CN118059075A - Solution preparation for atomized inhalation of Guiling tablet as well as preparation method and application thereof - Google Patents

Solution preparation for atomized inhalation of Guiling tablet as well as preparation method and application thereof Download PDF

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CN118059075A
CN118059075A CN202410206001.5A CN202410206001A CN118059075A CN 118059075 A CN118059075 A CN 118059075A CN 202410206001 A CN202410206001 A CN 202410206001A CN 118059075 A CN118059075 A CN 118059075A
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parts
solution
guiling
tablet
preparation
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律广富
刘芳馨
刘钧
刘毅
张洪伟
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JILIN LIHUA DRUG CO Ltd
Changchun University of Chinese Medicine
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JILIN LIHUA DRUG CO Ltd
Changchun University of Chinese Medicine
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    • A61K36/73Rosaceae (Rose family), e.g. strawberry, chokeberry, blackberry, pear or firethorn
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Abstract

The invention discloses a solution preparation for inhalation of Guiling tablet, relates to the technical field of solution preparation for inhalation and a preparation method thereof, and aims to solve the problems that the existing preparation cannot meet the requirements of the drug administration population, and has long treatment period, slow effect, high drug administration cost and slow effect particularly when treating acute lung diseases. The composition comprises the following components in percentage by weight: 10-20 parts of a Guiling tablet atomized solution, 20-40 parts of an isotonic agent, 1-1.4 parts of a buffer solution and 500-1000 parts of water for injection, wherein the mixture ratio of the Guiling tablet atomized solution is 20-60 parts of ephedra, 20-50 parts of poppy shell, 10-40 parts of fried bitter apricot kernel, 10-40 parts of Chinese magnoliavine fruit, 10-40 parts of walnut kernel and 1-5 parts of cardamon; a preparation method of a solution preparation for atomizing inhalation of Guiling tablets comprises the following steps: step one: weighing 10 parts of an atomized solution of Guiling tablets, 20-40 parts of an isotonic agent and 0.5-1 part of a buffer solution, adding 50-60ml of water for injection, and uniformly stirring to obtain a solution a; step two: and adding 0.4-0.5 part of buffer solution into the solution a, regulating the pH value to 3.0-8.0, and adding 450-950ml of water for injection.

Description

Solution preparation for atomized inhalation of Guiling tablet as well as preparation method and application thereof
Technical Field
The invention relates to the technical field of solution preparations for aerosol inhalation and a preparation method thereof, in particular to a solution preparation for aerosol inhalation of Guiling tablets and a preparation method and application thereof.
Background
Respiratory diseases are common and frequently-occurring diseases, and are mainly caused by the diseases of trachea, bronchus, lung and chest, and the patients with light diseases are affected by cough, chest pain and respiration, and the patients with serious diseases are caused by dyspnea, hypoxia and even respiratory failure. Patients with respiratory diseases proliferate with changes in air pollution, environment, and climate. Respiratory diseases have attracted considerable attention from the world. Respiratory diseases have become one of the risk factors threatening human health. Mortality from respiratory disease is third in the global non-infectious disease mortality rank, next to cardiovascular disease and tumors.
The Guiling tablet is prepared from 6 Chinese medicinal materials including ephedra, poppy shell, schisandra fruit, bitter apricot seed, walnut kernel and cardamon seed, and has the functions of astringing lung qi, relieving cough and asthma. The clinical application exceeds 30 years, the curative effect is definite, and the market feedback is good. At present, only two dosage forms of Guiling tablets and Guiling pills are available in the market, and are more traditional dosage forms, and the curative effect is definite, but the absorption effect and the treatment period are slower. In recent years, along with the increase of clinical medicine application crowds, the existing dosage forms cannot meet the requirements of the medicine application crowds, have long treatment period, slow effect and high medicine application cost, particularly have slow effect when treating acute lung diseases, so that a solution preparation for atomizing and inhaling Guiling tablets, a preparation method and application thereof are urgently needed in the market to solve the problems.
Disclosure of Invention
The invention aims to provide a solution preparation for atomizing inhalation of Guiling tablets, and a preparation method and application thereof, so as to solve the problems that the existing preparation formulation provided in the background art cannot meet the requirements of the people taking medicines, has long treatment period, slow effect and high medicine taking cost, and particularly has slow effect in treating acute lung diseases.
