Oral nicotine product and preparation method thereof

Abstract

The embodiment of the invention provides an oral nicotine product and a preparation method thereof, and the oral nicotine product comprises nicotine particles containing nicotine and a first carrier; and the active ingredient particles comprise an active ingredient and a second carrier, and the active ingredient comprises at least one ingredient suitable for relieving the irritation of nicotine to the stomach. In the oral process of the oral nicotine product, effective components in the effective component particles are better than nicotine in the nicotine particles to be released in the stomach, and the effective components act on the stomach before nicotine, so that irritation of nicotine to the stomach is relieved, and the taking experience of the oral nicotine product is improved.

Description

TECHNICAL FIELD

[0001] The present disclosure relates to the technical field of oral products, in particular to an oral nicotine product and a preparation method thereof. BACKGROUND

[0002] With the promotion of global tobacco control policy and the enhancement of public health awareness, nicotine replacement therapy (NRT) products have gradually become an important alternative to traditional tobacco products. Oral nicotine products are one of the important forms of NRT products, which mainly release nicotine in the oral cavity through oral use / mastication, and absorb nicotine through the oral mucosa, without burning and producing harmful substances such as tar and carbon monoxide, which can provide effective alternative therapy for relieving and quitting tobacco dependence.

[0003] Nicotine, also known as nicotine, is the main active ingredient in oral nicotine products. It is a high-concentration alkaloid with strong irritation. When nicotine in oral nicotine products is released into the oral cavity, it will directly stimulate the tissues in the oral cavity, causing a stinging or burning sensation. This discomfort is more pronounced when using nicotine products for the first time or using products with higher nicotine concentrations. In addition, the irritation of nicotine will also cause increased salivation, and some nicotine will inevitably flow through the throat and into the gastrointestinal tract with saliva, causing heartburn, belching, vomiting, stomach pain, and other discomforts.

[0004] The prior art mainly reduces nicotine irritation by directly adding antagonists of acetylcholine receptors and / or TRP ion channels. However, since most antagonists are released in the oral cavity and act on specific receptors, their main effect is to reduce the irritation of nicotine on the oral cavity and throat, and their effect on reducing gastrointestinal irritation is limited.

[0005] Therefore, there is a need to develop an oral nicotine product with reduced gastrointestinal irritation. SUMMARY

[0006] The present disclosure provides an oral nicotine product, which comprises: nicotine particles containing nicotine and a first carrier; and active ingredient particles containing an active ingredient and a second carrier, the active ingredient containing at least one ingredient suitable for reducing the irritation of nicotine on the stomach; wherein, during oral administration, the active ingredient in the active ingredient particles is released in the stomach faster than the nicotine in the nicotine particles.

[0007] In some embodiments, the second carrier has better hydrophilicity than the first carrier.

[0008] In some embodiments, the first carrier comprises one or more of microcrystalline cellulose, cellulose derivatives, plant fibers, and starch derivatives.

[0009] In some embodiments, the first carrier comprises one or more of hydroxypropyl methylcellulose (HPMC), hydroxyethyl cellulose (HEC), hydroxypropyl cellulose (HPC), methylcellulose, ethyl hydroxyethyl cellulose, carboxymethyl cellulose, modified cellulose gum and sodium carboxymethyl cellulose (NaCMC), microcrystalline cellulose, coconut shell fiber powder, bamboo fiber powder, peanut shell fiber, oat fiber powder, cocoa shell powder, tea fiber powder, coffee grounds powder, sugarcane fiber powder, apple fiber powder, citrus fiber powder, cassava fiber powder, flaxseed powder, pea fiber powder, wheat fiber powder, soybean fiber powder, modified starch, cross-linked starch.

[0010] In some embodiments, the second carrier comprises one or more of soluble starch, lactose, sucrose.

[0011] In some embodiments, the mass ratio of the nicotine particles to the active ingredient particles is 1:1 to 4:1.

[0012] In some embodiments, the mass fraction of the first carrier in the nicotine particles is 30wt% to 80wt%, and the mass fraction of the second carrier in the active ingredient particles is 20wt% to 70wt%.

[0013] In some embodiments, the active ingredient comprises at least one of ginger extract, ginger oleoresin, curcumin, 6-shogaol, 6-shogaol, borneol, isoborneol, borneol acetate, monoborneol succinate, monoisoborneol succinate, glycerol oxalate, monoborneol formate, menthol, cinnamaldehyde, eucalyptol (1,8-cineole), WS-3 (N-ethyl-2-isopropyl-5-methylcyclohexanecarboxamide, CAS No.: 39711-79-0), WS-23 (N,2,3-trimethyl-2-isopropylbutyramide, CAS No.: 51115-67-4), WS-12 (N-(4-methoxyphenyl)-p-menthyl-3-carboxamide, CAS No.: 68489-09-8), carvacrol, carveol, menthol, acetate, phosphate, citrate, carbonate, bicarbonate, borate, sodium alginate, potassium alginate, ammonium alginate; soybean lecithin, exogenous phospholipid, pectin, aluminum magnesium carbonate, bismuth potassium citrate, magnesium oxide, L-glutamine, tea polysaccharide, ganoderma lucidum polysaccharide, green tea extract, ascorbic acid, taurine, quercetin, resveratrol, carotenoid, anthocyanin.

[0014] In some embodiments, the oral nicotine product further comprises 1wt% to 30wt% of a binder, and / or 0.5wt% to 15wt% of a flavoring agent, and / or 1wt% to 10wt% of a humectant, and / or 1wt% to 3wt% of a pH adjuster, and / or 0.5wt% to 10wt% of a fragrance.

[0015] In some embodiments, the particle size of the effective ingredient particles is smaller than the particle size of the nicotine particles, and the first carrier and the second carrier comprise the same or different ingredients.

[0016] In some embodiments, the particle size of the effective ingredient particles is 15% to 80% of the particle size of the nicotine particles.

[0017] In some embodiments, the particle size of the effective ingredient particles is 15% to 50% of the particle size of the nicotine particles.

[0018] In some embodiments, the particle size of the nicotine particles is 16 to 50 mesh.

