Agilawood cough-relieving atomized composition and preparation method thereof

Through the reasonable proportioning and preparation method of agarwood, honeysuckle and isatis root extracts, an effective agarwood cough-relieving atomization composition was prepared, which solved the shortcomings of atomization inhalation in the prior art to relieve cough, and achieved rapid and uniform drug distribution and Significant cough relieving effect.

CN119174795APending Publication Date: 2024-12-24HAINAN DAGUAN AGARWOOD IND DEV CO LTD
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Patent Information

Application Number
CN202411428932.6
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-10-14
Publication Date
2024-12-24

AI Technical Summary

Technical Problem

The prior art is difficult to effectively relieve cough symptoms through atomization and inhalation, especially cough caused by dryness, and the distribution of drugs in the respiratory tract is uneven, making it difficult to play a role quickly.

Method used

The agarwood cough atomization composition is prepared by distillation, ultrasonic extraction and water decoction and other methods, and filtered and concentrated through a polyether sulfone filter membrane to form suitable Drop size and concentration ensures retention of active ingredients and rapid inhalation.

Benefits of technology

This method can quickly moisturize the respiratory tract, dilute sputum, reduce inflammatory reactions, speed up sputum removal, significantly relieve cough symptoms, and tests show that the finished product is prolonged in blood drug concentration and drug concentration in lung tissue, improving cough relieving effect.

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Abstract

The invention relates to a preparation method of an agilawood cough-relieving atomized composition which is prepared from the following raw materials in parts by weight: 10-13 parts of an agilawood extract, 15-20 parts of a honeysuckle flower extract and 6-10 parts of a radix isatidis extract. The raw materials are reasonable in proportion, the respiratory mucosa can be rapidly wetted, the cough symptom caused by dryness can be relieved, sputum can be diluted, and sputum coughing can be promoted. Effective components in the agilawood extract, the honeysuckle flower extract and the isatis root extract not only have an anti-inflammatory effect and can relieve inflammatory response of respiratory mucosa so as to relieve cough, but also have the effects of promoting movement of respiratory cilia and accelerating the clearing speed of sputum.
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Description

Technical Field

[0001] The invention belongs to the field of pharmaceutical preparations and relates to a method for preparing an agarwood cough-relieving atomization composition. Background Art

[0002] Agarwood is a solid condensate mixed with gum, resin, volatile oil, wood and other ingredients. It is a crystal formed by the external pathological changes of the agarwood tree. Agarwood has many pharmacological effects, such as inhibiting gastrointestinal motility, promoting secretion of digestive juices, promoting bile secretion, relieving asthma, anesthesia, analgesia, antibacterial, lowering blood pressure, and inhibiting the central nervous system.

[0003] Aerosol inhalation generally refers to inhaling drug particles into the airway or lungs by atomization, which allows the drug to be absorbed through the mucous membrane and act locally. The efficacy of atomization varies depending on the drug. In order to improve the effect of atomization inhalation in improving cough, a method for preparing an agarwood cough relieving atomization composition is proposed. Summary of the invention

[0004] In view of this, the present invention discloses a method for preparing an agarwood cough relieving atomization composition to solve the above problems.

[0005] The technical solution of the present invention is achieved in this way:

[0006] An agarwood cough relieving aerosol composition, wherein the raw materials include 10-13 parts of agarwood extract, 15-20 parts of honeysuckle extract and 6-10 parts of isatis root extract by weight.

[0007] Furthermore, the method for preparing the agarwood extract comprises the following steps:

[0008] (1) crushing agarwood, adding it into a distillation kettle, heating it to 70-80° C. for the first time, and heating it to 170-180° C. for the second time to obtain a distillate;

[0009] (2) Cooling the distillate and removing the upper essential oil to obtain the agarwood extract.

