Composition for alleviating chronic obstructive pulmonary disease and preparation method thereof

Abstract

The present invention belongs to the field of biomedicine technology, and specifically relates to a composition for alleviating chronic obstructive pulmonary disease and a preparation method thereof. The composition provided by the present invention is prepared from the following raw materials in parts by weight: 3-5 parts of patchouli, 1-3 parts of lavender, 1-2 parts of citrus peel, 1-2 parts of spearmint, and 1-2 parts of asarum. Furthermore, the above-mentioned raw materials are crushed and squeezed to obtain pressed oil. At the same time, the pressed residues are subjected to steam distillation, ethanol extraction and other operations to obtain extracts. The obtained pressed oil is combined with the extract and dehydrated to obtain the composition. In addition, in order to better achieve the efficacy of the above-mentioned composition in alleviating chronic obstructive pulmonary disease, it is compounded with an atomizing solvent to prepare an atomized liquid preparation. The obtained atomized liquid preparation shows a good improvement effect on chronic obstructive pulmonary disease.

Description

Technical Field

[0001] The present invention belongs to the technical field of biomedicine, and particularly relates to a composition for alleviating chronic obstructive pulmonary disease and a preparation method thereof. Background Art

[0002] Chronic obstructive pulmonary disease (COPD) is a common respiratory disease with a high incidence rate worldwide. Its main feature is that the lungs are affected by continuous airflow obstruction, which can cause chronic lung inflammation, excessive mucus secretion, airway remodeling, emphysema and many other problems, resulting in more serious lung diseases, with high disability and mortality rates. At present, the disease has become the third leading cause of death in the world, but it is also a preventable and remedial disease.

[0003] At present, oral chemical drugs are mostly used to alleviate and improve chronic obstructive pulmonary disease. Oral administration is simple and does not directly damage the skin or mucous membranes. It is painless and non-invasive. However, oral drugs are slow to take effect during the absorption process, and the efficacy is easily affected by gastrointestinal function and gastrointestinal contents. The bioavailability of the drug is low, and long-term use may also cause drug resistance. Therefore, the long-term treatment effect of oral drug treatment is not ideal.

[0004] To address the drawbacks of oral medications, existing research has begun formulating COPD medications into sprays, aerosols, or nasal drops for nasal delivery. For example, patent CN113694100A discloses a spray formulation for COPD. However, this patent utilizes supercritical carbon dioxide extraction technology to extract volatile oils from various raw materials, resulting in high costs and poor economic returns for industrial production. Summary of the Invention

[0005] In order to solve the above technical problems, the present invention provides a composition for alleviating chronic obstructive pulmonary disease and a preparation method thereof.

[0006] The first aspect of the present invention is to provide a composition for alleviating chronic obstructive pulmonary disease, wherein the composition is prepared from the following raw materials in parts by weight:

[0007] 3-5 parts of patchouli, 1-3 parts of lavender, 1-2 parts of citrus peel, 1-2 parts of spearmint, and 1-2 parts of asarum.

[0008] Preferably, 4 parts of patchouli, 2 parts of lavender, 2 parts of citrus peel, 1 part of spearmint, and 1 part of asarum.

[0009] As further preferred, the patchouli is patchouli leaves, the lavender is lavender flowers, the citrus peel is the dried peel of mature citrus, the spearmint is the stems and leaves of spearmint, and the asarum is the roots and stems of asarum.

[0010] Patchouli, according to the Chinese Pharmacopoeia, is "pungent and warm in nature, entering the spleen, stomach, and lung meridians. It has aromatic properties that clear turbidity, soothe the stomach and stop vomiting, and relieve heatstroke." Patchouli leaves are rich in volatile patchouli oil, primarily containing active ingredients such as patchoulene, patchouli alcohol, and patchouli ketone. These oils are effective for treating dampness and turbidity blocking the middle of the body, abdominal distension and vomiting, the initial onset of damp-heat syndrome, fever and fatigue, chest tightness and discomfort, cold-damp heat retention, abdominal pain, vomiting, diarrhea, and sinusitis and headache.

