目的研究华蟾蜍毒素在大鼠体内的组织分布特征,为临床合理用药提供依据.方法大鼠舌下iv 0.5、1mg/kg华蟾蜍毒素.采用HPLC法测定大鼠组织中不同时间点的药物浓度,组织生物样品用液-液萃取法处理.结果大鼠舌下iv华蟾蜍毒素后,组织分布较快,给药后30 min,除脂肪外其余8个组织均可测到华蟾蜍毒素;给药后60 min,大部分血流丰富组织即达到药物浓度峰值,其中肝脏药物浓度最高;当给药浓度成倍增加时,华蟾蜍毒素在各组织中的达峰时间并没有变化,只是相应时间点的药物浓度均略有升高,药物消除的时间也相应延长.结论华蟾蜍毒素在大鼠组织中分布广泛,吸收和消除均较快,在脑组织中也可达到较高药物浓度.

Objective To investigate the tissue distribution character of cinobufagin inin vivoin rats,in order to provide some references for rational drug use in the clinic.Methods Two kinds of solutions of cinobufagin were given to rats(0.5 and .mg/kg)by sublingual iv injection.The cinobufagin concentration in rat tissues corresponding to different time-point was determinated by HPLC.The biological samples of the different tissuses were performed by liquid-liquid extraction method.Results Cinobufagin distributed rapidly to tissue after sublingual iv injection.At 30 min cinobufagin in eight tissues except fat was detected.At 60 min the concentration in a majority of tissue achieved the peak value and liver's was tiptop.When the concentration of cinobufagin increased by gemination,the time of reaching peak value had no change.Only the concentration of cinobufagin increased slightly corresponding to the time-point.Conclusion The distribution of cinobufagin in tissues of rats is extensive.Both the absorption and elimination of cinbufagin are quick and up to the top concentration in brain tissue.

武警医学院青年基金资助项目(WYQ2006-13)