JP5066552B2 - Hair restorer additive and hair restorer composition - Google Patents
Hair restorer additive and hair restorer composition Download PDFInfo
- Publication number
- JP5066552B2 JP5066552B2 JP2009134744A JP2009134744A JP5066552B2 JP 5066552 B2 JP5066552 B2 JP 5066552B2 JP 2009134744 A JP2009134744 A JP 2009134744A JP 2009134744 A JP2009134744 A JP 2009134744A JP 5066552 B2 JP5066552 B2 JP 5066552B2
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- Prior art keywords
- hair
- hair restorer
- additive
- composition
- group
- 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 - Fee Related
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- Cosmetics (AREA)
Description
本発明は、育毛剤用添加剤及び育毛剤組成物に関し、さらに詳しくは、特定のシリコーン系化合物からなり、育毛剤に添加することにより、従来よりも薬効成分の使用量を減少させても十分な育毛効果が得られるため、副作用を減らすことができる育毛剤用添加剤及びそれを配合した育毛剤組成物に関する。 The present invention relates to an additive for hair restorer and a hair restorer composition, and more specifically, consists of a specific silicone compound, and it is sufficient to add to the hair restorer to reduce the amount of medicinal ingredients used than before. The present invention relates to an additive for hair restorer that can reduce side effects because a good hair restorer effect can be obtained, and a hair restorer composition containing the same.
従来より、禿や脱毛の原因を取り除く、あるいは、軽減するために、各種薬効成分を配合した養毛剤が知られ、広く使用さている。しかし、育毛剤中の薬効成分は副作用が発生する可能性のあるものが多い。例えば、近年広く使用される様になったミノキシジル(2,4−ジアミノ−6−ピペリジノピリミジン−3−オキサイド)は、本来、高血圧の治療薬として開発された医薬なので、育毛剤として使用する場合は、逆にミノキシジルの本来の薬効である血圧降下作用が好ましくない作用として問題となる。 Conventionally, in order to remove or reduce the cause of wrinkles and hair loss, hair nourishing agents containing various medicinal ingredients have been known and widely used. However, many medicinal ingredients in hair restorers may cause side effects. For example, minoxidil (2,4-diamino-6-piperidinopyrimidine-3-oxide), which has become widely used in recent years, is a drug originally developed as a therapeutic agent for hypertension and is therefore used as a hair restorer. In this case, the blood pressure lowering action, which is the original medicinal effect of minoxidil, becomes a problem as an undesirable action.
本発明の目的は、十分な育毛効果を維持しつつ、薬効成分の使用量を少なくすることにより、副作用の恐れの少ない安価な育毛剤組成物を提供することにある。 An object of the present invention is to provide an inexpensive hair-restoring composition with less fear of side effects by reducing the amount of medicinal ingredients while maintaining a sufficient hair-restoring effect.
本発明者等は、上記課題を解決すべく鋭意研究を重ねた結果、育毛剤組成物に特定の構造のシリコーン系化合物を配合することにより、薬効成分の使用量を減らしても十分な育毛作用が得られることを見出した。そして、本発明は、この知見に基づいて完成に至ったものである。 As a result of intensive studies to solve the above problems, the present inventors have incorporated a silicone compound having a specific structure into the hair restorer composition, so that sufficient hair restoring action can be achieved even when the amount of medicinal ingredients is reduced. It was found that can be obtained. The present invention has been completed based on this finding.
すなわち、本発明によれば、次の一般式(II)で表される育毛剤用添加剤が提供される。 That is, according to the present invention, an additive for hair restorer represented by the following general formula (II) is provided.
また、本発明によれば、薬効成分と、組成物全量基準で0.01〜0.2重量%の上記の育毛剤用添加剤を含有することを特徴とする育毛剤組成物が提供される。
さらに、本発明によれば、組成物全量基準で、上記薬効成分であるミノキシジルの含有量が0.05〜2重量%であり、上記育毛剤用添加剤の含有量が0.02〜2重量%であることを特徴とする上記の育毛剤組成物が提供される。
In addition, according to the present invention, there is provided a hair restorer composition comprising a medicinal component and 0.01 to 0.2% by weight of the above-mentioned additive for hair restorer based on the total amount of the composition. .
