微渗析技术研究葛根素滴眼液麻醉家兔眼内药动学  

Ocular pharmacokinetics of puerarin in anesthetic rabbits by microdialysis

作　　者：姚晨[1] 周绣棣[1] 曲涛[1] 位冬昱[2] 慕宏杰[1] 梁荣才[1] 王爱萍[1] 孙考祥[1] 

机构地区：[1]烟台大学药学院药剂研究室,山东烟台264005 [2]首都医科大学中医药学院,北京100069

出　　处：《中国中药杂志》2011年第16期2236-2239,共4页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金项目(30873447)

摘　　要：目的:建立微渗析实验模型,并对葛根素在麻醉家兔眼内的药物动力学进行研究。方法:通过手术将微渗析探针植入麻醉家兔的眼前房室内,待灌流平衡之后眼部给予1%葛根素滴眼液100μL,于不同时间收集渗析液,HPLC测定;流动相为甲醇-0.1%柠檬酸水溶液(30∶70),流速1.0 mL.min-1,检测波长249 nm。结果:给予自制葛根素滴眼液后,其能够迅速吸收进入眼前房室中,在1 h达到峰浓度,Cmax为(2.52±0.31)mg.L-1,然后渐渐降低,但在消除阶段3.5 h左右出现另外1个较低的峰浓度。可能是由于葛根素抑制了房水的生成,导致药物浓度的升高。药-时曲线下面积(AUC0～t)为(5.04±0.21)mg.h.L-1,半衰期(t1/2)为(0.38±0.13)h。结论:采用微渗析技术,能够用于测定葛根素眼部的药物动力学,并且为葛根素滴眼液的临床应用提供有参考价值的药动学参数。Objective： To establish the model of microdialysis,and study the ocular pharmacokinetics of puerarin in anesthetic rabbits.Method： Implanted the probe into anterior chamber of anesthetic rabbit by surgery.After balanced for 2 h,1% puerarin eye drop（100 μL） was applied into the cul-de-sac with micropipette.Immediately the dialysate was collected at different time and detected by HPLC with the detection wavelength of 249 nm.The mobile phase was methanol and 0.1% citric acid solution（30∶70）;the flow rate was 1.0 mL·min-1.Result： After the administration,puerarin can be absorbed into aqueous humor quickly.The peak concentration of puerarin appeared at about 1 h and then reduced gradually.The peak concentration（Cmax） is（2.52±0.31） mg·L-1.The other lower peak was shown at 3.5 h during the eliminate phase.This might be attributed to the inhibition of aqueous humor production by the puerarin and resulted in a high drug concentration.The area under concentration-time curve（AUC0-t） is（5.04±0.21） mg·h·L-1 and the eliminate half life（t1/2） is（0.38±0.13） h.Conclusion： The microdialysis technique can be used to detect the ocular pharmacokinetics of puerarin,and support the valuable pharmacokinetics parameter for the clinical applications of puerarin eye drop.

关 键 词：葛根素 微渗析技术 药动学 滴眼液 

分 类 号：R285[医药卫生—中药学]