Formulation strategies to improve the bioavailability of poorly absorbed drugs

  1. Espinar, Francisco Javier Otero
  2. Lavilla, Carlos Bendicho
  3. Fernández, Guillermo Blanco
  4. Tomé, Victoria Díaz
  5. Otero, Xurxo García
Libro:
Dosage Forms, Formulation Developments and Regulations: Recent and Future Trends in Pharmaceutics, Volume 1

ISBN: 9780323918176

Ano de publicación: 2024

Páxinas: 223-255

Tipo: Capítulo de libro

DOI: 10.1016/B978-0-323-91817-6.00008-5 GOOGLE SCHOLAR lock_openAcceso aberto editor

Resumo

One of the most frequent causes for discarding new drug molecules in the first phases of early drug discovery is their poor bioavailability. The pharmaceutical R&D researcher must also frequently deal with drug molecules that exhibit poor bioavailability.The two principal causes of drug bioavailability issues are the low drug solubility and dissolution rate in the aqueous biological media surrounding the absorption membranes or the poor drug permeability across membrane barriers.Biopharmaceutical Classification System (BCS) is a classification developed to identify the causes of drug bioavailability issues. BCS class II includes drugs with solubility problems, class III with permeability issues, and class IV with both low solubility and low permeability. To successfully approach the formulation of drugs included in BCS class II–IV, it is necessary to know the specific causes of the low solubility or permeability of the drug. Based on this knowledge, formulation scientists can properly select the best strategies to increase the bioavailability of drugs.This chapter addresses the causes of low drug bioavailability, as well as the tools and strategies that formulators have to enhance the bioavailability of drugs with low absorption.

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