A serum for clearing acne and controlling oil, and its preparation method

Abstract

This invention discloses an acne-clearing and oil-controlling essence and its preparation method, belonging to the field of skincare technology. The acne-clearing and oil-controlling essence of this invention comprises the following components in parts by weight: 0.05-5 parts of Magnolia officinalis bark extract, 0.01-5 parts of Candida albicans / glucose / methyl rapeseed oil fermentation product, 0.01-1 parts of Neem leaf extract, 0.05-5 parts of Peppermint leaf extract, 0.1-5 parts of Lonicera japonica flower extract, 0.1-5 parts of azelaic acid, 0.01-0.1 parts of glycyrrhetinic acid, 0.2-2 parts of salicylic acid, 0.01-5 parts of niacinamide, 0.01-1 parts of allantoin, and 0.01-5 parts of betaine. The technical solution provided by this invention uses multiple plant antibacterial agents as additives, and is combined with other components, exhibiting excellent acne-clearing, oil-controlling, soothing, and anti-inflammatory effects. Furthermore, this invention does not contain preservatives, therefore it is gentle and non-irritating.

Description

Technical Field

[0001] This invention belongs to the field of skin care technology, and in particular relates to an acne-clearing and oil-controlling essence and its preparation method. Background Technology

[0002] Acne, scientifically known as acne vulgaris, includes common types such as blackheads, whiteheads, papules, pustules, cysts, nodules, and conglobate cysts. There are many causes of acne, mainly the following four: (1) Excessive sebum secretion: The level of androgens, especially testosterone, rises rapidly, which promotes the development of sebaceous glands and produces a large amount of sebum. (2) Abnormal keratinization: Excessive keratinization of the hair follicle sebaceous gland duct, the duct diameter becomes smaller and narrower, and sebum is difficult to be discharged, causing hair follicle blockage. (3) Anaerobic bacteria proliferation: Excessive secretion of hair follicle sebaceous gland provides nutrients for microorganisms, and the blocked pores cause hypoxia inside the hair follicle, leading to the proliferation of Propionibacterium acnes and Staphylococcus aureus, resulting in skin acne outbreak. (4) Inflammatory response: The proliferation of a large number of anaerobic bacteria brings about an inflammatory response, destroys the hair follicle sebaceous gland, and then suppurates. At present, most acne removal products on the market use strong bactericides to achieve the effect of quick acne removal, but long-term use may produce drug resistance, which will gradually weaken the acne removal effect. Summary of the Invention

[0003] The purpose of this invention is to overcome the shortcomings of the prior art and provide an essence with good oil control and a gentle, long-lasting acne-removing effect.

[0004] To achieve the above objectives, the technical solution adopted by the present invention is as follows: an acne-clearing and oil-controlling essence, wherein the acne-clearing and oil-controlling essence comprises the following components in parts by weight: 0.05-5 parts of Magnolia officinalis bark extract, 0.01-5 parts of Candida albicans / glucose / methyl rapeseed oil fermentation product, 0.01-1 parts of Neem leaf extract, 0.05-5 parts of Peppermint leaf extract, 0.1-5 parts of Lonicera japonica flower extract, 0.1-5 parts of azelaic acid, 0.01-0.1 parts of glycyrrhetinic acid, 0.2-2 parts of salicylic acid, 0.01-5 parts of niacinamide, 0.01-1 parts of allantoin, and 0.01-5 parts of betaine.

[0005] This invention's acne-clearing and oil-controlling essence incorporates multiple plant-based antibacterial agents, such as extracts from Neem leaf, Magnolia officinalis bark, and Lonicera japonica flower. This well-balanced combination of plant-based antibacterial agents provides gentle anti-inflammatory, antibacterial, and acne-removing effects. Furthermore, the addition of plant extracts as antibacterial agents helps prevent drug resistance from long-term use. Additionally, this invention utilizes a multi-component combination of Candida albicans / glucose / methyl rapeseed oil fermentation products with azelaic acid and salicylic acid to achieve excellent oil-controlling effects. Furthermore, this invention also incorporates allantoin, betaine, Peppermint leaf extract, glycyrrhetinic acid, and other components to provide soothing, anti-allergic, and anti-inflammatory effects, effectively reducing skin irritation and achieving gentle acne removal. Therefore, this invention's technical solution, through the rational combination of various components, addresses acne from multiple dimensions, including oil control, improvement of abnormal follicular keratosis, unclogging pores, powerful antibacterial effects, and soothing and anti-inflammatory properties, thereby achieving optimal oil control and acne removal results.

