Antidandruff compositions of natural origin

Abstract

The invention provides an anti-dandruff composition of a natural source. The anti-dandruff composition comprises 0.1-2 wt% of dihydroartemisinin; 0.1-2 wt% of a Coptis chinensis extract; and a carrier acceptable in the personal care field. The invention further relates to application of the composition in preparation of personal care products with an anti-dandruff effect. The personal care products are selected from anti-dandruff shampoo, anti-dandruff scalp care lotion, anti-dandruff scalp care essence and scalp care hair masks.

Description

TECHNICAL FIELD

[0001] The present application relates to the field of natural pharmaceutical chemistry and the field of cosmetics, in particular to a synergistically effective anti-dandruff composition of natural origin. BACKGROUND

[0002] Dandruff is one of the main problems of the head that consumers face today. Dandruff is a common problem in the daily life of consumers and is one of the main scalp health problems that needs to be solved urgently, and also has broad market potential.

[0003] Dandruff is the result of a disruption in the balance between epidermal cell shedding and cell regeneration, causing keratinocytes to accumulate into visible flakes. Under normal circumstances, the scalp keratin will naturally metabolize and periodically shed, which is generally invisible to the naked eye and can be solved by frequent shampooing. When the scalp micro-ecosystem is imbalanced, it can lead to a large number of lipophilic Malassezia to proliferate, which in turn can cause an imbalance in the secretion of scalp sebum, producing a large amount of unsaturated free fatty acids, stimulating the scalp and causing dandruff. In addition, when the scalp barrier function is imbalanced, it can lead to changes in the scalp pH, water content, etc., which in turn can cause a large number of Malassezia to proliferate, causing an imbalance in sebum secretion, leading to itching, dandruff, and other phenomena (Chen Dongzhi, Xu Mingli, Huo Yanli, Research Overview of Mild Anti-dandruff Agent Pyrithione Ethanolamine Salt [J], Daily Chemical Industry, 2021, 44(5): 40-44). Numerous studies have shown that abnormal proliferation of Malassezia is closely related to the occurrence and severity of dandruff (Wang Ran, Lai Wei, Zhang Yuqing, et al. Role of Malassezia Quantitative Culture Method in Evaluation of Anti-dandruff Effect [C], Third Symposium on Dermatology and Venereology in Central China, 2006: 245-247; Liu Di, Development of Plant-derived Anti-dandruff Agents and Mechanism of Inhibition of Malassezia [D], Guangdong: Guangdong University of Technology, 2020). Therefore, inhibiting Malassezia has become one of the main targets of daily-use anti-dandruff products.

[0004] At present, the common anti-dandruff agents on the market include ZPT (zinc pyrithione), climbazole, HP100 (hexamidine disulphate), Runanti HS (dipyrithione), salicylic acid, SL-900 (dodecenoyl amide MEA sulfosuccinate disodium), etc. However, salicylic acid has poor anti-dandruff effect and strong irritation, and is easy to cause damage to the scalp; zinc pyrithione has good antibacterial effect, but its toxicity and use safety cannot be ignored; climbazole has inhibitory effect on Malassezia ovale or Malassezia furfur, as well as Candida albicans and Trichophyton, but it is harmful to aquatic organisms and can pollute the aquatic environment. In November 2021, the European Commission officially issued Regulation (EU) 2021 / 1902, which listed the anti-dandruff agent zinc pyrithione (ZPT) in the banned list because it is a reproductive toxicity 1B GHS classification. The above anti-dandruff agents have the disadvantages of high toxicity, high concentration, poor solubility, or poor anti-dandruff effect, and have different degrees of limitations in the application of daily chemical products.

[0005] Therefore, it is of great practical significance and broad market application value to develop a new natural source of safe and effective anti-dandruff agent for inhibiting Malassezia.

[0006] Dihydroartemisinin (DHA) is an extremely important derivative of artemisinin. Compared with artemisinin, DHA has better water solubility, higher bioavailability and easier metabolism, which greatly improves its pharmaceutical value. According to research, DHA has good effect in the aspects of anti-malaria, anti-tumor, anti-virus, anti-inflammatory, anti-other parasites, anti-fibrosis, antihypertensive and immune regulation. Existing patent research shows that dihydroartemisinin has good inhibitory effect on Malassezia and can be used as a safe and efficient anti-dandruff ingredient of natural origin, which is worthy of further research and application.

