Composition capable of effectively removing throat and adenoid allergens and relieving inflammation and preparation method thereof

Abstract

The invention relates to the technical field of medical supplies, in particular to a composition capable of effectively removing throat and adenoid allergens and relieving inflammation and a preparation method of the composition. The composition disclosed by the invention comprises the following components in percentage by weight: 0.01 wt%-10 wt% of beta-glucan, 0.05 wt%-15 wt% of cellulose ether, 0.01 wt%-2 wt% of Ectoine, 0.01 wt%-10 wt% of a cyclodextrin derivative, and the balance of water. Wherein the weight-average molecular weight of the beta-glucan is greater than or equal to 80WDa; the cellulose ether contains hydroxypropyl, and the content of the hydroxypropyl in the cellulose ether is 6%-12%.

Description

Technical Field

[0001] The present invention relates to the technical field of medical supplies, and particularly to a composition capable of effectively removing allergens in the throat and adenoids and relieving inflammation, and a preparation method thereof. Background Art

[0002] The throat is located behind the oral cavity, below the nasal cavity, and above the esophagus and trachea. The throat is a muscular tube through which food passes from the oral cavity to the esophagus and air passes from the nasal cavity to the lungs. Similar to the oral cavity and nasal cavity, the surface of the throat also has mucous membranes, and the cells in the mucous membranes produce mucus and have hairy protrusions (cilia). The adenoids, also known as pharyngeal tonsils or adenoid vegetations, are located at the top of the nasopharynx and the posterior pharyngeal wall and belong to lymphoid tissue. Under physiological conditions, allergens entering the throat or adenoids can be adhered by mucus and discharged through cilia; or, the adenoids can block a small part of the posterior nasal aperture, and resist inhaled allergens by adhering to, filtering, and buffering the nasal airflow, thereby protecting the airway. However, under pathological conditions (such as inflammation), the clearance function of the throat mucus-ciliary system is blocked, the pharyngeal mucosa is damaged, and the nerve sensitivity under the pharyngeal mucosa is increased, resulting in the accumulation and prolonged residence time of allergens in the throat, enhanced allergic reactions, and clinical features such as dryness, itching, dry cough without phlegm, and pale pharyngeal mucosa; or, the local immune defense ability of the adenoids against allergens decreases, and the tissue edema caused by allergens can further increase the volume of the adenoids, further changing the immune microenvironment of the adenoid tissue. Continuous allergen stimulation may damage the upper respiratory mucosa and may stimulate β receptors through the nerve endings under the exposed epithelial cells, causing a decrease in the excitability of β receptors, resulting in airway hyperresponsiveness and further leading to the occurrence of airway inflammation. Therefore, it is necessary to remove allergens entering the throat and adenoids to relieve or treat related inflammation.

[0003] Clinically, referring to the treatment regimens for allergic rhinitis and allergic asthma, the inflammation in the throat and adenoids is treated by using a drug regimen of antagonizing leukotrienes, antihistamines, and hormones for patients. However, the long-term efficacy of this single anti-allergy treatment is not very satisfactory, and symptoms such as dry itching and irritating cough in the pharynx of patients often cannot be effectively and safely treated. The allergic inflammation in the untreated throat and adenoids is likely to develop downward into the airway, secondary to other airway allergic inflammations and related diseases. Blocking allergens has fewer side effects than using clinically used anti-allergy drugs, and the efficacy is expected to be safer and more effective. However, at present, the research and development of allergen blockers are relatively few. Therefore, it is an urgent problem to explore and develop safer, more reasonable, and effective allergen blockers to effectively remove allergens in the throat and adenoids, reduce irritation, and relieve inflammation. Summary of the Invention

[0004] The present invention aims to solve at least one of the technical problems existing in the prior art. For this purpose, the present invention provides a composition for removing allergens from the throat and adenoids and relieving inflammation, and a preparation method thereof. The composition can isolate allergens, effectively relieve the inflammatory symptoms of the throat and adenoid regions, has safe raw materials and is convenient for medication.

[0005] In a first aspect of the present invention, there is provided a composition capable of effectively removing allergens from the throat and adenoids and relieving inflammation, the composition comprising:

[0006] 0.01 wt% to 10 wt% of β-glucan,

[0007] 0.05 wt% to 15 wt% of cellulose ether,

[0008] 0.01 wt% to 2 wt% of ectoin,

[0009] 0.01 wt% to 10 wt% of cyclodextrin derivative;

[0010] wherein the β-glucan has a weight-average molecular weight of ≥80 kDa;

[0011] the cellulose ether contains hydroxypropyl, and the content of hydroxypropyl in the cellulose ether is 6% to 12%.

