Oral nicotine composition and product thereof

Abstract

Embodiments of the present invention provide an oral nicotine composition and a product thereof, the oral nicotine composition comprising: a nicotine component, an active component that can be used to block nicotinic acetylcholine receptor and / or transient receptor potential ion channels, and lecithin, the lecithin is matched with the active component which can be used for blocking a nicotine acetylcholine receptor and / or transient receptor potential ion channel, so that nicotine stimulation, especially stomach stimulation, can be effectively relieved, and discomfort symptoms such as heartburn, hiccup and stomachache of a user are avoided.

Description

TECHNICAL FIELD

[0001] The present application belongs to the technical field of oral nicotine products, and particularly relates to an oral nicotine composition for reducing irritation and a product 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 absorb nicotine through the oral mucosa, do not need to be burned, and will not produce harmful substances such as tar and carbon monoxide, which can provide effective alternative therapy for relieving and quitting tobacco dependence.

[0003] Nicotine is the main active ingredient in tobacco, which 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 is particularly true when using nicotine products for the first time or using products with a higher nicotine concentration. In addition, the irritation of nicotine will also cause an increase in salivation, and part of the nicotine will inevitably flow through the throat and into the gastrointestinal tract with the saliva, causing heartburn, belching, vomiting, stomach pain, and other discomforts.

[0004] Some solutions have been proposed to address the discomfort caused by nicotine. For example, by inhibiting or blocking nicotinic acetylcholine receptors and / or transient receptor potential ion channels to reduce the perception of nicotine irritation, although it can reduce the irritation of nicotine to the oral cavity and throat to some extent, but the effect of reducing gastrointestinal irritation is limited. For example, by adding sweeteners, cooling agents, sour agents or their combinations to mask the irritation of nicotine, adding sweeteners such as lactose, sugar alcohols, etc. may cause intolerance symptoms in some users, and the irritation of cooling agents and sour agents may exacerbate the discomfort of users. Some technologies control the slow release of nicotine to avoid strong irritation caused by the massive release of nicotine in a short period of time. Although controlling the slow release of nicotine can alleviate irritation, it cannot meet the needs of users to quickly relieve nicotine cravings. SUMMARY

[0005] Based on the problems existing in the above-mentioned solutions to the discomfort caused by nicotine, the specific embodiments of the present application provide an oral nicotine composition that can effectively reduce nicotine irritation, especially gastrointestinal irritation, thereby avoiding the occurrence of heartburn, belching, stomach pain and other discomfort symptoms in users, and has no adverse side effects. The specific scheme is as follows:

[0006] An oral nicotine composition, comprising: a nicotine component, an active ingredient for blocking nicotinic acetylcholine receptors and / or transient receptor potential ion channels, and lecithin.

[0007] Optionally, the active ingredient that can be used to block the nicotinic acetylcholine receptor and / or transient receptor potential ion channel is at least one of gingerol, shogaol, zingerone, borneol, isoborneol, borneol acetate, monobornyl succinate, monoisobornyl succinate, glyceryl oxalate, or monobornyl formate.

[0008] Optionally, the lecithin is soy lecithin.

[0009] Optionally, the composition includes at least one of free nicotine, nicotine salt, or nicotine ion exchange resin.

[0010] Optionally, the active ingredient that can be used to block the nicotinic acetylcholine receptor and / or transient receptor potential ion channel is at a weight percentage of 0.5-10% in the composition.

[0011] Optionally, the lecithin is at a weight percentage of 0.5-10% in the composition.

[0012] Optionally, the weight ratio of the active ingredient that can be used to block the nicotinic acetylcholine receptor and / or transient receptor potential ion channel to the lecithin is 10:1-1:1.

[0013] Optionally, the nicotine ingredient is at a weight percentage of 1-25% in the composition.

[0014] Optionally, the composition further includes an anti-inflammatory and antioxidant active ingredient.