[0007] Coptis chinensis Franch. is a perennial herb of Ranunculaceae. The New Revised Materia Medica recorded that “Coptis chinensis Franch. is a rough and large node, extremely bitter, and the best treatment for thirst, and the node is like a chain of pearls in Jiangdong, which is good for treating dysentery.” In traditional Chinese medicine, Coptis chinensis Franch. has the effects of clearing heat and drying dampness, purging fire and detoxifying, killing insects and stopping vomiting, and is often used in the treatment of high fever, mouth sores, burns, and other diseases caused by dampness and heat, cold and heat. Modern pharmacological studies have shown that Coptis chinensis Franch. has various pharmacological effects such as antiarrhythmic, hypoglycemic, anti-inflammatory, antitumor, antibacterial, neuroprotective, and antifibrotic effects. Modern pharmacological studies have confirmed that Coptis chinensis Franch. extract and its decoction have good antibacterial effect; Liu Mingzhu et al. found that Coptis chinensis Franch. water extract can cause Vibrio alginolyticus to release its contents by damaging its cell wall, leading to lysis and death, thereby exerting antibacterial effect. Zhou Fangfang et al. found that Coptis chinensis Franch. detoxification decoction has good antibacterial effect on gram-positive bacteria, and the antibacterial effect from high to low is Staphylococcus hemolyticus, Staphylococcus aureus, Enterococcus faecium, and Enterococcus faecalis. Wu Lingling et al. found that when imipenem is combined with berberine hydrochloride to treat carbapenem-resistant Pseudomonas aeruginosa, the minimum inhibitory concentration is reduced. Tan Lihua used agar dilution method to study the inhibitory effect of five alkaloids of Coptis chinensis Franch. on Helicobacter pylori, and found that the effect of coptisine is the best, followed by berberine, epiberberine, palmatine, and jatrorrhizine. TSENG et al. found that berberine can reduce the biofilm formation of Mycobacterium abscessus and reduce its antibacterial resistance to linezolid (Liu Xiaolong, Li Chunyan, Xiao Xian, et al. Research Progress of Main Active Ingredients and Pharmacological Effects of Coptis chinensis Franch. [J]. Journal of Xinxiang Medical College, 2023, 40(8): 784-790).

[0008] The application of Coptis chinensis Franch. in inhibiting Pityrosporum ovale has not been developed and studied. The inhibitory effect of different natural source components on Malassezia needs to be further studied.

[0009] Wei Qiang et al. found in the study “Dihydroartemisinin improves mouse psoriasis-like skin inflammation by inhibiting the proliferation of keratinocytes and the production of pro-inflammatory cytokines” (Chinese Journal of Immunology, 2020(5):543-548) that dihydroartemisinin can improve the inflammatory response of mice with psoriasis-like skin induced by imiquimod, and its possible mechanism is to inhibit the excessive proliferation of keratinocytes and the cytokines secreted by them through the MAPK / NF-κB signaling pathway.

[0010] Chinese patent CN109939105A discloses the use of artemisinin and its derivatives in the preparation of drugs and cosmetics for improving the barrier function of the skin stratum corneum and preventing and treating skin inflammation.

[0011] Chinese patent CN116019734A discloses the anti-dandruff application of dihydroartemisinin. The patent research found that dihydroartemisinin has obvious inhibition zone at 5mM and 10mM concentrations, and the inhibition zone of 10mM is larger than that of positive control OCT, indicating that dihydroartemisinin has good effect on inhibiting malassezia.

[0012] Chinese patent CN113975317A provides the application of coptis in preparing products for promoting the proliferation of intestinal beneficial bacteria. By simulating the intestinal environment in vitro and taking the intestinal flora collected from the feces of healthy human body as sample, it is found that coptis can significantly promote the proliferation of intestinal beneficial bacteria, especially the proliferation of intestinal beneficial bacteria such as bifidobacterium and arismontia. In addition, the patent also provides the application of coptis in preparing drugs for treating or improving diseases caused by intestinal flora imbalance.

[0013] Chinese patent CN106176960A discloses a natural antibacterial spray prepared by heating and mixing chitosan oligosaccharide, berberine, lauricazidone, comfrey extract, tea tree essential oil, anhydrous ethanol and distilled water. The spray contains no heavy metal ions, is non-toxic and harmless, has no skin irritation, and has obvious antibacterial effect. It can be used for antibacterial and deodorization of clothes and shoes.

[0014] However, so far, there is no report on the combination of dihydroartemisinin and coptis extract for inhibiting malassezia, and there is no precedent for the combination of dihydroartemisinin and coptis extract as an antidandruff agent in daily chemical products. SUMMARY

[0015] In one aspect, the present application provides a natural source antidandruff composition comprising:

[0016] 0.1-2% by weight of dihydroartemisinin;

[0017] 0.1-2% by weight of coptis extract; and

[0018] a carrier acceptable in personal care field.

[0019] In a preferred embodiment, the composition comprises 0.1-0.5% by weight of dihydroartemisinin.

[0020] In a preferred embodiment, the composition comprises 0.3-1% by weight of coptis extract.

[0021] In a preferred embodiment, the antidandruff effect is achieved by inhibiting malassezia, and the diameter of the inhibition zone is greater than 9mm.

[0022] In a preferred embodiment, the content of coptis extract and dihydroartemisinin excludes the following conditions:

[0023] (a) the content of both the Coptis extract and dihydroartemisinin is ≤ 0.1%, or

[0024] (b) the content of dihydroartemisinin is ≥ 0.8%.

[0025] In another aspect, the present application also relates to the use of the natural dandruff-removing composition in the preparation of a personal care product having a dandruff-removing effect.

[0026] In a preferred embodiment, the use concentration of the composition is 0.01-5% by weight.

[0027] In a preferred embodiment, the personal care product is selected from the group consisting of a dandruff-removing shampoo, a dandruff-removing scalp care lotion, a dandruff-removing scalp care serum, and a scalp care hair mask. DETAILED DESCRIPTION

[0028] The present application surprisingly found that the Coptis extract alone has no significant inhibitory effect on Pityrosporum ovale, but the combination of dihydroartemisinin and Coptis extract of natural origin has a synergistic effect on the inhibition of Pityrosporum ovale within a certain proportion range. The combination of the two not only achieves better inhibitory effect on Pityrosporum ovale than the traditional mild dandruff-removing agent-piroctone olamine (OCT), but also helps to improve the utilization efficiency of raw materials through synergistic effect, which can replace the traditional dandruff-removing agent in hair care products.

