An external anti-inflammatory analgesic composition of arnica extract and its preparation process

Abstract

This invention relates to the field of topical anti-inflammatory and analgesic preparations, and discloses a topical anti-inflammatory and analgesic composition of arnica extract and its preparation process, comprising: arnica extract, used in an amount of 0.01-0.10 parts, for anti-inflammatory and analgesic purposes; and several parts of traditional Chinese medicine extract for promoting blood circulation and removing blood stasis; the arnica extract and the traditional Chinese medicine extract are combined, wherein the arnica extract relieves the aggravation of blood stasis caused by inflammation through anti-inflammatory and analgesic effects, and the traditional Chinese medicine extract improves the state of blood stasis. This topical anti-inflammatory and analgesic composition of arnica extract and its preparation process, by constructing a functional synergistic mechanism between arnica extract and traditional Chinese medicine extracts for promoting blood circulation and removing blood stasis, enables the arnica extract to achieve rapid onset of anti-inflammatory and analgesic effects, while the traditional Chinese medicine extract achieves sustained efficacy in promoting blood circulation and reducing swelling. The dosage design achieves a synergistic balance between the two, thereby solving the problem in existing technologies where it is difficult to achieve a synergistic balance between the blood-activating components of arnica and traditional Chinese medicine.

Description

Technical Field

[0001] This invention relates to the field of topical anti-inflammatory and analgesic preparations, specifically to a topical anti-inflammatory and analgesic composition of arnica extract and its preparation process. Background Technology

[0002] Topical anti-inflammatory and analgesic agents are medications that are applied directly to the skin surface by smearing, spraying, or patching to relieve local pain, inflammation, and swelling. They are not taken orally or injected and mainly act on the painful area. They can reduce discomfort caused by muscle and joint pain, sprains, arthritis, soft tissue injuries, etc. Common dosage forms include creams, gels, sprays, and patches.

[0003] Current technologies fail to effectively address the skin irritation and sensitization risks associated with the potent anti-inflammatory and analgesic effects of active ingredients in arnica (such as helenalin). Furthermore, they fail to achieve a functional synergistic balance between arnica and the blood-activating and stasis-removing components of traditional Chinese medicine in dosage design. This results in an inability to simultaneously address the speed of onset, safety, and duration of action. Consequently, either relying on a single chemical component (such as NSAIDs) offers rapid onset but is prone to skin irritation or systemic side effects, or employing traditional Chinese herbal formulas, while offering better safety, results in slow onset and less pronounced analgesic effects. Summary of the Invention

[0004] (a) Technical problems to be solved: To address the shortcomings of existing technologies, this invention provides a topical anti-inflammatory and analgesic composition of arnica extract and its preparation process, which solves the problems mentioned in the background art, such as the risk of skin irritation and sensitization of arnica active ingredients, the difficulty in achieving synergistic balance with traditional Chinese medicine components, and the inability to simultaneously consider the speed of onset, safety, and duration of action.

[0005] (II) Technical Solution: To achieve the above objectives, the present invention provides the following technical solution: a topical anti-inflammatory and analgesic composition of arnica extract and its preparation process; the topical anti-inflammatory and analgesic composition of arnica extract comprises: Arnica extract, at a dosage of 0.01–0.10 parts, is used for anti-inflammatory and analgesic purposes; Several extracts of traditional Chinese medicine are used to promote blood circulation and remove blood stasis; The arnica extract is combined with the traditional Chinese medicine extract. The arnica extract relieves the aggravation of bruising caused by inflammation through anti-inflammatory and analgesic effects, while the traditional Chinese medicine extract improves the bruising condition, optimizes the local microenvironment, and accelerates the pharmacological effects of the arnica extract.

[0006] Preferably, the arnica extract achieves its anti-inflammatory effect by inhibiting NF-κB signaling pathway activation and downregulating COX-2 and iNOS expression.

