微透析和高效液相色谱法测定大鼠脑内天麻素及天麻苷元含量

目的考察不同剂量天麻素皮下及口服给药后大鼠脑内的天麻素及其代谢产物天麻苷元的浓度变化。方法采用脑内微透析技术进行在体动态取样,建立了高效液相-串联四级杆质谱方法测定脑透析液中的天麻素含量,建立了高效液相-二极管阵列检测方法测定脑透析液中的天麻苷元含量。结果两种给药方式大鼠不同脑区内天麻素浓度均较低,天麻苷元脑内浓度明显高于其原型药物天麻素。结论天麻素的血脑屏障透过能力差,但其活性代谢产物天麻苷元能够较好地进入脑内发挥作用。

Microdialysis and HPLC method for the determination of gastrodin and gastrodige-nin in rat brain

Objective To detect the level of gastrodin and its metabolites gastrodigenin in rat brain dialysate after subcutaneous or oral administration of different doses of gastrodin. Methods Gastxodin in rat brain dialysate was determined by HPLC-MS/MS method and gastrodigenin was determined by HPLC-diode array detector method. Re- sults The gastrodin levels in different rat brain regions for both subcutaneous and oral administration were low while the concentration of gastrodigenin in rat brain was significantly higher than gastrodin. Conclusion The results show that gastrodin could hardly pass through the blood-brain barrier, but its active metabolites gastrodigenin has a greater a- bility to penetrate the blood-brain barrier and play a role in brain.