In hospitals and pharmacies, many kinds of pharmaceutical tablets are frequently crushed to powder in order to facilitate administration. However, there is concern about the influence of this process on the health of pharmacy workers. In this study, we conducted model experiments to estimate the potential exposure of pharmacy workers to pharmaceutical particles during tablet crushing and transfer of powder. Tablets were crushed in a tablet mill. Particulates released into the air during and after milling and transfer to a mortar were counted with a dust counter, and collected on the filter of an air sampler. Amounts of pharmaceutical active ingredients collected on the filter were determined by high-performance liquid chromatography (HPLC). During tablet crushing, particulates were released into the air. We found that the particle concentration in air was highest during transfer of the powder from the tablet mill to the mortar. The amount of active ingredient collected on the filter of the air sampler was significantly higher in the case of Loxonin, as compared with Neurovitan. Although conditions under which tablets are crushed are likely to vary greatly in practice, our results and calculations at least indicate that unmasked workers might routinely inhale microgram levels of active ingredients during tablet crushing and transfer of the resulting powder. Our results should be helpful in designing appropriate protective measures and in developing professional guidelines to minimize occupational exposure of pharmacy workers to drugs.