Chinese herbal active ingredient @ cyst complex with hair growth effect, its preparation method and its use
The Chinese herbal active substance@cyst complex addresses the solubility and absorption issues of existing herbal ingredients by forming a double-layered membrane structure for sustained release, enhancing hair nourishment and growth efficacy.
Patent Information
- Application Number
- JP2024536217
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2022-02-23
- Filing Date
- 2023-02-16
- Publication Date
- 2024-12-10
- Estimated Expiration
- 2043-02-16
AI Technical Summary
Existing Chinese herbal active ingredients, especially fat-soluble ones, have solubilized molecular states that hinder effective action on the scalp and hair follicles, leading to poor absorption and lack of sustained release, resulting in inadequate hair care effects.
A Chinese herbal active substance@cyst complex is developed, featuring a double-layered membrane structure that simultaneously solubilizes hydrophilic and hydrophobic ingredients, stabilizes the scalp and hair follicles, and provides a microecological environment for sustained release, enhancing absorption and efficacy.
The cyst complex improves solubility, dispersibility, and stability of active ingredients, promoting hair nourishment and growth by creating a stable microenvironment for sustained release and optimal utilization of medicinal properties.
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Figure 2024545680000001_ABST
Abstract
Description
[Technical field]
[0001] The present invention relates to a Chinese herbal actives@cyst complex having hair-growing effects and its preparation, which belongs to the field of cosmetics technology. [Background technology]
[0002] Hair is one of the components of the human body, and changes in hair are closely related to physiological and pathological changes in the human body. Modern people have a fast life rhythm, long working hours, great mental stress, and irregular work and breathing patterns, so hair loss has become a concern for more and more modern people, and the problem is becoming more prevalent at younger ages. In recent years, the number of people losing their hair in China has skyrocketed, with one in six people losing their hair. According to statistics, the hair loss rate in the world has reached 32.13%, and the number of people suffering from hair loss is increasing year by year. The demand for hair-growth cosmetics that help hair growth and reduce hair loss and breakage is becoming increasingly strong, and the demand for efficacy is also increasing. When hair is oily, dry, or falls out, it is not just a problem with the hair. If you trace it back to the source, it is actually a problem with the scalp and hair follicles. The scalp and hair are related to soil and plants, and good soil produces good plants, and in the same way, a good scalp can have good hair. Therefore, scalp care is the key to solving the hair loss problem. At present, there are many types of products to treat hair loss, among which Western medicines are mostly hormones, and long-term use may bring certain side effects to the body, and it is easy to stop taking the medicine and recover. Since 2015, as the national policy has deepened support for Chinese medicine and Chinese medicine, the number of Chinese medicine-based cosmetics has been increasing year by year. In fact, the history of Chinese medicine doctors treating hair diseases is long, and many medical classics have described good ways to nourish hair, which have been passed down to the present. Chinese herbal extracts contain a variety of natural ingredients, such as flavonoids, tannins, oxalic acid, ferric acid, saponin, amino acids, and trace elements, and have the functions of vasodilating, anti-inflammatory, antibacterial, antioxidant, and immunoregulating, which can effectively treat hair loss and promote hair growth. However, the active ingredients in Chinese herbal extracts are many and complex, and their physicochemical properties are also very different, making it difficult to dissolve them in the same solvent at the same time, which affects the dispersion and absorption of the active ingredients and inhibits the exertion of their medicinal effects. The cyst is a closed bilayer with a core-shell structure formed by the gathering of amphiphilic molecules, which can contain various substances and can be dissolved in different areas according to the polarity of the substances. Hydrophilic substances are contained in the hydrophilic microdomain, i.e., the water core, and hydrophobic substances are solubilized in the hydrocarbon chain middle layer of the amphiphilic molecules. Therefore, the hydrophilic and hydrophobic active ingredients in the Chinese herbal extract can be simultaneously dissolved and loaded into the cyst, and the solubility and dispersibility of the poorly soluble active substances can be increased, and the selective permeability and sustained release performance of the cyst bilayer structure can make the active substances stable and sustained on the scalp. Under the support of the cyst system, the active substances can generate a microecological environment on the scalp surface and around the hair follicles, reduce the damage to the hair follicles caused by iontophoresis, and effectively draw out the vitality of the hair follicles from the root, thereby obtaining the optimal use of medicinal properties and achieving the effects of hair nourishment and hair growth.
[0003] In Patent Document 1, in order to improve the bioavailability or absorption of poorly lipophilic drugs, the solubility of the active ingredient is increased by combining the herbal active ingredient with phosphatidylcholine. However, the liposome formed by phosphatidylcholine has poor permeability, which is unfavorable for the release of the active ingredient. In addition, the herbal medicine ingredients disclosed in this patent document are mainly for internal use, and the solubility and bioabsorption rate of the herbal extracts when used externally cannot be determined.
[0004] Patent Document 2 discloses a hair care composition for preventing hair loss and hair growth, and more specifically, relates to a hair care composition for preventing hair loss that promotes adhesion to the scalp and hair by mixed cysts containing cationic / anionic surfactants. However, when cationic / anionic surfactants are mixed, precipitation is likely to occur due to electrostatic interactions, and the cyst structure is formed only in a relatively narrow range of blending. In addition, it is easily affected by strong electrolytes such as acids, alkalis, and salts, as well as charged herbal extracts, which destroy the cyst structure and cause precipitation. [Prior art documents] [Patent documents]
[0005] [Patent Document 1] Indian patent document IN1764MUM2014A [Patent Document 2] Korean patent document KR1020090059445A Summary of the Invention
[0006] The existing herbal active ingredients, especially the fat-soluble active ingredients, are difficult to solubilize in the molecular state and enter the product to act on the scalp and hair follicles, and cannot exert optimal efficacy, so the hair loss and hair growth prevention effect is greatly reduced. In addition, most of the active ingredients in the existing products only have a high concentration effect on the scalp at the moment of use, and the slow and sustained release environment of the active ingredients is lacking, and a constant dynamic effective concentration cannot be maintained, so the absorption effect is poor. In response to the shortcomings of the prior art and the defects of the existing products, the present invention provides a herbal active @ cyst complex with safe and effective hair loss prevention and hair growth effects, and a method for preparing the same. The core-shell double-layer membrane structure of the cyst can not only simultaneously solubilize the hydrophilic and hydrophobic active ingredients in the herbal extract, but also form a stable herbal active @ cyst micro-ecological environment around the scalp and hair follicles due to its own selective permeability and sustained release ability, thereby obtaining optimal utilization of the medicinal effects and achieving the effects of hair growth and hair growth.
[0007] The herbal active@cyst complex with hair nourishing and hair growth effects described in the present invention has two characteristics: first, it is a complex formed by the coexistence of the herbal active and the cyst; second, the herbal active@cyst complex has a hair nourishing and hair growth effect.
[0008] One of the objectives of the present invention is to provide a Chinese herbal actives@cyst complex that is coated in and coexists with the cyst, and the complex has a specific core-shell structure, is size-controllable, and has good stability.
[0009] Another object of the present invention is to provide a method for preparing a Chinese herbal active@cyst complex, i.e., simultaneously preparing cysts spontaneously under the induction of Chinese herbal active, which is technically simple, convenient to operate, and suitable for large-scale production.
[0010] The third object of the present invention is to provide an application of the above-mentioned Chinese herbal actives@cyst complex, which has the effect of nourishing and growing hair and can be applied in the field of cosmetics.
