A big data approach to pharmaceutical flow properties.

Flowability is a key consideration during the formulation and process development of oral solid dosage forms as it can have a critical impact on product quality. With a limited number of examples available in the literature, there is a need to better understand and share the typical flow properties of pharmaceutical materials. Here, historical data (3909 experiments) from a shear cell apparatus were extracted and analysed. These data were composed of different material types, including APIs, excipients, blends and granules from nearly a decade of development projects. APIs were found to have poor flow properties (ffc <2), while other materials (excipients, blends and granules) generally had good flow properties. This analysis provided an enhanced understanding of the typical flow properties of pharmaceutical materials. By combining these data with information on the process and achieved drug load, it was possible to characterise our current operating space as a process flow map which could be used to focus future development.

Sucrose/Glucose molecular alloys by cryomilling.

We report here for the first time a series of amorphous sucrose/glucose molecular alloys prepared by cryomilling. Differential scanning calorimetry, X-ray powder diffraction and solution proton nuclear magnetic resonance showed that cryomilling drives a direct transformation from a two-phase mixture of crystalline sucrose and glucose, to a single-phase amorphous sucrose/glucose molecular alloy. The molecular alloys displayed a single Tg which varied linearly with composition. The effect of atmospheric moisture and the possibility of localised melting of the material because of milling-related friction were also discussed.