静脉注射根皮苷后在大鼠体内的药代动力学研究

Pharmacokinetics of phloridzin after intravenous administration in rats

目的:本实验旨在建立新的HPLC检测方法,探讨静脉注射根皮苷后的药代动力学特征,研究未经消化道处理的根皮苷在体循环中的代谢情况。方法:实验采用18只Wistar大鼠,分5、10和20 mg/kg三个剂量进行实验,麻醉后进行颈静脉给药,4 h内持续采血,样品经高效液相色谱法进行分析。结果:根皮苷经静脉注射后,体内AUC0-t分别为(66.4±39.1)mg·L^(-1)·min^(-1)、(333.1±91.2)mg·L^(-1)·min^(-1)和(516.4±249.3)mg·L^(-1)·min^(-1),t1/2分别为(74.5±27.2)min、(62.3±21.4)min和(75.0±47.2)min,Cmax值分别为(6.4±2.4)mg/L、(24.9±6.6)mg/L和(45.0±11.2)mg/L。结论:结果表明根皮苷经静脉注射后,在体内利用率明显高于口服给药,为根皮苷的临床药用开发和利用提供参考。

AIM： To investigate the pharmacokinetics of intravenous injection of phloridzin,and to study the metabolism of the phloridzin in the body circulation without the treatment of the digestive tract by establishing a new HPLC detection method.METHODS： The experiment used 18 Wistar rats,with six per group. After anesthesia,three doses of5,10 and 20 mg / kg were administration via jugular. The blood samples were collected in 4 hours.The samples were analyzed by high performance liquid chromatography. RESULTS： After intravenous injection of phloridzin, the value of AUC0-twere（ 66. 4 ± 39. 1） mg·L^-1·min^-1,（ 333. 1 ± 91. 2）mg·L^-1·min^-1and（ 516. 4 ± 249. 3） mg · L^-1·min^-1,t1 /2were（ 74. 5 ± 27. 2） min,（ 62. 3 ±21. 4） min and（ 75. 0 ± 47. 2） min,Cmaxwere（ 6. 4 ± 2. 4） mg /L,（ 24. 9 ± 6. 6） mg /L and（ 45. 0 ± 11. 2） mg /L. CONCLUSION： The results showed that the utilization rate of the phloridzin after intravenous injection was higher than that of oral administration,and it was a reference for the development and utilization of the medicine.