[0011] The technical aspects of the present invention are as follows: A Chinese herbal active @ cyst complex having a hair nourishing and hair growth effect, the complex comprises a Chinese herbal active and a cyst, the Chinese herbal active is coated in the cyst; the hydrophilic substance is coated in the hydrophilic microdomain, i.e., the water core, and the hydrophobic substance is dissolved between the two layers of the cyst.
[0012] According to the invention, the particle size of the composite is preferably 80 nm to 5 μm; the majority of the particles are 80 to 900 nm, more preferably 200 to 800 nm, with the minority of the composite particles being 1 to 5 μm in size.
[0013] According to the present invention, the cyst is a bilayer cyst, and the bilayer thickness is preferably 3 to 7 nm. According to the present invention, the content range of the herbal actives in the herbal actives@cyst complex is preferably 30-100g / L.
[0014] According to the present invention, preferably, the cysts are formed from an amphipathic molecular system, and the concentration of the amphipathic molecules ranges from 0.1 to 20 g / L, more preferably from 0.2 to 10 g / L. The present invention refers to the amphipathic molecules as cyst precursors.
[0015] According to the present invention, the said herbal actives are preferably extracted from the following raw materials: What-headed crow, Ink-durren, Shajin, Byakujutsu, Sawagata, Red peony, Blue bark, Yellow oak, Huang spirit, Suppressing crow, Chopped blue, Side oak leaf, Senkyu, Tianma, Umei charcoal, Jidako, Red axle grass, Agiao, More preferably, the weight ratio of the raw material drug of the Chinese herbal extract is: He Shouwu 5-15 parts, Sumidorian 5-15 parts, Sha Jin 20-50 parts, White Jutsu 20-50 parts, Zegata 5-15 parts, Red Peony 20-50 parts, Blue Peel 5-15 parts, Huangbai 5-15 parts, Huang Jing 20-50 parts, Seizure 20 to 50 parts of crow, 20 to 50 parts of shibori, 20 to 50 parts of lateral oak leaves, 5 to 15 parts of cypress, 5 to 15 parts of tenma, 5 to 15 parts of charcoal, 5 to 15 parts of japonicum, 20 to 50 parts of red axle grass, 20 to 50 parts of agu, More preferred are 10 parts of Polygonum multiflorum, 10 parts of Lotus Root, 30 parts of Shashen, 30 parts of White Scutellaria, 12 parts of Swertia Root, 30 parts of Red Peony, 12 parts of Green Skin, 15 parts of Phellodendron Bark, 30 parts of Yellow Jelly, 30 parts of Cyperus Root, 30 parts of Celastrus Root, 12 parts of Cnidium Root, 12 parts of Tianhe Hemp, 10 parts of Black Plum Charcoal, 10 parts of Earthworm Fruit, 25 parts of Red Chamomile, and 35 parts of Euglena.
[0016] According to the present invention, preferably, the cyst precursor can be selected from one or a combination of mono fatty acid glycerides, mono alkyl phosphate esters and their salts, 2-hydroxy fatty acids and their salts, nicotinic acid and its derivatives, and triblock copolymers.
[0017] According to the present invention, the mono fatty acid glyceride is preferably a linear mono fatty acid glyceride, more preferably a C8 to C 18 Straight chain mono-fatty acid glycerides of any chain length are preferred, more preferably glycerol octanoate, glycerol decanoate, glycerol laurate, glycerol myristate, glycerol pentadecanoate, and glycerol palmitate. According to the present invention, the monoalkyl phosphate ester and its salt are preferably linear alkyl phosphate ester and its salt, more preferably C8 to C 16 Linear chain monoalkyl phosphate esters or salts thereof, more preferably octyl phosphate and its sodium salt, potassium salt, magnesium salt or zinc salt, decyl phosphate and its sodium salt, potassium salt, magnesium salt or zinc salt, lauryl phosphate and its sodium salt, potassium salt, magnesium salt or zinc salt, palmisyl phosphate and its sodium salt, potassium salt, magnesium salt or zinc salt.
[0018] According to the present invention, the 2-hydroxy fatty acid and its salt are preferably 2-hydroxy straight chain fatty acids and their salts, more preferably C8-C 16 and 2-hydroxy straight-chain fatty acids of any of the above chain lengths and their salts, more preferably 2-hydroxyoctanoic acid and its sodium salt, potassium salt, magnesium salt or zinc salt, 2-hydroxydecanoic acid and its sodium salt, potassium salt, magnesium salt or zinc salt, 2-hydroxylauric acid and its sodium salt, potassium salt, magnesium salt or zinc salt, and 2-hydroxycarminic acid and its sodium salt, potassium salt, magnesium salt or zinc salt.
[0019] According to the present invention, nicotinic acid and its derivatives are preferably nicotinic acid, benzyl nicotinate, and tocopherol nicotinate.
[0020] According to the present invention, the chemical formula of the triblock copolymer is preferably PEO x - PPO y - PEO x , 13≦x≦133, 29≦y≦65, more preferably PEO 77 - PPO 29 - PEO 77 , P.E.O. 13 - PPO 30 - PEO 13 , P.E.O. 24 - PPO 35 - PEO 24 , P.E.O. 133 - PPO 50 - PEO 133 , P.E.O. 19 - PPO 30 - PEO 19 , P.E.O. 100 - PPO 65 - PEO 100 , P.E.O. 26 - PPO 40 - PEO 26 It is.
[0021] The herbal actives@cyst complex of the present invention is a homogeneous and stable system, which can be stored stably at room temperature for more than one year.
[0022] The method for preparing the Chinese herbal active@cyst complex according to the present invention comprises the following steps: The raw drug is extracted by adding mixed solvent, the extract is collected, and the cyst precursor is added, mixed, alcohol precipitated, centrifuged, filtered and concentrated to obtain the Chinese herbal actives@cyst compound. According to the present invention, the mixed solvent is preferably an ethanol-water mixed solution. According to the present invention, the volume percentage concentration of ethanol in the ethanol-water mixed solution is preferably 40% to 80%, more preferably 55% to 70%.
[0023] According to the present invention, preferably, the number of extractions is 1 to 5 times, the time for each extraction is 1 to 5 hours, and the extraction temperature is 55°C to 80°C. Most preferably, the number of extractions is 4, each extraction time is 4 hours, and the extraction temperature is 70°C.
[0024] According to the present invention, the Chinese herbal actives@cyst complex is prepared simultaneously with spontaneous cyst formation under the induction of Chinese herbal actives.
