Compound composition for preventing hair loss and promoting hair growth and application thereof

Abstract

The invention relates to the technical field of medicines, in particular to a compound composition for preventing alopecia and promoting hair growth and application thereof. The invention provides a compound composition for preventing hair loss and promoting hair growth. The compound composition is prepared from the following raw materials in parts by weight: 1-5 parts of amentoflavone and 1-10 parts of unodil. The invention provides an application of amentoflavone and unodil in hair loss prevention and hair growth. An in-vitro cell experiment shows that after the amentoflavone and the unodil are combined, the proliferation of human primary dermal papilla cells can be promoted. A preclinical animal experiment shows that after the amentoflavone and the unodil are locally used, the hair growth speed is increased, and the hair density is increased.

Description

Technical Field

[0001] This invention relates to the field of pharmaceutical technology, and in particular to a compound combination for preventing hair loss and promoting hair growth, and its application. Background Technology

[0002] Hair loss refers to the phenomenon of hair falling out. Normally shed hairs are those in the telogen (resting) and catagen (transitional) phases. Because the number of hairs entering the telogen phase and those newly entering the anagen (growth) phase is constantly in dynamic equilibrium, a normal amount of hair is maintained. Pathological hair loss refers to abnormal or excessive hair loss, the causes of which are more complex and are regulated by multiple factors and genes. On average, one in six people will experience hair loss, and the incidence of hair loss in men is twice that of women.

[0003] Currently, most medications used to treat hair loss require long-term maintenance, are prone to relapse after discontinuation, and often have significant side effects, including scalp itching and hirsutism, thus limiting treatment options. Minoxidil, a commonly used medication, primarily works by stimulating blood circulation in the scalp, promoting hair follicle activity and hair growth. However, it experiences a "rapid shedding phase" in the initial stages, which some patients find difficult to accept, leading them to discontinue treatment. Additionally, finasteride inhibits benign prostatic hyperplasia (BPH) and improves androgenetic alopecia by lowering dihydrotestosterone levels in the blood and prostate tissue. However, finasteride has significant side effects, such as erectile dysfunction, decreased libido, and gynecomastia.

[0004] Amentoflavone is a compound extracted from plants, medicinal herbs, or processed medicinal materials, and can also be synthesized artificially. Its English name is Amentoflavone; its molecular formula is C2. 30 H 18 O 10 The molecular weight is 538.46, and the chemical structural name is 4H-1-benzopyran-4-one, 8-[5-(5,7-dihydroxy-4-oxo-4H-1-benzopyran)-2-hydroxyphenyl]-5,7-dihydroxy-2-(4-hydroxyphenyl)-, and the English chemical structural name is 4H-1-Benzopyran-4-one, 8-[5-(5,7-dihydroxy-4-oxo-4H-1-benzopyran-2-y1)-2-hydroxypheny1]-5,7-dihydroxy-2-(4-hydroxyphenyl)-). The structural formula is as follows: Formula 1 Unodil is a compound that can be extracted from plants (such as the seeds of sea buckthorn) and can also be obtained through artificial synthesis. Its English name is Unodil, its molecular formula is C4H6N4O, its molecular weight is 126.12, and its chemical structural name is 2,4-diaminopyrimidine-3-oxide. The structural formula is as follows: Formula 2 With the development of the biomedical and cosmetic fields, an increasing number of natural plant ingredients and synthetic compounds are being used in research and product development for hair loss prevention and hair regrowth promotion. Taxodium flavonoids and unirandil, as two promising drug components, have gradually gained attention in the field of hair loss treatment in recent years. Studies have found that taxodium flavonoids can effectively stimulate the activity of hair follicle cells, promote hair growth, and have a significant effect on preventing hair loss. Unirandil, on the other hand, is a compound that has been found in recent years to have a significant hair regrowth-promoting effect. It effectively improves hair loss symptoms through mechanisms such as regulating the hair growth cycle and promoting hair follicle regeneration. Its unique mechanism of action makes it a promising candidate for widespread application in hair loss treatment.

