目的 建立小鼠iv醒脑静注射液后测定脑内栀子苷浓度的HPLC法，探讨醒脑静注射液中栀子苷在小鼠体内的药动学过程。方法 40只小鼠尾iv醒脑静注射液10.9 mg/kg（以栀子苷计）后，分别于1、3、5、10、30、60、90、120 min摘眼球放血后脱颈椎处死5只小鼠，迅速分离出小鼠全脑，制成脑匀浆，HPLC测定脑匀浆中栀子苷的量，以Kinetica软件拟合药动学参数，拟合方法选择非房室模型。结果 栀子苷脑药浓度在54～1 620 ng/g时线性关系良好，r＝0.999 1；栀子苷脑药浓度在216、864、1 620 ng/g时萃取回收率分别为（102.60±4.28）%、（102.16±4.48）%、（97. 66±3.25）%；日内、日间精密度的相对标准偏差（RSD）均小于4.10%。小鼠iv醒脑静注射液后，主要药动学参数C_max为（1 246.0±520.7）ng/g，t_max为1 min，MRT为（50.5±1.9）min，AUC为（35 780.3±6 148.0）ng/(min?g)。结论 该方法简便、快速、重复性好，适用于小鼠栀子苷脑药浓度测定及药动学研究。

Objective To develop an HPLC method for the determination of geniposide concentration in mouse brain and to investigate the pharmacokinetics after iv injection of Xingnaojing Injection. Methods Forty mice were iv injected with Xingnaojing Injection 18 mg/kg (by geniposide), and the brain samples were collected at 1, 3, 5, 10, 30, 60, 90, 120 min after eyeball bleeding and 5 mice were sacrificed by cervical dislocation. The whole brain of mice was separated quickly to prepare brain homogenates, and the concentration of geniposide was detected by HPLC. The pharmacokinetic parameters were calculated by the software of Kinetica and the fitting method was noncompartmental. Results The calibration curve was in good linear in the range of 54—1 620 ng/g, r＝0.999 1. The extraction recoveries of geniposide brain drug concentration at 216, 864, and 1 620 ng/g were (102.60 ± 4.28)%, (102.16 ± 4.48)%, and (97.66 ± 3.25)%, respectively. And the RSD values of inter- and intra-day were below 4.10%. The pharmacokinetic parameters were that the C_max was (1 246.0 ± 520.7) ng/g, the t_max was 1 min, the MRT was (50.5 ± 1.9) min, and the AUC was (35 780.3 ± 6 148.0) ng/(g?min). Conclusion The HPLC method for determining geniposide concentration in brain is simple, rapid, sensitive, and suitable for pharmacokinetic studies.

国家自然科学基金青年基金项目（81102816）；国家自然科学基金面上项目（81073057）；北京中医药大学创新团队发展计划（2011-CXTD-13）