A traditional Chinese medicine composition for treating ulcerative colitis, a preparation method and application thereof

Abstract

The application discloses a traditional Chinese medicine composition for treating ulcerative colitis and a preparation method and application thereof, and relates to a traditional Chinese medicine composition for treating ulcerative colitis, which is composed of the following components in proportion by weight: radix astragali, rhizoma coptidis, radix scrophulariae, bletilla striata, indigo naturalis, rhizoma corydalis and radix glycyrrhizae. The application has the following remarkable advantages: remarkable synergistic effect, the effect of the traditional Chinese medicine composition of the application on improving the weight loss, hematochezia, DAI score and reducing intestinal inflammation of ulcerative colitis mice is remarkably better than that of any single medicine in the important composition, which proves that there is a remarkable synergistic effect among the components; the mucosal barrier protection is better than that of infliximab; the comprehensive curative effect is equivalent, and the compliance is better; and the drug economy has the advantages that the medicinal materials selected by the application are common traditional Chinese medicines, are widely sourced and are low in price, thereby greatly reducing the treatment cost of patients and being suitable for long-term maintenance treatment.

Description

Technical Field

[0001] This invention belongs to the field of traditional Chinese medicine technology, specifically relating to a traditional Chinese medicine composition for treating ulcerative colitis, its preparation method, and its application. Background Technology

[0002] Ulcerative colitis (UC) is a chronic, nonspecific inflammatory bowel disease of unknown etiology, with lesions primarily limited to the colonic mucosa and submucosa. Clinical manifestations include diarrhea, bloody and mucous stools, and abdominal pain. The condition is characterized by recurrent episodes and is difficult to cure, leading the World Health Organization to classify it as one of the most intractable diseases in modern medicine.

[0003] Currently, clinical treatment for ulcerative colitis (UC) mainly employs aminosalicylic acids, glucocorticoids, immunosuppressants, and biologics (such as infliximab). Aminosalicylic acids are only suitable for mild to moderate UC. For severe UC or moderate to severe patients in the active phase, 5-ASA often fails to effectively control inflammation, requiring rapid escalation of treatment. Glucocorticoids are insufficient due to their "symptom-treating but not root-cause-treating" nature and significant side effects: inability to maintain remission, hormone dependence and resistance, severe systemic side effects, and lack of mucosal repair capacity. Immunosuppressants are also insufficient due to slow onset of action, risks associated with bone marrow transplantation, hepatotoxicity and tumor risk, and high testing costs. While biologics are effective in inducing remission and promoting mucosal healing, they suffer from high cost, inconvenient administration methods (mostly injection), poor patient compliance, potential for anti-antibody development with long-term use, and the risk of infection.

[0004] Traditional Chinese medicine categorizes ulcerative colitis under the terms "chronic dysentery," "relapsing dysentery," and "mastitis." Its core pathogenesis is often attributed to internal damp-heat, leading to stagnation of qi and blood in the intestines, damage to the intestinal mucosa, and tissue decay. Although numerous traditional Chinese medicine formulas exist, no oral formulas have been reported that address this pathogenesis in a way that simultaneously clears heat and dampness, regulates qi and blood, and is superior to biological agents in protecting the intestinal mucosal barrier function.

[0005] Therefore, developing a traditional Chinese medicine composition that is effective, inexpensive, easy to take, and can effectively repair the intestinal mucosal barrier is of great clinical significance and social value. Summary of the Invention

[0006] The purpose of this invention is to overcome the shortcomings of the prior art and provide a traditional Chinese medicine composition for treating ulcerative colitis.

[0007] The second objective of this invention is to provide a method for preparing a traditional Chinese medicine composition for treating ulcerative colitis.

[0008] A third objective of this invention is to provide the application of a traditional Chinese medicine composition for treating ulcerative colitis in the preparation of a medicament for treating ulcerative colitis.

[0009] The technical solution of this invention is summarized as follows: A traditional Chinese medicine composition for treating ulcerative colitis, comprising the following components in parts by weight: Astragalus membranaceus 30-60 parts, Coptis chinensis 15-30 parts, Scutellaria baicalensis 15-30 parts, Bletilla striata 25-45 parts, Indigo naturalis 2-5 parts, Corydalis yanhusuo 15-30 parts, and Glycyrrhiza uralensis 20-35 parts.

