摘要
目的建立HPLC法测定大鼠血浆中甲磺酸雷沙吉兰浓度,并研究其在大鼠体内的药物代谢动力学。方法以盐酸小檗碱为内标,血浆样品经乙腈沉淀后,采用Wondasil C18色谱柱(240 mm×4.6 mm,5μm),流动相:0.02 mol·L^(-1)醋酸铵溶液-乙腈(35∶65,v/v),流速:1.0 m L·min^(-1),检测波长:265 nm,柱温:室温。大鼠灌胃给予250 mg·kg-1的甲磺酸雷沙吉兰后,测定血浆中药物浓度并估算其药物代谢动力学参数。结果甲磺酸雷沙吉兰浓度在2.1~55.8μg·m L^(-1)与峰面积线性关系良好(r=0.9997,n=7),提取回收率在98.5%~105.3%,定量下限为2.1μg·m L^(-1),日内和日间RSD以及稳定性考察RSD均<5%。结论本方法简便快速,准确度与灵敏度均较高,适用于甲磺酸雷沙吉兰在大鼠体内的药物动力学研究。
Objective To establish an HPLC method to determine rasagiline mesylate(RM) in rat plasma and investigate its pharmacokinetics after an oral administration in rats. Methods Berberine hydrochloride was used as the internal standard. After protein precipitation of plasma samples with acetonitrile, the chromatographic analysis of RM in the rat plasma was performed on Wondasil C18(240 mm×4.6 mm, 5 μm) column with a mobile phase of 0.02 mol·L^(-1) ammonium acetate and acetonitrile(35 ∶ 65, v/v) and the flow rate was 1.0 m L·min^(-1). The UV detection wavelength was 265 nm and the column temperature was room temperature. Rat plasma samples were collected after the oral administration of 250 mg·kg^(-1) RM and the plasma drug concentrations were determined to calculate the pharmacokinetic parameters of the drug in the rats. Results There was a good linearity for RM at 2.1-55.8 μg·m L^(-1)(r = 0.9997, n = 7). The extraction recovery was 98.5%-105.3% and the lower limit of quantitation of the method was 2.1 μg·m L^(-1). The intra-day and inter-day RSD and stability exploration RSD were all less than 5%. Conclusion The established method is rapid, simple, accurate and sensitive, and it is suitable for studying the pharmacokinetics of RM in rats.
出处
《中南药学》
CAS
2016年第5期480-483,共4页
Central South Pharmacy
