川芎嗪在豚鼠血液、脑脊液和耳蜗外淋巴液中的分布

Ligustrazine Hydrochloride in Blood,Cerebrospinal Fluid and Perilymph Fluid of Guinea Pig after Intramuscular Injection

目的 测定肌肉注射盐酸川芎嗪注射液后川芎嗪在豚鼠血液、脑脊液和耳蜗外淋巴液中的分布。方法 豚鼠经肌肉注射盐酸川芎嗪注射液 (2ml/kg)后 ,采用高效液相色谱法 (HPLC)中的内标法和外标法测定血液、脑脊液和耳蜗外淋巴液中川芎嗪的浓度。结果 川芎嗪注射后 ,豚鼠血液中川芎嗪浓度迅速升高 ,2 0min达到最大值 (35 7.76 μg/ml) ,2h后血药浓度迅速下降 ;在脑脊液中 10min后才检测到川芎嗪 ,2 0min其浓度达到最大值(12 0 .5 0 μg/ml) ,70min后脑脊液药浓度迅速下降 ;在耳蜗外淋巴液中 5min时能检测到川芎嗪 ,5 0min时浓度达最大值 (2 15 .79μg/ml) ,70min后药物浓度明显降低。 结论 川芎嗪可吸收入血液并能够通过血脑屏障及血 -迷路屏障进入脑脊液和耳蜗外淋巴液 ,药物吸收及消除迅速。临床应用该药时 ,要维持川芎嗪在耳蜗内的药物浓度应该适当增加用药次数 。

Objective To investigate the distribution of ligustrazine hydrochloride in guinea pig blood, cerebrospinal fluid and perilymph fluid afte intramuscular injection. Methods The HPLC was used for determination of ligustrazine hydrochloride in guinea pig blood, cerebrospinal fluid and perilymph fluid afte intramuscular injection by internal and external standard method.Results Ligustrazine hydrochloride could be absorbed into blood rapidly after intramuscular administration in guinea pig. The concentration reach its high level in 20 min.It was 357.76 μg/ml. It decreased to low level 2 h after injection.It could be found in cerebrospinal fluid 10 min after injection. The concentration reached its high level in 20 min.It was 120.50 μg/ml.It decreased to low level 70 min after injection. The ligustrazine hydrochloride could be found in perilymph fluid 5 min later.Its high level in 20 min was 215.79 ug/ml.It decreased to low level 70 min after injection.The results indicated that ligustrazine hydrochloride was rapidly absorbed and eliminated after intramuscular administration in guinea pig.Conclusion Ligustrazine hydrochloride can be absorbed into blood, enter cerebrospinal fluid and perilymph fluid. It can pass through blood-brain barrier and blood-labyrinth barrier. The results indicates that ligustrazine hydrochloride is rapidly absorbed and eliminated after intramuscular administration in guinea pig.