去氢骆驼蓬碱静脉注射乳剂在动物体内的药代动力学  

PHARMACOKINETICS OF HARMINE INTRAVENOUS EMULSION IN RATS AND MICE

作　　者：高晓黎[1] 毕殿州[2] 孙殿甲[1] 苗爱东 

机构地区：[1]新疆医科大学,乌鲁木齐830054 [2]沈阳药科大学,沈阳110015 [3]空军乌鲁木齐医院,乌鲁木齐830001

出　　处：《药学学报》2000年第3期224-227,共4页Acta Pharmaceutica Sinica

基　　金：国家科委医药技术创新博士项目!(96 90 1 0 6 0 2 1 )

摘　　要：目的 :研究去氢骆驼蓬碱 (harmine ,HAR)静脉注射乳剂在大鼠体内的药动学和小鼠体内的组织分布。方法 :HPLC法测定血药浓度 ,计算药动学参数 ;用放射性同位素示踪法测定给药后各脏器组织的分布特征。结果 :iv给药 ,药动学过程可用三室开放模型拟合 ;乳剂的组织分布能力强于水溶液。iv或ig乳剂 ,3H HAR定向于肝、淋巴器官分布。乳剂的LD50 大于水溶液。结论 :将HAR制成静脉注射乳剂可改变HAR体内过程 ,降低其神经系统毒副作用。AIM: To study the pharmacokinetics of harmine (HAR) intravenous emulsion in rats and mice. METHODS: The pharmacokinetics of the emulsion and solution containing harmine were compared in rats by cross over test. The drug concentration was determined by HPLC. 3H was labelled in harmine, and the emulsion and solution of 3H HAR were prepared. The radioactivity (Bq) of the various organs and blood were detected by liquid scintillation counting. RESULTS: The concentration time curves for both the emulsion and the solution fit three compartments open model after intravenous injection to rats. The volume of distribution( V c), clearance(Cl) and the mean residence time(MRT) revealed significant differences between the emulsion and the solution, suggesting that the emulsion showed stronger tissue distributing ability than the solution. Meanwhile, lower radioactivity plasma concentration was found after iv injection of the emulsion to the rats, indicating that the drug delivery system may have other transport ways except blood transport. The distribution of emulsion in the tissue of mice showed that there were definite direction and accumulation in the lymph system. CONCLUSION: The intravenous emulsion, as drug delivery system, may enhance the drug quantity in targetted organs and prevent the drug from transporing to brain, so that the emulsion form can effectively reduce the toxicity and adverse effects of harmine. This conclusion was also evident from the results of LD 50 determination.

关 键 词：去氢骆驼蓬碱 静脉注射乳剂 药代动力学 

分 类 号：R969.1[医药卫生—药理学]