Oral use of the product

Abstract

The embodiment of the present application provides a kind of oral preparation, wherein the oral preparation provided by the embodiment of the present application includes functional layer, functional layer includes active substance, sweetening agent, cooling agent and mucous membrane protective agent.Therein, by using mucous membrane protective agent in functional layer, the stimulation of cooling agent, sweetening agent to oral mucosa is reduced, the care to gum is realized and the repair protection to gum is carried out, to improve the problem that existing oral preparation is prone to too intense oral stimulation due to flavor substance, improve user experience.

Description

Technical Field

[0001] This application belongs to the field of oral product technology, specifically relating to a sublingual product. Background Technology

[0002] Oral lozenges allow smokers to absorb active ingredients directly through the oral mucosa, helping them alleviate cravings. Compared to regular tobacco products, they reduce the intake of harmful substances such as tar and carbon monoxide, making them a healthier option for smokers trying to quit.

[0003] Oral products using related technologies often contain flavor additives such as cooling agents and sweeteners at high concentrations, which can easily cause chemical irritation to the oral cavity, gums, and mucous membranes, leading to stinging, dryness, or discomfort, and affecting the customer experience. Summary of the Invention

[0004] The technical problem to be solved by this application is to provide a mouthwash to improve the problem that existing mouthwashes are prone to causing excessive oral irritation due to flavor substances.

[0005] To address the aforementioned problems, this application provides the following technical solution: This application discloses a mouth-held product comprising a functional layer, the functional layer including an active substance, a sweetener, a cooling agent, and a mucosal protectant, wherein the mucosal protectant includes a first protectant and a second protectant, the first protectant including a moisturizing substance, and the second protectant including natural components.

[0006] Furthermore, in the oral product, the mucosal protectant includes at least one of sodium hyaluronate, β-glucan, panthenol, trehalose, aloe vera gel, polyglutamic acid, honeysuckle extract, dipotassium glycyrrhizate, centella asiatica extract, and tea polyphenols.

[0007] Furthermore, in the oral product, the first protective agent includes at least one of sodium hyaluronate, β-glucan, panthenol, trehalose, aloe vera gel, and polyglutamic acid, and the second protective agent includes at least one of honeysuckle extract, dipotassium glycyrrhizate, centella asiatica extract, and tea polyphenols.

[0008] Furthermore, in the oral product, the functional layer comprises, by weight parts: The active substance comprises 0.3 to 0.8 parts, the sweetener comprises 5 to 8 parts, the cooling agent comprises 0.1 to 0.3 parts, the first protective agent comprises 0.5 to 1.2 parts, and the second protective agent comprises 0.3 to 0.8 parts.

[0009] Furthermore, in the oral product, the functional layer further includes at least one of a humectant, a film-forming agent, a substrate, a pH adjuster, a flow aid, and a fragrance.

[0010] Furthermore, in the oral product, the moisturizer includes at least one of glycerin, propylene glycol, hyaluronic acid, and microcrystalline cellulose.

[0011] Furthermore, in the oral product, the film-forming agent includes at least one of hydroxypropyl cellulose, hydroxypropyl methylcellulose, polyoxyethylene, sodium alginate, carbomer, sodium carboxymethyl cellulose, ethyl cellulose, and polyvinyl alcohol.

[0012] Furthermore, in the oral product, the active substance includes at least one of nicotine and nicotine derivatives; and / or, The substrate includes at least one of pectin, gum arabic, gelatin, starch, and xanthan gum; and / or, The pH adjuster includes at least one of sodium bicarbonate, sodium carbonate, and sodium citrate; and / or, The sweetener comprises at least one of xylitol, sorbitol, mannitol, iodine, lactitol, maltitol, isomaltitol, hydrogenated starch hydrolysate, erythritol, maltotriol, aspartame, acesulfame potassium, sodium saccharin, sucralose, neotame, cyclamate, alitane, steviol glycosides, arabinitol, and monk fruit sweetener; and / or, The cooling agent includes at least one of menthol, N-ethyl-2-isopropyl-5-methylcyclohexaneformamide, menthyl lactate, menthyl acetate, and menthone glycerol ketal; The flow aid includes at least one of silica, talc, dicalcium phosphate, tricalcium phosphate, and magnesium stearate.

[0013] Furthermore, the oral article also includes a support layer that covers at least one surface of the functional layer.

[0014] Furthermore, the support layer is used to cover the oppositely disposed two surfaces of the functional layer; and / or, The support layer has at least a permeable portion, which can be used to permeate saliva.

[0015] Furthermore, in the oral article, the functional layer includes at least a first sub-functional layer and a second sub-functional layer.

[0016] Furthermore, in the oral article, a carrier layer is provided between the first sub-functional layer and the second sub-functional layer.

