WO2016033899A1

WO2016033899A1 - Dandruff removing composition for adjusting scalp oil balance

Info

Publication number: WO2016033899A1
Application number: PCT/CN2014/093562
Authority: WO
Inventors: 赵文忠; 洪盛杰; 谷志静; 胡卫华; 董志扬
Original assignee: 拉芳家化股份有限公司
Priority date: 2014-09-05
Filing date: 2014-12-11
Publication date: 2016-03-10
Also published as: CN104287982B; CN104287982A

Abstract

A dandruff removing composition, comprising a cosmetically acceptable carrier, a scalp barrier protection agent and a scalp sebum adjusting agent; the scalp barrier protection agent comprises 0.001 wt% to 1.0 wt% of N-palmitoylethanolamine, 0.01 wt% to 20 wt% of N-acetylethanolamine and 0.01 wt% to 2 wt% of tetrahydropyrimidine or hydroxytetrahydropyrimidine, a weight ratio of the N-palmitoylethanolamine and the N-acetylethanolamine being 1:100. The scalp sebum adjusting agent comprises 0.1 wt% to 15 wt% of trimethylglycine salicylate and 0.05 wt% to 3 wt% of vitamin B₁₂.

Description

Anti-dandruff composition for regulating balance of scalp oil

Technical field

The invention belongs to the field of daily chemistry, and in particular relates to a composition for regulating dander by balancing sebaceous sebaceum.

Background technique

The dandruff is born on the scalp and is a large amount of desquamation caused by excessive proliferation of scalp keratinocytes. About 60% of adults in China suffer from dandruff problems to varying degrees, and 15% of them are very serious. At present, although the personal care products claimed by the anti-dandruff function are endless, 70% of the people who use the anti-dandruff products think that the effect is not satisfactory.

The pathogenesis of dandruff has not yet been clarified. There are several theories about the cause of dandruff, the most important of which is the mechanism of action of Malassezia. Numerous studies have shown that Malassezia is closely related to the occurrence and severity of dandruff. The proliferation of Malassezia on the scalp causes excessive proliferation of the stratum corneum of the scalp, which causes the stratum corneum cells to fall off in the form of white or gray scales. This shedding scaly is dandruff.

Malassezia belongs to the yeast single-cell fungus and survives by consuming fatty acids in sebum. It is lipid-dependent and easily grows on sebum-rich skin. The mechanism of action of Malassezia in the etiology of dandruff: Malassezia on the scalp breaks down triglycerides in sebum by releasing lipase, triggering the hydrolysis of triglycerides, which produces unsaturated fatty acids, which destroy The scalp barrier, the stratum corneum, causes the infiltration of unsaturated fatty acids into the epidermis, stimulating the skin to produce an inflammatory response. The result of an inflammatory reaction caused by Malassezia is the excessive proliferation of scalp cells in the scalp, usually accompanied by abnormalities in the scalp ultrastructure. Occurrence includes incomplete keratinization, abnormal keratinous membrane, lipids contained in scalp cells and between cells.

From the classification and mechanism of action of dandruff agents, there are three main types: one is the stratum corneum exfoliating agent, the cytostatic agent and the antimicrobial preparation. The stratum corneum stripping agent removes damaged epidermal cells from the stratum corneum by desquamation to achieve dandruff removal. Early anti-dandruff agents, such as salicylic acid, sulfur, and shampoos containing coal tar, fall into this category. However, the odor of such products is poor and irritating, and its effect is not superior to other dandruff products, and long-term application will also destroy the epidermal structure to disturb the balance of the epidermis, which has certain damage to the skin. Long-term use may result in Skin allergies and itching; Second, cell growth inhibitors, mainly by inhibiting cell replication, its activity depends on its reduction of stratum corneum cell turnover rate, with the recovery of cell regeneration cycle length, normal physiological processes of keratinization and desquamation Also improved, selenium disulfide belongs to this category. Most cytostatics have a certain anti-microbial activity. Generally speaking, people with more dandruff caused by oily scalp can use it, but many clinical experiments show that these drugs do not control dandruff well. Clinical symptoms, and its main ingredients are irritating. After use, the hair feels rough. If the washing is not thorough, the hair may be discolored, a small number of users will increase hair loss, and there are also problems such as odor; the third type is anti- Microbial preparations achieve the purpose of inhibiting dandruff by inhibiting or destroying the formation of microbial entities, and their anti-dandruff action depends on the number of Malassezia that can reduce or control the scalp. With the gradual clarification of the pathogenic mechanism of Malassezia, antimicrobial preparations have been widely used in anti-dandruff products. At present, ketoconazole, clomiprazole and pyrithione in shampoos for dandruff in pharmacies or supermarkets are all antimicrobial agents. Shampoos containing ketoconazole and clomiprazole are mostly sold in hospitals and pharmacies, such as shampoos such as Picker. Anti-dandruff products containing Zinconazole ZPT are widely sold in shopping malls and barbershops, such as Head & Shoulders, Avon and other anti-dandruff shampoos, but also have poor solubility and strong degreasing ability.

