Pharmacokinetic of 5 components after oral administration of Fructus Forsythiae by HPLC-MS/MS and the effects of harvest time and administration times
Pharmacokinetic of 5 components after oral administration of Fructus Forsythiae by HPLC-MS/MS and the effects of harvest time and administration times
复制标题
HPLC-MS/MS测定连翘口服后5种成分的药代动力学及采收时间和给药次数的影响
DOI：
10.1016/j.jchromb.2015.04.041
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发表时间：
2015-07-01
影响因子：
3
通讯作者：
Chang, Yan-xu
中科院分区：
文献类型：
--
作者：
Bai, Yang;Li, Jin;Chang, Yan-xu
未熟连翘和成熟连翘是连翘市售连翘的两种临床形态。关于未成熟和成熟连翘体内活性成分药代动力学特性差异的信息有限。开发并验证了快速灵敏的液相色谱-串联质谱 (LC-MS/MS) 方法，可同时测定大鼠血浆中 9 种典型成分。九种分析物的分离在 Eclipse plus C18 (4.6 mm x 100 mm, 1.8 μm) 柱上进行，流动相由 0.1% 甲酸的水和乙腈混合物组成。方法验证表明该方法快速、特异、灵敏。结果发现，大鼠单次口服生连翘提取物后，5种成分（连翘苷A、芦丁、连翘苷、异鼠李素和槲皮素）的AUC（（0-24h））与单剂量口服成熟连翘提取物后的AUC（（0-24h））也有显着差异。多次口服连翘提取物后5种成分的全身暴露量较单次口服后显着增加。结果表明，采收时间不仅影响连翘活性成分的含量，而且影响其生物利用度，提示不同采收时间的商品连翘临床剂型会改变药物代谢的速率和程度。给药次数会影响连翘活性成分的生物利用度。 (C) 2015 Elsevier B.V. 保留所有权利。
The unripe Fructus Forsythiae (Qingqiao) and ripe Fructus Forsythiae (Laoqiao) are two types of the clinical forms of commercial fructus of Forsythia suspensa(Thunb.) Vahl. There is limited information available for differences in pharmacokinetic properties of active components between unripe and ripe Fructus Forsythiae in vivo. A rapid and sensitive liquid chromatography-tandem mass spectrometric (LC-MS/MS) method was developed and validated for the simultaneous determination of 9 typical components in rat plasma. The separation of nine analytes was performed on an Eclipse plus C18 (4.6 mm x 100 mm, 1.8 mu m) column with the mobile phases consisted of a mixture of 0.1% formic acid in water and acetonitrile. Method validation indicated that the developed method was rapid, specific and sensitive. It was found that the AUC((0-24h)) of 5 ingredients (forsythoside A, rutin, phillyrin, isorhamnetin and quercetin) in rats after single orally administrated unripe Fructus Forsythiae also had significant differences compared with those after single dose oral administration of ripe Fructus Forsythiae extract. The systemic exposure of 5 ingredients after multiple oral administration of Fructus Forsythiae extract had significantly increased than those after single oral administration. The results indicated that harvest time is not only effects the contents but the bioavailability of active components of Fructus Forsythiae, which suggests that the rate and extent of drug metabolism were altered when the clinical forms of commercial Fructus Forsythiae with different harvest time. The administration times could influence the bioavailability of active components of Fructus Forsythiae. (C) 2015 Elsevier B.V. All rights reserved.