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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
Author(s) -
Singh Yeshwant,
Hidau Mahendra Kumar,
Misra Anamika,
Kushwaha H.N.,
Tiwari Ashish,
Sharma Ashok Kumar,
Singh Shio Kumar
Publication year - 2015
Publication title -
drug testing and analysis
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.065
H-Index - 54
eISSN - 1942-7611
pISSN - 1942-7603
DOI - 10.1002/dta.1748
Subject(s) - pharmacokinetics , chromatography , bioavailability , triethylamine , protein precipitation , chemistry , pharmacology , bioequivalence , bioanalysis , high performance liquid chromatography , medicine , organic chemistry
A sensitive and selective ultra fast liquid chromatography (UFLC) method has been developed and validated for the determination of a potent and novel antitubercular compound S006‐830 in Sprague Dawley (SD) rat plasma. Samples were extracted and processed by protein precipitation method using acetonitrile. Chromatographic separation was achieved on a Phenomenex, Luna C‐18 column (3μm, 100mm x 2mm i.d.) under isocratic condition. Detection was performed on UFLC‐NEXERA system (LC‐30AD, Shimadzu, Kyoto, Japan) with a degasser (DGU‐20A), auto‐injector (SIL‐30AC), fixed with a 100‐μL loop. Method was found sensitive and reproducible over a linearity range of 15.6‐2000 ng/mL. Recovery of S006‐830 and internal standard was found >90% for spiked matrix control and standard quality control plasma samples. This validated method was successfully applied to generate pharmacokinetic profile of S006‐830 in SD rats. Oral dose proportionality studies were conducted at 100, 50, 25 mg/Kg dose levels, while an IV study was conducted at 25 mg/Kg dose. There was dose dependent increase in AUC and C max indicating S006‐830 to exhibit linear pharmacokinetics. S006‐830 exhibited favorable bioavailability in the range of 45‐55%. Copyright © 2014 John Wiley & Sons, Ltd.