Nicotine substitution compound, water-soluble nicotine-free preparation, preparation method of water-soluble nicotine-free preparation and aerosol system

Abstract

The invention provides a nicotine replacement compound, a water-soluble nicotine-free preparation, a preparation method of the water-soluble nicotine-free preparation and an aerosol system. The nicotine replacement compound disclosed by the invention is prepared from the following components: 6-methyl nicotine, 5-ethynyl nicotine and ABT-418, so that not only can sensory experience similar to that of nicotine be provided for smoking quitters be provided, but also addiction and health risk caused by nicotine can be avoided. By simulating the physiological and psychological effects of nicotine, a smoker is helped to gradually reduce the dependence on nicotine. The invention also provides a water-soluble nicotine-free formulation, a preparation method thereof and an aerosol system.

Description

Technical Field

[0001] The present invention belongs to the technical field of aerosols, and in particular relates to a nicotine replacement compound, a water-soluble nicotine-free preparation, a preparation method thereof, and an aerosol system. Background Art

[0002] Cigarettes, as the most common tobacco products, are usually made of finely chopped tobacco leaves and packaged in paper rolls. The harm of traditional cigarettes has been widely confirmed. The harmful substances contained in them, such as nicotine, tar, and carbon monoxide, will directly enter the human body during the smoking process, posing a serious threat to health. According to the World Health Organization (WHO), smoking is an important cause of many chronic diseases (such as lung cancer, cardiovascular disease, respiratory diseases, etc.). Ingredients such as tar and carbon monoxide are produced during the smoking process, directly damaging the smoker's lungs and cardiovascular system, while nicotine is an addictive substance that makes it difficult for smokers to quit smoking. Electronic cigarettes are a tobacco substitute that does not require combustion. They produce aerosols for inhalation by heating tobacco oil or nicotine solution. Since there is no combustion involved, promoters of electronic cigarettes believe that they may be a substitute for reducing the harm of traditional smoking. However, electronic cigarettes are not without health risks. Although they avoid the tar and carbon monoxide produced during the combustion of traditional tobacco, during the heating process, solvents in the tobacco oil, such as glycerol and propylene glycol, will still undergo chemical reactions at high temperatures to produce harmful substances such as formaldehyde and acetaldehyde. Studies have shown that long-term use of e-cigarettes can still cause harm to the lungs and cardiovascular system, and some studies believe that e-cigarettes may have a certain inducing effect on adolescents and young people, causing them to become dependent on nicotine.

[0003] Heat-not-burn (HNB) products are nicotine substitutes that release nicotine by heating tobacco instead of burning it. It works by heating tobacco to a certain temperature, evaporating the nicotine in the tobacco and forming an aerosol for inhalation, thereby reducing harmful substances such as tar and carbon monoxide caused by traditional smoking. Compared with traditional cigarettes, heat-not-burn products can reduce the release of harmful substances to a certain extent, so they are considered a "relatively safe" choice. However, studies have shown that even without combustion, HNB products still release a certain amount of formaldehyde, acetaldehyde and other harmful chemicals, and the harm of these substances to health cannot be ignored. Whether it is traditional cigarettes, e-cigarettes, or heat-not-burn products, nicotine is their common ingredient. Nicotine is a highly addictive substance that stimulates the central nervous system and causes smokers to become dependent. Once addicted, quitting smoking becomes very difficult and is accompanied by a series of withdrawal symptoms. The addictiveness of nicotine and its negative impact on health, especially damage to the cardiovascular, lung and nervous systems, have become the biggest health risks of tobacco products at present. Therefore, how to reduce nicotine intake or even completely eliminate nicotine has become the key to reducing the harm of tobacco products.

[0004] At present, although various alternatives that reduce the release of harmful substances have appeared on the market, such as e-cigarettes and heat-not-burn products, they still cannot completely eliminate nicotine dependence and health risks. Therefore, it is necessary to develop a nicotine replacement compound. Summary of the invention

[0005] The present invention aims to solve at least one of the above-mentioned technical problems existing in the prior art. To this end, the present invention provides a nicotine replacement compound that can provide a sensory experience similar to nicotine for smokers who quit smoking, while avoiding the addictiveness and health risks brought by nicotine itself. It helps smokers gradually reduce their dependence on nicotine by simulating the physiological and psychological effects of nicotine.

[0006] The present invention also provides a water-soluble nicotine-free preparation.

[0007] The present invention also provides a method for preparing a water-soluble nicotine-free preparation.

[0008] The invention also provides an aerosol system.

[0009] A first aspect of the present invention provides a nicotine replacement compound, the components of which include 6-methyl nicotine, 5-ethynyl nicotine and ABT-418.

