Study of Pharmacokinetics and Tissue Distribution of BITS-17 in Rat Plasma and Tissue Homogenate Using a Validated LC Method

Addepalli Venkata Ramani, Vadl

Abstract

Accurate, simple, sensitive, reproducible and specific liquid chromatographic method has been developed for estimation of BITS-17 in rat plasma and other biological tissues using β-naphthol as an internal standard (IS). The applicability of the validated method was tested to estimate the concentrations of BITS-17 (a novel anti tubercular agent) in plasma and tissues that were harvested in a rat tissue distribution study. A liquid - liquid extraction technique was used to extract BITS-17 and internal standard from the plasma and various tissue homogenates. The main pharmacokinetic parameters obtained after intravenous administration were t½=14 ± 0.20 h, Kel=0.62 ± 0.10 h-1, mean plasma clearance=1.35 ± 0.16 mg/h and mean volume of distribution = 1.99 ± 0.49L. The systemic absorption was tested with two formulations was slow after oral administration and maximum bioavailability was 33.02%. The peak plasma concentration of both the formulations was found to be 1.31 ± 0.06 and 1.0 ± 0.12 mg/mL, respectively, which was much above the levels of minimum inhibitory concentrations of BITS-17. The concentrations of BITS-17 were found in various tissues but the levels in lung and brain signifies a good therapeutic target.

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