A medical cataplasm hydrogel composition for transdermal absorption and a method for preparing the same

Abstract

This invention discloses a medical poultice hydrogel composition for transdermal absorption and its preparation method, belonging to the field of medical dressings and transdermal drug delivery technology. By weight, the composition comprises: Phase A: 15-25 parts glycerin, 5-8 parts sodium polyacrylate, 0.1-0.2 parts aluminum glycine, 0.05-0.15 parts disodium EDTA, 0.3-0.8 parts 1,2-hexanediol, and 0.05-0.2 parts sodium hyaluronate; Phase B: 60-80 parts purified water, 0.3-0.8 parts p-hydroxyacetophenone, 0.05-0.15 parts tartaric acid, and 0.5-1.5 parts polyacrylic acid; the total content of active ingredients is 0.01-0.1 parts, selected from one or more of acetyl hexapeptide-8, hydroxypropyl tetrahydropyranotriol, dipeptide diaminobutyryl benzylamide diacetate, superoxide dismutase, fibronectin, retinol, sodium DNA, and collagen; the remainder being pharmaceutical excipients. The preparation method includes weighing and verification, separate premixing of phases A and B, mixing in a main pot, coating, slitting, packaging, and inspection before warehousing. This composition exhibits good transdermal absorption, strong adhesion, and high stability, making it suitable for anti-wrinkle, repair, and moisturizing effects on facial skin folds such as nasolabial folds.

Description

Technical Field

[0001] This invention belongs to the field of medical dressings and transdermal drug delivery technology, specifically relating to a poultice hydrogel composition for the face (especially facial skin folds such as nasolabial folds) and its preparation method. Background Technology

[0002] Hydrogel patches are widely used in medical dressings and cosmetic patches due to their good biocompatibility, breathability and sustained-release properties. Hydrogel patches, also known as modern patches, are made by mixing water-soluble polymer materials and therapeutic drugs into a main matrix, coating it onto non-woven fabric and then molding it. Hydrophilic patches have received much attention in recent years due to their advantages such as good moisturizing properties, low allergy, non-adhesion to the skin, convenient application and easy transdermal drug absorption. Existing hydrogel patches have the following shortcomings: (1) low transdermal absorption efficiency, and active ingredients are difficult to effectively penetrate into the deep layers of the skin; (2) Insufficient adhesion and fit, especially for skin folds such as nasolabial folds, traditional patches are difficult to adhere tightly and the active ingredients are difficult to act evenly on the target skin area; (3) High skin irritation; some preservative systems or cross-linking agents are not friendly to sensitive skin; (4) Poor storage stability; the gel is prone to dehydration, separation, or microbial contamination. (5) The preparation process is poorly adapted to the production scale, and it is difficult to guarantee the consistency of quality of the same formula under different batch conditions.

[0003] Therefore, there is an important clinical and market demand for developing a medical poultice hydrogel with good transdermal absorption, soft and conformable texture, high stability, and suitability for large-batch preparation. Summary of the Invention

[0004] The present invention aims to provide a poultice hydrogel composition and its preparation method that has good transdermal absorption properties, is soft and fits well, has high stability and is suitable for mass industrial production, and is particularly suitable for anti-wrinkle, repair and moisturizing purposes in facial skin folds such as nasolabial folds. Technical solution

[0005] This invention provides a medical poultice hydrogel composition for transdermal absorption, comprising the following components by weight:

[0006] • Glycerin: 15-25 parts • Sodium polyacrylate: 5-8 parts • Aluminum glycine: 0.1-0.2 parts • Disodium EDTA: 0.05-0.15 parts • 1,2-Hexanediol: 0.3-0.8 parts • Sodium hyaluronate: 0.05-0.2 parts

[0007] • Purified water: 60-80 parts • p-Hydroxyacetophenone: 0.3-0.8 parts • Tartaric acid: 0.05-0.15 parts • Polyacrylic acid: 0.5-1.5 parts

[0008] Selected from acetyl hexapeptide-8, hydroxypropyl tetrahydropyranotriol, dipeptide diaminobutyryl benzylamide diacetate, superoxide dismutase (SOD), fibronectin, retinol, hydroxypinazone retinate, One or more of sodium DNA and collagen, with a total content of 0.01-0.1 parts.

