微透析技术研究天麻素、天麻苷元在肝阳上亢偏头痛大鼠体内的药动学  

Pharmacokinetics Study of Gastrodin and Gastrodigenin on Migraine in Rats with Hyperactivity of Liver-yang Using Microdialysis Method

作　　者：王美静[1] 刘明平[1] 李盛青[1] 黄志云[1] 毛禹康 郭思宇[1] 柯国韩 

机构地区：[1]广州中医药大学中药学院,广东广州510006

出　　处：《中药新药与临床药理》2017年第6期753-757,共5页Traditional Chinese Drug Research and Clinical Pharmacology

基　　金：国家自然科学基金(81274107)

摘　　要：目的建立微透析技术测定天麻素(GAS)、天麻苷元(HBA)的方法,并研究其在肝阳上亢型偏头痛模型大鼠的药动学特征。方法采用HPLC法,考察GAS、HBA微透析测定方法的专属性、线性关系、精密度及流速、浓度对回收率的影响;采用硝酸甘油加附子制备肝阳上亢大鼠模型,于颈静脉插入探针,收集样品,HPLC法检测样品中GAS、HBA浓度,计算其药动学参数。结果 GAS在肝阳上亢偏头痛模型大鼠的药动学参数:t_(1/2)=(65.32±8.16)min,T_(max)=(86.67±10.32)min,C_(max)=(70.31±7.36)μg·m L^(-1),AUC_(0-∞)=(15 385±1 205)μg·m L^(-1)·min,MRT_(0-∞)=(182.29±5.05)min;HBA药动学参数:t_(1/2)=(115.83±8.44)min,T_(max)=(120±48.99)min,C_(max)=(4.65±0.19)μg·m L^(-1),AUC_(0-∞)=(1 575.04±132)μg·m L^(-1)·min,MRT_(0-∞)=(236.62±6.21)min。结论微透析方法精密度高、稳定性好,可用于GAS和HBA在肝阳上亢偏头痛模型大鼠的药动学研究;GAS、HBA在肝阳上亢偏头痛模型大鼠体内的药-时曲线符合非房室模型特征。Objective To establish microdialysis method for study of pharmacokinetics characteristics of gastrodin（GAS）and gastrodigenin（p-hydroxybenzyl alcohol,HBA）on migraine of hyperactivity liver-yang rats. Methods The HPLC method was used to evaluate the specificity, linearity, and precision, and the influence of velocity,concentration to the recovery of microdialysis on GAS and HBA measurement. The migraine with hyperactivity liver-yang rat models were copied using nitroglycerin plus Aconiti lateralis radix praeparaia.The blood probes were inserted into the probeon jugular vein to collect the samples, and GAS and HBA concentrations were detected with HPLC, and the pharmacokinetic parameters of GAS and HBA were calculated. Results The pharmacokinetic parameters of GAS in the migraine with hyperactivity liver-yang model rats were： t_（1/2）=（65.32 ±8.16） min, T_（max）=（86.67±10.32）min, C_（max）=（70.31±7.36）μg·m L-1,AUC_（0-∞）=（15385±1205） μg·m L^（-1）·min,MRT_（0-∞）=（182.29±5.05） min;the pharmacokinetic parameters of HBA were：t_（1/2）=（115.83±8.44） min,T_（max）=（120±48.99） min,C_（max）=（4.65±0.19）μg·m L-1,AUC_（0-∞）=（1 575.04±132）μg·m L^（-1）·min,MRT_（0-∞）=（236.62±6.21）min. Conclusion The microdialysis method has high precision and good stability and can be used for the pharmacokinetic study of GAS and HBA in migraine with hyperactivity liver-yang model rats. The drug concentration-time curve of GAS and HBA fitted in noncompartment model features.

关 键 词：天麻 天麻素 天麻苷元 药物动力学 微透析 高效液相色谱法 

分 类 号：R285.5[医药卫生—中药学]