A traditional Chinese medicine composition for treating lung heat, its preparation method, and its application.

Abstract

This invention belongs to the field of traditional Chinese medicine compositions, specifically relating to a traditional Chinese medicine composition for treating lung heat, its preparation method, and its application. The Xiebai Powder provided by this invention is composed of the following ingredients: Lycium chinense root bark, stir-fried mulberry bark, stir-fried licorice root, japonica rice, pickled apricot kernels, and Pinellia ternata. The formula provided by this invention is both clearing and moistening, purging while also tonifying, and tonifying while dispersing. The addition of pickled apricot kernels and Pinellia ternata makes it more suitable for the immature Yin and Yang constitution of children, addressing both cough and diarrhea symptoms, thus balancing the root cause and the symptoms. It aligns with the characteristics of the lungs being a delicate organ, intolerant to cold and heat, and children's weak spleen and stomach, making them prone to diarrhea and cough, thereby shortening the course of the disease and improving efficacy.

Description

Technical Field

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

[0002] Cough is a common lung disease in clinical practice, and its causes are quite complex. In recent years, due to the continuous improvement of people's living standards, parental pampering, improper feeding, and children's diets often consisting of rich and greasy foods, children are prone to spleen and stomach dysfunction. In addition, changes in environmental factors have led to a significant increase in cases of lung heat cough in children in clinical practice.

[0003] Xiebai Powder is a traditional Chinese medicine formula originating from the Song Dynasty text *Xiao'er Yaozheng Zhijue*. It belongs to the category of heat-clearing agents that clear heat from the internal organs. Composed of mulberry bark, lycium bark, japonica rice, and licorice, it clears lung heat, relieves cough and asthma, and is primarily used to treat lung heat with cough and wheezing, characterized by wheezing, hot skin, red tongue with yellow coating, etc. Clinically, it is often used for early-stage measles, pneumonia, and bronchitis in children with latent heat in the lungs. The formula uses mulberry bark as the principal ingredient to clear lung heat, lycium bark as the assistant ingredient to reduce latent heat, and japonica rice and licorice as adjuvant ingredients to harmonize the spleen and stomach. Its combination is both cooling and moistening, targeting latent heat in the lungs rather than actual heat or yin deficiency. However, in current technology, Xiebai Powder is considered too cold in nature, limiting its applicability. During use, it can easily worsen diarrhea, leading to loss of appetite, loose stools, and abdominal pain in children. Summary of the Invention

[0004] To address the problems existing in the prior art, the present invention provides an improved traditional Chinese medicine composition for treating lung heat. The composition provided by the present invention, as an improved Xiebai powder, can effectively improve lung heat cough and wheezing, and also has the effect of stopping diarrhea.

[0005] The present invention also provides a method for preparing the above-mentioned traditional Chinese medicine composition.

[0006] The present invention also provides the application of the above-mentioned traditional Chinese medicine composition in the preparation of a medicine for treating lung heat and cough.

[0007] The technical solution adopted by the present invention to achieve the above objectives is as follows: This invention provides a traditional Chinese medicine composition for treating lung heat, which is composed of the following raw materials by weight: 8-10g of Lycium chinense root bark, 8-10g of stir-fried mulberry bark, 0.8-1g of stir-fried licorice root, 6-6.5g of japonica rice, 0.2-0.6g of sour-soaked apricot kernels, and 3-5g of Pinellia ternata.

[0008] Most preferably, the traditional Chinese medicine composition for treating lung heat is composed of the following ingredients by weight: 8.86g of Lycium chinense root bark, 8.86g of stir-fried mulberry bark, 0.89g of stir-fried licorice root, 6g of japonica rice, 0.25g of sour-soaked almond, and 3.85g of Pinellia ternata.

[0009] The acid-soaked almonds used in this invention are prepared by the following method: First, soak the almonds in saturated lime water for 20-24 hours, then take them out and soak them in acetic acid for 48-50 hours, then wash and dry them.

[0010] The present invention also provides a method for preparing the above-mentioned traditional Chinese medicine composition for treating lung heat, comprising the following steps: mixing the raw materials, grinding them into powder, and then adding water for decoction.

[0011] Preferably, the mass ratio of the total weight of the raw materials to water is 1:8-10.

[0012] Preferably, the liquid is simmered until it is 0.5-0.6 times the original amount of water added.

[0013] The present invention also provides the application of the above-mentioned traditional Chinese medicine composition in the preparation of a medicine for treating lung heat and cough.

