A traditional Chinese medicine composition for treating acute joint soft tissue injury and application thereof

Abstract

The present application relates to the technical field of acute joint soft tissue injury treatment medicine, and in particular to a traditional Chinese medicine composition for treating acute joint soft tissue injury and application thereof. In terms of weight parts, the raw materials of the efficacy components of the traditional Chinese medicine composition of the present application include 90-110 parts of gardenia, 180-220 parts of hibiscus leaf, 90-110 parts of cortex phellodendri, 90-110 parts of rhubarb, 45-55 parts of safflower, and 45-55 parts of turmeric. The present technical solution is used to solve the technical problem that the prior art lacks a traditional Chinese medicine external preparation which has definite curative effect, high safety, convenient use, and is precisely targeted at acute lateral malleolus ligament injury with qi stagnation and blood stasis syndrome. The composition of the present application not only can quickly relieve acute stage swelling, pain and blood stasis, but also can protect joint structure through multi-target, and has good industrialization and market promotion value.

Description

Technical Field

[0001] This invention relates to the field of pharmaceutical technology for treating acute joint soft tissue injuries, specifically to a traditional Chinese medicine composition for treating acute joint soft tissue injuries and its application. Background Technology

[0002] Acute soft tissue injury of the joint is one of the most common musculoskeletal injuries in clinical practice. It refers to acute contusions or tears in the soft tissues around the joint, such as ligaments, tendons, and joint capsules, caused by external force. It can occur in multiple locations, including the ankle, knee, wrist, and elbow. These injuries are usually caused by direct or indirect force, or excessive twisting. Clinically, they mainly manifest as local pain, swelling, subcutaneous ecchymosis, limited joint movement, and impaired weight-bearing function. If not treated properly in the early stages, they can develop into sequelae such as chronic joint instability and traumatic arthritis, severely affecting the patient's motor function and quality of life.

[0003] Currently, Western medicine treatment for acute joint soft tissue injuries generally follows the RICE principle (rest, ice, compression bandage, and elevation of the affected limb), combined with drug intervention. Nonsteroidal anti-inflammatory drugs (NSAIDs) are the most commonly used drugs for relieving pain and improving function. For mild to moderate pain, topical NSAIDs, such as flurbiprofen gel patches, are preferred; for moderate to severe pain, a combination of topical and oral NSAIDs can be used. However, the above treatment regimens have many limitations. Common adverse reactions of oral NSAIDs include gastrointestinal damage (such as nausea, vomiting, diarrhea, gastrointestinal bleeding, indigestion, etc.), neurological symptoms (such as headache, dizziness, drowsiness, etc.), and allergic reactions (such as rash, itching, etc.), and can also cause elevated transaminase levels. Patients with a history of gastrointestinal disease, cardiovascular disease, liver or kidney dysfunction, or other underlying conditions should not use oral NSAIDs. Topical NSAIDs can also cause local skin reactions such as itching, redness, and rashes, and may even cause serious adverse reactions such as shock and asthma. Furthermore, their use is restricted on damaged skin.

[0004] In existing TCM clinical practice, external treatments such as topical application of Chinese medicine are often used to achieve the effects of promoting blood circulation, reducing swelling, relaxing muscles and tendons, and promoting the repair of local tissues. For example, the existing technology (Liu Yusong, Wang Jian. Treatment of 68 cases of acute ankle sprain by topical application of Chinese medicine combined with bloodletting and cupping[J]. Journal of Practical Traditional Chinese Medicine, 2002, (4) 40.) discloses a method of treating acute ankle sprain by topical application of Chinese medicine combined with bloodletting and cupping. The method adopts different topical application strategies according to the time of injury: for those injured within 24 hours, the affected area is first cold-applied with ice or cold water, and then the empirical formula "swelling-reducing ointment" (the main ingredients are Scutellaria baicalensis, rhubarb, gardenia, turmeric, Phellodendron chinense, hibiscus flower leaves, etc.) is applied, and bandages are used for targeted bandaging and fixation; for those injured more than 24 hours later, the affected area is first heavily tapped with a dermal needle to induce bleeding and cupping is performed, and then the empirical formula "blood-activating and pain-relieving ointment" is applied after removing the cups. The plan emphasizes early cold compresses to control ruptured blood vessels and external application of traditional Chinese medicine to promote blood circulation and remove blood stasis.

[0005] According to traditional Chinese medicine theory, acute soft tissue injuries of joints fall under the category of "tendon injuries." The pathogenesis involves external force leading to damage to the meridians, blood leakage from the vessels, qi stagnation and blood stasis, and obstruction of the meridians, resulting in pain. The *Yizong Jinjian* states, "When the bone joints are misaligned, qi and blood stagnate," indicating that after a tendon injury, qi and blood stagnation obstructs the meridians, leading to impaired joint movement. Taking the most representative acute lateral malleolar ligament injury as an example, its primary TCM syndrome is qi stagnation and blood stasis. The *Expert Consensus on External Treatment of Acute Lateral Malleolar Ligament Injuries with Traditional Chinese Medicine* first proposed a three-stage external treatment plan: "cooling the blood and stopping bleeding, promoting blood circulation and removing blood stasis, and harmonizing the body and promoting new blood production." The publication of this consensus provides evidence-based support for the standardized TCM treatment of acute lateral malleolar ligament injuries, and its treatment principles also have important guiding significance for acute soft tissue injuries of other joints throughout the body.

[0006] In conclusion, developing a topical Chinese medicine preparation that is effective and safe for acute soft tissue injuries of joints has significant clinical and market value. Summary of the Invention

[0007] The present invention aims to provide a traditional Chinese medicine composition for treating acute joint soft tissue injuries, in order to solve the technical problem of the lack of existing external traditional Chinese medicine preparations that are effective, safe, easy to use, and precisely target the qi stagnation and blood stasis syndrome of acute joint soft tissue injuries.

[0008] To achieve the above objectives, the present invention adopts the following technical solution: In a first aspect, the present invention provides a traditional Chinese medicine composition for treating acute joint soft tissue injuries.

[0009] The traditional Chinese medicine composition, by weight, comprises the following raw materials for its active ingredients: 90-110 parts of gardenia, 180-220 parts of hibiscus leaves, 90-110 parts of phellodendron bark, 90-110 parts of rhubarb, 45-55 parts of safflower, and 45-55 parts of turmeric.

[0010] As a preferred technical solution, the raw materials of the active ingredients, by weight, include: 95-105 parts of gardenia, 190-210 parts of hibiscus leaves, 95-105 parts of phellodendron bark, 95-105 parts of rhubarb, 48-52 parts of safflower, and 48-52 parts of turmeric.

[0011] As a further preferred technical solution, the raw materials of the effective ingredients, by weight, include: 100 parts of gardenia, 200 parts of hibiscus leaves, 100 parts of phellodendron bark, 100 parts of rhubarb, 50 parts of safflower, and 50 parts of turmeric.

[0012] As a preferred technical solution, the raw materials of its active ingredients also include 5-25 parts of borneol and / or 15-40 parts of menthol by weight.

[0013] Secondly, the present invention provides a method for preparing the traditional Chinese medicine composition.

[0014] Gardenia, Hibiscus mutabilis leaves, rhubarb, Phellodendron bark, safflower, and turmeric were extracted using water extraction and / or alcohol extraction.

[0015] As a preferred technical solution, the alcohol extraction method is ethanol reflux extraction, the volume fraction of ethanol is 60% to 95%, the amount of ethanol used each time is 6 to 15 times the total weight of the medicinal materials, the number of extractions is 1 to 4 times, and the extraction time for each extraction is 0.5 to 3 hours; the extracts from each ethanol reflux extraction are combined to obtain an alcohol extraction mixture.

[0016] As a preferred technical solution, the water extraction method involves adding water and decocting, with the amount of water added each time being 6 to 15 times the total weight of the medicinal materials, and the number of decoctions being 1 to 4 times, with each decoction lasting 0.5 to 3 hours; the decoctions extracted from each decoction are combined to obtain a decoction mixture. After concentration, an extract with a relative density of 1.10 to 1.30 at 50-60℃ is obtained from the alcohol extraction mixture or the decoction mixture.

[0017] As a further preferred technical solution, the alcohol extraction method is as follows: Gardenia, Hibiscus mutabilis leaves, rhubarb, Phellodendron amurense, safflower, and turmeric are each pulverized into coarse powder and passed through a 10-mesh sieve. They are mixed evenly, and an 80% (v / v) ethanol solution is added for reflux extraction three times. For the first extraction, 11 times the volume of ethanol solution is added, and the mixture is refluxed for 1.5 hours. For the second extraction, 9 times the volume of ethanol solution is added, and the mixture is refluxed for 1.5 hours. For the third extraction, 9 times the volume of ethanol solution is added, and the mixture is refluxed for 1.5 hours. The extract is filtered and the extract is collected. The extracts are combined to obtain an alcohol extract mixture. The alcohol extract mixture is concentrated at 50-60℃ to a relative density of 1.10-1.30 to obtain the extract.

