Yao medicine characteristic powerful external plaster for treating gout and acute joint severe pain

Abstract

The invention provides a Yao medicine characteristic powerful external plaster for treating gout acute joint pain, and relates to the field of plasters, a preparation method comprises the following steps: S100, crushing a matrix until the particle size is less than or equal to 2 mm, adding 200 g of oil into per kilogram of the matrix, the oil being selected from soybean oil, rapeseed oil, sesame oil or blend oil; s200, heating with a soft fire of 50-80 DEG C until the matrix is completely dissolved to form a homogeneous oil phase; and S300, slowly adding 1000g of medicinal powder into the oil phase, and decocting at a stirring speed of 20-30r / min for 40-60 minutes until the color of the mixture becomes dark brown or black. According to the plaster, the borneol and the mentholum have a synergistic effect, so that the plaster can quickly permeate skin, a local ice feeling can be generated within 5 minutes after the plaster is applied, the median onset time is 20-30 minutes, and the plaster is obviously superior to an oral medicine, the tripterygium wilfordii extract inhibits the activity of xanthine oxidase, the scandent schefflera stem and leaf blocks an IL-1beta inflammation pathway, and the borneol is assisted to stimulate a TRPM8 receptor, so that the curative effect of the plaster is improved. And the pain relief rate is increased to 50-70%.

Description

Technical Field

[0001] The invention relates to the field of plasters, and in particular to a Yao medicine-specific strong external plaster for treating acute joint pain caused by gout. Background Art

[0002] Currently, oral nonsteroidal anti-inflammatory drugs (such as colchicine) or glucocorticoids are the preferred treatments in clinical practice. However, oral medications require systemic metabolism, generally take more than 1 hour to take effect, and are prone to gastrointestinal reactions. Commercially available topical patches (such as diclofenac sodium patches) only target inflammation or pain, lack synergistic uric acid-lowering and anti-inflammatory effects, and have low transdermal efficiency (drug utilization rate <50%), resulting in redness and swelling taking up to 3-5 days to subside. Traditional Yao medicine ointments mostly use water decoction extraction or direct powder grinding, with a loss rate of ≥40% for heat-sensitive components (such as triptolide), and excessively large particle size (>100 mesh) leading to poor transdermal absorption.

[0003] Therefore, we have made improvements to this and proposed a Yao medicine-specific strong external plaster for treating acute joint pain caused by gout. Summary of the Invention

[0004] The purpose of the present invention is to address the problems raised by the current background technology.

[0005] In order to achieve the above-mentioned purpose of the invention, the present invention provides a Yao medicine-specific strong external plaster for treating acute joint pain caused by gout, so as to improve the above-mentioned problems.

[0006] The specific application is as follows: The preparation method comprises the following steps: S100, crushing the matrix to a particle size of ≤2 mm, adding 200 g of oil per kg of the matrix, wherein the oil is selected from soybean oil, rapeseed oil, sesame oil or blended oil; S200, heat at 50-80℃ until the matrix is ​​completely melted and a homogeneous oil phase is formed; S300, slowly add 1000 g of the powder to the oil phase, and simmer at a stirring speed of 20-30 rpm for 40-60 minutes until the mixture turns dark brown or black; S400, after cooling to 120°C, add 200g of borneol and 200g of mint ice, and stir until completely dissolved; S500. Prepare the mixture into a patch by dripping or coating, with a coating thickness of 0.5-1.0 mm and an effective drug content of 2-3 g per patch.

[0007] As the preferred technical solution of this application, the medicinal powder is composed of the following Chinese medicinal raw materials in parts by weight: Yao medicine active ingredients: 30-40 parts of Tripterygium wilfordii extract, 20-30 parts of Aesculus multiflorus extract, and 10-15 parts of Herba schizonepetae extract; Auxiliary materials: 10-15 parts of astragalus polysaccharide, 5-8 parts of angelica volatile oil, 3-5 parts of ligustrazine, and 2-3 parts of nano-silicon dioxide.

[0008] As a preferred technical solution of the present application, the mass ratio of borneol to mint ice is 1:1, and the total amount added accounts for 5%-8% of the total weight of the mixture.

[0009] As a preferred technical solution of the present application, the surface of the coating layer of the patch is covered with a microporous breathable membrane with a pore size of 5-10 μm and an air permeability of ≥2000 g / m²·24h.

[0010] As a preferred technical solution of the present application, the matrix is ​​a composite matrix composed of beeswax and vaseline in a mass ratio of 3:7.

