In vitro-in vivo Pharmacokinetic correlation model for quality assurance of antiretroviral drugs
Abstract
Introduction: The in vitro-in vivo pharmacokinetic correlation models (IVIVC) are a fundamental part of the drug discovery and development process. The ability to accurately predict the in vivo pharmacokinetic profile of a drug based on in vitro observations can have several applications during a successful development process.
Objective: To develop a comprehensive model to predict the in vivo absorption of antiretroviral drugs based on permeability studies, in vitro and in vivo solubility and demonstrate its correlation with the pharmacokinetic profile in humans.
Methods: Analytical tools to test the biopharmaceutical properties of stavudine, lamivudine y zidovudine were developed. The kinetics of dissolution, permeability in caco-2 cells and pharmacokinetics of absorption in rabbits and healthy volunteers were evaluated.
Results: The cumulative areas under the curve (AUC) obtained in the permeability study with Caco-2 cells, the dissolution study and the pharmacokinetics in rabbits correlated with the cumulative AUC values in humans. These results demonstrated a direct relation between in vitro data and absorption, both in humans and in the in vivo model.
Conclusions: The analytical methods and procedures applied to the development of an IVIVC model showed a strong correlation among themselves. These IVIVC models are proposed as alternative and cost/effective methods to evaluate the biopharmaceutical properties that determine the bioavailability of a drug and their application includes the development process, quality assurance, bioequivalence studies and pharmacosurveillance.
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Ministerio de Protección Social, Colombia Ley 84 de 1989 y la Resolución 008430 de 1993.
WHO Regional Publications Eastern Mediterranean Series 30. Practical Guide for Health Researchers, 2004.
Amidon KS, Langguth P, Lennernäs ,Yu H, L, and Amidon GL. Bioequivalence of Oral Products and the Biopharmaceutics Classification System. Clin Pharmacol Ther. 90(3): 467–470, 2011. Disponible en:http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3228645/ pdf/nihms337891.pdf
Joseph M. Custodio, Chi-Yuan Wu, Leslie Z. Benet. Predicting Drug Disposition, Absorption / Elimination / Transporter Interplay And The Role Of Food On Drug Absorption. Published in final edited form as: Adv Drug Deliv Rev. 17; 60(6): 717–733. March 2008. Disponible en: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2292816
World Health Organization. Lamivudine. Final text for addition to The International Pharmacopoeia. Document QAS/05.124/Final. March. 2006. Disponible en: http://www.who.int/medicines/publications/pharmacopoeia/QAS_124rev2_Lamivudine.monoFINAL.pdf
Strauch S., Jantratid E., Dressman J. B. et al. Biowaiver Monographs for immediate release Solid Oral Dosage Forms: Lamivudine. Journal of Pharmaceutical Sciences, Vol. 100, 2054-2063 .2011. Disponible en: http://www.fip.org/files/fip/BPS/BCS/Monographs/ Lamivudine.pdf
National Institutes of Health, Health & Human Services. U.S. National Library of Medicine. Retrovir (zidovudine). [ViiV Healthcare Company]. Current Medication Information, Daily Med. Revised: December 2011. Disponible en: http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=360d8a6d-d3b6-43ef-8764-e99d83 1880a4#nlm34089-3
National Institutes of Health, Health & Human Services. U.S. National Library of Medicine. Stavudine capsule [Mylan Pharmaceuticals Inc.]. Current Medication Information, Daily Med. Revised: January 2012. Disponible en: http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=4794e7be-fb7b-d396-aeb3-9939b7 f57987#nlm34089-3
World Health Organization. Expert Committee on Specifications for Pharmaceutical Preparations. WHO Technical Report Series. 937, Fortieth Report. 2006. Disponible en: http://whqlibdoc.who.int/trs/WHO_TRS_937_eng.pdf
U.S. Department of Health and Human Services. Food and Drug Administration.Office of Generic Drugs Division of Bioequivalence Update Frequency: Quarterly. Dissolution Methods Disclaimer. Data Current through: January 11, 2010. Disponible en en: http://www.accessdata.fda.gov/scripts/cder/dissolution/dsp_SearchResults_Dissolutions.cfm
