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目的建立灵敏、准确的高效液相色谱方法(HPLC)测定大鼠血浆中吉非替尼的浓度,并研究其在大鼠体内的代谢动力学。方法大鼠灌胃或尾静脉注射给予吉非替尼后,自眼球后静脉丛采血,以埃罗替尼为内标物,HPLC法测定血药浓度:甲醇-10 mmol/L乙酸铵(70∶30)为流动相,流速:1.0 mL/min;检测波长:330 nm。结果测定吉非替尼的线性范围是0.02016~6.72μg/mL,精密度,稳定性(RSD)均小于15%,口服吉非替尼片绝对生物利用度59.81%。结论该分析方法专属性强,灵敏度高,吉非替尼血浆药物清除曲线符合二室模型。
Objective To establish a sensitive and accurate high performance liquid chromatography (HPLC) method for the determination of gefitinib in rat plasma and to study its pharmacokinetics in rats. Methods After intragastric or caudal vein injection of gefitinib, the blood was collected from the retrobulbar venous plexus. Erlotinib was used as the internal standard. The plasma concentration of methanol-10 mmol / L ammonium acetate : 30) as mobile phase, flow rate: 1.0 mL / min; detection wavelength: 330 nm. Results The linear range of gefitinib was 0.02016 ~ 6.72 μg / mL. The precision and stability (RSD) of gefitinib were all less than 15%. The absolute bioavailability of gefitinib was 59.81%. Conclusion The method is highly specific and sensitive, and the gefitinib plasma drug clearance curve conforms to the two-compartment model.