Depilatory emulsion containing paclitaxel and preparation method of depilatory emulsion

Abstract

The invention relates to a paclitaxel-containing depilatory emulsion and a preparation method thereof, and the paclitaxel-containing depilatory emulsion is prepared from the following raw materials in percentage by weight: 10-20% of grease, 8-12% of a humectant, 4-6% of an auxiliary emulsifier, 4-6% of an emulsifier, 8-12% of a paclitaxel solution, 0.5-1.0% of a preservative, 0.01-0.05% of minerals, 0.05-0.10% of essence essential oil and the balance of water. According to the preparation method of the unhairing emulsion, effective unhairing components such as paclitaxel are controlled to enter hair follicles to be absorbed and do not enter corium layers to be absorbed, and the unhairing emulsion has the advantages of being good in unhairing effect, safe, free of odor, free of skin allergy and suitable for continuous use; according to the preparation method disclosed by the invention, a stepped cooling and step-by-step emulsification mode is adopted to ensure that each component is fully and uniformly dispersed and a stable emulsification system is formed, and the preparation method has the advantages of simple steps and good emulsion stability.

Description

Technical Field

[0001] The invention relates to the technical field of special-purpose cosmetics, in particular to a depilatory emulsion containing paclitaxel and a preparation method thereof. Background Art

[0002] There are many types of human hair, and hair removal mainly targets the fine hair distributed on the face, neck, trunk and limbs. According to the depth of hair removal, common hair removal techniques can be divided into two categories. The first type of hair removal technology only removes the hair shaft visible on the surface of the skin, including shaving and the use of chemical depilatories; the second type of hair removal technology aims to completely remove the hair shaft and the hair bulb in the hair follicle, and the methods include plucking, waxing, sugaring and laser hair removal. However, both methods have obvious defects.

[0003] Although the first type of hair removal method is fast and convenient, it is short-lived. Although shaving is convenient, improper operation may cause skin scratches and may also cause pseudofolliculitis for people with sensitive skin. Chemical depilatories usually act on the disulfide bonds in the hair, destroying the hair structure through alkaline substances or thioglycolic acid and its salts, making it fragile and easy to break, so that it can be removed by wiping. However, chemical depilatories can irritate the skin and cause allergic reactions, so they should not be used frequently. In addition to possibly causing allergies, thiol compounds may also produce odors. Patent application No. CN115282080A introduces an enzyme-containing depilatory preparation that can gently decompose keratin in sweat hair, but long-term use may damage the skin's stratum corneum, reduce the skin's resistance, and increase the risk of infection.

[0004] Although the second type of hair removal method lasts longer, it is also more harmful to the skin. Plucking and waxing are painful and can easily lead to local redness, folliculitis, and ingrown hairs. Sugaring is only suitable for longer hairs, but may cause skin allergies. The effect of laser hair removal varies from person to person, and its main adverse reactions include burns, scabs, and pigmentation.

[0005] In the medical field, another method is to use eflornithine hydrochloride ointment to slow the growth of female facial hair, but this ointment has large side effects and may cause symptoms such as skin irritation, itching, redness and swelling, and may also cause increased skin pigmentation, so it needs to be used with caution under the guidance of a doctor.

[0006] Paclitaxel is a compound isolated and purified from Taxus chinensis. It can inhibit cell mitosis and only acts on cells in the division phase. It has no effect on cells in the interphase phase, so it is used as an anticancer drug. Paclitaxel is poorly soluble in water and cannot be absorbed into the blood through the skin or digestive tract, so it is usually injected intravenously in the form of an injection. After entering the blood, paclitaxel often causes severe allergic reactions in the human body, and can bring about a certain degree of bone marrow suppression, causing abnormal blood routine indicators. Therefore, the Ministry of Health's "Notice on Further Standardizing the Management of Health Food Ingredients" clearly lists Taxus chinensis as a "list of prohibited items for health foods."

[0007] The inventor recently published Green Science and Technology, 23(11), 3.128-130, which disclosed the application research of yew extract in daily chemical products. After the yew is effectively detoxified, other active ingredients such as volatile oils, flavonoids and other substances are basically retained, which can be used as raw materials or additives for daily chemical products to produce functional daily chemical products; by utilizing the cytotoxicity of alkaloid components in yew, appropriately retaining slightly toxic alkaloid components, it can stimulate local hair follicles, hinder hair growth and promote hair loss, and be used in the research and development of hair removal products; the "Cosmetics Supervision and Management Regulations" issued at the end of 2020 "Catalogue of Health Functions Permitted for Health Foods to Claim" and "Catalogue of Health Functions Permitted for Health Foods to Claim", these two regulations recognize that daily chemical products can have efficacy claims based on sufficient scientific evidence; many studies have proved the active effects of various components of Taxus chinensis, which shows that the application of Taxus chinensis in daily chemical products is reasonable and scientific; based on extraction technology and detoxification technology, the entire yew plant from branches and leaves to roots can be fully utilized. The research and development of functional daily chemical products such as cosmetics and aromatherapy is a new way to achieve the rational and efficient use of yew resources, which has great commercial prospects and value. At the same time, it is also of great significance to guide the industrial production of functional yew daily chemical products.

