Macrocyclic Liver-Specific Contrast Compositions for Safer CT Imaging
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Solution Overview
Problem
There is a need for new contrast agents for computed tomography (CT) imaging that exhibit properties similar to macrocyclic contrast agents for magnetic resonance imaging (MRI), particularly liver-specific agents that provide long-lasting contrast between lesion and liver tissue, as existing linear agents pose safety concerns and have limited uptake efficiency.
Innovation Solution
A pharmaceutical composition comprising both extracellular and liver-specific contrast agents, where the liver-specific agents have a macrocyclic structure to enhance stability and uptake, allowing simultaneous application in radiological imaging like MRI and CT.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Measurement precision
If linear gadolinium-based contrast agents are used for liver-specific imaging, then hepatocyte uptake and lesion-to-liver contrast are improved, but safety concerns arise due to gadolinium retention in brain tissues
Solution Approach 1:
The patent changes the molecular structure parameter from linear to macrocyclic chelate configuration, which fundamentally alters the stability and retention characteristics of gadolinium complexes while preserving their hepatocyte uptake capability and contrast enhancement properties
Solution Approach 2:
The patent creates a composite contrast agent system combining macrocyclic chelate structure with liver-specific targeting moieties, achieving both improved safety (reduced gadolinium retention) and maintained efficacy (hepatocyte uptake and lesion-to-liver contrast)
2Object-affected harmful factors
If macrocyclic liver-specific contrast agents are developed, then safety is improved by reducing gadolinium retention, but currently no such agents are commercially available limiting versatility
Solution Approach 1:
The patent segments the contrast agent development by creating distinct macrocyclic agents tailored for specific imaging phases (dynamic phase and hepatobiliary phase), enabling versatile clinical application across different imaging requirements
Solution Approach 2:
The patent develops macrocyclic contrast agents that can serve multiple functions: providing both dynamic phase imaging and hepatobiliary phase imaging capabilities, replacing the need for multiple different contrast agents
3Adaptability or versatility
If multiple contrast agent injections are administered, then imaging coverage is improved, but gadolinium accumulation in tissues increases
Solution Approach 1:
The patent enables continuous imaging coverage across different phases (dynamic and hepatobiliary) using a single macrocyclic contrast agent administration, eliminating the need for repeated injections and thereby preventing gadolinium accumulation
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 composition provides enhanced liver imaging capabilities in both MRI and CT, offering high relaxivity, stability, and efficient hepatocyte uptake, reducing the need for multiple injections and minimizing gadolinium retention in tissues.
Implementation Method 1
Gadolinium-based Contrast Agents (GBCAs) contain at least one paramagnetic ion of the rare earth metal Gadolinium (Gd3+), which possesses the highest number of unpaired electrons of any stable ion (seven), creating a high magnetic moment that is effective at enhancing proton relaxation
Implementation Method 2
Contrast agents alter the intrinsic tissue proton-relaxation T1 and T2 times resulting in an increase of the MRI contrast
Data Source
AI summary
The present invention relates to pharmaceutical compositions comprising contrast agents, to methods for preparing said pharmaceutical compositions and to their use for radiological imaging.