Quinazoline Derivative Stabilizer for Solubility and Stability
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Solution Overview
Problem
Current pharmaceutical compositions for inhibiting abnormal protein tyrosine kinase (PTK) activity, particularly in the erbB family, face challenges with solubility, stability, and bioavailability, limiting their effectiveness in treating diseases such as cancers and proliferative disorders.
Innovation Solution
A pharmaceutical composition comprising a pharmaceutically acceptable salt of N-{4-[3-chloro-4-(3-fluoro-benzyloxy)phenylamino]quinazolin-6-yl}-acrylamide, optionally with a carrier or diluent, and a stabilizer like high-molecular substances or surface active substances, which improves solubility, stability, and bioavailability by enhancing dispersion and protecting the active ingredient during storage and administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If quinazoline derivatives are used as PTK inhibitors, then therapeutic efficacy is improved, but solubility and stability are poor
Solution Approach 1:
The patent introduces a stabilizer as an intermediary substance that mediates between the quinazoline derivative and the formulation system. This stabilizer improves solubility and stability without interfering with the PTK inhibitory activity, thus resolving the contradiction between therapeutic efficacy and formulation stability.
Solution Approach 2:
The patent creates a composite pharmaceutical composition by combining the quinazoline derivative with a stabilizer and carrier materials. This composite formulation enhances solubility and stability while maintaining the active ingredient's PTK inhibitory activity, addressing both therapeutic efficacy and formulation challenges.
2Reliability
If quinazoline derivatives are used as PTK inhibitors, then therapeutic efficacy is improved, but bioavailability is limited
Solution Approach 1:
The stabilizer acts as a mediator that facilitates the absorption and bioavailability of the quinazoline derivative. By improving dissolution and dispersion properties, the stabilizer enhances bioavailability without compromising the PTK inhibitory effect, thus resolving the contradiction between therapeutic efficacy and bioavailability.
Solution Approach 2:
The patent modifies physical parameters of the formulation by introducing a stabilizer that changes solubility, dispersion, and absorption characteristics. These parameter changes enhance bioavailability while maintaining the active ingredient's pharmacological activity, addressing the contradiction between therapeutic efficacy and bioavailability.
3Stability of the object's composition
If stabilizer is added to improve solubility and stability, then formulation quality is improved, but composition complexity increases
Solution Approach 1:
The patent employs a stabilizer that serves its purpose efficiently and can be easily removed or degraded if necessary. This approach improves solubility and stability without creating permanently complex or difficult-to-manage formulation systems, thus resolving the contradiction between formulation quality and complexity.
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 exhibits excellent therapeutic efficacy and safety in treating diseases characterized by abnormal PTK activity, with improved bioavailability and stability, ensuring effective inhibition of erbB family signaling pathways.
Implementation Method 1
a stabilizer having dispersing and/or protective effect on the active ingredient
Implementation Method 2
a stabilizer having dispersing and/or protective effect on the active ingredient
Data Source
AI summary
The present invention provides a pharmaceutical composition, useful for the treatment of diseases characterized by abnormal PTKs activity of erbB family in a mammal, comprising pharmaceutically acceptable salts of N-{4-[3-chloro-4-(3-fluoro-benzyloxy) phenylamino]quinazolin-6-yl}-acrylamide, optionally a pharmaceutically applicable carrier or diluent, and a stabilizer having a dispersing and/or protective effect on the active ingredient. The present invention further provides a pharmaceutical formulation comprising said composition, methods for preparation of said composition and said formulation, as well as use of said composition and said formulation for treating diseases characterized by abnormal PTKs activity of erbB family in a mammal.