Cui Xiao-Bing, Qian Xiao-Cui, Huang Ping, Zhang Yong-Xin, Li Jun-Song, Yang Guang-Ming, Cai Bao-Chang
College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210023, China.
Jiangsu Provincial TCM Engineering Technology Research Center of High Efficient Drug Delivery System, Nanjing, 210023, China.
Biomed Chromatogr. 2015 Jul;29(7):1112-23. doi: 10.1002/bmc.3398. Epub 2014 Dec 26.
Radix Scutellariae (RS) is a herbal medicine with various pharmacological activities to treat inflammation, respiratory and gastrointestinal infections, etc. In this study, a rapid, sensitive and selective UPLC-ESI-MS/MS method was developed for simultaneous determination of 10 flavonoids - scutellarin, scutellarein, chrysin, wogonin, baicalein, apigenin, wogonoside, oroxylin A-7-O-glucuronide, oroxylin A and baicalin - from RS aqueous extracts in rat plasma with propyl paraben as internal standard (IS). Chromatographic separation was achieved on a C18 column using gradient elution with the mobile phase consisting of methanol and water (containing 0.1% formic acid) at a flow rate of 0.2 mL/min. The detection was performed in multiple reaction monitoring mode using electrospray ionization in negative mode. The validated method showed good linearity over a wide concentration range (r >0.9935). The intra- and interday assay variabilities were <9.5% and <12.4% for all analytes, respectively. The extraction recovery ranged from 71.2 to 89.7% for each analyte and IS. This method was successfully applied to pharmacokinetic comparision after oral administration of crude and wine-processed RS aqueous extracts. There were significant differences in some pharmacokinetic parameters of most analytes between crude and wine-processed RS. This suggested that wine-processing exerted effects absorption of most flavonoids.
黄芩是一种具有多种药理活性的草药,可用于治疗炎症、呼吸道和胃肠道感染等。在本研究中,建立了一种快速、灵敏且选择性高的超高效液相色谱-电喷雾串联质谱(UPLC-ESI-MS/MS)方法,以对羟基苯甲酸丙酯作为内标(IS),同时测定大鼠血浆中黄芩水提取物中的10种黄酮类化合物——黄芩苷、黄芩素、白杨素、汉黄芩素、黄芩苷元、芹菜素、汉黄芩苷、木犀草素-7-O-葡萄糖醛酸苷、木犀草素和黄芩苷。采用C18色谱柱,以甲醇和水(含0.1%甲酸)为流动相进行梯度洗脱,流速为0.2 mL/min,实现色谱分离。采用电喷雾电离负离子模式,在多反应监测模式下进行检测。验证后的方法在较宽的浓度范围内具有良好的线性关系(r>0.9935)。所有分析物的日内和日间测定变异系数分别<9.5%和<12.4%。各分析物和内标的提取回收率在71.2%至89.7%之间。该方法成功应用于黄芩生品和酒炙品水提取物口服给药后的药代动力学比较。黄芩生品和酒炙品中大多数分析物的一些药代动力学参数存在显著差异。这表明酒炙对大多数黄酮类化合物的吸收有影响。