摘要: |
将12只家兔分为A,B两组,A组为健康对照组,B组注射四氯化碳,复制肝损伤模型。A,B两组家兔均以140 mg/kg(以磺胺六甲氧嘧淀(SMM)计)剂量耳静脉注射磺胺六甲氧嘧啶钠(SMM-Na),分别于给药后0.08,0.25,0.5,1,2,3,4,6 h采血0.5 mL,采用改良Annino法测定血液SMM浓度,以残数法逐只家兔拟合药-时曲线,并计算药物代泄动力学参数。结果表明,SMM在肝功能损害家兔体内的动力学变化明显,其动力学参数与健康时比较,t1/2β延长了5.087倍,AUC延长了3.051倍,tcp延长了3.753倍。表明家兔肝功能损害后,SMM在其体内消除显著变慢,提示在肝脏损害时应相应增大SMM给药时间间隔或减小给药剂量。 |
关键词: 磺胺六甲氧嘧啶 家兔 肝功能损害 药物代泄动力学 |
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Studies on the pharmacokinetics of Sulfamonomethoxinum in rabbits with experimental reduced hepatic functions |
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Abstract: |
Pharmacokinetic parameters of Sulfamonomethoxinum (SMM) in 6 normal rabbits (control group) and in 6 rabbits with experimental reduced hepatic functions (test group) were calculated.Rabbits in two groups were treated with a single dosage of SMM (140 mg/kg) intravenously and rapidly,while the blood samples were collected from heart within 8 hours after giving drug.The results showed that the two compartment open model with first-order disabsorption factor adequately described whole blood SMM disposition.Great changes of pharmacokinetic parameters of SMM in reduced hepatic rabbits took place.Compared with normal rabbits (control group),AUC increased 3.051 times,t1/2β prolonged 5.087 times,tcp prolonged 3.753 times respectively in rabbits with experimental reduced hepatic functions.It will be seen that dosage of SMM should be decreased or interval time of giveing drug should be increased. |
Key words: Sulfamonomethoxinum rabbit experimental reduced hepatic function pharmacokinetics |