Classifications

• • A—HUMAN NECESSITIES
  • A24—TOBACCO; CIGARS; CIGARETTES; SIMULATED SMOKING DEVICES; SMOKERS' REQUISITES
  • A24F—SMOKERS' REQUISITES; MATCH BOXES; SIMULATED SMOKING DEVICES
  • A24F42/00—Simulated smoking devices other than electrically operated; Component parts thereof; Manufacture or testing thereof
  • A24F42/60—Constructional details
• • A—HUMAN NECESSITIES
  • A24—TOBACCO; CIGARS; CIGARETTES; SIMULATED SMOKING DEVICES; SMOKERS' REQUISITES
  • A24F—SMOKERS' REQUISITES; MATCH BOXES; SIMULATED SMOKING DEVICES
  • A24F42/00—Simulated smoking devices other than electrically operated; Component parts thereof; Manufacture or testing thereof
  • A24F42/20—Devices without heating means
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P25/00—Drugs for disorders of the nervous system
  • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
  • A61P25/34—Tobacco-abuse

Definitions

• This invention relates to a container comprising nicotine.
• the container is for use in an inhaling device.
• Such a device is for use in nicotine replacement therapy treatment (NRT) and tobacco dependence treatment.
• NRT nicotine replacement therapy treatment
• Background of the Invention Tobacco dependence and reduction thereof
• Nicotine (C10H14N2) is an organic compound and is the principal alkaloid of tobacco and it is the chief addictive ingredient in the tobacco used in cigarettes, cigars, snuff and the like. Nicotine is also an addictive drug and smokers characteristically display a strong tendency to relapse after having successfully stopped smoking for a time. Nicotine is among the world's most used drug, along with alcohol and caffeine from coffee and tea. It is an addictive poisonous alkaloid. And it is also used as an insecticide. The minimal acute lethal dose of nicotine in human adults is 40 to 60 mg.
• the administration of nicotine usually provides a pleasant feeling.
• the usual method of administration is by intake via the mouth, either by smoking e.g. a cigarette, a cigar or a pipe, or snuffing or chewing tobacco.
• smoking has, as earlier mentioned, health hazards and it is therefore desirable to formulate an alternative manner of administering nicotine in a pleasurable manner that can be used to facilitate withdrawal from smoking and/or used as a replacement for smoking.
• Nicotine replacement products Upon the smoking of a cigarette, nicotine is quickly absorbed into the smoker's blood and reaches the brain within around ten seconds after inhalation. This quick uptake of nicotine gives the consumer a rapid satisfaction, or kick, and this satisfaction lasts during the smoking time of the cigarette and for a period of time thereafter.
• the poisonous, toxic, carcinogenic, and addictive nature of smoking has provided efforts for methods, compositions and devices, which help in breaking the habit of smoking cigarettes. Nicotine replacement products
• the present successes in achieving reduction in the incidence of smoking have been relatively poor using presently known products.
• the present state of the art involves both behavioral approaches and pharmacological approaches. More than 80 % of the tobacco smokers who initially quit smoking after using some behavioral or pharmacological approach to singly reduce smoking incidence generally relapse and return to the habit of smoking at their former rate of smoking within about a one year's period of time.
• Nicotine-containing nose drops have been reported (Russell et al. 5 British Medical Journal, Vol. 286, p. 683 (1983); Jarvis et al., British Journal of Addiction, Vol. 82, p. 983 (1987)). Nose drops, however, are difficult to administer and are not convenient to use at work or in other public situations. Ways of administrating nicotine by delivering directly into the nasal cavity by spraying are known from US 4,579,858, DE 32 41 437 and WO 93/12764. There may, though, be local nasal irritation with use of nasal nicotine formulations. The difficulty in administration also results in unpredictability of the dose of nicotine administered.
• Nicotine mouth sprays see e.g. US 6,024,097 and US 5,810,018) and nicotine chewing gums (see e.g. US 3,845,217) are also known:-
• inhaling devices resembling a cigarette are known for uptake of nicotine vapors orally as suggested in US 5,167,242, wherein the inhaling device contains a nicotine reservoir.