[0005] Currently, there are some hair loss prevention and hair regrowth products on the market based on single ingredients, but most of these products have limited effectiveness or side effects. This invention innovatively combines paclitaxel biflavonoids and unoxidil to form a novel drug combination, aiming to enhance their respective pharmacological effects through synergistic action, achieving better hair loss prevention and hair regrowth promotion results. This drug combination not only demonstrates excellent efficacy in treating hair loss but also, to some extent, avoids the side effects of existing treatments. Summary of the Invention

[0006] The purpose of this invention is to provide a drug combination for preventing hair loss and promoting hair growth, and its application. The technical problem to be solved by this invention is to provide a drug combination for preventing hair loss and promoting hair growth. In practical applications, paclitaxel flavonoids and unoxidil can be used as effective ingredients to promote hair regeneration and growth, to prepare a skin-applied composition, which can be further prepared into pharmaceuticals, cosmetics, daily chemical products, medical devices, disinfectants, etc.

[0007] To achieve the above-mentioned objectives, the present invention provides the following technical solution: This invention provides a compound combination for preventing hair loss and promoting hair growth, comprising the following raw materials in parts by weight: 1-5 parts of Taxodium biflavonoids and 1-10 parts of Unodil.

[0008] Preferably, the raw material composition includes the following parts by weight: 2 parts of Taxodium biflavonoids and 5 parts of Unodil.

[0009] Preferably, the paclitaxel flavonoids are artificially synthesized or extracted from plant raw materials, including plant extracts with a paclitaxel flavonoid content of more than 5% obtained by processes such as enrichment and purification. Preferably, the unopidil is artificially synthesized or extracted from plant raw materials, including plant extracts with an unopidil content of more than 5% obtained through processes such as enrichment and purification.

[0010] This invention also provides the application of the aforementioned compound combination in the preparation of products for preventing hair loss and promoting hair growth.

[0011] Preferably, the hair growth promotion refers to promoting the generation of new hair and promoting the healthy growth of existing hair.

[0012] Preferably, the product is a pharmaceutical or daily chemical product.

[0013] Preferably, the drug is a topical dosage form or an oral preparation.

[0014] Preferably, the topical dosage form is: tincture, gel, foam, patch, ointment, cream preparation or spray.

[0015] Preferably, the oral preparation is a tablet, granule, capsule, syrup, pill, suspension, or drop.

[0016] Preferably, the daily chemical products are: shampoo, conditioner, hair oil, hair liquid, hair essence, scalp cream, hair gel, hair spray, hair mask, or eyebrow care liquid.

[0017] Compared with the prior art, the present invention has the following beneficial effects: This invention provides the application of paclitaxel flavonoids and unoxidil in preventing hair loss and promoting hair growth. In vitro cell experiments show that the combination of paclitaxel flavonoids and unoxidil can promote the proliferation of human primary dermal dermal papilla cells. Preclinical animal experiments show that topical application of paclitaxel flavonoids and unoxidil accelerates hair growth and increases hair density. Attached Figure Description

[0018] To more clearly illustrate the technical solutions in the embodiments of the present invention or the prior art, the drawings used in the description of the embodiments or the prior art will be briefly introduced below. Obviously, the drawings described below are only embodiments of the present invention. For those skilled in the art, other drawings can be obtained based on the provided drawings without creative effort.

[0019] Figure 1 The figure shows the results of the effects of different experimental groups on the proliferation capacity of human primary dermal dermal papilla cells (HDPCs) in Example 1. Figure 2The graph shows the therapeutic effects of different experimental groups on the spontaneous hair growth model of C57BL / 6 mice in Example 2; Figure 3 The results of dermoscopy and HE staining of different experimental groups in Example 2 show the hair regrowth in the C57BL / 6 mouse natural hair growth model.

