JP2015520228A - Composition for improving hair and scalp conditions containing natural extract as active ingredient, and method for producing the same - Google Patents

Abstract

The present invention relates to a hair and scalp condition improving composition containing a natural extract as an active ingredient, a method for producing the same, and a method for improving the condition of hair and scalp by administering the natural extract. The composition for improving hair and scalp condition according to No. 1 contains a natural extract as an active ingredient, has no fear of side effects or toxicity, does not require surgery, and can be applied economically and easily.

Description

  The present invention relates to a hair and scalp condition improving composition containing a natural extract as an active ingredient, and a method for producing the same, and a method for improving the condition of hair and scalp by administering the natural extract of the present invention. About.

  Male alopecia, the most common type of alopecia, is dihydrotestosterone (DHT), one of the male hormones, testosterone (testosterone), which is the active male hormone by 5α-reductase (testosterone 5α-reductase). The switched and activated dihydrotestosterone binds to the androgen receptor, delays protein synthesis in the hair follicle cells, shortens the hair follicle growth phase, shrinks the hair follicles, and removes hair loss. Trigger. In addition, sebum is excessively generated in the process of androgenic hair loss, and as a result, hair loss accompanied by inflammation appears in the scalp (see Non-Patent Document 1).

The usual hair loss treatment method is a hair transplantation method. That is, it is a method of transplanting a skin plug from which hair has come out from the scalp site where the hair grows to the hair removal site. Such a method is not only time consuming and relatively painful, but also expensive. Other non-drug treatments include ultraviolet radiation and exercise therapy.
Still another hair loss treatment is drug therapy. Merck, Inc. of the United States sells a hair growth agent manufactured by using finasteride for oral administration as a drug that inhibits the action of 5α reductase and suppresses the production of dihydrotestosterone (DHT). However, this has a problem that side effects due to steroidal drugs occur.
In addition, equol, which is a major metabolite of daidzein, a kind of phytoestrogens, directly binds to dihydrotestosterone (DHT) without any influence on testosterone, thereby causing a male hormone. The content of blocking the path of dihydrotestosterone (DHT) is reported.

  Therefore, there is a demand for the development of a natural product-derived therapeutic agent that is economical but does not cause various side effects or toxicity.

Dennis A.M. Holt, et. al, J Med. Chem. 33, 943, (1990)

  Therefore, in order to solve the above-mentioned problems, the present inventors have conducted experiments through Sone, Acupuncture, Akagami, Ishizuchi, Sobana, Senna leaf, Rosewood incense, Grass, Sawaka, Insane , Flaxseed, kuzuhana, kaoru, karonin, hemp and sugi extracts promote the growth of hair by inhibiting the efficacy of 5α reductase From the extract, the composition for improving hair and scalp conditions, its production method, and the method for improving hair and scalp conditions were clarified.

An object of this invention is to provide the composition for hair and scalp condition improvement which contains a natural extract as an active ingredient, and its manufacturing method.
In addition, the present invention includes radish, glaze, god of gods, sarcophagus, sobana, senna leaf, rosewood incense, grass, swamps, mulberry, flaxseed, kuzuhana, kyoou An object of the present invention is to provide a method for improving hair and scalp conditions, comprising the step of administering one or more extracts selected from the group consisting of garlic, hemp seed and soki to an individual having hair loss. And

  According to the present invention, a hair and scalp condition improving composition comprising a natural extract having an excellent inhibitory effect on 5α reductase as an active ingredient, a method for producing the same, and a method for improving the condition of hair and scalp by administering the natural extract Is provided. The hair and scalp condition improving composition contains a natural extract as an active ingredient, has no fear of side effects or toxicity, does not require surgery, and can be applied economically and easily.

FIG. 1 is an extracted-ion chromatography of d ₃ -testosterone obtained by Experimental Example 1 of the present invention ((a): Reference standard, (b): Microsoft fraction). FIG. 2 is an extracted-ion chromatography of testosterone obtained by Experimental Example 1 of the present invention ((a): Reference standard, (b): Microscopic fraction). FIG. 3 is an extracted-ion chromatogram of d ₃ -dihydrotestosterone (d ₃ -DHT) obtained by Experimental Example 1 of the present invention ((a): Reference standard, (b): Microscopic fraction). FIG. 4 is an extracted-ion chromatogram of dihydrotestosterone (DHT) obtained by Experimental Example 1 of the present invention ((a): Reference standard, (b): Microsoft fractionation). FIG. 5 is a drawing showing the degree of hair growth over time obtained in Experimental Example 4 of the present invention.

