大黄酸在刺参体内的药代动力学研究

Pharmacokinetics studies on rhein in Apostichopus japonicus

中文关键词: 大黄酸  刺参  药代动力学  高效液相色谱

英文关键词: Rhein  Apostichopus japonicus  Pharmacokinetics  HPLC

中文摘要:

      利用高效液相色谱（HPLC），对刺参(Apostichopus japonicus)体腔注射大黄酸（Rhein）后的药代动力学进行研究。以5.33mg/kg的剂量给刺参体腔注射大黄酸，测定大黄酸在其体腔液、呼吸树、肌肉、体壁中的药物浓度时间变化。结果表明：大黄酸在上述四种组织中的达峰时间(Tmax)分别为0.26、0.67、0.54和0.88h；消除半衰期(T1/2b)分别为6.24、26.1、71.48和8.93h；药时曲线下总面积(AUC)分别为69.29、105.6、132.38、20.99mg/L*h。除体壁中的大黄酸代谢规律符合一级吸收一室模型外，大黄酸在其它三种组织中均符合一级吸收二室模型。以上研究表明，体腔注射大黄酸后，药物在刺参体内吸收快，在各组织中能迅速达到峰值，消除半衰期长，代谢慢，主要经呼吸树排出体外。

英文摘要:

      Studies were conducted on the pharmacokinetics of rhein in Apostichopus japonicus. Coelomic fluid, respiratory trees, muscle and integument were sampled after coelomic injecting with a single dose of rhein 5.33mg/kg. The contents of rhein were determined by high performance liquid chromatography. The results showed that the peak time (Tmax), elimination half-time (T1/2b) and the area under the concentration-time curve (AUC) in Coelomic fluid, respiratory trees, muscle and integument were as follows: Tmax 0.26, 0.67, 0.54 and 0.88h ; T1/2b6.24, 26.1, 71.48 and 8.93h; AUC 69.29, 105.6, 132.38 and 20.99mg/L*h. The concentration-time course of rhein in coelomic fluid, respiratory trees and muscle could be described by a two-compartment model, except for the course in integument being described by a one-compartment model. These results are suggesting that rhein can reach the peak time with a high speed absorption in Apostichopus japonicus after injection, while it is slowly metabolized with a long elimination half-time. Rhein is mainly excreted from respiratory trees.