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目的:建立血浆中8-乙酰哈巴苷的HPLC测定方法,研究大鼠不同给药途径给予8-乙酰哈巴苷后的药代动力学特征。方法:大鼠分别注射和灌胃8-乙酰哈巴苷,于不同时间点取血;采用HPLC,流动相乙腈-异丙醇-水(1.8∶10.2∶88),检测波长207 nm,流速1.0 mL.min-1,绘制药-时曲线,建立药代动力学模型,计算药代动力学参数。结果:8-乙酰哈巴苷在血浆中的回归方程为Y=613 753.13X-86 995.55(r=0.999 2),在0.015 3～22.995μg线性关系良好。高、中、低3个剂量组日内精密度RSD分别为0.59%,0.38%,0.55%;日间精密度RSD分别为3.9%,2.1%,1.5%。回收率分别为94.89%,95.85%,95.25%。灌胃途径在体内基本检测不出;注射途径3个剂量组主要药代动力学参数t1/2分别为(21.15±3.36),(24.26±5.50),(16.58±5.65)min;tmax分别为(4.98±0),(4.98±0),(4.98±0)min;Cmax分别为(2.25±1.41),(0.09±0.03),(0.02±0.007)g.L-1。结论:该法灵敏度高,专属性强,准确可靠,操作快速简便,可用于8-乙酰哈巴苷在大鼠体内的药代动力学研究,注射给予8-乙酰哈巴苷在大鼠体内吸收快且不完全,消除相对较慢,但具有良好的药代动力学特征,房室模型拟合分析为一房室模型。
OBJECTIVE: To establish a HPLC method for the determination of 8-acetyl-habacin in plasma and study the pharmacokinetics of 8-acetyl-hababine administered by different routes of administration in rats. Methods: Rats were injected with 8-acetyl-7-acetyl-7-acetyl-habacin at different time points respectively. HPLC, mobile phase acetonitrile-isopropanol-water . min-1, draw the drug-time curve, the establishment of pharmacokinetic model, calculation of pharmacokinetic parameters. Results: The regression equation of 8-acetyl-habacin in plasma was Y = 613 753.13X-86 995.55 (r = 0.999 2), and the linearity was good at 0.015 3 ~ 22.995μg. The intra-day precision RSD of high, middle and low dose groups were 0.59%, 0.38% and 0.55%, respectively. The intraday precision RSD was 3.9%, 2.1% and 1.5% respectively. The recoveries were 94.89%, 95.85% and 95.25% respectively. The main pharmacokinetic parameters t1 / 2 in the three doses of injection route were (21.15 ± 3.36), (24.26 ± 5.50) and (16.58 ± 5.65) min, respectively; tmax were ( 4.98 ± 0, 4.98 ± 0, 4.98 ± 0 min, respectively; Cmax were (2.25 ± 1.41), (0.09 ± 0.03) and (0.02 ± 0.007) gL-1, respectively. Conclusion: This method has high sensitivity, specificity, accuracy and reliability, and is fast and easy to operate. It can be used for the pharmacokinetic study of 8-acetyl-hababine in rats. The injection of 8-acetyl- Incomplete, relatively slow elimination, but with good pharmacokinetic characteristics, atrioventricular model fitting analysis for one-compartment model.