Pharmacokinetic Behaviour of Phenylglyoxal Bis(Guanylhydrazone) (PGBG) after Intravenous Administration in Rabbits

Phenylglyoxal bis(guanylhydrazone) (PGBG) is a synthesized analogue of methylglyoxal bis(guanylhydrazone) (MGBG), which has demonstrated anti‐parasitic activity in rabbits. The pharmacokinetic behaviour of PGBG after intravenous administration (10 mg/kg bodyweight) was studied in five rabbits. Plasma concentrations of PGBG were measured by high‐performance liquid chromatography. Plasma PGBG concentrations decreased rapidly and were not detectable beyond 90 min after treatment. The mean [± standard deviation (SD)] volume of distribution at steady state (Vdss) was 2.19 ± 0.47 l/kg and the mean plasma clearance value (Cl) was 29.99 ± 3.98 ml/min kg. This drug is rapidly eliminated from the body in rabbits, having a short elimination half‐life (0.93 h) and mean residence time (1.21 h).