[0029] The purpose of the present application is to provide a natural dandruff-removing composition that is safe and efficient, which effectively inhibits the growth of Pityrosporum ovale through the synergistic effect of dihydroartemisinin and Coptis extract, and is applied to daily chemical hair care products to achieve the purpose of dandruff removal.

[0030] For the sake of providing a more concise description, some numerical expressions given herein are not modified by the term "about". It should be understood that each quantity given herein, whether or not explicitly modified by the term "about", is intended to refer to the actual given value, and is also intended to refer to the approximate value of the given value that can be reasonably inferred by a person of ordinary skill in the art, including the approximate value of the given value caused by experimental and / or measurement conditions.

[0031] For the sake of providing a more concise description, some numerical expressions given herein are described as a range of about X amount to about Y amount. It should be understood that when a range is described, the range is not limited to the recited upper and lower limits, but should include the entire range of about X amount to about Y amount or any amount therebetween.

[0032] Dihydroartemisinin

[0033] Dihydroartemisinin is an important derivative of artemisinin, which is reduced by sodium borohydride and other reducing agents using artemisinin from Artemisia annua L. as a precursor. Dihydroartemisinin has better antimalarial effect than artemisinin and is a new generation of antimalarial drug, and is widely used in the medical field. However, it is rarely used in the daily chemical field, especially as an anti-dandruff agent.

[0034] The specific structure of dihydroartemisinin is as follows:

[0035]

[0036] The composition of the present application uses dihydroartemisinin provided by the Institute of Chinese Materia Medica, Chinese Academy of Chinese Medical Sciences.

[0037] In some embodiments, the composition of the present application contains at least 0.1% by weight of dihydroartemisinin. In some embodiments, the composition of the present application contains 0.1-2% by weight of dihydroartemisinin, preferably 0.1-1% by weight, 0.1-0.5% by weight of dihydroartemisinin. In some embodiments, the composition of the present application contains 0.3-1% by weight of dihydroartemisinin.

[0038] Extract of coptis

[0039] Coptis is a perennial herbaceous plant of Ranunculaceae. In traditional Chinese medicine, Coptis has the effects of clearing heat and drying dampness, purging fire and detoxifying, killing insects and stopping vomiting, and is often used in the treatment of high fever, mouth sores, burns and other damp-heat and cold-heat diseases. Modern pharmacological studies have shown that Coptis has many pharmacological effects such as antiarrhythmic, hypoglycemic, anti-inflammatory, antitumor, antibacterial, neuroprotective and antifibrotic effects. Modern pharmacological studies have confirmed that Coptis extract and its decoction have good antibacterial effect. However, it is rarely used in the daily chemical field, especially as an anti-dandruff agent.

[0040] The composition of the present application uses Coptis extract provided by the Dalian Institute of Chemical Physics, Chinese Academy of Sciences.

[0041] In a preferred embodiment, the Coptis extract is prepared by solvent extraction method using water as the extraction solvent. In a preferred embodiment, the extraction process of Coptis extract is as follows: 50g of Coptis is extracted twice with 10-15 times of deionized water, filtered with filter paper, the filtrate is concentrated to 10 times the amount, purified, frozen at-60℃ for 24h to obtain Coptis extract.

[0042] In some embodiments, the composition of the present application comprises at least 0.1 wt% of the extract of Coptis chinensis. In some embodiments, the composition of the present application comprises 0.1-2 wt% of the extract of Coptis chinensis, preferably 0.1-1 wt%, 0.3-1 wt% of the extract of Coptis chinensis. In some embodiments, the composition of the present application comprises 0.5-1 wt% of the extract of Coptis chinensis.

[0043] Personal care product

[0044] The composition of dihydroartemisinin and the extract of Coptis chinensis has excellent inhibitory effect on Malassezia and can effectively remove dandruff. Therefore, the composition of dihydroartemisinin and the extract of Coptis chinensis can be used as an efficacy additive for preparing personal care products, especially hair products, to achieve the effect of removing dandruff.

[0045] The composition of the extract of Coptis chinensis and dihydroartemisinin has a good inhibitory effect on the growth of Pityrosporum ovale, and the components of the extract of Coptis chinensis and dihydroartemisinin have a synergistic effect on the inhibition of Malassezia within a certain ratio range.

[0046] The main purpose of the present application is to provide a safe and highly effective product of natural origin for inhibiting Malassezia, which has the effect of removing dandruff and can be used as a dandruff remover in daily-use products for the head, such as shampoo, hair conditioner, hair mask, etc.

[0047] In some embodiments, the composition of the present application can have a weight percentage of 0.0001%-20% (w / w) in the personal care product, preferably a weight percentage of 0.001%-10% (w / w), more preferably a weight percentage of 0.001%-5% (w / w), and most preferably a weight percentage of 0.01%-5% (w / w).

