される生理作用は多
数列挙されるが、本願の目的とする皮膚疾患を治
癒せしめるべく関連ある作用としては、その内か
ら作用機構的には皮脂分泌促進作用、末梢血管拡
張等により発汗促進作用である。 しかしながら実際の臨床において本願の目的と
する皮膚疾患を充分完治せしめる程度に外用剤と
してこれ等の基本的作用が認められ、しかも副作
用が少く、合目的々な薬剤は、副交感神経刺激剤
の内にも少いものである。以下本薬剤が、これら
皮脂分泌促進作用及び発汗作用が充分認められる
ことについての実験結果を示す。 (イ) 皮脂測定法 皮脂の測定はJ.Graham Smith Jr.ら
(1959)のオスミウム酸濾紙法を参照として、
被験部位はヒトの額を撰んだ。すなわち額の中
心部に3.0×4.0cmのWhatman No.42の濾紙をの
せ、それと同大のスポンジで覆いゴムバンドで
圧力が一定になる様に5分間圧着する。これを
2回繰り返し既存の皮脂を濾紙に吸収させる。
その後、カルプロニウムクロライド溶液(対照
の場合は溶媒のみ)を3.0×4.0cmの濾紙に0.3ml
しみこませ、上からアルミホイルで覆つて被験
部位に貼付し30分間作用させた。濾紙を取り去
り25分間放置後3.0×4.0cmのWhatman No.42の
濾紙を被験部位に5分間ゴムバンドで一定圧に
圧着、2回繰り返して測定すべき皮脂を濾紙に
吸収させた。皮脂を吸収した濾紙は2%オスミ
ウム酸水溶液を入れたビンの中で5分間オスミ
ウム酸蒸気にさらした後、水蒸気の充満したデ
シケーター中に24時間放置し、皮脂の黒化を安
定化させた。 黒化度の測定は濾紙の周辺部を除いた2.0×
2.0cmについて、写真用引伸器Durst M600と
Toshiba光電照度計LS−1−Aを用いて無処理
のWhatman No.42濾紙の透過率を100として測
定した。 カルプロニウムクロライドは10%エチルアル
コール含有のクエン酸緩衝液(PH5.5)に溶解
して使用した。 用量は1%(0.25mg/cm2)、2%(0.5mg/
cm2)、4%(1.0mg/cm2)及び8%(2.0mg/cm2
の4用量と対照として溶媒のみ(10%エチルア
ルコール含有クエン酸緩衝液、PH5.5)を用い
た。 (実験成績) 1群7名の男女(年令24〜58才)に各濃度の
カルプロニウムクロライド溶液を作用させ、溶
媒のみの対照の皮脂分泌量と作用後の分泌量の
差をt−検定して有意の増加を認めた。結果は
表1・2の通りである。
The present invention relates to a therapeutic agent for skin diseases containing carpronium chloride. Carpronium chloride, which was developed as a parasympathetic nerve stimulant and is used to treat gastrointestinal diseases such as gastritis and achlorhydria, has been found to be effective against various skin diseases as an external topical preparation through research conducted by the present inventors. The claimed invention has been completed. In order to use this drug for the purpose of the present invention, it may be used in a conventional ointment or cream containing it within the range of 0.1 to 3%. Especially 0.4
About 1% is suitable. The indications for which this drug is highly effective include domestic eczema, including contact dermatitis caused by detergents, etc., progressive digital palmar keratoderma, fissuring eczema (cracks and chapping), and winter pruritus. These include eczema, dermatitis, and other types of acne. As mentioned above, this drug is originally a parasympathetic nerve stimulant, and its basically assumed physiological effects can be enumerated in many ways. In terms of mechanism of action, it promotes sebum secretion and promotes sweating by dilating peripheral blood vessels. However, in actual clinical practice, these basic effects have been recognized as external agents to the extent that they can fully cure the skin diseases targeted by this application, and there are few side effects, and drugs that are suitable for various purposes are considered to be among the parasympathetic nerve stimulants. There are also few. The following are the experimental results showing that this drug has sufficient sebum secretion-promoting effect and sweating effect. (b) Sebum measurement method For the measurement of sebum, refer to the osmic acid filter paper method of J. Graham Smith Jr. et al. (1959).
The test site was a human forehead. That is, place a Whatman No. 42 filter paper measuring 3.0 x 4.0 cm in the center of the forehead, cover it with a sponge of the same size, and press it with a rubber band for 5 minutes to keep the pressure constant. Repeat this twice to allow the existing sebum to be absorbed into the filter paper.
Then, add 0.3 ml of carpronium chloride solution (solvent only for control) to a 3.0 x 4.0 cm filter paper.
It was soaked in, covered with aluminum foil, applied to the test site, and left to act for 30 minutes. After removing the filter paper and leaving it for 25 minutes, a 3.0 x 4.0 cm Whatman No. 42 filter paper was pressed onto the test site with a constant pressure using a rubber band for 5 minutes, and repeated twice to allow the sebum to be measured to be absorbed into the filter paper. The filter paper that had absorbed sebum was exposed to osmic acid vapor for 5 minutes in a bottle containing a 2% osmic acid aqueous solution, and then left in a desiccator filled with steam for 24 hours to stabilize the darkening of the sebum. The degree of blackening was measured at 2.0× excluding the peripheral area of the filter paper.
About 2.0cm, with photo enlarger Durst M600
Measurements were made using a Toshiba photoelectric luminometer LS-1-A with the transmittance of untreated Whatman No. 42 filter paper set at 100. Carpronium chloride was used after being dissolved in citrate buffer (PH5.5) containing 10% ethyl alcohol. The dose was 1% (0.25mg/cm 2 ), 2% (0.5mg/cm 2 ),
cm 2 ), 4% (1.0mg/cm 2 ) and 8% (2.0mg/cm 2 )
and solvent alone (citrate buffer containing 10% ethyl alcohol, pH 5.5) was used as a control. (Experimental results) A carpronium chloride solution of various concentrations was applied to 7 men and women (aged 24 to 58 years old) in one group, and a t-test was conducted to determine the difference between the sebum secretion amount in a control using only the solvent and the secretion amount after the action. A significant increase was observed. The results are shown in Tables 1 and 2.

