Traditional Chinese medicine capsule preparation for treating rheumatic waist and leg pain

Abstract

The invention discloses a traditional Chinese medicine capsule preparation for treating rheumatic waist and leg pain. The traditional Chinese medicine capsule preparation is prepared from 23 traditional Chinese medicines such as radix aconiti preparata and radix aconiti kusnezoffii preparata through a specific process. The extraction efficiency is optimized through the steps of ethanol disinfection, low-temperature drying, superfine grinding and the like, and the traditional compatibility theory of monarch, minister, assistant and guide is combined, so that the multi-target synergistic effects of resisting inflammation, easing pain, regulating immunity and the like are realized. Clinical tests show that the total effective rate of the preparation reaches 94.6%, which is significantly superior to that of a Fendel control group (Plt; 0.05) of the method. The invention also provides a preparation method, a quality control standard and new application extension, and is suitable for treating diseases such as rheumatic arthritis, lumbar disc herniation and the like.

Description

Technical Field

[0001] This invention relates to the field of traditional Chinese medicine, specifically to a traditional Chinese medicine capsule preparation for treating rheumatic back and leg pain. Background Technology

[0002] Rheumatic lumbago and leg pain is a common clinical disease, belonging to the category of Bi syndrome in Traditional Chinese Medicine (TCM). Its pathogenesis is complex and closely related to external wind-cold-dampness pathogens and insufficient vital energy in the body. Modern medicine believes that it is associated with inflammatory responses, immune abnormalities, and microcirculatory disorders. Currently, the main treatment methods for this condition include non-steroidal anti-inflammatory drugs (NSAIDs), hormone drugs, and physical therapy. Although NSAIDs can quickly relieve pain, long-term use can easily lead to adverse reactions such as gastrointestinal irritation and liver and kidney damage, and cannot fundamentally improve the patient's constitution. In recent years, TCM compound preparations have received widespread attention due to their multi-target regulatory effects, but there are still many problems in practical applications. Existing TCM compound preparations mostly use traditional water decoction processes, resulting in low extraction rates of effective components and high impurity content, making it difficult to guarantee product quality stability. Although some preparations use modern extraction technology, insufficient research on formulation compatibility and pharmacological mechanisms of action leads to inconsistent clinical efficacy. In addition, commercially available TCM capsules generally have problems such as excessive particle size (most products have a particle size ≥80 mesh) and low dissolution rate of effective components, usually below 75%, which directly affects drug absorption and utilization. Through years of clinical practice, the inventors have found that relying solely on drugs for dispelling wind and dampness or promoting blood circulation and removing blood stasis is insufficient to achieve ideal therapeutic effects. Extensive experimental research has confirmed that only by scientifically combining drugs to both eliminate pathogens and strengthen the body's resistance can the goal of treating both the symptoms and the root cause be achieved.

[0003] Existing traditional Chinese medicine preparations for treating rheumatic back and leg pain generally suffer from the following defects: First, the formulation lacks systematicity. Most preparations only focus on dispelling wind and dampness or promoting blood circulation and removing blood stasis, failing to take into account the overall conditioning effects such as tonifying the liver and kidneys and regulating immunity, resulting in unsustainable efficacy. Second, the preparation process is outdated. Most use traditional pulverization methods, resulting in a particle size of 80-100 mesh, low dissolution rate of effective ingredients, and poor bioavailability, affecting the therapeutic effect. Third, the quality control standards are incomplete. Most products only test a few indicators and lack quantitative control of key components such as diester-type alkaloids and flavonoids, leading to large batch-to-batch quality differences and prominent safety hazards. In addition, existing preparations mostly use ordinary capsule shells as carriers, which have poor moisture-proof performance and are prone to absorbing moisture and clumping during storage, affecting drug stability. Clinical studies show that the content of effective ingredients in traditional Chinese medicine capsules prepared using conventional processes can decrease by 15%-20% after being stored in an environment with 60% humidity for 3 months. Summary of the Invention

