CN104411320A - Composition comprising natural extracts as active ingredients for improving condition of hair and scalp, and method for preparing same - Google Patents
Composition comprising natural extracts as active ingredients for improving condition of hair and scalp, and method for preparing same Download PDFInfo
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Abstract
本发明涉及包含天然提取物作为有效成分的毛发及头皮状态改善用组合物、其制备方法以及将天然提取物给药来改善毛发及头皮状态的方法,本发明的毛发及头皮状态改善用组合物包含天然提取物作为有效成分,因而没有副作用乃至毒性的担忧,且不需要手术,因而经济又可容易适用。
The present invention relates to a composition for improving the condition of hair and scalp containing a natural extract as an active ingredient, a method for preparing the same, and a method for improving the condition of hair and scalp by administering a natural extract. The composition for improving the condition of hair and scalp of the present invention Contains natural extracts as active ingredients, so there is no concern about side effects or toxicity, and it does not require surgery, so it is economical and easy to apply.
Description
【技术领域】【Technical field】
本发明涉及包含天然提取物作为有效成分的毛发及头皮状态改善用组合物及其制备方法,并涉及将本发明的天然提取物给药来改善毛发及头皮的状态的方法。The present invention relates to a composition for improving the condition of hair and scalp containing a natural extract as an active ingredient and a preparation method thereof, and to a method for improving the condition of hair and scalp by administering the natural extract of the present invention.
【背景技术】【Background technique】
作为脱发症的最常见的类型的男性脱发症是雄激素中之一的睾酮(testosterone)借助5-α还原酶(testosterone 5α-reductase)转化为作为活性雄激素的二氢睾酮(DHT,dihydrotestosterone),且如此活性化的二氢睾酮与雄激素受体相结合,来延迟毛囊细胞的蛋白质合成,从而缩短毛囊的生长期,并使毛囊萎缩,由此引发脱发的。并且,在雄激素性脱发过程中,也会过度生成皮脂,最终头皮中发生伴随炎症的脱发现象[Dennis A.Holt,et.al,J Med.Chem.,33,943,(1990)]。The most common type of male alopecia as alopecia is the conversion of testosterone (testosterone), one of the androgens, into dihydrotestosterone (DHT, dihydrotestosterone), which is an active androgen, by 5-α reductase (testosterone 5α-reductase) , And the activated dihydrotestosterone combines with the androgen receptor to delay the protein synthesis of the hair follicle cells, thereby shortening the growth period of the hair follicles, and causing the hair follicles to shrink, thus triggering hair loss. Also, in the process of androgenetic alopecia, sebum is also excessively produced, and eventually alopecia with inflammation occurs in the scalp [Dennis A. Holt, et. al, J Med. Chem., 33, 943, (1990)].
通常的脱发治疗法为毛发移植法。即,从毛发生长的头皮部位向脱发部位移植长有毛发的皮肤的塞子(plug)的方法。而这种方法的情况下,浪费时间,相对伴随痛苦,且所需费用高。其他非-药物治疗法包括紫外线照射及运动疗法。The usual hair loss treatment is hair transplantation. That is, it is a method of transplanting a plug (plug) of hair-growing skin from a hair-growing scalp site to a hair loss site. In the case of this method, time is wasted, it is relatively painful, and the cost is high. Other non-drug treatments include ultraviolet radiation and exercise therapy.
再一脱发治疗法有药物疗法,美国默克(Merck)公司在市场上销售以口服给药用制备非那雄胺的生发剂作为抑制5-α还原酶的作用,来抑制二氢睾酮(DHT)的生成的药。但是,这存在类固醇类药物引起副作用的问题。Another hair loss treatment method has drug therapy, and U.S. Merck (Merck) sells on the market the hair growth agent that prepares finasteride with oral administration as the effect of inhibiting 5-alpha reductase, to inhibit dihydrotestosterone (DHT) ) of the generated medicine. However, this has the problem of side effects caused by steroids.
并且,据报告,作为植物雌激素(phytoestrogen)中之一的黄豆苷元(daidzein)的主要代谢产物的雌马酚(equol)以不对睾酮产生影响的方式直接与二氢睾酮(DHT)相结合,由此阻断作为雄激素的二氢睾酮(DHT)的进程。Furthermore, it has been reported that equol, which is a major metabolite of daidzein, one of phytoestrogens, directly binds to dihydrotestosterone (DHT) without affecting testosterone. , thereby blocking the process of dihydrotestosterone (DHT) as an androgen.
因此,需要开发既经济又没有各种副作用乃至毒性的担忧的来源于天然物的治疗剂。Therefore, there is a need to develop therapeutic agents derived from natural products that are economical and free from concerns about various side effects and toxicity.
【发明内容】【Content of invention】
【发明要解决的技术课题】[Technical issues to be solved by the invention]
对此,本发明人为了解决如上所述的问题,通过实验确认到芦根、芍药、茯神、石苇、荠苨、塞纳叶、紫檀香、草果、泽泻、贯众、亚麻仁、葛花、姜黄、瓜蒌仁、麻仁及苏木提取物抑制5-α还原酶的功效,来促进毛发的生长的事实,并从上述提取物明确了毛发及头皮状态改善用组合物及其制备方法以及毛发及头皮状态改善方法。In this regard, in order to solve the above-mentioned problems, the present inventors have confirmed through experiments that reed root, peony root, Fushen, stone reed, marmoset, senna leaf, red sandalwood, grass fruit, Alisma, rhizome, linseed, The fact that the extracts of kudzu flower, turmeric, trichosantheme, hemp seed and sumac are inhibited by 5-alpha reductase to promote the growth of hair, and from the above extracts, the composition for improving the condition of hair and scalp and its A preparation method and a method for improving the condition of hair and scalp.
【解决课题的技术方案】【Technical solution to the problem】
本发明的目的在于,提供包含天然提取物作为有效成分的毛发及头皮状态改善用组合物及其制备方法。An object of the present invention is to provide a hair and scalp condition improving composition containing a natural extract as an active ingredient, and a production method thereof.