[0009] Pharmaceutical excipients: selected from one or more of propylene glycol, polysorbate-80, ethylhexylglycerin, cetearyl alcohol, polysorbate-60, butylated hydroxytoluene, and phenoxyethanol, with the amount used being the balance. Beneficial effects

[0010] 1. Excellent transdermal absorption performance: This invention utilizes the synergistic effect of sodium hyaluronate and sodium polyacrylate in phase A, combined with the pH adjustment function of polyacrylic acid in phase B, to give the hydrogel matrix good hydrophilicity and skin permeability, allowing the active ingredients to effectively penetrate deep into the skin.

[0011] 2. Strong Adhesion: The soft structure of the patch, combined with the high moisturizing properties of glycerin, allows the hydrogel patch to adhere closely to complex skin folds such as nasolabial folds, ensuring that the active ingredients are evenly covered in the target area.

[0012] 3. Synergistic anti-wrinkle effect of multiple active ingredients: Acetyl hexapeptide-8, dipeptide diaminobutyryl benzylamide diacetate, SOD, fibronectin, collagen and other multiple components are combined to exert anti-wrinkle and repair effects through multiple pathways.

[0013] 4. The compound preservative system is mild and effective: the combination of 1,2-hexanediol and p-hydroxyacetophenone has a good broad-spectrum antibacterial effect, while avoiding skin irritation that may be caused by traditional preservatives.

[0014] 5. High stability: The cross-linking network formed by disodium EDTA complexing metal ions, aluminum glycinate, and sodium polyacrylate enhances the cohesive strength of the gel, ensuring the product remains stable over a wide temperature range and has a long shelf life.

[0015] 6. Batch process parameter control: Different mixing equipment and parameters are used according to different production batches to ensure the consistency of product quality in each batch, which is suitable for industrial scale-up production.

[0016] 7. Good safety: Microbial indicators are strictly controlled and there is no skin irritation.

[0017] Includes the following steps: 1. Weighing: Weigh each phase of material separately using an electronic scale with the specified accuracy according to the production order, and double-check the weighing.

[0018] 2. A phase mixing: At room temperature, add the A phase raw material to the premixing tank and stir until evenly mixed.

[0019] 3. Phase B mixing: At room temperature, add the Phase B raw material to another premixing tank and stir to disperse it evenly.

[0020] 4. Mixing in the main pot: Pour the mixed phase B liquid into the main pot, then pour in the mixed phase A liquid, and stir well.

[0021] 5. Coating and Slitting: Coat the well-stirred gel onto nonwoven fabric or membrane fabric, and cut it into the desired shape. The coating temperature should be controlled at 18-26℃.

[0022] 6. Packaging: In accordance with the production order requirements, inkjet printing, labeling, boxing, heat shrinking, and cartoning are performed.

[0023] 7. Inspection and warehousing: Sampling shall be carried out in accordance with the sampling procedure, and the finished products shall be inspected and qualified before being put into storage.

[0024] Small batch (≤2kg) electric mixer 80-1400 RPM, gradually increasing speed No less than 5 minutes Medium batch (2-50kg) hand blender 150 RPM No less than 10 minutes Large quantities (≥50kg) Vacuum homogenizing emulsifying mixer 15-50 Hz No less than 20 minutes

[0025] • Appearance: Transparent solid gel adhered to a white membrane. • Aroma: Meets the specified aroma requirements, exhibiting characteristic odors of the raw materials. Physicochemical indicators: • pH value: 4.0–8.5 • Heat resistance: After being kept at (40±1)℃ for 24 hours, there was no significant difference compared to the test results after returning to room temperature. • Cold resistance: After being kept at (-8±2)℃ for 24 hours, there was no significant difference compared to the pre-test temperature after returning to room temperature.

