JP2005314323A - Hair growth formulation - Google Patents

Hair growth formulation Download PDF

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JP2005314323A
JP2005314323A JP2004135662A JP2004135662A JP2005314323A JP 2005314323 A JP2005314323 A JP 2005314323A JP 2004135662 A JP2004135662 A JP 2004135662A JP 2004135662 A JP2004135662 A JP 2004135662A JP 2005314323 A JP2005314323 A JP 2005314323A
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minoxidil
hair
propylene glycol
composition
hair growth
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Hidehito Yamazaki
秀仁 山崎
Satoshi Nishijima
聡 西島
Hiroyasu Cho
博康 長
Fusae Shizume
二左枝 鎮目
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Sato Pharmaceutical Co Ltd
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Sato Pharmaceutical Co Ltd
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Abstract

<P>PROBLEM TO BE SOLVED: To provide a hair growth formulation which contains minoxidil and has a high hair growth effect and an excellent application texture. <P>SOLUTION: The hair growth formulation is one containing minoxidil, propylene glycol, and a volatile solvent, wherein the propylene glycol is contained in an amount larger than 5 times and smaller than 10 times (in terms of a mass ratio) that of the minoxidil. <P>COPYRIGHT: (C)2006,JPO&NCIPI

Description

本発明は、ミノキシジルを有効成分とする育毛効果の高い育毛剤組成物に関する。   The present invention relates to a hair restorer composition having a high hair growth effect comprising minoxidil as an active ingredient.

ミノキシジル(化学名:6−(1−ピペリジニル)−2,4−ピリミジンジアミン−3−オキサイド)は末梢血管拡張作用を有しており、高血圧症治療のための経口降圧剤として使用される一方、副作用としての多毛が注目され、育毛剤としての適応も提案されている(例えば、米国特許第4,139,619号、米国特許第4,695,812号)。以来、育毛剤におけるミノキシジルの至適濃度の検討(例えば、武田 克之らによる“男性型脱毛症に対するミノキシジル外用剤の二重盲検試験による至適濃度の検討I”(臨床医薬、1992年、第8巻、第7号、p.1597−1623)、および、同じく武田 克之らによる“男性型脱毛症に対するミノキシジル1%ローション剤および2%ローション剤の長期外用における有用性の検討”(Progress in Medicine、1992年、第12巻、第7号、p.1553−1565))等の積極的な検討がなされ、現在では既に幾つかのミノキシジル含有育毛剤が市販されている(例えば、1%のミノキシジルを含有するRiUP(登録商標)(大正製薬(株)製)、5%のミノキシジルを含有するRogaine(Phamacia&Upjoin製))。   While minoxidil (chemical name: 6- (1-piperidinyl) -2,4-pyrimidinediamine-3-oxide) has a peripheral vasodilatory action, it is used as an oral antihypertensive for the treatment of hypertension, Hairy as a side effect has attracted attention, and indication as a hair restorer has also been proposed (for example, US Pat. No. 4,139,619, US Pat. No. 4,695,812). Since then, studies on the optimal concentration of minoxidil in hair growth agents (for example, “Study on the optimal concentration of a topical preparation of minoxidil for male pattern baldness in double-blind studies by Katsuyuki Takeda I” (clinical medicine, 1992, No. 1) Vol. 8, No. 7, pp. 1597-1623) and Katsuyuki Takeda et al. “Study on the usefulness of minoxidil 1% lotion and 2% lotion for long-term external use for male pattern baldness” (Progress in Medicine) 1992, Vol. 12, No. 7, p.1553-1565)), and some minoxidil-containing hair restoration agents are already commercially available (for example, 1% minoxidil). Containing RiUP (registered trademark) (made by Taisho Pharmaceutical Co., Ltd.), Rogaine containing 5% minoxidil (Phama Made ia & Upjoin)).

