Scutellaria baicalensis composition for treating chloasma, preparation method and application thereof
Patent Information
- Application Number
- CN202611203207.8
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2026-08-10
- Publication Date
- 2026-10-09
AI Technical Summary
[0005]为了解决现有治疗黄褐斑的产品效果不稳定、副作用大、起效慢的问题，本发明提供一种治疗黄褐斑的黄芩组合物，该组合物疗效稳定、安全性高，能够有效改善黄褐斑色素沉着，不良反应少且起效更快
[0029]1.本发明的黄芩组合物中各组分相互配合，从抑制黑色素生成、抗炎、促进黑色素代谢、修复受损皮肤屏障等多个黄褐斑发病关键靶点共同发挥作用，相较于现有单一作用机制的产品，疗效更稳定，改善黄褐斑色素沉着的效果更显著。
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Abstract
Description
Technical Field
[0001] This invention relates to the field of dermatological medical technology, specifically to the treatment of melasma, and particularly to a Scutellaria baicalensis composition for treating melasma, its preparation method, and its application. Background Technology
[0002] Melasma, commonly known as chloasma, is a common acquired pigmentary skin disease that often occurs on sun-exposed areas of the face. It is symmetrically distributed and usually appears as a yellowish-brown color. The incidence rate is relatively high among young and middle-aged women. The pathogenesis is quite complex and is currently believed to be related to multiple factors such as ultraviolet radiation, endocrine disorders, genetics, changes in sex hormone levels, damage to the skin barrier, and chronic inflammatory responses. There is currently no cure in clinical practice.
[0003] Commonly used clinical treatments include topical medications, oral medications, chemical peels, and laser and photon therapies. However, these treatments have certain limitations: for example, hydroquinone cream, a classic topical medication, can easily cause adverse reactions such as contact dermatitis and permanent hypopigmentation with long-term use; laser treatment is expensive and carries the risk of post-inflammatory hyperpigmentation and recurrence, with most patients experiencing unstable results and difficulty in maintaining long-term remission; oral medications require long-term use and may cause certain systemic toxic side effects. Existing plant extract products for treating melasma also generally suffer from slow onset of action, failing to meet clinical treatment needs. Therefore, there is an urgent need to develop a new drug composition for treating melasma that is safe, effective, and has few side effects.
[0004] Therefore, developing a composition for treating melasma with stable efficacy and high safety has become an urgent problem to be solved in this field. Summary of the Invention
[0005] To address the issues of unstable efficacy, significant side effects, and slow onset of action in existing products for treating melasma, this invention provides a Scutellaria baicalensis composition for treating melasma. This composition exhibits stable efficacy, high safety, and can effectively improve melasma pigmentation with fewer adverse reactions and faster onset of action.
[0006] In a first aspect, this application provides a Scutellaria baicalensis composition for treating melasma, using the following technical solution:
[0007] A Scutellaria baicalensis composition for treating melasma, comprising the following components in parts by weight: 2-5 parts Scutellaria baicalensis compound extract, 0.2-0.5 parts matrine, 0.1-0.2 parts glycolic acid, 0.1-0.2 parts daisy flower extract, 0.01-0.02 parts lime peel extract, 0.002-0.005 parts hop flower extract and 0.002-0.005 parts monk fruit extract;
[0008] The compound extract of Scutellaria baicalensis contains at least 0.01% to 0.02% Scutellaria baicalensis root extract by mass percentage, with the remainder being solvent.
[0009] In the above technical solution, the Scutellaria baicalensis compound extract is a plant compound extract with Scutellaria baicalensis as the main component. Baicalin in the Scutellaria baicalensis root extract has good antioxidant, anti-inflammatory, and tyrosinase-inhibiting effects, which can reduce melanin production, alleviate chronic inflammatory reactions at the site of melasma lesions, improve local vasodilation, and reduce pigmentation from the pathogenesis level. Matrine can play an anti-inflammatory and antibacterial role, regulate the local immune status of the skin, and help repair the damaged skin barrier, reducing the activation of melanocytes by external stimuli. Glycolic acid is a mild chemical exfoliating ingredient that can promote the metabolism of surface aging keratinocytes and accelerate melanin production. The shedding of particles helps active ingredients penetrate the dermis, enhancing the efficacy of the composition. Daisy flower extract soothes skin irritation, reduces inflammation, inhibits melanocyte activity, and reduces melanin transfer to keratinocytes. Lime peel extract promotes skin metabolism, helps tighten the skin, and inhibits tyrosinase activity, reducing pigmentation. Hops flower extract has excellent anti-inflammatory and soothing effects, relieving skin sensitivity and reducing inflammatory triggers for melasma. Monk fruit extract helps scavenge free radicals and enhances the overall skincare effect of the composition. The components work synergistically, acting from multiple angles—inhibiting melanin production, reducing inflammation, promoting melanin metabolism, and repairing the skin barrier—to improve melasma through multiple targets. The treatment is stable and faster-acting, and since most are plant-derived, there are fewer adverse reactions and higher safety.