[0011] As a preferred technical solution of this application, the preparation method of the Tripterygium wilfordii extract includes: The rhizome of Tripterygium wilfordii was crushed and ultrasonically extracted twice with 70% ethanol. The combined extracts were concentrated under reduced pressure to a relative density of 1.2-1.3, and freeze-dried to obtain an extract.

[0012] As a preferred technical solution of the present application, the oil is a mixed oil composed of soybean oil and sesame oil in a mass ratio of 6:4.

[0013] As a preferred technical solution of the present application, the oil is a mixed oil composed of soybean oil and sesame oil in a mass ratio of 6:4.

[0014] As a preferred technical solution of the present application, the particle size of the medicinal powder is 80-100 mesh, and it is ultrafinely pulverized to a specific surface area of ​​≥5m² / g.

[0015] As a preferred technical solution of the present application, the packaging material of the patch is an aluminum-plastic composite film, and nitrogen is filled inside to isolate oxygen.

[0016] Compared with the prior art, the present invention has the following beneficial effects: In the scheme of this application: 1. The synergistic effect of borneol and mint ice in the patch allows rapid skin penetration, producing a localized cooling sensation within 5 minutes of application. The median onset of action is 20-30 minutes, significantly superior to oral medications. Tripterygium wilfordii extract inhibits xanthine oxidase activity, while quinquefolia blocks the IL-1β inflammatory pathway. Combined with borneol to stimulate the TRPM8 receptor, the patch achieves a 50%-70% pain relief rate. 2. Herba Lycopodii extract reduces TNF-α expression in the synovial membrane, angelica volatile oil promotes local microcirculation, and Tripterygium wilfordii extract (ethanol ultrasonic extraction, purity ≥85%) targets and inhibits urate synthase activity. Combined with the patch's transdermal sustained-release properties, this reduces blood uric acid levels. 3. With Yao herbs such as Tripterygium wilfordii and Aesculus quinquefolius as the core, combined with modern ultrafine grinding technology (powder specific surface area ≥ 5m² / g), the active ingredients have better transdermal efficiency and are easier to absorb than traditional water decoction technology. BRIEF DESCRIPTION OF THE DRAWINGS

[0017] Figure 1 A schematic diagram of the preparation method of the Yao medicine-specific potent external plaster provided in this application for treating acute joint pain caused by gout; DETAILED DESCRIPTION

[0018] In order to enable those skilled in the art to better understand the solutions of the present invention, the technical solutions in the embodiments of the present invention will be clearly and completely described below in conjunction with the drawings in the embodiments of the present invention. Obviously, the embodiments described are only part of the embodiments of the present invention, not all of the embodiments. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without making creative efforts should fall within the scope of protection of the present invention.

[0019] In order to enable those skilled in the art to better understand the solutions of the present invention, the technical solutions in the embodiments of the present invention will be clearly and completely described below with reference to the accompanying drawings.

[0020] It should be noted that, in the absence of conflict, the embodiments of the present invention and the features and technical solutions therein may be combined with each other.

[0021] It should be noted that similar reference numerals and letters denote similar items in the following drawings, and therefore, once an item is defined in one drawing, it does not need to be further defined or explained in subsequent drawings.

[0022] Example 1, please refer to Figure 1 A Yao medicine-specific strong external plaster for treating acute joint pain caused by gout, the preparation method of which comprises the following steps: S100, crushing the matrix to a particle size of ≤2 mm, adding 200 g of oil per kg of the matrix, wherein the oil is selected from soybean oil, rapeseed oil, sesame oil or blended oil; S200, heat at 50-80℃ until the matrix is ​​completely melted and a homogeneous oil phase is formed; S300, slowly add 1000 g of the powder to the oil phase, and simmer at a stirring speed of 20-30 rpm for 40-60 minutes until the mixture turns dark brown or black; S400, after cooling to 120°C, add 200g of borneol and 200g of mint ice, and stir until completely dissolved; S500. Prepare the mixture into a patch by dripping or coating, with a coating thickness of 0.5-1.0 mm and an effective drug content of 2-3 g per patch.

[0023] The matrix particle size is ≤2mm to ensure rapid fusion of the oil phase; the oil selection optimizes the release efficiency of the drug's fat-soluble components, increasing the permeability by 30%-40%.

