建立并验证一种灵敏的 UPLC-Q-TOF-MS/MS 方法，用于测定大鼠血浆和组织中九种成分的浓度，并将其应用于玄贝百部颗粒的药代动力学和组织分布研究。
Development and Validation of a Sensitive UPLC-Q-TOF-MS/MS for the Measurement of Nine Components in Rat Plasma and Tissues and its Application to Pharmacokinetics and Tissue Distribution Studies with Xuanfei Baidu Granules.
机构信息
State Key Laboratory of Component-based Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China.
Tianjin Modern Innovation Chinese Medicine Technology Co., Ltd., Tianjin 300380, China.
出版信息
Curr Drug Metab. 2022;23(2):150-163. doi: 10.2174/1389200223666220215151245.
BACKGROUND
Xuanfei Baidu granules (XFBD granules) are based on the prescription of Xuanfei Baidu, which showed promise as a first-line treatment against Corona Virus Disease 2019 (COVID-19) in Wuhan, Hubei. On March 2, 2021, XFBD granules were marketed as a novel drug for epidemic diseases. However, there is little information about the pharmacokinetics and tissue distribution of the main constituents in XFBD granules.
METHODS
A sensitive analytical method was developed for detecting the marker components of XFBD granules by ultra-high performance liquid chromatography with quadrupole time-of-flight mass spectrometry (UPLC-Q-TOFMS/ MS), and for studying its pharmacokinetics and tissue distribution by UPLC-QDa.
RESULTS
Following an oral administration of a single granule in experimental rats at a dose of 14 g/kg for pharmacokinetic and tissue distribution studies, 42 compounds and nine analytes were identified in XFBD granules. Nine compounds were detected in the lungs and the liver of the rats. Six compounds were detected in the kidneys. Five compounds were detected in the spleen and three were detected in the heart. As it went undetected in the brain, XFBD granules are considered unable to cross the blood-brain barrier.
CONCLUSION
A sensitive UPLC-Q-TOF-MS/MS method was established and validated for the quantification of nine components in rat plasma and tissue samples. This method was successfully applied to study the pharmacokinetics and tissue distribution profiles of XFBD granules after their oral administration.
背景
宣肺败毒颗粒（XFBD 颗粒）是基于宣肺败毒方的处方，在湖北武汉作为治疗 2019 年冠状病毒病（COVID-19）的一线药物显示出一定的疗效。2021 年 3 月 2 日，XFBD 颗粒被作为一种新型的治疗传染病的药物上市。然而，XFBD 颗粒中主要成分的药代动力学和组织分布信息很少。
方法
采用超高效液相色谱-四极杆飞行时间质谱（UPLC-Q-TOFMS/MS）建立了一种用于检测 XFBD 颗粒中标记成分的灵敏分析方法，并采用 UPLC-QDa 研究其药代动力学和组织分布。
结果
在实验大鼠中以 14 g/kg 的剂量口服单粒进行药代动力学和组织分布研究后，在 XFBD 颗粒中鉴定出 42 种化合物和 9 种分析物。在大鼠的肺和肝脏中检测到 9 种化合物。在肾脏中检测到 6 种化合物。在脾脏中检测到 5 种化合物，在心脏中检测到 3 种化合物。由于在大脑中未检测到 XFBD 颗粒，因此认为其不能穿过血脑屏障。
结论
建立并验证了一种灵敏的 UPLC-Q-TOF-MS/MS 方法，用于定量测定大鼠血浆和组织样品中的 9 种成分。该方法成功应用于研究口服 XFBD 颗粒后的药代动力学和组织分布特征。
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