Furthermore, according to the present invention, based on the total amount of the composition, the content of minoxidil as the medicinal component is 0.05 to 2% by weight, and the content of the hair restorer additive is 0.02 to 2% by weight. % Of the hair-restoring composition described above.
本発明の育毛剤用添加剤を添加することにより、育毛剤中の薬効成分を減らしても十分な発毛効果が得られるという利点を有する。そのため、本発明の育毛剤用添加剤およびそれを配合した育毛剤組成物は産業上非常に有用である。 By adding the additive for hair restorer of this invention, even if it reduces the medicinal component in a hair restorer, it has the advantage that sufficient hair growth effect is acquired. Therefore, the additive for hair restorer of this invention and the hair restorer composition which mix | blended it are very useful industrially.
以下に、本発明を詳細に説明する。
本発明の育毛剤用添加剤は、次の一般式(I):
The present invention is described in detail below.
The additive for hair restorer of the present invention has the following general formula (I):
上記一般式(I)の式中、R1の一つ以上は炭素原子数6〜30のアルキル基又は−YO(C2H4O)a(C3H6O)bR3で表される基であることが必須である。残りのR1の好ましいものはメチル基、エチル基、フェニル基又は(R2)3SiO−で表される基であるが、特に好ましくはメチル基または(CH3)3SiO−である。
R2は炭素原子数1〜5のアルキル基またはアリール基を表すが、好ましくは炭素原子数1〜3のアルキル基であり、特にはメチル基である。
R3は水素原子あるいは炭素数1〜6のアルキル基又はアセトキシ基を表すが、好ましくは水素原子、メチル基、ブチル基である。
Yの好ましい例としては−CH2CH2CH2−、−CH2CH(CH3)CH2−が挙げられ、特には−CH2CH2CH2−が好ましい。
mは平均で1〜50であることが必須であるが、好ましくは1〜5である。
a及びbはそれぞれ平均で0〜50の数を示し、a+b≧2であるが、好ましくはaは2〜20、bは0〜10である。
In the general formula (I), at least one R 1 is represented by an alkyl group having 6 to 30 carbon atoms or —YO (C 2 H 4 O) a (C 3 H 6 O) b R 3. It is essential to be a group. The remaining R 1 is preferably a methyl group, an ethyl group, a phenyl group or a group represented by (R 2 ) 3 SiO—, and particularly preferably a methyl group or (CH 3 ) 3 SiO—.
R 2 represents an alkyl group having 1 to 5 carbon atoms or an aryl group, preferably an alkyl group having 1 to 3 carbon atoms, particularly a methyl group.
R 3 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or an acetoxy group, preferably a hydrogen atom, a methyl group, or a butyl group.
Preferred examples of Y include —CH 2 CH 2 CH 2 — and —CH 2 CH (CH 3 ) CH 2 —, and —CH 2 CH 2 CH 2 — is particularly preferred.
Although it is essential that m is 1 to 50 on average, it is preferably 1 to 5.
a and b each represent an average number of 0 to 50 and a + b ≧ 2, but preferably a is 2 to 20 and b is 0 to 10.
上記一般式(I)で表される化合物の中でも、特に下記一般式(II): Among the compounds represented by the above general formula (I), in particular the following general formula (II):
で表されるものが好ましい。
具体的には下記式で表される化合物1〜化合物3が好ましいものとして挙げられる。
化合物1
The thing represented by these is preferable.
Specifically, compounds 1 to 3 represented by the following formula are preferred.
Compound 1
本発明の育毛剤用添加剤は、育毛剤に添加することにより、その薬効成分の使用量を低減することが可能である。育毛剤は、限定されないが、従来公知の育毛剤が使用可能である。育毛剤とは、通常、薬効成分、溶剤、その他添加剤からなる。 The additive for hair restorer of this invention can reduce the usage-amount of the medicinal component by adding to a hair restorer. Although a hair restorer is not limited, a conventionally well-known hair restorer can be used. A hair restorer usually consists of medicinal ingredients, solvents, and other additives.
