1353249 玫、發明說明： 【發明所屬之技術領域】 本發明與防止掉髮及促進生髮之組成物有關，尤其 效成份之細辛根（Asiasari Radix)萃取物有關 :田 j 縮短生髮循環中由休止期轉換到生長期所需的期間，2呈 環之生長期的優異效果，藉此快速地再生頭髮。 I現誘導生髮循 【先前技術】 -般人的頭皮上約有十萬至十五萬根頭髮，每 期的生髮循環而終至脫落，此週期會維持 敖人平均母天會掉落五十至一百根頭髮。 吟Ί 一般而言’充髮症是指處於生長期的頭髮相對比例較 止期的頭髮相對比例較多之謂，其將造成異常的掉髮。 ； r八主要原因已有許多假設性的討論，例如：男性荷爾蒙過多、皮 i 了 ㈣氧化物或細g的存在造朗皮的功能障 礙遺傳因素、老化、屢力及類似原因等。雖然真正導致 然而，禿髮確定與複雜的身體機制有關。 "，素複雜’迄今所發展出的包含各種有效成份的藥 、tit ΐ循環、增強髮根功能、頭皮賴、抑制頭皮 效果二然❿生髮循環之生長期、抑制男性荷輯活性等所需的 -些副^用。 "不盡理想，並且已有報告指出這些藥品會導致 定，促進生髮的主要實驗方法係利用動物試驗進行體内測 i用培料進行财，自從酬年代發展 paD i 11 a °ce 1 ^ H滤泡之主要細胞的乳頭狀突起皮膚細胞（derma 1 (outer r〇〇t sheath ceii) i出声的區分機制已積極地進行中。到目前為止，已發 = t 織的方法’其可用於頭髮再生、生髮及防止掉髮的研 ΐ生物ϊΐ驗的生長因素和基因的分離，使得可利用生化及分 養技術忽略了如頭髮濟篩選。然而，因為這些體外培 .，，織皮下、.且織間的互動及血液循環等直接或間接影響生髮的因素，致使 1353249 該等技術受限於應用範圍。因此，藉由 旲ίΓ Λ#上用於促魅髮或防止的產品具ίί多有用的效 及=ί 人滿意’這是因為__ 但仍未見以複雜細密人體機制開發的產品。 ’’、解、、， 的關^於髮^男性荷’有關，所以與男性荷爾蒙的分泌量有直接 之二已有許多用於藉由抑制男性荷爾蒙活性以防止並治療掉髮 =，出。r簡要的介紹謝男性荷爾蒙的機: 男性何爾豕之一的睪丸素酮（testosterone)係萨1353249 玫,发明说明: Technical Field of the Invention The present invention relates to a composition for preventing hair loss and promoting hair growth, and particularly relates to an ingredient of Asiasari Radix extract: Tian j shortens the cycle of hair growth by rest During the period of transition to the growth period, 2 is an excellent effect in the growth phase of the ring, thereby rapidly regenerating the hair. I now induces hair growth [previous technique] - There are about 100,000 to 150,000 hairs on the scalp of the human body. The hair growth cycle of each period ends and falls off. This cycle will keep the average mother's day drop by fifty. To one hundred hairs.吟Ί In general, 'filling disease' refers to the fact that the relative proportion of hair in the growing season is relatively large, which will cause abnormal hair loss. There are many hypothetical discussions on the eight main causes, such as: excessive male hormones, skin i (4) oxides or fine g in the presence of granulomatous dysfunction, genetic factors, aging, repeated and similar reasons. Although actually caused, however, baldness is determined to be related to complex physical mechanisms. ", complex complex's products that have been developed to date, including various active ingredients, tit ΐ circulation, enhanced hair root function, scalp rash, inhibition of scalp effect, growth cycle of growth cycle, suppression of male activity, etc. - some of the use of ^. "Not ideal, and there have been reports that these drugs will lead to the establishment of the main experimental method to promote hair growth using animal experiments for in vivo measurement i with the cultivation of materials, since the remuneration of the development of paD i 11 a °ce 1 ^ The differentiation mechanism of derma 1 (outer r〇〇t sheath ceii) i vocalization of the main cells of H follicles has been actively carried out. So far, the method of t-weaving has been made available. The growth factors and gene isolation of hair growth, hair growth and hair loss prevention studies make it possible to use biochemical and nutrient techniques to neglect such as hair screening. However, because of these in vitro culture, And the interaction between the weaving and the blood circulation directly or indirectly affect the factors of hair growth, so that the technology of 1353249 is limited by the application range. Therefore, the products used for fascinating or preventing by 旲ίΓ Λ# Useful effects and = ί people's satisfaction 'This is because __ but there is still no product developed with complex and fine human body mechanism. '', solution,,,,,,,,,,,,,,,,,,,,,,,,,, There are a number of direct secretions that have been used to prevent and treat hair loss by inhibiting male hormone activity. r Brief introduction of the device of male hormones: testosterone, one of the males Tissa
Cdihydroestosterone)^ A皮脂分“過旦髮的蛋白質而形成禿髮’由於該機制可能導 =士以過里、堵瘡粉刺或脂溢性皮膚炎，因而刺 =二之因5α—還原酶的作用致使二氨畢^ 從此Hi 還縣活性將可有效防止及治料性充髮。 以發t 療前列腺的治翁卜非那雄胺（fina細de) 有數種==性出侧那雄胺會 到有效治療男性禿髮的此外，僅抑制.還原酶活性無法達 各if上述問題，為了透過動物實驗識別生髮循環之生長期的誘導因 tit者已筛選數十種植物萃取物，因而找到細辛根萃取物，該萃取 物具有誘導生髮循環之生長期的優異能力。明確地說，本發明者選取數十 ^用^止掉髮且促進生髮、同時對人體保證安全且無毒性的植物萃取 、將研究引導至評估生髮循環中之生長期的誘導作用。最後本發明 ^發現細辛根萃取物可縮短生髮循環中從休止期轉換至生長誠需的期 竭，而呈現誘導生長期的優異效果，因而有本發明的誕生。 細辛根萃取物在頭髮相關產品的應用係揭示於韓國專利公開案第 Π^。3366號巾’依據此專利文件，在芝麻油巾的細辛鮮取物溶液添 ^又刑子（ViticisFmctus)、川寫（CnidiiRhk〇ma)、自定（Angelicae ahuricae Radix)及零陵香（Lysimachiae Foenumgraeci)的混合物。然 7 1353249 而 ’該細麟並無良好_決方法以完成技術上_用，w 不…此外，日本專利公開 辛根萃取_崎長生t循環之生長期，但是26 用細 =:=於生髮循環之生長期上的細辛根萃取物誘導作用3制 由於導致妓的因素相當繁雜，因 S髮細辛根萃取物、一抑制5α-還原酶活性成份及-活化 頭生長的效果，並且無任何副侧。 ，、職好_止料及促進 髮循3生多透過活化頭髮濾、泡細胞的作用以維持並延長生 報告’但是奴長生細祕料足輯到促進生 【發明内容】 止掉ίϊΓί^ί上述的諸多問題’其主要目的在提供—種驗有效防 i 物’其可從料生細、洲^姻酶活性及 二而-二 ' 的觀點，於許多錯綜複雜的錢機制上產生複雜的功 此’而适些觀點被認為具備促進生髮及防止掉髮的有效功能。 =^上述目的，本發明提供一種用於防止掉髮及促進生髮之組成 物，其包含一做為有效成份之細辛根萃取物。 該、辛根萃取物可藉由以低酒精、n—己院或二者之混合物所萃取之細 制，對於本發明之組成物總重而言，以此獲得的細辛根萃取物 的固態含量約〇. 01至l〇wt%。 若需要，本發明之組成物尚包含至少選自—抑制&還原酶活性之成 U下稱為、「5α—還原酶抑麵」）或一活化頭髮渡泡細胞之成份（以下 /、頭髮滤泡細胞活化劑」）。相較於組成物之總重而言，較佳的5α_ 旦原酶抑侧與頭魏泡細胞活化劑具有大約為請丨至腕%的固態含 •y 〇 依據t發明，該用於促進生髮之組成物係優於先前技術其原因在於 =細辛根萃取物可透過一特定機制，如生髮循環之生長期的誘導作用，而 現促進生髮的效果’並且5還原酶活性抑劑和頭髮濾泡細胞抑制劑二 者同時增加防止掉髮及促進生髮的效果。 _以本發明背景而言，本發明者選取數十種用於防止掉髮及促進生髮、 同時對人體保證安全且無毒性的植物萃取物，並將研究引導至評估生髮循 環中之生長期的誘導作用，從而，本發明者發現到細辛根萃取物具有誘導 生髮循環之生長期的優異效果，因此，本發縣以此發現為基礎。為了達 到更好的掉髮及促進生髮職果，必需透過各種_研究充髮的原 因，並審視每一機制中有效成份的最佳組合。為此目的，本發明者選擇以 下成份.可控制男性荷爾蒙活性的成份、可促進血液循環的成份、可促進 細胞活化的成份、具有抗發炎活性的成份及經證明對人體安全的各種成 份，並結合該等成份以尋找具有預防掉髮及促進生髮之 合。祕，本個者發現包含-細辛根萃取物、—5α_還原 頭髮濾泡細胞活化劑等三種有效成份之組成物，該組成物具有防止掉髮及 促進頭髮生命的良好絲。本發明者進-步發現鱗有效成份之__最佳組 合，而本發明係以該等發現為基礎。 因此，本發明提供一種具有防止掉髮及促進生髮良好效果之組成物， 該組成物從料生長期、活侧魏泡細胞及抑制5α_還原酶活性的觀 點，於許多導致紐的·上提供_的魏，這些觀職認為在促進生 髮及防止掉髮上具備有效的功能。 在本發明之組成物中，用以作為原料之細辛根係一天然藥物，其係藉 由切取屬於馬兜鈴（Aristol〇chiaceae)科之薄葉細辛（Asi站 sieboldi)及雞林細辛（Asiasaru]nheter〇tr〇p〇ides)的地上部分所獲得 之根及莖而製成 '細辛根具有—稍勻的f曲線條形狀，且包含3至5又顧 厚、黃咖啡色且粗糙的地下莖，及5至2〇刪長、約丨咖厚與地下莖連結 之根部。在根部的縱向中，形成淡咖啡色的淺凹槽。葉柄、花梗或芽苞可 1存在於地下莖的上部。磨碎根部及地下莖很容易，且磨碎後的表面係呈 黃白色。細辛根具有-自然的香味和辛辣的味道^細辛根的主要代表成份 包括：甲基丁香酚（methyleugen〇1)、桉油酚（cine〇1)、黃 及1-細辛素（1:asarin)。雞林細辛含有卜芝麻素（1_sesamin)、卡3 (kakuol)、asariein、saishinone、優香芹_ (eucarvone)及其它屬於同 屬之天然藥物成份。 在製，本發明之組成物中所含的細辛根萃取之前，首先將細辛根的根 部及地下莖洗淨並加以磨碎’然後冷浸於萃取溶射5 ϋ容劑之容量 1353249 需^於細辛根總量的ι〇倍以上。之後，將所得到的溶液過濾、濃縮並冷凍 乾燥，以取得細辛根萃取物的乾燥粉末。此處所使用之溶液包括但不限於： 純水；低酒精（例如：甲醇、乙醇、異丙醇^丁酸）；多元醇（例如：丙三 醇、丙二醇、1，3-丁二醇）以及烴基溶劑（例如：乙酸甲酯 '乙酸乙酯 '苯、 n-士烷、二乙醚'二氣甲烷等在這些溶劑當中，較佳的為低酒精（例如： 甲醇、乙醇、n-丁醇及n-己烷）。這些溶劑可單獨使用或結合使用。 相對於本發明之組成物總重，以此獲得的細辛根萃取物較佳具有大約 〇. 01至10wt%的固態含量。當細辛根萃取物含量少於〇 〇lwt%時，^髮循環 之生長期的誘導作用便無法令人滿意。另一方面，當細辛根萃取物之含量 超過10wt%時，過量的細辛根萃取物不會進一步改善生長期的誘導作用。 除了細辛根萃取物之外，本發明之組成物進一步包含一 5〇_還原酶抑 制劑及一頭髮濾泡細胞活化劑二有效成份，該等成份確信與男性禿髮密切 相關。因此，本發明之組成物具有防止掉髮及促進生髮的較佳效果。 本發明之組成物中所包含的5α-還原酶活性抑制劑係一種外部應用的 成份，其具有抑制人體頭髮遽泡細胞中5α-還原酶活性的作用，而有防止 掉髮的效果。只要對人體不造成傷害，可以單獨使用一種或結合多種成份， 作為5α-還原酶抑制劑。合適的5α-還原酶活性抑制劑成份的範例包括： 取自於植物的天然藥物，例如：苦參（Sophorae Radix)、薏炫仁（c〇icisCdihydroestosterone) ^ A sebum is divided into "a protein that is formed by baldness" because the mechanism may lead to sputum, acne or seborrheic dermatitis, so the role of 5α-reductase The result is that the activity of the sulphate will be effective to prevent and cure the sensation of the spleen. The treatment of the prostate for the treatment of the prostate is indomethacin (fina fine de) There are several kinds of == sexual side of the maleamine In addition to the effective treatment of male alopecia, only reductive enzyme activity can not reach the above problems, in order to identify the growth factor of the growth cycle through animal experiments, the titer has screened dozens of plant extracts, thus finding fine Singen extract, which has the excellent ability to induce the growth cycle of the hair growth cycle. Specifically, the inventors have selected a few hundred kinds of plant extracts which use hair to stop hair loss and promote hair growth while ensuring safe and non-toxicity to the human body. The study was directed to assess the induction of the growth phase in the germinal cycle. Finally, the present invention found that the extract of Asarum can shorten the period of transition from the resting period to the growth of the growth cycle, and exhibits induced growth. The excellent effect, and thus the birth of the present invention. The application of Asarum root extract in hair-related products is disclosed in Korean Patent Publication No. 3, No. 3366. According to this patent document, the fresh sesame oil in the sesame oil towel is taken. The mixture of the solution is a mixture of Viticis Fmctus, CnidiiRhk〇ma, Angelicae ahuricae Radix and Lysimachiae Foenumgraeci. 