[0004] The purpose of this invention is to provide a traditional Chinese medicine capsule preparation for treating rheumatic back and leg pain. This invention proposes a traditional Chinese medicine capsule preparation for treating rheumatic lumbago and leg pain. The active ingredients of this capsule preparation are made from the following raw materials in parts by weight: 4-8 parts of processed Aconitum carmichaelii, 4-8 parts of processed Aconitum kusnezoffii, 8-12 parts of Clematis chinensis, 10-14 parts of Gentiana macrophylla, 10-14 parts of Chaenomeles speciosa, 12-18 parts of Piper kadsura, 0.3-0.7 pieces of Bungarus fasciatus, 12-17 parts of stir-fried Paeonia lactiflora, 10-30 parts of Astragalus membranaceus, 8-12 parts of Saposhnikovia divaricata, 10-20 parts of Spatholobus suberectus, 10-20 parts of Angelica sinensis, 8-12 parts of Panax notoginseng powder, 8-12 parts of Dipsacus asper, 10-20 parts of Achyranthes bidentata, 8-12 parts of Drynaria fortunei, 4-8 parts of Carthamus tinctorius, 4-8 parts of Asarum heterotropoides, 6-12 parts of Cinnamomum cassia, 4-8 parts of Buthus martensii, 8-12 parts of Bombyx mori, 6-12 parts of Anemarrhena asphodeloides, and 4-8 parts of Phellodendron chinense. This preparation is made by spraying the above-mentioned medicinal materials with 75% medical alcohol for disinfection, then allowing them to soak for 48 hours, drying them until the moisture content is ≤5%, pulverizing them through a 120-mesh sieve, mixing them evenly, and filling them into No. 0 capsules, each capsule containing 0.5g of raw medicinal powder. This invention achieves multiple effects such as dispelling wind and cold, promoting blood circulation, and tonifying the liver and kidneys through scientific formulation. Specifically, processed Aconitum carmichaelii and processed Aconitum kusnezoffii synergistically enhance the warming and analgesic effects; Clematis chinensis and Piper kadsura co-exist to dilate blood vessels and improve local microcirculation; and Paeonia lactiflora and Astragalus membranaceus form a combined attack and tonification approach. The specially added white-flowered snake, scorpion, and silkworm pupae form a unique combination, whose active protease can penetrate biological membranes to reach the deep layers of the lesion and exert anti-inflammatory and analgesic effects. The preparation process uses gradient temperature drying technology to effectively retain heat-sensitive components such as astragaloside A, and ultra-micro pulverization technology to achieve a drug particle size of over 120 mesh, significantly improving the dissolution rate of active ingredients. The quality control system covers limit testing of diester-type alkaloids and quantitative detection of astragaloside A and total saponins of Panax notoginseng, ensuring batch-to-batch consistency. Clinical data show that the overall effective rate of this preparation reaches 94.6%, significantly better than the ibuprofen control group, and the relapse rate 6 months after discontinuation of the drug is only 12.3%.

[0005] Furthermore, the white-flowered snake used is either the golden-ringed white-flowered snake or the Qi snake, with each snake weighing ≥3g. This specification ensures the stability of the effective ingredient content of the snake-derived medicinal material. As authentic medicinal materials, the golden-ringed white-flowered snake and the Qi snake have stronger active protease activity in their venom. Modern pharmacological studies have confirmed that the anti-inflammatory and analgesic effects of these two snake species are more than 30% higher than those of other varieties. At the same time, the specification of ≥3g ensures the minimum threshold of effective ingredients in a single dose of the medicinal material, allowing the insect-derived medicine to play a special role in "guiding and penetrating the meridians" in the compound prescription, and has a special curative effect on intractable rheumatic pain.

[0006] Furthermore, the fineness of the Panax notoginseng powder is limited to 100-120 mesh. This particle size range has been verified through dissolution tests, allowing the total saponins of Panax notoginseng to achieve a dissolution rate of 89.4% within 45 minutes. Ultrafine pulverization technology breaks down plant cell walls, directly exposing the active ingredients. Compared to traditional pulverization processes, bioavailability is increased by more than four times. Particularly in improving microcirculation, nano-sized Panax notoginseng powder particles can rapidly penetrate capillary walls, promoting local blood circulation. Laboratory data shows that it can increase blood flow velocity in damaged joints by more than 25%.

[0007] Furthermore, the drying temperature is set at 50–60℃ for 2–3 hours. This gradient heating process softens the medicinal material at a constant temperature of 45℃ in the initial stage, and then gradually increases the temperature to 55℃ to complete the drying, effectively preserving heat-sensitive components such as astragaloside A. Testing showed that the retention rate of astragaloside A was 38% higher than that of traditional drying processes, while ensuring that the content of diester-type alkaloids in processed Aconitum carmichaelii is controlled below 0.01%, far below the toxicity limit of 0.15% stipulated in the pharmacopoeia. This temperature-controlled drying technology ensures both drug safety and maximizes the activity of the active ingredients.

[0008] Furthermore, the amount of alcohol sprayed in step a) is set at 10%–15% of the total weight of the medicinal materials. This proportion has been verified through orthogonal experiments, effectively killing microorganisms on the surface of the medicinal materials while avoiding solvent residue from affecting efficacy. The osmotic pressure of 75% medical alcohol is similar to that of the cell sap of the medicinal materials, which can promote the pre-leaching of effective components within the cells while disinfecting. Testing showed that the total alkaloid dissolution rate of processed Aconitum carmichaelii treated with this process was 23% higher than that of untreated materials, laying the foundation for subsequent extraction. In the quality control system, the content of diester-type alkaloids in processed Aconitum carmichaelii is strictly limited to ≤0.01%. This indicator is based on the requirements of the 2020 edition of the Chinese Pharmacopoeia and is detected by HPLC to ensure that the content of aconitine-type toxic components is below the safety threshold. The setting of astragaloside A content ≥0.08 mg / g is quantitatively analyzed using an ELSD detector to ensure the minimum content of qi-tonifying components. The specially introduced IL-6 and TNF-α inhibition rate detection (≥40%), using ELISA to assess anti-inflammatory effects, complements traditional analgesia tests and comprehensively evaluates the drug's mechanism of action.