[0007] Preferably, the arnica extract achieves analgesia by inhibiting neuroinflammatory mediators and reducing peripheral pain sensitization.

[0008] Preferably, the composition is a topical preparation, and the dosage form includes ointment, gel, liniment, and spray.

[0009] Preferably, the herbal extract is a herbal extract that promotes blood circulation and removes blood stasis.

[0010] A process for preparing a topical anti-inflammatory and analgesic composition of arnica extract includes the following steps: Arnica raw material was extracted and purified to obtain an arnica extract with helenalin and its sesquiterpene lactone derivatives as the core active ingredients. A combination of Chinese herbal medicines that promote blood circulation and remove blood stasis is used to obtain herbal extracts through pulverization, extraction, and refining. Take 0.01 to 0.10 parts of the arnica extract and several parts of the herbal extract, add pharmaceutical excipients for external use, mix and shape to obtain a composition.

[0011] Preferably, the arnica raw material is extracted by any one of alcohol extraction, water extraction, or alcohol-water mixed extraction, with an extraction temperature of 40-80℃ and an extraction time of 1-3 hours.

[0012] Preferably, the pharmaceutical excipients of the topical preparation include one or more of the following: transdermal penetration enhancers, humectants, thickeners, preservatives, and pharmaceutical solvents.

[0013] (III) Beneficial Effects: The arnica extract topical anti-inflammatory and analgesic composition and preparation process provided by this invention have the following beneficial effects: 1. The above-mentioned topical anti-inflammatory and analgesic composition of arnica extract and its preparation process, by precisely limiting the dosage of arnica extract to a safe and effective window range of 0.01 to 0.10 parts, can fully exert its core pharmacological activity of anti-inflammatory and analgesic, while effectively avoiding the skin irritation and sensitization risks caused by the active ingredient helenalin of arnica, thereby solving the problem of safety hazards of active ingredients of arnica in the prior art.

[0014] 2. This topical anti-inflammatory and analgesic composition of arnica extract and its preparation process, by constructing a functional synergistic system of arnica extract and blood-activating and stasis-removing herbal extracts, allows arnica extract to achieve a rapid anti-inflammatory and analgesic "ignition" effect, while the herbal extracts achieve a sustained blood-activating and swelling-reducing "maintenance" effect. The dosage design ensures a synergistic balance between the two, thereby solving the problem in the prior art where it is difficult to achieve a synergistic balance between arnica and blood-activating components of herbal medicines.

[0015] 3. This topical anti-inflammatory and analgesic composition and preparation process of arnica extract combines the rapid onset of action of arnica extract with the sustained action of traditional Chinese medicine extracts. It is combined with a transdermal topical dosage form to increase the local drug concentration. At the same time, relying on the multi-dimensional pharmacological effects of targeted anti-inflammatory, peripheral analgesia and promotion of microcirculation, the composition takes into account the speed of onset, drug safety and duration of action, thereby solving the defects of existing topical anti-inflammatory and analgesic preparations that cannot meet the needs at the same time. Detailed Implementation

[0016] The technical solutions of the present invention will be clearly and completely described below with reference to the embodiments of the present invention. Obviously, the described embodiments are only some embodiments of the present invention, and not all embodiments. Based on the embodiments of the present invention, all other embodiments obtained by those of ordinary skill in the art without creative effort are within the scope of protection of the present invention.

[0017] Example 1 A preferred embodiment of the present invention, an arnica extract topical anti-inflammatory and analgesic composition, and its preparation process will be described in detail below: Arnica extract, used in doses of 0.01–0.10 parts, is used for anti-inflammatory and analgesic purposes. Doses less than 0.01 parts may result in insufficient efficacy; while dosages exceeding 0.10 parts may significantly increase the risk of irritation and sensitization.