[0006] The fermentation product of *Candida albicans* / glucose / methyl rapeseed oil can slow down sebum production and regulate sebum secretion, thus achieving an oil-controlling effect. It also possesses unique antibacterial activity, inhibiting the proliferation of *Propionibacterium acnes* and *Corynebacterium xerosis*. The added azelaic acid, also known as "azoosic acid," improves skin keratinization, thereby unclogging pores and competitively inhibiting 5α-reductase activity, suppressing sebum secretion. Azelaic acid also has broad-spectrum antibacterial effects. The added salicylic acid, an oil-soluble acid, can dissolve the intercellular matrix, causing dead skin cells to shed, thus accelerating epidermal renewal and alleviating... The skin exhibits abnormal keratinization, and salicylic acid also has the effect of removing acne and cleaning pores. It can act on the hair follicle wall cells, penetrate deep into the pores and loosen the pore blockage. At the same time, it can also inhibit the proliferation of Propionibacterium acnes and Staphylococcus aureus. The added glycyrrhizic acid can inhibit the production of inflammatory factors and reduce skin inflammation. The added neem leaf extract has anti-inflammatory and antibacterial effects. The added magnolia bark extract contains magnolol, which has anti-inflammatory, antibacterial and antioxidant effects, and can effectively inhibit the reproduction of pathogens such as Propionibacterium acnes. The honeysuckle flower extract contains phenolic acids, saponins, flavonoids and other active ingredients, which have antibacterial, anti-inflammatory and antioxidant effects.

[0007] As a preferred embodiment of the acne-clearing and oil-controlling essence of the present invention, the acne-clearing and oil-controlling essence comprises the following components in parts by weight: 0.3-0.8 parts of Magnolia officinalis bark extract, 0.05-1 parts of Candida albicans / glucose / rapeseed oleate fermentation product, 0.02-0.1 parts of Neem leaf extract, 0.5-2 parts of Peppermint leaf extract, 0.3-1 parts of Lonicera japonica flower extract, 0.2-1 parts of azelaic acid, 0.02-0.08 parts of glycyrrhetinic acid, 0.5-1.5 parts of salicylic acid, 0.5-1.5 parts of niacinamide, 0.05-0.15 parts of allantoin, and 0.5-1.5 parts of betaine.

[0008] When the above-mentioned components are preferred, the prepared product has a better therapeutic effect on acne and the best oil control effect.

[0009] As a preferred embodiment of the acne-clearing and oil-controlling essence of the present invention, the acne-clearing and oil-controlling essence further includes the following components in parts by weight: 0.01-2 parts thickener, 0.01-2 parts pH adjuster, 0.2-0.5 parts antioxidant, 1-25 parts moisturizer, 0.01-1 part penetration enhancer, and 50-100 parts solvent.

[0010] The addition of penetration enhancers can improve the efficacy of the active ingredients added in this invention, thereby achieving stronger efficacy with a smaller dosage; it can also achieve better results at a faster pace to a certain extent.

[0011] In a preferred embodiment of the acne-clearing and oil-controlling essence of the present invention, the thickener comprises an acrylate / C10-30 alkanol acrylate crosspolymer.

[0012] In a preferred embodiment of the acne-clearing and oil-controlling essence of the present invention, the pH adjuster includes any one of triethanolamine, arginine, and aminomethylpropanol.

[0013] In a preferred embodiment of the acne-clearing and oil-controlling essence of the present invention, the moisturizer includes at least one of propylene glycol and 1,2-hexanediol.

[0014] As a preferred embodiment of the acne-clearing and oil-controlling essence of the present invention, the penetration enhancer includes at least one of tetrahydropiperine, pentylene glycol, and isosorbide dimethyl ether.