[0009] Furthermore, the carrier is a combination of starch, dextrin, and magnesium stearate. Starch acts as a filler to increase capsule volume, dextrin improves particle flowability, and magnesium stearate acts as a lubricant to reduce the coefficient of friction. The three components are mixed in a 1:0.5:0.3 ratio and optimized through hydrodynamic testing, resulting in a 35% increase in capsule filling efficiency and controlling the content variation within ±2%. This composition is designed for targeted drug release in the intestine. In vitro dissolution tests show that its cumulative release rate in pH 6.8 buffer reaches 98.2%, 12 percentage points higher than ordinary capsules.

[0010] Furthermore, the anti-inflammatory effect is achieved by inhibiting the expression of IL-6 and TNF-α. Animal experiments showed that this formulation reduced IL-6 levels by 42% and TNF-α levels by 38% in mice with inflammation. The analgesic effect was evaluated using the acetic acid writhing test; the number of writhing movements in the treated group was reduced by 45% compared to the control group (P<0.01). Regarding improvement in microcirculation, laser Doppler flowmetry showed that local blood flow velocity increased by 28% and vascular permeability improved by 32% after administration. These data confirm that this invention achieves comprehensive therapeutic effects of anti-inflammation, analgesia, and improvement of pathological damage through the synergistic action of multiple components.

[0011] The beneficial effects of this invention are:

[0012] This invention addresses the aforementioned technical challenges through systematic innovation and improvement. Firstly, the formulation design adheres to the holistic concept of Traditional Chinese Medicine, carefully selecting 23 medicinal herbs and constructing a multi-faceted treatment system through rigorous principles of principal, assistant, adjuvant, and guide herbs. Prepared aconite root and prepared aconite tuber serve as the principal herbs, synergistically enhancing the warming and dispersing effects; clematis root and sea pine stem serve as assistant herbs, exerting the effects of dispelling wind and unblocking the meridians; the combination of white peony root and astragalus root not only soothes the liver and relieves pain but also tonifies qi and strengthens the exterior, forming a combined tonifying and purging treatment pattern. Particularly noteworthy is the unique combination of white-flowered snake (0.3-0.7 pieces) with insect-derived herbs such as scorpion and silkworm pupae. Modern pharmacological studies have shown that these drugs contain various active proteases, capable of penetrating biological membranes to reach deep layers of the lesion, exerting anti-inflammatory and analgesic effects. This multi-dimensional and multi-layered formulation design breaks through the limitations of traditional Chinese medicine compound formulas with their single-effect properties, achieving the therapeutic goal of treating both the symptoms and the root cause.

[0013] In terms of preparation process, this invention employs a unique three-step synergistic technology to significantly improve drug quality. First, 75% medical alcohol is sprayed for disinfection, combined with a 48-hour soaking process, effectively killing microorganisms on the surface of the medicinal materials while avoiding the loss of active ingredients caused by traditional high-temperature sterilization. Testing shows that the content of diester-type alkaloids in processed Aconitum carmichaelii using this process can be controlled below 0.01%, far below the 0.15% upper limit stipulated in the pharmacopoeia. Second, an innovative gradient temperature drying technology is adopted, setting a segmented temperature control mode of 50-60℃ to maximize the retention of heat-sensitive components while ensuring the moisture content meets the standard (≤5%). For example, the retention rate of astragaloside A is increased by 38% compared to traditional drying processes. Finally, ultra-micro pulverization technology is introduced to control the drug particle size to above 120 mesh. Laser particle size analyzer testing shows a D90 value ≤15μm, increasing the dissolution rate of active ingredients by more than 4 times. Dissolution tests show that the dissolution rate of total saponins of Panax notoginseng reaches 89.4% within 45 minutes, significantly superior to ordinary capsules. The establishment of a quality control system is another important innovation of this invention. Addressing the problem of limited indicators in existing products, this invention establishes a quality control standard comprising eight core indicators. These include both qualitative identification items, such as thin-layer chromatography for identifying Astragalus membranaceus and Angelica sinensis, and quantitative detection indicators, such as high-performance liquid chromatography for determining the content of astragaloside A (≥0.08 mg / g) and the content of total saponins of Panax notoginseng (≥5.0%).

[0014] A modern bioactivity detection method was specifically introduced to evaluate the anti-inflammatory effect by measuring the inhibition rate (≥40%) of IL-6 and TNF-α in the sample. This multi-dimensional quality control system ensures the stability and reproducibility of the product's efficacy. Accelerated stability testing verified that after 6 months of storage at 40℃ / 75%RH, all indicators still met the prescribed standards. The breakthrough in clinical efficacy is the core value of this invention. Validated through a multicenter randomized controlled trial (RCT), the total effective rate in the treatment group (150 patients) reached 94.6%, significantly higher than the 80.0% in the control group (P<0.05). It showed particularly excellent results in improving patients' quality of life: the average morning stiffness time was reduced from 68 minutes to 25 minutes after treatment, and the joint mobility score increased from 42 to 78 (out of 100). Laboratory indicators showed that the C-reactive protein recovery rate was as high as 89.3%, 21.8 percentage points higher than the control group. More importantly, this invention demonstrates excellent safety—no serious adverse reactions occurred during the trial, and the incidence of gastrointestinal discomfort was only 3.3%, significantly lower than the 18.8% in the control group. These data fully demonstrate that this invention achieves a good balance between efficacy and safety. The innovative formulation is also noteworthy.

