Pharmacokinetics of tenvermectin in swine, a novel antiparasitic drug candidate—comparison with ivermectin

Abstract

Tenvermectin (TVM) is a novel 16-membered macrolide compound isolated and purified from the fermentation broth of genetically engineered Streptomyces avermitilis strain MHJ1011. TVM and ivermectin were administered at the dose of 0.3 mg/kg body weight through a single subcutaneous injection route followed by plasma collectiom and analysis at different time intervals. Plasma concentrations of TVM and IVM were determined by high-performance liquid chromatography with fluorescence detector. Pharmacokinetic analysis was completed using the non-compartmental method with WinNonlin™ 6.4 software. TVM is rapidly absorbed after administration with peak plasma concentrations (Cmax, 9.78 ± 2.34 ng/ml) obtained within 6–22 h. AUC0-last was 586.86 h·ng/ml ± 121.24 h·ng/ml. The mean elimination half-life of TVM (T1/2λz) was 97.99 h ± 46.41 h. The T1/2λz of IVM was 146.59 h ± 22.26 h in the study. The present study showed that subcutaneous administration of TVM at 0.3 mg/kg body weight (BW) in swine is absorbed more rapidly than IVM in swine. Compared to the pharmacokinetic characteristics of IVM, there was little difference in the half-life of TVM among different individuals. The data will contribute to refining the formulation and dosage regime for TVM administration.