注射用双黄连中连翘苷的药代动力学研究

Study on Pharmacokinetics of Phillyrin in Shuanghuanglian for Injection

目的:探讨注射用双黄连中连翘苷在大鼠体内的血药浓度及药代动力学。方法:SD系大鼠尾静脉注射双黄连后,于不同时间点采血,采用反相高效液相色谱法测定大鼠体内连翘苷的血药浓度,应用DAS 2.0软件计算药代动力学参数。结果:连翘苷在大鼠体内主要药代动力学参数为:t1/2(α)(0.44±0.06)h、t1/2(β)(2.77±0.36)h、V1(0.09±0.01)L/kg、CL(0.09±0.007)L/(h.kg)、AUC0～t(5.56±0.47)mg.h/L、AUC0～∞(6.44±0.53)mg.h/L。结论:连翘苷在大鼠体内符合二室开放模型,其特点为分布快、消除缓慢。

Objective： To study the plasma concentration and pharmacokinetics of phillyrin in Shuanghuanglian for injection in rats.Methods： SD rats were given Shuanghuanglian for injection by iv,blood samples were collected at different time.The phillyrin concentration in plasma was determined by RP-HPLC.The parameters of pharmacokinetics were analyzed by program DAS 2.0.Results：The main pharmacokinetics parameters of phillyrin in rats： t1/2（α）（0.44 ± 0.06） h、t1/2（β）（2.77 ± 0.36） h、V1（0.09 ± 0.01） L/kg、CL（0.09 ± 0.007） L/（h·kg） 、AUC0～t（5.56 ± 0.47 mg·h/L） 、AUC0 ～∞（6.44 ± 0.53） mg·h/L.Conclusion： Phillyrin has two compartment model in rats,the pharmacokinetics of phillyrin characteristic is a process of rapid dispatching and slow elimination in rats.