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引用本文:华雯妍,朱艺芳,张全英.天麻素血药浓度测定及药动学研究[J].中国现代应用药学,2010,27(7):634-636.
.Determination of Gastrodin in Human Plasma by LC-MS/MS and Its Application in Pharmacokinetic Study[J].Chin J Mod Appl Pharm(中国现代应用药学),2010,27(7):634-636.
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天麻素血药浓度测定及药动学研究
华雯妍,朱艺芳,张全英
作者单位
摘要:
目的 建立天麻素血浆药物浓度LC-MS/MS测定法,测定健康受试者血浆中天麻素的浓度并评价天麻素胶囊的药动学。方法 建立以阿昔洛韦为内标的天麻素血药浓度LC-MS/MS测定方法,色谱柱为Atlantics T3(100 mm×3.0 mm,3 μm),流动相为乙腈-水(10∶90),对18名健康受试者单剂量口服150 mg天麻素胶囊进行药动学研究。结果 建立了简单、专属的天麻素血浆药物浓度的LC-MS/MS测定法,以沉淀法进行样品前处理,无杂质干扰测定,灵敏度达到了3.00 ng∙mL-1,每个生物样品分析时间仅为2 min。18名健康受试者口服天麻素胶囊150 mg后,测定血浆样品并估算天麻素的药动学参数,Tmax均值为(0.8±0.3)h,t1/2均值为(2.1±0.4)h,Cmax均值为(378±84)ng∙mL-1,AUC0-12 均值为(878±175)ng∙h∙mL-1,AUC0-∞均值为(897±175)ng∙h∙mL-1。结论 本法快速、准确、灵敏度高且前处理简单,能很好的应用于药动学研究。
关键词:  天麻素  LC-MS/MS  药动学
DOI:
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基金项目:
Determination of Gastrodin in Human Plasma by LC-MS/MS and Its Application in Pharmacokinetic Study
HUA Wenyan  ZHU Yifang  ZHANG Quanying*
Abstract:
OBJECTIVE To determine the plasma concentration of gastrodin and evaluate the pharmacokinetics of the gastrodin capsule. METHODS We developed an LC-MS/MS assay method using aciclovir as the internal standard to determine the plasma concentration of gastrodin. An Atlantics T3 column (100 mm×3.0 mm, 3 μm) and the mobile phase of CH3CN-water (10∶90) were used for LC-ESI (-) and MRM for MS. RESULTS A simple and specific method has been developed to determinate the plasma concentrations of gastrodin by LC-MS/MS. Each plasma sample was preprocessed by adding methanol, and analysised within 2 minutes. No significant interfering peaks were observed. The lower limit of quantitation was 3.00 ng∙mL-1. An oral dose of gastrodin capsules was given to 18 healthy male volunteers. The pharmacokinetic parameters of the test capsule were as follows: the Tmax were (0.8±0.3)h, the t1/2 were (2.15±0.38)h, the Cmax were (378±84) ng∙mL-1, the AUC0-12 were (878±175) ng∙h∙mL-1,the AUC0-∞ were(897±175)ng∙h∙mL-1, respectively. CONCLUSION The method is simple in pretreatment and is rapid, sensitive and accurate in analysis. This method was successfully applied to study the pharmacokinetics of gastrodin in healthy Chinese volunteers.
Key words:  gastrodin  LC-MS/MS  pharmacokinetic
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