Aerosol Dissolution Testing with Cascade Impactor and Membrane

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Solution Overview

Problem

Current systems for testing the dissolution and release kinetics of aerosol formulations for inhalation are inadequate in simulating the lung environment, particularly for poorly soluble particles, as they do not allow for the separation of fine particles and fail to accurately measure the release behavior in an air-liquid interface, leading to inaccurate results and complex analytical processes.

Innovation Solution

A device comprising a commercially available inhaler and an Andersen cascade impactor to separate particles by size, followed by a membrane that immobilizes the fine fraction, which is then subjected to an air-liquid model system for continuous monitoring of active substance concentration, simulating the lung environment and reducing analytical effort.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If particles are submerged in release medium using current dissolution test systems, then dissolution testing can be performed, but the particles aggregate into larger structures forming diffusion barriers that dramatically slow down the apparent release rate

Engineering Contradiction:
Improverelease behavior measurementVSAvoidapparent release rate
Core Design Contradiction:
Measurement precisionVSReliability

Solution Approach 1:

The patent introduces a porous membrane as an intermediary carrier that holds particles in a dispersed state during dissolution testing. The membrane prevents direct contact between particles and release medium that would cause aggregation, while still allowing dissolution to occur. This mediator maintains the particles in their original dispersed configuration, enabling accurate measurement of release behavior without the formation of diffusion barriers.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Ease of operation

If total particle population is tested without separation, then testing is simpler, but the therapeutically ineffective coarse fraction masks the release behavior of the therapeutically effective fine fraction

Engineering Contradiction:
Improvetesting simplicityVSAvoidfine fraction release behavior
Core Design Contradiction:
Ease of operationVSMeasurement precision

Solution Approach 1:

The patent applies segmentation by separating the particle population into different size fractions using a cascade impactor before dissolution testing. The fine fraction (therapeutically effective) is separated from the coarse fraction (therapeutically ineffective) based on aerodynamic diameter. This segmentation allows the release behavior of the fine fraction to be measured independently without being masked by the coarse fraction, while maintaining operational feasibility through standardized separation equipment.

Inventive Principle:
Principle #1Segmentation

3Measurement precision

If complex analytical methods like HPLC are used to determine active ingredient concentration, then accurate measurement is achieved, but the analytical process becomes time-consuming and complex

Engineering Contradiction:
Improveactive ingredient concentrationVSAvoidanalytical process
Core Design Contradiction:
Measurement precisionVSDevice complexity

Solution Approach 1:

The patent replaces complex mechanical-analytical methods (HPLC) with optical detection methods. A photodetector measures the optical properties (absorbance, transmittance, or fluorescence) of the release medium to determine active ingredient concentration. This substitution maintains measurement precision while dramatically simplifying the analytical process, reducing both device complexity and analysis time.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

4Adaptability or versatility

If aqueous solution is used as release medium to simulate physiological environment, then physiological simulation is achieved, but non-water-soluble particles aggregate rapidly forming additional diffusion barriers

Engineering Contradiction:
Improvephysiological environment simulationVSAvoidrelease behavior
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The porous membrane acts as an intermediary that enables the use of aqueous release medium to simulate physiological conditions while preventing the aggregation problem. The membrane holds particles in a dispersed state, allowing aqueous medium to penetrate and dissolve the active ingredient without causing particle aggregation. This resolves the contradiction by decoupling the physiological simulation function from the aggregation problem.

Inventive Principle:
Principle #24Intermediary (Mediator)

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

Enables the accurate determination of the dissolution rate and release kinetics of aerosol formulations, specifically targeting the fine particle fraction, with continuous data acquisition and reduced analytical complexity, effectively simulating the lung environment and providing insights into the therapeutic effectiveness of aerosol formulations.

Implementation Method 1

an Andersen cascade impactor to separate particles by size

Methodology Applied
Scientific EffectImpaction: Impact Force

Implementation Method 2

a membrane that immobilizes the fine fraction

Methodology Applied
Scientific EffectAdsorption: Adsorption

Implementation Method 3

subjected to an air-liquid model system for continuous monitoring of active substance concentration

Methodology Applied
Scientific EffectDiffusion: Diffusion

Data Source

PatentEP2288898B1Device and method for determining the properties of aerosol formulations
Publication Date: 2015.08.12 BOEHRINGER INGELHEIM INT GMBH
  • EP2288898B1 patent drawingFigure 1
  • EP2288898B1 patent drawingFigure 2
  • EP2288898B1 patent drawingFigure 3

AI summary

A device (100) for determining the solution rate and release kinetics of aerosol formulations comprises an inhaler (2) connected to a cascade impacter (3), wherein a membrane (6) is disposed on a filter plate of the cascade impacter (2), and an air-liquid model system with a device for collecting measured data.