[0010] One of the technical solutions of the present invention regarding the nicotine replacement compound has at least the following beneficial effects:

[0011] Provide a sensory experience similar to nicotine. Nicotine, as one of the key ingredients in traditional tobacco products, can produce a "throat hit" and "pleasure" through its unique stimulation. These sensory experiences are usually one of the reasons why smokers continue to smoke. However, nicotine itself has strong addictiveness and potential harm to health, especially negative effects on the cardiovascular, nervous system and lungs. The nicotine replacement compound of the present invention, by containing 6-methyl nicotine, 5-ethynyl nicotine and ABT-418, can simulate a nicotine-like throat hit stimulation and pleasure in the absence of nicotine. This sensory substitution experience helps smokers reduce their dependence on traditional smoking during the process of quitting smoking and avoid discomfort or withdrawal symptoms caused by the lack of similar sensory stimulation. Among them, 6-methyl nicotine is a nicotine-like compound that is similar to nicotine in chemical structure and can act on nerve receptors to produce a certain sense of stimulation. 5-ethynyl nicotine can also effectively bind to nicotine receptors to produce effects similar to nicotine, but its toxicity and addictiveness are lower. ABT-418 is a nicotine receptor agonist that can mimic the effects of nicotine on neurotransmission in the brain, thereby producing similar pleasure and satisfaction. These ingredients combined together can effectively simulate the psychological and physiological satisfaction of smoking, helping users to relieve anxiety, irritability and other negative emotions caused by lack of nicotine during the process of quitting smoking, and reduce the possibility of relapse.

[0012] Avoid the negative effects of nicotine itself. As an addictive substance, nicotine is not only easy to cause dependence if used for a long time, but may also have adverse effects on the cardiovascular system, lungs and nervous system. Especially when smoking, nicotine enters the human body together with other harmful substances in the smoke (such as tar and carbon monoxide), causing long-term damage to health. A significant beneficial effect of nicotine replacement compound is that it does not contain nicotine, thus avoiding the negative effects of nicotine itself. The compound simulates the stimulation of nicotine through other compounds, but does not cause addiction or bring about nicotine-related health hazards. Specifically, the ingredients in the compound (such as 6-methyl nicotine, 5-ethynyl nicotine and ABT-418) do not have the toxicity and addictiveness of nicotine, so they will not cause nicotine dependence on users. These ingredients can effectively avoid cardiovascular stress, addictive reactions and overactivation of the nervous system caused by nicotine, and do not involve harmful smoke and chemicals produced during traditional smoking. This means that users can enjoy a nicotine-like experience without having to worry about the health risks associated with long-term use, especially the negative effects on cardiovascular health and the respiratory system.

[0013] Help smokers to reduce withdrawal symptoms. For many smokers, one of the biggest challenges in the process of quitting smoking is withdrawal symptoms, especially negative emotions such as anxiety, irritability and depression caused by lack of nicotine. These symptoms often make it difficult to quit smoking, causing many smokers to relapse during the process of quitting smoking. The purpose of the design of nicotine replacement complexes is to help users relieve withdrawal symptoms by mimicking the physiological stimulation of nicotine. Specifically, 6-methyl nicotine and 5-ethynyl nicotine can bind to nicotine receptors, activate the nervous system, produce a sense of pleasure and satisfaction similar to nicotine, and help smokers overcome the difficulties in the early stages of quitting smoking. ABT-418 can also effectively reduce withdrawal symptoms such as anxiety and irritability caused by lack of nicotine by stimulating nicotine receptors, and reduce the possibility of relapse. Therefore, the complex of the present invention can significantly improve the success rate of quitting smoking, especially for those who smoke for a long time and rely on nicotine. It provides smokers with a gentle transition method, allowing them to gradually reduce their dependence on nicotine and eventually quit smoking successfully.

[0014] Improve user experience and satisfaction. Smokers tend to develop a strong dependence on the sensory experience of smoking, such as the taste of smoke, throat stimulation, and satisfaction when inhaling. In order to effectively replace traditional tobacco products, the nicotine replacement compound of the present invention can reproduce the sensory experience of smoking through a carefully designed combination of ingredients without containing any harmful substances. 6-Methylnicotine and 5-ethynylnicotine can imitate the throat stimulation brought by nicotine, making smokers feel as satisfied as smoking during use. ABT-418, as a nicotine receptor agonist, can activate the reward system in the brain, thereby providing smokers with a sense of pleasure and reducing their craving for nicotine. The combined use of these ingredients can greatly improve the user experience of smoking cessation alternative products, allowing them to enjoy sensory stimulation similar to smoking while avoiding the negative effects of nicotine, thereby helping users to more easily transition to a nicotine-free lifestyle.

[0015] Nicotine replacement compounds are not only suitable for smokers who want to quit smoking, but also meet the needs of users who want to reduce nicotine intake or control nicotine dependence. For smokers who want to gradually reduce their nicotine intake, this compound can be used as a gradual transition solution to help them gradually get rid of nicotine dependence without producing obvious withdrawal symptoms.

[0016] Therefore, the nicotine replacement compound of the present invention has significant beneficial effects, which can not only provide a sensory experience similar to nicotine for smokers who quit smoking, but also avoid the addictiveness and health risks brought by nicotine itself. It helps smokers gradually reduce their dependence on nicotine by simulating the physiological and psychological effects of nicotine.

[0017] According to some embodiments of the present invention, the mass ratio of 6-methyl nicotine, 5-ethynyl nicotine and ABT-418 is 1:0.2-1.0:0.2-1.0.

[0018] According to some embodiments of the present invention, the mass ratio of 6-methyl nicotine, 5-ethynyl nicotine and ABT-418 is 1:0.4-0.6:0.4-0.6.

[0019] According to some embodiments of the present invention, the mass ratio of 6-methyl nicotine, 5-ethynyl nicotine and ABT-418 is 1:0.5:0.5.

