Integrating drug permeability with dissolution profile to develop IVIVC

Biopharmaceutics & Drug Disposition
Ryusuke TakanoShinji Yamashita

Abstract

In this review article, three different approaches to predict in vivo oral absorption based on the in vitro data of drug permeability, solubility and dissolution were introduced. At the drug discovery stage, the absorption potential of each candidate is most important to select better compounds for further development. The concept of maximum absorbable dose is applied widely, not only to evaluate the absorption potential but also to elucidate the rate-limiting process of oral absorption that helps us to understand the cause of poor absorption. To integrate the permeability of the drug with its dissolution profile, two different approaches, in vitro dissolution/permeation system (D/P system) and in silico model and simulation method, are proposed. In the D/P system, by mimicking the in vivo process of drug absorption, the permeated amount of drugs, that is the total output of dissolution and permeation processes, are correlated with the fraction absorbed in human (F(a)). This system is powerful for evaluating the improved absorption by various formulations and the effect of food intake. On the other hand, in the model and simulation approach, an intrinsic dissolution parameter of drug particle, z, was extracted from the small sc...Continue Reading

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Citations

Feb 24, 2016·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Amal Al DurdunjiMutasim Al-Ghazawi
Dec 17, 2015·The AAPS Journal·Alison MargolskeeLeon Aarons
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Sep 29, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Serena BertoniNadia Passerini
Feb 22, 2021·Advanced Drug Delivery Reviews·Zahari VinarovPatrick Augustijns

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