Controlled Release Oral Composition for Schizophrenia Treatment
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current pharmaceutical compositions for treating CNS diseases like schizophrenia require daily administration, which can be burdensome for patients, and there is a need for a composition that can maintain therapeutic blood concentrations for a longer period with less frequent dosing.
Innovation Solution
A controlled release oral pharmaceutical composition containing a salt of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one, specifically a fumaric acid salt, along with additives like fumaric acid and cellulose-based water-soluble polymers, which allows for sustained release of the active ingredient over a period of 5 to 30 hours.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If a high dose of active ingredient is administered to enable less frequent dosing, then the duration of therapeutic effect is improved, but excessive release after administration occurs causing harmful effects
Solution Approach 1:
The active ingredient is divided into multiple release stages through the layered tablet structure. The immediate-release layer provides initial therapeutic effect, while the controlled-release layer gradually releases the remaining drug over extended periods, preventing excessive single-dose release while maintaining duration of action.
Solution Approach 2:
The invention changes the release rate parameter of the active ingredient by using different excipient combinations in each layer. The immediate-release layer uses excipients that allow rapid dissolution, while the controlled-release layer uses excipients that slow down release, thereby controlling the release profile to match therapeutic requirements.
2Reliability
If once-daily oral administration is used to maintain therapeutic blood concentration, then the reliability of treatment is improved, but the burden on patients increases reducing compliance
Solution Approach 1:
The extended-release formulation provides continuous release of the active ingredient over 48 hours or longer, maintaining therapeutic blood concentrations continuously without requiring daily dosing. This continuous action reduces the frequency of administration while preserving treatment reliability.
Solution Approach 2:
The invention transforms the dosing schedule from daily periodic administration to weekly or bi-weekly periodic administration. By extending the release duration to cover multiple days, the treatment maintains its periodic effectiveness while significantly reducing the frequency of patient intervention.
3Duration of action of moving object
If a controlled release composition is designed to release active ingredient at an appropriate rate, then the duration of action is improved, but the device complexity increases
Solution Approach 1:
The composition is segmented into distinct layers with different release characteristics. This segmentation allows each layer to be optimized independently for its specific release function, achieving complex release profiles through simple layered structures rather than complicated single-matrix systems.
Solution Approach 2:
The invention uses composite materials combining different excipients in each layer to achieve controlled release. By selecting excipients with specific properties (solubility, swelling characteristics, binding strength), the desired release profile is achieved through material composition rather than complex structural design.
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 composition maintains a therapeutically effective blood concentration of the active ingredient for an extended period, enabling less frequent administration, such as once a week, thereby improving patient compliance and reducing treatment recurrence.
Implementation Method 1
the active ingredient is required to be continuously released from the composition at an appropriate rate
Implementation Method 2
A controlled release oral solid pharmaceutical composition comprising a salt of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one, specifically a fumaric acid salt
Implementation Method 3
a cellulose-based water-soluble polymer
Data Source
AI summary
Provided is a means that is capable of preventing initial excessive release of an active ingredient, and that allows for sustained release of a pharmaceutically active amount of the active ingredient over a long period of time.