[0010] Furthermore, the preparation method of the honeysuckle extract comprises the following steps:

[0011] S1: crushing honeysuckle to obtain honeysuckle powder;

[0012] S2: Mix honeysuckle powder and water, add complex enzyme, and perform ultrasonic extraction to obtain honeysuckle extract.

[0013] Furthermore, the Radix Isatidis extract is prepared by decocting in water.

[0014] Furthermore, in step (1), the first heating and insulation time is 30-50 minutes, and the second heating and insulation time is 2-4 hours.

[0015] 6 Further, in step S2, the mass ratio of the honeysuckle powder to water is 1:5-10, the complex enzyme includes β-glucanase and cellulase in a mass ratio of 1:2-2.5, and 5-8% of the complex enzyme is added according to the honeysuckle powder.

[0016] Furthermore, in step S2, the pH value of the honeysuckle powder and water is adjusted to 4-5 after mixing, and ultrasonic extraction is performed at 200-400W for 10-20min at a temperature of 20-40°C.

[0017] Furthermore, the water decoction is a first water decoction in which 7-10 times the amount of water is added according to the mass of the Isatis root and the decoction is performed for 1-2 hours, and a second water decoction in which 3-5 times the amount of water is added according to the mass of the Isatis root and the decoction is performed for 15-25 minutes.

[0018] Furthermore, the preparation method of the agarwood cough relieving aerosol composition comprises the following steps:

[0019] C1: mixing the agarwood extract, honeysuckle extract and isatis root extract, and filtering with a polyethersulfone filter membrane to obtain a filtrate;

[0020] C2: The filtrate is concentrated to 25-35% of the original volume to obtain the finished product.

[0021] Furthermore, the concentration temperature is 60-80°C.

[0022] Compared with the prior art, the present invention has the following beneficial effects:

[0023] In the present invention, the raw materials include 10-13 parts of agarwood extract, 15-20 parts of honeysuckle extract and 6-10 parts of isatis root extract by weight. The raw materials in the present invention are reasonably proportioned, which can not only quickly moisten the respiratory mucosa, relieve the cough symptoms caused by dryness, but also dilute sputum and promote sputum coughing. The effective ingredients in agarwood extract, honeysuckle extract and isatis root extract not only have anti-inflammatory effects, can reduce the inflammatory response of the respiratory mucosa, thereby relieving cough, but also promote the movement of respiratory cilia and accelerate the clearance of sputum.

[0024] The raw material extraction method of the present invention can dissolve the effective components in the raw materials in a solvent without destroying the effective components.

[0025] The agarwood cough-relieving atomization composition of the present invention uses a polyethersulfone filter membrane to filter out large impurities in the extraction process, avoiding the formation of large water droplets that cause choking when used. The filtrate is concentrated to 25-35% of the original volume, which can retain the effective ingredients in the composition, control the effective concentration of the finished product, form droplets of appropriate size when used, can quickly and accurately adhere to the respiratory tract, and quickly exert the effect of the physical and chemical composition. DETAILED DESCRIPTION

[0026] In order to better understand the technical content of the present invention, specific embodiments are provided below to further illustrate the present invention.

[0027] Unless otherwise specified, the experimental methods used in the embodiments of the present invention are all conventional methods.

[0028] Unless otherwise specified, the materials, reagents, etc. used in the embodiments of the present invention can be obtained from commercial sources.

[0029] Example 1

[0030] The method for preparing agarwood extract comprises the following steps:

[0031] (1) Grind the agarwood, add it into a distillation kettle, heat it to 70°C and keep it for 30 minutes, heat it to 170°C and keep it for 2 hours, and obtain a distillate;

[0032] (2) Cooling the distillate and removing the upper essential oil to obtain the agarwood extract.

