External emulsion for resisting inflammation and easing pain as well as preparation method and application of external emulsion

Abstract

The invention relates to the field of medicines, and particularly discloses an anti-inflammatory and analgesic external emulsion as well as a preparation method and application thereof. The external emulsion is prepared from nine traditional Chinese medicines including radix clematidis, phryma leptostachya, radix angelicae pubescentis, scandent schefflera stem and leaf, corydalis tuber, ligusticum wallichii, angelica sinensis, pseudo-ginseng and borneol according to a specific ratio, volatile oil is extracted through steam distillation, then ethanol reflux extraction is combined, and finally an emulsifier and a wetting agent are added. The preparation method realizes full-effect utilization of volatile oil and water-soluble and alcohol-soluble components in the medicinal materials. The external emulsion has dual effects of rapid analgesia and long-acting anti-inflammation, and pharmacodynamic experiments show that the anti-inflammation and analgesia effects of the external emulsion are obviously superior to those of a same-prescription spray without volatile oil. Meanwhile, the medicament is good in stability, free of skin irritation and suitable for treating various pains and inflammations such as rheumatic arthritis, soft tissue contusion and cold-dampness dysmenorrhea.

Description

Technical Field

[0001] This application relates to the field of biomedicine, and more specifically, to a topical emulsion for anti-inflammatory and analgesic purposes, its preparation method, and its application. Background Technology

[0002] Currently, there are many types of topical preparations used clinically to treat chronic inflammation and joint pain, such as ointments, plasters, gels, sprays, and emulsions, but all of them have significant drawbacks. Ointments (such as erythromycin ointment) are sticky and easily clog pores and stain clothing; plasters (such as musk analgesic plasters) have poor breathability and are prone to causing allergies; gels (such as ibuprofen gel) have limited drug loading capacity; and sprays (such as diclofenac sodium aerosol) and liniments have low drug utilization rates due to weak transdermal absorption or short duration of action.

[0003] In the field of emulsions, existing technologies are divided into pure traditional Chinese medicine emulsions and emulsions combining traditional Chinese and Western medicine. While the latter offers significant short-term effects, long-term use of Western medicine components can easily cause adverse skin reactions. Existing pure traditional Chinese medicine emulsions face a prominent technical contradiction: adding volatile oils and other active ingredients to enhance efficacy often increases the risk of skin irritation; conversely, omitting these ingredients to avoid irritation leads to incomplete extraction of medicinal components, hindering the full realization of efficacy. For example, compound aconite tincture emulsion has poor safety due to the presence of toxic medicinal materials, while other relatively safe emulsions have limited efficacy due to their limited medicinal composition or failure to fully utilize volatile oil components. Current technologies fail to provide a pure traditional Chinese medicine topical emulsion solution that can achieve full component extraction and ensure high efficacy by including volatile oils and other ingredients, while also guaranteeing good skin safety.

[0004] Therefore, there is an urgent need in this field for an innovative pure Chinese herbal external emulsion that can effectively coordinate the contradiction between "high efficacy" and "high safety" through reasonable prescription design and preparation process without introducing Western medicine and toxic medicinal flavors. This would provide clinical practice with an ideal external preparation that combines rapid analgesia, long-lasting anti-inflammatory effects, and is suitable for long-term use. Summary of the Invention

[0005] To address the aforementioned issues, this application provides a topical emulsion for anti-inflammatory and analgesic purposes, its preparation method, and its application.

[0006] The technical solution adopted in this application is as follows:

[0007] In a first aspect, this application provides a topical emulsion for anti-inflammatory and analgesic purposes, which is made from active pharmaceutical ingredients and pharmaceutical excipients;

[0008] The raw material is composed of the following medicinal materials in the following weight ratio: Clematis chinensis 60-90 parts, Clematis armandii 40-60 parts, Angelica pubescens 40-70 parts, Achyranthes bidentata 40-70 parts, Corydalis yanhusuo 29-50 parts, Ligusticum chuanxiong 30-60 parts, Angelica sinensis 30-55 parts, Panax notoginseng 20-40 parts, and Borneol 15-30 parts;

[0009] The pharmaceutical excipients are emulsifiers and wetting agents.