[0015] This invention uses No. 0 capsules as the drug delivery carrier. The capsule filling process was optimized through hydrodynamic testing, ensuring that the filling amount of each capsule is precisely controlled within an error range of 0.5g ± 2%. The capsule shell uses a novel enteric-coating material that remains intact for 2 hours in pH 1.2 hydrochloric acid and completely disintegrates and releases the drug within 30 minutes in pH 6.8 phosphate buffer. This design protects the drug components from gastric acid degradation while ensuring targeted release of the drug in the intestine, increasing local therapeutic concentration. In vitro release tests showed that the cumulative release rate of this product in simulated intestinal fluid reached 98.2%, 12 percentage points higher than ordinary capsules.

[0016] Precise control of production process parameters is key to achieving stable quality in this invention. Through orthogonal experiments on 12 key process parameters, the optimal process combination was determined. Specifically, the alcohol spraying amount was set to 12%-15% of the total weight of the medicinal materials, effectively disinfecting while avoiding solvent residue; the soaking time was precisely controlled at 48±1 hours to ensure thorough softening of the medicinal materials; the drying process employed a programmed temperature increase mode, initially maintaining a constant temperature of 45℃ for 2 hours, gradually increasing to 55℃ and maintaining it for 3 hours. This gradient temperature increase effectively reduces component volatilization loss; tests showed that the volatile oil retention rate reached 82.7%, an improvement of 27 percentage points compared to the one-step temperature increase method. The direct benefits of this technological innovation are reflected in several aspects. Cost calculations show that using the process of this invention to produce 10,000 capsules can save 12.5% ​​on medicinal material loss, reduce energy consumption by 18%, and increase production efficiency by 35%.

[0017] More importantly, this invention provides a new technological paradigm for the modernization of traditional Chinese medicine (TCM)—by deeply integrating traditional empirical formulas with modern pharmaceutical technology, it maintains the characteristics of TCM while enhancing the technological content of products, laying a solid foundation for the internationalization of TCM. Through systematic innovation, this invention solves three major long-standing problems in the treatment of rheumatic bone diseases (unstable efficacy, slow onset of action, and high relapse rate). Clinical trial data shows that the relapse rate six months after discontinuation of medication was only 12.3%, significantly lower than the 35.6% in the control group. This long-lasting effect is attributed to the sustained action of kidney-tonifying and bone-strengthening drugs such as *Drynaria fortunei* and *Dipsacus asper* in the formula, as well as the sustained clearance of pathological products by insect-derived drugs. Even more importantly, this invention provides new ideas and methods for the treatment of chronic and complex diseases with TCM, possessing significant academic value and promising clinical application prospects. Detailed Implementation

[0018] 1. Prescription composition and pharmacology

[0019] 1.1 Prescription Composition

[0020] Prepared Aconitum carmichaelii 4-8g, Prepared Aconitum kusnezoffii 4-8g, Clematis chinensis 8-12g, Gentiana macrophylla 10-14g, Chaenomeles speciosa 10-14g, Piper kadsura 12-18g, Bungarus fasciatus 0.3-0.7 pieces, Fried Paeonia lactiflora 12-17g, Astragalus membranaceus 10-30g, Saposhnikovia divaricata 8-12g, Spatholobus suberectus 10-20g, Angelica sinensis 10-20g, Panax notoginseng powder 8-12g, Dipsacus asper 8-12g, Achyranthes bidentata 10-20g, Drynaria fortunei 8-12g, Carthamus tinctorius 4-8g, Asarum heterotropoides 4-8g, Cinnamomum cassia 6-12g, Buthus martensii 4-8g, Bombyx mori 8-12g, Anemarrhena asphodeloides 6-12g, Phellodendron chinense 4-8g

[0021] 1.2 Pharmacology of Traditional Chinese Medicine

[0022] Prepared Aconitum carmichaelii: dispels wind and dampness, warms the meridians and relieves pain.

[0023] Processed aconite: dispels wind and dampness, warms the meridians, and relieves pain.

[0024] Clematis chinensis: dispels wind and dampness, unblocks meridians and relieves pain.

[0025] Gentiana macrophylla: dispels wind and dampness, unblocks meridians and relieves pain, reduces deficiency heat, and clears damp heat.

[0026] Papaya: It can relax muscles and tendons, harmonize the stomach, and dispel dampness.

[0027] Sea breeze vine: dispels wind and dampness, unblocks meridians and relieves pain.

[0028] White-flowered snake: dispels wind, unblocks meridians, stops spasms, and attacks toxins.

[0029] Stir-fried white peony root: nourishes blood and astringes yin, softens the liver and relieves pain, and calms liver yang.

[0030] Astragalus: Tonifies Qi and strengthens the spleen, raises Yang and lifts prolapse, benefits Wei Qi and consolidates the exterior, promotes diuresis and reduces swelling, and promotes tissue regeneration and detoxification.

[0031] Fangfeng: dispels wind and releases the exterior, eliminates dampness and relieves pain, and stops spasms.

[0032] Chicken blood vine: promotes blood circulation, replenishes blood, relaxes muscles and tendons.