[0010] Furthermore, based on the mass percentage of the Scutellaria baicalensis compound extract, it includes 0.01%~0.02% Scutellaria baicalensis root extract, 0.1%~0.2% Phellodendron amurense bark extract, 0.01%~0.1% Salix babylonica bark extract, 0.01%~0.1% Rehmannia glutinosa root extract, 0.01%~0.05% Melia toosendan leaf extract, 0.01%~0.02% Houttuynia cordata extract, 0.005%~0.01% Glycine max seed extract, 0.5%~1% Lactobacillus / pear juice fermentation product filtrate, 2%~4% solubilizing agent, 0.5%~2% antioxidant agent, and the balance being solvent.
[0011] In the above-mentioned technical solutions, Phellodendron bark extract can enhance anti-inflammatory and antibacterial effects and reduce skin inflammation; white willow bark extract can gently promote keratin metabolism; Rehmannia glutinosa root extract can provide antioxidant benefits and help soothe and repair the skin; Neem leaf extract can regulate skin condition and strengthen the skin barrier; Houttuynia cordata extract can provide anti-inflammatory and soothing effects and reduce skin sensitivity and discomfort; Soybean seed extract can help moisturize and repair the skin and enhance its resistance; and Lactobacillus / Pear juice ferment filtrate can regulate the skin microecology, maintain the stability of the skin barrier, and further improve the overall treatment effect.
[0012] Furthermore, the mass ratio of the Scutellaria baicalensis compound extract, matrine, glycolic acid, daisy flower extract, sour orange peel extract, hop flower extract, and monk fruit extract is 3:0.5:0.168:0.125:0.015:0.004:0.003.
[0013] Among the above technical solutions, the synergistic effect of each active ingredient is optimal at this ratio, which can achieve a better spot-fading effect with a lower dosage and further reduce the possibility of adverse reactions.
[0014] Furthermore, based on the weight parts of the Scutellaria baicalensis composition for treating melasma, the Scutellaria baicalensis composition for treating melasma further includes 0.01 to 0.03 parts of Euryale ferox extract and 0.005 to 0.01 parts of pomegranate peel extract.
[0015] In the above technical solution, Euryale ferox extract and pomegranate peel extract are further added to the Scutellaria baicalensis composition for treating melasma. The two extracts interact with other components in the Scutellaria baicalensis composition to further reduce angiogenesis, reduce capillary permeability, reduce erythrocyte extravasation, and alleviate erythema reaction at the melasma lesion site. At the same time, they can also enhance the antioxidant capacity of the composition, further inhibit melanin production, and improve the spot-lightening effect.
[0016] Furthermore, the mass ratio of the gorgon fruit extract to the pomegranate peel extract is 2:0.8. This ratio provides the best synergistic effect between the two extracts, allowing them to exert the greatest improvement effect at a relatively low dosage.
[0017] Secondly, this application provides a method for preparing the above-mentioned Scutellaria baicalensis composition for treating melasma, using the following technical solution:
[0018] A method for preparing a Scutellaria baicalensis composition for treating melasma: Weigh each component according to the corresponding weight parts, mix them thoroughly and evenly, and dissolve and disperse them to obtain the finished product.
[0019] Thirdly, this application provides the application of the above-mentioned Scutellaria baicalensis composition for treating melasma in the preparation of topical skin care products or topical medicines for treating melasma, using the following technical solution:
[0020] The Scutellaria baicalensis composition, when added to topical skin care products or medications, can stably exert a spot-fading effect, and when applied topically, it acts directly on the melasma lesions, reducing the adverse reactions caused by systemic medication.
[0021] Furthermore, the topical skincare product is a spot-fading lotion, and the Scutellaria baicalensis composition accounts for 1% to 10% of the spot-fading lotion by mass.
[0022] In the above technical solution, the amount added can ensure the spot-fading effect without increasing the risk of adverse reactions due to excessive addition.
[0023] Furthermore, the spot-fading lotion comprises the following raw materials in weight percentages: 1%~10% Scutellaria baicalensis composition, 0.1%~0.2% solubilizer, 0.2%~0.5% stabilizer, 0.01%~0.02% antioxidant, 0.01%~0.02% colorant, 0.001%~0.003% fragrance, with the balance being solvent.
[0024] Furthermore, the preparation method of the spot-fading lotion includes the following steps:
[0025] Step 1: Put the solvent into the emulsification pot, heat it to 80~85℃ while stirring, add the fragrance and stir well;
[0026] Step 2: Cool down to 42~48℃, add the remaining ingredients in sequence, stir and homogenize thoroughly, and filter to obtain the light spot solution.
[0027] In the above-mentioned technical solution, this application uses a simple preparation method and mild process conditions to maximize the protection of the activity of each active ingredient in the Scutellaria baicalensis composition, making it suitable for large-scale production.
[0028] In summary, this application includes at least one of the following beneficial technical effects:
[0029] 1. The components of the Scutellaria baicalensis composition of the present invention work together to exert their effects on multiple key targets of melasma pathogenesis, such as inhibiting melanin production, anti-inflammation, promoting melanin metabolism, and repairing damaged skin barrier. Compared with existing products with a single mechanism of action, the efficacy is more stable and the effect of improving melasma pigmentation is more significant.