7 1353249 and 'The thin lining is not good _ The method is to complete the technical use, w not... In addition, the Japanese patent discloses the sin root extraction _ saga longsheng t cycle growth period, but 26 with fine =: = in the growth cycle of the growth cycle of Asarum root extract induction The 3 system is quite complicated due to the factors causing cockroaches, due to the effect of S. sinensis root extract, an inhibitory activity of 5α-reductase and the growth of the activated head, and no secondary side, and a good job _ stop material and promote hair Through the role of 3 generations to activate hair filtration and blistering cells to maintain and prolong the birth report 'But the slaves and the secrets of the sequel to the promotion of life [invention content] stop ίϊΓ ί^ί the above problems 'the main purpose In the provision of - the effective detection of anti-i - 'from the perspective of raw material, continents ^ enzyme activity and two - two', on many complicated financial mechanisms to produce complex merits It is considered to have an effective function for promoting hair growth and preventing hair loss. The above object provides a composition for preventing hair loss and promoting hair growth, which comprises an extract of Asarum as an active ingredient. The root extract can be obtained by a fine method of extracting with a low alcohol, n-house or a mixture of the two, and the solid content of the extract of the asarum root obtained by the total weight of the composition of the present invention is about 〇 01 to l〇wt%. If necessary, the composition of the present invention further comprises at least a component selected from the group consisting of - inhibiting & reductase activity, "5α-reductase inhibitor", or an active hair blasting cell (below /, hair) Follicular cell activator"). Compared with the total weight of the composition, the preferred 5α-pro-enzyme inhibitor and the head vesicle cell activator have a solid content of about 丨 to 腕%, according to the invention of t, which is used to promote hair growth. The composition is superior to the prior art because the Aspergillus root extract can be induced by a specific mechanism, such as the growth phase of the growth cycle, and now promotes the effect of hair growth' and 5 reductase activity inhibitor and hair filter Both of the cytokine inhibitors simultaneously increase the effect of preventing hair loss and promoting hair growth. In the context of the present invention, the inventors selected dozens of plant extracts for preventing hair loss and promoting hair growth while ensuring safe and non-toxicity to the human body, and directed the study to assess the growth period in the hair growth cycle. Induction, the present inventors have found that the extract of Asarum root has an excellent effect of inducing the growth period of the germinal cycle, and therefore, the present county is based on this finding. In order to achieve better hair loss and promote career development, it is necessary to examine the reasons for the various ingredients and to examine the best combination of active ingredients in each mechanism. To this end, the present inventors have selected the following ingredients, components which can control male hormone activity, components which promote blood circulation, components which promote cell activation, components which have anti-inflammatory activity, and various components which have been proved to be safe for human body, and Combine these ingredients to find a combination that prevents hair loss and promotes hair growth. The present invention found a composition comprising three active ingredients, such as an extract of Asarum Root, a 5α-reduced hair follicle cell activator, which has a good silk which prevents hair loss and promotes hair life. The inventors have further discovered the best combination of the effective components of the scale, and the present invention is based on such findings. Accordingly, the present invention provides a composition having a good effect of preventing hair loss and promoting hair growth, which composition is provided on a plurality of materials from the viewpoints of growth period, living side vitreous cells, and inhibition of 5α_reductase activity. _ Wei, these positions are considered to have effective functions in promoting hair growth and preventing hair loss. In the composition of the present invention, as a raw material, Asahi root is a natural medicine, which is obtained by cutting out the sieboldi belonging to the family Aristol〇chiaceae (Asi station sieboldi) and chicken linshin (Asiasaru]nheter〇tr〇p〇ides) The roots and stems obtained from the above-ground parts are made of 'Thining Roots' with a slightly uniform f-curve shape, and contain 3 to 5 thick and yellow brown and rough The underground stems, and 5 to 2 〇 long, about 丨 丨 丨 thick and the roots of the underground stems. In the longitudinal direction of the root, a pale brown light groove is formed. Petiole, peduncle or bud can be present