現在までに検討されてきたミノキシジル含有育毛剤の剤形は、ローション剤、ゼリー剤、軟膏剤、クリーム剤、スプレー剤、エアゾール剤、トニック剤等、広範囲に及んでおり、これらの育毛剤において、プロピレングリコールは溶剤として広範に利用されている。   The dosage forms of minoxidil-containing hair restorers that have been studied to date have been widely applied to lotions, jellies, ointments, creams, sprays, aerosols, tonics, etc. Propylene glycol is widely used as a solvent.

米国特許第4,139,619号明細書US Pat. No. 4,139,619 米国特許第4,695,812号明細書US Pat. No. 4,695,812 臨床医薬、1992年、第8巻、第7号、p.1597−1623Clinical Medicine, 1992, Vol. 8, No. 7, p. 1597-1623 Progress in Medicine、1992年、第12巻、第7号、p.1553−1565Progress in Medicine, 1992, Vol. 12, No. 7, p. 1553-1565

ところで、これらミノキシジル含有育毛剤における育毛効果の向上は、主として育毛剤におけるミノキシジルの使用量を増加させることによって行なわれてきた。しかし、プロピレングリコールの使用量については詳細に検討されておらず、それぞれの剤形に応じて適宜選択されているにすぎない。わずかにプロピレングリコールの作用による接触性皮膚炎が懸念されること(上述の非特許文献1、2参照)が知られていることから、上述の市販の育毛剤では、プロピレングリコールがミノキシジルに対して質量比で10倍の量で使用されている。   By the way, the improvement of the hair-growth effect in these minoxidil-containing hair-growth agents has been carried out mainly by increasing the amount of minoxidil used in the hair-growth agent. However, the amount of propylene glycol used has not been studied in detail, and is only appropriately selected according to each dosage form. Since it is known that contact dermatitis due to the action of propylene glycol is slightly concerned (see Non-Patent Documents 1 and 2 above), in the above-mentioned commercially available hair restorer, propylene glycol is less than minoxidil. It is used in a mass ratio of 10 times.

発明者等は、これまで検討されてこなかったプロピレングリコールによって育毛効果が変化し得るのではないかと考えた。従って、本発明の課題は、ミノキシジルの育毛効果が十分に発揮された育毛効果の高い育毛剤であって、しかも使用感に優れた育毛剤を提供することである。   The inventors thought that the hair-growth effect could be changed by propylene glycol which has not been studied so far. Accordingly, an object of the present invention is to provide a hair-restoring agent having a high hair-growth effect in which the hair-growth effect of minoxidil is sufficiently exerted, and having an excellent usability.

発明者等は鋭意検討した結果、意外にも、プロピレングリコールの量によってミノキシジルの経皮吸収性が変化し、ミノキシジルの育毛効果が影響を受けることを発見した。そして、ミノキシジル、プロピレングリコール、および揮発性溶剤を含有する育毛剤組成物において、プロピレングリコールをミノキシジルに対して質量比で5倍より多く10倍より少ない量に調整することにより、上述の課題が達成され、育毛効果が高い上に使用感に優れた育毛剤が得られることを発見し、発明を完成させるに至った。尚、本明細書に関する限り、“揮発性溶剤”と言う語は、プロピレングリコールと相溶性があり、かつプロピレングリコールとの混合物の状態でミノキシジルを溶解する化合物であって、化合物単独での沸点が100℃以下であるような化合物、または、このような化合物の混合物を意味する。本発明では、揮発性溶剤は、エタノール、水、および、エタノールと水との混合物、からなる群から選択されるのが、育毛剤組成物の使用感の点から好ましい。   As a result of intensive studies, the inventors have unexpectedly discovered that the amount of propylene glycol changes the transdermal absorbability of minoxidil and affects the hair growth effect of minoxidil. And in the hair restorer composition containing a minoxidil, propylene glycol, and a volatile solvent, the above-mentioned subject is achieved by adjusting propylene glycol to a quantity ratio of more than 5 times and less than 10 times with respect to minoxidil. As a result, it was discovered that a hair-growth agent with high hair-growth effect and excellent usability was obtained, and the present invention was completed. As far as this specification is concerned, the term “volatile solvent” is a compound that is compatible with propylene glycol and dissolves minoxidil in a mixture with propylene glycol, and the boiling point of the compound alone is low. It means a compound that is 100 ° C. or lower, or a mixture of such compounds. In the present invention, the volatile solvent is preferably selected from the group consisting of ethanol, water, and a mixture of ethanol and water from the viewpoint of the feeling of use of the hair restorer composition.