[0030] 2. The Scutellaria baicalensis composition of the present invention is mainly composed of plant-derived ingredients. Compared with traditional chemotherapeutic drugs, it is less irritating to the skin, has a lower incidence of adverse reactions, and is safer for long-term use.
[0031] 3. The Scutellaria baicalensis composition of the present invention, by further adding Euryale ferox extract and pomegranate peel extract, can further reduce angiogenesis, reduce capillary permeability, reduce erythrocyte extravasation, alleviate erythema reaction at the lesion site of melasma, and at the same time enhance the antioxidant capacity of the composition, further inhibit melanin production, and improve the spot-lightening effect.
[0032] 4. The preparation process of the Scutellaria baicalensis composition of the present invention is simple, easy to scale up production, suitable for use in topical skin care products or topical medicines, and has a wide range of applications. Detailed Implementation
[0033] To better illustrate the purpose, technical solution, and advantages of the present invention, the present invention will be further described below in conjunction with specific embodiments.
[0034] Preparation Example 1
[0035] A Scutellaria baicalensis complex extract comprises 55.413g water, 35.927g butylene glycol, 0.01g Scutellaria baicalensis root extract, 0.2g Phellodendron amurense bark extract, 0.01g Salix babylonica bark extract, 0.1g Rehmannia glutinosa root extract, 0.01g Melia toosendan leaf extract, 0.02g Houttuynia cordata extract, 0.01g Glycine max seed extract, 1g Lactobacillus / Pear juice fermentation product filtrate, 5g PEG-60 hydrogenated castor oil, 1g ethylhexylglycerin, 1g glyceryl caprylate, and 0.3g o-cymene-5-ol.
[0036] Among them, the Scutellaria baicalensis root extract is an aqueous extract with an extraction ratio of 1:10, and was purchased from Guangzhou Tongyi Chemical Co., Ltd.
[0037] The bark extract of Phellodendron amurense is an aqueous extract with an extraction ratio of 1:10, and was purchased from Guangzhou Tongyi Chemical Co., Ltd.
[0038] The white willow bark extract is an aqueous extract with an extraction ratio of 1:10, and was purchased from Guangzhou Tongyi Chemical Co., Ltd.
[0039] Among them, the Chinese Rehmannia root extract is an aqueous extract with an extraction ratio of 1:10, and was purchased from Guangzhou Tongyi Chemical Co., Ltd.
[0040] Among them, the Indian neem leaf extract is an aqueous extract with an extraction ratio of 1:10, and was purchased from Guangzhou Tongyi Chemical Co., Ltd.
[0041] The houttuynia cordata extract is an aqueous extract with an extraction ratio of 1:10, and was purchased from Guangzhou Tongyi Chemical Co., Ltd.
[0042] Among them, the wild soybean seed extract is an aqueous extract with an extraction ratio of 1:10, and was purchased from Guangzhou Tongyi Chemical Co., Ltd.
[0043] The lactobacillus / pear juice fermentation product filtrate was purchased from Guangzhou Tongyi Chemical Co., Ltd.
[0044] The preparation method of the Scutellaria baicalensis compound extract includes:
[0045] Weigh each ingredient according to the formula ratio. First, add hydrogenated castor oil, ethylhexylglycerin, glyceryl caprylate, o-cymene-5-ol, and butylene glycol to water and stir until completely dissolved. Then, add the remaining ingredients in sequence and stir continuously for 35 minutes until evenly mixed. After filtration through a 0.22μm microporous membrane for sterilization, the Scutellaria baicalensis compound extract is obtained.
[0046] Preparation Example 2
[0047] A Scutellaria baicalensis compound extract, differing from Preparation Example 1, comprises 52.397 g water, 40.376 g butylene glycol, 0.018 g Scutellaria baicalensis root extract, 0.125 g Phellodendron chinense bark extract, 0.05 g Salix babylonica bark extract, 0.4 g Rehmannia glutinosa root extract, 0.02 g Melia toosendan leaf extract, 0.016 g Houttuynia cordata extract, 0.08 g Glycine max seed extract, 0.7 g Lactobacillus / pear juice fermentation product filtrate, 4 g PEG-60 hydrogenated castor oil, 1 g ethylhexylglycerin, 1 g glyceryl caprylate, and 0.25 g o-cymene-5-ol.
[0048] Preparation Example 3
[0049] A Scutellaria baicalensis compound extract, differing from Preparation Example 1, comprises 52.521 g water, 43.584 g butylene glycol, 0.02 g Scutellaria baicalensis root extract, 0.1 g Phellodendron amurense bark extract, 0.1 g Salix babylonica bark extract, 0.01 g Rehmannia glutinosa root extract, 0.05 g Melia toosendan leaf extract, 0.01 g Houttuynia cordata extract, 0.005 g Glycine max seed extract, 0.5 g Lactobacillus / pear juice fermentation product filtrate, 2 g PEG-60 hydrogenated castor oil, 0.5 g ethylhexylglycerin, 0.5 g glyceryl caprylate, and 0.1 g o-cymene-5-ol.