[0008] Transdermal absorption of cosmetics usually refers to the process by which the active ingredients in cosmetics penetrate the surface of the skin and penetrate deep into the skin tissue. Given that the skin surface is covered with a layer of stratum corneum, these active ingredients are difficult to penetrate. Therefore, the penetration-enhancing technology currently used in the cosmetics industry mainly focuses on utilizing intercellular spaces, which account for approximately 30% of the total volume of the stratum corneum, providing a channel for active ingredients to enter the deep layers of the skin, becoming a key path for transdermal absorption. In contrast, hair follicles account for a very small proportion of the skin surface area, and there is an epithelial sheath separating the hair follicles from the dermis. Therefore, cosmetics currently on the market do not rely primarily on hair follicles for absorption. Even if the detoxified yew extract described above is used in hair removal products, it is difficult to ensure that alkaloid components (such as paclitaxel) are limited to the hair follicles and do not penetrate into the dermis. This still requires further research and improvement. Summary of the invention

[0009] In view of the shortcomings of the prior art, the first object of the present invention is to provide a method for preparing a depilatory emulsion containing paclitaxel, which controls paclitaxel and other effective depilatory components to be absorbed into the hair follicles instead of being absorbed into the dermis, and has the advantages of good depilatory effect, safety, no odor, no skin allergy, and suitability for continuous use.

[0010] The second object of the present invention is to provide a method for preparing a depilatory emulsion containing paclitaxel, which has the advantages of simple steps and good emulsion stability.

[0011] To achieve the above first object, the present invention provides the following technical solutions: A depilatory emulsion containing paclitaxel is prepared from the following raw materials in percentage by weight: 10-20% of oil, 8-12% of moisturizer, 4-6% of auxiliary emulsifier, 4-6% of emulsifier, 8-12% of paclitaxel solution, 0.5-1.0% of preservative, 0.01-0.05% of mineral, 0.05-0.10% of essential oil, and the balance of water.

[0012] Furthermore, the oil is one or a combination of safflower seed oil and wheat germ oil.

[0013] Furthermore, the moisturizing agent is glycerin.

[0014] Furthermore, the auxiliary emulsifiers are stearic acid and hexadecanol, and the mass ratio of stearic acid to hexadecanol is 1-3:1.

[0015] Furthermore, the emulsifier is glyceryl monostearate, polysorbate 80 and sorbitan monostearate, and the mass ratio of glyceryl monostearate, polysorbate 80 and sorbitan monostearate is 2~5:2~3:1.

[0016] Furthermore, the concentration of paclitaxel in the paclitaxel solution is 0.15-2.00 mg / L, and the solvent in the paclitaxel solution is 90-100% v / v ethanol. The paclitaxel solution can be a simple solution obtained by directly dissolving purified paclitaxel in 90-100% v / v ethanol, or an extract obtained by extracting paclitaxel from the roots, stems, leaves, and bark of Taxus chinensis by various methods, and the solvent in the extract is 90-100% v / v ethanol.

[0017] Furthermore, the preservatives are kojic acid and paraben, and the mass ratio of kojic acid to paraben is 3-5:1.

[0018] Furthermore, the mineral is one or a combination of potassium hydroxide and potassium salt, wherein the potassium salt is a common form such as potassium chloride, potassium sulfate, potassium carbonate, etc.

[0019] Furthermore, the essential oil is peppermint essential oil. Among them, the main component of peppermint essential oil includes menthol (menthol), which is a colorless needle-shaped crystal or granular substance and is the main component of peppermint and peppermint essential oils; peppermint essential oil can be made by directly dissolving naturally purified or artificially synthesized menthol in a common flavor for cosmetics, and the flavor type is not limited as long as it can dissolve menthol, and it can also be peppermint oil extracted from peppermint plants.

[0020] To achieve the above second purpose, the present invention provides the following technical solutions: A method for preparing a depilatory emulsion containing paclitaxel comprises the following steps: S1 prepares raw materials including oil, moisturizer, auxiliary emulsifier, emulsifier, paclitaxel solution, preservative, minerals, essential oil, and water according to the proportion; S2 first heats the oil to 70-85°C, then adds the auxiliary emulsifier, stirs and disperses to obtain the oil phase; S3: first heat water to above 95°C, then add moisturizer, stir evenly, then add emulsifier, stir and disperse to obtain emulsion; S4: controlling the temperature of the emulsion obtained in S3 to 70-85° C., and slowly injecting the oil phase obtained in S2, stirring evenly, to obtain a matrix; S5: first slowly cool the matrix prepared in S4 to 45-55° C., then add paclitaxel solution, preservative, essential oil and minerals in sequence, stir and disperse evenly, and cool to below 40° C. to obtain the depilatory emulsion containing paclitaxel.

