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The role of formulation on the pharmacokinetics of antiretroviral drugs

, PharmD, , PhD (Faculty of Associated Medical Sciences) , , PharmD PhD & , PharmD PhD

Bibliography

  • UNAIDS. Global Report. UNAIDS Report on the global AIDS epidemic 2013. UNIAIDS, Geneva, Switzerland; 2013
  • UNAIDS. GR2013 HIV estimates with uncertainty bounds. Available from: www.unaids.org/en/media/unaids/contentassets/documents/epidemiology/2013/gr2013/gr2013_hiv [Last accessed 20 January 2014]
  • World Health Organization. Consolidated guidelines on the use of antiretroviral drugs for treating and preventing HIV infection. Recommendations for a public health approach. WHO, Geneva, Switzerland; 2013
  • Panel on Antiretroviral Therapy and Medical Management of HIV-Infected Children. Guidelines for the use of antiretroviral agents in pediatric HIV infection. Available from: http://aidsinfo.nih.gov/contentfiles/lvguidelines/pediatricguidelines.pdf [Last accessed 7 August 2013]
  • Neely MN, Rakhmanina NY. Pharmacokinetic optimization of antiretroviral therapy in children and adolescents. Clin Pharmacokinet 2011;50:143–89
  • Abdel-Rahman SM, Amidon GL, Kaul A, et al. Summary of the National Institute of Child Health and Human Development-best pharmaceuticals for Children Act Pediatric Formulation Initiatives Workshop-Pediatric Biopharmaceutics Classification System Working Group. Clin Pharmacokinet 2012;34:S11-24
  • Buggins TR, Dickinson PA, Taylor G. The effects of pharmaceutical excipients on drug disposition. Adv Drug Deliv Rev 2007;59:1482-503
  • Goole J, Lindley DJ, Roth W, et al. The effects of excipients on transporter mediated absorption. Int J Pharm 2010;393:17-31
  • Panakanti R, Narang AS. Impact of excipient interactions on drug bioavailability from solid dosage forms. Pharm Res 2012;29:2639-59
  • European Medicines Agency: Committee for Medicinal Products for Human use (CHMP). Guideline on the investigation of bioequivalence. 2010. Avaialble from http://CPMP/EWP/QWP/1401/98Rev.1/Corr
  • U.S. Food and Drug Administration: center for Drug Evaluation and Research. Guidance for industry: waiver of in vivo bioavailability and bioequivalence studies for immediate-release solid oral dosage forms on a biophamaceutics classification system. 2000. Available from: www.fda.gov/downloads/Drugs/Guidances/ucm070246.pdf
  • Aulton ME, Taylor KMG. Aulton’s pharmaceutics, the design and manufacture of medicines. 4th edition. Churchill Livingstone, London, UK; 2013
  • Amidon GL, Lennernas H, Shah VP, et al. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 1995;12:413-20
  • Lindenberg M, Kopp S, Dressman JB. Classification of orally administered drugs on the World Health Organization Model list of Essential Medicines according to the biopharmaceutics classification system. Eur J Pharm Biopharm 2004;58:265-78
  • Oral formulations platform. Inter-agency agreement between the Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) and the U.S. Food and Drug Administration (FDA). Available from: http://bpca.nichd.nih.gov/collaborativeefforts/initiatives/index.cfm [Last accessed 29 September 2013]
  • FDA; US Food and Drug Administration. Available from: www.accessdata.fda.gov/drugsatfda_docs [Last accessed January 2014]
  • EMA; European Medicines Agency. Available from: www.ema.europa.eu/docs [Last accessed January 2014]
  • Ruela Correa JC, D’Arcy DM, dos Reis Serra CH, et al. Darunavir: a critical review of its properties, use and drug interactions. Pharmacology 2012;90:102-9
  • Mathias A, Menning M, Wiser L, et al. Bioequivalence of the emtricitabine/rilpivirine/tenofovir disoproxil fumarate single tablet regimen. J Bioequiv Availab 2012;4:100-5
  • Chen ML, Straughn AB, Sadrieh N, et al. A modern view of excipient effects on bioequivalence: case study of sorbitol. Pharm Res 2007;24:73-80