In order to achieve the above purpose, the present invention provides the following technical solutions: a solution preparation for atomizing inhalation of Guiling tablet comprises the following components in parts by weight: 10-20 parts of a Guiling tablet atomized solution, 20-40 parts of an isotonic agent, 1-1.4 parts of a buffer solution and 500-1000 parts of water for injection, wherein the mixture ratio of the Guiling tablet atomized solution is 20-60 parts of ephedra, 20-50 parts of poppy shell, 10-40 parts of fried bitter apricot kernel, 10-40 parts of Chinese magnoliavine fruit, 10-40 parts of walnut kernel and 1-5 parts of cardamon.
Ma Huang is pungent and slightly bitter in flavor, warm in nature, enters lung meridian and bladder meridian. Has effects in inducing sweat, relieving exterior syndrome, dispersing lung qi, relieving asthma, inducing diuresis and relieving edema. Mainly treats chest distress, asthma and cough, edema of wind and water, phlegm nodule, asthma and cough, and the parts of poppy shell are preferably 28-32 parts based on the parts by mass of ephedra. The mass fraction of poppy shell is preferably 3/4 times of that of herba Ephedrae.
Papaver is sour and astringent in flavor, and enters lung, large intestine and kidney meridians. Has effects in astringing lung, astringing intestine, and relieving pain. Can be used for treating chronic cough and chronic diarrhea. The weight portion of the ephedra is preferably 18-22 portions of the fried bitter apricot seed. The weight part of the fried bitter apricot kernel is preferably 1/2 times of the weight part of the ephedra herb.
The fried bitter apricot kernel has bitter taste, slightly warmth, enters lung and large intestine channels, and has the functions of reducing qi, relieving cough and asthma, and relaxing bowel. Can be used for treating cough, asthma, chest fullness, excessive phlegm, constipation due to intestinal dryness. The weight portion of the Chinese ephedra is preferably 18-22 portions. The weight part of the schisandra chinensis is preferably 1/2 times of the weight part of the ephedra herb.
Schisandra chinensis is sour, sweet and warm in taste. It enters lung, heart and kidney meridians. Has effects in astringing, invigorating qi, promoting salivation, invigorating kidney, and tranquilizing mind. Can be used for treating chronic cough, deficiency asthma, nocturnal emission, enuresis, frequent urination, chronic diarrhea, spontaneous perspiration, night sweat, body fluid consumption, thirst, internal heat, diabetes, palpitation, and insomnia. The weight part of the Chinese ephedra is preferably 18-22 parts of the walnut kernel. The weight part of the walnut kernel is preferably 1/2 times of the weight part of the ephedra herb.
Walnut kernel is sweet and warm in taste. Enter kidney, lung and large intestine meridians. Has effects in invigorating kidney, warming lung, and moisturizing intestine. Can be used for treating kidney yang deficiency, soreness of waist and knees, sexual impotence, spermatorrhea, dyspnea and cough due to deficiency-cold, and constipation due to intestinal dryness. The weight part of the cardamon is preferably 2-3 parts based on the weight part of the ephedra herb. The mass part of the cardamom is preferably 1/16 times of the mass part of the ephedra.
Cardamon is pungent and warm. Enter lung, spleen and stomach meridians. Has effects in eliminating dampness, activating qi-flowing, warming middle energizer, relieving vomiting, stimulating appetite, and promoting digestion. Can be used for treating damp obstruction in middle energizer, anorexia, early stage of damp-warm syndrome, chest distress, hunger, cold-dampness vomiting, chest and abdominal distention and pain, and dyspepsia.
In the invention, the mass ratio of ephedra, poppy shell, schisandra chinensis, bitter apricot seed, walnut kernel and cardamon in the solution preparation for aerosol inhalation of the Guiling tablet is preferably 4:3:2:2:2:0.25, wherein the mass ratio of the atomized solution of the Guiling tablet to the isotonic solution is preferably 1:4.
