Detoxifying and stasis-removing traditional Chinese medicine composition, capsule and preparation method thereof

Abstract

The invention discloses a detoxifying and stasis-removing traditional Chinese medicine composition, a capsule and a preparation method thereof. The traditional Chinese medicine composition for detoxifying and removing stasis is prepared from the following raw materials in parts by mass: 285 to 315 parts of radix scutellariae, 185 to 215 parts of rhizoma coptidis, 185 to 215 parts of radix sophorae flavescentis, 225 to 255 parts of fructus forsythiae, 225 to 255 parts of radix salviae miltiorrhizae, 185 to 215 parts of rhizoma polygoni cuspidati, 285 to 315 parts of herba artemisiae scopariae and 185 to 215 parts of pericarpium citri reticulatae. The traditional Chinese medicine composition has the major functions of clearing heat and drying dampness, purging fire and removing toxin, and activating blood and removing stasis. The traditional Chinese medicine is suitable for acne vulgaris (excessive heat in lung and stomach and damp-heat in stomach and intestine). Particularly, the skin lesion degree, the number of inflammatory skin lesions, the skin lesion color, the smooth and bright face and other symptoms are obviously improved.

Description

Technical Field

[0001] The invention belongs to the field of medicine, and particularly relates to a detoxifying and stagnation-dispersing traditional Chinese medicine composition, a capsule and a preparation method thereof. Background Art

[0002] Acne is the most common chronic inflammatory disease of the hair follicles and sebaceous glands in dermatology. It occurs most commonly on the cheeks, forehead, and jawline, but can also affect the trunk, such as the chest, back, and scapula. Characterized by comedones, papules, pustules, nodules, cysts, and scars, it is often accompanied by sebum secretion. It is common in adolescent boys and girls and is commonly referred to as "acne." Acne is a common inflammatory disease whose inflammatory process stimulates excessive melanin production, leading to abnormal melanin deposition. This inflammatory-induced skin pigmentation disorder causes hyperpigmentation in acne patients, and post-acne hyperpigmentation seriously impacts patients' quality of life.

[0003] Antibiotics remain a common treatment for acne vulgaris, but the choice of first-line antibiotic is empirical. Acne treatments in China and abroad primarily rely on long-term, low-dose tetracycline and topical tretinoin ointment, followed by oral estrogen. While both have some efficacy, long-term use can cause side effects and is therefore less commonly used clinically.

[0004] Clinical research on Traditional Chinese Medicine (TCM) treatments for acne has made significant progress in recent years, but effective internal Chinese patent medicines for the condition are limited. A search revealed that currently, products specifically indicated for acne treatment primarily consist of topical medications and health supplements, while internal medications include a few, including Qingre Anchuang Pills (Tablets), Fufang Zhenzhu Anchuang Tablets, Jinhua Xiaochuang Pills, Danshenone Capsules, Dihuang Yangyin Granules, Yiqing Capsules, and Qingchun Cuochuang Tablets. These medications fall far short of meeting clinical needs.

[0005] Therefore, developing a new and effective Chinese patent medicine for treating acne has important practical significance. Summary of the Invention

[0006] The invention aims to provide a traditional Chinese medicine composition for detoxification and dispersing stagnation.

[0007] The detoxifying and stagnation-dispersing traditional Chinese medicine composition provided by the present invention is prepared from the following raw materials in parts by weight: 285-315 parts of scutellaria baicalensis, 185-215 parts of coptis chinensis, 185-215 parts of sophora flavescens, 225-255 parts of forsythia suspensa, 225-255 parts of salvia miltiorrhiza, 185-215 parts of polygonum cuspidatum, 285-315 parts of scutellaria baicalensis, and 185-215 parts of tangerine peel.

[0008] Preferably, the detoxifying and stagnation-dispersing Chinese medicine composition is made from the following raw materials in parts by mass: 300 parts of Scutellaria baicalensis, 200 parts of Coptis chinensis, 200 parts of Sophora flavescens, 240 parts of Forsythia suspensa, 240 parts of Salvia miltiorrhiza, 200 parts of Polygonum cuspidatum, 300 parts of Artemisia capillaris, and 200 parts of dried tangerine peel.