  • Olagunju A, Owen A, Cressey TR. Potential effect of pharmacogenetics on maternal, fetal and infant antiretroviral drug exposure during pregnancy and breastfeeding. Pharmacogenomics 2012;13:1501-22
  • Benet LZ, Broccatelli F, Oprea TI. BDDCS applied to over 900 drugs. AAPS J 2011;13:519-47
  • Wu CY, Benet LZ. Predicting drug disposition via application of BCS: transport/absorption/elimination interplay and development of a biopharmaceutics drug disposition classification system. Pharm Res 2005;22:11-23
  • European Medicines Agency: committee for Medicinal Products for Human use (CHMP). Reflection paper: formulations of choice for the paediatric population. 2006. Available from: http://EMEA/CHMP/PEG/194810/2005
  • Debra Boxwell KC, Linda Lewis, Kendall Marcus, Bindi Nikhar. Kaletra® oral solution toxicity in neonates—lopinavir, ethanol, and/or propylene glycol? 18th CROI Conference on Retroviruses and Opportunistic Infections; 27 February – 2 March 2011; Boston, Massachusetts, USA
  • U.S. Department of Health and Human Services F, Center for Drug Evaluation and Research (CDER). Guidance for industry: fixed dose combinations, co-packaged drug products, and single-entity versions of previously approved antiretrovirals for the treatment of HIV. 2006. Available from: www.fda.gov/ForConsumers/ByAudience/ForPatientAdvocates/HIVandAIDSActivities/ucm124426.htm
  • Breitkreutz J, Boos J. Paediatric and geriatric drug delivery. Expert Opin Drug Deliv 2007;4:37-45
  • Merck Sharp & Dohme Limited; Stocrin®. Summary of product characteristics. Available from: www.ema.europa.eu/ema/ [Last accessed 25 September 2013]
  • ter Heine R, Scherpbier HJ, Crommentuyn KM, et al. A pharmacokinetic and pharmacogenetic study of efavirenz in children: dosing guidelines can result in subtherapeutic concentrations. Antivir Ther 2008;13:779-87
  • Salem AH, Fletcher CV, Brundage RC. Pharmacometric characterization of efavirenz developmental pharmacokinetics and pharmacogenetics in HIV-infected children. Antimicrob Agents Chemother 2014;58:136-43
  • Wang LH, Wiznia AA, Rathore MH, et al. Pharmacokinetics and safety of single oral doses of emtricitabine in human immunodeficiency virus-infected children. Antimicrob Agents Chemother 2004;48:183-91
  • Gilead Sciences Inc. Emtriva®. Label information. Available from: www.accessdata.fda.gov/Scripts/cder/DrugsatFDA/ [Last accessed 8 August 2013]
  • Vanprapar N, Cressey TR, Chokephaibulkit K, et al. A chewable pediatric fixed-dose combination tablet of stavudine, lamivudine, and nevirapine: pharmacokinetics and safety compared with the individual liquid formulations in human immunodeficiency virus-infected children in Thailand. Pediatr Infect Dis J 2010;29:940-4
  • Chokephaibulkit K, Cressey TR, Capparelli E, et al. Pharmacokinetics and safety of a new paediatric fixed-dose combination of zidovudine/lamivudine/nevirapine in HIV-infected children. Antivir Ther 2011;16:1287-95
  • Kasirye P, Kendall L, Adkison KK, et al. Pharmacokinetics of antiretroviral drug varies with formulation in the target population of children with HIV-1. Clin Pharmacol Ther 2012;91:272-80
  • Bouazza N, Hirt D, Bardin C, et al. Is the recommended once-daily dose of lamivudine optimal in West African HIV-infected children? Antimicrob Agents Chemother 2010;54:3280-6
  • Bouazza N, Hirt D, Blanche S, et al. Developmental pharmacokinetics of lamivudine in 580 pediatric patients ranging from neonates to adolescents. Antimicrob Agents Chemother 2011;55:3498-504
  • Burger DM, Verweel G, Rakhmanina N, et al. Age-dependent pharmacokinetics of lamivudine in HIV-infected children. Clin Pharmacol Ther 2007;81:517-20
  • Tremoulet AH, Nikanjam M, Cressey TR, et al. Developmental pharmacokinetic changes of lamivudine in infants and children. J Clin Pharmacol 2012;52:1824-32
