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(12) Patent Application Publication (10) Pub. No.: US 2014/0166027 A1 FUSZ Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2014/0166027 A1 FUSZ Et Al US 2014O166027A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2014/0166027 A1 FUSZ et al. (43) Pub. Date: Jun. 19, 2014 (54) ENHANCED DELIVERY OF NICOTINE, THC, (52) U.S. Cl. TOBACCO, CANNABIDIOL OR BASE CPC .................................... A24F 47/002 (2013.01) ALKALOD FROMAN ELECTRONIC USPC ........................................... 131/328; 131/359 CGARETTE OR OTHERVAPOR PRODUCING DEVICE THROUGH USE OF AN ABSORPTION CONDITIONING UNIT (57) ABSTRACT (71) Applicants: Richard C. FUISZ, Beverly Hills, CA A method for the administration of nicotine, THC, tobacco, (US); Joseph M. FUISZ, Surfside, FL cannabidiol or a base alkaloid includes administering an (US) absorption conditioning unit having at least two agents (72) Inventors: Richard C. FUISZ, Beverly Hills, CA selected from the group consisting of (a) a buffer agent, (b) a (US); Joseph M. FUISZ, Surfside, FL capturing agent, (c) a penetration agent, and (d) a thermal (US) agent, to the mammal, and then administering by inhalation a (21) Appl. No.: 13/715,028 bioactive agent selected from the group consisting of nico tine, THC, cannabidiol and a base alkaloid. The absorption (22) Filed: Dec. 14, 2012 conditioning unit may be in a dosage form not containing a drug. The absorption conditioning unit may create a pH in the Publication Classification oral cavity of 7.8-10 for a period often minutes or more after (51) Int. Cl. administration, the dosage form not containing an acid and A24F 47/00 (2006.01) not containing a drug. US 2014/0166027 A1 Jun. 19, 2014 ENHANCED DELIVERY OF NICOTINE, THC, of (a) a buffer agent, (b) a capturing agent, (c) a penetration TOBACCO, CANNABIDIOL OR BASE agent, and (d) a thermal agent, to the mammal, and then ALKALOD FROMAN ELECTRONIC administering by inhalation a bioactive agent selected from CGARETTE OR OTHERVAPOR the group consisting of nicotine, THC, cannabidiol and a base PRODUCING DEVICE THROUGH USE OF AN alkaloid. ABSORPTION CONDITIONING UNIT 0007. The present invention also relates A method for the administration of nicotine, THC, cannabidiol or a base alka BACKGROUND loid to a mammal, including administering an absorption conditioning unit including at least at least one material that 0001 Electronic vapor devices are increasingly popular creates a pH in the oral cavity of 7.8-10 for a period often with consumers. Such devices comprise electronic cigarettes, minutes or more after administration; and then administering electronic pipes, electronic hookahs, personal vaporizers and by inhalation a bioactive agent selected from the group con other inhalator embodiments, both electronic and mechani sisting of nicotine, THC, tobacco, cannabidiol and a base cal. alkaloid. 0002 UBS estimates that US e-cigarette sales will reach 0008. In one aspect of the present invention, an absorption S500 million by the end of 2012, representing 100% growth conditioning unit includes a dosage form including at least from the preceding year (See UBS Tobacco Analyst Nik two agents selected from the group consisting of (a) a buffer Modi's May 14, 2012 report entitled “Clearing the Smoke on agent, (b) a capturing agent, (c) a penetration agent, and (d) a E-Cigarettes, the entirety of which is incorporated herein by thermal agent, wherein said absorption conditioning unit (i) reference). Arguably, the most well-respected tobacco ana does not have an essentially acidic character, (ii) does not lyst, Bonnie Herzog of Wells Fargo, has gone so far as to contain a drug, (iii) does not contain THC or other Marijuana Suggest in discussing Lorillard: “We remain very encouraged derived active ingredient, and (iv) does not contain tobacco by blu Lorillard's e-cigarette brand and see huge upside except for trace amounts in flavor. potential given our belief ecigs could overtake traditional 0009. In another aspect of the present invention, an cigarettes in 10 years. See Wells Fargo Lorillard Equity absorption conditioning unit, includes a dosage form includ Research dated Oct. 24, 2012, the entirely of which is incor ing at least at least one material that creates a pH in the oral porated herein by reference. British American Tobacco Chief cavity of 7.8-10 for a period often minutes or more after Financial Officer Nicandro Durante stated in an interview administration, the dosage form not containing an acid and with the Financial Times in September 2012 that the size of not containing a drug. the market for tobacco alternatives like the e-cigarette could account for as much as 40% of BAT's revenues (which were DETAILED DESCRIPTION OF THE INVENTION £1.5bn in 2011) in 20 years’ time. “It will be sizeable in 20 years time ... it's going to grow, he said. 0010. The present invention relates to a method for the 0003. Despite this rapid sales growth, it is understood that administration of nicotine, THC, cannabidiol or a base alka electronic cigarettes fail to deliver a steeply peaked blood loid to a mammal, especially to a human, and to a prior plasma delivery of nicotine like the conventional cigarette administered absorption conditioning unit useful in Such a does. method. 