Oral products and methods for their manufacture
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2026-03-09
- Publication Date
- 2026-07-14
Smart Images
Figure CN122375799A_ABST
Abstract
Description
Technical Field
[0001] This application belongs to the field of food or pharmaceutical technology, specifically relating to an oral product and its preparation method. Background Technology
[0002] Currently, smoking cessation typically involves using nicotine lozenges or other products containing active substances that alleviate cravings. These lozenges often contain nicotine and other active substances such as caffeine, which usually have a bitter taste, making it easy to cause discomfort when these active substances are released into the mouth.
[0003] To improve the natural bitterness of nicotine, existing oral products have added flavoring ingredients to mask the odor of nicotine and other active substances.
[0004] However, the flavoring in existing oral products is released too quickly, which can easily lead to insufficient flavor in the later stages and an inability to effectively mask the off-flavor of active substances, seriously affecting the customer experience. Summary of the Invention
[0005] The technical problem to be solved by this application is to provide a mouth-held product and its preparation method, so as to improve the problem that the flavoring in existing mouth-held products is released too quickly and cannot continuously mask the odor of active substances.
[0006] To address the aforementioned problems, this application provides the following technical solution: This application discloses a method for preparing an oral product, wherein the preparation method includes: A functional formulation is obtained, the functional formulation comprising an active substance and an adsorbent substrate supporting the active substance; The functional preparation is placed in a fumigation space and subjected to aromatherapy treatment to obtain an aromatherapy functional preparation; wherein, the fumigation space contains aromatherapy essential oils, and at least a portion of the aromatherapy essential oils are essential oil aerosols. The aromatherapy preparation is encapsulated to obtain a lozenge.
[0007] Furthermore, in the preparation method, the aromatherapy essential oil includes at least one of peppermint essential oil and bergamot essential oil; and / or, The essential oil particles in the essential oil aerosol have a particle size of 3μm~8μm; and / or, The active substance includes at least one of nicotine and nicotine derivatives; and / or, The incense treatment temperature is 5℃~10℃; and / or, The incense treatment time is 2 to 4 minutes.
[0008] Furthermore, in the preparation method, the aroma concentration of the essential oil aerosol in the fumigation space is 150ppm~170ppm.
[0009] Furthermore, in the preparation method, the aromatherapy essential oil further includes liquid essential oil, the fumigation space includes an atomizer for atomizing the liquid essential oil, and placing the functional preparation in the fumigation space includes: Obtain the real-time aroma concentration of the essential oil aerosol within the fumigation space; When the real-time aroma concentration is less than 150 ppm, the atomizer is activated to atomize the liquid essential oil into the essential oil aerosol. When the real-time aroma concentration is greater than 170 ppm, the atomizer is controlled to stop working.
[0010] Furthermore, in the preparation method described above, the atomizer is an ultrasonic atomizer.
[0011] Furthermore, in the preparation method, the functional formulation includes a functional layer and a support layer stacked together, wherein the functional layer includes the active substance, and the support layer has at least a porous structure, which is configured as the adsorption substrate.
[0012] Furthermore, in the preparation method, the functional formulation is a tablet, which is formed by pressing active particles containing the active substance, and the viscosity of the active particles is 48 mPa·s to 52 mPa·s.
[0013] Furthermore, in the preparation method, the active particles include basic excipients, wherein the basic excipients include carrier materials, sugar alcohol fillers, and binders, and the active particles also include at least one of viscosity modifiers, pH modifiers, antioxidants, lubricants, and flavoring agents.
[0014] Furthermore, in the preparation method, the active substance includes at least one of nicotine and nicotine derivatives; and / or, The adhesive comprises at least one of hydroxypropyl cellulose, hydroxypropyl methyl cellulose, ethyl cellulose, polyvinyl alcohol, and sodium alginate; and / or, The carrier material includes at least one of microcrystalline cellulose and porous starch; and / or, The sugar alcohol filler includes at least one of xylitol, mannitol, lactitol, erythritol, isomaltitol, and sorbitol; and / or, The antioxidants include at least one of the following: ethylparaben, trisodium citrate, sodium ascorbate, vitamin E, and tea polyphenols; The pH adjuster includes at least one of sodium bicarbonate, sodium carbonate, sodium citrate, citric acid, and malic acid; and / or, The viscosity modifier includes at least one of povidone, glyceryl monostearate, carbomer, sodium carboxymethyl cellulose, xanthan gum, and carrageenan; and / or, The lubricant includes at least one of talc, micronized silica gel, and magnesium stearate; and / or, The flavoring agents include sweeteners, cooling agents, flavoring agents, and salting agents.