[0018] As a further preferred technical solution, the water extraction method is as follows: Gardenia, Hibiscus mutabilis leaves, rhubarb, Phellodendron amurense, safflower, and turmeric are taken, crushed into coarse powder and passed through a 10-mesh sieve, mixed evenly, and decocted twice with water. The first time, 12 times the amount of water is added and decocted for 1.5 hours. The second time, 10 times the amount of water is added and decocted for 1.5 hours. The decoctions are filtered, and the decoctions are combined to obtain a decoction mixture. The decoction mixture is concentrated at 50-60℃ to a relative density of 1.10-1.30 to obtain the extract.

[0019] Thirdly, the present invention provides a product containing the aforementioned traditional Chinese medicine composition.

[0020] The product is a topical preparation, preferably any one of the following: plaster, gel, ointment, spray, lotion, liniment, or paste.

[0021] As a preferred technical solution, the product is a topical plaster, and the topical plaster uses a rubber-based matrix or a pressure-sensitive adhesive matrix.

[0022] As a further preferred technical solution, the rubber matrix includes a rubber matrix and any one of a tackifying resin, a softener, and an antioxidant added to the rubber matrix.

[0023] As a further preferred technical solution, the rubber matrix is ​​selected from one or more of natural rubber, styrene-butadiene rubber, and polyisobutylene rubber. This rubber matrix has good adhesion and good skin compatibility, making it suitable for long-term application.

[0024] As a preferred technical solution, the pressure-sensitive adhesive matrix is ​​a solvent-based pressure-sensitive adhesive or a hot-melt pressure-sensitive adhesive.

[0025] As a further preferred technical solution, the pressure-sensitive adhesive matrix is ​​composed of the following raw materials in parts by weight: 20-80 parts of styrene-isoprene-styrene (SIS), 15-80 parts of hydrogenated rosin glycerol ester, 10-50 parts of polyisobutylene, 8-50 parts of liquid paraffin, and 0.5-2 parts of butylated hydroxytoluene (BHT). As a further preferred technical solution, the external plaster is prepared by the following method: heating and melting the pressure-sensitive adhesive matrix, then mixing it evenly with the extract components, borneol and menthol to form a coating; applying the coating and cutting it to obtain the external plaster.

[0026] As a preferred technical solution, the product is a gel, ointment, spray, lotion, liniment, or paste.

[0027] Fourthly, the present invention provides the use of the traditional Chinese medicine composition in the preparation of a medicament for treating acute joint soft tissue injury.

[0028] As a preferred technical solution, the drug can be used to improve pain, swelling and / or local tenderness caused by acute joint soft tissue injury, improve the flexion and extension range of motion of the injured joint, and / or improve the weight-bearing function and walking stability of the injured joint.

[0029] As a preferred technical solution, the joint is the ankle joint, knee joint, wrist joint, or elbow joint. These joints are all joints with a high degree of mobility, heavy load, and are prone to injury. The composition of the present invention has good therapeutic effects on acute soft tissue injuries in these areas.

[0030] As a preferred technical solution, the soft tissue injury is a ligament injury, tendon injury, and / or joint capsule injury. Ligaments, tendons, and joint capsules are all important stabilizing structures of joints, and are prone to traction, tearing, or even rupture under acute external forces. The composition of the present invention has a repairing and protective effect on acute and chronic injuries to these soft tissue structures.

[0031] As a further preferred technical solution, the drug is used to treat soft tissue injuries at the site of injury; As a further preferred technical solution, the drug is used to improve pain, swelling and / or local tenderness caused by acute joint soft tissue injury, and / or improve the flexion and extension range of motion of the injured joint, and / or improve the weight-bearing function and walking stability of the injured joint, and / or improve the smoothness of the cartilage surface, and / or inhibit the formation of pannus.

[0032] The technical principle of this technical solution is as follows: Acute soft tissue injury of the joint falls under the category of "muscle dislocation and bone misalignment" in traditional Chinese medicine. The injury causes local blood vessels to break down and blood to spill out of the vessels, resulting in qi stagnation and blood stasis. The early pathogenesis is internal obstruction of blood stasis, local heat, swelling and pain. The treatment should adhere to the principles of "cooling blood and stopping bleeding, promoting blood circulation and removing blood stasis, and harmonizing the body and generating new blood" in the acute phase.

[0033] The traditional Chinese medicine composition of this invention is formulated according to the principle of monarch, minister, assistant, and guide: the monarch is gardenia and hibiscus leaf; the minister is rhubarb and phellodendron; the assistant is safflower and turmeric; and the guide is borneol and menthol.

[0034] Hibiscus mutabilis leaves are cold in nature and are effective in cooling the blood, reducing swelling, detoxifying, and relieving pain. They are specifically used to treat external injuries with blood heat and swelling. Gardenia is bitter and cold, clearing local heat and stasis, cooling the blood, and dispersing blood stasis. Together, they form the principal herbs, directly targeting the core symptoms of subcutaneous bleeding, redness, swelling, and burning in the acute phase, achieving rapid blood cooling, hemostasis, and dissipation of local heat and stasis. Phellodendron bark clears heat, dries dampness, reduces swelling, and astringes sores, relieving inflammatory redness and swelling at the injury site, and assisting the principal herbs in enhancing their heat-clearing, blood-stasis-dispersing, swelling-reducing, and pain-relieving effects. Rhubarb promotes blood circulation, removes blood stasis, breaks up accumulations, and reduces swelling, clearing the obstructed qi and blood in the injured area. Turmeric promotes blood circulation. This formula promotes qi circulation, removes blood stasis, unblocks meridians, and relieves pain, addressing both qi stagnation and blood stasis after injury, as well as joint stiffness. Safflower invigorates blood circulation, unblocks meridians, removes blood stasis, and relieves pain, specifically targeting the blood to resolve subcutaneous blood stasis. Menthol provides cooling relief, reduces itching, swelling, and pain, working synergistically with borneol to enhance transdermal absorption efficiency, while also alleviating the burning discomfort caused by patch application, harmonizing the overall cold properties of the formula, and reducing external irritation. Borneol's aromatic properties guide the active ingredients through the skin and fascia to reach the injured ligaments and lesions. The combined use of menthol and borneol with the aforementioned six herbs significantly increases the transdermal penetration rate of the drug, enhancing the local cooling and analgesic effects.

[0035] In this formula, safflower plays a crucial synergistic role. This invention selects safflower as an adjuvant, forming a synergistic combination with the principal ingredient, Hibiscus mutabilis leaf, and the assistant ingredient, Gardenia jasminoides. The principal and assistant ingredients focus on clearing local superficial redness, swelling, heat, and pain, while safflower can penetrate deep into soft tissues, dispersing stagnant blood stasis and guiding the heat-clearing medicinal power deep into the lesion. The combination of safflower with the principal and assistant ingredients addresses both the clearing of superficial inflammation and the dissipation of deep blood stasis, forming a "treating both the exterior and interior, and using medication in layers" logic, which differs from traditional external application formulas that solely clear heat or solely promote blood circulation.

[0036] Meanwhile, safflower and turmeric work synergistically to repair damaged lesions. Their combined use significantly enhances the effects of promoting qi and blood circulation. Comparative experiments show that removing safflower significantly reduces the repair effect of turmeric alone, suggesting that their combination as adjuvant herbs is a key combination for restoring joint function in this formula.

[0037] The comparative efficacy experiment further clarified the specific contribution of safflower in the compound formula. Data showed that formulas lacking safflower, using reduced amounts of safflower, or replacing safflower with Panax notoginseng or Scutellaria baicalensis all exhibited varying degrees of reduced overall efficacy. Analysis suggests that while Panax notoginseng can invigorate blood circulation, it is inferior to safflower in penetrating deep into the meridians and improving joint biomechanics; while Scutellaria baicalensis is good at clearing heat, it lacks the medicinal characteristics of invigorating blood circulation, removing blood stasis, and repairing soft tissues. In this formula, safflower exerted a comprehensive effect of penetrating deep into the meridians, dispersing blood stasis, and repairing joint damage—something difficult to achieve with equivalent substitutions or single-effect replacements of other commonly used traumatic medicines.

[0038] In summary, the composition of this treatment, when applied percutaneously to the joint soft tissue injury lesion, exerts a multi-target synergistic repair effect: it blocks pannus formation, thereby inhibiting pathological proliferation and microvascular angiogenesis of the synovium; it protects the hyaline cartilage of the joint, maintains the integrity and smoothness of the cartilage surface, reduces cartilage erosion and defects, and alleviates secondary organic cartilage lesions; it accelerates the metabolism and absorption of local blood stasis, repairs damaged ligaments and soft tissues, improves the joint biomechanical structure, enhances the weight-bearing capacity of the affected foot, and improves symptoms of joint instability and pain during movement.

[0039] Compared with existing technologies, the advantages of this technical solution are as follows: (1) To achieve effective treatment of joint soft tissue injuries Compared to other topical patches in the prior art, the composition of this invention is specifically designed for the acute phase of acute joint soft tissue injury characterized by qi stagnation and blood stasis. It strictly adheres to the industry expert consensus on the three-stage early treatment principle of "cooling the blood and stopping bleeding, promoting blood circulation and removing blood stasis, and harmonizing the body and promoting new blood production." The composition has a clear division of labor, effectively improving symptoms such as redness, swelling, heat, pain, subcutaneous hematoma, and joint instability. Animal pathological experiments have confirmed that the formulation of this invention can significantly reduce inflammatory cell infiltration at the injury site, inhibit pannus formation, maintain the smoothness and integrity of the cartilage surface, effectively repair ligaments and soft tissues, and improve the supporting strength of the affected foot, demonstrating outstanding efficacy.