[0020] Figure 4 The figure shows the effect of different experimental groups on the length of new hair growth in C57BL / 6 mice in Example 2.

[0021] Figure 5 The figure shows the effect of different experimental groups on the weight of new hair growth in C57BL / 6 mice in Example 2. Detailed Implementation

[0022] The technical solutions provided by the present invention will be described in detail below with reference to the embodiments, but they should not be construed as limiting the scope of protection of the present invention.

[0023] Example 1 The experiment on the promotion of proliferation of human primary dermal dermal papilla cells (HDPCs) by the composition was conducted as follows: First, dissolve the powdered paclitaxel flavonoids (40%) and unopil in DMSO to prepare a 20 mg / mL solution. Then, take 0.1 mL and add it to 0.9 mL of 1% HS-15 solution for dilution. Finally, dilute with culture medium (89% high-glucose DMEM medium, 10% fetal bovine serum and 1% penicillin and antibiotic) to the final required concentration.

[0024] Using the CCK-8 assay, human dermal papilla cell lines in the logarithmic growth phase were selected and analyzed at a concentration of 4.5 × 10⁻⁶. 3 Cells were seeded in 96-well plates (margin wells were filled with sterile PBS) and incubated at 37 °C with 5% CO2.

[0025] After the cells adhered to the culture vessel, different concentrations of the drug solution were used: 40% paclitaxel, minoxidil, and a combination (paclitaxel:minoxidil = 2:5), with concentration gradients of 0.2 μg / mL, 0.5 μg / mL, 1.0 μg / mL, 2.0 μg / mL, 5.0 μg / mL, and 10 μg / mL. A blank control group and a minoxidil control group were set up and cultured for 24 h.

[0026] After the drug effect was complete, the drug-containing culture medium was removed, and 100 μL of diluted CCK8 working solution was added per well. The culture plate was gently shaken several times and cultured at 37°C and 5% CO2 for another 2 h. The absorbance of each well was measured at 450 nm, and the cell proliferation rate was calculated.

[0027] The effects of paclitaxel flavonoids, unopidil, and the combination on the proliferation ability of HDPCs in Example 1 are as follows: Figure 1 As shown. By Figure 1 It can be concluded that, compared with the blank control, paclitaxel flavonoids, unopidil and the combination can effectively promote the proliferation of HDPCs, and the combination is superior to the use of paclitaxel flavonoids and unopidil alone.

[0028] Example 2 The efficacy evaluation experiment of the composition in the C57BL / 6 mouse spontaneous hair regrowth model was conducted as follows: The experimental animals were female C57BL / J6 mice, 6 weeks old, weighing 18-20g. The C57BL / 6 mice were raised under normal conditions, with a temperature of 25±2℃ and humidity of 50%-70%, alternating between 12 hours of light and 12 hours of darkness. They were allowed free access to food and water, and the corn cob bedding was changed every two days. The experiment began after they had adapted to the rearing environment for 7 days.

[0029] The powdered Taxodium biflavonoid monomer was dissolved in a solvent (anhydrous ethanol: TAE = 5:4), and then an appropriate amount of Tween 80 was added to promote dissolution. The mixture was heated and sonicated until it was completely dissolved, thus preparing a Taxodium biflavonoid solution with a mass concentration of 0.3%.

[0030] Mix phase A (48.75g water, 0.05g xanthan gum) evenly, heat to 75-80℃ and stir to swell for more than 4 hours. When the temperature drops to 65-70℃, add phase B (2g butylene glycol, 1g propylene glycol, 0.5g panthenol, 0.5g 1,2-hexanediol, 0.1g ethylhexylglycerin, 0.2g phenoxyethanol, 0.5g unopidil, 5g ethanol, 10g water, 1g SOLUBILISANT LRI, 0.2g PA-FR-30) to the system and continue to cool to below 45℃. Add phase C (0.2g cephalotaxel flavonoids, 20g ethanol, 10g diethylene glycol monoethyl ether) and stir until completely homogeneous. Then premix phase D (arginine / citric acid) evenly and slowly add it to the system. Adjust the pH to 6-7 to prepare the essence.

