WO1989003668A1 - Diazoxide-containing hair care product - Google Patents

Diazoxide-containing hair care product Download PDF

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Publication number
WO1989003668A1
WO1989003668A1 PCT/JP1987/000804 JP8700804W WO8903668A1 WO 1989003668 A1 WO1989003668 A1 WO 1989003668A1 JP 8700804 W JP8700804 W JP 8700804W WO 8903668 A1 WO8903668 A1 WO 8903668A1
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WIPO (PCT)
Prior art keywords
hair
diazoxide
growth
alopecia
care product
Prior art date
Application number
PCT/JP1987/000804
Other languages
French (fr)
Japanese (ja)
Inventor
Junichi Akiyama
Kinji Kaname
Original Assignee
Kabushiki Kaisha Kaminomoto Hompo
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 Kabushiki Kaisha Kaminomoto Hompo filed Critical Kabushiki Kaisha Kaminomoto Hompo
Priority to PCT/JP1987/000804 priority Critical patent/WO1989003668A1/en
Publication of WO1989003668A1 publication Critical patent/WO1989003668A1/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q7/00—Preparations for affecting hair growth
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds

Definitions

  • the present invention relates to a hair growth-promoting and hair-growing cosmetics exhibiting a hair-growth / hair-growth effect.
  • Alopecia areata or male pattern baldness, apart from congenital alopecia and scarring alopecia, include hair that is healthy and has hair roots in the skin. The function of production is reduced or stopped, and thinning hair and hugs usually develop. There are various theories as to the causes of alopecia, and despite much research, the causes have not been clarified, and methods for prevention and treatment are still well established. is the current situation. In today's social customs, hair has a significant cosmetic meaning, so what is the psychological distress of alopecia patients?]?
  • the present invention develops a hair growth-promoting cosmetic treatment that is effective in treating hair loss and hair loss in various types of alopecia accompanied by hair loss and elimination of hair loss in people with alopecia. This was done for the purpose of doing so.
  • diazokind also known as endemin
  • ⁇ was eh to the completion of the present invention is heading the door
  • Kuazoki Shi De is the chemical name 7 - click B B - 3 - methyltransferase - 2 Eta - 1, 2 4 - base emissions Zochia Zia di emissions - 1, 1 - Jioki shea de, chemical formula C e ii CN 3 0, S, a compound having a molecular weight of 230.70, having the following structural formula:
  • This quazoxide is hardly soluble in water, black hole homes and ethers, and is soluble in alcohol and alkaline solutions.
  • the drug dilates directly into the smooth muscles of the wall of the coccyx artery, which causes the blood vessels to dilate and increase the blood circulation around the follicles.
  • it is thought that it promotes the splitting ability of small deer groups related to hair growth, or activates the protein synthesizing action required for hair formation, thereby exhibiting effective plowing for hair growth and hair growth.
  • the inventors of the present invention have tried to use hair growth cosmetics with diazoxide and apply it to people with alopecia, and it has been found that at least 6 to 9 drugs are regarded as conventional treatments for alopecia. While the aesthetic effect is obvious when not applied to the moon, the diazoxide-containing hair restoration cosmetics of the present invention can be used for 1-2 months. In a short period of time, the pubescence of the pubic hairs increases.], And it has been found that there is a cosmetically satisfactory improvement. These satisfying changes can be seen in most alopecia patients except those with endogenous illnesses and the elderly.
  • the present inventors have tried to administer other components having a vasodilatory effect and antihypertensive agents to alopecia patients by external use, as well as diazoxide. It has a strong direct vascular smoothing, which is used as a therapeutic drug for hypertensive acute disease. It has a vasodilatory effect-trobulside soda (Sodium nitroprusside), Peripheral blood flow improver i) Cyclaadelate, which acts directly on vascular smooth muscle and shows vasodilatory effect, is a sympathetic ⁇ -blocker!
  • a drug having a blood pressure lowering action, a vasodilatory action or a blood flow promoting action does not necessarily have an excellent hair-growing cosmetic effect.
  • the diazoxide used in the present invention alone exerts its unique hair growth and hair growth effects due to its unique effect on the division and differentiation of hair root cells. It is considered to be something.
  • the hair restoration cosmetic of the present invention is characterized by dissolving or dispersing diazoxide as an active ingredient in a base usually used for this type of hair restoration cosmetic. , Lotions, gels, etc.
  • the amount of the active ingredient in the hair restoration cosmetics department is particularly limited, but it is usually
  • the hair growth cosmetic of the present invention is usually applied to 1 HI per day, but more or more. The effect can be obtained even with the following.
  • the following formulation was used to prepare a gel preparation with excellent hair-growing effect by a conventional method.
  • the hair growth and hair growth effects of the hair growth cosmetic of the present invention were tested as follows.
  • the hair growth cosmetic of the present invention is clear. * Hair growth * It has a hair growth effect, indicating that it is a convenient hair growth cosmetic.