[0012] After the composition of the present invention is administered, β-glucan gels together with cellulose ether to effectively adsorb allergens, thereby isolating allergens from entering the throat and adenoids; among them, high-molecular-weight β-glucan is beneficial to form a more uniform protective film, strengthening the removal and barrier functions of allergens. At the same time, the anti-inflammatory effect of β-glucan helps to relieve the inflammation of the throat and adenoid regions; on the one hand, due to its lower molecular weight, cellulose ether can improve the rheological properties of high-molecular-weight β-glucan, enhancing the regulation of the gel. On the other hand, the appropriate content of hydroxypropyl (6% to 12%) contained in cellulose ether helps to regulate the gel temperature, facilitating the transformation of the composition from a solution state to a gel state and exerting its barrier effect. Both ectoin and cyclodextrin derivative have the effects of moisturizing and humidifying. In addition, cyclodextrin derivative is beneficial for the composition to stay for a long time after reaching the throat and adenoids, and ectoin has a relieving effect on the edema of the throat and adenoid regions. The above four components cooperate to effectively prevent allergic inflammation caused by the stress response of foreign substances (such as allergens) to the throat and adenoids, and at the same time have a relieving effect on the inflammatory reaction at the throat and adenoids, and the effect is relatively persistent.

[0013] According to some embodiments of the present invention, the composition comprises 0.01 wt% to 10 wt% of β-glucan, that is, β-glucan accounts for 0.01 wt% to 10 wt% of the weight of the composition. For example, 0.01 wt% to 5 wt%, 0.01 wt% to 1 wt%, 0.01 wt% to 0.5 wt%, 0.01 wt% to 0.1 wt%, 0.01 wt% to 0.05 wt%, 0.05 wt% to 10 wt%, 0.05 wt% to 8 wt%, 0.05 wt% to 5 wt%, 0.05 wt% to 4 wt%, 0.05 wt% to 3 wt%, 0.05 wt% to 2 wt%, 0.05 wt% to 1 wt%, 0.05 wt% to 0.5 wt%, 0.1 wt% to 10 wt%, 0.1 wt% to 5 wt%, 0.1 wt% to 4 wt%, 0.1 wt% to 2 wt%, 0.1 wt% to 1 wt%, 0.1 wt% to 0.5 wt%, 0.5 wt% to 10 wt%, 0.5 wt% to 9 wt%, 0.5 wt% to 8 wt%, 0.5 wt% to 7 wt%, 0.5 wt% to 6 wt%, 0.5 wt% to 5 wt%, 0.5 wt% to 4 wt%, 0.5 wt% to 3 wt%, 0.5 wt% to 2 wt%, 0.5 wt% to 1 wt%.

[0014] According to some embodiments of the present invention, the composition comprises 0.05 wt% to 15 wt% of cellulose ether, that is, cellulose ether accounts for 0.05 wt% to 15 wt% of the weight of the composition. For example, 0.05 wt% to 12 wt%, 0.05 wt% to 10 wt%, 0.05 wt% to 5 wt%, 0.05 wt% to 1 wt%, 0.05 wt% to 0.5 wt%, 0.05 wt% to 0.1 wt%, 0.1 wt% to 10 wt%, 0.1 wt% to 8 wt%, 0.1 wt% to 5 wt%, 0.1 wt% to 2 wt%, 0.1 wt% to 1 wt%, 0.1 wt% to 0.5 wt%, 0.5 wt% to 5 wt%, 0.5 wt% to 2 wt%, 0.5 wt% to 1 wt%, 1 wt% to 10 wt%, 1 wt% to 8 wt%, 1 wt% to 6 wt%, 1 wt% to 5 wt%, 1 wt% to 4 wt%, 1 wt% to 3 wt%, 1 wt% to 2 wt%.

[0015] According to some embodiments of the present invention, the composition comprises 0.01 wt% to 2 wt% of ectoine, that is, ectoine accounts for 0.01 wt% to 2 wt% of the weight of the composition. For example, 0.01 wt% to 1.5 wt%, 0.01 wt% to 1 wt%, 0.01 wt% to 0.5 wt%, 0.01 wt% to 0.1 wt%, 0.1 wt% to 2 wt%, 0.1 wt% to 1.5 wt%, 0.1 wt% to 1 wt%, 0.1 wt% to 0.5 wt%.

[0016] According to some embodiments of the present invention, the composition comprises 0.01 wt% to 10 wt% of a cyclodextrin derivative, that is, the cyclodextrin derivative accounts for 0.01 wt% to 10 wt% of the weight of the composition. For example, 0.01 wt% to 5 wt%, 0.01 wt% to 1 wt%, 0.01 wt% to 0.5 wt%, 0.01 wt% to 0.1 wt%, 0.01 wt% to 0.05 wt%, 0.05 wt% to 10 wt%, 0.05 wt% to 8 wt%, 0.05 wt% to 5 wt%, 0.05 wt% to 4 wt%, 0.05 wt% to 3 wt%, 0.05 wt% to 2 wt%, 0.05 wt% to 1 wt%, 0.05 wt% to 0.5 wt%, 0.1 wt% to 10 wt%, 0.1 wt% to 5 wt%, 0.1 wt% to 4 wt%, 0.1 wt% to 2 wt%, 0.1 wt% to 1 wt%, 0.1 wt% to 0.5 wt%, 0.5 wt% to 10 wt%, 0.5 wt% to 9 wt%, 0.5 wt% to 8 wt%, 0.5 wt% to 7 wt%, 0.5 wt% to 6 wt%, 0.5 wt% to 5 wt%, 0.5 wt% to 4 wt%, 0.5 wt% to 3 wt%, 0.5 wt% to 2 wt%, 0.5 wt% to 1 wt%.