[0015] Optionally, the anti-inflammatory and antioxidant active ingredient is at least one of tea polysaccharide, tea polyphenol, theanine, ganoderma polysaccharide, green tea extract, ascorbic acid, taurine, quercetin, resveratrol, carotenoid, or anthocyanin.

[0016] Optionally, the composition further includes a pH adjuster.

[0017] Optionally, the pH adjuster is at least one of acetate, phosphate, citrate, carbonate, bicarbonate, borate, or tartrate.

[0018] An oral nicotine product formed from the above oral nicotine composition, the oral nicotine product being a pouch, a tablet, a chewing gum, or a mouth dissolving film.

[0019] The oral nicotine composition of the present embodiment can effectively reduce the stimulation of nicotine, especially the stimulation of the stomach, by the active ingredient that can be used to block the nicotinic acetylcholine receptor and / or the transient receptor potential ion channel, thereby avoiding the occurrence of symptoms such as heartburn, belching, stomach pain, and the like in the user. It is more friendly to the first-time user or the person with lower nicotine tolerance, and does not affect the oral release effect of nicotine, nor does it cause any additional stimulation or side effects. DETAILED DESCRIPTION

[0020] The oral nicotine composition of the present embodiment can effectively reduce the stimulation of nicotine, especially the stimulation of the stomach, by the active ingredient that can be used to block the nicotinic acetylcholine receptor and / or the transient receptor potential ion channel, thereby avoiding the occurrence of symptoms such as heartburn, belching, stomach pain, and the like in the user. It is more friendly to the first-time user or the person with lower nicotine tolerance, and does not affect the oral release effect of nicotine, nor does it cause any additional stimulation or side effects.

[0021] The inventors of the present application have found that the active ingredient that can be used to block the nicotinic acetylcholine receptor and / or the transient receptor potential ion channel, by the cooperation of lecithin, can effectively reduce the stimulation of nicotine, especially the stimulation of the stomach, thereby avoiding the occurrence of symptoms such as heartburn, belching, stomach pain, and the like in the user. The reason may be that lecithin is beneficial to form a protective barrier in the gastric mucosa, so that the active ingredient that can be used to block the nicotinic acetylcholine receptor and / or the transient receptor potential ion channel can better play a role, significantly enhancing the effect of reducing stimulation, especially in relieving the stimulation of the stomach.

[0022] The oral nicotine composition of the present embodiment can effectively reduce the stimulation of nicotine, especially the stimulation of the stomach, by the active ingredient that can be used to block the nicotinic acetylcholine receptor and / or the transient receptor potential ion channel, thereby avoiding the occurrence of symptoms such as heartburn, belching, stomach pain, and the like in the user. It is more friendly to the first-time user or the person with lower nicotine tolerance, and does not affect the oral release effect of nicotine, nor does it cause any additional stimulation or side effects.

[0023] The oral nicotine composition of the present embodiment can effectively reduce the stimulation of nicotine, especially the stimulation of the stomach, by the active ingredient that can be used to block the nicotinic acetylcholine receptor and / or the transient receptor potential ion channel, thereby avoiding the occurrence of symptoms such as heartburn, belching, stomach pain, and the like in the user. It is more friendly to the first-time user or the person with lower nicotine tolerance, and does not affect the oral release effect of nicotine, nor does it cause any additional stimulation or side effects.

[0024] The oral nicotine composition of the present embodiment can effectively reduce the stimulation of nicotine, especially the stimulation of the stomach, by the active ingredient that can be used to block the nicotinic acetylcholine receptor and / or the transient receptor potential ion channel, thereby avoiding the occurrence of symptoms such as heartburn, belching, stomach pain, and the like in the user. It is more friendly to the first-time user or the person with lower nicotine tolerance, and does not affect the oral release effect of nicotine, nor does it cause any additional stimulation or side effects.

[0025] The oral nicotine composition of the present embodiment, in some embodiments, the active ingredient that can be used to block nicotinic acetylcholine receptors and / or transient receptor potential ion channels in the composition is 0.5-10% by weight, and specifically for example can be 0.5%, 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, or 10%, etc.

