目的研究不同间隔时间冰片处理对大鼠栀子苷脑内浓度的影响,以指导临床用药。方法冰片分别灌胃5、15、30 min后静脉注射栀子苷,不同时间点取血取脑,样本预处理后采用HPLC检测栀子苷浓度,采用3P97计算血-药和脑-药参数,并获取脑靶相关参数。结果栀子苷在血浆和脑组织分布符合二室开放模型,冰片处理后可提高栀子苷脑-药动力学的Cmax和AUC,延长MRT,缩短Tmax。其中冰片15 min组对栀子苷脑内相对生物利用度和脑靶指数的提高作用最明显。结论冰片处理后可提高栀子苷入脑量和入脑速度,冰片灌胃15 min后血脑屏障开放最明显。
Aim To research on the the influence of borneol treatment interval on the concentration of geniposide in rat brains for clinic appliance.Methods Rats were treated with borneol orally and geniposide by intravenous injection with the interval of 5,15,30 min.The conentration of geniposide in the plasma and brain tissue was detected by RT-HPLC the chnology and the data was analyzed by 3P97 software.Results Pharmacokinetics of geniposide in the plasma and brain met with two-compartment model.Borneol could enhance the Cmax and AUC of geniposide compared with control group.In addition,the MRT was prolonged and Tmax was shortened.The borneol 15 min group was the most notable on the Fbrain and DTI.Conclusion Borneol can increase the quantity and velocity of geniposide permeating the brain and the opening of the BBB is the most obvious after it is intragastrically administered for 15 min.