[0050] Example 1
[0051] A Scutellaria baicalensis composition for treating melasma, comprising 2g of Scutellaria baicalensis compound extract, 0.5g of matrine, 0.1g of glycolic acid, 0.2g of daisy flower extract, 0.01g of lime peel extract, 0.005g of hop flower extract and 0.002g of monk fruit extract.
[0052] Matrine was purchased from Jiangsu Tiansheng Pharmaceutical Co., Ltd.
[0053] The glycolic acid was purchased from Guangzhou Tongyi Chemical Co., Ltd.
[0054] The Scutellaria baicalensis compound extract was prepared in Preparation Example 1.
[0055] The daisy extract is an aqueous extract with an extraction ratio of 1:10, and was purchased from Wuhan Lanabai Pharmaceutical Chemical Co., Ltd.
[0056] Among them, the sour orange peel extract is an aqueous extract with an extraction ratio of 1:10, and was purchased from Shaanxi Xiazhou Biotechnology Co., Ltd.
[0057] Among them, the hop flower extract is a water extract with an extraction ratio of 1:10, and was purchased from Fufeng Sinote Biotechnology Co., Ltd.
[0058] Among them, the monk fruit extract is a water extract with an extraction ratio of 1:10, and was purchased from Fufeng Sinote Biotechnology Co., Ltd.
[0059] The preparation method of the Scutellaria baicalensis composition for treating melasma includes:
[0060] Mix the components evenly according to the proportions, and stir at room temperature in the dark until there are no solid particles to obtain the Scutellaria baicalensis composition.
[0061] Example 2
[0062] A Scutellaria baicalensis composition for treating melasma, differing from Example 1, comprises 3g of Scutellaria baicalensis compound extract, 0.5g of matrine, 0.168g of glycolic acid, 0.125g of daisy flower extract, 0.015g of lime peel extract, 0.004g of hop flower extract and 0.003g of monk fruit extract.
[0063] The Scutellaria baicalensis compound extract was prepared in Preparation Example 2.
[0064] Example 3
[0065] A Scutellaria baicalensis composition for treating melasma, differing from Example 1, comprises 5g of Scutellaria baicalensis compound extract, 0.2g of matrine, 0.2g of glycolic acid, 0.1g of daisy flower extract, 0.02g of lime peel extract, 0.002g of hop flower extract and 0.005g of monk fruit extract.
[0066] The Scutellaria baicalensis compound extract was prepared in Preparation Example 3.
[0067] Example 4
[0068] A Scutellaria baicalensis composition for treating melasma, differing from Example 1, comprises 2g of Scutellaria baicalensis compound extract, 0.5g of matrine, 0.1g of glycolic acid, 0.2g of daisy flower extract, 0.01g of lime peel extract, 0.005g of hop flower extract, 0.002g of monk fruit extract, 0.01g of Euryale ferox extract, and 0.005g of pomegranate peel extract.
[0069] Among them, the Euryale ferox extract is a water extract with an extraction ratio of 1:10, and was purchased from Fufeng Sinote Biotechnology Co., Ltd.
[0070] Among them, the pomegranate peel extract is a water extract with an extraction ratio of 1:10, and was purchased from Ningxia Xiangcao Biotechnology Co., Ltd.
[0071] Example 5
[0072] A Scutellaria baicalensis composition for treating melasma, differing from Example 1, comprises 2g of Scutellaria baicalensis compound extract, 0.5g of matrine, 0.1g of glycolic acid, 0.2g of daisy flower extract, 0.01g of lime peel extract, 0.005g of hop flower extract, 0.002g of monk fruit extract, 0.02g of Euryale ferox extract, and 0.008g of pomegranate peel extract.
[0073] Example 6
[0074] A Scutellaria baicalensis composition for treating melasma, differing from Example 1, comprises 2g of Scutellaria baicalensis compound extract, 0.5g of matrine, 0.1g of glycolic acid, 0.2g of daisy flower extract, 0.01g of lime peel extract, 0.005g of hop flower extract, 0.002g of monk fruit extract, 0.03g of Euryale ferox extract, and 0.01g of pomegranate peel extract.
[0075] Example 7
[0076] A Scutellaria baicalensis composition for treating melasma, differing from Example 5 in that an equal amount of Euryale ferox extract is replaced with Calendula officinalis extract.
[0077] Among them, the calendula extract is a water extract with an extraction ratio of 1:10, and was purchased from Shanyang Lianfeng Biotechnology Co., Ltd.
[0078] Example 8
[0079] A Scutellaria baicalensis composition for treating melasma, differing from Example 5 in that an equal amount of pomegranate peel extract is replaced with cactus extract.
[0080] The cactus extract is a water extract with an extraction ratio of 1:10, and was purchased from Shanyang Lianfeng Biotechnology Co., Ltd.
[0081] Comparative Example 1
[0082] A composition for treating melasma, differing from Example 1 in that an equal amount of Scutellaria baicalensis compound extract is replaced with a mixture of water and butylene glycol.
