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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 study the tissue distribution of toad toxin in rats and provide the basis for clinical rational drug use. Methods Sublingual iv 0.5,1 mg / kg civet toxin. The drug concentration in rat tissues at different time points was determined by HPLC, and the biological samples were processed by liquid-liquid extraction. Results After sublingual iv toad toxin was subcutaneously administered to rats, the tissue distribution was rapid. After 30 min of administration, the amount of civead toxin was detected in the remaining 8 tissues except for fat. At 60 min after administration, most of the blood flow-rich tissues Reaching the peak of drug concentration, of which the drug concentration in the liver was the highest; when the drug concentration was increased exponentially, the peak time of Bufonin toxin in each tissue did not change, but the drug concentration at the corresponding time point increased slightly, The time is also extended accordingly. Conclusions Cinobufotin toxin is widely distributed in rat tissues and absorbed and eliminated rapidly, and high drug concentration can be achieved in brain tissue.