[0040] The composition of this invention can not only quickly relieve swelling, pain and bruising in the acute phase, but also protect the joint structure at multiple targets: inhibiting excessive local inflammatory infiltration, blocking pannus from eroding cartilage, repairing damaged soft tissue, and maintaining cartilage integrity, thus possessing important clinical preventive and therapeutic value.

[0041] (2) High security This invention is a topical preparation that applies the medication directly to the site of injury, eliminating the need for oral administration and completely avoiding systemic side effects such as gastrointestinal damage, hepatotoxicity, nephrotoxicity, and neurological discomfort caused by oral nonsteroidal anti-inflammatory drugs (NSAIDs). The addition of borneol and menthol balances the cooling properties of the medication, resulting in a low-allergenic and mild base that significantly reduces the risk of local irritation such as skin redness, itching, and rashes. It is safe for use by individuals with gastrointestinal diseases, cardiovascular diseases, or hepatic and renal insufficiency who are intolerant to oral anti-inflammatory drugs, thus broadening its applicability. Attached Figure Description

[0042] Figure 1 The image shows a representative stained tissue section of ankle joint tissue from Experiment 1 (magnification: ×100). Detailed Implementation

[0043] Unless otherwise defined, all technical terms in this document have the same meanings as commonly understood by one of ordinary skill in the art to which the subject matter of the claims pertains. Unless otherwise stated, all patents, patent inventions, and publications cited in this document are incorporated herein by reference in their entirety. If multiple definitions exist for terms in this document, the definitions in this chapter shall prevail.

[0044] First, the present invention provides a traditional Chinese medicine composition for treating acute joint soft tissue injury, the raw materials of which, by weight, include: 90-110 parts of gardenia, 180-220 parts of hibiscus leaves, 90-110 parts of phellodendron bark, 90-110 parts of rhubarb, 45-55 parts of safflower, and 45-55 parts of turmeric.

[0045] Preferably, a traditional Chinese medicine composition for treating acute joint soft tissue injury comprises, by weight, the following raw materials: 95-105 parts of gardenia, 190-210 parts of hibiscus leaf, 95-105 parts of phellodendron bark, 95-105 parts of rhubarb, 48-52 parts of safflower, and 48-52 parts of turmeric.

[0046] Most preferably, a traditional Chinese medicine composition for treating acute joint soft tissue injury comprises, by weight, the following raw materials: 100 parts gardenia, 200 parts hibiscus leaves, 100 parts phellodendron bark, 100 parts rhubarb, 50 parts safflower, and 50 parts turmeric.

[0047] In addition, to enhance the transdermal effect of active ingredients, menthol and / or borneol can be added to the formula, with borneol accounting for 5-25 parts by weight and menthol accounting for 15-40 parts by weight.

[0048] All the above-mentioned raw materials are commercially available products that meet the requirements of Part I - Medicinal Materials and Slices of Chinese Pharmacopoeia 2025 Edition.

[0049] Furthermore, this invention also provides a method for preparing the above-mentioned traditional Chinese medicine composition for treating acute joint soft tissue injuries. The method involves mixing and extracting gardenia, hibiscus leaves, phellodendron bark, rhubarb, safflower, and turmeric to prepare an extract, which is then used in the preparation of a plaster. The specific process is as follows: S1: Mixed Extraction Extraction can be performed by hot reflux using ethanol solution as the solvent, or by decoction using water as the solvent, as detailed below: Alcohol extraction method: Gardenia, Hibiscus mutabilis leaves, rhubarb, Phellodendron amurense, safflower, and turmeric were each coarsely ground (passing through a 10-20 mesh sieve), mixed evenly, and subjected to hot reflux extraction 1-4 times with a 60-95% (v / v) ethanol solution. The amount of ethanol solution used each time was 6-15 times the total weight of the medicinal materials (based on the total weight of the six raw materials, the material-to-liquid ratio was 1 kg: 6-15 L), and the extraction time for each hot reflux extraction was 0.5-3 hours. The extracts from each ethanol reflux extraction were combined through solid-liquid separation to obtain an ethanol-extract mixture. The ethanol-extract mixture was concentrated to obtain an extract with a relative density of 1.10-1.30 (50-60℃).

[0050] Preferably, the alcohol extraction is carried out in the following manner: Gardenia, Hibiscus mutabilis leaves, rhubarb, Phellodendron amurense, safflower, and turmeric were each pulverized into coarse powder and passed through a 10-mesh sieve. The powders were mixed evenly and extracted three times by reflux with an 80% ethanol solution. For the first extraction, 11 times the volume of ethanol solution was added and the mixture was refluxed for 1.5 hours. For the second extraction, 9 times the volume of ethanol solution was added and the mixture was refluxed for 1.5 hours. For the third extraction, 9 times the volume of ethanol solution was added and the mixture was refluxed for 1.5 hours. The extracts were filtered and the extracts were combined to obtain an ethanol-extract mixture. The ethanol-extract mixture was concentrated at 50-60℃ to a relative density of 1.10-1.30 to obtain the extract.

[0051] Water extraction method: Gardenia, Hibiscus mutabilis leaves, rhubarb, Phellodendron amurense, safflower, and turmeric are each ground into coarse powder (passed through a 10-20 mesh sieve), mixed evenly, and water is added at a ratio of 6 to 15 times the total weight of the medicinal materials (based on the total weight of the six raw materials, the material-to-liquid ratio is 1 kg: 6-15 L). The decoction is prepared 1 to 4 times, with each decoction lasting 0.5 to 3 hours. The decoctions are combined and concentrated to a relative density of 1.10 to 1.30 (50-60℃) to obtain the extract.

[0052] Preferably, the water extraction method is carried out in the following manner: Gardenia, Hibiscus mutabilis leaves, rhubarb, Phellodendron amurense, safflower, and turmeric are each ground into coarse powder and passed through a 10-mesh sieve. They are then mixed evenly and decocted twice with water. The first time, 12 times the amount of water is added and the decoction is decocted for 1.5 hours. The second time, 10 times the amount of water is added and the decoction is decocted for 1.5 hours. The decoctions are filtered and combined to obtain a decoction mixture. The decoction mixture is concentrated at 50-60℃ to a relative density of 1.10-1.30 to obtain the extract.

[0053] S2: Preparation of plaster First, the pressure-sensitive adhesive is melted. Under oil bath conditions of 140℃~170℃, the raw materials of the pressure-sensitive adhesive matrix—styrene-isoprene-styrene (SIS), hydrogenated rosin glycerol ester, polyisobutylene, liquid paraffin, and butylated hydroxytoluene (BHT)—are added to the reactor. The mixture is heated until the edges of the colloid melt, then stirred until the colloid is completely melted and mixed. The above raw materials are a classic combination of hot melt pressure-sensitive adhesive (HMPSA) type plaster matrix.

[0054] It should be noted that the pressure-sensitive adhesive matrix raw materials are all commercially available materials in the field, and corresponding products suitable for the preparation of medical plasters can be purchased through commercial channels. The selection and acquisition of the above raw materials are not the key technical improvement points of this solution, and therefore will not be elaborated upon here.

[0055] In the specific scenarios of this solution (the following embodiments and comparative examples), the composition of the pressure-sensitive adhesive matrix is: styrene-isoprene-styrene (SIS), hydrogenated rosin glycerol ester, polyisobutylene, liquid paraffin, and butylated hydroxytoluene (BHT) in a mass ratio of 20-80:15-80:10-50:8-50:0.5-2. Under this composition, the ratio of the active ingredient and the total amount of pressure-sensitive adhesive matrix can be adjusted according to the required drug concentration.

[0056] The method for preparing pressure-sensitive adhesive plaster using the aforementioned pressure-sensitive adhesive is as follows: Styrene-isoprene-styrene (SIS), hydrogenated rosin glycerol ester, polyisobutylene, liquid paraffin, and butylated hydroxytoluene (BHT) are added to a reaction apparatus and heated in an oil bath to 140℃~170℃. The mixture is continuously stirred in a molten state until completely homogeneous. The oil bath temperature is then lowered to 130℃, and the above-mentioned extract, menthol, and borneol are added (menthol and borneol are optional components, added depending on the actual formulation). The mixture is then routinely mixed. Next, vacuum degassing is performed at 130℃, stirring until homogeneous (forming a uniform, transparent, viscous liquid without obvious bubbles) to prepare the coating. Finally, the coating is applied using a coating machine at 80~120℃, covered with a backing, and sliced ​​to obtain the final product.

[0057] It should be further noted that, in addition to the methods described above for preparing the plaster, other types of pressure-sensitive adhesive matrices and rubber-based matrices that meet pharmaceutical requirements can also be used. The rubber-based matrices comprise a rubber matrix and tackifying resins, softeners, and antioxidants added to the rubber matrix; the rubber matrix is ​​selected from one or more of natural rubber, styrene-butadiene rubber, and polyisobutylene rubber. The pressure-sensitive adhesive matrix is ​​a solvent-based pressure-sensitive adhesive or a hot-melt pressure-sensitive adhesive. Solvent-based pressure-sensitive adhesives are uniformly coated and have stable adhesion after drying; hot-melt pressure-sensitive adhesives do not require organic solvents and are safe and environmentally friendly to produce.

