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Spatial and Temporal Visualization of Polymorphic Transformations in
Pharmaceutical Tablets

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The uploaded article emphasizes several key lessons related to the analysis of polymorphic transformations and structural changes in pharmaceutical formulations:

  1. Advanced Characterization Techniques:

    • X-ray Diffraction Computed Tomography (XRD-CT) offers a non-destructive method for spatially resolving polymorphic forms and analyzing the effects of compaction pressure on pharmaceutical tablets. This technique prevents errors caused by sample preparation-induced transformations.

  2. Role of Complementary Methods:

    • Electron diffraction is critical for solving crystal structures of unknown phases. It complements XRD-CT by providing detailed insights into the molecular structure of reaction products, as demonstrated by the identification of 2-(2-hydroxyacetoxy)acetic acid (HAA).

  3. Impact of Compaction Pressure:

    • Compression pressure can induce phase transformations in pharmaceutical formulations, such as the polymorphic transition observed for glycolide. The spatial distribution of these transformations within tablets is non-uniform, highlighting the importance of spatially resolved analysis.

  4. Environmental Effects on Stability:

    • Storage conditions can lead to significant chemical and structural changes in formulations. The study observed hydrolysis of glycolide into HAA during storage, influenced by the hygroscopic nature of microcrystalline cellulose (MCC).

  5. Integrated Approach to Analysis:

    • Combining advanced imaging and diffraction techniques, such as XRD-CT and electron diffraction, provides a holistic understanding of pharmaceutical formulations. This approach allows researchers to visualize and track changes over time and under varying conditions.

  6. Innovation in Pharmaceutical Research:

    • The use of cutting-edge tools like the ELDICO ED-1 for electron diffraction and synchrotron-based XRD-CT represents a step-change in the ability to investigate and optimize pharmaceutical products at the molecular level without sample destruction.

These lessons demonstrate how advanced analytical methods can be employed to improve the development, stability assessment, and quality control of pharmaceutical products.

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ELDICO Scientific AG (The Electron Diffraction Company) is a Swiss technology and service company founded in 2019 and based in the Switzerland Innovation Park Basel Area in Allschwil. ELDICO develops, manufactures and commercializes electron diffractometers , i.e. novel analytical instruments for electron based crystallography, enabling to investigate nano-crystalline samples. ELDICO has launched the first instrument specifically designed for nano-crystallographic investigations, the ELDICO ED-1. ELDICO’s clients are industrial and academic researchers in large and fast growing industries such as the pharmaceutical industry, the electromobility, and the advanced materials / MOF sector. The company partners with leading engineering companies and component suppliers among Dectris and Excillum to deliver superior performance. www.eldico-scientific.com