[0026] The oral nicotine composition of the present embodiment, in some embodiments, the lecithin in the composition is 0.5-10% by weight, and specifically for example can be 0.5%, 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, or 10%, etc.

[0027] The oral nicotine composition of the present embodiment, in some embodiments, the weight ratio of the active ingredient that can be used to block nicotinic acetylcholine receptors and / or transient receptor potential ion channels and lecithin is 10:1-1:1, and in some embodiments, the weight ratio of the active ingredient that can be used to block nicotinic acetylcholine receptors and / or transient receptor potential ion channels and lecithin is 5:1-1:1, and specifically for example can be 5:1, 4:1, 3:1, 2:1, or 1:1, etc.

[0028] The oral nicotine composition of the present embodiment, in some embodiments, the nicotine component in the composition is 1-25% by weight, and specifically for example can be 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, 10%, 11%, 12%, 13%, 14%, 15%, 16%, 17%, 18%, 19%, 20%, 21%, 22%, 23%, 24%, or 25%, etc.

[0029] The oral nicotine composition of the present embodiment, in some embodiments, the composition further comprises an anti-inflammatory and antioxidant active ingredient, and in some embodiments, the anti-inflammatory and antioxidant active ingredient is at least one of tea polysaccharide, tea polyphenol, theanine, ganoderma polysaccharide, green tea extract, ascorbic acid, taurine, quercetin, resveratrol, carotenoid, or anthocyanin, and in some embodiments, the anti-inflammatory and antioxidant active ingredient in the composition is 0-5% by weight, and specifically for example can be 1%, 2%, 3%, 4%, or 5%, etc.

[0030] The oral nicotine composition of the present embodiment, in some embodiments, further comprises a pH adjuster, which is at least one of acetate, phosphate, citrate, carbonate, bicarbonate, borate, or tartrate, specifically, for example, sodium carbonate, sodium bicarbonate, calcium carbonate, sodium citrate, calcium bicarbonate, potassium bicarbonate, sodium citrate, or sodium tartrate, etc., in some embodiments, the weight percentage of the pH adjuster in the composition is 0-5%, specifically, for example, it can be 1%, 2%, 3%, 4%, or 5%, etc.

[0031] The oral nicotine composition of the present embodiment, in some embodiments, further comprises a filler, which is at least one of a polymer having a mucosal adsorption promoting effect alone or in combination, which can have the characteristics of swelling and expanding when in contact with water, in some embodiments, the filler is a cellulose derivative, such as 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; plant fibers, such as coconut shell fiber powder, bamboo fiber powder, peanut shell fiber, oat fiber powder, cocoa shell powder, tea fiber powder, coffee grounds powder, sugar cane fiber powder, apple fiber powder, citrus fiber powder, cassava fiber powder, flaxseed powder, pea fiber powder, wheat fiber powder, soybean fiber powder; starch derivatives, such as at least one of denatured starch, cross-linked starch, in some embodiments, the weight percentage of the filler in the composition is 30-80%, specifically, for example, it can be 30%, 35%, 40%, 45%, 50%, 55%, 65%, 70%, 75%, or 80%, etc.

[0032] The oral nicotine composition of the present embodiment, in some embodiments, further comprises a binder, which is at least one of maltodextrin, gum arabic, cellulose, carboxymethyl cellulose, starch, liquid glucose, gelatin, copovidone, hydroxypropyl cellulose, carrageenan, xanthan gum, or guar gum, in some embodiments, the weight percentage of the binder in the composition is 1-30%, specifically, for example, it can be 1%, 5%, 15%, 20%, 25%, or 30%, etc.

[0033] The oral nicotine composition of the embodiments of the present application, in some embodiments, further comprises a flavoring agent, in some embodiments, the flavoring agent is at least one of sucrose, aspartame, sucralose, acesulfame or stevioside, in some embodiments, the weight percentage of the flavoring agent in the composition is 0.5-15%, for example, it can be 0.5%, 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, 10%, 11%, 12%, 13%, 14% or 15% and the like.