[0015] Furthermore, in the preparation method, the active particles, measured by mass parts, comprise: Nicotine 0.1-0.2 parts, sorbitol 40-50 parts, microcrystalline cellulose 18-25 parts, hydroxypropyl methylcellulose 10-20 parts, povidone 0.2-0.3 parts, vitamin E 1.0-1.5 parts, magnesium stearate 1.0-1.5 parts, sucralose 0.1-0.2 parts, to control the viscosity of the active particles to be 48 mPa·s-52 mPa·s.
[0016] This application also proposes an oral article, wherein it is prepared by the above-described preparation method.
[0017] Compared with the prior art, the embodiments of this application have the following advantages: In this embodiment, the preparation method includes: obtaining a functional preparation, which includes an active substance and an adsorbent substrate carrying the active substance; placing the functional preparation in a fumigation space and fumigating it to obtain a fumigated functional preparation, wherein the fumigation space contains essential oils, and at least a portion of the essential oils are essential oil aerosols; and encapsulating the fumigated functional preparation to obtain a sublingual product. Specifically, by first placing the functional preparation containing the active substance in a sealed environment and fumigating it with essential oils that are at least partially essential oil aerosols, followed by sealing, the method allows tiny particulate essential oil droplets to adhere to the surface of the functional preparation and penetrate it. Furthermore, the residual essential oil droplets in the sealed bag continue to penetrate into the interior of the functional preparation, enabling the simultaneous storage and release of the "active substance and aroma." This achieves uniform release of the active substance and continuous aroma throughout the entire sublingual process, masking the bitterness of the active substance and improving the comfort of consumption.
[0018] 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
[0019] Figure 1 This is a flowchart of the preparation method of the oral product provided in the embodiments of this application. Detailed Implementation
[0020] 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.
[0021] 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.
[0022] The inventors discovered that the aroma experience is disconnected from the function: existing products only mask the bitterness of nicotine by adding fragrances, and the aroma mostly adheres to the surface and disappears after 3-5 minutes of holding it in the mouth. This cannot achieve "fragrance accompanying nicotine release throughout the entire process". In addition, the fragrance and nicotine are prone to flavor antagonism, which aggravates oral discomfort.
[0023] ③ Nicotine has poor stability: ① Insufficient compatibility between incense and nicotine: Existing incense-making processes mostly involve open-air high-temperature fumigation, which easily leads to nicotine oxidation (oxidation rate exceeding 30%). Furthermore, aroma molecules cannot penetrate into the interior of the lozenge, only achieving surface-level fragrance enhancement with a short duration. In existing technologies, flavorings are added to lozenges through simple blending to mask odors. The flavorings are released too quickly, easily resulting in insufficient flavor in the later stages and failing to effectively mask the off-flavors of active substances, seriously affecting the customer experience.
[0024] In response to the above problems, such as Figure 1 As shown in the embodiment of this application, a method for preparing an oral product is provided, including steps 101 to 103: Step 101: Obtain a functional formulation, wherein the functional formulation includes an active substance and an adsorbent substrate supporting the active substance.
[0025] In this step, the active substance is a component that can help smokers alleviate withdrawal symptoms and can be directly absorbed through the oral mucosa; the adsorption record can both carry the active substance and load essential oil aerosols through adsorption and other methods.
[0026] Step 102: Place the functional preparation in a fumigation space and perform fumigation treatment on the functional preparation to obtain a fumigation functional preparation, wherein the fumigation space contains fumigation essential oil, and at least a portion of the fumigation essential oil is an essential oil aerosol.
[0027] In this step, the essential oil aerosol is atomized into a gaseous state of aromatherapy essential oil. Because the aromatherapy space contains aromatherapy essential oil, and at least part of the aromatherapy essential oil is an essential oil aerosol, the aromatherapy space is filled with essential oil aerosol. The functional preparation has an adsorbent substrate. Therefore, after the functional preparation is placed in the aromatherapy space, the essential oil aerosol will penetrate into the adsorbent substrate, thereby achieving aromatherapy treatment of the functional preparation.
[0028] In some implementations, the aforementioned fumigation space is a sealed space, which can effectively prevent the evaporation of essential oils and improve the efficiency of incense burning.