[0010] Furthermore, the emulsifier mentioned above is one of polyethylene glycol 4000, polyethylene glycol 6000 or Tween 80, and its amount is 1.2%-3.0% of the total mass of the final emulsion.

[0011] Furthermore, the aforementioned wetting agent is one of propylene glycol, glycerin, or poloxamer 188, and its amount is 7%-15% of the total mass of the final emulsion.

[0012] Furthermore, the above-mentioned external emulsion is prepared by first extracting volatile oils from Angelica sinensis, Angelica pubescens, Clematis chinensis and Ligusticum chuanxiong, then mixing them with Achyranthes bidentata, Clematis armandii, Corydalis yanhusuo and Panax notoginseng for alcohol extraction, and finally mixing the obtained volatile oils, water extracts, alcohol extracts and borneol, and adding the emulsifier and wetting agent.

[0013] Furthermore, the average particle size of the above-mentioned topical emulsion is between 200 nm and 400 nm, and the particle size and zeta potential do not change significantly within 30 days of being left at room temperature.

[0014] Secondly, this application provides a method for preparing a topical emulsion, comprising:

[0015] Angelica sinensis, Angelica pubescens, Clematis chinensis and Ligusticum chuanxiong were mixed and extracted by steam distillation with water. The distillate was collected and allowed to stand to separate to obtain volatile oil.

[0016] The seven-leaf lotus, the herb clematis, the corydalis, and the notoginseng are pulverized and added to the residue after the volatile oil is extracted. The residue is then extracted 2-3 times by reflux with a 50%-80% ethanol solution. The aqueous extract and the ethanol extract are combined, filtered, the ethanol is recovered, and the extract is concentrated to a relative density of 1.04-1.12 to obtain the medicinal solution.

[0017] The borneol was dissolved in ethanol and added to the drug solution. After mixing, an emulsifier and a wetting agent were added to obtain an aqueous phase.

[0018] Add the volatile oil to the aqueous phase, grind evenly, add water to the total volume, mix well, and the product is obtained.

[0019] Furthermore, in the process of preparing the above-mentioned volatile oil, the amount of water added is 6-8 times that of the medicinal material.

[0020] Furthermore, in the process of preparing the above-mentioned drug solution, the reflux extraction is performed twice. The first reflux extraction uses 7-9 times the amount of ethanol and is performed for 1.5-2.5 hours. The second reflux extraction uses 5-7 times the amount of ethanol and is performed for 1-2 hours.

[0021] Furthermore, the emulsifier mentioned above is polyethylene glycol 4000, and the wetting agent is propylene glycol.

[0022] Thirdly, this application provides the use of the above-mentioned topical emulsion in the preparation of anti-inflammatory and analgesic agents.

[0023] In summary, this application has the following beneficial effects:

[0024] The topical emulsion for anti-inflammatory and analgesic purposes and its preparation method provided in this application have the following significant advantages compared to the prior art:

[0025] 1. This preparation uses a pure Chinese herbal compound and does not contain any Western medicine ingredients or toxic herbs such as aconite. It avoids the side effects such as skin atrophy and pigmentation caused by long-term use of Western medicine, as well as the safety risks brought by toxic herbs. It is highly safe for long-term external use.

[0026] 2. The prescription contains nine medicinal herbs that are combined in accordance with traditional Chinese medicine theory. Clematis chinensis and Clematis armandii dispel wind and dampness, Angelica pubescens disperses cold and relieves pain, Panax notoginseng, Ligusticum chuanxiong, and Angelica sinensis invigorate blood and promote qi circulation, Corydalis yanhusuo and Coptis chinensis promote qi circulation and relieve pain, and Borneol guides the medicine directly to the affected area. Together, they exert the effects of dispelling wind and cold, invigorating blood and unblocking collaterals, promoting qi circulation and relieving pain. Targeting the pathogenesis of wind-cold-dampness arthralgia, qi stagnation and blood stasis, it achieves both symptomatic and root-cause treatment. It is suitable for a variety of diseases such as joint swelling and pain, soft tissue contusion, limb numbness, and even cold-dampness dysmenorrhea and stomach pain.

