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目的:以静脉给药为对照,研究灯盏花乙素口服给药在大鼠中的药代动力学及对大鼠实验性脑缺血的药效作用,探讨灯盏花乙素口服给药治疗脑梗死的可行性。方法:采用125I标记法测定SD大鼠尾静脉注射和灌胃0.4mg.kg-1灯盏花乙素后不同时间血浆中灯盏花乙素的浓度,3P87软件拟合房室模型,计算药动学参数;采用Longa线栓法制作SD大鼠局部脑缺血模型,脑缺血1h,再灌注24h,随机分为假手术组、模型组、灯盏花乙素口服给药与静脉给药组,每组6只,分别给予相应药物,观察各组对脑缺血大鼠神经功能、脑梗死面积的影响。结果:口服给药组Tmax、Cmax分别为42.70 min、0.28μg/mL,绝对生物利用度为30.54%。脑缺血1h,再灌注24h时模型组大鼠神经功能缺损严重,平均达4~5级;模型组梗死体积平均为21.82%,口服组给药组与静脉给药组分别为16.76%与14.01%,与模型组比较有显著性差异。结论:灯盏花乙素口服给药治疗脑梗死具有一定的可行性。
OBJECTIVE: To study the pharmacokinetics of scutellarin orally administered in rats and its pharmacological effects on experimental cerebral ischemia in rats by intravenous administration, and to investigate the effects of oral administration of scutellarin on brain Feasibility of infarction. Methods: The concentration of scutellarin in plasma of SD rats after tail vein injection and 0.4 mg.kg-1 0.4 mg.kg-1 scalp irrigation at different time was determined by 125I labeling method. The pharmacokinetics was calculated by 3P87 software The rats were randomly divided into sham-operation group, model group, scopolamine oral administration group and intravenous administration group, each 6 rats in each group were given the corresponding drugs to observe the effect of each group on neurological function and cerebral infarction area in rats with cerebral ischemia. Results: Tmax and Cmax of oral administration group were 42.70 min and 0.28 μg / mL, respectively. The absolute bioavailability was 30.54%. Neurological deficits in model group were severe at 1 hour after cerebral ischemia and 24 hours after reperfusion. The average volume of infarction volume in model group was 21.82%, while those in oral group and intravenous group were 16.76% and 14.01 %, Compared with the model group had significant differences. Conclusion: Oral administration of scutellarin has some feasibility in the treatment of cerebral infarction.