The objective of this study was to determine and compare the plasma concentrations of rosuvastatin following single- and multiple-dose administration in Chinese volunteers. The study was of an open label, randomized, three-way cross-over design and was conducted in 12 subjects. Single dose administration of the rosuvastatinon was characterized by a rapid absorption (2.045 +/- 0.891 h, 2.273 +/- 1.009 h and 1.667 +/- 0.651 h) and a marked peak plasma concentration (9.938 +/- 4.438, 28.09 +/- 12.075 and 43.092 +/- 22.09 ng/ml) for the three different doses (5 mg, 10 mg and 20 mg) of rosuvastatin. The apparent elimination half-life amounted to 7.914 +/- 3.813 h, 8.445 +/- 4.994 h and 15.401 +/- 5.429 h following administration, respectively. Similar findings were obtained after multiple dosing. A rapid absorption (3 +/- 1.365 h, 3.042 +/- 1.054 h and 2.375 +/- 0.829 h) and a marked peak plasma concentration (9.288 +/- 5.314, 18.808 +/- 6.687 and 49.808 +/- 23.516 ng/ml) for the three different doses (5 mg, 10 mg and 20 mg) of rosuvastatin were observed. The apparent elimination half-life amounted to 13.181 +/- 5.492 h, 8.035 +/- 3.331 h and 15.509 +/- 6.43 h following administration, respectively. Small differences in gender are not considered clinically relevant, and dose adjustments based on gender are not anticipated. But the state of fed or fasting will affect the pharmacokinetic of rosuvastatin.