• the present invention relates primarily, but not exclusively, to a novel and inventive improvement of the nicotine reservoir (plug) disclosed in US 5,167,242.
• One embodiment of the inhaling device disclosed in US 5,167,242 comprises a cylindrical cartridge in which is placed a nicotine reservoir.
• a reservoir consists of a porous plug made of polymer or other suitable material, which is loaded with nicotine.
• Suitable materials for such a plug are e.g. those mentioned in US 4,284,089, US 4,800,903 and US 4,813,437 e.g. polymeric material containing polyolefin, polyethylene, polypropylene, polybutadiene, poly-1-butene, polyisobutylene, polyisoprene, poly-4-methyl-l-pentene or combinations thereof, a fibrous material which may comprise cellulose- acetate polypropylene, polyester, polyethylene and combinations thereof.
• US 4,793,366 discloses a device for inhaling nicotine with a "draw” similar to that of a conventional cigarette - though without showing that such a "draw” may be obtained with the claimed device.
• US 5,101,838 discloses a device for smoking simulation where the carrier for nicotine preferably is made of spherical particles.
• US 5,167,242, US 4,284,089, US 4,800,903, US 4,813,437, US 4,793,366 and US 5,101,838 are hereby incorporated by reference.
• nicotine is intended to include nicotine, 3-(l-methyl-2-pyrrolidinyl)-pyridine, with its base form, racemic form, R- and S-forms, including synthetic nicotine as well as nicotine extracts from tobacco plants, or parts thereof, such as the genus Nicotiana alone or in combination; or pharmaceutically acceptable salts.
• capacil comprising nicotine is intended to include a nicotine reservoir loaded with nicotine that will allow air to pass through and that will deliver nicotine in gaseous or liquid aerosol form to a subject.
• fast reduction of the urge to smoke or use tobacco is herein intended to mean an initial priming of the subject so as to achieve a reduction of the urge to smoke or use tobacco.
• fibers and “filaments” are intended to mean any of the thread-like parts that are formed from plant and/or artificial material with arbitrary cross sections.
• tobacco-containing material may be material used for e g smoking, snuffing or chewing and may comprise a cigarette, a cigar, snuff, pipe tobacco and chewing tobacco.
• shaped mass is intended to mean a mass of material deliberately shaped.
• the present invention is intended to solve the above-mentioned problem, i.e. that the user does not receive enough nicotine per puff to experience satisfaction.
• said problem could't be solved by increasing the amount of nicotine in the container since the air inhaled with the existing device is already saturated with nicotine and hence cannot be loaded with more nicotine.
• said problem is solved by increasing the volume of air inhaled per puff thereby increasing the amount of nicotine being inhaled per puff - this being achieved by using a nicotine container comprising a shaped mass of fibers or filaments.
• The_main object of the present invention is thus to provide a container comprising nicotine and a shaped mass of fibers or filaments, which is able to reversibly retain and release nicotine.
• This container allow a larger amount of air being inhaled per puff and also provide that the air is inhaled with less efforts compared to the above-mentioned presently known plugs.
• the flow resistance through the present container is thus lower than the flow resistance through the existing plugs. It has also been found that with the present invention the flow resistance may be lowered to below a half, and even below a fourth, of the flow resistance of presently used plugs in nicotine inhalers. The air passing through the container is adequately saturated with nicotine in spite of the low airflow resistance.
• the present invention also provides a method for obtaining reduction of the urge to smoke or use tobacco containing material and/or for providing a fast sense of smoking satisfaction without smoking, comprising the steps of replacing at least partly the tobacco containing material used with an inhaling device that comprises the above-mentioned container comprising nicotine.
• the present invention also provides a system for delivering nicotine to a subject, which comprises said container comprising nicotine and at least one other means for obtaining reduction of the urge to smoke or use of tobacco and a system for obtaining reduction of the urge to smoke or otherwise use of tobacco and/or for providing a sense of smoking satisfaction without smoking, comprising said container comprising nicotine and at least one other method for obtaining reduction of the urge to smoke or otherwise use of tobacco.