The current mainstream products on the market are the number of Malassezia that inhibits the growth of microorganisms. To achieve the purpose of anti-dandruff, the overall anti-dandruff effect is also good, but the only drawback is that the main anti-dandruff agent of anti-microbial effect, such as Zinconazole zinc ZPT, has a relatively strong degreasing property, while killing Malassezia The scalp keratin barrier function is destroyed to varying degrees (see US patent PAT.NO.5053222. The lack of scalp keratin barrier function is easy to stimulate and lead to imbalance of scalp oil secretion, resulting in the invasion of various bacteria and fungi, all of which will make The whims of dandruff and itchy itch are not easy to solve.

In addition, studies have reported that on healthy scalp, Malassezia and humans have nothing to worry about, so the susceptibility of the scalp and the amount of scalp oil secretion will remain relatively balanced. Normally exfoliated keratinocytes are sporadic and transparent, and the naked eye cannot aware. Once this balance is broken, Malassezia will multiply abnormally, causing the epidermal metabolism to accelerate, and the epidermal cells will fall off in large groups. In turn, repeated episodes of dandruff severely damage the scalp cell layer, and the thinned scalp cell layer loses its barrier function, making the dandruff phenomenon recurrent and difficult to resolve. Therefore, the problem of dandruff is the focus of the present invention from the improvement of scalp sebum balance and the establishment of an improved scalp barrier function.

Summary of the invention

It is an object of the present invention to provide an anti-dandruff composition which modulates sebum balance in the scalp. The composition of the present invention is composed of a scalp sebum regulator and a scalp barrier protectant, and restores and enhances the barrier function of the scalp by the action of both to reduce the effect of dandruff.

The object of the invention is achieved by the following techniques:

An anti-dandruff composition comprising, in addition to a cosmetically acceptable carrier, a scalp barrier protectant and a scalp sebum regulating agent, the components and contents of which are as follows:

(1) Skin barrier protectant:

Between 0.001% and 1.0% by weight of the composition of N-palmitoylethanolamine and 100% by weight of the composition a composition of 0.01%-20% N-acetylethanolamine, and the weight ratio of the two is 1:100;

a content of 0.01% to 2% by weight of the composition of tetrahydropyrimidine or hydroxytetrahydropyrimidine;

(2) scalp sebum regulator:

By weight of the composition is from 0.1% to 15% of trimethylglycine and salicylate of the composition by weight of 0.05% to 3% of vitamin B _12.

The anti-dandruff composition of the present invention wherein the N-palmitoylethanolamine content is optimized to be from 0.005% to 0.5% by weight of the composition; and the N-acetylethanolamine is from 0.05% to 10% by weight of the composition. And the weight ratio of N-palmitoylethanolamine and N-palmitoylethanolamine was further optimized to 1:50.

Anti-dandruff compositions of the present invention, wherein the content of trimethylglycine salicylate optimization of the composition by weight of 0.2% to 8%; vitamin B ₁₂ weight percent of the composition is 0.1% -2%.

The skin barrier protectant in the anti-dandruff composition of the present invention is preferably hydroxytetrahydropyrimidine in an amount of from 0.05% to 1% by weight based on the total weight of the composition.

The anti-dandruff composition of the present invention further comprises from 0.05% to 0.5% by weight of the composition of allantoin and 5% by weight of the composition. Wherein the allantoin content is optimized to be from 0.08% to 0.2% by weight of the composition.

