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WO2025108387A1 - Liquide d'atomisation, procédé de préparation de liquide d'atomisation et dispositif d'atomisation électronique - Google Patents

Liquide d'atomisation, procédé de préparation de liquide d'atomisation et dispositif d'atomisation électronique Download PDF

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Publication number
WO2025108387A1
WO2025108387A1 PCT/CN2024/133590 CN2024133590W WO2025108387A1 WO 2025108387 A1 WO2025108387 A1 WO 2025108387A1 CN 2024133590 W CN2024133590 W CN 2024133590W WO 2025108387 A1 WO2025108387 A1 WO 2025108387A1
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WO
WIPO (PCT)
Prior art keywords
acid
atomized liquid
cytisine
nicotine
liquid according
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
PCT/CN2024/133590
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English (en)
Chinese (zh)
Inventor
邓晶晶
卢禁
楚明
刘章
赵婧
徐中立
李永海
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Shenzhen FirstUnion Technology Co Ltd
Original Assignee
Shenzhen FirstUnion Technology Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Shenzhen FirstUnion Technology Co Ltd filed Critical Shenzhen FirstUnion Technology Co Ltd
Publication of WO2025108387A1 publication Critical patent/WO2025108387A1/fr
Pending legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • A—HUMAN NECESSITIES
    • A24—TOBACCO; CIGARS; CIGARETTES; SIMULATED SMOKING DEVICES; SMOKERS' REQUISITES
    • A24B—MANUFACTURE OR PREPARATION OF TOBACCO FOR SMOKING OR CHEWING; TOBACCO; SNUFF
    • A24B15/00—Chemical features or treatment of tobacco; Tobacco substitutes, e.g. in liquid form
    • A24B15/10—Chemical features of tobacco products or tobacco substitutes
    • A24B15/16—Chemical features of tobacco products or tobacco substitutes of tobacco substitutes
    • A24B15/167—Chemical features of tobacco products or tobacco substitutes of tobacco substitutes in liquid or vaporisable form, e.g. liquid compositions for electronic cigarettes