[0010] Preferably, the composition of Astragalus membranaceus is 45.18 parts, Coptis chinensis is 20.88 parts, Scutellaria baicalensis is 20.88 parts, Bletilla striata is 34.74 parts, Indigo naturalis is 3.42 parts, Corydalis yanhusuo is 23.22 parts, and Glycyrrhiza uralensis is 27.72 parts.

[0011] A method for preparing a traditional Chinese medicine composition for treating ulcerative colitis includes the following steps: Step 1: Weigh the following medicinal slices as raw materials according to the following weight proportions: Astragalus membranaceus 30-60 parts, Coptis chinensis 15-30 parts, Scutellaria baicalensis 15-30 parts, Bletilla striata 25-45 parts, Corydalis yanhusuo 15-30 parts, and Glycyrrhiza uralensis 20-35 parts; Step 2: Soak the raw materials in water equivalent to 9-11 times their weight, and decoct for 1-2 hours; filter, add water equivalent to 7-9 times their weight to the residue, and decoct for 0.5-1 hour; combine the filtrates, concentrate to 1 / 15-1 / 10 of the combined filtrate volume, add 2-5 parts by weight of indigo powder, mix well, and obtain a traditional Chinese medicine composition for treating ulcerative colitis.

[0012] The application of the above-mentioned traditional Chinese medicine composition in the preparation of drugs for treating ulcerative colitis.

[0013] Advantages of this invention: Animal experiments have demonstrated that this invention has the following significant advantages compared to existing technologies: 1. Significant synergistic effect: The effects of the herbal composition of this invention on improving weight loss, hematochezia, DAI score and reducing intestinal inflammation in mice with ulcerative colitis are significantly better than the individual use of any single herb in the important composition, proving that there is a significant synergistic effect among the components.

[0014] 2. Superior Mucosal Barrier Protection Compared to Infliximab: Experimental results show that the herbal composition of this invention is significantly more effective than the first-line clinical drug infliximab in maintaining intestinal permeability and repairing the mucosal barrier. This is of crucial significance for preventing UC recurrence and blocking antigen translocation.

[0015] 3. Comparable overall efficacy with better patient compliance: The overall anti-inflammatory and anti-ulcer effects of the traditional Chinese medicine composition of this invention are basically equivalent to those of infliximab. However, the traditional Chinese medicine composition of this invention can be made into an oral formulation, avoiding the pain and inconvenience caused by injection of biological agents, and greatly improving patient compliance.

[0016] 4. Pharmacoeconomic advantages: The medicinal materials selected in this formula are all commonly used Chinese herbs, widely available and inexpensive, which greatly reduces the treatment cost for patients and is suitable for long-term maintenance therapy. This combination has the effects of clearing heat and dampness, regulating qi and blood. It is not only more effective than single herbs, but also superior to first-line clinical infliximab in protecting the mucosal barrier. Attached Figure Description

[0017] Figure 1 The figure shows the effect of the four groups of the present invention on the general condition and DAI score of mice with ulcerative colitis.

[0018] Figure 2 The figure shows the effect of the fourth group of the present invention on the loss of intestinal villi and inflammatory cell infiltration in mice with ulcerative colitis.

[0019] Figure 3 The figure shows the effect of the 4th group of the present invention on the mucosal barrier function of mice with ulcerative colitis. Detailed Implementation

[0020] Explanation: The composition of the present invention closely addresses the pathogenesis of "internal damp-heat".

[0021] The principal herbs are Coptis chinensis and Scutellaria baicalensis. Both are bitter and cold in nature, clearing heat and drying dampness, thickening the intestines and stopping dysentery, and directly counteracting the damp-heat in the middle jiao.

