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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 compare the pharmacokinetics of blood and cerebrospinal fluid after administration of gastrodia aglycone in rats after nasal administration and intravenous administration. Methods: Gastrodin intravenous injection dose of 50 or 10 mg.kg-1, nasal administration dose of 10 mg.kg-1. The concentrations of gastrodin in blood and cerebrospinal fluid were determined by HPLC. The parameters of non-atrioventricular model were calculated by DAS 2.0 pharmacokinetic software. Results: After administration, SPECT could rapidly enter the cerebrospinal fluid and AUCCSF was higher than AUCplasma. There was no significant difference in AUCCSF or AUCplasma nasal administration compared with intravenous administration. CONCLUSION: Gastrodia aglycone can rapidly and completely enter the systemic circulation after nasal administration, and nasal administration can substitute for intravenous administration. No direct transmission of nasal-brain route is observed.