[0009] The raw materials used to make the Chinese medicine composition of the present invention are proportioned according to parts by mass. During production, they can be increased or decreased according to the corresponding proportions. For example, large-scale production can be measured in kilograms or tons, and small-scale production can be measured in grams. The weight can be increased or decreased, but the mass ratio of the raw materials between the components remains unchanged.

[0010] The Chinese medicine composition provided by the present invention can be prepared into any oral preparation according to conventional Chinese medicine preparation methods. For example, the Chinese medicinal materials used to make the Chinese medicine composition can be mixed, decocted with water, filtered after decoction, and the filtrate collected. The decoction can be repeated twice, and the filtrates can be combined to obtain a water decoction (or decoction) of the Chinese medicine composition.

[0011] The ratio of the total mass of the Chinese medicinal materials to the mass of water can be 1:(8-10), and the specific amount of water added can be determined according to the mass of the medicinal materials.

[0012] To facilitate preparation and avoid the decocting step, each Chinese herbal medicine (such as Chinese herbal medicine slices) can be replaced with a corresponding amount of raw herbs in a commercially available Chinese herbal formula granules, and the Chinese herbal formula granules of each Chinese herbal medicine can be directly mixed. When using, it can be taken with boiled water.

[0013] "TCM formula granules" refer to single-ingredient TCM slices extracted using traditional Chinese medicine preparation methods, using appropriate solvents and procedures to extract the soluble active ingredients, followed by concentration and drying to produce powders or granules. They are packaged in fixed quantities for individual ingredients, allowing pharmacy personnel to follow physicians' orders and prescribe the prescribed dosage for direct patient consumption. TCM formula granules are extracts of the full ingredients of traditional TCM slices, offering comparable clinical efficacy and corresponding preparation requirements and quality control standards. They offer significant advantages over mixed decoctions of TCM slices in terms of stability and controllability.

[0014] In addition to the above two methods, each single herb (such as Chinese herbal medicine slices) in the above-mentioned Chinese medicine composition can be replaced with an extract of the main component of each herb in an equal amount of raw medicinal materials. The extracts of the main components of each single herb can be mixed and prepared into a solution, which can also achieve similar therapeutic effects after oral administration.

[0015] At the same time, the detoxification and stagnation-dispersing medicine prepared with the Chinese medicine composition provided by the present invention as the active ingredient also falls within the protection scope of the present invention.

[0016] The pharmaceutical composition can be prepared directly or by adding pharmaceutically acceptable excipients to any pharmaceutically acceptable dosage form. Examples of oral preparations include decoctions, granules, capsules, tablets, oral liquids, powders, pills, and dripping pills. These various dosage forms can be prepared according to conventional methods in the pharmaceutical field.

[0017] The present invention also protects the use of the above-mentioned traditional Chinese medicine composition in preparing medicines for treating acne.

[0018] Furthermore, the acne is acne vulgaris.

[0019] The Chinese medicine composition of this invention functions and treats: clearing away heat and dampness, purging fire and detoxifying, and promoting blood circulation and dispersing stagnation. It is suitable for acne vulgaris (a syndrome characterized by excessive heat in the lungs and stomach and damp-heat in the gastrointestinal tract). Symptoms include blackheads, red papules, and superficial pustules, sometimes accompanied by a small number of nodules; newly developed inflammatory skin lesions are swollen and painful; the face is oily and shiny; the mouth is dry, sticky, and bitter; the stool is constipated; and the urine is dark yellow; the tongue is red, with a greasy or white coating; and the pulse is stringy or slippery.

[0020] The present invention uses the theory of traditional Chinese medicine to explain the indications, pathogenesis and treatment principles: Acne falls under the categories of "lung wind acne," "acne face," and "alcohol acne" in Traditional Chinese Medicine. Ancient physicians believed the onset of acne was related to lung heat, while Western medicine links the onset of acne to factors such as excessive sebum secretion during adolescence, keratinization and blockage of the sebaceous gland ducts, proliferation of acne propionate rods, and endocrine imbalances.

