A bio-based highly viscous gel plaster matrix, its preparation method and application

Abstract

The present invention provides a bio-based highly viscous gel patch matrix and its preparation method, as well as a patch containing simvastatin; the matrix is composed of a variety of natural ingredients, including peppermint oil as a fragrance, crotamiton and isopropyl myristate as penetration enhancers, glycerol as a humectant, and specific cross-linking agents, fillers, excipients, and tackifiers, etc., which are prepared by precise proportioning and specific processes, and have excellent adhesiveness, moisturizing property, and skin friendliness. In particular, the tackifier adopts a composite formula of xanthan gum, gum arabic, guar gum, and flaxseed gum, further improving the adhesiveness, stability, and transdermal effect of the patch. On this basis, the present invention also provides a patch containing simvastatin, which is prepared by uniformly mixing simvastatin in the matrix, and has a therapeutic effect, not only exerting the pharmacological effect of simvastatin, but also improving the use comfort and effect.

Description

Technical Field

[0001] The invention belongs to the field of pharmaceutical preparations, and specifically discloses a bio-based high-viscosity gel patch matrix and a preparation method and application thereof. Background Art

[0002] In the medical and health care field, patches are widely used in the treatment and care of various skin diseases as a convenient and effective way of drug delivery. Traditional patch matrices are mostly made of chemically synthesized components. Although they have certain adhesion and drug release properties, they often have disadvantages such as high skin irritation, poor air permeability, and easy allergies, which limits their application range.

[0003] In recent years, with people's pursuit of natural, environmentally friendly and healthy concepts, bio-based high-viscosity gel patch matrices have gradually become a research hotspot. However, there are still some problems with the bio-based gel patch matrices in the prior art. On the one hand, although some matrices use natural ingredients, they are not sufficiently adhesive and cannot ensure that the patch can be stably attached to the skin for a long time, affecting the therapeutic effect; on the other hand, although some matrices have strong adhesion, they have poor moisturizing properties and can easily lead to dry skin, itching and other discomfort reactions. In addition, the patch matrices in the prior art often lack effective permeation promoters, which makes it difficult for drugs to penetrate the skin barrier and achieve deep treatment effects.

[0004] At the same time, in the preparation of patches containing specific active ingredients (such as simvastatin), how to ensure the uniform distribution of the active ingredients in the matrix and avoid excessively high or low local concentrations is also a problem that needs to be solved urgently in the existing technology. Uneven distribution not only affects the therapeutic effect, but also may bring safety risks.

[0005] In summary, the bio-based high-viscosity gel patch matrix in the prior art still has many deficiencies in terms of adhesion, moisturizing, promoting permeability and distribution of active ingredients, and cannot meet the market demand for high-quality and high-performance patches. Summary of the invention

[0006] The present invention provides a bio-based high-viscosity gel patch matrix and a preparation method and application thereof. The matrix has excellent adhesion, good moisture retention, can effectively promote the penetration of active ingredients and can improve the uniform distribution of active ingredients, which is of great significance for improving the therapeutic effect and comfort of the patch.

[0007] The technical solution of the present invention is as follows:

[0008] A bio-based high-viscosity gel patch matrix, comprising a fragrance, a permeation enhancer 1, a permeation enhancer 2, a moisturizer, a cross-linking agent, a cross-linking regulator, a filler 1, a filler 2, an excipient, a gel skeleton, a viscosity enhancer, a pH regulator and a solvent;

[0009] The fragrance is peppermint oil;

[0010] The permeation enhancer 1 is crotamiton, and the permeation enhancer 2 is isopropyl myristate;

[0011] The viscosity increasing agent is a plant gum, including but not limited to one or more of xanthan gum, gum arabic, guar gum and linseed gum;

[0012] The filler 1 is titanium dioxide, and the filler 2 is kaolin.

[0013] Furthermore, in the above-mentioned bio-based high-viscosity gel patch matrix, the viscosity enhancer is in a mass ratio of xanthan gum: gum arabic: guar gum: flaxseed gum = 1:1:1:2.

[0014] Furthermore, in the above-mentioned bio-based high-viscosity gel patch matrix, the moisturizer is glycerol; the cross-linking agent is aluminum glycolate; and the cross-linking regulator is disodium edetate.

