1.Guizhou Medical University;2.Guizhou medical University
The National Natural Science Foundation of China (General Program, Key Program, Major Research Plan)
目的 对盐酸川芎嗪与丹参配伍前后在急性心肌缺血（Acute myocardial ischemia，AMI）模型大鼠体内的组织分布差异进行探讨。方法 大鼠皮下注射盐酸异丙肾上腺素溶液复制AMI模型，采用UPLC-MS/MS方法测定单次尾静脉注射丹参注射液（DGI）、川芎嗪注射液（CGI）、参芎葡萄糖注射液（SGI）后不同时间点下川芎嗪和丹参素2种活性成分在心、肝、脾、肺、肾、脑组织中的含量差异。结果 经静脉注射后川芎嗪和丹参素在AMI大鼠各组织中分布广泛且迅速达峰；配伍前后，各组川芎嗪在脑组织中含量最高，在肝组织中含量最低；丹参素在肾组织中含量最高，在脑组织中含量最低，表明川芎嗪较丹参素更易透过血脑屏障，且主要蓄积组织有所差异；而配伍用药显著增加了川芎嗪和丹参素在靶器官心脏中的AUC（P＜0.001）。结论 推测川芎嗪与丹参配伍可能是通过增加主要药效成分在心脏中的分布增强治疗作用，进而使SGI能更好发挥药效。
Objective To investigate the difference in tissue distribution of ligustrazine hydrochloride and Salvia miltiorrhiza (Danshen) in Acute myocardial ischemia (AMI) rats. Methods AMI model was induced by subcutaneous injection of isoproterenol hydrochloride. UPLC-MS/MS method was used to determine the content differences of ligustrazine and danshensu in heart, liver, spleen, lung, kidney and brain tissues after single intravenous injection of Danshen injection (DGI), Ligustrazine injection (CGI) and Shenxiong glucose injection (SGI) at different time points. Results After intravenous injection, ligustrazine and danshensu were widely distributed in tissues of AMI rats and reached their peak rapidly. Before and after compatibility, the content of ligustrazine was the highest in brain tissue and the lowest in liver tissue. The content of danshensu in kidney tissue was the highest, and in brain tissue was the lowest, indicating that ligustrazine could penetrate the blood-brain barrier more easily than danshensu, and the main accumulation tissues were different. The AUC of ligustrazine and danshensu in the heart of the target organ was significantly increased (P < 0.001). Conclusion It is speculated that the combination of ligustrazine and salvia miltiorrhiza may enhance the therapeutic effect by increasing the distribution of main pharmacodynamic components in the heart, so that SGI can play a better role.