  In order to achieve the above-mentioned purpose, a preferred embodiment of the present invention includes a root, a glaze, a god, a sarcophagus, a sobana, a senna leaf, a rosewood incense, a grass fruit, a sardine, an intruder, For improving hair and scalp conditions containing as an active ingredient at least one extract selected from the group consisting of flaxseed, kuzuhana, kyouou, karonin, hemp and sugi A composition is provided.

Another desirable embodiment of the present invention provides a hair composition comprising the composition.
Further, another desirable specific example of the present invention is as follows: Sone, glaze, 茯神, 石 韋, sovana (soba), senna leaf, rosewood incense, herbaceous fruits, swallows, injuries, flaxseed, kuzuhana, Hair and scalp conditions including the step of administering one or more extracts selected from the group consisting of Kyoou, Karonin, hemp and Soki to individuals with hair loss Provide improvement methods.

  Further, another desirable specific example of the present invention is as follows: Sone, glaze, 茯神, 石 韋, sovana (soba), senna leaf, rosewood incense, herbaceous fruits, swallows, injuries, flaxseed, kuzuhana, Extracting one or more selected from the group consisting of Kyoou (Kouou), Karonin (Karojin), hemp and Soki with water, ethanol, or a mixed solvent thereof, and the extraction step A method for producing the hair and scalp condition improving composition comprising: a step of subjecting the extract obtained through filtration under reduced pressure; and a step of concentrating the filtrate obtained through the filtration step under reduced pressure.

Hereinafter, the present invention will be described in more detail.
5α reductase converts testosterone, which is one of the male hormones, to dihydrotestosterone (DHT), which is the active male hormone, and the activated dihydrotestosterone binds to the androgen receptor, thereby Delays protein synthesis, shortens hair follicle growth phase, causes hair follicles to shrink and induces hair loss. In addition, sebum is excessively produced in the process of androgenic hair loss, and as a result, hair loss accompanied by inflammation appears in the scalp [Dennis A. et al. 15 Holt, et. al, J Med. Chem. 33, 943, (1990)].

  Therefore, by inhibiting the 5α reductase, hair loss can be prevented, hair growth can be promoted, sebum secretion and scalp can be prevented or reduced, and scalp inflammation can be prevented or improved (Olsen EA, Hordinsky M, Whiting D, et al "The importance of dual 5alpha-reductaseinhibition in the treatment of MPB: results of a randomized placebo-controlled study of dutasteride versus finasteride" .J Am Acad Dermatol.55 (6), 2006, Leyden, James; Dunlap, Frank; Miller, Br uce; 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 American Academy of Dermatology 40 (6 Pt 1): 930-7, 1999).

  The inventors have no side effects or toxicity that can replace existing drugs that frequently cause undesirable side effects in connection with the improvement of the condition of hair and scalp, and have an excellent effect on improving the condition of hair and scalp. As a result of research for the development of a new form of natural product-derived preparation, the inventors have found that the extract of a specific medicinal material and the fraction thereof have a remarkably excellent 5α reductase inhibitory effect, and thus completed the present invention. .

In the present specification, the “extract” means one obtained by extracting from various organs of each medicine, for example, leaves, flowers, stems, fruits, seeds, roots, etc., or whole plants.
In this specification, 'improvement' means not only the prevention or treatment of symptoms, but also the reduction of the range of symptoms, delay or alleviation of symptom progression, reduction or stabilization of symptoms, partial or complete recovery, It is used in the sense of including any other advantageous results, and in particular, means an improvement in hair and scalp conditions.
More specifically, the improvement of the hair and scalp condition may desirably be prevention or treatment of hair loss (promotion of hair growth), and may desirably decrease sebum secretion, prevent scalp or prevent scalp inflammation. .
A composition for improving hair and scalp conditions according to a preferred embodiment of the present invention includes one or more extracts selected from 16 kinds of medicinal materials as active ingredients.
Examples of the chemicals include radish, glaze, god of gods, sarcophagus, sobana, senna leaves, rosewood incense, grasses, swamps, mulberry, flaxseed, kuzuhana, kyoou There are carrots, hemp seeds, and sugi, and the chemicals will be described in more detail as follows.

