Effect of borneol on the distribution of gastrodin to the brain in mice via oral administration
Effect of borneol on the distribution of gastrodin to the brain in mice via oral administration
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DOI：
10.1080/10611860701794395
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发表时间：
2008-01-01
影响因子：
4.5
通讯作者：
Pu, Junxue
中科院分区：
文献类型：
--
作者：
Cai, Zheng;Hou, Shixiang;Pu, Junxue
冰片和天麻素都是从中药中提取的生物活性物质。本文研究了冰片对天麻素经口给药后在小鼠脑内分布的影响。分别于灌胃天麻素(200 mg·kg~(-1))或与不同剂量(200、400、600 mg·kg~(-1))冰片同时灌胃或预先给予相同剂量(400 mg·kg~(-1))冰片后，用反相高效液相色谱法测定小鼠血浆中天麻素浓度和脑中天麻素浓度。与单用天麻素相比，天麻素与冰片合用可迅速从胃肠道吸收，血浆中天麻素的达峰时间缩短(5~15min比30min)，天麻素在脑内的生物利用度提高33.6~108.8%，具有明显的脑靶向性。冰片剂量过大(600 mg·kg~(-1))或冰片与天麻素之间的时间间隔超过40min时，其促进作用减弱。结果表明，冰片可促进天麻素在胃肠道的吸收，并促进其在脑内的分布。因此，冰片是一种很有前途的口服脑靶向给药促进剂。
Both borneol and gastrodin are bioactive substances derived from traditional Chinese medicine. In this paper, the effect of borneol on the distribution of gastrodin to the brain in mice via oral administration was investigated. Gastrodin concentrations in plasma and gastrodigenin (active metabolite of gastrodin) concentrations in the brain of mice were determined by reversed-phase high-performance liquid chromatography, after intragastric administration of gastrodin (200 mg kg(-1)) alone or combined with different doses (200, 400 and 600 mg kg(-1)) of borneol simultaneously or the same dose (400 mg kg(-1)) of borneol given 20 and 40 min beforehand, respectively. Compared with the administration of gastrodin alone, gastrodin coadministrated with borneol could have been rapidly absorbed from the gastrointestinal tract; the peak time of gastrodin in the plasma became shorter (5-15 vs. 30 min); the bioavailability of gastrodigenin in the brain was increased by 33.6-108.8%; and obvious brain-targeting effect was observed. The enhancing effect was attenuated when the dose of borneol was too high (600 mg kg(-1)), or the time interval between the administration of borneol and gastrodin was longer than 40 min. The results indicate that borneol can accelerate the absorption of gastrodin in the gastrointestinal tract and promote its distribution to the brain. Therefore, borneol is a promising promoter for oral brain-targeting drug delivery.