[0033] The preparation method of honeysuckle extract comprises the following steps:

[0034] S1: crushing honeysuckle and passing through a 200-mesh sieve to obtain honeysuckle powder;

[0035] S2: Mix honeysuckle powder and water in a mass ratio of 1:5, adjust the pH value to 4 with 1 mol / L hydrochloric acid solution, add 5% of a complex enzyme consisting of β-glucanase and cellulase in a mass ratio of 1:2 to the honeysuckle powder, extract with 200 W ultrasound for 10 min at an ultrasound temperature of 20°C, filter, and collect the filtrate to obtain a honeysuckle extract.

[0036] Add 7 times the amount of water according to the mass of Isatis root and boil for 1 hour. Add 3 times the amount of water according to the mass of Isatis root and boil for 15 minutes. Combine the filtrates to obtain Isatis root extract.

[0037] By weight, 10 parts of agarwood extract, 15 parts of honeysuckle extract and 6 parts of isatis root extract were weighed.

[0038] The agarwood extract, honeysuckle extract and isatis root extract are mixed, and filtered using a 0.45 μm polyethersulfone filter membrane to obtain a filtrate;

[0039] The filtrate was concentrated at 60°C to 25% of the original volume to obtain the finished product.

[0040] Example 2

[0041] The method for preparing agarwood extract comprises the following steps:

[0042] (1) crushing agarwood, adding it into a distillation kettle, heating it to 80°C for 50 min, heating it to 180°C for 4 h, and obtaining a distillate;

[0043] (2) Cooling the distillate and removing the upper essential oil to obtain the agarwood extract.

[0044] The preparation method of honeysuckle extract comprises the following steps:

[0045] S1: crushing honeysuckle and passing through a 200-mesh sieve to obtain honeysuckle powder;

[0046] S2: Mix honeysuckle powder and water in a mass ratio of 1:10, adjust the pH value to 5 with 1 mol / L hydrochloric acid solution, add 8% of a complex enzyme consisting of β-glucanase and cellulase in a mass ratio of 1:2.5 to the honeysuckle powder, extract with 400 W ultrasonically for 20 min at an ultrasonic temperature of 40°C, filter, and collect the filtrate to obtain a honeysuckle extract.

[0047] Add 10 times the amount of water according to the mass of Isatis root and boil for 2 hours. Add 5 times the amount of water according to the mass of Isatis root and boil for 25 minutes for the second water decoction. Combine the filtrates to obtain Isatis root extract.

[0048] By weight, 13 parts of agarwood extract, 20 parts of honeysuckle extract and 10 parts of isatis root extract were weighed.

[0049] The agarwood extract, honeysuckle extract and isatis root extract are mixed, and filtered using a 0.45 μm polyethersulfone filter membrane to obtain a filtrate;

[0050] The filtrate was concentrated at 80°C to 35% of the original volume to obtain the finished product.

[0051] Example 3

[0052] The method for preparing agarwood extract comprises the following steps:

[0053] (1) crushing agarwood, adding it into a distillation kettle, heating it to 75°C for 40 min, heating it to 175°C for 3 h, and obtaining a distillate;

[0054] (2) Cooling the distillate and removing the upper essential oil to obtain the agarwood extract.

[0055] The preparation method of honeysuckle extract comprises the following steps:

[0056] S1: crushing honeysuckle and passing through a 200-mesh sieve to obtain honeysuckle powder;

[0057] S2: Mix honeysuckle powder and water in a mass ratio of 1:8, adjust the pH value to 4.5 with 1 mol / L hydrochloric acid solution, add 6.5% of a complex enzyme consisting of β-glucanase and cellulase in a mass ratio of 1:2.25 to the honeysuckle powder, extract with 300 W ultrasound for 15 min at an ultrasound temperature of 30°C, filter, and collect the filtrate to obtain a honeysuckle extract.

[0058] Add 8 times the amount of water according to the mass of Isatis root and boil for 1.5 hours. Add 4 times the amount of water according to the mass of Isatis root and boil for 20 minutes for the second water decoction. Combine the filtrates to obtain Isatis root extract.

