【摘要】 目的 :探讨一次静注 8 氯腺苷在大鼠体内药代动力学的规律及特点 ,为临床实验提供理论依据。方法 :给大鼠单次静注 4种剂量 8 氯腺苷后 ,应用HPLC测定在体液和组织中原形物 8 氯腺苷的含量。结果 :8 氯腺苷在大鼠体内迅速转化为代谢产物 ,其消除半衰期为 1h左右。除脂肪、脑、睾丸组织外 ,8 氯腺苷在体内分布广泛 ,药物血浆蛋白结合率在 10～ 4 0 μg/ml浓度范围内约为 3 7% ,主要以代谢物形式从尿及胆汁中排泄。 结论 :8 氯腺苷的药代动力学为一级动力学二室模型 ,AUC在 2 5～ 10 0mg/kg的剂量范围时按比例增加 ,当剂量增加至 15 0mg/kg时 ,则AUC不成比例地增加 ,药物在体内的消除可能转入了零级动力学 ,8 氯腺苷在大鼠体内迅速代谢 ,从血中消除并从尿中排泄。更多还原

【Abstract】 OBJECTIVE:To study the pharmacokinetics of 8 chloro adenosine.METHODS:After iv bolus injection of 8 chloro adenosine,rats’serum drug concentrations were measured by HPLC.RESULTS:8 chloro adenosine were widely distributed in body tissues of rats after iv bolus injection and rapidly turned into metabolits and excreted form urine and bile with a t 1/2 of about 1h,and a plasma protein binding rate of about 37%.CONCLUSION:The serum concentration time curves of the drug fitted to two department model and behaved as a liner relation in rats in dose range of 25～100 mg/kg but as a non liner relation if dosage above 150 mg/kg.更多还原