An anti-dandruff composition having a composition and content of:

% by weight of the composition of 0.015% by weight of N-palmitoylethanolamine,

N-acetylethanolamine in an amount of 0.625% by weight of the composition,

3% by weight of the composition of hydroxytetrahydropyrimidine,

3% by weight of the composition of trimethylglycine salicylate,

1% by weight of the composition of vitamin B ₁₂ ,

0.1% by weight of the composition of allantoin,

5% by weight of the composition of glycerin,

0.1% by weight of the composition of xanthan gum,

0.05% by weight of the composition of disodium edetate,

Appropriate amount of preservatives, flavors and pigments. The balance is deionized water and the pH is adjusted to 7.

Advantageous Effects of Invention: The anti-dandruff composition of the present invention adopts a method of non-traditional inhibition and killing of Malassezia, and achieves synergy between scalp sebum regulation and scalp barrier protection, and the synergistic cooperation between the two can help the scalp The normal thickness of the water-lipid membrane is restored, and the scalp lipid dynamic balance is established, and the scalp barrier function is restored to reduce the dandruff. The anti-dandruff technique of the present invention can be applied to hair dandruff conditioner, anti-dandruff shampoo, etc., and the anti-dandruff composition of the present invention only explains the advantage of the anti-dandruff of the present invention in the form of a lotion formulation.

detailed description

The invention will now be described in detail in connection with the embodiments.

Usually we divide dandruff into oily dandruff and dry dandruff. Oily dandruff is dandruff produced by oily hair. It is large in block shape and easily adheres to the scalp and hair. It is less likely to fall off the shoulder and the color is partial. yellow. Oily dandruff is caused by excess oil irritating the scalp and inducing excessive reproduction of harmful bacteria (such as Maize), thereby destroying the balance of the scalp, causing abnormal metabolism of the scalp and causing the increase of dead skin, resulting in a large amount of dandruff. Produced, this is what we usually call oily dandruff; dry dandruff dry hair produces dandruff, small and many pieces, easy to fall off the shoulder, the color is white, which is due to insufficient secretion of scalp oil. The barrier function of the scalp is lost, the metabolism of the scalp is abnormal, and the dead skin is lost. Therefore, a large amount of dandruff, which is commonly referred to as dry dandruff, occurs.

The scalp oil has the function of protecting the scalp barrier, moisturizing and protecting the scalp and hair. Too much can not be done, so it is very important to find an effective way to regulate the scalp sebum.

The effect of the scalp sebum regulation of the present invention is to establish a balance between the oil and the dryness of the scalp. Over-tempering and removing scalp lipids while preventing excessive keratinization or shedding of the scalp, the previous regulation of scalp oil is through exfoliation of the stratum corneum and exfoliation of the stratum corneum by removing the damaged epidermal cells in the stratum corneum by desquamation. And to achieve the effect of removing dandruff. Early anti-dandruff agents, such as salicylic acid, sulfur, and shampoos containing coal tar, fall into this category. However, the odor of such products is poor and irritating, and its effect is not superior to other dandruff products, and long-term application will also destroy the epidermal structure to disturb the balance of the epidermis, which has certain damage to the skin. Long-term use may result in Skin allergies and itching; Second, through cell growth inhibitors, the previous use of selenium disulfide, mainly by inhibiting scalp caused by oily scalp, can be used, but many clinical experiments show that these drugs are not very good Controls the clinical symptoms of dandruff, and its main component, selenium disulfide, is highly irritating. After use, the hair feels rough. If the washing is not thorough, the hair may be discolored, a small number of users will increase hair loss, and there are also problems such as odor. .

The invention has undergone a large number of experiments, and the synergistic action of the scalp sebum regulator and the scalp barrier protectant acts to reduce and inhibit dandruff. The scalp sebum regulator of the present invention uses a derivative of salicylic acid and vitamin B. The substance, salicylic acid derivative is trimethylglycine salicylate, which can gently balance scalp sebum, vitamin B is made of vitamin B ₁₂ , vitamin B ₁₂ can well nourish the scalp and inhibit excessive scalp. The combination of a salicylic acid derivative and vitamin B plays a key role in regulating the sebum of the scalp.

The invention has found through a large number of experiments that the scalp barrier protection effect can be achieved by the endogenous lipid component of the skin and the extreme halophilic solute. The endogenous lipid components in the skin include N-palmitoylethanolamine and N-acetylethanolamine, and the extreme halophilic solute is tetrahydropyrimidine and a derivative of tetrahydropyrimidine, hydroxytetrahydropyrimidine, which restores and enhances the scalp barrier function.