[0011] Lavender is pungent and cooling in nature. Research has shown that lavender essential oil, extracted from lavender, is rich in over 30 different aromatic compounds, including linalool, linalyl acetate, cineole, β-rosinene, lavandinyl acetate, lavandinol, terpenoid-4-ol, and camphor. The Chinese Materia Medica records that lavender has the effects of clearing heat and detoxifying, dispelling wind and relieving itching.

[0012] Citrus peel, also known as tangerine peel, noble old peel, or red peel, is bitter and pungent in nature and flavor, warming the spleen and lung meridians. Besides containing cellulose, lignin, and essential oils, citrus peel is also rich in pectin, flavonoids, and polyphenols, which have the effects of regulating qi, regulating the middle, drying dampness, and resolving phlegm.

[0013] Spearmint, also known as green mint, is pungent, slightly warm, and has antipyretic, soothing, and qi-regulating properties. The plant contains 0.6% to 0.7% of an aromatic oil, known as spearmint oil or spearmint oil. The main component is citronellal, which accounts for 60% to 65%. Other active ingredients include citronellal and citronellal. The "Compendium of Chinese Materia Medica" lists spearmint's main benefits as "mainly treating colds, coughs, headaches, sore throats, conjunctivitis, epistaxis, stomachaches, abdominal distension, vomiting and diarrhea caused by cholera, dysmenorrhea, limb numbness, swelling and pain from falls, sores, boils, and chapped skin."

[0014] Asarum, also known as Xiaoxin and Duyecao, is pungent and warm, and enters the Heart, Lung, and Kidney meridians. It has the effects of dispelling cold, expelling wind and relieving pain, opening the orifices, and warming the lungs and eliminating fluid. It is commonly used to treat colds, headaches, toothaches, nasal congestion and runny nose, sinusitis, rheumatic pain, phlegm and fluid, and coughs and wheezing.

[0015] The extract obtained by compounding the above ingredients has a good effect on alleviating COPD disease.

[0016] The second aspect of the present invention is to provide a method for preparing the above-mentioned composition for alleviating chronic obstructive pulmonary disease, comprising the following steps:

[0017] (1) Take 3-5 parts of patchouli leaves, 1-3 parts of lavender flowers, 1-3 parts of dried ripe citrus peels, 1-2 parts of spearmint stems and leaves, and 1-2 parts of asarum roots and stems, wash them separately and set aside;

[0018] (2) The raw materials in (1) are crushed and squeezed in a juicer to obtain the pressed oil of each raw material, which is then dehydrated and the pressed residues of each raw material are separated. (3) The pressed residues of each raw material separated in (2) are distilled and condensed using water vapor for 3 to 4 hours. The volatile components of each raw material are collected and the separated residues of each raw material after distillation are dried.

[0019] (4) adding ethanol to the dried residues of the raw materials in (3) for extraction, and collecting the ethanol extracts of the raw materials;

[0020] (5) The pressed oils of the raw materials obtained in (2), the volatile components of the raw materials obtained in (3), and the ethanol extracts of the raw materials obtained in (4) are combined, dried, and dehydrated to obtain extracts of the raw materials. The extracts of the raw materials are mixed uniformly to obtain the composition.

[0021] In the preparation method of the above-mentioned composition provided by the present invention, preferably, in (3), the water vapor temperature is 100°C and the distillation time is 4 hours.

[0022] Preferably, during the extraction in (4), the mass of ethanol added is 2 to 3 times the mass of the residue after drying, the extraction temperature is 40 to 50°C, and the extraction time is 0.5 to 2 h.

[0023] More preferably, during the extraction in (4), the mass of ethanol added is 2.5 times the mass of the residue after drying, the extraction temperature is 45°C, and the extraction time is 1 h.

[0024] Furthermore, the use of the above-mentioned composition in the preparation of an inhaled drug for relieving chronic obstructive pulmonary disease is also the technical content protected by the present invention.

[0025] Preferably, the drug is selected from any one of aerosol liquid, nasal spray, and nasal drops.

[0026] More preferably, the medicine is an aerosolized liquid.

[0027] As further preferred, the atomizing liquid at least includes an atomizing solvent and the above-mentioned composition, and the atomizing solvent is selected from at least one of glycerol and propylene glycol.

[0028] Preferably, in the atomized liquid, the composition is dissolved in the atomizing solvent at a mass percentage of 0.5% to 5%.

