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Intracellular pharmacokinetic study of zidovudine and its phosphorylated metabolites

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Acta Pharmaceutica Sinica B 2016年第2期6卷 158-162页

作者： Lingli Mu Rui Zhou Fang Tang Xingling Liu Sanwang Li Feifan Xie Xiang Xie Jie Peng Peng Yu Medical College Hunan Normal University School of Pharmaceutical Sciences Central South University

zidovudine (AZT), the first drug approved by the US Food and Drug Administration for the treatment of human immunodeficiency virus (HIV) infection, is metabolized in the host cells to 5'-AZT triphosphate (AZT-TP) which inhibits HIV reverse transcriptase. As the pharmacokinetics of AZT and its phosphorylated metabolites in human peripheral blood mononuclear cells (hPBMCs) is limited, the aim of this study was to determine the pharmacokinetic parameters of AZT and its phosphorylated metabolites in hPBMCs from 12 healthy Chinese male subjects after a single oral dose of 600 mg of AZT. Blood samples were collected prior to drug administration, then at 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8 and 10 h after drug administration. Mononuclear cells collected by Ficoll-Hypaque density gradient centrifugation were used for determination of AZT and metabolites [AZT monophosphate (AZT-MP), AZT diphosphate (AZT-DP) and AZT-TP] and the plasma was used to evaluate the pharmacokinetics of AZT. Plasma concentration of AZT peaked within 0.583 h and intracellular concentrations of AZT, AZT-MP, AZT-DP and AZT-TP peaked within 1.083, 1.500, 1.417 and 1.583 h, respectively. AZT in plasma was eliminated rapidly with t(1/2) of 2.022 h, and AZT-MP, AZT-DP and AZT-TP were eliminated with t(1/2) of 13.428, 8.285 and 4.240 h, respectively. The plasma concentration of the phosphorylated metabolites was not quantifiable. (C) 2016 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.

关键词： LC-MS/MS zidovudine Metabolites Phosphates hPBMCs hPBMCs Pharmacokinetics Intracellular killed

Determination of zidovudine using anion exchange chromatography with integrated pulsed amperometric detection

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Chinese Chemical Letters 2012年第6期23卷 715-718页

作者： Yu Chen Yu Xiu Liu Zhi Dong Chen Mei Lan Chen Yan Zhu Hangzhou Vocational and Technical College Hangzhou 310018 China School of Chemistry and Chemical Engineering Changzhou University Changzhou 213164 China College of Biology and Envinonment Engineering. Zhejiang Shuren University l-langzhou 310015 China Department of Chemistry Zhejiang University Hangzhou 310028 China

A rapid and practical method for direct detection of zidovudine in high performance anion exchange chromatography （HPAEC） has been developed with integrated pulsed amperometric detection （IPAD）. Dionex AS18 （250mm × 2mm） and AG18 （50 mm× 2 mm） columns and 11 mmol/L NaOH solution were used for separation. Multi-step potential waveform parameters were optimized to maximize the signal-to-noise ratio （S/N）. Utilizing an optimized waveform, the repeatability （intra-day） precision and intermediate （inter-day） precision are obtained with relative standard deviation （RSD） of 1.88, 2.27, respectively. The limit of quantification （LOQ） and limit of detection （LOD） were found to be 9.70, 3.0 ng/mL, respectively, with correlation coefficients of 0.9992 over concentration range 0.01-10 μg/mL. The present method was successfully applied to the determination of zidovudine in human plasma. The recoveries of plasma sample spiked by 0.7 μg/mL, 2.7 μg/mL obtained were 95.3-101.5%, with relative standard deviation （RSD） of 2.54%, 2.21%, respectively.

