Gel plaster containing onion extract and its preparation method

Abstract

The present invention discloses a gel plaster containing onion extract and a preparation method thereof. The gel plaster containing onion extract comprises a release liner, a backing layer, and a medicated gel layer. The medicated gel layer is prepared from raw materials including the following components: onion extract, gel matrix, crosslinking agent, crosslinking regulator, pH regulator, penetration enhancer, filler, humectant, surfactant, and water; the penetration enhancer is a combination of azone and propylene glycol; the content of the penetration enhancer is 1.0% - 10.0% of the total weight of the medicated gel layer; the content of the onion extract is 1.0% - 10.0% of the total weight of the medicated gel layer. The gel plaster containing onion extract of the present invention has good skin permeability, can deliver more onion extract, and at the same time has good adhesiveness and is not easily detached during use.

Description

Technical Field

[0001] The present invention belongs to the field of pharmaceutical preparations, and particularly relates to a gel plaster containing onion extract and a preparation method thereof. Background Art

[0002] The formation of scars is often regarded as a sign of clinical healing. In surgical clinical practice, when skin injuries involve the dermis and subcutaneous tissues, wound healing is often accompanied by the formation of scar tissue. There are many factors contributing to scar formation, and there are also many methods for treating scars. However, there is currently no specific and effective therapy. It is necessary to seek a treatment method for scars with a short course of treatment, quick effect, good curative effect, and less pain for patients.

[0003] Onions are rich in phenolic substances, especially quercetin and its glycosides, phenolic acids, organosulfur compounds, vitamins, and minerals. Among them, active ingredients such as phenolic substances, phenolic acids, and organosulfur compounds have significant anti-inflammatory effects. Research shows that in the LPS-induced macrophage inflammation model, onion quercetin can not only promote the dissociation of Nrf2 and Ke-ap1, but also enhance the luciferase activity mediated by ARE in RAW267.4 cells; onion extract can inhibit the growth of various microorganisms such as Staphylococcus, Streptococcus, Vibrio, and Bacillus. At the same time, onion extract can inhibit fibroblasts from various sources, especially those from scars. In addition to inhibiting their mitosis, it can also reduce the synthesis of extracellular matrix such as proteoglycans. Onion extract is mainly used for preventing the formation of scars, improving the symptoms of scars, and anti-inflammatory. Currently, the main dosage forms are gels, creams, patches, and solid preparations, and there is no gel plaster containing onion extract on the market.

[0004] Gel plaster (cataplasm) is prepared by adding drugs to a matrix mainly composed of water-soluble polymer materials through processes such as mixing, coating, and cutting. Compared with other dosage forms, gel plaster has the following advantages: 1. Convenient administration, suitable for patients with difficulties in oral administration or injection, and without irritation; 2. Large drug loading capacity, reducing the number of drug administrations compared with patches; 3. High bioavailability, avoiding the first-pass effect of the liver.

[0005] Therefore, in order to improve the compliance of patients, at the same time, the sticking area is large, it can adapt to the treatment and prevention of larger areas of scars, and improve the clinical drug effect and reduce side effects, it is necessary to develop a gel plaster containing onion extract with good adhesiveness and transdermal absorption effect. Summary of the Invention

[0006] Based on this, the present invention provides a gel plaster containing onion extract, which has good skin permeability, can deliver more onion extract, and has good adhesiveness so that it is not easy to fall off.

[0007] The gel plaster containing onion extract of the present invention includes the following technical solutions.

[0008] A gel plaster containing onion extract, comprising a release liner, a backing layer, and a medicated gel layer, wherein the medicated gel layer is prepared from raw materials including the following components:

[0009] Onion extract, gel matrix, crosslinking regulator, crosslinking agent, pH regulator, penetration enhancer, filler, humectant, surfactant, water;

[0010] The penetration enhancer is a combination of azone and propylene glycol;

[0011] The content of the penetration enhancer is 1.0% - 10.0% of the total weight of the medicated gel layer;

[0012] The content of the onion extract is 1.0% - 10.0% of the total weight of the medicated gel layer.

[0013] In some embodiments, the penetration enhancer is a combination of azone and propylene glycol with a mass ratio of 1:0.8 - 1.2.

[0014] In some embodiments, the content of the penetration enhancer is 4.0% - 8.0% of the total weight of the medicated gel layer.

[0015] In some embodiments, the content of the penetration enhancer is 5.0% - 7.0% of the total weight of the medicated gel layer.

