目的 研究秦皮甲素两种给药途径在大鼠体内的药代动力学.方法 秦皮甲素经大鼠灌胃(ig)和腹腔注射(ip)给药( 100 mg/kg )后,采集不同时间点的大鼠血样,采用HPLC测定秦皮甲素在大鼠血浆中的浓度并计算其药代动力学参数.结果 秦皮甲素灌胃给药和腹腔注射给药两种途径的药动学均符合一级吸收一室开放模型,其关键药物动力学参数分别为AUC0→∞=(3.76±0.44) mg·h/L,(149.64±20.71) mg·h/L; Ke=(0.83±0.22)/h,(1.38±0.13)/h; Cmax=(2.63±0.60) mg/L,(164.37±16.94) mg/L; Tmax=(0.17±0.00) h,(0.17±0.00) h; T1/2 (ke) =(0.88±0.21) h,(0.51±0.05) h; MRT=(1.69±0.31) h,(0.99±0.06) h.结论 秦皮甲素两种给药途径的主要药动学参数有显著性差异,腹腔注射给药代谢速度较高,可以更加有效地降低血尿酸.%Objective To study the pharmacokinetics of aesculin in rats of two administration routine in vivo. Methods The rats were given aesculin by intragastric administration (ip) and intraperitoneal injection (ig) with a dosage of 100 mg/kg. The plasma at different time points was collected. The concentration of aesculin in rats' plasma was determined by HPLC and its pharmacokinetic parameters were calculated. Results The pharmacokinetics of aesculin by ig and ip routine met first-order and mono-compartment model, the critical parameters shown as below, respectively: AUC0→∞=(3.76±0.44) mg·h/L, (149.64±20.71) mg·h/L; Ke=(0.83±0.22)/h, (1.38±0.13)/h; Cmax=(2.63±0.60) mg/L, (164.37±16.94) mg/L;Tmax=(0.17±0.00) h, (0.17±0.00) h; T1/2 (ke) =(0.88±0.21) h,(0.51±0.05) h; MRT=(1.69±0.31) h, (0.99±0.06) h. Conclusion The pharmacokinetic parameters of aesculin by two routines showed significant difference, the ig route was with higher metabolic rate and can reduce blood uric acid effectively.
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