UPLC-HDMS法测定大鼠灌胃栀子柏皮片后小檗碱与栀子苷的药代动力学

目的:通过UPLC-HDMS法测定小檗碱和栀子苷在大鼠灌胃栀子柏皮片后的药代动力学。方法:用固相萃取柱法处理血浆样本后,以正离子扫描方式,采用萃取离子监测(EIC)方式进行检测,采用Winnolin软件计算药物动力学参数。结果:小檗碱的达峰时间为1.89±0.56 h,其AUC值为793±87 ng/mL/h,药代参数显示该成分在体内浓度较低,消除较快;栀子苷的达峰时间为2.09±0.88 h,其AUC值为4687±345 ng/mL/h,药代参数显示该成分在体内表观分布容积较大,消除也较快。结论:利用高灵敏度的液质联用仪器在血中成功检测到了小檗碱及栀子苷,提示小檗碱及栀子苷为栀子柏皮片体内潜在药效作用物质。

A Pharmacokinetic Study of Berberin and Gardenoside in Rats after Oral Administration of Zhi-Zi-Bai-Pi Tablet

ABSTRACT Objective: To study the pharmacokinetics of berberin and gardenoside after oral administration of Zhi-Zi-Bai-Pi tablet to rats. Methods: The plasma was disposed by solid phase extraction column and then analyzed in positive mode by EIC, and the pharma- cokinetic parameters was analyzed by Winnolin software. Results: The Tmax of berberin was 1.89±0.56 h, and the AUC was 793±87 ng/mL/h which indicated that berberin was excreted rapidly and the concentration was very low; The Tmax of gardenoside was 2.09±0.88 h, and the AUC was 4687±345 ng/mL/h ng/mL/h which indicated that gardenoside was widely distributed and then excreted rapidly. Conclusion: Berberin and gardenoside was successfully detected in rat plasma, suggesting that berberine and geniposide are potential pharmacodynamic substances of Zhi-Zi-Bai-Pi tablet.