【表】【table】

【表】 (ロ) 発汗測定法 被験部位はヒトの手の平の一定部位、大きさ
1.0×2.0cmの濾紙にカルプロニウムクロライド
溶液を0.05ml、対照として対側の手の平には溶
媒のみを0.05mlしみこませて貼付し、上からセ
ロテープで蒸発をふせぎ30分間検体を作用させ
た。30分後濾紙を取りさり25%塩化第二鉄の70
%エタノール溶液を塗布して25分間放置後5%
タンニン酸水溶液に3分間ひたして乾燥させた
セロフアン紙(1.0×2.0cm)をセロテープで10
分間圧着し、発汗によるセロフアン紙の黒化度
を対照と比較した。次回には左右の手の平を変
えて発汗を測定し、そのいずれの場合にも被験
液の作用した側の発汗が高いものだけを陽性と
した。 カルプロニウムクロライドは10%エチルアル
コール含有のクエン酸緩衝液(PH5.5)に溶解
して使用した。 用量は0.5%(0.125mg/cm2)、1.0%(0.25mg/
cm2)、2.0%(0.5mg/cm2)、4.0%(1.0mg/cm2)の
4用量とした。実験結果は下表3の通りであつ
た。
[Table] (b) Sweat measurement method The test site is a certain area and size of the human palm.
A 1.0 x 2.0 cm filter paper was soaked with 0.05 ml of carpronium chloride solution, and as a control, 0.05 ml of solvent alone was applied to the contralateral palm of the hand, and evaporation was prevented with Sellotape from above, and the sample was allowed to act for 30 minutes. After 30 minutes, remove the filter paper and add 70% of 25% ferric chloride.
After applying % ethanol solution and leaving it for 25 minutes, 5%
Cellophane paper (1.0 x 2.0 cm) soaked in an aqueous tannic acid solution for 3 minutes and dried is wrapped with cellophane tape for 10 minutes.
The degree of blackening of the cellophane paper due to perspiration was compared with that of a control. Next time, sweating was measured using different palms, and in each case, only those with higher sweating on the side where the test solution was applied were considered positive. Carpronium chloride was used after being dissolved in citrate buffer (PH5.5) containing 10% ethyl alcohol. The dose was 0.5% (0.125mg/cm 2 ), 1.0% (0.25mg/cm 2 ),
cm 2 ), 2.0% (0.5 mg/cm 2 ), and 4.0% (1.0 mg/cm 2 ). The experimental results are shown in Table 3 below.