[0015] Furthermore, in the above-mentioned bio-based high-viscosity gel patch matrix, the excipient is sodium carboxymethylcellulose; the gel skeleton is partially neutralized sodium polyacrylate; and the solvent is purified water.

[0016] Furthermore, in the above-mentioned bio-based high-viscosity gel patch matrix, the partially neutralized sodium polyacrylate is NP700.

[0017] Furthermore, the above-mentioned bio-based high-viscosity gel patch matrix is ​​composed of the following components in parts by weight:

[0018] Aromatherapy peppermint oil 0.2-1 part

[0019] Penetration enhancer 1 Crotamiton 0.2-1 part

[0020] Penetration enhancer 2: 0.2-1 part isopropyl myristate

[0021] Moisturizer Glycerin 20-40 parts

[0022] Cross-linking agent aluminum glycolate 0.05-0.2 parts

[0023] Cross-linking regulator disodium edetate 0.05-0.5 parts

[0024] Filler 1 Titanium dioxide 0.1-0.5 parts

[0025] Filler 2 Kaolin 1-5 parts

[0026] Excipient: 1-5 parts sodium carboxymethylcellulose

[0027] The gel skeleton is partially neutralized with 5-10 parts of sodium polyacrylate

[0028] Thickener, plant gum, 10 - 20 parts

[0029] pH regulator, tartaric acid, appropriately adjusted to pH = 5.0 - 7.0

[0030] Solvent, purified water, added to 100 parts.

[0031] The present invention also discloses a preparation method of the above - mentioned bio - based highly viscous gel plaster matrix, which includes the following steps:

[0032] a) Prepare a gel matrix solution: In glycerol, slowly add and stir partially neutralized sodium polyacrylate until it is completely dispersed to form a uniform gel matrix solution;

[0033] b) Add a cross - linking system: Add glyceryl aluminum hydroxide as a cross - linking agent and disodium edetate as a cross - linking regulator to the gel matrix solution, and stir while adding to ensure the uniform dispersion of each component and the stability of the plaster;

[0034] c) Add a shaping agent: Add sodium carboxymethyl cellulose as a shaping agent to the gel matrix solution, and continue to stir until it is completely dispersed to promote the formability of the plaster;

[0035] d) Add fillers: Add titanium dioxide and kaolin as fillers to the gel matrix solution, and continue to stir until it is completely dispersed to improve the spreadability and covering power of the plaster;

[0036] e) Add flavoring agents and penetration enhancers: Add menthol oil, crotamiton, and isopropyl myristate to the gel matrix solution, and stir while adding to ensure the uniform dispersion of each component, promote the skin penetration ability of the drug, and provide the use experience of the plaster;

[0037] f) Adjust the pH value: Dissolve an appropriate amount of tartaric acid in purified water, and adjust the pH value of the above - mentioned mixture to 5.0 - 7.0 to ensure the stability of the product;

[0038] g) Add a thickener: Dissolve plant gum in purified water, and add it to the above - mentioned mixture to improve the adhesiveness and persistence of the plaster. The plant gum is composed of xanthan gum: gum arabic: guar gum: linseed gum = 1:1:1:2;

[0039] h) Defoaming: Stir the above - mentioned mixture at high speed under vacuum conditions, and remove the bubbles generated during the stirring process to ensure the fineness and uniformity of the plaster. Finally, obtain the bio - based highly viscous gel plaster matrix.

[0040] The present invention also discloses a patch containing the active ingredient simvastatin, which is made of the bio - based highly viscous gel plaster matrix described in any one of the above and a therapeutic amount of simvastatin.

[0041] Further, a preparation method of the above-mentioned patch containing simvastatin active ingredient comprises the following steps:

[0042] S1 Mixing evenly: After the preparation of the bio-based highly viscous gel patch matrix is completed and it is still in a semi-solid state that can be stirred. First, dissolve simvastatin in a solvent (polysorbate 80, ethyl oleate), and slowly and evenly add it to the gel patch matrix. Through stirring treatment, ensure that the simvastatin active ingredient is evenly distributed in the matrix to avoid too high or too low local concentration;

[0043] S2 Molding and cutting: Mold the processed gel patch matrix containing simvastatin active ingredient according to a predetermined shape and size, and make a patch through the general preparation process of the patch.

[0044] Further, for the above-mentioned patch containing simvastatin active ingredient, the mass ratio of the bio-based highly viscous gel patch matrix to simvastatin is 10 - 100:1; preferably 30 - 70:1; more preferably 50:1.