Abstract

A hair care product containing 7-chloro-3-methyl-2H-1,2,4-benzothiadiazine 1,1-dioxide as an effective ingredient is disclosed.

Description

明 細 香  Incense
発明の名称  Title of invention
ジァゾキ シ ド配合養毛化粧料  Hairdressing cosmetics containing diazoxide
技術分野 Technical field
本発明は、 侵れた養毛 · 発毛効果を示す発毛促進養毛 化粧科に関する ものである。  TECHNICAL FIELD The present invention relates to a hair growth-promoting and hair-growing cosmetics exhibiting a hair-growth / hair-growth effect.
背景技銜 Background technique
脱毛症には先天性の無毛症や瘢痕性脱毛症な どは別と して、 円形脱毛症や男性型脱毛症は身体が健康で、 毛根 が皮膚中に存在するにもかかわらず毛を産生する機能が 低下ある は停止して しま 、 薄毛、 ハグが発症するの がほとんどである。 それら脱毛症の原因 と して種々 の説 があ 、 多 く の研究がされて きたに も かかわ らず、 その 原因は明確にされて く、 予防や治療の方法が今だに確 立してい のが現状である。 今日 の社会風俗において、 毛髮の有する美容的 意味は大きいため、 脱毛症患者の 精神的苦悩ははか ]? しれ いも のがある。  Alopecia areata or male pattern baldness, apart from congenital alopecia and scarring alopecia, include hair that is healthy and has hair roots in the skin. The function of production is reduced or stopped, and thinning hair and hugs usually develop. There are various theories as to the causes of alopecia, and despite much research, the causes have not been clarified, and methods for prevention and treatment are still well established. is the current situation. In today's social customs, hair has a significant cosmetic meaning, so what is the psychological distress of alopecia patients?]?
発明の開示 Disclosure of the invention
本発明は、 脱毛症で い人に対 しては育毛 · 化粧効果 があ ]? 、 また毛根の消失を伴わ 各種脱毛症の治療に 対 して有効である発毛促進養毛化粧科を開発する こ と を 目 的と して行なったも のである。  The present invention develops a hair growth-promoting cosmetic treatment that is effective in treating hair loss and hair loss in various types of alopecia accompanied by hair loss and elimination of hair loss in people with alopecia. This was done for the purpose of doing so.
本発明者らは、 高血圧性急性症に対する治療注射薬、 高血圧症の絰ロ治療薬と して用 られる ジァゾキ ン ド ( 別名エ ン デ ミ ン ） が優れた養毛 · 発毛効果を有する とを見 出 して本発明を完成するに えった β The present inventors have found that diazokind (also known as endemin), which is used as a therapeutic injection for hypertensive acute disease and as a therapeutic agent for hypertension, has excellent hair-growth and hair-growth effects. Β was eh to the completion of the present invention is heading the door
クァゾキ シ ドは、 化学名が 7 - ク ロ ロ - 3 - メ チル - 2 Η - 1, 2 4 - ベ ン ゾチア ジア ジ ン - 1 ， 1 - ジォキ シ ド、 化学式 C eii C N 30，S 、分子量 2 3 0. 7 0 の化合物 て、 次に示す構造式 ： Kuazoki Shi De is the chemical name 7 - click B B - 3 - methyltransferase - 2 Eta - 1, 2 4 - base emissions Zochia Zia di emissions - 1, 1 - Jioki shea de, chemical formula C e ii CN 3 0, S, a compound having a molecular weight of 230.70, having the following structural formula:
Figure imgf000004_0001
を有する白色 い し類白色の無臭結晶性粉末で、 融点は 3 3 0〜3 3 1 X：である β
Figure imgf000004_0001
Is a white or odorless crystalline powder having a melting point of 330-331 X: β
こ 'クァ ゾキ シ ドは、 水、 ク ロ 口ホ ル ム 、 エ ーテルに 殆ど溶けず、 ア ル コ ー ル 、 アルカ リ 溶液に可溶である。  This quazoxide is hardly soluble in water, black hole homes and ethers, and is soluble in alcohol and alkaline solutions.