育毛剤組成物においてプロピレングリコールがミノキシジルに対して質量比で5倍以下の量で含有されていると、十分に高い育毛効果を示す育毛剤組成物が得られない。発明者等の検討によると、プロピレングリコールの量が少ない場合に育毛効果が低下するのは、育毛剤組成物を頭皮等の皮膚上に適用した直後にミノキシジルが急激に体内に吸収されてしまうことが原因となっていると考えられる。言い換えると、ミノキシジルがある程度ゆっくり体内に吸収されて初めてミノキシジルの育毛効果が十分に発揮されると考えられる。また、育毛剤組成物においてプロピレングリコールがミノキシジルに対して質量比で10倍以上の量で含有されていると、育毛効果の向上がもはや望まれない上に、育毛剤を頭皮等に適用した際にベタついて使用感が低下する。さらには、上述のような接触性皮膚炎の発症も懸念される。   If the propylene glycol is contained in the hair growth composition in an amount of 5 times or less by mass ratio with respect to minoxidil, a hair growth composition showing a sufficiently high hair growth effect cannot be obtained. According to the study by the inventors, when the amount of propylene glycol is small, the hair-growth effect decreases because minoxidil is rapidly absorbed into the body immediately after applying the hair-growth composition on the skin such as the scalp. Is considered to be the cause. In other words, it is considered that the hair growth effect of minoxidil is fully exhibited only after minoxidil is absorbed into the body slowly to some extent. Moreover, when propylene glycol is contained in a mass ratio of 10 times or more with respect to minoxidil in the hair restorer composition, an improvement in the hair restore effect is no longer desired, and when the hair restorer is applied to the scalp, etc. The feeling of use is reduced due to stickiness. Furthermore, there is concern about the development of contact dermatitis as described above.

プロピレングリコールの量が少ない場合にミノキシジルが急激に体内に吸収されてしまう理由は、以下のように考えられる。育毛剤組成物を皮膚上に適用すると、ミノキシジルを溶解しているプロピレングリコールと揮発性溶剤との混合物のうち揮発性溶剤が適用直後に優先的に蒸発してしまう。その結果、ミノキシジルは主としてプロピレングリコールに溶解した状態で皮膚上に存在することになる。プロピレングリコールの量が少ない場合には、皮膚表面上に局所的にミノキシジルが極めて高濃度で存在することになるため、ミノキシジルの経皮吸収性が大幅に上がるものと考えられる。ミノキシジルの急激な体内への吸収は、上述のようにミノキシジルが降圧剤としても作用することを考慮すると、循環器系への影響も懸念される。   The reason why minoxidil is rapidly absorbed in the body when the amount of propylene glycol is small is considered as follows. When the hair restorer composition is applied onto the skin, the volatile solvent in the mixture of propylene glycol and mincedil dissolving minoxidil preferentially evaporates immediately after application. As a result, minoxidil is present on the skin mainly dissolved in propylene glycol. When the amount of propylene glycol is small, minoxidil is locally present at a very high concentration on the skin surface, and it is considered that the transdermal absorbability of minoxidil is greatly increased. The rapid absorption of minoxidil into the body is also concerned about the influence on the circulatory system, considering that minoxidil acts as a hypotensive agent as described above.

本発明の育毛剤組成物において、プロピレングリコールがミノキシジルに対して質量比で7倍より多く10倍より少ない量で含有されているのが特に好ましい。   In the hair restorer composition of the present invention, it is particularly preferable that propylene glycol is contained in an amount of more than 7 times and less than 10 times by mass ratio with respect to minoxidil.