The ephedra herb is a monarch drug, and has the effects of freeing lung, relieving asthma, sweating and relieving exterior syndrome; poppy shell and fried bitter apricot kernel are ministerial drugs for astringing lung and descending qi, relieving cough and asthma; it is combined with Ma Huang to strengthen the effect of astringing lung to arrest cough; fructus Schisandrae chinensis and semen Juglandis are used as adjuvant drugs, and have effects of invigorating qi, promoting fluid production, invigorating kidney, calming heart, warming lung, and moisturizing intestine; fructus Amomi rotundus is used as a guiding drug for resolving dampness, activating qi-flowing, warming middle energizer, relieving vomiting, stimulating appetite, resolving food stagnation, and guiding drugs for ascending and entering lung.
A preparation method of a solution preparation for atomizing inhalation of Guiling tablets comprises the following steps:
Step one: weighing 10 parts of an atomized solution of Guiling tablets, 20-40 parts of an isotonic agent and 0.5-1 part of a buffer solution, adding 50-60ml of water for injection, and uniformly stirring to obtain a solution a;
step two: and adding 0.4-0.5 part of buffer solution into the solution a, regulating the pH value to 3.0-8.0, and adding 450-950ml of water for injection.
The pH is preferably adjusted to 6.0-7.0.
Preferably, the preparation method of the Guiling tablet atomized solution comprises the following steps:
Step one: reflux-extracting fructus Amomi rotundus 1-5 parts, herba Ephedrae 20-60 parts, plantula Papaveris 20-50 parts and semen Juglandis 10-40 parts with water for two times, the first time for 3.5-4 hr and the second time for 2.5-3 hr, and mixing the extractive solutions;
Step two: filtering the extracting solution, concentrating the filtrate, adding 40-80ml of 80% ethanol, mixing, standing, filtering, recovering ethanol from the filtrate, adding purified water to 50-80ml, and refrigerating to obtain a first mixed solution;
Step three: parching 10-40 parts of semen Armeniacae amarum, squeezing to remove oil, mixing with fructus Schisandrae, reflux-extracting with 40-80ml of 80% ethanol for 1.5-2 hr for the first time and 1-1.5 hr for the second time, mixing extractive solutions, filtering, recovering ethanol from filtrate, adding purified water, and refrigerating to obtain mixed solution II;
step four: mixing the first mixed solution and the second mixed solution, uniformly mixing and concentrating to 50-100ml to obtain the atomized solution of Guiling tablet.
The preparation of the water extract and the alcohol extract is not time sequential. The invention carries out water reflux extraction and oil removal of the fried bitter apricot and schisandrin by the cardamon, the ephedra herb, the poppy shell and the walnut kernel, thereby ensuring the dissolution rate of the effective parts of the medicine. The oil removal of the fried bitter apricot is to remove oil and is beneficial to the dissolution of effective substances.
Preferably, the isotonic agent is one of potassium chloride, magnesium chloride, calcium chloride, glucose, xylitol and sorbitol, and preferably sodium chloride.
Preferably, the buffer solution is one of citric acid-disodium hydrogen phosphate, potassium dihydrogen phosphate-disodium hydrogen phosphate, citric acid-sodium hydroxide and citric acid-disodium hydrogen phosphate, and preferably citric acid-sodium citrate.
The addition of citric acid and sodium citrate buffer solvent is beneficial to the dissolution of the medicine on one hand; on the other hand, the pH value of the solution can be kept stable.
The prepared solution preparation for atomizing inhalation of the Guiling tablet is applied to the preparation of medicaments for cough, expectoration, pharyngitis, bronchial asthma and emphysema.
The dosage of the solution preparation for atomizing and inhaling the Guiling tablet is 0.1-0.8 times of that of the Guiling tablet, and the preferable dosage is 0.3-0.5 times of that of the Guiling tablet.