[0033] Angelica sinensis: Nourishes blood and regulates menstruation, promotes blood circulation and relieves pain, moistens the intestines and promotes bowel movement.

[0034] Panax notoginseng powder: removes blood stasis, stops bleeding, promotes blood circulation, and relieves pain.

[0035] Dipsacus: Nourishes the liver and kidneys, strengthens tendons and bones, stops bleeding and calms the fetus, heals wounds and heals fractures.

[0036] Achyranthes bidentata: invigorates blood circulation and regulates menstruation, tonifies the liver and kidneys, strengthens tendons and bones, promotes urination and relieves strangury, and guides fire (blood) downward.

[0037] Drynaria fortunei: promotes blood circulation, heals injuries, tonifies the kidneys, and strengthens bones.

[0038] Safflower: Promotes blood circulation, regulates menstruation, removes blood stasis, and relieves pain.

[0039] Asarum: It relieves exterior syndromes and dispels cold, dispels wind and relieves pain, clears the orifices, warms the lungs and resolves phlegm.

[0040] Cinnamon twig: It induces sweating and relieves muscle tension, warms and unblocks the meridians, and helps yang to transform qi.

[0041] Scorpion: It can relieve wind and spasms, attack toxins and dissipate nodules, and unblock meridians and relieve pain.

[0042] Silkworm: It can calm wind and stop spasms, dispel wind and relieve pain, and resolve phlegm and dissipate nodules.

[0043] Anemarrhena asphodeloides: Clears heat and drains fire, nourishes yin and moistens dryness.

[0044] Phellodendron bark: Clears heat and dries dampness, drains fire and detoxifies, and eliminates bone steaming.

[0045] Solution:

[0046] The formula contains prepared aconite root, prepared aconite tuber, clematis root, gentian root, papaya, sea pine vine, and white-flowered snake, which have the effects of dispelling wind and unblocking the meridians, dispersing cold and dampness, and relieving pain. These are the main ingredients of the formula. They are supplemented with white peony root, astragalus root, saposhnikovia root, chicken blood vine, angelica root, notoginseng root, dipsacus root, achyranthes root, drynaria rhizome, and safflower to tonify the liver and kidneys, invigorate blood, dispel wind, and relieve pain. They are combined with asarum root, cinnamon twig, scorpion, and silkworm to dispel wind and cold, warm the meridians and promote yang, and relieve pain. Anemarrhena rhizome and phellodendron bark are used to clear heat, dry dampness, and reduce deficiency heat, thus counteracting the drying nature of the damp-heat herbs. The entire formula has the effects of tonifying the liver and kidneys, dispelling wind and cold, unblocking the meridians, invigorating blood, and relieving pain.

[0047] 1.3 Pharmacology of Western Medicine

[0048] Processed Aconitum carmichaelii: has significant anti-inflammatory and analgesic effects.

[0049] Processed Aconitum carmichaelii: has significant anti-inflammatory and analgesic effects.

[0050] Clematis chinensis: It has antibacterial, anti-inflammatory, analgesic, and antispasmodic effects.

[0051] Gentiana macrophylla: It has sedative, analgesic, antipyretic, and anti-inflammatory effects, and has a certain inhibitory effect on viruses, bacteria, and fungi.

[0052] Papaya: anti-inflammatory, antibacterial, antioxidant, immune-regulating, and promotes wound healing.

[0053] Sea pine: Anti-inflammatory, antibacterial, protects joints and cartilage.

[0054] White-flowered snake: It has anti-inflammatory, analgesic, and anticoagulant effects.

[0055] Fried white peony root has anti-inflammatory, analgesic, antispasmodic, liver-protective, and immune-regulating effects.

[0056] Astragalus: It has the effects of regulating immunity and promoting metabolism.

[0057] Fangfeng: It has antipyretic, anti-inflammatory, analgesic, antibacterial, antiviral, and immunomodulatory effects.

[0058] Chicken blood vine: It has antibacterial, anti-inflammatory, and anti-thrombotic effects.

[0059] Angelica sinensis has the effects of improving blood circulation, promoting hematopoiesis, anti-inflammatory and analgesic properties, and regulating immunity.

[0060] Panax notoginseng powder has the effects of stopping bleeding, promoting blood circulation and removing blood stasis, promoting hematopoiesis, and anti-inflammatory and analgesic properties.

[0061] Dipsacus: It has the effects of promoting fracture healing, resisting osteoporosis, anti-inflammatory, analgesic and immune regulation.

[0062] Achyranthes bidentata: It has the effects of improving microcirculation, anti-inflammatory and analgesic properties, and regulating immunity.

[0063] Drynaria fortunei: It has the effects of promoting fracture healing, resisting osteoporosis, anti-inflammatory and analgesic, and improving cartilage health.

[0064] Safflower: It has the effects of promoting blood circulation, relieving pain, and protecting nerves.

[0065] Asarum: It has antipyretic, analgesic, anti-inflammatory, and antimicrobial effects.

[0066] Cinnamon twigs have anti-inflammatory, anti-allergic, antipyretic, analgesic, antibacterial, and antiviral effects.

[0067] Whole scorpion: It has analgesic, anticoagulant and antithrombotic, and immunomodulatory effects.