[0058] The hibiscus leaves described in this invention are those of the hibiscus plant (Hibiscus mutabilis), belonging to the Malvaceae family. Hibiscus mutabilis Dried leaves of L.

[0059] The gardenia mentioned in this invention is Gardenia jasminoides, a plant of the Rubiaceae family. Gardenia jasminoides The dried, ripe fruit of Ellis.

[0060] The cork tree described in this invention is the cork tree (Phellodendron amurense), a plant belonging to the Rutace Phellodendron chinense The dried bark of Schneid.

[0061] The rhubarb described in this invention is Rheum palmatum, a plant belonging to the Polygonaceae family. Rheumatism palmatum L., Tangut Rhubarb Rheumatism tangential Maxim. ex Balf. or medicinal rhubarb RhubarbDried roots and rhizomes of Baill.

[0062] The turmeric mentioned in this invention is the turmeric plant of the ginger family. Curcuma longa The dried rhizome of L.

[0063] The safflower mentioned in this invention is the safflower plant of the Asteraceae family. Safflower Dried flowers of L.

[0064] The menthol described in this invention is from the Lamiaceae plant *Mentha*. Mint haplocalyx A saturated cyclic alcohol, 1-1-methyl-4-isopropylcyclohexanol-3, is obtained by steam distillation, freezing, and recrystallization of the fresh stems and leaves of Briq.

[0065] The borneol described in this invention is camphor, a plant of the Lauraceae family. Cinnamon camphor (L.)Presl is made from the fresh branches and leaves through extraction and processing; or it may be a synthetic borneol.

[0066] The preparation method of this invention adopts two technical routes: water extraction and alcohol extraction. The choice can be made flexibly according to actual production conditions and dosage form requirements. Among them, water extraction is low-cost, safe and environmentally friendly, and suitable for large-scale production; alcohol extraction is more effective in extracting fat-soluble components (such as curcumin, rhubarb anthraquinones, safflower yellow pigment, etc.) and has a high retention rate of bioactive substances. Both methods can yield extracts with good pharmacological activity.

[0067] The traditional Chinese medicine composition described in this invention can be supplemented with pharmaceutically acceptable excipients and prepared into various external dosage forms according to conventional methods in the art. Plasters are easy to fix and provide sustained drug release; gels have good spreadability and offer a cooling and comfortable sensation; ointments provide occlusion and moisturization, facilitating drug penetration; sprays are convenient to use and avoid secondary contact that could cause injury; lotions are suitable for large-area injuries; liniments are easy to apply and massage locally; and pastes are suitable for astringent protection of exudative injuries. Different dosage forms can meet the clinical needs of different injury sites and different usage scenarios.

[0068] The preferred dosage form of the present invention is a patch, which has the following advantages: convenient administration and can be operated by the patient; the drug is in close contact with the skin, forming a closed environment and promoting transdermal absorption; the drug can be released continuously, prolonging the duration of action; and it provides physical protection to the injured site and restricts excessive joint movement.

[0069] The solvent-based pressure-sensitive adhesive of this invention has uniform coating and stable adhesion after drying; the hot-melt pressure-sensitive adhesive does not require organic solvents and is safe and environmentally friendly to produce.

[0070] In the pressure-sensitive adhesive matrix composition of this invention, SIS serves as a thermoplastic elastomer matrix material, imparting good cohesiveness and elasticity to the patch; hydrogenated rosin glyceryl ester is a tackifying resin, improving the initial tack and holding power of the patch to the skin; polyisobutylene is a toughening agent, improving low-temperature performance and flexibility; liquid paraffin is a plasticizer and softener, adjusting the hardness of the matrix and improving coating performance; and butylated hydroxytoluene is an antioxidant, preventing matrix aging and deterioration. The above components are combined to prepare a high-quality patch with moderate viscosity, good breathability, low skin irritation, and stable drug release.

[0071] The present invention will be further described in detail below with reference to embodiments, but the embodiments of the present invention are not limited thereto. Unless otherwise specified, the technical means used in the following embodiments and experimental examples are conventional means well known to those skilled in the art, and the materials, reagents, etc. used are all commercially available. Unless otherwise specified, the technical means used in the following embodiments are conventional means well known to those skilled in the art.

[0072] Example 1 The purpose of this embodiment is to provide a superior formulation and process for preparing a traditional Chinese medicine composition for treating acute joint soft tissue injuries, as detailed below: Formula: 100 parts gardenia, 200 parts hibiscus leaves, 100 parts phellodendron bark, 100 parts rhubarb, 50 parts safflower, 50 parts turmeric, 10 parts borneol, and 20 parts menthol.

[0073] Preparation process: Gardenia, Hibiscus mutabilis leaves, rhubarb, Phellodendron amurense, safflower, and turmeric were pulverized into coarse powder and passed through a 10-mesh sieve. They were mixed evenly and extracted three times by reflux with 80% ethanol solution. For the first extraction, 11 times the volume of ethanol solution was added and the mixture was refluxed for 1.5 hours. For the second extraction, 9 times the volume of ethanol solution was added and the mixture was refluxed for 1.5 hours. For the third extraction, 9 times the volume of ethanol solution was added and the mixture was refluxed for 1.5 hours. The extracts were filtered and the extracts were combined to obtain an alcoholic extract mixture. The alcoholic extract mixture was concentrated at 50℃ to a relative density of 1.10-1.30 to obtain extract A1.

[0074] The obtained extract A1, borneol, and menthol were added to the molten pressure-sensitive adhesive matrix according to the set drug concentration to prepare a plaster. Specifically, for the pressure-sensitive adhesive matrix, the mass ratio of styrene-isoprene-styrene (SIS), hydrogenated rosin glycerol ester, polyisobutylene, liquid paraffin, and butylated hydroxytoluene (BHT) was 50:50:30:30:1.

[0075] The specific preparation process is as follows: the above-mentioned matrix components are put into the reaction equipment and heated to 150°C in an oil bath. The mixture is stirred continuously in the molten state of the oil bath until it is completely mixed and homogeneous. Then, the oil bath temperature is lowered to 130°C, and extract A1, borneol and menthol are added in the proportions of the above-mentioned formula and mixed evenly. Next, vacuum degassing is performed at an oil bath temperature of 130°C, and the mixture is stirred until a uniform, transparent, viscous liquid without obvious bubbles is formed to make a coating. Finally, the coating machine temperature is controlled at 100°C, and the coating is applied, covered, and sliced ​​to obtain the plaster.

[0076] Example 2 This embodiment provides a traditional Chinese medicine composition for treating acute joint soft tissue injury. The difference between this composition and Example 1 is that the formula lacks borneol and menthol, in order to observe the effect of aromatic penetration-enhancing components on the overall efficacy and transdermal absorption of the formula.

[0077] The formula is as follows: 100 parts gardenia, 200 parts hibiscus leaves, 100 parts phellodendron bark, 100 parts rhubarb, 50 parts safflower, and 50 parts turmeric.

[0078] The preparation method is the same as described in Example 1, and extract A2 is prepared for later use.

[0079] The obtained extract A2 was added to the molten pressure-sensitive adhesive matrix according to the set drug concentration, and the plaster was prepared by conventional methods. Specifically, for the pressure-sensitive adhesive matrix, the mass ratio of styrene-isoprene-styrene (SIS), hydrogenated rosin glycerol ester, polyisobutylene, liquid paraffin, and butylated hydroxytoluene (BHT) was 50:50:30:30:1.

[0080] The specific preparation method of the plaster is as described in Example 1.

[0081] Experimental Example 1: Pharmacological Experiment 1.1 Experimental Modeling and Drug Administration SPF-grade Balb / c mice, half male and half female, were selected. An ankle sprain model was induced using the impact method. The specific procedure was as follows: The left hind limb of the model group mice was shaved and prepared. First, the left hind foot of the mouse was rotated 180° inward from its normal position and the plantar flexion was 180°, 100 times / minute, for 4 minutes. Then, the mouse was fixed on a piece of cardboard, and a 400g standard weight was dropped freely from a height of 10cm onto the left hind ankle joint using a self-made impact table. Palpation confirmed no fracture or dislocation. After modeling, mice with significant swelling at the model site were selected as animals for the acute ankle sprain model.

[0082] Ten normal mice were used as a blank control group. The successfully modeled ankle sprained mice were randomly divided into groups of 10 each. The groups were as follows: model control group (no drug treatment), positive drug group (Yunnan Baiyao plaster), clinical dose group of Example 1 (prepared in Example 1), high dose group of Example 1 (prepared in Example 1), and blank matrix group (except that the plaster did not contain the drug, it was consistent with Example 1).

[0083] Each group underwent regular skin preparation of the ankle area. Before daily administration, the plaster (containing extract and matrix, with identical matrix and preparation methods for each group) was cut to an area of ​​1cm × 1cm. Mice in each group applied the corresponding amount of test substance or control directly to the ankle joint of the left hind limb, securing the plaster with breathable medical adhesive tape to prevent it from falling off. Administration was once daily for 10 consecutive days. Regarding dosage, based on mouse body weight (20g), the dosage for the clinical dose group in Example 1 was 8g of raw medicinal materials / kg (Note: the amount of raw medicinal materials mentioned here and below refers to the total amount of medicinal herbs such as Hibiscus mutabilis leaves, Gardenia jasminoides, Carthamus tinctorius, and Curcuma longa in the prescription; borneol and menthol are not included in the total raw medicinal material count); the dosage for the high-dose group in Example 1 was set at 16g of raw medicinal materials / kg. The model control group and blank control group did not receive any treatment.