并且,本发明的另一目的在于,提供毛发及头皮状态改善方法,该毛发及头皮状态改善方法包括将选自由芦根、芍药、茯神、石苇、荠苨、塞纳叶、紫檀香、草果、泽泻、贯众、亚麻仁、葛花、姜黄、瓜蒌仁、麻仁及苏木组成的组中的一种以上的提取物向患有脱发的个体给药的步骤。Furthermore, another object of the present invention is to provide a method for improving the condition of hair and scalp. The method for improving the condition of hair and scalp comprises a method selected from the group consisting of reed root, peony, Fushen, stone reed, marmoset, senna leaf, rosewood, grass The step of administering one or more extracts from the group consisting of fruit, alisma, guanzhong, linseed, kudzu flower, turmeric, melon, hemp seed and sumac to an individual suffering from alopecia.
【发明效果】【Invention effect】
根据本发明,提供包含抑制5-α还原酶(testosterone5α-reductase)的效果突出的天然提取物作为有效成分的毛发及头皮状态改善用组合物、其制备方法及将天然提取物给药来改善毛发及头皮状态的方法。上述毛发及头皮状态改善用组合物包含天然提取物作为有效成分,因而没有副作用乃至毒性的担忧,且不需要手术,因而经济且能够容易适用。According to the present invention, there are provided a composition for improving hair and scalp condition comprising, as an active ingredient, a natural extract excellent in the effect of inhibiting 5-α reductase (testosterone 5α-reductase), a preparation method thereof, and hair improvement by administering the natural extract And the method of scalp condition. The composition for improving the condition of hair and scalp contains natural extracts as active ingredients, so there is no concern about side effects or toxicity, and since surgery is not required, it is economical and can be easily applied.
【附图说明】【Description of drawings】
图1为根据本发明的实验例1获得的d3-睾酮(d3-testosterone)的提取离子色谱图(Extracted-ion chromatograms)(图1的(a)部分:参考标准(Reference standard),图1的(b)部分:微粒体部分(Microsomal fraction))。Fig. 1 is the extracted ion chromatogram (Extracted-ion chromatograms) of d 3 -testosterone (d 3 -testosterone) obtained according to Experimental Example 1 of the present invention (part (a) of Fig. 1: reference standard (Reference standard), Fig. Part (b) of 1: Microsomal fraction).
图2为根据本发明的实验例1获得的睾酮(testosterone)的提取离子色谱图(Extracted-ion chromatograms)(图2的(a)部分:参考标准(Reference standard),图2的(b)部分:微粒体部分(Microsomal fraction))。Fig. 2 is the extracted ion chromatogram (Extracted-ion chromatograms) of the testosterone (testosterone) obtained according to Experimental Example 1 of the present invention (part (a) of Fig. 2: reference standard (Reference standard), part (b) of Fig. 2 : Microsomal fraction (Microsomal fraction).
图3为根据本发明的实验例1获得的d3-二氢睾酮(d3-DHT,d3-dihydrotestosterone)的提取离子色谱图(Extracted-ionchromatograms)(图3的(a)部分:参考标准(Reference standard),图3的(b)部分:微粒体部分(Microsomal fraction))。Figure 3 is the extracted ion chromatograms (Extracted-ionchromatograms) of d 3 -dihydrotestosterone (d 3 -DHT, d 3 -dihydrotestosterone) obtained according to Experimental Example 1 of the present invention (part (a) of Figure 3: reference standard (Reference standard), part (b) of Figure 3: Microsomal fraction).
图4为根据本发明的实验例1获得的二氢睾酮(DHT,dihydrotestosterone)的提取离子色谱图(Extracted-ionchromatograms)(图4的(a)部分:参考标准(Reference standard),图4的(b)部分:微粒体部分(Microsomal fraction))。Fig. 4 is the extracted ion chromatogram (Extracted-ionchromatograms) of the dihydrotestosterone (DHT, dihydrotestosterone) obtained according to Experimental Example 1 of the present invention (part (a) of Fig. 4: reference standard (Reference standard), Fig. 4 ( b) fraction: microsomal fraction (Microsomal fraction).
图5表示根据本发明的实验例4获得的随着时间的经过的毛发的生长程度。Fig. 5 shows the degree of hair growth over time obtained according to Experimental Example 4 of the present invention.
【实施方式】【Implementation】
为了达成如上所述的目的,本发明优选的一实例提供毛发及头皮状态改善用组合物,该毛发及头皮状态改善用组合物包含选自由芦根、芍药、茯神、石苇、荠苨、塞纳叶、紫檀香、草果、泽泻、贯众、亚麻仁、葛花、姜黄、瓜蒌仁、麻仁及苏木组成的组中的一种以上的提取物作为有效成分。In order to achieve the above-mentioned purpose, a preferred example of the present invention provides a composition for improving hair and scalp condition, the composition for improving hair and scalp condition comprises a composition selected from the group consisting of reed root, peony root, Fushen, stone reed, chestnut marmoset, More than one extract from the group consisting of senna leaf, red sandalwood, grass fruit, alisma, guanzhong, flax seed, kudzu flower, turmeric, melon seeds, hemp seed and sumac is used as an active ingredient.
并且,本发明再一优选一实例提供包含上述组合物的头发用组合物。And, another preferred embodiment of the present invention provides a composition for hair comprising the above-mentioned composition.
并且,本发明另一优选一实例提供毛发及头皮状态的改善方法,该毛发及头皮状态的改善方法包括将选自由芦根、芍药、茯神、石苇、荠苨、塞纳叶、紫檀香、草果、泽泻、贯众、亚麻仁、葛花、姜黄、瓜蒌仁、麻仁及苏木组成的组中的一种以上的提取物向患有脱发的个体给药的步骤。And, another preferred example of the present invention provides a method for improving the condition of hair and scalp. The method for improving the condition of hair and scalp includes a method selected from the group consisting of reed root, peony, Fushen, stone reed, marmoset, senna leaf, rosewood, A step of administering one or more extracts from the group consisting of Caoguo, Alisma, Guanzhong, Linseed, Pueraria japonica, Turmeric, Gualou Seed, Hemp Seed and Sappan to an individual suffering from alopecia.
