Wet-Granulated CYP11A1 Inhibitor Composition for Oral Stability
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Solution Overview
Problem
The compound 2-(isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one is prone to stability issues when formulated in solid oral compositions like tablets and capsules, and the suitable amount for human treatment is exceptionally small, making handling difficult.
Innovation Solution
A pharmaceutical composition using wet granulation with high intragranular drug load, neutral or slightly acidic ingredients, and oxygen scavengers to enhance stability and ensure effective release and uniformity, particularly suitable for hormonally regulated diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If the active ingredient is formulated in solid oral compositions with carriers and excipients, then the composition can be administered orally as tablets and capsules, but the active ingredient becomes prone to stability issues
Solution Approach 1:
The patent uses wet granulation as an intermediary process to encapsulate the active ingredient within granules, separating it from direct contact with oxygen and moisture in the solid composition. This mediator approach protects the active ingredient from degradation while maintaining oral administerability.
Solution Approach 2:
The patent creates a protected environment within the granule structure that limits exposure to reactive oxygen and moisture. By formulating the active ingredient in a controlled matrix with specific excipients, an inert-like environment is achieved that prevents oxidative degradation.
2Quantity of substance
If the amount of active ingredient is reduced to the suitable small range for human treatment, then the therapeutic dosage is appropriate, but the tablet becomes difficult to handle
Solution Approach 1:
The patent changes the physical parameters of the composition by using wet granulation to create a cohesive matrix that increases tablet mass and improves handling characteristics, while maintaining the low active ingredient content through high formulation efficiency.
3Stability of the object's composition
If high intragranular drug load is used, then the stability of active ingredient is improved, but the manufacturing precision requirements increase
Solution Approach 1:
The patent applies preliminary action by incorporating the active ingredient into the granule structure during the wet granulation process, ensuring uniform distribution before final tablet compression. This pre-mixing approach simplifies subsequent manufacturing steps while maintaining precision.
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 provides improved stability, dose content uniformity, and reproducible plasma concentrations, ensuring effective treatment of conditions like prostate and breast cancer.
Implementation Method 1
The package also comprising an oxygen scavenger
Data Source
AI summary
The present invention relates to a pharmaceutical composition for oral administration, particularly in the form of a tablet or a powder suitable to be filled into a capsule shell, comprising 2-(isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)-piperidin-4-yl)methoxy)-4H-pyran-4-one (I) or a pharmaceutically acceptable salt thereof as an active ingredient. Compound (I) or a pharmaceutically acceptable salt thereof is a selective inhibitor of CYP11A1 enzyme and is useful in the treatment of hormonally regulated diseases such as cancer including prostate cancer and breast cancer.