[0017] According to some embodiments of the present invention, the molecular weight of the β-glucan can be ≥80 kDa, for example ≥90 kDa, ≥100 kDa, ≥110 kDa, ≥120 kDa, ≥130 kDa, ≥140 kDa, ≥150 kDa, 80 - 150 kDa, 100 - 120 kDa.

[0018] According to some embodiments of the present invention, the β-glucan has a β-1,3-linkage as the main chain, and on average, 1 - 2 glucose side chains linked by β-1,6 are contained on every 3 - 7 main-chain glucose residues.

[0019] According to some embodiments of the present invention, the β-glucan is yeast β-glucan.

[0020] According to some embodiments of the present invention, the cellulose ether is selected from at least one of hydroxypropyl cellulose, hydroxypropyl methyl cellulose, hydroxypropyl ethyl cellulose, and hydroxypropyl carboxymethyl cellulose.

[0021] According to some embodiments of the present invention, the weight-average molecular weight of the cellulose ether is 4 to 20 kDa, for example, 4 to 18 kDa, 4 to 16 kDa, 4 to 15 kDa, 4 to 12 kDa, 4 to 10 kDa, 4 to 9 kDa, 4 to 8 kDa, 4 to 7 kDa, 4 to 6 kDa, 4 to 5 kDa, 5 to 18 kDa, 5 to 16 kDa, 5 to 15 kDa, 5 to 12 kDa, 5 to 10 kDa, 5 to 9 kDa, 5 to 8 kDa, 5 to 7 kDa, 5 to 6 kDa, 6 to 16 kDa, 6 to 15 kDa, 6 to 12 kDa, 6 to 10 kDa, 6 to 9 kDa, 6 to 8 kDa, 6 to 7 kDa, 7 to 15 kDa, 7 to 12 kDa, 7 to 10 kDa, 7 to 9 kDa, 7 to 8 kDa, 8 to 12 kDa, 8 to 10 kDa, 8 to 9 kDa.

[0022] According to some embodiments of the present invention, the content of hydroxypropyl in the cellulose ether is 6% to 12%, for example, 6% to 10%, 8% to 12%.

[0023] According to some embodiments of the present invention, the weight ratio of β-glucan to cellulose ether is 1:1 to 3, for example, 1:1 to 2.5, 1:1 to 2, 1:1 to 1.5, 1:1 to 1.2, 1:1.2 to 1.5, 1:1.5 to 3, 1:1.5 to 2.5, 1:1.5 to 2. The high-molecular-weight β-glucan used in the present invention has a network structure and can be used to provide the basic framework of the gel, while the low-molecular-weight cellulose ether may help regulate the viscosity and fluidity of the gel, etc. The combination of β-glucan and cellulose ether in a specific weight ratio can facilitate the use of the composition (for example, in the form of spraying), and promote the transformation of the composition into a gel state, thereby playing a barrier role.

[0024] According to some embodiments of the present invention, the cyclodextrin derivative is selected from at least one of α-cyclodextrin, glucosyl-α-cyclodextrin, maltosyl-α-cyclodextrin, β-cyclodextrin, methyl-β-cyclodextrin, dimethyl-β-cyclodextrin, hydroxyethyl-β-cyclodextrin, hydroxypropyl-β-cyclodextrin, carboxymethyl-β-cyclodextrin, glucosyl-β-cyclodextrin, maltosyl-β-cyclodextrin, γ-cyclodextrin, methyl-γ-cyclodextrin, and hydroxypropyl-γ-cyclodextrin.

[0025] According to some embodiments of the present invention, the composition further comprises 0.01 wt% to 50 wt% excipients, for example, 5 wt% to 10 wt% excipients.

[0026] According to some embodiments of the present invention, the excipients are selected from at least one of the following i-v:

[0027] i. 0.01 wt% to 10 wt% thickener;

[0028] ii. 0.01 wt% to 10 wt% auxiliary gel promoter;

[0029] iii. 0.01 wt% to 15 wt% isotonic agent;

[0030] iv. 0.01 wt% to 10 wt% pH regulator;

[0031] v. 0.01 wt% to 10 wt% preservative.

[0032] According to some embodiments of the present invention, when the excipient includes a thickener, the thickener accounts for 0.01 wt% to 10 wt% of the weight of the composition, for example, 0.01 wt% to 8 wt%, 0.01 wt% to 5 wt%, 0.01 wt% to 1 wt%, 0.05 wt% to 5 wt%, 0.05 wt% to 2 wt%, 0.1 wt% to 10 wt%, 0.1 wt% to 5 wt%, 0.5 wt% to 2 wt%. The thickener is selected from at least one of xanthan gum, carbomer, carrageenan, gelatin, fish glue, sodium alginate, agar, guar gum, konjac gum, locust bean gum, pectin, and starch.

[0033] According to some preferred embodiments of the present invention, the carbomer is selected from at least one of carbomer 940, carbomer 941, carbomer 980, carbomer 934, carbomer 1242, carbomer AQUASF-1, and carbomer ETD2020. Carbomer has good adhesiveness and film-forming properties, which can enhance the adhesiveness of the composition in the nasal cavity, throat, adenoids, etc., prolong the residence time of the composition at the lesion site, and thus improve the curative effect.

