克班宁注射剂在家兔体内的药动学研究

目的：建立血清中克班宁(crebanine,Cre)浓度的高效液相测定方法,探讨克班宁注射剂在家兔体内的药动学过程。方法：家兔按2.0 mg·kg^-1量耳缘静脉注射克班宁后5,10,20,30,50,70,90,110 min采血,用HPLC测定血清中克班宁浓度,以DAS软件拟合药动学参数。结果：克班宁平均回收率分别为(89.4±2.5)%,(105.4±4.1)%,(102.7±5.8)%；精密度分别为日内RSD 2.8%,3.9%,5.6%；日间RSD分别为8.2%,6.8%,7.2%。克班宁注射剂在家兔体内成二室模型,雌、雄兔体内的药动学参数经t检验差异无显著性意义。主要药动学参数为：t_1/2α=(3.246±0.222) min,t_1/2β=(36.675±5.525) min,C_max=(1.401±0.063) mg·L^-1,V_d=(5.928±0.877) L·kg^-1,Cl=(0.051±0.003) L·min^-1·kg^-1。结论：克班宁静注在家兔体内为超速处置类(t_1/2<1 h)药物,其在体内的分布迅速、广泛。

Study on pharmacokinetics of Crebanine injection in rabbits

OBJECTIVE: To develop an HPLC method for the determination of serum level of Crebanine (Cre) and study on the pharmacokinetics of Cre injection in rabbits. METHOD: To sample blood serum from the rabbits' ears which were injected the Cre by 2.0 mg x kg(-1) at different time and use HPLC to determine the concentration of Cre in it, the pharmacokinetic parameters were accessed by the DAS software. RESULT: Cre was fitted to a two compartment open pharmacokinetic model in rabbits. There was no signifiant difference between the male and female rabbits'pharmacokinetic by t-test. The mainly pharmacokinetic parameters were: t1/2alpha = (3. 246 +/-0.222) min, t1/2beta = (36.67+/-5.52) min, Cmax = (1.401 +/- 0.062) mg x L(-1), Vd = (5.928 +/- 0.877) L x kg(-1), Cl = (0. 051 +/-0.003) L x min(-1) x kg(-1). CONCLUSION: This experiment can objectively show the pharmacokinetics regularity of Crebanine injection in rabbits. Crebanine injection was a speeding disposition drug (t1/2 <1 h) and disposed extensively and rapidly in rabbits.