[0083] The mass ratio of water to butanediol is 1:0.8.
[0084] Comparative Example 2
[0085] A composition for treating melasma, differing from Example 1 in that matrine is replaced by an equal amount of water.
[0086] Comparative Example 3
[0087] A composition for treating melasma, differing from that in Case 1 of 8888, in that glycolic acid is replaced by an equal amount of water.
[0088] Comparative Example 4
[0089] A composition for treating melasma, differing from Example 1 in that daisy extract is replaced in equal amounts with calendula extract.
[0090] Among them, the calendula extract is a water extract with an extraction ratio of 1:10, and was purchased from Shanyang Lianfeng Biotechnology Co., Ltd.
[0091] Comparative Example 5
[0092] A composition for treating melasma, differing from Example 1 in that an equal amount of lime peel extract is replaced with peony root extract.
[0093] Among them, the peony root extract is an aqueous extract with an extraction ratio of 1:10, and was purchased from Fufeng Sinote Biotechnology Co., Ltd.
[0094] Comparative Example 6
[0095] A composition for treating melasma, differing from Example 1 in that an equal amount of hop flower extract is replaced with aloe vera extract.
[0096] The aloe vera extract is a water extract with an extraction ratio of 1:10, and was purchased from Fufeng Sinote Biotechnology Co., Ltd.
[0097] Comparative Example 7
[0098] A composition for treating melasma, differing from Example 1 in that an equal amount of monk fruit extract is replaced with purslane extract.
[0099] Among them, the purslane extract is a water extract with an extraction ratio of 1:10, and was purchased from Shanxi Zhongnuo Biotechnology Co., Ltd.
[0100] Application Example 1
[0101] A spot-fading lotion comprises 89.742g water, 2g glycerin, 5g propylene glycol, 2.817g Scutellaria baicalensis composition, 0.01g 1,2-hexanediol, 0.2g PEG-40 hydrogenated castor oil, 0.2g xanthan gum, 0.02g capryloyl hydroxamic acid, 0.01g caramel color, and 0.001g fragrance.
[0102] The Scutellaria baicalensis composition was prepared by the method described in Example 1.
[0103] The preparation method of the spot-fading lotion includes the following steps:
[0104] Step 1: Put water into the emulsification pot, heat it to 80℃ while stirring, add flavoring and stir well.
[0105] Step 2: Cool down to 42℃, add the remaining ingredients in sequence, stir and homogenize thoroughly, and filter to obtain the light spot solution.
[0106] Application Example 2
[0107] A spot-fading lotion, differing from Application Example 1, comprises 90.405g water, 3g glycerin, 2.231g propylene glycol, 3.815g Scutellaria baicalensis composition, 0.012g 1,2-hexanediol, 0.2g PEG-40 hydrogenated castor oil, 0.3g xanthan gum, 0.015g capryloyl hydroxamic acid, 0.019g caramel color, and 0.003g fragrance.
[0108] The Scutellaria baicalensis composition was prepared by the method described in Example 2.
[0109] The preparation method of the spot-fading lotion includes the following steps:
[0110] Step 1: Put water into the emulsification pot, heat it to 82°C while stirring, add flavoring and stir well.
[0111] Step 2: Cool down to 45℃, add the remaining ingredients in sequence, stir and homogenize thoroughly, and filter to obtain the light spot solution.
[0112] Application Example 3
[0113] A spot-fading lotion, differing from Application Example 1, comprises 86.82g water, 5g glycerin, 2g propylene glycol, 5.527g Scutellaria baicalensis composition, 0.02g 1,2-hexanediol, 0.1g PEG-40 hydrogenated castor oil, 0.5g xanthan gum, 0.01g capryloyl hydroxamic acid, 0.02g caramel color, and 0.003g fragrance.
[0114] The Scutellaria baicalensis composition was prepared using the method described in Example 3. The method for preparing the freckle-lightening lotion includes the following steps:
[0115] Step 1: Put water into the emulsification pot, heat it to 85°C while stirring, add flavoring and stir well.
[0116] Step 2: Cool down to 48℃, add the remaining ingredients in sequence, stir and homogenize thoroughly, and filter to obtain the light spot solution.
[0117] Application Example 4
[0118] A spot-fading lotion, differing from Application Example 1, comprises 90.39g water, 3g glycerin, 2.231g propylene glycol, 3.83g Scutellaria baicalensis composition, 0.012g 1,2-hexanediol, 0.2g PEG-40 hydrogenated castor oil, 0.3g xanthan gum, 0.015g capryloyl hydroxamic acid, 0.019g caramel color, and 0.003g fragrance.
[0119] The Scutellaria baicalensis composition was prepared by the method described in Example 4.
[0120] Application Example 5
[0121] A spot-fading lotion, differing from Application Example 1, comprises 90.377g water, 3g glycerin, 2.231g propylene glycol, 3.843g Scutellaria baicalensis composition, 0.012g 1,2-hexanediol, 0.2g PEG-40 hydrogenated castor oil, 0.3g xanthan gum, 0.015g capryloyl hydroxamic acid, 0.019g caramel color, and 0.003g fragrance.
