Natural plant composition for treating acne and application thereof
Through the combination of natural plant extracts such as Scutellaria baicalensis, the problems of skin irritation and drug resistance in existing acne treatments are solved, and safe and effective acne suppression and skin repair are achieved. It is suitable for mild acne and sensitive skin.
Patent Information
- Application Number
- CN202511203684.X
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2025-08-27
- Publication Date
- 2025-09-26
- Estimated Expiration
- 2045-08-27
AI Technical Summary
Among existing acne treatments, retinoic acid drugs have obvious initial skin irritation symptoms, and long-term use leads to drug resistance, affecting the treatment effect. In addition, the chemical synthetic ingredients are highly irritating and cannot meet the needs of mild acne and sensitive skin.
A natural plant composition of Scutellaria baicalensis extract, Cnidium monnieri extract, Viola yedoensis extract, Magnolia officinalis extract, Paeonia lactiflora extract, Ophiopogon japonicus extract and Gastrodia elata extract provides safe and non-irritating anti-acne treatment by inhibiting the proliferation of Propionibacterium acnes, regulating sebum metabolism, inhibiting skin cell inflammation and lightening pigmentation.
The composition significantly inhibits the growth of Propionibacterium acnes, reduces the expression of inflammatory factors, relieves acne and acne scars, repairs the skin barrier, reduces the side effects of chemical drugs, is suitable for mild acne and sensitive skin, and provides comprehensive acne treatment and long-term repair.
Smart Images

Figure CN120695114A_ABST
Abstract
Description
Technical Field
[0001] The invention relates to a natural plant composition for treating acne and application thereof, belonging to the technical field of medicines, disinfectants or daily chemicals. Background Art
[0002] "Acne", also known as "pimples", is a chronic inflammatory skin disease that affects the hair follicles and sebaceous glands. It is common on the face, chest and back. Clinically, it mainly manifests as comedones, papules, pustules, cysts or nodules, often accompanied by enlarged pores and sebum secretion.
[0003] It is currently believed that the pathogenesis of acne vulgaris is primarily related to androgen-induced hypertrophy of the sebaceous glands, excessive sebum secretion, abnormal keratinization of the hair follicle duct openings, the proliferation of microorganisms such as Propionibacterium acnes, and an immune inflammatory response. Androgen is the trigger for sebaceous gland hyperplasia and excessive sebum secretion. Androgen induces excessive keratinization and narrowing of the hair follicle openings. Excess sebum and shed keratinocytes accumulate within the follicle openings, forming whiteheads. Sebum oxidizes and mixes with surface dirt, forming blackheads. This accumulation of sebum provides abundant nutrients for microorganisms in the sebaceous glands, such as Propionibacterium acnes, Staphylococcus aureus, and Malassezia, promoting their proliferation. Bacterial enzymes break down triglycerides into large amounts of free fatty acids, further stimulating inflammation in the superficial dermal hair follicles, leading to the formation of papules and pustules. The increasing inflammation induces rupture of the hair follicle wall, allowing lipids and microorganisms to enter the deeper dermis, causing follicular and perifollicular inflammation and the formation of deep cysts and nodules. Clinically, acne can be divided into three degrees and four levels according to the degree of skin lesions: mild (level I, only comedones), moderate (level II and level III, with inflammatory papules and pustules), and severe (level IV with nodules and cysts).
[0004] Influenced by genetics, elevated androgen levels, and other factors, the ductal keratinocytes overproliferate and keratinize, causing the ducts to become smaller, narrower, or even clogged. This prevents sebum from being excreted normally, causing it to accumulate within the hair follicles and form comedones. Androgens stimulate sebaceous gland cell proliferation and sebum secretion. Excessive sebum provides a favorable growth medium for microorganisms such as Propionibacterium acnes, which then multiply and stimulate an inflammatory response in the hair follicles and surrounding tissues. Inflammatory mediators such as interleukins cause redness, swelling, and pain in the tissues surrounding the hair follicles, leading to the various inflammatory lesions of acne. Severe inflammatory reactions can further damage the hair follicle walls, allowing sebum and inflammatory substances to enter the surrounding tissues and penetrate the dermis, forming nodules, cysts, and even scars.
[0005] Currently, there are various treatment options for acne, depending on the severity and type of acne, as well as the individual patient's condition. Key topical treatments include retinoids (such as tretinoin cream and adapalene gel), which improve keratinization of the sebaceous ducts and dissolve microcomedones and comedones, and benzoyl peroxide, which has antibacterial and anti-inflammatory properties. For more severe infections, antibiotics such as fusidic acid cream and metronidazole gel can be used in combination to inhibit the growth of pathogenic microorganisms.
[0006] Among existing acne treatments, retinoids often cause skin irritation symptoms such as erythema, scaling, and burning sensations in the early stages of use. Some patients find it difficult to tolerate these symptoms, leading to reduced compliance. Over time, the skin may develop resistance to topical medications like benzoyl peroxide and antibiotics, gradually reducing their effectiveness. Irritation and resistance are significant factors that affect acne treatment, further contributing to poor efficacy. Summary of the Invention
[0007] The present invention aims to provide a natural plant composition for treating acne and its use. Based on the pathogenesis of acne, the natural plant composition of the present invention inhibits and repairs comedones, blackheads, redness, papules, pimples, pustules, acne scars, and skin barrier damage caused by P. acnes and inflammation by multiple pathways, including inhibiting the proliferation of P. acnes, regulating sebum metabolism, inhibiting skin cell inflammation, and reducing pigmentation. The composition is stable, safe, and non-irritating to the skin, and exhibits excellent anti-acne efficacy.
[0008] A first aspect of the present invention provides a natural plant composition for treating acne, comprising at least two or more selected from the group consisting of Scutellaria baicalensis extract, Cnidium monnieri extract, Viola yedoensis extract, Magnolia officinalis extract, Paeonia lactiflora extract, Ophiopogon japonicus extract, Milk thistle extract, and Gastrodia elata extract.
[0009] Furthermore, in the natural plant composition, by weight, the content of Scutellaria baicalensis extract is not higher than 80%, the content of Cnidium monnieri extract is not higher than 50%, the content of Viola yedoensis extract is not higher than 25%, the content of Magnolia officinalis extract is not higher than 35%, the content of Paeonia lactiflora extract is not higher than 80%, the content of Ophiopogon japonicus extract is not higher than 40%, the content of Milk thistle extract is not higher than 50%, and the content of Gastrodia elata extract is not higher than 50%.
[0010] According to an embodiment of the present invention, each extract is a pharmacopoeial part of a selected medicinal material, which is pulverized, extracted, separated, and purified to initially obtain a crude solid powder of the extract. The extraction method can be selected from water extraction or solvent extraction, and the separation and purification process can be a pharmaceutically acceptable membrane separation method, ultimately obtaining a solution of each plant extract.
[0011] As a specific example, the preparation method of the Gastrodia elata extract is: carefully selecting the dried roots of Gastrodia elata, crushing them, extracting them with a solvent, filtering, concentrating, and drying them to obtain a crude extract; adding butanediol and water to the crude extract to dissolve it, and then centrifuging it at high speed; microfiltration through a ceramic membrane with a pore size of 100 nm, and then passing through a spiral membrane with a molecular weight of 1000 Da to intercept the desired target component to obtain a Gastrodia elata extract solution.
[0012] The preparation methods of the scutellaria baicalensis extract, cnidium monnieri extract, viola yedoensis extract, magnolia bark extract, peony root extract, ophiopogon japonicus extract and silybum marianum extract refer to the preparation method of the scutellaria baicalensis extract above, and are carried out according to the pharmacopoeial parts of each medicinal material.
