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本文比较了灯盏花素鼻腔给药、口服给药与静脉给药在大鼠脑内的药物分布。采用SD大鼠尾静脉注射、经鼻给药和灌胃0.4mg.kg-1灯盏花素后,于一定时间点用小脑延髓池穿刺术采集大鼠脑脊液,125I标记法测定其在大鼠脑脊液,以及大脑、小脑、延脑、嗅区和嗅球等脑组织及血浆中药物含量,梯形法分别计算其AUC。结果显示鼻腔给药组大鼠脑脊液、大脑、小脑、延脑、嗅区、嗅球及血浆中AUC0-240min(μg.min.g-1)分别为11.686±1.919,5.676±1.025,7.989±0.925,7.956±1.159,17.465±2.136,24.2±2.906和78.51±12.05;静脉给药组AUC0-240min分别为6.79±0.661,6.251±0.40,10.805±1.161,9.146±1.04,9.892±1.532,7.871±0.842和173.91±10.02;口服给药组AUC0-240min分别为0.868±0.167,1.708±0.266,2.867±0.725,2.067±0.313,1.361±0.308,1.206±0.255和45.2±7.52。口服、静脉注射、鼻腔给药后脑组织的AUC0-240min分别为血浆AUC0-240min的22.29%,29.18%,95.49%,说明鼻腔给药的吸收率高于口服给药和静脉给药,并且鼻腔给药后药物在脑组织中分布较高,其与药效的关系值得进一步探讨。
This article compares the drug distribution of breviscapine nasal, oral and intravenous administration in rat brain. SD rats were injected through tail vein, nasal administration and intragastric administration of 0.4mg.kg-1 Breviscapine, cerebrospinal fluid (CSF) was collected from cerebellomedullary cistern at a certain time point and was measured in 125I-labeled rat cerebrospinal fluid , And brain, cerebellum, medulla, olfactory area and olfactory bulb and other brain tissue and plasma drug content, trapezoidal method were calculated AUC. The results showed that AUC0-240min (μg.min.g-1) in cerebrospinal fluid, cerebrum, cerebellum, medulla oblongata, olfactory area, olfactory bulb and plasma in nasal administration group were 11.686 ± 1.919,5.676 ± 1.025,7.989 ± 0.925, 7.956 ± 1.159, 17.465 ± 2.136, 24.2 ± 2.906 and 78.51 ± 12.05 respectively; the AUC0-240min of the intravenous administration group were 6.79 ± 0.661, 6.251 ± 0.40, 10.805 ± 1.161, 9.146 ± 1.04, 9.892 ± 1.532, 7.871 ± 0.842 and 173.91 ± 10.02; AUC0-240min for oral administration were 0.868 ± 0.167, 1.708 ± 0.266, 2.867 ± 0.725, 2.067 ± 0.313, 1.361 ± 0.308, 1.206 ± 0.255 and 45.2 ± 7.52, respectively. AUC0-240min of oral administration, intravenous injection and intranasal administration were 22.29%, 29.18% and 95.49% of the plasma AUC0-240min, respectively, indicating that nasal administration had higher absorption rate than oral administration and intravenous administration, and nasal administration Drugs in the brain distribution of drugs higher, the relationship with the efficacy worth further study.