奥扎格雷在大鼠体内的药代动力学研究

Study on Pharmacokinetics of Ozagrel in Wistar Rats

目的建立测定血浆中奥扎格雷浓度的高效液相色谱(H PLC)法,并用于大鼠体内的药代动力学研究。方法采用Diam onsil-C18柱(200m m×4.6m m,5μm),以甲醇-1%冰醋酸(8∶92)为流动相,测定6只W istar大鼠单剂量灌胃给予奥扎格雷后不同时刻血浆中奥扎格雷的质量浓度,并由此计算药代动力学参数。结果大鼠灌胃给予奥扎格雷后,血浆中的达峰时间(tmax)为(42.5±6.1)m in,峰浓度(Cmax)为(6.02±0.97)μg/m L,半衰期(t1/2)为(42.9±11.5)m in,0～t药-时曲线下面积(AUC0-t)为(473.8±88.5)μg.m in/m L,0～∞药-时曲线下面积(AUC0-∞)为(495.1±96.3)μg.m in/m L。结论H PLC法简便、可靠,可用于奥扎格雷的药代动力学研究。

Objective To establish a method for the determination of the concentration of ozagrel in plasma by HPLC, and to study its pharmacokineties in rats. Methods The chromatographic separation was performed on a Diamonsil-C18 column （200 mm ×4. 6 mm, 5 μm） with the mobile phase consisting of methanol-1%HAc （8：92）. The single oral doses of ozagrel were given to 6 Wistar rats to study the pharmacokinetics and the ozagrel concentrations in plasma were determined by the HPLC method. Results The pharmacokinetic parameters were as follows： tmax was （42.5 ±6.1）min, Cmax was （6.02 ±0. 97）μg/mL, t1/2 was （42.9 ± 11.5）min; AUC0-∞ was （473.8 ±88.5）μg · min/mL, AUC0-∞ was （495. 1± 96. 3）μg · min/mL. Conclusion The method is simple, which can be applied to the pharmacokinetie study.