银杏内酯B在中脑缺血/再灌后大鼠脑组织分布

Distribution of Ginkgolide B in The Brain of Rats Following Brain Ischemia/reperfusion Induced by Middle Cerebral Artery Occlusion

目的研究脑缺血再灌损伤是否影响银杏内酯B在脑内处置。方法大鼠大脑中动脉阻断缺血2h,再灌10min后,静脉注射12mg.kg-1银杏内酯B,于给药后不同时间处死动物,分取用LC/MS方法测定血浆、缺血侧和对照侧脑组织中银杏内酯B浓度。结果缺血侧脑组织中银杏内酯B浓度显著高于对照侧,其AUC约为对照侧的1.88倍。与正常动物比较,脑缺血鼠的血药浓度显著低于正常大鼠,其AUC仅为正常鼠的1/3。结论脑缺血损伤可改变银杏内酯B体内药代动力学行为,增加脑内浓度。

Aim To study whether brain ischemia/reperfusion affects pharmacokinetics of ginkgolide B in rats. Methods Brain ischemia was induced by middle cerebral artery occlusion for 2 h, followed by 10 min reperfusion. A dose of 12mg·kg^-1 ginkgolide B was intravenously given to the rats that were sacrificed at a designed time. Blood, ipsilateral and contralateral cerebral samples were obtained. The concentrations of ginkgolide B in plasma, ipsilateral and controlateral cerebral tissues were measured using LC/MS method. Results Concentrations of ginkgolide B in ipsilateral cerebral tissues were significantly higher than those in contralateral cerebral tissue, and the value of AUC in contralateral tissue was 1.88-fold that in contralateral tissue. The plasma concentrations of ginkgolide B were significantly lower than those in normal rats and the value of AUC was only one third that of normal rats. Conclusion Brain damage induced by middle cerebral artery occlusion/reperfusion may change pharmacokinetic behaviour of ginkgolide B in rats.