[0027] 3. This invention innovatively employs a combined extraction process: first, steam distillation to extract the volatile oil, followed by ethanol reflux extraction of the residue. This process overcomes the shortcomings of single ethanol extraction, which cannot effectively retain the active components of the volatile oil, or single water extraction, which results in the loss of effective components due to ethanol precipitation. It ensures that anti-inflammatory and analgesic components such as saponins, alkaloids, and volatile oils are extracted and retained to the maximum extent, realizing the "full component" utilization of the medicinal material and laying a material foundation for the full exertion of the medicinal effect.

[0028] 4. This application combines the advantages of high drug loading and good skin permeability by formulating the active ingredients into an emulsion. Borneol in the formula can act as a prescription ingredient to exert analgesic effects, and also as a transdermal absorption enhancer to promote drug absorption and improve drug utilization. Systematic pharmacodynamic experiments have confirmed that in collagen-induced arthritis models and formalin-induced pain models, the anti-inflammatory (significantly reducing inflammatory factors such as PGE2, IL-1, IL-6, and TNF-α) and analgesic effects of this emulsion are significantly superior to those of the same prescription spray, demonstrating the key role of emulsion formulation in enhancing efficacy. Simultaneously, the product quality is stable and controllable. The resulting emulsion has a particle size distribution between 200-400 nm, shows no stratification after 30 days at room temperature, and exhibits no significant changes in particle size or zeta potential, indicating good physical stability of the emulsion system, which is beneficial for storage and use. Attached Figure Description

[0029] Figure 1 This is a flowchart of the preparation method of the topical emulsion provided in this application. Detailed Implementation

[0030] The embodiments of the present invention will be described in detail below with reference to the examples. However, those skilled in the art will understand that the following examples are only for illustrating the present invention and should not be regarded as limiting the scope of the present invention. Specific conditions not specified in the examples shall be carried out according to conventional conditions or conditions recommended by the manufacturer. Reagents or instruments whose manufacturers are not specified are all conventional products that can be purchased commercially.

[0031] The following provides a detailed description of specific embodiments of the present invention. It should be understood that the specific embodiments described herein are for illustrative and explanatory purposes only and are not intended to limit the scope of the invention.

[0032] Example 1

[0033] This embodiment provides a topical emulsion for anti-inflammatory and analgesic purposes, the preparation method of which (as shown in the figure) includes:

[0034] (1) Preparation: 50g of seven-leaf lotus, 50g of angelica, 50g of angelica pubescens, 45g of corydalis, 90g of clematis, 50g of chuanxiong, 30g of notoginseng, 60g of clematis root, and 20g of borneol, a total of 9 herbs.

[0035] (2) Preparation of aqueous extract and volatile oil: Angelica sinensis, Angelica pubescens, Clematis chinensis and Ligusticum chuanxiong are crushed, mixed evenly, and 7 times the amount of water is added. The extract is extracted by steam distillation, the distillate is collected, and the volatile oil and aqueous extract are collected after standing for later use.

[0036] (3) Preparation of alcohol extract: Powdered lotus, clematis, corydalis and notoginseng were added to the residue from which the volatile oil was extracted. The residue was refluxed twice with 8 times and 6 times the amount of 70% ethanol, respectively. The first extraction lasted 2 hours and the second extraction lasted 1.5 hours. The water extract and alcohol extract were combined, filtered, and the solvent was recovered from the filtrate and concentrated to a relative density of 1.08.

[0037] (4) Add borneol: Dissolve borneol in a small amount of ethanol and add it to the medicine solution, then mix well.

[0038] (5) Preparation of aqueous phase: Add 2.0% polyethylene glycol 4000 and 10% propylene glycol, mix well, and use as aqueous phase.