in the upper part of the underground stem. It is easy to grind the roots and underground stems, and the surface after grinding is yellowish white. Asarum root has a natural aroma and a spicy taste. The main representative ingredients of Asarum Root include: methyleugenol (methyleugen〇1), oleophenol (cine〇1), yellow and 1-asarin (1 :asarin). Chicken linsin contains sesamin (1_sesamin), card 3 (kakuol), asariein, saishinone, eucarvone and other natural pharmaceutical ingredients belonging to the same genus. Before the extraction of Asarum root contained in the composition of the present invention, the roots and underground stems of Asarum root are first washed and ground, and then immersed in the extractive spray 5, the volume of the liquid is 1353249. The total amount of Asarum root is more than 〇. Thereafter, the obtained solution was filtered, concentrated, and freeze-dried to obtain a dry powder of the Asarum root extract. The solutions used herein include, but are not limited to: pure water; low alcohol (eg, methanol, ethanol, isopropanol / butyric acid); polyols (eg, glycerol, propylene glycol, 1,3-butanediol) and a hydrocarbon-based solvent (for example, methyl acetate 'ethyl acetate' benzene, n-stane, diethyl ether' di-methane, etc. among these solvents, preferably low alcohol (for example: methanol, ethanol, n-butanol and N-hexane). These solvents may be used singly or in combination. The sesame root extract thus obtained preferably has a solid content of about 0.1 to 10% by weight relative to the total weight of the composition of the present invention. When the content of sinensis extract is less than 〇〇lwt%, the induction of the growth cycle of the hair cycle is unsatisfactory. On the other hand, when the content of the extract of Asarum root exceeds 10% by weight, the excessive osmium root The extract does not further improve the induction in the growth phase. In addition to the Asarum root extract, the composition of the present invention further comprises a 5〇_reductase inhibitor and a hair follicle cell activator two active ingredients, such The ingredients are believed to be closely related to male baldness. Therefore, the composition of the present invention has a preferable effect of preventing hair loss and promoting hair growth. The 5α-reductase activity inhibitor contained in the composition of the present invention is an externally applied component which inhibits human hair cells. The effect of 5α-reductase activity, but has the effect of preventing hair loss. As long as it does not cause harm to the human body, it can be used alone or in combination with various components as a 5α-reductase inhibitor. Suitable inhibitor of 5α-reductase activity Examples of ingredients include: Natural medicines derived from plants, such as: Sophorae Radix, 薏炫仁 (c〇icis)
Semen)、丁香（Caryophylli Flos)、浮萍（Duckweed)(紫萍屬 SEHLEIDEN ; Spirodela polyrhiza SEHLEIDEN)、白樺（White birch)(曰本白樺；Betula platyphylla var. japonica)、五倍子（Galla Rhois)、姜活（Angelicae Koreanae Radix) ' 藁班（Rhiz〇ma Ligustici)、大黃（Rhei Rhizoma)、 桃仁（Persicae Semen)、白彊蠶（Bombycia Corpus)、白芨（Bleti 11a Striata)、檳榔（Arecae Semen)、紫蘇葉（periliae Folium)、薑黃 (Curcumae longae Rhizoma)、白芍（Paeoniae Radix)(芍藥；Paeonia albiflora、Paeonialactiflora)、GleditisSinensis、棕兒茶（Gambir)、 小茴香（Foeniculi Fructus)、遠志（Polygalae Radix)、荊芥 (Schizonepetae Herba)、牽牛子（Pharbitidis Semen)、車前子 (Plantaginis Semen)以及苦木（Picrasma guassioides)萃取物。上述 天然藥物係普遍描述於韓國藥典或韓國草藥典中，且在市場中銷售。這些 天然萃取物係藉由一般溶劑萃取法而取得，且對於萃取溶劑之選取並沒有 特別的限制。依據本發明之組成物總重為基礎，5α-還原酶活性抑制劑的 1353249 含量較佳範圍為〇· 001至l〇wt% ’更佳為〇 〇1至。 本發明之組成物中所包含的頭髮濾泡細胞活化劑也是一種外部應用的 成份，其具有活化人體頭髮濾泡細胞之作用，因而具有防止掉髮或&進生 髮的效果。只要對人體不造成傷害，可以單獨使用一種或多種成份作為頭 髮濾泡細胞活化劑。頭髮濾泡細胞活化劑的特定成份包括：檜木酚 (hinokitiol)、菸鹼醯胺（nic〇tinamide)、維生素B6、頂花防己碱 jcepharanthine)、生物素（biotin)及泛酸（pantothenic acid)，其可 單獨使用或結合使用。依據本發明之組成物總重為基礎，頭髮濾泡細胞活 化劑的含量較佳範圍為〇. 001至l〇wt%，更佳為〇 至5wt%。 亦即，本發明之組成物包含作為有效成份之細辛根萃取物、5α還原 酶抑制劑及頭髮濾泡細胞活化劑，其中該細辛根萃取物具有誘導生髮循環 之生長期的優異效果。5〇!-還原酶抑制劑之較佳成分包括：苦參、薏苡仁 及丁香萃取物。頭髮濾泡細胞活化劑的較佳成分包括：檜木酚和菸鹼醯胺， 尤其以各自之固態含量為基礎，細辛根萃取物具有約〇. 01至1〇wt% 5a_ 還原酶抑制劑具有約〇. 〇〇1至1〇 wt %及頭髮濾泡細胞活化劑具有約〇 〇〇ι 至 10 wt %。 當單獨使用這些在防止掉髮及促進生髮具有不同機制的有效成份時， 其效果不儘理想。反之，該包含細辛根萃取物、5α_還原酶抑制劑及頭髮 濾泡細胞活化劑之組成物，其對於防止掉髮及促進生髮則具有良好效果。 ，本發^之一較佳具體實施例中，透過動物實驗及與禿髮病患之臨床試驗 得以確認，該組成物具有防止掉髮及促進生髮的優良效果。 為了增強有效成份之功能並給予組成物額外的功能以符合病患之使 用，將至少一選自抗頭皮屑劑、深層潔淨劑、冰涼劑及保濕劑之輔助成份 添加至今發明之組成物中，在此情況中，該組成物具有良好的預防掉髮及 促進生髮之效果。該輔助成份（例如：抗頭皮屑劑、深層潔淨劑、冰涼劑 及保’燕劑）較佳的包括：辣椒g了（capSicum以此扣^)、生育盼乙酯 (tocopherol acetate)、煙酸节基（benzyl nic〇tinate )、 piroctonolamine、水楊酸（salicylicacid)、l-薄荷腦（Ι-menthol)等。 