Article(id=1322906772440228413, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1322887634511314961, articleNumber=null, orderNo=null, doi=null, pmid=null, cstr=null, oa=null, hot=null, price=null, onlineType=0, articleFormat=0, articleType=null, articleTypeStr=null, receivedDate=null, receivedDateStr=null, revisedDate=null, revisedDateStr=null, acceptedDate=1614096000000, acceptedDateStr=2021-02-24, onlineDate=1793335152968, onlineDateStr=2026-10-30, pubDate=1632931200000, pubDateStr=2021-09-30, doiRegisterDate=null, doiRegisterDateStr=null, onlineIssueDate=1793335152968, onlineIssueDateStr=2026-10-30, onlineJustAcceptDate=null, onlineJustAcceptDateStr=null, onlineFirstDate=null, onlineFirstDateStr=null, sourceXml=null, magXml=null, createTime=1793335152968, creator=13701087609, updateTime=1793335152968, updator=13701087609, issue=Issue{id=1322887634511314961, tenantId=1146029695717560320, journalId=1235980733773295621, year='2021', volume='30', issue='18', pageStart='1633', pageEnd='1728', issueExtLink='null', onlineDate='null', pubDate='1632931200000', pubDateStr='2021-09-30', beforeIssueId=null, nextIssueId=null, price=null, status=1, issueComplete=1, articleOrder=1, issueType=-1, specialIssue=null, createTime=1793330590131, creator='13701087609', updateTime=1793337355310, updator='13701087609', preIssue=null, nextIssue=null, articleTotal=null, ext={EN=IssueExt(id=1322916009916629692, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1322887634511314961, language=EN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=), CN=IssueExt(id=1322916009916629693, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1322887634511314961, language=CN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=)}, issueFiles=null, downloadFileDto=null}, startPage=1703, endPage=1708, ext={EN=ArticleExt(id=1322906772612194878, articleId=1322906772440228413, tenantId=1146029695717560320, journalId=1235980733773295621, language=EN, title=Pharmacokinetic investigation of berberine dernivative WZX20 in rats, columnId=null, journalTitle=Chinese Journal of New Drugs, columnName=null, runingTitle=null, highlight=null, articleAbstract=
Objective:

To study the pharmacokinetics of berberine dernivative WZX20 in rats.

Methods:

SD rats were intragastrically (ig) or intravenously (iv) given WZX20, and plasma were collected after injection. WZX20 components in plasma were determined by LC-MS. Pharmacokinetic parameters were determined from the plasma concentration-time data with DAS software package.

Results:

The pharmacokinetic parameters after gastric lavage were as follows: AUC0→t (596.46±22.22) ng·h·mL-1; AUC0-∞ (607.59±23.51) ng·h·mL-1; t1/2 (1.76±0.15) h; CL (32.96±1.3) L·h·kg-1; Vd (83.62±7.54) L·kg-1; Cmax (172.98±13.51) ng·mL-1; Tmax (0.5) h; F=33.19%. The intravenous pharmacokinetics parameters were as follows: AUC0→t (177.61±30.52) ng·h·mL-1; AUC0→∞(183.08±30.90) ng·h·mL-1; t1/2 (1.74±0.17) h; CL (11.23±2.18) L·h·kg-1; Vd (25.17±6.81) L·kg-1.

Conclusion:

The established LC-Ms method is accurate, sensitive and rapid, and can be used for the blood concentration determination of WZX20. The pharmacokinetic parameters of WZX20 provide a good foundation for the study on the druggability of WZX20.

