Segmented Phenylephrine Particles for Sustained Plasma Levels
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Solution Overview
Problem
Current phenylephrine formulations require frequent administration, leading to fluctuations in plasma levels and increased severity and frequency of side effects, necessitating the development of extended-release formulations that maintain therapeutic levels for longer durations.
Innovation Solution
Phenylephrine particles, either as resinate or coated with specific polymers, are designed to provide a peak plasma concentration within 0.1 to 16 hours and maintain levels above certain thresholds for at least 6 to 24 hours, potentially combined with immediate or sustained release of additional therapeutic agents like acetaminophen.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If immediate-release phenylephrine formulations are used, then rapid onset of action is achieved, but frequent administration is required leading to plasma level fluctuations and increased side effects
Solution Approach 1:
The phenylephrine dosage is segmented into multiple release phases using a multi-layered particle structure. Each layer contains phenylephrine in different physical forms (coated particles, resinate particles, immediate-release particles) that dissolve at different rates, creating a segmented release profile that maintains continuous therapeutic levels while preventing peak-trough fluctuations
Solution Approach 2:
The invention changes the physical and chemical parameters of phenylephrine delivery by using different coating materials (polymer coatings, resinate matrices) with varying dissolution rates. This parameter modification allows the same active ingredient to be released at different speeds from different particle types, achieving both rapid onset and extended duration
2Reliability
If frequent dosing is administered to maintain therapeutic levels, then adequate symptom relief is achieved, but patient compliance decreases and side effects increase
Solution Approach 1:
The multi-component particle formulation provides continuous phenylephrine release over an extended period (6-24 hours), eliminating the need for frequent dosing. The different release phases ensure that therapeutic levels are maintained continuously without gaps, providing reliable symptom relief while requiring only once-or twice-daily administration
Solution Approach 2:
The formulation dynamically adapts the release rate of phenylephrine to match the body's needs, with an initial rapid release phase for quick onset followed by a sustained release phase for prolonged effect. This dynamic release profile mimics the desired pharmacokinetic pattern while extending the dosing interval
3Duration of action of moving object
If extended-release formulations are developed, then dosing frequency is reduced, but formulation complexity increases
Solution Approach 1:
The invention merges multiple phenylephrine-containing particle types (coated particles, resinate particles, immediate-release particles) into a single combined formulation. This merging approach achieves extended-release functionality by combining simpler particle types rather than creating a single complex controlled-release mechanism, thereby reducing overall formulation complexity while maintaining extended duration of action
Data Source
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AI summary
Phenylephrine particles for solid, semi solid or liquid dosage forms are disclosed.