【摘要】 目的 研究苦参中有效成分槐果碱在大鼠体内血、组织和脏器中的浓度,进行药代动力学分析。方法建立槐果碱的高效液相色谱法(HPLC),对大鼠静注槐果碱(20 mg/kg)后的药时曲线、组织分布进行研究;房室模型及药动学参数通过3p87软件拟合计算。结果 槐果碱的相对回收率100.7％～108.7％,日内、日间精密度RSD<5％。血药浓度在0.625～20.0μg/mL、组织浓度在2.5～80.0μg/g范围内呈线性关系(r分别为0.99998、0.9964)。大鼠静注槐果碱后,药代过程符合二室模型。组织分布以肾最高,多数脏器给药后15 h仍能测到。结论 槐果碱在大鼠体内的药代动力学过程符合二室模型,且与组织有特异性结合。更多还原

【Abstract】 Objective The paper reported the distribution of effective substances of Kushen ( sophocarpine) in the serum and tissues of rats, and the pharmacokinetics of sophocarpine. Methods High perform liquid chromato-graphic (HPLC) analytical method was established for determining sophocarpine. The concentrations-time cure and distribution of sophocarpine in rats after iv. infusion with a dose of 20 mg/kg were studied. The compartment model and pharmacokinetical parameters were figured and calculated by 3p87 sofeware. Results The relative recovery of sophocarpine was 100. 7%-108. 7% . The RSD in one day and between-days was no more than 5% . The linear calibration curve in serum was from 0. 625μg/mL to 20. 0 μg/mL ( r = 0. 99998 ) and in tissue from 2. 5 μg/mL to 80.0 μMg/mL (r = 0.9964). Serum drug concentration-time curve fitted the 2-compartment open model. The distribution of sophocarpine was highest in the kidney and can be still detected after 15 h in most organs. Conclusion Pharmacokinetics of sophocarpine in rats fits the 2-compartment open model. Sophocarpine could connect with tissues particularly.更多还原