[0019] The present disclosure also provides a preparation method of any of the oral nicotine products described above, which comprises: uniformly mixing nicotine with the first carrier, granulating after sufficient stirring, drying the obtained wet powder particles at 30 to 60℃, and controlling the moisture content to be 3wt% to 30wt% to obtain the nicotine particles; uniformly mixing the effective ingredient with the second carrier, granulating after sufficient stirring, drying the obtained wet powder particles at 30 to 60℃, and controlling the moisture content to be 3wt% to 30wt% to obtain the effective ingredient particles; mixing and stirring the obtained nicotine particles and the effective ingredient particles to obtain the oral nicotine product.

[0020] In some embodiments, in the preparation of the nicotine particles, the particles are collected after drying through a 16 to 80 mesh sieve; and / or in the preparation of the effective ingredient particles, the particles are collected after drying through a 16 to 80 mesh sieve.

[0021] In some embodiments, in the preparation of the nicotine particles, at least one of a binder, a flavoring agent, a pH regulator, a humectant, and a fragrance is added to mix with nicotine and the first carrier; and / or in the preparation of the effective ingredient particles, at least one of a binder, a flavoring agent, a pH regulator, a humectant, and a fragrance is added to mix with the effective ingredient and the second carrier.

[0022] Compared with the prior art, the technical scheme of the present disclosure has the following beneficial effects:

[0023] In the oral process, the effective ingredient in the effective ingredient particles is released in the stomach before the nicotine in the nicotine particles, and the effective ingredient acts on the stomach before the nicotine, thereby reducing the stimulation of nicotine on the stomach and improving the experience of taking the oral nicotine product.

[0024] Further, the second carrier in the active ingredient particles has better hydrophilicity than the first carrier in the nicotine particles, and is more easily dissolved in water in the oral environment, so that the active ingredient is released faster than nicotine and enters the stomach, thereby reducing the irritation of nicotine to the stomach.

[0025] Further, the particle size of the active ingredient particles is smaller than that of the nicotine particles, so that the active ingredient particles are more easily swallowed into the stomach with saliva, and the release time of the active ingredient is differentiated from that of nicotine, and the active ingredient that enters the stomach and is released first helps to reduce the irritation of nicotine to the stomach. DETAILED DESCRIPTION

[0026] The main active ingredient in oral nicotine products is nicotine, and commonly used nicotine includes free nicotine, nicotine salt, and nicotine ion exchange resin. Free nicotine and nicotine salt are released faster and can cause greater irritation to the oral cavity, throat, gastrointestinal tract, etc., resulting in heartburn, belching, stomach pain, and even vomiting and other discomforts.

[0027] US9538782B2 combines the use of antagonists of nicotinic acetylcholine receptors and antagonists of TRP ion channels to inhibit the sensory stimulation during the consumption of smokeless tobacco products. CN116194106A uses at least two antagonists to inhibit or block the activation of nicotinic acetylcholine receptors (nAChR) and / or transient receptor potential (TRP) ion channels in the gastrointestinal tract and oral cavity by nicotine agonists, thereby relieving nicotine irritation. US20220233463A1 uses at least one transient receptor potential (TRP) channel modulator to reduce throat irritation caused by inhaling vapor or particles of at least one material selected from cannabis, cannabinoids, tobacco, herbal plants, or combinations thereof. CN118120958A activates specific TRP channels by adding menthol, 1,8-eucalyptol, gingerol, and cinnamyl aldehyde, etc. in the atomized liquid, to reduce throat irritation and pain caused by free alkaloids, mainly applied in the field of electronic cigarettes.

[0028] The prior art reduces nicotine irritation mainly by directly adding antagonists of nicotinic acetylcholine receptors and / or TRP ion channels, which mainly reduces the irritation of nicotine to the oral cavity and throat, and has limited effect on reducing gastrointestinal irritation.

[0029] The embodiments of the present disclosure improve the release mechanism of the active ingredient that reduces nicotine irritation, so that the active ingredient is released into the stomach faster than nicotine, thereby effectively reducing the irritation of nicotine to the stomach.

[0030] The oral nicotine product provided by the embodiments of the present disclosure comprises: nicotine particles containing nicotine and a first carrier; and active ingredient particles containing an active ingredient and a second carrier, the active ingredient containing at least one ingredient suitable for reducing the irritation of nicotine to the stomach. During oral administration of the oral nicotine product, the active ingredient in the active ingredient particles is released in the stomach faster than the nicotine in the nicotine particles, and / or the active ingredient enters the stomach before the nicotine. Therefore, the oral nicotine product of the embodiments of the present disclosure, by virtue of the structural design of the double particles, the nicotine and the active ingredient are prepared into different particles respectively, the active ingredient in the active ingredient particles is released in the stomach faster than the nicotine in the nicotine particles, the active ingredient acts on the stomach, thereby reducing the irritation of nicotine to the stomach, effectively avoiding the occurrence of symptoms such as heartburn, belching, vomiting, stomach pain and the like in the user, and improving the experience of oral administration of the oral nicotine product, especially for first-time users or people with lower nicotine tolerance. At the same time, the active ingredient for reducing irritation does not affect the oral release effect of nicotine, nor does it produce any additional irritation or side effects.

[0031] In some embodiments, the second carrier has better hydrophilicity than the first carrier, that is, the second carrier has better water solubility than the first carrier and is more easily dissolved in saliva in the oral environment, so that the active ingredient mixed therewith is released faster than nicotine.

[0032] In some embodiments, the first carrier has strong oral adhesion and hydrophobicity, and good film-forming property; in some embodiments, the first carrier comprises one or more of microcrystalline cellulose, cellulose derivatives, plant fibers, and starch derivatives.

[0033] In some embodiments, the first carrier comprises cellulose derivatives: one or more of hydroxypropyl methylcellulose (HPMC), hydroxyethyl cellulose (HEC), hydroxypropyl cellulose (HPC), methylcellulose, ethyl hydroxyethyl cellulose, carboxymethyl cellulose, modified cellulose gum, and sodium carboxymethyl cellulose (NaCMC).

[0034] In some embodiments, the first carrier comprises microcrystalline cellulose.

[0035] In some embodiments, the first carrier comprises plant fibers: one or more of coconut shell fiber powder, bamboo fiber powder, peanut shell fiber, oat fiber powder, cocoa shell powder, tea fiber powder, coffee residue powder, sugarcane fiber powder, apple fiber powder, citrus fiber powder, cassava fiber powder, flaxseed powder, pea fiber powder, wheat fiber powder, and soybean fiber powder.

[0036] In some embodiments, the first carrier includes one or more of starch derivatives: denatured starch, cross-linked starch.

