Propellant-Free Aerosol Formulation for Stable Lung Deposition
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Solution Overview
Problem
Propellant-free aerosol formulations for inhalation struggle to maintain minimum particle size during inhalation, leading to suboptimal lung deposition due to droplet evaporation, as highly volatile aerosols decrease in diameter rapidly, failing to effectively target respiratory sites.
Innovation Solution
Incorporating inert, non-volatile excipients in propellant-free solution formulations, such as sodium chloride, magnesium sulfate, and sodium bicarbonate, to achieve a total non-volatile component concentration of ≥3% by weight, ensuring stable particle sizes ≥0.5 μm for optimal lung deposition.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Device complexity
If propellant-free aerosol formulations are used, then the formulation is simpler and safer, but the particle size decreases due to droplet evaporation
Solution Approach 1:
The patent changes the chemical composition parameters of the aerosol formulation by incorporating non-volatile excipients (such as salts, sugars, or polymers) at concentrations of 1-10% w/v. These excipients modify the physical properties of the droplets, specifically reducing their volatility and preventing evaporation during inhalation, thereby maintaining particle size within the therapeutic range (>0.5 μm) despite the propellant-free design.
2Speed
If highly volatile aerosols are used, then the aerosol disperses quickly, but the droplet diameter decreases significantly during inhalation
Solution Approach 1:
The patent introduces non-volatile excipients as intermediary substances that act within the aerosol droplets. These excipients serve as a mediating mechanism that reduces the volatility of the solvent system, thereby slowing down evaporation rates while preserving the quick dispersion characteristics needed for effective aerosol delivery to the lungs.
3Stability of the object's composition
If propellant-free formulations are used, then the formulation is more stable, but the particle size cannot be maintained above 0.5 μm
Solution Approach 1:
The patent creates a composite aerosol formulation by combining the active pharmaceutical ingredient with non-volatile excipients (such as sodium chloride, magnesium sulfate, or polymeric substances). This composite material approach leverages the stability-providing properties of the excipients while maintaining the propellant-free design, resulting in aerosols that both remain stable during storage and maintain particle size >0.5 μm during inhalation.
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 use of inert, non-volatile excipients stabilizes particle sizes, enhancing lung deposition by maintaining droplet sizes within the therapeutic range, thereby improving the efficacy of aerosolized medications for respiratory diseases.
Implementation Method 1
Particularly volatile aerosols have the property that their droplets evaporate during inhalation, and their diameter decreases significantly in the process.
Implementation Method 2
adding inert, non-volatile excipients to the aerosol solution formulations
Data Source
AI summary
The invention relates to inhalant propellant-free aerosol formulations containing at least one inert, non-volatile auxiliary substance for adjusting defined droplet sizes.