川芎嗪脂肪乳在小鼠体内分布的研究

目的考察川芎嗪脂肪乳在小鼠体内的组织分布,为川芎嗪新制剂开发奠定基础。方法以川芎嗪静脉注射脂肪乳与盐酸川芎嗪注射液为样本,建立小鼠组织中川芎嗪的HPLC定量方法,并用该法测定经尾静脉给药后小鼠血液和组织匀浆中药物浓度,比较2种制剂的分布情况。结果川芎嗪脂肪乳能迅速通过小鼠血脑屏障,血液中分布最多,心脏消除最快;与盐酸川芎嗪注射液对照组比较,前者在测定的组织及血液中的滞留时间明显增加,浓度有显著性增高。脑内AUC值是对照组的2.76倍,AUC总值是对照组的2.40倍。结论使用脂肪乳作为载体,小鼠血液及各组织中川芎嗪分布量增多,消除减慢,具一定缓释作用。

Tissue distribution of tetramethylpyrazine intralipid in mice

Objective To investigate the tissue distribution of tetramethylpyrazine（TMP）intralipid in mice,and lay the foundation for the development of TMP new dosage forms.Methods An HPLC method for the determination of TMP in mouse tissues and plasma has been developed,validated,and applied in tissue distribution study of mice after i.v.administration of TMP intralipid and then compared with TMPH solution.Results TMP intralipid could quickly penetrate the blood-brain barrier（BBB）of the mice.The concentration of TMP intralipid in mouse plasma was much higher than that in other organs.Compared with the TMPH solution group,the concentrations of TMP in both plasma and tissues of intralipid group were significantly higher and mean residence time increased.The total area under concentration-time curve of intralipid group was about 2.40 times that of the control group and it was 2.76 times in the brain.Conclusion Using lipid emulsion as drug carrier,the distribution of TMP in mouce blood and tissues increased,and the elimination slowed down.TMP intralipid was proved to be sustained release.