[0084] 1.2 Detection Indicators (1) Before administration (D0), on the fourth day after administration (D4) and the day after the last administration, the animals in each group were observed and scored for the signs of bruising, swelling and other damage at the administration site and surrounding tissues. The scoring criteria are detailed in Table 1.

[0085] Table 1: Observation Indicators and Scoring Standards for the Degree of Soft Tissue Injury

[0086] (2) The hind limb support force was detected using a mouse bipedal balance analgesia tester, and the difference in support force between the two hind limbs was calculated. Specifically, the mice were placed in an experimental chamber with their forelimbs resting on an inclined support plate and their hind limbs standing independently in a natural exploratory posture. The left and right hind limbs were ensured to be fully positioned on the two pressure sensor plates, and the tail was placed in the narrow slot at the rear of the chamber and fully extended outside the chamber to prevent tail weight-bearing from interfering with the data. During the measurement, the pressure-bearing values ​​of the left and right hind limbs of the mice were continuously collected within 10 seconds. The difference in pressure between the healthy and affected hind limbs was calculated, and the average of three measurements was taken as the final indicator for the ankle pain behavior test of a single mouse.

[0087] (3) On the day after the last administration, mice in each group (including blank control group, model control group, blank matrix group, positive drug group, clinical dose group of Example 1 and high dose group of Example 1) were euthanized by cervical dislocation. Ankle joint tissue was taken, fixed in 10% neutral formalin solution, embedded in paraffin, sectioned, stained with HE, and observed under a microscope for morphological changes in the ankle joint and surrounding tissues.

[0088] 1.3 Experimental Results (1) Ankle sprain injury score (score criteria refer to Table 1) Table 2: Scoring results of soft tissue injury severity in mice ( (n=10)

[0089] Note: Compared with the blank control group, ++P < 0.01; compared with the model control group, *P < 0.05, **P < 0.01.

[0090] The experimental results are shown in Table 2. Compared with the blank control group, the ankle sprain injury score of the model control group was significantly increased on D0, D4, and the day after the last administration (P < 0.01), indicating that the impact method combined with excessive flexion effectively induced an acute soft tissue injury model of the mouse ankle joint. Furthermore, the model recovered slowly under natural conditions, exhibiting persistent subcutaneous ecchymosis, muscle swelling, and limited mobility. Compared with the model control group, the injury score of the positive drug group was significantly reduced on D4 (P < 0.05), and the injury scores of the clinical dose group and the high dose group of Example 1 were both significantly reduced (P < 0.01), indicating that the plaster of this invention has a certain onset speed and can improve local exudation and swelling in the early stage. Its efficacy at this stage is similar to that of commercially available Yunnan Baiyao plaster. By the day after the last administration, the score of the high dose group of Example 1 further decreased to 0.5 ± 0.5, showing a highly significant difference compared with the model group (P < 0.01), and the score was lower than that of the positive drug group and the clinical dose group of Example 1, showing a certain dose-response trend. The scores of the blank matrix group were similar to those of the model group, suggesting that the physical covering and protective effect of the pressure-sensitive adhesive matrix itself had little impact on the therapeutic effect, indicating that the active pharmaceutical ingredients played a major role in the treatment.

[0091] (2) Bipedal support force test Table 3: Effect of plaster on the difference in foot support force in a mouse ankle sprain model ( (n=10)

[0092] Note: Compared with the blank control group, ++P < 0.01; compared with the model control group, *P < 0.05.

[0093] The experimental results are shown in Table 3. The difference in bipedal support strength reflects, to some extent, the tendency of mice to avoid weight-bearing due to pain and mechanical injury in the affected limb. Compared with the blank control group, the difference in bipedal support strength in the model control group was significantly increased on D0, D4 and the day after the last administration (P < 0.01), indicating that the sprain caused significant mechanical pain sensitization and motor dysfunction.

[0094] Compared with the model control group, although the differences in weight-bearing capacity among the treatment groups showed a decreasing trend on day 4, there was no statistically significant difference, suggesting that the improvement in weight-bearing function may lag behind the recovery of apparent morphology. On the day after the last administration, the differences in bipedal support strength in the positive control group, the clinical dose group of Example 1, and the high dose group of Example 1 were all significantly reduced (P < 0.05), decreasing to 3.0 ± 0.8 g, 3.1 ± 0.6 g, and 2.9 ± 1.0 g, respectively. This result indicates that the plaster of this invention can not only significantly improve superficial swelling and other pathological conditions, but also have a positive effect on damaged ligaments and joint capsules and other stress-bearing structures, contributing to the recovery of ankle joint biomechanical support and weight-bearing function.

[0095] (2.3) Histopathological results like Figure 1 As shown, the ankle cartilage surface of mice in the blank control group was smooth and intact with a clear structure, and no obvious inflammatory cell infiltration or pannus formation was observed. In contrast, the ankle cartilage surface of mice in the model control group showed obvious roughness and damage, with a small amount of inflammatory cell infiltration and mild pannus formation visible in some areas, indicating that acute sprain successfully induced pathological damage to the joint microstructure.

[0096] Observations after drug administration revealed no significant improvement in inflammatory cell infiltration in any of the drug-treated groups compared to the model group. This may be due to the short drug administration period in this experiment, which prevented the full manifestation of the drug's clearing and regulating effects on local acute inflammatory cell infiltration, resulting in no significant differences in microscopic morphology between the groups. Regarding cartilage surface smoothness and pannus, each drug-treated group exhibited varying degrees of morphological changes. Specifically, the clinical dose group in Example 1 showed relatively mild cartilage surface damage and a smoother surface, demonstrating the strongest repair and improvement effect. The high-dose group in Example 1 showed a better inhibitory trend in pannus morphology, but its cartilage surface improvement was less than that of the clinical dose group. While the positive control group showed a certain numerical decrease in cartilage surface and pannus morphology compared to the model group, the overall morphological improvement was less than that of the clinical dose group in Example 1.

[0097] Analysis reveals that cartilage surface damage and pannus formation are crucial factors affecting subsequent joint recovery in the pathological progression of acute soft tissue injury. The clinical-dose plaster of this invention demonstrates a statistically significant advantage in improving cartilage surface smoothness. Its rational formulation and clinical dosage facilitate drug penetration into the synovial membrane and subchondral microcirculation, thereby inhibiting local angiogenesis and promoting cartilage matrix repair to a certain extent. Regarding deep structural protection, the high-dose group did not show a superior overall effect compared to the clinical-dose group; in fact, its cartilage surface improvement effect was weaker than that of the clinical-dose group, indicating that the clinical dosage has achieved a relatively optimal pharmacological balance.

[0098] Comparative Example 1 This comparative example provides a traditional Chinese medicine composition for treating acute joint soft tissue injury. The difference between this composition and Example 1 is that the formula lacks safflower, so as to observe the effect of the lack of the main medicine for promoting blood circulation and removing blood stasis on the efficacy.

[0099] The formula is as follows: 100 parts gardenia, 200 parts hibiscus leaves, 100 parts phellodendron bark, 100 parts rhubarb, 50 parts turmeric, 10 parts borneol, and 20 parts menthol. The preparation method is the same as described in Example 1, and extract B1 is prepared for later use; The obtained extract B1, borneol, and menthol were added to the molten pressure-sensitive adhesive matrix according to the set drug concentration, and the plaster was prepared using conventional methods. Specifically, the mass ratio of styrene-isoprene-styrene (SIS), hydrogenated rosin glycerol ester, polyisobutylene, liquid paraffin, and butylated hydroxytoluene (BHT) to the pressure-sensitive adhesive matrix was 50:50:30:30:1.

[0100] The specific preparation method of the plaster is as described in Example 1.

[0101] Comparative Example 2 This comparative example provides a traditional Chinese medicine composition for treating acute joint soft tissue injury. The difference between this composition and Example 1 is that Panax notoginseng is used instead of safflower in the formula to observe the effect of the combination of different blood-activating and stasis-removing herbs on the efficacy.

[0102] The formula is as follows: 100 parts gardenia, 200 parts hibiscus leaves, 100 parts phellodendron bark, 100 parts rhubarb, 50 parts notoginseng, 50 parts turmeric, 10 parts borneol, and 20 parts menthol. The preparation method is the same as described in Example 1, and extract B2 is prepared for later use.

[0103] The obtained extract B2, borneol, and menthol were added to the molten pressure-sensitive adhesive matrix according to the set drug concentration, and the plaster was prepared using conventional methods. Specifically, the mass ratio of styrene-isoprene-styrene (SIS), hydrogenated rosin glycerol ester, polyisobutylene, liquid paraffin, and butylated hydroxytoluene (BHT) to the pressure-sensitive adhesive matrix was 50:50:30:30:1.

[0104] The specific preparation method of the plaster is as described in Example 1.

[0105] Comparative Example 3 This comparative example provides a traditional Chinese medicine composition for treating acute joint soft tissue injury. The difference between this composition and Example 1 is that Scutellaria baicalensis is used instead of Carthamus tinctorius in the formulation to observe the effect of heat-clearing and dampness-drying drugs replacing blood-activating and stasis-removing drugs on the efficacy.