'クァゾキ シ ドを皮膚に投与するこ とで、 本薬剤のもつ 末棺動脈壁の平滑筋に対する直接的勉鑀作周によ 血管 を拡張し、 毛根局囲の血行を よ U盛んに し、 また毛成長 に関する細鹿群に対し分裂能を促進し、 ある は毛生成 に必要 タ ンパク合成作用を活性化する ことで養毛 · 発 毛に有効 鋤きを示すものと考えられる。  ク By administering quarzoxide to the skin, the drug dilates directly into the smooth muscles of the wall of the coccyx artery, which causes the blood vessels to dilate and increase the blood circulation around the follicles. In addition, it is thought that it promotes the splitting ability of small deer groups related to hair growth, or activates the protein synthesizing action required for hair formation, thereby exhibiting effective plowing for hair growth and hair growth.
本発明者 らはジァゾキ シ ドを配合し 養毛化粧料を脱 毛症の人に遍用を試みたと ころ、 従来の脱毛症の治療剤 と われる も のは、 少 く と も 6 〜 9 力月適用 しな と美 容的 効果は明 らかで ¾ぃと われて るのに対 して、 発明の ジァゾキ シ ド配合養毛化粧料は、 1 〜 2 力月の 短期間で、 軟毛の硬毛化が起 ]?、 美容的に満足でき る改 養が見られる こ とを見い出 した。 これらの満足でき る改 巷は、 内因的 ¾病気をもつ患者や高佘者を除 く殆どの脱 毛症患者に見る とができ る。 The inventors of the present invention have tried to use hair growth cosmetics with diazoxide and apply it to people with alopecia, and it has been found that at least 6 to 9 drugs are regarded as conventional treatments for alopecia. While the aesthetic effect is obvious when not applied to the moon, the diazoxide-containing hair restoration cosmetics of the present invention can be used for 1-2 months. In a short period of time, the pubescence of the pubic hairs increases.], And it has been found that there is a cosmetically satisfactory improvement. These satisfying changes can be seen in most alopecia patients except those with endogenous illnesses and the elderly.
本発明者らは、 ジァゾキ シ ドと同 じ く 、 他の血管拡張 作用を有する成分や血圧降下剤につ て も脱毛症の患者 へ外用に よる投与を試みたと ころ、 ジァゾキ シ ドと同様 に高血圧性急性症の治療薬と して用いられている強い直 接の血管平滑飭雖緩作用によ ]?血管拡張作用を示す- ト ロ ブル シ ド ソ ーダ ( Sodium Ni t ropruss ide ) 、 末梢血 流改善剤であ i)血管平滑筋に直接作用 して血管拡張作用 を示す 'ンク ラ ンデ レ ー ト （ Cyclaadelate )、 交感神経 ^ - 蘧断剤であ ！）交換神経 -受容体遮断作用に よ ]?血管 拡張作用を もつブロ ブ ラ ノ ー ル ( ropranolol ) 、 血圧 降下剤と して用 られァ ドネ ラ リ ン作動性神経節遮断作 用によ ]?血管拡張作用をもつグァネ チ ジ ン （ Giianetlii dine )、 また血圧降下剤であ ]? ア ン ジ ォ テ ン シ ン変換醇 素抑制作用に よ ]3血管拡張作用を もつ力 ブ ト リ ル （ Cap toril ) 等の各種薬剤につ て脱毛症患者への外用投与 を試みたが、 養毛、 毛生効果は見られ かった。  The present inventors have tried to administer other components having a vasodilatory effect and antihypertensive agents to alopecia patients by external use, as well as diazoxide. It has a strong direct vascular smoothing, which is used as a therapeutic drug for hypertensive acute disease. It has a vasodilatory effect-trobulside soda (Sodium nitroprusside), Peripheral blood flow improver i) Cyclaadelate, which acts directly on vascular smooth muscle and shows vasodilatory effect, is a sympathetic ^ -blocker! ) Due to sympathetic nerve-receptor blocking action ???????????????????????????????????: Branolanol (ropranolol), which is used as an antihypertensive agent, and is used to block ganglion-activated ganglia. ]? Gianetliidine, which has vasodilatory action, and is also a hypotensive agent.??Angiotensin-converted, which suppresses the concentration of melamine.] 3Body with vasodilatory action An attempt was made to externally administer various drugs such as Captoril to alopecia patients, but no effect on hair restoration or hair growth was found.
