Abstract: AIM: To investigate the pharmacokinetics (PK) of 10-hydroxycamptothec (HCPT) nanoparticle injection iv by comparing with the HCPT common injection in rabbits.METHODS: HCPT in plasma were quantitated by reversed-phase HPLC and UV detector.3p97 software was used in calculation of compartment model and PK parameters.RESULTS: The concentration-time profile of HCPT nanoparticle injection was best described by three-compartment model, and the common injection was described by two-compartment model.Plasma peak concentration (C_max) of HCPT common injection was three times as many as that of nanoparticle injection in equal dosage.Area under curve (AUC) of HCPT common injection was twofold higher than that of nanoparticle injection.Apparent volume of distribution of central compartment (Vc) of HCPT nanoparticle injection was greater than that of nanoparticle injection in equal dosage.HCPT nanoparticle injection had a longer elimination half life (T_1/2β) than that of common injection.CONCLUSIOM: The blood drug concentration and PK characteristic of HCPT nanoparticle injection were very different from HCPT common injection in rabbits.

Key words: antineoplastic agent, 10-hydroxycamptothec, nanoparticle, pharmacokinetics, blood drug level