[0029] Step 103: The aromatherapy functional preparation is packaged to obtain a lozenge.
[0030] In this step, after the incense treatment, the incense functional preparation is transferred into a packaging bag, which allows the residual aroma inside the bag to continuously penetrate into the incense functional preparation, achieving simultaneous storage and release of "active substances and aroma".
[0031] In some embodiments, the oxygen permeability of the aforementioned packaging bag is ≤0.05cc / 24h, and the water vapor permeability is ≤0.05g / 24h. This effectively prevents moisture from entering the bag and causing the oral product to become damp and soften, while also preventing the essential oils inside the bag from overflowing and diluting the aroma. In some embodiments, the aforementioned packaging bag can be an aluminum-plastic bag, etc.
[0032] In some implementations, after the incense treatment, the incense preparation is transferred into a packaging bag within 10 seconds via an automatic conveyor belt or the like to prevent the aroma from dissipating.
[0033] In some embodiments, the packaging bag is heat-sealed at a temperature of 160°C to 180°C for a time of 1 to 3 seconds. In some embodiments, the heat-sealing temperature of the packaging bag can be a range of 160°C, 170°C, 180°C, or any two of these values, and the time can be a range of 1 second, 2 seconds, 3 seconds, or any two of these values.
[0034] In this embodiment, the functional preparation containing active substances is first placed in a sealed environment and then treated with aromatherapy oil, which is at least partly an essential oil aerosol, before being sealed. This process allows tiny particulate aromatherapy oil droplets to adhere to the surface of the functional preparation and penetrate into it. Furthermore, the residual aromatherapy oil droplets in the sealed bag continue to penetrate into the interior of the functional preparation, enabling the simultaneous storage and release of "active substances and aroma". This achieves uniform release of active substances and continuous aroma throughout the entire process of oral administration, masking the bitterness of the active substances and improving the comfort of taking the medication.
[0035] In some embodiments, the active substance in the functional layer 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.
[0036] 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.
[0037] In some implementations, to meet various user needs, the active substance may include substances with specific medical properties, such as vitamins; the active substance may also include substances with specific active properties, such as caffeine, theophylline, capsaicin, etc.
[0038] In some embodiments, the functional formulation includes a functional layer and a support layer stacked together, that is, the functional formulation is an oral film or lozenge, wherein the functional layer includes an active substance, and the support layer has at least a porous structure in part, which is configured as an adsorption substrate, capable of both supporting the functional layer including the active substance and loading essential oil aerosols through adsorption or other means.
[0039] In some embodiments, the support layer can be a nonwoven fabric, which can utilize its porous structure to adsorb essential oil aerosols.
[0040] In other embodiments, the functional formulation is a tablet, which is formed by pressing active particles containing active substances. The viscosity of the active particles is 48 mPa·s to 52 mPa·s, which not only ensures a better taste, but also makes the entire tablet itself an adsorbent substrate, which can effectively attach aroma.
[0041] In some embodiments, the viscosity of the active particles can be a range of one or both of 48 mPa·s, 49 mPa·s, 50 mPa·s, 51 mPa·s, and 52 mPa·s.
[0042] In some embodiments, the active particles include basic excipients, which include carrier materials, sugar alcohol fillers, and binders to meet the user's personalized needs.
[0043] The carrier material serves as the framework of the functional layer; sugar alcohol fillers not only enhance tablet hardness and formability but also effectively fill the surface of active substances, prolonging their duration of action; the aforementioned binders not only bind nicotine, flavorings, and other powders or granules into uniform solids (such as sachets or tablets), preventing loosening or breakage and thus maintaining product shape and structure, but also regulate the dissolution rate to allow active substances and flavorings to be released slowly, avoiding large-scale release that could cause oral irritation or an overly strong taste. Furthermore, by controlling the type and proportion of binders, the smoke can be kept in the mouth for a longer period, improving the user experience; in addition, the binders bind fine particles into a smooth texture, avoiding a gritty or uncomfortable feeling during use, and also help nicotine, flavorings, pH adjusters, and other ingredients to be evenly distributed in the product, ensuring consistent dosage in every serving.
[0044] In some embodiments, sugar alcohol fillers may include substances such as xylitol, mannitol, lactitol, erythritol, isomaltitol, and sorbitol.