本発明の育毛剤組成物において、ミノキシジルは、育毛剤組成物100mLに対して0.1〜7gの量で含有されているのが望ましい。ミノキシジルの含有量が上述の範囲未満であると、育毛効果が不充分になる。また、ミノキシジルの含有量が高いほどミノキシジルの循環器系への影響が懸念される。   In the hair restorer composition of the present invention, it is desirable that minoxidil is contained in an amount of 0.1 to 7 g with respect to 100 mL of the hair restorer composition. When the content of minoxidil is less than the above range, the hair-growth effect is insufficient. In addition, the higher the content of minoxidil, there is concern about the influence of minoxidil on the circulatory system.

本発明の育毛剤組成物の剤形には特に限定がないが、特にミノキシジル含有量が組成物100mLに対して3〜7gと高い場合には、ローション剤またはゼリー剤であるのが望ましい。   The dosage form of the hair restorer composition of the present invention is not particularly limited, but it is preferably a lotion agent or a jelly agent particularly when the minoxidil content is as high as 3 to 7 g with respect to 100 mL of the composition.

本発明によると、ミノキシジルの育毛効果が十分に発揮された育毛効果の高い育毛剤が提供される。また、頭皮等に適用した際の使用感に優れた育毛剤が提供される。   According to the present invention, there is provided a hair restorer having a high hair-growth effect in which the hair-growth effect of minoxidil is sufficiently exhibited. Moreover, the hair restorer excellent in the usability | use_condition at the time of applying to a scalp etc. is provided.

本発明の育毛剤組成物は、育毛有効成分としてのミノキシジルの他、プロピレングリコール、および揮発性溶剤を少なくとも含有する。   The hair restorer composition of the present invention contains at least propylene glycol and a volatile solvent in addition to minoxidil as a hair restorer active ingredient.

本発明の育毛剤組成物において、ミノキシジルは、育毛剤組成物100mLに対して0.1〜7g、好ましくは0.5〜6g、特に好ましくは1〜5gの範囲になるように配合するのが望ましい。この範囲内で十分な育毛効果が得られる。   In the hair restorer composition of the present invention, minoxidil is blended so as to be in the range of 0.1 to 7 g, preferably 0.5 to 6 g, particularly preferably 1 to 5 g, per 100 mL of the hair restorer composition. desirable. A sufficient hair-growth effect can be obtained within this range.

本発明の育毛剤組成物において、プロピレングリコールは、ミノキシジルに対して、質量比で、5倍より多く10倍より少ない範囲、好ましくは6倍より多く10倍より少ない範囲、特に好ましくは7倍より多く10倍より少ない範囲になるように配合される。プロピレングリコールのミノキシジルに対する配合比が上述の範囲より小さいと、十分に高い育毛効果を示す育毛剤組成物が得られず、上述の範囲より多いと、育毛効果の向上がもはや望まれない上に、育毛剤を頭皮等に適用した際にベタついて使用感が低下する。   In the hair growth composition of the present invention, propylene glycol is in a mass ratio with respect to minoxidil in a range of more than 5 times and less than 10 times, preferably more than 6 times and less than 10 times, particularly preferably more than 7 times. It is blended so that it is less than 10 times more. If the blending ratio of propylene glycol to minoxidil is smaller than the above range, a hair restorer composition exhibiting a sufficiently high hair restoring effect cannot be obtained, and if it is more than the above range, an improvement in hair restoring effect is no longer desired. When a hair restorer is applied to the scalp, etc., it becomes sticky and the feeling of use decreases.

本発明の育毛剤組成物に配合される揮発性溶剤としては、エタノール、水、プロピルアルコール、イソプロピルアルコール、s−ブチルアルコール、t−ブチルアルコール等が挙げられる。育毛剤を頭皮等に適用した際の使用感の点から、揮発性溶剤は、エタノール、水、および、エタノールと水との混合物、からなる群から選択されるのが好ましい。   Examples of the volatile solvent blended in the hair restorer composition of the present invention include ethanol, water, propyl alcohol, isopropyl alcohol, s-butyl alcohol, and t-butyl alcohol. From the viewpoint of the feeling of use when the hair restorer is applied to the scalp and the like, the volatile solvent is preferably selected from the group consisting of ethanol, water, and a mixture of ethanol and water.