[0016] In some embodiments, the content of the onion extract is 3.0% - 8.0% of the total weight of the medicated gel layer.

[0017] In some embodiments, the content of the onion extract is 4.0% - 6.0% of the total weight of the medicated gel layer.

[0018] In some embodiments, the content of the pH regulator is 0.9% - 1.4% of the total weight of the medicated gel layer.

[0019] In some embodiments, the content of the pH regulator is 1.1% - 1.2% of the total weight of the medicated gel layer.

[0020] In some embodiments, each gram of the medicated gel layer includes the following components by weight:

[0021]

[0022] In some embodiments, each gram of the medicated gel layer includes the following components by weight:

[0023]

[0024]

[0025] In some of these embodiments, each gram of the medicated gel layer comprises components in the following weights:

[0026]

[0027] In some of these embodiments, the gel matrix is selected from at least one of partially neutralized sodium polyacrylate, gelatin, sorbitol, sodium carboxymethylcellulose, polyvinyl alcohol, and carbomer.

[0028] In some of these embodiments, the gel matrix is a combination of partially neutralized sodium polyacrylate, gelatin, and sodium carboxymethylcellulose in a mass ratio of 4 - 5:1.5 - 2.5:1.

[0029] In some of these embodiments, the cross - linker is selected from at least one of aluminum glycinate and aluminum hydroxide.

[0030] In some of these embodiments, the cross - linking regulator is selected from at least one of disodium edetate, citric acid, EDTA, and EDTA - 2Na.

[0031] In some of these embodiments, the pH regulator is selected from at least one of citric acid, tartaric acid, and oleic acid.

[0032] In some of these embodiments, the filler is selected from at least one of kaolin, colloidal silica, zinc oxide, titanium dioxide, talc, and calcium carbonate.

[0033] In some of these embodiments, the humectant is selected from at least one of glycerol, polyethylene glycol, sorbitol, and butanediol.

[0034] In some of these embodiments, the surfactant is polysorbate 80.

[0035] In some of these embodiments, the medicated gel layer further comprises other pharmaceutically acceptable excipients for topical preparations, including but not limited to pigments, flavors, etc.

[0036] In some of these embodiments, each gram of the medicated gel layer comprises components in the following weights:

[0037]

[0038] In some of these embodiments, the backing layer includes but is not limited to one of non - woven fabric, polyester non - woven fabric, polyethylene film, and aluminum foil.

[0039] In some of these embodiments, the anti - sticking layer is but not limited to one of a PET polyester film, a polypropylene film, a polyethylene film, and a paper - polyester composite film coated with paraffin or dimethyl silicone oil.

[0040] The present invention also provides a method for preparing the gel plaster containing onion extract, which includes the following technical solutions.

[0041] A method for preparing a gel plaster containing onion extract includes the following steps:

[0042] A. Add the onion extract to the mixed solvent made of the propylene glycol and an appropriate amount of water, and stir evenly to obtain Phase A;

[0043] B. Dissolve the disodium edetate in the remaining water, then add the tartaric acid and gelatin, heat and stir evenly to obtain Phase B;

[0044] C. Add the partially neutralized sodium polyacrylate, sodium carboxymethylcellulose, kaolin, polysorbate 80, azone and aluminum hydroxide to glycerol in sequence to obtain Phase C;

[0045] D. Mix Phase A and Phase C evenly and then add Phase B, and continue to stir until a uniform medicated gel matrix is obtained;

[0046] E. Coating, cutting and packaging the medicated gel matrix to obtain the gel plaster containing onion extract.

[0047] The present invention provides a gel plaster containing onion extract and a method for preparing the same. In the formula of the gel plaster containing onion extract of the present invention, azone and propylene glycol are selected and used in combination as transdermal penetration enhancers, and the combination of the two has a synergistic effect, so that the active ingredients in the obtained gel plaster containing onion extract have very excellent skin permeability, can deliver more onion extract, improve the clinical efficacy and reduce side effects.

[0048] Furthermore, by adjusting the type and dosage of the pH regulator, the adhesiveness of the obtained gel plaster can be improved, and it can maintain good adhesion. The gel plaster containing onion extract of the present invention has good adhesiveness while having an excellent transdermal absorption effect through the cooperation of each component in specific dosages, is not easy to fall off during use, has very good physical and chemical stability and very little skin irritation.

