Preparation of herpetrione nanosuspensions and preliminary study on its pharmacokinetics / 中国药学杂志

ABSTRACT

OBJECTIVE: To prepare herpetrione nanosuspension (PEDX-NS) and evaluate its pharmacokinetics in rats. METHODS: PEDX-NS was prepared by high pressure homogenization technology, and its morphology and mean diameter were determined. An HPLC method was employed to determine the concentration of herpetrione(PEDX), the index component of PEDX-NS, in plasma, and the bioavailability of the nanosuspension was compared with the reference formulation after oral administration in Wistar rats. RESULTS: The particles in the nanosuspension observed by scanning electron microscopy were irregular spheres, and the mean particle size of PEDX-NS was (238.6 ± 1.9)nm. Its pharmacokinetic process calculated with DAS2.0 software was fitted to a two-compartment model. The AUG was 25.19 μg · h · mL-1 and the pmax was 11.64 μg · mL-1, which were 2.47 and 2.63 times of the reference formulation, respectively (P < 0.01). CONCLUSION: It is feasible to prepare PEDX-NS by high pressure homogenization technology, and PEDX-NS can improve the bioavailability of PEDX notablely.