L-Malate C-Met Modulator Composition for Solubility and Stability
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Solution Overview
Problem
Existing pharmaceutical compositions for kinase modulators like Compound I face challenges in achieving desirable properties such as water-solubility, storage stability, hygroscopicity, and reproducibility, which impact drug development and efficacy.
Innovation Solution
Development of pharmaceutical compositions comprising Compound I in the form of its L-malate salt, combined with excipients like microcrystalline cellulose, lactose, hydroxypropyl cellulose, and magnesium stearate, optimized to enhance solubility, stability, and processability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If traditional pharmaceutical compositions are used for kinase modulators, then the basic therapeutic activity is maintained, but water-solubility, storage stability, and reproducibility are insufficient
Solution Approach 1:
The patent changes the physical-chemical parameters of the kinase modulator by forming an L-malate salt, which fundamentally alters the solubility and stability characteristics. This salt formation transforms the compound from having poor water-solubility to improved water-solubility, while also enhancing storage stability and reproducibility, directly resolving the technical contradictions in the original composition
2Reliability
If the kinase modulator is formulated with standard excipients, then the basic pharmaceutical requirements are met, but solubility and chemical/physical stability are insufficient
Solution Approach 1:
The patent modifies the chemical parameters of the active substance by converting it to its L-malate salt form. This chemical transformation changes the molecular properties to achieve both improved solubility (quantity of substance that can be dissolved) and enhanced chemical/physical stability, simultaneously addressing both requirements without needing additional excipients
Data Source
AI summary
Pharmaceutical compositions and unit dosage forms comprising Compound (I) are disclosed.