[0017] Furthermore, in the oral article, the carrier layer is a non-woven fabric; and / or, The thickness of the carrier layer is 0.3~0.5 mm; and / or, The carrier layer includes hydroxypropyl methylcellulose.

[0018] Compared with the prior art, the embodiments of this application have the following advantages: In this embodiment, the provided oral product includes a functional layer comprising active substances, sweeteners, cooling agents, and a mucosal protectant. The mucosal protectant includes a first protectant and a second protectant; the first protectant includes a moisturizing substance, and the second protectant includes natural components. By using a mucosal protectant comprising the first and second protectants in the functional layer, the irritation of the cooling agents and sweeteners to the oral mucosa is reduced, thus protecting and repairing the gums. This addresses the problem of existing oral products easily causing excessive oral irritation due to flavor substances, improving the user experience.

[0019] It should be understood that the above general description and the following detailed description are exemplary and explanatory only, and do not limit this application. Attached Figure Description

[0020] Figure 1 This is a schematic diagram of the structure of an oral article provided in an embodiment of this application; Figure 2 This is another structural schematic diagram of the oral article provided in the embodiments of this application. Detailed Implementation

[0021] To make the above-mentioned objectives, features and advantages of this application more apparent and understandable, the application will be further described in detail below with reference to the accompanying drawings and specific embodiments.

[0022] The terms "first" and "second" in the specification and claims of this application may explicitly or implicitly include one or more of the features. In the description of this application, unless otherwise stated, "multiple" means two or more. Furthermore, "and / or" in the specification and claims indicates at least one of the connected objects, and the character " / " generally indicates that the preceding and following objects are in an "or" relationship.

[0023] The inventors discovered that oral products often contain flavor additives such as cooling agents and sweeteners at high concentrations, which can easily cause chemical irritation to the oral cavity, gums, and mucous membranes, leading to stinging, dryness, or discomfort, thus affecting the customer experience. Most related technologies only alleviate irritation by reducing the content of flavor additives, which has limited irritation relief and cannot repair or protect the gums, seriously affecting the customer experience.

[0024] In response to the above problems, such as Figure 1As shown in Figure 2, this application provides an oral product 100 including a functional layer 10. The functional layer 10 includes an active substance, a sweetener, a cooling agent, and a mucosal protectant. The mucosal protectant includes a first protectant and a second protectant. The first protectant includes a moisturizing substance, and the second protectant includes natural components.

[0025] In this embodiment, the active substance is a component that can help smokers alleviate withdrawal symptoms and can be directly absorbed through the oral mucosa. By using a mucosal protectant including a first protectant and a second protectant in the functional layer, the first protectant includes a moisturizing substance and the second protectant includes natural components, the irritation of cooling agents and sweeteners to the oral mucosa can be reduced, thereby protecting and repairing the gums. This improves the problem that existing oral products are prone to causing excessive oral irritation due to flavor substances, and enhances the user experience.

[0026] In some embodiments, the active substance includes at least one of nicotine and nicotine derivatives. Nicotine includes natural nicotine and / or synthetic nicotine, and nicotine derivatives include one or more of nicotine salts, nicotine in a matrix such as a glycobase or organometallic complex, nicotine-resin combinations, nicotine inclusion complexes, and non-covalently bound nicotine. Non-covalently bound nicotine includes nicotine lactate, nicotine malate, nicotine salicylate, nicotine cyclodextrin-encapsulated complexes, nicotine hydrochloride, nicotine dihydrochloride, nicotine tartrate, nicotine tartrate dihydrate, nicotine sulfate, nicotine zinc chloride, and nicotine benzoate. Nicotine derivatives also include nicotine containing substituents, such as one or more mixtures of 6-methylnicotine, 6-methylnicotine lactate, 6-methylnicotine malate, 6-methylnicotine salicylate, 6-methylnicotine cyclodextrin encapsulated complex, 6-methylnicotine hydrochloride, 6-methylnicotine dihydrochloride, 6-methylnicotine tartrate, 6-methylnicotine tartrate dihydrate, 6-methylnicotine sulfate, 6-methylnicotine zinc chloride, and 6-methylnicotine benzoate.

[0027] The aforementioned active substances can not only dissolve rapidly in the oral cavity, releasing active substances to help smokers alleviate withdrawal symptoms, but also achieve a long-lasting and continuous stimulating effect.

[0028] In some implementations, to meet various user needs, the active substance may include substances with specific medical properties; the active substance may include substances with specific active properties, such as caffeine, theophylline, capsaicin, etc.

[0029] In some embodiments, the above-mentioned mucosal protectant includes at least one of sodium hyaluronate, β-glucan, panthenol, trehalose, aloe vera gel, polyglutamic acid, honeysuckle extract, dipotassium glycyrrhizate, centella asiatica extract, and tea polyphenols, which can effectively reduce the irritation of the oral mucosa by cooling agents, sweeteners, etc., while adding natural ingredients to achieve gum care.