[0048] The personal care product can further include one or more optional ingredients, which include, but are not limited to, pearl or opal agents, thickening agents, auxiliary conditioning agents, humectants, chelating agents, and additives for improving the appearance, feel, and fragrance of the product, such as colorants, fragrances, preservatives, pH adjusting agents, etc. For example, the pH of the shampoo product is preferably maintained at about 5 to about 7.5, more preferably about 5.5 to about 7.0.

[0049] Commercially available pearlescent or opacifying agents that suspend water-insoluble additives such as silicones and / or that alert the user to the fact that the product is a conditioning shampoo are suitable for use in the present invention. The amount of pearlescent or opacifying agent used is from about 1% to about 10%, preferably from about 1.5% to about 7%, and more preferably from about 2% to about 5%, based on the total weight of the product. Examples of suitable pearlescent or opacifying agents include, but are not limited to, mono- or diesters of (a) fatty acids having from about 16 to about 22 carbon atoms and (b) ethylene glycol or propylene glycol; (a) fatty acids having from about 16 to about 22 carbon atoms and (b) the formula: HO-(JO) a -H, wherein J is an alkylene group having from about 2 to about 3 carbon atoms and a is 2 or 3; fatty alcohols containing from about 16 to about 22 carbon atoms; fatty acid esters of the formula: KCOOCH2L, wherein K and L each contain from about 15 to about 21 carbon atoms; inorganic solids insoluble in shampoo products, and mixtures thereof.

[0050] In a preferred embodiment, the pearlescent or opacifying agent is added to the shampoo product in the form of a preformed, stable aqueous dispersion, such as is commercially available from Henkel Corporation of Hoboken, New Jersey under the trade name "Euperlan PK-3000." This material is glycol distearate (a diester of ethylene glycol and stearic acid), laureth-4 (CH3 (CH2) 10 The weight percentages of the combination of CH2(OCH2CH2)4OH) and cocamidopropyl betaine are preferably about 25 to about 30: about 3 to about 15: about 20 to about 25, respectively.

[0051] Commercially available thickeners that provide a suitable viscosity for conditioning shampoo are suitable for use in the present invention. If a thickener is used, the amount of thickener in the shampoo product should be sufficient to increase the Brookfield viscosity of the product to about 500 to about 10,000 centipoise. Examples of suitable thickeners include, but are not limited to: 1) having the formula: HO-(CH2CH2O) zpolyethylene glycols and 2) mono- or diesters of fatty acids containing from about 16 to about 22 carbon atoms, wherein z is an integer from about 3 to about 200; ethoxylated polyol fatty acid esters; ethoxylated derivatives of mono- or diesters of fatty acids and glycerol; hydroxyalkylcelluloses; alkylcelluloses; hydroxyalkyl alkylcelluloses; and mixtures thereof. Preferred thickening agents include polyethylene glycol esters, more preferably PEG-150 distearate, which is commercially available from Stepan Company of Northfield, Illinois or from ComieI, S.p.A. of Bologna, Italy under the trade name "PEG 6000 DS".

[0052] Commercially available co-conditioners which impart other properties to the hair such as shine, such as volatile silicones, are suitable for use in the present application. If a volatile silicone conditioner is used, it preferably has a boiling point of less than about 220°C at atmospheric pressure. The amount of volatile silicone conditioner is from about 0% to about 3%, such as from about 0.25% to about 2.5% or from about 0.5% to about 1.0%, by weight of the total product. Examples of suitable volatile silicones include, but are not limited to, polydimethylsiloxanes, polydimethylcyclosiloxanes, hexamethyldisiloxane, cyclomethicone fluids such as polydimethylcyclosiloxane commercially available from Dow Corning Corporation of Midland, Michigan under the trade name "DC-345", and mixtures thereof.

[0053] Commercially available humectants which impart moisturization and conditioning properties to personal care products are suitable for use in the present application. The amount of humectant is from about 0% to about 10%, preferably from about 0.5% to about 5%, more preferably from about 0.5% to about 3%, by weight of the total product. Examples of suitable humectants include, but are not limited to: 1) water soluble liquid polyols selected from the group consisting of glycerin, propylene glycol, hexylene glycol, butylene glycol, dipropylene glycol, and mixtures thereof; 2) mono- or diesters of fatty acids containing from about 16 to about 22 carbon atoms, of the formula: HO-(R")O b - polyalkylene glycols of the formula: H-O-(R")O 10 O 5- (OCH2CH2) c - polyethylene glycol ethers of methyl glucoside of the formula: (OCH2CH2)

[0054] Examples of suitable chelating agents include those which are capable of protecting and preserving the products of the present application. The preferred chelating agent is EDTA, more preferably tetrasodium EDTA available from Dow Chemical Company of Midland, Michigan under the trade name "Versene 100XL", in an amount of from about 0% to about 0.5%, preferably from about 0.05% to about 0.25%, based on the total weight of the product.

[0055] Suitable preservatives include Quaternium-15 available from Dow Chemical Corporation of Midland, Michigan under the name "Dowicil 200", in an amount of from about 0% to about 0.2%, preferably from about 0.05% to about 0.10%, based on the total weight of the product.