只要所添加的輔助劑不妨礙有效成份之效果並且可以維持配方之穩定性， 便不特別限制該辅助劑的數量，然而考量人體安全及配方之穩定性，辣椒 酊及生育酚乙酯之數量範圍較佳為〇 〇〇1至1〇wt%、煙酸苄基（benzyl nicotinate)較佳為 〇· 〇〇1 至 〇、pir〇ct〇n〇lar^ne 較佳為 〇 〇〇1 至 1353249 lwt% ’以及水楊酸與卜薄荷腦之數量範圍較佳〇. 〇1至lwt%。 本發明之組成物可調製成一般劑量形式，如：液狀、膏狀、糊狀及固 狀，其可塗抹於患有禿髮之頭皮上。本發明之組成物可應用在用於促進生 髮的各種相關的產品上，如：洗髮精、潤絲、乳液、滋養液及類似產品， 其中也包括以喷劑型態的應用。 【實施方式】 現在請參考以下之較佳實施例以詳細說明本發明。然而，這些實施例 僅用於說明之目的，不應解釋為本發明之範圍限制。 在以下的實施例中，利用C57BL/6老鼠做為動物模型用以評估生髮循 環之生長期的誘導作用。有自然禿髮的C57BL/6老鼠具有黑色體毛，其黑 色素細胞係僅存在於頭髮濾泡中，且黑色素的合成係與生髮循環同步了^ 於。5術6老鼠的纟髮循射以藉由視覺觀察其膚色之變化而判斷，因此 9 其已被廣泛用來做為研究生髮循環之生長期誘導作用的動物模型。 製備例：細辛根蕈取物之_偌 一細辛根萃取物係依據以下程序製備： 首先，磨碎細辛根的根部及地下莖（500g)並使其穿過篩網（#1〇), =後加入大約5000 ml的乙醇（韓國藥典），將所得到之溶液於室溫下冷 。浸5天。利用Whatman #2濾紙過濾該萃取物，並將所得到之過濾物在45 c的減壓環境下利用旋轉蒸汽機濃縮至乾燥，以獲得大約2〇g(產量 4%)的細辛根萃取物。 、 翅第例1 :細辛根萃取物對势生長期諉導作用的評估 使用老鼠（C57BL/6，Semen), Caryophylli Flos, Duckweed (Spirulina SEHLEIDEN; Spirodela polyrhiza SEHLEIDEN), White birch (Betula platyphylla var. japonica), Galla Rhois, Ginger (Angelicae Koreanae Radix) 'Rhiz〇ma Ligustici, Rhei Rhizoma, Persicae Semen, Bombycia Corpus, Bleti 11a Striata, Arecae Semen, Perilla Periliae Folium, Curcumae longae Rhizoma, Paeoniae Radix (peony), Galeitis Sinensis, Gambir, Foeniculi Fructus, Polygalae Radix, Schizonepetae Herba, Pharbitidis Semen, Plantaginis Semen, and Picrasma guassioides extracts. The above natural medicines are generally described in the Korean Pharmacopoeia or Korean Herbal Medicine and are marketed. These natural extracts are obtained by a general solvent extraction method, and there is no particular limitation on the selection of the extraction solvent. The content of 1353249 of the 5α-reductase activity inhibitor is preferably in the range of 〇· 001 to l〇wt% ‘more preferably 〇 至1 to based on the total weight of the composition of the present invention. The hair follicle cell activator contained in the composition of the present invention is also an externally applied component which has an effect of activating hair follicle cells of a human hair, and thus has an effect of preventing hair loss or & hair growth. As long as no harm is caused to the human body, one or more components may be used alone as a hair follicle cell activator. Specific components of hair follicle cell activators include: hinokitiol, nic〇tinamide, vitamin B6, jcepharanthine, biotin, and pantothenic acid. Can be used alone or in combination. The content of the hair follicle cell activator is preferably in the range of 0.001 to 10% by weight, more preferably 5% to 5% by weight based on the total weight of the composition of the present invention. That is, the composition of the present invention contains Asarum Root Extract, 5α Reductase Inhibitor and Hair Follicle Cell Activator as active ingredients, wherein the Asarum Root Extract has an excellent effect of inducing the growth period of the hair growth cycle. 5〇!- Preferred components of the reductase inhibitor include: Sophora flavescens, Coix seed, and clove extract. Preferred components of the hair follicle cell activator include: xylenol and nicotinamide, especially based on the respective solid content, the extract of Asarum Root has an amount of about 0.1 to 1% by weight. 5a_ Reductase inhibitor has约1 to 1〇wt% and hair follicle cell activator have an amount of about 〇〇〇1 to 10 wt%. When these are used alone to prevent hair loss and promote the development of active ingredients with different mechanisms, the effect is not satisfactory. On the other hand, the composition comprising an extract of Asarum Root, a 5α-reductase inhibitor and a hair follicle cell activator has a good effect for preventing hair loss and promoting hair growth. In a preferred embodiment of the present invention, it has been confirmed by animal experiments and clinical trials with alopecia, the composition has an excellent effect of preventing hair loss and promoting hair growth. In order to enhance the function of the active ingredient and give the composition an additional function to meet the use of the patient, at least one auxiliary component selected from the group consisting of an anti-dandruff agent, a deep cleansing agent, a cooling agent and a moisturizing agent is added to the composition of the invention. In this case, the composition has a good effect of preventing hair loss and promoting hair growth. Preferably, the auxiliary component (for example, anti-dandruff agent, deep cleansing agent, cooling agent and moisturizing agent) comprises: capsicum (capSicum), tocopherol acetate, niacin Benzyl nic〇tinate, piroctonolamine, salicylic acid, l-menthol, and the like. As long as the added adjuvant does not interfere with the effect of the active ingredient and can maintain the stability of the formulation, the amount of the adjuvant is not particularly limited, however, the safety of the human body and the stability of the formulation, the range of the amount of capsicum and tocopherol ethyl ester are considered. Preferably, 〇〇〇1 to 1% by weight, benzyl nicotinate is preferably 〇·〇〇1 to 〇, pir〇ct〇n〇lar^ne is preferably 〇〇〇1 to 1353249 Lwt% 'and the range of salicylic acid and menthol are better. 