[0045] In some embodiments, the carrier material can be at least one of microcrystalline cellulose (MCC), natural cellulose, porous starch, and maltodextrin. Microcrystalline cellulose not only absorbs water during wet granulation to form a viscous network that aids in granule formation, but it also regulates the distribution of moisture and humectants (such as glycerin) in cigarette smoke, preventing clumping or excessive moisture. Furthermore, the fine powder texture of microcrystalline cellulose reduces the grainy feel and improves user comfort.
[0046] In some embodiments, the adhesive includes at least one of hydroxypropyl cellulose, hydroxypropyl methyl cellulose, ethyl cellulose, polyvinyl alcohol, and sodium alginate, which can form covalent bonds using hydroxyl groups and other groups on the molecular chain to weave the originally linear molecular chain into a three-dimensional network structure. This results in active particles with ultra-high density water-absorbing materials, which can effectively disperse active substances and accelerate saliva penetration, thereby increasing the release rate of active substances in the early stage and meeting the user's immediate needs.
[0047] In some embodiments, the active particles also include at least one of viscosity modifiers, pH modifiers, antioxidants, lubricants, and flavorings, that is, the active particles are made of active substances, carrier materials, fillers, binders, viscosity modifiers, pH modifiers, lubricants, and flavorings.
[0048] The viscosity modifier adjusts the viscosity of the active particles to 48 mPa·s to 52 mPa·s, thereby improving adhesion and film-forming properties, which is beneficial for stabilizing active substances and adsorbing aroma. In some embodiments, the viscosity modifier includes at least one of povidone and polyvinyl alcohol, which not only effectively improves adhesion and film-forming properties, but also has good water solubility, uniform distribution, and can be prepared into a solution for dropwise addition. It can accurately calibrate the viscosity to the target range (48~52 mPa·s), and has good compatibility with the binder, which can enhance particle strength without interfering with its core function of controlling the release of active substances. In some embodiments, the viscosity modifier can be povidone K30, povidone K25, or povidone K90.
[0049] The lubricant not only maintains moisture, imparts a soft and smooth feel to the product, and reduces graininess, but also affects the dissolution rate of active substances by regulating water activity, achieving a slow-release effect and preventing discomfort caused by a sudden increase in concentration. Furthermore, the lubricant maintains the homogeneity of the mixture, preventing uneven drying or component separation during storage. In some embodiments, the lubricant includes at least one of talc, magnesium stearate, silica, micronized silica, and polyethylene glycol.
[0050] 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, sodium citrate, citric acid, and malic acid.
[0051] Antioxidants such as ethylparaben, vitamin E acetate, and ascorbic acid can inhibit the oxidation of nicotine, vegetable oils, or flavorings, preventing rancidity, discoloration, or inactivation, slowing down component degradation, and maintaining product stability and flavor consistency.
[0052] Lubricants not only maintain moisture and give products a soft, smooth feel, reducing the grainy texture, but also affect the dissolution rate of active substances by adjusting water activity, achieving a slow-release effect and avoiding discomfort caused by a sudden increase in concentration. In addition, lubricants can maintain the homogeneity of the mixture and prevent uneven drying or component separation during storage.
[0053] Flavoring agents include at least one of sweeteners, cooling agents, salting agents, acidulants, and flavorings.
[0054] Sweeteners can mask the bitter or pungent taste of active substances such as nicotine, enhancing the palatability of the product. Simultaneously, sweeteners can increase the sense of pleasure, making the product feel more like a snack or candy, reducing user resistance. Furthermore, sweeteners work synergistically with flavorings to enhance the expression of fruity, minty, and other flavors. In some embodiments, sweeteners may include at least one of xylitol, sorbitol, mannitol, yigerol, lactitol, maltitol, isomaltitol, hydrogenated starch hydrolysate, erythritol, maltodextrin, aspartame, acesulfame potassium, sodium saccharin, sucralose, neotame, cyclamate, alitane, steviol glycosides, arabinitol, and monk fruit sweetener.
[0055] Cooling agents can enhance the user experience by simulating a cooling sensation, effectively neutralizing or masking the odor of active ingredients, reducing direct irritation of the active ingredients to the oral mucosa, and minimizing burning or numbness after use. In some embodiments, cooling agents may include at least one of menthol, N-ethyl-2-isopropyl-5-methylcyclohexaneformamide, menthyl lactate, menthyl acetate, and menthone glycerol ketal.
[0056] Among them, saltiness agents can significantly enhance the overall flavor intensity of the product. A small amount added can stimulate saliva secretion, improve oral moisture, and suppress bitterness. It can also make sweetness sweeter, umami more savory, and aroma more intense. In some embodiments, saltiness agents may include at least one of sodium chloride and potassium chloride.