[0020] The second aspect of the present invention provides a water-soluble nicotine-free preparation, the components of which include the nicotine replacement compound of the first aspect of the present invention, a sweetener, a cooling agent, a preservative, an emulsifier, an acidulant and a water-soluble fruit flavor.

[0021] One of the technical solutions of the present invention regarding the water-soluble nicotine-free preparation has at least the following beneficial effects:

[0022] The preparation does not contain nicotine, thus eliminating the addictiveness and health risks of nicotine. While users experience the sensory effects similar to nicotine, they will not suffer from the potential harm of nicotine to the cardiovascular system, nervous system and lungs, reducing the health risks associated with long-term smoking.

[0023] Furthermore, by combining nicotine replacement compounds (such as 6-methyl nicotine, 5-ethynyl nicotine and ABT-418), the preparation can effectively simulate the throat stimulation and pleasure of smoking. Ingredients such as 6-methyl nicotine and 5-ethynyl nicotine can activate nicotine receptors and produce physiological and psychological satisfaction similar to smoking, thereby helping smokers who quit or reduce nicotine intake to maintain sensory satisfaction, alleviate withdrawal symptoms, and reduce the risk of relapse.

[0024] Furthermore, ingredients such as sweeteners, cooling agents, and fruity flavors are added to the formulation to enhance the taste and flavor of the product and improve the user experience. For some smokers who quit smoking, the satisfaction of the taste (such as cooling, sweetness, and fruity flavor) can help them adapt to nicotine-free alternatives more easily and reduce discomfort and cravings during the process of quitting smoking.

[0025] Unlike the harmful substances produced by smoke in traditional cigarettes, this preparation reduces the burden on the body through a water-soluble form, avoiding the intake of toxic substances such as tar and carbon monoxide. Long-term use will not cause the risk of chronic diseases similar to traditional smoking, making it a safer alternative.

[0026] In addition, water-soluble preparations are easy to adjust dosage and usage, and users can choose the appropriate dosage according to their personal needs, thereby achieving more precise nicotine replacement control. It is especially suitable for users who want to gradually reduce nicotine dependence, so that they can reduce nicotine intake without experiencing withdrawal symptoms.

[0027] In addition to smokers who want to quit smoking, the preparation is also suitable for people who want to reduce their daily nicotine intake, reduce nicotine dependence or do not want to take nicotine. For these users, the preparation provides an alternative that can enjoy a similar sensory experience of smoking without health risks. The water-soluble nicotine-free preparation of the present invention can significantly improve the success rate of smokers who quit smoking. By effectively alleviating withdrawal symptoms (such as anxiety, irritability, etc.), providing a similar sense of pleasure as smoking, and increasing user satisfaction through taste and aroma, etc., it helps them stick to their smoking cessation plans more easily.

[0028] According to some embodiments of the present invention, the components include, by mass percentage:

[0029] The nicotine replacement compound: 0.01wt% to 1.0wt%,

[0030] Sweetener: 0.2wt%~5wt%,

[0031] Cooling agent: 0.1wt%~1wt%,

[0032] Preservative: 0.05wt%~0.5wt%,

[0033] Emulsifier: 0.05wt%~0.5wt%,

[0034] Acidulant: 0.5wt%~5wt%,

[0035] Water-soluble fruit flavor: 1wt%~20wt%,

[0036] The balance is water.

[0037] According to some embodiments of the present invention, the components include, by mass percentage:

[0038] The nicotine replacement compound: 0.08wt%,

[0039] Sweetener: 1wt%,

[0040] Cooling agent: 0.3wt%,

[0041] Preservative: 0.3wt%,

[0042] Emulsifier: 0.3wt%,

[0043] Acidulant: 3wt%,

[0044] Water-soluble fruit flavor: 15wt%,

[0045] The balance is water.

[0046] According to some embodiments of the present invention, based on 100 parts, the sweetener includes 10 parts of erythritol, 10 parts of sorbitol, 10 parts of mannitol, 5 parts of sucralose, 5 parts of cyclamate, 5 parts of acesulfame potassium, 5 parts of steviol glycosides, 1 part of neotame, 0.5 parts of advantame, 1 part of glycine, 1 part of citric acid, and 46.5 parts of water.

[0047] On the one hand, a mixed formula of sweeteners can simulate the sweetness of sugar while avoiding the unpleasant taste that may be caused by a single sweetener. For example, sucralose and cyclamate are often used to enhance sweetness without obvious aftertaste. By combining different sweeteners, a more natural and balanced sweetness experience can be obtained; on the other hand, different sweeteners may interact with each other to provide a more stable and lasting sweetness. Some sweeteners (such as sucralose) are more stable and suitable for use at high temperatures, while other sweeteners (such as stevioside) may be more natural, so their proportions can be adjusted according to different needs to achieve the best effect.

[0048] According to some embodiments of the present invention, based on 100 parts, the cooling agent includes 45 parts of WS-23, 5 parts of WS-3, 5 parts of menthol, and 50 parts of propylene glycol.

[0049] WS-23 and WS-3 are both chemically synthesized cooling agents that can produce a cooling sensation in the mouth, throat or skin. They combine with the body's cold receptors to simulate a cool sensation, giving people a comfortable and refreshing experience. WS-23 is relatively mild and long-lasting in terms of cooling intensity, making it suitable for long-term use.