[0034] According to some embodiments of the present invention, when the excipient includes an auxiliary gel promoter, the auxiliary gel promoter accounts for 0.01 wt% to 10 wt% of the weight of the composition, for example, 0.01 wt% to 8 wt%, 0.01 wt% to 5 wt%, 0.01 wt% to 1 wt%, 0.05 wt% to 5 wt%, 0.05 wt% to 2 wt%, 0.1 wt% to 10 wt%, 0.1 wt% to 5 wt%. The auxiliary gel promoter is selected from at least one of citric acid, sodium citrate, malic acid, fumaric acid, acetic acid, sodium acetate, tartaric acid, lactic acid, potassium dihydrogen phosphate, dipotassium hydrogen phosphate, disodium hydrogen phosphate, and sodium dihydrogen phosphate.

[0035] According to some embodiments of the present invention, when the excipient includes an isotonic agent, the isotonic agent accounts for 0.01 wt% to 15 wt% of the weight of the composition, such as 0.01 wt% to 10 wt%, 0.01 wt% to 8 wt%, 0.01 wt% to 5 wt%, 0.01 wt% to 1 wt%, 0.1 wt% to 15 wt%, 0.1 wt% to 10 wt%, 0.1 wt% to 5 wt%, 1 wt% to 15 wt%, 1 wt% to 10 wt%, 1 wt% to 6 wt%, 1 wt% to 4 wt%. The isotonic agent is selected from at least one of sodium chloride, glycerol, sodium bisulfite, benzalkonium chloride, fructose, sodium citrate, crystalline sodium dihydrogen phosphate, sodium hydroxide, D-sorbitol solution, nicotinamide, thick glycerol, propylene glycol, benzyl alcohol, boric acid, borax, polyethylene glycol 4000, sodium phosphate hydroxide, potassium dihydrogen phosphate, and sodium dihydrogen phosphate.

[0036] According to some embodiments of the present invention, when the excipient includes a pH regulator, the pH regulator accounts for 0.01 wt% to 10 wt% of the weight of the composition, such as 0.01 wt% to 8 wt%, 0.01 wt% to 5 wt%, 0.01 wt% to 1 wt%, 0.05 wt% to 5 wt%, 0.05 wt% to 2 wt%, 0.1 wt% to 10 wt%, 0.1 wt% to 5 wt%, 0.5 wt% to 5 wt%. The pH regulator includes triethanolamine.

[0037] According to some embodiments of the present invention, when the excipient includes a preservative, the preservative accounts for 0.01 wt% to 10 wt% of the weight of the composition, such as 0.01 wt% to 8 wt%, 0.01 wt% to 5 wt%, 0.01 wt% to 1 wt%, 0.05 wt% to 5 wt%, 0.05 wt% to 2 wt%, 0.1 wt% to 10 wt%, 0.1 wt% to 5 wt%. The preservative is selected from at least one of sodium methylparaben, sodium ethylparaben, and sodium propylparaben.

[0038] According to some embodiments of the present invention, the composition comprises the following components:

[0039] 0.05 wt% to 10 wt% β-glucan;

[0040] 0.1 wt% to 15 wt% cellulose ether;

[0041] 0.01 wt% to 2 wt% ectoin;

[0042] 0.5 wt% to 5 wt% cyclodextrin derivative;

[0043] 0.1 wt% to 5 wt% thickener;

[0044] 1 wt% to 15 wt% of isotonic agent;

[0045] 0.1 wt% to 10 wt% of pH regulator.

[0046] According to some embodiments of the present invention, the composition further comprises an appropriate amount of water.

[0047] The administration route of the composition of the present invention can be an injection, an oral preparation or a topical preparation as needed according to different patients and symptoms. Specifically, examples include nasal drops, gels, ointments, creams, lotions, sprays, liquid preparations, nasal sprays, aerosols, jellies, cataplasms, patches, plasters, suspensions, emulsions, injections, mouthwashes, tablets, pills, capsules, granules, powders, etc. Any of these preparations can be prepared by conventional or well-known methods. Preferred are sprays, nasal drops, mouthwashes, gels, lotions; more preferably sprays.

[0048] In a second aspect of the present invention, there is provided a method for preparing the above composition, comprising the following steps:

[0049] Mix the β-glucan, cellulose ether, ectoin, and cyclodextrin derivative in proportion; if there are the excipients and / or water, add the excipients and / or water during the mixing process, and mix to obtain the composition.

[0050] The present invention does not particularly limit the temperature and time of mixing, which can be appropriately adjusted according to the different added components. For example, the mixing temperature can be 20°C to 80°C, and the mixing time can be 5 min to 60 min.

[0051] The composition of the present invention can be further processed to prepare different dosage forms, and the processing technology can adopt the conventional processes in the art, which is not particularly limited herein. For example, the composition of the present invention can be vacuum degassed and cooled to obtain a gel; or filtered through a 0.22 μm filter membrane, sterilized, subpackaged, and filled to obtain a spray.

[0052] In a third aspect of the present invention, there is provided the use of the above composition in the preparation of a medicament for 1) removing allergens in the throat and adenoids, or 2) relieving, preventing and / or treating throat and adenoid inflammations.

[0053] In a fourth aspect of the present invention, there is provided a product comprising the above composition.