[0014] The present invention further provides the application of the above-mentioned traditional Chinese medicine composition in the preparation of a drug for treating pediatric diarrhea.

[0015] In the formula provided by this invention, mulberry bark is sweet and cold in nature, and specifically enters the lung meridian. It is used as the chief ingredient. Its bark can promote the flow of qi, and its white color can return to the lungs. Its sweet and cold nature can both enter the lungs and clear heat. Moreover, its root penetrates the soil the deepest, and can clear and descend. Lycium bark penetrates deep into the lower body and is used as the assistant ingredient. Its sweet and cold nature can help the chief ingredient to purge the latent fire in the lungs. It can also enter the liver and kidneys, cool the blood and remove steaming heat. The use of the two barks is to descend lung qi. When lung qi descends, the fire will naturally disappear. Adding sourly soaked almonds, slightly astringent and warm in nature without being drying, enters the lung and large intestine meridians. As an adjuvant, it assists mulberry bark and lycium bark in astringing the lungs, stopping coughs, lowering qi, and relieving asthma, enhancing the cough-suppressing effect. It also astringes the intestines without causing diarrhea, thus stopping diarrhea, suitable for children with cough and diarrhea. Its warm nature also mitigates the coldness of mulberry and lycium bark, preventing damage to the spleen and stomach. Adding pinellia, pungent and warm in nature, enters the spleen, stomach, and lung meridians, also as an adjuvant. Its pungent and warm properties resolve phlegm, lower rebellious qi, and stop coughs, targeting qi stagnation and phlegm production. It assists the principal and assistant herbs in resolving phlegm and calming coughs. Pinellia also harmonizes the stomach, lowers rebellious qi, dries dampness, and stops diarrhea, alleviating diarrhea caused by impaired lung function and spleen-stomach disharmony. Combined with sourly soaked almonds, the astringent and resolving properties double the cough-suppressing and diarrhea-stopping effects, while also protecting the spleen and stomach, preventing cold-induced lung damage. Prepared licorice root and japonica rice nourish the stomach and harmonize the middle jiao to support lung qi, serving as adjuvants. When these six herbs are used together, they form a formula for purging white heat. This formula has the characteristics of clearing heat without harming yin, purging the lungs without harming the body's vital energy, stopping coughs without causing diarrhea, and stopping diarrhea without causing stagnation of qi. Together, they achieve the effects of clearing lung heat, relieving stagnation of qi and promoting appetite, stopping coughs and relieving asthma, and astringing the intestines to stop diarrhea.

[0016] The beneficial effects of this invention are as follows: The formula provided by this invention is both clearing and moisturizing, purging and tonifying, and tonifying while dispersing. After adding sour-soaked almonds and pinellia, it is more suitable for the immature yin and yang of children, and takes into account both cough and diarrhea. It addresses both the root cause and the symptoms, and is consistent with the characteristics of the lungs being a delicate organ that is intolerant to cold and heat, and the weak spleen and stomach of children, which makes them prone to diarrhea and cough. This shortens the course of the disease and improves the efficacy. Attached Figure Description

[0017] Figure 1 A comparison of IL-1β levels in bronchoalveolar lavage fluid from different groups of mice; Figure 2 A comparison of IL-6 levels in bronchoalveolar lavage fluid from different groups of mice; Figure 3 A comparison of IL-10 levels in bronchoalveolar lavage fluid from different groups of mice; Figure 4 A comparison of TNF-α levels in bronchoalveolar lavage fluid from different groups of mice; Figure 5 Image of the actual sample of Xiebai Powder; Figure 6 Characteristic spectra of 20 batches of reference samples; Figure 7 Thin-layer chromatography identification diagram of Xiebai Powder (mulberry bark); Figure 8 Thin-layer identification diagram of Xiebai Powder (Digupi). Detailed Implementation

[0018] The technical solution of the present invention will be further explained and described below through specific embodiments.

[0019] The almonds used in this invention are bitter almonds (northern almonds).

[0020] Example 1 The formula is as follows: 8.86g of Lycium chinense root bark, 8.86g of stir-fried mulberry bark, 0.89g of stir-fried licorice root, 6g of japonica rice, 0.25g of sourly soaked almonds, and 3.85g of Pinellia ternata.

[0021] The preparation method is as follows: (1) Soak almonds in saturated lime water for 24 hours, then soak them in acetic acid (50% by volume) for 48 hours, wash them and dry them to obtain acid-soaked almonds. (2) Grind the raw materials by weight into coarse powder, then add 300mL of water and boil down to 180mL.