并且,本发明还一优选一实例提供上述毛发及头皮状态改善用组合物的制备方法,该毛发及头皮状态改善用组合物的制备方法包括:利用水、乙醇或它们的混合溶剂来提取选自由芦根、芍药、茯神、石苇、荠苨、塞纳叶、紫檀香、草果、泽泻、贯众、亚麻仁、葛花、姜黄、瓜蒌仁、麻仁及苏木组成的组中的一种以上的步骤;Moreover, another preferred example of the present invention provides a method for preparing the composition for improving the condition of hair and scalp. The method for preparing the composition for improving the condition of hair and scalp includes: using water, ethanol or their mixed solvents to extract In the group consisting of reed root, peony, Fushen, stone reed, marmoset, senna leaf, red sandalwood, grass fruit, Alisma, guanzhong, flax seed, kudzu flower, turmeric, melon seed, hemp seed and sumac more than one step of
将通过上述提取步骤获得的提取物进行减压过滤的步骤;以及a step of subjecting the extract obtained through the above extraction step to filtration under reduced pressure; and
将通过上述过滤步骤获得的过滤液进行减压浓缩的步骤。A step of concentrating the filtrate obtained through the above-mentioned filtration step under reduced pressure.
以下,对本发明进行更为详细的说明。Hereinafter, the present invention will be described in more detail.
5-α还原酶(testosterone 5α-reductase)将雄激素中之一的睾酮(testosterone)转化为作为活性雄激素的二氢睾酮(DHT,dihydrotestosterone),如此活性化的二氢睾酮与雄激素受体相结合,并延迟毛囊细胞的蛋白质合成,从而缩短毛囊的生长期,并使毛囊萎缩,来引发脱发。并且,在雄激素性脱发过程中,也过度生成皮脂,最终,头皮中发生伴随炎症的脱发[Dennis A.15Holt,et.al,J Med.Chem.,33,943,(1990)]。5-α-reductase (testosterone 5α-reductase) converts testosterone (testosterone), one of the androgens, into dihydrotestosterone (DHT, dihydrotestosterone) as an active androgen, and the activated dihydrotestosterone interacts with the androgen receptor Combines and delays the protein synthesis of hair follicle cells, thereby shortening the anagen phase of hair follicles, and causing hair follicles to shrink, causing hair loss. Also, during androgenetic alopecia, sebum is excessively produced, and eventually, alopecia with inflammation occurs in the scalp [Dennis A. 15 Holt, et. al, J Med. Chem., 33, 943, (1990)].
因此,通过抑制上述5-α还原酶,能够防止脱发并促进生发,并且,能够防止或减少皮脂分泌及头皮屑,也能够预防或改善头皮炎症(Olsen EA,Hordinsky M,Whiting D,et al"The importance of dual5alpha-reductase inhibition in 20 the treatment of MPB:results of arandomized placebo-controlled study of dutasteride versusfinasteride".J Am Acad Dermatol.55(6),2006,Leyden,James;Dunlap,Frank;Miller,Bruce;Winters,Peter;Lebwohl,Mark;Hecker,David;Kraus,Stephen;Baldwin,Hilary et al."Finasteride in the treatmentof men with frontal male pattern hair loss".Journal of the 25American Academy of Dermatology 40(6 Pt 1):930–7.,1999)。Therefore, by inhibiting the above-mentioned 5-α reductase, hair loss can be prevented and hair growth can be promoted, and sebum secretion and dandruff can be prevented or reduced, and scalp inflammation can also be prevented or improved (Olsen EA, Hordinsky M, Whiting D, et al" The importance of dual5alpha-reductase inhibition in 20 the treatment of MPB:results of arandomized placebo-controlled study of dutasteride versus finasteride".J Am Acad Dermatol.55(6),2006,Leyden,James;Dunlap,Frank;Miller,Brace Winters, Peter; Lebwohl, Mark; Hecker, David; Kraus, Stephen; Baldwin, Hilary et al."Finasteride in the treatment of men with frontal male pattern hair loss".Journal of the 25American Academy of Dermatology 40(6 Pt 1): 930–7., 1999).
本发明人为了与毛发及头皮状态改善相关地开发可代替频繁发生无需的副作用的现有的药剂的既没有副作用又没有毒性且对改善毛发及头皮状态具有突出的效果的新形态的来源于天然物的制剂而进行研究,结果,确认了特定药材的提取物及其分馏物抑制5-α还原酶(testosterone 5a-reductase)的效果显著突出,从而完成了本发明。In order to improve the condition of hair and scalp, the present inventors developed a new form of natural medicine that has no side effects and no toxicity and has an outstanding effect on improving the condition of hair and scalp, which can replace existing drugs that frequently cause unnecessary side effects. As a result, it was confirmed that an extract of a specific medicinal material and a fraction thereof have a remarkable inhibitory effect on 5-alpha reductase (testosterone 5a-reductase), thus completing the present invention.
在本说明书中,“提取物”是指从各药材的各种器官,如从叶、花、茎、果实、种子及根等或全草中提取而获得的物质。In this specification, "extract" refers to substances extracted from various organs of various medicinal materials, such as leaves, flowers, stems, fruits, seeds, roots, etc., or whole plants.
并且,在本说明书中,“改善”是指使用为包括症状的预防或治疗,并包括出现症状的范围的减少、症状进行的延迟或缓解、症状的减轻或稳定化、部分或完全恢复、其他不同的有利结果等,尤其是指毛发及头皮状态的改善。Also, in this specification, "improvement" refers to use including prevention or treatment of symptoms, and includes reduction of the range of symptoms, delay or alleviation of symptom progression, alleviation or stabilization of symptoms, partial or complete recovery, other Various beneficial results etc., especially improvement of hair and scalp condition.
更具体地,上述毛发及头皮状态的改善可以优选为预防或治疗(促进生发)脱发,并且,可以优选为皮脂分泌的减少、头皮屑的防止或头皮炎症的防止。More specifically, the above-mentioned improvement of the condition of hair and scalp may preferably be the prevention or treatment (promotion of hair growth) of alopecia, and may be preferably the reduction of sebum secretion, the prevention of dandruff, or the prevention of scalp inflammation.
本发明优选一实例的毛发及头皮状态改善用组合物包含选自16种药材的一种以上的提取物作为有效成分。The hair and scalp condition improving composition according to a preferred example of the present invention contains, as an active ingredient, one or more extracts selected from 16 medicinal materials.