[0030] In some embodiments, the first protective agent includes at least one of sodium hyaluronate, β-glucan, panthenol, trehalose, and polyglutamic acid, which can form a moisturizing protective film on the gingival surface and relieve oral dryness.

[0031] The second protective agent includes natural ingredients, which are more conducive to gum care. In some embodiments, the aforementioned second protective agent includes at least one of the following: aloe vera gel, honeysuckle extract, dipotassium glycyrrhizate, centella asiatica extract, and tea polyphenols. It has a soothing effect and can reduce the incidence of gum redness and stinging, resulting in a reduction of oral irritation and discomfort scores by more than 60%.

[0032] In some implementations, the functional layer includes, by mass parts: 0.3-0.8 parts of active substance, 5-8 parts of sweetener, 0.1-0.3 parts of cooling agent, 0.5-1.2 parts of primary protectant, and 0.3-0.8 parts of secondary protectant.

[0033] In this embodiment, while reducing the content of sweeteners and cooling agents in the oral product, the addition of a first protective agent and a second protective agent not only directly reduces chemical irritation but also adds natural ingredients to protect the gums. Too much of these agents will result in a thick film that affects release and causes stickiness in the mouth; too little will prevent the formation of a complete protective film, leading to the precipitation of oily substances; and too little will fail to soothe the oral mucosa. In some embodiments, the functional layer 10 further includes at least one of a humectant, a film-forming agent, a substrate, a pH adjuster, a flow aid, and a fragrance.

[0034] The humectant, acting as a water-locking material, can fix the saliva secreted during the oral administration process, effectively preventing nicotine and additives from flowing into the stomach and throat with the saliva, thereby reducing digestive tract irritation.

[0035] Among them, film-forming agents are used to promote film formation, which can make the release curve stable, avoid the irritation caused by a sudden increase in nicotine concentration, and effectively prolong the action time of active substances.

[0036] In some embodiments, the moisturizer 10 includes at least one of glycerin, propylene glycol, hyaluronic acid, and microcrystalline cellulose. Experimental studies have shown that adding the above-mentioned moisturizer to the functional layer can reduce the incidence of gastrointestinal irritation (such as nausea and burning throat) by 70%.

[0037] In some embodiments, the film-forming agent includes at least one of hydroxypropyl cellulose, hydroxypropyl methylcellulose, polyoxyethylene, sodium alginate, carbomer, sodium carboxymethyl cellulose, ethyl cellulose, and polyvinyl alcohol, which can form a dense sustained-release layer, reduce the release rate of active substances by 50%, extend the action time from 15-20 minutes in the prior art to 30-40 minutes, and provide a stable release curve, avoiding irritation caused by a sudden increase in nicotine concentration.

[0038] The substrate serves as the framework of the functional layer. In some embodiments, the substrate includes at least one of pectin, gum arabic, gelatin, starch, and xanthan gum.

[0039] The pH adjuster not only neutralizes the irritation of acidic components and reduces the burning sensation in the mouth, maintaining a slightly alkaline environment, but also ensures that nicotine, in an alkaline environment (pH 8-9), exists in a non-ionic state, making it less prone to degradation and more easily absorbed through the oral mucosa, thus enhancing bioavailability and extending shelf life. In some embodiments, the pH adjuster includes at least one of sodium bicarbonate, sodium carbonate, and sodium citrate.

[0040] Sweeteners can mask the bitter or irritating taste of active substances such as nicotine, enhancing the palatability of the product. At the same time, sweeteners can also enhance the sense of pleasure, making the product closer to the experience of snacks or candy, reducing user resistance. In addition, sweeteners work synergistically with flavorings to enhance the expression of flavors such as fruit and mint.

[0041] In some embodiments, the sweeteners mentioned above include at least one of xylitol, sorbitol, mannitol, iodine, lactitol, maltitol, isomaltitol, hydrogenated starch hydrolysate, erythritol, maltotriol, aspartame, acesulfame potassium, sodium saccharin, sucralose, neotame, cyclamate, alitane, steviol glycosides, arabinitol, and monk fruit sweetener.

[0042] Cooling agents can enhance the user experience by simulating a cooling sensation, effectively neutralize or mask the odor of active ingredients, reduce the direct irritation of active ingredients to the oral mucosa, and reduce the burning or numbness after use.

[0043] In some embodiments, the cooling agent may include at least one of menthol, N,2,3-trimethyl-2-isopropylbutyramide (WS-23), N-ethyl-2-isopropyl-5-methylcyclohexaneformamide, menthyl lactate, menthyl acetate, and menthone glycerol ketal.

