Inhalable Nicotine Dry Powder Formulation for Smoking Cessation

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Solution Overview

Problem

There is a need for improved nicotine formulations suitable for inhalation, particularly dry powder formulations that effectively mimic the effects of smoking to aid in smoking cessation by gradually reducing nicotine cravings.

Innovation Solution

A dry powder nicotine formulation comprising nicotine, at least one sugar, and at least one amino acid, optionally including menthol or mint, with controlled particle sizes to ensure effective inhalation and absorption, reducing the risk of secondhand smoke and irritation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Object-affected harmful factors

If nicotine is delivered via traditional smoking, then nicotine absorption is achieved, but harmful factors (secondhand smoke, irritation, disease) are generated

Engineering Contradiction:

Improvesecondhand smoke and irritationVSAvoidnicotine delivery effectiveness

Core Design Contradiction:

Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent changes the physical and chemical parameters of nicotine delivery by using dry powder formulations with specific particle size distributions (MMAD 1-5 micrometers), controlled moisture content (0.1-10%), and specific excipient compositions. These parameter changes enable effective nicotine absorption through inhalation while eliminating combustion products and secondhand smoke, thus resolving the contradiction between effective nicotine delivery and harmful factor generation

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent employs composite material formulations consisting of nicotine combined with specific excipients including sugars (lactose, sucrose), amino acids (glycine, leucine), and phospholipids. These composite formulations improve nicotine delivery effectiveness while the non-combustible nature of the composite materials eliminates harmful combustion byproducts and secondhand smoke, resolving the technical contradiction

Inventive Principle:

Principle #40Composite materials

2Quantity of substance

If nicotine concentration is increased to reduce cravings, then addiction relief is improved, but irritation and harmful effects increase

Engineering Contradiction:

Improvenicotine concentrationVSAvoidirritation

Core Design Contradiction:

Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent controls nicotine concentration within specific ranges (0.1-10% w/w) and combines it with controlled particle size parameters (MMAD 1-5 micrometers) and moisture content (0.1-10%). These parameter optimizations ensure adequate nicotine delivery for craving relief while minimizing irritation through proper aerosolization and reduced contact time with airway tissues

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent introduces excipients as intermediary substances that modulate nicotine's effects. Sugars, amino acids, and phospholipids act as mediators that facilitate controlled nicotine release and reduce direct irritation to airway tissues, allowing effective nicotine concentration delivery while minimizing harmful irritation effects

Inventive Principle:

Principle #24Intermediary (Mediator)

3Productivity

If particle size is reduced to improve absorption, then nicotine uptake is enhanced, but manufacturing precision requirements increase

Engineering Contradiction:

Improvenicotine absorption efficiencyVSAvoidparticle size control

Core Design Contradiction:

ProductivityVSManufacturing precision

Solution Approach 1:

The patent specifies a target particle size parameter (mass median aerodynamic diameter of 1-5 micrometers) that balances absorption efficiency with manufacturability. This parameter range is optimized to ensure adequate lung deposition while remaining achievable through conventional pharmaceutical manufacturing techniques such as spray drying and micronization, resolving the contradiction between absorption efficiency and manufacturing precision

Inventive Principle:

Principle #35Parameter changes

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The formulation provides a controlled delivery of nicotine, effectively reducing cravings and minimizing irritation, while preventing nicotine from being exhaled into the environment, thus aiding in smoking cessation.

Implementation Method 1

The absorption of nicotine into the smoker's blood results in nicotine reaching various receptors in the nervous system of the smoker

Methodology Applied

Scientific EffectInhalation absorption: Absorption (physical)

Implementation Method 2

Menthol is a known and widely used topical analgesic, decongestant, and cough suppressant

Methodology Applied

Scientific EffectTopical analgesic effect:

Data Source

PatentUS10660883B2Inhalable nicotine formulations, and methods of making and using thereof

Publication Date: 2020.05.26 PHILIP MORRIS PRODUCTS SA

AI summary

The present invention provides dry powder formulations comprising nicotine, methods of using the same, and methods for making the same. The dry powder formulations may further comprise excipients, therapeutic agents, and flavor components. The dry powder formulations may be manufactured by dry processes and wet processes.