[0056] Optionally, the personal care product can also contain from about 0.01% to about 1.0%, preferably from about 0.01% to about 0.5%, more preferably from about 0.01% to about 0.2%, based on total weight, of at least one conditioning agent. Examples of suitable cationic conditioning agents include, but are not limited to, cationic cellulose derivatives; cationic guar gum derivatives; diallyldimethylammonium chloride; and mixtures thereof.

[0057] The cationic cellulose derivative is preferably a polymeric quaternary ammonium salt resulting from the reaction of hydroxyethyl cellulose and trimethylammonium-substituted epoxide. The material known as Polyquaternium-10, which is commercially available from Amerchol Corporation of Edison, New Jersey as "Polymer JR-400", is particularly useful in this regard.

[0058] The cationic guar gum derivative is preferably guar hydroxypropyltrimonium chloride, which is commercially available from Rhodia of Cranbury, New Jersey under the trade name "Jaguar-17".

[0059] Other cationic conditioning polymers are those derived from the monomer diallyldimethylammonium chloride. The homopolymer of this monomer is Polyquaternium-6, which is commercially available from Allied Colloids of Suffolk, Virginia under the trade name "Salcare SC30". Copolymers of diallyldimethylammonium chloride and acrylamide are known as Polyquaternium-7, which is also available from Allied Colloids under the trade name "Salcare SC10".

[0060] In one embodiment, the conditioning agent portion comprises from about 0.01% to about 0.5%, such as from about 0.01% to about 0.2%, based on total product weight, of a cationic guar gum derivative and from about 0.01% to about 0.5%, such as from about 0.01% to about 0.2%, of a homopolymer or copolymer of diallyldimethylammonium chloride.

[0061] Examples

[0062] The application will be further described in conjunction with specific examples. It is necessary to point out here that the examples are only used to further illustrate the application and cannot be understood as a limitation to the scope of protection of the application. Those skilled in the art can make some non-essential improvements and adjustments according to the content of the application described above. The test methods in the following examples, for which no specific conditions are indicated, are usually carried out under conventional conditions or under the conditions recommended by the manufacturers. All percentages and parts are by weight unless otherwise indicated.

[0063] Dihydroartemisinin, purity > 90%, provided by Institute of Chinese Medicine, Chinese Academy of Medical Sciences;

[0064] Extract of Coptis, total alkaloids > 40%, provided by Dalian Institute of Chemical Physics, Chinese Academy of Sciences.

[0065] Test Example 1: Bacteriostatic circle experiment

[0066] Sample preparation :

[0067] Example 1: Take 0.3 g of dihydroartemisinin and 0.3 g of extract of Coptis, dissolve in 12% aqueous AES solution, and quantitate to 100 g.

[0068] Example 2: Take 0.5 g of dihydroartemisinin and 0.1 g of extract of Coptis, dissolve in 12% aqueous AES solution, and quantitate to 100 g.

[0069] Example 3: Take 0.5 g of dihydroartemisinin and 0.3 g of extract of Coptis, dissolve in 12% aqueous AES solution, and quantitate to 100 g.

[0070] Example 4: Take 0.5 g of dihydroartemisinin and 0.5 g of extract of Coptis, dissolve in 12% aqueous AES solution, and quantitate to 100 g.

[0071] Example 5: Take 0.8 g of dihydroartemisinin and 0.1 g of extract of Coptis, dissolve in 12% aqueous AES solution, and quantitate to 100 g.

[0072] Example 6: Take 0.8 g of dihydroartemisinin and 0.3 g of extract of Coptis, dissolve in 12% aqueous AES solution, and quantitate to 100 g.

[0073] Example 7: Take 0.8 g of dihydroartemisinin and 0.5 g of Coptis extract, dissolve in 12% AES aqueous solution, and quantitate to 100 g.

[0074] Example 8: Take 1 g of dihydroartemisinin and 0.1 g of Coptis extract, dissolve in 12% AES aqueous solution, and quantitate to 100 g.

[0075] Example 9: Take 1 g of dihydroartemisinin and 0.3 g of Coptis extract, dissolve in 12% AES aqueous solution, and quantitate to 100 g.

[0076] Example 10: Take 1 g of dihydroartemisinin and 0.5 g of Coptis extract, dissolve in 12% AES aqueous solution, and quantitate to 100 g.

[0077] Comparative Example 1: Take 0.1 g of Coptis extract, dissolve in 12% AES aqueous solution, and quantitate to 100 g.

[0078] Comparative Example 2: Take 0.3 g of Coptis extract, dissolve in 12% AES aqueous solution, and quantitate to 100 g.

[0079] Comparative Example 3: Take 0.5 g of Coptis extract, dissolve in 12% AES aqueous solution, and quantitate to 100 g.

[0080] Comparative Example 4: Take 0.8 g of Coptis extract, dissolve in 12% AES aqueous solution, and quantitate to 100 g.

[0081] Comparative Example 5: Take 1 g of Coptis extract, dissolve in 12% AES aqueous solution, and quantitate to 100 g.

[0082] Comparative Example 6: Take 0.1 g of dihydroartemisinin, dissolve in 12% AES aqueous solution, and quantitate to 100 g.

[0083] Comparative Example 7: Take 0.3 g of dihydroartemisinin, dissolve in 12% AES aqueous solution, and quantitate to 100 g.

[0084] Comparative Example 8: Take 0.5 g of dihydroartemisinin, dissolve in 12% AES aqueous solution, and quantitate to 100 g.