[0050] Menthol is a natural cooling agent that comes from the mint plant and produces a noticeable cooling sensation. Menthol not only provides a refreshing cooling sensation, but also a unique aroma. Propylene glycol is often used as a solvent and stabilizer to dissolve and deliver other ingredients. It helps to evenly distribute the cooling agent ingredients and enhances the stability of other active ingredients. In addition, propylene glycol itself has a moisturizing effect, which can help maintain the texture and taste of the product, making it smoother when used.

[0051] According to some embodiments of the invention, the preservative comprises potassium sorbate.

[0052] According to some embodiments of the invention, the emulsifier comprises Tween 20.

[0053] According to some embodiments of the present invention, based on 100 parts, the acidulant includes: 10 parts of benzoic acid, 30 parts of lactic acid, 5 parts of levulinic acid, 5 parts of acetic acid, 1 part of butyric acid, 2 parts of 2-methylbutyric acid, 5 parts of citric acid, 2 parts of malic acid, 2 parts of tartaric acid and 38 parts of propylene glycol.

[0054] The advantage of compound acidulants is that they can provide a variety of sour levels, and each acidulant has its own unique sour characteristics and flavor. For example, citric acid and malic acid are often used to provide classic, refreshing sourness. Lactic acid provides a softer sour taste and is suitable for dairy products or fermented foods. Benzoic acid and acetic acid can add a sharper sour taste, especially when used in salty foods or sauces, which can bring certain preservative and seasoning effects. Levulinic acid, butyric acid and 2-methylbutyric acid have specific flavors and are often used to add more complex sourness and aroma, which may be suitable for foods with special tastes (such as some pickled foods or meat products).

[0055] Through the combination of these acidulants, the multi-layered and complex sour taste can be achieved without being monotonous, making the product taste richer and meeting the taste needs of different consumers.

[0056] According to some embodiments of the present invention, the water-soluble fruit flavor includes at least one of tobacco flavor, strawberry flavor, mango flavor, blueberry flavor, apple flavor and mint flavor.

[0057] The third aspect of the present invention provides a method for preparing the water-soluble nicotine-free preparation of the second aspect of the present invention, comprising uniformly mixing the nicotine replacement compound, a sweetener, a cooling agent, a preservative, an emulsifier, a sour agent and a water-soluble fruit flavor according to a proportion.

[0058] A technical solution in the method for preparing a water-soluble nicotine-free preparation of the present invention has at least the following beneficial effects:

[0059] The preparation method of the present invention can prepare a water-soluble nicotine-free preparation by simply mixing the components in a uniform ratio. The process does not require complex chemical reactions or high-temperature treatments, is simple to operate, and can reduce technical difficulties and costs in production. The production efficiency is high and can meet the needs of large-scale production. During preparation, the components are mixed in a scientific ratio to ensure the stability and consistency of each batch of preparations. This means that the effect and quality of the final product can be reliably controlled, ensuring that consumers have a consistent experience when using it.

[0060] The present invention can ensure uniform distribution of each component in the final preparation through precise proportioning and uniform mixing. In particular, the uniform distribution of active ingredients such as nicotine replacement compounds, sweeteners, cooling agents, etc. can ensure that the effect of the preparation is fully exerted, and avoid excessive or low concentrations of certain ingredients, thereby affecting the taste and physiological effects. Through strict mixing processes and proportions, the prepared water-soluble nicotine-free preparation can ensure stable quality in terms of taste, effect, etc., can meet user expectations and enhance market competitiveness. The preparation method of the present invention reduces the damage that may be caused to active ingredients (such as 6-methyl nicotine, 5-ethynyl nicotine, ABT-418, etc.) by a gentle mixing process, can retain the activity of these ingredients to the greatest extent, and ensure that they can play their due physiological and psychological effects when used.

[0061] The preparation method can prepare water-soluble nicotine-free preparations simply and efficiently by mixing nicotine replacement compounds, sweeteners, cooling agents, preservatives, emulsifiers, acidulants and water-soluble fruit flavors in a scientific ratio, ensuring the consistency, stability and taste of the product and ensuring that the activity of each component is not damaged. At the same time, the method has good large-scale production potential, high cost-effectiveness, and can enhance consumer experience and acceptance.

[0062] The fourth aspect of the present invention provides an aerosol system, comprising an atomizer and the nicotine replacement compound of the first aspect of the present invention or the water-soluble nicotine-free preparation of the second aspect of the present invention.

[0063] One of the technical solutions of the present invention regarding the aerosol system has at least the following beneficial effects:

[0064] The aerosol system can convert nicotine replacement compounds or nicotine-free preparations into tiny aerosol particles through a nebulizer. These tiny particles can be effectively inhaled by the respiratory system and quickly reach the lungs, thereby improving the absorption efficiency of active ingredients (such as 6-methyl nicotine, 5-ethynyl nicotine, etc.). Compared with traditional oral or sublingual administration, the aerosol system can achieve an increase in bioavailability in a shorter time, meeting the user's demand for quick satisfaction.