[0029] Furthermore, the method for using the atomized liquid is as follows:

[0030] The nebulized liquid is atomized by electronic heating atomization, with a heating temperature of 200~220℃, a single heating time of 2~4 s, a cooling time of 27~57 s, and a cycle operation; each time the nebulization is started, it lasts 30~60 minutes, 1~2 times a day, and is inhaled through the mouth and nose.

[0031] The beneficial effects of the present invention are:

[0032] (1) Provided is a Chinese medicine preparation composition for relieving chronic obstructive pulmonary disease, which uses patchouli, lavender, citrus peel, spearmint, and asarum as raw materials, and fully dissolves the active ingredients in each raw material by adopting a variety of different extraction methods. The active ingredients of each component in the obtained composition cooperate with each other to exert their effects, which not only has a good synergistic effect, but also has a low preparation and production cost and a high utilization rate;

[0033] (2) In the present invention, the obtained composition is prepared into an aerosolized liquid and administered by inhalation through the mouth and nose. Experimental results show that the aerosolized liquid can significantly reduce mucus secretion, improve airway airflow obstruction, alleviate lung inflammation, improve lung function, and effectively alleviate chronic obstructive pulmonary disease. BRIEF DESCRIPTION OF THE DRAWINGS

[0034] Figure 1 The effect of inhalation of aerosol solutions with different composition contents in Experimental Example 1 of the present invention on the levels of inflammatory factors in the alveolar lavage fluid of mice;

[0035] Figure 2 The lung function indicators FEV20 / FVC and FEV50 / FVC of mice after being treated with different amounts of the composition in Test Example 2 of the present invention;

[0036] Figure 3 The HE staining results of mouse lung tissue sections after inhalation of the aerosolized liquid of the composition at different contents in Experimental Example 3 of the present invention are shown;

[0037] Figure 4 The figures show the effects of treating mice with the compositions of different raw material ratios in Comparative Examples 1-8 of the present invention. DETAILED DESCRIPTION

[0038] In order to enable those skilled in the art to better understand the present invention, the present invention will be further explained in conjunction with specific embodiments.

[0039] Example 1

[0040] A composition for alleviating chronic obstructive pulmonary disease is prepared by the following method:

[0041] (1) Take the following raw materials in parts by weight: 4 parts of patchouli leaves, 2 parts of lavender flowers, 2 parts of dried ripe citrus peels, 1 part of spearmint stems and leaves, and 1 part of asarum root and stem, wash them clean and set aside;

[0042] (2) crushing each raw material in (1) and squeezing it in a juicer to obtain the pressed oil of each raw material, dehydrating it, and separating the pressed residue of each raw material;

[0043] (3) The pressed residues of the raw materials separated in (2) were distilled for 4 h using steam at 100°C, and the volatile components of the raw materials were collected respectively. The residues of the raw materials separated after distillation were dried under reduced pressure at 55°C;

[0044] (4) Add 2.5 times the mass of ethanol to the residue of each raw material after drying in (3), extract at 45°C for 1 hour, and collect the ethanol extract of each raw material;

[0045] (5) The pressed oils of the raw materials obtained in (2), the volatile components of the raw materials obtained in (3), and the ethanol extracts of the raw materials obtained in (4) are combined and dried to obtain extracts of the raw materials. The extracts of the raw materials are mixed uniformly to obtain the composition.

[0046] Example 2

[0047] The composition obtained in Example 1 was dissolved in glycerol at a mass percentage of 1.5% to form an atomized liquid.

[0048] The prepared atomized liquid was atomized by electronic heating atomization with a heating temperature of 220 °C, a single heating time of 3 s, a cooling time of 57 s, and a cyclic operation.

[0049] Example 3

[0050] The difference from Example 2 is that the mass percentage of the composition in the atomized liquid is 0.5%.

[0051] Example 4

[0052] The difference from Example 2 is that the mass percentage of the composition in the atomized liquid is 5%.

[0053] Test Example 1

[0054] Using C57BL / 6J model mice, different nebulized liquid inhalation doses were designed (the composition accounted for 0.5% in the low-dose group, 1.5% in the medium-dose group, and 5% in the high-dose group), once a day for 1 hour each time. The mice were divided into five groups: blank group (NOR), modeling group (CS), high-dose group (EO-H), medium-dose group (EO-M), and low-dose group (EO-L). After 80 days of inhalation, the inflammatory factors in the alveolar lavage fluid of each group of mice were examined. The results are shown in the attached figure. Figure 1 shown.