〇1 to lwt%. The compositions of the present invention can be formulated into a conventional dosage form such as a liquid, a paste, a paste, and a solid which can be applied to a scalp having alopecia. The composition of the present invention can be applied to various related products for promoting hair growth, such as shampoo, moisturizing, lotion, nourishing liquid and the like, and also includes application in a spray form. [Embodiment] The present invention will now be described in detail with reference to the preferred embodiments below. However, the examples are for illustrative purposes only and are not to be construed as limiting the scope of the invention. In the following examples, C57BL/6 mice were used as an animal model to evaluate the induction of the growth cycle of the germinal cycle. C57BL/6 mice with natural alopecia have black body hair, and the melanocyte cell line is only present in the hair follicles, and the melanin synthesis is synchronized with the germinal cycle. 5 The spurt of 6 mice was judged by visual observation of the change in skin color, so it has been widely used as an animal model for the long-term induction of postgraduate circulation. Preparation: Asarum root extract 偌 细 细 根 萃取 extract is prepared according to the following procedure: First, the roots and underground stems (500g) of Asarum root are ground and passed through the sieve (#1〇) , = about 5000 ml of ethanol (Korean Pharmacopoeia) was added, and the resulting solution was cooled at room temperature. Dip for 5 days. The extract was filtered using Whatman #2 filter paper, and the obtained filtrate was concentrated to dryness using a rotary steam machine under a reduced pressure of 45 c to obtain about 2 g (yield 4%) of the extract of Asarum. Wings Example 1: Evaluation of the effect of Asarum root extract on the growth potential of the growing period Using mice (C57BL/6,
首先’利用電動刮鬍刀將老鼠背部周圍的毛髮刮除。然後，測量 老鼠的重量並將所有的老鼠分為數組，每組12隻，以此方式祕翻沾舌First, use an electric razor to scrape the hair around the back of the mouse. Then, measure the weight of the mouse and divide all the mice into an array of 12 each, in such a way
奶，八αυ A 1的數量將試劑塗抹於每隻老鼠的背部並持續 12 1353249 ϊίί除生長期的誘導作用。藉由計算新毛髮生長面積及 率，及平均所得到的數值以確認每隻老鼠的生長期 !。根據不同濃度的細辛根萃取物所評㈣生長觸導作用，盆处 果如表1所示。 … 表1 濃度 0.001% 0.01% 1% 10% 控制劑 面積比率（％) 24.8 42.4 68.8 72.4 12.0 如表1所示，藉由細辛根萃取物濃度的控制方式，可以呈現優異的生 髮循環之生長期的誘導作用，其中濃度低4於〇. 01%的測試劑已具有比控制劑 為佳的生長期誘導作用’但是效果仍無法令人滿意。另一方面，在濃度高 於10%的情況下，過量的細辛根萃取物對於生長期之誘導作用沒有顯著的改 善0 f施例1至8及比鲂你Μ趸6 表2所呈現中是，細辛根萃取物及至少選自苦參萃取物、薏苡仁萃取 物、丁香萃取物、檜木酚及於驗醯酸的其中一種做為有效成份的組成物。The amount of milk, 八αυ A 1 was applied to the back of each mouse and continued for 12 1353249 ϊίί in addition to the induction of growth phase. Determine the growth period of each mouse by calculating the new hair growth area and rate, and the average value obtained. According to the different concentrations of Asarum root extract, (4) growth touch, the pot fruit is shown in Table 1. Table 1 Concentration 0.001% 0.01% 1% 10% Control agent area ratio (%) 24.8 42.4 68.8 72.4 12.0 As shown in Table 1, the growth of the germinal cycle can be exhibited by the control method of the concentration of the extract of Asarum Root. Induction of the period, wherein the concentration is lower than 4%. 01% of the test agent has a better growth-inducing effect than the control agent' but the effect is still unsatisfactory. On the other hand, in the case where the concentration is higher than 10%, the excessive Asarum root extract has no significant improvement in the induction effect in the growth phase. 0 f Examples 1 to 8 and 鲂 鲂 6 表 6 Table 2 It is a composition of Asarum root extract and at least one selected from the group consisting of Sophora flavescens extract, Coix seed extract, clove extract, eugenol, and one of the phthalic acid as an active ingredient.