  • Yuen GJ, Morris DM, Mydlow PK, et al. Pharmacokinetics, absolute bioavailability, and absorption characteristics of lamivudine. J Clin Pharmacol 1995;35:1174-80
  • Corbett AH, Hosseinipour MC, Nyirenda J, et al. Pharmacokinetics of generic and trade formulations of lamivudine, stavudine and nevirapine in HIV-infected Malawian children. Antivir Ther 2010;15:83-90
  • Esseku F, Joshi A, Oyegbile Y, et al. A randomized Phase I bioequivalence clinical trial of a paediatric fixed-dose combination antiretroviral reconstitutable suspension in healthy adult volunteers. Antivir Ther 2013;18:205-12
  • Monif T, Reyar S, Tiwari HK, et al. A single-dose, randomized, open-label, two-period crossover bioequivalence study comparing a fixed-dose pediatric combination of lamivudine and stavudine tablet for oral suspension with individual liquid formulations in healthy adult male volunteers. Arzneimittelforschung 2009;59:104-8
  • Monif T, Rao Thudi N, Koundinya Tippabhotla S, et al. A single-dose, randomized, open-label, two-period crossover bioequivalence study of a fixed-dose pediatric combination of lamivudine 40-mg, nevirapine 70-mg, and stavudine 10-mg tablet for oral suspension with individual liquid formulations in healthy adult male volunteers. Clin Ther 2007;29:2677-84
  • Piana C, Zhao W, Adkison K, et al. Covariate effects and population pharmacokinetics of lamivudine in HIV-infected children. Br J Clin Pharmacol 2014;77(5):861-72
  • Rhee EG, Rizk ML, Brainard DM, et al. A pharmacokinetic comparison of adult and pediatric formulations of raltegravir in healthy adults. Antivir Ther 2014. [Epub ahead of print]
  • Hartman NR, Yarchoan R, Pluda JM, et al. Pharmacokinetics of 2’,3’-dideoxyinosine in patients with severe human immunodeficiency infection. II. The effects of different oral formulations and the presence of other medications. Clin Pharmacol Ther 1991;50:278-85
  • Damle BD, Kaul S, Behr D, et al. Bioequivalence of two formulations of didanosine, encapsulated enteric-coated beads and buffered tablet, in healthy volunteers and HIV-infected subjects. J Clin Pharmacol 2002;42:791-7
  • Burger D, Meenhorst P, Mulder J, et al. Substitution of didanosine sachets by chewable tablets: a pharmacokinetic study in patients with AIDS. J Acquir Immune Defic Syndr Hum Retrovirol 1995;10:163-8
  • Zucman D, Camara S, Gravisse J, et al. Generic antiretroviral drugs in developing countries: friends or foes? AIDS 2014;28:607-9
  • Kaeser B, Charoin JE, Gerber M, et al. Assessment of the bioequivalence of two nelfinavir tablet formulations under fed and fasted conditions in healthy subjects. Int J Clin Pharmacol Ther 2005;43:154-62
  • Merck Sharp & Dohme Corp; Isentress®. Label information. Available from: www.accessdata.fda.gov/Scripts/cder/DrugsatFDA/ [Last accessed 11 September 2013]
  • Kaul S, Ji P, Lu M, et al. Bioavailability in healthy adults of efavirenz capsule contents mixed with a small amount of food. Am J Health Syst Pharm 2010;67:217-22
  • King J, McCall M, Cannella A, et al. A randomized crossover study to determine relative bioequivalence of tenofovir, emtricitabine, and efavirenz (Atripla) fixed-dose combination tablet compared with a compounded oral liquid formulation derived from the tablet. J Acquir Immune Defic Syndr 2011;56:e130-2
  • Kakuda TN, Berckmans C, De Smedt G, et al. Single-dose pharmacokinetics of pediatric and adult formulations of etravirine and swallowability of the 200-mg tablet: results from three Phase 1 studies. Int J Clin Pharmacol Ther 2013;51:725-37
  • Best BM, Capparelli EV, Diep H, et al. Pharmacokinetics of lopinavir/ritonavir crushed versus whole tablets in children. J Acquir Immune Defic Syndr 2011;58:385-91
  • Innes S, Norman J, Smith P, et al. Bioequivalence of dispersed stavudine: opened versus closed capsule dosing. Antivir Ther 2011;16:1131-4
