天麻苷元大鼠鼻腔和静脉注射给药的脑药动学研究

Pharmacokinetics of gastrodigenin in rat plasma and CSF after intranasal and intravenous administration

目的:研究比较天麻苷元在大鼠鼻腔给药和静注给药后的血和脑脊液药动学。方法:天麻苷元静注给药剂量为50或10 mg.kg-1,鼻腔给药剂量为10 mg.kg-1。采用高效液相法测定血和脑脊液中天麻苷元的浓度,以DAS 2.0药动学软件计算非房室模型参数。结果:给药后天麻苷元能迅速进入脑脊液中,AUCCSF高于AUCplasma,鼻腔给药的AUCCSF或AUCplasma与静注给药的相比无显著性差异。结论:鼻腔给药后天麻苷元能迅速完整地进入体循环中,鼻腔给药可替代静注给药,未观察到鼻-脑途径的直接传递。

Objective： To investigate the pharmacokinetics of gastrodigenin（p-hydroxybenzyl alcohol,HBA） in rat plasma and cerebrospinal fluid（CSF） after intravenous（i.v.） and intranasal（i.n.） administration.Methods： HBA was administered via i.v.at a dose of 50 or 10 mg·kg-1 and via i.n.at 10 mg·kg-1.Blood and CSF were collected at timed intervals for the measurement of HBA concentrations by high performance liquid chromatography.The calculations of pharmacokinetic parameters were performed by non-compartmental analysis using the software DAS 2.0.Results： HBA rapidly entered CSF after administration.AUCCSF was higher than AUCplasma.There was no significant difference in AUCCSF or AUCplasma between i.n.and i.v.administrations.Conclusion： HBA can be absorbed into the systemic circulation rapidly and completely after intranasal administration.Intranasal HBA may be a promising alternative to intravenous administration.No extra direct nose-CSF transport could be demonstrated.