Article(id=1291404591573233853, tenantId=1146029695717560320, journalId=1246415772164075586, issueId=1291404554201985968, articleNumber=null, orderNo=null, doi=10.13699/j.cnki.1001-6821.2025.06.020, pmid=null, cstr=null, oa=null, hot=null, price=null, onlineType=0, articleFormat=0, articleType=null, articleTypeStr=null, receivedDate=1728489600000, receivedDateStr=2024-10-10, revisedDate=null, revisedDateStr=null, acceptedDate=null, acceptedDateStr=null, onlineDate=1785824447768, onlineDateStr=2026-08-04, pubDate=1743091200000, pubDateStr=2025-03-28, doiRegisterDate=null, doiRegisterDateStr=null, onlineIssueDate=1785824447768, onlineIssueDateStr=2026-08-04, onlineJustAcceptDate=null, onlineJustAcceptDateStr=null, onlineFirstDate=null, onlineFirstDateStr=null, sourceXml=null, magXml=null, createTime=1785824447767, creator=13701087609, updateTime=1785824447767, updator=13701087609, issue=Issue{id=1291404554201985968, tenantId=1146029695717560320, journalId=1246415772164075586, year='2025', volume='41', issue='6', pageStart='751', pageEnd='900', issueExtLink='null', onlineDate='null', pubDate='1743091200000', pubDateStr='2025-03-28', beforeIssueId=null, nextIssueId=null, price=null, status=1, issueComplete=1, articleOrder=1, issueType=-1, specialIssue=null, createTime=1785824438858, creator='13701087609', updateTime=1785824438858, updator='13701087609', preIssue=null, nextIssue=null, articleTotal=null, ext=null, issueFiles=null, downloadFileDto=null}, startPage=857, endPage=861, ext={EN=ArticleExt(id=1291404591795531966, articleId=1291404591573233853, tenantId=1146029695717560320, journalId=1246415772164075586, language=EN, title=Determination of carfilzomib concentration in rat plasma by HPLC-MS/MS and pharmacokinetic study, columnId=1246531413395263850, journalTitle=Chinese Journal of Clinical Pharmacology, columnName=Research Method, runingTitle=null, highlight=null, articleAbstract=
Objective To establish a method for the determination of carfilzomib in rat plasma by high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS), and to investigate the pharmacokinetic characteristics of carfilzomib in rat plasma.
Methods The rat plasma samples were processed by a protein precipitation approach using methanol∶acetonitrile (1∶1, v/v). Chromatographic column: Thermo ScientificTM Hypersil GOLDTM C18 Column (2.1 mm×50.0 mm, 3 μm); mobile phase: 2 mmol·L-1 ammonium acetate-0.02% formic acid water (A)-methanol (B) in gradient elution mode; flow rate: 0.45 mL·min-1; injection volume: 5 μL. Electrospray ionization source in positive ion mode and multiple reaction monitoring were adopted. The specificity, standard curve and lower limit of quantification, residue effect, precision and extraction recovery rate, dilution reliability, matrix effect and stability of this method were examined. After a single intravenous injection of 4 mg·kg-1 carfilzomib into 6 healthy male SD rats, blood was collected from the inner corner of the eye, and the concentration of carfilzomib in the plasma was detected. The pharmacokinetic parameters were calculated using DAS 3.0.
Results Carfilzomib exhibited good specificity and linearity within the range of 0.5 to 1 250.0 ng·mL-1, with a standard curve of y=2.40×10-2x+6.81×10-2 (r=0.996 4), the quantitative limit of detection was 0.5 ng·mL-1, the sample residues were 7.64% and 1.00% of the quantitative limit of detection and the internal standard, respectively, the intra-day and inter-day precision were ≤7.51% and ≤8.16%, respectively, the intra-day and inter-day accuracy were -4.54% to 5.14% and -4.41% to 8.26%, respectively, the extraction recovery were 92.49% to 108.33%, and the methodological evaluation results of sample dilution effect, matrix effect and stability were all in accordance with the requirements for the validation of biological sample analysis methods. The main pharmacokinetic parameters of carfilzomib were: Cmax was (1.10×106±5.45×105) ng·L-1, t1/2 was (23.10±7.38) min, AUC0-t was (1.85×107±9.85×106) ng·L-1·min.
Conclusion The approach formulated in this study is operationally facile, highly discriminatory, sensitive, precise, dependable, and is appropriate for the determination and analysis of carfilzomib in rat plasma specimens.
, authors=Bo LIANG, Wei-wei XIE, Yu-qian ZHANG, Zhi-qing ZHANG, Yi-ran JIN, authorsList=Bo LIANG, Wei-wei XIE, Yu-qian ZHANG, Zhi-qing ZHANG, Yi-ran JIN, authorCompany=null, correspAuthors=Yi-ran JIN, 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=1291404592076550335, articleId=1291404591573233853, tenantId=1146029695717560320, journalId=1246415772164075586, language=CN, title=用HPLC-MS/MS法测定大鼠血浆中卡非佐米浓度及药代动力学研究, columnId=1246531413600784769, journalTitle=中国临床药理学杂志, columnName=研究方法, runingTitle=null, highlight=null, articleAbstract=
目的 建立一种通过高效液相色谱-串联质谱（HPLC-MS/MS）法测定大鼠血浆中卡非佐米的方法，并研究大鼠血浆中卡非佐米的药代动力学特征。
方法 用甲醇-乙腈（1∶1，v/v）蛋白沉淀法处理大鼠血浆样品。色谱柱：Thermo ScientificTM Hypersil GOLDTM C18 Column（2.1 mm×50.0 mm，3 μm）；流动相：2 mmol·L-1乙酸铵-0.02%甲酸水（A）-甲醇（B）；梯度洗脱；流速：0.45 mL·min-1；进样量：5 μL。电喷雾离子源，正离子模式，多反应离子监测。考察该方法的专属性、标准曲线和定量下限、残留效应、精密度与回收率、稀释效应、基质效应、稳定性。将6只健康雄性SD大鼠单次尾静脉注射4 mg·kg-1卡非佐米后，眼内眦取血，检测大鼠血浆中卡非佐米浓度，用DAS 3.0计算药代动力学参数。
结果 卡非佐米在0.5～1 250.0 ng·mL-1内，专属性及线性关系良好，标准曲线为y=2.40×10-2x+6.81×10-2（r=0.996 4），定量下限为0.5 ng·mL-1，样品残留分别为定量下限和内标的7.64%和1.00%，批内及批间精密度分别为≤7.51%、≤8.16%，批内及批间准确度分别为-4.54%～5.14%、-4.41%～8.26%，提取回收率为92.49%～108.33%，样品稀释效应、基质效应和稳定性的方法学考察结果均符合生物样品分析方法验证的要求。卡非佐米的主要药代动力学参数：Cmax为（1.10×106±5.45×105）ng·L-1，t1/2为（23.10±7.38）min，AUC0-t为（1.85×107±9.85×106）ng·L-1·min。
结论 本研究所建立的方法操作简单，选择性强，灵敏度高，准确可靠，适用于大鼠血浆样品中卡非佐米的测定分析。
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梁博（1990-），女，主管药师，主要从事临床药学方面的工作
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