[0045] Compared with the prior art, the present invention has the following beneficial effects:

[0046] The present invention discloses a bio-based highly viscous gel patch matrix, its preparation method and application. This matrix uses all-natural ingredients such as plant gum and glycerin, which not only ensures the safety and environmental protection of the product, but also greatly reduces the irritation and allergy risk to the skin. Through scientific proportioning and specific preparation processes, the matrix exhibits excellent adhesiveness and moisturizing properties, and can stably adhere to the skin for a long time, providing a strong guarantee for the effective release of drugs. At the same time, the penetration enhancers (crotamiton and isopropyl myristate) in the matrix combined with the plant gum adhesive significantly enhance the skin penetration ability of the drug, enabling the drug to penetrate the skin barrier more quickly and achieve the effect of deep treatment.

[0047] In addition, the present invention also discloses a patch containing simvastatin active ingredient using the above matrix. Its preparation process is simple and efficient, ensuring the uniform distribution of simvastatin in the matrix and avoiding the problem of uneven treatment caused by too high or too low local concentration. This patch not only has the unique therapeutic effect of simvastatin, but also combines the high adhesiveness, moisturizing property and enhanced permeability of the matrix, making the therapeutic effect more significant and lasting.

[0048] In summary, the bio-based highly viscous gel patch matrix of the present invention and the patch containing simvastatin active ingredient perform excellently in terms of adhesiveness, moisturizing property, enhanced permeability, skin friendliness, therapeutic effect and use comfort, providing a new patch product with high quality and high efficiency for the medical and health care fields. Description of the Drawings

[0049] Figure 1 For the weight loss test results in the test example, the Y-axis is the water loss rate wt%;

[0050] Figure 2 It is the test result of the relative transdermal absorption rate in the test example. Detailed implementation mode

[0051] A bio-based highly viscous gel plaster matrix, by weight, consists of the following components:

[0052] Fragrance, Peppermint oil, 0.2 - 1 part

[0053] Penetration enhancer 1, Crotamiton, 0.2 - 1 part

[0054] Penetration enhancer 2, Isopropyl myristate, 0.2 - 1 part

[0055] Humectant, Glycerol, 20 - 40 parts

[0056] Cross-linking agent, Dihydroxyaluminum aminoacetate, 0.05 - 0.2 part

[0057] Cross-linking regulator, Disodium edetate, 0.05 - 0.5 part

[0058] Filler 1, Titanium dioxide, 0.1 - 0.5 part

[0059] Filler 2, Kaolin, 1 - 5 parts

[0060] Excipient, Sodium carboxymethylcellulose, 1 - 5 parts

[0061] Gel skeleton, Partially neutralized sodium polyacrylate, 5 - 10 parts

[0062] Tackifier, Plant gum, 10 - 20 parts

[0063] pH regulator, Tartaric acid, adjusted to pH = 5.0 - 7.0 as appropriate

[0064] Solvent, Purified water, added to 100 parts.

[0065] The plant gum consists of xanthan gum:arabic gum:guar gum:linseed gum = 1:1:1:2.

[0066] The preparation method of the above bio-based highly viscous gel plaster matrix includes the following steps:

[0067] a) Prepare the gel matrix solution: Slowly add and stir partially neutralized sodium polyacrylate in glycerol until it is completely dispersed to form a uniform gel matrix solution;

[0068] b) Adding a crosslinking system: Aluminum glycinate is added as a crosslinking agent and disodium edetate is added as a crosslinking regulator to the gel matrix solution. Stir while adding to ensure the uniform dispersion of each component and the stability of the plaster.

[0069] c) Adding a shaping agent: Sodium carboxymethylcellulose is added as a shaping agent to the gel matrix solution, and stirring is continued until it is completely dispersed to promote the formability of the plaster.

[0070] d) Adding a filler: Titanium dioxide and kaolin are added as fillers to the gel matrix solution, and stirring is continued until it is completely dispersed to improve the spreadability and covering power of the plaster.

[0071] e) Adding a fragrance and a penetration enhancer: Menthol, crotamiton, and isopropyl myristate are added to the gel matrix solution. Stir while adding to ensure the uniform dispersion of each component, promote the skin penetration ability of the drug, and provide the use experience of the plaster.