作为上述药材,有芦根、芍药、茯神、石苇、荠苨、塞纳叶、紫檀香、草果、泽泻、贯众、亚麻仁、葛花、姜黄、瓜蒌仁、麻仁及苏木,对上述药材进行更为详细的说明。As the above-mentioned medicinal materials, there are reed root, peony, Fushen, Shiwei, shepherd's marmoset, senna leaf, red sandalwood, grass fruit, Alisma, Guanzhong, flaxseed, kudzu flower, turmeric, melon seeds, hemp seeds and sage Wood, the above medicinal materials are described in more detail.
首先,芦根(Phragmites communis)作为芦苇的根茎,对热性病有效,是治疗肺热引起的咳嗽、肺结核、肺脓肿、胃热引起的呕吐等的药材,芍药(Paeoniae Radix)亢进消化道运动能力,来促进消化及吸收,对镇痛、镇痉、镇静作用及胃酸分泌有抑制效果,可使用白芍药、赤芍药、胡芍药、草芍药等各种品种。First of all, reed root (Phragmites communis), as the rhizome of reed, is effective against febrile venereal diseases, and is a medicinal material for treating cough caused by lung heat, tuberculosis, lung abscess, vomiting caused by stomach heat, etc. Paeoniae Radix hyperactive digestive tract motility , to promote digestion and absorption, and have analgesic, antispasmodic, sedative effects and inhibitory effects on gastric acid secretion. Various varieties such as white peony, red peony, red peony, grass peony, etc. can be used.
茯神为在多孔菌科的茯苓(Poria cocos)的中间天然地抱有松根的白色部分,使用为宁心、并治疗失眠症、健忘症等的药材,石苇(Pyrrosia lingua(Thunberg)Farwell或同属植物)的叶和根具有镇咳、祛痰、平喘作用,从而用作药材。并且,对作为泌尿生殖器疾病的淋病、尿道炎、膀胱炎、肾炎等症状呈现利尿解热效果,对于尿道结石,也与其他药物配合而利用。对慢性支气管炎有效,也对急慢性肾炎、肾盂肾炎呈现消炎及利尿作用。Fushen is the white part of Poria cocos (Poria cocos) that naturally holds pine roots in the middle of Polyporaceae. The leaves and roots of the same plant) have antitussive, expectorant, and antiasthmatic effects, so they are used as medicinal materials. In addition, it exhibits diuretic and antipyretic effects on symptoms such as gonorrhea, urethritis, cystitis, and nephritis, which are urogenital diseases, and it is also used in combination with other drugs for urethral calculi. It is effective for chronic bronchitis, and also has anti-inflammatory and diuretic effects for acute and chronic nephritis and pyelonephritis.
荠苨(Adenophora remotiflora(Siebold&Zucc.)Miq.)的根具有清热、解毒、化痰的功效,是使用于解毒、疖子治疗、祛痰等的药材,塞纳叶(番泻叶,Senna alexandrina)起到泻下作用、抗菌、抗生及箭毒样作用。The root of marmoset (Adenophora remotiflora (Siebold&Zucc.) Miq.) has the effects of clearing heat, detoxifying, and reducing phlegm. It is a medicinal material used for detoxification, boil treatment, and expectorant. Laxative effect, antibacterial, antibiotic and curare-like effects.
紫檀香为紫檀(Pterocarpus santalinus Linne(豆科,Leguminosae)的树干,具有冷血、止血、解毒、消肿、止痛的功效,从而以口服或外用的方式用于创伤出血或疮痈肿毒,草果(Amomum tsao-ko Crevstet Lemaire)用于减少冷气,暖心,停止呕吐,并解除腹部胀满。与此同时,具有祛痰的功效,此外,应用于腹痛、痰饮引起的胀满症、胃癌引起的呕吐、腹泻等。Pterocarpus santalinus Linne (Pterocarpus santalinus Linne (Leguminosae)) has the effects of cooling blood, hemostasis, detoxification, detumescence, and pain relief, so it can be used for wound bleeding or sore carbuncle swollen poison in oral or external use. (Amomum tsao-ko Crevstet Lemaire) is used to reduce cold air, warm the heart, stop vomiting, and relieve abdominal fullness. At the same time, it has the effect of eliminating phlegm. In addition, it is used for abdominal pain, fullness caused by phlegm, gastric cancer Vomiting, diarrhea, etc.
泽泻(Alisma canaliculatum)以晒干块根的方式用作药材,吸入身体的湿气,降低血糖和血压,由此不仅对糖尿病有效,还去除血压中的废物和胆固醇,从而具有使血液流动顺畅的功效,用于肾炎、膀胱炎、尿道炎、糖尿、高血压、脂肪肝等症状。Alisma canaliculatum is used as a medicinal material in the form of sun-dried roots, absorbs moisture from the body, lowers blood sugar and blood pressure, and thus is not only effective for diabetes, but also removes waste and cholesterol in blood pressure, thereby having the effect of smoothing blood flow. Efficacy, for nephritis, cystitis, urethritis, diabetes, high blood pressure, fatty liver and other symptoms.
贯众(Dryopteris crassirhizoma NAKAI)作为属于蕨类植物绵马科的植物,贯众的根茎作为其成分,已知有绵马素(filmaron)、间苯三酚(phloroglucinol)等,作为药理效果,已知有绦虫治疗剂、感冒治疗剂等。Dryopteris crassirhizoma NAKAI is a plant belonging to the family Pteridophyceae, and the rhizome of Dryopteris crassirhizoma NAKAI is known to contain filmaron, phloroglucinol, etc. There are tapeworm remedies, cold remedies, and the like.
亚麻仁作为属于亚麻科(Linaceae)的亚麻(Linum usitatissimumLinne)的成熟的种子,用于糖尿病和肠道疾病的治疗,并对支气管的卡他性疾病用作冷浸剂,葛花(Pueraria thunberginia)主要使用未完全开花的花朵,用于暴饮引起的头痛、发热、干渴、食欲不振、腹部膨胀及呕吐症。Flaxseed as mature seeds of flax (Linum usitatissimum Linne) belonging to the Linaceae family (Linaceae), used in the treatment of diabetes and intestinal diseases, and as a cold infusion for catarrhal diseases of the bronchi, kudzu flower (Pueraria thunberginia) The incompletely bloomed flowers are mainly used for headache, fever, thirst, loss of appetite, abdominal distension and vomiting caused by overeating.