[0022] Comparative Example 1 The formula is as follows: 8.86g of Lycium chinense root bark, 8.86g of stir-fried mulberry bark, 0.89g of stir-fried licorice root, and 6g of japonica rice.

[0023] The preparation method is as follows: Grind the raw materials in parts by weight into coarse powder, then add 300mL of water and boil down to 180mL.

[0024] Comparative Example 2 The formula is as follows: 8.86g of Lycium chinense root bark, 8.86g of stir-fried mulberry bark, 0.89g of stir-fried licorice root, 6g of japonica rice, 0.25g of apricot kernel, and 3.85g of Pinellia ternata.

[0025] The preparation method is as follows: (1) Grind the raw materials by weight into coarse powder, then add 300mL of water and boil down to 180mL.

[0026] Effect Verification (Part 1) (1) Establishment of animal models SPF-grade male Wistar rats (200-250g), 6-8 weeks old, were purchased from Beijing Vital River Laboratory Animal Technology Co., Ltd. They were free from respiratory diseases and abnormal weight fluctuations, and were acclimatized for 5 days. They were given standard feed and sterilized purified water daily, and the ambient temperature was maintained at (22±2)℃, relative humidity at (55±5)%, with a 12h light / 12h dark cycle. They had free access to food and water.

[0027] Rats in the model group were intraperitoneally injected with a sensitizing solution (2 mg OVA dissolved in 1 ml of physiological saline, with an appropriate amount of alum adjuvant added and mixed well). The normal control group was injected with an equal volume of physiological saline and alum adjuvant. After sensitization, rats were kept still for 3 days to ensure full absorption of the sensitizing solution. Three days after sensitization, nebulization challenge began. Rats in the model group were placed in animal restraints within a negative pressure fume hood and continuously inhaled a 1.25% OVA physiological saline suspension via an ultrasonic nebulizer for 15 minutes each time, three times a week (Monday, Wednesday, and Friday), for three consecutive weeks. The normal control group inhaled an equal volume of physiological saline using the same method, with challenge conditions identical to the model group. During the modeling period, the rats' mental state, respiration, diet, and activity levels were observed daily. Symptoms such as rapid breathing, wheezing, and coughing were recorded. Rats were weighed regularly. If any rats died or showed severe discomfort, they were promptly removed and replaced to ensure a stable sample size for each group.

[0028] Continue until the rat exhibits signs of agitation, itchy nose scratching, head shaking, licking limbs, sneezing, or rapid breathing, irregular head nodding, or abdominal breathing, until the rat begins to show symptoms such as difficulty breathing or abdominal muscle spasms.

[0029] Administration method (10 animals per group): Model control group (mod): During the modeling period, normal saline was administered by gavage 1 hour before modeling each day instead of the drug dosage; Positive control group (dex): During the modeling period, dexamethasone was administered by gavage at a dose of 0.4 mg / kg 1 hour before modeling every day; Xiebai Powder S1 group: During the modeling period, Xiebai Powder decoction prepared in Example 1 was administered at a dose of 0.4 mg / kg and 6 g of raw drug / kg 1 hour before modeling each day; Xiebai Powder D1 group: During the modeling period, Xiebai Powder decoction prepared in Comparative Example 1 was administered at a dose of 0.4 mg / kg and 6 g of crude drug / kg 1 hour before modeling each day; Xiebai Powder D2 group: During the modeling period, Xiebai Powder decoction prepared in Comparative Example 2 was administered at a dose of 0.4 mg / kg and 6 g of raw drug / kg for 1 hour before modeling each day.

[0030] (2) Sample testing I. Bronchoalveolar lavage fluid: On the evening of day 20, rats in each group were fasted for 12 hours but allowed free access to water. Then, they were anesthetized by intraperitoneal injection of 10% chloral hydrate (3 mg / kg), fixed, and the thoracic cavity was opened and exposed. The right lung lobe of the first 5 rats in each group was ligated. The left lung was then lavaged with PBS solution 3 times, about 1 mL each time. After each lavage, the rats were allowed to equilibrate for 40 seconds. The lavage fluid was then combined into a 5 mL centrifuge tube.

