Microwave Induced Dielectric Heating for the On-demand Development of Indomethacin Amorphous Solid Dispersion Tablets

The poor aqueous solubility of drugs challenges their pharmaceutical development and oral bioavailability. At present, the development of dosage forms with poorly water-soluble drugs by means of amorphous solid dispersions (ASDs) approach has been an active area of research. Meanwhile, dielectric heating, a process in which a radio frequency (RF), radio wave or microwave electromagnetic radiation heats materials with dielectric properties, has been applied in the food industry and synthetic organic chemistry for many years. In this work, tablets of indomethacin (IND) amorphous solid dispersions (ASDs) with various polymer matrices were successfully obtained utilizing a novel dielectric heating method on-demand.

A series of solid-state analyses, including differential scanning calorimetry (DSC), powder X-ray diffraction (XRD), and polarized light microscopy (PLM) were used for examining drug/polymer miscibility, drug crystallinity and to determine the thermal stability of IND/polymer compositions. In addition, the comparative studies between the amorphous tablets and conventional directly compressed (DC) tablets exhibited higher hardness/compaction results for ASDs tablets (for Soluplus®, HPC HF), but smaller values for the other polymers (HPMC, HPMCAS, E PO, and P EO). The amorphous IND tablets showed improved drug release performance because the polymer matrix stabilized the solution that can maintain a thermodynamic environment for IND. An advanced release mechanism and kinetics study revealed that all ASD tablets exhibited mostly a Fickian diffusion. In contrast, non-cellulose polymer matrices showed swelling, erosion, or both swelling and erosion-controlled drug release. In summary, dielectric heating techniques offer a simple way to manufacture amorphous drug products and presents an alternative solution to the patient to optimize their treatment with conventional dosages. Continue on Microwave Induced Dielectric Heating for the On-demand Development of Indomethacin Amorphous Solid Dispersion Tablets