凡纳滨对虾体内大黄苷的药代动力学特征

Pharmacokinetic Characteristics of Rhein in the Body of Penaeus vannamei

【目的】研究大黄苷(Rhein)在凡纳滨对虾体内的吸收、分布和代谢规律,并制定临床给药方案。【方法】以5mg/kg剂量的大黄苷一次性肌肉注射凡纳滨对虾,利用高效液相色谱(HPLC)检测其在凡纳滨对虾血淋巴、肝胰脏、肌肉和鳃组织中的药物浓度-时间变化,并通过3P87软件进行数据处理,分析其在凡纳滨对虾体内的药代动力特征。【结果】大黄苷在4种组织里的达峰时间(Tmax)较早,分别为0.17h、2.73h、0.44h、0.23h;消除半衰期(T_(1/2Ke))较短,分别为2.13h、2.36h、3.12h、3.72h;在房室模型选择上,大黄苷在4种组织中的最适药动模型均符合一级吸收一室模型。【结论】肌注大黄苷后,药物在凡纳滨对虾各组织中分布广泛、吸收快、清除能力强。大黄苷在凡纳滨对虾鳃部的浓度较高,这为利用其治疗凡纳滨对虾烂鳃病提供理论依据。

【Objective】The absorption,distribution and metabolism of rhein in Penaeus vannamei were studied,and the clinical dosing regimen was established.【Methods】We analysed the pharmacokinetics of rhein in Penaeus vannamei,blood,hepatopancreas,muscle and gill were sampled after muscle injecting with a single dose of rhein（5mg/kg）,the contents of rhein was determined by HPLC,and 3P87 software were used to analyse the data processing.【Results】Rhein in four kinds of tissue in the peak time（Tmax）early and were 0.17 h,2.73 h,0.44 h,0.23h;elimination half-life（T1/2Ke）short were 2.13 h,2.36 h,3.12 h,3.72h;in compartment model choice,the four organizations rhein optimum pharmacokinetic model are suitable for a one-compartment model.【Conclusion】Rhein after intramuscular injection,the drug vannamei tissues peak time is short,wide distribution,rapid absorption,strong scavenging ability.The concentration of rhein vannamei gills is high,which provides a theoretical basis for using it to treat gill disease of Penaeus vannamei.