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Validated UPLC/Q-TOF-MS Method for Determination of Poliumoside in Rat Plasma and Its Application to Pharmacokinetic Study

机译:经验证的UPLC / Q-TOF-MS方法测定大鼠血浆中的Pol药苷及其在药代动力学研究中的应用

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Poliumoside is the main active constituent of Callicarpa kwangtungensis Chun (CK), a traditional Chinese medicine for management of hemostasis. In this study, a rapid and selective ultra-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UPLC/ Q-TOF-MS) method was developed and validated to quantify poliumoside in rat plasma. The targeted analytes in rat plasma were prepared through protein-precipitation method using 10% trichloroacetic acid (TCA). The chromatographic separation was performed on a Waters BEH C18 column (2.1 × 100 mm, 1.7 μm) by acetonitrile-water containing 0.1% formic acid. The calibration curve was linear over the range of 50 - 10,000 ng/mL (r2 > 0.99). The intra-day or inter-day precision was less than 7.97% and accuracy was within ?7.00% - 3.36%. The developed method was successfully applied to pharmacokinetic study of poliumoside in rat plasma. Although being rapidly absorbed (Tmax ≤ 30 min), poliumoside was poorly bioavailable after oral administration (the absolute bioavailability was only 0.69%).
机译:ium虫苷是广东止血中药Callicarpa kwangtungensis Chun(CK)的主要活性成分。在这项研究中,快速和选择性的超高效液相色谱结合四极杆飞行时间质谱(UPLC / Q-TOF-MS)方法得到了开发,并经过验证可以定量大鼠血浆中的lium苷。使用10%三氯乙酸(TCA)通过蛋白质沉淀法制备大鼠血浆中的目标分析物。色谱分离是在Waters BEH C18色谱柱(2.1×100 mm,1.7μm)上,通过含有0.1%甲酸的乙腈-水进行的。校准曲线在50-10,000 ng / mL的范围内呈线性(r2> 0.99)。日内或日间精度小于7.97%,精度在7.00%-3.36%之内。该方法成功应用于大鼠血浆中applied药苷的药代动力学研究。尽管po药苷吸收迅速(Tmax≤30分钟),但口服后的生物利用度很差(绝对生物利用度仅为0.69%)。

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