Imatinib Mesylate Tablet Coating for Polymorphic Stability
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Solution Overview
Problem
Imatinib mesylate formulations face challenges in maintaining polymorphic stability during storage, with existing forms prone to conversion, affecting the efficacy and consistency of the drug's performance in treating cancer and other conditions.
Innovation Solution
A pharmaceutical composition, preferably a tablet, is developed with crystalline imatinib mesylate forms V or X, coated with an organic solvent containing less than 20% w/v of water, specifically less than 10% w/v, to achieve high polymorphic stability, preventing conversion to forms α or β during storage.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing imatinib mesylate forms are used in formulations, then the drug can be administered orally for treating cancer and other conditions, but the formulations suffer from polymorphic conversion during storage, affecting efficacy and consistency
Solution Approach 1:
The patent applies parameter changes by carefully controlling the water content in the coating solution to less than 20% w/v (preferably less than 10% w/v, more preferably less than 5% w/v). This parameter modification prevents polymorphic conversion while maintaining the stability and efficacy of imatinib mesylate formulations during storage.
2Ease of manufacture
If crystalline imatinib mesylate is coated with aqueous coating solutions, then the tablets can be manufactured, but the high water content promotes polymorphic conversion to forms α or β during storage
Solution Approach 1:
The patent modifies the water content parameter in coating solutions to less than 20% w/v, thereby preventing polymorphic conversion while preserving the manufacturability of tablets through standard coating processes.
Solution Approach 2:
The patent introduces an organic solvent as an intermediary substance in the coating solution to replace water as the primary solvent. This intermediary approach maintains the coating processability while eliminating the harmful effects of high water content on polymorphic stability.
3Duration of action of stationary object
If imatinib formulations are stored at elevated temperature and humidity conditions, then the drug remains accessible for use, but polymorphic conversion accelerates, reducing drug performance consistency
Solution Approach 1:
The patent applies beforehand cushioning by pre-establishing a low-water-content coating environment that provides protective cushioning against polymorphic conversion. This preventive measure ensures that even when stored at elevated temperature and humidity conditions, the formulation maintains its polymorphic stability and drug performance consistency.
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 the initial polymorphic form with less than 3% conversion to other forms, ensuring stability and consistency over time, particularly at 40°C and 75% RH, thereby enhancing the drug's reliability and effectiveness.
Implementation Method 1
the pharmaceutical composition provides high polymorphic stability... preventing conversion to forms α or β during storage
Data Source
AI summary
Formulations containing imatinib, preferably imatinib mesylate, with high polymorphic stability and the processes for the preparation thereof are disclosed.