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目的 观察甘氨双唑钠 (CMNa)在动物体内的药代动力学。方法 采用HPLC方法测定生物样品中CMNa及其代谢物甲硝唑的含量。结果 小鼠体外转化试验表明血中 90minCMNa的转化率为 91 8% ,甲硝唑的生成率为 6 7 3 %。小鼠ivCMNa 5 7 3,171 9和 5 15 7mg·kg-1后CMNa的T1/2 β约为 1 0min ,甲硝唑的T1/2 β约为 6 0min。大鼠ivCMNa 171 9mg·kg-1后 2min及 5minCMNa及甲硝唑在组织含量较高 ;药后从尿中排泄的CMNa和甲硝唑分别占给药总量的 8 4%和 16 7% ,从胆汁排泄分别占 11 5 %和 5 1% ,从粪排泄占 0 14%和0 0 3%。CMNa平均血浆蛋白结合率为 14 2 %。结论 CMNa在体内迅速代谢为甲硝唑 ,原型药及代谢物的Cmax和AUC均与剂量正相关 ,二者主要经尿和胆汁排泄。
Objective To observe the pharmacokinetics of glycididazole sodium (CMNa) in animals. Methods The content of CMNa and its metabolite metronidazole in biological samples were determined by HPLC method. Results The mouse in vitro transformation test showed that the conversion rate of 90 min CMMNa in blood was 91.8%, and the metronidazole formation rate was 67.3%. The T1 / 2 β of CMNa was about 10 min after iv ivMNa 5 7 3,171 9 and 5 15 7 mg · kg -1, and the T1 / 2 β of metronidazole was about 60 min. The content of CMMNa and metronidazole in rat after iv 9 min · kg-1 at 9 mg · kg-1 was higher than that in the control group. CMNa and metronidazole excreted from the urine accounted for 84% and 16 7% Excretion from bile accounted for 11 5% and 51% respectively, excretion from feces accounted for 0 14% and 0 0 3%. CMNa average plasma protein binding rate of 14 2%. Conclusions CMNa is rapidly metabolized to metronidazole in vivo. The Cmax and AUC of prototype drugs and metabolites are positively correlated with the dose. Both of them are mainly excreted by urine and bile.