Revista de Bioanálise e Biomedicina

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

Abstract

Addepalli Venkata Ramani, Vadlamani Lakshmi Indira, SatyaVani, Sandeep Gill, Perumal Yogeeswari and Dharmarajan Sriram

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.