[0054] The product described in the present invention can be a drug or a medical device; when the product is a drug, the drug further includes pharmaceutically acceptable excipients, and the excipients include, but are not limited to, at least one of diluents, fillers, binders, absorption promoters, surfactants, adsorption carriers, lubricants, and flavoring agents. The diluent can be commonly used in the art and includes at least one of calcium sulfate, calcium bicarbonate, and calcium carbonate; the filler can be commonly used in the art and includes at least one of starch, sucrose, and lactose; the binder can be commonly used in the art and includes at least one of cellulose derivatives, alginates, gelatin, and polyvinylpyrrolidone; the absorption promoter can be a quaternary ammonium compound commonly used in the art; the surfactant can be cetyl alcohol commonly used in the art; the adsorption carrier can be commonly used in the art and includes at least one of kaolin or saponite clay; the lubricant can be commonly used in the art and includes at least one of talc, calcium stearate, magnesium stearate, and polyethylene glycol; the flavoring agent can be commonly used in the art and includes at least one of rose oil, rose essence, lemon oil, lemon essence, vanilla essence, vanillin, banana essence, pineapple essence, peppermint oil, orange peel oil, and apple essence.

[0055] According to some embodiments of the present invention, it has at least the following beneficial effects:

[0056] On the one hand, the composition provided by the present invention can act as a barrier to exogenous allergens and effectively remove allergens in the throat and adenoid regions. On the other hand, it can also relieve the edema in the throat and adenoid regions and significantly improve or relieve the inflammation in the throat and adenoid regions. In addition, the composition of the present invention does not contain drug ingredients, so it will not produce toxic and side effects, and has the advantages of safety, effectiveness, convenient use, wide application range, and low cost.

[0057] Other features and advantages of the present invention will be described in the following specification, and, in part, will be obvious from the specification, or will be understood by practicing the present invention. Detailed Embodiments

[0058] The following will clearly and completely describe the concept and technical effects generated by the present invention in combination with the embodiments to fully understand the purpose, features, and effects of the present invention. Obviously, the described embodiments are only a part of the embodiments of the present invention, rather than all embodiments. Other embodiments obtained by those skilled in the art based on the embodiments of the present invention without creative efforts shall fall within the scope of protection of the present invention.

[0059] For those not specified in the embodiments, they are carried out according to conventional conditions or the conditions recommended by the manufacturer. For reagents or instruments not specified by the manufacturer, they are all conventional products that can be obtained through commercial purchase.

[0060] When a numerical range is disclosed herein, the above range is considered continuous and includes the minimum and maximum values of the range, as well as each value therebetween. Further, when the range refers to integers, each integer between the minimum and maximum values of the range is included. In addition, when multiple ranges are provided to describe features or characteristics, the ranges may be combined. In other words, unless otherwise specified, all ranges disclosed herein should be understood to include any and all sub-ranges subsumed therein.

[0061] Unless otherwise specified, "about" in the present invention means an allowable error within ±10%.

[0062] Unless otherwise specified, the β-glucan used in the examples and comparative examples of the present invention is yeast β-glucan, with a weight average molecular weight of about 1.2 million Da, consisting of about 85% β-(1,3) glycosidic bonds as the main chain and about 15% β-(1,6) glycosidic bonds as the side chains.

[0063] Unless otherwise specified, the weight average molecular weight of the hydroxypropyl methylcellulose used in the examples and comparative examples of the present invention is about 18 kDa, wherein the mass percentage content of methoxy groups is about 28.5%, and the mass percentage content of hydroxypropyl groups is about 8%. It is purchased from Huzhou Outlook Pharmaceutical Co., Ltd.

[0064] The hydroxypropyl cellulose, hydroxypropyl carboxymethyl cellulose in the examples of the present invention are similar to hydroxypropyl methylcellulose, and the mass percentage content of hydroxypropyl groups is about 8%.

[0065] Example 1

[0066] This example provides a spray containing the following components:

[0067] β-glucan 3 g;

[0068] Hydroxypropyl methylcellulose 5 g;

[0069] Carbomer 941 1 g;

[0070] Sodium chloride 3 g;

[0071] Ectoin 2 g;

[0072] Hydroxypropyl β-cyclodextrin 1 g;

[0073] Propylene glycol 2 g;

[0074] Triethanolamine 0.5 g;

[0075] Sodium methylparaben 0.01 g;

[0076] Add purified water to 100 g.

[0077] The preparation method of the spray includes the following steps:

[0078] Add β-glucan, hydroxypropyl methylcellulose, ectoin, and sodium methylparaben to purified water, and stir at room temperature for 30 min; continue to add carbomer 941, hydroxypropyl-β-cyclodextrin, and sodium chloride, and stir for 10 min until uniform. Finally, add triethanolamine and propylene glycol, and stir for 5 min to obtain a mixed solution. After filtering through a 0.2-μm filter membrane, sterilizing, sub-packaging, and filling, the spray is obtained.

[0079] Example 2

[0080] This example provides a spray containing the following components:

[0081] β-glucan 4 g;

[0082] Hydroxypropyl methylcellulose 5 g;

[0083] Carbomer 941 1 g;

[0084] Sodium chloride 4 g;

[0085] Ectoin 1.5 g;

[0086] Hydroxypropyl-β-cyclodextrin 1 g;

[0087] Propylene glycol 1.5 g;

[0088] Benzyl alcohol 1.5 g;

[0089] Triethanolamine 1 g;

[0090] Sodium methylparaben 0.01 g;

[0091] Add purified water to 100 g.