[0057] Flavoring agents can improve taste and flavor, mask the odor of chemicals such as tobacco or nicotine, and enhance the user experience. Specifically, flavoring agents can be fragrances; flavorings such as mint and spicy spices can stimulate the oral mucosa, promote saliva secretion, help nicotine be released more quickly and absorbed through the mouth, and enhance its effect. In addition, the diverse flavor profiles of fragrances (such as coffee, chocolate, cinnamon, etc.) can satisfy different consumer preferences and increase product appeal. The aforementioned fragrance can be a type of mint flavoring.
[0058] In some embodiments, the oral article further includes a solvent, which includes at least one of water and ethanol.
[0059] In some embodiments, the active particles, by mass parts, comprise: Nicotine 0.1-0.2 parts, sorbitol 40-50 parts, microcrystalline cellulose 18-25 parts, hydroxypropyl methylcellulose 10-20 parts, povidone 0.2-0.3 parts, vitamin E 1.0-1.5 parts, magnesium stearate 1.0-1.5 parts, sucralose 0.1-0.2 parts, to control the viscosity of the active particles to 48 mPa·s-52 mPa·s. Appropriate solvents can also be added to control the humidity or water content of the active particles according to taste requirements.
[0060] In some embodiments, the aromatherapy essential oil includes at least one of peppermint essential oil and bergamot essential oil, is suitable for adjusting to a viscosity of less than 100 MPa, and is formed into an essential oil aerosol by atomization such as ultrasound, thereby enabling effective aromatherapy treatment of functional preparations.
[0061] In some embodiments, the particle size of the essential oil particles in the essential oil aerosol is 3μm to 8μm, for example, it can be one or any two of the following values: 3μm, 4μm, 5μm, 6μm, 7μm, 8μm, which can effectively penetrate into the functional formulation and adhere to the adsorption substrate to achieve the effect of long-lasting fragrance release.
[0062] In some embodiments, the incense treatment temperature is 5℃~10℃, for example, it can be one or any two of 5℃, 6℃, 7℃, 8℃, 9℃, and 10℃, which can effectively prevent the essential oils from atomizing and evaporating during the incense treatment. In this embodiment, by using "low-temperature process + high-barrier packaging", the oxidative degradation of active substances can be significantly reduced, allowing the product to be stored at 25℃ and 60% relative humidity for 6 months with an active substance retention rate of ≥90% and an aroma retention rate of ≥85%.
[0063] In some implementations, the incense treatment time is 2 to 4 minutes, for example, it can be one of 2 minutes, 3 minutes, 4 minutes or any two of them, which can effectively complete the incense treatment.
[0064] In some embodiments, the aroma concentration of the essential oil aerosol in the fumigation space is 150ppm to 170ppm, for example, it can be one or any two of 150ppm, 160ppm, and 170ppm, so that the aroma in the functional preparation is sufficient to mask the bitterness of the active substance without masking the irritating function of the active substance.
[0065] In some embodiments, the aromatherapy essential oil further includes liquid essential oil, and the fumigation space includes an atomizer for atomizing the liquid essential oil. Placing the functional preparation within the fumigation space includes: Obtain the real-time aroma concentration of the essential oil aerosol within the fumigation space; When the real-time aroma concentration is less than 150 ppm, the atomizer is activated to atomize the liquid essential oil into the essential oil aerosol. When the real-time aroma concentration is greater than 170 ppm, the atomizer is controlled to stop working.
[0066] In this embodiment, an aroma concentration probe is installed in the fumigation space to collect aroma concentration data in real time and transmit it to the electronic control system. When the aroma concentration is below 150ppm, the atomizer is automatically started to atomize the liquid essential oil into an essential oil aerosol. When the aroma concentration reaches 170ppm, the atomizer is automatically stopped. This achieves the goal of keeping the aroma concentration in the atomization space constant at 150ppm~170ppm through "intermittent start and stop", avoiding the effect of nicotine being masked by excessively high concentration and the bitterness being unable to be masked by excessively low concentration. In this embodiment, the aroma concentration probe can be a PG (propylene glycol) aroma concentration probe, and its aroma concentration detection range can be 0~300ppm. The electrical control system can be a programmable logic controller (PLC) electrical control system, thereby realizing the batch-to-batch aroma concentration difference ≤3% and active substance content difference ≤2% through PLC-PG linkage control.