[0021] In summary, the beneficial technical effects of the present invention are: 1. The mechanism of action of the present invention is different from that of traditional hair removal cosmetics. It cleverly utilizes the natural renewal cycle of sweat hair: since paclitaxel only acts on rapidly dividing cells, after using the hair removal lotion of the present invention, sweat hair in the growth phase will stop growing. As the sweat hair in the regression phase falls off naturally, the number of sweat hair on the skin surface gradually decreases, and there is no discomfort during the whole process. Therefore, from the perspective of the mechanism of action, the present invention effectively solves the problems of contact dermatitis, abnormal pigmentation and hair follicle damage that may be caused by traditional hair removal methods; 2. The depilatory lotion of the present invention combines the dual functions of depilation and skin moisturizing. Its main function is to remove sweat hair, but it needs to be used continuously to maintain the effect. For this reason, ingredients such as glycerin and kojic acid are incorporated into the depilatory lotion to ensure that it can maintain the depilatory effect while also playing a skin moisturizing role; 3. Since the stratum corneum on the surface of human skin has a barrier effect on fat-soluble compounds such as paclitaxel, but the sebaceous glands usually open into the hair follicles, and the hair follicles contain free fat, the depilatory emulsion of the present invention, under the synergistic effect of free fat and emulsifier, can allow paclitaxel to penetrate into the hair matrix cells along the gaps of the hair follicles and inhibit hair growth. At the same time, due to the barrier of the epithelial cells on the inner wall of the hair follicles, paclitaxel will not penetrate into the dermis or blood, thereby avoiding the common allergic reaction when injecting paclitaxel; 4. Paclitaxel is a low-toxic and highly effective anticancer drug, and its core function is to stabilize microtubules and hinder the normal progress of cell mitosis; therefore, it only acts on the hair matrix cells in the rapid growth phase, and is harmless to the hair matrix cells in the resting phase; this makes the hair removal effect of the present invention reversible: 1 to 2 months after stopping the use of the hair removal emulsion of the present invention, the hair matrix cells in the resting phase will be reactivated, and the hair will gradually resume growth; 5. Common skin penetration enhancers mainly focus on improving the permeability of the intercellular spaces in the stratum corneum, but the depilatory lotion of the present invention needs to simultaneously promote the entry of paclitaxel into the hair follicles and prevent it from entering the blood. To this end, the present invention adopts a combination strategy of menthol and moisturizer, that is, the moisturizer constructs a hydrophilic barrier in the stratum corneum of the skin to prevent paclitaxel from penetrating into the dermis, while menthol utilizes its property of dilating pores to promote paclitaxel to enter the hair follicles through the pores; 6. The depilatory lotion of the present invention utilizes the enhanced potassium absorption capacity of rapidly dividing hair matrix cells. At the same time, the transmembrane transport of paclitaxel into hair matrix cells requires energy provided by sodium-potassium ion pumps. Therefore, the minerals containing potassium ions added in the present invention help promote the further absorption of paclitaxel inside the hair follicles by hair matrix cells. 7. In order to ensure that the final texture of the depilatory emulsion of the present invention has excellent coating performance and does not produce a greasy feeling when used, the present invention designs it as an O / W type emulsion; during the preparation process, the preparation method of the present invention adopts a step-by-step cooling and step-by-step emulsification method to ensure that the various components are fully dispersed and uniformly form a stable emulsified system, and the obtained depilatory emulsion has stable quality and will not have stratification. BRIEF DESCRIPTION OF THE DRAWINGS

[0022] Figure 1 Schematic diagram of the appearance of the depilatory emulsion of Example 1 of the present invention.

[0023] Figure 2 This is a stability test diagram of the depilatory emulsion of Example 1 of the present invention.

[0024] Figure 3 This is a graph showing the total number of bacteria in the depilatory lotion of Example 2 of the present invention.

[0025] Figure 4 It is the chromatogram of the depilatory emulsion of Example 2 of the present invention.

[0026] Figure 5 This is a picture of the external ear of a rabbit after using the depilatory lotion of Example 2 of the present invention.

[0027] Figure 6 1 is a diagram showing the hair shedding condition after using the depilatory emulsion of Example 1 of the present invention. DETAILED DESCRIPTION

[0028] In order to make the technical means, creative features, objectives and functions achieved by the present invention clearer and easier to understand, the present invention is further explained below in conjunction with the accompanying drawings and specific implementation methods.

[0029] Preparation Example 1: Accurately weigh a certain amount of paclitaxel (Chengdu Munster Biotechnology Co., Ltd.), add 90% v / v ethanol solution, and dilute to a paclitaxel concentration of 0.5 mg / L to obtain a paclitaxel / ethanol solution.

[0030] Preparation Example 2: Take the bark of Taxus chinensis and grind it into a particle size of 100 mesh, add it to the extraction kettle of a supercritical carbon dioxide extraction device, and add ethanol with a water content of 10% v / v (i.e., 90% v / v ethanol solution) as an entrainer to mix well, heat it to 35°C, pressurize it to 35MPa, extract for 120min, and then discharge CO2 under reduced pressure in a separation kettle to obtain an extract containing paclitaxel; add anhydrous ethanol to the extract to dilute the paclitaxel concentration to 0.15 mg / L, and filter it with a 0.45μm microporous filter membrane to obtain a paclitaxel extract.