[0026] • Total bacterial count: ≤1000 CFU / g • Total mold and yeast count: ≤100 CFU / g

[0027] • Net content: Complies with JJF1070-2005 "Rules for Measurement and Inspection of Net Content of Prepackaged Commodities" • Packaging appearance: Complies with QB / T1685 standards

[0028] Weighing and preparing Actual value ÷ Theoretical value × 100% 95%-103% Coating and Slitting Actual value ÷ Theoretical value × 100% >40% Inner packaging (Number of qualified products + Number of unqualified products) ÷ Quantity issued × 100% 95%-105% Outer packaging (Number of qualified products + Number of unqualified products) ÷ Quantity issued × 100% 95%-105% The following is the preparation process of the hydrogel patch of the present invention.

[0029] Process flow: Weighing → A phase mixing / B phase mixing → Main pot mixing → Coating and slitting → Packaging → Inspection → Warehousing. Detailed Implementation

[0030] The present invention is further illustrated below with reference to specific embodiments, but the present invention is not limited to these embodiments. Example

[0031] Prepare the hydrogel composition according to the following parts by weight:

[0032] • Glycerin: Approximately 20 parts • Sodium polyacrylate: Approximately 6 parts • Aluminum glycine: Approximately 0.14 parts • Disodium EDTA: Approximately 0.10 parts • 1,2-Hexanediol: Approximately 0.50 parts • Sodium hyaluronate: Approximately 0.11 parts

[0033] • Purified water: Approximately 72 parts • p-Hydroxyacetophenone: Approximately 0.50 parts • Tartaric acid: approx. 0.10 parts • Polyacrylic acid: approx. 1.00 parts

[0034] • Acetyl hexapeptide-8: Trace amounts • Hydroxypropyltetrahydropyranotriol: Trace amounts • Dipeptide diaminobutyryl benzylamide diacetate: trace amounts • Superoxide dismutase (SOD): Trace amounts • Fibronectin: trace amounts • Sodium DNA: Trace amounts • Collagen: Trace amounts • Propylene glycol, polysorbate-80, ethylhexylglycerin: appropriate amount

[0035] 1. Weighing: Accurately weigh each ingredient according to the above formula, and double-check the weighing.

[0036] 2. Phase A mixing: Add the Phase A material to the premixing tank at room temperature and stir until evenly mixed.

[0037] 3. B phase mixing: Add the B phase material to another premixing tank at room temperature and stir to disperse evenly.

[0038] 4. Mixing in the main pot: Add phase B liquid to the main pot, followed by phase A liquid, and mix for an appropriate time using a vacuum homogenizing emulsifier.

[0039] 5. Coating and slitting: Coat the uniformly mixed hydrogel onto the nonwoven fabric at an appropriate temperature and cut it into the required shape (such as nasolabial fold patches).

[0040] 6. Packaging: inkjet printing, labeling, boxing, heat shrinking, and cartoning.

[0041] 7. Inspection: Sampling shall be carried out in accordance with the sampling procedure and inspection shall be carried out in accordance with the finished product inspection standard.

[0042] 8. Warehousing: After passing inspection, the goods are put into storage.

[0043] • Appearance: Transparent solid gel adheres to the membrane fabric, without air bubbles. • pH value: within the range of 4.0-8.5 • Heat resistance: Pass • Cold resistance: Passed • Microbiological indicators: Passed

[0044] Prepare small batches of samples by appropriately reducing the proportions of Example 1.

[0045] Preparation steps: 1. Accurately weigh each ingredient according to the formula.

[0046] 2. Add phase A material to the premix tank at room temperature and stir until homogeneous.