, authors=Gao-feng ZHU1, 2, Rui CHEN2, Yi-ming ZHANG3, Kai-hong ZHU3, Jian-ta WANG3, Lei TANG2, authorsList=Gao-feng ZHU, Rui CHEN, Yi-ming ZHANG, Kai-hong ZHU, Jian-ta WANG, Lei TANG, authorCompany=null, correspAuthors=Lei TANG, authorNote=null, correspAuthorsNote=null, copyrightStatement=null, copyrightOwner=null, extLink=null, articleAbsUrl=null, sourceXml=null, magXml=null, pdfUrl=null, pdf=null, pdfFileSize=null, pdfExtLink=null, richHtmlUrl=null, mobilePdfUrl=null, reviewReport=null, pdfFirstPage=null, abstractGraph=null, abstractGraphContent=null, abstractVideo=null, citation=null, cebUrl=null, magXmlContent=null, mapNumber=null, fund=null), CN=ArticleExt(id=1322906772918379071, articleId=1322906772440228413, tenantId=1146029695717560320, journalId=1235980733773295621, language=CN, title=黄连素衍生物WZX20在大鼠体内的药动学研究, columnId=1236330556003242277, journalTitle=中国新药杂志, columnName=实验研究, runingTitle=null, highlight=null, articleAbstract=
目的:

考察黄连素衍生物WZX20在大鼠体内的药动学特征。

方法:

将SD大鼠分别灌胃和尾静脉注射WZX20,采集不同时间点血样,LC-MS测定WZX20浓度,用DAS 2.0软件进行药动学分析。

结果:

WZX20灌胃药动学参数:AUC0→t为(596.46±22.22)ng·h·mL-1,AUC0-∞为(607.59±23.51)ng·h·mL-1,t1/2为(1.76±0.15)h,CL为(32.96±1.3)L·h·kg-1,Vd为(83.62±7.54)L·kg-1,Cmax为(172.98±13.51)ng·mL-1,Tmax为0.5 h,F为33.19%;WZX20静脉注射药动学参数:AUC0→t为(177.61±30.52)ng·h·mL-1,AUC0→∞为(183.08±30.90)ng·h·mL-1,t1/2为(1.74±0.17)h,CL为(11.23±2.18)L·h·kg-1,Vd为(25.17±6.81)L·kg-1。

结论:

本实验建立的检测方法专属性强、灵敏度高、准确度好,适用于WZX20血药浓度的测定。WZX20在大鼠体内的药-时曲线特征符合血管外给药一级吸收二室模型。WZX20的药动学参数为其成药性评价研究奠定了基础。

, authors=朱高峰1, 2, 陈瑞2, 张倚鸣3, 朱开红3, 王建塔3, 汤磊2, authorsList=朱高峰, 陈瑞, 张倚鸣, 朱开红, 王建塔, 汤磊, authorCompany=null, correspAuthors=汤磊, authorNote=

朱高峰,男,博士,主要从事药物合成与药物分析。E-mail:。

, correspAuthorsNote=
汤磊,男,教授,博士生导师,主要从事药物化学研究。联系电话:(0851)86908318,E-mail:。
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黄连素衍生物WZX20在大鼠体内的药动学研究
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朱高峰 1, 2 , 陈瑞 2 , 张倚鸣 3 , 朱开红 3 , 王建塔 3 , 汤磊 2
中国新药杂志 | 实验研究 2021,30(18): 1703-1708
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中国新药杂志 |实验研究 2021 , 30 (18) : 1703 -1708
黄连素衍生物WZX20在大鼠体内的药动学研究
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朱高峰1, 2 , 陈瑞2, 张倚鸣3, 朱开红3, 王建塔3, 汤磊2
作者信息
  • 1贵州医科大学基础医学院,贵阳 550025
  • 2贵州省化学合成药物研发利用工程技术研究中心,贵阳 550025
  • 3贵州医科大学药学院,贵阳 550025
通讯作者:
汤磊,男,教授,博士生导师,主要从事药物化学研究。联系电话:(0851)86908318,E-mail:。
作者简介:

朱高峰,男,博士,主要从事药物合成与药物分析。E-mail:。

Pharmacokinetic investigation of berberine dernivative WZX20 in rats
Gao-feng ZHU1, 2 , Rui CHEN2, Yi-ming ZHANG3, Kai-hong ZHU3, Jian-ta WANG3, Lei TANG2
Affiliations
  • 1School of Basic Medical Sciences, Guizhou Medical University, Guiyang 550025, China
  • 2Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guiyang 550025, China
  • 3School of Pharmacy, Guizhou Medical University, Guiyang 550025, China
出版时间: 2021-09-30
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目的:

考察黄连素衍生物WZX20在大鼠体内的药动学特征。

方法:

