Linearity of eprinomectin pharmacokinetics in lactating dairy sheep following pour-on administration: excretion in milk and exposure of suckling lambs.

摘要

Pharmacokinetics of eprinomectin (EPR) were studied in blood plasma and milk in two groups of six Istrian Pramenka dairy sheep and their suckling lambs following pour-on administration of EPR to ewes at dose levels of 0.5 and 1mg/kg. Maximum concentration in plasma was 2.22 and 5.25 microg/l, and AUC was 13.6 and 33.7 microg day/l for the 0.5 and 1.0mg/kg dose, respectively. These results indicate that drug exposure with a dose of 0.5mg/kg, which is commonly used in cattle, may be subtherapeutic. The concentration time course in milk paralleled plasma concentrations. In the dose range studied, linear pharmacokinetics of EPR were demonstrated. Milk-to-plasma AUC ratio was 0.79+/-0.12 and 1.12+/-0.43; the fraction of dose recovered in milk was 0.037+/-0.011 and 0.058+/-0.027% for the low and high dose, respectively. Maximum residual levels in milk were below the maximum acceptable level of 20 microg/kg; however, EPR was detected in all samples investigated. Despite low permeability in milk, AUC in plasma of suckling lambs was between 20 and 30% of the AUC in plasma of ewes.