[0065] By breathing in the aerosol, users can quickly experience a nicotine-like throat sensation and pleasant feeling, providing immediate physiological and psychological satisfaction. This is especially important for smokers who quit smoking or reduce their nicotine intake, as it helps them avoid anxiety or discomfort caused by the lack of nicotine stimulation during the smoking cessation process.

[0066] The water-soluble nicotine-free preparations used in aerosol systems eliminate the negative effects of nicotine, including addiction, cardiovascular disease, nervous system activation and other health risks. Compared with the harmful smoke in traditional cigarettes, aerosol systems do not produce harmful substances such as tar, carbon monoxide, etc., which significantly reduces the harm to health. This makes the aerosol system a safe alternative that helps smokers reduce the intake of harmful substances. The aerosol system can provide throat stimulation and pleasure similar to smoking through atomization technology. Whether using nicotine replacement compounds or water-soluble nicotine-free preparations, the active ingredients in the aerosol can produce physiological and psychological satisfaction similar to smoking by activating nicotine receptors. This sensory substitution effect helps smokers relieve withdrawal symptoms such as anxiety and irritability during the process of quitting smoking and reduce the possibility of relapse.

[0067] The aerosol system can produce smoke-like aerosols through an atomizer. After inhalation, users will have a sensory experience similar to smoking, helping smokers maintain satisfaction with traditional smoking methods in the process of quitting or reducing smoking, thereby reducing dependence on tobacco products. The aerosol system can also accurately control the amount of active ingredients (such as 6-methyl nicotine, 5-ethynyl nicotine, etc.) inhaled each time by adjusting the settings of the atomizer. This precise control allows users to adjust the intake according to personal needs and gradually reduce their dependence on nicotine. It is especially suitable for smokers who want to gradually reduce their nicotine intake. Compared with traditional smoking, the aerosol system can provide a more stable nicotine replacement experience, reduce the discomfort caused by fluctuations in nicotine intake during smoking, and avoid anxiety caused by excessive or insufficient intake.

[0068] The aerosol system of the present invention, combined with nicotine replacement compounds or water-soluble nicotine-free preparations, provides an efficient, safe and convenient alternative to smoking. It can effectively improve the absorption and bioavailability of active ingredients through atomization technology, provide a sensory experience similar to smoking, and eliminate the harmful substances and health risks of traditional smoking. For smokers who quit smoking or users who reduce nicotine intake, the aerosol system can effectively alleviate withdrawal symptoms, reduce the risk of relapse, and help users transition to a nicotine-free lifestyle more smoothly.

[0069] The aerosol system of the present invention may include an atomizer, which can generate an aerosol from a water-soluble liquid nicotine-free preparation. The atomizer may be an ultrasonic non-heating atomizer. The system controls the ultrasonic atomization core to vibrate by electronic components, thereby generating an inhalable aerosol from the water-soluble nicotine-free preparation. The system may include a container for holding the water-soluble liquid nicotine-free preparation, and the container is connected to the ultrasonic atomization device system. The container can be repeatedly injected with the water-soluble nicotine-free liquid preparation. DETAILED DESCRIPTION

[0070] The following are specific embodiments of the present invention, and the technical solutions of the present invention are further described in conjunction with the embodiments, but the present invention is not limited to these embodiments.

[0071] The following will be combined with the embodiments to clearly and completely describe the concept of the present invention and the technical effects produced, so as to fully understand the purpose, characteristics and effects of the present invention. Obviously, the described embodiments are only part of the embodiments of the present invention, not all of them. Based on the embodiments of the present invention, other embodiments obtained by those skilled in the art without creative work are all within the scope of protection of the present invention.

[0072] In the description of the present invention, the description with reference to the terms "one embodiment", "some embodiments", "illustrative embodiments", "examples", "specific examples", or "some examples" means that the specific features, structures, materials or characteristics described in conjunction with the embodiment or example are included in at least one embodiment or example of the present invention. In this specification, the schematic representation of the above terms does not necessarily refer to the same embodiment or example. Moreover, the specific features, structures, materials or characteristics described may be combined in any one or more embodiments or examples in a suitable manner.

[0073] Unless otherwise specified, "room temperature" in the present invention means 25°C±5°C.

[0074] Unless otherwise specified, "about" in the present invention means that the allowable error is within ±2%.

[0075] If the specific conditions are not specified in the examples, the experiments were carried out under conventional conditions or conditions recommended by the manufacturer. If the manufacturers of the reagents or instruments are not specified, they are all conventional products that can be purchased commercially.

[0076] 6-Methylnicotine was purchased from Zhejiang Zhanshen Biotechnology Co., Ltd.

[0077] 5-Ethynyl nicotine was purchased from Shanghai Aladdin Biochemical Technology Co., Ltd.

[0078] ABT-418 was purchased from Wuhan Aimijie Technology Co., Ltd.

[0079] Tobacco flavor was purchased from Shenzhen Boton Flavor Co., Ltd.

[0080] Example 1

[0081] First, a nicotine replacement compound was prepared, the components of which were 6-methyl nicotine, 5-ethynyl nicotine and ABT-418, and the mass ratio of 6-methyl nicotine, 5-ethynyl nicotine and ABT-418 was 1:0.5:0.5. The preparation method was as follows: 6-methyl nicotine, 5-ethynyl nicotine and ABT-418 were mixed in proportion.

