地克珠利在鲫体内的药代动力学研究
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林丽聪(1982-),女,硕士,高级工程师,研究方向为水产品药物代谢动力学与质量安全, linlicong82@163.com

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现代农业产业技术体系建设专项资金(CARS-46-35)


Pharmacokinetics of diclazuril in Carassius auratus
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    摘要:

     在(25±1) ℃水温条件下,按照鲫体质量为3.0 mg/kg的剂量,混饲投喂地克珠利,每天1次,连用5 d,并于第5天投喂后0.5、1、1.5、2、3、5、7、10、12、15、18、24、36、48、72、120、240、360、480、720、1 080、1 440、2 160、2 880、3 600 h采集鲫的血浆和肌肉样品,用高效液相色谱法测定血浆和肌肉中的药物浓度,研究了地克珠利在鲫体内的药代动力学特征。结果表明,鲫混饲投喂地克珠利后,其血浆和肌肉中地克珠利经时过程均符合一级吸收二室开放模型,其理论方程分别为C血浆=9.89e-6.710E-3t+3.66e-9.04E-4t-0.74e-4.379t,C肌肉=1.026e-6.379E-2t+0.1001e-1.53E-2t-1.82e-5.566t。鲫血浆和肌肉的达峰时间(Tmax)分别为11.11和11.00 h,峰浓度(Cmax)分别为30.58和1.108 mg/L,药时曲线下面积(AUC)分别为16 783和20.05 mg/(L·h ),消除半衰期(T1/2β)分别为827.6、45.41 h。实验结果表明地克珠利在鲫体内代谢缓慢。本研究为鲫的实际养殖过程中合理使用地克珠利提供理论依据,同时也为地克珠利在其他水产品中残留量的测定及药代动力学的研究提供技术支持。

    Abstract:

     At water temperature of (25±1) ℃, Carassius auratus was treated by oral administration of diclazuril in dose of 3 mg/kg once a day for 5 d. The concentration of diclazuril in the plasma and muscle of Carassius auratus at 0.5, 1, 1.5, 2, 3, 5, 7, 10, 12, 15, 18, 24, 36, 48, 72, 120, 240, 360, 480, 720, 1 080, 1 440, 2 160, 2 880 and 3 600 h after feeding were determined by high performance liquid chromatography, and the pharmacokinetics of diclazuril in Carassius auratus were studied.The results showed that following oral administration, the plasma and muscle concentration-time course of diclazuril both conformed to a two-compartment open model with the first order absorption. The pharmacokinetic equations were as follows, Cplasma=9.89e-6.710E-3t+3.66e-9.04E-4t -0.74e-4.379t, Cmuscle=1.026e-6.379E-2t+0.1001e-1.53E-2t-1.82e-5.566t. The time to peak (Tmax) of diclazuril in plasma and muscle were 11.11 and 11.00 h, respectively, and the peak concentration (Cmax) were 30.58 and 1.108 mg/L, respectively, and the area under the concentration-time curve (AUC) were 16 783 and 20.05 mg/(L·h ), respectively, and the elimination half-life(T1/2β)were 827.6 and 45.41 h, respectively.The results showed that diclazuril was eliminated slowly from Carassius auratus. This study provided theoretical basis for the actual breeding of Carassius auratus with diclazuril, and  technical support for the determination of residues and pharmacokinetic study of diclazuril in the other aquatic products.

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林丽聪,樊海平*,廖碧钗,等.地克珠利在鲫体内的药代动力学研究[J].中国渔业质量与标准,2017,7(1):16-21. LIN Licong, FAN Haiping*,LIAO Bichai, et al. Pharmacokinetics of diclazuril in Carassius auratus[J]. Chinese Fishery Quality and Standards,2017,7(1):16-21.

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