Phragmites communis is a rhizome of cocoons that is effective for heat-related diseases and is a drug for treating cough due to lung fever, pulmonary tuberculosis, lung abscess, vomiting due to gastric fever, and the like.
Paeoniae Radix enhances gastrointestinal motility, promotes digestion and absorption, has analgesic, antispasmodic, sedative and gastric acid secretion inhibitory effects. Various varieties can be used.

The sacred god is a white part that naturally holds a pine root in the middle of the Poria cocos, and is used as a medicine to calm the mind and treat insomnia, amnesia and the like.
Sarcophagus (Pyrrosia lingua (Thunberg) Farwell or the same genus) has antitussive, expectorant and flattening effects on leaves and roots and is used as a medicine. In addition, as a urogenital disease, it exhibits diuretic and antipyretic effects on symptoms such as hemorrhoids, urethritis, cystitis, nephritis, etc. It is also used in combination with other drugs for urethral stones. It is also effective in the treatment of late-onset bronchitis, and also exhibits anti-inflammatory and diuretic effects in acute chronic nephritis and pyelonephritis.

Adenophora remoflora (Siebold & Zucc.) Miq. Is a drug used for detoxification, swelling treatment, expectoration, etc., which has the effect of lowering heat to the roots, detoxifying and suppressing wrinkles.
Senna leaves (Sena alexandrina) have a laxative action, antibacterial, antibiotic and venom-like action.

Rosewood incense is the root of rosewood (Pterocarpus santalinus Linne (leguminous leguminosae)) and has the effect of cold blood, hemostasis, detoxification, antitumor, and pain relief, and is used as an internal or external application for wound bleeding and vaginosis.
Grass (Amoum tsao-ko Crevst et Lemaire) cures cold, warms the belly, stops vomiting, and eliminates abdominal distention. In the same way, it has the effect of eliminating sputum and is used for other abdominal pain, sputum due to sputum, vomiting due to stomach cancer, diarrhea and the like.

  Arisuma canalicatum is used as a medicine by drying tuberous roots, but it not only inhales moisture in the body and lowers blood sugar and blood pressure, but is effective in diabetes, but also removes waste products and cholesterol in the blood. It has the effect of improving blood flow and is used for symptoms such as nephritis, cystitis, urethritis, diabetes, hypertension and fatty liver.

  Dryopteris crushirhizoma NAKAI is a plant belonging to the ovine plant cottonseed family, and the rhizomes of the mushroom are known as components such as fimaron and phloroglucinol, and have pharmacological effects. As such, a tapeworm therapeutic agent, a cold therapeutic agent and the like are known.

Flaxseed is a well-ripened species of flax (Linum usitatisimum Linne) belonging to the Linaceae family, and is used as a cold soaking agent in the treatment of diabetes and bowel disease and bronchial catarrhal disease.
Kuzuka (Pueraria thunberginia) is mainly used for buds that are not fully flowered, and is used for headaches, fever, thirst, anorexia, abdominal distension, and vomiting due to excessive drinking.

  Curcuma longa is a dried rhizome of perennial herbs belonging to the family Ginger, which eliminates blood (blood), smoothes the flow of air, and passes through the menstrual period. It is a medicinal material that has the effect of stopping pain and making it easy to communicate that it does not occur.

  Karonin refers to the species of cucurbits of the cucurbitaceae (Trichosanthes kirirowii Maximowicz) or Trichosanthes kirirowiii Max. Var. Japonica Kitamura fever, There are effects such as. In particular, when fistula does not vomit well due to febrile bronchitis, it supplements and softens the lungs, lowers wrinkles and eliminates sputum, and is effective for acute bronchitis, pleurisy, pneumonia, etc.