The invention is based on the joint efforts of Lafang Jiahua Co., Ltd., the Institute of Microbiology of the Chinese Academy of Sciences and BASF of Germany, to study the problem of dandruff from the relationship between scalp health, scalp microenvironment and dandruff, and the present invention is more specific to the study. The relationship between scalp stratum corneum dysfunction and dandruff Dander to find new solutions. Different from the technical means of removing dandruff in the past, the present invention starts from the root of dandruff, that is, the scalp, and restores and strengthens the function of the scalp stratum corneum barrier, so that the scalp can effectively resist the invasion of bacteria and fungi, thereby further preventing and reducing. The production of dandruff.

The anti-dandruff composition of the present invention achieves the effect of inhibiting and reducing dandruff by regulating the balance of scalp sebum and enhancing the function of the scalp barrier.

The anti-dandruff composition contains, in addition to a cosmetically acceptable carrier, the active ingredients as follows:

(1) The scalp barrier protectant consists of the endogenous lipid component of the skin and the halophilic solute of the extreme:

The endogenous lipid component of the skin is 0.001%-1.0% by weight of the composition of N-palmitoylethanolamine and 0.01%-20% by weight of the composition of N-acetylethanolamine, and the weight ratio of the two is 1 :100; the extreme halophilic solute is one of tetrahydropyrimidine and hydroxytetrahydropyrimidine,

(2) to the scalp sebum modulators of the composition by weight 0.1% to 15% of trimethylglycine and salicylate of the composition by weight of 0.05% to 3% of vitamin B _12.

Scalp barrier protectant

Endogenous lipid components of the skin:

The scalp barrier protective agent in the anti-dandruff composition of the present invention is composed of an endogenous lipid component of the skin and an extremely halophilic solute: wherein the skin endogenous lipids include N-palmitoylethanolamine and N-acetylethanolamine.

In the present invention, N-palmitoylethanolamine has a molecular formula of C ₁₈ H ₃₇ NO ₂ , a molecular weight of 299.49 g mol ^{-1 and a} melting point of 59 to 60 ° C (138 to 140 ° F; 332 to 333 K).

Chemical Structure:

In the present invention, N-acetylethanolamine has the formula: CH ₃ -CO-NH-C ₂ H ₄ OH, the substance is a viscous liquid at room temperature, density (DIN/20 degrees Celsius) 1.12, molecular weight 103, boiling point 155 degrees Celsius (5mmHg), density 1.052g/cm ³ .

Chemical Structure:

According to the literature report Chao Yuan, Xue-Min Wang, Cl inical Interventions in Aging 2014: 91163-1169. "Application of N-palmitoylethanolamine and N-acetylethanolamine in the treatment of defolitic dermatitis" Shanghai Skin and Cosmetics Department, Department of Skin and Cosmetics, It is a skin-derived fatty acid amide originally used for anti-allergic use of the skin.

In the present invention, as a scalp barrier protectant, the skin endogenous lipid component is further optimized to be 0.005%-0.5% by weight of the composition of N-palmitoylethanolamine and 0.05%-10% by weight of the composition. N-acetylethanolamine.

The weight ratio of N-palmitoylethanolamine and N-palmitoylethanolamine in the present invention is further optimized to be 1:50. Scalp barrier protectant

Extreme halophilic solute:

The moisturizing factor in human skin, including lactic acid, sodium lactate, hyaluronic acid, urea, amino acid, lecithin, etc., is an indispensable physiological function moisturizing factor in human skin. The invention relates to a moisturizing agent extracted from a high salt-tolerant and high-cold microorganism (extreme halophilic bacteria) in an extreme environment.

On Earth, the environment outside the biosphere where humans live is called the extreme environment, which means that the physical and chemical conditions reach or exceed the life tolerance range. Microorganisms that can grow in extreme environments are called extreme microorganisms such as halophilic microorganisms. Hot microorganisms, psychrophilic microorganisms have been acidophilic microorganisms, etc. It is worth noting that these extreme microorganisms not only "tolerate" these extreme environments, but also require one or more extreme conditions for better growth and reproduction, among which moderate Halophilic microorganisms are one of them.

The present invention is applied to a microorganism that grows in an extreme environment, that is, a high salt and alpine environment. Solute-tetrahydropyrimidine and its derivative hydroxytetrahydropyrimidine (Ph.D., 2005.11.16 Zhao Baisuo) tetrahydropyrimidine and hydroxytetrahydropyrimidine as stabilizers extracted from the genus Salicorella and C. It protects microorganisms from enzymes, DNA and macromolecules. It acts against microbes in extreme environments, resists high salt, resists drying, freezes and prevents heat denaturation. It is a molecular chaperone and protection for extreme microorganisms to survive in extreme environments. God. The application of tetrahydropyrimidine and hydroxytetrahydropyrimidine in cosmetics has also received more and more attention. It was developed by Merck and the Institute of Microbiology of the Chinese Academy of Sciences.

