Scar repairing and itching relieving liniment in technical field of scar treatment and preparation process of scar repairing and itching relieving liniment

Abstract

The invention relates to the technical field of scar treatment, and particularly discloses a scar repairing and itching relieving liniment and a preparation process in the technical field of scar treatment. Comprising octamethylcyclotetrasiloxane, decamethylcyclopentasiloxane, cyclopentasiloxane, phenyl polytrimethylsiloxane, polymethylsilsesquioxane, an eucalyptus globulus extract, ascorbic acid laurocapram ester, a solvent, a plasticizer and polyvinyl alcohol. Through the synergistic effect of the eucalyptus globulus extract and the ascorbyl laurocapram ester, pruritus feeling caused by scars can be rapidly relieved, scar tissue repair can be effectively promoted, meanwhile, powerful anti-inflammatory and moisturizing functions are achieved, and the limitation that a traditional silicone product is single in function is remarkably improved.

Description

Technical Field

[0001] The present invention belongs to the technical field of scar treatment, and particularly relates to a scar repair and itching-relieving coating agent in the technical field of scar treatment and a preparation process thereof. Background Technique

[0002] The current mainstream technologies in the field of scar treatment mainly include silicone gel topical preparations, corticosteroid local injections, pressure therapy, and the application of some natural ingredients. Silicone gel reduces the water loss of scars through physical occlusion and is the most widely used non-invasive therapy in clinical practice.

[0003] However, the existing technologies have significant limitations. Although silicone gel can improve the appearance of scars, its functions of relieving itching, anti-inflammation, and promoting regeneration are weak, and it cannot meet the multi-dimensional treatment needs of complex scars. Summary of the Invention

[0004] The purpose of the present invention is to provide a scar repair and itching-relieving coating agent in the technical field of scar treatment and a preparation process thereof to solve the problems raised in the above background technique.

[0005] To achieve the above purpose, the present invention provides the following technical solutions:

[0006] A scar repair and itching-relieving coating agent in the technical field of scar treatment, calculated by weight, comprises the following raw material components:

[0007] Octamethylcyclotetrasiloxane 10 - 20 parts, decamethylcyclopentasiloxane 10 - 30 parts, cyclopentapoly(dimethylsiloxane) 10 - 30 parts, phenyltrimethylsiloxane 10 - 30 parts, polymethylsilsesquioxane 10 - 20 parts, eucalyptus extract 1 - 15 parts, laurocapram ascorbate 10 - 20 parts, solvent 600 - 1000 parts, plasticizer 60 - 140 parts, polyvinyl alcohol 80 - 150 parts.

[0008] Preferably, the solvent is one or a mixture of more of ethanol, propylene glycol, or deionized water.

[0009] Preferably, the plasticizer is one or a mixture of more of glycerol, propylene glycol, or phthalate compounds.

[0010] Preferably, the preparation method of laurocapram ascorbate comprises the following steps:

[0011] A1. Add laurocapram to dichloromethane, slowly drop thionyl chloride under ice bath conditions, and stir and react at room temperature for 1 - 2 hours to generate laurocapram acyl chloride;

[0012] A2. Dissolve ascorbic acid in pyridine, and slowly add dropwise the dichloromethane solution of laurocapramoyl chloride obtained in step A1 under ice bath. Start the reaction at 0 - 5 °C, and after raising the temperature to room temperature, stir for 24 - 48 hours to form a mixture of ascorbyl laurocapram.

[0013] A3. Pour the mixture obtained in step A2 into ice water, extract with dichloromethane, combine the organic phases, then dry, filter, concentrate, and purify by silica gel column chromatography, eluting with a mixed solvent of ethyl acetate - petroleum ether to obtain purified ascorbyl laurocapram.

[0014] Preferably, the molar amount of thionyl chloride in step A1 is 1.0 - 1.2 times that of laurocapram.

[0015] Preferably, the molar ratio of ascorbic acid to laurocapramoyl chloride in step A2 is 1:1 - 1.2.

[0016] Preferably, the volume ratio of ethyl acetate to petroleum ether in step A3 is 1:3 - 1:5.

[0017] A preparation process of a scar - repairing and itching - relieving coating agent in the field of scar treatment technology, comprising the following steps:

[0018] Mix octamethylcyclotetrasiloxane, decamethylcyclopentasiloxane, cyclopentasiloxane, phenyltrimethylsiloxane, polymethylsilsesquioxane with a solvent, heat to 40 - 60 °C and stir to dissolve, add a plasticizer and polyvinyl alcohol, and after cooling to room temperature, add eucalyptus extract and ascorbyl laurocapram, and homogenize to form a gel.

[0019] Preferably, the homogenization condition is stirring at 5000 - 8000 rpm for 10 - 30 minutes.