[0024] Stirring speed and time control to avoid powder agglomeration and ensure uniform dispersion of active ingredients The medicinal powder is composed of the following Chinese medicinal raw materials in parts by weight: Yao medicine active ingredients: 30-40 parts of Tripterygium wilfordii extract, 20-30 parts of Aesculus multiflorus extract, and 10-15 parts of Herba schizonepetae extract; Auxiliary materials: 10-15 parts of astragalus polysaccharide, 5-8 parts of angelica volatile oil, 3-5 parts of ligustrazine, and 2-3 parts of nano-silicon dioxide.

[0025] Tripterygium wilfordii extract inhibits xanthine oxidase activity and reduces uric acid production; Aesculus multiflorus extract blocks the IL-1β inflammatory pathway and reduces joint synovial damage.

[0026] Nano-silica is used as an adsorbent to increase drug loading rate and prolong sustained-release time.

[0027] The mass ratio of the borneol to the mint ice is 1:1, and the total amount added accounts for 5%-8% of the total weight of the mixture.

[0028] Borneol and menthol ice synergistically reduce local temperature (2-3°C lower in 5 minutes after application) and enhance the analgesic effect by stimulating TRPM8 receptors.

[0029] The surface of the coating layer of the patch is covered with a microporous breathable membrane with a pore size of 5-10 μm and an air permeability of ≥2000 g / m²·24h.

[0030] The microporous membrane design avoids sweat accumulation, reduces the risk of skin allergies, and maintains sustained drug release (release rate ≥90% within 12 hours).

[0031] The matrix is ​​a composite matrix composed of beeswax and vaseline in a mass ratio of 3:7.

[0032] Beeswax improves the adhesion of the patch (peel force ≥ 1.5N / cm), and petrolatum enhances skin moisturizing properties and reduces the incidence of dryness and desquamation after application.

[0033] The preparation method of the Tripterygium wilfordii extract comprises: The rhizome of Tripterygium wilfordii was crushed and ultrasonically extracted twice with 70% ethanol. The combined extracts were concentrated under reduced pressure to a relative density of 1.2-1.3, and freeze-dried to obtain an extract.

[0034] The ethanol ultrasonic extraction method retains active ingredients such as triptolide with a purity of ≥85%, avoiding the residual toxic components of the traditional water decoction process.

[0035] The oil is a mixed oil composed of soybean oil and sesame oil in a mass ratio of 6:4.

[0036] The proportion of unsaturated fatty acids in the mixed oil is ≥70%, which promotes the transdermal absorption of fat-soluble drug ingredients (such as ligustrazine) and increases the penetration rate by 25%.

[0037] The oil is a mixed oil composed of soybean oil and sesame oil in a mass ratio of 6:4.

[0038] The proportion of unsaturated fatty acids in the mixed oil is ≥70%, which promotes the transdermal absorption of fat-soluble drug ingredients (such as ligustrazine) and increases the penetration rate by 25%.

[0039] The particle size of the medicinal powder is 80-100 mesh, and the powder is ultrafinely pulverized to a specific surface area of ​​≥5m² / g.

[0040] Ultrafine grinding increases the contact area between the drug and the matrix, increasing the release rate of the active ingredient to more than 95%.

[0041] The packaging material of the patch is an aluminum-plastic composite film, and the interior is filled with nitrogen to isolate oxygen.

[0042] The oxygen permeability of the aluminum-plastic composite film is ≤0.5cm³ / m²·24h, and nitrogen protection increases the stability of the volatile components of borneol and mint ice by 50%.

[0043] The method of using the patch is as follows: Clean the skin before application, cut the patch into 1.2-1.5 times the size of the affected area, apply for 6-8 hours each time, change 1-2 times a day, and use continuously for no more than 7 days.

[0044] The trimming area optimizes drug coverage and avoids edge curling; the 7-day limit-use strategy prevents drug accumulation toxicity (clinical data show no significant changes in ALT / AST indicators).

[0045] The patch is used in combination with oral nonsteroidal anti-inflammatory drugs (such as colchicine), with the medication interval being ≥2 hours.

[0046] The synergistic effect of external application and internal administration increased the overall effective rate (pain VAS score decreased by ≥50%) from 65% of single medication to 85%.

[0047] The medicinal powder is sterilized by irradiation with 60Co-γ rays, with an irradiation dose of 8-10 kGy.

[0048] The irradiation sterilization method reduces the microbial limit to ≤10 CFU / g and the destruction rate of heat-sensitive components in the powder (such as angelica volatile oil) to ≤5%.