[0025] According to the present invention, the application of said Chinese herbal actives@cyst complex is in the field of cosmetics. The technical features and beneficial effects of the present invention are as follows: The existing herbal active ingredients, especially the fat-soluble active ingredients, are difficult to solubilize in the molecular state and enter the product to act on the scalp and hair follicles, and cannot exert optimal efficacy, so the hair loss and hair growth prevention effect is greatly reduced. In addition, most of the active ingredients in the existing products only have a high concentration effect on the scalp at the moment of use, and the slow and sustained release environment of the active ingredients is lacking, and a constant dynamic effective concentration cannot be maintained, so the absorption effect is poor. In response to the shortcomings of the prior art and the defects of the existing products, the present invention provides a herbal active @ cyst complex with safe and effective hair loss prevention and hair growth effects, and a method for preparing the same. The core-shell double-layer membrane structure of the cyst can not only simultaneously solubilize the hydrophilic and hydrophobic active ingredients in the herbal extract, but also form a stable herbal active @ cyst micro-ecological environment around the scalp and hair follicles due to its own selective permeability and sustained release ability, thereby obtaining optimal utilization of the medicinal effects and achieving the effects of hair growth and hair growth. 1. The present invention provides a Chinese herbal active substance@cyst complex, in which the active substance is coated in the cyst, enhancing the solubility and dispersibility of the poorly soluble active substance. The hydrophilic substance is coated in the hydrophilic microdomain, i.e., the water core, and the hydrophobic substance is dissolved in the bilayer membrane of the cyst. 2. The herbal actives @ cyst microenvironment technology of the present invention can release the actives stably and sustainably, and improve the stability of the active ingredient extracts, thereby achieving better hair growth effects. It has important future applications in the fields of drug delivery, controlled release and cosmetics. 3. The dispersion medium of the herbal active ingredient@cyst complex of the present invention is an ethanol-water mixture, which has better penetration and bactericidal ability than solvents such as pure water. 4. The preparation method of the Chinese herbal active ingredient@cyst complex of the present invention is simple, the reaction is mild, and it is suitable for large-scale production. 5. The herbal actives@cyst complex of the present invention is a homogeneous stable system, the content range of the herbal actives is 30-100g / L, the particle size of the complex is preferably nanoscale (200-800nm), and the particle size of the complex in small amounts can reach 1-5μm, and it can be stored stably at room temperature for more than one year. 6. The pH value of the herbal extract in the present invention is 5-6, and the Zeta potential is about -15±5.0mV, so that a nonionic surfactant or anionic surfactant is selected as the cyst precursor to avoid the inactivation or precipitation of the active substances extracted from the herbal extract. In particular, the cyst precursor of nonionic surfactants has good solubility in water or alcohol, is highly stable because it does not exhibit an ionic state, and is not easily affected by acids, alkalis, or strong electrolyte inorganic salts. In addition, it is compatible with other types of surfactants and can be used in combination. 7. The compound of the present invention adopts tincture solvent (ethanol-water mixture), in which short-chain alcohol is a commonly used cyst-destroying agent, so most of the phase cyst system cannot exist stably in tincture solution. The cyst compound of the present invention can be formed spontaneously in tincture solvent, exist stably, and have better transdermal ability, which is also the advantage of the dosage form of the present invention. [Brief description of the drawings]
[0026] [Figure 1] 1 shows the dynamic light scattering particle size distribution map and transmission electron microscope photograph of the Chinese herbal active @ lauric acid glyceride vesicle complex of Example 1. [Diagram 2] 2 shows the dynamic light scattering particle size distribution map and optical microscope photograph of the Chinese herbal active @monosodium dodecyl phosphate vesicle complex of Example 2. [Diagram 3] 1 shows the dynamic light scattering particle size distribution map and transmission electron microscope photograph of the Chinese herbal active@nicotinic acid (0.5 g / L) cyst complex of Example 3. [Figure 4] FIG. 13 is a dynamic light scattering particle size distribution map and transmission electron microscope photograph of the Chinese herbal actives@nicotinic acid (1 g / L) cyst complex of Example 4. [Diagram 5] FIG. 5 is a dynamic light scattering particle size distribution map and a transmission electron microscope photograph of the Chinese herbal active ingredient @ sodium 2-hydroxyoctanoate cyst complex of Example 5. [Figure 6] 1 shows a dynamic light scattering particle size distribution map and a transmission electron microscope photograph of PEO77-PPO29-PEO77 (5 g / L) cysts of the uncoated active material in Example 6. [Figure 7] FIG. 6 shows the dynamic light scattering particle size distribution map and transmission electron microscope photograph of the Chinese herbal active @PEO77-PPO29-PEO77 (5 g / L) cyst composite of Example 6. [Figure 8] Example 7: Dynamic light scattering particle size distribution map and transmission electron microscope photograph of Chinese herbal active @PEO77-PPO29-PEO77 (10 g / L) cyst complex. [Figure 9] FIG. 13 is a dynamic light scattering particle size distribution map and optical microscope photograph of the Chinese herbal active ingredient @PEO13-PPO30-PEO13 cyst composite of Example 8. [Figure 10] Test Example 1: This is a photograph showing the appearance of a mouse hair growth experiment using a Chinese herbal active @ cyst complex. [Figure 11] Test Example 1: Photomicrograph of mouse dorsal hair follicle of Chinese herbal active @cyst complex. [Figure 12] Test Example 1: Fluorescent staining of the herbal active ingredient @ cyst complex on mouse back inflammation factors. [Figure 13] 1 is a transmission electron microscope photograph of a Chinese herbal extract to which no cyst precursors were added in Comparative Example 1. [Figure 14] 1 is a transmission electron microscope photograph of a mixture of lauric acid glyceride and a Chinese herbal extract in which the order of addition was changed from that in Comparative Example 2. [Figure 15] Comparative Example 3: Transmission electron micrograph of a mixture of Chinese herbal active and Tween 80. [Figure 16] Comparative Example 4: Transmission electron microscope photograph of a mixture of Chinese herbal actives and glyceryl stearate. [Figure 17] Comparative Example 5: Transmission electron micrograph of a mixture of Chinese herbal actives and PEO77-PPO29-PEO77 (1 g / L). [Figure 18] Comparative Example 6: Transmission electron micrograph of a mixture of Chinese herbal actives and PEO13-PPO30-PEO13 (25 g / L). DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
[0027] The present invention will be further described below in combination with specific examples, but these examples are for more detailed specific explanation and do not limit the present invention in any way. Unless otherwise illustrated, the reagents, methods, and devices used in the present invention are conventional reagents, methods, and devices in the art.
[0028] Unless otherwise noted, reagents and materials used in the following examples are commercially available. The drugs used in the examples are as follows: What-headed crow, ink-dry lotus, shajin, white jutsu, sawagata, red peony, blue bark, yellow oak, yellow essence, restrained crow, strangulated blue, side oak leaf, senkyu, tianma, crow-bai charcoal, earth worm, red axle grass, agia. The process of extracting the active ingredients is as follows: The raw drug is extracted by adding mixed solvent, the extract is collected, the cyst precursor is added, mixed, alcohol precipitated, centrifuged, filtered and concentrated to obtain the herb actives@cyst complex.
[0029] Example 1 (1) 10g of each number-headed crow, 10g of ink-dry lotus, 30g of shajin, 30g of white jutsu, 12g of sawagata, 30g of red peony, 12g of blue bark, 15g of yellow barb, 30g of yellow spirit, 30 g of cuffed crow g, 30 g of shibori matai indigo, 30 g of cypress leaves, 12 g of cypress, 12 g of tenma, 10 g of charcoal, 10 g of jijiako, 25 g of red axle grass, and 35 g of Agia were mixed and ground into powder. (2) The herbal powder in operation (1) is placed in an extraction tank, and 650mL of tertiary water and 800mL of ethanol are added, soaked for 30 minutes, and then alcohol precipitated, concentrated and extracted to obtain the herbal extract, where the extraction is performed 4 times, the extraction time is 4 hours each time, and the extraction temperature is 70℃. (3) 0.3 g of lauric acid glyceride is added to the herbal extract obtained in step (2), and the mixture is stirred by a vortex, centrifuged, left to stand for 24 hours, filtered, and concentrated to obtain the herbal active ingredient@lauric acid glyceride cyst complex. The dynamic light scattering particle size distribution diagram and transmission electron microscope photograph of the Chinese herbal active ingredient @ lauric acid glyceride cyst complex obtained in this example are shown in Figure 1. As shown in Figure 1, a large number of cysts exist in the product of this example, and the cyst particle size distribution is about 700 nm. In addition, a large number of aggregates with a particle size of about 200 nm were observed in the negative staining transmission electron microscope photograph.