[0037] In some embodiments, the nicotine in the nicotine particles includes at least one of: free nicotine, nicotine salt, nicotine ion exchange resin; free nicotine is free state nicotine that is not combined with other compounds, nicotine salt is a compound formed by the combination of nicotine and organic acid, and nicotine ion exchange resin is a stable complex formed by the ion exchange between nicotine and resin.

[0038] In some embodiments, the amount of nicotine in the nicotine particles is adjusted to make the nicotine release at a more suitable speed; in some embodiments, the mass fraction of nicotine in the nicotine particles is 1wt%~10wt%, and specific examples can be 3.25%~5.2% and the like; in some embodiments, the mass fraction of the first carrier in the nicotine particles is 30wt%~80wt%, and specific examples can be 77.3%~79.25% and the like.

[0039] In some embodiments, the second carrier includes one or more of: soluble starch, lactose, sucrose; the second carrier has better hydrophilicity than the first carrier.

[0040] In some embodiments, the second carrier includes lactose and / or sucrose, which has good hydrophilicity and faster water solubility, and helps to release the active ingredients faster.

[0041] In some embodiments, the active ingredients include one or more of the following: active ingredients based on the mechanism of blocking the nicotine acetylcholine receptor and / or transient receptor potential ion channel to receive nicotine stimulation; active ingredients based on the mechanism of neutralizing gastric acid and reducing gastric acid secretion to quickly relieve stomach heartburn; active ingredients based on the mechanism of forming a gel barrier to protect the stomach wall; active ingredients based on the mechanism of anti-inflammatory and antioxidant, reducing gastric acid secretion, and promoting nicotine metabolism to reduce nicotine stimulation.

[0042] In some embodiments, the active ingredients include active ingredients based on the mechanism of blocking the nicotine acetylcholine receptor and / or transient receptor potential ion channel to receive nicotine stimulation, and specifically include one or more combinations of the following: ginger extract, ginger oleoresin, curcumin, 6-gingerol, 6-shogaol, borneol, isoborneol, borneol acetate, monobornyl succinate, monoisobornyl succinate, glycerol oxalate, monobornyl formate, menthol, cinnamaldehyde, eucalyptol (1,8-cineole), WS-3, WS-23, WS-12, carvacrol, carveol, menthol.

[0043] In some embodiments, the effective component has a faster release rate by adjusting the amount of the effective component and the second carrier in the effective component particles; in some embodiments, the mass fraction of the effective component in the effective component particles is 1wt%-60wt%, and specifically for example, can be 16%-40% and the like; in some embodiments, the mass fraction of the second carrier in the effective component particles is 20wt%-70wt%, and specifically for example, can be 30%-65%, 35%-59.6% and the like.

[0044] In some embodiments, the particle size of the effective component particles is the same as the particle size of the nicotine particles. In some embodiments, the particle size of the effective component particles is 16-80 mesh (0.18-1.2mm), and the particle size of the nicotine particles is 16-80 mesh (0.18-1.2mm); in some embodiments, the particle size of the effective component particles is 16-50 mesh (0.30-1.2mm), and the particle size of the nicotine particles is 16-50 mesh (0.30-1.2mm); in some embodiments, the particle size of the effective component particles is 30-35 mesh (0.50-0.59mm), and in some embodiments, the particle size of the nicotine particles is 30-35 mesh (0.50-0.59mm). In the case that the second carrier in the effective component particles has better hydrophilicity than the first carrier in the nicotine particles, controlling the particle size of the effective component particles to be the same as the particle size of the nicotine particles helps to ensure that the effective component is released faster than the nicotine.

[0045] It should be noted that the effective component particles and the nicotine particles of the embodiments of the present disclosure are collected by a specific number of sieves after granulation to obtain effective component particles and nicotine particles with a specific particle size range.

[0046] In some embodiments of the oral nicotine product of the embodiments of the present disclosure, the particle size of the effective component particles is smaller than the particle size of the nicotine particles, so that the effective component particles are more easily swallowed with saliva into the stomach, realizing the differentiation of the release time of the effective component and the nicotine, and the effective component that enters the stomach and is released first helps to reduce the irritation of nicotine to the stomach.

[0047] In some embodiments, the particle size of the active ingredient particles is 15% to 80% of the particle size of the nicotine particles, and can be specifically, for example, 18% to 65%. By controlling the ratio of the particle sizes of the active ingredient particles and the nicotine particles, the release time difference between the active ingredient and the nicotine can be more accurately controlled, so as to ensure that the release of the active ingredient does not affect the pleasure and stimulation brought by the release of nicotine in the oral cavity, while ensuring that the active ingredient is released faster in the stomach to reduce the stimulation of nicotine to the stomach, thereby avoiding the stimulation of nicotine to the stomach while ensuring that nicotine brings pleasure, and improving the user's experience. In some embodiments, the particle size of the active ingredient particles is 15% to 50% of the particle size of the nicotine particles, and can be specifically, for example, 18% to 45%, 18% to 25%, or 32% to 42%, and the like. Further reducing the ratio of the particle size of the active ingredient particles to the particle size of the nicotine particles can further improve the release speed of the active ingredient, thereby further reducing the stimulation of nicotine to the stomach.

[0048] In some embodiments, the particle size of the nicotine particles is 16 to 50 mesh (0.30 to 1.2 mm), and the particle size of the active ingredient particles is 30 to 80 mesh (0.18 to 0.59 mm).

[0049] In some embodiments, the particle size of the nicotine particles is 18 to 20 mesh (0.85 to 1.00 mm), and the particle size of the active ingredient particles is 30 to 35 mesh (0.50 to 0.59 mm).

[0050] In some embodiments, the particle size of the nicotine particles is 18 to 20 mesh (0.85 to 1.00 mm), and the particle size of the active ingredient particles is 70 to 80 mesh (0.18 to 0.21 mm).

[0051] In some embodiments, the particle size of the nicotine particles is 18 to 35 mesh (0.50 to 1.00 mm), and the particle size of the active ingredient particles is 70 to 80 mesh (0.18 to 0.21 mm).

[0052] In some embodiments, the particle size of the nicotine particles is 30 to 35 mesh (0.50 to 0.59 mm), and the particle size of the active ingredient particles is 70 to 80 mesh (0.18 to 0.21 mm).

