OBJECTIVE: To establish the liquid chromatography-tandem mass spectrometry（HPLC-MS/MS） method for the determination of rosuvastatin in human plasma

study the pharmacokinetic characteristics of Rosuvastatin calcium tablets in healthy Chinese subjects and evaluate its bioequivalence. METHODS: The random

open

two-sequence

two-period

cross-over pharmacokinetic study method was adopted

30 healthy subjects were respectively enrolled in the fasting group and the postprandial group. Subjects received a single oral dose of Rosuvastatin calcium tablets subject drug or reference drug for 10 mg. The concentrations of rosuvastatin in plasma were determined by HPLC-MS/MS

and the pharmacokinetic parameters were calculated by Phoenix WinNonlin 8.1 software to evaluate the bioequivalence. RESULTS: The main pharmacokinetic parameters of rosuvastatin after a single fasting dose of the test drug and the reference drug were as follows: the C

max

were respectively（9.31±4.77） and（9.68±4.64） ng/mL; t

max

were respectively（4.37±0.73） and（4.25±0.95） h; t

1/2

were respectively（7.76±2.01） and（8.37±2.88） h; AUC

0-72 h

were respectively（83.95±43.46） and（88.85±49.52） ng·h/mL; AUC

0-∞

were respectively（86.50±43.63） and（91.23±49.52） ng·h/mL. The main pharmacokinetic parameters of resulvastatin after single postprandial administration of the test drug and the reference drug were as follows: C

max

were respectively（5.09±2.29） and（5.28±2.30） ng/mL; t

max

were respectively（4.45±0.90） and（4.47±1.22） h; t

1/2

were respectively（10.05±3.36） and（9.69±2.39） h; AUC

0-72 h

were respectively（64.24±33.27） and（66.83±32.68） ng·h/mL; AUC

0-∞

were respectively（67.42±33.83） and（70.14±33.68） ng·h/mL. The 90%CI of T/R of C

max

AUC

0-72 h

and AUC

0-∞

of main pharmacokinetic parameters of rosuvastatin in fasting condition were from 91.46% to 101.61%

from 91.59% to 102.31%

from 91.91% to 102.16%; in fed condition were from 91.39% to 103.73%

from 90.64% to 101.61%

from 90.94% to 101.45%. CONCLUSIONS: The established HPLC-MS/MS method is rapid and accurate for the determination of rosuvastatin in human plasma. The main pharmacokinetic parameters of Rosuvastatin calcium tablets in fasting and postprandial states are similar and have bioequivalence.