[0106] The formula is as follows: 100 parts gardenia, 200 parts hibiscus leaves, 100 parts phellodendron bark, 100 parts rhubarb, 100 parts scutellaria root, 50 parts turmeric, 10 parts borneol, and 20 parts menthol.

[0107] The preparation method is the same as described in Example 1, and extract B3 is prepared for later use.

[0108] The obtained extract B3, borneol, and menthol were added to the molten pressure-sensitive adhesive matrix according to the set drug concentration, and the plaster was prepared using conventional methods. Specifically, the mass ratio of styrene-isoprene-styrene (SIS), hydrogenated rosin glycerol ester, polyisobutylene, liquid paraffin, and butylated hydroxytoluene (BHT) to the pressure-sensitive adhesive matrix was 50:50:30:30:1.

[0109] The specific preparation method of the plaster is as described in Example 1.

[0110] Comparative Example 4 This comparative example provides a traditional Chinese medicine composition for treating acute joint soft tissue injury. The difference between this composition and Example 1 is that Scutellaria baicalensis is used instead of Carthamus tinctorius in the formula, and the dosage of Scutellaria baicalensis is increased to change the principal and assistant herbs' compatibility relationship, so as to observe the effect of the adjustment of the compatibility relationship caused by increasing the dosage of heat-clearing herbs on the efficacy.

[0111] The formula is as follows: 100 parts gardenia, 200 parts hibiscus leaves, 100 parts phellodendron bark, 100 parts rhubarb, 150 parts scutellaria, 50 parts turmeric, 10 parts borneol, and 20 parts menthol.

[0112] The preparation method is the same as described in Example 1, and extract B4 is prepared for later use.

[0113] The obtained extract B4, borneol, and menthol were added to the molten pressure-sensitive adhesive matrix according to the set drug concentration, and the plaster was prepared using conventional methods. Specifically, the mass ratio of styrene-isoprene-styrene (SIS), hydrogenated rosin glycerol ester, polyisobutylene, liquid paraffin, and butylated hydroxytoluene (BHT) to the pressure-sensitive adhesive matrix was 50:50:30:30:1.

[0114] The specific preparation method of the plaster is as described in Example 1.

[0115] Comparative Example 5 Based on the aforementioned Comparative Example 4, this comparative example provides a traditional Chinese medicine composition for treating acute joint soft tissue injury. The difference between this composition and Example 1 is that Scutellaria baicalensis is used instead of Carthamus tinctorius in the formula, and the dosage of Scutellaria baicalensis is further increased.

[0116] The formula is as follows: Gardenia 100 parts, Hibiscus mutabilis leaves 200 parts, Phellodendron bark 100 parts, Rhubarb 100 parts, Scutellaria baicalensis 200 parts, Curcuma longa 50 parts, Borneol 10 parts, Menthol 20 parts.

[0117] The preparation method is the same as described in Example 1, and extract B5 is prepared for later use.

[0118] The obtained extract B5, borneol, and menthol were added to the molten pressure-sensitive adhesive matrix according to the set drug concentration, and the plaster was prepared using conventional methods. Specifically, the mass ratio of styrene-isoprene-styrene (SIS), hydrogenated rosin glycerol ester, polyisobutylene, liquid paraffin, and butylated hydroxytoluene (BHT) to the pressure-sensitive adhesive matrix was 50:50:30:30:1.

[0119] The specific preparation method of the plaster is as described in Example 1.

[0120] Comparative Example 6 This comparative example provides a traditional Chinese medicine composition for treating acute joint soft tissue injury. The difference between this composition and Example 1 is that the amount of safflower in the formula is reduced in order to observe the effect of reducing the proportion of blood-activating and stasis-removing herbs on the efficacy.

[0121] The formula is as follows: 100 parts gardenia, 200 parts hibiscus leaves, 100 parts phellodendron bark, 100 parts rhubarb, 25 parts safflower, 50 parts turmeric, 10 parts borneol, and 20 parts menthol; wherein, the ratio of hibiscus leaves to safflower is 200:25.

[0122] The preparation method is the same as described in Example 1, and extract B6 is prepared for later use.

[0123] The obtained extract B6, borneol, and menthol were added to the molten pressure-sensitive adhesive matrix according to the set drug concentration, and the plaster was prepared using conventional methods. Specifically, the mass ratio of styrene-isoprene-styrene (SIS), hydrogenated rosin glycerol ester, polyisobutylene, liquid paraffin, and butylated hydroxytoluene (BHT) to the pressure-sensitive adhesive matrix was 50:50:30:30:1.

[0124] The specific preparation method of the plaster is as described in Example 1.

[0125] Comparative Example 7 This comparative example provides a traditional Chinese medicine composition for treating acute joint soft tissue injury. The difference between this composition and Example 1 is that the amount of safflower is increased in the formula to observe the effect of increasing the proportion of blood-activating and stasis-removing herbs on the efficacy.

[0126] The formula is as follows: 100 parts gardenia, 200 parts hibiscus leaves, 100 parts phellodendron bark, 100 parts rhubarb, 75 parts safflower, 50 parts turmeric, 10 parts borneol, and 20 parts menthol; wherein, the ratio of hibiscus leaves to safflower is 200:75.

[0127] The preparation method is the same as described in Example 1, and extract B7 is prepared for later use.

[0128] The obtained extract B7, borneol, and menthol were added to the molten pressure-sensitive adhesive matrix according to the set drug concentration, and the plaster was prepared using conventional methods. Specifically, the mass ratio of styrene-isoprene-styrene (SIS), hydrogenated rosin glycerol ester, polyisobutylene, liquid paraffin, and butylated hydroxytoluene (BHT) to the pressure-sensitive adhesive matrix was 50:50:30:30:1.

[0129] The specific preparation method of the plaster is as described in Example 1.

[0130] Comparative Example 8 This comparative example provides a traditional Chinese medicine composition for treating acute joint soft tissue injury. The difference between this composition and Example 1 is that the ratio of the principal herbs, Hibiscus mutabilis leaves and safflower, was adjusted to observe the effect of increasing the proportion of blood-activating and stasis-removing herbs on the therapeutic effect.

[0131] The formula is as follows: 100 parts gardenia, 150 parts hibiscus leaves, 100 parts phellodendron bark, 100 parts rhubarb, 50 parts safflower, 50 parts turmeric, 10 parts borneol, and 20 parts menthol; wherein the ratio of hibiscus leaves to safflower is 150:50. Hibiscus leaves account for 27.27% of the formula (based on 6 Chinese medicinal herbs).

[0132] The preparation method is the same as described in Example 1, and extract B8 is prepared for later use; The obtained extract B8, borneol, and menthol were added to the molten pressure-sensitive adhesive matrix according to the set drug concentration, and the plaster was prepared using conventional methods. Specifically, the mass ratio of styrene-isoprene-styrene (SIS), hydrogenated rosin glycerol ester, polyisobutylene, liquid paraffin, and butylated hydroxytoluene (BHT) to the pressure-sensitive adhesive matrix was 50:50:30:30:1.

[0133] The specific preparation method of the plaster is as described in Example 1.

[0134] Comparative Example 9 This comparative example provides a traditional Chinese medicine composition for treating acute joint soft tissue injury. The difference between this composition and Example 1 is that the ratio of the principal herbs, Hibiscus mutabilis leaves and safflower, was adjusted to observe the effect of increasing the proportion of blood-activating and stasis-removing herbs on the therapeutic effect.

[0135] The formula is as follows: 100 parts gardenia, 250 parts hibiscus leaves, 100 parts phellodendron bark, 100 parts rhubarb, 50 parts safflower, 50 parts turmeric, 10 parts borneol, and 20 parts menthol; wherein the ratio of hibiscus leaves to safflower is 250:50. Hibiscus leaves account for 38.46% of the formula (based on 6 Chinese medicinal herbs).

[0136] The preparation method is the same as described in Example 1, and extract B9 is prepared for later use; The obtained extract B9, borneol, and menthol were added to the molten pressure-sensitive adhesive matrix according to the set drug concentration, and the plaster was prepared using conventional methods. Specifically, the mass ratio of styrene-isoprene-styrene (SIS), hydrogenated rosin glycerol ester, polyisobutylene, liquid paraffin, and butylated hydroxytoluene (BHT) to the pressure-sensitive adhesive matrix was 50:50:30:30:1.

[0137] The specific preparation method of the plaster is as described in Example 1.

[0138] Comparative Example 10 This comparative example provides a traditional Chinese medicine composition for treating acute joint soft tissue injury. The difference between this example and Example 1 is that the composition of the adjuvant was adjusted (to 100 parts of safflower, without the use of turmeric) to observe the effect of increasing the proportion of blood-activating and stasis-removing herbs on the efficacy.

[0139] The formula is as follows: 100 parts gardenia, 200 parts hibiscus leaves, 100 parts phellodendron bark, 100 parts rhubarb, 100 parts safflower, 10 parts borneol, and 20 parts menthol. The preparation method is the same as described in Example 1, and extract B10 is prepared for later use; The obtained extract B10, borneol, and menthol were added to the molten pressure-sensitive adhesive matrix according to the set drug concentration, and the plaster was prepared using conventional methods. Specifically, the mass ratio of styrene-isoprene-styrene (SIS), hydrogenated rosin glycerol ester, polyisobutylene, liquid paraffin, and butylated hydroxytoluene (BHT) to the pressure-sensitive adhesive matrix was 50:50:30:30:1.