[0034] The oral nicotine composition of the embodiments of the present application, in some embodiments, further comprises a flavoring agent, in some embodiments, the flavoring agent is at least one of sucrose, aspartame, sucralose, acesulfame or stevioside, in some embodiments, the weight percentage of the flavoring agent in the composition is 0.5-15%, for example, it can be 0.5%, 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, 10%, 11%, 12%, 13%, 14% or 15% and the like.

[0035] The oral nicotine composition of the embodiments of the present application, in some embodiments, further comprises a flavoring agent, in some embodiments, the flavoring agent is at least one of sucrose, aspartame, sucralose, acesulfame or stevioside, in some embodiments, the weight percentage of the flavoring agent in the composition is 0.5-15%, for example, it can be 0.5%, 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, 10%, 11%, 12%, 13%, 14% or 15% and the like.

[0036] The embodiments of the present application further provide an oral nicotine product formed by the above-mentioned oral nicotine composition, and the oral nicotine product is a pouch, a tablet, chewing gum or a mouth dissolving film.

[0037] The embodiments of the present application further provide a preparation method of the above-mentioned oral nicotine product, and the method comprises the following steps:

[0038] S1, mixing the nicotine component, the humectant and the binder in the above-mentioned oral nicotine composition with water to obtain a mixed solution;

[0039] S2, mixing the other components in the above-mentioned oral nicotine composition to obtain a dry mixed powder;

[0040] S3, stirring the dry mixed powder and the mixed solution under the action of a granulator until they are completely mixed and uniformly distributed, and then performing wet granulation;

[0041] S4 dry the obtained wet granules;

[0042] S5 prepare the oral nicotine product after screening the dried granules, for example, bagging, to obtain nicotine pouch products.

[0043] The present application is further illustrated by specific examples.

[0044] Example

[0045] Sensory evaluation:

[0046] After the preparation of the nicotine pouches in the examples, sensory score tests were performed. A test panel of 8 assessors evaluated the pouches. The test panel evaluated the pouches for 30 minutes for five parameters: burping, nausea, stomach burning, acid reflux, and overall acceptance.

[0047] Pouches of different formulations were tested.

[0048] Sensory evaluation criteria

[0049]

[0050] Note: Total score < 15, effect evaluation is poor; 15 < total score < 17, effect evaluation is general; 17 < total score < 20, effect evaluation is good; 20 < total score < 22, effect evaluation is better; total score > 22, effect evaluation is excellent.

[0051] Example 1

[0052] According to the composition and amount in Table 1, benzoic acid nicotine salt, water, glycerol, and maltodextrin were mixed uniformly to obtain a mixed solution, and other components were mixed uniformly to obtain a dry powder mixture. Then, the dry powder mixture and the mixed solution were thoroughly mixed, and the wet powder granules were obtained after drying treatment. After passing through a 20-mesh screen, the powder was bagged, with each bag containing 400 mg of powder. The bag material was non-woven fabric made of fiber. The sensory evaluation of the bagged nicotine pouches was performed, and the results are listed in Table 2 below.

[0053] Table 1 Composition of oral nicotine composition in Example 1

[0054]

[0055] Table 2 Sensory evaluation results of each nicotine pouch prepared in Example 1

[0056]

[0057] As shown in Table 2 above, combining soy lecithin with shogaol, an active ingredient that can block nicotine acetylcholine receptors and / or transient receptor potential ion channels, can effectively reduce nicotine irritation, especially stomach irritation, thus preventing users from experiencing discomfort such as heartburn, hiccups, and stomach pain. Compared with shogaol or soy lecithin alone, it has a significant effect, and it has a better effect than the combination of shogaol with green tea extract or sodium citrate.