[0053] In some embodiments, the first carrier and the second carrier contain different ingredients; in some embodiments, the first carrier and the second carrier contain the same ingredients, such as microcrystalline cellulose, cellulose derivatives, plant fibers, or starch derivatives.

[0054] In some embodiments, the particle size of the active ingredient particles is smaller than that of the nicotine particles, and the second carrier in the active ingredient particles has better hydrophilicity than the first carrier in the nicotine particles, so that the active ingredient is released before nicotine and acts on the stomach, thereby reducing the irritation of nicotine to the stomach.

[0055] In some embodiments, the mass ratio of the nicotine particles to the active ingredient particles is 1:1 to 4:1, specifically for example 2:1 or 3:1, and the like.

[0056] The oral nicotine product of the embodiments of the present disclosure, in some embodiments, in addition to including nicotine particles and active ingredient particles, also includes one or at least two of the following ingredients: a binder, a flavoring agent, a humectant, a pH regulator, a fragrance.

[0057] In some embodiments, the binder is one or a combination of at least two of the following ingredients: malt dextrin, sodium alginate, gum arabic, cellulose, carboxymethyl cellulose, starch, liquid glucose, gelatin, copovidone, hydroxypropyl cellulose, carrageenan, xanthan gum, guar gum.

[0058] In some embodiments, the mass fraction of the binder in the oral nicotine product is 1wt% to 30wt%.

[0059] In some embodiments, the flavoring agent is one or a combination of at least two of the following ingredients: sucrose, aspartame, sucralose, acesulfame potassium, stevioside.

[0060] In some embodiments, the mass fraction of the flavoring agent in the oral nicotine product is 0.5wt% to 15wt%.

[0061] In some embodiments, the humectant is one or a combination of at least two of the following ingredients: glycerol, propylene glycol, mannitol, sorbitol, maltitol, xylitol.

[0062] In some embodiments, the mass fraction of the humectant in the oral nicotine product is 1wt% to 10wt%.

[0063] In some embodiments, the pH regulator is one or a combination of at least two of the following ingredients: sodium carbonate, sodium bicarbonate, calcium carbonate, sodium citrate, calcium bicarbonate, potassium bicarbonate, citric acid, tartaric acid.

[0064] In some embodiments, the mass fraction of the pH regulator in the oral nicotine product is 1wt% to 3wt%.

[0065] In some embodiments, the flavoring is one or a combination of at least two of the following ingredients: mint, orange oil, vanilla, wintergreen, cinnamon, spearmint, vanillin, clove, cardamom, rose essential oil, sage, jasmine, cherry, blueberry, watermelon, lemon, honey, coffee, raspberry, ginger, goji, cocoa.

[0066] In some embodiments, the flavoring has a mass fraction of 0.5wt% to 10wt% in the oral nicotine product.

[0067] The oral nicotine product of the embodiments of the present disclosure, in some embodiments, is packaged in a mouth pouch to form a product.

[0068] The embodiments of the present disclosure also provide a preparation method of the oral nicotine product of any of the above embodiments, the preparation method comprising: mixing nicotine particles and active ingredient particles to form the oral nicotine product.

[0069] In some embodiments, the preparation method of the oral nicotine product comprises:

[0070] S1: uniformly mixing nicotine and a first carrier, granulating after sufficient stirring, drying the obtained wet powder particles at 30-60°C, controlling the water content to be 3wt%-30wt%, and preparing nicotine particles;

[0071] S2: uniformly mixing active ingredients and a second carrier, granulating after sufficient stirring, drying the obtained wet powder particles at 30-60°C, controlling the water content to be 3wt%-30wt%, and preparing active ingredient particles;

[0072] S3: mixing and stirring the prepared nicotine particles and active ingredient particles to obtain an oral nicotine product.

[0073] In S1, in some embodiments, the nicotine particles are collected through a 16-80 mesh sieve after drying; in some embodiments, the nicotine particles are collected through a 16-50 mesh sieve after drying; in some embodiments, the nicotine particles are collected through an 18-20 mesh sieve after drying, and nicotine particles with a particle size of 18-20 mesh (0.85mm-1.00mm) are collected; in some embodiments, the nicotine particles are collected through a 30-35 mesh sieve after drying, and nicotine particles with a particle size of 30-35 mesh (0.50mm-0.59mm) are collected.

[0074] In S2, in some embodiments, the effective ingredient particles are collected through a 16-80 mesh sieve after drying; in some embodiments, the effective ingredient particles are collected through a 16-50 mesh sieve after drying; in some embodiments, the effective ingredient particles are collected through a 30-35 mesh sieve after drying, and the effective ingredient particles with a particle size of 30-35 mesh (0.50-0.59 mm) are collected; in some embodiments, the effective ingredient particles are collected through a 70-80 mesh sieve after drying, and the effective ingredient particles with a particle size of 70-80 mesh (0.18-0.21 mm) are collected.

[0075] In some embodiments, in S1, the nicotine particles with a particle size of 18-20 mesh (0.85-1.00 mm) are collected through a 18-20 mesh sieve; in S2, the effective ingredient particles with a particle size of 30-35 mesh (0.50-0.59 mm) are collected through a 30-35 mesh sieve.

[0076] In some embodiments, in S1, the nicotine particles with a particle size of 18-20 mesh (0.85-1.00 mm) are collected through a 18-20 mesh sieve; in S2, the effective ingredient particles with a particle size of 70-80 mesh (0.18-0.21 mm) are collected through a 70-80 mesh sieve.

[0077] In some embodiments, in S1, the nicotine particles with a particle size of 30-35 mesh (0.50-0.59 mm) are collected through a 30-35 mesh sieve; in S2, the effective ingredient particles with a particle size of 70-80 mesh (0.18-0.21 mm) are collected through a 70-80 mesh sieve.

[0078] In some embodiments, in S1, the nicotine particles with a particle size of 30-35 mesh (0.50-0.59 mm) are collected through a 30-35 mesh sieve; in S2, the effective ingredient particles with a particle size of 30-35 mesh (0.50-0.59 mm) are collected through a 30-35 mesh sieve.

[0079] In S1 and S2, the drying of the wet powder particles at 30-60°C can be performed in an oven.

[0080] In some embodiments, in S1, the mass fraction of the added nicotine is 1wt%-10wt% of the total mass of the raw materials for preparing the nicotine particles, and can be specifically, for example, 3.25%-5.2% and the like.