[0049] The gel plaster containing onion extract of the present invention can be used for the treatment of scars, can prevent scars, have anti-inflammatory effects and improve the appearance of scars. Compared with traditional patches, oral preparations or gels, it provides a more convenient administration form, improves the medication compliance of patients, has the characteristics of convenient use, comfortable application and no skin irritation, and at the same time, its large delivery amount enables it to obtain better clinical efficacy and fewer side effects. Description of the Drawings

[0050] Figure 1Cumulative in vitro permeation amount-time curve of quercetin per unit area in the gel plaster containing onion extract (n = 4). Detailed implementation manners

[0051] The technical solutions of the present invention will be further described below through specific embodiments. Those skilled in the art should understand that the embodiments are only for helping to understand the present invention and should not be construed as specific limitations on the present invention.

[0052] Unless otherwise defined, all technical and scientific terms used in the present invention have the same meanings as those commonly understood by those skilled in the technical field to which the present invention belongs. The terms used in the description of the present invention are only for the purpose of describing specific embodiments and are not used to limit the present invention.

[0053] The terms "comprising" and "having" and any variations thereof in the present invention are intended to cover non-exclusive inclusion. For example, a process, method, device, product or equipment that includes a series of steps is not limited to the listed steps or modules, but optionally further includes steps not listed, or optionally further includes other steps inherent to these processes, methods, products or equipment.

[0054] "Plurality" mentioned in the present invention refers to two or more. "And / or" describes the association relationship of associated objects and indicates that three relationships can exist. For example, A and / or B can represent: A exists alone, A and B exist simultaneously, and B exists alone. The character " / " generally represents an "or" relationship between the associated objects before and after.

[0055] The following are specific embodiments.

[0056] Onion is the bulb of a herbaceous plant in the Liliaceae family. The main bioactive components in onion extract include: ① sulfur-containing compounds: including thiosulfinates, thioethers, thiols, etc., mainly existing in the form of disulfides. ② flavonoid compounds: mainly divided into flavones, flavonols, anthocyanins, etc. Quercetin has strong antioxidant ability and has pharmacological effects such as protecting the brain and cardiovascular system, anti-inflammatory, and antioxidant. ③ polysaccharides include xylose, arabinose, glucose, galactose, galacturonic acid, glucuronic acid. Among them, the effective part with antioxidant and antibacterial biological activities is the best with quercetin. There are various commercially available onion extracts, found in 16 major companies. Taking quercetin as an example, its specifications are 2%, 5%, 10%, etc.

[0057] The onion extract used in the embodiments of the present invention was purchased from Xi'an Ruihe Bioengineering Technology Co., Ltd. The sample property is a brownish-yellow fine powder, packaged in an aluminum foil bag or cardboard barrel, with a quercetin specification of 5%. The active ingredient is mainly quercetin in bioflavonoids, sourced from the fresh stem of Allium cepa in the Liliaceae family, and the extraction method is alcohol extraction. This product should be sealed and protected from light, and stored in a dry, cool and well-ventilated place.

[0058] Example 1

[0059] This example provides a gel plaster containing onion extract, and its prescription composition is shown in the following table:

[0060]

[0061]

[0062] Preparation process:

[0063] A. Add the prescribed amount of onion extract to the mixed solvent made of the prescribed amount of propylene glycol and an appropriate amount of purified water, stir evenly to obtain Phase A;

[0064] B. Dissolve the prescribed amount of disodium edetate in the remaining purified water, then add the prescribed amount of tartaric acid and dissolve, then add gelatin, heat to 40 °C and stir evenly, keep the temperature at 40 °C to obtain Phase B, that is, the aqueous phase;

[0065] C. Add the prescribed amounts of partially neutralized sodium polyacrylate, sodium carboxymethylcellulose, kaolin, polysorbate 80, azone, and aluminum hydroxide to glycerol in sequence to obtain Phase C, that is, the oil phase.

[0066] D. Mix Phase A and Phase C evenly and then add Phase B, continue to stir until a uniform medicated gel matrix is obtained.

[0067] E. Use non-woven fabric as the backing layer and polypropylene embossed film for external plasters as the anti-adhesive layer, and perform processes such as coating, cutting, and packaging on the above medicated gel matrix to obtain a gel plaster containing onion extract.

