Eutectic Mixture for Pulmonary Drug Delivery
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Solution Overview
Problem
Current pharmaceutical compositions for treating respiratory diseases, particularly chronic obstructive pulmonary disease (COPD) and asthma, face challenges in delivering two pharmacologically active ingredients to the lung effectively, including issues with particle stability, agglomeration, and inconsistent delivery due to variations in surface properties and processing methods, which affect the efficacy and onset time of the drugs.
Innovation Solution
A pharmaceutical composition comprising a eutectic mixture of a long-acting β2 agonist and a long-acting muscarinic antagonist, formed through methods such as dissolving and removing solvents, forming melts, or mechanical comminution, to create particles with a lower melting point and increased solubility, enhancing delivery and interaction with lung surfactants.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If two pharmacologically active ingredients are delivered as separate solid crystalline particles, then particle stability is maintained, but dissolution rate and onset time are slow
Solution Approach 1:
The patent changes the physical state parameter of the drug particles from stable crystalline solid to less stable amorphous or liquid-like eutectic form. This parameter change increases surface energy and molecular mobility, thereby dramatically increasing dissolution rate and onset time while accepting reduced particle stability as a trade-off
Solution Approach 2:
The patent utilizes phase transition by forming a eutectic composition that melts at a lower temperature than the individual components. The eutectic mixture transitions from solid to liquid-like state at physiological temperature, enabling rapid dissolution and absorption while maintaining physical integrity during storage
2Reliability
If two drugs are co-delivered to the lung, then synergistic therapeutic effects are achieved, but particle agglomeration and inconsistent delivery occur
Solution Approach 1:
The patent merges two separate drug particles into a single integrated eutectic particle system. The two pharmacologically active ingredients are combined at the molecular level in a eutectic composition, ensuring they remain together as a unified particle during inhalation and delivery, thereby preventing agglomeration and ensuring consistent co-delivery to the lung
Solution Approach 2:
The patent creates a composite particle system where two different pharmacologically active ingredients form a eutectic composition with specific physical and chemical properties. This composite structure ensures compatible surface properties and prevents differential behavior during processing and delivery, eliminating agglomeration issues
3Quantity of substance
If eutectic composition is used to increase solubility, then dissolution rate improves, but manufacturing complexity increases
Solution Approach 1:
The patent changes the compositional parameter by forming a eutectic mixture with specific ratios of two pharmacologically active ingredients. This parameter change results in a composition with lower melting point and higher solubility than the individual components, achieving improved dissolution rate through controlled formulation design
Solution Approach 2:
The patent utilizes established eutectic formation principles from pharmaceutical science to create the composition. By applying known methods for forming eutectic mixtures (such as co-milling or solvent evaporation), the manufacturing process leverages existing technical knowledge rather than requiring entirely new manufacturing approaches
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 eutectic composition improves the delivery and efficacy of both active ingredients to the lung, increasing their solubility and dissolution rate, leading to faster onset of action and enhanced therapeutic effects by maximizing synergistic interactions with lung tissue.
Implementation Method 1
The unique property of a eutectic is that it has a lower melting temperature than that of either pure compound
Implementation Method 2
When the eutectic composition is exposed to the gastrointestinal fluids, the soluble carrier dissolves rapidly, leaving the insoluble drug in an extremely fine state of subdivision
Data Source
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AI summary
This invention provides a pharmaceutical composition comprising a eutectic composition of two pharmacologically active ingredients for delivery to the lung by inhalation. This invention also provides a pharmaceutical composition comprising a eutectic composition of two pharmacologically active ingredients for the treatment of respiratory disease.