An animal model of clinical kinetic analyzed to diminazene aceturate in subjects with Tripanosoma infection

Diminazene aceturate has been reported to inhibit the reverse transcriptase activity by intercalating action mechanism of a number of protozoon eucaryot parasitic like Trypanosoma species. The phamacokinetics of diminazene in the blood plasma of five infected goats treated with single intramuscular doses of 7 mg diminazen base kg-1 body weight was investigated. The concentrations of the drug were determined by reverse phase high performance liquid chromatography. Results show that the mean (± SD) Absorption, Distribution, Metabolism and Excretion (ADME) of the drug plasma followed a tri-exponential process with Ka (minutes-1) were obtained at 5.10-2 ± 26.10-3, α (minutes-1), K12 (minutes-1) and K21 (minutes-1) were obtained at 18.10-3 ± 1.10-2, 14.10-3 ± 1.10-2 and 1.10-3 ± 1.10-3. The mean values of β (minutes-1) and K13 (minutes-1) were obtained at 1.4.10-4 ± 4. 10-5 and 3.10-3 ± 2.10-3. The mean values of Tmax (minutes) and Cmax (µg.ml-1) were obtained at 53.71 ± 30.61 and 13.40 ± 8.13. The mean values of Vds (L), Cl (ml.minutes-1), T1/2β(hours-1) and AUC0→∞ (µg.L-1.minutes) were obtained at 4.91 ± 3.12, 14.29 ± 4.08, 94.91 ± 33.23 and 12.680 ± 2.722. (Med J Indones 2006; 15:69-73) Keywords: Pharmacokinetics, Chagaz, Berenil, Veriben, Tri-exponential, AIC