EP2862454A1 - Composition liquide pour cigarette électronique - Google Patents

Composition liquide pour cigarette électronique Download PDF

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Publication number
EP2862454A1
EP2862454A1 EP20140189319 EP14189319A EP2862454A1 EP 2862454 A1 EP2862454 A1 EP 2862454A1 EP 20140189319 EP20140189319 EP 20140189319 EP 14189319 A EP14189319 A EP 14189319A EP 2862454 A1 EP2862454 A1 EP 2862454A1
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EP
European Patent Office
Prior art keywords
trp
liquid composition
activator
ethanol
agonist
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.)
Granted
Application number
EP20140189319
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German (de)
English (en)
Other versions
EP2862454B1 (fr
EP2862454B8 (fr
Inventor
Olaf Meinert
Ilonka Paul
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.)
Valeo GmbH
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Valeo Laboratories GmbH
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Publication date
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Publication of EP2862454A1 publication Critical patent/EP2862454A1/fr
Publication of EP2862454B1 publication Critical patent/EP2862454B1/fr
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Publication of EP2862454B8 publication Critical patent/EP2862454B8/fr
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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
    • 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 present invention relates to a liquid composition (e-liquid) for use in electronic cigarettes and to the use of a modulator and at least one TRP agonist / activator ("TRP" in English means “transient receptor potential” and can be used as " transient receptor potential) in a liquid, non-nicotine-containing composition that simulates the tobacco smoke or sensation of inhalation of a conventional tobacco cigarette.
  • TRP TRP agonist / activator
  • a tobacco smoker / e-cigarette steamer feels visibly uncomfortable during his stay in smoking-prohibiting areas.
  • the regular drop in nicotine levels in the body of a smoker / steamer favors this malaise, but this is not the only or most important factor controlling the craving for a tobacco or e-cigarette. Rather, the forced by use prohibitions suppressing the usual ritual on a tobacco or e-cigarette to draw, the smoke / vapor to inhale and expunge relish with relish the main cause of this malaise and the growing desire for this Ritual satisfaction.
  • a special part of this is the perceived during inhalation "flash" or "kick" in the mouth and throat and lung. This sensation, which is caused by the irritation of certain receptors, is important to the smoker / steamer in order to satisfy his desire.
  • liquids that nicotine is buried in are that while the satisfaction of the addiction is achieved, but still toxins are supplied to the body.
  • This disadvantage has been addressed by providing liquids that - mostly by adding flavors - try to create a "real smoking experience” similar to that of smoking cigarettes or nicotine-containing liquid smoking, but much less do not contain any nicotine.
  • these liquids have the disadvantage that the chemosensorics addressed by nicotine, i. the nicotine-induced "flash" is completely absent.
  • a liquid composition for an electronic cigarette ie a liquid
  • a liquid that contains no toxins such as nicotine, but still generates the above-described "flash" at the user, ie the chemosensory receptors in the way responds, as it does the smoker's usual nicotine.
  • the at least one TRP agonist / activator preferably activates at least one of the TRP receptors TRPA1, TRPV1, TRPV3 and TRPM8.
  • TRP agonists / activators are combined to activate different TRP channels.
  • Extracts comprising black pepper, horseradish, garlic, paprika, cinnamon, mint and vinegar and citric acid as TRP agonist / activator are preferably used in the liquid composition according to the invention.
  • active ingredients with at least 6-paradol and analogues serve as TRP agonist / activator.
  • 6-paradol and analogs include at least 1'-acetoxychavicol acetate and analogs, isothiocyanates and analogs, camphor and analogs, grains of paradise, thymol and analogues, and ethanol.
  • the at least one TRP agonist / activator is preferably based on the components of TRP channel subtypes.
  • liquid composition according to the invention preferably serve ethanol, glycol or glycerol as a modulator.
  • the present invention relates to a use of a modulator and at least one TRP agonist / activator in a liquid composition for electronic cigarettes that does not contain nicotine to inhale cigarette smoke.