本発明の育毛剤組成物は、育毛有効成分としてのミノキシジル、プロピレングリコール、および揮発性溶剤を上述のような配合比で配合することにより調製される。本発明の育毛剤組成物の剤形には特に限定がなく、ローション剤、ゼリー剤、トニック剤、軟膏剤、クリーム剤、スプレー剤、エアゾール剤等を採用することができが、特にミノキシジル含有量が組成物100mLに対して3〜7gと比較的高い場合には、ローション剤またはゼリー剤であるのが望ましい。これらの剤形等に応じて、本発明の育毛剤組成物には、ミノキシジル、プロピレングリコール、および揮発性溶剤の必須成分に加えて、保湿剤、保存剤、界面活性剤、ゲル化剤、pH調整剤、酸化防止剤、清涼化剤、溶解補助剤、乳化安定剤、粘着剤、香料等を、本発明の効果を損なわない範囲で適宜配合することができる。   The hair restorer composition of the present invention is prepared by blending minoxidil, propylene glycol, and a volatile solvent as hair restoration active ingredients at the blending ratio as described above. The dosage form of the hair restorer composition of the present invention is not particularly limited, and a lotion agent, jelly agent, tonic agent, ointment, cream agent, spray agent, aerosol agent and the like can be adopted, but in particular the content of minoxidil Is a lotion agent or jelly agent when it is relatively high at 3 to 7 g per 100 mL of the composition. In accordance with these dosage forms, the hair growth composition of the present invention includes a moisturizer, preservative, surfactant, gelling agent, pH in addition to the essential components of minoxidil, propylene glycol, and volatile solvent. A regulator, an antioxidant, a refreshing agent, a solubilizing agent, an emulsion stabilizer, a pressure-sensitive adhesive, a fragrance, and the like can be appropriately blended within a range not impairing the effects of the present invention.

保湿剤としては、グリセリン、ジグリセリン、1,3−ブタンジオール、ヒアルロン酸ナトリウム、コンドロイチン硫酸等を使用することができ、保存剤としては、パラベン類、安息香酸塩類等を使用することができ、界面活性剤としては、ポリオキシエチレン硬化ヒマシ油、ポリオキシエチレンソルビタン脂肪酸エステル、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等を使用することができる。ゲル化剤としては、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロース、カルボキシビニルポリマー等を使用することができ、pH調整剤としては、トリエタノールアミン、ジイソプロパノールアミン、クエン酸、乳酸、燐酸等を使用することができる。酸化防止剤としては、ジブチルヒドロキシトルエン、ピロ亜硫酸ナトリウム、トコフェノール、エデト酸ナトリウム、イソプロピルガレート等を使用することができ、清涼化剤としてはメントール、ハッカ油、カンフル等を使用することができる。溶解補助剤としては、アジピン酸ジイソプロピル、ミリスチン酸イソプロピル、γ−シクロデキストリン等を使用することができる。   As humectants, glycerin, diglycerin, 1,3-butanediol, sodium hyaluronate, chondroitin sulfate, etc. can be used, and as preservatives, parabens, benzoates, etc. can be used, As the surfactant, polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitan fatty acid ester, glycerin fatty acid ester, propylene glycol fatty acid ester and the like can be used. Hydroxypropylcellulose, hydroxypropylmethylcellulose, carboxyvinyl polymer, etc. can be used as gelling agents, and triethanolamine, diisopropanolamine, citric acid, lactic acid, phosphoric acid, etc. can be used as pH adjusters. Can do. Dibutylhydroxytoluene, sodium pyrosulfite, tocophenol, sodium edetate, isopropyl gallate and the like can be used as the antioxidant, and menthol, peppermint oil, camphor and the like can be used as the cooling agent. As a solubilizer, diisopropyl adipate, isopropyl myristate, γ-cyclodextrin, and the like can be used.