[0031] Example 1: A depilatory emulsion containing paclitaxel disclosed in the present invention is prepared from raw materials containing the following weight percentages: Oil 13%; of which the oil is safflower seed oil; Moisturizer 9%; wherein the moisturizer is glycerin; Auxiliary emulsifier 6%; wherein the auxiliary emulsifier is stearic acid and hexadecanol, and the mass ratio of stearic acid to hexadecanol is 2:1; Emulsifier 4.4%; wherein the emulsifier is glyceryl monostearate, polysorbate 80 and sorbitan monostearate, and the mass ratio of glyceryl monostearate, polysorbate 80 and sorbitan monostearate is 2.86:2.43:1; 8% paclitaxel solution; wherein the paclitaxel solution is the paclitaxel / ethanol solution prepared in Preparation Example 1; Preservative 1%; wherein the preservative is kojic acid and paraben, and the mass ratio of kojic acid to paraben is 4:1 Minerals 0.02%; wherein the mineral is potassium hydroxide; 0.05% of essential oil; wherein the essential oil is peppermint essential oil obtained by directly dissolving menthol in the essence; The balance is water.

[0032] The present invention also discloses a method for preparing a depilatory emulsion containing paclitaxel, comprising the following steps: S1 prepares raw materials including oil, moisturizer, auxiliary emulsifier, emulsifier, paclitaxel solution, preservative, minerals, essential oil, and water according to the proportion; S2 first heats the oil to 80°C, then adds the auxiliary emulsifier, stirs and disperses to obtain the oil phase; S3: first heat water to 95°C, then add moisturizer, stir evenly, then add emulsifier, stir and disperse to obtain emulsion; S4 controls the temperature of the emulsion prepared in S3 to 80°C, and slowly injects the oil phase prepared in S2, stirring evenly to obtain a matrix; S5 first slowly cools the matrix prepared in S4 to 45°C, then sequentially adds paclitaxel solution, preservative, essential oil and minerals, stirs and disperses evenly, and cools to 40°C to obtain a depilatory emulsion containing paclitaxel.

[0033] Example 2: A depilatory emulsion containing paclitaxel disclosed in the present invention is prepared from raw materials containing the following weight percentages: Oil 15%; of which the oil is wheat germ oil; Moisturizing agent 10%; wherein the moisturizing agent is glycerin; Auxiliary emulsifier 4%; wherein the auxiliary emulsifier is stearic acid and hexadecanol, and the mass ratio of stearic acid to hexadecanol is 3:1; Emulsifier 6%; wherein the emulsifier is glyceryl monostearate, polysorbate 80 and sorbitan monostearate, and the mass ratio of glyceryl monostearate, polysorbate 80 and sorbitan monostearate is 3:2:1; 10% paclitaxel solution; wherein the paclitaxel solution is the paclitaxel extract prepared in Preparation Example 2; Preservative 0.8%; the preservatives are kojic acid and paraben, and the mass ratio of kojic acid to paraben is 3:1 Minerals 0.05%; wherein the mineral is potassium chloride; 0.1% essential oil; wherein the essential oil is peppermint essential oil composed of peppermint oil extracted from peppermint plants; The balance is water.

[0034] The present invention also discloses a method for preparing a depilatory emulsion containing paclitaxel, comprising the following steps: S1 prepares raw materials including oil, moisturizer, auxiliary emulsifier, emulsifier, paclitaxel solution, preservative, minerals, essential oil, and water according to the proportion; S2 first heats the oil to 85°C, then adds the auxiliary emulsifier, stirs and disperses to obtain the oil phase; S3 first heats water to 100°C, then adds a moisturizer, stirs evenly, then adds an emulsifier, stirs and disperses to obtain an emulsion; S4 controls the temperature of the emulsion prepared in S3 to 85°C, and slowly injects the oil phase prepared in S2, stirring evenly to obtain a matrix; S5 first slowly cools the matrix prepared in S4 to 55°C, then sequentially adds paclitaxel solution, preservative, essential oil and minerals, stirs and disperses them evenly, and cools to 40°C to obtain a depilatory emulsion containing paclitaxel.

[0035] Example 3: A depilatory emulsion containing paclitaxel disclosed in the present invention is prepared from raw materials containing the following weight percentages: Oil 10%; wherein the oil is safflower seed oil; Moisturizer 8%; wherein the moisturizer is glycerin; Auxiliary emulsifier 4%; wherein the auxiliary emulsifier is stearic acid and hexadecanol, and the mass ratio of stearic acid to hexadecanol is 1:1; Emulsifier 4%; wherein the emulsifier is glyceryl monostearate, polysorbate 80 and sorbitan monostearate, and the mass ratio of glyceryl monostearate, polysorbate 80 and sorbitan monostearate is 2:2:1; 8.5% paclitaxel solution; wherein the paclitaxel solution is the paclitaxel / ethanol solution prepared in Preparation Example 1; Preservative 0.5%; wherein the preservative is kojic acid and paraben, and the mass ratio of kojic acid to paraben is 3:1 Minerals 0.01%; wherein the mineral is potassium hydroxide; 0.05% of essential oil; wherein the essential oil is peppermint essential oil obtained by directly dissolving menthol in the essence; The balance is water.