[0021] Traditional Chinese Medicine believes that young people are full of vitality and possess a preponderance of yang and heat. This, combined with mental stress, can lead to the transformation of the five emotions into fire, or excessive consumption of spicy foods can cause internal heat. This can lead to heat accumulation in the lungs and stomach, which can then travel up the meridians and cause red papules and pustules on the face. Excessive heat and toxicity can stagnate in the skin, locally obstructing the meridians and causing stasis of Qi and blood, resulting in deep, red papules, pustular papules, red nodules, and localized swelling and pain. Alternatively, an irregular diet, such as excessive consumption of greasy, fatty, and sweet foods, can cause dampness and heat in the stomach and intestines, which rises and becomes trapped in the skin, causing oiliness on the face and upper back, acne, papules, and even cysts. Over time, heat, toxic dampness, and heat can block the meridians, leading to internal blood clots. Alternatively, imbalance in the Chong and Ren meridians can cause blood stasis, or heat, toxic dampness, and heat can block Qi, affecting the distribution of body fluids and causing them to boil into phlegm. The phlegm and stasis can then coalesce, leading to dark red papules, nodules, abscesses, cysts, and scars.

[0022] According to the analysis of the pathogenesis, the treatment of acne should focus on clearing away heat from the lungs and stomach, detoxifying and drying out dampness, and activating blood circulation and dispersing stagnation.

[0023] The detoxification and stagnation-dispersing Chinese medicine composition provided by the present invention is explained as follows: According to the analysis of the pathogenesis, the treatment of acne should be based on clearing away heat and dampness in the lungs and stomach, detoxifying and drying dampness, and promoting blood circulation and dispersing stagnation. The functions of the detoxifying and dispersing stagnation Chinese medicine composition are clearing away heat and dampness, purging fire and detoxifying, and promoting blood circulation and dispersing stagnation. In the prescription, Scutellaria baicalensis is the monarch. Scutellaria baicalensis is bitter in taste and cold in nature. It has the functions of clearing heat and drying dampness, purging fire and detoxifying. It can not only clear the lung fire in the upper part of the body, but also clear damp heat in the intestines. Coptis chinensis and Sophora flavescens are the ministerial drugs. Coptis chinensis is good at clearing stomach fire in the middle part of the body, while Sophora flavescens is good at clearing heat and drying dampness, guiding damp heat to penetrate into the lower orifices. The three drugs work together to clear away heat and heat in the lungs and stomach, and clear damp heat in the stomach and intestines. Forsythia suspensa is also used as the ministerial drug. Forsythia suspensa has the functions of clearing heat and detoxifying, clearing light and floating, clearing heat and toxins in the upper part of the body, and has the effect of eliminating carbuncle and dispersing stagnation. It is a holy medicine for sores, assisting Scutellaria baicalensis in clearing heat and detoxifying, eliminating sores and dispersing stagnation. For the pathogenesis of heat toxicity stagnation and blood stasis, select Danshen and Polygonum cuspidatum as adjuvants. Danshen is slightly cold in nature, has the function of promoting blood circulation and relieving fatigue, and has cooling blood and nourishing blood. Polygonum cuspidatum is flat in nature, has the effect of promoting blood circulation and dredging menstruation, and can clear away heat and toxic substances and eliminate dampness. The two medicines assist the monarch and ministerial medicines in promoting blood circulation and regulating menstruation, dispersing stasis and relieving swelling and pain, and can promote skin lesions to disappear as soon as possible. Artemisia capillaris is also an adjuvant, clearing away damp-heat, guiding damp-heat downward, giving the evil that is blocked in the body a way out. With dried tangerine peel as the messenger, dried tangerine peel is pungent in taste, good at regulating qi and eliminating stagnation, and bitter and warming and drying dampness, resolving phlegm and dispersing stagnation, entering the lung meridian and reaching the skin, leading all medicines to directly reach the affected area. All medicines are used together to reach the effect of clearing away stomach heat toxicity, clearing away dryness and clearing damp-heat, promoting blood circulation and regulating menstruation, and resolving phlegm and dispersing stagnation.