[0072] f) Adjusting the pH value: An appropriate amount of tartaric acid is dissolved in purified water, and the pH value of the above-mentioned mixed solution is adjusted to 5.0 - 7.0 to ensure the stability of the product.

[0073] g) Adding a tackifier: A plant gum is dissolved in purified water and added to the above-mentioned mixed solution to improve the adhesiveness and durability of the plaster. The plant gum is composed of xanthan gum: gum arabic: guar gum: linseed gum = 1:1:1:2.

[0074] h) Defoaming: The above-mentioned mixed solution is subjected to high-speed stirring under vacuum conditions, and the bubbles generated during stirring are removed to ensure the fineness and uniformity of the plaster. Finally, the bio-based highly viscous gel plaster matrix is obtained.

[0075] The technical solutions in the embodiments of the present invention are clearly and completely described below. 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 scope of protection of the present invention.

[0076] Example 1

[0077] A bio-based highly viscous gel plaster matrix is composed of the following components by weight:

[0078] Fragrance Menthol 0.2 parts

[0079] Penetration enhancer 1 Crotamiton 0.2 parts

[0080] Penetration enhancer 2 Isopropyl myristate 0.2 parts

[0081] Humectant Glycerol 25 parts

[0082] Cross-linking agent: Dihydroxyaluminum aminoacetate, 0.05 parts

[0083] Cross-linking regulator: Disodium edetate, 0.08 parts

[0084] Filler 1: Titanium dioxide, 0.2 parts

[0085] Filler 2: Kaolin, 1 part

[0086] Excipient: Sodium carboxymethylcellulose, 1 part

[0087] Gel matrix: Partially neutralized sodium polyacrylate, 5 parts

[0088] Viscosity increasing agent: Vegetable gum, 10 parts

[0089] pH regulator: Tartaric acid, adjust the pH to 5.2 as appropriate

[0090] Solvent: Purified water, q.s. to 100 parts

[0091] The vegetable gum is composed of xanthan gum: gum arabic: guar gum: linseed gum = 1:1:1:2;

[0092] The preparation method of the above-mentioned bio-based highly viscous gel plaster matrix comprises the following steps:

[0093] a) Prepare the gel matrix solution: Slowly add and stir partially neutralized sodium polyacrylate in glycerol until it is completely dispersed to form a uniform gel matrix solution;

[0094] b) Add the cross-linking system: Add dihydroxyaluminum aminoacetate as a cross-linking agent and disodium edetate as a cross-linking regulator to the gel matrix solution, stirring while adding to ensure uniform dispersion of each component and the stability of the plaster;

[0095] c) Add the excipient: Add sodium carboxymethylcellulose as an excipient to the gel matrix solution and continue stirring until it is completely dispersed to promote the formability of the plaster;

[0096] d) Add the fillers: Add titanium dioxide and kaolin as fillers to the gel matrix solution and continue stirring until they are completely dispersed to improve the spreadability and covering power of the plaster;

[0097] e) Add the fragrance and penetration enhancer: Add menthol, crotamiton and isopropyl myristate to the gel matrix solution, stirring while adding to ensure uniform dispersion of each component, promote the skin penetration ability of the drug, and provide the usage experience of the plaster;

[0098] f) Adjust the pH value: Dissolve an appropriate amount of tartaric acid in purified water and adjust the pH value of the above-mentioned mixed solution to 5.0 - 7.0 to ensure the stability of the product;

[0099] g) Adding a viscosity enhancer: Dissolve the plant gum in purified water and add it to the above mixture to improve the adhesion and durability of the patch. The plant gum is composed of xanthan gum: gum arabic: guar gum: linseed gum = 1:1:1:2;

[0100] h) Degassing: The mixed solution is stirred at high speed under vacuum conditions to remove bubbles generated during the stirring process to ensure the fineness and uniformity of the patch, and finally the bio-based high-viscosity gel patch matrix is ​​obtained.