  Hemp (Cannabis sativa) is a seed of cannabis sativa that is rich in fat, shiny, moisturized dry, helps the intestines softly pass, and has a smooth blood circulation effect It is known to be used as an analgesic for dystocia and tumor pain.

  Sugi (Caesalpinia sappan L.) is a plant belonging to the Leguminosae family, and is called Sukatagi, Sukata, Akagi, Red Purple, etc. , Guangdong, Guangxi, Guizhou, Yunnan, Hainan Island, Taiwan and so on. The heart material of the stem and thick branch of the tree is called a tree, and is known to have an action on the heart and blood vessels, a central inhibitory action, an antibacterial action, and a blood glucose lowering action.

The hair and scalp condition improving composition according to an embodiment of the present invention includes one or more extracts among the 16 kinds of medicines having excellent 5α reductase inhibitory activity as an active ingredient. It can significantly improve the condition of the scalp. Desirably, it can include extracts of roots, glazes, gods of deity, stalagmites, hemp seeds, and sugi.
On the other hand, among the above-mentioned extracts, the extracts of radish, glaze, 茯神, kuzuhana and soki are preferably included in the form of powder, and are sarcophagus, sobana, senna leaf, rosewood incense. , Grasses, swamps, intruders, flaxseed, and cucumber extracts are preferably included in the form of extracts, and the extract of karo nin is in the form of oil. In addition, the extract of hemp seed is included in the form of a thin liquid.

The composition for improving hair and scalp conditions further comprises a suitable carrier, excipient, diluent and the like according to a method usually used for each field, and is used as a pharmaceutical composition, functional food composition, or hair composition. Applicable.
When provided as a pharmaceutical composition, the composition is administered orally or parenterally by conventional methods. For example, when administered orally, dosage forms such as powders, granules, tablets, suspensions, emulsions, and syrups are used. Used as
The desired dosage is a content suitable for the subject of administration and / or treatment or prevention of the disease, and this includes the age, sex, general health status and weight of the subject of administration, the type and severity of the disease, the type of dosage form, It can be adjusted by various factors including the type and content of other ingredients contained in the composition, the secretion rate of the composition, the route of administration and the duration, and can be appropriately selected by those skilled in the art. The administration subject is a mammal including a human.

When the composition is provided in the form of a hair composition, preferably the hair and scalp condition improving composition is 0.0001-99.9% by weight, based on the total weight of the hair composition, More desirably, the content is 0.1 to 50% by weight. Desirably, the composition may be provided in a dosage form selected from the group consisting of hair toner, hair lotion, hair cream, hair spray, hair mousse, hair gel, hair soap, hair shampoo, hair rinse, hair pack, and hair treatment. .
As another desirable specific example of the present invention, the hair and scalp including the step of administering one or more extracts among the 16 kinds of medicines excellent in 5α reductase inhibitory activity to an individual having hair loss. A state improvement method is provided.

The step of “administering” comprises oral or parenteral administration, and at the time of parenteral administration, external use for skin, subcutaneous injection, transdermal administration, topical administration, etc. can be selected, but this is not limited thereto. is not. Desirably, it is used for external use on the skin, and a method of applying to the skin can be used.
For topical administration, it is administered using a semisolid formulation, such as an ointment, cream or gel, and for transdermal administration, not only a matrix or reservoir patch, but also a semisolid product (aqueous) Alcoholic gels and the like) are also used and are not limited thereto.

According to still another preferred embodiment of the present invention, a method for producing the hair and scalp condition improving composition is provided.
Preferably, the manufacturing method is preferably radish, glaze, 茯神, stone 韋, sobana, senna leaf, rosewood incense, grass, swamp, mulberry, flaxseed, kuzuhana, kyoou. A step of extracting one or more selected from the group consisting of karo-nin (karoujin), hemp and sugi with water, ethanol, or a mixed solvent thereof, and an extract obtained through the extraction step And filtration of the filtrate obtained through the filtration step under reduced pressure.

In order to further increase the extraction efficiency, each of the chemicals is desirably subjected to a step of pulverization before the extraction stage. In particular, among the chemicals, those having a form such as fruit or seed are, for example, scissors. The tool can be used after being cut and crushed. The pulverization method is not particularly limited, and for example, various tools such as a mixer machine can be used.
Preferably, the extraction step is performed by a method of extracting each chemical separately or by mixing all the chemicals and extracting them in a mixture state. The solvents may be the same or different from each other.