Compared with the prior art, the invention has the beneficial effects that: the invention provides a solution preparation for inhalation of Guiling tablet, which is prepared by extracting an atomized solution of Guiling tablet from ephedra, poppy shell, fried bitter apricot seed, schisandra chinensis, walnut kernel and cardamon as raw materials, mixing the atomized solution of Guiling tablet with an isotonic solution, and adding a proper amount of buffer solution. The solution preparation for inhalation of the Guiling tablet fills the blank of atomizing administration of the Guiling tablet. Meanwhile, the application of atomized administration for treating respiratory diseases can avoid the first pass elimination effect, has the advantages of quick response, no toxic or side effect, high patient compliance, high targeting property, high local drug concentration, small dosage, convenient application, less systemic adverse reaction and the like, can remarkably improve the stability and bioavailability of the Guiling tablet, has different administration routes and reduced dosage compared with the Guiling tablet, can realize small-dosage, rapid and effective treatment, and has obvious advantages. In addition, the adopted preparation method is convenient for industrial production. According to the embodiment, the Guiling tablet aerosol inhalation preparation provided by the invention can effectively prolong the residence time of the medicine in the lung, increase the medicine availability, and has better cough and asthma relieving effects than an oral administration mode.
Drawings
FIG. 1 is a schematic diagram of the results of drug metabolism in various tissues of rats in the Guiling tablet atomization preparation group;
FIG. 2 is a schematic diagram of the results of drug metabolism in various tissues of rats in the Guiling tablet oral group;
FIG. 3 is a schematic representation of cell sorter counts after administration of rats of each group in the present invention;
FIG. 4 is a graph showing lung tissue associated cytokine levels following administration to various groups of rats in accordance with the present invention;
FIG. 5 is a schematic representation of the asthma-relieving latency after administration of each group of rats in the present invention;
FIG. 6 is a graphical representation of asthma behavior scores after administration of rats in each group of rats in the present invention;
FIG. 7 is a graph showing the pathological changes of the trachea of rats in each group according to the present invention;
FIG. 8 is a graph showing the pathological changes of lung tissue of rats in each group according to the present invention.
Detailed Description
The following description of the embodiments of the present invention will be made clearly and completely with reference to the accompanying drawings, in which it is apparent that the embodiments described are only some embodiments of the present invention, but not all embodiments.
Example 1:
Preparing an atomized solution of Guiling tablets:
40g of ephedra herb, 30g of poppy shell, 20g of fried bitter apricot seed, 20g of shizandra berry, 20g of walnut kernel and 2.5g of cardamon fruit are taken, the cardamon fruit, the ephedra herb, the poppy shell and the walnut kernel are put into a round-bottom flask, water is added for reflux extraction for two times, the first time is 4 hours and the second time is 2.5 hours, the extracting solutions are combined, filtered, the filtrate is concentrated to 40ml, 80ml of 80% ethanol is added for uniform mixing, after standing for 2 hours, the filtering is carried out, the ethanol is recovered from the filtrate, the purified water is added to 50ml, and the mixture is refrigerated for standby. Squeezing and deoiling semen armeniacae amarae, reflux-extracting fructus Schisandrae chinensis with 80% ethanol for 2 hr for the first time and 1 hr for the second time, mixing the extractive solutions, filtering, recovering ethanol from filtrate, adding purified water to 20ml, refrigerating for use, mixing the above solutions, and concentrating to obtain the atomized solution of Guiling tablet.
Preparation of an atomized solution of Guiling tablets:
Taking 10g of the active ingredients, 10g of sodium chloride and 0.5g of citric acid, adding 50ml of water for injection, and uniformly stirring to completely dissolve; adding 0.5mol/L sodium citrate into the solution, adjusting pH to 6.0-7.0, and adding injectable water to 500 ml;
Example 2
Preparation of an atomized solution of Guiling tablets: (same as in example 1)
Preparation of an atomized solution of Guiling tablets:
Taking 10g of the active ingredients, 20g of sodium chloride and 0.8g of citric acid, adding 50ml of water for injection, and uniformly stirring to completely dissolve; adding 0.5mol/L sodium citrate into the solution, adjusting pH to 6.0-7.0, and adding injectable water to 500 ml;
Example 3
Preparation of an atomized solution of Guiling tablets: (same as in example 1)
Preparation of an atomized solution of Guiling tablets:
Taking 10g of the active ingredients, 20g of magnesium chloride and 1g of citric acid, adding 50ml of water for injection, and uniformly stirring to completely dissolve; adding 0.4mol/L disodium hydrogen phosphate into the solution, adjusting pH to 6.0-7.0, and adding water for injection to 500 ml;
Example 4
Preparation of an atomized solution of Guiling tablets: (same as in example 1)
Preparation of an atomized solution of Guiling tablets:
taking 20g of the active ingredients, 40g of sodium chloride and 1g of citric acid, adding 50ml of water for injection, and uniformly stirring to completely dissolve; adding 0.4mol/L disodium hydrogen phosphate into the solution, adjusting pH to 6.0-7.0, and adding water for injection to 500 ml;
The atomized preparation of Guiling tablet prepared in example 4 was used for in vivo distribution experiment in rats
Wistar rats 40 were divided into a blank group, a model group, an oral administration group, and an aerosol administration group, each group having 10 animals. Saline was administered to the blank and model groups; the oral administration group is given with 0.5g/kg of Guiling tablet; atomized administration group 5ml/kg of the prepared atomized preparation of Guiling tablet was administered.