[0068] Silkworm: It has anticoagulant, antithrombotic, anticonvulsant, antibacterial, and nerve-nourishing effects.

[0069] Anemarrhena asphodeloides has antipyretic, anti-inflammatory, and antimicrobial effects.

[0070] Phellodendron bark has antibacterial, anti-inflammatory, antiviral, and immune-regulating effects.

[0071] Modern pharmacological studies of Western medicine suggest that this formula has anti-inflammatory, analgesic, antispasmodic, antiviral, antibacterial, antioxidant, hepatoprotective, antithrombotic, nerve-nourishing, osteoporosis-preventing, and immune-regulating effects.

[0072] How to use

[0073] I. Drug Composition and Specifications

[0074] The active ingredients of this preparation are composed of the following 23 Chinese medicinal herbs in the following weight proportions:

[0075] Prepared Aconitum carmichaelii 4-8 parts, Prepared Aconitum kusnezoffii 4-8 parts, Clematis chinensis 8-12 parts, Gentiana macrophylla 10-14 parts, Chaenomeles speciosa 10-14 parts, Piper kadsura 12-18 parts, Bungarus fasciatus 0.3-0.7 pieces, stir-fried Paeonia lactiflora 12-17 parts, Astragalus membranaceus 10-30 parts, Saposhnikovia divaricata 8-12 parts, Spatholobus suberectus 10-20 parts, Angelica sinensis 10-20 parts, Panax notoginseng powder 8-12 parts (claim 3), Dipsacus asper 8-12 parts, Achyranthes bidentata 10-20 parts, Drynaria fortunei 8-12 parts, Carthamus tinctorius 4-8 parts, Asarum heterotropoides 4-8 parts, Cinnamomum cassia 6-12 parts, Buthus martensii 4-8 parts, Bombyx mori 8-12 parts, Anemarrhena asphodeloides 6-12 parts, Phellodendron chinense 4-8 parts.

[0076] Dosage form and specifications: No. 0 capsules are used, each capsule is filled with 0.5g of raw medicinal powder (±2% error), and each bottle or box contains 24 capsules.

[0077] II. Usage and Dosage

[0078] 1. Oral dosage: Adults take 4 capsules each time, 3 times a day, with warm water after meals.

[0079] 2. Treatment Course Recommendation: The general course of treatment is 2 weeks, which can be adjusted according to the patient's condition and doctor's advice. Clinical data shows that continuous use for 3 months can significantly reduce the recurrence rate.

[0080] 3. Special populations: Contraindicated in pregnant women; use with caution in patients with hepatic or renal insufficiency.

[0081] III. Key Points of Preparation Process

[0082] 1. Processing of medicinal materials:

[0083] All medicinal materials were disinfected by spraying with 75% medical alcohol (10%–15% spray amount), and then dried after being left to moisten for 48 hours until the moisture content was ≤5%.

[0084] White-flowered snake (golden-money white-flowered snake or Qi snake, size ≥3g) needs to be crushed separately to ensure the activity of active protease.

[0085] 2. Crushing and mixing:

[0086] The medicinal materials are pulverized to a fineness of 120 mesh or higher (D90 value ≤ 15μm), and the fineness of Panax notoginseng powder is controlled at 100-120 mesh.

[0087] The mixed powder needs to be tested for particle size to ensure that the dissolution rate meets the standard.

[0088] 3. Quality Control:

[0089] The finished product needs to be tested for three core indicators: (1) the diester-type alkaloids in processed Aconitum carmichaelii ≤0.01% (claim 7); (2) the content of astragaloside A ≥0.08mg / g; (3) the content of total saponins of Panax notoginseng ≥5.0%.

[0090] IV. Clinical Application Guidelines

[0091] 1. Indications:

[0092] It is suitable for lower back and leg pain caused by rheumatoid arthritis, lumbar disc herniation, etc.

[0093] It has a significant effect on improving morning stiffness, limited joint mobility, and local microcirculation disorders.

[0094] 2. Onset time:

[0095] Pain relief can be seen after 3-5 days of continuous use, and morning stiffness time is shortened by ≥50% after 1 week.

[0096] 3. Combination therapy:

[0097] It can be used in combination with anti-inflammatory and analgesic drugs, but should be taken 1 hour apart to avoid drug interactions.

[0098] V. Precautions

[0099] 1. Storage conditions:

[0100] Store in a sealed, light-proof container in a dry place at room temperature (10-30℃), avoiding high temperature and high humidity environments.

[0101] It is recommended to use within 6 months after opening to prevent oxidation of the active ingredients.

[0102] 2. Adverse reactions:

[0103] Mild gastrointestinal discomfort may occasionally occur (incidence ≤3.3%), which can be relieved spontaneously after discontinuation of the medication.

[0104] If allergic reactions such as rash or palpitations occur, discontinue use immediately and seek medical attention.

[0105] 3. Contraindications:

[0106] This product is contraindicated in patients with known hypersensitivity to any of its ingredients.

[0107] This product is contraindicated in patients undergoing anticoagulation therapy or with a bleeding tendency (due to its blood-activating components such as scorpion and Panax notoginseng).

[0108] VI. Packaging and Transportation

[0109] Packed in aluminum-plastic blister packs, 12 tablets per blister pack, 2 blister packs per box.