  • the liquid composition for an electronic cigarette comprises a TRP modulator and at least one TRP agonist / activator, wherein the interaction of modulator and the at least one agonist / activator chemosensory imitation of inhaled cigarette smoke, and the liquid composition no Contains nicotine.
  • a modulator and at least one TRP agonist / activator is used in a liquid composition for electronic cigarettes that does not contain nicotine to inhale cigarette smoke.
  • the at least one TRP agonist / activator activates at least one of the TRP receptors TRPA1, TRPV1, TRPV3 and TRPM8. Furthermore, it is advantageous that multiple TRP agonists / activators are combined to activate different TRP channels. As a further advantageous embodiment, extracts containing black pepper, horseradish, garlic, paprika, cinnamon, mint and acetic and citric acid are used as the TRP agonist / activator.
  • drugs having at least 6-paradole and analogs comprise at least 1'-acetoxy-chiacicol acetate and analogs, isothiocyanates and analogues, camphors and analogues, grains of paradise, thymol and analogues, and ethanol.
  • the at least one TRP agonist / activator is based on the components of TRP channel subtypes.
  • ethanol, glycol or glycerol serve as a modulator.
  • the chemical components are mixed together.
  • the basic components of the liquid (propylene glycol, glycerine, ethanol and flavorings) are obtained directly from the chemical manufacturer or from the flavor supplier.
  • the ingredients of the liquid composition (BioNic) to be patented, for the most part, can not be conventionally sourced, at least not in the form as used in the present invention.
  • the grains of compassion so acquired can not be incorporated in the conventional form in the liquid, but it must first be extracted from this raw material, the corresponding active ingredient. This is usually done by extracting the active substance by means of ethanol by Soxhlet extraction from the raw material.
  • the active ingredient is bound directly into the ethanol, which is then introduced into the liquid. It is known to the person skilled in the art how the active substances are treated in order to be used in the liquid composition.
  • Nicotine has been shown to be a neurotoxin that, along with other conventional cigarettes, acts on sensory and autonomic afferent nerve endings, sending sensory information from the mouth, throat, and airways to the brain via the vagus, trigeminal, and other cranial nerves.
  • the brain acts accordingly, inducing autonomic reflexes and central nervous system effects that rely on the subjective experience of smoking, including "throat scratching" and behavioral behaviors stored to relieve the craving.
  • Cigarette smoking causes EEG changes and activates related, subjective behavioral reflexes on sensory reflexes, even before nicotine in the smoke is absorbed and nerve reactions can report that drug to the brain.
  • herbal analogues In order to simulate a smoking sensation as in a conventional cigarette, but without using toxins such as nicotine, herbal analogues were sought which produce these or similar chemosensory effects and no longer require the use of nicotine as a neurotoxin.
  • the sensory senses include taste, sense of smell and "chemical sensitivity” (also known as the "common chemical sense", or trigeminal chemosensorics).
  • Chemosensorics refers to effects, e.g. B. on nerve endings mediating sensations of pain or temperature.
  • specific substances such as pepperoni (capsaicin), black pepper (piperine), menthol, garlic (allicin), horseradish and wasabi (allyl isothiocyanate), camphor, wintergreen , Cinnamon (cinnamaldehyde), carbonic acid, for example, in drinks (carbon dioxide) and some air pollutants is caused.
  • Such sensations in the oral cavity and in the nasal cavities become over mediate the trigeminal nerve and are elements of the somatosensory system.
  • chemical signals are transmitted to the brain via the vagus nerve, which can directly influence the brain
  • the appetitive circuit is satisfied by chemosensory stimulation, without supplying the body with the actual active substance such as nicotine. Due to the chemosensory stimulation, the brain assumes that with the usual inhalation and the usual stimulating nicotine was supplied. In addition, and not less strong is the positive influence of the imitation of tactile, kinaesthetic and organoleptic aspects of smoking, for example, by an optically visible evaporation of the liquid and thus suggests that it is the same habitual ritual as smoking a cigarette, although it is merely an evaporation of much more harmless ingredients without toxins.