[0082] Then a water-soluble nicotine-free preparation was prepared, the components of which were:

[0083] Nicotine replacement compound: 0.5wt%,

[0084] Tobacco flavor: 15wt%,

[0085] Sweetener: 0.5wt%,

[0086] Acidulant: 0.5wt%,

[0087] Cooling agent: 0.3wt%,

[0088] Preservative Potassium Sorbate: 0.3wt%,

[0089] Emulsifier Tween 20: 0.3wt%,

[0090] The balance is water.

[0091] Among them, based on 100 parts, the formula of sweeteners is: 10 parts of erythritol, 10 parts of sorbitol, 10 parts of mannitol, 5 parts of sucralose, 5 parts of cyclamate, 5 parts of acesulfame potassium, 5 parts of steviol glycosides, 1 part of neotame, 0.5 parts of Advantame, 1 part of glycine, 1 part of citric acid, and 46.5 parts of water.

[0092] Based on 100 parts, the formula of the cooling agent is: 45 parts of WS-23, 5 parts of WS-3, 5 parts of menthol, and 50 parts of propylene glycol.

[0093] Based on 100 parts, the formula of the acidulant is: 10 parts of benzoic acid, 30 parts of lactic acid, 5 parts of levulinic acid, 5 parts of acetic acid, 1 part of butyric acid, 2 parts of 2-methylbutyric acid, 5 parts of citric acid, 2 parts of malic acid, 2 parts of tartaric acid and 38 parts of propylene glycol.

[0094] The preparation method is as follows: the components of the water-soluble nicotine-free preparation are mixed uniformly according to a proportion.

[0095] Example 2

[0096] First, a nicotine replacement compound was prepared, the components of which were 6-methyl nicotine, 5-ethynyl nicotine and ABT-418, and the mass ratio of 6-methyl nicotine, 5-ethynyl nicotine and ABT-418 was 1:0.5:0.5. The preparation method was as follows: 6-methyl nicotine, 5-ethynyl nicotine and ABT-418 were mixed in proportion.

[0097] Then a water-soluble nicotine-free preparation was prepared, the components of which were:

[0098] Nicotine replacement compound: 0.4wt%,

[0099] Tobacco flavor: 10wt%,

[0100] Sweetener: 0.7wt%,

[0101] Acidulant: 0.5wt%,

[0102] Cooling agent: 0.3wt%,

[0103] Preservative Potassium Sorbate: 0.4wt%,

[0104] Emulsifier Tween 20: 0.3wt%,

[0105] The balance is water.

[0106] The preparation method is as follows: the components of the water-soluble nicotine-free preparation are mixed uniformly according to a proportion.

[0107] Example 3

[0108] First, a nicotine replacement compound was prepared, the components of which were 6-methyl nicotine, 5-ethynyl nicotine and ABT-418, and the mass ratio of 6-methyl nicotine, 5-ethynyl nicotine and ABT-418 was 1:0.5:0.5. The preparation method was as follows: 6-methyl nicotine, 5-ethynyl nicotine and ABT-418 were mixed in proportion.

[0109] Then a water-soluble nicotine-free preparation was prepared, the components of which were:

[0110] Nicotine replacement compound: 0.3wt%,

[0111] Tobacco flavor: 16wt%,

[0112] Sweetener: 0.5wt%,

[0113] Acidulant: 0.5wt%,

[0114] Cooling agent: 0.3wt%,

[0115] Preservative Potassium Sorbate: 0.4wt%,

[0116] Emulsifier Tween 20: 0.3wt%,

[0117] The balance is water.

[0118] The preparation method is as follows: the components of the water-soluble nicotine-free preparation are mixed uniformly according to a proportion.

[0119] Example 4

[0120] First, a nicotine replacement compound was prepared, the components of which were 6-methyl nicotine, 5-ethynyl nicotine and ABT-418, and the mass ratio of 6-methyl nicotine, 5-ethynyl nicotine and ABT-418 was 1:0.5:0.5. The preparation method was as follows: 6-methyl nicotine, 5-ethynyl nicotine and ABT-418 were mixed in proportion.

[0121] Then a water-soluble nicotine-free preparation was prepared, the components of which were:

[0122] Nicotine replacement compound: 0.2wt%,

[0123] Tobacco flavor: 15wt%,

[0124] Sweetener: 0.5wt%,

[0125] Acidulant: 0.5wt%,

[0126] Cooling agent: 0.3wt%,

[0127] Preservative Potassium Sorbate: 0.4wt%,

[0128] Emulsifier Tween 20: 0.3wt%,

[0129] The balance is water.

[0130] The preparation method is as follows: the components of the water-soluble nicotine-free preparation are mixed uniformly according to a proportion.

[0131] Example 5

[0132] First, a nicotine replacement compound was prepared, the components of which were 6-methyl nicotine, 5-ethynyl nicotine and ABT-418, and the mass ratio of 6-methyl nicotine, 5-ethynyl nicotine and ABT-418 was 1:0.5:0.5. The preparation method was as follows: 6-methyl nicotine, 5-ethynyl nicotine and ABT-418 were mixed in proportion.