[0092] The preparation method of the spray refers to that in Example 1.

[0093] Example 3

[0094] This example provides a spray containing the following components: β-glucan 2 g;

[0095] Hydroxypropyl methylcellulose 3.5 g;

[0096] Carbomer 940 0.8 g;

[0097] Sodium chloride 2.5 g;

[0098] Ectoin 1 g;

[0099] Hydroxypropyl-β-cyclodextrin 1.5 g;

[0100] Triethanolamine 2 g;

[0101] Sodium methylparaben 0.02 g;

[0102] Add purified water to make 100 g.

[0103] The preparation method of this spray is referred to that in Example 1.

[0104] Example 4

[0105] This example provides a spray containing the following components: β-glucan 6 g;

[0106] Hydroxypropyl cellulose 8 g;

[0107] Carbomer 934 0.5 g;

[0108] Sodium chloride 0.5 g;

[0109] Ectoin 1.2 g;

[0110] Glucosyl β-cyclodextrin 1 g;

[0111] Propylene glycol 1.0 g;

[0112] Benzyl alcohol 2.0 g;

[0113] Triethanolamine 1.2 g;

[0114] Sodium methylparaben 0.02 g;

[0115] Add purified water to make 100 g.

[0116] The preparation method of this spray is referred to that in Example 1.

[0117] Example 5

[0118] This example provides a spray containing the following components:

[0119] β-glucan 10 g;

[0120] Hydroxypropyl carboxymethyl cellulose 12 g;

[0121] Carbomer 940 0.5 g;

[0122] Glycerol 1.5 g;

[0123] Ectoin 1.2 g;

[0124] Dimethyl β-cyclodextrin 1 g;

[0125] Benzyl alcohol 2.0 g;

[0126] Triethanolamine 1 g;

[0127] Sodium methylparaben 0.02 g;

[0128] Add purified water to make up 100 g.

[0129] The preparation method of this spray is referred to that in Example 1.

[0130] Comparative Example 1

[0131] This comparative example provides a spray. Referring to Example 2, the only difference is that it does not contain hydroxypropyl methylcellulose and the mass fraction of β-glucan is 9 parts.

[0132] The preparation method of this spray is referred to that in Example 1.

[0133] Comparative Example 2

[0134] This comparative example provides a spray. Referring to Example 2, the only difference is that it does not contain hydroxypropyl-β-cyclodextrin and the mass fraction of ectoine is 2.5 parts;

[0135] The preparation method of this spray is referred to that in Example 1.

[0136] Comparative Example 3

[0137] This comparative example provides a spray. Referring to Example 2, the only difference is that hydroxypropyl methylcellulose is replaced by methylcellulose (weight-average molecular weight is about 10 kDa) and the weight-average molecular weight of β-glucan is about 50 kDa.

[0138] The preparation method of this spray is referred to that in Example 1.

[0139] Test Example 1

[0140] 1. Test method

[0141] 1.1 Test animals

[0142] A total of 42 Sprague-Dawley rats at about 6 weeks old, with body weight (210 ± 25 g), half male and half female, were purchased from Hunan Slack Jingda Experimental Animal Co., Ltd. The cages and utensils for raising rats were strictly disinfected. The rats were allowed to freely eat and drink purified water, and were fed with conventional laboratory rat maintenance feed without any drugs.

[0143] 1.2 Animal model of allergic pharyngitis

[0144] For the model group, in the first two weeks of the experiment, every other day (i.e., on the 1st, 3rd, 5th, 7th, 9th, 11th, and 13th days), SD rats were sensitized by intraperitoneal injection of 300 μg ovalbumin (OVA), 25 mg aluminum hydroxide, and 1 mL normal saline. Then, from the 15th day to the 23rd day, every other day (i.e., on the 15th, 17th, 19th, 21st, and 23rd days), the pharynx of SD rats was sensitized by injecting 30 mg OVA and 1 mL normal saline into the pharynx of SD rats (expanding the rat's mouth to expose the posterior pharyngeal wall and injecting the OVA solution into the rat's pharynx in small amounts and multiple times).

[0145] Differently, in the first two weeks of the experiment, SD rats in the normal group were intraperitoneally injected with 1 mL normal saline, and then from the 15th day to the 23rd day, normal saline was injected into the pharynx of SD rats (the dose was the same as that in the model group).

[0146] 1.3. Experimental grouping

[0147] 42 SD rats were randomly divided into 7 groups, namely: normal group, model group, Example 1 group, Example 2 group, Comparative Example 1 group, Comparative Example 2 group, and Comparative Example 3 group; 6 rats in each group.

[0148] 1.4. Drug administration plan

[0149] On the 24th day of the experiment, drug administration treatment began. The SD rats in Example 1 and Example 2 groups were respectively administered the sprays prepared in Example 1 and Example 2, once a day, 2 mg each time, for 3 consecutive weeks. The SD rats in Comparative Example 1, Comparative Example 2, and Comparative Example 3 groups were respectively administered the sprays prepared in Comparative Example 1, Comparative Example 2, and Comparative Example 3, once a day, 2 mg each time, for 3 consecutive weeks; the SD rats in the normal group were not given any treatment measures; the SD rats in the model group were administered normal saline, once a day, with the same dose as that in the Example group or the Comparative Example group, for 3 consecutive weeks.