[0122] The Scutellaria baicalensis composition was prepared by the method described in Example 5.
[0123] Application Example 6
[0124] A spot-fading lotion, differing from Application Example 1, comprises 90.365g water, 3g glycerin, 2.231g propylene glycol, 3.855g Scutellaria baicalensis composition, 0.012g 1,2-hexanediol, 0.2g PEG-40 hydrogenated castor oil, 0.3g xanthan gum, 0.015g capryloyl hydroxamic acid, 0.019g caramel color, and 0.003g fragrance.
[0125] The Scutellaria baicalensis composition was prepared by the method described in Example 6.
[0126] Application Example 7
[0127] A spot-fading lotion, which differs from Application Example 5 in that the Scutellaria baicalensis composition is prepared by the preparation method of Example 7.
[0128] Application Example 8
[0129] A spot-fading lotion, which differs from Application Example 5 in that the Scutellaria baicalensis composition is prepared by the preparation method of Example 8.
[0130] Comparative Application Example 1
[0131] A spot-fading lotion, which differs from Application Example 1 in that the composition is prepared by the preparation method of Comparative Example 1.
[0132] Comparative Application Example 2
[0133] A spot-fading lotion, which differs from Application Example 1 in that the Scutellaria baicalensis composition is prepared by the preparation method of Comparative Example 2.
[0134] Comparative Application Example 3
[0135] A spot-fading lotion, which differs from Application Example 1 in that the Scutellaria baicalensis composition is prepared by the preparation method of Comparative Example 3.
[0136] Comparative Application Example 4
[0137] A spot-fading lotion, which differs from Application Example 1 in that the Scutellaria baicalensis composition is prepared by the preparation method of Comparative Example 4.
[0138] Comparative Application Example 5
[0139] A spot-fading lotion, which differs from Application Example 1 in that the Scutellaria baicalensis composition is prepared by the preparation method of Comparative Example 5.
[0140] Comparative Application Example 6
[0141] A spot-fading lotion, which differs from Application Example 1 in that the Scutellaria baicalensis composition is prepared by the preparation method of Comparative Example 6.
[0142] Comparative Application Example 7
[0143] A spot-fading lotion, which differs from Application Example 1 in that the Scutellaria baicalensis composition is prepared by the preparation method of Comparative Example 7.
[0144] Efficacy verification:
[0145] 1. Effect of the composition on TNF-α-induced VEGF expression in HaCaT cells:
[0146] HaCaT cells in logarithmic growth phase (Shanghai Xinyu Biotechnology Co., Ltd., catalog number: XY-H225) were used at a concentration of 1*10-1 5Cells were seeded at a density of cells / mL in 12-well plates. One control group, one model group, and 15 experimental groups were set up, with five replicates in each group. The control group was cultured in fresh DMEM medium (Shanghai Jiachu Bioengineering Co., Ltd., catalog number: 10-013-CVRC) for 24 h; the model group was cultured in DMEM medium containing 100 ng / mL TNF-α (Shanghai Qiyuan Biotechnology Co., Ltd., catalog number: 300-01A) for another 24 h; and the experimental groups were cultured in DMEM medium containing 100 ng / mL TNF-α and 0.5 μg / mL of the composition corresponding to the example or comparative example for another 24 h. After culture, the cell culture medium was collected from each group, centrifuged (4℃, 12000 r / min, 10 min), and the cell supernatant was collected. The VEGF content in the cell supernatant was detected using the Human VEGF ELISA kit (Shenzhen Zike Biotechnology Co., Ltd., catalog number: ZK-H008) according to the manufacturer's instructions. The experimental results were averaged and are shown in Table 1.
[0147] 2. Effect of the composition on VEGF-induced HUVEC cell proliferation:
[0148] HUVEC cells in logarithmic growth phase (Shanghai Xinyu Biotechnology Co., Ltd., catalog number: XY-H205) were used at a concentration of 1*102 5 Cells were seeded at a density of 100 μL / mL in 96-well plates. One control group, one model group, and 15 experimental groups were set up, with five replicates in each group. The control group was cultured in ECM complete medium (Beijing Bio-Innovation Technology Co., Ltd., catalog number: 1001) for 24 h; the model group was cultured in ECM complete medium containing 200 ng / mL VEGF165 (Beijing Baipusaisi Biotechnology Co., Ltd.) for 24 h; and the experimental groups were cultured in ECM complete medium containing 200 ng / mL VEGF165 and 0.5 μg / mL of the composition corresponding to the example or comparative example for 24 h. After culture, cell viability was detected using the MTT assay. Cell viability (%) = A1 / A2*100%, where A1 is the absorbance of the experimental and model groups, and A2 is the absorbance of the control group. The results were averaged and are shown in Table 1.