[0067] In some embodiments, the atomizer is an ultrasonic atomizer, which can rapidly atomize liquid essential oils into essential oil aerosols at low temperatures of 5°C to 10°C.
[0068] This application also proposes an oral preparation, which is prepared by the above-described preparation method.
[0069] In some embodiments, the oral product may be in the form of a mouth pouch, oral dissolving film, tablet, or tearable strip.
[0070] 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.
[0071] 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.
[0072] The present application will be described in detail below through embodiments.
[0073] Test methods (1) Nicotine content test: According to the high performance liquid chromatography (HPLC) method in the Chinese Pharmacopoeia, 10 tablets of each sample were randomly selected, crushed, dissolved and diluted to a certain volume and then injected for analysis to determine the nicotine content; (2) Nicotine content difference test: Calculate the relative standard deviation (RSD) of nicotine content in 10 samples.
[0074] (3) Aroma concentration difference test: Take 10 bags of oral product samples prepared in the same batch, randomly select 1 tablet from each bag, and place them in 500 mL sealed glass containers. Let them stand for 2 minutes at a temperature of 25±1℃ and a relative humidity of 60±5% to allow the aroma release to reach a stable state. The aroma concentration (in ppm) in the container was determined using a gas chromatograph or an online aroma concentration detection system equipped with a PG (propylene glycol) aroma concentration probe; wherein the PG aroma concentration probe has a detection range of 0~300 ppm, a resolution of ≤1 ppm, and a sampling time of ≤5 seconds; Record the aroma concentration value of each sample, calculate the average value and standard deviation, and obtain the relative standard deviation (RSD). RSD is used to characterize the difference in aroma concentration between batches.
[0075] (4) Nicotine dissolution and aroma release test: The sample was placed in 500 mL of pH 6.8 phosphate buffer and the dissolution reaction was carried out at a temperature of 37±0.5°C and a rotation speed of 50 r / min. 5 mL samples were taken at 2 min, 5 min, 10 min, 15 min, 20 min, 30 min, 45 min and 60 min respectively and an equal amount of fresh phosphate buffer was added. The nicotine concentration was detected by high performance liquid chromatography and the aroma concentration was detected by gas chromatography (GC). The cumulative release percentage was calculated and the release amount was recorded as reference data.
[0076] The high-performance liquid chromatography (HPLC) conditions were as follows: C18 column, mobile phase acetonitrile-phosphate buffer (pH 4.5) (50:50, v / v), and detection wavelength 260 nm.
[0077] (5) Stability test: After placing the oral product in an environment with a temperature of 37°C and a relative humidity of 75% for 6 months, the nicotine retention rate, hardness, and disintegration time were determined.
[0078] (6) Taste and evaluation Subjective evaluation data on the product in terms of bitterness intensity, stickiness, etc., were assessed using a sensory evaluation scoring method (0-5 points), with 100 evaluators conducting blind tests and scoring. After tasting each sample, each evaluator rinsed their mouth with water, waited 5 minutes, and then tasted the next sample. They used a 5-minute linear scale (0-5 points) to score the samples, with higher scores indicating a better experience. Among them, bitterness intensity (0~5 points): the higher the score, the weaker the bitterness, and 5 points means no bitterness; Stickiness (0-5 points): The higher the score, the more comfortable the taste.
[0079] Example 1 (1) By weight, take 500 parts of sorbitol, 300 parts of microcrystalline cellulose, and 200 parts of hydroxypropyl methylcellulose E5, put them into a double cone mixer (speed 150 r / min) and dry mix for 10 minutes to obtain a basic excipient mixture; (2) Add 3 parts of an aqueous solution of povidone K30 (3.75% by mass / volume) to the basic auxiliary mixture while stirring (200 r / min). After stirring for 15 minutes, measure the viscosity with a rotational viscometer (NDJ-8S type, 25℃, 60 r / min). If it is lower than 48 mPa·s, add 0.1% w / v of povidone K30 solution. If it is higher than 52 mPa·s, add sorbitol powder until the viscosity stabilizes at 48~52 mPa·s.