[0101] Example 2

[0102] A bio-based high-viscosity gel patch matrix, composed of the following components in parts by weight:

[0103] 0.2 parts of fragrance peppermint oil

[0104] Penetration enhancer 1 Crotamiton 0.5 parts

[0105] Penetration enhancer 2: 0.2 parts of isopropyl myristate

[0106] Moisturizer Glycerin 28 parts

[0107] Crosslinking agent aluminum glycolate 0.08 parts

[0108] Cross-linking regulator disodium edetate 0.1 part

[0109] Filler 1 Titanium dioxide 0.2 parts

[0110] Filler 2: 1 part kaolin

[0111] Excipient: 2 parts sodium carboxymethylcellulose

[0112] The gel skeleton is partially neutralized with 6 parts of sodium polyacrylate

[0113] 15 parts of tackifier vegetable glue

[0114] pH adjuster: tartaric acid is used to adjust the pH to 5.5

[0115] Solvent: 100 parts of purified water.

[0116] The preparation is the same as Example 1.

[0117] Example 3

[0118] A bio-based high-viscosity gel patch matrix, composed of the following components in parts by weight:

[0119] 0.2 parts of fragrance peppermint oil

[0120] Penetration enhancer 1 Crotamiton 0.5 parts

[0121] Penetration enhancer 2 Isopropyl myristate 0.5 parts

[0122] Humectant Glycerol 35 parts

[0123] Crosslinking agent Aluminium glycolate 0.15 parts

[0124] Crosslinking regulator Disodium edetate 0.2 parts

[0125] Filler 1 Titanium dioxide 0.2 parts

[0126] Filler 2 Kaolin 1 part

[0127] Excipient Sodium carboxymethylcellulose 3 parts

[0128] Gel matrix Partially neutralized sodium polyacrylate 8 parts

[0129] Viscosity increasing agent Vegetable gum 20 parts

[0130] pH regulator Tartaric acid Adjusted to pH = 5.7 as appropriate

[0131] Solvent Purified water 100 parts.

[0132] Prepared in the same manner as in Example 2.

[0133] Example 4

[0134] The vegetable gum consists of xanthan gum: gum arabic: guar gum: linseed gum = 1:1:1:1, and the rest is the same as in Example 2.

[0135] Example 5

[0136] The vegetable gum consists of xanthan gum: gum arabic: guar gum: linseed gum = 1:1:1:3, and the rest is the same as in Example 2.

[0137] Comparative Example 1

[0138] Compared with Example 2, the vegetable gum consists of xanthan gum: gum arabic: guar gum = 1:1:1.

[0139] Comparative Example 2

[0140] Compared with Example 2, the vegetable gum consists of xanthan gum: gum arabic = 1:1.

[0141] Comparative Example 3

[0142] Compared with Example 2, the vegetable gum is xanthan gum.

[0143] Comparative Example 4

[0144] Compared with Example 2, a chemical tackifier (20% polyacrylic acid solution of Toagosei Co., Ltd., Japan) was used.

[0145] Test Example 1

[0146] For the gel patch matrices of Examples 1-5 and Comparative Examples 1-4, 3x3 cm square patches were prepared in the conventional manner, each containing 5 g of the matrix. Each experimental sample was applied to the outer side of the upper arm of 25 volunteer subjects and kept for 8 h. The film residue, skin followability, use comfort, skin irritation, skin allergy, pain during peeling, etc. were evaluated and divided into three grades: good, medium, and poor. Good was rated 5 points, fair was rated 3 points, medium was rated 1 point, and poor was rated 0 points. After accumulation, the result was divided by the number of subjects and rounded to one decimal place. The results are shown in Table 1.

[0147] Table 1 Subjective Evaluation

[0148]

[0149] As can be seen from the above examples, Examples 1-5 and Comparative Examples 1-3 using plant gum were significantly better than the similar products using chemical tackifiers in terms of skin irritation, skin allergy, and pain during peeling. From the comparison between the examples and the comparative examples, it can be seen that the combined effects of using xanthan gum, gum arabic, guar gum, and linseed gum as plant gums were better than those of Comparative Examples 1-3; from the comparison between Example 2, Example 4, and Example 5, it can be seen that when the mass ratio of xanthan gum: gum arabic: guar gum: linseed gum was kept at 1:1:1:2, the best evaluations of film residue, skin followability, and use comfort could be obtained.

[0150] Test Example 2

[0151] Initial tack performance test (30° ramp rolling ball method), samples: samples of Examples 1-5 and Comparative Examples 1-4, patches were prepared according to the method of Test Example 1: adhesion was determined according to General Rule 0952 of the Fourth Part of Chinese Pharmacopoeia 2020 Edition. The results are shown in Table 2.

