The pharmacokinetic aspects of diminazene aceturate were studied in lactati
ng goats and sheep after single intravenous and intramuscular administratio
ns of 3.5 mg/kg b.wt. Plasma and milk concentrations were determined by use
of reversed phase high-performance liquid chromatography (HPLC) after ion-
pair extraction. Following intravenous injection, the disposition of dimina
zene in goats and sheep conformed to a two-compartment model with rapid dis
tribution and slower elimination phases. Values of (t(1/2 beta)) were obtai
ned indicating a slower final disappearance of the drug from plasma of shee
p (21.17 h) than in goats (16.39 h). Diminazene concentrations were maintai
ned for more than 4 days in the plasma of goats and sheep. In both species
of animals, diminazene was rapidly absorbed following intramuscular adminis
tration of 3.5 mg/kg b.wt. The peak plasma concentrations (C-max) were 7.00
and 8.11 mu g/ml and were attained at (T-max) 0.92 and 1.12 hours in goats
and sheep, respectively. The elimination half-life (t(1/2el)) of diminazen
e after intramuscular administration was shorter in goats (16.54 h) than in
sheep (18.80 h). Systemic bioavailabilities (F%) of diminazene after intra
muscular administration were 94.94% and 82.64% in goats and sheep, respecti
vely. Diminazene could be detected in milk of goats and sheep within 10 min
postinjection. Milk concentrations of the drug were lower in goats than in
sheep and were detected for 5 and 6 days following both routes of administ
ration, respectively.