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目的研究天麻素在大鼠十二指肠给药后的脑药动学和不同脑区的分布。方法将大鼠麻醉后,通过其十二指肠给天麻素,剂量为200 mg·kg~(-1)。在规定时间点收集血浆、脑脊液和4个不同脑区(皮质、海马、丘脑、小脑)的脑微透析液。采用HPLC法测定所收集液体中的药物浓度,采用DAS 2.0药动学软件计算药动学参数。结果天麻素给药后能迅速进入脑部,4个不同脑区和脑脊液的t_(max)分别为(40.0±6.1)、(42.5±7.7)、(37.5±9.5)、(42.5±7.7)和(55.8±16.0)min,其AUC与血浆AUC的比值分别为(2.6±1.0)%、(2.6±0.9)%、(3.0±0.9)%、(5.3±2.1)%和(6.0±2.6)%。天麻素在小脑的AUC明显大于在其他3个脑区的AUC(P<0.05)。结论天麻素经十二指肠给药后能迅速入脑部,但是入脑量低,所有AUC_脑/AUC_(血浆)均<6%。
Objective To study the pharmacokinetics and distribution of gastrodin in different brain regions after administration of gastrodin in duodenum of rats. Methods After the rats were anesthetized, gastrodin was given to the duodenum at a dose of 200 mg · kg ~ (-1). Plasma, cerebrospinal fluid and brain microdialysis fluid were collected at defined time points in 4 different brain regions (cortex, hippocampus, thalamus, cerebellum). The concentration of the drug in the collected liquid was measured by HPLC, and the pharmacokinetic parameters were calculated by using the DAS 2.0 pharmacokinetic software. Results Gastrodin quickly entered the brain after administration, and the t max of four different brain regions and cerebrospinal fluid were (40.0 ± 6.1), (42.5 ± 7.7), (37.5 ± 9.5), (42.5 ± 7.7) and (55.8 ± 16.0) min, and the ratio of AUC to plasma AUC was (2.6 ± 1.0)%, (2.6 ± 0.9)%, (3.0 ± 0.9)%, (5.3 ± 2.1)% and (6.0 ± 2.6)% respectively . Gastrodin AUC in the cerebellum was significantly greater than in the other 3 brain regions (P <0.05). Conclusion Gastrodin rapidly enters the brain after duodenal administration, but it has a low brain volume, with all AUC_ brain / AUC_ (plasma) <6%.