  • Mathias AA, Hinkle J, Menning M, et al. Bioequivalence of efavirenz/emtricitabine/tenofovir disoproxil fumarate single-tablet regimen. J Acquir Immune Defic Syndr 2007;46:167-73
  • Klein CE, Chiu YL, Awni W, et al. The tablet formulation of lopinavir/ritonavir provides similar bioavailability to the soft-gelatin capsule formulation with less pharmacokinetic variability and diminished food effect. J Acquir Immune Defic Syndr 2007;44:401-10
  • Mooij MG, de Koning BA, Huijsman ML, et al. Ontogeny of oral drug absorption processes in children. Expert Opin Drug Metab Toxicol 2012;8:1293-303
  • Batchelor HK, Kendall R, Desset-Brethes S, et al. Application of in vitro biopharmaceutical methods in development of immediate release oral dosage forms intended for paediatric patients. Eur J Pharm Biopharm 2013;85:833-42
  • Charkoftaki G, Dokoumetzidis A, Valsami G, et al. Elucidating the role of dose in the biopharmaceutics classification of drugs: the concepts of critical dose, effective in vivo solubility, and dose-dependent BCS. Pharm Res 2012;29:3188-98
  • Rinaki E, Valsami G, Macheras P. Quantitative biopharmaceutics classification system: the central role of dose/solubility ratio. Pharm Res 2003;20:1917-25
  • PENTA Steering Committee. PENTA 2009 guidelines for the use of antiretroviral therapy in paediatric HIV-1 infection. HIV Med 2009;10:591-613
  • Nahirya-Ntege P, Cook A, Vhembo T, et al. Young HIV-infected children and their adult caregivers prefer tablets to syrup antiretroviral medications in Africa. PLoS One 2012;7:e36186
  • Chittick GE, Gillotin C, McDowell JA, et al. Abacavir: absolute bioavailability, bioequivalence of three oral formulations, and effect of food. Pharmacotherapy 1999;19:932-42
  • Jullien V, Urien S, Chappuy H, et al. Abacavir pharmacokinetics in human immunodeficiency virus-infected children ranging in age from 1 month to 16 years: a population analysis. J clin Pharmacol 2005;45:257-64
  • Zhao W, Piana C, Danhof M, et al. Population pharmacokinetics of abacavir in infants, toddlers and children. Br J clin Pharmacol 2013;75:1525-35
  • L’Homme R F, Dijkema T, Warris A, et al. Pharmacokinetics of two generic fixed-dose combinations for HIV-infected children (Pedimune Baby & Pedimune Junior) are similar to the branded products in healthy adults. J Antimicrob Chemother 2007;59:92-6
  • Jullien V, Rais A, Urien S, et al. Age-related differences in the pharmacokinetics of stavudine in 272 children from birth to 16 years: a population analysis. Br J clin Pharmacol 2007;64:105-9
  • Drew RH, Weller S, Gallis HA, et al. Bioequivalence assessment of zidovudine (Retrovir) syrup, solution, and capsule formulations in patients infected with human immunodeficiency virus. Antimicrob Agents Chemother 1989;33:1801-3
  • Fauchet F, Treluyer JM, Frange P, et al. Population pharmacokinetics study of recommended zidovudine doses in HIV-1-infected children. Antimicrob Agents Chemother 2013;57:4801-8
  • Hugen PW, Burger DM, ter Hofstede HJ, et al. Development of an indinavir oral liquid for children. Am J Health Syst Pharm 2000;57:1332-9
  • Jullien V, Urien S, Hirt D, et al. Population analysis of weight-, age-, and sex-related differences in the pharmacokinetics of lopinavir in children from birth to 18 years. Antimicrob Agents Chemother 2006;50:3548-55
  • Rakhmanina N, van den Anker J, Baghdassarian A, et al. Population pharmacokinetics of lopinavir predict suboptimal therapeutic concentrations in treatment-experienced human immunodeficiency virus-infected children. Antimicrob Agents Chemother 2009;53:2532-8
  • Regazzi MB, Seminari E, Villani P, et al. Nelfinavir suspension obtained from nelfinavir tablets has equivalent pharmacokinetic profile. J Chemother 2001;13:569-74
