附子中3种双酯型生物碱在体外血浆中的水解规律研究

目的:建立体外血浆温孵法测定乌头碱、中乌头碱和次乌头碱水解规律的方法。方法:空白兔血浆加入不同浓度的3种生物碱混合对照品溶液,通过对温孵不同时间血浆样品的预处理(沉淀蛋白、除杂)、分离和检测等过程实现复杂生物样品中待测成分的分离分析。结果:乌头碱、中乌头碱和次乌头碱浓度在血浆中均随温孵时间的延长逐渐降低,水解速率中乌头碱>乌头碱>次乌头碱,与附子饮片在炮制过程中3种双酯型生物碱的水解规律一致。结论:所建立的体外水解方法简单、稳定、可控,对上述3种成分的体内药动学研究具有一定的参考意义。

Study on in vitro Hydrolysis in Rabbit Plasma of Three Diester-type Alkaloids from Radix Aconiti Lateralis

Objective:To develop a platform of incubation of plasma in vitro for analysis of conponents of traditional Chinese medicine. Methods:The aconitic alkaloids were as one of the examples. Aconitine, mesaconitine and hypaconitine were added to rabbit plasma and incubated for various durations. The plasma samples were processed with acetonitrile to denature and deposit the protein and extracted the three alkaloids, and the acetonitrile solution was analyzed by a RP chromatographic system. Results: The concentration of aconitine, mesaconitine and hypaconitine in plasma was descreased with the prolonged incubation time,the hydrolysis rate of mesaconitine was the fastest,aconitine was the second and hypaconitine was the third. Conclusion: A simple, stable and controllable method has been established, which has some reference value for pharmacokinetic study of aconitic alkaloids.