[0068] Example 2

[0069] This example provides a gel plaster containing onion extract, and its prescription composition is shown in the following table:

[0070]

[0071]

[0072] Preparation process:

[0073] A. Add the prescribed amount of onion extract to the mixed solvent made of the prescribed amount of propylene glycol and an appropriate amount of purified water, stir evenly to obtain Phase A;

[0074] B. Dissolve the prescribed amount of disodium edetate in the remaining purified water, then add the prescribed amount of tartaric acid and dissolve, then add gelatin, heat to 40 °C and stir evenly, keep the temperature at 40 °C to obtain Phase B, that is, the aqueous phase;

[0075] C. Add the partial neutralized sodium polyacrylate, sodium carboxymethyl cellulose, kaolin, polysorbate 80, azone, and aluminum hydroxide in the prescribed amounts to glycerin in sequence to obtain Phase C, i.e., the oil phase.

[0076] D. After uniformly mixing Phase A and Phase C, add Phase B and continue stirring until a uniform drug-containing gel matrix is obtained.

[0077] E. Using non-woven fabric as the backing layer and polypropylene embossed film for external patches as the anti-adhesive layer, subject the above drug-containing gel matrix to processes such as coating, cutting, and packaging to obtain the gel patch containing onion extract.

[0078] Example 3

[0079] This example provides a gel patch containing onion extract, and its prescription composition is shown in the following table:

[0080] Component Prescription ratio (mg / g) Function Onion extract 50 Active ingredient Partially neutralized sodium polyacrylate 65 Gel matrix Gelatin 30.9 Gel matrix Disodium edetate 0.05 Crosslinking regulator Aluminum hydroxide 0.55 Crosslinking agent Tartaric acid 14 pH regulator Azone 30 Transdermal enhancer Propylene glycol 30 Transdermal enhancer Sodium carboxymethyl cellulose 15 Gel matrix Kaolin 50 Filler Glycerol 280.5 Humectant Polysorbate 80 5 Surfactant Purified water 429 N / A

[0081] Preparation process:

[0082] A. Add the onion extract in the prescribed amount to the mixed solvent made of the prescribed amount of propylene glycol and an appropriate amount of purified water, and stir evenly to obtain Phase A.

[0083] B. Dissolve disodium edetate in the remaining purified water in the prescribed amount, then add tartaric acid in the prescribed amount and dissolve it, then add gelatin, heat to 40°C and stir evenly, and keep the temperature at 40°C to obtain Phase B, i.e., the water phase.

[0084] C. Add the partial neutralized sodium polyacrylate, sodium carboxymethyl cellulose, kaolin, polysorbate 80, azone, and aluminum hydroxide in the prescribed amounts to glycerin in sequence to obtain Phase C, i.e., the oil phase.

[0085] D. After uniformly mixing Phase A and Phase C, add Phase B and continue stirring until a uniform drug-containing gel matrix is obtained.

[0086] E. Using non-woven fabric as the backing layer and polypropylene embossed film for external patches as the anti-adhesive layer, subject the above drug-containing gel matrix to processes such as coating, cutting, and packaging to obtain the gel patch containing onion extract.

[0087] Example 4

[0088] This example provides a gel patch containing onion extract, and its prescription composition is shown in the following table:

[0089] Component Prescription ratio (mg / g) Function Onion extract 50 Active ingredient Partially neutralized sodium polyacrylate 65 Gel matrix Gelatin 30.9 Gel matrix Disodium edetate 0.05 Crosslinking regulator Aluminum hydroxide 0.55 Crosslinking agent Tartaric acid 12 pH regulator Sodium carboxymethyl cellulose 15 Gel matrix Kaolin 50 Filler Glycerol 280.5 Humectant Polysorbate 80 5 Surfactant Purified water 491 N / A

[0090] Preparation process:

[0091] A. Dissolve the prescribed amount of onion extract in an appropriate amount of purified water, and stir evenly to obtain Phase A;

[0092] B. Add the prescribed amount of disodium edetate to the remaining purified water and dissolve it. Then add the prescribed amount of tartaric acid and dissolve it. Then add gelatin, heat to 40 °C and stir evenly. Keep the temperature at 40 °C to obtain Phase B, that is, the aqueous phase;

[0093] C. Sequentially add the prescribed amounts of partially neutralized sodium polyacrylate, sodium carboxymethylcellulose, kaolin, polysorbate 80, and aluminum hydroxide to glycerin to obtain Phase C, that is, the oil phase.

[0094] D. Mix Phase A and Phase C evenly and then add Phase B, and continue to stir until a uniform drug-containing gel matrix is obtained.

[0095] E. Use non-woven fabric as the backing layer and polypropylene embossed film for external patches as the anti-adhesive layer, and perform processes such as coating, cutting, and packaging on the above drug-containing gel matrix to obtain a gel plaster containing onion extract.