本発明の育毛剤にはさらに、慣用の他の薬効成分、例えば血管拡張剤(塩化カルプロニウム、ニコチン酸ベンジル、オタネニンジンエキス、ビタミンEアセテート等)、代謝賦活剤(パンテノール、パントテン酸およびその誘導体等)、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等)、抗炎症剤(グアイアズレン、グリチルレチン酸等)、角質溶解剤(尿素、サリチル酸等)、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、ヒノキチオール、ピロクトンオラミン等)、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、ビオチン等)も、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。   The hair growth agent of the present invention further includes other conventional medicinal ingredients such as vasodilators (carpronium chloride, benzyl nicotinate, ginseng extract, vitamin E acetate, etc.), metabolic activators (panthenol, pantothenic acid and derivatives thereof, etc. ), Antihistamines (diphenhydramine hydrochloride, isothipentyl hydrochloride, etc.), anti-inflammatory agents (guaiazulene, glycyrrhetinic acid, etc.), keratolytic agents (urea, salicylic acid, etc.), fungicides (chlorhexidine gluconate, isopropylmethylphenol, hinokitiol, piroctone olamine) Etc.), vitamins (retinol acetate, pyridoxine hydrochloride, ascorbic acid, biotin, etc.) can also be incorporated within a range not impairing the effects of the present invention.

本発明の育毛剤組成物は、1日に1、2回程度、適量を皮膚表面に適用することにより使用される。   The hair restorer composition of the present invention is used by applying an appropriate amount to the skin surface about once or twice a day.

以下に、実施例を参照して本発明を具体的に説明するが、本発明はこれら実施例等により限定されない。   EXAMPLES The present invention will be specifically described below with reference to examples, but the present invention is not limited to these examples.

1.血中濃度の測定
以下の表1に示す組成で各化合物を配合した育毛溶液を調製した。
1. Measurement of blood concentration A hair growth solution was prepared by blending each compound with the composition shown in Table 1 below.

表1:育毛溶液の組成

Figure 2005314323
Table 1: Composition of hair growth solution
Figure 2005314323

Wistar系雄性ラット(7週令)を用いて、ミノキシジルの血中濃度測定を行なった。試験前日に動物用バリカンを使用して背部を毛刈りし、使用した。毛刈りしたラット背部(約4×6cm)に、表1の育毛溶液を500μL塗布し、塗布後、所定の時間(1、2、4、8時間)後に採血を行い、血清を得た。   The blood concentration of minoxidil was measured using Wistar male rats (7 weeks old). On the day before the test, the back was shaved with an animal clipper and used. 500 μL of the hair-growth solution shown in Table 1 was applied to the back of the shaved rat (about 4 × 6 cm), and blood was collected after a predetermined time (1, 2, 4, 8 hours) after application to obtain serum.

得られた血清サンプルは、前処理したカラムで固相抽出し、高速液体クロマトグラフィーにて定量を行なった。   The obtained serum sample was subjected to solid phase extraction with a pretreated column and quantified by high performance liquid chromatography.

図1に、測定結果を示す。図1より、育毛剤組成物におけるプロピレングリコール含有量のミノキシジル含有量に対する割合が大きいほど、一過性のミノキシジル血中濃度の上昇が抑えられることがわかる。   FIG. 1 shows the measurement results. From FIG. 1, it can be seen that as the ratio of the propylene glycol content to the minoxidil content in the hair growth composition increases, the transient increase in the blood concentration of minoxidil is suppressed.

2.育毛効果の確認試験
以下の表2〜4に示す組成で各化合物を配合し、育毛ローション剤を調製した。
2. Confirmation test of hair growth effect Each compound was mix | blended with the composition shown in the following Tables 2-4, and the hair growth lotion agent was prepared.