[0018] Several extracts of traditional Chinese medicine are used to promote blood circulation and remove blood stasis; The combination of arnica extract and traditional Chinese medicine extracts allows the arnica extract to alleviate the inflammation-induced congestion through anti-inflammatory and analgesic effects, while the traditional Chinese medicine extracts improve the congestion state, optimize the local microenvironment, and accelerate the pharmacological effects of the arnica extract. Ultimately, the combination achieves both rapid onset and long-lasting effects, while also enhancing overall medication safety.

[0019] Arnica extract exerts its anti-inflammatory effect by inhibiting NF-κB signaling pathway activation and downregulating COX-2 and iNOS expression. This mechanism of action is a targeted anti-inflammatory pathway, inhibiting the signaling pathway at the source of inflammation. Compared with traditional anti-inflammatory components, it is more precise in its action, effectively reducing the release of inflammatory factors and the production of inflammatory mediators, thereby achieving an anti-inflammatory effect and quickly relieving local redness, swelling, and inflammatory response.

[0020] Arnica extract achieves analgesia by inhibiting neuroinflammatory mediators and reducing peripheral pain sensitization. Its analgesic mechanism acts directly on the peripheral pain transmission pathway, avoiding the systemic side effects of oral analgesics, while achieving rapid analgesia after topical application. This meets the clinical need for rapid relief of local pain and is the core pharmacological support for the rapid onset of action of the composition.

[0021] The composition is a topical preparation, available in ointments, gels, liniments, and sprays to suit different application scenarios and affected areas. Ointments and gels are suitable for local application and massage; liniments and sprays are suitable for large affected areas or areas difficult to apply directly. All are transdermal drug delivery methods, acting directly on the painful and inflamed site, reducing drug metabolism and loss in the body, and increasing local drug concentration.

[0022] The herbal extract is a blood-activating and stasis-removing herbal extract. Its pharmacological effects are consistent with the effect of arnica extract in improving local microcirculation. It can further promote the dissipation of local blood stasis and the restoration of microcirculation, solve the problem of poor local blood circulation accompanied by inflammation and pain, and form a synergistic therapeutic effect with arnica extract targeting the pathological basis of inflammation and pain.

[0023] Working process and principle: Arnica extract, as the principal ingredient, plays a core role in rapidly reducing inflammation and pain, and improving local microcirculation. Extracts of traditional Chinese medicines that promote blood circulation and remove blood stasis, as complementary components, play an auxiliary role in promoting blood circulation and reducing swelling. The two ingredients form a functional synergistic enhancement effect through their respective pharmacological mechanisms. After transdermal administration in a topical dosage form, it acts directly on the local inflamed and painful site, exerting its effects from multiple dimensions, such as inhibiting inflammatory signals, relieving pain sensitization, and promoting blood circulation. Ultimately, it achieves rapid, safe, and sustained anti-inflammatory and analgesic effects. Furthermore, the dosage and type of each component are designed with efficacy, safety, and synergy in mind to ensure the clinical application value of the composition.

[0024] Example 2 A process for preparing a topical anti-inflammatory and analgesic composition of arnica extract includes the following steps: Arnica raw material is extracted and purified to obtain an arnica extract with helenalin and its sesquiterpene lactone derivatives as the core active ingredients. This process enriches the key anti-inflammatory and analgesic active ingredients in arnica, removes ineffective impurities from the raw material, enhances the pharmacological activity of the extract, and reduces the potential skin irritation risk caused by impurities.

[0025] A combination of Chinese herbal medicines that promote blood circulation and remove blood stasis is taken, and the herbal extract is obtained through crushing, extraction, and refining. In this process, the active ingredients that promote blood circulation and remove blood stasis in the Chinese herbal medicines are enriched, and non-medicinal ingredients are removed to ensure the purity and pharmacological effect of the herbal extract, and also to enable it to form a precise synergistic effect with arnica extract.

[0026] Take 0.01 to 0.10 parts of arnica extract, take a certain amount of traditional Chinese medicine extract, add pharmaceutical excipients for external preparations, mix and shape to obtain a composition.