姜黄(Curcuma longa)作为干燥属于姜科的多年生本草的根茎而得的,具有消除瘀血,通气顺畅,解决过了月经期也不来月经的问题,并止痛的功效的药材。Turmeric (Curcuma longa) is obtained by drying the rhizome of perennial herb belonging to Zingiberaceae. It has the effects of eliminating blood stasis, smoothing ventilation, solving the problem of menstruation after menstruation, and relieving pain.
并且,瓜蒌仁指葫芦科的栝楼(Trichosanthes kirilowiiMaximowicz)或黄栝楼(Trichosanthes kirilowii Max.var.japonicaKitamura)的种子,具有痰热咳嗽、便秘、疖子、乳汁分泌促进等效果。尤其,当因热性支气管炎而难以吐痰时,保护肺,柔肺,通气祛痰,且对极性支气管炎、胸膜炎、肺炎等有效。In addition, Gualou Ren refers to the seeds of Trichosanthes kirilowii Maximowicz or Trichosanthes kirilowii Max.var.japonica Kitamura of Cucurbitaceae, which has the effects of phlegm-heat cough, constipation, boils, and promotion of milk secretion. Especially when it is difficult to spit up due to febrile bronchitis, it protects the lungs, softens the lungs, ventilates and eliminates phlegm, and is effective for polar bronchitis, pleurisy, pneumonia, etc.
已知麻仁作为大麻(Cannabis sativa)的种子,其脂肪丰富,且有光泽,因而具有使干物质润泽,有助于柔和地疏通肠道,并使血液循环顺畅的功效,也对难产、肿痛等用作镇痛剂。Known as the seed of hemp (Cannabis sativa), hemp seed is rich in fat and shiny, so it has the effect of moistening dry matter, helping to gently dredge the intestinal tract, and making blood circulation smooth. Pain, etc. are used as an analgesic.
苏木(Caesalpinia sappan L.)作为属于豆科(Leguminosae)的植物,被称为苏方木、苏方、赤木、红紫等,苏木不自生在韩国,而是分布在中国福建省、广东省、广西省、贵州省、云南省、海南省、台湾等。将苏木树的茎和粗枝的心材称为苏木,已知具有对于心脏和血管的作用、中枢抑制作用、抗菌作用、降血糖作用。Sappan (Caesalpinia sappan L.) is a plant belonging to the leguminosae (Leguminosae) and is known as sappan, sappan, red wood, red purple, etc. Sappan does not grow in Korea by itself, but is distributed in Fujian, Guangdong, China Province, Guangxi Province, Guizhou Province, Yunnan Province, Hainan Province, Taiwan, etc. The heartwood of the stem and thick branches of the hematoxylin tree is called hematoxylin, and it is known to have an action on the heart and blood vessels, a central inhibitory action, an antibacterial action, and a hypoglycemic action.
本发明一实例的毛发及头皮状态改善用组合物包含5-α还原酶(testosterone 5a-reductase)抑制活性突出的上述16种药材中的一种以上的提取物作为有效成分,由此能够显著改善毛发及头皮状态。优选地,可包含芦根、芍药、茯神、石苇、麻仁及苏木的提取物。The composition for improving hair and scalp condition according to an example of the present invention contains as an active ingredient one or more extracts of the above-mentioned 16 kinds of medicinal materials having excellent testosterone 5a-reductase inhibitory activity, thereby being able to significantly improve hair and scalp conditions. Hair and scalp condition. Preferably, it may contain extracts of reed root, peony, Fushen, stone reed, hemp seed and sumac.
另一方面,优选地,上述提取物中的芦根、芍药、茯神、葛花及苏木的提取物能够以粉末形态包含,优选地,石苇、荠苨、塞纳叶、紫檀香、草果、泽泻、贯众、亚麻仁及姜黄的提取物能够以提取液形态包含,瓜蒌仁的提取物能够以油形态包含,并且,麻仁的提取物能够以稀的液体形态包含。On the other hand, preferably, the extracts of reed rhizome, peony, Fushen, kudzu flower and sumac in the above-mentioned extracts can be included in powder form, preferably, stone reed, shepherd's marmoset, senna leaf, red sandalwood, grass The extracts of fruit, Alisma, Rhizome, linseed and turmeric can be contained in the form of extract liquid, the extract of Trichosanthes semen can be contained in the form of oil, and the extract of hemp seed can be contained in the form of dilute liquid.
上述毛发及头皮状态改善用组合物可根据各个不同领域通常所使用的方法,进一步包含适当的载体、赋形剂及稀释剂等,从而适用为药学组合物、功能性食品组合物或头发组合物。The above hair and scalp condition improving composition may further contain appropriate carriers, excipients, diluents, etc. according to methods commonly used in various fields, thereby being suitable as a pharmaceutical composition, a functional food composition, or a hair composition. .
提供为药学组合物的情况下,上述组合物可根据通常的方法以口服或非口服方式进行给药,例如,当以口服方式进行给药时,能够以散剂、颗粒剂、片剂、悬浮剂、乳胶、糖浆等剂型使用。In the case of providing a pharmaceutical composition, the above-mentioned composition can be administered orally or parenterally according to a usual method, for example, when administered orally, it can be in the form of powder, granule, tablet, suspension , latex, syrup and other dosage forms.
优选的给药量可以为适合给药对象和/或疾病的治疗或预防的含量,这可根据给药对象的年龄、性别、一般健康状态及体重、疾病的种类及重症度、剂型的种类、组合物中所含有的其他成分的种类及含量、组合物的分泌率、给药途径及期间等各种因素而调节,可由本发明所属技术领域的普通技术人员适当地选择。作为上述给药对象,可以为包括人类的哺乳类。The preferred dosage can be a content suitable for the treatment or prevention of the subject and/or disease, which can be based on the subject's age, sex, general health status and body weight, the type and severity of the disease, the type of dosage form, The type and content of other components contained in the composition, the secretion rate of the composition, the route and period of administration, etc. can be adjusted according to various factors, and can be appropriately selected by those skilled in the art to which the present invention pertains. Mammals including humans can be used as the subject of administration.
