Integrating theoretical and experimental permeability estimations for provisional biopharmaceutical classification: Application to the WHO essential medicines

Biopharmaceutics & Drug Disposition
Miguel Ángel Cabrera-PérezYudileidy Brito-Ferrer

Abstract

The accuracy of the provisional estimation of the Biopharmaceutics Classification System (BCS) is heavily influenced by the permeability measurement. In this study, several theoretical and experimental models currently employed for BCS permeability classification have been analysed. The experimental models included the in situ rat intestinal perfusion, the ex vivo rat intestinal tissue in an Ussing chamber, the MDCK and Caco-2 cell monolayers, and the parallel artificial membrane (PAMPA). The theoretical models included the octanol-water partition coefficient and the QSPeR (Quantitative Structure-Permeability Relationship) model recently developed. For model validation, a dataset of 43 compounds has been recompiled and analysed for the suitability for BCS permeability classification in comparison with the use of human intestinal absorption and oral bioavailability values. The application of the final model, based on a majority voting system showed a 95.3% accuracy for predicting human permeability. Finally, the present approach was applied to the 186 orally administered drugs in immediate-release dosage forms of the WHO Model List of Essential Medicines. The percentages of the drugs that were provisionally classified as BCS Cla...Continue Reading

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Citations

Dec 1, 2018·Current Topics in Medicinal Chemistry·Hai Pham-TheGerardo M Casañola-Martin
Jul 3, 2019·International Journal of Molecular Sciences·Cheng-Ting ChiMax K Leong
Jul 1, 2020·Therapeutic Innovation & Regulatory Science·Claudia Miranda-Pérez de AlejoMiguel Ángel Cabrera-Pérez

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