Abstract: The pharmacokinetics and tissue distribution of the prepared docetaxel SBE-β-cyclodextrin inclusion complex (test preparation) and the commercial formulation (reference preparation) in rats were studied.After iv administration of test and reference preparations,the concentrations of docetaxel in rats plasma and tissue were determined by LC-MS/MS.The results showed that after a single iv administration of 10 mg/kg test and reference preparation to rats,the pharmacokinetic parameters of docetaxel were as follows:t_1/2 （3.4±0.9）and （4.0±1.0） h,Vz （31.999±14.16）and （35.526±7.218）L/kg,AUC_0-∞ (1 690±476) and (1 629±213) μg ·h/L.It was fit for two-compartment model.And after a single iv administration of 10 mg/kg test and reference preparation in rats,the concentration levels of docetaxel were higher in the bone marrow,lung,and spleen,and lower in the brain,fat and testes.Statistical analysis showed that there was no significant difference (P>0.05) between the test and reference preparations in major pharmacokinetic parameters and tissue distribution data in rats.