[0140] The specific preparation method of the plaster is as described in Example 1.

[0141] Comparative Example 11 This comparative example provides a traditional Chinese medicine composition for treating acute joint soft tissue injury. The difference between this example and Example 1 is that the composition of the adjuvant was adjusted (100 parts of turmeric, without the use of safflower) to observe the effect of increasing the proportion of blood-activating and stasis-removing herbs on the efficacy.

[0142] The formula is as follows: 100 parts gardenia, 200 parts hibiscus leaves, 100 parts phellodendron bark, 100 parts rhubarb, 100 parts turmeric, 10 parts borneol, and 20 parts menthol. The preparation method is the same as described in Example 1, and extract B11 is prepared for later use; The obtained extract B11, borneol, and menthol were added to the molten pressure-sensitive adhesive matrix according to the set drug concentration, and the plaster was prepared by conventional methods. Specifically, the mass ratio of styrene-isoprene-styrene (SIS), hydrogenated rosin glycerol ester, polyisobutylene, liquid paraffin, and butylated hydroxytoluene (BHT) to the pressure-sensitive adhesive matrix was 50:50:30:30:1.

[0143] The specific preparation method of the plaster is as described in Example 1.

[0144] Experimental Example 2: Comparison of the efficacy of different formulations Based on Experiment 1, this experiment further observes the effects of different formulation changes on the efficacy of the drug in a mouse ankle sprain model.

[0145] (1) Experimental methods A mouse ankle sprain model was established using the same method as in Example 1. Mice with successfully established models were randomly divided into groups of 10 each: model control group, positive drug group (Yunnan Baiyao plaster, commercially available product, National Drug Approval Number Z20073015), Example 1 group, Example 2 group, control groups 1-11 (plasters prepared from comparative examples 1-11), and blank matrix group. Ten normal mice were also used as the blank control group.

[0146] Referring to the drug administration and fixation method in Example 1, the test patches (or positive control patches) for each group were cut into 1cm pieces. 2Small pieces were applied topically to the affected area. The positive control ointment was a commercially available product. Except for the positive control group, the dosage for all other drug-containing groups was set at 8g of raw medicinal material / kg / day (i.e., the clinical dose determined in Example 1). The ointment was administered once daily for 10 consecutive days. Soft tissue injury scores were assessed according to the standards in Table 1 before administration (D0), on the fourth day of administration (D4), and the day after the last administration. Hind limb support strength was measured using a rat and mouse bipedal balance analgesia tester, and the difference in bipedal support strength was calculated.

[0147] In addition, based on the scores and bipedal support strength differences on the day following the last dose, the improvement rates of the scores relative to the model group and the improvement rates of the support strength differences relative to the model group were calculated to quantitatively assess the efficacy. The calculation method is as follows: The improvement rate (%) compared to the model control group is calculated as follows: [(Difference in score or support between the model control group and the treatment group - Difference in score or support between the treatment group) / Difference in score or support between the model control group and the treatment group] × 100%.

[0148] A higher improvement rate compared to the model control group indicates a better therapeutic and recovery effect of the drug on the injury model.

[0149] (2) Experimental results (2.1) Ankle sprain injury score Table 4: Scoring results of soft tissue injury severity in mice ( (n=10)

[0150] Note: Compared with the blank control group, ++P<0.01; compared with the model control group, *P<0.05; compared with the Example 1 group, #P<0.05.

[0151] Table 4 shows that the ankle sprain injury scores of the model control group at each time point were significantly higher than those of the blank control group (P < 0.01), indicating successful model establishment. On the 4th day of drug administration, the injury scores of the positive drug group, Example 1 group, Example 2 group, control group 7, and control group 10 were significantly lower than those of the model control group (P < 0.05), indicating that appropriate or large amounts of safflower have an advantage in relieving the apparent symptoms of ankle injury in the short term. Among them, Example 1 group showed the best improvement effect, indicating that the composition of the present invention has the advantage of rapid onset of action. Because Example 1 group contains a penetration-enhancing drug, its score improvement trend is better than that of Example 2 group.

[0152] Comparison of data from each group revealed that, given the presence of the penetration enhancers borneol and menthol, the drug ratio played a decisive role in efficacy. On the day after the last administration, the injury score improvement rate of the Example 1 group relative to the model group reached 75.00%, significantly better than all other groups except the positive control group, Example 2 group, and control group 7. The injury scores of control group 1 (complete removal of safflower), control groups 3 and 4 (replacing safflower with Scutellaria baicalensis), and control group 6 (reduced safflower dosage) were all significantly higher than those of the Example 1 group (P < 0.05). This indicates that removing safflower, reducing the dosage, or replacing it with Scutellaria baicalensis significantly weakens the overall efficacy. Although control group 2 (replacing safflower with Panax notoginseng) and control group 5 (replacing safflower with a high dose of Scutellaria baicalensis) showed significant improvement compared to the model group at the treatment endpoint, their relative improvement rates were both less than 50%, significantly lower than those of the Example 1 group (P < 0.05), suggesting that Panax notoginseng or a high dose of Scutellaria baicalensis cannot completely replace the core role of safflower. The control group with increased safflower dosage showed no significant difference in scores compared to the group in Example 1, indicating that safflower had reached a relatively optimal therapeutic threshold under the original formulation.

[0153] In addition, control groups 8 and 9 reduced or increased the dosage of the principal herb, Hibiscus mutabilis leaf, to examine the effect of the ratio of principal to adjuvant herbs on efficacy. The relative improvement rates of control groups 8 and 9 compared to the model group were 28.57% and 50.00%, respectively, both significantly lower than those of the Example 1 group (P < 0.05). This indicates that the ratio of principal to adjuvant herbs used in Example 1 is optimal; excessive deviation from this ratio significantly weakens the efficacy in reducing swelling and relieving pain. Therefore, to ensure efficacy, the ratio of Hibiscus mutabilis leaf to safflower needs to be maintained at 180–220:45–55, preferably 190–210:48–52, and further preferably 200:50; and the proportion of the principal herb, Hibiscus mutabilis leaf, in the entire formula (based on 6 medicinal herbs) needs to be maintained at 29%–38%, for example, 33.33%.

[0154] Control groups 10 and 11 were used to examine the synergistic effect of adjuvants by doubling the dosage of a single herb. The results showed that simply doubling the dosage of safflower to remove turmeric (control group 10, improvement rate 42.86% relative to the model group), or simply doubling the dosage of turmeric to remove safflower (control group 11, improvement rate 17.86% relative to the model group), resulted in significantly lower improvement rates relative to the model group compared to the Example 1 group (P < 0.05). With the total dosage of adjuvants consistent across the three experimental groups, the effect of the Example 1 group, using safflower and turmeric in combination, was far superior to that of the experimental groups using either herb alone. This further indicates that the effects of safflower and turmeric in this formula are not simply additive, but rather synergistic, and their combined use is one of the key factors for achieving the best therapeutic effect. This is the first time that safflower and turmeric have been used together in this formulation and shown a synergistic effect (in the treatment of acute joint soft tissue injuries). Such synergistic phenomena have not been observed in existing technical reports.

[0155] (2.2) Bipedal support force test Table 5: Effect of plaster on the difference in foot support force in a mouse ankle sprain model ( (n=10)

[0156] Note: Compared with the blank control group, ++P<0.01; compared with the model control group, *P<0.05; compared with the Example 1 group, #P<0.05.

[0157] Table 5 shows that the difference in bipedal support force at each time point in the model control group was significantly greater than that in the blank control group (P < 0.01). On the day after the last administration, the difference in bipedal support force in the positive drug group, Example 1 group, Example 2 group, control group 2, control group 5, control group 7, and control group 9 was significantly lower than that in the model control group (P < 0.05), but the improvement in Example 1 group was the best, indicating that the composition of the present invention can effectively improve the deep weight-bearing function of the affected limb and reduce pain under stress.

[0158] Regarding the recovery of supporting function, the improvement rate of the Example 1 group relative to the model group was 47.27%, showing the best therapeutic effect. The differences in bipedal supporting force in Control Groups 1, 3, 4, and 6 were all significantly greater than those in Example 1 (P < 0.05), and their improvement rates relative to the model group were all lower (all below 15%). This indicates that the lack of safflower, the use of conventional doses of Scutellaria baicalensis as a substitute, or insufficient safflower dosage had extremely limited effect on improving deep soft tissue and joint function. The differences in bipedal supporting force in Control Groups 2 and 5 were significantly greater than those in Example 1 (P < 0.05), and their improvement rates relative to the model group were 32.73% and 29.09%, respectively, both significantly lower than those in Example 1. Although Control Group 7 showed no significant statistical difference from Example 1, its improvement rate relative to the model group was lower than that of Example 1, indicating limited overall intervention effect. It is noteworthy that Control Group 7, with increased safflower dosage, had a bipedal supporting force difference that was basically the same as that in Example 1, indicating that a higher dosage of safflower is not necessarily better, and excessive increases do not simultaneously improve the repair capacity of soft tissue and joint function.