[0133] Then a water-soluble nicotine-free preparation was prepared, the components of which were:

[0134] Nicotine replacement compound: 0.5wt%,

[0135] Tobacco flavor: 18wt%,

[0136] Sweetener: 0.5wt%,

[0137] Acidulant: 0.5wt%,

[0138] Cooling agent: 0.3wt%,

[0139] Preservative Potassium Sorbate: 0.4wt%,

[0140] Emulsifier Tween 20: 0.3wt%,

[0141] The balance is water.

[0142] The preparation method is as follows: the components of the water-soluble nicotine-free preparation are mixed uniformly according to a proportion.

[0143] Comparative Example A

[0144] First, a nicotine replacement compound was prepared, the components of which were 6-methyl nicotine, 5-ethynyl nicotine and ABT-418, and the mass ratio of 6-methyl nicotine, 5-ethynyl nicotine and ABT-418 was 1:0.5:0.5. The preparation method was as follows: 6-methyl nicotine, 5-ethynyl nicotine and ABT-418 were mixed in proportion.

[0145] Then a water-soluble nicotine-free preparation was prepared, the components of which were:

[0146] Nicotine replacement compound: 0.5wt%,

[0147] Tobacco flavor: 40wt%,

[0148] Sweetener: 0.5wt%,

[0149] Acidulant: 0.5wt%,

[0150] Cooling agent: 0.3wt%,

[0151] Preservative Potassium Sorbate: 0.4wt%,

[0152] Emulsifier Tween 20: 0.3wt%,

[0153] The balance is water.

[0154] Comparative Example B

[0155] First, a nicotine replacement compound was prepared, the components of which were 6-methyl nicotine, 5-ethynyl nicotine and ABT-418, and the mass ratio of 6-methyl nicotine, 5-ethynyl nicotine and ABT-418 was 1:0.5:0.5. The preparation method was as follows: 6-methyl nicotine, 5-ethynyl nicotine and ABT-418 were mixed in proportion.

[0156] Then a water-soluble nicotine-free preparation was prepared, the components of which were:

[0157] Nicotine replacement compound: 0.5wt%,

[0158] Tobacco flavor: 40wt%,

[0159] Sweetener: 0.5wt%,

[0160] Acidulant: 0.5wt%,

[0161] Cooling agent: 0.3wt%,

[0162] Emulsifier Tween 20: 0.3wt%,

[0163] The balance is water.

[0164] The preparation method is as follows: the components of the water-soluble nicotine-free preparation are mixed uniformly according to a proportion.

[0165] Comparative Example C

[0166] First, a nicotine replacement compound was prepared, the components of which were 6-methyl nicotine, 5-ethynyl nicotine and ABT-418, and the mass ratio of 6-methyl nicotine, 5-ethynyl nicotine and ABT-418 was 1:0.5:0.5. The preparation method was as follows: 6-methyl nicotine, 5-ethynyl nicotine and ABT-418 were mixed in proportion.

[0167] Then a water-soluble nicotine-free preparation was prepared, the components of which were:

[0168] Nicotine replacement compound: 0.5wt%,

[0169] Tobacco flavor: 40wt%,

[0170] Sweetener: 0.5wt%,

[0171] Acidulant: 0.5wt%,

[0172] Cooling agent: 0.3wt%,

[0173] Preservative Potassium Sorbate: 0.4wt%,

[0174] The balance is water.

[0175] The detailed proportions of the embodiments and the comparative examples are shown in Table 1.

[0176] Table 1

[0177] Example Comparison A Control B Control C Example 1 Example 2 Example 3 Example 4 Example 5 Nicotine replacement compound 0.5 0.5 0.5 0.5 0.4 0.3 0.2 0.5 Tobacco flavor 40 40 40 15 10 16 15 18 Sweetener Combinations 0.5 0.5 0.5 0.5 0.7 0.5 0.5 0.5 Acidulant combination 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 Cooling agent combination 0.3 0.3 0.3 0.3 0.3 0.3 0.3 0.3 Potassium Sorbate 0.4 0 0.4 0.4 0.4 0.4 0.4 0.4 Twain 20 0.3 0.3 0 0.3 0.3 0.3 0.3 0.3 water 57.5 57.9 57.8 82.5 87.4 81.7 82.8 79.5

[0178] The atomizer of CN306986214S was used to atomize the aerosols of the examples and the control examples. The atomization effects are shown in Table 2.

[0179] Table 2

[0180]

[0181]

[0182] Control A, Control B and Control C have relatively turbid solutions due to excessive use of flavors, and the propylene glycol content in the system is too high, resulting in poor aerosol generation effects, which easily block the atomizer spray hole and cannot be atomized continuously.

[0183] After the example was placed at natural room temperature for 30 days, microbial detection was performed, and the microbial indicators were well controlled. The results are shown in Table 3.

[0184] Table 3

[0185]

[0186] Sensory quality evaluation

[0187] There are 6 evaluation items, including aroma quality, aroma quantity, harmony, irritation, miscellaneous smell, and aftertaste. The maximum scale of each evaluation item is 9 points, and each evaluation item is scored in 1 point. The specific evaluation criteria are shown in Table 4.

[0188] Table 4

[0189]

[0190]

[0191] Evaluation method: Provide samples and sensory quality evaluation standard forms to 15 professional absorption technicians, and evaluate various indicators according to the requirements of the form.

