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洛匹那韦药代动力学的研究进展

姚亚敏,  沐俊,  孙骥,  马芳,  卢洪洲,  张丽军

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文章导航 > 药学实践与服务  > 2012 >  30(5): 336-339
姚亚敏, 沐俊, 孙骥, 马芳, 卢洪洲, 张丽军. 洛匹那韦药代动力学的研究进展[J]. 药学实践与服务, 2012, 30(5): 336-339. doi: 10.3969/j.issn.1006-0111.2012.05.005
引用本文: 姚亚敏, 沐俊, 孙骥, 马芳, 卢洪洲, 张丽军. 洛匹那韦药代动力学的研究进展[J]. 药学实践与服务, 2012, 30(5): 336-339. doi: 10.3969/j.issn.1006-0111.2012.05.005
shu
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
shu

洛匹那韦药代动力学的研究进展

doi: 10.3969/j.issn.1006-0111.2012.05.005
  • 1.

    上海市公共卫生临床中心, 上海 201508

  • 2.

    苏州大学医学部, 江苏 苏州 215123

基金项目: 抗艾滋病病毒新药临床评价研究技术平台建设(2012ZX09303013);成人艾滋病适宜治疗策略研究与应用(2012ZX10001003)

Progress on pharmacokinetics of lopinavir

  • 1.

    Shanghai Public Health Clinical Center, Shanghai 201508, China

  • 2.

    Medical College of Suzhou University, Suzhou 215123, China

  • 摘要: 洛匹那韦作为第二代蛋白酶抑制剂,在艾滋病治疗领域得到广泛应用。然而,该药能被代谢酶CYP3A4快速代谢,在临床应用中,存在较大的个体差异。因此,对洛匹那韦进行药代动力学分析,了解其血药浓度与疗效以及不良反应的关系对优化临床用药具有重要意义。本文全面综述了近年来洛匹那韦浓度分析方法、药代动力学研究进展,为日后洛匹那韦治疗药物监测以及个体化用药研究提供归纳总结材料。
    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.
  • [1] Faux J, Venisse N, Olivie PJ,et al. Rapid high-performance liquid chromatography determination of lopinavir, a novel HIV-1 protease inhibitor, in human plasma[J]. Chromatographia, 2001, 54:469.
    [2] Jaspervander L,Anchalee A.clinical pharmacology and pharmacokinetics of antiretrovirals in Asia[J]. Asian Biomedicine,2009,3(1):53.
    [3] Eric D,Veronique R, Francois R, et al. A population approach to study the influence of nevirapine administration on lopinavir pharmacokinetics in HIV-1 infected patients[J]. Eur J Clin Pharmacol,2005,61:153.
    [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.
    [20] Natella R, John A, Aline B, et al.Population pharmacokinetics of lopinavir predict suboptimal therapeutic concentrations in treatment-experienced human immunodeficiency virus-infected children[J]. Antimicrob Agents Ch,2009, 53(6):2532.
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  • 收稿日期:  2011-12-06
  • 修回日期:  2012-01-14

洛匹那韦药代动力学的研究进展

doi: 10.3969/j.issn.1006-0111.2012.05.005
  • 1. 上海市公共卫生临床中心, 上海 201508
  • 2. 苏州大学医学部, 江苏 苏州 215123
    • 基金项目:  抗艾滋病病毒新药临床评价研究技术平台建设(2012ZX09303013);成人艾滋病适宜治疗策略研究与应用(2012ZX10001003)
  • 收稿日期: 2011-12-06
  • 修回日期: 2012-01-14

摘要: 洛匹那韦作为第二代蛋白酶抑制剂,在艾滋病治疗领域得到广泛应用。然而,该药能被代谢酶CYP3A4快速代谢,在临床应用中,存在较大的个体差异。因此,对洛匹那韦进行药代动力学分析,了解其血药浓度与疗效以及不良反应的关系对优化临床用药具有重要意义。本文全面综述了近年来洛匹那韦浓度分析方法、药代动力学研究进展,为日后洛匹那韦治疗药物监测以及个体化用药研究提供归纳总结材料。

English Abstract

姚亚敏, 沐俊, 孙骥, 马芳, 卢洪洲, 张丽军. 洛匹那韦药代动力学的研究进展[J]. 药学实践与服务, 2012, 30(5): 336-339. doi: 10.3969/j.issn.1006-0111.2012.05.005
引用本文: 姚亚敏, 沐俊, 孙骥, 马芳, 卢洪洲, 张丽军. 洛匹那韦药代动力学的研究进展[J]. 药学实践与服务, 2012, 30(5): 336-339. doi: 10.3969/j.issn.1006-0111.2012.05.005
shu
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
shu

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