左旋和右旋奥硝唑在大鼠体内的药代动力学

Pharmacokinetics of ornidazole enantiomers in rats

目的:研究大鼠口服和静注左旋、右旋奥硝唑,比较两者药代动力学行为差异。方法:大鼠分别口服和静注左旋、右旋奥硝唑后,用HPLC法测定血浆中药物的浓度。色谱柱为Lichrospher C18柱,流动相为甲醇-0.4%HOAc(30∶70),流速0.8 mL/min,柱温40℃,紫外检测波长316 nm。结果:口服给药后,左旋、右旋奥硝唑的t1/2分别为2.49和3.42 h,AUC分别为168.21和207.19μg.h/mL,CL/F分别为0.11和0.09 L/h。静脉注射给药后,左旋、右旋奥硝唑的t1/2分别为2.19和3.23h,AUC分别为138.40和203.09μg.h/mL,CL分别为0.08和0.05 L/h。结论:左旋、右旋奥硝唑在大鼠体内的药代动力学行为存在一定的差异。

Aim：To compare the differences in the pharmacokinetics between omidazole enantiomers following oral and intravenous administration. Methods： Plasma levels of each of omidazole enantiomers after oral and intravenous separate administration of （S）-or （R）-omidazole （90 mg/kg） were determined by HPLC. Chromatographic analysis was performed on a Lichrospher C18 column with methanole-0.4% HAc （30：70） being used as the mobile phase at a flow rate ofO.8 mL/min. The column was maintained at 40℃ and UV detector set at 316 nm. Results： Following oral administration of the （S）-and/or （R）-omidazole （90 mg/kg）, t1/2 was estimated at 2.49 h for （S）-ornidazole and 3.42 h for （R）-omidazole. The calculated AUC were 168.21 and 207.19 μg·h/mL for （S）-and （R）- omidazole, respectively. And the estimated CL/F were 0.11 and 0.09 L/h for （S）-and （R）-omidazole, respectively. Following intravenous separate administration of （S）-and （R）-omidazole （54 mg/kg）, tl/2 were estimated to be 2.19 and 3.23 h, AUC were 138.40 and 203.09 μg·h/mL, and CL were 0.08 and 0.05 L/h for （ S ）- and （R）-enantiomers, respectively. Conclusion： There are differences in the phannacokinetics between （S）-and （R） -omidazole.