[0059] By weight, 12 parts of agarwood extract, 18 parts of honeysuckle extract and 8 parts of isatis root extract were weighed.

[0060] The agarwood extract, honeysuckle extract and isatis root extract are mixed, and filtered using a 0.45 μm polyethersulfone filter membrane to obtain a filtrate;

[0061] The filtrate was concentrated at 70°C to 30% of the original volume to obtain the finished product.

[0062] Comparative Example 1

[0063] The method for preparing agarwood extract comprises the following steps:

[0064] (1) Grind the agarwood, add it into a distillation kettle, heat it to 70°C and keep it for 30 minutes, heat it to 170°C and keep it for 2 hours, and obtain a distillate;

[0065] (2) Cooling the distillate and removing the upper essential oil to obtain the agarwood extract.

[0066] The preparation method of honeysuckle extract comprises the following steps:

[0067] S1: crushing honeysuckle and passing through a 200-mesh sieve to obtain honeysuckle powder;

[0068] S2: Mix honeysuckle powder and water in a mass ratio of 1:5, adjust the pH value to 4 with 1 mol / L hydrochloric acid solution, add 5% of a complex enzyme consisting of β-glucanase and cellulase in a mass ratio of 1:2 to the honeysuckle powder, extract with 200 W ultrasound for 10 min at an ultrasound temperature of 20°C, filter, and collect the filtrate to obtain a honeysuckle extract.

[0069] Add 7 times the amount of water according to the mass of Isatis root and boil for 1 hour. Add 3 times the amount of water according to the mass of Isatis root and boil for 15 minutes. Combine the filtrates to obtain Isatis root extract.

[0070] By weight, weigh 10 parts of agarwood extract, 10 parts of honeysuckle extract and 10 parts of isatis root extract.

[0071] The agarwood extract, honeysuckle extract and isatis root extract are mixed, and filtered using a 0.45 μm polyethersulfone filter membrane to obtain a filtrate;

[0072] The filtrate was concentrated at 60°C to 25% of the original volume to obtain the finished product.

[0073] Test Example 1

[0074] The test was conducted using an Omron compression nebulizer. The finished product concentrations were examined at 10 mg / mL and 20 mg / mL. Samples were taken 1 hour and 4 hours after the nebulization test to detect the drug concentrations in the plasma and lung tissue of mice after nebulization inhalation. There were 3 mice in each test group, and a total of 12 mice were tested.

[0075]

[0076] The experimental results show that the agarwood cough relieving aerosol composition prepared by the present invention can be quickly delivered to the lung tissue within one hour. By examining the blood drug concentration and the drug concentration in the lung tissue for 4 hours, the results show that the agarwood cough relieving aerosol composition prepared by the present invention can prolong the blood drug concentration and the drug concentration in the lung tissue, and improve the cough relieving effect. By comparing the experimental results of the finished product concentrations of 10mg / mL and 20mg / mL, when the finished product concentration is 20mg / mL, the blood drug concentration and the drug concentration in the lung tissue did not increase significantly compared to the finished product with a concentration of 10mg / mL. By detecting the particle size after atomization, the finished product of Example 3 has a particle size of 2.4μm when the concentration is 10mg / mL; when the concentration is 20mg / ml, the particle size is 6.1μm. By analysis, it can be obtained that when the concentration of the finished product of the present invention is about 10mg / mL, the particle size can reach the lesion faster during atomization inhalation, achieving the effect of rapid cough relief.

[0077] Comparative Example 1 changes the raw material ratio, resulting in a decrease in the content of the effective cough suppressant in the agarwood cough suppressant atomization composition. When the concentration is 10 mg / ml, the particle size after atomization is 4.8 μm. Therefore, the blood drug concentration and the drug concentration in the lung tissue of the agarwood cough suppressant atomization composition are significantly reduced compared with Example 3.

[0078] Test Example 2

[0079] Healthy SD rats aged 4 to 6 weeks were used to test the nasal mucociliary activity.

