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A novel PVP coated norcantharidin-chitosan nanoparticles (PVP-NCTD-NPs) formulation with an average particle size of 140.03 ± 6.23 nm, entrapment efficiency of 56.33 ± 1.41％ and drug loading efficiency of 8.38 ± 0.56％, was obtained through ionic gelation. The pharmacokinetics and metabolites of norcantharidin (NCTD) and PVP-NCTD-NPs were analyzed by a rapid and specific LC/MS/MS method. According to the pharmacodynamical study of both formulations on oral and intravenous administration, it was revealed that the relative bioavailability were 173.3％ and 325.5％, respectively. After oral administration of PVP-NCTD-NPs, a prototype drug and a metabolite were found in the feres and seven metabolites in the urine. These results indicated that PVP-NCTD-NPs formulation enhanced the therapeutic effect more adequately, and decarboxylation and hydroxylation were the main metabolic pathway of NCTD, whose metabolites were excreted into rat kidney and finally into urine.