[0047] 3. At room temperature, add phase B material to another premixing tank and stir to disperse evenly.

[0048] 4. Add phase B liquid to the main pot, then add phase A liquid, and stir with an electric mixer at an appropriate speed for no less than 5 minutes.

[0049] 5. Coat the nonwoven fabric at an appropriate temperature and cut it into the desired shape.

[0050] 6. Packaging and inspection.

[0051] Test results: All indicators are qualified.

[0052] The proportions of Example 1 were scaled up to a pilot-scale.

[0053] 1. Weigh each ingredient accurately according to the formula, and double-check the weighing.

[0054] 2. Add phase A material to the premix tank at room temperature and stir until homogeneous.

[0055] 3. At room temperature, add phase B material to another premixing tank and stir to disperse evenly.

[0056] 4. Add phase B solution to the main pot, followed by phase A solution, and stir with a hand mixer at 150 rpm for at least 10 minutes. 5. Coat the mixture onto nonwoven fabric at a suitable temperature and cut it into the desired shape.

[0057] 6. Packaging and inspection.

[0058] Test results: All indicators are qualified.

[0059] p-Hydroxyacetophenone + 1,2-hexanediol (Solution of this invention) Both bacteria and fungi meet the standards, ensuring sufficient preservative efficacy. Non-irritating Phenoxyethanol Bacteria pass through, and fungi multiply later. Some areas showed slight redness and swelling. Sodium benzoate Bacteria begin to multiply in the later stages Some individuals experienced mild stinging. Comparative experimental results show that the 1,2-hexanediol and p-hydroxyacetophenone compound preservative system used in this invention has a better preservative effect than traditional preservative systems and is less irritating to the skin.

[0060] To avoid duplication with existing technologies, the key innovation of this invention lies in: 1. Active ingredient complex system: Contains multiple components including acetyl hexapeptide-8, dipeptide diaminobutyryl benzylamide diacetate, SOD, fibronectin, sodium DNA, and collagen. The aforementioned peptides and proteins... Combinations of similar active ingredients have not been disclosed in existing hydrogel poultices.

[0061] 2. Differentiated process parameter control for different batches: Different mixing equipment and parameters are used according to the production scale (small batch ≤2kg, medium batch 2-50kg, large batch ≥50kg) to ensure the quality consistency of different batches of products. This process control strategy is not recorded in existing poultice hydrogel patents.

[0062] 3. Compound preservative system: The specific application of the preservative compound scheme of 1,2-hexanediol and p-hydroxyacetophenone in poultice hydrogel compositions, especially its compatibility with the coexistence system of sodium hyaluronate and polyacrylic acid, has not yet been disclosed in any patents.

[0063] 4. Room temperature preparation process: All operations are carried out at room temperature to avoid degradation and damage of peptide active ingredients by high temperature.

[0064] 5. Specific application design: The formula and patch shape are specially optimized for the application needs of facial skin folds such as nasolabial folds.

[0065] The poultice hydrogel composition and its preparation method provided by this invention utilize readily available raw materials, have a simple and controllable preparation process, are suitable for large-scale industrial production, exhibit high product stability and a long shelf life, and can be widely applied in the fields of medical dressings and transdermal drug delivery. This product can be mass-produced in qualified cosmetic or medical device companies for anti-wrinkle, repair, and moisturizing applications, demonstrating promising industrial application prospects and market value. The above description is merely a preferred embodiment of the present invention and is not intended to limit the scope of protection of the present invention. The numerical values ​​listed in the specific embodiments of the present invention are merely illustrative examples and do not represent the optimal formula of the present invention. The optimal ratio in actual production can be reserved as a trade secret. Any modifications, equivalent substitutions, improvements, etc., made within the spirit and principles of the present invention should be included within the scope of protection of the present invention.