上記のこ とから、 血圧降下作用、 血管拡張作用あるい は血流增進作用のある薬剤が必ずしもす ぐれた養毛化粧 効果を もつも ので いこ とがわかる。 本発明で用 る ジ ァ ゾキ シ ドだけがも つ特有のす ぐれた毛根細胞の分裂 · 分化に対する作用によ ])、 発毛 · 育毛効果を発現 してい る も のと考え られる。 From the above, it can be understood that a drug having a blood pressure lowering action, a vasodilatory action or a blood flow promoting action does not necessarily have an excellent hair-growing cosmetic effect. The diazoxide used in the present invention alone exerts its unique hair growth and hair growth effects due to its unique effect on the division and differentiation of hair root cells. It is considered to be something.
本発明の養毛化粧料は、 有効成分である ジァ ゾキ シ ド を通常 この種の養毛化粧料に使用される基剤に溶藓また は分散させる 2：とによって、 ク リ ー ム 、 ロ ー シ ョ ン、 ゲ ル剤 ¾ ど種々 の剤型とする こ とができ る。  The hair restoration cosmetic of the present invention is characterized by dissolving or dispersing diazoxide as an active ingredient in a base usually used for this type of hair restoration cosmetic. , Lotions, gels, etc.
養毛化粧科中の有効成分量は特に限定される が通常 The amount of the active ingredient in the hair restoration cosmetics department is particularly limited, but it is usually
(L l 〜 2 （重量 ） の閩で £合され、 好ま し く は Ι 5ί程 度である。 本発明の養毛化粧料は通常 1 日 1 HI適用する 程度でよ が、 それ以上またはそれ以下でも効果は得ら れる。 (It is combined in the range of Ll to 2 (weight), preferably about 5Ι. The hair growth cosmetic of the present invention is usually applied to 1 HI per day, but more or more. The effect can be obtained even with the following.
発明を実施するための最良の形態 BEST MODE FOR CARRYING OUT THE INVENTION
^下に若干の実施例および試験例をあげて具体的に本 発明を説明するが、 本発明はこれ等のみに限定される も のでは 。  ^ The present invention will be specifically described with reference to some examples and test examples below, but the present invention is not limited thereto.
実施例 1 Example 1
次の処方によ 常法にて養毛効杲の優れたゲル製剤を 調製した。  The following formulation was used to prepare a gel preparation with excellent hair-growing effect by a conventional method.
(重量 )  (Weight)
' ァゾキ 'ン ド α 5  'Azoki' Hand α 5
濃グ リ セ リ ン a o  Dark glycerin a o
カルボキシビ ルボ リ マー 1. 0  Carboxyrubiomer 1.0
ト エタ ノ ール了 ミ ン 0. 4 5  Ethanol end Min. 0.45
ェ タ ノ — -ル 4 ο  —-— 4 ο
精 製 水 5 5.0 5  Refined water 5 5.0 5
実施例 2 次の処方によ ]?常法にて泰毛効果の侵れたハァー ト - ッ クを調製 した， Example 2 According to the following prescription] ???????????
ジァ ゾキ 、ン ド 5 s  Jia Zoki, 5 s
サ リ チル酸 0.1 g  Salicylic acid 0.1 g
1 , 3 -ブチレングリ コール 3.0 g  1,3-Butylene glycol 3.0 g
c -メ ン ト ール aig  c-menthol aig
ヱ タ ノ ール 7 O t  ヱ Tanor 7 O t
精 製 水 適量  Refined water
(以上全量 1 Ο Οι ^とする ） 実施例 3  (The total amount is 1 Ο Οι ^.)
次の処方に よ 常法にて養毛効果の侵れた軟胥製剤を 調製した。  The following formula was used to prepare a soft Xu Xu preparation with a hair-growth effect in a conventional manner.
ジァゾキ 'ン ド 1.0 g  Jizoki's Hand 1.0 g
局方親水軟膏 saog  Hydrophil ointment saog
試験例 Test example
本発明養毛化粧料の養毛 · 発毛効果を以下の ごと く試 験 した。  The hair growth and hair growth effects of the hair growth cosmetic of the present invention were tested as follows.
1.動物実験  1.animal experiments
