Design of taste-masked swellable drug particles using dry-coating technology with mechanical curing.

ABSTRACT

A novel dry coating technique for fine particles that does not require any liquids has been developed. Swellable ordered-mixed drug particles (Swell-OM-spheres, SOS), using a modified starch as the core particle and a drug coating layer have been previously developed. In the present work, SOS particles were further processed to generate 100-µm taste-masking particles using an all dry coating processes. SOS particles were coated with a gastric-soluble powder using a mechanical powder processor. The coated particles (CPs) were subsequently heated while rotating in the same powder processor, completing film formation by a process termed dynamic curing. As a control, conventional film formation (static curing) was performed using a drying oven. The CPs obtained by these two curing processes had distinct appearances, but exhibited equivalent dissolution suppression effects in a medium at pH 6.8 (the pH of the oral cavity). The suppression effect was further improved by adding a plasticizer to the coating powder, even though a lower heating temperature was required. Orally disintegrating tablets incorporating these CPs exhibited excellent taste-masking performance, i.e., suppressing taste in saliva while accelerating dissolution in gastric juice. The dissolution behavior indicated that the CPs can provide an ON/OFF switching function in drug release.