[0015] In a preferred embodiment of the acne-clearing and oil-controlling essence of the present invention, the penetration enhancer includes tetrahydropiperine.

[0016] Tetrahydropiperine was chosen as the penetration enhancer added in this invention because it is a plant-based penetration enhancer that can increase the fluidity of the lipid bilayer and open the tight junction proteins between cells, thereby increasing the rate at which the active ingredient penetrates the skin in the shortest possible time.

[0017] In addition, the present invention also provides a method for preparing the acne-clearing and oil-controlling essence, comprising the following steps:

[0018] (1) Mix phase C, heat and stir to obtain mixture I;

[0019] (2) Mix phase E, heat and stir to obtain mixture II;

[0020] (3) Mix phase A, heat and stir to homogenize, cool down, then add each component of phase B in sequence and stir evenly to obtain mixture III;

[0021] (4) After cooling mixture III, add mixture I, mixture II and phase D, and stir evenly; cool to room temperature to obtain acne-clearing and oil-controlling essence;

[0022] Phase A includes solvents, humectants, allantoin, betaine, and thickeners; Phase B is a pH adjuster; Phase C includes antioxidants and humectants; Phase D includes nicotinamide, Magnolia officinalis bark extract, Candida albicans / glucose / rapeseed oil methyl ester fermentation product, Neem leaf extract, Peppermint leaf extract, and Lonicera japonica flower extract; Phase E includes azelaic acid, glycyrrhetinic acid, salicylic acid, penetration enhancers, and humectants.

[0023] In a preferred embodiment of the preparation method of the acne-clearing and oil-controlling essence of the present invention, in step (1), the heating temperature is 55-65℃; in step (2), the heating temperature is 50-60℃; in step (3), the heating and stirring homogenization temperature is 80-85℃, and the heating and stirring homogenization time is 5-10 minutes; in step (4), the temperature after cooling is 40-45℃.

[0024] Compared with the prior art, the beneficial effects of the present invention are as follows:

[0025] First: The technical solution provided by this invention uses a variety of plant antibacterial agents as additives to achieve a mild antibacterial effect. At the same time, it is compounded with fermentation products of Candida albicans / glucose / rapeseed oil methyl ester and substances such as azelaic acid and salicylic acid, which have a significant oil-controlling effect while inhibiting bacteria. In addition, it adds soothing and anti-inflammatory field peppermint leaf extract, allantoin, and betaine; thereby relieving the inflammation caused by acne.

[0026] Second: The technical solution of the present invention also adds plant penetration enhancers on the basis of antibacterial, oil control and anti-inflammatory effects, which can promote the penetration of active ingredients into the skin, improve the efficacy of active ingredients, achieve stronger effects with smaller doses, or achieve faster acne removal, oil control and anti-inflammatory effects with the same dose.

[0027] Third: The technical solution provided by this invention does not contain preservatives, which further ensures that the overall formula is mild and non-irritating;

[0028] Fourth: The preparation method of the acne-clearing and oil-controlling essence provided by the technical solution of the present invention is simple, easy to operate, requires no special equipment, and is convenient for actual production. Attached Figure Description

[0029] Figure 1 Acne record images of volunteers before using this invention, i.e., 0 days after use;

[0030] Figure 2 Acne record images of volunteers after 7 days of using the product prepared in Example 3 of this invention;

[0031] Figure 3 Acne record images of volunteers after 14 days of using the product prepared in Example 3 of this invention. Detailed Implementation

[0032] To better illustrate the purpose, technical solution, and advantages of the present invention, the present invention will be further described below in conjunction with specific embodiments.

[0033] Table 1: Formulas of Acne-Clearing and Oil-Controlling Essences in Examples 1-5 and Comparative Examples 1-9 (The numbers in the table represent the percentage content of the corresponding component in the acne-clearing and oil-controlling essence).

[0034]

[0035]

[0036] The preparation methods of the acne-clearing and oil-controlling serums in Examples 1-5 and Comparative Examples 1-9 specifically include the following steps:

[0037] (1) Mix phase C, heat to 60°C, and stir to obtain mixture I;

[0038] (2) Mix phase E, heat to 55°C, and stir to obtain mixture II;

[0039] (3) Mix phase A, heat to 82°C, stir and homogenize for 8 minutes, cool to 65°C, then add each component of phase B in sequence and stir evenly to obtain mixture III;

[0040] (4) After cooling mixture III to 42°C, add mixture I, mixture II and phase D, and stir evenly; cool to room temperature to obtain acne-clearing and oil-controlling essence.

