Inhalation Composition Blending for Aerodynamic Diameter Control
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Solution Overview
Problem
Current pharmaceutical compositions for inhalation therapy face challenges in tuning the aerodynamic diameter of particles for multiple active substances to ensure precise delivery to different regions of the respiratory tract, leading to interactions and instability, especially in combination therapies.
Innovation Solution
A method involving preblending each active ingredient with a specific excipient, followed by a main blending process with varying intensity, to achieve independent control over the aerodynamic diameter and reduce interactions, enhancing stability and homogeneity, using excipients with different d50 values and weight ratios.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If multiple active substances are blended together in a single process, then the manufacturing process is simple, but the aerodynamic diameter cannot be precisely controlled for each substance
Solution Approach 1:
The patent divides the blending process into separate stages: first blending each active substance with its designated excipient independently to control aerodynamic diameter, then combining the preblends in a second blending step. This segmentation allows precise control of particle characteristics for each active substance while maintaining overall manufacturability.
2Ease of manufacture
If active ingredients are blended with excipients in a single step, then the process is straightforward, but interactions and instability occur
Solution Approach 1:
The formulation process is segmented into distinct blending stages where each active ingredient is separately combined with its assigned excipient. This prevents unwanted interactions between different active substances while maintaining formulation stability, and the separate preblends are then combined in a controlled second step.
3Stability of the object's composition
If the same excipient is used for all active ingredients, then the formulation is homogeneous, but the aerodynamic properties cannot be optimized for each substance
Solution Approach 1:
The patent applies different excipients to different active ingredients based on their specific aerodynamic requirements. Each active substance is blended with an excipient selected to optimize its particular aerosolization characteristics, allowing local optimization of aerodynamic properties while maintaining overall formulation homogeneity through controlled blending.
4Reliability
If more active ingredient is used to ensure adequate delivery, then the therapeutic effect is sufficient, but the amount of active ingredient needed increases
Solution Approach 1:
The patent utilizes aerosolization technology to deliver active ingredients in respiratory-sized particles (0.5-10 μm) that can be efficiently transported to the lungs. By optimizing the aerodynamic diameter through excipient selection and blending parameters, the formulation achieves reliable therapeutic delivery with reduced active ingredient quantities.
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
This approach allows for precise adjustment of particle entry into the respiratory tract, reducing active ingredient amounts needed for the same effect, improving homogeneity and stability, and enhancing therapeutic efficacy.
Implementation Method 1
each different active ingredient is blended in a preblending procedure with a suitable excipient to which said active ingredient adheres
Implementation Method 2
a dose of the pharmaceutical composition is positioned in an aerosolization chamber, where it is aerosolized and, hence, dispersed into respirable particles by airflow supplied by the patient's inspiration effort
Implementation Method 3
medicament particles deposit in specific areas of the pulmonary system based upon the aerodynamic size of the particles and the flow rate of the air within which they are entrained
Data Source
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AI summary
The present invention relates to a pharmaceutical composition for inhalation. The invention is further directed to a method for setting the performance characteristics of such a pharmaceutical composition and the use of such a composition in the treatment of asthma, COPD, allergies, infectious diseases and diseases of the cardiovascular system.