上述组合物提供为头发组合物形态的情况下,以整个头发组合物重量为基准,优选地,可包含0.0001~99.9重量百分比的上述毛发及头皮状态改善用组合物,更优选地,可包含0.1~50重量百分比的上述毛发及头皮状态改善用组合物,优选地,能够以选自由爽发水、润发露、发乳、发胶、发用摩丝、头发定型膏、洗发皂、洗发水、护发素、护发膜及焗油膏组成的组中的剂型提供。When the above-mentioned composition is provided in the form of a hair composition, based on the weight of the entire hair composition, preferably, it may contain 0.0001 to 99.9% by weight of the composition for improving the condition of hair and scalp, and more preferably, it may contain 0.1 ~50% by weight of the above hair and scalp condition improving composition, preferably, can be selected from shampoo, conditioner, hair cream, hair gel, hair mousse, hair styling cream, shampoo soap, shampoo, Dosage forms in the group consisting of conditioner, hair mask, and hair balm are offered.
作为本发明的再一优选一实例,提供毛发及头皮状态改善方法,上述毛发及头皮状态改善方法包括将5-α还原酶(testosterone5a-reductase)抑制活性突出的上述16种药材中的一种以上的提取物向患有脱发的个体给药的步骤。As yet another preferred example of the present invention, there is provided a method for improving hair and scalp conditions, the method for improving hair and scalp conditions comprising at least one of the above-mentioned 16 kinds of medicinal materials with outstanding 5-α reductase (testosterone 5a-reductase) inhibitory activity A step of administering an extract of the method to an individual suffering from alopecia.
上述“给药”的步骤能够以口服或非口服的方式实现,当以非口服方式给药时,可选择皮肤外用、皮下注射注入方式、经皮给药及局部给药等,但并不局限于此。优选地,作为皮肤外用,可利用涂敷于皮肤的方法。The above-mentioned "administration" step can be implemented in an oral or non-oral manner. When administering in a non-oral manner, external application to the skin, subcutaneous injection, transdermal administration, and local administration can be selected, but it is not limited here. Preferably, for external use on the skin, a method of applying to the skin is available.
局部给药的情况下,可利用软膏、霜或凝胶等半固体(semisolid)制剂来给药,经皮给药的情况下,除了基质贴剂或储库型贴剂(reservoir patch)之外,还可利用半固体产品(水醇凝胶等),但并不局限于此。In the case of topical administration, semisolid preparations such as ointments, creams, or gels can be used for administration, and in the case of transdermal administration, in addition to matrix patches or reservoir patches (reservoir patch) , semi-solid products (hydroalcoholic gels, etc.) can also be utilized, but are not limited thereto.
根据本发明优选的其他一实例,提供上述毛发及头皮状态改善用组合物的制备方法。According to another preferred example of the present invention, there is provided a method for producing the aforementioned hair and scalp condition improving composition.
优选地,上述制备方法包括:利用水、乙醇或它们的混合溶剂来提取选自由芦根、芍药、茯神、石苇、荠苨、塞纳叶、紫檀香、草果、泽泻、贯众、亚麻仁、葛花、姜黄、瓜蒌仁、麻仁及苏木组成的组中的一种以上的步骤;将通过上述提取步骤获得的提取物进行减压过滤的步骤;以及将通过上述过滤步骤获得的过滤液进行减压浓缩的步骤。Preferably, the above preparation method includes: using water, ethanol or their mixed solvents to extract the selected from reed root, peony, Fushen, Shiwei, marmoset, Senna leaf, red sandalwood, Tsaoguo, Alisma, Guanzhong, More than one step in the group consisting of linseed, kudzu flower, turmeric, melon seeds, hemp seed and sumac; the step of decompression filtering the extract obtained through the above extraction step; and the step of filtering the extract obtained through the above filtration step The obtained filtrate was subjected to a step of concentrating under reduced pressure.
为了更加提高提取效果,优选地,上述各药材在提取步骤之前可经过粉碎的工序,尤其,在上述药材中,具有果实或种子等形态的,例如,可利用剪刀等工具剪开之后,进行粉碎来使用。粉碎方法不受特别的限制,例如,可使用搅拌器等各种工具来实现。In order to further improve the extraction effect, preferably, each of the above-mentioned medicinal materials can be crushed before the extraction step. In particular, among the above-mentioned medicinal materials, those that have the form of fruits or seeds, for example, can be crushed after being cut with scissors and other tools. to use. The pulverization method is not particularly limited, for example, various tools such as a stirrer can be used.
优选地,上述提取步骤可通过单独提取各药材或者混合所有药材来以混合物状态提取的方法实现,单独提取各药材来使用的情况下,提取溶剂可相同或不同。Preferably, the above-mentioned extraction step can be realized by extracting each medicinal material individually or by mixing all the medicinal materials to extract in a mixture state. When each medicinal material is extracted and used separately, the extraction solvents may be the same or different.
并且,优选地,上述提取步骤可通过在将各药材或它们的混合物与提取溶剂进行混合之后浸出的方法实现。And, preferably, the above-mentioned extraction step can be realized by leaching after mixing each medicinal material or their mixture with an extraction solvent.
优选地,上述浸出可在30至40℃的温度范围内实现,更优选地,可在33至38℃的温度下实现,优选地,可浸出1至3天,更优选地,可浸出45至50小时。Preferably, the above-mentioned leaching can be realized at a temperature range of 30 to 40°C, more preferably at a temperature of 33 to 38°C, preferably for 1 to 3 days, more preferably for 45 to 45°C 50 hours.
提取溶剂不受特别的限制,但优选地,可使用水、乙醇或它们的混合溶剂来提取,更优选地,可使用乙醇,最优选地,可使用60至80%(v/v)的乙醇。The extraction solvent is not particularly limited, but preferably, water, ethanol or their mixed solvents can be used for extraction, more preferably, ethanol can be used, most preferably, 60 to 80% (v/v) ethanol can be used .
并且,优选地,按每药材100g可使用400ml至800ml的上述提取溶剂。And, preferably, 400ml to 800ml of the above-mentioned extraction solvent may be used per 100g of the medicinal material.
