Amorphous Solid Dispersion of ABX464 for Solubility
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Solution Overview
Problem
ABX464, a compound used for treating inflammatory diseases, has poor solubility in aqueous solutions, leading to incomplete targeting in the body due to its crystalline form, necessitating improved solubility for effective pharmaceutical formulations.
Innovation Solution
The development of an amorphous solid dispersion (ASD) formulation of ABX464, which maintains the compound in a stable amorphous form during storage and administration, significantly enhancing its solubility and bioavailability by incorporating it with pharmaceutically acceptable carriers like polyvinylpyrrolidone and polyvinylacetate copolymers through processes such as spray-drying.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If ABX464 is formulated in crystalline form, then physical stability and manufacturing simplicity are improved, but solubility in aqueous solutions deteriorates
Solution Approach 1:
The patent changes the physical state parameter of ABX464 from crystalline to amorphous form through formulation in amorphous solid dispersion. This parameter change enables the compound to maintain stability while achieving improved solubility, as the amorphous state allows better interaction with aqueous solutions compared to the crystalline structure.
Solution Approach 2:
The patent creates a composite material system by combining ABX464 with pharmaceutically acceptable carriers in an amorphous solid dispersion matrix. This composite formulation allows the active ingredient to be stabilized in an amorphous state while gaining enhanced solubility properties, resolving the contradiction between stability and solubility.
2Ease of manufacture
If ABX464 is formulated in crystalline form, then manufacturing simplicity and robustness are improved, but bioavailability deteriorates due to poor solubility
Solution Approach 1:
The patent changes the physical state from crystalline to amorphous, which fundamentally alters the dissolution characteristics. This parameter change enables better solubility and bioavailability while maintaining manufacturing feasibility through established amorphous solid dispersion techniques.
Solution Approach 2:
The patent introduces pharmaceutically acceptable carriers as intermediary substances that facilitate the transition from crystalline to amorphous state and enable improved solubility. These carriers act as mediators that allow the active ingredient to achieve better bioavailability while maintaining formulation robustness.
3Quantity of substance
If ABX464 is maintained in amorphous form, then solubility is improved, but stability during storage deteriorates
Solution Approach 1:
The patent creates a composite amorphous solid dispersion system where the active ingredient is embedded in a matrix of pharmaceutically acceptable carriers. This composite structure stabilizes the amorphous form of ABX464 during storage while maintaining its enhanced solubility properties, preventing crystallization and degradation.
Solution Approach 2:
The patent employs transient solvent systems during formulation that temporarily stabilize the amorphous form, with the understanding that the final formulation will be processed to remove excess solvent. This approach allows initial stabilization during manufacturing while ensuring long-term stability through proper formulation 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 ASD formulation ensures ABX464 remains in an amorphous form, improving its solubility and stability, allowing for effective targeting and treatment of inflammatory diseases like Inflammatory Bowel Disease, Rheumatoid Arthritis, and Multiple Sclerosis, while maintaining chemical and physical stability under stress conditions.
Implementation Method 1
The ASD technique allows to maintain ABX464 under a stable amorphous form during storage up to 100° C., in particular up to 80° C., in particular at least two weeks
Data Source
AI summary
The present invention relates to an amorphous solid dispersion comprising ABX464 and at least one pharmaceutically acceptable carrier. The present invention also concerns a pharmaceutical composition comprising said ASD, processes for their preparation, an ASD obtainable by specific processes, their use as a medicament and more particularly their use in the treatment and/or prevention of inflammatory diseases, diseases caused by viruses and/or cancer or dysplasia.