[0030] Example 2 (1) 10g of each number-headed crow, 10g of ink-dry lotus, 30g of shajin, 30g of white jutsu, 12g of sawagata, 30g of red peony, 12g of blue bark, 15g of yellow barb, 30g of yellow spirit, 30 g of cuffed crow g, 30 g of shibori matai indigo, 30 g of cypress leaves, 12 g of cypress, 12 g of tenma, 10 g of charcoal, 10 g of jijiako, 25 g of red axle grass, and 35 g of Agia were mixed and ground into powder. (2) The herbal powder in operation (1) is placed in an extraction tank, and 650mL of tertiary water and 800mL of ethanol are added, soaked for 30 minutes, and then alcohol precipitated, concentrated and extracted to obtain the herbal extract, where the extraction is performed 4 times, the extraction time is 4 hours each time, and the extraction temperature is 70℃. (3) 1.5 g of monosodium dodecyl phosphate is added to the herbal extract obtained in step (2), and the mixture is stirred by a vortex, centrifuged, left to stand for 24 hours, filtered, and concentrated to obtain the herbal active ingredient@monosodium dodecyl phosphate cyst complex. The dynamic light scattering particle size distribution diagram and transmission electron microscope photograph of the Chinese herbal actives@monosodium dodecyl phosphate cyst complex obtained in this example are shown in Figure 2. As can be seen from Figure 2, a large amount of nano-scale cysts and micron-scale cysts coexist in the product of this example, with particle size distributions between 10-100 nm and 1-5 μm, respectively.
[0031] Example 3 (1) 10g of each number-headed crow, 10g of ink-dry lotus, 30g of shajin, 30g of white jutsu, 12g of sawagata, 30g of red peony, 12g of blue bark, 15g of yellow barb, 30g of yellow spirit, 30 g of cuffed crow g, 30 g of shibori matai indigo, 30 g of cypress leaves, 12 g of cypress, 12 g of tenma, 10 g of charcoal, 10 g of jijiako, 25 g of red axle grass, and 35 g of Agia were mixed and ground into powder. (2) The herbal powder in operation (1) is placed in an extraction tank, and 650mL of tertiary water and 800mL of ethanol are added, soaked for 30 minutes, and then alcohol precipitated, concentrated and extracted to obtain the herbal extract, where the extraction is performed 4 times, the extraction time is 4 hours each time, and the extraction temperature is 70℃. (3) 0.5 g of nicotinic acid can be added to the herbal extract obtained in step (2), followed by vortexing, centrifugation, standing for 24 hours, filtering, and concentrating to obtain the herbal actives@nicotinic acid (0.5 g / L) cyst complex. The dynamic light scattering particle size distribution diagram and transmission electron microscope photograph of the Chinese herbal actives@nicotinic acid (0.5 g / L) cyst complex obtained in this example are shown in Figure 3. From Figure 3, it can be seen that there are a large number of cysts with a particle size of about 200 nm in the product of this example, and they are uniformly dispersed.
[0032] Example 4 (1) 10g of each number-headed crow, 10g of ink-dry lotus, 30g of shajin, 30g of white jutsu, 12g of sawagata, 30g of red peony, 12g of blue bark, 15g of yellow barb, 30g of yellow spirit, 30 g of cuffed crow g, 30 g of shibori matai indigo, 30 g of cypress leaves, 12 g of cypress, 12 g of tenma, 10 g of charcoal, 10 g of jijiako, 25 g of red axle grass, and 35 g of Agia were mixed and ground into powder. (2) The herbal powder in operation (1) is placed in an extraction tank, and 650mL of tertiary water and 800mL of ethanol are added, soaked for 30 minutes, and then alcohol precipitated, concentrated and extracted to obtain the herbal extract, where the extraction is performed 4 times, the extraction time is 4 hours each time, and the extraction temperature is 70℃. (3) 1 g of nicotinic acid can be added to the herbal extract obtained in step (2), followed by vortexing, centrifugation, standing for 24 hours, filtering, and concentrating to obtain the herbal actives@nicotinic acid (1 g / L) cyst complex. The dynamic light scattering particle size distribution diagram and transmission electron microscope photograph of the Chinese herbal active @ nicotinic acid (1 g / L) cyst complex obtained in this example are shown in Figure 4. From Figure 4, it can be seen that a large amount of cysts with a particle size of about 200 to 400 nm are present in the product of this example and are uniformly dispersed.
[0033] Example 5 (1) 10g of each number-headed crow, 10g of ink-dry lotus, 30g of shajin, 30g of white jutsu, 12g of sawagata, 30g of red peony, 12g of blue bark, 15g of yellow barb, 30g of yellow spirit, 30 g of cuffed crow g, 30 g of shibori matai indigo, 30 g of cypress leaves, 12 g of cypress, 12 g of tenma, 10 g of charcoal, 10 g of jijiako, 25 g of red axle grass, and 35 g of Agia were mixed and ground into powder. (2) The herbal powder in operation (1) is placed in an extraction tank, and 650mL of tertiary water and 800mL of ethanol are added, soaked for 30 minutes, and then alcohol precipitated, concentrated and extracted to obtain the herbal extract, where the extraction is performed 4 times, the extraction time is 4 hours each time, and the extraction temperature is 70℃. (3) 3.6 g of sodium 2-hydroxyoctanoate is added to the herbal extract obtained in step (2), and the mixture is stirred by a vortex, centrifuged, left to stand for 24 hours, filtered, and concentrated to obtain the herbal active ingredient @ sodium 2-hydroxyoctanoate cyst complex. The dynamic light scattering particle size distribution diagram and transmission electron microscope photograph of the Chinese herbal active ingredient @ sodium 2-hydroxyoctanoate cyst complex obtained in this example are shown in Figure 5. From Figure 5, it can be seen that there are a large number of cysts in the product of this example, the cyst particle size distribution is about 600 nm, and a large number of aggregates with a particle size of about 200 nm can also be observed in the negative staining transmission electron microscope photograph.
[0034] Example 6 (1) 10g of each number-headed crow, 10g of ink-dry lotus, 30g of shajin, 30g of white jutsu, 12g of sawagata, 30g of red peony, 12g of blue bark, 15g of yellow barb, 30g of yellow spirit, 30 g of cuffed crow g, 30 g of shibori matai indigo, 30 g of cypress leaves, 12 g of cypress, 12 g of tenma, 10 g of charcoal, 10 g of jijiako, 25 g of red axle grass, and 35 g of Agia were mixed and ground into powder. (2) The herbal powder in operation (1) is placed in an extraction tank, and 650mL of tertiary water and 800mL of ethanol are added, soaked for 30 minutes, and then alcohol precipitated, concentrated and extracted to obtain the herbal extract, where the extraction is performed 4 times, the extraction time is 4 hours each time, and the extraction temperature is 70℃. (3) The herbal extract obtained in step (2) was treated with PEO 77 -PPO29 -PEO 77 Add 5 g of the herbal extract, vortex, centrifuge, leave for 24 hours, filter, and concentrate to obtain the herbal extract @PEO. 77 -PPO 29 -PEO 77 (5 g / L) cyst complex can be obtained. PEO without coating of herbal actives 77 - PPO 29 - PEO 77 (5g / L) cyst and herbal actives obtained in this example @PEO 77 - PPO 29 - PEO 77 The dynamic light scattering particle size distribution diagram and transmission electron micrograph of the (5g / L) cyst composite are shown in Figure 6 and Figure 7, respectively. The cysts before uncoated active were uniformly dispersed, with particle sizes ranging from 200 to 400 nm (Figure 6). Meanwhile, the particle sizes of the herbal active@cysts after active coating increased significantly, to about 700 to 800 nm, and the membrane walls became thicker (Figure 7).