[0149] 3. Effects of the composition on VEGF-induced tubular structure in HUVEC cells:
[0150] HUVEC cells in logarithmic growth phase were harvested at a ratio of 2*102 5The cells were seeded at a density of 50 μL / mL in 96-well plates coated with matrix gel (Corning, 50 μL per well). One control group, one model group, and 15 experimental groups were set up, with five replicates in each group. The control group was incubated with complete ECM medium for 8 hours; the model group was incubated with complete ECM medium containing 200 ng / mL VEGF165 for 8 hours; and the experimental groups were incubated with complete ECM medium containing 200 ng / mL VEGF165 and 0.5 μg / mL of the composition of the corresponding example or comparative example for 8 hours. The cells were observed and photographed using an inverted biological microscope (Guangzhou Mingmei Optoelectronic Technology Co., Ltd.), and the images were analyzed using ImageJ to calculate the relative number of nodes and the relative tube length. The relative number of nodes = B1 / B2*100%, where B1 is the number of nodes in the experimental group and the model group, and B2 is the number of nodes in the blank group. The relative tube length = C1 / C2*100%, where C1 is the tube length in the experimental group and the model group, and C2 is the tube length in the blank group. The experimental results are taken as average values, as shown in Table 1.
[0151] Table 1:
[0152]
[0153] As can be seen from the data in Table 1, compared with the model group, the Scutellaria baicalensis composition of the present invention can significantly reduce the content of VEGF in HaCaT cells, effectively inhibit VEGF-induced HUVEC cell proliferation, and significantly reduce the number and total length of tubular structure nodes formed by VEGF-induced HUVECs. This indicates that the Scutellaria baicalensis composition of the present invention can effectively inhibit angiogenesis and has a certain intervention effect on melasma.
[0154] Specifically, based on the analysis of Examples 1, 5, and 7-8, it can be found that: compared to Example 1, Example 5 added Euryale ferox extract and pomegranate peel extract, Example 7 added Calendula officinalis extract and pomegranate peel extract, and Example 8 added Euryale ferox extract and cactus extract. Example 5 can significantly reduce the VEGF content in HaCaT cells and inhibit VEGF-induced HUVEC cell proliferation, reducing the number and total length of tubular structure nodes formed by VEGF-induced HUVECs. This indicates that only by further combining Euryale ferox extract and pomegranate peel extract in the Scutellaria baicalensis composition can the formation of new blood vessels be effectively reduced, capillary permeability reduced, erythrocyte extravasation reduced, erythema reaction at the lesion site of melasma alleviated, and the spot-lightening effect improved.
[0155] 4. Clinical observation on the efficacy of the freckle-fading lotion in treating melasma:
[0156] Participants: 160 female volunteers suffering from melasma were selected. They were diagnosed with melasma according to diagnostic criteria, aged 18-65 years, had not undergone any melasma treatment one month prior to the trial, and did not have other facial pigmentation disorders. The diagnostic criteria were based on the "Chinese Expert Consensus on the Diagnosis and Treatment of Melasma (2021 Edition)" and the "Expert Consensus on Traditional Chinese Medicine Treatment of Melasma."
[0157] Experimental Methods: Volunteers were randomly divided into 16 groups of 10 each. One group received basic treatment: after cleansing their face each evening, they first applied a face mask with water, then applied a moisturizing lotion. The remaining 15 groups, after cleansing their face each evening, used the spot-fading lotion corresponding to the application examples and control examples, respectively, followed by a face mask and then moisturizing lotion. Treatment was administered once daily for 12 weeks. During the trial, volunteers maintained normal sleep patterns and avoided sun exposure and additional spot-fading products. Specific application method: Fully soak a mask sheet in the spot-fading lotion, remove it, and apply it to the face. Leave it on for 15 minutes, then remove it. No rinsing is required. After the face is slightly dry, apply moisturizing lotion directly.
[0158] Indicators for evaluating therapeutic efficacy:
[0159] Irritation test: After 12 weeks of continuous use, only one volunteer experienced mild redness and stinging. The symptoms disappeared after discontinuation of use, and there were no other adverse reactions, indicating good safety.
[0160] The Area and Severity Index (MASI) of Melasma: Before treatment, and at 6 and 12 weeks after treatment, the same physician assessed the severity of melasma in four areas: forehead, left cheek, right cheek, and chin. The assessment included area, color depth, and evenness. The specific scoring method is shown in Table 2. The percentage of melasma in each area is represented by A, color depth by D, and color evenness by H. The MASI score is calculated as: Forehead [0.3A(D+H)] + Right Cheek [0.3A(D+H)] + Left Cheek [0.3A(D+H)] + Chin [0.1A(D+H)]
[24] . The average values of the above results are shown in Table 3.
[0161] Table 2:
[0162]
[0163] Facial pigmentation area analysis: Before treatment, and 6 and 12 weeks after treatment, the absolute values of spots, brown spots, and erythema areas were quantitatively analyzed using VISIA. Spot values reflect the superficial pigmentation of the skin surface; brown spot values reflect the deep pigmentation of the skin; and erythema areas reflect the dermal vascular and inflammatory state. The results were averaged and are shown in Table 3.