After administration, 6 rats were harvested at 1h, 3h, 6h and 12h, respectively, and after anesthesia with pentobarbital, blood was harvested from the abdominal aorta and serum was isolated. Taking brain, heart, liver, spleen, lung and kidney, flushing blood on the surface with physiological saline, sucking the blood with filter paper, and weighing 1g of each tissue respectively. Adding precooled PBS for homogenizing to prepare tissue homogenate. The content of ephedrine hydrochloride and pseudoephedrine hydrochloride in animal tissues of each group is detected by taking ephedrine hydrochloride and pseudoephedrine hydrochloride as reference substances.
The results are shown in table 1 and fig. 1 and 2.
TABLE 1 in vivo distribution of experimental data in rats
As shown in table 1 and the results in fig. 1, the total content of ephedrine hydrochloride and pseudoephedrine hydrochloride in the lung tissue of rats in the Guiling tablet atomization preparation group reaches a peak 3 hours after atomization administration, and the Guiling tablet oral administration group reaches a peak 6 hours; the total content of ephedrine hydrochloride and pseudoephedrine hydrochloride in rat lung tissue in the Guiling tablet atomized preparation group is obviously higher than that in Yu Gui tablet oral dosage groups in each time period. The content in other tissues is equivalent. Experimental results indicate that compared with an oral administration group, the accumulation concentration of the Guiling tablet atomization preparation group in the lung is obviously increased, and the lung disease can be treated in a targeted manner; and the accumulation speed in the lung is high, the peak is reached in 3 hours, and compared with an oral administration group of Guiling tablets, the lung disease can be treated more rapidly.
The atomized preparation of Guiling tablet prepared in example 4 is used for experimental study of animal in vivo
Experimental method
SPF grade SD rats were randomly divided into 6 groups: blank (CO), model (MO), guiling tablet 0.2g/kg atomization (AT-0.2), guiling tablet 0.1g/kg atomization (AT-0.1), guiling tablet 0.5g/kg oral (IG-0.5), guiling tablet 0.25g/kg oral (IG-0.25). After one week of adaptive rearing of 10 animals per group, asthma models were prepared.
Except for the blank control group, all rats were prepared with ovalbumin in combination with aluminum hydroxide to form an asthma model. The rats of each group were sensitized by subcutaneously injecting 20 μg ovalbumin and 1mg aluminum hydroxide mixture at 0d, 7d and 14d of the experiment; the asthma was stimulated by inhalation of the 1% ovalbumin suspension at 21d, 23d, 25d, 27d for 15 min. Meanwhile, the rats in the blank group were subcutaneously injected with an equivalent amount of physiological saline in experiments 0d, 7d, and 14d, and the 21d, 23d, 25d, and 27d were inhaled with an equivalent amount of atomized physiological saline.
After the model is successfully prepared, the blank control group and the model group are atomized and given with physiological saline; AT-0.2 and AT-0.1 were respectively given by atomization to 5ml/kg and 2.5ml/kg of the atomized preparation of Guiling tablet prepared in example 4; the groups IG-0.5 and IG-0.25 are respectively administrated with 0.5g/kg and 0.25g/kg of Guiling tablet by stomach irrigation. The administration treatment was started at 14d of a mixed solution of 20. Mu.g of ovalbumin and 1mg of aluminum hydroxide by subcutaneous injection, and the administration was continued for 14d. The rat's asthma-inducing latency was recorded after the last dose, and the number of cough-asthma behaviors in the rat for 5 minutes was recorded.
