Research on pharmacokinetics and bioavailability of pleuromutilin derivative BC-7013 in chickens

Objective The pharmacokinetical characteristics and bioavailability of pleuromutilin derivative BC-7013 in chickens were investigated.

Method Twenty chickens were randomly divided into two groups for pharmacokinelical experiments after a single intravenous(2.5 mg·kg^-1) and oral administra tion(15 mg·kg^-1).Blood samples were collected at different intervals after the administration of deriv ative BC-7013.The concentrations of derivative BC-7013 in plasma were determined by high-performance liquid chromatography-tandem mass spectrometry(HPLC-MS /MS) with internal standard method.Plas ma concentration-time profiles of derivative BC-7013 were analyzed by using non-compartmental analysis WinNonlin 5.2 software.

Result and conclusion The main pharmacokinetical parameters of i.v.ad ministration were as follows: t_1/2β=(1.37 ± 0.14) h, Vd=(1.87 ± 0.25) L·kg^-1, AUC_(0→∞)=(2.83 ± 0.56) μg·L^-1·h, CL=(1.14 ± 0.28) L·h^-1·kg^-1.The major pharmacokinetical parameters of oral administration were as follows: t_max=(1.94 ± 0.26) h, C_max=(126.18 ± 6.54) ng·mL^-1, AUC_(0→∞)=(1.38 ± 0.21) μg·mL^-1·h, MRT=(9.49 ± 0.57) h, F=(10.37 ± 1.48) %. The results show that the pharmacokinetical characteristics of pleuromutilin derivative BC-7013 in healthy chicken manifest wide distribution, rapid elimination as well as incomplete absorption and low oral bioavailability.