目的建立小鼠脑组织中天麻苷元的HPLC测定方法,并考察灌胃天麻素后小鼠脑中天麻苷元的药动学特性。方法脑匀浆用醋酸乙酯提取后,采用HPLC法测定。色谱柱为Diamonsil C18(250 mm×4.6 mm,5μm),流动相为乙腈-水(10.5∶89.5),体积流量1.0 mL/min;检测波长221 nm;柱温25℃;进样量20μL。结果方法线性范围为50~1 616 ng/mL(r=0.999 6),回收率为93.8%~95.1%,日内及日间RSD均低于10%。小鼠脑组织中天麻苷元的质量浓度与时间曲线呈现双峰(tmax1=15 min,tmax2=90 min),药时曲线下面积为52 822.5ng.min/g,消除半衰期为54.8 min。结论该分析方法灵敏、准确,适合于脑组织中天麻苷元的测定。天麻素经小鼠口服给药后,能较快入脑并代谢为天麻苷元,消除也较快。 OBJECTIVE: To establish a method for the determination of gastrodin in mouse brain by HPLC and to study the pharmacokinetics of gastrodin in mouse brain after gastrodin administration. Methods Brain homogenates were extracted with ethyl acetate and determined by HPLC. The column was Diamonsil C18 (250 mm × 4.6 mm, 5 μm). The mobile phase consisted of acetonitrile-water (10.5: 89.5), the volume flow rate was 1.0 mL / min, the detection wavelength was 221 nm, the column temperature was 25 ℃, and the injection volume was 20 μL. Results The linear range of the method was 50-1 616 ng / mL (r = 0.999 6). The recoveries ranged from 93.8% to 95.1%. The RSDs were less than 10% in both days and days. The curve of the concentration and time curve of the genistin in mouse brain showed a double peak (tmax1 = 15 min, tmax2 = 90 min). The area under the curve was 52 822.5 ng.min / g and the elimination half-life was 54.8 min. Conclusion The method is sensitive and accurate and suitable for the determination of genistein in brain tissue. Gastrodin by oral administration of mice, can quickly into the brain and metabolism to the gastrodin, elimination is also faster.