  • TRP Transient Receptor Potential
  • TRP channels are a class of receptors on sensory nerves that have the ability to activate them by triggering. TRP channels transmit the sensations of spicy, hot or cold, as well as components in the inhaled air to the central nervous system. In addition to chemosensory stimulation, activation of the sensory nerve endings by the TRP channels also induces local effects, such as coughing, sneezing, regulation of body temperature or other subjective sensations. In addition, the activation of TRP channels requires only very low constituents of the corresponding TRP-relevant active substance, so that in principle even a theoretically harmful concentration can be avoided.
  • the TRP channel activators provide minimal volatile components in the inspired air to induce a cigarette smoke-like chemosensory stimulation without the need to absorb a bioactive drug concentration in the body.
  • the following is an exemplary liquid composition at a product unit of 10000 mg: 4500 mg propylene glycol, 4000 mg Glycerols, 1000 mg food flavorings, 487 mg ethanol, further containing the following components in their entirety for a chemosensory reaction: 1.25 mg Piper nigrum, 3.75 mg Melegueta Aframomum, 1.25 mg benzoin, 0.5 mg allicin, 0 , 7 mg isothiocyanate, 0.425 mg zingiberis rhizoma, 4.15 mg capsaicin, 0.625 mg Zanthoxylum piperitum, 0.35 mg curcumin.
  • composition is as follows: propylene glycol: 40% to 50%, glycerols: 36% to 44%, food flavors: 9% to 11%, ethanol: 4.3% to 5.3%, further comprising the following as a whole for one chemosensory response components: Piper nigrum: 0.12% to 0.13%, Melegueta Aframomum: 0.03% to 0.04%, Benzoin: 0.012% to 0.014%, Allicin: 0.0049% to 0.0051% , Isothiocyanate: 0.006% to 0.008%, Zingiberis rhizoma: 0.0038% to 0.0047%, Capsaicin: 0.0037% to 0.0046%, Zanthoxylum piperitum: 0.0056% to 0.0069%, Curcumin: 0 , 0031% to 0.0039%.
  • TRP V1 is a temperature-sensing channel whose activation threshold can still be lowered by using ethanol as a TRP modulator.
  • TRP V1 agonists such as extracts of chilli, Szechuan pepper or mustard by using even lower concentrations can be achieved.
  • TRP activators provide a unique basis for the chemosensory imitation of inhaled cigarette smoke without the necessity of using incinerated, often carcinogenic substances.
  • TRP activators enables the imitation of subjective and physiological chemosensory experiences, such as the inhalation of cigarette smoke.
  • Known TRP activators are, for example, extracts of black pepper, horseradish, garlic, paprika, cinnamon, mint and other known TRP channels activating substances, as well as acetic and citric acid. By utilizing a complex mixture of these agents, the activation ability can be both broad and potentiated.
  • the use of low concentrations of these activators in the liquid supports the ability of the receptors for a rapid desensitization, so that after only a short time (as part of an inhalation interval of an electric cigarette) the chemosensory stimulation can be done again and in full sensation size.
  • TRP activators offer in particular the active ingredients which contain 6-paradol and analogues. These include, for example: 1'-acetoxychavicol acetate and analogs, isothiocyanates and analogs, camphor and analogs, grains of paradise, thymol and analogs, and ethanol. Among others, these activators are used in the liquid mixtures.
  • the liquid composition according to the invention makes it possible to activate each individual TRP channel (TRP A1, TRP V1, TRP V3 and TRP M8). The activation of each individual TRP channel with the respective activators is decisive here in order to achieve a corresponding tobacco smoke-like inhalation sensation.
  • the desired inclusion of the TRP M8 receptor in the functional base is based on its ability to suppress by stimulation / activation the inhalation sensation caused by coughing.
  • a complex composition of different activators is necessary along with a suitable choice of modulators.
