[1]方 伟,汪电雷,丁 艳,等.UPLC法测定大鼠血浆中海南粗榧内酯醇及其药代动力学研究[J].中国药理学通报,2018,(09):1263-1267.[doi:10.3969/j.issn.1001-1978.2018.09.016]
 FANG Wei,WANG Dian-lei,DING Yan,et al.Determination of hainanolidol and its pharmacokinetics in rat plasma by UPLC[J].Chinese Pharmacological Bulletin,2018,(09):1263-1267.[doi:10.3969/j.issn.1001-1978.2018.09.016]
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UPLC法测定大鼠血浆中海南粗榧内酯醇及其药代动力学研究()
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《中国药理学通报》[ISSN:/CN:]

卷:
期数:
2018年09期
页码:
1263-1267
栏目:
论著
出版日期:
2018-08-26

文章信息/Info

Title:
Determination of hainanolidol and its pharmacokinetics in rat plasma by UPLC
文章编号:
1001-1978(2018)09-1263-05
作者:
方 伟汪电雷丁 艳吴青青吴 洁姚兆敏
安徽中医药大学药学院,安徽 合肥 230031
Author(s):
FANG WeiWANG Dian-lei DING Yan WU Qing-qing WU Jie YAO Zhao-min
College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230031, China
关键词:
海南粗榧内酯醇 UPLC 大鼠 血药浓度 药代动力学 静脉注射
Keywords:
hainanolidol UPLC rats blood concentration pharmacokinetics intravenous injection
分类号:
R-332; R282.71; R284.1; R452; R446.11; R969.1
DOI:
10.3969/j.issn.1001-1978.2018.09.016
文献标志码:
A
摘要:
目的 采用UPLC建立大鼠血浆中海南粗榧内酯醇浓度测定方法,并研究其经大鼠尾静脉注射给药后初步药代动力学。方法 以甲醇-水(47:53)为流动相,流速0.17 mL·min-1,UV检测波长326 nm,以海南粗榧内酯为内标,乙腈沉淀蛋白,测定给药后海南粗榧内酯醇在大鼠体内的浓度,由DAS2.1软件拟合药动学参数。结果 海南粗榧内酯醇在0.05~10.0 mg·L-1浓度范围内线性关系良好(r=0.999 6),日内和日间差异RSD均小于6%,提取回收率大于85%,方法学考察均符合要求。海南粗榧内酯醇按1、2、4 mg·kg-1尾静脉给药后,在大鼠体内的半衰期T1/2分别为(39.82±0.92)、(40.11±0.79)、(41.61±2.07)min,AUC0-t为(65.77±1.08)、(130.48±1.26)、(268.75±1.24)min·mg·L-1。结论 该方法对海南粗榧内酯醇的专属性较强、快速方便、灵敏度较高,适合大批量生物样本分析。
Abstract:
Aim To establish a UPLC method for the determination of the concentration of hainanolidol in plasma of rats, and study the pharmacokinetics of hainanolidol in rat plasma after single dose i.v. administration of hainanolidol(1, 2, 4 mg·kg-1). Methods The UPLC method for the determination of hainanolidol in rat plasma was established using hainanolide as internal standard. The mobile phase was methanol-water(47:53), the flow rate was 0.17 mL·min-1, and the detection wavelength was UV 326 nm. The plasma concentration of hainanolidol in rats was determined by UPLC after single-dose intravenous injection in rats with 1, 2 and 4 mg·kg-1 of hainanolidol, and the pharmacokinetic parameters were calculated by DAS2.1. Results The result of calibration curve was linear over the range of 0.05~10.00 mg·L-1(r=0.999 6). The lower limit of quantification was 0.05 mg·L-1. The intra-day and inter-day precision were both lower than 5%, and the extraction recoveries were higher than 85%, respectively. The validated method was successfully applied to the pharmacokinetic study after i.v administration of hainanolidol in rats with doses of 1, 2 and 4 mg·kg-1. The T1/2 was(39.82±0.92),(40.11±0.79)and(41.61±2.07)min, respectively. The AUC0-t was(65.77±1.08),(130.48±1.26)and(268.75±1.24)min·mg·L-1, respectively. Conclusion A simple and specific UPLC method for the analysis of hainanolidol is successfully developed, which could be applied to pharmacokinetic study in rat plasma.

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备注/Memo

备注/Memo:
收稿日期:2018-04-14,修回日期:2018-05-16
基金项目:国家自然科学基金资助项目(No 81473536); 安徽省教育厅高等教育振兴计划人才项目(皖教秘[2014]181号)
作者简介:方 伟(1991-),男,硕士生,研究方向:药物代谢动力学,E-mail:498959612@qq.com;
汪电雷(1977-),男,博士,教授,硕士生导师,研究方向:药物代谢动力学,通讯作者,Tel:0551-68129153,E-mail:wdl8105@126.com
更新日期/Last Update: 2018-08-26