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目的本实验制备了herpetrione纳米混悬剂(PEDX-NS),并进行了大鼠体内药动学研究。方法采用高压均质法制备herpetrione纳米混悬剂,考察纳米混悬剂的形态及粒径分布。以herpetrione(PEDX)为指标成分,采用HPLC测定大鼠灌胃给药后的血药浓度,用DAS2.0药动学软件计算药动学参数。结果制得的纳米混悬剂呈不规则球形,平均粒径为(238.6±1.9)nm,多分散度指数为(0.183±0.017)。herpetrione在大鼠体内动力学行为符合二室模型。herpetrione纳米混悬剂药-时曲线下面积(AUC)为25.19μg.h.mL-1,达峰浓度(ρmax)为11.64μg.mL-1,与参比药herpetrione普通混悬剂(PEDX-S)相比,分别提高了2.47倍和2.63倍(P<0.01)。结论高压均质法制备herpetrione纳米混悬剂工艺简单可行,herpetrione纳米混悬剂能显著提高药物体内生物利用度。
Objective This experiment prepared herpetrione nanosuspension (PEDX-NS), and conducted pharmacokinetic studies in rats. Methods Herpetrione nanosuspension was prepared by high pressure homogenization and the morphology and particle size distribution of nanosuspension were investigated. Herpetrione (PEDX) was used as an index component to determine the plasma concentration after oral administration by HPLC. The pharmacokinetic parameters were calculated by DAS2.0 pharmacokinetic software. Results The resulting nanosuspension was irregular spherical with an average diameter of (238.6 ± 1.9) nm and a polydispersity index of (0.183 ± 0.017). Herpetrione behaves in a two-compartment model in rats. Herpetrione nanosuspension drug-time curve area (AUC) of 25.19μg.h.mL-1, the peak concentration (pmax) of 11.64μg.mL-1, and the reference drug herpetrione ordinary suspension (PEDX- S), respectively, increased 2.47 times and 2.63 times (P <0.01). Conclusion The preparation of herpetrione nanosuspension by high pressure homogenization is simple and feasible. Herpetrione nanosuspension can significantly improve the bioavailability of the drug in vivo.