【摘要】 单剂量静脉快速注射磺胺嘧啶140mg/kg,8h内不同时间心脏采血,测定了磺胺嘧啶在6只健康家兔及6只肾损害家兔体内的代谢动力学参数,结果表明,磺胺嘧啶在家兔体内的药代动力学配置符合无吸收因素二室开放模型。药-时曲线方程为:C正常=134.29e-7.968t+329.28e-0.522t,C肾损=165.59e-3.942t+264.33e-0.322t。肾损害家兔与健康家兔相比,分布速率常数下降了50.53%,消除相速率常数下降了38.34%,分布相半衰期延长了123.46%,消除半衰期延长了63.15%,曲线下面积增加了34.22%,体消除率降低了22.12%。这一结果显示,家兔肾功能损害后,其体内的磺胺嘧啶代谢发生了显著变化,提示在肾脏损害时应相应增大磺胺嘧啶给药间隔时间或减小给药剂量。更多还原

【Abstract】 Pharmacokinetic parameters of Sulfadiazinum （SD） in 6 normal rabbits （control group） and in 6 rabbits with experimental reduced renal functions （treated group） were calculated.Rabbits in two groups were treated with a single dosage of SD （140 mg/kg） intravenously and rapidly,while the blood samples were collected from heart within 8 hour after giving drug.The results showed that the two-compartment open model with first-order disabsorption factor adequately describes whole blood SD disposition and the best SD concentration-time equations are respectively:C （normal） =134.29e^-7.968t+329.28e^-0.522t,C （reduced） =165.59e^-3.942t+264.33e^-0.322t.Compared with normal rabbits （control group）,α decreased by 50.53%,β decreased by 38.34%,t_1/2α prolonged 123.46%,t_1/2β prolonged 63.15%,AUC increased by 34.22%,CL_B decreased by 22.12% respectively in rabbits with experimental reduced renal functions.It will be seen that pharmacokinetic parameters of SD in normal rabbits have taken place great change and dosage of SD should be decreased or interval time of given drug should be prolonged.更多还原