[0035] Example 7 (1) 10g of each number-headed crow, 10g of ink-dry lotus, 30g of shajin, 30g of white jutsu, 12g of sawagata, 30g of red peony, 12g of blue bark, 15g of yellow barb, 30g of yellow spirit, 30 g of cuffed crow g, 30 g of shibori matai indigo, 30 g of cypress leaves, 12 g of cypress, 12 g of tenma, 10 g of charcoal, 10 g of jijiako, 25 g of red axle grass, and 35 g of Agia were mixed and ground into powder. (2) The herbal powder in operation (1) is placed in an extraction tank, and 650mL of tertiary water and 800mL of ethanol are added, soaked for 30 minutes, and then alcohol precipitated, concentrated and extracted to obtain the herbal extract, where the extraction is performed 4 times, the extraction time is 4 hours each time, and the extraction temperature is 70℃. (3) The herbal extract obtained in step (2) was treated with PEO 77 -PPO 29 -PEO 77 Add 10 g of the herbal extract, vortex, centrifuge, leave for 24 hours, filter, and concentrate to obtain the herbal extract @PEO. 77 -PPO 29 -PEO 77 (10 g / L) cyst complex can be obtained. The herbal active ingredient @PEO obtained in this example 77 -PPO 29 -PEO 77 The dynamic light scattering particle size distribution diagram and transmission electron microscope photograph of the cyst complex (10 g / L) are shown in Figure 8. From Figure 8, it can be seen that a large number of cysts are present in the product of this example, the cyst particle size is about 200 nm, and they are uniformly dispersed.
[0036] Example 8 (1) 10g of each number-headed crow, 10g of ink-dry lotus, 30g of shajin, 30g of white jutsu, 12g of sawagata, 30g of red peony, 12g of blue bark, 15g of yellow barb, 30g of yellow spirit, 30 g of cuffed crow g, 30 g of shibori matai indigo, 30 g of cypress leaves, 12 g of cypress, 12 g of tenma, 10 g of charcoal, 10 g of jijiako, 25 g of red axle grass, and 35 g of Agia were mixed and ground into powder. (2) The herbal powder in operation (1) is placed in an extraction tank, and 650mL of tertiary water and 800mL of ethanol are added, soaked for 30 minutes, and then alcohol precipitated, concentrated and extracted to obtain the herbal extract, where the extraction is performed 4 times, the extraction time is 4 hours each time, and the extraction temperature is 70℃. (3) The herbal extract obtained in step (2) was treated with PEO 13 -PPO 30 -PEO 13 Add 5 g of the herbal extract, vortex, centrifuge, leave for 24 hours, filter, and concentrate to obtain the herbal extract @PEO. 13 -PPO 30 -PEO 13 Cystic complexes can be obtained. Herbal actives obtained in this example @PEO 13 -PPO 30 -PEO 13 The dynamic light scattering particle size distribution diagram and optical microscope photograph of the cyst complex are shown in Figure 9. From Figure 9, it can be seen that there are a large number of micron-class cysts in the product of this example, and the particle size distribution is wide, about 2 to 4 μm.
[0037] Example 9 (1) 15g of Hekubi, 5g of Bokudouren, 20g of Shajin, 30g of White Jutsu, 12g of Sawagata, 40g of Red Peony, 12g of Blue Peony, 15g of Huangbai, 30g of Huangjing, and 35g of Seibu Karasu , 25 g of shibori indigo, 30 g of cypress leaves, 12 g of cypress, 12 g of tenma, 10 g of charcoal, 10 g of jijiako, 25 g of red axle grass, and 35 g of Agia were mixed and ground into powder. (2) The herbal powder in operation (1) is placed in an extraction tank, and 650mL of tertiary water and 800mL of ethanol are added, soaked for 30 minutes, and then alcohol precipitated, concentrated and extracted to obtain the herbal extract, where the extraction is performed 4 times, the extraction time is 4 hours each time, and the extraction temperature is 70℃. (3) 0.3 g of lauric acid glyceride is added to the herbal extract obtained in step (2), and the mixture is stirred by a vortex, centrifuged, left to stand for 24 hours, filtered, and concentrated to obtain the herbal active ingredient @ lauric acid glyceride cyst complex II.
[0038] Example 10 (1) 5g of Hekuhuu Karasu, 5g of Sumidoren, 35g of Shajin, 30g of White Jutsu, 12g of Sawagata, 35g of Red Peony, 12g of Blue Peony, 10g of Huangbai, 40g of Huangjing, 30g of Seihuu Karasu , 30g of shibori indigo, 30g of cypress leaves, 12g of cypress, 12g of turquoise, 5g of charcoal, 15g of japonicum, 25g of red axle grass, and 35g of silver were mixed and ground into powder. (2) The herbal powder in operation (1) is placed in an extraction tank, and 650mL of tertiary water and 800mL of ethanol are added, soaked for 30 minutes, and then alcohol precipitated, concentrated and extracted to obtain the herbal extract, where the extraction is performed 4 times, the extraction time is 4 hours each time, and the extraction temperature is 70℃. (3) 1.5 g of monosodium dodecyl phosphate is added to the herbal extract obtained in step (2), and the mixture is stirred by a vortex, centrifuged, left to stand for 24 hours, filtered, and concentrated to obtain the herbal active ingredient @ monosodium dodecyl phosphate cyst complex II.
[0039] Example 11 (1) 10g of each number-headed crow, 20g of ink-dry lotus, 30g of shajin, 30g of white jutsu, 12g of sawagata, 20g of red peony, 12g of blue bark, 15g of yellow barb, 20g of yellow spirit, 35 g of cuffed crow g, 30 g of shibori indigo, 35 g of cypress leaves, 12 g of cypress, 10 g of tenma, 15 g of charcoal, 12 g of jijiako, 20 g of red axle grass, and 35 g of Agia were mixed and ground into powder. (2) The herbal powder in operation (1) is placed in an extraction tank, and 650mL of tertiary water and 800mL of ethanol are added, soaked for 30 minutes, and then alcohol precipitated, concentrated and extracted to obtain the herbal extract, where the extraction is performed 4 times, the extraction time is 4 hours each time, and the extraction temperature is 70℃. (3) The herbal extract obtained in step (2) was treated with PEO 77 -PPO 29 -PEO 77 Add 10 g of the herbal extract, vortex, centrifuge, leave for 24 hours, filter, and concentrate to obtain the herbal extract @PEO. 77 -PPO 29 -PEO 77 (10 g / L) cyst complex II can be obtained.