The solute component in the halomonas elongate of the present invention is a tetrahydropyrimidine or a derivative of tetrahydropyrimidine hydroxytetrahydropyrimidine. Tetrahydropyrimidine chemical name, 2 methyl-1,4,5,6-tetrahydropyrimidine 4carboxylic acid, molecular formula: C ₆ H ₁₀ N ₂ O ₂ , molecular weight: 142.2 g / mol, LD50 (oral-rat 2200mg/kg, white powder, SIGMA-ALDRICH, or developed by the Institute of Microbiology, Chinese Academy of Sciences.

Hydroxytetrahydropyrimidine, chemical name, (4S, 5S)-hydroxy-2-methyl-1.4.5.-tetrahydropyrimidine-4carboxylic acid, molecular weight: 158.2 g/mol, molecular formula: C ₆ H ₁₀ N ₂ O ₃ , white powder. SIGMA-ALDRICH, or the Institute of Microbiology, Chinese Academy of Sciences.

In the scalp barrier protectant of the present invention, the halophilic solute is preferably hydroxytetrahydropyrimidine, and the hydroxytetrahydropyrimidine according to the present invention is 0.01% to 2% by weight of the composition, further optimized to be 0.05% to 1%.

Scalp sebum regulator

Salicylic acid derivatives: salicylic acid as a scalp sebum inhibitor and a scalp exfoliating agent have a certain irritating effect on the scalp, and often have a destructive effect on the scalp barrier. Therefore, the present invention uses a derivative of salicylic acid, namely, a top three Glycine hydrochloride.

Trimethylglycine salicylate and β-hydroxy acid (BHAs) in salicylic acid are similar to α-hydroxy acids (AHAs), have the function of accelerating the exfoliation of squamous keratinocytes, and are more irritating than α-hydroxy acids (AHAs). ) much lower; trimethylglycine in betaine has moisturizing, increasing skin elasticity and hydration, Substructures have both cationic and anionic charges, while human skin, including the scalp and hair, are all negatively charged under normal physiological conditions, so they contain positively charged molecules that have a natural affinity for the scalp and hair. Therefore, the trimethylglycine salicylic acid ester used in the present invention perfectly combines the advantages of salicylic acid extracted from willow bark and trimethylglycine extracted from betaine, and forms a unique structure of salicylic acid, which is mild. Adjusting the thickness of the scalp stratum corneum to a relatively ideal state, which contributes to the formation and improvement of the scalp barrier function, and has a gentle regulation effect on the scalp and hair lipids.

The scalp sebum regulator of the present invention is trimethylglycine salicylate in an amount of 0.1% to 15% by weight of the composition, and is further optimized to be 0.2% to 8% by weight.

Scalp sebum regulator

Vitamins: Vitamins including vitamin A, vitamin C, vitamin D, and vitamin B are all participants in the physiological functions of the human body and play different roles in human skin and metabolism. Among them, B vitamins contain many types. The role in hair and scalp and its physiological functions is also prominent. Among them, B vitamins include B ₁ , B ₂ , B ₃ , B ₅ , B ₆ , B _{12 ,} etc. According to previous applications and literature reports, the role of provitamin B _{5 in} scalp and hair nourishment is a recognized fact. , Tanno O, Ota Y, Kitamura N, et al. Br J Dermatol. 2000; 143: 524-531. and J Cosmet Laser Ther. 2006 Jun; 8(2): 96-101. Reported that vitamin B ₃ has A function of enhancing the skin barrier and controlling the secretion of oil from the skin, U.S. Patent No. 6,110,472 discloses a cosmetic composition containing vitamin B ₁₂ for the treatment of abnormal scalp detachment.

The scalp sebum regulating agent of the present invention has a range of vitamin B ₁ , vitamin B ₂ , vitamin B ₃ , vitamin B ₆ , provitamin B ₅ , and vitamin B _{12 .} The vitamin B of the present invention is further screened for vitamin B ₃ , vitamin B ₆ and vitamin B. ₁₂ and further preferred vitamin B ₁₂ .