  • Marier JF, Borges M, Plante G, et al. Bioequivalence of abacavir generic and innovator formulations under fasting and fed conditions. Int J Clin Pharmacol Ther 2006;44:284-91
  • Schramm Andrade S, Kano EK, de Lima Souza Brioschi TM, et al. Bioavailability study of two oral formulations of didanosine in healthy volunteers. Arzneimittelforschung 2006;56:359-64
  • Estrela Rde C, Salvadori MC, Raices RS, et al. Determination of didanosine in human serum by on-line solid-phase extraction coupled to high-performance liquid chromatography with electrospray ionization tandem mass spectrometric detection: application to a bioequivalence study. J Mass Spectrom 2003;38:378-85
  • Kano EK, dos Reis Serra CH, Koono EE, et al. Determination of lamivudine in human plasma by HPLC and its use in bioequivalence studies. Int J Pharm 2005;297:73-9
  • Narang VS, Lulla A, Malhotra G, et al. Pharmacokinetic profiling and bioequivalence evaluation of 2 lamivudine tablet formulations after single oral administration in healthy human Indian volunteers. J Acquir Immune Defic Syndr 2005;38:566-9
  • Santos-Magalhaes NS, Pontes A, Cavalcante RM, et al. Bioequivalence of two lamivudine tablet formulations. Arzneimittelforschung 2001;51:310-14
  • Bahrami G, Mirzaeei S, Kiani A, et al. High-performance liquid chromatographic determination of lamivudine in human serum using liquid-liquid extraction; application to pharmacokinetic studies. J Chromatogr B Analyt Technol Biomed Life Sci 2005;823:213-17
  • Monif T, Tippabhotla SK, Garg M, et al. Comparative bioavailability/bioequivalence of two different stavudine 40 mg capsule formulations: a randomized, 2-way, crossover study in healthy volunteers under fasting condition. Int J Clin Pharmacol Ther 2007;45:469-74
  • Narang VS, Lulla A, Malhotra G, et al. Bioequivalence evaluation of two marketed brands of stavudine 40 mg capsules in healthy human South African volunteers. Pharmacol Res 2004;50:511-16
  • Raices RS, Salvadori MC, de Cassia EER, et al. Determination of stavudine in human serum by on-line solid-phase extraction coupled to high-performance liquid chromatography with electrospray ionization tandem mass spectrometry: application to a bioequivalence study. Rapid Commun Mass Spectrom 2003;17:1611-18
  • Yerino GA, Halabe EK, Zini E, et al. Bioequivalence study of two oral tablet formulations containing tenofovir disoproxil fumarate in healthy volunteers. Arzneimittelforschung 2011;61:55-60
  • Yadav M, Mishra T, Singhal P, et al. Rapid and specific liquid chromatographic tandem mass spectrometric determination of tenofovir in human plasma and its fragmentation study. J Chromatogr Sci 2009;47:140-8
  • Dos Reis Serra CH, Mori Koono EE, Kano EK, et al. Bioequivalence and pharmacokinetics of two zidovudine formulations in healthy Brazilian volunteers: an open-label, randomized, single-dose, two-way crossover study. Clin Ther 2008;30:902-8
  • Chompootaweep S, Poonsrisawat J, Xumseang P. Evaluation of the bioequivalence of zidovudine 100 mg capsules in healthy Thai male volunteers. J Med Assoc Thai 2006;89(Suppl 3):S79-85
  • Marier JF, Manthos H, Kebir S, et al. Comparative bioavailability study of zidovudine administered as two different tablet formulations in healthy adult subjects. Int J Clin Pharmacol Ther 2006;44:240-6
  • Marier JF, Morin I, Al-Numani D, et al. Comparative bioavailability of a generic capsule formulation of the reverse transcriptase inhibitor efavirenz and the innovator product. Int J Clin Pharmacol Ther 2006;44:180-4
  • Laurito TL, Santagada V, Caliendo G, et al. Nevirapine quantification in human plasma by high-performance liquid chromatography coupled to electrospray tandem mass spectrometry. Application to bioequivalence study. J Mass Spectrom 2002;37:434-41
  • Narang VS, Lulla A, Malhotra G, et al. Pharmacokinetic profiling and bioequivalence assessment of two marketed brands of nevirapine tablets in healthy Indian volunteers. Arzneimittelforschung 2005;55:598-603
