Amorphous Tapentadol Phosphate Stability
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Solution Overview
Problem
Tapentadol phosphate, a crucial analgesic, has a tendency to liquefy rapidly, making it unsuitable for pharmaceutical compositions and dosage forms, which is undesirable for workability and regulatory compliance.
Innovation Solution
The development of amorphous tapentadol phosphate, which can be processed and formulated into stable pharmaceutical compositions and dosage forms, characterized by the absence of long-range order and presence of short-range order, preventing liquefaction at room temperature.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If tapentadol phosphate is prepared using conventional methods, then it can be obtained as a solid, but it liquefies within a few seconds making it unsuitable for pharmaceutical compositions
Solution Approach 1:
The patent applies parameter changes by modifying the physical state of tapentadol phosphate from crystalline to amorphous form. This fundamental parameter change in molecular arrangement prevents the liquefaction issue while maintaining stability, making it suitable for pharmaceutical compositions and dosage forms.
Solution Approach 2:
The invention creates a composite material system by combining tapentadol phosphate with specific excipients and using particular processing methods (such as spray drying or freeze drying) to produce a stable amorphous solid dispersion. This composite approach prevents liquefaction while maintaining the active ingredient's efficacy.
2Reliability
If tapentadol phosphate is prepared as described in WO 2012/051246 A1, then it can be obtained as solid, but it liquefies rapidly which is highly undesirable for regulatory requirements
Solution Approach 1:
The patent fundamentally changes the physical parameter of tapentadol phosphate from crystalline to amorphous state. This parameter change eliminates the rapid liquefaction observed in conventional preparations, ensuring physical stability and compliance with regulatory requirements for pharmaceutical compositions.
Solution Approach 2:
The invention introduces intermediary substances (excipients) that stabilize the amorphous tapentadol phosphate and prevent liquefaction. These intermediaries act as matrices or carriers that maintain the physical stability of the active ingredient under various conditions.
Data Source
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AI summary
The present invention relates to tapentadol phosphate in crystalline form and to a process for producing tapentadol phosphate in crystalline form. Further, the present invention relates to a composition comprising crystalline tapentadol phosphate and to a dosage form containing the composition of the invention.