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采用高效液相色谱法对小鼠口服和静脉注射牡荆素-4''-O-葡萄糖苷后的排泄情况进行比较研究。

Comparative study on the excretion of vitexin-4''-O-glucoside in mice after oral and intravenous administration by using HPLC.

作者信息

Cai Shuang, Chen Yinghui, Zhang Wenjie, Ying Xixiang

机构信息

Department of Pharmacy, The First Affiliated Hospital of China Medical University, 155 Nanjing Street, Shenyang, 110001, People's Republic of China.

出版信息

Biomed Chromatogr. 2013 Nov;27(11):1375-9. doi: 10.1002/bmc.2931. Epub 2013 Jun 13.

Abstract

The aim of the present study was to characterize the excretion of pure vitexin-4"-O-glucoside (VOG) in mice following oral and intravenous administration at a dose of 30 mg/kg. A sensitive and specific HPLC method with hespridin as internal standard, a Diamonsil C18 column protected with a KR C18 guard column and a mixture consisting of methanol-acetonitrile-tetrahydrofuran-0.1% glacial acetic acid (6:2:18:74, v/v/v/v) as mobile phase was developed and validated for quantitative analysis in biological samples. VOG could be excreted as prototype in excreta including urine and feces after both routes of administration, and the cumulative excretion of VOG was 24.31 ± 11.10% (17.97 ± 5.59% in urinary excretion; 6.34 ± 5.51% in fecal excretion) following oral dosing and 5.66 ± 3.94% (4.78 ± 3.13% in urinary excretion; 0.88 ± 0.81% in fecal excretion) following intravenous dosing. The results showed that the elimination of VOG after the two routes was fairly low, which meant that VOG was metabolized as other forms and the elimination after oral dosing was almost 4.3-fold that after intravenous dosing. For both routes of administration, VOG excreted as prototype in urine was much more than that in feces, nearly 2.83-fold for oral administration and 5.43-fold for intravenous administration, which should be attributed to enterohepatic circulation. Taken together, renal excretion was the dominant path of elimination of VOG for oral and intravenous administration in mice and biliary excretion contributed less.

摘要

本研究的目的是表征小鼠经口和静脉注射30mg/kg剂量的纯牡荆素-4''-O-葡萄糖苷(VOG)后的排泄情况。建立了一种以橙皮苷为内标、采用KR C18保护柱的Diamonsil C18柱、以甲醇-乙腈-四氢呋喃-0.1%冰醋酸(6:2:18:74,v/v/v/v)组成的混合物为流动相的灵敏且特异的HPLC方法,并对其在生物样品中的定量分析进行了验证。两种给药途径后,VOG均可以原型形式排泄到尿液和粪便等排泄物中,经口给药后VOG的累积排泄率为24.31±11.10%(尿排泄率为17.97±5.59%;粪排泄率为6.34±5.51%),静脉给药后为5.66±3.94%(尿排泄率为4.78±3.13%;粪排泄率为0.88±0.81%)。结果表明,两种给药途径后VOG的消除率相当低,这意味着VOG被代谢为其他形式,且经口给药后的消除率几乎是静脉给药后的4.3倍。对于两种给药途径,以原型形式经尿液排泄的VOG远多于经粪便排泄的VOG,经口给药时约为2.83倍,静脉给药时约为5.43倍,这应归因于肝肠循环。综上所述,肾排泄是小鼠经口和静脉注射VOG后消除的主要途径,胆汁排泄的作用较小。

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