[0085] Comparative Example 9: Take 0.8 g of dihydroartemisinin, dissolve in 12% AES aqueous solution, and quantitate to 100 g.

[0086] Comparative Example 10: Take 1 g of dihydroartemisinin, dissolve in 12% AES aqueous solution, and quantitate to 100 g.

[0087] Comparative Example 11: Take 0.1 g of dihydroartemisinin and 0.1 g of Coptis extract, dissolve in 12% AES aqueous solution, and quantitate to 100 g.

[0088] Comparative Example 12: Take 0.8 g of dihydroartemisinin and 0.8 g of Coptis extract, dissolve in 12% AES aqueous solution, and quantitate to 100 g.

[0089] Comparative Example 13: Take 1 g of dihydroartemisinin and 1 g of Coptis extract, dissolve in 12% AES aqueous solution, and quantitate to 100 g.

[0090] Solvent Control 1 (deionized water): self-made in the laboratory, meeting the requirements of Grade 3 water specified in GB / T 6682.

[0091] Solvent Control 2 (12% AES aqueous solution): take 12 g of AES (trade name Texapon N70, supplier BASF), dissolve in deionized water, and quantitate to 100 g.

[0092] Positive Control 1: take 0.5 g of climbazole (trade name Crinipan AD, supplier symrise), dissolve in 12% AES aqueous solution, and quantitate to 100 g.

[0093] Positive Control 2: take 0.5 g of zinc pyrithione (trade name ZINC OMADINE 48% FPS, supplier Shanghai Pu'En Biochemical Technology Co., Ltd.), dissolve in 12% AES aqueous solution, and quantitate to 100 g.

[0094] Positive Control 3: take 0.5 g of piroctone olamine (trade name Octopirox, supplier Shanghai Shikele Chemical Technology Co., Ltd.), dissolve in 12% AES aqueous solution, and quantitate to 100 g.

[0095] Positive Control 4: take 1 g of piroctone olamine (trade name Octopirox, supplier Shanghai Shikele Chemical Technology Co., Ltd.), dissolve in 12% AES aqueous solution, and quantitate to 100 g.

[0096] Test procedure: oxford cup double layer plate method

[0097] Test strain: Malassezia furfur ATCC 44344 (Guangzhou Huayong Instrument Co., Ltd. Shanghai Branch).

[0098] The culture medium was self-made, with a ratio of 1% glucose, 1% proteose peptone, 0.2% yeast extract, 0.8% beef extract, 2% olive oil, 0.5% Tween 60, 1% glycerol, 0.05% glycerol monostearate, and 1.5% agar (all reagents were purchased from National Pharmaceutical Group Chemical Reagents), with the balance being water.

[0099] 1. Oxford cup double-layer plate preparation:

[0100] (1) Pour 10 ml of sterile culture medium heated and melted into a sterile culture dish, and let it stand until it solidifies.

[0101] (2) Put the sterilized Oxford cups vertically into the plate, and arrange them in order. The distance between the centers of the Oxford cups should be more than 25 mm, and the distance between the Oxford cups and the edge of the plate should be more than 15 mm. At least 3 or more Oxford cups should be placed on each plate (1 or more for the sample to be tested, 1 for the negative control with sterile saline, and 1 for the positive control with 0.5% OCT solution).

[0102] (3) Preparation of bacterial solution: rinse the bacterial slant with sterile saline solution, and place the rinse solution in a sterile test tube. Adjust the concentration of the bacterial solution to 10 7～8 CFU / ml.

[0103] (4) Take an appropriate amount of bacterial solution and add it to the sterile culture medium cooled to 50°C, and mix well to prepare a culture medium with a final concentration of 10 5 ~ 10 6 CFU / ml of indicator bacteria.

[0104] (5) Transfer 15 ml of the above bacterial solution-containing culture medium to a culture dish, and avoid air bubbles. After it is fully solidified, use sterile forceps to remove the Oxford cups.

[0105] 2. Sample addition: use a disposable pipette to take 100-200 ul of sample, and add it to the detection plate hole with sterile operation. Cover the plate and place it in a constant temperature incubator for 48 h.

[0106] 3. Measurement of inhibition zone diameter: remove each plate after incubation, measure the diameter of the inhibition zone (including the hole diameter), and record it.

[0107] 4. Determination of antibacterial effect:

[0108] (1) If the diameter of the inhibition zone is greater than 9 mm, it is determined to have antibacterial effect.

[0109] (2) The negative control group should have no inhibition ring, otherwise the experiment is invalid.

[0110] Test results:

[0111] Table 1: Inhibition zone data

[0112]

[0113]

[0114] Result analysis:

[0115] The bacteriostatic circle data of Comparative Examples 1, 3, 4, and 5 were equivalent to the solvent blank (12% AES), and the bacteriostatic circle of Comparative Example 2 was significantly higher than the solvent blank (equivalent to 12% AES), indicating that the Coptis extract had an inhibitory effect on Malassezia at an addition amount of 0.3%, and had no inhibitory effect at other concentrations.