[0055] By the attached Figure 1 It can be seen that by measuring the inflammatory factors IL-1β, TNF-α, and IL-6 in the alveolar lavage fluid of mice, the results showed that compared with the blank group, the content of inflammatory factors in the alveolar lavage fluid of mice in the modeling group was significantly increased, and the content of inflammatory factors in the alveolar lavage fluid of mice was significantly decreased after treatment with high, medium, and low doses of the composition. It can be seen that the composition has a reducing effect on the increase of inflammatory factors in the lungs of mice and can alleviate COPD symptoms.

[0056] Test Example 2

[0057] C57BL / 6J model mice were used to design different nebulized liquid inhalation doses (the composition accounted for 0.5% in the low-dose group, 1.5% in the medium-dose group, and 5% in the high-dose group), once a day for 1 hour each time. The mice were divided into five groups, namely, blank group (NOR), modeling group (CS), high-dose group (EO-H), medium-dose group (EO-M) and low-dose group (EO-L). After 80 days of inhalation, the lung function indicators FEV20 / FVC (%) and FEV50 / FVC (%) of the mice in each group were examined. The measurement results are shown in the attached figure. Figure 2 shown.

[0058] By the attached Figure 2 As can be seen, through the measurement of the lung function indicators FEV20 / FVC and FEV50 / FVC of mice, the results showed that the lung function of the modeling group was significantly reduced compared with the blank group, indicating that the modeling was successful. The primary indicator for evaluating COPD disease, FEV20 / FVC, was significantly improved after treatment with the composition, and the low-dose group had a better therapeutic effect than the high-dose group. FEV50 / FVC also recovered after treatment with the composition, indicating that the composition has a certain effect on improving the lung function of mice and can alleviate COPD symptoms.

[0059] Test Example 3

[0060] Using C57BL / 6J model mice, different nebulized liquid inhalation doses were designed (the composition accounted for 0.5% in the low-dose group, 1.5% in the medium-dose group, and 5% in the high-dose group), once a day for 1 hour each time. A total of six groups were divided into blank group, modeling group, blank solvent group (blank solvent refers to the nebulized liquid solvent, in order to prove that the solvent itself has no biological activity), high-dose group, medium-dose group and low-dose group. After 80 days of inhalation, the lung tissue pathology sections of mice in each group were stained. The results are shown in the attached figure. Figure 3 shown.

[0061] Attachment Figure 3 The results of lung tissue pathological section staining showed that compared with the blank group, the alveolar cavity structure of the modeling group was disordered, the alveolar wall was significantly thickened, and there was a large amount of inflammatory infiltration; the characteristics of the solvent group were similar to those of the modeling group, proving that the solvent had no therapeutic effect on mice; after treatment with the composition, the area of ​​inflammatory infiltration was reduced to varying degrees, the alveolar wall became thinner, and the morphology of the alveolar cavity gradually recovered, and the treatment effect of the low-dose group was better than that of the high-dose group. It can be seen that the composition provided by the present invention has a significant improvement effect on alleviating chronic obstructive pulmonary disease.

[0062] On the basis of the above embodiments, the inventors also conducted the following experiments:

[0063] Comparative Examples 1-8 differ from Example 1 in that the proportions of the components in the compositions of the comparative examples are different, as shown in Table 1 below.

[0064] Table 1 Ratios of ingredients in the compositions of Comparative Examples 1-8

[0065] Experimental group Patchouli Lavender citrus peels Spearmint Asarum Comparative Example 1 2 4 2 1 1 Comparative Example 2 1 4 1 2 2 Comparative Example 3 2 2 4 1 1 Comparative Example 4 1 1 4 2 2 Comparative Example 5 2 2 1 4 1 Comparative Example 6 1 1 2 4 2 Comparative Example 7 2 2 1 1 4 Comparative Example 8 1 1 2 2 4

[0066] After the above-mentioned comparative examples were used for treatment, the experimental results are shown in the attached Figure 4 As shown, there was no significant difference in the lung function index FEV20 / FVC of mice compared with the modeling group.

