冰片对大鼠经鼻腔给药灯盏花素体内药动学的影响

目的:探索冰片对大鼠经鼻腔给药灯盏花素体内药代动力学的影响。方法:采用同位素标记法125I检测实验大鼠经过尾静脉注射、单纯鼻腔给药和鼻腔给药联合冰片三种途径摄入0.4mg/kg灯盏花素以后的药代动力学,测定1、5、10、30、60、90、120、150、180、210、270min的血浆中灯盏乙素的浓度,绘制药时曲线并比较三种途径的药代动力学参数。结果:经鼻腔给药联合冰片组大鼠的tmax为22min短于单纯鼻腔给药组的tmax30min,差异有统计学意义(t=5.73,P=0.025);经鼻腔联合冰片组和单纯鼻腔给药组的Cmax分别为0.55、0.52μg/mL,绝对生物利用度分别为53.21%和53.71%,差异没有统计学意义。结论:冰片可以在一定程度上影响大鼠经鼻腔灯盏花素给药,使其血浆灯盏乙素浓度的达峰时间缩短,但是对灯盏乙素的绝对生物利用度没有明显影响,可以为灯盏花素新制剂的研究提供新方向。

Pharmacokinetic effect of borneol on breviscapine by intranasal administration in rats

AIM: To investigate the pharmacokinetic effect of Borneol on breviscapine by intranasal administration in rats.METHODS: The plasma concentration of scutellarin at 1,5,10,30,60,90,120,150,180,210,270 min were measured using 125 I isotope labeling experiments after the intake of 0.4 mg/kg Breviscapine through intravenous injection,nasal administration and nasal administration co-borneol,drew concentration-time curve and compared pharmacokinetic parameters of three ways.RESULTS:The tmax of co-borneol intranasal administration was 22 min which was significantly shorter than that of simple intranasal administration(30 min).And there is statistically difference between them(t=5.73,P=0.025);the Cmax of co-borneol intranasal group and simple intranasal administration group were 0.55,0.52 μg/mL,and absolute bioavailability were 53.21% and 53.71%,which was not statistically significant.CONCLUSION: To a certain extent,borneol could shorten the peak time of scutellar plasma concentrations in rats by nasal administration,but did not significantly affect the absolute bioavailability,which showed a new research direction on the combination of borneol and breviscapine.