鸡屎藤次苷在大鼠体内的药动学研究

Pharmacokinetic Study on Scandoside in Rats In Vivo

目的:测定大鼠血浆中鸡屎藤次苷的含量,并研究其在大鼠体内的药动学过程。方法:采用HPLC-UV法测定大鼠尾静脉注射给药后血浆中鸡屎藤次苷的血药浓度。色谱条件为:DiamonsilTM C18柱(250 mm×4.6 mm,5μm),流动相:甲醇-乙腈-0.1%冰醋酸(3∶2∶95,v/v/v),流速:1.0 mL.min-1,检测波长:230 nm。通过BAPP2.0软件求算其药动学参数。结果:鸡屎藤次苷血浆浓度在0.2～40μg.mL-1(Y=0.07321X-0.00939,r=0.9940)范围内线性关系良好。日内精密度不大于7.1%,日间精密度不大于13.5%,准确度RE值在-4.5%～1.8%之间。鸡屎藤次苷提取回收率为64.5%～73.1%,内标物提取回收率为74.5%。主要药动学参数为t1/2=(33.5±4.39)min,AUC0-180min=(922±129)μg.min.mL-1。结论:该法专属、准确、灵敏,适用于鸡屎藤次苷在大鼠体内的药动学研究,为进一步研究鸡屎藤次苷体内药动学行为提供了依据。

Objective：To develop an HPLC-UV method for the determination of scandoside in rat plasma,and to study pharmacokinetics of scandoside in rats in vivo.Methods：HPLC-UV method was used to determine the scandoside in rat plasma.The separation was performed on a DiamonsilTM C18 column（250 mm×4.6 mm,5 μm） with methanol-acetonitrile-water（3：2：95,v/v/v,containing 0.1% acetic acid） as the mobile phase at the flow rate of 1.0 mL·min-1.The UV detection was set at 230 nm and the column temperature was 25℃.Results：The calibration curves were linear over the concentration range 0.2～40 μg·mL-1（Y=0.07321X-0.00939,r=0.9940） in rat plasma was 0.2 μg·mL-1.The intra-day and inter-day precisions were within 7.1% and 13.5%,respectively,and RE was-4.5%～1.8%.The average extraction recoveries were 64.5%～73.1%.Following intravenous administration in rats（4.2 mg·kg-1）,the primary phamacokinetic parameters of scandoside in plasma were as follows：t1/2（33.5±4.39） min,AUC0-180 min（922±129） μg·min·mL-1.Conclusion：This method is selective,accurate and sensitive,which can be applied for the determination of scandoside in plasma and its pharmacokinetic studies.