  • the glycerine is one-quarter or more, and preferably two-thirds or less, of the liquid composition (by weight, expressed in "%", that is, percent by weight).
  • Particularly preferred weight fractions of the glycerol are 30% or more, more preferably 33% or more, even more preferably 36% or more and especially preferably 39% or more.
  • Upper limits of the content by weight of the glycerin are preferably 55% or less, more preferably 50% or less, still more preferably 45% or less, and particularly preferably 41% or less.
  • the proportion by weight of glycerol expressed in percent by weight is accordingly preferably 30%. to 55%, more preferably 33% to 50%, even more preferably 36% to 45%, and most preferably 39% to 41%.
  • the composition has a very low allergenic potential.
  • the allicin used in some exemplary embodiments of 0.0049% -0.0051% by weight, derived from mustard seeds, is suspected of inducing allergenic reactions.
  • the other constituents used according to the invention in particular glycerol and 6-paradole or analogues thereof, regularly trigger no allergenic reactions.
  • TRP activators are based on the constituents of the TRP channel subtypes.
  • the use of drug mixtures creates the possibility of activating or deactivating various TRP channels in variable intensities by means of also variably long time arcs.
  • This control affects not only the intensity and time arcs, but also the local space by the chemosensory sensation takes place, such as: oral cavity, pharynx, lung space.
  • Related tests have shown that activation of a subchannel enhances the actual chemosensory sensation without having to raise the concentration of the drug itself.
  • TRP channels in the human body chemosensory, since in humans TRP channels play an important role in the perception of taste (sweet, sour, umami), pheromones, temperature (hot, hot, cold) , Pain u. a. play.
  • ethanol in addition to glycol and glycerol, ethanol, optionally additionally one or more volatile agonists of TRPA1, TRPV1, TRPV3 and / or TRPM8 channels, and, if necessary, volatile, low molecular weight carboxylic acid and flavoring agents can be used.
  • One component of different concentrated liquid mixtures for electrical evaporation is an extract from the chili pepper, which activates the TRP receptor TRPV1 by inhalation and causes a chemosensory reaction.
  • a component of differently concentrated liquid mixtures for electrical evaporation is an extract of black pepper, which activates the TRP receptor TRPV1 by inhalation and causes a chemosensory reaction.
  • One component of different concentrated liquid mixtures for electrical evaporation is an extract of zingiberaceae (ginger plants), which activates the TRP receptor TRP-1 and TRP-2 by inhalation and causes a chemosensory reaction.
  • An ingredient of different concentrated liquid mixtures for electrical evaporation is an extract of isothiocyanates, which activates the TRP receptor TRPA1 by inhalation and causes a chemosensory reaction.
  • One component of differently concentrated liquid mixtures for electrical evaporation is an extract of cloves, which activates the TRP receptor TRPA1 by inhalation and causes a chemosensory reaction.
  • One component of differently concentrated liquid mixtures for electrical evaporation is an extract of camphor, which activates the TRP receptor TRPV1 + TRPV2 by inhalation and causes a chemosensory reaction.
  • One component of differently concentrated liquid mixtures for electrical evaporation is an extract of Aframomum melegueta (grains of paradise), which activates the TRP receptor TRPA1 + TRPV1 by inhalation and causes a chemosensory reaction.
  • a component of differently concentrated liquid mixtures for electrical evaporation is an extract of Zanthoxylum piperitum (Szechuan pepper), which by inhalation the TRP receptor TRPA1 + TRPV1 activated and causes a chemosensory reaction.
  • One component of differently concentrated liquid mixtures for electrical evaporation is an extract of thyme, which activates the TRP receptor TRPV3 by inhalation and causes a chemosensory reaction.
  • One component of different concentrated liquid mixtures for electrical evaporation is an extract of peppermint, which activates the TRP receptor TRPM8 by inhalation and causes a chemosensory reaction.