The vitamin B ₁₂ of the present invention comprises from 0.05% to 3% by weight of the composition, and is further optimized to be from 0.1% to 2%.

Scalp soothing agent: scalp soothing agent includes allantoin, licorice flavonoids, dipotassium glycyrrhizinate, etc. Among them, dipotassium glycyrrhizinate: white fine powder, sweet taste, and medicine, can activate corticosteroids (inhibition of metabolism) Enzyme). Indirect enhancement of the role of corticosteroids, due to all cosmetics such as cream, cream, water, lotion, milk and honey, it can neutralize or reduce the toxic substances of cosmetics, and also prevent allergic reactions of some cosmetics, the market The above specifications are UV ≥ 98%, and HPLC ≥ 76% (refers to the active ingredient of glycyrrhizic acid). Dipotassium glycyrrhizinate has a chemical formula of C ₄₂ H ₆₀ K ₂ O ₁₆ , a molecular weight of 899.1128, and a pH of 5-6.

Licorice flavonoids are natural ingredients extracted from specific varieties of licorice, licorice flavonoids such as licorice, licorice and aspartame, mannitol, etc., and the compound extracted from licorice - licorice flavonoids in beauty cosmetics The efficacy, at the same time, licorice flavonoids also inhibit tyrosinase activity, scavenging oxygen base, which has anti-inflammatory, anti-allergic effects. Flavonoids flavonoids: brown-red thick liquid, insoluble in water and various oil esters, soluble in ethanol, propylene glycol, glycerin and some organic solvents.

Solid content ≥ 20%, light licorice content ≥ 0.38%, heavy metal: ≤ 0.002%, flavonoid test: positive.

Allantoin Chinese alias: 5-urela-lactamamide, ureidoacetic acid lactam, urea imidazoledione, molecular formula: C ₄ H ₆ O ₃ N ₄ , molecular weight: 158.12, appearance: white crystalline powder, odorless and tasteless, Content (%) ≥ 98.0, Jiangsu Kunshan Shuangyou Daily Chemical Production. Allantoin has a physiological function of promoting cell growth, accelerating wound healing, softening keratin protein, and is a good healing agent and anti-ulcer agent for skin wounds. It can be used for alleviating and treating skin dryness, scaly skin diseases and skin ulcers. Because allantoin is an amphoteric compound, it can form a complex combination of various substances to keep the skin moist, moisturized and soft. It is a special additive for cosmetics such as beauty salons. It is widely used in freckle cream, acne, shampoo, soap, Additives such as toothpaste, shave lotion, hair conditioner, astringent, anti-sweat deodorant lotion, etc. Cosmetics containing allantoin have the functions of protecting tissues, hydrophilicity, water absorption and preventing water dispersion;

The scalp soothing agent in the present invention is preferably allantoin.

In the present invention, allantoin is mainly used for its soothing action on the scalp, and has a softening effect on the stratum corneum of the scalp. Helps the scalp to build a water-lipid film to enhance the hydration of the skin surface and reduce the loss of transepidermal water, thereby synergistically enhancing the barrier function of the skin.

In the present invention, allantoin comprises from 0.05% to 0.5% by weight of the composition, and is further optimized to be from 0.08% to 0.2%.

Cosmetic acceptable carrier

Polyol: In the present invention, the polyol may be 1,3 butanediol, propylene glycol, glycerin (glycerol), 1,2-pentanediol, ethanol, etc., and glycerin is preferred in the present invention, and the amount used is composition. The weight percentage is from 1% to 10% and is further optimized to be from 2% to 8% by weight of the composition.

Thickener: Thickeners which can be used in the present invention include acrylic acid polymers, carbopol resins, hydroxyethyl cellulose, xanthan gum, etc., and the use of xanthan gum in the present invention is preferably used in an amount of 0.02 by weight of the composition. % to 0.5% and further optimized to 0.05% to 0.3% by weight of the composition.

Chelating agent: The chelating agent which can be used in the present invention includes disodium edetate and tetrasodium ethylenediaminetetraacetate. In the present invention, disodium edetate is preferably used in an amount of 0.01% by weight of the composition. To 0.1%, and further optimized to be from 0.02% to 0.1% by weight of the composition.