[0013] As some embodiments of the present invention, the preparations of the natural plant composition include aqueous solutions, gels, emulsions, creams, ointments, and the like.
[0014] The preparation process of the natural plant composition aqueous solution may include: adding one or more moisturizers, such as glycerin, propylene glycol, etc.; and one or more preservatives, such as p-hydroxyacetophenone, phenoxyethanol, etc., to the natural plant composition to prepare the aqueous solution. The moisturizers and preservatives are not limited thereto.
[0015] The preparation process of the natural plant composition gel may include: taking a certain amount of a thickener, such as carbomer, xanthan gum, etc.; a moisturizer, such as glycerin, propylene glycol, sodium hyaluronate, etc.; a preservative, such as p-hydroxyacetophenone, phenoxyethanol, etc.; and a pH adjuster, such as triethanolamine, sodium hydroxide, etc., and preparing the gel with the natural plant composition. The thickener, moisturizer, preservative, pH adjuster, etc. are not limited thereto.
[0016] The preparation process of the natural plant composition emulsion and cream may include: taking two or more of an emollient, such as liquid paraffin, petrolatum, squalane, cetostearyl alcohol, caprylic capric triglyceride, ethylhexylglycerin, glyceryl caprylate, etc.; an emulsifier, such as polyoxyl 40 stearate, polyglyceryl-10 pentastearate, sodium stearoyl lactylate, polysorbate-60, sorbitan isostearate, etc.; a humectant, such as glycerin, propylene glycol, sodium hyaluronate, etc.; a preservative, such as p-hydroxyacetophenone, phenoxyethanol, etc., slowly adding the oil phase to the aqueous phase at a certain temperature, emulsifying, homogenizing, cooling, and formulating with the natural plant composition. The emollient, emulsifier, humectant, preservative, etc. are not limited to these.
[0017] According to one embodiment of the present invention, the natural plant composition may comprise scutellaria baicalensis extract, cnidium monnieri extract, viola yedoensis extract and magnolia bark extract, and is used for relieving itching, inhibiting bacteria, removing acne and anti-inflammation.
[0018] Baicalin, found in Scutellaria baicalensis, can inhibit the activity of 5α-reductase and reduce the conversion of androgens to dihydrotestosterone, which is the main cause of excessive sebaceous gland secretion. This can inhibit the production of dihydrotestosterone and reduce oil secretion from the root (Ju Qiang, Zhao Jianbin, Xia Longqing. Effects of hydrochloric acid scutellariae and baicalin on the expression of type I 5α-reductase mRNA in SZ95 human sebaceous gland cells [J]. Chinese Journal of Leprosy and Skin Diseases, 2009, 25(12):868-870).
[0019] Osthole in Cnidium monnieri not only has anti-inflammatory effects, but also can relieve itching, and can reduce the itching caused by acne skin damage ("Natural coumarin osthole achieves anti-itch effect by selectively inhibiting the skin thermosensitive TRPV3 channel", Molecular Pharmacology, 2018, 94(4), 1164–1173).
[0020] Viola yedoensis has a good inhibitory effect on common pathogenic bacteria (Li Jiaxin, Yang Fengqin, Wang Haoxin, et al. Study on the antibacterial effect of Viola yedoensis produced in Ningxia and Qinghai on 8 strains [J]. Journal of Ningxia Medical University, 2019, 41(1):49-52.). At the same time, Viola yedoensis can reduce the expression of inflammatory factors IL-1β, IL-6, and TNF-α, and reduce the expression of proinflammatory proteases COX-2 and iNOS, and has a significant inhibitory effect on inflammation in eczema skin ("Anti-atopic effect of Viola yedoensis ethanol extract on 2,4-dinitrochlorobenzene-induced atopic dermatitis-like skin dysfunction", Journal of Ethnopharmacology, 2021;280(0):114474-114474).
[0021] Magnolia bark contains honokiol and magnolol, which have the effect of inhibiting Propionibacterium acnes and reducing skin inflammation (Park, Junho et al., "In vitro antibacterial and anti-inflammatory effects of honokiol and magnolol against Propionibacterium acnes", European Journal of Pharmacology, Vol. 496, 1-3 (2004): 189-95).
[0022] From an antibacterial and antimicrobial perspective, unlike single antibacterial or anti-inflammatory ingredients, the combination of Scutellaria baicalensis extract, Cnidium monnieri extract, Viola yedoensis extract, and Magnolia officinalis extract reduces the risk of bacterial resistance, covers a wider bacterial community, and alleviates inflammatory symptoms through both immune and neurological responses. It also protects hair follicle epithelial cells and reduces oxidative sebum accumulation. Furthermore, the combination of Scutellaria baicalensis extract, Cnidium monnieri extract, Viola yedoensis extract, and Magnolia officinalis extract can significantly alleviate the pruritus associated with acne. This combination addresses the four core acne issues of bacteria, inflammation, oxidative stress, and pruritus, enhancing comprehensive treatment and mitigating bacterial resistance associated with long-term use of a single ingredient. The antipruritic effect of Cnidium monnieri can reduce reliance on topical hormones or antibiotics, minimizing drug side effects such as skin atrophy and bacterial imbalance. This combination of natural ingredients is particularly suitable for patients with sensitive skin or mild acne, minimizing the irritation of synthetic ingredients and providing a safe and effective solution for the acute treatment of acne.
[0023] According to another embodiment of the present invention, the natural plant composition may contain peony extract, ophiopogon extract and gastrodia extract, which are used to repair barrier damage caused by inflammation. Gastrodia, ophiopogon and peony contain gastrodia polysaccharide, ophiopogon polysaccharide and ophiopogon saponin, as well as paeoniflorin and other ingredients, among which gastrodin, polysaccharide, barisin, flavonoids and trace elements in gastrodia have antioxidant effects, and gastrodin, polysaccharide and flavonoids have antibacterial and anti-inflammatory and whitening effects (Hu Feng, Chen Hao, Huang Bangli, etc., Application Potential of Gastrodia in Cosmetics [J]. Agricultural Products Processing, 2023, (04): 96-100); the main active ingredient of peony is paeoniflorin, which is both It has an anti-allergic effect (Ruan Yonglan et al., "Paeoniflorin relieves CFA-induced inflammatory pain by inhibiting TRPV1 and succinate / SUCNR1-HIF-1α / NLPR3 pathways", International Immunopharmacology, Vol. 101, (2021): 108364), and an anti-inflammatory effect ("Peony extract relieves antibiotic and DNCB-induced atopic dermatitis symptoms by inhibiting inflammation and changing the composition of the intestinal microbiota of mice", Biomedicine and Drug Therapy, October 2022; 154: 113574). It can not only reduce the inflammatory response in the course of acne, but also reduce skin sensitivity, reduce the "pain" and "itching" caused by redness, swelling and inflammation, and soothe the skin. Ophiopogon japonicus extract contains Ophiopogon japonicus polysaccharides and Ophiopogon japonicus saponins, among which Ophiopogon japonicus saponins have significant anti-inflammatory effects ("Ophiopogon japonicus saponins alleviate blood-brain barrier dysfunction induced by cerebral ischemia by inhibiting TXNIP / NLRP3 inflammasome activation and MAPK pathway"), while Ophiopogon japonicus polysaccharides have the effect of repairing eczema skin and can repair the skin barrier damaged by acne inflammation.
