天津中医药2018，Vol.35Issue(7)：535-538,4.DOI:10.11656/j.issn.1672-1519.2018.07.16
黄芩苷纳米混悬剂大鼠体内药代动力学研究
Pharmacokinetics of baicalin nanosuspension in rats
摘要
Abstract
[Objective] To establish a liquid chromatography-mass spectrometry (LC-MS/MS) method to evaluate its pharmacokinetics in rats. [Methods] ALC-MS/MS method that column of Waters ACQUITY UPLC-HSS C18(1.8 μm, 2.1 mm×50 mm)and a mixture of 0.1% formic acid water solution (A)-acetonitrile (B) as the mobile phase at the flow-rate of 0.3 mL/min, the column temperature was 30℃and the injection volume was 5 μL. Carbamazepine was used as the internal standard, detection was by postive ion electrospray ionization (ESI) mass spectrometry with multiple-reaction monitoring (MRM). Detection of ion pairs respectively are m/z 447.09→270.80 for baicalin, m/z 237.10→193.80 for carbamazepine employed to determine the concentration of baicalin in plasma by oral administration in rats and the pharmacokinetics software of WinNonlin version 6.0 was used to calculate the pharmacokinetics parameters. [Results] The linear calibration curves were obtained over the concentration range 24.75~4 950.00 ng/mL. Endogenous substances in the plasma did not interfere with the determination, the recovery rate, matrix effect, precision, accuracy and stability of the method are in accordance with the requirements of biological samples. The Cmax of BL-NSPS and BL-Bulk were (3 329.10±499.10) ng/mL and (1 257.84 ± 158.21) ng/mL, respectively. The Cmax of BL-NSPS was significantly higher than that of BL-Bulk (P＜0.05), and the relative bioavailability of BL-NIPS was (160.97±47.78)%. [Conclusion] The LC-MS/MS method has high accuracy and specificity, and can be used to detect the pharmacokinetics of baicalin. What's more, the experimental results show that baicalin nanosuspensions can increase the absorption rate of drugs, shorten the onset time of the drugs, improve the bioavailability of the drug in vivo and lay a foundation for the further devel-opment of baicalin preparation.关键词
黄芩苷/纳米混悬剂/LC－MS/MS/大鼠/药代动力学Key words
baicalin/nanoparticle/LC-MS/MS/rat/pharmacokinetics分类
医药卫生引用本文复制引用
卢鹏,MAIKHONE VILAKHAMXAY,任 静,邢月,王舒雅,薛志峰,刘志东..黄芩苷纳米混悬剂大鼠体内药代动力学研究[J].天津中医药,2018,35(7):535-538,4.基金项目
国家自然科学基金面上项目(81673605). （81673605）