13 135324913 1353249
遡試例2 :诱過動物寬塗長期誘導彳乞 首先，實施例1至8及比較例i至6;的組成物利 I法（生長_導側崎估）進行她成物在生髮 =^相同之 作用的評估。在麟财所制的濃細體萃取物也用；^生長期誘導 14 1353249 各組成物。表3顯示施例1至8及比轉例1至6的細杰祕存斥雙神環中 的生長期誘導作用評估結果。 表3 範例 實方 包例 比較例 編號 1 2 3 4 5 6 7 8 1 2 3 4 5 6 面積 比率 (%) 64.0 85.8 77.8 82.2 75.2 66.8 98.8 99.8 43.4 38.6 39.2 56.0 41.8 34.2 如表3所不，比較例1至6的組成物包含具有促進生髮效果之5α還 原酶抑制劑及頭髮濾泡細胞活化劑，但其效果並不令人滿意。該包含細辛 着 根萃取物及苦參萃取物或薏炫仁萃取物（實施例2和3)之組成物；該包含 細辛根萃取物及檜木酚或菸鹼醯胺（實施例4和5)之組成物，較只包含一 ，該^效成份的組成物，具有較佳的生髮促進效果。該包含細辛根萃取物、 苦參萃取物及檜木齡（範例7和8)之組成物，較包含一或二種該有效成份 的組成物，具有更好的生髮促進效果。 运些結果指出，藉由細辛根萃取物、5α_還原酶活性的抑制及頭髮濾 泡細胞的活化而能誘導生長期之组成物，在促進生髮上展現出驚人的協同 效果。 〇 f些結果也證實了細辛根萃取物、苦參萃取物及檜木酚能透過誘導生 髮循環之生長期呈現出良好的生髮促進效果，相對地，5α-還原酶活性的 鲁 抑制及頭髮濾泡細胞的活化等因素的結合也都與防止掉髮及促進生髮的效 ^有關。此外’每一有效成份均具有其原本的活性，且不影響其它有效成 份，1性’因此’以適當比例組成之細辛根萃取物、苦參萃取物及檜木酚 之組合’在許多禿髮的精細機制上提供了複雜的功能。故盼望本發明之組 成物可呈__使用任—該等有效成份有更好的防止掉髮及促進生髮的 效果。 ^再者’從包含做為有效成份之細辛根萃取物、5 還原酶抑制劑及頭 Τ泡細胞活化_喊物並結合獅成份可以製備舰髮滋養液。臨床 試f就是利用頭髮滋養液用於絲病患上。 取物、芒彖&物及檜木酚之組成物進行臨床試驗 15 1353249 利用包含細辛根萃取物、苦參萃取物、檜木紛的組成物和其它辅助成 份進行臨床試驗，以確認組成物於禿髮病患上的效果。 在臨床試驗中’實施例7中包含細辛根萃取物、苦參萃取物及檜木酚 的組成物’實施例8中包含細辛根萃取物、苦參萃取物、檜木酚及其它輔 助成份的組成物，與比較例6中不包含有效成份之組成物，均可用於評估 防止掉髮及促進生髮的效果。 將組成物塗抹於15位受男性禿髮所苦之病患（年齡為2〇至5〇歲之成 年男女）’及15位平均每天掉落1〇〇根以上頭髮之病患（年齡為2〇至5〇 歲之成年男女）。此塗抹應以每天2至3滴（約2ml)的組成物進行，並且依 據其效果持續執行最少1個月以上至最多4個月。 藉由計算每天清洗時掉髮的數量及目視觀察來執行評估。將結果分類 ，以下5種等級（表4)並予以計分。最終效果的判斷係以分數的平均值表 示。當平均值為3. 0或更高時，判斷為有效。結果如表5所示。 表4 等級 清洗時掉髮的數量 目視觀察 5 顯著減少 顯著改善 4 平均減少 平均改善 3 輕微減少 輕微改善 2 無改變 »»»> {3^ —_!_ 增加 差 表5 範例編號 清洗時掉髮的數詈 目視觀窣 實施例7 3.6 3.4 實施例8 4.1 3.7 比較例6 2.6 2.4 糾組成物呈現輕微改善但是沒效果，而實施 ΐϋΓ卩纽紐的域物呈現她改善錢好，錢實施例8中 進一步包含辅助成份的組成物呈現平均改善錢好，因此 因 例7和8中的組成物在防止掉髮及促進生髮上具有良好的效^ ^， 1353249 為在臨床試驗期間的試驗對象身上沒有觀察到副作用，因此本發明之組 物證明為安全的。 x 、成* 綜上所述，透過動物實驗發現細辛根萃取物具有誘導生髮循環之生長 期的優異效果；同時亦發現結合細辛根萃取物、5α_還原酶抑_及頭髮 濾泡細胞活化劑之組合，具有較單獨使用其中一種該有效成份更好的促進 生髮效果。再者，包含二種有效成份之組成物係經過動物實驗及禿髮病串 的臨床試驗確認其具有防止掉髮及促進生髮的良好效果，因此，以適杏= 例組合該等有效成份的組成物，能於許多㈣的精細機制上提供複雜^ 望本剌之組成物可呈現較單獨使祕—種料有效成份更好的 防止掉髮及促進生髮的效果。 t勒容可_知道本發明提供—種包含做為有效成份之細辛根萃 進生髮的組成物’其中該細辛根萃取物具有誘導生髮循環之 發明之組成物可在防止掉髮及促進生髮上呈現良好 =效果，且*具任何毒性’尤其是，當馳成物又包含有5α 純細胞活化麟’仍是非常安全且具有防止掉髮及促進生髮的 雖然、本發明之較佳具體實_已說明揭示如上， 朗各雜改、獅減賴，^_隨附的遡Test Example 2: Long-term induction of cockroaches in animals. First, Examples 1 to 8 and Comparative Examples i to 6; Composition I Method (Growth_Guide Side Estimation) was carried out in her hair growth = ^ Evaluation of the same role. The concentrated extracts made in Lincai are also used to induce 14 1353249 constituents. Table 3 shows the results of the evaluation of the growth phase in the examples 1 to 8 and the fine secrets of the doubles. Table 3 Example real package comparison example No. 1 2 3 4 5 6 7 8 1 2 3 4 5 6 Area ratio (%) 64.0 85.8 77.8 82.2 75.2 66.8 98.8 99.8 43.4 38.6 39.2 56.0 41.8 34.2 As shown in Table 3, compare The compositions of Examples 1 to 6 contained a 5α reductase inhibitor and a hair follicle cell activator having a hair growth promoting effect, but the effect was not satisfactory. The composition comprising the extract of Asarum chinensis and the extract of Sophora flavescens L. or C. sylvestris (Examples 2 and 3); the extract comprising Asarum Root and the saponin or nicotinamide (Example 4 and The composition of 5) contains more than one, and the composition of the active ingredient has a better hair growth promoting effect. The composition comprising Asarum Root Extract, Sophora flavescens extract and Elm Age (Examples 7 and 8) has a better hair growth promoting effect than a composition comprising one or two of the active ingredients. These results indicate that the composition of the growth phase can be induced by the extract of Asarum root, the inhibition of 5α_reductase activity, and the activation of hair follicle cells, exhibiting a striking synergistic effect in promoting hair growth.结果f some results also confirmed that Asarum extract, Sophora flavescens extract and xylenol can promote a good hair growth promoting effect through the growth cycle of induced hair growth cycle, relatively, 5α-reductase activity inhibition and hair filtration The combination of factors such as activation of the vesicles is also related to the prevention of hair loss and the promotion of hair growth. In addition, 'Each active ingredient has its original activity, and does not affect other active ingredients, one's 'so' is a combination of Asarum extract, Sophora flavescens extract and eugenol in a proper proportion' in many baldnesses The sophisticated mechanism