[0024] The Jiedu Sanjie capsule formula provided herein is an effective acne treatment formula developed through years of clinical experience, continuous refinement, and repeated revisions. Researchers have been using this formula to treat acne since 1996, with clinical use in thousands of patients, demonstrating significant efficacy, safety, and no side effects. In 2001, in accordance with the technical requirements for the development of Class III new Chinese medicines, a systematic study of the preparation process, quality standards, and primary efficacy and toxicity studies was conducted. This solid foundation of preliminary work suggests promising prospects for development and application. On May 25, 2003, the formula received National Drug Clinical Research Approval No. 2003L01958. DETAILED DESCRIPTION

[0025] The present invention will be further described in detail below in conjunction with specific embodiments. The examples provided are only for illustrating the present invention and are not intended to limit the scope of the present invention. The examples provided below can serve as a guide for further improvements by those skilled in the art and are not intended to limit the present invention in any way.

[0026] Unless otherwise specified, the experimental methods in the following examples are conventional methods and were performed according to the techniques or conditions described in the literature in the field or according to the product instructions. The materials and reagents used in the following examples, unless otherwise specified, were all commercially available.

[0027] Example 1. Preparation of Jiedu Sanjie Capsules Prescription composition: Scutellaria baicalensis 300g, Coptis chinensis 200g, Sophora flavescens 200g, Forsythia suspensa 240g, Salvia miltiorrhiza 240g, Polygonum cuspidatum 200g, Artemisia capillaris 300g, and Tangerine peel 200g.

[0028] The above is the prescription amount for preparing 1000 capsules.

[0029] The preparation method is as follows: According to the prescribed amount, weigh the Chinese medicine formula granules of each medicinal material corresponding to the prescribed amount of crude drugs of each medicinal material, directly mix the above Chinese medicine formula granules, mix evenly and then pack them into 1000 capsules.

[0030] Example 2: Clinical efficacy data of Jiedu Sanjie Capsule in treating acne vulgaris According to the "Regulations on the Management of Clinical Trials of Drugs", "Several Provisions on Clinical Research of Drugs", "Clinical Research of New Chinese Medicines", Clinical Research Guidance Principles, Drug Registration Management Measures, Diagnosis and Efficacy Standards of Traditional Chinese Medicine Diseases and Syndromes, Practical Dermatology (Edited by Liu Furen. - Beijing: People's Medical Publishing House, 2nd edition, 1996), Jiedu Sanjie Capsules The prescription composition of Jiedu Sanjie Capsules, the preclinical pharmacology, toxicology, and pharmacodynamics research data of Jiedu Sanjie Capsules, and the clinical pilot research data of Jiedu Sanjie Capsules were discussed repeatedly by relevant experts, and the Phase II and Phase III research plans and programs for the clinical research were formulated.

[0031] According to the research plan, a Phase II clinical trial of Jiedu Sanjie Capsules was conducted from August 2003 to February 2004. The trial investigated the efficacy and safety of the drug for acne vulgaris (a syndrome characterized by excessive lung and stomach heat or combined with gastrointestinal damp-heat) and explored the appropriate dosage and course of treatment. The Phase II trial was led by the Affiliated Hospital of Hubei University of Traditional Chinese Medicine, with participation from the Beijing Hospital of Traditional Chinese Medicine affiliated with Capital Medical University, the Second Affiliated Hospital of Tianjin University of Traditional Chinese Medicine, and Tianjin Changzheng Hospital. A total of 240 subjects were randomly divided into a treatment group (Jiedu Sanjie Capsules) with 120 patients and a control group (Qingre Anchuang Tablets) with 120 patients. A total of 222 subjects completed the trial, including 109 in the treatment group and 113 in the control group. The treatment course lasted four weeks (the experimental group received the Jiedu Sanjie Capsules provided by the present invention orally, four capsules three times daily; the control group received Qingre Anchuang Tablets orally, four capsules three times daily). Efficacy scores were assessed before and after treatment, and safety assessments were conducted.

