Pharmacokinetic behavior of docetaxel lipid emulsion injection in rats / 中国药科大学学报

ABSTRACT

@#The aim of this study was to prepare and characterise docetaxel lipid emulsion injection and to conduct the characterization of its pharmacokinetics in rats after tail-vein injection. High pressure homogenization method was used to prepare docetaxel lipid emulsion. 12 Wistar rats were randomly divided into docetaxel lipid emulsion injection group and docetaxel injection group, and dosed at 6 mg/kg through tail-vein injection. Docetaxel concentration in plasma was determined by HPLC. The pharmacokinetic parameters of docetaxel in rats were obtained using the 3P97 program. Particle size, polydispersion index, Zeta potential of docetaxel lipid emulsion were found to be(221. 6±13. 4)nm, (0. 092±0. 003)and -30. 3 mV, respectively. t1/2(α) of docetaxel lipid emulsion injection and docetaxel injection were(0. 072±0. 014)and(0. 066±0. 015)h; t1/2(β) were(0. 573±0. 253)and(0. 432±0. 184)h; AUC0-12 h were(7. 98±1. 25)and(6. 26±1. 83)μg ·h/mL, respectively. Docetaxel lipid emulsion injection had similar pharmacokinetic characteristics to docetaxel injection. The pharmacokinetic data obtained for both preparations fitted a two-compartment model.