[0039] (6) Prepare an emulsion: Add the volatile oil to the aqueous phase, grind evenly, add water to 1000ml, mix well, and the emulsion is ready.

[0040] Example 2

[0041] This embodiment provides a topical emulsion for anti-inflammatory and analgesic purposes. Its preparation method differs from that of Example 1 in the formulation ratio, specifically:

[0042] Ingredients: 40g of Heptaphyllum, 55g of Angelica sinensis, 60g of Angelica pubescens, 35g of Corydalis yanhusuo, 80g of Clematis chinensis, 40g of Ligusticum chuanxiong, 20g of Panax notoginseng, 50g of Clematis armandii, and 25g of Borneol, a total of 9 herbs.

[0043] Example 3

[0044] This embodiment provides a topical emulsion for anti-inflammatory and analgesic purposes. Its preparation method differs from that of Example 1 in the formulation ratio, specifically:

[0045] Ingredients: 70g of Heptaphyllum, 45g of Angelica sinensis, 40g of Angelica pubescens, 50g of Corydalis yanhusuo, 60g of Clematis chinensis, 30g of Ligusticum chuanxiong, 20g of Panax notoginseng, 55g of Clematis armandii, and 20g of Borneol, a total of 9 herbs.

[0046] Example 4

[0047] This embodiment provides a topical emulsion for anti-inflammatory and analgesic purposes. Its preparation method differs from that of Example 1 in the formulation ratio, specifically:

[0048] Ingredients: 60g of Heptaphyllum, 30g of Angelica sinensis, 70g of Angelica pubescens, 29g of Corydalis yanhusuo, 70g of Clematis chinensis, 60g of Ligusticum chuanxiong, 40g of Panax notoginseng, 40g of Clematis armandii, and 30g of Borneol, a total of 9 herbs.

[0049] Example 5

[0050] This embodiment provides a topical emulsion for anti-inflammatory and analgesic purposes. The difference in its preparation method compared to Example 1 lies in the preparation step of the alcohol extract. Specifically:

[0051] Preparation of alcohol extract: After crushing the seven-leaf lotus, the herb *Clematis chinensis*, the corydalis rhizome, and the notoginseng, add them to the residue from which the volatile oil has been extracted. Reflux extract three times with 9, 7, and 6 times the amount of 50% ethanol, respectively. The first extraction lasts 1.5 hours, the second 1 hour, and the third 1 hour. Filter the extract, recover the solvent from the filtrate, and concentrate it to a solution with a relative density of 1.04.

[0052] Example 6

[0053] This embodiment provides a topical emulsion for anti-inflammatory and analgesic purposes. The difference in its preparation method compared to Example 1 lies in the preparation step of the alcohol extract. Specifically:

[0054] Preparation of alcohol extract: After crushing the seven-leaf lotus, the herb clematis, the corydalis, and the notoginseng, add them to the residue from which the volatile oil has been extracted. Reflux extract twice with 7 times and 5 times the amount of 80% ethanol, the first time for 2.5 hours and the second time for 2 hours. Filter, recover the solvent from the filtrate and concentrate it to a solution with a relative density of 1.12.

[0055] Example 7

[0056] This embodiment provides a topical emulsion for anti-inflammatory and analgesic purposes. The preparation method of this emulsion differs from that of Example 1 in that the emulsifier and its dosage are different. Specifically, polyethylene glycol 6000 is used as the emulsifier, and its dosage is 3.0% of the total amount of the final emulsion.

[0057] Example 8

[0058] This embodiment provides a topical emulsion for anti-inflammatory and analgesic purposes. The preparation method of this emulsion differs from that of Example 1 in that the emulsifier and its dosage are different. Specifically, Tween 80 is used as the emulsifier, and its dosage is 1.2% of the total amount of the final emulsion.

[0059] Example 9

[0060] This embodiment provides a topical emulsion for anti-inflammatory and analgesic purposes. The preparation method of this emulsion differs from that of Example 1 in that the wetting agent and its dosage are different. Specifically, glycerin is used as the wetting agent, and its dosage is 7% of the total amount of the final emulsion.