[0022] The accompanying herbs are: Astragalus membranaceus, Bletilla striata, and Corydalis yanhusuo. Astragalus membranaceus tonifies Qi and raises Yang, promotes tissue regeneration and eliminates toxins, thus assisting the body's vital energy; Bletilla striata astringes and stops bleeding, reduces swelling and promotes tissue regeneration, and is especially good at protecting the membranes; Corydalis yanhusuo invigorates blood, promotes Qi circulation, and relieves pain, thus regulating Qi and blood.

[0023] Adjuvant ingredient: Indigo naturalis. Salty and cold in nature, it clears heat, cools the blood, calms the nerves, and detoxifies. When taken with water, it can directly reach the affected area.

[0024] Medicinal herb: Licorice. It harmonizes the effects of other herbs and also has the functions of relieving pain, replenishing qi, and strengthening the middle jiao (spleen and stomach).

[0025] The formula works synergistically to clear heat and dampness, regulate qi and blood, and promote wound healing and tissue regeneration.

[0026] The present invention will be further described below through specific embodiments. The weight parts of the following embodiments are in grams, but do not limit the present invention.

[0027] Example 1 A traditional Chinese medicine composition for treating ulcerative colitis, comprising the following components by weight: Astragalus membranaceus 45.18 parts, Coptis chinensis 20.88 parts, Scutellaria baicalensis 20.88 parts, Bletilla striata 34.74 parts, Indigo naturalis 3.42 parts, Corydalis yanhusuo 23.22 parts, and Glycyrrhiza uralensis 27.72 parts.

[0028] Example 2 A traditional Chinese medicine composition for treating ulcerative colitis, comprising the following components in parts by weight: Astragalus membranaceus 30 parts, Coptis chinensis 30 parts, Scutellaria baicalensis 15 parts, Bletilla striata 45 parts, Indigo naturalis 2 parts, Corydalis yanhusuo 30 parts, and Glycyrrhiza uralensis 20 parts.

[0029] Example 3 A traditional Chinese medicine composition for treating ulcerative colitis, comprising the following components by weight: 60 parts Astragalus membranaceus, 15 parts Coptis chinensis, 30 parts Scutellaria baicalensis, 25 parts Bletilla striata, 5 parts Indigo naturalis, 15 parts Corydalis yanhusuo, and 35 parts Glycyrrhiza uralensis.

[0030] Example 4 A method for preparing a traditional Chinese medicine composition for treating ulcerative colitis includes the following steps: Step 1: Weigh the following medicinal slices as raw materials according to the following weight proportions: Astragalus membranaceus 45.18 parts, Coptis chinensis 20.88 parts, Scutellaria baicalensis 20.88 parts, Bletilla striata 34.74 parts, Corydalis yanhusuo 23.22 parts, and Glycyrrhiza uralensis 27.72 parts; Step 2: Soak the raw materials in water equal to 10 times their volume for 2 hours, then decoct for 1.5 hours; filter, add water equal to 8 times their volume to the residue and decoct for 1 hour; combine the filtrates, concentrate to 1 / 15 of the combined filtrate volume, add 3.42 parts by weight of indigo powder and mix well (or add during the formulation process) to obtain a traditional Chinese medicine composition for treating ulcerative colitis.

[0031] Example 5 A method for preparing a traditional Chinese medicine composition for treating ulcerative colitis includes the following steps: Step 1: Weigh the following medicinal slices as raw materials according to the following weight proportions: Astragalus membranaceus 30 parts, Coptis chinensis 30 parts, Scutellaria baicalensis 15 parts, Bletilla striata 45 parts, Corydalis yanhusuo 30 parts and Glycyrrhiza uralensis 20 parts; Step 2: Soak the raw materials in water equal to 9 times their volume for 2 hours, then decoct for 1 hour; filter, add water equal to 9 times their volume to the residue and decoct for 1 hour; combine the filtrates, concentrate to 1 / 15 of the combined filtrate volume, add 2 parts by weight of indigo powder and mix well (or add during the formulation process) to obtain a traditional Chinese medicine composition for treating ulcerative colitis.