[0164] Table 3:
[0165]
[0166] Based on the data in Table 3 and the analysis of application examples 1-8 and comparative application examples 1-7, it can be concluded that: compared with the blank control group that only received basic care, the group that used the freckle-fading lotion containing the Scutellaria baicalensis composition showed a greater decrease in MASI score and VISIA indicators after 12 weeks of treatment than the blank control group. This indicates that the Scutellaria baicalensis composition has a definite improving effect on melasma.
[0167] Specifically, in conjunction with the analysis of Application Example 1 and Comparative Application Examples 1-7, Application Example 1, which added the Scutellaria baicalensis composition prepared in Example 1, showed a good decrease in MASI score, VISIA spot, brown spot, and erythema area score. This proves that the Scutellaria baicalensis composition prepared in Example 1 is the core component for its spot-fading effect. Only when the components of Example 1 work together can a better spot-fading effect be achieved.
[0168] Specifically, combining the results of Application Example 5 with those of other groups: Application Example 5 further combined Euryale ferox extract and pomegranate peel extract with the Scutellaria baicalensis composition of Application Example 1. The freckle-lightening lotion prepared in Application Example 5 showed a significant decrease in MASI score after 12 weeks of treatment. At the same time, in the VISIA test, the superficial spots and deep brown spots in the application example group decreased significantly, and the erythema area also decreased significantly. This indicates that further combining Euryale ferox extract and pomegranate peel extract with the Scutellaria baicalensis composition can not only improve chloasma at the level of melanin deposition, but also significantly lighten spots by inhibiting angiogenesis and alleviating dermal inflammation.
[0169] This specific embodiment is merely an explanation of this application and is not intended to limit it. After reading this specification, those skilled in the art can make modifications to this embodiment without contributing any inventive step, but such modifications are protected by patent law as long as they fall within the scope of the claims of this application.
Claims
1. A Scutellaria baicalensis composition for treating melasma, characterized in that, It includes the following components by weight: 2-5 parts Scutellaria baicalensis compound extract, 0.2-0.5 parts matrine, 0.1-0.2 parts glycolic acid, 0.1-0.2 parts daisy flower extract, 0.01-0.02 parts lime peel extract, 0.002-0.005 parts hop flower extract and 0.002-0.005 parts monk fruit extract; The compound extract of Scutellaria baicalensis contains at least 0.01% to 0.02% Scutellaria baicalensis root extract by mass percentage, with the remainder being solvent.
2. The Scutellaria baicalensis composition for treating melasma according to claim 1, characterized in that, The compound extract of Scutellaria baicalensis comprises, by mass percentage, 0.01%–0.02% Scutellaria baicalensis root extract, 0.1%–0.2% Phellodendron chinense bark extract, 0.01%–0.1% Salix babylonica bark extract, 0.01%–0.1% Rehmannia glutinosa root extract, 0.01%–0.05% Melia toosendan leaf extract, 0.01%–0.02% Houttuynia cordata extract, 0.005%–0.01% Glycine max seed extract, 0.5%–1% Lactobacillus / pear juice fermentation product filtrate, 2%–4% solubilizing agent, 0.5%–2% antioxidant agent, with the balance being solvent.
3. The Scutellaria baicalensis composition for treating melasma according to claim 1, characterized in that, The mass ratio of the Scutellaria baicalensis compound extract, matrine, glycolic acid, daisy flower extract, sour orange peel extract, hop flower extract, and monk fruit extract is 3:0.5:0.168:0.125:0.015:0.004:0.
003.
4. The Scutellaria baicalensis composition for treating melasma according to claim 1, characterized in that, Based on the weight parts of the Scutellaria baicalensis composition for treating melasma, the composition further includes 0.01 to 0.03 parts of Euryale ferox extract and 0.005 to 0.01 parts of pomegranate peel extract.
5. The Scutellaria baicalensis composition for treating melasma according to claim 4, characterized in that, The mass ratio of the gorgon fruit extract to the pomegranate peel extract is 2:0.
8.
6. The use of a Scutellaria baicalensis composition for treating melasma as described in any one of claims 1 to 5 in the preparation of a topical skin care product or topical medicine for treating melasma.
7. The application of the Scutellaria baicalensis composition for treating melasma according to claim 6, characterized in that, The topical skin care product is a spot-fading lotion, and the Scutellaria baicalensis composition for treating melasma accounts for 1% to 10% of the mass percentage in the spot-fading lotion.
8. The application of the Scutellaria baicalensis composition for treating melasma according to claim 7, characterized in that, The spot-fading lotion comprises the following raw materials in weight percentages: 1%~10% Scutellaria baicalensis composition, 0.1%~0.2% solubilizer, 0.2%~0.5% stabilizer, 0.01%~0.02% antioxidant, 0.01%~0.02% colorant, 0.001%~0.003% fragrance, with the balance being solvent.
9. The application of the Scutellaria baicalensis composition for treating melasma according to claim 7, characterized in that, The preparation method of the spot-fading lotion includes the following steps: Step 1: Put the solvent into the emulsification pot, heat it to 80~85℃ while stirring, add the fragrance and stir well; Step 2: Cool to 42~48℃, add the remaining ingredients in sequence, stir and homogenize thoroughly, and filter to obtain the light spot solution.