丙硫咪唑在鸡体内的药代动力学及组织残留的研究

The Study on the Pharmacokinetics and Tissue Residue of Albendazole in Chickens

给鸡单剂量口服丙硫咪唑(15mg/kg),用HPLC法测定不同时间的鸡体内药物及其代谢物的浓度.结果,在血浆和组织中均未发现丙硫咪唑,而其两个代谢物丙硫咪唑亚砜(亚砜)和丙硫咪唑砜(砜)在血浆中的药代动力学行为符合方程:C(亚砜)=22.3581(e^(-0.142(t-0.6053))-e^(-0.4505(t-0.8053)));C(砜)=4951.7774(e^(-0.2769(t-0.9111))-e^(0.278(t-0.9111)))。亚砜和砜的主要药动学参数分别为:消除相半衰期(t1/2ke)为4.87和2.57h,表观分布容积(Vd)为0.98和0.76L/kg,峰时间(Tm)为4.34和4.52h,峰浓度(Cm)为8.98和7.22μg/mL。亚砜在心、肝、胰、肺、肾等组织中的残留量:给药后3d分别为1.14、5.35、2.42、1.78、2.45μg/g;5d分别为0.281.79、2.34、1.13、1.16μg/g;7d分别为0.12、0.68、1.69、0.48、0.69μg/g.砜在上述组织中的残留量:给药后3d分别为3.15、10.44、8.16、0.99、2.83μg/g;5d分别为1.53、1.04、4.11、0.86、0 89μg/g;7d分别为:0.77、0.67、2.09、0.53、0.12μg/g。

The concentrations of albendazole and its two major meta-bolites, the sulfoxide and sulfone, in plasma and tissues of chicken,which had been administered orally with albendazole suspension at dos-age of 15mg/kg body weight, were determined by HPLC. The pharmaco-kinetic parameters of albendazole sulfoxide and albendazole sulfone areas follows: the elimination half-life: 4.87 and 2.50 h; the apparentvolume of distribution: 0.98 and 0.76L/kg; the peak time: 4.34 and4.52 h; the peak concentration: 8.98 and 7.22 μg/mL, respectively. Thetissue residues of albendazole sulfoxide in heart muscle, liver, pancreas,lung and kidneys are 1.14, 5.35, 2.42, 1.78, 2.45 μg/g 3 days afteradministration; 0.28, 1.79, 2.34, 1.13, 1.16 μg/g after 5 days,and 0.12,0.68, 1.69, 0.48, 0.68μg/g, after 7 days, respectively. The albendazolesulfone residues in the aforementioned tissues are 3.15, 10.44, 8.16, 0.99,2.83 μg/g 3 days after administration; 1.53, 1.04, 4.11, 0.86, 0.89 μg/gafter 5 days, and 0.77, 0.67, 2.09, 0.53, 0.12 μg/g after 7 days,,respe-ctively.