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 administration( 15 mg·kg- 1). Blood samples were collected at different intervals after the administration of derivative 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. Plasma concentration-time profiles of derivative BC-7013 were analyzed by using non-compartmental analysis Win Nonlin 5. 2 software. 【Result and conclusion】The main pharmacokinetical parameters of i. v. administration were as follows: t1 /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: tmax=( 1. 94 ± 0. 26) h,Cmax=( 126. 18 ± 6. 54) ng·m L- 1,AUC( 0→∞)=( 1. 38 ± 0. 21) μg·m L- 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.