[0096] Example 5

[0097] This example provides a gel plaster containing onion extract, and its prescription composition is shown in the following table:

[0098]

[0099]

[0100] Preparation process:

[0101] A. Dissolve the prescribed amounts of onion extract and azone in an appropriate amount of purified water, and stir evenly to obtain Phase A;

[0102] B. Add the prescribed amount of disodium edetate to the remaining purified water and dissolve it. Then add the prescribed amount of tartaric acid and dissolve it. Then add gelatin, heat to 40 °C and stir evenly. Keep the temperature at 40 °C to obtain Phase B, that is, the aqueous phase;

[0103] C. Sequentially add the prescribed amounts of partially neutralized sodium polyacrylate, sodium carboxymethylcellulose, kaolin, polysorbate 80, borneol, and aluminum hydroxide to glycerin to obtain Phase C, that is, the oil phase.

[0104] D. Mix Phase A and Phase C evenly and then add Phase B, and continue to stir until a uniform drug-containing gel matrix is obtained.

[0105] E. Use non-woven fabric as the backing layer and polypropylene embossed film for external patches as the anti-adhesive layer, and perform processes such as coating, cutting, and packaging on the above drug-containing gel matrix to obtain a gel plaster containing onion extract.

[0106] Example 6

[0107] This example provides a gel plaster containing onion extract, and its prescription composition is shown in the following table:

[0108]

[0109]

[0110] Preparation process:

[0111] A. Dissolve the prescribed amount of onion extract and azone in an appropriate amount of purified water, and stir evenly to obtain Phase A;

[0112] B. Dissolve the prescribed amount of disodium edetate in the remaining purified water, then add the prescribed amount of tartaric acid and dissolve, then add gelatin, heat to 40 °C and stir evenly, and keep the temperature at 40 °C to obtain Phase B, that is, the aqueous phase;

[0113] C. Sequentially add the prescribed amount of partially neutralized sodium polyacrylate, sodium carboxymethylcellulose, kaolin, polysorbate 80, and aluminum hydroxide to glycerol to obtain Phase C, that is, the oil phase.

[0114] D. Mix Phase A and Phase C evenly and then add Phase B, and continue to stir until a uniform medicated gel matrix is obtained.

[0115] E. Use non-woven fabric as the backing layer and polypropylene embossed film for external patches as the anti-adhesive layer, and perform processes such as coating, cutting, and packaging on the above-mentioned medicated gel matrix to obtain a gel plaster containing onion extract.

[0116] Example 7

[0117] This example provides a gel plaster containing onion extract, and its prescription composition is shown in the following table:

[0118]

[0119]

[0120] Preparation process:

[0121] A. Dissolve the prescribed amount of onion extract and azone in an appropriate amount of purified water, and stir evenly to obtain Phase A;

[0122] B. Dissolve the prescribed amount of disodium edetate in purified water, then add the prescribed amount of tartaric acid and dissolve, then add gelatin, heat to 40 °C and stir evenly, and keep the temperature at 40 °C to obtain Phase B, that is, the aqueous phase;

[0123] C. Sequentially add the prescribed amount of partially neutralized sodium polyacrylate, sodium carboxymethylcellulose, kaolin, polysorbate 80, menthol, and aluminum hydroxide to glycerol to obtain Phase C, that is, the oil phase.

[0124] D. Mix phase A and phase C evenly and then add phase B, and continue stirring until a uniform drug-containing gel matrix is obtained.

[0125] E. Using non-woven fabric as the backing layer and polypropylene embossed film for external patches as the anti-adhesive layer, perform processes such as coating, cutting, and packaging on the above drug-containing gel matrix to obtain a gel patch containing onion extract.