After the end of the experiment, the animals were anesthetized with sodium pentobarbital (40 mg/kg), and alveolar lavage fluid was collected for cell counting and inflammatory cell sorting counting. Picking up the trachea and the right lung leaves, fixing the trachea and the right lung leaves in 10% paraformaldehyde solution, and performing HE staining after fixing the trachea and the right lung leaves completely; taking left lung leaf for tissue homogenate, collecting supernatant, and measuring and detecting the content of IL-4, IFN-gamma, IL-2 and TNF-alpha in the tissue homogenate by ELISA method.
The results are shown in tables 2 to 4 and figures 3 to 8.
Table 2 cell sorting counts of alveolar lavage fluid from each group of rats (. Times.105/ml)
Note that: compared to the blank, #p <0.01; p <0.01, P <0.05 compared to model group
As can be seen from table 2, fig. 3, the total cell number, neutrophil number and eosinophil number were all significantly increased in the alveolar lavage fluid of the rats in the asthma model group (p < 0.01) compared to the blank group; compared with the model group, the total cell number, the neutrophil number and the eosinophil number of the rats in the AT-0.2 group are all significantly reduced (p < 0.01); total cell number, neutrophil number, eosinophil number were significantly reduced in AT-0.1 group rats (p < 0.05); the total cell number of the group of rats of IG-0.5 is obviously reduced (p < 0.01), the number of neutrophils and eosinophils is reduced, and the difference is not obvious; the total cell number, neutrophil number and eosinophil number were all decreased in the IG-0.25 group, with no significant difference. The atomized preparation of the Guiling tablet is obviously superior to the Guiling tablet in reducing the total cell number, the neutrophil number and the eosinophil number in the alveolar lavage fluid of the rat in the asthma model.
TABLE 3 serum inflammatory factor levels in groups of rats
Note that: compared to the blank, #p <0.01; p <0.01, P <0.05 compared to model group
As can be seen from table 3 and fig. 4, the serum IL-4, IFN- γ, IL-2, TNF- α content was significantly increased (p < 0.01) in rats of asthma model group compared to the blank group; compared with the asthma model group, the serum IL-4, IFN-gamma, IL-2 and TNF-alpha contents of the rats in the AT-0.2 group are obviously reduced (p < 0.01); AT-0.1 group rats had significantly reduced IL-4, IFN- γ, IL-2 (p < 0.01) TNF- α content, but no significant differences; serum IL-4 content of the group of rats of IG-0.5 is reduced (p < 0.05), IFN-gamma, IL-2, TNF-alpha and IgE content are reduced, but no obvious difference exists; the serum IL-4, IFN-gamma, IL-2, TNF-alpha and IgE content of the group of rats of IG-0.25 are reduced, but the change is not obvious.
Table 4 rat asthma latency and asthma behavior score for each group
P <0.01, P <0.05 compared to model group
As shown in table 4 and fig. 5-6, compared with the model group, the Guiling tablet atomization preparation group and the oral administration group can obviously improve the asthma behavioral score of the asthma rat and prolong the asthma inducing latency period; however, from the aspect of treatment effect, the treatment effect of the Guiling tablet atomization preparation group on asthma rat asthma inducing latency and asthma behavior scoring is superior to that of the Guiling tablet oral administration group, so that the Guiling tablet atomization preparation group has better treatment effect on asthma.
Histopathological changes of the trachea and lungs of rats in each group
As can be seen from fig. 7-8, the lung tissue cells of the normal group rat have complete structure, clear boundary, ordered arrangement, no infiltration of inflammatory cells, complete tracheal mucosa structure, no obvious thickening of the mucosal wall and ordered arrangement of epithelial cells; the arrangement of lung tissue cells of a model group rat is disordered, a large amount of inflammatory cells infiltrate, alveolar walls thicken, alveolar structure intervals are increased, tracheal mucosa walls obviously thicken, epithelial cells are widely necrotized and shed, nuclei shrink deeply stain and disintegrate, necrotic cell fragments are mostly seen in a lumen, eosinophilic mucus infiltration is accompanied, and the arrangement of lamina propria connective tissue is disordered, glands expand and the shape is irregular; the Guiling tablet atomized preparation group and the Guiling tablet oral group have different degrees of improvement and repair effects on lung and bronchus tissue injury of rats in asthma models, but from pathological observation results, the Guiling tablet atomized preparation group has obvious better improvement degree on lung and bronchus tissue injury than the oral group, and particularly has obvious treatment effect on lung and bronchus tissue injury of rats in asthma models in the AT-0.2 group.
