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首页> 外文期刊>Acta Pharmacologica Sinica >Distribution of nimodipine in brain following intranasal administration in rats
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Distribution of nimodipine in brain following intranasal administration in rats

机译:鼻内给药后大鼠尼莫地平在脑中的分布

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AIM: To determine whether nasally applied nimodipine (NM) could improve its systemic bioavailability and be transported directly from the nasal cavity to the brain. METHODS: NM was administered nasally, intravenously (iv), and orally to male Sprague-Dawley rats. At different times post dose, blood, cerebrospinal fluid (CSF), and brain tissue samples were collected, and the concentrations of NM in the samples were analyzed by HPLC. RESULTS: Oral systemic bioavailability of NM in rats was 1.17 %, nasal dosing improved bioavailibility to 67.4 %. Following intranasal administration, NM concentrations in olfactory bulb (OB) within 30 min post dose were found significant higher than in the other brain tissues. However, similar NM levels in different brain regions were observed after iv injection. AUC in CSF and OB from the nasal route was 1.26 and 1.39 fold compared with the iv route, respectively. The brain-to-plasma AUC ratios were significantly higher after nasal administration than after iv administration (P<0.01). CONCLUSION: Nasally administered NM could markedly improve the bioavailability and a fraction of the NM dose could be transported into brain via the olfactory pathway in rats.
机译:目的:确定经鼻应用的尼莫地平(NM)是否可以改善其全身生物利用度,并将其直接从鼻腔转运至大脑。方法:对雄性Sprague-Dawley大鼠经鼻,静脉(iv)和口服给予NM。在给药后的不同时间,收集血液,脑脊液(CSF)和脑组织样品,并通过HPLC分析样品中NM的浓度。结果:NM大鼠的口服全身生物利用度为1.17%,鼻给药提高了67.4%的生物利用度。鼻内给药后,发现给药后30分钟内嗅球(OB)中的NM浓度明显高于其他脑组织。然而,静脉注射后在不同的大脑区域观察到相似的NM水平。鼻内途径的CSF和OB中的AUC分别是静脉内途径的1.26倍和1.39倍。鼻腔给药后脑与血浆的AUC比明显高于静脉内给药(P <0.01)。结论:鼻内施用NM可以显着提高生物利用度,一部分NM剂量可以通过大鼠嗅觉途径转运到大脑。

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