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

. 2023 Oct 02 ; 24 (7) : 199. [epub] 20231002

Language English Country United States Media electronic

Document type Journal Article

Grant support
CZ.02.2.67/0.0/0.0/18_057/0013355 Ministerstvo Školství, Mládeže a Tělovýchovy
A2_FCHT_2023_034 Vysoká Škola Chemicko-technologická v Praze

Links

PubMed 37783877
DOI 10.1208/s12249-023-02658-w
PII: 10.1208/s12249-023-02658-w
Knihovny.cz E-resources

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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