[0044] Flavorings can improve taste and flavor, mask the odor of chemicals such as tobacco or nicotine, and enhance the user experience. Meanwhile, flavorings such as mint and spicy spices can stimulate the oral mucosa, promote saliva production, and help nicotine be released and absorbed through the mouth more quickly, enhancing its effect. In addition, the diverse flavor profiles of flavorings (such as coffee, chocolate, cinnamon, etc.) can satisfy different consumer preferences and increase product appeal. The aforementioned flavoring can be a type of mint flavoring.

[0045] The flow aid includes at least one of silica, talc, dicalcium phosphate, tricalcium phosphate, and magnesium stearate, which facilitates preparation and molding.

[0046] In some embodiments, the oral article further includes a solvent, which includes at least one of water and ethanol.

[0047] In some embodiments, the functional layer 10 includes a first sub-functional layer 12 and a second sub-functional layer 13. In some embodiments, the formulations of each sub-functional layer may be the same, while in others, the formulations of the sub-functional layers may be different. Specifically, the types or concentrations of active substances, the types or concentrations of fragrances, etc., may be different, thereby independently regulating the release rates of active substances or fragrances in the first sub-functional layer 12 and the second sub-functional layer 13, which can create multiple tastes and make the stimulating layers more distinct.

[0048] In this embodiment, the types of active substances in the first sub-functional layer and the types of active substances in the second sub-functional layer 13 may be the same or different, and the relative content of active substances in the first sub-functional layer and the relative content of active substances in the second sub-functional layer may be the same or different.

[0049] The relative content of active substances in the first sub-functional layer refers to the mass fraction of active substances in the first sub-functional layer, and the relative content of active substances in the second sub-functional layer refers to the mass fraction of active substances in the second sub-functional layer.

[0050] In one implementation, the types and / or relative amounts of active substances in the first sub-functional layer differ from those in the second sub-functional layer. That is, the active substances in the first sub-functional layer are not entirely the same as those in the second sub-functional layer 13, which helps to enrich the user experience.

[0051] In this embodiment, by preparing two different functional layer membrane liquids, the first sub-functional layer and the second sub-functional layer can be designed as membrane materials with different concentrations of nicotine, different types of other active substances, or different flavors, thereby helping to enrich the user experience.

[0052] In some implementations, formulations can be designed independently for the first and second sub-functional layers, thereby independently regulating the release rates of active substances in the first and second sub-functional layers.

[0053] In some embodiments, a carrier layer 11 is provided between the first sub-functional layer 12 and the second sub-functional layer 13. That is, the first sub-functional layer 12 and the second sub-functional layer 13 are respectively disposed on the two sides of the carrier layer 11. This can prevent the first sub-functional layer 12 and the second sub-functional layer 13 on both sides from reacting with each other, and also help to prevent the collapse of the double-layer structure and maintain the clear distinction between the first sub-functional layer and the second sub-functional layer.

[0054] In some implementations, such as Figure 1 As shown, the oral product has a three-layer structure, including a first sub-functional layer 12, a carrier layer 11, and a second sub-functional layer 13 arranged sequentially.

[0055] In some embodiments, the carrier layer is a water-repellent fabric, which can effectively block the first sub-functional layer and the second sub-functional layer to prevent them from reacting.

[0056] In some embodiments, the carrier layer is a non-woven fabric with a thickness of 0.3~0.5mm, which can effectively support the first and second sub-functional layers while blocking the interaction between the first and second sub-functional layers, and at the same time slowing down the penetration rate of the active substance.

[0057] In some implementations, the thickness of the carrier layer can be one of 0.3 mm, 0.4 mm, 0.5 mm, or any value in the range of any two.

[0058] In some embodiments, the carrier layer includes hydroxypropyl methylcellulose. Specifically, the carrier layer includes a nonwoven fabric matrix, on which high-viscosity hydroxypropyl methylcellulose is compounded as a sustained-release material to encapsulate the active ingredient and reduce the release rate of the active ingredient.

[0059] In some implementations, such as Figure 2 As shown, the functional layer 10 also includes a support layer, which covers at least one side of the functional layer 10. The support layer can maintain the shape of the oral product and can also serve as an interface for direct contact with the oral mucosa, thus preventing the active substances from directly irritating the oral cavity.

[0060] In some embodiments, at least a portion of the support layer is a permeable portion that can be used to permeate saliva. This allows the support layer to maintain the shape of the oral product and also to serve as an interface for direct contact with the oral mucosa. This can prevent the active substance from directly irritating the oral cavity, while guiding saliva to permeate into the middle layer, initiating a controlled-release reaction, reducing the burning sensation in the throat and stomach, thereby improving the user experience.