例えば、薬効成分として、賦形剤、血管拡張剤(ミノキシジル、塩化カルプロニウム、ニコチン酸ベンジル、センブリ抽出液、オタネニンジンエキス、ビタミンEアセテート、トウガラシチンキなど)、抗ヒスタミン剤(塩酸ジフェンヒドラミン、塩酸イソチペンジルなど)、抗炎症剤(グリチルレチン酸、グアイアズレンなど)、角質溶解剤(尿素、サリチル酸など)、殺菌剤(グルコン酸クロルヘキシジン、イソプロピルメチルフェノール、第4級アンモニウム塩、ヒノキチオール、ピロクトンオラミンなど)、保湿剤(ヒアルロン酸ナトリウム、コンドロイチン硫酸など)、各種動植物(イチイ、ボタンピ、カンゾウ、オトギリソウ、附子、ビワ、カワラヨモギ、コンフリー、アシタバ、サフラン、サンシシ、ローズマリー、セージ、モッコウ、セイモッコウ、ホップ、プラセンタなど)の抽出物、ビタミン類(酢酸レチノール、塩酸ピリドキシン、アスコルビン酸、硝酸チアミン、シアノコバラミン、ビオチンなど)が挙げられる。 Examples of medicinal ingredients include excipients, vasodilators (minoxidil, carpronium chloride, benzyl nicotinate, assembly extract, ginseng extract, vitamin E acetate, red pepper tincture, etc.), antihistamines (diphenhydramine hydrochloride, isothipentyl hydrochloride, etc.), anti Inflammatory agents (such as glycyrrhetinic acid and guaiazulene), keratolytic agents (such as urea and salicylic acid), bactericides (such as chlorhexidine gluconate, isopropylmethylphenol, quaternary ammonium salts, hinokitiol and piroctone olamine), moisturizers (hyaluron) Acid sodium, chondroitin sulfate, etc., various animals and plants (yew, buttonpi, licorice, hypericum, appendix, loquat, sagebrush, comfrey, ashitaba, saffron, sanshishi, rosemary, sage, Kkou, Seimokkou, hops, extract of placenta, etc.), vitamins (retinol acetate, pyridoxine hydrochloride, ascorbic acid, thiamin nitrate, cyanocobalamin, biotin) can be mentioned.
溶剤として、水、アルコール類(メタノール、エタノール、2−プロパノール、変性エタノール等)、環状シロキサン類(デカメチルシクロペンタシロキサン等)が挙げられる。これらの内、水、エタノール又は2−プロパノールが好ましい。 Examples of the solvent include water, alcohols (such as methanol, ethanol, 2-propanol, and modified ethanol), and cyclic siloxanes (such as decamethylcyclopentasiloxane). Of these, water, ethanol or 2-propanol is preferred.
その他添加剤として、抗酸化剤(ジブチルヒドロキシトルエン、ピロ亜硫酸ナトリウム、トコフェロール、エデト酸ナトリウム、アスコルビン酸、イソプロピルガレートなど)、溶解補助剤(アジピン酸ジイソプロピル、ミリスチン酸イソプロピル、ポリエチレングリコール、中鎖脂肪酸トリグリセリド、脂肪酸エステル類、各種植物油、各種動物油、多価アルコール脂肪酸エステル、アルキルグリセリルエーテル、炭化水素類、乳酸、水酸化ナトリウムなど)、代謝賦活剤(パンテノールなど)、界面活性剤(ソルビタン脂肪酸エステル、グリセリン脂肪酸エステル、ポリグリセリン脂肪酸エステル、プロピレングリコール脂肪酸エステル、ポリオキシエチレンソルビタン脂肪酸エステル、ポリオキシエチレンソルビット脂肪酸エステル、ポリオキシエチレングリセリン脂肪酸エステル、ポリエチレングリコール脂肪酸エステル、ポリオキシエチレンアルキルエーテル、ポリオキシエチレンポリオキシプロピレンアルキルエーテル、ポリオキシエチレンアルキルフェニルエーテル、ポリオキシエチレン硬化ヒマシ油、ポリオキシエチレンヒマシ油、ポリオキシエチレンミツロウ誘導体、ポリオキシエチレンラノリン誘導体、ポリオキシエチレンアルキルアミド、ポリオキシエチレンアルキルアミン、レシチン誘導体、高分子乳化剤など)、乳化安定剤(高級アルコールなど)、ゲル化剤(水溶性高分子など)、粘着剤、香料、清涼化剤(メントール、ハッカ油、カンフルなど)、染料などの通常使用される成分を本発明の効果を損なわない範囲で配合することができる。 