Segmented Oral Dosage Form with Barrier Layer for Rapid Onset
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Solution Overview
Problem
Existing controlled release drug formulations often exhibit significant lag times in pharmacokinetic profiles, particularly when administered in a fed state, and may require longer times to achieve maximum plasma concentration (Cmax) compared to immediate release formulations.
Innovation Solution
The development of dosage forms that include a drug composition with a barrier layer and a drug layer, designed to provide a controlled release of pharmacologically active agents, reducing lag times and achieving a rapid onset of action followed by sustained release.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If controlled release formulation is used, then duration of sustained plasma levels is improved, but time to achieve Cmax is worsened
Solution Approach 1:
The dosage form is segmented into multiple functional layers: an immediate release drug composition core, a barrier layer, and a controlled release drug layer. This segmentation allows the immediate release portion to quickly achieve Cmax while the controlled release portion maintains sustained plasma levels, resolving the contradiction between rapid onset and prolonged duration.
Solution Approach 2:
The immediate release drug composition is nested within the barrier layer, which is in turn nested within the outer controlled release drug layer. This nested structure enables both immediate release characteristics (from the inner core) and controlled release characteristics (from the outer layer) to coexist, achieving rapid Cmax while maintaining sustained plasma levels.
2Duration of action of moving object
If controlled release formulation is used, then duration of sustained plasma levels is improved, but lag time in fed state is worsened
Solution Approach 1:
The dosage form is divided into an immediate release component (inner drug composition) and a controlled release component (outer drug layer). The immediate release segment rapidly dissolves even in fed state, reducing lag time, while the controlled release segment provides sustained plasma levels over 10-12 hours, resolving the contradiction between rapid onset and prolonged duration.
Solution Approach 2:
The immediate release drug composition is prepared in advance within the core, ready for rapid dissolution upon administration. This preliminary preparation ensures that even when administered with food, the drug quickly begins to dissolve and achieve Cmax within 2 hours, reducing the lag time that would otherwise occur with conventional controlled release formulations.
Data Source
AI summary
The present disclosure provides dosage forms designed to deliver active pharmaceutical ingredients (APIs) in a controlled release manner. For instance, the present disclosure includes dosage forms with adequate time of onset of action and reduced lag times in the fed state. Such dosage forms find use in a variety of conditions where a rapid onset of action is desired followed by an extended release phase for the active agent, for example in the treatment of ADHD, pain or anxiety. In some cases, the dosage form includes a drug composition including a pharmacologically active agent, a barrier layer covering at least a portion of the drug composition, and a drug layer covering at least a portion of the barrier layer, wherein the drug layer includes the pharmacologically active agent. Related methods of making and administering the disclosed dosage forms are also provided.