Thursday, May 29, 2014

Oh, patents! Oral transmucosal NRTs

Copyright © Françoise Herrmann


Ok, May 31, 2014  UN World No Smoking Day,  minus 36 hours! Or, what you really want, without the pain of withdrawal…!

Nicotine replacement therapies (NRTs) are recommended by the NIH (National Institutes of Health), the ACS (American Cancer Society) and the ALS (American Lung Association) as first line approaches to smoking cessation. NRTs  include patches, lozenges, sprays and gum. (See a previous post on .. for Transdermal nicotine patches). Research indicates that NRTs in association with counseling double your chances or quitting (Pierce et. al, 2012)

 If your Doctor skipped town, or has already given up on you… then you can always go to Walgreens to pick up some nicotine gum or lozenges, marketed under the brand name Nicorette®, one of the first FDA-approved NRTs.
Nicotine gum marketed as Nicorette®  uses a “park and chew” technology. Using the “park and chew” technology, a consumer “bites” on the gum to release nicotine, and then “parks” the gum inside their cheek, and then ”bites” again when more nicotine is needed. This prevents excess nicotine release, and the ensuing undesirable side effects such as dizziness, nausea or stomach problems.

The original (and expired) Nicorette® nicotine replacement patents from the 1970s are US3877468 titled Chewable tobacco substitute composition, disclosing Chewable smoking substitute composition comprises at least about 40 percent by weight of a gum base and a tobacco alkaloid dispersed in said gum base in an amount sufficient to provide smoking satisfaction.; US3901248 titled Chewable smoking substitute composition and US3845217 titled Buffered smoking substitute compositions. More recent Nicorette® patents include the nicotine lozenge patent  US2011110880 titled Nicotine Lozenge compositions, and  a flavoring patent,  US2006275344 titled Flavoring of drug-containing chewing gum.

Incidentally, nicotine gum is  a very patented product! The EPO returned 184 patents for a search on “nicotine gum”. There are in fact many different sorts of nicotine gums, that is, different formulations of the gum base and of the non-toxic active nicotine ingredient; different oral transmucosal delivery systems or release technologies for the nicotine in the gum; and different flavors that may be added to the gum to make it palatable or compatible with release of the active ingredient.

Here is an additional short list of the nicotine gum patents:
  • US2014099269 Chewing gum having sustained release of nicotine
  • US2013323184 Method of providing fast relief to a user of nicotine chewing gum
  • US2012039981 Coated nicotine-containing chewing gum, manufacture and use thereof
  • WO2013059592 Excipients for nicotine containing therapeutic compositions
  • WO2014091631 Method of releasing nicotine from chewing gum
  • US6344222B1 Nicotine, hydrophilic and hydrophobic polymer, buffer time-release agents (to improve release rates of nicotine)
  • US8658200 Flavoring of drug-containing chewing-gums
Finally, here is a cessation quote to ponder:
“Nicotine is an addictive poisonous alkaloid C5H4NC4H7NCH3, derived from the tobacco plant. Nicotine is also used as an insecticide. Approximately 40 milligrams* of nicotine is able to kill an adult (Merck Index).” (Extracted from US2006275344)
 *40 mg = 1 US teaspoon 
John P. Pierce, Sharon E. Cummins, Martha M. White, Aimee Humphrey, and Karen Messer (2012)
Quitlines and nicotine replacement for smoking cessation: Do we need to change policy? Annual Review of Public Health, 33:341-356.

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