[0116] The bacteriostatic circles of Comparative Examples 6-10 were significantly higher than the solvent blank (12% AES), and when the dihydroartemisinin content was ≥0.3%, the bacteriostatic circle was higher than the positive control group 0.5% OCT and 1% OCT, indicating that dihydroartemisinin had an inhibitory effect on Malassezia, and had a significant inhibitory effect on Malassezia when the content was ≥0.3%.

[0117] From the bacteriostatic circles of Example 1, Comparative Example 2, and Comparative Example 7, it can be seen that the bacteriostatic circle (24.98±0.50 mm) of the composition of 0.3% Coptis extract and 0.3% dihydroartemisinin was higher than the bacteriostatic circle (16.73±0.33 mm) of single 0.3% Coptis extract and the bacteriostatic circle (23.48±0.67 mm) of single 0.3% dihydroartemisinin, and was higher than the bacteriostatic circles of the positive controls 3 (0.5% OCT) and 4 (1% OCT), indicating that the composition of 0.3% Coptis extract and 0.3% dihydroartemisinin had a significant inhibitory effect on Malassezia, and the two had a synergistic effect.

[0118] From the bacteriostatic circles of Example 2, Comparative Example 3, and Comparative Example 6, it can be seen that the bacteriostatic circle (20.50±0.61 mm) of the composition of 0.5% Coptis extract and 0.1% dihydroartemisinin was higher than the bacteriostatic circle (10.66+0.60 mm) of single 0.5% Coptis extract and the bacteriostatic circle (17.81±0.37 mm) of single 0.1% dihydroartemisinin, indicating that 0.5% Coptis extract and 0.1% dihydroartemisinin had a synergistic inhibitory effect on Malassezia.

[0119] From the bacteriostatic circles of Example 3, Comparative Example 3, and Comparative Example 7, it can be seen that the bacteriostatic circle (25.05±0.32 mm) of the composition of 0.5% Coptis extract and 0.3% dihydroartemisinin was higher than the bacteriostatic circle (10.66+0.60 mm) of single 0.5% Coptis extract and the bacteriostatic circle (23.48±0.67 mm) of single 0.3% dihydroartemisinin, and was higher than the bacteriostatic circle of the positive control 3 (0.5% OCT), indicating that the composition of 0.5% Coptis extract and 0.3% dihydroartemisinin had a significant inhibitory effect on Malassezia, and the two had a synergistic effect.

[0120] From the inhibition zone of Example 4, Comparative Example 3, Comparative Example 8, it can be seen that the inhibition zone of the combination of 0.5% of the extract of Coptis and 0.5% of dihydroartemisinin (28.55±0.68mm) is higher than that of 0.5% of the extract of Coptis alone (10.66+0.60mm) and 0.5% of dihydroartemisinin alone (26.61±0.12mm), and higher than that of the positive control 3 (0.5% OCT) and the positive control 4 (1% OCT), indicating that the combination of 0.5% of the extract of Coptis and 0.5% of dihydroartemisinin has a significant inhibitory effect on Malassezia and the two have a synergistic effect.

[0121] From the inhibition zone of Example 5, Comparative Example 4, Comparative Example 6, it can be seen that the inhibition zone of the combination of 0.8% of the extract of Coptis and 0.1% of dihydroartemisinin (19.99±0.17mm) is higher than that of 0.8% of the extract of Coptis alone (11.71±0.27mm) and 0.1% of dihydroartemisinin alone (17.81±0.37mm), indicating that the combination of 0.8% of the extract of Coptis and 0.1% of dihydroartemisinin has a synergistic effect on the inhibition of Malassezia.

[0122] From the inhibition zone of Example 6, Comparative Example 4, Comparative Example 7, it can be seen that the inhibition zone of the combination of 0.8% of the extract of Coptis and 0.3% of dihydroartemisinin (25.47±0.25mm) is higher than that of 0.8% of the extract of Coptis alone (11.71±0.27mm) and 0.3% of dihydroartemisinin alone (23.48±0.67mm), and higher than that of the positive control 3 (0.5% OCT) and the positive control 4 (1% OCT), indicating that the combination of 0.8% of the extract of Coptis and 0.3% of dihydroartemisinin has a significant inhibitory effect on Malassezia and the two have a synergistic effect.

[0123] From the inhibition zone of Example 7, Comparative Example 4, Comparative Example 8, it can be seen that the inhibition zone of the combination of 0.8% of the extract of Coptis and 0.5% of dihydroartemisinin (28.65±0.30mm) is higher than that of 0.8% of the extract of Coptis alone (11.71±0.27mm) and 0.5% of dihydroartemisinin alone (26.61±0.12mm), and higher than that of the positive control 3 (0.5% OCT) and the positive control 4 (1% OCT), indicating that the combination of 0.8% of the extract of Coptis and 0.5% of dihydroartemisinin has a significant inhibitory effect on Malassezia and the two have a synergistic effect.

[0124] From the inhibition zone of Example 8, Comparative Example 5, Comparative Example 6, it can be seen that the inhibition zone of the combination of 1% of the extract of Coptis and 0.1% of dihydroartemisinin (18.32±0.81mm) is higher than that of 1% of the extract of Coptis alone (13.37±0.51mm) and that of 0.1% of dihydroartemisinin alone (17.81±0.37mm), indicating that the combination of 1% of the extract of Coptis and 0.1% of dihydroartemisinin has a synergistic effect on the inhibition of Malassezia.