[0032] Phase II clinical trial results showed that: Clinical efficacy of acne vulgaris: Based on the changes in symptom scores before and after treatment, such as the degree of skin lesions, the number of inflammatory lesions, the color of skin lesions, swelling and ulceration, oily and shiny face, dry and sticky mouth, constipation, and yellow urine, the efficacy is evaluated as clinically cured, significantly effective, effective, or ineffective.

[0033] The above analysis results showed that both the Jiedu Sanjie Capsule treatment group and the control group (Qingre Anchuang Tablet treatment group) had significant efficacy in treating acne vulgaris. After four weeks of treatment, the grading assessment of acne vulgaris efficacy showed that the cure and marked efficacy rates (cured + markedly effective) in the treatment group were 68.8% (ITT population) and 70.6% (PP population), and the total effective rate (cured + markedly effective + effective) was 87.6%. The cure and marked efficacy rates in the control group were 53.0% (ITT population) and 54.0% (PP population), and the total effective rate was 76.9% (ITT population) and 77.9% (PP population). The difference in efficacy between the two groups was P < 0.05 in the ITT population and P < 0.05 in the PP population, indicating that Jiedu Sanjie Capsule is more effective than Qingre Anchuang Tablet for treating acne vulgaris.

[0034] Evaluation of TCM syndrome efficacy: After four weeks of treatment, both groups showed significant efficacy in terms of TCM syndromes. The cure and marked efficacy rates (cured + markedly effective) in the treatment group were 63.4% (ITT population) and 65.1% (PP population), and the total effective rate (cured + markedly effective + effective) was 89.3% (ITT population) and 89.9% (PP population). In the control group, the cure and marked efficacy rates were 43.6% (ITT population) and 44.2% (PP population), and the total effective rate was 75.2% (ITT population) and 76.9% (PP population). The difference in efficacy between the two groups was P < 0.01 in the ITT population and P < 0.01 in the PP population, indicating that Jiedu Pingchuang Capsules are significantly more effective in treating acne vulgaris and superior to Qianqingre Anchuang Tablets.

[0035] Based on the results of the Phase II clinical trial, a Phase III clinical trial was conducted from May to October 2004, with a four-week course of treatment, to further evaluate the efficacy and safety of Jiedu Pingkang Jiaodu in the treatment of acne vulgaris (a syndrome characterized by excessive lung and stomach heat or combined with gastrointestinal damp-heat). The Phase III clinical trial was again led by the Affiliated Hospital of Hubei University of Traditional Chinese Medicine, with participation from the Beijing Hospital of Traditional Chinese Medicine affiliated with Capital Medical University, the Second Affiliated Hospital of Tianjin University of Traditional Chinese Medicine, Tianjin Changzheng Hospital, and Shaanxi Provincial People's Hospital. A total of 440 patients were enrolled, with 330 in the treatment group and 110 in the control group. Of these, 414 completed the entire trial, including 309 in the treatment group and 105 in the control group.

[0036] The efficacy results of the Phase III clinical trial showed that: Clinical efficacy of acne vulgaris: Based on the changes in the symptom scores before and after treatment, such as the degree of skin lesions, the number of inflammatory lesions, the color of skin lesions, swelling and ulceration, oily and shiny face, sticky and bitter mouth, constipation, and yellow urine, the treatment is evaluated as clinically cured, significantly effective, effective, or ineffective.

[0037] The above analysis results showed that both Jiedu Sanjie Capsules and Qingre Anchuang Tablets had significant efficacy in treating acne vulgaris. After four weeks of treatment, the treatment group had a cure and marked effect rate (cured + markedly effective) of 45.1% (FAS) and 45.3% (PPS) in the grading assessment of acne vulgaris efficacy, and a total effective rate (cured + markedly effective + effective) of 80.9% (FAS) and 80.9% (PPS). The control group had a cure and marked effect rate of 32.7% (FAS) and 31.4% (PPS), and a total effective rate of 69.1% (FAS) and 69.5% (PPS). The difference in efficacy between the two groups was P < 0.05 in the FAS group and P < 0.05 in the PPS group, indicating that Jiedu Sanjie Capsules were more effective than Qingre Anchuang Tablets in treating acne vulgaris.