关键词： zidovudine AIDS Integrated pulsed amperometry High performance anion exchange chromatography Plasma

ORIGINAL ARTICLE Development and validation of a normal-phase HPTLC method for the simultaneous analysis of Lamivudine and zidovudine in fixed-dose combination tablets

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Journal of Pharmaceutical Analysis 2012年第2期2卷 152-155页

作者： Palani Venkatesh Mahesh Daggumati Mother Theresa Post Graduate and Research Institute of Health Sciences Pondicherry UniversityPondicherry 605006India KMCH College of Pharmacy Kovai EstateKalapatti RoadCoimbatore 641048India

Simultaneous quantification of Lamivudine and zidovudine in tablets by HPTLC method was developed and *** chromatograms were developed using a mobile phase of toluene:ethyl acetate:methanol (4:4:2,v/v/v) on pre-coated plate of silica gel GF aluminum TLC plate and quantified by densitometric absorbance mode at 276 *** R f values were 0.4170.03 and 0.6070.04 for Lamivudine and zidovudine,*** linearity of the method was found to be within the concentration range of 50 250 ng/spot for Lamivudine and for zidovudine,it was 100 500 ng/*** lower limits of detection and quantification were 2.23 ng/spot and 7.90 ng/spot for Lamivudine and 2.90 ng/spot and 8.85 ng/spot for *** method was also validated for precision,specificity and *** developed method was used to analyze fixed-dose tablets (Duovir,Cipla Ltd) samples of Lamivudine and zidovudine.

关键词： Normal-phase HPTLC Lamivudine zidovudine Methanol

Steady-state pharmacokinetics of zidovudine in Chinese HIV-infected patients

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Chinese Medical Journal 2012年第11期125卷 1931-1935页

作者： LIU Li-feng WANG Lu FU Qiang ZHU Zhu XIE Jing HAN Yang LIU Zheng-yin YE Min LI Tai-sheng Department of Infectious Diseases Peking Union Medical College Hospital Peking Union Medical College Beijing 100730 China Department of Pharmacology Peking Union Medical College Hospital Peking Union Medical College Beijing 100730 China Chinese Academy of Medical Sciences STD/AIDS Research Center Beijing You An Hospital Capital Medical University Beijing 100071 China

Background The pharmacokinetics of zidovudine （AZT） are possibly influenced by weight, age, sex, liver and renal functions, severity of disease, and ethnicity. Currently, little information is available on the steady-state pharmacokinetics of AZT in Chinese HIV-infected patients. The current study aimed to characterize the steady-state pharmacokinetics of AZT in a Chinese set-up. Methods Eleven Chinese HIV-infected patients were involved in the steady-state pharmacokinetic study. In total, 300 mg of AZT, as a part of combination therapy, was given to patients, and serial blood samples were collected for 12 hours. The samples were measured by a high-performance liquid chromatography （HPLC） assay, and the results were analyzed by both the non-compartment model and the one-compartment model. Results The Cmax of AZT in Chinese patients was higher than that in non-Asian patients. The half-life of AZT, analyzed by the non-compartment model （P=-0.02）, in male patients （（1.02±0.22） hours） was shorter than that of AZT in female patients （（1.55±0.29） hours）. The AZT clearance, analyzed by the one-compartment model （P=0.045）, in male patients （（262.60±28.13） L/h） was higher than that in female patients （（195.85±60.51） L/h）. Conclusion The present study provides valuable information for the clinical practice of AZT-based highly active antiretroviral therapy in a Chinese set-up.

关键词： human immunodeficiency virus, steady-state pharmacokinetics zidovudine Chinesepatients

An antiretroviral regimen containing 6 months of stavudine followed by long-term zidovudine for first-fine HIV therapy is optimal in resource-limited settings： a prospective, multicenter study in China

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Chinese Medical Journal 2014年第1期127卷 59-65页

作者： Li Taisheng Guo Fuping Li Yijia Zhang Chengda Han Yang Lye Wei He Yun Lu Hongzhou Xie Jing Huang Aiqiong Li Yanling Tang Xiaoping Wang Hui Zhang Tong Gao Guiju Lei Junkang Zhang Xiaoying Wu Xinhua Sun Yongtao Bai Jinsong Luo Ling Wang Huanlmg Department of Infectious Diseases Peking Union Medical College Hospital Chinese Academy of Medical Sciences Beijing 100730China The infectious Disease Hospital of Henan Province ZhengzhouHenan 450061 China Shanghai Public Health Clinical Center Fudan University Shanghai201508 China Fuzhou Infectious Diseases Hospital Fujian Medical UniversityFuzhou Fujian 350002 China Guangzhou No. 8 People's Hospital Guangzhou Guangdong 510060 China Shenzhen Third People's Hospital Shenzhen Guangdong 518112China Beijing You'an Hospital Capital Medical University Beijing 100054China Beijing Ditan Hospital Capital Medical University Beijing 100011China Yunnan AIDS Care Center Kunming Yunnan 650000 China The First People's Hospital of Honghe State Honghe Yunnan 650000 China Tangdu Hospital Affiliated to the Fourth Military Medical University Xi'an Shaanxi 710038 China Kunming Third People's Hospital Kunming Yunnan 650041 China