[0126] Example 8

[0127] This example provides a gel patch containing onion extract, and its prescription composition is shown in the following table:

[0128] Component Prescription ratio (mg / g) Function Onion extract 50 Active ingredient Partially neutralized sodium polyacrylate 65 Gel matrix Gelatin 30.9 Gel matrix Disodium edetate 0.05 Crosslinking regulator Aluminum hydroxide 0.55 Crosslinking agent Tartaric acid 12 pH regulator Propylene glycol 30 Transdermal enhancer Menthol 30 Transdermal enhancer Sodium carboxymethyl cellulose 15 Gel matrix Kaolin 50 Filler Glycerol 280.5 Humectant Polysorbate 80 5 Surfactant Purified water 431 N / A

[0129] Preparation process:

[0130] A. Add the prescribed amount of onion extract to a mixed solvent made of the prescribed amount of propylene glycol and an appropriate amount of purified water, and stir evenly to obtain phase A;

[0131] B. Dissolve the prescribed amount of disodium edetate in purified water, then add the prescribed amount of tartaric acid and dissolve, then add gelatin, heat to 40 °C and stir evenly, and keep the temperature at 40 °C to obtain phase B, that is, the aqueous phase;

[0132] C. Sequentially add the prescribed amounts of partial neutralized sodium polyacrylate, sodium carboxymethylcellulose, kaolin, polysorbate 80, menthol, and aluminum hydroxide to glycerol to obtain phase C, that is, the oil phase.

[0133] D. Mix phase A and phase C evenly and then add phase B, and continue stirring until a uniform drug-containing gel matrix is obtained.

[0134] E. Using non-woven fabric as the backing layer and polypropylene embossed film for external patches as the anti-adhesive layer, perform processes such as coating, cutting, and packaging on the above drug-containing gel matrix to obtain a gel patch containing onion extract.

[0135] Example 9

[0136] This example provides a gel patch containing onion extract, and its prescription composition is shown in the following table:

[0137]

[0138]

[0139] Preparation process:

[0140] A. Add the prescribed amount of onion extract to a mixed solvent made of the prescribed amount of propylene glycol and an appropriate amount of purified water, and stir evenly to obtain phase A;

[0141] B. Dissolve the prescribed amount of disodium edetate in purified water, then add the prescribed amount of tartaric acid and dissolve it. Then add gelatin, heat to 40°C and stir evenly. Keep the temperature at 40°C constantly to obtain Phase B, i.e., the aqueous phase.

[0142] C. Add the prescribed amounts of partially neutralized sodium polyacrylate, sodium carboxymethylcellulose, kaolin, polysorbate 80, azone, menthol, and aluminum hydroxide to glycerol in sequence to obtain Phase C, i.e., the oil phase.

[0143] D. Mix Phase A and Phase C evenly, then add Phase B, and continue stirring until a uniform medicated gel matrix is obtained.

[0144] E. Use non-woven fabric as the backing layer and polypropylene embossed film for external patches as the anti-adhesive layer. Perform processes such as coating, cutting, and packaging on the above-mentioned medicated gel matrix to obtain the gel patch containing onion extract.

[0145] Test example: Performance test of the gel patch containing onion extract

[0146] 1. The detection method for initial adhesiveness is as follows: Place the gel patch (together with the packaging material) at 18 - 25°C and relative humidity of 40% - 70% for more than 2 hours. Scrub the surface of the inclined plate and the stainless steel ball with a wiping material dipped in anhydrous ethanol, and carefully dry it with a clean dust-free cloth. Repeat the cleaning process more than 3 times until the surfaces of the inclined plate and the stainless steel ball are visually inspected to be clean. Adjust the inclined plate at an inclination angle of 30°, and keep the base of the experimental device horizontal. Take 3 pieces of the gel patch test samples, and fix the backing of the test samples on the inclined plate with double-sided tape respectively. The upper end of the test sample should be located at the position of two horizontal lines 10 mm apart on the inclined plate, and the upper line is the starting position of the steel ball. The test sample should be flatly attached to the plate. After removing the cover liner of the test sample, complete the test as soon as possible, leaving a 5 cm gap in the middle of the paste surface. Place steel balls of different numbers on the starting line in sequence and let them freely fall from the top of the inclined plane, and record the largest steel ball number that can be adhered.

[0147] The detection results show that the largest ball numbers that the gel patch containing onion extract prepared in Example 1 of the present invention can adhere to are balls numbered 16 - 19, while the largest ball numbers that the gel patches containing onion extract prepared in Examples 2 - 3 can adhere to are balls numbered 9 - 12.

[0148] 2. The method for detecting the holding adhesion is as follows: Place the gel plaster at 18-25°C and relative humidity of 40%-70% for more than 2 hours. Clean the surfaces of the test plate and the loading plate. After cleaning, the test plate and the loading plate must not be touched by hand or other objects. Take the gel plaster containing onion extract of the present invention, and stick the gel plaster longitudinally parallel to the plate in the middle of the adjacent test plate and loading plate. Roll a roller back and forth on the test sample three times. After the test sample is stuck on the plate, let it stand at room temperature for 20 minutes, fix it on the test rack, and record the starting time and position of the test.