[0032] Example 6 A method for preparing a traditional Chinese medicine composition for treating ulcerative colitis includes the following steps: Step 1: Weigh the following medicinal slices as raw materials according to the following weight proportions: Astragalus membranaceus 60 parts, Coptis chinensis 15 parts, Scutellaria baicalensis 30 parts, Bletilla striata 25 parts, Corydalis yanhusuo 15 parts, and Glycyrrhiza uralensis 35 parts; Step 2: Soak the raw materials in water equivalent to 11 times their volume for 2 hours, then decoct for 2 hours; filter, add water equivalent to 7 times their volume for 7 times their volume to the residue and decoct for 0.5 hours; combine the filtrates, concentrate to 1 / 10 of the combined filtrate volume, add 5 parts by weight of indigo powder and mix well (or add during the formulation process) to obtain a traditional Chinese medicine composition for treating ulcerative colitis.

[0033] Example 7: Pharmacodynamic Evaluation Study 1. Experimental Materials and Methods Animals: C57BL / 6 male mice, weighing approximately 20g, 6-8 weeks old.

[0034] Grouping: Mice were randomly divided into a blank control group, a model group, a monoclonal antibody group, an example 4 group, and seven single-herb groups, with 10 mice in each group.

[0035] Blank control group: Free access to distilled water; Model group: A model of ulcerative colitis was established by allowing free access to distilled water containing 4% DSS (sodium dextran sulfate) for 6 days; Monoclonal antibody group: Infliximab (5 mg / kg, Sigma) was injected intraperitoneally on day 1 and day 4 after successful modeling. Example 4 group: After successful modeling, the drug prepared in Example 4 was administered by gavage in a volume of 0.2 mL for 5 consecutive days; Astragalus group: After successful modeling, Astragalus decoction was administered by gavage at a volume of 0.2 mL once a day for 5 consecutive days; Coptis chinensis group: After successful modeling, Coptis chinensis decoction was administered by gavage at a volume of 0.2 mL once a day for 5 consecutive days. Scutellaria baicalensis group: After successful modeling, Scutellaria baicalensis decoction was administered by gavage at a volume of 0.2 mL once a day for 5 consecutive days; Bletilla striata group: After successful modeling, Bletilla striata decoction was administered by gavage at a volume of 0.2 mL once a day for 5 consecutive days. Indigo group: After successful modeling, indigo water mixture was administered by gavage at a volume of 0.2 mL once a day for 5 consecutive days; Corydalis group: After successful modeling, Corydalis decoction was administered by gavage at a volume of 0.2 mL once a day for 5 consecutive days. Licorice group: After successful modeling, 0.2 mL of licorice decoction was administered by gavage for 5 consecutive days. The Astragalus group used 45.18 parts of Astragalus to replace the raw materials in step one of Example 4, and adopted the method in step two, without adding Indigo naturalis to obtain the decoction.

[0036] The Coptis chinensis group, Scutellaria baicalensis group, Bletilla striata group, Corydalis yanhusuo group, and Glycyrrhiza uralensis group were treated the same as the Astragalus membranaceus group.

[0037] The indigo group was prepared by taking 3.42 parts of indigo and adding 202 mL of water to obtain an indigo suspension.

[0038] 2. Detection indicators: Observe the general condition of mice, record changes in body weight, fecal hemorrhage, and DAI score; observe the histopathological changes in colon tissue (loss of intestinal villi, inflammatory cell infiltration) by HE staining; administer 100 mg / kg of FITC-glucan to mice by gavage on the day of tissue collection, and detect the fluorescence intensity of FITC in serum 4 hours later using a multi-functional microplate reader to characterize intestinal permeability and assess mucosal barrier function.

[0039] 3. Experimental Results (1) General condition and DAI score: such as Figure 1 As shown, compared with the blank control group, the model group mice showed significant weight loss, obvious rectal bleeding, and a significantly higher DAI score, indicating successful model construction. Compared with the model group, the weight loss of mice in the Example 4 group, the monoclonal antibody group, and the different single-herb treatment groups was delayed, rectal bleeding was significantly improved, and DAI scores were significantly reduced. Among them, the weight loss, rectal bleeding, and DAI score of the Example 4 group were significantly lower than those of the single-herb groups, and there was no significant difference from the monoclonal antibody group (infliximab).

