辣椒素在大鼠体内的药动学及分布研究  

Pharmacokinetics and distribution of capsaicin in rats

作　　者：段炼[1] 彭怀东[1] 卢钧雄[1] 王若伦[1] 

机构地区：[1]广州医科大学附属第二医院,广州510260

出　　处：《中南药学》2016年第6期603-606,共4页Central South Pharmacy

基　　金：国家自然科学基金资助项目(No.81403031);广州医科大学博士启动项目(No.2013c47)

摘　　要：目的研究辣椒素经口服给药后的药动学及其在组织内的分布情况。方法 SD大鼠灌胃辣椒素后,颈静脉取血计算辣椒素药动学参数,处死后,定量称取各部分组织样品,经前处理后,用高效液相色谱-质谱联用法检测各部分组织中的浓度。结果辣椒素灌胃后AUC(0~360 min)为(78.271±7.909)μg·h·m L^(-1),Cmax为(0.283±0.081)μg·m L^(-1),tmax为(60.000±25.819)min,药时曲线呈现双峰的现象。1~2 h时辣椒素在肝、空肠及回肠中的浓度较高。4 h时辣椒素在回肠中仍然具有很高的浓度。此外,辣椒素也能够通过血脑屏障到达脑部,并且在4 h后仍能检测到。结论辣椒素灌胃后在大鼠体内分布广泛,主要在肝代谢,并具有透过血脑屏障的能力。Objective To determine the pharmacokinetic parameters and tissue distribution of capsaicin in rats. Methods HPLC-MS/MS was used to detect the concentration of capsaicin in the blood and the tissue, and calculate the pharmacokinetic parameters by DAS program. Results After the oral administration, AUC（0360 min） was（78.271±7.909） μg·h·m L-1, Cmax was（0.283 ±0.081） μg·m L-1, and tmax was（60±25.819） min. The drugtime curve was bimodal. After 1- 2 hours, higher concentration was found in the liver, jejunum and ileum. The concentration of capsaicin was still high in the ileum after 4 hours. In addition, capsaicin can also across the bloodbrain-barrier to the brain, and it can be detected almost after 4 h later. Conclusion Capsaicin is widely distributed in rats after the oral administration, and mainly metabolized in the liver. It can penetrate the blood-brain barrier.

关 键 词：辣椒素 高效液相色谱串联质谱 口服 药动学 组织分布 

分 类 号：R285.5[医药卫生—中药学]