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HPLC study of pharmacokinetics and tissue distribution of morroniside in rats.

机译:高效液相色谱法研究鼠尾草苷的药代动力学和组织分布。

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摘要

Morroniside is an important constituent of traditional Chinese medicines Fructus Corni with several bioactivities. An HPLC method for determination of morroniside in rat plasma and tissues was developed and the pharmacokinetic and tissue distribution characteristics of morroniside after intravenous and oral administrations were investigated. The bio-samples were prepared based on a simple protein precipitation and the separation of morroniside was achieved on a C(18) column with a mobile phase consisted of acetonitrile-methanol-0.1% formic acid (10:10:80, v/v) at a flow rate of 1.0 ml/min. Chromatograms were monitored at 239 nm and the temperature of column was kept at 25 degrees C. Pharmacokinetic study found that morroniside was absorbed and eliminated rapidly in rat and manifested linear dynamics at 10-40 mg/kg range and absolute bioavailability of morroniside was lower. Tissue distribution showed the highest level was observed in small intestine, then in kidney and stomach, but no morroniside was detected in brain, which indicated that small intestine, kidney and stomach were major distribution tissues of morroniside in rats, and morroniside had difficulty in crossing the blood-brain barrier. It was also found there was no long-term accumulation of morroniside in rat tissues.
机译:沙棘苷是中药F子的重要成分,具有多种生物活性。建立了测定大鼠血浆和组织中morroniside含量的HPLC方法,并研究了静脉和口服给药后morroniside的药代动力学和组织分布特征。基于简单的蛋白质沉淀制备生物样品,并在C(18)色谱柱上进行morroniside的分离,流动相由乙腈-甲醇-0.1%甲酸(10:10:80,v / v)组成)流速为1.0 ml / min。在239 nm处监测色谱图,柱温保持在25°C。药代动力学研究发现,morroniside在大鼠中被快速吸收和消除,并且在10-40 mg / kg范围内表现出线性动力学,而morroniside的绝对生物利用度较低。组织分布显示,在小肠中最高,然后在肾脏和胃中,但在脑中未检测到morroniside,这表明小肠,肾脏和胃是大鼠morroniside的主要分布组织,morroniside难以通过血脑屏障。还发现在大鼠组织中没有长期的morroniside积累。

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