World Health Organization.Lamivudine.Final text for addition to The International Pharmacopoeia.Document QAS/05.124/Final. March. 2006. Disponible en: http://www.who.int/medicines/publications/pharmacopoeia/QAS_124rev2_Lamivudine.monoFINAL.pdf
Strauch S., Jantratid E., Dressman J. B. et al. Biowaiver Monographs for immediate release Solid Oral Dosage Forms: Lamivudine. Journal of Pharmaceutical Sciences, Vol. 100, 2054-2063 .2011. Disponible en: http://www.fip.org/files/fip/BPS/BCS/Monographs/ Lamivudine.pdf
National Institutes of Health, Health & Human Services.U.S. National Library of Medicine.Retrovir (zidovudine). [ViiV Healthcare Company]. Current Medication Information, Daily Med. Revised: December 2011. Disponible en: http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=360d8a6d-d3b6-43ef-8764-e99d83 1880a4#nlm34089-3
National Institutes of Health, Health & Human Services.U.S. National Library of Medicine. Stavudine capsule [Mylan Pharmaceuticals Inc.]. Current Medication Information, Daily Med. Revised: January 2012. Disponible en: http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=4794e7be-fb7b-d396-aeb3-9939b7 f57987#nlm34089-3
World Health Organization.Expert Committee on Specifications for Pharmaceutical Preparations. WHO Technical Report Series. 937, Fortieth Report. 2006. Disponible en: http://whqlibdoc.who.int/trs/WHO_TRS_937_eng.pdf
Corti G, Maestrelli F, Cirri M, Zerrouk N, Mura P. Development and evaluation of an in vitro method for prediction of human drug absorption II. Demonstration of the method suitability. Eur J Pharm Sci.; 27(4):354-62. Mar 2006
U.S. Food and Drug Administration. Center for Drug Evaluation and Research. Guidance for the industry. Bioanalytical Method Validation. May. 2001. http://www.fda.gov/downloads/Drµgs/GuidanceComplianceRegulatoryInformation/Guidances/UCM070107.pdf
Artursson Per, Palm K., Luthman K.Caco-2 monolayers in experimental and theoretical predictions of drug transport. Volume 46, Issues 1–3, 1, Pages 27–43. March 2001
Volpe Donna A. Application of Method Suitability for Drug Permeability Classification.The AAPS Journal, Vol. 12, No. 4,. DOI: 10.1208/s12248-010-9227-8. December 2010 Disponible en: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2976984/ pdf/12248_2010_Article_9227.pdf
U.S. Department of Health and Human. Services Food and Drug Administration Center for Drug Evaluation and Research (CDER). Waiver of In Vivo Bioavailability and Bioequivalence Studies for Immediate-Release Solid Oral Dosage Forms Based on a Biopharmaceutics Classification System. August 2000. Disponible en: http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/ucm070246.pdf
EuropeanMedicines Agency. Committee for Medicinal Products for Human Use (CHMP). Guideline on the Investigation of Bioequivalence. Doc. Ref.: CPMP/EWP/QWP/1401/98 Rev. 1/ Corr ** London, 20 January 2010. Disponible en: http://www.emea.europa.eu/docs/en_GB/document_library/Scientific_guideline/2010/01/WC500070039.pdf
Polli J.E., Abrahamsson B.S.I., Yu L.X., Amidon G.L. et al. Summary Workshop Report: Bioequivalence, Biopharmaceutics Classification System, and Beyond. The AAPS Journal, Vol. 10, No. 2, (# 2008). DOI: 10.1208/s12248-008-9040-9. June 2008. Disponible en: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2976984/pdf/12248_2010_ Article_9227.pdf
Palm K., Luthman K.Caco-2 monolayers in experimental and theoretical predictions of drug transport. Volume 46, Issues 1–3, 1, Pages 27–43. March 2001
Kumar.K.V, Swathi Karnati, Mamatha Reddy.B and Chandramouli.R. Caco-2 Cell Lines in Drug Discovery - An Updated Perspective. Journal of Basic and Clinical Pharmacy. Vol-001 Issue-002 March 2010 – May 2010. Disponible en: http://www.jbclinpharm.com/Volume1Issue2Articles/PDF/Pr_14.pdf)
The Nacional Academies.Science, Medicine and Animals.Committee to Update Science, Medicine and Animals.National Research Council. 2004
U.S. Department of Health and Human Services.ACPS Meeting Achieving and demonstrating “Quality by Design” with respect to drug release/dissolution performance for conventional or immediate release solid oral dosage forms.October 2005. Disponible en: http://www.fda.gov/OHRMS/DOCKETS/AC/05/briefing/2005-4187B1_01_03-Achieve-Demo - QbD.pdf.
