Pharmacokinetics and tissue residues of hydrochloric acid albendazole sulfoxide and its metabolites in crucian carp (Carassius auratus) after oral administration

文献类型： 外文期刊

第一作者： Li, Zaijian

作者： Li, Zaijian;Chen, Cuilan;Wang, Chunmei;Li, Jing;Qi, Yuanhua;Yi, Weixue;Shen, Hongchun;Cao, Jiyue;Ai, Diyun

作者机构：

关键词： Crucian carp;HCl albendazole sulfoxide;Metabolites;Pharmacokinetics;Residues

期刊名称：ENVIRONMENTAL TOXICOLOGY AND PHARMACOLOGY （ 影响因子：4.86； 五年影响因子：4.462 ）

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收录情况： SCI

摘要： The pharmacokinetics and residues elimination of hydrochloric acid albendazole sulfoxide (ABZSO) and its metabolites were studied in healthy crucian carp (Carassius auratus, 250±30g) kept at water temperatures of 10°C and 25°C. The concentrations of ABZSO and its metabolites concentration in plasma and tissues were determined using high-performance liquid chromatography (HPLC) using an ultraviolet detector. The results revealed that the plasma concentration of ABZSO in plasma was significantly higher than that of albendazole sulfone (ABZSO 2), whereas Albendazole-2-aminosulfone (ABZ-SO 2NH 2) was not detected. The plasma concentrations of ABZSO and its main metabolite ABZSO 2 concentration-time data were fitted using a single-compartment model at 10°C and 25°C. The absorption half-life (t1/2 ka) of ABZSO was 3.86h at 10°C and 1.29h at 25°C, whereas the elimination half-life (t1/2 ke) was 16.34h at 10°C and 6.72h at 25°C; the maximum plasma concentration (C max) and the time-point of maximum plasma concentration (T p) were calculated as 3.20μgmL -1 and 10.58h at 10°C, 4.39μgmL -1 and 3.80h at 25°C. The distribution volume (V d/F) of ABZSO was estimated to be 1.99Lkg -1 at 10°C and 1.53Lkg -1 at 25°C; the total body clearance (CL b) of ABZSO were computed as 0.08 and 0.19L/(hkg) at 10 and 25°C, respectively; the areas under the concentration-time curve (AUC) was 118.22μgmL -1h at 10°C and 63.12μgmL -1h at 25°C. The t1/2 ka of ABZSO 2 was found to be 6.39°C at 10°C and 3.73h at 25°C, whereas the t1/2 ke was 12.86h at 10°C and 6.56h at 25°C; the C max and T p of ABZSO 2 was calculated as 0.78μgmL -1 and 12.82h at 10°C, 1.03μgmL -1 and 7.04h at 25°C, respectively; the V d/F of ABZSO 2 were estimated to be 6.43Lkg -1 at 10°C and 4.61Lkg -1 at 25°C; the CL b of ABZSO 2 were computed as 0.34 and 0.49L/(hkg) at 10°C and 25°C, respectively; the AUC of ABZSO 2 were 28.86μgmL -1h at 10°C and 20.52μgmL -1h at 25°C. It was demonstrated that ABZSO 2 was the main metabolite of ABZSO. The concentrations of ABZSO and its main metabolite (ABZSO 2) were detected in muscle, skin, liver and kidney, whereas ABZ-SO 2NH 2 was only detected in liver and kidney. The ABZSO and it metabolite (ABZSO 2) could still be detected at 4 d time-point after administration at both temperatures in all tissues. The results revealed that the depletion of ABZSO and its metabolite (ABZSO 2) in crucian carp was slower with a long half-life time, especially at lower water temperature.

分类号： R9

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