C3H/HeN系雄性マウス(7週令)を用いて、育毛効果確認のための試験を行なった。マウス麻酔を施した後、背部の毛刈りを行なった。毛刈りした翌日から、1日2回(午前と午後)、表2〜4のローション剤の100μLをマウス背部に塗布した。育毛作用は、塗布開始から66日後の発毛個体割合(%)により評価した。表2〜4に、以下の式により算出した発毛個体割合(%)をまとめた。   A test for confirming the hair-growth effect was performed using C3H / HeN male mice (7 weeks old). After the mouse was anesthetized, the back was shaved. From the next day after shaving, 100 μL of the lotions shown in Tables 2 to 4 were applied to the back of the mouse twice a day (morning and afternoon). The hair-growth effect was evaluated by the percentage of hair growth individuals (%) 66 days after the start of application. Tables 2 to 4 summarize the percentage of hair growth individuals (%) calculated by the following formula.

発毛個体割合(%)=各群の発毛個体数×100/各群の例数








Hair growth individual ratio (%) = number of hair growth individuals in each group × 100 / number of cases in each group








表2:ローション剤の組成と評価結果

Figure 2005314323
Table 2: Lotion preparation composition and evaluation results
Figure 2005314323

表3:ローション剤の組成と評価結果

Figure 2005314323
Table 3: Lotion preparation composition and evaluation results
Figure 2005314323

表4:ローション剤の組成と評価結果

Figure 2005314323
Table 4: Lotion preparation composition and evaluation results
Figure 2005314323

表2〜4より、ローション剤におけるプロピレングリコール含有量のミノキシジル含有量に対する割合が増加するにつれて発毛個体割合が増加する(育毛効果が高くなる)傾向にあるが、プロピレングリコール含有量のミノキシジル含有量に対する割合が10倍になるとむしろ育毛効果が低下してしまうことがわかる。さらに、本発明の育毛剤組成物(ローション剤)を使用すると、発毛個体割合が80%以上の良好な結果が得られていることがわかる。   From Tables 2 to 4, the proportion of propylene glycol content in the lotion tends to increase as the proportion of the propylene glycol content to the minoxidil content increases (the hair growth effect increases), but the propylene glycol content of minoxidil content It can be seen that when the ratio to the ratio is 10 times, the hair-growth effect is rather lowered. Furthermore, it can be seen that when the hair-growing composition (lotion) of the present invention is used, good results with a hair growth individual ratio of 80% or more are obtained.

実施例3〜8、対照2、3、および比較例3に関しては、上述の発毛個体割合(%)による評価の他、発毛部位面積の評価も行なった。表3、4に、塗布開始から66日後における発毛部位面積をまとめた。   Regarding Examples 3 to 8, Controls 2 and 3, and Comparative Example 3, in addition to the evaluation based on the above-mentioned hair growth individual ratio (%), the hair growth site area was also evaluated. Tables 3 and 4 summarize the hair growth site areas 66 days after the start of application.

表3、4より、ミノキシジルが組成物100mLに対して3g配合されているローション剤を使用した場合に比較して5g配合されているローション剤を使用した場合に、発毛部位面積が増加していることがわかる。また、ミノキシジルが組成物100mLに対して3g配合されているローション剤の場合には、プロピレングリコール含有量のミノキシジル含有量に対する割合が増加するにつれて発毛部位面積も増加しているが、ミノキシジルが組成物100mLに対して5g配合されているローション剤の場合には、プロピレングリコール含有量のミノキシジル含有量に対する割合が7.5倍のローション剤において最大の発毛部位面積が認められ、さらにプロピレングリコール含有量のミノキシジル含有量に対する割合が増加すると発毛部位面積はむしろ減少していることがわかる。   From Tables 3 and 4, when using a lotion preparation containing 5 g of minoxidil in an amount of 3 g based on 100 mL of the composition, the hair growth area was increased. I understand that. Further, in the case of a lotion preparation containing 3 g of minoxidil per 100 mL of the composition, the hair growth site area increases as the ratio of the propylene glycol content to the minoxidil content increases. In the case of a lotion preparation containing 5 g per 100 mL of the product, the maximum hair growth area was observed in the lotion preparation with a ratio of propylene glycol content to minoxidil content of 7.5 times, and further contained propylene glycol. It can be seen that as the ratio of the amount to the minoxidil content increases, the hair growth site area rather decreases.

