Study On Pharmacokinetics Of Maquindox In Rabbits With Experimental Hepatic And Renal Injury

This paper studied the Pharmacokinetics of Maquindox in rabbits. By establishing rabbit pathological models of hepatic and renal injury, the Pharmacokinetics between the healthy group and the pathological models were compared.1. The Pharmacokinetics of Maquindox in Healthy Rabbits Rabbits in group A were treated with a rapid intravenous injection of single-dosaged Maquindox (20 mg/kg). The blood samples were collected from heart 8 times within 6 hours after the injection. The concentrations of Maquindox in serum were detected by HPLC. The results showed that the disposition of Maquindox in rabbits matched with non-absorption one-compartment open model. And the optimal concentration-time equations of the two groups were: C control group = 25.5642e-0.3716t. The main pharmacokinetics parameters included: C0=(25.5642±4.4766)μg·mL-1, t1/2=(1.8973±0.2953)h, AUC=(68.9221±8.9627)μg·mL-1·h, kel=(0.3716±0.0493)h-1 , Vd=(0.8127±0.0282)L·kg-1, CLB=(0.3028±0.0475)L·kg-1·h-1. It shows that the distribution of Maquindox in vivo was broad, and the elimination of it in vivo was rapid.2. The Pharmacokinetics of Maquindox in Rabbits with Hepatic Injury 24 h before the experiment, the rabbits in group B were treated with a hypodermic injection of CCl4 (0.4 mL/kg) for replicating the hepatic injury model. After 24 h rabbits in group B were also treated with a rapid intravenous injection of single-dosaged Maquindox (20 mg/kg). The blood samples were collected from heart 8 times within 6 hours after the injection. The concentrations of Maquindox in serum were detected by HPLC. The results demenstrated that the disposition of Maquindox in the group with hepatic injury matched with non-absorption one-compartment open model. The optimal concentration-time equation was: C hepatic injury = 24.3089e-0.144t. Compared with the group A, t1/2 hepatic injury prolonged by 166.49%, kel hepatic injury decreased by 61.25%, CLB hepatic injury decreased by 54.95%, AUC hepatic injury increased by 155.87%. 3. The Pharmacokinetics of Maquindox in Rabbits with Renal Injury 24 h before the experiment, the rabbits in group C were treated with a hypodermic injection of 10 g/L HgCl2 (1.5 mL/kg) for replicating the renal injury model.. After 24 h rabbits in group C were also treated with a rapid intravenous injection of single-dosaged Maquindox (20 mg/kg). The blood samples were collected from heart 8 times within 6 hours after the injection. The concentrations of Maquindox in serum were detected by HPLC. The results indicated that the disposition of Maquindox in the group C with renal injury also matched with the non-absorption one-compartment open model. The optimal concentration-time equations of this group were: C renal injury = 20.0266e-0.0998t. Compared with group A, t1/2 renal injury prolonged by 276.16%, kel renal injury decreased by 73.14%, CLB renal injury decreased by 69.91%, AUC renal injury increased by 187.57%.