目的采用脑-颈静脉双通道微透析法观察大鼠灌胃养阴通脑颗粒后主要成分葛根素的药动学参数。方法采用HPLC技术建立大鼠脑和颈静脉微透析液中葛根素的含量测定方法,并考察微透析探针回收率;大鼠植入颈静脉和脑微透析探针引导管,并制作大鼠大脑中动脉局灶性栓塞(MCAO)模型。灌胃给予2.5 g/mL养阴通脑颗粒,测定脑、颈静脉微透析液葛根素的浓度变化,参数拟合分析药动学参数。结果观察MCAO模型大鼠灌胃给予2.0 g/mL养阴通脑颗粒后微透析液中葛根素的浓度,发现脑内葛根素浓度低于颈静脉,Tmax更加靠后,葛根素生物利用度在脑部明显低于血液中。结论建立的脑-颈静脉双通道微透析技术分析获得大鼠不同部位的药-时曲线,有助于开展中药及相关制剂的药动学数据及成分分布、生物利用度等参数。
Objective: To study the pharmacokinetics of Puerarin in cerebral ischemia-reperfusion rats after intragastric administration of Yangyin Tongnao decoction by brain-jugular dual-channel microdialysis. Methods:HPLC was adopted to establish the determination method of Puerarin in microdialysates of cerebral and jugular veins,and the recovery rate of probe was detected. The guide tube was used to insert the jugular vein and brain microdialysis probe,making rats model of focal middle cerebral artery occlusion(MCAO). After intragastric administration of 2.5 g/mL Yangyin Tongnao decoction,the concentration of puerarin in brain and neck vein microdialysates were detected by using parameter fitting to analyze the pharmacokinetic parameters. Results: By observing the concentration of puerarin in brain and neck vein microdialysates after intragastric administration of 2.5g/mL Yangyin Tongnao decoction in MCAO models,the the concentration of puerarin in brain was lower than that in neck vein,as well as Tmax. Bioavailability of Puerarin in brain was obviously lower than that in the blood.Conclusion: obtaining different parts of the concentration-time curve by using the brain-jugular dual-channel microdialysis,it will be beneficial to the pharmacokinetic analysis of traditional Chinese medicine(TCM) and pharmaceutics and the study of composition distribution,bioavailability,and so on.