[0061] Example 10

[0062] This embodiment provides a topical emulsion for anti-inflammatory and analgesic purposes. The preparation method of this emulsion differs from that of Example 1 in that the wetting agent and its dosage are different. Specifically, poloxamer 188 is used as the wetting agent, and its dosage is 15% of the total amount of the final emulsion.

[0063] Comparative Example 1

[0064] This comparative example provides a spray for anti-inflammatory and analgesic purposes, the preparation method of which includes:

[0065] (1) Material preparation: Same as in Example 1

[0066] (2) Preparation of alcohol extract: Crush Clematis chinensis, Clematis armandii, Angelica pubescens, Achyranthes bidentata, Corydalis yanhusuo, Ligusticum chuanxiong, Angelica sinensis and Panax notoginseng and mix them. Reflux extract twice with 8 times and 6 times the amount of 70% ethanol, the first time for 2 hours and the second time for 1.5 hours. Filter, recover the solvent from the filtrate and concentrate it to a drug solution with a relative density of 1.06.

[0067] (3) Add borneol: Dissolve borneol in a small amount of ethanol and add it to the medicine solution, then mix well.

[0068] (4) Preparation of aqueous phase: Add 2.0% polyethylene glycol 4000 and 10% propylene glycol, mix well, and use as aqueous phase.

[0069] (5) Prepare the spray: Add water to 1000ml, mix well, and the spray is obtained.

[0070] Comparative Example 2

[0071] This comparative example provides a topical gel, which differs from Example 1 in that the pharmaceutical excipients and corresponding formulation processes are different. This comparative example uses 1% carbomer 940 as the gel matrix material. After adding triethanolamine to adjust to neutral, a mixture of volatile oil and drug solution is added under continuous and slow stirring. After stirring evenly, purified water is added to the specified total amount, and stirring is continued slowly until completely uniform. After vacuum degassing, the gel is obtained.

[0072] Comparative Example 3

[0073] This comparative example provides a topical emulsion, which differs from Example 1 in that it has a different formulation (does not contain Clematis chinensis), but the overall dosage is the same. Specifically:

[0074] 60g of Heptaphyllum, 60g of Angelica sinensis, 60g of Angelica pubescens, 55g of Corydalis yanhusuo, 60g of Ligusticum chuanxiong, 40g of Panax notoginseng, 80g of Clematis chinensis, and 30g of Borneol.

[0075] Comparative Example 4

[0076] This comparative example provides a topical emulsion, which differs from Example 1 in its formulation (it does not contain Clematis chinensis), while maintaining the same overall dosage. Specifically:

[0077] Clematis chinensis 100g, Achyranthes bidentata 70g, Angelica sinensis 70g, Angelica pubescens 70g, Corydalis yanhusuo 65g, Ligusticum chuanxiong 70g, Panax notoginseng 50g, Borneol 40g.

[0078] Performance testing

[0079] I. Stability Assessment

[0080] The stability of the formulations provided in Example 1 and Comparative Example 2 of this application was investigated within 30 days of storage at room temperature, and the particle size and zeta potential were measured.

[0081] The results are shown in Table 1:

[0082]

[0083] As shown in Table 1, the emulsion provided in Example 1 of this application is a highly stable and uniform nano-dispersion system. The particle size and zeta potential showed no significant changes within 30 days, indicating good physical stability and a long shelf life. In contrast, the gel in Comparative Example 2 exhibited extremely poor physical stability, failing to guarantee the uniformity of quality and the accuracy of dosage during storage, and thus lacking feasibility as a qualified commercial product.

[0084] Drug safety experiment

[0085] 1. Single-dose toxicity test

[0086] (1) Preparation of blank sample: Take 700ml of water, add 10% propylene glycol and 1.5% polyethylene glycol 4000, mix well, add ethanol to 1000ml, mix well, and the blank sample is obtained.

