A sensitive and selective liquid chromatography-electrospray ionization-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the determination of rosuvastatin in human plasma using gliclazide as ...A sensitive and selective liquid chromatography-electrospray ionization-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the determination of rosuvastatin in human plasma using gliclazide as an internal standard (IS). Rosuvastatin and gliclazide in plasma were extracted with ethyl acetate, separated on a C18 reversed phase column, eluted with mobile phase of acetonitrile-methanoic acid (0.1%) (60:40, v/v), ionized by positive ion pneumatically assisted electrospray and detected in the multi-reaction monitoring mode using precursor → product ions of m/z 482.1 → 258.1 for rosuvastatin and m/z 324.2 → 127.2 for IS, respectively. The calibration curve was linear (r2 > 0.99, n = 5) over the concentration range of 0.1 - 60 ng/mL. The speci?city, matrix effect, recovery, sensitivity, linearity, accuracy, precision, and stabilities were validated for rosuvastatin in human plasma. In conclusion, the validation results showed that this method was sensitive, economical and less toxic and it can successfully ful?ll the requirement of bioequivalence study of rosuvastatin calcium tablets in Chinese healthy volunteers.展开更多
In the present study,we aimed to investigate the interactions of pharmacokinetics and liver distributions between rosuvastatin and repaglinide in rats.Coadministration of repaglinide（0.5 mg/kg,1 mg/kg and 2 mg/kg） f...In the present study,we aimed to investigate the interactions of pharmacokinetics and liver distributions between rosuvastatin and repaglinide in rats.Coadministration of repaglinide（0.5 mg/kg,1 mg/kg and 2 mg/kg） for 7 d significantly increased the AUC0–24 and Cmax of rosuvastatin（P〈0.01）,but dramatically decreased the CL/F of rosuvastatin（P〈0.01） after a single dose of rosuvastatin（10 mg/kg）.There were no obviously changes in the parameters of Tmax and t1/2.Coadministration of repaglinide also decreased the liver distribution of rosuvastatin（P〈0.01）.Coadministration of rosuvastatin（20 mg/kg） for 7 days significantly increased the AUC0–12 and Cmax of repaglinide（P〈0.05）,and decreased the CL/F of repaglinide（P〈0.01） after a single dose of repaglinide（1 mg/kg）.The liver distribution of repaglinide was also decreased（P〈0.01）.Our animal study indicated that repaglinide could significantly affect the pharmacokinetics and liver distribution of rosuvastatin in rats and vice versa.展开更多
文摘A sensitive and selective liquid chromatography-electrospray ionization-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the determination of rosuvastatin in human plasma using gliclazide as an internal standard (IS). Rosuvastatin and gliclazide in plasma were extracted with ethyl acetate, separated on a C18 reversed phase column, eluted with mobile phase of acetonitrile-methanoic acid (0.1%) (60:40, v/v), ionized by positive ion pneumatically assisted electrospray and detected in the multi-reaction monitoring mode using precursor → product ions of m/z 482.1 → 258.1 for rosuvastatin and m/z 324.2 → 127.2 for IS, respectively. The calibration curve was linear (r2 > 0.99, n = 5) over the concentration range of 0.1 - 60 ng/mL. The speci?city, matrix effect, recovery, sensitivity, linearity, accuracy, precision, and stabilities were validated for rosuvastatin in human plasma. In conclusion, the validation results showed that this method was sensitive, economical and less toxic and it can successfully ful?ll the requirement of bioequivalence study of rosuvastatin calcium tablets in Chinese healthy volunteers.
文摘In the present study,we aimed to investigate the interactions of pharmacokinetics and liver distributions between rosuvastatin and repaglinide in rats.Coadministration of repaglinide（0.5 mg/kg,1 mg/kg and 2 mg/kg） for 7 d significantly increased the AUC0–24 and Cmax of rosuvastatin（P〈0.01）,but dramatically decreased the CL/F of rosuvastatin（P〈0.01） after a single dose of rosuvastatin（10 mg/kg）.There were no obviously changes in the parameters of Tmax and t1/2.Coadministration of repaglinide also decreased the liver distribution of rosuvastatin（P〈0.01）.Coadministration of rosuvastatin（20 mg/kg） for 7 days significantly increased the AUC0–12 and Cmax of repaglinide（P〈0.05）,and decreased the CL/F of repaglinide（P〈0.01） after a single dose of repaglinide（1 mg/kg）.The liver distribution of repaglinide was also decreased（P〈0.01）.Our animal study indicated that repaglinide could significantly affect the pharmacokinetics and liver distribution of rosuvastatin in rats and vice versa.