3.使用感の確認試験
以下の表5に示す組成で各化合物を配合し、ローション剤を調製した。
3. Usability Confirmation Test Each compound was blended with the composition shown in Table 5 below to prepare a lotion preparation.

表5:ローション剤の組成

Figure 2005314323
Table 5: Composition of lotion
Figure 2005314323

これらの実施例および比較例のローション剤について、20〜50代の男性被験者10名により使用感の評価を行った。評価方法は、頭部の右側に実施例のローション剤を、左側に比較例のローション剤を、それぞれ0.5mL塗布した。評価項目は、ローション剤の塗布直後におけるベタツキ感と、塗布5分後におけるベタツキ感および乾燥具合とし、以下に示す5段階により官能的に評価した。   About the lotion preparations of these Examples and Comparative Examples, the feeling of use was evaluated by 10 male subjects in their 20s to 50s. In the evaluation method, 0.5 mL of the lotion preparation of the example was applied to the right side of the head and the lotion preparation of the comparative example was applied to the left side. The evaluation items were a sticky feeling immediately after application of the lotion agent, a sticky feeling after 5 minutes of application, and the dryness, and the sensory evaluation was performed in the following five stages.

評価基準
ベタツキ感
5:かなりベタつく
4:ややベタつく
3:普通
2:ややサラサラする
1:かなりサラサラする
乾燥具合
5:かなり乾燥しにくい
4:やや乾燥しにくい
3:普通
2:やや乾燥しやすい
1:かなり乾燥しやすい
以下の表6に、被験者10名の評価の平均を示す。本発明の育毛剤組成物は、使用感に優れることが明らかになった。




Evaluation criteria Stickiness
5: Pretty sticky
4: Slightly sticky
3: Normal
2: Slightly smooth
1: It is quite smooth and dry
5: Very difficult to dry
4: Slightly difficult to dry
3: Normal
2: Slightly easy to dry
1: Pretty easy to dry Table 6 below shows the average of the evaluation of 10 subjects. It has been clarified that the hair restorer composition of the present invention is excellent in the feeling of use.




表6:評価結果

Figure 2005314323
Table 6: Evaluation results
Figure 2005314323

4.製剤例
以下の表7に示す、本発明の育毛剤組成物によるローション剤およびゼリー剤を製造した。
4). Formulation example The lotion agent and jelly agent by the hair restorer composition of this invention shown in the following Table 7 were manufactured.

表7−1:ローション剤の組成

Figure 2005314323
Table 7-1: Composition of lotion
Figure 2005314323

表7−2:ゼリー剤の組成

Figure 2005314323
Table 7-2: Composition of jelly agent
Figure 2005314323

ミノキシジルの血中濃度の時間変化を示した図である。It is the figure which showed the time change of the blood concentration of minoxidil.

Claims (3)

ミノキシジル、プロピレングリコール、および揮発性溶剤を含有する育毛剤組成物であって、
プロピレングリコールがミノキシジルに対して質量比で5倍より多く10倍より少ない量で含有されていることを特徴とする育毛剤組成物。
A hair restorer composition comprising minoxidil, propylene glycol, and a volatile solvent,
A hair restorer composition comprising propylene glycol in an amount of more than 5 times and less than 10 times by mass ratio with respect to minoxidil.
プロピレングリコールがミノキシジルに対して質量比で7倍より多く10倍より少ない量で含有されていることを特徴とする育毛剤組成物。   A hair restorer composition comprising propylene glycol in an amount of more than 7 times and less than 10 times by weight with respect to minoxidil. ミノキシジルが育毛剤組成物100mLに対して0.1〜7gの量で含有されていることを特徴とする、請求項1または2に記載の育毛剤組成物。   The hair restorer composition according to claim 1 or 2, wherein minoxidil is contained in an amount of 0.1 to 7 g with respect to 100 mL of the hair restorer composition.
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