[0041] Example of effect

[0042] 1. Characterization of properties and stability:

[0043] The serums prepared in Examples 1-5 are pale yellow liquids. The serums were mixed with water at a mass ratio of 1:10 and the pH of the aqueous solution was tested to be 5.0-6.5. The stability of the serums prepared in Examples 1-5 was then tested. The heat resistance test involved placing the serums at 45±2℃ for 3 months, and no abnormalities were found. The cold resistance test involved placing the serums at -18±2℃ for 3 months, and no abnormalities were found. The cyclic test involved placing the serums between 45℃, room temperature, and (-18)℃ for 7 cycles, and no abnormalities were found. These data demonstrate that the serums prepared using the method of this invention have good properties and excellent stability.

[0044] 2. Security Testing:

[0045] Safety tests were conducted on the serums prepared in Examples 1-5 and Comparative Examples 1-9. 140 volunteers aged 16-45 years were selected and divided into 14 groups of 10 each to test the safety of the serums obtained in Examples 1-5 and Comparative Examples 1-9. The specific testing method was as follows: 0.5g of the corresponding test sample was applied to the inner side of the right arm of each volunteer, and skin reactions were recorded at 1 hour, 4 hours, 8 hours, and 24 hours. The test results showed that no skin redness or erythema or other allergic reactions were observed in any of the 140 volunteers after 1 hour, 4 hours, 8 hours, and 24 hours of application, indicating that the product of this invention is mild, safe, and non-irritating.

[0046] 3. Acne-removing and oil-controlling effect test:

[0047] 280 volunteers aged 16-45 were selected and divided into 14 groups of 20 each to test the acne-reducing and oil-controlling effects of the serums obtained in Examples 1-5 and Comparative Examples 1-9 of this invention. Each volunteer was tested for both acne-reducing and oil-controlling effects simultaneously. All 280 volunteers had oily skin with mild to moderate acne. During the acne-reducing and oil-controlling test, volunteers maintained a regular lifestyle. The specific testing method was as follows: volunteers used the corresponding test sample every morning and evening. The test areas were the left and right cheekbones, the left and right cheeks at the intersection of the nose tip and pupil, and the left and right sides of the temples at the intersection of the corners of the mouth. Follow-up was conducted on days 0, 7, and 14 of the test. Changes in oil content and acne reduction after sample use were tested and recorded. The same person measured each group of volunteers. Skin oil content was measured using a Sebumeter skin oil content analyzer manufactured by Courage+Khazaka (CK) GmbH, Germany. The average value of the data from each group of volunteers was taken. The acne-reducing test results after 14 days of sample use are shown in Table 2, and the oil-controlling test results are shown in Table 3.

[0048] The acne treatment tracking involved before-and-after comparisons. Photos were taken, and the total number of non-inflammatory and inflammatory lesions on the patient's face was statistically analyzed. The treatment efficacy was judged by the lesion regression rate and the effectiveness rate. Lesion regression rate = (Number of lesions before treatment - Number of lesions after treatment) / Number of lesions before treatment * 100%. Cure: Lesion regression rate ≥ 90%; Significant improvement: 60% ≤ Lesion regression rate < 90%; Improvement: 20% ≤ Lesion regression rate < 60%; Ineffective: Lesion regression rate < 20%. The effectiveness rate was the percentage of cured and significantly improved cases out of the total number of cases.

[0049] The calculation method for the 7-day change in the oil control test table is as follows: 7-day change = (7-day oil content - 0-day oil content) / 0-day oil content * 100%; 14-day change = (14-day oil content - 0-day oil content) / 0-day oil content * 100%.