[0061] In some embodiments, a support layer is used to cover the oppositely disposed two surfaces of the functional layer 10. The support layer includes a first support layer 14 and a second support layer 15, that is, the functional layer is disposed between the first support layer 14 and the second support layer 15, avoiding the functional layer from directly adhering to the application site. This not only reduces oral irritation when using soluble substances, but also makes it easy to move the oral product to the release position, avoiding excessive irritation. In addition, the first support layer and the second support layer have a water-locking function, which can lock in some saliva, reduce the burning sensation in the throat and stomach, thereby improving the user experience.

[0062] In some embodiments, the support layer includes a first support layer 14 and a second support layer 15, and the functional layer 10 includes a first sub-functional layer 12 and a second sub-functional layer 13. The first support layer 14 is disposed on the surface of the first sub-functional layer 12 facing away from the carrier layer 11, and the second support layer 15 is disposed on the surface of the second sub-functional layer 13 facing away from the carrier layer 111. That is, the oral article in the embodiments of this application is a structure of at least five layers, consisting of the first support layer 14, the first sub-functional layer 12, the carrier layer 11, the second sub-functional layer 13, and the second support layer 15 stacked in sequence.

[0063] The first and second sub-functional layers contain active substances that can be released upon contact with saliva, thereby providing a stimulating sensation. The first and second support layers have water-permeable and water-locking functions, which can lock in some saliva and reduce the burning sensation in the throat and stomach.

[0064] By placing the carrier layer between the first and second sub-functional layers, the interaction between them can be reduced, thus improving stability. Furthermore, placing the first and second sub-functional layers between the first and second support layers prevents the functional layers from directly adhering to the application site. This not only reduces oral irritation when using soluble substances but also makes it easier for the oral product to move to the release position, avoiding excessive irritation. In addition, the first and second support layers have a water-locking function, which can lock in some saliva, reducing the burning sensation in the throat and stomach, thereby improving the user experience.

[0065] In one embodiment, the first support layer has pores with a pore size of 0.01 mm to 2 mm and a porosity of 1% to 10%. This not only allows saliva to pass through to facilitate the release of active substances in the functional layer, but also has a certain water-locking function to prevent the release rate of active substances from being too rapid and causing strong irritation and oral discomfort. The pore size can be one or a range of any two of 0.01 mm, 0.02 mm, 0.05 mm, 0.1 mm, 0.2 mm, 0.5 mm, 1 mm, 1.5 mm, and 2 mm, and the porosity can be one or a range of any two of 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, and 10%.

[0066] In one embodiment, the second support layer is porous with a pore size of 0.01 mm to 2 mm and a porosity of 1% to 10%. This allows saliva to pass through, facilitating the release of active substances in the functional layer, while also providing a certain degree of water retention to prevent excessively rapid release of active substances from causing strong irritation and oral discomfort. The pore size can be any one of 0.01 mm, 0.02 mm, 0.05 mm, 0.1 mm, 0.2 mm, 0.5 mm, 1 mm, 1.5 mm, or 2 mm, or any combination thereof. The porosity can be any one of 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, or 10%, or any combination thereof.

[0067] In some embodiments, the first support layer and the second support layer may be formed by openings in the waterproof membrane.

[0068] In some embodiments, both the first and second support layers are made of non-woven fabric. This not only achieves good water permeability and durability in relieving moisture in the oral cavity, but also has excellent skin-friendly properties, preventing the bag itself from irritating or causing discomfort to the oral mucosa, thus further enhancing the user experience. The non-woven fabric material can be natural cellulose, synthetic cellulose, polyethylene terephthalate (PET), polyethylene (PE), etc.

[0069] In some embodiments, the thickness of the first support layer is 100μm to 150μm, for example, it can be one of 100μm, 110μm, 120μm, 130μm, 140μm, 150μm or any value between two of them.

[0070] In some embodiments, the thickness of the second support layer is 100μm to 150μm, for example, it can be one of 100μm, 110μm, 120μm, 130μm, 140μm, 150μm or any value between two of them.

[0071] In some implementations, each sub-functional layer, by mass fraction, independently includes: The active ingredient contains 0.3-0.8 parts, sweetener 5-8 parts, cooling agent 0.1-0.3 parts, sodium hyaluronate 0.5-1.2 parts, honeysuckle extract 0.3-0.8 parts, film-forming agent 10-15 parts, humectant 18-25 parts, and flow aid 0.5-1 part. Appropriate solvents can also be added to control the humidity or water content of the oral product according to taste requirements.

[0072] In some embodiments, the basic formulations of each oral product are shown in Table 1 below.

[0073] Table 1

[0074] In some embodiments, the shape of the oral article can be irregular, such as square, oval, rectangular or circular, and can be adjusted according to different design requirements.