[0024] Unlike single anti-inflammatory or barrier-repairing ingredients, the combination of peony extract, Ophiopogon japonicus extract, and Gastrodia elata extract simultaneously addresses the three core issues of "inflammatory response, barrier damage, and allergic pruritus," targeting the pathological mechanisms of acne from multiple dimensions and providing a synergistic intervention for acne inflammation. The paeoniflorin in peony extract reduces inflammation and has anti-allergic effects, while Ophiopogon japonicus polysaccharides and Gastrodia elata polysaccharides enhance the skin's moisturizing capacity and work together to restore the lipid structure of the barrier. By repairing the skin barrier structurally, paeoniflorin reduces secondary inflammation caused by barrier damage and repairs the skin's immune barrier. Combining the immunomodulatory (peony), antioxidant (Gastrodia elata), and barrier-repairing (Ophiopogon japonicus) properties of natural ingredients, this product provides a safe and effective solution for the long-term repair and management of acne.
[0025] According to another embodiment of the present invention, the natural plant composition may include peony extract and milk thistle extract for use in removing acne scars and hyperpigmentation. Peony extract can inhibit the TRPV1 pathway, reducing redness, stinging, and burning of the skin ("Paeoniflorin alleviates CFA-induced inflammatory pain by inhibiting TRPV1 and the succinate / SUCNR1-HIF-1α / NLPR3 pathway"). Paeoniflorin in peony extract can also reduce redness caused by vasodilation and capillary permeability ("Peony extract alleviates antibiotic- and DNCB-induced atopic dermatitis symptoms by inhibiting inflammation and altering the composition of the mouse gut microbiota," Biomedicine & Pharmacotherapy, 2022, Oct;154:113574). Therefore, peony extract can reduce acne scars and hyperpigmentation caused by acne inflammation. At the same time, paeoniflorin has antioxidant activity (Li Na, Li Jinlian, Liu Yuling, et al. Extraction process and antioxidant activity of paeoniflorin [J]. Journal of Binzhou Medical College, 2020, 43(5): 373-376), which can reduce pigmentation caused by oxidative stress damage to keratinocytes.
[0026] Milk thistle extract has strong antioxidant activity ("In vitro antioxidant activity of silymarin", Journal of Enzyme and Medicinal Chemistry), which can exert antioxidant effects by downregulating the expression of ROS and MDA ("Silymarin vs. silymarin: Differences in antioxidant and neuroprotective effects against H2O2-induced oxidative stress in PC12 cells", Natural Product Communications, 2016;11(5)). Milk thistle can inhibit melanin production ("Silymarin inhibits melanin synthesis in melanocytes", Journal of Pharmacy and Pharmacology, Vol. 61, 5 (2009): 663-7), reduce melasma ("Silymarin cream for melasma", BMC Dermatology, Vol. 12, 18 (2012)) and lighten pigmentation ("Silymarin alleviates UV- and air pollution-induced oxidative stress and inflammation in human epidermis and activates β-endorphin release via cannabinoid receptor type 2").
[0027] In acne treatment, the repair process for acne scars caused by cellular damage, such as red and black acne marks left by inflammatory damage, is as follows: peony extract inhibits TRPV1 / NLRP3, reducing vascular leakage and thereby interrupting the vicious cycle of inflammation-vasodilation-pigmentation. Milk thistle extract inhibits oxidative stress by scavenging ROS, thereby protecting keratinocytes and preventing overactivation of melanocytes. Both peony and milk thistle extracts inhibit pigmentation from the entire synthesis-transport-deposition pathway. Peony targets the inflammatory vascular response, while milk thistle targets melanin metabolism, forming a three-dimensional intervention model of "anti-inflammatory, anti-oxidative, and anti-melanin." Simultaneously, these two ingredients mitigate cellular oxidative stress and damage, reducing the formation of acne scars. Their long-term effects on acne treatment include preventing new acne lesions (reducing the risk of hyperpigmentation), repairing existing acne scars (accelerating pigment metabolism), and reducing the appearance of acne scars.
[0028] According to a preferred embodiment of the present invention, the natural plant composition may include scutellaria baicalensis extract, cnidium monnieri extract, viola yedoensis extract, magnolia bark extract, peony extract, ophiopogon japonicus extract, milk thistle extract and gastrodia elata extract.
[0029] In the above preferred embodiment, further, in the natural plant composition, by weight, the content of Scutellaria baicalensis extract is not higher than 80%, the content of Cnidium monnieri extract is not higher than 50%, the content of Viola yedoensis extract is not higher than 25%, the content of Magnolia officinalis extract is not higher than 35%, the content of Paeonia lactiflora extract is not higher than 80%, the content of Ophiopogon japonicus extract is not higher than 40%, the content of Milk thistle extract is not higher than 50%, and the content of Gastrodia elata extract is not higher than 50%.
[0030] Furthermore, the natural plant composition comprises, by weight, 1-80% of Scutellaria baicalensis extract, 1-50% of Cnidium monnieri extract, 1-25% of Viola yedoensis extract, 1-35% of Magnolia officinalis extract, 1-80% of Paeonia lactiflora extract, 1-40% of Ophiopogon japonicus extract, 1-50% of Milk thistle extract and 1-50% of Gastrodia elata extract.
[0031] Furthermore, the natural plant composition comprises, by weight, 5-30% of the Scutellaria baicalensis extract, 5-25% of the Cnidium monnieri extract, 5-25% of the Viola yedoensis extract, 1-15% of the Magnolia officinalis extract, 1-15% of the Paeonia lactiflora extract, 1-20% of the Ophiopogon japonicus extract, 1-30% of the Milk thistle extract and 1-25% of the Gastrodia elata extract.
[0032] Furthermore, the natural plant composition comprises, by weight, 10-25% of Scutellaria baicalensis extract, 10-20% of Cnidium monnieri extract, 10-20% of Viola yedoensis extract, 5-12.5% of Magnolia officinalis extract, 5-12.5% of Paeonia lactiflora extract, 5-15% of Ophiopogon japonicus extract, 5-25% of Milk thistle extract and 5-20% of Gastrodia elata extract.
[0033] Furthermore, in the natural plant composition, the weight ratio of Scutellaria baicalensis extract, Cnidium monnieri extract, Viola yedoensis extract, Magnolia officinalis extract, Paeonia lactiflora extract, Ophiopogon japonicus extract, Milk thistle extract and Gastrodia elata extract is 1.5~5.5: 1.5~4.5: 1.5~4.5: 1~2.5: 1~2.5: 1~1.5: 1~3.5:1~1.5.
[0034] Furthermore, the natural plant composition comprises, by weight, 25% of Scutellaria baicalensis extract, 20% of Cnidium monnieri extract, 20% of Viola yedoensis extract, 10% of Magnolia bark extract, 10% of Paeonia lactiflora extract, 5% of Ophiopogon japonicus extract, 5% of Milk thistle extract and 5% of Gastrodia elata extract, or comprises 20% of Scutellaria baicalensis extract, 15% of Cnidium monnieri extract, 15% of Viola yedoensis extract, 12.5% of Magnolia bark extract, 12.5% of Paeonia lactiflora extract, 5% of Ophiopogon japonicus extract, 15% of Milk thistle extract and 5% of Gastrodia elata extract, or comprises 10% of Scutellaria baicalensis extract, 10% of Cnidium monnieri extract, 10% of Viola yedoensis extract, 5% of Magnolia bark extract, 5% of Paeonia lactiflora extract, 15% of Ophiopogon japonicus extract, 25% of Milk thistle extract and 20% of Gastrodia elata extract.
[0035] According to an embodiment of the present invention, the natural plant composition may further comprise a pharmaceutically acceptable excipient, which may be selected from any one of moisturizers, thickeners, preservatives, emulsifiers, and emollients, or a combination of at least two thereof.
[0036] The second aspect of the present invention provides a method for preparing the natural plant composition, comprising: weighing Scutellaria baicalensis extract, Cnidium monnieri extract, Viola yedoensis extract, Magnolia officinalis extract, Paeonia lactiflora extract, Ophiopogon japonicus extract, Milk thistle extract and Gastrodia elata extract according to weight fraction, and uniformly mixing two or more of them to obtain a compatible composition.
