The disposition of chloroquine in healthy Nigerians after single intravenous and oral doses

Abstract

The pharmacokinetics of chloroquine after single oral (600 mg) and intravenous (2 mg kg-1) doses were studied in healthy black Nigerian students. The plasma concentrations of chloroquine and its desethylmetabolite were determined using a high performance liquid chromatography technique. Concentrations as low as 3 ng ml-1 were reproducibly determined. After i.v. dosage, the half-life ranged between 144 and 298 h; the total plasma clearance was between 282 and 1130 ml min-1 and the volume of distribution between 142 and 398 1 kg-1. Renal clearance was about 52% of plasma clearance. The estimated total urinary recovery of chloroquine and desethylchloroquine was 77% of the oral dose. There was no significant difference in the pharmacokinetics between the oral and the i.v. administration. The pharmacokinetic properties of chloroquine, in these black subjects did not differ from those previously demonstrated in Caucasians.