[0125] From the inhibition zone of Example 9, Comparative Example 5, Comparative Example 7, it can be seen that the inhibition zone of the combination of 1% of the extract of Coptis and 0.3% of dihydroartemisinin (26.98±0.50mm) is higher than that of 1% of the extract of Coptis alone (13.37±0.51mm) and that of 0.3% of dihydroartemisinin alone (23.48±0.67mm), and is higher than that of the positive control 3 (0.5% OCT) and the positive control 4 (1% OCT), indicating that the combination of 1% of the extract of Coptis and 0.3% of dihydroartemisinin has a significant inhibitory effect on Malassezia, and the two have a synergistic effect.

[0126] From the inhibition zone of Example 10, Comparative Example 5, Comparative Example 8, it can be seen that the inhibition zone of the combination of 1% of the extract of Coptis and 0.5% of dihydroartemisinin (28.51±0.31mm) is higher than that of 1% of the extract of Coptis alone (13.37±0.51mm) and that of 0.5% of dihydroartemisinin alone (26.61±0.12mm), and is higher than that of the positive control 3 (0.5% OCT) and the positive control 4 (1% OCT), indicating that the combination of 1% of the extract of Coptis and 0.5% of dihydroartemisinin has a significant inhibitory effect on Malassezia, and the two have a synergistic effect.

[0127] From the inhibition zone of Comparative Example 11, Comparative Example 1, Comparative Example 6, it can be seen that the inhibition zone of the combination of 0.1% of the extract of Coptis and 0.1% of dihydroartemisinin (15.88±0.48mm) is lower than that of 0.1% of dihydroartemisinin alone (17.81±0.37mm), indicating that the combination of 0.1% of the extract of Coptis and 0.1% of dihydroartemisinin has no synergistic effect on the inhibition of Malassezia.

[0128] From the inhibition zone of Comparative Example 12, Comparative Example 4, Comparative Example 9, it can be seen that the inhibition zone (28.81±0.24mm) of the composition of 0.8% of the extract of Coptis and 0.8% of dihydroartemisinin is higher than the positive control 0.5% OCT, 1% OCT, but lower than the inhibition zone (31.81±0.23mm) of single 0.8% of dihydroartemisinin, which shows that 0.8% of the extract of Coptis and 0.8% of dihydroartemisinin have no synergistic effect on the inhibition of Malassezia, but the composition still has a good inhibitory effect on Malassezia.

[0129] From the inhibition zone of Comparative Example 13, Comparative Example 5, Comparative Example 10, it can be seen that the inhibition zone (28.65±0.51mm) of the composition of 1% of the extract of Coptis and 1% of dihydroartemisinin is higher than the positive control 0.5% COT, 1% OCT, but lower than the inhibition zone (31.00±0.38mm) of single 1% of dihydroartemisinin, which shows that 1% of the extract of Coptis and 1% of dihydroartemisinin have no synergistic effect on the inhibition of Malassezia, but the composition still has a good inhibitory effect on Malassezia.

[0130] In summary, from Example 1-10, it can be seen that when the content of the extract of Coptis is 0.3%-1% and the content of dihydroartemisinin is 0.1%-0.5%, the composition of the two has a synergistic effect on the inhibition of Malassezia. From Comparative Example 11-13, it can be seen that when the content of the extract of Coptis and dihydroartemisinin is ≤0.1%, or the content of dihydroartemisinin is ≥0.8%, the inhibitory effect of the composition of the two on Malassezia is lower than that of single dihydroartemisinin, which shows that at this content, the two have no synergistic effect on the inhibition of Malassezia. Comparative Example 12, 13 shows that when the content of dihydroartemisinin is ≥0.8%, it does not show synergy with the extract of Coptis on the inhibition of Malassezia, but the inhibition zone is still higher than the positive control group 0.5% OCT, 1% OCT, and still has certain research value.

Claims

1. A natural origin anti-dandruff composition comprising: 0.1-2 wt.% of dihydroartemisinin; 0.1-2 wt.% of a Coptis extract; and a carrier acceptable in the personal care field.

2. The composition of claim 1, wherein, The composition comprises 0.1-0.5 wt.% of dihydroartemisinin.

3. The composition of claim 1, wherein, The composition comprises 0.3-1 wt.% of the Coptis extract.

4. The composition of claim 1, wherein, The anti-dandruff effect is achieved by inhibiting Malassezia, with a zone of inhibition diameter greater than 9 mm.

5. The composition of claim 1, wherein, The content of the Coptis extract and dihydroartemisinin is such that: (a) both the Coptis extract and dihydroartemisinin are present in an amount of < 0.1%, or (b) dihydroartemisinin is present in an amount of > 0.8%.

6. Use of a composition according to any one of claims 1-5 for the manufacture of a personal care product having an anti-dandruff effect.

7. Use according to claim 6, wherein The composition is used at a concentration of 0.01-5 wt.%.

8. The use according to claim 6, wherein: The anti-dandruff effect is achieved by inhibiting Malassezia, with a zone of inhibition diameter greater than 9 mm.

9. The use of claim 6, wherein, The personal care product is selected from the group consisting of: anti-dandruff shampoos, anti-dandruff scalp care lotions, anti-dandruff scalp care serums, scalp care hair masks.

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