[0050] Table 2

[0051]

[0052]

[0053] Table 3

[0054]

[0055] As can be seen from Tables 2 and 3, the product obtained using the technical solution of this invention has excellent acne-removing and oil-controlling effects, with an acne-removing effectiveness rate of over 70%. Further... Figure 1-3 As can be seen from the examples, by using a volunteer from Example 3 for photographic recording, it can be observed that the acne-removing effect of the product of the present invention is significant. In addition, the oil control effect of the product of the present invention after 14 days can reach -46.37%, that is, the oil content is reduced by almost half compared to the initial state. As can be seen from Example 3 and Comparative Examples 1-6, when a certain component of the present invention is not added to the serum, the acne-removing effect and oil control effect are significantly worse. As can be seen from Example 3 and Comparative Example 7, when the content of the added component is not within the range of the present invention, the acne-removing effect and oil control effect of the serum also show a downward trend. As can be seen from Example 3 and Comparative Examples 8 and 9, whether it is Comparative Example 8 which does not add Magnolia officinalis bark extract and Neem leaf extract but makes up the difference with Lonicera japonica flower extract, or Comparative Example 9 which does not add salicylic acid but makes up the difference with azelaic acid, the effect is significantly worse than that of Example 3, indicating that the components added in the present invention have obvious synergistic effects.

[0056] 4. Antibacterial effect test

[0057] (1) Experimental materials:

[0058] 1) Test strain: Propionibacterium acnes (ATCC6919).

[0059] 2) Test samples: The essences obtained in Examples 1-5 and Comparative Examples 1-9 were stored at 4°C for later use.

[0060] 3) Culture medium: Propionibacterium acnes culture medium, adjusted to pH 6.6-7.0. Agar 15g / L is added to the solid culture medium.

[0061] (2) Experimental methods:

[0062] 1) Preparation and inoculation of bacterial suspension: Take 0.1 mL of the frozen bacterial suspension and put it into 5 mL of Propionibacterium acnes liquid culture medium. Incubate under anaerobic conditions at 37℃ for 2 days to obtain the experimental bacterial suspension.

[0063] 2) Preparation of the drug solution: The essences obtained in Examples 1-5 and Comparative Examples 1-9 were serially diluted. The first experiment used serial dilution concentrations of 100% (sample stock solution), 50%, 25%, 12.5%, 6.25%, 3.125%, 1.56%, and 0.78%. The second experiment repeated the serial dilution concentrations at 10%, 8%, 6%, 4%, 2%, and 1%.

[0064] 3) Preparation of bacterial suspension: Dilute the bacterial suspension with Propionibacterium acnes liquid culture medium to achieve a final bacterial concentration of 10. 6 CFU / mL.

[0065] (3) Cultivation and result interpretation

[0066] Add 100 μL of bacterial suspension and 100 μL of drug solution to each microwell. A negative control (without bacterial suspension) and a normal growth control (without drug solution) are also included. Three replicates are performed for each drug, and the average value is taken. Incubate anaerobically at 37℃ for 48 hours, then observe the results. Visual inspection is used to determine the presence of turbidity, and data are read directly. The results are interpreted based on the premise that the growth control is good, the blank control shows clear and sterile growth, and bacterial growth in other wells is inhibited with increasing drug concentration gradient. The results of the first inhibition gradient experiment are shown in Table 4, and the results of the second inhibition gradient experiment are shown in Table 5. "+" indicates bacterial growth, and "-" indicates no growth.

[0067] Table 4

[0068] 100％ 50％ 25％ 12.5％ 6.25％ 3.125％ 1.56％ 0.78％ Example 1 － － － － － － + + Example 2 － － － － － － + + Example 3 － － － － － － + + Example 4 － － － － － + + + Example 5 － － － － + + + + Comparative Example 1 － － + + + + + + Comparative Example 2 － － + + + + + + Comparative Example 3 － － － + + + + + Comparative Example 4 － － － － + + + + Comparative Example 5 － － － － + + + + Comparative Example 6 － － － － + + + + Comparative Example 7 － － － － + + + + Comparative Example 8 － － + + + + + + Comparative Example 9 － － + + + + + +

[0069] Table 5

[0070]

[0071]

