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目的建立HPLC法测定大鼠血浆中化合物Au20的浓度,研究其在大鼠体内的药动学及绝对生物利用度。方法双周期自身交叉设计,SD大鼠静注给药和灌胃给药化合物Au20,剂量分别为4.0和40.0 mg/kg,给药后不同时间点取血,HPLC法测定血浆中化合物Au20的浓度,用DAS 2.0软件计算其药动学参数。结果血浆中化合物Au20在7.8～1 000 ng/mL浓度范围内线性关系良好(r=0.999 9),提取回收率75.91%～89.06%,日内和日间RSD均小于5%。静脉注射给药的药-时曲线符合三室模型。经剂量校正,口服给药的绝对生物利用度为(4.08±1.85)%。结论化合物Au20口服给药的绝对生物利用度低。
OBJECTIVE To establish a HPLC method for the determination of the concentration of compound Au20 in rat plasma and study its pharmacokinetics and absolute bioavailability in rats. Methods Double-cycle self-designed crossover design. Sprague-Dawley rats were injected intraperitoneally with compound Au20 at a dose of 4.0 and 40.0 mg / kg, respectively. Blood samples were collected at different time points after administration. The concentration of compound Au20 The pharmacokinetic parameters were calculated using DAS 2.0 software. Results The concentration of Au20 in the plasma ranged from 7.8 to 1 000 ng / mL (r = 0.999 9). The recovery rates ranged from 75.91% to 89.06%. The intra-day and inter-day RSD were less than 5%. The drug-time curve for intravenous administration conformed to the three-compartment model. After dose correction, the absolute bioavailability of oral administration was (4.08 ± 1.85)%. Conclusion The absolute bioavailability of oral administration of compound Au20 is low.