[0192] Result statistics: The evaluation results of all 15 inhalation evaluation technical experts are valid. The arithmetic mean of the individual evaluation results of each inhalation evaluation expert is calculated, and the result is retained to one decimal place. The arithmetic mean of each individual item is added up to obtain the total score. The results are shown in Table 5.

[0193] Table 5

[0194] Example Fragrance Aroma volume Harmony Irritant Miscellaneous gas Throat hit Total score Comparison sample A 5.2 5.1 5.2 5.8 5.1 6.2 32.6 Example 1 7.1 7.3 7.5 7.5 8.2 7.2 44.8 Example 2 7.2 7.1 7.3 7.3 8.4 7.3 44.6 Example 3 7.4 7.9 7.2 7.4 8.5 7.5 45.9 Example 4 7.1 7.4 7.4 7.6 8.1 7.4 45.0 Example 5 7.2 8.0 7.6 7.5 8.3 7.2 45.8

[0195] From the examples, the water-soluble nicotine-free preparation of the present invention, after being atomized by the aerosol atomization system, obtains a better sensory experience. 6-Methylnicotine, 5-ethynylnicotine and ABT-418 are all nicotine analogs that can bind to human nicotine receptors to exert their effects.

[0196] In addition, the water-soluble nicotine-free preparation of the present invention can also provide the physiological satisfaction and throat hit of nicotine. According to the sensory test results, the use of the nicotine composite substitute obtains a better throat hit and satisfaction experience.

[0197] The water-soluble nicotine-free liquid preparation of the present invention creatively uses a combination of 6-methyl nicotine, 5-ethynyl nicotine and ABT-418 to obtain a physiological satisfaction and throat hit similar to or richer than nicotine, thus filling the technical gap of nicotine-free products in the current market.

[0198] It should be noted that the water-soluble nicotine-free liquid preparation of the present invention uses a cold atomization aerosol system that does not burn or heat. While obtaining a better sensory smoking experience, the chemical components do not undergo thermal decomposition and do not produce unexpected chemical components. The safety is greatly improved compared to conventional heated electronic cigarettes and HNBs, and it has a higher application value.

[0199] The present invention has been described in detail above in conjunction with the embodiments, but the present invention is not limited to the above embodiments, and various changes can be made within the knowledge scope of ordinary technicians in the relevant technical field without departing from the purpose of the present invention.

Claims

1. A nicotine replacement compound, characterized in that The ingredients include 6-methyl nicotine, 5-ethynyl nicotine and ABT-418.

2. The nicotine replacement compound according to claim 1, characterized in that The mass ratio of the 6-methyl nicotine, 5-ethynyl nicotine and ABT-418 is 1:0.2-1.0:0.2-1.

0.

3. The nicotine replacement compound according to claim 2, characterized in that The mass ratio of the 6-methyl nicotine, 5-ethynyl nicotine and ABT-418 is 1:0.4-0.6:0.4-0.

6.

4. A water-soluble nicotine-free preparation, characterized in that: The components include the nicotine replacement compound according to any one of claims 1 to 3, a sweetener, a cooling agent, a preservative, an emulsifier, a sour agent and a water-soluble fruit flavor.

5. The water-soluble nicotine-free preparation according to claim 4, characterized in that: In terms of mass percentage, the components include: The nicotine replacement compound: 0.01wt% to 1.0wt%, Sweetener: 0.2wt%~5wt%, Cooling agent: 0.1wt%~1wt%, Preservative: 0.05wt%~0.5wt%, Emulsifier: 0.05wt%~0.5wt%, Acidulant: 0.5wt%~5wt%, Water-soluble fruit flavor: 1wt%~20wt%, The balance is water.

6. The water-soluble nicotine-free preparation according to claim 4 or 5, characterized in that: Based on 100 parts, the sweetener includes 10 parts of erythritol, 10 parts of sorbitol, 10 parts of mannitol, 5 parts of sucralose, 5 parts of cyclamate, 5 parts of acesulfame potassium, 5 parts of steviol glycosides, 1 part of neotame, 0.5 parts of advantame, 1 part of glycine, 1 part of citric acid, and 46.5 parts of water.

7. The water-soluble nicotine-free preparation according to claim 4 or 5, characterized in that: Based on 100 parts, the cooling agent includes 45 parts of WS-23, 5 parts of WS-3, 5 parts of menthol, and 50 parts of propylene glycol.

8. The water-soluble nicotine-free preparation according to claim 4 or 5, characterized in that: Based on 100 parts, the acidulant includes: 10 parts of benzoic acid, 30 parts of lactic acid, 5 parts of levulinic acid, 5 parts of acetic acid, 1 part of butyric acid, 2 parts of 2-methylbutyric acid, 5 parts of citric acid, 2 parts of malic acid, 2 parts of tartaric acid and 38 parts of propylene glycol.

9. A method for preparing the water-soluble nicotine-free formulation according to any one of claims 4 to 8, characterized in that: The method comprises uniformly mixing the nicotine replacement compound, a sweetener, a cooling agent, a preservative, an emulsifier, a sour agent and a water-soluble fruit flavor according to a proportion.

10. An aerosol system, characterized in that: The invention comprises an atomizer and the nicotine replacement compound according to any one of claims 1 to 3 or the water-soluble nicotine-free preparation according to any one of claims 4 to 8.

Images