【表】 1群10名の男女(年令58〜24才)の被験者よ
り得られた成績よりカルプロニウムクロライド
の発汗作用のED50=0.20(0.103〜0.388)mg/
cm2で発汗作用の存在が証明された。 次に本発明の臨床効果を確認するために使用さ
れたクリーム剤の製造参考例を示す。 参考例
[Table] Based on the results obtained from 10 male and female subjects (58 to 24 years old) in group 1, the ED 50 of the sweating effect of carpronium chloride = 0.20 (0.103 to 0.388) mg/
The presence of a diaphoretic effect was proven in cm 2 . Next, a reference example of manufacturing a cream used to confirm the clinical effects of the present invention will be shown. Reference example

【表】 ン
[Table]

【表】 以上の配合比をもつて日本薬局方製剤総則軟膏
剤の製造法に従つて、まず水層に塩化カルプロニ
ウムを溶解し、流動パラフイン等の油性基剤と界
面活性剤(乳化剤)を用いてO/Wタイプクリー
ム剤とし、その他処方添加剤と共に製品とした。
なお、製剤のPHは5.0〜5.3の間に調整した。 以下本願発明の効果を治験薬(A)及び(B)による臨
床効果によつて説明する。 実施例 1
[Table] According to the manufacturing method of ointment according to the Japanese Pharmacopoeia General Preparations with the above compounding ratio, carpronium chloride is first dissolved in the aqueous layer, and an oily base such as liquid paraffin and a surfactant (emulsifier) are used. It was made into an O/W type cream and a product together with other prescription additives.
In addition, the pH of the formulation was adjusted between 5.0 and 5.3. The effects of the present invention will be explained below using the clinical effects of investigational drugs (A) and (B). Example 1

【表】【table】

【表】【table】

【表】 以上(A)(B)使用結果をまとめると【table】 To summarize the results of using (A) and (B) above,

【表】【table】

【表】 効果判定基準 個々の症例について、下記の結過表例挙の各項
目につき数回に亘り4段階評価し、初診時と判定
時の4段階評価(〓、+、±、−)を対比して、自
他覚症状の推移及び臨床症状の改善速度などを考
慮して、著効・有効・やゝ有効・無効と判定し
た。
[Table] Criteria for evaluating effectiveness For each case, each item in the results table below was evaluated several times in four stages, and the four-stage evaluation (〓, +, ±, -) was performed at the time of the first visit and at the time of evaluation. In comparison, the drug was judged to be excellent/effective, rather effective/ineffective, taking into consideration the changes in subjective and objective symptoms and the rate of improvement in clinical symptoms.

【表】【table】

【表】 実施例 2【table】 Example 2

【表】【table】

【表】【table】

【表】【table】

【表】【table】

【表】【table】

Claims (1)

【特許請求の範囲】 1 塩化カルプロニウムを含有することを特徴と
する皮膚疾患治療剤。 2 皮膚疾患が凍瘡及び湿疹・皮膚炎群の一以上
の疾患である特許請求範囲1の治療剤。 3 塩化カルプロニウムの含有量が0.1〜3%で
ある特許請求範囲1又は2の皮膚疾患治療剤。
[Scope of Claims] 1. A therapeutic agent for skin diseases characterized by containing carpronium chloride. 2. The therapeutic agent according to claim 1, wherein the skin disease is one or more diseases of the chiroacne and eczema/dermatitis group. 3. The therapeutic agent for skin diseases according to claim 1 or 2, wherein the content of carpronium chloride is 0.1 to 3%.
JP10887979A 1979-08-27 1979-08-27 Remedy for dermatosis Granted JPS5632415A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP10887979A JPS5632415A (en) 1979-08-27 1979-08-27 Remedy for dermatosis

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP10887979A JPS5632415A (en) 1979-08-27 1979-08-27 Remedy for dermatosis

Publications (2)

Publication Number Publication Date
JPS5632415A JPS5632415A (en) 1981-04-01
JPS6130644B2 true JPS6130644B2 (en) 1986-07-15

Family

ID=14495893

Family Applications (1)

Application Number Title Priority Date Filing Date
JP10887979A Granted JPS5632415A (en) 1979-08-27 1979-08-27 Remedy for dermatosis

Country Status (1)

Country Link
JP (1) JPS5632415A (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS6239512A (en) * 1985-08-15 1987-02-20 Yakurigaku Chuo Kenkyusho:Kk Cosmetic containing carpronium chloride
JPS6239858A (en) * 1985-08-16 1987-02-20 Mamiya Koki Kk Timer device for instant film development
JPWO2007013290A1 (en) * 2005-07-28 2009-02-05 興和株式会社 Anti-inflammatory analgesic

Also Published As

Publication number Publication date
JPS5632415A (en) 1981-04-01

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