UNDP/World Bank/WHO Special Programme for Research and Training in Tropical Disease (TDR). Good Laboratory Practices Training Manual. 2001
U.S. Department of Health and Human Services.Food and Drug Administration.Center for Drug Evaluation and Research (CDER). Bioavailability and Bioequivalence Studies for Orally Administered Drug Products — General Considerations. Guidance for Industry. March 2003. Documento electrónico: http://www.fda.gov/cder/guidance/index.htm.
WHO. Marketing Authorization of Pharmaceutical Products with Special Reference to Multisource (generics) Products: A Manual For Drug Regulatory Authorities. WHO/DMP/RGS/98.5. 1998. Disponible en: http://apps.who.int/medicinedocs/en/d/ Js2273e/
The European Agency for the Evaluation of Medicinal Products.Evaluation of Medicines for Human Use. Note for guidance on Investigation of bioavailability and Bioequivalence. December 2000 http://www.emea.europa.eu/pdfs/human/qwp/ 140198en.pdf.
Políticas de la Asociación Médica Mundial. Declaración de la Asociación Médica Mundial sobre el Uso de Animales en la Investigación Biomédica. Hong Kong. 1989
Tempelman Robert. Bioequivalence Testing en Animal Sciences.Department of Animal Science. Michigan State University, USA
U.S. Department of Health and Human Services.Food and Drug Administration.Center for Drug Evaluation and Research (CDER). Waiver of In Vivo Bioavailability and Bioequivalence Studies for Inmediate Release Solid Oral Dosage Forms Based on a Bipharmaceuticas Classification Systems. August 2000
Khandave SS, Onkar SV, Sawant SV and Joshi SS. Evaluation of Performance of the Truncated Area Under Curve (AUC) as a Primary Pharmacokinetic Parameter in Bioequivalence Studies. J Bioequiv Availab 2: 077-080. doi:10.4172/jbb.1000035 .Volume 2(4): 077-080 (2010) – 077. 2010. Disponible en: http://www.omicsonline.org/ ArchiveJBB/2010/July/01/JBB-02-077.pdf.
Shargel L., Wo-Pongs. and Yub.C. A. Applied Biopharmaceutics And Pharmacokinetics. Fifth Edition.McGraw Hill. United States of America. 2005. ISBN 0-07- 137550-3
World Health Organization. WHO Technical Report Series, No. 937 Annex 8 Proposal to waive in vivo bioequivalence requirements for the WHO Model List of Essential Medicines immediate release, solid oral dosage forms.; 391 - 437. 2006. Disponible en: http://healthtech.who.int/pq/info_general/documents/TRS937/WHO_TRS_937_eng.pdf#page=403.
Panamericana de la Salud. Medicamentos Genéricos. August 2005. Disponible en: http://www.paho.org
U.S. Department of Health and Human Services. Food and Drug Administration.Office of Generic Drugs Division of Bioequivalence Update Frequency: Quarterly. Dissolution Methods Disclaimer. Data Current through: January 11, 2010. Disponible en: http://www.accessdata.fda.gov/scripts/cder/dissolution/dsp_SearchResults_Dissolutions.cfm.
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