[0036] The present invention also discloses a method for preparing a depilatory emulsion containing paclitaxel, comprising the following steps: S1 prepares raw materials including oil, moisturizer, auxiliary emulsifier, emulsifier, paclitaxel solution, preservative, minerals, essential oil, and water according to the proportion; S2 first heats the oil to 70°C, then adds the auxiliary emulsifier, stirs and disperses to obtain the oil phase; S3: first heat water to 95°C, then add moisturizer, stir evenly, then add emulsifier, stir and disperse to obtain emulsion; S4 controls the temperature of the emulsion prepared in S3 to 70°C, and slowly injects the oil phase prepared in S2, stirring evenly to obtain a matrix; S5 first slowly cools the matrix prepared in S4 to 46°C, then sequentially adds paclitaxel solution, preservative, essential oil and minerals, stirs and disperses evenly, and cools to 38°C to obtain a depilatory emulsion containing paclitaxel.

[0037] Example 4: A depilatory emulsion containing paclitaxel disclosed in the present invention is prepared from raw materials containing the following weight percentages: Oil 12%; of which the oil is safflower seed oil; Moisturizer 9%; wherein the moisturizer is glycerin; Auxiliary emulsifier 4%; wherein the auxiliary emulsifier is stearic acid and hexadecanol, and the mass ratio of stearic acid to hexadecanol is 1.5:1; Emulsifier 4%; wherein the emulsifier is glyceryl monostearate, polysorbate 80 and sorbitan monostearate, and the mass ratio of glyceryl monostearate, polysorbate 80 and sorbitan monostearate is 2.5:2.5:1; 9% paclitaxel solution; wherein the paclitaxel solution is the paclitaxel / ethanol solution prepared in Preparation Example 1; Preservative 0.6%; wherein the preservative is kojic acid and paraben, and the mass ratio of kojic acid to paraben is 3.5:1 Minerals 0.02%; wherein the mineral is potassium hydroxide; 0.06% of essential oil; wherein the essential oil is peppermint essential oil obtained by directly dissolving menthol in the essence; The balance is water.

[0038] The present invention also discloses a method for preparing a depilatory emulsion containing paclitaxel, comprising the following steps: S1 prepares raw materials including oil, moisturizer, auxiliary emulsifier, emulsifier, paclitaxel solution, preservative, minerals, essential oil, and water according to the proportion; S2 first heats the oil to 72°C, then adds the auxiliary emulsifier, stirs and disperses to obtain the oil phase; S3 first heats water to 100°C, then adds a moisturizer, stirs evenly, then adds an emulsifier, stirs and disperses to obtain an emulsion; S4 controls the temperature of the emulsion prepared in S3 at 72°C, and slowly injects the oil phase prepared in S2, stirring evenly to obtain a matrix; S5 first slowly cools the matrix prepared in S4 to 48°C, then sequentially adds paclitaxel solution, preservative, essential oil and minerals, stirs and disperses evenly, and cools to 35°C to obtain a depilatory emulsion containing paclitaxel.

[0039] Example 5: A depilatory emulsion containing paclitaxel disclosed in the present invention is prepared from raw materials containing the following weight percentages: Oil 14%; of which the oil is safflower seed oil; Moisturizing agent 10%; wherein the moisturizing agent is glycerin; Auxiliary emulsifier 5%; wherein the auxiliary emulsifier is stearic acid and hexadecanol, and the mass ratio of stearic acid to hexadecanol is 1:1; Emulsifier 5%; wherein the emulsifier is glyceryl monostearate, polysorbate 80 and sorbitan monostearate, and the mass ratio of glyceryl monostearate, polysorbate 80 and sorbitan monostearate is 3.5:3:1; 9.5% paclitaxel solution; wherein the paclitaxel solution is the paclitaxel / ethanol solution prepared in Preparation Example 1; Preservative 0.7%; wherein the preservative is kojic acid and paraben, and the mass ratio of kojic acid to paraben is 4:1 Minerals 0.03%; of which, the mineral is potassium carbonate; 0.07% essential oil; wherein the essential oil is peppermint essential oil obtained by directly dissolving menthol in the essence; The balance is water.

[0040] The present invention also discloses a method for preparing a depilatory emulsion containing paclitaxel, comprising the following steps: S1 prepares raw materials including oil, moisturizer, auxiliary emulsifier, emulsifier, paclitaxel solution, preservative, minerals, essential oil, and water according to the proportion; S2 first heats the oil to 74°C, then adds the auxiliary emulsifier, stirs and disperses to obtain the oil phase; S3: first heat water to 95°C, then add moisturizer, stir evenly, then add emulsifier, stir and disperse to obtain emulsion; S4 controls the temperature of the emulsion prepared in S3 to 74°C, and slowly injects the oil phase prepared in S2, stirring evenly to obtain a matrix; S5 first slowly cools the matrix prepared in S4 to 50° C., then sequentially adds paclitaxel solution, preservative, essential oil and minerals, stirs and disperses evenly, and cools to 32° C. to obtain a depilatory emulsion containing paclitaxel.