[0072] As shown in Table 4, the serums of Examples 1-5, when diluted to a concentration of 12.5% ​​or higher, exhibited good inhibitory effects against *Propionibacterium acnes*. In contrast, the serums of Comparative Examples 3-7 required a dilution of 25% or higher to achieve the desired effect, while Comparative Examples 1, 2, 8, and 9 required concentrations of 50% or higher. Table 5 shows that the antibacterial concentrations of Examples 1-5 were achieved at a 10% dilution, and the antibacterial concentrations of Examples 1-3 were achieved at a 4% dilution. These results indicate that the minimum addition amount of the acne-removing ingredient described in this invention, approximately 10%, is sufficient to effectively inhibit *Propionibacterium acnes*, demonstrating that the serum of this invention can effectively inhibit *Propionibacterium acnes*. Furthermore, the various active ingredients in the serum of this invention, when used in combination, can exert a synergistic effect, enhancing the inhibitory effect on *Propionibacterium acnes*. Additionally, a comparison of the experimental results of Example 3 and Comparative Example 6 revealed that adding soothing active ingredients can also improve antibacterial efficiency.

[0073] Finally, it should be noted that the above embodiments are used to illustrate the technical solutions of the present invention and not to limit the scope of protection of the present invention. Although the present invention has been described in detail with reference to preferred embodiments, those skilled in the art should understand that modifications or equivalent substitutions can be made to the technical solutions of the present invention without departing from the essence and scope of the technical solutions of the present invention.

Claims

1. A serum for clearing acne and controlling oil, characterized in that, The acne-clearing and oil-controlling essence is composed of the following components in parts by weight: 0.3-0.8 parts Magnolia officinalis bark extract, 0.05-1 parts Candida albicans / glucose / methyl rapeseed oil fermentation product, 0.02-0.1 parts Neem leaf extract, 0.5-2 parts Peppermint leaf extract, 0.3-1 parts Lonicera japonica flower extract, 0.2-1 parts azelaic acid, 0.02-0.08 parts glycyrrhetinic acid, 0.5-1.5 parts salicylic acid, and niacinamide. 0.5-1.5 parts, allantoin 0.05-0.15 parts, betaine 0.5-1.5 parts, thickener 0.01-2 parts, pH adjuster 0.01-2 parts, antioxidant 0.2-0.5 parts, humectant 1-25 parts, penetration enhancer 0.01-1 part, solvent 50-100 parts; the penetration enhancer includes at least one of tetrahydropiperine, pentanediol, and isosorbide dimethyl ether; the thickener includes acrylate / C10-30 alkanol acrylate crosspolymer; the pH adjuster includes any one of triethanolamine, arginine, and aminomethylpropanol; the antioxidant is p-hydroxyacetophenone.

2. The acne-clearing and oil-controlling essence according to claim 1, characterized in that, The humectant includes at least one of propylene glycol and 1,2-hexanediol.

3. The preparation method of the acne-clearing and oil-controlling essence as described in claim 1 or 2, characterized in that, Includes the following steps: (1) Mix phase C, heat and stir to obtain mixture I; (2) Mix phase E, heat and stir to obtain mixture II; (3) Mix phase A, heat and stir to homogenize, cool down, then add each component of phase B in sequence and stir evenly to obtain mixture III; (4) After cooling mixture III, add mixture I, mixture II and phase D, and stir evenly; cool to room temperature to obtain acne-clearing and oil-controlling essence; Phase A includes solvents, humectants, allantoin, betaine, and thickeners; Phase B is a pH adjuster; Phase C includes antioxidants and humectants; Phase D includes nicotinamide, Magnolia officinalis bark extract, Candida albicans / glucose / rapeseed oil methyl ester fermentation product, Neem leaf extract, Peppermint leaf extract, and Lonicera japonica flower extract; Phase E includes azelaic acid, glycyrrhetinic acid, salicylic acid, penetration enhancers, and humectants.

4. The method for preparing the acne-clearing and oil-controlling essence according to claim 3, characterized in that, In step (1), the heating temperature is 55-65℃; in step (2), the heating temperature is 50-60℃; in step (3), the heating and stirring homogenization temperature is 80-85℃, and the heating and stirring homogenization time is 5-10 minutes; in step (4), the temperature after cooling is 40-45℃.

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