[0152] Table 2 Initial Tack Performance Test

[0153]

[0154] As can be seen from Table 2 above, when using the mixed plant gum of xanthan gum, gum arabic, guar gum, and linseed gum, its initial tack was the best, and when the mass ratio of gum arabic: guar gum: linseed gum was kept at 1:1:1:2, the best initial tack could be obtained.

[0155] Test Example 3

[0156] Weight Loss Test

[0157] Samples: Samples of Examples 1-5 and Comparative Examples 1-4 were used to prepare patches according to the method of Test Example 1.

[0158] Method: The trial-produced samples were stored in an indoor environment with a temperature of 20 °C and a humidity of 50%, and their weight loss was measured to investigate their water retention and stability, calculated as the wt% of weight reduction.

[0159] The results are shown in Figure 1 and Table 3.

[0160] Table 3 Weight Loss Test

[0161]

[0162] As can be seen from Table 3 above, the water loss weight of Example 2 in 10 days was only 1.28 wt%, far lower than the water loss values of the comparative examples. It can be seen that the combination of plant gums xanthan gum, gum arabic, guar gum and linseed gum not only has strong adhesiveness, but also has good moisture retention performance.

[0163] Test Example 4

[0164] Simvastatin (purchased from Shanghai Aladdin Biochemical Technology Co., Ltd.) was dissolved in solvents such as polysorbate and ethyl oleate, and added to the matrices of Examples 1-5 and Comparative Examples 1-4 according to the following steps to prepare a medicinal patch.

[0165] S1 Mixing evenly: After the preparation of the bio-based highly viscous gel patch matrix and when it is still in a semi-solid state that can be stirred. First, dissolve simvastatin in the solvent (polysorbate 80, ethyl oleate), and slowly and evenly add it to the gel patch matrix. Through stirring treatment, ensure that the simvastatin active ingredient is evenly distributed in the matrix to avoid too high or too low local concentration;

[0166] S2 Molding and cutting: The treated gel patch matrix containing the simvastatin active ingredient was molded according to a predetermined shape and size, and a patch was made through the general preparation process of the patch.

[0167] The mass ratio of the bio-based highly viscous gel patch matrix to simvastatin is 50:1.

[0168] The above-prepared medicinal patch was subjected to a transdermal absorption test:

[0169] Apparatus: Transdermal absorption diffusion instrument (PermeGear In-Line Cells, PermeGear online automatic transdermal diffusion system), liquid chromatograph

[0170] Test procedure

[0171] (1) Take the treated small pig skin sample and soak it in physiological saline for 2 h.

[0172] (2) Cut the skin sample into an appropriate size, apply the test sample on the outer side with a thickness of 1 mm, and fix it on the Franz diffusion cell (the inner side of the skin sample faces the diffusion liquid). Connect and fix the supply cell and the receiving cell. Add the receiving liquid preheated to 32 °C into the receiving cell.

[0173] (3) Place the diffusion cell with the fixed sample in a transdermal diffusion instrument water bath preheated to 32 °C and stir magnetically at 50 rpm.

[0174] (4) Take samples at 8 h. Take out 1 ml of the receiving liquid.

[0175] (5) Inject the sampled solution into a high performance liquid chromatograph for test analysis (calculate the transdermal water absorption rate based on the peak area of the simvastatin reference substance, and calculate the relative transdermal rate SPR of other examples based on the transdermal rate of Comparative Example 5 (1.0)).

[0176] The results are shown in Figure 2 and Table 4 as follows.

[0177] Table 4 Relative Transdermal Absorption Rate

[0178]

[0179] It can be seen from the data in Table 4 that the transdermal absorption rate of Example 2 is increased by nearly 80% compared with Comparative Example 4, indicating that the use of plant gums, preferably the combination of xanthan gum, gum arabic, guar gum and linseed gum, has a better effect of promoting drug penetration through the skin than chemical tackifiers and is more likely to exert the drug efficacy.

[0180] It can be seen from the data of the above examples that the present invention discloses a bio-based highly viscous gel patch matrix, its preparation method and application. This matrix uses all-natural ingredients such as plant gums and glycerin, which not only ensures the safety and environmental protection of the product, but also greatly reduces the irritation and allergy risks to the skin. Prepared by scientific proportioning and specific processes, the matrix exhibits excellent adhesiveness and moisturizing properties, can stably adhere to the skin for a long time, and provides a strong guarantee for the effective release of drugs. At the same time, the penetration enhancers (crotamiton and isopropyl myristate) in the matrix combined with the plant gum adhesive can significantly enhance the skin penetration ability of the drug, enabling the drug to penetrate the skin barrier more quickly and achieve the effect of deep treatment.

