Introduction: The in vitro-in vivo pharmacokinetic correlation\nmodels (IVIVC) are a fundamental part of the drug discovery and\ndevelopment process. The ability to accurately predict the in vivo\npharmacokinetic profile of a drug based on in vitro observations can\nhave several applications during a successful development process.\nObjective: To develop a comprehensive model to predict the in vivo\nabsorption of antiretroviral drugs based on permeability studies, in\nvitro and in vivo solubility and demonstrate its correlation with the\npharmacokinetic profile in humans.\nMethods: Analytical tools to test the biopharmaceutical properties\nof stavudine, lamivudine y zidovudine were developed. The kinetics\nof dissolution, permeability in caco-2 cells and pharmacokinetics of\nabsorption in rabbits and healthy volunteers were evaluated.\nResults: The cumulative areas under the curve (AUC) obtained in\nthe permeability study with Caco-2 cells, the dissolution study and\nthe pharmacokinetics in rabbits correlated with the cumulative AUC\nvalues in humans. These results demonstrated a direct relation between\nin vitro data and absorption, both in humans and in the in vivo model.\nConclusions: The analytical methods and procedures applied to the\ndevelopment of an IVIVC model showed a strong correlation among\nthemselves. These IVIVC models are proposed as alternative and cost/\neffective methods to evaluate the biopharmaceutical properties that\ndetermine the bioavailability of a drug and their application includes\nthe development process, quality assurance, bioequivalence studies\nand pharmacosurveillance.
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