[0087] (2) Animal grouping and administration: Rabbits were randomly divided into 3 groups of 10 each (5 males and 5 females) and their backs were dehaired (10% Na2S hair removal, hair removal area 4×4cm on the back). The treatment was as follows: (a) Blank group: 0.5ml of blank sample was applied to the hair removal area; (b) Experimental group 1: 0.5ml of spray provided in Comparative Example 1 was applied to the hair removal area; (c) Experimental group 2: 0.5ml of emulsion provided in Example 1 was applied to the hair removal area.

[0088] (3) Single-dose skin irritation test: Referring to the "Technical Guidelines for Drug Irritation, Allergy and Hemolysis Research", the same body left and right self-control method was adopted. The blank sample, spray and emulsion were evenly applied to the left side, and physiological saline was applied to the right side. They were kept alone and the drugs were removed with physiological saline after 4 hours.

[0089] (4) Evaluation of skin irritation reaction: Observe the animal's skin for local reactions such as erythema and edema at 4h, 6h, 8h and 12h after skin irritation administration, and score according to the severity in Table 2. The scoring criteria are: score <2 is no irritation, 2≤score<4 is mild irritation, 4≤score<8 is moderate irritation, and 8≤score<12 is severe irritation.

[0090]

[0091] (5) Evaluation results:

[0092] As shown in Table 3:

[0093] 2. Repeated-dose toxicity test

[0094] (1) Animal grouping and administration: Rabbits were randomly divided into 3 groups of 10 each (5 males and 5 females) and their backs were dehaired (10% Na2S hair removal, hair removal area 4×4cm on the back). The treatment was as follows: (a) Blank group: 0.5ml of blank sample was applied to the hair removal area; (b) Experimental group 1: 0.5ml of spray provided in Comparative Example 1 was applied to the hair removal area; (c) Experimental group 2: 0.5ml of emulsion provided in Example 1 was applied to the hair removal area.

[0095] (2) Repeated-dose skin irritation test: Referring to the "Technical Guidelines for Drug Irritation, Allergy and Hemolysis Research", the same-body left-right self-control method was used. The blank sample, spray, and emulsion were evenly applied to the left side, and physiological saline was applied to the right side. The animals were kept separately and the drugs were removed with physiological saline after 4 hours. The drugs were administered once every 24 hours for 10 consecutive days. The erythema and edema of the animal's skin were observed and recorded 4 hours after each administration, and scored according to the severity.

[0096] (3) Evaluation of skin irritation reaction: After administration of the drug to the skin, observe the animal's skin at a fixed time every day for local reactions such as erythema and edema, and score them according to the severity in Table 2. The scoring criteria are: score < 2 is no irritation, 2 ≤ score < 4 is mild irritation, 4 ≤ score < 8 is moderate irritation, and 8 ≤ score < 12 is severe irritation.

[0097] (4) Evaluation results:

[0098]

[0099] As shown in Tables 3 and 4, no obvious skin erythema or edema was observed after a single administration of either the spray or the emulsion; however, after repeated administration, obvious erythema and edema appeared successively on days 7-10 after the spray was administered, indicating that the spray is skin irritating.

[0100] III. Anti-inflammatory efficacy test (collagen-induced arthritis model)

[0101] (1) Grouping and modeling:

[0102] Fifty SD rats were randomly divided into five groups (blank group, experimental group 1, experimental group 2, experimental group 3, and experimental group 4), with ten rats in each group. 4 mg / ml of bovine type II collagen was dissolved in 0.1 mol / L acetic acid to prepare a 2 mg / ml solution, which was then mixed with Freund's complete adjuvant to prepare a 1 mg / ml solution. Each rat was injected with 0.25 ml of this solution at three points: tail, back, and right hind paw to induce inflammation. Twenty days later, the bovine type II collagen solution was mixed with Freund's complete adjuvant to prepare a 1 mg / ml solution, and injected again using the same method. Seven days later, the rats showed paw swelling and weight loss, indicating successful model establishment.