  • One component of the differently concentrated liquid mixtures for electrical evaporation is an extract of vanilla, which activates the TRP receptor TRPV3 by inhalation and causes a chemosensory reaction.
  • One component of differently concentrated liquid mixtures for electrical evaporation is an extract of eucalyptus, which activates the TRP receptor TRPM8 by inhalation and causes a chemosensory reaction.
  • An ingredient of liquid concentrated mixtures for electrical evaporation are flavor extracts that activate the TRPM8 TRPM8 by inhalation and induce a chemosensory reaction.
  • One component of different concentrated liquid mixtures for electrical evaporation is caffeine, which activates the TRP receptor TRPA1 by inhalation and causes a chemosensory reaction.
  • One component of different concentrated liquid mixtures for electrical evaporation are low molecular weight organic acids that activate a TRP receptor by inhalation and cause a chemosensory reaction.
  • One component of different concentrated liquid mixtures for electrical evaporation is ethanol, which activates the TRPV receptor TRPV1 by inhalation and causes a chemosensory reaction.
  • liquid mixtures according to the invention solves the object of the present invention.
  • a "real" smoke feeling is mediated, i. the already described “flash” takes place without toxins such as nicotine being used.
  • the smallest constituents of the extracts in the liquid are sufficient to achieve the desired effect.
  • compositions having different weight percentages of glycerol were prepared by appropriately decreasing or increasing the level, with the propylene glycol content adjusted accordingly to produce compositions having the same total weights.
  • the scores of the prepared eleven compositions (compositions 1a to 11a) by the subjects were averaged and summarized in the following Table 1: Table 1 Composition no. Glycerol content (% by weight) Average rating 1a 0 4.1 2a 10 3.8 3a 20 3.5 4a 30 2.5 5a 40 1.4 6a 50 2,4 7a 60 2.9 8a 70 3.7 9a 80 4.0 10a 90 4.3 11a 100 4.7
  • compositions 1 b to 11 b were asked to use compositions as in Table 1 above for the production of smoke and to assess the inhalation sensation in turn according to the above grading scale.
  • the corresponding grades by the subjects were again averaged and summarized in the following Table 2: Table 2 Composition no.
  • Glycerol content (% by weight) Average rating 1b 0 5.3 2 B 10 4.9 3b 20 4.5 4b 30 3.4 5b 40 2.6 6b 50 3.5 7b 60 4.9 8b 70 4.8 9b 80 5.1 10b 90 5.3 11b 100 5.7
  • TRP agonist / activator selected from 6-paradol and analogues (here Melegueta Aframomum) and glycerol as TRP modulator in all comparable compositions to a usually at least a grade better assessment of the inhalation sense than similar to tobacco smoke. Furthermore, it is clear that the inventively preferred Glyceringehalte led to a further increase in the positive inhalation sensation.

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  • Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
EP14189319.8A 2013-10-18 2014-10-17 Composition liquide pour cigarette électronique Active EP2862454B8 (fr)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
LU92296A LU92296B1 (de) 2013-10-18 2013-10-18 Fl}ssige Zusammensetzung f}r eine elektronische Zigarette

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EP2862454A1 true EP2862454A1 (fr) 2015-04-22
EP2862454B1 EP2862454B1 (fr) 2020-05-13
EP2862454B8 EP2862454B8 (fr) 2020-06-17