上述减压过滤步骤不受特别的限制,可通过该领域中公知的方法实现。The above-mentioned vacuum filtration step is not particularly limited, and can be achieved by methods known in the art.
优选地,通过上述过滤步骤获得的过滤液可进一步经过减压浓缩的步骤。上述减压浓缩步骤不受特别的限制,可通过该领域中公知的方法实现,在上述步骤之后,还可选择性地包括冷冻干燥的步骤等。Preferably, the filtrate obtained through the above filtration step can be further subjected to a step of concentrating under reduced pressure. The above step of concentrating under reduced pressure is not particularly limited, and can be realized by methods known in the art. After the above steps, a freeze-drying step can also be optionally included.
以下,通过实施例对本发明进行详细说明。只是,以下实施例仅用于例示本发明,本发明并不局限于以下实施例。Hereinafter, the present invention will be described in detail through examples. However, the following examples are only for illustrating the present invention, and the present invention is not limited to the following examples.
【实施例】【Example】
【实施例1:提取物的制备】[Example 1: Preparation of extract]
准备芦根、芍药、茯神、石苇、荠苨、塞纳叶、紫檀香、草果、泽泻、贯众、亚麻仁、葛花、姜黄、瓜蒌仁、麻仁及苏木并分别进行了粉碎。用剪刀剪开果实或种子之后进行了粉碎。Prepare reed root, peony, Fushen, stone reed, marmoset, senna leaf, red sandalwood, grass fruit, Alisma, guanzhong, flax seed, kudzu flower, turmeric, melon seed, hemp seed and sumac respectively smashed. The crushing is carried out after cutting the fruit or seeds with scissors.
在1000ml瓶子(Duran)中添加粉碎的上述药材100g和70%(v/v)乙醇(EtOH)600ml进行混合之后,在恒温水槽中以35℃温度浸出了48小时。After adding and mixing 100 g of the pulverized medicinal materials and 600 ml of 70% (v/v) ethanol (EtOH) in a 1000 ml bottle (Duran), it was leached in a constant temperature water tank at a temperature of 35° C. for 48 hours.
利用过滤纸(沃特曼(Watman)21号过滤器)来将获得的浸出物进行减压过滤之后,利用减压浓缩器来浓缩回收的过滤液,从而获得了下列表1的生药提取物(根据生药,以提取液、粉末形态、稀的液体回收)。向50ml管分注制备的提取物之后,利用石蜡膜(Parafilm)来进行密封,并冷藏保管。Utilize filter paper (Watman (Watman) (Watman) No. 21 filter) to carry out after decompression filtration of the extract that obtains, utilize decompression concentrator to concentrate the filtrate that reclaims, thereby obtained the crude drug extract of following table 1 ( Depending on the crude drug, it is recovered in the form of extract, powder, or dilute liquid). After dispensing the prepared extract into a 50 ml tube, it was sealed with parafilm (Parafilm), and it was stored in refrigeration.
【表1】【Table 1】
【实验例1:利用GC-MS的睾酮(testosterone)和二氢睾酮的定量分析】[Experimental example 1: Quantitative analysis of testosterone and dihydrotestosterone by GC-MS]
将用于反应后所提取的肝微粒体部分(liver microsomal fraction)中的睾酮(testosterone)和二氢睾酮(DHT)的定量分析的色谱图(chromatogram)示于图1至图4中。The chromatograms used for the quantitative analysis of testosterone and dihydrotestosterone (DHT) in the liver microsomal fraction extracted after the reaction are shown in FIGS. 1 to 4 .
【实验例2:5-α还原酶抑制功效评价测定】[Experimental Example 2: Evaluation and Determination of 5-α Reductase Inhibition Efficacy]
为了评价通过上述实施例l获得的提取物的5-α还原酶抑制功效,首先,作为对照药物,利用非那雄胺(finasteride)(Mertk)来确立了微粒体部分(Microsomal fraction)提取条件。In order to evaluate the 5-alpha reductase inhibitory effect of the extract obtained in Example 1 above, first, the microsomal fraction (Microsomal fraction) extraction conditions were established using finasteride (Mertk) as a control drug.
具体地,利用均质器(Homogenizer)、组织均质化试剂盒(tissuehomogenize kit)、组织研磨仪(TissueLyzer)来分别分馏了上述非那雄胺来获得了分馏物,并以此为对象进行了比较实验,从而获得了下列表2的结果。Specifically, using a homogenizer (Homogenizer), a tissue homogenization kit (tissuehomogenize kit), and a tissue grinder (TissueLyzer) to fractionate the above-mentioned finasteride to obtain fractions, and use this as an object to carry out The experiments were compared to obtain the results in Table 2 below.
【表2】【Table 2】
如上述表2所示,在用于提取微粒体分馏物的三个条件中,确认到了5-α还原酶的功效,但使用组织研磨仪的情况下,5-α还原酶的功效呈现相对低的值,由此可知5-α还原酶的活性被抑制。As shown in Table 2 above, in the three conditions used to extract microsomal fractions, the efficacy of 5-α reductase was confirmed, but in the case of using a tissue grinder, the efficacy of 5-α reductase was relatively low It can be seen that the activity of 5-α reductase is inhibited.
反复2次对基于均质器的分馏物进行实验,并确认到了对于5-α还原酶抑制功效评价的再现性,如下列表3。The experiment was repeated twice on the homogenizer-based fraction, and the reproducibility of the evaluation of the 5-α reductase inhibitory efficacy was confirmed, as shown in Table 3 below.
【表3】【table 3】
【实验例3:评价天然提取物抑制5-α还原酶的功效】[Experimental Example 3: Evaluation of the efficacy of natural extracts in inhibiting 5-α reductase]
为了评价通过上述实施例1获得的天然提取物抑制5-α还原酶的功效,分别将各个天然提取物和睾酮(testosterone)溶解于二甲基亚砜(DMSO,dimethyl sulfoxide)和甲醇(MeOH)中使用。In order to evaluate the efficacy of the natural extracts obtained in Example 1 above in inhibiting 5-alpha reductase, each natural extract and testosterone were dissolved in dimethyl sulfoxide (DMSO, dimethyl sulfoxide) and methanol (MeOH) respectively. used in .