[0037] The third aspect of the present invention provides an application of the natural plant composition in preparing a product for preventing, improving or treating acne, especially in preparing a product for improving acne such as blackheads, whiteheads, blackheads, pimples, papules, pustules, acne marks, pigmentation, and antibacterial, anti-inflammatory, soothing skin, removing acne marks, and removing pigmentation in oily and sensitive skin.
[0038] The products include medicines, disinfection products and daily chemicals.
[0039] A fourth aspect of the present invention provides a pharmaceutical preparation for preventing, improving or treating acne, comprising the natural plant composition. The pharmaceutical preparation can be in the form of an aqueous solution, a gel, an emulsion, a cream or an ointment.
[0040] A fifth aspect of the present invention provides a daily chemical product for preventing and improving acne, comprising the natural plant composition.
[0041] Beneficial effects:
[0042] The natural plant composition of the present invention has significant synergistic effects among the scutellaria baicalensis extract, the cnidium monnieri extract, the viola yedoensis extract, the magnolia bark extract, the peony extract, the ophiopogon japonicus extract, the milk thistle extract, and the gastrodia elata extract. They can synergistically and rapidly inhibit the growth and proliferation of Propionibacterium acnes, reduce the inflammatory factors induced by Propionibacterium acnes, reduce the levels of inflammatory factors in keratinocytes, alleviate and repair post-acne erythema and acne scars, and promote the regression of acne and self-repair of the skin. Focusing on the pathogenesis of acne, the composition "coordinately targets" various pathways of acne pathogenesis, including "antibacterial-immunomodulatory inhibition of inflammation-barrier repair-itch relief-vasodilation inhibition-reduction of pigmentation," to inhibit the proliferation of Propionibacterium acnes, reduce the level of IL-1β, an inflammatory factor produced by keratinocytes induced by Propionibacterium acnes, and inhibit the level of IL-1α, a barrier-damaging factor, in keratinocytes. Furthermore, the composition can treat acne and improve various acne symptoms, including redness, pimples, blackheads, inflammatory papules, acne scars, and acne scars. Moreover, the natural plant composition of the present invention is prepared from natural plant extracts. The composition has stable formula quality, is safe and has no skin irritation, provides a new idea for the treatment of acne and skin repair, and has good market application prospects. BRIEF DESCRIPTION OF THE DRAWINGS
[0043] Figure 1 This is a graph showing the inhibition rate of Propionibacterium acnes in each group in Test Example 1.
[0044] Figure 2 This is a graph showing the effects of each group in Test Example 2 on the expression level of the inflammatory factor IL-1β in keratinocytes induced by Propionibacterium acnes.
[0045] Figure 3 This is a graph showing the effects of each extract composition in Test Example 3 on the expression level of IL-1a, which is involved in keratinocyte barrier damage, induced by stimulating factors (TNF-α / IFN-γ and LPS).
[0046] Figure 4This is a graph showing the inhibitory effects of compositions of different dosage forms on acne symptoms in mice in Test Example 5.
[0047] Figure 5 This is a graph showing the scores of acne symptoms in mice treated with compositions of different dosage forms in Test Example 5.
[0048] Figure 6 The figure shows photographs (72 hours) of guinea pig skin treated with compositions of different formulations in Test Example 6. DETAILED DESCRIPTION
[0049] The technical solution of the present invention is further described below by specific embodiments. Those skilled in the art should understand that the following embodiments are only for helping to understand the present invention and should not be regarded as specific limitations of the present invention.
[0050] The processes, conditions, reagents, and test methods for carrying out the present invention are, except for those specifically mentioned below, common knowledge and general general knowledge in the art and are not particularly limited thereto. The test methods in the examples where specific conditions are not specified are generally performed under conventional conditions or as recommended by the manufacturer.
[0051] Unless otherwise specified, all technical and scientific terms used in this specification have the same meanings as those generally understood by those skilled in the art to which the present invention belongs. However, in the event of any conflict, the present specification including the definitions shall prevail.
[0052] The amounts used in the preparation examples and embodiments of the present invention are by weight, and the materials and instruments used in the preparation examples, embodiments and test examples of the present invention can all be purchased from the market.
[0053] Preparation Example: Preparation of a natural plant extract solution for treating acne
[0054] Preparation of Gastrodia elata extract (H):
[0055] Grind the raw Gastrodia elata medicinal material and pass it through a 20-mesh sieve to remove fine powder and impurities to obtain a coarse powder. Pour the coarse powder into an extraction tank, add 10-12 times the weight of the medicinal material in a 50% ethanol solution, and soak for 50 minutes. Heat the soaked medicinal material for 4-6 hours, filter, and collect the filtrate. Transfer the filtrate to an evaporator and concentrate it with rotary evaporation to obtain a dry product. Grind it, then sieve it to obtain a crude Gastrodia elata extract.
[0056] 2% crude Gastrodia elata extract was dissolved in 45% butanediol and 53% water, and then centrifuged at 20,000 r / min for 10 minutes. The mixture was then microfiltered through a 100 nm pore size ceramic membrane and then passed through a 1000 Da molecular weight spiral membrane to retain impurities, thereby obtaining a Gastrodia elata extract solution.
[0057] The preparation methods and processes of Scutellaria baicalensis extract (A), Cnidium monnieri extract (B), Viola yedoensis extract (C), Magnolia officinalis extract (D), Paeonia lactiflora extract (E), Ophiopogon japonicus extract (F) and Silybum marianum extract (G) refer to the preparation method of Gastrodia elata extract (H) above.
[0058] Example 1. Preparation of a natural plant composition for treating acne
[0059] Based on the extract solutions of each single medicinal material obtained in the above preparation examples, the following compositions were prepared by mixing the single extract components in the following proportions:
[0060] Scutellaria baicalensis extract (60%) and Paeonia lactiflora extract (40%) were compounded in a ratio of 3:2 to obtain composition 1;
[0061] The Scutellaria baicalensis extract (80%) and the Viola yedoensis (20%) extract were compounded in a ratio of 4:1 to obtain composition 2;
[0062] Scutellaria baicalensis extract (80%) and Ophiopogon japonicus extract (20%) were compounded at a ratio of 4:1 to obtain composition 3;
[0063] The peony extract (75%) and the Viola yedoensis extract (25%) were compounded in a ratio of 3:1 to obtain composition 4;
[0064] The peony extract (60%) and the ophiopogon extract (40%) were compounded in a ratio of 3:2 to obtain composition 5;
[0065] Scutellaria baicalensis extract (50%), Paeonia lactiflora extract (25%), and Viola yedoensis extract (25%) were compounded in a ratio of 2:1:1 to obtain composition 6;
[0066] Scutellaria baicalensis extract (40%), Ophiopogon japonicus extract (20%), and Paeonia lactiflora extract (40%) were compounded in a ratio of 2:1:2 to obtain composition 7;
[0067] Scutellaria baicalensis extract (30%), Cnidium monnieri extract (20%), Viola yedoensis extract (15%) and Magnolia officinalis extract (35%) were compounded in a ratio of 3:2:1.5:3.5 to obtain composition 8;
[0068] Scutellaria baicalensis extract (20%), Cnidium monnieri extract (15%), Viola yedoensis extract (15%), Magnolia officinalis extract (12.5%), Paeonia lactiflora extract (12.5%), Ophiopogon japonicus extract (5%), Silybum marianum extract (15%) and Gastrodia elata extract (5%) were compounded in a ratio of 4:3:3:2.5:2.5:1:3:1 to obtain composition 9.