[0150] 1.5. Detection indexes

[0151] Allergic pharyngitis is an inflammatory reaction of allergen invasion and aggregation that occurs in the throat tissues of specific individuals, and the main clinical features are symptoms such as itchy throat accompanied by irritating and paroxysmal dry cough. Therefore, after the last drug administration, the scratching of the mouth and nose, respiratory state, and pharyngeal manifestations of SD rats within half an hour were recorded.

[0152] In addition, 2 hours after the last drug administration, the rats were anesthetized with urethane, blood was taken from the abdominal aorta, left to stand at room temperature for 2 hours, centrifuged at 5000 r / min for 15 minutes (4 °C), the supernatant was taken, and according to the manufacturer's instructions, an ELISA kit was used to measure the levels of inflammation-related factors TNF-α and IL-4, and IgE in the rat serum.

[0153] 2. Test results and discussion

[0154] 2.1 Scratching the oropharynx

[0155] As shown in Table 1, after administration, the number of times of scratching the oropharynx in the SD rats of Example 1, 2 groups and Comparative Example 1-3 groups was significantly lower than that in the model group; especially, the condition of scratching the oropharynx in the rats of Example 1 and 2 groups was significantly improved, and the number of times of scratching the oropharynx in the SD rats was comparable to that in the normal group rats.

[0156] Table 1 Number of times of scratching the oropharynx in each group of SD rats

[0157] Scratching times of oropharynx in SD rats (times) Example 1 group 2.33±0.82 Example 2 group 1.83±0.75 Comparative Example 1 group 4.83±1.47 Comparative Example 2 group 3.67±0.82 Comparative Example 3 group 5.00±0.63 Normal group 2.00±0.89 Model group 9.50±1.05

[0158] 2.2 Respiratory condition

[0159] As shown in Table 2, the breathing of the rats in Example 1, 2 groups and the normal group was relatively gentle, the breath sound was relatively light, and the observed contraction amplitude of the abdomen was relatively small; after administration, the breathing of the SD rats in Comparative Example 1-3 groups was relatively rapid, the breath sound was relatively heavy, and the observed contraction amplitude of the abdomen was relatively large.

[0160] Table 2 Respiratory condition

[0161]

[0162] 2.3 Pharyngeal manifestation condition

[0163] As shown in Table 3, the surface of the pharyngeal tissue of the rats in the normal group was shiny, the saliva secretion volume was relatively small, and there was no redness and swelling; the pharyngeal tissues of the rats in Example 1 and 2 groups showed slight redness and swelling; the surface of the pharyngeal tissues of the SD rats in Comparative Example 1-3 groups was poorly shiny, the saliva secretion volume increased compared with the normal group, and there were redness, swelling and congestion in the pharynx; the pharyngeal tissues of the rats in the model group showed dark red, the saliva secretion volume increased significantly compared with the normal group, the pharynx was severely red and swollen, and there were local ulcers.

[0164] Table 3 Pharyngeal manifestation condition

[0165]

[0166]

[0167] 2.4 Levels of TNF-α, IL-4 and IgE in the sera of rats in each group

[0168] As shown in Table 4, after administration, the levels of TNF-α, IL-4 and IgE in the sera of the SD rats in Example 1, 2 groups and Comparative Example 1-3 groups were significantly lower than those in the model group; and the levels of TNF-α, IL-4 and IgE in the sera of the rats in Example 1 and 2 groups were significantly lower than those in Comparative Example 1-2 groups and were closer to those of the normal group rats.

[0169] Serum TNF-α, IL-4 and IgE levels of rats in each group in Table 4

[0170] TNF-α level (ng / mL) IL-4 level (pg / mL) IgE (ng / mL) Example 1 group 182.4±13.7 22.6±0.8 1.4±0.2 Example 2 group 159.2±10.6 19.8±1.5 1.3±0.3 Comparative Example 1 group 251.5±30.9 39.0±5.1 3.5±0.8 Comparative Example 2 group 217.1±12.8 31.5±5.3 3.4±1.2 Comparative Example 3 group 283.3±7.4 36.4±3.3 4.0±1.9 Normal group 109.7±14.6 11.6±2.1 1.1±0.4 Model group 359.5±20.9 58.3±8.7 5.1±0.9

[0171] Test Example 2

[0172] The sprays prepared in Example 1, Example 2 and Comparative Example 2 were dyed with edible indigo. Twelve mild pharyngitis volunteers were selected (among them, 7 males and 5 females, aged 18 - 40 years, and the pharyngitis symptoms were all manifested as pharyngeal swelling, bright red mucosa, etc.). According to age, gender and condition, the volunteers were divided into 3 groups with 4 people in each group. Each group was respectively administered the sprays prepared in Example 1, Example 2 or Comparative Example 2, 2 sprays per person (60 μg / spray), and the staining conditions of the volunteers' throats were observed. The proportion of the number of volunteers with a staining duration of more than 1 h was counted. The results are shown in Table 5.

