SNAC Polymorph A Thermal Treatment for Stability
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Solution Overview
Problem
Current methods for producing sodium N-(8-2-Hydroxybenzoyl)amino caprylate (SNAC) polymorphic form A suffer from high hygroscopicity, which affects stability and requires specific storage conditions, limiting its use in pharmaceutical solid dosage forms.
Innovation Solution
Heating SNAC polymorphic form A at temperatures above 90°C, specifically between 105-140°C for at least 5 minutes, reduces crystal imperfections and hygroscopicity, enabling improved stability and allowing for manufacturing and storage under ambient conditions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If SNAC polymorphic form A is produced using conventional methods, then it can be obtained for pharmaceutical use, but it exhibits high hygroscopicity which compromises stability and requires controlled storage conditions
Solution Approach 1:
The patent applies parameter changes by heating SNAC polymorphic form A at temperatures above 90°C (specifically 105-140°C for at least 5 minutes) to reduce crystal imperfections and hygroscopicity. This thermal treatment modifies the physical parameters of the material to achieve lower moisture uptake and improved storage stability without requiring controlled humidity conditions
Solution Approach 2:
The patent implements preliminary action by performing the heating treatment during the manufacturing process to pre-reduce hygroscopicity before the material is packaged and stored. This preliminary reduction of harmful properties eliminates the need for subsequent controlled storage conditions, allowing the material to be handled and stored under ambient conditions
2Ease of manufacture
If SNAC polymorphic form A with high hygroscopicity is used, then it can be produced without additional processing steps, but it requires low humidity and temperature controls during manufacturing and storage
Solution Approach 1:
By changing the thermal parameter (heating above 90°C), the patent reduces hygroscopicity to a level that eliminates the need for complex storage infrastructure. The material can then be manufactured and stored using simple ambient condition facilities, reducing device complexity while maintaining ease of manufacture
Solution Approach 2:
The patent converts the harmful effect of high hygroscopicity into a benefit by applying controlled heating that reduces moisture uptake. The thermal energy that could potentially cause degradation is instead used to reorganize the crystal structure and reduce imperfections, transforming a potential harm into an improvement in storage stability
3Reliability
If SNAC polymorphic form A undergoes heating treatment above 90°C, then hygroscopicity and crystal imperfections are reduced, but additional energy and time are required for the heating process
Solution Approach 1:
The patent applies partial action by heating the material to a specific temperature range (105-140°C) for a minimum duration (at least 5 minutes) rather than using excessive heating. This optimized parameter range achieves the necessary reduction in hygroscopicity and crystal imperfections while minimizing energy consumption and processing time
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 process significantly decreases hygroscopicity and enhances storage stability, allowing for the use of SNAC in pharmaceutical solid dosage forms without the need for low humidity and temperature controls, and permits the use of simpler, less expensive packaging.
Implementation Method 1
heating, optionally under reduced pressure, the SNAC polymorphic form A provided in step a. at a temperature of above 90° C.
Implementation Method 2
The process significantly decreases hygroscopicity and enhances storage stability
Data Source
AI summary
The present invention relates to a method of making sodium N-(8-2-Hydroxybenzoyl)amino capry late form A. SNAC polymorphic form A having improved stability and the use of said SNAC polymorphic form A in a solid pharmaceutical dosage form