[0040] Example 12 (1) 10g of each number-headed crow, 10g of ink-dry lotus, 30g of shajin, 30g of white jutsu, 12g of sawagata, 30g of red peony, 12g of blue bark, 15g of yellow barb, 30g of yellow spirit, 30 g of cuffed crow g, 30 g of shibori matai indigo, 30 g of cypress leaves, 12 g of cypress, 12 g of tenma, 10 g of charcoal, 10 g of jijiako, 25 g of red axle grass, and 35 g of Agia were mixed and ground into powder. (2) The Chinese herbal powder in operation (1) is placed in an extraction tank, and 650mL of tertiary water and 800mL of ethanol are added, soaked for 30 minutes, and then alcohol precipitated, concentrated and extracted to obtain the Chinese herbal extract, where the extraction is performed 4 times, the extraction time is 2 hours each time, and the extraction temperature is 80℃. (3) 0.3 g of lauric acid glyceride is added to the herbal extract obtained in step (2), and the mixture is stirred by a vortex, centrifuged, left to stand for 24 hours, filtered, and concentrated to obtain the herbal active ingredient @ lauric acid glyceride cyst complex III.
[0041] Example 13 (1) 10g of each number-headed crow, 10g of ink-dry lotus, 30g of shajin, 30g of white jutsu, 12g of sawagata, 30g of red peony, 12g of blue bark, 15g of yellow barb, 30g of yellow spirit, 30 g of cuffed crow g, 30 g of shibori matai indigo, 30 g of cypress leaves, 12 g of cypress, 12 g of tenma, 10 g of charcoal, 10 g of jijiako, 25 g of red axle grass, and 35 g of Agia were mixed and ground into powder. (2) The herbal powder in operation (1) is placed in an extraction tank, and 650mL of tertiary water and 800mL of ethanol are added, soaked for 30 minutes, and then alcohol precipitated, concentrated and extracted to obtain the herbal extract, where the extraction is performed 4 times, the extraction time is 5 hours each time, and the extraction temperature is 60℃. (3) 0.3 g of lauric acid glyceride is added to the herbal extract obtained in step (2), and the mixture is stirred by a vortex, centrifuged, left to stand for 24 hours, filtered, and concentrated to obtain the herbal active ingredient @ lauric acid glyceride cyst complex IV.
[0042] Test Example 1: Mouse hair growth test of Chinese herbal active @ cyst complex According to the literature survey, C57BL / 6 mice were selected as the subjects for constructing a hair loss model in this experiment. The hair of the mouse was black and could show a unique hair cycle synchronization. The melanocytes in the trunk skin of this mouse were only present in the hair follicle and synthesized melanin only during the anagen phase. During the anagen phase, melanin was constantly produced by the hairball melanocytes and transmitted to the hair follicle keratinocytes, resulting in a black appearance of the skin. During the catagen phase, melanin production decreased and the skin turned gray-black. During the telogen phase, the hair follicle stopped producing melanin due to the disappearance of the hairball microshrinkage, and the skin turned pink. The telogen hairs were able to induce a new hair cycle that was highly synchronized locally after removal, which was histologically consistent with the changes in the natural cycle of this mouse, so the changes in the hair cycle could be inferred from the changes in skin color.
[0043] Animal modeling: C57BL / 6 mice, female, 7 weeks old, weighing 18-20g. After simple shaving with an animal shaver, hair was removed with hair removal cream to a shaved area of 2 × 3 cm. 2, the skin was successfully modeled to be pink.
[0044] Administration method: The mice that were successfully modeled were randomly divided into 6 groups, with 5 mice in each group, and the corresponding drug was administered to each group twice a day (morning and evening). The application time was the same, and the application amount was 0.4 mL each time, and the administration was repeated for 21 days. The blank group was treated with 55% tincture solvent, the positive control group was administered with 3% minoxidil tincture, and the drug treatment group was administered with the sample prepared in the example of the present invention.
[0045] Now do the following: Group A was administered a herbal extract. Treatment group B was administered the compound of Example 2; Treatment group C was administered the compound of Example 7; How to apply: Apply evenly to hair removal area using a cotton swab. Evaluation index: After administration, the skin color change in the hair-removed area of the mice was observed every day (at a fixed time each day), and one set of photographs was taken every 7 days. The time when the skin color of the hair-removed area of each mouse changed from pink to gray and the time when hair grew back from the gray were recorded, the average hair length of the mice in each group was recorded, and the average change in weight of the mice was recorded.
[0046] After repeated administration for 21 days, the mice were decapitated, the hair was briefly shaved using an animal shaver, and the skin on the back was cut into 2 × 2 cm pieces using scissors. 2 The mice were trimmed to a shape of a hair follicle, and the surface hair was washed off with saline. They were then immersed in 4% paraformaldehyde for 24 to 36 hours. The cut skin tissue sections and HE staining were then observed under an optical microscope for the number of hair follicles in the cross-section and longitudinal section, and the hair follicle morphology. The mice in each group were sampled (×10) in a visual field, and the number of hair follicles was recorded using SPSS.26. TIFF2024545680000002.tif15166
[0047] The cut skin tissue was sectioned and stained with the inflammatory factors IL-6 and TNF-α, and then inflammation was observed under a fluorescent confocal microscope in a field (×200) of mouse skin tissue (positive areas are green). The results of the mouse hair growth test of the herbal actives@cyst complex are shown in Figure 10, Tables 1 and 2. The time it took for the skin color of the hair-removing area of the mice in the treatment group to turn black was significantly shorter than that of the blank group, the length of newly grown hair in the treatment group was significantly better than that of the blank group, and the mouse hair growth effect of the herbal actives@cyst complex is superior to that of the herbal extract system without the addition of cyst precursors. From the above, both Example 2 and Example 7 showed good properties of promoting hair growth in the mouse hair model.
[0048] [Table 1]
[0049] [Table 2]
[0050] [Table 3]
[0051] " ** " indicates a highly significant difference from the control group, P<0.01 The results of the photomicroscopy of the Chinese herbal actives@cyst complex on the back of mice are shown in Figure 11 and Table 3. The blank group had fewer hair follicles, lighter hair follicles, and the lower ends were degenerated and in the regressing stage. The positive control group and treatment groups A, B, and C had more hair follicles, tighter hair follicle distribution, larger hair papillae, obvious melanin pigment in the hair bulb, and hair follicles were still in the growth stage. In addition, the number of hair follicles in treatment groups B and C was slightly higher than that of treatment group A, showing good properties in promoting hair growth in the mouse hair model.
[0052] The results of the fluorescent staining experiment of inflammatory factors on the back of mice using the Chinese herbal actives@cyst complex are shown in Figure 12. There was no obvious difference in the inflammatory status of the mice in each group, the secretion of inflammatory factors in the skin tissue of the mice was normal, and the treatment groups A, B, and C showed no toxic effects on the growth of the mice within 21 days of treatment.
[0053] Test example 2: Human hair growth test of Chinese herbal active @ cyst complex (1) For Examples 1, 2, 4, 5, 7 and 8, a human hair growth experiment was carried out. (2) There were 120 subjects, 60 men and 60 women, aged 26-60 years, who met the inclusion criteria. The subjects were randomly divided into 6 groups, with 20 subjects in each group. (3) Treatment was performed using the herbal actives@cyst complexes prepared in Examples 1, 2, 4, 5, 7, and 8. (4) Apply 5 mL of the herbal actives@cyst complex to the scalp twice daily, observe for systemic and local side effects, and record the results in detail. Examine once weekly and observe for 4 weeks, the results of which are shown in Table 4. (5) The standard of therapeutic effectiveness is divided into (a) effective: no obvious hair loss and a large amount of new hair growth; (b) effective: hair loss is controlled and a small amount of new hair growth; (c) ineffective: no obvious change before and after treatment; and (d) adverse: systemic or local side effects. (6) The results of human trial studies of the herbal actives@cyst complex are shown in Table 1.