[0069] Scutellaria baicalensis extract (10%), Cnidium monnieri extract (10%), Viola yedoensis extract (10%), Magnolia officinalis extract (5%), Paeonia lactiflora extract (5%), Ophiopogon japonicus extract (15%), Silybum marianum extract (25%), and Gastrodia elata extract (20%) were compounded in a ratio of 2:2:2:1:1:3:5:4 to obtain composition 10.
[0070] Scutellaria baicalensis extract (25%), Cnidium monnieri extract (20%), Viola yedoensis extract (20%), Magnolia officinalis extract (10%), Paeonia lactiflora extract (10%), Ophiopogon japonicus extract (5%), Silybum marianum extract (5%) and Gastrodia elata extract (5%) were compounded in a ratio of 5:4:4:2:2:1:1:1 to obtain composition 11.
[0071] 5% of Scutellaria baicalensis extract, 25% of Cnidium monnieri extract, 20% of Viola yedoensis extract, 5% of Magnolia officinalis extract, 5% of Paeonia lactiflora extract, 5% of Ophiopogon japonicus extract, 30% of Silybum marianum extract and 5% of Gastrodia elata extract were compounded in a ratio of 1:5:4:1:1:1:6:1 to obtain composition 12.
[0072] 20% of Scutellaria baicalensis extract, 5% of Cnidium monnieri extract, 5% of Viola yedoensis extract, 5% of Magnolia officinalis extract, 5% of Paeonia lactiflora extract, 20% of Ophiopogon japonicus extract, 30% of Silybum marianum extract and 10% of Gastrodia elata extract were compounded in a ratio of 4:1:1:1:1:4:6:2 to obtain composition 13.
[0073] 20% of Scutellaria baicalensis extract, 5% of Cnidium monnieri extract, 5% of Viola yedoensis extract, 15% of Magnolia officinalis extract, 15% of Paeonia lactiflora extract, 20% of Ophiopogon japonicus extract, 10% of Silybum marianum extract and 10% of Gastrodia elata extract were compounded in a ratio of 4:1:1:3:3:4:2:2 to obtain composition 14.
[0074] Example 2. Preparation of gels, emulsions, and creams of natural plant compositions for treating acne
[0075] The composition in this example is composed of the following components in weight fractions (i.e., Composition 11): 25% Scutellaria baicalensis extract, 20% Cnidium monnieri extract, 20% Viola yedoensis extract, 10% Magnolia officinalis extract, 10% Paeonia lactiflora extract, 5% Ophiopogon japonicus extract, 5% Milk thistle extract, and 5% Gastrodia elata extract.
[0076] Preparation method:
[0077] (1) Preparation of the gel of composition 11:
[0078] Preparation of gel: Add 0.6% carbomer to water and swell overnight for later use;
[0079] Add 5% glycerin, 0.2% sodium hyaluronate, 0.1% ectoine, and 0.5% parahydroxyacetophenone and stir evenly, then add 10% of composition 11, and finally add an appropriate amount of triethanolamine and stir evenly to obtain a transparent composition 11 gel.
[0080] (2) Preparation of Composition 11 Emulsion:
[0081] Oil phase: Add 0.5% behenyl alcohol, 1% polyglyceryl-10 pentastearate, 0.5% sodium stearoyl lactylate, 2% caprylic capric triglyceride, 1% ethylhexylglycerin, 1% glyceryl caprylate, and 2% ethylhexyl palmitate to a beaker, heat and stir evenly, and keep warm at 70-80℃. This is used as the oil phase.
[0082] Aqueous phase: Add 1% polysorbate 60, 0.8% sorbitan isostearate, 0.2% hydroxyethyl acrylate / sodium acryloyldimethyl taurate copolymer, and 1% polyglyceryl-10 laurate to a beaker, add purified water and stir to dissolve, then add 5% glycerol and 0.5% p-hydroxyacetophenone and stir evenly. Keep warm at 70-80°C to prepare the aqueous phase.
[0083] Emulsification and homogenization: slowly add the oil phase into the water phase, emulsify for 2 to 5 minutes, and then start homogenization for 3 to 5 minutes;
[0084] Cooling: When the temperature drops to 40-50°C, add 0.2% sodium hyaluronate, 0.1% ectoine and 10% composition 11, stir evenly to obtain a composition 11 emulsion.
[0085] (3) Preparation of Composition 11 Cream:
[0086] Oil phase: Add 5% cetostearyl alcohol, 5% liquid paraffin, 5% vaseline, and 5% glyceryl mono- and distearate into a beaker, heat and stir evenly, and keep warm at 70-80℃. This is used as the oil phase.
[0087] Aqueous phase: Add 5% polyoxyl 40 stearate to a beaker, add purified water and stir to dissolve, then add 0.5% p-hydroxyacetophenone and 5% glycerol, and keep warm at 70-80°C to prepare the aqueous phase.
[0088] Emulsification and homogenization: slowly add the oil phase into the water phase, emulsify for 2 to 5 minutes, and then start homogenization for 3 to 5 minutes;
[0089] Cooling: When the temperature drops to 40-50°C, add 0.2% sodium hyaluronate, 0.1% ectoine and 10% composition 11, stir evenly to obtain a cream of composition 11.
[0090] Test Example 1. In vitro inhibition of the growth of P. acnes by a single extract and a combination
[0091] The single extract fractions and extract combinations were tested for their ability to inhibit the growth of P. acnes in vitro.
[0092] Test method: Cultivate Propionibacterium acnes to the logarithmic growth phase and measure the OD value of the bacterial solution using a microplate reader. 600 , adjust the bacterial concentration and add 100 μL / 2.5×10 5 CFU / mL suspension of P. acnes. Prepare various plant extracts (the preparation methods and concentrations of each extract are described below) as the test group, and set up a positive control group (BHI medium + 2.5×10 5 CFU / mL of P. acnes) and negative control group (culture medium). The inoculated 96-well plate was placed in an anaerobic culture bag and incubated in an incubator at 37°C for 48 h. 600 The inhibition rate was calculated based on the OD value measured at nm: inhibition rate (%) = (OD value of the positive control group - OD value of the test group) / (OD value of the positive control group - OD value of the negative control group) × 100%.
[0093] Among them, the preparation method and concentration of each extract are:
[0094] Weigh 1 g of each single plant extract prepared in the Preparation Example and dilute to 10 mL with purified water to obtain a 100 mg / mL test stock solution for later use. Prior to testing, dilute the test solutions with BHI medium to obtain 2 mg / mL concentrations of each of the following: Scutellaria baicalensis extract (A), Cnidium monnieri extract (B), Viola yedoensis extract (C), Magnolia officinalis extract (D), Paeonia lactiflora extract (E), Ophiopogon japonicus extract (F), Milk thistle extract (G), and Gastrodia elata extract (H). 100 μL / well of each solution was added to the test wells, for a final concentration of 1 mg / mL for all test solutions.
[0095] Weigh 1 g of each composition extract prepared in Example 1 and dilute to 10 mL with purified water to obtain a 100 mg / mL test stock solution for use. Prior to testing, dilute with BHI medium to obtain a 2 mg / mL concentration of each of the test solutions for Composition 1, Composition 2, Composition 3, Composition 4, Composition 5, Composition 6, Composition 7, Composition 8, Composition 9, Composition 10, Composition 11, Composition 12, Composition 13, and Composition 14. 100 μL / well was added to the test wells, resulting in a final concentration of 1 mg / mL for all test solutions.
[0096] Test results:
[0097] Figure 1 The results in Table 1 show that the extracts of Scutellaria baicalensis, Cnidium monnieri, Viola yedoensis, Magnolia officinalis, and Paeonia lactiflora all have a certain inhibitory effect on the growth of Propionibacterium acnes. The extracts of Ophiopogon japonicus, Silybum marianum, and Gastrodia elata have a weaker inhibitory effect on the growth of Propionibacterium acnes.