[0031] The obtained bronchoalveolar lavage fluid was centrifuged for 15 min (4℃, 3000 rpm), and the supernatant was transferred to centrifuge tubes. The concentrations of IL-1β, IL-6, IL-10, and TNF-α in the bronchoalveolar lavage fluid were determined using ELISA. Simultaneously, images of the cell pellet were taken, air-dried, and stained with Wright-Giemsa to detect eosinophils (Eos), macrophages (AM), and neutrophils (Neu). Specific results are shown in Table 1. The concentrations of IL-1β, IL-6, IL-10, and TNF-α in the bronchoalveolar lavage fluid of each group of rats were measured. Figures 1-4 As can be seen, compared with the positive control group, the concentrations of pro-inflammatory cytokines (IL-1β, IL-6, TNF-α) in the model group were increased, while the concentration of the dissipating factor IL-10 was decreased, confirming that inflammation did occur in the lungs of the heat-induced asthma rats. The Xiebai powder provided by this invention can effectively inhibit the secretion of IL-1β, IL-6, and TNF-α in heat-induced asthma rats, regulating the concentrations of pro-inflammatory cytokines back to a certain level; it also significantly increases the concentration of IL-10. Therefore, the Xiebai powder provided by this invention demonstrates a strong ability to reduce inflammation by decreasing pro-inflammatory cytokines and increasing the release of the dissipating factor.

[0032] Table 1 As shown in Table 2, in the OVA-induced mouse model, the levels of eosinophils (Eos), macrophages (AM), and neutrophils (Neu) in the BALF of the model group (Mod) mice were significantly increased, indicating a markedly enhanced airway inflammatory response. Compared with the model group, all Xiebaisan treatment groups and the dexamethasone (dex) positive control group reduced the number of inflammatory cells. The Xiebaisan prepared by this invention using a specific process reduced the levels of Eos, AM, and Neu to 0.35±0.08, 1.37±0.09, and 0.32±0.11×10⁻⁶, respectively. 5 / mL, which is similar to the improvement effect of the dexamethasone group. This result indicates that the Xiebai powder prepared in this invention can effectively relieve OVA-induced airway inflammation in asthma by inhibiting the recruitment of airway eosinophils, macrophages and neutrophils. (3) During the administration period, the incidence of diarrhea in each group was compared, and the specific results are shown in Table 2.

[0033] Table 2 Example 2 (a) Take the following ingredients, crushed into coarse particles: 26.58g of Lycium chinense root bark, 26.58g of stir-fried mulberry bark, 2.67g of stir-fried licorice root, 18g of japonica rice, 0.75g of sour-soaked apricot kernels, and 11.55g of Pinellia ternata. Add 2700 mL of water. First, heat the mixture to boiling point at 2000W (about 18 minutes), then reduce to 1000W and continue to simmer for 35 minutes to obtain the decoction. Filter the decoction while hot and bring the volume to 1620 mL. Then, freeze-dry the mixture using a freeze-drying instrument (T<-40℃, Vac<20Pa) for about 48 hours to obtain the freeze-dried powder, which is the reference sample.

[0034] The basic morphology of the prepared Xiebaisan reference sample is as follows: Figure 5 As shown, it is a light yellow to brownish-yellow powder with a rice aroma and a slightly sweet taste. It is packaged in a white, transparent resealable bag and stored in an electronic desiccant box under the following conditions: temperature 25℃, humidity 10%.

[0035] (II) Content determination This invention aims to establish a method for determining the content of mulberry bark glycoside A, lycopene, glycyrrhizin, and glycyrrhizic acid in a reference sample of Xiebai powder.

[0036] 1. Chromatographic conditions for content determination Chromatographic column: Agilent Poroshell 120 SB-C18 150×4.6mm, 4μm; column temperature: 30℃; aqueous phase A: 0.1% trifluoroacetic acid; organic phase B: acetonitrile; detection wavelength: 216 nm / 250 nm; gradient elution was performed according to the specifications in Table 3 above, with a flow rate of 1.0 mL per minute.

[0037] Table 3 The extraction method for determining the content of Xiebaisan (water decoction) is as follows: accurately transfer 15mL of Xiebaisan water decoction into a 50mL volumetric flask, accurately add 10mL of purified water, add about 20mL of methanol solution containing 1.0% acetic acid, sonicate for 10 minutes, cool, dilute to the mark with methanol solution containing 1.0% acetic acid, shake well, filter, and take the filtrate.

[0038] The extraction method for determining the content of Xiebaisan reference sample (lyophilized powder) is as follows: Take about 0.5g of Xiebaisan reference sample, accurately weigh it, accurately add 50mL of 50% methanol solution containing 0.5% acetic acid, seal tightly, weigh, sonicate for 30 minutes, cool, weigh again, replenish the lost weight with 50% methanol solution containing 0.5% acetic acid, shake well, filter, and take the filtrate.