[0080] (3) Dissolve 1.0 part of nicotine, 2 parts of vitamin E and 1 part of sucralose in ethanol to prepare an active ingredient solution; slowly add the solution to the excipient mixture with qualified viscosity while stirring (180 r / min) for 20 minutes, then add an appropriate amount of deionized water to make a soft material (which can be formed into a ball by hand and dispersed by light pressure), granulate through a 16-mesh sieve, dry in an oven at 45℃ for 1.5 hours (moisture content controlled at 3%~4%), and granulate through a 14-mesh sieve to obtain active granules; Add 15 parts of magnesium stearate to the active granules and mix gently for 3-5 minutes. Use this as the tableting material. Use a rotary tablet press (model ZP-35) with a circular die of 8 mm diameter and 3 mm thickness. Set the tableting pressure to 18-22 kN, the tableting temperature to 25-30℃, and the tableting speed to 25 tablets / minute to obtain the functional formulation.
[0081] (4) Preheat the sealed fumigation space to 5~10℃, and set the aroma concentration target value of 160ppm through PLC. Start the PG probe set in the fumigation space to obtain the real-time aroma concentration. The functional preparation is evenly spread on the tray inside the cavity (single layer). Liquid essential oil is used as the atomizing material. The liquid essential oil is made by diluting 5 parts peppermint essential oil and 3 parts bergamot essential oil with propylene glycol. The ultrasonic atomizer is turned on. When the real-time aroma concentration is less than 150 ppm, the atomized liquid essential oil is controlled to be an essential oil aerosol. When the real-time aroma concentration is greater than 170 ppm, the atomizer is controlled to stop working. The above-mentioned intermittent aromatherapy treatment is controlled to continue for 2 to 4 minutes. After being scented, the product is transferred via an automatic conveyor belt (within 10 seconds) into a high-barrier aluminum-plastic bag (10 pieces per bag), and then heat-sealed (at 170°C for 1.5 seconds) to complete the preparation of the oral product.
[0082] Comparative Example 1 (1) By weight, take 1.0 part of nicotine, 500 parts of sorbitol, 300 parts of microcrystalline cellulose, and 200 parts of hydroxypropyl methylcellulose E5, put them into a double cone mixer (speed 150 r / min) and dry mix for 10 minutes to obtain a basic excipient mixture; (2) Dissolve 2 parts of vitamin E, 1 part of sucralose, 5 parts of peppermint oil and 3 parts of bergamot oil in ethanol to prepare an active ingredient solution; add the basic excipient mixture to the solution while stirring (180 r / min) for 20 minutes, then add an appropriate amount of deionized water to make a soft material (which can be formed into a ball by hand and easily dispersed by light pressure), granulate through a 16-mesh sieve, dry in an oven at 45℃ for 1.5 hours (with moisture content controlled at 3%~4%), and granulate through a 14-mesh sieve to obtain active granules; (3) Add 15 parts of magnesium stearate to the active granules and mix gently for 3-5 minutes. Use it as the tableting material. Use a rotary tablet press (model ZP-35) with a circular die of 8 mm in diameter and 3 mm in thickness. Set the tableting pressure to 18-22 kN, the tableting temperature to 25-30 °C, and the tableting speed to 25 tablets / minute to obtain the functional formulation. (4) Transfer the functional preparation into a high-barrier aluminum-plastic bag (10 tablets per bag), heat seal (temperature 170℃, time 1.5 seconds) to complete the preparation of the oral product.
[0083] The tablet weight difference test, hardness test, disintegration time test, nicotine content test, nicotine content uniformity test, and aroma concentration difference test were performed on the oral products in the examples and comparative examples. The test results are shown in Table 1.
[0084] Table 1
[0085] The oral products in the examples and comparative examples were tested for nicotine dissolution, aroma concentration, and stability. The test results are shown in Table 2.
[0086] Table 2
[0087] Stability tests were conducted on the oral products in the examples and comparative examples, and the test results are shown in Table 3.
[0088]
[0089] As can be seen from Table 3, the oral products prepared by this method have significant stability advantages.
[0090] The oral products in the examples and comparative examples were taste-tested, and the results are shown in Table 4.
[0091] Table 4
[0092] In addition, blood nicotine concentration tests on 20 individuals who took the oral product prepared according to this protocol showed a peak concentration of 12.3±1.5 ng / mL, with no nausea, dizziness, or other discomfort, indicating that the safety met the requirements.
[0093] In summary, the oral product and preparation method provided in this application first place the functional preparation containing active substances in a sealed environment, and then perform aromatherapy treatment using aromatherapy essential oils that are at least partially composed of essential oil aerosols before sealing. This allows tiny particulate aromatherapy essential oil droplets to adhere to the surface of the functional preparation and penetrate into it. Furthermore, the residual aromatherapy essential oil droplets in the sealed bag continue to penetrate into the interior of the functional preparation, enabling the simultaneous storage and release of "active substances and aroma". This achieves uniform release of active substances and continuous aroma accompaniment throughout the entire oral administration process, masking the bitterness of the active substances and improving the comfort of taking the product.