[0098] After compounding the natural plants, it was found that compared with single extracts, Scutellaria baicalensis extract + Paeonia lactiflora extract (Composition 1), Scutellaria baicalensis extract + Viola yedoensis extract (Composition 2), Paeonia lactiflora extract + Viola yedoensis extract (Composition 4), Scutellaria baicalensis extract + Paeonia lactiflora extract + Viola yedoensis extract (Composition 6), Scutellaria baicalensis extract + Cnidium monnieri extract + Viola yedoensis extract + Magnolia bark extract (Composition 8) and Scutellaria baicalensis extract + Cnidium monnieri extract + Viola yedoensis extract + Magnolia bark extract + Paeonia lactiflora extract + Ophiopogon japonicus extract + Milk thistle extract + Gastrodia elata extract (Compositions 9, 10 and 11) still had significant antibacterial effects on Propionibacterium acnes, while the inhibitory effects of the combinations of Compositions 3, 5, 7 and 12, 13, and 14 on Propionibacterium acnes decreased or remained basically unchanged. The antibacterial effects of compositions 1, 2, 4, 6, 8, 9, 10 and 11 were significantly improved, and the antibacterial rates of these compositions were all greater than 80%, among which the antibacterial rates of compositions 6, 9 and 11 were greater than 90%.
[0099] Among them, the effect of inhibiting Propionibacterium acnes is: composition 11>composition 9>composition 6>composition 2>composition 4>composition 10>composition 8, indicating that in this experiment, composition 11 has the best synergistic effect on inhibiting Propionibacterium acnes.
[0100] The above results also show that in the composition of Scutellaria baicalensis extract + Cnidium monnieri extract + Viola yedoensis extract + Magnolia officinalis extract + Paeonia lactiflora extract + Ophiopogon japonicus extract + Milk thistle extract + Gastrodia elata extract, a better synergistic effect can be achieved by controlling the ratio of each single extract within an appropriate range. If the ratio of each single extract exceeds a certain range, they will not have a synergistic effect or the synergistic effect will be weak.
[0101] Table 1 Inhibitory rate of each test extract and composition against Propionibacterium acnes (mean ± standard deviation)
[0102]
[0103] Test Example 2. In vitro inhibition of the inflammatory factor interleukin-1β (IL-1β) level in keratinocytes by a single extract and a combination
[0104] The single extract components and extract combinations were tested for their ability to inhibit the level of the inflammatory factor interleukin-1β (IL-1β) in keratinocytes in vitro.
[0105] Experimental method: Human keratinocytes (HaCaT cells) were collected during the logarithmic growth phase and the cell concentration was adjusted to 2×10 5 Cells were seeded at a density of 100 cells / well in a 24-well cell culture plate and cultured for 24 hours. After culture, the test samples shown in Table 2 below were added to each well to ensure the same final concentration at each dose (the sample preparation was the same as in Experimental Example 1, except that the BHI medium was replaced with DMEM medium). After 1 hour of pretreatment, 4×10 inactivated Propionibacterium acnes (C. acnes) were added to each well, except for the blank control group. 7 CFU / well, and each plant extract or extract combination was added to the test group. After culturing for 23 h, cells were collected and RNA was extracted for qPCR detection. -ΔΔCt The relative expression of IL-1β mRNA was calculated by the method.
[0106] in:
[0107] The blank control group consisted of DMEM medium + HaCaT cells without plant extracts and Propionibacterium acnes;
[0108] The model group consisted of DMEM medium + HaCaT cells + Propionibacterium acnes without plant extracts;
[0109] The experimental group consisted of DMEM medium + HaCaT cells + Propionibacterium acnes + various plant extracts;
[0110] Test results:
[0111] Depend on Figure 2 The results in Table 2 show that the extracts of Scutellaria baicalensis, Cnidium monnieri, Viola yedoensis, Magnolia officinalis and Paeonia lactiflora can inhibit the expression level of interleukin-1β (IL-1β mRNA) of keratinocytes induced by Propionibacterium acnes, indicating that these extracts have the effect of inhibiting the inflammatory response induced by Propionibacterium acnes, have the effect of resisting acne skin inflammation, and can further reduce the redness, swelling, inflammatory papules and skin damage caused by inflammation.
[0112] After combining the natural botanicals, it was found that the combination of Scutellaria baicalensis extract and Ophiopogon japonicus extract (Composition 3) did not significantly enhance the inhibitory effect (anti-inflammatory) on IL-1β mRNA expression compared to either Scutellaria baicalensis extract or Paeonia lactiflora extract alone. The combination of Paeonia lactiflora extract and Ophiopogon japonicus extract (Composition 5) did not significantly enhance the inhibitory effect (anti-inflammatory) on IL-1β mRNA expression compared to either Paeonia lactiflora extract or Ophiopogon japonicus extract alone. Furthermore, the combination of Scutellaria baicalensis extract, Ophiopogon japonicus extract, and Paeonia lactiflora extract (Composition 7) did not significantly enhance the inhibitory effect (anti-inflammatory) on IL-1β mRNA expression compared to either Scutellaria baicalensis extract, Ophiopogon japonicus extract, or Paeonia lactiflora extract alone. This suggests that Compositions 3, 5, and 7 do not exhibit synergistic anti-inflammatory effects.
[0113] In addition, the inhibitory (anti-inflammatory) effects of Scutellaria baicalensis extract + Cnidium monnieri extract + Viola yedoensis extract + Magnolia officinalis extract + Paeonia lactiflora extract + Ophiopogon japonicus extract + Milk thistle extract + Gastrodia elata extract (combinations 12, 13, and 14) on IL-1β mRNA expression were weaker than those of single Cnidium monnieri extract, Viola yedoensis extract, Scutellaria baicalensis extract, Milk thistle extract, and Magnolia officinalis extract, indicating that compositions 12, 13, and 14 did not exhibit synergistic anti-inflammatory effects.
[0114] The downregulation effect on IL-1β mRNA expression was as follows: Composition 11 > Composition 9 > Composition 4 > Composition 6 > Composition 2 > Composition 8 > Composition 1 > Composition 10. Scutellaria baicalensis extract + Viola yedoensis extract (Composition 2), Paeonia lactiflora extract + Viola yedoensis extract (Composition 4), Scutellaria baicalensis extract + Paeonia lactiflora extract + Viola yedoensis extract (Composition 6), and Scutellaria baicalensis extract + Cnidium monnieri extract + Viola yedoensis extract + Magnolia bark extract + Paeonia lactiflora extract + Ophiopogon japonicus extract + Milk thistle extract + Gastrodia elata extract (Compositions 9 and 11) significantly enhanced the downregulation effect on IL-1β mRNA expression, demonstrating a synergistic effect. Composition 10 showed enhanced or essentially equivalent effects compared to the individual extracts.
[0115] For the combination of "Scutellaria baicalensis, Cnidium monnieri, Viola yedoensis, Magnolia officinalis, Paeonia lactiflora, Ophiopogon japonicus, Silybum marianum, and Gastrodia elata extracts", the inhibitory effect on IL-1β mRNA expression (anti-inflammatory) is: "5:4:4:2:2:1:1:1" (Composition 11) > "4:3:3:2.5:2.5:1:3:1" (Composition 9) > "2:2:2:1:1:1:1:1" (Composition 10) > "1:5:4:1:1:1:6:1" (Composition 12) > "4:1:1:1:1:4:6:2" (Composition 13) > "4:1:1:3:3:4:2:2" (Composition 14), among which "5:4:4:2:2:1:1:1" (Composition 11) has the strongest synergistic anti-inflammatory effect.
