Pharmacokinetics and tissue distribution of eupatilin and its metabolite in rats by an HPLC-MS/MS method
文献类型：期刊论文
| 作者 | Wang, Xixiao3; Ren, Jie3; Zhu, Shixing3,4; Ren, Guoqing1,3; Wang, Lei3; Chen, Xiaoyan4 ; Qiu, Zhixia2; Zhang, Chaofeng3
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| 刊名 | JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
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| 出版日期 | 2018-09-10 |
| 卷号 | 159页码:113-118 |
| 关键词 | Eupatilin E-7-G HPLC-MS/MS Pharmacokinetic Tissue distribution |
| ISSN号 | 0731-7085 |
| DOI | 10.1016/j.jpba.2018.06.037 |
| 文献子类 | Article |
| 英文摘要 | Eupatilin, a major pharmacologically active ingredient in Stillen (TM), has been known to possess anti peptic, anti-cancer and anti-allergy activities. A rapid, simple, sensitive and specific high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method for the simultaneous determination of eupatilin and its main metabolite (eupatilin-7 beta-O-glucuronide, E-7-G) in rat plasma and tissues was established and validated. The linear range of eupatilin and E-7-G was 0.20 similar to 500 ng/mL and 1.00-2500 ng/mL, and the lowest limit of quantification (LLOQ) of eupatilin and E-7-G was 0.20 and 1.00 ng/mL, respectively. The inter-day and intra-day precision of this assay was restricted to within 10%, with a highest accuracy of more than 90%. The matrix effect, recovery and stability of both eupatilin and E-7-G were all demonstrated to be within acceptable limits. The validated method was then successfully applied to a pharmacokinetics and tissue distribution study. The absolute bioavailability (F) of eupatilin was estimated to be 2.7%. After intravenous administration, eupatilin was degraded with high clearance (14.82 L/kg/h) and a short half-life t(1/2) (0.29 h). Eupatilin was rapidly metabolized to E-7-G with systemic exposure at 1288.8 ng h ml(-1), while the levels of the latter declined more slowly, with a longer t(1/2) (4.15 h). Moreover, both eupatilin and E-7-G were widely distributed across various tissues, including the liver, kidney and intestine. Taken together, eupatilin showed poor absorption, extensive metabolism into E-7G and a wide tissue distribution, especially in the intestine. These pharmacokinetic results yield helpful insights into the pharmacological actions of eupatilin. (C) 2018 Elsevier B.V. All rights reserved. |
| WOS关键词 | KAPPA-B ; CELLS ; ARTEMISIA ; MICE ; INFLAMMATION ; INHIBITION ; APOPTOSIS ; PROTECTS ; DAMAGE |
| 资助项目 | National Natural Science Foundation of China[81573553] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000442699900014 |
| 出版者 | ELSEVIER SCIENCE BV |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279583]  |
| 专题 | 上海药物代谢研究中心 |
| 通讯作者 | Qiu, Zhixia; Zhang, Chaofeng |
| 作者单位 | 1.Liaoning Univ Tradit Chinese Med, Coll Pharm, Dalian 116600, Peoples R China; 2.China Pharmaceut Univ, Sch Tradit Chinese Pharm, Dept Pharmacol Chinese Materia Med, 639 Longmian Rd, Nanjing 211198, Jiangsu, Peoples R China; 3.China Pharmaceut Univ, Sch Tradit Chinese Pharm, Res Dept Pharmacognosy, State Key Lab Nat Med, Nanjing 211198, Jiangsu, Peoples R China; 4.Chinese Acad Sci, Shanghai Inst Materia Med, 501 Haike Rd, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Xixiao,Ren, Jie,Zhu, Shixing,et al. Pharmacokinetics and tissue distribution of eupatilin and its metabolite in rats by an HPLC-MS/MS method[J]. JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,2018,159:113-118. |
| APA | Wang, Xixiao.,Ren, Jie.,Zhu, Shixing.,Ren, Guoqing.,Wang, Lei.,...&Zhang, Chaofeng.(2018).Pharmacokinetics and tissue distribution of eupatilin and its metabolite in rats by an HPLC-MS/MS method.JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,159,113-118. |
| MLA | Wang, Xixiao,et al."Pharmacokinetics and tissue distribution of eupatilin and its metabolite in rats by an HPLC-MS/MS method".JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS 159(2018):113-118. |
入库方式： OAI收割
来源：上海药物研究所
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