Abstract
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.
Highlights
Rosuvastatin (Figure 1) is a hydroxyl-methyl-glutaryl coenzyme A (HMG-CoA) reductase inhibitor used in the treatment of patients with dyslipidemia [1]
The validation results showed that this method was sensitive, economical and less toxic and it can successfully fulfill the requirement of bioequivalence study of rosuvastatin calcium tablets in Chinese healthy volunteers
Retention times of rosuvastatin and internal standard (IS) were 3.0 and 5.1 min, respectively, and overall run time was within 6 min
Summary
Rosuvastatin (Figure 1) is a hydroxyl-methyl-glutaryl coenzyme A (HMG-CoA) reductase inhibitor used in the treatment of patients with dyslipidemia [1]. The population pharmacokinetic study revealed that plasma exposure to rosuvastatin was significantly higher in Asian subjects than in White subjects living in the same environment [5]. Several methods have been reported for the quantification of rosuvastatin in plasma. Kumar TR et al published a HPLC-UV method for the determination of rosuvastatin in rat plasma [6]. Simultaneous quantitations of rosuvastatin and fenofibric acid [10] or other coadministrated drugs [11,12] in biological samples were proposed by some literatures, using HPLC with ultraviolet detection [11,12] or LC-MS/MS [10], but the lowest detection limit of these methods was 0.6 ng/mL, not sensitive enough to meet the requirement for rosuvastation determination in plasma. It was necessary to develop a more optimized LC-MS/MS method for the quantitation of rosuvastatin in plasma
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