[0116] The above results show that in the composition of Scutellaria baicalensis extract + Cnidium monnieri extract + Viola yedoensis extract + Magnolia officinalis extract + Paeonia lactiflora extract + Ophiopogon japonicus extract + Milk thistle extract + Gastrodia elata extract, by controlling the ratio of each individual extract within an appropriate range, a better synergistic effect can be achieved. If the ratio of each individual extract exceeds a certain range, they will not have a synergistic effect or the synergistic effect will be weak. This is similar to the results in Experimental Example 1.
[0117] Specifically, composition 11 exhibited the strongest synergistic effect in inhibiting IL-1β mRNA expression, demonstrating that, among the various compositions, composition 11, with a ratio of 5:4:4:2:2:1:1:1:1 (Scutellaria baicalensis extract: Cnidium monnieri extract: Viola yedoensis extract: Magnolia officinalis extract: Paeonia lactiflora extract: Ophiopogon japonicus extract: Silybum marianum extract: Gastrodia elata extract), exhibited the strongest synergistic effect. Composition 11 of the present invention exhibits the best synergistic effect in inhibiting the secretion of the inflammatory factor IL-1β by human HaCaT cells induced by Propionibacterium acnes, effectively alleviating whiteheads and blackheads in acne-prone skin and exhibiting a stronger therapeutic effect on acne symptoms such as redness, inflammatory papules, and skin lesions caused by inflammation.
[0118] Table 2 Effects of various extracts and compositions on the expression level of inflammatory factor IL-1β secreted by human HaCaT cells induced by Propionibacterium acnes (mean ± SD)
[0119]
[0120] Test Example 3. In vitro inhibition of keratinocyte barrier damage induced by the diffusion of inflammatory factors by the composition
[0121] In this test example, different plant extract compositions were compared in vitro to inhibit interleukin 1α (IL-1α) levels of keratinocyte barrier damage induced by the spread of inflammatory factors.
[0122] Acne is a common, complex, and multifactorial inflammatory skin disease associated with epidermal barrier dysfunction, with the hair follicle epithelial barrier being directly involved in changes during comedone formation and the inflammatory phase. While the absolute levels of IL-1α protein vary by cell type, barrier cells (such as endothelial and epithelial cells) consistently express this cytokine in high amounts. Cellular damage or infection can lead to the passive leakage of cytosolic IL-1α into the surrounding environment, where it activates inflammation in an interleukin receptor (IL-1RI)-dependent manner (Zouboulis CC, Eady A, Philpott M, Goldsmith LA, Orfanos C, Cunliffe WC, et al. What is the pathogenesis of acne? Experimental Dermatology. 2005;14:143). More severe barrier damage increases IL-1α release. In this study, HaCaT cells were induced with tumor necrosis factor α (TNF-α) and interferon γ (IFN-γ) for 18 h and then infected with LPS. ELISA detection showed that the IL-1α content in the supernatant was significantly increased.
[0123] Experimental method: HaCaT cells in the logarithmic growth phase were taken and 3.5×10 4 HaCaT cells were seeded at a density of 10 cells / well in a 24-well plate, with 0.5 mL of HaCaT cell suspension per well. After overnight culture, the cells were pretreated with the culture medium containing the test sample for 1 hour. TNF-α / IFN-γ (final concentration 20 ng / mL) were added to induce the HaCaT cells for 18 hours. Lipopolysaccharide (LPS) was then added (final concentration 10 μg / mL) and induction continued for 2 hours. The cell culture supernatant was collected and processed according to the kit instructions.
[0124] The preparation and concentration of each test sample were the same as those in Experimental Example 1, except that the BHI medium was replaced with DMEM medium.
[0125] Blank control group: only DMEM medium + HaCaT cells, without test samples, stimulating factors TNF-α / IFN-γ and LPS;
[0126] Model group (T / I+lps): DMEM medium + HaCaT cells + stimulating factors TNF-α / IFN-γ and LPS, without test samples;
[0127] Test wells: DMEM medium + HaCaT cells + stimulating factors TNF-α / IFN-γ and LPS + various test samples;
[0128] Depend on Figure 3The results in Table 3 show that each extract combination group inhibited the expression of IL-1α, a barrier-damaging factor in keratinocytes. This suggests that each extract combination has a certain effect in alleviating keratinocyte barrier damage induced by stimulatory factors (TNF-α / IFN-γ and LPS), and has a keratinocyte repair effect.
[0129] Among the compositions, Scutellaria baicalensis extract + Paeonia lactiflora extract (Composition 2), Paeonia lactiflora extract + Ophiopogon japonicus extract (Composition 5), Scutellaria baicalensis extract + Paeonia lactiflora extract + Viola yedoensis extract (Composition 6) and Scutellaria baicalensis extract + Cnidium monnieri extract + Viola yedoensis extract + Magnolia officinalis extract + Paeonia lactiflora extract + Ophiopogon japonicus extract + Milk thistle extract + Gastrodia elata extract (Compositions 9, 10 and 11) were more effective in reducing the barrier damage factor IL-1α than other composition groups.
[0130] Among them, the effect of reducing IL-1α, a factor that damages the keratinocyte barrier, is as follows: composition 9 > composition 5 > composition 11 > composition 6 > composition 2 > composition 10 > composition 1 > composition 7 > composition 3 > composition 8 > composition 12 > composition 14 > composition 13 > composition 4, indicating that composition 9 has the strongest ability to repair keratinocyte barrier damage.
[0131] The above results show that compared with other compositions, composition 9 (Scutellaria baicalensis extract: Cnidium monnieri extract: Viola yedoensis extract: Magnolia officinalis extract: Paeonia lactiflora extract: Ophiopogon japonicus extract: Milk thistle extract: Gastrodia elata extract = 4:3:3:2.5:2.5:1:3:1) has the strongest repairing effect on keratinocyte barrier damage.
[0132] Table 3 Effects of various extract compositions on the expression level of IL-1α in keratinocyte barrier damage induced by stimulatory factors (TNF-α / IFN-γ and LPS) (mean ± SD)
[0133]
[0134] Test Example 4. Transdermal Release Test of Compositions of Different Dosage Forms
[0135] Taking composition 11 as an example, osthole and silymarin were used as test substances to measure the transdermal release of different preparations of the composition.
[0136] Test method: Take the back skin of a 10-12 week old Bama Xiang pig, carefully shave the hair on the skin surface with a razor, and remove the subcutaneous fat layer to ensure uniform skin thickness, and then cut it into 25mm skin discs as release skin. With the skin surface facing up, fix it on the release tank, apply 0.3±0.05g of each preparation of composition 11 prepared in Example 2 on the skin of each release area, gently press the edge with a scraper to eliminate the gap between the preparation and the skin surface, and scrape the surface flat with a scraper before weighing. Add the release medium physiological saline to the receiving tank, stir at 32°C at a stirring speed of 600r / min; take samples at 2h, 4h, 6h, 8h, and 12h, and measure the concentration of the test substance in the medium.
[0137] Table 4 Transdermal release levels of different dosage forms of composition 11
[0138]
[0139] Test Conclusion: The results of the transdermal test indicate that, at the 12-hour test point, the transdermal release rates of the Composition 11 gel and Composition 11 emulsion were comparable, both exceeding those of the cream. Furthermore, the transdermal release rate of the Composition 11 gel was significantly higher than that of the emulsion and cream groups at 2, 4, and 6 hours, and gradually reached a release plateau at 8 and 12 hours, suggesting that the Composition 11 gel rapidly releases its active ingredient after application to the skin and is rapidly absorbed by the skin.