[0041] Example 6: A depilatory emulsion containing paclitaxel disclosed in the present invention is prepared from raw materials containing the following weight percentages: Oil 16%; of which the oil is safflower seed oil; Moisturizing agent 10%; wherein the moisturizing agent is glycerin; Auxiliary emulsifier 5%; wherein the auxiliary emulsifier is stearic acid and hexadecanol, and the mass ratio of stearic acid to hexadecanol is 1.5:1; Emulsifier 5%; wherein the emulsifier is glyceryl monostearate, polysorbate 80 and sorbitan monostearate, and the mass ratio of glyceryl monostearate, polysorbate 80 and sorbitan monostearate is 4:2:1; 10.5% paclitaxel solution; wherein the paclitaxel solution is the paclitaxel / ethanol solution prepared in Preparation Example 1; Preservative 0.8%; wherein the preservative is kojic acid and paraben, and the mass ratio of kojic acid to paraben is 4.5:1 Minerals 0.04%; wherein the mineral is potassium hydroxide; 0.08% of essential oil; wherein the essential oil is peppermint essential oil obtained by directly dissolving menthol in the essence; The balance is water.

[0042] The present invention also discloses a method for preparing a depilatory emulsion containing paclitaxel, comprising the following steps: S1 prepares raw materials including oil, moisturizer, auxiliary emulsifier, emulsifier, paclitaxel solution, preservative, minerals, essential oil, and water according to the proportion; S2 first heats the oil to 78°C, then adds the auxiliary emulsifier, stirs and disperses to obtain the oil phase; S3 first heats water to 100°C, then adds a moisturizer, stirs evenly, then adds an emulsifier, stirs and disperses to obtain an emulsion; S4 controls the temperature of the emulsion prepared in S3 to 78°C, and slowly injects the oil phase prepared in S2, stirring evenly to obtain a matrix; S5 first slowly cools the matrix prepared in S4 to 50°C, then sequentially adds paclitaxel solution, preservative, essential oil and minerals, stirs and disperses evenly, and cools to 30°C to obtain a depilatory emulsion containing paclitaxel.

[0043] Example 7: A depilatory emulsion containing paclitaxel disclosed in the present invention is prepared from raw materials containing the following weight percentages: Oil 18%; of which the oil is safflower seed oil; Moisturizer 11%; wherein the moisturizer is glycerin; Auxiliary emulsifier 6%; wherein the auxiliary emulsifier is stearic acid and hexadecanol, and the mass ratio of stearic acid to hexadecanol is 1:1; Emulsifier 6%; wherein the emulsifier is glyceryl monostearate, polysorbate 80 and sorbitan monostearate, and the mass ratio of glyceryl monostearate, polysorbate 80 and sorbitan monostearate is 4.5:2.5:1; Paclitaxel solution 11%; wherein the paclitaxel solution is the paclitaxel / ethanol solution prepared in Preparation Example 1; Preservative 0.9%; the preservatives are kojic acid and paraben, and the mass ratio of kojic acid to paraben is 5:1 Minerals 0.04%; wherein the mineral is potassium hydroxide; 0.09% of essential oil; wherein the essential oil is peppermint essential oil obtained by directly dissolving menthol in the essence; The balance is water.

[0044] The present invention also discloses a method for preparing a depilatory emulsion containing paclitaxel, comprising the following steps: S1 prepares raw materials including oil, moisturizer, auxiliary emulsifier, emulsifier, paclitaxel solution, preservative, minerals, essential oil, and water according to the proportion; S2 first heats the oil to 82°C, then adds the auxiliary emulsifier, stirs and disperses to obtain the oil phase; S3: first heat water to 95°C, then add moisturizer, stir evenly, then add emulsifier, stir and disperse to obtain emulsion; S4 controls the temperature of the emulsion prepared in S3 to 82°C, and slowly injects the oil phase prepared in S2, stirring evenly to obtain a matrix; S5 first slowly cools the matrix prepared in S4 to 52° C., then sequentially adds paclitaxel solution, preservative, essential oil and minerals, stirs and disperses them evenly, and cools to 40° C. to obtain a depilatory emulsion containing paclitaxel.

[0045] Example 8: A depilatory emulsion containing paclitaxel disclosed in the present invention is prepared from raw materials containing the following weight percentages: Oil 20%; the oil is safflower seed oil; Moisturizer 12%; wherein the moisturizer is glycerin; Auxiliary emulsifier 6%; wherein the auxiliary emulsifier is stearic acid and hexadecanol, and the mass ratio of stearic acid to hexadecanol is 3:1; Emulsifier 6%; wherein the emulsifier is glyceryl monostearate, polysorbate 80 and sorbitan monostearate, and the mass ratio of glyceryl monostearate, polysorbate 80 and sorbitan monostearate is 5:3:1; 12% paclitaxel solution; wherein the paclitaxel solution is the paclitaxel / ethanol solution prepared in Preparation Example 1; Preservative 1%; wherein the preservative is kojic acid and paraben, and the mass ratio of kojic acid to paraben is 5:1 Minerals 0.05%; wherein the mineral is potassium hydroxide; 0.1% essential oil; wherein the essential oil is peppermint essential oil obtained by directly dissolving menthol in the essence; The balance is water.