Background An zidovudine （AZT）-substitution regimen containing 24-week stavudine （d4T） followed by long-term AZT for HIV therapy is potential to trade off short-term AZT-related anemia and long-term risks associated with d4T in resourcelimited ***,evidence is *** study aims to assess the efficacy and safety of AZT-substitution regimen,aiming to find a regimen with better efficacy,less adverse events,and more affordability in resource-limited *** This prospective,multicenter study enrolled 499 （190 on d4T regimen,172 on AZT regimen,and 137 on AZT-substitution regimen） HIV-1-infected subjects who initiated combined antiretroviral therapy and attended follow-up visits over 96 weeks from 2009 to *** （3TC） and either nevirapine （NVP） or efavirenz （EFV） were the other two drugs in the antiretroviral *** and immunologic responses and adverse events were monitored at baseline and at weeks 4,12,24,36,48,60,72,84,and *** In terms of hematological adverse effects,AZT-substitution group had similar safety profiles to d4T group and was superior to AZT *** comparison with AZT-substitution group,AZT group was associated with higher risk of developing anemia （adjusted hazard ratio （aHR）for anemia ≥ grade Ⅱ,8.44,95％ CI 1.81-39.46） and neutropenia （aHR for neutropenia ≥ grade Ⅱ,1.86,95％ CI 1.19-2.93）.The prevalence of lipodystrophy in d4T group was 19.5％,while that in AZT-substitution group was *** to antiretroviral efficacy,these three groups showed no *** AZT-substitution regimen provides a relatively safe and effective first-line antiretroviral strategy in resource-limited settings.

关键词： human immunodeficiency virus acquired immunodeficiency syndrome antiretroviral therapy zidovudine stavudine anemia lipodystrophy

Determination of the Antiretroviral Drug zidovudine in Diluted Alkaline Electrolyte by Adsorptive Stripping Voltammetry at the Mercury Film Electrode

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American Journal of Analytical Chemistry 2011年第2期2卷 223-234页

作者： Arnaldo Aguiar Castro Ricardo Queiroz Aucélio Nicolás Adrián Rey Eliane Monsores Miguel Percio Augusto Mardini Farias 不详

This paper describes a stripping method for the determination of zidovudine at the submicromolar concentration levels. This method is based on the controlled adsorptive accumulation of zidovudine at the thin-film mercury electrode, followed by a linear-sweep stripping voltammetry measurement of the surface species. Optimal experimental conditions include a NaOH solution of 2.0 × 10–3 mol●L–1 (sup-porting electrolyte), an accumulation potential of –0.30 V and a scan rate of 100 mV?s–1. The response of zidovudine is linear over the concentration range 0.01 - 0.08 ppm. After an accumulation time of 5 minutes, the detection limit was found to be 0.67 ppb (2.5 × 10–9 mol●L–1). More convenient methods to measure zidovudine concentration in the presence of the didanosine, acyclovir, nevirapine, lamivudine, and efavirenz, were also investigated. The presence of zidovudine together with ATP or ssDNA demonstrates the utility of this method.

