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目的建立测定人血浆中西替利嗪浓度的方法,对国产盐酸西替利嗪咀嚼片和进口普通片进行生物等效性研究。方法18名健康男性志愿者按2×2交叉试验方案设计,分别口服受试制剂和参比制剂各10 mg,并采集36 h内动态血标本;采用LC-ESI-MS/MS法测定血浆中西替利嗪浓度,计算药动学参数,并判定2种制剂是否生物等效。结果受试制剂和参比制剂的主要药动学参数ρmax分别为(320.51±44.13)μg·L-1和(325.59±40.02)μg·L-1,tmax均为(1.3±0.3)h,AUC0→36h分别为(2 811.1±346.3)μg·h·L-1和(2 862.9±427.3)μg·h·L-1,AUC0→∞分别为(2 915.3±390.3)μg·h·L-1和(2 959.1±459.3)μg·h·L-1,t(1/2)(ke)分别为(7.20±1.44)h和(6.95±1.20)h,两制剂主要药动学参数经对数转换后进行方差分析及双单侧t检验,并计算90%置信区间,表明两种制剂生物等效,受试制剂的人体生物利用度为(99.04±10.59)%。结论国产盐酸西替利嗪咀嚼片和其进口普通片生物等效。
Abstract：AIM To establish the method to study the bioequivalence of cetirizine hydrochloride chewable tablets (test) and common tablets(reference) in healthy Chinese volunteers.METHODS 10 mg test and 10 mg reference preparations were given to 18 male healthy volunteers in a randomized two-period crossover design for the pharmacokinetic and relative bioavailability study.Plasma cetirizine was determined by LC-ESI-MS/MS.RESULTS The main pharma- cokinetic parameters of the two preparation were as follows:ρmax(320.51±44.13)μg·L-1 and(325.59±40.02)μg·L-1,tmax(1.3±0.3)h and (1.3±0.3)h ,AUC0→36h(2 811.1±346.3)μg·h·L-1 and (2 862.9±427.3)μg·h·L-1,AUC0→∞(2 915.3±390.3)μg·h·L-1 and (2 959.1±459.3)μg·h·L-1,t1/2(ke)(7.20±1.44)h and (6.95±1.20) h,respectively.The mean relative bioavailability of test preparation vs reference preparation were (99.04±10.59)%.CONCLUSION Statistical analysis confirms bioequivalent of the two preparations.
[1]徐学君，王永英．西替利嗪的临床应用概况[J]．国外医学情报，1999，20(7)：13．
[ 2] Paw B,Misztal G,Hopkala H,et al.Development and validation of a HPLC method for the determination of cetirizine in pharmaceutical dosage forms[ J ] .Pharmazie,2002,57(5):313.
[ 3] Jaber AM,Al Sherife HA,Al Omari MM,et al.Determination of ceti- rizine dihydrochloride,related impurities and preservatives in oral solu- tion and tablet dosage forms using HPLC [ J ].Pharm Biomed Anal, 2004,36(2):341.
[ 4] Valli A,Pelettini A,Papa P,et al.Comprehensive drug screening by in- tegratod use of gas chromatography/mass spectrometry and Remedi HS [J] .Therapeutic Drug Monitoring,2001,23(3):287.
[5] Song Q,Junga H,Tang Y,et al.Antomatod 96-well solid phase extrac- tion and hydrophilic interaction liquid chromatography-tandem mass spec- trometric method for the analysis of cetirizine (ZYRTEC) in human plas- ma-with emphasis on method ruggedness[J].Chromatogr B Analyt Tech- nol Biomed Life Sci ,2005,814(1):105.
[6] Gupta A,Jansson B,Chatelain P,et al.Quantitative determination of ce- tirizine enantiomers in guinea pig plasma,brain tissue and microdialysis samples using liquid chromatography/tandem mass spectrometry [ J ]. Rapid Commun Mass Spectrom,2005,19(12):1749.
[7] Ma M,Feng F,Sheng Y,et al.Development and evaluation of an effi- cient HPLC/MS/MS method for the simultaneous determination of pseu- doephedrine and cetirizine in human plasma:application to phase-Ⅰpharmcokinetic study [J].Chromatogr B Analyt Technol Biomed Life Sci ,2007,846(1-2):105.
[7]de Jager AD,Hundt HK,Swart KJ,et al.Extractionless and sensitive method for high-throughput quantitation of cetirizine in human plasma samples by liquid chromatography-tandem mass spectrometry[J].Chro- matogr B Analyt Technol Biomed Life Sci,2002,773(2):113.
基本信息:
DOI：10.19577/j.cnki.issn10074406.2008.04.012
中图分类号:R96
引用信息:
[1]邱畅,温预关,李烜,等.LC-ESI-MS/MS法测定人血浆中西替利嗪浓度及其咀嚼片人体生物等效性评价[J].中国临床药学杂志,2008(04):234-238.DOI:10.19577/j.cnki.issn10074406.2008.04.012.
2008-07-25
2008-07-25