It will be evident to those skilled in the art that the invention is not limited to the details of the foregoing illustrative embodiments, and that the present invention may be embodied in other specific forms without departing from the spirit or essential characteristics thereof. The present embodiments are, therefore, to be considered in all respects as illustrative and not restrictive, the scope of the invention being indicated by the appended claims rather than by the foregoing description, and all changes which come within the meaning and range of equivalency of the claims are therefore intended to be embraced therein. Any reference sign in a claim should not be construed as limiting the claim concerned.

Claims (6)

1. The solution preparation for atomizing inhalation of the Guiling tablet is characterized by comprising the following components in parts by weight: 10-20 parts of a Guiling tablet atomized solution, 20-40 parts of an isotonic agent, 1-1.4 parts of a buffer solution and 500-1000 parts of water for injection, wherein the mixture ratio of the Guiling tablet atomized solution is 20-60 parts of ephedra, 20-50 parts of poppy shell, 10-40 parts of fried bitter apricot kernel, 10-40 parts of Chinese magnoliavine fruit, 10-40 parts of walnut kernel and 1-5 parts of cardamon.
2. The preparation method of the solution preparation for inhalation by atomizing of the Guiling tablet is characterized by comprising the following steps:
Step one: weighing 10 parts of an atomized solution of Guiling tablets, 20-40 parts of an isotonic agent and 0.5-1 part of a buffer solution, adding 50-60ml of water for injection, and uniformly stirring to obtain a solution a;
step two: and adding 0.4-0.5 part of buffer solution into the solution a, regulating the pH value to 3.0-8.0, and adding 450-950ml of water for injection.
3. The method for preparing the solution preparation for atomized inhalation of the Guiling tablet according to claim 2, which is characterized in that the method for preparing the atomized solution of the Guiling tablet comprises the following steps:
Step one: reflux-extracting fructus Amomi rotundus 1-5 parts, herba Ephedrae 20-60 parts, plantula Papaveris 20-50 parts and semen Juglandis 10-40 parts with water for two times, the first time for 3.5-4 hr and the second time for 2.5-3 hr, and mixing the extractive solutions;
Step two: filtering the extracting solution, concentrating the filtrate, adding 40-80ml of 80% ethanol, mixing, standing, filtering, recovering ethanol from the filtrate, adding purified water to 50-80ml, and refrigerating to obtain a first mixed solution;
Step three: parching 10-40 parts of semen Armeniacae amarum, squeezing to remove oil, mixing with fructus Schisandrae, reflux-extracting with 40-80ml of 80% ethanol for 1.5-2 hr for the first time and 1-1.5 hr for the second time, mixing extractive solutions, filtering, recovering ethanol from filtrate, adding purified water, and refrigerating to obtain mixed solution II;
step four: mixing the first mixed solution and the second mixed solution, uniformly mixing and concentrating to 50-100ml to obtain the atomized solution of Guiling tablet.
4. The method for preparing the solution preparation for inhalation by atomizing of Guiling tablet according to claim 2, wherein the isotonic agent is one of potassium chloride, magnesium chloride, calcium chloride, glucose, xylitol and sorbitol, preferably sodium chloride.
5. The method for preparing a solution preparation for inhalation by atomizing a Guiling tablet according to claim 2, wherein the buffer is one of citric acid-disodium hydrogen phosphate, potassium dihydrogen phosphate-disodium hydrogen phosphate, citric acid-sodium hydroxide, and citric acid-disodium hydrogen phosphate, preferably citric acid-sodium citrate.
6. The method for preparing a solution preparation for inhalation by spraying Guiling tablet according to any one of claims 2 to 5, wherein the prepared solution preparation for inhalation by spraying Guiling tablet is applied to preparing medicines for cough, expectoration, pharyngitis, bronchial asthma and emphysema.
CN202410206001.5A 2024-02-26 2024-02-26 Solution preparation for atomized inhalation of Guiling tablet as well as preparation method and application thereof Pending CN118059075A (en)

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