[0110] During transportation, it is necessary to protect it from shock and moisture, and avoid squeezing and damage.

[0111] VII. Summary of Pharmacological Effects

[0112] This product achieves the following therapeutic effects through multi-target synergistic action:

[0113] 1. Anti-inflammatory effect: Inhibits the expression of IL-6 and TNF-α (inhibition rate ≥40%);

[0114] 2. Analgesic effect: Reduced the number of writhing movements in acetic acid-induced pain mice by ≥40% (P<0.01);

[0115] 3. Improves microcirculation: Increases local blood flow velocity by ≥25%, promoting joint repair.

[0116] Example

[0117] This clinical trial included 150 patients with low back and leg pain. The patients ranged in age from 28 to 72 years old, with an average age of 50 years. The longest duration of illness was 1 year, and the shortest was 20 days. Data showed that all 150 patients had normal erythrocyte sedimentation rate (ESR) and rheumatoid factor levels, and had previously taken other antirheumatic drugs.

[0118] Treatment

[0119] The treatment group received Rheumatism and Lumbago Capsules. The prescription consisted of: processed Aconitum carmichaelii, processed Aconitum kusnezoffii, Clematis chinensis, Gentiana macrophylla, Chaenomeles speciosa, Piper kadsura, Bungarus fasciatus, stir-fried Paeonia lactiflora, Astragalus membranaceus, Saposhnikovia divaricata, Spatholobus suberectus, Angelica sinensis, Panax notoginseng powder, stir-fried Dipsacus asper, Achyranthes bidentata, Drynaria fortunei, Carthamus tinctorius, Asarum heterotropoides, Cinnamomum cassia, Buthus martensii, Bombyx mori, Anemarrhena asphodeloides, and Phellodendron chinense (based on the dosage provided). The herbs were disinfected by spraying with 75% medical alcohol, left to stand for 48 hours, dried, powdered, and passed through a 120-mesh sieve. The prepared herbs were then mixed and made into No. 0 capsules. The dosage was 4 capsules orally, 3 times daily, taken with warm water after meals. The control group consisted of 80 patients who received Fenbid capsules produced by Tianjin Sino-American SmithKline Pharmaceutical Co., Ltd., orally, 1 capsule orally, twice daily, taken after meals. The efficacy of both groups was observed after 2 weeks of treatment.

[0120] Efficacy evaluation criteria: Based on the "Standards for Diagnosis and Efficacy Evaluation of Diseases and Syndromes in Traditional Chinese Medicine" issued by the State Administration of Traditional Chinese Medicine on June 28, 1994.

[0121] Recovery: Pain symptoms disappeared, lower back and leg mobility returned to normal, and there was no recurrence within six months.

[0122] Significant effect: Pain symptoms are reduced, waist and leg mobility is basically normal, and there is an occasional recurrence within six months.

[0123] Effective: Pain symptoms are slightly reduced, but waist and leg mobility is limited.

[0124] Ineffective: Pain symptoms were not relieved.

[0125] result

[0126] The efficacy of treatment group and control group

[0127] Table 1. Statistical table of efficacy between the treatment group and the control group.

[0128] Group Number of examples get well Effective efficient invalid Overall effectiveness % Treatment group 150 80 42 20 8 94.6％ control group 80 16 30 18 16 80％

[0129] The comparison between the two groups showed a highly significant difference (P < 0.05) according to the chi-square test.

[0130] Table 2 Comparison of clinical symptoms before and after treatment in the treatment group and the control group.

[0131]

[0132] Table 3 Relationship between TCM syndrome differentiation and therapeutic effect

[0133] Traditional Chinese Medicine Classification Number of examples get well Effective efficient invalid Overall effectiveness % Wind-cold-dampness arthralgia 90 60 15 15 0 100 Rheumatic fever 35 15 5 7 8 77 Phlegm and blood stasis obstruction 10 3 3 3 1 90 Liver and kidney deficiency 15 8 3 3 1 93

[0134] in conclusion

[0135] Rheumatic back and leg pain falls under the category of "Bi syndrome" in Traditional Chinese Medicine (TCM). It is characterized by pain, soreness, heaviness, numbness, or limited range of motion in the limbs, bones, joints, and muscles, often accompanied by stiffness, swelling, deformity, and impaired movement of the joints. Its onset is often related to external pathogenic factors such as wind, cold, dampness, and heat, as well as insufficient vital energy (Qi) in the body. The basic pathogenesis is obstruction of the meridians and stagnation of Qi and blood. The condition is recurrent, with a viscous and progressive course, severely impacting the patient's daily life. Western medicine attributes it to inflammation of the joints or soft tissues caused by certain bacterial or viral infections, and is associated with streptococcal infection and rheumatoid arthritis.

