大黄酸在刺参体内的药代动力学研究

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了研究。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4种组织中的达峰时间(Tmax)分别为0.26、0.67、0.54、0.88h;消除半衰期(T1/2β)分别为6.24、26.1、71.48、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,大黄酸在其他3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。

Pharmacokinetics studies on rhein in Apostichopus japonicus

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.