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WO2017103136A1 (fr) * 2015-12-18 2017-06-22 Philip Morris Products S.A. Éléments d'amélioration de résistance, et procédé permettant d'obtenir une amélioration de résistance dans un dispositif à vapoter électronique
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USD825102S1 (en) 2016-07-28 2018-08-07 Juul Labs, Inc. Vaporizer device with cartridge
US10045568B2 (en) 2013-12-23 2018-08-14 Juul Labs, Inc. Vaporization device systems and methods
US10045567B2 (en) 2013-12-23 2018-08-14 Juul Labs, Inc. Vaporization device systems and methods
US10058130B2 (en) 2013-12-23 2018-08-28 Juul Labs, Inc. Cartridge for use with a vaporizer device
US10076139B2 (en) 2013-12-23 2018-09-18 Juul Labs, Inc. Vaporizer apparatus
US10104915B2 (en) 2013-12-23 2018-10-23 Juul Labs, Inc. Securely attaching cartridges for vaporizer devices
US10111470B2 (en) 2013-12-23 2018-10-30 Juul Labs, Inc. Vaporizer apparatus
USD836541S1 (en) 2016-06-23 2018-12-25 Pax Labs, Inc. Charging device
USD842536S1 (en) 2016-07-28 2019-03-05 Juul Labs, Inc. Vaporizer cartridge
US10244793B2 (en) 2005-07-19 2019-04-02 Juul Labs, Inc. Devices for vaporization of a substance
CN109619656A (zh) * 2019-01-18 2019-04-16 薪火高科(深圳)有限公司 一种具有消炎抗菌功效的电子烟烟液
US10279934B2 (en) 2013-03-15 2019-05-07 Juul Labs, Inc. Fillable vaporizer cartridge and method of filling
USD848057S1 (en) 2016-06-23 2019-05-07 Pax Labs, Inc. Lid for a vaporizer
USD849996S1 (en) 2016-06-16 2019-05-28 Pax Labs, Inc. Vaporizer cartridge
USD851830S1 (en) 2016-06-23 2019-06-18 Pax Labs, Inc. Combined vaporizer tamp and pick tool
US10405582B2 (en) 2016-03-10 2019-09-10 Pax Labs, Inc. Vaporization device with lip sensing
US10512282B2 (en) 2014-12-05 2019-12-24 Juul Labs, Inc. Calibrated dose control
USD887632S1 (en) 2017-09-14 2020-06-16 Pax Labs, Inc. Vaporizer cartridge
US10865001B2 (en) 2016-02-11 2020-12-15 Juul Labs, Inc. Fillable vaporizer cartridge and method of filling
CN118120958A (zh) * 2024-02-20 2024-06-04 深圳昱朋科技有限公司 一种雾化香精添加剂及雾化香精
WO2024131270A1 (fr) * 2022-12-19 2024-06-27 惠州市新泓威科技有限公司 Liquide d'atomisation de cigarette électronique ayant un effet d'inhibition de l'activité de la monoamine oxydase
WO2024131309A1 (fr) * 2022-12-19 2024-06-27 惠州市新泓威科技有限公司 Liquide atomisé de cigarette électronique ayant un effet d'inhibition des monoamine oxydases

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US10638792B2 (en) 2013-03-15 2020-05-05 Juul Labs, Inc. Securely attaching cartridges for vaporizer devices
US10279934B2 (en) 2013-03-15 2019-05-07 Juul Labs, Inc. Fillable vaporizer cartridge and method of filling
US10201190B2 (en) 2013-12-23 2019-02-12 Juul Labs, Inc. Cartridge for use with a vaporizer device
US10058130B2 (en) 2013-12-23 2018-08-28 Juul Labs, Inc. Cartridge for use with a vaporizer device
US10701975B2 (en) 2013-12-23 2020-07-07 Juul Labs, Inc. Vaporization device systems and methods
US10058124B2 (en) 2013-12-23 2018-08-28 Juul Labs, Inc. Vaporization device systems and methods
US10045568B2 (en) 2013-12-23 2018-08-14 Juul Labs, Inc. Vaporization device systems and methods
US10070669B2 (en) 2013-12-23 2018-09-11 Juul Labs, Inc. Cartridge for use with a vaporizer device
US10076139B2 (en) 2013-12-23 2018-09-18 Juul Labs, Inc. Vaporizer apparatus
US10104915B2 (en) 2013-12-23 2018-10-23 Juul Labs, Inc. Securely attaching cartridges for vaporizer devices
US10111470B2 (en) 2013-12-23 2018-10-30 Juul Labs, Inc. Vaporizer apparatus
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