Formulation research offers step towards digital tablet design
Findings could lead to more robust tablet design and a minimising of the materials used, such as active pharmaceutical ingredients (APIs).
Novel insight on the relationship between tablet tensile strength, tablet brittleness and powder plasticity could advance drug formulation in the direction of digital tablet design, according to a new study.
“For a given material, tablets become more brittle and weaker as porosity increases, following an exponential decay relationship”, Elsergany et al. explained.
Tablet brittleness specifically has relevance for immediate-release tablets that are rapidly broken down in the gastrointestinal tract.
The study evaluated seven common excipients and twelve binary mixtures and demonstrated that material plasticity has a significant influence on both tablet strength and brittleness.
Elsergany et al.’s research offers the first experimental evidence supporting the hypothesised relationship between material plasticity and tablet brittleness.
Second author Changquan Calvin Sun, writing on LinkedIn, said: “Tablet brittleness is long expected to decrease with increasing material plasticity. However, because tablet brittleness is highly sensitive to tablet porosity, the relationship between tablet brittleness and material plasticity must be established at controlled porosity.”
The authors showed that “more plastic materials exhibit higher tensile strength and lower brittleness at the same tablet porosity”.
If validated, these observations could enable early-stage prediction of key tablet quality attributes of formulations, namely tensile strength and brittleness, using minimal amounts of active pharmaceutical ingredients”
“Importantly, the correlations observed at different tablet porosities enable the prediction of tablet brittleness at a porosity of interest directly from [in-die Py], which can be obtained from compression data using only a small amount of material with the help of a compaction simulator. This capability represents a meaningful step toward data-driven, digital tablet design, reducing reliance on extensive trial-and-error experimentation.”
If validated, these observations “could enable early-stage prediction of key tablet quality attributes of formulations, namely tensile strength and brittleness, using minimal amounts of active pharmaceutical ingredients” and guide drug developers in designing robust tablets.
This research will be published in International Journal of Pharmaceutics.
