目的比较白芍总苷在急性CCl4肝损伤大鼠与正常大鼠体内药物动力学过程的异同,为临床合理用药提供参考。方法采用一次性腹腔注射CCl4建立大鼠急性肝损伤模型,采用HPLC测定模型大鼠和正常大鼠灌胃给予白芍总苷后,不同时间点的Pae和Alb的血药浓度,根据药-时曲线计算药代动力学参数。结果在模型组大鼠体内,白芍总苷中芍药苷(Pae)和芍药内酯苷(Alb)在高、中、低剂量(0.047、0.141、0.282 g.mL-1)时的t1/2分别为5.02、4.52、4.91 h;5.22、5.04、5.05 h。ρmax分别为22.54、14.52、5.49μg.mL-1;9.02、5.04、2.34μg.mL-1。AUC0-t分别为(146.55±7.52)、(84.14±7.84)、(31.62±2.97)μg.h.mL-1;(56.56±8.70)、(32.18±3.49)、(13.48±1.66)μg.h.mL-1。tmax均为2 h。在正常大鼠体内,Pae和Alb在高、中、低剂量(0.047、0.141、0.282 g.mL-1)时的t1/2分别为3.95、3.69、3.95 h;3.74、3.98、3.79 h。ρmax分别为19.16、11.60、4.46μg.mL-1;7.16、4.00、1.93μg.mL-1。AUC0-t分别为(116.26.6±19.99)、(67.74±12.79)、(25.01±2.62)μg.h.mL-1;(45.03±5.84)、(27.26±3.57)、(10.59±1.86)μg.h.mL-1。tmax为2.5 h。结论与正常组比较,模型组的ρmax、AUC0-t显著增大,t1/2延长,tmax明显缩短。模型组和正常组的tmax和t1/2不受白芍总苷剂量影响,但剂量与ρmax和AUC0-t具一定的相关性。 Objective To compare the similarities and differences of pharmacokinetics of total glucosides of paeony in acute CCl4-induced liver injury and normal rats, and to provide a reference for rational clinical use. Methods Acute hepatic injury model was established by intraperitoneal injection of CCl4. The plasma concentrations of Pae and Alb at different time points after oral administration of total glucosides of paeony were measured by HPLC in both model and normal rats. Curves calculate pharmacokinetic parameters. Results In the model group, the total titers of paeoniflorin (Pae) ​​and albocide lactone (Alb) were higher than those at the high, medium and low doses (0.047,0.141,0.282 g.mL-1) Respectively 5.02,4.52,4.91 h; 5.22,5.04,5.05 h. ρmax were 22.54,14.52,5.49μg.mL-1; 9.02,5.04,2.34μg.mL-1. AUC0-t were (146.55 ± 7.52), (84.14 ± 7.84), (31.62 ± 2.97) μg.h.mL-1; (56.56 ± 8.70), (32.18 ± 3.49), (13.48 ± 1.66) μg.h .mL-1. tmax is 2 h. In normal rats, t1 / 2 of Pae and Alb were 3.95, 3.69, 3.95 h, 3.74, 3.98, 3.79 h at high, medium and low dose (0.047,0.141,0.282 g.mL-1) respectively. ρmax 19.16, 11.60, 4.46 μg.mL-1, 7.16, 4.00, 1.93 μg.mL-1, respectively. AUC0-t were (116.26.6 ± 19.99), (67.74 ± 12.79), (25.01 ± 2.62) μg.h.mL-1; (45.03 ± 5.84), (27.26 ± 3.57), (10.59 ± 1.86) μg .h.mL-1. tmax is 2.5 h. Conclusion Compared with the normal group, the ρmax and AUC0-t of the model group increased significantly, t1 / 2 prolonged, tmax significantly shortened. The tmax and t1 / 2 of model group and normal group were not affected by total glucosides dose of paeony, but the dose had some correlation with ρmax and AUC0-t.