关键词： zidovudine Determination Antiviral Drugs Ssdna Thin-Film Mercury Electrode Stripping Voltammetry

Simultaneous quantitation of lamivudine,zidovudine and nevirapine in human plasma by liquid chromatography-tandem mass spectrometry and application to a pharmacokinetic study

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Acta Pharmaceutica Sinica B 2012年第5期2卷 472-480页

作者： Murali Krishna Matta Nageswara Rao Pilli Jaswanth Kumar Inamadugu Laxminarayana Burugula Seshagiri Rao JVLN College of Pharmaceutical Sciences Jawaharlal Nehru Technological UniversityKukatpallyHyderabad 500085India Analytical and Environmental Chemistry Division Department of ChemistrySri Venkateswara UniversityTirupati 517502India College of Pharmaceutical Sciences Andhra UniversityVisakhapatnam 530003India

A rapid and sensitive LC-MS/MS method for the simultaneous quantitation of lamivudine,zidovudine and nevirapine in human plasma using abacavir as internal standard has been developed and *** analytes and IS were extracted from plasma by solid phase extraction using Oasis HLB cartridges and separated on a Hypurity Advance C18 column using a mixture of acetonitrile:0.1% formic acid(76:24,v/v)at a flow rate of 0.8 mL/*** involved an API-4000 LC MS/MS with electrospray ionization in the positive ion mode and multiple-reaction monitoring for *** method was validated according to FDA guidelines and shown to provide intra-and inter-day precision and accuracy within acceptable limits in a run time of only 3.5 *** method was sucessfully applied to a pharmacokinetic study involving a single oral administration of a combination tablet to human male volunteers.

关键词： Lamivudine zidovudine Nevirapine Solid phase extraction LC-MS/MS Pharmacokinetics

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叠氮胸苷zidovudine

药学进展 1989年第4期 44-45页

作者：廖清江

由Burroughs Wellcome公司开发的抗病毒药,已于1987年在英国首次上市。它原为美国密西根Detroit肿瘤研究所于1964年报道的化合物(筛选其抗癌活性),后来体外活性筛选试验中,发现它能对抗人类免疫缺陷病毒(Human Immunodeficiency Virus,... 详细信息

由Burroughs Wellcome公司开发的抗病毒药,已于1987年在英国首次上市。它原为美国密西根Detroit肿瘤研究所于1964年报道的化合物(筛选其抗癌活性),后来体外活性筛选试验中,发现它能对抗人类免疫缺陷病毒(Human Immunodeficiency Virus,简称HIV);对早期的获得性免疫缺陷综合症(Acquired Immunodeficiency Syndrome,简称AIDS)及其有关的ARC(AIDS relatedComplex)有临床疗效。1987年美国FDA批准其胶囊作为艾滋病的治疗药,并列为AA类。当年就在美国上市,年销售额4100万美元,1988年销售2.5亿美元,预测1990年销售额将达15.91亿美元。目前已被35个国家批准使用,该药每4 h口服3.5mg/kg或静脉滴注2.5 mg/kg可降低死亡率。

关键词：艾滋病获得性免疫缺陷综合征性病 AIDS zidovudine 抗病毒美元本位币 ARC

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免疫缺陷病治疗药zidovudine

国外医药.合成药.生化药.制剂分册 1989年第2期 110-111页

作者：徐照群

异名 Retrovir 化学名 3′-叠氮基-3′-脱氧胸(腺嘧啶核)苷药效分类免疫缺陷病治疗药开发单位 (日本)公司上市厂商 (日本)公司药理本品(AZT)在人免疫缺陷的病毒(HIV)感染细胞内,通过胸苷激酶、胸苷酸激酶的磷酸化作用,形成活化型三磷酸... 详细信息

异名 Retrovir 化学名 3′-叠氮基-3′-脱氧胸(腺嘧啶核)苷药效分类免疫缺陷病治疗药开发单位 (日本)公司上市厂商 (日本)公司药理本品(AZT)在人免疫缺陷的病毒(HIV)感染细胞内,通过胸苷激酶、胸苷酸激酶的磷酸化作用,形成活化型三磷酸体(AZTTP)。AZTTP竞争性抑制病毒逆转录酶,脱氧胸苷三磷酸代替病毒的DNA,使DNA链中止增长而阻碍病毒繁殖。因为AZTTP对病毒逆转录酶的亲和性比对正常

关键词：免疫缺陷病 AZT 免疫缺损综合征本品中性白细胞 zidovudine 逆转录酶淋巴球大鼠淋巴结肿胀