Claims

1. A medical poultice hydrogel composition for transdermal absorption, characterized in that, The product comprises the following components by weight: Phase A: 15-25 parts glycerol, 5-8 parts sodium polyacrylate, 0.1-0.2 parts aluminum glycine, 0.05-0.15 parts disodium EDTA, 0.3-0.8 parts 1,2-hexanediol, and 0.05-0.2 parts sodium hyaluronate; Phase B: 60-80 parts purified water, 0.3-0.8 parts p-hydroxyacetophenone, 0.05-0.15 parts tartaric acid, and 0.5-1.5 parts polyacrylic acid; Active ingredient: selected from one or more of acetyl hexapeptide-8, hydroxypropyl tetrahydropyranotriol, dipeptide diaminobutyryl benzylamide diacetate, superoxide dismutase, fibronectin, retinol, sodium DNA, and collagen, with a total content of 0.01-0.1 parts; and the balance being pharmaceutical excipients.

2. The medical poultice hydrogel composition for transdermal absorption according to claim 1, characterized in that, The active ingredients include at least acetyl hexapeptide-8 and collagen.

3. The medical poultice hydrogel composition for transdermal absorption according to claim 1, characterized in that, The active ingredient also includes dipeptide diaminobutyryl benzylamide diacetate.

4. The medical poultice hydrogel composition for transdermal absorption according to claim 1, characterized in that, The active ingredient also includes superoxide dismutase.

5. The medical poultice hydrogel composition for transdermal absorption according to claim 1, characterized in that, The pharmaceutical excipients are selected from one or more of propylene glycol, polysorbate-80, ethylhexylglycerin, cetearyl alcohol, polysorbate-60, butylated hydroxytoluene, and phenoxyethanol.

6. A method for preparing the composition according to any one of claims 1 to 5, characterized in that... Includes the following steps: (1) Weigh each phase of raw material accurately according to the formula, place them in a clean container, and double-check them; (2) Add phase A raw material to the premixing tank at room temperature and stir evenly; (3) Add phase B raw material to another premixing tank at room temperature and stir evenly; (4) Add phase B liquid to the main pot, then add phase A liquid and stir evenly at room temperature; (5) Coat the evenly mixed hydrogel onto non-woven fabric or membrane cloth and cut it into the required shape at 18-26℃; (6) Packaging: inkjet printing, labeling, boxing, heat shrinking, and packing; (7) After passing inspection, put it into the warehouse.

7. The preparation method according to claim 6, characterized in that, The stirring parameters in step (4) are as follows: When the batch size is less than or equal to the first threshold: use an electric mixer with a speed of 80-1400 rpm and a stirring time of not less than 5 minutes; When the batch size is greater than the first threshold and less than or equal to the second threshold: use a hand mixer with a speed of 150 rpm and a stirring time of not less than 10 minutes; When the batch size is greater than the second threshold: use a vacuum homogenizer with a frequency of 15-50 Hz and a stirring time of not less than 20 minutes; Wherein, the first threshold is 2 kg and the second threshold is 50 kg.

8. The preparation method according to claim 6, characterized in that, The coating temperature in step (5) is 18-26℃.

9. The preparation method according to claim 6, characterized in that, The sealing temperature in step (6) is 220-300℃.

10. A medical poultice hydrogel composition for transdermal absorption according to claim 1, characterized in that, The finished product meets the following criteria: Appearance: Transparent solid gel adheres to the membrane fabric; pH value: 4.0-8.5; Heat resistance: No change after maintaining (40±1)℃ for 24 hours; Cold resistance: No change after maintaining (-8±2)℃ for 24 hours; Total bacterial count ≤1000 CFU / g; Total mold and yeast count ≤100 CFU / g.

11. Use of the composition according to any one of claims 1 to 5 in the preparation of a medical patch for anti-wrinkle, repair or moisturizing of facial skin folds such as nasolabial folds.

12. A poultice hydrogel patch, characterized in that, It comprises the composition according to any one of claims 1 to 5 and a nonwoven or membrane substrate.