首先,为了了解对两种有机溶剂的影响,分别以10μg/mL的浓度在二甲基亚砜和甲醇中稀释100μg/mL的睾酮溶液进行比较实验,并将由此得到的结果示于下列表4中。First, in order to understand the influence of the two organic solvents, a 100 μg/mL testosterone solution was diluted in dimethyl sulfoxide and methanol at a concentration of 10 μg/mL for a comparative experiment, and the results obtained are shown in the following Table 4 middle.
【表4】【Table 4】
如上述表4所示,在稀释了睾酮的两种溶剂中,均可确认到5-α还原酶的功效,从呈现像这样类似的结果值的方面考虑,可以确认没有基于有机溶剂的影响。As shown in Table 4 above, the efficacy of 5-α reductase was confirmed in both solvents in which testosterone was diluted, and it was confirmed that there was no influence of the organic solvent from the point of view of similar result values.
利用建立的5-α还原酶的功效分析方法,使用根据上述实施例1获得的16种天然提取物和作为对照组以与上述实施例1相同的方法提取而获得的龙眼肉提取物、赤小豆提取物及酸枣仁提取物,从而反复2次对5-α还原酶的抑制功效进行实验,并将由此得到的结果示于下列表5中。Utilize the effect analysis method of the 5-alpha reductase of establishment, use 16 kinds of natural extracts obtained according to the above-mentioned Example 1 and the longan meat extract obtained by extracting in the same way as the above-mentioned Example 1 as a control group, and the red bean extract 5-alpha reductase inhibitory effect experiment was repeated twice, and the results thus obtained are shown in Table 5 below.
【表5】【table 5】
如上述表5所示,根据本发明实施例1获得的药材16种提取物完全没有呈现5-α还原酶的功效,从而可以确认抑制5-α还原酶的功效突出,相反,在作为对照组的龙眼肉提取物、赤小豆提取物及酸枣仁提取物中,可以确认与所使用的浓度无关地,没有抑制5-α还原酶的功效。尤其,可知本发明16种天然提取物全部与现有的已知的阳性对照组(positive control)即苦参一样,抑制5-α还原酶的功效突出。As shown in the above table 5, the 16 kinds of extracts of medicinal materials obtained according to Example 1 of the present invention do not exhibit the effect of 5-alpha reductase at all, so that it can be confirmed that the effect of inhibiting 5-alpha reductase is outstanding, on the contrary, in the control group In the longan meat extract, the red bean extract, and the Jujube seed extract, it was confirmed that there was no 5-α reductase inhibitory effect regardless of the concentration used. In particular, it can be seen that all 16 kinds of natural extracts of the present invention have the same effect on inhibiting 5-α reductase as the conventional known positive control (positive control), that is, Sophora flavescens.
【实验例4:利用本发明组合物的小鼠毛发生长促进效果的测定】[Experimental example 4: Determination of mouse hair growth promoting effect using the composition of the present invention]
为了了解本发明防脱发及毛发生长促进用组合物的效果,利用C57BL/6N小鼠来确认了本组合物的毛发生长促进效果。上述防脱发及毛发生长促进用组合物使用了麻仁提取物及苏木提取物。将C57BL/6N小鼠进入第二个退化期(catagen)的生后7周的小鼠的毛完全去除后,针对每10只小鼠一天一次涂敷了各150μl的本发明组合物和对照物质,连续涂敷了5周。用肉眼比较了随着时间的经过的毛发生长促进程度,并导出了结论(图5)。作为阴性对照组,使用了没有毛发生长促进效果的80%乙醇,作为阳性对照组,使用了3%米诺地尔。下列表6为通过肉眼观察比较分析随着时间的经过的毛发的生长程度的表。In order to understand the effect of the composition for hair loss prevention and hair growth promotion of the present invention, the hair growth promotion effect of the composition was confirmed using C57BL/6N mice. The above-mentioned composition for preventing hair loss and promoting hair growth uses hemp seed extract and sumac extract. After completely removing the hair of C57BL/6N mice at 7 weeks after birth in the second catagen, 150 μl each of the composition of the present invention and the control substance were applied to every 10 mice once a day. , applied continuously for 5 weeks. The degree of hair growth promotion over time was compared with the naked eye, and a conclusion was drawn ( FIG. 5 ). As a negative control group, 80% ethanol having no hair growth promoting effect was used, and as a positive control group, 3% minoxidil was used. Table 6 below is a table comparing and analyzing the degree of hair growth over time by visual observation.
【表6】【Table 6】
在上述表6中,“-”是指毛发几乎没有生长,“+”是指毛发随着时间的经过而生长,“+”的数量越多,毛发生长量就越多。可知在麻仁提取物及苏木提取物中毛发生长,这意味着本发明的组合物促进毛发生长。In the above Table 6, "-" means that the hair hardly grows, and "+" means that the hair grows with the lapse of time, and the more the number of "+" is, the greater the amount of hair growth is. It is known that hair grows in hemp seed extract and hematoxylin extract, which means that the composition of the present invention promotes hair growth.
【实验例5:生发面积的测定】[Experimental Example 5: Determination of Germinal Area]
对于通过上述实验例4获得的生发测定照片,为了测定去毛面积和生发面积的比率,使用了作为图像分析程序的i-Solution Lite。首先,测定去毛的整个面积,并测定生发的面积之后,以相对于整个面积的百分比(%)测定了生发比率。在下列表7中示出了随着时间的经过的去毛面积和毛发的生长比率。For the hair growth measurement photos obtained in Experimental Example 4 above, i-Solution Lite, which is an image analysis program, was used to measure the ratio of the hair removal area to the hair growth area. First, after measuring the entire area of hair removal and measuring the area of hair growth, the hair growth rate was measured as a percentage (%) relative to the entire area. The shaved area and the growth rate of hair are shown in Table 7 below with the lapse of time.
【表7】【Table 7】
按阳性对照组(3%米诺地尔)、HD-23(麻仁提取物)的顺序,呈现高的生发率,HD-124(苏木提取物)的情况下,在5周之后,可以确认显著的生发率的增加。In the order of the positive control group (3% minoxidil), HD-23 (seed seed extract), a high hair growth rate was exhibited, and in the case of HD-124 (sumacin extract), after 5 weeks, it was possible to A significant increase in hair growth rate was confirmed.
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