将SD大鼠分别灌胃和尾静脉注射WZX20,采集不同时间点血样,LC-MS测定WZX20浓度,用DAS 2.0软件进行药动学分析。

结果:

WZX20灌胃药动学参数:AUC0→t为(596.46±22.22)ng·h·mL-1,AUC0-∞为(607.59±23.51)ng·h·mL-1,t1/2为(1.76±0.15)h,CL为(32.96±1.3)L·h·kg-1,Vd为(83.62±7.54)L·kg-1,Cmax为(172.98±13.51)ng·mL-1,Tmax为0.5 h,F为33.19%;WZX20静脉注射药动学参数:AUC0→t为(177.61±30.52)ng·h·mL-1,AUC0→∞为(183.08±30.90)ng·h·mL-1,t1/2为(1.74±0.17)h,CL为(11.23±2.18)L·h·kg-1,Vd为(25.17±6.81)L·kg-1。

结论:

本实验建立的检测方法专属性强、灵敏度高、准确度好,适用于WZX20血药浓度的测定。WZX20在大鼠体内的药-时曲线特征符合血管外给药一级吸收二室模型。WZX20的药动学参数为其成药性评价研究奠定了基础。

黄连素  /  衍生物  /  药动学  /  生物利用度  /  液质联用
Objective:

To study the pharmacokinetics of berberine dernivative WZX20 in rats.

Methods:

SD rats were intragastrically (ig) or intravenously (iv) given WZX20, and plasma were collected after injection. WZX20 components in plasma were determined by LC-MS. Pharmacokinetic parameters were determined from the plasma concentration-time data with DAS software package.

Results:

The pharmacokinetic parameters after gastric lavage were as follows: AUC0→t (596.46±22.22) ng·h·mL-1; AUC0-∞ (607.59±23.51) ng·h·mL-1; t1/2 (1.76±0.15) h; CL (32.96±1.3) L·h·kg-1; Vd (83.62±7.54) L·kg-1; Cmax (172.98±13.51) ng·mL-1; Tmax (0.5) h; F=33.19%. The intravenous pharmacokinetics parameters were as follows: AUC0→t (177.61±30.52) ng·h·mL-1; AUC0→∞(183.08±30.90) ng·h·mL-1; t1/2 (1.74±0.17) h; CL (11.23±2.18) L·h·kg-1; Vd (25.17±6.81) L·kg-1.

Conclusion:

The established LC-Ms method is accurate, sensitive and rapid, and can be used for the blood concentration determination of WZX20. The pharmacokinetic parameters of WZX20 provide a good foundation for the study on the druggability of WZX20.

berberine  /  derivatives  /  pharmacokinetics  /  bioavailability  /  LC-MS
朱高峰, 陈瑞, 张倚鸣, 朱开红, 王建塔, 汤磊. 黄连素衍生物WZX20在大鼠体内的药动学研究. 中国新药杂志, 2021 , 30 (18) : 1703 -1708 .
Gao-feng ZHU, Rui CHEN, Yi-ming ZHANG, Kai-hong ZHU, Jian-ta WANG, Lei TANG. Pharmacokinetic investigation of berberine dernivative WZX20 in rats[J]. Chinese Journal of New Drugs, 2021 , 30 (18) : 1703 -1708 .
  • 贵州省化学合成药物研发利用工程技术研究中心平台项目(黔科合[2016]平台人才5402)
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2021年第30卷第18期
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  • 首发时间:2026-10-30
  • 出版时间:2021-09-30
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  • 录用日期:2021-02-24
基金
贵州省化学合成药物研发利用工程技术研究中心平台项目(黔科合[2016]平台人才5402)
作者信息
    1贵州医科大学基础医学院,贵阳 550025
    2贵州省化学合成药物研发利用工程技术研究中心,贵阳 550025
    3贵州医科大学药学院,贵阳 550025

通讯作者:

汤磊,男,教授,博士生导师,主要从事药物化学研究。联系电话:(0851)86908318,E-mail:。
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2种不同金属材料的力学参数
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genus
种数
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species
占总种数比例
Percentage of
total species (%)
属
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种数
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species
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Percentage of total
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鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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