[0094] 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.
[0095] The above provides a detailed description of an oral product and its preparation method provided in this application. 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 method for preparing a mouth-held product, characterized in that, The preparation method includes: A functional formulation is obtained, the functional formulation comprising an active substance and an adsorbent substrate supporting the active substance; The functional preparation is placed in a fumigation space and subjected to fumigation treatment to obtain a fumigation functional preparation, wherein the fumigation space contains fumigation essential oil, and at least a portion of the fumigation essential oil is an essential oil aerosol. The aromatherapy preparation is encapsulated to obtain a lozenge.
2. The preparation method according to claim 1, characterized in that, The aromatherapy essential oil includes at least one of peppermint essential oil and bergamot essential oil; and / or, The essential oil particles in the essential oil aerosol have a particle size of 3μm~8μm; and / or, The active substance includes at least one of nicotine and nicotine derivatives; and / or, The incense treatment temperature is 5℃~10℃; and / or, The incense treatment time is 2 to 4 minutes.
3. The preparation method according to claim 1, characterized in that, The aroma concentration of the essential oil aerosol in the fumigation space is 150ppm~170ppm.
4. The preparation method according to claim 3, characterized in that, The aromatherapy essential oil also includes liquid essential oil, the fumigation space includes an atomizer for atomizing the liquid essential oil, and placing the functional preparation in the fumigation space includes: Obtain the real-time aroma concentration of the essential oil aerosol within the fumigation space; When the real-time aroma concentration is less than 150 ppm, the atomizer is activated to atomize the liquid essential oil into the essential oil aerosol. When the real-time aroma concentration is greater than 170 ppm, the atomizer is controlled to stop working.
5. The preparation method according to claim 4, characterized in that, The atomizer is an ultrasonic atomizer.
6. The preparation method according to claim 1, characterized in that, The functional formulation includes a functional layer and a support layer stacked together, wherein the functional layer includes the active substance, and the support layer has at least a porous structure configured as the adsorption substrate.
7. The preparation method according to claim 1, characterized in that, The functional formulation is a tablet, which is formed by pressing active particles containing the active substance, and the viscosity of the active particles is 48 mPa·s to 52 mPa·s.
8. The preparation method according to claim 7, characterized in that, The active particles include basic excipients, which include carrier materials, sugar alcohol fillers, and binders. The active particles also include at least one of viscosity modifiers, pH modifiers, antioxidants, lubricants, and flavoring agents.
9. The preparation method according to claim 8, characterized in that, The adhesive comprises at least one of hydroxypropyl cellulose, hydroxypropyl methyl cellulose, ethyl cellulose, polyvinyl alcohol, and sodium alginate; and / or, The carrier material includes at least one of microcrystalline cellulose and porous starch; and / or, The sugar alcohol filler includes at least one of xylitol, mannitol, lactitol, erythritol, isomaltitol, and sorbitol; and / or, The antioxidants include at least one of the following: ethylparaben, trisodium citrate, sodium ascorbate, vitamin E, and tea polyphenols; The pH adjuster includes at least one of sodium bicarbonate, sodium carbonate, sodium citrate, citric acid, and malic acid; and / or, The viscosity modifier includes at least one of polyvinylpyrrolidone and polyvinyl alcohol; and / or, The lubricant comprises at least one of talc, magnesium stearate, silica, micronized silica powder, and polyethylene glycol; and / or, The flavoring agent includes at least one of sweeteners, cooling agents, flavoring agents, and salting agents.
10. The preparation method according to claim 7, characterized in that, The active particles, measured in parts by mass, comprise: Nicotine 0.1-0.2 parts, sorbitol 40-50 parts, microcrystalline cellulose 18-25 parts, hydroxypropyl methylcellulose 10-20 parts, povidone 0.2-0.3 parts, vitamin E 1.0-1.5 parts, magnesium stearate 1.0-1.5 parts, sucralose 0.1-0.2 parts, to control the viscosity of the active particles to be 48 mPa·s-52 mPa·s.
11. A mouth-held product, characterized in that, It is prepared by any one of the preparation methods described in claims 1 to 10.