[0054] [Table 4]
[0055] From Table 4, Examples 1, 2, 4, 5, 7 and 8 all showed good properties in promoting hair growth in the human body.
[0056] Comparative Example 1 (1) 10g of each number-headed crow, 10g of ink-dry lotus, 30g of shajin, 30g of white jutsu, 12g of sawagata, 30g of red peony, 12g of blue bark, 15g of yellow barb, 30g of yellow spirit, 30 g of cuffed crow g, 30 g of shibori mata indigo, 30 g of cypress leaves, 12 g of cypress, 12 g of tenma, 10 g of charcoal, 10 g of jijiako, 25 g of red axle grass, and 75 g of Agia were mixed and ground into powder. (2) The herbal powder in operation (1) is placed in an extraction tank, and 650 mL of tertiary water and 800 mL of ethanol are added, soaked for 30 minutes, and then alcohol precipitated, concentrated and extracted to obtain the herbal extract, where the extraction is performed 4 times, the extraction time is 4 hours each time, and the extraction temperature is 70°C. (3) The herbal extract obtained in step (2) was vortexed, centrifuged, allowed to stand for 24 hours, filtered and concentrated. The sample was separated into layers, but a precipitate was found at the bottom and a homogeneous and stable solution could not be formed at room temperature. In Comparative Example 1, no cyst precursors were added, and the transmission electron micrograph of the herbal extract is shown in Figure 13. The active materials in the extract have poor dispersibility and serious aggregation, which indicates that the cyst precursors play an important role in the dispersibility, uniformity and stability of the active materials in the herbal extract.
[0057] Comparative Example 2 (1) 10g of each number-headed crow, 10g of ink-dry lotus, 30g of shajin, 30g of white jutsu, 12g of sawagata, 30g of red peony, 12g of blue bark, 15g of yellow barb, 30g of yellow spirit, 30 g of cuffed crow g, 30 g of shibori matai indigo, 30 g of cypress leaves, 12 g of cypress, 12 g of tenma, 10 g of charcoal, 10 g of jijiako, 25 g of red axle grass, and 35 g of Agia were mixed and ground into powder. (2) The herbal powder in operation (1) is placed into an extraction tank, 0.3 g of lauric acid glyceride, 650 mL of tertiary water and 800 mL of ethanol are added, soaked for 30 minutes, subjected to alcohol precipitation, concentrated, extracted, centrifuged, left to stand for 24 hours, filtered, concentrated, and the sample is stratified. A large amount of oil droplets are precipitated, and the dispersion is poor, and a uniform and stable herbal active substance@cyst complex cannot be formed at room temperature. In Comparative Example 2, the order of addition of the cyst precursors was changed. As shown in FIG. 14, the transmission electron microscope image of the mixture of lauric acid glyceride and Chinese herbal extract showed poor dispersibility of the extract in the sample and serious aggregation, which demonstrated that the order of addition of the cyst precursors affected the solubility and dispersibility of the Chinese herbal extract.
[0058] Comparative Example 3 (1) 10g of each number-headed crow, 10g of ink-dry lotus, 30g of shajin, 30g of white jutsu, 12g of sawagata, 30g of red peony, 12g of blue bark, 15g of yellow barb, 30g of yellow spirit, 30 g of cuffed crow g, 30 g of shibori matai indigo, 30 g of cypress leaves, 12 g of cypress, 12 g of tenma, 10 g of charcoal, 10 g of jijiako, 25 g of red axle grass, and 35 g of Agia were mixed and ground into powder. (2) The herbal powder in operation (1) is placed in an extraction tank, and 650mL of tertiary water and 800mL of ethanol are added, soaked for 30 minutes, and then alcohol precipitated, concentrated and extracted to obtain the herbal extract, where the extraction is performed 4 times, the extraction time is 4 hours each time, and the extraction temperature is 70℃. (3) 5 g of Tween 80 was added to the Chinese herbal extract obtained in procedure (2), vortexed, centrifuged, allowed to stand for 24 hours, filtered and concentrated. No spherical cyst structure was found in the sample, and serious aggregation and stratification appeared after 48 hours. A homogeneous and stable Chinese herbal actives@cyst complex could not be formed at room temperature. The cyst precursor in Comparative Example 3 is Tween 80, and the transmission electron micrograph of its mixture with herbal actives is shown in Figure 15. Tween 80 cannot form cyst structures in the Chinese herbal extract, resulting in serious aggregation of the extract, poor dispersibility, and the active ingredients are encapsulated and not released.
[0059] Comparative Example 4 (1) 10g of each number-headed crow, 10g of ink-dry lotus, 30g of shajin, 30g of white jutsu, 12g of sawagata, 30g of red peony, 12g of blue bark, 15g of yellow barb, 30g of yellow spirit, 30 g of cuffed crow g, 30 g of shibori matai indigo, 30 g of cypress leaves, 12 g of cypress, 12 g of tenma, 10 g of charcoal, 10 g of jijiako, 25 g of red axle grass, and 35 g of Agia were mixed and ground into powder. (2) The herbal powder in operation (1) is placed in an extraction tank, and 650mL of tertiary water and 800mL of ethanol are added, soaked for 30 minutes, and then alcohol precipitated, concentrated and extracted to obtain the herbal extract, where the extraction is performed 4 times, the extraction time is 4 hours each time, and the extraction temperature is 70℃. (3) 0.4 g of glyceryl stearate was added to the Chinese herbal extract obtained in procedure (2), followed by vortex stirring, centrifugation, standing for 24 hours, filtration and concentration. The sample had poor dispersion, no cyst structure was found, and serious aggregation occurred. After 30 minutes, stratification occurred. A homogeneous and stable Chinese herbal actives@cyst complex could not be formed at room temperature. Comparative Example 4 Transmission electron micrograph of the mixture of Chinese herbal actives and stearic acid glyceride is shown in Figure 16. Only oil droplets were observed in the mixture sample, which explained that stearic acid glyceride could not form cyst structures in the Chinese herbal extract, and the system solubility and dispersibility were poor, so the active ingredients could not be encapsulated and released.
[0060] Comparative Example 5 (1) 10g of each number-headed crow, 10g of ink-dry lotus, 30g of shajin, 30g of white jutsu, 12g of sawagata, 30g of red peony, 12g of blue bark, 15g of yellow barb, 30g of yellow spirit, 30 g of cuffed crow g, 30 g of shibori matai indigo, 30 g of cypress leaves, 12 g of cypress, 12 g of tenma, 10 g of charcoal, 10 g of jijiako, 25 g of red axle grass, and 35 g of Agia were mixed and ground into powder. (2) The herbal powder in operation (1) is placed in an extraction tank, and 650mL of tertiary water and 800mL of ethanol are added, soaked for 30 minutes, and then alcohol precipitated, concentrated and extracted to obtain the herbal extract, where the extraction is performed 4 times, the extraction time is 4 hours each time, and the extraction temperature is 70℃. (3) The herbal extract obtained in step (2) was treated with PEO 77 -PPO 29 -PEO 77 After adding 1 g, vortexing, centrifuging, standing for 24 hours, filtering and concentrating, the sample had poor dispersion, no spherical cyst structure was found, and stratification appeared after 24 hours, failing to form a homogeneous and stable herbal actives@cyst complex at room temperature. Comparative Example 5: Chinese herbal actives and PEO 77 -PPO 29 -PEO 77 A transmission electron micrograph of the (1 g / L) mixture is shown in Figure 17. Cyst precursor PEO 77 -PPO 29 -PEO 77If the concentration is too low, cysts cannot be formed in the Chinese herbal extract system, the solubility and dispersibility of the sample is poor, and the active ingredients cannot be encapsulated and released.
