Development of an Image-based Method for Tablet Microstructure Description and Its Correlation with API Release Rate

The performance of a pharmaceutical formulation, such as the drug (API) release rate, is significantly influenced by the properties of the materials used, the composition of the final product and the tablet compression process parameters. However, in some cases, the knowledge of these input parameters does not necessarily provide a reliable description or prediction of tablet performance. Therefore, the knowledge of tablet microstructure is desirable to understand such formulations. Commonly used analytical techniques, such as X-ray tomography and intrusion mercury porosimetry, are not widely used in pharmaceutical companies due to their price and/or toxicity, and therefore, efforts are made to develop a tool for fast and easy microstructure description.

In this work, we have developed an image-based method for microstructure description and applied it to a model system consisting of ibuprofen and CaHPO₄∙2H₂O (API and excipient with different deformability). The obtained parameter, the quadratic mean of the equivalent diameter of the non-deformable, brittle excipient CaHPO₄∙2H₂O, was correlated with tablet composition, compression pressure and API release rate. The obtained results demonstrate the possibility of describing the tablet dissolution performance in the presented model system based on the microstructural parameter, providing a possible model system for compressed solid dosage forms in which a plastic component is present and specific API release is required.

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Materials

Two different batches of ibuprofen were used in this study (marked as Ibu I and Ibu II), both kindly provided by Zentiva, k.s., CZ in combination with CaHPO4∙2H2O (EmCompress®; JRS Pharma GmbH & Co., DE) for the model tablets preparation. One of the ibuprofen batches, Ibu I, was for some of the tested formulations milled, so its particle size was lower than with the two raw batches. Milling was performed using a planetary ball mill PM 100 CM (Retsch GmbH, DE) at 250 rpm for 15 min. This altered batch is further marked as Ibu Im. Since the importance of initial particle size and morphology of the input materials was taken into consideration, all four materials (CaHPO4∙2H2O and three ibuprofen variants) were characterised using a static light scattering system Mastersizer 3000 (Malvern Instruments, UK) for particle size distribution (Fig. 1). Scanning electron microscopy, SEM, (FE MIRA II LMU, Tescan s.r.o., CZ) was then used to describe and evaluate the particle morphology of these materials.

Römerová, S., Dammer, O. & Zámostný, P. Development of an Image-based Method for Tablet Microstructure Description and Its Correlation with API Release Rate. AAPS PharmSciTech 24, 199 (2023). https://doi.org/10.1208/s12249-023-02658-w

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