[0067] Comparative Example 9

[0068] The difference from Example 1 is that only the preparation process of the composition is adjusted, and the specific operations are as follows:

[0069] Patchouli leaves, lavender flowers, dried and mature citrus peels, spearmint stems and leaves, and asarum roots and stems are taken in formulated amounts, crushed separately, and then pressed in a juicer to obtain pressed oils of the raw materials, which are then dehydrated to obtain extracts.

[0070] Comparative Example 10

[0071] The difference from Example 1 is that only the preparation process of the composition is adjusted, and the specific operations are as follows:

[0072] Patchouli leaves, lavender flowers, dried ripe citrus peels, spearmint stems and leaves, and asarum roots and stems are taken in a formulated amount, crushed separately, and then pressed in a juicer to obtain pressed oil from each raw material, which is then dehydrated.

[0073] At the same time, the separated raw material pressing residue was distilled and condensed for 4 hours using steam distillation and condensation method to collect volatile components; the pressed oil and volatile components were combined and dried to obtain the extract.

[0074] The experimental results show that the extraction effect of the method of Comparative Examples 9-10 is poor, it is difficult to obtain the complete active ingredients in each component, and the purity of the obtained extract is not high, and the effect is poor.

Claims

1. A composition for alleviating chronic obstructive pulmonary disease, characterized in that: The composition is prepared from the following raw materials in parts by weight: 3-5 parts of patchouli, 1-3 parts of lavender, 1-3 parts of citrus peel, 1-2 parts of spearmint, and 1-2 parts of asarum, wherein the patchouli is patchouli leaves, the lavender is lavender flowers, the citrus peel is the dried peel of mature citrus, the spearmint is the stems and leaves of spearmint, and the asarum is the roots and stems of asarum; The method for preparing the composition comprises the following steps: (1) Take 3-5 parts of patchouli leaves, 1-3 parts of lavender flowers, 1-3 parts of dried ripe citrus peels, 1-2 parts of spearmint stems and leaves, and 1-2 parts of asarum roots and stems, wash them separately and set aside; (2) crushing each raw material in step (1) and placing it in a juicer for squeezing to obtain the pressed oil of each raw material, dehydrating it, and separating the pressed residue of each raw material; (3) using steam to distill and condense the pressed residues of the raw materials separated in step (2), with the distillation time being 3 to 4 hours, collecting the volatile components of the raw materials respectively, and drying the residues of the raw materials separated after distillation; (4) adding ethanol to the dried residues of each raw material in step (3) for extraction, and collecting the ethanol extracts of each raw material; (5) The pressed oil of each raw material obtained in step (2), the volatile components of each raw material obtained in step (3), and the ethanol extract of each raw material obtained in step (4) are combined, dried and dehydrated to obtain the extract of each raw material, and the extracts of each raw material are mixed uniformly to obtain the composition.

2. The composition according to claim 1, wherein In step (4), during extraction, the mass of ethanol added is 2 to 3 times the mass of the residue after drying, the extraction temperature is 40 to 50°C, and the extraction time is 0.5 to 2 h.

3. Use of the composition according to claim 1 in the preparation of an inhaled medicament for relieving chronic obstructive pulmonary disease.

4. The use according to claim 3, characterized in that The medicine is selected from any one of aerosol liquid, nasal spray, and nasal drops.

5. The use according to claim 4, characterized in that The medicine is an aerosolized liquid.

6. The use according to claim 5, characterized in that The atomizing liquid at least comprises an atomizing solvent and the composition according to claim 1, and the atomizing solvent is selected from at least one of glycerol and propylene glycol.

7. The use according to claim 6, characterized in that In the atomized liquid, the composition is dissolved in the atomizing solvent at a mass percentage of 0.5% to 5%.

8. The use according to claim 5, characterized in that The method of using the atomized liquid is as follows: The nebulized liquid is atomized by electronic heating atomization, with a heating temperature of 200~220℃, a single heating time of 2~4 s, a cooling time of 27~57 s, and a cycle operation; each time the nebulization is started, it lasts 30~60 minutes, 1~2 times a day, and is inhaled through the mouth and nose.

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