UFLC method development and validation of a novel triethylamine containing thiophene S006‐830 ‐ an antitubercular molecule and its application to pharmacokinetic and bioavailability studies in SD rats

• DOI: 10.1002/dta.1748
• Publication Date: 2014-11-21T01:31:09Z
• Authors: Yeshwant Singh; Mahendra Kumar Hidau; Anamika Misra; H.N. Kushwaha; Ashish Tiwari; Ashok Kumar Sharma; Shio Kumar Singh
• Keywords: Triethylamine; Protein precipitation; Bioequivalence; Bioanalysis

A sensitive and selective ultra fast liquid chromatography (UFLC) method has been developed validated for the determination of a potent novel antitubercular compound S006‐830 in Sprague Dawley (SD) rat plasma. Samples were extracted processed by protein precipitation using acetonitrile. Chromatographic separation was achieved on Phenomenex, Luna C‐18 column (3μm, 100mm x 2mm i.d.) under isocratic condition. Detection performed UFLC‐NEXERA system (LC‐30AD, Shimadzu, Kyoto, Japan) with degasser (DGU‐20A), auto‐injector (SIL‐30AC), fixed 100‐μL loop. Method found reproducible over linearity range 15.6‐2000 ng/mL. Recovery internal standard >90% spiked matrix control quality plasma samples. This successfully applied to generate pharmacokinetic profile SD rats. Oral dose proportionality studies conducted at 100, 50, 25 mg/Kg levels, while an IV study dose. There dependent increase AUC C max indicating exhibit linear pharmacokinetics. exhibited favorable bioavailability 45‐55%. Copyright © 2014 John Wiley & Sons, Ltd.