Pulsed Release Phenylephrine Dosage Forms for Extended Symptom Relief
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Solution Overview
Problem
Current phenylephrine dosage forms require frequent administration due to high first-pass metabolism and short half-life, making it inconvenient for consumers and challenging to combine with other drug actives in multi-symptom relief products, necessitating a longer-acting formulation for effective cold and flu symptom relief.
Innovation Solution
A multi-particle oral dosage form combining immediate release and pH-sensitive delayed release particles of phenylephrine, designed to provide controlled pulsed doses, with the delayed release particles coated to release in the distal small intestine, optimizing unconjugated phenylephrine levels and duration of action.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If immediate release phenylephrine dosage forms are used, then rapid onset of action is achieved, but frequent dosing (every 4 hours) is required due to short half-life and high first pass metabolism
Solution Approach 1:
The dosage form is segmented into multiple particle types with different release characteristics: immediate release particles for rapid onset and delayed release particles with pH-sensitive coatings for sustained effect. This segmentation allows the single dose to provide both rapid initial relief and extended duration of action, eliminating the need for frequent re-dosing.
Solution Approach 2:
The invention changes the release parameter of phenylephrine by using pH-sensitive coatings on delayed release particles. These coatings remain intact in the acidic stomach environment but dissolve at the higher pH of the small intestine, controlling the release timing and extending the duration of therapeutic effect.
2Reliability
If frequent dosing is required, then therapeutic effectiveness is maintained, but consumer convenience and compliance deteriorate
Solution Approach 1:
The multi-particle dosage form provides continuous therapeutic action by combining immediate release particles that act quickly with delayed release particles that continue releasing phenylephrine over several hours. This continuous action maintains therapeutic effectiveness while allowing single daily dosing, significantly improving consumer convenience and compliance.
3Duration of action of moving object
If extended release mechanisms are used, then dosing interval is prolonged, but low levels of unconjugated phenylephrine are present during extended release phase due to rapid first pass metabolism
Solution Approach 1:
The pH-sensitive coating acts as an intermediary that protects phenylephrine from premature release and first-pass metabolism in the stomach. By delaying release until the small intestine, the coating ensures that phenylephrine is released when absorption is more efficient, maintaining adequate unconjugated phenylephrine levels throughout the extended dosing interval.
4Adaptability or versatility
If multiple dosage forms are combined for multi-symptom relief, then comprehensive symptom coverage is achieved, but dosing complexity increases
Solution Approach 1:
The invention merges multiple functional components into a single dosage form: immediate release particles for rapid effect, delayed release particles for extended effect, and potentially multiple active ingredients for multi-symptom relief. This consolidation allows comprehensive symptom coverage while simplifying the dosing regimen to a single daily dose, reducing dosing complexity.
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 formulation extends the duration of therapeutic phenylephrine levels, allowing for effective relief over 6 to 12 hours, meeting or exceeding the bioavailability and bioequivalence of multiple immediate release doses, thus providing more convenient and sustained symptom relief.
Implementation Method 1
a plurality of delayed release particles comprising a coating comprising phenylephrine or salt thereof and a pH sensitive coating comprising a polymer
Data Source
AI summary
A multi-particle dosage form that can deliver phenylephrine in controlled pulsed doses. The dosage form can contain an immediate release form that can contain phenylephrine or a salt thereof and a plurality of delayed release particles with a coating that can contain phenylephrine or salt thereof and a pH sensitive coating.