[0173] Table 5

[0174] Total number of people Detected number of people Proportion of people Example 1 group 4 4 100％ Example 2 group 4 4 100％ Comparative Example 2 group 4 2 50％

[0175] The more the proportion of the number of staining cases, the longer the residence time of the spray in the throat. It can be seen from the above data that the sprays of Example 1 and Example 2 of the present invention can stay in the throat for a relatively long time, while the spray prepared in Comparative Example 2 has a relatively short residence time. In addition, no irritation or other reactions of the volunteers were observed during the detection, indicating that the sprays of the examples and the comparative examples all have good safety.

[0176] In addition, the sprays of Examples 3 - 5 have similar or equivalent effects to the sprays of Examples 1 and 2 in removing allergens in the throat and adenoids and relieving inflammation in the throat and adenoid areas.

[0177] The above content has described the embodiments of the present invention in detail. However, the present invention is not limited to the above embodiments. Within the knowledge scope of those of ordinary skill in the art, various changes can be made without departing from the gist of the present invention. In addition, without conflict, the embodiments of the present invention and the features in the embodiments can be combined with each other.

Claims

1. A composition capable of effectively removing allergens in the throat and adenoids and relieving inflammation, characterized in that, The composition comprises 0.01 wt% - 10 wt% β-glucan, 0.05 wt% - 15 wt% cellulose ether, 0.01 wt% - 2 wt% ectoin, and 0.01 wt% - 10 wt% cyclodextrin derivative; Among them, the weight-average molecular weight of the β-glucan is ≥80 kDa; The cellulose ether contains hydroxypropyl, and the content of hydroxypropyl in the cellulose ether is 6% - 12%.

2. The composition according to claim 1, wherein The β-glucan is yeast β-glucan.

3. The composition according to claim 1, wherein The cellulose ether is selected from at least one of hydroxypropyl cellulose, hydroxypropyl methyl cellulose, hydroxypropyl ethyl cellulose, and hydroxypropyl carboxymethyl cellulose; and / or, the weight-average molecular weight of the cellulose ether is 4 - 20 kDa.

4. The composition according to claim 1, wherein The cyclodextrin derivative is selected from at least one of α-cyclodextrin, glucosyl-α-cyclodextrin, maltosyl-α-cyclodextrin, β-cyclodextrin, methyl-β-cyclodextrin, dimethyl-β-cyclodextrin, hydroxyethyl-β-cyclodextrin, hydroxypropyl-β-cyclodextrin, carboxymethyl-β-cyclodextrin, glucosyl-β-cyclodextrin, maltosyl-β-cyclodextrin, γ-cyclodextrin, methyl-γ-cyclodextrin, and hydroxypropyl-γ-cyclodextrin.

5. The composition according to any one of claims 1 to 4, characterized in that, The composition further comprises 0.01 wt% - 50 wt% excipients; Preferably, the excipients are selected from at least one of i - v: i. 0.01 wt% - 10 wt% thickener; ii. 0.01 wt% - 10 wt% auxiliary gel promoter; iii. 0.01 wt% - 15 wt% isotonic agent; iv. 0.01 wt% - 10 wt% pH regulator; v. 0.01 wt% - 10 wt% preservative.

6. The composition according to claim 5, characterized in that, The thickener is selected from at least one of xanthan gum, carbomer, carrageenan, gelatin, fish glue, sodium alginate, agar, guar gum, konjac gum, locust bean gum, pectin, and starch; and / or, The auxiliary gel promoter is selected from at least one of citric acid, sodium citrate, malic acid, fumaric acid, acetic acid, sodium acetate, tartaric acid, lactic acid, potassium dihydrogen phosphate, dipotassium hydrogen phosphate, disodium hydrogen phosphate, and sodium dihydrogen phosphate; and / or, The isotonic agent is selected from at least one of sodium chloride, glycerol, sodium bisulfite, benzalkonium chloride, fructose, sodium citrate, crystalline sodium dihydrogen phosphate, sodium hydroxide, D-sorbitol solution, nicotinamide, concentrated glycerol, propylene glycol, benzyl alcohol, boric acid, borax, polyethylene glycol 4000, sodium phosphate hydroxide, potassium dihydrogen phosphate, and sodium dihydrogen phosphate; and / or, The pH regulator includes triethanolamine; and / or, The preservative is selected from at least one of sodium methylparaben, sodium ethylparaben, and sodium propylparaben.

7. The composition according to claim 1, wherein The dosage form of the composition is spray, nasal drops, gel, ointment, cream, lotion, liquid preparation, nasal spray, aerosol, jelly, cataplasm, patch, plaster, suspension, emulsion, injection, mouthwash, tablet, pill, capsule, granule, or powder.

8. A method for preparing a composition according to any one of claims 1 to 7, characterized in that, Comprising the following steps: Mix the β-glucan, cellulose ether, ectoin, and cyclodextrin derivative in proportion; if there are the excipients and / or water, add the excipients and / or water during the mixing process, and mix to obtain.

9. Use of a composition according to any one of claims 1 to 7 in the preparation of a medicament for 1) removing allergens in the throat and adenoids, or 2) relieving, preventing and / or treating throat and adenoid inflammation.

10. A product, characterized in that, Comprising the composition according to any one of claims 1 to 7 or the composition prepared by the preparation method according to claim 8.

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