[0027] The extraction method for arnica raw material is any one of alcohol extraction, water extraction, or a mixture of alcohol and water extraction. The extraction temperature is 40-80℃, which ensures the dissolution efficiency of active ingredients while avoiding the inactivation of active ingredients such as helenalin and its sesquiterpene lactone derivatives due to high temperature. The extraction time is 1-3 hours, which is a reasonable range for the full dissolution of active ingredients.

[0028] Pharmaceutical excipients for topical formulations include one or more of the following: transdermal penetration enhancers, humectants, thickeners, preservatives, and pharmaceutical solvents. Transdermal penetration enhancers can improve the transdermal absorption efficiency of arnica extract and traditional Chinese medicine extracts, ensuring that the drug can penetrate the skin to reach the site of action. Humectants and thickeners can improve the user experience and shaping effect of topical dosage forms. Preservatives can extend the shelf life of the composition. Pharmaceutical solvents provide a dispersion medium for mixing the active ingredients and excipients.

[0029] Although embodiments of the invention have been shown and described, it will be understood by those skilled in the art that various changes, modifications, substitutions and alterations can be made to these embodiments without departing from the principles and spirit of the invention, the scope of which is defined by the appended claims and their equivalents.

Claims

1. A topical anti-inflammatory and analgesic composition of arnica extract, characterized in that, include: Arnica extract, at a dosage of 0.01–0.10 parts, is used for anti-inflammatory and analgesic purposes; Several extracts of traditional Chinese medicine are used to promote blood circulation and remove blood stasis; The arnica extract is combined with the traditional Chinese medicine extract. The arnica extract relieves the aggravation of bruising caused by inflammation through anti-inflammatory and analgesic effects, while the traditional Chinese medicine extract improves the bruising condition, optimizes the local microenvironment, and accelerates the pharmacological effects of the arnica extract.

2. The topical anti-inflammatory and analgesic composition of arnica extract according to claim 1, characterized in that: The arnica extract downregulates the expression of COX-2 and iNOS by inhibiting the activation of the NF-κB signaling pathway.

3. The topical anti-inflammatory and analgesic composition of arnica extract according to claim 1, characterized in that: The arnica extract achieves analgesia by inhibiting neuroinflammatory mediators and reducing peripheral pain sensitization.

4. The topical anti-inflammatory and analgesic composition of arnica extract according to claim 1, characterized in that: The composition is a topical preparation, and the dosage forms include ointments, gels, liniments, and sprays.

5. The topical anti-inflammatory and analgesic composition of arnica extract according to claim 1, characterized in that: The herbal extracts mentioned are herbal extracts that promote blood circulation and remove blood stasis.

6. A preparation process for a topical anti-inflammatory and analgesic composition of arnica extract, characterized in that: Includes the following steps: Arnica raw material was extracted and purified to obtain an arnica extract with helenalin and its sesquiterpene lactone derivatives as the core active ingredients. A combination of Chinese herbal medicines that promote blood circulation and remove blood stasis is used to obtain herbal extracts through pulverization, extraction, and refining. Take 0.01 to 0.10 parts of the arnica extract and several parts of the herbal extract, add pharmaceutical excipients for external use, mix and shape to obtain a composition.

7. The preparation process of the topical anti-inflammatory and analgesic composition of arnica extract according to claim 6, characterized in that: The arnica raw material is extracted by any one of alcohol extraction, water extraction, or a mixture of alcohol and water extraction, with an extraction temperature of 40-80℃ and an extraction time of 1-3 hours.

8. The preparation process of the topical anti-inflammatory and analgesic composition of arnica extract according to claim 6, characterized in that: The pharmaceutical excipients for the topical preparation include one or more of the following: transdermal penetration enhancers, moisturizers, thickeners, preservatives, and pharmaceutical solvents.