SIMPLE AND RAPID HPLC METHOD DETERMINATION OF CSR1 AND CSR2, NEW HETEROCYCLIC THIAZOLIDINEDIONE DERIVATIVES, IN RAT PLASMA
Journal Title: International Journal of Pharmacy and Pharmaceutical Sciences - Year 2016, Vol 8, Issue 8
Abstract
Objective: This study aimed at developing a simple and rapid high-performance liquid chromatography (HPLC) method for determination of two thiazolidinedione derivatives, which were developed as anti-proliferative moieties (CSR1 and CSR2) in rat plasma. In addition, their oral pharmacokinetics were studied.Methods: Drugs were recovered from plasma using acetonitrile and analyzed on a Kromasil C8 column (250 mm × 4.6 mm; 4 μm). HPLC running conditions (0.01M phosphate buffer [pH = 3.0]; flow rate, 0.9 ml/min; at 210 nm; run time, 17 min) were optimized and further used for the determination of pharmacokinetic parameters.Results: At the described chromatographic conditions, CSR1, CSR2 and internal standard (metformin) eluted at 10.44, 9.41, and 3.15 min, respectively. The calibration curves were linear over the range of 0.25–20 µg/ml, with a correlation coefficient>0.999. The quantification limit was 0.25 µg/ml. Within- and between-day precision values were less than 15%. The developed HPLC method was successfully used to study the pharmacokinetics of CSR1 and CSR2 in rats. The developed method was successfully used to study the pharmacokinetics of CSR1 and CSR2. Cmax, AUC0-12, Tmax, t1/2 for CSR1 were 12.2±1.9 µg/ml, 65.34±0.12 µg h/ml, 4.07±0.23 h, t1/2= 4.54±0.12 h, respectively, and those for CSR2 were 10.6±2.2 µg/ml, 62.45±0.31 µg h/ml, 3.56±0.23 h, 3.86±0.09 h, respectively.Conclusion: A specific, linear, and reproducible method was successfully developed and implemented to determine pharmacokinetic activity for two thiazolidinedione derivatives (CSR1 and CSR2), which have been shown to have significant anti-proliferative activity.Â
Authors and Affiliations
Hardik Joshi, C. S. Ramaa
Keywords
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