Bismuth Coordination Polymers for Sustained Drug Release
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Solution Overview
Problem
Pharmaceutical agents often exhibit unfavorable pharmacokinetic properties when administered in vivo, leading to suboptimal therapeutic efficacy and safety issues, such as variable absorption, toxicity, and short therapeutic windows, which can limit their effectiveness in treating conditions like Parkinson's disease, hypothyroidism, ulcerative colitis, and cancer.
Innovation Solution
The development of bismuth-containing compounds where a biologically active agent is coordinated with bismuth, either alone or with a second metal, to form a compound that modulates pharmacokinetic properties, including improved bioavailability, extended release, and reduced variability, by forming coordination polymers that act as a depot in the gastrointestinal tract for gradual drug release.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If a biologically active agent is administered orally, then the drug can be delivered to the patient, but unfavorable pharmacokinetic properties such as variable absorption, short therapeutic windows, and toxicity occur
Solution Approach 1:
The patent forms coordination polymers comprising bismuth and a biologically active agent, creating a composite material that combines the therapeutic properties of the drug with the pharmacokinetic benefits of bismuth coordination. This composite structure provides sustained release and improved absorption reliability while reducing variability between subjects.
2Reliability
If the drug concentration is increased to improve therapeutic efficacy, then the treatment effectiveness increases, but dangerous concentration surges and toxicity occur
Solution Approach 1:
The coordination polymer provides periodic, sustained release of the biologically active agent at controlled rates, maintaining therapeutic concentrations within the therapeutic window over extended periods. This prevents both subtherapeutic levels and dangerous concentration surges, thereby improving efficacy while reducing toxicity.
3Speed
If the drug is released quickly to achieve rapid therapeutic effect, then the onset of action is fast, but the duration of action is short and concentration surges occur
Solution Approach 1:
The coordination polymer exhibits dynamic release properties, initially providing rapid onset of action as the polymer begins to dissociate, then transitioning to sustained, controlled release that maintains therapeutic levels over extended periods. This dynamic behavior simultaneously achieves fast onset and prolonged duration without dangerous surges.
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 bismuth-containing compounds enhance the plasma levels and therapeutic windows of drugs like levodopa, triiodothyronine, mesalamine, and dichloroacetate, providing sustained release and improved bioavailability, thereby addressing the limitations of existing pharmacokinetic properties and enhancing treatment efficacy and safety.
Implementation Method 1
a biologically active agent coordinated to the bismuth. The biologically active agent includes at least one heteroatom configured for coordination with the bismuth
Implementation Method 2
forming coordination polymers that act as a depot in the gastrointestinal tract for gradual drug release
Data Source
AI summary
Bismuth-containing compounds include bismuth and a biologically active agent coordinated to the bismuth. The biologically active agent includes at least one heteroatom configured for coordination with the bismuth. Coordination polymers include a polymer matrix that contains a bismuth-containing compound. Methods for modulating a pharmacokinetic property of a biologically active agent include coordinating the biologically active agent to bismuth to form a bismuth-containing compound, and administering the bismuth-containing compound orally to a patient. Methods for treating Parkinson's disease, methods for treating hypothyroidism, methods for treating ulcerative colitis, and methods for treating cancer each include administering a bismuth-containing compound to a patient.