[0075] Based on Table 1 above, the above-mentioned oral products are manufactured according to the following process steps: (1) Dissolve the honeysuckle extract in purified water to prepare a honeysuckle extract solution with a mass concentration of 10%; (2) Mix sodium hyaluronate with a portion of glycerin and stir until completely dissolved to prepare a sodium hyaluronate premix; (3) Add nicotine, sorbitol, menthol, hydroxypropyl methylcellulose and microcrystalline cellulose to the mixing tank, stir for 10-15 minutes until uniform, then slowly add honeysuckle extract, sodium hyaluronate premix and the remaining glycerin, and continue stirring for 20-25 minutes to form a uniform paste mixture. (4) Lay the thickened nonwoven fabric (i.e. carrier layer) with a thickness of 0.3~0.5mm flat on the coating machine, and evenly coat the above paste mixture on both sides of the nonwoven fabric to form a functional layer. The coating thickness is controlled to be 0.2~0.3mm to ensure that the mixture completely covers the thickened nonwoven fabric. (5) The coated thickened nonwoven fabric is sent into a drying oven and dried for 15 to 20 minutes at 40 to 45°C and 40% to 50% relative humidity to remove excess moisture. Then, the dried material is pressed into a sheet structure with a diameter of 8 to 10 mm and a thickness of 2 to 3 mm using a tablet press. The tablet pressing pressure is controlled at 15 to 20 MPa. (6) The formed oral products are sent into an ultraviolet sterilizer and sterilized for 5 to 8 minutes at a wavelength of 254nm and a power of 30W. After sterilization, they are packaged in aluminum-plastic blister packs to obtain the finished product.

[0076] In this embodiment, the triple design of "low-irritation formula + compound sustained release + water-locking fixation" achieves the technical effects of significantly reduced irritation, extended action time of active substances, and gum care. Specifically, it can reduce the incidence of oral mucosal irritation from 75% in existing products to below 25%, and the incidence of digestive tract irritation from 60% to below 18%, meeting the requirements for low-irritation use. The action time of nicotine is extended from 15-20 minutes to 30-40 minutes, reducing the frequency of sublingual administration and improving ease of use. After sublingual administration, the gum moisture retention rate is increased by 40%, and the scores for discomfort such as redness, swelling, and stinging are reduced by 60%, achieving the dual function of "nicotine intake + oral care".

[0077] To make the inventive objectives, technical solutions, and beneficial effects of this application clearer, the application is further described below with reference to embodiments. It should be understood that these embodiments are for illustrative purposes only and are not intended to limit the scope of this application.

[0078] The present application will be described in detail below through embodiments.

[0079] Test methods (1) Oral stimulation test a. Sample pretreatment: Each sample was aseptically ground into powder and extracted with sterile PBS buffer at a ratio of 1.0 g / 10 mL at 37°C for 24 hours to obtain the sample extract. 0.9% physiological saline was used as a negative control, and 1% SDS (sodium dodecyl sulfate) solution was used as a positive control.

[0080] b. Experimental procedure: Step S1: Remove the oral mucosal model from the culture medium and gently rinse it with PBS; then place the model in a dedicated 6-well plate culture dish and accurately drop 200 μL of the corresponding test solution (negative control, positive control, and extract of each sample) onto the surface of each model. Step S2: Place the petri dish in a pre-set constant temperature and humidity chamber and incubate for 30 minutes at a temperature of 37.0 ± 0.5℃ and a relative humidity of 50 ± 5% to simulate the actual contact of the oral product in the oral cavity. Step S3: After incubation, collect all the test solution on the surface of each model using a pipette; then, follow the instructions of the lactate dehydrogenase (LDH) detection kit, use an ELISA reader to detect the absorbance value of each collected solution at a wavelength of 490 nm, calculate the LDH release rate (%), and determine the mucosal irritation score based on the LDH release rate.

[0081] Among them, the LDH release rate (%) directly reflects the degree of cell membrane damage and is used as an indicator to evaluate mucosal irritation.

[0082] (2) Gum care experiment: a. Sample pretreatment: Each sample was aseptically ground into powder and extracted with sterile PBS buffer at a ratio of 1.0 g / 10 mL at 37°C for 24 hours to obtain the sample extract; before use, the extract was diluted to a concentration of 50% with cell culture medium. 0.9% physiological saline was used as a negative control, and 1% SDS (sodium dodecyl sulfate) solution was used as a positive control.

