An academic subcommittee of Japanese Society of Hospital Pharmacists formulated the guideline for the sterile preparation of antineoplastic agents in 2008. The practical methods to monitor a workplace contamination and occupational exposure to antineoplastic agents have not been introduced into a hospital setting yet. The aims of this study were to develop a monitoring method using doxorubicin for workplace contamination and occupational exposure to antineoplastic agents and to apply it to surveillance in a hospital setting. The surface contamination of workplace was wiped with non-woven fabric containing 70% 2-propanol. The occupational exposure was evaluated by spot urine sampling during 24 hours. Chromatographic separation was achieved by a reverse phase HPLC. Doxorubicin and fluorescein (internal standard) were detected at an excitation and emission wavelength of 470 and 550 nm, respectively. The monitoring method was applied to survey the workplace contamination and occupational exposure to antineoplastic agents in Hamamatsu University Hospital. The calibration curves for doxorubicin were linear over concentration ranges of 1.5-729 ng/100 cm(2) for surface contamination and 1.0-486 ng/ml for the urine. The run time was 10 min. The intra- and interassay precisions were within 8.5%. As the surveillance in a hospital setting, the flow line adhering to the guideline kept the exposure to low level. In addition, the occupational exposure in the workers was not observed. In conclusion, this study developed the monitoring method using doxorubicin for the workplace contamination and occupational exposure to antineoplastic agents. This method can be utilized to survey in a hospital setting.