[0046] The present invention also discloses a method for preparing a depilatory emulsion containing paclitaxel, comprising the following steps: S1 prepares raw materials including oil, moisturizer, auxiliary emulsifier, emulsifier, paclitaxel solution, preservative, minerals, essential oil, and water according to the proportion; S2 first heats the oil to 84°C, then adds the auxiliary emulsifier, stirs and disperses to obtain the oil phase; S3 first heats water to 100°C, then adds a moisturizer, stirs evenly, then adds an emulsifier, stirs and disperses to obtain an emulsion; S4 controls the temperature of the emulsion prepared in S3 to 84°C, and slowly injects the oil phase prepared in S2, stirring evenly to obtain a matrix; S5 first slowly cools the matrix prepared in S4 to 54°C, then sequentially adds paclitaxel solution, preservative, essential oil and minerals, stirs and disperses evenly, and cools to 40°C to obtain a depilatory emulsion containing paclitaxel.

[0047] Test Example 1: pH Determination The depilatory emulsion prepared in Example 2 was used to measure the pH value of the product using the method of GB / T13531.1-2008: 1 part of the depilatory emulsion was weighed, 9 parts of deionized water were added, the two were mixed and stirred at 40°C, cooled to 25°C, and the pH value of the mixture was measured with a pH meter to an accuracy of 0.1. The above test was repeated 5 times to calculate the average value.

[0048] The measurement results showed that the pH value was 7.0±0.2, which is within the allowable range of cosmetic pH value in the national standard.

[0049] Test Example 2: Stability Test After the depilatory lotion prepared in Example 1 was placed at room temperature for 1 week, 1.5 g of the depilatory lotion was taken into a centrifuge tube and centrifuged at 4000 r / min for 30 min to observe whether there was stratification and color uniformity. The depilatory lotion was placed in a 55°C oven and a -15°C refrigerator for 24 h to observe whether there was liquefaction, hardening, or roughening. The results are as follows: Figure 2 shown.

[0050] from Figure 2 It can be seen that under the extreme conditions set in the test, the depilatory lotion did not show any oil-emulsion stratification, liquefaction or hardening, indicating that the product is stable in nature.

[0051] Test Example 3: Total Bacterial Count Detection The depilatory lotion prepared in Example 2 was tested for total bacterial count according to the method of GB / T7918.1-1987. 10 g of the depilatory lotion was weighed and placed in a conical flask, 90 mL of sterile saline was added, and after sufficient oscillation and mixing, it was placed in a 30-32°C water bath and allowed to stand for 15 min to obtain a 1:10 dilution. The 1:10 dilution was further diluted with sterile saline to obtain a 1:10 dilution, a 1:100 dilution, and a 1:1000 dilution. The dilution was injected into a sterile plate, 3 plates for each dilution multiple, and 2 mL of the dilution was taken from each plate.

[0052] Prepare lecithin and Tween 80 nutrient agar medium according to the method of GB / T7918.2-1987. After sterilization, cool to 45-50℃ and pour into the plate with diluent, about 15mL per plate. Prepare another blank control plate. Rotate the plate to mix the sample and the medium thoroughly. After the agar solidifies, turn the plate over and place it in a 37℃ incubator for 48h. After 48h, observe with the naked eye, count the number of colonies, and after recording the number of colonies on each plate, calculate the average number of colonies grown on each plate with the same dilution. The results are as follows: Figure 3 shown.

[0053] from Figure 3 It can be seen that the total colony count is <1000CFU / g, which meets the requirements of GB7916-1987.

[0054] Test Example 4: Paclitaxel Content Detection 10 g of the depilatory lotion prepared in Example 2 was accurately weighed, 30 mL of methanol was added and ultrasonically treated for 30 min to make the mixture uniform, filtered and transferred to a 50 mL volumetric flask, and the volume was fixed with methanol as the sample solution. A paclitaxel standard curve was prepared according to the method in the literature "Zhou Xiuling, Peng Quancai. Determination of paclitaxel content in yew branches and leaves by high performance liquid chromatography [J]. Shizhen Traditional Chinese Medicine, 2008, (06): 1434-1436." and the paclitaxel content in the depilatory lotion was measured.

[0055] After testing, the paclitaxel content in the depilatory lotion is 0.014 mg / L. The sample chromatogram is shown in Figure 4 , among which, the peak at 28.030min is paclitaxel.