[0081] In some embodiments, in S1, the mass fraction of the added first carrier is 30wt%-80wt% of the total mass of the raw materials for preparing the nicotine particles, and can be specifically, for example, 77.3%-79.25% and the like.

[0082] In some embodiments, in S2, the mass fraction of the added active ingredient is 1wt% to 60wt% of the total mass of the raw materials for preparing the active ingredient particles, and specifically for example, can be 16% to 40% and the like.

[0083] In some embodiments, in S2, the mass fraction of the added second carrier is 20wt% to 70wt% of the total mass of the raw materials for preparing the active ingredient particles, and specifically for example, can be 30% to 65%, 35% to 59.6% and the like.

[0084] In S1, in some embodiments, at least one of the binder, the flavoring agent, the pH adjusting agent, the humectant, and the essence is mixed with the nicotine and the first carrier.

[0085] In S2, in some embodiments, at least one of the binder, the flavoring agent, the pH adjusting agent, the humectant, and the essence is mixed with the active ingredient and the second carrier.

[0086] The specific components of the binder, the flavoring agent, the pH adjusting agent, the humectant, and the essence are as described above, and will not be repeated here.

[0087] In some embodiments, by adjusting the amount of the binder added in S1 and / or S2, the mass fraction of the binder in the prepared oral nicotine product is 1wt% to 30wt%.

[0088] In some embodiments, by adjusting the amount of the flavoring agent added in S1 and / or S2, the mass fraction of the flavoring agent in the prepared oral nicotine product is 0.5wt% to 15wt%.

[0089] In some embodiments, by adjusting the amount of the humectant added in S1 and / or S2, the mass fraction of the humectant in the prepared oral nicotine product is 1wt% to 10wt%.

[0090] In some embodiments, by adjusting the amount of the pH adjusting agent added in S1 and / or S2, the mass fraction of the pH adjusting agent in the prepared oral nicotine product is 1wt% to 3wt%.

[0091] In some embodiments, by adjusting the amount of the essence added in S1 and / or S2, the mass fraction of the essence in the prepared oral nicotine product is 0.5wt% to 10wt%.

[0092] In S3, in some embodiments, the mixing mass ratio of the nicotine particles to the active ingredient particles is 4:1 to 1:1.

[0093] In S3, in some embodiments, the nicotine particles and the active ingredient particles are mixed, stirred in a mixer, and the prepared oral nicotine product is packaged into a mouth bag to produce the product.

[0094] The present disclosure is further illustrated by specific examples below.

[0095] Examples

[0096] Test method description

[0097] User evaluation: The user evaluates the use experience, sensory feeling, etc. of the oral nicotine product through user evaluation, specifically including:

[0098] A test team consisting of 8 trained evaluators evaluates the nicotine mouth bag composition, each evaluator evaluates all samples 3 times within 30 minutes to take an average score, and gives a score from the burping frequency, burping intensity, nausea duration, nausea intensity, and comprehensive experience five evaluation dimensions, and the score of each dimension of each nicotine mouth bag composition is the average score of the scores of 8 evaluators, and the evaluation standard is as shown in Table 1,

[0099] Table 1 Sensory evaluation standard

[0100]

[0101] The evaluation result is the sum of the scores of the five dimensions, and the total score <17 is evaluated as general; 17 < total score <20 is evaluated as good; 20 < total score <22 is evaluated as better; and total score >22 is evaluated as excellent.

[0102] Example 1

[0103] (1) Preparation of nicotine particles

[0104] Take 77.3g of microcrystalline cellulose, 2g of maltodextrin, 0.1g of acesulfame potassium, 0.5g of strawberry flavor, and 1.8g of sodium bicarbonate, mix them evenly with a mixer to obtain a dry powder mixture, then mix 5.2g of benzoic acid nicotine salt, 5g of water, and 8g of glycerol evenly to obtain a mixed solution, pour the dry powder mixture into the mixed solution, stir for 30min until it is evenly stirred to obtain a wet powder mixture, and then dry the wet powder mixture in an oven at 60°C until the moisture content is 5%. Adopt a grading screening process to control the particle size distribution, pass through 18 and 20 mesh sieves at the same time, so that the particle size is controlled between 18-20 mesh (0.85mm-1.00mm), and then package.

[0105] (2) Preparation of active ingredient particles

[0106] Take microcrystalline cellulose 59.6g, ginger extract 8g, borneol 8g, malt dextrin 2g, erythritol 2.0g, strawberry flavor 0.5g, sodium bicarbonate 1.8g, mix evenly with a mixer to get a dry powder mixture, then mix 5g water, 8g glycerol evenly to get a mixed solution, pour the dry powder mixture into the mixed solution and stir for 30min until evenly stirred to get a wet powder mixture, granulate the wet powder mixture, and dry the obtained wet powder particles in an oven at 60°C until the moisture content is 5%. Adopt a grading screening process to regulate the particle size distribution, pass through 30 and 35 mesh sieves at the same time, control the particle size between 30~35 mesh (0.50mm~0.59mm), and then bag.

[0107] (3) Take nicotine particles 50g, effective ingredient particles 50g, mix evenly, bag with 400mg per bag, and nicotine buccal bag composition is obtained.

[0108] Example 2

[0109] (1) Preparation of nicotine particles

[0110] Take microcrystalline cellulose 59.6g, ginger extract 8g, borneol 8g, malt dextrin 2g, erythritol 2.0g, strawberry flavor 0.5g, sodium bicarbonate 1.8g, mix evenly with a mixer to get a dry powder mixture, then mix 5g water, 8g glycerol evenly to get a mixed solution, pour the dry powder mixture into the mixed solution and stir for 30min until evenly stirred to get a wet powder mixture, granulate the wet powder mixture, and dry the obtained wet powder particles in an oven at 60°C until the moisture content is 5%. Adopt a grading screening process to regulate the particle size distribution, pass through 30 and 35 mesh sieves at the same time, control the particle size between 30~35 mesh (0.50mm~0.59mm), and then bag.

[0111] (2) Preparation of effective ingredient particles

[0112] Take microcrystalline cellulose 59.6g, ginger extract 8g, borneol 8g, malt dextrin 2g, erythritol 2.0g, strawberry flavor 0.5g, sodium bicarbonate 1.8g, mix evenly with a mixer to get a dry powder mixture, then mix 5g water, 8g glycerol evenly to get a mixed solution, pour the dry powder mixture into the mixed solution and stir for 30min until evenly stirred to get a wet powder mixture, granulate the wet powder mixture, and dry the obtained wet powder particles in an oven at 60°C until the moisture content is 5%. Adopt a grading screening process to regulate the particle size distribution, pass through 30 and 35 mesh sieves at the same time, control the particle size between 30~35 mesh (0.50mm~0.59mm), and then bag.

