Controlled Absorption Drug Particulates for Extended Release
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Solution Overview
Problem
Current oral drug formulations, particularly for water-soluble drugs like naproxen, are ineffective for more than a few hours due to rapid absorption and short half-life, necessitating frequent dosing and limiting their duration of action.
Innovation Solution
A controlled absorption pharmaceutical formulation comprising a core of pharmaceutically active substance interacting with drug binding polymers, coated with a membrane-forming polymer, which slows the release of the drug, extending its delivery beyond a single day.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If immediate release formulation is used, then rapid absorption and onset of action are achieved, but duration of action is limited to a few hours requiring frequent dosing
Solution Approach 1:
The formulation is segmented into multiple particle sizes (fine particles 1-50 μm, intermediate particles 50-200 μm, coarse particles 200-500 μm) with different release characteristics. Fine particles provide rapid initial release for quick onset, while coarse particles provide sustained release for extended duration, resolving the contradiction between fast absorption and long duration of action.
Solution Approach 2:
The patent changes physical parameters of the formulation including particle size distribution, polymer composition ratios, and coating thickness to control drug release kinetics. By adjusting these parameters, the formulation achieves both rapid initial release (15-30% in 0.5 hours) and sustained release (≥65% in 4 hours), eliminating the need for frequent dosing while maintaining therapeutic levels.
2Duration of action of moving object
If controlled release formulation with polymer coating is used, then duration of action is extended, but manufacturing complexity increases
Solution Approach 1:
Different regions of the particle population have different properties: fine particles provide rapid release for quick onset, intermediate particles provide moderate release, and coarse particles provide sustained release. This local differentiation within the formulation allows extended duration of action while using simple coating processes applied to each particle size fraction separately.
Solution Approach 2:
The formulation uses composite polymer systems combining enteric coatings (e.g., Eudragit L100, EC T20) with controlled-release polymers (e.g., HPMC, ethylcellulose). This composite approach enables both extended duration of action and simplified manufacturing by using commercially available polymer materials with known processing characteristics.
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 achieves a sustained release profile, with 15-30% drug release in 0.5 hours, 25-60% in 1 hour, and not less than 65% in 4 hours, effectively maintaining therapeutic levels for an extended period.
Implementation Method 1
A controlled absorption pharmaceutical formulation comprising a core of pharmaceutically active substance interacting with drug binding polymers, coated with a membrane-forming polymer, which slows the release of the drug
Data Source
AI summary
The present disclosure provides a once-daily water-soluble pharmaceutically active formulation for oral administration. In certain embodiments, the composition comprises a watersoluble pharmaceutically active organic compound incorporated into a small particulate, each particulate having a core of the water-soluble pharmaceutically active organic compound or an acceptable salt thereof in reversible association with a pharmaceutically acceptable drug-binding polymer. The core of the composition being surrounded by an insoluble water permeable membrane that is capable of delaying the dissolution of the pharmaceutically active compound therewithin and providing for extended release of the pharmaceutically active compound. In some embodiments, the formulation of the invention are designed to extend release of the pharmaceutically active organic compound liar about 3 hours to about 8 hours, thereby enabling preparation of an extended release formulation for any pharmaceutically active compound with a half-life of from about 16 hours to about 21 hours.