[0061] Comparative Example 6 (1) 10g of each number-headed crow, 10g of ink-dry lotus, 30g of shajin, 30g of white jutsu, 12g of sawagata, 30g of red peony, 12g of blue bark, 15g of yellow barb, 30g of yellow spirit, 30 g of cuffed crow g, 30 g of shibori matai indigo, 30 g of cypress leaves, 12 g of cypress, 12 g of tenma, 10 g of charcoal, 10 g of jijiako, 25 g of red axle grass, and 35 g of Agia were mixed and ground into powder. (2) The herbal powder in operation (1) is placed in an extraction tank, and 650mL of tertiary water and 800mL of ethanol are added, soaked for 30 minutes, and then alcohol precipitated, concentrated and extracted to obtain the herbal extract, where the extraction is performed 4 times, the extraction time is 4 hours each time, and the extraction temperature is 70℃. (3) The herbal extract obtained in step (2) was treated with PEO 13 -PPO 30 -PEO 13 After adding 25 g, vortexing, centrifuging, standing for 24 hours, filtering and concentrating, the sample had poor dispersion, no spherical cyst structure was found, and a homogeneous and stable Chinese herbal actives@cyst complex could not be formed at room temperature. Comparative Example 6: Chinese herbal actives and PEO 13 -PPO 30 -PEO 13 A transmission electron micrograph of the (25 g / L) mixture is shown in Figure 18. Cyst precursor PEO 13 -PPO 30 -PEO 13 If the concentration is too high, cysts cannot be formed in the system, the solubility and dispersibility of the mixed sample is poor, aggregation is serious, and the active ingredient cannot be encapsulated and released.
Claims
1. A herbal active ingredient @ cyst complex having a hair-growth effect, The present invention comprises a Chinese herbal active substance and a cyst, the Chinese herbal active substance being coated in the cyst, a hydrophilic substance being coated in the hydrophilic microdomain, i.e., the water core, and a hydrophobic substance being dissolved between the two layers of the cyst; A Chinese herbal active ingredient @ cyst complex with hair nourishing and hair growth effects.
2. The particle size of the composite is 80 nm to 5 μm; The cyst is a bilayered cyst, the bilayer thickness being between 3 and 7 nm; The herbal active ingredient@cyst complex having hair-growth and hair-restoring effects according to claim 1.
3. The content range of the herbal actives in the herbal actives@cyst complex is 30-100g / L; The herbal active ingredient@cyst complex having hair-growth and hair-restoring effects according to claim 1.
4. The cysts are formed from a system of amphiphilic molecules, the concentration of which ranges from 0.1 to 20 g / L, and the amphiphilic molecules are called cyst precursors. The herbal active ingredient@cyst complex having hair-growth and hair-restoring effects according to claim 1.
5. The herbal active ingredient is extracted from the following raw materials: What-headed crow, Ink-dry lotus, Shajin, Byakujutsu, Sawagata, Red peony, Blue skin, Yellow oak, Essence, Head-headed crow, String-legged blue, Side oak leaf, Senkyu, Tianma, Umei charcoal, Jidako, Red axle grass, Agiao, Preferably, the weight ratio of the raw material drug of the Chinese herbal extract is: Hekuhu Karasu 5-15 parts, Sumidoren 5-15 parts, Shajin 20-50 parts, White Jutsu 20-50 parts, Zegata 5-15 parts, Red Peony 20-50 parts, Blue Peel 5-15 parts, Huangbai 5-15 parts, Huang Jing 20-50 parts, Seiku Karasu 2 0 to 50 parts, 20 to 50 parts of shibori indigo, 20 to 50 parts of side oak leaves, 5 to 15 parts of nebula, 5 to 15 parts of tenma, 5 to 15 parts of charcoal, 5 to 15 parts of jijiako, 20 to 50 parts of red axle grass, 20 to 50 parts of agar. The herbal active ingredient@cyst complex having hair-growth and hair-restoring effects according to claim 1.
6. The cyst precursor is selected from one or a combination of mono fatty acid glycerides, mono alkyl phosphate esters and their salts, 2-hydroxy fatty acids and their salts, nicotinic acid and its derivatives, and triblock copolymers; The herbal active ingredient@cyst complex having hair-growth and hair-restoring effects according to claim 4.
7. The mono fatty acid glyceride is a linear mono fatty acid glyceride, preferably a linear mono fatty acid glyceride having a chain length of C8 to C18, more preferably glycerol octanoate, glycerol decanoate, glycerol laurate, glycerol myristate, glycerol pentadecanoate, or glycerol palmitate; Preferably, the monoalkyl phosphate ester and its salt are linear alkyl phosphate ester and its salt, more preferably, linear monoalkyl phosphate ester having a chain length of C8 to C16 or its salt, and even more preferably, octyl phosphate ester and its sodium salt, potassium salt, magnesium salt, zinc salt, decyl phosphate ester and its sodium salt, potassium salt, magnesium salt, zinc salt, lauryl phosphate ester and its sodium salt, potassium salt, magnesium salt, zinc salt, palmisyl phosphate ester and its sodium salt, potassium salt, magnesium salt, zinc salt, Preferably, the 2-hydroxy fatty acid and its salt are 2-hydroxy straight-chain fatty acids and their salts, more preferably C8 to C16 2-hydroxy straight-chain fatty acids and their salts, and even more preferably 2-hydroxyoctanoic acid and its sodium, potassium, magnesium or zinc salts, 2-hydroxydecanoic acid and its sodium, potassium, magnesium or zinc salts, 2-hydroxylauric acid and its sodium, potassium, magnesium or zinc salts, 2-hydroxycarminic acid and its sodium, potassium, magnesium or zinc salts, Preferred examples of nicotinic acid and its derivatives include nicotinic acid, benzyl nicotinate, and tocopherol nicotinate. Preferably, the chemical formula of the triblock copolymer is PEOx-PPOy-PEOx, 13≦x≦133, 29≦y≦65, more preferably PEO77-PPO29-PEO77, PEO13-PPO30-PEO13, PEO24-PPO35-PEO24, PEO133-PPO50-PEO133, PEO19-PPO30-PEO19, PEO100-PPO65-PEO100, PEO26-PPO40-PEO26. The herbal active ingredient@cyst complex having hair-growth and hair-restoring effects according to claim 6.
8. The method for producing the herbal active ingredient @ cyst complex having hair growth and hair care effects according to claim 1, Add mixed solvent to the raw drug to extract, collect the extract, add cyst precursor, mix, alcohol precipitate, centrifuge, filter and concentrate to obtain Chinese herbal actives @ cyst complex; A method for producing a Chinese herbal active @ cyst complex having a hair-growth effect, comprising:
9. The mixed solvent is an ethanol-water mixture, The volume percentage concentration of ethanol in the ethanol-water mixture is 40% to 80%; The number of times of extraction is 1 to 5 times, the time of extraction is 1 to 5 hours, and the extraction temperature is 55°C to 80°C. A method for preparing the herbal active ingredient@cyst complex having hair-growth effect according to claim 8.
10. Application of the herbal active ingredient@cyst complex having hair-growth effect according to claim 1 in the field of cosmetics.
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