摘要
目的 建立大鼠血浆中替加色罗的HPLC测定法 ,以测定大鼠ig替加色罗后的血药浓度 ,并对其药代动力学进行评价。方法 血浆样品加入内标后用乙酸乙酯提取 ,进行HPLC分析 ,流动相为甲醇 乙腈 水 (6 0∶8∶32 ,含 0 8%冰醋酸 ,0 4 %三乙胺 ,v/v) ,流速为 1 0ml/min ,检测波长为 310nm。大鼠ig 5 0、10 0、2 0 0mg·kg-1替加色罗后 ,测定其血浆中替加色罗的浓度 ,计算主要药动学参数。结果 血浆中替加色罗在 2 0 0ng/ml～ 80 0 0ng/ml浓度范围内线性关系良好 ,血浆中替加色罗的最低检测限为 1 0ng/ml。大鼠ig 5 0、10 0、2 0 0mg·kg 1替加色罗后 ,估算的末端相半衰期分别为 0 86、1 0 9、1 0 8h ,3种剂量的半衰期相近 ,AUC与剂量间呈良好的线性关系 (r =0 9996 )。结论 本实验建立的分析方法灵敏、准确、简便。在5 0～ 2 0 0mg·kg 1剂量范围内 ,替加色罗在大鼠体内符合线性药物动力学特征 ,平均半衰期为 1 0 1h。
Aim To develop a HPLC assay for determination of tegaserod in rats plasma and to study the pharmacokinetics of tegaserod in rats.Method After spiked with the internal standard, plasma was extracted by ethyl acetate and separated by a C 18reversed-phase column.Result After ig administration of tegaserod with 3 dosages of 5.0,10.0 and 20.0 mg·kg -1to rats, the half-life of tegaserod in rats were estimated to be 0.86,1.09 and 1.08 h respectively, and the aresa under the concentration time curves correlated well with doses (r=0.9996).Conclusion The assay was proved to be sensitive, accruate and convenient. In the dosage rang of 5.0～20.0 mg·kg -1the pharmacokinetics of tegaserod in rats was linear and the average half-life of tegaserod in rat was 1.01 h.
出处
《江苏药学与临床研究》
2004年第4期3-5,共3页
Jiangsu Pharmacertical and Clinical Research