Definitions

  • the embodiments of the present application relate to the field of aerosol liquid, and in particular to an aerosol liquid containing nicotine and cytisine.
  • e-cigarettes contain the physiologically active substance nicotine in their aerosol liquid. Users inhale nicotine by smoking e-cigarettes, thereby creating a physiological satisfaction similar to that of smoking traditional cigarettes.
  • an embodiment of the present application provides an atomizing liquid, and the atomizing liquid includes: nicotine, cytisine and a solvent.
  • the mass fraction of nicotine in the atomized liquid is 0.50%-3.00%.
  • the mass fraction of cytisine is 0.50%-5.00%.
  • the mass fraction of the solvent is 50.00%-99.90%.
  • the mass fraction of nicotine is 1.00%-2.00%.
  • the mass fraction of cytisine is 1.00%-4.00%.
  • cytisine includes the free base of cytisine.
  • cytisine includes cytisine salt.
  • the cytisine salt is generated by the reaction of cytisine with an organic acid
  • the organic acid is selected from one or a combination of formic acid, acetic acid, propionic acid, butyric acid, ⁇ -furanic acid, ⁇ -furanylbutyric acid, isovaleric acid, ⁇ -methylvaleric acid, levulinic acid, lactic acid, citric acid, malic acid, tartaric acid, succinic acid, oxalic acid, maleic acid, glycolic acid, lauric acid, myristic acid, palmitic acid, stearic acid, oleic acid, linoleic acid, linolenic acid, benzoic acid, phenylacetic acid, caffeic acid, coumaric acid, phthalic acid and terephthalic acid.
  • the atomized liquid provided in one embodiment of the present application further includes a sweetener, and the mass fraction of the sweetener is 0.01%-0.60%.
  • the sweetener includes one or a combination of neotame, cyclamate, sucralose, aspartame, steviol glycosides, acesulfame potassium and mogroside.
  • the atomized liquid provided in one embodiment of the present application further includes a cooling agent, and the mass fraction of the cooling agent is 0.10%-8.00%.
  • the cooling agent includes one or a combination of menthol, menthone, isomenthone, 2-isopropyl-N,2,3-trimethylbutyramide, N-ethyl-p-menthyl-3-carboxamide and N-(ethoxycarbonylmethyl)-p-alkane-3-carboxamide.
  • the atomized liquid provided in one embodiment of the present application further includes a flavor composition, and the mass fraction of the flavor composition is 1.00%-20.00%.
  • the solvent includes one or a mixture of several of propylene glycol, butylene glycol, 1,2,4-butanetriol, dipropylene glycol, diethylene glycol, triethylene glycol, polyethylene glycol 200, polyethylene glycol 400, triacetin, glycerol, dipropylene glycol ether, ethanol, water, triethyl citrate and caprylic acid glyceride.
  • An embodiment of the present application also provides a method for preparing an atomized liquid, comprising:
  • the second mixture was filtered to obtain a nebulized liquid.
  • a sweetener and a cooling agent are also added to the solution.
  • a flavor composition is also added to the first mixture.
  • An embodiment of the present application further provides an electronic atomization device, comprising the atomizing liquid provided in the above embodiment and an atomizer, wherein the atomizer is used to heat and atomize the atomizing liquid to generate an aerosol.
  • the present application provides an atomizing liquid, a preparation method of the atomizing liquid, and an electronic atomizing device, using cytisine which has a synergistic effect with nicotine to provide an atomizing liquid with better satisfaction and better effect of relieving smoking addiction without increasing the amount of nicotine.
  • FIG1 is a comparison chart of addiction relief scores of Examples 1-3 and Comparative Example 1 of the present application.
  • FIG2 is a comparison chart of addiction relief scores of Examples 4-6 and Comparative Example 2 of the present application.
  • FIG3 is a comparison chart of addiction relief scores of Example 7 and Comparative Example 3 of the present application.
  • FIG4 is a comparison chart of addiction relief scores of Example 8 and Comparative Example 4 of the present application.
  • FIG5 is a comparison chart of addiction relief scores of Examples 9-11 of the present application and Comparative Example 5.
  • An embodiment of the present application provides an atomized liquid, which includes nicotine, cytisine, and a solvent.
  • Cytisine which has a synergistic effect with nicotine, is used to provide an atomized liquid with a better sense of satisfaction and a better effect of relieving smoking addiction without increasing the amount of nicotine.
  • the mass fraction of nicotine in the atomized liquid is 0.50%-3.00%.
  • the mass fraction of cytisine is 0.50%-5.00%.
  • the mass fraction of the solvent is 50.00%-99.90%.
  • Nicotine is an important component of e-cigarette liquid. Nicotine can exist in free base form or salt form. Early e-cigarettes generally used nicotine free base. The volatile nicotine free base is more irritating and has a strong throat hit. It is mainly absorbed through the mouth and throat and is difficult to enter the lungs, resulting in a small amount entering the lungs, so the experience is poor. The use of nicotine salts has allowed e-cigarettes to develop further. Since nicotine salts are less volatile and cause less throat irritation, the smoke becomes smoother after using nicotine salts, and more aerosols enter the lungs to participate in lung absorption, thereby improving the experience of e-cigarettes.
  • cytisine The molecular formula of cytisine is C 11 H 14 N 2O . Its Chinese aliases are wild indigo alkaloids and urocanthine. It is a natural bioactive compound. It was first isolated from the golden chain flower of the genus Cytisus by Husemann and Marme in 1865. It mainly exists in plants of the genus Sophora, genus Cassia or Berberidaceae of the Leguminosae family, such as cytisine, Sophora flavescens, and Sophora alopecuroides. It has a high affinity for neuronal nicotinic acetylcholine receptors and is specific to the ⁇ -subtype.
  • cytisine It is a partial agonist of nicotinic acetylcholine receptors.
  • Modern studies have shown that cytisine has a variety of pharmacological effects, such as smoking cessation, enhancing myocardial contractility, stimulating breathing, anti-depression, dopamine neurotransmission, enhancing motor ability, improving cognitive function, analgesia, and anti-tumor.
  • cytisine was isolated only more than a hundred years ago, its history of use in medicine can be traced back thousands of years ago. Indians used cytisine seeds to induce vomiting and laxative effects.
  • traditional medicine uses alcohol extracts containing cytisine to treat constipation, migraine, insomnia, cough and neuralgia.
  • cytisine was developed into a smoking cessation drug and widely sold in Central and Eastern Europe. Clinical studies have proven that the drug has good efficacy and safety. During World War II, when tobacco was in short supply, broom leaves were used by Russian soldiers to smoke as a tobacco substitute. Studies have shown that cytisine has a high affinity for the ⁇ broom subtype of the nicotinic acetylcholine receptor and is a low nonspecific partial agonist.