[0113] (3) Take nicotine particles 50 g, effective ingredient particles 50 g, mix evenly, and bag at 400 mg per bag, to obtain nicotine pouch bag composition.

[0114] Example 3

[0115] (1) Preparation of nicotine particles

[0116] Take microcrystalline cellulose 77.3 g, malt dextrin 2 g, acesulfame 0.1 g, strawberry flavor 0.5 g, sodium bicarbonate 1.8 g, mix evenly with a mixer to obtain a dry powder mixture, then mix 5.2 g of benzoic acid nicotine salt, 5 g of water, and 8 g of glycerol evenly to obtain a mixed solution, pour the dry powder mixture into the mixed solution, stir for 30 min until evenly stirred to obtain a wet powder mixture, and then dry the wet powder mixture in a 60°C oven until the moisture content is 5%. Adopt a grading screening process to regulate the particle size distribution, pass through 18 and 20 mesh sieves at the same time, control the particle size between 18-20 mesh (0.85-1.00 mm), and then bag.

[0117] (2) Preparation of effective ingredient particles

[0118] Take lactose 59.6 g, ginger extract 8 g, borneol 8 g, malt dextrin 2 g, erythritol 2.0 g, strawberry flavor 0.5 g, sodium bicarbonate 1.8 g, mix evenly with a mixer to obtain a dry powder mixture, then mix 5 g of water and 8 g of glycerol evenly to obtain a mixed solution, pour the dry powder mixture into the mixed solution, stir for 30 min until evenly stirred to obtain a wet powder mixture, and then dry the wet powder mixture in a 60°C oven until the moisture content is 5%. Adopt a grading screening process to regulate the particle size distribution, pass through 30 and 35 mesh sieves at the same time, control the particle size between 30-35 mesh (0.50-0.59 mm), and then bag.

[0119] (3) Take nicotine particles 50 g, effective ingredient particles 50 g, mix evenly, and bag at 400 mg per bag, to obtain nicotine pouch bag composition.

[0120] Example 4

[0121] (1) Preparation of nicotine particles

[0122] Take 79.25 g of microcrystalline cellulose, 2 g of malt dextrin, 0.1 g of acesulfame potassium, 0.5 g of strawberry flavor, and 1.8 g of sodium bicarbonate, mix them evenly with a mixer to obtain a dry powder mixture. Then mix 3.25 g of benzoic acid nicotine salt, 5 g of water, and 8 g of glycerol evenly to obtain a mixed solution. Pour the dry powder mixture into the mixed solution and stir for 30 min until it is evenly stirred to obtain a wet powder mixture. Granulate the wet powder mixture, and place the obtained wet powder particles in a 60°C oven for drying treatment until the moisture content is 5%. Use a fractional sieving process to regulate the particle size distribution, pass it through 18 and 20 mesh sieves at the same time, control the particle size between 18-20 mesh (0.85-1.00 mm), and then bag it.

[0123] (2) Preparation of active ingredient particles

[0124] Take 35.6 g of lactose, 20 g of ginger extract, 20 g of borneol, 2 g of malt dextrin, 2.0 g of erythritol, 0.5 g of strawberry flavor, and 1.8 g of sodium bicarbonate, mix them evenly with a mixer to obtain a dry powder mixture. Then mix 5 g of water and 8 g of glycerol evenly to obtain a mixed solution. Pour the dry powder mixture into the mixed solution and stir for 30 min until it is evenly stirred to obtain a wet powder mixture. Granulate the wet powder mixture, and place the obtained wet powder particles in a 60°C oven for drying treatment until the moisture content is 5%. Use a fractional sieving process to regulate the particle size distribution, pass it through 30 and 35 mesh sieves at the same time, control the particle size between 30-35 mesh (0.50-0.59 mm), and then bag it.

[0125] Take 80 g of nicotine particles and 20 g of active ingredient particles, mix them evenly, bag them at 400 mg per bag, and obtain a nicotine oral pouch composition.

[0126] Example 5

[0127] (1) Preparation of nicotine particles

[0128] Take 77.3 g of microcrystalline cellulose, 2 g of malt dextrin, 0.1 g of acesulfame potassium, 0.5 g of strawberry flavor, and 1.8 g of sodium bicarbonate, mix them evenly with a mixer to obtain a dry powder mixture. Then mix 5.2 g of benzoic acid nicotine salt, 5 g of water, and 8 g of glycerol evenly to obtain a mixed solution. Pour the dry powder mixture into the mixed solution and stir for 30 min until it is evenly stirred to obtain a wet powder mixture. Granulate the wet powder mixture, and place the obtained wet powder particles in a 60°C oven for drying treatment until the moisture content is 5%. Use a fractional sieving process to regulate the particle size distribution, pass it through 18 and 20 mesh sieves at the same time, control the particle size between 18-20 mesh (0.85-1.00 mm), and then bag it.

[0129] (2) Preparation of active ingredient particles

[0130] Take lactose 59.6g, ginger extract 8g, borneol 8g, malt dextrin 2g, erythritol 2.0g, strawberry flavor 0.5g, sodium bicarbonate 1.8g, mix evenly with a mixer to get a dry powder mixture, then mix 5g water, 8g glycerol evenly to get a mixed solution, pour the dry powder mixture into the mixed solution and stir for 30min until evenly stirred to get a wet powder mixture, granulate the wet powder mixture, and dry the obtained wet powder particles in an oven at 60℃ until the moisture content is 5%. Adopt a grading screening process to regulate the particle size distribution, and pass through 70 and 80 mesh sieves at the same time, so that the particle size is controlled between 70~80 mesh (0.18mm~0.21mm), and then bagging.

[0131] (3) Take nicotine particles 50g, effective ingredient particles 50g, mix evenly, and bagging with 400mg per bag to get nicotine buccal bag composition.