[0056] Test Example 5: Animal Test Take a rabbit weighing 2.5±0.2kg, apply the depilatory lotion prepared in Example 2 to the auricle of the left ear, about 0.05mL each time, twice a day, do not apply to the left ear helix, do not apply to the right ear, and feed normally. On the 1st day, 7th day, and 14th day, gently wipe the applied area with a wet towel, and take pictures after the surface is dry. On the 11th day, 2h after applying the depilatory lotion, draw blood from the auricle vein, and detect the paclitaxel content in rabbit plasma according to the method of "Zhang Tianying, Guo Yuzhi, Zhang Dawei, et al. Validation of the HPLC method for determining the concentration of paclitaxel in human plasma [J]. Heilongjiang Medical Science, 2013, (2): 54-55", and perform blood routine tests with a blood cell analyzer. The results are as follows: Figure 5 shown.

[0057] from Figure 5 It can be seen that the hair on the left ear of the rabbit using the depilatory lotion has been significantly reduced, while the hair on the right ear of the rabbit not using the lotion has not changed. Since rabbit hair is constantly being renewed, a significant depilatory effect can be observed in 7 days. If paclitaxel enters the blood, it may cause damage to the hematopoietic function of the bone marrow. However, routine blood tests showed that there was no obvious abnormality in the number of various blood cells in the test rabbits, and paclitaxel was not detected in the blood, indicating that the effect of paclitaxel only stayed on the surface and did not enter the blood.

[0058] Test Example 6: Sensitization and efficacy verification test 10 volunteers with more body hair were recruited, and their arms, calves, and backs were used as the hair removal test areas. A sufficient amount of the hair removal lotion prepared in Example 1 was applied twice a day, and they were massaged and rubbed appropriately. The test period was 1 month. The hair removal efficacy was verified by observing the hair loss in the test area before and after. During the test, the 10 volunteers recorded whether there were any adverse skin reactions in the hair removal test area, including but not limited to symptoms such as erythema, itching, abnormal pigmentation, and contact dermatitis. The results are as follows: Figure 6 shown.

[0059] from Figure 6 It can be seen that all 10 volunteers achieved good hair removal effects, with a hair removal rate of 90% at the application site, no black spots appeared, and no allergic symptoms occurred.

[0060] Finally, it should be noted that the above embodiments are only used to illustrate the technical solution of the present invention rather than to limit it. Although the present invention has been described in detail with reference to the preferred embodiments, those skilled in the art should understand that the technical solution of the present invention can be modified or replaced by equivalents without departing from the purpose and scope of the technical solution of the present invention, which should be included in the scope of the claims of the present invention.

Claims

1. A depilatory emulsion containing paclitaxel, characterized in that: The invention is prepared from the following raw materials in weight percentage: 10-20% of oil, 8-12% of moisturizer, 4-6% of auxiliary emulsifier, 4-6% of emulsifier, 8-12% of paclitaxel solution, 0.5-1.0% of preservative, 0.01-0.05% of mineral, 0.05-0.10% of essential oil, and the balance of water.

2. A depilatory emulsion containing paclitaxel according to claim 1, characterized in that: The oil is one of safflower seed oil and wheat germ oil or a combination of the two.

3. A depilatory emulsion containing paclitaxel according to claim 1, characterized in that: The humectant is glycerin.

4. A depilatory emulsion containing paclitaxel according to claim 1, characterized in that: The auxiliary emulsifiers are stearic acid and hexadecanol, and the mass ratio of stearic acid to hexadecanol is 1-3:

1.

5. A depilatory emulsion containing paclitaxel according to claim 1, characterized in that: The emulsifiers are glyceryl monostearate, polysorbate 80 and sorbitan monostearate, and the mass ratio of glyceryl monostearate, polysorbate 80 and sorbitan monostearate is 2-5:2-3:

1.

6. A depilatory emulsion containing paclitaxel according to claim 1, characterized in that: The concentration of paclitaxel in the paclitaxel solution is 0.15-2.00 mg / L, and the solvent in the paclitaxel solution is 90-100% v / v ethanol.

7. A depilatory emulsion containing paclitaxel according to claim 1, characterized in that: The preservatives are kojic acid and paraben, and the mass ratio of kojic acid to paraben is 3-5:

1.

8. A depilatory emulsion containing paclitaxel according to claim 1, characterized in that: The mineral is one or a combination of potassium hydroxide and potassium salt.

9. A depilatory emulsion containing paclitaxel according to claim 1, characterized in that: The essential oil is peppermint essential oil.

10. The method for preparing a depilatory emulsion containing paclitaxel according to any one of claims 1 to 9, characterized in that: The following steps are included: S1 prepares raw materials including oil, moisturizer, auxiliary emulsifier, emulsifier, paclitaxel solution, preservative, minerals, essential oil, and water according to the proportion; S2 first heats the oil to 70-85°C, then adds the auxiliary emulsifier, stirs and disperses to obtain the oil phase; S3: first heat water to above 95°C, then add moisturizer, stir evenly, then add emulsifier, stir and disperse to obtain emulsion; S4: controlling the temperature of the emulsion obtained in S3 to 70-85° C., and slowly injecting the oil phase obtained in S2, stirring evenly, to obtain a matrix; S5: first slowly cool the matrix prepared in S4 to 45-55° C., then add paclitaxel solution, preservative, essential oil and minerals in sequence, stir and disperse evenly, and cool to below 40° C. to obtain the depilatory emulsion containing paclitaxel.

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