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目的:研究洋川芎内酯I在灌胃和静脉注射后在大鼠体尿液和胆汁中的排泄特征,为该成分的临床前研究和评价提供参考。方法:大鼠按剂量72 mg·kg-1灌胃和尾静脉给与洋川芎内酯I溶液,收集不同时间段尿液和胆汁,采用高效液相色谱-紫外检测器法(HPLC-VWD)测定大鼠尿液和胆汁中洋川芎内酯I的含量,检测波长均为278 nm,流动相均为乙腈-0.1%甲酸水溶液梯度洗脱。结果:灌胃和尾静脉给药48 h后累积经尿液排泄的原形药物量分别为(179.8±33.68),(264.8±87.28)μg,累积排泄率分别为(0.77±0.15)%和(1.35±0.26)%;给药36 h后累积经胆汁排泄的原形药物量依次为(359.4±75.66),(426.3±140.90)μg,累积排泄率分别为(1.22±0.49)%和(1.72±0.59)%。结论:洋川芎内酯I在大鼠尿液和胆汁内以原形药物的形式排出量较少,且排泄迅速。
Objective: To study the excretion of yangchongxiong I in rat urine and bile after gavage and intravenous injection, and provide reference for the preclinical study and evaluation of this composition. Methods: Rats were given 72 mg · kg-1 dose of Yang Chuanxiong lactone I solution by gavage and tail vein, urine and bile were collected at different time points, and HPLC-UV detector (HPLC-VWD) Determination of rat urinary and bile in Yang Chuanxiong lactone I, the detection wavelength was 278 nm, the mobile phase was acetonitrile -0.1% aqueous solution of gradient elution. Results: The cumulative amount of prototype drug excreted by the urine after oral administration and tail vein injection for 48 h were (179.8 ± 33.68) and (264.8 ± 87.28) μg, respectively, with cumulative excretion rates of (0.77 ± 0.15)% and (1.35 ± 0.26)%. The cumulative amount of prototype drug excreted by bile excreted 36 hours after administration was (359.4 ± 75.66) and (426.3 ± 140.90) μg, respectively. The cumulative excretion rates were (1.22 ± 0.49)% and (1.72 ± 0.59) %. Conclusion: Yang Chuanxiong lactone I in the form of prototype drugs in urine and bile less excreted, and excreted rapidly.