【摘要】 五味子醇甲为五味子乙醇提取物中有效成分之一,具有明显中枢安定作用,本文用薄层紫外扫描方法测定醇甲在大鼠及小鼠体内的吸收、分布、排泄及脑内分布。 大鼠口服醇甲后,胃肠吸收快,静注后血药浓度呈开放二室模型。组织分布以肺浓度最高,其次为肝、心、脑、肾、肠、脾及肠最低。脑内分布以下丘脑、纹体、海马浓度最高,其次为低位脑干及间脑,大脑皮层和小脑浓度较低。静注后由尿排出量很少。醇甲自整体小鼠的消失快。结果表明醇甲自胃肠道吸收快而完全,代谢及排泄较快,组织分布广。各脑区药物浓度的差别可能与其中枢作用有关。更多还原

【Abstract】 Schizandrol A is one of the active constituents isolated from the ethanol extract of dried fruit of Schizandra chinensis Baill （Fructus Schizandra）. It was found to have neuroleptic and anticonvulsive effects in animals. A method of high specificity using TLC for the determination of Schizandrol A in biological, specimens was developed and used in the study of the metabolism of the drug in rats and the distrubution in various areas of rat brain.After oral administration Schizandrol A was found to be readily, absorbed from the gastro-intestinal tract (t_1/2=58 min). The bloodlevel of Schizandrol A following iv injection showed a biphasic decline as a function of time, the distribution phase and the elimination phase. The pharmacokinetic parameters were as follows:t_1/2α=1.44 min, t_1/2β=42.14 min, K₁₀=0.08/min, K₁₂=0.32/min, K₂₁=0.10/min, V_c=0.75 L/kg, V_d=3.60 L/kg. Schizandrol A was detectable in urine one hour after oral administration About 0.35％ of the dose was recovered from urine within 26 hours. Five minutes after iv injection highest levels of Schizandrol A was found in the lung, moderate in liver, heart, brain and kidneys, and low in ileum and spleen. These results indicate that Schizandrol A was distributed widely in the body and eliminated rapidly.The distribution of Schizandrol A in various areas of the brain was as follows:highest levels was found in hypothalamus, striatum and hippocampus, moderate indiencephalon and lower stem, and low in cerebral Cortex and cerebelum. The different levels in various regions of the brain might be relevant to the neuroleptic and cataleptic effects of Schizandrol A.更多还原