芬苯达唑微晶体在猪体内的药物动力学试验

Pharmacokinetics of Fenbendazole nanocrystals in pigs

本试验以芬苯达唑（FBZ）原料药为对照,考察芬苯达唑微晶体对猪口服给药后FBZ的药动学特征。在0.02-2μg/m L的线性关系良好,相关系数为0.9990。FBZ在猪血浆中的回收率均在70%以上,日内变异系数小于5%,日间变异系数小于10%。芬苯达唑原料组和芬苯达唑微晶体组的主要药物动力学参数为：吸收半衰期（T1/2α）分别为1.65 h和1.07 h,消除半衰期（T1/2β）分别为28.28 h和33.92 h;药时曲线下面积（AUC）分别为29.09μg·h/m L和41.12μg·h/m L。经统计学分析得知,T1/2α、Tp、T1/2β、AUC差异显著（P〈0.05）。表明芬苯达唑微晶体能够改变芬苯达唑在动物体内的药动学特征,提高芬苯达唑的吸收速度,延长药物在体内的有效作用时间。

The present study was designed to investigate the pharmacokinetics of Fenbendazole nanocrystals in pigs with ad-ministered orally as the reference preparation.The correlation of calibration curve was good,and the correlation coefficient was0.9990. The average extraction recovery was more than 70% of FBZ from plasma. The intra-day coefficient of variations was lessthan 5%,and the inter-day coefficient of variations was less than 10%.Pigs were administered orally with a single dose of 10 mg/kg body weight of Fenbendazole nanocrystals and Fenbendazole in the Fenbendazole nanocrystals and Fenbendazole group,respec-tively. The absorption half-lives（T1/2α）of Fenbendazole nanocrystals and Fenbendazole were 1.07 and 1.65 h,respectively. Theelimination half-lives（T1/2β）were 33.92 and 28.28 h,The areas under the concentration-time curve（AUC）were 41.12 and 29.09μg·h/m L,respectively. Statistical analysis showed that these follow parameters were significantly different between the Fenbenda-zole nanocrystals and Fenbendazole（P〈0.05）. The pharmacokinetics study indicated that Fenbendazole nanocrystals equallyshowed rapid absorption,high bioavailability and slow elimination.