• Said system may be a system wherein the at least one other method is selected from the group consisting of administration through chewing gums, nasal sprays, transdermal patches, mouth sprays, lozenges, tablets and parenteral methods, subcutaneous methods, intravenous methods, rectal methods, vaginal methods and transmucousal methods; or otherwise use of tobacco.
• the present invention also relates to the use of said product that will according to the invention rapidly deliver nicotine to a subject and also to the use of the present invention for obtaining a quick and/or sustained and/or complete reduction of the urge to smoke or use tobacco and/or for providing a sense of smoking satisfaction without smoking resembUng the sense of smoking satisfaction and/or for obtaining a reduction of the urge to smoke obtained after regular smoking or use of tobacco.
• said container comprising nicotine has fibers or filaments that comprise polymeric substances.
• the polymeric substances may be selected from polyolefin, polyester or poly- amide and are preferably selected from the group consisting of polyethylene, polyethylene, preferably high-density polyethylene or ultra high molecular weight polyethylene, polypropylene, polybutadiene, poly-l-butene 5 polyisobutene, polyisoprene, polyvinylidene chloride, ethylene vinyl alcohol, poly- lactide-glycolide copolymer, polycarbonate, polyethylene naphthalene, polytrimethylene naphthalene, polyethylene terephthalate, terephthalate-isophthalate polyesters, polybutylene terephthalate, liquid crystalline polymer that comprises hydroxy benzoic acid and hydroxy naphtenic acid, a copolymer of acrylonitrile and methacrylate grafted to nitrile rubber, which is commercially available under the trademark Barex , nylon
• the fibers or filaments are non-sintered.
• the container may though comprise also non- sintered material.
• the fibers or filaments may comprise also non-polymeric materials, such as glass, metals, e g aluminum and/or steel.
• the fibers or filaments may optionally be coated.
• the container may also comprise non-fibrous material.
• the shaped mass of fibers or filaments is non-sintered.
• the container may though comprise also non-sintered material.
• the shaped mass of fibers or filaments may comprise non-polymeric material, such as glass, metals, e g aluminum and/or steel, paper, cellulose and/or cloth.
• a preferred type of fibers or filaments is made of polyethylene terephtalate, preferably covered with copolyolefin.
• the fibers or filaments may be manufactured in a number of different ways known in the art, such as through extrusion and spinning.
• the container should have a flow resistance of gas being lower than around 0,6 kPa, more preferably lower than around 0,3 kPa at an airflow rate of 1000 ml/min.
• the nicotine is preferably retained to the shaped mass of fibers or filaments by chemical binding and/or by adsorption and/or by absorption and released by breaking these mechanisms.
• the abso ⁇ tion and/or adsorption processes, which release nicotine may further be electrically enhanced and/or modified by temperature.
• the container is for use in a nicotine-inhaling device, which is adapted to be received in the mouth or in the nose.
• the container should preferably be encapsulated in such a way that nicotine will not unintentionally migrate out from the container and so that environmental oxygen will not enter the container.
• a nicotine-impermeable copolymer made of acrylonitrile and methacrylate and grafted to nitrile rubber can be used, said copolymer being commercially available under the trademark Barex ® .
• Polyethylene naphtalate, known under the name PEN, and/or a liquid crystalline polymer comprising hydroxy benzoic acid and hydroxy naphtenic acid, known under the name Vectra A530, can also be used for such encapsulation.
• said polymers can be laminated, e g with aluminum layer.
• said encapsulation should be made in an oxygen-free environment.
• the encapsulation is broken in order for the user to inhale through the container. Said encapsulation is essence is done according to the disclosure of the above- mentioned patent US 5,167,242.
• One preferred embodiment of loading the containers with nicotine is to let a gas comprising nicotine pass through the containers thus allowing the nicotine to be absorbed and/or adsorbed by the material of the container.
• the solvent is an organic solvent, preferably an organic solvent having a low boiling point and being more volatile than nicotine, more preferably an organic solvent being selected from the group of ethers, ketons and alcohols, even more preferably being an organic solvent being selected from alcohols, and most preferably being ethanol.
• Still another preferred embodiment of loading the containers with nicotine is to inject a solution comprising nicotine, with e.g. a syringe, in the containers.