  • Zhu Y, Zhang Q, Yu C, et al. Relative bioavailability of two formulations of nevirapine 200-mg tablets in healthy Chinese male volunteers: a single-dose, randomized-sequence, open-label, two-way crossover study. Clin Ther 2010;32:2258-64
  • Tarinas A, Tapanes RD, Gonzalez D, et al. Bioequivalence study of two nevirapine tablet formulations in human-immunodeficiency-virus-infected patients. Farm Hosp 2007;31:165-8
  • Yadav M, Trivedi V, Upadhyay V, et al. Comparison of extraction procedures for assessment of matrix effect for selective and reliable determination of atazanavir in human plasma by LC-ESI-MS/MS. J Chromatogr B Analyt Technol Biomed Life Sci 2012;885-886:138-49
  • Gupta A, Singhal P, Shrivastav PS, et al. Application of a validated ultra performance liquid chromatography-tandem mass spectrometry method for the quantification of darunavir in human plasma for a bioequivalence study in Indian subjects. J Chromatogr B Analyt Technol Biomed Life Sci 2011;879:2443-53
  • Chulavatnatol S, Malathum K, Kiertiburanakul S, et al. Bioequivalence of indinavir capsules in healthy volunteers. Asian Biomed 2010;4:98-101
  • Zala C, Alexander CS, Ochoa C, et al. Comparable pharmacokinetics of generic indinavir (Inhibisam) versus brand indinavir (Crixivan) when boosted with ritonavir. J Acquir Immune Defic Syndr 2005;38:363-4
  • Tippabhotla SK, Thudi NR, Raghuvanshi R, et al. A bioequivalence study comparing two formulations of lopinavir/ritonavir capsules. Int J Clin Pharmacol Ther 2008;46:204-10
  • Chachad S, Lulla A, Malhotra G, et al. Bioequivalence study of two fixed dose combination tablet formulations of lopinavir and ritonavir in healthy volunteers. Arzneimittelforschung 2009;59:263-8
  • Das Mishra T, Kurani H, Singhal P, et al. Simultaneous quantitation of HIV-protease inhibitors ritonavir, lopinavir and indinavir in human plasma by UPLC-ESI-MS-MS. J Chromatogr Sci 2012;50:625-35
  • Ramautarsing RA, van der Lugt J, Gorowara M, et al. Neither branded nor generic lopinavir/ritonavir produces adequate lopinavir concentrations at a reduced dose of 200/50 mg twice daily. J Acquir Immune Defic Syndr 2012;59:55-8
  • Hull MW, Harris M, Lima V, et al. Lopinavir/ritonavir pharmacokinetics in a substitution of high-dose soft-gelatin capsule to tablet formulation. J Clin Pharmacol 2009;49:155-61
  • van der Lugt J, Lange J, Avihingsanon A, et al. Plasma concentrations of generic lopinavir/ritonavir in HIV type-1-infected individuals. Antivir Ther 2009;14:1001-4
  • Puthanakit T, Chokephaibulkit K, Suntarattiwong P, et al. Therapeutic drug monitoring of lopinavir in human immunodeficiency virus-infected children receiving adult tablets. Pediatr Infect Dis J 2010;29:79-82
  • Ramautarsing RA, van der Lugt J, Gorowara M, et al. Pharmacokinetics and 48-week safety and efficacy of generic lopinavir/ritonavir in Thai HIV-infected patients. Antivir Ther 2013;18:249-52
  • Derakhshandeh K, Sohrabi A. Pharmacokinetic study and comparative bioavailability of two nelfinavir tablet formulations in Iranian healthy volunteers after a low-dose administration. Int J Clin Pharmacol Ther 2009;47:491-8
  • Bittner B, Riek M, Holmes B, et al. Saquinavir 500 mg film-coated tablets demonstrate bioequivalence to saquinavir 200 mg hard capsules when boosted with twice-daily ritonavir in healthy volunteers. Antivir Ther 2005;10:803-10
  • Winston A, Mallon PWG, Satchell C, et al. The safety, efficacy and pharmacokinetic profile of a switch in antiretroviral therapy to saquinavir, ritonavir, and atazanavir alone for 48 weeks and a switch in the saquinavir formulation. Clin Infect Dis 2007;44:1475-83
  • Yerino GA, Halabe EK, Zini E, et al. Bioequivalence study of two oral tablet formulations containing saquinavir mesylate boosted with ritonavir in healthy male subjects. Arzneimittelforschung 2011;61:481-7