[0049] In the present invention, unless otherwise specified or limited, the terms "installed," "connected," "connect," "fixed," etc. should be understood in a broad sense. For example, they can refer to fixed connection, detachable connection, or integration; mechanical connection, electrical connection, or communication; direct connection or indirect connection through an intermediate medium; internal communication between two elements or interaction between two elements, unless otherwise specified. Those skilled in the art will understand the specific meanings of the above terms in the present invention based on specific circumstances.

[0050] Obviously, the embodiments described above are only some embodiments of the present invention, rather than all embodiments. The preferred embodiments of the present invention are given in the accompanying drawings, but they do not limit the patent scope of the present invention. The present invention can be implemented in many different forms. On the contrary, the purpose of providing these embodiments is to make the understanding of the disclosure of the present invention more thorough and comprehensive. Although the present invention has been described in detail with reference to the aforementioned embodiments, for those skilled in the art, it is still possible to modify the technical solutions described in the aforementioned specific embodiments, or to make equivalent replacements for some of the technical features therein. Any equivalent structure made using the contents of the present invention specification and drawings, directly or indirectly used in other related technical fields, is also within the scope of patent protection of the present invention.

Claims

1. A Yao medicine-specific strong external plaster for treating acute joint pain caused by gout, characterized in that: The preparation method comprises the following steps: S100, crushing the matrix to a particle size of ≤2 mm, adding 200 g of oil per kg of the matrix, wherein the oil is selected from soybean oil, rapeseed oil, sesame oil or blended oil; S200, heat at 50-80℃ until the matrix is ​​completely melted and a homogeneous oil phase is formed; S300, slowly add 1000 g of the powder to the oil phase, and simmer at a stirring speed of 20-30 rpm for 40-60 minutes until the mixture turns dark brown or black; S400, after cooling to 120°C, add 200g of borneol and 200g of mint ice, and stir until completely dissolved; S500. Prepare the mixture into a patch by dripping or coating, with a coating thickness of 0.5-1.0 mm and an effective drug content of 2-3 g per patch.

2. The Yao medicine-specific potent external plaster for treating acute joint pain caused by gout according to claim 1, characterized in that: The medicinal powder is composed of the following Chinese medicinal raw materials in parts by weight: Yao medicine active ingredients: 30-40 parts of Tripterygium wilfordii extract, 20-30 parts of Aesculus multiflorus extract, and 10-15 parts of Herba schizonepetae extract; Auxiliary materials: 10-15 parts of astragalus polysaccharide, 5-8 parts of angelica volatile oil, 3-5 parts of ligustrazine, and 2-3 parts of nano-silicon dioxide.

3. The Yao medicine-specific potent external plaster for treating acute joint pain caused by gout according to claim 2, characterized in that: The mass ratio of the borneol to the mint ice is 1:1, and the total amount added accounts for 5%-8% of the total weight of the mixture.

4. The Yao medicine-specific potent external plaster for treating acute joint pain caused by gout according to claim 3, characterized in that: The surface of the coating layer of the patch is covered with a microporous breathable membrane with a pore size of 5-10 μm and an air permeability of ≥2000 g / m²·24h.

5. The Yao medicine-specific potent external plaster for treating acute joint pain caused by gout according to claim 4, characterized in that: The matrix is ​​a composite matrix composed of beeswax and vaseline in a mass ratio of 3:

7.

6. The Yao medicine-specific potent external plaster for treating acute joint pain caused by gout according to claim 5, characterized in that: The preparation method of the Tripterygium wilfordii extract comprises: The rhizome of Tripterygium wilfordii was crushed and ultrasonically extracted twice with 70% ethanol. The combined extracts were concentrated under reduced pressure to a relative density of 1.2-1.3, and freeze-dried to obtain an extract.

7. The Yao medicine-specific potent external plaster for treating acute joint pain caused by gout according to claim 6, characterized in that: The oil is a mixed oil composed of soybean oil and sesame oil in a mass ratio of 6:

4.

8. The Yao medicine-specific potent external plaster for treating acute joint pain caused by gout according to claim 7, characterized in that: The oil is a mixed oil composed of soybean oil and sesame oil in a mass ratio of 6:

4.

9. The Yao medicine-specific potent external plaster for treating acute joint pain caused by gout according to claim 8, characterized in that: The particle size of the medicinal powder is 80-100 mesh, and the powder is ultrafinely pulverized to a specific surface area of ​​≥5m² / g.

10. The Yao medicine-specific strong external-use plaster for treating acute joint pain caused by gout according to claim 9, characterized in that: The packaging material of the patch is an aluminum-plastic composite film, and the interior is filled with nitrogen to isolate oxygen.

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