[0020] Compared with the prior art, the beneficial effects of the present invention are:

[0021] (1) Through the synergistic effect of eucalyptus extract and ascorbyl laurocapram, it can not only quickly relieve the itching caused by scars, but also effectively promote the repair of scar tissue, and at the same time has strong anti - inflammatory and moisturizing functions, significantly improving the limitation of the single function of traditional silicone products.

[0022] (2) The flexible coating film formed has strong adhesion, high stability, no delamination phenomenon after long - term storage, and has high transdermal absorption ability, ensuring that the active ingredients reach the deep tissues directly. Brief Description of the Drawings

[0023] Figure 1 It is the process flow chart of the present invention. Detailed Embodiments

[0024] Next, the technical solutions in the embodiments of the present invention will be clearly and completely described in conjunction with the accompanying drawings in the embodiments of the present invention. Obviously, the described embodiments are only a part of the embodiments of the present invention, rather than all the embodiments. All other embodiments obtained by those of ordinary skill in the art based on the embodiments of the present invention without creative efforts shall fall within the protection scope of the present invention.

[0025] Embodiment 1:

[0026] The preparation of ascorbyl laurocapram includes the following steps:

[0027] Step A1: Dissolve 10 g of laurocapram in 100 mL of dichloromethane, and cool it to 0 °C in an ice bath; slowly add thionyl chloride (the molar amount is 1.1 times that of laurocapram), and stir and react at room temperature for 1.5 hours after dropping to form laurocapram acyl chloride.

[0028] Step A2: Dissolve 8 g of ascorbic acid in 50 mL of pyridine, and cool it to 0 °C in an ice bath; slowly add the dichloromethane solution of laurocapram acyl chloride obtained in Step A1 (the molar ratio of ascorbic acid to laurocapram acyl chloride is 1:1.05); the initial reaction temperature is 0 - 5 °C, and then it is heated to room temperature, and stir and react for 36 hours to form a mixture of ascorbyl laurocapram.

[0029] Step A3: Pour the reaction mixture into 200 mL of ice water, extract it with dichloromethane (3 × 50 mL), combine the organic phases, add anhydrous sodium sulfate for drying; filter and then concentrate under reduced pressure, purify it by silica gel column chromatography (the eluent is ethyl acetate - petroleum ether, volume ratio 1:4), collect the target component, and obtain 12.5 g of white powdery ascorbyl laurocapram after drying.

[0030] Embodiment 2:

[0031] The preparation of Eucalyptus globulus extract includes the following steps:

[0032] Crush the dried Eucalyptus globulus leaves to 40 meshes, put them into the extraction kettle, set the extraction pressure at 25 MPa, the temperature at 45 °C, the CO2 flow rate at 20 L / h, and the extraction time at 2 hours; the separation kettle pressure is 6 MPa, the temperature is 35 °C, collect the extract to obtain the Eucalyptus globulus extract.

[0033] Embodiment 3:

[0034] The preparation of the repair gel includes:

[0035] Select 15 parts of octamethylcyclotetrasiloxane, 20 parts of decamethylcyclopentasiloxane, 25 parts of cyclopentapoly(dimethylsiloxane), 20 parts of phenylpolytrimethylsiloxane, 15 parts of polymethylsilsesquioxane, 8 parts of blue gum extract, 15 parts of ascorbyl laurocapram, 800 parts of ethanol (solvent), 100 parts of glycerol (plasticizer), and 120 parts of polyvinyl alcohol;

[0036] Mix octamethylcyclotetrasiloxane, decamethylcyclopentasiloxane, cyclopentapoly(dimethylsiloxane), phenylpolytrimethylsiloxane, and polymethylsilsesquioxane with ethanol, heat to 50 °C and stir until completely dissolved; add glycerol and polyvinyl alcohol, continue stirring until homogeneous, and cool to 25 °C; add blue gum extract and ascorbyl laurocapram, transfer to a homogenizer, and homogenize and stir at 6000 rpm for 20 minutes to form a transparent gel.

[0037] Example 4:

[0038] Replace the solvent with propylene glycol and deionized water (3:7, volume ratio), select 60 parts of diethyl phthalate as the plasticizer, and the remaining raw materials are the same as in Example 3. The viscosity and moisture retention performance of the prepared gel are comparable to those of Example 3.

[0039] Comparative Example 1: Traditional silicone gel

[0040] The formula includes polydimethylsiloxane (silicone matrix), glycerol (plasticizer), and ethanol (solvent);

[0041] The preparation process is to mix and dissolve the silicone matrix with the solvent and then add the plasticizer, and homogenize and stir (3000 rpm, 10 minutes).

[0042] Comparative Example 2: The formula of the present invention without blue gum extract and ascorbyl laurocapram

[0043] The formula includes retaining the silicone matrix (octamethylcyclotetrasiloxane, decamethylcyclopentasiloxane, etc.), but removing the blue gum extract and ascorbyl laurocapram, and other components are the same as in Example 3;

[0044] The preparation process is the same as that of Example 3 and will not be elaborated here.

