地龙提取液抗凝效量与毒量药动力学参数的估测

Estimation of apparent pharmacokinetic parameters of anticoagulant and toxic components of earthworm extract

以地龙液注入兔静脉,按药效-对数剂量折算法进行效量药动力学参数估计,结果表明地龙抗凝成分注入体内属一级动力学消除,呈二室模型,α相 T 1/2为4.1min,β相 T 1/2为140min。将地龙液注入小鼠腹腔,按动物急性死亡率法估测毒量药动力学参数,结果表明地龙毒性成分注入体内亦属一级动力学消除,但呈一室模型,T 1/2为31.2min。

Apparent pharmacokinetic parameters(APKPs)of anticoagulant and toxic components ofearthworm extract were estimate.The APKPs ofanticoasulant components of earthworm extractwere determined by the method of effect-log dosetransformation.The results obtained from the rab-bits injected intravenously with earthworm extractshowed that the effective components were elimi-nated as first-order kinetics,and its distribution ap-peared to be two-compartment model and the T(1/2)αand T(1/2)β were estimated to be 4.1 minutes and 2.3hours respectively.The APKPs of the toxic compo-nents of earthworm extract were determined by themethod of acute mortality.The results obtainedfrom mice administrated intraperitoneally withearthworm extract demonstrated that this compo-nent was also eliminated as an first-order kinetics,and its distribution appeared to be one-compartmentmodel and the T(1/2) was 0.52 hour.