[0038] TCM syndrome efficacy: After 4 weeks of treatment, both TCM syndrome groups showed significant efficacy, and the cure rate (cured The total effective rate (cured + markedly effective + effective) was 41.1% (FAS population) and 41.1% (PPS population), and the total effective rate (cured + markedly effective + effective) was 41.1% (FAS population) and 41.1% (PPS population). The cure and significant cure rates in the control group were 76.8% (FAS group) and 77.7% (PPS group), respectively. The control group had a cure and significant cure rate of 30.0% (FAS group) and 28.6% (PPS group), and a total effective rate of 62.7% (FAS group) and 62.9% (PPS group). The difference in efficacy between the two groups was P < 0.05 in the FAS group and P < 0.05 in the PPS group, indicating that Jiedu Sanjie Capsule is more effective than Qingre Anchuang Tablet for treating acne vulgaris.

[0039] in conclusion 1. Clinical trials were conducted on 680 subjects in 5 clinical research centers. The results showed that Zuo Capsule has significant therapeutic effect in treating common acne vulgaris (excessive heat in the lungs and stomach or combined with damp-heat in the gastrointestinal tract), especially in improving the degree of skin lesions, the number of inflammatory lesions, the color of skin lesions, and the oily and shiny appearance of the face.

[0040] 2. Recommended dosage: Oral administration: 4 capsules each time, 3 times a day, 1 month as a course of treatment.

[0041] 3. No obvious adverse reactions were observed in clinical trials of Jiedu Sanjie Capsules, and no adverse effects were found on patients' blood, urine, stool routine, liver, kidney function, and electrocardiogram.

[0042] In summary, Jiedu Sanjie Capsule is effective in treating acne vulgaris caused by excessive heat in the lungs and stomach or combined with gastrointestinal dampness, with few toxic and side effects, and is worthy of clinical promotion and application.

[0043] The present invention has been described in detail above. It will be apparent to those skilled in the art that the present invention may be practiced over a wide range of parameters, concentrations, and conditions without departing from the spirit and scope of the present invention and without unnecessary experimentation. Although specific embodiments have been given herein, it should be understood that further modifications may be made to the present invention. In summary, this application is intended to encompass any variations, uses, or improvements to the present invention, including those made by conventional techniques known in the art that depart from the scope of the present invention. Applications of the essential features may be made within the scope of the following claims.

Claims

1. A detoxifying and stagnation-dispersing Chinese medicine composition, which is made from the following raw materials in parts by mass: 285-315 parts of Scutellaria baicalensis, 185-215 parts of Coptis chinensis, 185-215 parts of Sophora flavescens, 225-255 parts of Forsythia suspensa, 225-255 parts of Salvia miltiorrhiza, 185-215 parts of Polygonum cuspidatum, 285-315 parts of Artemisia capillaris, and 185-215 parts of dried tangerine peel.

2. The detoxification and stagnation-dispersing Chinese medicine composition according to claim 1 is made from the following raw materials in parts by mass: 300 parts of Scutellaria baicalensis, 200 parts of Coptidis rhizome, 200 parts of Sophora flavescens, 240 parts of Forsythia suspensa, 240 parts of Salvia miltiorrhiza, 200 parts of Polygonum cuspidatum, 300 parts of Artemisia capillaris, and 200 parts of dried tangerine peel.

3. A medicine for treating acne, the active ingredient of which comprises the Chinese medicine composition according to claim 1 or 2.

4. The drug according to claim 3, characterized in that: The acne is acne vulgaris.

5. The drug according to claim 4, characterized in that: The acne vulgaris is manifested as excessive heat in the lungs and stomach or combined with damp-heat in the gastrointestinal tract.

6. The drug according to any one of claims 3 to 5, characterized in that: The drug has obvious effects on improving the symptoms of acne such as the degree of skin lesions, the number of inflammatory skin lesions, the color of skin lesions, and the oily and shiny face.

7. A detoxification and relieving capsule, the active ingredient of which comprises the traditional Chinese medicine composition according to claim 1 or 2.