Quantification of rosiglitazone in rat plasma and tissues via LC–MS/MS: Method development, validation, and application in pharmacokinetic and tissue distribution studies

Abstract

A bioanalytical method for the quantification of rosiglitazone in rat plasma and tissues (adipose tissue, heart, brain, bone, and kidney) using LC–MS/MS was developed and validated. Chromatographic separation was achieved on a Gemini C18 column (50 × 4.6 mm, 3 μm) using a mobile phase consisting of 10 mM ammonium formate (pH 4.0) and acetonitrile (10:90, v/v) at a flow rate of 0.8 mL/min and injection volume of 10 μL (internal standard: pioglitazone). LC–MS detection was performed with multiple reaction monitoring mode using target ions at m/z → 358.0 and m/z → 357.67 for rosiglitazone and pioglitazone (internal standard), respectively. The calibration curve showed a good correlation coefficient (r2) over the concentration range of 1–10,000 ng/mL. The mean percentage recoveries of rosiglitazone were found to be over the range of 92.54–96.64%, with detection and lower quantification limit of 0.6 and 1.0 ng/mL, respectively. The developed method was validated per U.S. Food and Drug Administration guidelines and successfully utilized to measure rosiglitazone in plasma and tissue samples. Further, the developed method can be utilized for validating specific organ‐targeting delivery systems of rosiglitazone in addition to conventional dosage forms.

A Multiplex Molecular Cell-Based Sensor to Detect Ligands of PPARs: An Optimized Tool for Drug Discovery in Cyanobacteria

“…Comparing our results with the available bibliography, rosiglitazone’s LOQ in uniplex mode is of the same range as that observed using LC-MS in rat plasma and tissues, 1.68 nM [ 52 ]. In addition, for rosiglitazone, the EC 50 observed with the sensor in uniplex mode for PPARγ, 29.37 nM, was in the same range as determined with pBIND[Rluc]/pGL4.35[Fluc] system by other authors [ 53 ].…”