Preservatives: preservatives which can be used in the present invention include parabens, diazoalkyl ureas, phenoxyethanol, etc., and phenoxyethanol is preferably used in the present invention, and the amount used is 0.1% to 1.0% by weight of the composition. %, and further optimized to account for 0.5% to 0.8% by weight of the composition.

pH regulator

The triethanolamine and citric acid commonly used in the neutralization of the pH adjuster formulation technique of the present invention.

Preparation

An anti-dandruff composition of the present invention which modulates sebum balance of the scalp can be prepared by any known or otherwise effective technique suitable for providing a hair care composition, and the process of the present invention comprises conventional formulation and mixing techniques. Adding disodium edetate, allantoin, xanthan gum, glycerin, etc. to the components of the present invention in deionized water by weight, heating to 80 degrees and stirring to dissolve until transparent, and then stirring while cooling, when the temperature When reduced to 45 degrees, add vitamin B ₁₂ , N-palmitoylethanolamine, N-acetylethanolamine, hydroxytetrahydropyrimidine and trimethylglycine salicylate, respectively, by stirring, dissolve, and finally add preservatives and flavors. , a pigment, a pH adjuster, and the pH adjuster of the anti-dandruff composition is adjusted to 7.

Instructions

The anti-dandruff composition of the present invention for regulating the sebum balance of the scalp is used in the conventional manner of cleaning and conditioning the scalp, and mainly comprises the following steps:

(A) Wash the hair with a proper amount of shampoo and rinse off;

(B) Take the appropriate amount of this product, gently massage with the fingertip on the scalp for about 1-2 minutes, and wrap it with a hot towel for 5-15 minutes;

(C) Finally, it can be washed off with water or not.

These steps can be repeated as many times as needed to achieve the desired therapeutic effect.

Example

The following are non-limiting examples of anti-dandruff compositions of the present invention. The examples are given for the purpose of illustration only, and are not to be construed as limiting the scope of the invention. In these examples, all concentrations are by weight unless otherwise stated.

Example I-V

Example VI-X

Efficacy evaluation

The efficacy evaluation of the present invention is carried out based on the technical means employed in the anti-dandruff composition of the present invention.

The anti-dandruff composition of the invention adopts the technical scheme of non-traditional inhibition and killing of Malassezia, but is realized by the synergistic action of scalp sebum regulation and scalp barrier protection, and the synergistic cooperation between the two can help scalp recovery The normal thickness of the water lipid film establishes the dynamic balance of the scalp lipid and restores the scalp barrier function to reduce the dandruff. Therefore, in the efficacy test, the protective effect of the scalp barrier function was examined by the instrument TEWL method and the evaluation of the itching and anti-dandruff effect of the sensory evaluation test example.

The instrument test method is to test the value of TEWL of transepidermal water loss in the scalp. The larger the TEWL value, the faster the loss of water in the scalp, indicating that the barrier effect of the scalp is worse. Conversely, the smaller the TEWL value of the test indicates that the scalp remains moisture. The ability to be strong indicates that the scalp barrier function is enhanced. The measuring instrument used in the present invention, model: Delfin/VapoMeter, measuring range: 3-200 g/m ² h. Test site: top position.

The sensory evaluation method mainly tests the sensory effect of the embodiment on the anti-dandruff, and the sensory evaluation method of the complex head is: distributing the prepared embodiment to the tester, and the living habits in the process of using the sample of the embodiment of the invention The shampoo brands used did not change. None of the samples of the examples were used for four weeks, and the testers scored according to their own feelings, wherein the antipruritic effect was based on the start of the itching. It is scored by the degree of itching, and the anti-dandruff effect is scored according to the amount and size of the dandruff. The tester used the anti-dandruff composition sample, which was used after shampooing, and was used continuously for four weeks and three times a week. The tester scored according to his own feeling, and the antipruritic effect and anti-dandruff effect were based on the fifth embodiment. The first day of the week begins to calculate the start, according to the occurrence of itching and the onset of dandruff, if the first day of the fifth week begins to score 1 point, the next day 2 points, and so on If the itch starts on the seventh day, score 7 points. The scoring standard uses a 7-point scale, with 1 being the worst and 7 being the best. The higher the score, the better the better. The results of the evaluation of the use effects of various anti-dandruff compositions are shown in Table 1.

Choosing more serious dandruff (male and female), 22 cases, aged between 20-40 years old, divided into two groups, each group of 10 effective people, in the process of using the samples of the examples of the present invention, their living habits The shampoo brands used in the past have not changed.

