Modified Release Antipsychotic Composition for Chronotherapeutic Alignment
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Solution Overview
Problem
Current pharmaceutical formulations for antipsychotic agents, such as paliperidone, have limitations in delivering optimal plasma levels synchronized with patients' physiological biorhythms, leading to inefficiencies in efficacy and safety, and do not adequately address the need for adaptive and versatile drug delivery patterns to improve patient compliance and sleep quality.
Innovation Solution
A modified release pharmaceutical composition comprising an immediate release formulation of a hypersomnia-inducing antipsychotic agent, like quetiapine, combined with a delayed release formulation of another antipsychotic agent, such as paliperidone, using a pH-dependent polymeric release controlling layer to coordinate the release timing with chronotherapeutic requirements, allowing for once-daily administration before bedtime.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If extended release formulation is used for paliperidone, then duration of action is improved, but plasma concentration profile cannot be synchronized with physiological biorhythms
Solution Approach 1:
The patent segments the drug delivery into two distinct formulations: immediate release and delayed release. The immediate release formulation delivers the antipsychotic agent quickly to achieve rapid therapeutic effect, while the delayed release formulation provides sustained release to extend duration of action. This segmentation allows the combination to satisfy both the need for rapid onset and extended duration while aligning with physiological biorhythms.
Solution Approach 2:
The patent changes the release rate parameter of the antipsychotic agent by combining two formulations with different release characteristics. The immediate release formulation provides a high initial concentration, while the delayed release formulation maintains therapeutic levels over an extended period. This parameter change enables synchronization with physiological biorhythms while extending duration of action.
2Reliability
If multiple dosing on daily basis is administered, then plasma concentration can be maintained, but patient compliance deteriorates
Solution Approach 1:
The patent merges the immediate release formulation and delayed release formulation into a single pharmaceutical composition that can be administered once daily. The immediate release component ensures rapid achievement of therapeutic plasma concentration, while the delayed release component maintains this concentration throughout the day. This combination allows once-daily dosing while maintaining reliable plasma concentration levels, thereby improving patient compliance.
3Ease of manufacture
If conventional formulation design is used, then manufacturing is simplified, but efficacy and safety are compromised due to variable factors
Solution Approach 1:
The patent uses a composite formulation consisting of immediate release and delayed release components. This composite structure allows the pharmaceutical composition to maintain therapeutic plasma concentrations more consistently by providing both rapid onset and sustained release. The composite formulation improves efficacy and safety consistency while remaining manufacturable using conventional pharmaceutical technologies.
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
This composition enhances bioavailability, improves sleep quality, reduces the need for additional sleeping pills, and maintains therapeutic effects by aligning plasma concentration profiles with patients' physiological rhythms, thereby improving treatment outcomes and compliance.
Implementation Method 1
using a pH-dependent polymeric release controlling layer to coordinate the release timing with chronotherapeutic requirements
Data Source
AI summary
The present invention is concerned with a modified release pharmaceutical composition comprising an effective amount of at least one antipsychotic agent so that the antipsychotic agent(s) are released in such a manner to better accord with physiological and chronotherapeutic requirements of patients.