[0045] Application comparative example:

[0046] Compare Example 3 of the present invention with Comparative Example 1 and Comparative Example 2 in terms of anti-itching effect, scar repair rate, moisture retention performance, anti-inflammatory effect, film-forming performance, gel stability, and transdermal absorption efficiency. The specific data are as follows:

[0047]

[0048] Anti-itching effect: Visual analogue scale (VAS, 0-10 points) is used, and the lower the value, the lighter the itching sensation;

[0049] Scar repair rate: The percentage of scar area reduction measured by laser scanning (4-week usage period);

[0050] TEWL (Trans-epidermal water loss): The lower the value, the better the moisturizing performance;

[0051] Anti-inflammatory effect: The inhibition rate of TNF-α inflammatory factor determined by in vitro cell experiments;

[0052] Transdermal absorption efficiency: Fluorescently labeled active ingredients were used to measure the transdermal absorption rate within 24 hours (based on Comparative Example 3).

[0053] As can be seen from the above, eucalyptus extract and laurocapram ascorbate significantly improve anti-inflammatory and repair properties. The present invention is comprehensively superior to traditional formulations and simplified schemes in terms of antipruritic, repair, moisturizing and film-forming properties.

[0054] Although the embodiments of the present invention have been shown and described, it will be understood by those of ordinary skill in the art that various changes, modifications, substitutions and variations can be made to these embodiments without departing from the principles and spirit of the present invention. The scope of the present invention is defined by the appended claims and their equivalents.

Claims

1. A scar repair and itching-relieving coating agent in the technical field of scar treatment, characterized in that, By weight, it includes the following raw material components: Octamethylcyclotetrasiloxane 10 - 20 parts, decamethylcyclopentasiloxane 10 - 30 parts, cyclopentadimethylsiloxane 10 - 30 parts, phenyltrimethylsiloxane 10 - 30 parts, polymethylsilsesquioxane 10 - 20 parts, blue eucalyptus extract 1 - 15 parts, ascorbyl laurocapram 10 - 20 parts, solvent 600 - 1000 parts, plasticizer 60 - 140 parts, polyvinyl alcohol 80 - 150 parts.

2. The scar repair and itching relief coating agent in the field of scar treatment technology according to claim 1, wherein: The solvent is one or a mixture of ethanol, propylene glycol or deionized water.

3. The anti-itch coating agent for scar repair in the technical field of scar treatment according to claim 1, characterized in that: The plasticizer is one or a mixture of glycerol, propylene glycol or phthalate compounds.

4. A scar repair and itching relief coating agent in the technical field of scar treatment according to claim 1, characterized in that, The preparation method of the ascorbyl laurocapram includes the following steps: A1. Add laurocapram to dichloromethane, slowly drop thionyl chloride under ice bath conditions, and stir at room temperature for 1 - 2 hours to generate laurocapram acyl chloride; A2. Dissolve ascorbic acid in pyridine, slowly drop the dichloromethane solution of laurocapram acyl chloride obtained in step A1 under ice bath, start the reaction at 0 - 5 °C, warm up to room temperature and then stir for 24 - 48 hours to generate a mixture of ascorbyl laurocapram; A3. Pour the mixture obtained in step A2 into ice water, extract with dichloromethane, combine the organic phases, dry, filter, concentrate, and purify by silica gel column chromatography, elute with an ethyl acetate - petroleum ether mixed solvent to obtain purified ascorbyl laurocapram.

5. A scar repair and itching relief coating agent in the technical field of scar treatment according to claim 4, characterized in that: In step A1, the molar amount of thionyl chloride is 1.0 - 1.2 times that of laurocapram.

6. The anti-itch coating agent for scar repair in the field of scar treatment technology according to claim 4, characterized in that: In step A2, the molar ratio of ascorbic acid to laurocapram acyl chloride is 1:1 - 1.

2.

7. A scar repair and itching relief coating agent in the technical field of scar treatment according to claim 4, characterized in that: In step A3, the volume ratio of ethyl acetate to petroleum ether is 1:3 - 1:

5.

8. A preparation process of a scar repair and itching-relieving coating agent in the field of scar treatment technology, characterized in that, It includes the following steps: Mix octamethylcyclotetrasiloxane, decamethylcyclopentasiloxane, cyclopentadimethylsiloxane, phenyltrimethylsiloxane, polymethylsilsesquioxane with the solvent, heat to 40 - 60 °C and stir to dissolve, add the plasticizer and polyvinyl alcohol, cool to room temperature, then add the blue eucalyptus extract and ascorbyl laurocapram, and homogenize to form a gel.

9. The preparation process of a scar repair and itching-relieving coating agent in the technical field of scar treatment according to claim 8, characterized in that: The homogenization conditions are stirring at 5000 - 8000 rpm for 10 - 30 minutes.

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