[0040] (2) Anti-inflammatory effect: HE staining can characterize the degree of colonic mucosal loss and inflammatory cell infiltration, and is an important phenotype of intestinal inflammation. For example... Figure 2 The HE staining results showed that, compared with the blank group, the model group mice had more severe mucosal deficiencies and significant inflammatory cell infiltration. The intestinal mucosal structure of mice in the Example 4 group, the monoclonal antibody group, and the single herb treatment group were relatively intact, and the inflammatory cell infiltration was significantly reduced, indicating that they had good anti-inflammatory effects. Among them, the anti-inflammatory effect of the drug prepared in Example 4 was significantly better than that of the seven single herbs (p<0.05, p<0.001, p<0.0001), and comparable to that of the monoclonal antibody group.

[0041] (3) Mucosal barrier function (core advantage): The content of FITC-glucan in serum characterizes intestinal permeability and mucosal barrier function, which is the core pathological mechanism of ulcerative colitis. For example... Figure 3 As shown, compared with the blank control group, the serum FITC fluorescence intensity (characterizing FITC-glucan content) of mice in the model group was significantly increased, indicating severe damage to the mucosal barrier. The FITC fluorescence intensity of mice in the Example 4 group and the monoclonal antibody group was significantly lower than that of the model group, with the FITC fluorescence intensity of the Example 4 group being significantly lower than that of the monoclonal antibody group (P<0.05). The results indicate that the Example 4 group is superior to infliximab in protecting and repairing the intestinal mucosal mechanical barrier.

[0042] Experiments have shown that the traditional Chinese medicine compositions prepared in Examples 5 and 6 have similar effects on mouse body weight, fecal hemorrhage, DAI score, anti-inflammatory effect, and mucosal barrier function as those prepared in Example 4.

[0043] 4. Conclusion: This invention provides a treatment for ulcerative colitis that exerts its anti-ulcerative colitis effect through multiple targets and pathways. It not only retains the advantages of holistic regulation found in traditional Chinese medicine compound formulas (superior to single-herb formulations), but also surpasses existing biological agents such as infliximab in key mucosal repair indicators. Furthermore, it offers the advantages of oral administration and low cost, making it highly valuable for clinical application.

Claims

1. A traditional Chinese medicine composition for treating ulcerative colitis, characterized in that... The ingredients are composed of the following components by weight: Astragalus membranaceus 30-60 parts, Coptis chinensis 15-30 parts, Scutellaria baicalensis 15-30 parts, Bletilla striata 25-45 parts, Indigo naturalis 2-5 parts, Corydalis yanhusuo 15-30 parts, and Glycyrrhiza uralensis 20-35 parts.

2. The composition according to claim 1, characterized in that... The composition of the herbs was as follows: Astragalus membranaceus (45.18 parts), Coptis chinensis (20.88 parts), Scutellaria baicalensis (20.88 parts), Bletilla striata (34.74 parts), Indigo naturalis (3.42 parts), Corydalis yanhusuo (23.22 parts), and Glycyrrhiza uralensis (27.72 parts).

3. A method for preparing a traditional Chinese medicine composition for treating ulcerative colitis, characterized in that... Includes the following steps: Step 1: Weigh the following medicinal slices as raw materials according to the following weight proportions: Astragalus membranaceus 30-60 parts, Coptis chinensis 15-30 parts, Scutellaria baicalensis 15-30 parts, Bletilla striata 25-45 parts, Corydalis yanhusuo 15-30 parts, and Glycyrrhiza uralensis 20-35 parts; Step 2: Soak the raw materials in water equivalent to 9-11 times their weight, and decoct for 1-2 hours; filter, add water equivalent to 7-9 times their weight to the residue, and decoct for 0.5-1 hour; combine the filtrates, concentrate to 1 / 15-1 / 10 of the combined filtrate volume, add 2-5 parts by weight of indigo powder, mix well, and obtain a traditional Chinese medicine composition for treating ulcerative colitis.

4. The use of the traditional Chinese medicine composition of claim 1 in the preparation of a drug for treating ulcerative colitis.

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