[0080] The products prepared in Example 3 and Comparative Example 1 were administered to rats at a concentration of 1 mg / mL. There were 6 rats in each group, and a control group was set up, which did not use any product.

[0081] Observation of nasal mucociliary activity: Rats were killed by cervical dislocation, and the nasal mucosa of the rats was cut by surgery. The cilia of the mucosa were observed under a microscope, and then placed in a chromatography cylinder with a small amount of distilled water, sealed so that the water vapor was nearly saturated, and the ambient temperature was 25°C. The specimens were taken out every 10 minutes and observed under a microscope. If the cilia continued to sway, they were put back into the cylinder until the cilia stopped swaying, and the cilia swaying time was recorded.

[0082] name Example 3 Comparative Example 1 Control group Cilia beating duration (min) 578.6 565.9 558.2

[0083] The test results show that the agarwood cough-relieving aerosol composition prepared by the present invention can enhance the activity of nasal mucosal cilia.

[0084] The above description is only a preferred embodiment of the present invention and is not intended to limit the present invention. Any modifications, equivalent substitutions, improvements, etc. made within the spirit and principle of the present invention should be included in the protection scope of the present invention.

Claims

1. An agarwood cough relieving atomization composition, characterized in that: By weight, the raw materials include 10-13 parts of agarwood extract, 15-20 parts of honeysuckle extract and 6-10 parts of isatis root extract.

2. The agarwood cough relieving aerosol composition according to claim 1, characterized in that: The method for preparing the agarwood extract comprises the following steps: (1) crushing agarwood, adding it into a distillation kettle, heating it to 70-80° C. for the first time, and heating it to 170-180° C. for the second time to obtain a distillate; (2) Cooling the distillate and removing the upper essential oil to obtain the agarwood extract.

3. The agarwood cough relieving aerosol composition according to claim 1, characterized in that: The preparation method of the honeysuckle extract comprises the following steps: S1: crushing honeysuckle to obtain honeysuckle powder; S2: Mix honeysuckle powder and water, add complex enzyme, and perform ultrasonic extraction to obtain honeysuckle extract.

4. The agarwood cough relieving aerosol composition according to claim 1, characterized in that: The isatis root extract is prepared by decocting in water.

5. The agarwood cough relieving aerosol composition according to claim 2, characterized in that: In step (1), the first heating and insulation time is 30-50 minutes, and the second heating and insulation time is 2-4 hours.

6. The agarwood cough relieving aerosol composition according to claim 3, characterized in that: In step S2, the mass ratio of the honeysuckle powder to water is 1:5-10, the complex enzyme includes β-glucanase and cellulase in a mass ratio of 1:2-2.5, and 5-8% of the complex enzyme is added according to the honeysuckle powder.

7. The agarwood cough relieving aerosol composition according to claim 3, characterized in that: In step S2, the pH value of the honeysuckle powder and water is adjusted to 4-5 after mixing, and ultrasonic extraction is performed at 200-400W for 10-20min at a temperature of 20-40°C.

8. The agarwood cough relieving aerosol composition according to claim 4, characterized in that: The water decoction includes the first water decoction, adding 7-10 times the amount of water according to the mass of the Isatis root, and decocting for 1-2 hours; the second water decoction, adding 3-5 times the amount of water according to the mass of the Isatis root, and decocting for 15-25 minutes.

9. A method for preparing an agarwood cough relieving aerosol composition according to any one of claims 1 to 8, characterized in that: The following steps are involved: C1: mixing the agarwood extract, honeysuckle extract and isatis root extract, and filtering with a polyethersulfone filter membrane to obtain a filtrate; C2: The filtrate is concentrated to 25-35% of the original volume to obtain the finished product.

10. The method for preparing the agarwood cough relieving aerosol composition according to claim 9, characterized in that: The concentration temperature is 60-80°C.