[0103] (2) Anti-inflammatory test

[0104] On the day of successful model establishment, (a) control group: no medication was applied, and the animals were fed normally; (b) experimental group 1: 0.2 ml of spray (provided in Comparative Example 1) was applied to the above 3 inflammatory sites once a day; (c) experimental group 2: 0.2 ml of emulsion (provided in Comparative Example 3) was applied to the above 3 inflammatory sites once a day; (d) experimental group 3: 0.2 ml of emulsion (provided in Comparative Example 4) was applied to the above 3 inflammatory sites once a day; (e) experimental group 4: 0.2 ml of emulsion (provided in Example 1) was applied to the above 3 inflammatory sites once a day. All five groups were tested until day 15 when medication was discontinued, and then observed for another 3 days.

[0105] The mice that had been given the drug were euthanized, and their paws were symmetrically cut off from the left and right ankle joints. They were weighed immediately, and the degree of swelling and the rate of swelling inhibition were calculated. The contents of inflammatory factors PGE2, IL-1β, IL-6, IL-10 and TNF-α in the inflammatory tissue fluid were also measured.

[0106] (3) Result evaluation

[0107] The results are shown in Tables 5 and 6:

[0108]

[0109]

[0110] The results showed that, compared with the control group, both the spray and the emulsion significantly inhibited paw edema in rats, and the levels of PGE2, IL-1, IL-6, IL-10, and TNF-α in the inflammatory tissue fluid decreased to varying degrees. However, the emulsion-applied experimental groups 2-4 showed a more significant inhibitory effect on inflammatory factors, indicating that adding volatile oils to the spray to create an emulsion can enhance the anti-inflammatory effect. Furthermore, experimental groups 4 and 2-3 demonstrated that Clematis chinensis and Clematis armandii are indispensable as principal herbs; the absence of either would lead to a significant decrease in efficacy, proving the scientific validity and necessity of the synergistic formulation of the nine herbs in this invention, rather than a simple accumulation of herbs.

[0111] IV. Analgesic Efficacy Test (Formalin Analgesia Model)

[0112] (1) Modeling and grouping: 25 mice were randomly divided into 5 groups (blank group, experimental group 1, experimental group 2, experimental group 3 and experimental group 4), with 5 mice in each group. 20 µl of 2.0% formalin solution was injected subcutaneously into the dorsal side of the right hand of each mouse. After 30 min, the mice exhibited behavior of licking and biting their right hind paw, indicating successful modeling.

[0113] (2) Analgesia experiment: After successful modeling, the following treatments were performed: (a) Blank group: No drug treatment was given, and the animals were fed normally; (b) Experimental group 1: 0.1 ml of spray (provided by Comparative Example 1) was applied to the above-mentioned drug injection site; (c) Experimental group 2: 0.1 ml of this emulsion (provided by Comparative Example 3) was applied to the above-mentioned drug injection site; (d) Experimental group 3: 0.1 ml of this emulsion (provided by Comparative Example 4) was applied to the above-mentioned drug injection site; (e) Experimental group 4: 0.1 ml of this emulsion (provided by Example 1) was applied to the above-mentioned drug injection site.

[0114] Thirty minutes after administration, the cumulative number of mouse activities within 2 hours was recorded in 30-minute increments to evaluate the analgesic effect.

[0115] (3) Result evaluation:

[0116] The results are shown in Table 7.

[0117]

[0118] As shown in Table 7, both the spray and the emulsion have certain analgesic effects. However, the cumulative number of activities in the emulsion treatment group was significantly lower than that in the spray group, indicating that adding volatile oil to the spray to form an emulsion can enhance the analgesic effect. Meanwhile, in experimental groups 2 and 3, the synergistic effect of the prescription was disrupted due to the absence of the principal drug. Although their total analgesic effect (total number of times) was similar to or close to that of experimental group 4, analysis of data at different time points revealed that they were weaker than experimental group 4 in terms of rapid onset (first record) and sustained analgesia (fourth record). This demonstrates the comprehensive advantage of the complete prescription in terms of both onset speed and duration of efficacy.

