This study is to report the effect of OATP1B1 gene mutation in the 521T→C in Chinese human on the pharmacokinetics of rosuvastatin and guide the reasonable clinical application of rosuvastatin by the feature of genetic polymorphism of OATP1B1.  Plasma samples were determined with LC-MS: the analyte and internal standard pitavastatin were both analyzed by MS in the ESI, m/z was 480.0 for rosuvastatin and 420.0 for the IS, separately.  Genotyping of OATP1B1 was determined with the method of polymerase chain reaction - amplification refractory mutation system targeted at 40 healthy volunteers and showed that there were 7 subjects with 521T→C mutant, accounting to 17.5% of total and wild type homozygote accounted to 82.5%.  It was found that there were significant differences between OATP1B1 mutation in the 521T→C and wild type homozygote for rosuvastatin pharmacokinetic process in Chinese human.  In contrast to OATP1B1 wild type group, OATP1B1 mutation group’s absorption degree increased, elimination process decreased.  The OATP1B1 mutation should be noted for guiding the reasonable application of rosuvastatin during its clinical use.