第 8週令の 3H マ ウ ス （さ） を用いて、 1 群を 11 と して 2群を作 ]?、 全マ ウ ス の背部毛を 2·5α« X & 0«« の 範囲に抜毛 し、 一方の群を被検液塗布群と して ジァ ゾ キ シ ド （L l g/^ O エ タ ノ 一 ^溶液 の被検液を 連日、 1 日 1 回 2 0 0 づっ毛成長が終了するまで背部 に塗布投与 した、 また飽方を対照群と して溶媒のみを 同様に塗布投与 した。 両群のマ ウ ス の再生する背部毛 の長さ ( 1 ¾5当 1 回 15本） よび太さ ( 1 ¾当 ]? 100本 ） につ て測定した結果を表 Iおよび Sに示す 表 - I 毛 成長の長さ の測定 （ 举位 麵 ） Using a 3 H Ma cormorant nests 8 weeks of age (is), create the two groups and the first group and 11] ?, Zenma cormorant nests range of the back hair 2 · 5α «X & 0« « One of the groups was treated with the test solution, and the test solution of diazoxide (L lg / ^ O ethanoic ^ solution was applied to the subject once a day every day. The mice were applied to the back until the growth was completed, and the mice were re-applied and administered only the solvent in the same manner as the control group for the satiety. Tables I and S show the results of measurements on the length (1 ¾ 5 per 15 pcs) and the thickness (1 ¾ per?) Of 100 pcs. Table -I Measurement of hair growth length (举麵)
10 Ten
X5 X5
Figure imgf000008_0001
Figure imgf000008_0001
*o 2·臨床試驗 * o 2 ・ Clinical test
試験液と してジ了 ゾキシ ド dSffZェタ ノ ール 溶液を用 、 本試料液を 1 回約 日 2回頭部脱 毛部分に塗擦し、 約 5 力月間縫続使用を行 い、 塗擦 部位の新毛の発生 · 発育等を単位面積当た ]? の硬毛の « 毛幹数を針溺する毛密度溺定法と、 写真擐彭を行な 判定する score判定法にて評餾した。 score判定法の判定基準は次の通 ]? と した。 Use the zoxoxide dSffZ ethanol solution as a test solution, apply this sample solution once a day to the depilated part of the head about twice a day, and continue using it for about 5 power months.新 · 発 生 新 新 新 毛 新 毛 新 新 新 毛 毛 硬 密度 硬 硬 Judged by the score judgment method. The criteria for the score judgment method were as follows.
score  score
L 毛はほとんどま く、 僅かに軟毛が見 られるのみ 乙あ O  L Hair is almost round and only a little soft hair is seen.
2. 脱毛部位に多数の軟毛と催かに硬毛が見られる a 脱毛部位に密集して軟毛があ ]?半教程度の硬毛 が見られる β 2. a number of pubescence and Organized or to fluff densely in a hair loss site of terminal hairs can be seen there in the hair removal site]? Β half teaching about terminal hairs can be seen
硬毛で全体が覆われて るが頭皮がすけて見え The whole is covered with hard hairs, but the scalp looks soaked
10 Ten
5. 脱毛斑、 薄毛の状態がまった く見 られな 。 被検者^ 1 と 2 は円形脱毛症患者の脘毛班部位を用 ¾、 ■/¾ 3 と 4 は男性型脱毛患者の脱毛部位で行 ¾つ 次表 - Eに試験結果を示す。 5. No spots of baldness and thinning hair. Subjects ^ 1 and 2 use hair spots of alopecia areata patients, and ■ / ¾ 3 and 4 are hair loss sites of male pattern hair loss patients. The following Table-E shows the test results.
X5  X5
表 - S  Table-S
O O
Figure imgf000009_0001
S 上記両試験例に示すごと く 、 本発明養毛化粧料は明 らか ¾養毛 * 発毛効果を有し、 便れた養毛化粧料であ る ことがわかる。
Figure imgf000009_0001
S As shown in the above two test examples, the hair growth cosmetic of the present invention is clear. * Hair growth * It has a hair growth effect, indicating that it is a convenient hair growth cosmetic.

Claims

請 求 の 範 囲 The scope of the claims
L 有効成分と して 7 - ク ロ 口 - 3 - メ チル - 2 Η - 1* 2, 4 - ペ ン チア ジア ジ ン - 1,1 - ジォキ シ ドを含有 するこ とを特徴とする養毛化粧料。  L Nutrition characterized by containing 7-cloth-3 -methyl-2Η-1 * 2,4-penthiadiazine-1,1-dioxide as active ingredient Hair cosmetics.
χο χο
15  Fifteen
S毒  S poison
2S  2S
PCT/JP1987/000804 1987-10-20 1987-10-20 Diazoxide-containing hair care product WO1989003668A1 (en)

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Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5665811A (en) * 1979-10-23 1981-06-03 Wella Ag Hair and scalp conditioning cosmetic

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5665811A (en) * 1979-10-23 1981-06-03 Wella Ag Hair and scalp conditioning cosmetic

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