[0132] Example 6

[0133] (1) Preparation of nicotine particles

[0134] Take microcrystalline cellulose 77.3g, malt dextrin 2g, acesulfame potassium 0.1g, strawberry flavor 0.5g, sodium bicarbonate 1.8g, mix evenly with a mixer to get a dry powder mixture, then mix 5.2g benzoic acid nicotine salt, 5g water, 8g glycerol evenly to get a mixed solution, pour the dry powder mixture into the mixed solution and stir for 30min until evenly stirred to get a wet powder mixture, granulate the wet powder mixture, and dry the obtained wet powder particles in an oven at 60℃ until the moisture content is 5%. Adopt a grading screening process to regulate the particle size distribution, and pass through 30 and 35 mesh sieves at the same time, so that the particle size is controlled between 30~35 mesh (0.50mm~0.59mm), and then bagging.

[0135] (2) Preparation of effective ingredient particles

[0136] Take lactose 59.6g, ginger extract 8g, borneol 8g, malt dextrin 2g, erythritol 2.0g, strawberry flavor 0.5g, sodium bicarbonate 1.8g, mix evenly with a mixer to get a dry powder mixture, then mix 5g water, 8g glycerol evenly to get a mixed solution, pour the dry powder mixture into the mixed solution and stir for 30min until evenly stirred to get a wet powder mixture, granulate the wet powder mixture, and dry the obtained wet powder particles in an oven at 60℃ until the moisture content is 5%. Adopt a grading screening process to regulate the particle size distribution, and pass through 70 and 80 mesh sieves at the same time, so that the particle size is controlled between 70~80 mesh (0.18mm~0.21mm), and then bagging.

[0137] (3) Take nicotine particles 50 g, effective ingredient particles 50 g, mix evenly, bag 400 mg per bag, get nicotine pouch bag composition.

[0138] Example 7

[0139] (1) Preparation of nicotine particles

[0140] Take 77.3 g of coconut shell fiber, 2 g of malt dextrin, 0.1 g of acesulfame potassium, 0.5 g of strawberry flavor, 1.8 g of sodium bicarbonate, mix evenly with a mixer to get dry powder mixture, then mix 5.2 g of nicotine benzoate salt, 5 g of water, 8 g of glycerol evenly to get mixed solution, pour the dry powder mixture into the mixed solution and stir for 30 min until evenly stirred to get wet powder mixture, dry the wet powder mixture in an oven at 60°C until the moisture content is 5%. Adopt the classification screening process to regulate the particle size distribution, pass through 18 mesh and 20 mesh screens at the same time, control the particle size between 18-20 mesh (0.85mm-1.00mm), then bag.

[0141] (2) Preparation of effective ingredient particles

[0142] Take 59.6 g of sucrose, 8 g of ginger extract, 8 g of borneol, 2 g of malt dextrin, 2.0 g of erythritol, 0.5 g of strawberry flavor, 1.8 g of sodium bicarbonate, mix evenly with a mixer to get dry powder mixture, then mix 5 g of water, 8 g of glycerol evenly to get mixed solution, pour the dry powder mixture into the mixed solution and stir for 30 min until evenly stirred to get wet powder mixture, dry the wet powder mixture in an oven at 60°C until the moisture content is 5%. Adopt the classification screening process to regulate the particle size distribution, pass through 30 mesh and 35 mesh screens at the same time, control the particle size between 30-35 mesh (0.50mm-0.59mm), then bag.

[0143] (3) Take nicotine particles 50 g, effective ingredient particles 50 g, mix evenly, bag 400 mg per bag, get nicotine pouch bag composition.

[0144] Comparative Example 1

[0145] Take 71.9 g of microcrystalline cellulose, 0.1 g of acesulfame potassium, 0.5 g of strawberry flavor, 1.8 g of sodium bicarbonate, 4.0 g of ginger extract, 4.0 g of borneol, 0.1 g of potassium sorbate, mix evenly to get dry mixed powder;

[0146] Then mix 2.6 g of nicotine benzoate salt, 5.0 g of water, 8.0 g of glycerol, 2.0 g of malt dextrin evenly to get mixed solution;

[0147] The dry mixed powder is added to the mixed solution and stirred until uniform. After complete mixing, wet granulation is performed. The obtained wet powder particles are dried until the moisture content is 5%. A grading sieving process is used to regulate the particle size distribution. The particles are simultaneously sieved through a 30 mesh sieve and a 35 mesh sieve to control the particle size between 30-35 mesh (0.50mm-0.59mm). The particles are then bagged to obtain the nicotine pouch composition.

[0148] Comparative Example 2

[0149] 71.9g of microcrystalline cellulose, 0.1g of acesulfame, 0.5g of strawberry flavor, 1.8g of sodium bicarbonate, 4.0g of ginger extract, 4.0g of borneol, and 0.1g of potassium sorbate are uniformly mixed to obtain a dry mixed powder;

[0150] 2.6g of benzoic acid nicotine salt, 5.0g of water, 8.0g of glycerol, and 2.0g of maltodextrin are uniformly mixed to obtain a mixed solution;

[0151] The dry mixed powder is added to the mixed solution and stirred until uniform. After complete mixing, wet granulation is performed. The obtained wet powder particles are dried until the moisture content is 5%. A grading sieving process is used to regulate the particle size distribution. The particles are simultaneously sieved through an 18 mesh sieve and a 20 mesh sieve to control the particle size between 18-20 mesh (0.85mm-1.00mm). The particles are then bagged to obtain the nicotine pouch composition.

[0152] To more clearly show the components, content, particle size, etc. in the nicotine pouch composition in each of the examples, Table 2-Table 4 lists the relevant information.

[0153] Table 2: Content of each component in the nicotine pouch composition of Example 1-Example 7

[0154]

[0155] Table 3: Content of each component in the nicotine granules of Example 1-Example 7

[0156]

[0157] Table 4: Content of each component in the active ingredient granules of Example 1-Example 7

[0158]

[0159] The nicotine pouches prepared in Example 1-Example 7 and Comparative Example 1-Comparative Example 2 are respectively subjected to user evaluation. The evaluation results are shown in Table 5 below.

[0160] Table 5: Sensory evaluation score

[0161]

[0162] According to the evaluation results in Table 5, compared with the nicotine pouches prepared in Comparative Example 1 and Comparative Example 2, in which the active ingredients were added but no nicotine particle granulation and active ingredient particle granulation were performed, the nicotine pouches prepared in Example 1 to Example 7, in which nicotine particle granulation and active ingredient particle granulation were performed, scored higher in terms of burping, nausea, stomach burning, acid reflux, and overall experience during the test.