[0140] Experimental Example 5. Experimental study on the inhibitory effect of different dosage forms on acne symptoms in mice
[0141] In this test example, taking composition 11 as an example, the inhibitory effects of plant compositions in different dosage forms on acne symptoms in mice were compared.
[0142] Experimental Methods: Male BALB / c mice were randomly divided into six groups after hair removal: a normal control group, a model group, a Composition 11 cream group, a Composition 11 gel group, a Composition 11 emulsion group, and a positive control group (isotretinoin erythromycin gel). 50 μL of a P. acnes propionate suspension was injected intradermally on the left side of the depilated area on the back. Twenty-four hours later, another 50 μL of the same suspension was injected to establish the model. Following model establishment, 20 μL of sebum was applied daily to the injection site in both the experimental and positive control groups. Two hours after this application, 0.1 g of the drug was applied to the injection site.
[0143] The normal control group received no modeling treatment and no medication application. The model group received modeling but no application of Composition 11. The experimental groups (Composition 11 cream group, Composition 11 gel group, and Composition 11 emulsion group) received 0.1 g of each composition prepared in Example 2 applied once daily for six consecutive days. The positive control group (isotretinoin erythromycin gel) received 0.1 g of isotretinoin erythromycin gel applied once daily for six consecutive days. Acne symptoms and scores were observed on the backs of mice in each group.
[0144] Depend on Figure 4 、 Figure 5 The results in Table 5 show that each treatment group can effectively alleviate the symptoms and scores of the back skin of acne mice, among which the improvement effect on acne symptoms is: Composition 11 gel > Composition 11 emulsion > Composition 11 cream, and the effects of Composition 11 gel and Composition 11 emulsion are both better than the positive control group isotretinoin erythromycin gel.
[0145] Table 5 Scores of different formulations of Composition 11 on acne symptoms in mice (mean ± standard deviation)
[0146]
[0147] Test Example 6. Test on skin irritation of guinea pigs after single percutaneous administration of the composition
[0148] In this test example, taking Composition 11 as an example, a single percutaneous administration skin irritation test was conducted on guinea pigs to observe whether different formulations of the composition cause local skin irritation.
[0149] Test Methods: Prior to administration, the hair on the dorsal skin of each guinea pig was removed, covering an area of approximately 5 cm x 5 cm. A 3 cm x 3 cm area of the formulation was transdermally applied to the lateral dorsal skin of each guinea pig at a dose of 0.5 g per animal. The application area was covered with cellophane (approximately 4 cm x 4 cm) and gauze and secured with medical tape. Six hours after application, the dressing was removed, and any residual formulation on the skin of each group was cleaned with 0.9% sodium chloride injection. Skin irritation scores and irritation intensity were evaluated at 24, 48, and 72 hours, respectively, according to the scoring criteria shown in Table 6.
[0150] Among them, the normal control group: guinea pigs with normal hair removal without treatment; the cream group of Composition 11: applying the cream of Composition 11; the gel group of Composition 11: applying the gel of Composition 11; and the emulsion group of Composition 11: applying the emulsion of Composition 11.
[0151] Table 6 Scoring criteria for skin erythema and edema
[0152]
[0153] Table 7 Ratings of irritation to guinea pig skin by different formulations of Composition 11 (mean ± standard deviation)
[0154]
[0155] Depend on Figure 6 The results in Table 7 show that no erythema or edema was observed on the skin of the guinea pig's back where the drug was administered, and the scores were all 0, indicating that no irritation was observed in the different formulations of Composition 11.
Claims
1. A natural plant composition for treating acne, characterized in that: The natural plant composition comprises scutellaria baicalensis extract, cnidium monnieri extract, viola yedoensis extract, magnolia bark extract, peony root extract, ophiopogon japonicus extract, milk thistle extract and gastrodia elata extract.
2. The natural plant composition according to claim 1, characterized in that The natural plant composition comprises, by weight, 5-30% of scutellaria baicalensis extract, 5-25% of cnidium monnieri extract, 5-25% of viola yedoensis extract, 1-15% of magnolia bark extract, 1-15% of peony root extract, 1-20% of ophiopogon japonicus extract, 1-30% of milk thistle extract and 1-25% of gastrodia elata extract.
3. The natural plant composition according to claim 2, characterized in that The natural plant composition comprises, by weight, 10-25% of scutellaria baicalensis extract, 10-20% of cnidium monnieri extract, 10-20% of viola yedoensis extract, 5-12.5% of magnolia bark extract, 5-12.5% of peony root extract, 5-15% of ophiopogon japonicus extract, 5-25% of milk thistle extract and 5-20% of gastrodia elata extract.
4. The natural plant composition according to claim 2, characterized in that In the natural plant composition, the weight ratio of the scutellaria baicalensis extract, the cnidium monnieri extract, the viola yedoensis extract, the magnolia bark extract, the peony extract, the ophiopogon japonicus extract, the milk thistle extract and the gastrodia elata extract is 1.5~5.5: 1.5~4.5: 1.5~4.5: 1~2.5: 1~2.5: 1~1.5: 1~3.5:1~1.
5.
5. The natural plant composition according to claim 2, characterized in that The natural plant composition comprises, by weight, 25% of scutellaria baicalensis extract, 20% of cnidium monnieri extract, 20% of viola yedoensis extract, 10% of magnolia bark extract, 10% of peony extract, 5% of ophiopogon japonicus extract, 5% of milk thistle extract and 5% of gastrodia elata extract; or comprises 20% of scutellaria baicalensis extract, 15% of cnidium monnieri extract, 15% of viola yedoensis extract, 12.5% of magnolia bark extract, 12.5% of peony extract, 5% of ophiopogon japonicus extract, 15% of milk thistle extract and 5% of gastrodia elata extract; or comprises 10% of scutellaria baicalensis extract, 10% of cnidium monnieri extract, 10% of viola yedoensis extract, 5% of magnolia bark extract, 5% of peony extract, 15% of ophiopogon japonicus extract, 25% of milk thistle extract and 20% of gastrodia elata extract.
6. The natural plant composition according to any one of claims 1 to 5, characterized in that Each extract is a pharmacopoeial part of a selected medicinal material, which is extracted, separated, and purified after being crushed to obtain an extract solution. Wherein, the extraction method is selected from water extraction or solvent extraction, and the separation and purification process is a pharmaceutically acceptable membrane separation method.
7. The natural plant composition according to any one of claims 1 to 5, characterized in that The natural plant composition further comprises a pharmaceutically acceptable excipient, Wherein, the auxiliary material is selected from any one or a combination of at least two of moisturizers, thickeners, preservatives, emulsifiers and emollients.
8. Use of the natural plant composition according to any one of claims 1 to 7 in preparing a product for preventing, improving or treating acne.
9. A pharmaceutical preparation for preventing, improving or treating acne, characterized in that: The pharmaceutical preparation comprises the natural plant composition according to any one of claims 1 to 7.
10. The pharmaceutical preparation according to claim 9, characterized in that The dosage form of the pharmaceutical preparation is selected from any one of aqueous solution, gel, emulsion, cream and ointment.
11. A daily chemical product for preventing and improving acne, characterized in that: The daily chemical product comprises the natural plant composition according to any one of claims 1 to 7.
Citation Information
Patent Citations
Acne-removing composition particles based on natural plant extracts and preparation method thereof
CN119732879A
Composition for treating acne and preparation method thereof
CN120131728A
Cited By
TRPV1 inhibition type soothing and repairing plant composition based on silybum marianum extract and paeonia lactiflora extract and application of TRPV1 inhibition type soothing and repairing plant composition
CN121370703A
Composition for the care and treatment of atopic skin
PL453799A1