  • the purpose of the present application is to utilize the synergistic effect of cytisine, a partial agonist of nicotine acetylcholine, on nicotine, so that the electronic cigarette liquid has better suction satisfaction and higher addiction relief without increasing the amount of nicotine, so as to better meet the needs of consumers who have a substitute for smoking; utilize cytisine to partially replace nicotine to achieve a synergistic and synergistic comprehensive experience, reduce the amount of nicotine, and use a low dose of nicotine electronic atomization liquid to achieve the satisfaction of the usual dose (20mg/ml) of electronic atomization liquid on the market, thereby reducing the exposure to nicotine, further reducing the addictiveness and health hazard risks of electronic cigarettes, and making electronic cigarettes a more effective substitute for smoking and smoking cessation tools.
  • the components of the atomized liquid in some embodiments and comparative examples of the present application are shown in Tables 1-2.
  • the components of the atomized liquid in Tables 1 and 2 are all calculated based on mass fractions.
  • the mass fraction of nicotine is 1.80%
  • the mass fraction of cytisine increases from 0 to 3.00%
  • 15.00% mango flavor is added to the flavor composition.
  • the mass fraction of nicotine is 1.60%
  • the mass fraction of cytisine increases from 0 to 2.80%
  • the flavor composition is 2.00% tobacco extract and 12.00% tobacco flavor.
  • Example 7 the mass fraction of nicotine is 3.00%, the mass fraction of cytisine increases from 0 to 2.50%, and the flavor composition is blueberry flavor. It can be seen that in the blueberry flavored atomized liquid, as the mass fraction of cytisine increases, the addiction relief of the atomized liquid is significantly improved.
  • Comparative Example 4 and Example 8 the mass fraction of nicotine is 0.50%, the mass fraction of cytisine increases from 0 to 5.00%, and the flavor composition is 13.00% grape flavor.
  • Example 8 when the mass fraction of nicotine in Example 8 is 0.50%, the scores of irritation, head feeling, and sustained effect of the atomized liquid are 2.86, 2.71, and 2.07, respectively.
  • the mass fraction of nicotine in Example 11 is 1.00%, and the scores of irritation, head feeling, and sustained effect of the atomized liquid are 4.25, 3.32, and 3.12, respectively, and the addiction relief degree of the atomized liquid is greatly improved.
  • the EU stipulates that the nicotine content in electronic cigarettes is less than 2.00%. Therefore, in some embodiments of the present application, the mass fraction of nicotine in the atomized liquid is 1.00%-2.00%, and the addiction relief degree of the atomized liquid is relatively high.
  • the mass fraction of cytisine is 1.00%-5.00%.
  • the mass fraction of nicotine remains unchanged, the mass fraction of cytisine increases, and the addiction relief degree of the atomized liquid is significantly improved. Therefore, in terms of improving the addiction relief degree, cytisine and nicotine have a synergistic effect.
  • the mass fraction of cytisine is 1.00%-4.00%.
  • the mass fraction of nicotine is 1.00%-2.00%, the mass fraction of nicotine is reduced, and cytisine is used to replace part of the nicotine.
  • the mass fraction of cytisine is 1.00%-4.00%, which can maintain the addiction-relieving degree of the atomized liquid at a certain level.
  • cytisine can be used to partially replace nicotine to achieve a synergistic and comprehensive experience, reduce the amount of nicotine, and use a low dose of nicotine electronic atomization liquid to achieve the satisfaction of the usual dose (20mg/ml) of electronic atomization liquid on the market, thereby reducing the exposure to nicotine, further reducing the addictiveness and health hazard risks of electronic cigarettes, and making electronic cigarettes a more effective smoking cessation tool.
  • the mass fraction of cytisine is 1.00%-3.00%.
  • the addiction relief degree of the atomized liquid is significantly improved during the process of increasing the mass fraction of cytisine from 1.00% to 3.00%, and the synergistic effect of cytisine and nicotine on addiction relief is relatively significant.
  • cytisine includes the free base of cytisine.
  • cytisine includes cytisine salts.
  • the cytisine salt is generated by reacting cytisine with an organic acid
  • the organic acid is selected from one or a combination of formic acid, acetic acid, propionic acid, butyric acid, ⁇ -furanic acid, ⁇ -furanomethylbutyric acid, isovaleric acid, ⁇ -methylvaleric acid, levulinic acid, lactic acid, citric acid, malic acid, tartaric acid, succinic acid, oxalic acid, maleic acid, glycolic acid, lauric acid, myristic acid, palmitic acid, stearic acid, oleic acid, linoleic acid, linolenic acid, benzoic acid, phenylacetic acid, caffeic acid, coumaric acid, phthalic acid and terephthalic acid.
  • the atomized liquid further includes a sweetener, and the mass fraction of the sweetener is 0.01%-0.60%.
  • the sweetener includes one or a combination of neotame, cyclamate, sucralose, aspartame, steviol glycosides, acesulfame potassium and mogroside.
  • the atomized liquid further includes a cooling agent, and the mass fraction of the cooling agent is 0.10%-8.00%.
  • the cooling agent includes one or a combination of menthol, menthone, isomenthone, WS-23 (2-isopropyl-N,2,3-trimethylbutyramide), WS-3 (N-ethyl-p-menthyl-3-carboxamide) and WS-5 (N-(ethoxycarbonylmethyl)-p-alkane-3-carboxamide).
  • the atomized liquid further includes a flavor composition, and the mass fraction of the flavor composition is 1.00%-20.00%.
  • the atomized liquid further includes a flavor composition, and the mass fraction of the flavor composition is 10.00%-15.00%.
  • the solvent includes one or a mixture of several of propylene glycol, butylene glycol, 1,2,4-butanetriol, dipropylene glycol, diethylene glycol, triethylene glycol, polyethylene glycol 200, polyethylene glycol 400, triacetin, glycerol, dipropylene glycol ether, ethanol, water, triethyl citrate and caprylic acid glyceride.
  • the added amounts of sweeteners, cooling agents and flavor compositions can be determined according to user needs and are not limited to the contents and types provided in this specification.
  • An embodiment of the present application also provides a method for preparing an atomized liquid, comprising:
  • the second mixture was filtered to obtain a nebulized liquid.
  • a sweetener and a cooling agent are also added to the solution.
  • the process of adding nicotine to the first mixture and stirring to obtain the second mixture also includes adding a flavor composition to the first mixture.
  • 80-120 mesh filter cloth is used for filtration.
  • a method for preparing an atomized liquid comprising:
  • the second mixture was filtered through a filter cloth having a mesh size of 80 to 120 to obtain an atomized liquid.
  • One embodiment of the present application further provides an electronic atomization device, comprising the atomizing liquid and an atomizer provided in the above embodiment, the atomizer being used to atomize the atomizing liquid to generate an aerosol.
  • the atomizer may use a heating element using resistance heating, electromagnetic induction heating, infrared radiation heating, or microwave heating; in other examples, the atomizer may use a high-frequency vibration element to atomize the atomizing liquid to form aerosol particles, such as an ultrasonic atomizer.