• the containers may also be loaded with nicotine by spraying or soaking or immersing the fibers or filaments with nicotine or with a nicotine-containing liquid directly upon the fibers or filaments, and the optional non-fibrous material, having been manufactured, e g upon them having been extruded or spun, prior to the fibers or filaments being formed to a shaped mass.
• the same loading principle could be applied if the containers optionally comprise also non-fibrous material.
• additives may optionally be added to the containers, e g one or more stabilizing additives, such as those selected from the group consisting of antioxidants including vitamin E, i.e. tocopheroles, vitamin C, i.e. ascorbic acid, sodium pyrosulfite, butylhydroxytoluene, butylated hydroxyanisole; and preservatives including parabenes, citric acid, tartaric acid, lactic acid, malic acid, acetic acid, benzoic acid, and sorbic acid; and chelating agents, such as EDTA; and galates, such as propyl galate.
• antioxidants including vitamin E, i.e. tocopheroles, vitamin C, i.e. ascorbic acid, sodium pyrosulfite, butylhydroxytoluene, butylated hydroxyanisole
• preservatives including parabenes, citric acid, tartaric acid, lactic acid, malic acid, acetic acid, benzoic acid
• additives can comprise one or more additives selected from the group consisting of enhancers, such as azone, vitamins, such as vitamins B, C and E, minerals, such as fluorides, especially sodium fluoride, sodium monofluoro phosphate and stannous fluoride, anti-odors, such as zinc and cyclodextrins, propellants, such as 1,1,2,2-tetrafluoroethane (HFC- 134a), optionally being liquefied, and 1,1,1,2,3,3, 3-heptafluororpropane (HFC-227), optionally being liquefied, sweeteners including one or more synthetic or natural sugars, such as those selected from the group consisting of arti- ficial sweeteners such as saccharin, sodium saccharin, aspartame, e g NutraSweet, acesulfame or acesulfame K (also called potassium acesulfame), thaumatin and glycyrrhizin
• Flavor and aroma additives can also be added. These may comprise one or more synthetic or natural flavoring or aromatizing agents. Flavor and aroma agents may be selected from the group comprising essential oils and preparations thereof including distillations, solvent extractions, or cold expressions of chopped flowers, leaves, peel or pulped whole fruit comprising mixtures of alcohol, esters, aldehydes and lactones; essences including either diluted solutions of essential oils, or mixtures of synthetic chemicals blended to match the natural flavor of the fruit, e g strawberry, raspberry and black currant; artificial and natural flavors of brews and liquors, e.g.
• cognac, whisky, rum, gin, sherry, port, and wine tobacco, coffee, tea, cocoa, and mint; fruit juices including expelled juice from washed, scrubbed fruits such as lemon, orange, and lime; spear mint, pepper mint, wintergreen, cacoe/cocoa, vanilla, liquorice, menthol, eucalyptus, aniseeds, nuts, e.g. peanuts, coconuts, hazelnuts, chestnuts, walnuts, cola nuts; almonds, raisins; barks, e.g. cinnamon, roots, e.g. ginger, and mixtures thereof.
• nuts e.g. peanuts, coconuts, hazelnuts, chestnuts, walnuts, cola nuts
• almonds, raisins barks, e.g. cinnamon, roots, e.g. ginger, and mixtures thereof.
• the nicotine should be in gaseous or liquid aerosol form when inhaled in order to facilitate the absorption and uptake anywhere in the mouth or oral cavity and/or the upper respiratory tract and/or lungs.
• the nicotine may act as a substituted stimulant e.g. to obtain a rapid reduction of the urge to smoke or to use tobacco.
• the effect may be to provide a sense of smoking satisfaction without smoking.
• Another effect of the administered nicotine may be a reduction of the urge to smoke or use tobacco.
• the effect may also be a combination of reduction of said urge and providing a sense of smoking satisfaction without smoking.
• the amount of the nicotine should be sufficient to provide such an effect in a subject. This amount may, of course, vary from person to person.
• Containers from a shaped mass of fibers or filaments of polyethylene terephtalate covered with a copolyolefin sheath 100 000 pieces
• Plastic cartridges made of Barex ® 100 000 pieces
• the manufacturing phases were:
• the containers were added to a vacuum cone blender.