0004 Still, there are good reasons for using the e-cigarette 0011 Nicotine inhalers are known art. For example, Pfizer as compared with cigarettes. The level of toxicants from the markets Nicotrol(R) in the United States. The Nicotrol(R) electronic cigarette is a small fraction as compared with a inhaler consists of a mouthpiece and a plastic cartridge deliv conventional cigarette. See, e.g., John H. Lauterbach, Murray ering 4 mg of nicotine from a porous plug containing 10 mg Laugesen, James D. Ross, “Suggested protocol forestimation nicotine. The cartridge is inserted into the mouthpiece prior to of harmful and potentially harmful constituents in main use. Nicotine is released when air is inhaled through the stream aerosals generated by electronic delivery systems inhaler. No heating element is used—the product relies on the (ENDS)”, SOT, San Francisco, Calif., Mar. 10-16, 2012 natural propensity of nicotine to Sublime at room tempera (http://cigtoxdoc.ehost-services 113.com/ ture. sot2012poster 1860aspresented.pdf) hereby incorporated by 0012 Despite the inhalation-route of administration by reference). the user of Nicotrol(R) abuccal route of absorption is described 0005. It is typically considered in the industry that elec in the Nicotrol(R) package insert despite the users inhalation tronic vapor device adoption by consumers would be of nicotine from the product (the entire package insert for enhanced by faster, improved nicotine delivery from an elec Nicotrol(R) is incorporated herein by reference as if fully set tronic vapor device. Thus, there is a need to improve nicotine forth). delivery from an electronic vapor device to its user. There is in 0013 The NicotrolR package insert describes its method addition need for delivery improvement (faster and more of action: “Most of the nicotine released from the efficient) in connection with the use of all vapor devices NICOTROL Inhaler is deposited in the mouth. Only a frac (mechanical and electronic), of any nicotine, tobacco, or tion of the dose released, less than 5%, reaches the lower marijuana actives. respiratory tract. An intensive inhalation regimen (80 deep inhalations over 20 minutes) releases on the average 4 mg of nicotine content of each cartridge of which about 2 mg is SUMMARY OF THE INVENTION systemically absorbed. Peak plasma concentrations are typi 0006. The present invention relates, inter alfa, to a method cally reached within 15 minutes of the end of inhalation . for the administration of nicotine, THC, tobacco, cannabidiol Absorption of nicotine through the buccal mucosa is rela or a base alkaloid to a mammal, e.g., a human. The method tively slow and the high and rapid rise followed by the decline includes administering an absorption conditioning unit, com in nicotine arterial plasma concentrations seen with cigarette prising at least two agents selected from the group consisting smoking are not achieved with the inhaler. After the use of the US 2014/0166027 A1 Jun. 19, 2014 single inhaler the arterial nicotine concentrations rise slowly 0022 Published studies on nicotine update from elec to an average of 6 ng/mL in contrast to those of a cigarette, tronic cigarettes similarly show a Substantially lower Cmax which increase rapidly and reach a mean Cmax of approxi and slower Tmax for nicotine delivery than a cigarette does mately 49 ng/mL within five minutes . Adlibitum use of (See e.g. Electronic Cigarettes: Effective Nicotine Delivery the NICOTROL Inhaler typically produces nicotine plasma After Acute Administration by Andrea Vansickel and Thomas levels of 6-8 ng/mL, corresponding to about /3 of those Eissenberg, Nicotine and Tobacco Research Adances Access achieved with cigarette Smoking.” published Feb. 6, 2012; Clinical Laboratory Assessment of 0014. The discrepancy between 4 mg of nicotine leaving the Abuse Liablity of an Electronic Cigarette' by Andrea the cartridge with just 2 mg being absorbed is noted. One Vansickel, Michael Weaver and Thomas Eissenberg submit Source of this discrepancy is that much of the nicotine is not ted 14 Oct. 2011 to the Society for the Study of Addiction, and buccally absorbed and is swallowed where nicotine is only available online; each of which is specifically incorporated poorly absorbed in the GI tract. herein by reference). 0015 Now, the typical cigarette contains less than 2 mg of 0023 Now, it has been suggested on electronic cigarette nicotine (http://www.bigsixSmokes.com/Camel.shtml), yet forums (www.e-cigarette-forum.com) to enhance nicotine delivers a far higher peak systemic nicotine plasma concen delivery by chewing a TUMS(R) antacid by well know e-ciga tration (Cmax), far quicker (Tmax), than NicotrolR (see rette blogger “Tropical Bob' but he states that this method http://pharmrev.aspetournals.org/content/57/1/79/T1...ex does not work (“I concur that e-liquid is NOT alkaline pansion.html which is incorporated by reference).
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