  • Yuen GJ, Lou Y, Thompson NF, et al. Abacavir/lamivudine/zidovudine as a combined formulation tablet: bioequivalence compared with each component administered concurrently and the effect of food on absorption. J Clin Pharmacol 2001;41:277-88
  • Cremieux AC, Katlama C, Gillotin C, et al. A comparison of the steady-state pharmacokinetics and safety of abacavir, lamivudine, and zidovudine taken as a triple combination tablet and as abacavir plus a lamivudine-zidovudine double combination tablet by HIV-1-infected adults. Pharmacotherapy 2001;21:424-30
  • Narang VS, Lulla A, Malhotra G, et al. A combined-formulation tablet of lamivudine/nevirapine/stavudine: bioequivalence compared with concurrent administration of lamivudine, nevirapine, and stavudine in healthy Indian subjects. J Clin Pharmacol 2005;45:265-74
  • Byakika-Kibwika P, Lamorde M, Kalemeera F, et al. Steady-state pharmacokinetic comparison of generic and branded formulations of stavudine, lamivudine and nevirapine in HIV-infected Ugandan adults. J Antimicrob Chemother 2008;62:1113-17
  • Byakika-Tusiime J, Chinn LW, Oyugi JH, et al. Steady state bioequivalence of generic and innovator formulations of stavudine, lamivudine, and nevirapine in HIV-infected Ugandan adults. PLoS One 2008;3:e3981
  • Hosseinipour MC, Corbett AH, Kanyama C, et al. Pharmacokinetic comparison of generic and trade formulations of lamivudine, stavudine and nevirapine in HIV-infected Malawian adults. AIDS 2007;21:59-64
  • Monif T, Tippabhotla SK, Garg M, et al. Nevirapine/lamivudine/stavudine as a combined-formulation tablet: bioequivalence study compared with each component administered concurrently under fasting condition. Int J Clin Pharmacol Ther 2006;44:276-83
  • Marier JF, Dimarco M, Guilbaud R, et al. Pharmacokinetics of lamivudine, zidovudine, and nevirapine administered as a fixed-dose combination formulation versus coadministration of the individual products. J Clin Pharmacol 2007;47:1381-9
  • Vezina HE, Henry K, Ravindran GD, et al. A randomized crossover study to determine bioequivalence of generic and brand name nevirapine, zidovudine, and lamivudine in HIV-negative women in India. J Acquir Immune Defic Syndr 2006;41:131-6
  • Chachad S, Lulla A, Malhotra G, et al. Bioequivalence evaluation of a fixed dose combination lamivudine + stavudine tablet with concurrent administration of lamivudine tablet and stavudine capsule in healthy volunteers. Arzneimittelforschung 2009;59:537-40
  • Wattananat T, Prasanchaimontri IO, Akarawut W. Simultaneous determination of stavudine and lamivudine in human plasma by high performance liquid chromatography and its application to a bioavailability study. Southeast Asian J Trop Med Public Health 2010;41:369-77
  • Feleder Ethel C, Yerino Gustavo A, Halabe Emilia K, et al. Single-dose bioequivalence of a new fixed-dose combination tablet containing tenofovir disoproxil fumarate and lamivudine. J Bioequiv Availab 2011;3:236-43
  • Moore KH, Shaw S, Laurent AL, et al. Lamivudine/zidovudine as a combined formulation tablet: bioequivalence compared with lamivudine and zidovudine administered concurrently and the effect of food on absorption. J Clin Pharmacol 1999;39:593-605
  • Estrela Rde C, Salvadori MC, Suarez-Kurtz G. A rapid and sensitive method for simultaneous determination of lamivudine and zidovudine in human serum by on-line solid-phase extraction coupled to liquid chromatography/tandem mass spectrometry detection. Rapid Commun Mass Spectrom 2004;18:1147-55
  • Kayitare E, Vervaet C, Ntawukulilyayo JD, et al. Development of fixed dose combination tablets containing zidovudine and lamivudine for paediatric applications. Int J Pharm 2009;370:41-6

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