[0031] After weighing, the mice were anesthetized with isoflurane, and the skin on their backs was shaved short using an electric clipper. Hair removal cream was applied evenly to the backs and wiped off after about one minute. The area of ​​hair removed from the mice's backs was approximately 2 cm × 3 cm. This induced the development of highly synchronized anagen-phase hair follicles, which were morphologically indistinguishable from spontaneously formed anagen-phase hair follicles.

[0032] Twelve C57BL / 6 mice were randomly divided into four groups: a model control group (blank), a minoxidil tincture group, a 0.3% calceolone flavonoid group (monomer, DT), and a combination group (essence, JH), with three mice in each group. Starting after hair removal, the mice were treated once daily for 15 consecutive days on the shaved area of ​​their backs. The commercially available minoxidil tincture had a concentration of 5%, and the dosage was 200 μL per mouse. The blank group received a drug-free solution; the 0.3% calceolone flavonoid group received the corresponding monomer solution; and the combination group received the corresponding essence solution, all at a dosage of 200 μL per mouse.

[0033] The efficacy of each experimental group is as follows Figure 2 As shown, dermoscopic observation and HE staining of hair regrowth in a C57BL / 6 mouse natural hair regrowth model using cypermethrin and its composition are as follows. Figure 3 As shown, compared with the blank control group, both paclitaxel flavonoids and the combination significantly promoted hair growth. Furthermore, compared with the positive control drug minoxidil tincture (5%), paclitaxel flavonoids and the combination also significantly promoted hair growth.

[0034] The effect of Taxodium biflavonoids and the composition on the length of newly grown hair in C57BL / 6 mice in Example 2 is as follows: Figure 4 As shown, the effects of Taxodium biflavonoids and the combination on the weight of newly grown hair in C57BL / 6 mice are as follows: Figure 5 As shown. Taxodium biflavonoids and the combination have significant therapeutic effects in promoting hair growth in mice, especially the combination, which is superior to minoxidil tincture in promoting hair growth.

[0035] The above description is only a preferred embodiment of the present invention. It should be noted that for those skilled in the art, several improvements and modifications can be made without departing from the principle of the present invention, and these improvements and modifications should also be considered within the scope of protection of the present invention.

Claims

1. A combination of compounds for preventing hair loss and promoting hair growth, characterized in that, The compound combination comprises amentoflavone and unodeer.

2. The compound combination according to claim 1, characterized in that, The raw material composition comprises amentoflavone 1-5 parts and unodeer 1-10 parts by weight.

3. The compound combination according to claim 1, characterized in that, The raw material composition comprises amentoflavone 2 parts and unodeer 5 parts by weight.

4. The compound combination according to claim 1, characterized in that, The amentoflavone is artificially synthesized or extracted from plant raw materials; the unodeer is artificially synthesized or extracted from plant raw materials.

5. Use of the compound combination according to any one of claims 1-4 in the preparation of a product for preventing hair loss and promoting hair growth.

6. Use according to claim 5, characterized in that, The promoting hair growth is promoting new hair growth and promoting existing hair growth in a healthy state.

7. Use according to claim 5, characterized in that, The product is a pharmaceutical product or a daily-use product.

8. Use according to claim 7, characterized in that, The pharmaceutical product is an external use dosage form or an oral preparation.

9. Use according to claim 8, characterized in that, The external use dosage form is tincture, gel, foam, patch, ointment, cream preparation or spray; the oral preparation is tablet, granule, capsule, syrup, pill, suspension or dropping pill.

10. Use according to claim 7, characterized in that, The daily-use product is shampoo, hair conditioner, hair oil, hair liquid, hair essence, scalp cream, hair gel, hair spray, hair mask or eyebrow care liquid.

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