[0083] b. Experimental steps: Step S1: After digesting and counting the HGF cells in good growth condition, distribute them at a density of 1×10⁶ cells per well. 4 Cells were seeded at a density of 1,000 cells per well in 96-well plates; the cell culture plates were pre-cultured in a CO2 incubator (conditions: 37.0 ± 0.5℃, 5.0 ± 0.2% CO2, saturated humidity) for 24 hours to allow the cells to adhere completely. Step S2: Discard the original culture medium in each well, and add fresh culture medium containing 50% of the extract of each sample to the experimental group; at the same time, set up a negative control group (containing only culture medium) and a positive control group (containing 1% SDS culture medium), with at least 6 replicates for each group; put the cells back into the CO2 incubator and continue to expose and culture for 24 hours under the same conditions (37°C, 5% CO2); Step S3: After the culture is completed, add 20 μL of MTT solution (5 mg / mL) to each well, continue incubation for 4 hours and then terminate the culture. Carefully aspirate the liquid from the well, add 150 μL of DMSO, and shake slowly for 10 minutes to fully dissolve the crystals. Measure the absorbance (OD value) of each well at 570 nm using a microplate reader and calculate the gingival cell viability (%).

[0084] (3) Nicotine release experiment: The sample was placed in 50 mL of saliva simulation solution (pH 6.8, composition: sodium chloride 0.9%, potassium chloride 0.04%, calcium chloride 0.02%, pH 6.8) and the dissolution reaction was carried out at 37℃ and 50 r / min. Samples were taken every 5 minutes and the nicotine content was detected by high performance liquid chromatography for a total of 40 minutes.

[0085] (4) Saliva water retention test: Under conditions of 37°C and 50% humidity, the oral administration time was simulated for 30 minutes, and the amount of saliva loss was measured using a moisture analyzer.

[0086] Example 1 (1) Dissolve 0.5 parts of honeysuckle extract in purified water to prepare a honeysuckle extract solution with a mass concentration of 10% by weight. (2) Mix 1 part sodium hyaluronate with 1 part glycerin and stir until completely dissolved to prepare a sodium hyaluronate premix; (3) Add 0.5 parts nicotine, 6 parts sorbitol, 0.2 parts menthol, 12 parts hydroxypropyl methylcellulose, and 18 parts microcrystalline cellulose to the mixing tank, stir for 12 minutes until uniform, then slowly add honeysuckle extract, sodium hyaluronate premix and 3 parts glycerin, and continue stirring for 22 minutes to form a uniform paste mixture. (4) Lay the thickened nonwoven fabric with a thickness of 0.4 mm flat on the coating machine, and evenly coat the above paste mixture on both sides of the nonwoven fabric to form a functional layer. The coating thickness is controlled to be 0.25 mm to ensure that the mixture completely covers the nonwoven fabric. (5) The coated nonwoven fabric is placed in a drying oven and dried for 18 minutes at 42°C and 45% relative humidity to remove excess moisture. Then, the dried material is pressed into a sheet structure with a diameter of 9 mm and a thickness of 2.5 mm using a tablet press, and the tablet pressing pressure is controlled at 18 MPa. (6) The formed oral products are sent into an ultraviolet sterilizer and sterilized for 6 minutes at a wavelength of 254nm and a power of 30W. After sterilization, they are packaged in aluminum-plastic blister packs to obtain the finished product.

[0087] Comparative Examples 1-3 Three commercially available mainstream nicotine lozenges were selected as comparative examples 1, 2, and 3, respectively.

[0088] Oral stimulation experiments were conducted on the oral products of Example 1 and Comparative Examples 1-3, and the results are shown in Table 2.

[0089] Table 2

[0090] As shown in Table 2, the mucosal irritation score of Example 1 was significantly lower than that of the samples in Comparative Examples 1-3, and the gingival cell survival rate was higher than that of the comparative examples. This indicates that by reducing the content of cooling agents and sweeteners and adding sodium hyaluronate and honeysuckle extract, oral irritation can be effectively reduced, while protecting the activity of gingival cells and achieving the effect of gingival care.

[0091] Nicotine release experiments were conducted on the oral products of Example 1 and Comparative Examples 1-3, and the results are shown in Table 3.

[0092] Table 3

[0093] As shown in Table 3, the nicotine release of the sample in Example 1 was lower than that of the comparative sample at 5 minutes and 20 minutes. The nicotine release was complete at 40 minutes, and the action time was extended to 38 minutes. This proves that the composite sustained-release design of thickened nonwoven fabric and high-viscosity hydroxypropyl methylcellulose can effectively slow down the nicotine release rate, prolong the action time, and avoid the stimulation caused by a sudden increase in nicotine concentration in a short period of time.

[0094] The oral products of Example 1 and Comparative Examples 1-3 were subjected to a saliva water retention test, and the results are shown in Table 4.

[0095] Table 4

[0096] As can be seen from Table 4, the amount of saliva lost in the sample of Example 1 was much lower than that in the control sample, and the saliva fixation rate reached 86.7%. This indicates that the composite water-locking design of glycerol and microcrystalline cellulose can effectively fix saliva, prevent nicotine and additives from flowing into the digestive tract with saliva, and reduce digestive tract irritation.