[0149] The test results show that the peeling time of the gel plaster containing onion extract prepared in Example 1 of the present invention exceeded 24 hours, while the peeling time of the gel plaster containing onion extract prepared in Example 3 was 20 hours, and the peeling time of the gel plaster containing onion extract prepared in Example 2 was 15 hours.

[0150] From the above experimental results, it can be seen that the gel plaster obtained when the proportion of tartaric acid in the prescription is 1.2% has the best adhesion (holding adhesion). The order of the adhesion (holding adhesion) strength of the gel plasters with different tartaric acid contents is: 1.2% > 1.4% > 1.0%. Experiments have proved that different contents of tartaric acid affect the adhesion of the gel plaster. This is because when the amount of tartaric acid is insufficient, the release of aluminum ions is insufficient and the reaction is incomplete; when the amount of tartaric acid is too much, the acidity is too strong, resulting in too fast an adhesive reaction, an increase in the cohesive force inside the paste, and a decrease in the surface holding adhesion; when the amount of tartaric acid is appropriate, the adhesive reaction speed is moderate, which can fully adhere and increase the initial adhesion and holding adhesion of the gel plaster. From the experimental results, it can be seen that when the proportion of tartaric acid reaches 1.2%, the initial adhesion and holding adhesion of the obtained gel plaster reach the peak.

[0151] 3. In vitro transdermal test:

[0152] The diffusion cell method is adopted, using the pig skin of Bama miniature pigs as a barrier, and the gel plasters containing onion extract prepared in Examples 1, 4-6 are used for in vitro transdermal tests.

[0153] The transdermal conditions include: release medium: pH 7.4; device: diffusion cell method; sampling time: 2h, 4h, 6h, 8h, 12h, 16h, 20h, 24h; sampling mode: full discharge and full replenishment; medium volume: 9 ml; medium temperature: 32°C.

[0154] The calculation formula is as follows:

[0155] <![CDATA[(1)C S =(m×P) / V1]]> <![CDATA[(2) f = C S / A S > <![CDATA[(3) Release amount per unit area (μg / cm 2 ) = (f × A X × V 溶媒 × 1000) / S 取样 > <![CDATA[(4) Cumulative release amount per unit area (μg / cm 2 ) = ∑ Release amount per unit area]]> <![CDATA[(5) Cumulative permeation amount (%) = ∑(f × A X × V 溶媒 ) × 100 / m 取样 > <![CDATA[(6) Paste residue amount, intradermal retention amount, concomitant content (%) = f × A X × V2 / m 取样 > <![CDATA[C S : Concentration of reference solution, mg / ml <!-- 15 -->]]> m: Sampling amount, mg P: Purity of reference substance <![CDATA[V1: Dilution volume of reference substance solution, ml]]> f: Correction factor of reference substance solution <![CDATA[V2: Dilution volume of the test solution, ml]]> <![CDATA[A S : Peak area of reference solution]]> <![CDATA[A X: Peak area of the test solution]]> <![CDATA[V 溶媒 : Volume of dissolution medium released from the sample]]> <![CDATA[S 取样 : Sampling area of the sample]]> <![CDATA[m 取样 : Labeled amount of sample sampling area]]>

[0156] The measurement method is as follows:

[0157] During the experiment, the pigskin was taken out of the refrigerator and thawed, cooled to room temperature, dried, and the transdermal water loss value of the pigskin was measured with a transdermal water loss analyzer. Then it was washed with normal saline, the surface moisture was blotted dry with filter paper, and the thickness of the pigskin was measured with a caliper. A plaster with a diameter of 14 mm was cut, the film was removed, and the sample was applied to the center of the pigskin. The pigskin was laid flat on the diffusion cell. After fixed installation, an appropriate amount of release medium was added, and the rotation speed was set at 600 rpm and the constant temperature was 32 °C. 9 ml of the release medium was absorbed at 2, 4, 6, 8, 12, 16, 20, and 24 h after administration, and an equal amount of receiving solution was added at the same time. The cumulative permeation amount was calculated, and the test results are shown in Table 1 and Figure 1 as shown.