provides sophisticated functionality. Therefore, it is expected that the composition of the present invention can be used __the active ingredients have better effects of preventing hair loss and promoting hair growth. ^ Again, the ship's nourishing liquid can be prepared from the extract containing Asarum Root as an active ingredient, 5 reductase inhibitors, and sputum cell activation _ shouts combined with lion ingredients. The clinical test f is to use hair nourishing liquid for silk disease. Clinical trials of the composition of the extract, the scorpion & and the camphor phenol 15 1353249 The clinical trial was carried out using a composition comprising Asarum root extract, Sophora flavescens extract, eucalyptus extract and other auxiliary ingredients to confirm the composition The effect of alopecia onset. In the clinical trial, 'Example 7 includes the composition of Asarum Root Extract, Sophora flavescens extract and xylenol', and Example 8 contains Asarum Root Extract, Sophora flavescens extract, eugenol and other auxiliary ingredients. The composition and the composition excluding the active ingredient in Comparative Example 6 can be used for evaluating the effect of preventing hair loss and promoting hair growth. The composition was applied to 15 patients suffering from male baldness (adult men and women aged 2 to 5 years old) and 15 patients with an average of more than 1 root per day (age 2) 〇 to 5 years old adult men and women). This application should be carried out in a composition of 2 to 3 drops (about 2 ml) per day, and it is continuously performed for at least 1 month up to a maximum of 4 months depending on the effect. The evaluation is performed by calculating the number of hair loss during daily cleaning and visual observation. The results were classified into the following five grades (Table 4) and scored. The final effect is judged by the average of the scores. When the average value is 3.0 or higher, it is judged to be valid. The results are shown in Table 5. Table 4 Visual inspection of the number of hair loss during grade cleaning 5 Significantly reduced significant improvement 4 Average reduction Average improvement 3 Minor reduction Minor improvement 2 No change »»»> {3^ —_!_ Increase the difference table 5 Sample number is washed off詈 詈 窣 窣 窣 窣 7 窣 窣 窣 窣 窣 窣 窣 窣 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 2.6 The composition further comprising the auxiliary component in 8 exhibited an average improvement in the amount of money, and therefore the compositions in Examples 7 and 8 had good effects in preventing hair loss and promoting hair growth, and 1353249 was the subject during the clinical trial. No side effects were observed, so the composition of the present invention proved to be safe. x, into * In summary, through animal experiments, it was found that Asarum root extract has the excellent effect of inducing the growth cycle of the hair growth cycle; it is also found that combined with Asarum root extract, 5α_reductase inhibitor and hair follicular cells The combination of activators has a better hair growth promoting effect than using one of the active ingredients alone. Furthermore, the composition containing the two active ingredients is confirmed by the animal test and the clinical trial of the bald onset to have a good effect of preventing hair loss and promoting hair growth. Therefore, the composition of the active ingredients is combined with apricots. It is possible to provide a complex composition of many (four) fine mechanisms to exhibit a better effect of preventing hair loss and promoting hair growth than the effective ingredients of the secret ingredient alone. The present invention provides a composition comprising as an active ingredient an extract of Asarum roots, wherein the Asarum extract has a composition for inducing a hair growth cycle, which is capable of preventing hair loss and promotion The hair growth shows a good = effect, and * has any toxicity 'especially, when the chimeric substance contains 5α pure cell activation Lin' is still very safe and has the ability to prevent hair loss and promote hair growth, although the preferred embodiment of the present invention Real _ has been revealed as above, Lange miscellaneous change, lion reduction, ^_ accompanying
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