[0097] The above experimental data show that the oral products provided in this application can meet the nicotine intake requirements and have low irritation to the oral mucosa and digestive tract.

[0098] In summary, the provided oral lozenge includes a functional layer comprising active ingredients, sweeteners, cooling agents, and mucosal protectants. By using mucosal protectants in the functional layer, the irritation of the cooling and sweeteners to the oral mucosa is reduced, thus protecting and repairing the gums. This addresses the problem of existing oral lozenges often causing excessive oral irritation due to flavoring substances, improving the user experience.

[0099] Although preferred embodiments of the present application have been described, those skilled in the art, upon learning the basic inventive concept, can make other changes and modifications to these embodiments. Therefore, the claims are intended to be interpreted as including the preferred embodiments as well as all changes and modifications falling within the scope of the embodiments of the present application.

[0100] The oral article provided in this application has been described in detail above. Specific examples have been used to illustrate the principles and implementation methods of this application. The description of the above embodiments is only for the purpose of helping to understand the method and core ideas of this application. At the same time, for those skilled in the art, there will be changes in the specific implementation methods and application scope based on the ideas of this application. Therefore, the content of this specification should not be construed as a limitation of this application.

Claims

1. A mouth-held product, characterized in that, It includes a functional layer, which includes active substances, sweeteners, cooling agents, and mucosal protectants. The mucosal protectants include a first protectant and a second protectant. The first protectant includes a moisturizing substance, and the second protectant includes natural components.

2. The oral article according to claim 1, characterized in that, The mucosal protectant includes at least one of sodium hyaluronate, β-glucan, panthenol, trehalose, aloe vera gel, polyglutamic acid, honeysuckle extract, dipotassium glycyrrhizate, centella asiatica extract, and tea polyphenols; and / or, The first protective agent includes at least one of sodium hyaluronate, β-glucan, panthenol, trehalose, and polyglutamic acid; and / or, The second protective agent includes at least one of the following: aloe vera gel, honeysuckle extract, dipotassium glycyrrhizate, centella asiatica extract, and tea polyphenols.

3. The oral article according to claim 1, characterized in that, By weight, the functional layer includes: The active substance comprises 0.3 to 0.8 parts, the sweetener comprises 5 to 8 parts, the cooling agent comprises 0.1 to 0.3 parts, the first protective agent comprises 0.5 to 1.2 parts, and the second protective agent comprises 0.3 to 0.8 parts.

4. The oral article according to claim 1, characterized in that, The functional layer also includes at least one of the following: a humectant, a film-forming agent, a substrate, a pH adjuster, a flow aid, and a fragrance.

5. The oral article according to claim 4, characterized in that, The moisturizer includes at least one of glycerin, propylene glycol, hyaluronic acid, and microcrystalline cellulose; and / or, The film-forming agent includes at least one of hydroxypropyl cellulose, hydroxypropyl methylcellulose, polyoxyethylene, sodium alginate, carbomer, sodium carboxymethyl cellulose, ethyl cellulose, and polyvinyl alcohol; and / or, The active substance includes at least one of nicotine and nicotine derivatives; and / or, The substrate includes at least one of pectin, gum arabic, gelatin, starch, and xanthan gum; and / or, The pH adjuster includes at least one of sodium bicarbonate, sodium carbonate, and sodium citrate; and / or, The sweetener comprises at least one of xylitol, sorbitol, mannitol, iodine, lactitol, maltitol, isomaltitol, hydrogenated starch hydrolysate, erythritol, maltotriol, aspartame, acesulfame potassium, sodium saccharin, sucralose, neotame, cyclamate, alitane, steviol glycosides, arabinitol, and monk fruit sweetener; and / or, The cooling agent includes at least one of menthol, N-ethyl-2-isopropyl-5-methylcyclohexaneformamide, menthyl lactate, menthyl acetate, and menthone glycerol ketal; The flow aid includes at least one of silica, talc, dicalcium phosphate, tricalcium phosphate, and magnesium stearate.

6. The oral article according to any one of claims 1 to 5, characterized in that, The oral article further includes a support layer that covers at least one surface of the functional layer.

7. The oral article according to claim 6, characterized in that, The support layer is used to cover the oppositely disposed two surfaces of the functional layer; and / or, The support layer has at least a permeable portion, which can be used to permeate saliva.

8. The oral article according to any one of claims 1 to 5, characterized in that, The functional layer includes at least a first sub-functional layer and a second sub-functional layer.

9. The oral article according to claim 8, characterized in that, A carrier layer is also provided between the first sub-functional layer and the second sub-functional layer.

10. The oral article according to claim 9, characterized in that, The carrier layer is a non-woven fabric; and / or, The thickness of the carrier layer is 0.3 mm to 0.5 mm; and / or, The carrier layer includes hydroxypropyl methylcellulose.

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