Other additives include antioxidants (dibutylhydroxytoluene, sodium pyrosulfite, tocopherol, sodium edetate, ascorbic acid, isopropyl gallate, etc.), solubilizers (diisopropyl adipate, isopropyl myristate, polyethylene glycol, medium chain fatty acid triglycerides) , Fatty acid esters, various vegetable oils, various animal oils, polyhydric alcohol fatty acid esters, alkyl glyceryl ethers, hydrocarbons, lactic acid, sodium hydroxide, etc., metabolic activators (pantenol, etc.), surfactants (sorbitan fatty acid esters, Glycerin fatty acid ester, polyglycerin fatty acid ester, propylene glycol fatty acid ester, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene sorbit fatty acid ester, Reoxyethylene glycerin fatty acid ester, polyethylene glycol fatty acid ester, polyoxyethylene alkyl ether, polyoxyethylene polyoxypropylene alkyl ether, polyoxyethylene alkylphenyl ether, polyoxyethylene hydrogenated castor oil, polyoxyethylene castor oil, polyoxyethylene Beeswax derivatives, polyoxyethylene lanolin derivatives, polyoxyethylene alkylamides, polyoxyethylene alkylamines, lecithin derivatives, polymer emulsifiers, etc.), emulsion stabilizers (such as higher alcohols), gelling agents (such as water-soluble polymers), Commonly used components such as pressure-sensitive adhesives, fragrances, refreshing agents (menthol, mint oil, camphor, etc.), dyes and the like can be blended within a range that does not impair the effects of the present invention.
本発明の育毛剤用添加剤の添加量は、限定されないが、好ましくは育毛剤中に0.01〜2重量%、特に好ましくは0.02〜0.2重量%となる量を添加して使用できる。 The addition amount of the hair growth additive of the present invention is not limited, but preferably 0.01 to 2% by weight, particularly preferably 0.02 to 0.2% by weight is added to the hair growth agent. Can be used.
本発明の育毛剤用添加剤を育毛剤に添加する場合、添加方法は限定されず、通常の方法により混合して添加可能である。また、育毛剤に直接添加しても良いが、予め溶剤に溶解させてから使用することもできる。溶剤としては前記の育毛剤に使用されるものが使用可能である。また、市販の育毛剤は、保存安定性を考慮した処方となっているので、本発明の育毛剤用添加剤を添加すると系のバランスが崩れ、安定性が低下する場合がある。従って、本発明の育毛剤用添加剤又はその溶液を使用時に育毛剤に添加し混合して用いても良い。
上記の薬効成分、溶剤及び育毛剤用添加剤、更に必要に応じてその他添加剤からなる育毛剤組成物もまた、本発明の一形態である。
When the hair growth additive of the present invention is added to the hair growth agent, the addition method is not limited and can be mixed and added by a normal method. Moreover, although you may add directly to a hair restorer, it can also be used, after making it melt | dissolve in a solvent previously. As the solvent, those used for the above-mentioned hair restorer can be used. Moreover, since the commercially available hair restorer has a formulation that takes into account storage stability, the addition of the hair restorer additive of the present invention may disrupt the balance of the system and reduce the stability. Therefore, the hair restorer additive of the present invention or a solution thereof may be added to and mixed with the hair restorer at the time of use.
A hair restorer composition comprising the above-mentioned medicinal ingredients, solvent and hair restorer additive, and other additives as required is also an embodiment of the present invention.