[0163] According to the evaluation results in Table 5, compared with Example 1, in which only particle size regulation (the carrier in the nicotine particles and the carrier in the active ingredient particles (with a smaller particle size) were different in particle size, and the components were the same), and Example 2, in which only carrier component regulation (the carrier in the nicotine particles and the carrier in the active ingredient particles (with better hydrophilicity) were different in component, and the particle sizes were the same), Example 3 to Example 7 simultaneously regulated the particle size and the carrier component (the carrier in the nicotine particles and the carrier in the active ingredient particles (with better hydrophilicity and smaller particle size) were different in both component and particle size), and showed better sensory evaluation during the test.

[0164] According to the evaluation results in Table 5, compared with Example 3 to Example 4, the carriers were the same in Example 5 to Example 6, and the ratio of the particle size of the active ingredient particles to the particle size of the nicotine particles was smaller, so that the active ingredient could be released faster, further reducing the sensory irritation of nicotine to the user, improving the taking experience, and the effect evaluation results were better during the test.

[0165] The above-described embodiments are merely exemplary embodiments adopted for the purpose of illustrating the principles of the present disclosure, and are not intended to limit the protection scope of the present disclosure. Various modifications and improvements can be made by those of ordinary skill in the art without departing from the spirit and essential characteristics of the present disclosure, and these modifications and improvements are also within the protection scope of the present disclosure.

Claims

1. An oral nicotine product, characterized in that, include: Nicotine particles, containing nicotine and a primary carrier; Active ingredient particles, comprising an active ingredient and a second carrier, wherein the active ingredient comprises at least one component suitable for reducing the stomach irritation caused by nicotine; In this oral nicotine product, during oral administration, the active ingredient in the active ingredient granules is released into the stomach in a manner superior to that of the nicotine in the nicotine granules.

2. The oral nicotine product according to claim 1, characterized in that, The second carrier has better hydrophilicity than the first carrier.

3. The oral nicotine product according to claim 2, characterized in that, The first carrier includes one or more of the following: microcrystalline cellulose, cellulose derivatives, plant fibers, and starch derivatives.

4. The oral nicotine product according to claim 3, characterized in that, The first carrier includes one or more of the following: hydroxypropyl methylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, methylcellulose, ethyl hydroxyethylcellulose, carboxymethylcellulose, modified cellulose gum and sodium carboxymethylcellulose, microcrystalline cellulose, coconut shell fiber powder, bamboo fiber powder, peanut shell fiber, oat fiber powder, cocoa shell powder, tea fiber powder, coffee grounds powder, sugarcane fiber powder, apple fiber powder, citrus fiber powder, cassava fiber powder, flaxseed powder, pea fiber powder, wheat fiber powder, soybean fiber powder, modified starch, and cross-linked starch.

5. The oral nicotine product according to claim 2, characterized in that, The second carrier includes one or more of soluble starch, lactose, and sucrose.

6. The oral nicotine product according to claim 1, characterized in that, The mass ratio of the nicotine particles to the active ingredient particles is 1:1 to 4:

1.

7. The oral nicotine product according to claim 1, characterized in that, The mass fraction of the first carrier in the nicotine particles is 30wt%~80wt%, and the mass fraction of the second carrier in the active ingredient particles is 20wt%~70wt%.

8. The oral nicotine product according to claim 1, characterized in that, The active ingredients include at least one of the following: ginger extract, gingerol, curcumin, 6-shogaol, 6-shogaol, borneol, isoborneol, borneol acetate, monoborneol succinate, monoisoborneol succinate, glyceryl oxalate, monoborneol formate, menthol, cinnamaldehyde, eucalyptol (1,8-cineole), WS-3, WS-23, WS-12, carvacrol, carvacrol, menthol, acetate, phosphate, citrate, carbonate, bicarbonate, borate, sodium alginate, potassium alginate, ammonium alginate; soybean lecithin, exogenous phospholipids, pectin, magnesium aluminum carbonate, bismuth potassium citrate, magnesium oxide, L-glutamine, tea polysaccharide, Ganoderma lucidum polysaccharide, green tea extract, ascorbic acid, taurine, quercetin, resveratrol, carotenoids, anthocyanins.

9. The oral nicotine product according to claim 1, characterized in that, Also includes: 1wt% to 30wt% of binders, and / or 0.5wt% to 15wt% of flavoring agents, and / or 1wt% to 10wt% of humectants, and / or 1wt% to 3wt% of pH adjusters, and / or 0.5wt% to 10wt% of fragrances.

10. The oral nicotine product according to any one of claims 1 to 9, characterized in that, The particle size of the active ingredient particles is smaller than that of the nicotine particles.

11. The oral nicotine product according to claim 10, characterized in that, The particle size of the active ingredient is 15% to 80% of the particle size of the nicotine particles.

12. The oral nicotine product according to claim 10, characterized in that, The particle size of the active ingredient particles is 15% to 50% of the particle size of the nicotine particles.

13. The oral nicotine product according to claim 10, characterized in that, The nicotine particles have a particle size of 16-50 mesh.

14. A method for preparing an oral nicotine product as described in any one of claims 1 to 13, characterized in that, include: Nicotine is mixed evenly with the first carrier, and after thorough stirring, it is granulated. The resulting wet powder granules are dried at 30~60℃, and the moisture content is controlled to be 3wt%~30wt% to obtain the nicotine granules. The active ingredient is mixed evenly with the second carrier, and after thorough stirring, it is granulated. The resulting wet powder particles are dried at 30~60℃, and the moisture content is controlled to be 3wt%~30wt% to obtain the active ingredient particles. The prepared nicotine granules are mixed and stirred with the active ingredient granules to obtain the oral nicotine product.

15. The preparation method according to claim 14, characterized in that, In the preparation of the nicotine granules, the granules are collected after drying through a 16-80 mesh sieve; and / or In the preparation of the active ingredient granules, the granules are collected after drying through a 16-80 mesh sieve.

16. The preparation method according to claim 14, characterized in that, In the preparation of the nicotine granules, at least one of a binder, flavoring agent, pH adjuster, humectant, and fragrance is added and mixed with nicotine and the first carrier; and / or In the preparation of the active ingredient particles, at least one of a binder, flavoring agent, pH adjuster, humectant, and fragrance is added and mixed with the active ingredient and the second carrier.

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