• the loading solution was added to a blender and the containers were mixed with the loading solution.
• a vacuum was applied and the temperature was increased to about 50°C in order to remove ethanol.
• the drying process was terminated by cooling the jacket of the blender.
• the nicotine-loaded containers were transferred to airtight bulk containers, which were evacuated and filled with nitrogen.
• the assembly of the nicotine-loaded containers into the plastic cartridges was performed in separated zones, involving feeding of the containers and cartridges from a first zone, and the subsequent assembly in a second zone. Sealing of the plastic cartridges was made by welding with Barex ® -coated aluminum foil. All zones were separately fed with nitrogen.
• a method for delivering nicotine to a subject comprises the steps of a) administering to a subject air loaded with nicotine by using an inhalation device containing the container comprising nicotine and b) allowing the nicotine to be released in the mouth oral cavity and/or the upper respiratory tract and/or the lungs and then being absorbed into the blood plasma of the subject.
• a method for obtaining reduction of the urge to smoke or use tobacco -containing material and/or for providing a sense of smoking satisfaction without smoking comprises the steps of: a) replacing at least partly the tobacco containing material with an inhaling devise comprising the container comprising nicotine, b) administering to a subject nicotine according with the help of the container comprising nicotine into the oral cavity and/or the upper respiratory tract and/or the lungs of the subject, and c) allowing the nicotine to be absorbed by the subject.
• the administration of nicotine takes place by the subject inhaling air loaded with nicotine i.e. the subject puffs on the inhaler comprising the container comprising nicotine as the air passes said container the nicotine is released from said container and the subject will thus receive air loaded with nicotine.
• the administration is essentially intended for the mouth/oral cavity and/or the upper respiratory tract and/or the lungs.
• Even further embodiments of the method for delivering nicotine to a subject may comprise the steps of combining the method of using the present inhaling device with at least one other method for obtaining reduction of the urge to smoke or use of tobacco.
• the container comprising nicotine may be used for obtaining a quick and/or sustained and/or complete reduction of the urge to smoke or use of tobacco and/or for providing a sense of smoking satisfaction without smoking as further discussed below.
• the fast relief provides the subject with a sense of rapid smoking satisfaction without smoking.
• a system for delivering nicotine to a subject comprises the container comprising nicotine according to the present invention and an inhalation device, and at least one other means for obtaining reduction of the urge to smoke.
• Another system according to the invention may also be a system for obtaining reduction of the urge to smoke or use of tobacco and/or for providing a sense of smoking satisfaction without smoking.
• a system comprises the container comprising nicotine according to the invention and at least one other means for obtaining reduction of the urge to smoke or use tobacco.
• Other means/methods may also be a concomitant or concurrent method selected from the group consisting of administration through nasal sprays, transdermal patches, lozenges, tablets and parenteral methods, subcutaneous methods, intravenous methods, rectal methods, vaginal methods and transmucosal methods; or use of tobacco.
• the at least one other method/method comprises administration of nicotine.
• the use of the container comprising nicotine according to the invention for obtaining a fast and/or sustained and/or complete reduction of the urge to smoke and use tobacco or for providing a sense of smoking without smoking as described above.
• the dose of the nicotine is chosen to give the subject an individual sensory perception and nicotine satisfaction.
• the use of the container comprising nicotine according to the invention may also be a sole use according to the invention or a combination with other means or methods known in the field of drug abuse.
• the present invention may be used in combination with other means as described above in the methods in the paragraphs above.
• the use may give a quick reduction of the urge to smoke or use tobacco.

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Cited By (16)

Citations (7)

• 2003
  • 2003-02-28 SE SE0300520A patent/SE0300520D0/xx unknown
• 2004
  • 2004-02-20 WO PCT/IB2004/000587 patent/WO2004076289A2/en active Application Filing
  • 2004-02-25 CL CL200400365A patent/CL2004000365A1/es unknown
  • 2004-02-27 AR ARP040100624A patent/AR043422A1/es not_active Application Discontinuation
  • 2004-02-27 TW TW093105136A patent/TW200427417A/zh unknown

Patent Citations (7)

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