数字农科院2.0

The pharmacokinetics of nitazoxanide active metabolite (tizoxanide) in goats and its protein binding ability in vitro

文献类型： 外文期刊

作者： Zhao, Z.;Xue, F.;Zhang, L.;Zhang, K.;Fei, C.;Zheng, W.;Wang, X.;Wang, M.;Zhao, Z.;Meng, X.;Zhao, Z.;Xue, F.;Zhang, L.;Zhang, K.;Fei, C.;Zheng, W.;Wang, X.;Wang, M.;Zhao, Z.;Meng, X.

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期刊名称： JOURNAL OF VETERINARY PHARMACOLOGY AND THERAPEUTICS

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收录情况： SCI

摘要： Zhao, Z., Xue, F., Zhang, L., Zhang, K., Fei, C., Zheng, W., Wang, X., Wang, M., Zhao, Z., Meng, X. The pharmacokinetics of nitazoxanide active metabolite (tizoxanide) in goats and its protein binding ability in vitro. J. vet. Pharmacol. Therap.33, 147-153. The pharmacokinetics of tizoxanide (T), the active metabolite of nitazoxanide (NTZ), and its protein binding ability in goat plasma and in the solutions of albumin and l-1-acid-glycoprotein were investigated. The plasma and protein binding samples were analyzed using a high-performance liquid chromatography (HPLC) assay with UV detection at 360 nm. The plasma concentration of T was detectable in goats up to 24 h. Plasma concentrations vs. time data of T after 200 mg/kg oral administration of NTZ in goats were adequately described by one-compartment open model with first order absorption. As to free T, the values of t/Ka, t/Ke, Tmax, Cmax, AUC, V/FcZ, and ClsZ were 2.51 pl 0.41 h, 3.47 pl 0.32 h, 4.90 pl 0.13 h, 2.56 pl 0.25 og/mL, 27.40 pl 1.54 (og/mL) x h, 30.17 pl 2.17 L/kg, and 7.34 pl 1.21 L/(kg x h), respectively. After o-glucuronidase hydrolysis to obtain total T, t/ke, Cmax, Tmax, AUC increased, while the V/FcZ and ClsZ decreased. Study of the protein binding ability showed that T with 4 og/mL concentration in goat plasma and in the albumin solution achieved a protein binding percentage of more than 95%, while in the solution of l-1-acid-glycoprotein, the percentage was only about 49%. This result suggested that T might have much more potent binding ability with albumin than with l-1-acid-glycoprotein, resulting from its acidic property.

分类号： S85

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