In the first group, among the 10 persons, 5 of them used blank 1, and the remaining 5 used blank 2. The method of use was based on the method of use of the present invention, and the 7th day, the 14th day, the 21st day, the 28th, respectively. The TEWL value of the scalp was measured (averaged) in days and scored according to the above requirements to observe the degree of dandruff;

In the second group, among the 10 persons, the present inventions I to X were respectively used, and the method of use was determined according to the method of use of the present invention, and the scalp was measured on the 7th day, the 14th day, the 21st day, and the 28th day, respectively. TEWL values and scores for observing dandruff;

Table 1 TEWL values and evaluation of anti-dandruff effect

From the above results, it was shown that the control blank 1 of the present invention was used as required, and the percutaneous water loss value of the scalp on the 7th day after use and the transepidermal water loss value on the 28th day after use were measured, and the scalp transepidermal water loss value on the 28th day was measured. The decrease of 0.8% indicates that the value of transepidermal water loss of the scalp is not changed after the use of blank 1; the control blank 2 of the present invention measures the transepidermal water loss value of the scalp on the 7th day after use and the scalp on the 28th day after use. Percutaneous water loss values showed that the transepidermal water loss value of the scalp decreased by 1.4% on the 28th day, indicating that the value of transepidermal water loss of the scalp did not change much after using the blank 2, which was equivalent to no change.

Compared with the examples I to X of the present invention, the measured transepidermal water loss value of the scalp was reduced to a different extent on the 28th day than the seventh day (for example, in the example VI with the least reduction value, the TEWL was reduced by 15.7%, such as Example VII with the largest reduction value, TEWL decreased by 34.6%), indicating that the scalp barrier function was enhanced after using the embodiment of the present invention; and the antipruritic effect and the anti-dandruff effect obtained by the sensory evaluation method were obtained with blank 1 and blank 2 The sensory effect contrast has been greatly improved, indicating that the present invention inhibits and reduces dandruff by regulating the balance of scalp sebum and the enhancement of scalp barrier function without containing bacteriostatic and bactericidal agents.

Claims

An anti-dandruff composition comprising, in addition to a cosmetically acceptable carrier, a scalp barrier protectant and a scalp sebum regulating agent, the components and contents of which are as follows:

(1) Skin barrier protectant:

Between 0.001% and 1.0% by weight of the composition of N-palmitoylethanolamine and 0.01% to 20% by weight of the composition of N-acetylethanolamine, and the weight ratio of the two is 1:100;

And tetrahydropyrimidine or hydroxytetrahydropyrimidine in an amount of from 0.01% to 2% by weight of the composition;

(2) scalp sebum regulator:

Of the composition by weight of 0.1% to 15% of trimethylglycine salicylate and 0.05% of the composition to 3% by weight of vitamin B 12.
The anti-dandruff composition according to claim 1, wherein the N-palmitoylethanolamine content is from 0.005% to 0.5% by weight of the composition; and the N-acetylethanolamine is from 0.05% to 10% by weight of the composition.
The anti-dandruff composition according to claim 2, wherein the weight ratio of N-palmitoylethanolamine to N-palmitoylethanolamine is further optimized to 1:50.
The antidandruff composition according to claim 1, wherein trimethylglycine salicylate content of the composition by weight of 0.2% to 8%; vitamin B 12 weight percent of the composition is 0.1% -2%.
The anti-dandruff composition of claim 1 wherein the skin barrier protectant is selected from the group consisting of hydroxytetrahydropyrimidines in an amount from 0.05% to 1% by weight of the composition.
The anti-dandruff composition of claim 1 further comprising from 0.05% to 0.5% by weight of the composition of allantoin and 5% by weight of the composition.
The anti-dandruff composition of claim 6 wherein the allantoin content is from 0.08% to 0.2% by weight of the composition.
An anti-dandruff composition having a composition and content of:

% by weight of the composition of 0.015% by weight of N-palmitoylethanolamine,

N-acetylethanolamine in an amount of 0.625% by weight of the composition,

3% by weight of the composition of hydroxytetrahydropyrimidine,

3% by weight of the composition of trimethylglycine salicylate,

1% by weight of the composition of vitamin B 12 ,

0.1% by weight of the composition of allantoin,

5% by weight of the composition of glycerin,

0.1% by weight of the composition of xanthan gum,

0.05% by weight of the composition of disodium edetate,

Appropriate amount of preservatives, flavors and pigments. The balance is deionized water and the pH is adjusted to 7.