[0119] This specific embodiment is merely an explanation of this application and is not intended to limit it. After reading this specification, those skilled in the art can make modifications to this embodiment without contributing any inventive step, but such modifications are protected by patent law as long as they fall within the scope of the claims of this application.

Claims

1. A topical emulsion for anti-inflammatory and analgesic purposes, characterized in that, It is made from active pharmaceutical ingredients and pharmaceutical excipients; The raw material is composed of the following medicinal materials in the following weight ratio: Clematis chinensis 60-90 parts, Clematis armandii 40-60 parts, Angelica pubescens 40-70 parts, Achyranthes bidentata 40-70 parts, Corydalis yanhusuo 29-50 parts, Ligusticum chuanxiong 30-60 parts, Angelica sinensis 30-55 parts, Panax notoginseng 20-40 parts, and Borneol 15-30 parts; The pharmaceutical excipients are emulsifiers and wetting agents.

2. The topical emulsion for anti-inflammatory and analgesic purposes according to claim 1, characterized in that, The emulsifier is one of polyethylene glycol 4000, polyethylene glycol 6000 or Tween 80, and its amount is 1.2%-3.0% of the total mass of the final emulsion.

3. The topical emulsion for anti-inflammatory and analgesic purposes according to claim 1, characterized in that, The wetting agent is one of propylene glycol, glycerin, or poloxamer 188, and its amount is 7%-15% of the total mass of the final emulsion.

4. The topical emulsion for anti-inflammatory and analgesic purposes according to any one of claims 1-3, characterized in that, The topical emulsion is prepared by first extracting volatile oils from Angelica sinensis, Angelica pubescens, Clematis chinensis, and Ligusticum chuanxiong, then mixing them with Achyranthes bidentata, Clematis armandii, Corydalis yanhusuo, and Panax notoginseng for alcohol extraction, and finally mixing the obtained volatile oils and alcohol extracts with borneol, and adding the emulsifier and wetting agent.

5. The topical emulsion for anti-inflammatory and analgesic purposes according to any one of claims 1-3, characterized in that, The average particle size of the topical emulsion is between 200 nm and 400 nm, and the particle size and zeta potential do not change significantly within 30 days at room temperature.

6. A method for preparing a topical emulsion as described in any one of claims 1-5, characterized in that, It includes: Angelica sinensis, Angelica pubescens, Clematis chinensis and Ligusticum chuanxiong are pulverized and mixed, water is added and steam distilled to extract, the distillate is collected and allowed to stand to separate to obtain volatile oil; The seven-leaf lotus, the herb clematis, the corydalis, and the notoginseng are pulverized and added to the residue after the volatile oil is extracted. The residue is then extracted 2-3 times by reflux with a 50%-80% ethanol solution. The aqueous extract and the ethanol extract are combined, filtered, the ethanol is recovered, and the extract is concentrated to a relative density of 1.04-1.12 to obtain the medicinal solution. The borneol was dissolved in ethanol and added to the drug solution. After mixing, an emulsifier and a wetting agent were added to obtain an aqueous phase. Add the volatile oil to the aqueous phase, grind evenly, add water to the total volume, mix well, and the product is obtained.

7. The method for preparing the topical emulsion according to claim 6, characterized in that, In the preparation of the volatile oil, the amount of water added is 6-8 times that of the medicinal materials.

8. The method for preparing the topical emulsion according to claim 6, characterized in that, In the preparation of the drug solution, the reflux extraction is performed twice. The first reflux extraction uses 7-9 times the amount of ethanol and is performed for 1.5-2.5 hours. The second reflux extraction uses 5-7 times the amount of ethanol and is performed for 1-2 hours.

9. The method for preparing the topical emulsion according to claim 6, characterized in that, The emulsifier is polyethylene glycol 4000, and the wetting agent is propylene glycol.

10. The use of a topical emulsion as described in any one of claims 1-5 in the preparation of an anti-inflammatory and analgesic agent.

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