[0039] The content of 20 batches of reference samples was determined, and the results are shown in Table 4.

[0040] Table 4. Content of each dose (mg / dose) of the reference components of 20 batches of Xiebai Powder After testing, the fingerprint similarity of 20 batches of reference samples was compared using the "Traditional Chinese Medicine Chromatographic Fingerprint Similarity Evaluation System" software. For example... Figure 6 As shown in the results: comparative analysis of 15 common peaks in 20 batches of reference samples showed that the matching degree between each peak was greater than 95%, indicating that the fingerprint spectrum similarity of the 20 batches of reference samples was good.

[0041] (III) Quality Study of Xiebai Powder Using mulberry bark and lycium bark as research subjects: (1) Thin-layer identification of mulberry bark Preparation of test sample and reference medicinal material solution: Take 0.5g of mulberry bark reference medicinal material powder, 1.0g of Xiebai powder reference sample, and 1.0g of negative lyophilized powder, add 20mL of anhydrous ethanol to each, sonicate for 40min, filter, evaporate the filtrate to dryness, and dissolve the residue in 2mL of anhydrous ethanol to obtain the test sample and reference medicinal material solution.

[0042] Thin-layer chromatography identification method for mulberry bark: Apply 2-3 μL of mulberry bark reference solution, 5-6 μL each of Xiebai powder and mulberry bark negative test solution to the same silica gel G thin-layer plate. Develop to 10 cm using petroleum ether-toluene-chloroform (2:1:2) as the developing solvent. Remove, air dry, spray with 10% sulfuric acid ethanol solution, and heat at 105℃ until the spots are clearly visible. Examine under sunlight. In the chromatogram of the test sample, spots of the same color appear at the corresponding positions as in the chromatogram of the reference material; negative samples show no interference. Figure 7 ).

[0043] (2) Identification of thin layers of Lycium bark Take 0.5g of Lycium chinense root bark reference powder, 1.0g of Xiebai powder, and 1.0g of negative lyophilized powder. Add 20mL of methanol to each, sonicate for 30min, filter, evaporate the filtrate to dryness, and dissolve the residue in 1mL of methanol to prepare the test solution. Perform thin-layer chromatography (General Chapter 0502, Chinese Pharmacopoeia 2020 Edition). Apply 5μL of the test solution to the same silica gel G thin-layer plate, using toluene-acetone-formic acid (10:1:0.1) as the developing solvent. Develop, remove, air dry, and examine under ultraviolet light (365nm). In the chromatogram of the test sample, fluorescent spots of the same color appear at the corresponding positions as in the chromatogram of the reference medicinal material. See the thin-layer chromatogram below. Figure 8 .

Claims

1. A traditional Chinese medicine composition for treating lung heat, characterized in that, The ingredients are composed of the following ingredients by weight: 8-10g of Lycium chinense root bark, 8-10g of stir-fried mulberry bark, 0.8-1g of stir-fried licorice root, 6-6.5g of japonica rice, 0.2-0.6g of sourly soaked almonds, and 3-5g of Pinellia ternata.

2. The pediatric purgative powder according to claim 1, characterized in that, The ingredients are composed of the following ingredients by weight: 8.86g of Lycium chinense root bark, 8.86g of stir-fried mulberry bark, 0.89g of stir-fried licorice root, 6g of japonica rice, 0.25g of sourly soaked almonds, and 3.85g of Pinellia ternata.

3. The traditional Chinese medicine composition according to claim 1 or 2, characterized in that, The acid-soaked almonds are prepared by the following method: First, soak the almonds in saturated lime water for 20-24 hours, then take them out and soak them in acetic acid for 48-50 hours. After washing, they are dried.

4. A method for preparing a traditional Chinese medicine composition according to any one of claims 1-3, characterized in that, Includes the following steps: After mixing the ingredients, grind them into powder, then add water and boil.

5. The preparation method according to claim 4, characterized in that, The mass ratio of the total weight of the raw materials to water is 1:8-10.

6. The preparation method according to claim 4 or 5, characterized in that, Simmer until the volume of water increases to 0.5-0.6 times the original volume.

7. The use of a traditional Chinese medicine composition as described in any one of claims 1-3 in the preparation of a medicine for treating lung heat and cough.

8. The use of a traditional Chinese medicine composition as described in any one of claims 1-3 in the preparation of a drug for treating pediatric diarrhea.

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