[0136] In summary, this study used this formula for treatment. A comparison between the treatment group and the control group revealed that the effective rate in the treatment group (94.6%) was significantly higher than that in the control group (80.0%) (P<0.05). The comparative analysis showed that the treatment group had a significantly better therapeutic effect. Rheumatic lumbago and leg pain fall under the category of "Bi syndrome" in Traditional Chinese Medicine (TCM). Pharmacological studies of TCM have found that this formula has the effects of tonifying the liver and kidneys, dispelling wind and cold, clearing the meridians, promoting blood circulation, and relieving pain. Pharmacological studies of Western medicine have found that this formula has anti-inflammatory, analgesic, antispasmodic, antiviral, antibacterial, antioxidant, hepatoprotective, antithrombotic, nerve-nourishing, osteoporosis-preventing, and immune-regulating effects. The TCM and Western medicine pharmacological effects of this formula are consistent in their therapeutic efficacy, effectively strengthening the body, clearing the meridians, reducing swelling and pain, and preventing recurrence. The capsule formulation is convenient to carry, not affected by time or location, has obvious therapeutic effects, and is highly accepted by patients, making it worthy of widespread promotion in clinical practice.

[0137] Although the present invention has been disclosed above with reference to preferred embodiments, it is not intended to limit the invention. Any person skilled in the art can make various modifications and refinements without departing from the spirit and scope of the invention; therefore, the scope of protection of the present invention should be defined by the claims.

Claims

1. A traditional Chinese medicine capsule preparation for treating rheumatic lumbago and leg pain, characterized in that: Its active ingredient is made from the following parts by weight of raw materials: Prepared Aconitum carmichaelii 4-8 parts, Prepared Aconitum kusnezoffii 4-8 parts, Clematis chinensis 8-12 parts, Gentiana macrophylla 10-14 parts, Chaenomeles speciosa 10-14 parts, Piper kadsura 12-18 parts, Bungarus fasciatus 0.3-0.7 pieces, Fried Paeonia lactiflora 12-17 parts, Astragalus membranaceus 10-30 parts, Saposhnikovia divaricata 8-12 parts, Spatholobus suberectus 10-20 parts, Angelica sinensis 10-20 parts, Panax notoginseng powder 8-12 parts, Dipsacus asper 8-12 parts, Achyranthes bidentata 10-20 parts, Bone marrow The preparation consists of 8-12 parts of Drynaria fortunei, 4-8 parts of Carthamus tinctorius, 4-8 parts of Asarum heterotropoides, 6-12 parts of Cinnamomum cassia, 4-8 parts of Buthus martensii, 8-12 parts of Bombyx mori, 6-12 parts of Anemarrhena asphodeloides, and 4-8 parts of Phellodendron chinense. The preparation is made by spraying the above-mentioned medicinal materials with 75% medical alcohol for disinfection, then allowing them to soak for 48 hours, drying them until the moisture content is ≤5%, pulverizing them through a 120-mesh sieve, mixing them evenly, and filling them into No. 0 capsules. Each capsule contains 0.5g of raw medicinal powder.

2. The traditional Chinese medicine capsule preparation for treating rheumatic lumbago and leg pain according to claim 1, characterized in that: The white-flowered snakes mentioned are either the golden-ringed white-flowered snake or the Qi snake, with each snake weighing ≥3g.

3. The traditional Chinese medicine capsule preparation for treating rheumatic lumbago and leg pain according to claim 1, characterized in that: The fineness of the Panax notoginseng powder is 100-120 mesh.

4. The traditional Chinese medicine capsule preparation for treating rheumatic lumbago and leg pain according to claim 1, characterized in that: In the preparation method, the drying temperature is 50-60℃ and the drying time is 2-3 hours.

5. The method for preparing a traditional Chinese medicine capsule formulation for treating rheumatic lumbago and leg pain according to claim 1, characterized in that: Includes the following steps: a) Weigh out each medicinal material according to the proportion, spray the surface with 75% medical alcohol for disinfection, and let it sit for 48 hours; b) Dry the moistened medicinal materials at 50-60℃ until the moisture content is ≤5%; c) Pulverize the dried medicinal materials and pass them through a 120-mesh sieve; d) Mix them evenly and fill them into No. 0 capsules, each capsule containing 0.5g of raw medicinal powder.

6. The method for preparing a traditional Chinese medicine capsule formulation for treating rheumatic lumbago and leg pain according to claim 5, characterized in that: In step a), the amount of alcohol sprayed is 10% to 15% of the total weight of the medicinal materials.

7. A traditional Chinese medicine capsule preparation for treating rheumatic lumbago and leg pain according to claim 1, characterized in that: Its quality control methods include the following indicators: The content of diester-type alkaloids in processed Aconitum carmichaelii is ≤0.01%; Astragaloside A content ≥0.08mg / g; The total saponin content of Panax notoginseng is ≥5.0%.

8. A traditional Chinese medicine capsule preparation for treating rheumatic lumbago and leg pain according to claims 1-7, characterized in that: The traditional Chinese medicine capsule formulation comprises a pharmaceutically acceptable carrier, wherein the carrier includes one or more of starch, dextrin, and magnesium stearate.

9. The application of the traditional Chinese medicine capsule preparation for treating rheumatic lumbago as described in claim 1 in the preparation of a drug having the following functions, characterized in that: Anti-inflammatory effects, inhibiting the expression of IL-6 and TNF-α; Analgesic effect, reduced the number of acetic acid writhing movements in mice by ≥40% (P<0.01 compared with the model group); It improves microcirculation and increases local blood flow velocity by ≥25%.

Images