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  • Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Des modes de réalisation de la présente demande proposent un liquide d'atomisation. Le liquide d'atomisation comprend : de la nicotine, de la cytisine et un solvant. En utilisant de la cytisine qui agit de manière synergique avec de la nicotine, le liquide d'atomisation qui garantit une meilleure satisfaction et qui présente un meilleur effet de soulagement à la dépendance au tabac est fourni sans augmenter le dosage de nicotine.
PCT/CN2024/133590 2023-11-24 2024-11-21 Liquide d'atomisation, procédé de préparation de liquide d'atomisation et dispositif d'atomisation électronique Pending WO2025108387A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN202311586681.X 2023-11-24
CN202311586681.XA CN120036520A (zh) 2023-11-24 2023-11-24 一种雾化液、雾化液的制备方法以及电子雾化装置

Publications (1)

Publication Number Publication Date
WO2025108387A1 true WO2025108387A1 (fr) 2025-05-30

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Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107660815A (zh) * 2016-07-27 2018-02-06 湖南中烟工业有限责任公司 一种稳定释放烟香的电子烟液
EP3834814A1 (fr) * 2019-12-10 2021-06-16 Adamed Pharma S.A. Composition pharmaceutique liquide comprenant de la cytisine
CN113100490A (zh) * 2021-05-21 2021-07-13 张家港外星人新材料科技有限公司 生物碱与酚反应合成物、雾化液、雾化弹及电子雾化器
CN114947174A (zh) * 2021-02-25 2022-08-30 深圳市合元科技有限公司 气溶胶形成基质以及气溶胶生成系统
CN115119955A (zh) * 2022-08-03 2022-09-30 昌宁德康生物科技（深圳）有限公司 一种无烟型雾化液、及其制备方法和使用方法
CN115998682A (zh) * 2023-02-22 2023-04-25 深圳市真味生物科技有限公司 含有烟酰胺单核苷酸的雾化液及其制备方法和应用

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107660815A (zh) * 2016-07-27 2018-02-06 湖南中烟工业有限责任公司 一种稳定释放烟香的电子烟液
EP3834814A1 (fr) * 2019-12-10 2021-06-16 Adamed Pharma S.A. Composition pharmaceutique liquide comprenant de la cytisine
CN114947174A (zh) * 2021-02-25 2022-08-30 深圳市合元科技有限公司 气溶胶形成基质以及气溶胶生成系统
CN113100490A (zh) * 2021-05-21 2021-07-13 张家港外星人新材料科技有限公司 生物碱与酚反应合成物、雾化液、雾化弹及电子雾化器
CN115119955A (zh) * 2022-08-03 2022-09-30 昌宁德康生物科技（深圳）有限公司 一种无烟型雾化液、及其制备方法和使用方法
CN115998682A (zh) * 2023-02-22 2023-04-25 深圳市真味生物科技有限公司 含有烟酰胺单核苷酸的雾化液及其制备方法和应用

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