[0159] Furthermore, comparative examples 8 and 9, which adjusted the dosage of the principal herb *Hibiscus mutabilis* leaf, showed improvement rates of 12.73% and 30.91% relative to the model group, respectively, both significantly lower than that of example 1 (P < 0.05). This suggests that changes in the ratio of the principal herb to the adjuvant herb, and the overall proportion of the principal herb, not only affect the reduction of apparent swelling but also the recovery of the mechanical function of deep tissues. To ensure efficacy, the ratio of *Hibiscus mutabilis* leaf to safflower needs to be maintained at 180–220:45–55, with the proportion of *Hibiscus mutabilis* leaf in the formula maintained at 29%–38%. The improvement rates of comparative examples 10 and 11 relative to the model group were 27.27% and 21.82%, respectively, also significantly inferior to that of example 1 (P < 0.05). The results indicate that simply adding a single blood-activating herb cannot replace the restorative effect of the combined use of safflower and turmeric on supporting function; the specific compatibility ratio of safflower and turmeric is one of the key factors for this formula to achieve deep tissue repair and functional recovery. In this formula, safflower and turmeric showed a synergistic effect in treating acute joint soft tissue injuries (specifically, the recovery of biomechanical function in cases of acute joint soft tissue injuries).

[0160] Finally, it should be specifically noted that the formulation of Example 2 lacks borneol and menthol, aiming to observe the effect of aromatic penetration enhancers on the overall efficacy and transdermal absorption of the formula. The experimental results show that the injury score and the difference in bipedal support strength in the Example 2 group on the day after the last administration were still significantly improved compared to the model control group (P < 0.05), with improvement rates of 57.14% and 40.00% respectively relative to the model group. This indicates that the core efficacy of the composition of the present invention is still determined by the specific combination of six medicinal materials: gardenia, hibiscus leaf, phellodendron bark, rhubarb, safflower, and turmeric. Even in the absence of aromatic penetration enhancers, this basic formulation (see Example 2 group) still possesses a definite therapeutic effect on acute joint soft tissue injury, and compared to the positive control group, the Example 2 group exhibits comparable efficacy for the indications of the present invention. Compared to the Example 2 group, the addition of borneol and menthol in the Example 1 group mainly serves to accelerate the onset of action, enhance the overall efficacy, and improve deep mechanical function. Therefore, in practical applications, the addition of borneol and menthol can be flexibly chosen, or their dosage can be adjusted appropriately, based on factors such as specific dosage form requirements, patient skin tolerance, or production costs, to meet different clinical and industrial needs.

[0161] In summary, safflower is the core ingredient in this composition for its blood-activating, stasis-removing, swelling-reducing, pain-relieving, and deep weight-bearing functions. The absence or reduction of safflower, or its substitution with Panax notoginseng or Scutellaria baicalensis, as well as the absence of penetration enhancers, will all lead to a decrease in the efficacy of the compound or a delayed onset of action. Furthermore, comparative experiments by adjusting the proportions of the principal and adjuvant herbs confirmed that the formulation of Example 1 of this invention achieved an optimal balance in improving soft tissue injury scores and restoring joint biomechanical function, with significant synergistic effects among the components.

[0162] The above descriptions are merely embodiments of the present invention, and common knowledge such as specific technical solutions and / or characteristics are not described in detail here. It should be noted that those skilled in the art can make various modifications and improvements without departing from the technical solutions of the present invention, and these should also be considered within the scope of protection of the present invention. These modifications and improvements will not affect the effectiveness of the implementation of the present invention or the practicality of the patent. The scope of protection claimed in this application should be determined by the content of its claims, and the specific embodiments described in the specification can be used to interpret the content of the claims.

Claims

1. A traditional Chinese medicine composition for treating acute joint soft tissue injury, characterized in that: By weight, the active ingredients are composed of 90-110 parts of gardenia, 180-220 parts of hibiscus leaf, 90-110 parts of phellodendron bark, 90-110 parts of rhubarb, 45-55 parts of safflower and 45-55 parts of turmeric. Alternatively, by weight, the active ingredients are composed of 90-110 parts of gardenia, 180-220 parts of hibiscus leaf, 90-110 parts of phellodendron bark, 90-110 parts of rhubarb, 45-55 parts of safflower, 45-55 parts of turmeric, and 5-25 parts of borneol. Alternatively, by weight, the active ingredients are composed of 90-110 parts of gardenia, 180-220 parts of hibiscus leaf, 90-110 parts of phellodendron bark, 90-110 parts of rhubarb, 45-55 parts of safflower, 45-55 parts of turmeric, and 15-40 parts of menthol. Alternatively, by weight, the active ingredients are composed of 90-110 parts gardenia, 180-220 parts hibiscus leaves, 90-110 parts phellodendron bark, 90-110 parts rhubarb, 45-55 parts safflower, 45-55 parts turmeric, 5-25 parts borneol, and 15-40 parts menthol.

2. The traditional Chinese medicine composition for treating acute joint soft tissue injury according to claim 1, characterized in that: By weight, the active ingredients are composed of 95-105 parts of gardenia, 190-210 parts of hibiscus leaf, 95-105 parts of phellodendron bark, 95-105 parts of rhubarb, 48-52 parts of safflower, and 48-52 parts of turmeric. Alternatively, by weight, the active ingredients are composed of 95-105 parts of gardenia, 190-210 parts of hibiscus leaf, 95-105 parts of phellodendron bark, 95-105 parts of rhubarb, 48-52 parts of safflower, 48-52 parts of turmeric, and 5-25 parts of borneol. Alternatively, by weight, the active ingredients are composed of 95-105 parts of gardenia, 190-210 parts of hibiscus leaf, 95-105 parts of phellodendron bark, 95-105 parts of rhubarb, 48-52 parts of safflower, 48-52 parts of turmeric, and 15-40 parts of menthol. Alternatively, by weight, the active ingredients are composed of 95-105 parts of gardenia, 190-210 parts of hibiscus leaf, 95-105 parts of phellodendron bark, 95-105 parts of rhubarb, 48-52 parts of safflower, 48-52 parts of turmeric, 5-25 parts of borneol, and 15-40 parts of menthol.

3. The traditional Chinese medicine composition for treating acute joint soft tissue injury according to claim 2, characterized in that: By weight, the active ingredients are composed of 100 parts gardenia, 200 parts hibiscus leaves, 100 parts phellodendron bark, 100 parts rhubarb, 50 parts safflower, and 50 parts turmeric. Alternatively, by weight, the active ingredients are composed of 100 parts gardenia, 200 parts hibiscus leaves, 100 parts phellodendron bark, 100 parts rhubarb, 50 parts safflower, 50 parts turmeric, and 10 parts borneol. Alternatively, by weight, the active ingredients are composed of 100 parts gardenia, 200 parts hibiscus leaves, 100 parts phellodendron bark, 100 parts rhubarb, 50 parts safflower, 50 parts turmeric, and 20 parts menthol. Alternatively, by weight, the active ingredients are composed of 100 parts gardenia, 200 parts hibiscus leaves, 100 parts phellodendron bark, 100 parts rhubarb, 50 parts safflower, 50 parts turmeric, 10 parts borneol, and 20 parts menthol.

4. A traditional Chinese medicine composition for treating acute joint soft tissue injury according to any one of claims 1-3, characterized in that: It is used to obtain active ingredients by the following method: taking gardenia, hibiscus leaves, rhubarb, phellodendron bark, safflower and turmeric, and extracting them by water extraction and / or alcohol extraction; The alcohol extraction method is ethanol reflux extraction, with an ethanol volume fraction of 60% to 95%, and the amount of ethanol used each time is 6 to 15 times the total weight of the medicinal materials. The number of extractions is 1 to 4 times, and the extraction time for each extraction is 0.5 to 3 hours. The extracts from each ethanol reflux extraction are combined to obtain an alcohol extraction mixture. The water extraction method involves adding water and decocting, with the amount of water added each time being 6 to 15 times the total weight of the medicinal materials, and the number of decoctions being 1 to 4 times, with each decoction lasting 0.5 to 3 hours; the decoctions extracted from each decoction are combined to obtain a decoction mixture. After concentration, an extract with a relative density of 1.10 to 1.30 at 50-60℃ is obtained from the alcohol extraction mixture or the decoction mixture.

5. A traditional Chinese medicine composition for treating acute joint soft tissue injury according to any one of claims 1-3, characterized in that: The product is a topical preparation; the topical preparation is any one of the following: plaster, gel, ointment, spray, lotion, liniment or paste.

6. The product according to claim 5, characterized in that: The product is a topical plaster, and the topical plaster uses a rubber-based matrix or a pressure-sensitive adhesive matrix.

7. The product according to claim 6, characterized in that: The rubber matrix comprises a rubber matrix and any one of a tackifying resin, a softener, and an antioxidant added to the rubber matrix.

8. The use of a traditional Chinese medicine composition for treating acute joint soft tissue injury according to any one of claims 1-3 in the preparation of a medicament for treating acute joint soft tissue injury.

9. The application according to claim 8, characterized in that: The drug is used to improve pain, swelling and / or local tenderness caused by acute soft tissue injury of the joint, and / or improve the range of motion of the injured joint, and / or improve the weight-bearing function and walking stability of the injured joint, and / or improve the smoothness of the cartilage surface, and / or inhibit the formation of pannus.

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