[0181] The above are only several preferred embodiments of the present invention, and the description is relatively specific and detailed, but it should not be construed as a limitation on the scope of the present 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.

Claims

1. A bio-based highly viscous gel plaster matrix, characterized in that, By weight parts, it consists of the following components: Fragrance, Peppermint Oil, 0.2 - 1 part Penetration Enhancer 1, Crotamiton, 0.2 - 1 part Penetration Enhancer 2, Isopropyl Myristate, 0.2 - 1 part Humectant, Glycerol, 20 - 40 parts Cross - linker, Aluminium Glycinate, 0.05 - 0.2 part Cross - linking Regulator, Disodium Edetate, 0.05 - 0.5 part Filler 1, Titanium Dioxide, 0.1 - 0.5 part Filler 2, Kaolin, 1 - 5 parts Excipient, Sodium Carboxymethylcellulose, 1 - 5 parts Gel Matrix, Partially Neutralized Sodium Polyacrylate NP700, 5 - 10 parts Viscosity - increasing Agent, Vegetable Gum, 10 - 20 parts pH Regulator, Tartaric Acid, adjusted to pH = 5.0 - 7.0 as appropriate Solvent, Purified Water, added to 100 parts; The preparation method of the above - mentioned bio - based highly viscous gel plaster matrix includes the following steps: a) Prepare the gel matrix solution: Slowly add and stir partially neutralized sodium polyacrylate NP700 in glycerol until it is completely dispersed to form a uniform gel matrix solution; b) Add the cross - linking system: Add the cross - linker aluminium glycinate and the cross - linking regulator disodium edetate to the gel matrix solution, stirring while adding to ensure that each component is evenly dispersed; c) Add the excipient: Add the excipient sodium carboxymethylcellulose to the gel matrix solution, and continue to stir until it is completely dispersed to promote the formability of the plaster; d) Add the fillers: Add the fillers titanium dioxide and kaolin to the gel matrix solution, and continue to stir until they are completely dispersed to improve the spreadability and covering power of the plaster; e) Add the fragrance and penetration enhancers: Add peppermint oil, crotamiton and isopropyl myristate to the gel matrix solution, stirring while adding to ensure that each component is evenly dispersed and promote the skin penetration ability of the drug; f) Adjust the pH value: Dissolve an appropriate amount of tartaric acid in purified water, and adjust the pH value of the mixture obtained in step e) to 5.0 - 7.0 to ensure the stability of the product; g) Add the viscosity - increasing agent: Dissolve the vegetable gum in purified water, and add it to the mixture obtained in step f) to enhance the adhesiveness and persistence of the plaster; the vegetable gum is composed of xanthan gum: gum arabic: guar gum: linseed gum = 1:1:1:2; h) Defoaming: Stir the mixture obtained in step g) at high speed under vacuum conditions and remove the bubbles generated during stirring to ensure the fineness and uniformity of the plaster, and finally obtain the bio - based highly viscous gel plaster matrix.

2. A patch containing the active ingredient simvastatin, characterized in that, It is made of the bio - based highly viscous gel plaster matrix as described in claim 1 and a therapeutic amount of simvastatin.

3. The patch containing the active ingredient of simvastatin according to claim 2, characterized in that, It is prepared by the following steps: S1 Mix evenly: After the bio - based highly viscous gel plaster matrix is prepared and while it is still in a semi - solid state that can be stirred, first dissolve simvastatin in the solvent; the solvent is polysorbate 80 and ethyl oleate; slowly and evenly add it to the gel plaster matrix, and through stirring treatment, ensure that the simvastatin active ingredient is evenly distributed in the matrix to avoid too high or too low local concentration; S2 Molding and cutting: Mold the processed gel plaster matrix containing the simvastatin active ingredient according to a predetermined shape and size, and make a patch through the general preparation process of the patch.

4. The patch containing the active ingredient of simvastatin according to claim 2, characterized in that, The mass ratio of the bio-based highly viscous gel patch matrix to simvastatin is 10 - 100:1.

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