Smoking Substitutes For Nasal Administration-I

What is this patent about?

'858 is related to the field of smoking cessation, specifically addressing the need for a socially acceptable and effective nicotine replacement therapy. The background acknowledges the difficulty smokers face when trying to quit due to nicotine dependence and the harmful effects of tobacco combustion products. Existing nicotine replacement methods, like chewing gum, are not suitable for all smokers, highlighting the need for alternative delivery systems.

The underlying idea behind '858 is to deliver nicotine directly to the nasal mucosa via an aqueous solution. This bypasses the harmful combustion products of smoking and offers a more socially acceptable alternative to traditional snuff. The key inventive insight is formulating a nicotine solution with a specific pH range (2-6) and viscosity (not less than 100 centipoise) that allows for effective nicotine absorption without causing intolerable local sensations or rapid absorption that leads to adverse effects.

The claims of '858 focus on a smoking substitute composition designed for nasal application. This composition consists of an aqueous solution of nicotine (or a physiologically acceptable salt), a nasally-acceptable thickening agent, and optionally, a buffer, emulsifying agent, preservative, flavoring agent, or antioxidant. The nicotine concentration is specified as 0.5 to 10% w/v, calculated as the free base, and the pH is maintained between 2 and 6.

In practice, the invention involves administering a small volume (0.05 to 0.5 ml) of the nicotine solution into the nasal cavity. The thickening agent ensures the solution adheres to the nasal mucosa, facilitating nicotine absorption into the bloodstream. The controlled pH is crucial; it ensures that nicotine is primarily in its salt form, which is absorbed more slowly than the free base, preventing rapid spikes in nicotine levels and minimizing unpleasant side effects.

The invention differentiates itself from prior art by addressing the social unacceptability of snuff and the limitations of other nicotine replacement therapies. Unlike snuff, the nicotine is delivered in a clean, aqueous solution. The controlled pH and viscosity are also key differentiators, allowing for a tolerable and effective nicotine delivery method that mimics the blood nicotine levels achieved through smoking, thus satisfying the smoker's craving without the harmful effects of burning tobacco. The use of unit-dose containers with a nostril-insertable neck is also highlighted as a convenient delivery mechanism.