Sustained-Release PDE10 Inhibitor Matrix for Safer Plasma Control
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Solution Overview
Problem
Therapeutic compounds often exhibit sharp increases and subsequent decreases in plasma levels due to rapid release in the gastrointestinal tract, posing safety concerns for drugs that are not well-tolerated at high levels, and existing sustained release formulations do not effectively provide therapeutically safe and effective plasma concentration profiles.
Innovation Solution
A sustained release matrix pharmaceutical composition comprising a PDE10 inhibitor, a water insoluble matrix forming release agent (e.g., modified glyceryl), and a hydrophilic matrix forming release agent (e.g., hydroxypropyl cellulose or polyethylene oxide) is used, with specific ratios and melt granulation techniques to control drug release and prolong the therapeutic effect.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If therapeutic compounds are released quickly in the gastrointestinal tract, then the compound is rapidly delivered to the system, but the plasma level concentration increases sharply and then decreases significantly, posing safety concerns
Solution Approach 1:
The patent changes the release rate parameter by using a matrix formulation with hydrophilic matrix-forming release agents that control the dissolution rate. The composition includes specific ratios of release agents (e.g., HPMC, HPC, PEO) that modulate the release kinetics, transforming the release profile from rapid to sustained, thereby maintaining plasma levels within a safe therapeutic window without sharp peaks
Solution Approach 2:
The patent employs a composite matrix formulation combining multiple matrix-forming release agents (hydrophilic polymers such as HPMC, HPC, and PEO) with the active ingredient. This composite structure provides controlled release characteristics that prevent sharp plasma concentration increases while ensuring adequate drug delivery, thus resolving the contradiction between release speed and safety
2Duration of action of moving object
If sustained release formulations are prepared to protect the active ingredient, then the drug release profile is prolonged, but the granulation of the system needs improvement to achieve therapeutically safe and effective plasma level concentration
Solution Approach 1:
The patent optimizes the granulation process by adjusting physical parameters such as moisture content, granulation time, and mixing speed. The formulation includes specific amounts of matrix-forming agents (e.g., 20-80% w/w of the total composition) that facilitate proper granulation and achieve the desired sustained release profile with consistent plasma level concentrations
Solution Approach 2:
The patent applies local quality by creating a matrix structure where the active ingredient is distributed throughout the formulation with specific matrix-forming agents concentrated in certain phases. This localized arrangement ensures both proper granulation characteristics and sustained release, achieving therapeutically safe and effective plasma levels
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 moderate plasma levels with decreased peak concentrations, providing sustained and safe therapeutic benefits by controlling the release of PDE10 inhibitors.
Implementation Method 1
a hydrophilic matrix forming release agent
Implementation Method 2
hydrophilic matrix forming release agent
Implementation Method 3
a water insoluble matrix forming release agent
Data Source
AI summary
The invention relates to a sustained release pharmaceutical composition comprising a tablet core comprising a therapeutically effective amount of a compound selected from Group 1, or a pharmaceutically acceptable salt thereof, an insoluble matrix forming release agent and a hydrophilic matrix forming release agent.