Preferably, the extraction step is performed by leaching after mixing each drug substance or a mixture thereof with an extraction solvent.
The leaching is desirably performed within a temperature range of 30 to 40 ° C., more desirably at a temperature of 33 to 38 ° C., desirably 1 to 3 days, and more desirably 45 to 50 hours.
The extraction solvent is not particularly limited, but is preferably extracted using water, ethanol, or a mixed solvent thereof, more preferably ethanol, most preferably 60 to 80% (v / v). Of ethanol can be used.
In addition, preferably, the extraction solvent can be used in an amount of 400 to 800 mL per 100 g of the chemical.

  The vacuum filtration step is not particularly limited, and a method widely known to those skilled in the art can be used. The filtrate obtained through the filtration step may be further subjected to a concentration step under reduced pressure. The vacuum concentration step is not particularly limited, and is performed using a method widely known to those skilled in the art, and may optionally include a step of freeze-drying after the step.

  Hereinafter, the present invention will be described in detail by way of examples. However, the following examples illustrate the present invention, and the present invention is not limited to the following examples.

Example 1. Manufacture of extracts Sone, glaze, 茯神, 韋韋, sobana, senna leaf, rosewood incense, herbaceous fruit, swamp, sardine, flaxseed, kuzuhana, kyouou, karonin (Karoujin), hemp seed and Sugi were prepared and crushed. The fruits and seeds were cut with scissors and then crushed.
In a 1000 mL bottle (Duran), 100 g of the pulverized drug substance and 600 mL of 70% (v / v) ethanol (EtOH) were added and mixed, and then leached for 48 hours at 35 ° C. in a constant temperature water bath.
The obtained leachate was filtered under reduced pressure using filter paper (Watman No. 21 filter), and then the collected filtrate was concentrated with a vacuum concentrator to obtain herbal extracts as shown in Table 1 below (herbal medicine) Recovered in the form of extract, powder, thin liquid). The manufactured extract was collected in a 50 mL tube, sealed with Parafilm, and stored refrigerated.

Experimental Example 1 After quantitative reaction of testosterone and DHT using GC-MS , chromatogram for quantitative analysis of testosterone and dihydrotestosterone (DHT) in the extracted liver microsome fraction (liver microsomal fraction) 1 to FIG. 4.

Experimental Example 2.5 Evaluation and Measurement of Inhibitory Efficacy of α-Reductase In order to evaluate the inhibitory efficacy of 5α-reductase of the extract obtained through Example 1, first, as a control drug, finasteride (Merck) was used. Used to establish the extraction conditions for microsomal fractions.
Specifically, the finasteride is fractionated into a homogenizer, a tissue homogenizer kit, and a tissue lyzer to obtain fractions, and comparative experiments are performed on the fractions to obtain the results shown in Table 2 below. It was.

As shown in Table 2 above, the efficacy of 5α reductase could be confirmed under any of the three conditions for extraction of the microsomal fraction. However, when TissueLizer was used, the efficacy of 5α reductase was relative. It was found that the activity of 5α reductase was suppressed.

  The fraction obtained with the homogenizer was repeatedly tested twice, and the reproducibility for the evaluation of the inhibitory effect of 5α reductase was confirmed as shown in Table 3 below.

Experimental Example 3. Evaluation of inhibitory efficacy of 5α reductase of natural extract In order to evaluate the inhibitory efficacy of 5α reductase of the natural extract obtained through Example 1, each natural extract and testosterone were mixed with DMSO and methanol ( MeOH) and used.
First, in order to investigate the influence on two organic solvents, a 100 μg / mL testosterone solution was diluted with DMSO and methanol (MeOH) at a concentration of 10 μg / mL, respectively, and a comparative experiment was conducted. The results are shown in Table 4 below. expressed.

As shown in Table 4 above, the efficacy of 5α reductase was confirmed in both of the two solvents diluted with testosterone, and there was no influence by the organic solvent in view of the similar result values. I was able to confirm.