[0058] Example 2

[0059] According to the composition and dosage in Table 3, nicotine benzoate, water, glycerin, and maltodextrin were mixed evenly to obtain a mixed solution. The other components were then mixed evenly to obtain a dry powder. The dry powder and the mixed solution were then completely mixed and wet-granulated to obtain wet powder granules, which were then dried. After passing through a 20-mesh sieve, the powder was packaged into bags, each containing 400 mg of powder. The bag material was non-woven fabric made of fiber. Sensory evaluation of the packaged nicotine bags was performed, and the results are listed in Table 4 below.

[0060] Table 3 Composition of the oral nicotine composition in Example 2

[0061]

[0062] Table 4 Sensory evaluation results of the nicotine bags prepared in Example 2

[0063]

[0064] As shown in Table 4 above, when the weight percentage of gingerol is 2-10 wt% and the weight percentage of soy lecithin is 1-5 wt%, it can effectively reduce nicotine irritation, especially stomach irritation, thereby avoiding discomfort symptoms such as heartburn, hiccups, and stomach pain. When the weight percentage of gingerol is 4-10 wt% and the weight percentage of soy lecithin is 1-2 wt%, especially when the weight percentage of gingerol is 6 wt% and the weight percentage of soy lecithin is 2 wt%, the effect is even better.

[0065] While the present invention has been disclosed above, it is not limited thereto. Any person skilled in the art can make various modifications and alterations without departing from the spirit and scope of the invention; therefore, the scope of protection of the present invention should be determined by the scope defined in the claims.

Claims

1. An oral nicotine composition, characterized in that, include: Nicotine, an active ingredient that can block nicotine acetylcholine receptors and / or transient receptor potential ion channels, and lecithin.

2. The nicotine composition according to claim 1, characterized in that, The active ingredient that can block nicotinic acetylcholine receptors and / or transient receptor potential ion channels is selected from at least one of gingerol, shogaol, gingerol, borneol, isoborneol, borneol acetate, monoborneol succinate, monoisoborneol succinate, glyceryl oxalate, or monoborneol formate.

3. The oral nicotine composition according to claim 1, characterized in that, The lecithin mentioned is soybean lecithin.

4. The oral nicotine composition according to claim 1, characterized in that, The composition includes at least one of free nicotine, nicotine salt, or nicotine ion exchange resin.

5. The oral nicotine composition according to claim 1, characterized in that, The active ingredient, which can block nicotinic acetylcholine receptors and / or transient receptor potential ion channels, is present in the composition at a weight percentage of 0.5–10%.

6. The oral nicotine composition according to claim 1, characterized in that, The lecithin in the composition is 0.5% to 10% by weight.

7. The oral nicotine composition according to claim 1, characterized in that, The weight ratio of the active ingredient that can be used to block nicotinic acetylcholine receptors and / or transient receptor potential ion channels to lecithin is 10:1 to 1:

1.

8. The oral nicotine composition according to claim 1, characterized in that, The nicotine component is present in the composition at a weight percentage of 1 to 25%.

9. The oral nicotine composition according to claim 1, characterized in that, The composition also includes anti-inflammatory and antioxidant active ingredients.

10. The oral nicotine composition according to claim 9, characterized in that, The anti-inflammatory and antioxidant active ingredients are at least one of tea polysaccharides, tea polyphenols, theanine, Ganoderma lucidum polysaccharides, green tea extract, ascorbic acid, taurine, quercetin, resveratrol, carotenoids, or anthocyanins.

11. The oral nicotine composition according to claim 1, characterized in that, The composition also includes a pH adjuster.

12. The oral nicotine composition according to claim 11, characterized in that, The pH adjuster is at least one of acetate, phosphate, citrate, carbonate, bicarbonate, borate, or tartrate.

13. An oral nicotine product, characterized in that, The oral nicotine product is formed from the oral nicotine composition according to any one of claims 1-12, and the oral nicotine product is a lozenge, tablet, chewing gum or oral dissolving film.

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