不同剂量冰片对栀子苷在大鼠脑内浓度的影响  

Effects of borneol at different doses on concentration of geniposide in rat brains

作　　者：董小平[1,2] 阮鸣[3] 喻斌[1] 金路[1,2] 朱冬清[1,2] 方泰惠[1,2] 

机构地区：[1]南京中医药大学药学院,江苏南京210046 [2]江苏省中药药效与安全性评价重点实验室,江苏南京210046 [3]南京晓庄学院药用菌物研究所,江苏南京211171

出　　处：《中草药》2012年第7期1366-1370,共5页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金青年基金资助项目(81001651)

摘　　要：目的研究大鼠ig不同剂量冰片后对栀子苷在大鼠脑内浓度的影响。方法大鼠ig给予冰片0.05、0.1、0.2、0.4 g/kg15 min后,尾iv栀子苷300 mg/kg,于栀子苷给药后0.5、1、5、10、15、30、45、60、90 min采血、取脑,HPLC法测定血样和脑组织样本中栀子苷的量,采用3P97软件计算栀子苷在血浆和脑组织中的药动学参数,计算栀子苷在血浆和脑组织中的相对生物利用度和脑靶相关参数。结果栀子苷在血浆和脑组织分布符合二室开放模型,经冰片处理后可提高栀子苷在脑组织中的Cmax和AUC,延长MRT,缩短tmax,其中冰片0.2 g/kg剂量对栀子苷的影响最显著。结论大鼠ig冰片后iv栀子苷,冰片可提高栀子苷入脑量和入脑速度,以冰片0.2 g/kg剂量对栀子苷的影响最显著。Obleetive To study the concentration of geniposide in brains of rats ig administrated with borneol at different doses. Methods Rats were ig administrated with 0.05, 0.1, 0.2, and 0.4 g/kg ofborneol, and then iv injected with 300 mg/kg of geniposide. After 0.5, 1, 5, 10, 15, 30, 45, 60, and 90 min of geniposide injection, blood and brain tissue were collected, and the concentration of geniposide in the plasma and brain tissue was detected by RP-HPLC. The pharmacokinetic parameters of geniposide in plasma and brain tissue were analyzed by 3P97 software, and the relative bioavailability and brain target-correlated parameters of geniposide were calculated. Results Pharmacokinetics of geniposide in plasma and brain tissue was accorded with two-compartment model. After treated with borneol, Cmax and AUC of geniposide in brain tissue were increased, MRT was prolonged, and tmax was shortened. Besides, borneol with dose of 0.2 g/kg had the most significant effect. Conclusion Borneol could increase the quantity and velocity of geniposide permeating the blood-brain barrier and the effect will be most obvious when the dose ofbomeol is 0.2 g/kg.

关 键 词：冰片 栀子苷 药动学 脑靶 生物利用度 

分 类 号：R969.2[医药卫生—药理学]