  Using the constructed method for analyzing the efficacy of 5α reductase, 16 natural extracts obtained in Example 1 and a control group were extracted by the same method as in Example 1 as a control group. Using the extract, the red bean extract, and the acid vinegar extract, the inhibitory effect of 5α reductase was repeated twice, and the results are shown in Tables 5-1 and 5-2 below.

  As shown in Table 5-1 and Table 5-2, the extract of 16 kinds of medicines obtained by Example 1 of the present invention does not show any efficacy of 5α reductase, and inhibits 5α reductase. It was confirmed that the efficacy was excellent. On the other hand, it was confirmed that the control group, longan meat extract, red bean extract, and acid soy sauce extract, had no inhibitory effect on 5α reductase regardless of the concentration used. In particular, it was found that all of the 16 natural extracts of the present invention are excellent in the inhibitory effect of 5α reductase, as is the case with bitterness which is a known positive control group (positive control).

Experimental Example 4 Measurement of mouse hair growth promoting effect using the composition of the present invention In order to examine the effect of the composition for preventing hair loss and promoting hair growth according to the present invention, the effect of promoting hair growth of this composition using C57BL / 6N mice was examined. confirmed. The composition for preventing hair loss and promoting hair growth used a hemp extract and a soy extract. After completely removing the hair of 7-week-old mice C57BL / 6N mice entering the second stage of catagen, 150 μL of the composition of the present invention and control substance once per day for 10 mice. It was 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 in which the degree of hair growth over time is comparatively analyzed through visual observation.

In Table 6, “−” means that the hair is hardly grown, and “+” means that the hair grows with time, and the larger the number of +, the more the hair is. It has grown. It can be seen that hair grows with hemp extract and Soki extract, which means that the composition according to the invention promotes hair growth.

Experimental Example 5. Measurement of hair growth area In order to measure the ratio of the hair growth area to the hair removal area of the hair growth measurement photograph obtained through Experimental Example 4, i-Solution Lite, an image analysis program, was used. First, after measuring the total area of hair removal and measuring the area of hair growth, the hair growth ratio was measured as a percentage (%) with respect to the total area. Table 7 below shows the hair growth ratio with respect to the hair removal area over time.

In the order of the positive control group (3% minoxidil) and HD-23 (seed extract), the hair growth rate appears higher, but in the case of HD-124 (Sugi extract), significant hair growth occurs after 5 weeks. An increase in rate could be confirmed.

Claims (9)

  Sone, glaze, god of god, stone wall, sobana, senna leaf, rosewood incense, grass, swamp, incense, flaxseed, kuzuhana, kyouou, karonin ), A composition for improving hair and scalp conditions, comprising, as an active ingredient, one or more extracts selected from the group consisting of hemp and sugi.   The composition according to claim 1, wherein the composition comprises a root extract, a glaze extract, a shrine extract, a sarcophagus extract, a hemp extract and a sugi extract.   The composition according to claim 1, wherein the composition is for preventing or treating hair loss.   The composition according to claim 1, wherein the composition is for reducing sebum secretion, preventing scalp or preventing scalp inflammation.   A composition for hair comprising the composition according to any one of claims 1 to 4.   The hair composition is in at least one dosage form selected from the group consisting of hair toner, hair lotion, hair cream, hair spray, hair mousse, hair gel, hair soap, hair shampoo, hair rinse, hair pack, and hair treatment. 6. A composition according to claim 5 provided. Sone, glaze, god of god, stone wall, sobana, senna leaf, rosewood incense, grass, swamp, incense, flaxseed, kuzuhana, kyouou, karonin ), Extracting one or more selected from the group consisting of hemp and sugi with water, ethanol, or a mixed solvent thereof;
Filtering the extract obtained through the extraction step under reduced pressure;
Concentrating the filtrate obtained through the filtration step under reduced pressure;
The manufacturing method of the composition for hair and scalp condition improvement in any one of Claim 1 to 4 containing this.   The method according to claim 7, wherein in the extraction step, the root, the glaze, the god of God, the stone wall, the hemp seed and the sugi are extracted individually or mixed with ethanol in the form of a mixture.   The said extraction is a manufacturing method of Claim 8 performed at the temperature of 30-40 degreeC for 1-3 days.