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YAO Ya-min, MU Jun, SUN Ji, MA Fang, LU Hong-zhou, ZHANG Li-jun. Progress on pharmacokinetics of lopinavir[J]. Journal of Pharmaceutical Practice and Service, 2012, 30(5): 336-339. doi: 10.3969/j.issn.1006-0111.2012.05.005
Citation: YAO Ya-min, MU Jun, SUN Ji, MA Fang, LU Hong-zhou, ZHANG Li-jun. Progress on pharmacokinetics of lopinavir[J]. Journal of Pharmaceutical Practice and Service, 2012, 30(5): 336-339. doi: 10.3969/j.issn.1006-0111.2012.05.005

Progress on pharmacokinetics of lopinavir

doi: 10.3969/j.issn.1006-0111.2012.05.005
  • Received Date: 2011-12-06
  • Rev Recd Date: 2012-01-14
  • Lopinavir was widely used as a second generation protease inhibitor in AIDS therapy, which was quickly metabolized by CYP3A4. For individual variance might lead to different metabolism, it was important to study the pharmacokinetic parameters of lopinavir and learn the relationship between drug concentration and curative effect or adverse reactions. The methods for determining lopinavir concentration and the progress of pharmacokinetic research were reviewed in this paper which might offer some help for treatment drug monitoring (TDM) and personalized dosage research.
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    [4] Matthias G, Stephanie R, Stephanie L,et al. Pharmacogenomic adaptation of antiretroviral therapy:overcoming the failure of lopinavir in an African infant with CYP2D6 ultrarapid metabolism[J]. Eur J Clin Pharmacol,2010,66:107.
    [5] Rajasekhar D, Jaswanthumar I, Ravik, et al. Simultaneous determination of ritonavir and lopinavir in human plasma after protein precipitation and LC-MS-MS[J]. Chromatographia, 2010, 71:815.
    [6] Difrancesco R, Dicenzo R, Vicente G, et al. Determination of lopinavir cerebral spinal fluid and plasma ultrafiltrate concentrations by liquid chromatography coupled to tandem mass spectrometry[J]. J Pharm Biomed Anal, 2007, 44 (5):1139.
    [7] Frerichs VA, Difrancesco R, Morse GD. Determination of protease inhibitors using liquid chromatography-tandem mass spectrometry[J]. J Chromatogr B Analyt Technol Biomed Life Sci, 2003, 787(2):393.
    [8] Perry GW, Jack SW, Grace K, et al. Validation and application of a high-performance liquid chromatography-tandem mass spectrometric method for simultaneous quantification of lopinavir and ritonavir in human plasma usingsemi-automated 96-well liquid-liquid extraction[J]. J Chromatogr A, 2006,1130:302.
    [9] Yoshiko USAMI, Tsuyoshi OKI, Masahiko NAKAI, et al.A simple HPLC method for simultaneous determination of lopinavir,ritonavir and efavirenz[J]. Chem Pharm Bull,2003, 51(6):715.
    [10] Rita CEE, Fabio SR, Brayan VS, et al.Determination of lopinavir and ritonavir in blood plasma, seminal plasma, saliva and plasmaultra-filtrate by liquid chromatography/tandem mass spectrometry detection[J]. Rapid Commun Mass Spectrom,2008,22:657.
    [11] Manuela E, Marion M, Walter EH, et al. Monitoring of lopinavir and ritonavir in peripheral blood mononuclear cells, plasma, and ultrafiltrate using a selective and highly sensitive LC/MS/MS assay[J]. J Chromatogr B, 2007, 850:249.
    [12] Manish Y, Rajasekhar R, Hemal K,et al. Application of a rapid and selective method for the simultaneous determination of protease inhibitors, lopinavir and ritonavir in human plasma by UPLC-ESI-MS/MS for bioequivalence study in Indian subjects[J]. J Pharmaceut Biomed,2009, 49:1115.
    [13] Heinea R,Rosinga H,Gorpb ECM,et al.Quantification of protease inhibitors and non-nucleoside reverse transcriptase inhibitors in dried blood spots by liquid chromatography-triple quadrupole mass spectrometry[J]. J Chromatogr B,2008,867:208.
    [14] Yao Y,Sun J,Chen J,et al.LC-MS/MS method for simultaneous quantification of lopinavir and ritonavir in human plasma[J]. Acta Pharmaceut Sin,2010, 45 (2):279.
    [15] Slish JC,Catnzaro LM, Ma Q,et al. Update on the pharmacokinetic aspects of antiretroviral agents:implications in therapeutic drug monitoring[J]. Current Pharmaceutical Design, 2006, 12:1129.
    [16] Van Heeswijk RPG, Bourbeau M, Seguin I, et al. Absence of circadian variation in the pharmacokinetics of lopinavir/ritonavir given as a once daily dosing regimen in HIV-1-infected patients[J]. Br J Clin Pharmacol, 2005, 59 (4):398.
    [17] Gondi NK, Venkata KJ, Marianne KJ,et al. Metabolism and disposition of the HIV-1 protease inhibitor lopinavir (ABT-378) given in combination with ritonavir in rats, dogs, and humans[J]. Pharmacol Res, 2004, 21(9):1622.
    [18] Jackson A, Hill A, Puls R,et al.Pharmacokinetics of plasma lopinavir/ritonavir following the administration of 400/100 mg, 200/150 mg and 200/50 mg twice daily in HIV-negative volunteers[J]. J Antimicro Chemoth,2011,66(3):635.
    [19] Ann H, Jeffrey I, Scott B. Pharmacokinetic-pharmacodynamic analysis of lopinavir-ritonavir in combination with efavirenz and two nucleoside reverse transcriptase inhibitors in extensively pretreated human immunodeficiency virus-infected patients[J]. Antimicrob Agents Ch,2003, 47(1):350.
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Progress on pharmacokinetics of lopinavir

doi: 10.3969/j.issn.1006-0111.2012.05.005

Abstract: Lopinavir was widely used as a second generation protease inhibitor in AIDS therapy, which was quickly metabolized by CYP3A4. For individual variance might lead to different metabolism, it was important to study the pharmacokinetic parameters of lopinavir and learn the relationship between drug concentration and curative effect or adverse reactions. The methods for determining lopinavir concentration and the progress of pharmacokinetic research were reviewed in this paper which might offer some help for treatment drug monitoring (TDM) and personalized dosage research.

YAO Ya-min, MU Jun, SUN Ji, MA Fang, LU Hong-zhou, ZHANG Li-jun. Progress on pharmacokinetics of lopinavir[J]. Journal of Pharmaceutical Practice and Service, 2012, 30(5): 336-339. doi: 10.3969/j.issn.1006-0111.2012.05.005
Citation: YAO Ya-min, MU Jun, SUN Ji, MA Fang, LU Hong-zhou, ZHANG Li-jun. Progress on pharmacokinetics of lopinavir[J]. Journal of Pharmaceutical Practice and Service, 2012, 30(5): 336-339. doi: 10.3969/j.issn.1006-0111.2012.05.005
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