[0158] Table 1 Transdermal penetration parameters of quercetin in the gel plaster containing onion extract (n = 4)

[0159] Group <![CDATA[Cumulative Throughput (μg / cm 2 )]]> <![CDATA[Steady-state permeation rate (μg·cm 2 / h)]]> Example 1 93.10±0.12 4.45±0.09 Example 4 30.16±0.12 1.44±0.22 Example 5 37.10±0.15 1.77±0.15 Example 6 45.10±0.20 2.16±0.30 Example 7 60.10±0.11 2.87±0.20 Example 8 55.27±0.07 2.64±0.10 Example 9 75.13±0.09 3.59±0.20

[0160] Result analysis: The penetration enhancer used in Example 1 was azone + propylene glycol, Example 4 did not use a penetration enhancer, the penetration enhancer used in Example 5 was azone + borneol, the penetration enhancer used in Example 6 was azone, the penetration enhancer used in Example 7 was azone + menthol, the penetration enhancer used in Example 8 was propylene glycol + menthol, and the penetration enhancer used in Example 9 was azone + propylene glycol + menthol; from the results of the in vitro transdermal test, the comparison result of the cumulative in vitro permeation amount per unit area of quercetin was: Example 1 > Example 9 > Example 7 > Example 8 > Example 6 > Example 5 > Example 4; in terms of the steady-state permeation rate, Example 1 was significantly better than other examples; therefore, using azone + propylene glycol as the penetration enhancer can more effectively promote the transdermal absorption of the active ingredients in the gel plaster containing onion extract, so as to achieve better clinical efficacy.

[0161] The technical features of the above-described embodiments can be combined arbitrarily. For the sake of brevity of description, not all possible combinations of the technical features in the above embodiments are described. However, as long as there is no contradiction in the combination of these technical features, it should be considered as the scope described in this specification.

[0162] The above-described embodiments only represent several implementation manners of the present invention, and their descriptions are relatively specific and detailed, but they should not be construed as limiting the scope of the invention patent. It should be noted that for those of ordinary skill in the art, without departing from the concept of the present invention, several modifications and improvements can still be made, and these all belong to the protection scope of the present invention. Therefore, the protection scope of the present invention patent should be subject to the appended claims.

Claims

1. A gel plaster containing onion extract, characterized in that, It includes an anti-adhesive layer, a backing layer, and a medicated gel layer, and the medicated gel layer is prepared from the following raw materials: Onion extract, gel matrix, cross-linking agent, cross-linking regulator, pH regulator, transdermal enhancer, filler, humectant, surfactant, water; The weight of each component in every gram of the medicated gel layer is as follows: The transdermal enhancer is a combination of azone and propylene glycol with a mass ratio of 1:0.8 - 1.2; The pH regulator is tartaric acid; The gel matrix is a combination of partially neutralized sodium polyacrylate, gelatin, and sodium carboxymethylcellulose with a mass ratio of 4 - 5:1.5 - 2.5:1; The cross-linking agent is aluminum hydroxide; The cross-linking regulator is disodium edetate.

2. The gel plaster containing onion extract according to claim 1, characterized in that, The content of the pH regulator is 1.2% of the total weight of the medicated gel layer.

3. The gel patch containing onion extract according to claim 1, wherein The filler is selected from at least one of kaolin, microcrystalline silica, zinc oxide, titanium dioxide, talc powder, and calcium carbonate; and / or, The humectant is selected from at least one of glycerol, polyethylene glycol, sorbitol, and butanediol; and / or, The surfactant is polysorbate 80; and / or, The backing layer is one of non-woven fabric, polyester non-woven fabric, polyethylene film, and aluminum foil; and / or, The anti-adhesive layer is one of PET polyester film, polypropylene film, polyethylene film, and paper-polyester composite film coated with paraffin or dimethyl silicone oil.

4. The gel plaster containing onion extract according to claim 1, characterized in that Every gram of the medicated gel layer is composed of components with the following weights: 。 5. A method for preparing the gel plaster containing onion extract according to claim 4, characterized in that, It includes the following steps: A. Add the onion extract into the mixed solvent made of the propylene glycol and an appropriate amount of water, and stir evenly to obtain phase A; B. Dissolve the disodium edetate in the remaining water, then add the tartaric acid and gelatin, heat and stir evenly to obtain phase B; C. Sequentially add the partially neutralized sodium polyacrylate, sodium carboxymethylcellulose, kaolin, polysorbate 80, azone, and aluminum hydroxide into glycerol to obtain phase C; D. Mix phase A and phase C evenly and then add phase B, and continue to stir until a uniform medicated gel matrix is obtained; E. Coat, cut, and package the medicated gel matrix to obtain the gel patch containing onion extract.

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