Omecamtiv Mecarbil Matrix Tablet for Stable Plasma Release
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Solution Overview
Problem
Current omecamtiv mecarbil formulations exhibit peak-to-trough ratios that are too great for safe and effective chronic or preventative use, leading to potential side effects and variability in plasma levels.
Innovation Solution
A pharmaceutical formulation comprising omecamtiv mecarbil, a control release agent, a pH modifying agent, a filler, and a lubricant, which is prepared by blending, lubricating, and compressing to create a modified release matrix tablet that controls the release of omecamtiv mecarbil through a gel layer, minimizing pH-dependent release and reducing plasma concentration fluctuations.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If standard release formulations are used, then plasma levels of omecamtiv mecarbil can be delivered, but peak to trough ratios are too great for safe and effective chronic use
Solution Approach 1:
The patent applies dynamics by transitioning from a static standard release formulation to a dynamic controlled-release system that adapts release rates. The formulation uses multiple polymer matrices with different release characteristics to dynamically adjust drug release, maintaining plasma levels within a therapeutic window suitable for chronic administration.
Solution Approach 2:
The patent changes the release rate parameter by incorporating controlled-release mechanisms. By modifying the formulation to include polymers with specific release rates and using enteric coating technologies, the patent transforms the drug delivery parameters to achieve sustained plasma concentrations without excessive peak-to-trough variations.
2Productivity
If standard release formulations are used, then omecamtiv mecarbil can be delivered, but plasma levels fluctuate too much for preventative setting
Solution Approach 1:
The patent segments the drug delivery system into multiple components with different release rates. By dividing the formulation into immediate-release and sustained-release portions, or using multiple polymer layers with staggered release profiles, the system maintains consistent plasma levels throughout the dosing interval, preventing both peaks and troughs.
Solution Approach 2:
The patent ensures continuous drug delivery by designing a formulation that releases omecamtiv mecarbil at a steady rate over an extended period. This continuous action eliminates the interruption between doses that causes trough levels, maintaining therapeutic presence throughout the dosing interval for effective prevention.
3Duration of action of stationary object
If extended release formulations are used, then release duration is increased, but peak to trough ratios remain too great
Solution Approach 1:
The patent uses composite materials by combining multiple polymer matrices with different release characteristics. The composite formulation includes polymers that provide both initial burst release and sustained release phases, or polymers with different degradation rates, creating a multi-phase release profile that extends duration while controlling peak-to-trough ratios.
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 modified release matrix tablets provide a more stable and controlled release of omecamtiv mecarbil, reducing plasma peak-trough ratios, minimizing side effects, and improving patient safety and efficacy by maintaining consistent plasma levels.
Implementation Method 1
controls the release of omecamtiv mecarbil through a gel layer
Data Source
AI summary
Provided are certain pharmaceutical formulations of omecamtiv mecarbil and methods for their preparation and use.