中文摘要：

目的 研究盐酸川芎嗪（TMPH）经大鼠鼻腔给药后的脑内药动学特性。方法 采用脑微透析取样技术，以清醒自由活动大鼠为实验模型，连续收集盐酸川芎嗪鼻腔和静脉注射给药后大鼠脑内纹状体透析液，HPLC测定其浓度，并经回收率校正后，以WinNonlin4.0.1药动学软件处理，计算药动学参数并进行统计学分析。结果 TMPH鼻腔给药5min后脑纹状体中的药物浓度为（1.43±0.29）mg·L^-1，而静脉注射后在相同时间点入脑不显著。鼻腔给药的ρmax低于静脉注射，分别为（3.43±0.46）和（4.67±0.76）mg·L^-1，但二者的tmax,AUC0-∞,MRT,CLs近似，无显著性差异（P〉0.05）.结论 TMPH鼻腔给药后可迅速吸收入脑，且吸收量与静脉注射近似，因此有望成为一种新的给药途径。

英文摘要：

OBJECTIVE To investigate the brain pharmacokinetics of tetramethylpyrazine hydrochloride（TMPH）after intranasal administration in rats. METHODS Striatum dialysate samples were continuously collected by brain mierodialysis technique in awake freely-moving rats. The concentration of TMPlt in dialysate samples were measured by HPLC. The pharmaeokinetie parameters were calculated by WinNonlin4. 0. 1 and statistically analyzed. RESULTS The TMPH concentration in striatum five minutes after intranasal administration was （ 1.43 ± 0. 29） mg·L^-1, while much lower concentration was found atier intravenous injection administration. The value of p after intranasal administration was （3.43 ± 0. 46） mg · L^-1, lower than the value of intravenous injection, （4.67 ±0. 76） mg ·L^-1. However, there was no signitieant rill＇terence among the values of tmax AUC0-∞, AUC0-∞ , MRT and CLs of the two administration routes（ P 〉0.05 ）. CONCLUSION TMPH coohl be absorbed into the brain promptly after in administration and the ahsorption amount was similar to iv administration. Therefore, it could be a promising alternative delivery tot TMPH in the future.