薬効成分の配合量は、その種類により異なるが、例えばミノキシジルの場合は0.05〜2重量%であることが好ましく、塩化カルプロニウムの場合は0.25〜2重量%であることが好ましい。また、育毛剤用添加剤の配合量は上記の通りである。 The compounding amount of the medicinal component varies depending on the type, but for example, it is preferably 0.05 to 2% by weight in the case of minoxidil, and preferably 0.25 to 2% by weight in the case of carpronium chloride. Moreover, the compounding quantity of the additive for hair restorer is as above-mentioned.
本発明の育毛剤用添加剤が作用するメカニズムは明らかでないが、従来の育毛剤中の薬効成分は主に頭皮から経皮吸収されて毛乳頭に作用していたのに対し、本発明の育毛剤用添加剤を配合すると、毛根と毛包の間の極めて狭い隙間に浸透しやすいため、経皮吸収に加えて直接毛乳頭に到達する事ができ、その結果、薬効成分が効率良く毛乳頭に作用し、薬効成分の少ない使用量でも十分な効果が発揮されるものと推察される。 Although the mechanism by which the hair restorer additive of the present invention acts is not clear, the medicinal ingredients in conventional hair restorers were absorbed percutaneously mainly from the scalp and acted on the hair papilla, whereas the hair restorer of the present invention When blended with a pharmaceutical additive, it can easily penetrate into the narrow gap between the hair root and the hair follicle, so it can reach the hair papilla directly in addition to percutaneous absorption. It is presumed that sufficient effects are exerted even with a small amount of medicinal ingredients.
以下、実施例により更に本発明を詳細に説明するが、本発明の主旨を越えない限り、これらに限定されるものではない。 EXAMPLES Hereinafter, the present invention will be described in more detail with reference to examples, but the present invention is not limited to these examples as long as the gist of the present invention is not exceeded.
[育毛剤組成物の調製]
表1(実施例1、2は参考例)に示した処方で、ミノキシジルに、他の成分を配合し、無水エタノールおよび精製水で全量を100mlとし、撹拌溶解してローションタイプの外用剤を調製した。
[Preparation of hair restorer composition]
In the formulation shown in Table 1 (Examples 1 and 2 are reference examples), other ingredients are added to minoxidil, and the total amount is made up to 100 ml with absolute ethanol and purified water, and stirred to prepare a lotion-type external preparation. did.
[発毛試験]
C3H系マウス(雄性、7週齢)10匹を一群とし、各群の動物について、その背部の2×3cmの範囲をバリカンで除毛し試験に供した。表1の処方の各々にそれぞれ個別の群の動物を割り当て、その除毛部に1日1回、0.2mlずつ20日間塗布した。
試験に使用した動物の体毛は黒色で、除毛部の皮膚の色は茶色であり、その毛の成長と共に灰色から黒色に色調が変化することから、毛の色の黒さの程度を肉眼により、0:発毛が全く認められない、1:発毛している、2:硬毛が生え揃っている、3:硬毛が正常の約50%生えている、4:硬毛が正常の約70%生えている、5:硬毛が正常のほぼ100%生えている、の6段階で評価した。結果を表1に示した。
[Hair growth test]
A group of 10 C3H mice (male, 7 weeks old) was used as a group, and the 2 × 3 cm area of the back of each group of animals was removed with a clipper and subjected to the test. An individual group of animals was assigned to each of the formulations in Table 1, and 0.2 ml was applied to the hair removal site once a day for 20 days.
The body hair of the animal used in the test was black and the skin color of the hair removal part was brown, and the color tone changed from gray to black with the growth of the hair, so the degree of blackness of the hair color was visually examined. , 0: no hair growth is observed, 1: hair is growing, 2: hair is grown, 3: hair is about 50% normal, 4: hair is normal The evaluation was made on a 6-point scale: about 70% growing, 5: almost 100% normal hair growing. The results are shown in Table 1.
表1から明らかなように、本発明の育毛剤用添加剤を添加した育毛剤組成物は、配合しないものよりも薬効成分を減らしても十分な発毛効果が得られることが確認された。 As is clear from Table 1, it was confirmed that the hair restorer composition to which the additive for hair restorer of the present invention was added could obtain a sufficient hair growth effect even if the medicinal components were reduced compared to those not blended.
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